| 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 |
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| ADRs Induced by Drug |
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