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Sci Adv. 2019 Sep 18;5(9):eaaw6127. doi: 10.1126/sciadv.aaw6127. eCollection 2019 Sep.
2
CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitor.CYP1A1 和 1B1 介导的多拉韦林（一种 HIV 整合酶抑制剂）的代谢途径。
Biochem Pharmacol. 2018 Dec;158:174-184. doi: 10.1016/j.bcp.2018.10.012. Epub 2018 Oct 17.
3
Identification of Novel Pathways in Idelalisib Metabolism and Bioactivation.鉴定依鲁替尼代谢和生物活化中的新途径。
Chem Res Toxicol. 2018 Jul 16;31(7):548-555. doi: 10.1021/acs.chemrestox.8b00023. Epub 2018 Jun 26.
4
Dolutegravir-Related Neurological Adverse Events: A Case Report of Successful Management with Therapeutic Drug Monitoring.多替拉韦相关的神经系统不良事件：一例通过治疗药物监测成功处理的病例报告
Curr Drug Saf. 2018;13(1):69-71. doi: 10.2174/1574886313666180116124046.
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Cost-effectiveness of public-health policy options in the presence of pretreatment NNRTI drug resistance in sub-Saharan Africa: a modelling study.撒哈拉以南非洲地区存在预处理 NNRTI 耐药性情况下的公共卫生政策选择的成本效益：建模研究。
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6
BCRP/ABCG2 and high-alert medications: Biochemical, pharmacokinetic, pharmacogenetic, and clinical implications.BCRP/ABCG2 与高危药物：生化、药代动力学、遗传药理学和临床意义。
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7
Impact of UGT1A1 gene polymorphisms on plasma dolutegravir trough concentrations and neuropsychiatric adverse events in Japanese individuals infected with HIV-1.UGT1A1基因多态性对日本HIV-1感染者血浆度鲁特韦谷浓度及神经精神不良事件的影响。
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8
High plasma concentrations of dolutegravir in patients with ABCG2 genetic variants.ABCG2基因变异患者中多替拉韦血浆浓度较高。
Pharmacogenet Genomics. 2017 Nov;27(11):416-419. doi: 10.1097/FPC.0000000000000308.
9
Adverse events of raltegravir and dolutegravir.拉替拉韦和度鲁特韦的不良事件。
AIDS. 2017 Aug 24;31(13):1853-1858. doi: 10.1097/QAD.0000000000001590.
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ABCG2 缺乏不改变多替拉韦的代谢和药代动力学。

ABCG2 Deficiency Does Not Alter Dolutegravir Metabolism and Pharmacokinetics.

机构信息

Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy (J.Z., X.T., A.I.S., X.M.) and Division of Infectious Disease, Department of Medicine (D.K.M.), University of Pittsburgh, Pittsburgh, Pennsylvania.

Center for Pharmacogenetics, Department of Pharmaceutical Sciences, School of Pharmacy (J.Z., X.T., A.I.S., X.M.) and Division of Infectious Disease, Department of Medicine (D.K.M.), University of Pittsburgh, Pittsburgh, Pennsylvania

出版信息

J Pharmacol Exp Ther. 2020 Jul;374(1):38-43. doi: 10.1124/jpet.119.264424. Epub 2020 Apr 17.

DOI:10.1124/jpet.119.264424
PMID:32303561
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7292963/
Abstract

Dolutegravir (DTG) is a potent integrase inhibitor of human immunodeficiency virus. Because DTG is a substrate of the efflux transporter ABCG2 and ABCG2 is highly polymorphic, we asked whether dose adjustment of DTG is needed for ABCG2-deficient individuals. Using Abcg2-null mice, the current work investigated the impact of ABCG2 deficiency on DTG metabolism and pharmacokinetics. Compared with wild-type mice, no statistically significant difference was found in the systemic and tissue-specific (liver, kidney, and brain) pharmacokinetics of DTG in Abcg2-null mice. In addition, ABCG2 deficiency had no statistically significant impact on the production and excretion of DTG metabolites. In summary, this study demonstrated that deficiency of ABCG2 does not alter DTG metabolism and pharmacokinetics, suggesting that dose adjustment of DTG is not needed for individuals with ABCG2 deficiency. SIGNIFICANCE STATEMENT: The current work demonstrated that deficiency of ATP-binding cassette subfamily G member 2 (ABCG2) does not alter Dolutegravir (DTG) metabolism and pharmacokinetics, suggesting that dose adjustment of DTG is not needed for individuals with ABCG2 deficiency.

摘要

多替拉韦（DTG）是一种有效的人类免疫缺陷病毒整合酶抑制剂。由于 DTG 是外排转运蛋白 ABCG2 的底物，而 ABCG2 高度多态性，我们想知道 ABCG2 缺乏的个体是否需要调整 DTG 的剂量。本研究使用 Abcg2 基因敲除小鼠，研究了 ABCG2 缺乏对 DTG 代谢和药代动力学的影响。与野生型小鼠相比，Abcg2 基因敲除小鼠的 DTG 全身和组织特异性（肝、肾和脑）药代动力学无统计学差异。此外，ABCG2 缺乏对 DTG 代谢物的生成和排泄也没有统计学显著影响。综上所述，本研究表明 ABCG2 缺乏不改变 DTG 的代谢和药代动力学，提示 ABCG2 缺乏的个体无需调整 DTG 剂量。

声明：本研究表明，ABCG2 缺乏不改变多替拉韦（DTG）的代谢和药代动力学，提示 ABCG2 缺乏的个体无需调整 DTG 剂量。