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The discovery of the TIBO compounds led to the definition of the NNRTI class in the late 1980s [2] when they were unexpectedly found to inhibit RT. This finding initiated researches on mechanism of action for these compounds. The HEPT compounds were described before the TIBO compounds and were originally believed to be NRTIs.
A second mechanism is the disruption of important interactions on the inside of the pocket. For example, Y181C and Y188L result in the loss of important aromatic rings involved in NNRTI binding. [20] [21] The third type of mutations result in changes in the overall conformation or the size of the NNRTI binding pocket. An example is G190E, which ...
Mechanism of action [ edit ] Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), designed to be active against HIV with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs, mutation K103N for efavirenz and Y181C for nevirapine . [ 11 ]
Nevirapine (NVP), sold under the brand name Viramune among others, is a medication used to treat and prevent HIV/AIDS, specifically HIV-1. [5] It is generally recommended for use with other antiretroviral medications. [5]
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.
Schematic description of the mechanism of the four classes of available antiretroviral drugs against HIV. There are six classes of drugs, which are usually used in combination, to treat HIV infection. Antiretroviral (ARV) drugs are broadly classified by the phase of the retrovirus life-cycle that the drug inhibits. Typical combinations include ...
It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase. [1] Efavirenz was approved for medical use in the United States in 1998, [1] and in the European Union in 1999. [4] It is on the World Health Organization's List of Essential Medicines. [6]
In some literature articles, the terms "mechanism of action" and "mode of action" are used interchangeably, typically referring to the way in which the drug interacts and produces a medical effect. However, in actuality, a mode of action describes functional or anatomical changes, at the cellular level, resulting from the exposure of a living ...