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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 ...
NNRTIs block reverse transcriptase by binding directly to the enzyme. NNRTIs are not incorporated into the viral DNA like NRTIs, but instead inhibit the movement of protein domains of reverse transcriptase that are needed to carry out the process of DNA synthesis. NNRTIs are therefore classified as non-competitive inhibitors of reverse ...
NNRTIs affect the handling of substrate (nucleotides) by reverse transcriptase by binding near the active site. NNRTIs can be further classified into 1st generation and 2nd generation NNRTIs. 1st generation NNRTIs include nevirapine and efavirenz. 2nd generation NNRTIs are etravirine and rilpivirine. [13] HIV-2 is intrinsically resistant to ...
Rilpivirine, sold under the brand names Edurant and Rekambys, is a medication, developed by Tibotec, used for the treatment of HIV/AIDS. [5] [6] It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs such as efavirenz.
The reverse transcriptase of HIV-1 has been the main foundation for the development of anti-HIV drugs. [5] 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 ...
Etravirine is a human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitor (NNRTI). [1] Unlike agents in the class, resistance to other NNRTIs does not seem to confer resistance to etravirine. [4] Etravirine is marketed by Janssen, a subsidiary of Johnson & Johnson.
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It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase. [5] Nevirapine was approved for medical use in the United States in 1996. [5] It is on the World Health Organization's List of Essential Medicines. [7] It is available as a generic medication. [5]
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