NCT02751294

A Randomized, Open-label, Single-period, Parallel-group Study in Healthy Subjects to Determine the Effects of Dissolution Profile on the Pharmacokinetics (Via Both Venous and Peripheral Micro-samples) of Single Oral 300 mg Doses of Tafenoquine (SB-252263) Tablets + 30 mg Tafenoquine Stable Isotope Labelled (SIL) Solution

Completed Phase 1 Last updated 19 January 2017

What this trial tests

Phase 1 trial testing Tafenoquine Control in Malaria, Vivax in 14 participants. Completed in 1 August 2016.

Timeline

1 May 2016

Primary endpoint
1 August 2016

1 August 2016

Quick facts

Lead sponsor	GlaxoSmithKline
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	parallel
Masking	none
Primary purpose	treatment
Enrollment	14
Start date	1 May 2016
Primary completion	1 August 2016
Estimated completion	1 August 2016
Sites	1 location across United States

Drugs / interventions tested

• Tafenoquine Control — full drug profile →
• Tafenoquine dissolution profile X — full drug profile →
• Tafenoquine SIL — full drug profile →

Conditions studied

• Malaria, Vivax — all drugs for Malaria, Vivax →

Sponsor

GlaxoSmithKline — full company profile →

Who can join

Adults 18 to 55, male only, with Malaria, Vivax. Healthy volunteers can join.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• Ratio of the geometric means for the area under plasma concentration-time curve (AUC) for Tafenoquine X
  Time frame: Samples will be collected at Pre-dose and 1, 2, 6, 9, 12, 15, 20, 24, 36, 48, 60, and 72 hours post dose on Day 1 and single sample on Day 7, 14, 21, 28, and 56
  Blood samples for PK analysis of TQ will be collected for evaluation of ratio of the geometric means (90% Confidence Interval \[CI\]) for the area under plasma concentration-time curve from 0 to time t (AUC \[0-t\]) and area under the concentration-time curve from 0 to infinity (AUC\[0-inf\]) for the treatment group dissolution profile X compared to Control.

Sponsor's own description

This study will investigate the effect of Tafenoquine (TQ) 150 mg tablet ageing (dissolution profiles) on human exposure of TQ comparing the relative bioavailability of TQ from tablets exhibiting different dissolution profiles in healthy subjects. This is a single-centre, 2-arm, randomized open-label, parallel-group study in healthy subjects. All subjects will arrive in the unit approximately 24 hours prior to dosing and will be discharged after the 72-hour post-dose assessments are completed. Subjects will return for outpatient visits on Days 7, 14, 21, 28, and 56 after dosing. A total of 14 subjects (n=7 subjects in each arm) are planned to be enrolled. All subjects will receive a single dose of study medication (2x150 mg TQ tablets + 30 mg TQ SIL in solution) and participate through a 56-day post dose follow-up visit. To enable the application of peripheral microsampling in planned paediatric studies, a comparison of the measured pharmacokinetic (PK) exposure via peripheral blood collection (via microsampling) to venous collection will also be performed in this study.

Publications & conference data

2 peer-reviewed publications reference this trial (live from Europe PMC):

1. Population Pharmacokinetics of Tafenoquine, a Novel Antimalarial.
   Thakkar N, Green JA, Koh GCKW, Duparc S, et al · · 2018 · cited 20× · PMID 30201820 · DOI 10.1128/aac.00711-18
2. Application of the Stable Isotope Label Approach in Clinical Development-Supporting Dissolution Specifications for a Commercial Tablet Product with Tafenoquine, a Long Half-life Compound.
   Goyal N, Mohamed K, Rolfe K, Sahota S, et al · · 2018 · cited 1× · PMID 29869298 · DOI 10.1208/s12248-018-0234-5