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. 2016 Aug 18;5(3):329–352. doi: 10.1007/s40121-016-0126-x

Table 4.

Tenofovir formulations

TAF TDF
Mechanism of action Prodrug of tenofovir that undergoes intracellular metabolism by cathepsin A Undergoes an initial diester hydrolysis to convert to tenofovir and subsequent phosphorylations by cellular enzymes to form tenofovir diphosphate
Indication HIV, HBVa HIV, HBV, PrEP
Plasma concentration 80–90% reduction in plasma levels High
Intracellular concentration 5.3-fold higher compared to TDF Low
Dosing

Formulated as a STR: 10 mg

Formulated with emtricitabine: 25 mg

300 mg
Renal dosing considerations CrCl >30 ml/min CrCl >50 ml/min
Adverse event Reduced renal and bone side effects Higher rate of renal and bone side effects

CrCl creatinine clearance, HBV hepatitis B virus, PrEP pre-exposure prophylaxis, STR single tablet regimen, TAF tenofovir alafenamide, TDF tenofovir disoproxil fumarate

aData were recently presented to support the use of TAF for HBV, but it is not currently approved for this indication