Abstract: Among the nonresponders carrying a resistant virus (86.6%) at virological failure, 26% harbored clinically relevant low-frequency DRMs in the cell-associated DNA at month six (0.5%-20%; K103N, G190A, Y181C, and M184I).
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
Abstract: A second generation benzimidazolone inhibitor (compound 42) not only showed inhibitory activity against wild-type HIV but also remained active against HIV containing the K103N, Y181C, and K103N/Y181C drug resistance mutations.
Abstract: The first generation benzimidazolone inhibitors were found to be potent inhibitors of wild-type HIV reverse transcriptase but were ineffective in the presence of common resistance mutations such as K103N and Y181C.
Synthesis and anti-human immunodeficiency virus activity of substituted ( o,o-difluorophenyl)-linked-pyrimidines as potent non-nucleoside reverse transcriptase inhibitors.
Abstract: Antiviral activities of 20 compounds were measured against wild type human immunodeficiency virus-1 and mutant reverse transcriptase strains (K103N, Y181C) using a cytoprotection assay.
Conclusion: A new series of trisubstituted DAPY analogues was prepared starting from commercially available trisubstituted pyrimidines and evaluated for their anti-HIV potency against wild type and two clinically relevant mutant strains (K103N and Y181C).
Introduction: K103N and
Result: Selected derivatives were also tested against clinically relevant K103N and Y181C HIV RT mutants (Table 1).
Table: Y181C
Persistence of Human Immunodeficiency Virus-1 Drug Resistance Mutations in Proviral Deoxyribonucleic Acid After Virologic Failure of Efavirenz-Containing Antiretroviral Regimens.
PMID: 30863788
2019
Open forum infectious diseases
Introduction: Studies of drug resistance mutations (DRMs) in plasma virus ribonucleic acid (RNA) by Sanger consensus sequencing frequently identify mutations associated with nonnucleoside reverse-transcriptase inhibitors (NNRTIs); most often K103N, followed by G190S, V106A/M, Y181C, Y188L, and P225H.
Introduction: Compound 13 is similar to RPV in terms of its therapeutic index and its antiretroviral efficacy against a panel of HIV-1 mutants containing RT mutations, including L100I, K103N, V106A, E138K, Y181C, Y188L, H221Y, and K103N/Y181C.
Introduction: In those trials, the viruses in participants who failed RPV-containing therapies had the RT mutations L100I, K101E, K103N, V108I, E138K/R, Y1
The Utility of Efavirenz-based Prophylaxis Against HIV Infection. A Systems Pharmacological Analysis.
Abstract: Trough concentrations achieved after 600 mg once daily dosing (median: 2017 ng/mL, 95% CI:445-9830) and after reduced dose (400 mg) efavirenz (median: 1349ng/mL, 95% CI: 297-6553) provided complete protection against wild-type virus and the Y181C mutant, and median trough concentrations provided about 90% protection against the K103N and G190S mutants.
Abstract: We predicted that plasma concentrations of 11, 36, 1287 and 1486ng/mL prevent 90% sexual transmissions with wild type and Y181C, K103N and G190S mutants, respectively.
Incidence and types of HIV-1 drug resistance mutation among patients failing first-line antiretroviral therapy.
PMID: 30928089
2019
Journal of pharmacological sciences
Abstract: RESULTS: 103 cases were successfully amplified, and the main drug resistance mutations in the reverse transcriptase (RT) region were M184V (50.49%), K103N (28.16%), Y181C (25.24%), and K65R (27.18%), while no drug main resistance mutation was found in the protease (PR) region.
Primary HIV Drug Resistance among Recently Infected Cases of HIV in North-West India.
Abstract: Observed mutations were K219R, L74V, K219N, and Y181C.
Abstract: The fact that both Y181C isolates are IDUs is important and represents 2/21 (~10%) NNRTI drug resistance.
Result: Two isolates had Y181C, a major NNRTI resistance mutation accountable for high level resistance to Nevirapine (NVP), intermediate resistance to efavirenz (EFV), etravirine (ETR), and rilpivirine (RPV).
Diversity of HIV-1 genotypes and high prevalence of pretreatment drug resistance in newly diagnosed HIV-infected patients in Shanghai, China.
Result: The most frequent NNRTI associated mutation was V179D/E, which was observed in 10.1% (32/317) of patients, followed by Y181C (2.5%, 8/55) and K103 N (1.9%, 6/317).
Prevalence of drug resistance mutations among ART-naive and -experienced HIV-infected patients in Sierra Leone.
PMID: 30989237
2019
The Journal of antimicrobial chemotherapy
Abstract: The most prevalent PDR mutations were K103N (14.3%), M184V (8.2%) and Y181C (4.1%).
Result: The most prevalent RT PDR mutations were as follows: K103N (n = 7, 14.3%), M184V (n = 4, 8.2%) and Y181C (n = 2, 4.1%).
HIV mutation literature information.
PMID: 
2019
Journal of medical virology
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