Skip to main content
. Author manuscript; available in PMC: 2022 Jan 14.
Published in final edited form as: J Med Chem. 2020 Dec 31;64(1):216–232. doi: 10.1021/acs.jmedchem.0c01530

Table 1.

Linker Chemistries of the ADCs Approved for Clinical Use

ADC Linker Chemistry Year approved

Enzyme cleavable
Brentuximab vedotin (Adcetris) carbamate, dipeptide, thioether 2011
Polatuzumab vedotin (Polivy) carbamate, dipeptide, thioether 2019
Enfortumab vedotin (Padcev) carbamate, dipeptide, thioether 2019
Trastuzumab deruxtecan (Enhertu) amide, tripeptide, thioether 2019
Trastuzumab emtansine (Kadcyla) thioether, amide 2013

Enzyme or acid cleavable/ Reducible disulfide
Gemtuzumab ozogamicin (Mylotarg) disulfide, hydrazone, amide 2000*
Inotuzumab ozogamicin (Besponza) disulfide, hydrazone, amide 2017

Acid cleavable
Sacituzumab govitecan (Trodelvy) carbonate, triazole, thioether 2020
*

It was taken off market in 2010 and reapproved in 2017