Raymond J Patch, Rui Zhang, Suzanne Edavettal, Mark J Macielag, Annette J Eckardt, Jiali Li, Marie-Laure Rives, Wilson Edwards, Simon A Hinke, Xi Qiu, Wenying Jian, Ondrej Libiger, Songmao Zheng, Jey Jeyaseelan, Yin Liang, Shamina M Rangwala, James N Leonard, Pamela Hornby
Pramlintide is an equipotent amylin analogue that reduces food intake and body weight in obese subjects and has been clinically approved as an adjunctive therapy for the treatment of adult diabetic patients. However, due to its extremely short half-life in vivo, a regimen of multiple daily administrations is required for achieving clinical effectiveness. Herein is described the development of prototypical long-acting pramlintide bioconjugates, in which pramlintide's disulfide-linked macrocycle was replaced by a cyclic thioether motif...
June 5, 2022: European Journal of Medicinal Chemistry