Lorlatinib (Lorviqua) is a third-generation ALK inhibitor that provides an important treatment option for patients with ALK-positive non-small cell lung cancer (NSCLC).

Dosage and Administration, Recommended Dose of Lorlatinib (Lorviqua)

Dosage and Administration

(1) Lorlatinib is indicated for adult patients with ALK-positive metastatic non-small cell lung cancer confirmed by an FDA-approved testing method.

(2) Its standard treatment regimen is 100 mg orally once daily, which can be taken with or without food.

(3) The tablets must be swallowed whole; chewing, crushing, or splitting the tablets is prohibited.

(4) If a tablet is found to be broken, cracked, or incomplete, it should not be taken.

Medication Precautions

(1) In terms of medication timing management, it is recommended to take the drug at a fixed time every day.

(2) If a dose is missed, it should be taken as soon as it is remembered, unless less than 4 hours remain before the next scheduled dose, in which case the missed dose should be skipped.

(3) If vomiting occurs after taking the medication, no supplementary dose is needed, and the next dose should be taken as originally scheduled.

(4) It should be noted that strong CYP3A inducers are contraindicated with lorlatinib. Before starting lorlatinib treatment, it is necessary to ensure that strong CYP3A inducers have been discontinued for more than 3 plasma half-lives of the inducing drug.

Dose Adjustment of Lorlatinib (Lorviqua)

Adjustment Based on Adverse Reactions

(1) Central Nervous System Effects: For Grade 1 reactions, the original dose can be maintained or the drug can be suspended until recovery to baseline before resuming. For Grade 2-3 reactions, the drug should be suspended until recovery to Grade 0-1 before resuming at a reduced dose. For Grade 4 reactions, permanent discontinuation is required.

(2) Hyperlipidemia: When Grade 4 hypercholesterolemia or hypertriglyceridemia occurs, the drug should be suspended until it returns to ≤ Grade 2 before resuming at the original dose. If severe hyperlipidemia recurs, dose reduction is needed for maintenance.

Management of Specific Organ Toxicities

(1) Atrioventricular (AV) Block: For second-degree AV block, the drug should be suspended until the PR interval is <200ms before resuming at a reduced dose. For the first occurrence of complete AV block, a pacemaker should be implanted or the drug should be suspended until the PR interval returns to normal before resuming at a reduced dose.

(2) Interstitial Lung Disease (ILD)/Pneumonitis: Any grade of treatment-related ILD/pneumonitis requires permanent discontinuation of the drug.

(3) Hypertension: For Grade 3 hypertension, the drug should be suspended until it returns to Grade 1 or below before resuming at the original dose. If Grade 3 hypertension recurs or Grade 4 hypertension occurs, dose reduction or permanent discontinuation is required.

Use of Lorlatinib (Lorviqua) in Special Populations

Patients with Hepatic or Renal Impairment

Patients with severe renal impairment require dose adjustment, and it is recommended to reduce the dose from 100 mg to 75 mg once daily.

Reproductive and Pregnant Populations

(1) Based on its teratogenic mechanism, use in pregnant women poses a risk to the fetus.

(2) Women of childbearing potential are advised to use effective non-hormonal contraceptive measures during treatment and for at least 6 months after the last dose.

(3) Male patients are advised to take effective contraceptive measures during treatment and for 3 months after the last dose.