|| Lung Cancer
|| ALK-positive NSCLC
| Mode of Action
|| Kinase inhibitor (targeted therapy)
| Approval Status
|| EMA approved (EU); FDA approved (USA); TGA approved (AUS)
| CAS Number || 1032900-25-6
|| 150 mg
Who is ceritinib for?
Zykadia (ceritinib) is indicated for the treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC) . While the FDA and EMA recommend it for first-line treatment , the TGA recommend it for patients whose disease has progressed on, or who are intolerant of crizotinib .
Complete information about Zykadia (ceritinib) dosage and administration can be found here: .The standard dosage is:
Consult your treating doctor for personalised dosing.
- 750 mg (5 capsules) orally once daily.
- Taken at least 1 hour before or at least 2 hours after a meal.
What is ceritinib and how does it work?
Zykadia (ceritinib) is a kinase inhibitor indicated for the treatment of patients with metastatic ALK-positive NSCLC .Mutations of the ALK gene can occur in several different types of cells, including lung cells, and can result in the development of a tumour . ALK gene mutations occur in 2 to 7 % of patients with NSCLC . Ceritinib is an ALK-inhibitor, which acts by inhibiting the activity of the ALK protein, and may thus prevent ALK-positive NSCLC-cells from growing and spreading .
What is ceritinib's approval status?
Zykadia (ceritinib) was approved by:
as monotherapy for the treatment of adult patients with anaplastic lymphoma kinase (ALK) positive locally advanced or metastatic non-small cell lung cancer (NSCLC).The EMA and TGA approvals of ceritinib for ALK-positive NSCLC in previously treated patients were based on two main global, multicentre, open-label, single-arm studies (study X2101 and study A2201) which involved in total 303 patients in whom the disease progressed despite previous treatment with crizotinib (Xalkori). In both studies, the medicine was not compared with any other treatment. The overall response rate (ORR) was 56.4 % [95 % CI: 48.5, 64.2] in Study X2101 and 37.1 % [95 % CI: 29.1, 45.7] in study A2201. The median duration of response (DoR) was 8.3 months [95 % CI: 6.8, 9.7] in Study X2101 and 9.2 months [95 % CI: 5.6, NE] in study A2201. The median progression-free survival (PFS) was 6.9 months [95 % CI: 5.6, 8.7] in Study X2101 and 5.7 months [95 % CI: 5.3, 7.4] in study A2201 .The FDA and EMA approval of ceritinib for ALK-positive NSCLC in previously untreated patients was based on an open-label, randomized, active-controlled multicenter
Study (ASCEND-4) involving 376 previously untreated ALK-positive NSCLC patients who were treated with Zykadia (ceritinib) or chemotherapy. The median PFS was 16.6 months [95 % CI: 12.6, 27.2] in the ceritinib arm and 8.1 months [95 % CI: 5.8, 11.1] in the chemotherapy arm. The ORR, was 73 % [95 % CI: 66, 79] and 27 % (95 % CI: 21, 34) in the ceritinib and chemotherapy arms, respectively. The median DoR was 23.9 months [95 % CI: 16.6, not estimable] and 11.1 months [95 % CI: 7.8, 16.4] in the ceritinib and chemotherapy arms, respectively. In patients with measurable central nervous system (CNS) lesions on baseline brain scans, the confirmed overall intracranial response rate (OIRR) was 57 % [95 % CI: 37, 76] in the ceritinib arm and 22 % [95 % CI 9, 42] in the chemotherapy arm. The median CNS response duration was 16.6 months [95 % CI: 8.1, NE] and not estimable [95 % CI: 1.5, NE] in the ceritinib and chemotherapy arms, respectively .
- FDA (USA) on April 4, 2014  with an accelerated approval for ALK-positive NSCLC in patients whose disease has progressed on or who are intolerant of crizotinib; and on May 26, 2017  with regular approval for previously untreated ALK-positive metastatic NSCLC
- EMA (EU) on May 6, 2015 
- TGA (AUS) on March 3, 2016 
The most common side effects are diarrhoea, nausea (feeling sick), vomiting, tiredness, abnormal liver tests, abdominal (belly) pain, decreased appetite, weight loss, constipation, rash, increases in the level of a waste product called creatinine in the blood (a possible sign of kidney problems), oesophageal disorder and anaemia (low levels of red blood cells) 
Summary of Product Characteristics [FDA]: Zykadia (ceritinib), Novartis, May 2017. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205755s009lbl.pdf
Summary of Product Characteristics [EMA]: Zykadia (ceritinib), Novartis, Mar. 2017. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/003819/WC500187504.pdf
Summary of Product Characteristics [TGA]: Zykadia (ceritinib), Novartis, Mar. 2016. https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2016-PI-01610-1
FDA News Release: FDA approves new oral therapy to treat ALK-positive lung cancer, 11/12/2015. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm476926.htm
Drugs.com. FDA approves Zykadia, Apr. 2014. https://www.drugs.com/newdrugs/fda-approves-zykadia-ceritinib-metastatic-non-small-cell-lung-cancer-4035.html
EMA. Human Medicines: Zykadia (ceritinib), 04/06/2015, (last update: 23/03/2017), cited on 20/06/2017. http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/003819/human_med_001860.jsp&mid=WC0b01ac058001d124
FDA. Approved Drugs: FDA broadens ceritinib indication to previously untreated ALK-positive metastatic NSCLC, 26/05/2017. https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm560873.htm
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