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lutetium (177Lu) rosopatamab tetraxetan + enzalutamide
- Development stage
- Phase 3
- Lead developer
- Telix Pharmaceuticals
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous (lutetium (177Lu) Rosopatamab Tetraxetan)[1][2][5], Oral (enzalutamide)
01
Overview
**Lutetium (177Lu) rosopatamab tetraxetan + enzalutamide** is a combination therapy under clinical investigation for **PSMA-positive metastatic castration-resistant prostate cancer (mCRPC)**. Lutetium (177Lu) rosopatamab tetraxetan, also referred to as TLX591 or 177Lu-DOTA-TLX591, is a **radioimmunoconjugate (rADC)** consisting of a monoclonal antibody (rosopatamab) targeting **prostate-specific membrane antigen (PSMA)**, conjugated to the beta-emitting radioisotope lutetium-177 via a tetraxetan chelator. This modality delivers targeted radiation to PSMA-expressing cancer cells, aiming for tumor cell destruction while minimizing off-target effects. **Enzalutamide** is a **small molecule androgen receptor inhibitor** used as standard of care (SOC) to block the androgen receptor pathway, essential in prostate cancer cell survival and proliferation. The combination is hypothesized to synergize by radiosensitizing tumor cells through hormonal blockade and simultaneously targeting/murdering tumor cells via radiopharmaceutical-induced DNA damage[1][2][4][5]. The combination is currently in **Phase III clinical trials** for patients who have progressed after androgen receptor pathway inhibitors, including abiraterone or enzalutamide[1][2][4][5].
- Other names
- lutetium (177Lu) rosopatamab tetraxetanenzalutamide
02
Targets
AR (Adrenergic receptors)PSMA (Prostate-specific membrane antigen)
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