TY - JOUR
T1 - Synthesis and evaluation of homocamptothecin antibody-drug conjugates for cancer treatment
AU - Li, Yalong
AU - Cheng, Zhiyang
AU - Zhou, Wei
AU - Wang, Lei
AU - Li, Xiaomei
AU - Xia, Guangxin
AU - Lu, Wei
AU - Zhu, Shulei
N1 - Publisher Copyright:
© 2024 Elsevier Masson SAS
PY - 2024/12/5
Y1 - 2024/12/5
N2 - As an emerging tumor therapeutic strategy, antibody-drug conjugates (ADCs) overcome the high toxicity of traditional small molecule chemotherapy and improve the targeting of treatment. In this study, we successfully constructed a novel ADC, Tras-16b, for the first time using homocamptothecin 16b as the payload. Tras-16b, at a dose of 3 mg/kg, exhibited comparable anti-tumor activity to Enhertu and demonstrated an enhanced safety profile in the NCI–N87 xenograft model. Notably, this is the first ADC developed based on homocamptothecin, marking a significant advancement with promising prospects for the structural modification of camptothecin ADCs.
AB - As an emerging tumor therapeutic strategy, antibody-drug conjugates (ADCs) overcome the high toxicity of traditional small molecule chemotherapy and improve the targeting of treatment. In this study, we successfully constructed a novel ADC, Tras-16b, for the first time using homocamptothecin 16b as the payload. Tras-16b, at a dose of 3 mg/kg, exhibited comparable anti-tumor activity to Enhertu and demonstrated an enhanced safety profile in the NCI–N87 xenograft model. Notably, this is the first ADC developed based on homocamptothecin, marking a significant advancement with promising prospects for the structural modification of camptothecin ADCs.
KW - Antibody-drug conjugates (ADCs)
KW - Cancer treatment
KW - Homocamptothecin
UR - https://www.scopus.com/pages/publications/85204430525
U2 - 10.1016/j.ejmech.2024.116899
DO - 10.1016/j.ejmech.2024.116899
M3 - 文章
C2 - 39321689
AN - SCOPUS:85204430525
SN - 0223-5234
VL - 279
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
M1 - 116899
ER -
