Relative Bioavailability Trial of Oral Dispersible Praziquantel Tablets in Healthy Volunteers

January 3, 2017 updated by: Merck KGaA, Darmstadt, Germany

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

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.

Study Overview

Status

Completed

Conditions

Intervention / Treatment

Study Type

Interventional

Enrollment (Actual)

32

Phase

  • Phase 1

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Locations

  • Germany
      • Darmstadt, Germany
        • Please contact the Merck KGaA Communication Center

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Ages Eligible for Study

18 years to 55 years (Adult)

Accepts Healthy Volunteers

No

Genders Eligible for Study

Male

Description

Inclusion Criteria:

  • 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

Exclusion Criteria:

  • 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
  • Vulnerable subjects
  • Legal incapacity or limited legal capacity

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

  • Primary Purpose: Treatment
  • Allocation: Randomized
  • Interventional Model: Crossover Assignment
  • Masking: None (Open Label)

Arms and Interventions

Participant Group / Arm
Intervention / Treatment
Experimental: Sequence A-B-C1-D1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-C1-D2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-C2-D1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-C2-D2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-D1-C1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-D2-C1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-D1-C2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence A-B-D2-C2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-C1-D1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-C1-D2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-C2-D1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-C2-D2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-D1-C1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-D2-C1
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-D1-C2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Experimental: Sequence B-A-D2-C2
Drug: Oral dispersible tablet of praziquantel (ODT-PZQ)
Treatment A (test): ODT-PZQ (MSC1028703A) at a single dose of 40 milligram per kilogram (mg/kg) orally dispersed in water after meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment B (reference): Cysticide tablet at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ
Drug: ODT-PZQ
Treatment C1 (test): ODT-PZQ (MSC1028703A) at a single dose of 20 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment C2 (test): ODT-PZQ (MSC1028703A) at a single dose of 60 mg/kg orally dispersed in water after a meal.
Other Names:
  • MSC1028703A
Drug: ODT-PZQ
Treatment D1 (test): ODT-PZQ (MSC1028703A) at a single dose of 40 mg/kg orally dispersed in water without a meal.
Other Names:
  • MSC1028703A
Drug: Cysticide
Treatment D2 (reference): Cysticide crushed tablets at a single dose of 40 mg/kg will be given with water orally after a meal.
Other Names:
  • PZQ

What is the study measuring?

Primary Outcome Measures

Outcome Measure
Measure Description
Time Frame
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)
Time Frame: 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
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 Outcome Measures

Outcome Measure
Measure Description
Time Frame
Maximum Observed Concentration in Plasma (Cmax) Adjusted for the Actual Administered Dose (Cmax, Adj) of L-PZQ, D-PZQ and Racemate PZQ
Time Frame: 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
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
Time Frame: 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
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
Time Frame: 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 was defined as the time required for the plasma concentration of drug to decrease 50 percent in the final stage of its elimination.
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
Time Frame: 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
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
Time Frame: 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
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
Extrapolated Area Under the Plasma Concentration Curve From Time Tlast to Infinity (AUCextra) of L-PZQ, D-PZQ, and Racemate PZQ
Time Frame: 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
AUCextra was reported in terms of percentage of AUC0-inf.
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 Elimination Rate Constant (λz) of L-PZQ, D-PZQ, and Racemate PZQ
Time Frame: 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
λz was determined from the terminal slope of the log-transformed plasma concentration curve using linear regression method.
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
Relative Bioavailability (Frel) of L-PZQ, D-PZQ, and Racemate PZQ
Time Frame: 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
Frel was calculated for Treatment A versus Treatment B only. It was calculated by using AUC0-∞, with treatment A as the Test and treatment B as the Reference. Frel = AUC0-inf (test) / AUC0-inf (reference).
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 Total Body Clearance of Drug From Plasma (CL/f) of L-PZQ, D-PZQ, and Racemate PZQ
Time Frame: 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
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.
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 Volume of Distribution During the Terminal Phase (Vz/f) of L-PZQ, D-PZQ, and Racemate PZQ
Time Frame: 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
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. Vz/f after oral dose was influenced by the fraction absorbed.
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
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 D-PZQ and Racemate PZQ
Time Frame: 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
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 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
Number of Subjects With Treatment-emergent Adverse (TEAEs), Serious TEAEs, TEAEs Leading to Discontinuation
Time Frame: Baseline up to end of treatment (up to Day 32)
An adverse event (AE) was defined as any untoward medical occurrence in a subject 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 stud drug.
Baseline up to end of treatment (up to Day 32)
Palatability Assessment Based on Visual Analog Scale (VAS) Score
Time Frame: Immediately and 2-5 minutes (min) after dosing on Day 1 of each treatment
Palatability was assessed in terms of Flavor, Smell, Sweetness, Overall liking of the medicine, Taste and Acceptability to swallow, each parameter assessed on a 0 to 100 millimeter (mm) visual analog scale (VAS), where 0 indicates "Did not like" and 100 indicates "very much liked". Flavor, Smell, Sweetness and Overall liking of the medicine were evaluated immediately after taking the medication (Day 1, 0 Hour) and Taste and Acceptability to swallow were assessed 2-5 minutes post administration of medication.
Immediately and 2-5 minutes (min) after dosing on Day 1 of each treatment
Number of Subjects With Clinically Significant Change From Baseline in Vital Signs, Physical Examinations, Electrocardiogram (ECG) and Laboratory Parameters
Time Frame: Baseline up to end of treatment (up to Day 32)
Vital signs included oral body temperature, blood pressure and pulse rate. Body weight was recorded for physical examinations. The 12-lead ECGs were recorded after the subjects have rested for at least 5 minutes in supine position. The parameters heart rate (HR), RR, PR, QRS, QT and QTcB calculated by the Bazett formula. Laboratory investigation including chemistry, hematology and urinalysis.
Baseline up to end of treatment (up to Day 32)

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

Merck KGaA, Darmstadt, Germany

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start

January 1, 2015

Primary Completion (Actual)

January 1, 2015

Study Completion (Actual)

March 1, 2015

Study Registration Dates

First Submitted

December 11, 2014

First Submitted That Met QC Criteria

December 21, 2014

First Posted (Estimate)

December 25, 2014

Study Record Updates

Last Update Posted (Actual)

February 23, 2017

Last Update Submitted That Met QC Criteria

January 3, 2017

Last Verified

January 1, 2017

More Information

Terms related to this study

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Other Study ID Numbers

  • 200585-001

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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