Adverse Drug Reaction Classification System

         

Pharmaceutical Information
Drug Name Brigatinib
Drug ID BADD_D02509
Description Brigatinib, originally named AP26113, is a reversible dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). It presents selectivity against the mutant forms of EGFR compared to the wild-type.[A31311] It also exhibits selectivity against 9 different Crizotinib-resistant mutants of the EML4-ALK fusion gene, which is a pivotal player in the transformation of susceptible lung parenchyma.[A31313] Brigatinib was developed by Ariad Pharmaceuticals, a subsidiary of Takeda Pharmaceutical Company Limited, and FDA-approved on April 28, 2017.[L1026]
Indications and Usage The anaplastic lymphoma kinase positive, metastatic non-small cell lung cancer (ALK+ NSCLC), represents only 3-5% of the NSCLC cancer cases, but the ALK mutation, overexpression and presence in several oncogenic fusion proteins in solid and hematologic tumors have pointed out the importance as well as its potential as a cancer therapy target.[A31311] The ALK-related cases of NSCLC are associated with the presence of the fusion gene EML4-ALK which fused the ALK protein with the echinoderm microtubule-associated protein like-4 whose original function is the correct formation of microtubules.[A31313] The presence of the aberrant fusion protein results in abnormal signaling that provokes increased cell growth, proliferation and survival.[A31316] Crizotinib is indicated for the treatment of such cases but the presence of ALK kinase domain mutations confer resistance to the treatment. Thus, brigatinib is indicated for the treatment of patients with ALK+ NSCLC with intolerance to Crizotinib.[A31314]
Marketing Status approved; investigational
ATC Code L01ED04
DrugBank ID DB12267
KEGG ID D10866
MeSH ID C000598580
PubChem ID 68165256
TTD Drug ID D08PIE
NDC Product Code 63020-180; 50683-0420; 63020-198; 63020-090; 65392-3311; 63020-113
UNII HYW8DB273J
Synonyms brigatinib | Alunbrig | AP26113
Chemical Information
Molecular Formula C29H39ClN7O2P
CAS Registry Number 1197953-54-0
SMILES CN1CCN(CC1)C2CCN(CC2)C3=CC(=C(C=C3)NC4=NC=C(C(=N4)NC5=CC=CC=C5P(=O)(C)C)Cl)OC
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)
Metastases to central nervous system17.02.10.013; 16.22.02.0040.003358%Not Available
Drug resistance08.06.01.0050.000470%Not Available
Adverse event08.06.01.0100.000448%Not Available
Brain neoplasm17.20.01.003; 16.30.01.0030.000168%Not Available
Neoplasm progression16.16.02.0050.003750%Not Available
Decreased appetite14.03.01.005; 08.01.09.0280.002104%
Adverse drug reaction08.06.01.0090.001265%Not Available
Chondrocalcinosis14.04.01.017; 15.01.06.0060.000224%Not Available
Disease progression08.01.03.0380.002619%
Drug intolerance08.06.01.0130.000660%Not Available
Non-small cell lung cancer22.08.01.002; 16.19.01.0010.006044%Not Available
Pulmonary toxicity22.01.02.007; 12.03.01.0130.000448%Not Available
Metastasis16.22.01.0010.001511%Not Available
Renal impairment20.01.03.0100.000783%Not Available
Pulmonary arterial hypertension24.08.03.003; 22.06.01.0020.000168%Not Available
Oropharyngeal pain07.05.05.004; 22.12.03.0160.000302%
Drug-induced liver injury12.03.01.044; 09.01.07.0230.000168%Not Available
Faeces soft07.01.03.0080.000112%Not Available
Multiple organ dysfunction syndrome08.01.03.0570.000168%
Lung adenocarcinoma22.08.01.007; 16.19.01.0020.000336%Not Available
Lung adenocarcinoma stage IV16.19.01.007; 22.08.01.0170.000336%Not Available
Lung carcinoma cell type unspecified recurrent22.08.01.018; 16.19.02.0050.000224%Not Available
Metastases to bone16.22.02.005; 15.09.03.0060.000280%Not Available
Metastases to lymph nodes16.22.02.006; 01.09.01.0150.000112%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; 16.19.01.0100.000112%Not Available
Metastases to meninges17.02.10.012; 16.22.02.0030.000280%Not Available
Lymphangiosis carcinomatosa24.09.02.007; 16.22.02.009; 01.09.01.0270.000112%Not Available
Non-small cell lung cancer metastatic22.08.01.021; 16.19.01.0090.000392%Not Available
Internal haemorrhage24.07.01.0720.000112%Not Available
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