Liposomal Formulation of Hydroxychloroquine Can Inhibit Autophagy In Vivo by Wieslawa H. Dragowska, Jagbir Singh, Mohamed Wehbe, Malathi Anantha, Katarina Edwards, Sharon M. Gorski, Marcel B. Bally, Ada W. Y. Leung

“…<b>Methods:</b> We developed two liposomal formulations of HCQ: a pH-loaded formulation and a formulation based on copper complexation. The pharmacokinetics of each formulation was evaluated in CD1 mice following intravenous administration. …”
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Neuroprotection by chronic administration of Fluoroethylnormemantine (FENM) in mouse models of Alzheimer's disease by Allison Carles, Aline Freyssin, Sarra Guehairia, Thomas Reguero, Michel Vignes, Hélène Hirbec, Gilles Rubinstenn, Tangui Maurice

“…Here, as drug infusion is likely to better reflect drug bioavailability due to the interspecies pharmacokinetics variation, we analyzed the efficacy of FENM after chronic subcutaneous (SC) infusion, in comparison with IP injections in two AD mouse models, Aβ25–35-injected mice and the transgenic APPswe/PSEN1∂E9 (APP/PS1) line. …”
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Efficacy and Safety Assessment of Antifungal Prophylaxis with Posaconazole Using Therapeutic Drug Monitoring in Pediatric Patients with Oncohematological Disorders—A Single-Centre... by Karolina Liszka, Paweł Marschollek, Dawid Przystupski, Jowita Frączkiewicz, Monika Mielcarek-Siedziuk, Igor Olejnik, Zuzanna Gamrot, Natalia Haze, Agnieszka Kwella, Paulina Zalewska, Matylda Resztak, Marek Ussowicz, Krzysztof Kałwak

“…Materials and methods: In total, 171 oncohematological pediatric patients on posaconazole prophylaxis were included. Full pharmacokinetic posaconazole profiles were assessed in 51 children. …”
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Development of [F]FPy-WL12 as a PD-L1 Specific PET Imaging Peptide by Wojciech G. Lesniak PhD, Ronnie C. Mease PhD, Samit Chatterjee PhD, Dhiraj Kumar PhD, Ala Lisok MA, Bryan Wharram MS, Venkateswara Rao Kalagadda PhD, Leisha A. Emens MD, PhD, Martin G. Pomper MD, PhD, Sridhar Nimmagadda PhD

“…The majority of [ 18 F]FPy-WL12 radioactivity was localized in the tumors, liver, and kidneys indicating the need for optimization of the labeling strategy to improve the in vivo pharmacokinetics of the radiotracer.…”
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First-in-human phase 1 study of the arginase inhibitor INCB001158 alone or combined with pembrolizumab in patients with advanced or metastatic solid tumours by Michael Smith, Aung Naing, Todd Bauer, Kyriakos P Papadopoulos, Osama Rahma, Elena Garralda, Glenn J Hanna, Michael J Pishvaian, Xuejun Chen, Sven Gogov, Omar Saavedra, Howard Kallender, LuLu Cheng, Emil Kuriakose

“…Objective The arginase inhibitor INCB001158 was evaluated for safety (primary endpoint) in locally advanced or metastatic solid tumours; pharmacokinetics, pharmacodynamics and efficacy were also assessed.Methods and analysis In this non-randomised, open-label, three-part phase 1 study, INCB001158 was orally administered two times per day as monotherapy or in combination with intravenous pembrolizumab 200 mg every 3 weeks. …”
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Proceedings of the 14th European immunogenicity platform open symposium on immunogenicity of biopharmaceuticals by Sophie Tourdot, Daniel Baltrunkonis, Sofie Denies, Viswanath Devanarayan, Joanna Grudzinska-Goebel, Arno Kromminga, Gregor P. Lotz, Laurent Malherbe, Lydia Michaut, Karin N. Weldingh, Joao A. Pedras-Vasconcelos, Laura. I. Salazar-Fontana, Sebastian Spindeldreher, Zuben Sauna, Veerle Snoeck, Daniela Verthelyi, Daniel Kramer

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PET imaging of 52Mn labeled DOTATATE and DOTAJR11 by James M. Omweri, Hailey A. Houson, Shannon E. Lynch, Volkan Tekin, Anna G. Sorace, Suzanne E. Lapi

“…As an agonist, [68Ga]Ga-DOTATATE has demonstrated significant internalization upon interaction with receptor ligands, whereas [68Ga]Ga-DOTA-JR11(as an antagonist) exhibits limited internalization but better pharmacokinetics and increased tumor uptake. The goal of this study was to label both DOTATATE and DOTA-JR11 peptides with 52Mn in high radiochemical yields (RCY) and sufficient specific activity. …”
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Phase I Trial of Upamostat Combined With Gemcitabine in Locally Unresectable or Metastatic Pancreatic Cancer: Safety and Preliminary Efficacy Assessment by Xiuping Lai, Di Cheng, Huixin Xu, Jingshu Wang, Xiaozhi Lv, Herui Yao, Liuning Li, Junyan Wu, Suiwen Ye, Zhihua Li

“…Safety profiles, tumor response (including response rate and progression‐free survival), pharmacokinetics, and changes in CA199 and D‐dimer levels were assessed. …”
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Oleanolic Acid Cubic Liquid Crystal Nanoparticle-Based Thermosensitive Gel Attenuates Depression Symptoms in Chronic Unpredictable Mild Stress Rats by Shi Z, Wang Q, Li Q, Jia F, Xu W

“…This study aimed to evaluate the effects of OANG on depression symptoms in rats.Methods: OANG was prepared using Poloxamer F127 and F68 as the gel matrix, and the ratios of F127 and F68 were investigated. The pharmacokinetics of OANG was studied in rats, and OA content was determined using liquid chromatography-mass spectrometry (LC-MS). …”
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Transport and inhibition of the sphingosine-1-phosphate exporter SPNS2 by Huanyu Z. Li, Ashley C. W. Pike, Yung-Ning Chang, Dheeraj Prakaash, Zuzana Gelova, Josefina Stanka, Christophe Moreau, Hannah C. Scott, Frank Wunder, Gernot Wolf, Andreea Scacioc, Gavin McKinley, Helena Batoulis, Shubhashish Mukhopadhyay, Andrea Garofoli, Adán Pinto-Fernández, Benedikt M. Kessler, Nicola A. Burgess-Brown, Saša Štefanić, Tabea Wiedmer, Katharina L. Dürr, Vera Puetter, Alexander Ehrmann, Syma Khalid, Alvaro Ingles-Prieto, Giulio Superti-Furga, David B. Sauer

“…SPNS2 also exports the S1P-mimicking FTY720-P (Fingolimod) and thereby is central to the pharmacokinetics of this drug when treating multiple sclerosis. …”
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Efficacy of intranasal naloxone compared to other administration routes in prehospital opioid overdose management and beyond: a narrative review by Luigi Venuso, Francesco Ricciardi, Antonio Del Prete, Michele Virgolesi, Gianluca Pucciarelli, Luigi Langella, Teresa Rea

“…The review shows that intranasal naloxone, especially at a 2 mg dose, achieves plasma levels similar to intramuscular formulations and has linear pharmacokinetics across dosages. While its bioavailability is lower (46% to 50%) compared to intravenous administration, it is a safer and more practical option for non-clinical settings. …”
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Helicobacter pylori infection at long-term treatment by proton pump inhibitors for acid-related diseases (Literature review and resolution of Advisory council, March 22, 2018) by V. T. Ivashkin, I. V. Mayev, R. A. Abdulkhakov, O. P. Alekseyeva, S. A. Alekseyenko, A. Yu. Baranovsky, Ye. K. Baranskaya, I. L. Klyaritskaya, N. V. Korochanskaya, Yu. A. Kucheryavy, T. L. Lapina, M. F. Osipenko, V. I. Simanenkov, G. N. Tarasova, A. S. Trukhmanov, I. B. Khlynov, A. A. Sheptulin

“…The choice of specific PPI for treatment of patients with GERD and other acid-related diseases, carrying out H. pylori eradication therapy or substitution of one PPI agent to another are individualized and depend on the indications registered in the drugs administration instructions, features of its pharmacokinetics and pharmacodynamics, possible drug-to-drug interactions. …”
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Evaluation of the effectiveness of GASMAN anesthesia simulation software combined with case-based learning versus traditional lecture-based learning in inhalation anesthesia educat... by Chao Chen, Chao Chen, Shengfeng Yang, Xinglong Xiong, Xinglong Xiong, Yewei Shi, Yewei Shi, Zhenyan Zhu, Zhenyan Zhu, Jing Shi, Jing Shi

“…These scenarios were integrated with the GASMAN software to provide interactive simulations, enhancing students’ understanding of pharmacokinetics and pharmacodynamics. Teaching effectiveness was evaluated through expert assessments and student feedback, with learning outcomes compared via post-course assessments.ResultsThe IGC group scored significantly higher in student evaluations in areas such as comprehending and mastering theoretical knowledge, resolving clinical challenges, nurturing clinical reasoning, increasing learning interest, enhancing learning efficiency, consolidating memory, improving analytical skills, and refining application proficiency (adjusted P &lt; 0.001), however, there were no significant differences between the two groups in the improvement of practical skills. …”
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Computer-assisted discovery of natural inhibitors for platelet-derived growth factor alpha as novel therapeutics for thyroid cancer by Hira Khalid, Farah Sattar, Iqra Ahmad, Valdir Ferreira de Paula Junior, Valdir Ferreira de Paula Junior, Umar Nishan, Umar Nishan, Riaz Ullah, Hanna Dib, Khaled W. Omari, Mohibullah Shah, Mohibullah Shah

“…Not only the top 7 hits exhibited higher docking scores in docking simulation but also optimal drug-likeness and non-toxic profiles in pharmacokinetics analysis among 119 compounds. Our top hits are non-mutagenic, can cross the blood-brain barrier, and inhibit p-glycoprotein, while the N-cis-feruloyltyramine has the potential to become a lead compound. …”
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Lucidin from <i>Rubia cordifolia</i> Outperforms FDA-Approved Lapatinib as a Potential Multitargeted Candidate for Breast Cancer Signalling Proteins by Akram Ahmed Aloqbi, Hadil Alahdal, Amany I. Alqosaibi, Mashael M. Alnamshan, Ibtesam S. Al-Dhuayan, Ahood A. Al-Eidan, Hind A. S. Alzahrani, Nouf K. ALaqeel, Fatmah Hazza Alsharif, Abeer Al Tuwaijri

“…Comparative analyses of Lucidin and Lapatinib included molecular interaction fingerprints, pharmacokinetics, WaterMap computations (5 ns) to assess water thermodynamics and binding interactions, and Molecular Dynamics Simulations (100 ns) in water to evaluate complex stability and dynamic behaviour. …”
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Immunogenicity in humans of a transdermal multipeptide melanoma vaccine administered with or without a TLR7 agonist by Craig L Slingluff, Gina R Petroni, Walter C Olson, Kimberly A Chianese-bullock, Donna Deacon, Mark Smolkin, William W Grosh, Max O Meneveau, Kevin T Lynch, Elise P Salerno, Elizabeth Woodson, James W Patterson

“…Further study is warranted into the pharmacokinetics and immunobiology of TLR agonists as vaccine adjuvants during transcutaneous application. …”
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Identification of promising SARS-CoV-2 main protease inhibitor through molecular docking, dynamics simulation, and ADMET analysis by Ganesh Sharma, Neeraj Kumar, Chandra Shekhar Sharma, Taha Alqahtani, Yewulsew Kebede Tiruneh, Sharifa Sultana, Gabriel Vinícius Rolim Silva, Gabriela de Lima Menezes, Magdi E. A. Zaki, Jonas Ivan Nobre Oliveira

“…The physicochemical properties, pharmacokinetics, and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) profiles were evaluated to determine drug similarity and safety. …”
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Safety and Efficacy of 188-Rhenium-Labeled Antibody to Melanin in Patients with Metastatic Melanoma by M. Klein, M. Lotem, T. Peretz, S. T. Zwas, S. Mizrachi, Y. Liberman, R. Chisin, J. Schachter, I. G. Ron, G. Iosilevsky, J. A. Kennedy, E. Revskaya, A. W. de Kater, E. Banaga, V. Klutzaritz, N. Friedmann, E. Galun, G. L. DeNardo, S. J. DeNardo, A. Casadevall, E. Dadachova, G. B. Thornton

“…The objectives of Phase Ia/Ib studies were to evaluate the safety, pharmacokinetics, dosimetry, and antitumor activity of 188Re-6D2, a 188-Rhenium-labeled antibody to melanin. …”
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Microneedle technology for enhanced topical treatment of skin infections by Tingting Peng, Yangyan Chen, Xuanyu Luan, Wanshan Hu, Wentao Wu, Bing Guo, Chao Lu, Chuanbin Wu, Xin Pan

“…Also, integrating biosensing functionality to MNs offers point-of-care wearable medical devices for analyzing specific pathogens, disease status, and drug pharmacokinetics, thus providing personalized therapy for skin infections. …”
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TIGIT inhibitor M6223 as monotherapy or in combination with bintrafusp alfa in patients with advanced solid tumors: a first-in-human, phase 1, dose-escalation trial by Wei Gao, Ping Hu, Aung Naing, Meredith McKean, Anthony Tolcher, Lillian L Siu, Keyvan Tadjalli-Mehr, Anja Victor, Emilia Richter, Marco A F Nogueira Filho, Thomas Kitzing, Stephan Gleicher, Daniel Holland

“…M6223±BA displayed a linear pharmacokinetic profile. Anti-TIGIT mode-of-action-related pharmacodynamic effects were observed in peripheral blood and in tumor tissue. …”
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