Pronunciation sə-RIH-ti-nib Routes of
administration By mouth (capsules) Molar mass 558.14 g/mol | Trade names Zykadia ATC code L01XE28 (WHO) | |
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AHFS/Drugs.com Multum Consumer Information Pregnancy
category US: D (Evidence of risk) | ||
Debate alk positive nsclc front line therapy ceritinib
Ceritinib (INN, trade name Zykadia zy-KAY-dee-ə) is a drug for the treatment of a specific type of lung cancer. It is an anaplastic lymphoma kinase (ALK) inhibitor. It was developed by Novartis. It was approved in April 2014 by the Food and Drug Administration for the treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC) in patients that failed treatment with crizotinib. It is a more effective, but more toxic, alternative to traditional platinum-based chemotherapies.
Contents
Ceritinib in crizotinib resistant nsclc
Mechanism
Ceritinib was found at physiological concentrations to inhibit ALK, insulin-like growth factor 1 receptor (IGF-1R), and ROS1.
Adverse effects
Serious adverse effects include gastrointestinal toxicity, hepatotoxicity, interstitial lung disease, prolonged QT syndrome, hyperglycemia, bradycardia, and pancreatitis. The most commonly reported side effects were diarrhea, nausea, elevated liver enzymes, vomiting, abdominal pain, fatigue, decreased appetite, and constipation.
More than half of patients in clinical trials experienced adverse events that necessitated a reduction in dose.
History
Ceritinib was granted breakthrough status in March 2013 for ALK-positive NSCLC unresponsive to crizotinib, and FDA approval in April 2014 for the same indication.