Drug intelligence / Profile preview

BI 1595043 + midazolam

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

Overview

**BI 1595043 + midazolam** is an experimental oral combination consisting of **BI 1595043**, a selective inhibitor of the vanin-1 and vanin-2 enzymes, and **midazolam**, a well-established short-acting benzodiazepine and CYP3A substrate. BI 1595043 was developed for its potential effects on epithelial cell protection and reduction of inflammatory mediators via vanin inhibition, and was primarily investigated for its pharmacokinetics, safety, tolerability, and bioavailability. Midazolam is commonly used as a CYP3A probe to evaluate drug-drug interactions and metabolic pathways. This combination, when studied in clinical trials, aimed to assess the pharmacokinetic interaction and bioavailability profile of BI 1595043, typically using midazolam’s CYP3A-substrate properties as an index drug. BI 1595043 development was terminated following reports of adverse ophthalmologic events in healthy volunteers.

02

Targets

VNN1 (Vanin-1)VNN2 (Vanin-2)GABRR (GABA-A receptor subunit rho)

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