Drug intelligence / Profile preview

third-generation EGFR-TKI + vinorelbine

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy consisting of a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and vinorelbine. Third-generation EGFR-TKIs, such as osimertinib, are small molecule inhibitors that selectively target both sensitizing and T790M resistance mutations in the EGFR gene, which are commonly found in non-small cell lung cancer (NSCLC). These agents block the ATP-binding site of mutant EGFR, inhibiting downstream signaling pathways involved in tumor cell proliferation and survival. Vinorelbine is a semi-synthetic vinca alkaloid chemotherapy agent that disrupts microtubule assembly by binding to tubulin, thereby inhibiting mitosis and inducing apoptosis in rapidly dividing cancer cells. The combination aims to leverage targeted inhibition of oncogenic signaling with cytotoxic disruption of cell division for enhanced antitumor efficacy, particularly in NSCLC patients with activating EGFR mutations.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))

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