sacituzumab govitecan

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Ligands
sacituzumab govitecan

GtoPdb Ligand ID: 8253

Synonyms: hRS7-SN-38-ADC | IMMU-132 | sacituzumab govitecan-hziy | Trodelvy®

sacituzumab govitecan is an approved drug (FDA (2020), EMA (2021))

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.

References
1. 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.
2. 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]
3. Sahota S, Vahdat LT. (2017) Sacituzumab govitecan: an antibody-drug conjugate. Expert Opin Biol Ther, 17 (8): 1027-1031. [PMID:28503956]
4. 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]
5. 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]
6. 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]

References

1. 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.

2. 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]

3. Sahota S, Vahdat LT. (2017)
Sacituzumab govitecan: an antibody-drug conjugate.
Expert Opin Biol Ther, 17 (8): 1027-1031. [PMID:28503956]

4. 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]

5. 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]

6. 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]