|
- Globally, this will be the first TRPV3 molecule to enter clinical trials
- It will be Glenmark’s seventh molecule in clinical trials
- GRC 15300 filed for Phase I trials with MHRA, UK
Mumbai, India | January 23 2009 | Glenmark Pharmaceuticals Ltd. (GPL) today announced that its candidate for Osteoarthritic pain, Neuropathic pain, and other Inflammatory pain conditions – GRC 15300 has been filed for Phase I trials. The company intends to develop GRC 15300, a Transient Receptor Potential Vanilloid (TRPV)3 Antagonist in neuropathic pain as the primary indication. The molecule has been filed for Phase 1 approval with MHRA(Medicines and Healthcare Products Regulatory Agency), United Kingdom. Glenmark expects to complete Phase I trials for GRC 15300 and initiate Phase II before the end of CY 2009.
GRC 15300 will be the first TRPV3 molecule to enter clinics globally. With this molecule being filed for phase I trials, Glenmark has demonstrated its strengths in the TRP area and will have one of the most in-depth research programs in TRP channels globally. The highlight for this research program is that the TRPV3 target acts in a different temperature range devoid of hyperthermia issues, contrary to some of the TRPV1 antagonists, currently in development. GRC 15300 is highly efficacious as compared to current Gold standard molecules (Pregabalin, Gabapentin), as seen in animal models. Another positive for this molecule is that it is nonhabit forming and presents a better option for chronic pain therapy.
Speaking on this development, Mr. Glenn Saldanha, MD & CEO, Glenmark Pharmaceuticals Ltd. said, “We are extremely glad to take GRC 15300 forward into Phase I trials. This is a significant development for our organization as this molecule will be the first TRPV3 antagonist globally to be filed for Phase I trials making it a potential first-in-class. This development is a reaffirmation of Glenmark’s research capabilities and focused approach towards drug discovery and our commitment towards setting new benchmarks in speed, efficiency and continuous progress in the drug discovery space.”
About GRC 15300 :
GRC 15300 carries a first-in-class potential with a target launch date of 2015. It is a novel, potent and selective human transient receptor potential vanilloid (TRPV-3) receptor antagonist, has completed the battery of pre-clinical studies and has demonstrated favorable results, a good safety margin and also exhibited superior efficacy in in-vivo models of neuropathic & inflammatory pain. The phase-I study will be conducted in a highly experienced Clinical Pharmacology Research unit in the UK. This is a randomized, double blind, placebo controlled study. The safety and pharmacokinetics of six single ascending doses and three multiple ascending doses of GRC 15300 will be evaluated in this study. Furthermore, this Phase I study is designed to provide an early indication of proof of mechanism in healthy volunteers.
About TRPV3 :
There has been significant scientific interest and commercial attention devoted to the vanilloid receptors as potential pain targets. Several companies have active programs in the TRPV3 space including Pfizer which entered into a collaboration agreement with Hydra Biosciences in 2007 that included potential milestone payment of upto USD 195 million for the first developed product launched, with upside potential for additional approved indications. However so far, no TRPV3 compounds have reported entry into clinical trials. The Transient Receptor Potential Vanilloid 3 (TRPV3), is a thermosensitive, voltagedependant ligand-gated cation channel. Its tissue expression varies across species. In humans, it is expressed in the superior cervical and trigeminal ganglia and is also expressed in the brain, spinal cord, keratinocytes, tongue and dorsal root ganglion (DRG) of sensory neurons. Across species, TRPV3 subunits are also co-expressed with TRPV1 where they form heteromultimeric structures by interacting with TRPV1 monomers.
TRPV3 receptor mainly acts as a warmth sensor and responds to warm temperatures (33 – 39°C). It is strongly sensitized by various repeated stimuli such as heat, camphor, 2 – aminoethyl diphenylborate (2-APB), carvacrol, thymol and eugenol indicating a potential role in nociception. TRPV3 receptor antagonists are also implicated in the treatment of myasthenic syndrome, NIDDM, breast cancer, and there is limited data available suggesting its putative roles in the neurophysiology of pruritis. Thus, TRPV3 receptor antagonists may be of potential therapeutic benefit in inflammatory and neuropathic pain conditions and a variety of other indications mentioned above with combined market size in excess of 10 Billion worldwide in 2007.
The addressable market: There is a large un-met medical need and the recent concerns around the safety of cox-2 inhibitors should propel sales of safer products. The neuropathic pain market is estimated at around USD 5 billion with over 40 million patients worldwide while the Osteoarthritis market is valued at over USD 5 billion with over 200 million patients worldwide. It is estimated that 9.6% of men and 18.0% of women aged over 60 years have symptomatic osteoarthritis(WHO Report)
About Glenmark Pharmaceuticals Ltd:
Glenmark Pharmaceuticals Ltd. (GPL) is a research-driven, global, integrated pharmaceutical company headquartered at Mumbai, India. Its shares are listed on India’s two large stock exchanges, the Bombay Stock Exchange (BSE) and the National Stock Exchange (NSE). It employs over 5000 people across its global operations over 85 countries. The Company is a leader in India in the discovery of new molecules and is focused in the areas of inflammation [Asthma/COPD, etc.], dermatology and metabolic disorders [Diabetes, Obesity, etc.]. The Company is in the process of creating marketing front-ends for the launch of its proprietary products in the future. GRC 6211, a TRPV1 Antagonist in Phase II clinical trials has been outlicensed to Eli Lilly & company. Glenmark’s Asthma/COPD molecule, Oglemilast [GRC 3886], was licensed out to Forest Laboratories and Teijin Pharma Limited for the North American and Japanese markets, respectively, in two landmark deals. Oglemilast is presently undergoing Phase II clinical trials in the US. Glenmark’s API and generics business interests span over the highly regulated markets of USA, Latin America and Europe, and are managed by its subsidiary Glenmark Generics Limited. For more information on GPL, log on to www.glenmarkpharma.com
SOURCE: Glenmark Pharmaceuticals Ltd |
