Table 2.
Discontinued antibody–drug conjugates for patients with metastatic breast cancer.
| Drug | Target | Antibody | Linker-payload | DAR | Patient cohort | Main reason for discontinuation |
|---|---|---|---|---|---|---|
| PF-06664178 | Trop-2 | RN926 | AcLys-VCAur0101 | 2 | BC, NSCLC, ovarian cancer | Toxicity |
| Trastuzumab tesirine conjugate (ADCT-502) | HER2 | Anti-HER2 IgG1 | Cathepsin B-cleavable valine-alanine PBD | 1.7 | BC, NSCLC, bladder cancer, gastroesophageal cancer | Narrow therapeutic index |
| XMT-1522 | HER2 | HT-19 | Dolaflexin, AF-HPA | 12 | BC, NSCLC, gastric cancer | Company’s decision due to the competitive environment for HER2-targeted therapies |
| Glembatumumab vedotin (CDX-011) | gpNMB | CR011 | vc-MMAE | 2.7 | BC | No significant advantage of response and survival for CDX-011 |
AF-HPA, auristatin F-hydroxypropylamide; BC, breast cancer; DAR, drug antibody ratio; HER2, human epidermal growth factor receptor 2; MMAE, monomethyl auristatin E; NSCLC, non-small cell lung cancer; PBD, pyrrolobenzodiazepines; VC, valine-citrulline.