Drug intelligence / Profile preview

epratuzumab-SN-38

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Epratuzumab-SN-38** is an antibody-drug conjugate (ADC) comprising the humanized anti-CD22 monoclonal antibody epratuzumab conjugated to SN-38, the active metabolite of irinotecan, via a linker that enables slow dissociation (approximately 50% of IgG-bound SN-38 released in serum every 24 hours). It targets CD22 on B-cell malignancies, leveraging rapid internalization for enhanced intracellular delivery of SN-38, a topoisomerase I inhibitor that induces DNA damage and cell death. Developed by Immunomedics, it demonstrates nanomolar potency against lymphoma and leukemia cell lines (IC50 0.06-2.7 nM) in vitro, superior efficacy in Ramos xenografts compared to non-binding conjugates, and potential for combination with anti-CD20 antibodies like veltuzumab.[1][5][8]

Other names
epratuzumab-SN-38epratuzumab-SN38epratuzumab-SN 38
02

Targets

TOP1 (DNA Topoisomerase I)CD22 (Cluster of Differentiation 22)

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