An Open Label, Single Dose, Three Part Study to Assess the Effects of Rolapitant (2 mg/mL IV Solution) on the Pharmacokinetics of Digoxin; Sulfasalazine; and the Cooperstown Cocktail (Midazolam, Omeprazole, Warfarin, Caffeine, and Dextromethorphan in Healthy Subjects



Status:Completed
Conditions:Cancer
Therapuetic Areas:Oncology
Healthy:No
Age Range:18 - 55
Updated:4/21/2016
Start Date:May 2015
End Date:August 2015

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An Open Label, Single Dose, Three Part Study to Assess the Effects of Rolapitant (1.8 mg/mL Rolapitant IV Solution) on the Pharmacokinetics of Digoxin (P-gp); Sulfasalazine (BCRP); and the Cooperstown Cocktail (Midazolam [CYP3A4], Omeprazole [CYP2C19], Warfarin [CYP2C9], Caffeine [CYP1A2], and Dextromethorphan [CYP2D6]) in Healthy Subjects

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.

Main Inclusion Criteria:

- Subjects must be healthy males or females aged 18 to 55 years (inclusive)

- Female subjects (of childbearing potential) must have a negative pregnancy test at
Screening and on Day -1

- Female subjects of childbearing potential must agree to use an accepted method of
birth control (excluding hormonal birth control methods) before Visit 1 and to
continue its use during the study and for at least 30 days after the final dose

- Subjects must have a body mass index (BMI) from 18.5 to 32.0 kg/m2 (inclusive) and a
weight of ≥50 kg at Screening

- Subjects must be capable of understanding the informed consent after the risks and
benefits of the study have been explained; subjects must be able to sign a written
informed consent and be willing to comply with the protocol requirements

- Subjects must be in general good health as determined by the Investigator based on
pre-study medical and surgical history, physical examination [PE], and clinical
laboratory tests

Main Exclusion Criteria:

- Subjects who have participated in another investigational study within 30 days or 5
half-lives of the test drug's biologic activity, whichever is longer, before the time
of the first study dose

- Subjects who have a history of relevant allergies (including asthma, food, or drug
allergies) as determined by the Investigator

- Subjects who have had significant blood loss, or have donated or received ≥1 units
(450 mL) of blood, within 30 days before the first study dose

- Subjects who have a history of hypersensitivity to rolapitant IV or any of its
excipients or who have participated in a previous rolapitant study within 6 months
prior to administration of the first dose of study drug (Day 1)

- Subjects with poor venous access and/or cannot tolerate venipuncture

- Subjects with a history of significant complications or anxiety associated with the
IV administration of medications that, in the opinion of the Investigator, could make
the subject

- Subjects who have a history of hypersensitivity to sulfasalazine (Part B only).
We found this trial at
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Baltimor, Maryland 21225
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Baltimor, MD
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