Drug intelligence / Profile preview

BI 474121 + itraconazole

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

Overview

BI 474121 + itraconazole is a combination therapy used exclusively in clinical research settings to study drug-drug interactions. BI 474121 is an investigational small molecule developed by Boehringer Ingelheim, hypothesized to be metabolized primarily via the CYP3A4 enzyme. Itraconazole is a well-known oral antifungal from the triazole class and a strong CYP3A4 inhibitor—commonly used as an index inhibitor in pharmacokinetic studies. In the referenced phase 1 clinical trial, healthy male volunteers are administered BI 474121 alone and in combination with itraconazole to assess how itraconazole affects the absorption, distribution, metabolism, and excretion of BI 474121. The combination aims to characterize potential increases in plasma levels and half-life of BI 474121 when the metabolic pathway is inhibited, with relevance for patients with Alzheimer’s disease (AD) or cognitive impairment associated with schizophrenia (CIAS) in the broader drug development program[1][3].

Brand names
Sempera
Other names
SporanoxTolsura
02

Targets

CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)PDE2 (Phosphodiesterase 2)

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