Rovalpituzumab tesirine (Rova-T) 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 is being tested for use in small-cell lung cancer.
Video Rovalpituzumab tesirine
Development
A phase III trial is evaluating the drug as a maintenance therapy after chemotherapy for small cell lung cancer. A phase II trial is using the drug as a third-line treatment for relapsed or refractory lung cancer.
Maps Rovalpituzumab tesirine
Chemical structure
Chemical structure of "tesirine" (drawn in black). It consists of a pyrrolobenzodiazepine type dimer (top), 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 (rovalpituzumab's) peptide backbone, drawn blue. Each rovalpituzumab molecule has an average of two such attachments.
See also
- Vadastuximab talirine, with a similar cytotoxin
References
Source of article : Wikipedia