Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.
Introduction: Finally, substitutions that disrupt the NNRTI-binding pocket, such as Y188L and M230L, confer pan-resistance against all NNRTIs.
Introduction: Other single substitutions including G190E/S, V106A, Y188L, and M230L reduced DOR susceptibility >10-fold.
Introduction: The G190S, Y188L, and M230L substitutions confer >95-fold resistance.
Introduction: The highest levels of reduction in DOR susceptibility were associated with V106A or Y188L or each of these two mutations in combination with at least
Prevalence of acquired drug resistance mutations in antiretroviral- experiencing subjects from 2012 to 2017 in Hunan Province of central South China.
Drug Resistance Mutations Against Protease, Reverse Transcriptase and Integrase Inhibitors in People Living With HIV-1 Receiving Boosted Protease Inhibitors in South Africa.
Result: H221Y and M230L occurred in one (1%) patient each; both these patients were receiving AZT plus 3TC.
Table: M230L
HIV-1 Drug Resistance, Distribution of Subtypes, and Drug Resistance-Associated Mutations in Virologic Failure Individuals in Chengdu, Southwest China, 2014-2016.
Result: K103N (37.55%, 92/245) was the most frequent mutation, followed by G190A/E/K/Q/S/V (28.57%, 70/245), V179I/D/E/T (27.76%, 68/245), V106A/I/M (26.12%, 64/245), Y181C/V (18.78%, 46/245), K101E/H/P (14.69%, 36/245), Y188C/H/L (5.71%, 14/245), L100I (4.08%, 10/245), and M230L (4.08%, 10/245).
Discussion: The L100I and M230L mutations (4.08%) had low incidence and intermediate or high resistance to RPV and ETR but no resistance to the first-line drugs EFV and NVP.
Virologic suppression in patients with a documented M184V/I mutation based on the number of active agents in the antiretroviral regimen.
Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.
PMID: 32925358
2020
Journal of acquired immune deficiency syndromes (1999)
Discussion: In this NNRTI-experienced population (N = 6893), intermediate-level (defined as detection of any RT V106A/M, Y188C/H, V108I, and K103N + P225H substitution) and high-level (defined as detection of any RT Y188L, M230L, G190E, V106A/M + F227L, and V106A/M + L234I substitutions) DOR resistance was seen in 12.7% and 6.1%, respectively, and the most common high-level DOR resistance-associated substitution was PMID: 32986709
2020
PloS one
Table: M230L
HIV-1 re-suppression on a first-line regimen despite the presence of phenotypic drug resistance.
Result: The prevalence of other major NNRTI resistance mutations (Y181CS, Y188CH, G190A and M230L) was <=8%.
Table: M230L
Prevalence of human immunodeficiency virus-1 drug-resistant mutations among adults on first- and second-line antiretroviral therapy in a resource-limited health facility in Busia County, Kenya.
PMID: 33654530
2020
The Pan African medical journal
Table: M230L
Retrospective analysis of HIV-1 drug resistance mutations in Suzhou, China from 2009 to 2014.
Abstract: Two of the mutations, M230L and L100I, which confer a high level of resistance efavirenz (EFV) and nevirapine (NVP) used as NNRTIs for first-line antiretroviral therapy (ART), were detected in this study.
HIV mutation literature information.
PMID: 
2020
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