Investigational Drug Details
| Drug ID: | D189 |
| Drug Name: | Itraconazole |
| Synonyms: | Itraconazole; Oriconazole |
| Type: | Chemical drug |
| DrugBank ID: | DB01167 |
| DrugBank Description: | One of the triazole antifungal agents that inhibits cytochrome P-450-dependent enzymes resulting in impairment of ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis & aspergillosis. |
| PubChem ID: | 55283 |
| CasNo: | 84625-61-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | Clc1c([C@@]2(O[C@H](CO2)COc2ccc(N3CCN(CC3)c3ccc(n4c(=O)n(nc4)C(CC)C)cc3)cc2)Cn2ncnc2)ccc(Cl)c1 |
| Structure: |
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| InChiKey: | VHVPQPYKVGDNFY-ZPGVKDDISA-N |
| Molecular Weight: | 705.647 |
| DrugBank Targets: | Lanosterol 14-alpha demethylase inhibitor; Lanosterol 14-alpha demethylase inhibitor |
| DrugBank MoA: | Itraconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Itraconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. |
| DrugBank Pharmacology: | Itraconazole is an imidazole/triazole type antifungal agent. Itraconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Itraconazole exhibits <i>in vitro</i> activity against <i>Cryptococcus neoformans</i> and <i>Candida spp.</i> Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to <i>Cryptococcus neoformans</i> and for systemic infections due to <i>Candida albicans</i>. |
| DrugBank Indication: | For the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis. |
| Targets: | P450 inhibitor |
| Therapeutic Category: | -- |
| Clinical Trial Progress: | Phase 1 completed (NCT04845646) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0145 | NCT04845646 | Phase 1 | Completed | No Results Available | March 16, 2021 | July 19, 2021 | Details |
| L0310 | NCT03213145 | Phase 1 | Completed | No Results Available | July 11, 2017 | November 6, 2017 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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