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N,N-Diethyl-2-(2-(4-(2[(18)F]-Fluoroethoxy)Phenyl)5,7Dimethylpyrazolo[1,5A]Pyrimidin-3-Yl)Acetamide

This article explores the use of [18F]DPA-714, a novel radiotracer, in clinical trials for imaging neuroinflammation and various brain disorders. [18F]DPA-714 is being investigated as a tool to visualize and measure microglial activation, which plays a crucial role in neuroinflammation. The trials discussed here cover a range of conditions, including schizophrenia, multiple sclerosis, Alzheimer’s disease, and epilepsy, highlighting the potential of this imaging technique to advance our understanding and treatment of neurological and psychiatric disorders.

Table of Contents

Introduction

[18F]DPA-714 is an innovative radiotracer being studied for its potential to help diagnose and monitor various brain conditions. This article will explain what [18F]DPA-714 is, how it works, and what researchers hope to learn from using it in brain imaging studies.

What is [18F]DPA-714?

N,N-DIETHYL-2-(2-(4-(2[(18)F]-FLUOROETHOXY)PHENYL)5,7DIMETHYLPYRAZOLO[1,5A]PYRIMIDIN-3-YL)ACETAMIDE, also known as [18F]DPA-714, is a radioactive substance used in a type of medical imaging called Positron Emission Tomography (PET)[1]. It’s specifically designed to help visualize inflammation in the brain.

How [18F]DPA-714 Works

[18F]DPA-714 works by binding to a protein called TSPO (translocator protein), which is found in higher amounts in areas of brain inflammation[1]. When injected into the body, it travels to the brain and attaches to these proteins. The radioactive element (18F) in the compound allows special cameras to detect where it has accumulated, creating detailed images of inflammation in the brain.

Medical Conditions Studied

Researchers are investigating the use of [18F]DPA-714 in several neurological conditions, including:

  • Schizophrenia: To study brain inflammation in patients with this mental disorder[1]
  • Multiple Sclerosis (MS): To examine neuroinflammation in patients with MS[2]
  • Alzheimer’s Disease: To investigate the relationship between brain inflammation, tau protein accumulation, and synaptic density[3]
  • Epilepsy: To help locate the source of seizures in patients with drug-resistant epilepsy[4]
  • Stroke: To study inflammation in the brain and carotid arteries after a stroke or transient ischemic attack[5]

Potential Benefits

The use of [18F]DPA-714 in PET imaging may offer several potential benefits:

  • More accurate diagnosis of neurological conditions
  • Better understanding of disease progression
  • Improved planning for treatments like epilepsy surgery
  • Ability to monitor the effectiveness of treatments targeting brain inflammation

How [18F]DPA-714 is Administered

[18F]DPA-714 is given as an intravenous injection, which means it’s injected directly into a vein[4]. The dose is typically measured in MBq (megabecquerels), a unit used to measure radioactivity. After injection, patients undergo PET scanning, often combined with MRI (Magnetic Resonance Imaging) for more detailed pictures.

Possible Side Effects

As [18F]DPA-714 is still being studied, all potential side effects may not be known. However, the following precautions are typically taken:

  • Patients with severe kidney problems may be excluded from studies[1]
  • Pregnant or breastfeeding women are usually not eligible for studies using this tracer[4]
  • The radiation exposure is generally considered low and safe for research purposes

Ongoing Research

Several clinical trials are currently underway to further investigate the use of [18F]DPA-714:

  • A study examining microglial activation in schizophrenia patients[1]
  • Research on neuroinflammation in multiple sclerosis[2]
  • An investigation into the relationship between inflammation, tau pathology, and synaptic density in Alzheimer’s disease[3]
  • A study to improve localization of epileptic foci in drug-resistant epilepsy[4]
  • Research on brain inflammation in stroke patients[5]

Conclusion

[18F]DPA-714 is a promising tool for visualizing brain inflammation in various neurological conditions. While still in the research phase, it has the potential to improve diagnosis, treatment planning, and our understanding of how these diseases affect the brain. As studies continue, we may learn more about its effectiveness and safety in clinical use.

Study Focus Condition Key Objectives Participants
Microglial activation in schizophrenia Schizophrenia Assess correlation between cortical neuroinflammation and C4 expression Schizophrenia patients and healthy volunteers
Neuroinflammation in carotid stenosis Stroke or transient ischemic attack Evaluate association between ficolin-2 levels and carotid/brain inflammation Patients with carotid stenosis
Neuroinflammation in multiple sclerosis Multiple sclerosis Quantify smoldering component of white matter lesions MS patients and healthy controls
Microglial activation in Alzheimer’s disease Alzheimer’s disease Analyze interplay between microglial activation, tau pathology, and synaptic density AD patients and healthy volunteers
Neuroinflammation in epilepsy Drug-resistant epilepsy Evaluate contribution of [18F]DPA-714 PET in locating seizure zones Epilepsy patients and healthy volunteers

FAQ

  • What is [18F]DPA-714 and how is it used in clinical trials? [18F]DPA-714 is a radiotracer used in Positron Emission Tomography (PET) imaging to visualize and measure neuroinflammation in the brain. In clinical trials, it is injected into patients to help researchers study microglial activation in various brain disorders.
  • What conditions are being studied using [18F]DPA-714? Clinical trials are using [18F]DPA-714 to study a variety of conditions, including schizophrenia, multiple sclerosis, Alzheimer's disease, epilepsy, and the neurological effects of COVID-19.
  • How does [18F]DPA-714 imaging work? [18F]DPA-714 binds to a protein called TSPO, which is expressed on activated microglia in the brain. When the radiotracer is injected, it can be detected using PET scans, allowing researchers to visualize and measure the level of neuroinflammation in specific brain regions.
  • Are there any risks associated with [18F]DPA-714 imaging? While [18F]DPA-714 imaging involves exposure to a small amount of radiation, the risks are generally considered low. However, pregnant or breastfeeding women are typically excluded from these studies as a precaution.
  • What are the potential benefits of [18F]DPA-714 imaging research? Research using [18F]DPA-714 imaging may lead to better understanding of neuroinflammation in various brain disorders, potentially improving diagnosis, treatment selection, and monitoring of disease progression. It could also help in developing new therapies targeting neuroinflammation.

Ongoing Clinical Trials on N,N-Diethyl-2-(2-(4-(2[(18)F]-Fluoroethoxy)Phenyl)5,7Dimethylpyrazolo[1,5A]Pyrimidin-3-Yl)Acetamide

  • Study on Brain Inflammation in Schizophrenia Patients Using 18F-DPA-714

    Recruiting

    4 1 1
    Investigated diseases:
    Investigated drugs:
    France

  • Study of [18F]-DPA-714 PET imaging to assess neuroinflammation in multiple sclerosis patients compared to healthy controls

    Recruiting

    4 1 1
    Investigated drugs:
    France

  • Evaluation of 18F-DPA-714 PET-MRI imaging for locating epileptic focus in patients with drug-resistant partial epilepsy before surgery

    Recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    France

  • Study of microglial activation and synaptic density using [18F]-DPA-714, [18F]-Ro948, [11C]-UCB-J, and [11C]PiB PET imaging in patients with Alzheimer’s disease

    Not recruiting

    2 1 1
    Investigated diseases:
    Investigated drugs:
    France

  • Study on the Effects of Dexmedetomidine on Neuroinflammation in COVID-19 ARDS Survivors

    Not recruiting

    3 1 1 1
    Investigated diseases:
    Investigated drugs:
    France

  • Study on Brain Inflammation in Stroke Patients Using Ficolin-2, Gadoteric Acid, and 18F-DPA-714

    Not recruiting

    2 1 1 1
    Investigated diseases:
    Investigated drugs:
    France

Glossary

  • PET: Positron Emission Tomography, an imaging technique that uses radioactive tracers to visualize and measure metabolic processes in the body.
  • Neuroinflammation: Inflammatory responses within the brain or spinal cord, often involving activation of immune cells like microglia.
  • Microglia: Immune cells in the central nervous system that respond to injury or disease by becoming activated.
  • TSPO: Translocator Protein, a marker of microglial activation that is targeted by [18F]DPA-714.
  • Radiotracer: A radioactive substance used in medical imaging to visualize specific biological processes or structures.
  • Schizophrenia: A complex mental disorder characterized by distortions in thinking, perception, emotions, language, sense of self, and behavior.
  • Multiple Sclerosis (MS): A chronic disease affecting the central nervous system, where the immune system attacks the protective covering of nerve fibers.
  • Alzheimer's Disease: A progressive brain disorder that slowly destroys memory and thinking skills, eventually affecting the ability to carry out simple tasks.
  • Epilepsy: A neurological disorder characterized by recurrent seizures, which are sudden, uncontrolled electrical disturbances in the brain.
  • ARDS: Acute Respiratory Distress Syndrome, a serious lung condition that causes low blood oxygen levels.
  • SUV: Standardized Uptake Value, a measure used in PET imaging to quantify the concentration of radiotracer in a specific region.
  • DVR: Distribution Volume Ratio, a measure used in PET imaging to quantify the binding of a radiotracer in tissue relative to a reference region.
  • MRI: Magnetic Resonance Imaging, a non-invasive imaging technique that uses magnetic fields and radio waves to create detailed images of the body's internal structures.

References

  1. http://clinicaltrials.eu/trial-id/2023-504181-38-00
  2. http://clinicaltrials.eu/trial-id/2023-510304-53-00
  3. http://clinicaltrials.eu/trial-id/2024-516566-11-00
  4. http://clinicaltrials.eu/trial-id/2024-517638-16-00
  5. http://clinicaltrials.eu/trial/study-on-brain-inflammation-in-stroke-patients-using-ficolin-2-gadoteric-acid-and-18f-dpa-714/