A Phase I/II, Open-label, Multi-center Study of [225Ac]Ac-PSMA-R2 in Men With PSMA-positive Prostate Cancer With or Without Prior 177Lu-PSMA Radioligand Therapy.

• Status: Recruiting
• Trial end date: 2026-08-28
• Target enrollment: 0
• Participant gender: Male

Summary

The purpose of the study is to characterize the safety, tolerability, pharmacokinetics (PK), and anti-tumor activity of 225Ac-PSMA-R2 in male adult participants with metastatic castration-resistant prostate cancer (mCRPC) previously treated with androgen receptor pathway inhibitors in post-177Lu and pre-177Lu settings.

• Phase: Phase 1/Phase 2
• Accepts Healthy Volunteers?: No

Details

• Lead Sponsor: Novartis Pharmaceuticals
• Treatments: Gallium 68 PSMA-11

Criteria

Key Inclusion Criteria:

• Evidence of PSMA-positive disease by 68Ga-PSMA-R2 PET/CT and eligible as determined by central reading

• Documented progressive mCRPC

• Adequate organ function (bone marrow reserve, hepatic, renal)

• Prior orchiectomy and/or ongoing ARPI and taxane-based chemotherapy and should have received prior 177Lu-PSMA-RLT (Group1 dose escalation & expansion) or never received 177Lu-PSMA-RLT (Group 2 dose escalation & expansion).

Key Exclusion Criteria:

• Any other investigational agents within 28 days of the anticipated C1D1 of 225Ac-PSMA-R2 therapy

• Any systemic anti-cancer therapy within 28 days of the anticipated C1D1 of 225Ac-PSMA-R2 therapy

• Uncontrolled pain or incompatibility that may result in participant's lack of ability to comply with imaging procedures

• History of CNS metastases and symptomatic cord compression, or clinical or radiologic findings indicative of impending cord compression

• Uncontrolled cardiovascular history

• Diagnosis of other malignancies expected to alter life expectancy or may interfere with disease assessment

Other protocol-defined inclusion/exclusion criteria may apply.