Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2023 Jun;83(8):725-729. doi: 10.1007/s40265-023-01874-9.
Omaveloxolone (SKYCLARYS™) is an orally active, small molecule semi-synthetic triterpenoid drug that increases antioxidant activity, which is being developed by Reata Pharmaceuticals, Inc. for the treatment of Friedreich's ataxia. In patients with Friedreich's ataxia, the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway is suppressed, which is associated with oxidative stress, mitochondrial dysfunction and damage to cells, including central and peripheral neurones. The Nrf2 pathway may be activated by omaveloxolone as it blocks the ubiquitination and degradation of Nrf2. Omaveloxolone was approved in February 2023 in the USA for the treatment of Friedreich's ataxia. This article summarizes the milestones in the development of omaveloxolone leading to this first approval for the treatment of Friedreich's ataxia in adults and adolescents aged 16 years and older.
奥马伐洛酮(SKYCLARYS)是一种具有口服活性的小分子半合成三萜类药物,可增加抗氧化活性,由 Reata 制药公司开发,用于治疗弗里德里希共济失调。在弗里德里希共济失调患者中,核因子(红系衍生 2)样 2(Nrf2)途径受到抑制,这与氧化应激、线粒体功能障碍和细胞损伤有关,包括中枢和周围神经元。奥马伐洛酮可能通过阻止 Nrf2 的泛素化和降解来激活 Nrf2 途径。奥马伐洛酮于 2023 年 2 月在美国获得批准,用于治疗弗里德里希共济失调。本文总结了奥马伐洛酮开发过程中的重要里程碑,这是该药物首次获得批准,用于治疗 16 岁及以上成年和青少年的弗里德里希共济失调。