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Effect of Lemborexant on Daytime Functioning in Adults With Insomnia: Patient-Reported Outcomes From a Phase 3 Clinical Trial.
Prim Care Companion CNS Disord
January 2025
Eisai Inc, Nutley, New Jersey.
Insomnia and some insomnia treatments can impact an individual's daytime functioning. Here, we performed post hoc analyses of patient-reported outcomes from a phase 3 clinical trial to assess the impact of lemborexant (LEM), a dual orexin receptor antagonist, on daytime functioning. Adults with insomnia were randomized 1:1:1 to receive placebo, LEM 5 mg (LEM5) or LEM 10 mg (LEM10) for 6 months.
View Article and Find Full Text PDFSulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDFEvaluating the Antidiabetic Activity of Latex in Alloxan-Induced Diabetic Rats and the Development of a Novel Effervescent Granule-Based Delivery System.
ScientificWorldJournal
January 2025
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Sana'a University, Sana'a, Yemen.
Ethnomedicine exhibits potential in developing affordable effective antidiabetic agents. This work aimed to explore the antidiabetic properties of latex extract both in vivo, utilizing alloxan-induced diabetic rats, and in vitro, through -amylase enzyme testing. Additionally, it sought to formulate optimal effervescent granules derived from the extract.
View Article and Find Full Text PDFA physiologically-based quantitative systems pharmacology model for mechanistic understanding of the response to alogliptin and its application in patients with renal impairment.
J Pharmacokinet Pharmacodyn
January 2025
Department of Clinical Pharmacy and Pharmacy Administration, West China school of Pharmacy, Sichuan University, Chengdu, 610064, China.
Alogliptin is a highly selective inhibitor of dipeptidyl peptidase-4 and primarily excreted as unchanged drug in the urine, and differences in clinical outcomes in renal impairment patients increase the risk of serious adverse reactions. In this study, we developed a comprehensive physiologically-based quantitative systematic pharmacology model of the alogliptin-glucose control system to predict plasma exposure and use glucose as a clinical endpoint to prospectively understand its therapeutic outcomes with varying renal function. Our model incorporates a PBPK model for alogliptin, DPP-4 activity described by receptor occupancy theory, and the crosstalk and feedback loops for GLP-1-GIP-glucagon, insulin, and glucose.
View Article and Find Full Text PDFPopulation pharmacokinetics and exposure-response analysis of durvalumab in combination with gemcitabine and cisplatin in patients with advanced biliary tract cancer.
Cancer Chemother Pharmacol
January 2025
Clinical Pharmacology & Quantitative Pharmacology, BioPharmaceuticals R&D, AstraZeneca, Waltham, MA, USA.
Purpose: Durvalumab in combination with gemcitabine/cisplatin has shown a favorable benefit-risk profile in the TOPAZ-1 study for advanced biliary tract cancers (BTC). This analysis evaluated the population pharmacokinetics (PopPK) of durvalumab, and exposure-response for efficacy and safety (ERES) of TOPAZ-1.
Methods: The PopPK model for durvalumab was updated using data from 5 previously analysed studies and TOPAZ-1.
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