GPCR双靶细胞株_EN_2024/3/13_2024/3/13
Key Material Preparation of Drug Screening for Bispecific GPCR Targets
Background
In the current landscape, GLP-1R targeted drugs dominate both hypoglycemic and weight loss fields, capturing half of the market share. Moreover, there has been a significant rise in bispecific and multi-specific drugs, with targets including GLP-1R, GCGR, and GIPR, making their way into the market.
• GLP-1 (glucagon-like peptide-1), also known as intestinal stimulating insulin, correlates closely with GIP (glucose-dependent insulin-releasing peptide) and GCG (glucagon) as its targets. In pancreatic β cells, activation of GLP-1R stimulates cAMP production through Gs protein, thereby enhancing glucose-stimulated insulin secretion.
• GIPR belongs to the B1 subfamily of the GPCR (G protein-coupled receptor superfamily), consisting of an extracellular N-terminal, 7 transmembrane domains, and an intracellular C-terminal.
• GCGR, belongs to the B-class GPCRs family and plays a pivotal role in maintaining glucose homeostasis in humans.
GLP-1R marketed drug
The first and only bispecific agonist drug on the market:Tirzepatide

Tirzepatide, approved by the FDA in May 2022, is a novel drug targeting adult type 2 diabetes, acting on both GLP-1R and GIPR simultaneously. On November 8, 2023, Lilly announced that Telposide had received FDA approval for weight loss indication. In its debut year, Telposide achieved global sales of $480 million, with sales reaching to $1.548 billion in the first half of 2023, aiming for a full-year target of $4 billion. Could Telposide positively impact PK Smegglutide?
 
       Schematic diagram of GLP-1 / GIP receptor activation therapy for type 2 diabetes
 Product list

With the approval of Tirzepatide, more than 10 GLP-1 / GIP bispecific agonists have entered clinical stages worldwide. Researchers have gradually shifted their resources towards the GLP-1 / GIP bispecific direction, aiming to achieve product differentiation and unleash product potential while addressing existing clinical issues. At present, Sanyou Biopharmaceuticals offer functional cell lines targeting GLP-1R, GIPR, and GCGR, accelerating the drug development processes.