Ceritinib

What it is and how it works

Mechanism of Action Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 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.

Mechanism class: Tyrosine Kinase Inhibitors · Cytochrome P450 3A Inhibitors · Cytochrome P450 2C9 Inhibitors

Indications

® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test . ZYKADIA is a kinase inhibitor indicated for the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )

Dosage and administration (summary)

Recommended Dosage: 450 mg orally once daily with food. Patient Selection Select patients for treatment of metastatic NSCLC with ZYKADIA based on the presence of ALK positivity in tumor specimens . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics. 2. 2 Recommended Dosage The recommended dosage of ZYKADIA is 450 mg orally once daily with food until disease progression or unacceptable toxicity . If a dose of ZYKADIA is missed, make up that dose unless the next dose is due within 12 hours.

Contraindications

None. None.

Warnings and precautions

Gastrointestinal Adverse Reactions : ZYKADIA can cause gastrointestinal adverse reactions. If severe or intolerable, withhold if not responsive to antiemetics or antidiarrheals; upon improvement, resume ZYKADIA at a reduced dose. ( 2.3 , 5.1 ) Hepatotoxicity : ZYKADIA can cause hepatotoxicity. Monitor liver laboratory tests at least monthly. Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.2 ) Interstitial Lung Disease/Pneumonitis : Occurred in 2.4% of patients.

Pregnancy

Pregnancy Risk Summary Based on animal studies and its mechanism of action , ZYKADIA can cause fetal harm when administered to a pregnant woman. The limited available data on the use of ZYKADIA in pregnant women are insufficient to inform a risk.

Storage and supply

150 mg capsules Hard gelatin capsule with opaque blue cap and opaque white body; opaque blue cap marked in black ink with “LDK 150MG”, opaque white body marked in black ink with “NVR”. Available in: Bottles of 70 capsules…………………………………………………………………………………….NDC 0078-0640-70 Store at 20°C to 25°C (68°F to 77°F).

Source: Ceritinib (Zykadia) — US FDA prescribing information, 2025-12-15, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.