In vitro and in vivo evaluation of cysteine rebridged trastuzumab–MMAE antibody drug conjugates with defined drug-to-antibody ratios
P Bryant, M Pabst, G Badescu, M Bird… - Molecular …, 2015 - ACS Publications
The conjugation of monomethyl auristatin E (MMAE) to trastuzumab using a reduction bis-
alkylation approach that is capable of rebridging reduced (native) antibody interchain
disulfide bonds has been previously shown to produce a homogeneous and stable
conjugate with a drug-to-antibody ratio (DAR) of 4 as the major product. Here, we further
investigate the potency of the DAR 4 conjugates prepared by bis-alkylation by comparing to
lower drug loaded variants to maleimide linker based conjugates possessing typical mixed …
alkylation approach that is capable of rebridging reduced (native) antibody interchain
disulfide bonds has been previously shown to produce a homogeneous and stable
conjugate with a drug-to-antibody ratio (DAR) of 4 as the major product. Here, we further
investigate the potency of the DAR 4 conjugates prepared by bis-alkylation by comparing to
lower drug loaded variants to maleimide linker based conjugates possessing typical mixed …
[PDF][PDF] In Vitro and In Vivo Evaluation of Cysteine Rebridged Trastuzumab-MMAE Antibody Drug Conjugates With Defined DARs
EL Peciak, R Grygorash, A Kyle, D Morris, V Parekh… - researchgate.net
The conjugation of monomethyl auristatin E (MMAE) to trastuzumab using a reduction
bisalkylation approach that is capable of rebridging reduced (native) antibody interchain
disulfide bonds has been previously shown to produce a homogeneous and stable
conjugate with a drug to antibody ratio (DAR) of 4 as the major product. Here, we further
investigate the potency of the DAR 4 conjugates prepared by bis-alkylation by comparing to
lower drug loaded variants and to maleimide linker based conjugates possessing typical …
bisalkylation approach that is capable of rebridging reduced (native) antibody interchain
disulfide bonds has been previously shown to produce a homogeneous and stable
conjugate with a drug to antibody ratio (DAR) of 4 as the major product. Here, we further
investigate the potency of the DAR 4 conjugates prepared by bis-alkylation by comparing to
lower drug loaded variants and to maleimide linker based conjugates possessing typical …
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