[18F]SF12051 for Imaging the 18-kDa Translocator Protein (TSPO) in Brain and Whole Body of Healthy Subjects

NCT05564429 | Terminated Phase 1 Results FDA Drug

• 2 other identifiers: 10000674000674-M
• Study Type: interventional
• Target: 10
• Locations: 1 country
• Sites: 1

Brief Summary

Background: Inflammation in the brain plays a role in many diseases. Being able to measure inflammation in a person's brain might help to diagnose and treat these diseases. One protein (TSPO) appears in higher numbers when inflammation affects the brain. To see TSPO when a person's body is scanned, researchers need a substance called a radiotracer that will attach to this protein and no other molecules. Objective: This study will test whether a new radiotracer (\[18F\]SF12051) can make TSPO appear on PET scans of a person's brain and body. Eligibility: Healthy people aged 18 and older. Design: This study requires 2 to 4 visits to the clinic. All participants will be screened. They will have a physical exam. They will have blood tests and a test of their heart function. Some participants will have a positron emission tomography (PET) scan of the whole body. The radiotracer will be injected through a tube (catheter) placed in a vein in the arm. The PET scanner is a machine shaped like a doughnut. Participants will lie on a bed that slides in and out of the scanner. The scan will take about 2 hours. Some participants will have a PET scan of just their head. After they are injected with the radiotracer, they will lie on a bed with their head in the scanner. Blood will be drawn from a catheter in the wrist during the scan. Some participants will have a magnetic resonance imaging (MRI) scan of the brain. They will lie on a narrow bed that slides into a tube.

Conditions

Healthy

Keywords

PET Imaging; Neuroinflammation; Tspo

Outcome Measures

Primary Outcomes (3)

• Whole Body PET Uptake of [18F]SF12051 - Phase 1

  Participant received whole body PET scan and Uptake of \[18F\]SF12051 was measured using the Siemens Biograph mCT. Organ dosimetry was measured as microsieverts per mega-becquerel (uSv/MBq).

  Up to 120 minutes during the scan

• Brain PET Uptake of [18F]SF12051 - Phase 2

  Participant received brain PET scan and Uptake of \[18F\]SF12051 was measured using the Siemens Biograph mCT. Volume of distribution (Vt) was calculated via 2-Tissue-Compartment Model with plasma input function.

  Up to 120 minutes during the scan

• Whole Body PET Uptake of [18F]SF12051 - Phase 3

  Participant received whole body PET scan and Uptake of \[18F\]SF12051 was measured using the Siemens Biograph mCT. Organ dosimetry was measured as microsieverts per mega-becquerel (uSv/MBq).

  Up to 120 minutes during the scan

Secondary Outcomes (4)

• Area Under the Organ Time-Activity Curves From 0-120 - Phase 1

  Up to 120 minutes during the scan

• Area Under the Organ Time-Activity Curves From 0-120 - Phase 3

  Up to 120 minutes during the scan

• Test-Retest Variability of [18F]SF12051

  Up to 120 minutes during the scan

• Test-Retest Reliability of [18F]SF12051

  Up to 120 minutes during the scan

Study Arms (3)

High affinity binder (HAB) Translocator Protein (TSPO) genotype

EXPERIMENTAL

Healthy participants with HAB TSPO genotype receive 18F-SF12051 intravenously followed by whole body or brain positron emission tomography (PET) scan. Participants were randomized to either phase 1, 2, or 3. Phases 1 \& 3 had whole body PET scan and phase 2 had brain PET scan.

Drug: 18F-SF12051

Low affinity binder (LAB) Translocator Protein (TSPO) genotype

EXPERIMENTAL

Healthy participants with LAB TSPO genotype receive 18F-SF12051 intravenously followed by whole body or brain positron emission tomography (PET) scan. Participants were randomized to either phase 1, 2, or 3. Phases 1 \& 3 had whole body PET scan and phase 2 had brain PET scan.

Drug: 18F-SF12051

Mixed affinity binder (MAB) Translocator Protein (TSPO) genotype

EXPERIMENTAL

Healthy participants with MAB TSPO genotype receive 18F-SF12051 intravenously followed by whole body or brain positron emission tomography (PET) scan. Participants were randomized to either phase 1, 2, or 3. Phases 1 \& 3 had whole body PET scan and phase 2 had brain PET scan.

Drug: 18F-SF12051

Interventions

18F-SF12051 DRUG

Injected intravenously followed by PET scanning

High affinity binder (HAB) Translocator Protein (TSPO) genotype; Low affinity binder (LAB) Translocator Protein (TSPO) genotype; Mixed affinity binder (MAB) Translocator Protein (TSPO) genotype

Eligibility Criteria

• Age: 18 Years - 99 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• To be eligible to participate in this study, an individual must meet all of the following criteria:
• Aged 18 years or older.
• Healthy based on medical history, physical examination, and laboratory testing.
• Able to provide informed consent.
• Willing and able to complete all study procedures.
• Have been screened for TSPO genotype under 01-M-0254 "The Evaluation of Patients with Mood and Anxiety Disorders and Healthy Participants".
• Have their radial artery pulse checked for the presence of adequate ulnar collateral flow and the absence of any metal or foreign objects in both wrists\*.
• Agree to adhere to the lifestyle considerations
• Does not apply to Phase 1 and 3 participants as they will not have an arterial line.

You may not qualify if:

• An individual who meets any of the following criteria will be excluded from participation in this study:
• Clinically significant abnormalities on EKG or laboratory testing. This includes CBC; acute care panel (Na, K, Cl, CO2, creatinine, glucose, urea nitrogen); hepatic panel (alkaline phosphatase, ALT, AST, bilirubin total, and bilirubin direct); mineral panel (albumin, calcium, magnesium, phosphorus); prothrombin and partial prothrombin tests.
• Participants should not have taken NSAIDs or willow bark tea for two weeks prior to the PET scan.
• Any current Axis I diagnosis.
• Positive test for HIV.
• Unable to have an MRI scan\*.
• History of neurologic illness or injury with the potential to affect study data interpretation.
• History of seizures, other than in childhood and related to fever.
• Recent exposure to radiation (i.e., PET from other research) which when combined with this study would be above the allowable limits.
• Inability to lie flat on camera bed for at least two hours, including claustrophobia and weight greater than the maximum for the scanner (500 lbs).
• Pregnancy or breast feeding.
• Able to get pregnant but does not use birth control.
• Unable to travel to NIH.
• National Institute of Mental Health (NIMH) staff or an NIH employee who is a subordinate/relative/co-worker of the investigators.
• Phase 1 and 3 participants will not get an MRI.

Sponsors & Collaborators

• National Institute of Mental Health (NIMH): lead

Study Sites (1)

National Institutes of Health Clinical Center

Bethesda, Maryland, 20892, United States

Location

Related Publications (1)

• Yan X, Simeon FG, Liow JS, Morse CL, Jana S, Montero Santamaria JA, Jenkins M, Zoghbi SS, Pike VW, Innis RB, Zanotti-Fregonara P. [18F]SF51, a novel 18F-labeled PET radioligand for translocator protein 18kDa (TSPO) in brain, works well in monkeys but fails in humans. J Cereb Blood Flow Metab. 2025 Feb;45(2):365-372. doi: 10.1177/0271678X241304924. Epub 2024 Dec 9.

  PMID: 39654356 DERIVED

Related Links

• NIH Clinical Center Detailed Web Page

MeSH Terms

Conditions

Neuroinflammatory Diseases

Condition Hierarchy (Ancestors)

Nervous System Diseases; Inflammation; Pathologic Processes; Pathological Conditions, Signs and Symptoms

Results Point of Contact

• Title: Dr Robert Innis
• Organization: National Institute of Mental Health (NIMH)

robert.innis@nih.gov

301-594-1368

Study Officials

• Robert B Innis, M.D.

  National Institute of Mental Health (NIMH)

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: DIAGNOSTIC
• Intervention Model: PARALLEL
• Sponsor Type: NIH
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 29, 2022
• First Posted: October 3, 2022
• Study Start: February 2, 2023
• Primary Completion: May 9, 2023
• Study Completion: January 30, 2024
• Last Updated: July 9, 2024
• Results First Posted: July 9, 2024

Record last verified: 2024-01

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL
• Time Frame: 18 months after closure of protocol
• Access Criteria: BTRIS

Locations

US (1)