Bioequivalence Study of Combination Tablets of Saxagliptin / Dapagliflozin / Metformin XR (Extended-release) and Dapagliflozin / Metformin XR Relative to Individual Components in Healthy Subjects

NCT ID: NCT03138356

Last Updated: 2017-12-07

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

126 participants

Study Classification

INTERVENTIONAL

Study Start Date

2017-05-25

Study Completion Date

2017-11-28

Brief Summary

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In this integrated, Phase I study, the safety, tolerability, food effect, and pharmacokinetic (PK) properties of Fixed-Dose Combination Tablets of Saxagliptin / Dapagliflozin / Metformin XR and Dapagliflozin / Metformin XR Relative to Individual Components in Healthy Subjects will be investigated.

Detailed Description

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This study will be an open-label, randomized, 3-period, 3-treatment, single-dose crossover study in healthy subjects (males and females), performed at a single study center, conducted in 3 cohorts. A total of 126 healthy male or female subjects (3 cohorts of 42 subjects each \[each cohort consisting of 3 treatments\]) will be randomized in this study to ensure that at least 108 subjects (36 in each cohort) are evaluable. Each subject will receive 3 single-dose treatments, and each treatment will be administered within 1 of the 3 successive treatment periods. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences with 7 subjects prescribing the ordered sequence of 3 administered treatments in each treatment sequence, and will receive the IMPs in either a fasted or fed-state according to the assigned treatment. For fed-state cohorts, all doses of study drug will be administered to subjects after consuming a standard meal (light fat, low calorie) in the morning. Subjects will start consuming the meal 30 minutes prior to the dose and will finish the meal within 25 minutes. Dosing will then start after 30 minutes after the start of the meal. Subjects in the fasted state cohort will be fasted overnight (at least 10 hours) before dosing

The study will comprise:

* A Screening period of maximum 28 days;
* Three treatment periods during which subjects will be resident in the Unit from the day before dosing with the IMP (Day -1) until at least 72 hours after dosing; discharged on the morning of Day 4; and
* A final Follow-up Visit within 5 to 7 days after the last administration of the IMP.

There will be a minimum washout period of 7 to 14 days between each dose administration

Conditions

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Type 2 Diabetes Mellitus

Keywords

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Type 2 diabetes mellitus, saxagliptin, dapagliflozin, metformin XR, fixed-dose combination, healthy subjects, crossover, cohorts.

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

CROSSOVER

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Cohort 1 Treatment A

Single-dose of saxagliptin (2.5 mg), dapagliflozin (5 mg), metformin (1000 mg) XR (Extended-release) FDC (Fixed-dose combination) tablet administered orally under fasted condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (ABC), (ACB), (BAC), (BCA), (CAB) or (CBA).

Group Type EXPERIMENTAL

2.5 mg saxagliptin / 5 mg dapagliflozin / 1000 mg metformin XR FDC tablet

Intervention Type DRUG

Used in Treatment A and Treatment D.

Cohort 1 Treatment B

Single-dose of saxagliptin (2.5 mg), dapagliflozin (5 mg), metformin (850 mg) XR FDC tablet, administered orally under fasted condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (ABC), (ACB), (BAC), (BCA), (CAB) or (CBA).

Group Type EXPERIMENTAL

2.5 mg saxagliptin / 5 mg dapagliflozin / 850 mg metformin XR FDC tablet

Intervention Type DRUG

Used in Treatment B and Treatment E.

Cohort 1 Treatment C (Reference product)

Single-dose of Onglyza® (2.5 mg saxagliptin), Forxiga® (5 mg dapagliflozin) and Glucophage XR® (2 x 500 mg metformin XR) co-administered under fasted condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (ABC), (ACB), (BAC), (BCA), (CAB) or (CBA).

Group Type ACTIVE_COMPARATOR

2.5 mg ONGLYZA® (saxagliptin) tablet

Intervention Type DRUG

Used in treatments C and F.

5 mg Forxiga® (dapagliflozin) tablet

Intervention Type DRUG

Used in treatments C, F and I.

500 mg Glucophage XR®

Intervention Type DRUG

Used in treatments C, F and I.

Cohort 2 Treatment D

Single-dose of saxagliptin (2.5 mg), dapagliflozin (5 mg), metformin (1000 mg) XR FDC tablet administered orally under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state

The treatment sequences are (DEF), (DFE), (EDF), (EFD), (FDE) or (FED).

Group Type EXPERIMENTAL

2.5 mg saxagliptin / 5 mg dapagliflozin / 1000 mg metformin XR FDC tablet

Intervention Type DRUG

Used in Treatment A and Treatment D.

Cohort 2 Treatment E

Single-dose of saxagliptin (2.5 mg), dapagliflozin (5 mg), metformin (850 mg) XR FDC tablet, administered orally under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (DEF), (DFE), (EDF), (EFD), (FDE) or (FED).

Group Type EXPERIMENTAL

2.5 mg saxagliptin / 5 mg dapagliflozin / 850 mg metformin XR FDC tablet

Intervention Type DRUG

Used in Treatment B and Treatment E.

Cohort 2 Treatment F (Reference Product)

Single-dose of Onglyza® (2.5 mg saxagliptin), Forxiga® (5 mg dapagliflozin) and Glucophage XR® (2 x 500 mg metformin) co-administered under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (DEF), (DFE), (EDF), (EFD), (FDE) or (FED).

Group Type ACTIVE_COMPARATOR

2.5 mg ONGLYZA® (saxagliptin) tablet

Intervention Type DRUG

Used in treatments C and F.

5 mg Forxiga® (dapagliflozin) tablet

Intervention Type DRUG

Used in treatments C, F and I.

500 mg Glucophage XR®

Intervention Type DRUG

Used in treatments C, F and I.

Cohort 3 Treatment G

Single-dose dapagliflozin (5 mg) / metformin (1000 mg) XR FDC tablet administered orally under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (GHI), (GIH), (HGI), (HIG), (IHG) or (IGH).

Group Type EXPERIMENTAL

5 mg dapagliflozin / 1000 mg metformin XR FDC

Intervention Type DRUG

Used in Treatment G.

Cohort 3 Treatment H

Single-dose dapagliflozin (5 mg) / metformin (850 mg) XR FDC tablet administered orally under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (GHI), (GIH), (HGI), (HIG), (IHG) or (IGH).

Group Type EXPERIMENTAL

5 mg dapagliflozin / 850 mg metformin XR FDC

Intervention Type DRUG

Used in Treatment H.

Cohort 3 Treatment I (Reference Product)

Single-dose Forxiga® (5 mg dapagliflozin) and Glucophage XR® (2 x 500 mg metformin) co-administered under fed condition. Within each cohort, subjects will be randomized to 1 of 6 treatment sequences, each subject will receive 3 single-dose treatments in either a fasted or fed-state.

The treatment sequences are (GHI), (GIH), (HGI), (HIG), (IHG) or (IGH).

Group Type ACTIVE_COMPARATOR

5 mg Forxiga® (dapagliflozin) tablet

Intervention Type DRUG

Used in treatments C, F and I.

500 mg Glucophage XR®

Intervention Type DRUG

Used in treatments C, F and I.

Interventions

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2.5 mg saxagliptin / 5 mg dapagliflozin / 850 mg metformin XR FDC tablet

Used in Treatment B and Treatment E.

Intervention Type DRUG

2.5 mg saxagliptin / 5 mg dapagliflozin / 1000 mg metformin XR FDC tablet

Used in Treatment A and Treatment D.

Intervention Type DRUG

5 mg dapagliflozin / 850 mg metformin XR FDC

Used in Treatment H.

Intervention Type DRUG

5 mg dapagliflozin / 1000 mg metformin XR FDC

Used in Treatment G.

Intervention Type DRUG

2.5 mg ONGLYZA® (saxagliptin) tablet

Used in treatments C and F.

Intervention Type DRUG

5 mg Forxiga® (dapagliflozin) tablet

Used in treatments C, F and I.

Intervention Type DRUG

500 mg Glucophage XR®

Used in treatments C, F and I.

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

* For inclusion in the study subjects should fulfill the following criteria:

1. Provision of signed and dated, written informed consent prior to any study specific procedures.
2. Healthy male and/or female subjects aged 18 to 55 years with suitable veins for cannulation or repeated venipuncture.
3. Female subject must either:

3.1. Be of non-childbearing potential:

* Must have a negative serum pregnancy test (minimum sensitivity 25 IU/L or equivalent units of human chorionic gonadotropin) at Screening and negative urine pregnancy test within 24 hours prior to first IMP administration.
* Documentation of irreversible surgical sterilization by hysterectomy, bilateral oophorectomy or bilateral salpingectomy but not tubal ligation. 3.2. Or, if of childbearing potential:
* Must have a negative serum pregnancy test (minimum sensitivity 25 IU/L or equivalent units of human chorionic gonadotropin) at Screening and within 24 hours prior to first IMP administration.
* Must not be nursing (breastfeeding).
* If heterosexually active, agree to consistently use a highly effective method of contraception to avoid pregnancy, from at least 4 weeks prior to dosing and throughout the study and for up to 90 days after the last dose of IMP. 4. Sexually active fertile male subjects must use effective birth control for the entire study and 90 days after the last dose of IMP if their partners are women of childbearing potential. 5. Have a body mass index (BMI) between 18 and 32 kg/m2 inclusive and weigh at least 50 kg and no more than 100 kg inclusive.

Exclusion Criteria

1. History of any clinically significant disease or disorder which, in the opinion of the PI, may either put the volunteer at risk because of participation in the study, or influence the results or the volunteer's ability to participate in the study.
2. Current or recent (within 3 months of first IMP dosing) gastrointestinal disease that may impact drug absorption and affect the PK of the study drugs. Additionally, any gastrointestinal surgery (e.g., partial gastrectomy, pyloroplasty) including cholecystectomy that may impact drug absorption.
3. Any major surgery, as determined by the investigator, within 4 weeks of first IMP dosing.
4. Donation of \> 400 mL of blood within 8 weeks or donation of plasma (except at the Screening Visit) within 4 weeks of first IMP dosing.
5. Blood transfusion within 4 weeks of first IMP dosing.
6. Inability to tolerate oral medication.
7. Inability to tolerate venipuncture or inadequate venous access as determined by the investigator.
8. Recent (within 6 months of first IMP dosing) drug or alcohol abuse as defined in the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition (DSM-IV), Diagnostic Criteria for Drug and Alcohol Abuse.
9. Subjects who drink more than 3 cups of coffee or other caffeinecontaining products a day, or 5 cups of tea a day.
10. Use of tobacco-containing or nicotine-containing products (including but not limited to cigarettes, pipes, cigars, chewing tobacco, nicotine patches, nicotine lozenges, or nicotine gum) within 6 months prior to first check-in (Day -1, Treatment Period 1), or a positive nicotine test (i.e., cotinine) at Screening and/or check-in.
11. History of diabetes mellitus.
12. History of heart failure.
13. History of chronic or recurrent urinary tract infection (defined as 3 occurrences per year)
14. Recent vulvovaginal mycotic infection (within 2 months prior to first IMP dosing).
15. Any other sound medical, psychiatric and/or social reason as determined by the investigator.
16. Any clinically significant illness, medical/surgical procedure, or trauma within 4 weeks of Screening.
17. Any positive result on screening for serum hepatitis B surface antigen, hepatitis C antibody, and human immunodeficiency virus (HIV) antibody.
18. Has received another new chemical entity (defined as a compound which has not been approved for marketing) within 3 months of the first administration of IMP in this study. The period of exclusion begins 3 months after the final dose or one month after the last visit whichever is the longest. Note: subjects consented and screened, but not randomized in this study or a previous Phase1 study, are not excluded.
19. History of severe allergy/hypersensitivity or ongoing allergy/hypersensitivity, as judged by the PI or history of hypersensitivity to drugs with a similar chemical structure or class to saxagliptin, dapagliflozin and metformin.
20. Positive screen for drugs of abuse or cotinine at Screening or on first admission to the study center or positive screen for alcohol on first admission to the study center
21. Use of saxagliptin, dapagliflozin and/or metformin within 3 months prior to the first administration of IMP.
22. Use of any prescription drugs or OTC acid controllers within 4 weeks prior to the first administration of IMP except medication cleared by the medical monitor.
23. Use of drugs with enzyme-inducing properties such as St John's Wort within 3 weeks prior to the first administration of IMP.
24. Use of any prescribed or non-prescribed medication including analgesics (other than paracetamol/acetaminophen), herbal remedies, megadose vitamins (intake of 20 to 600 times the recommended daily dose) and minerals during the 2 weeks prior to the first administration of IMP or longer if the medication has a long half-life. Note: Hormonal replacement therapy is not allowed.
25. Involvement of any AstraZeneca, PAREXEL or study site employee or their close relatives.
26. Vulnerable subjects, e.g., kept in detention, protected adults under guardianship, trusteeship, or committed to an institution by governmental or juridical order.
Minimum Eligible Age

18 Years

Maximum Eligible Age

55 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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AstraZeneca

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Pablo ForteSoto, MD, MSc, PhD

Role: PRINCIPAL_INVESTIGATOR

PAREXEL Early Phase Clinical Unit London

Locations

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Research Site

Harrow, , United Kingdom

Site Status

Countries

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United Kingdom

Other Identifiers

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D168AC00002

Identifier Type: -

Identifier Source: org_study_id