Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors.
Article Details
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Liu D, Offin M, Harnicar S, Li BT, Drilon A
Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors.
Ther Clin Risk Manag. 2018 Jul 20;14:1247-1252. doi: 10.2147/TCRM.S147381. eCollection 2018.
- PubMed ID
- 30050303 [ View in PubMed]
- Abstract
Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naive patients along with substantial intracranial activity. In ROS1-rearranged lung cancers, entrectinib results in durable disease control and prolonged progression-free survival. The drug is well tolerated and has a safety profile that includes adverse events mediated by on-target tropomyosin-related kinase A/B/C inhibition.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Entrectinib BDNF/NT-3 growth factors receptor Protein Humans UnknownInhibitorDetails Entrectinib High affinity nerve growth factor receptor Protein Humans YesInhibitorDetails Entrectinib NT-3 growth factor receptor Protein Humans YesInhibitorDetails Entrectinib Proto-oncogene tyrosine-protein kinase ROS Protein Humans YesInhibitorDetails - Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Entrectinib Cytochrome P450 3A4 Protein Humans UnknownSubstrateDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareEntrectinibPhenytoin The metabolism of Entrectinib can be increased when combined with Phenytoin. EntrectinibPentobarbital The metabolism of Entrectinib can be increased when combined with Pentobarbital. EntrectinibCarbamazepine The metabolism of Entrectinib can be increased when combined with Carbamazepine. EntrectinibMitotane The metabolism of Entrectinib can be increased when combined with Mitotane. EntrectinibPrimidone The metabolism of Entrectinib can be increased when combined with Primidone.