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PMC5020538
core_pubmed_pmc
A randomized controlled study of 5 and 10 days treatment with phenoxymethylpenicillin for pharyngotonsillitis caused by streptococcus group A – a protocol study
A randomized controlled study of 5 and 10 days treatment with phenoxymethylpenicillin for pharyngotonsillitis caused by streptococcus group A – a protocol study Abstract Abstract Background In 2014 the Swedish government assigned to The Public Health Agency of Sweden to conduct studies to evaluate optimal use of existi...
PMC12127903
core_pubmed_pmc
First-in-Human Study to Evaluate the Safety and Efficacy of Anti-GDF15 Antibody AZD8853 in Patients with Advanced/Metastatic Solid Tumors
First-in-Human Study to Evaluate the Safety and Efficacy of Anti-GDF15 Antibody AZD8853 in Patients with Advanced/Metastatic Solid Tumors Abstract Abstract Purpose: Growth and differentiation factor 15 (GDF15) is overexpressed in multiple solid tumors and is thought to exert immunosuppressive effects in the tumor micro...
PMC11875313
core_pubmed_pmc
Rational Design of Safer Inorganic Nanoparticles via Mechanistic Modeling-informed Machine Learning
Rational Design of Safer Inorganic Nanoparticles via Mechanistic Modeling-informed Machine Learning Abstract The safety of inorganic nanoparticles (NPs) remains a critical challenge for their clinical translation. To address this, we developed a machine-learning (ML) framework that predicts NP toxicity both in vitro an...
PMC5574663
core_pubmed_pmc
Nanomedicinal products: a survey on specific toxicity and side effects
Nanomedicinal products: a survey on specific toxicity and side effects Abstract Abstract Due to their specific properties and pharmacokinetics, nanomedicinal products (NMPs) may present different toxicity and side effects compared to non-nanoformulated, conventional medicines. To facilitate the safety assessment of NMP...
PMC8674003
core_pubmed_pmc
Assessing the predictive performance of population pharmacokinetic models for intravenous polymyxin B in critically ill patients
Assessing the predictive performance of population pharmacokinetic models for intravenous polymyxin B in critically ill patients Abstract Abstract Polymyxin B (PMB) has reemerged as a last‐line therapy for infections caused by multidrug‐resistant gram‐negative pathogens, but dosing is challenging because of its narrow ...
PMC3162150
core_pubmed_pmc
Effect of ketoconazole-mediated CYP3A4 inhibition on clinical pharmacokinetics of panobinostat (LBH589), an orally active histone deacetylase inhibitor
Effect of ketoconazole-mediated CYP3A4 inhibition on clinical pharmacokinetics of panobinostat (LBH589), an orally active histone deacetylase inhibitor Abstract Purpose Panobinostat is partly metabolized by CYP3A4 in vitro. This study evaluated the effect of a potent CYP3A inhibitor, ketoconazole, on the pharmacokineti...
PMC9301121
core_pubmed_pmc
CYP2A6 and GABRA2 Gene Polymorphisms are Associated With Dexmedetomidine Drug Response
CYP2A6 and GABRA2 Gene Polymorphisms are Associated With Dexmedetomidine Drug Response Abstract Abstract Background: Dexmedetomidine is a commonly used clinical sedative; however, the drug response varies among individuals. Thus, the purpose of this study was to explore the association between dexmedetomidine response ...
PMC11597305
core_pubmed_pmc
Manipulation of Lipid Nanocapsules as an Efficient Intranasal Platform for Brain Deposition of Clozapine as an Antipsychotic Drug
Manipulation of Lipid Nanocapsules as an Efficient Intranasal Platform for Brain Deposition of Clozapine as an Antipsychotic Drug Abstract Abstract Background/objectives: The blood–brain barrier (BBB) significantly limits the treatment of central nervous system disorders, such as schizophrenia, by restricting drug deli...
PMC12835540
core_pubmed_pmc
In silico identification of bilobetin and ginsenoside as dual CK2 and ULK2 inhibitors targeting triple-negative breast cancer
In silico identification of bilobetin and ginsenoside as dual CK2 and ULK2 inhibitors targeting triple-negative breast cancer Abstract Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer characterized by the absence of hormone receptors and HER2 amplification, which limits the effectiveness o...
PMC12618229
core_pubmed_pmc
Budigalimab, an anti-PD-1 inhibitor, for people living with HIV-1: a randomized, placebo-controlled phase 1b study
Budigalimab, an anti-PD-1 inhibitor, for people living with HIV-1: a randomized, placebo-controlled phase 1b study Abstract Abstract Chronic human immunodeficiency virus type 1 (HIV-1) disease results in immune exhaustion and dampened T cell responses, and programmed cell death 1 (PD-1) inhibitors offer a potential app...
PMC8008381
core_pubmed_pmc
In Vivo Functional Effects of CYP2C9 M1L, a Novel and Common Variant in the Yup’ik Alaska Native Population
In Vivo Functional Effects of CYP2C9 M1L, a Novel and Common Variant in the Yup’ik Alaska Native Population Abstract Abstract Alaska Native people are under-represented in genetic research but have unique gene variation that may critically impact their response to pharmacotherapy. Full resequencing of CYP2C9 in a cross...
PMC9031453
core_pubmed_pmc
The Intake of Coffee Increases the Absorption of Aspirin in Mice by Modifying Gut Microbiome
The Intake of Coffee Increases the Absorption of Aspirin in Mice by Modifying Gut Microbiome Abstract Abstract The absorption of orally administered aspirin into the blood was affected by gastrointestinal environmental factors such as gut pH, digestive enzymes, and microbiota. The intake of coffee affects the pharmacol...
PMC5352798
core_pubmed_pmc
Phase I study of Nivolumab, an anti-PD-1 antibody, in patients with malignant solid tumors
Phase I study of Nivolumab, an anti-PD-1 antibody, in patients with malignant solid tumors Abstract Summary Background This study evaluated the safety, tolerability, pharmacokinetics, immunogenicity and antitumor activity of single and multiple doses of nivolumab in Japanese patients with malignant solid tumors. Subjec...
PMC12943953
core_pubmed_pmc
The Potential Role of Therapeutic Drug Monitoring for Safe and Effective Anti-Infective Therapy with Manipulated Dosage Forms
The Potential Role of Therapeutic Drug Monitoring for Safe and Effective Anti-Infective Therapy with Manipulated Dosage Forms Abstract Background: Therapeutic drug monitoring (TDM) is essential for ensuring safe, effective, and individualized anti-infective therapy, particularly in patients with complex clinical needs....
PMC7496774
core_pubmed_pmc
The pharmacokinetics, efficacy, and safety of a novel selective‐dose cannabis inhaler in patients with chronic pain: A randomized, double‐blinded, placebo‐controlled trial
The pharmacokinetics, efficacy, and safety of a novel selective‐dose cannabis inhaler in patients with chronic pain: A randomized, double‐blinded, placebo‐controlled trial Abstract Abstract Background Precise cannabis treatment dosing remains a major challenge, leading to physicians’ reluctance to prescribe medical can...
PMC7153617
core_pubmed_pmc
Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods
Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods Abstract Due the implementation of nanotechnologies in the pharmaceutical industry over the last few decades, new type of cutting-edge formulations—nanopharmaceutics—have been proposed. These comprise pharmaceutical products at the...
PMC3986910
core_pubmed_pmc
Visualization of angiogenesis during cancer development in the polyoma middle T breast cancer model: molecular imaging with ( R )-[ 11 C]PAQ
Visualization of angiogenesis during cancer development in the polyoma middle T breast cancer model: molecular imaging with ( R )-[ 11 C]PAQ Abstract Background Vascular endothelial growth factor receptor 2 (VEGFR2) is a crucial mediator of tumour angiogenesis. High expression levels of the receptor have been correlate...
PMC8978631
core_pubmed_pmc
Combined Effect of CYP2C19 Genetic Polymorphisms and C-Reactive Protein on Voriconazole Exposure and Dosing in Immunocompromised Children
Combined Effect of CYP2C19 Genetic Polymorphisms and C-Reactive Protein on Voriconazole Exposure and Dosing in Immunocompromised Children Abstract Abstract Background Pediatric patients have significant interindividual variability in voriconazole exposure. The aim of the study was to identify factors associated with vo...
PMC6821771
core_pubmed_pmc
Evaluation of the dose-related concentration approach in therapeutic drug monitoring of diuretics and β-blockers – drug classes with low adherence in antihypertensive therapy
Evaluation of the dose-related concentration approach in therapeutic drug monitoring of diuretics and β-blockers – drug classes with low adherence in antihypertensive therapy Abstract Detection of antihypertensive drugs in biological samples is an important tool to assess the adherence of hypertensive patients. Urine a...
PMC10386950
core_pubmed_pmc
The Activity of Members of the UDP-Glucuronosyltransferase Subfamilies UGT1A and UGT2B is Impaired in Patients with Liver Cirrhosis
The Activity of Members of the UDP-Glucuronosyltransferase Subfamilies UGT1A and UGT2B is Impaired in Patients with Liver Cirrhosis Abstract Abstract Background and Objective The impact of liver cirrhosis on the activity of UDP-glucuronosyltransferases (UGTs) is currently not well characterized. We investigated the glu...
PMC10926053
core_pubmed_pmc
Clinical pharmacokinetics of atropine oral gel formulation in healthy volunteers
Clinical pharmacokinetics of atropine oral gel formulation in healthy volunteers Abstract Abstract Sialorrhea or drooling is a common problem in children and adults with neurodevelopmental disorders. It can negatively impact the quality of life due to its physical and psychological manifestations. Providers commonly pr...
PMC5909632
core_pubmed_pmc
Pharmacodynamics and cellular accumulation of amphotericin B and miltefosine in Leishmania donovani -infected primary macrophages
Pharmacodynamics and cellular accumulation of amphotericin B and miltefosine in Leishmania donovani -infected primary macrophages Abstract Abstract Objectives We examined the in vitro pharmacodynamics and cellular accumulation of the standard anti-leishmanial drugs amphotericin B and miltefosine in intracellular Leishm...
PMC10454446
core_pubmed_pmc
Antimicrobial Peptides Demonstrate Activity against Resistant Bacterial Pathogens
Antimicrobial Peptides Demonstrate Activity against Resistant Bacterial Pathogens Abstract The antimicrobial resistance crisis is an ongoing major threat to public health safety. Low- and middle-income countries are particularly susceptible to higher fatality rates and the economic impact of antimicrobial resistance (A...
PMC11255104
core_pubmed_pmc
LC-MS/MS-based chemical profiling of water extracts of Moringa oleifera leaves and pharmacokinetics of their major constituents in rat plasma
LC-MS/MS-based chemical profiling of water extracts of Moringa oleifera leaves and pharmacokinetics of their major constituents in rat plasma Abstract Abstract Moringa oleifera leaves (MOL) are native to India and have high biological activities. To better understand the basic pharmacodynamic materials, the chemical co...
PMC7989531
core_pubmed_pmc
Single and Repeated Intrapleural Ropivacaine Administration: A Plasma Concentration and Pharmacodynamics Study
Single and Repeated Intrapleural Ropivacaine Administration: A Plasma Concentration and Pharmacodynamics Study Abstract Background Intrapleural analgesia has been increasingly recommended for postoperative analgesia after thoracic surgery. However, the analgesic effect provided by a single intrapleural administration i...
PMC7367645
core_pubmed_pmc
Sorafenib and everolimus in patients with advanced solid tumors and KRAS‐mutated NSCLC: A phase I trial with early pharmacodynamic FDG‐PET assessment
Sorafenib and everolimus in patients with advanced solid tumors and KRAS‐mutated NSCLC: A phase I trial with early pharmacodynamic FDG‐PET assessment Abstract Abstract Background Treatment of patients with solid tumors and KRAS mutations remains disappointing. One option is the combined inhibition of pathways involved ...
PMC7158209
core_pubmed_pmc
Integration of Omics Data Sources to Inform Mechanistic Modeling of Immune‐Oncology Therapies: A Tutorial for Clinical Pharmacologists
Integration of Omics Data Sources to Inform Mechanistic Modeling of Immune‐Oncology Therapies: A Tutorial for Clinical Pharmacologists Abstract Abstract Application of contemporary molecular biology techniques to clinical samples in oncology resulted in the accumulation of unprecedented experimental data. These “omics”...
PMC11695271
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Cannabidiol, Delta‐9‐Tetrahydrocannabinol, and Their Metabolites in Healthy Adults After Administration by Multiple Routes
Physiologically Based Pharmacokinetic Modeling of Cannabidiol, Delta‐9‐Tetrahydrocannabinol, and Their Metabolites in Healthy Adults After Administration by Multiple Routes Abstract ABSTRACT The two most extensively studied cannabinoids, cannabidiol (CBD) and delta‐9‐tetrahydrocannabinol (THC), are used for myriad cond...
PMC11458340
core_pubmed_pmc
Exploration of pharmacokinetic differences between East Asians and Caucasians: insights from pharmacokinetic studies in healthy subjects
Exploration of pharmacokinetic differences between East Asians and Caucasians: insights from pharmacokinetic studies in healthy subjects Abstract Interethnic differences in the pharmacokinetics of drugs result from a complex interplay of environmental, genetic, and demographic factors. Identifying ethnic differences in...
PMC8449774
core_pubmed_pmc
A phase I study of combined trabectedin and pegylated liposomal doxorubicin therapy for advanced relapsed ovarian cancer
A phase I study of combined trabectedin and pegylated liposomal doxorubicin therapy for advanced relapsed ovarian cancer Abstract Background Advanced relapsed ovarian cancer has a poor prognosis, and treatment options are limited. Methods This phase I trial investigated the dosage, safety, pharmacokinetics and efficacy...
PMC6225135
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Properties of Rosmarinic Acid in Rat Cholestatic Liver Injury
Pharmacokinetic and Pharmacodynamic Properties of Rosmarinic Acid in Rat Cholestatic Liver Injury Abstract The objective of this study was to evaluate the hepatoprotective and metabolic effects of rosmarinic acid (RA) in rats. RA [100 mg/kg body weight (BW)] was intragastrically (i.g.) administered to Sprague-Dawley (S...
PMC8003731
core_pubmed_pmc
Comparison of Coated and Immobilized Chiral Stationary Phases Based on Amylose tris-[( S )-α-Methylbenzylcarbamate] for the HPLC Enantiomer Separation of α-Lipoic Acid and Its Reduced Form
Comparison of Coated and Immobilized Chiral Stationary Phases Based on Amylose tris-[( S )-α-Methylbenzylcarbamate] for the HPLC Enantiomer Separation of α-Lipoic Acid and Its Reduced Form Abstract Abstract The couple of chiral sulfur compounds α-lipoic acid (ALA)/α-dihydrolipoic acid (DHALA) has attracted considerable...
PMC6719325
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Analysis of GLPG1690, an Autotaxin Inhibitor, in Healthy Volunteers and Patients with Idiopathic Pulmonary Fibrosis
Population Pharmacokinetic and Pharmacodynamic Analysis of GLPG1690, an Autotaxin Inhibitor, in Healthy Volunteers and Patients with Idiopathic Pulmonary Fibrosis Abstract Abstract Background and Objectives GLPG1690 is an autotaxin inhibitor in development for the treatment of idiopathic pulmonary fibrosis. Several pub...
PMC3202762
core_pubmed_pmc
Cumulative clinical experience from over a decade of use of levofloxacin in community-acquired pneumonia: critical appraisal and role in therapy
Cumulative clinical experience from over a decade of use of levofloxacin in community-acquired pneumonia: critical appraisal and role in therapy Abstract Abstract Levofloxacin is the synthetic L -isomer of the racemic fluoroquinolone, ofloxacin. It interferes with critical processes in the bacterial cell such as DNA re...
PMC2892437
core_pubmed_pmc
Development and application of a biomarker assay for determining the pharmacodynamic activity of an antagonist candidate biotherapeutic antibody to IL21R in whole blood
Development and application of a biomarker assay for determining the pharmacodynamic activity of an antagonist candidate biotherapeutic antibody to IL21R in whole blood Abstract Background In preparation for potential clinical development of Ab-01, an antagonistic antibody directed against the IL21R, studies were under...
PMC5995255
core_pubmed_pmc
CD44 positive and sorafenib insensitive hepatocellular carcinomas respond to the ATP-competitive mTOR inhibitor INK128
CD44 positive and sorafenib insensitive hepatocellular carcinomas respond to the ATP-competitive mTOR inhibitor INK128 Abstract The mTOR pathway is activated in about 50% of patients with hepatocellular carcinoma (HCC). In an effort to identify new pathways and compounds to treat advanced HCC, we considered the ATP-com...
PMC12796777
core_pubmed_pmc
Pharmacokinetics of Ampicillin Trihydrate in Plasma, Interstitial, and Peritoneal Fluid Following Intraperitoneal or Intramuscular Administration in Steers at the Beginning of a Standing Flank Laparotomy
Pharmacokinetics of Ampicillin Trihydrate in Plasma, Interstitial, and Peritoneal Fluid Following Intraperitoneal or Intramuscular Administration in Steers at the Beginning of a Standing Flank Laparotomy Abstract ABSTRACT Prophylactic and perioperative use of antibiotics is common prior to abdominal surgery in cattle f...
PMC5853285
core_pubmed_pmc
Necessity of Bumped Kinase Inhibitor Gastrointestinal Exposure in Treating Cryptosporidium Infection
Necessity of Bumped Kinase Inhibitor Gastrointestinal Exposure in Treating Cryptosporidium Infection Abstract Abstract There is a substantial need for novel therapeutics to combat the widespread impact caused by Crytosporidium infection. However, there is a lack of knowledge as to which drug pharmacokinetic (PK) charac...
PMC11733549
core_pubmed_pmc
A Comprehensive Review of Naringenin, a Promising Phytochemical with Therapeutic Potential
A Comprehensive Review of Naringenin, a Promising Phytochemical with Therapeutic Potential Abstract Abstract Disorders, including cancer, metabolic disorders, and neurodegenerative diseases, can threaten human health; therefore, disease prevention is essential. Naringenin, a phytochemical with low toxicity, has been us...
PMC4056781
core_pubmed_pmc
Optimal dosing of antibiotics in critically ill patients by using continuous/extended infusions: a systematic review and meta-analysis
Optimal dosing of antibiotics in critically ill patients by using continuous/extended infusions: a systematic review and meta-analysis Abstract Abstract Introduction The aim of this study was to determine whether using pharmacodynamic-based dosing of antimicrobials, such as extended/continuous infusions, in critically ...
PMC8302247
core_pubmed_pmc
Nivolumab exposure–response analysis for adjuvant treatment of melanoma supporting a change in posology
Nivolumab exposure–response analysis for adjuvant treatment of melanoma supporting a change in posology Abstract Abstract Nivolumab monotherapy is approved as adjuvant treatment for melanoma based on results from the pivotal CheckMate 238 trial. We present a model‐based, benefit–risk assessment of nivolumab in adjuvant...
PMC11449971
core_pubmed_pmc
Comparative pharmacokinetic evaluation of nanoparticle-based vs. conventional pharmaceuticals containing statins in attenuating dyslipidaemia
Comparative pharmacokinetic evaluation of nanoparticle-based vs. conventional pharmaceuticals containing statins in attenuating dyslipidaemia Abstract Abstract Dyslipidaemia describes the condition of abnormal lipid levels in a person’s bloodstream. Since the 1980s, statin medications have been used to treat dyslipidae...
PMC3983358
core_pubmed_pmc
64 Cu-Labeled Inhibitors of Prostate-Specific Membrane Antigen for PET Imaging of Prostate Cancer
64 Cu-Labeled Inhibitors of Prostate-Specific Membrane Antigen for PET Imaging of Prostate Cancer Abstract Abstract Prostate-specific membrane antigen (PSMA) is a well-recognized target for identification and therapy of a variety of cancers. Here we report five 64 Cu-labeled inhibitors of PSMA, [ 64 Cu] 3 – 7 , which a...
PMC8466904
core_pubmed_pmc
Antibiotics in Necrotizing Soft Tissue Infections
Antibiotics in Necrotizing Soft Tissue Infections Abstract Abstract Necrotizing soft tissue infections (NSTIs) are rare life-threatening bacterial infections characterized by an extensive necrosis of skin and subcutaneous tissues. Initial urgent management of NSTIs relies on broad-spectrum antibiotic therapy, rapid sur...
PMC10581271
core_pubmed_pmc
A protocol for an international, multicentre pharmacokinetic study for Screening Antifungal Exposure in Intensive Care Units: The SAFE-ICU study
A protocol for an international, multicentre pharmacokinetic study for Screening Antifungal Exposure in Intensive Care Units: The SAFE-ICU study Abstract Abstract Objective To describe whether contemporary dosing of antifungal drugs achieves therapeutic exposures in critically ill patients that are associated with opti...
PMC5993114
core_pubmed_pmc
A stable isotope dilution tandem mass spectrometry method of major kavalactones and its applications
A stable isotope dilution tandem mass spectrometry method of major kavalactones and its applications Abstract Abstract Kava is regaining its popularity with detailed characterizations warranted. We developed an ultraperformance liquid chromatography high-resolution tandem mass spectrometry (UPLC-MS/MS) method for major...
PMC9693517
core_pubmed_pmc
Application of Physiologically Based Pharmacokinetic Modeling to Predict Maternal Pharmacokinetics and Fetal Exposure to Oxcarbazepine
Application of Physiologically Based Pharmacokinetic Modeling to Predict Maternal Pharmacokinetics and Fetal Exposure to Oxcarbazepine Abstract Pregnancy is associated with physiological changes that may affect drug pharmacokinetics (PKs). The aim of this study was to establish a maternal–fetal physiologically based ph...
PMC11459965
core_pubmed_pmc
Serum ganciclovir drug exposure in children receiving standard ganciclovir dosing
Serum ganciclovir drug exposure in children receiving standard ganciclovir dosing Abstract ABSTRACT Intravenous ganciclovir (GCV) is used for the treatment of cytomegalovirus (CMV) infection in immunocompromised children. Although the therapeutic target for treatment is unclear, studies have shown a serum area under th...
PMC7344759
core_pubmed_pmc
A Novel Derivative of Thioridazine Shows Low Toxicity and Efficient Activity against Gram-Positive Pathogens
A Novel Derivative of Thioridazine Shows Low Toxicity and Efficient Activity against Gram-Positive Pathogens Abstract Thioridazine hydrochloride (HCl) has been suggested as a promising antimicrobial helper compound for the treatment of infections with antimicrobial-resistant bacteria. Unfortunately, the therapeutic con...
PMC4018313
core_pubmed_pmc
Combined isosorbide dinitrate and ibuprofen as a novel therapy for muscular dystrophies: evidence from Phase I studies in healthy volunteers
Combined isosorbide dinitrate and ibuprofen as a novel therapy for muscular dystrophies: evidence from Phase I studies in healthy volunteers Abstract We designed two Phase I studies that assessed healthy volunteers in order to evaluate the safety and to optimize the dosing of the combination of the drugs isosorbide din...
PMC6058490
core_pubmed_pmc
Puerarin-loaded PEG-PE micelles with enhanced anti-apoptotic effect and better pharmacokinetic profile
Puerarin-loaded PEG-PE micelles with enhanced anti-apoptotic effect and better pharmacokinetic profile Abstract Abstract Puerarin (PUE) is the most abundant isoflavonoid in kudzu root. It is widely used as a therapeutic agent for the treatment of cardiovascular diseases. However, the short elimination half-life, poor-b...
PMC4339912
core_pubmed_pmc
Antimicrobial dosing in critically ill patients with sepsis-induced acute kidney injury
Antimicrobial dosing in critically ill patients with sepsis-induced acute kidney injury Abstract Abstract Severe sepsis often leads to multiple organ dysfunction syndromes (MODS) with acute kidney injury (AKI). AKI affects approximately, 35% of Intensive Care Unit patients, and most of these are due to sepsis. Mortalit...
PMC11304744
core_pubmed_pmc
Population pharmacokinetics of rifabutin among HIV/TB co-infected children on lopinavir/ritonavir-based antiretroviral therapy
Population pharmacokinetics of rifabutin among HIV/TB co-infected children on lopinavir/ritonavir-based antiretroviral therapy Abstract ABSTRACT In adults requiring protease inhibitor (PI)-based antiretroviral therapy (ART), replacing rifampicin with rifabutin is a preferred option, but there is lack of evidence to gui...
PMC4412377
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of the Endothelin Receptor Antagonist Macitentan
Clinical Pharmacokinetics and Pharmacodynamics of the Endothelin Receptor Antagonist Macitentan Abstract Pulmonary arterial hypertension (PAH) is a progressive disease of the lung vascular system, which leads to right-sided heart failure and ultimately death if untreated. Treatments to regulate the pulmonary vascular p...
PMC3898188
core_pubmed_pmc
Comparative Bioavailability and Tolerability of a Single 2-mg Dose of 2 Repaglinide Tablet Formulations in Fasting, Healthy Chinese Male Volunteers: An Open-Label, Randomized-Sequence, 2-Period Crossover Study ☆
Comparative Bioavailability and Tolerability of a Single 2-mg Dose of 2 Repaglinide Tablet Formulations in Fasting, Healthy Chinese Male Volunteers: An Open-Label, Randomized-Sequence, 2-Period Crossover Study ☆ Abstract Background Repaglinide, an oral insulin secretagogue, was the first meglitinide analogue to be appr...
PMC9267083
core_pubmed_pmc
Efficacy and Outcomes of CYP3A5 Genotype-Based Tacrolimus Dosing Compared to Conventional Body Weight-based Dosing in Living Donor Kidney Transplant Recipients
Efficacy and Outcomes of CYP3A5 Genotype-Based Tacrolimus Dosing Compared to Conventional Body Weight-based Dosing in Living Donor Kidney Transplant Recipients Abstract Introduction: Clinical use of tacrolimus has been challenging due to its narrow therapeutic index and highly variable pharmacokinetics. In this study, ...
PMC12641124
core_pubmed_pmc
Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Pakistan: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints
Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Pakistan: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine the antibiotic susceptibility of Streptococcus pneumoniae and Haemophilus influenzae isolates from com...
PMC5608803
core_pubmed_pmc
Assessment of pharmacokinetics for microvessel proliferation by DCE-MRI for early detection of physeal bone bridge formation in an animal model
Assessment of pharmacokinetics for microvessel proliferation by DCE-MRI for early detection of physeal bone bridge formation in an animal model Abstract Objectives Bone bridge formation occurs after physeal lesions and can lead to growth arrest if not reversed. Previous investigations on the underlying mechanisms of th...
PMC8439242
core_pubmed_pmc
Pharmacokinetic study on the interaction between pachymic acid and bavachin and its potential mechanism
Pharmacokinetic study on the interaction between pachymic acid and bavachin and its potential mechanism Abstract Abstract Context Pachymic acid and bavachin are commonly used drugs in the therapy of lung cancer. Objective The co-administration of pachymic acid and bavachin was investigated to evaluate their potential d...
PMC9437282
core_pubmed_pmc
A single-dose, randomized, open-labeled, parallel-group study comparing the pharmacokinetics, pharmacodynamics and safety of leuprolide acetate microspheres 3.75 mg and Enantone ® 3.75 mg in healthy male subjects
A single-dose, randomized, open-labeled, parallel-group study comparing the pharmacokinetics, pharmacodynamics and safety of leuprolide acetate microspheres 3.75 mg and Enantone ® 3.75 mg in healthy male subjects Abstract Abstract Leuprolide acetate microspheres developed by Shanghai Livzon Pharmaceutical Co., Ltd. (T)...
PMC12254183
core_pubmed_pmc
Combined Chronic Oral Methylphenidate and Fluoxetine Decreases D2R Levels in the Caudate Putamen and Nucleus Accumbens
Combined Chronic Oral Methylphenidate and Fluoxetine Decreases D2R Levels in the Caudate Putamen and Nucleus Accumbens Abstract Abstract Methylphenidate (MP) is a commonly prescribed psychostimulant for treating Attention-Deficit/Hyperactive Disorder (ADHD). Many patients with ADHD also experience anxiety and depressio...
PMC8933683
core_pubmed_pmc
Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions ☆
Enhanced circulation longevity and pharmacodynamics of metformin from surface-modified nanostructured lipid carriers based on solidified reverse micellar solutions ☆ Abstract Abstract Metformin hydrochloride (MTH) has been associated with poor/incomplete absorption (50–60%), low bioavailability, short half-life (0.4–0....
PMC9541287
core_pubmed_pmc
Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib
Pharmacology, safety, efficacy and clinical uses of the COX‐2 inhibitor robenacoxib Abstract Abstract Robenacoxib is a veterinary‐approved non‐steroidal anti‐inflammatory drug (NSAID) of the coxib group. It possesses anti‐hyperalgesic, anti‐inflammatory and anti‐pyretic properties. Robenacoxib inhibits the cyclooxygena...
PMC6247064
core_pubmed_pmc
Dose‐finding study of the checkpoint kinase 1 inhibitor, prexasertib, in Japanese patients with advanced solid tumors
Dose‐finding study of the checkpoint kinase 1 inhibitor, prexasertib, in Japanese patients with advanced solid tumors Abstract Abstract Prexasertib is a novel inhibitor of checkpoint kinase 1. The primary objective of this study was to evaluate prexasertib tolerability in Japanese patients with advanced solid tumors. T...
PMC5859905
core_pubmed_pmc
Buprenorphine and pain treatment in pediatric patients: an update
Buprenorphine and pain treatment in pediatric patients: an update Abstract Abstract Introduction The usual management of moderate to severe pain is based on the use of opioids. Buprenorphine (BPN) is an opioid with an analgesic potency 50 times greater than that of morphine. It is widely used in various pain models and...
PMC4522830
core_pubmed_pmc
A study of pharmacokinetic interactions among co-existing ingredients in Viscum coloratum after intravenous administration of three different preparations to rats
A study of pharmacokinetic interactions among co-existing ingredients in Viscum coloratum after intravenous administration of three different preparations to rats Abstract Abstract Background: Viscum coloratum (Komar) Nakai, known as Hujisheng in china, has been widely used as a herb medicine to treat a variety of dise...
PMC7359159
core_pubmed_pmc
Evaluation of the Potential Pharmacokinetic Interactions Between Vixotrigine and an Oral Contraceptive
Evaluation of the Potential Pharmacokinetic Interactions Between Vixotrigine and an Oral Contraceptive Abstract Abstract Background and Objective Vixotrigine is a voltage- and use-dependent sodium channel blocker in development for neuropathic pain management. This study evaluated the effect of coadministration of vixo...
PMC8398570
core_pubmed_pmc
Evaluation of the Predictive Performance of Population Pharmacokinetic Models of Adalimumab in Patients with Inflammatory Bowel Disease
Evaluation of the Predictive Performance of Population Pharmacokinetic Models of Adalimumab in Patients with Inflammatory Bowel Disease Abstract Abstract Adalimumab is a monoclonal antibody used for inflammatory bowel disease. Due to its considerably variable pharmacokinetics, the loss of response and the development o...
PMC5493866
core_pubmed_pmc
Prediction of marbofloxacin dosage for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida by pharmacokinetic/pharmacodynamic modelling
Prediction of marbofloxacin dosage for the pig pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida by pharmacokinetic/pharmacodynamic modelling Abstract Abstract Background Bacterial pneumonia in pigs occurs widely and requires antimicrobial therapy. It is commonly caused by the pathogens Acti...
PMC5412702
core_pubmed_pmc
The Pharmacology of Spinal Opioids and Ziconotide for the Treatment of Non-Cancer Pain
The Pharmacology of Spinal Opioids and Ziconotide for the Treatment of Non-Cancer Pain Abstract Background Intrathecal drug delivery has undergone a revitalization following a better understanding of this delivery route and its pharmacokinetics. Driven by patient safety and outcomes, clinicians are motivated to rethink...
PMC4592530
core_pubmed_pmc
Physiologically Based Pharmacokinetic Model to Assess the Influence of Blinatumomab-Mediated Cytokine Elevations on Cytochrome P450 Enzyme Activity
Physiologically Based Pharmacokinetic Model to Assess the Influence of Blinatumomab-Mediated Cytokine Elevations on Cytochrome P450 Enzyme Activity Abstract Abstract Blinatumomab is a CD19/CD3 bispecific T-cell engager (BiTE®) antibody construct for treatment of leukemia. Transient elevation of cytokines (interleukin (...
PMC12882400
core_pubmed_pmc
Comparison of two sevoflurane formulations in low-flow anesthesia: a retrospective observational study
Comparison of two sevoflurane formulations in low-flow anesthesia: a retrospective observational study Abstract Abstract Background This study aimed to compare two different sevoflurane formulations (Sevones ® and Sevorane ® ) under low-flow anesthesia in terms of time to 1 Minimum Alveolar Concentration (MAC), agent c...
PMC8935415
core_pubmed_pmc
Alkalising agents in urinary tract infections: theoretical contraindications, interactions and synergy
Alkalising agents in urinary tract infections: theoretical contraindications, interactions and synergy Abstract Introduction: Alkalising agents have the potential to enhance the efficacy of many antimicrobial agents used in the treatment of Urinary Tract Infections; they also have the potential to cause significant pat...
PMC9454408
core_pubmed_pmc
Drug dosing in children with obesity: a narrative updated review
Drug dosing in children with obesity: a narrative updated review Abstract Abstract Childhood obesity and its associated comorbidities are highly prevalent diseases that may add to any other possible health problem commonly affecting the pediatric age. Uncertainties may arise concerning drug dosing when children with ob...
PMC7033540
core_pubmed_pmc
Enhancement of skin permeation of vitamin C using vibrating microneedles
Enhancement of skin permeation of vitamin C using vibrating microneedles Abstract This study was performed to evaluate the use of vibrating microneedles for the transdermal delivery of vitamin C. The microneedles were designed to vibrate at three levels of intensity. In vitro permeation by vitamin C was evaluated accor...
PMC4688463
core_pubmed_pmc
Equivalent Lung Dose and Systemic Exposure of Budesonide/Formoterol Combination via Easyhaler and Turbuhaler
Equivalent Lung Dose and Systemic Exposure of Budesonide/Formoterol Combination via Easyhaler and Turbuhaler Abstract Abstract Background: Easyhaler ® device-metered dry powder inhaler containing budesonide and formoterol fumarate dihydrate (hereafter formoterol) for the treatment of asthma and chronic obstructive pulm...
PMC10239301
core_pubmed_pmc
Florfenicol and Florfenicol Amine Quantification in Bull Serum and Seminal Plasma by a Single Validated UHPLC-MS/MS Method
Florfenicol and Florfenicol Amine Quantification in Bull Serum and Seminal Plasma by a Single Validated UHPLC-MS/MS Method Abstract Abstract Florfenicol is a broad-spectrum antibiotic belonging to the amphenicols class that inhibits protein synthesis by binding to bacteria's ribosomal subunits. This drug is commonly us...
PMC8561230
core_pubmed_pmc
Inter‐ethnic differences in pharmacokinetics—is there more that unites than divides?
Inter‐ethnic differences in pharmacokinetics—is there more that unites than divides? Abstract Abstract Inter‐ethnic variability in pharmacokinetics (PK) has been attributed to several factors ranging from genetic to environmental. It is not clear how current teaching in higher education (HE) reflects what published lit...
PMC11977408
core_pubmed_pmc
Safety, Pharmacokinetics, and Efficiency of JS005, a Novel Anti-interleukin-17A Monoclonal Antibody, in Healthy Chinese Adults and Patients with Moderate to Severe Psoriasis
Safety, Pharmacokinetics, and Efficiency of JS005, a Novel Anti-interleukin-17A Monoclonal Antibody, in Healthy Chinese Adults and Patients with Moderate to Severe Psoriasis Abstract JS005 is a novel anti-IL-17A monoclonal antibody. A Phase Ia study (Study 1) in healthy adults, followed by a Phase Ib/II study (Study 2)...
PMC8841431
core_pubmed_pmc
Preclinical Pharmacokinetics and Dosimetry of an 89 Zr Labelled Anti-PDL1 in an Orthotopic Lung Cancer Murine Model
Preclinical Pharmacokinetics and Dosimetry of an 89 Zr Labelled Anti-PDL1 in an Orthotopic Lung Cancer Murine Model Abstract Anti-PDL1 is a monoclonal antibody targeting the programmed death-cell ligand (PD-L1) by blocking the programmed death-cell (PD-1)/PD-L1 axis. It restores the immune system response in several tu...
PMC4735425
core_pubmed_pmc
A Humanized Clinically Calibrated Quantitative Systems Pharmacology Model for Hypokinetic Motor Symptoms in Parkinson’s Disease
A Humanized Clinically Calibrated Quantitative Systems Pharmacology Model for Hypokinetic Motor Symptoms in Parkinson’s Disease Abstract Abstract The current treatment of Parkinson’s disease with dopamine-centric approaches such as L -DOPA and dopamine agonists, although very successful, is in need of alternative treat...
PMC6645601
core_pubmed_pmc
Construction and in vivo / in vitro evaluation of a nanoporous ion-responsive targeted drug delivery system for recombinant human interferon α-2b delivery
Construction and in vivo / in vitro evaluation of a nanoporous ion-responsive targeted drug delivery system for recombinant human interferon α-2b delivery Abstract Abstract Background Like most protein macromolecular drugs, the half-life of rhIFNɑ-2b is short, with a low drug utilization rate, and the preparation and r...
PMC3920104
core_pubmed_pmc
Obstetric Pharmacokinetic Dosing Studies are Urgently Needed
Obstetric Pharmacokinetic Dosing Studies are Urgently Needed Abstract Use of pharmacotherapy during pregnancy is common and increasing. Physiologic changes during pregnancy may significantly alter the overall systemic drug exposure, necessitating dose changes. A search of PubMed for pharmacokinetic clinical trials show...
PMC2831956
core_pubmed_pmc
The Implications of Using a Physiologically Based Pharmacokinetic (PBPK) Model for Pesticide Risk Assessment
The Implications of Using a Physiologically Based Pharmacokinetic (PBPK) Model for Pesticide Risk Assessment Abstract Background A physiologically based pharmacokinetic (PBPK) model would make it possible to simulate the dynamics of chemical absorption, distribution, metabolism, and elimination (ADME) from different ro...
PMC11206399
core_pubmed_pmc
In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations
In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations Abstract Abstract This study aims to evaluate and determine the correlation between in vitro release and in vivo pharmacokinetics of two extended-release dosage forms of Cilostazol. In vitro release profiles for two dosage forms, tablet and ca...
PMC5815475
core_pubmed_pmc
High-dose amikacin for achieving serum target levels in critically ill elderly patients
High-dose amikacin for achieving serum target levels in critically ill elderly patients Abstract Abstract Introduction To achieve target concentrations, the application of higher-than-standard doses of amikacin is proposed for the treatment of sepsis due to an increase in volume of distribution and clearance, but littl...
PMC10547635
core_pubmed_pmc
SubQ-Sim: A Subcutaneous Physiologically Based Biopharmaceutics Model. Part 1: The Injection and System Parameters
SubQ-Sim: A Subcutaneous Physiologically Based Biopharmaceutics Model. Part 1: The Injection and System Parameters Abstract Purpose To construct a detailed mechanistic and physiologically based biopharmaceutics model capable of predicting 1) device-formulation-tissue interaction during the injection process and 2) bind...
PMC10534582
core_pubmed_pmc
A Pharmacokinetic Study of Sixteen Major Bioactive Components of Jinshui-Huanxian Granules in Pulmonary Fibrosis Model and Control Rats Using Orbitrap Fusion Mass Spectrometry
A Pharmacokinetic Study of Sixteen Major Bioactive Components of Jinshui-Huanxian Granules in Pulmonary Fibrosis Model and Control Rats Using Orbitrap Fusion Mass Spectrometry Abstract Abstract Jinshui-Huanxian granules (JHGs), a Chinese herbal compound prescription, have shown a therapeutic effect in reducing lung tis...
PMC12629334
core_pubmed_pmc
Preclinical pharmacology, pharmacokinetics, and pharmacodynamics of veligrotug, a full antagonist antibody to the IGF-1 receptor in development for thyroid eye disease
Preclinical pharmacology, pharmacokinetics, and pharmacodynamics of veligrotug, a full antagonist antibody to the IGF-1 receptor in development for thyroid eye disease Abstract ABSTRACT Clinical and preclinical studies have confirmed insulin-like growth factor-1 receptor (IGF-1R) antagonism can reduce the inflammation ...
PMC7238177
core_pubmed_pmc
Real Life Population Pharmacokinetics Modelling of Eight Factors VIII in Patients with Severe Haemophilia A: Is It Always Relevant to Switch to an Extended Half-Life?
Real Life Population Pharmacokinetics Modelling of Eight Factors VIII in Patients with Severe Haemophilia A: Is It Always Relevant to Switch to an Extended Half-Life? Abstract Abstract We retrospectively analysed the data files of 171 adults and 87 children/adolescents with severe haemophilia, except for 14 patients (m...
PMC8522782
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Immunogenicity of a Monoclonal Antibody (SCTA01) Targeting SARS-CoV-2 in Healthy Adults: a Randomized, Double-Blind, Placebo-Controlled, Phase I Study
Safety, Tolerability, Pharmacokinetics, and Immunogenicity of a Monoclonal Antibody (SCTA01) Targeting SARS-CoV-2 in Healthy Adults: a Randomized, Double-Blind, Placebo-Controlled, Phase I Study Abstract ABSTRACT SCTA01 is a novel monoclonal antibody with promising prophylactic and therapeutic potential for COVID-19. T...
PMC11706882
core_pubmed_pmc
Pharmacometrics-Enhanced Bayesian Borrowing for Pediatric Extrapolation – A Case Study of the DINAMO Trial
Pharmacometrics-Enhanced Bayesian Borrowing for Pediatric Extrapolation – A Case Study of the DINAMO Trial Abstract Abstract Bayesian borrowing analyses have an important role in the design and analysis of pediatric trials. This paper describes use of a prespecified Pharmacometrics Enhanced Bayesian Borrowing (PEBB) an...
PMC3820465
core_pubmed_pmc
Clinical Pharmacology in Old Persons
Clinical Pharmacology in Old Persons Abstract Abstract The epidemiological transition, with a rapid increase in the proportion in the global population aged over 65 years from 11% in 2010 to 22% in 2050 and 32% in 2100, represents a challenge for public health. More and more old persons have multimorbidities and are tr...
PMC11966721
core_pubmed_pmc
Pharmacokinetics, pharmacogenetics, and toxicity of co-administered efavirenz and isoniazid
Pharmacokinetics, pharmacogenetics, and toxicity of co-administered efavirenz and isoniazid Abstract Abstract Background CYP2B6 slow metabolisers have higher efavirenz concentrations, which are further increased by isoniazid inhibiting efavirenz’s accessory metabolic pathway. Objectives We investigated the association ...
PMC11580011
core_pubmed_pmc
Dose, exposure, and treatment regimen of intravenous immunoglobulin G in multifocal motor neuropathy
Dose, exposure, and treatment regimen of intravenous immunoglobulin G in multifocal motor neuropathy Abstract Abstract Introduction Intravenous immunoglobulin (IVIG) is the only approved treatment for multifocal motor neuropathy (MMN), a rare, chronic, immune-mediated demyelinating neuropathy. There is a significant ga...
PMC7060353
core_pubmed_pmc
Maltotriose-based probes for fluorescence and photoacoustic imaging of bacterial infections
Maltotriose-based probes for fluorescence and photoacoustic imaging of bacterial infections Abstract Abstract Currently, there are no non-invasive tools to accurately diagnose wound and surgical site infections before they become systemic or cause significant anatomical damage. Fluorescence and photoacoustic imaging ar...
PMC12399562
core_pubmed_pmc
Published population pharmacokinetic models of mycophenolate sodium: a systematic review and external evaluation in a Chinese sample of renal transplant recipients
Published population pharmacokinetic models of mycophenolate sodium: a systematic review and external evaluation in a Chinese sample of renal transplant recipients Abstract Background Immunosuppressive therapy remains the primary method for preventing rejection in renal transplant recipients. While multiple population ...
PMC10014700
core_pubmed_pmc
The impact of genetic variability in urate transporters on oxypurinol pharmacokinetics
The impact of genetic variability in urate transporters on oxypurinol pharmacokinetics Abstract Abstract The genetic determinants of the allopurinol dose‐concentration relationship have not been extensively studied. We aimed to clarify what factors, including genetic variation in urate transporters, influence oxypurino...
PMC10305115
core_pubmed_pmc
Development of a Minimalistic Physiologically Based Pharmacokinetic (mPBPK) Model for the Preclinical Development of Spectinamide Antibiotics
Development of a Minimalistic Physiologically Based Pharmacokinetic (mPBPK) Model for the Preclinical Development of Spectinamide Antibiotics Abstract Abstract Spectinamides 1599 and 1810 are lead spectinamide compounds currently under preclinical development to treat multidrug-resistant (MDR) and extensively drug-resi...
PMC6792382
core_pubmed_pmc
Using Collaborative Cross Mouse Population to Fill Data Gaps in Risk Assessment: A Case Study of Population-Based Analysis of Toxicokinetics and Kidney Toxicodynamics of Tetrachloroethylene
Using Collaborative Cross Mouse Population to Fill Data Gaps in Risk Assessment: A Case Study of Population-Based Analysis of Toxicokinetics and Kidney Toxicodynamics of Tetrachloroethylene Abstract Background: Interindividual variability in susceptibility remains poorly characterized for environmental chemicals such a...