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离体人胎盘绒毛膜灌流模型中雷特格韦和马拉维若的胎盘转运。宫内治疗先天性巨细胞病毒感染的新视角。

Placental transfer of Letermovir & Maribavir in the ex vivo human cotyledon perfusion model. New perspectives for in utero treatment of congenital cytomegalovirus infection.

机构信息

APHP, Fetal Medicine and Obstetric Department, Necker-Enfants Malades Hospital, Paris, France.

EHU7328, IMAGINE Institute, University Paris Descartes, Paris, France.

出版信息

PLoS One. 2020 Apr 30;15(4):e0232140. doi: 10.1371/journal.pone.0232140. eCollection 2020.

Abstract

BACKGROUND

Congenital cytomegalovirus infection can lead to severe sequelae. When fetal infection is confirmed, we hypothesize that fetal treatment could improve the outcome. Maternal oral administration of an effective drug crossing the placenta could allow fetal treatment. Letermovir (LMV) and Maribavir (MBV) are new CMV antivirals, and potential candidates for fetal treatment.

METHODS

The objective was to investigate the placental transfer of LMV and MBV in the ex vivo method of the human perfused cotyledon. Term placentas were perfused, in an open-circuit model, with LMV or MBV at concentrations in the range of clinical peak plasma concentrations. Concentrations were measured using ultraperformance liquid chromatography coupled with tandem mass spectrometry. Mean fetal transfer rate (FTR) (fetal (FC) /maternal concentration), clearance index (CLI), accumulation index (AI) (retention of each drug in the cotyledon tissue) were measured. Mean FC were compared with half maximal effective concentrations of the drugs (EC50(LMV) and EC50(MBV)).

RESULTS

For LMV, the mean FC was (± standard deviation) 1.1 ± 0.2 mg/L, 1,000-fold above the EC50(LMV). Mean FTR, CLI and AI were 9 ± 1%, 35 ± 6% and 4 ± 2% respectively. For MBV, the mean FC was 1.4 ± 0.2 mg/L, 28-fold above the EC50(MBV). Mean FTR, CLI and AI were 10 ± 1%, 50 ± 7% and 2 ± 1% respectively.

CONCLUSIONS

Drugs' concentrations in the fetal side should be in the range for in utero treatment of fetuses infected with CMV as the mean FC was superior to the EC50 for both molecules.

摘要

背景

先天性巨细胞病毒感染可导致严重的后遗症。当胎儿感染被确诊时,我们假设胎儿治疗可以改善结局。母体口服能穿过胎盘的有效药物可以实现胎儿治疗。来特莫韦(LMV)和马拉韦罗(MBV)是新的 CMV 抗病毒药物,也是胎儿治疗的潜在候选药物。

方法

本研究旨在通过体外人胎盘灌流模型研究 LMV 和 MBV 在胎盘的转运。采用开放回路模型,用临床峰血浆浓度范围内的 LMV 或 MBV 浓度对足月胎盘进行灌流。采用超高效液相色谱-串联质谱法测量浓度。测量胎儿转移率(FTR)(胎儿(FC)/母体浓度)、清除指数(CLI)、积累指数(AI)(药物在胎盘组织中的保留)的平均值。比较了每个药物的 FC 均值与半数最大有效浓度(EC50(LMV)和 EC50(MBV))。

结果

对于 LMV,平均 FC(±标准差)为 1.1±0.2mg/L,是 EC50(LMV)的 1000 倍。平均 FTR、CLI 和 AI 分别为 9±1%、35±6%和 4±2%。对于 MBV,平均 FC 为 1.4±0.2mg/L,是 EC50(MBV)的 28 倍。平均 FTR、CLI 和 AI 分别为 10±1%、50±7%和 2±1%。

结论

由于胎儿侧的药物浓度应处于可用于治疗 CMV 感染胎儿的范围,因此,对于这两种分子,平均 FC 均优于 EC50。

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