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Safety, Tolerability and PK of Single and Multiple Doses of Oxantel Pamoate Tablets

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT06606860
Lead Sponsor
Swiss Tropical & Public Health Institute
Brief Summary

The goal of this clinical trial is to evaluate the safety, tolerability and pharmacokinetics of oxantel pamoate tablet after administration of a single and multiple dose in healthy male and female adult volunteers.

The main questions aim to answer if oxantel pamoate is safe and well tolerated in healthy volunteers and if is it absorbed by the human body.

A single dose and a multiple dose of oxantel pamoate will be compared to placebo to see if there are any different effects.

Detailed Description

Objectives:

Primary objective:

To investigate the safety and tolerability of oxantel pamoate after single and multiple oral administration of a chewable tablet formulation.

Secondary objective:

To investigate the pharmacokinetics (PK) of oxantel pamoate after single and multiple oral administration of a chewable tablet formulation.

Study Design:

This is a randomized, placebo controlled, double blind, 3-arm Phase I single centre study in a total of 45 healthy adults. The participants will be randomized into one of the following three study arms:

* Study arm 1, 20 participants: Treatment with single dose of 20 mg/kg oxantel pamoate on day 1 followed by administration of two daily doses placebo

* Study arm 2, 20 participants: Treatment with three daily dose of 20 mg/kg oxantel pamoate

* Study arm 3, 5 participants: Treatment with three daily dose of placebo PK sampling will be performed at 13 defined time points (baseline included).

The participants will be admitted to the ward one day prior to commencement of the study treatment (day -1) and will stay until one day after the last dose has been administered. They will have a final follow-up visit on day 14. The safety and tolerability will be assessed as of the first dosage up to the last follow-up visit. Biochemistry, haematology, coagulation and urinalysis will be checked at baseline, day 3 and at the final follow-up visit.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
45
Inclusion Criteria
  • Healthy adult male or non-pregnant (confirmed by a negative serum pregnancy test) and non-breastfeeding female participants, aged between 18 to 45 years at the time of consent.
  • Written informed consent (IC) obtained before any study procedure.
  • Ability to read and write and to understand the participant information sheet and the nature of the trial and any hazards from participating in it (following a test with a maximum of two attempts). Ability to communicate satisfactorily with the Investigator and to participate in, and comply with the requirements of, the entire trial.
  • Women of childbearing potential (WOCBP) must agree to use a highly effective form of contraception from at least 28 days prior to first dosage to 30 days after discharge from the ward.
  • Normal body weight range (BMI between 18 and 29.9 kg/ m2).
Exclusion Criteria
  • Participation in another clinical trial within 3 months prior to the study, or within 5-times the half-life of the drug tested in the previous clinical trial, whichever is longer (time calculated relative to the last dose in the previous clinical trial).
  • Regular daily consumption of more than one liter of xanthine-containing beverages (e.g. tea, coffee, cola or chocolate drinks).
  • Regular daily consumption of more than 5 cigarettes daily.
  • Use of a prescription medicine during the 28 days before the first dose of trial medication or use of an over-the-counter medicine, during the 7 days before the first dose of trial medication.
  • Use of dietary supplements or herbal remedies (such as St John's Wort) known to interfere with the CYP3A4 and/or P-gp metabolic pathway during the 28 days before the first dose of trial medication.
  • Therapies which may impact on the interpretation of study results in the opinion of the Investigator.
  • Medical, social condition, psychiatric disorder or occupational reasons that, in the judgment of the Investigator, is a contraindication to the protocol, may impair the volunteer's ability to give informed consent or effectively participate in the study, may significantly increase the risk to the volunteer because of participation in the study or may impair interpretation of the study data.
  • Blood pressure (BP) and heart rate (HR) in supine position at the screening examination outside the ranges (systolic BP range: 105-136 mm Hg systolic, diastolic BP range: 58-84 mm Hg diastolic; HR range: 56- 96 beats/min).
  • Febrile illness within 1 week before the start of study treatment.
  • History of relevant diseases of vital organs, of the central nervous system or other organs.
  • Known renal or hepatic impairment
  • Participants with a history of allergies, non-allergic drug reactions, adverse reaction to any drug, or multiple drug allergies.
  • Presence or history of drug or alcohol abuse in the last 10 years.
  • Surgery (e.g. stomach bypass) or medical condition that might affect absorption of study drug taken orally.
  • Clinically relevant abnormal medical history, concurrent medical condition, acute or chronic illness or history of chronic illness sufficient to invalidate the volunteer's participation in the trial or make it unnecessarily hazardous.
  • Relevant pathological abnormalities in the electrocardiogram (ECG) such as a second or third-degree AV block, prolongation of the QRS complex over 120 msec or of the QTcF-interval over 450 msec (corrected interval according to Fridericia's formula).
  • Positive test for human immunodeficiency virus (HIV), hepatitis B or C.
  • Positive stool or urine test for helminth infestation by Kato-Katz, urine filtration or Baermann test.
  • Positive for malaria by thick blood smear (TBS).
  • Presence of abnormal physical findings, or laboratory values at the screening assessment that could interfere with the objectives of the trial or the safety of the volunteer.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Arm 1Oxantel PamoateTreatment with a single dose of 20 mg/kg oxantel pamoate followed by administration of two daily doses placebo
Arm 2Oxantel PamoateTreatment with three daily dose of 20 mg/kg oxantel pamoate
Arm 3PlaceboTreatment with three daily doses of placebo
Primary Outcome Measures
NameTimeMethod
General safety (number, frequency, severity, seriousness and duration of adverse events)After first dosage on day 0 to day 14

Summarized statistics on adverse events will be reported under categories such as total adverse events, serious adverse events, treatment emerging adverse events

Heart rate from baselineAfter first dosage on day 0 to day 14

Change of pulse rate from baseline

Blood pressure from baselineAfter first dosage on day 0 to day 14

Change of blood pressure from baseline. Systolic and diastolic blood pressure will be assessed

Temperature from baselineAfter first dosage on day 0 to day 14

Change of axillary temperature from baseline

Respiratory rate from baselineAfter first dosage on day 0 to day 14

Change of respiratory rate from baseline

Creatinine value from baselineAfter first dosage on day 0 to day 14

Change of creatinine value from baseline

Alanine aminotransferase value from baselineAfter first dosage on day 0 to day 14

Change of alanine aminotransferase value from baseline

Aspartate aminotransferase value from baselineAfter first dosage on day 0 to day 14

Change of aspartate aminotransferase value from baseline

Total bilirubin value from baselineAfter first dosage on day 0 to day 14

Change of total bilirubin value from baseline

Sodium value from baselineAfter first dosage on day 0 to day 14

Change of sodium value from baseline

Potassium value from baselineAfter first dosage on day 0 to day 14

Change of potassium value from baseline

Blood urea nitrogen value from baselineAfter first dosage on day 0 to day 14

Change of blood urea nitrogen value from baseline

Haemoglobin value from baselineAfter first dosage on day 0 to day 14

Change of haemoglobin value from baseline

Red blood cell count from baselineAfter first dosage on day 0 to day 14

Change of red blood cell count from baseline

Mean corpuscular volume from baselineAfter first dosage on day 0 to day 14

Change of mean corpuscular volume from baseline

Mean corpuscular haemoglobin value from baselineAfter first dosage on day 0 to day 14

Change of mean corpuscular haemoglobin value from baseline

Mean corpuscular haemoglobin concentration from baselineAfter first dosage on day 0 to day 14

Change of mean corpuscular haemoglobin concentration from baseline

Platelets value from baselineAfter first dosage on day 0 to day 14

Change of platelets value from baseline

White blood cell count from baselineAfter first dosage on day 0 to day 14

Change of white blood cell count from baseline

Neutrophils value from baselineAfter first dosage on day 0 to day 14

Change of neutrophils value from baseline

Lymphocytes value from baselineAfter first dosage on day 0 to day 14

Change of lymphocytes value from baseline

Monocytes value from baselineAfter first dosage on day 0 to day 14

Change of monocytes value from baseline

Eosinophils value from baselineAfter first dosage on day 0 to day 14

Change of eosinophils value from baseline

Basophils value from baselineAfter first dosage on day 0 to day 14

Change of basophils value from baseline

Prothrombin time from baselineAfter first dosage on day 0 to day 14

Change of prothrombin time value from baseline

Activated partial thromboplastin time from baselineAfter first dosage on day 0 to day 14

Change of activated partial thromboplastin time value from baseline

Protein in urine from baselineAfter first dosage on day 0 to day 14

Change of proteine in urine from baseline

Blood in urine from baselineAfter first dosage on day 0 to day 14

Change of blood in urine from baseline

Secondary Outcome Measures
NameTimeMethod
Cmax of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

Peak Plasma Concentration (Cmax) of oxantel pamoate, if detectable

Tmax of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

Time to reach Cmax (Tmax), in case of plasma concentration determined.

AUC of oxantel pamoatePlasma samples taken pre-dose -0.5 hours, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

Area under the curve (AUC) of the plasma concentration determined.

AUC (0-t) of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

Concentration from time zero to the last quantifiable concentration at time t, in case plasma concentration can be determined.

T1/2 of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

The plasma elimination half-life, In case plasma concentration can be determined.

AUC (tau) of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

The area under the plasma concentration curve over dosing interval, in case plasma concentration can be determined.

AUC (0-∞) of oxantel pamoatePlasma samples taken pre-dose -0.5 hours prior first dose, then 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after first dose and 1 hour, 3 hours, 5 hours, 8 hours, 12 hours, 24 hours after third dose

The AUC of the plasma concentration from time zero to infinity with extrapolation of the terminal phase, In case plasma concentration can be determined.

Trial Locations

Locations (1)

Ifakara Health Institute

🇹🇿

Bagamoyo, Tanzania

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