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molecules of the month

sebetralstat

oral, on-demand plasma kallikrein inhibitor

Ph. III candidate for on-demand treatment of HAE attacks

opt. from a known starting point

J. Med. Chem.

KalVista Pharmaceuticals Ltd., Salisbury, U.K.

Sebetralstat chemical structure oral, on-demand plasma kallikrein inhibitor - KalVista Pharmaceuticals Ltd., Salisbury, U.K.
5 mins read

Context. Sebetralstat (KalVista Pharmaceuticals) is an oral, on-demand plasma kallikrein (PKa) inhibitor intended for hereditary angioedema (HAE). As an on-demand medication, it can be administered to treat acute attacks rather than chronically to prevent attacks. Its structure was first disclosed at the ACS Spring Meeting earlier this year. HAE is a rare autosomal dominant disease caused by a deficiency in functional C1 inhibitor, a protease inhibitor protein involved in regulation of the complement, contact, and coagulation pathways. Insufficient C1 inhibitor protein results in the inability to suppress PKa activity, causing elevated levels of the vasodilator bradykinin that then leads to painful swelling. This swelling can be life-threatening if localized in the upper airway. Inhibitors of PKa have been explored, with…


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