Abstract

Preclinically, PARP inhibitors (PARPi) + TOP1 inhibitors have shown highly synergistic antitumour effects, but clinical development has been hampered by overlapping toxicities. Tumour-targeted delivery of a TOP1 inhibitor may reduce systemic toxicity of the combination; thus, we evaluated the PARPi rucaparib + SG, an antibody-drug conjugate composed of an anti-Trop2 antibody coupled to the active metabolite of irinotecan (SN-38) via a unique hydrolyzable linker.

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