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I-131-1095 + enzalutamide
- Development stage
- Unknown
- Lead developer
- Lantheus
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
**I-131-1095 + enzalutamide** is a combination of a PSMA-targeted radiotherapeutic small molecule (I-131-1095) and androgen receptor antagonist enzalutamide, developed to treat metastatic castration-resistant prostate cancer (mCRPC) in chemotherapy-naïve patients who are PSMA-avid and have progressed on abiraterone[1][2][4][5][7]. I-131-1095 is a glutamate-urea-lysine analogue radiolabeled with iodine-131 that binds to the extracellular domain of prostate-specific membrane antigen (PSMA), highly expressed in prostate cancer cells; upon binding, it is internalized and delivers cytotoxic beta-radiation to the malignant cell[1][3][4]. Enzalutamide blocks androgen receptor signaling, reducing prostate cancer cell proliferation. Preclinical and compassionate-use data support synergy, as enzalutamide can sensitize tumor cells to radiotherapy-induced cell death[1].
- Other names
- I-131-1095 + enzalutamide
02
Targets
PSMA (Prostate-specific membrane antigen)AR (Adrenergic receptors)
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