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SN-38 is the active form of the chemotherapy irinotecan and the payload of sacituzumab govitecan. It blocks topoisomerase I so DNA breaks during copying, but it kills cells only at nanomolar concentrations, so the ADC carries roughly eight copies per antibody and uses a linker that releases it in the tumour; slow metabolisers (UGT1A1*28) get more diarrhoea.
SN-38 blocks topoisomerase I, the enzyme that relieves twisting in DNA during copying, so the copying machinery collides with trapped complexes and the DNA breaks. It is about a thousand times more potent than irinotecan itself but only nanomolar, which is why sacituzumab govitecan carries roughly eight copies per antibody and uses a linker that lets go in the tumour environment. It is pumped out by the ABCG2 transporter, one route to resistance, and people who metabolise it slowly (UGT1A1*28) get more diarrhoea and low blood counts.
Showing the molecule this term concerns: Sacituzumab govitecan.
Shares Topoisomerase-I inhibitor payloads, Drug efflux pumps (ABC transporters), Payload (ADC), Topoisomerase-I inhibitors (and ADC payloads).
Shares Topoisomerase-I inhibitor payloads, Drug efflux pumps (ABC transporters), DNA replication & origin licensing, Drug efflux pumps (ABC transporters).
Shares Topoisomerase-I inhibitor payloads, DNA replication & origin licensing, Drug efflux pumps (ABC transporters), Payload (ADC).
Shares CL2A, Topoisomerase-I inhibitor payloads, Drug efflux pumps (ABC transporters), Sacituzumab govitecan.
Shares Sacituzumab govitecan, Topoisomerase-I inhibitors (and ADC payloads), Antibody-drug conjugate (ADC).
Shares Sacituzumab govitecan, Topoisomerase-I inhibitors (and ADC payloads), Antibody-drug conjugate (ADC).
Shares Sacituzumab govitecan, Topoisomerase-I inhibitors (and ADC payloads), Antibody-drug conjugate (ADC).
Shares Drug efflux pumps (ABC transporters), Drug efflux pumps (ABC transporters), Payload (ADC), Antibody-drug conjugate (ADC).