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Clinical Pharmacokinetics

Clinical Pharmacokinetics

IF: 4.59
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Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics.

Published:1 January 2004 DOI: 10.2165/00003088-200443090-00003 PMID: 15217303
Brian P Kearney, John F Flaherty, Jaymin Shah

Abstract

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

Substances (6)

Related products
Procduct Name CAS Molecular Formula Supplier Price
Tenofovir 147127-20-6 C9H14N5O4P 668 suppliers $5.00-$1200.00
Tenofovir disoproxil fumarate 202138-50-9 C23H34N5O14P 557 suppliers $5.00-$1700.00
Dideoxyinosine 69655-05-6 C10H12N4O3 343 suppliers $5.00-$2440.00
Atazanavir 198904-31-3 C38H52N6O7 324 suppliers $5.00-$2400.00
TENOFOVIR DIPHOSPHATE 166403-66-3 C9H16N5O10P3 44 suppliers Inquiry
Tenofovir Diphosphate 206646-04-0 C9H15N5O7P2 21 suppliers Inquiry

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