MC4R Antagonists: A Promising New Hope for the Treatment of Cachexia and Wasting Diseases

Melanocortin-4 receptor (MC4R) is a key receptor in the hypothalamus regulating appetite and energy metabolism. Research has indicated that MC4R agonists have demonstrated potential for weight loss; its antagonists may stimulate appetite and weight gain, showing potential therapeutic applications in patients with anorexia or cachexia or those requiring weight restoration. However, the signaling mechanism, clinical applications, and safety profile of MC4R antagonists still require in-depth investigation. The purpose of this review is to comprehensively summarize the research progress of MC4R antagonists, analyze their mechanism of action and clinical applications, evaluate their safety profile, and explore future research directions. Future studies should focus on developing safer and more effective MC4R antagonists and exploring the therapeutic potential of MC4R in other diseases.

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Publication Details

Journal
˜Die œPharmazie
Published
2026-04-27
DOI
https://doi.org/10.31083/pharmazie51802
Primary Topic
Regulation of Appetite and Obesity
Type
article
Field-Weighted Citation Impact
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article

MC4R Antagonists: A Promising New Hope for the Treatment of Cachexia and Wasting Diseases

Jiaying Xiong, Yuehua Chen, Chao Hao, Ling Huang et al.
˜Die œPharmazie
Regulation of Appetite and Obesity
article

MC4R Antagonists: A Promising New Hope for the Treatment of Cachexia and Wasting Diseases

Jiaying Xiong, Yuehua Chen, Chao Hao, Ling Huang, Jiajia Shi
article en

Abstract

Melanocortin-4 receptor (MC4R) is a key receptor in the hypothalamus regulating appetite and energy metabolism. Research has indicated that MC4R agonists have demonstrated potential for weight loss; its antagonists may stimulate appetite and weight gain, showing potential therapeutic applications in patients with anorexia or cachexia or those requiring weight restoration. However, the signaling mechanism, clinical applications, and safety profile of MC4R antagonists still require in-depth investigation. The purpose of this review is to comprehensively summarize the research progress of MC4R antagonists, analyze their mechanism of action and clinical applications, evaluate their safety profile, and explore future research directions. Future studies should focus on developing safer and more effective MC4R antagonists and exploring the therapeutic potential of MC4R in other diseases.

˜Die œPharmazieVol. 81(1-4)
Jiangsu University (CN), Guangxi University of Science and Technology (CN), Wuhan College (CN)
Openalex Percentile: Top 10%
Regulation of Appetite and Obesity
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