Phase 1
Completed N=36
Relative Bioavailability Trial of L-Praziquantel in Healthy Volunteers
Healthy
Source: ClinicalTrials.gov NCT02271984 ↗
Enrolled (actual)
36
Serious AEs
0.0%
Results posted
Jan 2018
Primary outcomePrimary: Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Infinity (AUC0-inf) Adj of L-Praziquantel (L-PZQ) After Dose Adjustment — 825.2; 2066.0; 216.7; 2324.9 hour*nanogram per milliliter (h*ng/mL)
Summary
This is a phase I, open-label, randomized, 5 period, crossover, single-center trial. The purpose of this trial is to assess the relative bio-availability of L-praziquantel (L-PZQ [MSC2499550A]) oral dispersible tablet (ODT) formulation (150 milligram [mg]) versus the current marketed racemate praziquantel (PZQ) (Cysticide® 500 mg) formulation in healthy male volunteers under fed conditions.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Infinity (AUC0-inf) Adj of L-Praziquantel (L-PZQ) After Dose Adjustment |
825.2; 2066.0; 216.7; 2324.9; 506.2; 954.5 | — |
| SECONDARY Time to Reach the Maximum Plasma Concentration (Tmax) of L-Praziquantel (L-PZQ) |
2.500; 2.500; 2.250; 3.000; 2.000; 4.000 | — |
| SECONDARY Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of L-Praziquantel (L-PZQ) |
0.0; 0.0; 0.0; 0.0; 0.0; 0.0 | — |
| SECONDARY Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Last Sampling Time at Which the Concentration is at or Above the Lower Limit of Quantification (AUC0-t) of L-Praziquantel (L-PZQ) After Dose Adjustment |
791.0; 2010.7; 186.2; 2273.5; 464.7; 918.0 | — |
| SECONDARY Extrapolated Area Under the Concentration Time Curve (AUC) From Time Tlast to Infinity Given as Percentage From AUC0-inf (AUCextra) of L-Praziquantel (L-PZQ) |
3.40; 2.20; 6.62; 1.80; 5.81; 3.15 | — |
| SECONDARY Maximum Observed Concentration in Plasma (Cmax) of L-Praziquantel (L-PZQ) After Dose Adjustment |
378.83; 727.27; 89.93; 1051.76; 131.06; 471.18 | — |
| SECONDARY Apparent Terminal Half-life (T1/2) of L-Praziquantel (L-PZQ) |
2.984; 3.788; 1.059; 3.296; 2.801; 2.711 | — |
| SECONDARY Relative Bioavailability (Frel) of L-Praziquantel (L-PZQ) |
40.075 | — |
| SECONDARY Apparent Terminal Elimination Rate Constant (Lambda Z) of L-Praziquantel (L-PZQ) |
0.250; 0.181; 0.432; 0.206; 0.244; 0.264 | — |
| SECONDARY Apparent Total Body Clearance of Drug From Plasma (CL/f) of L-Praziquantel (L-PZQ) |
1665; 667.3; 3091; 923.5; 2729; 1440 | — |
| SECONDARY Apparent Volume of Distribution During the Terminal Phase (Vz/f) of L-Praziquantel (L-PZQ) |
6671; 3685; 7155; 4478; 11170; 5452 | — |
| SECONDARY Number of Subjects With Treatment Emergent Adverse Events (TEAEs) and Serious TEAEs, TEAEs Leading to Death and TEAEs Leading to Discontinuation |
8; 17; 4; 4; 5; 1 | — |
| SECONDARY Palatability Score |
67.5; 45.8; 72.2; 68.8; 65.9; 32.9 | — |
| SECONDARY Number of Subjects With Clinical Significant Laboratory Abnormalities, Electrocardiogram (ECG), Physical Examination and Vital Signs Reported as Treatment Emergent Adverse Events |
0; 0; 0; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Healthy males aged 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
- Written informed consent prior to any trial related procedure
- Have a body weight of greater than or equal to (>=) 55.0 kilogram (kg) to less than ( 5 cups ) of coffee a day, or equivalent or inability to stop consuming caffeine from 48 hours prior to drug administration 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 (for example, persons kept in detention)
- Legal incapacity or limited legal capacity
Data sourced from ClinicalTrials.gov (NCT02271984). 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.