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azasetron
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Azasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27 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". Pharmacokinetics data from S. Tsukagoshi.
In the Vinony graph
Vinony's link graph records 1,400 inbound references to azasetron, and connects out to N-methylserotonin, glaucine and 5-carboxamidotryptamine.
It sits within the topics 5-HT3 antagonists, Chemical pages without DrugBank identifier and Chlorobenzene derivatives.
Vinony links it to 7 Wikipedia language editions.
Chemical data
- Formula
- C17H20ClN3O3
- Molecular weight
- 349.8 g/mol
- IUPAC name
- N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Phase 2
- Molecule type
- Small molecule
- Indications
- hearing loss
via ChEMBL · EBI
Research
106 papers- Efficacy of azasetron on postoperative chronic pain after pulmonary surgery: a randomized triple-blind controlled trial.BMC anesthesiology · 2024
- Stability of azasetron-dexamethasone mixture for chemotherapy-induced nausea and vomiting administration.Oncotarget · 2017
- Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis.The Cochrane database of systematic reviews · 2021
- Determination of azasetron hydrochloride in rabbit plasma by liquid chromatography tandem mass spectrometry and its application.Biomedical chromatography : BMC · 2011
- Comparison of azasetron and ondansetron for preventing postoperative nausea and vomiting in patients undergoing gynecological laparoscopic surgery.Yonsei medical journal · 2010
via PubMed
Wikidata facts
- Mass
- 349.119319
Show 3 more facts
- chemical formula
- C₁₇H₂₀ClN₃O₃
- canonical SMILES
- CN1C(=O)COC2=C1C=C(C=C2C(=O)NC3CN4CCC3CC4)Cl
- Commons category
- Azasetron
Sources (2)
via Wikidata · CC0
~1 min read
Encyclopedic overview
1 sectionsContents
- References
Azasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27 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". Pharmacokinetics data from S. Tsukagoshi.
Arazasetron besylate (SENS-401) is an investigational drug formulation containing exclusively the R-enantiomer of azasetron. The compound has been studied to prevent hearing loss related to sudden sensorineural hearing loss (SSNHL), acoustic trauma, and cisplatin-induced ototoxicity.
Excerpted from Wikipedia’s “azasetron” article, available under the CC BY-SA 4.0 licence.