Drug intelligence / Profile preview

dorzagliatin + sitagliptin

Development stage
Unknown
Lead developer
Hua Medicine
Modality
Small Molecules
Administration
Oral
01

Overview

This is a fixed combination of **dorzagliatin**, a first-in-class dual-acting glucokinase activator, and **sitagliptin**, a dipeptidyl peptidase-4 (DPP-4) inhibitor. Both are **oral small molecule** antidiabetic agents. **Dorzagliatin** enhances glucose homeostasis by selectively activating glucokinase in the pancreas and liver, restoring impaired glucose sensing, promoting insulin secretion, and increasing GLP-1 secretion in a glucose-dependent manner. **Sitagliptin** inhibits DPP-4, blocking incretin (GLP-1 and GIP) degradation, which also boosts insulin secretion and lowers glucagon during hyperglycemia. Combined, these drugs improve blood glucose control and may provide synergistic or additive benefits in type 2 diabetes, including improved glycemic and lipid parameters based on preclinical and clinical results[1][3][4][6][7].

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)GCK (Glucokinase)

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