Glenmark Announces the Discovery of a Novel Chemical Entity ‘GRC 17536′, a TRPA1 Receptor Antagonist, a Potential First-in-Class Molecule Globally

August 31, 2010

MUMBAI, India, August 31, 2010 /PRNewswire-FirstCall/ –

– With This Announcement, Glenmark has Clearly Reaffirmed its Position
Globally as the Leader in the TRP Space

Glenmark Pharmaceuticals today 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 1 enabling GLP studies. Preclinical studies have been
completed and Glenmark plans to file the Phase 1 application in January 2011.
This is another potential first-in-class molecule globally for Glenmark

Commenting on this discovery, Glenn Saldanha, CEO & MD, Glenmark
Pharmaceuticals ltd mentioned ” Both our earlier TRP molecules i.e. TRPV1 and
TRPV3 resulted in outlicensing 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

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 has proven 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.

About Glenmark Pharmaceuticals Ltd

Glenmark Pharmaceuticals Ltd. (GPL) is a research-driven, global,
integrated pharmaceutical company headquartered at Mumbai, India. It is a
leading player in the discovery of new molecules both NCEs (new chemical
entity) and NBEs (new biological entity). The company has a significant
presence in branded generics markets across emerging economies including

    For further information, please contact:
    Jason D'Souza
    Glenmark, Mumbai, India
    Tel: +91-22-40189919
    Email: media@glenmarkpharma.com

SOURCE Glenmark Pharmaceuticals Ltd.

Source: newswire

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