Xalkori

Crizotinib

Advanced NSCLC whose tumors are anaphylastic lymphoma kinase (ALK) or ROS1 +ve.

250 mg bd until disease progression or intolerance. 1st dose reduction: 200 mg bd. 2nd dose reduction: 250 mg once daily. Preexisting moderate hepatic impairment 200 mg bd. Concomitant use w/ strong CYP3A inhibitor, preexisting severe hepatic impairment, severe renal impairment not requiring dialysis 250 mg once daily.

May be taken with or without food: Swallow whole, do not crush/chew/open cap.

Hypersensitivity.

Discontinue use in patients w/ new onset of severe visual loss; treatment-related pneumonitis. Avoid use in patients w/ congenital long QT syndrome. Cardiac failure; symptomatic bradycardia; drug-induced hepatotoxicity; ILD/pneumonitis. Monitor ECG & electrolytes in patients w/ CHF, bradyarrhythmias, electrolyte abnormalities or taking medications prolonging QT interval. Regularly monitor heart rate & BP. Monitor LFT including ALT, AST & total bilirubin every 2 wk during 1st 2 mth of treatment then once mthly; signs & symptoms of heart failure. Avoid concomitant use w/ drugs causing bradycardia eg, β-blockers, non-dihydropyridine Ca-channel blockers, clonidine, digoxin. Hepatic & severe renal impairment. May impair fertility. Women of childbearing potential should use effective contraception during & for 90 days after last dose. Not to be used during pregnancy & lactation. Ped patients. Elderly ≥65 yr.

Bradycardia, QT prolongation; vision disorder; diarrhea, vomiting, nausea, constipation, abdominal pain, dyspepsia, dysphagia, esophagitis; pulmonary embolism, edema, pyrexia; upper resp infection; increased/decreased wt; pain in extremity, muscle spasm; dysgeusia, headache, dizziness, syncope, fatigue; decreased appetite, neuropathy; rash; ILD; renal cyst; syncope; esophagitis; hepatic failure; decreased blood testosterone; dyspnea; elevated transaminases, neutropenia, lymphopenia, hypokalemia, hypophosphatemia, increased blood creatine phosphokinase.

Increased plasma conc w/ strong CYP3A inhibitors; grapefruit or grapefruit juice. Decreased plasma conc w/ strong CYP3A inducers. Avoid concomitant use w/ CYP3A substrates, drugs prolonging QT interval & causing bradycardia. Moderate CYP3A inhibitors.

Targeted Cancer Therapy

L01ED01 - crizotinib ; Belongs to the class of anaplastic lymphoma kinase (ALK) inhibitors. Used in the treatment of cancer.

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