Mavatrep
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| Other names | JNJ-39439335 |
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| Formula | C25H21F3N2O |
| Molar mass | 422.451 g·mol−1 |
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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
[edit]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 non-renally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.[2]
See also
[edit]References
[edit]- 1 2 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.
- 1 2 3 4 5 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.