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A **combination regimen** comprised of the radioligand therapy **177Lu-PSMA-617**, which targets the *prostate-specific membrane antigen (PSMA)* on prostate cancer cells and delivers cytotoxic beta-particle radiation, plus **androgen receptor-directed therapy** (e.g., enzalutamide, abiraterone, apalutamide, darolutamide) and **androgen deprivation therapy** (e.g., GnRH agonists/antagonists or orchiectomy). This regimen is primarily investigated for advanced **prostate cancer**, especially **metastatic castration-resistant prostate cancer (mCRPC)**, with ongoing research in earlier stages. - **177Lu-PSMA-617** is a small molecule radiopharmaceutical that binds PSMA and delivers targeted radiation, sparing most normal cells[1][3]. - **Androgen receptor-directed therapies** are small molecules that antagonize or inhibit the androgen receptor, blocking androgen signaling and inhibiting prostate cancer growth[2][4][6]. - **Androgen deprivation therapy** decreases circulating androgen levels, depriving the tumor of ligand for the androgen receptor (by chemical or surgical castration)[6][8]. - The combination has shown enhanced anticancer activity and improved progression-free and overall survival in clinical trials[1][3][7].
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