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Exatecan is a camptothecin that blocks topoisomerase I; it was too toxic to use as a free chemotherapy, but attached to an antibody that toxicity becomes useful, and it is the parent of deruxtecan and most next-generation ADC payloads. The family shares resistance mechanisms, so switching between exatecan ADCs after progression often disappoints.
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.
Iza-bren (Ed-04) carries a camptothecin-derived TOP1 inhibitor; exatecan shown as the class representative.
Showing the molecule this term concerns: Izalontamab brengitecan.
Shares Topoisomerase-I inhibitor payloads, DNA replication & origin licensing, Drug efflux pumps (ABC transporters), Payload (ADC).
Shares Topoisomerase-I inhibitor payloads, DNA replication & origin licensing, Drug efflux pumps (ABC transporters), Payload (ADC).
Shares Topoisomerase-I inhibitor payloads, Payload (ADC), Topoisomerase-I inhibitors (and ADC payloads), Antibody-drug conjugate (ADC).
Shares ADC sequencing, Payload (ADC), Topoisomerase-I inhibitors (and ADC payloads), Antibody-drug conjugate (ADC).
Shares Tilatamig samrotecan, AK146D1, ADC sequencing, Izalontamab brengitecan.