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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.
Even though apricitabine is a little less potent in vitro compared to some other NRTIs, it maintains its activity against a broad spectrum of HIV-1 variants with NRTI resistance mutations. Apricitabine is in the final stage of clinical development for the treatment of NRTI-experienced patients.
Figure 3 Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) inhibit the reverse-transcriptase enzyme (RT) and therefore the replication of new viruses. The NNRTIs act by binding non-competitively to the RT enzyme (figure 3). The binding causes conformational change in the three-dimensional structure of the enzyme and creates the NNIBP.
Typical combinations include two nucleoside reverse-transcriptase inhibitors (NRTI) as a "backbone" along with one non-nucleoside reverse-transcriptase inhibitor (NNRTI), protease inhibitor (PI) or integrase inhibitors (also known as integrase nuclear strand transfer inhibitors or INSTIs) as a "base". [7]
NRTIs / NtRTIs: 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 ...
Therefore, this NNRTI-binding pocket will inhibit reverse transcription in a way that is distinct to the NRTIs. [ 33 ] Nevirapine is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.
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]
Efavirenz is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class. [ 20 ] As most NNRTIs bind within the same pocket, viral strains which are resistant to efavirenz are usually also resistant to the other NNRTIs, nevirapine and delavirdine .