LORBRENA® Highlights

(lorlatinib)

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use LORBRENA safely and effectively. See full prescribing information for LORBRENA.

LORBRENA (lorlatinib) tablets, for oral use
Initial U.S. Approval: 2018

INDICATIONS AND USAGE

LORBRENA is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. (1, 2.1)

DOSAGE AND ADMINISTRATION

Recommended dosage: 100 mg orally once daily. (2.2)

Severe Renal Impairment: 75 mg orally once daily. (2.8, 8.7, 12.3)

DOSAGE FORMS AND STRENGTHS

Tablets: 25 mg or 100 mg. (3)

CONTRAINDICATIONS

Concomitant use with strong CYP3A inducers. (4)

WARNINGS AND PRECAUTIONS

•
Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers: Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA. (2.4, 5.1)
•
Central Nervous System (CNS) Effects: CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity. (2.3, 5.2)
•
Hyperlipidemia: Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity. (2.3, 5.3)
•
Atrioventricular Block: Withhold and resume LORBRENA at same or reduced dose based on severity. (2.3, 5.4)
•
Interstitial Lung Disease/Pneumonitis: Immediately withhold LORBRENA in patients with suspected ILD/pneumonitis. Permanently discontinue LORBRENA for treatment-related ILD/pneumonitis of any severity. (2.3, 5.5)
•
Hypertension: Monitor blood pressure after 2 weeks and then at least monthly during treatment. For severe hypertension, withhold LORBRENA, then dose reduce or permanently discontinue. (2.3, 5.6)
•
Hyperglycemia: Assess fasting serum glucose prior to starting LORBRENA and regularly during treatment. If not adequately controlled with optimal medical management, withhold LORBRENA, then consider dose reduction or permanently discontinue, based on severity. (2.3, 5.7)
•
Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus. Advise males and females of reproductive potential to use an effective non-hormonal method of contraception. (5.8, 7.2, 8.1, 8.3)

ADVERSE REACTIONS

Most common (incidence ≥20%) adverse reactions and Grade 3–4 laboratory abnormalities are edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hypercholesterolemia, hypertriglyceridemia, and cough. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or www.pfizer.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong CYP3A Inducers: Contraindicated. (2.4, 7.1)
•
Moderate CYP3A Inducers: Avoid concomitant use. If coadministration cannot be avoided, increase the LORBRENA dose. (2.5, 7.1)
•
Strong CYP3A Inhibitors: Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. (2.6, 7.1)
•
Fluconazole: Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. (2.7, 7.1)
•
Certain CYP3A Substrates: Avoid concomitant use with CYP3A substrates for which minimal concentration changes may lead to serious therapeutic failures. (7.2)
•
Certain P-gp Substrates: Avoid concomitant use with P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures. (7.2)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 4/2023

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Highlights

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use LORBRENA safely and effectively. See full prescribing information for LORBRENA.

LORBRENA (lorlatinib) tablets, for oral use
Initial U.S. Approval: 2018

INDICATIONS AND USAGE

LORBRENA is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. (1, 2.1)

DOSAGE AND ADMINISTRATION

Recommended dosage: 100 mg orally once daily. (2.2)

Severe Renal Impairment: 75 mg orally once daily. (2.8, 8.7, 12.3)

DOSAGE FORMS AND STRENGTHS

Tablets: 25 mg or 100 mg. (3)

CONTRAINDICATIONS

Concomitant use with strong CYP3A inducers. (4)

WARNINGS AND PRECAUTIONS

•
Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers: Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA. (2.4, 5.1)
•
Central Nervous System (CNS) Effects: CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity. (2.3, 5.2)
•
Hyperlipidemia: Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity. (2.3, 5.3)
•
Atrioventricular Block: Withhold and resume LORBRENA at same or reduced dose based on severity. (2.3, 5.4)
•
Interstitial Lung Disease/Pneumonitis: Immediately withhold LORBRENA in patients with suspected ILD/pneumonitis. Permanently discontinue LORBRENA for treatment-related ILD/pneumonitis of any severity. (2.3, 5.5)
•
Hypertension: Monitor blood pressure after 2 weeks and then at least monthly during treatment. For severe hypertension, withhold LORBRENA, then dose reduce or permanently discontinue. (2.3, 5.6)
•
Hyperglycemia: Assess fasting serum glucose prior to starting LORBRENA and regularly during treatment. If not adequately controlled with optimal medical management, withhold LORBRENA, then consider dose reduction or permanently discontinue, based on severity. (2.3, 5.7)
•
Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus. Advise males and females of reproductive potential to use an effective non-hormonal method of contraception. (5.8, 7.2, 8.1, 8.3)

ADVERSE REACTIONS

Most common (incidence ≥20%) adverse reactions and Grade 3–4 laboratory abnormalities are edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hypercholesterolemia, hypertriglyceridemia, and cough. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or www.pfizer.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong CYP3A Inducers: Contraindicated. (2.4, 7.1)
•
Moderate CYP3A Inducers: Avoid concomitant use. If coadministration cannot be avoided, increase the LORBRENA dose. (2.5, 7.1)
•
Strong CYP3A Inhibitors: Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. (2.6, 7.1)
•
Fluconazole: Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. (2.7, 7.1)
•
Certain CYP3A Substrates: Avoid concomitant use with CYP3A substrates for which minimal concentration changes may lead to serious therapeutic failures. (7.2)
•
Certain P-gp Substrates: Avoid concomitant use with P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures. (7.2)

USE IN SPECIFIC POPULATIONS

Lactation: Advise not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 4/2023
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