In short
BI 1358894 is an investigational substance developed by Boehringer Ingelheim. It is being studied for use in mental health conditions. The clinical trials data includes one completed Phase 1 trial in 32 healthy women. This trial looked at whether BI 1358894 affects how the body processes a common contraceptive pill.
Key points
- BI 1358894 is an investigational drug being studied in psychiatry for mental disorders.
- The registered trial is a Phase 1 study completed in 32 healthy women.
- The trial measured how BI 1358894 affects blood levels of ethinylestradiol and drospirenone, two hormones in a contraceptive pill.
- BI 1358894 was given orally at doses of 25 mg and 100 mg in the trial.
- The study status is Completed, meaning the research has finished.
- BI 1358894 is a substituted 3,7-dihydro-1H-purine-2,6-dione compound.
What is BI 1358894?
BI 1358894 is an investigational substance being developed by Boehringer Ingelheim. It is a substituted 3,7-dihydro-1H-purine-2,6-dione compound. The substance is being studied in the therapeutic area of psychiatry and psychology, specifically for mental disorders. BI 1358894 does not currently have a marketing authorisation, meaning it is not yet an approved medicine. It is also known by its chemical name, substituted 3,7-dihydro-1H-purine-2,6-dione.
How does BI 1358894 work?
The exact mechanism of action of BI 1358894 is not described in the available sources. The registered trial data does not provide details on the molecular target of this substance. The chemical structure of BI 1358894, a substituted 3,7-dihydro-1H-purine-2,6-dione, is recorded in the European Medicines Agency decision document. The published Phase I studies in healthy male volunteers investigated the safety, tolerability and pharmacokinetics of BI 1358894, but the specific mechanism of action is not stated in the available trial record.
Which conditions is BI 1358894 studied for?
- Mental disorders — the therapeutic area recorded for BI 1358894 is psychiatry and psychology, specifically mental disorders.
- Pharmacokinetic trial — the registered clinical trial is a pharmacokinetic study in healthy women, which investigates how the body processes the drug rather than testing it in patients with a specific condition.
How is BI 1358894 given?
BI 1358894 is given orally. In the registered trial, the drug was administered as an oral dosage form at doses of 25 mg and 100 mg. The trial also involved an oral contraceptive, Yasmin®, which contains ethinylestradiol 0.03 mg and drospirenone 3 mg, also given orally.
What do the clinical trials show?
One clinical trial is registered for BI 1358894 in the EU Clinical Trials Information System. This is a Phase 1 study that has been completed. The trial enrolled 32 healthy women. The main objective was to investigate the effect of multiple oral doses of BI 1358894 on the pharmacokinetics of ethinylestradiol and drospirenone, the active ingredients in the contraceptive pill Yasmin®.
The primary outcomes measured were AUCτ,ss (the area under the concentration-time curve of the analyte in plasma at steady state over the uniform dosing interval τ) and Cmax,ss (the maximum measured concentration of the analyte in plasma at steady state over the uniform dosing interval τ). These measurements show how much of the contraceptive hormones remain in the blood when BI 1358894 is taken at the same time.
Published Phase I studies in healthy male volunteers also investigated the safety, tolerability and pharmacokinetics of single and multiple ascending doses of BI 1358894. These studies were partially randomised.
What side effects are known?
The published Phase I studies in healthy male volunteers investigated the safety and tolerability of single and multiple ascending doses of BI 1358894. The available sources do not provide a detailed list of side effects for BI 1358894. The registered trial in healthy women was a pharmacokinetic study and did not list side effect data in the trial record.
Ongoing research and future directions
The European Medicines Agency has agreed a paediatric investigation plan for BI 1358894, with a deferral and a waiver granted in September 2023. This means that studies in children may be required at a later stage, but some age groups may be exempt. The application was submitted by Boehringer Ingelheim International GmbH on 9 September 2022.