Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor. It was approved by the FDA in August 2019... It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors.
- Mechanism
- Curator reviewed · 6 references
Entrectinib is a tyrosine kinase inhibitor which acts on several receptors. It functions as an ATP competitor to inhibit tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, TRKC, as well as proto-oncogene tyrosine-protein kinase ROS1 and anaplastic lymphoma kinase (ALK). TRK receptors produce cell proliferation via downstream signalling through the mitogen activated protein kinase, phosphoinositide 3-kinase, and phospholipase C-γ. ALK produces similar signalling with the addition of downstream JAK/STAT activation. Inhibition of these pathways suppresses cancer cell proliferation and shifts the balance in favor of apoptosis resulting in shrinking of tumor volume.
- Primary indication
- Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults.Curator reviewed · 10 structured indications
- Formula / weight
- C31H34F2N6O2 · 560.65 g/mol (avg)
- First approval
- Canada, 2020 · United States, 2019 · European Union, 2024
- Also known as
- N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
- Code names
- RO7102122 · RXDX-101
- Brand names
Resolves to
HAYYBYPASCDWEQ-UHFFFAOYSA-NSMILESCN1CCN(CC1)C1=CC=C(C(=O)NC2=NNC3=CC=C(CC4=CC(F)=CC(F)=C4)C=C23)C(NC2CCOCC2)=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Entrectinib, and which of those have an active Phase 3 trial?
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