eis-12656 + trastuzumab deruxtecan

EIS-12656 + trastuzumab deruxtecan is a **combination therapy** under investigation for solid tumors. - **EIS-12656** is a first-in-class, oral, brain-penetrant small molecule inhibitor targeting the chromatin helicase ALC1 (CHD1L) via allosteric mechanisms, thereby suppressing cancer-relevant genome reorganization and inducing cancer cell death in tumors with DNA repair deficiencies. It is specifically designed to overcome resistance to PARP inhibitors and has shown synergy with standard therapies in preclinical studies[2][4][6]. - **Trastuzumab deruxtecan** is an antibody-drug conjugate that links trastuzumab (which binds HER2 receptor and blocks signaling) to deruxtecan, a topoisomerase I inhibitor. After binding HER2 on cancer cells, it internalizes to deliver deruxtecan, causing DNA damage and cell death, and is approved for HER2-positive and HER2-low breast cancer, NSCLC, and gastric adenocarcinoma[1][3][5]. The combination is under study for synergistic anti-tumor effects, especially in genetically-defined advanced solid tumors and those refractory to PARP inhibitors[2][4][6].

Other names

fam-trastuzumab deruxtecan-nxki