Chemical Linkers in Antibody–Drug Conjugates (ADCs)
The covalent conjugation of potent cytotoxic agents to monoclonal antibodies, known as antibody-drug conjugates (ADCs) is a powerful approach in the field of targeted treatment of cancer. Clearly, both monoclonal antibody and cytotoxic payload are crucial elements in determining the clinical value of an ADC and have receive ample attention. However, the structural element connecting the two –the chemical linker– also plays an essential role in mode-of-action, efficacy, pharmacokinetics and safety profile of an ADC, but is often underappreciated in considerations of ADC design.
Chemical Linkers in Antibody–Drug Conjugates aims to shine a detailed light on the various key attributes of chemical linkers in ADCs, for drug-to-antibody ratio, for stability, for release mechanism of payload, for pharmacokinetics, for stability determination, and for efficacy and safety. Ideal for postgraduate students and active researchers in drug discovery and development, this book provides a comprehensive description of linkers used in ADCs (clinical and late preclinical), insight into key quality attributes of linkers for ADCs, and aids the reader in understanding the role of linker chemistry and designing new ADCs.
Chemical Linkers in Antibody–Drug Conjugates (ADCs), The Royal Society of Chemistry, 2021.
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Table of contents
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Chapter 1: Introduction to Antibody–Drug Conjugatesp1-31ByJohn M. Lambert;John M. LambertHonorary Professor, Queen's University BelfastUKIndependent Consultant19 Chalk StreetCambridgeMA 02139USASearch for other works by this author on:F. L. van DelftF. L. van DelftSearch for other works by this author on:
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Chapter 2: Antibody Conjugation Technologiesp32-70ByG. T. Hermanson;G. T. HermansonQuantaBioDesign7470 Montgomery DrivePlain CityOH 43064USASearch for other works by this author on:F. L. van DelftF. L. van DelftSearch for other works by this author on:
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Chapter 3: Linker Design and Impact on ADC Propertiesp71-135ByN. CamperN. CamperSearch for other works by this author on:
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Chapter 4: Non-cleavable Linkers: Permanently Linked, for Better or for Worsep136-172ByNareshkumar JainNareshkumar JainSearch for other works by this author on:
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Chapter 5: Protease-sensitive Linkersp173-212ByH.-G. LerchenH.-G. LerchenSearch for other works by this author on:
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Chapter 6: Acid-labile Linkersp213-231ByC. E. BerkmanC. E. BerkmanSearch for other works by this author on:
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Chapter 7: ADC Linkers Strategies for the Release of Alcohol-containing Payloadsp232-262ByJared T. Miller;Jared T. MillerBinghamton University, School of Pharmacy and Pharmaceutical SciencesPO Box 6000BinghamtonNY 13902-6000USA[email protected]Search for other works by this author on:L. Nathan TumeyL. Nathan TumeyBinghamton University, School of Pharmacy and Pharmaceutical SciencesPO Box 6000BinghamtonNY 13902-6000USA[email protected]Search for other works by this author on:
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Chapter 8: Click-cleavable ADC Linkersp263-285ByM. S. RobillardM. S. RobillardSearch for other works by this author on:
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Chapter 9: The Use of Uniform PEG Compounds in the Design of ADCsp286-376ByP. D. DavisP. D. DavisSearch for other works by this author on:
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Chapter 10: Enhancing the Polarity of the Linker-drug in ADCsp377-421BySander S. van BerkelSander S. van BerkelSearch for other works by this author on:
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Chapter 11: Trastuzumab Deruxtecan Targeting HER2-expressing Cancers with a DXd-ADC System Consisting of a Novel Protease-sensitive Linker and DNA Topoisomerase I Inhibitor with a Hydroxyl Groupp422-450ByTakashi Nakada;Takashi NakadaDaiichi Sankyo Co., Ltd., Research Function R&D Division1-2-58 HiromachiShinagawa-kuTokyo 140-8710Japan[email protected]Search for other works by this author on:Yuki Abe;Yuki AbeDaiichi Sankyo Co., Ltd., Research Function R&D Division1-2-58 HiromachiShinagawa-kuTokyo 140-8710Japan[email protected]Search for other works by this author on:Toshinori AgatsumaToshinori AgatsumaDaiichi Sankyo Co., Ltd., Research Function R&D Division1-2-58 HiromachiShinagawa-kuTokyo 140-8710Japan[email protected]Search for other works by this author on:
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