Serlopitant

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;

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]

References

^ "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.
^ 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.
^ 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.
^ "For Irritating Itch, a Promising Option Under Scrutiny".

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[INN-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".

[1]

[2]

[3]

[4]

v t e Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Elinzanetant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Elinzanetant Fezolinetant Osanetant Pavinetant SB-218,795 SB-222,200 Talnetant

See also

References