Effect of Antacid on Bioavailability of Febuxostat After Administration of a Febuxostat 80 mg Extended-Release Capsule

NCT02382640 | Completed Phase 1 Results

• 2 other identifiers: Febuxostat XR-1010U1111-1163-1813
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess the effect of antacid administration, and its timing, on the bioavailability of a single dose of febuxostat extended-release (XR) 80 mg.

Conditions

Healthy Volunteers

Keywords

Drug therapy

Outcome Measures

Primary Outcomes (8)

• Cmax: Maximum Observed Plasma Concentration for Febuxostat

  Days 1 at multiple timepoints (up to 48 hours) post-dose

• AUC(0-tau): Area Under the Plasma Concentration-time Curve During the Dosing Interval for Febuxostat

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

• AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Febuxostat

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

• Number of Participants With Treatment-Related Adverse Events (AEs) and Serious Adverse Events (SAEs)

  Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

• Number of Participants With Clinically Significant Change From Baseline in Vital Signs

  Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

• Number of Participants With Clinically Significant Change From Baseline in Physical Examination Findings

  Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

• Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Evaluation

  Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

• Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG)

  Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

Study Arms (4)

Sequence 1: ABDC

EXPERIMENTAL

Experimental: Sequence 1: ABDC Febuxostat 80 mg extended-release (XR) capsule, orally, once, after a 10-hour fast, and 20 mL Maalox Advance Regular Strength liquid containing Aluminum Hydroxide 200 mg, Magnesium Hydroxide 200 mg, and Simethicone 20 mg/5 mL (hereafter referred as Maalox) or equivalent, orally, once, after a 10-hour fast, on Day 1 of Period 1 (A), followed by a 7-day washout period, followed by Maalox or equivalent, orally, once, after a 9-hour fast, and febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast (1 hour after Maalox or equivalent), on Day 1 of Period 2 (B), followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, on Day 1 of Period 3 (D), followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after an 11-hour fast (1 hour after febuxostat), on Day 1 of Period 4 (C).

Drug: Febuxostat XR; Drug: Maalox Advance Regular Strength liquid

Sequence 2: DACB

EXPERIMENTAL

Experimental: Sequence 2: DACB Febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, on Day 1 of Period 1, followed by a 7-day washout period, followed by febuxostat 80 mg extended-release (XR) capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after a 10-hour fast, on Day 1 of Period 2, followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after an 11-hour fast (1 hour after febuxostat), on Day 1 of Period 3, followed by a 7-day washout period, followed by Maalox or equivalent, orally, once, after a 9-hour fast, and febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast (1 hour after Maalox or equivalent), on Day 1 of Period 4.

Drug: Febuxostat XR; Drug: Maalox Advance Regular Strength liquid

Sequence 3: CDBA

EXPERIMENTAL

Febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after an 11-hour fast (1 hour after febuxostat), on Day 1 of Period 1, followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, on Day 1 of Period 2, followed by a 7-day washout period, followed by Maalox or equivalent, orally, once, after a 9-hour fast, and febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast (1 hour after Maalox or equivalent), on Day 1 of Period 3, followed by a 7-day washout period, followed by Febuxostat 80 mg extended-release (XR) capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after a 10-hour fast, on Day 1 of Period 4.

Drug: Febuxostat XR; Drug: Maalox Advance Regular Strength liquid

Sequence 4: BCAD

EXPERIMENTAL

Maalox or equivalent, orally, once, after a 9-hour fast, and febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast (1 hour after Maalox), on Day 1 of Period 1, followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after an 11-hour fast (1 hour after febuxostat), on Day 1 of Period 2, followed by a 7-day washout period, followed by febuxostat 80 mg extended-release (XR) capsule, orally, once, after a 10-hour fast, and Maalox or equivalent, orally, once, after a 10-hour fast, on Day 1 of Period 3, followed by a 7-day washout period, followed by febuxostat 80 mg XR capsule, orally, once, after a 10-hour fast, on Day 1 of Period 4.

Drug: Febuxostat XR; Drug: Maalox Advance Regular Strength liquid

Interventions

Febuxostat XR DRUG

Febuxostat extended-release (XR) capsules

Sequence 1: ABDC; Sequence 2: DACB; Sequence 3: CDBA; Sequence 4: BCAD

Maalox Advance Regular Strength liquid DRUG

Maalox Advance Regular Strength liquid containing Aluminum Hydroxide 200 mg, Magnesium Hydroxide 200 mg, and Simethicone 20 mg/5 mL or equivalent

Sequence 1: ABDC; Sequence 2: DACB; Sequence 3: CDBA; Sequence 4: BCAD

Eligibility Criteria

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

You may qualify if:

• Is a healthy adult male or female aged 18 to 55 years, inclusive, by check-in (Day-1 of Period 1)
• Weighs at least 50 kg (110 pounds), and has a body mass index (BMI) between 18.0 kg/m\^2 to 30 kg/m\^2, inclusive at Screening.
• Has estimated glomerular filtration rate ≥90 mL/min

You may not qualify if:

• Any participant who meets any of the following criteria will not qualify for entry into the study:
• 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 a known hypersensitivity to any xanthine oxidase inhibitor, xanthine compounds or any component of the formulation of febuxostat tablets (see Package Insert) or to caffeine.
• Has a known hypersensitivity to aluminum, magnesium hydroxide, or any component of the formulation of antacid (Maalox Advanced Regular Strength or equivalent) (see Package Insert).
• 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. If female, the participant is pregnant or lactating or intending to become pregnant before, during, or within 30 days after participating in this study; or intending to donate ova during such time period.
• 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 \[eg, cholecystectomy\]).

Sponsors & Collaborators

• Takeda: lead

Study Sites (1)

Unknown Facility

Austin, Texas, 78744, United States

Location

Results Point of Contact

• Title: Medical Director
• 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: March 3, 2015
• First Posted: March 9, 2015
• Study Start: March 1, 2015
• Primary Completion: May 1, 2015
• Study Completion: May 1, 2015
• Last Updated: April 29, 2016
• Results First Posted: April 29, 2016

Record last verified: 2016-03

Locations

US (1)