avoralstat

Avoralstat is a potent, orally active small molecule inhibitor of plasma kallikrein (PKK), developed primarily for the prophylactic treatment of hereditary angioedema (HAE). Plasma kallikrein is a serine protease involved in the generation of bradykinin, which increases vascular permeability and leads to angioedema attacks in HAE patients. By inhibiting plasma kallikrein, avoralstat aims to reduce bradykinin production and thus prevent or lessen the severity of HAE attacks. The drug was developed by BioCryst Pharmaceuticals and has been evaluated in phase 3 clinical trials for hereditary angioedema; however, these studies did not demonstrate sufficient efficacy for attack prevention. More recently, avoralstat is being investigated as a potential therapy for diabetic macular edema via suprachoroidal administration using Clearside Biomedical’s SCS Microinjector[1][3][5][7][10].

Other names

avoralstat3-(2-((4-Carbamimidoylphenyl)carbamoyl)-4-ethenyl-5-methoxyphenyl)-6-((cyclopropylmethyl)carbamoyl)pyridine-2-carboxylic acid3-[2-(4-carbamimidoyl-phenylcarbamoyl)-5-methoxy-4-vinyl-phenyl]-6-(cyclopropylmethyl-carbamoyl)-pyridine-2-carboxylic acid