Food Effect Study of Febuxostat XR in Healthy Participants

NCT02374164 | Completed Phase 1 Results

• 2 other identifiers: Febuxostat-XR-1009U1111-1165-0441
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess the effect of food on the bioavailability of febuxostat after a single oral dose of 80 mg febuxostat XR and to evaluate the pharmacokinetics (PK) of febuxostat after single oral doses of 40 and 80 mg febuxostat XR.

Conditions

Gout

Keywords

Drug therapy

Outcome Measures

Primary Outcomes (6)

• Cmax: Maximum Observed Plasma Concentration for Febuxostat XR 80 mg in Fed (Regimen A) and Fasted (Regimen C) States

  Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple timepoints (up to 48 hours) post dose

• Cmax: Maximum Observed Plasma Concentration for Febuxostat XR 40 mg (Regimen B) and Febuxostat XR 80 mg (Regimen C) in Fasted States

  Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple time points (up to 48 hours) post dose

• AUCt: Area Under the Plasma Concentration-Time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration for Febuxostat XR 80 mg in Fed (Regimen A) and Fasted (Regimen C) States

  AUCt is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration. Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple timepoints (up to 48 hours) post dose

• AUCt: Area Under the Plasma Concentration-Time Curve (AUC) From Time 0 to Time of the Last Quantifiable Concentration for Febuxostat XR 40 mg (Regimen B) and Febuxostat XR 80 mg (Regimen C) in Fasted States

  AUCt is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUCt) Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple timepoints (up to 48 hours) post dose

• AUCinf: Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity for Febuxostat XR 80 mg in Fed (Regimen A) and Fasted (Regimen C) States

  AUCinf is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple timepoints (up to 48 hours) post dose

• AUCinf: Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity for Febuxostat XR 40 mg (Regimen B) and Febuxostate XR 80 mg (Regimen C) in Fasted States

  AUCinf is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. Participant blood samples were collected pre-dose and following a single oral dose.

  Day 1 pre-dose and at multiple timepoints (up to 48 hours) post dose

Study Arms (3)

Treatment Sequence ABC

EXPERIMENTAL

Febuxostat extended release (XR) 80 mg, capsules, orally, once on Day 1 of Period 1 after a high-fat meal, followed by a 7-day washout period, followed by febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 2 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80, capsules, orally, once on Day 1 of Period 3 after a 10-hour fast.

Drug: Febuxostat XR

Treatment Sequence BCA

EXPERIMENTAL

Febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 1 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 2 after a 10-hour fast, followed by a 7-day washout period, followed by Febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 3 after a high-fat meal.

Drug: Febuxostat XR

Treatment Sequence CAB

EXPERIMENTAL

Febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 1 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 2 after a high-fat meal, followed by a 7-day washout period, followed by febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 3 after a 10-hour fast.

Drug: Febuxostat XR

Interventions

Febuxostat XR DRUG

Febuxostat XR capsules

Treatment Sequence ABC; Treatment Sequence BCA; Treatment Sequence CAB

Eligibility Criteria

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

You may qualify if:

• Has an estimated glomerular filtration rate ≥90 mL/min.
• 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.
• 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 dose.
• 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.
• Able to attend all the visits scheduled in the study.
• Willing to refrain from strenuous exercise from Day -1 until Study Exit (Day 3 of Period 3).

You may not qualify if:

• Hypersensitivity to Febuxostat or to any of the components of the formulation.
• Has received any investigational compound within 30 days prior to the first dose of study medication.
• Has received febuxostat in a previous clinical study or as a therapeutic agent.
• Has uncontrolled, clinically significant disease or other abnormality, which may impact the ability of the participant to participate or potentially confound the study results.
• Has a known hypersensitivity to any xanthine oxidase (XO) inhibitor, xanthine compounds, Febuxostat or any component of the formulation of Febuxostat tablets, or to caffeine.
• Has a positive urine drug result for drugs of abuse at Screening or Check-in (Day -1 of Period 1).
• 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.
• 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.
• Intends to impregnate others or donate sperm during the course of this study or for 30 days post last dose.
• 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 participant'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.
• 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 \[eg, cholecystectomy\]).
• 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.
• 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.
• 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).
• Has poor peripheral venous access.

Sponsors & Collaborators

• Takeda: lead

Study Sites (1)

Unknown Facility

Austin, Texas, United States

Location

MeSH Terms

Conditions

Gout

Condition Hierarchy (Ancestors)

Arthritis; Joint Diseases; Musculoskeletal Diseases; Crystal Arthropathies; Rheumatic Diseases; Purine-Pyrimidine Metabolism, Inborn Errors; Metabolism, Inborn Errors; Genetic Diseases, Inborn; Congenital, Hereditary, and Neonatal Diseases and Abnormalities; Metabolic Diseases; Nutritional and Metabolic Diseases

Results Point of Contact

• Title: Medical Director, Clinical Science
• Organization: Takeda

trialdisclosures@takeda.com

+1-877-825-3327

Study Officials

• Medical Director Clinical Science

  Takeda

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 22, 2015
• First Posted: February 27, 2015
• Study Start: February 1, 2015
• Primary Completion: March 1, 2015
• Study Completion: April 1, 2015
• Last Updated: April 27, 2016
• Results First Posted: April 27, 2016

Record last verified: 2016-03

Locations

US (1)