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PMC8283551 | core_pubmed_pmc | Study protocol for a phase 2A trial of the safety and tolerability of increased dose rifampicin and adjunctive linezolid, with or without aspirin, for HIV-associated tuberculous meningitis [LASER-TBM] | Study protocol for a phase 2A trial of the safety and tolerability of increased dose rifampicin and adjunctive linezolid, with or without aspirin, for HIV-associated tuberculous meningitis [LASER-TBM] Abstract Background: Tuberculous meningitis (TBM) is the most lethal form of tuberculosis with a mortality of ~50% in t... |
PMC9598284 | core_pubmed_pmc | A Minimal Physiologically Based Pharmacokinetic Model to Characterize CNS Distribution of Metronidazole in Neuro Care ICU Patients | A Minimal Physiologically Based Pharmacokinetic Model to Characterize CNS Distribution of Metronidazole in Neuro Care ICU Patients Abstract Abstract Understanding antibiotic concentration-time profiles in the central nervous system (CNS) is crucial to treat severe life-threatening CNS infections, such as nosocomial ven... |
PMC6333349 | core_pubmed_pmc | The influence of concomitant antiepileptic drugs on lamotrigine serum concentrations in Northwest Chinese Han population with epilepsy | The influence of concomitant antiepileptic drugs on lamotrigine serum concentrations in Northwest Chinese Han population with epilepsy Abstract Objective The aims of this study were to identify the influencing factors such as gender, age, dose and combinations of other antiepileptic drugs (AEDs), especially in triple c... |
PMC11361584 | core_pubmed_pmc | Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions | Development and validation of a reversed-phase HPLC-UV method for simultaneous determination of levosulpiride and omeprazole in human plasma: Applicability of the method for evaluation of pharmacokinetic drug-drug interactions Abstract Levosulpiride and omeprazole are co-prescribed for gastrointestinal disorders associ... |
PMC3590411 | core_pubmed_pmc | Ten Years of Experience with Biphasic Insulin Aspart 30 | Ten Years of Experience with Biphasic Insulin Aspart 30 Abstract Biphasic insulin aspart 30 (BIAsp 30) includes 30% soluble rapid-acting insulin aspart (IAsp) along with an intermediate-acting 70% protaminated IAsp that provides coverage of prandial and basal insulin in a single injection. As BIAsp 30 has been availabl... |
PMC6272185 | core_pubmed_pmc | Antimycobacterial and Anti-Inflammatory Activities of Substituted Chalcones Focusing on an Anti-Tuberculosis Dual Treatment Approach | Antimycobacterial and Anti-Inflammatory Activities of Substituted Chalcones Focusing on an Anti-Tuberculosis Dual Treatment Approach Abstract Abstract Tuberculosis (TB) remains a serious public health problem aggravated by the emergence of M. tuberculosis (Mtb) strains resistant to multiple drugs (MDR). Delay in TB tre... |
PMC9607246 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modelling of Daptomycin for Schedule Optimization in Patients with Renal Impairment | Population Pharmacokinetic/Pharmacodynamic Modelling of Daptomycin for Schedule Optimization in Patients with Renal Impairment Abstract Abstract The aims of this study are (i) to develop a population pharmacokinetic/pharmacodynamic model of daptomycin in patients with normal and impaired renal function, and (ii) to est... |
PMC4363212 | core_pubmed_pmc | Tedizolid Phosphate: a Next-Generation Oxazolidinone | Tedizolid Phosphate: a Next-Generation Oxazolidinone Abstract Treatment of multidrug-resistant Gram-positive infections continues to challenge clinicians as the emergence of new resistance mechanisms outpaces introduction of novel antimicrobial agents. Tedizolid phosphate is a next-generation oxazolidinone with activit... |
PMC8409942 | core_pubmed_pmc | Immunosuppressive effect of PLGA-FK506-NPs in treatment of acute cardiac rejection via topical subcutaneous injection | Immunosuppressive effect of PLGA-FK506-NPs in treatment of acute cardiac rejection via topical subcutaneous injection Abstract Abstract FK506, a first-line immunosuppressant, is routinely administered orally and intravenously to inhibit activation and proliferation of T cells after heart transplantation (HT). Current a... |
PMC7508576 | core_pubmed_pmc | Relationship between Gepotidacin Exposure and Prevention of On-Therapy Resistance Amplification in a Neisseria gonorrhoeae Hollow-Fiber In Vitro Infection Model | Relationship between Gepotidacin Exposure and Prevention of On-Therapy Resistance Amplification in a Neisseria gonorrhoeae Hollow-Fiber In Vitro Infection Model Abstract Multidrug-resistant Neisseria gonorrhoeae has emerged as a threat to global health. The relationship between gepotidacin exposure and prevention of on... |
PMC7388563 | core_pubmed_pmc | Population pharmacokinetics model and initial dose optimization of tacrolimus in children and adolescents with lupus nephritis based on real-world data | Population pharmacokinetics model and initial dose optimization of tacrolimus in children and adolescents with lupus nephritis based on real-world data Abstract Abstract The present study aimed to establish a population pharmacokinetics model of tacrolimus and further optimize the initial dosing regimen of tacrolimus i... |
PMC12712551 | core_pubmed_pmc | An Open Label, Randomized, Comparative Bioavailability Study of BioTurm™ Extract Versus Curcuma longa Extract With Piperine in Healthy Adult Volunteers | An Open Label, Randomized, Comparative Bioavailability Study of BioTurm™ Extract Versus Curcuma longa Extract With Piperine in Healthy Adult Volunteers Abstract Abstract Introduction Curcumin (95%) from Curcuma longa rhizomes holds significant therapeutic promise, but its clinical efficacy is limited by poor oral bioav... |
PMC10196421 | core_pubmed_pmc | Relationship between factor VIII levels and bleeding for rFVIII‐SingleChain in severe hemophilia A: A repeated time‐to‐event analysis | Relationship between factor VIII levels and bleeding for rFVIII‐SingleChain in severe hemophilia A: A repeated time‐to‐event analysis Abstract Abstract Publications on the exposure‐effect relationships of factor concentrates for hemophilia treatment are limited, whereas such analyses give insight on treatment efficacy.... |
PMC9960599 | core_pubmed_pmc | Considerations for Intravenous Anesthesia Dose in Obese Children: Understanding PKPD | Considerations for Intravenous Anesthesia Dose in Obese Children: Understanding PKPD Abstract The intravenous induction or loading dose in children is commonly prescribed per kilogram. That dose recognizes the linear relationship between volume of distribution and total body weight. Total body weight comprises both fat... |
PMC6256002 | core_pubmed_pmc | Influence of age and renal impairment on the steady state pharmacokinetics of filgotinib, a selective JAK1 inhibitor | Influence of age and renal impairment on the steady state pharmacokinetics of filgotinib, a selective JAK1 inhibitor Abstract Abstract Aims Filgotinib (GS‐6034, formerly GLPG0634) is an oral, selective Janus kinase 1 (JAK1) inhibitor that showed early response and sustained efficacy in patients with rheumatoid arthriti... |
PMC8891439 | core_pubmed_pmc | Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen | Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen Abstract Abstract Background The optimal procedure for combining radiotherapy (RT) with tamoxifen treatment is controversial as RT may alter the pharmacokinetics and biotransformation of tamoxifen. The present study investigated this poten... |
PMC9395984 | core_pubmed_pmc | Drug-drug interactions between antithrombotics and direct-acting antivirals in hepatitis C virus (HCV) patients: A brief, updated report | Drug-drug interactions between antithrombotics and direct-acting antivirals in hepatitis C virus (HCV) patients: A brief, updated report Abstract Hepatitis C virus (HCV) is one of the leading causes of chronic liver disease affecting over 71 million people worldwide. An increased incidence of atherothrombotic events [e... |
PMC3160947 | core_pubmed_pmc | Microemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo | Microemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo Abstract Objective To deliver 2,3,5,6-tetramethylpyrazine (TMP) in a relatively large dose through a transdermal route and facilitate the practical application of microemulison in transdermal dr... |
PMC7321154 | core_pubmed_pmc | Pharmacokinetic Properties of 68 Ga-labelled Folic Acid Conjugates: Improvement Using HEHE Tag | Pharmacokinetic Properties of 68 Ga-labelled Folic Acid Conjugates: Improvement Using HEHE Tag Abstract Abstract The folate receptor (FR) is a promising cell membrane-associated target for molecular imaging and radionuclide therapy of cancer (FR-α) and potentially also inflammatory diseases (FR-β) through use of folic ... |
PMC12024006 | core_pubmed_pmc | Pharmacokinetics, Withdrawal Time, and Physiological Effects of Single Oral Administration of Enrofloxacin in Dybowski’s Frog ( Rana dybowskii ) | Pharmacokinetics, Withdrawal Time, and Physiological Effects of Single Oral Administration of Enrofloxacin in Dybowski’s Frog ( Rana dybowskii ) Abstract Background : As a broad-spectrum fluoroquinolone, enrofloxacin (ENR) is commonly employed to manage bacterial infections in aquatic species. Nevertheless, there have ... |
PMC6798029 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Gamithromycin Treatment of Pasteurella multocida in a Murine Lung Infection Model | Pharmacokinetics and Pharmacodynamics of Gamithromycin Treatment of Pasteurella multocida in a Murine Lung Infection Model Abstract Abstract Gamithromycin is approved for the treatment and prevention of bovine respiratory disease (BRD), which is caused mainly by Mannheimia haemolytica, Pasteurella multocida, Histophilu... |
PMC5986681 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Asunaprevir in Subjects with Hepatitis C Virus Infection | Population Pharmacokinetic Analysis of Asunaprevir in Subjects with Hepatitis C Virus Infection Abstract Abstract Introduction Asunaprevir (ASV) is a potent, pangenotypic, twice-daily hepatitis C virus (HCV) NS3 inhibitor indicated for the treatment of chronic HCV infection. Methods A population pharmacokinetic (PPK) m... |
PMC11743626 | core_pubmed_pmc | Evaluation of the effectiveness of GASMAN anesthesia simulation software combined with case-based learning versus traditional lecture-based learning in inhalation anesthesia education | Evaluation of the effectiveness of GASMAN anesthesia simulation software combined with case-based learning versus traditional lecture-based learning in inhalation anesthesia education Abstract Abstract Objective To evaluate the effectiveness of integrating GASMAN anesthesia simulation software with case-based learning ... |
PMC12447529 | core_pubmed_pmc | Ibrexafungerp: Mechanism of Action, Clinical, and Translational Science | Ibrexafungerp: Mechanism of Action, Clinical, and Translational Science Abstract ABSTRACT Ibrexafungerp is a first‐in‐class triterpenoid antifungal that targets β‐(1,3)‐glucan synthase in fungal cell wall development. It is indicated for vulvovaginal candidiasis (VVC) and recurrent vulvovaginal candidiasis (RVVC) in ad... |
PMC6508715 | core_pubmed_pmc | Neoadjuvant therapy for locally advanced gastric cancer patients. A population pharmacodynamic modeling | Neoadjuvant therapy for locally advanced gastric cancer patients. A population pharmacodynamic modeling Abstract Abstract Background Perioperative chemotherapy (CT) or neoadjuvant chemoradiotherapy (CRT) in patients with locally advanced gastric (GC) or gastroesophageal junction cancer (GEJC) has been shown to improve ... |
PMC12538932 | core_pubmed_pmc | Renal maturation and catch-up clearance of ganciclovir in a preterm neonate: Bayesian pharmacokinetic analysis using a population model | Renal maturation and catch-up clearance of ganciclovir in a preterm neonate: Bayesian pharmacokinetic analysis using a population model Abstract Background Congenital cytomegalovirus (CMV) infection is a major cause of neonatal morbidity. However, optimizing ganciclovir (GCV) dosing in preterm infants is complicated by... |
PMC5515048 | core_pubmed_pmc | Pharmacokinetics-based adherence measures for antiretroviral therapy in HIV-infected Kenyan children | Pharmacokinetics-based adherence measures for antiretroviral therapy in HIV-infected Kenyan children Abstract Abstract Background : Traditional medication adherence measures do not account for the pharmacokinetic (PK) properties of the drugs, potentially misrepresenting true therapeutic exposure. Methods : In a populat... |
PMC11990103 | core_pubmed_pmc | Anticancer Activity and Safety Profile of Novel 1-(4-Fluorophenoxyacetyl)-4-substituted Thio/Semicarbazide Derivatives | Anticancer Activity and Safety Profile of Novel 1-(4-Fluorophenoxyacetyl)-4-substituted Thio/Semicarbazide Derivatives Abstract Compounds with thiosemicarbazide and semicarbazide scaffolds are among the most promising structures in medicinal chemistry due to the possibility of forming multiple hydrogen bonds. Therefore... |
PMC12017596 | core_pubmed_pmc | Prasugrel Intermediate Metabolite Modulates Platelet Inhibition by Negatively Interfering With an Active Metabolite: An Ex Vivo, In Vitro, and In Silico Study | Prasugrel Intermediate Metabolite Modulates Platelet Inhibition by Negatively Interfering With an Active Metabolite: An Ex Vivo, In Vitro, and In Silico Study Abstract Abstract BACKGROUND: Prasugrel is converted into prasugrel active metabolite (PAM; R-138727) through the cytochrome P450–mediated conversion of an inter... |
PMC11865102 | core_pubmed_pmc | Assessing early therapeutic drug monitoring of adalimumab as a predictor of treatment efficacy and immunogenicity in rheumatic diseases: “early therapeutic drug monitoring of adalimumab” | Assessing early therapeutic drug monitoring of adalimumab as a predictor of treatment efficacy and immunogenicity in rheumatic diseases: “early therapeutic drug monitoring of adalimumab” Abstract Abstract Introduction Therapeutic drug monitoring (TDM) in inflammatory rheumatic diseases (RMDs) is gaining interest. Howev... |
PMC11936814 | core_pubmed_pmc | Bioequivalence of China- and Germany-manufactured bisoprolol (Concor ® ) tablets in fasted and fed healthy Chinese participants: a randomized, open-label, two-way, crossover study | Bioequivalence of China- and Germany-manufactured bisoprolol (Concor ® ) tablets in fasted and fed healthy Chinese participants: a randomized, open-label, two-way, crossover study Abstract Background The bioequivalence of Concor ® (Merck Healthcare KGaA, Darmstadt, Germany), a bisoprolol-containing tablet, manufactured... |
PMC9834375 | core_pubmed_pmc | Pharmacokinetics and Safety of Follitropin Delta in Gonadotropin Down-Regulated Healthy Chinese Women | Pharmacokinetics and Safety of Follitropin Delta in Gonadotropin Down-Regulated Healthy Chinese Women Abstract Background Follitropin delta, a novel recombinant follicle-stimulating hormone (rFSH) preparation derived from a human cell line, has different pharmacokinetic and pharmacodynamic properties compared with exis... |
PMC5034953 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Lumefantrine in Young Ugandan Children Treated With Artemether-Lumefantrine for Uncomplicated Malaria | Population Pharmacokinetics and Pharmacodynamics of Lumefantrine in Young Ugandan Children Treated With Artemether-Lumefantrine for Uncomplicated Malaria Abstract Abstract Background. The pharmacokinetics and pharmacodynamics of lumefantrine, a component of the most widely used treatment for malaria, artemether-lumefan... |
PMC12561088 | core_pubmed_pmc | LLM-Enhanced Multimodal Framework for Drug–Drug Interaction Prediction | LLM-Enhanced Multimodal Framework for Drug–Drug Interaction Prediction Abstract Background: Drug–drug interactions (DDIs) involve pharmacokinetic or pharmacodynamic changes that occur when multiple drugs are co-administered, potentially leading to reduced efficacy or adverse effects. As polypharmacy becomes more preval... |
PMC5752984 | core_pubmed_pmc | A Pilot Study of Immune Activation and Rifampin Absorption in HIV-Infected Patients without Tuberculosis Infection: A Short Report | A Pilot Study of Immune Activation and Rifampin Absorption in HIV-Infected Patients without Tuberculosis Infection: A Short Report Abstract Abstract Background Rifampin malabsorption is frequently observed in tuberculosis patients coinfected with human immunodeficiency virus (HIV) but cannot be predicted by patient fac... |
PMC5702903 | core_pubmed_pmc | Predicting Drug Concentration‐Time Profiles in Multiple CNS Compartments Using a Comprehensive Physiologically‐Based Pharmacokinetic Model | Predicting Drug Concentration‐Time Profiles in Multiple CNS Compartments Using a Comprehensive Physiologically‐Based Pharmacokinetic Model Abstract Abstract Drug development targeting the central nervous system (CNS) is challenging due to poor predictability of drug concentrations in various CNS compartments. We develo... |
PMC6219411 | core_pubmed_pmc | Pharmacokinetic evaluation of a transdermal anastrozole-in-adhesive formulation | Pharmacokinetic evaluation of a transdermal anastrozole-in-adhesive formulation Abstract Background and objective Anastrozole is a well-established active pharmaceutical ingredient (API) used for the treatment of hormone-sensitive breast cancer (BC) in postmenopausal women. However, treatment with the only available or... |
PMC4782683 | core_pubmed_pmc | Extracorporeal treatment for carbamazepine poisoning: Systematic review and recommendations from the EXTRIP workgroup | Extracorporeal treatment for carbamazepine poisoning: Systematic review and recommendations from the EXTRIP workgroup Abstract Abstract Context . The Extracorporeal Treatments in Poisoning (EXTRIP) workgroup was created to provide evidence and consensus-based recommendations on the use of extracorporeal treatments (ECT... |
PMC7643733 | core_pubmed_pmc | Model-Based Meta-analysis of Rifampicin Exposure and Mortality in Indonesian Tuberculous Meningitis Trials | Model-Based Meta-analysis of Rifampicin Exposure and Mortality in Indonesian Tuberculous Meningitis Trials Abstract Abstract Background Intensified antimicrobial treatment with higher rifampicin doses may improve outcome of tuberculous meningitis, but the desirable exposure and necessary dose are unknown. Our objective... |
PMC4136845 | core_pubmed_pmc | Evaluation of Antimalarial Activity and Toxicity of a New Primaquine Prodrug | Evaluation of Antimalarial Activity and Toxicity of a New Primaquine Prodrug Abstract Plasmodium vivax is the most prevalent of the five species causing malaria in humans. The current available treatment for P. vivax malaria is limited and unsatisfactory due to at least two drawbacks: the undesirable side effects of pr... |
PMC11334799 | core_pubmed_pmc | CG001, a C3b-targeted complement inhibitor, blocks 3 complement pathways: development and preclinical evaluation ∗ | CG001, a C3b-targeted complement inhibitor, blocks 3 complement pathways: development and preclinical evaluation ∗ Abstract Key Points • The human-derived and antibody-like C3b-targeted fusion protein CG001 may simultaneously and effectively block 3 complement pathways. • CG001 holds high potential of further developme... |
PMC12170689 | core_pubmed_pmc | The dawn of a new era: can machine learning and large language models reshape QSP modeling? | The dawn of a new era: can machine learning and large language models reshape QSP modeling? Abstract Quantitative Systems Pharmacology (QSP) has emerged as a cornerstone of modern drug development, providing a robust framework to integrate data from preclinical and clinical studies, enhance decision-making, and optimiz... |
PMC9610999 | core_pubmed_pmc | Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B | Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B Abstract Gilteritinib, an FDA-approved tyrosine kinase inhibitor approved for the treatment of relapsed/refractory FLT3-mutated acute myeloid leukemia, is primarily eliminated via CYP3A4-mediated metabolism, a pathway that is sensi... |
PMC11292196 | core_pubmed_pmc | Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers | Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers Abstract Abstract Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin remodeling complex subunit ARID1A occur frequently in advanced urothelial, endometrial, and ovarian clear cell... |
PMC5269655 | core_pubmed_pmc | Discovery and Investigation of Natural Editing Function against Artificial Amino Acids in Protein Translation | Discovery and Investigation of Natural Editing Function against Artificial Amino Acids in Protein Translation Abstract Fluorine being not substantially present in the chemistry of living beings is an attractive element in tailoring novel chemical, biophysical, and pharmacokinetic properties of peptides and proteins. Th... |
PMC7839485 | core_pubmed_pmc | Continuous Learning in Model‐Informed Precision Dosing: A Case Study in Pediatric Dosing of Vancomycin | Continuous Learning in Model‐Informed Precision Dosing: A Case Study in Pediatric Dosing of Vancomycin Abstract Model‐informed precision dosing (MIPD) leverages pharmacokinetic (PK) models to tailor dosing to an individual patient’s needs, improving attainment of therapeutic drug exposure targets and thus potentially i... |
PMC9258944 | core_pubmed_pmc | On-Line Solid Phase Extraction High Performance Liquid Chromatography Method Coupled With Tandem Mass Spectrometry for the Therapeutic Monitoring of Cannabidiol and 7-Hydroxy-cannabidiol in Human Serum and Saliva | On-Line Solid Phase Extraction High Performance Liquid Chromatography Method Coupled With Tandem Mass Spectrometry for the Therapeutic Monitoring of Cannabidiol and 7-Hydroxy-cannabidiol in Human Serum and Saliva Abstract Cannabidiol is a novel antiseizure medication approved in Europe and the US for the treatment of s... |
PMC5527615 | core_pubmed_pmc | Linezolid Dose That Maximizes Sterilizing Effect While Minimizing Toxicity and Resistance Emergence for Tuberculosis | Linezolid Dose That Maximizes Sterilizing Effect While Minimizing Toxicity and Resistance Emergence for Tuberculosis Abstract ABSTRACT Linezolid has an excellent sterilizing effect in tuberculosis patients but high adverse event rates. The dose that would maximize efficacy and minimize toxicity is unknown. We performed... |
PMC12497745 | core_pubmed_pmc | Population pharmacokinetics modelling to predict DDI from zopiclone on clozapine in schizophrenia patients | Population pharmacokinetics modelling to predict DDI from zopiclone on clozapine in schizophrenia patients Abstract Introduction Clozapine, as a core drug for the treatment of schizophrenia, is widely used in the drug treatment of schizophrenia patients. However, when multiple drugs are used in combination, it is not c... |
PMC6437231 | core_pubmed_pmc | Population Pharmacokinetics of Semaglutide for Type 2 Diabetes | Population Pharmacokinetics of Semaglutide for Type 2 Diabetes Abstract Introduction The aim of the present analysis was to characterise the absorption, distribution and elimination of semaglutide by means of population pharmacokinetic (PK) models using data from nine clinical pharmacology trials conducted in both heal... |
PMC11859217 | core_pubmed_pmc | Compartment Model and Neural Network-Based Analysis of Combination Medication Ratios | Compartment Model and Neural Network-Based Analysis of Combination Medication Ratios Abstract Background: Combination medication strategies often involve complex interactions, making determining the appropriate pharmacodynamic component ratios challenging. Methods: This study established a time–dose relationship model ... |
PMC6624146 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of natalizumab in pediatric patients with RRMS | Pharmacokinetics and pharmacodynamics of natalizumab in pediatric patients with RRMS Abstract Abstract Objective This phase I study investigated pharmacokinetic (PK) and pharmacodynamic (PD) profiles of natalizumab in pediatric patients with relapsing-remitting MS (RRMS). Methods Pediatric patients with RRMS who were p... |
PMC6043562 | core_pubmed_pmc | Relation of Prenatal Air Pollutant and Nutritional Exposures with Biomarkers of Allergic Disease in Adolescence | Relation of Prenatal Air Pollutant and Nutritional Exposures with Biomarkers of Allergic Disease in Adolescence Abstract Prenatal exposures may be critical for immune system development, with consequences for allergic disease susceptibility. We examined associations of prenatal exposures (nutrient intakes and air pollu... |
PMC2996221 | core_pubmed_pmc | An Assessment of the Interindividual Variability of Internal Dosimetry during Multi-Route Exposure to Drinking Water Contaminants | An Assessment of the Interindividual Variability of Internal Dosimetry during Multi-Route Exposure to Drinking Water Contaminants Abstract Abstract The objective of this study was to evaluate inter-individual variability in absorbed and internal doses after multi-route exposure to drinking water contaminants (DWC) in a... |
PMC6717586 | core_pubmed_pmc | Glucocorticoids and selumetinib are highly synergistic in RAS pathway-mutated childhood acute lymphoblastic leukemia through upregulation of BIM | Glucocorticoids and selumetinib are highly synergistic in RAS pathway-mutated childhood acute lymphoblastic leukemia through upregulation of BIM Abstract Abstract New drugs are needed for the treatment of relapsed acute lymphoblastic leukemia and preclinical evaluation of the MEK inhibitor, selumetinib, has shown that ... |
PMC12672407 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Galcanezumab, an Anti‐CGRP Antibody, in Healthy Chinese Participants | Safety, Tolerability, and Pharmacokinetics of Galcanezumab, an Anti‐CGRP Antibody, in Healthy Chinese Participants Abstract Abstract Galcanezumab is used in several regions, including the United States, Europe, and China, as a preventive treatment for migraine. This study aimed to evaluate the safety, tolerability, and... |
PMC7682670 | core_pubmed_pmc | Design and rationale of two phase 3 randomised controlled trials (COUGH-1 and COUGH-2) of gefapixant, a P2X3 receptor antagonist, in refractory or unexplained chronic cough | Design and rationale of two phase 3 randomised controlled trials (COUGH-1 and COUGH-2) of gefapixant, a P2X3 receptor antagonist, in refractory or unexplained chronic cough Abstract Background We present study designs, dose selection and preliminary patient characteristics from two phase 3 clinical trials of gefapixant... |
PMC8426299 | core_pubmed_pmc | Effect of severe renal impairment on the pharmacokinetics of brigatinib | Effect of severe renal impairment on the pharmacokinetics of brigatinib Abstract Abstract Background Brigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor, targets activated, mutant forms of ALK and overcomes mechanisms of resistance to the ALK inhibitors crizotinib, ceritinib, and alectinib. Brigati... |
PMC12804539 | core_pubmed_pmc | In-silico assessment of phytochemical derivatives generated using CHEESE webserver for advancement of druggable candidate in pancreatic cancer therapy | In-silico assessment of phytochemical derivatives generated using CHEESE webserver for advancement of druggable candidate in pancreatic cancer therapy Abstract Abstract Research efforts for pancreatic cancer (PC) therapy has led to investigations of numerous therapeutic targets, yet there are still limited efficacy out... |
PMC5617436 | core_pubmed_pmc | Wogonoside inhibits IL-1β induced catabolism and hypertrophy in mouse chondrocyte and ameliorates murine osteoarthritis | Wogonoside inhibits IL-1β induced catabolism and hypertrophy in mouse chondrocyte and ameliorates murine osteoarthritis Abstract The inflammatory environment is correlated with extracellular matrix (ECM) degradation and chondrocyte hypertrophy in the development of osteoarthritis (OA). Previous studies have reported th... |
PMC12066394 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Single and Multiple Topical Applications of Sodium Taurodeoxycholate, a Treatment for Atopic Dermatitis | Safety, Tolerability, and Pharmacokinetics of Single and Multiple Topical Applications of Sodium Taurodeoxycholate, a Treatment for Atopic Dermatitis Abstract ABSTRACT Sodium taurodeoxycholate (TDCA) gel is a novel candidate for the treatment of atopic dermatitis and is currently under clinical development. TDCA is a t... |
PMC7557242 | core_pubmed_pmc | Novel Approach for Characterizing Propofol Binding Affinities to Serum Albumins from Different Species | Novel Approach for Characterizing Propofol Binding Affinities to Serum Albumins from Different Species Abstract Abstract The interaction between the main carrier (serum albumin, SA) of endogenous and exogenous compounds in the bloodstream of different species (human, bovine, canine, rat, rabbit, and sheep) and a genera... |
PMC5684313 | core_pubmed_pmc | Longrange PCR-based next-generation sequencing in pharmacokinetics and pharmacodynamics study of propofol among patients under general anaesthesia | Longrange PCR-based next-generation sequencing in pharmacokinetics and pharmacodynamics study of propofol among patients under general anaesthesia Abstract The individual response of patients to propofol results from the influence of genetic factors. However, the state of knowledge in this matter still remains insuffic... |
PMC12541016 | core_pubmed_pmc | Identification of stigmasterol derived AChE inhibitors for Alzheimer’s disease using high throughput virtual screening and molecular dynamics simulations | Identification of stigmasterol derived AChE inhibitors for Alzheimer’s disease using high throughput virtual screening and molecular dynamics simulations Abstract Abstract Alzheimer’s disease (AD), a progressive neurodegenerative disorder, poses a significant global health burden due to its intricate pathology and the ... |
PMC10142039 | core_pubmed_pmc | From Personalized to Precision Medicine in Oncology: A Model-Based Dosing Approach to Optimize Achievement of Imatinib Target Exposure | From Personalized to Precision Medicine in Oncology: A Model-Based Dosing Approach to Optimize Achievement of Imatinib Target Exposure Abstract Abstract Imatinib is a targeted cancer therapy that has significantly improved the care of patients with chronic myeloid leukemia (CML) and gastrointestinal stromal tumor (GIST... |
PMC4984800 | core_pubmed_pmc | A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies | A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies Abstract Abstract Background: The kinase activity of mTOR involves 2 multiprotein complexes, (mTORC1-mTORC2). Targeting mTORC1 with rapalogues induces compensatory feedback loops resulting in AKT/ERK a... |
PMC11111785 | core_pubmed_pmc | Quantifying combined effects of colistin and ciprofloxacin against Escherichia coli in an in silico pharmacokinetic-pharmacodynamic model | Quantifying combined effects of colistin and ciprofloxacin against Escherichia coli in an in silico pharmacokinetic-pharmacodynamic model Abstract Co-administering a low dose of colistin (CST) with ciprofloxacin (CIP) may improve the antibacterial effect against resistant Escherichia coli , offering an acceptable benef... |
PMC9293327 | core_pubmed_pmc | Exposure–Response Analyses for Therapeutic Dose Selection of Belantamab Mafodotin in Patients With Relapsed/Refractory Multiple Myeloma | Exposure–Response Analyses for Therapeutic Dose Selection of Belantamab Mafodotin in Patients With Relapsed/Refractory Multiple Myeloma Abstract Abstract Belantamab mafodotin is an antibody–drug conjugate comprising a humanized anti‐B‐cell maturation antigen (BCMA) monoclonal antibody conjugated to monomethyl auristati... |
PMC8539586 | core_pubmed_pmc | A Case of In Situ Phage Therapy against Staphylococcus aureus in a Bone Allograft Polymicrobial Biofilm Infection: Outcomes and Phage-Antibiotic Interactions | A Case of In Situ Phage Therapy against Staphylococcus aureus in a Bone Allograft Polymicrobial Biofilm Infection: Outcomes and Phage-Antibiotic Interactions Abstract Phage therapy (PT) shows promising potential in managing biofilm infections, which include refractory orthopedic infections. We report the case of a 13-y... |
PMC12489687 | core_pubmed_pmc | Pharmacokinetic Profiling and Tissue Distribution of Seven Key Saponins in Rats Following Oral Administration of Panacis Japonici Rhizoma Extracts | Pharmacokinetic Profiling and Tissue Distribution of Seven Key Saponins in Rats Following Oral Administration of Panacis Japonici Rhizoma Extracts Abstract Abstract The pharmacokinetics and distribution of natural compounds in living organisms are crucial to understanding their therapeutic potential and safety. In the ... |
PMC10582335 | core_pubmed_pmc | In vivo evaluation of the pharmacokinetic interactions between almonertinib and rivaroxaban, almonertinib and apixaban | In vivo evaluation of the pharmacokinetic interactions between almonertinib and rivaroxaban, almonertinib and apixaban Abstract Background: Almonertinib, a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), is commonly used as a first-line treatment for non-small cell lung cancer (N... |
PMC11047535 | core_pubmed_pmc | Pharmacokinetics and Nephrotoxicity of Polymyxin MRX-8 in Rats: A Novel Agent against Resistant Gram-Negative Bacteria | Pharmacokinetics and Nephrotoxicity of Polymyxin MRX-8 in Rats: A Novel Agent against Resistant Gram-Negative Bacteria Abstract Abstract MRX-8 is a novel polymyxin for carbapenem-resistant Gram-negative infections that has been recently evaluated in Phase I clinical trials. Herein, its pharmacokinetics (PK) and nephrot... |
PMC5384962 | core_pubmed_pmc | First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases | First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases Abstract Purpose PI3Ks are potential therapeutic targets in immune-inflammatory diseases. These studies aimed to investigate the safety, tolerability and PK profile of selet... |
PMC4063799 | core_pubmed_pmc | New orally active anticoagulant agents for the prevention and treatment of venous thromboembolism in cancer patients | New orally active anticoagulant agents for the prevention and treatment of venous thromboembolism in cancer patients Abstract Abstract Patients with cancer have a 6–7-fold higher risk of venous thromboembolism (VTE) as compared with non-cancer patients. Effective and safe anticoagulation for the prevention and treatmen... |
PMC8584645 | core_pubmed_pmc | NICLOSAMIDE-EXFOLIATED ANIONIC CLAY NANOHYBRID REPURPOSED AS AN ANTIVIRAL DRUG FOR TACKLING COVID-19; ORAL FORMULATION WITH TWEEN 60/EUDRAGIT S100 | NICLOSAMIDE-EXFOLIATED ANIONIC CLAY NANOHYBRID REPURPOSED AS AN ANTIVIRAL DRUG FOR TACKLING COVID-19; ORAL FORMULATION WITH TWEEN 60/EUDRAGIT S100 Abstract Abstract The ongoing pandemic, COVID-19 (SARS-CoV-2), has afflicted millions of people around the world, necessitating that the scientific community work, diligentl... |
PMC12625185 | core_pubmed_pmc | Population Pharmacokinetics Modeling of Selpercatinib to Support Posology in Pediatric Patients With RET ‐Altered Metastatic Thyroid Cancer or Solid Tumors | Population Pharmacokinetics Modeling of Selpercatinib to Support Posology in Pediatric Patients With RET ‐Altered Metastatic Thyroid Cancer or Solid Tumors Abstract ABSTRACT Selpercatinib is a first‐in‐class, highly selective, RET kinase inhibitor with CNS activity, approved for the treatment of RET‐altered lung, thyro... |
PMC10547630 | core_pubmed_pmc | Is the One-Compartment Model with First Order Absorption a Useful Approximation? | Is the One-Compartment Model with First Order Absorption a Useful Approximation? Abstract Abstract Purpose The one-compartment model with first order absorption (ka1C) has been extensively used to fit oral data. But when the disposition parameters of the drug are not available, the bias in the parameter estimates remai... |
PMC9095536 | core_pubmed_pmc | Comparative Plasma and Interstitial Tissue Fluid Pharmacokinetics of Meropenem Demonstrate the Need for Increasing Dose and Infusion Duration in Obese and Non-obese Patients | Comparative Plasma and Interstitial Tissue Fluid Pharmacokinetics of Meropenem Demonstrate the Need for Increasing Dose and Infusion Duration in Obese and Non-obese Patients Abstract Background and Objectives A quantitative evaluation of the PK of meropenem, a broad-spectrum β-lactam antibiotic, in plasma and interstit... |
PMC9780524 | core_pubmed_pmc | Bioavailability of dissolved and crushed single tablets of bictegravir, emtricitabine, tenofovir alafenamide in healthy adults: the SOLUBIC randomized crossover study | Bioavailability of dissolved and crushed single tablets of bictegravir, emtricitabine, tenofovir alafenamide in healthy adults: the SOLUBIC randomized crossover study Abstract Abstract Background Crushing or dissolving bictegravir/tenofovir alafenamide/emtricitabine (BIC/TAF/FTC) tablets is not recommended because ther... |
PMC4811836 | core_pubmed_pmc | Therapeutic Dose Monitoring for Linezolid in a Patient with MRSA Pneumonia with Bacteremia in Diabetes Insipidus | Therapeutic Dose Monitoring for Linezolid in a Patient with MRSA Pneumonia with Bacteremia in Diabetes Insipidus Abstract Introduction Few studies have investigated the effect of increased creatinine clearance (CrCl) on linezolid (LZD) concentration. Herein, we report the pharmacokinetic/pharmacodynamic (PK/PD) profile... |
PMC8645831 | core_pubmed_pmc | Delanzomib, a Novel Proteasome Inhibitor, Combined With Adalimumab Drastically Ameliorates Collagen-Induced Arthritis in Rats by Improving and Prolonging the Anti-TNF-α Effect of Adalimumab | Delanzomib, a Novel Proteasome Inhibitor, Combined With Adalimumab Drastically Ameliorates Collagen-Induced Arthritis in Rats by Improving and Prolonging the Anti-TNF-α Effect of Adalimumab Abstract Delanzomib is a novel proteasome inhibitor initially developed for treating multiple myeloma. It was found to inhibit the... |
PMC9047970 | core_pubmed_pmc | A high-throughput bioanalytical assay to support pharmacokinetic interaction study of oxycodone and diazepam in Sprague Dawley rats | A high-throughput bioanalytical assay to support pharmacokinetic interaction study of oxycodone and diazepam in Sprague Dawley rats Abstract Benzodiazepines potentiate respiratory depression when combined with an opioid leading the U.S Food and Drug Administration (FDA) to recommend updating the labels of these product... |
PMC7970569 | core_pubmed_pmc | Effect of Disease State on the Pharmacokinetics of Bedaquiline in Renal-Impaired and Diabetic Rats | Effect of Disease State on the Pharmacokinetics of Bedaquiline in Renal-Impaired and Diabetic Rats Abstract Bedaquiline (TMC-207) is a key anti-tubercular drug to fight against multidrug resistance tuberculosis. Little information is available till date on the impact of any disease state toward its pharmacokinetic beha... |
PMC8847520 | core_pubmed_pmc | Does Prolonged Infusion Time Really Improve the Efficacy of Meropenem Therapy? A Prospective Study in Critically Ill Patients | Does Prolonged Infusion Time Really Improve the Efficacy of Meropenem Therapy? A Prospective Study in Critically Ill Patients Abstract Introduction Meropenem is a carbapenem antibiotic, which has demonstrated excellent antimicrobial activity against gram-negative clinical isolates. It is also commonly used in criticall... |
PMC9797969 | core_pubmed_pmc | Evaluation of drug-drug interaction between rilpivirine and rifapentine using PBPK modelling | Evaluation of drug-drug interaction between rilpivirine and rifapentine using PBPK modelling Abstract Abstract Tuberculosis remains the leading cause of death among people living with HIV. Rifapentine is increasingly used to treat active disease or prevent reactivation, in both cases given either as weekly or daily the... |
PMC7668473 | core_pubmed_pmc | Population pharmacokinetics and dosing optimization of metformin in Chinese patients with type 2 diabetes mellitus | Population pharmacokinetics and dosing optimization of metformin in Chinese patients with type 2 diabetes mellitus Abstract Abstract Approximately 35% of patients fail to attain ideal initial blood glucose control under metformin monotherapy. The objective of this observational study is to simulate the optimal protocol... |
PMC11263521 | core_pubmed_pmc | Subcutaneous Levodopa: A New Engine for the Vintage Molecule | Subcutaneous Levodopa: A New Engine for the Vintage Molecule Abstract Abstract The management of Parkinson’s disease (PD) continues to evolve with advancements in non-oral levodopa-based therapies aiming to provide continuous drug delivery (CDD). Such therapies address the challenges posed by the emergence of motor flu... |
PMC12298815 | core_pubmed_pmc | Oral Metronomic Delivery of Atorvastatin and Docetaxel via Transporter-Targeted Nanoemulsions Enhances Antitumor Efficacy and Immune Modulation in Colon Cancer | Oral Metronomic Delivery of Atorvastatin and Docetaxel via Transporter-Targeted Nanoemulsions Enhances Antitumor Efficacy and Immune Modulation in Colon Cancer Abstract Abstract Background/Objectives : This study aimed to enhance the oral delivery and therapeutic synergy of atorvastatin (AT) and docetaxel (DT) through ... |
PMC8216263 | core_pubmed_pmc | Pharmacokinetics of gallic acid and protocatechuic acid in humans after dosing with Relinqing (RLQ) and the potential for RLQ-perpetrated drug–drug interactions on organic anion transporter (OAT) 1/3 | Pharmacokinetics of gallic acid and protocatechuic acid in humans after dosing with Relinqing (RLQ) and the potential for RLQ-perpetrated drug–drug interactions on organic anion transporter (OAT) 1/3 Abstract Abstract Context Relinqing granules (RLQ) are being used alone or in combination with antibacterial drugs to tr... |
PMC8938880 | core_pubmed_pmc | Serial measurement of M. tuberculosis in blood from critically-ill patients with HIV-associated tuberculosis | Serial measurement of M. tuberculosis in blood from critically-ill patients with HIV-associated tuberculosis Abstract Summary Background Despite being highly prevalent in hospitalised patients with severe HIV-associated tuberculosis (TB) and sepsis, little is known about the mycobacteriology of Mycobacterium tuberculos... |
PMC4065469 | core_pubmed_pmc | Development of novel risperidone implants using blends of polycaprolactones and in vitro in vivo correlation studies | Development of novel risperidone implants using blends of polycaprolactones and in vitro in vivo correlation studies Abstract Abstract The objective of this study was to develop a novel implant containing risperidone intended for long-term treatment in Schizophrenia utilizing in vitro in vivo correlation (IVIVC) studie... |
PMC10672599 | core_pubmed_pmc | Drug Clearance in Patients with Inflammatory Bowel Disease Treated with Biologics | Drug Clearance in Patients with Inflammatory Bowel Disease Treated with Biologics Abstract Abstract Biological therapy is very effective for treating patients with moderate to severe inflammatory bowel disease (IBD). However, up to 40% can have primary non-response, and up to 50% of the patients can experience a loss o... |
PMC7684313 | core_pubmed_pmc | In vitro and in vivo pharmacological activity of minor cannabinoids isolated from Cannabis sativa | In vitro and in vivo pharmacological activity of minor cannabinoids isolated from Cannabis sativa Abstract Abstract The Cannabis sativa plant contains more than 120 cannabinoids. With the exceptions of ∆ 9 -tetrahydrocannabinol (∆ 9 -THC) and cannabidiol (CBD), comparatively little is known about the pharmacology of th... |
PMC6068438 | core_pubmed_pmc | Phase I safety and pharmacokinetic study of cipatinib, an original dual tyrosine kinase inhibitor | Phase I safety and pharmacokinetic study of cipatinib, an original dual tyrosine kinase inhibitor Abstract Background Cipatinib is a novel tyrosine kinase inhibitor against both EGFR and HER2/neu . This phase I trial was conducted to assess the safety, dose‐limiting toxicities (DLTs), and maximum‐tolerated dose of cipa... |
PMC10289903 | core_pubmed_pmc | A phase Ib study of adavosertib, a selective Wee1 inhibitor, in patients with locally advanced or metastatic solid tumors | A phase Ib study of adavosertib, a selective Wee1 inhibitor, in patients with locally advanced or metastatic solid tumors Abstract Abstract Adavosertib selectively inhibits Wee1, which regulates intra-S and G2/M cell-cycle checkpoints. This study investigated dosing schedules for adavosertib monotherapy, determining th... |
PMC8520746 | core_pubmed_pmc | Pharmacokinetic modeling of R and S‐Methadone and their metabolites to study the effects of various covariates in post‐operative children | Pharmacokinetic modeling of R and S‐Methadone and their metabolites to study the effects of various covariates in post‐operative children Abstract Abstract Methadone is a synthetic opioid used as an analgesic and for the treatment of opioid abuse disorder. The analgesic dose in the pediatric population is not well‐defi... |
PMC10087065 | core_pubmed_pmc | A mechanistic PK / PD model to enable dose selection of the potent anti‐tryptase antibody ( MTPS9579A ) in patients with moderate‐to‐severe asthma | A mechanistic PK / PD model to enable dose selection of the potent anti‐tryptase antibody ( MTPS9579A ) in patients with moderate‐to‐severe asthma Abstract Abstract Tryptase, a protease implicated in asthma pathology, is secreted from mast cells upon activation during an inflammatory allergic response. MTPS9579A is a n... |
PMC12037183 | core_pubmed_pmc | The Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Subcutaneous Administration of a Novel Anti-NGF Monoclonal Antibody (AK115) in Healthy Participants: A Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Phase I Clinical Trial | The Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Subcutaneous Administration of a Novel Anti-NGF Monoclonal Antibody (AK115) in Healthy Participants: A Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Phase I Clinical Trial Abstract Abstract Objective This study aimed to investigat... |
PMC9335275 | core_pubmed_pmc | A long-acting C-natriuretic peptide for achondroplasia | A long-acting C-natriuretic peptide for achondroplasia Abstract Significance The C-natriuretic peptide (CNP) analog vosoritide has recently been approved for the treatment of achondroplasia in children. However, the dosing regimen is burdensome, requiring daily subcutaneous injections in pediatric patients over multipl... |
PMC11638133 | core_pubmed_pmc | Dose‐exposure‐response of CARDALIS® (benazepril/spironolactone) on the classical and alternative arms of the renin‐angiotensin‐aldosterone system in healthy dogs | Dose‐exposure‐response of CARDALIS® (benazepril/spironolactone) on the classical and alternative arms of the renin‐angiotensin‐aldosterone system in healthy dogs Abstract Abstract Background Benazepril exhibits a dose‐dependent effect on biomarkers of the circulating renin‐angiotensin‐aldosterone system (RAAS) in dogs.... |
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