泰国跨性别女性中基于替诺福韦艾拉酚胺口服暴露前预防（PrEP）与女性化激素疗法之间无显著药物相互作用：iFACT-3研究

No significant drug-drug interaction between oral TAF-based PrEP and feminizing hormone therapy among transgender women in Thailand: the iFACT-3 study.

作者信息

Hiransuthikul Akarin, Thammajaruk Narukjaporn, Kerr Stephen, Janamnuaysook Rena, Nonenoy Siriporn, Hongchookiat Piranun, Trichavaroj Rapee, Tawon Yardpiroon, Boonruang Jakkrapatara, Teeratakulpisarn Nipat, Cressey Tim R, Anderson Peter L, Phanuphak Nittaya

机构信息

Institute of HIV Research and Innovation (IHRI), Bangkok, Thailand.

Department of Preventive and Social Medicine, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand.

出版信息

J Int AIDS Soc. 2025 May;28(5):e26502. doi: 10.1002/jia2.26502.

DOI:10.1002/jia2.26502

PMID:40390323

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12089648/

Abstract

INTRODUCTION

Concerns regarding potential drug-drug interaction (DDI) between feminizing hormone therapy (FHT) and HIV pre-exposure prophylaxis (PrEP) may hinder PrEP use among transgender women. We assessed the potential DDI between FHT and emtricitabine-tenofovir alafenamide (F/TAF)-based PrEP among transgender women.

METHODS

Transgender women without HIV who never underwent orchiectomy were enrolled between January and February 2022. Oral FHT (oestradiol valerate 2 mg and cyproterone acetate 25 mg) was initiated at baseline and continued until week 9, while oral PrEP (F/TAF 200/25 mg) was initiated at week 3 and continued until week 12. Intensive blood sampling was performed at weeks 3 and 9 to assess the impact of PrEP on FHT; and weeks 9 and 12 to assess the impact of FHT on PrEP. Pharmacokinetics (PKs) of plasma oestradiol (E2), TAF, tenofovir (TFV) and emtricitabine (FTC); urine TFV and FTC; and tenofovir-diphosphate (TFV-DP) and emtricitabine-triphosphate (FTC-TP) in peripheral blood mononuclear cells (PBMCs) and rectal tissues were assessed.

RESULTS

Eighteen participants completed all PK visits. No significant differences in PK parameters for plasma E2, TAF and TFV were observed with FHT and F/TAF administration. The geometric mean of FTC AUC at week 9 was 9% lower than at week 12, but the 90% CI (0.88-0.95) remained within the 80-125% range. There were no significant differences in PBMCs and rectal tissues TFV-DP and FTC-TP concentrations when F/TAF was administered with FHT.

CONCLUSIONS

No bidirectional clinically significant DDI between FHT and F/TAF-based PrEP was observed across systemic and local tissue anatomical compartments, supporting the use of oral F/TAF-based PrEP among transgender women.

CLINICAL TRIAL NUMBER

NCT04590417.

摘要

引言

对于女性化激素疗法（FHT）与艾滋病毒暴露前预防（PrEP）之间潜在的药物相互作用（DDI）的担忧，可能会阻碍跨性别女性使用PrEP。我们评估了跨性别女性中FHT与基于恩曲他滨替诺福韦艾拉酚胺（F/TAF）的PrEP之间潜在的DDI。

方法

2022年1月至2月招募了未感染艾滋病毒且从未接受过睾丸切除术的跨性别女性。口服FHT（戊酸雌二醇2毫克和醋酸环丙孕酮25毫克）在基线时开始服用并持续至第9周，而口服PrEP（F/TAF 200/25毫克）在第3周开始服用并持续至第12周。在第3周和第9周进行密集采血，以评估PrEP对FHT的影响；在第9周和第12周进行评估，以评估FHT对PrEP的影响。评估血浆雌二醇（E2）、替诺福韦艾拉酚胺（TAF）、替诺福韦（TFV）和恩曲他滨（FTC）的药代动力学（PKs）；尿液中的TFV和FTC；以及外周血单核细胞（PBMCs）和直肠组织中的二磷酸替诺福韦（TFV-DP）和三磷酸恩曲他滨（FTC-TP）。

结果

18名参与者完成了所有PK访视。在同时给予FHT和F/TAF的情况下，未观察到血浆E2、TAF和TFV的PK参数有显著差异。第9周时FTC曲线下面积（AUC）的几何平均值比第12周时低9%，但90%置信区间（0.88 - 0.95）仍在80 - 125%范围内。当F/TAF与FHT同时给药时，PBMCs和直肠组织中TFV-DP和FTC-TP的浓度没有显著差异。