Synthesis, evaluation of the biological activity against Trypanosoma cruzi and Leishmania donovani. Preliminary in silico ADMET studies of 5-nitroimidazole derivatives by Miguel A. Rodríguez, Ali Mijoba, Nereida J. Parra-Giménez, Zuleyma Blanco, Katiuska Chávez, Alirica I. Suárez, Esteban Fernandez-Moreira, Hegira Ramírez, Jaime E. Charris

“…The toxicity (ADME/Tox) assessment study were carried out to predict the molecular properties associated with pharmacokinetic aspects of novel compounds. The trypanocidal and leishmanicidal activities of all synthesized hybrids were evaluated, compounds 7a and 8b were active against the epimastigote form of T. cruzi. …”
Get full text

Clonazepam as Agonist Substitution Treatment for Benzodiazepine Dependence: A Case Report by Angelo Giovanni Icro Maremmani, Luca Rovai, Fabio Rugani, Silvia Bacciardi, Matteo Pacini, Liliana Dell'Osso, Icro Maremmani

“…We decided to use clonazepam for its pharmacokinetic properties. The advantage of choosing a slow-onset, long-lasting BZD for the treatment of our patient was that it led us to a remarkable improvement in the clinical situation, including the cessation of craving, absence of withdrawal symptoms, reduced anxiety, improvements in social functioning, and a better cognition level.…”
Get full text

Feasibility of Imaging Myelin Lesions in Multiple Sclerosis by Maria I. Zavodszky, John F. Graf, Cristina A. Tan Hehir

“…Physiology-based pharmacokinetic modeling combined with PET image simulation applied to a brain model was used to examine whether such an agent would allow the differentiation of artificial lesions 4–10 mm in diameter from the surrounding normal-looking white and gray matter. …”
Get full text

Reconstruction of Exposure to m-Xylene from Human Biomonitoring Data Using PBPK Modelling, Bayesian Inference, and Markov Chain Monte Carlo Simulation by Kevin McNally, Richard Cotton, John Cocker, Kate Jones, Mike Bartels, David Rick, Paul Price, George Loizou

“…We investigated the integration of physiologically based pharmacokinetic modelling, global sensitivity analysis, Bayesian inference, and Markov chain Monte Carlo simulation to obtain a population estimate of inhalation exposure to m-xylene. …”
Get full text

A SYSTEMATIC REVIEW OF THE USE OF TULATHROMYCIN IN VETERINARY MEDICINE by Carmen (Pop) Moldovan, Alexandra Dreancă, Oana Rotar, Mihai Madru, Ioan Marcus

“…Key studies demonstrate that tulathromycin is effective in treating bacterial pathogens responsible for respiratory disease, including Mannheimia haemolytica and Pasteurella multocida. The pharmacokinetic properties of tulathromycin, characterized by rapid absorption, extensive tissue distribution, and prolonged elimination half-life, contribute to its therapeutic advantages. …”
Get full text

Nivolumab plasma concentration and clearance associated with overall survival in patients with renal cell carcinoma by Aurélien Marabelle, Laurence Albiges, Angelo Paci, Cécile Dalban, David Combarel, Sophie Broutin, Christophe Maritaz, Louis Blondel

“…Here we describe the development of a new population pharmacokinetic (PPK) model in patients treated with nivolumab in clinical trials. …”
Get full text

Solid Self-Microemulsifying Drug Delivery System for Improved Oral Bioavailability of Relugolix: Preparation and Evaluation by Li ZL, Deng GX, Fang CZ, Zhao YQ, Yuan J, Chen L, Zhong HJ, Guo F

“…In vitro cellular uptake experiments revealed that the uptake of RLGL-S-SMEDDS by Caco-2 cells was three times higher than that of free RLGL, and that S-SMEDDS can enhance the drug absorption through lymphatic absorption and inhibition of intestinal transporter. In vivo pharmacokinetic evaluation demonstrated that the oral bioavailability of RLGL-S-SMEDDS was 1.9 times higher than that of RLGL-suspensions. …”
Get full text

Translation of PET radiotracers for cancer imaging: recommendations from the National Cancer Imaging Translational Accelerator (NCITA) consensus meeting by Martina A. McAteer, Daniel R. McGowan, Gary J. R. Cook, Hing Y. Leung, Tony Ng, James P. B. O’Connor, Luigi Aloj, Anna Barnes, Phil J. Blower, Kevin M. Brindle, John Braun, Craig Buckley, Daniel Darian, Paul Evans, Vicky Goh, David Grainger, Carol Green, Matt G. Hall, Thomas A. Harding, Catherine D. G. Hines, Simon J. Hollingsworth, Penny L. Hubbard Cristinacce, Rowland O. Illing, Martin Lee, Baptiste Leurent, Sue Mallett, Radhouene Neji, Natalia Norori, Nora Pashayan, Neel Patel, Kieran Prior, Thomas Reiner, Adam Retter, Alasdair Taylor, Jasper van der Aart, Joseph Woollcott, Wai-Lup Wong, Jan van der Meulen, Shonit Punwani, Geoff S. Higgins

“…For evaluating established radiotracers in new cancer types, in vitro and preclinical studies were considered unnecessary, clinical pharmacokinetic studies were considered appropriate, and clinical dosimetry and biodistribution studies were considered unnecessary, if sufficient previous data existed. …”
Get full text

Efficacy of esomeprazole at treatment of patients with gastroesophageal reflux disease by Yu. V. Yevsyutina

“…Esomeprazole, in particular generic drug Emanera, is one of the most effective and safe antisecretory drugs. Pharmacokinetic and pharmacodynamic properties of the drug determined its ability to relief heartburn faster than other PPIs, to provide higher rate of erosion healing than omeprazole. …”
Get full text

A Novel Polyacrylamide Magnetic Nanoparticle Contrast Agent for Molecular Imaging using MRI by Bradford A. Moffat, G. Ramachandra Reddy, Patrick McConville, Daniel E. Hall, Thomas L. Chenevert, Raoul R. Kopelman, Martin Philbert, Ralph Weissleder, Alnawaz Rehemtulla, Brian D. Ross

“…Administration of PAM nanoparticles into rats bearing orthotopic 9L gliomas allowed quantitative pharmacokinetic analysis of the uptake of nanoparticles in the vasculature, brain, and glioma. …”
Get full text

GutBugDB: a web resource to predict the human gut microbiome-mediated biotransformation of biotic and xenobiotic molecules by Usha Longwani, Ashok K. Sharma, Aditya S. Malwe, Shubham K. Jaiswal, Vineet K. Sharma

“…There has been a growing recognition of the significant role played by the human gut microbiota in altering the bioavailability as well as the pharmacokinetic and pharmacodynamic aspects of orally ingested xenobiotic and biotic molecules. …”
Get full text

Low‐dimensional neural ordinary differential equations accounting for inter‐individual variability implemented in Monolix and NONMEM by Dominic Stefan Bräm, Bernhard Steiert, Marc Pfister, Britta Steffens, Gilbert Koch

“…The potential of such implementations is shown on various demonstrational datasets available in the Monolix model library, including pharmacokinetic (PK), pharmacodynamic (PD), target‐mediated drug disposition (TMDD), and survival analyses. …”
Get full text

Diosgenin: Recent Highlights on Pharmacology and Analytical Methodology by Mafalda Jesus, Ana P. J. Martins, Eugenia Gallardo, Samuel Silvestre

“…Due to its pharmacological and industrial importance, several extraction and analytical procedures have been developed and applied over the years to isolate, detect, and quantify diosgenin, not only in its natural sources and pharmaceutical compositions, but also in animal matrices for pharmacodynamic, pharmacokinetic, and toxicological studies. Within these, HPLC technique coupled to different detectors is the most commonly analytical procedure described for this compound. …”
Get full text

Grape Seed Procyanidin Extract Improves Insulin Production but Enhances Bax Protein Expression in Cafeteria-Treated Male Rats by Lídia Cedó, Anna Castell-Auví, Victor Pallarès, Mayte Blay, Anna Ardévol, Montserrat Pinent

“…Considering that pharmacokinetic and pharmacodynamic parameters in females are different from these parameters in males, the aim of the present study was to evaluate the effects of GSPE on male Wistar cafeteria-induced obese rats. …”
Get full text

Effective cancer immunotherapy combining mRNA-encoded bispecific antibodies that induce polyclonal T cell engagement and PD-L1-dependent 4-1BB costimulation by Oana Hangiu, Oana Hangiu, Oana Hangiu, Rocío Navarro, Susana Frago, Laura Rubio-Pérez, Laura Rubio-Pérez, Laura Rubio-Pérez, Antonio Tapia-Galisteo, Antonio Tapia-Galisteo, Antonio Tapia-Galisteo, Laura Díez-Alonso, Laura Díez-Alonso, Laura Díez-Alonso, Marina Gómez-Rosel, Marina Gómez-Rosel, Marina Gómez-Rosel, Noelia Silva-Pilipich, Noelia Silva-Pilipich, Lucía Vanrell, Cristian Smerdou, Cristian Smerdou, Kenneth A. Howard, Laura Sanz, Luis Álvarez-Vallina, Luis Álvarez-Vallina, Luis Álvarez-Vallina, Marta Compte

“…The mRNAs encoding both bispecific LiTERNA and Albu-LiTCoRNA, showed similar binding specificity and in vitro function to their protein analogues. Pharmacokinetic studies demonstrated sustained expression of both bispecific antibodies following intravenous administration of the mRNAs formulated using a polymer/lipid-based nanoparticle (LNP) but different pharmacokinetic profiles, shorter for the TCE and longer for the PD-L1 x 4-1BB. …”
Get full text

Scorpion Venom and the Inflammatory Response by Vera L. Petricevich

“…Scorpion venoms consist of a complex of several toxins that exhibit a wide range of biological properties and actions, as well as chemical compositions, toxicity, and pharmacokinetic and pharmacodynamic characteristics. These venoms are associated with high morbility and mortality, especially among children. …”
Get full text

Receptor Inhibitors in Acute Coronary Syndromes: What Is New on the Horizon? by Adriana Dana Oprea, Wanda M. Popescu

“…Variable response to clopidogrel has received close attention, and pharmacokinetic, pharmacodynamic, and pharmacogenomic factors have been identified as culprits. …”
Get full text

2-Amino-1,3,4-thiadiazoles as prospective agents in trypanosomiasis and other parasitoses by Serban Georgeta

“…The chemical, physical and pharmacokinetic properties recommend 1,3,4-thiadiazole ring as a target in drug development. …”
Get full text

Imidazole: Having Versatile Biological Activities by Amita Verma, Sunil Joshi, Deepika Singh

“…Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. …”
Get full text

Plucked Human Hair Shafts and Biomolecular Medical Research by Kevin Schembri, Christian Scerri, Duncan Ayers

“…Furthermore, current diagnostic and clinical applications of plucked hair follicles include their use as autologous and/or three-dimensional epidermal equivalents, together with their utilization as surrogate tissue in pharmacokinetic and pharmacodynamics studies. Consequently, the use of noninvasive diagnostic procedures on hair follicle shafts, posing as a surrogate molecular model for internal organs in the individual patient for a spectrum of human disease conditions, can possibly become a reality in the near future.…”
Get full text