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05 / Tirzepatide

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

  • 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
  • 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
  • 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

Library

Research and Whitepapers

Tirzepatide: A Dual Incretin Agonist in Human Trials

Tirzepatide is a single 39-residue peptide that activates two incretin receptors, GIP and GLP-1. Its phase 3 trials in type 2 diabetes and obesity are among the largest in the field. It is also an approved pharmaceutical, which sets it apart from most compounds in this library.

For research purposes only. Not for human or veterinary consumption. Not for use in diagnostic, therapeutic, or clinical procedures.