Drug intelligence / Profile preview

volasertib + romidepsin

Development stage
Discontinued
Lead developer
Oncoheroes Biosciences
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

Volasertib + romidepsin is a combination therapy investigated for the treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL). Volasertib is a small molecule inhibitor of polo-like kinase 1 (PLK1), an enzyme essential for the progression of mitosis; its inhibition leads to cell cycle arrest at the G2/M phase and subsequent apoptosis. Romidepsin is a selective, potent inhibitor of Class I histone deacetylases (HDACs), which are enzymes that remove acetyl groups from histones, thereby regulating gene expression. By inhibiting HDACs, romidepsin induces histone hyperacetylation, leading to the transcriptional activation of genes involved in cell cycle arrest and apoptosis. The combination was evaluated in a Phase 1 trial (NCT01971476) sponsored by Dr. Anne Beaven to determine the maximum tolerated dose and efficacy in T-cell lymphomas.

Brand names
Istodax
Other names
Volasertib and Romidepsin combination
02

Targets

HDAC2 (Histone deacetylase 2)BRD4 (Bromodomain-containing protein 4)HDAC1 (Histone Deacetylase 1)PLK1 (Polo like kinase 1)HDAC3 (Histone Deacetylase 3)

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