Table 3.
Detailed information on antibody-drug conjugates (ADCs) and ligand-targeted drugs.
| Name | Target | Linker | Payload | Indication | Current stage |
|---|---|---|---|---|---|
| Antibody–drug conjugates (ADCs) | |||||
| Gemtuzumab ozogamicin | CD33 | Cleavable hydrazone linker attached to random lysines | Calicheamicin | Acute myeloid leukemia | Approved by FDA for the treatment of newly diagnosed CD33-positive acute myeloid leukemia in 2017 |
| Trastuzumab emtansine | HER2 | Non-cleavable thioether linker attached to random lysines | DM1 | HER2+ metastatic breast cancer | Entered market in 2013 |
| Brentuximab vedotin | CD30 | Protease-cleavable linker attached to hinge cysteines | MMAE | Anaplastic large-cell lymphoma and Hodgkin lymphoma | Entered market in 2013 |
| Vadastuximab talirine | CD33 | Protease-cleavable linker attached to engineered heavy-chain cysteine (S239C) | SGD-1882 | Acute myeloid leukemia | PhaseIII for acute myeloid leukemia |
| Ligand-targeted therapeutic agents | |||||
| 177Lu-PSMA617 | PSMA | By labeling | 177Lu | Prostate cancer | PhaseII in progressive metastatic castration resistant prostate cancer |
| Vintafolide | FR | Disulphide bond linker | Vinblastine | Ovarian cancer; endometrial cancer; adenocarcinoma of the lung; solid tumor; non-small cell lung cancer | PhaseI for ovarian cancer, endometrial cancer has been completed; Phases I and II for non-small cell lung cancer, solid tumor have been completed |
| Ligand-targeted imaging agents | |||||
| Etarfolatide | FR | Peptide linker | Technetium-99m | FR-positive malignant diseases (e.g., lung, kidney, brain or ovarian cancer); autoimmune diseases | Phase III in FR-positive cancer |
| OTL38 | FR | peptide linker | NIR dye | Fluorescence-guided surgery | PhaseIII for fluorescence-guided surgery of ovarian, breast, lung and kidney cancers |