Department of Pharmacy & Pharmacology, The Netherlands Cancer Institute - Antoni van Leeuwenhoek Hospital, Amsterdam, The Netherlands.
Int J Antimicrob Agents. 2022 Jan;59(1):106459. doi: 10.1016/j.ijantimicag.2021.106459. Epub 2021 Oct 23.
Miltefosine is an alkylphosphocholine agent with a broad spectrum of antiparasitic properties. For over two decades, miltefosine has remained the only oral drug licensed and used in the treatment of the neglected tropical disease, leishmaniasis. The last extensive review of the pharmacology of miltefosine was published in 2012. Additional data on the clinical pharmacokinetics (PK) and pharmacodynamics (PD) of miltefosine have become available in the last decade, and there are ongoing and future studies in this area. Miltefosine PK are characterized by slow absorption and elimination, resulting in accumulation of drug in plasma until the end of treatment. Several recent studies established exposure-response relationships for various regimens of miltefosine in the treatment of visceral and cutaneous leishmaniasis, leading to the identification of PK parameters predictive of clinical relapse and outcome. This review provides an update on the most recent developments in the area of clinical pharmacology of miltefosine, including a discussion of the current dosing regimens.
米替福新是一种具有广谱抗寄生虫特性的烷基磷酸胆碱药物。二十多年来,米替福新一直是唯一被许可用于治疗被忽视的热带病——利什曼病的口服药物。米替福新的药理学最后一次广泛综述发表于 2012 年。在过去十年中,米替福新的临床药代动力学(PK)和药效学(PD)的更多数据已经可用,并且在该领域正在进行和未来的研究。米替福新 PK 的特征是吸收和消除缓慢,导致药物在血浆中积累,直到治疗结束。最近的几项研究确定了米替福新治疗内脏和皮肤利什曼病的各种方案的暴露-反应关系,从而确定了预测临床复发和结果的 PK 参数。本综述提供了米替福新临床药理学领域的最新进展,包括对当前给药方案的讨论。