termsTerm
DNA crosslinker payloads (PBD dimers)
aka pyrrolobenzodiazepine dimers, tesirine, talirine
PBD dimers are picomolar DNA crosslinkers: enormously potent, so ADCs carry very little, but the narrow safety margin has sunk most programmes.
PBD dimers crosslink DNA in the minor groove with little distortion, evading repair. The potency allows drug-to-antibody ratios near two, but fluid retention, skin and liver toxicity have ended several programmes. Loncastuximab tesirine remains the approved example.
Category
ADC chemistry
Pages like this
not linked directly; found by shared links- TermVal-Ala dipeptide
Shares PBD dimer (SG3199 / tesirine), Loncastuximab tesirine, Antibody-drug conjugate (ADC).
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