Medically reviewed by Drugs.com. Last updated on Sep 22, 2020.
Applies to the following strengths: 25 mg; 100 mg
Usual Adult Dose for:
Additional dosage information:
Usual Adult Dose for Non-Small Cell Lung Cancer
100 mg orally once a day until disease progression or unacceptable toxicity
Use: For the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on crizotinib and at least one other ALK inhibitor for metastatic disease OR alectinib as the first ALK inhibitor therapy for metastatic disease
OR ceritinib as the first ALK inhibitor therapy for metastatic disease.
Renal Dose Adjustments
-Mild or moderate renal impairment (CrCl 30 to 89 mL/min): No adjustment recommended.
-Severe renal impairment (CrCl less than 30 mL/min): Data not available
Liver Dose Adjustments
-Mild hepatic impairment (total bilirubin less than or equal to upper limit of normal (ULN) with AST greater than ULN or total bilirubin greater than 1 to 1.5 x ULN with any AST): No adjustment recommended.
-Moderate or severe hepatic impairment: Data not available
Dose Modifications for Adverse Reactions:
-First dose reduction: 75 orally once a day
-Second dose reduction: 50 mg orally once a day
-Permanently discontinue therapy in patients who are unable to tolerate 50 mg orally once daily.
Central Nervous System Adverse Effects:
-Grade 1: Continue at same dose or withhold the dose until recovery to baseline; resume at the same dose or at reduced dose.
-Grade 2 or 3: Withhold dose until recovery to Grade 0 or 1; resume at reduced dose.
-Grade 4: Permanently discontinue therapy.
Grade 4 hypercholesterolemia OR Grade 4 hypertriglyceridemia: Withhold until recovery to Grade 2 or less; resume at same dose. If severe hypercholesterolemia and/or hypertriglyceridemia recurs, resume at reduced dose.
Atrioventricular (AV) Block:
-Second-degree AV block: Withhold until PR interval is less than 200 ms; resume at reduced dose.
-First occurrence of complete AV block: Withhold until pacemaker placed OR PR interval is less than 200 ms; if a pacemaker is placed, resume at same dose; if no pacemaker is placed, resume at reduced dose.
-Recurrent complete AV block: Place pacemaker or permanently discontinue this drug.
Interstitial Lung Disease (ILD)/Pneumonitis:
-Any Grade treatment-related ILD/pneumonitis: Permanently discontinue this drug.
Other Adverse Reactions:
-Grade 1 or 2: Continue at same or reduced dose.
-Grade 3 or 4: Withhold until symptoms resolve to Grade 2 or less or baseline; resume at reduced dose.
Concomitant Use of Strong or Moderate CYP450 3A Inducers:
-This drug is contraindicated in patients taking strong CYP450 3A inducers. Discontinue strong CYP450 3A inducers for 3 plasma half-lives prior to initiating this drug.
-Avoid concomitant use of this drug with moderate CYP450 3A inducers.
Dose Modification for Strong CYP450 3A Inhibitors:
-Avoid concomitant use of this drug with strong CYP450 3A inhibitors. If concomitant use with a strong CYP450 3A inhibitor cannot be avoided, reduce the starting dose of this drug from 100 mg once a day to 75 mg orally once a day.
-In patients who have had a reduction to 75 mg orally once a day due to adverse reactions and who initiate a strong CYP450 3A inhibitor, reduce the dose of this drug to 50 mg orally once a day.
-If concomitant use of a strong CYP450 3A inhibitor is discontinued, increase the dose of this drug (after 3 plasma half-lives of the strong CYP450 3A inhibitor) to the dose that was used before starting the strong inhibitor.
-Concomitant administration with strong CYP450 3A inducers because of the potential for serious hepatotoxicity
Safety and efficacy have not been established in patients younger than 18 years.
Consult WARNINGS section for additional precautions.
Data not available
-This drug may be taken with or without food.
-Swallow tablets whole, do not chew, crush or split.
-Do not ingest if tablets are broken, cracked, or otherwise not intact.
-If a dose is missed, take the missed dose unless the next dose is due within 4 hours; do not take 2 doses at the same time to make up for a missed dose.
-Do not take an additional dose if vomiting occurs but continue with the next scheduled dose.
-Store at 20C to 25C (68F to 77F); excursions permitted between 15C to 30C (59F to 86F).
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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- Drug class: multikinase inhibitors
Other brands: Lorbrena