Anti-TAG-72/MMAE Antibody-drug Conjugate TGW101

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of a diabody directed against the tumor-associated antigen (TAA) tumor-associated glycoprotein 72 (TAG-72) site-specifically conjugated, via a trans-cyclooctene (TCO) cleavable linker, to the auristatin derivative and microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of anti-TAG-72/MMAE ADC TGW101, the anti-TAG-72 antibody moiety selectively targets and binds to tumor cells expressing TAG-72. Upon subsequent administration of the tetrazine-based trigger molecule TRG001, TRG001 selectively cleaves the chemical linker of tumor-bound TGW101 and releases MMAE directly within the tumor microenvironment (TME). Upon diffusion into nearby tumor cells, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in TAG-72-expressing tumor cells. TAG-72, a non-internalizing human pan-carcinoma antigen, is overexpressed on multiple epithelial-derived malignancies.

**Synonyms:** - Anti-TAG-72 ADC TGW101 - Anti-TAG-72 Antibody-drug Conjugate TGW101 - Anti-TAG-72/MMAE ADC TGW101 - Anti-TAG-72/MMAE TCO-linked Antibody-drug Conjugate TGW101 - Click-cleavable ADC TGW101 - TGW 101 - TGW-101 - TGW101