Rovalpituzumab tesirine
Rovalpituzumab tesirine is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells. It was originally developed by Stemcentrx and was purchased by AbbVie. It was tested for use in small-cell lung cancer, but development was terminated after unsuccessful phase III trial.Development
In 2018, an Independent Data Monitoring Committee found that in the TAHOE phase III trial, Rova-T shortened survival of lung cancer patients compared to SOC chemotherapy topotecan, prompting termination of trial enrollment. Another phase III trial demonstrated no survival benefit over placebo. A phase II trial using the drug as a third-line treatment for relapsed or refractory lung cancer showed objective response rate at just 16%.Chemical structure of "tesirine". It consists of a pyrrolobenzodiazepine type dimer, which is the actual anti-cancer agent, a Val–Ala structure that can be cleaved by an enzyme to detach the anti-cancer agent from the antibody, a polyethylene glycol spacer, and a maleimide linker which is attached to a cysteine in the antibody's peptide backbone, drawn blue. Each rovalpituzumab molecule has an average of two such attachments.
