Trial Outcomes & Findings for Praziquantel Bioequivalence Study (NCT NCT03437447)
NCT ID: NCT03437447
Last Updated: 2019-09-18
Results Overview
Area under the plasma concentration-time curve from 0 to the time of the last quantifiable concentration.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
60 participants
Primary outcome timeframe
Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dose
Results posted on
2019-09-18
Participant Flow
Participant milestones
| Measure |
First Cisticid, Then Biltricide, Then Biltricide
Participants received single oral dose of 1200 milligrams (mg) (two 600 mg tablets) Cisticid (Test) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Biltricide (Reference) on Day 8 in Treatment Period 2 and on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Cisticid, Then Biltricide
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 8 in Treatment Period 2 and then single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Biltricide, Then Cisticid
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 and on Day 8 in Treatment Period 2 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
|---|---|---|---|
|
Treatment Period 1
STARTED
|
20
|
20
|
20
|
|
Treatment Period 1
COMPLETED
|
20
|
20
|
19
|
|
Treatment Period 1
NOT COMPLETED
|
0
|
0
|
1
|
|
Treatment Period 2
STARTED
|
20
|
20
|
19
|
|
Treatment Period 2
COMPLETED
|
20
|
20
|
19
|
|
Treatment Period 2
NOT COMPLETED
|
0
|
0
|
0
|
|
Treatment Period 3
STARTED
|
20
|
20
|
19
|
|
Treatment Period 3
COMPLETED
|
20
|
20
|
19
|
|
Treatment Period 3
NOT COMPLETED
|
0
|
0
|
0
|
Reasons for withdrawal
| Measure |
First Cisticid, Then Biltricide, Then Biltricide
Participants received single oral dose of 1200 milligrams (mg) (two 600 mg tablets) Cisticid (Test) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Biltricide (Reference) on Day 8 in Treatment Period 2 and on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Cisticid, Then Biltricide
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 8 in Treatment Period 2 and then single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Biltricide, Then Cisticid
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 and on Day 8 in Treatment Period 2 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
|---|---|---|---|
|
Treatment Period 1
Withdrawal by Subject
|
0
|
0
|
1
|
Baseline Characteristics
All participants who were randomized into the study.
Baseline characteristics by cohort
| Measure |
First Cisticid, Then Biltricide, Then Biltricide
n=20 Participants
Participants received single oral dose of 1200 milligrams (mg) (two 600 mg tablets) Cisticid (Test) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Biltricide (Reference) on Day 8 in Treatment Period 2 and on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Cisticid, Then Biltricide
n=20 Participants
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 8 in Treatment Period 2 and then single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
First Biltricide, Then Biltricide, Then Cisticid
n=20 Participants
Participants received single oral dose of 1200 mg (two 600 mg tablets) Biltricide (Reference) on Day 1 in Treatment Period 1 and on Day 8 in Treatment Period 2 followed by single oral dose of 1200 mg (two 600 mg tablets) of Cisticid (Test) on Day 15 in Treatment Period 3. A washout period will be maintained between 3 treatment periods.
|
Total
n=60 Participants
Total of all reporting groups
|
|---|---|---|---|---|
|
Age, Continuous
|
27.80 Years
STANDARD_DEVIATION 7.83 • n=93 Participants • All participants who were randomized into the study.
|
28.65 Years
STANDARD_DEVIATION 7.46 • n=4 Participants • All participants who were randomized into the study.
|
27.20 Years
STANDARD_DEVIATION 5.31 • n=27 Participants • All participants who were randomized into the study.
|
27.88 Years
STANDARD_DEVIATION 6.86 • n=483 Participants • All participants who were randomized into the study.
|
|
Sex: Female, Male
Female
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Sex: Female, Male
Male
|
20 Participants
n=93 Participants • All participants who were randomized into the study.
|
20 Participants
n=4 Participants • All participants who were randomized into the study.
|
20 Participants
n=27 Participants • All participants who were randomized into the study.
|
60 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
20 Participants
n=93 Participants • All participants who were randomized into the study.
|
20 Participants
n=4 Participants • All participants who were randomized into the study.
|
20 Participants
n=27 Participants • All participants who were randomized into the study.
|
60 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
Black or African American
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
White
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
More than one race
|
20 Participants
n=93 Participants • All participants who were randomized into the study.
|
20 Participants
n=4 Participants • All participants who were randomized into the study.
|
20 Participants
n=27 Participants • All participants who were randomized into the study.
|
60 Participants
n=483 Participants • All participants who were randomized into the study.
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants • All participants who were randomized into the study.
|
0 Participants
n=4 Participants • All participants who were randomized into the study.
|
0 Participants
n=27 Participants • All participants who were randomized into the study.
|
0 Participants
n=483 Participants • All participants who were randomized into the study.
|
PRIMARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: Pharmacokinetic (PK) analysis set included all participants who received all administrations of treatment and have PK parameters for AUC0-t and maximum observed plasma concentration (Cmax) in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
Area under the plasma concentration-time curve from 0 to the time of the last quantifiable concentration.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of L-Praziquantel (L-PZQ)
|
441.53 Hour*nanogram per milliliter (h*ng/ml)
Standard Deviation 345.70
|
547.41 Hour*nanogram per milliliter (h*ng/ml)
Standard Deviation 384.82
|
460.25 Hour*nanogram per milliliter (h*ng/ml)
Standard Deviation 343.37
|
PRIMARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participant who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
The maximum observed plasma concentration of L-Praziquantel (L-PZQ).
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Maximum Observed Plasma Concentration (Cmax) of L-Praziquantel (L-PZQ)
|
310.87 ng/mL
Standard Deviation 249.02
|
426.42 ng/mL
Standard Deviation 324.01
|
363.20 ng/mL
Standard Deviation 333.50
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participant who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
Time of the maximum drug concentration.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Time to Reach Maximum Plasma Concentration (Tmax) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
2.5 hours
Interval 1.5 to 5.5
|
2 hours
Interval 1.0 to 3.5
|
2.5 hours
Interval 1.0 to 4.5
|
|
Time to Reach Maximum Plasma Concentration (Tmax) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
2.5 hours
Interval 1.5 to 5.5
|
2 hours
Interval 1.0 to 3.5
|
2.5 hours
Interval 1.0 to 4.5
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participant who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
Time prior to the first measurable (non-zero) concentration; calculated as last time point at which the concentration is less than (\<) Lower Limit of Quantification (LLOQ) before the occurrence of the first quantifiable concentration.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
1 hours
Interval 0.25 to 3.0
|
1 hours
Interval 0.25 to 2.5
|
1 hours
Interval 0.25 to 3.5
|
|
Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
0.75 hours
Interval 0.0 to 2.0
|
0.75 hours
Interval 0.25 to 2.0
|
0.75 hours
Interval 0.0 to 2.5
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set: All participants who received all administrations of treatment \& have PK parameters for AUC0-t \& Cmax in all periods without any relevant protocol violations \& factors likely to affect comparability of PK results. Here "Number analyzed" signifies those participants who were evaluable for this outcome measure for specified category.
AUC0-inf is defined as the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf).
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
468.52 h*ng/ml
Standard Deviation 352.29
|
584.23 h*ng/ml
Standard Deviation 410.05
|
497.89 h*ng/ml
Standard Deviation 348.81
|
|
Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
2130.19 h*ng/ml
Standard Deviation 1417.81
|
2509.42 h*ng/ml
Standard Deviation 1624.33
|
2189.25 h*ng/ml
Standard Deviation 1403.14
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set: All participants who received all administrations of treatment \& have PK parameters for AUC0-t \& Cmax in all periods without any relevant protocol violations \& factors likely to affect comparability of PK results. Here "Number analyzed" signifies those participants who were evaluable for this outcome measure for specified category.
AUCextra was reported in terms of percentage of AUC0-inf.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Extrapolated Area Under the Plasma Concentration Curve From Time Tlast to Infinity (AUCextra) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
5.36 Percentage of AUC0-inf
Standard Deviation 3.73
|
5.49 Percentage of AUC0-inf
Standard Deviation 6.47
|
5.74 Percentage of AUC0-inf
Standard Deviation 4.02
|
|
Extrapolated Area Under the Plasma Concentration Curve From Time Tlast to Infinity (AUCextra) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
2.60 Percentage of AUC0-inf
Standard Deviation 1.73
|
2.84 Percentage of AUC0-inf
Standard Deviation 2.56
|
2.57 Percentage of AUC0-inf
Standard Deviation 1.56
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set: All participants who received all administrations of treatment \& have PK parameters for AUC0-t \& Cmax in all periods without any relevant protocol violations \& factors likely to affect comparability of PK results. Here "Number analyzed" signifies those participants who were evaluable for this outcome measure for specified category.
Elimination Half Life (t1/2) was defined as the time required for the concentration or amount of drug in the body to be reduced by one-half.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Terminal Elimination Half-Life (t1/2) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
1.87 hours
Standard Deviation 1.12
|
2.59 hours
Standard Deviation 3.01
|
2.32 hours
Standard Deviation 1.65
|
|
Terminal Elimination Half-Life (t1/2) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
2.19 hours
Standard Deviation 0.91
|
2.54 hours
Standard Deviation 1.73
|
2.18 hours
Standard Deviation 0.90
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participants who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
Lambda Z was determined from the terminal slope of the log-transformed plasma concentration curve using linear regression method.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Terminal Elimination Rate Constant (Lambda Z) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
0.452927 Per hour
Interval 0.103378 to 1.120808
|
0.383267 Per hour
Interval 0.032567 to 0.721124
|
0.370854 Per hour
Interval 0.073375 to 0.944209
|
|
Terminal Elimination Rate Constant (Lambda Z) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
0.365639 Per hour
Interval 0.135661 to 0.646499
|
0.331359 Per hour
Interval 0.060282 to 0.635357
|
0.370806 Per hour
Interval 0.125134 to 0.638226
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set: All participants who received all administrations of treatment \& have PK parameters for AUC0-t \& Cmax in all periods without any relevant protocol violations \& factors likely to affect comparability of PK results. Here "Number analyzed" signifies those participants who were evaluable for this outcome measure for specified category.
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Apparent Clearance (CL/f) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
749261.50 Milliliter per hour
Standard Deviation 744206.88
|
585260.42 Milliliter per hour
Standard Deviation 541013.95
|
673193.51 Milliliter per hour
Standard Deviation 531848.19
|
|
Apparent Clearance (CL/f) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
147268.6 Milliliter per hour
Standard Deviation 122977.13
|
128110.14 Milliliter per hour
Standard Deviation 122864.03
|
155851.99 Milliliter per hour
Standard Deviation 145104.37
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set: All participants who received all administrations of treatment \& have PK parameters for AUC0-t \& Cmax in all periods without any relevant protocol violations \& factors likely to affect comparability of PK results. Here "Number analyzed" signifies those participants who were evaluable for this outcome measure for specified category.
Volume of distribution was defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Vd/f after oral dose was influenced by the fraction absorbed.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Apparent Volume of Distribution During Terminal Phase (Vd/f) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
Rac-PZQ
|
430368.23 Milliliter
Standard Deviation 328721.73
|
385223.26 Milliliter
Standard Deviation 279076.69
|
431494.33 Milliliter
Standard Deviation 350782.53
|
|
Apparent Volume of Distribution During Terminal Phase (Vd/f) of L-Praziquantel (L-PZQ) and Racemate PZQ (Rac-PZQ)
L-PZQ
|
1540237.10 Milliliter
Standard Deviation 1069504.21
|
1660474.33 Milliliter
Standard Deviation 1619772.26
|
1800582.47 Milliliter
Standard Deviation 1385707.17
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participant who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
Area under the drug plasma concentration-time curve from time zero to the time last measurable concentration.
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Racemate PZQ (Rac-PZQ)
|
2071.35 h*ng/ml
Standard Deviation 1370.58
|
2421.73 h*ng/ml
Standard Deviation 1518.94
|
2131.01 h*ng/ml
Standard Deviation 1353.64
|
SECONDARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 8.0, 9.0, 10.0 and 12.0 hours post-dosePopulation: PK analysis set included all participant who received all administrations of treatment and have PK parameters for AUC0-t and Cmax in all periods and without any relevant protocol violations and factors likely to affect the comparability of PK results.
The maximum observed plasma concentration of rac-Praziquantel (rac-PZQ).
Outcome measures
| Measure |
Cisticid
n=59 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=59 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Maximum Observed Plasma Concentration (Cmax) of Racemate PZQ (Rac-PZQ)
|
1209.15 ng/mL
Standard Deviation 803.20
|
1530.23 ng/mL
Standard Deviation 944.12
|
1356.18 ng/mL
Standard Deviation 1011.46
|
SECONDARY outcome
Timeframe: Baseline up to Day 29Population: Safety Analysis Set included all participants who received at least one dose of study treatment.
An adverse event (AE) was defined as any untoward medical occurrence in a participant which does not necessarily have a causal relationship with the treatment. An AE was any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, whether or not considered related to the medicinal product. A serious adverse event (SAE) was an AE that resulted in any of the following outcomes: death; life threatening; persistent/significant disability/incapacity; initial or prolonged inpatient hospitalization; congenital anomaly/birth defect or was otherwise considered medically important. The term TEAE is defined as AEs starting or worsening after the first intake of the study drug. TEAEs included both Serious TEAEs and non-serious TEAEs.
Outcome measures
| Measure |
Cisticid
n=60 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious TEAEs
Participants with TEAEs
|
2 Participants
|
5 Participants
|
6 Participants
|
|
Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious TEAEs
Participants with Serious TEAEs
|
0 Participants
|
0 Participants
|
0 Participants
|
SECONDARY outcome
Timeframe: Baseline up to Day 29Population: Safety Analysis Set included all participants who received at least one dose of study treatment.
Number of participants with clinically significant abnormalities in laboratory parameters were reported. Laboratory investigation included hematology, biochemistry, urinalysis and coagulation.
Outcome measures
| Measure |
Cisticid
n=60 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Number of Participants With Clinically Significant Abnormalities in Laboratory Parameters
|
0 Participants
|
0 Participants
|
0 Participants
|
SECONDARY outcome
Timeframe: Baseline up to Day 29Population: Safety Analysis Set included all participants who received at least one dose of study treatment.
Number of participants with clinically significant abnormalities in vital signs were reported. Vital signs included body temperature, systolic / diastolic blood pressure, and pulse rate.
Outcome measures
| Measure |
Cisticid
n=60 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Number of Participants With Clinically Significant Abnormalities in Vital Signs
|
0 Participants
|
0 Participants
|
0 Participants
|
SECONDARY outcome
Timeframe: Baseline up to Day 29Population: Safety Analysis Set included all participants who received at least one dose of study treatment.
Number of participants with clinically significant abnormalities in 12-lead electrocardiogram (ECG) were reported. The 12-lead ECGs were recorded after the participants have rested for at least 5 minutes in supine position.
Outcome measures
| Measure |
Cisticid
n=60 Participants
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=60 Participants
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Number of Participants With Clinically Significant Abnormalities in 12-lead Electrocardiogram (ECG) Findings
|
0 Participants
|
0 Participants
|
0 Participants
|
Adverse Events
Cisticid
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Biltricide First Administration
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Biltricide Second Administration
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Cisticid
n=60 participants at risk
All participants who received single oral dose of 1200 mg (two 600 mg tablets) Cisticid (Test) on Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
Biltricide First Administration
n=60 participants at risk
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 1 (Treatment Period 1) or Day 8 (Treatment Period 2).
|
Biltricide Second Administration
n=60 participants at risk
All participants who received 600 mg of Biltricide (Reference) tablet at a dose of 1200 mg on either Day 8 (Treatment Period 2) or Day 15 (Treatment Period 3).
|
|---|---|---|---|
|
Injury, poisoning and procedural complications
Joint injury
|
1.7%
1/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
|
Nervous system disorders
Headache
|
1.7%
1/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
3.3%
2/60 • Baseline up to Day 29
|
|
Respiratory, thoracic and mediastinal disorders
Cough
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
|
Investigations
Aspartate Aminotransferase Increased
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
|
Investigations
Alanine Transaminase Increased
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
|
Injury, poisoning and procedural complications
Multiple injuries
|
0.00%
0/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
|
Injury, poisoning and procedural complications
Head injury
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
|
Blood and lymphatic system disorders
Anaemia
|
0.00%
0/60 • Baseline up to Day 29
|
3.3%
2/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
|
Gastrointestinal disorders
Abdominal pain
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
|
Gastrointestinal disorders
Vomiting
|
0.00%
0/60 • Baseline up to Day 29
|
1.7%
1/60 • Baseline up to Day 29
|
0.00%
0/60 • Baseline up to Day 29
|
Additional Information
Communication Center
Merck KGaA, Darmstadt, Germany
Phone: +49-6151-72-5200
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place