CompletedNCT02382640Updated Apr 29, 2016Results posted

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

A Phase 1 interventional study of Febuxostat XR and Maalox Advance Regular Strength liquid in Healthy Volunteers, sponsored by Takeda. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2016-04-29.

Sponsored by Takeda · Phase 1, Interventional, and Treatment

Phase: Phase 1
Study type: Interventional
Enrollment: 36
Allocation: Randomized
Ages: 18 Years to 55 Years
Sex: All

Study 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.

Read the detailed description

The drug being tested in this study is called febuxostat extended-release (XR). Febuxostat XR is being tested to assess if antacids affect how the drug moves throughout the body. This study will look at lab safety and side effects in people who take febuxostat XR.

This cross-over study will enroll approximately 36 patients. Participants will be randomly assigned to one of four treatment sequences. All participants will receive the following study medications by the end of the study:

Febuxostat XR 80 mg capsules
Maalox Advance Regular Strength liquid containing Aluminum Hydroxide 200 mg, Magnesium Hydroxide 200 mg, and Simethicone 20 mg/5 mL or equivalent

All participants will be administered one dose of one or both of the study medications on Day 1 of four separate study periods.

This single-centre trial will be conducted in the United States. The overall time to participate in this study is up to 84 days. Participants will make 5 visits to the clinic including four 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.

Conditions studied

Healthy Volunteers

Keywords

Drug therapy

In context

Lead sponsor

Takeda is the lead sponsor of 1,002 studies on the registry; 92 are open to participants now.

Of its 173 completed or terminated interventional studies of FDA-regulated products, 149 (86%) have results posted.

Counted across the registry records on this site, refreshed daily.

Who can participate

Ages eligible: 18 Years to 55 Years
Sexes eligible: All
Accepts healthy volunteers: Yes

Inclusion criteria

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

Exclusion criteria

Exclusion Criteria:

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]).

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Randomized
Intervention model: Crossover assignment
Masking: None (open label)
Enrollment: 36 participants (actual)

Study arms

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

DrugFebuxostat XR
Febuxostat extended-release (XR) capsules
DrugMaalox Advance Regular Strength liquid
Maalox Advance Regular Strength liquid containing Aluminum Hydroxide 200 mg, Magnesium Hydroxide 200 mg, and Simethicone 20 mg/5 mL or equivalent

What researchers measure

Primary outcomes

Cmax: Maximum Observed Plasma Concentration for Febuxostat
Time frame: 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
Time frame: 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
Time frame: 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)
Time frame: 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
Time frame: 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
Time frame: 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
Time frame: 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)
Time frame: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)

Results

Posted Apr 29, 2016

Participant flow

Participants took part in the study at 1 investigative site in United States from 23-Feb-15 to 04-May-15.

Intervention Period 1 (3 Days)

Participant flow — Intervention Period 1 (3 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Washout Period 1 (7 Days)

Participant flow — Washout Period 1 (7 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Intervention Period 2 (3 Days)

Participant flow — Intervention Period 2 (3 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Washout Period 2 (7 Days)

Participant flow — Washout Period 2 (7 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Intervention Period 3 (3 Days)

Participant flow — Intervention Period 3 (3 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Washout Period 3 (7 Days)

Participant flow — Washout Period 3 (7 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	9	9	9	9
Not completed	0	0	0	0

Intervention Period 4 (3 Days)

Participant flow — Intervention Period 4 (3 Days)
Milestone	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D
Started	9	9	9	9
Completed	8	9	9	9
Not completed	1	0	0	0
Withdrew: Laboratory abnormality	1	0	0	0

Outcome measures

PrimaryCmax: Maximum Observed Plasma Concentration for Febuxostat

Time frame:: Days 1 at multiple timepoints (up to 48 hours) post-dose
Reported as:: Mean · nanogram per milliliter (ng/mL)

Cmax: Maximum Observed Plasma Concentration for Febuxostat
nanogram per milliliter (ng/mL)	Regimen A	Regimen B	Regimen C	Regimen D
Cmax: Maximum Observed Plasma Concentration for Febuxostat	883.58 ± 898.49	1075.08 ± 941.46	765.89 ± 480.2	1456.42 ± 875.39

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

Time frame:: Days 1 pre-dose and at multiple timepoints (up to 48 hours) post-dose
Reported as:: Mean · nanogram*hour per milliliter (ng*hr/mL)

AUC(0-tau): Area Under the Plasma Concentration-time Curve During the Dosing Interval for Febuxostat
nanogramhour per milliliter (nghr/mL)	Regimen A	Regimen B	Regimen C	Regimen D
AUC(0-tau): Area Under the Plasma Concentration-time Curve During the Dosing Interval for Febuxostat	4680.69 ± 2427.11	5877.99 ± 2888.9	4412.22 ± 1718.42	7316.21 ± 2811.1

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

Time frame:: Days 1 pre-dose and at multiple timepoints (up to 48 hours) post-dose
Reported as:: Mean · ng*hr/mL

AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Febuxostat
ng*hr/mL	Regimen A	Regimen B	Regimen C	Regimen D
AUC(0-inf): Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Febuxostat	5901 ± 2739.92	6999.9 ± 2912.71	4844.33 ± 1918.73	7697.85 ± 2732.63

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

Time frame:: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)
Reported as:: Number · participants

Number of Participants With Treatment-Related Adverse Events (AEs) and Serious Adverse Events (SAEs)
participants	Regimen A	Regimen B	Regimen C	Regimen D
TEAE	2	1	3	2
SAE	0	0	0	0

PrimaryNumber of Participants With Clinically Significant Change From Baseline in Vital Signs

Time frame:: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)
Reported as:: Number · participants

Number of Participants With Clinically Significant Change From Baseline in Vital Signs
participants	Regimen A	Regimen B	Regimen C	Regimen D
Number of Participants With Clinically Significant Change From Baseline in Vital Signs	0	0	0	0

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

Time frame:: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)
Reported as:: Number · participants

Number of Participants With Clinically Significant Change From Baseline in Physical Examination Findings
participants	Regimen A	Regimen B	Regimen C	Regimen D
Number of Participants With Clinically Significant Change From Baseline in Physical Examination Findings	0	0	0	0

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

Time frame:: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)
Reported as:: Number · participants

Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Evaluation
participants	Regimen A	Regimen B	Regimen C	Regimen D
Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Evaluation	0	0	0	0

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

Time frame:: Day 1 up to 30 days after last dose of drug (Day 31 for each of the 4 periods)
Reported as:: Number · participants

Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG)
participants	Regimen A	Regimen B	Regimen C	Regimen D
Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG)	0	0	0	0

Adverse events

Collected over Treatment-emergent adverse events are adverse events that started after the first dose of double-blind study drug and no more than 14 days (or 30 days for a serious adverse event) after the last dose of double-blind study drug.. Non-serious events are listed at a 0% frequency threshold.

Adverse event summary by group
Group	Deaths	Serious	Other
Regimen A	—	0/36 (0%)	2/36 (5.6%)
Regimen B	—	0/36 (0%)	1/36 (2.8%)
Regimen C	—	0/35 (0%)	3/35 (8.6%)
Regimen D	—	0/36 (0%)	2/36 (5.6%)

Most frequent other events

Most frequent other events
Event	Regimen A	Regimen B	Regimen C	Regimen D
DiarrhoeaGastrointestinal disorders	1/36	0/36	1/35	0/36
NauseaGastrointestinal disorders	0/36	0/36	1/35	0/36
HeadacheNervous system disorders	0/36	0/36	1/35	0/36
Oral herpesInjury, poisoning and procedural complications	1/36	0/36	0/35	0/36
MyalgiaMusculoskeletal and connective tissue disorders	0/36	0/36	0/35	1/36
DizzinessNervous system disorders	0/36	0/36	0/35	1/36
EcchymosisSkin and subcutaneous tissue disorders	0/36	1/36	0/35	0/36

Baseline characteristics

The safety set was defined as all participants who were enrolled and received at least 1 dose of study drug.

Age, Continuous
Age, Continuous(years)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Mean	37.8 ± 7.36	34.7 ± 13.42	31.7 ± 9.18	35.8 ± 11.38	35.0 ± 10.36

Sex: Female, Male
Sex: Female, Male(Participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Female	5	5	5	6	21
Male	4	4	4	3	15

Race/Ethnicity, Customized
Race/Ethnicity, Customized(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Hispanic or Latino	5	3	4	5	17
Not Hispanic or Latino	4	6	5	4	19

Race/Ethnicity, Customized
Race/Ethnicity, Customized(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Black or African American	1	2	4	3	10
White	8	6	5	5	24
Multiracial	0	1	0	1	2

Smoking classification
Smoking classification(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Has never smoked	8	9	8	8	33
Is an ex-smoker	1	0	1	1	3

Alcohol classification
Alcohol classification(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Has never drunk	2	4	5	4	15
Is a current drinker	4	1	1	2	8
Is an ex-drinker	3	4	3	3	13

Xanthine/caffeine consumption
Xanthine/caffeine consumption(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Had xanthine/caffeine consumption	5	5	3	5	18
Had no xanthine/caffeine consumption	4	4	6	4	18

Female reproductive status
Female reproductive status(participants)	Regimen A, Then B, Then D, Then C	Regimen D, Then A, Then C, Then B	Regimen C, Then D, Then B, Then A	Regimen B, Then C, Then A, Then D	Total
Female of childbearing potential	4	5	4	4	17
Surgically sterile	1	0	1	2	4
N/A (participant is male)	4	4	4	3	15

Study locations

1 site

Austin, Texas 78744, United States

Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on Apr 29, 2016, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT02382640
Lead sponsor: Takeda
Responsible party: Sponsor
First posted: Mar 9, 2015
Start date: Mar 2015
Primary completion: May 2015
Completion: May 2015
Results posted: Apr 29, 2016
Last update: Apr 29, 2016

Study contacts

Medical Director Clinical Science

study director · Takeda

Oversight

Data monitoring committee: No

View the source record on ClinicalTrials.gov ↗

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