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Zabadinostat (formerly CXD101 and AZD-9468) is an orally bioavailable, Class I selective histone deacetylase (HDAC) inhibitor being developed by Celleron Therapeutics. It specifically targets HDAC1, HDAC2, and HDAC3 with high potency, which are enzymes involved in the epigenetic regulation of gene expression. By inhibiting these targets, zabadinostat is designed to alter the transcriptional profile of cancer cells, leading to cell cycle arrest, apoptosis, and potentially reversing immune evasion. The drug is primarily being investigated for the treatment of advanced or metastatic cancers, including microsatellite-stable (MSS) colorectal cancer, where it is evaluated in combination with immune checkpoint inhibitors like nivolumab to sensitize tumors that are typically resistant to immunotherapy.
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