Drug intelligence / Profile preview

radiprodil + itraconazole

Development stage
Unknown
Lead developer
GRIN Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Radiprodil + itraconazole is a combination of two small molecule drugs: radiprodil, a negative allosteric modulator of the NMDA receptor subunit GluN2B, and itraconazole, a triazole antifungal. This combination is under investigation to evaluate the pharmacokinetic interactions and safety profile when both agents are co-administered orally. The primary rationale for this combination in clinical research is to investigate potential drug-drug interactions—especially given that itraconazole is a strong CYP3A4 inhibitor and radiprodil's metabolism may be affected by CYP3A4 inhibition. The combination is currently being studied in healthy volunteers. Radiprodil is being developed primarily for neurological disorders such as tuberous sclerosis complex, focal cortical dysplasia, and other seizure-related disorders, while itraconazole is used as a standard antifungal agent. The combination does not have a unique brand name and is being used only in a controlled clinical trial setting for drug-drug interaction assessment[1][2][4].

02

Targets

GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)

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