Drug intelligence / Profile preview

quisinostat + gemcitabine + cisplatin

Development stage
Preclinical
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a **combination therapy** consisting of **quisinostat** (a second-generation histone deacetylase inhibitor), **gemcitabine** (a nucleoside analog antineoplastic agent), and **cisplatin** (a platinum-based DNA-damaging agent). Quisinostat inhibits histone deacetylases, leading to increased acetylation of histones and altered gene expression, thereby promoting apoptosis and cell cycle arrest in cancer cells. Gemcitabine incorporates into DNA, inhibiting DNA synthesis, while cisplatin induces inter- and intra-strand DNA crosslinks, leading to apoptosis. Research indicates that quisinostat has a **synergistic effect** with cisplatin (and separately with gemcitabine) in urothelial carcinoma cell lines, including in cisplatin-resistant sublines, resulting in enhanced cell cycle disturbance, apoptosis, and DNA damage. The combination of gemcitabine and cisplatin is a long-established regimen for a variety of solid tumors, especially biliary tract and bladder cancers, and is FDA-approved when used as a two-drug combination. The three-drug combination, specifically quisinostat + gemcitabine + cisplatin, is under investigation and demonstrates increased efficacy with tolerable toxicity in preclinical models[1][5].

Other names
quisinostat + gemcitabine + cisplatin
02

Targets

DNAHDAC (HDAC family)

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