General Information

Zykadia (ceritinib) is a highly selective inhibitor of anaplastic lymphoma kinase (ALK). ALK is a key gene implicated in the development of some lung cancers.

Zykadia is specifically indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer who have progressed on or are intolerant to crizotinib.

Zykadia is supplied as a capsule (150 mg) for oral administration. The recommended initial dose is 750 mg orally once daily. Administer Zykadia on an empty stomach.

Mechanism of Action

Zykadia (ceritinib) is a highly selective inhibitor of anaplastic lymphoma kinase (ALK), a gene implicated in the development of some cancers. Zykadia 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.

Side Effects

Adverse events associated with the use of Zykadia may include, but are not limited to, the following:

• diarrhea
• nausea
• elevated transaminases
• vomiting
• abdominal pain
• fatigue
• decreased appetite
• constipation

Clinical Trial Results

Zykadia was approved under accelerated approval based on tumor response rate and duration of response. An improvement in survival or disease-related symptoms has not been established. A multicenter, single-arm, open-label clinical trial was conducted in 163 subjects with metastatic ALK-positive NSCLC who progressed while receiving or were intolerant to crizotinib. All subjects received Zykadia at a dose of 750 mg once daily. The major efficacy outcome measure was objective response rate (ORR) according to RECIST as evaluated by both investigators and a Blinded Independent Central Review Committee (BIRC). Duration of response (DOR) was an additional outcome measure. ORR: Investigator assessment: 54.6% and BIRC assessment: 43.6%. DOR, median (months): Investigator assessment: 7.4 and BIRC assessment: 7.1.