Rolapitant is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
IC50 & Target：Ki: 0.66 nM (neurokinin)
Room temperature in continental US; may vary elsewhere.
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Rolapitant has a high affinity for the human NK1 receptor with a Ki of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit.
Rolapitant reverses NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, consistent with clinical data for other NK1 antagonists. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication.
LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548209/ PubMed PMID: 31643534.
Heo YA, Deeks ED. Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting. Drugs. 2017 Oct;77(15):1687-1694. doi: 10.1007/s40265-017-0816-z. Review. PubMed PMID: 28929404.
Rapoport BL, Aapro M, Chasen MR, Jordan K, Navari RM, Schnadig I, Schwartzberg L. Recent developments in the clinical pharmacology of rolapitant: subanalyses in specific populations. Drug Des Devel Ther. 2017 Sep 5;11:2621-2629. doi: 10.2147/DDDT.S133943. eCollection 2017. Review. PubMed PMID: 28919712; PubMed Central PMCID: PMC5592904.
Rapoport BL. Rolapitant: An NK-1 Receptor Antagonist for the Prevention of Chemotherapy- Induced Nausea and Vomiting. Rev Recent Clin Trials. 2017;12(3):193-201. doi: 10.2174/1574887112666170406104854. Review. PubMed PMID: 28393710.
Rashad N, Abdel-Rahman O. Differential clinical pharmacology of rolapitant in delayed chemotherapy-induced nausea and vomiting (CINV). Drug Des Devel Ther. 2017 Mar 24;11:947-954. doi: 10.2147/DDDT.S108872. eCollection 2017. Review. PubMed PMID: 28392676; PubMed Central PMCID: PMC5373840.
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