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Dapagliflozin/sitagliptin

Phase 1

Healthy Volunteers (Intended Indication: Type 2 Diabetes Mellitus) | Small molecule | Metabolic |AstraZeneca PLC|Last Updated: Jul 5, 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 Enrollment46

FDA Designations

No designations recorded

Clinical trial landscape

Dapagliflozin/sitagliptin · 1 trial · 1 indication

Phase 1 1
NCT05266404Phase 1 Bioequivalence Study of Dapagliflozin/Sitagliptin FDC vs Loose Combination of Single ComponentsHealthy Volunteers (Intended Indication: Type 2 Diabetes Mellitus)
COMPLETED46 Analytics
PHASE1COMPLETED
Phase 1 Bioequivalence Study of Dapagliflozin/Sitagliptin FDC vs Loose Combination of Single Components
Healthy Volunteers (Intended Indication: Type 2 Diabetes Mellitus)Unlock trial analytics

Study Endpoints

Primary Endpoints

Area under plasma concentration-time curve from zero to infinity (AUCinf)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Area under the plasma concentration-curve from zero to the last quantifiable concentration (AUClast)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Maximum observed plasma (peak) drug concentration (Cmax)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Time to reach peak or maximum observed concentration or response following drug administration (tmax)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Half-life associated with terminal slope (λz) of a semi-logarithmic concentration-time curve (t1/2λz)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Mean residence time of the unchanged drug in the systemic circulation from zero to infinity (MRTinf)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Terminal rate constant, estimated by log-linear least squares regression of the terminal part of the concentration-time curve (λz)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Apparent total body clearance of drug from plasma after extravascular administration (CL/F)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Volume of distribution (apparent) following extravascular administration (based on terminal phase) (Vz/F)
Day 1, Day 2, Day 3 and Day 4

To demonstrate the fasted-state bioequivalence between a dapagliflozin/sitagliptin FDC tablet relative to dapagliflozin 10 mg + sitagliptin 100 mg when co administered as individual tablets in healthy subjects.

Secondary Endpoints

Area under plasma concentration-time curve from zero to infinity (AUCinf)
Day 1, Day 2, Day 3 and Day 4
Area under the plasma concentration-curve from zero to the last quantifiable concentration (AUClast)
Day 1, Day 2, Day 3 and Day 4
Maximum observed plasma (peak) drug concentration (Cmax)
Day 1, Day 2, Day 3 and Day 4
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment A (Test Formulation): Dapagliflozin/Sitagliptin FDC tabletEXPERIMENTALSubjects will receive single dose of dapagliflozin/sitagliptin fixed dose combination (FDC) (test formulation).
Treatment B (Reference Formulation): Dapagliflozin+SitagliptinACTIVE_COMPARATORSubjects will receive single dose of dapagliflozin 10 mg tablet + sitagliptin 100 mg tablet co-administered as individual tablets (reference formulation).

Interventions

NameTypeDescription
Dapagliflozin/sitagliptin FDCDRUGSubjects will receive single dose of Dapagliflozin/sitagliptin FDC orally.
SitagliptinDRUGSubjects will receive 100 mg single dose of Sitagliptin orally.
DapagliflozinDRUGSubjects will receive 10 mg single dose of Dapagliflozin orally.
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy male and female subjects aged 18 to 55 years with suitable veins for cannulation or repeated venipuncture. * Females must have a negative serum pregnancy test at Screening and negative urine pregnancy test within 24 hours prior to investigational Medicinal product (IMP...

Countries:Germany
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Frequently asked questions about Dapagliflozin/sitagliptin

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.