Drug intelligence / Profile preview

BI 685509 + itraconazole

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

Overview

- **BI 685509 + itraconazole** is an investigational, fixed-dose combination consisting of BI 685509, a soluble guanylyl cyclase (sGC) activator, and itraconazole, an established triazole-class antifungal medication. - **BI 685509 (Avenciguat)** enhances cyclic GMP signaling by directly activating soluble guanylyl cyclase, independent of nitric oxide, and is being developed for conditions including portal hypertension, liver cirrhosis, systemic sclerosis, and diabetic kidney disease[1][5]. - **Itraconazole** inhibits fungal cell membrane synthesis by blocking cytochrome P450-dependent 14-α-demethylase (lanosterol demethylase), thereby impairing ergosterol formation in fungi, and is used clinically for a range of fungal infections[2][7]. - There is no evidence this combination is approved or marketed; it is most likely used in drug-drug interaction studies, with itraconazole acting as a CYP3A4 inhibitor to study BI 685509 pharmacokinetics.

02

Targets

CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)sGC (Soluble Guanylyl Cyclase)

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