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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
2. Trade name: LORBRENA®
Lorlatinib is suitable for the treatment of anaplastic lymphoma kinase (ALK)-positive metastasis. Patients with metastatic non-small cell lung cancer (NSCLC) whose disease has progressed under the following conditions:
1. Previously received crizotinib and at least one other ALK inhibitor treatment;
2. Or previously received alectinib as the first ALK inhibitor treatment;
3. Or previously received ceritinib as the first ALK inhibitor treatment.
This indication received accelerated approval based on tumor response rate and response duration, and subsequent confirmatory clinical trials may be required to verify its clinical effectiveness.
Lolatinib tablets are available in two specifications:
1. 25mg: Film-coated tablets
2. 100mg: Film-coated tablets
1. Each tablet contains 25mg or 100mg of lorlatinib.
2. Excipients include: microcrystalline cellulose, anhydrous calcium hydrogen phosphate, hydroxypropyl starch, magnesium stearate, etc.
3. Film coating contains: hypromellose, lactose, polyethylene glycol 3350, triacetin, titanium dioxide, iron oxide, etc.
1. The recommended dose is 100 mg orally once a day, which can be taken with food or on an empty stomach;
2. The tablet should be swallowed whole and should not be chewed, crushed or divided. Cut;
3. Take the medicine at roughly the same time every day. If you miss a dose and it is more than 4 hours before the next dose, you can take it again, otherwise skip;
4. If you vomit after taking the medicine, you should not take the next dose as originally planned.
Adjust the dose according to the severity of adverse reactions:
1. The first reduction: 75 mg once a day;
2. The second reduction: 50 mg once a day;
3. If 50 mg is still intolerable, discontinue the drug permanently.
Specific adjustments are based on the severity of adverse reactions such as central nervous system reactions, hyperlipidemia, atrioventricular block, and interstitial lung disease.
1. Avoid combined use with potent CYP3A inducers, otherwise severe liver toxicity may occur;
2. Central nervous system symptoms (such as cognitive impairment, mood changes, hallucinations, epilepsy, etc.) may occur during medication, and close monitoring is required;
3. Blood lipids need to be tested regularly level, and start or adjust lipid-lowering drugs if necessary;
4. Monitor electrocardiogram and pay attention to the risk of atrioventricular block;
5. If respiratory symptoms occur, you should be alert to interstitial lung disease/pneumonia, and you need to stop taking the drug and evaluate it immediately;
6. Men and women of childbearing age need to take effective non-hormonal contraceptive measures, because this product may make hormonal contraceptives ineffective.
1. Pregnant women: It may cause fetal damage, and it is necessary to confirm that you are not pregnant before taking the medication;
2. Lactation: Breastfeeding is prohibited during medication and within 7 days after the last dose. Breast;
3. Elderly people: Limited data show no significant difference from young patients;
4. Liver and renal insufficiency: There is no need to adjust the dosage for patients with mild to moderate liver and renal dysfunction, and there is insufficient data on medication for severe patients.
Common adverse reactions (incidence rate ≥20%) include: Edema, peripheral neuropathy, cognitive effects, dyspnea, fatigue, weight gain, joint pain, mood changes, diarrhea, etc.
Laboratory abnormalities include hypercholesterolemia, hypertriglyceridemia, anemia, hyperglycemia, elevated transaminases, etc.
It is prohibited to use this product in combination with strong CYP3A inducers.
1. Avoid combination with moderate CYP3A inducers;
2. Avoid combination with strong CYP3A inhibitors. If combination is necessary, the dose of lorlatinib needs to be adjusted;
3. Avoid combination with CYP3A substrate drugs, as their efficacy may be reduced.
Store at 20°C to 25°C (68°F to 77°F), short-term storage allowed between 15°C to 30°C (59°F to 86°F).