Prospects in folate receptor-targeted radionuclide therapy

Area of Science:

• Oncology
• Radiopharmaceutical Therapy
• Molecular Imaging

Background:

• Targeted radionuclide therapy utilizes radiopharmaceuticals directed to tumor-specific targets for localized radiation delivery.
• Folate receptor (FR) is a promising target for various cancers due to restricted expression in healthy tissues.
• Folic acid's high binding affinity makes it an ideal targeting agent, but renal toxicity has limited therapeutic applications.

Purpose of the Study:

• To review recent developments in folate radioconjugate therapy for cancer.
• To explore novel folate radioconjugate designs and application protocols to overcome limitations.
• To assess the potential for clinical translation of FR-targeted radionuclide therapy.

Main Methods:

• Review of current literature on folate radioconjugates for therapy.
• Analysis of new folate radioconjugate constructs and their tissue distribution.
• Evaluation of preclinical therapy experiments using novel folate radioconjugates and pharmacological interactions.

Main Results:

• Folate receptor targeting is effective for various cancers like ovarian, lung, brain, renal, and colorectal.
• High accumulation in kidneys has been a major obstacle for therapeutic folate radioconjugates.
• New constructs and protocols have enabled initial preclinical therapy experiments with radiofolates.

Conclusions:

• Improved folate radioconjugate designs are crucial for safe and effective clinical application.
• Preclinical studies show promise for FR-targeted radionuclide therapy.
• Further research into optimized folate radioconjugates could lead to new cancer treatment options.