TS-021

TS-021 is a selective, orally active, and reversible dipeptidyl peptidase-4 (DPP-4) inhibitor developed by Taisho Pharmaceutical for the treatment of type 2 diabetes. It functions by inhibiting the degradation of incretin hormones, such as glucagon-like peptide-1 (GLP-1), thereby enhancing insulin secretion and improving glucose tolerance in a glucose-dependent manner. TS-021 is characterized by its high selectivity for DPP-4 over related enzymes like DPP-8 and DPP-9, which minimizes potential off-target toxicities. Preclinical and early clinical studies have demonstrated its efficacy in improving glycemic control and potentially increasing pancreatic beta-cell mass, particularly when used in combination with metformin. The drug is typically studied as a monobenzenesulfonate salt.

Other names

(2S,4S)-4-Fluoro-1-{[(2-hydroxy-1,1-dimethylethyl)amino]acetyl}-pyrrolidine-2-carbonitrile monobenzenesulfonateCAS 667865-69-2CAS667865-69-2CAS-667865-69-2