Tenofovir alafenamide was granted approval in the US for treating adults with HBV infection with compensated liver disease In November ***6.
Tenofovir alafenamide fumarate (TAF) is a novel prodrug of tenofovir (TFV) that is more stable in human plasma and more efficiently penetrates into target cells than TFV. Tenofovir converted from TAF reaches plasma concentration which is *0% lower than that of TFV converted from TDF. Conversely, the active metabolite converted from TAF reaches a higher intracellular level in target cells than TFV from TDF. This allows a substantial reduction of its oral dose, decreasing the risk for renal and bone toxicity. It is even possible to reduce the dose of TAF in case it is administered concurrently with cobicistat further improving its absorption and optimizing its pharmacokinetic profile. Pharmacokinetic properties are another factor substantially influencing its safety profile. TAF is not a substrate for renal organic anion transporters and thus shows no cytotoxicity related to their expression.