Drug intelligence / Profile preview

cilobradine + itraconazole

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Cilobradine + itraconazole is a combination of two pharmaceutical drugs: cilobradine, a selective heart rate lowering agent (If current inhibitor), and itraconazole, an azole antifungal. While itraconazole is approved for fungal infections and extensively documented, cilobradine is primarily an investigational substance for heart rate control and not widely marketed or approved. This combination is not documented in standard pharmaceutical sources as a marketed or investigational product. Mechanistically, cilobradine inhibits the cardiac pacemaker channel (“funny” channel, HCN4), reducing heart rate, while itraconazole inhibits fungal ergosterol synthesis by inhibiting lanosterol 14α-demethylase. No established indication, clinical data, or market formulation exists for the exact combination “cilobradine + itraconazole,” and there is no evidence for joint use for any disease, nor for drug-drug or pharmacodynamic interaction between the compounds[4]. Note: The combination may present interaction risks as azoles like itraconazole are strong inhibitors of cytochrome P450 3A4; if cilobradine is metabolized through this pathway, plasma levels could be affected, potentially leading to increased risk of adverse cardiac or systemic effects[4].

02

Targets

HCN4 (Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)

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