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PMC7829356 | core_pubmed_pmc | In vivo Pharmacokinetic and Pharmacodynamic (PK/PD) Modeling and Establishment of the PK/PD Cutoff of Florfenicol Against Pasteurella multocida in Ducks | In vivo Pharmacokinetic and Pharmacodynamic (PK/PD) Modeling and Establishment of the PK/PD Cutoff of Florfenicol Against Pasteurella multocida in Ducks Abstract Abstract Pasteurella multocida can invade and translocate through endothelial cells and result in vascular-system infection, which can cause severe economic l... |
PMC12116316 | core_pubmed_pmc | Evaluation of drug interactions in outpatients taking antipsychotic medications | Evaluation of drug interactions in outpatients taking antipsychotic medications Abstract Abstract Introduction Drug-drug interactions (DDIs) of antipsychotic medications are clinically significant as they can result in toxicity or treatment failure. This study aims to assess the potential drug-drug and drug-tobacco int... |
PMC7669507 | core_pubmed_pmc | Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment | Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment Abstract Aim Agomelatine (AGM) is the first melatonergic antidepressant. It suffers from low oral bioavailability (<5%) due to extensive hepatic ... |
PMC6041735 | core_pubmed_pmc | In silico (computed) modelling of doses and dosing regimens associated with morphine levels above international legal driving limits | In silico (computed) modelling of doses and dosing regimens associated with morphine levels above international legal driving limits Abstract Abstract Background: Morphine can cause central nervous system side effects which impair driving skills. The legal blood morphine concentration limit for driving is 20 µg/L in Fr... |
PMC6816231 | core_pubmed_pmc | A Phase 1, Randomized, Double-Blind, Single-Dose, Placebo-Controlled Safety, Tolerability, And Pharmacokinetic/Pharmacodynamic Study Of Evolocumab In Healthy Chinese Subjects | A Phase 1, Randomized, Double-Blind, Single-Dose, Placebo-Controlled Safety, Tolerability, And Pharmacokinetic/Pharmacodynamic Study Of Evolocumab In Healthy Chinese Subjects Abstract Purpose Evolocumab is a human monoclonal antibody that reduces circulating low-density lipoprotein cholesterol (LDL-C) by inhibiting pro... |
PMC9146690 | core_pubmed_pmc | Morphine Accumulates in the Retina Following Chronic Systemic Administration | Morphine Accumulates in the Retina Following Chronic Systemic Administration Abstract Abstract Opioid transport into the central nervous system is crucial for the analgesic efficacy of opioid drugs. Thus, the pharmacokinetics of opioid analgesics such as morphine have been extensively studied in systemic circulation an... |
PMC8876811 | core_pubmed_pmc | Oligonucleotide Therapeutics: From Discovery and Development to Patentability | Oligonucleotide Therapeutics: From Discovery and Development to Patentability Abstract Abstract Following the first proof of concept of using small nucleic acids to modulate gene expression, a long period of maturation led, at the end of the last century, to the first marketing authorization of an oligonucleotide-based... |
PMC3059997 | core_pubmed_pmc | Exploring Indirect Sources of Human Exposure to Perfluoroalkyl Carboxylates (PFCAs): Evaluating Uptake, Elimination, and Biotransformation of Polyfluoroalkyl Phosphate Esters (PAPs) in the Rat | Exploring Indirect Sources of Human Exposure to Perfluoroalkyl Carboxylates (PFCAs): Evaluating Uptake, Elimination, and Biotransformation of Polyfluoroalkyl Phosphate Esters (PAPs) in the Rat Abstract Abstract Background Perfluorinated carboxylic acids (PFCAs) are ubiquitous in human sera worldwide. Biotransformation ... |
PMC7500907 | core_pubmed_pmc | COVID-19 outbreak: Challenges in pharmacotherapy based on pharmacokinetic and pharmacodynamic aspects of drug therapy in patients with moderate to severe infection | COVID-19 outbreak: Challenges in pharmacotherapy based on pharmacokinetic and pharmacodynamic aspects of drug therapy in patients with moderate to severe infection Abstract Highlights • Individualized pharmacotherapy is required in COVID-19 patients with underlying diseases, especially cardiac, liver and kidney disease... |
PMC10624793 | core_pubmed_pmc | The use of therapeutic drug monitoring to highlight an over-looked drug-drug interaction leading to imatinib treatment failure | The use of therapeutic drug monitoring to highlight an over-looked drug-drug interaction leading to imatinib treatment failure Abstract Abstract Background Chronic oral anticancer therapies, are increasingly prescribed and present new challenges including the enhanced risk of overlooked drug-drug interactions (DDIs). L... |
PMC12165970 | core_pubmed_pmc | Pharmacokinetic bioequivalence of the fixed-dose combination of pertuzumab and trastuzumab administered subcutaneously using a handheld syringe or an on-body delivery system | Pharmacokinetic bioequivalence of the fixed-dose combination of pertuzumab and trastuzumab administered subcutaneously using a handheld syringe or an on-body delivery system Abstract Abstract Purpose This randomized, open-label, two-arm, parallel-group, single dose, multi-center phase I study (ClinicalTrials.gov ID, NC... |
PMC9928655 | core_pubmed_pmc | A phase III, randomised, double‐blind, multi‐national clinical trial comparing SB12 (proposed eculizumab biosimilar) and reference eculizumab in patients with paroxysmal nocturnal haemoglobinuria | A phase III, randomised, double‐blind, multi‐national clinical trial comparing SB12 (proposed eculizumab biosimilar) and reference eculizumab in patients with paroxysmal nocturnal haemoglobinuria Abstract Abstract Treatment of paroxysmal nocturnal haemoglobinuria (PNH) includes the monoclonal antibody eculizumab. This ... |
PMC7979602 | core_pubmed_pmc | Mechanism-based modeling of the effect of a novel inhibitor of vascular adhesion protein-1 on albuminuria and renal function markers in patients with diabetic kidney disease | Mechanism-based modeling of the effect of a novel inhibitor of vascular adhesion protein-1 on albuminuria and renal function markers in patients with diabetic kidney disease Abstract The vascular adhesion protein-1 (VAP-1) inhibitor ASP8232 reduces albuminuria in patients with type 2 diabetes and chronic kidney disease... |
PMC5438822 | core_pubmed_pmc | Pharmacokinetics and safety of carfilzomib in patients with relapsed multiple myeloma and end-stage renal disease (ESRD): an open-label, single-arm, phase I study | Pharmacokinetics and safety of carfilzomib in patients with relapsed multiple myeloma and end-stage renal disease (ESRD): an open-label, single-arm, phase I study Abstract Purpose The pharmacokinetics (PK) of carfilzomib have been previously studied in multiple myeloma patients with varying degrees of renal impairment ... |
PMC9458004 | core_pubmed_pmc | Simultaneous Determination and Pharmacokinetics Study of Three Triterpenes from Sanguisorba officinalis L. in Rats by UHPLC–MS/MS | Simultaneous Determination and Pharmacokinetics Study of Three Triterpenes from Sanguisorba officinalis L. in Rats by UHPLC–MS/MS Abstract Abstract A selective and rapid ultra-high-performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) method was established and validated for the determination of ziyu... |
PMC12554205 | core_pubmed_pmc | Safety, pharmacokinetic, pharmacodynamic, and efficacy properties of orally administered APG-2449 in patients with advanced ALK + and ROS1 + non-small-cell lung cancer: a multicentre, open-label, single-arm phase 1 trial | Safety, pharmacokinetic, pharmacodynamic, and efficacy properties of orally administered APG-2449 in patients with advanced ALK + and ROS1 + non-small-cell lung cancer: a multicentre, open-label, single-arm phase 1 trial Abstract Summary Background APG-2449 is a focal adhesion kinase (FAK) inhibitor and a third-generat... |
PMC10751523 | core_pubmed_pmc | A nude mutant rat derived from Sprague Dawley-National Institute of Nutrition rat colony with normal thymus: A potential model for noncommunicable diseases | A nude mutant rat derived from Sprague Dawley-National Institute of Nutrition rat colony with normal thymus: A potential model for noncommunicable diseases Abstract BACKGROUND: A spontaneous mutant rat with a hairless phenotype and an intact thymus was discovered in a long-standing Sprague Dawley-National Institute of ... |
PMC6061137 | core_pubmed_pmc | Phase 1 and pharmacokinetic study of LY3007113, a p38 MAPK inhibitor, in patients with advanced cancer | Phase 1 and pharmacokinetic study of LY3007113, a p38 MAPK inhibitor, in patients with advanced cancer Abstract Summary Background The signaling protein p38 mitogen-activated protein kinase (MAPK) regulates the tumor cell microenvironment, modulating cell survival, migration, and invasion. This phase 1 study evaluated ... |
PMC5038241 | core_pubmed_pmc | Single-Ascending-Dose Pharmacokinetic Study of Tribendimidine in Opisthorchis viverrini -Infected Patients | Single-Ascending-Dose Pharmacokinetic Study of Tribendimidine in Opisthorchis viverrini -Infected Patients Abstract Abstract Praziquantel is the only drug available for the treatment of Opisthorchis viverrini infections. Tribendimidine has emerged as a potential treatment alternative; however, its pharmacokinetic (PK) ... |
PMC10933606 | core_pubmed_pmc | In vitro PK/PD modeling of tyrosine kinase inhibitors in non‐small cell lung cancer cell lines | In vitro PK/PD modeling of tyrosine kinase inhibitors in non‐small cell lung cancer cell lines Abstract Abstract Tyrosine kinase inhibitors (TKIs) are routinely prescribed for the treatment of non‐small cell lung cancer (NSCLC). As with all medications, patients can experience adverse events due to TKIs. Unfortunately,... |
PMC11649739 | core_pubmed_pmc | Population Pharmacokinetics of Ensitrelvir in Healthy Participants and Participants with SARS-CoV-2 Infection in the SCORPIO-SR Study | Population Pharmacokinetics of Ensitrelvir in Healthy Participants and Participants with SARS-CoV-2 Infection in the SCORPIO-SR Study Abstract Abstract Introduction Ensitrelvir, a novel oral inhibitor of the 3C-like protease of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has shown efficacy and safety ... |
PMC5711937 | core_pubmed_pmc | MALDI mass spectrometry imaging of erlotinib administered in combination with bevacizumab in xenograft mice bearing B901L, EGFR-mutated NSCLC cells | MALDI mass spectrometry imaging of erlotinib administered in combination with bevacizumab in xenograft mice bearing B901L, EGFR-mutated NSCLC cells Abstract Abstract Combination therapy of erlotinib plus bevacizumab improves progression-free survival of patients with epidermal growth factor receptor–mutated (EGFR-mutat... |
PMC12013959 | core_pubmed_pmc | Efficacy of Mavacamten in Reducing Cardiac Obstruction in an Elderly Patient with Hypertrophic Cardiomyopathy: A Case Study | Efficacy of Mavacamten in Reducing Cardiac Obstruction in an Elderly Patient with Hypertrophic Cardiomyopathy: A Case Study Abstract Patient: Male, 91-year-old Final Diagnosis: Hypertrophic cardiomyopathy Symptoms: Worsening shortness of breath Clinical Procedure: — Specialty: Cardiology Objective: Unusual or unexpecte... |
PMC10301107 | core_pubmed_pmc | Effectiveness of Pharmacokinetic-Guided Hydroxyurea Dose Individualization in Patients with Sickle Cell Anemia: A Mini-Review | Effectiveness of Pharmacokinetic-Guided Hydroxyurea Dose Individualization in Patients with Sickle Cell Anemia: A Mini-Review Abstract Inconsistent therapeutic responses have been observed among patients with sickle cell anemia (SCA) undergoing hydroxyurea (HU) following the adoption of the standardized protocol. Moreo... |
PMC11235400 | core_pubmed_pmc | Comparative In Vitro and In Silico Analyses of Phytochemicals From Butea monosperma for Wound-Healing Potential in Human Cells | Comparative In Vitro and In Silico Analyses of Phytochemicals From Butea monosperma for Wound-Healing Potential in Human Cells Abstract Aim The objective of this study is to investigate the phytochemicals present in Butea monosperma and assess their potential for healing wounds using a computational comparative method.... |
PMC6944734 | core_pubmed_pmc | NGP 555, a γ-secretase modulator, shows a beneficial shift in the ratio of amyloid biomarkers in human cerebrospinal fluid at safe doses | NGP 555, a γ-secretase modulator, shows a beneficial shift in the ratio of amyloid biomarkers in human cerebrospinal fluid at safe doses Abstract Introduction Currently, there is no cure for Alzheimer's disease (AD), and it is widely accepted that AD is a complex disease with multiple approaches necessary to prevent an... |
PMC8172216 | core_pubmed_pmc | Comparative pharmacokinetic analysis of raw and steamed Panax notoginseng roots in rats by UPLC-MS/MS for simultaneously quantifying seven saponins | Comparative pharmacokinetic analysis of raw and steamed Panax notoginseng roots in rats by UPLC-MS/MS for simultaneously quantifying seven saponins Abstract Abstract Context After being steamed, the restorative effects of Panax notoginseng (Burk.) F. H. Chen (Araliaceae) will be strengthened. However, the underlying me... |
PMC4792338 | core_pubmed_pmc | Treatment with subcutaneous and transdermal fentanyl: results from a population pharmacokinetic study in cancer patients | Treatment with subcutaneous and transdermal fentanyl: results from a population pharmacokinetic study in cancer patients Abstract Purpose Transdermal fentanyl is effective for the treatment of moderate to severe cancer-related pain but is unsuitable for fast titration. In this setting, continuous subcutaneous fentanyl ... |
PMC12844645 | core_pubmed_pmc | Hitting the Target: Model-Informed Precision Dosing of Tobramycin in Pediatric Patients with Cystic Fibrosis | Hitting the Target: Model-Informed Precision Dosing of Tobramycin in Pediatric Patients with Cystic Fibrosis Abstract Background: Tobramycin is a key therapy for pulmonary exacerbations in children and adolescents with cystic fibrosis (CF), yet its variable pharmacokinetics (PK) combined with narrow therapeutic index n... |
PMC10175976 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of fluoropezil ( DC20 ), a novel acetylcholinesterase inhibitor: A phase I study in healthy young and elderly Chinese subjects | Safety, tolerability, and pharmacokinetics of fluoropezil ( DC20 ), a novel acetylcholinesterase inhibitor: A phase I study in healthy young and elderly Chinese subjects Abstract Abstract The present study evaluated the safety, tolerability, and pharmacokinetics of fluoropezil (DC20), a novel acetylcholinesterase inhib... |
PMC8000041 | core_pubmed_pmc | New Insights into the Metabolism of the Flavanones Eriocitrin and Hesperidin: A Comparative Human Pharmacokinetic Study | New Insights into the Metabolism of the Flavanones Eriocitrin and Hesperidin: A Comparative Human Pharmacokinetic Study Abstract Abstract The intake of hesperidin-rich sources, mostly found in orange juice, can decrease cardiometabolic risk, potentially linked to the gut microbial phase-II hesperetin derivatives. Howev... |
PMC5591810 | core_pubmed_pmc | Target-Mediated Drug Disposition Population Pharmacokinetics Model of Alirocumab in Healthy Volunteers and Patients: Pooled Analysis of Randomized Phase I/II/III Studies | Target-Mediated Drug Disposition Population Pharmacokinetics Model of Alirocumab in Healthy Volunteers and Patients: Pooled Analysis of Randomized Phase I/II/III Studies Abstract Abstract Background and Objective Proprotein convertase subtilisin/kexin type 9 inhibition with monoclonal antibodies such as alirocumab sign... |
PMC3520775 | core_pubmed_pmc | Pharmacokinetic modeling of P-glycoprotein function at the rat and human blood–brain barriers studied with ( R )-[ 11 C]verapamil positron emission tomography | Pharmacokinetic modeling of P-glycoprotein function at the rat and human blood–brain barriers studied with ( R )-[ 11 C]verapamil positron emission tomography Abstract Background This study investigated the influence of P-glycoprotein (P-gp) inhibitor tariquidar on the pharmacokinetics of P-gp substrate radiotracer ( R... |
PMC9227286 | core_pubmed_pmc | Pre-Clinical Evaluation of Tenofovir and Tenofovir Alafenamide for HIV-1 Pre-Exposure Prophylaxis in Foreskin Tissue | Pre-Clinical Evaluation of Tenofovir and Tenofovir Alafenamide for HIV-1 Pre-Exposure Prophylaxis in Foreskin Tissue Abstract Background: HIV-1 pre-exposure prophylaxis (PrEP) has focused predominantly on protective efficacy in receptive sex, with limited research on the dosing requirements for insertive sex. We pre-cl... |
PMC6856260 | core_pubmed_pmc | The Effect of Food Intake on the Pharmacokinetics of Oral Basal Insulin: A Randomised Crossover Trial in Healthy Male Subjects | The Effect of Food Intake on the Pharmacokinetics of Oral Basal Insulin: A Randomised Crossover Trial in Healthy Male Subjects Abstract Abstract Background Oral insulin 338 is a novel tablet formulation of a long-acting basal insulin. This randomised, open-label, four-period crossover trial investigated the effect of t... |
PMC11488435 | core_pubmed_pmc | Rapid and sensitive liquid chromatographic–tandem mass spectrometric methods for the quantitation of dolutegravir in human plasma and breast milk | Rapid and sensitive liquid chromatographic–tandem mass spectrometric methods for the quantitation of dolutegravir in human plasma and breast milk Abstract Highlights • Development of LC–MS/MS methods for the quantitation of DTG in plasma and breast milk. • Validation of LC–MS/MS methods for DTG quantitation across matr... |
PMC10081366 | core_pubmed_pmc | Serotonin is a Common Thread Linking Different Classes of Antidepressants | Serotonin is a Common Thread Linking Different Classes of Antidepressants Abstract Summary: Depression pathology remains elusive. The monoamine hypothesis has placed much focus on serotonin, but due to the variable clinical efficacy of monoamine reuptake inhibitors, the community is looking for alternative therapies su... |
PMC2858169 | core_pubmed_pmc | Long-Acting Insulin Analogs and the Risk of Diabetic Ketoacidosis in Children and Adolescents With Type 1 Diabetes | Long-Acting Insulin Analogs and the Risk of Diabetic Ketoacidosis in Children and Adolescents With Type 1 Diabetes Abstract Abstract OBJECTIVE To investigate if long-acting insulin analogs decrease the risk of diabetic ketoacidosis (DKA) in young individuals with type 1 diabetes. RESEARCH DESIGN AND METHODS Of 48,110 t... |
PMC6511062 | core_pubmed_pmc | Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition | Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition Abstract Significance Safer and more effective oral drugs are urgently required to treat visceral leishmaniasis (VL), a neglected parasitic disease that kills 20,000–40,000 people each year in parts of Asia, Africa... |
PMC11252018 | core_pubmed_pmc | Reduced hepatic impairment study to evaluate pharmacokinetics and safety of zavegepant and to inform dosing recommendation for hepatic impairment | Reduced hepatic impairment study to evaluate pharmacokinetics and safety of zavegepant and to inform dosing recommendation for hepatic impairment Abstract Abstract Zavegepant, a high‐affinity, selective, small‐molecule calcitonin gene‐related peptide (CGRP) receptor antagonist, is approved in the United States for acut... |
PMC8224731 | core_pubmed_pmc | CFTR Modulators: Does One Dose Fit All? | CFTR Modulators: Does One Dose Fit All? Abstract Abstract For many people with cystic fibrosis (pwCF), CFTR modulators will be the cornerstone of their treatment. These modulators show robust treatment effects at group level in pwCF with specific mutations. The individual effect however, is variable. In this review we ... |
PMC4000412 | core_pubmed_pmc | Novel LHRH-receptor-targeted cytolytic peptide, EP-100: first-in-human phase I study in patients with advanced LHRH-receptor-expressing solid tumors | Novel LHRH-receptor-targeted cytolytic peptide, EP-100: first-in-human phase I study in patients with advanced LHRH-receptor-expressing solid tumors Abstract Abstract Purpose To conduct a phase I study determining the safety, pharmacokinetics and preliminary efficacy of EP-100, a novel anticancer drug consisting of nat... |
PMC8558060 | core_pubmed_pmc | Patient-Tailored Levothyroxine Dosage with Pharmacokinetic/Pharmacodynamic Modeling: A Novel Approach After Total Thyroidectomy | Patient-Tailored Levothyroxine Dosage with Pharmacokinetic/Pharmacodynamic Modeling: A Novel Approach After Total Thyroidectomy Abstract Abstract Background: After seven decades of levothyroxine (LT4) replacement therapy, dosage adjustment still takes several months. We have developed a decision aid tool (DAT) that mod... |
PMC5912368 | core_pubmed_pmc | Evaluating cardiac risk: exposure response analysis in early clinical drug development | Evaluating cardiac risk: exposure response analysis in early clinical drug development Abstract Abstract The assessment of a drug’s cardiac liability has undergone considerable metamorphosis by regulators since International Council for Harmonization of Technical Requirement for Pharmaceuticals for Human Use E14 guidel... |
PMC6028400 | core_pubmed_pmc | Failure of ceftolozane‐tazobactam salvage therapy in complicated pneumonia with lung abscess | Failure of ceftolozane‐tazobactam salvage therapy in complicated pneumonia with lung abscess Abstract Key Clinical Message Treatment of Pseudomonas aeruginosa remains challenging, despite the availability ceftolozane‐tazobactam. We report a treatment failure with ceftolozane‐tazobactam salvage therapy for pneumonia com... |
PMC4919369 | core_pubmed_pmc | A phase I study of the investigational NEDD8-activating enzyme inhibitor pevonedistat (TAK-924/MLN4924) in patients with metastatic melanoma | A phase I study of the investigational NEDD8-activating enzyme inhibitor pevonedistat (TAK-924/MLN4924) in patients with metastatic melanoma Abstract Summary Purpose The therapeutic index of proteasome inhibitors may be improved through selective inhibition of a sub-component of the ubiquitin-proteasome system, such as... |
PMC12785003 | core_pubmed_pmc | Hinokiflavone as a Potential Antitumor Agent: From Pharmacology to Pharmaceutics | Hinokiflavone as a Potential Antitumor Agent: From Pharmacology to Pharmaceutics Abstract Abstract Hinokiflavone (HF), a natural C-O-C-linked biflavonoid originally isolated from Chamaecyparis obtusa , is a promising multifunctional antitumor agent. Despite challenges posed by multidrug resistance and tumor heterogenei... |
PMC4514594 | core_pubmed_pmc | Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity | Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity Abstract Numerous studies have shown a paradoxical positive correlation between elevated levels of plasminogen activator inhibitior-1 (PAI-1) in tumors and blood of cancer patients with poor clinical outc... |
PMC6197107 | core_pubmed_pmc | Metabolism and metabolomics of ketamine: a toxicological approach | Metabolism and metabolomics of ketamine: a toxicological approach Abstract ABSTRACT Ketamine is a phencyclidine derivative and a non-competitive antagonist of N -methyl- D -aspartate (NMDA) receptor for which glutamate is the full agonist. It produces a functional dissociation between the thalamocortical and limbic sys... |
PMC7292822 | core_pubmed_pmc | Effect of P-glycoprotein (P-gp) Inducers on Exposure of P-gp Substrates: Review of Clinical Drug–Drug Interaction Studies | Effect of P-glycoprotein (P-gp) Inducers on Exposure of P-gp Substrates: Review of Clinical Drug–Drug Interaction Studies Abstract Abstract Understanding transporter-mediated drug–drug interactions (DDIs) for investigational agents is important during drug development to assess DDI liability, its clinical relevance, an... |
PMC10272295 | core_pubmed_pmc | Barriers to global pharmacometrics: educational challenges and opportunities across the globe | Barriers to global pharmacometrics: educational challenges and opportunities across the globe Conclusion ROADMAP FOR NEXT STEPS Training the next generation of pharmacometricians is a challenging task. Until now, it has been tackled through varying approaches across the globe, showcasing unique local challenges that mi... |
PMC5161049 | core_pubmed_pmc | Effect of diurnal variation, CYP2B6 genotype and age on the pharmacokinetics of nevirapine in African children | Effect of diurnal variation, CYP2B6 genotype and age on the pharmacokinetics of nevirapine in African children Abstract Objectives To characterize the effects of CYP2B6 polymorphisms, diurnal variation and demographic factors on nevirapine pharmacokinetics in African children. Methods Non-linear mixed-effects modelling... |
PMC4683619 | core_pubmed_pmc | PRINT: A Protein Bioconjugation Method with Exquisite N-terminal Specificity | PRINT: A Protein Bioconjugation Method with Exquisite N-terminal Specificity Abstract Chemical conjugation is commonly used to enhance the pharmacokinetics, biodistribution, and potency of protein therapeutics, but often leads to non-specific modification or loss of bioactivity. Here, we present a simple, versatile and... |
PMC5385201 | core_pubmed_pmc | Population Pharmacokinetics of Necitumumab in Cancer Patients | Population Pharmacokinetics of Necitumumab in Cancer Patients Abstract Abstract Necitumumab is a second-generation, recombinant, human immunoglobulin G1, epidermal growth factor (EGFR) receptor antibody that specifically blocks the ligand binding site of EGFR. Necitumumab potentially acts by blocking ligand epidermal g... |
PMC3664741 | core_pubmed_pmc | Inhalation of a Dry Powder Ciprofloxacin Formulation in Healthy Subjects: A Phase I Study | Inhalation of a Dry Powder Ciprofloxacin Formulation in Healthy Subjects: A Phase I Study Abstract Background Oral and intravenous formulations of ciprofloxacin have established efficacy and safety profiles in respiratory infections. A dry powder for inhalation (DPI) that uses Novartis’ PulmoSphere™ technology has been... |
PMC11991819 | core_pubmed_pmc | Exploring the Potential of Mitochondria-Targeted Drug Delivery for Enhanced Breast Cancer Therapy | Exploring the Potential of Mitochondria-Targeted Drug Delivery for Enhanced Breast Cancer Therapy Abstract Breast cancer stands as the utmost prevalent malignancy in women, impacting the epithelial tissue of the breast and often displaying resistance to effective treatment due to its diverse molecular and histological ... |
PMC11069600 | core_pubmed_pmc | Molecular docking analysis of marine compounds with voltage gated calcium channel for potential anti-epileptic molecules | Molecular docking analysis of marine compounds with voltage gated calcium channel for potential anti-epileptic molecules Abstract Epileptic seizures are directly linked with an anomalous influx of extracellular calcium or sodium anions through voltage-gated channels disturb the chemical and electrical gradients, result... |
PMC12263513 | core_pubmed_pmc | Enhancing Drug Development for Paediatric Pulmonary Hypertension—An Integrative Perspective | Enhancing Drug Development for Paediatric Pulmonary Hypertension—An Integrative Perspective Abstract ABSTRACT As with adult pulmonary hypertension (PH), high morbidity and mortality persist with diverse types of paediatric PH. Despite major advances in pharmacologic therapies based on extensive studies in adult PH, few... |
PMC8405496 | core_pubmed_pmc | A latent variable approach to account for correlated inputs in global sensitivity analysis | A latent variable approach to account for correlated inputs in global sensitivity analysis Abstract In drug development decision-making is often supported through model-based methods, such as physiologically-based pharmacokinetics (PBPK). Global sensitivity analysis (GSA) is gaining use for quality assessment of model-... |
PMC10904433 | core_pubmed_pmc | Pharmacokinetics of the Novel Nonsteroidal Mineralocorticoid Receptor Antagonist Ocedurenone (KBP-5074) in Individuals with Moderate Hepatic Impairment | Pharmacokinetics of the Novel Nonsteroidal Mineralocorticoid Receptor Antagonist Ocedurenone (KBP-5074) in Individuals with Moderate Hepatic Impairment Abstract Background and Objectives Ocedurenone (KBP-5074) is a novel nonsteroidal mineralocorticoid receptor antagonist that has demonstrated safety and efficacy in cli... |
PMC12360993 | core_pubmed_pmc | A phase I trial evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of intravenously administered low-anticoagulant heparin (M6229) in critically ill sepsis patients | A phase I trial evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of intravenously administered low-anticoagulant heparin (M6229) in critically ill sepsis patients Abstract Abstract Background Histones released in response to cellular injury are important mediators of organ failure and death in... |
PMC12641085 | core_pubmed_pmc | A Pharmacometric Method for Quantitative Determination of Improvement in Body Composition and Characterization of the Exposure–Response Relationship during Treatment of Obesity with Tirzepatide | A Pharmacometric Method for Quantitative Determination of Improvement in Body Composition and Characterization of the Exposure–Response Relationship during Treatment of Obesity with Tirzepatide Abstract Abstract About half of the world’s population is living with overweight or obesity. Tirzepatide is an approved treatm... |
PMC4341010 | core_pubmed_pmc | Phase I study of nanoliposomal irinotecan (PEP02) in advanced solid tumor patients | Phase I study of nanoliposomal irinotecan (PEP02) in advanced solid tumor patients Abstract Purpose To define the dose-limiting toxicity (DLT), maximum tolerated dose (MTD) and pharmacokinetics (PK) of PEP02, a novel liposome-encapsulated irinotecan, in patients with advanced refractory solid tumors. Methods Patients w... |
PMC8004375 | core_pubmed_pmc | Pharmacokinetic Study of Safrole and Methyl Eugenol after Oral Administration of the Essential Oil Extracts of Asarum in Rats by GC-MS | Pharmacokinetic Study of Safrole and Methyl Eugenol after Oral Administration of the Essential Oil Extracts of Asarum in Rats by GC-MS Abstract Abstract Asarum is a traditional medicine and has been widely used as remedies for inflammatory diseases, toothache, headache, local anesthesia, and aphthous stomatitis in Chin... |
PMC10174206 | core_pubmed_pmc | Allometric Scaling of Testosterone Enanthate Pharmacokinetics to Adolescent Hypogonadal Males (IM and SC Administration) | Allometric Scaling of Testosterone Enanthate Pharmacokinetics to Adolescent Hypogonadal Males (IM and SC Administration) Abstract Abstract Context Intramuscular (IM) testosterone enanthate (TE) and testosterone pellets were US Food and Drug Administration approved before 1962 for pediatric use but not studied in contro... |
PMC8765251 | core_pubmed_pmc | Orally administered intelligent self-ablating nanoparticles: a new approach to improve drug cellular uptake and intestinal absorption | Orally administered intelligent self-ablating nanoparticles: a new approach to improve drug cellular uptake and intestinal absorption Abstract Abstract Oral drug delivery to treat diabetes is being increasingly researched. The mucus and the epithelial cell layers hinder drug delivery. We designed a self-ablating nanopa... |
PMC9685347 | core_pubmed_pmc | MagMD: Database summarizing the metabolic action of gut microbiota to drugs | MagMD: Database summarizing the metabolic action of gut microbiota to drugs Abstract An increasing number of studies have reported that microbiome can affect drug response by altering pharmacokinetics and pharmacodynamics of formation of toxic metabolites. With the development of metagenomic sequencing, gut microbial c... |
PMC11719599 | core_pubmed_pmc | Exploring the Impact of Pharmaceutical Excipient PEG400 on the Pharmacokinetics of Mycophenolic Acid Through In Vitro and In Vivo Experiments | Exploring the Impact of Pharmaceutical Excipient PEG400 on the Pharmacokinetics of Mycophenolic Acid Through In Vitro and In Vivo Experiments Abstract Abstract Mycophenolic acid (MPA) is a commonly used immunosuppressant. In the human body, MPA is metabolized into mycophenolic acid 7-O-glucuronide (MPAG) and mycophenol... |
PMC10800285 | core_pubmed_pmc | Preclinical Activity of Two Paclitaxel Nanoparticle Formulations After Intraperitoneal Administration in Ovarian Cancer Murine Xenografts | Preclinical Activity of Two Paclitaxel Nanoparticle Formulations After Intraperitoneal Administration in Ovarian Cancer Murine Xenografts Abstract Abstract Background Epithelial ovarian cancer is associated with high mortality due to diagnosis at later stages associated with peritoneal involvement. Several trials have ... |
PMC5868588 | core_pubmed_pmc | Influence of ABCB1 and CYP3A5 gene polymorphisms on pharmacokinetics of apixaban in patients with atrial fibrillation and acute stroke | Influence of ABCB1 and CYP3A5 gene polymorphisms on pharmacokinetics of apixaban in patients with atrial fibrillation and acute stroke Abstract Introduction Difficulties in non-vitamin K anticoagulant (NOAC) administration in acute stroke can be associated with changes in pharmacokinetic parameters of NOAC such as biot... |
PMC7772249 | core_pubmed_pmc | A New Framework to Implement Model-Informed Dosing in Clinical Guidelines: Piperacillin and Amikacin as Proof of Concept | A New Framework to Implement Model-Informed Dosing in Clinical Guidelines: Piperacillin and Amikacin as Proof of Concept Abstract Background : Modeling and simulation is increasingly used to study pediatric pharmacokinetics, but clinical implementation of age-appropriate doses lags behind. Therefore, we aimed to develo... |
PMC4444288 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling Is Essential in 90 Y-Labeled Anti-CD66 Radioimmunotherapy | Physiologically Based Pharmacokinetic Modeling Is Essential in 90 Y-Labeled Anti-CD66 Radioimmunotherapy Abstract Introduction Radioimmunotherapy (RIT) with 90 Y-labeled anti-CD66 antibody is used to selectively irradiate the red marrow (RM) before blood stem cell transplantation of acute leukemia patients. To calculat... |
PMC6219487 | core_pubmed_pmc | Safety and pharmacokinetics of MM-302, a HER2-targeted antibody–liposomal doxorubicin conjugate, in patients with advanced HER2-positive breast cancer: a phase 1 dose-escalation study | Safety and pharmacokinetics of MM-302, a HER2-targeted antibody–liposomal doxorubicin conjugate, in patients with advanced HER2-positive breast cancer: a phase 1 dose-escalation study Abstract Background This phase 1 dose-escalation trial studied MM-302, a novel HER2-targeted PEGylated antibody–liposomal doxorubicin co... |
PMC5962729 | core_pubmed_pmc | Yinchenhao Decoction Ameliorates Alpha-Naphthylisothiocyanate Induced Intrahepatic Cholestasis in Rats by Regulating Phase II Metabolic Enzymes and Transporters | Yinchenhao Decoction Ameliorates Alpha-Naphthylisothiocyanate Induced Intrahepatic Cholestasis in Rats by Regulating Phase II Metabolic Enzymes and Transporters Abstract Abstract Yinchenhao Decoction (YCHD), a famous traditional Chinese formula, has been used for treating cholestasis for 1000s of years. The cholagogic ... |
PMC3333800 | core_pubmed_pmc | Predicting the F(ab)-mediated effect of monoclonal antibodies in vivo by combining cell-level kinetic and pharmacokinetic modelling | Predicting the F(ab)-mediated effect of monoclonal antibodies in vivo by combining cell-level kinetic and pharmacokinetic modelling Abstract Cell-level kinetic models for therapeutically relevant processes increasingly benefit the early stages of drug development. Later stages of the drug development processes, however... |
PMC7384592 | core_pubmed_pmc | Ideal benznidazole dose regimen in chronic chagasic patients: a systematic review | Ideal benznidazole dose regimen in chronic chagasic patients: a systematic review Abstract ABSTRACT The present study aimed to review the existing literature and to evaluate the best dose regimen for benznidazole in adult patients with Chagas disease in the chronic phase. A systematic review was conducted followed by m... |
PMC9389458 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics/pharmacodynamics of JMT103 in patients with bone metastases from solid tumors | Safety, tolerability, and pharmacokinetics/pharmacodynamics of JMT103 in patients with bone metastases from solid tumors Abstract Bone metastases are common complications of solid tumors. The outcome is poor despite major progress in cancer therapies. We describe a multicenter, open-label, phase 1, dose escalation and ... |
PMC7810192 | core_pubmed_pmc | UPLC-MS/MS Method for the Determination of Hyperoside and Application to Pharmacokinetics Study in Rat After Different Administration Routes | UPLC-MS/MS Method for the Determination of Hyperoside and Application to Pharmacokinetics Study in Rat After Different Administration Routes Abstract Abstract A rapid and sensitive UPLC-MS/MS method was developed and fully validated for the quantification of hyperoside in rat plasma after intragastric, intraperitoneal ... |
PMC4030100 | core_pubmed_pmc | Safety and Pharmacokinetics of Escalating Doses of Human Recombinant Nerve Growth Factor Eye Drops in a Double-Masked, Randomized Clinical Trial | Safety and Pharmacokinetics of Escalating Doses of Human Recombinant Nerve Growth Factor Eye Drops in a Double-Masked, Randomized Clinical Trial Abstract Abstract Background and Objectives Nerve growth factor (NGF) is a neurotrophin with therapeutic possibilities that extend from the nervous system to the eye. We teste... |
PMC4352278 | core_pubmed_pmc | Expression of drug transporters in human kidney: impact of sex, age, and ethnicity | Expression of drug transporters in human kidney: impact of sex, age, and ethnicity Abstract Abstract Background Differences in expression of drug transporters in human kidney contribute to changes in pharmacokinetics and toxicokinetics of a variety of drug compounds. The basal expression levels of genes involved in dru... |
PMC5011836 | core_pubmed_pmc | Modelling concentrations of antimicrobial drugs: comparative pharmacokinetics of cephalosporin antimicrobials and accuracy of allometric scaling in food-producing and companion animals | Modelling concentrations of antimicrobial drugs: comparative pharmacokinetics of cephalosporin antimicrobials and accuracy of allometric scaling in food-producing and companion animals Abstract Abstract Background To optimize antimicrobial dosing in different animal species, pharmacokinetic information is necessary. Du... |
PMC7072124 | core_pubmed_pmc | Astroglial Connexin 43 Deficiency Protects against LPS-Induced Neuroinflammation: A TSPO Brain µPET Study with [ 18 F]FEPPA | Astroglial Connexin 43 Deficiency Protects against LPS-Induced Neuroinflammation: A TSPO Brain µPET Study with [ 18 F]FEPPA Abstract Astroglial connexin 43 (Cx43) has been recognized as a crucial immunoregulating factor in the brain. Its inactivation leads to a continuous immune recruitment, cytokine expression modific... |
PMC9111027 | core_pubmed_pmc | PK/PD modeling links accelerated resolution of COVID‐19‐related clinical symptoms to SARS‐CoV‐2 viral load reduction in patients following treatment with Bamlanivimab alone or Bamlanivimab and Etesevimab together | PK/PD modeling links accelerated resolution of COVID‐19‐related clinical symptoms to SARS‐CoV‐2 viral load reduction in patients following treatment with Bamlanivimab alone or Bamlanivimab and Etesevimab together Abstract Abstract The relationship between severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) vir... |
PMC12122640 | core_pubmed_pmc | Off-label drugs in laryngology– what should the doctor and the patient know about such therapies? A consensus statement of the European Laryngological Society | Off-label drugs in laryngology– what should the doctor and the patient know about such therapies? A consensus statement of the European Laryngological Society Abstract Abstract Purpose Off-label drugs are being used in laryngology. Prescribing of a medicinal product is a decision taken within the relationship between a... |
PMC3124690 | core_pubmed_pmc | Computer aided screening of inhibitors to 5-α reductase type 2 for prostate cancer | Computer aided screening of inhibitors to 5-α reductase type 2 for prostate cancer Abstract Abstract Traditionally, drugs are discovered by testing compounds synthesized in time consuming multi-step processes against a battery of invivo biological screens. Promising compounds are then further studied in development, wh... |
PMC12559310 | core_pubmed_pmc | Tumor-targeted top1 inhibitor delivery with optimized parp inhibition in advanced solid tumors: a phase i trial of gapped scheduling | Tumor-targeted top1 inhibitor delivery with optimized parp inhibition in advanced solid tumors: a phase i trial of gapped scheduling Abstract Abstract Despite mechanistic rationale for combining PARP inhibitors with topoisomerase I inhibitors, clinical use has been hindered by dose-limiting toxicities. We hypothesized ... |
PMC5872632 | core_pubmed_pmc | In Vivo Study on Site of Action of Sinapine Thiocyanate following Acupoint Herbal Patching | In Vivo Study on Site of Action of Sinapine Thiocyanate following Acupoint Herbal Patching Abstract Objective To investigate the site of action of sinapine thiocyanate (ST), following acupoint herbal patching (AHP). Methods Twenty Wistar rats were randomized into five groups (groups A, B, C, D, and E), and all groups r... |
PMC9563381 | core_pubmed_pmc | Magnesium sulfate pharmacokinetics after intramuscular dosing in women with preeclampsia | Magnesium sulfate pharmacokinetics after intramuscular dosing in women with preeclampsia Abstract Abstract BACKGROUND Current intramuscular magnesium dosing regimens in low and middle-income countries are based on indirect absorption parameters to inform pharmacokinetic and pharmacodynamic response. OBJECTIVE To determ... |
PMC10610490 | core_pubmed_pmc | The Impact of Inflammation on the In Vivo Activity of the Renal Transporters OAT1/3 in Pregnant Women Diagnosed with Acute Pyelonephritis | The Impact of Inflammation on the In Vivo Activity of the Renal Transporters OAT1/3 in Pregnant Women Diagnosed with Acute Pyelonephritis Abstract Inflammation can regulate hepatic drug metabolism enzymes and transporters. The impact of inflammation on renal drug transporters remains to be elucidated. We aimed to quant... |
PMC8151265 | core_pubmed_pmc | Drug Safety in Translational Paediatric Research: Practical Points to Consider for Paediatric Safety Profiling and Protocol Development: A Scoping Review | Drug Safety in Translational Paediatric Research: Practical Points to Consider for Paediatric Safety Profiling and Protocol Development: A Scoping Review Abstract Translational paediatric drug development includes the exchange between basic, clinical and population-based research to improve the health of children. This... |
PMC3975355 | core_pubmed_pmc | Interactive Association of Drugs Binding to Human Serum Albumin | Interactive Association of Drugs Binding to Human Serum Albumin Abstract Abstract Human serum albumin (HSA) is an abundant plasma protein, which attracts great interest in the pharmaceutical industry since it can bind a remarkable variety of drugs impacting their delivery and efficacy and ultimately altering the drug’s... |
PMC12767490 | core_pubmed_pmc | AI-driven de novo design of BRAF inhibitors with enhanced binding affinity and optimized drug-likeness | AI-driven de novo design of BRAF inhibitors with enhanced binding affinity and optimized drug-likeness Abstract Abstract Background Traditional drug discovery methods, such as high-throughput screening (HTS), are often inefficient and costly, especially in complex areas like oncology. The BRAF V600E mutation is a valid... |
PMC10404595 | core_pubmed_pmc | Preclinical Evaluation of a Protein-Based Nanoscale Contrast Agent for MR Angiography at an Ultralow Dose | Preclinical Evaluation of a Protein-Based Nanoscale Contrast Agent for MR Angiography at an Ultralow Dose Abstract Abstract Purpose BSA-biomineralized Gd nanoparticles (Gd@BSA NPs) have been recognized as promising nanoscale MR contrast agents. The aim of this study was to carry out a preclinical evaluation of these NP... |
PMC4173069 | core_pubmed_pmc | Characterizing plasma albumin concentration changes in TB/HIV patients on anti retroviral and anti –tuberculosis therapy | Characterizing plasma albumin concentration changes in TB/HIV patients on anti retroviral and anti –tuberculosis therapy Abstract Purpose Plasma albumin, a biomarker for hepatic function, is reported to correspondingly decrease in concentration as disease severity increases in chronic infections including HIV and TB. O... |
PMC12073438 | core_pubmed_pmc | Stereoselectivity of In Vivo Processes and Bioactivity of Farrerol Enantiomers | Stereoselectivity of In Vivo Processes and Bioactivity of Farrerol Enantiomers Abstract Abstract Farrerol, a bioactive compound found in Folium Rhododendri daurici, demonstrates various biological and pharmacological effects. Nevertheless, the stereoselectivity of in vivo processes and bioactivity between its enantiome... |
PMC5694427 | core_pubmed_pmc | A Randomized Multiple Dose Pharmacokinetic Study of a Novel PDE10A Inhibitor TAK-063 in Subjects with Stable Schizophrenia and Japanese Subjects and Modeling of Exposure Relationships to Adverse Events | A Randomized Multiple Dose Pharmacokinetic Study of a Novel PDE10A Inhibitor TAK-063 in Subjects with Stable Schizophrenia and Japanese Subjects and Modeling of Exposure Relationships to Adverse Events Abstract Background Phosphodiesterase 10A (PDE10A) is selectively expressed in medium spiny neurons of the striatum. T... |
PMC8840493 | core_pubmed_pmc | Plasma Bead Entrapped Liposomes as a Potential Drug Delivery System to Combat Fungal Infections | Plasma Bead Entrapped Liposomes as a Potential Drug Delivery System to Combat Fungal Infections Abstract Fibrin-based systems offer promises in drug and gene delivery as well as tissue engineering. We established earlier a fibrin-based plasma beads (PB) system as an efficient carrier of drugs and antigens. In the prese... |
PMC10298183 | core_pubmed_pmc | Transdermal Detection of MB-102 and Correlation to Meropenem Pharmacokinetics During Continuous Renal Replacement Therapy: In Vivo Results | Transdermal Detection of MB-102 and Correlation to Meropenem Pharmacokinetics During Continuous Renal Replacement Therapy: In Vivo Results Abstract Critically ill patients undergoing continuous renal replacement therapy (CRRT) have medical conditions requiring extensive pharmacotherapy. Continuous renal replacement the... |
PMC8742633 | core_pubmed_pmc | Evaluation of the safety, tolerability, and pharmacokinetics of RO7049389 in healthy Chinese volunteers | Evaluation of the safety, tolerability, and pharmacokinetics of RO7049389 in healthy Chinese volunteers Abstract Abstract The objectives of this phase I study are to assess the safety, tolerability, and pharmacokinetics (PKs) of RO7049389 in healthy Chinese volunteers (HVs) and evaluate potential ethnic differences in ... |
PMC4515672 | core_pubmed_pmc | Manganese-Induced Parkinsonism and Parkinson’s Disease: Shared and Distinguishable Features | Manganese-Induced Parkinsonism and Parkinson’s Disease: Shared and Distinguishable Features Abstract Abstract Manganese (Mn) is an essential trace element necessary for physiological processes that support development, growth and neuronal function. Secondary to elevated exposure or decreased excretion, Mn accumulates i... |
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