Table 1 Primary specifics of ADCs currently approved worldwide in treating solid tumors
From: The promise and challenges of combination therapies with antibody-drug conjugates in solid tumors
Drug name | Target | mAb | Linker | Payload | Indications | Year of Approval | Efficacy | DAR | Regimen |
|---|---|---|---|---|---|---|---|---|---|
Kadcyla® (ado-trastuzumab emtansine) | HER2 | IgG1 | SMCC | DM1 | HER2 + metastatic BC previously treated with trastuzumab & a taxane | 2013 | T-DM1 vs. capecitabine-lapatinib; mOS 30.9 vs. 25.1 mo (HR 0.65; 95% CI 0.64–0.88); mPFS 9.6 vs. 6.4 mo (HR 0.65; 95% CI 0.55–0.77) | 3.5 | 3.6 mg/kg, Q3W |
HER2 + early BC after neoadjuvant taxane & trastuzumab-based treatment | 2019 | T-DM1 vs. trastuzumab; 3y iDFS 88.3% vs. 77% (HR 0.5; 95% CI 0.39–0.64) | |||||||
Enhertu®(famtrastuzumab deruxtecannxki) | HER2 | IgG1 | GGFG | DXd | Unresectable or metastatic HER2 + BC after 2 or more anti-HER2 regimens | 2019 | Single-arm ORR = 61.4% | 8 | 6.4 mg/kg, Q3W |
Locally advanced or metastatic HER2 + gastric or gastroesophageal junction adenocarcinoma after a trastuzumab-based regimen | 2021 | T-DXd vs. CT, ORR: 51% vs. 14% | |||||||
Aidixi ®(Disitamab vedotin) | HER2 | IgG1 | MC-VA-PABC | MMAE | HER2 + (IHC 3 + or 2 +) locally advanced or metastatic UC who previously failed at least one line of CT | 2020 | Single-arm ORR = 51.2%; mPFS = 6.9mo | 4 | 2.5 mg/kg, Q2W |
HER2-overexpressing (IHC 2 + or 3 +), locally advanced or metastatic GC/GEJC who were under at least second-line therapy | 2021 | Single-arm ORR = 24.8% | |||||||
Padcev® (enfortumab vedotin-ejfv) | Nectin-4 | IgG1 | MC-VC-PABC | MMAE | Locally advanced or metastatic UC who were previously treated with platinum CT and anti-PD-1/L1 therapy | 2019 | Single-arm ORR = 44% | 3.8 | 1.25 mg/kg on days 1, 8 and 15, Q4W |
Trodelvy® (sacituzumab govitecan hziy) | TROP2 | IgG1 | CL2A | SN38 | Locally advanced or metastatic TNBC after at least two prior therapies | 2020 | SG vs.CT; mPFS 5.6 vs. 1.7 mo (HR 0.41; 95% CI 0.32–0.52) | 7.6 | 10 mg/kg, days 1 and 8, Q3W |
Akalux® (cetuximab saratolacan sodium) | EGFR | IgG1 | N/A | IRDye/700DX | Unresectable locally advanced or recurrent head and neck cancer | 2020 | Single-arm ORR = 26.7% | NA | 640 mg/m2, and the light dose was fixed at 50 J/cm2 for superficial tumors and 100 J/cm2 fiber diffuser length for interstitial tumors |
Tivdak®(tisotumab vedotin-tftv) | TF | IgG1 | MC-VC-PABC | MMAE | Recurrent or metastatic cervical cancer with disease progression on or after CT | 2021 | Single-arm ORR = 24% | 4 | 2 mg/kg (up to a maximum of 200 mg for patients weighing ≥ 100 kg), Q3W |
Elahere®(mirvetuximab soravtansine-gynx) | FRα | IgG1 | sulfoSPDB | DM4 | High-grade serous epithelial ovarian cancer, primary peritoneal, or fallopian tube cancer | 2022 | Single-arm ORR = 32.4% | 3.4 | 6 mg/kg using adjusted ideal body weight, Q3W |