Vahe Bedian, Nikolaos Biris, Charles Omer, Jou-Ku Chung, James Fuller, Rafif Dagher, Sachin Chandran, Peter Harwin, Tomas Kiselak, Jonathan Violin, Andrew Nichols, Pradeep Bista
Hereditary angioedema (HAE) is a rare autosomal dominant disorder caused by a deficiency in functional C1 esterase inhibitor, a serpin family protein that blocks the activity of plasma kallikrein. Insufficient inhibition of plasma kallikrein results in the overproduction of bradykinin, a vasoactive inflammatory mediator that produces both pain and unpredictable swelling during HAE attacks, with potentially life-threatening consequences. We describe the generation of STAR-0215, a humanized IgG1 antibody with a long circulating half-life (t1/2 ) that potently inhibits plasma kallikrein activity, with a >1000-fold lower affinity for prekallikrein and no measurable inhibitory activity against other serine proteases...
November 2023: Journal of Pharmacology and Experimental Therapeutics