| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized |
| Target | DLL3 |
| Clinical data | |
| ATC code |
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| Identifiers | |
| CAS Number | |
| ChemSpider |
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| UNII | |
| KEGG | |
| Chemical and physical data | |
| Formula | C6416H9894N1698O2028S46 (non-glycosylated) |
Rovalpituzumab tesirine (Rova-T) is an experimentalantibody-drug conjugate targeting the proteinDLL3 on tumor cells.[1][2] It was originally developed byStemcentrx and was purchased byAbbVie.[3] It was tested for use insmall-cell lung cancer, but development was terminated after unsuccessfulphase III trial.[4][5]
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 (MERU) demonstrated no survival benefit over placebo.[6][7] 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%.[8]
Chemical structure of "tesirine" (drawn in black). It consists of apyrrolobenzodiazepine typedimer (top), which is the actual anti-cancer agent, aVal–Ala structure that can be cleaved by an enzyme to detach the anti-cancer agent from the antibody, apolyethylene glycol spacer, and amaleimide linker which is attached to acysteine in the antibody's (rovalpituzumab's)peptide backbone, drawn blue. Each rovalpituzumab molecule has an average of two such attachments.[9]
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