Palonosetron

Description: Palonosetron (also known as RS 25259, RS 25259 197; trade name: Aloxi and Akynzeo) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. As of April 2018, the combination of fosnetupitant and palonosetron has been approved by FDA to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Palonosetron is a highly potent, selective, second-generation 5-HT3 receptor antagonist with a 5-HT3 receptor binding affinity that is ?100-fold higher than other 5-HT3 receptor antagonists (pKi 10.5 compared with 8.91 for granisetron, 8.81 for tropisetron, 8.39 for ondansetron, 7.6 for dolasetron).

References: Br J Pharmacol. 1995 Feb; 114(4):851-9; Ann Oncol. 2003 Oct; 14(10):1570-7.

Related CAS#:135729-62-3 (HCl); 135729-75-8 ((R, R)-Palonosetron Hydrochloride)