Establishment of intracellular tenofovir-diphosphate as the key determinant for in vitro-in vivo translation of antiviral efficacy.
Antiviral Res
; 151: 1-3, 2018 03.
Article
em En
| MEDLINE
| ID: mdl-29337165
ABSTRACT
In vitro evaluation of tenofovir disproxil fumarate (TDF) and tenofovir alafenamide (TAF) revealed comparable antiviral effects with respect to the tenofovir-diphosphate (TFV-DP) level in human peripheral blood mononuclear cells (PBMCs), despite the EC50 values determined based on prodrug concentrations were nearly two orders of magnitude apart. In vivo EC50 obtained from meta-analyses were in good agreement with the in vitro results, indicating intracellular TFV-DP can be employed for in vitro-in vivo translation of viral inhibition for tenofovir prodrugs. Current analysis indicated that the intracellular concentrations of TFV-DP achieving maximal antiviral effect in vitro can be directly translatable in the clinic to accomplish maximal viral load suppression attainable by tenofovir-prodrugs.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Organofosfatos
/
Replicação Viral
/
Adenina
/
Fármacos Anti-HIV
Tipo de estudo:
Systematic_reviews
Limite:
Humans
Idioma:
En
Revista:
Antiviral Res
Ano de publicação:
2018
Tipo de documento:
Article