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Phase 1 Completed N=36 Randomized Other

Bioequivalence Study of Coated Cesol Tablet Formulation Versus Biltricide

Healthy
Source: ClinicalTrials.gov NCT04314037 ↗
Enrolled (actual)
36
Serious AEs
0.0%
Results posted
Aug 2021
Primary outcomePrimary: Maximum Observed Plasma Concentration (Cmax) of Racemic-Praziquantel (Rac-PZQ) — 421; 415; 425; 459 nanogram per milliliter (ng/mL)

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.

Outcome Measures

OutcomeResultp-value
PRIMARY
Maximum Observed Plasma Concentration (Cmax) of Racemic-Praziquantel (Rac-PZQ)
421; 415; 425; 459
PRIMARY
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Racemic-Praziquantel (Rac-PZQ)
894; 873; 886; 964
SECONDARY
Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Treatment Related TEAEs
6; 6; 7; 7; 6; 6
SECONDARY
Number of Participants With Treatment Emergent Adverse Events (TEAEs) by Severity According to Qualitative Toxicity Scale
5; 5; 5; 5; 2; 1
SECONDARY
Number of Participants With Clinically Relevant Changes From Baseline in Laboratory Parameters
0; 0; 0; 0
SECONDARY
Number of Participants With Clinically Relevant Changes From Baseline in Vital Signs
0; 0; 0; 0
SECONDARY
Number of Participants With Clinically Significant Changes From Baseline in 12-Lead Electrocardiogram (ECG) Findings
0; 0; 0; 0
SECONDARY
Maximum Observed Plasma Concentration (Cmax) of Praziquantel (PZQ) Enantiomers: R-(-)-PZQ and S-(+) PZQ
67.8; 71.4; 66.2; 80.0; 349; 346
SECONDARY
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Praziquantel (PZQ) Enantiomers: R-(-)-PZQ and S-(+)-PZQ
103; 111; 104; 125; 772; 758
SECONDARY
Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
932; 907; 926; 1001; 175; 166
SECONDARY
Time to Reach Maximum Plasma Concentration (Tmax) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
2.50; 2.00; 2.50; 2.50; 2.50; 2.00
SECONDARY
Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
0.750; 0.500; 1.00; 0.750; 1.00; 1.00
SECONDARY
Terminal Elimination Half-Life (T1/2) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
2.44; 2.08; 2.43; 2.20; 1.39; 1.35
SECONDARY
Terminal Rate Constant (Lambda z) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
0.284; 0.334; 0.285; 0.315; 0.499; 0.514
SECONDARY
Apparent Clearance (CL/f) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
1287; 1323; 1296; 1199; 6868; 7251
SECONDARY
Apparent Volume of Distribution During Terminal Phase (Vz/f) of Racemic-Praziquantel (Rac-PZQ), R-(-)-PZQ and S-(+)-PZQ
4528; 3963; 4542; 3801; 13761; 14100

Eligibility Criteria

Inclusion Criteria

  • 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
  • Other protocol defined inclusion criteria could apply

Exclusion Criteria

  • 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
  • Other protocol defined exclusion criteria could apply
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT04314037). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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