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New HBV Drug PMEO-DAPym Active In Vitro Against Drug Resistant Mutants of HBV
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Reported by Jules Levin
AASLD, Oct 2006, Boston, MA
INHIBITORY ACTIVITY OF THE
2,4-DIAMINO-6-(2-PHOSPHONOMETHOXY-ETHOXY)-PYRIMIDINE (PMEO-DAPym) AGAINST WILD TYPE AND DRUG RESISTANT MUTANTS OF HBV
M.N. Brunelle (1), J. Lucifora (1), S. Villet (1), J. Neyts (2), A. Holy (3), C.Trepo (1), F. Zoulim (1)
1) INSERM U271, Lyon, France
2) Rega institute for Medical Research, Leuven, Belgium
3) Institute of Organic Chemistry and Biochemistry, Prague, Czech Republic.
AUTHOR CONCLUSIONS
PMEO-DAPym inhibits viral DNA synthesis of the most common HBV drug resistant strains in vitro
Its inhibitory effect is comparable on the LAM-R, ADV-R, ETV-R and MDR harboring a complex pattern of polymerase gene mutations
PMEO-DAPym is an interesting candidate for pre-clinical evaluations in animal models of hepadnavirus infection
Perspective for clinical applications :
- rescue of multidrug resistant mutant infections,
- interesting cross-resistance profile for combination therapy to prevent drug resistance
INTRODUCTION
Main problems with antiviral therapy of chronic hepatitis B:
-- Prolonged administration of antivirals
-- Selection of drug resistant mutants
-- Problem of cross-resistance
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