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'''Miltefosine''' ([[International Nonproprietary Name|INN]], trade names '''Impavido''' and '''Miltex''') is an [[antiprotozoal]] [[medication|drug]]. Originally developed as an [[antineoplastic]], it is finding use as an [[antiprotozoal]] drug. It can be administered orally and intravenously. | '''Miltefosine''' ([[International Nonproprietary Name|INN]], trade names '''Impavido''' and '''Miltex''') is an [[antiprotozoal]] [[medication|drug]]. Originally developed as an [[antineoplastic]], it is finding use as an [[antiprotozoal]] drug. It can be administered orally and intravenously. | ||
Revision as of 17:27, 9 August 2012
| File:Miltefosine.svg | |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| ATC code | |
| Pharmacokinetic data | |
| Bioavailability | High |
| Elimination half-life | 6 to 8 days |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C21H46NO4P |
| Molar mass | 407.568 g/mol |
Miltefosine (INN, trade names Impavido and Miltex) is an antiprotozoal drug. Originally developed as an antineoplastic, it is finding use as an antiprotozoal drug. It can be administered orally and intravenously.
Current antiprotozoal and antifungal applications
Leishmania: Miltefosine is registered and used by Zentaris GmbH in India, Colombia and Germany for the treatment of visceral and cutaneous leishmaniasis, and is undergoing clinical trials for this use in several other countries, such as Brazil[1] and Guatemala.[2] It is currently the only effective oral treatment for leishmaniasis.
Miltefosine is one of the few orally administered drugs that is effective against Leishmania [3]
Investigatory antiprotozoal and antifungal usage
Miltefosine is being investigated by researchers interested in finding treatments for infections which have become resistant to existing drugs. Animal and in-vitro studies suggest it may have broad anti-protozoal and anti-fungal properties:
- Animal studies suggest miltefosine may also be effective against Trypanosoma cruzi, the parasite responsible for Chagas' disease. [4]
- Several studies have found the drug to be effective against Cryptococcus neoformans, Candida, Aspergillus and Fusarium.[5]
- An in-vitro study found that Miltefosine is effective against metronidazole-resistant variants of Trichomonas vaginalis, a sexually transmitted protozoal disease.[6]
- Hexadecyltrimethylammonium bromide, a compound structurally similar to miltefosine, was recently found to exhibit potent in vitro activity against Plasmodium falciparum.[7]
Side effects
The main side effects reported with miltefosine treatment are nausea and vomiting. Miltefosine has exhibited teratogenicity, and should not be administered to pregnant women.
References
- ↑ Cristina, Márcia (September 2005). "Hospital de Doenças Tropicais testa droga contra calazar". Sapiência (in Portuguese). Fundação de Amparo à Pesquisa do Estado do Piauí. Retrieved 2006-09-01. Unknown parameter
|coauthors=ignored (help) - ↑ Soto J, Berman J (2006). "Treatment of New World cutaneous leishmaniasis with miltefosine". Trans R Soc Trop Med Hyg. PMID 16930649.
- ↑ Berman J (2005). "Clinical status of agents being developed for leishmaniasis". Expert opinion on investigational drugs. 14 (11): 1337–46. doi:10.1517/13543784.14.11.1337. PMID 16255674.
- ↑ Saraiva V, Gibaldi D, Previato J, Mendonça-Previato L, Bozza M, Freire-De-Lima C, Heise N (2002). "Proinflammatory and cytotoxic effects of hexadecylphosphocholine (miltefosine) against drug-resistant strains of Trypanosoma cruzi". Antimicrob Agents Chemother. 46 (11): 3472–7. PMID 12384352.
- ↑ Widmer F, Wright L, Obando D, Handke R, Ganendren R, Ellis D, Sorrell T (2006). "Hexadecylphosphocholine (miltefosine) has broad-spectrum fungicidal activity and is efficacious in a mouse model of cryptococcosis". Antimicrob Agents Chemother. 50 (2): 414–21. PMID 16436691.
- ↑ Blaha C, Duchêne M, Aspöck H, Walochnik J (2006). "In vitro activity of hexadecylphosphocholine (miltefosine) against metronidazole-resistant and -susceptible strains of Trichomonas vaginalis". J. Antimicrob. Chemother. 57 (2): 273–8. doi:10.1093/jac/dki417. PMID 16344287.
- ↑ Choubey V, Maity P, Guha M, Kumar S, Shrivastava K, Puri SK, Bandyopadhyay U (2006). "Inhibition of Plasmodium falciparum choline kinase by hexadecyltrimethylammonium bromide: A possible antimalarial mechanism of hexadecyltrimethylammonium bromide". Antimicrob Agents Chemother. PMID 17145794.
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