| Autor: |
E. De Clercq, Johan Neyts, Jan Balzarini, N. Bischofberger, Lieve Naesens |
| Rok vydání: |
1995 |
| Předmět: |
|
| Zdroj: |
Nucleosides, Nucleotides and Nucleic Acids. 14:767-770 |
| ISSN: |
1525-7770 |
| Popis: |
The bis-pivaloyloxymethyl(POM)- and diphenyl-ester prodrugs of the broad spectrum antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) have been evaluated in vivo for antiviral efficacy upon oral administration in severe combined immune deficiency (SCID) mice infected with Moloney murine sarcoma virus (MSV). Oral bis (POM)-PMEA proved highly efficient in delaying MSV-induced tumor formation and associated death, its effect being equal to that of subcutaneous PMEA at an equimolar dose. Compared to bis(POM)-PMEA, oral diphenyl-PMEA had lower antiviral efficacy, whereas PMEA as such was poorly effective when administered orally. Our studies indicate that bis(POM)-PMEA must have a favorable oral bioavailability and justify its clinical investigation as an oral prodrug of PMEA in the treatment of HIV infections. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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