NCT05930782

Piperaquine Granule Formulation Relative Bioavailability and Food Effect Study in Healthy Volunteers.

A Randomized, Open Label, Two-part, Parallel-group, Phase I Study to Evaluate the Pharmacokinetics of Piperaquine Oral Dispersible Granules Formulation Compared to Piperaquine Hard Tablets Administered as a Single Dose in Fasting Condition (Part 1) and of Piperaquine Oral Dispersible Granules Formulation Administered as Single Dose in Various Fed States (Part 2) in Healthy Adult Participants

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 60 (actual)
• Sponsor: Medicines for Malaria Venture · Academic / Other
• Sex: All
• Age: 18 Years – 55 Years
• Healthy volunteers: Accepted

Summary

This trial aims to characterise the pharmacokinetic (PK) profile and estimate drug exposure of a single oral dose of piperaquine (PQP) in a dispersible granule formulation compared to the PQP hard tablet formulation in the fasted state (Part 1), to advise the selection of dose when the PQP granule formulation is administered in a fed state in healthy adult participants. Part 2 will assess the effect on different types of meal composition on the PK of a single dose of PQP granule formulation in healthy adult participants.

Detailed description

Adult participants who give written informed consent will be screened within 45 days to determine their eligibility before entering the trial on Day -1. The trial will initially establish the pharmacokinetic (PK) profile and estimated drug exposure of a single oral dose of PQP in a dispersible granule formulation compared to the PQP hard tablet formulation in the fasted state (Part 1). In the second study part, and based on the PK results of Part 1, it is intended to administer the same dose level of 320 mg PQP dispersible granules concomitant with different fed conditions. However, if from Part 1 of the study it is shown that PQP dispersible granules formulation provides a significant improvement in Cmax values in the fasted state, this dose level may be adjusted for Part 2, in order to take into account a potential 3-fold increase in exposure which is the observed food effect when film-coated tablets (Eurartesim®) are administered with a high fat/high calorie meal. Such dose adjustment will be based on the safety and preliminary PK interim results of the granule formulation in the fasted state. The PQP dose selected in Part 2 (as dispersible granules formulation) will take into account a 3-fold factor increase in exposure when administered with food (see above) with such predicted exposure in the presence of food being not higher than after the administration of 960 mg PQP in tablet of Eurartesim® in adult subjects dosed in fasting conditions. Furthermore, sufficient data will be available to address key questions on both, safety and PK parameters to enable the review and recommendation by the SRC for the optimal dose of the granule formulation to be administered in Part 2.

Conditions

• Malaria

Interventions

Type	Name	Description
DRUG	Piperaquine Tetraphosphate uncoated tablets	Piperaquine tetraphosphate hard tablet 320 mg; single dose (320 mg) given orally with 240 ml of water
DRUG	Piperaquine Tetraphosphate dispersible granules	Piperaquine tetraphosphate dispersible granules 320 mg dose equivalent dispersed in 25 ml of water; single dose (320 mg) given orally

Timeline

• Start date: 2023-08-14
• Primary completion: 2023-12-06
• Completion: 2024-01-03
• First posted: 2023-07-05
• Last updated: 2025-03-18
• Results posted: 2025-03-06

Locations

1 site across 1 country: Tanzania