Drug intelligence / Profile preview

abexinostat

Development stage
Phase 3
Lead developer
Xynomic Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Abexinostat is an orally bioavailable, small molecule, broad-spectrum hydroxamic acid-based histone deacetylase (HDAC) inhibitor being developed as an antineoplastic agent. It primarily inhibits HDAC1, but also targets HDAC2, 3, 6, and 10. Abexinostat inhibits HDACs, leading to the accumulation of acetylated histones and tubulin in tumor cells, resulting in chromatin remodeling and selective transcriptional activation of tumor suppressor genes, inducing cell cycle arrest and apoptosis in cancer cells. It has shown antitumor activity across various hematologic malignancies and solid tumors. Developers include Xynomic Pharmaceuticals, GSK, Janssen Inc., Massachusetts General Hospital, Memorial Sloan-Kettering Cancer Center, Pharmacyclics (now part of AbbVie), Servier, and University of California at San Francisco. It is administered orally with dosing schedules designed to maintain effective drug concentrations while managing toxicity.

Other names
abexinostat hydrochloride
02

Targets

HDAC6 (Histone deacetylase 6)MBLAC2 (Metallo-beta-lactamase domain-containing protein 2)HDAC10 (Histone Deacetylase 10)HDAC1 (Histone Deacetylase 1)HDAC8 (Histone Deacetylase 8)

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