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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
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Summary of Clinical Use Click here for help
Sacituzumab govitecan (IMMU-132) was progressed to clinical evaluation as a therapy for epithelial-derived cancers. The US FDA granted fast track status for IMMU-132 as a therapy for triple negative breast cancer (TNBC) and small-cell lung cancer (SCLC) and orphan designation for SCLC and pancreatic cancer. In April 2020, the FDA approved sacituzumab govitecan as a therapy for heavily pretreated metastatic TNBC (at least two prior therapies in the metastatic setting). In April 2021, the FDA granted accelerated approval as a therapy for advanced or metastatic urothelial cancer, in patients who have already been treated with a platinum-containing chemotherapy and either a PD-1 or PD-L1 inhibitor. January 2023 saw expansion of FDA approval to include treament of unresectable locally advanced or metastatic hormone receptor positive, HER2-negative breast cancer (in patients who have already been treated with endocrine-based therapy and at ≥2 additional systemic therapies in the metastatic setting)
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02161679 Phase II Study of IMMU-132 Alone or in Combination With Carboplatin in Patients With Triple-Negative Breast Cancer Phase 2 Interventional Immunomedics, Inc.
NCT02574455 ASCENT-Study of Sacituzumab Govitecan in Refractory/Relapsed Triple-Negative Breast Cancer Phase 3 Interventional Immunomedics, Inc. Approval for TNBC was based on evidence of efficacy from this trial.
NCT01631552 Phase I/II Study of IMMU-132 in Patients With Epithelial Cancers Phase 1/Phase 2 Interventional Immunomedics, Inc.