ArticleAntibodies (Basel, Switzerland)2018
Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility.
Article in Antibodies (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Structure-Activity Relationships of Antibody-Drug Conjugates: A Systematic Review of Chemistry on the Trastuzumab Scaffold.Bioconjugate chemistry · 2022Pooled it
- Exatecan Payload-Based Antibody-Drug Conjugates with a Short Hydrophilic Cleavable Linker.ACS medicinal chemistry letters · 2026Article
- Formulation Matters: The Overlooked Engine of Stability and Success in Antibody-Drug Conjugates.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Antibody-Drug Conjugates in Hematological Malignancies: Current Landscape and Future Perspectives.International journal of molecular sciences · 2026Review
- Legumain-Cleavable Top1i Antibody-Drug Conjugates without Self-Immolative Spacers Demonstrate Potent Antitumor Activity.Journal of medicinal chemistry · 2025Article
- Article
- Exo-Cleavable Linkers: Enhanced Stability and Therapeutic Efficacy in Antibody-Drug Conjugates.Journal of medicinal chemistry · 2024Article
- Antibody-drug conjugates in solid tumors; new strategy for cancer therapy.Japanese journal of clinical oncology · 2024Review
- Antibody-Drug Conjugate Overview: a State-of-the-art Manufacturing Process and Control Strategy.Pharmaceutical research · 2024Review
- Drug conjugates for the treatment of lung cancer: from drug discovery to clinical practice.Experimental hematology & oncology · 2024Review
- Impact of dipeptide on ADC physicochemical properties and efficacy identifies Ala-Ala as the optimal dipeptide.RSC medicinal chemistry · 2024Article
- Engineering CD276/B7-H3-targeted antibody-drug conjugates with enhanced cancer-eradicating capability.Cell reports · 2023Article
- Antibody-Drug Conjugates in Solid Tumor Oncology: An Effectiveness Payday with a Targeted Payload.Pharmaceutics · 2023Review
- AJICAP Second Generation: Improved Chemical Site-Specific Conjugation Technology for Antibody-Drug Conjugate Production.Bioconjugate chemistry · 2023Article
- Advances and Limitations of Antibody Drug Conjugates for Cancer.Biomedicines · 2021Review
- The clinical development of antibody-drug conjugates - lessons from leukaemia.Nature reviews. Clinical oncology · 2021Review
- Site-Specific, Stoichiometric-Controlled, PEGylated Conjugates of Fibroblast Growth Factor 2 (FGF2) with Hydrophilic Auristatin Y for Highly Selective Killing of Cancer Cells Overproducing Fibroblast Growth Factor Receptor 1 (FGFR1).Molecular pharmaceutics · 2020Article
- A Purification Strategy Utilizing Hydrophobic Interaction Chromatography to Obtain Homogeneous Species from a Site-Specific Antibody Drug Conjugate Produced by AJICAP™ First Generation.Antibodies (Basel, Switzerland) · 2020Article
- Site-Specific Bioconjugation and Multi-Bioorthogonal Labeling via Rapid Formation of a Boron-Nitrogen Heterocycle.Bioconjugate chemistry · 2019Article
- Assessing the Interactions of Auristatin Derivatives with Mixed Phospholipid-Sodium Dodecyl Sulfate Aggregate Dispersions.Langmuir : the ACS journal of surfaces and colloids · 2019Article
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Antibody-drug conjugates (ADCs) offer a combination of antibody therapy and specific delivery of potent small-molecule payloads to target cells. The properties of the ADC molecule are determined by the balance of its components. The efficacy of the payload component increases with higher drug-to-antibody ratio (DAR), while homogeneous DAR = 8 ADCs are easily prepared by conjugation to the four accessible antibody hinge cystines. However, use of hydrophobic payloads has permitted only DAR = 2-4, due to poor pharmacokinetics and aggregation problems. Here, we describe generation and characterization of homogeneous DAR = 8 ADCs carrying a novel auristatin β-D-glucuronide, MMAU. The glycoside payload contributed to overall hydrophilicity of the ADC reducing aggregation. Compared to standard DAR = 2-4 ADCs, cytotoxicity of the homogeneous DAR = 8 ADCs was improved to low-picomolar IC
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