Rovalpituzumab tesirine explained
| Type: | mab |
| Mab Type: | mab |
| Source: | zu |
| Target: | DLL3 |
| Cas Number: | 1613313-09-9 |
| Atc Prefix: | None |
| Chemspiderid: | none |
| Unii: | P256HB60FF |
| Kegg: | D10981 |
| Chemical Formula: | C6416H9894N1698O2028S46 (non-glycosylated) |
Rovalpituzumab tesirine (Rova-T) is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells.[1] [2] It was originally developed by Stemcentrx and was purchased by AbbVie.[3] It was tested for use in small-cell lung cancer, but development was terminated after unsuccessful phase III trial.[4] [5]
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 (MERU) demonstrated no survival benefit over placebo.[6] 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%.[7]
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.
[8] See also
Notes and References
- Web site: Statement On A Nonproprietary Name Adopted By The USAN Council: USAN (de-144) Rovalpituzumab . Searchusan.ama-assn.org . 2017-05-23.
- Lashari BH, Vallatharasu Y, Kolandra L, Hamid M, Uprety D . Rovalpituzumab Tesirine: A Novel DLL3-Targeting Antibody-Drug Conjugate . Drugs in R&D . 18 . 4 . 255–258 . December 2018 . 30232719 . 6277321 . 10.1007/s40268-018-0247-7 .
- Web site: Rova-T (Rovalpituzumab tesirine) . BioCentury .
- Web site: AbbVie Discontinues Rovalpituzumab Tesirine (Rova-T) Research and Development Program AbbVie News Center . news.abbvie.com . 29 August 2019.
- Web site: Alternative Names: Rova-T; SC16LD6.5 . Rovalpituzumab tesirine - AdisInsight . Adisinsight.springer.com . 2017-05-22.
- Web site: It's official—AbbVie dumps Rova-T after another lung cancer fail . FierceBiotech . 29 August 2019 . en.
- Web site: AbbVie ditches plans for accelerated Rova-T review after weak phase 2 data . FierceBiotech . 29 August 2019 . en.
- WHO Drug Information. 30. 1. 2016. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 75. World Health Organization. 151.
