vadastuximab talirine   Click here for help

GtoPdb Ligand ID: 9434

Synonyms: SGN-CD33A
Immunopharmacology Ligand
Compound class: Antibody
Comment: Vadastuximab talirine (SGN-CD33A; Seattle Genetics) is an humanized anti-CD33 antibody-drug conjugate (ADC) which delivers a toxic payload to CD33 +ve cells [1]. Talirine is a pyrrolobenzodiazepine (PBD) dimer (PubChem CID 45257190), which is a DNA crosslinking agent, causing DNA damage and ultimately apoptosis of targeted cells. Talirine is conjugated to engineered Cys residues in the antibody via a cathepsine B cleavable linker.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
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Ligand Activity Visualisation Charts

These 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.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Both the US FDA and EMA have designated vadastuximab talirine as an orphan drug for acute myeloid leukemia (AML). In late 2016, the FDA put holds on phase 1 and 1/2 trials of vadastuximab talirine in AML following the deaths of several trial participants, whilst any link between hepatotoxicity and vadastuximab talirine is assessed. Click here to link to ClinicalTrials.gov's full list of vadastuximab talirine trials.