Mavatrep (JNJ‐39439335) is a TRPV1 receptor selective competitive antagonist.[1] It is an investigational analgesic that may be a potential treatment for pain and/or inflammation.

Phase I trials have been completed in healthy Japanese and Caucasian volunteers.[1][2]

Potential common adverse effects include thermohypoesthesia, chills, feeling cold, and feeling hot.[2]

Pharmacokinetics

When administered orally once a day, mavatrep reached steady-state in healthy volunteers in approximately 14 days.[2] It has a relatively long half life between 68 and 101 hours in Japanese subjects and between 82 and 130 hours in Caucasian subjects.[2]

Mavatrep is largely eliminated nonrenally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.[2]

See also

References

  1. ^ a b Manitpisitkul P, Shalayda K, Russell L, Sanga P, Williams Y, Solanki B, et al. (September 2018). "Bioavailability and Pharmacokinetics of TRPV1 Antagonist Mavatrep (JNJ-39439335) Tablet and Capsule Formulations in Healthy Men: Two Open-Label, Crossover, Single-Dose Phase 1 Studies". Clinical Pharmacology in Drug Development. 7 (7): 699–711. doi:10.1002/cpdd.412. PMID 29125700. S2CID 32666782.
  2. ^ a b c d e Manitpisitkul P, Shalayda K, Russell L, Sanga P, Solanki B, Caruso J, et al. (September 2018). "Pharmacokinetics and Safety of Mavatrep (JNJ-39439335), a TRPV1 Antagonist in Healthy Japanese and Caucasian Men: A Double-Blind, Randomized, Placebo-Controlled, Sequential-Group Phase 1 Study". Clinical Pharmacology in Drug Development. 7 (7): 712–726. doi:10.1002/cpdd.413. PMID 29125703. S2CID 11755963.