Perspectives of Methotrexate-Based Radioagents for Application in Nuclear Medicine.

Abstract

Methotrexate is a gold standard among disease modifying antirheumatic drugs and is also extensively used clinically in combination with oncological therapies. Thus, it is not surprising that nuclear medicine found an interest in methotrexate in the search for diagnostic and therapeutic solutions. Numerous folate-related radiopharmaceuticals have been proposed for nuclear medicine purposes; however, methotrexate radioagents represent only a minority. This imbalance results from the fact that methotrexate has significantly weaker affinity for folate receptors than folic acid. Nevertheless, radiolabeled methotrexate agents utilized as a tool for early detection and imaging of inflammation in rheumatoid arthritis patients gave promising results. Similarly, the use of multimodal MTX-release nanosystems may find potential applications in radiosynovectomy and theranostic approaches in folate receptor positive cancers.

• Authors: Paweł Krzysztof Halik, Przemysław Koźmiński, Ewa Gniazdowska
• Journal: Molecular pharmaceutics (Mol Pharm) Vol. 18 Issue 1 Pg. 33-43 (01 04 2021) ISSN: 1543-8392 [Electronic] United States
• PMID: 33251808 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antirheumatic Agents
• Folate Receptors, GPI-Anchored
• Radiopharmaceuticals
• Folic Acid
• Methotrexate

Topics

• Antirheumatic Agents (chemistry, therapeutic use)
• Arthritis, Rheumatoid (drug therapy, metabolism)
• Folate Receptors, GPI-Anchored (metabolism)
• Folic Acid (metabolism)
• Humans
• Methotrexate (chemistry, therapeutic use)
• Nuclear Medicine (methods)
• Radiopharmaceuticals (chemistry, therapeutic use)