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Updated: Jul 4, 2026
Surface-enhanced Resonance Raman Scattering Nanoprobe Ratiometry for Detecting Microscopic Ovarian Cancer via Folate Receptor Targeting
Published on: March 25, 2019
Tumor detection using folate receptor-targeted imaging agents
Emanuela I Sega1, Philip S Low
1Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA. esega@stanford.edu
Abstract:
Folate receptors are up-regulated on a variety of human cancers, including cancers of the breast, ovaries, endometrium, lungs, kidneys, colon, brain, and myeloid cells of hematopoietic origin. This over-expression of folate receptors (FR) on cancer tissues can be exploited to target folate-linked imaging and therapeutic agents specifically to FR-expressing tumors, thereby avoiding uptake by most healthy tissues that express few if any FR. Four folate-targeted therapeutic drugs are currently undergoing clinical trials, and several folate-linked chemotherapeutic agents are in late stage preclinical development. However, because not all cancers express FR, and because only FR-expressing cancers respond to FR-targeted therapies, FR-targeted imaging agents have been required to select patients with FR-expressing tumors likely to respond to folate-targeted therapies. This review focuses on recent advances in the use of the vitamin folic acid to target PET agents, gamma-emitters, MRI contrast agents and fluorescent dyes to FR(+) cancers for the purpose of diagnosing and imaging malignant masses with improved specificity and sensitivity.
Insights
Folate receptors (FR) are over-expressed in many cancers. Targeting these FR-expressing tumors with folic acid-linked imaging agents helps diagnose and treat cancers more effectively.
Area of Science:
- Oncology
- Molecular Imaging
- Drug Development
Background:
- Folate receptors (FR) are significantly over-expressed on various human cancers, including breast, ovarian, lung, and brain cancers.
- This specific expression pattern presents a unique opportunity for targeted cancer therapies and diagnostics.
- Most healthy tissues exhibit minimal FR expression, allowing for tumor-specific targeting.
Purpose of the Study:
- To review recent advancements in utilizing folic acid for targeting diagnostic and therapeutic agents to FR-expressing tumors.
- To highlight the application of folic acid in developing novel imaging agents for improved cancer detection.
- To discuss the role of FR-targeted imaging in patient selection for folate-targeted therapies.
Main Methods:
- Focuses on recent literature and research in the field of folate receptor-targeted oncology.
- Reviews the development and application of various imaging modalities, including PET, SPECT (gamma-emitters), MRI, and fluorescence imaging.
- Examines the use of folic acid as a targeting ligand for these imaging agents.
Main Results:
- Folic acid effectively targets imaging agents to FR-positive tumors, enhancing diagnostic specificity and sensitivity.
- Advancements include PET agents, gamma-emitters, MRI contrast agents, and fluorescent dyes for FR(+) cancer imaging.
- FR-targeted imaging is crucial for identifying patients who will benefit from FR-targeted therapies.
Conclusions:
- Folic acid-targeted imaging agents offer a promising strategy for the precise diagnosis and visualization of FR-expressing cancers.
- This approach improves the selection of patients for targeted therapies, maximizing treatment efficacy.
- Continued research in this area holds potential for significant improvements in cancer care.
