Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of DWP16001 After Oral Administration in Healthy Male Volunteers

Daewoong Pharmaceutical Co. LTD.123 enrolled

Overview

This is a dose block-randomized, double-blind, placebo- and active-controlled, single and multiple dosing, dose-escalation clinical phase 1 trial to investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of DWP16001 after oral administration in healthy male volunteers.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

DOUBLE

Enrollment

123

Conditions

Healthy

Interventions

DWP16001DRUG

DWP16001 tablets

PlaceboDRUG

DWP16001 placebo-matching tablets, Active control placebo-matching tablets

DapagliflozinDRUG

Forxiga®

Eligibility

Sex: MALEMin age: 19 YearsMax age: 50 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: 1. Healthy male adults aged 19 to 50 at the time of screening test. 2. Body weight between 50.0 kg and 90.0 kg and Body Mass Index (BMI) between 18.0 and 27.0. 3. Written consent on voluntary decision of participation prior to the screening procedure after being fully informed of and completely understanding this study. 4. Eligible to participate in the study by discretion of the investigator following medical examination by interview, physical examination, and clinical examination. Exclusion Criteria: 1. Presence of a clinically significant hepatic, renal, nervous, respiratory, endocrine, blood•tumor, cardiovascular, urogenital, psychiatric disorder or prior history. 2. Presence or prior history of a gastrointestinal disorder (e.g., gastrointestinal ulcers, gastritis, stomach cramps, gastroesophageal reflux disease, Crohn's disease, etc.), or prior history of surgery (except for simple appendectomy or hernia surgery) that may affect safety and PK/PD assessment. 3. Hypersensitivity to a drug containing an ingredient of the investigational product (DWP16001), Dapagliflozin or similar ingredient or other drugs (e.g., aspirin, antibiotics, etc.) or medical history of clinically significant hypersensitivity. 4. Following laboratory abnormalities identified during the screening test: * AST (SGOT), ALT (SGPT) \>1.5 upper limit of normal range * Creatinine clearance calculated by the MDRD equation \< 90 mL/min * Repeatedly confirmed QTc interval \> 450 ms * Fasting serum glucose \> 110mg/dL or \< 70mg/dL * Serum HbA1c \> 6.5 mg/dL

Locations (1)

Seoul National University Hospital

Seoul, South Korea

Outcomes

Primary Outcomes

Number and percentage of Participants With Adverse Events (AE)

All AE standardized using MedDRA was assessed by investigator using the protocol defined grading system. Intensity was categorized as mild, moderate and severe

Time frame: Day -2(Randomization) to Day 8~12(Post-study visit) in single ascending dose or Day-3d to Day 22~ (Post-study visit)

Number and percentage of Participants With Adverse Drug Reactions (ADR)

An adverse drug reaction (ADR) is an injury caused by taking an investigational product

Time frame: Day -2(Randomization) to Day 8~12(Post-study visit) in single ascending dose or Day-3d to Day 22~ (Post-study visit)

Number of Participants With Clinically Significant Vital Sign findings

Blood pressure, pulse and body temperature were tested. The Average, Median, Standard Deviation, Min, Max values will be calculated to assess the safety/tolerability

Time frame: Day -2(Randomization) to Day 8~12(Post-study visit) in single ascending dose or Day-3d to Day 22~ (Post-study visit)

Number of Participants With Clinically Significant Electrocardiogram(12-lead ECG) findings

Ventricular rate, RR interval, PR interval, QRS duration, QTcB and QTcF were recorded. The results of 12-lead ECG will be categorized Normal/Abnormal NCS(No clinically significant)/Abnormal CS(clinically significant).

Time frame: Day -2(Randomization) to Day 8~12(Post-study visit) in single ascending dose or Day-3d to Day 22~ (Post-study visit)

Number of Participants With Clinically Significant Laboratory results

Hematology, Blood chemistry, Coagulation and Urinalysis were tested. The Average, Median, Standard Deviation, Min, Max values will be calculated to assess the safety/tolerability.

Time frame: Day -2(Randomization) to Day 8~12(Post-study visit) in single ascending dose or Day-3d to Day 22~ (Post-study visit)

Data from ClinicalTrials.gov

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Cmax: Maximum concentration of DWP16001

in single ascending dose cohort

Time frame: 0 hour (pre-dose), 0.25 hour, 0.5 hour, 0.75 hour, 1 hour, 1.5 hour, 2 hour, 3 hour, 4 hour, 6 hour, 8 hour, 10 hour, 12hour, 24 hour, 36 hour, 48 hour, 72 hour

Cmax,ss: Maximum concentration of DWP16001 at steady state

in multiple ascending dose cohort

Time frame: Day1 pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour, Day 4, 7, 10, 13 0 hour (pre dose), Day 15 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour

Cmin,ss: Minimum concentration of DWP16001 at steady state

in multiple ascending dose cohort

Time of maximum concentration

in single ascending dose cohort

Time frame: 0 hour (pre-dose), 0.25 hour, 0.5 hour, 0.75 hour, 1 hour, 1.5 hour, 2 hour, 3 hour, 4 hour, 6 hour, 8 hour, 10 hour, 12hour, 24 hour, 36 hour, 48 hour, 72 hour

Tmax,ss: Time of maximum concentration at steady state

in multiple ascending dose cohort

AUClast: Area under the plasma concentration-time curve from time 0 to 72hours

in single ascending dose cohort

Time frame: 0 hour (pre-dose), 0.25 hour, 0.5 hour, 0.75 hour, 1 hour, 1.5 hour, 2 hour, 3 hour, 4 hour, 6 hour, 8 hour, 10 hour, 12hour, 24 hour, 36 hour, 48 hour, 72 hour

AUCinf: Area under the plasma concentration-time curve from time 0 to infinity

in single ascending dose cohort

Time frame: 0 hour (pre-dose), 0.25 hour, 0.5 hour, 0.75 hour, 1 hour, 1.5 hour, 2 hour, 3 hour, 4 hour, 6 hour, 8 hour, 10 hour, 12hour, 24 hour, 36 hour, 48 hour, 72 hour

AUCtau: Area under the plasma concentration-time curve from time 0 to tau(dosing interval)

in multiple ascending dose cohort

T1/2: Elimination half-life

in single ascending dose cohort

Time frame: 0 hour (pre-dose), 0.25 hour, 0.5 hour, 0.75 hour, 1 hour, 1.5 hour, 2 hour, 3 hour, 4 hour, 6 hour, 8 hour, 10 hour, 12hour, 24 hour, 36 hour, 48 hour, 72 hour

T1/2: Elimination half-life

in multiple ascending dose cohort

concentration of serum glucose

in single ascending dose cohort

Time frame: 0(pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour

concentration of serum glucose

in multiple ascending dose cohort

Time frame: Day 1 pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour, Day 4, 7, 10, 13 pre dose, Day 15 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour

concentration of insulin

in multiple ascending dose cohort

Time frame: Day -1 pre dose, 0.5, 1, 1.5, 2, 3, 4 hour, Day 15 pre dose, 0.5, 1, 1.5, 2, 3, 4 hour

Changes from baseline for Body weight in kilograms

in multiple ascending dose cohort

Time frame: Day -1 0 hour, Day 15 0 hour

Changes from baseline for HbA1C in percent

in multiple ascending dose cohort

Time frame: Day -1 0 hour, Day 15 0 hour

concentration of Urine glucose excretion

in single ascending dose cohort

Time frame: 0(pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour

concentration of Urine glucose excretion

in multiple ascending dose cohort

Time frame: Day 1 pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour, Day 4, 7, 10, 13 pre dose, Day 15 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72 hour

Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of DWP16001 After Oral Administration in Healthy Male Volunteers

Overview

Conditions

Interventions

Eligibility

Locations (1)

Outcomes

Primary Outcomes

Secondary Outcomes