FDA Approves Inlyta for advanced kidney cancer (renal cell carcinoma)

The U.S. FDA,  approved Inlyta (axitinib) to treat patients with advanced kidney cancer (renal cell carcinoma) who have not responded to another drug for this type of cancer. 

The safety and effectiveness of Inlyta were evaluated in a single randomized, open-label, multi-center clinical study of 723 patients whose disease had progressed on or after treatment with one prior systemic therapy. The study was designed to measure progression-free survival, the time a patient lived without the cancer progressing. Results showed a median progression-free survival of 6.7 months compared to 4.7 months with a standard treatment (sorafenib).

The most common side effects observed in greater than 20 percent of patients in the clinical study were diarrhea, high blood pressure (hypertension), fatigue, decreased appetite, nausea, loss of voice (dysphonia), hand-foot syndrome (palmar-plantar erythrodysesthesia), weight loss, vomiting, weakness (asthenia) and constipation.

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FDA Approves BYDUREON™ -- The First and Only Once-Weekly Treatment for Type 2 Diabetes

In continuation of my up date on Exenatide...

Amylin Pharmaceuticals, Inc. and Alkermes plc today announced that the U.S. Food and Drug Administration (FDA) has approved Bydureon  (exenatide extended-release for injectable suspension) – the first once-weekly treatment for type 2 diabetes. Bydureon is a glucagon-like peptide-1 (GLP-1) receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes in multiple clinical settings....

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Drug May Slow Early Prostate Cancer: Study

In continuation of my update on Dutasteride (Avodaart)

New research suggests that Avodart, a drug used to treat an enlarged prostate gland, may help slow the progression of early stage prostate cancer, reducing the need for aggressive treatment in some men. 

Avodart belongs to a class of drugs called 5-alpha reductase inhibitors. These drugs work by interfering with the effects of certain male hormones on the prostate. In the three-year study, prostate cancer progressed in 38 percent of 144 men with early prostate cancer who were treated with Avodart and 48 percent of the 145 men who received a placebo....

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Could 'Magic' Mushrooms Ease Depression?

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

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...

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

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

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

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

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

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.

 

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

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

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

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

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...

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

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..........

   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.

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

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....

 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

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."

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.

More.....

Notch inhibitor appears to treat breast cancer....

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

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

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......

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

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......

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

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

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

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

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

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

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

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

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

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

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

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)

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

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.....

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

 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....

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

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

Old drugs find new target for treating brain tumor

Researchers discover new class of antimalarial compounds...

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 ?

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

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

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?

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.......

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

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

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

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. ....

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