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IV Casopitant (GW679769)

GlaxoSmithKline · Phase 3 active Small molecule

Casopitant is a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center to prevent chemotherapy-induced nausea and vomiting.

Casopitant is a neurokinin-1 (NK1) receptor antagonist that blocks substance P signaling in the chemoreceptor trigger zone and vomiting center to prevent chemotherapy-induced nausea and vomiting. Used for Chemotherapy-induced nausea and vomiting (CINV) prevention in patients receiving highly emetogenic chemotherapy.

At a glance

Generic nameIV Casopitant (GW679769)
SponsorGlaxoSmithKline
Drug classNK1 receptor antagonist
TargetNK1 receptor (neurokinin-1 receptor)
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Casopitant selectively antagonizes the NK1 receptor, which is a key mediator of nausea and vomiting pathways in the central nervous system. By blocking substance P binding to NK1 receptors, it prevents both acute and delayed emetic responses triggered by chemotherapy. This mechanism complements 5-HT3 antagonists and corticosteroids in multimodal antiemetic regimens.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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