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midazolam + dabigatran etexilate + pitavastatin + rosuvastatin + atorvastatin
- Development stage
- Phase 4
- 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
BZD site (GABA-A receptor benzodiazepine site)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)F2 (Thrombin)ABCG2 (Breast cancer resistance protein)SLCO1B3 (Organic anion transporting polypeptide 1B3)
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