Glenmark’s molecule for neuropathic pain, osteoarthritis - GRC 10693, successfully completes Phase I trials

GRC 10693 is a selective cannabinoid-2 [CB-2] receptor agonist and has first-in-class potential

Mumbai, India | April 13, 2009 | Glenmark Pharmaceuticals Ltd. (GPL) today announced that its candidate for neuropathic pain, osteoarthritis and other inflammatory pain disorders – GRC 10693 has successfully completed Phase I trials in Europe.

 

The Phase I study was conducted on 80 healthy human subjects using escalating single and multiple oral doses with the objective of assessing safety, tolerability and pharmacokinetics of GRC 10693. The highest single dose achieved in the study was 1200 mg. The study demonstrated that GRC 10693 was well tolerated by the subjects at all dose levels and was found to have a dose proportional pharmacokinetic profile with good exposure levels. There were no serious or significant adverse events, including no significant cardiovascular effects or QT prolongation seen in either the single dose or the multiple dose cohorts. The latter cohort received 300mg of GRC 10693 once daily for 14 days and achieved exposure levels equivalent to those in the highest tested single dose.

 

In the Phase 1 studies, high exposure levels of the drug were reached, which exceeded by several folds the levels required for efficacy in various in vivo acute and chronic pain models in animals. In addition, several well validated pain models included in the study for confirmation of Proof of Mechanism in the multiple dose phase, demonstrated significant improvements in various pain scores at both 2 and 13 days, the key efficacy timepoints defined in the protocol. This combination of a very good safety profile and pharmacokinetics, combined with good Proof of Mechanism results, marks a very promising start to the clinical development of GRC 10693.

Initially, the company intends to develop GRC 10693 in neuropathic pain as the primary indication, with Phase IIb trials planned to be initiated later this year. 2 of 3 GRC 10693 is the only selective cannabinoid-2 [CB-2] receptor agonist currently reported in clinical development following oral route of administration and has first-in-class potential. GRC 10693 has >4700-fold functional selectivity for CB2 over CB1 making it one of the most selective CB2 agonist reported in development.

Speaking on this development, Mr. Glenn Saldanha, MD & CEO, Glenmark Pharmaceuticals Ltd. (GPL) said, “This is a significant achievement for our organization as GRC10693 will be our fourth molecule which will enter Phase II trials. He further added “We are very excited with the results from the Phase 1 studies of GRC 10693. It offers a novel treatment approach to pain and has attracted a lot of scientific and commercial interest. By being successful in an area where very few molecules have passed to the clinical development stage, it also reinforces Glenmark’s capability in advancing drugs with first-in-class potential.”

Dr. John Efthimiou, President Clinical R&D & CMO of Glenmark was delighted at this development and explained that “The design of this Phase 1 study allowed us to establish a very good therapeutic window by evaluating not just the pharmacokinetics and safety, but also by obtaining an early read on the Proof of Mechanism. For a novel target, this data validates the approach and opens the path for us to expedite subsequent development with substantial confidence.”

Note on the Molecule: GRC 10693 is potentially a first-in-class molecule, with block buster potential and is likely to be an early launcher in this class of compounds with a target launch date of 2014. The molecule is a novel, potent and selective human cannabinoid (CB-2) receptor agonist, with over 4700-fold selectivity over the CB-1 receptor and good bioavailability across species tested. The molecule 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 and inflammatory pain.

 

Note on 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 4 billion with over 200 million patients. 3 of 3

About Glenmark Pharmaceuticals Ltd:

Glenmark Pharmaceuticals Ltd. (GPL) is a research-driven, global, integrated pharmaceutical company headquartered at Mumbai, India. The company is listed on India’s two premier stock exchanges, the Bombay Stock Exchange (BSE) and the National Stock Exchange (NSE). It employs over 5500 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.], 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. Glenmark’s first 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. GRC 6211 has been out-licensed to Eli Lilly & company. For more information on GPL, log on to http://www.glenmarkpharma.com/

SOURCE: Glenmark
 

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