DXd
DXd is the topoisomerase poison inside Enhertu and Dato-DXd: about ten times stronger than SN-38, it spreads to neighbouring cells and leaves the body quickly once released.
DXd is a derivative of exatecan. Its potency allows a drug-to-antibody ratio of eight while remaining tolerable, and because the free payload crosses membranes it kills nearby cells that lack the target (the bystander effect), which is why Enhertu works in HER2-low disease. Its short half-life once released limits systemic exposure. Interstitial lung disease is the characteristic toxicity of the DXd platform. It is a partial substrate for efflux pumps, so payload resistance can be shared with other topoisomerase-I ADCs.
Pages like this
not linked directly; found by shared links- TermSN-38
Shares Topoisomerase-I inhibitor payloads, Drug efflux pumps (ABC transporters), DNA replication & origin licensing, Drug efflux pumps (ABC transporters).
- TermT030 (belotecan derivative)
Shares Topoisomerase-I inhibitor payloads, Drug efflux pumps (ABC transporters), Payload (ADC), Topoisomerase-I inhibitors (and ADC payloads).
- TermExatecan (and derivatives)
Shares Topoisomerase-I inhibitor payloads, DNA replication & origin licensing, Drug efflux pumps (ABC transporters), Payload (ADC).
- IdeaTumour-on-a-chip with blood flow to test whether big drugs actually get in
Shares Bystander effect (ADC), Payload (ADC), Trastuzumab deruxtecan, Antibody-drug conjugate (ADC).
- TermMMAE
Shares Bystander effect (ADC), Drug efflux pumps (ABC transporters), Drug efflux pumps (ABC transporters), Payload (ADC).
- IdeaDose and schedule optimisation trials specific to antibody-drug conjugates
Shares Interstitial lung disease (ILD) / pneumonitis, Payload (ADC), Trastuzumab deruxtecan, Antibody-drug conjugate (ADC).
- IdeaLinked human organ chips to predict side effects before people are dosed
Shares Interstitial lung disease (ILD) / pneumonitis, Payload (ADC), Antibody-drug conjugate (ADC).
- PairingCaution: DXd ADC + agents with pneumonitis risk
Shares Interstitial lung disease (ILD) / pneumonitis, Datopotamab deruxtecan, Trastuzumab deruxtecan.