Summary
- Merck TRPV1 Antagonists MK-2295: Results of clinical studies and reasons why it will not make it to market
- MK-2295 was administered to normal individuals for 14 days. The investigator tested for heat sensitivity by applying a heat probe to the skin or the subjects having taken MK-2295 or placebo. They also immersed their hands in hot water (48 degree C) or asked them to drink hot water. The results were impressive with the subjects taking MK-2295 displaying a raised threshold to heat. The problem is that often they did do not find unpleasant temperatures around 48 degree C.
Analysis
- Because of the risk of accidental heat injuries, Merck will not further trial this compound for osteoarthritis (OA) or other clinical applications for which it would be administered systemically.
- Of note the increase in core temperature described with TRPV1 agonists did occur but lasted only 2 days, therefore this is not as much a problem.
- Most likely, all the other pharma developing TRPV1 antagonists observed the same effects, and will not further push these compounds to clinical trial.
- Merck still might develop MK-2295 for topical applications.
Analyses are solely the work of the authors and have not been edited or endorsed by GLG.