Tirzepatide 5mg
$155.00
out of stock
Description
Overview
What Is Tirzepatide?
Tirzepatide is a unimolecular co-agonist of the glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors recently approved for the treatment of type 2 diabetes by the US Food and Drug Administration and the European Medicine Agency. Tirzepatide treatment results in an unprecedented improvement of glycaemic control and lowering of body weight, but the contribution of the GIP receptor-activating component of tirzepatide to these effects is uncertain. In this review, we present the current knowledge about the physiological roles of the incretin hormones GLP-1 and GIP, their receptors, and previous results of co-targeting the two incretin hormone receptors in humans. We also analyse the molecular pharmacological, preclinical, and clinical effects of tirzepatide to discuss the role of GIP receptor activation for the clinical effects of tirzepatide. Based on the available literature on the combination of GLP-1 and GIP receptor activation, tirzepatide does not seem to have a classical co-activating mode of action in humans. Rather, in vitro studies of the human GLP-1 and GIP receptors reveal a biased GLP-1 receptor activation profile and GIP receptor downregulation. Therefore, we propose three hypotheses for the mode of action of tirzepatide, which can be addressed in future, elaborate clinical trials.
Scientific Information
Glucagon-like peptide-1 (GLP-1) receptor agonists have been used extensively in the clinic and have an established safety profile in cardiovascular disease settings. For the treatment of peptide-secreting enteroendocrine cells, most research has focused on developing peptide multi-agonists as most of these cells are multihormonal. Among the various peptides secreted by enteroendocrine cells, the combination of GLP-1 and glucose-dependent insulinotropic polypeptide (GIP) is an attractive strategy for treating type 2 diabetes mellitus (T2DM) because both of these hormones have glucose-lowering actions. Tirzepatide, a synthetic peptide composed of 39 amino acids, functions as a dual receptor agonist of both the GIP and GLP-1 receptors. This unique mechanism of action has earned tirzepatide the nickname “twincretin.” Tirzepatide’s dual agonist activity may be the mechanism by which tirzepatide significantly reduces glycated hemoglobin levels and body weight in patients with T2DM as observed in phase 3 clinical trials. Besides its glucose-lowering and anti-obesity effects, tirzepatide has been reported to have potential cardiovascular benefits. In this review, we discuss the cardiovascular effects of tirzepatide based on the available preclinical and clinical data.
Research Highlights
Tirzepatide is a revolutionary medication for the treatment of type 2 diabetes. It’s given through weekly subcutaneous injections, making the dosing regimen quite convenient for patients. However, the key distinguishing feature of Tirzepatide lies in its mechanism of action. Tirzepatide is providing hope in the management of type 2 diabetes and obesity. Its ability to improve blood glucose levels, lower A1C, promote lipolysis, reduce BMI, and stimulate pancreatic insulin release positions it as a potent treatment for these interconnected health issues. While mindful of potential side effects, Tirzepatide’s advantages significantly outweigh its disadvantages, marking a substantial stride forward in the medical field.
References
- Current Knowledge on Tirzepatide – Diabetes, Obesity and Metabolism: https://dom-pubs.onlinelibrary.wiley.com/doi/abs/10.1111/dom.15216#
- Cardiovascular Effects of Tirzepatide – PubMed: https://pubmed.ncbi.nlm.nih.gov/37800107/
- Tirzepatide: A Game Changer for Type 2 Diabetes and Obesity Management – Burick Center: https://burickcenter.com/peptide-of-the-week-tirzepatide-a-game-changer-for-type-2-diabetes-and-obesity-management/
Additional information
