Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Berotralstat
Drug ID BADD_D02534
Description Berotralstat is a selective inhibitor of plasma kallikrein used in the prophylaxis of attacks of hereditary angioedema (HAE).[L26661] It works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.[A225166] Developed by BioCryst Pharmaceuticals, berotralstat is taken once-daily as oral capsules.[A225106] Under the market name Orladeyo, berotralstat was approved by the FDA on December 3, 2020, as the first oral, once-daily therapy to prevent angioedema attacks of HAE in adults and pediatric patients 12 years and older. In clinical trials, berotralstat was shown to significantly reduce attack rates at 24 weeks compared to placebo, which was sustained through 48 weeks. Berotralstat is strictly used to prevent, but not treat, these attacks.[L26656] Previous oral therapies used for prophylaxis of HAE attacks, such as androgens, were limited by undesirable adverse effects and several contraindications.[A225121] In clinical trials, berotralstat displayed a fast onset of action, long duration of action, and acceptable tolerance in patients.[A225106]
Indications and Usage Berotralstat is indicated for prophylaxis of attacks of hereditary angioedema (HAE) in adults and pediatric patients 12 years and older. It is not used for the treatment of acute HAE attacks.[L26661]
Marketing Status approved
ATC Code B06AC06
DrugBank ID DB15982
KEGG ID D11673
MeSH ID C000706836
PubChem ID 137528262
TTD Drug ID DQ1S0B
NDC Product Code Not Available
UNII XZA0KB1BDQ
Synonyms berotralstat | BCX7353 | BCX-7353 | 1H-pyrazole-5-carboxamide, 1-(3-(aminomethyl)phenyl)-N-(5-((R)-(3-cyanophenyl)((cyclopropylmethyl) | 1-(3-(aminomethyl)phenyl)-N-(5-((R)-(3-cyanophenyl)((cyclopropylmethyl)amino)methyl)-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
Chemical Information
Molecular Formula C30H26F4N6O
CAS Registry Number 1809010-50-1
SMILES C1CC1CNC(C2=CC(=C(C=C2)F)NC(=O)C3=CC(=NN3C4=CC=CC(=C4)CN)C(F)(F)F)C5=CC=CC(=C5)C #N
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)
Abdominal pain07.01.05.002-
Abdominal pain upper07.01.05.003-
Condition aggravated08.01.03.004--
Diarrhoea07.02.01.001-
Dizziness02.11.04.006; 17.02.05.003; 24.06.02.007-
Drug ineffective08.06.01.006--
Dyspepsia07.01.02.001-
Fatigue08.01.01.002-
Gastrooesophageal reflux disease07.02.02.003-
Gastrointestinal disorder07.11.01.001--
Headache17.14.01.001-
Nausea07.01.07.001-
Oedema peripheral02.05.04.007; 08.01.07.007; 14.05.06.011-
Rash23.03.13.001--
Vomiting07.01.07.003-
Deep vein thrombosis24.01.02.003--
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