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DDP-4 inhibitors, glugaon-like peptide 1(GLP-1) agonist - Coggle Diagram
DDP-4 inhibitors
藥物
Linagliptin
xanthine
oral
ketoacidosis患者不適用
蛋白結合率高80%
呼吸道感染
Alogliptin
sitagliptin
vildagliptin
saxagliptin
高效、高專一
CYP3A4代謝後有效
(和CYP3A4inhibitot/inducer共用要注意)
結構
aminoacylpyrrolidine
xanthine
pyrimidine-2,4-dione
cyano親電子和DDP-4產生離子鍵相接
vildagliptin
saxagliptin
aglogliptin
分布
膜上
游離在細胞質中
DDP-4是一種dipeptidyl peptidase enzymes
serine
protease
抑制劑和
serine的OH
產生離子鍵
glugaon-like peptide 1(GLP-1) agonist
降解
DDP-4切掉N端His Ala
28min就被降解
改變N端鏈結 增加效用
AiB aminoisobutyric acid
藥物
exenatide
liraglutide
接16C長鏈再N端，減緩DDP-4影響
和Thyroid C-cell tumors有關
dulaglutide
2條GLP-1 analogues，由雙硫鍵連接
長效
albiglutide
和albumin 共價接合減少腎
清除
兩GLP-1 analogues(改成Gly8)
lixisenitide
exenatide在C端加上6個Lys
semaglutide
超級長效
C18 fatty acid
隱憂
SC
potential immunogenicity