NCT03809234

Pgp Transporter and CNS Biodistribution of Ondansetron in Healthy Volunteers

Effects of Pgp Transporter Inhibition on CNS Biodistribution of Ondansetron in Healthy Volunteers

• Status: Terminated
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 14 (actual)
• Sponsor: Washington University School of Medicine · Academic / Other
• Sex: All
• Age: 18 Years – 50 Years
• Healthy volunteers: Accepted

Summary

To determine the time-course of plasma and CSF concentrations of intravenous (IV) ondansetron in healthy subjects, with and without selective inhibition of Pgp efflux transporter.

Detailed description

The study hypothesis is that inhibition of Pgp efflux transporters will increase the CNS bio-distribution of the 5-HT3R antagonist ondansetron. Specifically: 1. Intravenous administration of ondansetron is expected to yield low CSF exposure. 2. Co-administration of ondansetron with intravenous tariquidar, an inhibitor of Pgp efflux transporters, will result in increased CSF exposure of ondansetron.

Conditions

• Neuropathic Pain

Interventions

Type	Name	Description
DRUG	Ondansetron 8mg with Saline & Tariquidar	Each participant will receive two IV infusions of ondansetron, 24 hours apart. In the first and second sessions, respectively, placebo (D5W) or tariquidar (4mg/kg dose in D5W) 22 will be administered IV over 60 minutes. Ondansetron will be diluted in 50mL 0.9% normal saline, and tariquidar will be diluted in 250mL D5W.
DRUG	Ondansetron 16mg with Saline & Tariquidar	Each participant will receive two IV infusions of ondansetron, 24 hours apart. In the first and second sessions, respectively, placebo (D5W) or tariquidar (4mg/kg dose in D5W) 22 will be administered IV over 60 minutes. Ondansetron will be diluted in 50mL 0.9% normal saline, and tariquidar will be diluted in 250mL D5W.

Timeline

• Start date: 2019-05-20
• Primary completion: 2020-11-30
• Completion: 2020-11-30
• First posted: 2019-01-18
• Last updated: 2022-04-07

Locations

1 site across 1 country: United States

Regulatory

• FDA-regulated drug study