In Vitro Characterization of MK-1439, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor

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Published inAntimicrobial Agents and Chemotherapy Vol. 58; no. 3; pp. 1652 - 1663
Main Authors LAI, Ming-Tain, MEIZHEN FENG, CAUCHON, Elizabeth, CAMPEAU, Louis-Charles, GROBLER, Jay, YOUWEI YAN, DUCHARME, Yves, COTE, Bernard, ASANTE-APPIAH, Ernest, HAZUDA, Daria J, MILLER, Michael D, FALGUEYRET, Jean-Pierre, TAWA, Paul, WITMER, Marc, DISTEFANO, Daniel, YUAN LI, BURCH, Jason, SACHS, Nancy, MEIQING LU
Format Journal Article
LanguageEnglish
Published Washington, DC American Society for Microbiology 01.03.2014
Subjects
Anti-HIV Agents
Anti-HIV Agents - administration & dosage
Anti-HIV Agents - adverse effects
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral Agents
Biological and medical sciences
Drug Synergism
HIV Infections - drug therapy
HIV Reverse Transcriptase
HIV Reverse Transcriptase - antagonists & inhibitors
HIV Reverse Transcriptase - metabolism
HIV-1
HIV-1 - drug effects
HIV-1 - enzymology
Human immunodeficiency virus 1
Human viral diseases
Humans
Immunodeficiencies
Immunodeficiencies. Immunoglobulinopathies
Immunopathology
In Vitro Techniques
Infectious diseases
Macrophages - drug effects
Medical sciences
Monocytes - drug effects
Pharmacology. Drug treatments
Pyridones
Pyridones - adverse effects
Pyridones - pharmacology
Triazoles
Triazoles - adverse effects
Triazoles - pharmacology
Viral diseases
Viral diseases of the lymphoid tissue and the blood. Aids
Virus Replication - drug effects
Immunopathology
HIV-1 virus
Non nucleoside compound
Retroviridae
AIDS
Immune deficiency
Lentivirus
In vitro
Infection
Virus
Characterization
Viral disease
Reverse transcriptase inhibitor
Antiviral
Human immunodeficiency virus
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Abstract Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit StumbleUpon Twitter current issue AAC About AAC Subscribers Authors Reviewers Advertisers Inquiries from the Press Permissions & Commercial Reprints ASM Journals Public Access Policy AAC RSS Feeds 1752 N Street N.W. • Washington DC 20036 202.737.3600 • 202.942.9355 fax • journals@asmusa.org Print ISSN: 0066-4804 Online ISSN: 1098-6596 Copyright © 2014 by the American Society for Microbiology.   For an alternate route to AAC .asm.org, visit: AAC       
AbstractList Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel NNRTI with a 50% inhibitory concentration (IC 50 ) of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. Selectivity and cytotoxicity studies confirmed that MK-1439 is a highly specific NNRTI with minimum off-target activities. In the presence of 50% normal human serum (NHS), MK-1439 showed excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC 95 ) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC 95 of 43, 27, and 55 nM, respectively. MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses). In addition, the susceptibility of a broader array of clinical NNRTI-associated mutant viruses (a total of 96 viruses) to MK-1439 and other benchmark NNRTIs was investigated. The results showed that the mutant profile of MK-1439 was superior overall to that of efavirenz (EFV) and comparable to that of etravirine (ETR) and rilpivirine (RPV). Furthermore, E138K, Y181C, and K101E mutant viruses that are associated with ETR and RPV were susceptible to MK-1439 with a fold change (FC) of <3. A two-drug in vitro combination study indicated that MK-1439 acts nonantagonistically in the antiviral activity with each of 18 FDA-licensed drugs for HIV infection. Taken together, these in vitro data suggest that MK-1439 possesses the desired properties for further development as a new antiviral agent.
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel NNRTI with a 50% inhibitory concentration (IC50) of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. Selectivity and cytotoxicity studies confirmed that MK-1439 is a highly specific NNRTI with minimum off-target activities. In the presence of 50% normal human serum (NHS), MK-1439 showed excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC95 of 43, 27, and 55 nM, respectively. MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses). In addition, the susceptibility of a broader array of clinical NNRTI-associated mutant viruses (a total of 96 viruses) to MK-1439 and other benchmark NNRTIs was investigated. The results showed that the mutant profile of MK-1439 was superior overall to that of efavirenz (EFV) and comparable to that of etravirine (ETR) and rilpivirine (RPV). Furthermore, E138K, Y181C, and K101E mutant viruses that are associated with ETR and RPV were susceptible to MK-1439 with a fold change (FC) of <3. A two-drug in vitro combination study indicated that MK-1439 acts nonantagonistically in the antiviral activity with each of 18 FDA-licensed drugs for HIV infection. Taken together, these in vitro data suggest that MK-1439 possesses the desired properties for further development as a new antiviral agent.
Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit StumbleUpon Twitter current issue AAC About AAC Subscribers Authors Reviewers Advertisers Inquiries from the Press Permissions & Commercial Reprints ASM Journals Public Access Policy AAC RSS Feeds 1752 N Street N.W. • Washington DC 20036 202.737.3600 • 202.942.9355 fax • journals@asmusa.org Print ISSN: 0066-4804 Online ISSN: 1098-6596 Copyright © 2014 by the American Society for Microbiology.   For an alternate route to AAC .asm.org, visit: AAC       
Author Yves Ducharme
Jay Grobler
Michael D. Miller
Paul Tawa
Jason Burch
Yuan Li
Ernest Asante-Appiah
Daniel DiStefano
Louis-Charles Campeau
Jean-Pierre Falgueyret
Marc Witmer
Daria J. Hazuda
Youwei Yan
Ming-Tain Lai
Bernard Côté
Nancy Sachs
Meiqing Lu
Elizabeth Cauchon
Meizhen Feng
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Copyright © 2014, American Society for Microbiology. All Rights Reserved.
Copyright © 2014, American Society for Microbiology. All Rights Reserved. 2014 American Society for Microbiology
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Issue 3
Keywords Immunopathology
HIV-1 virus
Non nucleoside compound
Retroviridae
AIDS
Immune deficiency
Lentivirus
In vitro
Infection
Virus
Characterization
Viral disease
Reverse transcriptase inhibitor
Antiviral
Human immunodeficiency virus
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PublicationTitle Antimicrobial Agents and Chemotherapy
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PublicationYear 2014
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Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients....
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SubjectTerms Anti-HIV Agents
Anti-HIV Agents - administration & dosage
Anti-HIV Agents - adverse effects
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral Agents
Biological and medical sciences
Drug Synergism
HIV Infections - drug therapy
HIV Reverse Transcriptase
HIV Reverse Transcriptase - antagonists & inhibitors
HIV Reverse Transcriptase - metabolism
HIV-1
HIV-1 - drug effects
HIV-1 - enzymology
Human immunodeficiency virus 1
Human viral diseases
Humans
Immunodeficiencies
Immunodeficiencies. Immunoglobulinopathies
Immunopathology
In Vitro Techniques
Infectious diseases
Macrophages - drug effects
Medical sciences
Monocytes - drug effects
Pharmacology. Drug treatments
Pyridones
Pyridones - adverse effects
Pyridones - pharmacology
Triazoles
Triazoles - adverse effects
Triazoles - pharmacology
Viral diseases
Viral diseases of the lymphoid tissue and the blood. Aids
Virus Replication - drug effects
Title In Vitro Characterization of MK-1439, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor
URI http://aac.asm.org/content/58/3/1652.abstract
https://www.ncbi.nlm.nih.gov/pubmed/24379202
https://journals.asm.org/doi/10.1128/AAC.02403-13
https://search.proquest.com/docview/1505334845
https://pubmed.ncbi.nlm.nih.gov/PMC3957832
Volume 58
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