In a randomized, crossover pharmacokinetic study in healthy volunteers (N = 14), a single dose of 2 g probenecid (PRO)-boosted 600 mg tenofovir disoproxil fumarate (TDF)/400 mg emtricitabine (FTC) (test (T) +PRO) was compared with the current on-demand HIV preexposure prophylaxis from the IPERGAY study (a 600 mg TDF/400 mg FTC on day 1 and 300 mg TDF/200 mg FTC on days 2 and 3) (control, C IPERGAY). PRO increased mean single-dose area under the plasma concentration-time curve extrapolated to infinity (AUC0-∞,SD ) of tenofovir (TFV) and FTC by 61% and 68%, respectively. The TFV-diphosphate (TFV-DP) concentrations in peripheral blood mononuclear cells were higher (~30%) at 24 hours in T +PRO but then fell significantly lower (~40%) at 72 hours compared with C IPERGAY. The interaction between FTC and PRO was unexpected and novel. Further study is needed to determine if this PRO-boosted TDF/FTC regimen would be clinically effective.

中文翻译：

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丙磺舒对替诺福韦富马酸替诺福韦酯和恩曲他滨的药物代谢动力学的抑制作用，按需预防艾滋病毒的暴露。

在一项针对健康志愿者（N = 14）的随机，交叉药代动力学研究中，单剂量2 g丙磺舒（PRO）增强了600 mg替诺福韦富马酸替诺福韦酯（400 mg）恩曲他滨（FTC）（测试（T）+ PRO ）与IPERGAY研究中目前按需的HIV暴露前预防措施（第1天为600 mg TDF / 400 mg FTC，第2天和第3天为300 mg TDF / 200 mg FTC）进行了比较（对照，C IPERGAY）。PRO将血浆浓度-时间曲线下的平均单剂量面积外推至替诺福韦（TFV）和FTC的无穷大（AUC0-∞，SD）分别增加了61％和68％。与C IPERGAY相比，在T + PRO中24小时时外周血单核细胞中的TFV-二磷酸（TFV-DP）浓度较高（〜30％），但在72小时时显着下降（〜40％）。FTC和PRO之间的交互是出乎意料的且新颖的。