Mavatrep

{{Short description|Investigational analgesic drug}}

{{Infobox drug

| drug_name =

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| IUPAC_name = 2-[2-[2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol

| image = Mavatrep.svg

| image_class = skin-invert-image

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| CAS_number = 956274-94-5

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| PubChem = 17751090

| ChemSpiderID = 29271895

| DrugBank = DB12875

| UNII = F197218T99

| KEGG = D10370

| ChEMBL = 2364618

| synonyms = JNJ-39439335

| C=25|H=21|F=3|N=2|O=1

| StdInChI=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+

| StdInChIKey = ORDHXXHTBUZRCN-NTEUORMPSA-N

| 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

}}

Mavatrep (JNJ‐39439335) is a TRPV1 receptor selective competitive antagonist.{{cite journal | vauthors = Manitpisitkul P, Shalayda K, Russell L, Sanga P, Williams Y, Solanki B, Caruso J, Moyer JA | s2cid = 32666782 | display-authors = 6 | title = 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 | journal = Clinical Pharmacology in Drug Development | volume = 7 | issue = 7 | pages = 699–711 | date = September 2018 | pmid = 29125700 | doi = 10.1002/cpdd.412 }} 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.{{cite journal | vauthors = Manitpisitkul P, Shalayda K, Russell L, Sanga P, Solanki B, Caruso J, Iwaki Y, Moyer JA | s2cid = 11755963 | display-authors = 6 | title = 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 | journal = Clinical Pharmacology in Drug Development | volume = 7 | issue = 7 | pages = 712–726 | date = September 2018 | pmid = 29125703 | doi = 10.1002/cpdd.413 }}

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

Pharmacokinetics

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

Mavatrep is largely eliminated non-renally. Mavatrep appears to be metabolized into two primary metabolites which are also eliminated nonrenally.

See also

References