Rovalpituzumab tesirine and DLL3: a new challenge for small-cell lung cancer

DLL3—an atypical inhibitor of the Notch ligand—has been identified in tumour-initiating cells isolated from small-cell lung cancer. It is expressed on the surface of tumour cells in about 85% of patients with small-cell lung cancer and large-cell neuroendocrine cancer, but not in healthy tissues and non-neuroendocrine tumours. 1 Saunders LR Bankovich AJ Anderson WC et al. A DLL3-targeted antibody-drug conjugate eradicates high-grade pulmonary neuroendocrine tumor-initiating cells in vivo. Sci Transl Med. 2015; 7: 302ra136 Crossref PubMed Scopus (381) Google Scholar DLL3 is a novel and promising target for development of specific inhibitors to treat patients with small-cell lung cancer. Rovalpituzumab tesirine, a DLL3-targeted antibody-drug conjugate, in recurrent small-cell lung cancer: a first-in-human, first-in-class, open-label, phase 1 studyRovalpituzumab tesirine shows encouraging single-agent antitumour activity with a manageable safety profile. Further development of rovalpituzumab tesirine in DLL3-expressing malignant diseases is warranted. Full-Text PDF