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Tenapanor (RDX5791, AZD1722), a first-in-class small molecule with minimal systemic availability, is an inhibitor of the sodium/hydrogen exchanger isoform 3. Tenapanor acts locally in the gut, where it reduces absorption of sodium and phosphate. It is being studied in patients with chronic kidney disease requiring dialysis, who are often administered phosphate binders such as sevelamer to help control hyperphosphatemia. We investigated whether coadministration of tenapanor with phosphate binders (sevelamer or calcium-based binders) impacts the pharmacodynamic effects of tenapanor. In vitro studies suggested a binding interaction between tenapanor and sevelamer, but this did not translate into altered pharmacodynamic effects in rats. An open-label, 2-way crossover study was then conducted in healthy volunteers (NCT02346890). This showed that 4 days' treatment with tenapanor hydrochloride (15 mg twice daily) with or without sevelamer carbonate (800 mg 3 times daily) resulted in comparable 24-hour stool and urinary sodium and phosphorus levels. Stool frequency, consistency, and weight were also comparable between the treatments. These results suggest that the binding between sevelamer and tenapanor observed in vitro does not translate into altered pharmacodynamic effects in humans.
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http://dx.doi.org/10.1002/cpdd.307 | DOI Listing |
Talanta
December 2024
Institute of Chemical Biology and Nanomedicine (ICBN), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, China. Electronic address:
Sweat lactate levels are closely related to an individual's physiological state and serve as critical indicators for assessing exercise intensity, muscle fatigue, and certain pathological conditions. Screen-printed electrodes (SPEs) offer a promising avenue for the development of low-cost, high-performance wearable devices for electrochemical sweat analysis. The material composition of SPEs significantly impacts their detection sensitivity and stability.
View Article and Find Full Text PDFInt Urol Nephrol
December 2024
Faculty of Medicine, Mansoura University, Mansoura, Egypt.
Background: Hyperphosphatemia is common in chronic kidney disease (CKD) patients, especially patients on hemodialysis. Tenapanor is a novel drug with fewer side effects and high compliance compared to traditional phosphate binders. We conducted a systematic review and meta-analysis to evaluate the efficacy and safety of tenapanor.
View Article and Find Full Text PDFNefrologia (Engl Ed)
December 2024
Department of Medical Doctor Study Program, Faculty of Medicine, Hasanuddin University, Makassar City, South Sulawesi Province, Indonesia.
Background: Chronic kidney disease (CKD) is a major global health problem. Hyperphosphatemia is frequent in CKD and a reason for increased morbidity and mortality as it generates hyperparathyroidism, high fibroblast growth factor 23 (FGF23), and hypocalcemia. Available hyperphosphatemia therapies still have limitations, including risk of metal overload, cardiovascular calcification, and systemic adverse effects (AEs).
View Article and Find Full Text PDFDrug Dev Ind Pharm
December 2024
Quotient Sciences, Nottingham, UK.
Objective: This pilot study aimed to develop a liquid formulation of tenapanor and evaluate taste and palatability with different sweetener and flavor combinations.
Significance: Tenapanor is a first-in-class, minimally absorbed, small molecule inhibitor of intestinal sodium/hydrogen exchanger 3, indicated (as tablets) to treat adults with constipation-predominant irritable bowel syndrome. It is also approved as add-on therapy to reduce serum phosphorus in adults with chronic kidney disease on dialysis who are intolerant of, or unacceptably responsive to, any dose of phosphate binder therapy.
Cureus
November 2024
Department of Nephrology, Universiti Malaya Medical Centre, Kuala Lumpur, MYS.
Background Calcific uremic arteriolopathy (CUA) is a rare but debilitating disease affecting patients with kidney disease. Reported risk factors of CUA in the literature include female sex, obesity, diabetes mellitus, and vitamin K antagonists' (VKAs) usage. CUA prevalence in Malaysia is unknown and has not been reported before.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!