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Zykadia (ceritinib)

Zykadia blocks the activity of the ALK protein, which is involved in the growth and spread of cancer cells.

Zykadia (ceritinib) is a small molecule kinase inhibitor developed by Novartis, targeting the ALK tyrosine kinase receptor. It is approved for the treatment of ALK fusion gene-positive non-small-cell lung cancer and non-small cell lung cancer. Zykadia was first approved by the FDA in 2014 and remains a patented product. Key safety considerations include monitoring for hepatotoxicity and gastrointestinal adverse events. As a kinase inhibitor, Zykadia works by blocking the activity of the ALK protein, which is involved in the growth and spread of cancer cells.

At a glance

Mechanism of action

Ceritinib is kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Ceritinib inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice and rats. Ceritinib exhibited dose-dependent anti-tumor activity in mice bearing EML4-ALK-positive NSCLC xenografts with demonstrated resistance to crizotinib, at concentrations within clinically relevant range.

Approved indications

• ALK fusion gene-positive non-small-cell lung cancer
• Non-small cell lung cancer

Common side effects

• Diarrhea
• Nausea
• Vomiting
• Fatigue
• Abdominal pain
• Pneumonia
• Pleural effusion
• Dyspnea
• Hyperglycemia
• AST increased
• Lung infection
• Pericardial effusion

Key clinical trials

• Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer (PHASE2)
• Next Generation Personalized Neuroblastoma Therapy (PHASE1)
• Molecular Profiling and Matched Targeted Therapy for Patients With Unresectable Advanced or Metastatic Melanoma (PHASE2)
• Study of Trametinib + Ceritinib in Patients With Unresectable Melanoma (PHASE1)
• Pediatric Precision Laboratory Advanced Neuroblastoma Therapy (PHASE2)
• Ceritinib Plus Docetaxel in ALK-Negative, EGFR WT Advanced NSCLC (PHASE1)
• Roll-over Study to Allow Access to Certinib (LDK378) for Patients Who Are on Ceritinib Treatment in a Novartis-sponsored Study (PHASE4)
• Study of Safety and Efficacy of Ceritinib in Combination With Nivolumab in Patients With ALK-positive Non-small Cell Lung Cancer (PHASE1)

Patents

Primary sources

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