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radium-223 + lutetium-177 PSMA-I&T
- Development stage
- Unknown
- Lead developer
- Peter MacCallum Cancer Centre
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Radium-223 + lutetium-177 PSMA-I&T is an investigational radiopharmaceutical combination under evaluation for the treatment of metastatic castration-resistant prostate cancer (mCRPC)[1][3][5][7]. Radium-223 is an alpha-emitting radionuclide that selectively targets areas of increased bone turnover, delivering cytotoxic radiation to bone metastases. Lutetium-177 PSMA-I&T is a small-molecule radioligand that binds to prostate-specific membrane antigen (PSMA), allowing targeted beta-radiation to PSMA-expressing tumor cells[2][3][4][6]. The mechanism involves dual targeting: radium-223 delivers alpha radiation to micrometastatic osseous disease, while lutetium-177 PSMA-I&T delivers beta radiation to PSMA-positive lesions throughout the body[3]. The rationale is to improve efficacy against bone and soft tissue metastases, with non-overlapping biodistribution and clearance routes (radium-223 is cleared fecally, lutetium-177 PSMA-I&T is cleared renally)[3]. The combination aims to maximize tumor cell death, especially in micro-metastatic bone sites, and overcome the limitations of single-agent radiopharmaceutical approaches.
- Other names
- 223Ra + 177Lu-PSMA-I&T
02
Targets
PSMA (Prostate-specific membrane antigen)
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