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PMC6244714 | core_pubmed_pmc | Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects | Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects Abstract Abstract Background and Objectives Roxadustat is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of anemia in chronic kidney disease. This study in... |
PMC12340365 | core_pubmed_pmc | Propofol: A Medication That Changed Pediatric Anesthesia Practice | Propofol: A Medication That Changed Pediatric Anesthesia Practice Abstract ABSTRACT The introduction of propofol changed our understanding of pediatric anesthesia pharmacology, research approaches for intravenous drug study, and led to infusion pump development for the maintenance phase of anesthesia. The story of prop... |
PMC4006848 | core_pubmed_pmc | Probable fatal drug interaction between intravenous fenretinide, ceftriaxone, and acetaminophen: a case report from a New Approaches to Neuroblastoma (NANT) Phase I study | Probable fatal drug interaction between intravenous fenretinide, ceftriaxone, and acetaminophen: a case report from a New Approaches to Neuroblastoma (NANT) Phase I study Abstract Abstract Background Patients with relapsed/refractory stage 4 high-risk neuroblastoma were enrolled on a phase I study (NANT2004-03) of intr... |
PMC9608995 | core_pubmed_pmc | Tunable Polymeric Mixed Micellar Nanoassemblies of Lutrol F127/Gelucire 44/14 for Oral Delivery of Praziquantel: A Promising Nanovector against Hymenolepis nana in Experimentally-Infected Rats | Tunable Polymeric Mixed Micellar Nanoassemblies of Lutrol F127/Gelucire 44/14 for Oral Delivery of Praziquantel: A Promising Nanovector against Hymenolepis nana in Experimentally-Infected Rats Abstract Hymenolepiasis represents a parasitic infection of common prevalence in pediatrics with intimidating impacts, particul... |
PMC11652817 | core_pubmed_pmc | A User‐Driven Framework for Dose Selection in Pregnancy: Proof of Concept for Sertraline | A User‐Driven Framework for Dose Selection in Pregnancy: Proof of Concept for Sertraline Abstract Despite growing knowledge of pregnancy‐induced changes in physiology that may alter maternal and fetal pharmacokinetics, evidence‐based antenatal doses are lacking for most drugs. Pharmacokinetic modeling and expanding cli... |
PMC9502491 | core_pubmed_pmc | New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen | New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen Abstract Abstract Nebivolol (NEB) is a highly selective β1 receptor antagonist with a distinct pharmacological profile. This drug is approved for the treatment of hypertension in the US, and hypertension and heart failure in Eur... |
PMC11531813 | core_pubmed_pmc | Population pharmacokinetics of unbound cefazolin in infected hospitalized patients requiring intermittent high-flux haemodialysis: can a three-times-weekly post-dialysis dosing regimen provide optimal treatment? | Population pharmacokinetics of unbound cefazolin in infected hospitalized patients requiring intermittent high-flux haemodialysis: can a three-times-weekly post-dialysis dosing regimen provide optimal treatment? Abstract Abstract Objectives To describe the population pharmacokinetics of cefazolin in infected hospitaliz... |
PMC11850462 | core_pubmed_pmc | A Maximum-Use Trial of Ruxolitinib Cream in Children Aged 2–11 Years with Moderate to Severe Atopic Dermatitis | A Maximum-Use Trial of Ruxolitinib Cream in Children Aged 2–11 Years with Moderate to Severe Atopic Dermatitis Abstract Abstract Background Ruxolitinib cream has demonstrated anti-inflammatory and antipruritic activity and was well tolerated in a phase 3 study in patients aged 2–11 years with mild to moderate atopic de... |
PMC11588095 | core_pubmed_pmc | The limitation of lipidation: Conversion of semaglutide from once-weekly to once-monthly dosing | The limitation of lipidation: Conversion of semaglutide from once-weekly to once-monthly dosing Abstract The objective of this work was to develop a long-acting form of the lipidated peptide semaglutide that can be administered to humans once-monthly. Semaglutide was attached to hydrogel microspheres by a cleavable lin... |
PMC5604554 | core_pubmed_pmc | Pharmacokinetic and safety evaluation of MB12066, an NQO1 substrate | Pharmacokinetic and safety evaluation of MB12066, an NQO1 substrate Abstract Abstract Objective This study evaluated the pharmacokinetics (PKs) and safety of a newly developed β-lapachone (MB12066) tablet, a natural NAD(P)H:quinone oxidoreductase 1 (NQO1) substrate, in healthy male volunteers. Methods In a randomized, ... |
PMC11094421 | core_pubmed_pmc | First-in-Human Study of the Ataxia Telangiectasia and Rad3-Related (ATR) Inhibitor Tuvusertib (M1774) as Monotherapy in Patients with Solid Tumors | First-in-Human Study of the Ataxia Telangiectasia and Rad3-Related (ATR) Inhibitor Tuvusertib (M1774) as Monotherapy in Patients with Solid Tumors Abstract Abstract Purpose: Tuvusertib (M1774) is a potent, selective, orally administered ataxia telangiectasia and Rad3-related (ATR) protein kinase inhibitor. This first-i... |
PMC8540953 | core_pubmed_pmc | Preparation and Pharmacokinetic Characterization of an Anti-Virulence Compound Nanosuspensions | Preparation and Pharmacokinetic Characterization of an Anti-Virulence Compound Nanosuspensions Abstract Abstract Antibiotic resistance has become a worldwide public health threat due to the rapid evolution and spread of antibiotic-resistant bacteria. CCG-211790 is a novel anti-virulence compound that does not kill bact... |
PMC12508949 | core_pubmed_pmc | Evaluation of the Pharmacokinetic Interactions of Maytenus ilicifolia Mart. ex Reiss Extracts on Drug Intestinal Permeability and Hepatic Metabolism | Evaluation of the Pharmacokinetic Interactions of Maytenus ilicifolia Mart. ex Reiss Extracts on Drug Intestinal Permeability and Hepatic Metabolism Abstract Maytenus ilicifolia Mart. ex Reiss is a plant native to South America, popularly used in the treatment of gastric disorders. The increase in the consumption of he... |
PMC7243819 | core_pubmed_pmc | A Polyclonal Immune Function Assay Allows Dose-Dependent Characterization of Immunosuppressive Drug Effects but Has Limited Clinical Utility for Predicting Infection on an Individual Basis | A Polyclonal Immune Function Assay Allows Dose-Dependent Characterization of Immunosuppressive Drug Effects but Has Limited Clinical Utility for Predicting Infection on an Individual Basis Abstract Abstract Dosage of immunosuppressive drugs after transplantation critically determines rejection and infection episodes. I... |
PMC12257272 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Cutoff Values for Doxycycline in Pigs to Support the Establishment of Clinical Breakpoints for Antimicrobial Susceptibility Testing | Pharmacokinetic–Pharmacodynamic Cutoff Values for Doxycycline in Pigs to Support the Establishment of Clinical Breakpoints for Antimicrobial Susceptibility Testing Abstract ABSTRACT This meta‐analysis provides a population model of doxycycline (DOXY) disposition in pigs for computation of PK/PD cutoff values correspond... |
PMC8614407 | core_pubmed_pmc | Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Integration of Enrofloxacin Following Single Oral Administration of Different Doses in Brown Trout ( Salmo trutta ) | Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Integration of Enrofloxacin Following Single Oral Administration of Different Doses in Brown Trout ( Salmo trutta ) Abstract Abstract Simple Summary The pharmacokinetic/pharmacodynamic studies report the use of enrofloxacin at higher doses than 10 mg/kg in fish. Phar... |
PMC5972636 | core_pubmed_pmc | Guidelines for the treatment of severe acute malnutrition: a systematic review of the evidence for antimicrobial therapy | Guidelines for the treatment of severe acute malnutrition: a systematic review of the evidence for antimicrobial therapy Abstract Abstract Background Severe acute malnutrition (SAM) affects nearly 20 million children worldwide and is responsible for up to 1 million deaths per year in children under the age of 5 years. ... |
PMC5434277 | core_pubmed_pmc | New Modified UPLC/Tandem Mass Spectrometry Method for Determination of Risperidone and Its Active Metabolite 9-Hydroxyrisperidone in Plasma: Application to Dose-Dependent Pharmacokinetic Study in Sprague-Dawley Rats | New Modified UPLC/Tandem Mass Spectrometry Method for Determination of Risperidone and Its Active Metabolite 9-Hydroxyrisperidone in Plasma: Application to Dose-Dependent Pharmacokinetic Study in Sprague-Dawley Rats Abstract Abstract Sensitive and specific liquid-chromatography tandem mass spectrometry (UPLC-MS/MS) ass... |
PMC6084327 | core_pubmed_pmc | How to optimise drug study design: pharmacokinetics and pharmacodynamics studies introduced to paediatricians | How to optimise drug study design: pharmacokinetics and pharmacodynamics studies introduced to paediatricians Abstract Abstract Objectives In children, there is often lack of sufficient information concerning the pharmacokinetics (PK) and pharmacodynamics (PD) of a study drug to support dose selection and effective eva... |
PMC6462750 | core_pubmed_pmc | Favorable pharmacokinetics in hemophilia B for nonacog beta pegol versus recombinant factor IX‐Fc fusion protein: A randomized trial | Favorable pharmacokinetics in hemophilia B for nonacog beta pegol versus recombinant factor IX‐Fc fusion protein: A randomized trial Abstract Abstract Background and Objective Nonacog beta pegol (N9‐GP) and recombinant factor IX‐Fc fusion protein (rFIXFc) are extended half‐life rFIX compounds. We report the first singl... |
PMC10774961 | core_pubmed_pmc | Comparison of clinical safety between standard versus extended interval dosing of immune checkpoint inhibitors: a real-world retrospective cohort study | Comparison of clinical safety between standard versus extended interval dosing of immune checkpoint inhibitors: a real-world retrospective cohort study Abstract Abstract Background Extended interval dosing (ED) for inhibitors of programmed cell death protein 1 (anti-PD-1) (nivolumab, pembrolizumab) or its ligand (anti-... |
PMC7835864 | core_pubmed_pmc | Potential Herb–Drug Interactions in the Management of Age-Related Cognitive Dysfunction | Potential Herb–Drug Interactions in the Management of Age-Related Cognitive Dysfunction Abstract Late-life mild cognitive impairment and dementia represent a significant burden on healthcare systems and a unique challenge to medicine due to the currently limited treatment options. Plant phytochemicals have been conside... |
PMC12063698 | core_pubmed_pmc | Boswellia carteri Birdw. Resin Extract Induces Phase-I Cytochrome P-450 Enzyme Gene Expressions in Human Hepatocarcinoma (Hep G2) Cells: In vitro and in silico Studies | Boswellia carteri Birdw. Resin Extract Induces Phase-I Cytochrome P-450 Enzyme Gene Expressions in Human Hepatocarcinoma (Hep G2) Cells: In vitro and in silico Studies Abstract Abstract Introduction Boswellia carteri ( B. carteri ) resin is widely recognized for its anti-inflammatory, wound-healing, and immunomodulator... |
PMC8964916 | core_pubmed_pmc | Similar Clinical Outcomes in Patients with Systemic Juvenile Idiopathic Arthritis and Adult-Onset Still’s Disease Treated with Canakinumab: Bayesian and Population Model-Based Analyses | Similar Clinical Outcomes in Patients with Systemic Juvenile Idiopathic Arthritis and Adult-Onset Still’s Disease Treated with Canakinumab: Bayesian and Population Model-Based Analyses Abstract Abstract Introduction Systemic juvenile idiopathic arthritis (sJIA) and adult-onset Still’s disease (AOSD) represent pediatric... |
PMC5741395 | core_pubmed_pmc | The potential for interaction of tolbutamide with pomegranate juice against diabetic induced complications in rats | The potential for interaction of tolbutamide with pomegranate juice against diabetic induced complications in rats Abstract Background Pomegranate can inhibit cytochrome P450 (CYP) 2C9 activity, which is largely responsible for the metabolism of sulfonylureas. The present study was undertaken to evaluate the pharmacoki... |
PMC3022839 | core_pubmed_pmc | (R) -[ 11 C]Verapamil PET studies to assess changes in P-glycoprotein expression and functionality in rat blood-brain barrier after exposure to kainate-induced status epilepticus | (R) -[ 11 C]Verapamil PET studies to assess changes in P-glycoprotein expression and functionality in rat blood-brain barrier after exposure to kainate-induced status epilepticus Abstract Abstract Background Increased functionality of efflux transporters at the blood-brain barrier may contribute to decreased drug conce... |
PMC11509255 | core_pubmed_pmc | Development and Validation of a New Eco-Friendly HPLC-PDA Bioanalytical Method for Studying Pharmacokinetics of Seliciclib | Development and Validation of a New Eco-Friendly HPLC-PDA Bioanalytical Method for Studying Pharmacokinetics of Seliciclib Abstract Abstract Background and Objectives: Seliciclib (SEL) is the first selective, orally bioavailable potential drug containing cyclin-dependent kinase inhibitors. Preclinical studies showed an... |
PMC12964783 | core_pubmed_pmc | The evolution of SSRI research: trajectories of knowledge domains across four decades | The evolution of SSRI research: trajectories of knowledge domains across four decades Abstract Abstract Background Since their introduction in 1982, Selective Serotonin Reuptake Inhibitors (SSRIs) have fundamentally transformed psychiatric care, becoming the first-line pharmacological treatment for depression and expan... |
PMC11359785 | core_pubmed_pmc | A Physiologically-Based Pharmacokinetic Simulation to Evaluate Approaches to Mitigate Efavirenz-Induced Decrease in Levonorgestrel Exposure with a Contraceptive Implant | A Physiologically-Based Pharmacokinetic Simulation to Evaluate Approaches to Mitigate Efavirenz-Induced Decrease in Levonorgestrel Exposure with a Contraceptive Implant Abstract Abstract Background: Levonorgestrel implant is a highly effective hormonal contraceptive, but its efficacy may be compromised when used with c... |
PMC7531516 | core_pubmed_pmc | A Phase 1 and pharmacokinetic study evaluating daily or weekly schedules of the humanized anti-GD2 antibody hu14.18K322A in recurrent/refractory solid tumors | A Phase 1 and pharmacokinetic study evaluating daily or weekly schedules of the humanized anti-GD2 antibody hu14.18K322A in recurrent/refractory solid tumors Abstract ABSTRACT Hu14.18K322A is a humanized anti-GD2 monoclonal antibody with a single point mutation that reduces complement-mediated cytotoxicity, with a maxi... |
PMC12566802 | core_pubmed_pmc | Enteric Coating Enhances the Biopharmaceutical Performance of a Silica–Lipid Formulation of Abiraterone Acetate | Enteric Coating Enhances the Biopharmaceutical Performance of a Silica–Lipid Formulation of Abiraterone Acetate Abstract Abstract Background/Objectives: Lipid-based formulations are widely used to enhance the oral bioavailability of poorly water-soluble drugs. However, for weakly basic drugs with higher solubility unde... |
PMC11601558 | core_pubmed_pmc | SLC6A19 inhibition facilitates urinary neutral amino acid excretion and lowers plasma phenylalanine | SLC6A19 inhibition facilitates urinary neutral amino acid excretion and lowers plasma phenylalanine Abstract BACKGROUND The toxic accumulation of phenylalanine (Phe) in the brain underlies the neurological presentation of phenylketonuria (PKU). Solute carrier family 6 member 19 (SLC6A19) is the major transporter respon... |
PMC7065596 | core_pubmed_pmc | Targeting of Hepatic Macrophages by Therapeutic Nanoparticles | Targeting of Hepatic Macrophages by Therapeutic Nanoparticles Abstract Hepatic macrophage populations include different types of cells with plastic properties that can differentiate into diverse phenotypes to modulate their properties in response to different stimuli. They often regulate the activity of other cells and... |
PMC8637478 | core_pubmed_pmc | Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro , in - vivo and pharmacokinetic assessment | Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro , in - vivo and pharmacokinetic assessment Abstract Efavirenz is inhibitor of non-nucleoside reverse transcriptase enzyme; BCS class II drug. The objective of the present research was to prepare and evaluate nanosuspension of ... |
PMC8669703 | core_pubmed_pmc | Multidirectional facets of obesity management in the metabolic syndrome population after liver transplantation | Multidirectional facets of obesity management in the metabolic syndrome population after liver transplantation Abstract Abstract The obesity pandemic has resulted in an increasing demand for liver transplantation and has significantly altered the profile of liver transplant candidates in addition to affecting posttrans... |
PMC11230136 | core_pubmed_pmc | Prophylactic treatment with the c-Abl inhibitor, neurotinib, diminishes neuronal damage and the convulsive state in pilocarpine-induced mice | Prophylactic treatment with the c-Abl inhibitor, neurotinib, diminishes neuronal damage and the convulsive state in pilocarpine-induced mice Abstract SUMMARY The molecular mechanisms underlying seizure generation remain elusive, yet they are crucial for developing effective treatments for epilepsy. The current study sh... |
PMC10994248 | core_pubmed_pmc | First-In-Human Phase I Study of Tinengotinib (TT-00420), a Multiple Kinase Inhibitor, as a Single Agent in Patients With Advanced Solid Tumors | First-In-Human Phase I Study of Tinengotinib (TT-00420), a Multiple Kinase Inhibitor, as a Single Agent in Patients With Advanced Solid Tumors Abstract Abstract Purpose This first-in-human phase I dose-escalation study evaluated the safety, pharmacokinetics, and efficacy of tinengotinib (TT-00420), a multi-kinase inhib... |
PMC8504117 | core_pubmed_pmc | Advances in the study of emodin: an update on pharmacological properties and mechanistic basis | Advances in the study of emodin: an update on pharmacological properties and mechanistic basis Abstract Abstract Rhei Radix et Rhizoma, also known as rhubarb or Da Huang , has been widely used as a spice and as traditional herbal medicine for centuries, and is currently marketed in China as the principal herbs in vario... |
PMC10267530 | core_pubmed_pmc | Development and validation of a UPLC-MS/MS method for simultaneous detection of doxorubicin and sorafenib in plasma: Application to pharmacokinetic studies in rats | Development and validation of a UPLC-MS/MS method for simultaneous detection of doxorubicin and sorafenib in plasma: Application to pharmacokinetic studies in rats Abstract An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was developed for the simultaneous quantitation of doxorubicin (DO... |
PMC10133668 | core_pubmed_pmc | Combined therapy with pioglitazone and FGF21 mRNA synergistically ameliorates metabolic disorders in NAFLD rats | Combined therapy with pioglitazone and FGF21 mRNA synergistically ameliorates metabolic disorders in NAFLD rats Abstract Abstract Background Current study aims to investigate the ameliorative effect of pioglitazone (PIO) combined with mRNA encoding FGF21 (termed mFGF21) on the metabolic disorders in rats with nonalcoho... |
PMC9730833 | core_pubmed_pmc | Targeting OCT2 with Duloxetine to Prevent Oxaliplatin-induced Peripheral Neurotoxicity | Targeting OCT2 with Duloxetine to Prevent Oxaliplatin-induced Peripheral Neurotoxicity Abstract Abstract Oxaliplatin-induced peripheral neurotoxicity (OIPN) is a debilitating side effect that afflicts approximately 90% of patients that is initiated by OCT2-dependent uptake of oxaliplatin in dorsal root ganglion (DRG) n... |
PMC9485817 | core_pubmed_pmc | Riociguat in children with pulmonary arterial hypertension: The PATENT–CHILD study | Riociguat in children with pulmonary arterial hypertension: The PATENT–CHILD study Abstract Abstract Riociguat, a soluble guanylate cyclase stimulator, is approved for treatment of adults with pulmonary arterial hypertension (PAH). The safety, tolerability, and pharmacokinetics (PK) of oral riociguat in a pediatric pop... |
PMC11625052 | core_pubmed_pmc | A randomized phase 1 study of safety, tolerability, and pharmacokinetics of MK-1088, a novel dual adenosine receptor antagonist, in healthy adult participants | A randomized phase 1 study of safety, tolerability, and pharmacokinetics of MK-1088, a novel dual adenosine receptor antagonist, in healthy adult participants Abstract This phase 1 first-in-human study evaluated the safety, tolerability, and pharmacokinetics of MK-1088, a novel, small-molecule dual inhibitor of adenosi... |
PMC6854432 | core_pubmed_pmc | Prediction of Drug Permeability Using In Vitro Blood–Brain Barrier Models with Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells | Prediction of Drug Permeability Using In Vitro Blood–Brain Barrier Models with Human Induced Pluripotent Stem Cell-Derived Brain Microvascular Endothelial Cells Abstract Abstract The strong barrier function of the blood–brain barrier (BBB) protects the central nervous system (CNS) from xenobiotic substances, while the ... |
PMC3527451 | core_pubmed_pmc | A Pilot Randomized, Placebo Controlled, Double Blind Phase I Trial of the Novel SIRT1 Activator SRT2104 in Elderly Volunteers | A Pilot Randomized, Placebo Controlled, Double Blind Phase I Trial of the Novel SIRT1 Activator SRT2104 in Elderly Volunteers Abstract Background SRT2104 has been developed as a selective small molecule activator of SIRT1, a NAD + -dependent deacetylase involved in the regulation of energy homeostasis and the modulatio... |
PMC10641973 | core_pubmed_pmc | Efficacy, safety, and pharmacokinetics of MR13A11A, a generic of remifentanil, for pain management of Japanese patients in the intensive care unit: a double-blinded, fentanyl-controlled, randomized, non-inferiority phase 3 study | Efficacy, safety, and pharmacokinetics of MR13A11A, a generic of remifentanil, for pain management of Japanese patients in the intensive care unit: a double-blinded, fentanyl-controlled, randomized, non-inferiority phase 3 study Abstract Background The aims of this study were to evaluate the efficacy, safety, and pharm... |
PMC12886207 | core_pubmed_pmc | The use of generic versus brand names in (clinical) pharmacology education across Europe: a cross-sectional survey | The use of generic versus brand names in (clinical) pharmacology education across Europe: a cross-sectional survey Abstract Purpose In pharmacology and clinical pharmacology (P&CP) teaching, using generic names of medicines contributes to global comprehensibility. However, brand names are often used in routine clinical... |
PMC12670146 | core_pubmed_pmc | Development and implementation of a gyrolab-based generic anti-drug antibody assay for antibody-drug conjugates in cynomolgus monkey studies | Development and implementation of a gyrolab-based generic anti-drug antibody assay for antibody-drug conjugates in cynomolgus monkey studies Abstract Abstract Introduction Non-clinical immunogenicity yields valuable insights into pharmacokinetics, efficacy, and safety. Given the complex nature of ADC therapeutics, earl... |
PMC11103493 | core_pubmed_pmc | Albumin-seeking dyes with adjustable assemblies in situ enable programmable imaging windows and targeting tumor imaging | Albumin-seeking dyes with adjustable assemblies in situ enable programmable imaging windows and targeting tumor imaging Abstract Cyanine dyes are widely used organic probes for in vivo imaging due to their tunable fluorescence. They can form complexes with endogenous albumin, resulting in enhanced brightness and photos... |
PMC10361278 | core_pubmed_pmc | Pharmacokinetics of Efavirenz 600mg in Combination with Rifampicin in Chinese HIV/TB Co-Infection Patients | Pharmacokinetics of Efavirenz 600mg in Combination with Rifampicin in Chinese HIV/TB Co-Infection Patients Abstract Background Rifampicin is a known inducer of the cytochrome P450 (CYP2B6) enzyme, which can lead to a decrease in the concentration of efavirenz. Therefore, we conducted a study to evaluate the effect of d... |
PMC5563081 | core_pubmed_pmc | Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS | Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS Abstract Summary Mutations activating KRAS underlie many forms of cancer, but are refractory to therapeutic targeting. Here, we develop Poloppin, an inhibitor of protein-protein interactions via the Polo-box domain (PBD) of t... |
PMC6133081 | core_pubmed_pmc | A Population Pharmacokinetic and Pharmacodynamic Analysis of RP5063 Phase 2 Study Data in Patients with Schizophrenia or Schizoaffective Disorder | A Population Pharmacokinetic and Pharmacodynamic Analysis of RP5063 Phase 2 Study Data in Patients with Schizophrenia or Schizoaffective Disorder Abstract Background and Objective RP5063 is a novel multimodal dopamine (D)–serotonin (5-HT) stabilizer possessing partial agonist activity for D 2/3/4 and 5-HT 1A/2A , antag... |
PMC4058586 | core_pubmed_pmc | White Pepper and Piperine Have Different Effects on Pharmacokinetics of Puerarin in Rats | White Pepper and Piperine Have Different Effects on Pharmacokinetics of Puerarin in Rats Abstract This study attempted to explore the effects of white pepper and its major component piperine on puerarin administered to rats. Pharmacokinetic parameters of puerarin in rats were determined by oral administration (400 mg/k... |
PMC11750661 | core_pubmed_pmc | Tregs levels and phenotype modifications during Amyotrophic Lateral Sclerosis course | Tregs levels and phenotype modifications during Amyotrophic Lateral Sclerosis course Abstract Abstract Introduction T regulatory cells (Tregs) inversely correlate with disease progression in Amyotrophic Lateral Sclerosis (ALS) and fast-progressing ALS patients have been reported to exhibit dysfunctional, as well as red... |
PMC12945925 | core_pubmed_pmc | Population Pharmacokinetic–Pharmacodynamic Analysis of Zolpidem in Healthy Volunteers: Covariate Contributions to Variability in CNS Responses | Population Pharmacokinetic–Pharmacodynamic Analysis of Zolpidem in Healthy Volunteers: Covariate Contributions to Variability in CNS Responses Abstract ABSTRACT Population pharmacokinetic–pharmacodynamic (PK–PD) modeling was used to explore covariate effects on zolpidem PKs and PDs in 30 healthy Korean volunteers (15 m... |
PMC9609924 | core_pubmed_pmc | In Vitro Characterization of Inhibitors for Lung A549 and Leukemia K562 Cell Lines from Fungal Transformation of Arecoline Supported by In Silico Docking to M3-mAChR and ADME Prediction | In Vitro Characterization of Inhibitors for Lung A549 and Leukemia K562 Cell Lines from Fungal Transformation of Arecoline Supported by In Silico Docking to M3-mAChR and ADME Prediction Abstract The search for anticancer drugs is of continuous interest. Arecoline is an alkaloid with anticancer activity. Herein, the met... |
PMC10651646 | core_pubmed_pmc | Clinical covariates that improve the description of high dose methotrexate pharmacokinetics in a diverse population to inform MTXPK.org | Clinical covariates that improve the description of high dose methotrexate pharmacokinetics in a diverse population to inform MTXPK.org Abstract Abstract The MTXPK.org webtool was launched in December 2019 and was developed to facilitate model‐informed supportive care and optimal use of glucarpidase following the admin... |
PMC10800288 | core_pubmed_pmc | Population Pharmacokinetics and Model-Based Dose Optimization of Vancomycin in Sudanese Adult Patients with Renal Impairment | Population Pharmacokinetics and Model-Based Dose Optimization of Vancomycin in Sudanese Adult Patients with Renal Impairment Abstract Abstract Purpose The study aimed to perform a population pharmacokinetic (PK) analysis to obtain vancomycin PK parameter estimates in Sudanese adult patients. The population PK model is ... |
PMC9926085 | core_pubmed_pmc | A naïve pooled data approach for extrapolation of Phase 0 microdose trials to therapeutic dosing regimens | A naïve pooled data approach for extrapolation of Phase 0 microdose trials to therapeutic dosing regimens Abstract Abstract Microdosing is a strategy to obtain knowledge of human pharmacokinetics prior to Phase I clinical trials. The most frequently used method to extrapolate microdose (≤100 μg) pharmacokinetics to the... |
PMC8955020 | core_pubmed_pmc | Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis | Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis Abstract Nafamostat, a synthetic serine protease inhibitor, has been used for the treatment of inflammatory diseases such as pancreatitis. Recently, an increasing number of studies have shown the promising antiviral effects... |
PMC12024054 | core_pubmed_pmc | Comparative Pharmacological Assessment of Amoxicillin in Five Cultured Fish Species: Implications for Off-Label Use in Aquaculture | Comparative Pharmacological Assessment of Amoxicillin in Five Cultured Fish Species: Implications for Off-Label Use in Aquaculture Abstract Background : Amoxicillin (AMOX) is widely used in aquaculture for bacterial infections due to its efficacy and safety. Despite official approval for select species, off-label use i... |
PMC9837157 | core_pubmed_pmc | Potential inhibitory properties of structurally modified quercetin/isohamnetin glucosides against SARS-CoV-2 Mpro; molecular docking and dynamics simulation strategies | Potential inhibitory properties of structurally modified quercetin/isohamnetin glucosides against SARS-CoV-2 Mpro; molecular docking and dynamics simulation strategies Abstract Abstract Concerned organizations and individuals are fully engaged in seeking appropriate measures towards managing Severe Acute Respiratory Sy... |
PMC12706394 | core_pubmed_pmc | Population Pharmacokinetic Model of Pegbing in Healthy Subjects and Chronic Hepatitis B Patients | Population Pharmacokinetic Model of Pegbing in Healthy Subjects and Chronic Hepatitis B Patients Abstract ABSTRACT Pegbing (peginterferon alpha‐2b) is a polyethylene glycol‐modified interferon α‐2b injection that has demonstrated favorable efficacy and safety profiles in the treatment of chronic hepatitis B (CHB). This... |
PMC12042697 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of INT‐787, a Novel Farnesoid X Receptor Agonist, in Healthy Volunteers: A Phase 1 Trial | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of INT‐787, a Novel Farnesoid X Receptor Agonist, in Healthy Volunteers: A Phase 1 Trial Abstract ABSTRACT Aberrant farnesoid X receptor (FXR) signaling is implicated in cholestatic, inflammatory, and fibrotic liver diseases. In preclinical/clinical studies, ... |
PMC7902338 | core_pubmed_pmc | Influence of Cation Transporters (OCTs and MATEs) on the Renal and Hepatobiliary Disposition of [ 11 C]Metoclopramide in Mice | Influence of Cation Transporters (OCTs and MATEs) on the Renal and Hepatobiliary Disposition of [ 11 C]Metoclopramide in Mice Abstract Abstract Purpose To investigate the role of cation transporters (OCTs, MATEs) in the renal and hepatic disposition of the radiolabeled antiemetic drug [ 11 C]metoclopramide in mice with... |
PMC5813206 | core_pubmed_pmc | Integration of mechanistic and pharmacokinetic information to derive oral reference dose and margin‐of‐exposure values for hexavalent chromium | Integration of mechanistic and pharmacokinetic information to derive oral reference dose and margin‐of‐exposure values for hexavalent chromium Abstract Abstract The current US Environmental Protection Agency (EPA) reference dose (RfD) for oral exposure to chromium, 0.003 mg kg −1 day −1 , is based on a no‐observable‐ad... |
PMC9531372 | core_pubmed_pmc | Metabolic profiling and pharmacokinetic studies of Baihu-Guizhi decoction in rats by UFLC-Q-TOF–MS/MS and UHPLC-Q-TRAP-MS/MS | Metabolic profiling and pharmacokinetic studies of Baihu-Guizhi decoction in rats by UFLC-Q-TOF–MS/MS and UHPLC-Q-TRAP-MS/MS Abstract Abstract Background Baihu-Guizhi decoction (BHGZD) is a well-documented traditional Chinese Medicine (TCM) prescription that has been extensively applied to treating rheumatoid arthritis... |
PMC9375819 | core_pubmed_pmc | Radiofluorination of a highly potent ATM inhibitor as a potential PET imaging agent | Radiofluorination of a highly potent ATM inhibitor as a potential PET imaging agent Abstract Abstract Purpose Ataxia telangiectasia mutated (ATM) is a key mediator of the DNA damage response, and several ATM inhibitors (ATMi) are currently undergoing early phase clinical trials for the treatment of cancer. A radiolabel... |
PMC9858801 | core_pubmed_pmc | Riluzole for treating spasticity in patients with chronic traumatic spinal cord injury: Study protocol in the phase ib/iib adaptive multicenter randomized controlled RILUSCI trial | Riluzole for treating spasticity in patients with chronic traumatic spinal cord injury: Study protocol in the phase ib/iib adaptive multicenter randomized controlled RILUSCI trial Abstract Abstract Background Satisfactory treatment is often lacking for spasticity, a highly prevalent motor disorder in patients with spin... |
PMC7383646 | core_pubmed_pmc | Changes in perampanel levels during de‐induction: Simulations following carbamazepine discontinuation | Changes in perampanel levels during de‐induction: Simulations following carbamazepine discontinuation Abstract Objective To evaluate the time course of changes in perampanel levels when co‐administered with carbamazepine, and following carbamazepine discontinuation, using a physiologically based pharmacokinetic (PBPK) ... |
PMC3142667 | core_pubmed_pmc | Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans | Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans Abstract Opioid neurotransmission has a key role in mediating reward-related behaviours. Opioid receptor (OR) antagonists, such as naltrexone (NTX), c... |
PMC8167886 | core_pubmed_pmc | Optimizing Pharmacology Studies in Pregnant and Lactating Women Using Lessons From HIV: A Consensus Statement | Optimizing Pharmacology Studies in Pregnant and Lactating Women Using Lessons From HIV: A Consensus Statement Abstract Abstract Information on the extent of drug exposure to mothers and infants during pregnancy and lactation normally becomes available years after regulatory approval of a drug. Clinicians face knowledge... |
PMC9200635 | core_pubmed_pmc | Impact of busulfan pharmacokinetics on outcome in adult patients receiving an allogeneic hematopoietic cell transplantation | Impact of busulfan pharmacokinetics on outcome in adult patients receiving an allogeneic hematopoietic cell transplantation Abstract Busulfan (Bu) is widely used in conditioning regimens before allogeneic hematopoietic cell transplantation, with variable metabolism due to interindividual differences of pharmacokinetics... |
PMC12121915 | core_pubmed_pmc | Pharmacokinetics/pharmacodynamics of gamithromycin for treating Pasteurella multocida infection in cattle using a tissue cage model | Pharmacokinetics/pharmacodynamics of gamithromycin for treating Pasteurella multocida infection in cattle using a tissue cage model Abstract Abstract In this study, gamithromycin, a long-acting azalide antibiotic recently introduced for bovine respiratory disease (BRD) treatment, was evaluated for its effectiveness aga... |
PMC3555823 | core_pubmed_pmc | Effectiveness of Efavirenz-Based Regimens in Young HIV-Infected Children Treated for Tuberculosis: A Treatment Option for Resource-Limited Settings | Effectiveness of Efavirenz-Based Regimens in Young HIV-Infected Children Treated for Tuberculosis: A Treatment Option for Resource-Limited Settings Abstract Abstract Background Antiretroviral treatment (ART) options for young children co-infected with HIV and tuberculosis are limited in resource-poor settings due to li... |
PMC7211192 | core_pubmed_pmc | The Path Towards a Tailored Clinical Biosimilar Development | The Path Towards a Tailored Clinical Biosimilar Development Abstract Since the first approval of a biosimilar medicinal product in 2006, scientific understanding of the features and development of biosimilar medicines has accumulated. This review scrutinizes public information on development programs and the contributi... |
PMC7911516 | core_pubmed_pmc | Investigation of the Factors Responsible for the Poor Oral Bioavailability of Acacetin in Rats: Physicochemical and Biopharmaceutical Aspects | Investigation of the Factors Responsible for the Poor Oral Bioavailability of Acacetin in Rats: Physicochemical and Biopharmaceutical Aspects Abstract Acacetin, an important ingredient of acacia honey and a component of several medicinal plants, exhibits therapeutic effects such as antioxidative, anticancer, anti-infla... |
PMC6244763 | core_pubmed_pmc | Simulation-based suggestions to improve ibuprofen dosing for patent ductus arteriosus in preterm newborns | Simulation-based suggestions to improve ibuprofen dosing for patent ductus arteriosus in preterm newborns Abstract Abstract Purpose Ibuprofen is the drug of choice for treatment of patent ductus arteriosus (PDA). There is accumulating evidence that current ibuprofen-dosing regimens for PDA treatment are inadequate. We ... |
PMC12668896 | core_pubmed_pmc | Effects of Intravenous Administration of Vancomycin on Peritonitis in a Patient on Peritoneal Dialysis | Effects of Intravenous Administration of Vancomycin on Peritonitis in a Patient on Peritoneal Dialysis Abstract ABSTRACT In settings where intraperitoneal vancomycin is unavailable or off‐label (e.g., Japan), intravenous vancomycin can be a viable treatment option for peritoneal dialysis‐associated peritonitis. Due to ... |
PMC6183038 | core_pubmed_pmc | Sequencing of high-efficacy disease-modifying therapies in multiple sclerosis: perspectives and approaches | Sequencing of high-efficacy disease-modifying therapies in multiple sclerosis: perspectives and approaches Abstract Multiple sclerosis (MS) is characterized by chronic inflammation in conjunction with neurodegeneration within the central nervous system. Most individuals with MS begin with a relapsing remitting course t... |
PMC3032760 | core_pubmed_pmc | Two-dose-level confirmatory study of the pharmacokinetics and tolerability of everolimus in Chinese patients with advanced solid tumors | Two-dose-level confirmatory study of the pharmacokinetics and tolerability of everolimus in Chinese patients with advanced solid tumors Abstract Abstract Background This phase I, randomized, multicenter, open-label study investigated the pharmacokinetics, safety, and efficacy of the oral mammalian target of rapamycin i... |
PMC8167102 | core_pubmed_pmc | Pharmacodynamic evaluation of suppression of in vitro resistance in Acinetobacter baumannii strains using polymyxin B-based combination therapy | Pharmacodynamic evaluation of suppression of in vitro resistance in Acinetobacter baumannii strains using polymyxin B-based combination therapy Abstract Abstract The emergence of polymyxin resistance in Gram-negative bacteria infections has motivated the use of combination therapy. This study determined the mutant sele... |
PMC8788976 | core_pubmed_pmc | Pharmacology of enflicoxib, a new coxib drug: Efficacy and dose determination by clinical and pharmacokinetic‐guided approach for the treatment of osteoarthritis in dogs based on an acute arthritis induction model | Pharmacology of enflicoxib, a new coxib drug: Efficacy and dose determination by clinical and pharmacokinetic‐guided approach for the treatment of osteoarthritis in dogs based on an acute arthritis induction model Abstract Abstract Enflicoxib is a newly developed NSAID of the coxib class. The optimal therapeutic dose t... |
PMC8134669 | core_pubmed_pmc | Hereditary Spastic Paraplegia and Future Therapeutic Directions: Beneficial Effects of Small Compounds Acting on Cellular Stress | Hereditary Spastic Paraplegia and Future Therapeutic Directions: Beneficial Effects of Small Compounds Acting on Cellular Stress Abstract Hereditary spastic paraplegia (HSP) is a group of inherited neurodegenerative conditions that share a characteristic feature of degeneration of the longest axons within the corticosp... |
PMC5480307 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Tolvaptan in Autosomal Dominant Polycystic Kidney Disease: Phase 2 Trials for Dose Selection in the Pivotal Phase 3 Trial | Pharmacokinetics and Pharmacodynamics of Tolvaptan in Autosomal Dominant Polycystic Kidney Disease: Phase 2 Trials for Dose Selection in the Pivotal Phase 3 Trial Abstract Abstract In the pivotal TEMPO 3:4 trial, the arginine vasopressin V2‐receptor antagonist tolvaptan reduced the rate of kidney growth in patients wit... |
PMC9243242 | core_pubmed_pmc | Mechanistic Considerations and Pharmacokinetic Implications on Concomitant Drug Administration During CytoSorb Therapy | Mechanistic Considerations and Pharmacokinetic Implications on Concomitant Drug Administration During CytoSorb Therapy Abstract OBJECTIVE: The CytoSorb hemoadsorption device (CytoSorbents Inc, Monmouth Junction, NJ) is increasingly used in many critical disease states. The potential impact on the pharmacokinetic (PK) o... |
PMC8772806 | core_pubmed_pmc | Bacterial Mixology: Combining Pharmacodynamic Models to Predict In Vitro Competition of MCR-1-Harboring E. coli | Bacterial Mixology: Combining Pharmacodynamic Models to Predict In Vitro Competition of MCR-1-Harboring E. coli Abstract The emergence of mobile colistin resistance ( mcr )-mediated polymyxin resistance has resulted in a significant detriment to the utility of the polymyxins in the clinical setting. Though the risk for... |
PMC11530684 | core_pubmed_pmc | Computational screening of phytochemicals present in some Nigerian medicinal plants against sickle cell disease | Computational screening of phytochemicals present in some Nigerian medicinal plants against sickle cell disease Abstract Abstract Four hundred Phytochemical (bio-active) compounds having predictive activity for treating Sickle Cell Anemia were screened, using PASS online computational resource. Twenty-six compounds out... |
PMC7058714 | core_pubmed_pmc | Dose-Finding Study and Pharmacokinetics Profile of the Novel 13-Mer Antisense miR-221 Inhibitor in Sprague-Dawley Rats | Dose-Finding Study and Pharmacokinetics Profile of the Novel 13-Mer Antisense miR-221 Inhibitor in Sprague-Dawley Rats Abstract Abstract miR-221 is overexpressed in several malignancies where it promotes tumor growth and survival by interfering with gene transcripts, including p27Kip1, PUMA, PTEN, and p57Kip2. We previ... |
PMC12917657 | core_pubmed_pmc | Repositioning HDAC Inhibitors for Glioma Treatment: Synthesis and Biological Evaluation | Repositioning HDAC Inhibitors for Glioma Treatment: Synthesis and Biological Evaluation Abstract Abstract Gliomas are a type of brain tumor associated with poor patient prognosis, with current treatment, surgical resection when feasible, followed by radiotherapy and chemotherapy (Temozolomide), yielding a median surviv... |
PMC6682992 | core_pubmed_pmc | Bioavailability of Sulforaphane Following Ingestion of Glucoraphanin-Rich Broccoli Sprout and Seed Extracts with Active Myrosinase: A Pilot Study of the Effects of Proton Pump Inhibitor Administration | Bioavailability of Sulforaphane Following Ingestion of Glucoraphanin-Rich Broccoli Sprout and Seed Extracts with Active Myrosinase: A Pilot Study of the Effects of Proton Pump Inhibitor Administration Abstract We examined whether gastric acidity would affect the activity of myrosinase, co-delivered with glucoraphanin (... |
PMC9796281 | core_pubmed_pmc | Interdisciplinary model‐informed drug development for extending duration of elagolix treatment in patients with uterine fibroids | Interdisciplinary model‐informed drug development for extending duration of elagolix treatment in patients with uterine fibroids Abstract Abstract Aim Elagolix, a gonadotropin‐releasing hormone receptor antagonist, was recently approved for heavy menstrual bleeding associated with uterine fibroids (UF, Oriahnn) at a do... |
PMC7755218 | core_pubmed_pmc | Age influences on Propofol estimated brain concentration and entropy during maintenance and at return of consciousness during total intravenous anesthesia with target-controlled infusion in unparalyzed patients: An observational prospective trial | Age influences on Propofol estimated brain concentration and entropy during maintenance and at return of consciousness during total intravenous anesthesia with target-controlled infusion in unparalyzed patients: An observational prospective trial Abstract Purpose Aging affects pharmacodynamics/pharmacokinetics of anest... |
PMC6315097 | core_pubmed_pmc | Pharmacological evaluation of HM41322, a novel SGLT1/2 dual inhibitor, in vitro and in vivo | Pharmacological evaluation of HM41322, a novel SGLT1/2 dual inhibitor, in vitro and in vivo Abstract Abstract HM41322 is a novel oral sodium-glucose cotransporter (SGLT) 1/2 dual inhibitor. In this study, the in vitro and in vivo pharmacokinetic and pharmacologic profiles of HM41322 were compared to those of dapagliflo... |
PMC10129982 | core_pubmed_pmc | Radiation dosimetry and pharmacokinetics of the tau PET tracer florzolotau (18F) in healthy Japanese subjects | Radiation dosimetry and pharmacokinetics of the tau PET tracer florzolotau (18F) in healthy Japanese subjects Abstract Abstract Objective Abnormal aggregation of tau in the brain is a major contributing factor in various neurodegenerative diseases. Florzolotau (18F) (florzolotau, APN-1607, PM-PBB3) has been shown to be... |
PMC3302113 | core_pubmed_pmc | Pharmacodynamic Modelling of Biomarker Data in Oncology | Pharmacodynamic Modelling of Biomarker Data in Oncology Abstract Abstract The development of pharmacodynamic (PD) biomarkers in oncology has implications for design of clinical protocols from preclinical data and for predicting clinical outcomes from early clinical data. Two classes of biomarkers have received particul... |
PMC7935831 | core_pubmed_pmc | Population Pharmacokinetic Evaluation of Amikacin Liposome Inhalation Suspension in Patients with Treatment-Refractory Nontuberculous Mycobacterial Lung Disease | Population Pharmacokinetic Evaluation of Amikacin Liposome Inhalation Suspension in Patients with Treatment-Refractory Nontuberculous Mycobacterial Lung Disease Abstract Abstract Background and Objectives Use of parenteral amikacin to treat refractory nontuberculous mycobacterial (NTM) lung disease is limited by system... |
PMC5348890 | core_pubmed_pmc | Effect of Moringa oleifera Lam. leaf powder on the pharmacokinetics of nevirapine in HIV-infected adults: a one sequence cross-over study | Effect of Moringa oleifera Lam. leaf powder on the pharmacokinetics of nevirapine in HIV-infected adults: a one sequence cross-over study Abstract Background Moringa oleifera Lam., an herb commonly consumed by HIV-infected people on antiretroviral therapy, inhibits cytochrome P450 3A4, 1A2 and 2D6 activity in vitro; an... |
PMC10602507 | core_pubmed_pmc | Bempegaldesleukin Plus Nivolumab in Untreated Advanced Melanoma: The Open-Label, Phase III PIVOT IO 001 Trial Results | Bempegaldesleukin Plus Nivolumab in Untreated Advanced Melanoma: The Open-Label, Phase III PIVOT IO 001 Trial Results Abstract PURPOSE Despite marked advances in the treatment of unresectable or metastatic melanoma, the need for novel therapies remains. Bempegaldesleukin (BEMPEG), a pegylated interleukin-2 (IL-2) cytok... |
PMC6971975 | core_pubmed_pmc | Morphine plasmatic concentration in a pregnant mare and its foal after long term epidural administration | Morphine plasmatic concentration in a pregnant mare and its foal after long term epidural administration Abstract Background Epidural administration of morphine has been shown to be an effective analgesic strategy in horses; however, the possible occurrence of side effects limits its usage. In order to decrease their f... |
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