trofolastat

Trofolastat is a small-molecule inhibitor of prostate-specific membrane antigen (PSMA), developed as a radiopharmaceutical imaging agent for the detection of prostate cancer. It is typically used in combination with the radioactive tracer technetium‑99m, forming Technetium (99mTc) trofolastat, which is administered as a single intravenous injection. The compound binds specifically to PSMA, a protein highly expressed on prostate cancer cells, enabling visualization of cancerous lesions using single photon emission computed tomography (SPECT). Trofolastat has demonstrated high sensitivity and specificity for detecting prostate cancer lesions and can be used to assess disease extent before treatment, detect recurrence in patients with rising PSA levels, and evaluate suitability for targeted therapies in metastatic cases[3][6][7]. The drug was originally developed by Molecular Insight Pharmaceuticals and Progenics Pharmaceuticals (now part of Lantheus Holdings), with recent regulatory approval under the brand name RoTecPSMA in the UK.

Brand names

RoTecPSMA

Other names

Technetium (99mTc) trofolastat