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Molecules
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Current Developments in Antibody Drug Conjugates as Cancer Therapeutics
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Current Developments in Antibody Drug Conjugates as Cancer Therapeutics

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 28663

Special Issue Editor

Prof. Dr. Khondaker Miraz Rahman

E-Mail Website
Guest Editor
School of Cancer and Pharmaceutical Science, King's College London, London, UK
Interests: antimicrobial resistance research; development of new chemical tools; antibacterial drug discovery; antifungal drug discovery; efflux pumps
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear colleagues,

Antibody–drug conjugates (ADCs) are a family of targeted therapeutic agents for the treatment of cancer. ADC development is a rapidly expanding field of research, with over 80 ADCs currently in clinical development and eleven ADCs (nine containing small-molecule payloads and two with biological toxins) approved for use by the FDA. This Special Issue aims to give readers a comprehensive understanding of current research in ADC-based cancer therapeutics. The issue aims to publish research work and review articles that detail current advances in each of the ADC components (i.e., monoclonal antibodies, linker moieties and cytotoxic payloads), as well as the ADCs that are at different stages of pre-clinical and clinical evaluation against both solid and liquid tumors. We believe this Special Issue will be of interest to the ADC community, both in industry and academia, and to the early career researchers who are working in the anticancer drug discovery space.

Submissions are welcomed on the following areas:

  • Advances in chemistry of cytotoxic payloads;
  • Advances in linker development for antibody–drug conjugates;
  • Conjugation of payloads with monoclonal antibodies;
  • Characterization of antibody–drug conjugates;
  • In vitro and in vivo evaluation of antibody–drug conjugates;
  • Pre-clinical development of antibody–drug conjugates;
  • Clinical evaluation of antibody–drug conjugates;
  • Identification of new payloads for antibody–drug conjugates;
  • Chemical modification of existing payload classes;
  • Identification of new linker types for antibody–drug conjugates, etc.;
  • Studies involving new monoclonal antibodies.

Dr. K Miraz Rahman
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • antibody–drug conjugate
  • ADC
  • monoclonal antibody
  • linker
  • cytotoxic payload
  • liquid and solid tumor
  • targeted chemotherapy
  • drug antibody ratio (DAR)
  • conjugation
  • pre-clinical development of ADCs
  • clinical development of ADCs

Published Papers (3 papers)

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Review

21 pages, 913 KiB  
Review
Site-Specific Antibody Conjugation with Payloads beyond Cytotoxins
by Qun Zhou
Molecules 2023, 28(3), 917; https://doi.org/10.3390/molecules28030917 - 17 Jan 2023
Cited by 12 | Viewed by 6631
Abstract
As antibody–drug conjugates have become a very important modality for cancer therapy, many site-specific conjugation approaches have been developed for generating homogenous molecules. The selective antibody coupling is achieved through antibody engineering by introducing specific amino acid or unnatural amino acid residues, peptides, [...] Read more.
As antibody–drug conjugates have become a very important modality for cancer therapy, many site-specific conjugation approaches have been developed for generating homogenous molecules. The selective antibody coupling is achieved through antibody engineering by introducing specific amino acid or unnatural amino acid residues, peptides, and glycans. In addition to the use of synthetic cytotoxins, these novel methods have been applied for the conjugation of other payloads, including non-cytotoxic compounds, proteins/peptides, glycans, lipids, and nucleic acids. The non-cytotoxic compounds include polyethylene glycol, antibiotics, protein degraders (PROTAC and LYTAC), immunomodulating agents, enzyme inhibitors and protein ligands. Different small proteins or peptides have been selectively conjugated through unnatural amino acid using click chemistry, engineered C-terminal formylglycine for oxime or click chemistry, or specific ligation or transpeptidation with or without enzymes. Although the antibody protamine peptide fusions have been extensively used for siRNA coupling during early studies, direct conjugations through engineered cysteine or lysine residues have been demonstrated later. These site-specific antibody conjugates containing these payloads other than cytotoxic compounds can be used in proof-of-concept studies and in developing new therapeutics for unmet medical needs. Full article
(This article belongs to the Special Issue Current Developments in Antibody Drug Conjugates as Cancer Therapeutics)
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11 pages, 937 KiB  
Review
A New Kid on the Block: Sacituzumab Govitecan for the Treatment of Breast Cancer and Other Solid Tumors
by Giuliana Pavone, Lucia Motta, Federica Martorana, Gianmarco Motta and Paolo Vigneri
Molecules 2021, 26(23), 7294; https://doi.org/10.3390/molecules26237294 - 01 Dec 2021
Cited by 12 | Viewed by 6531
Abstract
Human trophoblast cell-surface antigen-2 (Trop-2) is a membrane glycoprotein involved in cell proliferation and motility, frequently overexpressed in epithelial tumors. Thus, it represents an attractive target for anticancer therapies. Sacituzumab govitecan (SG) is a third-generation antibody-drug conjugate, consisting of an anti-Trop-2 monoclonal antibody [...] Read more.
Human trophoblast cell-surface antigen-2 (Trop-2) is a membrane glycoprotein involved in cell proliferation and motility, frequently overexpressed in epithelial tumors. Thus, it represents an attractive target for anticancer therapies. Sacituzumab govitecan (SG) is a third-generation antibody-drug conjugate, consisting of an anti-Trop-2 monoclonal antibody (hRS7), a hydrolyzable linker, and a cytotoxin (SN38), which inhibits topoisomerase 1. Specific pharmacological features, such as the high antibody to payload ratio, the ultra-toxic nature of SN38, and the capacity to kill surrounding tumor cells (the bystander effect), make SG a very promising drug for cancer treatment. Indeed, unprecedented results have been observed with SG in patients with heavily pretreated advanced triple-negative breast cancer and urothelial carcinomas, and the drug has already received approval for these indications. These results are coupled with a manageable toxicity profile, with neutropenia and diarrhea as the most frequent adverse events, mainly of grades 1–2. While several trials are exploring SG activity in different tumor types and settings, potential biomarkers of response are under investigation. Among these, Trop-2 overexpression and the presence of BRCA1/2 mutations seem to be the most promising. We review the available literature concerning SG, with a focus on its toxicity spectrum and possible biomarkers of its response. Full article
(This article belongs to the Special Issue Current Developments in Antibody Drug Conjugates as Cancer Therapeutics)
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Figure 1

19 pages, 2590 KiB  
Review
Antibody–Drug Conjugates—A Tutorial Review
by Stephanie Baah, Mark Laws and Khondaker Miraz Rahman
Molecules 2021, 26(10), 2943; https://doi.org/10.3390/molecules26102943 - 15 May 2021
Cited by 84 | Viewed by 14705
Abstract
Antibody–drug conjugates (ADCs) are a family of targeted therapeutic agents for the treatment of cancer. ADC development is a rapidly expanding field of research, with over 80 ADCs currently in clinical development and eleven ADCs (nine containing small-molecule payloads and two with biological [...] Read more.
Antibody–drug conjugates (ADCs) are a family of targeted therapeutic agents for the treatment of cancer. ADC development is a rapidly expanding field of research, with over 80 ADCs currently in clinical development and eleven ADCs (nine containing small-molecule payloads and two with biological toxins) approved for use by the FDA. Compared to traditional small-molecule approaches, ADCs offer enhanced targeting of cancer cells along with reduced toxic side effects, making them an attractive prospect in the field of oncology. To this end, this tutorial review aims to serve as a reference material for ADCs and give readers a comprehensive understanding of ADCs; it explores and explains each ADC component (monoclonal antibody, linker moiety and cytotoxic payload) individually, highlights several EMA- and FDA-approved ADCs by way of case studies and offers a brief future perspective on the field of ADC research. Full article
(This article belongs to the Special Issue Current Developments in Antibody Drug Conjugates as Cancer Therapeutics)
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