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用于感染性疾病和神经退行性疾病的前药疗法。

Prodrug Therapies for Infectious and Neurodegenerative Diseases.

作者信息

Markovic Milica, Deodhar Suyash, Machhi Jatin, Yeapuri Pravin, Saleh Maamoon, J Edagwa Benson, Mosley Rodney Lee, Gendelman Howard E

机构信息

Department of Pharmacology and Experimental Neuroscience, College of Medicine, University of Nebraska Medical Center, Omaha, NE 68198-5880, USA.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198-5880, USA.

出版信息

Pharmaceutics. 2022 Feb 26;14(3):518. doi: 10.3390/pharmaceutics14030518.

Abstract

Prodrugs are bioreversible drug derivatives which are metabolized into a pharmacologically active drug following chemical or enzymatic modification. This approach is designed to overcome several obstacles that are faced by the parent drug in physiological conditions that include rapid drug metabolism, poor solubility, permeability, and suboptimal pharmacokinetic and pharmacodynamic profiles. These suboptimal physicochemical features can lead to rapid drug elimination, systemic toxicities, and limited drug-targeting to disease-affected tissue. Improving upon these properties can be accomplished by a prodrug design that includes the careful choosing of the promoiety, the linker, the prodrug synthesis, and targeting decorations. We now provide an overview of recent developments and applications of prodrugs for treating neurodegenerative, inflammatory, and infectious diseases. Disease interplay reflects that microbial infections and consequent inflammation affects neurodegenerative diseases and vice versa, independent of aging. Given the high prevalence, personal, social, and economic burden of both infectious and neurodegenerative disorders, therapeutic improvements are immediately needed. Prodrugs are an important, and might be said a critical tool, in providing an avenue for effective drug therapy.

摘要

前药是生物可逆的药物衍生物,在经过化学或酶修饰后会代谢成为具有药理活性的药物。这种方法旨在克服母体药物在生理条件下面临的几个障碍,这些障碍包括药物快速代谢、溶解性差、渗透性差以及药代动力学和药效学特征欠佳。这些欠佳的物理化学特性可能导致药物快速消除、全身毒性以及药物对疾病影响组织的靶向性有限。通过前药设计可以改善这些特性,前药设计包括仔细选择前体部分、连接子、前药合成以及靶向修饰。我们现在概述前药在治疗神经退行性疾病、炎症性疾病和感染性疾病方面的最新进展和应用。疾病相互作用表明,微生物感染及随之而来的炎症会影响神经退行性疾病,反之亦然,且与衰老无关。鉴于感染性疾病和神经退行性疾病的高发病率以及个人、社会和经济负担,迫切需要改进治疗方法。前药是提供有效药物治疗途径的重要工具,甚至可以说是关键工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/45e7/8953076/e488de75dfa6/pharmaceutics-14-00518-g001.jpg

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