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PMC7938611 | core_pubmed_pmc | Extended half‐life factor VIII concentrates in adults with hemophilia A: Comparative pharmacokinetics of two products | Extended half‐life factor VIII concentrates in adults with hemophilia A: Comparative pharmacokinetics of two products Abstract Abstract Background The use of pharmacokinetic (PK) studies to help design personalized prophylaxis regimens for factor VIII (FVIII) concentrate in individuals with hemophilia A has been recogn... |
PMC12967222 | core_pubmed_pmc | New Adrenaline Devices for Treating Anaphylaxis: Results of a Joint Survey From the European Anaphylaxis Registry and the Allergy‐Vigilance Network | New Adrenaline Devices for Treating Anaphylaxis: Results of a Joint Survey From the European Anaphylaxis Registry and the Allergy‐Vigilance Network Abstract ABSTRACT Background Adrenaline auto‐injectors (AAI) are underused to treat anaphylaxis. New adrenaline devices are currently under investigation or have been recen... |
PMC7837237 | core_pubmed_pmc | Gamma-hydroxybutyrate Abuse: Pharmacology and Poisoning and Withdrawal Management | Gamma-hydroxybutyrate Abuse: Pharmacology and Poisoning and Withdrawal Management Abstract Abstract Gamma-hydroxybutyrate (GHB) is a central nervous system depressant primarily used as a recreational drug of abuse, but also for the treatment of narcolepsy with cataplexy in adult patients and as an adjuvant for control ... |
PMC7822530 | core_pubmed_pmc | The potential of microdialysis to estimate rifampicin concentrations in the lung of guinea pigs | The potential of microdialysis to estimate rifampicin concentrations in the lung of guinea pigs Abstract Abstract Optimised pre-clinical models are required for TB drug development to better predict the pharmacokinetics of anti-tuberculosis (anti-TB) drugs to shorten the time taken for novel drugs and combinations to b... |
PMC12001264 | core_pubmed_pmc | Tutorial on Conditional Simulations With a Tumor Size‐Overall Survival Model to Support Oncology Drug Development | Tutorial on Conditional Simulations With a Tumor Size‐Overall Survival Model to Support Oncology Drug Development Abstract ABSTRACT The gold standard for regulatory approval in oncology is overall survival (OS). Because OS data are initially limited, early drug development decisions are often based on early efficacy en... |
PMC4735354 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Integration and Modeling of Enrofloxacin in Swine for Escherichia coli | Pharmacokinetic and Pharmacodynamic Integration and Modeling of Enrofloxacin in Swine for Escherichia coli Abstract The aim of this study was to optimize the dose regimens of enrofloxacin to reduce the development of fluoroquinolone resistance in Escherichia coli ( E. coli) using pharmacokinetic/pharmacodynamic (PK/PD)... |
PMC7998926 | core_pubmed_pmc | Formulation, Stability, Pharmacokinetic, and Modeling Studies for Tests of Synergistic Combinations of Orally Available Approved Drugs against Ebola Virus In Vivo | Formulation, Stability, Pharmacokinetic, and Modeling Studies for Tests of Synergistic Combinations of Orally Available Approved Drugs against Ebola Virus In Vivo Abstract Outbreaks of Ebola ebolavirus (EBOV) have been associated with high morbidity and mortality. Milestones have been reached recently in the management... |
PMC3914806 | core_pubmed_pmc | Administration of a Probiotic Can Change Drug Pharmacokinetics: Effect of E. coli Nissle 1917 on Amidarone Absorption in Rats | Administration of a Probiotic Can Change Drug Pharmacokinetics: Effect of E. coli Nissle 1917 on Amidarone Absorption in Rats Abstract The growing interest in the composition and effects of microbiota raised the question how drug pharmacokinetics could be influenced by concomitant application of probiotics. The aim of ... |
PMC12084189 | core_pubmed_pmc | Clinical Pharmacokinetics and Safety of Orally Administered VH4011499, a New HIV-1 Capsid Inhibitor, in Adults Without HIV | Clinical Pharmacokinetics and Safety of Orally Administered VH4011499, a New HIV-1 Capsid Inhibitor, in Adults Without HIV Abstract Introduction This first-time-in-human study describes the pharmacokinetics, drug–drug interaction potential, and safety of VH4011499 (VH-499), a new HIV-1 capsid inhibitor. Methods This do... |
PMC11396525 | core_pubmed_pmc | Pharmacokinetics of Efmoroctocog alfa by Two-Compartment Model Highlights Hemophilia A Patients with Biphasic Decay, Long Mean Residence Time, and Beta Half-Life | Pharmacokinetics of Efmoroctocog alfa by Two-Compartment Model Highlights Hemophilia A Patients with Biphasic Decay, Long Mean Residence Time, and Beta Half-Life Abstract Abstract Background/Objectives: A compartmental pharmacokinetics (PK) analysis of new extended half-life FVIII concentrates has never been performed ... |
PMC9306949 | core_pubmed_pmc | Pharmacokinetics and Macrophage Inhibitory Cytokine‐1 Pharmacodynamics of the Murine Double Minute 2 Inhibitor, Navtemadlin (KRT‐232) in Fed and Fasted Healthy Subjects | Pharmacokinetics and Macrophage Inhibitory Cytokine‐1 Pharmacodynamics of the Murine Double Minute 2 Inhibitor, Navtemadlin (KRT‐232) in Fed and Fasted Healthy Subjects Abstract Abstract This single 60‐mg dose, 4‐period crossover study assessed the effect of food and formulation change on navtemadlin (KRT‐232) pharmaco... |
PMC3363964 | core_pubmed_pmc | The Impact of Caesarean Delivery on Paracetamol and Ketorolac Pharmacokinetics: A Paired Analysis | The Impact of Caesarean Delivery on Paracetamol and Ketorolac Pharmacokinetics: A Paired Analysis Abstract Abstract Pharmacokinetics is a first, but essential step to improve population-tailored postoperative analgesia, also after Caesarean delivery. We therefore aimed to quantify the impact of caesarean delivery on th... |
PMC11579075 | core_pubmed_pmc | A quantitative modeling framework to understand the physiology of the hypothalamic-pituitary-adrenal axis and interaction with cortisol replacement therapy | A quantitative modeling framework to understand the physiology of the hypothalamic-pituitary-adrenal axis and interaction with cortisol replacement therapy Abstract Congenital adrenal hyperplasia (CAH) is characterized by impaired adrenal cortisol production. Hydrocortisone (synthetic cortisol) is the drug-of-choice fo... |
PMC12520790 | core_pubmed_pmc | Investigating the consequences of the mating system for drug resistance evolution in Caenorhabditis elegans | Investigating the consequences of the mating system for drug resistance evolution in Caenorhabditis elegans Abstract Abstract The rise of anthelmintic-resistant strains in livestock threatens both animal and human health. Understanding the factors influencing anthelmintic resistance is crucial to mitigate the threat po... |
PMC9257893 | core_pubmed_pmc | Effect of cytochrome P450 inhibition on toxicity of diclofenac in chickens: Unravelling toxicity in Gyps vultures | Effect of cytochrome P450 inhibition on toxicity of diclofenac in chickens: Unravelling toxicity in Gyps vultures Abstract Diclofenac was responsible for the decimation of Gyps vulture species on the Indian subcontinent during the 1980s and 1990s. Gyps vultures are extremely sensitive (the lethal dose 50 [LD 50 ] ~ 0.1... |
PMC11905878 | core_pubmed_pmc | Phase 1 Mass Balance Study of Pizuglanstat: An Investigational Hematopoietic Prostaglandin D Synthase Inhibitor | Phase 1 Mass Balance Study of Pizuglanstat: An Investigational Hematopoietic Prostaglandin D Synthase Inhibitor Abstract Abstract Pizuglanstat is a novel hematopoietic prostaglandin D synthase inhibitor and investigational treatment for Duchenne muscular dystrophy. This Phase 1 mass balance study aimed to characterize ... |
PMC7037993 | core_pubmed_pmc | Radiosynthesis of [ 18 F]-Labelled Pro-Nucleotides (ProTides) | Radiosynthesis of [ 18 F]-Labelled Pro-Nucleotides (ProTides) Abstract Phosphoramidate pro-nucleotides (ProTides) have revolutionized the field of anti-viral and anti-cancer nucleoside therapy, overcoming the major limitations of nucleoside therapies and achieving clinical and commercial success. Despite the translatio... |
PMC10387801 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of an anti-LAG-3 antibody SHR-1802 in patients with advanced solid tumors: a phase I dose-escalation and dose-expansion study | Safety, tolerability, and pharmacokinetics of an anti-LAG-3 antibody SHR-1802 in patients with advanced solid tumors: a phase I dose-escalation and dose-expansion study Abstract Background: Lymphocyte-activation gene 3 (LAG-3), a checkpoint molecule contributing to immune suppressive microenvironment, is regarded as a ... |
PMC8420016 | core_pubmed_pmc | Pharmacokinetics and diuretic effect of furosemide after single intravenous, oral tablet, and newly developed oral disintegrating film administration in healthy beagle dogs | Pharmacokinetics and diuretic effect of furosemide after single intravenous, oral tablet, and newly developed oral disintegrating film administration in healthy beagle dogs Abstract Background Furosemide, a diuretic that acts on the loop of Henle, is commonly used to treat congestive heart failure in veterinary medicin... |
PMC12963678 | core_pubmed_pmc | Next Generation DNA Damage Response Inhibitors: Harnessing Nanocarriers and Tumor Microenvironment for Precision Cancer Therapy | Next Generation DNA Damage Response Inhibitors: Harnessing Nanocarriers and Tumor Microenvironment for Precision Cancer Therapy Abstract Abstract Tumor survival, genomic stability, and therapy resistance are dictated by the DNA damage response (DDR). Although poly (ADP-ribose) polymerase (PARP) inhibitors have establis... |
PMC11283786 | core_pubmed_pmc | Highly Drug-Loaded Nanoaggregate Microparticles for Pulmonary Delivery of Cyclosporin A | Highly Drug-Loaded Nanoaggregate Microparticles for Pulmonary Delivery of Cyclosporin A Abstract Introduction Nanoparticles have the advantages of improving the solubility of poorly water-soluble drugs, facilitating the drug across biological barriers, and reducing macrophage phagocytosis in pulmonary drug delivery. Ho... |
PMC5368402 | core_pubmed_pmc | Selective Blockade of the Ubiquitous Checkpoint Receptor CD47 Is Enabled by Dual-Targeting Bispecific Antibodies | Selective Blockade of the Ubiquitous Checkpoint Receptor CD47 Is Enabled by Dual-Targeting Bispecific Antibodies Abstract Abstract CD47 is a ubiquitously expressed immune checkpoint receptor that is often upregulated in cancer. CD47 interacts with its counter-receptor SIRPα on macrophages and other myeloid cells to inh... |
PMC3603475 | core_pubmed_pmc | A Semi-Mechanistic Metabolism Model of CYP3A Substrates in Pregnancy: Predicting Changes in Midazolam and Nifedipine Pharmacokinetics | A Semi-Mechanistic Metabolism Model of CYP3A Substrates in Pregnancy: Predicting Changes in Midazolam and Nifedipine Pharmacokinetics Abstract Abstract Physiological changes in pregnancy, including changes in body composition and metabolic enzyme activity, can alter drug pharmacokinetics. A semi-mechanistic metabolism ... |
PMC9662946 | core_pubmed_pmc | A Phase I Study Investigating AZD8186, a Potent and Selective Inhibitor of PI3Kβ/δ, in Patients with Advanced Solid Tumors | A Phase I Study Investigating AZD8186, a Potent and Selective Inhibitor of PI3Kβ/δ, in Patients with Advanced Solid Tumors Abstract Abstract Purpose: To characterize safety and tolerability of the selective PI3Kβ inhibitor AZD8186, identify a recommended phase II dose (RP2D), and assess preliminary efficacy in combinat... |
PMC3232088 | core_pubmed_pmc | Development of matrix type transdermal patches of lercanidipine hydrochloride: physicochemical and in-vitro characterization | Development of matrix type transdermal patches of lercanidipine hydrochloride: physicochemical and in-vitro characterization Abstract Background and the purpose of the study Lercanidipine hydrochloride (LRDP) is used in the treatment of hypertension because of its selectivity and specificity on the smooth vascular cell... |
PMC9747120 | core_pubmed_pmc | Muscle velocity recovery cycles as pharmacodynamic biomarker: Effects of mexiletine in a randomized double‐blind placebo‐controlled cross‐over study | Muscle velocity recovery cycles as pharmacodynamic biomarker: Effects of mexiletine in a randomized double‐blind placebo‐controlled cross‐over study Abstract Abstract Measuring muscle velocity recovery cycles (MVRCs) is a method to obtain information on muscle cell excitability, independent of neuromuscular transmissio... |
PMC4541558 | core_pubmed_pmc | Pharmacokinetics and bioavailability study of two ondansetron oral soluble film formulations in fasting healthy male Chinese volunteers | Pharmacokinetics and bioavailability study of two ondansetron oral soluble film formulations in fasting healthy male Chinese volunteers Abstract Abstract Background Ondansetron oral soluble film is designed to be applied on top of the tongue without requiring water to aid dissolution or swallowing, which is especially ... |
PMC11544175 | core_pubmed_pmc | Modeling on in vivo disposition and cellular transportation of RNA lipid nanoparticles via quantum mechanics/physiologically-based pharmacokinetic approaches | Modeling on in vivo disposition and cellular transportation of RNA lipid nanoparticles via quantum mechanics/physiologically-based pharmacokinetic approaches Abstract Abstract The lipid nanoparticle (LNP) has been so far proven as a strongly effective delivery system for mRNA and siRNA. However, the mechanisms of LNP's... |
PMC12511804 | core_pubmed_pmc | Pharmacokinetics and safety of a fixed-dose combination of pregabalin and thioctic acid in healthy volunteers: a randomized, open-label, phase 1 crossover study | Pharmacokinetics and safety of a fixed-dose combination of pregabalin and thioctic acid in healthy volunteers: a randomized, open-label, phase 1 crossover study Abstract Abstract Background Pregabalin (PGB) is a first-line therapy for painful diabetic neuropathy (PDN), but its adverse effects limit use. Thioctic acid, ... |
PMC5042539 | core_pubmed_pmc | An In Silico Knockout Model for Gastrointestinal Absorption Using a Systems Pharmacology Approach - Development and Application for Ketones | An In Silico Knockout Model for Gastrointestinal Absorption Using a Systems Pharmacology Approach - Development and Application for Ketones Abstract Abstract Gastrointestinal absorption and disposition of ketones is complex. Recent work describing the pharmacokinetics (PK) of d -β-hydroxybutyrate (BHB) following oral i... |
PMC11283705 | core_pubmed_pmc | Chemopreventive effect of modified zeng-sheng-ping on oral squamous cell carcinoma by regulating tumor associated macrophages through targeting tnf alpha induced protein 6 | Chemopreventive effect of modified zeng-sheng-ping on oral squamous cell carcinoma by regulating tumor associated macrophages through targeting tnf alpha induced protein 6 Abstract Abstract Background Oral squamous cell carcinoma (OSCC) is the most common malignancy of the head and neck. Zeng-Sheng-Ping, composed of So... |
PMC9354582 | core_pubmed_pmc | Instability Mechanism of Osimertinib in Plasma and a Solving Strategy in the Pharmacokinetics Study | Instability Mechanism of Osimertinib in Plasma and a Solving Strategy in the Pharmacokinetics Study Abstract Abstract Osimertinib is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and a star medication used to treat non-small-cell lung carcinomas (NSCLCs). It has caused broad p... |
PMC11800234 | core_pubmed_pmc | Addressing Ethnicity in the Design and Evaluation of an Educational Intervention on Interindividual Variation in Pharmacokinetics | Addressing Ethnicity in the Design and Evaluation of an Educational Intervention on Interindividual Variation in Pharmacokinetics Abstract ABSTRACT Interindividual variation in pharmacokinetics can occur due to diet, environmental or lifestyle factors, underlying pathology, and gene variants, typically single nucleotid... |
PMC3758456 | core_pubmed_pmc | High prevalence of potential drug interactions affecting mycophenolic acid pharmacokinetics in nonmyeloablative hematopoietic stem cell transplant recipients | High prevalence of potential drug interactions affecting mycophenolic acid pharmacokinetics in nonmyeloablative hematopoietic stem cell transplant recipients Abstract Objective: Mycophenolic acid (MPA) exposure is associated with clinical outcomes in hematopoietic cell transplant (HCT) recipients. Various drug interact... |
PMC10069754 | core_pubmed_pmc | Brief Report: Suboptimal Lopinavir Exposure in Infants on Rifampicin Treatment Receiving Double-dosed or Semisuperboosted Lopinavir/Ritonavir: Time for a Change | Brief Report: Suboptimal Lopinavir Exposure in Infants on Rifampicin Treatment Receiving Double-dosed or Semisuperboosted Lopinavir/Ritonavir: Time for a Change Abstract Supplemental Digital Content is Available in the Text. Key Words: lopinavir, infants, rifampin, HIV, tuberculosis, CYP3A4, drug–drug interaction Backg... |
PMC8764983 | core_pubmed_pmc | Pharmacodynamic and pharmacokinetic interaction of losartan with glimepiride-metformin combination in rats and rabbits | Pharmacodynamic and pharmacokinetic interaction of losartan with glimepiride-metformin combination in rats and rabbits Abstract OBJECTIVES: The presence of comorbidities such as cardiovascular disease, peripheral vascular disease, and chronic renal disease, or and the prevention of these ailments in diabetics, frequent... |
PMC11087525 | core_pubmed_pmc | In-vitro and in-vivo assessment of nirmatrelvir penetration into CSF, central nervous system cells, tissues, and peripheral blood mononuclear cells | In-vitro and in-vivo assessment of nirmatrelvir penetration into CSF, central nervous system cells, tissues, and peripheral blood mononuclear cells Abstract Abstract Three years after SARS-CoV-2 emerged as a global infectious threat, the virus has become endemic. The neurological complications such as depression, anxie... |
PMC4613337 | core_pubmed_pmc | Pharmacogenetics of BCR/ABL Inhibitors in Chronic Myeloid Leukemia | Pharmacogenetics of BCR/ABL Inhibitors in Chronic Myeloid Leukemia Abstract Abstract Chronic myeloid leukemia was the first haematological neoplasia that benefited from a targeted therapy with imatinib nearly 15 years ago. Since then, several studies have investigated the role of genes, their variants ( i.e ., polymorp... |
PMC12783212 | core_pubmed_pmc | Low Target Attainment of Intravenous Cefuroxime in Critically Ill Term Neonates and Children: A Pooled Population Pharmacokinetics Study | Low Target Attainment of Intravenous Cefuroxime in Critically Ill Term Neonates and Children: A Pooled Population Pharmacokinetics Study Abstract Abstract Background and Objective Cefuroxime is a widely prescribed beta-lactam antibiotic, particularly in pediatric cardiac and medical–surgical intensive care units. The a... |
PMC6562844 | core_pubmed_pmc | A Basic Study of Photodynamic Therapy with Glucose-Conjugated Chlorin e6 Using Mammary Carcinoma Xenografts | A Basic Study of Photodynamic Therapy with Glucose-Conjugated Chlorin e6 Using Mammary Carcinoma Xenografts Abstract By using the Warburg effect—a phenomenon where tumors consume higher glucose levels than normal cells—on cancer cells to enhance the effect of photodynamic therapy (PDT), we developed a new photosensitiz... |
PMC3551257 | core_pubmed_pmc | A Multi-Scale Modeling Framework for Individualized, Spatiotemporal Prediction of Drug Effects and Toxicological Risk | A Multi-Scale Modeling Framework for Individualized, Spatiotemporal Prediction of Drug Effects and Toxicological Risk Abstract In this study, we focus on a novel multi-scale modeling approach for spatiotemporal prediction of the distribution of substances and resulting hepatotoxicity by combining cellular models, a 2D ... |
PMC10893115 | core_pubmed_pmc | Chemical Composition Antioxidant and Anti-Inflammatory Activities of Myrtus communis L. Leaf Extract: Forecasting ADMET Profiling and Anti-Inflammatory Targets Using Molecular Docking Tools | Chemical Composition Antioxidant and Anti-Inflammatory Activities of Myrtus communis L. Leaf Extract: Forecasting ADMET Profiling and Anti-Inflammatory Targets Using Molecular Docking Tools Abstract Compounds derived from natural sources continue to serve as chemical scaffolds for designing prophylactic/therapeutic opt... |
PMC5439386 | core_pubmed_pmc | Genetic polymorphisms of multidrug and toxin extrusion proteins (MATE1 and MATE2) in South Indian population | Genetic polymorphisms of multidrug and toxin extrusion proteins (MATE1 and MATE2) in South Indian population Abstract Introduction: Drug transporters are key determinants of pharmacokinetic and pharmacodynamic profiles of certain drugs. SLC47A1 (MATE1) and SLC47A2 (MATE2) are major efflux transporters involved in the h... |
PMC11473484 | core_pubmed_pmc | The versatile multi-functional substance NMN: its unique characteristics, metabolic properties, pharmacodynamic effects, clinical trials, and diverse applications | The versatile multi-functional substance NMN: its unique characteristics, metabolic properties, pharmacodynamic effects, clinical trials, and diverse applications Abstract β-nicotinamide mononucleotide (NMN) is a naturally occurring biologically active nucleotide widely present in organisms and an inherent substance in... |
PMC10164338 | core_pubmed_pmc | Model-based assessment of combination therapies – ranking of radiosensitizing agents in oncology | Model-based assessment of combination therapies – ranking of radiosensitizing agents in oncology Abstract Background To increase the chances of finding efficacious anticancer drugs, improve development times and reduce costs, it is of interest to rank test compounds based on their potential for human use as early as po... |
PMC10657815 | core_pubmed_pmc | Pharmacokinetics and absorption mechanism of tandospirone citrate | Pharmacokinetics and absorption mechanism of tandospirone citrate Abstract Tandospirone citrate (TDS) is commonly used for the treatment of patients with generalized anxiety disorder in clinical practice, and several studies are developing new indications for TDS. However, the in vivo processes and absorption propertie... |
PMC10486604 | core_pubmed_pmc | Discovery of VIP236, an αvβ3-Targeted Small-Molecule–Drug Conjugate with Neutrophil Elastase-Mediated Activation of 7-Ethyl Camptothecin Payload for Treatment of Solid Tumors | Discovery of VIP236, an αvβ3-Targeted Small-Molecule–Drug Conjugate with Neutrophil Elastase-Mediated Activation of 7-Ethyl Camptothecin Payload for Treatment of Solid Tumors Abstract Simple Summary The goal of this work was to improve the tumor selectivity of chemotherapy to reduce side effects and improve efficacy. W... |
PMC8367944 | core_pubmed_pmc | Phase 1 study of the ATR inhibitor berzosertib in combination with cisplatin in patients with advanced solid tumours | Phase 1 study of the ATR inhibitor berzosertib in combination with cisplatin in patients with advanced solid tumours Abstract Abstract Background Berzosertib (formerly M6620, VX-970) is a highly potent and selective, first-in-class ataxia telangiectasia-mutated and Rad3-related protein kinase (ATR) inhibitor. We assess... |
PMC7066681 | core_pubmed_pmc | Allergen immunotherapy phase II trials: Challenges in dose finding | Allergen immunotherapy phase II trials: Challenges in dose finding Abstract Abstract Phase II studies on allergen immunotherapy (AIT) should define the dose with the best balance between efficacy and safety (“optimal dose”). Their key role is based on dose selection for subsequent pivotal studies (phase III, field stud... |
PMC8214796 | core_pubmed_pmc | Evaluation of body-surface-area adjusted dosing of high-dose methotrexate by population pharmacokinetics in a large cohort of cancer patients | Evaluation of body-surface-area adjusted dosing of high-dose methotrexate by population pharmacokinetics in a large cohort of cancer patients Abstract Abstract Background The aim of this study was to identify sources of variability including patient gender and body surface area (BSA) in pharmacokinetic (PK) exposure fo... |
PMC3130785 | core_pubmed_pmc | Small Compound 6- O -Angeloylplenolin Induces Mitotic Arrest and Exhibits Therapeutic Potentials in Multiple Myeloma | Small Compound 6- O -Angeloylplenolin Induces Mitotic Arrest and Exhibits Therapeutic Potentials in Multiple Myeloma Abstract Abstract Background Multiple myeloma (MM) is a disease of cell cycle dysregulation while cell cycle modulation can be a target for MM therapy. In this study we investigated the effects and mecha... |
PMC11093098 | core_pubmed_pmc | Iterative nanoparticle bioengineering enabled by x-ray fluorescence imaging | Iterative nanoparticle bioengineering enabled by x-ray fluorescence imaging Abstract Nanoparticles (NPs) are currently developed for drug delivery and molecular imaging. However, they often get intercepted before reaching their target, leading to low targeting efficacy and signal-to-noise ratio. They tend to accumulate... |
PMC11183791 | core_pubmed_pmc | Vancomycin population pharmacokinetics and dosing proposal for the initial treatment in obese adult patients | Vancomycin population pharmacokinetics and dosing proposal for the initial treatment in obese adult patients Abstract Abstract Aim The aim of this study was to develop a vancomycin population pharmacokinetic model in adult obese patients and propose covariate-based dosing individualization in order to maximize the achi... |
PMC3351968 | core_pubmed_pmc | What is a preferred angiotensin II receptor blocker-based combination therapy for blood pressure control in hypertensive patients with diabetic and non-diabetic renal impairment? | What is a preferred angiotensin II receptor blocker-based combination therapy for blood pressure control in hypertensive patients with diabetic and non-diabetic renal impairment? Abstract Hypertension has a major associated risk for organ damage and mortality, which is further heightened in patients with prior cardiova... |
PMC7914879 | core_pubmed_pmc | Prevalence and Clinical Significance of Drug–Drug and Drug–Dietary Supplement Interactions among Patients Admitted for Cardiothoracic Surgery in Greece | Prevalence and Clinical Significance of Drug–Drug and Drug–Dietary Supplement Interactions among Patients Admitted for Cardiothoracic Surgery in Greece Abstract Abstract Background: Drug interactions represent a major issue in clinical settings, especially for critically ill patients such as those with cardiovascular d... |
PMC11949687 | core_pubmed_pmc | Pharmacodynamic Modeling of Cinacalcet in Secondary Hyperparathyroidism: Efficacy and Influencing Factors Analysis | Pharmacodynamic Modeling of Cinacalcet in Secondary Hyperparathyroidism: Efficacy and Influencing Factors Analysis Abstract Abstract Context Cinacalcet, the first FDA-approved calcimimetic agent for treating secondary hyperparathyroidism (SHPT), has unclear factors influencing its therapeutic efficacy in clinical pract... |
PMC8349200 | core_pubmed_pmc | Real-World Use of Dalbavancin in the Era of Empowerment of Outpatient Antimicrobial Treatment: A Careful Appraisal Beyond Approved Indications Focusing on Unmet Clinical Needs | Real-World Use of Dalbavancin in the Era of Empowerment of Outpatient Antimicrobial Treatment: A Careful Appraisal Beyond Approved Indications Focusing on Unmet Clinical Needs Abstract Abstract Dalbavancin is a novel, long-acting lipoglycopeptide characterized by a long elimination half-life coupled with excellent in v... |
PMC7609071 | core_pubmed_pmc | Liposomal delivery of hydrophobic RAMBAs provides good bioavailability and significant enhancement of retinoic acid signalling in neuroblastoma tumour cells | Liposomal delivery of hydrophobic RAMBAs provides good bioavailability and significant enhancement of retinoic acid signalling in neuroblastoma tumour cells Abstract Abstract Retinoid treatment is employed during residual disease treatment in neuroblastoma, where the aim is to induce neural differentiation or death in ... |
PMC4809623 | core_pubmed_pmc | Model‐Based Assessment of Plasma Citrate Flux Into the Liver: Implications for NaCT as a Therapeutic Target | Model‐Based Assessment of Plasma Citrate Flux Into the Liver: Implications for NaCT as a Therapeutic Target Abstract Abstract Cytoplasmic citrate serves as an important regulator of gluconeogenesis and carbon source for de novo lipogenesis in the liver. For this reason, the sodium‐coupled citrate transporter (NaCT), a ... |
PMC7897820 | core_pubmed_pmc | Pharmacokinetics of Tobramycin Administered at the Beginning of Intermittent Hemodialysis Session (ESRD Study) | Pharmacokinetics of Tobramycin Administered at the Beginning of Intermittent Hemodialysis Session (ESRD Study) Abstract Abstract Background and Objectives: There is a renewed interest in the successful use of aminoglycosides due to increasing resistance in gram-negative infections. Few studies to date have examined the... |
PMC7499297 | core_pubmed_pmc | Bisoprolol responses (PK/PD) in hypertensive patients: A cytochrome P450 (CYP) 2D6 targeted polymorphism study | Bisoprolol responses (PK/PD) in hypertensive patients: A cytochrome P450 (CYP) 2D6 targeted polymorphism study Abstract Background Bisoprolol is an effective β1-adrenergic blocker, an inter-individual genetic variability was recorded in its response. This study aimed at investigating the association of CYP2D6*2A (rs108... |
PMC11476011 | core_pubmed_pmc | UROPOT: study protocol for a randomized, double-blind phase I/II trial for metabolism-based potentiation of antimicrobial prophylaxis in the urological tract | UROPOT: study protocol for a randomized, double-blind phase I/II trial for metabolism-based potentiation of antimicrobial prophylaxis in the urological tract Abstract Background Urinary tract catheters, including Double-J or ureteral stents, are prone to bacterial colonization forming biofilms and leading to asymptomat... |
PMC11554354 | core_pubmed_pmc | Assessing Pharmacokinetics and Safety of Therapeutic Alpha-1-Microglobulin in First-in-Human Kidney Transplantation: A Noncomparative Open-Label Multiple-Dose Phase 1b Study | Assessing Pharmacokinetics and Safety of Therapeutic Alpha-1-Microglobulin in First-in-Human Kidney Transplantation: A Noncomparative Open-Label Multiple-Dose Phase 1b Study Abstract Abstract Background. RMC-035 is a modified version of alpha-1-microglobulin, an endogenous protein developed as a renoprotective agent. I... |
PMC8873822 | core_pubmed_pmc | Emergence and Mechanism of Resistance of Tulathromycin Against Mycoplasma hyopneumoniae in a PK/PD Model and the Fitness Costs of 23S rRNA Mutants | Emergence and Mechanism of Resistance of Tulathromycin Against Mycoplasma hyopneumoniae in a PK/PD Model and the Fitness Costs of 23S rRNA Mutants Abstract Macrolides are widely used in diseases caused by Mycoplasma spp. The new semi-synthetic macrolide antibiotic tulathromycin is currently in wide use for the treatmen... |
PMC4544271 | core_pubmed_pmc | Effect of variations in treatment regimen and liver cirrhosis on exposure to benzodiazepines during treatment of alcohol withdrawal syndrome | Effect of variations in treatment regimen and liver cirrhosis on exposure to benzodiazepines during treatment of alcohol withdrawal syndrome Abstract Abstract Purpose: Benzodiazepines (BDZs) are the drugs of choice to prevent the symptoms of alcohol withdrawal syndrome (AWS). Various treatment protocols are published a... |
PMC4588186 | core_pubmed_pmc | Pharmacogenomics Implications of Using Herbal Medicinal Plants on African Populations in Health Transition | Pharmacogenomics Implications of Using Herbal Medicinal Plants on African Populations in Health Transition Abstract Abstract The most accessible points of call for most African populations with respect to primary health care are traditional health systems that include spiritual, religious, and herbal medicine. This rev... |
PMC12616872 | core_pubmed_pmc | The Dorsal Forearm as a Novel Target for Intramuscular Injections: Clinical Pharmacokinetic Results With Naloxone | The Dorsal Forearm as a Novel Target for Intramuscular Injections: Clinical Pharmacokinetic Results With Naloxone Abstract ABSTRACT The dorsal forearm represents a potentially viable location for a convenient wearable device for the administration of intramuscular (IM) injections, but this site has not previously been ... |
PMC12030146 | core_pubmed_pmc | The In Vitro Pharmacokinetics of Medicinal Plants: A Review | The In Vitro Pharmacokinetics of Medicinal Plants: A Review Abstract Abstract Background: This review examines in vitro techniques for characterizing the pharmacokinetics of medicinal plants, focusing on their role in understanding absorption, distribution, metabolism, and excretion (ADME). The diverse bioactive compou... |
PMC11856606 | core_pubmed_pmc | Exploring Marine Natural Compounds: Innovative Therapeutic Candidates Against Chagas Disease Through Virtual Screening and Molecular Dynamics | Exploring Marine Natural Compounds: Innovative Therapeutic Candidates Against Chagas Disease Through Virtual Screening and Molecular Dynamics Abstract Abstract Chagas disease, caused by the protozoan Trypanosoma cruzi , represents a significant public health challenge, particularly in Latin America’s endemic regions. T... |
PMC5736845 | core_pubmed_pmc | Pharmacokinetics of multiple doses of co‐crystal of tramadol–celecoxib: findings from a four‐way randomized open‐label phase I clinical trial | Pharmacokinetics of multiple doses of co‐crystal of tramadol–celecoxib: findings from a four‐way randomized open‐label phase I clinical trial Abstract Abstract Aim We compared the pharmacokinetic (PK) profiles of co‐crystal of tramadol–celecoxib (CTC) vs. each reference product (alone and in open combination) after sin... |
PMC4441120 | core_pubmed_pmc | Gene expression studies of a human monocyte cell line identify dissimilarities between differently manufactured glatiramoids | Gene expression studies of a human monocyte cell line identify dissimilarities between differently manufactured glatiramoids Abstract Abstract Glatiramer Acetate (GA) has provided safe and effective treatment for multiple sclerosis (MS) patients for two decades. It acts as an antigen, yet the precise mechanism of actio... |
PMC8635024 | core_pubmed_pmc | Dose Optimization of Aditoprim-Sulfamethoxazole Combinations Against Trueperella pyogenes From Patients With Clinical Endometritis by Using Semi-mechanistic PK/PD Model | Dose Optimization of Aditoprim-Sulfamethoxazole Combinations Against Trueperella pyogenes From Patients With Clinical Endometritis by Using Semi-mechanistic PK/PD Model Abstract Combinations of two and more drugs with different target sites are being used as a new treatment regimen for resistant clones of bacteria. Tho... |
PMC11600154 | core_pubmed_pmc | Slow-Binding and Covalent HDAC Inhibition: A New Paradigm? | Slow-Binding and Covalent HDAC Inhibition: A New Paradigm? Abstract The dysregulated post-translational modification of proteins is an established hallmark of human disease. Through Zn 2+ -dependent hydrolysis of acyl-lysine modifications, histone deacetylases (HDACs) are key regulators of disease-implicated signaling ... |
PMC6267549 | core_pubmed_pmc | Pharmacokinetics, Safety and Tolerability of Oral Semaglutide in Subjects with Renal Impairment | Pharmacokinetics, Safety and Tolerability of Oral Semaglutide in Subjects with Renal Impairment Abstract Background Semaglutide, a glucagon-like peptide-1 (GLP-1) analogue, has been co-formulated with the absorption enhancer sodium N -(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) as a tablet for oral administration. Th... |
PMC8048922 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Target Attainment in Adult and Pediatric Patients Following Administration of Ceftaroline Fosamil as a 5‐Minute Infusion | Pharmacokinetic and Pharmacodynamic Target Attainment in Adult and Pediatric Patients Following Administration of Ceftaroline Fosamil as a 5‐Minute Infusion Abstract Abstract The key pharmacokinetic/pharmacodynamic (PK/PD) efficacy index for β‐lactam antibiotics is the percentage of time that free drug concentrations e... |
PMC9952492 | core_pubmed_pmc | Tigecycline Pharmacokinetic and Pharmacodynamic Profile in Patients with Chronic Obstructive Pulmonary Disease Exacerbation | Tigecycline Pharmacokinetic and Pharmacodynamic Profile in Patients with Chronic Obstructive Pulmonary Disease Exacerbation Abstract Background: We aimed to evaluate the pharmacokinetic profile of tigecycline in plasma and its penetration to sputum in moderately ill patients with an infectious acute exacerbation of chr... |
PMC3337408 | core_pubmed_pmc | Clinical pharmacology of trastuzumab emtansine (T-DM1): an antibody–drug conjugate in development for the treatment of HER2-positive cancer | Clinical pharmacology of trastuzumab emtansine (T-DM1): an antibody–drug conjugate in development for the treatment of HER2-positive cancer Abstract Purpose Trastuzumab emtansine (T-DM1) is an antibody–drug conjugate comprising trastuzumab and DM1, a microtubule polymerization inhibitor, covalently bound via a stable t... |
PMC8212751 | core_pubmed_pmc | Effect of meal timing on pharmacokinetics and pharmacodynamics of tegoprazan in healthy male volunteers | Effect of meal timing on pharmacokinetics and pharmacodynamics of tegoprazan in healthy male volunteers Abstract Abstract Abstract Tegoprazan, a novel potassium‐competitive acid blocker, is used to treat acid‐related diseases. However, there is no information on the pharmacokinetic (PK) and pharmacodynamic (PD) profile... |
PMC10674218 | core_pubmed_pmc | Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers | Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers Abstract The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be approp... |
PMC6061080 | core_pubmed_pmc | Modeling and simulations to support dose selection for eslicarbazepine acetate therapy in pediatric patients with partial-onset seizures | Modeling and simulations to support dose selection for eslicarbazepine acetate therapy in pediatric patients with partial-onset seizures Abstract Abstract Modeling and simulations were used to support body weight-based dose selection for eslicarbazepine acetate (ESL) in pediatric subjects aged 4–17 years with partial-o... |
PMC11706428 | core_pubmed_pmc | Immunostimulatory/Immunodynamic model of mRNA ‐1273 to guide pediatric vaccine dose selection | Immunostimulatory/Immunodynamic model of mRNA ‐1273 to guide pediatric vaccine dose selection Abstract Abstract COVID‐19 vaccines, including mRNA‐1273, have been rapidly developed and deployed. Establishing the optimal dose is crucial for developing a safe and effective vaccine. Modeling and simulation have the potenti... |
PMC11212004 | core_pubmed_pmc | Preclinical evaluation of ELP‐004 in mice | Preclinical evaluation of ELP‐004 in mice Abstract Abstract This study provides a detailed understanding of the preclinical pharmacokinetics and metabolism of ELP‐004, an osteoclast inhibitor in development for the treatment of bone erosion. Current treatments for arthritis, including biological disease‐modifying antir... |
PMC5708953 | core_pubmed_pmc | Effect of MDR1 C1236T polymorphism on cyclosporine pharmacokinetics | Effect of MDR1 C1236T polymorphism on cyclosporine pharmacokinetics Abstract Abstract Background: Cyclosporine (CsA) is one of the immunosuppressive drugs, whose pharmacokinetic characteristics vary greatly among individuals. The published data reveal conflicting effects of the polymorphism of MDR1 exon 12 SNP C1236T o... |
PMC11141866 | core_pubmed_pmc | Pyrimidine depletion enhances targeted and immune therapy combinations in acute myeloid leukemia | Pyrimidine depletion enhances targeted and immune therapy combinations in acute myeloid leukemia Abstract Acute myeloid leukemia (AML) is a fatal disease characterized by the accumulation of undifferentiated myeloblasts, and agents that promote differentiation have been effective in this disease but are not curative. D... |
PMC12386373 | core_pubmed_pmc | Antifungal Agents in the 21st Century: Advances, Challenges, and Future Perspectives | Antifungal Agents in the 21st Century: Advances, Challenges, and Future Perspectives Abstract Abstract Invasive fungal infections (IFIs) represent a growing global health threat, particularly for immunocompromised populations, with mortality exceeding 1.5 million deaths annually. Despite their clinical and economic bur... |
PMC3824208 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of sitafloxacin in patients with community-acquired respiratory tract infections | Population pharmacokinetics and pharmacodynamics of sitafloxacin in patients with community-acquired respiratory tract infections Abstract Abstract An optimal dosage regimen of sitafloxacin was considered based on a pharmacokinetics and pharmacodynamics (PK–PD) analysis in patients with community-acquired respiratory t... |
PMC7718284 | core_pubmed_pmc | Buprenorphine is a weak dopamine releaser relative to heroin, but its pretreatment attenuates heroin‐evoked dopamine release in rats | Buprenorphine is a weak dopamine releaser relative to heroin, but its pretreatment attenuates heroin‐evoked dopamine release in rats Abstract Abstract Aims The United States of America is currently in an opioid epidemic. Heroin remains the most lethal opioid option with its death rate increasing by over 500% in the las... |
PMC7188736 | core_pubmed_pmc | 18 F-Fluciclovine ( 18 F-FACBC) PET imaging of recurrent brain tumors | 18 F-Fluciclovine ( 18 F-FACBC) PET imaging of recurrent brain tumors Abstract Purpose The aim of our study was to investigate the efficacy of 18 F-Fluciclovine brain PET imaging in recurrent gliomas, and to compare the utility of these images to that of contrast enhanced magnetic resonance imaging (MRI) and to [ 11 C-... |
PMC11799634 | core_pubmed_pmc | Study of the effect of different diluents for syringe immersion test on Rhipicephalus microplus larvae against macrocyclic lactones | Study of the effect of different diluents for syringe immersion test on Rhipicephalus microplus larvae against macrocyclic lactones Abstract Abstract Background: Macrocyclic lactones (MLs) are pharmaceutical compounds extensively utilized in the management of Rhipicephalus microplus tick infestations in bovine populati... |
PMC5351320 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Comparison of Sildenafil‐Bosentan and Sildenafil‐Ambrisentan Combination Therapies for Pulmonary Hypertension | Pharmacokinetic and Pharmacodynamic Comparison of Sildenafil‐Bosentan and Sildenafil‐Ambrisentan Combination Therapies for Pulmonary Hypertension Abstract To elucidate whether the pharmacokinetics (PK) and pharmacodynamics (PD) of sildenafil are influenced differently when it is coadministered with bosentan (S+B) or wi... |
PMC11334299 | core_pubmed_pmc | Challenges with sirolimus experimental data to inform QSP model of post‐transplantation cyclophosphamide regimens | Challenges with sirolimus experimental data to inform QSP model of post‐transplantation cyclophosphamide regimens Abstract Abstract Dose optimization of sirolimus may further improve outcomes in allogeneic hematopoietic cell transplant (HCT) patients receiving post‐transplantation cyclophosphamide (PTCy) to prevent gra... |
PMC7284437 | core_pubmed_pmc | Naturally Occurring PCSK9 Inhibitors | Naturally Occurring PCSK9 Inhibitors Abstract Abstract Genetic, epidemiological and pharmacological data have led to the conclusion that antagonizing or inhibiting Proprotein convertase subtilisin/kexin type 9 (PCSK9) reduces cardiovascular events. This clinical outcome is mainly related to the pivotal role of PCSK9 in... |
PMC12167918 | core_pubmed_pmc | A Model‐Based Approach to Evaluate Anti‐Drug Antibody Impact on Drug Exposure With Biologics: A Case Example With the CD3 T‐Cell Bispecific Cibisatamab | A Model‐Based Approach to Evaluate Anti‐Drug Antibody Impact on Drug Exposure With Biologics: A Case Example With the CD3 T‐Cell Bispecific Cibisatamab Abstract ABSTRACT The administration of biologics can lead to immunogenic responses that trigger anti‐drug antibody (ADA) formation. ADAs can decrease drug exposure. A ... |
PMC7188670 | core_pubmed_pmc | Two first-in-human studies of xentuzumab, a humanised insulin-like growth factor (IGF)-neutralising antibody, in patients with advanced solid tumours | Two first-in-human studies of xentuzumab, a humanised insulin-like growth factor (IGF)-neutralising antibody, in patients with advanced solid tumours Abstract Background Xentuzumab, an insulin-like growth factor (IGF)-1/IGF-2-neutralising antibody, binds IGF-1 and IGF-2, inhibiting their growth-promoting signalling. Tw... |
PMC10361915 | core_pubmed_pmc | Analgesic effect of oral paracetamol 1000 mg/ibuprofen 400 mg, paracetamol 1000 mg/codeine 60 mg, paracetamol 1000 mg/ibuprofen 400 mg/codeine 60 mg, or placebo on acute postoperative pain: a single-dose, randomized, and double-blind study | Analgesic effect of oral paracetamol 1000 mg/ibuprofen 400 mg, paracetamol 1000 mg/codeine 60 mg, paracetamol 1000 mg/ibuprofen 400 mg/codeine 60 mg, or placebo on acute postoperative pain: a single-dose, randomized, and double-blind study Abstract Abstract Purpose Combining analgesics with different mechanisms of acti... |
PMC7775138 | core_pubmed_pmc | Bioavailability and Pharmacokinetics of Anisatin in Mouse Blood by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry | Bioavailability and Pharmacokinetics of Anisatin in Mouse Blood by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Abstract Background Anisatin is a neurotoxic sesquiterpene dilactone wildly found in plants of the family Illiciaceae . Due to morphological similarities among Illiciaceae fruits, fatal po... |
PMC9811505 | core_pubmed_pmc | Polymeric encapsulation of a ruthenium( ii ) polypyridyl complex: from synthesis to in vivo studies against high-grade epithelial ovarian cancer † | Polymeric encapsulation of a ruthenium( ii ) polypyridyl complex: from synthesis to in vivo studies against high-grade epithelial ovarian cancer † Abstract The in vitro to in vivo translation of metal-based cytotoxic drugs has proven to be a significant hurdle in their establishment as effective anti-cancer alternative... |
PMC10818085 | core_pubmed_pmc | Pharmacokinetics and coagulation biomarkers in children and adults with hemophilia A receiving emicizumab prophylaxis every 1, 2, or 4 weeks | Pharmacokinetics and coagulation biomarkers in children and adults with hemophilia A receiving emicizumab prophylaxis every 1, 2, or 4 weeks Abstract Background Emicizumab is a bispecific antibody that bridges activated factor (F)IX and FX, mimicking the function of missing activated FVIII and thus improving hemostasis... |
PMC9293430 | core_pubmed_pmc | Type of proton‐pump inhibitor and risk of iron deficiency in kidney transplant recipients – results from the TransplantLines Biobank and Cohort Study | Type of proton‐pump inhibitor and risk of iron deficiency in kidney transplant recipients – results from the TransplantLines Biobank and Cohort Study Abstract Summary Proton‐pump inhibitors (PPIs) have been associated with iron deficiency (ID) in kidney transplant recipients (KTRs). Gastric acid plays a pivotal role in... |
PMC4756062 | core_pubmed_pmc | Augmentation of Endoxifen Exposure in Tamoxifen-Treated Women Following SSRI Switch | Augmentation of Endoxifen Exposure in Tamoxifen-Treated Women Following SSRI Switch Abstract Abstract Background and Objective The anti-oestrogen tamoxifen requires metabolic activation to endoxifen by cytochrome P450 (CYP) enzymes, predominantly CYP2D6. Potent CYP2D6-inhibiting antidepressants can seriously disrupt ta... |
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