Next-Generation Antibody-Drug Conjugates (ADCs)

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 20 December 2024 | Viewed by 5187

Special Issue Editor


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Guest Editor
Texas Therapeutics Institute, The Brown Foundation Institute of Molecular Medicine, The University of Texas Health Science Center at Houston, TMC3 Collaborative Building, 7255 Helix Park Avenue, Houston, TX 77030, USA
Interests: medicinal chemistry; targeted therapy; drug delivery; antibody-drug conjugate; structural molecular biology; nuclear receptor superfamily; cancer; immune disease

Special Issue Information

Dear Colleagues,

I am pleased to invite you to contribute to the Special Issue entitled “Next-Generation Antibody–Drug Conjugates”.

ADCs are an emerging drug class for cancer treatment, with 11 successful FDA-approved ADCs for many indications, including both hematological malignancies and solid tumors. Recent advances, including antibody formats (such as a bispecific antibody), conjugation chemistry, linker technology and novel payloads beyond cytotoxic molecules (such as an immunomodulator), can move ADCs to the next generation.

This Special Issue aims to provide cutting-edge knowledge in the field of ADCs. Original research articles and reviews are welcome. Research topics may include the following (but are not limited to): novel antigens, antibodies including fragments and other formats (e.g., bispecific), conjugation methods, linkers and payloads for ADCs. Papers reporting on basic to translational/(pre)clinical research are welcome. Other submissions that facilitate the development of ADCs are also welcome.

I look forward to receiving your contributions.

Dr. Yasuaki Anami
Guest Editor

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Keywords

  • antibody–drug conjugate
  • bioconjugation
  • vancer therapy
  • targeted therapy
  • bystander effect

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Published Papers (2 papers)

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Research

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13 pages, 2032 KiB  
Communication
Antitumor Activity of a Pyrrolobenzodiazepine Antibody–Drug Conjugate Targeting LGR5 in Preclinical Models of Neuroblastoma
by Jianghua Tu, Yukimatsu Toh, Adela M. Aldana, Jake J. Wen, Ling Wu, Joan Jacob, Li Li, Sheng Pan, Kendra S. Carmon and Qingyun J. Liu
Pharmaceutics 2024, 16(7), 943; https://doi.org/10.3390/pharmaceutics16070943 - 15 Jul 2024
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Abstract
Neuroblastoma (NB) is a cancer of the peripheral nervous system found in children under 15 years of age. It is the most frequently diagnosed cancer during infancy, accounting for ~12% of all cancer-related deaths in children. Leucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5) is [...] Read more.
Neuroblastoma (NB) is a cancer of the peripheral nervous system found in children under 15 years of age. It is the most frequently diagnosed cancer during infancy, accounting for ~12% of all cancer-related deaths in children. Leucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5) is a membrane receptor that is associated with the primary tumor formation and metastasis of cancers in the gastrointestinal system. Remarkably, high levels of LGR5 are found in NB tumor cells, and high LGR5 expression is strongly correlated with poor survival. Antibody–drug conjugates (ADCs) are monoclonal antibodies that are covalently linked to cell-killing cytotoxins to deliver the payloads into cancer cells. We generated an ADC with an anti-LGR5 antibody and pyrrolobenzodiazepine (PBD) dimer-based payload SG3199 using a chemoenzymatic conjugation method. The resulting anti-LGR5 ADC was able to inhibit the growth of NB cells expressing LGR5 with high potency and specificity. Importantly, the ADC was able to completely inhibit the growth of NB xenograft tumors in vivo at a clinically relevant dose for the PBD class of ADCs. The findings support the potential of targeting LGR5 using the PBD class of payload for the treatment of high-risk NBs. Full article
(This article belongs to the Special Issue Next-Generation Antibody-Drug Conjugates (ADCs))
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Review

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33 pages, 2541 KiB  
Review
The Evolving Paradigm of Antibody–Drug Conjugates Targeting the ErbB/HER Family of Receptor Tyrosine Kinases
by Peyton High, Cara Guernsey, Shraddha Subramanian, Joan Jacob and Kendra S. Carmon
Pharmaceutics 2024, 16(7), 890; https://doi.org/10.3390/pharmaceutics16070890 - 2 Jul 2024
Cited by 1 | Viewed by 3321
Abstract
Current therapies targeting the human epidermal growth factor receptor (HER) family, including monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs), are limited by drug resistance and systemic toxicities. Antibody–drug conjugates (ADCs) are one of the most rapidly expanding classes of anti-cancer therapeutics with [...] Read more.
Current therapies targeting the human epidermal growth factor receptor (HER) family, including monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs), are limited by drug resistance and systemic toxicities. Antibody–drug conjugates (ADCs) are one of the most rapidly expanding classes of anti-cancer therapeutics with 13 presently approved by the FDA. Importantly, ADCs represent a promising therapeutic option with the potential to overcome traditional HER-targeted therapy resistance by delivering highly potent cytotoxins specifically to HER-overexpressing cancer cells and exerting both mAb- and payload-mediated antitumor efficacy. The clinical utility of HER-targeted ADCs is exemplified by the immense success of HER2-targeted ADCs including trastuzumab emtansine and trastuzumab deruxtecan. Still, strategies to improve upon existing HER2-targeted ADCs as well as the development of ADCs against other HER family members, particularly EGFR and HER3, are of great interest. To date, no HER4-targeting ADCs have been reported. In this review, we extensively detail clinical-stage EGFR-, HER2-, and HER3-targeting monospecific ADCs as well as novel clinical and pre-clinical bispecific ADCs (bsADCs) directed against this receptor family. We close by discussing nascent trends in the development of HER-targeting ADCs, including novel ADC payloads and HER ligand-targeted ADCs. Full article
(This article belongs to the Special Issue Next-Generation Antibody-Drug Conjugates (ADCs))
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