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.
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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
SINGLE
Enrollment
36
The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.
The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.
The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.
University of Mississippi
University, Mississippi, United States
Change in Methemoglobin concentration in blood from baseline
Change in Methemoglobin concentration in blood from baseline (% hemoglobin)
Time frame: Days 0, 3, 5, 7
Primaquine Plasma concentration, ng/mL
Plasma concentrations of parent drug
Time frame: Days 0, 3, 5, 7
Carboxy- Primaquine Plasma concentration, ng/mL
Plasma concentrations of carboxy-primaquine metabolite
Time frame: Days 0, 3, 5, 7
Primaquine N-carbamoyl-glucuronide Plasma concentration, ng/mL
Plasma concentrations of Primaquine N-carbamoyl-glucuronide metabolite
Time frame: Days 0, 3, 5, 7
Primaquine Orthoquinone Plasma concentration, ng/mL
Plasma concentrations of Primaquine Orthoquinone metabolite
Time frame: Days 0, 3, 5, 7
Change in Hematocrit (%) Compared to baseline
Change in Hematocrit (%) Compared to baseline
Time frame: Days 0, 3, 5, 7
Change in Hemoglobin (g/dL) Compared to baseline
Change in Hemoglobin (g/dL) Compared to baseline
Time frame: Days 0, 3, 5, 7
Change in AST (U/L) Compared to baseline
Change in Aspartate aminotransferase (U/L) Compared to baseline; used to monitor liver function
Time frame: Days 0, 3, 5, 7
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
The study will compare the individual enantiomers of primaquine - R- (-)-PQ, S-(+)-PQ, and Placebo along with the racemic version.
Change in ALT (U/L) Compared to baseline
Change in Alanine aminotransferase (U/L) Compared to baseline; used to monitor liver function
Time frame: Days 0, 3, 5, 7
Change in Total Bilirubin (mg/dL) Compared to baseline
Change in Total Bilirubin (mg/dL) Compared to baseline; used to monitor liver function and red cell integrity
Time frame: Days 0, 3, 5, 7