Design, Synthesis, and Structure–Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody–Drug Conjugates

2020 ◽  
Vol 63 (22) ◽  
pp. 13913-13950
Author(s):  
Naidu S. Chowdari ◽  
Yong Zhang ◽  
Ivar McDonald ◽  
Walter Johnson ◽  
David R. Langley ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Antibody Drug Conjugates ◽  
Structure Activity Relationships ◽  
Drug Conjugates ◽  
Structure Activity ◽  
Antibody Drug

Design, synthesis and evaluation of novel, potent DNA alkylating agents and their antibody-drug conjugates (ADCs)

2019 ◽  
Vol 29 (17) ◽  
pp. 2455-2458
Author(s):  
Emily E. Reid ◽  
Katie E. Archer ◽  
Manami Shizuka ◽  
Molly A. McShea ◽  
Erin K. Maloney ◽  
...  
Keyword(s):  
Alkylating Agents ◽  
Design Synthesis ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Antibody Drug

scholarly journals Antibody-Drug Conjugates: The New Frontier of Chemotherapy

2020 ◽  
Vol 21 (15) ◽  
pp. 5510 ◽  
Author(s):  
Sara Ponziani ◽  
Giulia Di Vittorio ◽  
Giuseppina Pitari ◽  
Anna Maria Cimini ◽  
Matteo Ardini ◽  
...  
Keyword(s):  
First Generation ◽  
Antitumor Agents ◽  
Therapeutic Index ◽  
European Medicines Agency ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Recent Developments ◽  
Random Coupling ◽  
Personalized Cancer ◽  
Antibody Drug

In recent years, antibody-drug conjugates (ADCs) have become promising antitumor agents to be used as one of the tools in personalized cancer medicine. ADCs are comprised of a drug with cytotoxic activity cross-linked to a monoclonal antibody, targeting antigens expressed at higher levels on tumor cells than on normal cells. By providing a selective targeting mechanism for cytotoxic drugs, ADCs improve the therapeutic index in clinical practice. In this review, the chemistry of ADC linker conjugation together with strategies adopted to improve antibody tolerability (by reducing antigenicity) are examined, with particular attention to ADCs approved by the regulatory agencies (the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA)) for treating cancer patients. Recent developments in engineering Immunoglobulin (Ig) genes and antibody humanization have greatly reduced some of the problems of the first generation of ADCs, beset by problems, such as random coupling of the payload and immunogenicity of the antibody. ADC development and clinical use is a fast, evolving area, and will likely prove an important modality for the treatment of cancer in the near future.

Design, Synthesis, and Biological Evaluation of Antibody−Drug Conjugates Comprised of Potent Camptothecin Analogues

2009 ◽  
Vol 20 (6) ◽  
pp. 1242-1250 ◽  
Author(s):  
Patrick J. Burke ◽  
Peter D. Senter ◽  
David W. Meyer ◽  
Jamie B. Miyamoto ◽  
Martha Anderson ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Synthesis And Biological Evaluation ◽  
Camptothecin Analogues ◽  
Antibody Drug
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