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PMC7478950
core_pubmed_pmc
Asian race and origin have no clinically meaningful effects on polatuzumab vedotin pharmacokinetics in patients with relapsed/refractory B-cell non-Hodgkin lymphoma
Asian race and origin have no clinically meaningful effects on polatuzumab vedotin pharmacokinetics in patients with relapsed/refractory B-cell non-Hodgkin lymphoma Abstract Purpose The CD79b-targeted antibody–drug conjugate polatuzumab vedotin (pola), alone and with chemoimmunotherapy, has clinical efficacy and a tole...
PMC10087980
core_pubmed_pmc
Population Pharmacokinetics of Oral Brepocitinib in Healthy Volunteers and Patients
Population Pharmacokinetics of Oral Brepocitinib in Healthy Volunteers and Patients Abstract Abstract Brepocitinib is a tyrosine kinase 2 and Janus kinase 1 inhibitor in development for treatment of inflammatory autoimmune diseases. This analysis aimed to add to the pharmacokinetic knowledge of the medication, through ...
PMC7783832
core_pubmed_pmc
A survey of therapeutic drug monitoring in a teaching hospital
A survey of therapeutic drug monitoring in a teaching hospital Abstract Abstract Objectives Therapeutic drug monitoring (TDM) is one of the tools that aim to improve and ensure the best therapeutic effects while avoiding drug toxicity. This study aimed to identify the clinical utilization and application of TDM at a ma...
PMC9880317
core_pubmed_pmc
Development and validation of two bioanalysis methods for the determination of etimicin in human serum and urine by liquid chromatography-tandem mass spectrometry: Applications to a human pharmacokinetic and breakpoint study
Development and validation of two bioanalysis methods for the determination of etimicin in human serum and urine by liquid chromatography-tandem mass spectrometry: Applications to a human pharmacokinetic and breakpoint study Abstract Etimicin is a fourth-generation aminoglycoside antibiotic. It has potent activity and ...
PMC9128966
core_pubmed_pmc
Evaluation of pharmacokinetic interactions of amoxicillin with ranitidine in healthy human volunteers of Karachi, Pakistan
Evaluation of pharmacokinetic interactions of amoxicillin with ranitidine in healthy human volunteers of Karachi, Pakistan Abstract Abstract Polypharmacy may be considered as the customary practice to provide optimum care services to patients but inter resulted in augmented probability of multiple drug interaction. Kee...
PMC5932779
core_pubmed_pmc
ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing’s syndrome
ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing’s syndrome Abstract Background Cushing’s syndrome in humans shares many similarities with its counterpart in dogs in terms of etiology (pituitary versus adrenal causes), clinical signs, and p...
PMC9174838
core_pubmed_pmc
Inhaled recombinant human IL-15 in dogs with naturally occurring pulmonary metastases from osteosarcoma or melanoma: a phase 1 study of clinical activity and correlates of response
Inhaled recombinant human IL-15 in dogs with naturally occurring pulmonary metastases from osteosarcoma or melanoma: a phase 1 study of clinical activity and correlates of response Abstract Purpose Although recombinant human interleukin-15 (rhIL-15) has generated much excitement as an immunotherapeutic agent for cancer...
PMC9967935
core_pubmed_pmc
Transferability of Published Population Pharmacokinetic Models for Apixaban and Rivaroxaban to Subjects with Obesity Treated for Venous Thromboembolism: A Systematic Review and External Evaluations
Transferability of Published Population Pharmacokinetic Models for Apixaban and Rivaroxaban to Subjects with Obesity Treated for Venous Thromboembolism: A Systematic Review and External Evaluations Abstract Apixaban and rivaroxaban have first-line use for many patients needing anticoagulation for venous thromboembolism...
PMC9563815
core_pubmed_pmc
Overcoming high level adenosine-mediated immunosuppression by DZD2269, a potent and selective A2aR antagonist
Overcoming high level adenosine-mediated immunosuppression by DZD2269, a potent and selective A2aR antagonist Abstract Background Adenosine is a potent immunosuppressant whose levels in the tumor microenvironment (TME) are often much higher than those in normal tissues. Binding of adenosine to its receptor A2aR activat...
PMC5659256
core_pubmed_pmc
Developing a novel dual PI3K–mTOR inhibitor from the prodrug of a metabolite
Developing a novel dual PI3K–mTOR inhibitor from the prodrug of a metabolite Abstract This study presents a process of developing a novel PI3K–mTOR inhibitor through the prodrug of a metabolite. The lead compound (compound 1) was identified with similar efficacy as that of NVP-BEZ235 in a tumor xenograft model, but the...
PMC11579193
core_pubmed_pmc
pyDarwin machine learning algorithms application and comparison in nonlinear mixed-effect model selection and optimization
pyDarwin machine learning algorithms application and comparison in nonlinear mixed-effect model selection and optimization Abstract Forward addition/backward elimination (FABE) has been the standard for population pharmacokinetic model selection (PPK) since NONMEM® was introduced. We investigated five machine learning ...
PMC3281083
core_pubmed_pmc
Impact of the Herbal Medicine Sophora flavescens on the Oral Pharmacokinetics of Indinavir in Rats: The Involvement of CYP3A and P-Glycoprotein
Impact of the Herbal Medicine Sophora flavescens on the Oral Pharmacokinetics of Indinavir in Rats: The Involvement of CYP3A and P-Glycoprotein Abstract Sophora flavescens is a Chinese medicinal herb used for the treatment of gastrointestinal hemorrhage, skin diseases, pyretic stranguria and viral hepatitis. In this st...
PMC12112792
core_pubmed_pmc
Dihydrogeodin from Fennellia flavipes Modulates Platelet Aggregation via Downregulation of Calcium Signaling, αIIbβ 3 Integrins, MAPK, and PI3K/Akt Pathways
Dihydrogeodin from Fennellia flavipes Modulates Platelet Aggregation via Downregulation of Calcium Signaling, αIIbβ 3 Integrins, MAPK, and PI3K/Akt Pathways Abstract Abstract Cardiovascular disease remains a leading cause of morbidity and mortality worldwide, frequently arising from platelet hyperactivation and subsequ...
PMC9924091
core_pubmed_pmc
Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine
Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine Abstract Nirmatrelvir (PF-07321332) is a nitrile-bearing small-molecule inhibitor that, in combination with ritonavir, is used to treat infections by severe acute respiratory sy...
PMC5651442
core_pubmed_pmc
Ponezumab in mild-to-moderate Alzheimer's disease: Randomized phase II PET-PIB study
Ponezumab in mild-to-moderate Alzheimer's disease: Randomized phase II PET-PIB study Abstract Abstract Introduction The safety, pharmacokinetics, and effect on peripheral and central amyloid β (Aβ) of multiple doses of ponezumab, an anti-Aβ monoclonal antibody, were characterized in subjects with mild-to-moderate Alzhe...
PMC7467913
core_pubmed_pmc
Preclinical Pharmacokinetic/Pharmacodynamic Studies and Clinical Trials in the Drug Development Process of EMA-Approved Antibacterial Agents: A Review
Preclinical Pharmacokinetic/Pharmacodynamic Studies and Clinical Trials in the Drug Development Process of EMA-Approved Antibacterial Agents: A Review Abstract Abstract Development of new antibacterial agents is necessary as drug-resistant bacteria are a threat to global health. In Europe, the European Medicines Agency...
PMC3485533
core_pubmed_pmc
Population pharmacokinetics of farletuzumab, a humanized monoclonal antibody against folate receptor alpha, in epithelial ovarian cancer
Population pharmacokinetics of farletuzumab, a humanized monoclonal antibody against folate receptor alpha, in epithelial ovarian cancer Abstract Abstract Purpose The purpose of this analysis was to develop a population pharmacokinetic model for farletuzumab, a humanized immunoglobulin (Ig)G 1 monoclonal antibody (mAb)...
PMC8482274
core_pubmed_pmc
Inadequate Cerebrospinal Fluid Concentrations of Available Salvage Agents Further Impedes the Optimal Treatment of Multidrug-Resistant Enterococcus faecium Meningitis and Bacteremia
Inadequate Cerebrospinal Fluid Concentrations of Available Salvage Agents Further Impedes the Optimal Treatment of Multidrug-Resistant Enterococcus faecium Meningitis and Bacteremia Abstract Background: Vancomycin-resistant Enterococcus faecium (VRE) in particular has evolved as an important cause of hospital acquired ...
PMC9723225
core_pubmed_pmc
Effects of intestinal microbiota on pharmacokinetics of cyclosporine a in rats
Effects of intestinal microbiota on pharmacokinetics of cyclosporine a in rats Abstract Abstract Background Intestinal microbiota has been confirmed to influencing the pharmacokinetic processes of a variety of oral drugs. However, the pharmacokinetic effects of the gut microbiota on cyclosporine A, a drug with a narrow...
PMC7217812
core_pubmed_pmc
Clinical Pharmacokinetics of Upadacitinib: Review of Data Relevant to the Rheumatoid Arthritis Indication
Clinical Pharmacokinetics of Upadacitinib: Review of Data Relevant to the Rheumatoid Arthritis Indication Abstract Abstract Upadacitinib is a Janus kinase 1 inhibitor developed for treatment of moderate to severe rheumatoid arthritis (RA) and was recently approved by the US Food and Drug Administration for this indicat...
PMC6853762
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Profiles of Cefiderocol, a Novel Siderophore Cephalosporin
Pharmacokinetic and Pharmacodynamic Profiles of Cefiderocol, a Novel Siderophore Cephalosporin Abstract Abstract Cefiderocol, a novel parenteral siderophore cephalosporin, exhibits potent in vitro activity and in vivo efficacy against most gram-negative bacteria, including carbapenem-resistant strains of Enterobacteria...
PMC9229563
core_pubmed_pmc
Pharmacokinetics and the Dermal Absorption of Bromochlorophene, a Cosmetic Preservative Ingredient, in Rats
Pharmacokinetics and the Dermal Absorption of Bromochlorophene, a Cosmetic Preservative Ingredient, in Rats Abstract Abstract The cosmetic industry has flourished in recent years. Accordingly, the safety of cosmetic ingredients is increasing. Bromochlorophene (BCP) is a commonly used cosmetic preservative. To evaluate ...
PMC9049328
core_pubmed_pmc
Pre-clinical pharmacokinetic and pharmacodynamic modelling study of 4-hydroxyisoleucine using validated ultra-performance liquid chromatography-tandem mass spectrometry †
Pre-clinical pharmacokinetic and pharmacodynamic modelling study of 4-hydroxyisoleucine using validated ultra-performance liquid chromatography-tandem mass spectrometry † Abstract Abstract A reliable and sensitive ultra-performance liquid chromatography-tandem mass spectrometry-based method has been developed for the e...
PMC12170649
core_pubmed_pmc
Therapeutic vancomycin monitoring: a comparative analysis of high-performance liquid chromatography and chemiluminescent microparticle immunoassay methods in liver transplant recipients
Therapeutic vancomycin monitoring: a comparative analysis of high-performance liquid chromatography and chemiluminescent microparticle immunoassay methods in liver transplant recipients Abstract Background Vancomycin is a glycopeptide antibiotic of choice for treating serious Gram-positive bacterial infections, includi...
PMC8027607
core_pubmed_pmc
Acute dose-dependent effects of lysergic acid diethylamide in a double-blind placebo-controlled study in healthy subjects
Acute dose-dependent effects of lysergic acid diethylamide in a double-blind placebo-controlled study in healthy subjects Abstract Abstract Growing interest has been seen in using lysergic acid diethylamide (LSD) in psychiatric research and therapy. However, no modern studies have evaluated subjective and autonomic eff...
PMC11704096
core_pubmed_pmc
Identification of novel 3-dehydroquinate dehydratase (DHQD) inhibitors for anti-tuberculosis activity: insights from virtual screening, molecular docking, and dynamics simulations
Identification of novel 3-dehydroquinate dehydratase (DHQD) inhibitors for anti-tuberculosis activity: insights from virtual screening, molecular docking, and dynamics simulations Abstract Tuberculosis (TB) remains a pressing global health concern, causing substantial mortality and morbidity despite existing drugs and ...
PMC7254632
core_pubmed_pmc
Can we optimise doxorubicin treatment regimens for children with cancer? Pharmacokinetic simulations and a Delphi consensus procedure
Can we optimise doxorubicin treatment regimens for children with cancer? Pharmacokinetic simulations and a Delphi consensus procedure Abstract Abstract Background Despite its cardiotoxicity doxorubicin is widely used for the treatment of paediatric malignancies. Current treatment regimens appear to be suboptimal as tre...
PMC9381914
core_pubmed_pmc
Machine learning algorithms to estimate everolimus exposure trained on simulated and patient pharmacokinetic profiles
Machine learning algorithms to estimate everolimus exposure trained on simulated and patient pharmacokinetic profiles Abstract Abstract Everolimus is an immunosuppressant with a small therapeutic index and large between‐patient variability. The area under the concentration versus time curve (AUC) is the best marker of ...
PMC6850607
core_pubmed_pmc
Population pharmacokinetics of brodalumab in patients with moderate to severe plaque psoriasis
Population pharmacokinetics of brodalumab in patients with moderate to severe plaque psoriasis Abstract Abstract Brodalumab is a fully human monoclonal antibody targeting the IL‐17 receptor A leading to an inhibition of the biological effect of IL‐17A, IL‐17F, IL‐17A/F heterodimer, IL‐17C and IL‐17E isoforms. It has sh...
PMC6351525
core_pubmed_pmc
Optimal dosing of dihydroartemisinin-piperaquine for seasonal malaria chemoprevention in young children
Optimal dosing of dihydroartemisinin-piperaquine for seasonal malaria chemoprevention in young children Abstract Abstract Young children are the population most severely affected by Plasmodium falciparum malaria. Seasonal malaria chemoprevention (SMC) with amodiaquine and sulfadoxine-pyrimethamine provides substantial ...
PMC4226839
core_pubmed_pmc
Irinophore C™, a lipid nanoparticle formulation of irinotecan, abrogates the gastrointestinal effects of irinotecan in a rat model of clinical toxicities
Irinophore C™, a lipid nanoparticle formulation of irinotecan, abrogates the gastrointestinal effects of irinotecan in a rat model of clinical toxicities Abstract Summary Irinotecan is a water-soluble camptothecin derivative with clinical activity against colorectal and small cell lung cancers and is currently a standa...
PMC2837469
core_pubmed_pmc
Quality of Graphite Target for Biological/Biomedical/Environmental Applications of 14 C-Accelerator Mass Spectrometry
Quality of Graphite Target for Biological/Biomedical/Environmental Applications of 14 C-Accelerator Mass Spectrometry Abstract Abstract Catalytic graphitization for 14 C-accelerator mass spectrometry ( 14 C-AMS) produced various forms of elemental carbon. Our high-throughput Zn reduction method (C/Fe = 1:5, 500 °C, 3 h...
PMC10536516
core_pubmed_pmc
Improved Pharmacokinetic Feasibilities of Mirabegron-1,2-Ethanedisulfonic Acid, Mirabegron-1,5-Naphthalenedisulfonic Acid, and Mirabegron-L-Pyroglutamic Acid as Co-Amorphous Dispersions in Rats and Mice
Improved Pharmacokinetic Feasibilities of Mirabegron-1,2-Ethanedisulfonic Acid, Mirabegron-1,5-Naphthalenedisulfonic Acid, and Mirabegron-L-Pyroglutamic Acid as Co-Amorphous Dispersions in Rats and Mice Abstract Mirabegron (MBR) is a β 3 -adrenoceptor agonist used for treating overactive bladder syndrome. Due to its po...
PMC7090185
core_pubmed_pmc
A First-in-Human Dose Finding Study of Camrelizumab in Patients with Advanced or Metastatic Cancer in Australia
A First-in-Human Dose Finding Study of Camrelizumab in Patients with Advanced or Metastatic Cancer in Australia Abstract Purpose Camrelizumab inhibits PD-1 in non-clinical models and showed typical non-clinical pharmacokinetic (PK) and safety profiles for an IgG4 monoclonal antibody. We report results from the First-in...
PMC7687182
core_pubmed_pmc
Safety and Pharmacokinetics of High‐Dose TAS‐303 in Healthy Japanese Volunteers: A Single‐Center, Single‐Blind, Randomized, Placebo‐Controlled, Parallel‐Group, Multiple‐Ascending‐Dose Study
Safety and Pharmacokinetics of High‐Dose TAS‐303 in Healthy Japanese Volunteers: A Single‐Center, Single‐Blind, Randomized, Placebo‐Controlled, Parallel‐Group, Multiple‐Ascending‐Dose Study Abstract Abstract Preclinical data of TAS‐303 (4‐piperidinyl 2,2‐diphenyl‐2‐[propoxy‐1,1,2,2,3,3,3‐ d 7 ] acetate hydrochloride), ...
PMC10787208
core_pubmed_pmc
Eliciting the antitumor immune response with a conditionally activated PD‐L1 targeting antibody analyzed with a quantitative systems pharmacology model
Eliciting the antitumor immune response with a conditionally activated PD‐L1 targeting antibody analyzed with a quantitative systems pharmacology model Abstract Abstract Conditionally activated molecules, such as Probody therapeutics (PbTx), have recently been investigated to improve antitumoral response while reducing...
PMC6782035
core_pubmed_pmc
Pharmacokinetics of prednisolone in children: an open-label, randomised, two-treatment cross-over trial investigating the bioequivalence of different prednisolone formulations in children with airway disease
Pharmacokinetics of prednisolone in children: an open-label, randomised, two-treatment cross-over trial investigating the bioequivalence of different prednisolone formulations in children with airway disease Abstract Introduction One in three Danish children under 3 years of age experience asthma-like symptoms, and one...
PMC5890768
core_pubmed_pmc
Modelling of mycobacterial load reveals bedaquiline’s exposure–response relationship in patients with drug-resistant TB
Modelling of mycobacterial load reveals bedaquiline’s exposure–response relationship in patients with drug-resistant TB Abstract Abstract Background Bedaquiline has been shown to reduce time to sputum culture conversion (SCC) and increase cure rates in patients with drug-resistant TB, but the influence of drug exposure...
PMC7382147
core_pubmed_pmc
An effective UFLC–MS/MS method used to study pharmacokinetics of major constituents of Fukeqianjin formula in rat plasma
An effective UFLC–MS/MS method used to study pharmacokinetics of major constituents of Fukeqianjin formula in rat plasma Abstract Background Fukeqianjin formula (FKQJF) is a Chinese medicine prescription, which has been widely used individually or in combination with other western medicine for the treatment of various ...
PMC9946901
core_pubmed_pmc
The Evaluation of the Efficacy and Safety of Midazolam Nasal Spray in Patients With Seizure Clusters: A Systematic Review and Meta-Analysis
The Evaluation of the Efficacy and Safety of Midazolam Nasal Spray in Patients With Seizure Clusters: A Systematic Review and Meta-Analysis Abstract Abstract Midazolam nasal spray (MDZ-NS) is a new emerging rescue medication that suppresses epileptic seizures. Until now, few studies, pharmacokinetic (PK) and pharmacody...
PMC7898678
core_pubmed_pmc
The Burden of the Serious and Difficult-to-Treat Infections and a New Antibiotic Available: Cefiderocol
The Burden of the Serious and Difficult-to-Treat Infections and a New Antibiotic Available: Cefiderocol Abstract Background: Infection is a disease that can occur due to the entrance of a virus, bacteria, and other infectious agents. Cefiderocol is innovative cephalosporin drug that belongs to a special class of antibi...
PMC10973027
core_pubmed_pmc
Evaluation and Application of a PET Tracer in Preclinical and Phase 1 Studies to Determine the Brain Biodistribution of Minzasolmin (UCB0599)
Evaluation and Application of a PET Tracer in Preclinical and Phase 1 Studies to Determine the Brain Biodistribution of Minzasolmin (UCB0599) Abstract Abstract Purpose Minzasolmin (UCB0599) is an orally administered, small molecule inhibitor of ASYN misfolding in development as a potential disease-modifying therapy for...
PMC11215271
core_pubmed_pmc
Differentiation between primary central nervous system lymphomas and gliomas according to pharmacokinetic parameters derived from dynamic contrast-enhanced magnetic resonance imaging
Differentiation between primary central nervous system lymphomas and gliomas according to pharmacokinetic parameters derived from dynamic contrast-enhanced magnetic resonance imaging Abstract Abstract Purpose It is difficult to differentiate between primary central nervous system lymphoma and primary glioblastoma due t...
PMC12467171
core_pubmed_pmc
Development of HPLC-MS/MS Method for Simultaneous Detection of Esketamine and Norketamine: Application to Pharmacokinetics Drug Interactions Affected by Dexmedetomidine
Development of HPLC-MS/MS Method for Simultaneous Detection of Esketamine and Norketamine: Application to Pharmacokinetics Drug Interactions Affected by Dexmedetomidine Abstract Abstract Purpose Dexmedetomidine (DEX) and esketamine (ESK) are often used together during anesthesia. This study aimed to establish a sensiti...
PMC8424097
core_pubmed_pmc
Population Pharmacokinetics of Polymyxin B and Dosage Optimization in Renal Transplant Patients
Population Pharmacokinetics of Polymyxin B and Dosage Optimization in Renal Transplant Patients Abstract Abstract Currently, polymyxin B has been widely used in the treatment of multidrug-resistant Gram-negative pathogen infections. Due to the limited pharmacokinetic/pharmacodynamic data, the optimal dosage regimen for...
PMC7187203
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non–Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non–Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers Abstract Abstract Tropifexor (LJN452) is a potent, orally available, non–bile acid farnesoid X receptor agonist under clinical development for chronic liver diseases. Here, we pr...
PMC3423889
core_pubmed_pmc
Adjuvant Bidirectional Chemotherapy with Intraperitoneal Pemetrexed Combined with Intravenous Cisplatin for Diffuse Malignant Peritoneal Mesothelioma
Adjuvant Bidirectional Chemotherapy with Intraperitoneal Pemetrexed Combined with Intravenous Cisplatin for Diffuse Malignant Peritoneal Mesothelioma Abstract Abstract Cytoreductive surgery (CRS) with heated intraoperative intraperitoneal chemotherapy (HIPEC) has emerged as optimal treatment for diffuse malignant perit...
PMC11124465
core_pubmed_pmc
A Sensitive Assay for Unbound Docetaxel Using Ultrafiltration plus HPLC-MS and Its Application to a Clinical Study
A Sensitive Assay for Unbound Docetaxel Using Ultrafiltration plus HPLC-MS and Its Application to a Clinical Study Abstract Abstract Introduction: Docetaxel, a taxane used in the treatment of solid tumours, exerts pharmacological activity when in its unbound form. We report a sensitive assay to quantify unbound docetax...
PMC8961198
core_pubmed_pmc
TRUE-1: Trial of Repurposed Unithiol for snakebite Envenoming phase 1 (safety, tolerability, pharmacokinetics and pharmacodynamics in healthy Kenyan adults)
TRUE-1: Trial of Repurposed Unithiol for snakebite Envenoming phase 1 (safety, tolerability, pharmacokinetics and pharmacodynamics in healthy Kenyan adults) Abstract Background: Snakebites affect over 5 million people each year, and over 100,000 per year die as a result. The only available treatment is antivenom, which...
PMC11602888
core_pubmed_pmc
Population pharmacokinetic/target engagement modelling of tozorakimab in healthy volunteers and patients with chronic obstructive pulmonary disease
Population pharmacokinetic/target engagement modelling of tozorakimab in healthy volunteers and patients with chronic obstructive pulmonary disease Abstract Abstract Aims This study describes the pharmacokinetic (PK)/target engagement (TE) relationship of tozorakimab, an anti‐interleukin (IL)‐33 antibody, by building a...
PMC8513154
core_pubmed_pmc
Structural principles of insulin formulation and analog design: A century of innovation
Structural principles of insulin formulation and analog design: A century of innovation Abstract Abstract Background The discovery of insulin in 1921 and its near-immediate clinical use initiated a century of innovation. Advances extended across a broad front, from the stabilization of animal insulin formulations to th...
PMC4605235
core_pubmed_pmc
Preparation, characterization, in vivo pharmacokinetics, and biodistribution of polymeric micellar dimethoxycurcumin for tumor targeting
Preparation, characterization, in vivo pharmacokinetics, and biodistribution of polymeric micellar dimethoxycurcumin for tumor targeting Abstract Dimethoxycurcumin (DMC) is an analog of curcumin with superior efficacy in various disease models. Currently, drug delivery system research on DMC is very limited, and it has...
PMC7806714
core_pubmed_pmc
Statins for the prevention of proliferative vitreoretinopathy: cellular responses in cultured cells and clinical statin concentrations in the vitreous
Statins for the prevention of proliferative vitreoretinopathy: cellular responses in cultured cells and clinical statin concentrations in the vitreous Abstract Proliferative vitreoretinopathy (PVR) with rhegmatogenous retinal detachment (RRD) is a complex inflammatory ocular disease. Statins are widely used cholesterol...
PMC6864417
core_pubmed_pmc
Everolimus Exposure as a Predictor of Toxicity in Renal Cell Cancer Patients in the Adjuvant Setting: Results of a Pharmacokinetic Analysis for SWOG S0931 (EVEREST), a Phase III Study ( NCT01120249 )
Everolimus Exposure as a Predictor of Toxicity in Renal Cell Cancer Patients in the Adjuvant Setting: Results of a Pharmacokinetic Analysis for SWOG S0931 (EVEREST), a Phase III Study ( NCT01120249 ) Abstract Abstract Background: S0931 is assessing recurrence-free survival in renal cell carcinoma (RCC) patients randomi...
PMC12776353
core_pubmed_pmc
Pharmacodynamic individualization of phage therapy against a KPC-5-producing Pseudomonas aeruginosa
Pharmacodynamic individualization of phage therapy against a KPC-5-producing Pseudomonas aeruginosa Abstract Abstract Background There is a resurgence of interest in bacteriophage (phage) therapy as antimicrobials, resulting from growing antimicrobial resistance to small-molecule antibiotics. Phages are bacterial virus...
PMC12200682
core_pubmed_pmc
SHR-A1811, a novel anti-HER2 antibody–drug conjugate with optimal drug-to-antibody ratio, efficient tumor killing potency, and favorable safety profiles
SHR-A1811, a novel anti-HER2 antibody–drug conjugate with optimal drug-to-antibody ratio, efficient tumor killing potency, and favorable safety profiles Abstract Abstract HER2-targeting antibody–drug conjugates (ADCs), especially trastuzumab deruxtecan (T-DXd), have revolutionized the treatment landscape of HER2-expres...
PMC9287224
core_pubmed_pmc
Liver Cirrhosis Affects the Pharmacokinetics of the Six Substrates of the Basel Phenotyping Cocktail Differently
Liver Cirrhosis Affects the Pharmacokinetics of the Six Substrates of the Basel Phenotyping Cocktail Differently Abstract Abstract Background Activities of hepatic cytochrome P450 enzymes (CYPs) are relevant for hepatic clearance of drugs and known to be decreased in patients with liver cirrhosis. Several studies have ...
PMC8467065
core_pubmed_pmc
Evaluation of the Pharmacokinetics of Intranasal Drug Delivery for Targeting Cervical Lymph Nodes in Rats
Evaluation of the Pharmacokinetics of Intranasal Drug Delivery for Targeting Cervical Lymph Nodes in Rats Abstract A well-developed lymphatic network is located under the nasal mucosa, and a few drugs that permeate the nasal mucosa are absorbed into the lymphatic capillaries. Lymph from the nasal cavity flows to the ce...
PMC11279552
core_pubmed_pmc
Unveiling Moroccan Nature’s Arsenal: A Computational Molecular Docking, Density Functional Theory, and Molecular Dynamics Study of Natural Compounds against Drug-Resistant Fungal Infections
Unveiling Moroccan Nature’s Arsenal: A Computational Molecular Docking, Density Functional Theory, and Molecular Dynamics Study of Natural Compounds against Drug-Resistant Fungal Infections Abstract Candida albicans and Aspergillus fumigatus are recognized as significant fungal pathogens, responsible for various human ...
PMC6223703
core_pubmed_pmc
A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose, Multiple Dose, and Food Effect Trial of the Safety, Tolerability and Pharmacokinetics of Highly Purified Cannabidiol in Healthy Subjects
A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose, Multiple Dose, and Food Effect Trial of the Safety, Tolerability and Pharmacokinetics of Highly Purified Cannabidiol in Healthy Subjects Abstract Abstract Background A formal single ascending and multiple dose pharmacokinetic (PK) trial of ...
PMC4076805
core_pubmed_pmc
Evaluation of 4β-Hydroxycholesterol as a Clinical Biomarker of CYP3A4 Drug Interactions Using a Bayesian Mechanism–Based Pharmacometric Model
Evaluation of 4β-Hydroxycholesterol as a Clinical Biomarker of CYP3A4 Drug Interactions Using a Bayesian Mechanism–Based Pharmacometric Model Abstract A Bayesian mechanism–based pharmacokinetic/pharmacodynamic model of cytochrome P450 3A4 (CYP3A4) activity was developed based on a clinical study of the effects of ketoc...
PMC12300650
core_pubmed_pmc
Development and Characterization of a New Oral Antileishmanial Bis(pyridine-2-Carboxamidine) Drug Through Innovative Dissolution Testing in Biorelevant Media Combined with Pharmacokinetic Studies
Development and Characterization of a New Oral Antileishmanial Bis(pyridine-2-Carboxamidine) Drug Through Innovative Dissolution Testing in Biorelevant Media Combined with Pharmacokinetic Studies Abstract Abstract Background/Objectives : Currently there are very few effective oral antileishmanial treatments. In this st...
PMC10342511
core_pubmed_pmc
Opioid Analgesics after Bariatric Surgery: A Scoping Review to Evaluate Physiological Risk Factors for Opioid-Related Harm
Opioid Analgesics after Bariatric Surgery: A Scoping Review to Evaluate Physiological Risk Factors for Opioid-Related Harm Abstract The persisting use of opioids following bariatric surgery has emerged as a prevalent complication, heightening the probability of opioid-related harm (ORM), such as opioid-related fataliti...
PMC12857141
core_pubmed_pmc
Receptor identification and in vivo efficacy of a lytic phage vB_EcoStr-FJ63A against colistin-resistant Escherichia coli
Receptor identification and in vivo efficacy of a lytic phage vB_EcoStr-FJ63A against colistin-resistant Escherichia coli Abstract Abstract Bacteriophages (phages), as natural predators of bacteria, represent promising alternatives to antibiotics. However, challenges such as narrow host range and insufficient pharmacok...
PMC10674228
core_pubmed_pmc
Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization
Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization Abstract Abstract Bioavailability is an important biopharmaceutical characteristic of active pharmaceutical ingredients (APIs) that is often correlated with their solubility in water. One of the methods of increasing ...
PMC5625157
core_pubmed_pmc
Lack of clinically important PK interaction between coformulated ledipasvir/sofosbuvir and rilpivirine/emtricitabine/tenofovir alafenamide
Lack of clinically important PK interaction between coformulated ledipasvir/sofosbuvir and rilpivirine/emtricitabine/tenofovir alafenamide Abstract Abstract The drug–drug interaction (DDI) potential between the fixed‐dose combinations of ledipasvir/sofosbuvir 90/400 mg for hepatitis C virus and emtricitabine/rilpivirin...
PMC10861834
core_pubmed_pmc
Pharmacokinetic Comparison Between a Fixed-Dose Combination of Atorvastatin/Omega-3-Acid Ethyl Esters and the Corresponding Loose Combination in Healthy Korean Male Subjects
Pharmacokinetic Comparison Between a Fixed-Dose Combination of Atorvastatin/Omega-3-Acid Ethyl Esters and the Corresponding Loose Combination in Healthy Korean Male Subjects Abstract Abstract Purpose Statins are widely used in combination with omega-3 fatty acids for the treatment of patients with dyslipidemia. The aim...
PMC8342882
core_pubmed_pmc
Prediction of Rivaroxaban-Rifampin Interaction After Major Orthopedic Surgery: Physiologically Based Pharmacokinetic Modeling and Simulation
Prediction of Rivaroxaban-Rifampin Interaction After Major Orthopedic Surgery: Physiologically Based Pharmacokinetic Modeling and Simulation Abstract Abstract Rivaroxaban is commonly used for the prophylaxis of venous thromboembolism (VTE) for patients undergoing major orthopedic surgery. Rivaroxaban is primarily elimi...
PMC6587524
core_pubmed_pmc
The JAK1 Inhibitor Upadacitinib Has No Effect on the Pharmacokinetics of Levonorgestrel and Ethinylestradiol: A Study in Healthy Female Subjects
The JAK1 Inhibitor Upadacitinib Has No Effect on the Pharmacokinetics of Levonorgestrel and Ethinylestradiol: A Study in Healthy Female Subjects Abstract Abstract Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. Oral contraceptives are...
PMC5506666
core_pubmed_pmc
Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac
Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac Abstract The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and eval...
PMC8567945
core_pubmed_pmc
Saikosaponin D: review on the antitumour effects, toxicity and pharmacokinetics
Saikosaponin D: review on the antitumour effects, toxicity and pharmacokinetics Abstract Abstract Context Bupleuri Radix , the dried root of Bupleurum chinense DC and Bupleurum scorzonerifolium Willd (Apiaceae), is an important medicinal herb widely used to treat cancers for hundreds of years in Asian countries. As the...
PMC10887906
core_pubmed_pmc
Exploring the Link between Altitude of Residence and Smoking Patterns in the United States
Exploring the Link between Altitude of Residence and Smoking Patterns in the United States Abstract Abstract Introduction: Smoking-related diseases affect 16 million Americans, causing approximately 480,000 deaths annually. The prevalence of cigarette smoking varies regionally across the United States, and previous res...
PMC11938900
core_pubmed_pmc
In silico exploration of bioactive secondary metabolites with anesthetic effects on sodium channels Nav 1.7, 1.8, and 1.9 in painful human dental pulp
In silico exploration of bioactive secondary metabolites with anesthetic effects on sodium channels Nav 1.7, 1.8, and 1.9 in painful human dental pulp Abstract Abstract Aim: To investigate the efficacy of medicinal plant bioactive secondary metabolites as inhibitors of voltage-gated sodium channels (Nav1.7, Nav1.8, and...
PMC5600110
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic integration and modelling of oxytetracycline for the porcine pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida
Pharmacokinetic/pharmacodynamic integration and modelling of oxytetracycline for the porcine pneumonia pathogens Actinobacillus pleuropneumoniae and Pasteurella multocida Abstract Abstract Pharmacokinetic–pharmacodynamic (PK/PD) integration and modelling were used to predict dosage schedules of oxytetracycline for two ...
PMC4436099
core_pubmed_pmc
Pharmacokinetics and the optimal regimen for levofloxacin in critically ill patients receiving continuous hemodiafiltration
Pharmacokinetics and the optimal regimen for levofloxacin in critically ill patients receiving continuous hemodiafiltration Abstract Abstract The aim of this study was to establish the pharmacokinetics of levofloxacin (LVFX) and determine the optimal dose of this drug in critically ill patients receiving continuous hem...
PMC10977013
core_pubmed_pmc
Human monoclonal antibody F61 nasal spray effectively protected high-risk populations from SARS-CoV-2 variants during the COVID-19 pandemic from late 2022 to early 2023 in China
Human monoclonal antibody F61 nasal spray effectively protected high-risk populations from SARS-CoV-2 variants during the COVID-19 pandemic from late 2022 to early 2023 in China Abstract ABSTRACT Following the national dynamic zero-COVID strategy adjustment, the utilization of broad-spectrum nasal neutralizing antibodi...
PMC11176165
core_pubmed_pmc
Combating the causative agent of amoebic keratitis, Acanthamoeba castellanii , using Padina pavonica alcoholic extract: toxicokinetic and molecular docking approaches
Combating the causative agent of amoebic keratitis, Acanthamoeba castellanii , using Padina pavonica alcoholic extract: toxicokinetic and molecular docking approaches Abstract Natural products play a significant role in providing the current demand as antiparasitic agents, which offer an attractive approach for the dis...
PMC10058213
core_pubmed_pmc
In Silico Exploration of Metabolically Active Peptides as Potential Therapeutic Agents against Amyotrophic Lateral Sclerosis
In Silico Exploration of Metabolically Active Peptides as Potential Therapeutic Agents against Amyotrophic Lateral Sclerosis Abstract Abstract Amyotrophic lateral sclerosis (ALS) is regarded as a fatal neurodegenerative disease that is featured by progressive damage of the upper and lower motor neurons. To date, over 4...
PMC10386382
core_pubmed_pmc
Therapeutic Potential and Predictive Pharmaceutical Modeling of Stilbenes in Cannabis sativa
Therapeutic Potential and Predictive Pharmaceutical Modeling of Stilbenes in Cannabis sativa Abstract Cannabis sativa is a plant used for recreational and therapeutic purposes; however, many of the secondary metabolites in the plant have not been thoroughly investigated. Stilbenes are a class of compounds with demonstr...
PMC8464829
core_pubmed_pmc
Review: Influence of the CYP450 Genetic Variation on the Treatment of Psychotic Disorders
Review: Influence of the CYP450 Genetic Variation on the Treatment of Psychotic Disorders Abstract Abstract Second-generation antipsychotic metabolism is mainly carried out by the CYP450 superfamily, which is highly polymorphic. Therefore, knowing the influence of the different known CYP450 polymorphisms on antipsychot...
PMC11949362
core_pubmed_pmc
Population pharmacokinetic analysis of intravenous voriconazole in cancer patients
Population pharmacokinetic analysis of intravenous voriconazole in cancer patients Abstract Purpose The pharmacokinetics of voriconazole have been studied across various populations but data specific to the Pakistani cancer population has not yet been reported. The aim of present study was to explore and identify covar...
PMC3637032
core_pubmed_pmc
Effect of famotidine on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor
Effect of famotidine on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor Abstract Background Apixaban is an oral, selective, direct factor Xa inhibitor approved for thromboprophylaxis after orthopedic surgery and stroke prevention in patients with atrial fibrillation, and under development for treat...
PMC12508793
core_pubmed_pmc
Distribution of CYP2D6 multiplication, CYP2D6*5, and clinical implications in postoperative patients receiving tramadol analgesia in the Minangkabau ethnic group, Indonesia
Distribution of CYP2D6 multiplication, CYP2D6*5, and clinical implications in postoperative patients receiving tramadol analgesia in the Minangkabau ethnic group, Indonesia Abstract Background Cytochrome P450 2D6 (CYP2D6) is an important enzyme that metabolizes commonly used drugs, such as tramadol hydrochloride. Genet...
PMC4230447
core_pubmed_pmc
Modeling bioavailability to organs protected by biological barriers
Modeling bioavailability to organs protected by biological barriers Abstract Abstract Computational pharmacokinetic (PK) modeling gives access to drug concentration vs. time profiles in target organs and allows better interpretation of clinical observations of therapeutic or toxic effects. Physiologically-based PK (PBP...
PMC12515116
core_pubmed_pmc
Pharmacokinetics of UGN‑102, an investigational mitomycin‑containing reverse thermal gel for the treatment of non-muscle invasive bladder cancer
Pharmacokinetics of UGN‑102, an investigational mitomycin‑containing reverse thermal gel for the treatment of non-muscle invasive bladder cancer Abstract Purpose To evaluate the pharmacokinetic properties of UGN-102, a mitomycin-containing reverse thermal gel. Methods Twelve patients with NMIBC received 6 once-weekly i...
PMC6587371
core_pubmed_pmc
Intravenous vortioxetine to accelerate onset of effect in major depressive disorder: a 2-week, randomized, double-blind, placebo-controlled study
Intravenous vortioxetine to accelerate onset of effect in major depressive disorder: a 2-week, randomized, double-blind, placebo-controlled study Abstract This 2-week randomized, double-blind, placebo-controlled fixed-dose study (NCT02919501) explored the potential of accelerating onset of antidepressant efficacy and p...
PMC3509570
core_pubmed_pmc
Bioavailability and Brain-Targeting of Geniposide in Gardenia-Borneol Co-Compound by Different Administration Routes in Mice
Bioavailability and Brain-Targeting of Geniposide in Gardenia-Borneol Co-Compound by Different Administration Routes in Mice Abstract Both geniposide (Ge) and borneol (Bo) are bioactive substances derived from traditional Chinese medicine. Injections containing co-compound of Gardenia-Borneol are widely used for stroke...
PMC12388763
core_pubmed_pmc
Experimental Evidence of Caffeic Acid’s Neuroprotective Activity in Alzheimer’s Disease: In Vitro, In Vivo, and Delivery-Based Insights
Experimental Evidence of Caffeic Acid’s Neuroprotective Activity in Alzheimer’s Disease: In Vitro, In Vivo, and Delivery-Based Insights Abstract Abstract Background and Objectives : Alzheimer’s disease (AD) is a complex neurodegenerative disorder marked by cholinergic deficits, oxidative stress, amyloid-β (Aβ) aggregat...
PMC7984088
core_pubmed_pmc
Renal water conservation and the volume kinetics of fluid‐induced diuresis: A retrospective analysis of two cohorts of elderly men
Renal water conservation and the volume kinetics of fluid‐induced diuresis: A retrospective analysis of two cohorts of elderly men Abstract Abstract Renal water conservation after an overnight fast mirrors the habitual intake of liquid. The hypothesis in the present study was that water conservation influences the diur...
PMC9827893
core_pubmed_pmc
Semimechanistic Physiologically‐Based Pharmacokinetic/Pharmacodynamic Model Informing Epcoritamab Dose Selection for Patients With B‐Cell Lymphomas
Semimechanistic Physiologically‐Based Pharmacokinetic/Pharmacodynamic Model Informing Epcoritamab Dose Selection for Patients With B‐Cell Lymphomas Abstract Epcoritamab is a CD3xCD20 bispecific antibody (bsAb) that induces T‐cell–mediated cytotoxicity against CD20‐positive B cells. Target engagement and crosslinking of...
PMC10949877
core_pubmed_pmc
Invasive fungal infections and oomycoses in cats 2. Antifungal therapy
Invasive fungal infections and oomycoses in cats 2. Antifungal therapy Abstract Clinical relevance: Invasive fungal infections (IFIs) and oomycoses (hereafter termed invasive fungal-like infections [IFLIs]) are characterised by penetration of tissues by fungal elements. The environment is the most common reservoir of i...
PMC8304499
core_pubmed_pmc
Polyester Polymeric Nanoparticles as Platforms in the Development of Novel Nanomedicines for Cancer Treatment
Polyester Polymeric Nanoparticles as Platforms in the Development of Novel Nanomedicines for Cancer Treatment Abstract Simple Summary Despite the existence of powerful therapeutic agents, cancer is still an incurable disease in many clinical scenarios. In this regard, nanomedicine and particularly polymeric nanoparticl...
PMC4036650
core_pubmed_pmc
Cannabinoid-Induced Hyperemesis: A Conundrum—From Clinical Recognition to Basic Science Mechanisms
Cannabinoid-Induced Hyperemesis: A Conundrum—From Clinical Recognition to Basic Science Mechanisms Abstract Abstract Cannabinoids are used clinically on a subacute basis as prophylactic agonist antiemetics for the prevention of nausea and vomiting caused by chemotherapeutics. Cannabinoids prevent vomiting by inhibition...
PMC5301423
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic modeling of sarafloxacin against avian pathogenic Escherichia coli in Muscovy ducks
Pharmacokinetic and pharmacodynamic modeling of sarafloxacin against avian pathogenic Escherichia coli in Muscovy ducks Abstract Background This study focused on utilizing pharmacokinetics/pharmacodynamics (PK/PD) modeling to optimize therapeutic dosage regimens of sarafloxacin against avian pathogenic Escherichia. col...
PMC11255622
core_pubmed_pmc
Safety, Tolerability, and Pharmacodynamics of AZD3366 (Optimized Human CD39L3 Apyrase) Alone and in Combination With Ticagrelor and Acetylsalicylic Acid: A Phase 1, Randomized, Placebo‐Controlled Study
Safety, Tolerability, and Pharmacodynamics of AZD3366 (Optimized Human CD39L3 Apyrase) Alone and in Combination With Ticagrelor and Acetylsalicylic Acid: A Phase 1, Randomized, Placebo‐Controlled Study Abstract Abstract Background ADP and ATP are importantly involved in vascular and thrombotic homeostasis, via multiple...
PMC11128879
core_pubmed_pmc
Physiologically based pharmacokinetic model for predicting the biodistribution of albumin nanoparticles after induction and recovery from acute lung injury
Physiologically based pharmacokinetic model for predicting the biodistribution of albumin nanoparticles after induction and recovery from acute lung injury Abstract Abstract The application of nanomedicine in the treatment of acute lung injury (ALI) has great potential for the development of new therapeutic strategies....
PMC3608883
core_pubmed_pmc
An Open-Label Investigation of the Pharmacokinetic Profiles of Lisdexamfetamine Dimesylate and Venlafaxine Extended-Release, Administered Alone and in Combination, in Healthy Adults
An Open-Label Investigation of the Pharmacokinetic Profiles of Lisdexamfetamine Dimesylate and Venlafaxine Extended-Release, Administered Alone and in Combination, in Healthy Adults Abstract Background Lisdexamfetamine dimesylate (LDX), a prodrug consisting of d -amphetamine and l -lysine, is being studied in clinical ...
PMC6677645
core_pubmed_pmc
Questionable Industry-Sponsored Postneonatal Pediatric Studies in Slovenia
Questionable Industry-Sponsored Postneonatal Pediatric Studies in Slovenia Abstract Background US and EU pediatric laws promote industry-sponsored pediatric studies, based on the therapeutic orphans concept that claims discrimination of children in drug treatment and drug development. Objective We investigated the medi...
PMC5083757
core_pubmed_pmc
Effect of veliparib (ABT-888) on cardiac repolarization in patients with advanced solid tumors: a randomized, placebo-controlled crossover study
Effect of veliparib (ABT-888) on cardiac repolarization in patients with advanced solid tumors: a randomized, placebo-controlled crossover study Abstract Abstract Purpose Veliparib (ABT-888) is an orally bioavailable potent inhibitor of poly(ADP-ribose) polymerase (PARP)-1 and PARP-2. This phase 1 study evaluated the e...
PMC9010192
core_pubmed_pmc
Determination of Senegenin and Tenuifolin in Mouse Blood by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry and Their Pharmacokinetics
Determination of Senegenin and Tenuifolin in Mouse Blood by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry and Their Pharmacokinetics Abstract Abstract An ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of senegenin and tenuifolin in...