Tenofovir alafenamide in the treatment of chronic hepatitis B: design, development, and place in therapy.

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Citation

Ogawa E, Furusyo N, Nguyen MH

Tenofovir alafenamide in the treatment of chronic hepatitis B: design, development, and place in therapy.

Drug Des Devel Ther. 2017 Nov 6;11:3197-3204. doi: 10.2147/DDDT.S126742. eCollection 2017.

PubMed ID
29158666 [ View in PubMed
]
Abstract

Tenofovir alafenamide (TAF), a novel prodrug of tenofovir (TFV), has been approved for the treatment of chronic hepatitis B virus (HBV) infection. TAF has been shown to be a potent inhibitor of HBV replication at a low dose, with high intracellular concentration and more than 90% lower systemic TFV concentration than tenofovir disoproxil fumarate (TDF). In two randomized, double-blind, multinational, Phase 3, non-inferiority trials for hepatitis B e antigen (HBeAg)-positive and -negative patients (primary analysis: 48 weeks), TAF 25 mg orally once-daily was not inferior to TDF 300 mg in achieving an HBV DNA level <29 IU/mL at week 48. No amino-acid substitutions associated with viral breakthrough were detected by deep sequencing, and no resistance to TAF was found through week 96. In addition, no difference in the frequency of HBeAg or hepatitis B surface antigen loss was observed. However, TAF was associated with a significantly higher ALT normalization rate than was TDF, based on the American Association for the Study of Liver Diseases criteria (male: ALT

DrugBank Data that Cites this Article

Drugs
Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
Tenofovir alafenamideSolute carrier organic anion transporter family member 1B1ProteinHumans
No
Substrate
Details
Tenofovir alafenamideSolute carrier organic anion transporter family member 1B3ProteinHumans
No
Substrate
Details