An Open-Label, Randomized, Pivotal, Bioequivalence Study of Oral and Intravenous Rolapitant

To assess the bioequivalence of a single oral dose of 200 mg rolapitant and a single
intravenous dose of 185 mg rolapitant administered as an infusion.

Inclusion Criteria:

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

2. Female subjects of childbearing potential must have a negative pregnancy test at the
Screening visit and on Day -1.

3. Female subjects of childbearing potential must agree to use an accepted method of
birth control (excluding hormonal birth control methods) from 72 hours before
admission to the clinical unit until study completion.

4. Subjects must have a BMI from 18.5 to 32.0 kg/m2 (inclusive) and a weight of ≥ 50 kg
at the Screening visit.

5. Subjects must be able to provide informed consent after risks and benefits have been
explained. Subjects must be capable of understanding, able to sign a written informed
consent and willing to comply with the protocol requirements.

6. Subjects must be non-tobacco users (defined as a subject who has not smoked or used
nicotine products in the last 90 days before administration of study drug) and have a
negative cotinine test for nicotine at the Screening visit and Day -1.

7. Subjects must agree to discontinue intake of alcohol and beverages or food known to
interfere with CYP metabolic enzymes such as: grapefruit- and quinine-containing food
and beverages (e.g., tonic water, bitter lemon), orange juice, prune juice, pomelos,
cranberry, pomegranate, star fruit, Seville oranges (or marmalade made from them),
garlic supplements, St. John's Wort or licorice from 72 hours before admission to the
clinical unit until completion of the study.

8. Subjects must be in general good health as determined by the Investigator, based on
prestudy medical and surgical history, physical examination and clinical laboratory
tests.

9. Subjects must have cardiovascular (including 12-lead ECG) function at the Screening
visit that has no clinically significant abnormalities as determined by the
Investigator.

Exclusion Criteria:

1. 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 first study dose.

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

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

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

5. Subjects who have received any prescription medications or over-the-counter (OTC)
medications or herbal supplements within 14 days before the first study dose. By
exception, acetaminophen ≤ 1 g/day is permitted.

6. Subjects who have current or recent (within 1 year of the Screening visit) history of
alcohol abuse, illicit drug use, physical dependence or addiction to alcohol or any
opioid.

7. Cholecystectomized subjects (since biliary excretion is a predominant mode of
excretion with rolapitant).

8. Subjects who have any clinical or psychiatric condition or prior therapy that, in the
Investigator's opinion, would make the subject unsuitable for the study or unable to
comply with the dosing requirements.

9. Subjects who are unwilling or unable to avoid xanthine- and caffeine-containing
drinks (including many soft drinks, energy drinks, coffee and tea) and foods (such as
chocolate or coffee flavored) from 72 hours before admission through until the
subjects are discharged on Day 39.