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Completed

NCT Number: NCT02898779

Metabolism and Pharmacokinetics of Primaquine Enantiomers in Human Volunteers, Study 1

To investigate the comparative tolerability, metabolism and pharmacokinetics of individual enantiomers of PQ in healthy human volunteers. The specific aim is the comparative evaluation of the metabolism, pharmacokinetic behavior, and tolerability of the isomers of PQ (RPQ and SPQ and the racemic mixture RSPQ) in normal healthy human volunteers.

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Key information

Conditions

Malaria Infections Mosquito-Borne Diseases Parasitic Diseases Protozoan Infections Vector Borne Diseases

Age range

18 year–60 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

University of Mississippi

Oxford, Mississippi, 38677, United States

About this study

The primary objective of this project is to investigate the comparative tolerability, metabolism and pharmacokinetics of individual enantiomers of PQ in healthy human volunteers.

The overall approach is as follows: in 36 healthy volunteers with documented normal G6PD activity, we will administer a single oral dose of RPQ, SPQ, or RSPQ. At various times after dosing, we will draw blood samples, in which we will record the plasma levels of the parent drugs, along with plasma and urinary metabolites. The comparative pharmacokinetics, tolerability and hematological effects of these two enantiomers and the racemate will be assessed.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Adults (18-60 years of age)
  • Informed consent
  • Healthy

Exclusion criteria

  • Known history of liver, kidney or hematological disease;
  • known history of cardiac disease, arrhythmia, QT prolongation;
  • Autoimmune disorder;
  • Report of an active infection;
  • Evidence of G6PD deficiency

Treatment and study plan

Primaquine, R-Primaquine, S-Primaquine, SR Primaquine

Drug

Cohort 1: Eighteen individuals (6 per group) Cohort 2: Eighteen individuals (6 per group)

Group 1-15 mg of S-Primaquine followed by one-week washout, 15 mg of R-Primaquine followed by one week washout, and 30 mg of RS-Primaquine.

Group 2- 15 mg of R-Primaquine followed by one-week washout, 30 mg of RSPQ followed by one week washout, and 15 mg of SPQ.

Group 3- 30 mg of RS-Primaquine followed by one week washout,15 mg of SPQ followed by a one week washout, and 15 mg of RPQ.

Other names: Primaquine

Primary outcomes

  1. Primary outcome: Plasma concentration of parent primaquine and carboyprimaquine following a single dose treatment with primaquine (racemate or enantiomers) not to exceed 45 mg

    Time frame: between 0-24 Hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers

Secondary outcomes

  1. Area Under Curve (AUC) for primaquine up to 24 hours after the primaquine administration

    Time frame: between 0-24 hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers

  2. Maximum concentration (Cmax) for primaquine up to 24 hours after the primaquine administration

    Time frame: between 0-24 hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers

  3. Area Under Curve (AUC) for carboxyprimaquine, the major plasma metabolite of primaquine, up to 24 hours after primaquine administration

    Time frame: between 0-24 hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers

  4. Maximum concentration of carboxyprimaquine, the major plasma metabolite of primaquine, up to 24 hours after primaquine administration

    Time frame: between 0-24 hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers

  5. Maximum concentration of selected metabolites primaquine (other than carboxyprimaquine) up to 24 hours after primaquine administration

    Time frame: between 0-24 hours

    This study would provide information on differential pharmacokinetics and metabolism of enantiomers of primaquine in normal human volunteers. The exact nature of these metabolites will be determined from previous animal and human studies

  6. hemoglobin and methemoglobin levels in the blood after administration of primaquine

    Time frame: 0-72 hours

    To monitor hemoglobin and methemoglobin levels in normal human volunteers treated with single dose of primaquine not to exceed 45 mg

  7. Genotyping of Cytochrome P-450 (CYP)

    Time frame: day 0

    To determine correlation between metabolism of primaquine and CYP 2D6 genotype

Sponsors and collaborators

Lead sponsor

University of Mississippi, Oxford

Other

Registry information

Official study title

Development of Safer Drugs for Malaria in U.S. Troops, Civilian Personnel, and Travelers: Clinical Evaluation of Primaquine Enantiomer

Important dates

Study start
2017
Primary completion
2018
Study completion
2018
First posted
Sep 13, 2016
Registry last updated
May 15, 2018

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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