The said clinical trial has been approved by the U.K.’s Medicines and Healthcare Products Regulatory Agency (MHRA).
Glenmark Pharmaceuticals plans on developing GRC 4039 (a PDE 4 inhibitor) in rheumatoid arthritis – its primary indication. Completion of the Phase 1 trials is expected by Glenmark by October 2008, while the initiation of Phase II by January 2009.
GRC 4039, a selective PDE4 inhibitor is intended for rheumatoid arthritis [RA] and inflammatory disorders. After the withdrawal/setback of COX-2 Inhibitors and the void that exists in RA therapy for orally available potent small molecules, this is a potential block-buster opportunity in the global market.
According to Mr. Glenn Saldanha, MD & CEO, Glenmark Pharmaceuticals Ltd.:
“We are happy to take GRC 4039 forward into Phase I trials. This is Glenmark’s fourth molecule to enter the clinics from our pipeline of eight NCEs and NBEs, and demonstrates our steady progress in the drug discovery space.
RA has been selected as the primary indication for its commercial attractiveness, the unmet medical need for potent and convenient oral therapies and the sound biological rationale for PDE-4 inhibitor–based treatment in RA.”
During pre-clinical testing, GRC 4039 demonstrated over 3700 fold selectivity to PDE4, indicating the potential for a once-daily regimen.
Additionally, there was no emesis in the pre-clinical models. The molecule demonstrated favourable results in early toxicology studies, a good safety margin and also exhibited good efficacy in in-vivo RA and TNF- α inhibition models.
PDE4 (phosphodiesterase) inhibitor is a drug that can block the major cAMP-metabolizing enzyme found in inflammatory and immune cells — thus have the potential as anti-inflammatory drugs that can fight against an inflammatory condition such as rheumatoid arthritis.
Find more details from the Glenmark Pharma PR (a pdf file).