# Ceritinib

Source: https://onco.cc/drugs/ceritinib/  
OnCo record `ceritinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Ceritinib is a second-generation ALK pill for lung cancer, effective after crizotinib but with gastrointestinal toxicity that limited uptake.

## Summary

Ceritinib is a second-generation ALK tyrosine kinase inhibitor active against several crizotinib-resistance mutations including L1196M, G1269A, I1171T and S1206Y. The ASCEND-1, 2 and 5 studies established activity after crizotinib, and ASCEND-4 showed first-line superiority over chemotherapy with median progression-free survival of 16.6 versus 8.1 months. It received accelerated US approval in 2014 after crizotinib and full first-line approval in 2017. Gastrointestinal toxicity at the original 750 mg fasting dose limited uptake; the 450 mg dose taken with food improved tolerability with equivalent exposure. It is rarely used now because alectinib, brigatinib and lorlatinib offer better tolerability and CNS control. Ceritinib was proof that resistance to the first ALK drug could be overcome by a more potent one.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-24
- Tags: gap-fill
- Brand: Zykadia
- Modality: Small-molecule ALK TKI (second generation)
- Mechanism: Potent ALK inhibitor active against several crizotinib-resistance mutations (L1196M, G1269A, I1171T, S1206Y).
- Approvals: US 2014: ALK-positive metastatic NSCLC after crizotinib; US 2017: First-line ALK-positive metastatic NSCLC; EU 2015: Conditional May 2015; full approval 2017; England (NICE) 2018: Untreated ALK-positive advanced non-small-cell lung cancer

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Ceritinib
- ASCEND-4 (Lancet 2017): https://doi.org/10.1016/S0140-6736(17)30123-X
- Label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=ceritinib
- NICE TA500: ceritinib for untreated ALK-positive non-small-cell lung cancer: https://www.nice.org.uk/guidance/ta500

## Connected records

- cancers: [ALK-positive non-small-cell lung cancer](https://onco.cc/cancers/alk-positive-nsclc/), [Inflammatory myofibroblastic tumour (IMT)](https://onco.cc/cancers/inflammatory-myofibroblastic-tumour/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [ALK](https://onco.cc/targets/alk/)
- companies: [Novartis](https://onco.cc/companies/novartis/)
- trials: [ASCEND-4](https://onco.cc/trials/nct01828099/), [LDK378 Versus Chemotherapy in ALK Rearranged (ALK Positive) Patients Previously Treated With Chemotherapy (Platinum Doublet) and Crizotinib](https://onco.cc/trials/nct01828112/), [Molecular Profiling of Advanced Soft-tissue Sarcomas](https://onco.cc/trials/nct03784014/), [Using Tumor Models to Determine Treatments](https://onco.cc/trials/nct06813079/)
- key papers: [First-line ceritinib versus platinum-based chemotherapy in advanced ALK-rearranged non-small-cell lung cancer (ASCEND-4): a randomised, open-label, phase 3 study](https://onco.cc/key-papers/paper-ascend-4-lancet-2017/), [Molecular mechanisms of resistance to first- and second-generation ALK inhibitors in ALK-rearranged lung cancer](https://onco.cc/key-papers/paper-gainor-alk-resistance-mutations-cancer-discov-2016/)
- terms: [Lung cancer drugs in England: what NICE has recommended](https://onco.cc/terms/lung-uk-drug-access/)
- biomarkers: [ALK fusion (ALK-positive)](https://onco.cc/biomarkers/alk-fusion/)

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