Drug intelligence / Profile preview

entrectinib + osimertinib

Development stage: Preclinical
Lead developer: Genentech
Modality: Small Molecules
Administration: Oral

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).

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)JAK2 (Janus kinase 2)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TNK2 (Activated Cdc42-associated kinase 1)

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