A Double-blind, Randomized, Placebo-controlled, Dose-ranging, Single-dose Study of the Safety, Pharmacokinetics, and Pharmacodynamics of DBPR108 in Healthy Male Subjects
Overview
- Phase
- Phase 1
- Intervention
- DBPR108
- Conditions
- Diabetes Mellitus, Type 2
- Sponsor
- National Health Research Institutes, Taiwan
- Enrollment
- 32
- Locations
- 1
- Primary Endpoint
- Number of Participants With Adverse Events as a Measure of Safety and Tolerability
- Status
- Completed
- Last Updated
- 11 years ago
Overview
Brief Summary
The study is being performed to assess the safety, tolerability, and pharmacokinetic (PK) and pharmacodynamic (PD) properties of single oral doses of DBPR108 in healthy male subjects.
Detailed Description
This study represents the first administration of dipeptidyl peptidase 4 (DPP4) inhibitor DBPR108 to humans to evaluate the safety, tolerability, and pharmacokinetic (PK) and pharmacodynamic (PD) properties following single oral doses in healthy subjects. DPP4 is a validated drug target for the treatment of human type 2 diabetes. Objectives of the study will be to characterize the safety and tolerability of single doses of DBPR108; to characterize the single dose PK of DBPR108 in plasma and urine; to characterize the single dose PD of DBPR108 on glucose, glucagon, dipeptidyl peptidase 4 activity, and total and active forms of glucagon-like peptide-1 (GLP-1) in plasma levels and insulin and C-peptide in serum levels.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Male with suitable veins for cannulation or repeated venipuncture, and must be able to swallow the study drug intact;
- •Aged between 20 and 45 years (inclusive) at the screening visit; and
- •Able to provide written informed consent and willing to comply with the study protocol procedures and restrictions.
Exclusion Criteria
- •Has a body weight less than 50 kg and/or body mass index (BMI) less than 18 kg/m2 or greater than 30 kg/m2 at the screening visit;
- •Has a creatinine clearance (Ccr) less than 80 mL/min at screening;
- •Is not in good general health as judged by the Investigator based on routine medical history, vital signs, physical examination, ECG, laboratory tests, and urinalysis at the screening visit or at admission for the residential period;
- •Is not normoglycemic defined as fasting glucose at less than 70 mg/dL (3.9 mmol/L) and greater than 100 mg/dL (5.5 mmol/L);
- •Has a platelet count less than 150,000/µL;
- •Uses any antihyperglycemic agents at screening or at admission for the residential period;
- •Has a history or presence of any disease or condition known to interfere with the absorption, distribution, metabolism, or excretion of drugs at the screening visit or at admission for the residential period;
- •Has a clinically significant psychiatric, renal, hepatic, cardiovascular, gastrointestinal, or neurologic disease at screening or at admission for the residential period;
- •Is a smoker and/or has used nicotine-containing products within the last 6 months prior to the screening for the current study and/or has a history of alcohol abuse;
- •Has donated blood or participated in another clinical study within 8 weeks preceding the day of admission;
Arms & Interventions
DBPR108
Intervention: DBPR108
matching placebo
Intervention: matching placebo
Outcomes
Primary Outcomes
Number of Participants With Adverse Events as a Measure of Safety and Tolerability
Time Frame: Adverse events were collected from Day -1 (baseline) through the end of the study, up to Day 7.
There were 4 mild adverse events observed during the course of study.
Secondary Outcomes
- Change of Dipeptidyl Peptidase 4 (DPP4) Activities Between 48 Hrs Post Dose and 0 hr Predose(predose (0 hr) and 48 hrs post dose)
- Profile of Pharmacokinetics - Area Under the Plasma Concentration-Time Curve (AUC From 0 to Infinity)(predose (0 hr), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36 and 48 hrs post dose)
- Profile of Pharmacokinetics - Observed Maximum Plasma Concentration (Cmax)(predose (0 hr), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36 and 48 hrs post dose)
- Profile of Pharmacokinetics - Time of Maximum Plasma Concentration (Tmax)(predose (0 hr), 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36 and 48 hrs post dose)