Friday, August 31, 2012

Combination [of Vismodegib (GDC-0449) and Gemcitabine] therapy may help defeat pancreatic cancer

 In continuation of my update on (GDC-0449) Visodegib and Gemcitabine
GDC-0449 targets the Smoothened (SMO) protein in the Hedgehog signaling pathway. It was approved for use in basal cell carcinoma and is marketed as vismodegib. Kim and his colleagues felt that treating patients with pancreatic cancer first with GDC-0449 and then with the standard chemotherapeutic drug gemcitabine might disrupt the desmoplastic stroma and improve the efficacy of the chemotherapy. 

They evaluated this strategy in treatment-naive patients with advanced pancreatic cancer. Patients underwent needle biopsies of the cancer before and after taking GDC-0449 for three weeks to study the effects of GDC-0449 on the Hedgehog pathway signals, tumor stroma and pancreatic cancer stem cells. Gemcitabine was added to GDC-0449 following the second biopsy.

Thursday, August 30, 2012

Keryx Biopharmaceuticals Announces Top-Line Data from the Perifosine (KRX-0401) X-PECT Phase 3 Clinical Trial

Keryx Biopharmaceuticals, Inc. reported today that the Phase 3 "X-PECT" (Xeloda® + Perifosine Evaluation in Colorectal cancer Treatment) clinical trial evaluating perifosine (KRX-0401) + capecitabine (Xeloda) in patients with refractory advanced colorectal cancer did not meet the primary endpoint of improving overall survival versus capecitabine + placebo.

This Phase 3 trial was conducted pursuant to a Special Protocol Assessment (SPA) agreement with the FDA.  468 patients at sixty-five U.S. sites participated in this study. 

Ron Bentsur, Chief Executive Officer of Keryx, stated, "We are all extremely disappointed with the results of the study.  We thank the investigators who participated in what we believe was a well-run study, despite the outcome.  We will evaluate whether our Phase 3 study of Perifosine in relapsed/refractory multiple myeloma will continue as planned."
Mr. Bentsur commented further, "With approximately $31 million in cash as of March 31, 2012, and a well-controlled burn rate, we plan to focus our resources on the pending completion of the Zerenex (ferric citrate) long-term Phase 3 study for end stage renal disease (ESRD) patients with hyperphosphatemia, expected in the fourth quarter of 2012, and the New Drug Application (NDA) filing for Zerenex which will hopefully follow shortly thereafter."

KRX-0401 (perifosine) is in-licensed by Keryx from AeternaZentaris Inc. in the United States, Canada and Mexico.

Ref :

Wednesday, August 29, 2012

Cancer publishes Aeterna Zentaris' perifosine Phase 2 trials in RCC


In the Perifosine 228 trial, 1 patient achieved a partial response (objective response rate, 4%; 95% confidence interval, 0.7%-20%), and 11 patients (46%) had stable disease as their best response. The median progression-free survival was 14.2 weeks (95% confidence interval, 7.7-21.6 weeks). In the Perifosine 231 trial, 5 patients achieved a partial response (objective response rate, 10%; 95% confidence interval, 4.5%-22.2%) and 16 patients (32%) had stable disease as their best response. The median progression-free survival was 14 weeks (95% confidence interval, 12.9, 20.7 weeks). Overall, perifosine was well tolerated, and there were very few grade 3 and 4 events. The most common toxicities included nausea, diarrhea, musculoskeletal pain, and fatigue.


Although perifosine demonstrated activity in patients with advanced RCC after failure on VEGF-targeted therapy, its activity was not superior to currently available second-line agents. Nonetheless, perifosine may be worthy of further study in RCC in combination with other currently available therapies. 

Ref :

 Cancer publishes Aeterna Zentaris' perifosine Phase 2 trials in RCC//

Tuesday, August 28, 2012

Drug shows promise as skin cancer treatment

In continuation of my update on Vismodegib

Drug shows promise as skin cancer treatment: A new vismodegibdrug for a type of skin cancer caused by a rare genetic disease can not only substantially shrink the tumors, but can also prevent the growth of new cancers, US investigators have discovered.

Monday, August 27, 2012

Health Canada approves Sunovion’s LATUDA NDA to treat schizophrenia

In continuation of my update on Lurasidone..

Health Canada approves Sunovion’s LATUDA NDA to treat schizophrenia: Sunovion Pharmaceuticals Canada Inc. today announced that the New Drug Submission (NDS) for LATUDA (lurasidone HCl), for the treatment of adult patients with acute schizophrenia has been approved by Health Canada.

Sunday, August 26, 2012

Insomnia Drug Closer to Approval | News | Drug Discovery and Development Magazine

Merck & Co. said that its experimental insomnia drug suvorexant (see structure) helped patients fall asleep faster and stay asleep longer in two late-stage tests of the drug, seen as a potential blockbuster in a multibillion-dollar market. 

Merck said the drug worked better than a placebo at measurements including total sleep time, time to falling asleep, and continuous sleep after one month and three months of treatment. The company said patients reported better results on suvorexant compared with placebo, and their sleeping habits also were measured electronically.

Suvorexant is a new type of insomnia drug designed to help patients sleep while minimizing morning grogginess. It is one of Merck's major drug candidates. The company plans to file for U.S. marketing approval this year, and it is one of six planned product filings for Merck in 2012 and 2013.

The two trials involved more than 2,000 patients who had insomnia that was not caused by another medical problem. The most common side effects of suvorexant were tiredness and headache.

Saturday, August 25, 2012

Two Possible Treatments for Bipolar Disorder Found

Researchers at the University of Leeds investigating the genetic causes of bipolar disorder have identified two new drugs – one of which has already been found safe in clinical trials – that may be effective in treating the disorder.

Bipolar disorder is characterised by mood swings between mania and depression. Like autism, it is thought to be a spectrum of disorders and, although its causes are not well understood, it seems to run in families and is thought to be caused by both genetic and environmental factors.

Dr Steve Clapcote, of the Institute of Membrane and Systems Biology at the University of Leeds, who led the study, says: "We suspected from published studies of bipolar patients that levels of enzymes known as NKA or sodium pumps may be abnormal in bipolar disorder, but so far the evidence has not been convincing enough to warrant detailed clinical investigations."

The research, published today in the US journal Proceedings of the National Academy of Sciences (PNAS), used a strain of genetically modified mice that exhibit symptoms very similar to humans in the manic phase of the disorder.
The mice were bred with a particular mutation that prevents the NKA enzyme from functioning normally. When tested, the mice showed characteristics closely associated with bipolar disorder, such as increased tendency to take risks, hyperactivity, and disturbed sleep patterns. They also exhibited reduced mania when treated with anti-manic drugs.

Current drugs available to treat bipolar disorders, although usually successful, are limited to either Lithium or Valproate. They can't be matched to specific types of bipolar disorder, and can sometimes cause unpleasant side effects. There is therefore a need for treatments which can be better targeted, and which are more effective and better tolerated by patients.

The Leeds researchers found that the mice showed decreased activity of the NKA enzyme, as well as increased activity of a protein called ERK. Drugs known to have an effect on these two elements were administered to the mice, including Rostafuroxin and SL327 (see structure right), and both reduced their mania-like behaviour.

"Rostafuroxin (see structure left) has been found to be safe in clinical trials for treating high blood pressure," explained Dr Clapcote. "No one has previously looked at this drug's effects on the brain, but our mouse studies show there's a possibility that it might also be suitable for people with mania. Similarly, SL327, which is known to inhibit ERK activity, was also found to reduce manic behaviour in the mice."

"We think there is enough evidence now to start screening people with bipolar disorder to look for genetic mutations in the same NKA enzyme as that affected in our mice," says Dr Clapcote. "This will help us identify whether there is a group of bipolar patients that may be responsive to the novel treatments we have tested in the mice."....

Friday, August 24, 2012

Reformulated Copaxone Meets Goals........

Teva Pharmaceutical Industries Ltd. said that a new version of its multiple sclerosis drug Copaxone met its goals in a late-stage clinical trial.....

We know that, COPAXONE is the brand name for glatiramer acetate (formerly known as copolymer-1). Glatiramer acetate, the active ingredient of COPAXONE (glatiramer acetate) , consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies.

Chemically, glatiramer acetate is designated L-glutamic acid polymer with L-alanine, L-lysine and L-tyrosine, acetate (salt). Its structural formula is:

(Glu, Ala, Lys, Tyr)x•xCH3COOH
CAS - 147245-92-9

COPAXONE (glatiramer acetate) is a clear, colorless to slightly yellow, sterile, nonpyrogenic solution for subcutaneous injection. Each 1 mL of solution contains 20 mg of glatiramer acetate and 40 mg of mannitol. The pH range of the solution is approximately 5.5 to 7.0. The  biological activity of COPAXONE (glatiramer acetate) is determined by its ability to block the induction of experimental autoimmune encephalomyelitis (EAE) in mice.

Thursday, August 23, 2012

New action for ancient heart drug

Since the 13th century, the herb and poisonous plant Foxglove has been used to cleanse wounds and its dried leaves were carefully brewed by Native Americans to treat leg swelling caused by heart problems. Digoxin (see structure), the active ingredient in digitalis, or the poisonous plant Foxglove, can enhance the body's own protective mechanism against high blood pressure and heart failure.
High blood pressure can be prevented by reducing salt intake, being active and keeping a healthy weight, but about 1 in 3 Americans has high blood pressure, also called hypertension, which can damage the body in many ways.  Most current treatments prevent excess hormone and stress signals that can lead to high blood pressure and heart failure.

But recent studies have found that the body has the ability to keep excess stimulation in check through production of a family of inhibitors called RGS proteins. Researchers looked for ways to "re-purpose" old drugs to tap into this protective mechanism which is lost among some individuals with high blood pressure and heart failure. 


Tuesday, August 21, 2012

Promising preliminary data for axitinib in metastatic kidney cancer

In continuation of my update on Axitinib

Promising preliminary data for axitinib in metastatic kidney cancer: Preliminary study data show that axitinib may be an effective first-line treatment for metastatic renal cell carcinoma, particularly in patients with high therapeutic drug exposure and a rise in blood pressure during the first 2 weeks of treatment, researchers report.

Licensed from Medwire news with permission from Springer Healthcare Ltd. ©Springer Healthcare Ltd. All rights reserved. Neither of these parties endorse or recommend any commercial products, services, or equipment.

Monday, August 20, 2012

Investigational ultra-long-acting insulin degludec reduces rates of nocturnal hypoglycaemia in type 2 diabetes patients versus insulin glargine...

Ultra-long-acting insulin degludec, (see structure) an investigational insulin being developed by Novo Nordisk, significantly reduced the rate of hypoglycaemia* at night in adults with type 2 diabetes while obtaining equivalent improvement in glucose control compared with insulin glargine over a 52-week period. This phase 3a study was presented  at the 72nd Scientific Sessions of the American Diabetes Association (ADA). 

The study also found that insulin degludec had significantly lower rates of severe hypoglycaemia compared to insulin glargine.

"Nocturnal, or night-time, hypoglycaemia is a particular challenge for people living with diabetes, as these episodes are often unpredictable and difficult to detect", said Bernard Zinman, lead author and director of the diabetes centre at Mount Sinai Hospital, and professor of medicine, University of Toronto: "This study demonstrated that treatment with insulin degludec significantly reduced the rate of nocturnal hypoglycaemia". 

This randomised, open-label, non-inferiority, treat-to-target trial compared efficacy and safety of insulin degludec to insulin glargine. Both insulins were given once-daily in 1,030 insulin-naïve type 2 diabetes adults inadequately controlled with oral anti-diabetic medications.

Findings of the study include:
  • Nocturnal hypoglycaemic rates were significantly lower by 36% with insulin degludec than with insulin glargine (0.25 versus 0.39 episodes per patient per year; p=0.04).
  • Overall confirmed hypoglycaemic rates were 1.52 versus 1.85 episodes per patient per year for insulin degludec and insulin glargine respectively (p=0.11).
  • Overall severe hypoglycaemia was infrequent in both treatment populations, but it was significantly lower with insulin degludec than with insulin glargine (0.003 versus 0.023 episodes/patient-year; p=0.02).
  • At one year, this noninferiority, treat-to-target trial demonstrated comparable HbA1c reductions with insulin degludec versus insulin glargine (-1.06% versus -1.19%).**
  • Fasting plasma glucose (FPG) reductions were significantly greater with insulin degludec than with insulin glargine (-67.7 versus -59.5 mg/dl, estimated treatment difference (EDT) -7.7 mg/dl, p=0.005).
Overall adverse event rates were low and similar between groups.

Sunday, August 19, 2012

Zafgen announces new data from two Phase 1 studies of beloranib on obesity

Zafgen announces new data from two Phase 1 studies of beloranib on obesity: Zafgen, Inc., the world's first biopharmaceutical company dedicated to addressing the unmet need of severely obese patients, today announced new data from two Phase 1 studies of beloranib, a selective methionine aminopeptidase 2 inhibitor (MetAP2), which showed significant weight loss and improvements in cardiometabolic risk markers in severely obese women.

Treatment with beloranib (see structure) was associated with improvements in weight loss and triglycerides, LDL cholesterol, waist circumference and diastolic blood pressure, with no evidence of major tolerability or safety issues.  Body composition measured in one study indicated a reduction in fat mass with beloranib.  

Saturday, August 18, 2012

Turmeric stopped potentially deadly Rift Valley fever virus from multiplying in infected cells

In continuation of my update on curcumin.....

Curcumin,  found in turmeric  stopped the potentially deadly Rift Valley Fever virus from multiplying in infected cells, says Aarthi Narayanan, lead investigator on a new study and a research assistant professor in Mason's National Center for Biodefense and Infectious Diseases.

Dapagliflozin more effective than sitagliptin for adult patients with type 2 diabetes

In continuation of my update on dapagliflozin and sitagliptin

The study also demonstrated significant reductions in total body weight and fasting plasma glucose (FPG) levels in patients taking dapagliflozin added to sitagliptin (with or without metformin), with results maintained throughout the duration of the study extension.

Patients were actively questioned at each study visit for signs, symptoms or events suggestive of genital infections and urinary tract infections. These events were more frequent with the dapagliflozin treatment group compared to the placebo treatment group, and were generally mild to moderate in intensity, with most patients responding to standard treatment.
"Type 2 diabetes is a complex disease that often requires patients to take multiple treatments to control their blood sugar levels, with DPP4 inhibitors being some of the most widely prescribed therapies," said Serge Jabbour, M.D., Division Director of Endocrinology, Thomas Jefferson University. "In this study, dapagliflozin, in addition to diet and exercise, resulted in reduced blood sugar levels when added to sitagliptin, a DPP4 inhibitor. These findings add to our understanding of the effect of dapagliflozin in combination with commonly prescribed type 2 diabetes treatments."

Bristol-Myers Squibb Company and AstraZeneca today announced results from a Phase 3 clinical study that showed the investigational compound dapagliflozin 10 mg demonstrated significant reductions in blood sugar levels (glycosylated hemoglobin levels, or HbA1c) compared with placebo at 24 weeks when either agent was added to existing sitagliptin therapy (with or without metformin) in adult patients with type 2 diabetes.

Friday, August 17, 2012

FDA accepts Avanir IND for AVP-923 to treat agitation in patients with AD

FDA accepts Avanir IND for AVP-923 to treat agitation in patients with AD: Avanir Pharmaceuticals, Inc. today announced that the U.S. Food and Drug Administration (FDA) accepted the company's Investigational New Drug (IND) application for the study of AVP-923, an investigational drug for the treatment of agitation in patients with Alzheimer's disease (AD).

"This marks the fourth IND for the AVP-923 (AVP-923, a combination of    dextromethorphan  hydrobromide   and quinidine sulfate, see the structures from left to right respectively)

program, reflecting our belief that the unique dual sigma-1 and NMDA receptor pharmacology has significant potential," saidJoao Siffert, MD, senior vice president of R&D at Avanir Pharmaceuticals. "With no approved treatments for agitation in patients with Alzheimer's disease, this remains an area of tremendous unmet medical need. We look forward to initiating our clinical research program later this year." 

Thursday, August 16, 2012

Lexicon presents six posters on LX4211 at ADA meeting

Lexicon presents six posters on LX4211 at ADA meeting: Lexicon Pharmaceuticals, Inc. will present six posters summarizing the mechanism of action and safety of LX4211, a dual inhibitor of sodium glucose transporters 1 and 2 (SGLT1 and SGLT2) currently in mid-stage development for type 2 diabetes, at the 72nd Scientific Sessions of the American Diabetes Association (ADA) in Philadelphia, Pennsylvania during the Saturday morning poster session on June 9, 2012. 

Lexicon has completed dosing in a Phase 2b study of LX4211 in 299 patients with type 2 diabetes and expects to report top-line results at the end of June.

Wednesday, August 15, 2012

Amylin announces results from SYMLIN clinical studies on type 2 or 1 diabetes

Amylin announces results from SYMLIN clinical studies on type 2 or 1 diabetes: Amylin Pharmaceuticals, Inc. today announced results from new analyses of previously completed clinical studies demonstrating that patients with type 2 or type 1 diabetes achieved a greater proportion of blood glucose measurements in the normal range when SYMLIN (pramlintide acetate, see structure) injection treatment was used along with insulin...

Ref :

Tuesday, August 14, 2012

Amylin, Alkermes announce results from BYDUREON clinical study on type 2 diabetes

 In continuation of my update on Bydureon

We know that, Exenatide (marketed as Byetta, Bydureon see structure) is a medication approved in April 2005 for the treatment of diabetes mellitus type 2. It belongs to the group of incretin mimetics and is manufactured by Amylin Pharmaceuticals. Exenatide in its Byetta form is administered as a subcutaneous injection (under the skin) of the abdomen, thigh, or arm, any time within the 60 minutes before the first and last meal of the day. A once-weekly injection has been approved as of January 27, 2012 under the trademark Bydureon. 

Now Amylin Pharmaceuticals, Inc. (Nasdaq: AMLN) and Alkermes plc (Nasdaq: ALKS) today announced results from the long-term extension of the DURATION-1 study, which showed that BYDUREON™ (exenatide extended-release for injectable suspension), the first and only once-weekly treatment for type 2 diabetes, was associated with clinically significant and sustained improvements in glycemic control during four years of treatment in adults with type 2 diabetes.......

Monday, August 13, 2012

Savient announces results from KRYSTEXXA Phase III trials on gout-related kidney disease

Post-hoc analysis evaluated more than 200 patients with CKD stages one through four (n=34, 74, 80, 23, respectively) who were randomized to receive treatment with KRYSTEXXA (pegloticase, see structure) 8 mg every other week, 8 mg every four weeks or placebo. Baseline CKD stage was similar across treatment arms, and there was no significant difference in rates of response to KRYSTEXXA by CKD stage (p<0.311). Additionally, treatment with KRYSTEXXA did not impact estimated GFR levels in patients with or without CKD. Similar results were seen in a 24-month open-label extension study.                 

In another study presented as a poster at EULAR, 35 percent of patients diagnosed with gout in Western Europe reported experiencing pain in the last 30 days (versus 20 percent in the control group of those who did not report gout; p<0.05).  Of those patients, 23 percent reported severe daily pain (versus 13.5 percent in control group; p<0.05), which impacted quality of life as assessed by the SF-12 health outcome measurement tool.  Based on study data, it is estimated that one in five gout patients in Western Europe experiences moderate to severe daily pain, one of the symptoms of gout.

Savient announces results from KRYSTEXXA Phase III trials on gout-related kidney disease: Savient Pharmaceuticals, Inc. announced new data presented in an oral session at the European League Against Rheumatism (EULAR) 2012 congress showed that patients with refractory chronic gout (RCG) who also suffer from chronic kidney disease (CKD) responded to treatment with KRYSTEXXA (pegloticase) regardless of baseline CKD stage.

Sunday, August 12, 2012

AB Science announces data from development program of masitinib in GIST

In continuation of my update on Masitinib
AB Science announces data from development program of masitinib in GIST: AB Science SA, a pharmaceutical company specializing in the research, development and commercialization of protein kinase inhibitors (PKIs), announces today that data from the development program of masitinib in gastrointestinal stromal tumors (GIST) have been presented as part of three presentations delivered at the American Society of Clinical Oncology (ASCO) 2012 Annual Meeting, 1-5 June in Chicago, Illinois.

Saturday, August 11, 2012

Three-drug regimen provides rapid, durable responses for multiple myeloma

In continuation of my update on three drug combination
A three-drug treatment for the blood cancer multiple myeloma provided rapid, deep and potentially durable responses, researchers report today online in Blood, the Journal of the American Society of Hematology, and yesterday, Sunday, June 3, 2012, at the American Society of Clinical Oncology's Annual Meeting in Chicago, IL, USA.

The researchers, led by Andrzej J. Jakubowiak, MD, PhD, professor of medicine and director of the multiple myeloma program at the University of Chicago Medical Center, found that combining carfilzomib, a next generation proteasome inhibitor, with two standard drugs -- lenalidomide and low-dose dexamethasone compared favorably to other frontline regimens.
The longer patients stayed on the therapy, the better their response. After at least eight 28-day cycles of treatment, 61 percent of the 36 patients who remained on the therapy had a stringent complete response, defined as no detectable tumor cells or myeloma protein in the blood or bone marrow; 78 percent had at least a near complete response. More than 90 percent of patients had no progression of their disease at two years.
"These rapid and durable response rates are higher than those achieved by the best established regimens for newly diagnosed multiple myeloma," said Jakubowiak. "We have observed excellent efficacy, the best reported to date, and very good tolerability, including limited peripheral neuropathy that has been problematic with other drug combinations."

 Ref :

Friday, August 10, 2012

HIV drug may slow down metastatic breast cancer

The HIV drugs known as CCR5 antagonists (Maraviroc or Vicriviroc see below structures from left to right respectively) may also help prevent aggressive breast cancers from metastasizing, researchers from the Kimmel Cancer Center at Jefferson suggest in a preclinical study. 

Such drugs target the HIV receptor CCR5, which the virus uses to enter and infect host cells, and has historically only been associated with expression in inflammatory cells in the immune system. Researchers have now shown, however, that CCR5 is also expressed in breast cancer cells, and regulates the spread to other tissue.

What's more, blocking the receptor with the CCR5 antagonists Maraviroc and Vicriviroc, two drugs that slow down the spread of the HIV virus by targeting the CCR5 co-receptor of the chemokine CCL5, also prevents migration and spread of basal breast cancer cells, the researchers found.

"These results are dramatic," said Richard Pestell, M.D., Ph.D., FACP, Director of Jefferson's Kimmel Cancer Center and Chair of the Department of Cancer Biology at Thomas Jefferson University, and study senior author. "Our team showed that the CCR5/CCL5 axis plays a key role in invasiveness, and that a CCR5 antagonist can slow down the invasion of basal breast cancer cells."

"This suggests it may prove to be a viable adjuvant therapy to reduce the risk of metastasis in the basal breast cancer subtype," he added.

Basal tumors, which do not express the androgen or estrogen receptors or HER-2, are typically associated with metastasis and often do not respond to hormonal therapies. Current treatments include chemotherapy, radiation, and surgery, but all demonstrate poor outcomes, thus highlighting the urgent need for a specific targeted therapy for the subtype.

More :

Thursday, August 9, 2012

New drug found effective against rare form of basal cell skin cancer

In continuation of my up date on vismodegib..

A clinical study has demonstrated that a new drug, a targeted molecular therapy called vismodegib (trade name Erivedge™), can dramatically shrink basal cell skin cancers and prevent the formation of new ones, in patients with basal cell nevus syndrome (BCNS). This rare genetic condition causes dozens, and sometimes hundreds or thousands, of skin cancers on each patient's body. The primary treatment option is surgical removal. These study results are significant as they indicate the possibility of an alternative treatment with oral medication; although side effects remain a consideration. 

Wednesday, August 8, 2012

Kinase Inhibitor Trials Show Melanoma Benefits | News | Drug Discovery and Development Magazine

Findings from GlaxoSmithKline (GSK) plc’s Phase 3 clinical study program evaluating single agent therapy with the targeted anti-cancer agents, dabrafenib (below left structure) and trametinib (below right structure), in patients with BRAF V600 mutation positive metastatic melanoma have been released. 
Both the BREAK3 study of dabrafenib (BRAF inhibitor) and the METRIC study of trametinib (MEK inhibitor) demonstrated a statistically significant benefit in the length of time patients with BRAF V600 mutation positive advanced or metastatic melanoma lived without progression of their disease or death (Progression Free Survival or PFS) compared to those receiving chemotherapy. Additionally, patients in the METRIC study who received trametinib lived significantly longer (overall survival or OS) than those who received chemotherapy with dacarbazine. OS data are not yet mature in the BREAK3 trial.

“The results from the clinical studies of dabrafenib and trametinib presented at this meeting represent important progress towards understanding how these investigational agents could benefit patients with advanced and metastatic melanoma. Importantly, trametinib is the first MEK inhibitor to demonstrate clinical benefit in a late phase melanoma trial.” said Dr. Rafael Amado, Head of Oncology R&D for GlaxoSmithKline. “We are planning regulatory submissions for dabrafenib and trametinib as single agent therapies and have recently started a Phase 3 program to further investigate the effect of the combination in this disease.”

Tuesday, August 7, 2012

OGX-427 Improves PFS in Prostate Cancer | News | Drug Discovery and Development Magazine

In continuation of my update on OGX-427 

OncoGenex Pharmaceuticals Inc. announced data from a Phase 2 study of its investigational compound OGX-427 in chemotherapy-naive metastatic castration resistant prostate cancer (mCRPC) patients. Preliminary results show a higher number of patients taking OGX-427 plus prednisone without disease progression at 12 weeks and with declines in prostate-specific antigen (PSA), compared with those taking prednisone alone.

Sixty-four of 72 planned patients have been randomized to the study and data on 42 patients [22 who received OGX-427 plus prednisone and 20 who received prednisone alone] are now available at or beyond the 12 week assessment time point. Highlights are as follows: 

Monday, August 6, 2012

Phase 3 Elagolix Trial Begins | News | Drug Discovery and Development Magazine

Elagolix (see structure) is an oral gonadotropin-releasing hormone (GnRH) antagonist. "Endometriosis can be a debilitating disease that affects millions of women around the world and the exploration of new treatments could offer other options for women with this disease," said Dr. Hugh Taylor, M.D., Chief of Division of Reproductive Endocrinology and Infertility, Yale School of Medicine.

The Phase 3 trial (M12-665) is a 24-week, multinational, randomized, double-blind, placebo-controlled study designed to evaluate the safety and efficacy of elagolix in 875 women, age 18 to 49, with moderate-to-severe endometriosis-associated pain. It will be conducted at approximately 160 sites in the United States, Puerto Rico and Canada.
"The investigation of elagolix for endometriosis is an important step in the exploration of potential treatments for this underserved patient population," said Rita Jain, M.D., divisional vice president, Pain, Respiratory and Metabolic Development, Global Pharmaceutical R&D, Abbott.

The trial has begun screening for enrollment. A second Phase 3 study is planned with an NDA filing targeted in 2016.

Phase 3 Elagolix Trial Begins | News | Drug Discovery and Development Magazine

Sunday, August 5, 2012

Nicotinamide riboside can protect against obesity

A natural ingredient found in milk can protect against obesity even as mice continue to enjoy diets that are high in fat. 

The researchers identified this ingredient, known as nicotinamide riboside (see structure), as they were searching for alternative ways to boost the well-known gene SIRT1, which comes with benefits for both metabolism and longevity. One way to do that is to target SIRT1 directly, as the red wine ingredient resveratrol appears to do, at least at some doses.

Auwerx's team lead by Johan Auwerx, suspected there might be a simpler way to go about it, by boosting levels of one of SIRT1's molecular sidekicks, the cofactor NAD+. 

This milk ingredient does just that in a rather appealing way. Not only is it a natural product, but it also gets trapped within cells, where it can do its magic.

Mice that take nicotinamide riboside in fairly high doses along with their high-fat meals burn more fat and are protected from obesity. They also become better runners thanks to muscles that have greater endurance.

Saturday, August 4, 2012

BioLineRx receives two U.S. patent allowances for BL-1021 to treat neuropathic pain

BioLineRx, a biopharmaceutical development company, announced today that two Notices of Allowance have been issued by the United States Patent and Trademark Office (USPTO) for BL-1021 (see structure), an orally available small molecule for treating neuropathic pain. The first has been issued for a patent application claiming BL-1021's composition, that when issued, will be valid until at least September 2022. Additional patents claiming BL-1021's composition are granted or pending in Europe, Japan, Canada, Korea, Mexico, Israel, India, China and Australia. The other Notice of Allowance is for a patent application claiming the use of BL-1021 for the treatment of pain, that when issued, will be valid until at least January 2028.

BioLineRx receives two U.S. patent allowances for BL-1021 to treat neuropathic pain: BioLineRx, a biopharmaceutical development company, announced today that two Notices of Allowance have been issued by the United States Patent and Trademark Office (USPTO) for BL-1021, an orally available small molecule for treating neuropathic pain.

Friday, August 3, 2012

Novel way to treat drug-resistant brain tumor cells

In continuation of my update on Lapatinib
Research by Dr. Paul Clark, a scientist in Kuo's lab and the study's lead author, shows why. When cetuximab treatment switches off EGFR activity and should inhibit cancer-cell growth, cancer stem cells compensate by turning on two other EGFR family receptors (ERBB2 and ERBB3) and continue to grow. One of these receptors, ERBB2, is implicated in certain types of chemotherapy-resistant breast cancer. Fortunately, another novel drug already approved by the FDA, lapatinib (see the structure), inhibits ERBB2 activity and signaling by multiple EGFR members.
This study shows that cancer stem-cell growth was markedly inhibited by lapatinib treatment, which results in combined knockout of multiple EGFR family members.
"This is good news, because these drugs target an important mechanism for the (GBM) cancer cells to grow so quickly and evade current therapies, and these molecularly targeted drugs are also well-tolerated by patients and have minimal side effects," Dr. Clark said.

Novel way to treat drug-resistant brain tumor cells: New research explains why the incurable brain cancer, glioblastoma multiforme (GBM), is highly resistant to current chemotherapies.

Thursday, August 2, 2012

Increased fiber intake associated with lower risk of dying over twelve year period - Life Extension Update

Fiber could promote health via several mechanisms, including helping to control weight, improving glycemic control, and aiding in the maintenance of a favorable intestinal environment. Fiber may help protect against circulatory diseases by lowering low density lipoprotein (LDL) cholesterol, which, when elevated, is a major risk factor for cardiovascular disease. Fiber intake has also been associated with a reduction in inflammatory markers including C-reactive protein, interleukin-6 and tumor necrosis factor-alpha. The authors note that greater total fiber intake could be a marker of an overall dietary pattern that benefits health.

"We observed inverse associations between total dietary fiber intake and mortality, and specifically mortality from circulatory, digestive, and non-cardiovascular disease, noncancer inflammatory diseases," the authors conclude. "These results show that high fiber intake, mainly from cereals and vegetables, may reduce the risk of death from these diseases."