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bexarotene + gefitinib

Development stage: Unknown
Lead developer: Stanford Cancer Institute
Modality: Small Molecules
Administration: Oral

Overview

Bexarotene + gefitinib is a combination therapy that has been studied for the treatment of non-small-cell lung cancer (NSCLC). Bexarotene is a selective retinoid X receptor (RXR) agonist that can repress cyclin D1 and EGFR expression, while gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. Both drugs affect similar oncogenic pathways and are metabolized through cytochrome P450 CYP3A4. Pharmacokinetic studies have shown that bexarotene appears to lower the Cmax and AUC0-24 of gefitinib, likely through induction of CYP3A4 metabolism[1].

Targets

RXRA (Retinoid X receptor alpha)EGFR (Epidermal growth factor receptor)

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