Med-Chemist : "Quintessential Medicinal Chemistry"
Tuesday, September 11, 2012
Enoxaparin prevents PVT in advanced cirrhosis
In continuation of my update on Enoxaparin
Enoxaparin (see structure) significantly reduces portal vein thrombosis (PVT) and increases overall survival in patients with advanced cirrhosis, the results of an Italian study show. The authors also found additional benefits beyond the drug's established effect on PVT.
The study included 70 cirrhosis patients with a Child-Pugh score of 7-10, aged 18-75 years who received enoxaparin 4000 IU/day for 48 weeks or no treatment. Patients were followed up for a mean of 58 weeks in the control group and 89 weeks in the enoxaparin group, with ultrasound evaluation of the portal vein system every 3 months.
As reported by the authors, patients receiving enoxaparin were 90% less likely to experience PVT than those who did not. Overall, 8.8% of enoxaparin-treated patients developed PVT compared with 27.7% in the control group, and no cases developed in the enoxaparin group within the first 2 years.
While decompensation occurred at an equal rate in both groups during the follow-up period, significantly fewer patients experienced progression during active treatment (11.7 vs 59.4%).
Enoxaparin prevents PVT in advanced cirrhosis
Monday, September 10, 2012
FDA Approves Myrbetriq...
“Myrbetriq (see below structure) is the first oral OAB treatment with a distinct mechanism of action since the launch of anticholinergic agents 30 years ago,” said Steven Ryder, MD, president, Astellas Pharma Global Development. “The approval of Myrbetriq represents an important milestone in OAB treatment and in our ongoing commitment to advancing urological health.”....
FDA_Approval_Press_Release_FINAL 6.28.12.pdf (application/pdf Object)
Sunday, September 9, 2012
Lexicon announces results from two initial trials of LX4211 for type 2 diabetes
Thirty-six patients with type 2 diabetes mellitus (T2DM) were randomized 1:1:1 to receive a once-daily oral dose of placebo or 150 or 300 mg of the dual SGLT1/SGLT2 inhibitor LX4211 for 28 days. Relative to placebo, LX4211 (see structure) enhanced urinary glucose excretion by
inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA1c; and significantly lowered serum triglycerides. LX4211 also mediated trends for lower weight, lower blood pressure, and higher glucagon-like peptide-1 levels. In a follow-up single-dose study in 12 patients with T2DM, LX4211 (300 mg) significantly increased glucagon-like peptide-1 and peptide YY levels relative to pretreatment values, probably by delaying SGLT1-mediated intestinal glucose absorption. In both studies, LX4211 was well tolerated without evidence of increased gastrointestinal side effects. These data support further study of LX4211-mediated dual SGLT1/SGLT2 inhibition as a novel mechanism of action in the treatment of T2DM.
Lxicon announces results from two initial trials of LX4211 for type 2 diabetes: Lexicon Pharmaceuticals, Inc. announced today the publication of results from two initial trials of LX4211 in patients with type 2 diabetes in the online edition of the journal Clinical Pharmacology & Therapeutics.
Saturday, September 8, 2012
Provectus Pharmaceuticals - ASCO 2010
We know that,
Rose Bengal (4,5,6,7-tetrachloro-2',4',5',7'-tetraiodofluorescein) is a stain. Its sodium salt is commonly used in eye drops to stain damaged conjunctival and corneal cells and thereby identify damage to the eye. The stain is also used in the preparation of Foraminifera for microscopic analysis, allowing the distinction between forms that were alive or dead at the time of collection.
A form of Rose Bengal is also being studied as a treatment for certain cancers and skin conditions. The cancer formulation of the drug, known as PV-10, (see the structure) is currently undergoing clinical trials for melanoma and breast cancer. The company also has formulated a drug based on Rose Bengal for the treatment of eczema and psoriasis; this drug, PH-10, is currently in clinical trials as well.
Top-line final data from Provectus’ PV-10 phase 2 trial on metastatic melanoma
Friday, September 7, 2012
Thursday, September 6, 2012
Xalkori Helps Lung Cancer Patients | News | Drug Discovery and Development Magazine
In continuation of my update Crizotinib/Xalkori
Pfizer Inc. said its lung cancer drug Xalkori helped lung cancer patients who had previously been treated for the disease.
Pfizer said Xalkori (see the structre) worked better than two older cancer drugs in the late-stage clinical trial. All patients had a rare type of non-small cell lung cancer and had previously been treated. The Food and Drug Administration approved Xalkori in August for use in patients whose cancer had not been treated.
In the study, patients took Xalkori, Alimta, or Taxotere. Pfizer said patients who took Xalkori had greater progression-free survival, or time from the start of treatment until they died or experienced disease progression. Xalkori is a pill taken twice per day while Alimta and Taxotere are given intravenously.
Xalkori is approved for use against non-small cell lung cancer in patients who have an abnormal gene that causes tumor growth. Xalkori blocks that gene, which is found in 1 percent to 7 percent of non-small cell lung cancer. About 85 percent of lung cancers are the non-small cell variety...
Pfizer said Xalkori (see the structre) worked better than two older cancer drugs in the late-stage clinical trial. All patients had a rare type of non-small cell lung cancer and had previously been treated. The Food and Drug Administration approved Xalkori in August for use in patients whose cancer had not been treated.
In the study, patients took Xalkori, Alimta, or Taxotere. Pfizer said patients who took Xalkori had greater progression-free survival, or time from the start of treatment until they died or experienced disease progression. Xalkori is a pill taken twice per day while Alimta and Taxotere are given intravenously.
Xalkori is approved for use against non-small cell lung cancer in patients who have an abnormal gene that causes tumor growth. Xalkori blocks that gene, which is found in 1 percent to 7 percent of non-small cell lung cancer. About 85 percent of lung cancers are the non-small cell variety...
More...
Anacardic acid can rescue some ALS phenotypes in vitro...
A research group at the Center for iPS Cell Research and Application (CiRA) at Japan's Kyoto University has successfully recapitulated amyotrophic lateral sclerosis (ALS)-associated abnormalities in motor neurons differentiated from induced pluripotent stem cells (iPSCs) obtained from patients with familial ALS, a late-onset, fatal disorder which is also known for Lou Gehrig's disease. In a drug screening assay using the disease model, the team further found that the chemical compound anacardic acid (see structure) can rescue some ALS phenotypes in vitro.
Wednesday, September 5, 2012
Green coffee beans show potential for losing weight..
In a study presented, at the American Chemical Society’s spring national meeting in San Diego, 16 over weight young adults took, by turns, a low dose of green coffee bean extract, a high dose of the supplement, and a placebo. Though the study was small, the results were striking: Subjects lost an average of 17.5 pounds in 22 weeks and reduced their overall body weight by 10.5%.If green coffee extract were a medication seeking approval from the Food and Drug Administration, these results would make it a viable candidate — more than 35% of subjects lost more than 5% of their body weight, and weight loss appeared to be greater while subjects were taking the pills than when they were on the placebo.
Joe Vinson, the University of Scranton chemist who conducted the pilot study, said the findings should pave the way for more rigorous research on coffee bean extract’s effects. A larger trial involving 60 people is being planned.Vinson, whose research focuses on plant polyphenols and their effects on human health, said it appears that green coffee bean extract may work by reducing the absorption of fat and glucose in the gut; it may also reduce insulin levels, which would improve metabolic function. There were no signs of ill effects on any subjects, Vinson reported.
The study used a “cross-over” design, which allowed each subject to serve as his or her own comparison group. For six weeks, volunteers swallowed capsules three times a day, ingesting either 700 or 1,050 milligrams of green coffee extract a day or taking a placebo. After a two-week break, they moved, round-robin style, to another arm of the trial.Subjects did not change their calorie intake over the course of the trial. But the more extract they consumed, the more weight and fat they lost. Altogether, they reduced their body fat by 16%, on average.Of the 16 volunteers, six wound up with a body mass index in the healthful range.One downside is that the extract is “extremely bitter.” It would be difficult to take without a lot of water, Vinson reported.....
Ref : Detailed article read at
Ref : Detailed article read at
I found the following link more informative...
Tuesday, September 4, 2012
‘Orphan drug’ used to treat sleep disorders may be a potent cancer-fighting agent used for many malignancies, study finds
An inexpensive "orphan drug" used to treat sleep disorders appears to be a potent inhibitor of cancer cells, according to a new study led by scientists at Fred Hutchinson Cancer Research Center. Their novel approach, using groundbreaking technology that allows rapid analysis of the genome, has broad implications for the development of safer, more-effective cancer therapies.
A research team led by corresponding author Carla Grandori, M.D., Ph.D., an investigator in the Hutchinson Center's Human Biology Division, used a high-speed robotic technology called high-throughput screening and a powerful genetic technique called siRNA genesilencing to uncover fatal weaknesses in cancer cells driven by an oncogene known as "Myc," which is hyperactive in many cancers, including those of the brain, breast, lung, ovary and liver.
Monday, September 3, 2012
Exelixis reports data from cabozantinib phase 3 trial on MTC
Exelixis, Inc. reported data from the phase 3 pivotal trial of cabozantinib in patients with progressive, unresectable, locally advanced or metastatic medullary thyroid cancer (MTC). The trial, known as EXAM, met its primary endpoint of improving progression-free survival (PFS), with patients in the cabozantinib (see structure) arm achieving a median PFS of 11.2 months compared with 4.0 months for patients in the placebo arm. Overall response rate (ORR), a secondary endpoint, was 28% in the cabozantinib arm and 0% in the placebo arm. Estimated PFS at one year was 47.3% with cabozantinib vs. only 7.2% with placebo. Data for overall survival (OS), another secondary endpoint, are not yet mature. Patients on the cabozantinib arm of the trial received a dose of 140 mg (free base equivalent). Adverse events were generally manageable allowing for treatment with cabozantinib for prolonged periods of time. Exelixis recently submitted a New Drug Application (NDA) for cabozantinib in MTC to the U.S. Food and Drug Administration (FDA).
Exelixis reports data from cabozantinib phase 3 trial on MTC: Exelixis, Inc. reported data from the phase 3 pivotal trial of cabozantinib in patients with progressive, unresectable, locally advanced or metastatic medullary thyroid cancer (MTC).
Sunday, September 2, 2012
Experimental drug tested against multi-drug resistant TB
"Researchers who tested a novel type of antibiotic against multi-drug-resistant tuberculosis [MDR-TB] are reporting that nearly half of patients who got the new drug cleared the bacteria from their lung fluid in two months," according to a study published in the New England Journal of Medicine. Japanese pharmaceutical company Otsuka developed the experimental drug, delamanid (see structure), and "also designed and financed the clinical trial, which took place in 17 medical centers across nine countries."
"'We've invested a lot of time and money to develop this drug, but we are not seeking robust sales growth immediately,' Masuhiro Yoshitake, Otsuka's head of tuberculosis projects, said in an interview," Bloomberg Businessweek reports. "We want to begin selling to people who know how to use the drug," he added, the news service notes. "Doctors must balance the need to fight hard-to-treat cases against prolonging the medicine's potency,"
More : http://www.nejm.org/doi/full/10.1056/NEJMoa1112433
Experimental drug tested against multi-drug resistant TB
Saturday, September 1, 2012
GSK and XenoPort receive FDA approval for Horizant® for postherpetic neuralgia
GlaxoSmithKline plc and XenoPort, Inc. announced today that the United States (US) Food and Drug Administration (FDA) has approved Horizant® (gabapentin enacarbil see structure below) Extended-Release Tablets for the management of postherpetic neuralgia (PHN) in adults.
The efficacy and safety of Horizant for the management of PHN was evaluated in a single 12-week principal efficacy trial, plus two supportive studies that all met their respective primary endpoints. The three clinical studies involved 574 adult patients from the US, Canada and Germany.
The recommended dosage for the management of PHN in adults is 600 mg twice daily. Treatment should be initiated at a dose of 600 mg in the morning for three days followed by 600 mg twice daily (1,200 mg/day) beginning on day four. Doses must be adjusted in patients with impaired renal function. In the 12-week, controlled study in patients with PHN, somnolence and dizziness were the most frequently reported side effects. Somnolence was reported in 10% of patients treated with 1,200 mg of Horizant per day compared with 8% of patients receiving placebo. Dizziness was reported in 17% of patients receiving 1,200 mg of Horizant per day compared with 15% of patients receiving placebo.
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 : http://investors.keryx.com/phoenix.zhtml?c=122201&p=irol-newsArticle&ID=1678920&highlight=
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