The purpose of this study is to assess the effect of food on the bio availability of
Febuxostat after a single oral dose of 80 mg febuxostat XR and to evaluate the PK of
Febuxostat after single oral doses of 40 and 80 mg Febuxostat XR.
The drug being tested in this study is called Febuxostat extended- release (XR). This study
is evaluating the effect of food on how febuxostat-XR moves throughout the body. This study
will also look at the side effects and all safety results in people who took the study drug.
This 3-way crossover study will enroll approximately 36 participants. Eligible participants
will be randomly (by chance) assigned to one of the 3 treatment sequences at 1:1:1 ratio.
Sequence defines the order in which participants receive Regimens A (Febuxostat XR 80 mg
after a high fat meal), B (Febuxostat XR 40 mg after fasting) and C (Febuxostat XR 80 mg
Sequence 1: A, B, C
Sequence 2: B, C, A
Sequence 3: C, A, B The dose in a period and the dose in the subsequent period will be
separated by a minimum 7-day washout interval. This single-centre trial will be conducted
in the United States.
Participants will make 4 visits to the clinic including three 4-day periods of confinement
to the clinic, and will be contacted by telephone 30 days after last dose of study drug for
a follow-up assessment.
1. Has an estimated glomerular filtration rate ≥90 mL/min.
2. Weighs at least 50 kg (110 pounds) and has a body mass index (BMI) from 18.0 to 30.0
kg/m^2, inclusive, at Screening.
3. A male participant who is nonsterilized and sexually active with a female partner of
childbearing potential agrees to use adequate contraception from the signing of the
informed consent throughout the duration of the study and for 30 days after the last
4. A female participant of childbearing potential who is sexually active with a
nonsterilized male partner agrees to use routinely adequate contraception from
signing of informed consent throughout the duration of the study and for 30 days
after the last dose.
5. Able to attend all the visits scheduled in the study.
6. Willing to refrain from strenuous exercise from Day -1 until Study Exit (Day 3 of
1. Hypersensitivity to Febuxostat or to any of the components of the formulation.
2. Has received any investigational compound within 30 days prior to the first dose of
3. Has received febuxostat in a previous clinical study or as a therapeutic agent.
4. Has uncontrolled, clinically significant disease or other abnormality, which may
impact the ability of the subject to participate or potentially confound the study
5. Has a known hypersensitivity to any XO inhibitor, xanthine compounds, Febuxostat or
any component of the formulation of Febuxostat tablets, or to caffeine.
6. Has a positive urine drug result for drugs of abuse at Screening or Check-in (Day -1
of Period 1).
7. Has a history of drug abuse (defined as any illicit drug use) or a history of alcohol
abuse within 1 year prior to the Screening visit or is unwilling to agree to abstain
from alcohol and drugs throughout the study.
8. Is pregnant or lactating or intending to become pregnant before, during, or within 30
days post last dose; or intending to donate ova during such time period.
9. Intends to impregnate others or donate sperm during the course of this study or for
30 days post last dose.
10. Has evidence of current cardiovascular, central nervous system, hepatic,
hematopoietic disease, renal dysfunction, metabolic or endocrine dysfunction, serious
allergy, asthma, hypoxemia, hypertension, seizures, or allergic skin rash. There is
any finding in the subject's medical history, physical examination, or safety
laboratory tests giving reasonable suspicion of a disease that would contraindicate
taking febuxostat XR, or a similar drug in the same class, or a disease that might
interfere with the conduct of the study. This includes, but is not limited to, peptic
ulcer disease, seizure disorders, and cardiac arrhythmias.
11. Has current or recent (within 6 months) gastrointestinal disease that would be
expected to influence the absorption of drugs (ie, a history of malabsorption,
esophageal reflux, peptic ulcer disease, erosive esophagitis, frequent [more than
once per week] occurrence of heartburn, or any surgical intervention [eg,
12. Has a history of cancer, except basal cell carcinoma that has been in remission for
at least 5 years prior to Day 1 of Period 1.
13. Has a positive test result for hepatitis B surface antigen (HBsAg), hepatitis C virus
(HCV) antibody or a known history of human immunodeficiency virus infection.
14. Has used nicotine-containing products (including, but not limited to, cigarettes,
pipes, cigars, chewing tobacco, nicotine patch, or nicotine gum) within 28 days prior
to Check-in (Day -1 of Period 1) or is unwilling to agree to abstain from
nicotine-containing products. Cotinine test is positive at Screening or Check-in (Day
1 of Period 1).
15. Has poor peripheral venous access.
16. Has donated or lost 450 mL or more of his or her blood volume (including
plasmapheresis) or had a transfusion of any blood product within 30 days prior to Day
1 of Period 1.
17. Has a Screening abnormal (clinically significant) ECG.
18. Has abnormal Screening or Day -1 of Period 1 laboratory values that suggest a
clinically significant underlying disease or subject with the following lab
abnormalities: ALT and/or AST >1.5 x the upper limit of normal.