Drug intelligence / Profile preview

azasetron

Development stage
Phase 1
Lead developer
Torii Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Azasetron is a small molecule antiemetic drug that acts as a selective antagonist of the serotonin 5-hydroxytryptamine 3 (5-HT3) receptor. It is primarily used for the prevention and management of nausea and vomiting induced by cancer chemotherapy, including cisplatin-based regimens. Azasetron is administered orally or intravenously and has high bioavailability (about 90%). The drug is approved for marketing in Japan under the brand name Serotone and marketed exclusively by Torii Pharmaceutical. In addition to its antiemetic effects, preclinical studies have suggested potential antimitogenic and apoptotic effects on cancer cell lines as well as investigational use in preventing hearing loss related to sudden sensorineural hearing loss (SSNHL), acoustic trauma, and cisplatin-induced ototoxicity[1][4][5].

Brand names
Serotone
Other names
azasetron hydrochlorideazasetron besylateN-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)

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