trastuzumab deruxtecan + ceralasertib

This is a combination of two investigational anticancer agents: **trastuzumab deruxtecan**, a HER2-directed antibody-drug conjugate, and **ceralasertib**, a selective, oral ATR kinase inhibitor. Trastuzumab deruxtecan consists of a humanized anti-HER2 IgG1 monoclonal antibody linked to a cytotoxic topoisomerase I inhibitor (deruxtecan). It binds to HER2 on tumor cells, is internalized, and releases the cytotoxic agent inside the cell, causing targeted DNA damage and apoptosis[9][15][19]. Ceralasertib inhibits ATR kinase, a key regulator in the DNA damage response pathway. By inhibiting ATR, ceralasertib increases sensitivity to DNA-damaging agents and suppresses tumor cell replication stress response[10][12][18][20]. The combination is under clinical development for advanced solid tumors, leveraging complementary mechanisms: targeting HER2-expressing cells (trastuzumab deruxtecan) and potentiating DNA damage (ceralasertib)[12]. Primary indications under investigation are **HER2-positive and HER2-expressing advanced solid tumors**.

Other names

fam-trastuzumab deruxtecan-nxki