Table 3 Pharmacokinetic characteristics and schedule of administration of approved ADCs. Information about the FDA-approved medical indication, target and payload is also provided
Drug name | Condition | Target | Payload (MW) | Half-life | Dose | Frequency |
|---|---|---|---|---|---|---|
Belantamab mafodotin (Bienrep) | MM > 3 lines, including anti-CD38, proteasome inhibitor and one immunomodulator | BCMA | MMAF (732) | ADC: 11.5 days | 2.5 mg/kg (Max 125 mg) | Q3W |
cys-mcMMAF (925) | ||||||
Brentuximab vedotin (Adcetris) | HL Ill or IV treatment-naive | CD30 | MMAE (718) | ADC: 3.79–4.43 days | 1.8 mg/kg | Q3W |
Free drug: 3–4 days | ||||||
Enfortumab vedotin (Padcev) | Advanced urothelioma that has received anti-PD-(L)l and platinum | Nectin-4 | MMAE (718) | ADC: 3.4 days | 1.25 mg/kg | Days 1, 8 and 15 every 28 days |
Free drug: 2.4 days | ||||||
Gemtuzumab ozogamicin (Mylotarg) | AML CD33 + treatment-naïve Elderly, ECOG 2 | CD33 | Calicheamicin (1368) | ADC: 160h (6 days) | 3 mg/m2/dose | Days 1, 4 y 7 induction phase |
Inotuzumab ozogamicin (Besponsa) | Relapsed or refractory ALL CD22 + | CD22 | Calicheamicin (1368) | ADC: Cycle 1: 6 days Cycle 4: 13 days | First cycle: 1.8 mg/m2 Next cycles if complete response: 1.5 mg/m2 Next cycles if not complete response: 1.8 mg/m2 | First cycle: 0.8 mg/m2 day 1 0.5 mg/m2 day 8 and 15 After the first three weeks: 0.5 mg/m2 on days 1, 8 y 15 every 28 days in case of complete response |
Loncastuximab tesirine (Zynlonta) | DLBCL or HGBL. > 1 previous line | CD19 | SG3199 (585) | ADC: Cycle 1: 14.6 days Cycle 5: 20.8 days | 0.15 mg/kg in the first two cycles 0.075 mg/kg from cycle 3 on | Q3W |
Mirvetuximab soravtansine (Elahere) | Ovarian cancer. Platinum-resistant. 1–3 previous lines. FRa positive | FRa | DM4 (780) | ADC: 4 days | 6 mg/kg | Q3W |
Free drug: 2.6 days | ||||||
Polatuzumab vedotin (Polivy) | With rituximab, cyclophosphamide, doxorubicin, and prednisone (R-CHP) for adult patients who have previously untreated diffuse large B-cell lymphoma (DLBCL), not otherwise specified (NOS), or high-grade B-cell lymphoma (HGBL) and who have an InternationaI Prognostic Index (IPI) score of 2 or greater | CD79 | MIMAE (718) | ADC: 12 days (cycle 6) | 1.8 mg/kg | Q3W |
Free drug: 3.8 days (cycle 1) | ||||||
Sacituzumab govitecan (Trodelvy) | mTNBC > 2 previous lines. mLBC. Endocrine therapy, CDK-i and > 2 previous CT | Trop-2 | SN-38 (392) | ADC: 16h | 10 mg/kg | 1 and 8 every 21 days |
Total drug: 18h | ||||||
Free drug: 18h | ||||||
Metabolite: 15h | ||||||
Tisotumab vedotin (Tivdak) | Metastatic cervix uterii. 1–2 previous lines | Tissue factor | MMAE (718) | ADC: 4 days | 2 mg/kg (Max 200 mg) | Q3W |
Free drug: 2.6 days | ||||||
Trastuzumab Deruxtecan (Enhertu) | MBC HER2 + , previous line with a taxane and trastuzumab HER2 + eBC with residual disease after NACT with taxane and trastuzumab mCM HER2 + . Previous taxane and trastuzumab, no T-DMl | HER2 | DM1 (734) | ADC: 4 days | 3.6 mg/kg | Q3W |
Trastuzumab Emtansine (Kadcyla) | mCM HER2-low. HR + and HR-1–2 previous CT | HER2 | Dxd (1034) | ADC: 5.4–5.7 days | 5.4 mg/kg (breast and Iung) 6.4 mg/kg (gastric) | Q3W |
mNSCLC. HER2 activating mutations > lL CT Gastric o GEJ HER2 + . Previous trastuzumab, FluorP and platinum agent and > 2 L | Free drug: 5.4–6.1 days |