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E3-SG3249
- Development stage
- Preclinical
- Lead developer
- IRBM
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
E3-SG3249 is a **potential first-in-class antibody-drug conjugate (ADC)** currently in preclinical development, designed to target and inhibit the thymic stromal lymphopoietin receptor (**TSLPR**, also known as CRLF2), primarily for the treatment of **Philadelphia chromosome-like (Ph-like) acute lymphoblastic leukemia (ALL)**. The ADC consists of a monoclonal antibody (AM E3) specific for CRLF2/TSLPR, conjugated via a cathepsin B-cleavable valine-alanine linker to the pyrrolobenzodiazepine (PBD) dimer cytotoxic payload **tesirine (SG3249)**. This design enables **targeted delivery of a potent DNA cross-linking agent** specifically to leukemic cells overexpressing CRLF2/TSLPR, aiming to provide effective therapy for aggressive hematologic malignancies with high relapse rates, particularly affecting adolescents. Developed and presented by **IRBM**, E3-SG3249 is characterized by favorable pharmacologic and conjugation properties of its tesirine component[1][2][3][5][6][7].
- Other names
- AM E3-SG3249
02
Targets
DNATSLPR (TSLP receptor)
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