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At a glance

Lorlatinib is a kinase inhibitor used for ALK-positive non-small cell lung cancer (NSCLC) that has progressed on crizotinib and at least one other ALK inhibitor, or alectinib or ceritinib.

Indications
  • ALK-positive metastatic non-small cell lung cancer (NSCLC) - progressed on crizotinib and at least one other ALK inhibitor, or alectinib or ceritinib
Pharmacology

Lorlatinib inhibits ALK and ROS1 kinases, disrupting ALK- and ROS1-mediated signaling and inhibiting tumor cell growth in ALK- and ROS1-overexpressing tumor cells.

Dosage

Adult Dose (Oral):

  • 100 mg once daily
  • With or without food
  • Continue until disease progression or unacceptable toxicity
  • First dose reduction: 75 mg/day; Second dose reduction: 50 mg/day

Hepatic Impairment: Mild: no dose adjustment; Moderate-severe: recommended dose not established

Side effects

Common Side Effects (>10%):

  • Hypercholesterolemia (96%)
  • Hypertriglyceridemia (90%)
  • Edema (57%)
  • Hyperglycemia (52%)
  • Anemia (52%)
  • Peripheral neuropathy (47%)
  • Increased AST (37%), ALT (28%)
  • Cognitive effects (27%)
  • Dyspnea (27%)
  • Fatigue (26%)
  • Weight gain (24%)
  • Mood effects (23%)
Use in pregnancy

Use in Pregnancy: Embryo-fetal harm may occur when administered to a pregnant woman. Females of reproductive potential should use effective non-hormonal contraception during treatment and for 6 months after the final dose.

Precautions & warnings
  • Severe hepatotoxicity occurred with strong CYP3A inducers
  • CNS effects (seizures, hallucinations, cognitive changes, mood) may occur
  • Increased serum cholesterol and triglycerides; initiate or increase lipid-lowering agents
  • PR interval prolongation and AV block reported; monitor ECG
  • ILD/pneumonitis may occur
Overdose effects

Overdose treatment: general supportive measures; ECG monitoring recommended due to dose-dependent PR interval effects; no antidote.

Storage conditions

Store below 30°C, protected from moisture and light; keep out of reach of children.

Lorlatinib — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.