Relative Bioavailability Trial of Oral Dispersible Praziquantel Tablets in Healthy Volunteers
A Phase I, Open-label, Randomized, Four-period, Crossover, Single Center Trial to Assess the Relative Bioavailability of a Single Oral Dose of the New 150 mg Oral Dispersible Tablet (ODT) Formulation of Praziquantel (PZQ), MSC1028703A, at Different Dose Levels vs the Current Commercial 500 mg Tablet Formulation of PZQ in Healthy Male Volunteers
1 other identifier
interventional
32
1 country
1
Brief Summary
This is a phase I, open-label, randomized, 4 period, crossover, single-center trial. The purpose of this trial is to assess the relative bio-availability of racemate Oral Dispersible Tablet praziquantel (ODT-PQZ) (MSC1028703A) 150 milligram (mg) versus the current marketed praziquantel (PZQ) (Cysticide® 500 mg) formulation in healthy male volunteers.
Trial Health
Trial Health Score
Automated assessment based on enrollment pace, timeline, and geographic reach
participants targeted
Target at P50-P75 for phase_1 healthy
Started Jan 2015
Shorter than P25 for phase_1 healthy
1 active site
Health score is calculated from publicly available data and should be used for screening purposes only.
Trial Relationships
Click on a node to explore related trials.
Study Timeline
Key milestones and dates
First Submitted
Initial submission to the registry
December 11, 2014
CompletedFirst Posted
Study publicly available on registry
December 25, 2014
CompletedStudy Start
First participant enrolled
January 1, 2015
CompletedPrimary Completion
Last participant's last visit for primary outcome
January 1, 2015
CompletedStudy Completion
Last participant's last visit for all outcomes
March 1, 2015
CompletedResults Posted
Study results publicly available
February 23, 2017
CompletedFebruary 23, 2017
January 1, 2017
Same day
December 11, 2014
January 3, 2017
January 3, 2017
Conditions
Keywords
Outcome Measures
Primary Outcomes (1)
Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Infinity (AUC0-inf) Adjusted for the Actual Administered Dose (AUC0-inf, Adj) of L-Praziquantel (L-PZQ)
AUC0-inf is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. AUC0-inf, adj was defined as the AUC0-inf adjusted for the actual administered dose of L-PZQ.
Pre-dose,0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
Secondary Outcomes (14)
Maximum Observed Concentration in Plasma (Cmax) Adjusted for the Actual Administered Dose (Cmax, Adj) of L-PZQ, D-PZQ and Racemate PZQ
Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
Time to Reach Maximum Plasma Concentration (Tmax) of L-PZQ, D-PZQ, and Racemate PZQ
Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
Apparent Terminal Half-life (t1/2) of L-PZQ, D-PZQ, and Racemate PZQ
Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of L-PZQ, D-PZQ, and Racemate PZQ
Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
AUC From Time Zero to the Last Sampling Time at Which the Concentration is at or Above the Lower Limit of Quantification (AUC0-t) Adjusted for the Actual Administered Dose (AUC0-t, Adj) of L-PZQ, D-PZQ, and Racemate PZQ
Pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 8, 12, 16 and 24 hours post-dose on Day 1 of each treatment
- +9 more secondary outcomes
Study Arms (16)
Sequence A-B-C1-D1
EXPERIMENTALSequence A-B-C1-D2
EXPERIMENTALSequence A-B-C2-D1
EXPERIMENTALSequence A-B-C2-D2
EXPERIMENTALSequence A-B-D1-C1
EXPERIMENTALSequence A-B-D2-C1
EXPERIMENTALSequence A-B-D1-C2
EXPERIMENTALSequence A-B-D2-C2
EXPERIMENTALSequence B-A-C1-D1
EXPERIMENTALSequence B-A-C1-D2
EXPERIMENTALSequence B-A-C2-D1
EXPERIMENTALSequence B-A-C2-D2
EXPERIMENTALSequence B-A-D1-C1
EXPERIMENTALSequence B-A-D2-C1
EXPERIMENTALSequence B-A-D1-C2
EXPERIMENTALSequence B-A-D2-C2
EXPERIMENTALInterventions
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Eligibility Criteria
You may qualify if:
- Healthy males 18-55 years of age (inclusive at screening)
- Male subjects with partners of childbearing potential must have had a vasectomy or use acceptable methods of birth control (that is, condoms) and not donate sperm during, and until 90 days after the last dose of the trial medication
- Provide written informed consent prior to any trial related procedure
- Body weight of greater than or equal to (\>=)55.0 kg to less than (\<) 95.0 kg and a body mass index (BMI) between 18.5 and 29.9 kilogram per square meter (kg/m\^2)
- Able to communicate well with the Investigator, understand the protocol requirements and restrictions, and willing to comply with the requirements of the entire trial
- Non-smoker (= 0 cigarettes, pipes, cigars or other) from at least 3 months prior to start of trial
- Electrocardiogram (ECG) recording (12-lead) without signs of clinically relevant pathology, in particular QTcB \< 450 milliseconds (ms)
- Vital signs (systolic blood pressure, diastolic blood pressure and pulse) in supine position are within the normal range or show no clinically relevant deviation as judged by the Investigator
You may not qualify if:
- Any surgical or medical condition, including findings in the medical history or in the pre-study assessments, or any other significant disease, that in the opinion of the Investigator, constitutes a risk or a contraindication for the participation of the subject in the trial or that could interfere with the trial objectives, conduct or evaluation
- History of gastrointestinal (GI) tract surgery, other GI tract diseases or acute GI tract infections within the last 2 weeks that could influence the GI absorption and/or motility according to the Investigator's opinion
- Any clinically relevant abnormality in the safety laboratory parameters as judged by the Investigator
- Positive results from serology examination for Hepatitis B surface antigen (HBsAg), Hepatitis C Virus (HCV) or Human Immunodeficiency Virus (HIV)
- Have an ascertained or presumptive contraindication or hypersensitivity to the active drug substance and/or formulations' ingredients
- Have any clinically significant history of allergic conditions which the Investigator considers may affect the outcome of the trial
- History or presence of drug abuse or alcohol abuse (as defined by the assessment of the investigator) at screening and on each admission
- Blood donation or loss of more than 400 mL of blood within 3 months before the first administration of the investigational product
- Administration of any investigational product or use of any investigational device within 60 days prior to first dosing that may affect the pharmacokinetics of the investigational product
- Subjects who have used drugs that may affect the pharmacokinetics (PK) of PZQ from 15 days before the first administration of the investigational product until the last PK sample
- Consumption of substances known to be potent inhibitors or inducers of cytochrome P450s (CYPs) within 2 weeks before the first administration of the investigational product
- Unlikely to comply with the protocol requirements, instructions and trial-related restrictions
- Non-acceptance of the study breakfast
- Excessive consumption of beverages containing xanthine (greater than \[\>\] 5 cups of coffee a day or equivalent) and the inability to refrain from the use of caffeine-containing beverages from 48 hours before the first administration of the investigational product until discharge from the clinic
- Subject is the Investigator or any Sub-Investigator, research assistant, pharmacist, trial coordinator, other staff or relative thereof directly involved in the conduct of the trial
- +2 more criteria
Contact the study team to confirm eligibility.
Sponsors & Collaborators
Study Sites (1)
Please contact the Merck KGaA Communication Center
Darmstadt, Germany
MeSH Terms
Interventions
Intervention Hierarchy (Ancestors)
Results Point of Contact
- Title
- Merck KGaA Communication Center
- Organization
- Merck Healthcare, a business of Merck KGaA, Darmstadt, Germany
Study Officials
- STUDY DIRECTOR
Medical Responsible
Merck KGaA, Darmstadt, Germany
Publication Agreements
- PI is Sponsor Employee
- No
- Restrictive Agreement
- No
Study Design
- Study Type
- interventional
- Phase
- phase 1
- Allocation
- RANDOMIZED
- Masking
- NONE
- Purpose
- TREATMENT
- Intervention Model
- CROSSOVER
- Sponsor Type
- INDUSTRY
- Responsible Party
- SPONSOR
Study Record Dates
First Submitted
December 11, 2014
First Posted
December 25, 2014
Study Start
January 1, 2015
Primary Completion
January 1, 2015
Study Completion
March 1, 2015
Last Updated
February 23, 2017
Results First Posted
February 23, 2017
Record last verified: 2017-01