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PMC9095520 | core_pubmed_pmc | Extending the viability of human precision-cut intestinal slice model for drug metabolism studies | Extending the viability of human precision-cut intestinal slice model for drug metabolism studies Abstract Human Precision-cut intestinal slices (hPCIS) are used to study intestinal physiology, pathophysiology, drug efficacy, toxicology, kinetics, and metabolism. However, the use of this ex vivo model is restricted to ... |
PMC11936181 | core_pubmed_pmc | Screening potential anti-osteoarthritis compounds using molecular docking based on MAPK and NFκB pathways and validating their anti-osteoarthritis effect | Screening potential anti-osteoarthritis compounds using molecular docking based on MAPK and NFκB pathways and validating their anti-osteoarthritis effect Abstract Osteoarthritis is an extremely common disease. However, it lacks effective nonsurgical treatments. Molecular docking has been widely used in drug discovery. ... |
PMC4189705 | core_pubmed_pmc | A novel hydrolysis-resistant lipophilic folate derivative enables stable delivery of targeted liposomes in vivo | A novel hydrolysis-resistant lipophilic folate derivative enables stable delivery of targeted liposomes in vivo Abstract Abstract Instability of targeting ligand is a roadblock towards successful development of folate targeted liposomes. Folate ligands have been linked to polyethylene glycol (PEG) and cholesterol by an... |
PMC8044368 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Dosage Individualization of Suppressive Beta-Lactam Therapy Administered by Subcutaneous Route in Patients With Prosthetic Joint Infection | Pharmacokinetic/Pharmacodynamic Dosage Individualization of Suppressive Beta-Lactam Therapy Administered by Subcutaneous Route in Patients With Prosthetic Joint Infection Abstract Abstract Suppressive parenteral antibiotic therapy with beta-lactams may be necessary in patients with Gram-negative bone and joint infectio... |
PMC6680770 | core_pubmed_pmc | Effect of Ticagrelor, a Cytochrome P450 3A4 Inhibitor, on the Pharmacokinetics of Tadalafil in Rats | Effect of Ticagrelor, a Cytochrome P450 3A4 Inhibitor, on the Pharmacokinetics of Tadalafil in Rats Abstract Abstract Tadalafil is a cytochrome P450 (CYP) 3A4 substrate. Because there are few data on drug-drug interactions, it is advisable to take sufficient consideration when co-administering tadalafil with CYP3A4 ind... |
PMC5266375 | core_pubmed_pmc | Investigation of the Regulatory Effects of Saccharin on Cytochrome P450s in Male ICR Mice | Investigation of the Regulatory Effects of Saccharin on Cytochrome P450s in Male ICR Mice Abstract Saccharin, the first artificial sweetener, was discovered in 1879 that do not have any calories and is approximately 200~700 times sweeter than sugar. Saccharin was the most common domestically produced sweetener in Korea... |
PMC4296935 | core_pubmed_pmc | Warfarin Dosage Response Related Pharmacogenetics in Chinese Population | Warfarin Dosage Response Related Pharmacogenetics in Chinese Population Abstract Objectives As the most frequently prescribed anticoagulant, warfarin has large inter-individual variability in dosage. Genetic polymorphisms could largely explain the differences in dosage requirement. rs9923231 (VKORC1), rs7294 (VKORC1), ... |
PMC8343808 | core_pubmed_pmc | A Clinician’s Guide to Dosing Analgesics, Anticonvulsants, and Psychotropic Medications in Continuous Renal Replacement Therapy | A Clinician’s Guide to Dosing Analgesics, Anticonvulsants, and Psychotropic Medications in Continuous Renal Replacement Therapy Abstract Abstract Acute kidney injury (AKI) requiring continuous renal replacement therapy (CRRT) is a common complication in critical illness and has a significant impact on pharmacokinetic f... |
PMC12264984 | core_pubmed_pmc | The antipsychotics functional index (AFI) in schizophrenia | The antipsychotics functional index (AFI) in schizophrenia Abstract Abstract Schizophrenia can lead to significant and long-lasting deficits in patient functionality. The present study proposes a theoretical index that predicts the ability of an antipsychotic to improve the functionality of patients with schizophrenia.... |
PMC12718592 | core_pubmed_pmc | Phase 1 study evaluating the safety, preliminary efficacy, and pharmacodynamics of recombinant interleukin-15 in combination with nivolumab and ipilimumab in patients with refractory cancers | Phase 1 study evaluating the safety, preliminary efficacy, and pharmacodynamics of recombinant interleukin-15 in combination with nivolumab and ipilimumab in patients with refractory cancers Abstract Abstract Purpose Combinations of immune checkpoint inhibitors and cytokine therapies have shown promise in cancer immuno... |
PMC11217551 | core_pubmed_pmc | Integration of individual preclinical and clinical anti‐infective PKPD data to predict clinical study outcomes | Integration of individual preclinical and clinical anti‐infective PKPD data to predict clinical study outcomes Abstract Abstract The AIDA randomized clinical trial found no significant difference in clinical failure or survival between colistin monotherapy and colistin–meropenem combination therapy in carbapenem‐resist... |
PMC12942897 | core_pubmed_pmc | Development and Systematic Evaluation of a Low-Irritation PFD-AIS Formulation for Pulmonary-Targeted Therapy | Development and Systematic Evaluation of a Low-Irritation PFD-AIS Formulation for Pulmonary-Targeted Therapy Abstract Abstract Background: To overcome the gastrointestinal and hepatic toxicity of oral pirfenidone (PFD) in the treatment of idiopathic pulmonary fibrosis (IPF), this study systematically constructed a mini... |
PMC9555197 | core_pubmed_pmc | Safety and Biological Activity of Rozibafusp alfa, a Bispecific Inhibitor of Inducible Costimulator Ligand and B Cell Activating Factor, in Patients With Rheumatoid Arthritis: Results of a Phase 1b, Randomized, Double‐Blind , Placebo‐Controlled , Multiple Ascending Dose Study | Safety and Biological Activity of Rozibafusp alfa, a Bispecific Inhibitor of Inducible Costimulator Ligand and B Cell Activating Factor, in Patients With Rheumatoid Arthritis: Results of a Phase 1b, Randomized, Double‐Blind , Placebo‐Controlled , Multiple Ascending Dose Study Abstract Objective To assess the safety and... |
PMC5064155 | core_pubmed_pmc | A Faropenem, Linezolid, and Moxifloxacin Regimen for Both Drug-Susceptible and Multidrug-Resistant Tuberculosis in Children: FLAME Path on the Milky Way | A Faropenem, Linezolid, and Moxifloxacin Regimen for Both Drug-Susceptible and Multidrug-Resistant Tuberculosis in Children: FLAME Path on the Milky Way Abstract Background. The regimen of linezolid and moxifloxacin was found to be efficacious in the hollow fiber system model of pediatric intracellular tuberculosis. Ho... |
PMC10097575 | core_pubmed_pmc | Prenatal Ambient Air Pollutant Mixture Exposure and Early School-age Lung Function | Prenatal Ambient Air Pollutant Mixture Exposure and Early School-age Lung Function Abstract Introduction: Research linking prenatal ambient air pollution with childhood lung function has largely considered one pollutant at a time. Real-life exposure is to mixtures of pollutants and their chemical components; not consid... |
PMC6617920 | core_pubmed_pmc | Nocturnal Glycemic Control with New Insulin Glargine 300 U/mL | Nocturnal Glycemic Control with New Insulin Glargine 300 U/mL Abstract Abstract Insulin glargine 300 U/mL (Gla-300) is a new generation basal insulin product that has been demonstrated to have more stable pharmacokinetic and pharmacodynamic characteristics than insulin glargine 100 U/mL (Gla-100). To evaluate the real-... |
PMC12055491 | core_pubmed_pmc | Safe and effective use of vancomycin | Safe and effective use of vancomycin Abstract SUMMARY Vancomycin is an important antimicrobial for prophylactic, empirical and directed therapy of Gram-positive organisms. Therapeutic drug monitoring is recommended for all patients expected to receive vancomycin for more than 48 hours to optimise drug exposure. Monitor... |
PMC4895815 | core_pubmed_pmc | Safety and tolerability of an anti-CD19 monoclonal antibody, MEDI-551, in subjects with systemic sclerosis: a phase I, randomized, placebo-controlled, escalating single-dose study | Safety and tolerability of an anti-CD19 monoclonal antibody, MEDI-551, in subjects with systemic sclerosis: a phase I, randomized, placebo-controlled, escalating single-dose study Abstract Abstract Background Systemic sclerosis (SSc) is a clinically heterogeneous, life-threatening disease characterized by fibrosis, mic... |
PMC4333237 | core_pubmed_pmc | A pharmacometric pulmonary model predicting the extent and rate of distribution from plasma to epithelial lining fluid and alveolar cells—using rifampicin as an example | A pharmacometric pulmonary model predicting the extent and rate of distribution from plasma to epithelial lining fluid and alveolar cells—using rifampicin as an example Abstract Abstract Purpose The purpose of the study was to develop a drug-unspecific approach to pharmacometric modeling for predicting the rate and ext... |
PMC8953460 | core_pubmed_pmc | Development and Performance Verification of the PBPK Model for Antazoline and Its Metabolite and Its Utilization for Pharmacological Hypotheses Formulating | Development and Performance Verification of the PBPK Model for Antazoline and Its Metabolite and Its Utilization for Pharmacological Hypotheses Formulating Abstract Antazoline is an antihistaminic drug that is effective in the termination of paroxysmal atrial fibrillation. Despite its long presence in the market, antaz... |
PMC9300170 | core_pubmed_pmc | Population Pharmacokinetics of Ponatinib in Healthy Adult Volunteers and Patients With Hematologic Malignancies and Model‐Informed Dose Selection for Pediatric Development | Population Pharmacokinetics of Ponatinib in Healthy Adult Volunteers and Patients With Hematologic Malignancies and Model‐Informed Dose Selection for Pediatric Development Abstract Abstract The BCR‐ABL1 inhibitor ponatinib is approved for the treatment of adults with chronic myeloid leukemia or Philadelphia chromosome–... |
PMC5909170 | core_pubmed_pmc | Inconsistencies in dosage practice in children with overweight or obesity: A retrospective cohort study | Inconsistencies in dosage practice in children with overweight or obesity: A retrospective cohort study Abstract Abstract Obesity can affect the pharmacokinetics of most drugs, which may result in under‐ or overdosing if traditional pediatric dosing strategies are used. To investigate currently applied dosage strategie... |
PMC10222980 | core_pubmed_pmc | Donepezil Brain and Blood Pharmacokinetic Modeling after Nasal Film and Oral Solution Administration in Mice | Donepezil Brain and Blood Pharmacokinetic Modeling after Nasal Film and Oral Solution Administration in Mice Abstract Abstract Intranasal delivery is a non-invasive mode of administration, gaining popularity due to its potential for targeted delivery to the brain. The anatomic connection of the nasal cavity with the ce... |
PMC9379816 | core_pubmed_pmc | Role of Therapeutic Drug Monitoring in the Treatment of Persistent Mycobacterium abscessus Central Nervous System Infection: A Case Report and Review of the Literature | Role of Therapeutic Drug Monitoring in the Treatment of Persistent Mycobacterium abscessus Central Nervous System Infection: A Case Report and Review of the Literature Abstract Abstract A patient presenting with recurrent ventriculoperitoneal shunt infection was found to have Mycobacterium abscessus growing from cerebr... |
PMC3053459 | core_pubmed_pmc | Facile labelling of an anti-epidermal growth factor receptor Nanobody with 68 Ga via a novel bifunctional desferal chelate for immuno-PET | Facile labelling of an anti-epidermal growth factor receptor Nanobody with 68 Ga via a novel bifunctional desferal chelate for immuno-PET Abstract Abstract Purpose The ∼15 kDa variable domains of camelid heavy-chain-only antibodies (called Nanobodies®) have the flexibility to be formatted as monovalent, monospecific, m... |
PMC12796225 | core_pubmed_pmc | GLYCO-BUILD: an enzymatic pipeline for the synthesis of peptides carrying eukaryotic N -glycans | GLYCO-BUILD: an enzymatic pipeline for the synthesis of peptides carrying eukaryotic N -glycans Abstract Peptides and proteins containing defined N -glycans hold great promise for biomedicine because the attached glycans engage in specific interactions, influence targeted delivery and folding, and improve pharmacokinet... |
PMC10133723 | core_pubmed_pmc | Standards for model-based early bactericidal activity analysis and sample size determination in tuberculosis drug development | Standards for model-based early bactericidal activity analysis and sample size determination in tuberculosis drug development Abstract Background: A critical step in tuberculosis (TB) drug development is the Phase 2a early bactericidal activity (EBA) study which informs if a new drug or treatment has short-term activit... |
PMC10368306 | core_pubmed_pmc | Impact of Obesity on the Drug–Drug Interaction Between Dolutegravir and Rifampicin or Any Other Strong Inducers | Impact of Obesity on the Drug–Drug Interaction Between Dolutegravir and Rifampicin or Any Other Strong Inducers Abstract Abstract Background Obesity is increasingly prevalent among people with HIV. Obesity can impact drug pharmacokinetics and consequently the magnitude of drug–drug interactions (DDIs) and, thus, the re... |
PMC9746849 | core_pubmed_pmc | A Phase 3, Open-Label Study of Lumacaftor/Ivacaftor in Children 1 to Less Than 2 Years of Age with Cystic Fibrosis Homozygous for F508del-CFTR | A Phase 3, Open-Label Study of Lumacaftor/Ivacaftor in Children 1 to Less Than 2 Years of Age with Cystic Fibrosis Homozygous for F508del-CFTR Abstract Rationale Previous phase 3 trials showed that treatment with lumacaftor/ivacaftor was safe and efficacious in people aged ⩾2 years with cystic fibrosis (CF) homozygous ... |
PMC11265664 | core_pubmed_pmc | Modeling soybean growth: A mixed model approach | Modeling soybean growth: A mixed model approach Abstract Abstract The evaluation of plant and animal growth, separately for genetic and environmental effects, is necessary for genetic understanding and genetic improvement of environmental responses of plants and animals. We propose to extend an existing approach that c... |
PMC5136567 | core_pubmed_pmc | Intravenous Topiramate: Pharmacokinetics in Dogs with Naturally Occurring Epilepsy | Intravenous Topiramate: Pharmacokinetics in Dogs with Naturally Occurring Epilepsy Abstract Abstract Rationale Barriers to developing treatments for human status epilepticus include the inadequacy of experimental animal models. In contrast, naturally occurring canine epilepsy is similar to the human condition and can s... |
PMC8840471 | core_pubmed_pmc | Polymyxin B Combined with Minocycline: A Potentially Effective Combination against bla OXA-23 -harboring CRAB in In Vitro PK/PD Model | Polymyxin B Combined with Minocycline: A Potentially Effective Combination against bla OXA-23 -harboring CRAB in In Vitro PK/PD Model Abstract Polymyxin-based combination therapy is commonly used to treat carbapenem-resistant Acinetobacter baumannii (CRAB) infections. In the present study, the bactericidal effect of po... |
PMC8279414 | core_pubmed_pmc | Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins | Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins Abstract Abstract The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and s... |
PMC3369391 | core_pubmed_pmc | Maximum Recommended Dosage of Lithium for Pregnant Women Based on a PBPK Model for Lithium Absorption | Maximum Recommended Dosage of Lithium for Pregnant Women Based on a PBPK Model for Lithium Absorption Abstract Treatment of bipolar disorder with lithium therapy during pregnancy is a medical challenge. Bipolar disorder is more prevalent in women and its onset is often concurrent with peak reproductive age. Treatment t... |
PMC8398830 | core_pubmed_pmc | Mechanistic PBPK Modelling to Predict the Advantage of the Salt Form of a Drug When Dosed with Acid Reducing Agents | Mechanistic PBPK Modelling to Predict the Advantage of the Salt Form of a Drug When Dosed with Acid Reducing Agents Abstract Acid reducing agents (ARAs) reduce the dissolution rate of weakly basic drugs in the stomach potentially leading to lower bioavailability. Formulating the API as a rapidly dissolving salt is one ... |
PMC4625864 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Lampalizumab Administered Intravitreally to Patients With Geographic Atrophy | Population Pharmacokinetics and Pharmacodynamics of Lampalizumab Administered Intravitreally to Patients With Geographic Atrophy Abstract Abstract Intravitreally administered lampalizumab is an investigational complement inhibitor directed against complement factor D (CFD) for the treatment of geographic atrophy (GA) s... |
PMC3291529 | core_pubmed_pmc | Living on Three Time Scales: The Dynamics of Plasma Cell and Antibody Populations Illustrated for Hepatitis A Virus | Living on Three Time Scales: The Dynamics of Plasma Cell and Antibody Populations Illustrated for Hepatitis A Virus Abstract Understanding the mechanisms involved in long-term persistence of humoral immunity after natural infection or vaccination is challenging and crucial for further research in immunology, vaccine de... |
PMC6849292 | core_pubmed_pmc | Sedative and hypnotic effects of compound Anshen essential oil inhalation for insomnia | Sedative and hypnotic effects of compound Anshen essential oil inhalation for insomnia Abstract Backgrounds The chemical composition of many essential oils indicates that they have sedative and hypnotic effects, but there is still a lack of systematic studies on the sedative and hypnotic effects of essential oils. In a... |
PMC8538957 | core_pubmed_pmc | A Novel Method for Predicting the Human Inherent Clearance and Its Application in the Study of the Pharmacokinetics and Drug–Drug Interaction between Azidothymidine and Fluconazole Mediated by UGT Enzyme | A Novel Method for Predicting the Human Inherent Clearance and Its Application in the Study of the Pharmacokinetics and Drug–Drug Interaction between Azidothymidine and Fluconazole Mediated by UGT Enzyme Abstract In order to improve the benefit–risk ratio of pharmacokinetic (PK) research in the early development of new... |
PMC7764275 | core_pubmed_pmc | In Vivo Targeted Metabolomic Profiling of Prostanit, a Novel Anti-PAD NO-Donating Alprostadil-Based Drug | In Vivo Targeted Metabolomic Profiling of Prostanit, a Novel Anti-PAD NO-Donating Alprostadil-Based Drug Abstract Abstract Prostanit is a novel drug developed for the treatment of peripheral arterial diseases. It consists of a prostaglandin E 1 (PGE 1 ) moiety with two nitric oxide (NO) donor fragments, which provide a... |
PMC11672653 | core_pubmed_pmc | Therapeutic Monitoring of Vancomycin Implemented by Eremomycin ELISA | Therapeutic Monitoring of Vancomycin Implemented by Eremomycin ELISA Abstract Background/Objectives: Due to a narrow therapeutic window, side-effects, toxicities, and individual pharmacokinetics (PK) variability, WHO classifies vancomycin (VCM) as a “watch antibiotic” whose use should be monitored to improve clinical e... |
PMC3594737 | core_pubmed_pmc | Learning from Bacteriophages - Advantages and Limitations of Phage and Phage-Encoded Protein Applications | Learning from Bacteriophages - Advantages and Limitations of Phage and Phage-Encoded Protein Applications Abstract Abstract The emergence of bacteria resistance to most of the currently available antibiotics has become a critical therapeutic problem. The bacteria causing both hospital and community-acquired infections ... |
PMC6175224 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Oral Propranolol in Pediatric Patients With Infantile Hemangioma | Population Pharmacokinetics and Pharmacodynamics of Oral Propranolol in Pediatric Patients With Infantile Hemangioma Abstract Abstract This study aimed to characterize the population pharmacokinetics and exposure‐response relationship of propranolol (Hemangiol ® Syrup for Pediatric) in infants with infantile hemangioma... |
PMC7849180 | core_pubmed_pmc | A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose, Multiple Ascending Dose and Food Effect Study to Evaluate the Tolerance, Pharmacokinetics of Jaktinib, a New Selective Janus Kinase Inhibitor in Healthy Chinese Volunteers | A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose, Multiple Ascending Dose and Food Effect Study to Evaluate the Tolerance, Pharmacokinetics of Jaktinib, a New Selective Janus Kinase Inhibitor in Healthy Chinese Volunteers Abstract Background: Jaktinib is a novel selective janus kinase 1/2 ... |
PMC5363590 | core_pubmed_pmc | Polymeric nanoparticle-docetaxel for the treatment of advanced solid tumors: phase I clinical trial and preclinical data from an orthotopic pancreatic cancer model | Polymeric nanoparticle-docetaxel for the treatment of advanced solid tumors: phase I clinical trial and preclinical data from an orthotopic pancreatic cancer model Abstract We assessed the efficacy of the polymeric nanoparticle containing docetaxel (PNP-DTX) in preclinical mouse models and determined the maximum tolera... |
PMC11609745 | core_pubmed_pmc | Effects of frequently prescribed antiseizure medications on motor vehicle driving performance: Narrative review based on a tiered approach for the assessment of clinically meaningful driving impairment in the Ministry of Health, Labour, and Welfare guideline | Effects of frequently prescribed antiseizure medications on motor vehicle driving performance: Narrative review based on a tiered approach for the assessment of clinically meaningful driving impairment in the Ministry of Health, Labour, and Welfare guideline Abstract Abstract Patients with epilepsy often require long‐t... |
PMC3581152 | core_pubmed_pmc | Amikacin Population Pharmacokinetics in Critically Ill Kuwaiti Patients | Amikacin Population Pharmacokinetics in Critically Ill Kuwaiti Patients Abstract Abstract Amikacin pharmacokinetic data in Kuwaiti (Arab) intensive care unit (ICU) patients are lacking. Fairly sparse serum amikacin peak and trough concentrations data were obtained from adult Kuwaiti ICU patients. The data were analysed... |
PMC7075646 | core_pubmed_pmc | Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors | Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors Abstract Abstract The hexameric α-helical coiled-coil formed between the C-terminal and N-terminal heptad repeat (CHR and NHR) regions of class I viral fusion proteins plays a... |
PMC12907681 | core_pubmed_pmc | Induced-proximity therapeutics for targeted protein and RNA degradation: An organic chemistry Perspective-A review | Induced-proximity therapeutics for targeted protein and RNA degradation: An organic chemistry Perspective-A review Abstract Induced-proximity therapeutics have emerged as a transformative paradigm in chemical biology and drug discovery, enabling selective control of cellular processes beyond conventional inhibitors. Be... |
PMC6063740 | core_pubmed_pmc | Application of PBPK Modeling and Virtual Clinical Study Approaches to Predict the Outcomes of CYP2D6 Genotype‐Guided Dosing of Tamoxifen | Application of PBPK Modeling and Virtual Clinical Study Approaches to Predict the Outcomes of CYP2D6 Genotype‐Guided Dosing of Tamoxifen Abstract Abstract The Tamoxifen Response by CYP2D6 Genotype‐based Treatment‐1 (TARGET‐1) study ( n = 180) was conducted from 2012–2017 in Japan to determine the efficacy of tamoxifen ... |
PMC3405224 | core_pubmed_pmc | Sorafenib in advanced melanoma: a critical role for pharmacokinetics? | Sorafenib in advanced melanoma: a critical role for pharmacokinetics? Abstract Abstract Background: Inter-patient pharmacokinetic variability can lead to suboptimal drug exposure, and therefore might impact the efficacy of sorafenib. This study reports long-term pharmacokinetic monitoring of patients treated with soraf... |
PMC10209389 | core_pubmed_pmc | The Fragile Patient: Considerations in the Management of Invasive Mould Infections (IMIs) in India | The Fragile Patient: Considerations in the Management of Invasive Mould Infections (IMIs) in India Abstract Abstract Invasive mould infections (IMIs), which are mostly caused by Aspergillus spp. and Mucormycetes , are opportunistic infections that impose a substantial threat to patients who are considered to be ‘fragil... |
PMC7119000 | core_pubmed_pmc | Effect of chito-oligosaccharide on the oral absorptions of phenolic acids of Flos Lonicerae extract | Effect of chito-oligosaccharide on the oral absorptions of phenolic acids of Flos Lonicerae extract Abstract Phenolic acids, the main active ingredients in Flos Lonicerae extract possess strong antibacterial, antioxidant and antiviral effects, and their contents was higher largely than that of other ingredients such as... |
PMC7356390 | core_pubmed_pmc | Dehydrozingerone, a Curcumin Analog, as a Potential Anti-Prostate Cancer Inhibitor In Vitro and In Vivo | Dehydrozingerone, a Curcumin Analog, as a Potential Anti-Prostate Cancer Inhibitor In Vitro and In Vivo Abstract Abstract Curcumin (Cur) exhibits biological activities that support its candidacy for cancer treatment. However, there are limitations to its pharmacological effects, such as poor solubility and bioavailabil... |
PMC5856887 | core_pubmed_pmc | Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug–Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers | Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug–Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers Abstract Background Guanfacine extended-release (GXR) is an orally administered, non-stimul... |
PMC9985425 | core_pubmed_pmc | A Phase 1, Multicenter, Open-Label Study to Evaluate the Pharmacokinetics of Iberdomide in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared with Healthy Subjects | A Phase 1, Multicenter, Open-Label Study to Evaluate the Pharmacokinetics of Iberdomide in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared with Healthy Subjects Abstract Introduction Iberdomide, a novel cereblon modulator (CELMoD ® ), is currently under clinical investigation for hematology indicati... |
PMC7809008 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacogenetic Analysis of Mitotane in Patients with Adrenocortical Carcinoma: Towards Individualized Dosing | Population Pharmacokinetic and Pharmacogenetic Analysis of Mitotane in Patients with Adrenocortical Carcinoma: Towards Individualized Dosing Abstract Background Mitotane is the only approved treatment for patients with adrenocortical carcinoma (ACC). A better explanation for the variability in the pharmacokinetics (PK)... |
PMC12156807 | core_pubmed_pmc | The Chemical Composition, Pharmacological Activity, Quality Control, Toxicity, and Pharmacokinetics of the Genus Clinopodium L. | The Chemical Composition, Pharmacological Activity, Quality Control, Toxicity, and Pharmacokinetics of the Genus Clinopodium L. Abstract The genus Clinopodium L. (Lamiaceae) comprises perennial herbaceous plants known for their diverse pharmacological properties. Clinically, these plants are mainly used for the treatme... |
PMC3357105 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Tamoxifen and its Metabolites in Women of Different CYP2D6 Phenotypes Provides New Insight into the Tamoxifen Mass Balance | Physiologically Based Pharmacokinetic Modeling of Tamoxifen and its Metabolites in Women of Different CYP2D6 Phenotypes Provides New Insight into the Tamoxifen Mass Balance Abstract Abstract Tamoxifen is a first-line endocrine agent in the mechanism-based treatment of estrogen receptor positive (ER + ) mammary carcinom... |
PMC7657519 | core_pubmed_pmc | Measurement of fasted state gastric antral motility before and after a standard bioavailability and bioequivalence 240 mL drink of water: Validation of MRI method against concomitant perfused manometry in healthy participants | Measurement of fasted state gastric antral motility before and after a standard bioavailability and bioequivalence 240 mL drink of water: Validation of MRI method against concomitant perfused manometry in healthy participants Abstract Abstract Objective The gastrointestinal environment in which drug products need to di... |
PMC4917797 | core_pubmed_pmc | A randomized phase l pharmacokinetic study comparing SB4 and etanercept reference product (Enbrel®) in healthy subjects | A randomized phase l pharmacokinetic study comparing SB4 and etanercept reference product (Enbrel®) in healthy subjects Abstract Abstract Aims SB4 has been developed as a biosimilar of etanercept. The primary objective of the present study was to demonstrate the pharmacokinetic (PK) equivalence between SB4 and European... |
PMC6321354 | core_pubmed_pmc | Prospects and Challenges of Phospholipid-Based Prodrugs | Prospects and Challenges of Phospholipid-Based Prodrugs Abstract Nowadays, the prodrug approach is used already at the early stages of drug development. Lipidic prodrug approach is a growing field for improving a number of drug properties/delivery/therapy aspects, and can offer solutions for various unmet needs. This a... |
PMC3997483 | core_pubmed_pmc | Aminostyrylbenzofuran Directly Reduces Oligomeric Amyloid-β and Reverses Cognitive Deficits in Alzheimer Transgenic Mice | Aminostyrylbenzofuran Directly Reduces Oligomeric Amyloid-β and Reverses Cognitive Deficits in Alzheimer Transgenic Mice Abstract Alzheimer's disease is an irreversible neurodegenerative disorder that is characterized by the abnormal aggregation of amyloid-β into neurotoxic oligomers and plaques. Although many disease-... |
PMC9315275 | core_pubmed_pmc | Sedation level with midazolam: A pediatric surgery approach | Sedation level with midazolam: A pediatric surgery approach Abstract Midazolam (MDZ) is a short-acting benzodiazepine that is widely used to induce and maintain general anesthesia during diagnostic and therapeutic procedures in pediatric patients due to its sedative properties. The aim of this study was to perform a sy... |
PMC10539020 | core_pubmed_pmc | A Phase I/II Trial of Oral SRA737 (a Chk1 Inhibitor) Given in Combination with Low-Dose Gemcitabine in Patients with Advanced Cancer | A Phase I/II Trial of Oral SRA737 (a Chk1 Inhibitor) Given in Combination with Low-Dose Gemcitabine in Patients with Advanced Cancer Abstract Abstract Purpose: This was a Phase I/II trial of the novel checkpoint kinase 1 (Chk1) inhibitor SRA737 given in combination with gemcitabine. Its objectives were to establish the... |
PMC6110634 | core_pubmed_pmc | Preparation and characterization of pH-sensitive nanoparticles of budesonide for the treatment of ulcerative colitis | Preparation and characterization of pH-sensitive nanoparticles of budesonide for the treatment of ulcerative colitis Abstract Abstract Objective The aim of this study was to develop pH sensitive nanoparticles of budesonide for the treatment of ulcerative colitis. Methods The NPs system was characterized by the transmis... |
PMC6566491 | core_pubmed_pmc | Effects of Ginkgo leaf tablets on the pharmacokinetics of atovastatin in rats | Effects of Ginkgo leaf tablets on the pharmacokinetics of atovastatin in rats Abstract Abstract Context: Ginkgo leaf tablets (GLT), an effective traditional Chinese multi-herbal formula, are often combined with atorvastatin calcium (AC) for treating coronary heart disease in clinic. Objective: This study investigated t... |
PMC3034722 | core_pubmed_pmc | Anti-infliximab antibodies are already detectable in most patients with rheumatoid arthritis halfway through an infusioncycle: an open-label pharmacokinetic cohort study | Anti-infliximab antibodies are already detectable in most patients with rheumatoid arthritis halfway through an infusioncycle: an open-label pharmacokinetic cohort study Abstract Background This study in patients with rheumatoid arthritis (RA) treated with infliximab describes prospectively the course of (anti)inflixim... |
PMC11743120 | core_pubmed_pmc | High-throughput screening of natural antiviral drug candidates against white spot syndrome virus targeting VP28 in Penaeus monodon : Computational drug design approaches | High-throughput screening of natural antiviral drug candidates against white spot syndrome virus targeting VP28 in Penaeus monodon : Computational drug design approaches Abstract Highlights • A virtual library of 187 bioactive constituents from Azadirachta indica and Bacopa monnieri was created to fight WSSV. • Identif... |
PMC10946580 | core_pubmed_pmc | In silico evaluation of a beta‐lactam dosing guideline among adults with serious infections | In silico evaluation of a beta‐lactam dosing guideline among adults with serious infections Abstract Abstract Study Objective The aim of this study was to compare the achievement of therapeutic pharmacokinetic–pharmacodynamic (PK‐PD) exposure targets for beta‐lactam antibiotics using product information dosing or guide... |
PMC12518504 | core_pubmed_pmc | Pharmacokinetics and Safety of Fixed‐Dose Versus Separate Enavogliflozin/Gemigliptin Combinations, and Food Effect on Enavogliflozin in Healthy Korean Subjects | Pharmacokinetics and Safety of Fixed‐Dose Versus Separate Enavogliflozin/Gemigliptin Combinations, and Food Effect on Enavogliflozin in Healthy Korean Subjects Abstract ABSTRACT Envlo (enavogliflozin) 0.3 mg, an SGLT2 inhibitor, was approved in Korea in 2022 for glycemic control in type 2 diabetes (T2DM). This study ev... |
PMC8538714 | core_pubmed_pmc | Voriconazole Pharmacokinetics Are Not Altered in Critically Ill Patients with Acute-on-Chronic Liver Failure and Continuous Renal Replacement Therapy: An Observational Study | Voriconazole Pharmacokinetics Are Not Altered in Critically Ill Patients with Acute-on-Chronic Liver Failure and Continuous Renal Replacement Therapy: An Observational Study Abstract Infection and sepsis are a main cause of acute-on-chronic liver failure (ACLF). Besides bacteria, molds play a role. Voriconazole (VRC) i... |
PMC11537163 | core_pubmed_pmc | Penetration Enhancer-Free Mixed Micelles for Improving Eprinomectin Transdermal c Efficiency in Animal Parasitic Infections Therapy | Penetration Enhancer-Free Mixed Micelles for Improving Eprinomectin Transdermal c Efficiency in Animal Parasitic Infections Therapy Abstract Abstract Introduction Eprinomectin offers promise against parasitic infections. This study develops Eprinomectin (EPR) mixed micelles for transdermal delivery, aiming to enhance e... |
PMC4494180 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males | Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males Abstract Abstract Lesinurad is a selective uric acid reabsorption inhibitor under investigation for the treatment of gout. Single and multiple ascending dose studies were conducted to evalua... |
PMC11905876 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Certepetide in Human Subjects With Metastatic Pancreatic Ductal Adenocarcinoma | Population Pharmacokinetic Modeling of Certepetide in Human Subjects With Metastatic Pancreatic Ductal Adenocarcinoma Abstract Abstract Certepetide (aka LSTA1 and CEND‐1) is a novel cyclic tumor‐targeting internalizing arginyl glycylaspartic acid peptide being developed to treat solid tumors. Certepetide is designed to... |
PMC8193675 | core_pubmed_pmc | Population Pharmacokinetics of Ropeginterferon Alfa-2b: A Comparison Between Healthy Caucasian and Chinese Subjects | Population Pharmacokinetics of Ropeginterferon Alfa-2b: A Comparison Between Healthy Caucasian and Chinese Subjects Abstract Objective: To develop a population pharmacokinetic (PK) model for ropeginterferon alfa-2b and to compare its PK properties between Caucasian and Chinese populations. Methods: A population PK mode... |
PMC12389225 | core_pubmed_pmc | Phytochemical Modulators of Nociception: A Review of Cannabis Terpenes in Chronic Pain Syndromes | Phytochemical Modulators of Nociception: A Review of Cannabis Terpenes in Chronic Pain Syndromes Abstract Abstract Cannabis sativa L. is a phytochemically rich plant with therapeutic potential across various clinical domains, including pain, inflammation, and neurological disorders. Among its constituents, terpenes are... |
PMC5011932 | core_pubmed_pmc | Comparative pharmacokinetics and pharmacodynamics of intravenous artelinate versus artesunate in uncomplicated Plasmodium coatneyi -infected rhesus monkey model | Comparative pharmacokinetics and pharmacodynamics of intravenous artelinate versus artesunate in uncomplicated Plasmodium coatneyi -infected rhesus monkey model Abstract Abstract Background The US Army designed artelinate/lysine salt (AL) to overcome the instability of sodium artesunate in aqueous solution (AS). To sel... |
PMC9101974 | core_pubmed_pmc | General Purpose Pharmacokinetic-Pharmacodynamic Models for Target-Controlled Infusion of Anaesthetic Drugs: A Narrative Review | General Purpose Pharmacokinetic-Pharmacodynamic Models for Target-Controlled Infusion of Anaesthetic Drugs: A Narrative Review Abstract Target controlled infusion (TCI) is a clinically-available and widely-used computer-controlled method of drug administration, adjusting the drug titration towards user selected plasma-... |
PMC4766526 | core_pubmed_pmc | Histopathological nerve and skeletal muscle changes in rats subjected to persistent insulin-induced hypoglycemia | Histopathological nerve and skeletal muscle changes in rats subjected to persistent insulin-induced hypoglycemia Abstract Abstract New insulin analogues with a longer duration of action and a flatter pharmacodynamic profile are developed to improve convenience and safety for diabetic patients. During the nonclinical de... |
PMC5828935 | core_pubmed_pmc | Individualized treatment strategies for hyperuricemia informed by a semi‐mechanistic exposure‐response model of uric acid dynamics | Individualized treatment strategies for hyperuricemia informed by a semi‐mechanistic exposure‐response model of uric acid dynamics Abstract Abstract To provide insight into pharmacological treatment of hyperuricemia we developed a semi‐mechanistic, dynamical model of uric acid (UA) disposition in human. Our model repre... |
PMC9213336 | core_pubmed_pmc | Population kinetics of homoarginine and optimized supplementation for cardiovascular risk reduction | Population kinetics of homoarginine and optimized supplementation for cardiovascular risk reduction Abstract Abstract Homoarginine is an endogenous amino acid whose levels are reduced in patients with renal, cardio- and cerebrovascular disease. Moreover, low homoarginine concentrations independently predict morbidity a... |
PMC8748341 | core_pubmed_pmc | In silico evaluation of limited sampling strategies for individualized dosing of extended half-life factor IX concentrates in hemophilia B patients | In silico evaluation of limited sampling strategies for individualized dosing of extended half-life factor IX concentrates in hemophilia B patients Abstract Purpose Hemophilia B is a bleeding disorder, caused by a factor IX (FIX) deficiency. Recently, FIX concentrates with extended half-life (EHL) have become available... |
PMC7718230 | core_pubmed_pmc | Association of clozapine-related metabolic disturbances with CYP3A4 expression in patients with schizophrenia | Association of clozapine-related metabolic disturbances with CYP3A4 expression in patients with schizophrenia Abstract Abstract Clozapine is effective in treatment-resistant schizophrenia; however, adverse effects often result in discontinuation of clozapine therapy. Many of the side-effects are associated with pharmac... |
PMC5136565 | core_pubmed_pmc | Parameter Identifiability of Fundamental Pharmacodynamic Models | Parameter Identifiability of Fundamental Pharmacodynamic Models Abstract Issues of parameter identifiability of routinely used pharmacodynamics models are considered in this paper. The structural identifiability of 16 commonly applied pharmacodynamic model structures was analyzed analytically, using the input-output ap... |
PMC7529628 | core_pubmed_pmc | Practical Challenges—Use of Paracetamol in Children and Youth Who are Overweight or Obese: A Narrative Review | Practical Challenges—Use of Paracetamol in Children and Youth Who are Overweight or Obese: A Narrative Review Abstract Abstract Worldwide, > 380 million children and adolescents are overweight or obese, including 41 million children aged < 5 years. Obesity can change the pharmacokinetic properties of drugs by altering ... |
PMC12208167 | core_pubmed_pmc | Binding of therapeutic Fc-fused factor VIII to the neonatal Fc receptor at neutral pH associates with poor half-life extension | Binding of therapeutic Fc-fused factor VIII to the neonatal Fc receptor at neutral pH associates with poor half-life extension Abstract Fusion of therapeutic proteins to the Fc fragment of human immunoglobulin (Ig) G1 promotes their neonatal Fc receptor (FcRn)-mediated recycling and subsequent extension in circulating ... |
PMC3414220 | core_pubmed_pmc | Cyclic RGD peptide-modified liposomal drug delivery system: enhanced cellular uptake in vitro and improved pharmacokinetics in rats | Cyclic RGD peptide-modified liposomal drug delivery system: enhanced cellular uptake in vitro and improved pharmacokinetics in rats Abstract Abstract Background Integrins α v β 3 and α v β 5 , both of which specifically recognize the Arg-Gly-Asp (RGD) motif, are overexpressed on many solid tumors and in tumor neovascul... |
PMC4124105 | core_pubmed_pmc | Effects of combined netupitant and palonosetron (NEPA), a cancer supportive care antiemetic, on the ECG of healthy subjects: an ICH E14 thorough QT trial | Effects of combined netupitant and palonosetron (NEPA), a cancer supportive care antiemetic, on the ECG of healthy subjects: an ICH E14 thorough QT trial Abstract Abstract Chemotherapy-induced nausea and vomiting is ranked among the worst side effects of chemotherapy. NEPA is an oral fixed-dose combination antiemetic u... |
PMC5394393 | core_pubmed_pmc | Salvia miltiorrhiza Roots against Cardiovascular Disease: Consideration of Herb-Drug Interactions | Salvia miltiorrhiza Roots against Cardiovascular Disease: Consideration of Herb-Drug Interactions Abstract Salvia miltiorrhiza root (Danshen) is widely used in Asia for its cardiovascular benefits and contains both hydrophilic phenolic acids and lipophilic tanshinones, which are believed to be responsible for its thera... |
PMC5672994 | core_pubmed_pmc | Radiochemistry and Preclinical PET Imaging of 68 Ga-Desferrioxamine Radiotracers Targeting Prostate-Specific Membrane Antigen | Radiochemistry and Preclinical PET Imaging of 68 Ga-Desferrioxamine Radiotracers Targeting Prostate-Specific Membrane Antigen Abstract Radiotracers incorporating the urea-based Glu-NH-C(O)-NH-Lys group have gained prominence due to their role in targeting prostate-specific membrane antigen (PSMA)—a clinical biomarker o... |
PMC8952231 | core_pubmed_pmc | Pharmacokinetics of a Fixed-Dose Combination Product of Dapagliflozin and Linagliptin and Its Comparison with Co-Administration of Individual Tablets in Healthy Humans | Pharmacokinetics of a Fixed-Dose Combination Product of Dapagliflozin and Linagliptin and Its Comparison with Co-Administration of Individual Tablets in Healthy Humans Abstract Dapagliflozin, a selective sodium–glucose co-transporter-2 inhibitor, and linagliptin, a competitive, reversible dipeptidyl peptidase-4 inhibit... |
PMC10752084 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of candesartan to predict the exposure in hepatic and renal impairment and elderly populations | Physiologically based pharmacokinetic modeling of candesartan to predict the exposure in hepatic and renal impairment and elderly populations Abstract Background: Candesartan cilexetil is a widely used angiotensin II receptor blocker with minimal adverse effects and high tolerability for the treatment of hypertension. ... |
PMC9888309 | core_pubmed_pmc | Prediction of Busulfan Clearance by Predose Plasma Metabolomic Profiling | Prediction of Busulfan Clearance by Predose Plasma Metabolomic Profiling Abstract Abstract Intravenous busulfan doses are often personalized to a target plasma exposure (targeted busulfan) using an individual’s busulfan clearance (BuCL). We evaluated whether BuCL could be predicted by a predose plasma panel of 841 endo... |
PMC6586554 | core_pubmed_pmc | Strategies for using mathematical modeling approaches to design and interpret multi-organ microphysiological systems (MPS) | Strategies for using mathematical modeling approaches to design and interpret multi-organ microphysiological systems (MPS) Abstract Abstract Recent advances in organ-on-a-chip technology have resulted in numerous examples of microscale systems that faithfully mimic the physiology and pathology of human organs and disea... |
PMC10092624 | core_pubmed_pmc | A single‐centre, open‐label, single‐arm, fixed‐sequence pharmacokinetic study of SHR3680 on repaglinide and bupropion in prostate cancer patients | A single‐centre, open‐label, single‐arm, fixed‐sequence pharmacokinetic study of SHR3680 on repaglinide and bupropion in prostate cancer patients Abstract Abstract To evaluate the pharmacokinetic effects of SHR3680 on repaglinide and bupropion and its metabolite hydroxybupropion. Methods A single‐centre, open‐label, si... |
PMC4365273 | core_pubmed_pmc | A pharmacokinetic binding model for bevacizumab and VEGF 165 in colorectal cancer patients | A pharmacokinetic binding model for bevacizumab and VEGF 165 in colorectal cancer patients Abstract Abstract Purpose To characterize the population pharmacokinetics of bevacizumab, its binding properties to VEGF 165 and the effect of demographic data and VEGF-A polymorphisms on the interplay between bevacizumab serum p... |
PMC11064628 | core_pubmed_pmc | Comparison of lumefantrine, mefloquine, and piperaquine concentrations between capillary plasma and venous plasma samples in pregnant women with uncomplicated falciparum and vivax malaria | Comparison of lumefantrine, mefloquine, and piperaquine concentrations between capillary plasma and venous plasma samples in pregnant women with uncomplicated falciparum and vivax malaria Abstract ABSTRACT Capillary samples offer practical benefits compared with venous samples for the measurement of drug concentrations... |
PMC9026289 | core_pubmed_pmc | The Role of SLC22A1 and Genomic Ancestry on Toxicity during Treatment in Children with Acute Lymphoblastic Leukemia of the Amazon Region | The Role of SLC22A1 and Genomic Ancestry on Toxicity during Treatment in Children with Acute Lymphoblastic Leukemia of the Amazon Region Abstract Abstract In Brazil, Acute lymphoid leukemia (ALL) is the leading cause of cancer deaths in children and adolescents. Treatment toxicity is one of the reasons for stopping che... |
PMC6967289 | core_pubmed_pmc | A Phase 1b Study of Vismodegib with Pirfenidone in Patients with Idiopathic Pulmonary Fibrosis | A Phase 1b Study of Vismodegib with Pirfenidone in Patients with Idiopathic Pulmonary Fibrosis Abstract Introduction Components of the hedgehog signaling pathway are upregulated in patients with idiopathic pulmonary fibrosis (IPF). Vismodegib, a small-molecule inhibitor of hedgehog signaling, when used in combination w... |
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