Development of miltefosine as an oral treatment for leishmaniasis

被引：148

作者：

Sindermann, H. ^{[1
]}

Engel, J. ^{[1
]}

机构：

[1] Zentaris GmbH, D-60314 Frankfurt, Germany

来源：

TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE | 2006年 / 100卷

关键词：

visceral leishmaniasis; cutaneous leishmaniasis; antileishmanial; miltefosine; alkyl-phospholipid; anticancer agent;

D O I：

10.1016/j.trstmh.2006.02.010

中图分类号：

R1 [预防医学、卫生学];

学科分类号：

1004 ; 120402 ;

摘要：

Miltefosine was originally formulated and registered as a topical treatment for cutaneous cancers. For this indication and in subsequent development for leishmaniasis, a large body of non-clinical data has been generated. The gastrointestinal organ is the main site of toxicity, in both animal and in human studies. The testis and retina were identified as target organs in rats, although corresponding changes were not observed in clinical studies in humans. In terms of pharmacokinetics, the terminal elimination half-life is long (84 h and 159 h in rats and dogs respectively). Miltefosine is widely distributed in body organs and not metabolized by cytochrome P450 enzymes in vitro. The drug is embryotoxic and fetotoxic in rats and rabbits, and teratogenic in rats but not in rabbits. It is therefore contraindicated for use during pregnancy, and contraception is required beyond the end of treatment in women of child-bearing age. (c) 2006 Royal Society of Tropical Medicine and Hygiene. Published by Elsevier Ltd. All rights reserved.

引用

页码：S17 / S20

页数：4

共 15 条

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