scholarly journals Antibody–drug conjugates as novel anti-cancer chemotherapeutics

2015 ◽  
Vol 35 (4) ◽  
Author(s):  
Christina Peters ◽  
Stuart Brown
Keyword(s):  
Monoclonal Antibodies ◽  
Small Molecule ◽  
Current Knowledge ◽  
Cytotoxic Agent ◽  
Cancer Drugs ◽  
Antibody Drug Conjugates ◽  
Cancer Chemotherapeutics ◽  
Drug Conjugates ◽  
Anti Cancer ◽  
Antibody Drug

Antibody drug conjugates (ADCs) are an efficacious class of anti-cancer drugs that comprise monoclonal antibodies (mAbs) conjugated to small-molecule cytotoxic agent via a stable linker. This review summarizes the current knowledge and developments in the field of ADCs.

Monoclonal antibodies, small molecule inhibitors and antibody-drug conjugates as HER2 inhibitors

2020 ◽  
Vol 27 ◽  
Author(s):  
Xiu-Fang Li ◽  
Chen-Fu Liu ◽  
Guo-Wu Rao
Keyword(s):  
Monoclonal Antibodies ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Growth Factor Receptor ◽  
Research Progress ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Her 2 ◽  
Epidermal Growth ◽  
Antibody Drug

: Overexpression of human epidermal growth factor receptor (HER)-2 is found in a variety of cancers, often portending poor clinical outcomes. Therefore, HER2 is an attractive target for treatment. This review describes the research progress of HER2 targeted inhibitors in recent years. Excellent reviews are available, so we focus on the development, mechanisms of action, and structure-activity relationships of different types of inhibitors, including monoclonal antibodies, small molecule inhibitors, and antibody-drug conjugates (ADCs). In addition, the differences among them are compared.

Translational aspects of biologicals: monoclonal antibodies and antibody-drug conjugates as examples

2021 ◽  
pp. 329-350
Author(s):  
Sophia N. Karagiannis ◽  
Ricarda M. Hoffmann ◽  
Mano Nakamura ◽  
Silvia Crescioli ◽  
Heather J. Bax ◽  
...  
Keyword(s):  
Monoclonal Antibodies ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Antibody Drug

scholarly journals Therapeutic Monoclonal Antibodies and Antibody Products: Current Practices and Development in Multiple Myeloma

Cancers ◽  
2019 ◽  
Vol 12 (1) ◽  
pp. 15 ◽  
Author(s):  
Francesca Bonello ◽  
Roberto Mina ◽  
Mario Boccadoro ◽  
Francesca Gay
Keyword(s):  
Multiple Myeloma ◽  
Clinical Trials ◽  
Monoclonal Antibodies ◽  
T Cell ◽  
Plasma Cells ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Promising Target ◽  
Therapeutic Monoclonal Antibodies ◽  
Antibody Drug

Immunotherapy is the latest innovation for the treatment of multiple myeloma (MM). Monoclonal antibodies (mAbs) entered the clinical practice and are under evaluation in clinical trials. MAbs can target highly selective and specific antigens on the cell surface of MM cells causing cell death (CD38 and CS1), convey specific cytotoxic drugs (antibody-drug conjugates), remove the breaks of the immune system (programmed death 1 (PD-1) and PD-ligand 1/2 (L1/L2) axis), or boost it against myeloma cells (bi-specific mAbs and T cell engagers). Two mAbs have been approved for the treatment of MM: the anti-CD38 daratumumab for newly-diagnosed and relapsed/refractory patients and the anti-CS1 elotuzumab in the relapse setting. These compounds are under investigation in clinical trials to explore their synergy with other anti-MM regimens, both in the front-line and relapse settings. Other antibodies targeting various antigens are under evaluation. B cell maturation antigens (BCMAs), selectively expressed on plasma cells, emerged as a promising target and several compounds targeting it have been developed. Encouraging results have been reported with antibody drug conjugates (e.g., GSK2857916) and bispecific T cell engagers (BiTEs®), including AMG420, which re-directs T cell-mediated cytotoxicity against MM cells. Here, we present an overview on mAbs currently approved for the treatment of MM and promising compounds under investigation.

scholarly journals An enzymatic deconjugation method for the analysis of small molecule active drugs on antibody-drug conjugates

mAbs ◽  
2016 ◽  
Vol 8 (4) ◽  
pp. 698-705 ◽  
Author(s):  
Yi Li ◽  
Christine Gu ◽  
Jason Gruenhagen ◽  
Peter Yehl ◽  
Nik P. Chetwyn ◽  
...  
Keyword(s):  
Small Molecule ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Antibody Drug

What Can We Learn about Antibody-Drug Conjugates from the T-DM1 Experience?

2015 ◽  
pp. e117-e125 ◽  
Author(s):  
Francisco J. Esteva ◽  
Kathy D. Miller ◽  
Beverly A. Teicher
Keyword(s):  
Small Molecule ◽  
Antibody Fragment ◽  
Cytotoxic Agents ◽  
Specific Cell ◽  
Malignant Cells ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Protein Toxin ◽  
Antibody Conjugates ◽  
Antibody Drug

Antibody conjugates are a diverse class of therapeutics that consist of a cytotoxic agent linked covalently to an antibody or antibody fragment directed toward a specific cell surface target expressed by tumor cells. The notion that antibodies directed toward targets on the surface of malignant cells could be used for drug delivery is not new. The history of antibody conjugates has been marked by hurdles identified and overcome. Early conjugates used mouse antibodies, drugs that either were not sufficiently potent, were immunogenic (proteins), or were too toxic, and linkers that were not sufficiently stable in circulation. Four main avenues have been explored using antibodies to target cytotoxic agents to malignant cells: antibody-protein toxin (or antibody fragment–protein toxin fusion) conjugates, antibody-chelated radionuclide conjugates, antibody-small molecule conjugates, and antibody-enzyme conjugates administered along with small molecule prodrugs that require metabolism by the conjugated enzyme to release the activated species. Technology is continuing to evolve regarding the protein and small molecule components, and it is likely that single chemical entities soon will be the norm for antibody-drug conjugates. Only antibody-radionuclide conjugates and antibody-drug conjugates have reached the regulatory approval stage, and there are more than 40 antibody conjugates in clinical trials. The time may have come for this technology to become a major contributor to improving treatment for patients with cancer.

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