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Synonyms: hRS7-SN-38-ADC | IMMU-132 | sacituzumab govitecan-hziy | Trodelvy®
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 [1]) [2-3,5]. TROP-2 is a transmembrane glycoprotein, cell surface antigen which has oncogenic activity in cancers of epithelial origin [6], 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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| Bioactivity Comments |
| Stein et al (1993) [4] and (1994) [5] 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. |
| Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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