Products
Ceritinib is commercially available in capsule form (Zykadia). It was approved in the United States in 2014 and in the EU and many countries in 2015. In 2020, film-coated tablets were registered.
Structure and properties
Ceritinib (C28H36N5O3ClS, Mr = 558.14 g/mol) exists as a white to slightly yellow or slightly brown powder.
Effects
Ceritinib (ATC L01XE28) has antitumor and antiproliferative properties. The effects are due to inhibition of the kinase ALK (anaplastic lymphoma kinase). The half-life ranges from 31 to 41 hours.
Indications
For the treatment of patients with advanced ALK-positive non-small cell lung cancer (ALK+NSCLC) who have been pretreated with crizotinib.
Dosing
According to the SmPC. Capsules are taken once daily, at the same time of day, fasting (2 hours before or 2 hours after a meal).
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Ceritinib is a substrate of CYP3A and corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include diarrhea, nausea, vomiting, fatigue, abdominal pain, poor appetite, constipation, rash, esophageal disease, and anemia.