NCT06348355

A Positron-emission Tomography Study to Determine Brain Exposure of [11C]Savolitinib in Healthy Volunteers

A Phase I, Open-label, Positron-Emission Tomography Study to Determine Brain Exposure of [11C]Savolitinib in Healthy Volunteers

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 7 (actual)
• Sponsor: AstraZeneca · Industry
• Sex: All
• Age: 50 Years – 65 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to measure brain exposure of \[11C\]savolitinib in healthy volunteers. This study will determine brain exposure of \[11C\]savolitinib in up to 8 healthy volunteers under physiological conditions, ie, when the BBB is intact. The study design allows up to 3 site visits. Two PET examinations will be performed for each healthy volunteer. The first PET examination will use IV administration of \[11C\]savolitinib. The second PET examination using \[11C\]savolitinib will occur after a single oral dose of 300 mg of savolitinib. PET image analysis will include kinetic compartment modelling using arterial input function, and will generate a set of brain exposure parameters (eg, maximum %ID, maximum \[11C\]savolitinib concentration in brain, partition coefficients between brain and plasma).

Detailed description

This is a Phase I, open-label, non-randomised, single-centre study to determine brain distribution and exposure of \[11C\]savolitinib following IV bolus injections of a microdose in one cohort of healthy adult volunteers. The study is composed of the following parts: Visit 1: Screening: Screening, including brain MRI, within 45 days prior to PET imaging Visit 2: PET examination: Single microdose (≤ 10 μg) of \[11C\]savolitinib administered as an IV bolus at the start of PET imaging. Brain radioactivity measurements using PET/CT (radioactivity in brain) and radioactivity measurements in arterial blood (radioactivity in blood) will be taken over a maximum of 90 minutes. 300 mg savolitinib will be administered orally approximately 2 hours after the end of the first PET examination. The second microdose of \[11C\]savolitinib will be administered as IV bolus at approximately 2 hours after the oral administration of savolitinib, and a second PET examination will be conducted over 90 minutes. PET2 examination can be performed on a separate day, within 14 days after PET1, if it was not performed the same day due to technical/participant related reasons. Oral savolitinib will be given on the same day as the second PET examination. Visit 3: Follow-up: Telephone assessment 7 days (± 3 days) after receiving the last microdose of \[11C\]savolitinib and PET examination

Conditions

• Healthy Volunteers

Interventions

Type	Name	Description
DRUG	[11C]savolitinib	Radiopharmaceutical; IMP; Sterile solution for IV injection, not more than 10 μg, single administration
DRUG	Savolitinib	IMP; 300 mg tablet, oral single administration

Timeline

• Start date: 2024-04-12
• Primary completion: 2024-06-24
• Completion: 2024-06-24
• First posted: 2024-04-04
• Last updated: 2025-08-06

Locations

1 site across 1 country: Sweden