Detailed Chinese usage guide for Lorlatinib/Lorlatinib

1. Brief description of drugs

Lorlatinib, also known as lorlatinib, is a treatment for adults with metastatic non-small cell lung cancer (NSCLC), specifically those whose tumors are confirmed to be anaplastic lymphoma kinase (ALK) positive by an FDA-approved test.

2. Treatment objects

This drug is mainly used to treat adult patients with metastatic non-small cell lung cancer, and their tumors must be confirmed by testingALK positivity.

3. Usage and dosage

1) Pre-treatment evaluation: Based on the positive test result of ALK in the tumor sample, the doctor will decide whether to treat with lorlatinib.

2) Recommended dosage: Patients are usually recommended to take 100mg of lorlatinib every day, which can be taken with food or alone, until the disease progresses or signs of drug intolerance appear. This medicine is in tablet form and should be swallowed whole at the same time each day and avoid chewing, crushing or splitting the tablet. Do not take if tablet is broken. If you miss a dose, you should take it as soon as possible, unless it is less than 4 hours before the next dose. If you vomit after taking the medicine, there is no need to take more medicine. Just wait for the next normal time to take the medicine.

3) Dose adjustment: If the patient experiences adverse reactions during treatment, the doctor will adjust the dose according to the situation. It can be reduced to 75mg per day for the first time and to 50mg again. If the patient still cannot tolerate a dose of 50 mg, the drug should be permanently discontinued.

When used concomitantly with moderateCYP3A inducers, the dose of lorlatinib should be increased to 125 mg; if used concomitantly with strong CYP3A inhibitors, the starting dose should be reduced to 75 mg.

Lorlatinib should not be used in patients taking strongCYP3A inducers.

In patients with severely impaired renal function (creatinine clearance15-<30mL/min), the daily dose should be reduced to 75 mg.

4. Possible adverse reactions

Common adverse reactions include edema, peripheral neuropathy, weight gain, cognitive impairment, fatigue, dyspnea, joint pain, diarrhea, etc. Common adverse reactions in laboratory tests include high cholesterol and hypertriglyceridemia.

5. Drug supply and storage

Larlatinib is available as 25 mg or 100 mg tablets and is recommended for storage at 20°C to 25°C, with an allowed temperature deviation range of 15°C to 30°C.

6. Taboos

Due to the potential for severe hepatotoxicity, lorlatinib should not be used in patients taking strong CYP3A inducers.

7. Drug action mechanism

Lorlatinib is a kinase inhibitor that can effectively inhibitALK, ROS1 and other kinases. It also shows activity against a variety of ALK enzyme mutant forms in in vitro experiments, including some mutations that are resistant to crizotinib and other ALK inhibitors.

8. Usage recommendations for special patient groups

1) Pregnant women: According to animal experiments and drug action mechanism, lorlatinib may cause damage to the fetus. It is recommended that women of childbearing potential use non-hormonal contraceptive methods during treatment and for at least 6 months after stopping treatment, and to avoid breastfeeding during treatment and for 7 days after stopping treatment.

2) Male patients: Animal experiments show that lorlatinib may temporarily affect male fertility. Therefore, it is recommended that male patients with sexual partners take effective contraceptive measures during treatment and for at least 3 months after discontinuation of treatment.