Bioequivalence Study of Coated Cesol Tablet Formulation Versus Biltricide

NCT04314037 | Completed Phase 1 Results

• 2 other identifiers: MS200585_00042019-002868-27
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess the bioequivalence (BE) of new coated Cesol tablet (Test) versus Biltricide tablets (Comparator) in healthy male participants. Praziquantel (rac-PZQ) is the active ingredient for Cesol and Biltricide tablets.

Conditions

Healthy

Keywords

Bioavailability; Bioequivalence; Praziquantel; Cesol; Pharmacokinetics

Outcome Measures

Primary Outcomes (2)

• Maximum Observed Plasma Concentration (Cmax) of Racemic-Praziquantel (Rac-PZQ)

  Cmax was obtained directly from the concentration versus time curve.

  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 hours post-dose in each treatment period

• Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Racemic-Praziquantel (Rac-PZQ)

  Area under the plasma concentration versus time curve from time zero to the last sampling time t at which the concentration was at or above the lower limit of quantification (LLQ). AUC0-t was calculated according to the mixed log-linear trapezoidal rule.

  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 hours post-dose in each treatment period

Secondary Outcomes (14)

• Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Treatment Related TEAEs

  Baseline up to Day 27

• Number of Participants With Treatment Emergent Adverse Events (TEAEs) by Severity According to Qualitative Toxicity Scale

  Baseline up to Day 27

• Number of Participants With Clinically Relevant Changes From Baseline in Laboratory Parameters

  Baseline up to Day 27

• Number of Participants With Clinically Relevant Changes From Baseline in Vital Signs

  Baseline up to Day 27

• Number of Participants With Clinically Significant Changes From Baseline in 12-Lead Electrocardiogram (ECG) Findings

  Baseline up to Day 27

Study Arms (2)

Sequence 1 (T1-R1-T2-R2)

EXPERIMENTAL

Participants will receive first dose of Cesol on Day 1 in treatment period 1 followed by first dose of Biltricide on Day 8 in treatment period 2 followed by second dose of Cesol on Day 15 in treatment period 3 followed by second dose of Biltricide on Day 22 in treatment period 4. A washout period of 7 days will be maintained between 4 treatment periods.

Drug: Cesol (Test); Drug: Biltricide (Reference)

Sequence 2 (R1-T1-R2-T2)

EXPERIMENTAL

Participants will receive first dose of Biltricide on Day 1 in treatment period 1 followed by first dose of Cesol on Day 8 in treatment period 2 followed by second dose of Biltricide on Day 15 in treatment period 3 followed by second dose of Cesol on Day 22 in treatment period 4. A washout period of 7 days will be maintained between 4 treatment periods.

Drug: Cesol (Test); Drug: Biltricide (Reference)

Interventions

Cesol (Test) DRUG

Participant will receive coated cesol tablet in sequence 1 (Day 1 and Day 15) and in sequence 2 (Day 8 and Day 22). A washout period of 7 days will be maintained between 4 treatment periods.

Also known as: Praziquantel

Sequence 1 (T1-R1-T2-R2); Sequence 2 (R1-T1-R2-T2)

Biltricide (Reference) DRUG

Participant will receive biltricide tablet in Sequence 1 (Day 8 and Day 22) and in sequence 2 (Day 1 and Day 15). A washout period of 7 days will be maintained between 4 treatment periods.

Also known as: Praziquantel

Sequence 1 (T1-R1-T2-R2); Sequence 2 (R1-T1-R2-T2)

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants who are overtly healthy as determined by medical evaluation, including medical history, physical examination, laboratory tests, and cardiac monitoring
• Nonsmoker (=0 cigarettes, pipes, cigars or others) since at least 3 months
• Have a body weight within 55.0 to 95.0 kilogram (kg) and body mass index within the range of 18.5 to 29.9 kilogram per meter squared (kg/m\^2)
• Electrocardiogram recording (12-lead) without signs of clinically relevant pathology in particular heart-rate corrected \[QTc\] (Bazett) \<450 milliseconds (ms)
• Vital signs should be in normal range (systolic blood pressure: 90 to 140 millimeters of mercury \[mmHg\]; diastolic blood pressure: 50 to 90 mmHg; pulse rate: 50 to 90 beats per minute \[bpm\]; auricular body temperature between 35.9 degree centigrade \[°C\] to 37.6°C)
• Are males agreeing to refrain from donating sperm, Use a male condom when having sexual intercourse with a woman of child-bearing potential, who is not currently pregnant, and advise her to use a highly effective contraceptive method with a failure rate of less than (\< )1 percent (%) per year

You may not qualify if:

• Any condition, including any clinically relevant abnormality in the safety laboratory parameters as judged by the Investigator, that in the Investigator's opinion constitutes an inappropriate risk or a contraindication for participation in the study or that could interfere with the study objectives, conduct, or evaluation
• Have positive results from serology examination for Hepatitis B surface antigen (indicative of active Hepatitis B), Hepatitis C Virus or Human Immunodeficiency Virus (Human Immunodeficiency Virus 1/2 antibodies)
• Participants who have used drugs that may affect the pharmacokinetics of rac-PZQ from 15 days before dosing until the last PK sample, example., phenytoin, barbiturates, primidone, carbamazapine, oxcarbazepine, topiramate, felbamate, rifampicin, nelfinavir, ritonavir, griseofulvin, oral ketoconazole
• Positive test for drugs of abuse (including alcohol) at Screening and prior to each dosing
• Unlikely to comply with the protocol requirements, instructions and study-related restrictions; example, uncooperative attitude, inability to return for follow-up visits, and improbability of completing the study
• Participant is the Principal Investigator or any Sub investigator, research assistant, pharmacist, study coordinator, other staff or relative thereof directly involved in the conduct of the study
• Inability to communicate or cooperate with the Investigator (example. language problem, illiterates, poor mental status) or to comply with the requirements of the entire study, including dietary restrictions
• Vulnerable participants (example., persons kept in detention).
• Legal incapacity or limited legal capacity

Sponsors & Collaborators

• Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany: lead

Study Sites (1)

Nuvisan GmbH

Neu-Ulm, 89231, Germany

Location

Related Links

• Trial Awareness and Transparency website
• Medical Information Location Map - Med Info Contacts

MeSH Terms

Interventions

Praziquantel

Intervention Hierarchy (Ancestors)

Isoquinolines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds

Results Point of Contact

• Title: Communication Center
• Organization: Merck Healthcare KGaA, Darmstadt Germany, an affiliate of Merck KGaA, Darmstadt, Germany

service@emdgroup.com

+49-6151-72-5200

Study Officials

• Medical Responsible

  Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: No

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 17, 2020
• First Posted: March 18, 2020
• Study Start: June 17, 2020
• Primary Completion: July 30, 2020
• Study Completion: July 30, 2020
• Last Updated: August 13, 2021
• Results First Posted: August 13, 2021

Record last verified: 2021-06

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)