Glucose-dependent insulinotropic polypeptide receptor therapies for the treatment of obesity, do agonists=antagonists?
Open accessAbstract
Glucose-dependent insulinotropic polypeptide receptor (GIPR) is associated with obesity in human genome-wide association studies. Similarly, mouse genetic studies indicate that loss of function alleles and glucose-dependent insulinotropic polypeptide overexpression both protect from high-fat diet–induced weight gain. Together, these data provide compelling evidence to develop therapies targeting GIPR for the treatment of obesity. Further, both antagonists and agonists alone prevent weight gain, but result in remarkable weight loss when codosed or molecularly combined with glucagon-like peptide-1 analogs preclinically. Here, we review the current literature on GIPR, including biology, human and mouse genetics, and pharmacology of both agonists and antagonists, discussing the similarities and differences between the 2 approaches. Despite opposite approaches being investigated preclinically and clinically, there may be viability of both agonists and antagonists for the treatment of obesity, and we expect this area to continue to evolve with new clinical data and molecular and pharmacological analyses of GIPR function.
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Combining a GLP-1 agonist with a GIP receptor antagonist provides more weight reduction than a selective GLP-1 receptor agonist alone.
“recent research has shown that combining a GLP-1 agonist with a GIP receptor antagonist will also provide more weight reduction than with a selective GLP-1 receptor agonist alone.152”
From GLP-1 receptor agonists and next-generation incretin-based medications: metabolic, cardiovascular, and renal benefits (2026) · cites this paper as [152]
The “Synergism of GIPR Therapeutics With GLP-1RAs” section reports greater weight loss with a GIP receptor antagonist plus a GLP-1 receptor agonist in preclinical models. The “Pharmacological Antagonism” section identifies those models as mice and obese nonhuman primates. The unqualified prediction that the combination “will” provide more weight reduction goes beyond the evidence reported here; no page number is available for these passages. (LLM, conf=0.84)
Experimental — accuracy not yet measuredGIP antagonism is a potential obesity treatment as in preclinical studies it improved the metabolic profile and reduced food intake.
“GIP antagonism is also a potential obesity treatment as in preclinical studies improved the metabolic profile and reduced food intake [54–56].”
From What is the pipeline for future medications for obesity? (2025) · cites this paper as [56]
Whole-genome association studies have shown associations between different activity levels of human GIP receptor variants and the degree of obesity.
“Whole-genome association studies have shown associations between different activity levels of human GIP receptor variants and the degree of obesity [60].”
From New Developments in Pharmacological Treatment of Obesity and Type 2 Diabetes—Beyond and within GLP-1 Receptor Agonists (2024) · cites this paper as [60]
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“GIP antagonism is also a potential obesity treatment as in preclinical studies improved the metabolic pro fi le and reduced food intake [54 – 56].”
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Killion, E. A., Chen, M., Falsey, J. R., Sivits, G., Hager, T., Atangan, L., Helmering, J., Lee, J., Li, H., Wu, B., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-18751-8 · Cited by 151 · see citing works
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Incretin Hormones and Type 2 Diabetes—Mechanistic Insights and Therapeutic Approaches
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The impact of COVID-19 on people with diabetes in Brazil
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Nauck, M. A., Tuttle, K. R., Tschöp, M. H., & Blüher, M. (2026) · The Lancet · doi:10.1016/s0140-6736(25)02105-1 · Cited by 123 · see citing works
Lu, S.-C., Chen, M., Atangan, L., Killion, E. A., Komorowski, R., Cheng, Y., Netirojjanakul, C., Falsey, J. R., Stolina, M., Dwyer, D., et al. (2021) · Cell Reports Medicine · doi:10.1016/j.xcrm.2021.100263 · Cited by 91 · see citing works
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Thondam, S. K., Cuthbertson, D. J., & Wilding, J. P. H. (2020) · Peptides · doi:10.1016/j.peptides.2019.170208 · Cited by 77 · see citing works
Frías, J. P. (2020) · Expert Review of Endocrinology & Metabolism · doi:10.1080/17446651.2020.1830759 · Cited by 73 · see citing works
The Role of GIP Receptor in the CNS for the Pathogenesis of Obesity
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GIP reduces osteoclast activity and improves osteoblast survival in primary human bone cells
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Zaffina, I., Pelle, M. C., Armentaro, G., Giofrè, F., Cassano, V., Sciacqua, A., & Arturi, F. (2023) · Frontiers in Endocrinology · doi:10.3389/fendo.2023.1095753 · Cited by 49 · see citing works
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“Whole-genome association studies have shown associations between different activity levels of human GIP receptor variants and the degree of obesity [60].”
BackgroundBoer, G. A., Keenan, S. N., Miotto, P. M., Holst, J. J., & Watt, M. J. (2021) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00646.2020 · Cited by 38 · see citing works
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- Authors
- Killion, E. A., Lu, S.-C., Fort, M., Yamada, Y., Véniant, M. M., & Lloyd, D. J.
- Affiliations
- Amgen (United States) (US)
- Akita University (JP)
- Corresponding author
- Lloyd, David J
- ORCID
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 2019-09-12
- Volume
- 41
- Issue
- 1
- Pages
- 1-21
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2972438698
- Cited by
- 94
- References
- 129
- Citations by year
- 2026: 8 · 2025: 15 · 2024: 13 · 2023: 14 · 2022: 11 · 2021: 16 · 2020: 11 · 2019: 5
- FWCI
- 1.29
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model (vor)
- Locations
- Endocrine Reviews (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
- Health Sciences › Medicine › Epidemiology › Adipokines, Inflammation, and Metabolic Diseases
- Keywords
- glucose-dependent insulinotropic polypeptide, GIP receptor, obesity, GIP receptor agonist, GIP receptor antagonist, glucagon-like peptide-1 analogues, combination therapy, weight gain, high-fat diet, loss-of-function alleles
- MeSH terms
- Animals, Humans, Obesity, Receptors, Gastrointestinal Hormone, Anti-Obesity Agents, Mice, Genome-Wide Association Study, Molecular Targeted Therapy
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