Drug intelligence / Profile preview

alectinib + entrectinib

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Alectinib + entrectinib is an investigational combination of two oral small molecule tyrosine kinase inhibitors being studied for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) with specific genetic alterations. - **Alectinib** is a next-generation inhibitor of anaplastic lymphoma kinase (ALK) that blocks ALK-mediated signaling, leading to inhibition of cancer cell proliferation and survival. - **Entrectinib** is a multi-targeted inhibitor that blocks the activity of TRK (TRKA/TRKB/TRKC, encoded by NTRK1/2/3), ROS1, and ALK fusion proteins, suppressing oncogenic signaling, cell proliferation, and tumor growth[1][3][5]. Both drugs are being tested individually and in combination in clinical trials to address therapeutic resistance and improve outcomes in NSCLC and other solid tumors harboring ALK rearrangements, NTRK fusions, or ROS1 rearrangements[4][7][8].

02

Targets

TNK2 (Activated Cdc42-associated kinase 1)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)JAK2 (Janus kinase 2)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK3 (Tropomyosin receptor kinase C)RET (Rearranged during transfection receptor tyrosine kinase)

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