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99mTc-DMTHF-chelate is a technetium-99m labeled radiopharmaceutical imaging agent developed at Purdue University for the selective detection of folate receptor alpha (FR-α) positive tumors. The agent utilizes a reduced and alkylated folate derivative, N5, N10-dimethyl tetrahydrofolate (DMTHF), as its targeting ligand. Unlike conventional folate-based tracers that bind with high affinity to both FR-α (found on malignant cells) and FR-β (found on activated macrophages), 99mTc-DMTHF-chelate demonstrates high specificity for the alpha isoform. This selectivity enables the agent to distinguish cancer tissue from sites of inflammation, such as those associated with rheumatoid arthritis, atherosclerosis, or ulcerative colitis, which are characterized by the accumulation of FR-β expressing macrophages. Preclinical studies in KB cell lines and animal models have confirmed its ability to selectively image FR-α expressing tumors while avoiding uptake in inflammatory lesions.
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