[Strategy for development of imaging biomarkers]

Area of Science:

• Molecular imaging
• Radiopharmaceutical chemistry
• Neuroscience

Context:

• Imaging biomarkers are vital for assessing physiological functions, higher brain functions, and disease pathophysiology.
• Positron Emission Tomography (PET) and single-photon emission computed tomography are key molecular imaging modalities.
• Radiopharmaceuticals are essential for successful in vivo molecular imaging.

Purpose:

• To outline the comprehensive process of developing radioligands for central nervous system (CNS) studies.
• To detail the critical steps from biomarker selection to safety evaluation.
• To provide insights into the application of PET in both normal subjects and patient populations.

Summary:

• Radioligand development for PET imaging follows a structured process: biomarker and compound selection, synthesis optimization, in vitro/in vivo validation (imaging potential, selectivity, specificity, species differences), and safety assessments (toxicity, dosimetry).
• The manuscript details the author's experiences and concepts in developing radioligands specifically for CNS research.
• Clinical application involves initial studies in healthy individuals, followed by patient studies, with recent advancements including direct radiation dosimetry measurements.

Impact:

• Facilitates the development of novel diagnostic and therapeutic agents for neurological disorders.
• Enhances understanding of brain function and pathophysiology through advanced molecular imaging.
• Contributes to the advancement of personalized medicine in neurology by enabling targeted drug development and evaluation.