Serlopitant

Serlopitant (INN,[1] codenamed VPD-737) is a drug which acts as an NK₁ receptor antagonist. It was assessed in clinical trials for the treatment of urinary incontinence and overactive bladder, but while it was superior to placebo it provided no advantage over existing approved drugs, and was not approved for further development for this indication.[2][3] Serlopitant is now undergoing clinical trials for the treatment of chronic pruritus (itch)[4]

Serlopitant

Clinical data
Routes of administration	By mouth
ATC code	None
Identifiers
IUPAC name 3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one
CAS Number	860642-69-9
PubChem CID	23653789
ChemSpider	24686685
UNII	277V92K32B
KEGG	D09378
ChEMBL	ChEMBL447955
CompTox Dashboard (EPA)	DTXSID701006599
Chemical and physical data
Formula	C29H28F7NO2
Molar mass	555.537 g·mol^−1
3D model (JSmol)	Interactive image
SMILES C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@H]2CC[C@@H]3CN(C[C@H]3[C@@H]2C4=CC=C(C=C4)F)C5=CC(=O)CC5
InChI InChI=1S/C29H28F7NO2/c1-16(19-10-20(28(31,32)33)12-21(11-19)29(34,35)36)39-26-9-4-18-14-37(23-7-8-24(38)13-23)15-25(18)27(26)17-2-5-22(30)6-3-17/h2-3,5-6,10-13,16,18,25-27H,4,7-9,14-15H2,1H3/t16-,18-,25-,26+,27+/m1/s1 Key:FLNYCRJBCNNHRH-OIYLJQICSA-N

See also

• NK₁ receptor antagonist

References

1. "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 62" (PDF). World Health Organization. 2009. pp. 261–2. Retrieved 17 November 2016.
2. Frenkl TL, Zhu H, Reiss T, Seltzer O, Rosenberg E, Green S (August 2010). "A multicenter, double-blind, randomized, placebo controlled trial of a neurokinin-1 receptor antagonist for overactive bladder". The Journal of Urology. 184 (2): 616–22. doi:10.1016/j.juro.2010.03.147. PMID 20639026.
3. Payton S (August 2010). "Urinary incontinence: Neurokinin receptor antagonist inferior to tolterodine for OAB". Nature Reviews. Urology. 7 (8): 418. doi:10.1038/nrurol.2010.105. PMID 20726068. S2CID 33202979.
4. "For Irritating Itch, a Promising Option Under Scrutiny".