In vitro activity of 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine against multidrug-resistant hepatitis B virus mutants.
The susceptibilities of drug-resistant hepatitis B virus (HBV) mutants to lamivudine, adefovir, tenofovir, entecavir, and 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]-pyrimidine (PMEO-DAPym), a novel acyclic pyrimidine analogue, were assessed in vitro. Most drug-resistant mutants, including multidrug-resistant strains, remained sensitive to tenofovir and PMEO-DAPym. Therefore, the latter molecule deserves further evaluation for the treatment of HBV infection.
Brunelle
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MN
INSERM, U871, 151 Cours Albert Thomas, 69424 Lyon cedex 03, France.
Lucifora
J
J
Neyts
J
J
Villet
S
S
Holy
A
A
Trepo
C
C
Zoulim
F
F
D000225:Adenine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D024921:Drug Resistance, Multiple, Viral; D006515:Hepatitis B virus / Q000187:drug effects* / Q000201:enzymology / Q000235:genetics; D019694:Hepatitis B, Chronic / Q000821:virology; D006801:Humans; D008826:Microbial Sensitivity Tests; D009154:Mutation; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D011741:Pyrimidine Nucleosides / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D000068698:Tenofovir; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D063065:Organophosphonates; D011741:Pyrimidine Nucleosides; D018894:Reverse Transcriptase Inhibitors; D000068698:Tenofovir; D000225:Adenine