Bangalore, Sep 1, 2010: Glenmark Pharmaceuticals, an Indian pharma player in the discovery of new molecules has announced the discovery of a Novel Chemical Entity(NCE) 'GRC 17536'. The new NCE program is targeting TRPA1 receptor antagonists for pain and respiratory disorders. TRPA1 belongs to Transient Receptor Potential (TRP) family of ion channels, which have generated a lot of interest as pain targets due to their distinguishing role in peripheral and/or central pain signal transmission.

Glenmark has selected a lead molecule named GRC 17536, which is currently finishing up phase I enabling GLP studies. Glenmark plans to file the phase I application in January 2011. This is said to be another potential first-in-class molecule globally for Glenmark

Commenting on this discovery, Mr Glenn Saldanha, CEO & MD, Glenmark Pharmaceuticals said, “Both our earlier TRP molecules i.e. TRPV1 and TRPV3 resulted in out-licensing deals for the company. GRC 17536 which is a TRPA1 receptor antagonist is another potential first-in-class globally and we are encouraged by the results shown by the molecule in animal studies. GRC 17536 is highly selective even when compared with other TRPs and can be administered orally"

Glenmark is now positioned as one of the leading companies engaged in the discovery of novel TRP antagonists. Previously Glenmark has worked on TRPV1 and TRPV3 receptors and was able to successfully bring programs into clinical development. Both of these programs also resulted in out-licensing deals for Glenmark.

GRC 17536, which is Glenmark's lead, is a highly potent (< 10nM) TRPA1 antagonist, which is highly selective (> 1000 fold over other TRPs) and orally available. It is said to be highly efficacious in treating inflammatory and neuropathic pain in animal models compared to gold standard drugs. It reversed hyperalgesia in vivo models of Freund's complete adjuvant - induced inflammatory and chronic constriction injury (CCI) - induced neuropathic pain with an EC50 of less than 10 mg/kg. In addition, when tested in an in vivo model of asthma, it showed promising effect on airway inflammation, bronchoconstriction and cough. So far, the compound has showed good safety in the safety pharmacology and toxicology studies performed till date.