Lerisetron

Lerisetron
Clinical data
Other names	F-0930-RS
ATC code	None;
Identifiers
	IUPAC name 1-Benzyl-2-piperazin-1-yl-1H-benzimidazole;
CAS Number	143257-98-1 ;
PubChem CID	65997 ;
ChemSpider	59389 ;
UNII	Q36R82SXRG ;
ChEMBL	ChEMBL56900 ;
CompTox Dashboard (EPA)	DTXSID90162368 ;
Chemical and physical data
Formula	C18H20N4
Molar mass	292.386 g·mol−1
	InChI InChI=1S/C18H20N4/c1-2-6-15(7-3-1)14-22-17-9-5-4-8-16(17)20-18(22)21-12-10-19-11-13-21/h1-9,19H,10-14H2 ; Key:PWWDCRQZITYKDV-UHFFFAOYSA-N ;
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Last updated September 02, 2025

Lerisetron (code name F-0930-RS) is a drug which acts as an antagonist at the 5-HT₃ receptor.^[1] It is a potent antiemetic ^[2]^[3] and was in clinical trials for the treatment of nausea associated with cancer chemotherapy.^[4]

References

↑ Orjales A, Mosquera R, Labeaga L, Rodes R (February 1997). "New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation". Journal of Medicinal Chemistry. 40 (4): 586–93. doi:10.1021/jm960442e. PMID 9046349.
↑ Gomez-de-Segura IA, Grande AG, De Miguel E (1998). "Antiemetic effects of Lerisetron in radiation-induced emesis in the dog". Acta Oncologica. 37 (7–8): 759–63. doi: 10.1080/028418698430160 . PMID 10050999.
↑ Cooper M, Sologuren A, Valiente R, Smith J (2002). "Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers". Arzneimittel-Forschung. 52 (9): 689–94. doi:10.1055/s-0031-1299952. PMID 12404884. S2CID 24423582.
↑ Huckle R (July 2003). "Lerisetron. FAES". Current Opinion in Investigational Drugs. 4 (7): 874–7. PMID 14619411.

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[1] Orjales A, Mosquera R, Labeaga L, Rodes R (February 1997). "New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation". Journal of Medicinal Chemistry. 40 (4): 586–93. doi:10.1021/jm960442e. PMID 9046349.

[2] Gomez-de-Segura IA, Grande AG, De Miguel E (1998). "Antiemetic effects of Lerisetron in radiation-induced emesis in the dog". Acta Oncologica. 37 (7–8): 759–63. doi: 10.1080/028418698430160 . PMID 10050999.

[3] Cooper M, Sologuren A, Valiente R, Smith J (2002). "Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers". Arzneimittel-Forschung. 52 (9): 689–94. doi:10.1055/s-0031-1299952. PMID 12404884. S2CID 24423582.

[4] Huckle R (July 2003). "Lerisetron. FAES". Current Opinion in Investigational Drugs. 4 (7): 874–7. PMID 14619411.

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Lerisetron

See also

References