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bexarotene + gefitinib
- Development stage
- Phase 2
- Lead developer
- Stanford Cancer Institute
- Modality
- Small Molecules
- Administration
- Oral
01
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].
02
Targets
EGFR (Epidermal growth factor receptor)RXRA (Retinoid X receptor alpha)
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