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lutetium (177Lu) rosopatamab tetraxetan + abiraterone
- Development stage
- Unknown
- Lead developer
- Telix Pharmaceuticals
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
This combination therapy comprises **lutetium (177Lu) rosopatamab tetraxetan** (an experimental radioimmunoconjugate, also known as TLX591) and **abiraterone** (an androgen biosynthesis inhibitor). Lutetium (177Lu) rosopatamab tetraxetan is a monoclonal antibody (rosopatamab) conjugated to the radioactive isotope lutetium-177 via the chelator tetraxetan, targeting the **prostate-specific membrane antigen (PSMA)** highly expressed on prostate cancer cells. It delivers targeted radiation to PSMA-expressing cells, resulting in tumor cell death. Abiraterone is a CYP17 inhibitor that reduces androgen production, suppressing tumor growth in castration-resistant prostate cancer. This combination is under investigation for the treatment of **PSMA-positive metastatic castration-resistant prostate cancer (mCRPC)**, especially in patients who have progressed on prior androgen receptor pathway inhibitors. The combination strategy aims to maximize antitumor effects by delivering localized radiation with TLX591 and systemic hormonal inhibition with abiraterone[1][2][3][4][5][9][10].
- Other names
- lutetium Lu 177 rosopatamab tetraxetan + abiraterone177Lu-rosopatamab tetraxetan + abiraterone177Lu-TLX591 + abiraterone
02
Targets
CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)PSMA (Prostate-specific membrane antigen)
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