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midazolam + dabigatran etexilate + pitavastatin + rosuvastatin + atorvastatin
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A microdose cocktail containing midazolam, dabigatran etexilate, pitavastatin, rosuvastatin, and atorvastatin established for clinical drug interaction studies. This combination allows simultaneous assessment of a perpetrator's impact on the most common drug metabolizing enzyme, cytochrome P450 (CYP)3A, and major transporters including organic anion-transporting polypeptides (OATP)1B, breast cancer resistance protein (BCRP), and MDR1 P-glycoprotein (P-gp). The clinical utility of these microdose cocktail probe substrates has been validated through clinical drug interaction studies with various inhibitors.
02
Targets
ABCG2 (Breast cancer resistance protein)F2 (Thrombin)OATP1B1 (Organic anion transporting polypeptide 1B1)ABCB1 (P-glycoprotein)BZD site (GABA-A receptor benzodiazepine site)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)CYP3A4 (Cytochrome P450 3A4)SLCO1B3 (Organic anion transporting polypeptide 1B3)
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