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ART-101 is an investigational, lipophilic, prostate-specific membrane antigen-targeting small-molecule radioligand platform developed for prostate cancer. Radiolabeled ART-101 binds PSMA on prostate cancer cells and is designed to support theranostic use: indium-111-labeled ART-101 is being evaluated for first-in-human imaging and pharmacology assessment, while therapeutic versions have been studied with lutetium-177, actinium-225, and terbium-161. Preclinical studies report prolonged tumor retention, increased tumor radiation dose, and lower normal-tissue and salivary-gland uptake relative to PSMA-617; Archeus Technologies is conducting a Phase 1 study in metastatic castration-resistant prostate cancer. ([archeustech.com](https://www.archeustech.com/resources/archeus-technologies-doses-first-patient-with-art-101-in-phase-1-prostate-cancer-study))
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