# Exatecan (and derivatives)

Source: https://onco.cc/terms/exatecan/  
OnCo record `exatecan` (Term). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Summary

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.

## Fields

- Kind: Term
- Last checked: 2026-09-09
- Also known as: DX-8951; Ed-04; ZD06519; DX-8951; Ed-04 in iza-bren; ZD06519

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Exatecan
- Wikipedia: https://en.wikipedia.org/wiki/Exatecan

## Connected records

- technologies: [Antibody-drug conjugate (ADC)](https://onco.cc/technologies/adc/), [Topoisomerase-I inhibitors (and ADC payloads)](https://onco.cc/technologies/topoisomerase-inhibitors/)
- terms: [ADC sequencing](https://onco.cc/terms/adc-sequencing/), [Payload (ADC)](https://onco.cc/terms/payload/), [Topoisomerase-I inhibitor payloads](https://onco.cc/terms/topoisomerase-i-payloads/)
- drugs: [AK146D1](https://onco.cc/drugs/ak146d1/), [Izalontamab brengitecan](https://onco.cc/drugs/izalontamab-brengitecan/), [Puxitatug samrotecan](https://onco.cc/drugs/puxitatug-samrotecan/), [Tilatamig samrotecan](https://onco.cc/drugs/tilatamig-samrotecan/)
- pathways: [DNA replication & origin licensing](https://onco.cc/pathways/dna-replication-licensing/), [Drug efflux pumps (ABC transporters)](https://onco.cc/pathways/drug-efflux-pumps/)

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JSON: https://onco.cc/api/v1/entities/exatecan.json