Drug intelligence / Profile preview

casopitant

Development stage
Phase 3
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Casopitant is a small molecule neurokinin 1 (NK1) receptor antagonist developed by GlaxoSmithKline for the prevention of chemotherapy-induced and postoperative nausea and vomiting. It acts by competitively binding to and blocking the NK1 receptor, thereby inhibiting the action of substance P, a neuropeptide involved in emesis pathways. Casopitant was investigated in both oral and intravenous formulations as an add-on therapy to standard antiemetic regimens. Although it reached phase III clinical trials for antiemetic indications, its regulatory applications were withdrawn due to safety concerns requiring further assessment. More recently, casopitant has been studied as a potential antidepressant for major depressive disorder, with at least one phase II trial completed[1][3][4][5][7].

Brand names
RezonicZunrisa
Other names
casopitant [INN]
02

Targets

TACR1 (Neurokinin‑1 Receptor)

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