.Pharmacolibrary.Drugs.ATC.A.A04AD13 .Pharmacolibrary.Drugs.ATC.A.A04AD13| name: | Casopitant |
| ATC code: | A04AD13 | route: | oral |
| n-compartments | 2 |
Casopitant is a neurokinin-1 (NK1) receptor antagonist that was developed for the prevention of chemotherapy-induced nausea and vomiting (CINV). Clinical development was discontinued and the drug is not currently approved for use in any country.
Pharmacokinetic parameters estimated for healthy adult subjects following single oral administration. No published human PK model available; values estimated based on available summaries from clinical study result reports.
Bauman, JW, et al., & Gutierrez, M (2012). Effect of hepatic or renal impairment on the pharmacokinetics of casopitant, a NK-1 receptor antagonist. Investigational new drugs 30(2) 662–671. DOI:10.1007/s10637-010-9604-2 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21188466
Hesketh, PJ, et al., & Makhson, A (2012). Single-dose intravenous casopitant in combination with ondansetron and dexamethasone for the prevention of oxaliplatin-induced nausea and vomiting: a multicenter, randomized, double-blind, active-controlled, two arm, parallel group study. Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer 20(7) 1471–1478. DOI:10.1007/s00520-011-1235-4 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21822913
Zamuner, S, et al., & Cunningham, VJ (2012). A pharmacokinetic PET study of NK₁ receptor occupancy. European journal of nuclear medicine and molecular imaging 39(2) 226–235. DOI:10.1007/s00259-011-1954-2 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21993526