Drug intelligence / Profile preview

casopitant + docetaxel

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

Overview

Casopitant + docetaxel is a combination of two pharmaceutical agents used primarily in the context of cancer therapy and supportive care. Docetaxel is a taxoid antineoplastic agent that promotes the assembly and stabilization of microtubules by binding to the β-subunit of tubulin, thereby inhibiting their depolymerization. This disrupts mitotic cell division and leads to apoptosis in rapidly dividing cancer cells[1][4][5]. Casopitant is a potent neurokinin-1 (NK1) receptor antagonist that acts centrally to block substance P-mediated emetic signaling pathways. It has been investigated for its antiemetic properties in chemotherapy-induced nausea and vomiting (CINV), particularly as an adjunct to regimens containing cytotoxic agents like docetaxel[7]. The combination has been studied for safety and pharmacokinetic interactions; coadministration does not significantly alter the pharmacokinetics or toxicity profile of docetaxel[3].

02

Targets

TACR1 (Neurokinin‑1 Receptor)

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