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Tirzepatide: A Novel Dual GIP and GLP-1 Receptor Agonist

Published:November 09, 2022DOI:https://doi.org/10.1016/j.nurpra.2022.10.003
      Diabetes-related mortality rates are approximately 11.3% worldwide.
      • Saeedi P.
      • Salpea P.
      • Karuranga S.
      • et al.
      Mortality attributable to diabetes in 20–79 years old adults, 2019 estimates: Results from the International Diabetes Federation Diabetes Atlas.
      Prevention and delay of diabetes-related complications is of utmost importance to improving outcomes associated with this growing epidemic.
      • Saeedi P.
      • Salpea P.
      • Karuranga S.
      • et al.
      Mortality attributable to diabetes in 20–79 years old adults, 2019 estimates: Results from the International Diabetes Federation Diabetes Atlas.
      ,
      • Chavda V.P.
      • Ajabiya J.
      • Teli D.
      • Bojarska J.
      • Apostolopoulos V.
      Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: a mini-review.
      In the armory of available drug options to manage this health condition and improve glycemic control are incretin mimetics. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are incretin hormones produced in the intestines secondary to food consumption and stimulate insulin secretion from the pancreas in a glucose-dependent manner.
      • Chavda V.P.
      • Ajabiya J.
      • Teli D.
      • Bojarska J.
      • Apostolopoulos V.
      Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: a mini-review.
      ,
      • Fisman E.Z.
      • Tenenbaum A.
      The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect.
      These hormones also inhibit glucagon secretion, delay gastric emptying, and promote satiety. The effects of GLP-1 and GIP are relatively short-lived with its metabolism and deactivation by an enzyme known as dipeptidyl peptidase 4. Targeting the incretin effect led to the development of GLP-1 receptor agonists and dipeptidyl peptidase 4 inhibitors.
      • Fisman E.Z.
      • Tenenbaum A.
      The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect.
      Tirzepatide (Mounjaro™; see Table) is the latest incretin-based pharmacotherapy option available for the management of type 2 diabetes mellitus (T2DM). Also referred to as a “twin-cretin,” it acts as a dual GLP-1 and GIP receptor agonist to increase insulin secretion, decrease glucagon levels, decrease fasting and postprandial glucose concentrations, promote weight loss, and reduce food intake.
      • Chavda V.P.
      • Ajabiya J.
      • Teli D.
      • Bojarska J.
      • Apostolopoulos V.
      Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: a mini-review.
      ,
      Notably, tirzepatide is the first-in-class drug that binds to both incretin hormones to improve glucose homeostasis in adult patients as a once-weekly subcutaneous injection.
      • Chavda V.P.
      • Ajabiya J.
      • Teli D.
      • Bojarska J.
      • Apostolopoulos V.
      Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: a mini-review.
      • Fisman E.Z.
      • Tenenbaum A.
      The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect.
      TableHighlights of Tirzepatide
      • Novel dual GLP-1 and GIP analog that promotes glucose homeostasis
      • Decreases fasting and postprandial glucose concentrations, promotes weight loss, and reduces food intake
      • Administered subcutaneously and once weekly without regards to meals
      • US Food and Drug Administration approved as an adjunct to diet and exercise for the management of adult patients with type 2 diabetes mellitus
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      References

        • Saeedi P.
        • Salpea P.
        • Karuranga S.
        • et al.
        Mortality attributable to diabetes in 20–79 years old adults, 2019 estimates: Results from the International Diabetes Federation Diabetes Atlas.
        Diabetes Res Clin Pract. 2020; 162 (9th edition): 108086https://doi.org/10.1016/j.diabres.2020.108086
        • Chavda V.P.
        • Ajabiya J.
        • Teli D.
        • Bojarska J.
        • Apostolopoulos V.
        Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: a mini-review.
        Molecules. 2022; 27: 4315https://doi.org/10.3390/molecules27134315
        • Fisman E.Z.
        • Tenenbaum A.
        The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect.
        Cardiovasc Diabetol. 2021; 20: 225https://doi.org/10.1186/s12933-021-01412-5
      1. Mounjaro™ (tirzepatide) injection [prescribing information]. Indianapolis. Eli Lilly and Company, 2022
        • Rosenstock J.
        • Wysham C.
        • Frías J.P.
        • et al.
        Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial.
        Lancet. 2021; 398: 143-155https://doi.org/10.1016/S0140-6736(21)01324-6
        • Jastreboff A.M.
        • Aronne L.J.
        • Ahmad N.N.
        • et al.
        SURMOUNT-1 Investigators. Tirzepatide once weekly for the treatment of obesity.
        N Engl J Med. 2022; 387: 205-216https://doi.org/10.1056/NEJMoa2206038
        • American Diabetes Association Professional Practice Committee; 9
        Pharmacologic approaches to glycemic treatment: Standards of Medical Care in Diabetes—2022.
        Diabetes Care. 2022; 45: S125-S143https://doi.org/10.2337/dc22-S009

      Biography

      Elaine Wong, PharmD, MBA, BCPS, BC-ADM, is a Professor of Pharmacy Practice at the Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University in Brooklyn, New York. Dr. Wong can be reached at [email protected] .