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Three NNRTI compounds of the first generation have been approved by the FDA for treating HIV-1 infection. Nevirapine was approved in 1996, delavirdine in 1997 and efavirenz in 1998 (table 1). Two of these drugs, nevirapine and efavirenz, are cornerstones of first line HAART while delavirdine is hardly used nowadays.
Treatment with a regimen including efavirenz (EFV) and nevirapine (NVP) typically results in mutations L100I, Y181C/I, K103N, V106A/M, V108I, Y188C/H/L and G190A/S. [17] There are three main mechanisms of NNRTI resistance. In the first NRTI mutations disrupt specific contacts between the inhibitor and the NNRTI binding pocket.
The first NRTI was zidovudine, approved by the U.S. Food and Drug Administration (FDA) in 1987, which was the first step towards treatment of HIV. Six NRTI agents and one NtRTI have followed. The NRTIs and the NtRTI are analogues of endogenous 2´-deoxy-nucleoside and nucleotide.
NNRTI: INSTI: PI: PK enhancer: Combivir: lamivudine zidovudine: September 26, 1997 ViiV Healthcare: No Kaletra (developed countries) Aluvia (developing countries) lopinavir: ritonavir: September 15, 2000 Abbott Laboratories: No Trizivir: abacavir lamivudine zidovudine November 15, 2000 ViiV Healthcare Yes Epzicom Kivexa (EU, RU) abacavir ...
The liver problems and skin rash may be severe and should be checked for during the first few months of treatment. [5] [6] It appears to be safe for use during pregnancy. [5] It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and works by blocking the function of reverse transcriptase. [5]
Zidovudine was first described in 1964. [7] It was resynthesized from a public-domain formula by Burroughs Wellcome. [8] It was approved in the United States in 1987 and was the first treatment for HIV. [6] [9] It is on the World Health Organization's List of Essential Medicines. [10] It is available as a generic medication. [6]
NNRTI 1998 Elvitegravir: HIV Gilead Sciences Integrase inhibitor 2012 (Fixed-dose combo Stribild) 2014 (single pill) 2015 ; Emtricitabine: HIV Gilead Sciences NRTI 2003 Enfuvirtide: HIV Entry inhibitor 2003 Ensitrelvir: COVID-19: Shionogi: 3C-like protease inhibitor Entecavir: HIV NRTI 2005 Etravirine (Intelence) [8] HIV NNRTI 2008 Famciclovir ...
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]