Azasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27 [1] It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg".[2] Pharmacokinetics data from S. Tsukagoshi.[3]
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Routes of administration | Oral |
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Pharmacokinetic data | |
Bioavailability | 90% |
Excretion | 60-70% |
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Formula | C17H20ClN3O3 |
Molar mass | 349.82 g·mol−1 |
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R-azasetron besylate (SENS-401) has been studied to prevent hearing loss related to sudden sensorineural hearing loss (SSNHL),[4] acoustic trauma,[5] and cisplatin-induced ototoxicity.[4][6]
SENS-401 for Platinum-Induced Ototoxicity Sensorion has received the FDAs orphan drug designation for SENS-401 for the prevention of platinum-induced ototoxicity in pediatric patients. As many as 60% of patients develop severe hearing loss due to platinum-based chemo therapies. There is no approved pharmaceutical treatment. SENS-401 (R-azasetron besylate) is designed to protect and preserve inner ear tissue when lesions may cause progressive hearing impairments. The drug (both oral and injectable) is also in development for the treatment of sudden sensorineural hearing loss. Sensorion expects to initiate a phase 2 clinical trial in this indication in the first half of 2018.