7. Neutron Capture Therapy

概要

INTRODUCTION:
Only p-dihydroxyboronophenylalanine (BPA) is cur- rently used in BNCT as a boron agent. However, BPA has issues such as low tumor accumulation and selectivity, large single-dose amounts, and water solubility, so there is a need to develop novel agents that show more favora- ble distribution in the body and higher tumor uptake. Many novel drugs are currently under development, in- cluding boron-containing porphyrins, amino acids, pep- tides, monoclonal antibodies, liposomes, various nano- particles, boron cluster compounds, and copolymers.

Prostate cancer is the most commonly diagnosed form of cancer and the second leading cause of cancer-related deaths in men in the world. The prostate specific mem- brane antigen (PSMA) is an attractive target for diagnosis and therapy of prostate cancer because of its high expres- sion in prostate cancer.1,2 PSMA is expressed in normal prostate tissue, primary prostate cancer, and lymph node metastases of prostate cancer,2 although PSMA expression in prostate cancer is 10- to 100-fold higher than that in normal prostate tis- sue.3

PSMA exhibits GCP-II (glutamatecarboxy pepti- dase-II) activity. Previously, several asymmetric urea compounds (X-CO-Glu) were reported to act as GCP-II inhibitors. We also demonstrated the high affinity of asymmetric urea compounds (maleimido-Cys-CO-Glu) for PSMA in vivo.4

Given this background, in this study, we designed and synthesized a novel BNCT agent targeting PSMA (BP-1).

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