Drug intelligence / Profile preview

capecitabine + vorinostat

Development stage
Unknown
Lead developer
Merck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Capecitabine + vorinostat is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action, evaluated primarily in oncology. Capecitabine is an orally administered prodrug that is enzymatically converted to 5-fluorouracil (5-FU) within tumor cells, where it acts as a nucleoside metabolic inhibitor and antimetabolite, interfering with DNA synthesis and leading to cancer cell death[3][2]. Vorinostat (also known as suberoylanilide hydroxamic acid or SAHA) is a histone deacetylase (HDAC) inhibitor that modulates gene expression by altering chromatin structure, resulting in cell cycle arrest, differentiation, and apoptosis in cancer cells[1][2]. Preclinical studies have shown that vorinostat can upregulate thymidine phosphorylase—an enzyme involved in the activation of capecitabine—thereby enhancing the antitumor effects of capecitabine through synergistic mechanisms[2]. This combination has been studied for its potential efficacy in various cancers including colorectal cancer and head and neck squamous cell carcinoma[2][4].

Brand names
ZolinzaXeloda
Other names
SAHAsuberoylanilide hydroxamic acid
02

Targets

TS (Thymidylate synthase)

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