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 …

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 …

The pharmacologic basis for antibody-auristatin conjugate activity

SC Alley, X Zhang, NM Okeley, M Anderson… - … of Pharmacology and …, 2009 - ASPET
Antibody-drug conjugates (ADCs) made with auristatin antimitotic agents have shown
significant preclinical and clinical oncology activity. SGN-75 is composed of the anti-CD70 …

Site-specific conjugation of monomethyl auristatin E to anti-CD30 antibodies improves their pharmacokinetics and therapeutic index in rodent models

F Lhospice, D Brégeon, C Belmant… - Molecular …, 2015 - ACS Publications
Antibody–drug conjugates (ADCs) have demonstrated clinical benefits that have led to the
recent FDA approval of KADCYLA and ADCETRIS. Most ADCs that are currently in clinical …

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 …

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 …

DCDT2980S, an anti-CD22-monomethyl auristatin E antibody–drug conjugate, is a potential treatment for non-Hodgkin lymphoma

D Li, KA Poon, SF Yu, R Dere, MA Go, J Lau… - Molecular cancer …, 2013 - AACR
Abstract Antibody–drug conjugates (ADC), potent cytotoxic drugs linked to antibodies via
chemical linkers, allow specific targeting of drugs to neoplastic cells. We have used this …

Effect of attachment site on stability of cleavable antibody drug conjugates

M Dorywalska, P Strop, JA Melton-Witt… - Bioconjugate …, 2015 - ACS Publications
The systemic stability of the antibody–drug linker is crucial for delivery of an intact antibody–
drug conjugate (ADC) to target-expressing tumors. Linkers stable in circulation but readily …

A novel anti-CD22 anthracycline-based antibody–drug conjugate (ADC) that overcomes resistance to auristatin-based ADCs

SF Yu, B Zheng, MA Go, J Lau, S Spencer, H Raab… - Clinical Cancer …, 2015 - AACR
Purpose: We are interested in identifying mechanisms of resistance to the current generation
of antibody–drug conjugates (ADC) and developing ADCs that can overcome this …

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 …