Recent Developments in Carbon-11 Chemistry and Applications for First-In-Human PET Studies

Area of Science:

• Radiochemistry
• Molecular Imaging
• Nuclear Medicine

Background:

• Positron emission tomography (PET) is a key molecular imaging technique utilizing radiolabeled molecules for in vivo studies.
• Carbon-11 (¹¹C) is a versatile radionuclide for PET tracer development, preserving molecular properties.
• The short half-life of ¹¹C necessitates on-site cyclotrons and presents synthetic challenges, driving innovation.

Purpose of the Study:

• To review recent advancements in carbon-11 (¹¹C) radiolabeling methodologies.
• To highlight novel ¹¹C building blocks and radiochemical transformations.
• To showcase PET tracers incorporating ¹¹C that have progressed to human studies.

Main Methods:

• Literature review focusing on publications from the past five years.
• Identification of new radiochemical transformations and building blocks for ¹¹C labeling.
• Analysis of PET tracers that have reached first-in-human clinical evaluation.

Main Results:

• Significant progress in developing novel ¹¹C radiolabeling strategies.
• Introduction of new ¹¹C-labeled building blocks enhancing synthetic versatility.
• Several new ¹¹C PET tracers have successfully advanced to initial human trials.

Conclusions:

• Recent innovations have expanded the synthetic scope of ¹¹C radiochemistry.
• These advancements facilitate broader application of ¹¹C PET imaging.
• The development of new tracers shows promise for improved in vivo molecular evaluation.