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    DAE Class; Rx

    Common Brand Names; Lorbrena

    • Antineoplastics, Anaplastic Lymphoma Kinase Inhibitors

    Kinase inhibitor
    Used for certain types of metastatic NSCLC
    Risk of serious hepatotoxicity when administered with CYP3A inducers; contraindicated with strong CYP3A inducers

    Indicated for metastatic non-small cell lung cancer (NSCLC) in patients whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test

    Coadministration with strong CYP3A inducers due to potential for serious hepatotoxicity


    Dyspnea (27%)

    Fatigue (26%)

    Weight gain (24%)

    Increased lipase (24%)

    Increased alkaline phosphatase (24%)

    Thrombocytopenia (23%)

    Arthralgia (23%)

    Mood effects (23%)

    Diarrhea (22%)

    Increased amylase (22%)

    Lymphopenia (22%)

    Hyperkalemia (21%)

    Hypomagnesemia (21%)

    Headache (18%)

    Cough (18%)

    Nausea (18%)

    Myalgia (17%)

    Dizziness (16%)

    Vision disorder (15%)

    Constipation (15%)

    Rash (14%)

    Back pain (13%)

    Pain in extremity (13%)

    Vomiting (12%)

    Speech effects (12%)

    Pyrexia (12%)

    Upper respiratory tract infection (12%)

    Grades 3 or 4

    • Hypercholesterolemia (18%)
    • Hypertriglyceridemia (18%)

    1-10% (All Grades)

    Sleep effects (10%)

    Hallucinations (7%)

    Pneumonia (3.4%)

    Dyspnea (2.7%)

    Pyrexia (2%)

    Mental status changes (1.4%)

    Respiratory failure (1.4%)

    1-10% (Grades 3 or 4)

    Dyspnea (5.4%)

    Hyperglycemia (5%)

    Hypophosphatemia (4.8%)

    Anemia (4.8%)

    Increased amylase (3.9%)

    Lymphopenia (3.4%)

    Peripheral neuropathy (2.7%)

    Increased AST/ALT (2.1%)

    Cognitive effects (2%)

    Mood effects (1.7%)

    Vomiting (1%)

    Increased alkaline phosphatase (1%)

    Hypokalemia (1%)

    Hypoalbuminemia (1%)

    <1% (Grades 3 or 4)

    Vision disorder





    Speech effects



    Back pain

    Pain in extremity





    Increased serum cholesterol and triglycerides may occur; initiate or increase dose of lipid-lowering agents in patients with hyperlipidemia; monitor serum cholesterol and triglycerides; withhold and resume at same dose for first occurrence; resume at same or a reduced dose for recurrence based on severity

    PR interval prolongation and AV block reported; monitor ECG before initiating treatment and periodically thereafter; withhold and resume at reduced dose or at same dose in patients who undergo pacemaker placement; permanently discontinue for recurrence in patients without a pacemaker

    Severe or life-threatening pulmonary adverse reactions consistent with ILD/pneumonitis can occur; promptly investigate for ILD/pneumonitis in any patient who presents with worsening of respiratory symptoms indicative of ILD/pneumonitis (eg, dyspnea, cough, and fever); immediately withhold drug in patients with suspected ILD/pneumonitis; permanently discontinue therapy for treatment-related ILD/pneumonitis of any severity

    Hypertension reported; median time to onset was 6.4 months (1 day to 2.8 years), and 2.3% of patients temporarily discontinued for hypertension; control blood pressure before initiating; monitor blood pressure after 2 weeks and at least monthly thereafter during treatment; withhold and resume at reduced dose or permanently discontinue drug based on severity

    Hyperglycemia can occur; median time to onset of hyperglycemia was 4.8 months (1 day to 2.9 years), and 0.8% of patients temporarily discontinued for hyperglycemia; assess fasting serum glucose prior to initiating and monitor periodically thereafter; withhold and resume at reduced dose or permanently discontinue based on severity

    Fetal harm may occur


    Based on findings from animal studies and its mechanism of action, embryo-fetal harm may occur when administered to a pregnant woman

    No available data on use in pregnant women

    Advise pregnant women of the potential risk to fetus

    Verify pregnancy status in females of reproductive potential before initiating treatment


    No data on presence of lorlatinib or its metabolites in either human or animal milk or its effects on the breastfed infant or on milk production

    Because of potential for serious adverse reactions in breastfed infants, instruct women not to breastfeed during treatment and for 7 days after final dose


    100 mg PO once daily.


    100 mg PO once daily.


    Safety and efficacy not established.


    Safety and efficacy not established.


    Safety and efficacy not established.


    Safety and efficacy not established.



    • 25mg
    • 100mg