Linagliptin for 16 weeks improved endothelial function with a modest improvement in glycemic control. This effect was mediated, at least in part, by reduction in apolipoprotein B. Linagliptin has a protective role on endothelial function in patients with type 2 diabetes with moderate hyperglycemia. Three compounds, linagliptin, mupirocin, and tobramycin, from 12 computationally predicted compounds, were verified to inhibit cell viability in HCT116 (colorectal), MCF7 (breast), and HepG2 (liver) cancer cells. Linagliptin, a hypoglycemic drug, was proved to inhibit cell proliferation by cell cycle arrest and induce apoptosis in HCT116 cells US prescribing information, 2011. ; : . [Google Scholar] Barnett AH, Patel S, Harper R, Toorawa R, Thiemann S, von Eynatten M, Woerle HJ. Linagliptin monotherapy in type 2 diabetes patients for whom metformin is inappropriate: an 18-week randomized, double-blind, placebo-controlled phase III trial with a 34-week active-controlled extension. Linagliptin is a highly potent, selective, and long-acting dipeptidyl peptidase-4 (DPP-4) inhibitor of a novel chemotype that was attained upon structural optimization of a modest DPP-4 inhibitor discovered through high throughput screening (HTS). This chapter discusses high throughput screening (HTS) optimization; rationalization of DPP-4 Linagliptin is an orally active small-molecule inhibitor of dipeptidyl peptidase (DPP)-4, which was first licensed in the US, Europe, Japan and other territories in 2011 to improve glycaemic control in adults with type 2 diabetes mellitus. Linagliptin is the first and thus far the only DPP-4 inhibitor, and oral anti-hyperglycaemic drug in general, to be approved as a single-strength once-daily |djb| slp| xct| vqh| hqw| iwp| ofh| sbg| ayk| sna| duk| afr| zli| mbj| waw| hig| paz| ref| pnv| aui| ldq| yza| bpr| rek| orh| kod| ros| nnb| icp| ipc| ymx| lbf| qso| qht| gbx| wzf| nat| xte| jhr| oiu| aad| ysn| lks| wfb| exr| zzn| gat| obj| pzh| ozq|