The incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are responsible for up to 65% of postprandial insulin secretion. Tirzepatide, developed by Eli Lilly, is a dual GIP/GLP-1 receptor agonist in the form of a synthetic linear peptide; its acylation technology allows it to bind to albumin, thus making it possible to dose the drug once a week. This review summarizes the key characteristics and pharmacokinetics of tirzepatide. The authors present the results of a phase 1, 2, and 3 clinical trial on the effects of tirzepatide on glycaemic and lipid control and the beneficial effects on body weight in a dose-dependent manner in patients with type 2 diabetes mellitus (T2DM). Tirzepatide has the ability to reduce glycaemic levels, improve insulin sensitivity, reduce body weight, and improve lipid metabolism, which is critically important in T2DM. Tirzepatide administered by weekly subcutaneous injections appears to be a promising drug for the treatment of T2DM as well as cardiometabolic disorders. The mechanism of action and safety profile of tirzepatide potentially fills important gaps in the current treatment of T2DM.
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http://dx.doi.org/10.5603/EP.a2022.0029 | DOI Listing |
Pharmaceuticals (Basel)
December 2024
Department of Endocrinology and Metabolism, Peking University People's Hospital, No.11 Xizhimen South Street, Xicheng District, Beijing 100044, China.
Type 2 diabetes and weight loss are associated with detrimental skeletal health. Incretin-based therapies (GLP-1 receptor agonists, and dual GIP/GLP-1 receptor agonists) are used clinically to treat diabetes and obesity. The potential effects of semaglutide and tirzepatide on bone metabolism in type 2 diabetic mice remain uncertain.
View Article and Find Full Text PDFInt Immunopharmacol
January 2025
Department of Endocrinology, Second Hospital of Shanxi Medical University, Taiyuan 030000, China. Electronic address:
Tirzepatide is a dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors and is a promising therapeutic option for type 2 diabetes mellitus (T2DM). Nevertheless, its effect and underlying mechanism on hepatic steatosis remain ambiguous. Herein, we explored the impact of tirzepatide on improving hepatic steatosis in diabetic mice, with a particular focus on the gut microbiota and bile acids (BAs) using animal models.
View Article and Find Full Text PDFObes Pillars
December 2024
Abbott Laboratories, 2900 Easton Square Place, ES1, Columbus, OH, USA.
[This corrects the article DOI: 10.1016/j.obpill.
View Article and Find Full Text PDFRev Med Liege
December 2024
Service de Diabétologie, Nutrition et Maladies métaboliques, CHU Liège, Belgique.
Tirzepatide is a unimolecular dual agonist of both glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors, which has been developed as once-weekly injection first for the treatment of type 2 diabetes (T2DM), then for the treatment of obesity. Because of the complementarity of action of the two incretins, tirzepatide showed, in a dose-dependent manner (5, 10 and 15 mg), a better efficacy (greater reduction in HbA1c and body weight) compared with placebo, semaglutide 1 mg, basal insulin and preprandial boluses of insulin lispro in six studies of the SURPASS programme. In the SURMOUNT programme, tirzepatide showed a marked reduction in body weight, never reached before with a drug, among people with obesity or overweight associated with complications linked to excess weight.
View Article and Find Full Text PDFmedRxiv
November 2024
Montefiore-Einstein Cerebrovascular Research Lab, Albert Einstein College of Medicine, Bronx, NY, USA.
Introduction: Idiopathic intracranial hypertension (IIH) is a neurological disorder characterized by elevated intracranial pressure, predominantly affecting obese women of reproductive age. While GLP-1 receptor agonists have shown promise in IIH management, the potential of dual GIP/GLP-1 receptor activation through tirzepatide remains unexplored. This study aimed to evaluate tirzepatide's efficacy as an adjunctive therapy in IIH management.
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