Trial Outcomes & Findings for A Phase 1, Bioequivalence Study of SYR-472 25mg and 50mg Tablets (NCT NCT02372097)
NCT ID: NCT02372097
Last Updated: 2023-12-22
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
24 participants
Primary outcome timeframe
Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each period
Results posted on
2023-12-22
Participant Flow
Participants took part in the study at 1 investigative site in Japan from 04 March 2015 to 08 April 2015.
Healthy male participants were enrolled in 1 of the 2 treatment sequences in either Period 1 or 2: Group A: 25 milligram (mg) tablet in Period 1 followed by 50 mg tablet in Period 2, Group B: 50 mg tablet in Period 1 followed by 25 mg tablet in Period 2.
Participant milestones
| Measure |
SYR-472 25 mg + SYR-472 50 mg
SYR-472 25 mg, 2 tablets, orally, on Day 1 of the first intervention period (8 days), followed by at least 13 days washout period, followed by SYR-472 50 mg, tablet, orally on Day 1 of the second intervention period (8 days).
|
SYR-472 50 mg + SYR-472 25 mg
SYR-472 50 mg, 1 tablet, orally, on Day 1 of the first intervention period (8 days), followed by at least 13 days washout period, followed by SYR-472 25 mg, 2 tablets, orally on Day 1 of the second intervention period (8 days).
|
|---|---|---|
|
First Intervention Period (8 Days)
STARTED
|
12
|
12
|
|
First Intervention Period (8 Days)
COMPLETED
|
12
|
12
|
|
First Intervention Period (8 Days)
NOT COMPLETED
|
0
|
0
|
|
Wash Out Period (13 Days)
STARTED
|
12
|
12
|
|
Wash Out Period (13 Days)
COMPLETED
|
12
|
12
|
|
Wash Out Period (13 Days)
NOT COMPLETED
|
0
|
0
|
|
Second Intervention Period (8 Days)
STARTED
|
12
|
12
|
|
Second Intervention Period (8 Days)
COMPLETED
|
12
|
12
|
|
Second Intervention Period (8 Days)
NOT COMPLETED
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Phase 1, Bioequivalence Study of SYR-472 25mg and 50mg Tablets
Baseline characteristics by cohort
| Measure |
SYR-472 25 mg + SYR-472 50 mg
n=12 Participants
SYR-472 25 mg, 2 tablets, orally, on Day 1 of the first intervention period (8 days), followed by at least 13 days washout period, followed by SYR-472 50 mg, tablet, orally on Day 1 of the second intervention period (8 days).
|
SYR-472 50 mg + SYR-472 25 mg
n=12 Participants
SYR-472 50 mg, 1 tablet, orally, on Day 1 of the first intervention period (8 days), followed by at least 13 days washout period, followed by SYR-472 25 mg, 2 tablets, orally on Day 1 of the second intervention period (8 days).
|
Total
n=24 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
23.7 Years
STANDARD_DEVIATION 2.64 • n=5 Participants
|
22.3 Years
STANDARD_DEVIATION 3.17 • n=7 Participants
|
23.0 Years
STANDARD_DEVIATION 2.93 • n=5 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
12 Participants
n=5 Participants
|
12 Participants
n=7 Participants
|
24 Participants
n=5 Participants
|
|
Region of Enrollment
Japan
|
12 participants
n=5 Participants
|
12 participants
n=7 Participants
|
24 participants
n=5 Participants
|
|
Height
|
172.0 centimeter (cm)
STANDARD_DEVIATION 6.93 • n=5 Participants
|
172.8 centimeter (cm)
STANDARD_DEVIATION 7.48 • n=7 Participants
|
172.4 centimeter (cm)
STANDARD_DEVIATION 7.06 • n=5 Participants
|
|
Weight
|
64.51 kilogram (kg)
STANDARD_DEVIATION 9.707 • n=5 Participants
|
62.79 kilogram (kg)
STANDARD_DEVIATION 6.087 • n=7 Participants
|
63.65 kilogram (kg)
STANDARD_DEVIATION 7.972 • n=5 Participants
|
|
Body Mass Index (BMI)
|
21.69 kilogram per square meter (kg/m^2)
STANDARD_DEVIATION 1.866 • n=5 Participants
|
21.05 kilogram per square meter (kg/m^2)
STANDARD_DEVIATION 1.948 • n=7 Participants
|
21.37 kilogram per square meter (kg/m^2)
STANDARD_DEVIATION 1.894 • n=5 Participants
|
|
Smoking Classification
Never Smoked
|
7 participants
n=5 Participants
|
7 participants
n=7 Participants
|
14 participants
n=5 Participants
|
|
Smoking Classification
Current Smoker
|
5 participants
n=5 Participants
|
4 participants
n=7 Participants
|
9 participants
n=5 Participants
|
|
Smoking Classification
Ex-Smoker
|
0 participants
n=5 Participants
|
1 participants
n=7 Participants
|
1 participants
n=5 Participants
|
|
Alcohol Classification
Drinks a Few Days per Week
|
2 participants
n=5 Participants
|
5 participants
n=7 Participants
|
7 participants
n=5 Participants
|
|
Alcohol Classification
Drinks a Few Days per Month
|
7 participants
n=5 Participants
|
4 participants
n=7 Participants
|
11 participants
n=5 Participants
|
|
Alcohol Classification
Never Drunk
|
3 participants
n=5 Participants
|
3 participants
n=7 Participants
|
6 participants
n=5 Participants
|
|
Caffeine Classification
Caffeine Consumer
|
4 participants
n=5 Participants
|
2 participants
n=7 Participants
|
6 participants
n=5 Participants
|
|
Caffeine Classification
Caffeine Non-Consumer
|
8 participants
n=5 Participants
|
10 participants
n=7 Participants
|
18 participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
AUC(0-168): Area Under the Plasma Concentration-Time Curve From Time 0 to 168 Hours Postdose for Unchanged SYR-472 (SYR-472Z)
|
2733 nanogram hour per milliliter(ng*hr/mL)
Standard Deviation 445.48
|
2780 nanogram hour per milliliter(ng*hr/mL)
Standard Deviation 437.95
|
PRIMARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Cmax: Maximum Observed Plasma Concentration for SYR-472Z
|
196.5 nanogram per milliliter(ng/mL)
Standard Deviation 54.034
|
223.6 nanogram per milliliter(ng/mL)
Standard Deviation 67.200
|
SECONDARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
AUC(0-inf): Area Under the Plasma Concentration-Time Curve From Time 0 to Infinity for SYR-472Z
|
2829 ng*hr/mL
Standard Deviation 466.32
|
2889 ng*hr/mL
Standard Deviation 454.46
|
SECONDARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Tmax: Time to Reach the Cmax for SYR-472Z
|
1.5000 hour(hr)
Interval 0.5 to 6.0
|
1.000 hour(hr)
Interval 0.5 to 6.0
|
SECONDARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
MRT: Mean Residence Time From Time Zero to Infinity for SYR-472Z
|
32.52 hr
Standard Deviation 4.7575
|
33.07 hr
Standard Deviation 4.8613
|
SECONDARY outcome
Timeframe: Day 1: pre dose (within 3 hours prior to dosing), and at multiple time points (up to 168 hours) post dose in each periodPopulation: The PK analysis set included all participants who received study drug, satisfied the minimum requirements of the protocol with no significant deviations, and were assessable for PK.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Apparent Terminal Elimination Rate Constant (λz) for SYR-472Z
|
0.01399 per hour(hr-1)
Standard Deviation 0.0036008
|
0.01254 per hour(hr-1)
Standard Deviation 0.0028378
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 up to the day of hospital discharge (Day 29) in Period 2Population: The safety analysis set included all participants who received study drug.
Collection of AEs commenced from the time that the participant was first administered study drug in Period 1 (Day 1). Routine collection of AEs continued until the end (hospital discharge) of Period 2 (Day 29).
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Number of Participants Reporting One or More Treatment-Emergent Adverse Events (TEAEs)
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 up to the day of hospital discharge (Day 29) in Period 2Population: The safety analysis set included all participants who received study drug.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Number of Participants With TEAEs Related to Vital Signs
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 up to the day of hospital discharge (Day 29) in Period 2Population: The safety analysis set included all participants who received study drug.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Number of Participants With TEAEs Related to Body Weight
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 up to the day of hospital discharge (Day 29) in Period 2Population: The safety analysis set included all participants who received study drug.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Number of Participants With TEAEs Categorized Into Investigations System Organ Class (SOC) Related to Laboratory Values
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: Baseline up to 7 days after the last dose of study drug (Day 8) in each periodPopulation: The safety analysis set included all participants who received study drug.
Participants whose results of electrocardiograms were judged as abnormal and clinically significant by investigator after study drug administration were counted in this measure.
Outcome measures
| Measure |
SYR-472 25 mg
n=24 Participants
SYR-472 25 mg, 2 tablets, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
SYR-472 50 mg
n=24 Participants
SYR-472 50 mg, tablet, once orally, on Day 1 of either Period 1 or Period 2. A washout of 13 days was maintained between the two periods.
|
|---|---|---|
|
Number of Participants Who Had Abnormal and Clinically Significant 12-lead Electrocardiograms (ECG) Findings After Study Drug Administration
|
0 participants
|
0 participants
|
Adverse Events
SYR-472 25 mg
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
SYR-472 50 mg
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
Adverse event data not reported
Additional Information
Medical Director
Takeda (Note: This product was divested to Teijin Pharma Limited in 2023)
Phone: +1-877-825-3327
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee No publication related to study results will be made without Sponsor's prior written approval. Any proposed publication or presentation will be submitted to Sponsor for review 60 days in advance of publication. Institution will remove Sponsor confidential information unrelated to study results. Sponsor can delay a proposed publication for an additional 60 days to preserve intellectual property.
- Publication restrictions are in place
Restriction type: OTHER