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rosuvastatin + BI 1358894
- Development stage
- Phase 1
- 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
HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)TRPC4 (Transient receptor potential cation channel subfamily C member 4)TRPC5 (Transient receptor potential Canonical-5)
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