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 Not Available
ATC Code L01ED04
DrugBank ID DB12267
KEGG ID D10866
MeSH ID C000598580
PubChem ID 68165256
NDC Product Code 63020-113; 63020-090; 63020-180; 50683-0420; 63020-198; 65392-3311
Synonyms brigatinib | Alunbrig | AP26113
Chemical Information
Molecular Formula C29H39ClN7O2P
CAS Registry Number 1197953-54-0
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Not AvailableNot AvailableNot AvailableNot AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal distension07.01.04.0010.000799%
Abdominal pain07.01.05.0020.001066%
Adenocarcinoma16.16.01.0040.000139%Not Available
Alanine aminotransferase increased13.03.01.0030.000533%
Amylase increased13.05.01.0090.000533%
Asthenia08.01.01.0010.001066%Not Available
Back pain15.03.04.0050.001066%
Blood creatine phosphokinase increased13.04.01.0010.002931%
Blood pressure increased13.14.03.0050.001598%Not Available
Bone pain15.02.01.0010.000533%
C-reactive protein increased13.09.01.0070.000533%Not Available
Cerebral haemorrhage24.07.04.001; Available
Chest discomfort22.02.08.001;; Available
Depressed mood19.15.02.0010.000533%Not Available
Discomfort08.01.08.0030.000533%Not Available
Dry mouth07.06.01.0020.001332%
Dyspnoea exertional02.01.03.003; Available
Erythema23.03.06.0010.000799%Not Available
Feeling abnormal08.01.09.0140.000533%Not Available
Gastrooesophageal reflux disease07.02.02.0030.000533%
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