Andersson Axel G, Xu Yiyi, Kärrman Anna, Cederlund Julia, Lindh Christian H, Pineda Daniela, Fletcher Tony, Jakobsson Kristina, Li Ying
School of Public Health and Community Medicine, Institute of Medicine, Sahlgrenska Academy, University of Gothenburg, Gothenburg, Box 414, 405 30 Gothenburg, Sweden.
School of Public Health and Community Medicine, Institute of Medicine, Sahlgrenska Academy, University of Gothenburg, Gothenburg, Box 414, 405 30 Gothenburg, Sweden.
Environ Int. 2025 Oct;204:109794. doi: 10.1016/j.envint.2025.109794. Epub 2025 Sep 16.
Some per- and polyfluoroalkyl substances (PFAS) such as perfluorohexane sulfonic acid (PFHxS), perfluorooctane sulfonic acid (PFOS) and perfluorooctanoic acid (PFOA) are very long-lived in humans, with serum half-lives of several years. In PFAS hot spots, such as Ronneby, Sweden, high exposures over time have led to markedly elevated serum PFAS levels, which may result in health risks as well as transfer to the next generation through pregnancy and breastfeeding. Bile acid sequestrants and organic anion transporter inhibitors are drug candidates for increasing PFAS elimination in humans.
This is a cross-over, clinical study in 10 individuals from Ronneby, Sweden. First, participants were given the bile acid sequestrant cholestyramine and the organic anion transporter inhibitor probenecid for 1 week each. Urinary and fecal concentrations were measured prior, during and after the administration. Then, the changes of serum PFAS concentrations during a 12-week intervention with the bile acid sequestrant colesevelam were compared to a control period.
The study population was mainly exposed to PFHxS (serum mean 50 ng/mL, range 5.8-170), PFOS (serum mean 46 ng/mL, range 9.2-130) and PFOA (serum mean 2.2, range 0.7-4.4). Cholestyramine intervention increased the serum adjusted fecal PFOS concentrations by 23.1 times (95 %CI: 13.6, 39.2), while probenecid was associated with 0.79 times (95 %CI 0.63, 1.0) serum-adjusted urinary PFOS concentrations, compared to no intervention. The 12-week intervention with colesevelam resulted in a mean serum PFOS decline of 38 % (95 %CI -42, -34), compared to 2 % (95 %CI -8, 5) in the control period. The decline was smaller for PFHxS and PFOA.
Bile acid sequestrants could be used for accelerating PFAS excretion in highly PFAS exposed individuals. Studies are needed to evaluate the risks, costs and benefits of using it for this purpose.
一些全氟和多氟烷基物质（PFAS），如全氟己烷磺酸（PFHxS）、全氟辛烷磺酸（PFOS）和全氟辛酸（PFOA）在人体内的半衰期很长，可达数年。在PFAS热点地区，如瑞典的吕讷堡，长期的高暴露导致血清PFAS水平显著升高，这可能会带来健康风险，并通过怀孕和哺乳传递给下一代。胆汁酸螯合剂和有机阴离子转运体抑制剂是有望增加人体PFAS清除率的药物。
这是一项针对瑞典吕讷堡10名个体的交叉临床研究。首先，参与者分别服用胆汁酸螯合剂考来烯胺和有机阴离子转运体抑制剂丙磺舒各1周。在给药前、给药期间和给药后测量尿液和粪便中的浓度。然后，将服用胆汁酸螯合剂考来维仑进行12周干预期间血清PFAS浓度的变化与对照期进行比较。
研究人群主要暴露于PFHxS（血清均值50 ng/mL，范围5.8 - 170）、PFOS（血清均值46 ng/mL，范围9.2 - 130）和PFOA（血清均值2.2，范围0.7 - 4.4）。与未干预相比，考来烯胺干预使血清校正后的粪便PFOS浓度增加了23.1倍（95%CI：13.6，39.2），而丙磺舒使血清校正后的尿液PFOS浓度增加了0.79倍（95%CI 0.63，1.0）。与对照期2%（95%CI -8，5）相比，考来维仑12周干预使血清PFOS平均下降了38%（95%CI -42，-34）。PFHxS和PFOA的下降幅度较小。
胆汁酸螯合剂可用于加速PFAS高暴露个体的PFAS排泄。需要开展研究以评估为此目的使用该药物的风险、成本和益处。
