The objective of this Open Label Study is to evaluate effects of Rolapitant IV solution, and its metabolite, on the pharmacokinetics (PK) of the P-gp substrate (digoxin), the BCRP substrate (sulfasalazine), and multiple cytochrome P450 (CYP) probe substrates in a healthy adult population.
* Part A will compare the PK of oral digoxin alone and in combination with an IV infusion of rolapitant. * Part B will compare the PK of an oral dose of sulfasalazine alone to the PK of an oral dose of sulfasalazine in combination with an IV infusion of rolapitant * Part C will compare the PK of an oral dose of the Cooperstown Cocktail (midazolam, omeprazole, warfarin, caffeine, and dextromethorphan) alone and when given in combination with an IV infusion of rolapitant.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
102
P-gp substrate
BCRP substrate
Midazolam, omeprazole, warfarin, caffeine, and dextromethorphan
Parexel Early Phase Unit
Baltimore, Maryland, United States
AUC: area under the plasma concentration-time curve
To evaluate the effect of Rolapitant on the PK of probe substrates
Time frame: Predose - up to 120 hours postdose
Cmax = observed maximum plasma concentration
To evaluate the effect of Rolapitant on the PK of probe substrates
Time frame: Predose - up to 120 hours postdose
Number of participants with adverse events
To evaluate the safety and tolerability of combination administration of the P-gp substrate (digoxin), the BCRP substrate (sulfasalazine), and CYP probe substrates (midazolam, omeprazole, warfarin, caffeine, and dextromethorphan \[Cooperstown Cocktail\]) with a single dose of rolapitant IV in a healthy adult population, as assessed by incidence and severity of AEs.
Time frame: 0 - 38 days
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