Case Study
Dual-Target Agonist — A New Breakthrough in Type 2 Diabetes and Obesity Treatment
Highlights
The BGM0504 (GLP-1R/GIPR Dual-Target Agonist) solves the "long-acting & high-
activity" dilemma of drugs via AI + molecular dynamics, featuring 2-3 times higher
agonistic activity than Tirzepatide and better efficacy in diabetic mouse experiments,
showing academic and clinical potential.
Project Overview
Client
Brightgene
Objective
Develop GLP-1R/GIPR Dual-Target Agonist to
improve treatment effect of diabetes and obesity
improve treatment effect of diabetes and obesity
Main Challenge
Difficult to balance half-life and activity of existing drugs (e.g., Tirzepatide).
Design Strategy /
Approach
Approach
- Adopted dual-target activation strategy, referring to Tirzepatide's clinical verification logic;
- Used molecular dynamics to find the defect that Tirzepatide's acylation side chain disrupts salt bridges;
- Optimized BGM0504 peptide sequence, repositioned acylation side chain to retain long-acting property and activity;
- Gradually verified the scheme's effectiveness through simulation, in vitro/in vivo experiments.
Key Results /
Milestones
Milestones
- K20 salt bridge is key to activity, exposing K20 can increase activity by 3 times;
Acylation side chain prolongs half-life but may disrupt activity; - At the same dose, BGM0504 has significantly better efficacy than Tirzepatide in db/db mice.
Achievements published in Nature sub-journal, widely covered by both domestic and international media, including
PR Newswire, the Associated Press, and others.View Article Details
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