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OpenTrials
Completed

NCT Number: NCT02434861

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

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.

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Key information

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Parexel Early Phase Unit

Baltimore, Maryland, 21225, United States

About this study

  • 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.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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).

Treatment and study plan

Rolapitant

Drug

Digoxin

Drug

P-gp substrate

Sulfasalazine

Drug

BCRP substrate

Cooperstown Cocktail

Drug

Midazolam, omeprazole, warfarin, caffeine, and dextromethorphan

Primary outcomes

  1. AUC: area under the plasma concentration-time curve

    Time frame: Predose - up to 120 hours postdose

    To evaluate the effect of Rolapitant on the PK of probe substrates

  2. Cmax = observed maximum plasma concentration

    Time frame: Predose - up to 120 hours postdose

    To evaluate the effect of Rolapitant on the PK of probe substrates

Secondary outcomes

  1. Number of participants with adverse events

    Time frame: 0 - 38 days

    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.

Sponsors and collaborators

Lead sponsor

Tesaro, Inc.

Industry

Registry information

Official study title

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

Important dates

Study start
2015
Primary completion
2015
Study completion
2015
First posted
May 5, 2015
Registry last updated
Aug 25, 2015

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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