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
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H28F7NO2
Molar mass555.537 g·mol−1
3D model (JSmol)
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

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".
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