Drug intelligence / Profile preview

topotecan + vorinostat

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

Overview

Topotecan + vorinostat is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action, evaluated primarily for the treatment of relapsed or recurrent small cell lung cancer (SCLC). Topotecan is a topoisomerase I inhibitor that induces DNA damage by stabilizing the topoisomerase I-DNA complex, leading to replication arrest and apoptosis. Vorinostat is a histone deacetylase (HDAC) inhibitor that modulates gene expression and promotes cell cycle arrest and apoptosis. Preclinical studies have demonstrated strong synergistic antitumor effects when these agents are combined, resulting in enhanced S-phase cell cycle arrest, increased DNA double-strand breaks, and caspase-dependent apoptosis. The combination has been explored in early-phase clinical trials for chemosensitive recurrent SCLC[1][2][5].

Other names
vorinostat and topotecantopotecan and vorinostat
02

Targets

TOP1 (DNA Topoisomerase I)

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