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PMC3141160
core_pubmed_pmc
Failed rapid sequence induction in an achondroplastic dwarf
Failed rapid sequence induction in an achondroplastic dwarf Abstract Abstract Achondroplasia, a common cause of short limbed type of dwarfism is due to quantitative decrease in rate of endochondral ossification. This abnormal bone growth leads to disproportionate body and head structure, thus placing them under high ri...
PMC3527132
core_pubmed_pmc
Safety and pharmacodynamic effects of a pharmacological chaperone on α-galactosidase A activity and globotriaosylceramide clearance in Fabry disease: report from two phase 2 clinical studies
Safety and pharmacodynamic effects of a pharmacological chaperone on α-galactosidase A activity and globotriaosylceramide clearance in Fabry disease: report from two phase 2 clinical studies Abstract Background Fabry disease (FD) is a genetic disorder resulting from deficiency of the lysosomal enzyme α-galactosidase A ...
PMC9717595
core_pubmed_pmc
Population Pharmacokinetics of Levofloxacin and Moxifloxacin, and the Probability of Target Attainment in Ethiopian Patients with Multidrug-Resistant Tuberculosis
Population Pharmacokinetics of Levofloxacin and Moxifloxacin, and the Probability of Target Attainment in Ethiopian Patients with Multidrug-Resistant Tuberculosis Abstract Objective This study aimed to explore the population pharmacokinetic modeling (PopPK) of levofloxacin (LFX) and moxifloxacin (MXF), as well as the p...
PMC7238265
core_pubmed_pmc
Exposure-Response and Clinical Outcome Modeling of Inhaled Budesonide/Formoterol Combination in Asthma Patients
Exposure-Response and Clinical Outcome Modeling of Inhaled Budesonide/Formoterol Combination in Asthma Patients Abstract Abstract Exposure-response and clinical outcome (CO) model for inhaled budesonide/formoterol was developed to quantify the relationship among pharmacokinetics (PK), pharmacodynamics (PD) and CO of th...
PMC7246321
core_pubmed_pmc
Comparison of the Pharmacokinetics of Highly Variable Drugs in Healthy Subjects Using a Partial Replicated Crossover Study: A Fixed-Dose Combination of Fimasartan 120 mg and Atorvastatin 40 mg versus Separate Tablets
Comparison of the Pharmacokinetics of Highly Variable Drugs in Healthy Subjects Using a Partial Replicated Crossover Study: A Fixed-Dose Combination of Fimasartan 120 mg and Atorvastatin 40 mg versus Separate Tablets Abstract Abstract Purpose A fixed-dose combination (FDC) of fimasartan and atorvastatin is used to tr...
PMC6231259
core_pubmed_pmc
Rivaroxaban plasma levels in patients admitted for bleeding events: insights from a prospective study
Rivaroxaban plasma levels in patients admitted for bleeding events: insights from a prospective study Abstract Abstract Background Serious bleeding events have been frequently described in patients taking direct oral anticoagulants (DOAC). In secondary analyses of phase 3 trials, DOAC plasma concentrations were shown t...
PMC12324035
core_pubmed_pmc
Impact of Extending Beta-Lactam Infusions on IV Access Requirements
Impact of Extending Beta-Lactam Infusions on IV Access Requirements Abstract Abstract This study aimed to determine if extended infusion (EI; over > 3 hr) beta-lactam therapy increased IV access requirements compared with traditional dosing (TD; over 30 min). Eighty-six adult ICU patients treated with TD anti-pseudomon...
PMC10222168
core_pubmed_pmc
The Effect of Intracellular Tacrolimus Exposure on Calcineurin Inhibition in Immediate- and Extended-Release Tacrolimus Formulations
The Effect of Intracellular Tacrolimus Exposure on Calcineurin Inhibition in Immediate- and Extended-Release Tacrolimus Formulations Abstract Abstract Despite intensive monitoring of whole blood tacrolimus concentrations, acute rejection after kidney transplantation occurs during tacrolimus therapy. Intracellular tacro...
PMC10681461
core_pubmed_pmc
Clinical decision support for chemotherapy‐induced neutropenia using a hybrid pharmacodynamic/machine learning model
Clinical decision support for chemotherapy‐induced neutropenia using a hybrid pharmacodynamic/machine learning model Abstract Abstract Consensus guidelines recommend use of granulocyte colony stimulating factor in patients deemed at risk of chemotherapy‐induced neutropenia, however, these risk models are limited in the...
PMC11964056
core_pubmed_pmc
Novel Relaxin Receptor RXFP1 Agonist AZD3427 in the Treatment of Heart Failure: A Phase 1a/b, First‐in‐Human, Randomized, Single‐Blind, Placebo‐Controlled Study
Novel Relaxin Receptor RXFP1 Agonist AZD3427 in the Treatment of Heart Failure: A Phase 1a/b, First‐in‐Human, Randomized, Single‐Blind, Placebo‐Controlled Study Abstract Background Heart failure mortality remains high despite recent progress in pharmacological treatment. AZD3427 is a selective long‐acting analog of rel...
PMC12795415
core_pubmed_pmc
Adaptive optics stimulated Raman scattering microscopy for topical product pharmacokinetic imaging
Adaptive optics stimulated Raman scattering microscopy for topical product pharmacokinetic imaging Abstract Abstract Topically applied drug products are used to treat various dermatological conditions, enabling local and targeted delivery of active pharmaceutical ingredients. To ensure appropriate topical drug efficacy...
PMC10218847
core_pubmed_pmc
Human Hemoglobin and Antipsychotics Clozapine, Ziprasidone and Sertindole: Friends or Foes?
Human Hemoglobin and Antipsychotics Clozapine, Ziprasidone and Sertindole: Friends or Foes? Abstract Abstract Packed with hemoglobin, an essential protein for oxygen transport, human erythrocytes are a suitable model system for testing the pleiotropic effects of lipophilic drugs. Our study investigated the interaction ...
PMC8779995
core_pubmed_pmc
Metabolic Soft Spot and Pharmacokinetics: Functionalization of C-3 Position of an Eph–Ephrin Antagonist Featuring a Bile Acid Core as an Effective Strategy to Obtain Oral Bioavailability in Mice
Metabolic Soft Spot and Pharmacokinetics: Functionalization of C-3 Position of an Eph–Ephrin Antagonist Featuring a Bile Acid Core as an Effective Strategy to Obtain Oral Bioavailability in Mice Abstract Abstract UniPR129, an L-β-homotryptophan conjugate of the secondary bile acid lithocholic acid (LCA), acts as an eff...
PMC4859860
core_pubmed_pmc
Phase 1 study of pembrolizumab (MK-3475; anti-PD-1 monoclonal antibody) in Japanese patients with advanced solid tumors
Phase 1 study of pembrolizumab (MK-3475; anti-PD-1 monoclonal antibody) in Japanese patients with advanced solid tumors Abstract Summary Background This phase I study evaluated the safety and tolerability, pharmacokinetics and pharmacodynamics, immunogenicity, and antitumor activity of pembrolizumab in Japanese patient...
PMC8646094
core_pubmed_pmc
Physiologically Based Modeling of the Effect of Physiological and Anthropometric Variability on Indocyanine Green Based Liver Function Tests
Physiologically Based Modeling of the Effect of Physiological and Anthropometric Variability on Indocyanine Green Based Liver Function Tests Abstract Abstract Accurate evaluation of liver function is a central task in hepatology. Dynamic liver function tests (DLFT) based on the time-dependent elimination of a test subs...
PMC5698362
core_pubmed_pmc
Mizoribine therapy combined with steroids and mizoribine blood concentration monitoring for idiopathic membranous nephropathy with steroid-resistant nephrotic syndrome
Mizoribine therapy combined with steroids and mizoribine blood concentration monitoring for idiopathic membranous nephropathy with steroid-resistant nephrotic syndrome Abstract Abstract Background We designed a prospective and randomized trial of mizoribine (MZR) therapy combined with prednisolone (PSL) for idiopathic ...
PMC11415237
core_pubmed_pmc
A framework for multi-scale intervention modeling: virtual cohorts, virtual clinical trials, and model-to-model comparisons
A framework for multi-scale intervention modeling: virtual cohorts, virtual clinical trials, and model-to-model comparisons Abstract Abstract Computational models of disease progression have been constructed for a myriad of pathologies. Typically, the conceptual implementation for pathology-related in silico interventi...
PMC6496063
core_pubmed_pmc
Considerations for Dose Selection and Clinical Pharmacokinetics/Pharmacodynamics for the Development of Antibacterial Agents
Considerations for Dose Selection and Clinical Pharmacokinetics/Pharmacodynamics for the Development of Antibacterial Agents Abstract In June 2017, The National Institute of Allergy and Infectious Diseases, part of the National Institutes of Health, organized a workshop entitled “Pharmacokinetics-Pharmacodynamics (PK/P...
PMC9146184
core_pubmed_pmc
Liver Injury with Nintedanib: A Pharmacovigilance–Pharmacokinetic Appraisal
Liver Injury with Nintedanib: A Pharmacovigilance–Pharmacokinetic Appraisal Abstract Abstract Drug-induced liver injury (DILI) with nintedanib has emerged as an adverse event of special interest in premarketing clinical trials. We characterized DILI with nintedanib in the real world and explored the underlying pharmaco...
PMC9974508
core_pubmed_pmc
Photoactivatable nanoagonists chemically programmed for pharmacokinetic tuning and in situ cancer vaccination
Photoactivatable nanoagonists chemically programmed for pharmacokinetic tuning and in situ cancer vaccination Abstract Significance Cancer immunotherapy based on T cell checkpoint blockade only shows response in a subset of patients due to immunosuppressive tumor microenvironment. Poor pharmacokinetic properties and un...
PMC10224337
core_pubmed_pmc
Lipid Emulsion to Treat Acute Poisonings: Mechanisms of Action, Indications, and Controversies
Lipid Emulsion to Treat Acute Poisonings: Mechanisms of Action, Indications, and Controversies Abstract Abstract Biodetoxification using intravenous lipid emulsion (ILE) in acute poisoning is of growing interest. As well as for local anesthetics, ILE is currently used to reverse toxicity caused by a broad-spectrum of l...
PMC6251026
core_pubmed_pmc
pRAD50: a novel and clinically applicable pharmacodynamic biomarker of both ATM and ATR inhibition identified using mass spectrometry and immunohistochemistry
pRAD50: a novel and clinically applicable pharmacodynamic biomarker of both ATM and ATR inhibition identified using mass spectrometry and immunohistochemistry Abstract Background AZD0156 and AZD6738 are potent and selective inhibitors of ataxia-telangiectasia-kinase (ATM) and ataxia-telangiectasia-mutated and Rad3-rela...
PMC9865692
core_pubmed_pmc
Analytical Method Development of Benzisothiazolinone, a Biocide, Using LC–MS/MS and a Pharmacokinetic Application in Rat Biological Matrices
Analytical Method Development of Benzisothiazolinone, a Biocide, Using LC–MS/MS and a Pharmacokinetic Application in Rat Biological Matrices Abstract Benzisothiazolinone (BIT), a biocide widely used as a preservative in household cleaning and personal care products, is cytotoxic to lung cells and a known skin allergen ...
PMC11597508
core_pubmed_pmc
Advancements in Virtual Bioequivalence: A Systematic Review of Computational Methods and Regulatory Perspectives in the Pharmaceutical Industry
Advancements in Virtual Bioequivalence: A Systematic Review of Computational Methods and Regulatory Perspectives in the Pharmaceutical Industry Abstract Abstract Background/Objectives: The rise of virtual bioequivalence studies has transformed the pharmaceutical landscape, enabling more efficient drug development proce...
PMC5982397
core_pubmed_pmc
Evaluation of Meropenem Pharmacokinetics in an Experimental Acute Respiratory Distress Syndrome (ARDS) Model during Extracorporeal Membrane Oxygenation (ECMO) by Using a PenP β -Lactamase Biosensor
Evaluation of Meropenem Pharmacokinetics in an Experimental Acute Respiratory Distress Syndrome (ARDS) Model during Extracorporeal Membrane Oxygenation (ECMO) by Using a PenP β -Lactamase Biosensor Abstract Abstract Introduction: The use of antibiotics is mandatory in patients during extracorporeal membrane oxygenation...
PMC11578122
core_pubmed_pmc
Interim analysis, a tool to enhance efficiency of pharmacokinetic studies: Pharmacokinetics of rifampicin in lactating mother–infant pairs
Interim analysis, a tool to enhance efficiency of pharmacokinetic studies: Pharmacokinetics of rifampicin in lactating mother–infant pairs Abstract Abstract Pharmacokinetic studies are important for understanding drug disposition in the human body. However, pregnant and lactating women are often excluded from primary p...
PMC11222182
core_pubmed_pmc
Population Pharmacokinetics of Cabozantinib in Metastatic Renal Cell Carcinoma Patients: Towards Drug Expenses Saving Regimens
Population Pharmacokinetics of Cabozantinib in Metastatic Renal Cell Carcinoma Patients: Towards Drug Expenses Saving Regimens Abstract Introduction Cabozantinib is one of the preferred treatment options in the latest metastatic renal cell carcinoma (mRCC) guidelines. Cabozantinib is also associated with high drug expe...
PMC7766516
core_pubmed_pmc
Allometric Optimization of Enrofloxacin Dosage in Growing Male Turkeys: Empirical Evidence for Improved Internal Exposure
Allometric Optimization of Enrofloxacin Dosage in Growing Male Turkeys: Empirical Evidence for Improved Internal Exposure Abstract Abstract Rapid weight gain in turkeys causes a major change in the pharmacokinetics of drugs, leading to age-dependent variability in the internal exposure and, possibly, treatment failure ...
PMC11731019
core_pubmed_pmc
Effectiveness of PK-Guided Personalized Recombinant FVIII Treatment in Patients with Hemophilia A: Clinical Case Experiences Based on an Observational Study
Effectiveness of PK-Guided Personalized Recombinant FVIII Treatment in Patients with Hemophilia A: Clinical Case Experiences Based on an Observational Study Abstract Abstract Purpose Prophylaxis with recombinant factor VIII (rFVIII) products is the gold-standard treatment for hemophilia A. However, interindividual diff...
PMC8839712
core_pubmed_pmc
The Therapeutic Effect of Acanthopanax senticosus Components on Radiation-Induced Brain Injury Based on the Pharmacokinetics and Neurotransmitters
The Therapeutic Effect of Acanthopanax senticosus Components on Radiation-Induced Brain Injury Based on the Pharmacokinetics and Neurotransmitters Abstract Acanthopanax senticosus (AS) is a medicinal and food homologous plant with many biological activities. In this research, we generated a brain injury model by 60 Co ...
PMC9511055
core_pubmed_pmc
Anti-asthmatic fraction screening and mechanisms prediction of Schisandrae Sphenantherae Fructus based on a combined approach
Anti-asthmatic fraction screening and mechanisms prediction of Schisandrae Sphenantherae Fructus based on a combined approach Abstract Objective: Schisandrae Sphenantherae Fructus (SSF) is a traditional Chinese medicine used to treat coughs and pulmonary inflammatory diseases. However, the pharmacodynamic material basi...
PMC12765256
core_pubmed_pmc
In vivo analysis techniques for antibody drug: Recent advances and methodological insights
In vivo analysis techniques for antibody drug: Recent advances and methodological insights Abstract Abstract Antibody drugs, such as monoclonal antibodies and antibody-drug conjugates, have shown significant potential in treating diseases due to their high specificity and affinity. In vivo analysis of antibody drugs wi...
PMC11869157
core_pubmed_pmc
Baseline Drug Clearance Predicts Outcomes in Children With Inflammatory Bowel Disease Treated With Vedolizumab: Results From the VedoKids Prospective Multicentre Study
Baseline Drug Clearance Predicts Outcomes in Children With Inflammatory Bowel Disease Treated With Vedolizumab: Results From the VedoKids Prospective Multicentre Study Abstract ABSTRACT Background The pharmacokinetics of biologic agents can differ between children and adults with inflammatory bowel disease (IBD), often...
PMC4391595
core_pubmed_pmc
Revisiting loxapine: a systematic review
Revisiting loxapine: a systematic review Abstract Abstract Loxapine is an antipsychotic used in psychiatry for over 40 years with a well-established profile. Loxapine is a dibenzoxazepine tricyclic antipsychotic agent, available for oral, intramuscular and inhalatory administration. In the light of the recent approval ...
PMC10860405
core_pubmed_pmc
Pediatric oncology drug development and dosage optimization
Pediatric oncology drug development and dosage optimization Abstract Abstract Oncology drug discovery and development has always been an area facing many challenges. Phase 1 oncology studies are typically small, open-label, sequential studies enrolling a small sample of adult patients (i.e., 3-6 patients/cohort) in dos...
PMC8905578
core_pubmed_pmc
Pharmacokinetic Modeling of [ 11 C]GSK-189254, PET Tracer Targeting H 3 Receptors, in Rat Brain
Pharmacokinetic Modeling of [ 11 C]GSK-189254, PET Tracer Targeting H 3 Receptors, in Rat Brain Abstract Abstract The histamine H 3 receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective...
PMC8813043
core_pubmed_pmc
An intravitreal implant injection method for sustained drug delivery into mouse eyes
An intravitreal implant injection method for sustained drug delivery into mouse eyes Abstract Summary Using small molecule drugs to treat eye diseases carries benefits of specificity, scalability, and transportability, but their efficacy is significantly limited by a fast intraocular clearance rate. Ocular drug implant...
PMC11959343
core_pubmed_pmc
Pharmacokinetics of sulfur-containing compounds in aged garlic extract: S -Allylcysteine, S -1-propenylcysteine, S -methylcysteine, S -allylmercaptocysteine and others (Review)
Pharmacokinetics of sulfur-containing compounds in aged garlic extract: S -Allylcysteine, S -1-propenylcysteine, S -methylcysteine, S -allylmercaptocysteine and others (Review) Abstract Abstract Aged garlic extract (AGE) is produced by aging raw garlic ( Allium sativum L. ) in an alcoholic solution for >10 months. AGE ...
PMC8828382
core_pubmed_pmc
Evidence-based dosing of convalescent plasma for COVID-19 in future trials
Evidence-based dosing of convalescent plasma for COVID-19 in future trials Abstract Background Two years into the pandemic, convincing evidence in favour of convalescent plasma (ConvP) as a treatment for coronavirus disease 2019 (COVID-19) is still lacking. This contrasts sharply with the efficacy of potent virus-neutr...
PMC4006523
core_pubmed_pmc
Assessment of pharmacokinetic changes of meropenem during therapy in septic critically ill patients
Assessment of pharmacokinetic changes of meropenem during therapy in septic critically ill patients Abstract Background Meropenem is a carbapenem antibiotic commonly used in critically ill patients to treat severe infections. The available pharmacokinetic (PK) data has been mostly obtained from healthy volunteers as we...
PMC8745431
core_pubmed_pmc
Circulating Nucleic Acid-Based Biomarkers of Type 2 Diabetes
Circulating Nucleic Acid-Based Biomarkers of Type 2 Diabetes Abstract Abstract Type 2 diabetes (T2D) is a deficiency in how the body regulates glucose. Uncontrolled T2D will result in chronic high blood sugar levels, eventually resulting in T2D complications. These complications, such as kidney, eye, and nerve damage, ...
PMC12799758
core_pubmed_pmc
A Nonparametric Approach to Practical Identifiability of Nonlinear Mixed Effects Models
A Nonparametric Approach to Practical Identifiability of Nonlinear Mixed Effects Models Abstract Mathematical modelling is a widely used approach to understand and interpret clinical trial data. This modelling typically involves fitting mechanistic mathematical models to data from individual trial participants. Despite...
PMC6386724
core_pubmed_pmc
Humanized UGT2 and CYP3A transchromosomic rats for improved prediction of human drug metabolism
Humanized UGT2 and CYP3A transchromosomic rats for improved prediction of human drug metabolism Abstract Significance Genomically humanized animals overcoming species differences are invaluable for biomedical research. Although rats would be preferred over mice for several applications, generation of a humanized model ...
PMC6373543
core_pubmed_pmc
Pharmacokinetics of HIV-Integrase Inhibitors During Pregnancy: Mechanisms, Clinical Implications and Knowledge Gaps
Pharmacokinetics of HIV-Integrase Inhibitors During Pregnancy: Mechanisms, Clinical Implications and Knowledge Gaps Abstract Abstract Prevention of mother-to-child transmission of HIV and optimal maternal treatment are the most important goals of antiretroviral therapy in pregnant women with HIV. These goals may be at ...
PMC5648746
core_pubmed_pmc
Population Pharmacokinetic Analysis of Ixazomib, an Oral Proteasome Inhibitor, Including Data from the Phase III TOURMALINE-MM1 Study to Inform Labelling
Population Pharmacokinetic Analysis of Ixazomib, an Oral Proteasome Inhibitor, Including Data from the Phase III TOURMALINE-MM1 Study to Inform Labelling Abstract Ixazomib is an oral proteasome inhibitor, approved in USA, Canada, Australia and Europe in combination with lenalidomide and dexamethasone, for the treatment...
PMC11321340
core_pubmed_pmc
Rational In Silico Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket
Rational In Silico Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket Abstract TMPRSS6 is a potential therapeutic target for the treatment of iron overload due to its role in regulating levels of hepcidin. Although potent TMPRSS6 inhibitors have been previously developed, their l...
PMC6311967
core_pubmed_pmc
Assessment of acute kidney injury in neurologically and traumatically injured intensive care patients receiving large vancomycin doses
Assessment of acute kidney injury in neurologically and traumatically injured intensive care patients receiving large vancomycin doses Abstract Abstract Background: Previous reports note that in a mixed patient population, vancomycin doses >4 g/day are associated with increased rates of acute kidney injury (AKI). Objec...
PMC6039306
core_pubmed_pmc
Comparative efficacy, toxicity and biodistribution of the liposomal amphotericin B formulations Fungisome ® and AmBisome ® in murine cutaneous leishmaniasis
Comparative efficacy, toxicity and biodistribution of the liposomal amphotericin B formulations Fungisome ® and AmBisome ® in murine cutaneous leishmaniasis Abstract Fungisome ® (F), a liposomal amphotericin B (AmB) product, is marketed in India as a safe and effective therapeutic for the parasitic infection visceral l...
PMC5845223
core_pubmed_pmc
Continuous hypoxia reduces the concentration of streptomycin in the blood
Continuous hypoxia reduces the concentration of streptomycin in the blood Abstract Background A high incidence and mortality of plague in the past two decades occurred in the Qinghai-Tibet Plateau, China. High dose streptomycin (6–8 g/d) remained the first practical strategy for controlling the progressive, vicious cli...
PMC7774308
core_pubmed_pmc
Semi-Mechanistic Modeling of HY-021068 Based on Irreversible Inhibition of Thromboxane Synthetase
Semi-Mechanistic Modeling of HY-021068 Based on Irreversible Inhibition of Thromboxane Synthetase Abstract Background: HY-021068 [4-(2-(1H-imidazol-1-yl) ethoxy)-3-methoxybenzoate], developed by Hefei Industrial Pharmaceutical Institute Co., Ltd. (Anhui, China), is a potential thromboxane synthetase inhibitor under dev...
PMC3575161
core_pubmed_pmc
A novel drug–phospholipid complex enriched with micelles: preparation and evaluation in vitro and in vivo
A novel drug–phospholipid complex enriched with micelles: preparation and evaluation in vitro and in vivo Abstract Mixed micelles are widely used to increase solubility and bioavailability of poorly soluble drugs. One promising antitumor drug candidate is 20(S)-protopanaxadiol (PPD), although its clinical application i...
PMC8619476
core_pubmed_pmc
Molecular Insights into Binding Mode and Interactions of Structure-Based Virtually Screened Inhibitors for Pseudomonas aeruginosa Multiple Virulence Factor Regulator (MvfR)
Molecular Insights into Binding Mode and Interactions of Structure-Based Virtually Screened Inhibitors for Pseudomonas aeruginosa Multiple Virulence Factor Regulator (MvfR) Abstract Multi-drug resistance (MDR) bacterial pathogens pose a threat to global health and warrant the discovery of new therapeutic molecules, par...
PMC10684409
core_pubmed_pmc
Evolution of Ritlecitinib Population Pharmacokinetic Models During Clinical Drug Development
Evolution of Ritlecitinib Population Pharmacokinetic Models During Clinical Drug Development Abstract Background Ritlecitinib is an oral Janus kinase 3/tyrosine kinase expressed in hepatocellular carcinoma family inhibitor undergoing parallel clinical development for alopecia areata, vitiligo, ulcerative colitis, Crohn...
PMC10598009
core_pubmed_pmc
Population pharmacokinetic modeling of multiple-dose intravenous fosfomycin in critically ill patients during continuous venovenous hemodialysis
Population pharmacokinetic modeling of multiple-dose intravenous fosfomycin in critically ill patients during continuous venovenous hemodialysis Abstract Abstract The aim of this study was to investigate the pharmacokinetics of multiple-dose intravenous (i.v.) fosfomycin in critically ill patients during continuous ven...
PMC12670296
core_pubmed_pmc
Pharmacokinetics and Toxicity of Dimethylacetamide and Its Metabolite in Pediatric Patients Treated With High Dose Intravenous Busulphan
Pharmacokinetics and Toxicity of Dimethylacetamide and Its Metabolite in Pediatric Patients Treated With High Dose Intravenous Busulphan Abstract ABSTRACT N,N‐dimethylacetamide (DMA) is an organic solvent, used in busulphan, iv‐formulation, (Busulfex). DMA is metabolized primarily to N‐methylacetamide (MMA) via CYP2E1....
PMC9413113
core_pubmed_pmc
Real-Life Therapeutic Concentration Monitoring of Long-Acting Cabotegravir and Rilpivirine: Preliminary Results of an Ongoing Prospective Observational Study in Switzerland
Real-Life Therapeutic Concentration Monitoring of Long-Acting Cabotegravir and Rilpivirine: Preliminary Results of an Ongoing Prospective Observational Study in Switzerland Abstract Abstract SHCS#879 is an ongoing Switzerland-wide multicenter observational study conducted within the Swiss HIV Cohort Study (SHCS) for th...
PMC6060703
core_pubmed_pmc
Folate receptor-targeted mixed polysialic acid micelles for combating rheumatoid arthritis: in vitro and in vivo evaluation
Folate receptor-targeted mixed polysialic acid micelles for combating rheumatoid arthritis: in vitro and in vivo evaluation Abstract Abstract Objective: Rheumatoid arthritis (RA) is associated with chronic inflammation. The suppression of inflammation is key to the treatment of RA. Glucocorticoids (GCs) are classical a...
PMC8754666
core_pubmed_pmc
UPLC-MS/MS Method for Simultaneous Determination of 14 Antimicrobials in Human Plasma and Cerebrospinal Fluid: Application to Therapeutic Drug Monitoring
UPLC-MS/MS Method for Simultaneous Determination of 14 Antimicrobials in Human Plasma and Cerebrospinal Fluid: Application to Therapeutic Drug Monitoring Abstract Abstract Pharmacokinetics/pharmacodynamics is the foundation for guiding the rational application of antibiotics in clinical practice, so it is necessary to ...
PMC3719006
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and pharmacodynamics of a long-acting release (LAR) formulation of pasireotide (SOM230) in patients with gastroenteropancreatic neuroendocrine tumors: results from a randomized, multicenter, open-label, phase I study
Safety, tolerability, pharmacokinetics, and pharmacodynamics of a long-acting release (LAR) formulation of pasireotide (SOM230) in patients with gastroenteropancreatic neuroendocrine tumors: results from a randomized, multicenter, open-label, phase I study Abstract Purpose Pasireotide (SOM230), a novel multireceptor li...
PMC2964772
core_pubmed_pmc
Preparation, Characterization and in vivo Evaluation of Parenteral Sustained Release Microsphere Formulation of Zopiclone
Preparation, Characterization and in vivo Evaluation of Parenteral Sustained Release Microsphere Formulation of Zopiclone Abstract The aim of this study was to prepare zopiclone-loaded polycaprolactone microspheres by emulsion solvent evaporation technique with different drug-to-carrier ratios {MP 1 (1:1), MP 2 (1:2), ...
PMC12275926
core_pubmed_pmc
Self-Assembled Nanoplatform with pH/NIR Light-Responsive Drug Delivery for Combined Therapy of Glioma in vitro
Self-Assembled Nanoplatform with pH/NIR Light-Responsive Drug Delivery for Combined Therapy of Glioma in vitro Abstract Purpose The integration of multifunctional components into a single nanoplatform offers significant potential for personalized and minimally invasive therapeutic applications. Herein, we present a fac...
PMC12138356
core_pubmed_pmc
Remimazolam, a novel drug, for safe and effective endoscopic sedation
Remimazolam, a novel drug, for safe and effective endoscopic sedation Abstract Remimazolam is a novel benzodiazepine with unique pharmacokinetic and pharmacodynamic properties, making it an ideal candidate for sedation during endoscopic procedures. Distinguished by its rapid onset and short duration of action, remimazo...
PMC6989252
core_pubmed_pmc
Prediction of the human in vivo antiplatelet effect of S- and R-indobufen using population pharmacodynamic modeling and simulation based on in vitro platelet aggregation test
Prediction of the human in vivo antiplatelet effect of S- and R-indobufen using population pharmacodynamic modeling and simulation based on in vitro platelet aggregation test Abstract Abstract Indobufen (Ibustrin®), a reversible inhibitor of platelet aggregation, exists in two enantiomeric forms in 1:1 ratio. Here, we ...
PMC5760952
core_pubmed_pmc
LC–MS/MS assay for the determination of natamycin in rabbit and human plasma: Application to a pharmacokinetics and protein binding study
LC–MS/MS assay for the determination of natamycin in rabbit and human plasma: Application to a pharmacokinetics and protein binding study Abstract To enable reliable quantification of natamycin in rabbit and human plasma, a validated, sensitive and selective liquid chromatography–tandem mass spectrometry assay was deve...
PMC11239757
core_pubmed_pmc
Relevance of plasma lenvatinib concentrations and endogenous urinary cytochrome P450 3A activity biomarkers in clinical practice
Relevance of plasma lenvatinib concentrations and endogenous urinary cytochrome P450 3A activity biomarkers in clinical practice Abstract Abstract Lenvatinib (LEN), a multitarget tyrosine kinase inhibitor used in various cancer treatments, is mainly metabolized by cytochrome P450 3A (CYP3A) enzymes. The importance of t...
PMC6469168
core_pubmed_pmc
Localization of 99m Tc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses
Localization of 99m Tc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses Abstract The overexpression of gastrin-releasing peptide receptors (GRPRs) in frequently occurring human tumors has provided the opportunity to use bombesin (BBN) analogs as radionuc...
PMC8652615
core_pubmed_pmc
Exploration for the effect of renal function and renal replacement therapy on pharmacokinetics of remdesivir and GS‐441524 in patients with COVID‐19: A limited case series
Exploration for the effect of renal function and renal replacement therapy on pharmacokinetics of remdesivir and GS‐441524 in patients with COVID‐19: A limited case series Abstract Abstract Remdesivir, an antiviral agent for the treatment of coronavirus disease 2019 (COVID‐19), is metabolized intracellularly, with thes...
PMC3361741
core_pubmed_pmc
Pharmacokinetic Models for FcRn-Mediated IgG Disposition
Pharmacokinetic Models for FcRn-Mediated IgG Disposition Abstract Abstract The objectives were to review available PK models for saturable FcRn-mediated IgG disposition, and to explore an alternative semimechanistic model. Most available empirical and mechanistic PK models assumed equal IgG concentrations in plasma and...
PMC8282326
core_pubmed_pmc
Clofazimine for Treatment of Cryptosporidiosis in Human Immunodeficiency Virus Infected Adults: An Experimental Medicine, Randomized, Double-blind, Placebo-controlled Phase 2a Trial
Clofazimine for Treatment of Cryptosporidiosis in Human Immunodeficiency Virus Infected Adults: An Experimental Medicine, Randomized, Double-blind, Placebo-controlled Phase 2a Trial Abstract Abstract Background We evaluated the efficacy, pharmacokinetics (PK), and safety of clofazimine (CFZ) in patients living with hum...
PMC12097056
core_pubmed_pmc
Phase 2 study design and analysis approach for BBT-877: an autotaxin inhibitor targeting idiopathic pulmonary fibrosis
Phase 2 study design and analysis approach for BBT-877: an autotaxin inhibitor targeting idiopathic pulmonary fibrosis Abstract Abstract Introduction Proof-of-concept (POC) studies are vital in determining the feasibility of further drug development, primarily by assessing preliminary efficacy signals with credible end...
PMC6742948
core_pubmed_pmc
Exposure–Response Modeling and Simulation of Progression‐Free Survival and Adverse Events of Sorafenib Treatment in Patients With Advanced Thyroid Cancer
Exposure–Response Modeling and Simulation of Progression‐Free Survival and Adverse Events of Sorafenib Treatment in Patients With Advanced Thyroid Cancer Abstract Abstract Sorafenib is an oral multikinase inhibitor approved for the treatment of differentiated thyroid carcinoma (DTC), renal cell carcinoma, and hepatocel...
PMC8458857
core_pubmed_pmc
Prudent Use of Tylosin for Treatment of Mycoplasma gallisepticum Based on Its Clinical Breakpoint and Lung Microbiota Shift
Prudent Use of Tylosin for Treatment of Mycoplasma gallisepticum Based on Its Clinical Breakpoint and Lung Microbiota Shift Abstract Abstract The aim of this study was to explore the prudent use of tylosin for the treatment of chronic respiratory infectious diseases in chickens caused by Mycoplasma gallisepticum (MG) b...
PMC9038162
core_pubmed_pmc
Pairing 3D-Printing with Nanotechnology to Manage Metabolic Syndrome
Pairing 3D-Printing with Nanotechnology to Manage Metabolic Syndrome Abstract Introduction This work was aimed to develop a Curcuma oil-based self-nanoemulsifying drug delivery system (SNEDDS) 3D-printed polypills containing glimepiride (GMD) and rosuvastatin (RSV) for treatment of dyslipidemia in patients with diabete...
PMC9418647
core_pubmed_pmc
Results From Drug–Drug Interaction Studies In Vitro and In Vivo Investigating the Inhibitory Effect of Finerenone on the Drug Transporters BCRP, OATP1B1, and OATP1B3
Results From Drug–Drug Interaction Studies In Vitro and In Vivo Investigating the Inhibitory Effect of Finerenone on the Drug Transporters BCRP, OATP1B1, and OATP1B3 Abstract Abstract Background and Objectives In vitro and in vivo studies were performed with the novel, selective, nonsteroidal mineralocorticoid receptor...
PMC3977458
core_pubmed_pmc
Targeted treatments in advanced renal cell carcinoma: focus on axitinib
Targeted treatments in advanced renal cell carcinoma: focus on axitinib Abstract Abstract Antiangiogenesis options have evolved rapidly in the last few years, with an increasing number of agents currently approved by the US Food and Drug Administration and European Medicines Agency. Angiogenesis inhibitors have been sh...
PMC7205763
core_pubmed_pmc
Analyses of Nivolumab Exposure and Clinical Safety Between 3-mg/kg Dosing and 240-mg Flat Dosing in Asian Patients with Advanced Renal Cell Carcinoma in the Real-World Clinical Setting
Analyses of Nivolumab Exposure and Clinical Safety Between 3-mg/kg Dosing and 240-mg Flat Dosing in Asian Patients with Advanced Renal Cell Carcinoma in the Real-World Clinical Setting Abstract Abstract We aimed to identify the clinical characteristics related to increased nivolumab exposure in Japanese patients with r...
PMC10448172
core_pubmed_pmc
Statistical optimization of tetrahydrocurcumin loaded solid lipid nanoparticles using Box Behnken design in the management of streptozotocin-induced diabetes mellitus
Statistical optimization of tetrahydrocurcumin loaded solid lipid nanoparticles using Box Behnken design in the management of streptozotocin-induced diabetes mellitus Abstract Abstract In the past, curcumin was the go-to medication for diabetes, but recent studies have shown that tetrahydrocurcumin is more effective. T...
PMC5586895
core_pubmed_pmc
Impact of Brief and Sequential Exposure to Nystatin on the Germ Tube Formation and Cell Surface Hydrophobicity of Oral Candida Albicans Isolates from Human Immunodeficiency Virus-Infected Patients
Impact of Brief and Sequential Exposure to Nystatin on the Germ Tube Formation and Cell Surface Hydrophobicity of Oral Candida Albicans Isolates from Human Immunodeficiency Virus-Infected Patients Abstract Abstract Objective To evaluate the impact of brief and sequential exposure to nystatin on the germ tube formation ...
PMC3964211
core_pubmed_pmc
Pharmacokinetic modeling optimizes inhibition of the ‘undruggable’ EWS-FLI1 transcription factor in Ewing Sarcoma
Pharmacokinetic modeling optimizes inhibition of the ‘undruggable’ EWS-FLI1 transcription factor in Ewing Sarcoma Abstract Transcription factors have long been deemed ‘undruggable’ targets for therapeutics. Enhanced recognition of protein biochemistry as well as the need to have more targeted approaches to treat cancer...
PMC4266272
core_pubmed_pmc
Pilot Phase II study of mazindol in children with attention deficit/hyperactivity disorder
Pilot Phase II study of mazindol in children with attention deficit/hyperactivity disorder Abstract Objective Mazindol has been proposed as a potential treatment of children with attention deficit/hyperactivity disorder (ADHD). The purpose of this pilot study was to assess its pharmacokinetics, short-term efficacy, and...
PMC11211886
core_pubmed_pmc
Preclinical pharmacokinetic characterization of amdizalisib, a novel PI3Kδ inhibitor for the treatment of hematological malignancies
Preclinical pharmacokinetic characterization of amdizalisib, a novel PI3Kδ inhibitor for the treatment of hematological malignancies Abstract Abstract Amdizalisib, also named HMPL-689, a novel selective and potent PI3Kδ inhibitor, is currently under Phase II clinical development in China for treating hematological mali...
PMC10566117
core_pubmed_pmc
Doxapram versus placebo in preterm newborns: a study protocol for an international double blinded multicentre randomized controlled trial (DOXA-trial)
Doxapram versus placebo in preterm newborns: a study protocol for an international double blinded multicentre randomized controlled trial (DOXA-trial) Abstract Abstract Background Apnoea of prematurity (AOP) is one of the most common diagnoses among preterm infants. AOP often leads to hypoxemia and bradycardia which ar...
PMC3929878
core_pubmed_pmc
Pazopanib exposure decreases as a result of an ifosfamide-dependent drug–drug interaction: results of a phase I study
Pazopanib exposure decreases as a result of an ifosfamide-dependent drug–drug interaction: results of a phase I study Abstract Abstract Background: The vascular endothelial growth factor receptor (VEGFR) pathway plays a pivotal role in solid malignancies and is probably involved in chemotherapy resistance. Pazopanib, i...
PMC9186361
core_pubmed_pmc
Orally delivered rutin in lipid-based nano-formulation exerts strong antithrombotic effects by protein disulfide isomerase inhibition
Orally delivered rutin in lipid-based nano-formulation exerts strong antithrombotic effects by protein disulfide isomerase inhibition Abstract Abstract Thrombosis occurs in both macrovasculature and microvasculature, causing various cardio-cerebral vascular diseases. The lack of effective and safe antithrombotic drugs ...
PMC10604117
core_pubmed_pmc
Incorporation of Perillyl Alcohol into Lipid-Based Nanocarriers Enhances the Antiproliferative Activity in Malignant Glioma Cells
Incorporation of Perillyl Alcohol into Lipid-Based Nanocarriers Enhances the Antiproliferative Activity in Malignant Glioma Cells Abstract Abstract Perillyl alcohol (PA), a naturally existing monocyclic terpene related to limonene, is characterized by its poor aqueous solubility and very limited bioavailability. Its po...
PMC3383348
core_pubmed_pmc
Cisplatin-loaded core cross-linked micelles: comparative pharmacokinetics, antitumor activity, and toxicity in mice
Cisplatin-loaded core cross-linked micelles: comparative pharmacokinetics, antitumor activity, and toxicity in mice Abstract Abstract Polymer micelles with cross-linked ionic cores are shown here to improve the therapeutic performance of the platinum-containing anticancer compound cisplatin. Biodistribution, antitumor ...
PMC10865990
core_pubmed_pmc
Molecular pharmacodynamics of meropenem for nosocomial pneumonia caused by Pseudomonas aeruginosa
Molecular pharmacodynamics of meropenem for nosocomial pneumonia caused by Pseudomonas aeruginosa Abstract ABSTRACT Hospital-acquired pneumonia (HAP) is a leading cause of morbidity and mortality, commonly caused by Pseudomonas aeruginosa . Meropenem is a commonly used therapeutic agent, although emergent resistance oc...
PMC12115112
core_pubmed_pmc
Accelerating Biologics PBPK Modelling with Automated Model Building: A Tutorial
Accelerating Biologics PBPK Modelling with Automated Model Building: A Tutorial Abstract Physiologically based pharmacokinetic (PBPK) modelling for biologics, such as monoclonal antibodies and therapeutic proteins, involves capturing complex processes, including target-mediated drug disposition (TMDD), FcRn-mediated re...
PMC7745057
core_pubmed_pmc
BEBT-109, a pan-mutant-selective EGFR inhibitor with potent antitumor activity in EGFR-mutant non-small cell lung cancer
BEBT-109, a pan-mutant-selective EGFR inhibitor with potent antitumor activity in EGFR-mutant non-small cell lung cancer Abstract Highlights • BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. • Pharmacokinetic profiles of BEBT-109 minimize the off-target toxicity. • Two major metabolites of BEBT-109 show no wi...
PMC6510375
core_pubmed_pmc
Evaluation of the Ability of Immune Humanized Mice to Demonstrate CD20‐Specific Cytotoxicity Induced by Ofatumumab
Evaluation of the Ability of Immune Humanized Mice to Demonstrate CD20‐Specific Cytotoxicity Induced by Ofatumumab Abstract Abstract CD20 monoclonal antibodies are well‐established therapeutics for the treatment of B‐cell malignancies. Several mechanisms of target cell killing occur from anti‐CD20 therapy, including co...
PMC12626815
core_pubmed_pmc
Serial TIL infusions and PD-1 blockade drive long-term clonal persistence in prostate cancer
Serial TIL infusions and PD-1 blockade drive long-term clonal persistence in prostate cancer Abstract Abstract Adoptive cell therapy using tumor-infiltrating lymphocytes (TIL) can achieve durable responses in patients with metastatic cancers, but the long-term clonal dynamics after multiple administration and synergy w...
PMC4942489
core_pubmed_pmc
Single therapeutic and supratherapeutic doses of sacubitril/valsartan (LCZ696) do not affect cardiac repolarization
Single therapeutic and supratherapeutic doses of sacubitril/valsartan (LCZ696) do not affect cardiac repolarization Abstract Abstract Purpose Sacubitril/valsartan (LCZ696) is a first-in-class angiotensin receptor neprilysin inhibitor (ARNI) indicated to reduce the risk of cardiovascular death and hospitalization for he...
PMC12823941
core_pubmed_pmc
Multimodal data-driven predictive model for vancomycin serum concentrations in postoperative cardiac surgery patients under cardiopulmonary bypass: a single-center retrospective study
Multimodal data-driven predictive model for vancomycin serum concentrations in postoperative cardiac surgery patients under cardiopulmonary bypass: a single-center retrospective study Abstract Background This study analyzed the pharmacokinetic data of vancomycin in patients after cardiac surgery under cardiopulmonary b...
PMC8779343
core_pubmed_pmc
Enzyme Activity of Natural Products on Cytochrome P450
Enzyme Activity of Natural Products on Cytochrome P450 Abstract Abstract Drug-metabolizing enzymes, particularly the cytochrome P450 (CYP450) monooxygenases, play a pivotal role in pharmacokinetics. CYP450 enzymes can be affected by various xenobiotic substrates, which will eventually be responsible for most metabolism...
PMC9680504
core_pubmed_pmc
Rational Design and In Vivo Characterization of mRNA-Encoded Broadly Neutralizing Antibody Combinations against HIV-1
Rational Design and In Vivo Characterization of mRNA-Encoded Broadly Neutralizing Antibody Combinations against HIV-1 Abstract Monoclonal antibodies have been used successfully as recombinant protein therapy; however, for HIV, multiple broadly neutralizing antibodies may be necessary. We used the mRNA-LNP platform for ...
PMC3304359
core_pubmed_pmc
Development of domperidone bilayered matrix type transdermal patches: physicochemical, in vitro and ex vivo characterization
Development of domperidone bilayered matrix type transdermal patches: physicochemical, in vitro and ex vivo characterization Abstract Abstract Background and the purpose of the study Domperidone (DOM) is a dopamine- receptor (D 2 ) antagonist, which is widely used in the treatment of motion-sickness. The pharmacokineti...
PMC8292148
core_pubmed_pmc
Pharmacogenetic information in Swiss drug labels – a systematic analysis
Pharmacogenetic information in Swiss drug labels – a systematic analysis Abstract Implementation of pharmacogenetics (PGx) and individualization of drug therapy is supposed to obviate adverse drug reactions or therapy failure. Health care professionals (HCPs) use drug labels (DLs) as reliable information about drugs. W...
PMC10766854
core_pubmed_pmc
Evaluating the bioequivalence and safety of liraglutide injection versus Victoza ® in healthy Chinese subjects: a randomized, open, two-cycle, self-crossover phase I clinical trial
Evaluating the bioequivalence and safety of liraglutide injection versus Victoza ® in healthy Chinese subjects: a randomized, open, two-cycle, self-crossover phase I clinical trial Abstract Abstract Background: Liraglutide is an acylated glucagon-like peptide-1 (GLP-1) analog, and its pharmacokinetic and pharmacodynami...
PMC10014045
core_pubmed_pmc
Bayesian PBPK modeling using R/Stan/Torsten and Julia/SciML/Turing.Jl
Bayesian PBPK modeling using R/Stan/Torsten and Julia/SciML/Turing.Jl Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) models are mechanistic models that are built based on an investigator's prior knowledge of the in vivo system of interest. Bayesian inference incorporates an investigator's prior knowledg...
PMC5569364
core_pubmed_pmc
Glucuronides of phytoestrogen flavonoid enhance macrophage function via conversion to aglycones by β‐glucuronidase in macrophages
Glucuronides of phytoestrogen flavonoid enhance macrophage function via conversion to aglycones by β‐glucuronidase in macrophages Abstract Abstract Introduction Flavonoids are converted to inactive metabolites like glucuronides in the gut, and circulate mainly as glucuronides in blood stream, resulting in low concentra...