Drug intelligence / Profile preview

vorinostat + bexarotene

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**Vorinostat + bexarotene** is an investigational **combination therapy** of two small-molecule drugs: vorinostat, a histone deacetylase (HDAC) inhibitor, and bexarotene, a retinoid X receptor (RXR) agonist. Both agents are individually approved for use in cutaneous T-cell lymphoma (CTCL) and have shown activity as monotherapies. The rationale for the combination is based on preclinical and clinical evidence that pairing an HDAC inhibitor (vorinostat) with an RXR agonist (bexarotene) leads to cooperative activation of gene transcription and increased apoptosis in malignant T-cells. Clinical trials in CTCL patients refractory to other treatments indicate that this combination can be administered with manageable toxicity if lower doses than monotherapy are used. Most common adverse effects include hypothyroidism, hypertriglyceridemia, and fatigue[1][2][3].

02

Targets

HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC11 (Histone Deacetylase 11)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)RXRA (Retinoid X receptor alpha)RXRB (Retinoid X receptor beta)RXRG (RXRγ)

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