期刊
TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE
卷 100, 期 -, 页码 S17-S20出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.trstmh.2006.02.010
关键词
visceral leishmaniasis; cutaneous leishmaniasis; antileishmanial; miltefosine; alkyl-phospholipid; anticancer agent
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.
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