Lesinurad/Allopurinol 200/300 Fixed-Dose Combination (FDC) Tablets Bioequivalence.

NCT03272425 — Phase 1, Completed, 32 participants, Ardea Biosciences, Inc.

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A Randomized, Open-label, Replicate, Crossover, 4-period Study to Assess the Bioequivalence of Lesinurad/Allopurinol Fixed-dose Combination 200/300 mg Tablets From Ardea Biosciences, Inc. (Test Drug) Versus Lesinurad, 200 mg Tablet From AstraZeneca (Comparator 1) Coadministered With Zyloric®, Allopurinol 300 mg Tablet From Aspen Pharma Industria Farmaceutica Ltda. (Comparator 2) in Healthy Female and Male Adult Subjects, Under Fasting Conditions.

Registry	NCT03272425
Status	Completed
Phase	Phase 1
Study type	Interventional; randomized, crossover, masking: none, treatment
Enrollment	32 (Actual)
Sponsor	Ardea Biosciences, Inc. (Industry)
Conditions	Gout
Interventions	lesinurad/allopurinol 200/300 FDC tablets, lesinurad 200 mg, allopurinol 300 mg (Drug)
Dates	start 2017-08-14, primary completion 2017-10-04, completion 2017-10-04, first posted 2017-09-05, last updated 2018-11-07
Locations	1 site in Brazil

-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.

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+Arms and interventions

Arm	Type	Interventions	Description
Sequence ABBA	Experimental	Drug: lesinurad/allopurinol 200/300 FDC tablets; Drug: lesinurad 200 mg; Drug: 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	Experimental	Drug: lesinurad/allopurinol 200/300 FDC tablets; Drug: lesinurad 200 mg; Drug: 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	Experimental	Drug: lesinurad/allopurinol 200/300 FDC tablets; Drug: lesinurad 200 mg; Drug: 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	Experimental	Drug: lesinurad/allopurinol 200/300 FDC tablets; Drug: lesinurad 200 mg; Drug: 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).

lesinurad/allopurinol 200/300 FDC tablets (Drug): Test Drug
lesinurad 200 mg (Drug): Comparator 1
allopurinol 300 mg (Drug): Comparator 2

+Outcome measures

Primary outcomes

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 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
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

Secondary outcomes

Incidence of Adverse Events in terms of changes in laboratory parameters [26 days]
Incidence of Adverse Events in terms of electrocardiogram 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]

+Eligibility

Sex: All, ages: 18 Years to 65 Years, accepts healthy volunteers

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.

+Locations (1)

Facility	City	Country	Status
CAEP - Centro Avançado de Estudos e Pesquisas Ltda.	Campinas, São Paulo	Brazil

+Investigators

N. Bhakta, Study director, Ardea Biosciences, Inc.