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 | |||
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.