This paper gives a brief review of the pharmacokinetic studies performed on pirenzepine (L S 519 Cl2, Gastrozepin hitherto. Particular attention will be paid thereby to the clinical significance of the pharmacokinetic parameters.
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AAPS J
January 2025
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, State University of New York at Buffalo, 160 Hayes Rd, Buffalo, New York, 14214, USA.
The study quantitatively analyzes and compares the pharmacokinetics (PK) of methylprednisolone (MPL) in humans upon administration of various dosage forms. The PK parameters and profiles of MPL in healthy subjects were collected from 22 literature sources. A minimal physiologically based pharmacokinetic (mPBPK) model consisting of blood and two tissue (lumped liver and kidney, remainder) compartments with nonlinear tissue partitioning was applied to describe MPL disposition.
View Article and Find Full Text PDFLancet Oncol
January 2025
Department of Medical Oncology, Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-sen University, Research Unit of Precision Diagnosis and Treatment for Gastrointestinal Cancer, Chinese Academy of Medical Sciences, Guangzhou, China. Electronic address:
Background: CMG901 is a novel first-in-class antibody-drug conjugate with a humanised anticlaudin 18.2 antibody linked to microtubule-disrupting agent monomethyl auristatin E. We aimed to assess the antitumour activity and safety of CMG901 in patients with advanced gastric or gastro-oesophageal junction cancer and other solid tumours.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Department of Pharmacy, Institute of Pharmaceutical Science and Technology, College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do, 15588, Republic of Korea. Electronic address:
JNK3, a brain-specific stress-activated protein kinase, plays a critical role in Alzheimer's disease pathogenesis through phosphorylation of Tau and APP. This study aimed to develop selective JNK3 inhibitors based on a pyrazole scaffold, focusing on (E)-1-(2-aminopyrimidin-4-yl)-4-styryl-1H-pyrazole-3-carboxamide derivatives. Through systematic structural modifications and extensive SAR analysis, we identified compounds 24a and 26a as highly potent JNK3 inhibitors, with IC values of 12 and 19 nM, respectively.
View Article and Find Full Text PDFAm J Gastroenterol
December 2024
Adiso Therapeutics, Inc, Concord, Massachusetts, USA.
Objectives: Ulcerative colitis (UC) is characterized by colonic inflammation, with neutrophils playing a key role in UC activity, prognosis, and response to therapies. Current UC therapeutics can have significant side effects and limited efficacy. ADS051 is a novel, oral, gut-restricted small molecule that modulates neutrophil migration and activation without in vitro suppression of T-cell activation.
View Article and Find Full Text PDFPLoS One
January 2025
Faculty of Pharmacy, Sardar Bahadur Khan Women University Quetta, Quetta, Pakistan.
Controlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticles were fabricated through a simple solvent evaporation method, employing various drug-to-polymer ratios to formulate different controlled-release batches labeled as F1 to F5.
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