NCT03239522

Absorption and Elimination of Radiolabeled Daprodustat

An Open-label Study in Healthy Male Participants to Determine the Mass Balance, Absolute Bioavailability and Pharmacokinetics of Daprodustat, Administered as a Single Intravenous Microtracer (Concomitant With an Oral Dose of Non-radiolabelled Daprodustat) and a Single, Oral Radiolabelled Dose

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 6 (actual)
• Sponsor: GlaxoSmithKline · Industry
• Sex: Male
• Age: 30 Years – 55 Years
• Healthy volunteers: Accepted

Summary

Absorption, metabolism and excretion of daprodustat (GSK1278863) have been studied in previous clinical trials; however, the elimination routes and metabolic pathways of daprodustat have not been fully elucidated in humans. This is an open-label, single-center, non-randomized, 2-period, single-sequence, crossover, mass balance study in 6 healthy male participants. The aim of the study is to assess the excretion balance of daprodustat using \[14C\]-radiolabeled drug substance administered orally, and as an intravenous (IV) infusion, administered as a microtracer dose (concomitant with an oral, non-radiolabeled dose). Absolute bioavailability of an oral dose will also be assessed. Each participant will be involved in the study for up to 10 weeks which include a screening visit, two treatment periods (treatment periods 1 and 2), separated by about 7 days (at least 14 days between oral doses), and a follow up visit 1-2 weeks after the last assessment in treatment period 2. The primary objective of the study is to gain a better understanding of the compound's excretory and metabolic profile. This study will include sampling of duodenal bile to conduct qualitative assessment of drug metabolites in this matrix in order to characterize biliary elimination pathways.

Conditions

• Anaemia

Interventions

Type	Name	Description
DRUG	[14C]-GSK1278863 solution for IV infusion	It is a clear, colorless solution free from visible particulate matter. Participants will receive 10 mL of 5 µg/mL of \[14C\]-GSK1278863 IV solution (total dose: 50 µg) by IV infusion over 1 hour.
DRUG	[14C]-GSK1278863 oral solution	It is a clear, colorless solution. Participants will receive 125 mL of 200 µg/mL of \[14C\]-GSK1278863 oral solution (total dose: 25 mg).
DRUG	Daprodustat 6 mg oral tablet	It is a 9.0 millimeter (mm) round, white film coated tablet.

Timeline

• Start date: 2017-10-10
• Primary completion: 2017-11-28
• Completion: 2017-11-28
• First posted: 2017-08-04
• Last updated: 2019-12-03
• Results posted: 2019-03-18

Locations

1 site across 1 country: United Kingdom

Regulatory

• FDA-regulated drug study