Med-Chemist

Could 'Magic' Mushrooms Ease Depression?

2012-01-27T07:00:00.000+05:30

Psychedelic mushrooms (see above picture) may point to new ways to treat depression, suggest two small brain imaging studies that seem to show how psilocybin (see right structure) the active ingredient in such mushrooms -affects the brain.

One study included 30 healthy people who had psilocybin inserted into their blood while magnetic resonance imaging (MRI) scanners measured changes in their brain activity. The scans revealed that psilocybin caused decreased activity in what the researchers described as the brain's "hub" regions -- areas especially well-connected with other areas.

The second study included 10 healthy volunteers and found that psilocybin boosted their recall of personal memories and their emotional well-being for up to two weeks. The researchers said this suggests that psilocybin might prove useful as an adjunct to psychotherapy.

"Psychedelics are thought of as 'mind-expanding' drugs, so it has commonly been assumed that they work by increasing brain activity, but surprisingly, we found that psilocybin actually caused activity to decrease in areas that have the densest connections with other areas," Nutt said....

Researchers lead by Dr.David Nutt, add that result is consistent with earlier finding that psilocybin decreases mPFC activity, as many effective depression treatments do. The effects need to be investigated further and this study was only a small study, and are interested in exploring psilocybin's potential as a therapeutic tool.....

Experimental Drug Might Help Some a Bit With Colon Cancer

2012-01-26T07:30:00.000+05:30

In continuation of my update on regorafenib

The experimental cancer drug regorafenib appears to extend survival slightly in patients with metastatic colorectal cancer, a new trial indicates.

Regorafenib is a so-called multikinase inhibitor, which targets several of the ways cancer develops and grows, researchers said.

"The drug was tested on patients with metastatic colorectal cancer who had progressed after standard therapies, meaning they had no treatment options available," lead researcher Dr. Axel Grothey, a professor of oncology at the Mayo Clinic.

The investigators found that patients taking regorafenib survived an average of 6.4 months, compared with five months for those receiving a placebo -- an increase in survival of 29 percent.

In addition, 44 percent of the patients taking regorafenib responded to the drug or had their cancer slowed, compared with 15 percent of the patients receiving placebo, they reported.

Ref : http://gicasym.org/GastrointestinalCancersSymposiumDailyNews/GI385.aspx

New Drug Combo for Hepatitis C Shows Promise...

2012-01-25T07:30:00.000+05:30

A new cocktail of two investigational drugs appears to have successfully cleared the hepatitis C virus in people who don't respond to standard treatment. What's more, the approach seems to work without the need for injections with interferon alpha, an onerous medication that causes serious side effects in many patients.

"We saw a sustained virologic response -- the virus was undetectable in the patients -- during treatment and remained undetectable after the drugs were stopped," said study author Dr. Anna Lok, director of clinical hepatology at the University of Michigan Medical School in Ann Arbor.

The study had two arms: a group of 10 patients received four medications, including the two investigational drugs, the antivirals daclatasvir (see right structure) and asunaprevir (see left structure-courtesy: ChemSpider), along with the standard treatment combination of interferon and ribavirin. The other arm of the study included 11 patients who received only the two investigational drugs. Both groups underwent treatment for 24 weeks.

The 10 patients on the four-drug regimen experienced a sustained virologic response with undetectable virus at the end of treatment and again at 12 weeks beyond their treatment, the researchers reported. In the two-drug group, four of the 11 patients also had undetectable levels of the hepatitis C virus in their blood 12 weeks after treatment ended.

"The four-drug arm was very impressive. These patients had not shown a response before and now we get a 90 to 100 percent rate of sustained response," said Lok....

Ref : http://www.nejm.org/doi/full/10.1056/NEJMoa1104430

More Evidence for Oxaliplatin as Colon Cancer Chemotherapy

2012-01-24T12:50:00.002+05:30

In continuation of my update on Oxaliplatin

Adding oxaliplatin to a standard chemotherapy regimen boosts survival rates for patients with advanced colon cancer, according to a new study that bolsters previous research on the drug by looking at a broader group of patients.

In past studies, oxaliplatin, as an adjuvant to the established treatment of 5-fluorouracil (5-FU), improved survival by up to 23 percent. But the new study looked at a different group of colon cancer patients, who were older, sicker, more racially diverse and had never participated in a controlled clinical study.

To determine whether oxaliplatin would show a similar benefit among a "real-world" population of patients, the authors sifted through five cancer registries containing survival information on more than 4,000 people with stage 3 colon cancer. All were younger than 75, and all had begun chemotherapy -- either a standard regimen or in combination with oxaliplatin -- within four months of having surgery between 2004 and 2009.

Researchers lead by Dr.Hanna K. Sanoff compared their survival rates with those of nearly 8,300 patients who had participated in one of five different clinical trials using oxaliplatin.

The addition of oxaliplatin to standard chemotherapy protocols was found to be just as effective in prolonging survival among the community-based set of patients - including the elderly, minorities and those with additional complicating health issues who were not enrolled in studies.

More....

Voraxaze receives FDA approval for treatment of toxic methotrexate levels

2012-01-19T06:31:00.000+05:30

Voraxaze receives FDA approval for treatment of toxic methotrexate levels: The U.S. Food and Drug Administration today approved Voraxaze (see structure, glucarpidase) to treat patients with toxic levels of methotrexate in their blood due to kidney failure.

Anti-malaria drug synthesised with the help of oxygen and light

2012-01-18T12:48:00.000+05:30

In continuation of my update, artemisinin...

The most effective anti-malaria drug can now be produced inexpensively and in large quantities. This means that it will be possible to provide medication for the 225 million malaria patients in developing countries at an affordable price. Researchers at the Max Planck Institute of Colloids and Interfaces in Potsdam and the Freie Universität Berlin have developed a very simple process for the synthesis of artemisinin, the active ingredient that pharmaceutical companies could only obtain from plants up to now. The chemists use a waste product from current artemisinin production as their starting substance. This substance can also be produced biotechnologically in yeast, which the scientists convert into the active ingredient using a simple yet very ingenious method.....

Look at http://www.mpg.de/4984709/artemisinin_malaria

Dabigatran, New Blood Thinner Linked To Higher Heart Attack Risk

2012-01-11T12:34:00.000+05:30

In continuation of my update on Dabigatran...

Researchers lead by Dr.Ken Uchino from the Cleveland Clinic in Ohio looked at seven trials involving Pradaxa (Dabigatran) that included more than 30,000 patients. This process, called a meta-analysis, uses data from published clinical trials to tease out a pattern that might not show up in a single study. Researchers found Pradaxa was associated with an increased risk of heart attack or acute coronary syndrome (heart attack or angina), compared with two other commonly used blood thinners, warfarin (Coumadin, Jantoven) and enoxaparin (Lovenox).

As per the claim by the researchers, those taking Pradaxa, 1.19 percent had a heart attack or suffered from acute coronary syndrome compared with 0.79 percent of those taking either of the other drugs, they noted. Although there was a 33 percent increase in relative risk for a heart attack among those taking Pradaxa, the absolute increased risk -- that is, the added risk for any one individual of having a heart attack if on Pradaxa -- was 0.27 percent, researchers said.

Pradaxa was approved by the U.S. Food and Drug Administration in October 2010 for people with a common heart rhythm problem called atrial fibrillation. People with atrial fibrillation are at a higher risk for stroke and are often prescribed medication to prevent clotting....

Ref : http://my.clevelandclinic.org/cerebrovascular_center/medical_professionals/clinical_trials.aspx

Idenix Reports Positive Interim Data for HCV Nucleotide Inhibitor, IDX184

2012-01-10T12:32:00.002+05:30

Idenix Pharmaceuticals, Inc. a biopharmaceutical company engaged in the discovery and development of drugs for the treatment of human viral diseases, recently announced interim data from a 12-week phase IIb clinical trial of IDX184, the Company's lead product candidate for the treatment of hepatitis C virus (HCV) infection. IDX184 (below structure), a pan-genotypic oral nucleotide polymerase inhibitor, has demonstrated a high barrier to resistance in vitro and potent antiviral activity in both preclinical and clinical studies..

Following are the highlights .....

No serious adverse events observed in phase IIb study of IDX184; Data Safety Monitoring Board (DSMB) recommends continuation of the clinical trial.
In the 100 mg IDX184 arm, 73% of patients achieved a rapid virologic response (RVR) and 87% were undetectable at most recent visit; In the 50 mg IDX184 arm, 63% of patients achieved an RVR and 94% were undetectable at most recent visit.

More...

Positive Results from Clinical Study of CVT-301, an Inhaled L-dopa for Parkinson’s Disease..

2012-01-07T12:54:00.001+05:30

In continuation of my update on Levodopa....

The Phase 1 study (by Civitas Therapeutics, Inc) showed that CVT-301 achieved sufficient plasma levels of L-dopa through inhaled delivery to the lung, resulting in a pharmacokinetic profile that supports its therapeutic potential. Immediate absorption and dose proportional pharmacokinetics were seen across all doses tested. In addition, all doses tested of CVT-301 were safe and well tolerated.

More....

Ref : http://civitastherapeutics.com/cms/sites/default/files/news/CVT-301%20Clinical%20results%20press%20release%20FINAL%2006Jan2012_0.pdf

Breakthrough in Treatment to Prevent Blindness | www.ucsf.edu

2012-01-05T08:05:00.000+05:30

In continuation of my update on Azithromycin....
Breakthrough in Treatment to Prevent Blindness | www.ucsf.edu

A Novel Neurotrophic Drug for Cognitive Enhancement and Alzheimer's Disease

2012-01-02T13:10:00.000+05:30

A new drug candidate may be the first capable of halting the devastating mental decline of Alzheimer's disease. The drug, known as J147 (above structure), improved memory and prevented brain damage caused by the disease claims the researchers from Salk's Cellular Neurobiology Laboratory, lead by David Schubert. The new compound, could be tested for treatment of the disease in humans in the near future.Researchers add that, J147 enhances memory in both normal and Alzheimer's mice and also protects the brain from the loss of synaptic connections.

Salk researchers went on to show that it prevented cognitive decline in animals with Alzheimer's and that mice and rats treated with the drug produced more of a protein called brain-derived neurotrophic factor (BDNF), a molecule that protects neurons from toxic insults, helps new neurons grow and connect with other brain cells, and is involved in memory formation.

Because of the broad ability of J147 to protect nerve cells, the researchers believe that it may also be effective for treating other neurological disorders, such as Parkinson's disease, Huntington's disease and amyotrophic lateral sclerosis (ALS), as well as stroke.

Although it is yet unknown whether the compound will prove safe and effective in humans, the Salk researchers' say their results suggest the drug may hold potential for treatment of people with Alzheimer's...

Ref : http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0027865

Bristol-Myers Squibb and Tibotec partner to evaluate daclatasvir-TMC435 combination for HCV

2012-01-02T12:07:00.000+05:30

Bristol-Myers Squibb and Tibotec partner to evaluate daclatasvir-TMC435 combination for HCV: Bristol-Myers Squibb Company announced today that it has entered into a clinical collaboration agreement with Tibotec Pharmaceuticals to evaluate the utility of daclatasvir (BMS-790052), Bristol-Myers Squibb's investigational NS5A replication complex inhibitor, in combination with Tibotec Pharmaceuticals' investigational NS3 protease inhibitor, TMC435, for the treatment of chronic hepatitis C virus (HCV).

Alkermes commences ALKS 9070 phase 3 clinical trial for schizophrenia...

2012-01-01T07:00:00.000+05:30

Alkermes plc (NASDAQ: ALKS) announced the initiation of a phase 3 clinical trial of ALKS 9070 (Aripiprazole) for the treatment of schizophrenia. ALKS 9070, a proprietary Alkermes molecule, is designed to provide patients with once-monthly dosing of a medication that, once in the body, converts into aripiprazole...

Ref : http://phx.corporate-ir.net/phoenix.zhtml?c=92211&p=irol-corporateNewsArticle&ID=1640788&highlight=

Lostartan can reduce cigarette smoke-induced lung injury

2011-12-30T12:19:00.000+05:30

Researchers from Johns Hopkins University, BaltimoreLostartan, lead by have found that, Dr.Enid R. Neptune Losartan a drug used widely in the clinic (e.g., to treat high blood pressure), reduced lung disease in mice caused by exposure to cigarette smoke. Losartan blocks the protein angiotensin receptor type 1, and its effects on cigarette smoke-induced lung injury were a result of the fact that blocking angiotensin receptor type 1 leads to a decrease in levels of the soluble molecule TGF-beta. The authors therefore suggest that other TGF-beta-targeted therapeutics might also be viable candidates for the treatment of chronic obstructive pulmonary disease, COPD....

Ref : http://www.jci.org/articles/view/46215?search[article_text]=&search[authors_text]=Enid+Neptune

MK 1775 shows promise against sarcomas..........

2011-12-29T07:30:00.000+05:30

2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6- (4-(4-methyl- piperazin-1-yl)phenylamino)-1H-pyra -zolo [3,4-d]pyrimidin-3(2H)-one.

MK 1775 (see structure), a small, selective inhibitor molecule, has been found to be active against many sarcomas when tested by researchers at Moffitt Cancer Center in Tampa, Fla. Researchers found that MK1775 treatment induces apoptopic cell death in four sarcoma cell lines at clinically relevant doses.

To further prove that inhibition of Wee1 by MK1775 leads to mitotic cell death in sarcomas cells, the researchers performed additional studies, including studies on sarcomas related to mutations, such as with the p53 gene. They also showed that MK1775 was an active inhibitor of Wee1 regardless of the p53 mutation status of the tumors in the cell lines tested.

"The cytotoxic effect of Wee1 inhibition on sarcoma cells appears to be independent of p53 mutation status following our testing sarcoma cell lines with different p53 mutations," he said. "All of them were highly sensitive to MK1775, suggesting that Wee1 inhibition may represent a novel approach in the treatment of sarcomas."

Researchers concluded that their laboratory tests on sarcoma cell lines suggest that MK1775 is effective as a monotherapy even in the cell lines that include p53 wild, p53 null and p53 mutant statuses.

More...

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint

2011-12-28T10:47:00.000+05:30

In continuation of my update on gemcitabine

Oncolytics REOLYSIN-Gemzar combination Phase 2 pancreatic cancer clinical trial meets primary endpoint: Oncolytics Biotech Inc. announced the interim data from a Phase 2 clinical trial using intravenous administration of REOLYSIN® in combination with gemcitabine (Gemzar) in patients with advanced pancreatic cancer (REO 017) indicated that the clinical study had successfully reached its primary endpoint, and that the drug combination is active.

New Antibodies Treat Autoimmune Disease like Crohn's in Mice....

2011-12-27T10:25:00.000+05:30

Synthetic drugs treat (below structure) Crohn's disease in mice.................

[zinc-binding motif (where X is any amino acid) in MMPs, a symmetrical tripodal tris-imidazol–zinc complex (Zn-tripod; ZnC₃₆H₅₉N₁₁O₈)]

New Antibodies Treat Autoimmune Disease in Mice
Ref : http://www.nature.com/nm/journal/vaop/ncurrent/full/nm.2582.html

Salk scientists develop new drug that improves memory and prevents brain damage in mice

2011-12-26T07:30:00.000+05:30

A new drug candidate may be the first capable of halting the devastating mental decline of Alzheimer's disease, based on the findings by a research group of Salk's Cellular Neurobiology Laboratory.

When given to mice with Alzheimer's, the drug, known as J147 (see structure), improved memory and prevented brain damage caused by the disease. The new compound, developed by scientists at the Salk Institute for Biological Studies, could be tested for treatment of the disease in humans in the near future.

"J147 enhances memory in both normal and Alzheimer's mice and also protects the brain from the loss of synaptic connections," says David Schubert, the head of Salk's Cellular Neurobiology Laboratory, whose team developed the new drug. "No drugs on the market for Alzheimer's have both of these properties."

More.....

Notch inhibitor appears to treat breast cancer....

2011-12-25T14:36:00.000+05:30

In a novel therapeutic approach to treating breast cancer, Loyola University Medical Center researchers are reporting positive results from a clinical trial of a drug that targets tumor stem cells. A pilot study at Loyola found that an experimental drug known as a "notch inhibitor" appears to block this process by turning off key genes. Prior to surgery, the patients received one of two commonly used drugs, tamoxifen or letrozole. These drugs work by blocking estrogen stimulation of breast cancer cells. In addition to tamoxifen or letrozole, patients also received the experimental notch-inhibitor drug, MK-0752 (see structure).

"The notch inhibitor appears to be doing what it is intended to do," said Dr. Clodia Osipo....

There were minimal side effects from either the notch inhibitor or the estrogen-blocking drugs. One patient experienced puffy eyes and coughing and four patients experienced facial acne. No patients experienced diarrhea or surgical complications.

Ref : Loyola Medicine News Release

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

2011-12-24T07:30:00.000+05:30

In continuation of my update on Zoledronic acid....

Zoledronic Acid Shows Long-Term Benefit in Survivorship for Premenopausal ER-Positive Breast Cancer

Scientists identify why African naked mole-rat feels no pain when exposed to acid

2011-12-22T14:49:00.001+05:30

In continuation of my update naked mole-rat

Scientists identify why African naked mole-rat feels no pain when exposed to acid: British researchers of the Max Delbr-ck Center for Molecular Medicine (MDC) Berlin-Buch have found out why the African naked mole-rat (Heterocephalus glaber), one of the world's most unusual mammals, feels no pain when exposed to acid.

Ref : http://www.mdc-berlin.de/en/news/2011/20111220-mdc_researchers__ion_channel_makes_african1/index.html

Drug Duo of Ixabepilone and sunitinib Kills Chemotherapy-resistant Ovarian Cancer Cells......

2011-12-20T14:37:00.000+05:30

In continuation of Sunitinib...

The use of two drugs never tried in combination before in ovarian cancer resulted in a 70 percent destruction of cancer cells already resistant to commonly used chemotherapy agents, say researchers at Mayo Clinic in Florida. Research suggests that this combination (ixabepilone and sunitinib), might offer a much needed treatment option for women with advanced ovarian cancer. When caught at late stages, ovarian cancer is often fatal because it progressively stops responding to the chemotherapy drugs used to treat it. The finding also highlights the importance of the role of a molecule, RhoB, that the researchers say is activated by the drug duo. Neither drug is approved for use in ovarian cancer. Ixabepilone is a chemotherapy drug that, like other taxane drugs, targets the microtubules and stops dividing cells from forming a spindle. It has been approved for use in metastatic breast cancer. Sunitinib, approved for use in kidney cancer, belongs to a class of tyrosine kinase inhibitors that stops growth signals from reaching inside cancer cells.

Sunitinib Ixabepilone

Ref : http://www.mayoclinic.org/news2011-jax/6573.html

Geron Initiates Phase 2 Trial of GRN1005 in Brain Metastases from Breast Cancer

2011-12-18T07:30:00.000+05:30

In continuation of my update on Paclitaxel and drug discovery....

Geron Corporation, announced the initiation of GRABM-B (GRN1005 Against Brain Metastases - Breast Cancer), a Phase 2 clinical trial to evaluate GRN1005 in patients with brain metastases arising from breast cancer. GRN1005 is the company's lead LRP-directed peptide-drug conjugate (LRP-directed PDC) that consists of the cytotoxic drug, paclitaxel, linked to a peptide (Angiopep-2) that targets the LRP receptor to cross the blood-brain barrier (BBB) and to target tumors in the brain.

The purpose of the Phase 2 study is to assess the efficacy, safety and tolerability of GRN1005 in patients with brain metastases from breast cancer. The trial is designed to include 100 patients with HER2 positive or HER2 negative metastatic breast cancer (MBC) disease, who will be assessed in two separate cohorts of 50 patients each.....

More...

Ref : http://www.geron.com/media/pressview.aspx?id=1287

Drug combination highly effective for newly diagnosed myeloma patients......

2011-12-17T16:52:00.000+05:30

A three-drug combination treatment for the blood cancer multiple myeloma compares favorably to the best established therapy for newly diagnosed patients, according to a multi-center study led by Andrzej Jakubowiak, MD, PhD, professor of medicine and director of the multiple myeloma program at the University of Chicago Medical Center.

( Carfilzomib)

(Lenalidomide)

( Thalidomide)

The combination includes an investigational medicine called carfilzomib combined with two standard medications: lenalidomide, an analogue of thalidomide, and low-dose dexamethasone, an anti-inflammatory with anti-cancer properties.

"This combination appears to deliver everything we expected and more," said Jakubowiak, who came to the University of Chicago this fall from the University of Michigan. "We have seen excellent efficacy — the best reported to date — without the neurotoxicity that has been problematic with other drug combinations."

Ref : http://www.uchospitals.edu/news/2011/20111206-myeloma.html

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

2011-12-16T09:14:00.000+05:30

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

Synta's ganetespib shows potent in vitro and in vivo activity against multiple breast cancer types

2011-12-16T07:30:00.000+05:30

Synta researchers have reported that, Ganetespib (structure) shows potent in vitro and in vivo activity against multiple types of breast cancer including HER2-positive, ER/PR positive, triple-negative, and inflammatory breast cancer.

"These results demonstrating that ganetespib potently inhibits key signaling pathways involved in the growth and proliferation of multiple forms of breast cancer are encouraging, and supportive of the results presented earlier at this meeting showing single-agent, anti-tumor activity in patients with breast cancer who have progressed on or failed to respond to multiple prior therapies," said Vojo Vukovic, M.D., Ph.D., Chief Medical Officer, Synta.

Researchers conclude that, the combined preclinical and clinical results create a strong rationale for advancing ganetespib development in both HER2-positive and triple-negative breast cancer.

More : http://phoenix.corporate-ir.net/phoenix.zhtml?c=147988&p=irol-newsArticle&ID=1638540&highlight=

Combination of bortezomib and panobinostat shows promise against advanced multiple myeloma

2011-12-15T08:00:00.000+05:30

In co\continuation of my update on Bortezomib...

A phase 2 clinical trial has shown that pairing bortezomib with an experimental drug, panobinostat: Panobinostat is a histone deacetylase (HDAC) inhibitor, a type of drug that blocks key processes involved in gene expression and protein degradation. Panobinostat clogs up a protein disposal mechanism in myeloma cells so that harmful byproducts accumulate and eventually cause programmed cell death.(see below structure), may be a promising new treatment for such patients, Dana-Farber Cancer Institute researchers say.

The PANORAMA 2 trial included 53 patients with relapsed multiple myeloma who had undergone multiple rounds of prior treatment and, in more than half, also stem cell transplant. The researchers reported on 44 patients receiving the panobinostat-bortezomib-dexamethasone combination.

Results showed that in the first phase of the treatment, 9 of the patients had at least a partial response of their disease, and 2 of the 9 saw their myeloma almost disappear, a so-called near complete response. Another 7 patients experienced minimal response, which is also associated with clinical benefit.

More : http://ash.confex.com/ash/2011/webprogram/Paper41145.html

Ruxolinitib reduces spleen size by 35% in patients with myelofibrosis

2011-12-14T11:50:00.000+05:30

In continuation of my ruxolinitib

In a major advance in treatment, a multicenter study found that ruxolinitib did a better job than off-label chemotherapy drugs reducing the terrible symptoms associated with myelofibrosis, including pain, enlarged spleen, anemia, fever, chills, fatigue, and weight loss.

Only about 10 percent of myelofibrosis patients are eligible for a bone marrow transplant and chemotherapy often falls short, Dr. Mesa says. A handful of off-label chemotherapy drugs have been modestly helpful, he says.

A randomized, double-blind clinical trial, known as the COMFORT-1 study, showed that ruxolinitib reduced spleen size by more than 35 percent in almost all of the 154 patients studied. An enlarged spleen, caused by sequestered over-proliferating blood cells, causes discomfort and can also lead to the need for blood transfusions and further medical complications for patients.

"The studies confirmed the drug is very effective. As a representative of a particular class of molecular inhibitors called JAK2 inhibitors, which are now being widely studied, ruxolinitib suggests this category will continue to be promising for myelofibrosis," Dr. Mesa says.

Ref : More...

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

2011-12-12T15:12:00.000+05:30

American Friends of Tel Aviv University: Beating Superbugs with a High-Tech Cleanser

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

2011-12-09T20:48:00.000+05:30

Total Synthesis of Indolizidine (+)-223A :: ChemViews Magazine :: ChemistryViews

UMass Amherst Researchers Test a Drug-Exercise Program Designed to Prevent Type 2 Diabetes

2011-12-06T21:00:00.001+05:30

In continuation of my update on Metformin...

Kinesiology researcher Barry Braun of the University of Massachusetts Amherst and colleagues recently reported unexpected results of a study suggesting that exercise and one of the most commonly prescribed drugs for diabetes, metformin, each improves insulin resistance when used alone, but when used together, metformin blunted the full effect of a 12-week exercise program in pre-diabetic men and women.

Ref : http://www.umass.edu/newsoffice/newsreleases/articles/142505.php

Editorial: An apple a day keeps colitis away

2011-12-02T22:26:00.000+05:30

In continuation on my update on the benefits of apple

Editorial: An apple a day keeps colitis away:

More : http://msuextension.org/publications/AgandNaturalResources/MT200812AG.pdf

'via Blog this'

European Commission approves Vyndaqel® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP)

2011-11-28T07:15:00.000+05:30

We know that, Tafamidis (see structure) or Vyndaqel was discovered in the Jeffery W. Kelly Laboratory at The Scripps Research Institute using a structure-based drug design strategy and was developed at FoldRx pharmaceuticals, a biotechnology company led by Richard Labaudiniere that was acquired by Pfizer in 2010.

Tafamidis or Vyndaqel functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. In patients with FAP, this protein dissociates in a process that is rate limiting for aggregation including amyloid fibril formation, causing neurodegeneration and failure of the autonomic nervous system and/or the peripheral nervous system and/or the heart.

Now, European Commission has approved Vyndaqel^® (tafamidis) for the treatment of Transthyretin Familial Amyloid Polyneuropathy (TTR-FAP) in adult patients with stage 1 symptomatic polyneuropathy.

More...

HSC NEWS - Bat plant could give some cancers a devil of a time

2011-11-27T07:55:00.001+05:30

In a new study published this month in the Journal of the American Chemical Society, researchers with The University of Texas Health Science Center at San Antonio have pinpointed the cancer-fighting potential in the bat plant, or Tacca chantrieri......

HSC NEWS - Bat plant could give some cancers a devil of a time

FDA Approves Intermezzo.....

2011-11-26T08:00:00.000+05:30

The U.S. Food and Drug Administration today approved Intermezzo (zolpidem tartrate sublingual tablets) for use as needed to treat insomnia characterized by middle-of-the-night waking followed by difficulty returning to sleep.

This is the first time the FDA has approved a drug for this condition. Intermezzo should only be used when a person has at least four hours of bedtime remaining. It should not be taken if alcohol has been consumed or with any other sleep aid....

More....

Coffee may protect against womb cancer: Study

2011-11-24T08:45:00.000+05:30

In continuation of my update on the benefits of coffee

A new study shows that regular intake of coffee may significantly lower risk for endometrial or womb cancer.

For the study the researchers looked at coffee consumption and endometrial cancer risk in more than 67,000 women aged between 34 and 59 enrolled in the long-running Nurses' Health Study. The researchers found that women who took more than four cups of coffee a day over a 26-year period were 25 percent less likely to get the cancer. Women who drank two to three cups a day were 7 percent less likely to get it. Drinking less than four cups a day was not associated with reduced risk. Furthermore drinking tea did not reduce the risk. Additionally drinking more than two cups of decaffeinated coffee a day was tied to a 22 percent reduced risk for endometrial cancer.

The benefit wasn't a complete surprise, since coffee has been shown to lower estrogen and insulin levels, and higher levels of these hormones have been associated with an increased risk of endometrial cancer. But the new findings do help to clarify how obesity, estrogen and coffee might interact in triggering tumors.

“It would be premature to make a recommendation that women drink coffee to lower their endometrial cancer risk,” study author Dr. Edward Giovannucci, professor of nutrition and epidemiology at Harvard School of Public Health...

Ref : http://cebp.aacrjournals.org/content/early/2011/10/03/1055-9965.EPI-11-0766.abstract?sid=d8d229ed-e4b4-4b7a-bc6a-f3f86cba4c0e

Cisplatin anti-cancer drug binds pervasively to RNA....

2011-11-23T10:59:00.001+05:30

In continuation of my update on Cisplatin.....

An anti-cancer drug used extensively in chemotherapy binds pervasively to RNA -- up to 20-fold more than it does to DNA, a surprise finding that suggests new targeting approaches might be useful, according to University of Oregon researchers, lead by Victoria J. DeRose

Ref : http://uonews.uoregon.edu/archive/news-release/2011/11/cancer-drug-cisplatin-found-bind-glue-cellular-rna

Old drugs find new target for treating brain tumor

2011-11-20T10:34:00.000+05:30

In continuation of erlotinib ................................

Old drugs find new target for treating brain tumor

Researchers discover new class of antimalarial compounds...

2011-11-19T07:09:00.000+05:30

Researchers have discovered a group of chemical compounds that might one day be developed into drugs that can treat malaria infection in both the liver and the bloodstream. The study, which appears in the Nov. 18 issue of Science, was led by Elizabeth A. Winzeler, Ph.D., of the Scripps Research Institute in La Jolla, Calif., and was partially funded by the National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health.

By screening more than 4,000 chemical compounds that had previously shown activity against blood-stage Plasmodium, the investigators searched for a compound that would also inhibit liver-stage parasites and whose protein structure would allow the modification necessary for future drug development. They found that a group of three related compounds, known collectively as the imidazolopiperazine (IP) cluster, fit these criteria. In addition, strains of Plasmodium that had acquired resistance to other malaria drugs were susceptible to the IP cluster.

Using the IP cluster as a foundation, the researchers designed a drug candidate, GNF179, that reduced levels of one Plasmodium species by 99.7 percent and extended survival by an average of 19 days when tested in malaria-infected mice. By examining infected cells, the researchers confirmed that GNF179 (see the structure) was active in the liver stage of infection. Rresearchers note that while additional studies will be needed to fully understand the drug's mechanism of action and its specific targets within the liver, this study provides a potential starting point for developing new dual-stage antimalarial drugs.....

More : http://www.sciencemag.org/content/early/2011/11/16/science.1211936.abstract

New efficient synthesis for Taxol ?

2011-11-18T19:19:00.000+05:30

In continuation of my update on taxol....

Baran's group reports erecting that Rockefeller tree and adding the first few ornaments -- a molecule called taxadiene. A conventional taxadiene synthesis is inefficient and involves 26 steps to produce. The Baran group's method involves just 10 steps to produce many times what has been previously synthesized -- more than sufficient for planned research to find a way to efficiently produce Taxol®.

Innovation Leads to Access.....

The taxadiene synthesis is more than just a midway stop on the way to Taxol®. The current commercial Taxol® production method, which involves culturing cells from the yew tree, is more economical than any new synthesis is likely to be. Instead, Baran and his team are aiming to understand the processes used in nature to produce the compound, which are many times more efficient than those used by scientists to date. "It's my opinion that when there's a huge discrepancy between the efficiency of nature and humans, in the space between, there's innovation.

More specifically, lead researcher Phil Baran believes that, while developing an efficient synthesis for Taxol®, they will gain a fundamentally improved understanding of the chemistry involved and develop more widely applicable techniques. Such innovation could allow production of a whole range of taxanes currently inaccessible for drug discovery research either because the quantities researchers can produce are vanishingly small, or because they can't produce them at all. Control of the taxane oxidation process therefore offers the potential for discovering new and important drugs, perhaps even one or more that is better at fighting specific cancers than Taxol®.

Establishing the remaining steps between taxadiene and Taxol® or other more complex taxanes remains a challenging task that Baran estimates will take years.

"Nature has a choreography in the way she decorates the tree," he said. "It's a precise dance she has worked out over millennia. We have to figure out a way to bring that efficiency to the laboratory setting."

More... : http://www.nature.com/nchem/journal/vaop/ncurrent/full/nchem.1196.html

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF

2011-11-15T10:11:00.000+05:30

In continuation of my up date on rivaroxaban.....

Janssen receives FDA approval for Xarelto to prevent stroke in people with AF: The U.S. Food and Drug Administration today approved the anti-clotting drug Xarelto (rivaroxaban) to reduce the risk of stroke in people who have abnormal heart rhythm.

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

2011-11-13T13:10:00.000+05:30

In continuation of my update on the benefits of nuts...

Universitat de Barcelona - A scientific study describes new benefits of nut consumption

Crocin for multiple sclerosis?

2011-11-08T07:00:00.000+05:30

Medical researchers at the University of Alberta have discovered that an active ingredient in the Persian spice saffron may be a potential treatment for diseases involving neuroinflammation, such as multiple sclerosis. Researchers found there is a compound in saffron, known as crocin (see the structure below), that exerts a protective effect in brain cell cultures and other models of MS. It prevented damage to cells that make myelin in the brain.

Lead researcher Power said. "Myelin is insulation around nerves. MS is characterized by inflamed brain cells that have lost this protective insulation, which ultimately leads to neurodegeneration.......

More......

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

2011-11-06T07:44:00.001+05:30

Probiotics effective in combating antibiotic-associated diarrhea, studies find; 'Good bugs' look promising as anti-inflammatory agents

Ref : http://www.nature.com/ajg/journal/v106/n10/full/ajg2011201a.html

World's most efficient flexible organic light-emitting diodes created on plastic

2011-11-05T18:24:00.000+05:30

World's most efficient flexible organic light-emitting diodes created on plastic

2011-11-04T09:32:00.000+05:30

In continuation of my update on usefulness of benzodiazepine derivatives

Lundbeck Inc. presented interim data from its long-term, open-label extension study evaluating ONFI™ (clobazam see structure below) CIV for the adjunctive treatment of drop seizures associated with Lennox-Gastaut syndrome (LGS). Company claims that, these interim results support the reductions in drop seizure rates associated with ONFI when used as add-on therapy for adult and pediatric patients, two years of age or older, with a current or previous diagnosis of LGS. ....

More....

Biogen’s Multiple Sclerosis pill succeeds at a late phase clinical trial

2011-11-03T08:56:00.000+05:30

Biogen Idec Inc. has reported success in a late stage clinical trial of its oral multiple sclerosis drug BG-12 (see below structure), a competitor's of Teva Pharmaceutical Industries’ Laquinimod. A 240-milligram dose of BG-12 administered two or three times a day significantly reduced the proportion of patients who relapsed by 49% and 50%, respectively, after two years compared with a placebo....

Company adds that, in addition to significantly reducing ARR, BG-12 met all secondary relapse and MRI endpoints for both dose regimens.....

Ref : http://www.biogenidec.com/PRESS_RELEASE_DETAILS.aspx?ID=5981&ReqId=1621631

Leafy greens (broccoli and cabbage) protect the gut’s immune system

2011-11-02T08:09:00.000+05:30

In continuation of my update on Broccoli and its usefulness

Research from the Babraham Institute and the Medical Research Council (MRC), were able to prove that leafy greens protect a certain type of immune cell known as intra-epithelial lymphocytes (IELs). IELs play a crucial role in keeping the gut lining healthy and preventing ‘bad’ bacteria from entering the gut while maintaining the balance of ‘good’ bacteria which help us to break down our food. Researchers studied mice fed a diet containing many vitamins and minerals known to be essential for good health, but which lacked vegetables. Over three weeks the mice lost 70 to 80 per cent of IELs.

The research showed for the first time that mice fed a diet low in vegetables rapidly lose these specialised immune cells lining the intestinal tract, but not other immune cells. The team discovered that IELs depend on chemical signals from the digestive breakdown products of a substance called Indole-3-carbinol, high levels of which are found in vegetables like broccoli and cabbage.......

Ref :1. http://www.mrc.ac.uk/Newspublications/News/MRC008231
2. http://www.sciencedirect.com/science/article/pii/S0092867411011366

INNOPHARMA Receives FDA Approval of Generic Levetiracetam Injection

2011-11-01T10:28:00.000+05:30

In continuation of my update on Olanzapine......

INNOPHARMA Receives FDA Approval of Generic Levetiracetam Injection

Phase III Trial of Regorafenib in Metastatic Colorectal Cancer Meets Primary Endpoint of Improving Overall Survival...

2011-10-31T21:50:00.001+05:30

Bayer HealthCare Pharmaceuticals, announced the results from its Phase III trial evaluating its investigational compound regorafenib (see structure below, BAY 73-4506) for the treatment of patients with metastatic colorectal cancer (mCRC) whose disease has progressed after approved standard therapies: The trial met its primary endpoint of statistically significant improvement in overall survival.

This is the result of a pre-planned interim analysis conducted by an independent Data Monitoring Committee (DMC) of the CORRECT (Patients with metastatic colorectal cancer treated with regorafenib or placebo after failure of standard t herapy) trial. Per the recommendation of the DMC, the study has been unblinded and patients in the placebo arm will be offered treatment with regorafenib. In this trial, the safety and tolerability of regorafenib were generally as expected.

"These data are significant because they demonstrate that regorafenib increased overall survival in patients with heavily pretreated metastatic colorectal cancer, an area of high unmet medical need," said Kemal Malik .....

Ref : http://www.bayer.com/en/news-detail.aspx?newsid=15124

Researcher's compound disables bacteria instead of killing them

2011-10-31T08:34:00.000+05:30

A microbiologist at the University of Wisconsin-Milwaukee (UWM) has discovered a different approach: Instead of killing the bacteria, why not disarm them, quashing disease without the worry of antibiotic resistance?

Ching-Hong Yang, associate professor of biological sciences, has developed a compound that shuts off the "valve" in a pathogen's DNA that allows it to invade and infect. The research is so promising that two private companies are testing it with an eye toward commercialization.

"Researchers analyzed the genomic defense pathways in plants to identify all the precursors to infection and used the information to discover a group of novel small molecules that interrupt one channel in the intricate pathway system."..

Yang and collaborator Xin Chen, a professor of chemistry at Changzhou University in China, have tested the compound on two virulent bacteria that affect plants and one that attacks humans. They found it effective against all three and believe the compound can be applied to treatments for plants, animals and people.

Ref : Ching-Hong Yang et.al.,

WPI Research Shows How Cranberry Juice Fights Bacteria at the Molecular Level

2011-10-29T22:18:00.000+05:30

The study tested proanthocyanidins or PACs, a group of flavonoids found in cranberries. Because they were thought to be the ingredient that gives the juice its infection-fighting properties, PACs have been considered a hopeful target for an effective extract. The new WPI report, however, shows that cranberry juice, itself, is far better at preventing biofilm formation, which is the precursor of infection, than PACs alone. The data is reported in the paper "Impact of Cranberry Juice and Proanthocyanidins on the Ability of Escherichia coli to Form Biofilms," which will be published on-line, ahead of print on Oct. 31, 2011, by the journal Food Science and Biotechnology.

WPI Research Shows How Cranberry Juice Fights Bacteria at the Molecular Level

New dual drug combinations in development for various cancers

2011-10-22T07:11:00.000+05:30

New dual drug combinations in development for various cancers: A rarely used—and as yet largely unproven—approach to drug development has emerged as a significant tool in the effort to create high-impact new cancer drugs.

New data on novel gene-silencing oligonucleotide technology...

2011-10-21T07:28:00.000+05:30

Idera announced new data on its novel gene-silencing oligonucleotide (GSO) technology at the Cell Symposium on Regulatory RNAs in Chicago, IL. In preclinical studies, systemic delivery of GSOs targeted to ApoB or PCSK9 mRNA caused a reduction in the level of the targeted mRNA and associated protein and resulted in a decrease in serum total cholesterol and LDL-cholesterol concentration. ApoB and PCSK9 are two validated targets associated with cardiovascular diseases.

In this study, Idera created 19mer GSOs for apolipoprotein B (ApoB) and proprotein convertase subtilisin/kexin type 9 (PCSK9) mRNA and evaluated their in vivo activity in mice following subcutaneous administration. The data demonstrate that treatment with each GSO led to a significant reduction in the concentration of the target associated mRNAs and protein. The effects were specific, with no significant effects being observed on ABCA1, ABCG1 or LXR mRNA levels. In addition, treatment with GSOs for either ApoB or PCSK9 resulted in a decrease in total serum cholesterol and LDL-cholesterol.

More...

Yawning May Help the Brain Chill Out

2011-10-19T07:58:00.002+05:30

Yawning May Help the Brain Chill Out: Yawning may be a natural way of regulating brain temperature, a new study suggests.U.S. researchers examined the frequency of yawns among 80 people in the winter and another 80 people in the summer and found seasonal...

HSV1 drugs could slow progression of Alzheimer's disease

2011-10-18T13:30:00.000+05:30

HSV1 drugs could slow progression of Alzheimer's disease: Antiviral drugs used to target the herpes virus could be effective at slowing the progression of Alzheimer's disease (AD), a new study shows.

New Alzheimer's Drug Shows Early Promise

2011-10-15T07:40:00.000+05:30

An experimental Alzheimer's disease drug, gantenerumab, may help lower levels of amyloid plaque in the brains of people with the disease, an early clinical trial indicates. Researchers claims that, of 16 people with mild-to-moderate Alzheimer's disease, those who received two to seven infusions of the experimental drug every four weeks showed marked reductions in the amount of plaque in their brains via imaging tests that were conducted several months after their treatments.....

More...

Ginger Supplements Might Ease Inflammation Linked to Colon Cancer..

2011-10-14T13:47:00.002+05:30

A small, preliminary study finds that ginger root supplements seem to reduce inflammation in the intestines a potential sign that the pills might reduce the risk of colon cancer. Previous research in animals has suggested that ginger can reduce inflammation but isn't potentially toxic to the stomach like aspirin, Zick noted. And scientists have linked chronic inflammation in the gut to colon cancer, suggesting that easing this inflammation could reduce the risk of the disease.

In the new study, Zick's team randomly assigned 30 people to take pills containing 2 grams of ground ginger root extract or a "dummy" placebo pill each day for 28 days. They measured the level of inflammation in the participants' intestines before and after the test period. The researchers found that the level of inflammation in the subjects who took the ginger pills fell by an average of 28 percent, while staying about the same in those who took the placebo.

Ref : http://cancerpreventionresearch.aacrjournals.org/content/early/2011/10/07/1940-6207.CAPR-11-0224.abstract

Teriflunomide drug reduces relapse rate of people with MS

2011-10-11T07:06:00.000+05:30

In continuation of my update on Teriflunomide
A new oral drug has been shown in a large international clinical trial to significantly reduce the relapse rate of people with multiple sclerosis and to slow the progression of the disease.

More....

First combination drug to treat type 2 diabetes and high cholesterol receives FDA approval

2011-10-10T13:54:00.000+05:30

In continuation of my update on Simvastin

The U.S. Food and Drug Administration recently approved Juvisync (sitagliptin and simvastatin), a fixed-dose combination (FDC) prescription medication that contains two previously approved medicines in one tablet for use in adults who need both sitagliptin and simvastatin.....

More....

Blueberry powder may control triple negative breast cancer

2011-10-06T09:08:00.000+05:30

In continuation of my update on blue berry's usefulness....

Blueberry powder may control triple negative breast cancer: In several studies recently conducted at the Beckman Research Institute at the City of Hope, Duarte, CA researchers found that feeding blueberry powder to mice significantly reduced the growth and spread of triple negative breast cancer cells, a very aggressive form of cancer.

Health Canada approves Trajenta (linagliptin) for type 2 diabetes

2011-10-05T09:11:00.000+05:30

Linagliptin (below structure, BI-1356, trade name Tradjenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly. Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Both GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Thus, linagliptin stimulates the release of insulin in a glucose-dependent manner and decreases the levels of glucagon in the circulation.

Now Health Canada approves....

More...

Novel drug shows promise for MLL leukemia

2011-10-04T09:51:00.001+05:30

Novel drug shows promise for MLL leukemia:

According to British scientists a potential new drug from GlaxoSmithKline could treat mixed-lineage leukemia (MLL). MLL is the most common form of leukemia in babies. The study appeared in the journal Nature where scientists from the British drugmaker collaborating with the charity Cancer Research UK (CRUK) and Cellzome AG found that the experimental drug, called I-BET151.

More......

Ref : http://www.nature.com/nature/journal/vaop/ncurrent/full/nature10509.html

Drug Shows Promise Against Deadly Lung Disease

2011-09-29T07:12:00.000+05:30

An experimental drug mayoffer a thin ray of hope to people suffering from the rapidly fatal lungdisease known as idiopathic pulmonary fibrosis. The compound, currently known only as BIBF1120 (see structure below: Vargatef™), seems to slow the disease, decrease exacerbations and improvequality of life for patients, according to a study funded by the drug's maker,Boehringer Ingelheim.

"Itimproves the course of disease and, in my opinion, it's the first drug tosignificantly ameliorate the really devastating progression of thedisease,"

said Dr. Norman Edelman, (chief medical officer for the AmericanLung Association, who noted that current treatments for the disease "arealmost desperation attempts. There's very little evidence they work)..."

Authors don't claim [BIBF 1120] is going to reverse thedisease. They claim it's going to slow it down, but even that is a majorfactor.

Patientswith IPF usually die within two to three years of diagnosis. While the diseaseused to be considered relatively rare, Edelman noted that doctors have beennoticing an uptick in recent ears, especially among older men. Idiopathicpulmonary fibrosis (IPF) involves a relentless stiffening of the lungs due tooverproduction of collagen, the "cement" that holds lung tissuetogether.

More : http://www.nejm.org/doi/full/10.1056/NEJMoa1103690

Broccoli, Cabbage, and other Veggies May Protect Against Colon Cancer

2011-09-28T08:37:00.000+05:30

In continuation of my update on the usefulness of broccoli
Austrailian researchers examined the diets of 918 colorectal cancer patients and 1,021 people with no history of the disease and found that consumption of certain vegetables and fruits were associated with a decreased risk of cancer in the proximal and distal colon, that is, the upper and lower portions of the colon.

Consumption of brassica vegetables (also known as cole crops) such as broccoli, kale, cauliflower, turnips and cabbage, for example, appeared to reduce the risk of cancer in the upper colon, while both total fruit and vegetable intake (and total vegetable intake alone) reduced the risk of cancer in the lower colon.

They also found that eating more apples and dark, yellow vegetables was linked with a significantly reduced risk of lower colon cancer...

More....

Preclinical studies shows EmPAC more effective than Taxol

2011-09-22T09:13:00.000+05:30

Cornerstone Pharmaceuticals, Inc. has announced the publication of data from preclinical studies on EmPAC™ (nanoparticle reformulation of paclitaxel). Company claims the data demonstrating improved safety and efficacy of EmPAC™ versus Taxol®, the generic formulation of paclitaxel and one of the most widely prescribed chemotherapies. EmPAC™ is a nanoemulsion formulation of Paclitaxel and is the lead product candidate of Cornerstone’s proprietary Emulsiphan™ cancer selective delivery nanotechnology platform. Taxol®, an injectable formulation of Paclitaxel, is currently used to treat a variety of cancers, including ovarian carcinomas, breast cancer, non-small cell lung cancer, and AIDS-related Kaposi’s sarcoma....

More : http://www.cornerstonepharma.com/wp-content/uploads/Empac-JNN-Release-FINAL-Sept_15_2011.pdf

2011-09-21T08:40:00.000+05:30

Santarus, Inc. recently announced that analysis of top-line safety data from a double blind, multicenter 12-month extended use study in patients treated daily with either the investigational drug budesonide (see structure) MMX^® 6 mg or placebo will be provided as support for the company's planned submission of a New Drug Application (NDA) for budesonide MMX 9 mg to the U.S. Food and Drug Administration (FDA) for the induction of remission of mild or moderate active ulcerative colitis. Santarus had previously announced results from two Phase III clinical studies that evaluated the safety and efficacy of budesonide MMX 9 mg over an eight week course of treatment for induction of remission of mild or moderate active ulcerative colitis.

Highlights (of the study of 123 patients) are:

The frequency of treatment related adverse events for budesonide MMX 6 mg (21.0%) was similar to placebo (21.3%).
Mean morning plasma Cortisol levels remained within normal limits at all visits for both budesonide MMX 6 mg and placebo.
There were no clinically meaningful differences in the numbers of patients with abnormal bone mineral density scans at baseline and end-of-study between budesonide MMX 6 mg and placebo.

"Now that we have the top-line safety data from the extended use study, we are moving forward as planned to submit the NDA in December 2011 for budesonide MMX 9 mg for the induction of remission of mild to moderate active ulcerative colitis," said Gerald T. Proehl, CEO/President of the company...

More.: http://ir.santarus.com/releasedetail.cfm?ReleaseID=606515

2011-09-20T08:05:00.000+05:30

We know that, Linagliptin (BI-1356, trade name Tradjenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes. Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.

Now the companies have announced results of a 102 week Phase III study for linagliptin (trade name Trajenta® in Europe), which show meaningful and durable reductions in blood glucose for adults with type 2 diabetes (T2D). In the two-year study presented today at the 47^th Annual Meeting of the European Association for the Study of Diabetes (EASD), the DPP-4 inhibitor linagliptin showed a favourable safety profile and lowered HbA1c levels by 0.8% over the long term in those patients treated with linagliptin for the full study period.

Researchers conclude that, these results show that the efficacy achieved by linagliptin is reliable and meaningful in a clinical setting, but also that it is durable over the long term. This is especially important in chronic conditions such as type 2 diabetes.

The data from these patients demonstrate the efficacy and tolerability of linagliptin as mono-, dual- (plus metformin or initial combination with pioglitazone) or triple (plus metformin and sulphonylurea) oral therapy over a period of 102 weeks. Reductions in HbA1c of 0.8% after 24 weeks of blinded treatment were seen to be durable over the additional 78 weeks. Overall, the rate of hypoglycaemic events was low and body weight remained unchanged.

More..

New drug cure nearly any viral infection?...

2011-09-17T20:20:00.000+05:30

Could new drug cure nearly any viral infection? Technology shows promise against common cold, influenza and other ailments, researchers say

More : Broad-Spectrum Antiviral Therapeutics

Biologists identify mechanism of H. pylori that damages DNA of gastric mucosal cells

2011-09-13T09:32:00.000+05:30

In continuation of my update on H.Pylorihttp://www.med-chemist.com/search?q=pylori..

We know that, stomach bacterium Helicobacter pylori is one of the biggest risk factors for the development of gastric cancer, the third most common cause of cancer-related deaths in the world. Molecular biologists from the University of Zurich have now identified a mechanism of Helicobacter pylori that damages the DNA of cells in the gastric mucosa and sets them up for malignant transformation.

More at :

Biologists identify mechanism of H. pylori that damages DNA of gastric mucosal cells

2011-09-12T08:48:00.000+05:30

In continuation of my updates on Rivaroxaban...

FDA Issues Complete Response Letter to Johnson & Johnson Pharmaceutical Research & Development Regarding New Drug Application for Tapentadol Extended Release....

Researchers rethink fenretinide for prevention of oral cancer

2011-09-10T09:04:00.000+05:30

In continuation of my update on fenretinide...

For more than two decades, researchers have studied and used fenretinide, a synthetic vitamin A derivative. Fenretinide's capacity to induce both terminal differentiation and cell death yielded highly promising results with cultured human cancer cells. Likewise, studies in lung, breast skin, prostate and bladder animal cancer models re-enforced fenretinide's cancer-preventing effects at the in vivo level. However, when it came to prevention of oral cancer, fenretinide efficacy wasn't what scientists expected. After multiple studies with lackluster results, oral cancer researchers moved away from fentretinide to look elsewhere for an answer.

Now researchers lead by Dr. Susan Mallery started rethinking about the failure and wanted to find a way to circumvent issues with poor systemic uptake by delivering the compound directly to the lesion.

Mallery found the answer in partnering with two University of Michigan pharmaceutical chemists (Steven Schwendeman and Kashappa Goud Desai) to develop a first of its kind patch that sticks to the inside of the mouth, and delivers a continuous therapeutic dose of fenretinide directly to the precancerous lesion. The patch consists of three layers: a disk saturated with fenretinide and polymers that make the lipid soluble fenretinide better adsorbed in a water-rich environment, a secondary adhesive ring to hold the disk in place, and a final backing layer that ensures the medication stays inside the area of the patch.

The research team has just completed a pharmacokinetic study in rabbits. Subsequent plans include an initial Phase zero study in humans, followed by a clinical trial to evaluate efficacy in patients with precancerous oral lesions. A companion formulation designed to prevent emergence of pre-cancerous cells within the entire mouth may also be used in the fenretinide patch clinical trial.

Ref : http://cancer.osu.edu/mediaroom/releases/Pages/Oral-Patch.aspx

Redesigned Vancomycin As Potent Antimicrobial Activity Against Vancomycin-Resistant Bacteria...

2011-09-09T09:52:00.000+05:30

In continuation of my update on vancomycin....

A team of scientists from The Scripps Research Institute has successfully reengineered an important antibiotic (Vancomycin) to kill the deadliest antibiotic-resistant bacteria. The researchers claim that compound could one day be used clinically to treat patients with life-threatening and highly resistant bacterial infections. The compound synthesized is an analogue of the well-known commercial antibiotic vancomycin.

Vancomycin normally works by grabbing hold of and sequestering the bacterial cell-wall making machinery, a peptidoglycan (carbohydrate and peptide containing molecule). Only Gram-positive bacteria have a cell wall, which is a membrane on the cell's outer surface. Unfortunately, bacteria have found a way to alter the peptidoglycan in such a way that the antibiotic can no longer grab hold. Researchers claim that, the new vancomycin analogue can grab hold of the mutant peptidoglycan, and again prevent the bacteria from making the cell wall and killing the resistant bacteria. But what is so remarkable about the design is that the redesigned antibiotic maintains its ability to bind the wild type peptidoglycan as well.

New compound has an amidine (an iminium, RC=NH+ linked to a nitrogen, N) instead of an amide at a key position buried in the interior of the natural product. I appreciate the idea and the simplicity in achieving the target functional group.

Researchers add that, although it is still at its early stages and there is much work ahead.In my opinion it is a good beginning...

Ref : A Redesigned Vancomycin Engineered for Duald-Ala-d-Ala andd-Ala-d-Lac Binding Exhibits Potent Antimicrobial Activity Against Vancomycin-Resistant Bacteria

New class of anti-diabetic compound established

2011-09-08T08:58:00.001+05:30

New class of anti-diabetic compound established

2011-09-05T19:09:00.000+05:30

In continuation of my update on Valproic acid...

New research suggests brain tumor patients who take the seizure drug valproic acid on top of standard treatment may live longer than people who take other kinds of epilepsy medications to control seizures. The research is published in the August 31, 2011, online issue of Neurology®, the medical journal of the American Academy of Neurology.....

Ref : http://www.neurology.org/content/75/24/2229.abstract?sid=49b511a0-d597-4598-865c-297439b6eb39

Heat in Chili Peppers Can Ease Sinus Problems, Research Shows

2011-09-03T22:53:00.000+05:30

In continuation of my update on the usefulness of Casaicin...

We know that, Capsicum annum contains capsaicin, which is the main component of chili peppers and produces a hot sensation. Capsaicin is also the active ingredient in several topical medications used for temporary pain relief. It is approved for use by the U.S. Food and Drug Administration and is available over the counter.

Now researchers lead by Jonathan A. Bernstein of University of Cincinnati College of Medicine, Cincinnati, Ohio, have come up with an interesting finding about Capsicum annum. As per the claim by the researchers a nasal spray containing an ingredient derived from hot chili peppers (Capsicum annum) may help people "clear up" certain types of sinus inflammation. Researchers add that, study which showed that participants who used a nasal spray with Capsicum reported a faster onset of action or relief, on average within a minute of using the spray, than the control group and the spray is safe and effective on non-allergic rhinitis.

Interestingly, this is the first controlled trial where capsaicin was able to be used on a continuous basis to control symptoms. It is considered a significant advance, because of the fact that in the previous trials the ingredient was too hot to administer without anesthesia.

Ref : http://www.annallergy.org/article/S1081-1206%2811%2900383-8/abstract

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

2011-09-01T07:27:00.000+05:30

In continuation of my update on Crizotinib.....
Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

Medical engineers develop sensor chip to monitor cancerous tumors

2011-08-31T19:37:00.000+05:30

A team of medical engineers headed by Prof. Bernhard Wolf at the TUM Heinz Nixdorf Chair of Medical Electronics have now developed a sensor chip that can be implanted close to a tumor. The sensor chip measures the concentration of dissolved oxygen in the tissue and wirelessly transmits this information to a receiver carried by the patient. The receiver forwards the data to the patient's doctor, who can then monitor the tumor's development and arrange for an operation or therapies such as chemotherapy. The tumor is thus continually monitored and the patient does not have to visit the practice or hospital as frequently for check-ups.

Researchers claim that, sensor chip has already passed laboratory tests with cell and tissue cultures. The main challenge for the researchers was developing a sensor that functions entirely autonomously for long periods of time. The sensor must continue to function and deliver correct values even in the presence of protein contamination or cell debris. It also has to be “invisible” to the body so that it is not identified as a foreign object, attacked and encapsulated in tissue.

We designed the sensor chip to self-calibrate to a set dissolved oxygen concentration at measurement intervals," explains engineer and project manager Sven Becker.....

More....

Scientists Re-engineer an Antibiotic to Overcome Resistant Bacteria - Topix

2011-08-28T19:57:00.000+05:30

Scientists Re-engineer an Antibiotic to Overcome Resistant Bacteria - Topix

Yale scientists synthesize huperzine A to combat Alzheimer's

2011-08-27T20:14:00.000+05:30

Scientists at Yale University have developed the first practical method to create a compound called huperzine A (see structure below) in the lab. Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the plant firmoss Huperzia serrata. Huperzine A is also an Acetylcholinesterase inhibitor, which has a mechanism of action similar to donepezil, rivastigmine, and galantamine. In the US, Huperzine A is sold as a dietary supplement for memory support. The botanical has been used in China for centuries for the treatment of swelling, fever and blood disorders. Clinical trials in China have shown it to be effective in the treatment of Alzheimer's disease and enhancing memory in students.

More at : http://opac.yale.edu/news/article.aspx?id=8796

FDA Approves Zelboraf - Potent New Melanoma Drug

2011-08-21T08:57:00.000+05:30

Plexxikon Inc., a member of the Daiichi Sankyo Group, today announced that applications for market approval for vemurafenib ( PLX4032/RG7204, see below structure) for the treatment of metastatic melanoma have been submitted to the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA). The company had

Phase 2 and 3 trials (BRIM2 and BRIM3) that evaluated vemurafenib in patients with BRAF ^V600 mutation-positive melanoma, as determined by the cobas 4800 BRAF ^V600Mutation Test.

Earlier this year, the company reported positive data from an interim analysis of BRIM3 which showed that the study met the pre-specified criteria for co-primary endpoints for BRIM3 for progression-free survival and overall survival, and that the safety profile was generally consistent with the previous vemurafenib studies. Based on these results, the data safety monitoring board for the trial recommended early termination of the trial and allowed dacarbazine-treated patients to immediately cross over to vemurafenib treatment. BRIM2 results reported earlier showed a 52 percent confirmed response rate, with tumor shrinkage in the majority of patients, consistent with results from earlier studies.

More....

Green tea shows promise against two types of tumors, HHS

2011-08-20T08:29:00.001+05:30

In continuation of my update on green tea

Researchers lead by Dr. Thomas Smith at The Donald Danforth Plant Science Center and his colleagues at The Children’s Hospital of Philadelphia, have found that a compound found in green tea shows great promise for the development of drugs to treat two types of tumors and a deadly congenital disease.

Dr. Smith and his colleagues discovered that two compounds found naturally in green tea are able to compensate for this genetic disorder by turning off GDH in isolated and when the green tea compounds were administered orally. The Smith lab also used X-ray crystallography to determine the atomic structure of these green tea compounds bound to the enzyme. With this atomic information, they hope to be able to modify these natural compounds to design and develop better drugs.

Interestingly, two other research groups have validated and extended these findings to demonstrate that blocking GDH with green tea is very effective at killing two different kinds of tumors; glioblastomas, an aggressive type of brain tumor, and tuberous sclerosis complex disorder, a genetic disease that causes non-malignant tumors to grow on a number of organs.

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EMA has accepted Pfizer's regulatory submissions for review of two investigational compounds crizotinib and bosutinib

2011-08-20T08:03:00.002+05:30

European Medicines Agency (EMA) has accepted Pfizer's regulatory submissions for review of two investigational compounds crizotinib, an oral first-in-class anaplastic lymphoma kinase (ALK) inhibitor, for the treatment of patients with previously treated ALK-positive advanced non-small cell lung cancer (NSCLC); and bosutinib for the treatment of adult patients with newly diagnosed Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase.

Crizotinib

Bosutinib

Dr. Andreas Penk, president of Pfizer Oncology Europe, claims that,

"With the EMA submissions for crizotinib and bosutinib, we are one step closer to potentially bringing two promising agents to patient populations in areas of significant unmet medical need"......

Two Randomized Trials of Linaclotide for Chronic Constipation

2011-08-15T09:04:00.001+05:30

We know that, Linaclotide (BELOW STRUCTURE) is an experimental peptide agonist of guanylate cyclase 2C that is undergoing clinical trials for use in treating abdominal pain in patients with irritable bowel syndrome (IBS) accompanied by constipation. The drug was developed by Ironwood Pharmaceuticals, based in Cambridge, Massachusetts.

Now researchers lead by, Dr. Anthony J. Lembo, an associate professor of medicine at Harvard Medical School and director of the GI Motility Center at Beth Israel Deaconess Medical Center in Boston, have come up with interesting claim that "people who received the drug had improvement in symptoms, and the treatment was generally well-tolerated".

Researchers conclude that, linaclotide significantly reduced bowel and abdominal symptoms in patients with chronic constipation (2 trials). Additional studies are needed to evaluate the potential long-term risks and benefits of linaclotide in chronic constipation...

Ref : http://www.nejm.org/doi/full/10.1056/NEJMoa1010863

Study Pits New Blood Thinner Against Warfarin For Irregular Heartbeat

2011-08-14T09:18:00.002+05:30

A new drug, Rivaroxaban, (see structure) that lowers stroke risk among people with an irregular heartbeat may give the old standby, warfarin, some competition, a new study shows.

We know that, Rivaroxaban (BAY 59-7939) is an oral anticoagulant invented and manufactured by Bayer; in a number of countries it is marketed as Xarelto. In the United States, it is marketed by Janssen Pharmaceutica. It is the first available orally active direct factor Xa inhibitor. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs four hours after a dose. The effects lasts 8–12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible. Now the new trial pitted the newer drug, rivaroxaban, against warfarin in more than 14,000 patients who were randomly assigned either warfarin or rivaroxaban. Neither the patients nor the doctors knew who was taking which drug. As per the claim by the resarchers, new agent proved to be as effective as warfarin at reducing the risk of ischemic stroke -- the most common kind of stroke, but it did not need to be monitored as closely as warfarin since it is given as a one-size-fits-all dose....

"a reasonable alternative to warfarin, with less intracranial or fatal bleeding." claims the lead researcher, Dr. Manesh R. Patel...

Ref : http://www.newsroom.heart.org/index.php?s=43&item=1191

Bear bile chemical could help keep hearts in rhythm

2011-08-12T10:46:00.003+05:30

We know that, the compound, ursodeoxycholic acid (UDCA, see structure), is already used to lower cholesterol and help dissolve gallstones, and it's a key ingredient in many traditional Chinese medicines, which use bear bile. According to the latest research from Imperial College London it might also be able to treat abnormal heart rhythm, or arrhythmia, in fetuses and heart attack victims.

“These findings are exciting because the treatments we have now are largely ineffective at preventing arrhythmia in patients who develop an abnormal heart rhythm after a heart attack,” said Dr. Julia Gorelik...........

Ref : http://www3.imperial.ac.uk/newsandeventspggrp/imperialcollege/newssummary/news_2-8-2011-10-25-30

Positive results from combination drug trial for late-stage ovarian cancer

2011-08-11T08:34:00.000+05:30

In continuation of my update on carboplatin

Researchers from IU Medical Sciences Program-Bloomington and Indiana University Melvin, have found that, an experimental two-drug combination (decitabine & carboplatin) for treating late-stage ovarian cancer continues to produce strong results, leading its Indiana University researchers to actively pursue the next step, conducting a larger clinical trial to test the therapy and to see how it compares with existing treatments for ovarian cancer.

The researchers have been investigating the addition of decitabine, which is marketed as Dacogen in the United States, because they suspect it reactivates tumor suppression genes that are turned off in ovarian cancer cells and improves cells' susceptibility to anti-cancer drugs like carboplatin.

"The science associated with the trial is novel and exciting and could have impact in the future," she said.....

More...

Diabetes drug rosiglitazone can reduce development of neuropathic pain..

2011-08-09T09:00:00.000+05:30

In continuation of my update on Rosiglitazone,

The diabetes drug rosiglitazone (Avandia) can control inflammation leading to nerve damage and abnormal pain responses, claims the researchers of Juntendo University School of Medicine, Tokyo.

As per the claim by the researchers, Rosiglitazone works by blocking a specific pathway—called PPAR-gamma—which appears to play a critical role in the development of disabling neuropathic pain. Researchers therefore propose PPAR-gamma regulation of the macrophage-mediated inflammatory response as a novel therapeutic target for treating neuropathic pain development.

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FDA Accepts NDA Filing for Ruxolitinib as a Treatment for Myelofibrosis

2011-08-08T16:21:00.002+05:30

FDA Accepts NDA Filing for Ruxolitinib as a Treatment for Myelofibrosis

Taxoxifen combined with dasatinib reverses chemo-resistance in breast cancer cells

2011-08-04T20:35:00.000+05:30

Researchers from Thomas Jefferson University Hospita, found that taxoxifen combined with dasatinib, a protein-tyrosine kinase inhibitor, reverses the chemo-resistance caused by cancer-associated fibroblasts in the surrounding tissue by normalizing glucose intake and reducing mitochondrial oxidative stress, the process that fuels the cancer cells.

In this study, researchers sought to better understand drug resistance by looking at the metabolic basis in an ER (+) cell line and cancer-associated fibroblasts. Researchers claim that the resistance to chemotherapeutic agents is a metabolic and stromal phenomenal and the drug combination had an "antioxidant effect" in these types of cancer cells.

Researchers showed that ER (+) cancer cells alone responded to tamoxifen but when co-cultured with human fibroblasts had little to no effect. Similarly, dasatinib, a chemotherapy drug used to treat leukemia patients who can no longer benefit from other medications, had no effect on fibroblasts alone or cancer cells. Together, however, the drugs prevented the cancer cells co-cultured with the fibroblasts from using high-energy nutrients from the fibroblasts. Researchers conclude that,

"The drugs have no effect when they are used alone-it's in unison when they effectively kill the cancer cells in the presence of fibroblasts and combination resulted in nearly 80 percent cell death"

Ref: http://www.jeffersonhospital.org/News/leukemia-drug-reverses-tamoxifen-resistance-in-breast-cancer-cells.aspx

New cough suppressant from cocoa

2011-08-02T19:25:00.000+05:30

Researchers are carrying out the final stages of clinical trials of a drug that contains theobromine (see structure), an ingredient found in chocolate and cocoa. The drug could be in the market in another two years.

New cough suppressant from cocoa

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

2011-08-02T19:22:00.000+05:30

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

New three-drug combination may be effective for newly diagnosed blood cancer patients: Study

2011-08-01T19:24:00.000+05:30

New three-drug combination may be effective for newly diagnosed blood cancer patients: Study

When Having the Blues is a Good Thing: Blueberries & Cancer Prevention

2011-08-01T09:17:00.001+05:30

In continuation of my up date on the usefulness of blue berries.

Now researchers from the Department of Nutrition Sciences at the University of Alabama at Birmingham, lead by Laura Newton have come up with another interesting finding about blue berries, i.e., as little as a cup a day can help prevent cell damage linked to cancer.

As per the claim by the researchers, free radicals, atoms that contain an odd number of electrons and are highly reactive, can cause cellular damage, one of the factors in the development of cancer; many believe a diet filled with fruits and vegetables may help reduce the risk.

Lead researcher says

"Studies suggest that antioxidants may help prevent the free-radical damage associated with cancer"

Researchers add that, Blueberries also are rich in vitamin C, which helps the immune system and can help the body to absorb iron. "Vitamin C also helps to keep blood vessels firm, offering protection from bruising. Blueberry juice and other products may be nutritious but often contain less fiber than the whole fruit, and added sugar or corn syrup may decrease their nutritional value. Consuming fresh, raw blueberries provides the most benefits; the average serving size of raw blueberries is one cup, which contains about 80 calories...

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Ivabradine also effective in reducing the risk of diastolic heart failure..

2011-08-01T08:50:00.001+05:30

Researchers from the Montreal Heart Institute (MHI) have come up with the new findings about the drug, ivabradine (see structure). Researchers claim that, a heart rate reduction medication, is also effective in reducing the risk of diastolic heart failure (left ventricular insufficiency) and cardiac fibrosis.

As per the claim by the researchers Ivabradine, reduces Diastolic Dysfunction and Cardiac Fibrosis. The study was conducted on rabbits given a standard diet, a cholesterol-enriched diet or a cholesterol-enriched diet with ivabradine. Researchers found that apart from improving the myocardial performance index, ivabradine greatly improved left ventricular diastolic dysfunction in animals receiving a cholesterol-enriched diet. Ivabradine also reduced fibrosis of the heart chambers adds the researchers.

According to Dr. Jean-Claude Tardif, Director of the MHI Research Centre and professor of medicine at the Universit- de Montr-al,

"The effectiveness of ivabradine in treating angina pectoris is now well known. However, few treatments are available to patients with diastolic heart failure. The beneficial effects of ivabradine demonstrated in laboratory suggest that this course of treatment should be further investigated." Clinical studies with subjects are expected to follow..........

http://www.icm-mhi.org/files//pdf/Communique-EN-2011/press_release_Ivabradine.pdf