Drug intelligence / Profile preview

rosuvastatin + BI 1358894

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

Overview

**Rosuvastatin + BI 1358894** is a combination of two pharmaceutical agents: **rosuvastatin**, a statin used primarily for lipid lowering in dyslipidemias, and **BI 1358894**, a novel small-molecule inhibitor of transient receptor potential canonical (TRPC) ion channels TRPC4 and TRPC5 under development (by Boehringer Ingelheim) for the treatment of major depressive disorder and other neuropsychiatric conditions. BI 1358894 is a selective TRPC4/5 inhibitor, with primary activity modulating cortico-limbic brain regions relevant to anxiety and depression, and has completed phase I and II trials. When co-administered with rosuvastatin, BI 1358894 has been shown to increase the bioavailability of rosuvastatin (Cmax increased by ~74%) without significant new safety risks reported in phase I healthy volunteer studies. There is no indication that this combination is marketed as a fixed-dose product or has a unique brand name; rather, it has been used in clinical pharmacology studies to assess drug-drug interactions.

Other names
rosuvastatin + BI1358894
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)TRPC4 (Transient receptor potential cation channel subfamily C member 4)ABCG2 (Breast cancer resistance protein)TRPC5 (Transient receptor potential Canonical-5)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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