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PMC12945960
core_pubmed_pmc
In Silico Clinical Trials in Drug Development: A Systematic Review
In Silico Clinical Trials in Drug Development: A Systematic Review Abstract In the context of clinical research, computational models have received increasing attention over the past decades. In this systematic review, we aimed to provide an overview of the role of so-called in silico clinical trials (ISCTs) in medical...
PMC4888741
core_pubmed_pmc
Modeling the oxygen uptake kinetics during exercise testing of patients with chronic obstructive pulmonary diseases using nonlinear mixed models
Modeling the oxygen uptake kinetics during exercise testing of patients with chronic obstructive pulmonary diseases using nonlinear mixed models Abstract Background The six-minute walk test (6MWT) is commonly used to quantify exercise capacity in patients with several cardio-pulmonary diseases. Oxygen uptake ( \documen...
PMC9570604
core_pubmed_pmc
Efficacy and Mechanism of Pueraria lobata and Pueraria thomsonii Polysaccharides in the Treatment of Type 2 Diabetes
Efficacy and Mechanism of Pueraria lobata and Pueraria thomsonii Polysaccharides in the Treatment of Type 2 Diabetes Abstract Diabetes is called a “wasting and thirsting disorder” in Chinese traditional medicine because there is a depletion of vital substances in the body independent of the intake of food or water and ...
PMC7481523
core_pubmed_pmc
Onset times and duration of analgesic effect of various concentrations of local anesthetic solutions in standardized volume used for brachial plexus blocks
Onset times and duration of analgesic effect of various concentrations of local anesthetic solutions in standardized volume used for brachial plexus blocks Abstract Visualization of the nerve structures of brachial plexus allows anesthesiologists to use a lower dose of local anesthetics. The content of this low dose is...
PMC12226948
core_pubmed_pmc
AEROfen: protocol for a phase I, open-label, randomised crossover study evaluating the efficiency of nebulised fentanyl in healthy volunteers – comparing facial versus intranasal administration via pharmacometric modelling
AEROfen: protocol for a phase I, open-label, randomised crossover study evaluating the efficiency of nebulised fentanyl in healthy volunteers – comparing facial versus intranasal administration via pharmacometric modelling Abstract Abstract Introduction Pain accounts for approximately 80% of emergency department admiss...
PMC10694947
core_pubmed_pmc
Induction of CYP3A activity by dexamethasone may not be strong, even at high doses: insights from a case of tacrolimus co-administration
Induction of CYP3A activity by dexamethasone may not be strong, even at high doses: insights from a case of tacrolimus co-administration Abstract Background Dexamethasone (DEX) induces CYP3A activity in a concentration-dependent manner. However, no study has examined changes in the blood concentration of CYP3A substrat...
PMC3475973
core_pubmed_pmc
The toxicokinetics cell demography model to explain metal kinetics in terrestrial invertebrates
The toxicokinetics cell demography model to explain metal kinetics in terrestrial invertebrates Abstract Metal toxicokinetics in invertebrates are usually described by one-compartment first-order kinetic model. Although the model gives an adequate description of the toxicokinetics in certain cases, it has been shown to...
PMC7242238
core_pubmed_pmc
Clinical Drug-Drug Interaction Studies to Evaluate the Effects of a P-Glycoprotein Inhibitor, CYP3A Inhibitors, and a CYP3A Inducer on the Pharmacokinetics of Naldemedine in Healthy Subjects
Clinical Drug-Drug Interaction Studies to Evaluate the Effects of a P-Glycoprotein Inhibitor, CYP3A Inhibitors, and a CYP3A Inducer on the Pharmacokinetics of Naldemedine in Healthy Subjects Abstract Background Naldemedine is a peripherally acting μ-opioid receptor antagonist that is indicated to treat opioid-induced c...
PMC12930009
core_pubmed_pmc
Safety and pharmacokinetics of a novel potent GABA analogue crisugabalin in Chinese subjects with various degrees of renal impairment
Safety and pharmacokinetics of a novel potent GABA analogue crisugabalin in Chinese subjects with various degrees of renal impairment Abstract Abstract Aims Crisugabalin is a novel calcium channel α2δ subunit ligand and a highly selective oral gamma‐aminobutyric acid (GABA) analogue developed for the treatment of diabe...
PMC6332076
core_pubmed_pmc
Plasma Pharmacokinetics of Polyphenols in a Traditional Japanese Medicine, Jumihaidokuto, Which Suppresses Propionibacterium acnes -Induced Dermatitis in Rats
Plasma Pharmacokinetics of Polyphenols in a Traditional Japanese Medicine, Jumihaidokuto, Which Suppresses Propionibacterium acnes -Induced Dermatitis in Rats Abstract Abstract Most orally administered polyphenols are metabolized, with very little absorbed as aglycones and/or unchanged forms. Metabolic and pharmacokine...
PMC8977638
core_pubmed_pmc
Development and Validation of a Novel Tool for the Prediction of Clopidogrel Response in Chinese Acute Coronary Syndrome Patients: The GeneFA Score
Development and Validation of a Novel Tool for the Prediction of Clopidogrel Response in Chinese Acute Coronary Syndrome Patients: The GeneFA Score Abstract Abstract Aim: Growing evidence indicated that CYP2C19 genotypes could only explain a fraction of the pharmacodynamic response to clopidogrel, while a number of cli...
PMC12060349
core_pubmed_pmc
Effect of CYP3A4 inhibitor and induction on the pharmacokinetics and safety of FHND9041, a novel EGFR T790M inhibitor, in healthy Chinese
Effect of CYP3A4 inhibitor and induction on the pharmacokinetics and safety of FHND9041, a novel EGFR T790M inhibitor, in healthy Chinese Abstract Abstract Background Non-small cell carcinoma is the main pathologic type of lung cancer, and a large number of clinical trials have shown that epidermal growth factor recept...
PMC11532771
core_pubmed_pmc
Exploration of drug therapy related problems in a general medicine ward of a tertiary care hospital of Eastern Nepal
Exploration of drug therapy related problems in a general medicine ward of a tertiary care hospital of Eastern Nepal Abstract Abstract Background Inpatients are at higher risk of Drug Therapy Related Problems (DTRPs), and early identification and management of these DTRPs is crucial for optimal treatment outcomes and e...
PMC4999606
core_pubmed_pmc
New generalized poisson mixture model for bimodal count data with drug effect: An application to rodent brief‐access taste aversion experiments
New generalized poisson mixture model for bimodal count data with drug effect: An application to rodent brief‐access taste aversion experiments Abstract Pharmacodynamic (PD) count data can exhibit bimodality and nonequidispersion complicating the inclusion of drug effect. The purpose of this study was to explore four d...
PMC7230366
core_pubmed_pmc
Linezolid Concentrations in Plasma and Subcutaneous Tissue are Reduced in Obese Patients, Resulting in a Higher Risk of Underdosing in Critically Ill Patients: A Controlled Clinical Pharmacokinetic Study
Linezolid Concentrations in Plasma and Subcutaneous Tissue are Reduced in Obese Patients, Resulting in a Higher Risk of Underdosing in Critically Ill Patients: A Controlled Clinical Pharmacokinetic Study Abstract Abstract Background: Linezolid is used for the treatment of soft tissue infections in critically ill patien...
PMC6585617
core_pubmed_pmc
Model‐Informed Drug Development for Ixazomib, an Oral Proteasome Inhibitor
Model‐Informed Drug Development for Ixazomib, an Oral Proteasome Inhibitor Abstract Model‐informed drug development (MIDD) was central to the development of the oral proteasome inhibitor ixazomib, facilitating internal decisions (switch from body surface area (BSA)‐based to fixed dosing, inclusive phase III trials, por...
PMC12421129
core_pubmed_pmc
Phase 1, randomized trials of MEDI1341: cerebrospinal fluid free α-synuclein lowered by >50%
Phase 1, randomized trials of MEDI1341: cerebrospinal fluid free α-synuclein lowered by >50% Abstract Abstract Accumulation of pathological forms of α-synuclein is a hallmark of Parkinson’s disease. MEDI1341 (also known as TAK-341) is a high-affinity, α-synuclein-specific, fully human monoclonal antibody that binds the...
PMC7170552
core_pubmed_pmc
Study protocol for SFX-01 after subarachnoid haemorrhage (SAS): a multicentre randomised double-blinded, placebo controlled trial
Study protocol for SFX-01 after subarachnoid haemorrhage (SAS): a multicentre randomised double-blinded, placebo controlled trial Abstract Introduction Subarachnoid haemorrhage (SAH) from a ruptured cerebral aneurysm carries high morbidity and mortality. Despite huge advances in techniques to secure the aneurysm, there...
PMC6537040
core_pubmed_pmc
Population pharmacokinetic analysis of tramadol and O- desmethyltramadol with genetic polymorphism of CYP2D6
Population pharmacokinetic analysis of tramadol and O- desmethyltramadol with genetic polymorphism of CYP2D6 Abstract Aim: Tramadol is widely used to treat acute, chronic, and neuropathic pain. Its primary active metabolite, O- desmethyltramadol (M1), is mainly responsible for its µ-opioid receptor-related analgesic ef...
PMC9643156
core_pubmed_pmc
A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer
A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer Abstract Enzalutamide (ENZ) is a second-generation androgen receptor (AR) antagonist used for the treatment of castration-resistant prostate cancer (CRPC) and reportedly prolongs survival time ...
PMC10761660
core_pubmed_pmc
Preclinical evaluation of an 18 F-labeled N ε -acryloyllysine piperazide for covalent targeting of transglutaminase 2
Preclinical evaluation of an 18 F-labeled N ε -acryloyllysine piperazide for covalent targeting of transglutaminase 2 Abstract Abstract Background Transglutaminase 2 (TGase 2) is a multifunctional protein and has a prominent role in various (patho)physiological processes. In particular, its transamidase activity, which...
PMC5532402
core_pubmed_pmc
Eribulin shows high concentration and long retention in xenograft tumor tissues
Eribulin shows high concentration and long retention in xenograft tumor tissues Abstract Purpose Eribulin, a synthetic analog of the natural product halichondrin B, is a microtubule dynamics inhibitor. In this study, we report the pharmacokinetic profiles of eribulin in mice, rats, and dogs following intravenous admini...
PMC8401956
core_pubmed_pmc
A Repeated Time-to-Positive Symptoms Improvement among Malaysian Patients with Schizophrenia Spectrum Disorders Treated with Clozapine
A Repeated Time-to-Positive Symptoms Improvement among Malaysian Patients with Schizophrenia Spectrum Disorders Treated with Clozapine Abstract Clozapine remains the drug of choice for resistant schizophrenia. However, its dose-response relationship is still controversial. The current investigation aimed to develop a r...
PMC8846633
core_pubmed_pmc
Physiologically‐based pharmacokinetic modeling of oxcarbazepine and levetiracetam during adjunctive antiepileptic therapy in children and adolescents
Physiologically‐based pharmacokinetic modeling of oxcarbazepine and levetiracetam during adjunctive antiepileptic therapy in children and adolescents Abstract Abstract Oxcarbazepine (OXZ) and levetiracetam (LEV) are two new generation anti‐epileptic drugs, often co‐administered in children with enzyme‐inducing antiepil...
PMC5114201
core_pubmed_pmc
A Single Dose-Escalation Study to Evaluate the Safety and Pharmacokinetics of Orally Administered Des-Aspartate Angiotensin I in Healthy Subjects
A Single Dose-Escalation Study to Evaluate the Safety and Pharmacokinetics of Orally Administered Des-Aspartate Angiotensin I in Healthy Subjects Abstract Abstract Des-aspartate-angiotensin I (DAA-I) is an endogenous angiotensin peptide and a prototype angiotensin receptor agonist (ARA). It acts on the angiotensin AT 1...
PMC7438815
core_pubmed_pmc
Application of Physiologically‐Based Pharmacokinetic Modeling to Predict Gastric pH‐Dependent Drug–Drug Interactions for Weak Base Drugs
Application of Physiologically‐Based Pharmacokinetic Modeling to Predict Gastric pH‐Dependent Drug–Drug Interactions for Weak Base Drugs Abstract Weak‐base drugs are susceptible to drug–drug interactions (DDIs) when coadministered with gastric acid–reducing agents (ARAs). We developed PBPK models to evaluate the potent...
PMC11368863
core_pubmed_pmc
C286, an orally available retinoic acid receptor β agonist drug, regulates multiple pathways to achieve spinal cord injury repair
C286, an orally available retinoic acid receptor β agonist drug, regulates multiple pathways to achieve spinal cord injury repair Abstract Abstract Retinoic acid receptor β2 (RARβ2) is an emerging therapeutic target for spinal cord injuries (SCIs) with a unique multimodal regenerative effect. We have developed a first-...
PMC12359132
core_pubmed_pmc
First-in-human study of the benzothiazinone and DprE1 inhibitor BTZ-043, a novel drug candidate for the treatment of Tuberculosis
First-in-human study of the benzothiazinone and DprE1 inhibitor BTZ-043, a novel drug candidate for the treatment of Tuberculosis Abstract Abstract Objectives This first-in-human, single ascending dose study evaluated the safety, tolerability and pharmacokinetics (PK) of the decaprenylphosphoryl-β- D- ribose-2′-epimera...
PMC11377956
core_pubmed_pmc
Preparation, pharmacokinetics and anti‐obesity effects on dogs of nuciferine liposomes
Preparation, pharmacokinetics and anti‐obesity effects on dogs of nuciferine liposomes Abstract Abstract Background Nuciferine (NUC), a natural compound extracted from lotus leaves, has been proven to have anti‐obesity effects. However, the development and application of NUC as an anti‐obesity drug in dogs are hindered...
PMC12309136
core_pubmed_pmc
Association of vancomycin trough levels, AUC and AUC/MIC ratios with clinical outcomes in patients with enterococcal bacteremia: a prospective cohort study
Association of vancomycin trough levels, AUC and AUC/MIC ratios with clinical outcomes in patients with enterococcal bacteremia: a prospective cohort study Abstract Abstract Background The optimal vancomycin pharmacokinetic/pharmacodynamic (PK/PD) targets for successful treatment of enterococcal infections remain contr...
PMC4312668
core_pubmed_pmc
Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs)
Eliminating the Heart from the Curcumin Molecule: Monocarbonyl Curcumin Mimics (MACs) Abstract Abstract Curcumin is a natural product with several thousand years of heritage. Its traditional Asian application to human ailments has been subjected in recent decades to worldwide pharmacological, biochemical and clinical i...
PMC3781304
core_pubmed_pmc
Drug-Drug Interaction Studies of Cardiovascular Drugs Involving P-Glycoprotein, an Efflux Transporter, on the Pharmacokinetics of Edoxaban, an Oral Factor Xa Inhibitor
Drug-Drug Interaction Studies of Cardiovascular Drugs Involving P-Glycoprotein, an Efflux Transporter, on the Pharmacokinetics of Edoxaban, an Oral Factor Xa Inhibitor Abstract Abstract Background Edoxaban, an oral direct factor Xa inhibitor, is in development for thromboprophylaxis, including prevention of stroke and ...
PMC7721468
core_pubmed_pmc
Evaluation of sodium valproate low dose efficacy in radicular pain management and it’s relation with pharmacokinetics parameters
Evaluation of sodium valproate low dose efficacy in radicular pain management and it’s relation with pharmacokinetics parameters Abstract Background Radiculopathy due to lumbar or cervical disc disease is the most common chronic neuropathic pain in adults. The aim of present study was evaluation of low dose of sodium v...
PMC7533161
core_pubmed_pmc
Bioequivalence of the pharmacokinetics between tofacitinib aspartate and tofacitinib citrate in healthy subjects
Bioequivalence of the pharmacokinetics between tofacitinib aspartate and tofacitinib citrate in healthy subjects Abstract Abstract Tofacitinib is an oral disease-modifying anti-rheumatic drug to selectively inhibit Janus kinases. Tofacitinib is a representative small molecule inhibitor that is used to treat many diseas...
PMC10496058
core_pubmed_pmc
Pharmacokinetics, safety, and tolerability of single and multiple doses of zuranolone in Japanese and White healthy subjects: A phase 1 clinical trial
Pharmacokinetics, safety, and tolerability of single and multiple doses of zuranolone in Japanese and White healthy subjects: A phase 1 clinical trial Abstract Abstract Aim This phase 1 study assessed the pharmacokinetics, safety, and tolerability of zuranolone in Japanese and White healthy adults, and Japanese healthy...
PMC11852071
core_pubmed_pmc
Pharmacogenetics and Pharmacokinetics of Moxifloxacin in MDR-TB Patients in Indonesia: Analysis for ABCB1 and SLCO1B1
Pharmacogenetics and Pharmacokinetics of Moxifloxacin in MDR-TB Patients in Indonesia: Analysis for ABCB1 and SLCO1B1 Abstract Background/Objectives : Studies show that SNPs in ABCB1 rs2032582 and SLCO1B1 rs4149015 affect the PK profile of moxifloxacin, a key drug for MDR-TB. This study aimed to assess the genotype fre...
PMC11892992
core_pubmed_pmc
Influence of Remifentanil on the Pharmacokinetics and Pharmacodynamics of Remimazolam in Healthy Volunteers
Influence of Remifentanil on the Pharmacokinetics and Pharmacodynamics of Remimazolam in Healthy Volunteers Abstract Abstract Background: Synergistic effects between opioids and remimazolam on Bispectral Index (BIS) and Modified Observer’s Assessment of Alertness and Sedation (MOAAS) score were previously described. Th...
PMC12764180
core_pubmed_pmc
Measurement of Centanafadine Concentrations in a Pharmacokinetic Trial: Comparison of Traditional Venipuncture Versus Blood Microsampling
Measurement of Centanafadine Concentrations in a Pharmacokinetic Trial: Comparison of Traditional Venipuncture Versus Blood Microsampling Abstract ABSTRACT In clinical pharmacology trials, pharmacokinetic samples are typically collected via venipuncture by trained staff. However, recent advances in blood collection dev...
PMC11496682
core_pubmed_pmc
Annonaceous acetogenins mimic AA005 targets mitochondrial trifunctional enzyme alpha subunit to treat obesity in male mice
Annonaceous acetogenins mimic AA005 targets mitochondrial trifunctional enzyme alpha subunit to treat obesity in male mice Abstract Abstract Obesity and related diseases pose a major health risk, yet current anti-obesity drugs inadequately addressing clinical needs. Here we show AA005, an annonaceous acetogenin mimic, ...
PMC10359732
core_pubmed_pmc
Efficacy and safety of CM310 in severe eosinophilic chronic rhinosinusitis with nasal polyps (CROWNS-1): a multicentre, randomised, double-blind, placebo-controlled phase 2 clinical trial
Efficacy and safety of CM310 in severe eosinophilic chronic rhinosinusitis with nasal polyps (CROWNS-1): a multicentre, randomised, double-blind, placebo-controlled phase 2 clinical trial Abstract Summary Background Severe eosinophilic chronic rhinosinusitis with nasal polyps (ECRSwNP) remains the most relapsed subtype...
PMC8203602
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MK2 Inhibitor ATI-450 in Healthy Subjects: A Placebo-Controlled, Randomized Phase 1 Study
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MK2 Inhibitor ATI-450 in Healthy Subjects: A Placebo-Controlled, Randomized Phase 1 Study Abstract Abstract Purpose ATI-450 is an oral, small-molecule inhibitor of the p38α mitogen-activated protein kinase (MAPK)/MAPK-activated protein kinase 2 (MK2) i...
PMC11576657
core_pubmed_pmc
Towards a platform quantitative systems pharmacology (QSP) model for preclinical to clinical translation of antibody drug conjugates (ADCs)
Towards a platform quantitative systems pharmacology (QSP) model for preclinical to clinical translation of antibody drug conjugates (ADCs) Abstract Abstract A next generation multiscale quantitative systems pharmacology (QSP) model for antibody drug conjugates (ADCs) is presented, for preclinical to clinical translati...
PMC9898489
core_pubmed_pmc
A physiologically based pharmacokinetic model for [ 68 Ga]Ga-(HA-)DOTATATE to predict whole-body distribution and tumor sink effects in GEP-NET patients
A physiologically based pharmacokinetic model for [ 68 Ga]Ga-(HA-)DOTATATE to predict whole-body distribution and tumor sink effects in GEP-NET patients Abstract Background Little is known about parameters that have a relevant impact on (dis)similarities in biodistribution between various 68 Ga-labeled somatostatin ana...
PMC7318183
core_pubmed_pmc
Comparing the Pharmacokinetics of 2 Novel Intravenous Tramadol Dosing Regimens to Oral Tramadol: A Randomized 3‐Arm Crossover Study
Comparing the Pharmacokinetics of 2 Novel Intravenous Tramadol Dosing Regimens to Oral Tramadol: A Randomized 3‐Arm Crossover Study Abstract Abstract Tramadol is a dual‐mechanism (opiate and monoamine reuptake inhibition) analgesic. Intravenous (IV) tramadol has been widely prescribed outside the United States. However...
PMC6662383
core_pubmed_pmc
Pharmacokinetics of Anakinra in Subjects of Heavier vs. Lighter Body Weights
Pharmacokinetics of Anakinra in Subjects of Heavier vs. Lighter Body Weights Abstract This trial (20010168) studied how body weight (BW) and body mass index (BMI) influenced the pharmacokinetics (PK) of anakinra. Subjects ( n = 32) were assigned to four groups ( n = 8) according to BW and BMI. Randomization was accordi...
PMC12294077
core_pubmed_pmc
Phytocompounds in Precision Dermatology: COX-2 Inhibitors as a Therapeutic Target in Atopic-Prone Skin
Phytocompounds in Precision Dermatology: COX-2 Inhibitors as a Therapeutic Target in Atopic-Prone Skin Abstract Abstract Atopic dermatitis (AD) is a chronic, multifactorial inflammatory skin disease characterized by persistent pruritus, immune system dysregulation, and an increased expression of cyclooxygenase-2 (COX-2...
PMC9953611
core_pubmed_pmc
Role of the Intestinal Microbiota in the Genesis of Major Depression and the Response to Antidepressant Drug Therapy: A Narrative Review
Role of the Intestinal Microbiota in the Genesis of Major Depression and the Response to Antidepressant Drug Therapy: A Narrative Review Abstract A major depressive disorder is a serious mental illness characterized by a pervasive low mood that negatively concerns personal life, work life, or education, affecting milli...
PMC6088477
core_pubmed_pmc
Antibiotic Dosing in Sustained Low-Efficiency Dialysis in Critically Ill Patients
Antibiotic Dosing in Sustained Low-Efficiency Dialysis in Critically Ill Patients Abstract Purpose of review: Sustained low-efficiency dialysis (SLED) is increasingly used as a renal replacement modality in critically ill patients with acute kidney injury (AKI) and hemodynamic instability. There is, therefore, a greate...
PMC10480294
core_pubmed_pmc
First-in-Human Study of the Safety, Pharmacokinetics, and Pharmacodynamics of MHV370, a Dual Inhibitor of Toll-Like Receptors 7 and 8, in Healthy Adults
First-in-Human Study of the Safety, Pharmacokinetics, and Pharmacodynamics of MHV370, a Dual Inhibitor of Toll-Like Receptors 7 and 8, in Healthy Adults Abstract Abstract Background and Objective MHV370, a dual antagonist of human Toll-like receptors (TLR) 7 and 8, suppresses cytokines and interferon-stimulated genes i...
PMC5336534
core_pubmed_pmc
In Vitro and In Vivo Modeling of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Erosion Under Fasting and Postprandial Status
In Vitro and In Vivo Modeling of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Erosion Under Fasting and Postprandial Status Abstract Purpose To develop a model linking in vitro and in vivo erosion of extended release tablets under fasting and postprandial status. Methods A nonlinear mixed-effects model was develo...
PMC8655892
core_pubmed_pmc
Pharmacokinetic Assessment of Rottlerin from Mallotus philippensis Using a Highly Sensitive Liquid Chromatography–Tandem Mass Spectrometry-Based Bioanalytical Method
Pharmacokinetic Assessment of Rottlerin from Mallotus philippensis Using a Highly Sensitive Liquid Chromatography–Tandem Mass Spectrometry-Based Bioanalytical Method Abstract Rottlerin is a key bioactive phytoconstituent present in the pericarp of Mallotus philippensis . It shows promising multifaceted pharmacological ...
PMC4514946
core_pubmed_pmc
Response of a clinical Escherichia coli strain to repeated cefquinome exposure in a piglet tissue-cage model
Response of a clinical Escherichia coli strain to repeated cefquinome exposure in a piglet tissue-cage model Abstract Background In order to provide some basis for effective dosage regimens that optimize efficacy with respect to bacteriological and clinical cures, the in vivo activity of cefquinome against a clinical E...
PMC5055907
core_pubmed_pmc
Use of population approach non-linear mixed effects models in the evaluation of biosimilarity of monoclonal antibodies
Use of population approach non-linear mixed effects models in the evaluation of biosimilarity of monoclonal antibodies Abstract Purpose Population pharmacokinetic analyses (PPK) have been used to establish bioequivalence for small molecules and some biologicals. We investigated whether PPK could also be useful in biosi...
PMC12650091
core_pubmed_pmc
Cytokine Dynamics During Ustekinumab Induction as Predictors of Treatment Response in Crohn’s Disease: An Observational Study
Cytokine Dynamics During Ustekinumab Induction as Predictors of Treatment Response in Crohn’s Disease: An Observational Study Abstract Abstract Background/Objectives : Crohn’s disease (CD) is a chronic immune-mediated disorder with heterogeneous response to biologic therapies. Ustekinumab (UST), an anti-IL-12/23 monocl...
PMC8235515
core_pubmed_pmc
Brain Disposition of Antibody-Based Therapeutics: Dogma, Approaches and Perspectives
Brain Disposition of Antibody-Based Therapeutics: Dogma, Approaches and Perspectives Abstract Due to their high specificity, monoclonal antibodies have been widely investigated for their application in drug delivery to the central nervous system (CNS) for the treatment of neurological diseases such as stroke, Alzheimer...
PMC5897516
core_pubmed_pmc
Compromised Blood–Brain Barrier Integrity Is Associated With Total Magnetic Resonance Imaging Burden of Cerebral Small Vessel Disease
Compromised Blood–Brain Barrier Integrity Is Associated With Total Magnetic Resonance Imaging Burden of Cerebral Small Vessel Disease Abstract Objective Several studies have demonstrated that compromised blood–brain barrier (BBB) integrity may play a pivotal role in the pathogenesis of individual cerebral small vessel ...
PMC9131543
core_pubmed_pmc
Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses
Pharmacokinetics, adverse effects and effects on thermal nociception following administration of three doses of codeine to horses Abstract Abstract Background In humans, codeine is a commonly prescribed analgesic that produces its therapeutic effect largely through metabolism to morphine. In some species, analgesic eff...
PMC6005123
core_pubmed_pmc
The Potential for Treatment Shortening With Higher Rifampicin Doses: Relating Drug Exposure to Treatment Response in Patients With Pulmonary Tuberculosis
The Potential for Treatment Shortening With Higher Rifampicin Doses: Relating Drug Exposure to Treatment Response in Patients With Pulmonary Tuberculosis Abstract Abstract Background Tuberculosis remains a huge public health problem and the prolonged treatment duration obstructs effective tuberculosis control. Higher r...
PMC10067887
core_pubmed_pmc
Successful switching from risperidone to cariprazine in a schizophrenic patient with pronounced functional deficit. Case report
Successful switching from risperidone to cariprazine in a schizophrenic patient with pronounced functional deficit. Case report Abstract A 22-year-old male was admitted to an in-patient psychiatric unit for treatment, after a period of 2 years of increasing psychotic symptoms corresponding to a very severe case of schi...
PMC4580721
core_pubmed_pmc
Clinical Pharmacokinetic Studies of Enzalutamide
Clinical Pharmacokinetic Studies of Enzalutamide Abstract Abstract Background and Objectives Oral enzalutamide (160 mg once daily) is approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). This article describes the pharmacokinetics of enzalutamide and its active metabolite N -desmethyl ...
PMC5830021
core_pubmed_pmc
Efficacy and Safety of Insulin Glargine 300 U/mL versus 100 U/mL in Diabetes Mellitus: A Comprehensive Review of the Literature
Efficacy and Safety of Insulin Glargine 300 U/mL versus 100 U/mL in Diabetes Mellitus: A Comprehensive Review of the Literature Abstract Abstract To achieve good metabolic control in diabetes and maintain it in the long term, a combination of changes in lifestyle and pharmacological treatment is necessary. The need for...
PMC9863862
core_pubmed_pmc
Transplant-Associated Thrombotic Microangiopathy in the Context of Allogenic Hematopoietic Stem Cell Transplantation: Where We Stand
Transplant-Associated Thrombotic Microangiopathy in the Context of Allogenic Hematopoietic Stem Cell Transplantation: Where We Stand Abstract Abstract Transplant-associated thrombotic microangiopathy (TA-TMA) constitutes a significant contributor to the increased morbidity and mortality after allogenic hematopoietic st...
PMC12958287
core_pubmed_pmc
High-Throughput Physiologically Based Pharmacokinetic Model for Rodent Pharmacokinetics Prediction Using Machine Learning-Predicted Inputs and a Large In Vivo Pharmacokinetics Data Set
High-Throughput Physiologically Based Pharmacokinetic Model for Rodent Pharmacokinetics Prediction Using Machine Learning-Predicted Inputs and a Large In Vivo Pharmacokinetics Data Set Abstract Accurate prediction of the pharmacokinetic (PK) properties of small-molecule drug candidates is a critical aspect of pharmaceu...
PMC9414097
core_pubmed_pmc
Liposomal Mineral Absorption: A Randomized Crossover Trial
Liposomal Mineral Absorption: A Randomized Crossover Trial Abstract Multivitamin/mineral (MVM) supplements are one of the most popular dietary supplement categories. The purpose of this analysis was to determine if a novel liposomal delivery mechanism improves mineral absorption from an MVM product. In a randomized cro...
PMC10818978
core_pubmed_pmc
Development and Validation of a UPLC-MS/MS Method for Therapeutic Drug Monitoring, Pharmacokinetic and Stability Studies of First-Line Antituberculosis Drugs in Urine
Development and Validation of a UPLC-MS/MS Method for Therapeutic Drug Monitoring, Pharmacokinetic and Stability Studies of First-Line Antituberculosis Drugs in Urine Abstract Abstract Tuberculosis (TB) remains one of the leading global causes of mortality. Several methods have been established to detect anti-TB agents...
PMC6027249
core_pubmed_pmc
Plant-Derived Anticancer Agents: Lessons from the Pharmacology of Geniposide and Its Aglycone, Genipin
Plant-Derived Anticancer Agents: Lessons from the Pharmacology of Geniposide and Its Aglycone, Genipin Abstract Abstract For centuries, plants have been exploited by mankind as sources of numerous cancer chemotherapeutic agents. Good examples of anticancer compounds of clinical significance today include the taxanes (e...
PMC10393936
core_pubmed_pmc
Validating a novel three-times-weekly post-hemodialysis ceftriaxone regimen in infected Indigenous Australian patients—a population pharmacokinetic study
Validating a novel three-times-weekly post-hemodialysis ceftriaxone regimen in infected Indigenous Australian patients—a population pharmacokinetic study Abstract Abstract Objectives To describe the total and unbound population pharmacokinetics of a 2 g three-times-weekly post-dialysis ceftriaxone regimen in Indigenous...
PMC12879164
core_pubmed_pmc
Sustained Benefit of Blinatumomab in Infants With KMT2A -Rearranged ALL: Long-Term Outcomes, Toxicity, and Pharmacokinetics
Sustained Benefit of Blinatumomab in Infants With KMT2A -Rearranged ALL: Long-Term Outcomes, Toxicity, and Pharmacokinetics Abstract KMT2A -rearranged infant ALL ( KMT2A -r ALL) has a poor prognosis. Adding blinatumomab, a bispecific T-cell engager targeting CD19, to standard chemotherapy for infants with KMT2A -r ALL ...
PMC6138487
core_pubmed_pmc
Effect of single and multiple doses of elobixibat, an ileal bile acid transporter inhibitor, on chronic constipation: A randomized controlled trial
Effect of single and multiple doses of elobixibat, an ileal bile acid transporter inhibitor, on chronic constipation: A randomized controlled trial Abstract Abstract Aims Elobixibat is a minimally absorbed ileal bile acid transporter inhibitor. This study aimed to investigate the safety, tolerability, efficacy, pharmac...
PMC7264171
core_pubmed_pmc
The atorvastatin metabolic phenotype shift is influenced by interaction of drug-transporter polymorphisms in Mexican population: results of a randomized trial
The atorvastatin metabolic phenotype shift is influenced by interaction of drug-transporter polymorphisms in Mexican population: results of a randomized trial Abstract Abstract Atorvastatin (ATV) is a blood cholesterol-lowering drug used to prevent cardiovascular events, the leading cause of death worldwide. As pharmac...
PMC9673800
core_pubmed_pmc
Structure and Function of Recombinant versus Plasma-Derived von Willebrand Factor and Impact on Multimer Pharmacokinetics in von Willebrand Disease
Structure and Function of Recombinant versus Plasma-Derived von Willebrand Factor and Impact on Multimer Pharmacokinetics in von Willebrand Disease Abstract Abstract Background Recombinant von Willebrand factor (rVWF, vonicog alfa) is a purified VWF concentrate produced from Chinese hamster ovary cells. rVWF is not exp...
PMC7076374
core_pubmed_pmc
Improved Pharmacokinetics and Tissue Uptake of Complexed Daidzein in Rats
Improved Pharmacokinetics and Tissue Uptake of Complexed Daidzein in Rats Abstract Abstract The pharmacokinetic profile and tissue uptake of daidzein (DAI) was determined in rat serum and tissues (lungs, eyes, brain, heart, spleen, fat, liver, kidney, and testes) after intravenous and intraperitoneal administration of ...
PMC3502166
core_pubmed_pmc
Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda
Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda Abstract Background Malaria in pregnancy increases the risk of maternal anemia, abortion and low birth weight. Approximately 85.3 million pregnancies occur annually in areas with...
PMC8469090
core_pubmed_pmc
Bleomycin Concentration in Patients’ Plasma and Tumors after Electrochemotherapy. A Study from InspECT Group
Bleomycin Concentration in Patients’ Plasma and Tumors after Electrochemotherapy. A Study from InspECT Group Abstract The plasma concentration profile of bleomycin in the distribution phase of patients younger than 65 years is needed to determine the suitable time interval for efficient application of electric pulses d...
PMC3797131
core_pubmed_pmc
Global Metabolomic Profiling Reveals an Association of Metal Fume Exposure and Plasma Unsaturated Fatty Acids
Global Metabolomic Profiling Reveals an Association of Metal Fume Exposure and Plasma Unsaturated Fatty Acids Abstract Abstract Background Welding-associated air pollutants negatively affect the health of exposed workers; however, their molecular mechanisms in causing disease remain largely unclear. Few studies have sy...
PMC5306088
core_pubmed_pmc
Lesion remyelinating activity of GSK239512 versus placebo in patients with relapsing-remitting multiple sclerosis: a randomised, single-blind, phase II study
Lesion remyelinating activity of GSK239512 versus placebo in patients with relapsing-remitting multiple sclerosis: a randomised, single-blind, phase II study Abstract Histamine H 3 receptor blockade may enhance lesion remyelination in multiple sclerosis (MS). The efficacy (using a magnetic resonance imaging marker of m...
PMC10197937
core_pubmed_pmc
Venetoclax Penetrates the Blood Brain Barrier: A Pharmacokinetic Analysis in Pediatric Leukemia Patients
Venetoclax Penetrates the Blood Brain Barrier: A Pharmacokinetic Analysis in Pediatric Leukemia Patients Abstract Infiltration of malignant cells into the central nervous system in hematological malignancies correlates with poor clinical outcomes. Investigations into the penetration of venetoclax into the central nervo...
PMC12188672
core_pubmed_pmc
Determination of the latent geometry of atorvastatin pharmacokinetics by transfer entropy to identify bottlenecks
Determination of the latent geometry of atorvastatin pharmacokinetics by transfer entropy to identify bottlenecks Abstract Abstract Background In mathematics, a physical network (e.g. biological network, social network, IT network, communication network) is usually represented by a graph. The determination of the metri...
PMC5648736
core_pubmed_pmc
Pharmacokinetics and Tolerability of a Single Dose of Semaglutide, a Human Glucagon-Like Peptide-1 Analog, in Subjects With and Without Renal Impairment
Pharmacokinetics and Tolerability of a Single Dose of Semaglutide, a Human Glucagon-Like Peptide-1 Analog, in Subjects With and Without Renal Impairment Abstract Background The pharmacokinetics and tolerability of semaglutide, a once-weekly human glucagon-like peptide-1 analog in development for the treatment of type 2...
PMC7033572
core_pubmed_pmc
Cytochrome P450-Based Drug-Drug Interactions of Vonoprazan In Vitro and In Vivo
Cytochrome P450-Based Drug-Drug Interactions of Vonoprazan In Vitro and In Vivo Abstract Background Vonoprazan fumarate is a potassium-competitive acid blocker that was developed as a novel acid-suppressing drug for multiple indications. As a potential alternative to proton-pump inhibitors, the determination of the dru...
PMC9920246
core_pubmed_pmc
Entinostat-Bortezomib Hybrids against Multiple Myeloma
Entinostat-Bortezomib Hybrids against Multiple Myeloma Abstract Although proteasome inhibitors have emerged as the therapeutic backbone of multiple myeloma treatment, patients often relapse and become drug refractory. The combination between proteasome and histone deacetylase inhibitors has shown to be more efficient c...
PMC11879997
core_pubmed_pmc
Phytochemical baicalin potentially inhibits Bcl-2 and VEGF: an in silico approach
Phytochemical baicalin potentially inhibits Bcl-2 and VEGF: an in silico approach Abstract Background The rising prevalence of cancer cells exhibits uncontrolled growth and invasive and aggressive properties, leading to metastasis, which poses a significant challenge for global health. Central to cancer development are...
PMC11547995
core_pubmed_pmc
Safety Evaluations of Rapamycin Perfluorocarbon Nanoparticles in Ovarian Tumor-Bearing Mice
Safety Evaluations of Rapamycin Perfluorocarbon Nanoparticles in Ovarian Tumor-Bearing Mice Abstract Nanomedicine holds great potential for revolutionizing medical treatment. Ongoing research and advancements in nanotechnology are continuously expanding the possibilities, promising significant advancements in healthcar...
PMC8891208
core_pubmed_pmc
Population Pharmacokinetic Modeling of Inebilizumab in Subjects with Neuromyelitis Optica Spectrum Disorders, Systemic Sclerosis, or Relapsing Multiple Sclerosis
Population Pharmacokinetic Modeling of Inebilizumab in Subjects with Neuromyelitis Optica Spectrum Disorders, Systemic Sclerosis, or Relapsing Multiple Sclerosis Abstract Abstract Background and Objective Inebilizumab is a humanized, affinity-optimized, afucosylated immunoglobulin (Ig)-G1κ monoclonal antibody that bind...
PMC10714243
core_pubmed_pmc
Molecular docking, drug-likeness and DFT study of some modified tetrahydrocurcumins as potential anticancer agents
Molecular docking, drug-likeness and DFT study of some modified tetrahydrocurcumins as potential anticancer agents Abstract Abstract The present study utilized molecular docking and density functional theory (DFT) approaches, and ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties to invest...
PMC4427304
core_pubmed_pmc
First-In-Human, Double-Blind, Placebo-Controlled, Randomized, Dose-Escalation Study of BG00010, a Glial Cell Line-Derived Neurotrophic Factor Family Member, in Subjects with Unilateral Sciatica
First-In-Human, Double-Blind, Placebo-Controlled, Randomized, Dose-Escalation Study of BG00010, a Glial Cell Line-Derived Neurotrophic Factor Family Member, in Subjects with Unilateral Sciatica Abstract Objective To evaluate the safety, tolerability, and pharmacokinetics of single doses of BG00010 (neublastin, artemin,...
PMC12259677
core_pubmed_pmc
Curcumin, EGCG and apigenin in cervical cancer: mechanistic insights and therapeutic potential
Curcumin, EGCG and apigenin in cervical cancer: mechanistic insights and therapeutic potential Abstract Abstract Cervical cancer (CC) continues to be the major cause of death from cancer in women worldwide and highlights the necessity for novel therapeutic approaches that target key oncogenic pathways. Conventional tre...
PMC7303306
core_pubmed_pmc
Intensive Hemodiafiltration Successfully Removes Ganciclovir Overdose and Largely Exceeds Reported Elimination During Hemodialysis—A Case Report and Review of the Literature
Intensive Hemodiafiltration Successfully Removes Ganciclovir Overdose and Largely Exceeds Reported Elimination During Hemodialysis—A Case Report and Review of the Literature Abstract Abstract We present the case of a kidney transplant patient (Cockroft-Gault estimated creatinine clearance 14 ml/min) who was inadvertent...
PMC8020358
core_pubmed_pmc
Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects Abstract Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritu...
PMC8617681
core_pubmed_pmc
P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO)
P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO) Abstract Selpercatinib is a targeted, FDA-approved, oral, small-molecule inhibitor for the treatment of rearranged during transfection (RET) proto-onc...
PMC12567070
core_pubmed_pmc
Immunomodulatory Activities of Emerging Rare Ginsenosides F1, Rg5, Rk1, Rh1, and Rg2: From Molecular Mechanisms to Therapeutic Applications
Immunomodulatory Activities of Emerging Rare Ginsenosides F1, Rg5, Rk1, Rh1, and Rg2: From Molecular Mechanisms to Therapeutic Applications Abstract Abstract Ginsenosides, the primary bioactive components of Panax ginseng , have demonstrated significant immunomodulatory potential. While major ginsenosides have been ext...
PMC8879246
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Two Empagliflozin, with Evaluation in Healthy Jordanian Subjects under Fasting and Fed Conditions
Pharmacokinetics and Bioequivalence of Two Empagliflozin, with Evaluation in Healthy Jordanian Subjects under Fasting and Fed Conditions Abstract The current study is a randomized, open-label, two-period, two-sequence, two-way crossover pharmacokinetic study in healthy Jordanian subjects to evaluate the pharmacokinetic...
PMC6879261
core_pubmed_pmc
Safety, Pharmacokinetics, and Antiviral Activity of AT-527, a Novel Purine Nucleotide Prodrug, in Hepatitis C Virus-Infected Subjects with or without Cirrhosis
Safety, Pharmacokinetics, and Antiviral Activity of AT-527, a Novel Purine Nucleotide Prodrug, in Hepatitis C Virus-Infected Subjects with or without Cirrhosis Abstract AT-527 is a novel modified guanosine nucleotide prodrug inhibitor of the hepatitis C virus (HCV) NS5B polymerase, with increased in vitro antiviral act...
PMC3934676
core_pubmed_pmc
Preparation and the Biopharmaceutical Evaluation for the Metered Dose Transdermal Spray of Dexketoprofen
Preparation and the Biopharmaceutical Evaluation for the Metered Dose Transdermal Spray of Dexketoprofen Abstract The objective of the present work was to develop a metered dose transdermal spray (MDTS) formulation for transdermal delivery of dexketoprofen (DE). DE release from a series of formulations was assessed in ...
PMC12529375
core_pubmed_pmc
Crocetin Impairs the Cytochrome P450 Epoxygenase Pathway toward Potentiating the Therapeutic Efficacy of Paclitaxel in Metastatic Breast Cancer
Crocetin Impairs the Cytochrome P450 Epoxygenase Pathway toward Potentiating the Therapeutic Efficacy of Paclitaxel in Metastatic Breast Cancer Abstract Abstract Triple-negative breast cancer (TNBC) is the most fatal subtype of breast cancer owing to its aggressive nature and limited treatment strategies. Despite signi...
PMC12474851
core_pubmed_pmc
18 F-BMS-986229 PET imaging of tumor PD-L1 expression in glioblastoma patients
18 F-BMS-986229 PET imaging of tumor PD-L1 expression in glioblastoma patients Abstract Abstract Background Neurooncologists urgently need biomarkers that can optimize the clinical development of PD-L1 targeted immunotherapy in the treatment of glioblastoma. This study evaluated PD-L1 targeted tumor imaging by positron...
PMC5788661
core_pubmed_pmc
Dose- and time-dependence of the host-mediated response to paclitaxel therapy: a mathematical modeling approach
Dose- and time-dependence of the host-mediated response to paclitaxel therapy: a mathematical modeling approach Abstract Abstract It has recently been suggested that pro-tumorigenic host-mediated processes induced in response to chemotherapy counteract the anti-tumor activity of therapy, and thereby decrease net therap...
PMC10864494
core_pubmed_pmc
Tolerability, safety, and pharmacokinetics of a single intravenous administration of a novel recombinant humanized anti-interleukin-6 receptor monoclonal antibody in healthy Chinese volunteers
Tolerability, safety, and pharmacokinetics of a single intravenous administration of a novel recombinant humanized anti-interleukin-6 receptor monoclonal antibody in healthy Chinese volunteers Abstract Abstract Aim: VDJ001 is a novel recombinant humanized monoclonal antibody against the anti-interleukin-6 receptor. As ...
PMC7318214
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamics of Ontamalimab (SHP647), a Fully Human Monoclonal Antibody Against Mucosal Addressin Cell Adhesion Molecule‐1 (MAdCAM‐1), in Patients With Ulcerative Colitis or Crohn's Disease
Population Pharmacokinetics and Pharmacodynamics of Ontamalimab (SHP647), a Fully Human Monoclonal Antibody Against Mucosal Addressin Cell Adhesion Molecule‐1 (MAdCAM‐1), in Patients With Ulcerative Colitis or Crohn's Disease Abstract Abstract Ontamalimab (SHP647) is a fully human, immunoglobulin G 2 , antihuman mucosa...
PMC7327145
core_pubmed_pmc
Effects of Diabetes Mellitus on the Disposition of Tofacitinib, a Janus Kinase Inhibitor, in Rats
Effects of Diabetes Mellitus on the Disposition of Tofacitinib, a Janus Kinase Inhibitor, in Rats Abstract Abstract Tofacitinib, a Janus kinase inhibitor, was developed for the treatment of rheumatoid arthritis. Recently, it has been associated with an increased change in arthritis development in patients with diabetes...