Two decades of [¹¹C]PiB synthesis, 2003-2023: a review

Because carbon-11 (¹¹C) radiotracers cannot be shipped over long distances, their use in routine positron emission tomography (PET) studies is dependent on the production capabilities of individual radiochemistry laboratories. Since 2003, ¹¹C-labeled Pittsburgh compound B ([¹¹C]PiB) has been the gold standard PET radiotracer for in vivo imaging of amyloid β (Aβ) plaques. For more than two decades, researchers have been working to develop faster, higher-yielding, more robust, and optimized production methods with higher radiochemical yields for various imaging applications. This review evaluates progress in [¹¹C]PiB radiochemistry. An introductory overview assesses how it has been applied in clinical neurologic imaging research. We examine the varying approaches reported for radiolabeling, purification, extraction, and formulation. Further considerations for QC methods, regulatory considerations, and optimizations were also discussed.