As of now, a total of 17 ADC drugs have been approved and marketed globally, among which 5 are conjugated via lysine residues.
| Product Name | Company | Target | DAR | Toxin | Linker | Antibody Type | Payload Type |
| Mylotarg | Pfizer | CD33 | 2~3 | Calicheamicin | Disulfide Acid-cleavable |
IgG4 | DNA damaging agent |
| Kadcyla | Roche | Her2 | 3.5 | DM1 | SMCC Non-cleavable |
IgG1 | Microtubule inhibitor |
| Besponsa | Pfizer | CD22 | 5~7 | Calicheamicin | Disulfide Acid-cleavable |
IgG4 | DNA damaging agent |
| Akalux | Rakuten | EGFR | NA | IRDye700DX | Direct conjugation / photo-cleavable linker Non-cleavable |
IgG1 | Phototoxic agent |
| ELAHERE | ImmunoGen | FRα | 3.4 | DM4 | Sulfo-SPDB Reducible |
IgG1 | Microtubule inhibitor |
What is ado-trastuzumab emtansine?
Ado-trastuzumab emtansine is an antibody-drug conjugate (ADC) composed of trastuzumab (an anti-HER2 IgG1 antibody) and the microtubule inhibitor DM1 (a maytansine derivative), linked via a thioether linker. The drug binds to the HER2 receptor through its antibody component, blocking activation of the HER2 signaling pathway and thereby inhibiting tumor cell proliferation. After internalization by tumor cells, DM1 is released in the intracellular environment, where it binds to tubulin, disrupts the microtubule network, and induces cell cycle arrest and apoptotic cell death. Ado-trastuzumab emtansine is primarily used for the treatment of HER2-positive breast cancer, including early-stage and metastatic breast cancer.
| Item | Information |
| Product Name | Kadcyla |
| Generic Name | Ado-trastuzumab emtansine |
| Manufacturer | Roche |
| Indication | HER2-positive breast cancer (for treatment of patients with previously treated HER2-positive metastatic breast cancer) |
| Target | HER2 |
| Dosage Form | Lyophilized powder |
| Strength | 100 mg, 160 mg/vial – 20 mg/mL |
| Reconstitution Solution Type | Buffer: 10 mM succinic acid |
| Stabilizer: 60 mg/mL sucrose | |
| Surfactant: 0.2 mg/mL polysorbate 20, pH 5.0 |
What is gemtuzumab ozogamicin?
Gemtuzumab ozogamicin is an antibody-drug conjugate (ADC) targeting CD33, composed of a humanized monoclonal antibody against CD33 (IgG4 κ antibody hP67.6) covalently linked to the cytotoxic antitumor antibiotic calicheamicin (N-acetyl-γ-calicheamicin) via a bifunctional linker. The drug binds to CD33-positive leukemia cells through its antibody component and is subsequently internalized into the cells. Inside the cell, the linker is cleaved by lysosomal enzymes, releasing calicheamicin, which induces DNA double-strand breaks, leading to cell cycle arrest and apoptosis. Gemtuzumab ozogamicin is used for the treatment of CD33-positive acute myeloid leukemia (AML), including both newly diagnosed and relapsed or refractory patients.
| Item | Information |
| Product Name | Mylotarg |
| Generic Name | Gemtuzumab ozogamicin |
| Manufacturer | Pfizer (USA) |
| Indication | CD33-positive acute myeloid leukemia |
| Target | CD33 |
| Dosage Form | Lyophilized powder |
| Strength | 4.5 mg/vial – 1 mg/mL |
| Reconstitution Solution Type | Buffer: 5 mM sodium succinate |
| Stabilizer: 14 mg/mL sucrose, 8 mg/mL polysorbate 40 | |
| Surfactant: None, pH 7.4 |
What is inotuzumab ozogamicin?
Inotuzumab ozogamicin is a CD22-targeted ADC composed of a humanized monoclonal antibody (IgG4 κ) against CD22, linked to the cytotoxic agent ozogamicin (N-acetyl-γ-calicheamicin dimethyl hydrazide) via an AcBut linker. The drug binds to CD22-positive cells and is internalized. Within the lysosome, the linker is cleaved to release ozogamicin, which causes DNA damage leading to cell death. Inotuzumab ozogamicin is used to treat relapsed or refractory CD22-positive B-cell acute lymphoblastic leukemia (ALL).
| Item | Description |
| Brand Name | Besponsa (Inotuzumab Ozogamicin) |
| Generic Name | Inotuzumab Ozogamicin |
| Manufacturer | Pfizer Inc. (Wyeth Pharma, a Pfizer subsidiary) |
| Indication | Besponsa is indicated for the treatment of adult patients with relapsed or refractory B-cell precursor acute lymphoblastic leukemia (ALL). |
| Target | CD22 |
| Form | Lyophilized Powder |
| Specification | 1 mg/vial, 0.25 mg/mL |
| Reconstitution Solution Type | Buffer: 18 mM tris(hydroxymethyl)aminomethane |
| Stabilizer: 45 mg/mL sucrose, 5 mg/mL sodium chloride | |
| Surfactant: 0.1 mg/mL polysorbate 80, pH 8.0 |
What is cetuximab sarotalocan?
Cetuximab sarotalocan is an ADC composed of a monoclonal antibody (IgG1) targeting the epidermal growth factor receptor (EGFR), conjugated to the cytotoxic agent sarotalocan (a topoisomerase I inhibitor) via a cleavable linker. The drug binds to EGFR-positive tumor cells via the antibody portion and is subsequently internalized. Inside the cell, the linker is cleaved, releasing sarotalocan, which induces DNA damage and cell death by inhibiting topoisomerase I. Cetuximab sarotalocan is used to treat EGFR-positive solid tumors, including colorectal cancer and squamous cell carcinoma of the head and neck.
| Item | Description |
| Brand Name | Akalux |
| Generic Name | Cetuximab Sarotalocan |
| Manufacturer | Rakuten |
| Indication | Colorectal Cancer, Head and Neck Cancer |
| Target | EGFR |
| Form | Lyophilized Powder |
| Specification | 250 mg/vial, 5 mg/mL |
| Reconstitution Solution Type | Buffer: 10 mM Phosphate |
| Stabilizer: 90 mg/mL Trehalose | |
| Surfactant: 0.2 mg/mL Polysorbate 80, pH 7.1 |
What is mirvetuximab soravtansine-gynx?
Mirvetuximab soravtansine-gynx is a folate receptor alpha (FRα)-targeted ADC composed of a monoclonal antibody against FRα, a cleavable linker, and the cytotoxic agent DM4, a microtubule inhibitor. The antibody is a chimeric IgG1, conjugated to DM4 via a cleavable linker. After binding to FRα, the ADC is internalized, and DM4 is released inside the cell through proteolytic cleavage. DM4 disrupts the microtubule network, leading to cell cycle arrest and apoptotic cell death. This drug is used to treat FRα-positive ovarian cancer, particularly in patients with platinum-resistant epithelial ovarian, fallopian tube, or primary peritoneal cancer.
| Item | Description |
| Brand Name | Elahere |
| Generic Name | Mirvetuximab Soravtansine-gynx |
| Indication | Epithelial Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer |
| Target | Folate Receptorα (FRα) |
| Form | Injection |
| Specification | 100 mg/vial, 5 mg/mL |
| Reconstitution Solution Type | Buffer: 0.22 mg/mL Glacial Acetic Acid, 0.53 mg/mL Sodium Acetate |
| Stabilizer: 90 mg/mL Sucrose | |
| Surfactant: 0.1 mg/mL Polysorbate 20, pH 5.0 |
ADCs Cytotoxin at BOC Sciences
Featured products at BOC Sciences
| Catalog | Product Name | CAS Number |
| B2696-096388 | SMCC | 64987-85-5 |
| 1228105-52-9 | DM4-SMCC | 1228105-52-9 |
| 400647-59-8 | Doxorubicin-SMCC | 400647-59-8 |
| B0238-477036 | DM1-SMCC | 1228105-51-8 |
| B2699-079694 | Sulfo-SMCC sodium | 92921-24-9 |
| 115088-06-7 | SPDB | 115088-06-7 |
| 1626359-59-8 | sulfo-SPDB-DM4 | 1626359-59-8 |
| B0238-477039 | DM4-SPDB | 1626359-62-3 |