Drug intelligence / Profile preview

erlotinib + fulvestrant

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intramuscular, Oral
01

Overview

Erlotinib + fulvestrant is a combination therapy consisting of erlotinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and fulvestrant, a selective estrogen receptor degrader (SERD). Erlotinib inhibits EGFR signaling pathways involved in cell proliferation and survival, while fulvestrant binds to estrogen receptors and accelerates their degradation, blocking estrogen-driven tumor growth. This combination has been investigated primarily for advanced or metastatic non-small cell lung cancer (NSCLC), particularly in patients whose tumors express hormone receptors. The rationale is based on preclinical evidence of cross-talk between the EGFR and estrogen receptor pathways in NSCLC. Clinical trials have shown that the combination is well tolerated with mainly mild dermatologic and gastrointestinal side effects. Some increased activity was observed among EGFR wild-type NSCLC patients compared to erlotinib alone[1][2][3][4][5].

Brand names
FaslodexTarceva
Other names
none
02

Targets

ESR2 (ERβ)EGFR T790M (Epidermal growth factor receptor T790M mutant)ESR1 (ERα)

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