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entrectinib (Rozlytrek)
Indications:
- ROS1-positive metastatic non-small cell lung cancer (NSCLC)
- solid tumors with neurotrophic tyrosine receptor kinase (NTRK) gene fusion
- orphan drug designation for treatment of neuroblastoma
- orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, ROS1- & ALK-positive non-small cell lung cancer (NSCLC) & metastatic colorectal cancer
Dosage:
- 600 mg PO QD
Tabs: 100 mg, 200 mg
Adverse effects:
- most common (>= 20%):
- fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, visual impairment
- serious:
- congestive heart failure, central nervous system dysfunction, bone fractures, hepatotoxicity, hyperuricemia, QT prolongation, visual impairment
Mechanism of action:
- ALK inhibitor
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid= 25141092
References
- RxNorm
- Wikipedia: Entrectinib
https://en.wikipedia.org/wiki/Entrectinib
- FDA News Release. Aug 15, 2019.
FDA approves entrectinib for NTRK solid tumors and ROS-1 NSCLC
https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-entrectinib-ntrk-solid-tumors-and-ros-1-nsclc
- Highlight of Prescribing Information
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212725s000lbl.pdf