Tirzepatide
Available as EIRA
Molecular profile
| Sequence |
39-amino-acid synthetic peptide, backbone based on the GIP sequence, with a C20 fatty di-acid moiety conjugated via a linker at Lys20 |
| Formula |
C225H348N48O68 |
| Class |
Dual GIP and GLP-1 receptor agonist |
A single peptide that activates both the glucose-dependent insulinotropic polypeptide receptor and the GLP-1 receptor, studied in type 2 diabetes and obesity trials and approved as a pharmaceutical (Mounjaro, Zepbound). Peptheos supplies tirzepatide as a research reagent only. It is not the branded pharmaceutical and is not offered as a substitute for it.
Discovery and dual-receptor pharmacology
Tirzepatide (development code LY3298176) was characterised in a 2018 study reporting activation of both GIP and GLP-1 receptor signalling in vitro and reductions in blood glucose, body weight, and food intake in diet-induced obese mice, alongside a phase 1 readout in adults with type 2 diabetes.
Type 2 diabetes, phase 3
In SURPASS-2, an open-label 40-week phase 3 trial in 1,879 adults with type 2 diabetes on metformin, the trial examined tirzepatide at 5, 10, and 15 mg against semaglutide 1 mg, reporting greater mean reductions in glycated haemoglobin and body weight across all three doses.
Obesity, phase 3
In SURMOUNT-1, a 72-week phase 3 double-blind trial in 2,539 adults with obesity or overweight without diabetes, the trial examined 5, 10, and 15 mg once weekly against placebo, reporting mean weight reductions of 15.0%, 19.5%, and 20.9% at the three doses.
Peer-reviewed references
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Coskun T, Sloop KW, Loghin C, et al. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol Metab. 2018;18:3-14. doi.org/10.1016/j.molmet.2018.09.009
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Frias JP, Davies MJ, Rosenstock J, et al. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. N Engl J Med. 2021;385(6):503-515. doi.org/10.1056/NEJMoa2107519
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Jastreboff AM, Aronne LJ, Ahmad NN, et al. Tirzepatide Once Weekly for the Treatment of Obesity. N Engl J Med. 2022;387(3):205-216. doi.org/10.1056/NEJMoa2206038