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177Lu-PSMA-617
177Lu-PSMA-617 is a radioligand that binds to prostate-specific membrane antigen (PSMA) on cancer cells and delivers targeted radiation therapy to kill PSMA-expressing tumors.
177Lu-PSMA-617 is a radioligand that binds to prostate-specific membrane antigen (PSMA) on cancer cells and delivers targeted radiation therapy to kill PSMA-expressing tumors. Used for Metastatic castration-resistant prostate cancer (mCRPC) with PSMA expression.
At a glance
| Generic name | 177Lu-PSMA-617 |
|---|---|
| Also known as | 177Lutetium -PSMA 617 also referred to as 177Lu-PSMA, Lutetium-177-PSMA-617, (177Lu)-PSMA-617, 177Lu-PSMA, [177Lu]Lu-PSMA-617 |
| Sponsor | European Organisation for Research and Treatment of Cancer - EORTC |
| Drug class | Radioligand therapy / Targeted radionuclide therapy |
| Target | PSMA (Prostate-Specific Membrane Antigen) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
This drug combines a lutetium-177 radioisotope with a small molecule ligand (617) that specifically targets PSMA, a cell-surface antigen highly expressed on prostate cancer cells. Once bound to PSMA, the radioisotope delivers localized beta radiation directly to tumor cells, causing DNA damage and cell death while minimizing exposure to healthy tissues. This approach is known as radioligand therapy or targeted radionuclide therapy.
Approved indications
- Metastatic castration-resistant prostate cancer (mCRPC) with PSMA expression
Common side effects
- Hematologic toxicity (anemia, thrombocytopenia, leukopenia)
- Xerostomia (dry mouth)
- Nausea
- Fatigue
- Renal toxicity
Key clinical trials
- 177 LuPSMA-617 vs Docetaxel in Metastatic Castration Resistant and PSMA-Positive Prostate Cancer (PHASE2)
- Low PSMA SUV Boost (LPS-Boost): Intensified 177Lu-PSMA-617 Treatment for Patients With Metastatic Castrate-Resistant Prostate Cancer With Low PSMA Expressing Disease (PHASE2)
- Open-label Study Comparing AAA817 Versus Standard of Care in the Treatment of Previously Treated PSMA-positive mCRPC Adults Who Have Disease Progressed on or After [177Lu]Lu-PSMA Targeted Therapy (PHASE2, PHASE3)
- Neoadjuvant Lu-177-PSMA-617 in Patients With High Risk Localized Prostate Cancer Undergoing Radical Prostatectomy (PHASE2)
- 177Lu-PSMA-617 vs. Androgen Receptor-Directed Therapy in the Treatment of Progressive Metastatic Castrate Resistant Prostate Cancer (PHASE3)
- 177Lu-PSMA-617 With Liver Directed Therapy in Metastatic Castration Resistant Prostate Cancer (PHASE1)
- A Study Evaluating [177Lu]Lu-PSMA-617 vs. a Change of Androgen Receptor-directed Therapy in Taxane Treatment Naive Chinese Male Patients With Progressive Metastatic Castrate Resistant Prostate Cancer (PHASE2)
- A Real-world Study of Characteristics, Treatment Patterns, and Clinical Outcomes Among Lutetium-177 Vipivotide Tetraxetan Treated Patients
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |