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CYP and transporter probe substrates cocktail
- Development stage
- Unknown
- Lead developer
- ViiV Healthcare
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A cocktail of eight specific probe substrates used in clinical pharmacology to evaluate the drug-drug interaction (DDI) potential of investigational compounds. In the context of ViiV Healthcare's development of the HIV-1 maturation inhibitor BMS-955176, this cocktail was administered to healthy subjects to determine if BMS-955176 inhibits or induces key metabolic enzymes and transporters. The cocktail consists of caffeine (probes CYP1A2), metoprolol (probes CYP2D6), montelukast (probes CYP2C8), flurbiprofen (probes CYP2C9), omeprazole (probes CYP2C19), midazolam (probes CYP3A), digoxin (probes P-gp), and pravastatin (probes OATP1B1/1B3). By analyzing the plasma concentrations of these probes, researchers can predict how the investigational drug might interact with other medications commonly prescribed to HIV patients.
- Other names
- CYP and transporter probe substratesBMS-955176 DDI probe cocktailBMS955176 DDI probe cocktailBMS 955176 DDI probe cocktail
02
Targets
CYP2C19 (Cytochrome P450 2C19)OATP1B1 (Organic anion transporting polypeptide 1B1)CYP1A2 (Cytochrome P450 1A2)SLCO1B3 (Organic anion transporting polypeptide 1B3)ABCB1 (P-glycoprotein)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP2C8 (Cytochrome P450 2C8)
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