literature

HIV mutation literature information.

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,

Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.

PMID: 35011517 2022 Molecules (Basel, Switzerland)

Introduction: K103N/ Y181C double mutations were associated with resistance to EFV and NVP NNRTI inhibitors.

Introduction: A high prevalence of NNRTIs drug mutations was found in K103N, V106M, Y181C, and G190A.

Introduction: This research aimed to isolate potential specific anti-HIV-1 RT DNA aptamers again

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,

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

Discussion: Since the 48-week analysis in ATLAS-2M, 1 participant with HIV-1 subtype B and the L74I polymorphism met CVF criteria; this individual had RT mutations K103N and Y181C but no INSTI RAMs at CVF.

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)

Result: The treatment-naive participant had K103N and K70R in RT and Q148H and G140S in IN genes.

Table: K103N/S

Table: K103N

Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV1 non-nucleoside reverse transcriptase inhibitors.

PMID: 34890994 2022 Bioorganic & medicinal chemistry

Abstract: Notably, (3-ethylphenyl)boronic acid substituted indole-2-carboxamide maintained excellent activities against the single HIV-1 mutants L100I (EC50 = 7.3 nM), K103N (EC50 = 9.2 nM), as well as the double mutant V106A/F227L (EC50 = 21.1 nM).

Rising rates of recent preexposure prophylaxis exposure among men having sex with men newly diagnosed with HIV: antiviral resistance patterns and treatment outcomes.

PMID: 34873084 2022 AIDS (London, England)

Table: K103N/S

Drug Resistance Mutations in a Population Before Antiretroviral Therapy Initiation in Northern South Africa.

PMID: 34107774 2022 AIDS research and human retroviruses

Abstract: The most frequent SDRMs based on drug class were; K103N (7.9%-NNRTI), K65R (2.5%-NRTI), and D30N (0.8%-PI).

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.

Result: At the 80 mg dose level, 2 partici

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: For drugs with a lower barrier, effective resistance can be achieved with a single mutation while maintaining viral fitness; for example, efavirenz resistance can occur via the single reverse transcriptase substitution K103N.

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