Ceritinib (Zykadia)

Ceritinib approved for patients with late-stage non-small cell lung cancer (NSCLC).

A second generation TKI With activity against ALK and ROS1.

Trade name Zykadia.

An anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) that blocks proteins that promote the development of cancerous cells.

Inhibits 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.

It is for patients with metastatic ALK-positive NSCLC who were previously treated with crizotinib, the only other approved ALK TKI.

ALK-positive NSCLCs account for only two to seven percent of cases.

In a clinical trial of 163 participants with metastatic ALK-positive NSCLC, about half of the participants responded and this effect lasted an average of about seven months (Shaw AT et al).

Overall response rates in patients with ALK-positive NSCLC prior crizotinib was 54.6% with a 1.2% complete response.

ASCEND Trial compared ceritinib with chemotherapy: intracranial response rate was 72.7% for ceritinib and 27% for chemotherapy.

Common side effects include gastrointestinal symptoms such as diarrhea, nausea, vomiting, and abdominal pain.

Laboratory abnormalities include: increased liver enzymes, pancreatic enzymes, and increased glucose levels.

Taken on an empty stomach at least 2 hours before and after a medial: 750 mg once daily until disease progression unacceptable toxicity

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