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A Review on Pharmacokinetics Properties of Antiretroviral Drugs to Treat HIV-1 Infections.
Current Computer-Aided Drug Design ( IF 1.5 ) Pub Date : 2021-01-01 , DOI: 10.2174/1573409916666201006143007
Mohd Aqueel Khan 1 , Krishna Kant Gupta 2 , Sanjeev Kumar Singh 1
Affiliation  

BACKGROUND The HIV-1 pandemic is undoubtedly the major public-health crisis of our time. The extensive research on HIV has deepened our understanding of its pathogenesis and transmission dynamics. Some new entity molecules have been approved by the FDA for HIV treatment, but till now, the protective vaccine remains elusive. Scientists are targeting many important proteins of HIV-1; gp41, gp120, CCR5 coreceptor, integrase, reverse transcriptase and protease. Few compounds are used as nucleotide analogues to stop HIV replication. Altogether, these compounds and their derivatives specifically block HIV entry and DNA replication. Using ADMET studies, people are working on these compounds to reduce toxicity and increase potency. OBJECTIVES Our main aim is to discuss the Pharmacokinetics properties of 23 important FDA antiretroviral drugs used for the treatment of HIV-1 infections. METHODS We have searched literature related to pharmacokinetics properties in PubMed, Google Scholar search engine. CONCLUSION Here, we have reviewed the pharmacokinetic properties such as absorption, bioavailability, distribution, metabolism, and excretion of 23 important FDA-approved drugs. These drugs are Fuzeon, Selzentry, Complera, Epivir, Retrovir, Emtriva, Ziagen, Edurant, Intelence, Pifeltro, Sustiva, Viramune, Isentress, Genvoya, Tivicay, Reyataz, Prezista, Lexiva, Invirase, Aptivus etc. classified into five major classes: fusion inhibitors, Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), Integrase Strand transfer inhibitors (INSTIs) and Protease inhibitors (PIs). This review may be helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties.

中文翻译:

抗逆转录病毒药物治疗 HIV-1 感染的药代动力学特性综述。

背景 HIV-1 大流行无疑是我们这个时代的主要公共卫生危机。对艾滋病毒的广泛研究加深了我们对其发病机制和传播动力学的理解。一些新的实体分子已被 FDA 批准用于 HIV 治疗,但直到现在,保护性疫苗仍然难以捉摸。科学家们正在瞄准 HIV-1 的许多重要蛋白质。gp41、gp120、CCR5 辅助受体、整合酶、逆转录酶和蛋白酶。很少有化合物用作核苷酸类似物来阻止 HIV 复制。总之,这些化合物及其衍生物可特异性阻断 HIV 进入和 DNA 复制。使用 ADMET 研究,人们正在研究这些化合物以降低毒性并提高效力。目的 我们的主要目的是讨论用于治疗 HIV-1 感染的 23 种重要的 FDA 抗逆转录病毒药物的药代动力学特性。方法 我们在 PubMed、Google Scholar 搜索引擎中检索了与药代动力学特性相关的文献。结论 在此,我们回顾了 FDA 批准的 23 种重要药物的药代动力学特性,例如吸收、生物利用度、分布、代谢和排泄。这些药物是 Fuzeon、Selzentry、Complera、Epivir、Retrovir、Emtriva、Ziagen、Edurant、Intelence、Pifeltro、Sustiva、Viramune、Isentress、Genvoya、Tivicay、Reyataz、Prezista、Lexiva、Invirase、Aptivus 等。分为五个主要类别:融合抑制剂、核苷/核苷酸逆转录酶抑制剂 (NRTIs)、非核苷逆转录酶抑制剂 (NNRTIs)、整合酶链转移抑制剂 (INSTI) 和蛋白酶抑制剂 (PI)。该综述可能有助于未来开发具有改善药代动力学特性的强效抗逆转录病毒药物。
更新日期:2020-10-06
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