Ceritinib

Initial US Approval

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

Ceritinib 450 mg orally once daily with food until disease progression or unacceptable toxicity.1

First-dose reduction: 300 mg taken orally once daily with food.¹
Second-dose reduction: 150 mg taken orally once daily with food.¹
Discontinue ceritinib for patients unable to tolerate 150 mg taken orally once daily with food.¹

Treatment Setting: Treatment naive ALK+ metastatic NSCLC
Key Inclusion Criteria: Eligible participants in ASCEND-4 included patients with advanced ALK-positive NSCLC who had not received prior therapy for metastatic disease and an ECOG status of 0-2.
Treatment: Ceritinib at a dose of 750 mg once daily under fasted conditions.

Treatment Setting: Previously treated ALK+ metastatic NSCLC
Key Inclusion Criteria: Participants in ASCEND-1 included patients with metastatic ALK-positive NSCLC who were intolerant to crizotinib or had experienced disease progression while receiving treatment with crizotinib.
Treatment: Ceritinib at a dose of 750 mg once daily under fasted conditions.

Ceritinib: Efficacy Data

Common Adverse Reactions (≥20%): The most frequently reported any grade AEs were diarrhea (85%), nausea (69%), vomiting (67%), fatigue (45%), abdominal pain (40%), decreased appetite (34%), cough (25%), weight loss (24%), non-cardiac chest pain (21%), rash (21%), and constipation (20%).
Common Laboratory Abnormalities (≥20%): The most frequently reported any grade laboratory abnormalities were
Dosage Interruptions Due to AEs: 77%
Dosage Reduction Due to AEs: 66%
Permanent Discontinuation Due to AEs: 12%

Common Adverse Reactions (≥20%): The most frequently reported any grade AEs were diarrhea (86%), nausea (80%), vomiting (60%), abdominal pain (54%), fatigue (52%), decreased appetite (34%), and constipation (29%).
Common Laboratory Abnormalities (≥20%): The most frequently reported any grade laboratory abnormalities were anemia (84%), increased ALT (80%), increased AST (75%), increase creatinine (58%), hyperglycemia (49%), hypophosphatemia (36%), and increased lipase (28%).
Dosage Reduction Due to AEs: 59%
Permanent Discontinuation Due to AEs: 10%

Ceritinib: Most Common Adverse Events of Grade 3 or 4

Zykadia (ceritinib). Prescribing information. Novartis Pharmaceuticals Corporation; 2021. Accessed December 12, 2024. https://www.novartis.com/us-en/sites/novartis_us/files/zykadia.pdf
Soria JC, Tan DSW, Chiari R, Wu, et al. 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. Lancet.2017;389(10072):917-929. doi:10.1016/S0140-6736(17)30123-X
Kim DW, Mehra R, Tan DSW, et al. Activity and safety of ceritinib in patients with ALK-rearranged non-small-cell lung cancer (ASCEND-1): updated results from the multicentre, open-label, phase 1 trial. Lancet Oncol. 2016;17(4):452-463. doi:10.1016/S1470-2045(15)00614-2
Dziadziuszko R, Peters S, Ruf T, et al. Clinical experience and management of adverse events in patients with advanced ALK-positive non-small-cell lung cancer receiving alectinib. ESMO Open. 2022;7(6):100612. doi:10.1016/j.esmoop.2022.100612
Zhou F, Yang Y, Zhang L, et al. Expert consensus of management of adverse drug reactions with anaplastic lymphoma kinase tyrosine kinase inhibitors. ESMO Open. 2023;8(3):101560. doi:10.1016/j.esmoop.2023.101560
Schaefer ES, Baik C. Proactive management strategies for potential gastrointestinal adverse reactions with ceritinib in patients with advanced ALK-positive non-small-cell lung cancer. CMAR. Published online March 2016:33. doi:10.2147/CMAR.S96471