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A Crossover Bioavailability Clinical Trial of Parenteral Pyronaridine and Artesunate

Phase 1
Not yet recruiting
Conditions
Severe Malarial Treatment
Interventions
Drug: artesunate-pyronaridine
Registration Number
NCT05929157
Lead Sponsor
Centre de Recherche Médicale de Lambaréné
Brief Summary

The clinical trial is a Phase I monocentric clinical trial with a two-armed crossover design to evaluate the bioavailability of parenteral Pyronaridine and Artesunate.

Pyronaridine and Artesunate are antimalarial agents with a history of clinical use, and Artesunate has been used clinically in combination with other drugs also. The action of Artesunate is a rapid knock down of the parasites, after which, the drug is quickly cleared as it has a short systemic half-life. Pyronaridine is also rapidly effective in the short term but has a long blood half-life thus providing a more sustained schizonticidal effect.

12 study subjects will be included into the clinical trial after having signed the informed consent, being screened and judged to be eligible. 6 of them (group 1) will, on Day 0, be injected intravenously with 4 mg base/kg of Pyronaridine together with 4 mg/kg of Artesunate. The group 2 (the other 6 subjects) will on the same day (Day 0) be injected intramuscularly with the 4 mg base/kg of Pyronaridine together with 4 mg/kg of Artesunate (into separate sites) 8 weeks later group 1 will be injected intramuscularly with the same amount of Pyronaridine and Artesunate as on Day 0. Group 2 will also get the same amount as on Day 0 but this time the injection will be intravenously for group 2.

The primary objective is to assess the safety and tolerability by measuring (a) the proportion of subjects with adverse events (AEs) and serious adverse events (SAEs) throughout the study; (b) the proportion of subjects with solicited AEs 15 days after IMP injection; (c) the proportion of subjects with unsolicited AEs throughout the clinical trial. Further, the pharmacokinetics of both drugs will be determined.

Detailed Description

The clinical trial is a Phase I monocentric clinical trial with a two-armed crossover design to evaluate the bioavailability of parenteral Pyronaridine and Artesunate.

Pyronaridine and Artesunate are antimalarial agents with a history of clinical use, and Artesunate has been used clinically in combination with other drugs also. The action of Artesunate is a rapid knock down of the parasites, after which, the drug is quickly cleared as it has a short systemic half-life. Pyronaridine is also rapidly effective in the short term but has a long blood half-life thus providing a more sustained schizonticidal effect.

12 study subjects will be included into the clinical trial after having signed the informed consent, being screened and judged to be eligible. 6 of them (group 1) will, on Day 0, be injected intravenously with 4 mg base/kg of Pyronaridine together with 4 mg/kg of Artesunate. The group 2 (the other 6 subjects) will on the same day (Day 0) be injected intramuscularly with the 4 mg base/kg of Pyronaridine together with 4 mg/kg of Artesunate (into separate sites) 8 weeks later group 1 will be injected intramuscularly with the same amount of Pyronaridine and Artesunate as on Day 0. Group 2 will also get the same amount as on Day 0 but this time the injection will be intravenously for group 2.

The primary objective is to assess the safety and tolerability by measuring (a) the proportion of subjects with adverse events (AEs) and serious adverse events (SAEs) throughout the study; (b) the proportion of subjects with solicited AEs 15 days after IMP injection; (c) the proportion of subjects with unsolicited AEs throughout the clinical trial. Further, the pharmacokinetics of both drugs will be determined.

Recruitment & Eligibility

Status
NOT_YET_RECRUITING
Sex
All
Target Recruitment
12
Inclusion Criteria
  • Male and female volunteers aged 18-45 years with an asymptomatic Plasmodium falciparum infection.
  • Able and willing (in the investigator's opinion) to comply with all trial requirements.
  • General good health based on medical history and clinical examination.
  • Written informed consent.
  • Available to participate in follow-up for the duration of the trial (4 months in total).
  • Reachable by phone during the whole trial period.
  • Women only: Must agree to practice continuous effective contraception for the duration of the trial.
Exclusion Criteria
  • Pregnancy, lactation, or intention to become pregnant during the trial.
  • Known HIV-, HBV- and HCV-infection.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Artesunate-pyronaridine intramuscularartesunate-pyronaridine-
Artesunate-pyronaridine intravenousartesunate-pyronaridine-
Primary Outcome Measures
NameTimeMethod
Plasma level of Pyronaridineiwithin the two week post injection

Change in concentration of post IV/IM injection whole blood and plasma level of Pyronaridine will be summarized over time

Plasma level of Artesunate/dihydroartemisininwithin the two week post injection

Change in concentration of post IV/IM injection plasma level of Artesunate/dihydroartemisinin will be summarized over time

Safety of injectable artesunate-pyronaridinewithin the two week post injection

To assess the safety and tolerability by measuring (a) the proportion of subjects with adverse events (AEs) and serious adverse events (SAEs) throughout the study; (b) the proportion of subjects with solicited AEs 15 days after IMP injection; (c) the proportion of subjects with unsolicited AEs throughout the clinical trial

Secondary Outcome Measures
NameTimeMethod
Pyronaridine area under the curvewithin the two week post injection

Pyronaridine area under the whole blood and plasma concentration versus time curves (AUC), over a 24-hour period, following dosing

Artesunate/dihydroartemisinin area under the curvewithin the two week post injection

Artesunate/dihydroartemisinin area under the plasma concentration versus time curve (AUC) , over a 24-hour period, following dosing

Trial Locations

Locations (1)

Centre de Recherches Médicales de Lammbaréné

🇬🇦

Lambaréné, Moyen- Ogooué, Gabon

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