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Rovalpituzumab tesirine

Rovalpituzumab tesirine
Monoclonal antibody
TypeWhole antibody
SourceHumanized
TargetDLL3
Clinical data
ATC code
  • None
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC6416H9894N1698O2028S46 (non-glycosylated)

Rovalpituzumab tesirine (Rova-T) is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells.[1] It was originally developed by Stemcentrx and was purchased by AbbVie.[2] It was tested for use in small-cell lung cancer, but development was terminated after unsuccessful phase III trial.[3][4]

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.[5][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

Tesirine skeletal.svg

Chemical structure of "tesirine" (drawn in black). It consists of a pyrrolobenzodiazepine type dimer (top), which is the actual anti-cancer agent, a ValAla 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

References

  1. ^ "Statement On A Nonproprietary Name Adopted By The USAN Council: USAN (de-144) Rovalpituzumab" (PDF). Searchusan.ama-assn.org. Retrieved 2017-05-23.
  2. ^ [bciq.biocentury.com]
  3. ^ "AbbVie Discontinues Rovalpituzumab Tesirine (Rova-T) Research and Development Program | AbbVie News Center". news.abbvie.com. Retrieved 29 August 2019.
  4. ^ Alternative Names: Rova-T; SC16LD6.5. "Rovalpituzumab tesirine - AdisInsight". Adisinsight.springer.com. Retrieved 2017-05-22.
  5. ^ "It's official—AbbVie dumps Rova-T after another lung cancer fail". FierceBiotech. Retrieved 29 August 2019.
  6. ^ "A Study of Rovalpituzumab Tesirine as Maintenance Therapy Following First-Line Platinum-Based Chemotherapy in Participants With Extensive Stage Small Cell Lung Cancer (MERU) - Full Text View". ClinicalTrials.gov. Retrieved 2017-05-22.
  7. ^ "AbbVie ditches plans for accelerated Rova-T review after weak phase 2 data". FierceBiotech. Retrieved 29 August 2019.
  8. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 75" (PDF). WHO Drug Information. World Health Organization. 30 (1): 151. 2016.