Lesinurad/Allopurinol 200/300 Fixed-Dose Combination (FDC) Tablets Bioequivalence.
Phase 1
Completed
- Conditions
- Gout
- Interventions
- Registration Number
- NCT03272425
- Lead Sponsor
- Ardea Biosciences, Inc.
- Brief Summary
To assess the bioequivalence between lesinurad/allopurinol 200/300 FDC tablets and coadministered lesinurad and allopurinol tablets in the fasted state based on the pharmacokinetic (PK) evaluation of lesinurad and allopurinol in healthy adult subjects.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 32
Inclusion Criteria
- Body mass index ranging between 18.5 kg/m2 and 30 kg/m2.
- Screening serum urate level is ≤ 7.0 mg/dL.
Exclusion Criteria
- Asian subject who has a positive test for the HLA-B*5801 allele.
- History or current diagnosis of kidney stones.
- Estimated creatinine clearance, as determined at Screening, of ≤ 80 mL/min calculated by the Cockcroft-Gault formula using ideal body weight.
- Undergone major surgery within 3 months prior to Screening.
- Donated blood within 4 weeks prior to Day 1 or experienced an event (other than blood donation) of significant blood loss (> 450 mL) within 12 weeks prior to Day 1 or has given a plasma donation within 4 weeks prior to Day 1.
- Inadequate venous access or unsuitable veins for repeated venipuncture.
- Received any strong or moderate enzyme-inducing drug or product within 2 months prior to Screening.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Sequence BAAB lesinurad 200 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABBA lesinurad 200 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence BABA allopurinol 300 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABAB lesinurad/allopurinol 200/300 FDC tablets Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABAB lesinurad 200 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABBA lesinurad/allopurinol 200/300 FDC tablets Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence BABA lesinurad/allopurinol 200/300 FDC tablets Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABBA allopurinol 300 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence BABA lesinurad 200 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence BAAB lesinurad/allopurinol 200/300 FDC tablets Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence ABAB allopurinol 300 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2). Sequence BAAB allopurinol 300 mg Treatment A: Lesinurad/Allopurinol FDC Tablets - 200/300 mg (test product); Treatment B: lesinurad, tablets, 200 mg + Zyloric®, allopurinol, tablet, 300 mg (comparator 1 + comparator 2).
- Primary Outcome Measures
Name Time Method Pharmacokinetics (PK) endpoints in terms of maximum observed concentration (Cmax) for lesinurad/allopurinol 200/300 FDC tablets relative to lesinurad and allopurinol monocomponent tablets Days 1, 8, 15 and 22 Cmax is the maximum observed concentration of a drug after administration
PK endpoints in terms of time of occurrence of maximum observed concentration (tmax) for lesinurad/allopurinol 200/300 FDC tablets relative to lesinurad and allopurinol monocomponent tablets Days 1, 8, 15 and 22 Tmax is the time of occurrence of cmax
PK endpoints in terms of apparent terminal half-life (t1/2) for lesinurad/allopurinol 200/300 FDC tablets relative to lesinurad and allopurinol monocomponent tablets Days 1, 8, 15 and 22 t1/2 is a measure of apparent terminal half-life
PK endpoints in terms of area under the plasma concentration time curve from zero to the last quantifiable sampling timepoint (AUC last) for lesinurad/allopurinol 200/300 FDC tablets relative to lesinurad and allopurinol monocomponent tablets Days 1, 8, 15 and 22 AUC last is the area under the plasma concentration time curve from zero to the last quantifiable sampling timepoint
PK endpoints in terms of area under the plasma concentration time curve from and from zero to infinity (AUC 0-∞) for lesinurad/allopurinol 200/300 FDC tablets relative to lesinurad and allopurinol monocomponent tablets Days 1, 8, 15 and 22 AUC 0-∞ is a meausre of total concentration from time zero to infinity
- Secondary Outcome Measures
Name Time Method Incidence of Adverse Events in terms of changes in laboratory parameters 26 days Incidence of Adverse Events in terms of vital signs 26 days Incidence of Adverse Events in terms of physical examination findings 26 days Incidence of Adverse Events in terms of electrocardiogram parameters 26 days
Trial Locations
- Locations (1)
CAEP - Centro Avançado de Estudos e Pesquisas Ltda.
🇧🇷Campinas, Sao Paulo, Brazil