Trial Outcomes & Findings for A Study to Assess the Pharmacokinetics, Safety and Tolerability of Sitagliptin in Adolescents (0431-081) (NCT NCT00730275)
NCT ID: NCT00730275
Last Updated: 2017-05-12
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
35 participants
Primary outcome timeframe
Pre-study through 10 to 14 days following administration of study drug
Results posted on
2017-05-12
Participant Flow
Participant milestones
| Measure |
Sitagliptin 50 mg
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Overall Study
STARTED
|
9
|
9
|
8
|
9
|
|
Overall Study
COMPLETED
|
9
|
9
|
8
|
8
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
1
|
Reasons for withdrawal
| Measure |
Sitagliptin 50 mg
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Overall Study
Withdrawal by Subject
|
0
|
0
|
0
|
1
|
Baseline Characteristics
A Study to Assess the Pharmacokinetics, Safety and Tolerability of Sitagliptin in Adolescents (0431-081)
Baseline characteristics by cohort
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
n=9 Participants
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
Total
n=35 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Continuous
|
13.9 years
STANDARD_DEVIATION 2.52 • n=5 Participants
|
14.3 years
STANDARD_DEVIATION 1.41 • n=7 Participants
|
14.8 years
STANDARD_DEVIATION 1.75 • n=5 Participants
|
14.1 years
STANDARD_DEVIATION 2.26 • n=4 Participants
|
14.3 years
STANDARD_DEVIATION 1.98 • n=21 Participants
|
|
Sex: Female, Male
Female
|
6 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
5 Participants
n=5 Participants
|
8 Participants
n=4 Participants
|
24 Participants
n=21 Participants
|
|
Sex: Female, Male
Male
|
3 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
3 Participants
n=5 Participants
|
1 Participants
n=4 Participants
|
11 Participants
n=21 Participants
|
PRIMARY outcome
Timeframe: Pre-study through 10 to 14 days following administration of study drugPopulation: All enrolled participants.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
n=9 Participants
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Number of Participants Who Experienced at Least One Adverse Event
|
3 participants
|
1 participants
|
1 participants
|
2 participants
|
PRIMARY outcome
Timeframe: Pre-dose through 72 hours post-dosePopulation: All participants who received a single dose of sitagliptin 50 mg, 100 mg, or 200 mg.
Serum samples were used to determine the AUC from time 0 to infinity for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Area Under the Concentration-time Curve (AUC) From Time 0 to Infinity Following a Single Dose of Sitagliptin
|
3438 nM*hour
Interval 2881.0 to 4103.0
|
5869 nM*hour
Interval 4918.0 to 7003.0
|
12965 nM*hour
Interval 10749.0 to 15638.0
|
—
|
SECONDARY outcome
Timeframe: Pre-dose through 72 hours post-dosePopulation: All participants who received a single dose of sitagliptin 50 mg, 100 mg, or 200 mg.
Serum samples were used to determine the Cmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Maximum Concentration (Cmax) Following a Single Dose of Sitagliptin
|
366 nM
Interval 288.0 to 464.0
|
666 nM
Interval 526.0 to 845.0
|
1876 nM
Interval 1458.0 to 2413.0
|
—
|
SECONDARY outcome
Timeframe: Pre-dose through 72 hours post-dosePopulation: All participants who received a single dose of sitagliptin 50 mg, 100 mg, or 200 mg.
Serum samples were used to determine the Tmax for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Time of Occurence of Maximum Concentration (Tmax) Following a Single Dose of Sitagliptin
|
3.0 hours
Interval 1.5 to 5.0
|
3.0 hours
Interval 2.0 to 4.5
|
2.5 hours
Interval 1.0 to 3.1
|
—
|
SECONDARY outcome
Timeframe: Pre-dose through 72 hours post-dosePopulation: All participants who received a single dose of sitagliptin 50 mg, 100 mg, or 200 mg.
Serum samples were used to determine the apparent t1/2 for sitagliptin. The placebo group is not included in the table below; this outcome measure only evaluated the sitagliptin groups.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Apparent Terminal Half-life (Apparent t1/2) Following a Single Dose of Sitagliptin
|
12.1 hours
Standard Deviation 1.7
|
11.2 hours
Standard Deviation 2.1
|
11.7 hours
Standard Deviation 1.8
|
—
|
SECONDARY outcome
Timeframe: Pre-dose through 24 hours post-dosePopulation: All participants who received a single dose of sitagliptin or placebo.
Plasma DPP-4 activity was analyzed using the 24-hour weighted average inhibition (WAI) and percent inhibition at 24 hours post-dose. WAI was defined as the AUC of inhibition divided by the length of the post-dose time interval. Positive values of WAI represent a decrease in DPP-4 activity.
Outcome measures
| Measure |
Sitagliptin 50 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 Participants
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 Participants
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
n=8 Participants
Participants who received a single oral dose of a matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Plasma Dipeptidyl Peptidase-4 (DPP-4) Activity Following a Single Dose of Sitagliptin or Placebo
24-hour WAI of DPP-4 activity
|
73.98 Percent inhibition
Interval 70.59 to 76.99
|
80.53 Percent inhibition
Interval 77.98 to 82.78
|
87.96 Percent inhibition
Interval 86.29 to 89.43
|
6.76 Percent inhibition
Interval -6.21 to 18.14
|
|
Plasma Dipeptidyl Peptidase-4 (DPP-4) Activity Following a Single Dose of Sitagliptin or Placebo
DDP-4 activity at 24 hours post-dose
|
53.98 Percent inhibition
Interval 46.74 to 60.24
|
62.78 Percent inhibition
Interval 56.92 to 67.84
|
75.76 Percent inhibition
Interval 71.7 to 79.24
|
3.57 Percent inhibition
Interval -12.6 to 17.43
|
Adverse Events
Sitagliptin 50 mg
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Sitagliptin 100 mg
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Sitagliptin 200 mg
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Placebo
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Sitagliptin 50 mg
n=9 participants at risk
Participants who received a single oral dose of sitagliptin 50 mg.
|
Sitagliptin 100 mg
n=9 participants at risk
Participants who received a single oral dose of sitagliptin 100 mg.
|
Sitagliptin 200 mg
n=8 participants at risk
Participants who received a single oral dose of sitagliptin 200 mg.
|
Placebo
n=9 participants at risk
Participants who received a single oral dose of matching placebo to sitagliptin 50 mg, 100 mg, or 200 mg.
|
|---|---|---|---|---|
|
Blood and lymphatic system disorders
Anaemia
|
0.00%
0/9
|
0.00%
0/9
|
0.00%
0/8
|
11.1%
1/9
|
|
Gastrointestinal disorders
Abdominal pain
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Gastrointestinal disorders
Abdominal pain upper
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Gastrointestinal disorders
Diarrhoea
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Gastrointestinal disorders
Vomiting
|
0.00%
0/9
|
0.00%
0/9
|
12.5%
1/8
|
0.00%
0/9
|
|
General disorders
Infusion site pain
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
General disorders
Infusion site swelling
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
General disorders
Pyrexia
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Metabolism and nutrition disorders
Hypoglycaemia
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Nervous system disorders
Headache
|
0.00%
0/9
|
0.00%
0/9
|
0.00%
0/8
|
11.1%
1/9
|
|
Reproductive system and breast disorders
Dysmenorrhoea
|
11.1%
1/9
|
0.00%
0/9
|
0.00%
0/8
|
0.00%
0/9
|
|
Respiratory, thoracic and mediastinal disorders
Nasal congestion
|
0.00%
0/9
|
0.00%
0/9
|
0.00%
0/8
|
11.1%
1/9
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
0.00%
0/9
|
0.00%
0/9
|
0.00%
0/8
|
11.1%
1/9
|
|
Vascular disorders
Phlebitis
|
0.00%
0/9
|
11.1%
1/9
|
0.00%
0/8
|
0.00%
0/9
|
Additional Information
Senior Vice President, Global Clinical Development
Merck Sharpe & Dohme Corp
Phone: 1-800-672-6372
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee The sponsor must have the opportunity to review all proposed abstracts, manuscripts, or presentations regarding this study 60 days prior to submission for publication/presentation. Any information identified by the sponsor as confidential must be deleted prior to submission.
- Publication restrictions are in place
Restriction type: OTHER