Drug intelligence / Profile preview

sunitinib + cisplatin + capecitabine

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This drug refers to the **combination of the small molecule tyrosine kinase inhibitor sunitinib, the platinum-based chemotherapeutic agent cisplatin, and the oral fluoropyrimidine prodrug capecitabine**. Sunitinib inhibits multiple receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), and others, yielding anti-angiogenic and antitumor effects. Cisplatin forms DNA adducts and crosslinks, interfering with DNA replication and transcription, ultimately leading to apoptosis. Capecitabine is a prodrug, metabolized preferentially in tumor tissues to 5-fluorouracil (5-FU), which inhibits thymidylate synthase, impairing DNA synthesis. This combination is under investigation for its safety, tolerability, and antitumor activity in advanced solid tumors, particularly gastrointestinal cancers, based on rationales of complimentary mechanisms and evidence of manageable safety profiles in initial studies[1][5][3].

02

Targets

DNAPDGFR (PDGFR family)TS (Thymidylate synthase)VEGFR (VEGFR family)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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