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testosterone cypionate + lutetium Lu 177 vipivotide tetraxetan

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

Overview

testosterone cypionate + lutetium Lu 177 vipivotide tetraxetan is an experimental combination regimen being evaluated by the H. Lee Moffitt Cancer Center and Research Institute for the treatment of metastatic castration-resistant prostate cancer (mCRPC). This sequential therapy utilizes high-dose testosterone cypionate (400 mg), a strategy known as Bipolar Androgen Therapy (BAT), to potentially upregulate the expression of Prostate-Specific Membrane Antigen (PSMA) on tumor cells. This priming step is followed by the administration of lutetium Lu 177 vipivotide tetraxetan (PSMA-617), a targeted radioligand therapy. PSMA-617 consists of a ligand that binds with high affinity to PSMA, a linker, and a radioactive payload, Lutetium-177. Upon binding, the drug is internalized, delivering concentrated beta-particle radiation to the cancer cells, resulting in DNA damage and cell death. The combination aims to overcome resistance and enhance the therapeutic index of radioligand therapy in patients with advanced prostate cancer.

Brand names: PluvictoDepo-Testosterone
Other names: 177Lu-PSMA-617Lutetium Lu 177 vipivotide tetraxetanTestosterone cypionate

Targets

PSMA (Prostate-specific membrane antigen)

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