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Drugs. 2018 Sep;78(14):1517-1523. doi: 10.1007/s40265-018-0979-2.
Tafenoquine (Krintafel™, Arakoda™), an orally-active 8-aminoquinoline anti-malarial drug, is a long-acting analogue of primaquine with activity against pre-erythrocytic (liver) and erythrocytic (asexual) forms as well as gametocytes of Plasmodium species that include Plasmodium vivax (P. vivax) and Plasmodium falciparum. It has been developed by GlaxoSmithKline (formerly SmithKline Beecham) for the radical cure of P. vivax malaria and by 60 Degrees Pharmaceuticals for the prophylaxis of malaria. The exact mechanism(s) of action underlying the anti-Plasmodium activity of tafenoquine are unknown, although it may exert its effect by inhibiting haematin polymerization and, additionally, by inducing mitochondrial dysfunction leading to the apoptotic-like death of the organism. In July 2018, tafenoquine was approved in the USA for the radical cure of P. vivax malaria in patients aged ≥ 16 years who are receiving appropriate antimalarial therapy for acute P. vivax malaria. Subsequently, in August 2018, tafenoquine was approved in the USA for the prophylaxis of malaria in patients aged ≥ 18 years. This article primarily summarizes the milestones in the development of tafenoquine leading to its first global approval for the radical cure of P. vivax malaria.
他非喹（商品名：Krintafel、Arakoda），一种口服活性 8-氨基喹啉类抗疟药，是长效伯氨喹类似物，对疟原虫的红细胞前期（肝脏）和红细胞内期（无性生殖）以及配子体均有活性，包括间日疟原虫（P. vivax）和恶性疟原虫（P. falciparum）。它由葛兰素史克（原史克必成）开发，用于根治间日疟，由 60 度制药公司开发，用于疟疾预防。他非喹抗疟作用的确切作用机制尚不清楚，尽管它可能通过抑制血红素聚合以及诱导线粒体功能障碍来发挥作用，导致生物体凋亡样死亡。2018 年 7 月，他非喹在美国获得批准，用于治疗年龄≥16 岁的间日疟患者，这些患者正在接受急性间日疟的适当抗疟治疗。随后，2018 年 8 月，他非喹在美国获得批准，用于年龄≥18 岁的疟疾预防。本文主要总结了他非喹开发过程中的里程碑事件，最终使其在全球范围内首次获得批准，用于根治间日疟。
