Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics.

摘要: Tenofovir disoproxil fumarate (tenofovir DF) is an oral prodrug of tenofovir, a nucleotide (nucleoside monophosphate) analogue with activity against retroviruses, including HIV-1, HIV-2 and hepadnaviruses. Following absorption, tenofovir DF rapidly converted to which metabolised intracellularly its active anabolite diphosphate, competitive inhibitor HIV-1 reverse transcriptase terminates the growing DNA chain. exerts antiviral effects in variety cell types, resting cells. exhibits longer serum (17 hours) intracellular (≥60 half-lives than those nucleoside analogues, supports flexible once-daily administration schedule. The pharmacokinetics are dose-proportional similar healthy volunteers HIV-infected individuals. bioavailability enhanced by high-fat meal, but at steady state when administered or without typical meal. not substrate, inducer human cytochrome P450 enzymes vitro vivo. has been studied 15 other antiretroviral concomitant medications frequently used HIV-1-infected population. With exception didanosine atazanavir, require dosage modifications, no clinically significant drug interactions have observed DF. recommended adults 300 mg/day. eliminated renal elimination, tubular secretion; dose-interval adjustments necessary for patients impairment. No adjustment liver disease.