OnCo
termsTerm

Drug-to-antibody ratio (DAR)

The drug-to-antibody ratio (DAR) is how many payload molecules ride on each antibody, typically 2 to 8.

Higher DAR delivers more drug per binding event (T-DXd ~8, sacituzumab ~7.6) but increases hydrophobicity, aggregation, and clearance unless hydrophilic linkers are used. Homogeneous DAR from site-specific conjugation improves pharmacokinetics.

ADC: what this kind of term is about · animated schematic, not to scale
Category
ADC

Key papers

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rctNew England Journal of Medicine 2022changed practice
DESTINY-Breast03: trastuzumab deruxtecan beats T-DM1 as second-line treatment of HER2-positive metastatic breast cancer

For HER2-positive metastatic breast cancer that has progressed after trastuzumab and a taxane, trastuzumab deruxtecan is now the standard second-line treatment and T-DM1 has moved later in the sequence. The benefit is large enough that ADC design, not just the target, is understood to be what matters. Patients need lung monitoring because of the risk of pneumonitis.

Connected

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Pages like this

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technologies

2
Antibody-drug conjugate (ADC)Site-specific conjugation & linker chemistry

terms

1
Hydrophilic next-generation linkers (TMALIN, Dolaflexin, sulfonyl-pyrimidine, PEG-containing)

ideas

1
Dose and schedule optimisation trials specific to antibody-drug conjugates

key papers

1
DESTINY-Breast03: trastuzumab deruxtecan beats T-DM1 as second-line treatment of HER2-positive metastatic breast cancer