- Generic nameOlintatug Tesirine
[Antineoplastic Antibody-Drug Conjugate]
- Synonyms
ADCT-901
- Target
- Highest phase
Phase 1
- NCI
An antibody-drug conjugate (ADC) composed of olintatug, a humanized monoclonal antibody directed against human kidney associated antigen 1 (KAAG1; RU2) and conjugated, through a cathepsin-cleavable linker, to SG3199, a cytotoxic pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration of olintatug tesirine, the anti-KAAG1 antibody moiety targets and binds to KAAG1, which is expressed on the surfaces of a variety of cancer cell types. Upon endocytosis and enzymatic cleavage by cathepsin, free PBD is released and forms highly cytotoxic DNA interstrand cross-links, thereby blocking cell division and killing KAAG1-expressing cancer cells. KAAG1, overexpressed by certain tumor cell types, plays a key role in tumor cell proliferation. Its expression on healthy tissue is very restricted.
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