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
References
1. Cheng Y, Yuan X, Tian Q, Huang X, Chen Y, Pu Y, Long H, Xu M, Ji Y, Xie J et al.. (2022)
Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132.
Front Oncol, 12: 951589. [PMID:36620535]
2. Govindan SV, Qu Z, Hansen HJ, Goldenberg DM. (2013)
RS7 antibodies.
Patent number: US8574575. Assignee: Immunomedics, Inc.. Priority date: 01/03/2002. Publication date: 05/11/2013.
3. Ocean AJ, Starodub AN, Bardia A, Vahdat LT, Isakoff SJ, Guarino M, Messersmith WA, Picozzi VJ, Mayer IA, Wegener WA et al.. (2017)
Sacituzumab govitecan (IMMU-132), an anti-Trop-2-SN-38 antibody-drug conjugate for the treatment of diverse epithelial cancers: Safety and pharmacokinetics.
Cancer, 123 (19): 3843-3854. [PMID:28558150]
4. Sahota S, Vahdat LT. (2017)
Sacituzumab govitecan: an antibody-drug conjugate.
Expert Opin Biol Ther, 17 (8): 1027-1031. [PMID:28503956]
5. Stein R, Basu A, Chen S, Shih LB, Goldenberg DM. (1993)
Specificity and properties of MAb RS7-3G11 and the antigen defined by this pancarcinoma monoclonal antibody.
Int J Cancer, 55 (6): 938-46. [PMID:8253531]
6. Stein R, Basu A, Goldenberg DM, Lloyd KO, Mattes MJ. (1994)
Characterization of cluster 13: the epithelial/carcinoma antigen recognized by MAb RS7.
Int J Cancer Suppl, 8: 98-102. [PMID:8194903]
7. Stoyanova T, Goldstein AS, Cai H, Drake JM, Huang J, Witte ON. (2012)
Regulated proteolysis of Trop2 drives epithelial hyperplasia and stem cell self-renewal via β-catenin signaling.
Genes Dev, 26 (20): 2271-85. [PMID:23070813]