DS-3939a: A TA-MUC1-Directed Antibody-Drug Conjugate with Broad Antitumor Activity.

ABSTRACT: Tumor-associated mucin-1 (TA-MUC1) is a glycoform of the MUC1 protein that is aberrantly glycosylated and is primarily observed in cancer cells. TA-MUC1 is highly expressed in various human epithelial cancers, making it an attractive target for cancer therapies. In this study, we describe the development of DS-3939a, a novel TA-MUC1-targeting antibody-drug conjugate that utilizes the potent DNA topoisomerase I inhibitor DXd, and evaluation of its pharmacologic activity in preclinical in vitro and in vivo models. IHC of clinical tumor tissue microarrays of various cancer types exhibited positive staining for TA-MUC1 in a number of samples, with a particularly high positive rate in bladder, lung, and breast cancers. In vitro profiling of DS-3939a confirmed that it could specifically bind to

SUBMITTER: Takano K 

PROVIDER: S-EPMC12757726 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature