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PMC8009078 | core_pubmed_pmc | Pharmacoinformatics-based identification of transmembrane protease serine-2 inhibitors from Morus Alba as SARS-CoV-2 cell entry inhibitors | Pharmacoinformatics-based identification of transmembrane protease serine-2 inhibitors from Morus Alba as SARS-CoV-2 cell entry inhibitors Abstract Abstract Transmembrane protease serine-2 (TMPRSS2) is a cell-surface protein expressed by epithelial cells of specific tissues including those in the aerodigestive tract. I... |
PMC2921067 | core_pubmed_pmc | A model of hypertension and proteinuria in cancer patients treated with the anti-angiogenic drug E7080 | A model of hypertension and proteinuria in cancer patients treated with the anti-angiogenic drug E7080 Abstract Abstract Hypertension and proteinuria are commonly observed side-effects for anti-angiogenic drugs targeting the VEGF pathway. In most cases, hypertension can be controlled by prescription of anti-hypertensiv... |
PMC9786194 | core_pubmed_pmc | Development and Pharmacokinetics of a Novel Acetylsalicylic Acid Dry Powder for Pulmonary Administration | Development and Pharmacokinetics of a Novel Acetylsalicylic Acid Dry Powder for Pulmonary Administration Abstract Aspirin is an historic blockbuster product, and it has been proposed in a wide range of formulas. Due to exacerbation risks, the pulmonary route has been seldom considered as an alternative to conventional ... |
PMC2845558 | core_pubmed_pmc | Quantitative relationship between the octanol/water partition coefficient and the diffusion limitation of the exchange between adipose and blood | Quantitative relationship between the octanol/water partition coefficient and the diffusion limitation of the exchange between adipose and blood Abstract Background The goal of physiologically based pharmacokinetics (PBPK) is to predict drug kinetics from an understanding of the organ/blood exchange. The standard appro... |
PMC6548768 | core_pubmed_pmc | In the Search of Glycoside-Based Molecules as Antidiabetic Agents | In the Search of Glycoside-Based Molecules as Antidiabetic Agents Abstract This review is an effort to summarize recent developments in synthesis of O -glycosides and N -, C -glycosyl molecules with promising antidiabetic potential. Articles published after 2000 are included. First, the O -glycosides used in the treatm... |
PMC4985661 | core_pubmed_pmc | Integrated identification, qualification and quantification strategy for pharmacokinetic profile study of Guizhi Fuling capsule in healthy volunteers | Integrated identification, qualification and quantification strategy for pharmacokinetic profile study of Guizhi Fuling capsule in healthy volunteers Abstract Guizhi Fuling capsule (GZFL), a traditional Chinese medicine formulation, is widely used in China to relieve pain from dysmenorrhea and is now in a Phase II clin... |
PMC6797643 | core_pubmed_pmc | Evaluation of Clinically Relevant Drug–Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial | Evaluation of Clinically Relevant Drug–Drug Interactions and Population Pharmacokinetics of Darolutamide in Patients with Nonmetastatic Castration-Resistant Prostate Cancer: Results of Pre-Specified and Post Hoc Analyses of the Phase III ARAMIS Trial Abstract Abstract Background Darolutamide, an androgen receptor antag... |
PMC6021672 | core_pubmed_pmc | Characterizing Blood-Stage Antimalarial Drug MIC Values In Vivo Using Reinfection Patterns | Characterizing Blood-Stage Antimalarial Drug MIC Values In Vivo Using Reinfection Patterns Abstract ABSTRACT The MIC is an essential quantitative measure of the asexual blood-stage effect of an antimalarial drug. In areas of high malaria transmission, and thus frequent individual infection, patients who are treated wit... |
PMC12273743 | core_pubmed_pmc | Sensitivity of Tepotinib to Inhibitors or Inducers of CYP3A4 and P‐Gp: Drug Interaction Studies and Physiologically‐Based Pharmacokinetic Analysis | Sensitivity of Tepotinib to Inhibitors or Inducers of CYP3A4 and P‐Gp: Drug Interaction Studies and Physiologically‐Based Pharmacokinetic Analysis Abstract ABSTRACT Tepotinib is a highly selective, potent, mesenchymal‐epithelial transition factor (MET) inhibitor, approved for the treatment of non‐small cell lung cancer... |
PMC10014962 | core_pubmed_pmc | A phase I open-label clinical trial to study drug-drug interactions of Dorzagliatin and Sitagliptin in patients with type 2 diabetes and obesity | A phase I open-label clinical trial to study drug-drug interactions of Dorzagliatin and Sitagliptin in patients with type 2 diabetes and obesity Abstract Abstract This is a phase 1, open-label, single-sequence, multiple-dose, single-center trial conducted in the US (NCT03790839), to evaluate the clinical pharmacokineti... |
PMC8885939 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Sitagliptin Phosphate/Metformin Hydrochloride Tablets in Healthy Chinese Subjects: A Randomized, Open-Label, Crossover Study | Pharmacokinetics and Bioequivalence of Sitagliptin Phosphate/Metformin Hydrochloride Tablets in Healthy Chinese Subjects: A Randomized, Open-Label, Crossover Study Abstract Abstract Objective Our objective was to evaluate the pharmacokinetics and bioequivalence of test and reference (JANUMET ® ) formulations of sitagli... |
PMC12558512 | core_pubmed_pmc | Development and characterisation of fast dispersible dimenhydrinate tablets: Compactional study and in-silico PBPK modeling | Development and characterisation of fast dispersible dimenhydrinate tablets: Compactional study and in-silico PBPK modeling Abstract Abstract The aim of this study was to optimize and evaluate dimenhydrinate fast dispersible tablets (50 mg) by utilizing cost effective direct compression method. A total of nine formulat... |
PMC11404431 | core_pubmed_pmc | Potential target and mechanism exploration from α-mangostin against triple-negative breast cancer: An in silico study | Potential target and mechanism exploration from α-mangostin against triple-negative breast cancer: An in silico study Abstract Abstract Triple-negative breast cancer (TNBC) is one of the most common types of serious breast cancer. Due to the absence of therapeutic hormone receptors, TNBC treatment generally involves ch... |
PMC8657617 | core_pubmed_pmc | Recombinant Human HPS Protects Mice and Nonhuman Primates from Acute Liver Injury | Recombinant Human HPS Protects Mice and Nonhuman Primates from Acute Liver Injury Abstract Acute liver injury shares a common feature of hepatocytes death, immune system disorders, and cellular stress. Hepassocin (HPS) is a hepatokine that has ability to promote hepatocytes proliferation and to protect rats from D-gala... |
PMC3405476 | core_pubmed_pmc | A systematic review of the safety and efficacy of artemether-lumefantrine against uncomplicated Plasmodium falciparum malaria during pregnancy | A systematic review of the safety and efficacy of artemether-lumefantrine against uncomplicated Plasmodium falciparum malaria during pregnancy Abstract Malaria during pregnancy, particularly Plasmodium falciparum malaria, has been linked to increased morbidity and mortality, which must be reduced by both preventive mea... |
PMC4467676 | core_pubmed_pmc | Genetic determinants of cocaine-associated agranulocytosis | Genetic determinants of cocaine-associated agranulocytosis Abstract Abstract Background Drug-induced agranulocytosis is a recognized adverse drug event associated with serious infectious complications. Levamisole is an antihelminthic and immunomodulator withdrawn from North American markets in 2005 after reports of agr... |
PMC10622308 | core_pubmed_pmc | Local application of engineered insulin-like growth factor I mRNA demonstrates regenerative therapeutic potential in vivo | Local application of engineered insulin-like growth factor I mRNA demonstrates regenerative therapeutic potential in vivo Abstract Abstract Insulin-like growth factor I (IGF-I) is a growth-promoting anabolic hormone that fosters cell growth and tissue homeostasis. IGF-I deficiency is associated with several diseases, i... |
PMC11672196 | core_pubmed_pmc | Safety and Phosphate‐Binding Capacity of Oxylanthanum Carbonate in Healthy Volunteers | Safety and Phosphate‐Binding Capacity of Oxylanthanum Carbonate in Healthy Volunteers Abstract ABSTRACT Despite the widespread use of currently available serum phosphate management options, elevated serum phosphate is common in patients with end‐stage kidney disease on dialysis. Characteristics of currently available p... |
PMC8833153 | core_pubmed_pmc | Randomized Trial on Echocardiography-Guided Ductus Arteriosus Treatment to Reduce Necrotizing Enterocolitis | Randomized Trial on Echocardiography-Guided Ductus Arteriosus Treatment to Reduce Necrotizing Enterocolitis Abstract Objective Patent ductus arteriosus (PDA) approach remains controversial. We aim to evaluate whether echocardiography-guided (EchoG) PDA closure (to reduce drug exposure) and 24-h continuous ibuprofen inf... |
PMC6359228 | core_pubmed_pmc | Chitosan-Coated Flexible Liposomes Magnify the Anticancer Activity and Bioavailability of Docetaxel: Impact on Composition | Chitosan-Coated Flexible Liposomes Magnify the Anticancer Activity and Bioavailability of Docetaxel: Impact on Composition Abstract Flexible liposomes (FLs) were developed as promising nano-carriers for anticancer drugs. Coating them with chitosan (CS) could improve their drug delivery properties. The aim of this study... |
PMC6499763 | core_pubmed_pmc | Pharmacokinetic and exploratory exposure–response analysis of pertuzumab in patients with operable HER2-positive early breast cancer in the APHINITY study | Pharmacokinetic and exploratory exposure–response analysis of pertuzumab in patients with operable HER2-positive early breast cancer in the APHINITY study Abstract Purpose To characterize the pharmacokinetics (PK) of, and perform an exploratory exposure–response (E–R) analysis for, pertuzumab in patients with HER2-posi... |
PMC5600351 | core_pubmed_pmc | N-acetyl-L-methionine is a superior protectant of human serum albumin against post-translational oxidation as compared to N-acetyl-L-tryptophan | N-acetyl-L-methionine is a superior protectant of human serum albumin against post-translational oxidation as compared to N-acetyl-L-tryptophan Abstract Sodium octanoate and N-acetyl-L-tryptophan (N-AcTrp) are widely used as stabilizers during pasteurization and storage of albumin products. However, as compared with N-... |
PMC12300973 | core_pubmed_pmc | Three-Compartment Pharmacokinetics of Inhaled and Injected Sinapine Thiocyanate Manifest Prolonged Retention and Its Therapeutics in Acute Lung Injury | Three-Compartment Pharmacokinetics of Inhaled and Injected Sinapine Thiocyanate Manifest Prolonged Retention and Its Therapeutics in Acute Lung Injury Abstract Abstract Background : Acute lung injury (ALI) is driven by inflammatory cascades and reactive oxygen species (ROS) generation, with the progression to severe ca... |
PMC5829157 | core_pubmed_pmc | Comparison of TPMT and NUDT15 polymorphisms in Chinese patients with inflammatory bowel disease | Comparison of TPMT and NUDT15 polymorphisms in Chinese patients with inflammatory bowel disease Abstract AIM To observe gene polymorphisms of TPMT and NUDT15 , and compare their predictive value for azathioprine (AZA)-induced leukopenia in inflammatory bowel disease (IBD). METHODS This study enrolled 219 patients diagn... |
PMC9836799 | core_pubmed_pmc | Marmesin and Marmelosin Interact with the Heparan Sulfatase-2 Active Site: Potential Mechanism for Phytochemicals from Bael Fruit Extract as Antitumor Therapeutics | Marmesin and Marmelosin Interact with the Heparan Sulfatase-2 Active Site: Potential Mechanism for Phytochemicals from Bael Fruit Extract as Antitumor Therapeutics Abstract Abstract Human heparan sulfatase-2 (HSULF-2) is an oncoprotein overexpressed in the surface of all types of tumor cells and its activity plays a cr... |
PMC10063958 | core_pubmed_pmc | In-vivo magnetic resonance spectroscopy of lactate as a non-invasive biomarker of dichloroacetate activity in cancer and non-cancer central nervous system disorders | In-vivo magnetic resonance spectroscopy of lactate as a non-invasive biomarker of dichloroacetate activity in cancer and non-cancer central nervous system disorders Abstract Abstract The adverse effects of lactic acidosis in the cancer microenvironment have been increasingly recognized. Dichloroacetate (DCA) is an oral... |
PMC11672368 | core_pubmed_pmc | Effectiveness, pharmacokinetics, and safety of triptorelin acetate microspheres in patients with locally advanced and metastatic prostate cancer | Effectiveness, pharmacokinetics, and safety of triptorelin acetate microspheres in patients with locally advanced and metastatic prostate cancer Abstract Abstract Background: A newly generic microspheres, sustained-release formulation of triptorelin acetate 3.75 mg has been developed. Objectives: To evaluate the effica... |
PMC3978529 | core_pubmed_pmc | Application of Pharmacokinetic and Pharmacodynamic Analysis to the Development of Liposomal Formulations for Oncology | Application of Pharmacokinetic and Pharmacodynamic Analysis to the Development of Liposomal Formulations for Oncology Abstract Liposomal formulations of anticancer agents have been developed to prolong drug circulating lifetime, enhance anti-tumor efficacy by increasing tumor drug deposition, and reduce drug toxicity b... |
PMC8426393 | core_pubmed_pmc | Interactions of anti-COVID-19 drug candidates with hepatic transporters may cause liver toxicity and affect pharmacokinetics | Interactions of anti-COVID-19 drug candidates with hepatic transporters may cause liver toxicity and affect pharmacokinetics Abstract Transporters in the human liver play a major role in the clearance of endo- and xenobiotics. Apical (canalicular) transporters extrude compounds to the bile, while basolateral hepatocyte... |
PMC4744679 | core_pubmed_pmc | Pharmacokinetics and tissue distribution of novel platinum containing anticancer agent BP‐C1 studied in rabbits using sector field inductively coupled plasma mass spectrometry | Pharmacokinetics and tissue distribution of novel platinum containing anticancer agent BP‐C1 studied in rabbits using sector field inductively coupled plasma mass spectrometry Abstract A method of platinum quantification in whole blood samples after microwave digestion using sector field inductively coupled plasma mass... |
PMC4061166 | core_pubmed_pmc | Enhanced and selective delivery of enzyme therapy to 9L-glioma tumor via magnetic targeting of PEG-modified, β-glucosidase-conjugated iron oxide nanoparticles | Enhanced and selective delivery of enzyme therapy to 9L-glioma tumor via magnetic targeting of PEG-modified, β-glucosidase-conjugated iron oxide nanoparticles Abstract The stability of enzyme-conjugated magnetic iron oxide nanoparticles in plasma is of great importance for in vivo delivery of the conjugated enzyme. In ... |
PMC3987181 | core_pubmed_pmc | A study of potential drug-drug interactions among hospitalized cardiac patients in a teaching hospital in Western Nepal | A study of potential drug-drug interactions among hospitalized cardiac patients in a teaching hospital in Western Nepal Abstract Abstract Aim: Drug-drug interaction (DDI) is of major concern in patients with complex therapeutic regimens. The involvement of cardiovascular medicines in drug interaction is even higher. Ho... |
PMC8969540 | core_pubmed_pmc | Delamanid or pretomanid? A Solomonic judgement! | Delamanid or pretomanid? A Solomonic judgement! Abstract Abstract Given the low treatment success rates of drug-resistant tuberculosis (TB), novel TB drugs are urgently needed. The landscape of TB treatment has changed considerably over the last decade with the approval of three new compounds: bedaquiline, delamanid an... |
PMC7932970 | core_pubmed_pmc | Pharmacodynamic and Pharmacokinetic Interaction Profile of Vericiguat: Results from Three Randomized Phase I Studies in Healthy Volunteers | Pharmacodynamic and Pharmacokinetic Interaction Profile of Vericiguat: Results from Three Randomized Phase I Studies in Healthy Volunteers Abstract Abstract Background Vericiguat, a direct stimulator of soluble guanylate cyclase, has been developed as a first-in-class therapy for symptomatic chronic heart failure (HF) ... |
PMC6337900 | core_pubmed_pmc | Ceftaroline fosamil doses and breakpoints for Staphylococcus aureus in complicated skin and soft tissue infections | Ceftaroline fosamil doses and breakpoints for Staphylococcus aureus in complicated skin and soft tissue infections Abstract Abstract Objectives To describe the pharmacokinetic/pharmacodynamic (PK/PD) modelling and microbiological data that were used to support the recent European approval of ceftaroline fosamil 600 mg ... |
PMC11702666 | core_pubmed_pmc | The anti-COVID-19 drug Paxlovid crosses biological barriers of the placenta and brain in rats | The anti-COVID-19 drug Paxlovid crosses biological barriers of the placenta and brain in rats Abstract Abstract Paxlovid (nirmatrelvir plus ritonavir) is an orally available drug for the treatment of COVID-19 disease. However, limited information remains on the biological barrier transfer of nirmatrelvir. In the presen... |
PMC10782143 | core_pubmed_pmc | Glucagon‐like peptide agonists: A prospective review | Glucagon‐like peptide agonists: A prospective review Abstract Abstract Background Glucagon‐like peptide‐1 receptor agonists (GLP‐1RAs) have emerged as promising therapeutic options for addressing Type‐2 diabetes, obesity, and related conditions. Among these, semaglutide, tirzepatide, liraglutide etc., all notable GLP‐1... |
PMC12915777 | core_pubmed_pmc | Gut bacterial O -demethylation modulates systemic exposure to oral etoposide | Gut bacterial O -demethylation modulates systemic exposure to oral etoposide Abstract ABSTRACT Gut microbial O -demethylation has been reported for plant-derived dietary compounds containing O -methylated aromatic(s). However, the significance of gut microbial O -demethylation in drug metabolism and disposition remains... |
PMC12773697 | core_pubmed_pmc | Expert perspectives on exposure-response functions for urban health policy: Lessons from a UBDPolicy workshop | Expert perspectives on exposure-response functions for urban health policy: Lessons from a UBDPolicy workshop Abstract Policy-makers require robust, quantitative evidence in order to better align urban and transport planning practices with public health goals. Epidemiologically derived exposure-response functions can q... |
PMC3335337 | core_pubmed_pmc | High-Performance Liquid Chromatography Assay for Moxifloxacin in Brain Tissue and Plasma: Validation in a Pharmacokinetic Study in a Murine Model of Cerebral Listeriosis | High-Performance Liquid Chromatography Assay for Moxifloxacin in Brain Tissue and Plasma: Validation in a Pharmacokinetic Study in a Murine Model of Cerebral Listeriosis Abstract Moxifloxacin is a broad-spectrum antibacterial 8-methoxy-fluoroquinolone. In order to evaluate the pharmacokinetic properties of moxifloxacin... |
PMC6060385 | core_pubmed_pmc | Intravenous delivery of a liposomal formulation of voriconazole improves drug pharmacokinetics, tissue distribution, and enhances antifungal activity | Intravenous delivery of a liposomal formulation of voriconazole improves drug pharmacokinetics, tissue distribution, and enhances antifungal activity Abstract Abstract Voriconazole (VCZ), a triazole with a large spectrum of action is one of the most recommended antifungal agents as the first line therapy against severa... |
PMC5854746 | core_pubmed_pmc | Monitoring of erlotinib in pancreatic cancer patients during long-time administration and comparison to a physiologically based pharmacokinetic model | Monitoring of erlotinib in pancreatic cancer patients during long-time administration and comparison to a physiologically based pharmacokinetic model Abstract Purpose In this study, a therapeutic drug monitoring (TDM) of erlotinib in pancreatic cancer patients was performed over 50 weeks to reveal possible alterations ... |
PMC8709966 | core_pubmed_pmc | Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda | Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda Abstract Background In Uganda, artemether-lumefantrine (AL) is first-li... |
PMC5848174 | core_pubmed_pmc | Pharmacokinetics of Snake Venom | Pharmacokinetics of Snake Venom Abstract Understanding snake venom pharmacokinetics is essential for developing risk assessment strategies and determining the optimal dose and timing of antivenom required to bind all venom in snakebite patients. This review aims to explore the current knowledge of snake venom pharmacok... |
PMC5323062 | core_pubmed_pmc | Bioavailability of a dexlansoprazole delayed-release orally disintegrating tablet: effects of food and mode of administration | Bioavailability of a dexlansoprazole delayed-release orally disintegrating tablet: effects of food and mode of administration Abstract Abstract Background Dexlansoprazole is a proton pump inhibitor (PPI) approved for use in dual delayed-release capsule and orally disintegrating tablet (ODT) formulations. Aim To assess ... |
PMC4406961 | core_pubmed_pmc | Emerging Insights for Translational Pharmacokinetic and Pharmacokinetic-Pharmacodynamic Studies: Towards Prediction of Nose-to-Brain Transport in Humans | Emerging Insights for Translational Pharmacokinetic and Pharmacokinetic-Pharmacodynamic Studies: Towards Prediction of Nose-to-Brain Transport in Humans Abstract To investigate the potential added value of intranasal drug administration, preclinical studies to date have typically used the area under the curve (AUC) in ... |
PMC12702135 | core_pubmed_pmc | No Effect of Immunogenicity on Pharmacokinetics, Efficacy, and Safety of the Oligonucleotide Telomerase Inhibitor Imetelstat in Lower‐Risk Myelodysplastic Syndromes | No Effect of Immunogenicity on Pharmacokinetics, Efficacy, and Safety of the Oligonucleotide Telomerase Inhibitor Imetelstat in Lower‐Risk Myelodysplastic Syndromes Abstract ABSTRACT Imetelstat is a first‐in‐class, 13‐mer oligonucleotide telomerase inhibitor approved in the United States and European Union for the trea... |
PMC10046592 | core_pubmed_pmc | Developmental Pharmacokinetics of Antibiotics Used in Neonatal ICU: Focus on Preterm Infants | Developmental Pharmacokinetics of Antibiotics Used in Neonatal ICU: Focus on Preterm Infants Abstract Neonatal Infections are among the most common reasons for admission to the intensive care unit. Neonatal sepsis (NS) significantly contributes to mortality rates. Empiric antibiotic therapy of NS recommended by current... |
PMC4725632 | core_pubmed_pmc | Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers | Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers Abstract Abstract Purpose To investigate the effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in humans. Methods Two independent, open-label, randomized, crossover studies were conducted ... |
PMC12015819 | core_pubmed_pmc | Effect of Acute Lung Injury (ALI) Induced by Lipopolysaccharide (LPS) on the Pulmonary Pharmacokinetics of an Antibody | Effect of Acute Lung Injury (ALI) Induced by Lipopolysaccharide (LPS) on the Pulmonary Pharmacokinetics of an Antibody Abstract Abstract Objective: To investigate the effect of Lipopolysaccharide (LPS)-induced acute lung injury (ALI) on the pulmonary pharmacokinetics (PK) of a systemically administered antibody in mice... |
PMC12736094 | core_pubmed_pmc | Validation of a UPLC-MS/MS Method for Quantifying Intracellular Olaparib Levels in Resistant Ovarian Cancer Cells | Validation of a UPLC-MS/MS Method for Quantifying Intracellular Olaparib Levels in Resistant Ovarian Cancer Cells Abstract Abstract Background: Ovarian cancer remains one of the leading causes of cancer-related mortality among women and constitutes a major unmet medical need. A common treatment-limiting factor for ovar... |
PMC3591361 | core_pubmed_pmc | Combined Delivery of Paclitaxel and Tanespimycin via Micellar Nanocarriers: Pharmacokinetics, Efficacy and Metabolomic Analysis | Combined Delivery of Paclitaxel and Tanespimycin via Micellar Nanocarriers: Pharmacokinetics, Efficacy and Metabolomic Analysis Abstract Abstract Background Despite the promising anticancer efficacy observed in preclinical studies, paclitaxel and tanespimycin (17-AAG) combination therapy has yielded meager responses in... |
PMC6952969 | core_pubmed_pmc | Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [ 18 F]FAZA PET In Vivo | Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [ 18 F]FAZA PET In Vivo Abstract Abstract Tumors lack a well-regulated vascular supply of O 2 and often fail to balance O 2 supply and demand. Net O 2 tension within many tumors may not only dep... |
PMC11858921 | core_pubmed_pmc | Targeting Plasmodium falciparum Schizont Egress Antigen-1 in Infected Red Blood Cells: Docking-Based Fingerprinting, Density Functional Theory, Molecular Dynamics Simulations, and Binding Free Energy Analysis | Targeting Plasmodium falciparum Schizont Egress Antigen-1 in Infected Red Blood Cells: Docking-Based Fingerprinting, Density Functional Theory, Molecular Dynamics Simulations, and Binding Free Energy Analysis Abstract Abstract Background: Malaria remains a global health crisis, with the World Health Organization (WHO) ... |
PMC9495958 | core_pubmed_pmc | Clinical Application of Pharmacokinetics to Appraise Adherence to Levetiracetam in Portuguese Epileptic Patients | Clinical Application of Pharmacokinetics to Appraise Adherence to Levetiracetam in Portuguese Epileptic Patients Abstract Adherence to antiseizure drug treatment determines its effectiveness and safety, and consequently affects patients’ quality of life. Herein, we assessed adherence to levetiracetam in Portuguese pati... |
PMC8341194 | core_pubmed_pmc | Ropeginterferon alfa‐2b in patients with genotype 1 chronic hepatitis C: Pharmacokinetics, safety, and preliminary efficacy | Ropeginterferon alfa‐2b in patients with genotype 1 chronic hepatitis C: Pharmacokinetics, safety, and preliminary efficacy Abstract ABSTRACT Background and Aim Ropeginterferon alfa‐2b (P1101) is a novel long‐acting mono‐PEGylated recombinant proline interferon (IFN) conjugated to a 40 kDa branched polyethylene glycol ... |
PMC6274500 | core_pubmed_pmc | LC-MS/MS Analysis and Pharmacokinetics of Sodium (±)-5-Bromo-2-(α-hydroxypentyl) Benzoate (BZP), an Innovative Potent Anti - Ischemic Stroke Agent in Rats | LC-MS/MS Analysis and Pharmacokinetics of Sodium (±)-5-Bromo-2-(α-hydroxypentyl) Benzoate (BZP), an Innovative Potent Anti - Ischemic Stroke Agent in Rats Abstract A rapid, sensitive and selective liquid chromatography-triple quadrupole mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneou... |
PMC7491210 | core_pubmed_pmc | Lithium toxicity following bariatric surgery | Lithium toxicity following bariatric surgery Abstract A patient with morbid obesity and several psychiatric comorbidities underwent laparoscopic sleeve gastrectomy and experienced success with weight loss. However, she experienced lightheadedness, nausea, and a fall and was admitted to the hospital for encephalopathy d... |
PMC7898666 | core_pubmed_pmc | Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity | Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity Abstract Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacologic... |
PMC9960864 | core_pubmed_pmc | Population Pharmacokinetics of Isavuconazole in Critical Care Patients with COVID-19-Associated Pulmonary Aspergillosis and Monte Carlo Simulations of High Off-Label Doses | Population Pharmacokinetics of Isavuconazole in Critical Care Patients with COVID-19-Associated Pulmonary Aspergillosis and Monte Carlo Simulations of High Off-Label Doses Abstract Isavuconazole is a triazole antifungal agent recently recommended as first-line therapy for invasive pulmonary aspergillosis. With the COVI... |
PMC12371661 | core_pubmed_pmc | The human photosensitive epilepsy model for clinical proof‐of‐principle trials of novel antiseizure medications: 2. Analysis of drug trials and predictive value of the model | The human photosensitive epilepsy model for clinical proof‐of‐principle trials of novel antiseizure medications: 2. Analysis of drug trials and predictive value of the model Abstract Abstract Clinical development of novel antiseizure medications (ASMs) would benefit from an early proof of principle (POP) model. The pho... |
PMC12394303 | core_pubmed_pmc | Assessing the Effect of Food on the Pharmacokinetics of Iclepertin in Healthy Volunteers: A Phase I, Open-Label, Randomised, Cross-over Trial | Assessing the Effect of Food on the Pharmacokinetics of Iclepertin in Healthy Volunteers: A Phase I, Open-Label, Randomised, Cross-over Trial Abstract Background and objectives Iclepertin, a selective glycine transporter-1 inhibitor, was investigated as a potential treatment for cognitive impairment associated with sch... |
PMC12135513 | core_pubmed_pmc | Individual target pharmacokinetic/pharmacodynamic attainment rates among cefepime-treated patients admitted to the ICU with hospital-acquired pneumonia with and without ECMO | Individual target pharmacokinetic/pharmacodynamic attainment rates among cefepime-treated patients admitted to the ICU with hospital-acquired pneumonia with and without ECMO Abstract ABSTRACT Cefepime (FEP) is used for hospital- and ventilator-associated pneumonia when Pseudomonas aeruginosa is involved. However, its p... |
PMC5656457 | core_pubmed_pmc | Optimal timing for the oral administration of Da-Cheng-Qi decoction based on the pharmacokinetic and pharmacodynamic targeting of the pancreas in rats with acute pancreatitis | Optimal timing for the oral administration of Da-Cheng-Qi decoction based on the pharmacokinetic and pharmacodynamic targeting of the pancreas in rats with acute pancreatitis Abstract AIM To identify the optimal oral dosing time of Da-Cheng-Qi decoction (DCQD) in rats with acute pancreatitis (AP) based on the pharmacok... |
PMC11830013 | core_pubmed_pmc | Joint analysis of time-varying effect of vaccine and antiviral drug for preventing severe complications and mortality | Joint analysis of time-varying effect of vaccine and antiviral drug for preventing severe complications and mortality Abstract This study investigated the time-varying effects of vaccines and oral antiviral drugs in preventing severe COVID-19 complications and mortality in Hong Kong. Utilizing data from hospitalized pa... |
PMC6731969 | core_pubmed_pmc | The safety, pharmacodynamics, and pharmacokinetics of immediate-release formulation containing esomeprazole 20 mg/sodium bicarbonate 800 mg in healthy adult male | The safety, pharmacodynamics, and pharmacokinetics of immediate-release formulation containing esomeprazole 20 mg/sodium bicarbonate 800 mg in healthy adult male Abstract Abstract Background Esomeprazole is the most effective treatment for acid-related disorders and is widely used with enteric coating due to rapid degr... |
PMC7036667 | core_pubmed_pmc | Comparison of Pharmacokinetics of a Fixed-Dose Combination of Amlodipine/Losartan/Rosuvastatin with Concomitant Administration of Amlodipine/Losartan and Rosuvastatin in Healthy Volunteers | Comparison of Pharmacokinetics of a Fixed-Dose Combination of Amlodipine/Losartan/Rosuvastatin with Concomitant Administration of Amlodipine/Losartan and Rosuvastatin in Healthy Volunteers Abstract Abstract Background A fixed-dose combination (FDC) tablet formulation of amlodipine/losartan/rosuvastatin 5/100/20 mg was ... |
PMC11578140 | core_pubmed_pmc | Investigation of a fully mechanistic physiologically based pharmacokinetics model of absorption to support predictions of milk concentrations in breastfeeding women and the exposure of infants: A case study for albendazole | Investigation of a fully mechanistic physiologically based pharmacokinetics model of absorption to support predictions of milk concentrations in breastfeeding women and the exposure of infants: A case study for albendazole Abstract Abstract Due to limited non‐clinical and clinical data, European guidance recommends to ... |
PMC7699441 | core_pubmed_pmc | Comparison of Bioavailability and Bioequivalence of Generic and Brand Name Formulations of Escitalopram Oxalate Tablets in Healthy Chinese Population Under Fasting and Fed Conditions | Comparison of Bioavailability and Bioequivalence of Generic and Brand Name Formulations of Escitalopram Oxalate Tablets in Healthy Chinese Population Under Fasting and Fed Conditions Abstract Abstract Purpose This study compared the bioequivalence of two formulations of escitalopram oxalate 20 mg tablets in terms of bi... |
PMC11784299 | core_pubmed_pmc | Population pharmacokinetic analyses for sulbactam–durlobactam using Phase 1, 2, and 3 data | Population pharmacokinetic analyses for sulbactam–durlobactam using Phase 1, 2, and 3 data Abstract ABSTRACT Sulbactam–durlobactam is a β-lactam/β-lactamase inhibitor combination approved in the United States for the treatment of hospital-acquired and ventilator-associated bacterial pneumonia caused by susceptible isol... |
PMC8534053 | core_pubmed_pmc | Semi-Mechanistic Model for the Antitumor Response of a Combination Cocktail of Immuno-Modulators in Non-Inflamed (Cold) Tumors | Semi-Mechanistic Model for the Antitumor Response of a Combination Cocktail of Immuno-Modulators in Non-Inflamed (Cold) Tumors Abstract Simple Summary The clinical efficacy of immunotherapies when treating cold tumors is still low, and different treatment combinations are needed when dealing with this challenging scena... |
PMC5977051 | core_pubmed_pmc | Delayed-Onset Seizure in a Mild Quetiapine Overdose: Report of a Case and Review of the Literature | Delayed-Onset Seizure in a Mild Quetiapine Overdose: Report of a Case and Review of the Literature Abstract Among atypical antipsychotics, quetiapine is commonly prescribed and considered to have a favorable side effect and safety profile. Here, we report the case of a patient who developed a generalized tonic-clonic s... |
PMC5332445 | core_pubmed_pmc | The relationship between pharmacokinetic parameters of carbamazepine and therapeutic response in epileptic patients | The relationship between pharmacokinetic parameters of carbamazepine and therapeutic response in epileptic patients Abstract Introduction The prescribed dose and carbamazepine plasma concentration to achieve the optimal therapeutic efficacy are highly variable from one patient to the other. Our study aimed to determine... |
PMC9785594 | core_pubmed_pmc | Silviridoside: A New Triterpene Glycoside from Silene viridiflora with Promising Antioxidant and Enzyme Inhibitory Potential | Silviridoside: A New Triterpene Glycoside from Silene viridiflora with Promising Antioxidant and Enzyme Inhibitory Potential Abstract A new triterpene glycoside, silviridoside, was isolated from the aerial parts of Silene viridiflora (Caryophyllaceae) using different chromatographic techniques. The structure of silviri... |
PMC10281847 | core_pubmed_pmc | Pilot study: bioequivalence of dihydroartemisinin in dihydroartemisinin-piperaquine tablet generic formulation in healthy Indonesian volunteers | Pilot study: bioequivalence of dihydroartemisinin in dihydroartemisinin-piperaquine tablet generic formulation in healthy Indonesian volunteers Abstract ABSTRACT Bioequivalence test should be carried out for copy medicine, including dihydroartemisinin-piperaquine (DHP), which is used to treat critical diseases requirin... |
PMC8277188 | core_pubmed_pmc | Quantitative Method for the Analysis of Ivacaftor, Hydroxymethyl Ivacaftor, Ivacaftor Carboxylate, Lumacaftor, and Tezacaftor in Plasma and Sputum Using Liquid Chromatography With Tandem Mass Spectrometry and Its Clinical Applicability | Quantitative Method for the Analysis of Ivacaftor, Hydroxymethyl Ivacaftor, Ivacaftor Carboxylate, Lumacaftor, and Tezacaftor in Plasma and Sputum Using Liquid Chromatography With Tandem Mass Spectrometry and Its Clinical Applicability Abstract Abstract Background: The novel cystic fibrosis transmembrane conductance re... |
PMC10987161 | core_pubmed_pmc | Multivalent Rhamnose‐Modified EGFR‐Targeting Nanobody Gains Enhanced Innate Fc Effector Immunity and Overcomes Cetuximab Resistance via Recruitment of Endogenous Antibodies | Multivalent Rhamnose‐Modified EGFR‐Targeting Nanobody Gains Enhanced Innate Fc Effector Immunity and Overcomes Cetuximab Resistance via Recruitment of Endogenous Antibodies Abstract Abstract Cetuximab resistance is a significant challenge in cancer treatment, requiring the development of novel therapeutic strategies. I... |
PMC7550288 | core_pubmed_pmc | Population pharmacokinetic approach for evaluation of treosulfan and its active monoepoxide disposition in plasma and brain on the basis of a rat model | Population pharmacokinetic approach for evaluation of treosulfan and its active monoepoxide disposition in plasma and brain on the basis of a rat model Abstract Purpose Efficacy of treosulfan, used in the treatment of marrow disorders, depends on the activity of its monoepoxy—(EBDM) and diepoxy compounds. The study aim... |
PMC8780964 | core_pubmed_pmc | Evaluation of the Pharmacokinetics of the Pancreastatin Inhibitor PSTi8 Peptide in Rats: Integration of In Vitro and In Vivo Findings | Evaluation of the Pharmacokinetics of the Pancreastatin Inhibitor PSTi8 Peptide in Rats: Integration of In Vitro and In Vivo Findings Abstract Abstract PSTi8 is a pancreastatin inhibitory peptide that is effective in the treatment of diabetic models. This study investigates the pharmacokinetic (PK) properties of PSTi8 ... |
PMC3358232 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of medication in asphyxiated newborns during controlled hypothermia. The PharmaCool multicenter study | Pharmacokinetics and pharmacodynamics of medication in asphyxiated newborns during controlled hypothermia. The PharmaCool multicenter study Abstract Background In the Netherlands, perinatal asphyxia (severe perinatal oxygen shortage) necessitating newborn resuscitation occurs in at least 200 of the 180–185.000 newly bo... |
PMC7812971 | core_pubmed_pmc | Delayed-Release Dimethyl Fumarate Safety and Efficacy in Pediatric Patients With Relapsing-Remitting Multiple Sclerosis | Delayed-Release Dimethyl Fumarate Safety and Efficacy in Pediatric Patients With Relapsing-Remitting Multiple Sclerosis Abstract Abstract Background: Pediatric multiple sclerosis (MS) is rare: only 1.5–5% of MS cases are diagnosed before 18 years of age, and data on disease-modifying therapies (DMTs) for pediatric MS a... |
PMC12568872 | core_pubmed_pmc | Reduced-Dose Edoxaban in Patients Aged ≥ 80 Years: A Single-Center Real-World Analysis | Reduced-Dose Edoxaban in Patients Aged ≥ 80 Years: A Single-Center Real-World Analysis Abstract Abstract Background Optimal anticoagulation strategies in octogenarians remain controversial owing to age-related risks of thromboembolism and bleeding. This study evaluates real-world outcomes of reduced-dose edoxaban (15–3... |
PMC6160999 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution and Excretion of a Novel Diuretic (PU-48) in Rats | Pharmacokinetics, Tissue Distribution and Excretion of a Novel Diuretic (PU-48) in Rats Abstract Abstract Methyl 3-amino-6-methoxythieno [2,3-b] quinoline-2-carboxylate (PU-48) is a novel diuretic urea transporter inhibitor. The aim of this study is to investigate the profile of plasma pharmacokinetics, tissue distribu... |
PMC5073218 | core_pubmed_pmc | Pharmacodynamics and Pharmacokinetics Following Once-Daily and Twice-Daily Dosing of Tiotropium Respimat ® in Asthma Using Standardized Sample-Contamination Avoidance | Pharmacodynamics and Pharmacokinetics Following Once-Daily and Twice-Daily Dosing of Tiotropium Respimat ® in Asthma Using Standardized Sample-Contamination Avoidance Abstract Abstract Background: This study was conducted to confirm the 24-hour bronchodilator efficacy and pharmacokinetic profile of once-daily tiotropiu... |
PMC12277834 | core_pubmed_pmc | Efficacy and safety of bevacizumab biosimilar SIBP04 compared with bevacizumab (Avastin®) as first-line treatment for locally advanced or metastatic non-squamous non-small-cell lung cancer: A randomized, double-blind, phase 3 trial ☆ | Efficacy and safety of bevacizumab biosimilar SIBP04 compared with bevacizumab (Avastin®) as first-line treatment for locally advanced or metastatic non-squamous non-small-cell lung cancer: A randomized, double-blind, phase 3 trial ☆ Abstract Abstract Background SIBP04 is a biosimilar of bevacizumab (Avastin®, Roche, B... |
PMC7032110 | core_pubmed_pmc | Influence of pretreatment of piperazine ferulate on pharmacokinetic parameters of methotrexate in methotrexate-induced renal injury model rats by HPLC-MS | Influence of pretreatment of piperazine ferulate on pharmacokinetic parameters of methotrexate in methotrexate-induced renal injury model rats by HPLC-MS Abstract Abstract The present study was designed to investigate the influence of the pretreatment of piperazine ferulate on pharmacokinetic parameters of methotrexate... |
PMC8529163 | core_pubmed_pmc | Synthesis, Computational Pharmacokinetics Report, Conceptual DFT-Based Calculations and Anti-Acetylcholinesterase Activity of Hydroxyapatite Nanoparticles Derived From Acorus Calamus Plant Extract | Synthesis, Computational Pharmacokinetics Report, Conceptual DFT-Based Calculations and Anti-Acetylcholinesterase Activity of Hydroxyapatite Nanoparticles Derived From Acorus Calamus Plant Extract Abstract Over the years, Alzheimer’s disease (AD) treatments have been a major focus, culminating in the identification of ... |
PMC8316023 | core_pubmed_pmc | A Phase I Evaluation of the Pharmacokinetics and Tolerability of the HIV-1 Maturation Inhibitor GSK3640254 and Tenofovir Alafenamide/Emtricitabine in Healthy Participants | A Phase I Evaluation of the Pharmacokinetics and Tolerability of the HIV-1 Maturation Inhibitor GSK3640254 and Tenofovir Alafenamide/Emtricitabine in Healthy Participants Abstract ABSTRACT GSK3640254 is a next-generation maturation inhibitor that would likely be combined with standard antiretroviral agents to form a re... |
PMC10448036 | core_pubmed_pmc | Therapeutic advantages of the combined use of closantel and moxidectin in lambs parasitized with resistant gastrointestinal nematodes | Therapeutic advantages of the combined use of closantel and moxidectin in lambs parasitized with resistant gastrointestinal nematodes Abstract The serious widespread development of nematode resistance has motivated the use of combined anthelmintic formulations. However, the advantages/disadvantages of the combined use ... |
PMC12073177 | core_pubmed_pmc | Synthesis and Biological Evaluation of Novel Ramalin Derivatives as Multi-Target Agents for Alzheimer’s Disease | Synthesis and Biological Evaluation of Novel Ramalin Derivatives as Multi-Target Agents for Alzheimer’s Disease Abstract Alzheimer’s disease (AD) is a complex neurodegenerative disorder characterized by cognitive decline, oxidative stress, neuroinflammation, amyloid-beta (Aβ) accumulation, and tau protein hyperphosphor... |
PMC7070818 | core_pubmed_pmc | Itraconazole Increases Ibrutinib Exposure 10‐Fold and Reduces Interindividual Variation—A Potentially Beneficial Drug‐Drug Interaction | Itraconazole Increases Ibrutinib Exposure 10‐Fold and Reduces Interindividual Variation—A Potentially Beneficial Drug‐Drug Interaction Abstract The oral bioavailability of ibrutinib is low and variable, mainly due to extensive first‐pass metabolism by cytochrome P450 (CYP) 3A4. The unpredictable exposure can compromise... |
PMC10365885 | core_pubmed_pmc | Modulation of Extravascular Binding of Recombinant Factor IX Impacts the Duration of Efficacy in Mouse Models | Modulation of Extravascular Binding of Recombinant Factor IX Impacts the Duration of Efficacy in Mouse Models Abstract Abstract Background There is an emerging concept that in addition to circulating coagulation factor IX (FIX), extravascular FIX contributes to hemostasis. Objective Our objective was to evaluate the ef... |
PMC7808764 | core_pubmed_pmc | Application of physiologically based pharmacokinetic modeling to predict the pharmacokinetics of telavancin in obesity with renal impairment | Application of physiologically based pharmacokinetic modeling to predict the pharmacokinetics of telavancin in obesity with renal impairment Abstract Abstract Purpose U.S. Food and Drug Administration (FDA) recommended telavancin dosing is based on total body weight (TBW) but lacks adjusted regimens for obese subjects ... |
PMC5923120 | core_pubmed_pmc | Acylhydrazones as Antifungal Agents Targeting the Synthesis of Fungal Sphingolipids | Acylhydrazones as Antifungal Agents Targeting the Synthesis of Fungal Sphingolipids Abstract ABSTRACT The incidence of invasive fungal infections has risen dramatically in recent decades. Current antifungal drugs are either toxic, likely to interact with other drugs, have a narrow spectrum of activity, or induce fungal... |
PMC8932751 | core_pubmed_pmc | Atorvastatin population pharmacokinetics in a real‐life setting: Influence of genetic polymorphisms and association with clinical response | Atorvastatin population pharmacokinetics in a real‐life setting: Influence of genetic polymorphisms and association with clinical response Abstract Abstract The purpose of this study was to investigate the potential clinical relevance of estimating the apparent clearance (CL/F) of atorvastatin through population pharma... |
PMC8212743 | core_pubmed_pmc | Hybrid physiologically‐based pharmacokinetic model for remdesivir: Application to SARS‐CoV‐2 | Hybrid physiologically‐based pharmacokinetic model for remdesivir: Application to SARS‐CoV‐2 Abstract Abstract A novel coronavirus, severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) or coronavirus disease 2019 (COVID‐19), has caused a pandemic that continues to cause catastrophic health and economic carnage ... |
PMC11356797 | core_pubmed_pmc | Nebivolol Polymeric Nanoparticles-Loaded In Situ Gel for Effective Treatment of Glaucoma: Optimization, Physicochemical Characterization, and Pharmacokinetic and Pharmacodynamic Evaluation | Nebivolol Polymeric Nanoparticles-Loaded In Situ Gel for Effective Treatment of Glaucoma: Optimization, Physicochemical Characterization, and Pharmacokinetic and Pharmacodynamic Evaluation Abstract Abstract Nebivolol hydrochloride (NEB), a 3rd-generation beta-blocker, was recently explored in managing open-angle glauco... |
PMC11447725 | core_pubmed_pmc | Comparative Pharmacokinetics and Tissue Distribution of Hexahydrocurcumin Following Intraperitoneal vs Oral Administration in Mice Using LC-MS/MS | Comparative Pharmacokinetics and Tissue Distribution of Hexahydrocurcumin Following Intraperitoneal vs Oral Administration in Mice Using LC-MS/MS Abstract A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to determine hexahydrocurcumin (HHC) levels in mouse plasma, brain, li... |
PMC12153937 | core_pubmed_pmc | Pharmacokinetics and Safety of Oxycodone/Naloxone Prolonged-Release Tablets in Chinese Patients with Chronic Pain | Pharmacokinetics and Safety of Oxycodone/Naloxone Prolonged-Release Tablets in Chinese Patients with Chronic Pain Abstract Purpose The study aimed to assess pharmacokinetics and safety of two oxycodone/naloxone prolonged-release tablet formulations in the Chinese population. Methods The study was conducted in 36 Chines... |
PMC3507764 | core_pubmed_pmc | Pharmacokinetic and -dynamic modelling of G-CSF derivatives in humans | Pharmacokinetic and -dynamic modelling of G-CSF derivatives in humans Abstract Background The human granulocyte colony-stimulating factor (G-CSF) is routinely applied to support recovery of granulopoiesis during the course of cytotoxic chemotherapies. However, optimal use of the drug is largely unknown. We showed in th... |
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