TY - JOUR
T1 - Enzymatic strategies for (near) clinical development of antibody-drug conjugates
AU - van Berkel, Sander S.
AU - van Delft, Floris L.
PY - 2018/12
Y1 - 2018/12
N2 - Target-specific killing of tumor cells with antibody-drug conjugates (ADCs) is an elegant concept in the continued fight against cancer. However, despite more than 20 years of clinical development, only four ADC have reached market approval, while at least 50 clinical programs were terminated early. The high attrition rate of ADCs may, at least in part, be attributed to heterogeneity and instability of conventional technologies. At present, various (chemo)enzymatic approaches for site-specific and stable conjugation of toxic payloads are making their way to the clinic, thereby potentially providing ADCs with increased therapeutic window.
AB - Target-specific killing of tumor cells with antibody-drug conjugates (ADCs) is an elegant concept in the continued fight against cancer. However, despite more than 20 years of clinical development, only four ADC have reached market approval, while at least 50 clinical programs were terminated early. The high attrition rate of ADCs may, at least in part, be attributed to heterogeneity and instability of conventional technologies. At present, various (chemo)enzymatic approaches for site-specific and stable conjugation of toxic payloads are making their way to the clinic, thereby potentially providing ADCs with increased therapeutic window.
U2 - 10.1016/j.ddtec.2018.09.005
DO - 10.1016/j.ddtec.2018.09.005
M3 - Article
AN - SCOPUS:85054586144
SN - 1740-6749
VL - 30
SP - 3
EP - 10
JO - Drug Discovery Today: Technologies
JF - Drug Discovery Today: Technologies
ER -