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epratuzumab-CL2E-SN-38
- Development stage
- Discontinued
- Lead developer
- Gilead Sciences
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Epratuzumab-CL2E-SN-38 is an experimental antibody-drug conjugate (ADC) developed by Immunomedics (now Gilead Sciences) for the treatment of B-cell malignancies. It consists of the humanized anti-CD22 monoclonal antibody epratuzumab conjugated to the topoisomerase I inhibitor SN-38 via a serum-stable, cathepsin B-cleavable CL2E linker. While the CL2E linker was designed for high stability in circulation, preclinical studies demonstrated that it was significantly less potent (approximately 40–55 times) than the related CL2A-linked conjugate, likely due to slower drug release following internalization. Consequently, development was deprioritized in favor of the CL2A-linked variant (epratuzumab-SN-38).
- Other names
- epratuzumab-CL2E-SN-38epratuzumab-CL-2E-SN-38epratuzumab-CL 2E-SN-38
02
Targets
CD22 (Cluster of Differentiation 22)TOP1 (DNA Topoisomerase I)
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