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OpenTrials
Completed

NCT Number: NCT03934450

Metabolism and Pharmacokinetics of Primaquine Enantiomers in Human Volunteers Receiving a Seven Day Dose Regimen

To investigate the comparative tolerability, metabolism and pharmacokinetics of individual enantiomers of PQ in healthy human volunteers, receiving study drug over the course of 7 days.

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Key information

Conditions

Malaria Anemia Anemia, Hemolytic Anemia, Hemolytic, Congenital Carbohydrate Metabolism, Inborn Errors Congenital, Hereditary, and Neonatal Diseases and Abnormalities Genetic Diseases, Inborn Glucose 6 Phosphate Dehydrogenase Deficiency Glucosephosphate Dehydrogenase Deficiency Hematologic Diseases Hemic and Lymphatic Diseases Hemolysis Infections Metabolic Diseases Metabolism, Inborn Errors Mosquito-Borne Diseases Nutritional and Metabolic Diseases Parasitic Diseases Pathologic Processes Pathological Conditions, Signs and Symptoms Protozoan Infections Vector Borne Diseases

Age range

18 year–65 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

University of Mississippi

University, 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. Based on the results of this study, if one enantiomer seems to show a better safety profile (in terms of hematological effects), an analogous study will be carried out in G6PD deficient individuals (under a separate protocol). The studies are primarily aimed at understanding the tolerability and safety of the enantiomers in G6PD deficiency. If one shows a better safety profile, ultimately the evaluation of its efficacy will be required.

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Normal, healthy adults aged 18 to 65 years

Exclusion criteria

  • Known history of liver, kidney or hematological disease
  • Known history of cardiac disease, Non Sinus Rhythm arrhythmia or QT prolongation
  • Autoimmune disorders
  • Report of an active infection
  • Evidence of G6PD deficiency
  • Participant is pregnant or breast-feeding, or is expecting to conceive during the study.

Treatment and study plan

RPQ

Drug

The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.

Other names: R-(-) Enantiomer of Primaquine Phosphate

SPQ

Drug

The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.

Other names: S-(+) Enantiomer of Primaquine Phosphate

Primaquine Phosphate

Drug

The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.

Other names: Racemic Primaquine

Placebo

Drug

The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.

Primary outcomes

  1. Change in Methemoglobin concentration in blood from baseline

    Time frame: Days 0, 3, 5, 7

    Change in Methemoglobin concentration in blood from baseline (% hemoglobin)

Secondary outcomes

  1. Primaquine Plasma concentration, ng/mL

    Time frame: Days 0, 3, 5, 7

    Plasma concentrations of parent drug

  2. Carboxy- Primaquine Plasma concentration, ng/mL

    Time frame: Days 0, 3, 5, 7

    Plasma concentrations of carboxy-primaquine metabolite

  3. Primaquine N-carbamoyl-glucuronide Plasma concentration, ng/mL

    Time frame: Days 0, 3, 5, 7

    Plasma concentrations of Primaquine N-carbamoyl-glucuronide metabolite

  4. Primaquine Orthoquinone Plasma concentration, ng/mL

    Time frame: Days 0, 3, 5, 7

    Plasma concentrations of Primaquine Orthoquinone metabolite

  5. Change in Hematocrit (%) Compared to baseline

    Time frame: Days 0, 3, 5, 7

    Change in Hematocrit (%) Compared to baseline

  6. Change in Hemoglobin (g/dL) Compared to baseline

    Time frame: Days 0, 3, 5, 7

    Change in Hemoglobin (g/dL) Compared to baseline

  7. Change in AST (U/L) Compared to baseline

    Time frame: Days 0, 3, 5, 7

    Change in Aspartate aminotransferase (U/L) Compared to baseline; used to monitor liver function

  8. Change in ALT (U/L) Compared to baseline

    Time frame: Days 0, 3, 5, 7

    Change in Alanine aminotransferase (U/L) Compared to baseline; used to monitor liver function

  9. Change in Total Bilirubin (mg/dL) Compared to baseline

    Time frame: Days 0, 3, 5, 7

    Change in Total Bilirubin (mg/dL) Compared to baseline; used to monitor liver function and red cell integrity

Sponsors and collaborators

Lead sponsor

University of Mississippi, Oxford

Other

Registry information

Important dates

Study start
2018
Primary completion
2019
Study completion
2019
First posted
May 1, 2019
Registry last updated
May 14, 2019

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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