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lutetium (177Lu) vipivotide tetraxetan + enzalutamide

Development stage: Unknown
Lead developer: Novartis
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Intravenous, Oral

Overview

This combination therapy consists of the radiopharmaceutical **lutetium (177Lu) vipivotide tetraxetan** (Pluvicto) and the androgen receptor inhibitor **enzalutamide** (Xtandi). It is being investigated by the **Australian and New Zealand Urogenital and Prostate Cancer Trials Group (ANZUP)** in the **ENZA-p** trial (ANZUP 1901) for patients with chemotherapy-naive metastatic castration-resistant prostate cancer (mCRPC) who exhibit high-risk features. Lutetium (177Lu) vipivotide tetraxetan is a radioligand therapy that targets prostate-specific membrane antigen (PSMA) to deliver localized beta-radiation directly to cancer cells. Enzalutamide is a small molecule that competitively inhibits androgen binding to the androgen receptor, thereby blocking receptor translocation and DNA binding. The combination aims to improve progression-free and overall survival by simultaneously targeting the hormonal drivers of prostate cancer and delivering targeted radiation to PSMA-expressing cells.

Brand names: PluvictoXtandi
Other names: Lu-PSMA177Lu-PSMA-617lutetium-177-PSMA-617lutetium177-PSMA-617lutetium 177-PSMA-617enzalutamidelutetium (177Lu) vipivotide tetraxetanLuPSMA

Targets

PSMA (Prostate-specific membrane antigen)AR (Adrenergic receptors)

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