First-in-human phase 1 dose-escalation results with livmoniplimab, an antibody targeting the GARP:TGF-ß1 complex, as monotherapy and in combination with the anti–PD-1 antibody budi... by Toshio Shimizu, Toshio Shimizu, John Powderly, Albiruni Abdul Razak, Patricia LoRusso, Kathy D. Miller, Steven Kao, Sarah Kongpachith, Catherine Tribouley, Michelle Graham, Brian Stoll, Maulik Patel, Mohammad Sahtout, Martha Blaney, Rachel Leibman, Talia Golan, Talia Golan, Anthony Tolcher

“…Secondary objectives were to assess safety and pharmacokinetics (PK), and exploratory objectives included evaluating preliminary efficacy.ResultsFifty-seven patients enrolled in the dose escalation: 23 in monotherapy cohorts and 34 in combination therapy cohorts. …”
Get full text

Nebulized aminoglycosides for ventilator-associated pneumonia: Methodological considerations and lessons from experimental studies by Jean-Jacques Rouby, Jing Xia, Jayesh Dhanani, Gianluigi Li Bassi, Antoine Monsel, Antoni Torres, Kostoula Arvaniti, Mona Assefi, Matteo Bassetti, Stijn Blot, Matthieu Boisson, Adrien Bouglé, Jean-Michel Constantin, Jayesh Dhanani, George Dimopoulos, Jonathan Dugernier, Pauline Dureau, Stephan Ehrmann, Timothy Felton, Marin Kollef, Antonia Koutsoukou, Anna Kyriakoudi, Pierre-François Laterre, Marc Leone, Victoria Lepère, Gianluigi Li Bassi, Xuelian Liao, Shakti Bedanta Mishra, Olivier Mimoz, Antoine Monsel, Girish B Nair, Michael Niederman, Lucy B Palmer, Jose Manuel Pereira, Konstantinos Pontikis, Garyphalia Poulakou, Jérôme Pugin, Chuanyun Qian, Jie-ming Qu, Jordi Rello, Jason Roberts, Jean-Jacques Rouby, Christina Routsi, Gerald C. Smaldone, Antoni Torres, Melda Türkoğlu, Tobias Welte, Michel Wolff, Xia Jing, Li Yang, Ting Yang, Ying-gang Zhu

“…Lung microdialysis is the only technique able to accurately assess lung pharmacokinetics in animals with inoculation pneumonia treated by nebulized aminoglycosides. …”
Get full text

Clinical and experimental rationale for using phenylephrine with hypromellose for the treatment of extra accommodation strain in patients with myopia by M.V. Makhova, E.V. Shikh, V.V. Strakhov, D.S. Blinov, G.K. Poluosmak, E.V. Semeleva, E.V. Blinova

“…</p> <p> <b>Conclusion</b>: the addition of hypromellose as an excipient to FDF of 2.5% phenylephrine solution helps to optimize pharmacodynamics and pharmacokinetics of the active ingredient by accelerating its inflow in the aqueous humor within the eye anterior chamber, increasing the topical bioavailability, and extending the exposure interval. …”
Get full text

Pegilated interferon alpha 2b «Pegaltevir» chronic hepatitis C treatment (randomized clinical trial) by Marina V. Mayevskaya, Ye. N. Bessonova, P. O. Bogomolov, N. I. Geyvandova, K. V. Zhdanov, V. G. Morozov, V. D. Pasechnikov, I. Yu. Khomenko, A. V. Yagoda, V. T. Ivashkin

“…These qualities formed the basis for development of the Russian pegilated interferon-alpha 2b (Pegaltevir®, LLC «FARMAPARK», Russia) and carrying out doublestaged randomized open clinical trial: study of safety, tolerability and pharmacokinetics of Pegaltevir® at single injection of increasing doses in various groups of healthy volunteers - the I stage; studying of efficacy and safety of Pegaltevir® in comparison to PegIntron® (Schering-Plough, USA) at CHC as a part of double antiviral therapy with ribavirin (Rebetol®, Schering-Plough, USA) - the II stage. …”
Get full text

Hybridization-based discovery of novel quinazoline-2-indolinone derivatives as potent and selective PI3Kα inhibitors by Changqun Liu, Yuening Cao, Yi Zuo, Chaozheng Zhang, Senmiao Ren, Xin Zhang, Chuanqi Wang, Yingjie Zeng, Jie Ling, Yilan Liu, Zixian Chen, Xiujun Cao, Zhengzhi Wu, Chuantao Zhang, Jun Lu

“…Molecular hybridization, with the advantage of simplified pharmacokinetics and drug-drug interactions, emerged as one of the important avenues for discovering potential drugs. …”
Get full text

Macrophage-mimicking nanotherapy for attenuation of acute pancreatitis by Fengyu Shi, Akmal Ergashev, Zhenyan Pan, Hongwei Sun, Lingming Kong, Yuepeng Jin, Tan Zhang, Zhu Liu, Haonan Xie, Jinhui Wang, Huiping Li, Yi Wang, Lifei Zheng, Jianliang Shen, Andreas Herrmann, Gang Chen, Hongru Kong

“…However, systemically administered nanoparticle therapy is rapidly cleared from circulation by the mononuclear phagocyte system (MPS), leading to suboptimal drug concentrations in inflamed tissues and suboptimal pharmacokinetics. To address this challenge, we herein demonstrate a surface masking strategy that involves coating the surface of selenylated Poria cocos polysaccharide nanoparticles with a layer of macrophage plasma membrane to circumvent MPS sequestration, thereby enhancing the therapeutic efficacy of selenylated Poria cocos polysaccharide nanoparticles. …”
Get full text

Microarray Gene Expression Analysis of Murine Tumor Heterogeneity Defined by Dynamic Contrast-Enhanced MRI by Nick G. Costouros, Dominique Lorang, Yantian Zhang, Marshall S. Miller, Felix E. Diehn, Stephen M. Hewitt, Michael V. Knopp, King C. P. Li, Peter L. Choyke, H. Richard Alexander, Steven K. Libutti

“…Using DCE-MRI in a murine subcutaneous tumor model, we were able to perform pharmacokinetic functional analysis of a tumor, coregistration of MRI images with histological cross-sections, immunohistochemistry, laser capture microdissection, and genetic profiling of tumor heterogeneity based on pharmacokinetic parameters. …”
Get full text

Comparative Bioavailability of Four Marketed Sparfloxacin Formulations in Healthy Human Volunteers by K. Ravindra Rao, J. Vijaya Ratna, T. Manikya Rao

“…The objective of the study was to obtain the pharmacokinetic data of four marketed tablet formulations of sparfloxacin and compare the relative bioavailability of the formulations with standard formulation. …”
Get full text

Physiologically Based Structure of Mean Residence Time by Mária Durišová

“…Primarily this is because MRT structures cannot be identified by traditional pharmacokinetic methods used for the determination of MRT. …”
Get full text

Liquid Chromatography-Tandem Mass Spectrometric Assay for Determination of Stavudine in Human Plasma by Fengdan Jin

“…Stavudine was detected by a LC-MS/MS system. The pharmacokinetic parameters of stavudine in different formulations were calculated by noncompartment model statistics. …”
Get full text

Predictive Assessment of the Antiviral Properties of Imperata cylindrica against SARS-CoV-2 by Frank Eric Tatsing Foka, Hazel Tumelo Mufhandu

“…Molecular docking and in silico pharmacokinetic assays were used to assess 72 phytocompounds that are found in I. cylindrica as ligands and Mpro (6LU7) as the target. …”
Get full text

Development and validation of an LC-MS/MS method for the simultaneous estimation of tadalafil and macitentan in rat plasma: Greenness assessment and design of experiment approach by Sravanthi Gandu, Kumaraswamy Gandla, Lalitha Repudi

“…This study presents the development and validation of a sensitive LC-MS/MS method for the simultaneous quantification of tadalafil and macitentan in rat plasma, enabling detailed pharmacokinetic profiling following single-dose administration. …”
Get full text

Prospective Trial of a Novel Nomogram to Achieve Updated Vancomycin Trough Concentrations by Amber R. Wesner, Marcia L. Brackbill, Larissa L. Coyle, Robert S. Kidd

“…Patients were randomized to the active group, dosed using the nomogram, or to the control group, dosed using traditional pharmacokinetic calculations already in place at our institution. …”
Get full text

Antimicrobial Doses in Continuous Renal Replacement Therapy: A Comparison of Dosing Strategies by Anna P. Kempke, Abbie S. Leino, Farzad Daneshvar, John Andrew Lee, Bruce A. Mueller

“…Several guidelines and pharmacokinetic equations have been proposed as tools for CRRT drug dosing. …”
Get full text

Metabolic stability and its role in the discovery of new chemical entities by Słoczyńska Karolina, Gunia-Krzyżak Agnieszka, Koczurkiewicz Paulina, Wójcik-Pszczoła Katarzyna, Żelaszczyk Dorota, Popiół Justyna, Pękala Elżbieta

“…Determination of metabolic profiles of new chemical entities is a key step in the process of drug discovery, since it influences pharmacokinetic characteristics of therapeutic compounds. …”
Get full text

Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties by Kato Bredael, Silke Geurs, Dorien Clarisse, Karolien De Bosscher, Matthias D’hooghe

“…By chemically modifying a hit structure, an improved compound can be obtained in terms of activity, selectivity, and pharmacokinetic ADME (absorption, distribution, metabolism, and excretion) properties. …”
Get full text

Moroccan natural products for multitarget-based treatment of Alzheimer's disease: A computational study. by Fatima Zahra Guerguer, Amal Bouribab, El Mehdi Karim, Meriem Khedraoui, Fatiha Amegrissi, Yasir S Raouf, Abdelouahid Samadi, Samir Chtita

“…These compounds exhibit favourable pharmacokinetic profiles and strong binding affinities for the five key targets associated with the disease. …”
Get full text

Inhaled Therapy in Respiratory Disease: The Complex Interplay of Pulmonary Kinetic Processes by Jens Markus Borghardt, Charlotte Kloft, Ashish Sharma

“…In this review, we describe these pharmacokinetic processes and explain how they may be influenced by drug-, formulation- and device-, and patient-related factors. …”
Get full text

Ciprofloxacin and Clozapine: A Potentially Fatal but Underappreciated Interaction by Jonathan M. Meyer, George Proctor, Michael A. Cummings, Laura J. Dardashti, Stephen M. Stahl

“…Clozapine provides a 50%–60% response rate in refractory schizophrenia but has a narrow therapeutic index and is susceptible to pharmacokinetic interactions, particularly with strong inhibitors or inducers of cytochrome P450 (CYP) 1A2. …”
Get full text

Combined therapeutic option for NDM-producing Serratia Marcescens – an in vitro study from clinical samples by Balbina Chilombo Albano, Leticia Ramos Dantas, Gabriel Burato Ortis, Paula Hansen Suss, Felipe Francisco Tuon

“…Concentrations used were those maximized by pharmacokinetic and pharmacodynamic assessments. Synergy evaluation involved a static macrodilution test followed by a time-kill curve assay. …”
Get full text