Trial Outcomes & Findings for Correlation of Mesalamine Pharmacokinetics With Local Availability (NCT NCT01999400)
NCT ID: NCT01999400
Last Updated: 2017-05-15
Results Overview
The AUC is the area under the concentration-time curve from time 0 to last time point. The data are organized by the different drug formulations of mesalamine, which include Pentasa (0 to 72 hours), Apriso (0 to 72 hours), Lialda (0 to 96 hours), and Delzicol (0 to 24 hours). The AUC is measured in units of nanomoles of mesalamine per liter of plasma (nM) multiplied by time in hours (nM\*h). The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations.
COMPLETED
NA
30 participants
0 hours pre-dose and up to 96 hours post-dose
2017-05-15
Participant Flow
Participant milestones
| Measure |
Arm 1: Pentasa Then Delzicol Then Apriso Then Lialda
1. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
|
Arm 2: Pentasa Then Delzicol Then Lialda Then Apriso
1. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
|
Arm 3: Apriso Then Delzicol Then Pentasa Then Lialda
1. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
|
Arm 4: Apriso Then Delzicol Then Lialda Then Pentasa
1. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
|
Arm 5: Lialda Then Delzicol Then Pentasa Then Apriso
1. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
|
Arm 6: Lialda Then Delzicol Then Apriso Then Pentasa
1. Lialda 1200 mg tablet x 1 with 240 mL water, single dose.
2. Washout period of 10 days.
3. Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose.
4. Washout period of 10 days.
5. Apriso 375 mg capsule x 3 with 240 mL water, single dose.
6. Washout period of 10 days.
7. Pentasa 500 mg capsule x 2 with 240 mL water, single dose.
|
|---|---|---|---|---|---|---|
|
First Intervention (1 Day)
STARTED
|
6
|
6
|
5
|
5
|
4
|
4
|
|
First Intervention (1 Day)
COMPLETED
|
4
|
4
|
3
|
2
|
4
|
3
|
|
First Intervention (1 Day)
NOT COMPLETED
|
2
|
2
|
2
|
3
|
0
|
1
|
|
Washout (10 Days)
STARTED
|
1
|
0
|
1
|
0
|
0
|
0
|
|
Washout (10 Days)
COMPLETED
|
1
|
0
|
1
|
0
|
0
|
0
|
|
Washout (10 Days)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
|
Second Intervention (1 Day)
STARTED
|
5
|
4
|
3
|
2
|
3
|
3
|
|
Second Intervention (1 Day)
COMPLETED
|
5
|
4
|
3
|
2
|
3
|
3
|
|
Second Intervention (1 Day)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
|
Third Intervention (1 Day)
STARTED
|
2
|
0
|
1
|
1
|
1
|
1
|
|
Third Intervention (1 Day)
COMPLETED
|
2
|
0
|
1
|
1
|
1
|
0
|
|
Third Intervention (1 Day)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
1
|
|
Fourth Intervention (1 Day)
STARTED
|
1
|
0
|
1
|
0
|
0
|
0
|
|
Fourth Intervention (1 Day)
COMPLETED
|
1
|
0
|
1
|
0
|
0
|
0
|
|
Fourth Intervention (1 Day)
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Correlation of Mesalamine Pharmacokinetics With Local Availability
Baseline characteristics by cohort
| Measure |
All Study Participants
n=30 Participants
Participants who were randomized to one of the six arms of this study:
Arm 1: Pentasa then Delzicol then Apriso then Lialda Arm 2: Pentasa then Delzicol then Lialda then Apriso Arm 3: Apriso then Delzicol then Pentasa then Lialda Arm 4: Apriso then Delzicol then Lialda then Pentasa Arm 5: Lialda then Delzicol then Pentasa then Apriso Arm 6: Lialda then Delzicol then Apriso then Pentasa
|
|---|---|
|
Age, Continuous
|
32.9 years
STANDARD_DEVIATION 9.7 • n=99 Participants
|
|
Sex: Female, Male
Female
|
9 Participants
n=99 Participants
|
|
Sex: Female, Male
Male
|
21 Participants
n=99 Participants
|
|
Body Mass Index
|
26.9 kg per m squared
STANDARD_DEVIATION 5.6 • n=99 Participants
|
PRIMARY outcome
Timeframe: 0 hours pre-dose and up to 96 hours post-doseThe AUC is the area under the concentration-time curve from time 0 to last time point. The data are organized by the different drug formulations of mesalamine, which include Pentasa (0 to 72 hours), Apriso (0 to 72 hours), Lialda (0 to 96 hours), and Delzicol (0 to 24 hours). The AUC is measured in units of nanomoles of mesalamine per liter of plasma (nM) multiplied by time in hours (nM\*h). The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations.
Outcome measures
| Measure |
Pentasa
n=10 Participants
Pentasa 500 mg capsule x 2 with 240 mL water, single dose
Pentasa 500 mg capsule x 2 with 240 mL water; single dose
|
Apriso
n=7 Participants
Apriso 375 mg capsule x 3 with 240 mL water, single dose
Apriso 375 mg capsule x 3 with 240 mL water; single dose
|
Lialda
n=9 Participants
Lialda 1200 mg tablet x 1 with 240 mL water, single dose
Lialda 1200 mg tablet x 1 with 240 mL water; single dose
|
Delzicol
n=20 Participants
Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose
Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
|
|---|---|---|---|---|
|
The AUC of Mesalamine in Plasma
|
40.8 nM*h
Standard Deviation 29.5
|
57.6 nM*h
Standard Deviation 24.1
|
36.8 nM*h
Standard Deviation 16.0
|
7.9 nM*h
Standard Deviation 3.7
|
PRIMARY outcome
Timeframe: 0 hours pre-dose and up to 96 hours post-doseThe AUC is the area under the concentration-time curve from time 0 to last time point. The data are organized by the different drug formulations of mesalamine, which include Pentasa (0 to 72 hours), Apriso (0 to 72 hours), Lialda (0 to 96 hours), and Delzicol (0 to 24 hours). The AUC is measured in units of nanomoles of N-acetyl-mesalamine per liter of plasma (nM) multiplied by time in hours (nM\*h). The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations.
Outcome measures
| Measure |
Pentasa
n=10 Participants
Pentasa 500 mg capsule x 2 with 240 mL water, single dose
Pentasa 500 mg capsule x 2 with 240 mL water; single dose
|
Apriso
n=7 Participants
Apriso 375 mg capsule x 3 with 240 mL water, single dose
Apriso 375 mg capsule x 3 with 240 mL water; single dose
|
Lialda
n=9 Participants
Lialda 1200 mg tablet x 1 with 240 mL water, single dose
Lialda 1200 mg tablet x 1 with 240 mL water; single dose
|
Delzicol
n=20 Participants
Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose
Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
|
|---|---|---|---|---|
|
The AUC of Metabolite (N-acetyl-mesalamine) in Plasma
|
162 nM*h
Standard Deviation 59.7
|
189 nM*h
Standard Deviation 92.2
|
124 nM*h
Standard Deviation 80.5
|
20.4 nM*h
Standard Deviation 7.7
|
SECONDARY outcome
Timeframe: 0 hours pre-dose and up to 7 hours post-dosePopulation: The number of subjects that were administered Pentasa, Apriso, Lialda were 10, 7, and 9, respectively. However, we were only able to collect gastrointestinal fluid from the distal jejunum for only 3 subjects in each of these arms due to the placement of the gastrointestinal tube.
The AUC is the area under the concentration-time curve from time 0 to 7 hours. The data are organized by the different drug formulations of mesalamine, which include Pentasa, Apriso, and Lialda. The AUC is measured in units of micromoles of mesalamine per liter of plasma (µM) multiplied by time in hours (µM\*h).The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations. The solution formulation (Delzicol) was not administered in this portion of the study. Therefore no results pertaining to the solution formulation are included in this outcome measure.
Outcome measures
| Measure |
Pentasa
n=3 Participants
Pentasa 500 mg capsule x 2 with 240 mL water, single dose
Pentasa 500 mg capsule x 2 with 240 mL water; single dose
|
Apriso
n=3 Participants
Apriso 375 mg capsule x 3 with 240 mL water, single dose
Apriso 375 mg capsule x 3 with 240 mL water; single dose
|
Lialda
n=3 Participants
Lialda 1200 mg tablet x 1 with 240 mL water, single dose
Lialda 1200 mg tablet x 1 with 240 mL water; single dose
|
Delzicol
Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose
Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
|
|---|---|---|---|---|
|
The AUC of Mesalamine in Distal Jejunum
|
8456 uM*h
Standard Deviation 7444
|
4923 uM*h
Standard Deviation 8506
|
2.9 uM*h
Standard Deviation 3.9
|
—
|
SECONDARY outcome
Timeframe: 0 hours pre-dose and up to 7 hours post-dosePopulation: The number of subjects that were administered Pentasa, Apriso, Lialda were 10, 7, and 9, respectively. However, we were only able to collect gastrointestinal fluid from the distal jejunum for only 3 subjects in each of these arms due to the placement of the gastrointestinal tube.
The AUC is the area under the concentration-time curve from time 0 to 7 hours. The data are organized by the different drug formulations of mesalamine, which include Pentasa, Apriso, and Lialda. The AUC is measured in units of micromoles of mesalamine per liter of plasma (µM) multiplied by time in hours (µM\*h).The AUC results are reported over the time-period because this provides a more meaningful comparison of potential differences in the bioequivalence of formulations. The solution formulation (Delzicol) was not administered in this portion of the study. Therefore no results pertaining to the solution formulation are included in this outcome measure.
Outcome measures
| Measure |
Pentasa
n=3 Participants
Pentasa 500 mg capsule x 2 with 240 mL water, single dose
Pentasa 500 mg capsule x 2 with 240 mL water; single dose
|
Apriso
n=3 Participants
Apriso 375 mg capsule x 3 with 240 mL water, single dose
Apriso 375 mg capsule x 3 with 240 mL water; single dose
|
Lialda
n=3 Participants
Lialda 1200 mg tablet x 1 with 240 mL water, single dose
Lialda 1200 mg tablet x 1 with 240 mL water; single dose
|
Delzicol
Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose
Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
|
|---|---|---|---|---|
|
The AUC of Metabolite (N-acetyl-mesalamine) in Distal Jejunum
|
5048 uM*h
Standard Deviation 5553
|
1225 uM*h
Standard Deviation 2024
|
3.4 uM*h
Standard Deviation 3.4
|
—
|
Adverse Events
Pentasa
Apriso
Lialda
Delzicol
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Pentasa
n=14 participants at risk
Pentasa 500 mg capsule x 2 with 240 mL water, single dose
Pentasa 500 mg capsule x 2 with 240 mL water; single dose
|
Apriso
n=13 participants at risk
Apriso 375 mg capsule x 3 with 240 mL water, single dose
Apriso 375 mg capsule x 3 with 240 mL water; single dose
|
Lialda
n=11 participants at risk
Lialda 1200 mg tablet x 1 with 240 mL water, single dose
Lialda 1200 mg tablet x 1 with 240 mL water; single dose
|
Delzicol
n=20 participants at risk
Delzicol 100 mg mesalamine x 1 with 245 mL water, single dose
Delzicol 100 mg mesalamine x 1 with 245 mL water; single dose
|
|---|---|---|---|---|
|
Nervous system disorders
vasovagal syncope
|
0.00%
0/14
|
0.00%
0/13
|
9.1%
1/11
|
0.00%
0/20
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place