Berotralstat

• CAT Number: I023288
• CAS Number: 1809010-50-1
• Molecular Formula: C30H26F4N6O
• Molecular Weight: 562.56
• Purity: 98%
• Synonyms: 2-[3-(aminomethyl)phenyl]-N-[5-[(R)-(3-cyanophenyl)-(cyclopropylmethylamino)methyl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
• Target Protein: P03952
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• InChI: InChI=1S/C30H26F4N6O/c31-24-10-9-22(28(37-17-18-7-8-18)21-5-1-3-19(11-21)15-35)13-25(24)38-29(41)26-14-27(30(32,33)34)39-40(26)23-6-2-4-20(12-23)16-36/h1-6,9-14,18,28,37H,7-8,16-17,36H2,(H,38,41)/t28-/m1/s1
• InChIKey: UXNXMBYCBRBRFD-MUUNZHRXSA-N
• SMILES: C1CC1CN[C@@H](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

Berotralstat（Cat No.:I023288）is an oral medication used to prevent attacks of hereditary angioedema (HAE), a rare genetic disorder characterized by recurrent episodes of severe swelling. It works by inhibiting plasma kallikrein, an enzyme responsible for the excessive production of bradykinin, which triggers swelling in HAE patients. By blocking kallikrein, Berotralstat reduces the frequency and severity of angioedema attacks. Its once-daily oral dosing provides a convenient, non-invasive option for long-term prophylaxis, improving quality of life and reducing the burden of HAE-related hospitalizations and emergency treatments.

Reference

[1]. Zuraw B, et al. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial [published online ahead of print, 2020 Oct 21]. J Allergy Clin Immunol. 2020;S0091-6749(20)31484-6.
[Content Brief]

[2]. Manning ME, et al. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies. Allergy Asthma Proc. 2021;42(4):274-282.
[Content Brief]