Drug intelligence / Profile preview

entrectinib

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

Overview

Entrectinib is a small molecule tyrosine kinase inhibitor used as an anti-cancer agent. It selectively inhibits tropomyosin receptor kinases (TRKA, TRKB, and TRKC), proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK). By blocking these kinases, entrectinib interferes with downstream signaling pathways that drive cancer cell proliferation and survival. This leads to reduced tumor growth and increased apoptosis of cancer cells. Entrectinib is primarily indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) that is ROS1-positive in adults, as well as for solid tumors with NTRK gene fusions in adults and children 1 month of age or older who have no satisfactory alternative treatments or whose disease has progressed on other therapies[1][2][4][5][8]. The drug was developed by Ignyta (acquired by Roche) and is marketed under the brand name Rozlytrek.

Brand names
Rozlytrek
02

Targets

TNK2 (Activated Cdc42-associated kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)

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