PET Study to Determine the Relationship Between Plasma Concentrations and Muscarinic Type 1 Receptor (M1AChR) Occupancy of PIPE-307 in Healthy Volunteers

A Phase 1, Open-label Study of PIPE-307 to Determine Muscarinic Type I Receptor (M1AChR) Occupancy Parameters by [11C] PIPE-307 PET Imaging in Healthy Volunteers

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04941781

Enrollment

Registered

2021-06-28

Start date

2021-09-01

Completion date

2021-11-10

Last updated

2022-10-05

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Multiple Sclerosis

Keywords

Multiple Sclerosis

Brief summary

This is a Phase 1, single-center, open-label, adaptive-design PET study to investigate the occupancy of brain muscarinic Type 1 receptors (M1AChR) by PIPE-307 in healthy volunteers.

Detailed description

This is a Phase 1, single-center, open-label, adaptive-design study to investigate the occupancy of brain M1AChR after a single oral dose of PIPE-307 in healthy volunteers by positron emission tomography (PET) using the radioligand \[11C\] PIPE-307. This study will have an adaptive design to adequately evaluate the relationship between PIPE-307 exposure and brain M1AChR occupancy.

Interventions

DRUGPIPE-307

Each dose cohort will receive a single oral dose of PIPE-307. Doses to be tested in subsequent cohorts will be determined by the analysis of the exposure from PK data and the PET scans with \[11C\] PIPE-307. Subjects will receive an intravenous dose of the radioligand \[11C\] PIPE-307 prior to PET imaging.

Study design

Allocation

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

25 Years to 65 Years

Healthy volunteers

Yes

Inclusion criteria

Key Criteria: * Normotensive male or female volunteers between 25-65 years old * Deemed healthy on the basis of a clinical history, physical examination, ECG, vital signs, and laboratory tests of blood and urine Key

Exclusion criteria

* Clinically relevant abnormal findings at the screening assessments * Clinically relevant abnormal medical history or concurrent medical condition * Acute or chronic illness * Contraindications to MRI, CT, PET, or arterial cannulation procedures * Significant exposure to research related radiation or other exposure (defined as ICRP category IIb or no more than 10 mSv) * Positive tests for hepatitis B surface antigen (HBsAg) & Hepatitis C virus (HCV) antibody, human immunodeficiency virus (HIV) antibody * Drug or alcohol abuse * Smoke more than 10 cigarettes daily * Loss of more than 400 mL blood * Vital signs or ECGs outside the acceptable range

Design outcomes

Primary

Measure	Time frame
M1AChR receptor occupancy as determined by regional total volume of distribution (VT) of [11C] PIPE-307 at 24 hours	24 hours

Countries

United Kingdom

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026