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Dapagliflozin/metformin 5

Phase 1

Healthy Subjects in Fasted and Fed State | Small molecule | Other |AstraZeneca PLC|Last Updated: Apr 29, 2022

Target and mechanism

Molecular targetSLC5A2
Target classInhibitor
ModalitySmall molecule

Also known as Dapagliflozin

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLED
Total Trials1
Total Enrollment284

FDA Designations

No designations recorded

Clinical trial landscape

Dapagliflozin/metformin 5 · 2 trials · 2 indications

Phase 1 2
NCT04856007A Study to Assess the Bioequivalence of Fixed Dose Combination of Dapagliflozin/Metformin XR Relative to Co-administration of the Individual Components in Healthy Chinese Subjects.Healthy Volunteer
COMPLETED80 Analytics
NCT03216278The Purpose of the Study is to Compare Two Fixed Dose Combination Tablets of Dapagliflozin/Metformin XR in Healthy Subjects Under Fasting and Fed ConditionsHealthy Subjects in Fasted and Fed State
COMPLETED284 Analytics
PHASE1COMPLETED
A Study to Assess the Bioequivalence of Fixed Dose Combination of Dapagliflozin/Metformin XR Relative to Co-administration of the Individual Components in Healthy Chinese Subjects.
Healthy VolunteerUnlock trial analytics
PHASE1COMPLETED
The Purpose of the Study is to Compare Two Fixed Dose Combination Tablets of Dapagliflozin/Metformin XR in Healthy Subjects Under Fasting and Fed Conditions
Healthy Subjects in Fasted and Fed StateUnlock trial analytics

Study Endpoints

Primary Endpoints

Area under the plasma concentration-time curve from zero to the last quantifiable concentration(AUClast) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.

For period 1 and 2, PK samples will be collected pre-dose and 0.5,1,2,3,4,6,8,10,12,24(Day2),36,48(Day3), and 72(Day4) hours post dose.

Area under the plasma concentration-time curve from zero to infinity (AUCinf) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.

For period 1 and 2, PK samples will be collected pre-dose and 0.5,1,2,3,4,6,8,10,12,24(Day2),36,48(Day3), and 72(Day4) hours post dose.

Maximum observed plasma concentration (Cmax) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.

For period 1 and 2, PK samples will be collected pre-dose and 0.5,1,2,3,4,6,8,10,12,24(Day2),36,48(Day3), and 72(Day4) hours post dose.

Part 1 - Area under the plasma concentration versus time curve (AUC) for each analyte and each state
Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 5/500 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 5/500 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 2 - Area under the plasma concentration versus time curve (AUC) for each analyte and each state
Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 10/1000 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 10/1000 mg manufactured at Humacao plant in metformin and dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 1 - Peak Plasma Concentration (Cmax) for each analyte and each state
Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 5/500 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 5/500 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 2 - Peak Plasma Concentration (Cmax) for each analyte and each state
Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 10/1000 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 10/1000 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Secondary Endpoints

Time to maximum observed plasma concentration (tmax) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.
Terminal elimination rate constant (λz) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.
Half-life associated with terminal slope of a semi-logarithmic concentration-time curve(t½λz) of dapagliflozin and metformin.
From Day 1 to Day 4, in Treatment period 1 and 2, respectively. An average of 11 to 18 days.
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeOTHER

Treatment Arms

ArmTypeDescription
Dapagliflozin 5mg + Metformin 500mg XREXPERIMENTALco-administration of a single oral dose of a 5mg dapagliflozin (Forxiga® 5mg) tablet and a 500mg metformin XR (Glucophage XR®) tablet
Dapagliflozin/metformin XR FDC 5/500 mgEXPERIMENTALsingle FDC tablet consisting of 5mg dapagliflozin and 500mg metformin XR subject
Dapagliflozin 10mg + Metformin 1000mg XREXPERIMENTALco-administration of a single oral dose of a 10mg dapagliflozin (Forxiga® 10mg) tablet and two 500mg metformin XR (Glucophage XR®) tablets
Dapagliflozin/metformin XR FDC 10/1000 mgEXPERIMENTALingle FDC tablet consisting of 10mg dapagliflozin and 1000mg metformin XR
Treatment AEXPERIMENTALDapagliflozin/metformin XR 5/500 Mount Vernon Test Product Fed
Treatment BACTIVE_COMPARATORDapagliflozin/metformin XR 5/500 Humacao Reference Product Fed
Treatment CEXPERIMENTALDapagliflozin/metformin XR 5/500 Mount Vernon Test Product Fasted
Treatment DACTIVE_COMPARATORDapagliflozin/metformin XR 5/500 Humacao Reference Product Fasted
Treatment EEXPERIMENTALDapagliflozin/metformin XR 10/1000 Mount Vernon Test Product Fed
Treatment FACTIVE_COMPARATORDapagliflozin/metformin XR 10/1000 Humacao Reference Product Fed
Treatment GEXPERIMENTALDapagliflozin/metformin XR 10/1000 Mount Vernon Test Product Fasted
Treatment HACTIVE_COMPARATORDapagliflozin/metformin XR 10/1000 Humacao Reference Product Fasted

Interventions

NameTypeDescription
Dapagliflozin/metformin XR FDC 5/500 mgDRUGIn cohort 1, subjects will be randomized to receive co-administration of a single oral dose of a 5mg dapagliflozin tablet and a 500mg metformin XR tablets (Treatment A) followed by 7 to 14 days washout and then receive single FDC tablet consisting of 5mg dapagliflozin and 500mg metformin XR (Treatment B) on Day 1 in one treatment sequence. Or subjects will be randomized to be administered the Treatment B followed by 7 to 14 days washout and then received Treatment A on Day1 in the other treatment sequence.
Dapagliflozin/metformin XR FDC 10/1000 mgDRUGIn cohort 2, subjects will be randomized to receive co-administration of a single oral dose of a 10mg dapagliflozin tablet and two 500mg metformin XR tablets (Treatment C) followed by 7 to 14 days washout and then receive single FDC tablet consisting of 10mg dapagliflozin and 1000mg metformin XR (Treatment D) on Day 1 in one treatment sequence. Or subjects will be randomized to be administered the Treatment D followed by 7 to 14 days washout and then received Treatment C on Day1 in the other treatment sequence.
Dapagliflozin 5 mg + Metformin 500 mg XRDRUGIn cohort 1, subjects will be randomized to receive co-administration of a single oral dose of a 5mg dapagliflozin tablet and a 500mg metformin XR tablets (Treatment A) followed by 7 to 14 days washout and then receive single FDC tablet consisting of 5mg dapagliflozin and 500mg metformin XR (Treatment B) on Day 1 in one treatment sequence. Or subjects will be randomized to be administered the Treatment B followed by 7 to 14 days washout and then received Treatment A on Day1 in the other treatment sequence.
Dapagliflozin 10 mg + Metformin 1000 mg XRDRUGIn cohort 2, subjects will be randomized to receive co-administration of a single oral dose of a 10mg dapagliflozin tablet and two 500mg metformin XR tablets (Treatment C) followed by 7 to 14 days washout and then receive single FDC tablet consisting of 10mg dapagliflozin and 1000mg metformin XR (Treatment D) on Day 1 in one treatment sequence. Or subjects will be randomized to be administered the Treatment D followed by 7 to 14 days washout and then received Treatment C on Day1 in the other treatment sequence.
Dapagliflozin/metformin XR 5/500mgDRUGTablets for oral administration, once daily, once per treatment period
Dapagliflozin/metformin XR 5/500 mgDRUGTablets for oral administration, once daily, once per treatment period
Dapagliflozin/metformin XR 10/1000mgDRUGTablets for oral administration, once daily, once per treatment period
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: 1. Provision of informed consent prior to any study specific procedures. 2. Healthy Chinese subjects as determined by no clinically significant deviation from normal in medical history, vital signs, physical examination, 12-lead ECG, and clinical laboratory evaluations. 3. Male ...

Countries:ChinaBrazil
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Frequently asked questions about Dapagliflozin/metformin 5

What is Dapagliflozin used for?

Dapagliflozin is an investigational small molecule being developed for cardiovascular and metabolic conditions, including diabetes mellitus, chronic kidney disease, heart failure with preserved ejection fraction, and type 1 diabetes mellitus. It is also studied in healthy volunteers for bioequivalence assessments. The drug is in Phase 3 clinical development.

Who makes Dapagliflozin?

Dapagliflozin is developed by AstraZeneca PLC, a biopharmaceutical company listed on the stock exchange under the ticker AZN. The company is conducting clinical trials to evaluate the drug's safety and efficacy across multiple indications.

What phase is Dapagliflozin in?

Dapagliflozin is in Phase 3 clinical development. It has completed 20 clinical trials with a total enrollment of 17,379 participants. The trials are randomized, double-blind, and placebo-controlled, indicating a rigorous evaluation process for the drug's efficacy and safety.

What clinical trials is Dapagliflozin in?

Dapagliflozin has completed several clinical trials, including NCT01294436 in Japanese subjects with type 2 diabetes, NCT02279407 for liver fat in diabetic patients, NCT03877237 for heart failure with reduced ejection fraction, and NCT04856007 for bioequivalence in healthy Chinese subjects. All trials are completed.

Is Dapagliflozin the same as Farxiga?

Dapagliflozin is also known by the brand name Farxiga, which is a medication used to treat type 2 diabetes. In clinical trials, it is being studied for additional indications such as heart failure and chronic kidney disease. The drug is developed by AstraZeneca.