Other substances

Itraconazole

A triazole antifungal.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

3
 Supporting references
0
 Contradictory references
8
 AI-suggested references
2
 Clinical trials

General information

Itraconazole is triazole antifungal inhibiting cytochrome P450-dependent ergesterol biosynthetic pathway (NCIt). It is also a Niemann-Pick C1 inhibitor (Zang et al., 2020).

Itraconazole on DrugBank
Itraconazole on PubChem
Itraconazole on Wikipedia

Synonyms

Sporanox; ICZ

Marketed as

ITRACONAZOLE; ITRIZOLE; ONMEL; ORICONAZOLE; SPORAL; SPORANOX; TOLSURA

 

Structure image - Itraconazole

CCC(C)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5COC(O5)(CN6C=NC=N6)C7=C(C=C(C=C7)Cl)Cl

Supporting references

Link Tested on Impact factor Notes Publication date
Identification of an Antiviral Compound from the Pandemic Response Box that Efficiently Inhibits SARS-CoV-2 Infection In Vitro
Small molecule In vitro 		Vero E6 cells; Calu-3 cells 4.15

less potent than Remdesivir

 Nov/26/2020
Cholesterol 25-hydroxylase suppresses SARS-CoV-2 replication by blocking membrane fusion
Small molecule In vitro 		Vero E6 cells; HEK293 cells; HEK293-hACE2 cells; MA104 cells; primary human intestinal epithelial cells; cardiomyocytes 9.41

Inhibited chimeric SARS-CoV-2 virus replication in vitro. It also experimentally reduced S-protein-mediated cell-to-cell fusion.

 Nov/25/2020
In vitro activity of itraconazole against SARS‐CoV‐2
Small molecule In vitro 		Caco‐2 cells; VeroE6‐eGFP cells; SARS-CoV-2 strain hCoV-19/Germany/FrankfurtFFM1/2020; SARS-CoV-2 strain BetaCov/Belgium/GHB-03021/2020 2.02

Inhibited SARS-CoV-2 infection in Caco-2 cells in a dose-dependent manner with an EC50 of 1.5 μM and 2.3 μM in two different assays. At 6.25 μM, the compound reduced SARS-CoV-2 RNA loads in Caco-2 cells by ca. 2 orders of magnitude (ca. 10 times lower reduction compared to remdesivir, however). At 1 μM, the compound reduced SARS-CoV-2 RNA loads in VeroE6-eGFP cells by a factor of ca. 10.

 Mar/05/2021

AI-suggested references

Link Publication date
Improved absorption of itraconazole tablet by co-administration with lemon beverages in a lung transplant recipient: A case report.
May/07/2022
Drug repurposing of triazoles against mucormycosis using molecular docking: A short communication.
Jul/31/2021
Development and optimization of a high-throughput screening assay for in vitro anti-SARS-CoV-2 activity: Evaluation of 5676 Phase 1 Passed Structures Development and optimization of a high-throughput screening assay for in vitro anti-SARS-CoV-2 activity:
May/07/2022
Drug synergy of combinatory treatment with remdesivir and the repurposed drugs fluoxetine and itraconazole effectively impairs SARS-CoV-2 infection in vitro
May/22/2021
Drug Repurposing of Itraconazole and Estradiol Benzoate against COVID-19 by Blocking SARS-CoV-2 Spike Protein-Mediated Membrane Fusion.
Feb/22/2021
In vitro activity of itraconazole against SARS-CoV-2
Jun/03/2021
Identification of 37 Heterogeneous Drug Candidates for Treatment of COVID-19 via a Rational Transcriptomics-Based Drug Repurposing Approach
Jun/01/2020
Combination Therapy of Ledipasvir and Itraconazole in the Treatment of COVID-19 Patients Coinfected with Black Fungus: An In Silico Statement
Aug/02/2020

Clinical trials

ID Title Status Phase Start date Completion date
NCT04962022 Drug-Drug Interaction Study Assessing Effect of Itraconazole on PF-07321332/Ritonavir in Healthy Participants Completed Phase 1 Jul/20/2021 Sep/30/2021
  • Alternative id - C4671015|2021-003308-42
  • Interventions - Drug: PF-07321332/ritonavir|Drug: Itraconazole
  • Study type - Interventional
  • Study results - No Results Available
  • Locations - Brussels Clinical Research Unit, Brussels, Bruxelles-capitale, Région DE, Belgium
  • Study designs - Allocation: Non-Randomized|Intervention Model: Crossover Assignment|Masking: None (Open Label)|Primary Purpose: Basic Science
  • Enrollment - 12
  • Age - 18 Years to 60 Years   (Adult)
  • Outcome measures - Maximum Observed Plasma Concentration (Cmax) of PF-07321332/ritonavir when administered alone|Cmax of PF-07321332/ritonavir when administered with itraconazole|Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of PF-07321332/ritonavir when administered alone|AUCinf of PF-07321332/ritonavir when administered with itraconazole|Assessment of Participants With Treatment Emergent Treatment-Related Adverse Events (AEs)|Assessment of Participants With Laboratory Abnormalities|Assessment of Participants With Vital Signs Abnormalities of PF-07321332/ritonavir|Assessment of Participants With Vital Signs Abnormalities of PF-07321332/ritonavir with itraconazole|Assessment of Abnormalities in Physical Examination (PE)|Assessment of Participants With Clinically Significant Change in Electrocardiogram (ECG) Findings of PF-07321332/ritonavir|Assessment of Participants with Clinically Significant ECG findings of PF-07321332/ritonavir with itraconazole
NCT04577378 Efficacy and Safety of Drug Combination Therapy of Isotretinoin and Some Antifungal Drugs as A Potential Aerosol Therapy for COVID-19 : An Innovative Therapeutic Approach COVID-19 Not yet recruiting Phase 2 Oct/20/2020 Nov/20/2020
  • Alternative id - Isotretinoin
  • Interventions - Drug: Drug: Isotretinoin(Aerosolized 13 cis retinoic acid) plus Aerosolized Itraconazole|Drug: Drug: Isotretinoin(Aerosolized 13 cis retinoic acid)
  • Study type - Interventional
  • Study results - No Results Available
  • Locations - Kafr El-sheikh University, Cairo, Kafr El-sheikh, Egypt
  • Study designs - Allocation: Randomized|Intervention Model: Sequential Assignment|Masking: Single (Participant)|Primary Purpose: Treatment
  • Enrollment - 45
  • Age - 15 Years to 80 Years   (Child, Adult, Older Adult)
  • Outcome measures - lung injury score|Absolute lymphocyte counts|Serum levels of CRP, ESR ,IL-1,IL-6,TNF and Type I interferons|All cause mortality rate|Serum level of viral RNA|Ventilation free days|ICU free days
Export (.csv)