Drug intelligence / Profile preview

everolimus + gefitinib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Everolimus + gefitinib is an investigational combination therapy consisting of two small molecule inhibitors used primarily in clinical trials for advanced cancers, notably non-small cell lung cancer (NSCLC) and metastatic castration-resistant prostate cancer. Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR), a key regulator of cell growth, proliferation, and survival. Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, which blocks downstream signaling pathways involved in tumor cell proliferation and survival. The rationale for combining these agents is to concurrently inhibit both EGFR-mediated signaling and mTOR-driven pathways to overcome resistance mechanisms and enhance antitumor activity. Clinical studies have shown some synergistic effects in preclinical models and modest response rates in NSCLC patients; however, overall antitumor activity has been limited in clinical settings[1][2][3][7].

02

Targets

Mechanistic target of rapamycin complex 1EGFR (Epidermal growth factor receptor)

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