Preferred Label : Rovalpituzumab Tesirine;
NCIt synonyms : Rova-T;
NCIt definition : 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.;
UNII : P256HB60FF;
CAS number : 1613313-09-9;
Molecule name : SC16LD6.5;
NCI Metathesaurus CUI : CL451868;
Origin ID : C107678;
UMLS CUI : C4507507;
CISMeF manual mappings
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
