Tirzepatide
An extensively studied dual GIP/GLP-1 receptor agonist with a novel mechanism engaging two incretin pathways simultaneously. Research has investigated its dual receptor pharmacology and effects on metabolic signaling.
From ReVia
Mechanism of Action
Tirzepatide is a synthetic peptide that activates both the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. It is based on the native GIP sequence with modifications to enable GLP-1 receptor cross-reactivity and a C20 fatty diacid moiety for albumin binding and extended half-life. GIP receptor agonism enhances the metabolic signaling effects of GLP-1 pathway activation, including modulation of lipid metabolism and central satiety signaling pathways. The dual mechanism engages complementary metabolic pathways compared to single-receptor agonist approaches.
Research Applications
- Studies have investigated dual incretin receptor pharmacology and metabolic pathway modulation
- Research has examined glycemic signaling in dual-agonist receptor activation models
- Studies have explored effects on hepatic lipid metabolism and steatosis biomarkers
- Research has investigated cardiovascular biomarkers and respiratory signaling pathways
Key Published Studies
Jastreboff AM, et al. Tirzepatide once weekly for the treatment of obesity. N Engl J Med. 2022;387(3):205-216.
Key finding: Research investigated the dose-dependent pharmacology of dual GIP/GLP-1 receptor agonism and its effects on metabolic signaling pathways over 72 weeks, comparing dual-receptor engagement to single-agonist approaches.
Frias JP, et al. Tirzepatide versus semaglutide once weekly in patients with type 2 diabetes. N Engl J Med. 2021;385(6):503-515.
Key finding: Research compared the receptor pharmacology and glycemic signaling effects of dual GIP/GLP-1 agonism versus selective GLP-1 receptor agonism across multiple dose groups.
Chemical Properties
- Type
- Peptide (dual GIP/GLP-1 agonist)
- CAS Number
- 2023788-19-2
Research Use Only (RUO): This page summarizes published scientific research and is provided for educational and informational purposes only. It is not intended as medical advice, diagnosis, or treatment recommendations. The compound described carries a Research Use Only designation and is intended for laboratory research use only. It is not intended for human or animal consumption, or for use in the diagnosis, treatment, cure, or prevention of any disease. Consult qualified professionals before making any health-related decisions.