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177Lu-PSMA
177Lu-PSMA is a radioligand therapy that delivers lutetium-177, a beta-emitting radioisotope, directly to prostate-specific membrane antigen (PSMA) on cancer cells, causing targeted cell death.
177Lu-PSMA is a radioligand therapy that delivers lutetium-177, a beta-emitting radioisotope, directly to prostate-specific membrane antigen (PSMA) on cancer cells, causing targeted cell death. Used for Metastatic castration-resistant prostate cancer (mCRPC) with PSMA expression.
At a glance
| Generic name | 177Lu-PSMA |
|---|---|
| Sponsor | Istituto Romagnolo per lo Studio dei Tumori Dino Amadori IRST S.r.l. IRCCS |
| Drug class | Radioligand therapy |
| Target | PSMA (prostate-specific membrane antigen) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 2 |
Mechanism of action
The drug consists of lutetium-177 (a therapeutic radioisotope) conjugated to a ligand that binds with high affinity to PSMA, a transmembrane protein overexpressed on prostate cancer cells. Once bound, the radioisotope delivers localized radiation to kill cancer cells while minimizing exposure to healthy tissue. This targeted approach is particularly effective in metastatic castration-resistant prostate cancer.
Approved indications
- Metastatic castration-resistant prostate cancer (mCRPC) with PSMA expression
Common side effects
- Hematologic toxicity (anemia, thrombocytopenia, leukopenia)
- Xerostomia (dry mouth)
- Nausea
- Fatigue
- Kidney 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)
- An Open-label Study Comparing Lutetium (177Lu) Vipivotide Tetraxetan Versus Observation in PSMA Positive OMPC. (PHASE3)
- 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)
- 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 Study to Learn How Safe the Study Treatment Actinium-225-macropa-pelgifatamab (BAY3546828) is, How it Affects the Body, How it Moves Into, Through and Out of the Body, and About Its Anticancer Activity in Participants With Advanced Metastatic Castration-resistant Prostate Cancer (mCRPC) (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- 177Lu-PSMA CI brief — competitive landscape report
- 177Lu-PSMA updates RSS · CI watch RSS
- Istituto Romagnolo per lo Studio dei Tumori Dino Amadori IRST S.r.l. IRCCS portfolio CI