ADC Solid tumor indication
Target antigen Linker type (DAR) Cytotoxic payload
(payload action)
(date of approval)
MAH Pivotal trial(s)
(Phase: Clinical trial identifier)
Trastuzumab emtansine Locally advanced or metastatic HER2+ BC (≥2L) HER2 Non-cleavable thioether linker (DAR 3−4) Emtansine/DM1 (microtubule inhibitor) US (Feb 2013);
Switzerland (May 2013);
EU (Sept 2013)
Genentech/Roche EMILIA (phase III: NCT00829166) [@111503]
Early HER2+ BC post-neoadjuvant with no pCR US (May 2019);
EU (Nov 2019);
Switzerland (Jan 2020)
KATHERINE (phase III: NCT01772472) [@111504]
Trastuzumab deruxtecan* Unresectable or metastatic HER2+ BC (≥2L) HER2 Enzyme cleavable tetrapeptide-based linker (DAR 8) Deruxtecan (topoisomerase inhibitor) US (Aug 2019);
EU (Dec 2020);
Switzerland (Nov 2021)
Daiichi Sankyo/AstraZeneca DESTINY-Breast01 (phase II: NCT03248492) [@111515]
locally advanced or metastatic HER2+ G/GEJ adenocarcinoma US (Jan 2021) DESTINY-Gastric01 (phase II: NCT03329690) [@111576]
Sacituzumab govitecan* Metastatic TN BC (≥2L) Trop-2 Acid cleavable CL2A peptide linker (DAR 7.6) Govitecan/SN-38 (topoisomerase inhibitor) US (Apr 2020);
EU (Oct 2021);
Switzerland (Sept 2021)
Gilead Sciences ASCENT (phase III: NCT02574455) [@111505]
Locally advanced or metastatic UC (≥2L) US (Apr 2021) TROPHY U-01 (phase II: NCT03547973); TROPiCS-04 (phase III: NCT04527991) [@111514]
Enfortumab vedotin* Locally advanced or metastatic UC (≥2L) Nectin-4 Enzyme cleavable valine-citrulline linker (DAR 4) MMAE (microtubule inhibitor) US (Dec 2019);
Switzerland (Nov 2021)
Astellas/Seagen Inc. EV-301 (phase III: NCT03474107) [@111577]
Tisotumab vedotin* Recurrent or metastatic CC (≥2L) Tissue factor Enzyme cleavable linker (DAR 4) MMAE (microtubule inhibitor) US (Sept 2021) Seagen Inc. InnovaTV 204 (phase II: NCT03438396) [@111524]