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entrectinib + osimertinib
- Development stage
- Preclinical
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination therapy consisting of entrectinib (an NTRK fusion inhibitor) and osimertinib (an EGFR-TKI). This combination has been studied for treating EGFR-mutated non-small cell lung cancer (NSCLC) that has developed resistance to osimertinib monotherapy through acquired NTRK fusion. The approach works by simultaneously targeting both the original EGFR mutation (with osimertinib) and the acquired NTRK fusion (with entrectinib).
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)JAK2 (Janus kinase 2)NTRK3 (Tropomyosin receptor kinase C)TNK2 (Activated Cdc42-associated kinase 1)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)EGFR T790M (Epidermal growth factor receptor T790M mutant)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)
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