Antibody-drug conjugates have attracted a great amount of attention as a therapeutic strategy for diseases where targeting specific tissues and cells are critical components, such as in cancer therapy. Although promising, the number of approved ADC drugs is relatively limited. This emanates from the challenges associated with generating the conjugates and the complexities associated with the stability requirements for these conjugates during circulation and after reaching the target. Here, we provide a comprehensive overview of the design challenges facing the ADC field. These challenges also provide several unique research and development opportunities, which are also highlighted throughout the review.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4933296 | PMC |
| http://dx.doi.org/10.1021/acs.bioconjchem.5b00399 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Analytical and Clinical Validation of the Plasma-Based Guardant360 CDx Test for Assessing HER2 (ERBB2) Mutation Status in Patients with Non-Small-Cell Lung Cancer for Treatment with Trastuzumab Deruxtecan in DESTINY-Lung01/02.
J Mol Diagn
February 2025
Daiichi Sankyo, Inc., Basking Ridge, New Jersey.
This study demonstrates the analytical and clinical validity of the approved (United States and Japan) plasma-based Guardant360 companion diagnostic (CDx) test for selecting patients with human epidermal growth factor receptor 2 (HER2 [ERBB2])-mutated (HER2m) non-small-cell lung cancer (NSCLC) for trastuzumab deruxtecan (T-DXd) treatment. Concordance between the Guardant360 CDx test and the plasma-based AVENIO ctDNA Expanded Kit Assay (AVENIO), as well as the tissue-based clinical trial assays (CTAs) was investigated. Clinical utility was assessed by comparing T-DXd clinical efficacy results of patients in DESTINY-Lung01/02 who tested positive for HER2 mutations using the Guardant360 CDx test to benchmark efficacy results from DESTINY-Lung01/02.
View Article and Find Full Text PDFWork loss in patients with rheumatoid arthritis treated with abatacept, rituximab, tocilizumab or TNF inhibitors: a nationwide direct drug-to-drug comparison.
RMD Open
January 2025
Clinical Epidemiology Division, Dept of Medicine, Karolinska Institutet, Stockholm, Sweden.
Objective: To compare work loss after starting tumour necrosis factor inhibitors (TNFi), rituximab, abatacept or tocilizumab in patients with rheumatoid arthritis (RA).
Methods: We used data from the Swedish Rheumatology Quality Register to identify patients aged 19-62 years who were treated with TNFi (n=15 093), rituximab (n=2123), abatacept (n=1877) or tocilizumab (n=1720) between 2007 and 2020. Data on work loss (0-365 days per year) from sick leave and disability pension were retrieved from linkage to the Social Insurance Agency.
Synthesis and evaluation of KX-01 analogs with an exploration of linker attachment points for antibody-drug conjugates.
Bioorg Med Chem Lett
January 2025
Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon 34114 Republic of Korea; Medicinal Chemistry & Pharmacology, University of Science & Technology, Daejeon 34113 Republic of Korea. Electronic address:
KX-01 (tirbanibulin, Klisyri®) is a recently FDA-approved drug for treating actinic keratosis, with a distinct dual mechanism of action combining microtubule disruption and non-ATP-competitive Src inhibition. This unique mechanism and novel chemotype highlight KX-01's potential as a payload for antibody-drug conjugates. In this study, we synthesized and evaluated KX-01 derivatives to enhance anticancer potency and explore functional groups suitable for antibody conjugation.
View Article and Find Full Text PDFCathepsin B dependent activatable trigger fluorophore (CAT-Fluor) for in situ functional imaging of antibody-drug conjugates.
Biosens Bioelectron
January 2025
Deparment of Pharmacy, the Second Affiliated Hospital, Zhejiang University School of Medicine and College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China. Electronic address:
Antibody-drug conjugates (ADC) have emerged as an important class of therapeutic agents that combine the target specificity of a monoclonal antibody with the potency of a cytotoxic payload. Despite clinical success, our understanding of receptor endocytosis and ADC toxicity remains limited. Less than 1% of ADCs reach tumors, raising concerns about off-target cytotoxicity.
View Article and Find Full Text PDFArtificial intelligence for diagnosis and predictive biomarkers in Non-Small cell lung cancer Patients: New promises but also new hurdles for the pathologist.
Lung Cancer
January 2025
Institute of Pathology Heidelberg, University Hospital Heidelberg, In Neuenheimer Feld 224 69120 Heidelberg, Germany.
The rapid development of artificial intelligence (AI) based tools in pathology laboratories has brought forward unlimited opportunities for pathologists. Promising AI applications used for accomplishing diagnostic, prognostic and predictive tasks are being developed at a high pace. This is notably true in thoracic oncology, given the significant and rapid therapeutic progress made recently for lung cancer patients.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!