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PMC6976987 | core_pubmed_pmc | Effects of paroxetine, ketoconazole, and rifampin on the metabolism of eliglustat, an oral substrate reduction therapy for Gaucher disease type 1 | Effects of paroxetine, ketoconazole, and rifampin on the metabolism of eliglustat, an oral substrate reduction therapy for Gaucher disease type 1 Abstract Eliglustat is an oral glucosylceramide synthase inhibitor indicated for the long-term treatment of adults with Gaucher disease type 1 and CYP2D6 extensive, intermedi... |
PMC8637893 | core_pubmed_pmc | Influence of Inflammation on Cytochromes P450 Activity in Adults: A Systematic Review of the Literature | Influence of Inflammation on Cytochromes P450 Activity in Adults: A Systematic Review of the Literature Abstract Abstract Background: Available in-vitro and animal studies indicate that inflammation impacts cytochromes P450 (CYP) activity via multiple and complex transcriptional and post-transcriptional mechanisms, dep... |
PMC12823826 | core_pubmed_pmc | Pharmacological characterization and preclinical evaluation of 11h: a novel, brain-penetrant PDE4 inhibitor for neurological disorders | Pharmacological characterization and preclinical evaluation of 11h: a novel, brain-penetrant PDE4 inhibitor for neurological disorders Abstract Background Phosphodiesterase 4 (PDE4) inhibitors hold promise for treating neuroinflammatory and neurodegenerative disorders, but their clinical application in central nervous ... |
PMC11350865 | core_pubmed_pmc | Isavuconazole Pharmacokinetics in Critically Ill Patients: Relationship with Clinical Effectiveness and Patient Safety | Isavuconazole Pharmacokinetics in Critically Ill Patients: Relationship with Clinical Effectiveness and Patient Safety Abstract Abstract Isavuconazole is used to treat fungal infections. This study aims to describe isavuconazole pharmacokinetics in critically ill patients and evaluate their relationship with clinical e... |
PMC11246651 | core_pubmed_pmc | Pharmacokinetics and Safety of Estradiol Valerate Tablet and Its Generic: A Phase 1 Bioequivalence Study in Healthy Chinese Postmenopausal Female Subjects | Pharmacokinetics and Safety of Estradiol Valerate Tablet and Its Generic: A Phase 1 Bioequivalence Study in Healthy Chinese Postmenopausal Female Subjects Abstract Abstract Purpose Estradiol valerate (Progynova ® ) is used as hormone therapy to supplement estrogen deficiency. This study aimed to assess the bioequivalen... |
PMC4600921 | core_pubmed_pmc | A probabilistic model of human variability in physiology for future application to dose reconstruction and QIVIVE | A probabilistic model of human variability in physiology for future application to dose reconstruction and QIVIVE Abstract Abstract The risk assessment of environmental chemicals and drugs is undergoing a paradigm shift in approach which seeks the full replacement of animal testing with high throughput, mechanistic, in... |
PMC9840612 | core_pubmed_pmc | Effect of date molasses on levetiracetam pharmacokinetics in healthy rats | Effect of date molasses on levetiracetam pharmacokinetics in healthy rats Abstract Abstract Twelve healthy eight-week-old male Wistar rats weighing 200 g were used. Rats were chosen randomly, and their tails were identified and separated into cages/groups. The first group received an oral dose of 11.5 mg of levetiracet... |
PMC8400702 | core_pubmed_pmc | Mathematical Modeling of Remdesivir to Treat COVID-19: Can Dosing Be Optimized? | Mathematical Modeling of Remdesivir to Treat COVID-19: Can Dosing Be Optimized? Abstract Abstract The antiviral remdesivir has been approved by regulatory bodies such as the European Medicines Agency (EMA) and the US Food and Drug administration (FDA) for the treatment of COVID-19. However, its efficacy is debated and ... |
PMC9651907 | core_pubmed_pmc | Feasibility of a Pragmatic PBPK Modeling Approach: Towards Model-Informed Dosing in Pediatric Clinical Care | Feasibility of a Pragmatic PBPK Modeling Approach: Towards Model-Informed Dosing in Pediatric Clinical Care Abstract Abstract Background and Objective More than half of all drugs are still prescribed off-label to children. Pharmacokinetic (PK) data are needed to support off-label dosing, however for many drugs such dat... |
PMC9747124 | core_pubmed_pmc | Determination of a clinically effective evobrutinib dose: Exposure–response analyses of a phase II relapsing multiple sclerosis study | Determination of a clinically effective evobrutinib dose: Exposure–response analyses of a phase II relapsing multiple sclerosis study Abstract Abstract The pharmacometric analysis of the double‐blind, randomized, phase II study ( NCT02975349 ) investigating the safety and efficacy of evobrutinib, explored exposure–resp... |
PMC9284555 | core_pubmed_pmc | 4″-Sulfation Is the Major Metabolic Pathway of Epigallocatechin-3-gallate in Humans: Characterization of Metabolites, Enzymatic Analysis, and Pharmacokinetic Profiling | 4″-Sulfation Is the Major Metabolic Pathway of Epigallocatechin-3-gallate in Humans: Characterization of Metabolites, Enzymatic Analysis, and Pharmacokinetic Profiling Abstract Abstract Epigallocatechin-3-gallate (EGCG), a major green tea polyphenol, has beneficial effects on human health. This study aimed to elucidate... |
PMC6959988 | core_pubmed_pmc | Duodenum Intestine-Chip for preclinical drug assessment in a human relevant model | Duodenum Intestine-Chip for preclinical drug assessment in a human relevant model Abstract Abstract Induction of intestinal drug metabolizing enzymes can complicate the development of new drugs, owing to the potential to cause drug-drug interactions (DDIs) leading to changes in pharmacokinetics, safety and efficacy. Th... |
PMC3376947 | core_pubmed_pmc | Reconstruction of Exposure to m -Xylene from Human Biomonitoring Data Using PBPK Modelling, Bayesian Inference, and Markov Chain Monte Carlo Simulation | Reconstruction of Exposure to m -Xylene from Human Biomonitoring Data Using PBPK Modelling, Bayesian Inference, and Markov Chain Monte Carlo Simulation Abstract Abstract There are numerous biomonitoring programs, both recent and ongoing, to evaluate environmental exposure of humans to chemicals. Due to the lack of expo... |
PMC11227190 | core_pubmed_pmc | Interaction mechanism of oseltamivir phosphate with bovine serum albumin: multispectroscopic and molecular docking study | Interaction mechanism of oseltamivir phosphate with bovine serum albumin: multispectroscopic and molecular docking study Abstract Abstract Oseltamivir phosphate (OP) is an antiviral drug with potential risks to human health due to overuse, leading to serious consequences such as gastrointestinal disturbances, abnormal ... |
PMC3815009 | core_pubmed_pmc | Long-acting injectable antiretrovirals for HIV treatment and prevention | Long-acting injectable antiretrovirals for HIV treatment and prevention Abstract Purpose of review Long-acting antiretroviral (ARV) drugs may improve adherence to therapy and extend opportunities for therapeutic or prophylactic intervention to underserved patient populations. This review focuses on recent advances in t... |
PMC6972979 | core_pubmed_pmc | Patisiran Pharmacokinetics, Pharmacodynamics, and Exposure‐Response Analyses in the Phase 3 APOLLO Trial in Patients With Hereditary Transthyretin‐Mediated (hATTR) Amyloidosis | Patisiran Pharmacokinetics, Pharmacodynamics, and Exposure‐Response Analyses in the Phase 3 APOLLO Trial in Patients With Hereditary Transthyretin‐Mediated (hATTR) Amyloidosis Abstract Abstract Hereditary transthyretin‐mediated (hATTR) amyloidosis is an inherited, rapidly progressive, life‐threatening disease caused by... |
PMC8488224 | core_pubmed_pmc | Mechanistic Modeling of Maternal Lymphoid and Fetal Plasma Antiretroviral Exposure During the Third Trimester | Mechanistic Modeling of Maternal Lymphoid and Fetal Plasma Antiretroviral Exposure During the Third Trimester Abstract Abstract Pregnancy-induced changes in plasma pharmacokinetics of many antiretrovirals (ARV) are well-established. Current knowledge about the extent of ARV exposure in lymphoid tissues of pregnant wome... |
PMC8597021 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling to Support the Clinical Management of Drug–Drug Interactions With Bictegravir | Physiologically‐Based Pharmacokinetic Modeling to Support the Clinical Management of Drug–Drug Interactions With Bictegravir Abstract Bictegravir is equally metabolized by cytochrome P450 (CYP)3A and uridine diphosphate‐glucuronosyltransferase (UGT)1A1. Drug–drug interaction (DDI) studies were only conducted for strong... |
PMC6274275 | core_pubmed_pmc | LC-MS/MS Validation Analysis of Trastuzumab Using dSIL Approach for Evaluating Pharmacokinetics | LC-MS/MS Validation Analysis of Trastuzumab Using dSIL Approach for Evaluating Pharmacokinetics Abstract Quantitative targeted proteomics based approaches deploy state-of-the-art Liquid chromatography tandem mass spectrometry LC-MS technologies and are evolving as a complementary technique to standard ligand-binding ba... |
PMC5466683 | core_pubmed_pmc | Development and Evaluation of 18 F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC | Development and Evaluation of 18 F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC Abstract Abstract To prepare and evaluate a new radiotracer 18 F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo . Uptake and efflux of 18 F-IRS were performed with four NSCLC cell lines including HCC827, H1975, ... |
PMC12844744 | core_pubmed_pmc | Complexed Linalool with Beta-Cyclodextrin Improve Antihypertensive Activity: Pharmacokinetic and Pharmacodynamic Insights | Complexed Linalool with Beta-Cyclodextrin Improve Antihypertensive Activity: Pharmacokinetic and Pharmacodynamic Insights Abstract Abstract Background: Arterial hypertension (AH) remains a global health concern due to its multifactorial etiology, limited therapeutic success, and high cardiovascular risk. In this contex... |
PMC8420671 | core_pubmed_pmc | Phase 1 open-label trial of intravenous administration of MVA-BN-brachyury-TRICOM vaccine in patients with advanced cancer | Phase 1 open-label trial of intravenous administration of MVA-BN-brachyury-TRICOM vaccine in patients with advanced cancer Abstract Abstract Background MVA-BN-brachyury-TRICOM is a recombinant vector-based therapeutic cancer vaccine designed to induce an immune response against brachyury. Brachyury, a transcription fac... |
PMC4802034 | core_pubmed_pmc | Effects of Jia-Wei-Xiao-Yao-San on the Peripheral and Lymphatic Pharmacokinetics of Paclitaxel in Rats | Effects of Jia-Wei-Xiao-Yao-San on the Peripheral and Lymphatic Pharmacokinetics of Paclitaxel in Rats Abstract Paclitaxel is effective against breast cancer. The herbal medicine, Jia-Wei-Xiao-Yao-San (JWXYS), is the most frequent prescription used to relieve the symptoms of breast cancer treatments. The aim of the stu... |
PMC8190279 | core_pubmed_pmc | Spatiotemporal imaging and pharmacokinetics of fluorescent compounds in zebrafish eleuthero-embryos after different routes of administration | Spatiotemporal imaging and pharmacokinetics of fluorescent compounds in zebrafish eleuthero-embryos after different routes of administration Abstract Abstract Zebrafish ( Danio rerio ) is increasingly used to assess the pharmacological activity and toxicity of compounds. The spatiotemporal distribution of seven fluores... |
PMC4901840 | core_pubmed_pmc | Determination of Liposomal Cisplatin by High-Performance Liquid Chromatography and Its Application in Pharmacokinetic Studies | Determination of Liposomal Cisplatin by High-Performance Liquid Chromatography and Its Application in Pharmacokinetic Studies Abstract Abstract Liposomes have been employed as carriers for antineoplastic drugs to improve delivery. We describe an HPLC–UV method for determining cisplatin levels in liposomal and biologica... |
PMC10972884 | core_pubmed_pmc | Model-based exploration of the rationality of off-label use of cetirizine in Chinese pediatric patients: a prospective cohort study | Model-based exploration of the rationality of off-label use of cetirizine in Chinese pediatric patients: a prospective cohort study Abstract Aims: Cetirizine is frequently administered at an increased dosage in clinical practice and recommended by several guidelines. Nonetheless, the pharmacokinetic (PK) profile and re... |
PMC5020452 | core_pubmed_pmc | Pathway-specific inhibition of primaquine metabolism by chloroquine/quinine | Pathway-specific inhibition of primaquine metabolism by chloroquine/quinine Abstract Abstract Background There has been some evidence to suggest that the addition of chloroquine (CQ) or quinine (QN) to 8-aminoquinoline (8-AQ) treatment regimens may increase the therapeutic efficacy of the 8-AQ and simultaneously mitiga... |
PMC8452709 | core_pubmed_pmc | Effects of apolipoprotein E isoform, sex, and diet on insulin BBB pharmacokinetics in mice | Effects of apolipoprotein E isoform, sex, and diet on insulin BBB pharmacokinetics in mice Abstract Abstract Age, apolipoprotein E (apoE) isoform, sex, and diet can independently affect the risk for the development of Alzheimer’s disease (AD). Additionally, synergy between some of these risk factors have been observed.... |
PMC12890909 | core_pubmed_pmc | The future of mathematical oncology in the age of AI | The future of mathematical oncology in the age of AI Abstract Abstract This perspective article discusses emerging advances at the interface of mechanistic modeling and data-driven machine learning, highlighting opportunities for AI to accelerate discovery, improve predictive modeling, and enhance clinical decision-mak... |
PMC10470189 | core_pubmed_pmc | Engineered clinical-grade mesenchymal stromal cells combating SARS-CoV-2 omicron variants by secreting effective neutralizing antibodies | Engineered clinical-grade mesenchymal stromal cells combating SARS-CoV-2 omicron variants by secreting effective neutralizing antibodies Abstract Background The emergence of SARS-CoV-2 becomes life-threatening for the older and immunocompromised individuals, whereas limited treatment is available on these populations. ... |
PMC9300975 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Target Attainment of Vancomycin, at Three Reported Infusion Modes, for Methicillin-Resistant Staphylococcus aureus (MRSA) Bloodstream Infections in Critically Ill Patients: Focus on Novel Infusion Mode | Pharmacokinetic/Pharmacodynamic Target Attainment of Vancomycin, at Three Reported Infusion Modes, for Methicillin-Resistant Staphylococcus aureus (MRSA) Bloodstream Infections in Critically Ill Patients: Focus on Novel Infusion Mode Abstract Abstract Objective The study aimed to evaluate and compare the pharmacokineti... |
PMC9355221 | core_pubmed_pmc | Tolerability and pharmacokinetic evaluation of inhaled dry powder hydroxychloroquine in healthy volunteers | Tolerability and pharmacokinetic evaluation of inhaled dry powder hydroxychloroquine in healthy volunteers Abstract Abstract Rationale Inhaled antimicrobials enable high local concentrations where needed and, compared to orally administration, greatly reduce the potential for systemic side effects. In SARS-CoV-2 infect... |
PMC7468310 | core_pubmed_pmc | Rebalancing of the gut flora and microbial metabolism is responsible for the anti-arthritis effect of kaempferol | Rebalancing of the gut flora and microbial metabolism is responsible for the anti-arthritis effect of kaempferol Abstract Kaempferol is a natural flavonol that possesses various pharmacological activities, including anti-arthritis effects, yet the underlying mechanisms remain controversial. To evaluate the anti-arthrit... |
PMC8431646 | core_pubmed_pmc | Efficient Attenuation of Dextran Sulfate Sodium-Induced Colitis by Oral Administration of 5,6-Dihydroxy-8Z,11Z,14Z,17Z-eicosatetraenoic Acid in Mice | Efficient Attenuation of Dextran Sulfate Sodium-Induced Colitis by Oral Administration of 5,6-Dihydroxy-8Z,11Z,14Z,17Z-eicosatetraenoic Acid in Mice Abstract Abstract 5,6-dihydroxy-8Z,11Z,14Z,17Z-eicosatetraenoic acid (5,6-DiHETE) is an eicosapentaenoic acid-derived newly discovered bioactive anti-inflammatory lipid me... |
PMC7924256 | core_pubmed_pmc | Engineering Exosome-Like Nanovesicles Derived from Asparagus cochinchinensis Can Inhibit the Proliferation of Hepatocellular Carcinoma Cells with Better Safety Profile | Engineering Exosome-Like Nanovesicles Derived from Asparagus cochinchinensis Can Inhibit the Proliferation of Hepatocellular Carcinoma Cells with Better Safety Profile Abstract Background Exosomes are a type of membrane vesicles secreted by living cells. Recent studies suggest exosome-like nanovesicles (ELNVs) from fru... |
PMC12304827 | core_pubmed_pmc | Drug–drug interaction profile of ritlecitinib as perpetrator and victim through cytochrome P450 | Drug–drug interaction profile of ritlecitinib as perpetrator and victim through cytochrome P450 Abstract Abstract Aims To assess the effect of a potent cytochrome P450 (CYP) 3A inhibitor and CYP inducer on the pharmacokinetics of ritlecitinib, a JAK3/TEC family kinase inhibitor, and assess the effect of ritlecitinib on... |
PMC12140393 | core_pubmed_pmc | KIFC1 inhibition: Exploring the potential of propolis-derived small molecules for targeting cancer progression through in silico analysis | KIFC1 inhibition: Exploring the potential of propolis-derived small molecules for targeting cancer progression through in silico analysis Abstract Abstract Propolis, a resinous compound produced by bees, possesses diverse medicinal properties and has gained significant attention for its potential in cancer therapy. Thi... |
PMC8891203 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Roxadustat | Clinical Pharmacokinetics and Pharmacodynamics of Roxadustat Abstract The pharmacokinetics of roxadustat are well characterized, with an apparent volume of distribution after oral administration of 22–57 L, apparent clearance of 1.2–2.65 L/h, and renal clearance of 0.030–0.026 L/h in healthy volunteers; the elimination... |
PMC5970165 | core_pubmed_pmc | Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice | Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice Abstract Abstract PMX53 and PMX205 are cyclic hexapeptide inhibitors of complement C5a receptors (C5aR1), that are widely used to study C5aR1 pathobiology in mouse models of disease... |
PMC10175034 | core_pubmed_pmc | Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS / MS | Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS / MS Abstract Abstract Background As a pan‐HER tyrosine kinase inhibitor with a promising application prospect, poziotinib is likely to be coadministered with Schisandrins in clinical treatment due to its anticancer a... |
PMC12423258 | core_pubmed_pmc | Strategies for Switching between Oral Postsynaptic Antidopaminergic Antipsychotics in Patients with Schizophrenia: A Systematic Review | Strategies for Switching between Oral Postsynaptic Antidopaminergic Antipsychotics in Patients with Schizophrenia: A Systematic Review Abstract Abstract Background Antipsychotic switching is common in the treatment of schizophrenia. Pharmacokinetic and pharmacodynamic properties of antipsychotics can inform switch stra... |
PMC6851786 | core_pubmed_pmc | Drug‐Drug Interaction Study to Assess the Effect of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of the Novel Cereblon Modulator Avadomide (CC‐122) in Healthy Adult Subjects | Drug‐Drug Interaction Study to Assess the Effect of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of the Novel Cereblon Modulator Avadomide (CC‐122) in Healthy Adult Subjects Abstract Abstract Avadomide (CC‐122) is a novel immunomodulatory drug that binds to cereblon, a member of the Cullin 4‐RING E3... |
PMC5496203 | core_pubmed_pmc | Therapeutic miRNA and siRNA: Moving from Bench to Clinic as Next Generation Medicine | Therapeutic miRNA and siRNA: Moving from Bench to Clinic as Next Generation Medicine Abstract In the past few years, therapeutic microRNA (miRNA) and small interfering RNA (siRNA) are some of the most important biopharmaceuticals that are in commercial space as future medicines. This review summarizes the patents of mi... |
PMC8522729 | core_pubmed_pmc | Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 Inhibitors TBA-7371, PBTZ169, and OPC-167832 | Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 Inhibitors TBA-7371, PBTZ169, and OPC-167832 Abstract ABSTRACT Multiple drug discovery initiatives for tuberculosis are currently ongoing to identify and develop new potent drugs with novel targets in order to shorten treatment... |
PMC7067402 | core_pubmed_pmc | Effects of intestinal flora on the pharmacokinetics and pharmacodynamics of aspirin in high-altitude hypoxia | Effects of intestinal flora on the pharmacokinetics and pharmacodynamics of aspirin in high-altitude hypoxia Abstract Since hypobaric hypoxia significantly affects metabolic characteristics of intestinal flora, which plays an important role in the biotransformation of aspirin, high altitudes may influence the pharmacok... |
PMC8767159 | core_pubmed_pmc | Multiparameter Optimization of Trypanocidal Cruzain Inhibitors With In Vivo Activity and Favorable Pharmacokinetics | Multiparameter Optimization of Trypanocidal Cruzain Inhibitors With In Vivo Activity and Favorable Pharmacokinetics Abstract Cruzain, the main cysteine protease of Trypanosoma cruzi , plays key roles in all stages of the parasite’s life cycle, including nutrition acquisition, differentiation, evasion of the host immune... |
PMC10890982 | core_pubmed_pmc | Inhibition of Receptor-Interacting Protein Kinase 1 in Chronic Plaque Psoriasis: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study | Inhibition of Receptor-Interacting Protein Kinase 1 in Chronic Plaque Psoriasis: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Abstract Introduction Receptor-interacting protein kinase 1 (RIPK1), a key mediator of inflammation through necroptosis and proinflammatory cytokine production, may play a r... |
PMC5124029 | core_pubmed_pmc | A short review of drug–food interactions of medicines treating overactive bladder syndrome | A short review of drug–food interactions of medicines treating overactive bladder syndrome Abstract Background Overactive bladder syndrome is a condition where one or more of the symptoms such as pollakiuria, urgent need to urinate, nocturia and urinary incontinence is observed. Its prevalence ranges between 7 and 27 %... |
PMC12659662 | core_pubmed_pmc | Efficacy and Blood Concentrations of Cetuximab in a Hemodialysis Patient with Tongue Squamous Cell Carcinoma: A Case Report | Efficacy and Blood Concentrations of Cetuximab in a Hemodialysis Patient with Tongue Squamous Cell Carcinoma: A Case Report Abstract Abstract Introduction Cetuximab is an effective therapy for unresectable locoregionally advanced head and neck cancer, but for patients with end-stage renal disease (ESRD), clinical trial... |
PMC10384145 | core_pubmed_pmc | Anti- Leishmania amazonensis Activity, Cytotoxic Features, and Chemical Profile of Allium sativum (Garlic) Essential Oil | Anti- Leishmania amazonensis Activity, Cytotoxic Features, and Chemical Profile of Allium sativum (Garlic) Essential Oil Abstract Abstract Human tegumentary leishmaniasis (HTL) is a serious tropical disease caused by Leishmania amazonensis . Developing new leishmanicidal agents can help overcome current treatment chall... |
PMC9924185 | core_pubmed_pmc | A validated LC–MS/MS method for clinical pharmacokinetics and presumptive phase II metabolic pathways following oral administration of Andrographis paniculata extract | A validated LC–MS/MS method for clinical pharmacokinetics and presumptive phase II metabolic pathways following oral administration of Andrographis paniculata extract Abstract Abstract Andrographis paniculata , a medicinal plant in Thailand national list of essential medicines, has been proposed for treatment of patien... |
PMC4077254 | core_pubmed_pmc | Development and antitumor activity of a BCL-2 targeted single-stranded DNA oligonucleotide | Development and antitumor activity of a BCL-2 targeted single-stranded DNA oligonucleotide Abstract PNT100 is a 24-base, chemically unmodified DNA oligonucleotide sequence that is complementary to a region upstream of the BCL-2 gene. Exposure of tumor cells to PNT100 results in suppression of proliferation and cell dea... |
PMC10870242 | core_pubmed_pmc | Biomarker and pharmacodynamic activity of the transforming growth factor‐beta ( TGFβ) inhibitor SAR439459 as monotherapy and in combination with cemiplimab in a phase I clinical study in patients with advanced solid tumors | Biomarker and pharmacodynamic activity of the transforming growth factor‐beta ( TGFβ) inhibitor SAR439459 as monotherapy and in combination with cemiplimab in a phase I clinical study in patients with advanced solid tumors Abstract Abstract SAR439459, a ‘second‐generation’ human anti‐transforming growth factor‐beta (TG... |
PMC8552828 | core_pubmed_pmc | An experience on the model-based evaluation of pharmacokinetic drug-drug interaction for a long half-life drug | An experience on the model-based evaluation of pharmacokinetic drug-drug interaction for a long half-life drug Abstract Abstract Fixed-dose combinations development requires pharmacokinetic drug-drug interaction (DDI) studies between active ingredients. For some drugs, pharmacokinetic properties such as long half-life ... |
PMC11047560 | core_pubmed_pmc | Revisiting the Checkerboard to Inform Development of β-Lactam/β-Lactamase Inhibitor Combinations | Revisiting the Checkerboard to Inform Development of β-Lactam/β-Lactamase Inhibitor Combinations Abstract A two-dimensional “checkerboard” array employing systematic titration (e.g., serial two-fold dilutions) is a well-established in vitro method for exploring the antibacterial effects of novel drug combinations. Mini... |
PMC12382569 | core_pubmed_pmc | Safety and feasibility trial protocol of metformin in infants after perinatal brain injury | Safety and feasibility trial protocol of metformin in infants after perinatal brain injury Abstract Abstract Introduction Infants with hypoxic-ischaemic encephalopathy (HIE) are at a high risk for neurodevelopmental impairment, and adjunctive treatments to promote brain repair are needed. The antidiabetic drug metformi... |
PMC7445982 | core_pubmed_pmc | Cytotoxicity Activity and Druggability Studies of Sigmasterol Isolated from Marine Sponge Dysidea avara Against Oral Epithelial Cancer Cell (KB/C152) and T-Lymphocytic Leukemia Cell Line (Jurkat/ E6-1) | Cytotoxicity Activity and Druggability Studies of Sigmasterol Isolated from Marine Sponge Dysidea avara Against Oral Epithelial Cancer Cell (KB/C152) and T-Lymphocytic Leukemia Cell Line (Jurkat/ E6-1) Abstract Abstract Background: Marine sponge is a rich natural resource of many pharmacological compounds and various b... |
PMC12739525 | core_pubmed_pmc | Pharmacogenetic hSLCO1B1*14 ‐Guided Dosing of Methotrexate in Transgenic Arthritic Mice Normalizes Exposure and Response | Pharmacogenetic hSLCO1B1*14 ‐Guided Dosing of Methotrexate in Transgenic Arthritic Mice Normalizes Exposure and Response Abstract ABSTRACT Juvenile idiopathic arthritis (JIA) is a chronic autoimmune disease that negatively affects ~100,000 children under the age of 16 in the United States. About ~30% of these patients ... |
PMC5297531 | core_pubmed_pmc | Quantitative characterization of the mechanism of action and impact of a ‘proteolysis-permitting’ anti-PCSK9 antibody | Quantitative characterization of the mechanism of action and impact of a ‘proteolysis-permitting’ anti-PCSK9 antibody Abstract ABSTRACT A recent report described a novel mechanism of action for an anti-proprotein convertase subtilisin-kexin type 9 (PCSK9) monoclonal antibody (LY3015014, or LY), wherein the antibody has... |
PMC5354814 | core_pubmed_pmc | In silico and in vitro drug screening identifies new therapeutic approaches for Ewing sarcoma | In silico and in vitro drug screening identifies new therapeutic approaches for Ewing sarcoma Abstract Abstract The long-term overall survival of Ewing sarcoma (EWS) patients remains poor; less than 30% of patients with metastatic or recurrent disease survive despite aggressive combinations of chemotherapy, radiation a... |
PMC7032193 | core_pubmed_pmc | Double-layered osmotic pump controlled release tablets of actarit: In vitro and in vivo evaluation | Double-layered osmotic pump controlled release tablets of actarit: In vitro and in vivo evaluation Abstract Abstract The aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations.... |
PMC11048044 | core_pubmed_pmc | Early, precise, and safe clinical evaluation of the pharmacodynamic effects of novel agents in the intact human tumor microenvironment | Early, precise, and safe clinical evaluation of the pharmacodynamic effects of novel agents in the intact human tumor microenvironment Abstract Abstract Introduction: Drug development is systemically inefficient. Research and development costs for novel therapeutics average hundreds of millions to billions of dollars, ... |
PMC4254869 | core_pubmed_pmc | Enhancing Patient Flexibility of Subcutaneous Immunoglobulin G Dosing: Pharmacokinetic Outcomes of Various Maintenance and Loading Regimens in the Treatment of Primary Immunodeficiency | Enhancing Patient Flexibility of Subcutaneous Immunoglobulin G Dosing: Pharmacokinetic Outcomes of Various Maintenance and Loading Regimens in the Treatment of Primary Immunodeficiency Abstract Abstract Introduction Standard treatment for patients with primary immunodeficiency (PID) is monthly intravenous immunoglobuli... |
PMC4778608 | core_pubmed_pmc | Cyclophosphamide pharmacokinetics and pharmacogenetics in children with B-cell non-Hodgkin's lymphoma | Cyclophosphamide pharmacokinetics and pharmacogenetics in children with B-cell non-Hodgkin's lymphoma Abstract Introduction Variation in cyclophosphamide pharmacokinetics and metabolism has been highlighted as a factor that may impact on clinical outcome in various tumour types. The current study in children with B-cel... |
PMC6787744 | core_pubmed_pmc | Plasma Disappearance Rate of Indocyanine Green for Determination of Liver Function in Three Different Models of Shock | Plasma Disappearance Rate of Indocyanine Green for Determination of Liver Function in Three Different Models of Shock Abstract Abstract The measurement of the liver function via the plasma disappearance rate of indocyanine green (PDR ICG ) is a sensitive bed-side tool in critical care. Yet, recent evidence has question... |
PMC4101223 | core_pubmed_pmc | A Novel Chemically Modified Curcumin Reduces Severity of Experimental Periodontal Disease in Rats: Initial Observations | A Novel Chemically Modified Curcumin Reduces Severity of Experimental Periodontal Disease in Rats: Initial Observations Abstract Tetracycline-based matrix metalloproteinase- (MMP-) inhibitors are currently approved for two inflammatory diseases, periodontitis and rosacea. The current study addresses the therapeutic pot... |
PMC10958225 | core_pubmed_pmc | Therapeutic potential of orally applied KB-R7943 in streptozotocin-induced neuropathy in rats | Therapeutic potential of orally applied KB-R7943 in streptozotocin-induced neuropathy in rats Abstract Both peripheral neuropathy and depression can be viewed as neurodegeneration's consequences of diabetes, at least in part coexisting with or resulting from sodium-calcium dysbalance. This study aims to assess the ther... |
PMC8275546 | core_pubmed_pmc | In silico comparison of pharmacokinetic properties of three extended half-life factor IX concentrates | In silico comparison of pharmacokinetic properties of three extended half-life factor IX concentrates Abstract Purpose Pharmacokinetic (PK) differences between the extended half-life (EHL) factor IX (FIX) concentrates for hemophilia B exist, which may influence hemostatic efficacy of replacement therapy in patients. Th... |
PMC8994193 | core_pubmed_pmc | Nucleoside analog GS‐441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid‐19 | Nucleoside analog GS‐441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid‐19 Abstract Abstract GS‐441524, the parent nucleoside of remdesivir, has been proposed to be effective against Covid‐19 based on in vitro studies and studies in animals. However, randomized clinical tri... |
PMC8284454 | core_pubmed_pmc | In Vitro Profiling of Antitubercular Compounds by Rapid, Efficient, and Nondestructive Assays Using Autoluminescent Mycobacterium tuberculosis | In Vitro Profiling of Antitubercular Compounds by Rapid, Efficient, and Nondestructive Assays Using Autoluminescent Mycobacterium tuberculosis Abstract ABSTRACT Anti-infective drug discovery is greatly facilitated by the availability of in vitro assays that are more proficient at predicting the preclinical success of s... |
PMC5146818 | core_pubmed_pmc | Coagulase negative staphylococcal sepsis in neonates: do we need to adapt vancomycin dose or target? | Coagulase negative staphylococcal sepsis in neonates: do we need to adapt vancomycin dose or target? Abstract Background Despite differences in types of infection and causative organisms, pharmacokinetic-pharmacodynamic (PKPD) targets of vancomycin therapy derived from adult studies are suggested for neonates. We aimed... |
PMC8252934 | core_pubmed_pmc | Factor VIII activity and bleeding risk during prophylaxis for severe hemophilia A: a population pharmacokinetic model | Factor VIII activity and bleeding risk during prophylaxis for severe hemophilia A: a population pharmacokinetic model Abstract During factor VIII prophylaxis for severe hemophilia A, bleeding risk increases with time when factor VIII activity is below 1%. However, maintaining trough activity above 1% does not protect a... |
PMC9298894 | core_pubmed_pmc | Assessment of Pharmacokinetic Interaction Between Gefapixant (MK‐7264), a P2X3 Receptor Antagonist, and the OATP1B1 Drug Transporter Substrate Pitavastatin | Assessment of Pharmacokinetic Interaction Between Gefapixant (MK‐7264), a P2X3 Receptor Antagonist, and the OATP1B1 Drug Transporter Substrate Pitavastatin Abstract Abstract Gefapixant (MK‐7264, AF‐219), a first‐in‐class P2X3 antagonist, is being developed as oral treatment for refractory or unexplained chronic cough. ... |
PMC7373696 | core_pubmed_pmc | Model informed quantification of the feed‐forward stimulation of growth hormone by growth hormone‐releasing hormone | Model informed quantification of the feed‐forward stimulation of growth hormone by growth hormone‐releasing hormone Abstract Aims Growth hormone (GH) secretion is pulsatile and secretion varies highly between individuals. To understand and ultimately predict GH secretion, it is important to first delineate and quantify... |
PMC9379324 | core_pubmed_pmc | Utomilumab in Patients With Immune Checkpoint Inhibitor-Refractory Melanoma and Non-Small-Cell Lung Cancer | Utomilumab in Patients With Immune Checkpoint Inhibitor-Refractory Melanoma and Non-Small-Cell Lung Cancer Abstract Section Head Clinical/translational cancer immunotherapy Background The goal of this study was to estimate the objective response rate for utomilumab in adults with immune checkpoint inhibitor (ICI)-refra... |
PMC5843319 | core_pubmed_pmc | Effect of Tinidazole on Norfloxacin Disposition | Effect of Tinidazole on Norfloxacin Disposition Abstract Abstract Co-administration of norfloxacin (NFX) and tinidazole (TNZ) has been used for the treatment of gastrointestinal and urinary tract infections. Concomitant oral administration of NFX with TNZ may affect NFX absorption and consequently its blood concentrati... |
PMC8495293 | core_pubmed_pmc | Phase 1, pharmacogenomic, dose‐expansion study of pegargiminase plus pemetrexed and cisplatin in patients with ASS1‐deficient non‐squamous non‐small cell lung cancer | Phase 1, pharmacogenomic, dose‐expansion study of pegargiminase plus pemetrexed and cisplatin in patients with ASS1‐deficient non‐squamous non‐small cell lung cancer Abstract Abstract Introduction We evaluated the arginine‐depleting enzyme pegargiminase (ADI‐PEG20; ADI) with pemetrexed (Pem) and cisplatin (Cis) (ADIPem... |
PMC6148059 | core_pubmed_pmc | Interaction of p-synephrine on the pharmacodynamics and pharmacokinetics of gliclazide in animal models | Interaction of p-synephrine on the pharmacodynamics and pharmacokinetics of gliclazide in animal models Abstract Background Type 2 diabetes is frequently seen in patients suffering from obesity. p-synephrine and gliclazide are widely used medicines for the treatment of obesity and diabetes, respectively. Objectives The... |
PMC4777260 | core_pubmed_pmc | Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target | Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target Abstract Abstract The benefits of novel oral anticoagulants are hampered by bleeding. Since coagulation factor IX (fIX) lies upstream of fX in the coagulation cascade, and intermediate levels have been associated with reduc... |
PMC12538705 | core_pubmed_pmc | Recent advances in biomimetic nanodelivery systems for the treatment of osteoporosis | Recent advances in biomimetic nanodelivery systems for the treatment of osteoporosis Abstract Abstract Osteoporosis is a progressive skeletal disorder characterized by imbalanced bone remodeling, microarchitectural deterioration, and increased fracture risk. Despite the availability of various antiresorptive and anabol... |
PMC7354451 | core_pubmed_pmc | Failure of Achieving Tacrolimus Target Blood Concentration Might Be Avoided by a Wide Genotyping of Transplanted Patients: Evidence from a Retrospective Study | Failure of Achieving Tacrolimus Target Blood Concentration Might Be Avoided by a Wide Genotyping of Transplanted Patients: Evidence from a Retrospective Study Abstract Abstract Precise tacrolimus treatment in transplanted patients is achieved in the clinical setting by performing therapeutic drug monitoring (TDM) and c... |
PMC11712606 | core_pubmed_pmc | The Effect of Exercise on Pharmacodynamics and Pharmacokinetics of a Single Dose of Unfractionated Heparin—A Randomized, Controlled, Crossover Study | The Effect of Exercise on Pharmacodynamics and Pharmacokinetics of a Single Dose of Unfractionated Heparin—A Randomized, Controlled, Crossover Study Abstract ABSTRACT Exercise increases blood and lymph flow in working muscles, potentially affecting the bioavailability and effect of subcutaneously administered drugs. Th... |
PMC12014301 | core_pubmed_pmc | Ruxolitinib-dependent reduction of seizure load and duration is accompanied by spatial memory improvement in the rat pilocarpine model of temporal lobe epilepsy | Ruxolitinib-dependent reduction of seizure load and duration is accompanied by spatial memory improvement in the rat pilocarpine model of temporal lobe epilepsy Abstract Abstract Molecules with optimized pharmacokinetic properties selectively aimed at the inhibition of STAT3 phosphorylation in brain have recently emerg... |
PMC7496261 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Dupilumab in Healthy Adult Subjects | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Dupilumab in Healthy Adult Subjects Abstract Abstract Dupilumab is a fully human monoclonal antibody directed against the interleukin (IL)‐4 receptor α subunit (IL‐4Rα) of IL‐4 heterodimeric type I and type II receptors that mediate IL‐4/IL‐13 signaling th... |
PMC6332412 | core_pubmed_pmc | Validated LC-MS/MS Method for the Determination of Scopoletin in Rat Plasma and Its Application to Pharmacokinetic Studies | Validated LC-MS/MS Method for the Determination of Scopoletin in Rat Plasma and Its Application to Pharmacokinetic Studies Abstract Abstract A rapid, sensitive and selective liquid chromatography-electrospray ionization-tandem mass spectrometric method was developed and validated for the quantification of scopoletin in... |
PMC4500654 | core_pubmed_pmc | Utility of a high VWF:FVIII ratio in preventing FVIII accumulation: a study in VWF-deficient mice | Utility of a high VWF:FVIII ratio in preventing FVIII accumulation: a study in VWF-deficient mice Abstract Abstract Treatment of von Willebrand disease typically requires multiple infusions of von Willebrand factor (VWF)/factor VIII (FVIII) concentrate. Accumulation of FVIII is a clinical concern due to potential risk ... |
PMC6272098 | core_pubmed_pmc | RK‐287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model | RK‐287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model Abstract Abstract Aberrant activation of Wnt/β‐catenin signaling causes tumorigenesis and promotes the proliferation of colorectal cancer cells. Porcupine inhibitors, which block secretion of Wnt ligands, m... |
PMC8488766 | core_pubmed_pmc | Neoadjuvant Treatment with Angiogenesis‐Inhibitor Dovitinib Prior to Local Therapy in Hepatocellular Carcinoma: A Phase II Study | Neoadjuvant Treatment with Angiogenesis‐Inhibitor Dovitinib Prior to Local Therapy in Hepatocellular Carcinoma: A Phase II Study Abstract Abstract Background Hepatocellular carcinoma (HCC) recurrence rates following locoregional treatment are high. As multireceptor tyrosine kinase inhibitors targeting vascular endothel... |
PMC7904081 | core_pubmed_pmc | Acute coronary syndromes with high thrombotic burden: therapeutic innovations | Acute coronary syndromes with high thrombotic burden: therapeutic innovations Abstract Abstract Antiplatelet agents represent one of the cornerstones of drug therapy for acute coronary syndromes (ACS). In the last decade, the arrival of prasugrel and ticagrelor, faster and more powerful oral platelet receptor P2Y12 inh... |
PMC9982780 | core_pubmed_pmc | Target attainment and population pharmacokinetics of flucloxacillin in critically ill patients: a multicenter study | Target attainment and population pharmacokinetics of flucloxacillin in critically ill patients: a multicenter study Abstract Purpose Insufficient antimicrobial exposure has been associated with worse clinical outcomes. Reportedly , flucloxacillin target attainment in critically ill patients was heterogeneous considerin... |
PMC10526757 | core_pubmed_pmc | Cannabinoids in Medicine: A Multifaceted Exploration of Types, Therapeutic Applications, and Emerging Opportunities in Neurodegenerative Diseases and Cancer Therapy | Cannabinoids in Medicine: A Multifaceted Exploration of Types, Therapeutic Applications, and Emerging Opportunities in Neurodegenerative Diseases and Cancer Therapy Abstract Abstract In this review article, we embark on a thorough exploration of cannabinoids, compounds that have garnered considerable attention for thei... |
PMC10368966 | core_pubmed_pmc | Safety and efficacy of AK0529 in respiratory syncytial virus‐infected infant patients: A phase 2 proof‐of‐concept trial | Safety and efficacy of AK0529 in respiratory syncytial virus‐infected infant patients: A phase 2 proof‐of‐concept trial Abstract Abstract Background Respiratory syncytial virus (RSV) infection is a cause of substantial morbidity and mortality in young children. There is currently no effective therapy available. Methods... |
PMC10293630 | core_pubmed_pmc | Randomized controlled phase IIa clinical trial of safety, pharmacokinetics and pharmacodynamics of tenofovir and tenofovir plus levonorgestrel releasing intravaginal rings used by women in Kenya | Randomized controlled phase IIa clinical trial of safety, pharmacokinetics and pharmacodynamics of tenofovir and tenofovir plus levonorgestrel releasing intravaginal rings used by women in Kenya Abstract Introduction Globally, many young women face the overlapping burden of HIV infection and unintended pregnancy. Prote... |
PMC7375060 | core_pubmed_pmc | The association of COMT genotype with buproprion treatment response in the treatment of major depressive disorder | The association of COMT genotype with buproprion treatment response in the treatment of major depressive disorder Abstract Abstract Background Pharmacodynamics and pharmacogenetics are being explored in pharmacological treatment response for major depressive disorder (MDD). Interactions between genotype and treatment r... |
PMC10535857 | core_pubmed_pmc | Comprehensive Assessment of Pharmacokinetics, Pharmacodynamics, and Tolerability of Ligelizumab in Healthy Volunteers and Patients with Chronic Spontaneous Urticaria to Optimize Its Subcutaneous Delivery System | Comprehensive Assessment of Pharmacokinetics, Pharmacodynamics, and Tolerability of Ligelizumab in Healthy Volunteers and Patients with Chronic Spontaneous Urticaria to Optimize Its Subcutaneous Delivery System Abstract Abstract Ligelizumab is a highly potent, humanized IgG1, anti-IgE monoclonal antibody. To explore it... |
PMC4632357 | core_pubmed_pmc | Impact of chrysosplenetin on the pharmacokinetics and anti-malarial efficacy of artemisinin against Plasmodium berghei as well as in vitro CYP450 enzymatic activities in rat liver microsome | Impact of chrysosplenetin on the pharmacokinetics and anti-malarial efficacy of artemisinin against Plasmodium berghei as well as in vitro CYP450 enzymatic activities in rat liver microsome Abstract Background Artemisinin (ART) is an efficacious and safe anti-malarial drugs but has low oral bioavailability and auto-ind... |
PMC6132501 | core_pubmed_pmc | Individualization of Irinotecan Treatment: A Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics | Individualization of Irinotecan Treatment: A Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics Abstract Since its clinical introduction in 1998, the topoisomerase I inhibitor irinotecan has been widely used in the treatment of solid tumors, including colorectal, pancreatic, and lung cancer. Irinotecan ... |
PMC7915178 | core_pubmed_pmc | Exploring the Interplay between Drug Release and Targeting of Lipid-Like Polymer Nanoparticles Loaded with Doxorubicin | Exploring the Interplay between Drug Release and Targeting of Lipid-Like Polymer Nanoparticles Loaded with Doxorubicin Abstract Targeted delivery of doxorubicin still poses a challenge with regards to the quantities reaching the target site as well as the specificity of the uptake. In the present approach, two colloida... |
PMC7035301 | core_pubmed_pmc | Food Effect on a Single High Dose of Carotegrast Methyl, an Oral Antagonist of α4-Integrin, in Healthy Male Subjects: A Randomised, Placebo-Controlled, Double-Blind Study | Food Effect on a Single High Dose of Carotegrast Methyl, an Oral Antagonist of α4-Integrin, in Healthy Male Subjects: A Randomised, Placebo-Controlled, Double-Blind Study Abstract Background and Objectives Carotegrast methyl, a novel prodrug, oral antagonist of α4-integrin, is in development for the treatment of active... |
PMC8111026 | core_pubmed_pmc | A randomized trial of safety and pharmacodynamic interactions between a selective glucocorticoid receptor antagonist, PT150, and ethanol in healthy volunteers | A randomized trial of safety and pharmacodynamic interactions between a selective glucocorticoid receptor antagonist, PT150, and ethanol in healthy volunteers Abstract PT150, a novel competitive glucocorticoid receptor (GR) antagonist, has proven safe in animal models, healthy volunteers, and people with depression. Ou... |
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