Product Description

 

Tenofovir disoproxil fumarate Usage And Synthesis

Overview 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[1-4]. It should be noted that it is the first nucleotide reverse transcriptase inhibitor that has ever used for the treatment of HIV infection[5]. Tenofovir disoproxil fumarate is converted to tenofovir in vivo, which is an acyclic nucleoside phosphonate[nucleotide] analog of adenosine 5'-monophosphate[5,6]. It is generally used in combination with other kinds of medicine. HIV medicines can't cure HIV/AIDS, but taking a combination of HIV medicines[called an HIV regimen] every day can help people with HIV live longer, healthier lives[7]. Based on the FDA document, tenofovir disoproxil fumarate can also be for the treatment of chronic hepatitis B virus[HBV] infection in adults and children 12 years of age and older[1,3, 4, 8].

Indication and application Tenofovir disoproxil fumarate[trade name: Viread®], an antiviral drug, is indicated as the treatment for both HIV and Hepatitis B virus[HBV]. Viread® is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 2 years of age and older. It is also indicated for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older[2,9].

Mode of action Tenofovir[the prodrug type of Viread] can effectively inhibit the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, leading to DNA chain termination[1, 5, 7, 8]. Specifically, the drugs are analogues of the naturally occurring deoxynucleotides needed to synthesize the viral DNA and they compete with the natural deoxynucleotides for incorporation into the growing viral DNA chain[8, 10, 11]. However, unlike the natural deoxynucleotides substrates, NRTIs and NTRTIs[nucleoside/tide reverse transcriptase inhibitors] lack a 3'-hydroxyl group on the deoxyribose moiety. As a result, following incorporation of an NRTI or an NtRTI, the next incoming deoxynucleotide cannot form the next 5'-3' phosphodiester bond needed to extend the DNA chain. Thus, when an NRTI or NtRTI is incorporated, viral DNA synthesis is halted, a process known as chain termination. All NRTIs and NtRTIs are classified as competitive substrate inhibitors[2].