Weight Loss Blockbuster Development: A Role for Unimolecular Polypharmacology

IF 11.2 1区医学 Q1 PHARMACOLOGY & PHARMACY Annual review of pharmacology and toxicology Pub Date : 2024-09-11 DOI:10.1146/annurev-pharmtox-061324-011832

Qingtong Zhou, Guanyi Li, Kaini Hang, Jie Li, Dehua Yang, Ming-Wei Wang

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Abstract

Obesity and type 2 diabetes mellitus (T2DM) impact more than 2.5 billion adults worldwide, necessitating innovative therapeutic approaches. Unimolecular polypharmacology, which involves designing single molecules to target multiple receptors or pathways simultaneously, has revolutionized treatment strategies. Blockbuster drugs such as tirzepatide and retatrutide have shown unprecedented success in managing obesity and T2DM, demonstrating superior efficacy compared to conventional single agonists. Tirzepatide, in particular, has garnered tremendous attention for its remarkable effectiveness in promoting weight loss and improving glycemic control, while offering additional cardiovascular and renal benefits. Despite their promises, such therapeutic agents also face challenges that include gastrointestinal side effects, patient compliance issues, and body weight rebound after cessation of the treatment. Nonetheless, the development of these therapies marks a significant leap forward, underscoring the transformative potential of unimolecular polypharmacology in addressing metabolic diseases and paving the way for future innovations in personalized medicine.

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减肥大片的开发：单分子多药理学的作用

肥胖症和 2 型糖尿病（T2DM）影响着全球超过 25 亿成年人，因此需要创新的治疗方法。单分子多药理学（Unimolecular polypharmacology）涉及设计单分子同时靶向多个受体或通路，它彻底改变了治疗策略。诸如替扎帕肽（tirzepatide）和雷他鲁肽（retatrutide）等大片药物在治疗肥胖症和 T2DM 方面取得了前所未有的成功，与传统的单一激动剂相比，疗效更加显著。尤其是替哌肽，它在促进减肥和改善血糖控制方面效果显著，同时还能为心血管和肾脏带来额外的益处，因此受到了极大的关注。尽管这类治疗药物前景广阔，但也面临着一些挑战，包括胃肠道副作用、患者依从性问题以及停止治疗后体重反弹等。不过，这些疗法的开发标志着一个重大飞跃，凸显了单分子多药理学在解决代谢性疾病方面的变革潜力，并为未来个性化医学的创新铺平了道路。

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来源期刊

Annual review of pharmacology and toxicology 医学-毒理学

CiteScore

27.80

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0.00%

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期刊介绍： Since 1961, the Annual Review of Pharmacology and Toxicology has been a comprehensive resource covering significant developments in pharmacology and toxicology. The journal encompasses various aspects, including receptors, transporters, enzymes, chemical agents, drug development science, and systems like the immune, nervous, gastrointestinal, cardiovascular, endocrine, and pulmonary systems. Special topics are also featured in this annual review.

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