Mavatrep

Description: Mavatrep (formerly known as JNJ-39439335) is a novel, orally bioavailable, potent and selective TRPV1 antagonist with Ki of 6.5 nM. It exhibits minimal effect on the enzymatic activity (IC50 > 25 uM) of CYP isoforms 3A4, 1A2, and 2D6. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca(2+) influx, with an IC50 value of 4.6 nM. In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of its superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain

References: J Med Chem. 2015 May 14; 58(9):3859-74.