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Updated: Dec 26, 2025

An Immunohistopathologic Study to Profile the Folate Receptor Beta Macrophage and Vascular Immune Microenvironment in Giant Cell Arteritis
Published on: February 8, 2019
Exploiting the folate receptor α in oncology
Mariana Scaranti1,2, Elena Cojocaru1,2, Susana Banerjee1,2
1The Institute of Cancer Research, London, UK.
Abstract:
Folate receptor α (FRα) came into focus as an anticancer target many decades after the successful development of drugs targeting intracellular folate metabolism, such as methotrexate and pemetrexed. Binding to FRα is one of several methods by which folate is taken up by cells; however, this receptor is an attractive anticancer drug target owing to the overexpression of FRα in a range of solid tumours, including ovarian, lung and breast cancers. Furthermore, using FRα to better localize effective anticancer therapies to their target tumours using platforms such as antibody-drug conjugates, small-molecule drug conjugates, radioimmunoconjugates and, more recently, chimeric antigen receptor T cells could further improve the outcomes of patients with FRα-overexpressing cancers. FRα can also be harnessed for predictive biomarker research. Moreover, imaging FRα radiologically or in real time during surgery can lead to improved functional imaging and surgical outcomes, respectively. In this Review, we describe the current status of research into FRα in cancer, including data from several late-phase clinical trials involving FRα-targeted therapies, and the use of new technologies to develop FRα-targeted agents with improved therapeutic indices.
Insights
Folate receptor alpha (FRα) is a promising anticancer target due to its overexpression in solid tumors. FRα-targeted therapies and imaging show potential for improved cancer treatment and patient outcomes.
Area of Science:
- Oncology
- Molecular Biology
- Drug Development
Background:
- Folate receptor alpha (FRα) is overexpressed in various solid tumors, including ovarian, lung, and breast cancers.
- FRα-mediated folate uptake is a key cellular process exploited by cancer cells.
- Traditional intracellular folate metabolism drugs exist, but FRα presents a distinct targeting opportunity.
Purpose of the Study:
- To review the current research status of folate receptor alpha (FRα) in oncology.
- To discuss the potential of FRα-targeted therapies and diagnostic tools in cancer treatment.
- To highlight advancements in developing novel FRα-targeting agents.
Main Methods:
- Review of existing literature and clinical trial data on FRα-targeted therapies.
- Analysis of FRα's role in cancer cell uptake and its potential as a drug target.
- Examination of emerging technologies for FRα-based drug delivery and imaging.
Main Results:
- FRα overexpression in solid tumors makes it an attractive target for anticancer drugs.
- Various platforms like antibody-drug conjugates and CAR T-cells are being developed to target FRα.
- FRα also serves as a predictive biomarker and can be used for improved imaging and surgical guidance.
Conclusions:
- FRα-targeted therapies, including those in late-phase clinical trials, hold significant promise for improving outcomes in FRα-overexpressing cancers.
- New technologies are enabling the development of FRα-targeted agents with enhanced therapeutic indices.
- The multifaceted role of FRα in cancer necessitates continued research for optimized therapeutic and diagnostic strategies.
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