drug_type
RELEVANT_DRUG
intervention_type
Small-molecule TKI
drug_description
Small-molecule tyrosine kinase inhibitor targeting ROS1 (also active against NTRK).
nci_thesaurus_concept_id
C114984
nci_thesaurus_definition
An orally bioavailable inhibitor of the tyrosine kinases tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon administration, entrectinib binds to and inhibits TrkA, TrkB, TrkC, ROS1 and ALK. Inhibition of these kinases may result in a disruption of TrkA-, TrkB-, TrkC-, ROS1-, and ALK-mediated signaling. This leads to an induction of apoptosis and an inhibition of tumor cell proliferation in tumor cells that express these kinases. TrkA, TrkB, TrkC, ROS1 and ALK are overexpressed in a variety of cancer cell types.
drug_mesh_term
Entrectinib
drug_category
SMALL MOLECULE DRUG
drug_class
Inhibitor
drug_delivery_route
Oral
drug_mechanism_of_action
Orally bioavailable tyrosine kinase inhibitor that binds the ATP sites of TRK A/B/C (NTRK1/2/3), ROS1, and ALK, blocking kinase phosphorylation and downstream signaling (e.g., MAPK/PI3K pathways), leading to growth inhibition and apoptosis in tumors driven by these fusions/activations.
drug_name
Entrectinib
nct_id_drug_ref
NCT05845671