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In vitro activity of itraconazole against SARS-CoV-2.
Van Damme, Ellen; De Meyer, Sandra; Bojkova, Denisa; Ciesek, Sandra; Cinatl, Jindrich; De Jonghe, Steven; Jochmans, Dirk; Leyssen, Pieter; Buyck, Christophe; Neyts, Johan; Van Loock, Marnix.
  • Van Damme E; Janssen Pharmaceutica NV, Beerse, Belgium.
  • De Meyer S; Janssen Pharmaceutica NV, Beerse, Belgium.
  • Bojkova D; Institute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt, Germany.
  • Ciesek S; Institute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt, Germany.
  • Cinatl J; German Center for Infection Research (DZIF), Braunschweig, Germany.
  • De Jonghe S; Institute of Medical Virology, University Hospital Frankfurt, Goethe University, Frankfurt, Germany.
  • Jochmans D; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Leyssen P; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Buyck C; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Neyts J; Janssen Pharmaceutica NV, Beerse, Belgium.
  • Van Loock M; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
J Med Virol ; 93(7): 4454-4460, 2021 Jul.
Article in English | MEDLINE | ID: covidwho-1263094
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ABSTRACT
Although vaccination campaigns are currently being rolled out to prevent coronavirus disease (COVID-19), antivirals will remain an important adjunct to vaccination. Antivirals against coronaviruses do not exist, hence global drug repurposing efforts have been carried out to identify agents that may provide clinical benefit to patients with COVID-19. Itraconazole, an antifungal agent, has been reported to have activity against animal coronaviruses. Using cell-based phenotypic assays, the in vitro antiviral activity of itraconazole and 17-OH itraconazole was assessed against clinical isolates from a German and Belgian patient infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Itraconazole demonstrated antiviral activity in human Caco-2 cells (EC50 = 2.3 µM; 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay). Similarly, its primary metabolite, 17-OH itraconazole, showed inhibition of SARS-CoV-2 activity (EC50 = 3.6 µM). Remdesivir inhibited viral replication with an EC50 = 0.4 µM. Itraconazole and 17-OH itraconazole resulted in a viral yield reduction in vitro of approximately 2-log10 and approximately 1-log10 , as measured in both Caco-2 cells and VeroE6-eGFP cells, respectively. The viral yield reduction brought about by remdesivir or GS-441524 (parent nucleoside of the antiviral prodrug remdesivir; positive control) was more pronounced, with an approximately 3-log10 drop and >4-log10 drop in Caco-2 cells and VeroE6-eGFP cells, respectively. Itraconazole and 17-OH itraconazole exert in vitro low micromolar activity against SARS-CoV-2. Despite the in vitro antiviral activity, itraconazole did not result in a beneficial effect in hospitalized COVID-19 patients in a clinical study (EudraCT Number 2020-001243-15).
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Pyrroles / Triazines / Adenosine Monophosphate / Itraconazole / Alanine / Furans / SARS-CoV-2 / COVID-19 Drug Treatment Type of study: Prognostic study Topics: Vaccines Limits: Animals / Humans Language: English Journal: J Med Virol Year: 2021 Document Type: Article Affiliation country: Jmv.26917

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Pyrroles / Triazines / Adenosine Monophosphate / Itraconazole / Alanine / Furans / SARS-CoV-2 / COVID-19 Drug Treatment Type of study: Prognostic study Topics: Vaccines Limits: Animals / Humans Language: English Journal: J Med Virol Year: 2021 Document Type: Article Affiliation country: Jmv.26917