ArticleDrug metabolism and disposition: the biological fate of chemicals2020
Evaluation of Quantitative Relationship Between Target Expression and Antibody-Drug Conjugate Exposure Inside Cancer Cells.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 46 citations in OpenAlex.
- Genotoxic antibody-drug conjugates combined with BCL-XL inhibitors enhance therapeutic efficacy in metastatic castration-resistant prostate cancer.The Journal of clinical investigation · 2026Article
- Tyrosine Kinase Inhibitors, Antibody-Drug Conjugates, and Bispecific Antibodies in Oncogene-Driven Non-Small-Cell Lung Cancer: Evolving Roles in Treatment Sequencing and Resistance Management.International journal of molecular sciences · 2026Review
- Multi-institutional assessment of HER2 immunohistochemistry in gastric and esophagogastric junction cancer.iScience · 2026Article
- Immuno-cytotoxic convergence: integrating antibody‒drug conjugates and immunofusion proteins to overcome resistance in gastrointestinal cancers.Journal of hematology & oncology · 2026Review
- Receptor-Mediated Drug Delivery: Redefining Targeted Drug Conjugates in Oncology.Pharmaceutics · 2026Review
- Targeting Biliary Tract Cancers with Antibody-Drug Conjugates: Advances in Molecular Targets and Rational Combinations.Cancers · 2026Review
- Expression of antibody-drug conjugate targets in post-mortem samples of breast cancer metastases and normal tissue.Nature communications · 2025Article
- Review
- SC134-deruxtecan, a fucosyl-GM1 targeting ADC for small cell lung cancer therapy.Journal of translational medicine · 2025Article
- Exploring Experimental and In Silico Approaches for Antibody-Drug Conjugates in Oncology Therapies.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Overview of antibody-drug conjugates nonclinical and clinical toxicities and related contributing factors.Antibody therapeutics · 2025Review
- Targeting uPAR with an antibody-drug conjugate suppresses tumor growth and reshapes the immune landscape in pancreatic cancer models.Science advances · 2025Article
- Review
- Assessment of targets of antibody drug conjugates in SCLC.NPJ precision oncology · 2025Article
- Tissue factor expression in salivary gland carcinoma: a potential novel therapeutic target for advanced disease.Therapeutic advances in medical oncology · 2025Article
- Affimer reagents enable targeted delivery of therapeutic agents and RNA via virus-like particles.iScience · 2024Article
- Epidermal Growth Factor Receptor Targeting in Colorectal Carcinoma: Antibodies and Patient-Derived Organoids as a Smart Model to Study Therapy Resistance.International journal of molecular sciences · 2024Review
- Surface-Available HER2 Levels Alone Are Not Indicative of Cell Response to HER2-Targeted Antibody-Drug Conjugate Therapies.Pharmaceutics · 2024Article
- Applications of Flow Cytometry in Drug Discovery and Translational Research.International journal of molecular sciences · 2024Review
- Antibody-Drug Conjugates: The Dynamic Evolution from Conventional to Next-Generation Constructs.Cancers · 2024Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Antibody-drug conjugates (ADCs) employ overexpressed cell surface antigens to deliver cytotoxic payloads inside cancer cells. However, the relationship between target expression and ADC efficacy remains ambiguous. In this manuscript, we have addressed a part of this ambiguity by quantitatively investigating the effect of antigen expression levels on ADC exposure within cancer cells. Trastuzumab-valine-citrulline-monomethyl auristatin E was used as a model ADC, and four different cell lines with diverse levels of human epidermal growth factor receptor 2 (HER2) expression were used as model cells. The pharmacokinetics (PK) of total trastuzumab, released monomethyl auristatin E (MMAE), and total MMAE were measured inside the cells and in the cell culture media following incubation with two different concentrations of ADC. In addition, target expression levels, target internalization rate, and cathepsin B and MDR1 protein concentrations were determined for each cell line. All the PK data were mathematically characterized using a cell-level systems PK model for ADC. It was found that SKBR-3, MDA-MB-453, MCF-7, and MDA-MB-468 cells had ∼800,000, ∼250,000, ∼50,000, and ∼10,000 HER2 receptors per cell, respectively. A strong linear relationship (
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.