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,
HIV-1 drug resistance among individuals who seroconverted in the ASPIRE dapivirine ring trial.
PMID: 34762770
2021
Journal of the International AIDS Society
Table: P236L
Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.
Introduction: Across those clinical isolates (no subtype information was provided), DOR displayed a good antiviral activity with fold changes in EC50<9 against most single mutant viruses, including A98G, E138A/G/K/Q, G190A, K101E/P, K103N/S, L100I, P236L, V106M, V108I, V197D, V90I,
Introduction: Other substitutions such as V106M, V108I, V179D, Y188H, or P236L conferred less than 10-FC against DOR.
The algorithm used for the interpretation of doravirine transmitted drug resistance strongly influences clinical practice and guideline recommendations.
PMID: 32030406
2020
The Journal of antimicrobial chemotherapy
Abstract: METHODS: We used the WHO 2009 list to investigate the prevalence of NNRTI, NRTI and PI TDR, in treatment-naive HIV-1-infected patients, adding mutations E138A/G/K/Q/R, V106I, V108I, V179L, G190Q, H221Y, F227C/L/V, M230IDR, L234I, P236L and Y318F in RT.
Comparison of HIV drug resistance profiles across HIV-1 subtypes A and D for patients receiving a tenofovir-based and zidovudine-based first line regimens in Uganda.
Result: This was followed by G190A/S/E/G that occurred in 55 (30.2%) of the patients, P236L mutation occurred in 2 (1.1%) and L234I that occurred in only 4 (2.2%) of the participants.
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: 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.
HIV-1 reverse transcriptase and protease mutations for drug-resistance detection among treatment-experienced and naive HIV-infected individuals.
Rare occurrence of doravirine resistance-associated mutations in HIV-1-infected treatment-naive patients.
PMID: 30476106
2019
The Journal of antimicrobial chemotherapy
Abstract: We studied the prevalence of doravirine resistance-associated mutations previously identified in vitro: V106A/M, V108I, Y188L, V190S, H221Y, F227C/L/V, M230I/L, L234I, P236L, Y318F and K103N/Y181C.
A decade of viral mutations and associated drug resistance in a population of HIV-1+ Puerto Ricans: 2002-2011.
Result: The RT mutations with the highest average frequencies were M184V (47.9%), K103N (42.6%) and M41L (34.2%) (Figs 2 and 5); the three least common RT mutations over the 10-year period were K103T, Y188C and P236L (S1 Table).
Rilpivirine and Doravirine Have Complementary Efficacies Against NNRTI-Resistant HIV-1 Mutants.
PMID: 27124362
2016
Journal of acquired immune deficiency syndromes (1999)
Result: HIV-1 variants
Result: We chose NNRTI resistant mutants that are known to contribute to virological failure in HIV-infected individuals or mutants that were selected in cell culture: G190A, G190S, M230L, P236L, L100I/K103N, K103N/P225H, and V106A/G190A/F227L.
Discussion: The P236L mutation causes a modest decrease in DOR susceptibility by introducing clash and preventing the CH-pi interaction between the triazolone of DOR and P236.
HIV mutation literature information.
PMID: 
2022
Antimicrobial agents and chemotherapy
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