|By mouth (tablets)|
|Metabolites||C4-pyrrolidine-hydroxylated rolapitant (major)|
|Biological half-life||169–183 hours|
|Excretion||Feces (52–89%), urine (9–20%)|
|Chemical and physical data|
|Molar mass||500.476 g/mol|
|3D model (Jmol)||Interactive image|
Rolapitant (INN, trade name Varubi vuh-ROO-bee, code name SCH 619734) is a drug originally developed by Schering-Plough and licensed for clinical development by Tesaro, which acts as a selective NK1 receptor antagonist (antagonist for the NK1 receptor). It has been approved as a medication for the treatment of chemotherapy-induced nausea and vomiting (CINV) after clinical trials showed it to have similar or improved efficacy and some improvement in safety over existing drugs for this application.
Rolapitant is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.
- "Varubi (rolapitant) Tablets, for Oral Use. Full Prescribing Information" (PDF). TESARO, Inc. 1000 Winter St., #3300, Waltham, MA 02451.
- "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 59" (PDF). World Health Organization. p. 64. Retrieved 5 October 2016.
- Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. doi: 10.1016/j.pbb.2012.03.021. PMID 22497992
- Jordan K, Jahn F, Aapro M. Recent developments in the prevention of chemotherapy-induced nausea and vomiting (CINV): a comprehensive review. Ann Oncol. 2015 Jun;26(6):1081-90. doi: 10.1093/annonc/mdv138. PMID 25755107
- Nasir SS, Schwartzberg LS. Recent Advances in Preventing Chemotherapy-Induced Nausea and Vomiting. Oncology (Williston Park). 2016 Aug;30(8). pii: 218410. PMID 27539626
- Rapoport B, Schwartzberg L, Chasen M, Powers D, Arora S, Navari R, Schnadig I. Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy. Eur J Cancer. 2016 Apr;57:23-30. doi: 10.1016/j.ejca.2015.12.023. PMID 26851398
- Chasen MR, Rapoport BL. Rolapitant for the treatment of chemotherapy-induced nausea and vomiting: a review of the clinical evidence. Future Oncol. 2016 Mar;12(6):763-78. doi: 10.2217/fon.16.11. PMID 26842387