Drug intelligence / Profile preview

rolapitant

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous Emulsion
01

Overview

Rolapitant is a selective and competitive antagonist of the human substance P/neurokinin 1 (NK1) receptor. It is used in combination with other antiemetic agents to prevent delayed nausea and vomiting associated with emetogenic cancer chemotherapy in adults. Rolapitant works by blocking signals to the brain that cause nausea and vomiting. It is typically administered as a single oral dose before chemotherapy and has a long elimination half-life allowing for sustained effect over several days[2][10][3]. The drug was originally developed by Schering-Plough.

Brand names
VarubiVaruby
Other names
(5S,8S)-8-({(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-onerolapitant hydrochloride monohydrate
02

Targets

TACR3 (Neurokinin 3 Receptor)TACR1 (Neurokinin‑1 Receptor)GR (Glucocorticoid receptor)

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