Oncology

Quisinostat is a novel selective oral, highly-potent pan-histone deacetylase (HDAC1) inhibitor originated from Janssen Pharmaceuticals.

Histone deacetylase (HDAC) inhibitors have been shown to induce cell cycle arrest, terminal differentiation, and/or apoptosis in a broad spectrum of human tumor cell lines in vitro, and exhibit potent in vivo antitumor activity in human xenograft models in nude mice. Inhibition of the HDAC enzyme promotes the acetylation of nucleosome histone tails, favoring a more transcriptionally competent chromatin structure, which in turn leads to altered expression of genes involved in cellular processes such as cell proliferation, apoptosis, and differentiation.

Nonclinical studies of quisinostat showed that the compound exhibits potent anti-tumor activity in tumor cell lines and animal tumor models.

A number of non clinical, Phase I and II clinical trials evaluated quisinostat's safety and efficacy and showed that qusinostat has a promising anti-tumor activity against several types of advanced refractory solid and hematological malignancies, including platinum-resistant ovarian cancer in combination with paclitaxel and carboplatin, uveal melanoma and synovial sarcoma.