Contraindicated in:
Use Cautiously in:
CV: edema, hypertension.
Derm: alopecia, hair color changes, rash.
EENT: ↑tear production.
Endo: hyperthyroidism, hypothyroidism.
F and E: hypokalemia, hypomagnesemia, hyponatremia, hypophosphatemia.
GI: abdominal pain, constipation, diarrhea, dyspepsia, hyperbilirubinemia, hypoalbuminemia, ↑liver enzymes, nausea, vomiting, GI BLEEDING.
GU: acute kidney injury, ↓ fertility.
Hemat: anemia, leukopenia, neutropenia, thrombocytopenia.
Neuro: cognitive impairment, dizziness, headache, mood disorders, sleep disorders, taste disturbances, hallucinations, INTRACRANIAL HEMORRHAGE, speech disorders.
Resp: dyspnea, pleural effusion.
Drug-Drug:
Gastrointestinal Stromal Tumor Harboring PDGFRA Exon 18 Mutations
Advanced Systemic Mastocytosis
Therapeutic Classification: antineoplastics
Pharmacologic Classification: kinase inhibitors, platelet-derived growth factor receptor alpha blockers
Absorption: Extent of absorption increased with high-fat meals.
Distribution: Extensively distributed to tissues.
Metabolism/Excretion: Primarily metabolized by the liver via CYP3A4 isoenzyme (and CYP2C9 to a lesser extent). Primarily excreted in feces (70%; 11% as unchanged drug); 18% excreted in urine (primarily as metabolites).
Half-life: 3257 hr.