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Topoisomerase-I inhibitor payloads are the payload class behind Enhertu, Trodelvy and Dato-DXd: poisons that trap the enzyme that untwists DNA, so dividing cells break their own DNA.
Camptothecin derivatives (SN-38, DXd, exatecan and its children, T030) stabilise topoisomerase I on DNA. They are membrane permeable, so most give a bystander effect, and they tolerate high drug-to-antibody ratios. The class shares resistance routes: TOP1 mutations, loss of SLFN11 and efflux pumps, which is why a second topoisomerase-I ADC after the first fails is often disappointing. Interstitial lung disease, neutropenia and diarrhoea are class toxicities that differ in weight between members.
Showing the molecule this term concerns: Sacituzumab govitecan.
Shares SN-38, Exatecan (and derivatives), DXd, Bystander effect (ADC).
Shares DXd, Raludotatug deruxtecan, Patritumab deruxtecan, Ifinatamab deruxtecan.
Shares Bystander effect (ADC), Payload (ADC), Sacituzumab govitecan, Trastuzumab deruxtecan.
Shares Drug efflux pumps (ABC transporters), ADC sequencing, Datopotamab deruxtecan, Sacituzumab govitecan.
Shares SN-38, Bystander effect (ADC), Sacituzumab govitecan, Antibody-drug conjugate (ADC).
Shares Tilatamig samrotecan, AK146D1, ADC sequencing, Izalontamab brengitecan.
Shares Izalontamab brengitecan, Datopotamab deruxtecan, Sacituzumab govitecan, Trastuzumab deruxtecan.
Shares Drug efflux pumps (ABC transporters), Izalontamab brengitecan, Sacituzumab tirumotecan, Antibody-drug conjugate (ADC).