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. 

Luc Jasmin, MD, PhD consults with leading institutions through GLG

Luc Jasmin, MD, PhD, Attending Neurosurgeon and a Research Scientist
Luc Jasmin

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Attending Neurosurgeon and a Research Scientist, CEDARS-SINAI MEDICAL CENTER

 
Analyses are solely the work of the authors and have not been edited or endorsed by GLG.