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Technetium (99mTc) trofolastat (99mTc-MIP-1404) is a small-molecule radiopharmaceutical diagnostic imaging agent designed for the detection and staging of prostate cancer using SPECT/CT. It consists of a glutamate-urea-lysine binding motif that targets the extracellular enzymatic domain of Prostate-Specific Membrane Antigen (PSMA), which is highly overexpressed in approximately 95% of prostate cancer cells. The molecule utilizes proprietary Single Amino Acid Chelate (SAAC) technology to bind the technetium-99m radioisotope. Following intravenous administration, the tracer selectively concentrates in PSMA-positive primary and metastatic prostate cancer lesions, allowing for high-contrast visualization 3–6 hours post-injection. It has been evaluated in Phase 3 clinical trials for the detection of prostate cancer in men with high-risk disease scheduled for prostatectomy and for the localization of recurrence in patients with biochemical failure.
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