Synonyms: CAT-8015 | GCR-8015 | HA22 | Lumoxiti® | moxetumomab pasudotox-tdfk
moxetumomab pasudotox is an approved drug (FDA (2018), EMA (2021))
Compound class:
Antibody
Comment: Peptide sequence information for this antibody is available from its IMGT/mAb-DB link. The moxetumomab monoclonal has been mutated to increase affinity for CD22 [6] (patent WO2003027135[1]), and the antibody is fused to a 38 KDa fragment of Pseudomonas exotoxin-A (PE38) [2,4] (patent US7982011 [5]). The Uniprot accession for Pseudomonas exotoxin-A is P11439.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
No information available. |
Summary of Clinical Use |
Moxetumomab pasudotox was assessed as a potential treatment for B-cell malignancies, such as chronic lymphocytic leukemia (CLL) and hairy cell leukemia [3]. Click here to view ClinicalTrials.gov's listing of moxetumomab pasudotox trials. FDA approval for hairy cell leukemia was granted in 2018. In the EU, the antibody has had EMA orphan designation for the treatment of B-lymphoblastic leukaemia / lymphoma since 2013. |
Mechanism Of Action and Pharmacodynamic Effects |
The Fv portion of moxetumomab pasudotox binds to CD22, a cell surface receptor expressed on a variety of malignant B-cells.This targets the toxin moiety, PE38, directly to tumor cells. Internalized PE38 induces caspase-mediated apoptosis via a mechanism involving mitochondrial damage and blocks translational elongation by binding to elongation factor 2 (EF-2) [7]. |
External links |
For extended ADME data see the following: Drugs.com |