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vestipitant

Development stage: Phase 2
Lead developer: GSK
Modality: Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration: Oral

Overview

Vestipitant is a potent and selective small molecule antagonist of the neurokinin 1 (NK1) receptor, developed by GlaxoSmithKline. It was investigated as an antiemetic for postoperative nausea and vomiting, as well as for potential use in anxiety disorders, major depressive disorder, tinnitus, hearing loss, dyspepsia, and insomnia. Vestipitant demonstrated anxiolytic properties and was shown to improve sleep maintenance in patients with primary insomnia without next-day cognitive impairment. Despite its favorable safety profile and pharmacokinetic properties, clinical development has been discontinued for all indications due to lack of efficacy or strategic reasons[2][3][4][5].

Brand names: vestipitant
Other names: vestipitant

Targets

TACR1 (Neurokinin‑1 Receptor)

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