Drug intelligence / Profile preview

itraconazole + methylprednisolone

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Itraconazole + methylprednisolone is a combination of two pharmaceutical agents used together, typically in clinical or investigational settings. Itraconazole is a triazole antifungal agent that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase, disrupting ergosterol synthesis and compromising fungal cell membrane integrity. Methylprednisolone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties; it acts by binding to the glucocorticoid receptor and modulating gene expression to suppress inflammation and immune responses. When administered together, itraconazole significantly increases plasma concentrations of methylprednisolone by inhibiting hepatic CYP3A4-mediated metabolism of the corticosteroid. This pharmacokinetic interaction can lead to enhanced suppression of endogenous cortisol secretion due to higher systemic exposure to methylprednisolone[1][2][3]. The combination may be considered in certain clinical scenarios where both antifungal therapy and strong anti-inflammatory effects are required, but careful monitoring for increased steroid-related side effects is warranted.

02

Targets

CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)GR (Glucocorticoid receptor)

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