Lysosomal trafficking and cysteine protease metabolism confer target-specific cytotoxicity by peptide-linked anti-CD30-auristatin conjugates

MSK Sutherland, RJ Sanderson, KA Gordon… - Journal of Biological …, 2006 - ASBMB
The chimeric anti-CD30 monoclonal antibody cAC10, linked to the antimitotic agents
monomethyl auristatin E (MMAE) or F (MMAF), produces potent and highly CD30-selective …

Engineered antibody–drug conjugates with defined sites and stoichiometries of drug attachment

CF McDonagh, E Turcott, L Westendorf… - Protein Engineering …, 2006 - academic.oup.com
The chimeric anti-CD30 IgG1, cAC10, conjugated to eight equivalents of monomethyl
auristatin E (MMAE) was previously shown to have potent antitumor activity against CD30 …

Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity

SO Doronina, BA Mendelsohn, TD Bovee… - Bioconjugate …, 2006 - ACS Publications
We have previously shown that antibody− drug conjugates (ADCs) consisting of cAC10 (anti-
CD30) linked to the antimitotic agent monomethylauristatin E (MMAE) lead to potent in vitro …

In vivo Drug-Linker Stability of an Anti-CD30 Dipeptide-Linked Auristatin Immunoconjugate

RJ Sanderson, MA Hering, SF James, MMC Sun… - Clinical cancer …, 2005 - AACR
Effective antibody-drug conjugates (ADC) combine high drug-linker stability in circulation
and efficient intratumoral release of drug. Conjugation of monomethyl auristatin E (MMAE) to …

cAC10-vcMMAE, an anti-CD30–monomethyl auristatin E conjugate with potent and selective antitumor activity

JA Francisco, CG Cerveny, DL Meyer, BJ Mixan… - Blood, 2003 - ashpublications.org
The chimeric monoclonal antibody cAC10, directed against CD30, induces growth arrest of
CD30+ cell lines in vitro and has pronounced antitumor activity in severe combined …

Anti-CD30 diabody-drug conjugates with potent antitumor activity

KM Kim, CF McDonagh, L Westendorf, LL Brown… - Molecular cancer …, 2008 - AACR
Anti-CD30 diabodies were engineered with two cysteine mutations for site-specific drug
conjugation in each chain of these homodimeric antibody fragments. Diabodies were …

Effects of drug loading on the antitumor activity of a monoclonal antibody drug conjugate

KJ Hamblett, PD Senter, DF Chace, MMC Sun… - Clinical cancer …, 2004 - AACR
Purpose: An antibody-drug conjugate consisting of monomethyl auristatin E (MMAE)
conjugated to the anti-CD30 monoclonal antibody (mAb) cAC10, with eight drug moieties …

Non‐internalizing antibody–drug conjugates display potent anti‐cancer activity upon proteolytic release of monomethyl auristatin E in the subendothelial extracellular …

R Gébleux, M Stringhini, R Casanova… - … journal of cancer, 2017 - Wiley Online Library
Antibody–drug conjugates (ADCs) represent a promising class of biopharmaceuticals with
the potential to localize at the tumor site and improve the therapeutic index of cytotoxic …

Potent cytotoxicity of an auristatin-containing antibody-drug conjugate targeting melanoma cells expressing melanotransferrin/p97

LM Smith, A Nesterova, SC Alley, MY Torgov… - Molecular cancer …, 2006 - AACR
Identifying factors that determine the sensitivity or resistance of cancer cells to cytotoxicity by
antibody-drug conjugates is essential in the development of such conjugates for therapy …

Development of potent monoclonal antibody auristatin conjugates for cancer therapy

SO Doronina, BE Toki, MY Torgov… - Nature …, 2003 - nature.com
We describe the in vitro and in vivo properties of monoclonal antibody (mAb)-drug
conjugates consisting of the potent synthetic dolastatin 10 analogs auristatin E (AE) and …