Design and development of a new glucagon-like peptide-1 receptor agonist to obtain high oral bioavailability
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DOI:
文献链接: DOI: 10.1007/s11095-022-03265-3
其他信息:
H Chen, Y Lu, S Shi, Q Zhang, X Cao, L Sun…
Pharmaceutical …, 2022
Springer
Purpose Semaglutide is the only oral GLP-1 RA in the market, but oral bioavailability is generally limited in range of 0.4–1%. In this study, a new GLP-1RA named SHR-2042 was developed to gain higher oral bioavailability than semaglutide. Method Self-association of SHR-2042, semaglutide and liraglutide were assessed using SEC-MALS. The intestinal perfusion test in SD rats was used to select permeation enhancers (PEs) including SNAC, C10 and LCC. ITC, CD and DLS were used to explore the interaction between SHR-2042 …
