What Is Ceritinib (Zykadia)? FDA Approval, Licensing and Reimbursement in Turkey
In this article
Powerful Blockade in ALK-Positive Lung Cancer: Ceritinib
One of the groundbreaking agents for ALK-positive metastatic non-small cell lung cancer (NSCLC), ceritinib (Zykadia®) is a highly effective tyrosine kinase inhibitor that stops tumor growth both in the first line and when resistance develops after crizotinib.
Drug Profile
- Brand Name: Zykadia®
- Active Ingredient: Ceritinib
- Class: Signal Transduction Inhibitor, Tyrosine Kinase Inhibitor (TKI)
- Route of Administration: Oral (Capsule)
- Manufacturer: Novartis
- License: Licensed in Turkey.
- Reimbursement: Included on the SGK reimbursement list.
-
Therapeutic indications:
• Indicated as first-line monotherapy until progression in adults with advanced non-small cell lung cancer, provided anaplastic lymphoma kinase (ALK) positivity is assessed by an accredited laboratory.
• Indicated as monotherapy until progression in adults with ALK-positive advanced non-small cell lung cancer previously treated with crizotinib who developed progression at the end of treatment.
Ceritinib is not used after progression on ALK inhibitors other than crizotinib.
Treatment duration: Treatment duration with Zykadia (ceritinib) may vary with the patient's response and tolerance. In general, treatment continues until disease progression stops or unacceptable adverse effects occur.
- March 2026 Price: The retail pharmacy price of the 150 mg capsule is 137085.38 TL.
Approved Indications
- Metastatic NSCLC (ALK+): Patients with newly diagnosed (first-line) metastatic ALK-positive NSCLC or progression after crizotinib.
FDA Approval History
Zykadia was initially approved for patients with ALK-positive NSCLC resistant to or intolerant of crizotinib.
Following successful clinical studies, its use was expanded to first-line treatment for newly diagnosed metastatic disease.
What Is Ceritinib and How Does It Work at the Molecular Level?
Ceritinib is a selective tyrosine kinase inhibitor targeting signaling by the abnormal ALK protein. It cuts off cancer cell growth commands at their source.
🔬 How It Works at the Molecular Level
- 1. ALK and ROS1 Inhibition:
In addition to anaplastic lymphoma kinase (ALK), it inhibits ROS1, IGF-1R, and insulin receptors, producing a multifaceted antitumor effect. - 2. Activity Against Resistance Mutations:
It may retain activity in tumors with specific resistance mutations such as L1196M and G1269A that develop with crizotinib use. - 3. Inhibiting Metastasis:
It slows disease spread by blocking signaling pathways that trigger tumor angiogenesis (blood vessel formation) and metastasis.
Administration and Dosage
- Standard Dose: The recommended dose is 750 mg once daily (usually 5 capsules of 150 mg).
- Fasting Requirement: Ceritinib must be taken on an empty stomach. Taking it at least 2 hours before or 2 hours after meals is critical for absorption.
- Food Interaction: The dietary rule must be followed strictly because fatty foods can cause an uncontrolled increase in drug levels.
Mechanisms of Resistance
| Mechanism | Description |
|---|---|
| Genetic Mutations | New ALK mutations such as G1202R or F1174C may cause resistance. |
| EMT Transition | Cells change their structure (mesenchymal transition) and become unresponsive to treatment. |
| Alternative Pathways | Activation of MEK and SRC signaling pathways bypasses the drug. |
Adverse Effects and Management
- Gastrointestinal System: Nausea, vomiting, diarrhea, and abdominal pain are very common. Amylase/lipase monitoring is also required because of the risk of pancreatitis.
- Liver Toxicity: ALT/AST elevations may occur. Regular blood tests are essential.
- Pulmonary Effects: Watch for pulmonary toxicity (ILD) presenting with cough and shortness of breath.
- Metabolic Changes: Elevated blood glucose (hyperglycemia) may occur.
- Cardiac Status: ECG monitoring is recommended because of the risks of QT prolongation and a slow pulse (bradycardia).
Special Situations and Warnings
- Interaction with Acid Suppressants: PPIs, H2 blockers, and antacids may impair absorption. They must not be used together with the drug.
- Foods to Avoid: Avoid grapefruit, pomelo, star fruit, and Seville oranges.
- Pregnancy and Breastfeeding: It harms the fetus. Breastfeeding must be avoided during treatment and for 2 weeks after the last dose.
- Drug Interactions: Drugs acting through CYP3A4, such as ketoconazole (an inhibitor) or rifampin (an inducer), can dangerously alter drug levels.
Pharmacokinetic Summary
- Peak Level: 4-6 hours after oral administration.
- Half-Life: Approximately 40 hours.
- Excretion: 92% is excreted in feces and only 1.3% in urine.
Sources
Was this article helpful?
Your feedback helps us improve our content.
Reader comments
Share your comment
Your name and comment are published only after administrator approval. Your email address is never shown to visitors.
Be the first to comment.