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GLP-1RA + tesaglitazar
- Development stage
- Preclinical
- Lead developer
- Helmholtz Munich
- Modality
- Peptides, Small Molecules
- Administration
- Subcutaneous
01
Overview
GLP-1RA + tesaglitazar is a novel, covalently linked conjugate of a glucagon-like peptide 1 receptor agonist (GLP-1RA) and the dual peroxisome proliferator-activated receptor alpha/gamma (PPARα/γ) agonist tesaglitazar. This combination is designed to leverage the glucose-lowering and weight-reducing effects of GLP-1RAs with the insulin-sensitizing and lipid-modulating actions of tesaglitazar. By linking these two agents, tesaglitazar is selectively delivered to tissues expressing the GLP-1 receptor, thereby enhancing efficacy in glucose control while reducing off-target adverse effects associated with systemic exposure to tesaglitazar alone. Preclinical studies have demonstrated that this conjugate improves body weight, food intake, and glucose metabolism more effectively than either component alone in obese animal models. The approach aims to provide acute treatment for hyperglycemia and insulin resistance with reduced risk of side effects such as kidney damage that limited previous development of standalone PPARα/γ agonists[1][2][5].
- Other names
- GLP-1RA/tesaglitazar
02
Targets
PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)GLP1R (GLP-1R)
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