Doravirine and Islatravir Have Complementary Resistance Profiles and Create a Combination with a High Barrier to Resistance.
PMID: 35491829
2022
Antimicrobial agents and chemotherapy
Abstract: Based on the frequent emergence of F227C, we hypothesized that DOR and ISL would create a combination (DOR/ISL) with a high barrier to resistance.
Abstract: Isolate hypersusceptibility to ISL required F227C, in contrast to zidovudine, an NRTI, which required M184V.
Abstract: The most common DOR resistance-associated mutation (RAM) detected in 5 of the 7 resistant isolates was F227C.
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: Furthermore, we excluded people with the following mutations for NNRTI: L100I, K101E/H/NP/Q, E138A/G/K/Q/R, V179L, Y181C/F/G/I/S/V, Y188L, G190A/C/E/Q/S/T/V, H221Y, F227C/L, and M230L.
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,
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)
Table: F227C
Phase 2 Open-Label Study of Long-Term Safety, Tolerability, and Antiviral Activity of Rilpivirine in Antiretroviral-Naive Adolescents Living with HIV-1.
PMID: 34871089
2022
Antimicrobial agents and chemotherapy
Method: Patients with previously documented HIV-2 infection, with active AIDS, and with documented genotypic evidence of >=1 NNRTI resistance-associated mutation (RAM) from a predefined list of the following NNRTI RAMs at screening were excluded: A98G, L100I, K101E, K101P, K101Q, K103H, K103N, K103S, K103T, V106A, V106M, V108I, E138A, E138G,
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)
Discussion: F227C is an NNRTI-resistance-associated variant that is clinically rare (<=0.5% of all clinical samples), observed primarily in patients receiving doravirine and less frequently in people receiving etravirine or rilpivirine.
Discussion: F227C would not be expected to emerge in combination with an antiretroviral of another class with activity against F227C; the intended clinical use of MK-8507 is as part of a weekly combination therapy.
Discussion: In a second participant without a viral rebound 14 days postdose, F227C was found as a minority variant using UDS.
Discussion: No rebound was observed in the first 7 days postdose in this study, and detection of K103N at 7 days postdose in 1 participant and F227C in anothe
HIV-1 drug resistance among individuals who seroconverted in the ASPIRE dapivirine ring trial.
PMID: 34762770
2021
Journal of the International AIDS Society
Table: F227C/I
Temporal Trends in HIV-1 Mutations Used for the Surveillance of Transmitted Drug Resistance.
Result: Figure 2 shows the locations of the NNRTI-SDRMs and the six candidate mutations (E138K/Q, V179L, H221Y, and F227C/L) within the three-dimensional structure of the polymerase coding region of p66 and the finger domain of p51 HIV-1 Discussion: Six candidate NNRTI-SDRMs were identified as potentially useful additions to an expanded NNRTI SDRM list because they are associated with reduced susceptibility to rilpivirine (E138K/Q, V179L, and H221Y) and doravirine (F227L/C) and because they increased in prevalence since 2009.
Phylogenetic and Drug-Resistance Analysis of HIV-1 Sequences From an Extensive Paediatric HIV-1 Outbreak in Larkana, Pakistan.
Prevalence of doravirine-associated resistance mutations in HIV-1-infected antiretroviral-experienced patients from two large databases in France and Italy.
PMID: 31976534
2020
The Journal of antimicrobial chemotherapy
Abstract: RESULTS: The frequencies of doravirine-associated resistance mutations (total dataset versus NNRTI-failing patients) were: V106A/M, 0.8% versus 2.6%; V108I, 3.3% versus
Abstract: The following mutations were considered as resistance mutations: V106A/M, V108I, Y188L, G190S, F227C/L/V, M230I/L, L234I, P236L, K103N + Y181C, K103N + P225H and K103N + L100I.