Drug intelligence / Profile preview

pracinostat

Development stage
Phase 3
Lead developer
MEI Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Pracinostat is an orally bioavailable, small-molecule histone deacetylase (HDAC) inhibitor based on hydroxamic acid. It selectively inhibits class I, II, and IV HDACs (excluding class III), including HDAC6 in class IIb, but does not affect other zinc-binding enzymes, receptors, or ion channels. Pracinostat accumulates in tumor cells and exerts continuous inhibition of histone deacetylases, leading to the accumulation of acetylated histones, chromatin remodeling, transcriptional activation of tumor suppressor genes, cell cycle arrest and/or apoptosis. It has demonstrated anti-tumor activity in preclinical models and is being investigated for the treatment of various cancers including acute myeloid leukemia (AML), T-cell lymphoma, sarcoma, prostate cancer, myelofibrosis, myelodysplastic syndrome (MDS), diffuse large B-cell lymphoma (DLBCL), and colorectal cancer. The drug has been granted Orphan Drug status by the FDA for AML and T-cell lymphoma[1][2][4][5][6][7].

Other names
pracinostatumpracinostat dihydrochloride
02

Targets

HDAC2 (Histone deacetylase 2)HDAC1 (Histone Deacetylase 1)HDAC8 (Histone Deacetylase 8)Class II and IV histone deacetylasesHDAC3 (Histone Deacetylase 3)

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