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tacedinaline

Development stage: Phase 3
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

Tacedinaline is an orally bioavailable small molecule that functions as a selective class I histone deacetylase (HDAC) inhibitor, primarily targeting HDAC1, HDAC2, and HDAC3. Its mechanism involves inhibiting histone deacetylation, which leads to histone hyperacetylation. This epigenetic modification promotes transcriptional activation of genes involved in differentiation, cell-cycle arrest, and apoptosis in susceptible tumor cells. Tacedinaline has demonstrated antineoplastic activity in preclinical models and has been investigated in clinical trials for various cancers, including non-small cell lung cancer and pancreatic cancer.

Other names: AcetyldinalineN-acetyldinaline

Targets

HDAC8 (Histone Deacetylase 8)HDAC1 (Histone Deacetylase 1)

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