Serlopitant

Last updated
Serlopitant
Serlopitant.svg
Clinical data
Routes of
administration
By mouth
ATC code
  • None
Identifiers
  • 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
Formula C29H28F7NO2
Molar mass 555.537 g·mol−1
3D model (JSmol)
  • 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=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

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]

See also

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<span class="mw-page-title-main">Vofopitant</span> Chemical compound

Vofopitant (GR205171) is a drug which acts as an NK1 receptor antagonist. It has antiemetic effects as with other NK1 antagonists, and also shows anxiolytic actions in animals. It was studied for applications such as the treatment of social phobia and post-traumatic stress disorder, but did not prove sufficiently effective to be marketed.

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<span class="mw-page-title-main">Vibegron</span> Medication

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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".