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

NCT02434861 | Completed Phase 1

• 1 other identifier: PR-11-5021-C
• Study Type: interventional
• Target: 102
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Chemotherapy-induced Nausea and Vomiting

Outcome Measures

Primary Outcomes (2)

• AUC: area under the plasma concentration-time curve

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

  Predose - up to 120 hours postdose

• Cmax = observed maximum plasma concentration

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

  Predose - up to 120 hours postdose

Secondary Outcomes (1)

• Number of participants with adverse events

  0 - 38 days

Study Arms (3)

Part A

EXPERIMENTAL

Rolapitant IV and Digoxin

Drug: Rolapitant; Drug: Digoxin

Part B

EXPERIMENTAL

Rolapitant IV and Sulfasalazine

Drug: Rolapitant; Drug: Sulfasalazine

Part C

EXPERIMENTAL

Rolapitant IV and Cooperstown Cocktail

Drug: Rolapitant; Drug: Cooperstown Cocktail

Interventions

Rolapitant DRUG

Part A; Part B; Part C

Digoxin DRUG

P-gp substrate

Part A

Sulfasalazine DRUG

BCRP substrate

Part B

Cooperstown Cocktail DRUG

Midazolam, omeprazole, warfarin, caffeine, and dextromethorphan

Part C

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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).

Sponsors & Collaborators

• Tesaro, Inc.: lead

Study Sites (1)

Parexel Early Phase Unit

Baltimore, Maryland, 21225, United States

Location

MeSH Terms

Conditions

Vomiting

Interventions

rolapitant; Digoxin; Sulfasalazine

Condition Hierarchy (Ancestors)

Signs and Symptoms, Digestive; Signs and Symptoms; Pathological Conditions, Signs and Symptoms

Intervention Hierarchy (Ancestors)

Digitalis Glycosides; Cardenolides; Cardiac Glycosides; Cardanolides; Steroids; Fused-Ring Compounds; Polycyclic Compounds; Glycosides; Carbohydrates; Sulfonamides; Amides; Organic Chemicals; Sulfones; Sulfur Compounds

Study Officials

• Dennis Vargo, MD

  Tesaro, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: April 30, 2015
• First Posted: May 5, 2015
• Study Start: May 1, 2015
• Primary Completion: July 1, 2015
• Study Completion: August 1, 2015
• Last Updated: August 25, 2015

Record last verified: 2015-08

Locations

US (1)