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PBD dimers (tesirine, talirine) are DNA crosslinkers that kill at picomolar concentrations, so ADCs need a drug-to-antibody ratio of only about two. Fluid retention and skin and liver toxicity have ended most programmes; loncastuximab tesirine is the approved example.
PBD dimers, the pyrrolobenzodiazepine dimers also known as tesirine and talirine, are picomolar DNA crosslinkers: they kill at such low concentrations that ADCs carry only about two molecules per antibody, but their narrow safety margin has sunk most programmes. They crosslink DNA in the minor groove with little distortion of the helix, which lets the damage evade repair. The potency allows drug-to-antibody ratios near two, yet fluid retention and skin and liver toxicity have ended several programmes, and Loncastuximab tesirine remains the approved example. The class belongs to the Antibody-drug conjugate (ADC) technology and the Payload (ADC) term, and it is referenced by the specific payload record PBD dimer (SG3199 / tesirine).
Showing the molecule this term concerns: Loncastuximab tesirine.
Shares PBD dimer (SG3199 / tesirine), Loncastuximab tesirine, Antibody-drug conjugate (ADC).
Shares Loncastuximab tesirine, Antibody-drug conjugate (ADC).
Shares Loncastuximab tesirine, Antibody-drug conjugate (ADC).
Shares Loncastuximab tesirine, Antibody-drug conjugate (ADC).