Cited by 126Pharmacology and Obesity TreatmentDiabetes Treatment and ManagementRegulation of Appetite and Obesity

The DOI matches its Crossref record; 206 of the 219 references it cites were found in a registry or an index; 112 of the 274 sources its claims cite were checked for support.

Transforming obesity: The advancement of multi-receptor drugs

Open access

Abstract

For more than a century, physicians have searched for ways to pharmacologically reduce excess body fat. The tide has finally turned with recent advances in biochemically engineered agonists for the receptor of glucagon-like peptide-1 (GLP-1) and their use in GLP-1-based polyagonists. These polyagonists reduce body weight through complementary pharmacology by incorporating the receptors for glucagon and/or the glucose-dependent insulinotropic polypeptide (GIP). In their most advanced forms, gut-hormone polyagonists achieve an unprecedented weight reduction of up to ∼20%-30%, offering a pharmacological alternative to bariatric surgery. Along with favorable effects on glycemia, fatty liver, and kidney disease, they also offer beneficial effects on the cardiovascular system and adipose tissue. These new interventions, therefore, hold great promise for the future of anti-obesity medications.

Overview

AI snapshot

Written from the paper’s full text.

TL;DR

This review traces the shift from single GLP-1 receptor agonists to unimolecular multi-receptor drugs that add GIP and/or glucagon receptor activity, reporting weight losses that approach bariatric surgery. It argues these agents also improve glycemia, fatty liver, kidney, cardiovascular and adipose outcomes, while flagging durability, tolerability, muscle loss, access and unresolved mechanism questions.

Key findings

  • Multi-receptor gut-hormone agonists can achieve roughly 20–30% weight reduction, with retatrutide (GLP-1R/GIPR/GCGR) producing ~24.2% placebo-corrected weight loss at 48 weeks in obese subjects without T2D, and tirzepatide (GLP-1R/GIPR) producing up to 20.9% weight loss at 72 weeks in SURMOUNT-1.
  • Tirzepatide showed strong glycemic effects: in SURPASS-1, ~92% of treated subjects reached HbA1c <7.0% versus 19% with placebo at 40 weeks; in SURPASS J-mono, HbA1c fell by −2.8% versus −1.3% with dulaglutide at 52 weeks.
  • GLP-1R/GCGR co-agonists also lowered weight: mazdutide reduced body weight by ~11.3% at 24 weeks in 248 overweight/obese Chinese subjects; pemvidutide gave ~10.3% placebo-corrected weight loss at 12 weeks; cotadutide reduced the urinary albumin-to-creatinine ratio by 51% after 32 days in T2D with chronic kidney disease.
  • Benefits extend beyond weight: retatrutide reduced liver fat by up to 86% over 48 weeks in a MASLD substudy, and the review reports favorable effects on glycemia, fatty liver, kidney disease, cardiovascular risk and adipose tissue across these drug classes.

Methods

  • Narrative review synthesizing preclinical and clinical literature on GLP-1, GIP and glucagon mono-, co- and triagonist peptides.
  • Evidence includes rodent and non-human primate studies plus human trials such as SURPASS, SURMOUNT, and Phase 1/2 studies of mazdutide, cotadutide, pemvidutide, tirzepatide and retatrutide, with endpoints including body weight, HbA1c, lipids, liver fat, kidney measures and adverse events.
  • No systematic search, meta-analysis or new primary data are reported.

Limitations

  • Stated: weight regain follows discontinuation of semaglutide or tirzepatide; in SURMOUNT-4, placebo-treated subjects regained 14% after prior tirzepatide-induced loss but still maintained ~10% below baseline, suggesting lifelong exposure may be needed.
  • Stated: lean/muscle mass loss is a concern, especially in older or sarcopenic patients and in lean T2D; dosing for lean T2D is unknown; supply, cost and insurance access may worsen disparities; trial cohorts need greater ethnic diversity; GIPR mechanism and glucagon’s cardiovascular risk remain unresolved.
  • Evident: as a narrative review, evidence selection is not systematic, and many cited trials are ongoing or unpublished, so conclusions may change; preclinical findings may not fully translate to humans.

Model-written summary. Check it against the paper before relying on it.

Integrity signals

Registry

Crossref · 10.1016/j.cell.2024.06.003

Cites

206 of 206 references verified0 citation errors · 0 not checkable

Statistics

Nothing to recompute.

Verification

Claims the paper makes

70 No full text of the sources · 62 Couldn’t confirm · 42 Own interpretation · 15 Partly supported · 11 Not supported · 7 No basis given · 4 Supported · 2 Not checked yet · 1 Supported so far · 1 Sources not found · accuracy not yet measured

Show all 105 claims

  • It may state two separate claims as one. 100
  • Probably not a substantial claim. 18
110 of 110
  • The authors state this as an assumption.

    The benefits of polypharmacotherapy depend on the assumption that the agents will increase weight loss through complementary pharmacology at each target receptor.

    “Importantly, the benefits of such polypharmacotherapy are not only tethered on the assumption that these agents would bolster weight loss efficacy through complementary pharmacology at each target receptor”
  • The authors state this as an assumption.

    The benefits of polypharmacotherapy also depend on the assumption that the positive glycemic and cardiovascular effects of incretins will restrain any potentially detrimental effects of GCGR agonism.

    “but also that the positive glycemic and cardiovascular effects of the incretins would restrain any potentially detrimental effects that may, or may not, reside in GCGR agonism.”
  • The paper relies on this without support.

    The body has an intrinsic drive to preserve energy and defend a higher body weight, which hinders weight loss and promotes regain.

    “The major challenge in obesity management is the system’s intrinsic drive to preserve energy to defend the higher body weight.”
  • The authors state this as an assumption.

    A single peptide with balanced activity at all three target receptors would further enhance glycemic control and accelerate weight loss, with the hope of surpassing what had already been achieved with bariatric surgery.

    “it was naturally intuitive to assume that a single peptide that displays balanced activity at all three target receptors would further enhance glycemic control and accelerate weight loss, with the hope of surpassing what had already been achieved with bariatric surgery8,76.”
  • The paper relies on this without support.

    Anti-obesity medications have high monthly costs.

    “the high monthly costs that individuals must bear”
  • The paper relies on this without support.

    The majority of health insurance plans do not cover the costs of anti-obesity medications.

    “the majority of health insurance plans do not cover the costs of anti-obesity medications”
  • The paper relies on this without support.

    Drug-induced weight loss is not exclusively due to a loss in fat mass; a significant amount of muscle loss may accompany it.

    “the degree of weight loss induced by drug treatment is not exclusively due to a loss in fat mass, rather, there is a significant amount of muscle loss that may accompany this.”
7 of 7

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

Each contradiction between two passages listed here was confirmed by an independent check.

2 of 2

Citations

Cites

Show all 219 references

Research works printed but not linked: 2

  1. von Mering, 1889, Diabetes mellitus nach Pankreasextirpation, Centralblatt Klin. Med. Leipzig, 10, 393
  2. Sanyal, 2023, Retatrutide NAFLD - Phase 2 Trial Results in Subset of Patients with Obesity and NAFLD, Abstracts from the 83rd Scientific Sessions of the American Diabetes Association, 2023

Cited by

Sorted by citations

Metadata

Authors
Kusminski, C. M., Perez-Tilve, D., Müller, T. D., DiMarchi, R. D., Tschöp, M. H., & Scherer, P. E.
Affiliations
  • The University of Texas Southwestern Medical Center (US)
  • Helmholtz Munich (DE)
  • Indiana University Bloomington (US)
Venue
Cell
Publisher
Elsevier BV
Published
2024-07
Volume
187
Issue
15
Pages
3829-3853
ISSN
0092-8674 (ISSN-L)
OpenAlex
W4400978403
Cited by
126
References
219
Citations by year
2026: 48 · 2025: 63 · 2024: 15
FWCI
7.87
Type
journal article
Language
en
Open access
Locations
  • Cell (publishedVersion, cc-by-nc-nd)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
  • Europe PMC (PubMed Central) (acceptedVersion)
  • mediaTUM – the media and publications repository of the Technical University Munich (Technical University Munich) (submittedVersion)
  • PuSH - Publication Server of Helmholtz Zentrum München (submittedVersion)
Funders
  • ERC
  • NIDDK (R01-DK131537, RC2-DK118620, R01-DK127274, R01-DK55758, R01-DK099110)
  • Deutsches Zentrum für Diabetesforschung
  • German Research Foundation (TRR152, GRK 2816/1, SFB1123)
  • California Department of Fish and Game (TRR296)
  • Novo Nordisk
  • National Institutes of Health
  • European Commission
  • NIA (P01 AG051459-06)
Topics
  • Health Sciences › Medicine › Pharmacology (medical) › Pharmacology and Obesity Treatment
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
Keywords
obesity, anti-obesity drugs, GLP-1 receptor agonists, glucagon receptor, glucose-dependent insulinotropic polypeptide, gastrointestinal hormones, weight loss, bariatric surgery alternatives, glycemia, hepatic steatosis, kidney disease, cardiovascular effects, adipose tissue
MeSH terms
Glucagon-Like Peptide-1 Receptor, Glucagon-Like Peptide-1 Receptor Agonists, Adipose Tissue, Animals, Humans, Obesity, Anti-Obesity Agents, Glucagon-Like Peptide 1

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