The in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant Leishmania species of Brazil

• Published in: Memórias do Instituto Oswaldo Cruz Vol. 106; no. 4; pp. 475 - 478
• Main Authors: de Morais-Teixeira, Eliane, Damasceno, Quesia Souza, Galuppo, Mariana Kolos, Romanha, Alvaro José, Rabello, Ana
• Format: Journal Article
• Language: English
• Published: Brazil Fundação Oswaldo Cruz, Fiocruz 01-06-2011; Instituto Oswaldo Cruz, Ministério da Saúde; Fundação Oswaldo Cruz (FIOCRUZ)
• Subjects: Animals; Antiprotozoal Agents - classification; Antiprotozoal Agents - pharmacology; in vitro drug evaluation; Inhibitory Concentration 50; Leishmania; Leishmania - drug effects; Leishmania, miltefosine, in vitro drug evaluation; Macrophages - parasitology; Mice; Mice, Inbred BALB C; miltefosine; Parasitic Sensitivity Tests; PARASITOLOGY; Phosphorylcholine - analogs & derivatives; Phosphorylcholine - pharmacology; TROPICAL MEDICINE; in vitro drug evaluation; Leishmania; miltefosine
• ISSN: 1678-8060; 0074-0276; 1678-8060; 0074-0276
• DOI: 10.1590/s0074-02762011000400015

The in vitro leishmanicidal activity of miltefosine® (Zentaris
GmbH) was assessed against four medically relevant Leishmania species
of Brazil: Leishmania (Leishmania) amazonensis, Leishmania (Viannia)
braziliensis, Leishmania (Viannia) guyanensis and Leishmania
(Leishmania) chagasi. The activity of miltefosine against these New
World species was compared to its activity against the Old World
strain, Leishmania (Leishmania) donovani, which is known to be
sensitive to the effects of miltefosine. The IC50 and IC90 results
suggested the New World species harboured similar in vitro
susceptibilities to miltefosine; however, miltefosine was approximately
20 times more active against the Old World L. (L.) donovani than
against the New World L. (L.) chagasi species. The selectivity index
varied from 17.2-28.9 for the New World Leishmania species and up to
420.0 for L. (L.) donovani. The differences in susceptibility to
miltefosine suggest that future clinical trials with this drug should
include a laboratory pre-evaluation and a dose-defining step.