Indications
Ceritinib is used to treat adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive. This must be confirmed by an FDA-approved test.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Ceritinib is a kinase inhibitor. In biochemical or cellular assays, at clinically relevant concentrations, it was found to act on ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR) and ROS1. Of these, Ceritinib is most active against ALK. In in vitro and in vivo assays, it blocked autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and the proliferation of ALK dependent cancer cells.
Absorption: After a single oral dose in patients, peak plasma levels (Cmax) of Ceritinib were reached at about 4 to 6 hours. AUC and Cmax rose in proportion to the dose over 50 to 750 mg under fasted conditions. The absolute bioavailability of Ceritinib has not been determined.
Distribution: Ceritinib is 97% bound to human plasma proteins, and this does not depend on the drug concentration. The apparent volume of distribution is 4230 L after a single 750 mg fasted dose in patients. Ceritinib also distributes slightly more into red blood cells than into plasma, with a mean in vitro blood-to-plasma ratio of 1.35.
Elimination: After a single 750 mg fasted dose, the geometric mean apparent plasma terminal half life (t½) of Ceritinib in patients was 41 hours. Its PK is nonlinear over time. The geometric mean apparent clearance was lower at steady-state (33.2 L/h) after 750 mg daily dosing than after a single 750 mg dose (88.5 L/h).
Metabolism: In vitro studies showed that CYP3A was the major enzyme involved in the metabolic clearance of Ceritinib. After a single 750 mg radiolabeled oral dose under fasted conditions, the parent compound was the main circulating component in human plasma (82%).
Excretion: After a single 750 mg radiolabeled oral dose under fasted conditions, 92.3% of the dose was recovered in the feces (68% of it as unchanged parent compound), while 1.3% of the dose was recovered in the urine.
Pregnancy & Breastfeeding
Ceritinib can harm an unborn baby when it is given to a pregnant woman. If a woman uses it during pregnancy, or becomes pregnant while she is taking it, she should be told about the possible danger to the baby.
There are no data on whether Ceritinib or its metabolites pass into human milk. Nor is there any information on what it does to a breastfed infant or to milk production. Ceritinib can cause serious adverse reactions, including gastrointestinal adverse reactions, hepatotoxicity, pneumonitis, bradycardia and pancreatitis. Because of this, a woman should be advised not to breastfeed during treatment with Ceritinib and for 2 weeks after she completes therapy.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.