Drug intelligence / Profile preview

itraconazole + prednisolone

Development stage
Unknown
Lead developer
OMJ Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Itraconazole + prednisolone is a combination of two pharmaceutical agents used primarily in the management of acute-stage allergic bronchopulmonary aspergillosis (ABPA) complicating asthma. Itraconazole is a triazole antifungal that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase, thereby impairing ergosterol synthesis and disrupting fungal cell membrane formation. Prednisolone is a synthetic glucocorticoid with potent anti-inflammatory and immunosuppressive properties, acting via the glucocorticoid receptor to modulate gene expression and suppress immune responses. The rationale for combining these drugs in ABPA is to target both the underlying hypersensitivity inflammation (with prednisolone) and reduce fungal burden (with itraconazole). Clinical studies suggest this combination may reduce exacerbation rates compared to monotherapy, though results have not reached statistical significance[1][5][6]. Drug-drug interactions are notable; itraconazole can increase systemic steroid exposure by inhibiting CYP3A4-mediated metabolism of corticosteroids[1][2][3].

02

Targets

GR (Glucocorticoid receptor)CYP51A1 (Sterol 14α-demethylase)

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