Anwar S, Yokota T
Department of Medical Genetics, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada.
Department of Medical Genetics, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada; The Friends of Garrett Cumming Research and Muscular Dystrophy Canada, HM Toupin Neurological Science Research Chair, Edmonton, Alberta, Canada.
Drugs Today (Barc). 2020 Aug;56(8):491-504. doi: 10.1358/dot.2020.56.8.3159186.
Duchenne muscular dystrophy (DMD) is a life-shortening X-linked genetic disorder characterized by progressive wasting and weakening of muscles in boys. Loss-of-function mutations in the DMD gene, which codes for dystrophin, lead to this disease. The majority of mutations in this gene result in the exclusion of one or more exons from the transcript, eventually causing the remaining exons not to fit together correctly (i.e., out-of-frame mutations). Antisense oligonucleotides, e.g., phosphorodiamidate morpholino oligomers (PMOs), can induce therapeutic exon skipping during pre-mRNA processing to restore the reading frame of the primary transcript of DMD. As a result, truncated but partially functional dystrophin is produced, potentially slowing down the disease progression. Golodirsen is a provisionally approved PMO-based drug for approx. 8% of all DMD patients amenable to exon 53 skipping. This article summarizes golodirsen's pharmacology, efficacy and safety information. It also discusses some controversies that golodirsen met after the approval.
杜氏肌营养不良症(DMD)是一种缩短寿命的X连锁遗传病,其特征是男孩的肌肉进行性萎缩和衰弱。编码抗肌萎缩蛋白的DMD基因功能丧失突变会导致这种疾病。该基因中的大多数突变会导致转录本中一个或多个外显子被排除,最终导致其余外显子无法正确拼接在一起(即移码突变)。反义寡核苷酸,例如磷酰二胺吗啉代寡聚物(PMO),可以在mRNA前体加工过程中诱导治疗性外显子跳跃,以恢复DMD初级转录本的阅读框。结果,会产生截短但部分功能正常的抗肌萎缩蛋白,有可能减缓疾病进展。golodirsen是一种基于PMO的临时批准药物,适用于约8%适合跳过外显子53的DMD患者。本文总结了golodirsen的药理学、疗效和安全性信息。还讨论了golodirsen批准后遇到的一些争议。