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PMC4703389
core_pubmed_pmc
A Novel Platform for the Potentiation of Therapeutic Antibodies Based on Antigen-Dependent Formation of IgG Hexamers at the Cell Surface
A Novel Platform for the Potentiation of Therapeutic Antibodies Based on Antigen-Dependent Formation of IgG Hexamers at the Cell Surface Abstract Abstract IgG antibodies can organize into ordered hexamers on cell surfaces after binding their antigen. These hexamers bind the first component of complement C1 inducing com...
PMC12401645
core_pubmed_pmc
Administration Studies in Equine Antidoping Research: Designing Scientific Investigations to Effectively Direct Medication Control in Racehorses
Administration Studies in Equine Antidoping Research: Designing Scientific Investigations to Effectively Direct Medication Control in Racehorses Abstract ABSTRACT Pharmacokinetics is the study of the movement of drug in the body and includes the processes of absorption, distribution, metabolism, and excretion. Pharmaco...
PMC8360104
core_pubmed_pmc
The Pharmacology, Efficacy, and Safety of Rivaroxaban in Renally Impaired Patient Populations
The Pharmacology, Efficacy, and Safety of Rivaroxaban in Renally Impaired Patient Populations Abstract Abstract Rivaroxaban is a factor Xa inhibitor oral anticoagulant first approved for use in the United States in 2011. Under the drug class commonly termed direct oral anticoagulants, rivaroxaban is approved for the mo...
PMC10096047
core_pubmed_pmc
Targeting Toxoplasma gondii ME49 TgAPN2: A Bioinformatics Approach for Antiparasitic Drug Discovery
Targeting Toxoplasma gondii ME49 TgAPN2: A Bioinformatics Approach for Antiparasitic Drug Discovery Abstract Abstract As fewer therapeutic options are available for treating toxoplasmosis, newer antiparasitic drugs that can block TgAPN2 M1 aminopeptidase are of significant value. Herein, we employed several computer-ai...
PMC9298194
core_pubmed_pmc
Clinical Pharmacokinetics of Daprodustat: Results of an Absorption, Distribution, and Excretion Study With Intravenous Microtracer and Concomitant Oral Doses for Bioavailability Determination
Clinical Pharmacokinetics of Daprodustat: Results of an Absorption, Distribution, and Excretion Study With Intravenous Microtracer and Concomitant Oral Doses for Bioavailability Determination Abstract Abstract Daprodustat, an oral hypoxia‐inducible factor prolyl hydroxylase inhibitor, is being investigated for treatmen...
PMC11578138
core_pubmed_pmc
Informing the risk assessment related to lactation and drug exposure: A physiologically based pharmacokinetic lactation model for pregabalin
Informing the risk assessment related to lactation and drug exposure: A physiologically based pharmacokinetic lactation model for pregabalin Abstract Abstract Breastfeeding is important in childhood development, and medications are often necessary for lactating individuals, yet information on the potential risk of infa...
PMC10056526
core_pubmed_pmc
Quorum Quenchers from Reynoutria japonica in the Battle against Methicillin-Resistant Staphylococcus aureus (MRSA)
Quorum Quenchers from Reynoutria japonica in the Battle against Methicillin-Resistant Staphylococcus aureus (MRSA) Abstract Abstract Over the past decade, methicillin-resistant Staphylococcus aureus (MRSA) has become a major source of biofilm formation and a major contributor to antimicrobial resistance. The genes that...
PMC10786722
core_pubmed_pmc
Integrating rare genetic variants into DPYD pharmacogenetic testing may help preventing fluoropyrimidine-induced toxicity
Integrating rare genetic variants into DPYD pharmacogenetic testing may help preventing fluoropyrimidine-induced toxicity Abstract Variability in genes involved in drug pharmacokinetics or drug response can be responsible for suboptimal treatment efficacy or predispose to adverse drug reactions. In addition to common g...
PMC11179708
core_pubmed_pmc
Physiologically based pharmacokinetics modeling and transporter proteomics to predict systemic and local liver and muscle disposition of statins
Physiologically based pharmacokinetics modeling and transporter proteomics to predict systemic and local liver and muscle disposition of statins Abstract Abstract Statins are used to reduce liver cholesterol levels but also carry a dose‐related risk of skeletal muscle toxicity. Concentrations of statins in plasma are o...
PMC3085714
core_pubmed_pmc
Evaluation of α 2 -Integrin Expression as a Biomarker for Tumor Growth Inhibition for the Investigational Integrin Inhibitor E7820 in Preclinical and Clinical Studies
Evaluation of α 2 -Integrin Expression as a Biomarker for Tumor Growth Inhibition for the Investigational Integrin Inhibitor E7820 in Preclinical and Clinical Studies Abstract E7820 is an orally active inhibitor of α 2 -integrin mRNA expression, currently tested in phases I and II. We aimed to evaluate what levels of i...
PMC4834132
core_pubmed_pmc
Translational Pharmacokinetic‐Pharmacodynamic Modeling and Simulation: Optimizing 5‐Fluorouracil Dosing in Children With Pediatric Ependymoma
Translational Pharmacokinetic‐Pharmacodynamic Modeling and Simulation: Optimizing 5‐Fluorouracil Dosing in Children With Pediatric Ependymoma Abstract We previously investigated novel therapies for pediatric ependymoma and found 5‐fluorouracil (5‐FU) i.v. bolus increased survival in a representative mouse model. Howeve...
PMC5434660
core_pubmed_pmc
Endogenous and xenobiotic metabolic stability of primary human hepatocytes in long-term 3D spheroid cultures revealed by a combination of targeted and untargeted metabolomics
Endogenous and xenobiotic metabolic stability of primary human hepatocytes in long-term 3D spheroid cultures revealed by a combination of targeted and untargeted metabolomics Abstract Abstract Adverse reactions or lack of response to medications are important concerns for drug development programs. However, faithful pr...
PMC5524163
core_pubmed_pmc
Identification of human IgG1 variant with enhanced FcRn binding and without increased binding to rheumatoid factor autoantibody
Identification of human IgG1 variant with enhanced FcRn binding and without increased binding to rheumatoid factor autoantibody Abstract ABSTRACT Various studies have demonstrated that Fc engineering to enhance neonatal Fc receptor (FcRn) binding is effective for elongating half-life or increasing cellular uptake of Ig...
PMC6978998
core_pubmed_pmc
In Vitro Pharmacodynamic Analyses Help Guide the Treatment of Multidrug-Resistant Enterococcus faecium and Carbapenem-Resistant Enterobacter cloacae Bacteremia in a Liver Transplant Patient
In Vitro Pharmacodynamic Analyses Help Guide the Treatment of Multidrug-Resistant Enterococcus faecium and Carbapenem-Resistant Enterobacter cloacae Bacteremia in a Liver Transplant Patient Abstract Abstract Background Infections due to multidrug-resistant pathogens are particularly deadly and difficult to treat in imm...
PMC4898153
core_pubmed_pmc
Pharmacokinetic analysis and comparison of caffeine administered rapidly or slowly in coffee chilled or hot versus chilled energy drink in healthy young adults
Pharmacokinetic analysis and comparison of caffeine administered rapidly or slowly in coffee chilled or hot versus chilled energy drink in healthy young adults Abstract Abstract Context : There is a paucity of data describing the impact of type of beverage (coffee versus energy drink), different rates of consumption an...
PMC9774837
core_pubmed_pmc
β-Lactam Dosing in Critical Patients: A Narrative Review of Optimal Efficacy and the Prevention of Resistance and Toxicity
β-Lactam Dosing in Critical Patients: A Narrative Review of Optimal Efficacy and the Prevention of Resistance and Toxicity Abstract Abstract Antimicrobial prescription in critically ill patients represents a complex challenge due to the difficult balance between infection treatment and toxicity prevention. Underexposur...
PMC9078286
core_pubmed_pmc
Comparative pharmacokinetics of four active components on normal and diabetic rats after oral administration of Gandi capsules †
Comparative pharmacokinetics of four active components on normal and diabetic rats after oral administration of Gandi capsules † Abstract The Gandi capsule, a famous traditional Chinese medicine (TCM), is a hospital preparation that has been widely used in China for decades for the treatment of diabetes. The aim of thi...
PMC9279693
core_pubmed_pmc
Current Use of Asparaginase in Acute Lymphoblastic Leukemia/Lymphoblastic Lymphoma
Current Use of Asparaginase in Acute Lymphoblastic Leukemia/Lymphoblastic Lymphoma Abstract Abstract Pediatric Acute Lymphoblastic Leukemia (ALL) cure rates have improved exponentially over the past five decades with now over 90% of children achieving long-term survival. A direct contributor to this remarkable feat is ...
PMC10827984
core_pubmed_pmc
Comparative pharmacokinetics of free doxorubicin and a liposomal formulation in cats following intravenous administration
Comparative pharmacokinetics of free doxorubicin and a liposomal formulation in cats following intravenous administration Abstract Doxorubicin, a potent chemotherapeutic agent used extensively in cancer treatment, displays complex pharmacokinetic behavior, especially across various formulations. With a rising incidence...
PMC12653452
core_pubmed_pmc
Advances in Cytotoxicity Testing: From In Vitro Assays to In Silico Models
Advances in Cytotoxicity Testing: From In Vitro Assays to In Silico Models Abstract Cytotoxicity testing remains a cornerstone of modern toxicology, providing critical insight into how chemicals and drugs affect cell viability and function. Classical colorimetric assays such as MTT, LDH release, and neutral red uptake ...
PMC5930430
core_pubmed_pmc
Pharmacokinetics of Chinese medicines: strategies and perspectives
Pharmacokinetics of Chinese medicines: strategies and perspectives Abstract The modernization and internationalization of Chinese medicines (CMs) are hampered by increasing concerns on the safety and the efficacy. Pharmacokinetic (PK) study is indispensable to establish concentration-activity/toxicity relationship and ...
PMC6999687
core_pubmed_pmc
Mephedrone and Alcohol Interactions in Humans
Mephedrone and Alcohol Interactions in Humans Abstract Mephedrone (4-MMC, mephedrone) is a synthetic cathinone derivative included in the class of new psychoactive substances. It is commonly used simultaneously with alcohol (ethanol). The aim of the present study was to evaluate the interactions on subjective, cardiova...
PMC8965754
core_pubmed_pmc
The Role of in silico Research in Developing Nanoparticle-Based Therapeutics
The Role of in silico Research in Developing Nanoparticle-Based Therapeutics Abstract Abstract Nanoparticles (NPs) hold great potential as therapeutics, particularly in the realm of drug delivery. They are effective at functional cargo delivery and offer a great degree of amenability that can be used to offset toxic si...
PMC7965838
core_pubmed_pmc
A Mechanistic In Vivo / Ex Vivo Pharmacokinetic‐Pharmacodynamic Model of Tenofovir for HIV Prevention
A Mechanistic In Vivo / Ex Vivo Pharmacokinetic‐Pharmacodynamic Model of Tenofovir for HIV Prevention Abstract Abstract Defining tissue and plasma‐specific prophylactic drug concentrations is central to pre‐exposure prophylaxis product development for sexual transmission of HIV‐1. Pharmacokinetic (PK) data from study R...
PMC11702893
core_pubmed_pmc
Idarubicin-loaded drug-eluting microspheres transarterial chemoembolization for intermediate stage hepatocellular carcinoma: safety, efficacy, and pharmacokinetics
Idarubicin-loaded drug-eluting microspheres transarterial chemoembolization for intermediate stage hepatocellular carcinoma: safety, efficacy, and pharmacokinetics Abstract Abstract Background Transarterial chemoembolization (TACE) is the treatment of choice for the intermediate stage hepatocellular carcinoma (HCC). Do...
PMC5784558
core_pubmed_pmc
Extended-release oral capsule of carbidopa–levodopa in Parkinson disease
Extended-release oral capsule of carbidopa–levodopa in Parkinson disease Abstract Motor fluctuations complicate the treatment of patients with Parkinson’s disease receiving levodopa. Extended-release carbidopa–levodopa has a pharmacokinetic profile that provides a more continuous levodopa serum concentration. Patients ...
PMC9926080
core_pubmed_pmc
Comparison of P‐glycoprotein function in peripheral blood mononuclear cells ex vivo in stable Black and White male and female kidney transplant recipients
Comparison of P‐glycoprotein function in peripheral blood mononuclear cells ex vivo in stable Black and White male and female kidney transplant recipients Abstract Abstract Kidney allograft survival remains poorer in Black compared to White recipients due to racial differences in calcineurin inhibitor (CNI) pharmacolog...
PMC12903041
core_pubmed_pmc
Optimization of Pyrazolo[3,4‑ b ]pyridine Analogues: Synthesis, In Vitro Anticancer Evaluation and In Vivo Pharmacokinetics
Optimization of Pyrazolo[3,4‑ b ]pyridine Analogues: Synthesis, In Vitro Anticancer Evaluation and In Vivo Pharmacokinetics Abstract In this study, we designed and synthesized a series of novel pyrazolo­[3,4- b ]­pyridine analogues, based on a lead compound, previously identified by our group, namely 4-(2-(cyclohexylam...
PMC11568381
core_pubmed_pmc
Candidate-gene studies related to drug pharmacokinetics, pharmacodynamics, safety, and efficacy in the era of extensive technological developments: could we empower them by more efficient implementation of established epidemiological concepts?
Candidate-gene studies related to drug pharmacokinetics, pharmacodynamics, safety, and efficacy in the era of extensive technological developments: could we empower them by more efficient implementation of established epidemiological concepts? Methods Small and large samples, small and large effects, and meta-analysis ...
PMC9514000
core_pubmed_pmc
Unraveling the mystery of efficacy in Chinese medicine formula: New approaches and technologies for research on pharmacodynamic substances
Unraveling the mystery of efficacy in Chinese medicine formula: New approaches and technologies for research on pharmacodynamic substances Abstract Traditional Chinese medicine (TCM) is the key to unlock treasures of Chinese civilization. TCM and its compound play a beneficial role in medical activities to cure disease...
PMC12000929
core_pubmed_pmc
Distribution of Intranasally Administered rIL‐10 Along the Olfactory Nerve and Perivascular Space After Intracerebral Hemorrhage
Distribution of Intranasally Administered rIL‐10 Along the Olfactory Nerve and Perivascular Space After Intracerebral Hemorrhage Abstract ABSTRACT Rationale The utilization of anti‐inflammatory therapy for treating brain diseases holds promise; however, research on intranasal administration of drug compounds remains li...
PMC10719607
core_pubmed_pmc
Efficacy and Safety of Iptacopan in Patients With C3 Glomerulopathy
Efficacy and Safety of Iptacopan in Patients With C3 Glomerulopathy Abstract Abstract Introduction Complement 3 glomerulopathy (C3G) is a rare inflammatory kidney disease mediated by dysregulation of the alternative complement pathway. No targeted therapy exists for this aggressive glomerulonephritis. Efficacy, safety,...
PMC7383037
core_pubmed_pmc
External Validation of Model-Based Dosing Guidelines for Vancomycin, Gentamicin, and Tobramycin in Critically Ill Neonates and Children: A Pragmatic Two-Center Study
External Validation of Model-Based Dosing Guidelines for Vancomycin, Gentamicin, and Tobramycin in Critically Ill Neonates and Children: A Pragmatic Two-Center Study Abstract Background The Dutch Pediatric Formulary (DPF) increasingly bases its guidelines on model-based dosing simulations from pharmacokinetic studies. ...
PMC11855824
core_pubmed_pmc
Molecular Precision Medicine: Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug–Drug Interactions Between Lidocaine and Rocuronium/Propofol/Paracetamol
Molecular Precision Medicine: Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug–Drug Interactions Between Lidocaine and Rocuronium/Propofol/Paracetamol Abstract Abstract The perioperative period, encompassing preoperative, intraoperative, and postoperative phases, is crucial for comprehensiv...
PMC12598126
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Analysis of First‐Line Osimertinib Plus Chemotherapy in Patients with EGFR ‐Mutated Advanced NSCLC
Population Pharmacokinetics and Exposure‐Response Analysis of First‐Line Osimertinib Plus Chemotherapy in Patients with EGFR ‐Mutated Advanced NSCLC Abstract Osimertinib, a third‐generation, central nervous system‐active epidermal growth factor receptor‐tyrosine kinase inhibitor, potently and selectively inhibits epide...
PMC11774993
core_pubmed_pmc
Kinetically-derived maximal dose (KMD) confirms lack of human relevance for high-dose effects of octamethylcyclotetrasiloxane (D4)
Kinetically-derived maximal dose (KMD) confirms lack of human relevance for high-dose effects of octamethylcyclotetrasiloxane (D4) Abstract The kinetically-derived maximal dose (KMD) is defined as the maximum external dose at which kinetics are unchanged relative to lower doses, e.g., doses at which kinetic processes a...
PMC9543479
core_pubmed_pmc
In Silico Modeling for Ex Vivo Placental Transfer of Morphine
In Silico Modeling for Ex Vivo Placental Transfer of Morphine Abstract Abstract Morphine may be administered in pregnant women as an analgesic agent. The transplacental pharmacokinetics (PK) of morphine varies during pregnancy because of physiological and metabolic changes. In this work, we use a multi‐compartment mode...
PMC5529749
core_pubmed_pmc
Pharmacometric Modeling of Liver Metastases' Diameter, Volume, and Density and Their Relation to Clinical Outcome in Imatinib‐Treated Patients With Gastrointestinal Stromal Tumors
Pharmacometric Modeling of Liver Metastases' Diameter, Volume, and Density and Their Relation to Clinical Outcome in Imatinib‐Treated Patients With Gastrointestinal Stromal Tumors Abstract Abstract Three‐dimensional and density‐based tumor metrics have been suggested to better discriminate tumor response to treatment t...
PMC7675190
core_pubmed_pmc
Is it Time for Reviewer 3 to Request Human Organ Chip Experiments Instead of Animal Validation Studies?
Is it Time for Reviewer 3 to Request Human Organ Chip Experiments Instead of Animal Validation Studies? Abstract Abstract For the past century, experimental data obtained from animal studies have been required by reviewers of scientific articles and grant applications to validate the physiological relevance of in vitro...
PMC8852715
core_pubmed_pmc
Iberdomide in patients with systemic lupus erythematosus: a randomised, double-blind, placebo-controlled, ascending-dose, phase 2a study
Iberdomide in patients with systemic lupus erythematosus: a randomised, double-blind, placebo-controlled, ascending-dose, phase 2a study Abstract Objective To evaluate safety, pharmacokinetics, pharmacodynamics and efficacy of iberdomide in patients with SLE. Iberdomide is a high-affinity cereblon ligand that targets t...
PMC12845059
core_pubmed_pmc
The Role of Clinical Pharmacogenetics and Opioid Interactions in Pain Management: Current Evidence and Future Perspectives
The Role of Clinical Pharmacogenetics and Opioid Interactions in Pain Management: Current Evidence and Future Perspectives Abstract Abstract Introduction : Opioids are the most commonly used analgesic drugs for acute and chronic severe pain and are metabolized in the liver via cytochrome P450 (CYP) enzymes and UDP-gluc...
PMC8468663
core_pubmed_pmc
Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats
Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats Abstract Coronavirus disease 2019 (COVID-19), caused by a new strain of coronavirus called severe acute respiratory syndrome coronavirus 2 (SARS-CoV-...
PMC7201957
core_pubmed_pmc
Extended half-life target module for sustainable UniCAR T-cell treatment of STn-expressing cancers
Extended half-life target module for sustainable UniCAR T-cell treatment of STn-expressing cancers Abstract Background Adapter chimeric antigen receptor (CAR) approaches have emerged has promising strategies to increase clinical safety of CAR T-cell therapy. In the UniCAR system, the safety switch is controlled via a t...
PMC3626800
core_pubmed_pmc
Phase I study of OM-174, a lipid A analogue, with assessment of immunological response, in patients with refractory solid tumors
Phase I study of OM-174, a lipid A analogue, with assessment of immunological response, in patients with refractory solid tumors Abstract Background Lipids A, the lipophilic partial structure of lipopolysaccharides, induce regression of several tumor types in animal models. Rather than exerting direct cytotoxic effect,...
PMC10404290
core_pubmed_pmc
CBD-oil as a potential solution in case of severe tamoxifen-related side effects
CBD-oil as a potential solution in case of severe tamoxifen-related side effects Abstract Tamoxifen may lead to bothersome side effects contributing to non-compliance and decreased quality of life. Patients searching for relief are increasingly turning to cannabinoids such as CBD-oil. However, CBD-oil might affect tamo...
PMC7469706
core_pubmed_pmc
Assessment of immunogenicity from galcanezumab phase 3 trials in patients with episodic or chronic migraine
Assessment of immunogenicity from galcanezumab phase 3 trials in patients with episodic or chronic migraine Abstract Background This analysis characterizes the immunogenicity profile of galcanezumab, a humanized monoclonal antibody that selectively binds calcitonin gene-related peptide and inhibits its activity, in pha...
PMC6100046
core_pubmed_pmc
Plasma Pharmacokinetic Determination of Canagliflozin and Its Metabolites in a Type 2 Diabetic Rat Model by UPLC-MS/MS
Plasma Pharmacokinetic Determination of Canagliflozin and Its Metabolites in a Type 2 Diabetic Rat Model by UPLC-MS/MS Abstract Abstract Canagliflozin is a novel, orally selective inhibitor of sodium-dependent glucose co-transporter-2 (SGLT2) for the treatment of patients with type 2 diabetes mellitus. In this study, a...
PMC10962654
core_pubmed_pmc
An auxiliary strategy of partial least squares regression in pharmacokinetic/pharmacodynamic studies: A case of application of guhong injection in myocardial ischemia/reperfusion rats
An auxiliary strategy of partial least squares regression in pharmacokinetic/pharmacodynamic studies: A case of application of guhong injection in myocardial ischemia/reperfusion rats Abstract Guhong injection (GHI) has been applied in the therapy of cardio-cerebrovascular disease in clinic, but there is no report abou...
PMC3334764
core_pubmed_pmc
Effect of fluid loading during hypovolaemic shock on caspofungin pharmacokinetic parameters in pig
Effect of fluid loading during hypovolaemic shock on caspofungin pharmacokinetic parameters in pig Abstract Introduction Caspofungin treatment is frequently initiated in shock patients. In the present study, we investigated the influence of hypovolaemic shock requiring fluid loading on the plasma and pulmonary pharmaco...
PMC12693484
core_pubmed_pmc
Development of Prediction Capabilities for High-Throughput Screening of Physiochemical Properties by Biomimetic Chromatography
Development of Prediction Capabilities for High-Throughput Screening of Physiochemical Properties by Biomimetic Chromatography Abstract Abstract The ever-increasing costs of in vitro and in vivo testing are compelling scientists to increasingly rely on computational models for predictive characterisation at early stage...
PMC5433401
core_pubmed_pmc
Safety, tolerability and pharmacodynamics of a novel immunomodulator, MIS416, in patients with chronic progressive multiple sclerosis
Safety, tolerability and pharmacodynamics of a novel immunomodulator, MIS416, in patients with chronic progressive multiple sclerosis Abstract Background Preclinical studies have demonstrated that MIS416, a bacterially derived immune modulator, targets myeloid cells following systemic delivery. MIS416 stimulated myeloi...
PMC4774502
core_pubmed_pmc
Blockade of P-Glycoprotein Decreased the Disposition of Phenformin and Increased Plasma Lactate Level
Blockade of P-Glycoprotein Decreased the Disposition of Phenformin and Increased Plasma Lactate Level Abstract This study aimed to investigate the in vivo relevance of P-glycoprotein (P-gp) in the pharmacokinetics and adverse effect of phenformin. To investigate the involvement of P-gp in the transport of phenformin, a...
PMC5227308
core_pubmed_pmc
A Novel Microspheres Formulation of Puerarin: Pharmacokinetics Study and In Vivo Pharmacodynamics Evaluations
A Novel Microspheres Formulation of Puerarin: Pharmacokinetics Study and In Vivo Pharmacodynamics Evaluations Abstract Abstract The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of puerarin loaded carboxymethyl chitosan microspheres (Pue-CCMs). The differences in pharmacokinetics parame...
PMC12490336
core_pubmed_pmc
Pharmacokinetics, Safety, and Dialyzability of Gadoquatrane in Patients With Impaired Renal Function
Pharmacokinetics, Safety, and Dialyzability of Gadoquatrane in Patients With Impaired Renal Function Abstract Abstract Objectives: The aims of the study were to evaluate the safety, tolerability and pharmacokinetics of gadoquatrane in men and women with mild to moderate renal impairment and in matching participants wit...
PMC4516859
core_pubmed_pmc
The Distinct Prandial and Basal Pharmacodynamics of IDegAsp Observed in Younger Adults Are Preserved in Elderly Subjects with Type 1 Diabetes
The Distinct Prandial and Basal Pharmacodynamics of IDegAsp Observed in Younger Adults Are Preserved in Elderly Subjects with Type 1 Diabetes Abstract Background Management of diabetes in elderly patients is complicated by the elevated risk of insulin-induced hypoglycaemia. This is the first study to report the pharmac...
PMC12785113
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Modeling of Antibody-Drug Conjugates
Pharmacokinetic and Pharmacodynamic Modeling of Antibody-Drug Conjugates Abstract Simple Summary Antibody-drug conjugates are a growing class of drugs that combine the selectivity of monoclonal antibodies with the potency of chemotherapeutics. They are designed to target potent drugs to tumor cells and, ideally, spare ...
PMC11022021
core_pubmed_pmc
Polymeric Propranolol Nanoparticles for Intraocular Delivery: Formulation, Characterization, and Vitreous Pharmacokinetics
Polymeric Propranolol Nanoparticles for Intraocular Delivery: Formulation, Characterization, and Vitreous Pharmacokinetics Abstract Abstract Purpose Recent studies have reported the promising effect of intravitreal propranolol on retinal neovascularization. However, rapid clearance and short half-life of the drug in th...
PMC6521334
core_pubmed_pmc
Pharmacokinetics and Safety of Icotinib Hydrochloride Cream in Patients with Mild to Moderate Chronic Plaque Psoriasis: A Randomized Double-Blind Vehicle-Controlled Phase 1 Study
Pharmacokinetics and Safety of Icotinib Hydrochloride Cream in Patients with Mild to Moderate Chronic Plaque Psoriasis: A Randomized Double-Blind Vehicle-Controlled Phase 1 Study Abstract Objective This phase I study aimed to systematically assess the safety, local tolerability, pharmacokinetics, and preliminary effica...
PMC10072072
core_pubmed_pmc
Structure-based engineering of a novel CD3ε-targeting antibody for reduced polyreactivity
Structure-based engineering of a novel CD3ε-targeting antibody for reduced polyreactivity Abstract ABSTRACT Bispecific antibodies continue to represent a growth area for antibody therapeutics, with roughly a third of molecules in clinical development being T-cell engagers that use an anti-CD3 binding arm. CD3 antibodie...
PMC5769330
core_pubmed_pmc
Flaxseed-enriched diets change milk concentration of the antimicrobial danofloxacin in sheep
Flaxseed-enriched diets change milk concentration of the antimicrobial danofloxacin in sheep Abstract Background Flaxseed is the most common and rich dietary source of lignans and is an acceptable supply of energy for livestock. Flaxseed lignans are precursors of enterolignans, mainly enterolactone and enterodiol, prod...
PMC9160491
core_pubmed_pmc
Preparation, characterization, and pharmacokinetics of rivaroxaban cocrystals with enhanced in vitro and in vivo properties in beagle dogs
Preparation, characterization, and pharmacokinetics of rivaroxaban cocrystals with enhanced in vitro and in vivo properties in beagle dogs Abstract Rivaroxaban (RIV) is a direct Factor Xa inhibitor anticoagulant, but the oral bioavailability of RIV is estimated to be only 60% due to its poor solubility. The aim of the ...
PMC10853469
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics and safety of 15 mg-tolvaptan administered orally for 7 consecutive days to Chinese patients with child-Pugh B cirrhosis
Pharmacokinetics, pharmacodynamics and safety of 15 mg-tolvaptan administered orally for 7 consecutive days to Chinese patients with child-Pugh B cirrhosis Abstract Background: Tolvaptan, a selective vasopressin V 2 -receptor antagonist, can elicit a diuretic effect without significant electrolyte loss. The aims were t...
PMC9055162
core_pubmed_pmc
Engineering a protease-based and site-specific PEGylation-based strategy for the controlled release of exenatide
Engineering a protease-based and site-specific PEGylation-based strategy for the controlled release of exenatide Abstract Abstract Using the commercially available antidiabetic drug exenatide (exendin-4) as a model peptide, we designed a novel exenatide derivative, termed LEX-1, comprising a 12-mer albumin-binding pept...
PMC12210098
core_pubmed_pmc
Less frequent dosing of GLP‐1 receptor agonists as a viable weight maintenance strategy
Less frequent dosing of GLP‐1 receptor agonists as a viable weight maintenance strategy Abstract Abstract Objective Incretin mimetics are revolutionizing obesity treatment, but high prices and supply shortages limit patient access. Some clinicians have suggested less frequent dosing as an off‐ramping strategy to mainta...
PMC11766674
core_pubmed_pmc
Exploring the Pharmacological Potential of Carrageenan Disaccharides as Antitumor Agents: An In Silico Approach
Exploring the Pharmacological Potential of Carrageenan Disaccharides as Antitumor Agents: An In Silico Approach Abstract Abstract Carrageenans have demonstrated enhanced antitumor activity upon depolymerization into disaccharides. However, the pharmacological viability of these disaccharides and their mechanisms of ant...
PMC8685623
core_pubmed_pmc
Pharmacokinetics and safety/tolerability of isoniazid, rifampicin and pyrazinamide in children and adolescents treated for tuberculous meningitis
Pharmacokinetics and safety/tolerability of isoniazid, rifampicin and pyrazinamide in children and adolescents treated for tuberculous meningitis Abstract Abstract Objective To assess the pharmacokinetics and safety/tolerability of isoniazid, rifampicin and pyrazinamide in children and adolescents with tuberculous meni...
PMC12408011
core_pubmed_pmc
[ 11 C]Fentanyl: Radiosynthesis and Preclinical PET Imaging for Its Pharmacokinetics
[ 11 C]Fentanyl: Radiosynthesis and Preclinical PET Imaging for Its Pharmacokinetics Abstract Background Fentanyl is a potent synthetic opioid widely used for pain management and anesthesia, but the high prevalence of its misuse and its key contribution to overdose fatalities in the United States have made it a major d...
PMC11418297
core_pubmed_pmc
Enhancing Anesthesia Education and Clinical Practice: A Comprehensive Review of GASMAN Simulation Software
Enhancing Anesthesia Education and Clinical Practice: A Comprehensive Review of GASMAN Simulation Software Abstract Abstract GASMAN software, a simulation tool for inhalational anesthetics’ pharmacokinetics and pharmacodynamics, has become essential in both anesthesia education and clinical practice. This review explor...
PMC8207885
core_pubmed_pmc
The Role of Opioids in Pain Management in Elderly Patients with Chronic Kidney Disease: A Review Article
The Role of Opioids in Pain Management in Elderly Patients with Chronic Kidney Disease: A Review Article Abstract Chronic kidney disease (CKD) is a global public health problem. Pain is one of the most generally experienced symptoms by CKD patients. Pain management is a key clinical activity; nonetheless, insufficient ...
PMC11990156
core_pubmed_pmc
Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective
Spontaneous Reaction of Oleacein and Oleocanthal with Primary Amines: A Biochemical Perspective Abstract Abstract Oleacein (Olea) and Oleocanthal (Oleo) are two phenolic compounds found in olive oil. Cell and animal studies have shown these two compounds can modulate inflammation, cancer, and neurodegenerative diseases...
PMC7993318
core_pubmed_pmc
Optimizing the Therapeutic Window of Targeted Drugs in Oncology: Potency‐Guided First‐in‐Human Studies
Optimizing the Therapeutic Window of Targeted Drugs in Oncology: Potency‐Guided First‐in‐Human Studies Abstract Abstract Many targeted therapies are administered at or near the maximum tolerated dose (MTD). With the advent of precision medicine, a larger therapeutic window is expected. Therefore, dose optimization will...
PMC9763164
core_pubmed_pmc
Pharmacokinetics and tolerability of intranasal or intravenous administration of nalbuphine in infants
Pharmacokinetics and tolerability of intranasal or intravenous administration of nalbuphine in infants Abstract Objectives Intranasal nalbuphine could be a safe, efficacious and non-invasive alternative to parenteral pain medication in infants. We aimed to assess pharmacokinetics (PK) and tolerability of intranasal and...
PMC12460385
core_pubmed_pmc
Sex and gender differences in cancer pathogenesis and pharmacology
Sex and gender differences in cancer pathogenesis and pharmacology Abstract Sex and gender may influence the epidemiology, pathogenesis, and prognosis of cancer. This narrative review describes sex and gender differences in the epidemiology and pathogenesis of cancer, and how such differences may impact the pharmacodyn...
PMC12938352
core_pubmed_pmc
Natural Products as Potentiators of β-Lactam Antibiotics: A Review of Mechanisms, Advances, and Future Directions
Natural Products as Potentiators of β-Lactam Antibiotics: A Review of Mechanisms, Advances, and Future Directions Abstract This review focuses on the research progress on natural products as β-lactam antibiotic adjuvants, aiming to address the escalating challenge of antibiotic resistance, particularly the inactivation...
PMC11652809
core_pubmed_pmc
Pharmacokinetic, Safety, and Pharmacodynamic Profiles of Saroglitazar Magnesium in Cholestatic Cirrhosis With Hepatic Impairment and Participants With Renal Impairment
Pharmacokinetic, Safety, and Pharmacodynamic Profiles of Saroglitazar Magnesium in Cholestatic Cirrhosis With Hepatic Impairment and Participants With Renal Impairment Abstract Abstract Saroglitazar magnesium, a dual PPAR α/γ agonist, currently in Phase III for treating primary biliary cholangitis (PBC), was evaluated ...
PMC12079988
core_pubmed_pmc
A study on the pharmacokinetic bioequivalence of oral tablet formulations of riluzole among healthy volunteers utilizing HPLC-MS/MS
A study on the pharmacokinetic bioequivalence of oral tablet formulations of riluzole among healthy volunteers utilizing HPLC-MS/MS Abstract Abstract Introduction This randomized, open-label, two period, two treatment, fasting bioequivalence trial was conducted to demonstrate the bioequivalence between riluzole tablets...
PMC9769544
core_pubmed_pmc
In Vitro Susceptibilities of Worldwide Isolates of Intrapulmonary Aspergillus Species and Important Candida Species in Sterile Body Sites against Important Antifungals: Data from the Antimicrobial Testing Leadership and Surveillance Program, 2017–2020
In Vitro Susceptibilities of Worldwide Isolates of Intrapulmonary Aspergillus Species and Important Candida Species in Sterile Body Sites against Important Antifungals: Data from the Antimicrobial Testing Leadership and Surveillance Program, 2017–2020 Abstract ABSTRACT To understand the changes of resistance in clinica...
PMC6376854
core_pubmed_pmc
Variability and exposure–response relationships of isavuconazole plasma concentrations in the Phase 3 SECURE trial of patients with invasive mould diseases
Variability and exposure–response relationships of isavuconazole plasma concentrations in the Phase 3 SECURE trial of patients with invasive mould diseases Abstract Abstract Objectives This analysis evaluated the variability of isavuconazole plasma concentrations between subjects and between sampling times, and assesse...
PMC9695346
core_pubmed_pmc
Personalized Medicine for Classical Anesthesia Drugs and Cancer Progression
Personalized Medicine for Classical Anesthesia Drugs and Cancer Progression Abstract Abstract In this review, we aim to discuss the use and effect of five different drugs used in the induction of anesthesia in cancer patients. Propofol, fentanyl, rocuronium, sugammadex, and dexamethasone are commonly used to induce ane...
PMC6781558
core_pubmed_pmc
Skin-on-a-Chip Device for Ex Vivo Monitoring of Transdermal Delivery of Drugs—Design, Fabrication, and Testing
Skin-on-a-Chip Device for Ex Vivo Monitoring of Transdermal Delivery of Drugs—Design, Fabrication, and Testing Abstract To develop proper drug formulations and to optimize the delivery of their active ingredients through the dermal barrier, the Franz diffusion cell system is the most widely used in vitro/ex vivo techni...
PMC11672403
core_pubmed_pmc
Artificial Intelligence and Machine Learning Applications to Pharmacokinetic Modeling and Dose Prediction of Antibiotics: A Scoping Review
Artificial Intelligence and Machine Learning Applications to Pharmacokinetic Modeling and Dose Prediction of Antibiotics: A Scoping Review Abstract Abstract Background and Objectives: The use of artificial intelligence (AI) and, in particular, machine learning (ML) techniques is growing rapidly in the healthcare field....
PMC3857035
core_pubmed_pmc
The Pharmacokinetics and Pharmacodynamics of Iron Preparations
The Pharmacokinetics and Pharmacodynamics of Iron Preparations Abstract Standard approaches are not appropriate when assessing pharmacokinetics of iron supplements due to the ubiquity of endogenous iron, its compartmentalized sites of action, and the complexity of the iron metabolism. The primary site of action of iron...
PMC12622822
core_pubmed_pmc
Computational identification of novel SIRT4 inhibitors for diabetic nephropathy using pharmacophore modeling, molecular simulations, and DFT calculations
Computational identification of novel SIRT4 inhibitors for diabetic nephropathy using pharmacophore modeling, molecular simulations, and DFT calculations Abstract Sirtuin 4 (SIRT4) plays a critical role in regulating oxidative stress, apoptosis, and mitochondrial dysfunction in diabetic nephropathy (DN). This study emp...
PMC12915415
core_pubmed_pmc
Pharmacokinetic Changes of Ceftazidime–Avibactam with Veno-Arterial Extracorporeal Membrane Oxygenation in a Critically Ill Patient with Severe Renal Impairment: A Case Report
Pharmacokinetic Changes of Ceftazidime–Avibactam with Veno-Arterial Extracorporeal Membrane Oxygenation in a Critically Ill Patient with Severe Renal Impairment: A Case Report Abstract Abstract Veno-arterial extracorporeal membrane oxygenation (VA-ECMO) is an advanced life support therapy, but evidence regarding its im...
PMC9419547
core_pubmed_pmc
Reshaped as polyester-based nanoparticles, gallic acid inhibits platelet aggregation, reactive oxygen species production and multi-resistant Gram-positive bacteria with an efficiency never obtained †
Reshaped as polyester-based nanoparticles, gallic acid inhibits platelet aggregation, reactive oxygen species production and multi-resistant Gram-positive bacteria with an efficiency never obtained † Abstract Abstract Natural polyphenols such as Gallic Acid (GA) form an important class of bioactive chemical entities th...
PMC8541017
core_pubmed_pmc
Potent and Selective Inhibitors of Human Monoamine Oxidase A from an Endogenous Lichen Fungus Diaporthe mahothocarpus
Potent and Selective Inhibitors of Human Monoamine Oxidase A from an Endogenous Lichen Fungus Diaporthe mahothocarpus Abstract Abstract Using 126 endogenous lichen fungus (ELF) extracts, inhibitory activities against monoamine oxidases (MAOs) and cholinesterases (ChEs) were evaluated. Among them, extract ELF29 of the e...
PMC10493385
core_pubmed_pmc
Pharmacokinetics of mebendazole in plasma and cerebrospinal fluid following a single oral dose in healthy dogs
Pharmacokinetics of mebendazole in plasma and cerebrospinal fluid following a single oral dose in healthy dogs Abstract Abstract Novel therapies are needed for treatment of gliomas. Mebendazole previously demonstrated anti-neoplastic effects on canine glioma cell lines at in vitro mean inhibitory concentrations (IC 50 ...
PMC12472219
core_pubmed_pmc
Optimization of (Dithioperoxo)thiolate-Based Antifungal Agents for Triazole-Resistant Aspergillus Fumigatus
Optimization of (Dithioperoxo)thiolate-Based Antifungal Agents for Triazole-Resistant Aspergillus Fumigatus Abstract Abstract This investigation on novel antifungal agents featuring a thiol-reactive (dithioperoxo)thiolate chemical nucleus [-NC(S)S-SR] established that the optimal levels of fungal growth inhibition were...
PMC10934217
core_pubmed_pmc
Rat Pharmacokinetics and In Vitro Metabolite Identification of KM-819, a Parkinson’s Disease Candidate, Using LC-MS/MS and LC-HRMS
Rat Pharmacokinetics and In Vitro Metabolite Identification of KM-819, a Parkinson’s Disease Candidate, Using LC-MS/MS and LC-HRMS Abstract FAF1 (FAS-associated factor 1) is involved in the activation of Fas cell surface death receptors and plays a role in apoptosis and necrosis. In patients with Parkinson’s disease, F...
PMC8210330
core_pubmed_pmc
Could simulation methods solve the curse of sparse data within clinical studies of antibiotic resistance?
Could simulation methods solve the curse of sparse data within clinical studies of antibiotic resistance? Abstract Abstract Infectious disease (ID) physicians and ID pharmacists commonly confront therapeutic questions relating to antibiotic resistance. Randomized controlled trial data are few and meta-analytic-based ap...
PMC7342477
core_pubmed_pmc
Engineering Thermo-pH Dual Responsive Hydrogel for Enhanced Tumor Accumulation, Penetration, and Chemo-Protein Combination Therapy
Engineering Thermo-pH Dual Responsive Hydrogel for Enhanced Tumor Accumulation, Penetration, and Chemo-Protein Combination Therapy Abstract Abstract Purpose Combined chemotherapeutic drug and protein drug has been a widely employed strategy for tumor treatment. To realize both tumor accumulation and deep tumor penetrat...
PMC5629135
core_pubmed_pmc
Impact of Genetic Polymorphisms on Phenytoin Pharmacokinetics and Clinical Outcomes in the Middle East and North Africa Region
Impact of Genetic Polymorphisms on Phenytoin Pharmacokinetics and Clinical Outcomes in the Middle East and North Africa Region Abstract Background Genetic polymorphisms are known to influence outcomes with phenytoin yet effects in the Middle East and North Africa region are poorly understood. Objectives The objective o...
PMC9929823
core_pubmed_pmc
Biosynthesis and pharmacokinetics of Panax notoginseng enteric-coated soft capsules
Biosynthesis and pharmacokinetics of Panax notoginseng enteric-coated soft capsules Abstract Background To investigate the biosynthesis and pharmacokinetic course of enteric-coated soft capsules of Panax notoginseng saponins (PNS) in a beagle dog model. Methods To satisfy the enteric properties of soft capsules, the PN...
PMC8314475
core_pubmed_pmc
Pharmacokinetics and safety of liposomal bupivacaine after local infiltration in healthy Chinese adults: a phase 1 study
Pharmacokinetics and safety of liposomal bupivacaine after local infiltration in healthy Chinese adults: a phase 1 study Abstract Abstract Background Liposomal bupivacaine (LB) is a long-acting formulation of bupivacaine. The safety and efficacy of LB has been demonstrated across surgical procedures. However, pharmacok...
PMC5432259
core_pubmed_pmc
Selenomethionine and methyl selenocysteine: multiple-dose pharmacokinetics in selenium-replete men
Selenomethionine and methyl selenocysteine: multiple-dose pharmacokinetics in selenium-replete men Abstract According to the Nutritional Prevention of Cancer (NPC) trial, a selenized yeast supplement containing selenium, 200 mcg/day, decreased the incidence of total cancer, cancers of the prostate, colon and lung, and ...
PMC11136738
core_pubmed_pmc
Maximum a posteriori Bayesian methods out-perform non-compartmental analysis for busulfan precision dosing
Maximum a posteriori Bayesian methods out-perform non-compartmental analysis for busulfan precision dosing Abstract Dose personalization improves patient outcomes for many drugs with a narrow therapeutic index and high inter-individuality variability, including busulfan. Non-compartmental analysis (NCA) and model-based...
PMC9550080
core_pubmed_pmc
Randomized, placebo controlled phase I trial of the safety, pharmacokinetics, pharmacodynamics and acceptability of a 90 day tenofovir plus levonorgestrel vaginal ring used continuously or cyclically in women: The CONRAD 138 study
Randomized, placebo controlled phase I trial of the safety, pharmacokinetics, pharmacodynamics and acceptability of a 90 day tenofovir plus levonorgestrel vaginal ring used continuously or cyclically in women: The CONRAD 138 study Abstract Abstract Multipurpose prevention technologies (MPTs), which prevent sexually tra...
PMC9556337
core_pubmed_pmc
A Population Pharmacokinetic Modelling Approach to Unravel the Complex Pharmacokinetics of Vincristine in Children
A Population Pharmacokinetic Modelling Approach to Unravel the Complex Pharmacokinetics of Vincristine in Children Abstract Abstract Background Vincristine, a chemotherapeutic agent that extensively binds to β-tubulin, is commonly dosed at 1.4–2.0 mg/m 2 capped at 2 mg. For infants, doses vary from 0.025–0.05 mg/kg or ...
PMC4065376
core_pubmed_pmc
Effects of WIN 55,212-2 (a non-selective cannabinoid CB 1 and CB 2 receptor agonist) on the protective action of various classical antiepileptic drugs in the mouse 6 Hz psychomotor seizure model
Effects of WIN 55,212-2 (a non-selective cannabinoid CB 1 and CB 2 receptor agonist) on the protective action of various classical antiepileptic drugs in the mouse 6 Hz psychomotor seizure model Abstract Abstract The aim of this study was to characterize the influence of WIN 55,212-2 (WIN—a non-selective cannabinoid CB...
PMC9798869
core_pubmed_pmc
Integration of In Vitro and In Vivo Models to Predict Cellular and Tissue Dosimetry of Nanomaterials Using Physiologically Based Pharmacokinetic Modeling
Integration of In Vitro and In Vivo Models to Predict Cellular and Tissue Dosimetry of Nanomaterials Using Physiologically Based Pharmacokinetic Modeling Abstract Nanomaterials (NMs) have been increasingly used in a number of areas, including consumer products and nanomedicine. Target tissue dosimetry is important in t...