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midazolam + rosuvastatin calcium + digoxin
- Development stage
- Unknown
- Lead developer
- Jemincare
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This combination is a drug cocktail consisting of midazolam, rosuvastatin calcium, and digoxin, primarily utilized in clinical pharmacology studies to evaluate drug-drug interactions (DDI). Each component serves as a probe for specific metabolic or transport pathways: midazolam is a sensitive substrate for cytochrome P450 3A4 (CYP3A4); rosuvastatin calcium is a substrate for organic anion transporting polypeptides (OATP1B1 and OATP1B3) and breast cancer resistance protein (BCRP); and digoxin is a substrate for P-glycoprotein (P-gp). By administering these drugs together, researchers can assess the inhibitory or inductive effects of an investigational drug on multiple clearance pathways simultaneously. This specific cocktail was used in Phase I trials by Jemincare to characterize the DDI profile of their candidate JMKX003142.
- Other names
- Cocktail Substrates
02
Targets
CYP3A4 (Cytochrome P450 3A4)ABCG2 (Breast cancer resistance protein)ABCB1 (P-glycoprotein)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)SLCO1B3 (Organic anion transporting polypeptide 1B3)OATP1B1 (Organic anion transporting polypeptide 1B1)GABRR (GABA-A receptor subunit rho)
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