Products
Crizotinib has been approved in many countries since 2012 in capsule form (Xalkori).
Structure and properties
Crizotinib (C21H22Cl2FN5O, Mr = 450.3 g/mol) is an aminopyridine. It exists as a white to yellowish powder that is soluble in acidic solution to 10 mg/mL.
Effects
Crizotinib (ATC L01XE16) has antitumor and antiproliferative properties. The effects are due to inhibition of the tyrosine kinases ALK, HGFR, c-Met, and RON. Anaplastic lymphoma kinase (ALK) protein contributes to tumor growth and survival.
Indications
For the treatment of ALK-positive non-small cell lung cancer (NSCLC).
Dosage
According to the drug label. Capsules are taken twice daily with or without food.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Crizotinib is mainly biotransformed by CYP3A4/5. Therefore, potential drug-drug interactions with CYP inhibitors and inducers must be considered.
Adverse effects
The most common potential adverse effects include visual disturbances, nausea, diarrhea, vomiting, oedema, and constipation. Life-threatening pneumonitis, changes in liver enzymes, and prolongation of the QT interval have been reported.
