Drug intelligence / Profile preview

balcinrenone + itraconazole

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of balcinrenone (AZD9977) and itraconazole refers to a clinical study regimen used to evaluate drug-drug interactions. Balcinrenone is a novel, selective, nonsteroidal mineralocorticoid receptor (MR) modulator developed by AstraZeneca for the treatment of heart failure and chronic kidney disease. It acts as a partial MR antagonist, providing cardio-renal protection with a reduced risk of hyperkalemia compared to traditional MR antagonists like eplerenone. Itraconazole is a triazole antifungal agent and a potent inhibitor of the Cytochrome P450 3A4 (CYP3A4) enzyme. Because balcinrenone is a substrate for CYP3A4, this combination is primarily investigated in Phase 1 clinical pharmacology trials (such as NCT03909750) to determine the impact of strong CYP3A4 inhibition on the pharmacokinetic profile, safety, and tolerability of balcinrenone.

Brand names
Sporanox
Other names
AZD9977 + itraconazolebalcinrenone + itraconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)MR (Mineralocorticoid receptor)

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