Description
Mavatrep is an orally bioavailable, potent and selective TRPV1 antagonist with Ki value of 6.5 nM, which exhibits minimal effect on the enzymatic activity of CYP isoforms 3A4, 1A2, and 2D6. It antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM in a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels. It blocks the activation of hTRPV1 channels by Capsaicin and pH in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM respectively. It exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain in vivo. It was selected for clinical development for the treatment of pain. It was developed by Johnson & Johnson and now in clinic phase 1 with no progress