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Location Matters: Site of Conjugation Modulates Stability and Pharmacokinetics of Antibody Drug Conjugates
Authors:Pavel Strop,Shu-Hui Liu,Magdalena Dorywalska,Kathy Delaria,Russell   G. Dushin,Thomas-Toan Tran,Wei-Hsien Ho,Santiago Farias,Meritxell   Galindo Casas,Yasmina Abdiche,Dahui Zhou,Ramalakshmi Chandrasekaran,Caroline Samain,Carole Loo,Andrea Rossi,Mathias Rickert,Stellanie Krimm,Teresa Wong,Arvind Rajpal
Affiliation:1. Rinat-Pfizer, 230 East Grand Avenue, South San Francisco, CA 94080, USA;2. Medicinal Chemistry, Pfizer, 445 Eastern Point Road, Groton, CT 06340, USA;3. Oncology Research Unit, Pfizer, 401 North Middletown Road, Pearl River, NY 10965, USA
Abstract:
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  • Highlights? Site-specific conjugation of diverse payloads can be achieved with transglutaminase ? Efficient conjugation was achieved at multiple positions throughout an antibody ? Site of conjugation has significant impact on ADC stability and pharmacokinetics ? Differences in ADC stability and pharmacokinetics are species dependent
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