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177Lu-PSMA-617 + androgen receptor-directed therapy + androgen deprivation therapy
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous (for 177Lu-PSMA-617)[1][3], Oral (for Most Androgen Receptor-directed Therapies)[4][6], Intramuscular Or Subcutaneous (for Some GnRH Agonists/antagonists)[8], Surgical (orchiectomy As A Form Of Androgen Deprivation Therapy)[8]
01
Overview
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].
- Brand names
- None known for the combination itself
- Other names
- None known for the combination itself
02
Targets
AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)PSMA (Prostate-specific membrane antigen)
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