sacituzumab govitecan   Click here for help

GtoPdb Ligand ID: 8253

Synonyms: hRS7-SN-38-ADC | IMMU-132 | sacituzumab govitecan-hziy | Trodelvy®
Approved drug
sacituzumab govitecan is an approved drug (FDA (2020), EMA (2021))
Compound class: Antibody
Comment: IMMU-132 is an antibody-drug conjugate (ADC) with SN-38 (the active metabolite of the topoisomerase inhibitor irinotecan) covalently linked to an anti-TROP-2 monoclonal antibody (see patent US8574575 [2]) [3-4,6]. TROP-2 is a transmembrane glycoprotein, cell surface antigen which has oncogenic activity in cancers of epithelial origin [7], but expression is restricted in normal tissue. Directing SN-38 to cancer cells via TROP-2 binding is predicted to limit toxicity towards healthy tissue/cells.
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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
Bioactivity Comments
Stein et al (1993) [5] and (1994) [6] report the specificity and properties of monoclonal antibody RS7-3G11, the murine antibody on which IMMU-132 is based. These articles do not provide binding affinity data for the interaction between the antibody and TROP-2. Covalent linking of SN-38 would be designed in such a way as to have minimal effect on antibody-antigen affinity. SPR-determined binding affinity was reported in [1], which directly compared the binding profiles of sacituzumab govitecan and sacituzumab tirumotecan.
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
tumor associated calcium signal transducer 2 Primary target of this compound Hs Antibody Binding 9.5 pKd - 1-2
⤷ pKd 9.5 (Kd 2.9x10-10 M) [1-2]
Description: Binding affinity determined by SPR