Rovalpituzumab tesirine
Today, we want to delve into the exciting world of Rovalpituzumab tesirine. Whether we are talking about the history of Rovalpituzumab tesirine, its impact on society today, or its possible applications in the future, Rovalpituzumab tesirine is a topic that never ceases to amaze us. Throughout this article, we will explore the different aspects of Rovalpituzumab tesirine, from its origins to its implications in daily life. Regardless of whether you are an expert on the subject or are just discovering its existence, we invite you to immerse yourself in this fascinating universe and discover everything that Rovalpituzumab tesirine has to offer us.
| 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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| Formula | C6416H9894N1698O2028S46 (non-glycosylated) |
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 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 (MERU) 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
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
- ^ "Statement On A Nonproprietary Name Adopted By The USAN Council: USAN (de-144) Rovalpituzumab" (PDF). Searchusan.ama-assn.org. Retrieved 2017-05-23.
- ^ Lashari BH, Vallatharasu Y, Kolandra L, Hamid M, Uprety D (December 2018). "Rovalpituzumab Tesirine: A Novel DLL3-Targeting Antibody-Drug Conjugate". Drugs in R&D. 18 (4): 255–258. doi:10.1007/s40268-018-0247-7. PMC 6277321. PMID 30232719.
- ^ "Rova-T (Rovalpituzumab tesirine)". BioCentury.
- ^ "AbbVie Discontinues Rovalpituzumab Tesirine (Rova-T) Research and Development Program | AbbVie News Center". news.abbvie.com. Retrieved 29 August 2019.
- ^ Alternative Names: Rova-T; SC16LD6.5. "Rovalpituzumab tesirine - AdisInsight". Adisinsight.springer.com. Retrieved 2017-05-22.
{{cite web}}: CS1 maint: multiple names: authors list (link) CS1 maint: numeric names: authors list (link) - ^ "It's official—AbbVie dumps Rova-T after another lung cancer fail". FierceBiotech. Retrieved 29 August 2019.
- ^ Clinical trial number NCT03033511 for "A Study of Rovalpituzumab Tesirine as Maintenance Therapy Following First-Line Platinum-Based Chemotherapy in Participants With Extensive Stage Small Cell Lung Cancer (MERU) " at ClinicalTrials.gov
- ^ "AbbVie ditches plans for accelerated Rova-T review after weak phase 2 data". FierceBiotech. Retrieved 29 August 2019.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 75" (PDF). WHO Drug Information. 30 (1). World Health Organization: 151. 2016.