Drug intelligence / Profile preview

vorinostat + lutetium Lu 177 vipivotide tetraxetan

Development stage
Phase 2
Lead developer
Fred Hutch
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination therapy consists of vorinostat, a histone deacetylase (HDAC) inhibitor, and lutetium Lu 177 vipivotide tetraxetan, a PSMA-targeted radioligand therapy. In the context of the VALOR phase II trial conducted by Fred Hutchinson Cancer Center, vorinostat is utilized as an epigenetic priming agent to upregulate the expression of prostate-specific membrane antigen (PSMA) in patients with PSMA-low metastatic castration-resistant prostate cancer (mCRPC). By increasing PSMA density on tumor cells, vorinostat aims to enhance the binding and therapeutic efficacy of the subsequent radiopharmaceutical, 177Lu-PSMA-617, which delivers targeted beta-particle radiation to the cancer cells.

Other names
vorinostat + 177Lu-PSMA-617vorinostat + lutetium (177Lu) vipivotide tetraxetan
02

Targets

HDAC (HDAC family)PSMA (Prostate-specific membrane antigen)

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