Med-Chemist : "Quintessential Medicinal Chemistry"
Monday, February 18, 2013
Breakthrough in ovarian cancer: Selumetinib
In continuation of my update on Seumetinab
Ref : http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(12)70572-7/fulltext
Breakthrough in ovarian cancer: Selumetinib
We know that, Selumetinib (AZD6244) is a drug being investigated for the treatment of various types of cancer, for example non-small cell lung cancer (NSCLC).
Mode of action : The gene BRAF is part of the MAPK/ERK pathway, a chain of proteins in cells that communicates input from growth factors. Activating mutations in the BRAF gene, primarily V600E (meaning that the amino acid valine in position 600 is replaced by glutamic acid), are associated with lower survival rates in patients with papillary thyroid cancer. Another type of mutation that leads to undue activation of this pathway occurs in the gene KRAS and is found in NSCLC. A possibility of reducing the activity of the MAPK/ERK pathway is to block the enzyme MAPK kinase (MEK), immediately downstream of BRAF, with the drug selumetinib. More specifically, selumetinib blocks the subtypes MEK1 and MEK2 of this enzyme....
The study was initially developed in 2007, with 52 patients enrolled for the Phase II clinical trial between December 2007 and November 2009. Patients were given 50 milligrams of selumetinib orally twice daily. Of those participants, eight had a measurable decrease in tumor size, seven had partial responses and 34 patients saw their tumors stabilize. The findings suggest that inhibitors of the MAPK pathway warrant further investigation in patients with low-grade ovarian cancer.
"There just aren't very good treatments for low-grade ovarian cancer, so this discovery opens up a lot of new exciting possibilities for us," Dr. Farley said. He added that Phase III of this trial is scheduled to begin in the next few weeks, with that trial to be the "definitive test" before the treatment becomes available to the general population.
Breakthrough in ovarian cancer: Selumetinib
Sunday, February 17, 2013
Saturday, February 16, 2013
FDA Approves Pomalyst for Advanced Multiple Myeloma
We know that, Pomalidomide (INN, originally CC-4047 or 3-amino-thalidomide, marketed as Pomalyst by Celgene), is a derivative of thalidomide that is anti-angiogenic and also acts as an immunomodulator. Pomalidomide was approved on February 8, 2013 by the U.S. Food and Drug Administration (FDA) as a treatment for relapsed and refractory multiple myeloma....
Friday, February 15, 2013
FDA Approves Ravicti for the Chronic Management of Some Urea Cycle Disorders
The U.S. Food and Drug Administration today approved Ravicti (glycerol phenylbutyrate) for the chronic management of some urea cycle disorders (UCDs) in patients ages 2 years and older.
UCDs are genetic disorders that involve deficiencies of specific enzymes involved in the urea cycle, a series of biochemical steps normally required to remove ammonia from the blood. When protein is absorbed and broken down by the body, it produces nitrogen as a waste product. The urea cycle removes nitrogen from the blood and converts it to urea, which is removed from the body through urine. In people with UCDs, nitrogen accumulates and remains in the body as ammonia, which can travel to the brain and cause brain damage, coma or death.
Thursday, February 14, 2013
Wednesday, February 13, 2013
Top-line results from Vanda's tasimelteon Phase IIb/III study on major depressive disorder
We know that, Tasimelteon (BMS-214,778) is a drug which is under development for the treatment of insomnia and other sleep disorders. It is a selective agonist for the melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, similar to older drugs such as ramelteon. It has been through Phase III trials successfully and was shown to improve both onset and maintenance of sleep, with few side effects.
A year-long (2011-2012) study at Harvard is testing the use of tasimelteon in blind subjects with non-24-hour sleep-wake disorder.
Now Vanda Pharmaceuticals Inc. (NASDAQ: VNDA), announced top-line results of the Phase IIb/III clinical study (MAGELLAN) in Major Depressive Disorder (MDD), investigating the efficacy and safety of tasimelteon as a monotherapy in the treatment of patients with MDD. The clinical study did not meet the primary endpoint of change from baseline in the Hamilton Depression Scale (HAMD-17) after 8 weeks of treatment as compared to placebo. Both tasimelteon and placebo treated patients had an approximately 40% reduction of their MDD symptoms from baseline. Tasimelteon was shown to be safe and well-tolerated, consistent with observations in prior studies. Given these current proof of concept clinical study results, Vanda has decided to discontinue all activities in this indication.
Vanda has recently reported positive results in two phase III clinical studies of tasimelteon in Non-24-Hour Disorder (Non-24) and plans to submit a New Drug Application to the U.S. Food and Drug Administration in mid-2013......
"These results are disappointing, as there is still a significant unmet medical need for patients with Major Depression," said Mihael H. Polymeropoulos , M.D., President and CEO of Vanda. "Tasimelteon's application in the treatment of blind individuals with Non-24 remains our top priority as we pursue our planned NDA submission this year."
Vanda has recently reported positive results in two phase III clinical studies of tasimelteon in Non-24-Hour Disorder (Non-24) and plans to submit a New Drug Application to the U.S. Food and Drug Administration in mid-2013......
Tuesday, February 12, 2013
Hops, Key to Flavor in Beer, May Prove Useful in New Drugs - Drugs.com MedNews
We know that, Humulone (α-lupulic acid) is a bitter-tasting chemical compound found in the resin of mature hops (Humulus lupulus). Humulone is a prevalent member of the class of compounds known as alpha acids, which collectively give beer its characteristic bitter flavor.
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In a new study, researchers determined the precise configuration of humulones, substances derived from hops that give beer its unique flavor.
"Now that we have the right results, what happens to the bitter hops in the beer-brewing process makes a lot more sense," study lead author Werner Kaminsky, a University of Washingto.
Previous research has suggested that moderate consumption of beer and therefore its bitter compounds might have positive effects on diseases such as diabetes and some types of cancer, as well as aiding weight loss and decreasing inflammation.
The new findings could help scientists determine which humulones might prove useful in efforts to develop new drugs, Kaminsky said.
The authors wrote in their report that while "excessive beer consumption cannot be recommended to propagate good health isolated humulones and their derivatives can be prescribed with documented health benefits."
Ref : http://onlinelibrary.wiley.com/doi/10.1002/anie.201208450/abstract
Ref : http://onlinelibrary.wiley.com/doi/10.1002/anie.201208450/abstract
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