Saturday, June 30, 2012

Two-Drug Combo (naproxen and sumatriptan) Helps Teens With Migraines


A two-drug combination that relieves migraines in adults also works well in adolescents, new research indicates.
Because the combination of Imitrex (sumatriptan see structure left) and naproxen (structure right) sodium (Aleve and other brand names) isn't approved for use by the U.S. Food and Drug Administration for this age group, doctors must prescribe it "off label" to adolescents.
"There are no FDA-approved abortive [migraine] treatments for children," said Dr. Noah Rosen, director of the Headache Center at the Cushing Neuroscience Institute in Great Neck, N.Y. "This is the first really large-scale abortive treatment study for adolescents."
Migraines in children and adolescents are physiologically no different from migraines in adults, said Drexler, although migraines in younger people tend not to last as long.
The class of drugs known as triptans are the most studied, but none of those trials have shown a great benefit, possibly because of a large placebo response, the study authors wrote.

Friday, June 29, 2012

Advanced Prostate Cancer Drug May Help at Earlier Stage

In continuation of my update on abiraterone

Advanced Prostate Cancer Drug May Help at Earlier Stage:  A drug approved to treat advanced prostate cancer appears to help men who have localized high-risk prostate cancer if given before surgery. Adding Zytiga (abiraterone) to conventional hormonal treatments eliminated or nearly...

Thursday, June 28, 2012

Experimental Drug Helps Fight Some Childhood Cancers, Study Finds

In continuation of my update on Crizotinib
Experimental Drug Helps Fight Some Childhood Cancers, Study Finds:  A new targeted drug therapy may help treat certain advanced cancers in children, a new preliminary study indicates.In some cases, the oral medication even made tumors disappear after regular cancer treatments had failed, the...

Wednesday, June 27, 2012

Abiraterone acetate can help eliminate prostate tumors

In continuation of my update Abiraterone

Abiraterone acetate can help eliminate prostate tumors: A hormone-depleting drug approved last year for the treatment of metastatic prostate cancer can help eliminate or nearly eliminate tumors in many patients with aggressive cancers that have yet to spread beyond the prostate, according to a clinical study to be presented at the annual meeting of the American Society of Clinical Oncology (ASCO), June 1-5, in Chicago.

Tuesday, June 26, 2012

Mylan receives final FDA approval for Clopidogrel Tablets ANDA



Mylan receives final FDA approval for Clopidogrel Tablets ANDA: Mylan Inc.  announced that its subsidiary Mylan Pharmaceuticals Inc. has received final approval from the U.S. Food and Drug Administration (FDA) for its Abbreviated New Drug Application (ANDA) for Clopidogrel Tablets USP, 75 mg and 300 mg.

Monday, June 25, 2012

Celery Chemical, Apigenin Tackles Breast Cancer


Apigenin, a natural substance found in grocery store produce aisles, shows promise as a non-toxic treatment for an aggressive form of human breast cancer, following a new study at the University of Missouri. MU researchers found apigenin shrank a type of breast cancer tumor that is stimulated by progestin, a synthetic hormone given to women in combination with estrogens to ease symptoms related to menopause.


“This is the first study to show that apigenin, which can be extracted from celery, parsley and many other natural sources, is effective against human breast cancer cells that had been influenced by a certain chemical used in hormone replacement therapy,” said co-author Salman Hyder, the Zalk Endowed Professor in Tumor Angiogenesis and professor of biomedical sciences in the College of Veterinary Medicine and the Dalton Cardiovascular Research Center.


In the study, Hyder and his colleagues implanted cells of a deadly, fast-growing human breast cancer, known as BT-474, into a specialized breed of mouse. Some of the mice were then treated with medroxyprogesterone acetate (MPA), a type of progestin commonly given to post-menopausal women. A control group did not receive MPA.



Later one group of MPA-treated mice was treated with apigenin. Cancerous tumors grew rapidly in the mice which did not receive apigenin. In the apigenin-treated mice, breast cancer cell growth dropped to that of the control group, and the tumors shrank.



Sunday, June 24, 2012

New combination of two previously approved FDA drugs treat lung cancer

In continuation of my update on Erlotinib..

Dr. Narla's laboratory focuses on the identification and characterization of the genes and pathways involved in cancer metastasis. By studying the functional role of the KLF6 tumor suppressor gene, Dr. Narla and his team have identified new signaling pathways regulated by this gene family thus providing new insight into cancer diagnosis and treatment. The team's research found that KLF6 and FOXO1, both tumor suppressor genes, are turned off as cancer spreads through the body. By using a combination of two existing FDA drugs -Erlotinib (left structure), a targeted cancer drug, and Trifluoperazine (below right structure), a medication used to treat schizophrenia, the team developed an understanding of the properties that turn these critical genes back on, initiating tumor cells to die.
Since first discovering the KLF6 gene 13 years ago as a medical student at the Mount Sinai School of Medicine in the laboratory of Dr. Scott Friedman, Dr. Narla has been involved in the identification and characterization of the KLF6 gene and its role in cancer development and the progression of cancer.
Read details at JCI.....

Saturday, June 23, 2012

Caffeine can prevent memory loss in diabetes


Caffeine can prevent memory loss in diabetes: Badly controlled diabetes are known to affect the brain causing memory and learning problems and even increased incidence of dementia, although how this occurs is not clear. But now a study in mice with type 2 diabetes has discovered how diabetes affects a brain area called hippocampus causing memory loss, and also how caffeine can prevent this. 

Friday, June 22, 2012

Isis commences ISIS-APOCIIIRx Phase 2 study in hypertriglyceridemia



Isis Pharmaceuticals, Inc. announced the initiation of a Phase 2 study 
evaluating ISIS-APOCIIIRx in patients with hypertriglyceridemia......


Ref:http://ir.isispharm.com/phoenix.zhtml?c=222170&p=irol-newsArticle_pf&ID=1509616

Wednesday, June 20, 2012

Potential new drugs for fox tapeworm infection in humans

Potential new drugs for fox tapeworm infection in humans: Scientists are reporting development and testing of a new series of drugs that could finally stop the fox tapeworm  which causes a rare but life-threatening disease in humans  dead in its tracks. The report shows that specific organometallic substances that help combat cancer are also the surprising best new hope for a treatment against tapeworm infection.

The group prepared and evaluated several ruthenium complexes (see structure)

as potential drugs against the fox tapeworm. Some were effective in killing the tapeworms and also were less toxic on normal cells in laboratory dish tests, making them prime candidates for further development as treatments for AE.


Tuesday, June 19, 2012

Phase I clinical trial shows drug shrinks melanoma brain metastases

The drug dabrafenib (see structure), which targets the Val600 BRAF mutation that is active in half of melanoma cases, also cut the size of tumors in 25 of 36 patients with late-stage melanoma that had not spread to the brain. The drug also showed activity in other cancer types with the BRAF mutation.

"Nine out of 10 responses among patients with brain metastases is really exciting. No other systemic therapy has ever demonstrated this much activity against melanoma brain metastases," said study co-lead author Gerald Falchook, M.D., assistant professor in the Department of Investigational Cancer Therapeutics at The University of Texas MD Anderson Cancer Center.


Phase I clinical trial shows drug shrinks melanoma brain metastases

Monday, June 18, 2012

Scientists Discover Drug Candidate for Alzheimer’s, Huntington’s

Scientists at the Gladstone Institutes have identified a drug candidate that diminishes the effects of both Alzheimer's disease and Huntington's disease in animal models, offering new hope for patients who currently lack any medications to halt the progression of these two debilitating illnesses.

Gladstone Investigator Paul Muchowski, PhD, has identified a new compound called JM6 in experiments done in collaboration with an international team of researchers, and which are being published today in an online article in Cell. In laboratory tests involving mice genetically engineered to model one or the other of the two diseases, Dr. Muchowski's team found that JM6 blocks kynurenine 3-monooxygenase (KMO), an enzyme that has long been speculated to play a role in neurodegenerative diseases.

In mice modeling Alzheimer's disease, the novel compound prevented memory deficits and the loss of synaptic connections between brain cells—both of which are key features of the human disease. In mice modeling Huntington's disease, JM6 prevented brain inflammation and the loss of synaptic connections between brain cells, while also extending lifespan.

“This discovery has significant implications for two devastating diseases and suggests that the KMO enzyme is a good protein for us to target with medications in diverse neurodegenerative disorders,” said Lennart Mucke, MD, who oversees all neurological research at Gladstone and who won the prestigious Potamkin Prize last year for developing experimental strategies to make the brain more resistant to Alzheimer's. “With any luck, Dr. Muchowski and his colleagues could begin testing this drug in patients within the next two years.”

Remarkably, JM6 (see structure) does not penetrate into the brain, but works by inhibiting KMO in the blood. The blood cells then send a protective signal to the brain, to stabilize brain-cell function and prevent neurodegeneration. The fact that the compound does not pass the so-called blood-brain barrier will facilitate testing in patients, as JM6's potential impact could be confirmed with a simple blood test.

JM6 was named for Dr. Muchowski's father, Dr. Joseph Muchowski, PhD, a retired medicinal chemist who helped his son devise the novel KMO inhibitor. The study was carried out in collaboration with the laboratories of Dr. Robert Schwarcz, a University of Maryland School of Medicine professor who pioneered studies linking KMO and metabolically related enzymes to nerve-cell loss, and Professor Eliezer Masliah at the University of California, San Diego, an expert in neuropathology.

 Ref : www.cell.com/abstract/S0092-8674(11)00581-2

Sunday, June 17, 2012

Positive Results of Diltiazem from Fissure Trial

Ventrus Biosciences Inc. reported positive results from its Phase 3, randomized, double-blind, placebo-controlled clinical trial of diltiazem hydrochloride cream (VEN 307) in patients with anal fissures.

Ventrus' development partner, S.L.A. Pharma, has completed most of the outputs for the statistical analysis plan of the Phase 3 trial, and Ventrus is pleased to communicate the data that they have generated.

The Phase 3 study randomized 465 subjects to diltiazem hydrochloride 4% or 2% w/w cream, or placebo, applied topically three times daily (TID) for 8 weeks, followed by a 4 week blinded observation period. Both 4% and 2% diltiazem treatment arms demonstrated significant improvements compared to placebo in the primary endpoint of average of worst anal pain associated with or following defecation (pain score improvement 0.44, p=0.0108, 4%; 0.43, p=0.0134, 2%) and in the secondary endpoints of overall anal-fissure-related pain (pain score 0.36, p=0.030, 4%; 0.40, p=0.0183, 2%) and anal fissure healing (32.7%, p=0.0181, 4%; 31.2%, p=0.0359, 2%). Pain endpoints were assessed using an 11-point numerical pain rating scale (Likert-like scale).

Adverse events (AEs) were similar for the three treatment arms. Gastrointestinal Disorders were the most common. Reports of headaches were similar in the three arms (14.7% of 4% diltiazem, 12.3% of 2% diltiazem, and 14.2% of placebo). There was one serious adverse event of surgery for hemorrhoid reported in this trial. The study was conducted in 31 centers in Europe by S.L.A. Pharma, the product candidate's licensor. Ventrus holds rights to diltiazem hydrochloride cream in North America.

Based on these results, Ventrus will request a meeting with the U.S. Food and Drug Administration (FDA) to discuss the Phase 3 diltiazem study, as well as steps to move forward toward a New Drug Application (NDA). Because diltiazem is approved in oral formulations for the treatment of angina and high blood pressure, it is eligible for the FDA's 505(b)2 registration pathway. The Company is also preparing to initiate a second pivotal Phase 3 study of VEN 307 in anal fissures in the second half of 2012.

Ref : http://investor.ventrusbio.com/releasedetail.cfm?ReleaseID=672924

Saturday, June 16, 2012

Trial will evaluate resveratrol in Alzheimer's dementia


In continuation of my update on Resveratrol

Researchers at Georgetown University and 25 other U.S. academic institutions affiliated with the Alzheimer's Disease Cooperative Study will be conducting a phase II double-blinded, placebo-controlled trial that will test the effects of resveratrol in Alzheimer's disease patients. "This is the gold-standard for conducting a clinical study because it allows us to objectively determine if resveratrol is offering any benefits," stated Brigid Reynolds, NP, who is the lead researcher for the study's center at Georgetown.

The twelve-month trial, funded by the National Institute on Aging, will enroll men and women age 50 and over with mild to moderate dementia diagnosed as probable Alzheimer's disease and will require one caregiver or friend for each patient. Participants will be initially assigned to 500 milligrams resveratrol or a placebo daily, with dosage to be increased at 13 week intervals to a maximum of 1,000 milligrams twice per day. Lumbar punctures, brain magnetic resonance imaging (MRI) scans, and blood and urine tests will monitor the subjects' progress over the course of ten visits. The researchers hope to determine whether supplementation with resveratrol is helpful in delaying or altering the deterioration of memory and daily function that occurs in Alzheimer's disease.

"Most resveratrol studies showing any health benefits have been conducted in animal models, such as mice, and with doses that far exceed intake from sipping wine or nibbling on chocolate," stated R. Scott Turner, MD, PhD, who is the director of Georgetown University Medical Center's Memory Disorders Program and the national study's lead investigator. "With this clinical trial, we'll find out if daily doses of pure resveratrol can delay or alter memory deterioration and daily functioning in people with mild to moderate dementia due to Alzheimer's."

"During this study, we will also test whether resveratrol improves glucose and insulin metabolism in older individuals -- although those who already have diabetes will not be included in this study," he added....

Friday, June 15, 2012

Ebola, Marburg Virus Treatments Safe in Phase 1 Studies

In continuation of my update on antisense drugs and RNAi

AVI BioPharma Inc. announced positive safety results from the first five cohorts of Phase 1 single ascending dose trials of AVI-6002 and AVI-6003, AVI's lead drug candidates being evaluated for the treatment of the Ebola virus and Marburg virus.

Data were evaluated by an independent Data and Safety Monitoring Board (DSMB), which issued recommendations for both studies to progress as planned to the next highest dosing level after no safety concerns were identified. The Phase 1 single ascending dose trials are designed to characterize the safety, tolerability, and pharmacokinetics of each therapeutic candidate in healthy adult volunteers.

"We are very encouraged that these two drugs, which use our advanced PMOplus chemistry, have demonstrated a favorable safety profile through five cohorts in our dose-escalation studies,”says Chris Garabedian, president and chief executive officer of AVI BioPharma...

Ref : http://phx.corporate-ir.net/phoenix.zhtml?c=64231&p=RssLanding&cat=news&id=1619940

To date, 25 healthy human subjects (five per group) have been enrolled into five sequential dose groups in each of the two studies. Within each group, four subjects received the indicated dose of the therapeutic and one subject received placebo. For each group, safety, clinical laboratory and renal biomarker results through five days after treatment were reviewed by a DSMB. Subjects enrolled in the sixth group for the drug studies will receive 9.0 mg/kg of the therapeutic or placebo. Final, un-blinded safety and pharmacokinetic results for all subjects will be available upon completion of the trial.

Both candidates employ AVI's patented PMOplus technology that selectively introduces positive charges to its phosphorodiamidate morpholino oligomer (PMO) backbone to improve interaction between the drug and its target.

Thursday, June 14, 2012

Tivozanib Improves RCC (renal cell carinomas) Survival

Tivozanib (see structure, AV-951) is an oral VEGF receptor tyrosine kinase inhibitor. It is undergoing clinical trial investigation for the treatment of renal cell carinomas. An oral quinoline urea derivative, tivozanib suppresses angiogenesis by being selectively inhibitory against vascular endothelial growth factor.

The positive results of this Phase 2 trial informed the design and implementation of TIVO-1, a pivotal Phase 3 clinical study in advanced RCC demonstrating tivozanib superiority over sorafenib in the primary endpoint of PFS in the first-line setting, top-line data from which were reported in January 2012.
“Current RCC therapies are associated with toxicities that can interfere with patients’ treatment regimens and impact treatment efficacy and activities of daily living,” said Dmitry A. Nosov, M.D., Ph.D., senior clinical researcher at the Blokhin Oncology Research Center, Moscow, Russian Federation, lead author of the Phase 2 study and TIVO-1 investigator.

“Despite recent progress in treating patients with RCC, patients and physicians would benefit from a new RCC treatment option that delivers both improved efficacy and a more tolerable safety profile. The combined tivozanib efficacy and safety data demonstrated in this Phase 2 study supports tivozanib as a potential advancement in the RCC treatment landscape.”

Based on the positive Phase 2 data and success of the TIVO-1 trial, AVEO and its collaborator Astellas Pharma Inc. are moving forward with plans for submitting the tivozanib NDA in RCC in the third quarter of 2012, with the MAA submission to follow.

“We believe that the efficacy and safety profile consistently demonstrated by tivozanib and recently validated in our Phase 3 TIVO-1 trial represent an important step forward in the treatment of patients who have advanced RCC,” said William Slichenmyer, M.D., Sc.M., chief medical officer, AVEO. “We are pleased with the opportunity to collaborate with tivozanib study investigators on publishing these positive Phase 2 data in the Journal of Clinical Oncology, and look forward to advancing our work with our global partners at Astellas to bring tivozanib to patients who can benefit from this therapy.”....

http://jco.ascopubs.org/content/30/14/1678.abstract?sid=1fe73024-e1cc-481f-acc3-1dc09b596f7f

Wednesday, June 13, 2012

Dalcetrapib Testing Halted..

A second experimental cholesterol medicine in a once-promising class of drugs meant to replace blockbusters such as Lipitor has failed in testing, casting doubt on whether any of the drugs will ever make it to pharmacies.

Swiss drugmaker Roche Holding AG said it has halted testing of its dalcetrapib (see structure), which the company had hoped would become a blockbuster, with eventual annual sales of more than $1 billion. The drug was in expensive late-stage patient testing as a treatment to raise HDL, or so-called good cholesterol, in heart disease patients.

Basel-based Roche said it decided to pull the plug on the recommendation of its independent data and safety monitoring board after an interim analysis, in a study called dal-OUTCOMES, found no "clinically meaningful" benefit.

Ref : http://www.roche.com/media/media_releases/med-cor-2012-05-07.htm

Tuesday, June 12, 2012

Positive Data from aripiprazole intramuscula for Schizophrenia Trial

Otsuka Pharmaceutical Co. Ltd. and H. Lundbeck A/S announced results from a Phase 3 clinical trial evaluating the efficacy, safety and tolerability of once-monthly aripiprazole (see structure) intramuscular (IM) depot formulation for the maintenance treatment of adults with schizophrenia. Trial results were presented in four poster presentations at the 2012 American Psychiatric Association (APA) Annual Meeting in Philadelphia. 


In a 52-week, double-blind, randomized, placebo-controlled study conducted by Otsuka Pharmaceutical Development & Commercialization, Inc. (OPDC), aripiprazole IM depot formulation significantly delayed time-to-impending relapse compared to placebo, the primary endpoint of the study (Hazard ratio = 5.03, p<0.0001). In addition, improvements in the symptoms [as measured by the Positive and Negative Syndrome Scale (PANSS) total score] were maintained throughout the study in patients treated with aripiprazole IM depot formulation, while patients who received placebo reported significantly worsening scores (mean change from baseline at week 52 was 1.4 for aripiprazole IM depot formulation compared to 11.6 for placebo; LOCF analysis, p<0.0001).

Canagliflozin Provided Substantial and Sustained Glycemic Improvements as Monotherapy and in Add-On Combinations in Adults with Type 2 Diabetes in Five Phase 3 Studies

Canagliflozin is an experimental drug being developed by Johnson & Johnson for the treatment of type 2 diabetes. It is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine..

Monday, June 11, 2012

Lilly, Boehringer Ingelheim announce results from linagliptin Phase III trial on T2D

 In continuation of my update on Linagliptin



Results of the one Phase III study presented (Poster No. 999-P) showed that linagliptin was effective as an add-on therapy to basal insulin alone or in combination with metformin and/or pioglitazone in reducing blood glucose levels in adult patients with T2D, when compared to placebo as an add-on to these background therapies. Linagliptin demonstrated a placebo-adjusted reduction in HbA1c of 0.65% (p<0.0001) from a baseline HbA1c of 8.3% at 24 weeks without weight gain or additional risk of hypoglycaemia.  HbA1c is measured in people with diabetes to provide an index of blood glucose control for the previous two to three months. 

A post-hoc analysis from a second Phase III trial (Poster No. 1044-P) found that in hyperglycaemic patients on a background of metformin randomised to add linagliptin or glimepiride, a greater proportion of patients taking linagliptin achieved target HbA1c <7% without weight gain and/or hypoglycaemia than those taking glimepiride after 104 weeks (linagliptin 54% versus glimepiride 23%) while comparably improving blood glucose levels.

Drug kills cancer cells by restoring faulty tumor suppressor

A new study describes a compound that selectively kills cancer cells by restoring the structure and function of one of the most commonly mutated proteins in human cancer, the "tumor suppressor" p53. The research, published by Cell Press in the May 15th issue of the journal Cancer Cell, uses a novel, computer based strategy to identify potential anti-cancer drugs, including one that targets the third most common p53 mutation in human cancer, p53-R175H. 

Restoring the function of mutant p53 with a drug has long been recognized as an attractive cancer therapeutic strategy," explains senior study author, Dr. Darren R. Carpizo, from The Cancer Institute of New Jersey. "However, it has proven difficult to find compounds that restore the lost function of a defective tumor-suppressor."

Using the National Cancer Institute's anticancer drug screen data researchers identified two compounds from the thiosemicarbazone family that manifest increased growth inhibitory activity in mutant p53 cells, particularly for the p53R175 mutant. Mechanistic studies reveal that NSC319726 (see structure) restores WT structure and function to the p53R175 mutant. 


This compound kills p53R172H knockin mice with extensive apoptosis and inhibits xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner. This activity depends upon the zinc ion chelating properties of the compound as well as redox changes. These data identify NSC319726 as a p53R175 mutant reactivator and as a lead compound for p53-targeted drug development.

Drug kills cancer cells by restoring faulty tumor suppressor

Combination of vaccine and letrozole effectively improves survival from breast cancer

In continuation of my update on Letrozole

Combination of vaccine and letrozole effectively improves survival from breast cancer: A vaccine that targets cancer cells in combination with the drug letrozole, a standard hormonal therapy against breast cancer, significantly increased survival when tested in mice, a team of UC Davis investigators has found.

Sunday, June 10, 2012

Pungent Ingredient, piperine, in Black Pepper Targets Fat Cells

A preliminary new study suggests that the pungent component in black pepper known as piperine fights fat by blocking the formation of new fat cells.
If further studies confirm these effects, researchers say black pepper may offer a natural alternative for the treatment of fat-related disorders like obesity.

"Our findings suggest that piperine (see above structure), a major component of black pepper, inhibits fat cell differentiation ... thus leading to its potential use in the treatment of obesity-related diseases," writes researcher Ui-Hyun Park of Sejong University in Seoul, Korea 
Black Pepper the Fat Fighter....

Researchers say the benefits of black pepper and the black pepper plant have been known for centuries in traditional Eastern medicine, in which it is used to treat cholera, diarrhea, and other gastrointestinal issues.

In their study, researchers looked at the effects of piperine on gene expression in fat tissue in the lab and in computer models.

The results showed that piperine interfered with the activity of genes responsible for forming new fat cells.

Researchers say this benefit of black pepper sets up a chain reaction that helps keep the formation of fat in check in other ways as well.
"Overall, our results suggest that piperine could be a lead natural compound for the treatment of fat-related disorders," the researchers write.

Saturday, June 9, 2012

Topical Gel (from Euphorbia peplus) Treats Precancerous Skin Condition, Actinic Keratosis


A new prescription gel may quickly treat a common precancerous skin condition called actinic keratosis, a new study shows.

The gel is derived from the sap of the Euphorbia peplus plant. This has long been used as a folk remedy for skin lesions.

The new gel, Picato (ingenol mebutate, see below structure), is applied once daily for two or three days, depending on the area being treated. Other available topical treatments must be used for several weeks, and often irritate the skin. Cryotherapy, or freezing the affected skin area, is also used but can sometimes leave a scar.

Because the new gel is only used for a few days, any irritation is usually short-lived. The short duration also makes people more likely to stay the course, another advantage, according to the study’s authors.

“The shorter application period is what makes ingenol mebutate a breakthrough in the treatment of actinic keratosis,” researcher Mark Lebwohl, MD, says in a news release. He is a professor and chair of the department of dermatology at Mount Sinai School of Medicine in New York City.

Friday, June 8, 2012

Experimental cholesterol drug, REGN727 (PCSK9 inhibitor) results called ‘game changing

In continuation on my update on drug discovery in the class of  Monoclonal antibodies



Researchers have known for some time that when the protein PCSK9, (below structure) which stands for proprotein convertase subtilisin/kexin 9, binds to LDL receptors on the liver, it compromises the organ’s ability to filter the bad cholesterol from the blood.

Too much LDL cholesterol circulating in the blood can lead to the thickening of artery walls, making them less flexible and therefore impairing their function and increasing the risk of heart disease.

In a phase one clinical trial, which is designed to determine if a drug is safe, researchers found that using a monoclonal antibody (lab-produced protein) called REGN727, was not only safe, but effectively blocked PCSK9 and therefore signficantly reduced bad cholesterol in healthy patients as well as those also taking the popular cholesterol-lowering drug Lipitor.


“Wars for PCSK9 are far bigger than the statin wars,” said Dr. Evan A Stein, lead author of the study and researcher at the Metabolic and Atherosclerosis Research Center in Cincinnati, Ohio. “This is a hot research area and everybody is so close together.”

The REGN727 study included three trial arms. Two arms used 72 healthy volunteers who were either injected with a single dose of the drug in increasing amounts to test for side effects, which is the purpose of a phase one clinical trial.  A third arm included 21 people with a family history of high cholesterol, and 30 people with nonfamilial high cholesterol. All of those subjects were also receiving treatment with the statin Lipitor.

A control group of subjects with nonfamilial high cholesterol was treated only with a special diet.  None of the subjects who received REGN727 discontinued the study because of adverse effects, and the subjects who received REGN727 had a striking reduction of 60 to 65%  in LDL cholesterol, according to Stein.

A PCSK9 inhibitor, Stein said, differs from statins “because it’s unlike any other drug. With statins you get toxicity – with these drugs we don’t see any side effects with the antibody.”

In an accompanying editorial, authors Dr. Stephen G. Young, and Loren G. Fong, Ph.D. write: “At this point, the status of PCSK9 therapeutics appears to be full speed ahead. Soon, we can expect more human trials in which investigators will dissect the properties of different PCSK9 antibodies and assess the effect of these agents.”

However, without long-term safety data and evidence that PCSK9 inhibitors truly help prevent heart disease, Young and Fong caution that it will remain unclear how important this class of drugs will be.

The cost of this drug will also play a role in determining which patients might use it, Fong and Young say.  But they also note that “patients who cannot tolerate statins could benefit greatly.”


Researchers also claim that,  the study methodology was thorough because it included people with high cholesterol as well as people with genetic familial high cholesterol, which is proven to be a result of impaired PCSK9 genetic function.

Researchers have known for some time that when the protein PCSK9, which stands for proprotein convertase subtilisin/kexin 9, binds to LDL receptors on the liver, it compromises the organ’s ability to filter the bad cholesterol from the blood.

Researchers conclude that, In three phase 1 trials, a monoclonal antibody to PCSK9 significantly reduced LDL cholesterol levels in healthy volunteers and in subjects with familial or nonfamilial hypercholesterolemia.

Wednesday, June 6, 2012

Soy Supplements Can Cool Hot Flashes



In continuation of my update on Soy...

Taking soy to relieve hot flashes has received mixed reviews over the years. Now, researchers who took another look at 19 published studies find that soy supplements may help, at least over time. Soy has been touted as an alternative treatment to hormone replacement therapy after HRT was linked to an increased risk of breast cancer.

“For many women with symptoms and especially with concerns about hormone replacement therapy, trying soy for six to 12 weeks to see if it relieves their symptoms could be a first line of treatment,” says Melissa Melby, PhD, a professor of medical anthropology at the University of Delaware.
Researchers conclude that, Soy isoflavone supplements, derived by extraction or chemical synthesis, are significantly more effective than placebo in reducing the frequency and severity of hot flashes. Additional studies are needed to further address the complex array of factors that may affect efficacy, such as dose, isoflavone form, baseline hot flash frequency, and treatment duration.


Ref : http://journals.lww.com/menopausejournal/Abstract/publishahead/Extracted_or_synthesized_soybean_isoflavones.98844.aspx

Tuesday, June 5, 2012

Lorcaserin Receives Positive Vote From FDA Advisory Committee

In continuation of my update on Lorcaserin

(FDA) Endocrinologic and Metabolic Drugs Advisory Committee voted 18 to 4, with one abstention, that the available data demonstrate that the potential benefits of lorcaserin outweigh the potential risks when used long-term in a population of overweight and obese individuals. Lorcaserin is an investigational drug candidate intended for weight management, including weight loss and maintenance of weight loss, in patients who are obese (BMI greater than or equal to 30) or patients who are overweight (BMI greater than or equal to 27) and have at least one weight-related co-morbid condition.
"The advisory committee's positive vote supports our belief in lorcaserin as a potential new treatment option for the medical management of overweight and obesity," said Jack Lief, Arena's President and Chief Executive Officer. "We will continue to work with the FDA as the agency completes its review of the lorcaserin new drug application."

Monday, June 4, 2012

Curry spice component may help slow prostate tumor growth

In continuation of my update on curcumin,,,,

Curcumin, an active component of the Indian curry spice turmeric, may help slow down tumor growth in castration-resistant prostate cancer patients on androgen deprivation therapy (ADT), a study from researchers at Jefferson's Kimmel Cancer Center suggests. More

 Curry spice component may help slow prostate tumor growth

Sunday, June 3, 2012

2 Drugs Better Than 1 to Treat Youth With Type 2 Diabetes

2 Drugs Better Than 1 to Treat Youth With Type 2 DiabetesA combination of two diabetes drugs, metformin and rosiglitazone, was more effective in treating youth with recent-onset type 2 diabetes than metformin alone, a study funded by the National Institutes of Health (NIH) has found. Adding an intensive lifestyle intervention to metformin provided no more benefit than metformin therapy alone.

The study also found that metformin therapy alone was not an effective treatment for many of these youth. In fact, metformin had a much higher failure rate in study participants than has been reported in studies of adults treated with metformin alone.
The study found that treatment with metformin alone was inadequate for maintaining acceptable, long-term, blood glucose control in 51.7 percent of youth over an average follow-up of 46 months. The failure rate was 38.6 percent in the metformin and rosiglitazone group, a 25.3 percent reduction from metformin alone. In the metformin plus lifestyle group the failure rate was 46.6 percent.

Saturday, June 2, 2012

A trial looking at curcumin and FOLFOX for advanced bowel cancer (CUFOX)

In continuation of  my update on curcumin
An upcoming clinical trial conducted by the Cancer Research UK and National Institute for Health Research Experimental Cancer Medicine Centre (ECMC) in Leicester, England will evaluate the effectiveness of curcumin, a compound that occurs in turmeric, as a means of improving the results of standard chemotherapy for metastatic colon cancer. The compound has been found to enhance chemotherapy's ability to kill colon cancer cells in previous research involving cell cultures. 

Doctors often treat bowel cancer that has spread with chemotherapy. The combination of chemotherapy they usually use is called FOLFOX. It is made up of the drugs folinic acid (leucovorin), fluorouracil (5FU) and oxaliplatin. But this doesn’t always work very well.  And it often causes side-effects such as numbness and tingling in hands and feet (peripheral neuropathy). This means the doctors sometimes need to lower the dose or even stop chemotherapy, so they are keen to improve treatment.

Curcumin is a plant extract found in the spice turmeric and is found in many everyday foods. We know from research that curcumin can help shrink tumours in the laboratory. It has also been used in several studies involving patients with a range of conditions, including cancer.



Friday, June 1, 2012

FDA AAC recommends approval of Pfizer’s tofacitinib for RA

In continuation of my update on  Tofacitinib...

FDA AAC recommends approval of Pfizer’s tofacitinib for RA: Pfizer Inc. the Arthritis Advisory Committee to the U.S. Food and Drug Administration (FDA) voted 8-2 to recommend approval of the investigational agent tofacitinib for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA). The Committee's recommendation will be considered by the FDA in its review of the New Drug Application (NDA) for tofacitinib. The FDA has provided an anticipated Prescription Drug User Fee Act (PDUFA) action date in August 2012. If approved by the FDA, tofacitinib would be the first new oral disease-modifying antirheumatic drug (or DMARD) for RA in more than 10 years and the first RA treatment in a new class of medicines known as Janus kinase (JAK) inhibitors..