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

University of Mississippi, Oxford

Status and phase: Completed; Phase 1

Conditions: Glucose 6 Phosphate Dehydrogenase Deficiency; Malaria

Treatments: Drug: RPQ; Drug: SPQ; Drug: Placebo; Drug: Primaquine Phosphate

Study type: Interventional

Funder types: Other

Identifiers

NCT03934450

PQ Study 2

Details and patient eligibility

About

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.

Full description

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.

Enrollment: 36 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

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.

Trial design

Primary purpose: Basic Science

Allocation: Non-Randomized

Interventional model: Crossover Assignment

Masking: Single Blind

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36 participants in 4 patient groups, including a placebo group

RPQ (-) enantiomer

Experimental group

Description:

Cohort 1 will receive 15 mg of RPQ (3A) every day for 7 days Cohort 2 will receive 22.5 mg of RPQ (3A) every day for 7 days

Treatment:

Drug: RPQ

SPQ (+) enantiomer

Experimental group

Description:

Cohort 1 will receive 15 mg of SPQ (2A) every day for 7 days Cohort 2 will receive 22.5 mg of SPQ (2A) every day for 7 days

Treatment:

Drug: SPQ

Primaquine Phosphate

Active Comparator group

Description:

Cohort 1 will receive 30 mg of RSPQ (1A) every day for 7 days Cohort 2 will receive 45 mg of RSPQ (1A) every day for 7 days

Treatment:

Drug: Primaquine Phosphate

Placebo

Placebo Comparator group

Description:

Cohort 1 will receive placebo (4A) capsules everyday for seven days Cohort 2 will receive placebo (4A) capsules everyday for seven days

Treatment:

Drug: Placebo