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r-norverapamil
- Development stage
- Unknown
- Lead developer
- MUW
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
R-norverapamil is the R-enantiomer of norverapamil, the primary active metabolite of the calcium channel blocker verapamil, formed via N-demethylation. It functions as an L-type calcium channel blocker and a P-glycoprotein (P-gp) inhibitor and substrate. In clinical research, particularly in studies led by the Medical University of Vienna (Medizinische Universität Wien), R-norverapamil is significant as a metabolite of the PET tracer (R)-[11C]verapamil. This tracer is used in Phase 3 imaging studies to evaluate P-glycoprotein function at the blood-brain barrier and measure cerebral blood flow, serving as a potential predictive biomarker for surgery outcomes in patients with temporal lobe epilepsy.
- Other names
- (R)-NorverapamilR-desmethylverapamilr-norverapamil
02
Targets
CYP3A4 (Cytochrome P450 3A4)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)ABCB1 (P-glycoprotein)
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