Sacituzumab

Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab is used for the synthesis of antibody-drug conjugates (ADC) drugs. Antibody-drug conjugates with sacituzumab (sacituzumab govitecan) (HY-132254) targeting TROP-2 have been approved for the field of triple-negative breast cancer[1][2][3][4].

[1] Zhou DD, et al. Elucidating the development, characterization, and antitumor potential of a novel humanized antibody against Trop2[J]. Int J Biol Macromol. 2023 Dec 31;253(Pt 6):127105. DOI:10.1016/j.ijbiomac.2023.127105
[2] Sun M, et al. Structural insights into the cis and trans assembly of human trophoblast cell surface antigen 2[J]. iScience. 2021 Sep 30;24(10):103190. DOI:10.1016/j.isci.2021.103190
[3] Shih LB, et al. In vitro and in vivo reactivity of an internalizing antibody, RS7, with human breast cancer[J]. Cancer Res. 1995 Dec 1;55(23 Suppl):5857s-5863s. PMID:7493360
[4] Bardia A, et al. Biomarker analyses in the phase III ASCENT study of sacituzumab govitecan versus chemotherapy in patients with metastatic triple-negative breast cancer. Ann Oncol. 2021 Sep;32(9):1148-1156. DOI:10.1016/j.annonc.2021.06.002