Neurotoxicity with high-dose disulfiram and vorinostat used for HIV latency reversal

The aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well tolerated and can enhance HIV latency reversal. Vorinostat and disulfiram can increase HIV transcription in PWH on ART. Together, these agents ma...

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Veröffentlicht in:AIDS (London) Jg. 36; H. 1; S. 75
Hauptverfasser: McMahon, James H, Evans, Vanessa A, Lau, Jillian S Y, Symons, Jori, Zerbato, Jennifer M, Chang, Judy, Solomon, Ajantha, Tennakoon, Surekha, Dantanarayana, Ashanti, Hagenauer, Michelle, Lee, Sulggi, Palmer, Sarah, Fisher, Katie, Bumpus, Namandje, Heck, Carley J S, Burger, David, Wu, Guoxin, Zuck, Paul, Howell, Bonnie J, Zetterberg, Henrik H, Blennow, Kaj, Gisslen, Magnus, Rasmussen, Thomas A, Lewin, Sharon R
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Sprache:Englisch
Veröffentlicht: England 01.01.2022
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ISSN:1473-5571, 1473-5571
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Abstract The aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well tolerated and can enhance HIV latency reversal. Vorinostat and disulfiram can increase HIV transcription in PWH on ART. Together, these agents may lead to significant HIV latency reversal. Virologically suppressed PWH on ART received disulfiram 2000 mg daily for 28 days and vorinostat 400 mg daily on days 8-10 and 22-24. The primary endpoint was plasma HIV RNA on day 11 relative to baseline using a single copy assay. Assessments included cell-associated unspliced RNA as a marker of latency reversal, HIV DNA in CD4+ T-cells, plasma HIV RNA, and plasma concentrations of ART, vorinostat, and disulfiram. The first two participants (P1 and P2) experienced grade 3 neurotoxicity leading to trial suspension. After 24 days, P1 presented with confusion, lethargy, and ataxia having stopped disulfiram and ART. Symptoms resolved by day 29. After 11 days, P2 presented with paranoia, emotional lability, lethargy, ataxia, and study drugs were ceased. Symptoms resolved by day 23. CA-US RNA increased by 1.4-fold and 1.3-fold for P1 and P2 respectively. Plasma HIV RNA was detectable from day 8 to 37 (peak 81 copies ml-1) for P2 but was not increased in P1 Antiretroviral levels were therapeutic and neuronal injury markers were elevated in P1. The combination of prolonged high-dose disulfiram and vorinostat was not safe in PWH on ART and should not be pursued despite evidence of latency reversal.
AbstractList The aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well tolerated and can enhance HIV latency reversal. Vorinostat and disulfiram can increase HIV transcription in PWH on ART. Together, these agents may lead to significant HIV latency reversal. Virologically suppressed PWH on ART received disulfiram 2000 mg daily for 28 days and vorinostat 400 mg daily on days 8-10 and 22-24. The primary endpoint was plasma HIV RNA on day 11 relative to baseline using a single copy assay. Assessments included cell-associated unspliced RNA as a marker of latency reversal, HIV DNA in CD4+ T-cells, plasma HIV RNA, and plasma concentrations of ART, vorinostat, and disulfiram. The first two participants (P1 and P2) experienced grade 3 neurotoxicity leading to trial suspension. After 24 days, P1 presented with confusion, lethargy, and ataxia having stopped disulfiram and ART. Symptoms resolved by day 29. After 11 days, P2 presented with paranoia, emotional lability, lethargy, ataxia, and study drugs were ceased. Symptoms resolved by day 23. CA-US RNA increased by 1.4-fold and 1.3-fold for P1 and P2 respectively. Plasma HIV RNA was detectable from day 8 to 37 (peak 81 copies ml-1) for P2 but was not increased in P1 Antiretroviral levels were therapeutic and neuronal injury markers were elevated in P1. The combination of prolonged high-dose disulfiram and vorinostat was not safe in PWH on ART and should not be pursued despite evidence of latency reversal.
The aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well tolerated and can enhance HIV latency reversal.OBJECTIVEThe aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well tolerated and can enhance HIV latency reversal.Vorinostat and disulfiram can increase HIV transcription in PWH on ART. Together, these agents may lead to significant HIV latency reversal.DESIGNVorinostat and disulfiram can increase HIV transcription in PWH on ART. Together, these agents may lead to significant HIV latency reversal.Virologically suppressed PWH on ART received disulfiram 2000 mg daily for 28 days and vorinostat 400 mg daily on days 8-10 and 22-24. The primary endpoint was plasma HIV RNA on day 11 relative to baseline using a single copy assay. Assessments included cell-associated unspliced RNA as a marker of latency reversal, HIV DNA in CD4+ T-cells, plasma HIV RNA, and plasma concentrations of ART, vorinostat, and disulfiram.METHODSVirologically suppressed PWH on ART received disulfiram 2000 mg daily for 28 days and vorinostat 400 mg daily on days 8-10 and 22-24. The primary endpoint was plasma HIV RNA on day 11 relative to baseline using a single copy assay. Assessments included cell-associated unspliced RNA as a marker of latency reversal, HIV DNA in CD4+ T-cells, plasma HIV RNA, and plasma concentrations of ART, vorinostat, and disulfiram.The first two participants (P1 and P2) experienced grade 3 neurotoxicity leading to trial suspension. After 24 days, P1 presented with confusion, lethargy, and ataxia having stopped disulfiram and ART. Symptoms resolved by day 29. After 11 days, P2 presented with paranoia, emotional lability, lethargy, ataxia, and study drugs were ceased. Symptoms resolved by day 23. CA-US RNA increased by 1.4-fold and 1.3-fold for P1 and P2 respectively. Plasma HIV RNA was detectable from day 8 to 37 (peak 81 copies ml-1) for P2 but was not increased in P1 Antiretroviral levels were therapeutic and neuronal injury markers were elevated in P1.RESULTSThe first two participants (P1 and P2) experienced grade 3 neurotoxicity leading to trial suspension. After 24 days, P1 presented with confusion, lethargy, and ataxia having stopped disulfiram and ART. Symptoms resolved by day 29. After 11 days, P2 presented with paranoia, emotional lability, lethargy, ataxia, and study drugs were ceased. Symptoms resolved by day 23. CA-US RNA increased by 1.4-fold and 1.3-fold for P1 and P2 respectively. Plasma HIV RNA was detectable from day 8 to 37 (peak 81 copies ml-1) for P2 but was not increased in P1 Antiretroviral levels were therapeutic and neuronal injury markers were elevated in P1.The combination of prolonged high-dose disulfiram and vorinostat was not safe in PWH on ART and should not be pursued despite evidence of latency reversal.CONCLUSIONThe combination of prolonged high-dose disulfiram and vorinostat was not safe in PWH on ART and should not be pursued despite evidence of latency reversal.
Author Lee, Sulggi
Zetterberg, Henrik H
Bumpus, Namandje
Solomon, Ajantha
Evans, Vanessa A
Zerbato, Jennifer M
Fisher, Katie
Tennakoon, Surekha
Wu, Guoxin
Hagenauer, Michelle
Lewin, Sharon R
Palmer, Sarah
Dantanarayana, Ashanti
Burger, David
Chang, Judy
Symons, Jori
Blennow, Kaj
McMahon, James H
Zuck, Paul
Rasmussen, Thomas A
Lau, Jillian S Y
Heck, Carley J S
Howell, Bonnie J
Gisslen, Magnus
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  organization: Department of Infectious Diseases, Alfred Hospital and Monash University
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  givenname: Vanessa A
  surname: Evans
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  organization: The Peter Doherty Institute for Infection and Immunity, The University of Melbourne and Royal Melbourne Hospital, Melbourne, Victoria, Australia
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  organization: Department of Infectious Diseases, Alfred Hospital and Monash University
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  organization: The Peter Doherty Institute for Infection and Immunity, The University of Melbourne and Royal Melbourne Hospital, Melbourne, Victoria, Australia
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  organization: The Peter Doherty Institute for Infection and Immunity, The University of Melbourne and Royal Melbourne Hospital, Melbourne, Victoria, Australia
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  surname: Hagenauer
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  organization: Department of Infectious Diseases, Alfred Hospital and Monash University
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  fullname: Lee, Sulggi
  organization: University of California San Francisco, San Francisco, California, USA
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  fullname: Palmer, Sarah
  organization: The Westmead Institute for Medical Research, University of Sydney, Sydney, Westmead, Australia
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  surname: Fisher
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  organization: The Westmead Institute for Medical Research, University of Sydney, Sydney, Westmead, Australia
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  organization: Johns Hopkins University, Baltimore, Maryland, USA
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  organization: Johns Hopkins University, Baltimore, Maryland, USA
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  organization: Department of Pharmacy, Radboud University Medical Center, Nijmegen, the Netherlands
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  organization: Department of Infectious Disease & Vaccine Research, Merck & Co., Inc., Kenilworth, New Jersey, USA
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  givenname: Paul
  surname: Zuck
  fullname: Zuck, Paul
  organization: Department of Infectious Disease & Vaccine Research, Merck & Co., Inc., Kenilworth, New Jersey, USA
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  givenname: Bonnie J
  surname: Howell
  fullname: Howell, Bonnie J
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Snippet The aim of this study was to examine whether administering both vorinostat and disulfiram to people with HIV (PWH) on antiretroviral therapy (ART) is well...
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SubjectTerms Disulfiram - administration & dosage
Drug Therapy, Combination - adverse effects
HIV Infections - drug therapy
Humans
Virus Latency - physiology
Vorinostat - administration & dosage
Title Neurotoxicity with high-dose disulfiram and vorinostat used for HIV latency reversal
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