termsTerm
Acid-labile hydrazone (AcBut)
aka acid-cleavable linker
The hydrazone linker is acid-sensitive and breaks in the lysosome's low pH. It was used in the calicheamicin ADCs, but is too leaky for most modern designs.
Hydrazone linkers hydrolyse at pH 4 to 5 and are relatively unstable in plasma, contributing to the off-target toxicity of first-generation ADCs. Gemtuzumab ozogamicin and inotuzumab ozogamicin use a hydrazone combined with a disulfide.
Category
ADC chemistry
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Shares Calicheamicin, Gemtuzumab ozogamicin, Antibody-drug conjugate (ADC).
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Shares Gemtuzumab ozogamicin, Antibody-drug conjugate (ADC).
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Shares Gemtuzumab ozogamicin, Antibody-drug conjugate (ADC).