Drug intelligence / Profile preview

vorinostat + melphalan + prednisone

Development stage
Phase 2
Lead developer
Tiziana Marangon
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Vorinostat + melphalan + prednisone (ZMP) is a combination regimen investigated for the treatment of relapsed or refractory multiple myeloma. Vorinostat (Zolinza) is a small molecule inhibitor of Class I and II histone deacetylases (HDAC), which induces cell cycle arrest and apoptosis in malignant cells. Melphalan is a nitrogen mustard alkylating agent that causes DNA cross-linking, and prednisone is a synthetic corticosteroid with anti-inflammatory and immunosuppressive properties. This specific combination was evaluated in a Phase I/II clinical trial (NCT00857324) led by Tiziana Marangon at the University of Turin to determine if the synergistic effects of HDAC inhibition could enhance the efficacy of the standard melphalan-prednisone (MP) backbone in advanced myeloma patients.

Other names
vorinostat-melphalan-prednisoneSAHA + melphalan + prednisonesuberoylanilide hydroxamic acid + melphalan + prednisone
02

Targets

DNAGR (Glucocorticoid receptor)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)

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