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. 2023 Nov 29;30(12):10211–10223. doi: 10.3390/curroncol30120743

Table 1.

Completed phase III clinical trials involving antibody drug conjugates.

Trastuzumab Emantasine (T-DM1) Trastuzumab Deruxtecan (T-DXd) Sacituzumab Govitecan (SG)
Target antigen HER2 HER2 Trop-2
Linker cleavage No Enzymatic pH-dependent and enzymatic
Membrane-permeable Payload? No Yes Yes
hydrophobic low
Payload/mechanism of action Maytansine/
Tubulin inhibitor
Deruxtecan/
Topoisomerase 1 inhibitor
SN-38/
Topoisomerase 1 inhibitor
Drug–antibody ratio (DAR) 3.5:1 8:1 7.6:1
Phase III Setting
  • HER2-positive ABC 2L [4]

  • Post-neoadjuvant residual disease [5]

  • HER2-positive ABC 3L [14]

  • HER2- positive ABC 2L [13]

  • HER2-low ABC 2L [21]

  • TNBC ABC 2L [18]

  • ER/PR+ ABC ≥ 2L [20]

Common AE fatigue, nausea, musculoskeletal pain, thrombocytopenia, headache, elevated transaminases, reduction in LVEF nausea, leukopenia, anemia, thrombocytopenia, elevated transaminases, diarrhea, hypokalemia, cough neutropenia, nausea, diarrhea, fatigue, alopecia, anemia, vomiting, constipation, decreased appetite, rash, abdominal pain

Abbreviations: Advanced breast cancer—ABC; Triple-negative breast cancer—TNBC; prior lines of therapy—L; left ventricular ejection fraction—LVEF.