Drug intelligence / Profile preview

rosiglitazone + bexarotene

Development stage
Unknown
Lead developer
Vanderbilt University
Modality
Small Molecules
Administration
Oral
01

Overview

This is an investigational combination therapy consisting of the PPARγ agonist rosiglitazone and the retinoid X receptor (RXR) agonist bexarotene. Developed by Vanderbilt University, the combination was evaluated in a Phase 2 pilot study for the treatment of cutaneous T-cell lymphoma (CTCL). The rationale for the combination is based on in vitro evidence suggesting synergistic induction of apoptosis in CTCL cells through the activation of the PPARγ-RXR heterodimer. Bexarotene is an approved treatment for CTCL, while rosiglitazone is a thiazolidinedione typically used for type 2 diabetes. The study investigated whether adding rosiglitazone to a stable bexarotene regimen could improve clinical outcomes in patients with stable or progressive disease, showing modest clinical benefits and alleviation of pruritus, though accompanied by adverse events such as hyperlipidemia and cytopenias.

Other names
rosiglitazone and bexarotene
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)RXRA (Retinoid X receptor alpha)

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