Products
Lorlatinib was approved in the form of film-coated tablets in the United States in 2018, in the EU in 2019, and in many countries in 2020 (Lorviqua, or Lorbrena in the United States).
Structure and properties
Lorlatinib (C21H19FN6O2, Mr = 406.4 g/mol) exists as a white powder.
Effects
Lorlatinib (ATC L01XE44) has antitumor and antiproliferative properties. The effects are due to inhibition of ALK and ROS1 tyrosine kinases. Other kinases are inhibited by lorlatinib. The half-life is in the range of 23 hours.
Indications
For the treatment of adult patients with ALK-positive advanced non-small cell lung cancer (NSCLC).
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Concurrent use of strong CYP3A4/5 inducers.
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Lorlatinib is metabolized primarily by CYP3A4 and UGT1A4. Corresponding interactions may occur.
Adverse effects
The most common potential adverse effects include:
- Hypercholesterolemia
- Hypertriglyceridemia
- Edema
- Peripheral neuropathy
- Cognitive and affective effects
- Fatigue
- Weight gain