Discovery of Novel Nav1.7-Selective Inhibitors with the 1H-Indole-3-Propionamide Scaffold for Effective Pain Relief by Gaoang Wang, Hang Wu, Yingying Wang, Xiangying Liu, Shuijiao Peng, Wenxing Wang, Meijing Wu, Yifei Liu, Ercheng Wang, Zhe Wang, Lei Xu, Xiaojian Wang, Wei Yang, Haiyi Chen, Xi Zhou, Tingjun Hou

“…Additionally, it displays favorable subtype selectivity and positive drug safety in acute toxicity studies. Pharmacokinetic studies indicate that WN2-R has high bioavailability (F = 20.29%), highlighting its considerable potential for drug development. …”
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CADD based designing and biological evaluation of novel triazole based thiazolidinedione coumarin hybrids as antidiabetic agent by Anchal Sharma, Anmol Narang, Nitish Kumar, Rupali Rana, Megha, Pooja, Muskan Dhir, Harmandeep Kaur Gulati, Jyoti, Aanchal Khanna, Jatinder Vir Singh, Sukhraj Kaur, Preet Mohinder Singh Bedi

“…Compound I-1 was synthesized based on the insights gained from molecular docking and simulations, which helped predict interactions and identify critical structural features. Pharmacokinetic properties were evaluated through drug-likeness and ADMET studies. …”
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Children and providers’ perspectives on once-weekly rifapentine and isoniazid TB preventive therapy by A.J. Marthinus, D.T. Wademan, Z. Saule, Y. Hirsch-Moverman, L. Viljoen, J. Winckler, L. van der Laan, M. Palmer, S.L. Barnabas, R. Boyd, A.C. Hesseling, G. Hoddinott

“…METHODS: Serial, in-depth qualitative interviews with 20 child-caregiver dyads, including 5 children living with HIV (CLWH) and 9 healthcare providers across two study sites implementing a pharmacokinetic and safety trial of 3HP, were analysed deductively. …”
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Nanotherapeutic smart approaches for combating Alzheimer’s disease and overcoming existing obstacles: A novel eco-friendly green approach by Ahmed M. Almehdi, Doha H. Aboubaker, Rania Hamdy, Ali El-Keblawy

“…It depends on enhancing the way that medications are distributed pharmacokinetically throughout the central nervous system. …”
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Identification of Two Flavonoids as New and Safe Inhibitors of Kynurenine Aminotransferase II via Computational and In Vitro Study by Redouane Rebai, Luc Jasmin, Abdennacer Boudah

“…ADMET analysis revealed that the selected compounds have favorable pharmacokinetic parameters, moderate bioavailability, and a safe toxicity profile, which supports their potential use. …”
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PROTACs: Mechanism and Bioavailability enhancement strategies by nanotechnology, RNA viral infections (vaccine strategy) and Prodrug development by Sanaul Mustafa, Md Sabir Hussain Siddiquee

“…The newest approaches in nanotechnology-aided drug delivery and the use of nanocarriers to address the limitations in PROTACs and their pharmacokinetic and pharmacodynamic properties are discussed. …”
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A review on intrathecal administration of medications for leptomeningeal metastases in solid tumors by Xuemei Wang, Chi Yao, Li Quan, Junxiang Zhou

“…It is hoped that future research will focus on exploring more potentially effective anti-tumor drugs for IT treatment, conducting in-depth pharmacokinetic studies, and developing long-acting and low-toxic IT administration regimens for the treatment of meningeal metastases.…”
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Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye by Ahmad Karami, Shahla Mirzaeei, Leila Rezaei, Ali Nokhodchi

“…The inserts were studied for morphology, drug–polymer interaction, physicochemical properties, and in vitro drug-release study. The pharmacokinetic properties of fibers were examined alongside consideration for irritation using a rabbit model and cell compatibility. …”
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Interaction of α-Cembrenediol with Human Serum Albumin Based on Spectroscopic and Computational Analyses by Xian-Kun Su, Zhen-Chun Sun, Chang-You Zhao, Hui Yang, Tian-Ming Zhao, Chao Ma, Guo-Fei Zhu

“…This study offers crucial insights into the interaction between α-cembrenediol and HSA, contributing to an improved understanding of the compound’s pharmacokinetic properties.…”
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Synthesis, in vitro safety and antioxidant activity of new pyrrole hydrazones by Tzankova Diana, Vladimirova Stanislava, Aluani Denitsa, Yordanov Yordan, Peikova Lily, Georgieva Maya

“…“Lipinski’s rule of five” parameters were applied for preliminary evaluation of the pharmacokinetic properties of the target molecules. The initial in vitro safety screening for cytotoxicity (on HepG2 cells) and hemocompatibility (hemolysis assay) showed good safety of the new compounds, where ethyl 5-(4-bromophenyl)-1-(1-(2-(4-hydroxy-3-methoxybenzylidene)-hydrazineyl)-1-oxo-3-phenylpropan-2-yl)-2-methyl-1H-pyr-role-3-carboxylate (4d) and ethyl 5-(4-bromophenyl)-1-(1-(2-(2-hydroxybenzylidene)hydrazineyl)-1-oxo-3-phenylpropan--2-yl)-2-methyl-1H-pyrrole-3-carboxylate (4a) were the least toxic. …”
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System Pharmacological Approach to Investigate and Validate Multitargeted and Therapeutic Effect of Furocoumarins of Apium graveolens L. for Treatment of Kidney Disease by null Yasheshwar, null Gaurav, Rustam Ekkbal, Prem Gupta, Rajendra Gyawali

“…In silico ADME analysis was also performed to investigate the pharmacokinetic behavior of targeted furocoumarins. Results. …”
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Computational design of potent dimeric phenylthiazole NS5A inhibitors for hepatitis C virus by Wissal Liman, Mehdi Oubahmane, Nouhaila Ait Lahcen, Ismail Hdoufane, Driss Cherqaoui, Rachid Daoud, Achraf El Allali

“…Finally, the absorption, distribution, metabolism, excretion, and toxicity analysis were performed to assess the pharmacokinetic and toxicity profiles of the inhibitor candidates. …”
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Characterizing the plasma protein binding profiles of chemistry diversified antisense oligonucleotides in human and mouse plasma using an ultrafiltration method by Cassandra Yun, Kazuki Fukami, Raku Shinkyo, Rongrong (Rosa) Jiang

“…IntroductionPlasma protein binding plays a significant role in influencing the pharmacokinetic and pharmacodynamic properties of drugs. …”
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Antibacterial and Antioxidant Activities of Triterpenoids and Cyclic 1,7-Diarylheptanoids from the Stem Bark of Myrica salicifolia: A Combined Experimental and Computational Study by Abraham Dilnesa Gashaw, Kibrom Gebreheiwot Bedane, Taye B. Demissie, Japheth O. Ombito, Estifanos Ele Yaya, Mekonnen Abebayehu Desta

“…In silico ADMET predictions revealed that compounds 3 and 8 met all the requirements for pharmacokinetic properties.…”
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Optimization of meropenem continuous infusion based on Monte Carlo simulation integrating with degradation study. by Nguyen Tran Nam Tien, Vu Ngan Binh, Pham Thi Thanh Ha, Dang Thi Ngoc Lan, Yong-Soon Cho, Nguyen Phuoc Long, Jae-Gook Shin, Nguyen Hoang Anh, Truong Anh Quan, Do Ngoc Tuan, Nguyen Khac Tiep, Pham The Thach, Nguyen Hoang Anh, Vu Dinh Hoa

“…In-bottle stability data was subsequently integrated as input for a deterministic and stochastic simulation using a published population pharmacokinetic model of critical illness. The impact of the degradation on target attainment at 98%fT>MIC was assessed.…”
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PBPK modeling: What is the role of CYP3A4 expression in the gastrointestinal tract to accurately predict first‐pass metabolism? by Justine Henriot, André Dallmann, François Dupuis, Jérémy Perrier, Sebastian Frechen

“…Physiologically‐based pharmacokinetic (PBPK) modeling is a powerful tool to integrate these processes mechanistically. …”
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RUBY® – a tetravalent (2+2) bispecific antibody format with excellent functionality and IgG-like stability, pharmacology and developability properties by Barnabas Nyesiga, Mattias Levin, Anna Säll, Anna Rosén, Kim Jansson, Sara Fritzell, Karin Hägerbrand, Dietmar Weilguny, Laura von Schantz

“…Also, retained interaction with FcRn is demonstrated to translate into a pharmacokinetic profile in mice and non-human primates that is comparable to mAb controls. …”
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Predicting the clinical subcutaneous absorption rate constant of monoclonal antibodies using only the primary sequence: a machine learning approach by Ronghua Bei, Justin Thomas, Shiven Kapur, Mahlet Woldeyes, Adam Rauk, Jason Robarge, Jiangyan Feng, Kaoutar Abbou Oucherif

“…Our model does not need clinically observed plasma concentration-time data; this is a novel capability not previously achieved in predictive pharmacokinetic models. The model also showed improved performance when benchmarked against a recently reported mechanistic model that relied on clinical data to predict subcutaneous absorption of mAbs. …”
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Optimizing ibrutinib bioavailability: Formulation and assessment of hydroxypropyl-β-cyclodextrin-based nanosponge delivery systems by Sunitha Sampathi, Nitiraj Kulkarni, D.V.R.N. Bhikshapathi, Jagadish V. Tawade, Nainaru Tarakaramu, Rzgar Farooq Rashid, Aziz Kubaev

“…Further validation through zeta sizing, microscopic and spectral analysis, release studies, and pharmacokinetic assessments confirmed the optimization. …”
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Characterization of LY3324954 a long-acting glucagon-receptor agonist by William Roell, Tamer Coskun, Teayoun Kim, Libbey O’Farrell, Jennifer A. Martin, Shelly Nason, Jasmin Hernandez-Alamillo, Saidharshana Dhantu, Daniel J. Drucker, Kyle W. Sloop, James P. Steele, Jorge Alsina-Fernandez, Kirk M. Habegger

“…Methods: LY3324954 was administered to DIO mice, rats, dogs, and monkeys to evaluate pharmacokinetic (PK) profile. Biweekly treatments were conducted in lean and DIO mice to characterize LY3324954-effects on glucose homeostasis and energy balance. …”
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