Preferred Label : Anti-mesothelin-Pseudomonas Exotoxin 24 Cytolytic Fusion Protein LMB-100;
NCIt synonyms : Anti-MSLN-PE24 cFP LMB-100;
NCIt related terms : LMB-100;
NCIt definition : An anti-mesothelin (MSLN) recombinant cytolytic fusion protein (cFP) composed of a
humanized Fab fragment of anti-MSLN monoclonal antibody SS1 linked to a truncated
and de-immunized 24 kDa fragment of the Pseudomonas exotoxin (PE) (PE24), with potential
antineoplastic activity. Upon intravenous administration of anti-MSLN-PE24 cFP LMB-100,
the anti-MSLN moiety targets and binds to MSLN-expressing tumor cells. Upon binding
and internalization through endocytosis, the toxin moiety ADP-ribosylates and inactivates
eukaryotic elongation factor 2 (eEF2), preventing the elongation step of protein synthesis
and leading to both an inhibition of protein synthesis and an induction of MSLN-expressing
tumor cell apoptosis. MSLN, a tumor-associated antigen overexpressed in a variety
of cancer cell types, plays a key role in tumor cell proliferation and migration.
The engineered PE24 portion of LMB-100 does contain the targeting domain and furin
cleavage site, which are needed for cytotoxicity, but most of the translocation domain
II is deleted and the catalytic domain III contains point mutations, which result
in the deletion and silencing of most T- and B-cell epitopes; therefore, the immunogenicity
and toxicity is reduced compared to non-engineered PE toxin, which allows for the
administration of larger doses of LMB-100.;
UNII : D6AT024T4P;
CAS number : 1841500-93-3;
Molecule name : RG-7787; RO 6927005; RO6927005; RG 7787; LMB-100;
Origin ID : C121653;
UMLS CUI : C4287742;
Semantic type(s)
- UMLS correspondences (same concept)
- LMB-100 [MeSH Supplementary Concept]
- concept_is_in_subset
- has_target
