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dasatinib + osimertinib

Development stage: Unknown
Lead developer: AstraZeneca
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy consisting of dasatinib, a Src inhibitor, and osimertinib, an EGFR tyrosine kinase inhibitor. This combination was developed to target both EGFR mutations and Src activation, with the hypothesis that dual inhibition could overcome resistance to EGFR-TKI therapy in EGFR-mutant non-small cell lung cancer (NSCLC). The combination demonstrated anticancer activity in clinical trials but was limited by chronic toxicities mainly attributed to dasatinib.

Targets

SFK (SRC family kinases)EGFR T790M (Epidermal growth factor receptor T790M mutant)PDGFR (PDGFR family)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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