Drug intelligence / Profile preview

vorinostat + capecitabine + cisplatin

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

Overview

Vorinostat + capecitabine + cisplatin is an investigational combination chemotherapy regimen studied primarily for the treatment of unresectable or metastatic gastric cancer. Vorinostat is a small molecule histone deacetylase (HDAC) inhibitor that modulates gene expression by altering chromatin structure, leading to cell cycle arrest and apoptosis in cancer cells. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a pyrimidine analog that inhibits thymidylate synthase, thereby interfering with DNA synthesis and repair. Cisplatin is a platinum-based chemotherapeutic agent that forms DNA crosslinks, resulting in apoptosis. The combination aims to enhance antitumor activity through synergistic effects on multiple cellular pathways involved in tumor growth and survival[1][2]. This regimen has been evaluated as first-line therapy for advanced gastric cancer but did not meet its primary endpoint in clinical trials due to increased toxicity compared with standard doublet regimens[1][2].

02

Targets

HDAC2 (Histone deacetylase 2)HDAC1 (Histone Deacetylase 1)HDAC6 (Histone deacetylase 6)DNAHDAC3 (Histone Deacetylase 3)TS (Thymidylate synthase)

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