Adverse Drug Reaction Classification System

         

Pharmaceutical Information
Drug Name Ceritinib
Drug ID BADD_D00414
Description Ceritinib is used for the treatment of adults with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) following failure (secondary to resistance or intolerance) of prior crizotinib therapy. About 4% of patients with NSCLC have a chromosomal rearrangement that generates a fusion gene between EML4 (echinoderm microtubule-associated protein-like 4) and ALK (anaplastic lymphoma kinase), which results in constitutive kinase activity that contributes to carcinogenesis and seems to drive the malignant phenotype. Ceritinib exerts its therapeutic effect by inhibiting autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells. Following treatment with crizotinib (a first-generation ALK inhibitor), most tumours develop drug resistance due to mutations in key "gatekeeper" residues of the enzyme. This occurrence led to development of novel second-generation ALK inhibitors such as ceritinib to overcome crizotinib resistance. The FDA approved ceritinib in April 2014 due to a surprisingly high response rate (56%) towards crizotinib-resistant tumours and has designated it with orphan drug status.
Indications and Usage Ceritinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This indication is approved under accelerated approval based on tumor response rate and duration of response. An improvement in survival or disease-related symptoms has not been established. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.
Marketing Status approved
ATC Code L01ED02
DrugBank ID DB09063
KEGG ID D10551
MeSH ID C586847
PubChem ID 57379345
TTD Drug ID D04LVK
NDC Product Code 0078-0694; 54893-0072
UNII K418KG2GET
Synonyms ceritinib | 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine | Zykadia | LDK378
Chemical Information
Molecular Formula C28H36ClN5O3S
CAS Registry Number 1032900-25-6
SMILES CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Drug-induced liver injury12.03.01.044; 09.01.07.0230.000168%Not Available
Hepatic cancer16.07.02.004; 09.04.02.0080.000112%Not Available
Multiple organ dysfunction syndrome08.01.03.0570.000224%
Concomitant disease aggravated08.01.03.0630.000336%Not Available
Lung adenocarcinoma22.08.01.007; 16.19.01.0020.000280%Not Available
Lung adenocarcinoma stage IV22.08.01.017; 16.19.01.0070.000112%Not Available
Malignant pleural effusion22.05.04.001; 16.32.03.0140.000224%Not Available
Metastases to bone16.22.02.005; 15.09.03.0060.000728%Not Available
Metastases to lymph nodes16.22.02.006; 01.09.01.0150.000224%Not Available
Metastases to pleura22.05.04.002; 16.22.02.0220.000112%Not Available
Non-small cell lung cancer stage IV22.08.01.022; 16.19.01.0100.002295%Not Available
Metastases to meninges17.02.10.012; 16.22.02.0030.000168%Not Available
Cell death14.11.02.005; 08.03.03.0030.000224%Not Available
Non-small cell lung cancer metastatic22.08.01.021; 16.19.01.0090.000336%Not Available
Inflammatory myofibroblastic tumour15.09.02.003; 16.33.08.0010.000112%Not Available
Gait inability08.01.02.011; 17.02.05.0690.000112%Not Available
Illness08.01.03.091--Not Available
Non-small cell lung cancer stage IIIB16.19.01.018; 22.08.01.0340.000112%Not Available
Therapy non-responder08.06.01.0630.000492%Not Available
Therapy partial responder08.06.01.0640.000224%Not Available
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