Rolapitant

Rolapitant
Clinical data
Pronunciation roe-LA-pi-tant
Trade names Varubi
Routes of
administration		 By mouth (tablets)
ATC code None
Legal status
Legal status
Pharmacokinetic data
Protein binding 99.8%
Metabolism CYP3A4
Metabolites C4-pyrrolidine-hydroxylated rolapitant (major)
Biological half-life 169–183 hours
Excretion Feces (52–89%), urine (9–20%)[1]
Identifiers
CAS Number 552292-08-7 YesY
PubChem (CID) 10311306
IUPHAR/BPS 5749
DrugBank DB09291 YesY
ChemSpider 8486772
UNII NLE429IZUC N
KEGG D10742
ChEBI CHEBI:90908 YesY
Chemical and physical data
Formula C25H26F6N2O2
Molar mass 500.476 g/mol
3D model (Jmol) Interactive image

Rolapitant (INN,[2] 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).[3] 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.[4][5][6][7]

Indications

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.[1]

See also

References

  1. 1 2 "Varubi (rolapitant) Tablets, for Oral Use. Full Prescribing Information" (PDF). TESARO, Inc. 1000 Winter St., #3300, Waltham, MA 02451.
  2. ↑ "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.
  3. ↑ 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
  4. ↑ 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
  5. ↑ Nasir SS, Schwartzberg LS. Recent Advances in Preventing Chemotherapy-Induced Nausea and Vomiting. Oncology (Williston Park). 2016 Aug;30(8). pii: 218410. PMID 27539626
  6. ↑ 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
  7. ↑ 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
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