Contraindicated in:
Use Cautiously in:
CV: QT INTERVAL PROLONGATION, edema, hypotension, HF, myocarditis, syncope.
Derm: rash.
EENT: blurred vision, cataracts, diplopia, photophobia, visual impairment.
Endo: hyperuricemia.
F and E: hyperkalemia, hypernatremia, hypocalcemia, hypophosphatemia.
GI: HEPATOTOXICITY, abdominal pain, constipation, diarrhea, dysgeusia, dysphagia, hypoalbuminemia, ↑amylase, ↑lipase, ↑liver enzymes, nausea, vomiting.
GU: dehydration, ↑serum creatinine.
Hemat: neutropenia, anemia, lymphopenia.
MS: arthralgia, bone fractures, muscle weakness, myalgia.
Neuro: balance disorder, paresthesia, peripheral neuropathy , ataxia, confusion, dizziness, fatigue, headache, agitation, amnesia, anxiety, aphasia, attention disturbances, cognitive disorders, depression, delirium, hallucinations, insomnia, memory impairment, mental status changes, sedation.
Resp: PULMONARY EMBOLISM, cough, dyspnea, pleural effusion.
Misc: fever.
Drug-Drug:
Drug-Food:
ROS1-Positive Non-Small Cell Lung Cancer
NTRK Gene Fusion-Positive Solid Tumors
Absorption: Well absorbed following oral administration.
Distribution: Extensively distributed to tissues.
Protein Binding: >99%.
Metabolism/Excretion: Primarily metabolized in the liver by the CYP3A4 isoenzyme to an active metabolite (M5). Primarily excreted in feces (36% as unchanged drug, 22% as M5), with minimal excretion in urine (3%).
Half-life: Entrectinib 20 hr; M5 40 hr.
NDC Code*