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.

Clinical Results

FDA Approval
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.

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.