Rovalpituzumab tesirine

Rovalpituzumab
Monoclonal antibody
Type Whole antibody
Source Humanized
Target DLL3
Clinical data
ATC code
  • None
Identifiers
CAS Number
ChemSpider
  • none
UNII
Chemical and physical data
Formula C6416H9894N1698O2028S46 (non-glycosylated)

Rovalpituzumab tesirine is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells.[1] It was developed by Stemcentrx. It is being tested for use in small-cell lung cancer.[2]

Development

A phase III trial is evaluating the drug as a maintenance therapy after chemotherapy for small cell lung cancer.[3] A phase II trial is using the drug as a third-line treatment for relapsed or refractory lung cancer.[4]

Chemical structure

Chemical structure of "tesirine" (drawn 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.[5]

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. ↑ Alternative Names: Rova-T; SC16LD6.5. "Rovalpituzumab tesirine - AdisInsight". Adisinsight.springer.com. Retrieved 2017-05-22.
  3. ↑ "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.
  4. ↑
  5. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 75" (PDF). WHO Drug Information. World Health Organization. 30 (1): 151. 2016.


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