termsTerm
Exatecan (and derivatives)
aka DX-8951, Ed-04, ZD06519, DX-8951; Ed-04 in iza-bren; ZD06519
Exatecan is a very potent camptothecin that is the parent of most next-generation ADC payloads, including those in iza-bren and several Chinese ADCs.
Exatecan (DX-8951) failed as a standalone chemotherapy because it was too toxic, but attached to an antibody its potency becomes an advantage. Deruxtecan, Ed-04 (izalontamab brengitecan), ZD06519 (Zymeworks) and other derivatives tune solubility, release and bystander behaviour. The class shares topoisomerase-I resistance mechanisms (TOP1 mutations, SLFN11 loss, efflux), so switching between exatecan-family ADCs after progression often disappoints.
Category
ADC chemistry