Wang Y, Bhargava P
Department of Neurology, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.
Drugs Today (Barc). 2020 Jul;56(7):431-437. doi: 10.1358/dot.2020.56.7.3151521.
On October 29, 2019, the Food and Drug Administration (FDA) of the United States approved diroximel fumarate (DRF) as an oral fumarate for the treatment of relapsing forms of multiple sclerosis. Another oral fumarate, dimethyl fumarate (DMF), was approved for the same indication on March 27, 2013. Prior to its approval, DRF did not undergo rigorous testing to determine its efficacy, as its active metabolite, monomethyl fumarate, is the same as that of DMF (bioequivalency). The efficacy, safety and tolerability of DMF have previously been demonstrated in a number of clinical trials and real-world studies. For DRF, one phase III study has been completed, and another is in progress to determine its safety, tolerability and efficacy. In this paper, we review the pharmacology, pharmacokinetics, metabolism, clinical studies and drug safety of DRF.
2019年10月29日，美国食品药品监督管理局（FDA）批准了富马酸二甲酯（DRF）作为一种口服富马酸盐用于治疗复发型多发性硬化症。另一种口服富马酸盐，即富马酸二甲酯（DMF），于2013年3月27日被批准用于相同适应症。在获得批准之前，DRF并未进行严格测试以确定其疗效，因为其活性代谢物单甲基富马酸盐与DMF的相同（生物等效性）。DMF的疗效、安全性和耐受性此前已在多项临床试验和真实世界研究中得到证实。对于DRF，一项III期研究已经完成，另一项正在进行中，以确定其安全性、耐受性和疗效。在本文中，我们综述了DRF的药理学、药代动力学、代谢、临床研究和药物安全性。
