PARP targeted Auger emitter therapy with [¹²⁵I]PARPi-01 for triple-negative breast cancer.

ABSTRACT:

Background

Triple-negative breast cancer (TNBC) lacks biomarkers for targeted therapy. Auger emitters display the best therapeutic effect, if delivered directly into the nucleus proximal to DNA. The nuclear protein Poly (ADP-ribose)-Polymerase 1 (PARP1) is a suitable target against which few inhibitors (PARPi) are clinically approved for treatment of breast cancer with germline BRCA mutation (BRCA^mut). In this study, a theranostic approach was investigated in a TNBC xenografted mouse model by radiolabelling a close derivative of a PARPi Olaparib (termed PARPi-01) with the Auger emitters ^123/125I.

Methods

TNBC cell line MDA-MB-231 was subcutaneously implanted in female NOD/SCID mice. At a tumour size of ~ 500mm³, [¹²³I]PARPi-01 was

SUBMITTER: Ambur Sankaranarayanan R 

PROVIDER: S-EPMC9474773 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature