Treatment of locally advanced or metastatic(ALK- positive) non-small cell lung cancer (NSCLC)
#仿單變更2021

Crizotinib is a kinase inhibitor, including anaplastic lymphoma kinase (ALK). In ALK-positive patients with non-small cell lung cancer, this inhibition prevents the expression of oncogenic fusion proteins from activating gene expression, which subsequently impairs cell proliferation and survival of these proteins in tumors.

Oral bioavailability: 43%( range: 32% to 66%); Protein binding: 91%; Crizotinib is extensively metabolized in the liver predominantly by CYP3A4/5; Excretion: Feces (63%; 53% as unchanged drug); urine (22%; 2% as unchanged drug); Elimination half-life: 42 hours.

Hypersensitivity to crizotinib or any component of the formulation; congenital long QT syndrome or with persistent Fridericia-corrected QT interval (QTcF) ≧500 msec. (Canadian labeling)

1. Category D (All Trimesters) Rating Fetal risk cannot be ruled out.
2. Pregnancy should be avoided while under medication. <20221129>

Excretion in breast milk unknown/not recommended

Vision disorder (began within 2 weeks of treatment initiation), edema, nausea, diarrhea, vomiting, constipation, AST/ALT increased, appetite decreased, neuropathy, pulmonary embolism <20210304>, lymphocytopenia (48% to 51%; grades 3/4: 7% to 9%), neutropenia (49% to 52%; grades 3/4: 11% to 12%) <20221129>

Oral: 250 mg twice daily. If dose reduction is necessary, reduce dose to 200 mg orally twice daily; if necessary, further reduce to 250 mg once daily. Crizotinib can be administered with or without food.