Rovalpituzumab Tesirine: A Novel DLL3-Targeting Antibody–Drug Conjugate

• Published in: Drugs in R&D Vol. 18; no. 4; pp. 255 - 258
• Main Authors: Lashari, Bilal H., Vallatharasu, Yazhini, Kolandra, Lakshmi, Hamid, Mohsin, Uprety, Dipesh
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.12.2018; Springer Nature B.V; Adis, Springer Healthcare
• Subjects: Internal Medicine; Lung cancer; Medicine; Medicine & Public Health; Pharmacology/Toxicology; Pharmacotherapy; Review; Review Article
• ISSN: 1174-5886; 1179-6901
• DOI: 10.1007/s40268-018-0247-7

Small cell lung cancer (SCLC) comprises about 15% of all cases of lung cancer. In recent years, owing to a change in the epidemiology of smoking habits, the incidence of the tumor has decreased; however, it remains a significant challenge to global health. While the tumor has a favorable initial response to chemoradiation, relapse is invariable, and second-line regimens may be intolerable given the severity of side effects. For patients with tumors resistant to second-line regimens, no current standard regimens exist. Rovalpituzumab tesirine is a novel antibody–drug conjugate, targeting delta-like protein 3, fundamental in the downstream cellular signaling for proliferation and apoptosis. This drug is reported to have shown promise in pre-clinical and phase I trials. It appears effective in decreasing tumor burden and is reported to be well tolerated, albeit with a significant adverse effect profile. Currently, it is being studied as part of initial and subsequent line chemotherapeutic regimens; it remains to be seen if this is a viable option in the treatment of SCLC. This may add to the agents that can be used against SCLC, and help improve outcomes.