PMID: 34740228
2022
Current opinion in HIV and AIDS
Abstract: Doravirine has a high genetic barrier to resistance with retained activity in the presence of single NNRTI mutations K103N, Y181C and G190A.
Single Oral Doses of MK-8507, a Novel Non-Nucleoside Reverse Transcriptase Inhibitor, Suppress HIV-1 RNA for a Week.
PMID: 34654041
2022
Journal of acquired immune deficiency syndromes (1999)
Introduction: Preclinical studies demonstrated MK-8507 has high antiviral potency, has a half-maximal inhibitory concentration (IC50) of approximately 50 nM, and shows only modest changes in activity to the most prevalent NNRTI-associated resistance mutations (eg, K103N, Y181C).
Method: Inclusion criteria included diagnosis of HIV-1 infection >=3 months before screening, plasma HIV-1 RNA >=10,000 copies/mL, CD4+ T-cell count >200/mm3, no evidence of NNRTI-associated resistance mutations (eg, K103N, Y181C, and V108I) appearing in the Stanford University HIV Drug Resistance Database, and no evidence of active hepatitis C or hepatitis B infection.
HIV-1 molecular transmission network among sexually transmitted populations in Liaoning Province, China.
Result: Among them, 9 cases were protease inhibitor-related resistance, and the main resistance sites were L33F, V82A, Q58E, M46L, M46I; There were 4 cases of nucleoside reverse transcriptase inhibitor resistance, the main mutation sites were V75VI, K219Q, T215A, K65R; There were 5 cases of non-nucleoside reverse transcriptase inhibitor resistance,
Discussion: Mutations K65R, Y181C+G190S, which produced high drug resistance, did not enter the transmission network.
Increase in HIV-1-transmitted drug resistance among ART-naive youths at the China-Myanmar border during 2009 ~ 2017.
Result: K103N and Y181C were the most common TDRMs in NNRTI.
Result: The K103N group, Y181C group, and NRTI_TDRMs group had lower mean CD4 counts (337/mm395% CI: 246.42 ~ 427.57/mm
Table: Y181C
Discussion: Among these mutations, K103N (n = 9) and Y181C/I (n = 7) were the most common TDRMs.
Discussion: In summary, large sample size and more epidemiological data are required to evaluate the potential role of three classes of TDR (NNRTI/NRTI/PI) or K103N, Y181C in affecting the decline of CD4 count.
High Detection Rate of HIV Drug Resistance Mutations among Patients Who Fail Combined Antiretroviral Therapy in Manaus, Brazil.
Discussion: Due to the presence of mutations, such as L100I, K101P, Y181C, M230L, observed in of individuals failing in the use of EFV, the viability of using ETR in a rescue scheme is reduced for few individuals (data not shown).
HIV-1 non-group M phenotypic susceptibility in vitro to bictegravir and cabotegravir.
PMID: 34151963
2021
The Journal of antimicrobial chemotherapy
Abstract: Around 50% of the strains of this group naturally show a mutation (Y181C) providing them with resistance to NNRTIs and making therapeutic management more difficult.
High HIV-1 Virological Failure and Drug Resistance among Adult Patients Receiving First-Line ART for At least 12 Months at a Decentralized Urban HIV Clinic Setting in Senegal before the Test-and-Treat.
Abstract: Of the 27 viraemic isolates successfully genotyped, 20 (74.1%) carried DR mutations; most frequent were M184VI (55.6%), K103N (37.1%), thymidine analog mutations (29.6%), Y181CY (22.2%).
Result: The most frequent resistant genotypes to NNRTIs were K103N (37.04%), Y181CY (22.2%), and A98AG (18.5%).
Table: Y181C
Discussion: EFV and NVP have a lower genetic barrier, thus facilitating the selection of K103N and Y181C mutations.
Near-point-of-care assay with a visual readout for detection of HIV-1 drug resistance mutations: A proof-of-concept study.
Abstract: Here, we present a proof-of-concept study of a rapid and simple molecular method to detect two major mutations (K103 N, Y181C) conferring resistance to first-line nonnucleoside reverse transcriptase inhibitor regimens.
In vitro cross-resistance to doravirine in a panel of HIV-1 clones harbouring multiple NNRTI resistance mutations.
PMID: 32974670
2021
The Journal of antimicrobial chemotherapy
Abstract: As expected, single NNRTI mutations K103N and Y181C did not impair doravirine susceptibility (FC 1.4 and 1.8, respectively), while reduced activity was observed with the single M230L or double K103N/Y181C mutations (FC 7.6 and 4.9, respectively).
Abstract: METHODS: In vitro phenotypic susceptibility to doravirine was assessed in 10 clinically derived infectious clones with intermediate- to high-level resistance to rilpivirine, etravirine, efavirenz and nevirapine, and in NL4-3 site-directed mutants harbouring K103N, Y181C, M230L or K103N/Y181C NNRTI m
Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction.
Discussion: However, doravirine appears to be more efficient than efavirenz and/or rilpivirine in suppressing resistance breakthrough of HIV-1 strains with the common NNRTI resistance-associated mutations such as K103N, Y181C or K103N/Y181C.
Discussion: The highest levels of doravirine resistance (fold-change >100) have been associated with amino acid substitutions V106A/G190A/F227L, E138K/Y181C/M230L and Y188L (alone or in combination with K103N or V106I).
HIV mutation literature information.
PMID: 
2022
Current opinion in HIV and AIDS
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