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Lorlatinib is a third-generation anaplastic lymphoma kinase (ALK) and ROS1 tyrosine kinase inhibitor. It has a significant inhibitory effect on a variety of ALK resistance mutations (such as G1202R, I1171T, etc.), and can penetrate the blood-brain barrier to effectively control metastatic lesions in the central nervous system.
1. Generic name : Lorlatinib (Lorlatinib)
2. Trade name :LORBRENA®
3. Dosage form : Film-coated tablets
4. Main ingredients : Each tablet contains lorlatinib 25mg or 100mg, excipients include microcrystalline cellulose, anhydrous calcium hydrogen phosphate, sodium carboxymethyl starch, magnesium stearate, etc.
ALK-positive metastatic non-small cell lung cancer (NSCLC) : For the treatment of patients with disease progression after treatment with crizotinib and at least one other ALK inhibitor, or as an option after failure of alectinib or ceritinib as the first ALK inhibitor. This indication is approved under accelerated approval based on tumor response rate and response duration, and further verification of clinical benefit is required.
1. Specifications of : 25mg, 100mg.
2. Characteristics : Film-coated tablets with smooth surface and white to off-white powder content.
1. Recommended dose : 100 mg orally, once a day, with food or on an empty stomach.
2. How to take : Swallow the tablet whole, do not chew, crush or break it. If you miss a dose, you can take it again if it is >4 hours before the next dose. There is no need to take it after vomiting.
1. Adverse reaction adjustment : Reduce the dose to 75 mg once a day for the first time, and to 50 mg once a day for the second time. If the drug is not tolerated, discontinue the drug permanently.
2. Hepatic insufficiency : For patients with moderate to severe hepatic insufficiency, the starting dose is halved.
3. Drug interaction : When combined with a strong CYP3A inhibitor, the dose is reduced to 75 mg once a day, and it is contraindicated when used in combination with a strong CYP3A inducer.
1. Central nervous system reaction : 54% of patients experience cognitive impairment, mood changes or hallucinations and need to avoid driving or operating machinery.
2. Hepatotoxicity monitoring : Monitor ALT/AST every 2 weeks in the first month of treatment, and then change to monthly monitoring.
3. Drug interaction : It is prohibited to use strong CYP3A inducers (such as rifampicin) in combination with moderate CYP3A inducers or sensitive CYP3A substrates.
1. Pregnant women: : Disabled (animal experiments show teratogenicity).
2. Lactation : Breastfeeding is prohibited during treatment and within 7 days after the last dose.
3. Children : Safety has not been established.
4. U200c for the elderly: No need to adjust the dosage.
1. Common (≥20%) : Edema (57%), peripheral neuropathy (47%), cognitive impairment (27%), dyspnea (27%), fatigue (26%), weight gain (24%), joint pain (23%), mood disorders (23%), diarrhea (22%).
2. Severe reactions :ILD/pneumonia (1.5%), grade 3-4 ALT/AST elevation (2.1%), complete atrioventricular block (0.3%).
Combined use of strong CYP3A inducers (such as rifampicin, phenytoin).
1. Strong CYP3A inhibitor (such as ketoconazole): Increase the plasma concentration of lorlatinib and need to reduce the dose.
2. CYP3A substrate (such as midazolam): Reduce its efficacy and avoid combined use.
1. Store in original packaging, away from light and moisture.
2. Storage temperature: 20-25°C (short-term fluctuation of 15-30°C is allowed).
Note : During treatment, electrocardiogram, blood lipids and neurological symptoms need to be monitored regularly. Avoid use with grapefruit or St. John's wort.