Mavatrep

Mavatrep
Clinical data
Other names	JNJ-39439335
Identifiers
	IUPAC name 2-[2-[2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol;
CAS Number	956274-94-5;
PubChem CID	17751090;
DrugBank	DB12875;
ChemSpider	29271895;
UNII	F197218T99;
ChEMBL	ChEMBL2364618;
CompTox Dashboard (EPA)	DTXSID90241905 ;
Chemical and physical data
Formula	C25H21F3N2O
Molar mass	422.451 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)(C1=CC=CC=C1C2=CC3=C(C=C2)N=C(N3)/C=C/C4=CC=C(C=C4)C(F)(F)F)O;
	InChI InChI=1S/C25H21F3N2O/c1-24(2,31)20-6-4-3-5-19(20)17-10-13-21-22(15-17)30-23(29-21)14-9-16-7-11-18(12-8-16)25(26,27)28/h3-15,31H,1-2H3,(H,29,30)/b14-9+; Key:ORDHXXHTBUZRCN-NTEUORMPSA-N;

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 non-renally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.^[2]

References

^ ^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.
^ ^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.

[:0-1] 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] 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.

[1]

[2]

Pharmacokinetics

See also

References