I knew about Naproxen, because my first job was with Rallis India Limited and the pharma division (sold to Shreya Group) was selling it as a gel. It works by inhibiting both the COX-1 and COX-2 enzymes and that is the reason, why it has side effects. It has been established already that the selective inhibitors of COX-2 & 5 -LO will be the best drugs with least or no ulcerogenecity. We have some drug like Celecoxib with selective inhibition of COX-2 (cyclo oxygenase enzyme), still we need to have selective inhibitors of both COX-2 & 5 -LO, so that there will not be any cases like Rofecoxib withdrawal.
Naproxcinod, is a nitroxybutyl ester of naproxen. The ester group allow it to also act as a nitric oxide donor. Interestingly, this second mechanism of action makes naproxcinod the first of a new class of drugs, the cyclooxygenase inhibiting nitric oxide donators (CINODs), that are expected to produce similar analgesic efficacy to traditional NSAIDs, but with less gastrointestinal and cardiovascular side effects. Now NicOx S.A announced that European Medicines Agency (EMEA) has validated the Marketing Authorization Application (MAA) for naproxcinod. NicOx is seeking approval for an indication for the relief of the signs and symptoms of primary osteoarthritis. This follows the acceptance for filing of a New Drug Application (NDA) by the US Food and Drug Administration (FDA) in November 2009.
More interestingly, in addition to naproxcinod, NicOx's pipeline includes several nitric oxide- donating NCEs, which are in development internally and with partners, including Merck & Co., Inc., for the treatment of widespread eye diseases, cardiometabolic diseases, hypertension and dermatological disease.
Details of the press release, one can read at the link....
2 comments:
As we know most of the NSAIDs (COX-1 inhibitors) have ulcerogenic effect and those specific to COX-2 are less ulcerogenic but still has cardiovascular effects..for instance rofecoxib.
It's good to hear that naproxcinod has a potential to avoid both side effects in some extent.
thanks for the information.
Hi Med chem,
In my opinion compounds with selective inhibition of 5-LO (lipo oxygynase) and COX-2 (cyclo oxygenase) will be the best ones, as nonulcerogenic NSAIDs and with least or no cardiovascular effects. (importance of 5-LO inhibition !)....
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