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PMC6955635
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Adrenomedullin in Healthy Males: A Randomized, Double-Blind, Phase 1 Clinical Trial
Safety, Tolerability, and Pharmacokinetics of Adrenomedullin in Healthy Males: A Randomized, Double-Blind, Phase 1 Clinical Trial Abstract Background Adrenomedullin (AM), an endogenous vasodilative peptide, has immunomodulative effects and acts as an accelerator of mucosal regeneration in the digestive tract. AM has sh...
PMC8453750
core_pubmed_pmc
Effects of Itraconazole and Rifampin on the Pharmacokinetics of Mobocertinib (TAK‐788), an Oral Epidermal Growth Factor Receptor Inhibitor, in Healthy Volunteers
Effects of Itraconazole and Rifampin on the Pharmacokinetics of Mobocertinib (TAK‐788), an Oral Epidermal Growth Factor Receptor Inhibitor, in Healthy Volunteers Abstract Abstract Mobocertinib (TAK‐788) is an investigational oral tyrosine kinase inhibitor targeting epidermal growth factor receptor and human epidermal g...
PMC9312564
core_pubmed_pmc
Development of Long-Acting Human Adrenomedullin Fc-Fusion Proteins
Development of Long-Acting Human Adrenomedullin Fc-Fusion Proteins Abstract Abstract Simple Summary Adrenomedullin (AM) is a hypotensive peptide hormone that exerts anti-inflammatory effects and is involved in wound healing and embryogenesis. However, treatment requires continuous administration as the half-life of nat...
PMC12579162
core_pubmed_pmc
Synthesized Depside Molecules Suppress the Progression of Colorectal Cancer by Binding VDAC1/PHB/MMP9 Being at the Crossroads of Stemness, Motility, Apoptosis, and Metabolism
Synthesized Depside Molecules Suppress the Progression of Colorectal Cancer by Binding VDAC1/PHB/MMP9 Being at the Crossroads of Stemness, Motility, Apoptosis, and Metabolism Abstract ABSTRACT Lichen secondary metabolites have shown potential in cancer therapy, but strategies to enhance cancer‐specific selectivity are ...
PMC4629266
core_pubmed_pmc
Pharmacokinetic study of salvianolic acid D after oral and intravenous administration in rats
Pharmacokinetic study of salvianolic acid D after oral and intravenous administration in rats Abstract A sensitive, specific and rapid LC-MS method was developed and validated for the determination of salvianolic acid D (SalD) in rat plasma. This method used a single quadrupole mass spectrometer with an electrospray io...
PMC11786813
core_pubmed_pmc
Clinical trial to compare safety and tolerability between intravenous infusion and bolus intravenous injection of ApTOLL in healthy volunteers
Clinical trial to compare safety and tolerability between intravenous infusion and bolus intravenous injection of ApTOLL in healthy volunteers Abstract ApTOLL, a new modulator of Toll-like receptor 4, has demonstrated safety and efficacy in healthy subjects and in stroke patients; however, the route of administration u...
PMC8652670
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamics of the Neutralizing Antibodies Bamlanivimab and Etesevimab in Patients With Mild to Moderate COVID‐19 Infection
Population Pharmacokinetics and Pharmacodynamics of the Neutralizing Antibodies Bamlanivimab and Etesevimab in Patients With Mild to Moderate COVID‐19 Infection Abstract Abstract Bamlanivimab and etesevimab are neutralizing antibodies indicated for treatment of coronavirus disease 2019 (COVID‐19) in patients with early...
PMC6586910
core_pubmed_pmc
Population pharmacokinetics of PF-05280014 (a trastuzumab biosimilar) and reference trastuzumab (Herceptin ® ) in patients with HER2-positive metastatic breast cancer
Population pharmacokinetics of PF-05280014 (a trastuzumab biosimilar) and reference trastuzumab (Herceptin ® ) in patients with HER2-positive metastatic breast cancer Abstract Purpose PF-05280014 is a biosimilar to trastuzumab (Herceptin ® ). Following demonstration of pharmacokinetic (PK) similarity in healthy volunte...
PMC7374078
core_pubmed_pmc
Cefiderocol, a New Siderophore Cephalosporin for the Treatment of Complicated Urinary Tract Infections Caused by Multidrug-Resistant Pathogens: Preclinical and Clinical Pharmacokinetics, Pharmacodynamics, Efficacy and Safety
Cefiderocol, a New Siderophore Cephalosporin for the Treatment of Complicated Urinary Tract Infections Caused by Multidrug-Resistant Pathogens: Preclinical and Clinical Pharmacokinetics, Pharmacodynamics, Efficacy and Safety Abstract Abstract Cefiderocol (Fetroja ® ) is a siderophore cephalosporin and has demonstrated ...
PMC6468355
core_pubmed_pmc
Impact of Curcumin (with or without Piperine) on the Pharmacokinetics of Tamoxifen
Impact of Curcumin (with or without Piperine) on the Pharmacokinetics of Tamoxifen Abstract Abstract Tamoxifen is a prodrug that is primarily metabolized into the pharmacologically active metabolite endoxifen and eventually into inactive metabolites. The herb curcumin may increase endoxifen exposure by affecting phase ...
PMC12775547
core_pubmed_pmc
Population Pharmacokinetic Model‐Based Dose Selection of Extended‐Release Injectable Olanzapine (TV‐44749) for Subcutaneous Use in Phase 3 Clinical Trial in Adults with Schizophrenia
Population Pharmacokinetic Model‐Based Dose Selection of Extended‐Release Injectable Olanzapine (TV‐44749) for Subcutaneous Use in Phase 3 Clinical Trial in Adults with Schizophrenia Abstract Abstract TV‐44749 is a long‐acting subcutaneous (SC) injectable olanzapine based on a novel copolymer drug delivery technology e...
PMC7150903
core_pubmed_pmc
The Influence of the Different Disposition Characteristics of Snake Toxins on the Pharmacokinetics of Snake Venom
The Influence of the Different Disposition Characteristics of Snake Toxins on the Pharmacokinetics of Snake Venom Abstract Abstract Snake venom is comprised of a combination of different proteins and peptides with a wide range of molecular weights and different disposition processes inherent to each compound. This caus...
PMC9589050
core_pubmed_pmc
The OBTAINS study: A nationwide cross-sectional survey on the implementation of extended or continuous infusion of β-lactams and vancomycin among neonatal sepsis patients in China
The OBTAINS study: A nationwide cross-sectional survey on the implementation of extended or continuous infusion of β-lactams and vancomycin among neonatal sepsis patients in China Abstract Background: Dosing strategies of β-lactams and vancomycin should be optimized according to pharmacokinetic/pharmacodynamic principl...
PMC5423921
core_pubmed_pmc
Influence of Renal Impairment on the Pharmacokinetics of Afatinib: An Open-Label, Single-Dose Study
Influence of Renal Impairment on the Pharmacokinetics of Afatinib: An Open-Label, Single-Dose Study Abstract Background and Objective Afatinib is an oral irreversible ErbB-Family Blocker indicated for treatment of patients with EGFR mutation positive advanced non-small cell lung cancer. This trial assessed whether rena...
PMC7783234
core_pubmed_pmc
Hydrogel-based matrices for controlled drug delivery of etamsylate: Prediction of in-vivo plasma profiles
Hydrogel-based matrices for controlled drug delivery of etamsylate: Prediction of in-vivo plasma profiles Abstract Abstract Objectives To design oral controlled release (CR) hydrogel matrix tablets of etamsylate using various hydrophilic polymers. Additionally, to predict plasma concentration-time profiles of etamsylat...
PMC5920327
core_pubmed_pmc
Stochastic Pharmacokinetic-Pharmacodynamic Modeling for Assessing the Systemic Health Risk of Perfluorooctanoate (PFOA)
Stochastic Pharmacokinetic-Pharmacodynamic Modeling for Assessing the Systemic Health Risk of Perfluorooctanoate (PFOA) Abstract Abstract A phase 1 dose-escalation trial assessed the chemotherapeutic potential of ammonium perfluorooctanoate (APFO). Forty-nine primarily solid-tumor cancer patients who failed standard th...
PMC11770336
core_pubmed_pmc
IGF-1 Assessment During Weekly Somatrogon Treatment in Pediatric Patients With GH Deficiency
IGF-1 Assessment During Weekly Somatrogon Treatment in Pediatric Patients With GH Deficiency Abstract Abstract Context In patients with GH deficiency (GHD) receiving GH treatment, IGF-1 concentrations are used by physicians to monitor treatment safety and efficacy and guide dosing decisions. Somatrogon is a long-acting...
PMC12813290
core_pubmed_pmc
Model-based assessment of VRC07-523LS dosing in infants through population pharmacokinetic -pharmacodynamic modelling in adults and infants
Model-based assessment of VRC07-523LS dosing in infants through population pharmacokinetic -pharmacodynamic modelling in adults and infants Abstract Abstract Objectives To develop a population pharmacokinetic (popPK) model to understand factors affecting the broadly neutralizing HIV antibody (bNAb) VR07-523LS dispositi...
PMC9813077
core_pubmed_pmc
Safety and antitumor activity of copanlisib in Japanese patients with relapsed/refractory indolent non-Hodgkin lymphoma: a phase Ib/II study
Safety and antitumor activity of copanlisib in Japanese patients with relapsed/refractory indolent non-Hodgkin lymphoma: a phase Ib/II study Abstract The safety, efficacy, and pharmacokinetics of copanlisib were evaluated in this phase Ib/II study in Japanese patients with relapsed/refractory indolent non-Hodgkin lymph...
PMC9701462
core_pubmed_pmc
Rencofilstat, a cyclophilin inhibitor: A phase 2a, multicenter, single‐blind, placebo‐controlled study in F2/F3 NASH
Rencofilstat, a cyclophilin inhibitor: A phase 2a, multicenter, single‐blind, placebo‐controlled study in F2/F3 NASH Abstract Abstract Rencofilstat (RCF) demonstrated antifibrotic effects in preclinical models and was safe and well tolerated in Phase 1 studies. The aim of this Phase 2a study was safety, tolerability, p...
PMC12895850
core_pubmed_pmc
A human liver organoids-on-chip for the assessment of drug-induced liver injury
A human liver organoids-on-chip for the assessment of drug-induced liver injury Abstract Abstract Background Drug-induced liver injury (DILI) is a leading cause of liver disease. Current drug toxicology screening primarily relies on 2D cell cultures and animal models, which have limitations in predicting clinical hepat...
PMC3728092
core_pubmed_pmc
Improvement of Pharmacokinetics Behavior of Apocynin by Nitrone Derivatization: Comparative Pharmacokinetics of Nitrone-Apocynin and its Parent Apocynin in Rats
Improvement of Pharmacokinetics Behavior of Apocynin by Nitrone Derivatization: Comparative Pharmacokinetics of Nitrone-Apocynin and its Parent Apocynin in Rats Abstract Apocynin, a potent inhibitor of NADPH-oxidase, was widely studied for activities in diseases such as inflammation-mediated disorders, asthma and cardi...
PMC11905544
core_pubmed_pmc
Mycophenolic acid trough level assessment in patients with lupus nephritis; does it make a difference?
Mycophenolic acid trough level assessment in patients with lupus nephritis; does it make a difference? Abstract Abstract Introduction Mycophenolate Mofetil (MMF) has become one of the cornerstone treatments of lupus nephritis (LN). It is converted into mycophenolic acid (MPA), an active metabolite, that displays high i...
PMC7790722
core_pubmed_pmc
Rituximab for the treatment of multiple sclerosis: a review
Rituximab for the treatment of multiple sclerosis: a review Abstract Abstract In the last decades, evidence suggesting the direct or indirect involvement of B cells on multiple sclerosis (MS) pathogenesis has accumulated. The increased amount of data on the efficacy and safety of B-cell-depleting therapies from several...
PMC7293976
core_pubmed_pmc
Associations between model-predicted rivaroxaban exposure and patient characteristics and efficacy and safety outcomes in the prevention of venous thromboembolism
Associations between model-predicted rivaroxaban exposure and patient characteristics and efficacy and safety outcomes in the prevention of venous thromboembolism Abstract Anticoagulant plasma concentrations and patient characteristics might affect the benefit–risk balance of therapy. The study objective was to assess ...
PMC10557076
core_pubmed_pmc
Folate-receptor-targeted co-self-assembly carrier-free gemcitabine nanoparticles loading indocyanine green for chemo-photothermal therapy
Folate-receptor-targeted co-self-assembly carrier-free gemcitabine nanoparticles loading indocyanine green for chemo-photothermal therapy Abstract The carrier-free chemo-photothermal therapy has become a promising strategy to improve anti-cancer therapeutic efficacy owing to the combination of chemotherapy and photothe...
PMC10053955
core_pubmed_pmc
Effect of Dexamethasone on Abiraterone Pharmacokinetics in Mice: Determined by LC/MS Analysis
Effect of Dexamethasone on Abiraterone Pharmacokinetics in Mice: Determined by LC/MS Analysis Abstract Abstract Background: Abiraterone acetate is a cytochrome P450 17A1 (CYP17A1) inhibitor that is indicated for use in both castration-resistant and castration-sensitive prostate cancer patients. To manage the mineraloco...
PMC8876599
core_pubmed_pmc
Physicochemical Characterizations and Pharmacokinetic Evaluation of Pentazocine Solid Lipid Nanoparticles against Inflammatory Pain Model
Physicochemical Characterizations and Pharmacokinetic Evaluation of Pentazocine Solid Lipid Nanoparticles against Inflammatory Pain Model Abstract Pentazocine (PTZ), a narcotic-antagonist analgesic, has been extensively used in the treatment of initial carcinogenic or postoperative pain. Hepatic first-pass metabolism r...
PMC12468889
core_pubmed_pmc
Comparative Molecular Profiling and Bioactivity Analysis of Algerian Propolis: Antioxidant, Antibacterial Activities, and In Silico NRF2-KEAP1 Pathway Modulation
Comparative Molecular Profiling and Bioactivity Analysis of Algerian Propolis: Antioxidant, Antibacterial Activities, and In Silico NRF2-KEAP1 Pathway Modulation Abstract Abstract Propolis, a natural bee-derived product rich in diverse phytochemicals with potential therapeutic benefits, remains underexplored in Algeria...
PMC12299782
core_pubmed_pmc
From Structure to Function: The Promise of PAMAM Dendrimers in Biomedical Applications
From Structure to Function: The Promise of PAMAM Dendrimers in Biomedical Applications Abstract PAMAM dendrimers are distinguished by their capacity for functionalization, which enhances the properties of the compounds they transport, rendering them highly versatile nanoparticles with extensive applications in the biom...
PMC7808976
core_pubmed_pmc
Pharmacokinetics of ASP4345 from Single Ascending-Dose and Multiple Ascending-Dose Phase I Studies
Pharmacokinetics of ASP4345 from Single Ascending-Dose and Multiple Ascending-Dose Phase I Studies Abstract Background Cognitive impairment is a core feature of schizophrenia. While first- and second-generation antipsychotic drugs treat psychotic exacerbations, no treatment is approved for the cognitive dysfunction. We...
PMC7449170
core_pubmed_pmc
ATI-2173, a Novel Liver-Targeted Non-Chain-Terminating Nucleotide for Hepatitis B Virus Cure Regimens
ATI-2173, a Novel Liver-Targeted Non-Chain-Terminating Nucleotide for Hepatitis B Virus Cure Regimens Abstract ATI-2173 is a novel liver-targeted molecule designed to deliver the 5′-monophosphate of clevudine for the treatment of chronic hepatitis B infection. Unlike other nucleos(t)ides, the active clevudine-5′-tripho...
PMC3852421
core_pubmed_pmc
Inclusion of CYP3A5 genotyping in a nonparametric population model improves dosing of tacrolimus early after transplantation
Inclusion of CYP3A5 genotyping in a nonparametric population model improves dosing of tacrolimus early after transplantation Abstract Abstract Following organ engraftment, initial dosing of tacrolimus is based on recipient weight and adjusted by measured C 0 concentrations. The bioavailability and elimination of tacrol...
PMC11022103
core_pubmed_pmc
Pretreatment and analysis techniques development of TKIs in biological samples for pharmacokinetic studies and therapeutic drug monitoring
Pretreatment and analysis techniques development of TKIs in biological samples for pharmacokinetic studies and therapeutic drug monitoring Abstract Tyrosine kinase inhibitors (TKIs) have emerged as the first-line small molecule drugs in many cancer therapies, exerting their effects by impeding aberrant cell growth and ...
PMC4150924
core_pubmed_pmc
Interaction Between Domperidone and Ketoconazole: Toward Prediction of Consequent QTc Prolongation Using Purely In Vitro Information
Interaction Between Domperidone and Ketoconazole: Toward Prediction of Consequent QTc Prolongation Using Purely In Vitro Information Abstract Abstract We aimed to investigate the application of combined mechanistic pharmacokinetic (PK) and pharmacodynamic (PD) modeling and simulation in predicting the domperidone (DOM)...
PMC6541944
core_pubmed_pmc
Development of Functional Antibodies Directed to Human Dialyzable Leukocyte Extract (Transferon®)
Development of Functional Antibodies Directed to Human Dialyzable Leukocyte Extract (Transferon®) Abstract Abstract Transferon® is an immunomodulator made of a complex mixture of peptides from human dialyzable leucocyte extracts (hDLEs). Development of surrogate antibodies directed to hDLE is an indispensable tool for ...
PMC6211326
core_pubmed_pmc
Ombitasvir/Paritaprevir/Ritonavir With or Without Dasabuvir and With or Without Ribavirin for Adolescents With HCV Genotype 1 or 4
Ombitasvir/Paritaprevir/Ritonavir With or Without Dasabuvir and With or Without Ribavirin for Adolescents With HCV Genotype 1 or 4 Abstract In adults, treatment of hepatitis C virus (HCV) infection with ombitasvir (OBV)/paritaprevir (PTV)/ritonavir (r) with or without dasabuvir (DSV) and ±ribavirin (RBV) results in hig...
PMC12850561
core_pubmed_pmc
Mitigating subtherapeutic cabozantinib exposure after prior mitotane therapy in adrenocortical carcinoma: Pharmacological boosting with cobicistat
Mitigating subtherapeutic cabozantinib exposure after prior mitotane therapy in adrenocortical carcinoma: Pharmacological boosting with cobicistat Abstract Mitotane is an adrenolytic drug with cytotoxic effects, registered for the treatment of advanced adrenocortical carcinoma (ACC), a rare but aggressive tumour type w...
PMC8245084
core_pubmed_pmc
Docetaxel loaded mPEG-PLA nanoparticles for sarcoma therapy: preparation, characterization, pharmacokinetics, and anti-tumor efficacy
Docetaxel loaded mPEG-PLA nanoparticles for sarcoma therapy: preparation, characterization, pharmacokinetics, and anti-tumor efficacy Abstract Abstract Sarcoma represents one of the most common malignant tumors with poor treatment outcomes and prognosis. Docetaxel (DTX) is acknowledged as one of the most important chem...
PMC7383911
core_pubmed_pmc
Stable Isotopically Labeled Intravenous Microdose Pharmacokinetic Trials as a Tool to Assess Absolute Bioavailability: Feasibility and Paradigm to Apply for Protein Kinase Inhibitors in Oncology
Stable Isotopically Labeled Intravenous Microdose Pharmacokinetic Trials as a Tool to Assess Absolute Bioavailability: Feasibility and Paradigm to Apply for Protein Kinase Inhibitors in Oncology Discussion Discussion An important finding of this review is that for more than half the FDA‐registered smPKIs an absolute bi...
PMC11668715
core_pubmed_pmc
Repurposing pinaverium bromide against Staphylococcus and its biofilms with new mechanisms
Repurposing pinaverium bromide against Staphylococcus and its biofilms with new mechanisms Abstract Antibiotic resistance by methicillin-resistant Staphylococcus aureus (MRSA) is an urgent threat to human health. The biofilm and persister cells formation ability of MRSA and Staphylococcus epidermidis often companied wi...
PMC9992410
core_pubmed_pmc
Insights into the pharmacodynamics and pharmacokinetics of meldonium after exposure to acute high altitude
Insights into the pharmacodynamics and pharmacokinetics of meldonium after exposure to acute high altitude Abstract Abstract Objective: Meldonium, a well-known cardioprotective drug, has been reported to be protective against pulmonary injury at high altitudes; however, the pharmacodynamics of meldonium in other vital ...
PMC11412384
core_pubmed_pmc
Mathematical Models of Ocular Drug Delivery
Mathematical Models of Ocular Drug Delivery Abstract Drug delivery is an important factor for the success of ocular drug treatment. However, several physical, biochemical, and flow-related barriers limit drug exposure of anterior and posterior ocular target tissues during drug treatment via topical, subconjunctival, in...
PMC3600722
core_pubmed_pmc
Nonlinear Population Pharmacokinetics of Sirolimus in Patients With Advanced Cancer
Nonlinear Population Pharmacokinetics of Sirolimus in Patients With Advanced Cancer Abstract Sirolimus, the prototypical inhibitor of the mammalian target of rapamycin, has substantial antitumor activity. In this study, sirolimus showed nonlinear pharmacokinetic characteristics over a wide dose range (from 1 to 60 mg/w...
PMC6099239
core_pubmed_pmc
Pharmacokinetic Interaction Between Fingolimod and Carbamazepine in Healthy Subjects
Pharmacokinetic Interaction Between Fingolimod and Carbamazepine in Healthy Subjects Abstract Abstract This open‐label, single‐sequence study in healthy subjects investigated the effects of steady‐state carbamazepine on the pharmacokinetic (PK) profile of a single 2‐mg dose of fingolimod. In period 1, a single oral dos...
PMC7484984
core_pubmed_pmc
Pharmacogenetic‐Pharmacokinetic Interactions in Drug Marketing Authorization Applications via the European Medicines Agency Between 2014 and 2017
Pharmacogenetic‐Pharmacokinetic Interactions in Drug Marketing Authorization Applications via the European Medicines Agency Between 2014 and 2017 Abstract Abstract This study aimed to determine to which extent data on potential pharmacogenetic‐pharmacokinetic (PG‐PK) interactions are provided to, and assessed by, the E...
PMC5539083
core_pubmed_pmc
Efficacy of Cefquinome against Escherichia coli Environmental Mastitis Assessed by Pharmacokinetic and Pharmacodynamic Integration in Lactating Mouse Model
Efficacy of Cefquinome against Escherichia coli Environmental Mastitis Assessed by Pharmacokinetic and Pharmacodynamic Integration in Lactating Mouse Model Abstract This work investigates the pharmacodynamic effectiveness of cefquinome against environmental Escherichia coli mastitis infection, following an intramammary...
PMC8684803
core_pubmed_pmc
Glutamine Antagonist GA-607 Causes a Dramatic Accumulation of FGAR which can be used to Monitor Target Engagement
Glutamine Antagonist GA-607 Causes a Dramatic Accumulation of FGAR which can be used to Monitor Target Engagement Abstract Abstract Background Metabolomic analyses from our group and others have shown that tumors treated with glutamine antagonists (GA) exhibit robust accumulation of formylglycinamide ribonucleotide (FG...
PMC11885412
core_pubmed_pmc
Evaluation of Innate Immune System, Body Habitus, and Sex on the Pharmacokinetics and Pharmacodynamics of Anetumab Ravtansine in Patients With Cancer
Evaluation of Innate Immune System, Body Habitus, and Sex on the Pharmacokinetics and Pharmacodynamics of Anetumab Ravtansine in Patients With Cancer Abstract ABSTRACT Anetumab ravtansine, like other ADC drugs, has high inter‐patient variability in its pharmacokinetic (PK) and pharmacodynamic (PD) outcomes, which raise...
PMC8885935
core_pubmed_pmc
A Randomized, Double-Blind, Placebo- and Active-Controlled, Escalating Single-Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Profiles of Subcutaneous Eflapegrastim in Healthy Japanese and Caucasian Subjects
A Randomized, Double-Blind, Placebo- and Active-Controlled, Escalating Single-Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Profiles of Subcutaneous Eflapegrastim in Healthy Japanese and Caucasian Subjects Abstract Abstract Background Eflapegrastim (Rolontis ® ) is a novel long‐a...
PMC11431462
core_pubmed_pmc
In Vivo Tissue Distribution and Pharmacokinetics of FITC-Labelled Hizikia fusiforme Polyphenol–Polysaccharide Complex in Mice
In Vivo Tissue Distribution and Pharmacokinetics of FITC-Labelled Hizikia fusiforme Polyphenol–Polysaccharide Complex in Mice Abstract In this study, a quantitative method based on fluorescein isothiocyanate (FITC)-labelled Hizikia fusiforme polyphenol–polysaccharide complex (HPC) and its purified fractions (PC1, PC4) ...
PMC6099358
core_pubmed_pmc
Empagliflozin as adjunct to insulin in Japanese participants with type 1 diabetes: Results of a 4‐week, double‐blind, randomized, placebo‐controlled phase 2 trial
Empagliflozin as adjunct to insulin in Japanese participants with type 1 diabetes: Results of a 4‐week, double‐blind, randomized, placebo‐controlled phase 2 trial Abstract Abstract Aims This phase 2, double‐blind, randomized, placebo‐controlled trial ( http://clinicaltrials.gov NCT02702011 ) with 4 sites in Japan inves...
PMC10087178
core_pubmed_pmc
A comprehensive pharmacogenomic study indicates roles for SLCO1B1 , ABCG2 and SLCO2B1 in rosuvastatin pharmacokinetics
A comprehensive pharmacogenomic study indicates roles for SLCO1B1 , ABCG2 and SLCO2B1 in rosuvastatin pharmacokinetics Abstract Aims The aim was to comprehensively investigate the effects of genetic variability on the pharmacokinetics of rosuvastatin. Methods We conducted a genome‐wide association study and candidate g...
PMC10338412
core_pubmed_pmc
Regulation of ABC transporters by sex steroids may explain differences in drug resistance between sexes
Regulation of ABC transporters by sex steroids may explain differences in drug resistance between sexes Abstract Abstract Drug efficacy is dependent on the pharmacokinetics and pharmacodynamics of therapeutic agents. Tight junctions, detoxification enzymes, and drug transporters, due to their localization on epithelial...
PMC4102944
core_pubmed_pmc
Phase I ficlatuzumab monotherapy or with erlotinib for refractory advanced solid tumours and multiple myeloma
Phase I ficlatuzumab monotherapy or with erlotinib for refractory advanced solid tumours and multiple myeloma Abstract Background: Ficlatuzumab, a humanised hepatocyte growth factor (HGF) IgG1κ inhibitory monoclonal antibody, was evaluated for recommended phase II dose (RP2D), safety, pharmacokinetics (PKs), antidrug a...
PMC4745494
core_pubmed_pmc
Grape Seed Procyanidin Extract Improves Insulin Production but Enhances Bax Protein Expression in Cafeteria-Treated Male Rats
Grape Seed Procyanidin Extract Improves Insulin Production but Enhances Bax Protein Expression in Cafeteria-Treated Male Rats Abstract In a previous study, the administration of a grape seed procyanidin extract (GSPE) in female Wistar rats improved insulin resistance, reduced insulin production, and modulated apoptosis...
PMC5292604
core_pubmed_pmc
Psychotropic drugs and liver disease: A critical review of pharmacokinetics and liver toxicity
Psychotropic drugs and liver disease: A critical review of pharmacokinetics and liver toxicity Abstract Abstract The liver is the organ by which the majority of substances are metabolized, including psychotropic drugs. There are several pharmacokinetic changes in end-stage liver disease that can interfere with the meta...
PMC9199203
core_pubmed_pmc
Expert clinical pharmacological advice may make an antimicrobial TDM program for emerging candidates more clinically useful in tailoring therapy of critically ill patients
Expert clinical pharmacological advice may make an antimicrobial TDM program for emerging candidates more clinically useful in tailoring therapy of critically ill patients Abstract Background Therapeutic drug monitoring (TDM) may represent an invaluable tool for optimizing antimicrobial therapy in septic patients, but ...
PMC5604209
core_pubmed_pmc
CT-721, a Potent Bcr-Abl Inhibitor, Exhibits Excellent In Vitro and In Vivo Efficacy in the Treatment of Chronic Myeloid Leukemia
CT-721, a Potent Bcr-Abl Inhibitor, Exhibits Excellent In Vitro and In Vivo Efficacy in the Treatment of Chronic Myeloid Leukemia Abstract Kinase inhibitors that target Bcr-Abl are highly effective in the treatment of chronic myeloid leukemia (CML). However, these inhibitors are often invalidated due to the drug resist...
PMC6529376
core_pubmed_pmc
Population pharmacokinetics of inotuzumab ozogamicin in relapsed/refractory acute lymphoblastic leukemia and non-Hodgkin lymphoma
Population pharmacokinetics of inotuzumab ozogamicin in relapsed/refractory acute lymphoblastic leukemia and non-Hodgkin lymphoma Abstract Abstract This population pharmacokinetics analysis evaluated the target-mediated drug disposition of inotuzumab ozogamicin (InO) through an empirical time-dependent clearance (CL t ...
PMC9723340
core_pubmed_pmc
The combination effect of meropenem/sulbactam/polymyxin-B on the pharmacodynamic parameters for mutant selection windows against carbapenem-resistant Acinetobacter baumannii
The combination effect of meropenem/sulbactam/polymyxin-B on the pharmacodynamic parameters for mutant selection windows against carbapenem-resistant Acinetobacter baumannii Abstract The objective of this study was to evaluate whether combinations of sulbactam, meropenem, and polymyxin-B could reduce or close the gap o...
PMC10289985
core_pubmed_pmc
Brigatinib pharmacokinetics in patients with chronic hepatic impairment
Brigatinib pharmacokinetics in patients with chronic hepatic impairment Abstract Abstract Brigatinib is an anaplastic lymphoma kinase (ALK) inhibitor approved for the treatment of ALK -positive non-small cell lung cancer. This open-label, parallel-group study investigated the effect of chronic hepatic impairment on the...
PMC5904242
core_pubmed_pmc
Pharmacokinetic Optimization of Everolimus Dosing in Oncology: A Randomized Crossover Trial
Pharmacokinetic Optimization of Everolimus Dosing in Oncology: A Randomized Crossover Trial Abstract Abstract Background The mammalian target of rapamycin (mTOR) inhibitor everolimus is used in the treatment of breast cancer, neuroendocrine tumors, and renal cancer. The approved 10 mg once-daily dose is associated with...
PMC5415873
core_pubmed_pmc
Tracking Antibody Distribution with Near-Infrared Fluorescent Dyes: Impact of Dye Structure and Degree of Labeling on Plasma Clearance
Tracking Antibody Distribution with Near-Infrared Fluorescent Dyes: Impact of Dye Structure and Degree of Labeling on Plasma Clearance Abstract Monoclonal antibodies labeled with near-infrared (NIR) fluorophores have potential use in disease detection, intraoperative imaging, and pharmacokinetic characterization of the...
PMC11743709
core_pubmed_pmc
Exploring the antifungal potential of Cannabis sativa -derived stilbenoids and cannabinoids against novel targets through in silico protein interaction profiling
Exploring the antifungal potential of Cannabis sativa -derived stilbenoids and cannabinoids against novel targets through in silico protein interaction profiling Abstract Abstract Cannabinoid and stilbenoid compounds derived from Cannabis sativa were screened against eight specific fungal protein targets to identify po...
PMC11314343
core_pubmed_pmc
Improving the Solubility, Stability, and Bioavailability of Albendazole through Synthetic Salts
Improving the Solubility, Stability, and Bioavailability of Albendazole through Synthetic Salts Abstract Abstract Albendazole (ABZ) is a highly effective yet poorly water-soluble antiparasitic drug known to form salts (ABZ-FMA, ABZ-DTA, and ABZ-HCl) with fumaric acid (FMA), D-tartaric acid (DTA), and hydrochloric acid ...
PMC5909780
core_pubmed_pmc
Review of antimicrobial use and considerations in the elderly population
Review of antimicrobial use and considerations in the elderly population Abstract Pharmacologic management of infections in elderly patients presents multiple challenges to health care professionals due to variable pharmacokinetics, pharmacodynamics, and immune function. Age is a well-established risk factor for infect...
PMC7868528
core_pubmed_pmc
The Immunobiogram, a Novel In Vitro Assay to Evaluate Treatment Resistance in Patients Receiving Immunosuppressive Therapy
The Immunobiogram, a Novel In Vitro Assay to Evaluate Treatment Resistance in Patients Receiving Immunosuppressive Therapy Abstract Abstract Immunosuppressive drugs are widely used to treat several autoimmune disorders and prevent rejection after organ transplantation. However, intra-individual variations in the pharma...
PMC9540496
core_pubmed_pmc
Evaluation of the Effect of Abrocitinib on Drug Transporters by Integrated Use of Probe Drugs and Endogenous Biomarkers
Evaluation of the Effect of Abrocitinib on Drug Transporters by Integrated Use of Probe Drugs and Endogenous Biomarkers Abstract Abrocitinib is an oral Janus kinase 1 (JAK1) inhibitor currently approved in the United Kingdom for the treatment of moderate‐to‐severe atopic dermatitis (AD). As patients with AD may use med...
PMC7753424
core_pubmed_pmc
Investigational Treatments for COVID‐19 may Increase Ventricular Arrhythmia Risk Through Drug Interactions
Investigational Treatments for COVID‐19 may Increase Ventricular Arrhythmia Risk Through Drug Interactions Abstract Abstract Many drugs that have been proposed for treatment of coronavirus disease 2019 (COVID‐19) are reported to cause cardiac adverse events, including ventricular arrhythmias. In order to properly weigh...
PMC8470007
core_pubmed_pmc
In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System
In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System Abstract Abstract Diltiazem hydrochloride is a calcium channel blocker, which belongs to the family of benzothiazepines. It is commonly used to treat hypertension and atrial fibrillation. Even though t...
PMC10420877
core_pubmed_pmc
Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation
Nanocrystals of Mangiferin Using Design Expert: Preparation, Characterization, and Pharmacokinetic Evaluation Abstract Making nanoscale drug carriers could boost the bioavailability of medications that are slightly water soluble. One of the most promising approaches for enhancing the chemical stability and bioavailabil...
PMC9941642
core_pubmed_pmc
Bioequivalence study of ipratropium bromide inhalation aerosol using PBPK modelling
Bioequivalence study of ipratropium bromide inhalation aerosol using PBPK modelling Abstract Abstract Aims Systemic pharmacokinetic (PK) studies can reflect the overall exposure of orally inhaled drug Products (OIDPs) in the blood after inhalation into the lung and can be used to evaluate the bioequivalence of test and...
PMC7817048
core_pubmed_pmc
Lassa viral dynamics in non-human primates treated with favipiravir or ribavirin
Lassa viral dynamics in non-human primates treated with favipiravir or ribavirin Abstract Lassa fever is an haemorrhagic fever caused by Lassa virus (LASV). There is no vaccine approved against LASV and the only recommended antiviral treatment relies on ribavirin, despite limited evidence of efficacy. Recently, the nuc...
PMC5064743
core_pubmed_pmc
Evaluation of assay interference and interpretation of CXCR4 receptor occupancy results in a preclinical study with MEDI 3185, a fully human antibody to CXCR 4
Evaluation of assay interference and interpretation of CXCR4 receptor occupancy results in a preclinical study with MEDI 3185, a fully human antibody to CXCR 4 Abstract Background Receptor occupancy (RO) assays provide a means to measure the direct interaction of therapeutics with their cell surface targets. Free recep...
PMC10789046
core_pubmed_pmc
Establishing a trigger tool based on global trigger tools to identify adverse drug events in obstetric inpatients in China
Establishing a trigger tool based on global trigger tools to identify adverse drug events in obstetric inpatients in China Abstract Background Pregnant women belong to the special population of drug therapy, and their physiological state, pharmacokinetics and pharmacodynamics are significantly different from the genera...
PMC6273429
core_pubmed_pmc
Pharmacokinetics of Tyrosol Metabolites in Rats
Pharmacokinetics of Tyrosol Metabolites in Rats Abstract Tyrosol is considered a potential antioxidant; however, little is known regarding the pharmacokinetics of its metabolites. To study the pharmacokinetics of tyrosol-derived metabolites after oral administration of a single dose of tyrosol, we attempted to identify...
PMC4288004
core_pubmed_pmc
Lewis Sheiner ISoP/UCSF Lecturer Award: From Drug Use to Statistical Models and Vice Versa
Lewis Sheiner ISoP/UCSF Lecturer Award: From Drug Use to Statistical Models and Vice Versa Abstract Abstract I was very honored to receive the University of California, San Francisco, and the International Society of Pharmacometrics Lewis Sheiner lecturer award in May 2013. In the present perspective, I outline the mai...
PMC12706419
core_pubmed_pmc
Using Virtual Patients to Evaluate Dosing Strategies for Bispecifics With a Bell‐Shaped Efficacy Curve
Using Virtual Patients to Evaluate Dosing Strategies for Bispecifics With a Bell‐Shaped Efficacy Curve Abstract ABSTRACT Bispecific antibodies can be broadly divided into two categories: those that are pharmacologically active as either dimers bound to a single target or as trimers bound to both targets, and those that...
PMC5473807
core_pubmed_pmc
Distribution and kinetics of the Kv1.3-blocking peptide HsTX1[R14A] in experimental rats
Distribution and kinetics of the Kv1.3-blocking peptide HsTX1[R14A] in experimental rats Abstract Abstract The peptide HsTX1[R14A] is a potent and selective blocker of the voltage-gated potassium channel Kv1.3, which is a highly promising target for the treatment of autoimmune diseases and other conditions. In order to...
PMC8513371
core_pubmed_pmc
Comparison of aflibercept and bevacizumab in the treatment of type 1 retinopathy of prematurity
Comparison of aflibercept and bevacizumab in the treatment of type 1 retinopathy of prematurity Abstract Abstract Background To evaluate the outcome of intravitreal bevacizumab (IVB) and aflibercept (IVA) injection for patients with retinopathy of prematurity (ROP). Methods In this single-center retrospective cohort, t...
PMC5049594
core_pubmed_pmc
Ceftolozane/tazobactam pharmacokinetic/pharmacodynamic‐derived dose justification for phase 3 studies in patients with nosocomial pneumonia
Ceftolozane/tazobactam pharmacokinetic/pharmacodynamic‐derived dose justification for phase 3 studies in patients with nosocomial pneumonia Abstract Abstract Ceftolozane/tazobactam is an antipseudomonal antibacterial approved for the treatment of complicated urinary tract infections (cUTIs) and complicated intra‐abdomi...
PMC4182446
core_pubmed_pmc
Combining MK626, a Novel DPP-4 Inhibitor, and Low-Dose Monoclonal CD3 Antibody for Stable Remission of New-Onset Diabetes in Mice
Combining MK626, a Novel DPP-4 Inhibitor, and Low-Dose Monoclonal CD3 Antibody for Stable Remission of New-Onset Diabetes in Mice Abstract Combining immune intervention with therapies that directly influence the functional state of the β-cells is an interesting strategy in type 1 diabetes cure. Dipeptidyl peptidase-4 (...
PMC10363574
core_pubmed_pmc
Relative bioavailability of delamanid 50 mg tablets dispersed in water in healthy adult volunteers
Relative bioavailability of delamanid 50 mg tablets dispersed in water in healthy adult volunteers Abstract Abstract Aim Delamanid is a novel drug for the treatment of drug‐resistant tuberculosis, manufactured as 50‐mg solid and 25‐mg dispersible tablets. We evaluated the effects of dispersing the 50‐mg tablet, focusin...
PMC12250129
core_pubmed_pmc
Exploring the Therapeutic Potential of 177 Lu-PSMA-617 in a Mouse Model of Prostate Cancer Bone Metastases
Exploring the Therapeutic Potential of 177 Lu-PSMA-617 in a Mouse Model of Prostate Cancer Bone Metastases Abstract Abstract Prostate cancer is the second leading cause of cancer-related death in men, with metastatic castration-resistant prostate cancer (mCRPC) and bone metastases representing a critical clinical chall...
PMC11503523
core_pubmed_pmc
Metal Complexation for the Rational Design of Gemcitabine Formulations in Cancer Therapy
Metal Complexation for the Rational Design of Gemcitabine Formulations in Cancer Therapy Abstract Abstract Nanoformulation of chemotherapies represents a promising strategy to enhance outcomes in cancer therapy. Gemcitabine is a chemotherapeutic agent approved by the Food and Drug Administration for the treatment of va...
PMC7062412
core_pubmed_pmc
Study on the Formation of Antihypertensive Twin Drugs by Caffeic Acid and Ferulic Acid with Telmisartan
Study on the Formation of Antihypertensive Twin Drugs by Caffeic Acid and Ferulic Acid with Telmisartan Abstract Abstract Purpose This study aimed to synthesize twin drugs from cinnamic acid compounds, caffeic acid (CFA) and ferulic acid (FLA), which can antagonize endothelin-1 (ET-1) with telmisartan through ester bon...
PMC10891860
core_pubmed_pmc
Antifungal Resistance in Cryptococcal Infections
Antifungal Resistance in Cryptococcal Infections Abstract Antifungal therapy, especially with the azoles, could promote the incidence of less susceptible isolates of Cryptococcus neoformans and C. gattii species complexes (SC), mostly in developing countries. Given that these species affect mostly the immunocompromised...
PMC9031826
core_pubmed_pmc
Pharmacokinetics of Tildipirosin in Plasma, Milk, and Somatic Cells Following Intravenous, Intramuscular, and Subcutaneous Administration in Dairy Goats
Pharmacokinetics of Tildipirosin in Plasma, Milk, and Somatic Cells Following Intravenous, Intramuscular, and Subcutaneous Administration in Dairy Goats Abstract Tildipirosin is a macrolide currently authorized for treating respiratory diseases in cattle and swine. The disposition kinetics of tildipirosin in plasma, mi...
PMC3781849
core_pubmed_pmc
Effects of Ketoconazole on the Pharmacokinetics of Ponatinib in Healthy Subjects
Effects of Ketoconazole on the Pharmacokinetics of Ponatinib in Healthy Subjects Abstract Ponatinib is a BCR-ABL tyrosine kinase inhibitor (TKI) approved for the treatment of chronic myeloid leukemia and Philadelphia chromosome–positive acute lymphoblastic leukemia in patients resistant or intolerant to prior TKIs. In ...
PMC4085596
core_pubmed_pmc
Human Growth Hormone Delivery with a Microneedle Transdermal System: Preclinical Formulation, Stability, Delivery and PK of Therapeutically Relevant Doses
Human Growth Hormone Delivery with a Microneedle Transdermal System: Preclinical Formulation, Stability, Delivery and PK of Therapeutically Relevant Doses Abstract Abstract This study evaluated the feasibility of coating formulated recombinant human growth hormone (rhGH) on a titanium microneedle transdermal delivery s...
PMC4791286
core_pubmed_pmc
Puquitinib mesylate, an inhibitor of phosphatidylinositol 3-kinase p110δ, for treating relapsed or refractory non-Hodgkin's lymphoma
Puquitinib mesylate, an inhibitor of phosphatidylinositol 3-kinase p110δ, for treating relapsed or refractory non-Hodgkin's lymphoma Abstract Abstract Objectives To determine the safety of Puquitinib Mesylate (XC-302), an oral inhibitor of phosphatidylinositol 3-kinase, in treating relapsed or refractory non-Hodgkin's ...
PMC5845419
core_pubmed_pmc
Pharmacodynamic and pharmacokinetic effects and safety of verinurad in combination with allopurinol in adults with gout: a phase IIa, open-label study
Pharmacodynamic and pharmacokinetic effects and safety of verinurad in combination with allopurinol in adults with gout: a phase IIa, open-label study Abstract Abstract Objectives Verinurad (RDEA3170) is a high affinity, selective uric acid transporter (URAT1) inhibitor indevelopment for treating gout and asymptomatic ...
PMC12278471
core_pubmed_pmc
Zanamivir exposure in healthy rats and rats with acute lung injury
Zanamivir exposure in healthy rats and rats with acute lung injury Abstract Abstract Objectives The aim of this study was to evaluate the pharmacokinetics and lung penetration of zanamivir in healthy rats and rats with lipopolysaccharide (LPS)-induced acute lung injury (ALI). Materials and methods Three pharmacokinetic...
PMC10587312
core_pubmed_pmc
Evaluation of ceftriaxone pharmacokinetics in hospitalized Egyptian pediatric patients
Evaluation of ceftriaxone pharmacokinetics in hospitalized Egyptian pediatric patients Abstract This study aimed to evaluate ceftriaxone pharmacokinetics that affects the achievement of targets in the treatment of critically ill children (meningitis, pneumonia, urinary tract infection, peritonitis, and infective endoca...
PMC5699174
core_pubmed_pmc
The margin of internal exposure (MOIE) concept for dermal risk assessment based on oral toxicity data – A case study with caffeine
The margin of internal exposure (MOIE) concept for dermal risk assessment based on oral toxicity data – A case study with caffeine Abstract Highlights • The concept of Margin of Internal Exposure (MOIE) is proposed for route-to-route extrapolation. • It is an extension of the Margin of Exposure (MOE) approach for cosme...
PMC8859451
core_pubmed_pmc
Tofacitinib Suppresses Natural Killer Cells In Vitro and In Vivo : Implications for Amyotrophic Lateral Sclerosis
Tofacitinib Suppresses Natural Killer Cells In Vitro and In Vivo : Implications for Amyotrophic Lateral Sclerosis Abstract Abstract Amyotrophic lateral sclerosis (ALS) is a fatal and incurable neurodegenerative disease with few therapeutic options. However, the immune system, including natural killer (NK) cells, is lin...
PMC9221999
core_pubmed_pmc
Differences in Multicomponent Pharmacokinetics, Tissue Distribution, and Excretion of Tripterygium Glycosides Tablets in Normal and Adriamycin–Induced Nephrotic Syndrome Rat Models and Correlations With Efficacy and Hepatotoxicity
Differences in Multicomponent Pharmacokinetics, Tissue Distribution, and Excretion of Tripterygium Glycosides Tablets in Normal and Adriamycin–Induced Nephrotic Syndrome Rat Models and Correlations With Efficacy and Hepatotoxicity Abstract Abstract Tripterygium glycosides tablets (TGT) are widely used for treating neph...
PMC12150001
core_pubmed_pmc
Development and Validation of a Liquid Chromatography High‐Resolution Mass Spectrometry Method for Blood Desmopressin Quantification and Its Application in Hemophilia A Patients
Development and Validation of a Liquid Chromatography High‐Resolution Mass Spectrometry Method for Blood Desmopressin Quantification and Its Application in Hemophilia A Patients Abstract ABSTRACT Desmopressin (DDAVP), which indirectly increases Coagulation Factor VIII concentrations in the blood, is a common treatment ...
PMC12152399
core_pubmed_pmc
Studies on curcumin-glucoside in the prevention of alpha-synuclein aggregation
Studies on curcumin-glucoside in the prevention of alpha-synuclein aggregation Abstract Background α-synuclein (α-syn) deposition in the mid-brain region is one of the hallmark pathologies of Parkinson's disease (PD). The key steps involve the transformation of α-synuclein into a toxic oligomer and insoluble fibrillar ...