Basic Information
ID DDInter193
Drug Type small molecule
Molecular Formula C30H26F4N6O
Molecular Weight 562.573
CAS Number 1809010-50-1
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] Berotralstat is strictly used to prevent, but not treat, these attacks.[L26656] Developed by BioCryst Pharmaceuticals, berotralstat is marketed under the name Orladeyo as oral capsules.[A225106] Berotralstat was first approved by the FDA on December 3, 2020, as the first once-daily oral therapy to prevent angioedema attacks of HAE in adults and pediatric patients 12 years and older.[L26661] Berotralstat was approved by the European Commission on April 30, 2021 [L41965] and by Health Canada on June 06, 2022.[L41960]
ATC Classification B06AC06
IUPAC Name 1-[3-(aminomethyl)phenyl]-N-{5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl}-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
InChI UXNXMBYCBRBRFD-MUUNZHRXSA-N
Canonical SMILES NCC1=CC(=CC=C1)N1N=C(C=C1C(=O)NC1=CC(=CC=C1F)[C@H](NCC1CC1)C1=CC=CC(=C1)C#N)C(F)(F)F
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