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rovalpituzumab tesirine

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Overview

Generic Name(s):
rovalpituzumab tesirine
NCI Definition [1]:
An antibody-drug conjugate (ADC) containing a humanized IgG1 monoclonal antibody (MAb) directed against the delta-like protein 3 (DLL3), conjugated to the cytotoxic pyrrolobenzodiazepine (PBD) dimer D6.5 (SC-DR002) via a maleimide-containing linker with an eight-carbon polyethylene glycol spacer and a cathepsin B-cleavable valine-alanine dipeptide, with potential antineoplastic activity. The MAb moiety of rovalpituzumab tesirine selectively binds to DLL3 on tumor cell surfaces. Upon internalization of the ADC, the dipeptide linker is cleaved and D6.5 is released. Then the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death, and inhibits the proliferation of DLL3-overexpressing tumor cells. DLL3, a membrane protein that binds to Notch receptors and regulates Notch-mediated signaling and gene transcription, is overexpressed by certain cancers but is rarely expressed by normal, healthy cells.

Clinical Trials

View Clinical Trials for rovalpituzumab tesirine

Rovalpituzumab tesirine has been investigated in 6 clinical trials, of which 1 is open and 5 are closed. Of the trials investigating rovalpituzumab tesirine, 2 are phase 1 (1 open), 1 is phase 1/phase 2 (0 open), and 3 are phase 3 (0 open).

DLL3 Expression is the most frequent biomarker inclusion criterion for rovalpituzumab tesirine clinical trials.

Small cell lung carcinoma is the most common disease being investigated in rovalpituzumab tesirine clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Rovalpituzumab Tesirine
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Rovalpituzumab Tesirine
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating rovalpituzumab tesirine and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
sc16ld6.5, sc0002, 1613313-09-9, anti-sc16 adc sc16ld6.5, rova-t, antibody-drug conjugate sc16ld6.5
Drug Target(s) [2]:
DLL3
NCIT ID [1]:
C107678

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.