termsTerm
PBD dimer (SG3199 / tesirine)
aka pyrrolobenzodiazepine dimer, tesirine payload, SG3199
The PBD dimer SG3199 is an extremely potent DNA crosslinker that works at very low doses but has been hard to make tolerable; loncastuximab tesirine is the approved example.
Pyrrolobenzodiazepine dimers bind in the minor groove and crosslink DNA without distorting it, so cells struggle to detect and repair the damage. Potency is picomolar, allowing low drug-to-antibody ratios. Fluid retention, skin reactions and light sensitivity are characteristic, and several PBD programmes were stopped for toxicity (for example vadastuximab talirine). Loncastuximab tesirine in large B-cell lymphoma is the successful case.
Category
ADC chemistry
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