The development of divinylpyrimidine (DVP) reagents for the synthesis of antibody-drug conjugates (ADCs) with efficacy and tolerability is reported. Detailed structural characterisation of the synthesised ADCs was first conducted followed by and evaluation of the ADCs' ability to safely and selectively eradicate target-positive tumours.
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http://dx.doi.org/10.1039/d1cc06766d | DOI Listing |
Vaccines (Basel)
January 2025
Laboratory of Immunology and General Pathology, Department of Biotechnology and Life Sciences, University of Insubria, 21100 Varese, Italy.
Effective cancer therapies must address the tumor microenvironment (TME), a complex network of tumor cells and stromal components, including endothelial, immune, and mesenchymal cells. Durable outcomes require targeting both tumor cells and the TME while minimizing systemic toxicity. Interleukin-2 (IL-2)-based therapies have shown efficacy in cancers such as metastatic melanoma and renal cell carcinoma but are limited by severe side effects.
View Article and Find Full Text PDFCurr Oncol
December 2024
Jewish General Hospital, Montreal, QC H3T 1E2, Canada.
Background: Trastuzumab deruxtecan (TDXd) is an antibody-drug conjugate that has demonstrated impressive activity in randomized controlled clinical trials in the context of patients with HER2-amplified and HER2-low metastatic breast cancer. We aimed to review the activity and adverse event profile of TDXd in heavily pretreated breast cancer patients in real practice.
Methods: We describe a single-center retrospective case series of metastatic breast cancer patients who were treated with TDXd.
Background: Antibody-drug conjugate (ADC) is an anticancer drug that links toxins to specifically targeted antibodies via linkers, offering the advantages of high target specificity and high cytotoxicity. However, complexity of its structural composition poses a greater difficulty for drug design studies.
Objectives: Pharmacokinetic/pharmacodynamic (PK/PD) based consideration of ADCs has increasingly become a hot research topic for optimal drug design in recent years, providing possible ideas for obtaining ADCs with desirable properties.
Cancer Treat Rev
January 2025
Gastrointestinal Unit, Department of Medicine, Royal Marsden Hospital, London and Surrey, UK. Electronic address:
Claudins (CLDNs) play a crucial and indispensable role as fundamental components within the structure of tight junctions. Due to the distinct and unique distribution pattern exhibited by CLDNs in both normal and malignant tissues, these proteins have garnered significant attention as pivotal targets for systemic anti-cancer therapy and as noteworthy diagnostic markers. This review provides a comprehensive and detailed elucidation of the fundamental understanding surrounding CLDNs, their intricate expression patterns, the potential role they play in cancer diagnosis and therapeutic potentials; all encapsulated within a succinct summary of the cutting-edge advancements and the information derived from various clinical trials.
View Article and Find Full Text PDFRev Med Suisse
January 2025
Service d'oncologie, Hôpitaux universitaires de Genève, 1211 Genève 14.
New therapeutic agents in oncology are emerging rapidly, both in terms of the number of approved drugs and the technological and biological innovation of new treatments. Antibody-drug conjugates (ADC) offer a promising cancer therapy by specifically targeting tumor cells. ADC are composed of a monoclonal antibody recognizing the tumor cell via specific antigens, coupled with a potent cytotoxic agent that resembles classical chemotherapy.
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