Phase 1
Completed N=32
Relative Bioavailability Trial of Oral Dispersible Praziquantel Tablets in Healthy Volunteers
Healthy
Source: ClinicalTrials.gov NCT02325713 ↗
Enrolled (actual)
32
Serious AEs
0.0%
Results posted
Feb 2017
Primary outcomePrimary: 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) — 1969.6; 2047.9; 345.4; 4871.3 Hour*nanograms per milliliter (h*ng/mL)
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY 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) |
1969.6; 2047.9; 345.4; 4871.3; 924.9; 1537.7 | — |
| SECONDARY Maximum Observed Concentration in Plasma (Cmax) Adjusted for the Actual Administered Dose (Cmax, Adj) of L-PZQ, D-PZQ and Racemate PZQ |
881.3; 762.6; 154.6; 1548; 189.3; 446.3 | — |
| SECONDARY Time to Reach Maximum Plasma Concentration (Tmax) of L-PZQ, D-PZQ, and Racemate PZQ |
3.000; 1.500; 4.000; 3.000; 4.250; 2.500 | — |
| SECONDARY Apparent Terminal Half-life (t1/2) of L-PZQ, D-PZQ, and Racemate PZQ |
3.305; 3.830; 1.916; 4.202; 4.168; 3.072 | — |
| SECONDARY Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of L-PZQ, D-PZQ, and Racemate PZQ |
0.000; 0.000; 0.000; 0.000; 0.000; 0.000 | — |
| SECONDARY 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 |
1928.0; 1994.0; 300.5; 4770.1; 863.7; 1342.6 | — |
| SECONDARY Extrapolated Area Under the Plasma Concentration Curve From Time Tlast to Infinity (AUCextra) of L-PZQ, D-PZQ, and Racemate PZQ |
1.86; 2.23; 5.25; 1.60; 5.52; 2.30 | — |
| SECONDARY Apparent Terminal Elimination Rate Constant (λz) of L-PZQ, D-PZQ, and Racemate PZQ |
0.210; 0.181; 0.362; 0.165; 0.166; 0.226 | — |
| SECONDARY Relative Bioavailability (Frel) of L-PZQ, D-PZQ, and Racemate PZQ |
96.175; 90.951; 92.2 | — |
| SECONDARY Apparent Total Body Clearance of Drug From Plasma (CL/f) of L-PZQ, D-PZQ, and Racemate PZQ |
716.8; 691.3; 2028.4; 438.5; 1466.9; 971.1 | — |
| SECONDARY Apparent Volume of Distribution During the Terminal Phase (Vz/f) of L-PZQ, D-PZQ, and Racemate PZQ |
3417.6; 3820.4; 5605.6; 2658.4; 8820.4; 4304.4 | — |
| SECONDARY 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 |
7542.3; 8292.7; 2226.0; 14685.8; 4996.0; 6508.9 | — |
| SECONDARY Number of Subjects With Treatment-emergent Adverse (TEAEs), Serious TEAEs, TEAEs Leading to Discontinuation |
5; 4; 1; 6; 0; 3 | — |
| SECONDARY Palatability Assessment Based on Visual Analog Scale (VAS) Score |
43.4; 44.6; 50.3; 46.1; 55.9; 20.1 | — |
| SECONDARY Number of Subjects With Clinically Significant Change From Baseline in Vital Signs, Physical Examinations, Electrocardiogram (ECG) and Laboratory Parameters |
0; 0; 0; 0; 0; 0 | — |
Eligibility Criteria
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 ( ] 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
Data sourced from ClinicalTrials.gov (NCT02325713). 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.