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Nucleoside analog reverse-transcriptase inhibitors (NARTIs or NRTIs) compose the first class of antiretroviral drugs developed. In order to be incorporated into the viral DNA, NRTIs must be activated in the cell by the addition of three phosphate groups to their deoxyribose moiety, to form NRTI triphosphates.
The first nucleoside reverse-transcriptase inhibitor with in vitro anti-HIV activity was zidovudine. [6] Since zidovudine was approved in 1987, six nucleosides and one nucleotide reverse-transcriptase inhibitor (NRTI) have been approved by FDA. [6]
Nucleoside reverse-transcriptase inhibitors (NRTI) and nucleotide reverse-transcriptase inhibitors (NtRTI) are nucleoside and nucleotide analogues which inhibit reverse transcription. HIV is an RNA virus, so it can not be integrated into the DNA in the nucleus of the human cell unless it is first "reverse" transcribed into DNA.
The most popular target in the field of antiretroviral drug development is the HIV-1 reverse transcriptase (RT) enzyme. [1] There are two classes of drugs that target the HIV-1 RT enzyme, nucleoside/nucleotide reverse-transcriptase inhibitors (NRTIs/NtRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). Drugs in these classes are ...
ZDV is of the nucleoside analog reverse-transcriptase inhibitor (NRTI) class. [6] It works by inhibiting the enzyme reverse transcriptase that HIV uses to make DNA and therefore decreases replication of the virus. [6] Zidovudine was first described in 1964. [7] It was resynthesized from a public-domain formula by Burroughs Wellcome. [8]
Zalcitabine (2′-3′-dideoxycytidine, ddC), also called dideoxycytidine, is a nucleoside analog reverse-transcriptase inhibitor (NRTI) sold under the trade name Hivid. Zalcitabine was the third antiretroviral to be approved by the Food and Drug Administration (FDA) for the treatment of HIV/AIDS. It is used as part of a combination regimen.
Racivir is an experimental nucleoside reverse transcriptase inhibitor (NRTI), developed by Pharmasset for the treatment of HIV. [1] It is the enantiomer of emtricitabine, a widely used NRTI, meaning that the two compounds are mirror images of each other. Emtricitabine, the enantiomer of racivir and a widely used NRTI
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) of HIV-1. Tenofovir is a nucleotide reverse transcriptase inhibitor of HIV-1, and it can be classified as an NtRTI. These three drugs work in combination to target the HIV reverse transcriptase protein in three ways, which reduces the virus's capacity to mutate. [5]