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Published on: September 3, 2013
Novel PSMA-Targeting Radionuclide Peptidomimetics for Treating Prostate Cancer
1Experimental Drug Development Centre. 10 Biopolis Road, Chromos #08-01, Singapore 138670, Singapore.
Abstract:
Prostate cancer is the third-most commonly diagnosed cancer and is one of the leading causes of cancer-related deaths in men worldwide. Although an armamentarium of approved drugs exists, treatment options become severely limited when resistance develops against last-line taxane chemotherapeutics. In March 2022, the FDA approved a first-in-class targeted radionuclide therapy, lutetium Lu 177 vipivotide tetraxetan (Pluvicto), for treating metastatic castration-resistant prostate cancer. The drug constitutes a prostate-specific membrane antigen-targeting peptidomimetic moiety conjugated to a radionuclide chelator via a linker. This Patent Highlight reveals the structure-activity relationship of key compounds against prostate cancer cells.
Insights
Lutetium Lu 177 vipivotide tetraxetan is a novel targeted radionuclide therapy for metastatic castration-resistant prostate cancer. This study highlights its structure-activity relationship against prostate cancer cells, offering new treatment avenues.
Area of Science:
- Oncology
- Radiopharmaceutical Therapy
- Medicinal Chemistry
Background:
- Prostate cancer is a leading cause of cancer death in men globally.
- Treatment options are limited for patients with resistance to taxane chemotherapeutics.
- Metastatic castration-resistant prostate cancer (mCRPC) presents significant therapeutic challenges.
