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1
Implications for the future of the HIV epidemic if drug resistance against dolutegravir cannot occur in first-line therapy.如果一线治疗中不会出现对多替拉韦的耐药性，对HIV流行趋势未来的影响。
J Int AIDS Soc. 2015 Dec 4;18(1):20824. doi: 10.7448/IAS.18.1.20824. eCollection 2015.
2
First case of Dolutegravir and Darunavir/r multi drug-resistant HIV-1 in Cameroon following exposure to Raltegravir: lessons and implications in the era of transition to Dolutegravir-based regimens.喀麦隆首例拉替拉韦暴露后多药物耐药 HIV-1 型病毒（达芦那韦/利托那韦）：在向基于多替拉韦方案过渡时代的经验与启示。
Antimicrob Resist Infect Control. 2020 Aug 26;9(1):143. doi: 10.1186/s13756-020-00799-2.
3
Dolutegravir-Selected HIV-1 Containing the N155H and R263K Resistance Substitutions Does Not Acquire Additional Compensatory Mutations under Drug Pressure That Lead to Higher-Level Resistance and Increased Replicative Capacity.含有N155H和R263K耐药性替代的多替拉韦选择的HIV-1在药物压力下不会获得导致更高水平耐药性和复制能力增加的额外补偿性突变。
J Virol. 2015 Oct;89(20):10482-8. doi: 10.1128/JVI.01725-15. Epub 2015 Aug 5.
4
Viral suppression and HIV-1 drug resistance 1 year after pragmatic transitioning to dolutegravir first-line therapy in Malawi: a prospective cohort study.马拉维采用实用方法将多替拉韦作为一线治疗方案 1 年后的病毒抑制和 HIV-1 耐药情况：一项前瞻性队列研究。
Lancet HIV. 2022 Aug;9(8):e544-e553. doi: 10.1016/S2352-3018(22)00136-9.
5
Clinical benefit of dolutegravir in HIV-1 management related to the high genetic barrier to drug resistance.多替拉韦在 HIV-1 管理方面的临床获益与药物耐药的高遗传屏障有关。
Virus Res. 2017 Jul 15;239:1-9. doi: 10.1016/j.virusres.2016.07.006. Epub 2016 Jul 12.
6
Efficacy and safety of dolutegravir or darunavir in combination with lamivudine plus either zidovudine or tenofovir for second-line treatment of HIV infection (NADIA): week 96 results from a prospective, multicentre, open-label, factorial, randomised, non-inferiority trial.多替拉韦或达芦那韦联合拉米夫定加齐多夫定或替诺福韦用于治疗 HIV 感染的二线治疗的疗效和安全性（NADIA）：一项前瞻性、多中心、开放标签、析因、随机、非劣效性试验的第 96 周结果。
Lancet HIV. 2022 Jun;9(6):e381-e393. doi: 10.1016/S2352-3018(22)00092-3. Epub 2022 Apr 20.
7
Dolutegravir versus ritonavir-boosted lopinavir both with dual nucleoside reverse transcriptase inhibitor therapy in adults with HIV-1 infection in whom first-line therapy has failed (DAWNING): an open-label, non-inferiority, phase 3b trial.多替拉韦与利托那韦增强洛匹那韦联合双核苷逆转录酶抑制剂治疗在一线治疗失败的 HIV-1 感染成人中的疗效（DAWNING）：一项开放标签、非劣效性、3b 期临床试验。
Lancet Infect Dis. 2019 Mar;19(3):253-264. doi: 10.1016/S1473-3099(19)30036-2. Epub 2019 Feb 4.
8
Dolutegravir for first-line antiretroviral therapy in low-income and middle-income countries: uncertainties and opportunities for implementation and research.多替拉韦用于中低收入国家的一线抗逆转录病毒治疗：实施和研究的不确定性和机遇。
Lancet HIV. 2018 Jul;5(7):e400-e404. doi: 10.1016/S2352-3018(18)30093-6. Epub 2018 Jun 5.
9
Mutations Located outside the Integrase Gene Can Confer Resistance to HIV-1 Integrase Strand Transfer Inhibitors.突变位于整合酶基因之外可赋予 HIV-1 整合酶链转移抑制剂耐药性。
mBio. 2017 Sep 26;8(5):e00922-17. doi: 10.1128/mBio.00922-17.
10
Limited emergence of resistance to integrase strand transfer inhibitors (INSTIs) in ART-experienced participants failing dolutegravir-based antiretroviral therapy: a cross-sectional analysis of a Northeast Nigerian cohort.在接受多替拉韦（ dolutegravir ）为基础的抗逆转录病毒治疗失败的 ART 经验丰富的参与者中，整合酶链转移抑制剂（INSTIs）耐药性的出现有限：尼日利亚东北部队列的一项横断面分析。
J Antimicrob Chemother. 2023 Aug 2;78(8):2000-2007. doi: 10.1093/jac/dkad195.

引用本文的文献

1
7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir.7 步流合成 HIV 整合酶抑制剂多替拉韦。
Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7181-7185. doi: 10.1002/anie.201802256. Epub 2018 May 14.
2
The latest evidence for possible HIV-1 curative strategies.关于可能的HIV-1治愈策略的最新证据。
Drugs Context. 2018 Feb 21;7:212522. doi: 10.7573/dic.212522. eCollection 2018.
3
Genotypic and Phylogenetic Insights on Prevention of the Spread of HIV-1 and Drug Resistance in "Real-World" Settings.在“真实世界”环境中预防 HIV-1 传播和耐药性的基因和系统发育分析。
Viruses. 2017 Dec 28;10(1):10. doi: 10.3390/v10010010.
4
Dolutegravir-lamivudine as initial therapy in HIV-1 infected, ARV-naive patients, 48-week results of the PADDLE (Pilot Antiretroviral Design with Dolutegravir LamivudinE) study.多替拉韦-拉米夫定作为初治的HIV-1感染且未接受抗逆转录病毒治疗患者的初始治疗方案：PADDLE（多替拉韦-拉米夫定先导抗逆转录病毒设计）研究的48周结果
J Int AIDS Soc. 2017 May 9;20(1):21678. doi: 10.7448/IAS.20.01.21678.
5
The R263K Dolutegravir Resistance-Associated Substitution Progressively Decreases HIV-1 Integration.R263K多替拉韦耐药相关替代突变会逐渐降低HIV-1整合。
mBio. 2017 Apr 4;8(2):e00157-17. doi: 10.1128/mBio.00157-17.
6
Quantitative evaluation of the antiretroviral efficacy of dolutegravir.评价度鲁特韦抗逆转录病毒疗效的定量研究。
JCI Insight. 2016 Nov 17;1(19):e90033. doi: 10.1172/jci.insight.90033.
7
Polymorphic substitution E157Q in HIV-1 integrase increases R263K-mediated dolutegravir resistance and decreases DNA binding activity.HIV-1整合酶中的多态性替代E157Q增加了R263K介导的多替拉韦耐药性并降低了DNA结合活性。
J Antimicrob Chemother. 2016 Aug;71(8):2083-8. doi: 10.1093/jac/dkw109. Epub 2016 Apr 15.

本文引用的文献

1
Dolutegravir-lamivudine as initial therapy in HIV-1 infected, ARV-naive patients, 48-week results of the PADDLE (Pilot Antiretroviral Design with Dolutegravir LamivudinE) study.多替拉韦-拉米夫定作为初治的HIV-1感染且未接受抗逆转录病毒治疗患者的初始治疗方案：PADDLE（多替拉韦-拉米夫定先导抗逆转录病毒设计）研究的48周结果
J Int AIDS Soc. 2017 May 9;20(1):21678. doi: 10.7448/IAS.20.01.21678.
2
Hit me with your best shot: dolutegravir - a space in the next WHO guidelines?向我发起最有力的一击：多替拉韦——在世卫组织的下一轮指南中会有一席之地吗？
AIDS. 2015 Oct 23;29(16):2067-70. doi: 10.1097/QAD.0000000000000813.
3
Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence.对整合酶链转移抑制剂的耐药性及其与HIV持续存在的相关性。
Viruses. 2015 Jul 7;7(7):3703-18. doi: 10.3390/v7072790.
4
In vitro activity of dolutegravir against wild-type and integrase inhibitor-resistant HIV-2.多替拉韦对野生型和整合酶抑制剂耐药HIV-2的体外活性。
Retrovirology. 2015 Feb 5;12:10. doi: 10.1186/s12977-015-0146-8.
5
Dolutegravir in HIV-2-Infected Patients With Resistant Virus to First-line Integrase Inhibitors From the French Named Patient Program.法国患者计划中一线整合酶抑制剂耐药的 HIV-2 感染者使用度鲁特韦的情况。
Clin Infect Dis. 2015 May 15;60(10):1521-7. doi: 10.1093/cid/civ124. Epub 2015 Feb 17.
6
Differential effects of the G118R, H51Y, and E138K resistance substitutions in different subtypes of HIV integrase.HIV整合酶不同亚型中G118R、H51Y和E138K耐药性替代的差异效应
J Virol. 2015 Mar;89(6):3163-75. doi: 10.1128/JVI.03353-14. Epub 2014 Dec 31.
7
Dolutegravir versus placebo in subjects harbouring HIV-1 with integrase inhibitor resistance associated substitutions: 48-week results from VIKING-4, a randomized study.多替拉韦与安慰剂在携带具有整合酶抑制剂耐药相关替代位点的HIV-1感染者中的比较：随机研究VIKING-4的48周结果
Antivir Ther. 2015;20(3):343-8. doi: 10.3851/IMP2878. Epub 2014 Oct 16.
8
Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naive adults with HIV-1 infection (FLAMINGO): 48 week results from the randomised open-label phase 3b study.在初治 HIV-1 感染的成人中，每日一次多替拉韦与达芦那韦/利托那韦比较（FLAMINGO）：随机、开放标签、3b 期研究的 48 周结果。
Lancet. 2014 Jun 28;383(9936):2222-31. doi: 10.1016/S0140-6736(14)60084-2. Epub 2014 Apr 1.
9
Dolutegravir in antiretroviral-experienced patients with raltegravir- and/or elvitegravir-resistant HIV-1: 24-week results of the phase III VIKING-3 study.多替拉韦用于既往接受抗逆转录病毒治疗且对拉替拉韦和/或埃替拉韦耐药的HIV-1患者：III期VIKING-3研究的24周结果
J Infect Dis. 2014 Aug 1;210(3):354-62. doi: 10.1093/infdis/jiu051. Epub 2014 Jan 19.
10
What if HIV were unable to develop resistance against a new therapeutic agent?如果 HIV 无法对新的治疗药物产生耐药性，会怎样？
BMC Med. 2013 Nov 22;11:249. doi: 10.1186/1741-7015-11-249.

Implications for the future of the HIV epidemic if drug resistance against dolutegravir cannot occur in first-line therapy.

作者信息

Wainberg Mark A, Mesplede Thibault

机构信息

McGill University AIDS Centre, Jewish General Hospital, Montreal, QC, Canada;

McGill University AIDS Centre, Jewish General Hospital, Montreal, QC, Canada.

出版信息

J Int AIDS Soc. 2015 Dec 4;18(1):20824. doi: 10.7448/IAS.18.1.20824. eCollection 2015.

DOI:10.7448/IAS.18.1.20824
PMID:26642452
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4671285/
Abstract
摘要