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CompletedPhase 1Results posted

Bexagliflozin Drug/Drug Interaction Study With Exenatide Injection

A Phase 1, Open-label, Randomized, Two-period, Two-treatment, Crossover Study to Evaluate the Effect of Exenatide on the Pharmacokinetics and Pharmacodynamics of Bexagliflozin in Healthy Subjects

Lead sponsor

Theracos

Asset

Exenatide

Subcutaneous · GLP-1 agonist

Listed sites

1

Recruiting sites

Enrollment

20

actual

Study population

Healthy volunteers

Key I/E criterion

BMI 18-32

Primary endpoints

CmaxTmax (Time of Cmax)T1/2

Footprint

Where this trial recruits

Site locations as reported to ClinicalTrials.gov. Site count is not enrollment count; per-site enrollment is not available from source.

Identifiers

Registered as

NCT IDNCT03167411
Org study IDTHR-1442-C-458

Timeline

Milestones

Study start2017-05-24actual
Study first posted2017-05-30actual
Primary completion2017-06-29actual
Study completion2017-06-29actual
Last update posted2021-05-28actual
Results first posted2021-05-28actual

Assets

Investigational agents

Study populations

Who this study enrolls

Healthy volunteers

Eligibility

Who can enroll

Minimum age18 Years
Maximum age65 Years
SexAll
Healthy volunteersAccepted

Inclusion criteria

1. Male and female subjects who were between the ages of 18 and 65 years, inclusive, in good health based on medical history, physical examination, electrocardiogram and routine laboratory tests.

2. Subjects with body-mass index (BMI) between 18.0 kg/m2 and 32.0 kg/m2, inclusive.

3. Subjects who were non-smokers for at least 3 months prior to screening.

4. Subjects with adequate venous access at multiple sites in both arms.

5. Subjects who were willing and able to be confined to the clinical research facility as required by the protocol.

6. Subjects who had the ability to comprehend and who were willing to provide written informed consent in accordance with institutional and regulatory guidelines.

Exclusion criteria

1. Subjects who were determined by the investigator or sub-investigator to be unsuitable for participation in the study based on medical conditions or factors that would have influenced adherence to study activities.

2. Subjects with a clinically significant history of allergy to drugs or latex.

3. Subjects with a history of hypoglycemia.

4. Subjects with a history of alcohol or drug dependence in the last 12 months.

5. Subjects who donated 400 mL of whole blood within 56 days, 200 mL of whole blood within one month, or donated blood components within 14 days of screening.

6. Subjects who used prescription or over-the-counter (OTC) drugs within 14 days prior to the first dose.

7. Subjects who used vitamin preparations or supplements (including St. John's Wort and ginseng) within 14 days prior to the first dose .

8. Subjects who were not willing to refrain from smoking, alcohol, grapefruit, grapefruit juice or related products, caffeine consumption (including chocolate), and strenuous exercise within 72 h prior to Day 1 and through the end of the PK study.

9. Male subjects who did not agree to refrain from donating sperm and use appropriate birth control methods including condoms with spermicide, female partner's use of diaphragm with spermicide, or stable oral, implanted, or injected contraceptive hormones, or with an intrauterine device, or female partner is surgically sterile (i.e. have undergone partial or full hysterectomy, or bilateral oophorectomy) or postmenopausal (absence of menses greater than 12 months and age >45 years), for a period of 30 days after discharge from the clinic.

10. Female subjects of childbearing potential who were not willing to use an adequate method of contraception including bilateral tubal ligation, intrauterine device, diaphragm with spermicide and male partner's use of male condom with spermicide, and to not become pregnant for the duration of the study. Female subjects who were surgically sterile (partial or full hysterectomy, or bilateral oophorectomy) or postmenopausal (absence of menses greater than 12 months and age >45 years) were eligible if they tested negative on the pregnancy test.

11. Subjects who had been treated with an investigational drug within 30 days or 7 half-lives of the investigational drug, whichever is longer, prior to the first dose of study drug in this trial.

12. Subjects who had previously received exenatide, or any other GLP-1 RAs within three months from the screening or subjects who had had any GLP-1 RA and suffered an adverse reaction due to the medication.

13. Subjects who had previously received bexagliflozin, or any other SGLT2 inhibitors within 3 months from the screening.

14. Subjects whose screening ECG demonstrates any one of the following: heart rate >100 bpm, QRS >120 msec, QTc >470 msec (corrected by Fridericia's formula), PR >220 msec (a subject with PR >220 msec was generally to be excluded but exceptions may have been allowed at the discretion of the investigator), or any clinically significant arrhythmia.

15. Subjects whose sitting blood pressure was above 140/90 mmHg at screening. If the sitting blood pressure at screening was above 140/90 mmHg, one repeat measurement was allowed and the subject may have been randomized if the blood pressure was 140/90 +/-5 mm Hg at the discretion of the Investigator.

16. Subjects who had a positive result of hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibody, urinary drug or urinary cotinine test.

17. Subjects with human immunodeficiency virus (HIV) infection.

18. Subjects who had had a febrile illness within 5 days prior to the first dose of study medication.

19. Subjects vaccinated within 30 days (with the exception of the flu vaccine) prior to the first dose of investigational drug.

20. Subjects with a history of acute or chronic pancreatitis or gall stones.

21. Positive urine glucose at screening.

22. Subjects with estimated glomerular filtration rate (eGFR) <90 mL/min/1.73 m2 or a history of kidney transplant.

23. Subjects with digestion problems, including gastroesophageal reflux disease, irritable bowel syndrome, gastroparesis, and any other disorder deemed by the investigator to be clinically significant.

Endpoints (5)

What's being measured

Protocol endpoints and posted registry outcome measures, grouped into outcome categories. Composite endpoints show their component event types. Standard codes (LOINC, SNOMED CT) are shown where available.

Coverage by outcome category

Safety / tolerability / PK
4
Glycemic / diabetes
1

Glycemic / diabetes

1 endpoint
Secondary/protocol endpoint

Urinary Glucose Excretion (UGE)

Time frame:0-48 hours

descriptive

Posted result

GroupValue (mean), g95% CI
BexagliflozinPre-dose (-12 to 0 hours)0.07
0 - 12 hours38.32
12 - 24 hours26.89
24 - 36 hours21.93
36 - 48 hours9.56
0 - 24 hours65.21
0 - 48 hours96.70
Bexagliflozin With ExenatidePre-dose (-12 to 0 hours)0.05
0 - 12 hours26.38
12 - 24 hours28.95
24 - 36 hours22.16
36 - 48 hours9.21
0 - 24 hours55.65
0 - 48 hours88.11

Safety / tolerability / PK

4 endpoints
Primary/protocol endpoint

Cmax (Maximum Observed Plasma Concentration)

Time frame:Up to 48 hrs

Cmax

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng/mL95% CI
Bexagliflozin95.9
Bexagliflozin With Exenatide121.6
Point Estimate (%)125.2790% CI104.45150.24
Primary/protocol endpoint

Tmax (Time of Maximum Observed Plasma Concentration)

Time frame:Up to 48 hrs

Tmax

descriptive

Posted result

GroupValue (median), hours95% CI
Bexagliflozin2.001 – 5
Bexagliflozin With Exenatide5.002 – 10
Primary/protocol endpoint

T1/2 (Apparent Terminal Elimination Half-life)

Time frame:Up to 48 hrs

Half-life

descriptive

Posted result

GroupValue (geometric_mean), hours95% CI
Bexagliflozin12.1
Bexagliflozin With Exenatide8.8
Primary/protocol endpoint

AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Time frame:Up to 48 hrs

AUC₀–∞

concentration, descriptive

Posted result

GroupValue (geometric_mean), hr*ng/mL95% CI
Bexagliflozin776.0
Bexagliflozin With Exenatide1085.3
Point Estimate (%)137.5690% CI122.28154.75

Provenance

Sources

Trial identity, design, statusClinicalTrials.gov API v2
Snapshot dateJuly 1, 2026
Endpoint classificationDelfa endpoint taxonomy v2 (May 13, 2026)
Results tableClinicalTrials.gov results section

Trial facts come from public ClinicalTrials.gov records. Endpoint categories are Delfa's classification of those records, not a ClinicalTrials.gov field. All figures reflect the July 1, 2026 snapshot.