Department of Vascular Medicine, Academic Medical Center, PO box 22660, 1100 DD, Amsterdam, The Netherlands.
Department of Internal Medicine, Slotervaart Hospital, PO box 90440, 1006 BK, Amsterdam, The Netherlands.
Sci Rep. 2017 Oct 26;7(1):14174. doi: 10.1038/s41598-017-14526-2.
Eprotirome, a liver specific thyroid hormone agonist, was shown to induce significant increases in markers of liver injury along with a modest decrease in atherogenic lipids and lipoproteins. To get more insight into whether these effects on liver parameters were compound specific or the effect of mimicking thyrotoxicosis, we studied the effects of supra-physiological levothyroxine dosages on liver parameters, lipids and lipoproteins. We used data of a single-blinded, randomized controlled crossover trial. Herein, healthy volunteers received levothyroxine or no medication for 14 days. Thyroid hormone excess did not induce clinically relevant changes in liver parameters, while significant reductions in total cholesterol, low-density lipoprotein-cholesterol as well as apolipoprotein-B levels were observed in the intervention periods compared with the control periods. Supra-physiological thyroid hormone levels did not induce clinically relevant increases in markers of liver injury after 2 weeks of exposure, while it reduced total cholesterol, low-density lipoprotein cholesterol and apolipoprotein B levels. This suggests that the effects of eprotirome on liver parameters in previous studies were either off-target and compound specific or due to drug-drug interaction at the level of the liver. The results of our study are relevant for the development of novel thyroid hormone agonists to reduce atherogenic lipoproteins.
促甲状腺激素受体激动剂艾塞那肽可显著增加肝损伤标志物,同时适度降低致动脉粥样硬化脂质和脂蛋白。为了更深入地了解这些对肝脏参数的影响是特定于化合物还是模拟甲状腺毒症的影响,我们研究了超生理剂量左甲状腺素对肝脏参数、脂质和脂蛋白的影响。我们使用了一项单盲、随机对照交叉试验的数据。在此,健康志愿者接受左甲状腺素或 14 天不接受药物治疗。甲状腺激素过多不会导致肝脏参数发生临床相关变化,而在干预期间与对照期间相比,总胆固醇、低密度脂蛋白胆固醇和载脂蛋白 B 水平显著降低。超生理甲状腺激素水平在暴露 2 周后不会导致肝脏损伤标志物的临床相关增加,而会降低总胆固醇、低密度脂蛋白胆固醇和载脂蛋白 B 水平。这表明,在之前的研究中,艾塞那肽对肝脏参数的影响要么是脱靶和特定于化合物,要么是由于肝脏水平的药物相互作用。我们的研究结果与开发新型甲状腺激素激动剂以降低致动脉粥样硬化脂蛋白有关。