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Glucagon-like Receptor Agonists

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
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Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...

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Oral Hypoglycemic Agents: Biguanides and Glitazones

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Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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Combination Therapies and Personalized Medicine

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Related Experiment Video

Updated: Jul 2, 2026

Multidisciplinary Approach to Obesity Management: A Case Report

Multidisciplinary Approach to Obesity Management: A Case Report

Published on: May 30, 2025

GLP-1-based combination strategies for weight loss: Multi-target agents and combination therapies.

Xinyao Wang¹, Rutao Lin¹, Qinmei Sun²

¹Institute of Liver Diseases, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China; Key Laboratory of Liver and Kidney Diseases, Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, China.

Pharmacological Research

|June 30, 2026

Summary

Combination therapies using glucagon-like peptide-1 receptor agonists (GLP-1RAs) offer enhanced weight loss by targeting multiple pathways. Future research aims to optimize personalized treatments and explore long-term safety and efficacy.

Keywords:

Combination therapy GLP-1 receptor agonists Multi-target agonists Obesity Weight loss

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Last Updated: Jul 2, 2026

Multidisciplinary Approach to Obesity Management: A Case Report

Multidisciplinary Approach to Obesity Management: A Case Report

Published on: May 30, 2025

An Acupoint Catgut-embedding Therapy for Treating Obesity

An Acupoint Catgut-embedding Therapy for Treating Obesity

Published on: April 4, 2025

Area of Science:

Pharmacology
Metabolic Diseases
Drug Development

Background:

Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have revolutionized obesity pharmacotherapy.
Single-target mechanisms of current GLP-1RAs present limitations for maximal weight loss.
Combination strategies targeting multiple pathways are emerging as a key area in obesity drug development.

Purpose of the Study:

To systematically review GLP-1RA-based combination weight-loss strategies.
To examine the scientific rationale and research progress in single-agent multi-target and multi-drug combination therapies.
To evaluate the efficacy and safety of these advanced weight-loss approaches.

Main Methods:

Review of scientific literature on GLP-1RA combination therapies.
Analysis of single-agent multi-target agonists (dual and triple agonists targeting receptors like GLP-1R, GIPR, GCGR, AMYR).
Evaluation of multi-drug combination therapies (free and fixed-dose combinations).

Main Results:

Single-agent multi-target agonists achieve superior weight loss via synergistic regulation of appetite, metabolism, and lipolysis.
Multi-drug combinations, both free and fixed-dose, improve weight loss and metabolic parameters.
Common side effects include gastrointestinal events; potential risks like increased heart rate and hypoglycemia require monitoring, alongside long-term thyroid and muscle safety.

Conclusions:

GLP-1RA-based combination strategies represent a significant advancement in obesity pharmacotherapy.
Personalized treatment, head-to-head comparisons, oral formulations, and long-term maintenance are crucial for future research.
These approaches hold promise for comprehensive obesity management and improved cardiometabolic health.