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Release date: 2026-01-26 17:54:09 Recommended: 17
Lorlatinib is a third-generation targeted therapy indicated for ALK-positive metastatic non-small cell lung cancer (NSCLC), primarily used in patients who have developed resistance to or experienced disease progression following treatment with other ALK inhibitors.
It blocks cancer cell growth by inhibiting the activity of abnormal ALK proteins. Common adverse reactions include edema, neuropathy, and weight gain. Dosage adjustment should be made based on individual conditions, and the drug is contraindicated in patients hypersensitive to any of its components.
Indications
Lorlatinib is indicated for patients with ALK-positive metastatic non-small cell lung cancer, particularly those who have experienced disease progression or developed resistance after treatment with first-generation or second-generation ALK inhibitors such as crizotinib.
Mechanism of Action
As a third-generation dual ALK/ROS1 inhibitor, lorlatinib can cross the blood-brain barrier, exerting efficacy against brain metastases, and inhibit various ALK resistance mutations (e.g., G1202R, L1196M).
Standard Dosage
The recommended standard dose is 100 mg orally once daily, which can be taken with or without food.
Dosage Adjustment
In case of grade 3 or higher adverse reactions (e.g., elevated liver enzymes, interstitial lung disease), treatment should be suspended until symptoms resolve, after which the dose may be reduced to 75 mg or 50 mg orally once daily.
Frequently Occurring Adverse Reactions
Edema (facial and extremities): May be alleviated with diuretics or dosage adjustment.
Neurological reactions: Such as dizziness and paresthesia. Patients should avoid driving or operating machinery.
Metabolic abnormalities: Including hypercholesterolemia and hyperglycemia. Regular monitoring and dietary control are required.
Severe Adverse Reactions
Interstitial lung disease/pneumonitis: Discontinue treatment immediately and seek medical attention.
Cardiotoxicity (QT interval prolongation): Regular electrocardiogram monitoring is necessary.
Contraindicated Populations
Patients hypersensitive to any component of lorlatinib.
Patients with uncontrolled severe cardiovascular diseases.
Drug Interactions
Avoid co-administration with potent CYP3A inducers (e.g., rifampicin) or inhibitors (e.g., ketoconazole), as these may affect drug efficacy or increase toxicity.
Pregnant women: Strict contraception is required due to the drug's fetal toxicity.
Lactating women: Use of the drug is prohibited during breastfeeding.
Pediatric patients: The safety and efficacy of lorlatinib in children have not been established.
Storage Conditions
Store below 30℃ in a light-protected place, and keep the original packaging sealed to protect from moisture.
Missed Dose Management
If a dose is missed by more than 4 hours, skip the missed dose and do not double the next dose.
Monitoring Requirements
Routine monitoring of liver function, blood lipids, blood glucose, and electrocardiogram is required before and during treatment.
Clinical studies have demonstrated that lorlatinib achieves an objective response rate (ORR) of 50%-60% in patients with brain metastases, with a median progression-free survival (PFS) of approximately 9-12 months. Patients should maintain close communication with healthcare providers, report adverse reactions promptly, and refrain from adjusting the treatment regimen without medical guidance.
