两种逆转录酶抑制剂，富马酸替诺福韦艾拉酚胺和富马酸替诺福韦二吡呋酯的探索性药物遗传学初步研究。
An Exploratory Pharmacogenetic Pilot Study of Two Reverse Transcriptase Inhibitors, Tenofovir Alafenamide Fumarate and Tenofovir Disoproxil Fumarate.
作者信息
Murrell Derek E, Kennard Benjamin C, Bertoni Maria E, Cluck David B, Moorman Jonathan P, Brown Stacy D, Wang Kesheng, Duffourc Michelle M, Harirforoosh Sam
机构信息
Department of Pharmaceutical Sciences, Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN, USA.
Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN, USA.
出版信息
Drugs R D. 2025 May 25. doi: 10.1007/s40268-025-00509-6.
BACKGROUND AND OBJECTIVES
The nucleoside reverse transcriptase inhibitors tenofovir alafenamide fumarate and tenofovir disoproxil fumarate are frequently employed in treating human immunodeficiency virus. Further, each form of tenofovir requires laboratory monitoring to determine efficacy and tolerability among patients. This study sought to investigate the relationship, if any, of single nucleotide polymorphisms (SNPs) and selected clinical parameters.
METHODS
The study population, predominantly Caucasian males with a median age of 53.0 years [interquartile range 46.0-59.0], was assayed for genetic variations using an iPLEX ADME PGx Pro v1.0 Panel.
RESULTS
Although several SNP relationships were found with both forms of tenofovir, many of the reported SNPs were displayed only in the comprehensive regimen grouping, making it difficult to distinguish between the two prodrug forms.
CONCLUSIONS
Being an exploratory study, the findings of this substudy serve as potential avenues for further research.
背景与目的
核苷类逆转录酶抑制剂富马酸替诺福韦艾拉酚胺和富马酸替诺福韦二吡呋酯常用于治疗人类免疫缺陷病毒。此外，每种替诺福韦形式都需要实验室监测以确定患者的疗效和耐受性。本研究旨在调查单核苷酸多态性（SNP）与选定临床参数之间的关系（若存在）。
方法
研究人群主要为年龄中位数为53.0岁[四分位间距46.0 - 59.0]的白种男性，使用iPLEX ADME PGx Pro v1.0 Panel检测基因变异。
结果
虽然发现了几种SNP与两种替诺福韦形式均有关联，但许多报道的SNP仅在综合治疗方案分组中出现，难以区分这两种前体药物形式。
结论
作为一项探索性研究，本亚组研究结果为进一步研究提供了潜在途径。
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