The Mode of Action and Clinical Outcomes of Sacituzumab Govitecan in Solid Tumors.

ABSTRACT: Sacituzumab govitecan (SG), a trophoblast cell-surface antigen-2 (Trop-2)-directed antibody-drug conjugate, is currently approved to treat metastatic triple-negative breast cancer and HR+/HER2- breast cancer and is under clinical investigation for a range of other tumor types. This review describes its mode of action, development, and clinical outcomes. SG is composed of SN-38 (a topoisomerase I inhibitor derived from irinotecan) covalently linked to an anti-Trop-2 mAb (sacituzumab; hRS7) via a hydrolyzable CL2A linker. SN-38 was chosen due to its potent antitumor activity; CL2A occupies the most effective position on SN-38 for maintaining stability during transport, with pH-sensitive payload release in the tumor, and the antigen target (Trop-2) is highly expressed on many solid tumors. SG

SUBMITTER: Tolaney SM 

PROVIDER: S-EPMC11995006 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature