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Cancer-Therapy-Induced Cardiotoxicity: Results of the Analysis of the UK Yellow Card Adverse Drug Reaction (ADR) Reporting.
Cancers (Basel)
December 2024
School of Life and Medical Sciences, University of Hertfordshire, Hatfield AL10 9AB, UK.
Non-small cell lung cancer (NSCLC) is a predominant cause of oncological mortality in the United Kingdom. There is a diverse spectrum of therapeutic options available, such as chemotherapies, targeted therapies and immunotherapies, which have significantly advanced patient prognoses. However, despite these advancements, there is an escalating concern regarding the potential cardiotoxic effects associated with these treatments.
View Article and Find Full Text PDFDesign and evaluation of anaplastic lymphoma kinase degraders using a covalent fumarate handle.
Bioorg Med Chem Lett
December 2024
Therapeutics and Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon 34114, Republic of Korea; Medicinal Chemistry and Pharmacology, Korea University of Science and Technology, Daejeon 34113, Republic of Korea. Electronic address:
Targeted protein degradation has emerged as a novel therapeutic paradigm in drug discovery. Despite the FDA approval of anaplastic lymphoma kinase (ALK) inhibitors, the pursuit of compounds with enhanced potency and prolonged efficacy remains crucial to mitigate inevitable adverse effects. In this context, we endeavored to develop ALK degraders utilizing FDA-approved ALK inhibitors-crizotinib, ceritinib, brigatinib, and alectinib-as ALK binders, along with 4-methoxyphenylfumarate as a covalent handle to bind to RNF126 E3 ligase.
View Article and Find Full Text PDFHyperbilirubinemia in a Patient Receiving Alectinib for Anaplastic Lymphoma Kinase Positive Non-Small-Cell Lung Cancer: A Histological Features.
Onco Targets Ther
December 2024
Department of Infectious Disease, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, People's Republic of China.
Background: Alectinib is a second generation of anaplastic lymphoma kinase (ALK) inhibitor that has been approved for the treatment of advanced non-small-cell lung cancer (NSCLC) with ALK rearrangements. Hepatotoxicity is the most common adverse drug reaction. However, there is currently no published report on the pathologic findings of alectinib-induced hyperbilirubinemia.
View Article and Find Full Text PDFSex and Common Germline Variants Affect the Toxicity Profile and Pharmacokinetics of Alectinib: A Nationwide Cohort Study in Patients With ALK-Positive NSCLC.
J Thorac Oncol
November 2024
Department of Medical Oncology, Erasmus MC Cancer Institute, Erasmus University Medical Center, Rotterdam, The Netherlands; Department of Pulmonary Medicine, Erasmus MC Cancer Institute, Erasmus University Medical Center, Rotterdam, The Netherlands.
Article Synopsis
- Alectinib is a treatment for ALK+ non-small cell lung cancer, but many patients experience drug-related toxicity requiring dose adjustments, potentially linked to genetic variants.
- In a study of 215 patients, 47% had severe toxicity, with females being more affected and having higher drug levels. Additionally, specific genetic variants like PPAR-α 209G>A were associated with increased toxicity.
- Identifying these genetic factors could help tailor treatments and reduce adverse effects, suggesting the need for pre-treatment genetic testing and possible dose modifications.
Targeting ErbB and tankyrase1/2 prevent the emergence of drug-tolerant persister cells in ALK-positive lung cancer.
NPJ Precis Oncol
November 2024
Product Research Department, Chugai Pharmaceutical Co., Ltd, Yokohama, Japan.
Targeting the drug tolerant persister (DTP) state in cancer cells should prevent further development of resistance mechanisms. This study explored combination therapies to inhibit alectinib-induced DTP cell formation from anaplastic lymphoma kinase-positive non-small cell lung cancer (ALK + NSCLC) patient-derived cells. After drug-screening 3114 compounds, pan-HER inhibitors (ErbB pathway) and tankyrase1/2 inhibitors (Wnt/β-catenin signaling) emerged as top candidates to inhibit alectinib-induced DTP cells growth.
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