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Tirzepatide: a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) dual agonist in development for the treatment of type 2 diabetes

Pages 379-394 | Received 17 Jun 2020, Accepted 28 Sep 2020, Published online: 08 Oct 2020

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Juan Pablo Frías. (2023) An update on tirzepatide for the management of type 2 diabetes: a focus on the phase 3 clinical development program. Expert Review of Endocrinology & Metabolism 18:2, pages 111-130.
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Lina Naseralallah & Bodoor Aboujabal. (2023) Profile of tirzepatide in the management of type 2 diabetes mellitus: design, development, and place in therapy. Expert Opinion on Pharmacotherapy 24:4, pages 407-418.
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Bin Yang, Ana Gomes Dos Santos, Sanyogitta Puri, Annette Bak & Liping Zhou. (2022) The industrial design, translation, and development strategies for long-acting peptide delivery. Expert Opinion on Drug Delivery 19:10, pages 1233-1245.
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Nour Zaïmia, Joelle Obeid, Annie Varrault, Julia Sabatier, Christophe Broca, Patrick Gilon, Safia Costes, Gyslaine Bertrand & Magalie A. Ravier. (2023) GLP-1 and GIP receptors signal through distinct β-arrestin 2-dependent pathways to regulate pancreatic β cell function. Cell Reports 42:11, pages 113326.
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Chiara Ruocco, Alexis Elias Malavazos, Maurizio Ragni, Michele O. Carruba, Alessandra Valerio, Gianluca Iacobellis & Enzo Nisoli. (2023) Amino acids contribute to adaptive thermogenesis. New insights into the mechanisms of action of recent drugs for metabolic disorders are emerging. Pharmacological Research 195, pages 106892.
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Ana Luiza Arruda, April Hartley, Georgia Katsoula, George Davey Smith, Andrew P. Morris & Eleftheria Zeggini. (2023) Genetic underpinning of the comorbidity between type 2 diabetes and osteoarthritis. The American Journal of Human Genetics 110:8, pages 1304-1318.
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Dimitrios Patoulias, Athina Dimosiari & Nikolaos Fragakis. (2023) Tirzepatide for the treatment of heart failure in Type 2 diabetes mellitus: (SUR)PASS, or not?. Future Cardiology.
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Tito Borner, Benjamin C. Reiner, Richard C. Crist, C. Daniel Furst, Sarah A. Doebley, Julia G. Halas, Minrong Ai, Ricardo J. Samms, Bart C. De Jonghe & Matthew R. Hayes. (2023) GIP receptor agonism blocks chemotherapy-induced nausea and vomiting. Molecular Metabolism 73, pages 101743.
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Yaochen Xie, Qian Zhou, Qiaojun He, Xiaoyi Wang & Jincheng Wang. (2023) Opportunities and challenges of incretin-based hypoglycemic agents treating type 2 diabetes mellitus from the perspective of physiological disposition. Acta Pharmaceutica Sinica B 13:6, pages 2383-2402.
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Mariana Abdel-Malek, Lisa Yang & Alexander Dimitri Miras. (2023) Pharmacotherapy for chronic obesity management: a look into the future. Internal and Emergency Medicine 18:4, pages 1019-1030.
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Fei Lin, Bin Yu, Baodong Ling, Guangyao Lv, Huijun Shang, Xia Zhao, Xiaoling Jie, Jing Chen & Yan Li. (2023) Weight loss efficiency and safety of tirzepatide: A Systematic review. PLOS ONE 18:5, pages e0285197.
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Rachel Sinha, Dimitris Papamargaritis, Jack A. Sargeant & Melanie J. Davies. (2023) Efficacy and Safety of Tirzepatide in Type 2 Diabetes and Obesity Management. Journal of Obesity & Metabolic Syndrome 32:1, pages 25-45.
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Mads M Helsted, Lærke S Gasbjerg, Tina Vilsbøll, Casper K Nielsen, Julie L Forman, Mikkel B Christensen & Filip K Knop. (2023) Separate and combined effects of long-term GIP and GLP-1 receptor activation in patients with type 2 diabetes: a structured summary of a study protocol for a double-blind, randomised, placebo-controlled clinical trial. BMJ Open 13:2, pages e065736.
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Giovanni Targher, Alessandro Mantovani & Christopher D Byrne. (2023) Mechanisms and possible hepatoprotective effects of glucagon-like peptide-1 receptor agonists and other incretin receptor agonists in non-alcoholic fatty liver disease. The Lancet Gastroenterology & Hepatology 8:2, pages 179-191.
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Caroline E. Geisler, Meghan P. Antonellis, Wolfgang Trumbauer, Jennifer A. Martin, Tamer Coskun, Ricardo J. Samms & Matthew R. Hayes. (2022) Tirzepatide suppresses palatable food intake by selectively reducing preference for fat in rodents. Diabetes, Obesity and Metabolism 25:1, pages 56-67.
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Amrit Bhusal. (2023) Advent of tirzepatide: boon for diabetic and obese?. Annals of Medicine & Surgery 85:2, pages 71-72.
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Imma Forzano, Fahimeh Varzideh, Roberta Avvisato, Stanislovas S. Jankauskas, Pasquale Mone & Gaetano Santulli. (2022) Tirzepatide: A Systematic Update. International Journal of Molecular Sciences 23:23, pages 14631.
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Liliane El Eid, Christopher A. Reynolds, Alejandra Tomas & Ben Jones. (2022) Biased agonism and polymorphic variation at the GLP-1 receptor: Implications for the development of personalised therapeutics. Pharmacological Research 184, pages 106411.
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Ricardo J. Samms, GuoFang Zhang, Wentao He, Olga Ilkayeva, Brian A. Droz, Steven M. Bauer, Cynthia Stutsman, Valentina Pirro, Kyla A. Collins, Ellen C. Furber, Tamer Coskun, Kyle W. Sloop, Joseph T. Brozinick & Christopher B. Newgard. (2022) Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue. Molecular Metabolism 64, pages 101550.
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Rouchan Ali, Sharma Arvind Virendra & Pooja A Chawla. (2022) Bumps and humps in the success of Tirzepatide as the first GLP1 and GIP receptor agonist. Health Sciences Review 4, pages 100032.
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Tamer Coskun, Shweta Urva, William C. Roell, Hongchang Qu, Corina Loghin, Julie S. Moyers, Libbey S. O’Farrell, Daniel A. Briere, Kyle W. Sloop, Melissa K. Thomas, Valentina Pirro, David B. Wainscott, Francis S. Willard, Matthew Abernathy, LaRonda Morford, Yu Du, Charles Benson, Ruth E. Gimeno, Axel Haupt & Zvonko Milicevic. (2022) LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metabolism 34:9, pages 1234-1247.e9.
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Vivek P. Chavda, Jinal Ajabiya, Divya Teli, Joanna Bojarska & Vasso Apostolopoulos. (2022) Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review. Molecules 27:13, pages 4315.
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Natasha P Malkani & Vanita R Aroda. (2022) SURPASSing the current dogma: is our framework shifting?. The Lancet Diabetes & Endocrinology 10:6, pages 375-376.
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Bingfa Sun, Francis S. Willard, Dan Feng, Jorge Alsina-Fernandez, Qi Chen, Michal Vieth, Joseph D. Ho, Aaron D. Showalter, Cynthia Stutsman, Liyun Ding, Todd M. Suter, James D. Dunbar, John W. Carpenter, Faiz Ahmad Mohammed, Eitaro Aihara, Robert A. Brown, Ana B. Bueno, Paul J. Emmerson, Julie S. Moyers, Tong Sun Kobilka, Matthew P. Coghlan, Brian K. Kobilka & Kyle W. Sloop. (2022) Structural determinants of dual incretin receptor agonism by tirzepatide. Proceedings of the National Academy of Sciences 119:13.
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Fei-Fei Xie, Yu-Fang Zhang, Yan-Fang Hu, Yun-Yun Xie, Xiao-Ying Wang, Shu-Zhen Wang & Bao-Qiang Xie. (2022) Significance of serum glucagon-like peptide-1 and matrix Gla protein levels in patients with diabetes and osteoporosis. World Journal of Clinical Cases 10:5, pages 1527-1535.
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Tito Borner, Ian C. Tinsley, Robert P. Doyle, Matthew R. Hayes & Bart C. De Jonghe. (2021) Glucagon‐like peptide‐1 in diabetes care: Can glycaemic control be achieved without nausea and vomiting?. British Journal of Pharmacology 179:4, pages 542-556.
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Neil Tanday, Peter R. Flatt & Nigel Irwin. (2021) Metabolic responses and benefits of glucagon‐like peptide‐1 (GLP‐1) receptor ligands. British Journal of Pharmacology 179:4, pages 526-541.
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Renata Spezani & Carlos Alberto Mandarim-de-Lacerda. (2022) The current significance and prospects for the use of dual receptor agonism GLP-1/Glucagon. Life Sciences 288, pages 120188.
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Akshaya Srikanth Bhagavathula, Kota Vidyasagar & Wubshet Tesfaye. (2021) Efficacy and Safety of Tirzepatide in Patients with Type 2 Diabetes Mellitus: A Systematic Review and Meta-Analysis of Randomized Phase II/III Trials. Pharmaceuticals 14:10, pages 991.
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Safia Costes, Gyslaine Bertrand & Magalie A. Ravier. (2021) Mechanisms of Beta-Cell Apoptosis in Type 2 Diabetes-Prone Situations and Potential Protection by GLP-1-Based Therapies. International Journal of Molecular Sciences 22:10, pages 5303.
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Mohamed Suliman & NagiHashim Mohammed. (2021) Conference highlights: The 81 st Annual (Virtual) conference of the American diabetes association: June 25–29, 2021 . Journal of Diabetes and Endocrine Practice 4:3, pages 143.
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Najeeb Shah, Mohammed Altigani Abdalla, Harshal Deshmukh & Thozhukat Sathyapalan. (2021) Therapeutics for type-2 diabetes mellitus: a glance at the recent inclusions and novel agents under development for use in clinical practice. Therapeutic Advances in Endocrinology and Metabolism 12, pages 204201882110421.
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K. Clément & O. Ziegler. 2021. Les Obésités. Les Obésités 663 672 .

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