Drug intelligence / Profile preview

erlotinib + bexarotene

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Erlotinib + bexarotene is an investigational oral combination therapy consisting of two small molecule drugs with distinct mechanisms of action. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, while bexarotene is a rexinoid that selectively activates retinoid X receptors (RXRs). The combination has been studied primarily in non-small cell lung cancer (NSCLC), including KRAS-mutant and chemotherapy-refractory cases, as well as other advanced aerodigestive tract cancers. Preclinical and clinical studies have shown that the combination cooperatively represses cyclin D1 expression through different pathways, resulting in enhanced suppression of tumor cell growth compared to either agent alone. The regimen has demonstrated biological activity in early-stage NSCLC and clinical responses in advanced disease, with a safety profile similar to the individual agents[1][2][4].

02

Targets

EGFR (Epidermal growth factor receptor)RXRB (Retinoid X receptor beta)RXRG (RXRγ)RXRA (Retinoid X receptor alpha)

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