Result: In this study,19 substitutions conferring major resistance to DTG at 10 amino acid positions in the IN (T66A/I/K, E92G, G118R, E138K/A/T, G140S/A/C, Y143R/C/H, S147G, Q148H/R/K, N155H, and R263K) were assessed to explore the genetic barrier to DTG.
Result: No major DRMs known to be associated with DTG resistance (T66K, E92Q, G118R, E138K/A/T, G140S/A/C<
Integrase Strand Transfer Inhibitor (INSTI) Genotypic Resistance Analysis in Treatment-nNaive, INSTI Free Antiretroviral-Experienced and INSTI-Experienced Turkish Patients Infected with HIV-1.
Abstract: Additional mutations, E92Q, E138K, G140A, S147G, and Q148R were found in elvitegravir; E192Q, E138K/T, G140A/S, S147G, Q148H/R, N155H, E157Q were found in dolutegravir (DTG) experienced patients.
Abstract: Major INSTI-mutations E138K, Y143R, S147G, Q148R, N155H, and E157Q were found in raltegrav
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
Method: We also excluded PWH with the following INSTI mutations: T66I, E92Q, G118R, G140S, Y143A/C/G/H/K/R/S, S147G, Q148H/K/N/R, N155H/S/T, and R263K.
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
Introduction: Although L74I has not been observed in association with INSTI resistance (https://hivdb.stanford.edu/dr-summary/resistance-notes/INSTI/), the L74M mutation in combination with INSTI resistance-associated mutations (RAMs) T66I/K, E92V, Y143C, or N155H reduced susceptibility 14- to >200-fold to raltegravir or elvitegravir.
Brief Report: Bictegravir/Emtricitabine/Tenofovir Alafenamide Efficacy in Participants With Preexisting Primary Integrase Inhibitor Resistance Through 48 Weeks of Phase 3 Clinical Trials.
PMID: 34897227
2022
Journal of acquired immune deficiency syndromes (1999)
Introduction: Primary INSTI drug resistance reported in surveillance studies are mainly substitutions that cause resistance to RAL and EVG (T66A/I, E92Q, Y143C/H/R, S147G, Q148H/K/R, and N155H pathways) and R263K, which confers low-level reduced susceptibility to EVG, DTG, and bictegravir (BIC).
Introduction: Specifically, compared with DTG, BIC has greater in vitro activity against variants with G140/Q148 mutations accompanied by 1-2 additional substitutions and variants with the E92Q/N155H combination.
Discussion: Successful virologic outcomes in the presence of select IN
Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study.
PMID: 34694877
2022
Antimicrobial agents and chemotherapy
Discussion: Dolutegravir has selected for N155H, both alone and in combination with E138K and/or other integrase substitutions, in ART-experienced participants from several studies, including SAILING and multiple trials evaluating dolutegravir monotherapy.
Discussion: It was demonstrated that mutations at integrase positions 148 and 155 did not coexist on the same viral genome during raltegravir phase III trials, likely because sufficiently high-level raltegravir resistance was achieved with the separate substitutions and because N155H plus Q148 conferred substantial reductions in HIV-1 replication capacity.
Discussion: One participant in DAWNING had emergence of the integrase substitutions E138K, G140S,
In vitro analysis of the replicative capacity and phenotypic susceptibility to integrase inhibitors of HIV-2 mutants with integrase insertions.
PMID: 34741606
2022
The Journal of antimicrobial chemotherapy
Abstract: The SDM with T97A+N155H, with or without E92Q, was resistant to all INSTIs, except bictegravir.
No difference in HIV-1 integrase inhibitor resistance between CSF and blood compartments.
PMID: 33693680
2021
The Journal of antimicrobial chemotherapy
Abstract: The HIV-1 integrase sequences from CSF presented resistance mutations for 9/27 (33.3%) and 8/32 (25.0%) for ARV-naive (L74I, n = 3; L74I/M, n = 1; T97A, n = 1; E157Q, n = 4) and ARV-treated (L74I, n = 6; L74M, n = 1; T97A, n = 1; N155H, n = 1) patients, respectively.
HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana.
Result: Amongst the individuals previously exposed to RAL ART (seven out of eleven), DRMs selected whilst failing their current DTG based regimens were E138K, G140A, Q148R; and N155H Figure 3.
Discussion: Comparable with others, amongst individuals with prior exposure to RAL, the most common mutations selected were N155H (n = 4), Q148R (n = 4), S147G (n = 4) and E138K (n = 3) as others have similarly found.
Discussion: In our study, E138K (n = 5), S147G (n = 4), Q148R (n = 4) and N155H (n = 4) where the most frequent INSTI D
Short Communication: Integrase Strand Transfer Inhibitors Drug Resistance Mutations in Puerto Rico HIV-Positive Individuals.
PMID: 33800269
2021
International journal of environmental research and public health
Abstract: We identified the Q148HKR, G140S, Y143R, N155H, S147G, and E138EA major drug resistance mutations and the D232DN, T97TA, E157Q, G163GART accessory mutations.
Result: The most frequent integrase mutations in our analyzed patient samples were the Q148HKR (31%), G140S (28%), and, although at lower frequencies, we were able to identify the N155H, S147G, Y143R, and
HIV mutation literature information.
PMID: 
2022
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