Abstract: Notably, (3-ethylphenyl)boronic acid substituted indole-2-carboxamide maintained excellent activities against the single HIV-1 mutants L100I (EC50 = 7.3 nM), K103N (EC50 = 9.2 nM), as well as the double mutant V106A/F227L (EC50 = 21.1 nM).
Impact of Integrase Sequences from HIV-1 Subtypes A6/A1 on the In Vitro Potency of Cabotegravir or Rilpivirine.
PMID: 34978890
2022
Antimicrobial agents and chemotherapy
Discussion: Since the 48-week analysis in ATLAS-2M, 1 participant with HIV-1 subtype B and the L74I polymorphism met CVF criteria; this individual had RT mutations K103N and Y181C but no INSTI RAMs at CVF.
Switching efavirenz to rilpivirine in virologically suppressed adolescents with HIV: a multi-centre 48-week efficacy and safety study in Thailand.
PMID: 35001501
2022
Journal of the International AIDS Society
Method: We excluded individuals with prior evidence of NNRTI-associated resistance mutations based on the IAS-USA HIV drug-resistance mutations list (2019) (V90I, A98G, L100I, K101E/H/P/Q/R/N, K103N/S, V106A/M/I, V108I, E138K/A/G/Q/R, V179D/F/L/T, Y181C/I/V, Y188L/C/H, G190A/S/E,H221Y, P225H, F227L/C/R,
Biophysical Characterization of Novel DNA Aptamers against K103N/Y181C Double Mutant HIV-1 Reverse Transcriptase.
Abstract: K103N (59%) and M184V (52%) were the most common mutations, followed by V106M and K65R (31% each).
Management of a human immunodeficiency virus case with discordant antiviral drug resistance profiles in cerebrospinal fluid compared with plasma: a case report.
PMID: 35164871
2022
Journal of medical case reports
Conclusion: The HIV-1 pol gene genotypic resistance analysis showed development of the NRTI M184V mutation, and NNRTI K103N and E138EK mutations in plasma, respectively.
Conclusion: The nonpolymorphic NNRTI K103N mutation causes high-level resistance to efavirenz (EFV), and E138K mutation causes potential low-level cross-resistance to EFV, which was discontinued together with 3TC.
Could Long-Acting Cabotegravir-Rilpivirine Be the Future for All People Living with HIV? Response Based on Genotype Resistance Test from a Multicenter Italian Cohort.
PMID: 35207677
2022
Journal of personalized medicine
Abstract: We excluded patients with HBsAg positivity, evidence of non-nucleoside reverse transcriptase inhibitor (except K103N) and integrase inhibitor mutations, and with a detectable HIV-RNA (>50 copies/mL).
Method: Therefore, we considered eligible for treatment with long-acting CAB/RPV, PWH with an undetectable HIV-RNA (<50 copies/mL) for at least 12 months, who are HBsAg negative, and who do not have evidence of NNRTI (except K103N) or Integrase Strand Transfer Inhibitor (INSTI) mutations.
Trends of Transmitted and Acquired Drug Resistance in Europe From 1981 to 2019: A Comparison Between the Populations of Late Presenters and Non-late Presenters.
Abstract: Of 1818 patients with VL 50-999 copies/mL, 182 (10.0%) experienced HIVDR, the most common DRAM were M184I/V 28.6%, K103N 19.2%, and V181C/I/V 10.4% (multidrug resistance: 27.5%), and patients with HIVDR had a higher risk of CD4 cell counts < 200 cells/muL (AOR 3.8, 95% CI 2.6-5.5, p < 0.01) comparing with those without HIVDR.
Abstract: Of 925 patients with VL >= 1000 copies/mL, 495 (53.5%) acquired HIVDR, the most common DRAM were K103N 43.8%, M184I/V 43.2%, M41L 19.0%, D67N/G 16.4%, V181C/I/V 14.5%, G190A/S 13.9% and K101E 13.7% (multidrug resistance: 75.8%), and patients with HIVDR had
HIV mutation literature information.
PMID: 
2022
Bioorganic & medicinal chemistry
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