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Pharmaceutics
Special Issues
Antibody–Drug Conjugates (ADC)
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Antibody–Drug Conjugates (ADC)

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Gene and Cell Therapy".

Deadline for manuscript submissions: closed (28 February 2021) | Viewed by 7758

Special Issue Editors

Prof. Stefano Iacobelli

E-Mail Website
Guest Editor
1. Department of Gynecology and Obstetrics, Catholic University, 00168 Rome, Italy
2. MediaPharma Srl, Via Colonnetta, 50/A, 66100 Chieti, Italy
Interests: cancer; antibody; antibody–drug conjugate; targeted therapy; precision oncology; breast cancer; melanoma; translational research
Prof. Dr. Rodolfo Ippoliti

E-Mail Website1 Website2
Guest Editor
Department of Life, Health and Environmental Sciences, University of L’Aquila, 67100 L’Aquila, Italy
Interests: drug delivery; toxins; immune conjugates; cancer therapy; protein structure
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibody Drug Conjugates (ADC)s made of antibodies chemically linked to toxic payloads represent one of the emerging frontiers of cancer therapy, and their usefulness in clinics has continuously increased over the last 10 years. At the moment there are seven different formulations on the market: they, differ for the target, the type of antibody, the linker structure and finally the nature of the payload. Notwithstanding the improvement of these bio-based drugs, there are still several critical issues to be solved, including stability, decreasing of the off-target toxicity, site-selective conjugation and engineering of the antibody molecule. This volume will approach innovation in this field, including the discovery of new targets for the development of more specific, highly penetrating and efficient ADC(s). We encourage your contribution with the aim of involving top scientist in describing more recent achievements, and with the hope that Paul Ehrlich’s vision will soon become reality.

Prof. Stefano Iacobelli
Prof. Rodolfo Ippoliti
Guest Editors

Manuscript Submission Information

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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. Pharmaceutics is an international peer-reviewed open access monthly 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 2900 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)
  • Target therapy
  • Chemistry of conjugation
  • Cytotoxic agents
  • Linkers
  • Cancer

Published Papers (2 papers)

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Research

16 pages, 2117 KiB  
Article
EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors
by Emily Capone, Rossano Lattanzio, Fabio Gasparri, Paolo Orsini, Cosmo Rossi, Valentina Iacobelli, Vincenzo De Laurenzi, Pier Giorgio Natali, Barbara Valsasina, Stefano Iacobelli and Gianluca Sala
Pharmaceutics 2021, 13(4), 483; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13040483 - 02 Apr 2021
Cited by 8 | Viewed by 3100
Abstract
HER-3 is becoming an attractive target for antibody–drug conjugate (ADC)-based therapy. Indeed, this receptor and its ligands are found to be overexpressed in several malignancies, and re-activation of its downstream signaling axis is known to play a critical role in modulating the sensitivity [...] Read more.
HER-3 is becoming an attractive target for antibody–drug conjugate (ADC)-based therapy. Indeed, this receptor and its ligands are found to be overexpressed in several malignancies, and re-activation of its downstream signaling axis is known to play a critical role in modulating the sensitivity of targeted therapeutics in different tumors. In this study, we generated a novel ADC named EV20/NMS-P945 by coupling the anti-HER-3 antibody EV20 with a duocarmycin-like derivative, the thienoindole (TEI) NMS-P528, a DNA minor groove alkylating agent through a peptidic cleavable linker. This ADC showed target-dependent cytotoxic activity in vitro on several tumor cell lines and therapeutic activity in mouse xenograft tumor models, including those originating from pancreatic, prostatic, head and neck, gastric and ovarian cancer cells and melanoma. Pharmacokinetics and toxicological studies in monkeys demonstrated that this ADC possesses a favorable terminal half-life and stability and it is well tolerated. These data support further EV20/NMS-P945 clinical development as a therapeutic agent against HER-3-expressing malignancies. Full article
(This article belongs to the Special Issue Antibody–Drug Conjugates (ADC))
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14 pages, 2169 KiB  
Article
Assessments of the In Vitro and In Vivo Linker Stability and Catabolic Fate for the Ortho Hydroxy-Protected Aryl Sulfate Linker by Immuno-Affinity Capture Liquid Chromatography Quadrupole Time-of-Flight Mass Spectrometric Assay
by Byeong ill Lee, Seo-jin Park, Yuri Park, Seok-Ho Shin, Jang-mi Choi, Min-jae Park, Jeong-hyeon Lim, Sun Young Kim, Hyangsook Lee and Young G. Shin
Pharmaceutics 2021, 13(1), 125; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13010125 - 19 Jan 2021
Cited by 4 | Viewed by 3789
Abstract
Antibody–drug conjugate (ADC) linkers play an important role in determining the safety and efficacy of ADC. The Ortho Hydroxy-Protected Aryl Sulfate (OHPAS) linker is a newly developed linker in the form of a di-aryl sulfate structure consisting of phenolic payload and self-immolative group [...] Read more.
Antibody–drug conjugate (ADC) linkers play an important role in determining the safety and efficacy of ADC. The Ortho Hydroxy-Protected Aryl Sulfate (OHPAS) linker is a newly developed linker in the form of a di-aryl sulfate structure consisting of phenolic payload and self-immolative group (SIG). In this study, using two bioanalytical approaches (namely “bottom-up” and “middle-up” approaches) via the liquid chromatography-quadrupole time-of-flight mass spectrometric (LC-qTOF-MS) method, in vitro and in vivo linker stability experiments were conducted for the OHPAS linker. For comparison, the valine-citrulline-p-aminobenzyloxycarbonyl (VC-PABC) linker was also evaluated under the same experimental conditions. In addition, the catabolite identification experiments at the subunit intact protein level were simultaneously performed to evaluate the catabolic fate of ADCs. As a result, the OHPAS linker was stable in the in vitro mouse/human plasma as well as in vivo pharmacokinetic studies in mice, whereas the VC-PABC linker was relatively unstable in mice in vitro and in vivo. This is because the VC-PABC linker was sensitive to a hydrolytic enzyme called carboxylesterase 1c (Ces1c) in mouse plasma. In conclusion, the OHPAS linker appears to be a good linker for ADC, and further experiments would be warranted to demonstrate the efficacy and toxicity related to the OHPAS linker. Full article
(This article belongs to the Special Issue Antibody–Drug Conjugates (ADC))
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