Drug intelligence / Profile preview

egf816 + ribociclib

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

EGF816 + ribociclib is a combination of two small molecule targeted therapies investigated for the treatment of advanced non-small cell lung cancer (NSCLC) harboring EGFR mutations. **EGF816 (nazartinib)** is a third-generation, irreversible EGFR tyrosine kinase inhibitor (TKI) that targets T790M-mediated resistance mutations in EGFR-mutant tumors. **Ribociclib (LEE011)** is an orally bioavailable inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are critical for the regulation of the cell cycle. The combination aims to enhance antitumor efficacy by simultaneously inhibiting EGFR signaling and blocking cell cycle progression, potentially overcoming or delaying resistance mechanisms in EGFR-mutant NSCLC[1][2][3][4].

02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)HSP90AA1 (Heat shock protein HSP90-alpha)CTNNB1 (Beta-catenin)

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