Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).IC50 Value:Target: 5-HT3 ReceptorPalonosetron is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy.
[1]. Celio L, Agustoni F, Testa I, Dotti K, De Braud F.Palonosetron: an evidence-based choice in prevention of nausea and vomiting induced by moderately emetogenic chemotherapy.Tumori. 2012 May;98(3):279-86. [2]. Blazer M, Phillips G, Reardon J, Efries D, Smith Y, Weatherby L, Juergens K, Rose J, Griffith N, Bekaii-Saab T.Antiemetic control with palonosetron in patients with gastrointestinal cancer receiving a fluoropyrimidine-based regimen in addition to either irinotecan or oxaliplatin: a retrospective study.Oncology. 2012;83(3):135-40. Epub 2012 Jul 18. [3]. Dogan U, Yavas G, Tekinalp M, Yavas C, Ata OY, Ozdemir K.Evaluation of the acute effect of palonosetron on transmural dispersion of myocardial repolarization.Eur Rev Med Pharmacol Sci. 2012 Apr;16(4):462-8. [4]. Jin Y, Sun W, Gu D, Yang J, Xu Z, Chen J.Comparative efficacy and safety of palonosetron with the first 5-HT3 receptor antagonists for the chemotherapy-induced nausea and vomiting: a meta-analysis.Eur J Cancer Care (Engl). 2012 Apr 22. [5]. Clark, Robin D.; Miller, Aaron B.; Berger, Jacob; Repke, David B.; Weinhardt, Klaus K.; Kowalczyk, Bruce A.; Eglen, Richard M.; Bonhaus, Douglas W.; Lee, Chi Ho; et al.2-(Quinuclidin-3-yl)pyrido[4,3-b]indol-1-ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor antagonists.J. Med. Chem., 1993, 36 (18), pp 2645-2657