Ceritinib

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.

• ZYKADIA ® 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 [see Dosage and Administration (2.1)] . 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.ICD-10: C34.90, C85.90

• None. None.contraindicated

Recommended Dosage: 450 mg orally once daily with food. ( 2.2 ) 2.1 Patient Selection Select patients for treatment of metastatic NSCLC with ZYKADIA based on the presence of ALK positivity in tumor specimens [see Clinical Studies (14.1)] . 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 [see Clinical Pharmacology (12.3)] . If a dose of ZYKADIA is missed, make up that dose unless the next dose is due within 12 hours. If vomiting occurs during the course of treatment, do not administer an additional dose and continue with the next scheduled dose of ZYKADIA. 2. 3 Dosage Modifications for Adverse Reactions Table 1: Recommended ZYKADIA Dose Reductions Dose Reduction Recommended Dosage First-dose reduction 300 mg taken orally once daily with food Second-dose reduction 150 mg taken orally once daily with food Discontinue ZYKADIA for patients unable to tolerate 150 mg taken orally once daily with food. Dosage modifications for selected adverse reactions of ZYKADIA are provided in Table 2. If dose reduction is required due to an adverse reaction not listed in Table 2, then reduce the daily dose of ZYKADIA by 150 mg.

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. Permanently discontinue ZYKADIA in patients diagnosed with treatment-related interstitial lung disease (ILD)/pneumonitis. ( 2.3 , 5.3 ) QT Interval Prolongation : ZYKADIA can cause QTc interval prolongation. Monitor electrocardiograms and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval. Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.4 ) Hyperglycemia : ZYKADIA can cause hyperglycemia. Monitor fasting glucose prior to treatment and periodically thereafter. Initiate or optimize anti-hyperglycemic medications as indicated. Withhold, then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.5 ) Bradycardia : ZYKADIA can cause bradycardia. Monitor heart rate and blood pressure regularly. Withhold, then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.6 ) Pancreatitis : Elevations of lipase and/or amylase and pancreatitis can occur.

The following clinically significant adverse reactions are described elsewhere in the labeling: Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.3)] QT Interval Prolongation [see Warnings and Precautions (5.4)] Hyperglycemia [see Warnings and Precautions (5.5)] Bradycardia [see Warnings and Precautions (5.6)] Pancreatitis [see Warnings and Precautions (5.7)] The most common adverse reactions (incidence of ≥ 25%) in patients treated with ZYKADIA 450 mg with food are diarrhea, nausea, abdominal pain, vomiting, and fatigue; and with ZYKADIA 750 mg under fasted conditions are diarrhea, nausea, vomiting, fatigue, abdominal pain, decreased appetite, and weight loss. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Lactation : Advise not to breastfeed. ( 8.2 ) Severe Hepatic Impairment : For patients with severe hepatic impairment (Child-Pugh C), dose reduce ZYKADIA. ( 8.6 ) 8.1 Pregnancy Risk Summary Based on animal studies and its mechanism of action [see Clinical Pharmacology (12.1)] , 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. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits ( see Data ). Advise a pregnant woman of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study in which pregnant rats were administered daily doses of ceritinib during organogenesis, dose-related skeletal anomalies were observed at doses as low as 50 mg/kg (less than 0.5-fold the human exposure by AUC at the recommended dose). Findings included delayed ossifications and skeletal variations.

Metabolism

After a single oral administration of ZYKADIA in patients, AUC and C max increased dose proportionally over 50 mg to 750 mg under fasted conditions. Following ZYKADIA 750 mg once daily under fasted conditions, steady state was reached by 15 days with a geometric mean accumulation ratio of 6.2 after 3 weeks.

• Mar 18, 2019NDANDA211225Novartis

1. 1Malignant Neoplasm Progression42618%
2. 2Diarrhoea42418%
3. 3Nausea34014%
4. 4Death27912%
5. 5Vomiting2239.4%
6. 6Metastases To Central Nervous System1727.3%
7. 7Fatigue1335.6%
8. 8Non-small Cell Lung Cancer1295.4%
9. 9Decreased Appetite1174.9%
10. 10Disease Progression1114.7%
11. 11Dyspnoea1004.2%
12. 12Abdominal Pain984.1%
13. 13Asthenia903.8%
14. 14Non-small Cell Lung Cancer Stage Iv903.8%
15. 15Drug Ineffective843.5%

The 10 most recently updated of 56 ClinicalTrials.gov registrations naming Ceritinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study of Safety and Efficacy of Ceritinib in Combination With Nivolumab in Patients With ALK-positive Non-small Cell Lung Cancer
  Active not recruiting · Phase 1 · Interventional · 57 enrolled · Novartis Pharmaceuticals
  NCT02393625updated 2026-06-11
• Roll-over Study to Allow Access to Certinib (LDK378) for Patients Who Are on Ceritinib Treatment in a Novartis-sponsored Study
  Active not recruiting · Phase 4 · Interventional · 233 enrolled · Novartis Pharmaceuticals
  NCT02584933updated 2026-06-11
• Molecular Profiling and Matched Targeted Therapy for Patients With Unresectable Advanced or Metastatic Melanoma
  Completed · Phase 2 · Interventional · 216 enrolled · Melanoma Institute Australia
  NCT02645149updated 2026-05-29
• A Study of Neladalkib (NVL-655) in Patients With Advanced NSCLC and Other Solid Tumors Harboring ALK Rearrangement or Activating ALK Mutation (ALKOVE-1)
  Recruiting · Phase 1 · Phase 2 · Interventional · 840 enrolled · Nuvalent Inc.
  NCT05384626updated 2026-05-27
• Ceritinib and Everolimus in Treating Patients With Locally Advanced or Metastatic Solid Tumors or Stage IIIB-IV Non-small Cell Lung Cancer
  Active not recruiting · Phase 1 · Interventional · 37 enrolled · M.D. Anderson Cancer Center
  NCT02321501updated 2026-05-20
• Ceritinib Plus Docetaxel in ALK-Negative, EGFR WT Advanced NSCLC
  Active not recruiting · Phase 1 · Interventional · 21 enrolled · H. Lee Moffitt Cancer Center and Research Institute
  NCT03611738updated 2026-05-15
• Molecular Profiling of Advanced Soft-tissue Sarcomas
  Completed · Phase 3 · Interventional · 603 enrolled · Institut National de la Santé Et de la Recherche Médicale, France
  NCT03784014updated 2026-04-29
• Pediatric Precision Laboratory Advanced Neuroblastoma Therapy
  Recruiting · Phase 2 · Interventional · 500 enrolled · Giselle Sholler
  NCT02559778updated 2026-04-28
• Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer
  Terminated · Phase 2 · Interventional · 10 enrolled · National Cancer Institute (NCI)
  NCT03737994updated 2026-04-23
• Managed Access Programs for LDK378, Ceritinib
  No longer available · Expanded access · Novartis Pharmaceuticals
  NCT05100134updated 2026-04-01

Frequently asked questions

How does Ceritinib work?

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.

What is Ceritinib used for?

According to FDA labeling, Ceritinib carries indications including: ZYKADIA ® 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 [see Dosage and Administration (2.1)] . 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ceritinib?

Ceritinib is classified as Anaplastic lymphoma kinase (ALK) inhibitors, Kinase Inhibitor, Cytochrome P450 2C9 Inhibitors, Cytochrome P450 3A Inhibitors, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Ceritinib?

Ceritinib is marketed under brand names including Zykadia.

What are the contraindications for Ceritinib?

Ceritinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.