Drug intelligence / Profile preview

vorinostat + capecitabine

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

Overview

Vorinostat + capecitabine is a combination therapy investigated for the treatment of advanced solid tumors. Vorinostat (also known as suberoylanilide hydroxamic acid or SAHA) is a small molecule histone deacetylase (HDAC) inhibitor that works by inhibiting Class I and II HDACs, thereby modulating gene expression to induce cell cycle arrest and apoptosis. Capecitabine is an oral fluoropyrimidine carbamate prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in vivo. 5-FU subsequently inhibits thymidylate synthase, disrupting DNA synthesis and cell proliferation. This specific combination was evaluated by the University Health Network in Toronto in a Phase I dose-escalation study to determine the safety and optimal dosing for patients with unresectable or metastatic solid tumors.

Brand names
ZolinzaXeloda
Other names
suberoylanilide hydroxamic acidN-hydroxy-N'-phenyloctanediamide
02

Targets

HDAC6 (Histone deacetylase 6)TS (Thymidylate synthase)HDAC1 (Histone Deacetylase 1)

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