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Brain distribution study of [C]-Riluzole following intranasal administration in mice.
Int J Pharm
January 2025
Institute of Pharmaceutical Science, Faculty of Life Sciences & Medicine, King's College London, London, United Kingdom; Department of Pharmacology and Pharmacy, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong Special Administrative Region of China. Electronic address:
Amyotrophic lateral sclerosis (ALS) presents a substantial challenge due to its complex nature, limited effective treatment options, and modest benefits from current therapies in slowing disease progression. This study explores the potential of intranasal (IN) delivery to enhance the CNS delivery of riluzole (RLZ), a standard ALS treatment which is subject to blood-brain barrier efflux mechanisms. Additionally, the impact of elacridar (ELC), an efflux pump inhibitor, on IN RLZ CNS bioavailability was examined.
View Article and Find Full Text PDFAncillary subunits KChIP2c and DPP6 differentially modulate the inhibition of Kv4.2 channels by riluzole.
Eur J Pharmacol
January 2025
Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Av. 25 de Julio 965 Col, Villas San Sebastián, Colima, COL, 28045, Mexico. Electronic address:
In native tissue, Kv4.2 channels associate with the ancillary subunits Kv channels interacting proteins (KChIPs) and dipeptidyl peptidase-related proteins (DPPs) to evoke rapidly activating/inactivating currents in the heart (I) and brain (I). Despite extensive knowledge of Kv4.
View Article and Find Full Text PDFExploring the Therapeutic Potential of N-Methyl-D-Aspartate Receptor Antagonists in Neuropathic Pain Management.
Int J Mol Sci
October 2024
Faculty of Pharmacy, "Ovidius" University of Constanța, Căpitan Aviator Al. Şerbănescu 6, 900470 Constanța, Romania.
Neuropathic pain (NeP) is a complex and debilitating condition that impacts millions of people globally. Although various treatment options exist, their effectiveness is often limited, and they can be accompanied by significant side effects. In recent years, there has been increasing interest in targeting the N-methyl-D-aspartate receptor (NMDAR) as a potential therapeutic approach to alleviate different types of neuropathic pain.
View Article and Find Full Text PDFRiluzole Enhancing Anti-PD-1 Efficacy by Activating cGAS/STING Signaling in Colorectal Cancer.
Mol Cancer Ther
January 2025
Department of Cancer Biology and Genetics, James Comprehensive Cancer Center, Wexner Medical Center, The Ohio State University, Columbus, Ohio.
Colorectal cancer is the second leading cause of cancer mortality in the United States. Although immune checkpoint blockade therapies including anti-PD-1/PD-L1 have been successful in treating a subset of patients with colorectal cancer, the response rates remain low. We have found that riluzole, a well-tolerated FDA-approved oral medicine for treating amyotrophic lateral sclerosis, increased intratumoral CD8+ T cells and suppressed tumor growth of colon cancer cells in syngeneic immune-competent mice.
View Article and Find Full Text PDFTofersen for SOD1 ALS.
Neurodegener Dis Manag
October 2024
Department of Neurology, Washington University School of Medicine, Saint Louis, MO 63110, USA.
Article Synopsis
- Amyotrophic lateral sclerosis (ALS) is a complex neurological disease that impacts muscle control, making research and clinical trials challenging due to its varied nature.
- Genetic mutations causing ALS, particularly those involving SOD1, allow for targeted treatment strategies, such as the 'knock-down' approach that reduces harmful protein production.
- Tofersen, an experimental treatment that decreases SOD1 mRNA, showed promising biomarker results, and although its Phase III trial didn’t hit its main goal, follow-up data indicate it may help slow down the progression of the disease in SOD1 ALS patients.
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