Preferred Label : Sacituzumab Tirumotecan;
NCIt synonyms : ADC SKB264; Anti-TROP2 Antibody-drug Conjugate MK-2870; ADC MK-2870; Anti-TROP2 Antibody-drug Conjugate SKB264;
NCIt definition : An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 kappa (IgG1k)
monoclonal antibody directed against the tumor-associated antigen (TAA) trophoblast
cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2;
TROP-2; TACSTD2; GA733-1; M1S1) conjugated, via a methyl sulfonyl pyrimidine linker,
to the belotecan derivative and topoisomerase I inhibitor tirumotecan, with potential
antineoplastic activity. Upon administration of sacituzumab tirumotecan, sacituzumab
targets and binds to TROP2 expressed on tumor cells. Upon both extracellular pH-sensitive
cleavage and intracellular enzymatic cleavage of the linker, tirumotecan is released
and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and
resulting in cell cycle arrest and apoptosis in tumor cells expressing TROP2. In addition,
the bystander effect induced by sacituzumab tirumotecan further inhibits tumor cell
proliferation. TROP2 is a transmembrane protein overexpressed in various tumors while
its expression is low and/or restricted in normal, healthy tissues; its expression
is associated with enhanced tumor aggressiveness, metastasis, drug resistance and
increased tumor cell survival.;
UNII : 3DV5TD1VL3;
CAS number : 2768350-77-0;
Molecule name : SKB 264; SKB-264; MK 2870; MK-2870;
NCI Metathesaurus CUI : CL971661;
Origin ID : C166409;
UMLS CUI : C5908084;
Semantic type(s)
- concept_is_in_subset
- has_target
