Sunday, April 24, 2011
A natural product inspired/derived first in class oral drug fingolimod (Gilenya) was approved by FDA for treating multiple sclerosis. This drug pocess novel mechanism of action compared to other drugs with immuno modulation. It is a structural analogue of myriocin, a sphingosine metabolite isolated from the fungus Isaria sinclairii. Fingolimod get phosphorylated with sphingosine kinases mainly sphingosine kinase-2 and binds to extra cellular G-protein coupled receptors mainly sphingosine-1-phosphate receptor S1PR1. It then prevents sequester lymphocytes in lymph node and preventing them from moving into central nervous system and stops the damage. A complete story was published on fingolimod in a recent Journal of Natural Products article
Sunday, January 31, 2010
In October 2009, US FDA approved a new therapy for renal cell carcinoma. This was highlighted in Nature Reviews: Drug Discovery January, 2010 issue. Complete priscription information given on FDA web site.
Wednesday, December 2, 2009
Nice video town hall discussion about future cancer research, little old one but good one on Future Cancer Research. Genentech focusing on anti-body conjugates for targeted specific delivery and pro apoptotic agents are undergoing clinical trails. In addition, Hedgehog signaling pathway also targeted to find cure for skin cancers.
Wednesday, August 12, 2009
In western diets prepared using vegetable and animal oils, a plenty available common fatty acids (palmitic/stearic acid) also have good tendency to bind like LPS on Toll-Like Receptor-4 (TLR-4) in humans, this produces similar inflammatory response by cytokine release and activation of NF-kb and JNK1 pathways. Once JNK1 activates, it phosphorylates Insulin Substrate Receptor-1 (IRS-1), which interfere with insulin signaling. Continuation of this Free Fatty Acids (FFAs) activation leads to human whole body inflammation (obesity), insulin resistance/type 2-diabetes and organ failures.
Thursday, July 9, 2009
Saturday, June 20, 2009
The concept of selective inhibitors (Magic Bullets) one drug-one disease is no more an ideal in drug discovery. Knocking down one protein target is not enough to treat complex diseases like cancer. If we knock down multiple targets in a biological pathway of a disease with Designed Multiple Ligands (DMLs), we may expect improved efficacy. The trend in recent developments in anticancer drug discovery shifting towards a multi-target approach. One good example is recent wave of FDA approvals, "lapatinib" a dual EGFR and Her-2/neu kinase inhibitor. The other one “dasatanib” a multi kinase inhibitor and many more.