Tenofovir Disoproxil Fumarate CAS NO 202138-50-9 Inquire about Tenofovir Disoproxil Fumarate

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What is Tenofovir Disoproxil Fumarate?

Tenofovir disoproxil fumarate, a prodrug of tenofovir[Trade name: “Viread”] developed by Gilead Sciences, is a kind of nucleotide-analogues antiretroviral drugs, taking effect through acting as the reverse transcriptase inhibitors[nRTIs], which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. It should be noted that it is the first nucleotide reverse transcriptase inhibitor that has ever used for the treatment of HIV infection.

Mechanism of Action:

Tenofovir disoproxil is a nucleotide analog reverse-transcriptase inhibitor (NtRTI). It selectively inhibits viral reverse transcriptase, a crucial enzyme in retroviruses such as human immunodeficiency virus (HIV), while showing limited inhibition of human enzymes, such as DNA polymerases α, β, and mitochondrial DNA polymerase γ. In vivo tenofovir disoproxil fumarate is converted to tenofovir, an acyclic analog of deoxyadenosine 5′-monophosphate (d-AMP). Tenofovir lacks a hydroxyl group in the position corresponding to the 3′ carbon of the d-AMP, preventing the formation of the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation. Once incorporated into a growing DNA strand, tenofovir causes premature termination of DNA transcription, preventing viral replication.

Pharmacokinetics:

Tenofovir disoproxil is a prodrug that is quickly absorbed from the gut and cleaved to release tenofovir.Inside cells, tenofovir is phosphory lated to tenofovir diphosphate (which is actually a triphosphate, as tenofovir itself already has one phosphate residue), the active compound that inhibits reverse transcriptase via chain termination.
In fasting persons, bioavailability is 25%, and highest blood plasma concentrations are reached after one hour. When taken with fatty food, highest plasma concentrations are reached after two hours, and the area under the curve is increased by 40%. It is an inhibitor of cytochrome P450 1A2.

Tenofovir Disoproxil Fumarate Drug Interactions:

Tenofovir interacts with didanosine and HIV-1 protease inhibitors. Tenofovir increases didanosine concentrations and can result in adverse effects such as pancreatitis and neuropathy. Tenofovir also interacts with HIV-1 protease inhibitors such as atazanavir, by decreasing atazanavir concentrations while increasing tenofovir concentrations. In addition, since tenofovir is excreted by the kidney, medications that impair renal function can also cause problems.

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