半数抑制量(IC50)<10 nmoL即可抑制DPP-4。对DPP-4的选择性约为DPP-8和DPP-9的10000倍,且浓度高达30 μmoL时也不会抑制CYP3A4,且不阻断hERG通道,降低使QT间期延长的不良反应风险[17]。5种抑制剂的结构式见图1。 表1 已上市DPP-4抑制剂列表Tab1 List of listed DPP-4 inhibitors? 2 对DPP-4选择性和...
Aims: To evaluate the methodological quality of systematic reviews (SRs), and summarize evidence of important outcomes from dipeptidyl peptidase-4 inhibitors (DPP4-I) in treating type 2 diabetes mellitus (T2DM).Methods: We included SRs of DPP4-I for the treatment of T2DM until January, 2018 by...
Currently, five PRRs are known to form inflammasomes: Nlrp1, Nlrc4, Nlrp3, Aim2, and Pyrin. We hypothesized that Dpp8/9 inhibitors might activate one of these five PRRs through an unknown mechanism. Notably, Nlrp1 and Nlrc4 both contain caspase activation and recruitment domains (CARDs) ...
DPP-4 inhibitorsSystematic reviewObjectiveTo conduct a systematic review of cost-effectiveness, cost-utility, and cost-benefit studies of DPP-4 inhibitors for diabetes treatment versus other antidiabetics.MethodsThree investigators searched the CRD York, Tufts CEA Registry, and MEDLINE databases through ...
DPP‐4 inhibitors or "gliptins" are weight neutral, pose lesser risk of hypoglycemia, and provide a long‐term post‐meal glycemic control. In this review, an attempt has been made to investigate novel potential compounds that can be added to the existing list of anti‐diabetic drugs.doi:...
Insulin glargine was dominant when compared with sitagliptin.ConclusionsAccording to the WHO threshold applied to the country and year of each study, DPP-4 inhibitors were highly cost-effective as second-line, as add-ons to metformin, in comparison with sulfonylureas. More recent therapies (GLP-1...
($m) for Byetta for diabetes in the seven major markets, 2008-2018 160Table 32: Impacting factors on the revenues of the Byetta franchise, 2008-2018 162Table 33: Januvia: key facts 163Table 34: Janumet: key facts 163Table 35: Clinical profile of approved...
Keywords: incretin; GLP-1; GIP; DPP-4 inhibitors; type-2 diabetes; CDOCKER; pharmacophore generation; molecular dynamics simulation 1. Introduction Worldwide 314 million individuals are suffering from (metabolic disorder) type-2 diabetes mellitus, which has been classified as a disease of glucose ...
2.5.4. FBPase The remaining seven FBPase candidate inhibitors displayed better affinity towards the protein than at least one reference compound (Figure 13). Only the MM/PBSA scores of C-0829 (−95.90 kJ/mol) and C-1933 (−95.49 kJ/mol) did not surpass the score of the reference CS9...