Belinostat — Drug Monograph

Brand names: Beleodaq

Drug class: Other

Mechanism of Action

Belinostat is a histone deacetylase (HDAC) inhibitor. It inhibits the enzymatic activity of histone deacetylases, which results in the accumulation of acetyl groups on histone proteins. This leads to an open chromatin structure (euchromatin) and increased transcription of tumor suppressor genes, resulting in cell cycle arrest and apoptosis. Belinostat also induces hyperacetylation of non-histone proteins like transcription factors and chaperone proteins, further contributing to its antineoplastic effects.

FDA Indications

Common Side Effects

Clinical Pearl

Patients known to be homozygous for the UGT1A1*28 allele have reduced clearance of belinostat and should start at a reduced dose of 600 mg/m². Unlike some other HDAC inhibitors like romidepsin, belinostat does not have a black box warning for QT prolongation, though it should still be used with caution in patients with cardiac risk factors. The "5 days on, 16 days off" schedule is intensive for an IV drug, so coordination with infusion centers is key. Monitor for tumor lysis syndrome in…

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