Anti-TROP2 Antibody-drug Conjugate ESG401

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of sacituzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) covalently linked via the protease-labile linker maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl (MC-VC-PABC), to the topoisomerase-1 inhibitor and the active metabolite of irinotecan 7-ethyl-10-hydroxycamptothecin (SN-38), with potential antineoplastic activity. Upon administration of the anti-TROP-2 ADC ESG401, the anti-TROP-2 antibody targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and proteolytic cleavage, SN-38 is released, selectively stabilizes topoisomerase I-DNA covalent complexes, resulting in DNA breaks and an inhibition of DNA replication and induction of apoptosis. This inhibits the proliferation of TROP-2-expressing tumor cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.

**Synonyms:** - ADC ESG401 - Anti-TROP-2 ADC ESG401 - Anti-TROP2 ADC ESG401 - Anti-TROP2/SN-38 ADC ESG401 - Anti-TROP2/SN-38 Antibody-drug Conjugate ESG401 - ESG 401 - ESG-401 - ESG401