Drug intelligence / Profile preview

vorinostat + lenalidomide + dexamethasone

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

Overview

Vorinostat + lenalidomide + dexamethasone is a combination therapy investigated primarily for the treatment of relapsed or refractory multiple myeloma. Vorinostat is a small molecule inhibitor of class I and II histone deacetylases (HDACs), which modulates gene expression and induces cell cycle arrest, differentiation, and apoptosis in malignant cells. Lenalidomide is an immunomodulatory agent structurally related to thalidomide that exerts anti-myeloma effects through direct tumoricidal activity, inhibition of angiogenesis, and modulation of the immune microenvironment. Dexamethasone is a synthetic glucocorticoid with potent anti-inflammatory and immunosuppressive properties that also induces apoptosis in certain hematologic malignancies. Preclinical studies suggest synergy between these agents due to their distinct but complementary mechanisms of action. Clinical trials have demonstrated that this combination can be effective and generally well-tolerated in patients with relapsed or refractory multiple myeloma[1][2][3][4][5][6].

Other names
Vorinostat-Lenalidomide-DexamethasoneSAHA + lenalidomide + dexamethasone
02

Targets

CRBN (Cereblon)GR (Glucocorticoid receptor)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)

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