Pathophysiologic and Pharmacologic Considerations to Improve the Design and Application of Antibody–Drug Conjugates

Boghaert, Erwin R.; Cox, Megan C.; Vaidya, Kedar S.

doi:10.1158/0008-5472.can-21-3236

Cited by 17Monoclonal and Polyclonal Antibodies ResearchNanoparticle-Based Drug DeliveryToxin Mechanisms and Immunotoxins

Pathophysiologic and Pharmacologic Considerations to Improve the Design and Application of Antibody–Drug Conjugates

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Boghaert, Erwin R., Cox, Megan C., Vaidya, Kedar S.·2022·Cancer Research

DOI 10.1158/0008-5472.can-21-3236

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Abstract

Antibody–drug conjugates (ADC) have emerged as one of the pillars of clinical disease management in oncology. The biggest hurdle to widespread development and application of ADCs has been a narrow therapeutic index. Advances in antibody technologies and formats as well as novel linker and payload chemistries have begun to facilitate structural improvements to ADCs. However, the interplay of structural characteristics with physiologic and pharmacologic factors determining therapeutic success has garnered less attention. This review elaborates on the pharmacology of ADCs, the pathophysiology of cancerous tissues, and the reciprocal consequences on ADC properties and functions. While most currently approved ADCs utilize either microtubule inhibition or DNA damage as primary mechanisms of action, we present arguments to expand this repertoire and highlight the need for payload mechanisms that exploit disease-specific vulnerabilities. We promote the idea that the choice of antibody format, targeting antigen, linker properties, and payload of an ADC should be deliberately fit for purpose by taking the pathophysiology of disease and the specific pharmacology of the drug entity into account, thus allowing a higher probability of clinical success.

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The histological architecture of mCRPC-characterized by dense stroma, low vascularity, and high between-tumor heterogeneity-has limited ADC penetration and distribution within tumor tissue.
“In particular, the histological architecture of mCRPC—characterized by dense stroma, low vascularity, and high between-tumor heterogeneity—has limited ADC penetration and distribution within tumor tissue219–222.”
From The evolving landscape of antibody-drug conjugates (ADCs) for treatment of prostate cancer (2025) · cites this paper as [219]
The ‘Active and passive targeting’ section says that solid-tumor histopathology can hinder ADC access to cancer cells, and ‘The use of advanced preclinical cancer models’ discusses stromal barriers to penetration and distribution. The paper does not establish that mCRPC specifically has dense stroma, low vascularity, or high between-tumor heterogeneity, or that those features have limited ADC distribution in mCRPC. Page numbers are unavailable in our copy. (LLM, conf=0.86)
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Establishment of a human hemangiosarcoma cell line (ISO-HAS)
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Maytansine-bearing antibody-drug conjugates induce in vitro hallmarks of immunogenic cell death selectively in antigen-positive target cells
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Structural insights into the mechanism of action of a biparatopic anti-HER2 antibody
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Natural Product Splicing Inhibitors: A New Class of Antibody–Drug Conjugate (ADC) Payloads
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Evaluation of Quantitative Relationship Between Target Expression and Antibody-Drug Conjugate Exposure Inside Cancer Cells
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A Biparatopic Antibody–Drug Conjugate to Treat MET-Expressing Cancers, Including Those that Are Unresponsive to MET Pathway Blockade
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The Next Generation of Antibody Drug Conjugates
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A Brief Introduction to Antibody–Drug Conjugates for Toxicologic Pathologists
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Antigen Shedding May Improve Efficiencies for Delivery of Antibody-Based Anticancer Agents in Solid Tumors
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Targeting Multiple EGFR-expressing Tumors with a Highly Potent Tumor-selective Antibody–Drug Conjugate
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A clinical and scientific overview of tositumomab and iodine I 131 tositumomab
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Clinical pharmacology strategies in supporting drug development and approval of antibody–drug conjugates in oncology
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Does sacituzumab-govitecan act as a conventional antibody drug conjugate (ADC), a prodrug of SN-38 or both?
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The Volume of Three-Dimensional Cultures of Cancer Cells In Vitro Influences Transcriptional Profile Differences and Similarities with Monolayer Cultures and Xenografted Tumors
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Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues
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HER2 monoclonal antibodies that do not interfere with receptor heterodimerization-mediated signaling induce effective internalization and represent valuable components for rational antibody-drug conjugate design
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The spliceosome-associated protein Nrl1 suppresses homologous recombination-dependent R-loop formation in fission yeast
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APOMAB Antibody–Drug Conjugates Targeting Dead Tumor Cells are Effective In Vivo
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Design, Synthesis, and Biological Investigation of Thailanstatin A and Spliceostatin D Analogues Containing Tetrahydropyran, Tetrahydrooxazine, and Fluorinated Structural Motifs
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Combination Treatment with an Antibody–Drug Conjugate (A1mcMMAF) Targeting the Oncofetal Glycoprotein 5T4 and Carboplatin Improves Survival in a Xenograft Model of Ovarian Cancer
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Sorted by citations

The Journey of Antibody–Drug Conjugates: Lessons Learned from 40 Years of Development
Colombo, R., Tarantino, P., Rich, J. R., LoRusso, P. M., & de Vries, E. G. E. (2024) · Cancer Discovery · doi:10.1158/2159-8290.cd-24-0708 · Cited by 254 · see citing works
The evolving landscape of antibody-drug conjugates (ADCs) for treatment of prostate cancer
Lin, C., Hadfield, M. J., Santopietro, A., Lagos, G., Cheng, L., El-Deiry, W. S., Aggarwal, R., Mega, A., Hyams, E., & Carneiro, B. A. (2025) · npj Precision Oncology · doi:10.1038/s41698-025-01131-0 · Cited by 20 · see citing works

Authors: Boghaert, E. R., Cox, M. C., & Vaidya, K. S.
Affiliations: AbbVie (United States) (US)
Jazz Pharmaceuticals (United States) (US)
Corresponding author: Boghaert, Erwin R.
ORCID: Boghaert, Erwin R.
Cox, Megan C.
Vaidya, Kedar S.
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2022-03-17
Volume: 82
Issue: 10
Pages: 1858-1869
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-21-3236
OpenAlex: W4220764795
Cited by: 17
References: 136
Citations by year: 2026: 3 · 2025: 8 · 2024: 3 · 2023: 2 · 2022: 1
FWCI: 0.59
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Monoclonal and Polyclonal Antibodies Research
Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Life Sciences › Immunology and Microbiology › Immunology › Toxin Mechanisms and Immunotoxins
Keywords: antibody-drug conjugates, tumor pathophysiology, linker chemistry, antibody formats, microtubule inhibitors, DNA damage, narrow therapeutic index, targeted cancer therapy
MeSH terms: Antibodies, Antineoplastic Agents, Humans, Neoplasms, Immunoconjugates

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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

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Pathophysiologic and Pharmacologic Considerations to Improve the Design and Application of Antibody–Drug Conjugates

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