Folate-based radiotracers for PET imaging--update and perspectives

Area of Science:

• Nuclear medicine
• Radiochemistry
• Oncology

Background:

• Folate receptor (FR) is overexpressed in various cancers, including ovarian and lung cancer.
• Folic acid's high affinity for FR enables targeted delivery of diagnostic or therapeutic agents to tumors.
• Accurate identification of FR-positive tumors is crucial for patient selection in FR-targeted therapies.

Purpose of the Study:

• To review the design, preparation, and preclinical evaluation of folate derivatives for PET radiolabeling.
• To discuss the application of these folate-based PET tracers for imaging FR-positive malignancies.
• To highlight advancements in PET imaging for patient stratification in FR-targeted treatment strategies.

Main Methods:

• Review of literature on folate derivatives synthesis and radiolabeling for PET.
• Preclinical investigation of novel folate-based radiotracers.
• Discussion of established and emerging PET radioisotopes (e.g., 18F, 68Ga, 152Tb, 44Sc) for folate tracers.

Main Results:

• Folate derivatives have been successfully developed and radiolabeled for PET imaging.
• PET imaging offers superior resolution and sensitivity for detecting FR-positive tumors compared to SPECT.
• Emerging PET isotopes like 152Tb and 44Sc show potential for improved imaging characteristics.

Conclusions:

• Folate-based PET tracers are valuable tools for identifying FR-positive cancers.
• These tracers facilitate patient selection for FR-targeted therapies, improving treatment outcomes.
• Ongoing research into novel folate PET agents promises expanded clinical applications.