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PMC5995553 | core_pubmed_pmc | Standardization of the infusion sequence of antineoplastic drugs used in the treatment of breast and colorectal cancers | Standardization of the infusion sequence of antineoplastic drugs used in the treatment of breast and colorectal cancers Abstract ABSTRACT The definition of antineoplastic administration sequences can help planning of therapeutic regimens in a more rational way, and thus optimize chemotherapy effects on patients, increa... |
PMC6156522 | core_pubmed_pmc | Dosing Regimen of Enrofloxacin Impacts Intestinal Pharmacokinetics and the Fecal Microbiota in Steers | Dosing Regimen of Enrofloxacin Impacts Intestinal Pharmacokinetics and the Fecal Microbiota in Steers Abstract Abstract Objective: The intestinal concentrations of antimicrobial drugs that select for resistance in fecal bacteria of cattle are poorly understood. Our objective was to associate active drug concentrations ... |
PMC3854123 | core_pubmed_pmc | Phase I dose-finding study of cabazitaxel administered weekly in patients with advanced solid tumours | Phase I dose-finding study of cabazitaxel administered weekly in patients with advanced solid tumours Abstract Background Cabazitaxel is approved in patients with metastatic hormone-refractory prostate cancer previously treated with a docetaxel-containing regimen. This study evaluated a weekly cabazitaxel dosing regime... |
PMC9067469 | core_pubmed_pmc | Elimination of plasma soluble antigen in cynomolgus monkeys by combining pH-dependent antigen binding and novel Fc engineering | Elimination of plasma soluble antigen in cynomolgus monkeys by combining pH-dependent antigen binding and novel Fc engineering Abstract ABSTRACT A conventional antibody targeting a soluble antigen in circulation typically requires a huge dosage and frequent intravenous administration to neutralize the antigen. This is ... |
PMC9381890 | core_pubmed_pmc | Application of SHAP values for inferring the optimal functional form of covariates in pharmacokinetic modeling | Application of SHAP values for inferring the optimal functional form of covariates in pharmacokinetic modeling Abstract Abstract In population pharmacokinetic (PK) models, interindividual variability is explained by implementation of covariates in the model. The widely used forward stepwise selection method is sensitiv... |
PMC3852065 | core_pubmed_pmc | Estimation of feasible solution space using Cluster Newton Method: application to pharmacokinetic analysis of irinotecan with physiologically-based pharmacokinetic models | Estimation of feasible solution space using Cluster Newton Method: application to pharmacokinetic analysis of irinotecan with physiologically-based pharmacokinetic models Abstract Background To facilitate new drug development, physiologically-based pharmacokinetic (PBPK) modeling methods receive growing attention as a ... |
PMC7828678 | core_pubmed_pmc | Impact of DOTA Conjugation on Pharmacokinetics and Immunoreactivity of [ 177 Lu]Lu-1C1m-Fc, an Anti TEM-1 Fusion Protein Antibody in a TEM-1 Positive Tumor Mouse Model | Impact of DOTA Conjugation on Pharmacokinetics and Immunoreactivity of [ 177 Lu]Lu-1C1m-Fc, an Anti TEM-1 Fusion Protein Antibody in a TEM-1 Positive Tumor Mouse Model Abstract Abstract 1C1m-Fc, an anti-tumor endothelial marker 1 (TEM-1) scFv-Fc fusion protein antibody, was previously successfully radiolabeled with 177... |
PMC6394711 | core_pubmed_pmc | Timing flexibility of oral NEPA, netupitant-palonosetron combination, administration for the prevention of chemotherapy-induced nausea and vomiting (CINV) | Timing flexibility of oral NEPA, netupitant-palonosetron combination, administration for the prevention of chemotherapy-induced nausea and vomiting (CINV) Abstract Abstract Purpose The administration timing of antiemetic and chemotherapeutic regimens is often determined by regulatory indications, based on registration ... |
PMC5596462 | core_pubmed_pmc | A phase I open-label dose-escalation study of the anti-HER3 monoclonal antibody LJM716 in patients with advanced squamous cell carcinoma of the esophagus or head and neck and HER2-overexpressing breast or gastric cancer | A phase I open-label dose-escalation study of the anti-HER3 monoclonal antibody LJM716 in patients with advanced squamous cell carcinoma of the esophagus or head and neck and HER2-overexpressing breast or gastric cancer Abstract Background Human epidermal growth factor receptor 3 (HER3) is important in maintaining epid... |
PMC4231369 | core_pubmed_pmc | TNF-α blockade is ineffective in animal models of established polycystic kidney disease | TNF-α blockade is ineffective in animal models of established polycystic kidney disease Abstract Background Given the large medical burden of polycystic kidney disease (PKD) and recent clinical trial failures, there is a need for novel, safe and effective treatments for the disorder. Methods In PCK rat and PKD2 (ws25/w... |
PMC12715038 | core_pubmed_pmc | Evaluation of Fentanyl-Emerged Adverse Events and Pharmacokinetics in Neonates: A Physiologically Based Pharmacokinetic Modeling Approach | Evaluation of Fentanyl-Emerged Adverse Events and Pharmacokinetics in Neonates: A Physiologically Based Pharmacokinetic Modeling Approach Abstract Background Despite its common use for analgesia in neonatal intensive care units, the optimal dosing and safety profile of fentanyl, particularly regarding suspected fentany... |
PMC3010156 | core_pubmed_pmc | Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats | Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats Abstract The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half ... |
PMC6617324 | core_pubmed_pmc | Effect of Pharmacist Intervention on a Population in Taiwan with High Healthcare Utilization and Excessive Polypharmacy | Effect of Pharmacist Intervention on a Population in Taiwan with High Healthcare Utilization and Excessive Polypharmacy Abstract Patients with high healthcare utilization are at increased risk of polypharmacy and drug interactions. This study investigated the changes in the number of medications, drug interactions and ... |
PMC12387457 | core_pubmed_pmc | Role of OCT1 and MAP3K5 Genetic Polymorphisms in Hydroxyurea Pharmacokinetics | Role of OCT1 and MAP3K5 Genetic Polymorphisms in Hydroxyurea Pharmacokinetics Abstract Abstract Background: Hydroxyurea is approved for the treatment of paediatric and adult sickle cell disease patients. It causes the synthesis of foetal haemoglobin and decreases platelets and granulocytes, but with a high interindivid... |
PMC4475836 | core_pubmed_pmc | Effect of HPMC and mannitol on drug release and bioadhesion behavior of buccal discs of buspirone hydrochloride: In-vitro and in-vivo pharmacokinetic studies | Effect of HPMC and mannitol on drug release and bioadhesion behavior of buccal discs of buspirone hydrochloride: In-vitro and in-vivo pharmacokinetic studies Abstract Abstract Delivery of orally compromised therapeutic drug molecules to the systemic circulation via buccal route has gained a significant interest in rece... |
PMC12094251 | core_pubmed_pmc | ALLG APML5: bioavailability and safety of oral arsenic trioxide assessed during consolidation therapy for APL | ALLG APML5: bioavailability and safety of oral arsenic trioxide assessed during consolidation therapy for APL Abstract Key Points • Pharmacokinetic analysis of a novel oral ATO formulation in patients with APL shows bioequivalence with the IV formulation. • No unanticipated toxicity signals were evident during short-te... |
PMC9050759 | core_pubmed_pmc | DiffErenCes in AntihypertenSive Drug Blood Levels in Patients with HypertensiON (DECISION): Protocol for a Prospective Observational Study Comparing Pharmacokinetics and Pharmacodynamics Between Young and Elderly Patients | DiffErenCes in AntihypertenSive Drug Blood Levels in Patients with HypertensiON (DECISION): Protocol for a Prospective Observational Study Comparing Pharmacokinetics and Pharmacodynamics Between Young and Elderly Patients Abstract Abstract Adequate controlled blood pressure decreases the risk of cardiovascular events. ... |
PMC7271939 | core_pubmed_pmc | The NOCTURNE Randomized Trial Comparing 2 Tolvaptan Formulations | The NOCTURNE Randomized Trial Comparing 2 Tolvaptan Formulations Abstract Abstract Introduction Tolvaptan, a treatment for autosomal dominant polycystic kidney disease (ADPKD), inhibits vasopressin V2 receptor signaling, which causes aquaretic adverse events (AAEs). The short-term efficacy and tolerability of a once-da... |
PMC8359281 | core_pubmed_pmc | Comparison of Steroidogenic Exposure Following the Administration of Repository Corticotropin Injection With a Synthetic ACTH 1‐24 Depot and Methylprednisolone in Healthy Subjects | Comparison of Steroidogenic Exposure Following the Administration of Repository Corticotropin Injection With a Synthetic ACTH 1‐24 Depot and Methylprednisolone in Healthy Subjects Abstract Abstract The pharmacokinetics (PK) and pharmacodynamics (PD) of clinically relevant doses of repository corticotropin injection (Ac... |
PMC12406672 | core_pubmed_pmc | Pharmacokinetics and hematologic toxicity of linezolid in children: a prospective, two-center cohort study | Pharmacokinetics and hematologic toxicity of linezolid in children: a prospective, two-center cohort study Abstract ABSTRACT Despite the widespread pediatric use of linezolid, data on its hematologic toxicity—particularly among children exposed to anticancer chemotherapy—remain limited and inconsistent. This study aime... |
PMC5761479 | core_pubmed_pmc | Liquid chromatography/tandem mass spectrometry method for quantitative estimation of solutol HS15 and its applications | Liquid chromatography/tandem mass spectrometry method for quantitative estimation of solutol HS15 and its applications Abstract A rapid, sensitive and selective pseudoMRM (pMRM)-based method for the determination of solutol HS15 (SHS15) in rat plasma was developed using liquid chromatography/tandem mass spectrometry (L... |
PMC8920421 | core_pubmed_pmc | Biological Matrix Supply Chain Shortages: More Matrices Are Now Rare—the Case for Surrogate Matrices | Biological Matrix Supply Chain Shortages: More Matrices Are Now Rare—the Case for Surrogate Matrices Abstract Abstract The COVID-19 pandemic has strained the biological matrix supply chain. An upsurge in demand driven by numerous COVID-19 therapeutic and vaccine development programs to combat the pandemic, along with l... |
PMC11271359 | core_pubmed_pmc | Population Pharmacokinetics of Inotuzumab Ozogamicin in Pediatric Relapsed/Refractory B-Cell Precursor Acute Lymphoblastic Leukemia: Results of Study ITCC-059 | Population Pharmacokinetics of Inotuzumab Ozogamicin in Pediatric Relapsed/Refractory B-Cell Precursor Acute Lymphoblastic Leukemia: Results of Study ITCC-059 Abstract Abstract Background and Objective Inotuzumab ozogamicin is an antibody-drug conjugate approved for treating relapsed/refractory B-cell precursor acute l... |
PMC8861990 | core_pubmed_pmc | The role of circadian clock pathways in viral replication | The role of circadian clock pathways in viral replication Abstract The daily oscillations of bi ological and behavioural processes are controlled by the circadian clock circuitry that drives the physiology of the organism and, in particular, the functioning of the immune system in response to infectious agents. Circadi... |
PMC11975206 | core_pubmed_pmc | Multiple‐Dose Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Subcutaneous Rusfertide, a Hepcidin Mimetic, in Healthy Subjects | Multiple‐Dose Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Subcutaneous Rusfertide, a Hepcidin Mimetic, in Healthy Subjects Abstract Abstract Rusfertide, a peptide hepcidin mimetic, has shown efficacy in polycythemia vera. This trial investigated the multiple‐dose pharmacokinetics, pharmacodynamics, ... |
PMC9922511 | core_pubmed_pmc | Profile of Linzagolix in the Management of Endometriosis, Including Design, Development and Potential Place in Therapy: A Narrative Review | Profile of Linzagolix in the Management of Endometriosis, Including Design, Development and Potential Place in Therapy: A Narrative Review Abstract Abstract Estrogens play a critical role in the pathogenesis of endometriosis and it is logical to assume that lowering estradiol levels with oral gonadotropin-releasing hor... |
PMC9557769 | core_pubmed_pmc | Cannabinoids for behavioral symptoms in severe dementia: Safety and feasibility in a long-term pilot observational study in nineteen patients | Cannabinoids for behavioral symptoms in severe dementia: Safety and feasibility in a long-term pilot observational study in nineteen patients Abstract Context The management of behavioral symptoms and rigidity in patients with dementia constitutes a significant challenge. Short-term studies suggest an interest in the u... |
PMC12875009 | core_pubmed_pmc | A comparative pharmacokinetic evaluation of two aqueous progesterone 25 mg injections in healthy postmenopausal women under fasting conditions: An open‐label, balanced, randomized, two‐treatment, two‐period, two‐sequence, single‐dose, crossover bioequivalence study | A comparative pharmacokinetic evaluation of two aqueous progesterone 25 mg injections in healthy postmenopausal women under fasting conditions: An open‐label, balanced, randomized, two‐treatment, two‐period, two‐sequence, single‐dose, crossover bioequivalence study Abstract Abstract The growing demand for assisted repr... |
PMC3304397 | core_pubmed_pmc | A systematic review on pharmacokinetic changes in critically ill patients: role of extracorporeal membrane oxygenation | A systematic review on pharmacokinetic changes in critically ill patients: role of extracorporeal membrane oxygenation Abstract Objective Several factors including disease condition and different procedures could alter pharmacokinetic profile of drugs in critically ill patients. For optimizing patient's outcome, changi... |
PMC12130181 | core_pubmed_pmc | An open-label phase I comparator-controlled clinical trial to assess tolerability and pharmacokinetics of IHL-675 A a fixed dose combination of cannabidiol plus hydroxychloroquine in healthy volunteers | An open-label phase I comparator-controlled clinical trial to assess tolerability and pharmacokinetics of IHL-675 A a fixed dose combination of cannabidiol plus hydroxychloroquine in healthy volunteers Abstract Abstract This was a phase I randomised comparator controlled clinical trial that assessed the pharmacokinetic... |
PMC5762626 | core_pubmed_pmc | Pharmacokinetics of gene recombined angiogenesis inhibitor Kringle 5 in vivo using 131 I specific markers and SPECT/CT ☆ | Pharmacokinetics of gene recombined angiogenesis inhibitor Kringle 5 in vivo using 131 I specific markers and SPECT/CT ☆ Abstract Abstract The previous pharmacokinetic methods can be only limited to drug analysis in vitro, which provide less information on the distribution and metabolismof drugs, and limit the interpre... |
PMC12197546 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Modeling of Enrofloxacin and Its Metabolite Ciprofloxacin in Pregnant Goats | Pharmacokinetic and Pharmacodynamic Modeling of Enrofloxacin and Its Metabolite Ciprofloxacin in Pregnant Goats Abstract Simple Summary Pharmacokinetics studies how drugs move in the body between the blood and different organs and tissues. When a treatment is given to a pregnant animal, it is important to consider that... |
PMC6713085 | core_pubmed_pmc | Effects of glycyrrhizin on the pharmacokinetics of paeoniflorin in rats and its potential mechanism | Effects of glycyrrhizin on the pharmacokinetics of paeoniflorin in rats and its potential mechanism Abstract Abstract Context: Paeoniflorin is reported to possess numerous pharmacological activities. Paeoniflorin and glycyrrhizin are always used together for the treatment of disease in China clinics; however, the drug–... |
PMC8092737 | core_pubmed_pmc | Mycobactericidal Effects of Different Regimens Measured by Molecular Bacterial Load Assay among People Treated for Multidrug-Resistant Tuberculosis in Tanzania | Mycobactericidal Effects of Different Regimens Measured by Molecular Bacterial Load Assay among People Treated for Multidrug-Resistant Tuberculosis in Tanzania Abstract Rifampin or multidrug-resistant tuberculosis (RR/MDR-TB) treatment has largely transitioned to regimens free of the injectable aminoglycoside component... |
PMC8643159 | core_pubmed_pmc | The Pharmacokinetic Effect of Itraconazole and Voriconazole on Ripretinib in Beagle Dogs by UPLC-MS/MS Technique | The Pharmacokinetic Effect of Itraconazole and Voriconazole on Ripretinib in Beagle Dogs by UPLC-MS/MS Technique Abstract Background A new UPLC-MS/MS technique for the determination of ripretinib in beagle dog plasma was developed, and the pharmacokinetic effects of voriconazole and itraconazole on ripretinib in beagle... |
PMC9540482 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of the Therapeutic and Adverse Effects of Ketamine in Patients With Treatment‐Refractory Depression | Population Pharmacokinetics and Pharmacodynamics of the Therapeutic and Adverse Effects of Ketamine in Patients With Treatment‐Refractory Depression Abstract We aimed to develop population pharmacokinetic/pharmacodynamic (PK/PD) models that can effectively describe ketamine and norketamine PK/PD relationships for Montg... |
PMC11955179 | core_pubmed_pmc | An Open-Label, Single and Multiple Dose Study to Evaluate the Pharmacokinetics and Safety of Fezolinetant in Healthy Chinese Female Subjects | An Open-Label, Single and Multiple Dose Study to Evaluate the Pharmacokinetics and Safety of Fezolinetant in Healthy Chinese Female Subjects Abstract Purpose To evaluate pharmacokinetics (PK) and safety of fezolinetant after single-dose and multiple-dose administration of 15, 30, and 60 mg in healthy Chinese women. Pat... |
PMC10786778 | core_pubmed_pmc | A Multicenter, Randomized, Double-Blind, Placebo-Controlled, and Dose-Increasing Study on the Safety, Tolerability and PK/PD of Multiple Doses of HSK7653 by Oral Administration in Patients with Type 2 Diabetes Mellitus in China | A Multicenter, Randomized, Double-Blind, Placebo-Controlled, and Dose-Increasing Study on the Safety, Tolerability and PK/PD of Multiple Doses of HSK7653 by Oral Administration in Patients with Type 2 Diabetes Mellitus in China Abstract Introduction This study assessed the safety, tolerability, and PK/PD of HSK7653 tab... |
PMC10431047 | core_pubmed_pmc | Population pharmacokinetic dosimetry model using imaging data to assess variability in pharmacokinetics of 177 Lu‐PSMA‐617 in prostate cancer patients | Population pharmacokinetic dosimetry model using imaging data to assess variability in pharmacokinetics of 177 Lu‐PSMA‐617 in prostate cancer patients Abstract Abstract Studies to evaluate and optimize [ 177 Lu]Lu‐PSMA treatment focus primarily on individual patient data. A population pharmacokinetic (PK) dosimetry mod... |
PMC7251631 | core_pubmed_pmc | A Neurofunctional Domains Approach to Evaluate D1/D5 Dopamine Receptor Partial Agonism on Cognition and Motivation in Healthy Volunteers With Low Working Memory Capacity | A Neurofunctional Domains Approach to Evaluate D1/D5 Dopamine Receptor Partial Agonism on Cognition and Motivation in Healthy Volunteers With Low Working Memory Capacity Abstract Abstract Background Dopamine D1 receptor signaling plays key roles in core domains of neural function, including cognition and reward process... |
PMC7280633 | core_pubmed_pmc | Prioritization of Anti‐SARS‐Cov‐2 Drug Repurposing Opportunities Based on Plasma and Target Site Concentrations Derived from their Established Human Pharmacokinetics | Prioritization of Anti‐SARS‐Cov‐2 Drug Repurposing Opportunities Based on Plasma and Target Site Concentrations Derived from their Established Human Pharmacokinetics Abstract There is a rapidly expanding literature on the in vitro antiviral activity of drugs that may be repurposed for therapy or chemoprophylaxis agains... |
PMC8116828 | core_pubmed_pmc | Targeting Sphingosine-1-Phosphate Signaling in Immune-Mediated Diseases: Beyond Multiple Sclerosis | Targeting Sphingosine-1-Phosphate Signaling in Immune-Mediated Diseases: Beyond Multiple Sclerosis Abstract Abstract Sphingosine-1-phosphate (S1P) is a bioactive lipid metabolite that exerts its actions by engaging 5 G-protein-coupled receptors (S1PR1-S1PR5). S1P receptors are involved in several cellular and physiolog... |
PMC4174045 | core_pubmed_pmc | Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose | Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose Abstract Abstract Background Mebendazole (MBZ) is an extremely insoluble and therefore poorly absorbed drug and the variable clinical results may correlate with blood concentrati... |
PMC12618439 | core_pubmed_pmc | Systematic Search of Height and Weight Changes of Exclusively Breastfed Infants Until 1 Year of age: A Contribution from the ConcePTION Project | Systematic Search of Height and Weight Changes of Exclusively Breastfed Infants Until 1 Year of age: A Contribution from the ConcePTION Project Abstract Physiologically based pharmacokinetic (PBPK) modelling and simulation allows prediction of drug exposure in specific populations, such as infants during lactation. How... |
PMC10565828 | core_pubmed_pmc | Clinical trial simulation to evaluate tenofovir disoproxil fumarate/emtricitabine HIV pre-exposure prophylaxis dosing during pregnancy | Clinical trial simulation to evaluate tenofovir disoproxil fumarate/emtricitabine HIV pre-exposure prophylaxis dosing during pregnancy Abstract Objective To evaluate upward-adjustment of tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) pre-exposure prophylaxis (PrEP) dosing during pregnancy in order to maintain ... |
PMC11981651 | core_pubmed_pmc | Phase I study on the pharmacokinetics of intravaginal, self-administered artesunate vaginal pessaries among women in Kenya | Phase I study on the pharmacokinetics of intravaginal, self-administered artesunate vaginal pessaries among women in Kenya Abstract Abstract Cervical cancer remains a significant global health issue, especially in low- and middle-income countries (LMICs), where access to prevention and treatment is limited and women ar... |
PMC9669664 | core_pubmed_pmc | Renal adverse reactions of tyrosine kinase inhibitors in the treatment of tumours: A Bayesian network meta-analysis | Renal adverse reactions of tyrosine kinase inhibitors in the treatment of tumours: A Bayesian network meta-analysis Abstract Objectives: Tumours remain a serious threat to human life. Following rapid progress in oncology research, tyrosine kinase inhibitors have been used to treat multiple tumour types. Given the great... |
PMC6419616 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic modelling to investigate in vitro synergy between colistin and fusidic acid against MDR Acinetobacter baumannii | Pharmacokinetic-pharmacodynamic modelling to investigate in vitro synergy between colistin and fusidic acid against MDR Acinetobacter baumannii Abstract Abstract Objectives The potential for synergy between colistin and fusidic acid in the treatment of MDR Acinetobacter baumannii has recently been shown . The aim of th... |
PMC10991139 | core_pubmed_pmc | Pharmacokinetics, bioavailability and tissue distribution of chitobiose and chitotriose in rats | Pharmacokinetics, bioavailability and tissue distribution of chitobiose and chitotriose in rats Abstract Chitooligosaccharides (COSs) have various physiological activities and broad application prospects; however, their pharmacokinetics and tissue distribution remain unclear. In this study, a sensitive and selective ul... |
PMC4055786 | core_pubmed_pmc | Visualization and Communication of Pharmacometric Models With Berkeley Madonna | Visualization and Communication of Pharmacometric Models With Berkeley Madonna Abstract Abstract Population or other pharmacometric models are a useful means to describe, succinctly, the relationships between drug administration, exposure (concentration), and downstream changes in pharmacodynamic (PD) biomarkers and cl... |
PMC5361694 | core_pubmed_pmc | A first-in-human phase 1 study of a hepcidin monoclonal antibody, LY2787106, in cancer-associated anemia | A first-in-human phase 1 study of a hepcidin monoclonal antibody, LY2787106, in cancer-associated anemia Abstract Abstract Background Hepcidin plays a central role in iron homeostasis and erythropoiesis. Neutralizing hepcidin with a monoclonal antibody (mAb) may prevent ferroportin internalization, restore iron efflux ... |
PMC10847209 | core_pubmed_pmc | Use of Pharmacokinetic and Pharmacodynamic Data to Develop the CDK4/6 Inhibitor Ribociclib for Patients with Advanced Breast Cancer | Use of Pharmacokinetic and Pharmacodynamic Data to Develop the CDK4/6 Inhibitor Ribociclib for Patients with Advanced Breast Cancer Abstract Ribociclib is an orally bioavailable, selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. CDK4/6 inhibition by ribociclib leads to retinoblastoma tumor suppressor protei... |
PMC7811439 | core_pubmed_pmc | The Impact of First-Line Anti-Tubercular Drugs’ Pharmacokinetics on Treatment Outcome: A Systematic Review | The Impact of First-Line Anti-Tubercular Drugs’ Pharmacokinetics on Treatment Outcome: A Systematic Review Abstract Background Tuberculosis remains the major public health problem besides tremendous efforts to combat it. Most tuberculosis patients are treated with a standard dose of first-line anti-TB drugs. The cure r... |
PMC3247120 | core_pubmed_pmc | The Effect of a High-Fat Breakfast on the Pharmacokinetics of Moxidectin in Healthy Male Subjects: A Randomized Phase I Trial | The Effect of a High-Fat Breakfast on the Pharmacokinetics of Moxidectin in Healthy Male Subjects: A Randomized Phase I Trial Abstract Abstract The objective of this study was to assess the effect of a high-fat meal on the pharmacokinetics of moxidectin. Healthy male subjects were randomized to receive single oral 8 mg... |
PMC12082735 | core_pubmed_pmc | Influential predictors of azithromycin pharmacokinetics: a systematic review of population pharmacokinetics | Influential predictors of azithromycin pharmacokinetics: a systematic review of population pharmacokinetics Abstract Abstract Introduction Azithromycin exhibits significant pharmacokinetic variability. Thus, dosage optimization is crucial for optimal therapeutic outcomes. This systematic review aims to analyze the popu... |
PMC12506886 | core_pubmed_pmc | Synthesis, biological evaluation, and docking analysis of novel benzimidazole–triazole hybrids as potential anticancer agents | Synthesis, biological evaluation, and docking analysis of novel benzimidazole–triazole hybrids as potential anticancer agents Abstract A series of novel benzimidazole–triazole acetamide hybrids with different substitutions at the acetamide moiety were designed and synthesized in an effort to discover potential anticanc... |
PMC9714297 | core_pubmed_pmc | Occupational health risk assessment methods in China: A scoping review | Occupational health risk assessment methods in China: A scoping review Abstract Abstract Background Over the decades, many assessment methods have been developed around the world and used for occupational health risk assessment (OHRA). This scoping review integrated the literature on methodological studies of OHRA in C... |
PMC4354323 | core_pubmed_pmc | Effects of Baicalin on Oral Pharmacokinetics of Caffeine in Rats | Effects of Baicalin on Oral Pharmacokinetics of Caffeine in Rats Abstract Scutellaria baicalensis is one of the most widely used herbal medicines in East Asia. Because baicalein and baicalin are major components of this herb, it is important to understand the effects of these compounds on drug metabolizing enzymes, suc... |
PMC11435260 | core_pubmed_pmc | Pharmacometrics to Evaluate Dosing of the Patient-Friendly Ivermectin CHILD-IVITAB in Children ≥ 15 kg and <15 kg | Pharmacometrics to Evaluate Dosing of the Patient-Friendly Ivermectin CHILD-IVITAB in Children ≥ 15 kg and <15 kg Abstract The antiparasitic drug ivermectin is approved for persons > 15 kg in the US and EU. A pharmacometric (PMX) population model with clinical PK data was developed (i) to characterize the effect of the... |
PMC6352406 | core_pubmed_pmc | Humanised effector-null FcγRIIA antibody inhibits immune complex-mediated proinflammatory responses | Humanised effector-null FcγRIIA antibody inhibits immune complex-mediated proinflammatory responses Abstract Abstract Objective Immune complexes (ICs) play a critical role in the pathology of autoimmune diseases. The aim of this study was to generate and characterise a first-in-class anti-FcγRIIA antibody (Ab) VIB9600 ... |
PMC6699521 | core_pubmed_pmc | Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment | Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment Abstract Introduction The intention of this work was to load olmesartan medoxomil (OLM), a sparsely water soluble antihypertensive bioactive with low oral... |
PMC4793306 | core_pubmed_pmc | Palatability and pharmacokinetics of flunixin when administered to sheep through feed | Palatability and pharmacokinetics of flunixin when administered to sheep through feed Abstract Applying analgesics to feed is a potentially easy method of providing pain-relief to sheep and lambs that undergo painful husbandry procedures. To be effective, the medicated feed needs to be readily accepted by sheep and its... |
PMC4744690 | core_pubmed_pmc | Pharmacodynamics and Pharmacokinetics of Fluticasone Furoate/Vilanterol in Healthy Chinese Subjects | Pharmacodynamics and Pharmacokinetics of Fluticasone Furoate/Vilanterol in Healthy Chinese Subjects Abstract Study Objective To investigate the pharmacodynamic and pharmacokinetic profiles of fluticasone furoate ( FF )/vilanterol ( VI ) – a fixed‐dose combination of an inhaled corticosteroid ( ICS ) and a long‐acting β... |
PMC6766783 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Tezepelumab ( AMG 157) in Healthy and Atopic Dermatitis Adult Subjects | Pharmacokinetics, Safety, and Tolerability of Tezepelumab ( AMG 157) in Healthy and Atopic Dermatitis Adult Subjects Abstract Tezepelumab ( AMG 157) is a monoclonal antibody that targets thymic stromal lymphopoietin and has shown benefits in treating asthma. We assessed the safety, tolerability, and pharmacokinetics of... |
PMC10632206 | core_pubmed_pmc | Pharmacokinetics and Safety of Eptinezumab in Healthy Chinese Participants: A Randomized Clinical Trial | Pharmacokinetics and Safety of Eptinezumab in Healthy Chinese Participants: A Randomized Clinical Trial Abstract Abstract Background and Objective Most evidence suggests that the pharmacokinetics of monoclonal antibodies (mAbs) are not meaningfully altered by patient characteristics, including racial/ethnic differences... |
PMC5551468 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics Evaluation of Tramadol in Thermoreversible Gels | Pharmacokinetics and Pharmacodynamics Evaluation of Tramadol in Thermoreversible Gels Abstract Abstract We evaluated pharmacokinetics (PK) and pharmacodynamics (PD) induced by new formulations of tramadol (TR) in thermoreversible gels. The poloxamer- (PL-) tramadol systems were prepared by direct dispersion of the drug... |
PMC11537990 | core_pubmed_pmc | Febuxostat-induced agranulocytosis in a pediatric hematopoietic stem cell transplant recipient: Case Report and literature review | Febuxostat-induced agranulocytosis in a pediatric hematopoietic stem cell transplant recipient: Case Report and literature review Abstract This report describes a pediatric case of isolated agranulocytosis occurring months after hematopoietic stem cell transplantation (HSCT). Secondary cytopenia, or secondary transplan... |
PMC8469431 | core_pubmed_pmc | Pre-Clinical Pharmacokinetic Characterization, Tissue Distribution, and Excretion Studies of Novel Edaravone Oral Prodrug, TEJ-1704 | Pre-Clinical Pharmacokinetic Characterization, Tissue Distribution, and Excretion Studies of Novel Edaravone Oral Prodrug, TEJ-1704 Abstract Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) is a free radical scavenger approved for the treatment of amyotrophic lateral sclerosis, a fatal neuromuscular disease. Edaravone i... |
PMC12854691 | core_pubmed_pmc | Design, synthesis, in vitro , and in silico studies on promising α-glucosidase inhibitors based on a quinazolinone–thiophene scaffold | Design, synthesis, in vitro , and in silico studies on promising α-glucosidase inhibitors based on a quinazolinone–thiophene scaffold Abstract Abstract To discover novel inhibitors for α-glucosidase, a new scaffold featuring a quinazolinone–thiophene skeleton was designed through molecular hybridization. Eighteen deriv... |
PMC12274659 | core_pubmed_pmc | Drug Exposure in Chronic Kidney Disease: It Is Not Just About the Glomerular Filtration Rate | Drug Exposure in Chronic Kidney Disease: It Is Not Just About the Glomerular Filtration Rate Abstract ABSTRACT Chronic kidney disease (CKD) affects over 10% of the world's population and is associated with high morbidity and mortality rates. The management of CKD is complex; CKD alters drug pharmacokinetics and pharmac... |
PMC12395723 | core_pubmed_pmc | In vivo pharmacokinetic and pharmacodynamic profiles of orbifloxacin against Staphylococcus aureus in a neutropenic murine thigh infection model | In vivo pharmacokinetic and pharmacodynamic profiles of orbifloxacin against Staphylococcus aureus in a neutropenic murine thigh infection model Abstract Background Orbifloxacin is a broad-spectrum fluoroquinolone antibiotic developed for veterinary use in the treatment of skin and soft tissue infections, as well as re... |
PMC5695027 | core_pubmed_pmc | Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats | Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats Abstract The purpose of this study was to evaluate the potential of micelle to change the pharmacokinetics of quercetin (QUT), with a primary goal of enhancing its oral bioavailability. QUT... |
PMC6446108 | core_pubmed_pmc | Pharmacokinetic and Bioavailability Studies of Embelin after Intravenous and Oral Administration to Rats | Pharmacokinetic and Bioavailability Studies of Embelin after Intravenous and Oral Administration to Rats Abstract Embelin exhibits the broad bioactivities such as antitumor, antifertility, antidiabetic, anti-inflammatory, antioxidant, anticonvulsant, anxiolytic, antimicrobial, and hepatoprotective activity. In order to... |
PMC8997238 | core_pubmed_pmc | Cannabis-Based Products in a Neurological Setting: A Clinical and Pharmacokinetic Survey | Cannabis-Based Products in a Neurological Setting: A Clinical and Pharmacokinetic Survey Abstract Background and Aim Limited data are available in clinical settings on the pharmacokinetics of delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). We investigated the use of cannabis-based products in neurological pra... |
PMC11916359 | core_pubmed_pmc | Dosing‐time contributes to chronotoxicity of clofarabine in mice via means other than pharmacokinetics | Dosing‐time contributes to chronotoxicity of clofarabine in mice via means other than pharmacokinetics Abstract Abstract To evaluate the time‐ and dose‐dependent toxicity of clofarabine in mice and to further define the chronotherapy strategy of it in leukemia, we compared the mortality rates, LD 50 s, biochemical para... |
PMC4163303 | core_pubmed_pmc | Pharmacokinetics of Two Alkaloids after Oral Administration of Rhizoma Coptidis Extract in Normal Rats and Irritable Bowel Syndrome Rats | Pharmacokinetics of Two Alkaloids after Oral Administration of Rhizoma Coptidis Extract in Normal Rats and Irritable Bowel Syndrome Rats Abstract Abstract A comparative pharmacokinetic study of berberine and palmatine after oral administration of Rhizoma Coptidis extract (96 mg/kg, containing berberine 22 mg/kg and pal... |
PMC12848320 | core_pubmed_pmc | Disposition and effects of alpha-pyrrolidinoisohexanophenone (α-PHiP) in comparison with cocaine: an observational study | Disposition and effects of alpha-pyrrolidinoisohexanophenone (α-PHiP) in comparison with cocaine: an observational study Abstract Abstract Introduction Alpha-pyrrolidinoisohexanophenone (α-PHiP) is a synthetic cathinone structurally related to alpha-pyrrolidinopentiophenone (α-PVP) and other pyrrolidinophenones, acting... |
PMC11583987 | core_pubmed_pmc | Randomized evaluation of the loss‐of‐function carboxylesterase 1 ( CES1 ) G143E variant on clopidogrel and ticagrelor pharmacodynamics | Randomized evaluation of the loss‐of‐function carboxylesterase 1 ( CES1 ) G143E variant on clopidogrel and ticagrelor pharmacodynamics Abstract Abstract Antiplatelet therapy with a P2Y 12 receptor inhibitor, in combination with aspirin, is standard of care for medical management of patients with coronary artery disease... |
PMC4676165 | core_pubmed_pmc | Epigenetic treatment of solid tumours: a review of clinical trials | Epigenetic treatment of solid tumours: a review of clinical trials Abstract Abstract Epigenetic treatment has been approved by regulatory agencies for haematological malignancies. The success observed in cutaneous lymphomas represents a proof of principle that similar results may be obtained in solid tumours. Several a... |
PMC4791858 | core_pubmed_pmc | Effect of mild medical hypothermia on in vitro growth of Plasmodium falciparum and the activity of anti-malarial drugs | Effect of mild medical hypothermia on in vitro growth of Plasmodium falciparum and the activity of anti-malarial drugs Abstract Abstract Background Cerebral malaria remains a medical emergency with high mortality. Hypo-perfusion due to obstructed blood vessels in the brain is thought to play a key role in the pathophys... |
PMC8360843 | core_pubmed_pmc | Biorelevant In Vitro Skin Permeation Testing and In Vivo Pharmacokinetic Characterization of Lidocaine from a Nonaqueous Drug-in-Matrix Topical System | Biorelevant In Vitro Skin Permeation Testing and In Vivo Pharmacokinetic Characterization of Lidocaine from a Nonaqueous Drug-in-Matrix Topical System Abstract Recently, lidocaine topical systems utilizing nonaqueous matrices have been developed and provide efficient lidocaine delivery through the skin, such that lower... |
PMC2890630 | core_pubmed_pmc | Pharmacokinetics of Linezolid and Ertapenem in experimental parapneumonic pleural effusion | Pharmacokinetics of Linezolid and Ertapenem in experimental parapneumonic pleural effusion Abstract Abstract Objective To determine the extent of linezolid and ertapenem penetration into the empyemic fluid using a rabbit model of empyema. Methods An empyema was created via the intrapleural injection of Escherichia coli... |
PMC6282495 | core_pubmed_pmc | Dipeptidyl Peptidase 1 Inhibitor AZD7986 Induces a Sustained, Exposure‐Dependent Reduction in Neutrophil Elastase Activity in Healthy Subjects | Dipeptidyl Peptidase 1 Inhibitor AZD7986 Induces a Sustained, Exposure‐Dependent Reduction in Neutrophil Elastase Activity in Healthy Subjects Abstract Abstract Neutrophil serine proteases (NSPs), such as neutrophil elastase (NE), are activated by dipeptidyl peptidase 1 (DPP1) during neutrophil maturation. High NSP lev... |
PMC4237545 | core_pubmed_pmc | Lixisenatide resensitizes the insulin-secretory response to intravenous glucose challenge in people with type 2 diabetes – a study in both people with type 2 diabetes and healthy subjects | Lixisenatide resensitizes the insulin-secretory response to intravenous glucose challenge in people with type 2 diabetes – a study in both people with type 2 diabetes and healthy subjects Abstract Aims Glucagon-like peptide-1 (GLP-1) receptor agonists improve blood glucose control by enhancing glucose-sensitive insulin... |
PMC8091820 | core_pubmed_pmc | Dosage strategies for delaying resistance emergence in heterogeneous tumors | Dosage strategies for delaying resistance emergence in heterogeneous tumors Abstract Abstract Drug resistance in cancer treatments is a frequent problem that, when it arises, leads to failure in therapeutic efforts. Tumor heterogeneity is the primary reason for resistance emergence and a precise treatment design that t... |
PMC9441929 | core_pubmed_pmc | What do we do now that the long-acting growth hormone is here? | What do we do now that the long-acting growth hormone is here? Abstract In standard 52-week phase III clinical trials, once weekly lonapegsomatropin, somatrogon and somapacitan have been found to yield non-inferior height velocities and similar safety profiles to daily GH (DGH) in children with pediatric growth hormone... |
PMC3558988 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics and efficacy of novel FabI inhibitor AFN-1252 against MSSA and MRSA in the murine thigh infection model | Pharmacokinetics, pharmacodynamics and efficacy of novel FabI inhibitor AFN-1252 against MSSA and MRSA in the murine thigh infection model Abstract Abstract AFN-1252, a new antimicrobial agent, specifically and potently inhibits fatty acid synthesis in Staphylococcus aureus . We characterized in vivo pharmacokinetic an... |
PMC10514552 | core_pubmed_pmc | Mim8, a novel factor VIIIa mimetic bispecific antibody, shows favorable safety and pharmacokinetics in healthy adults | Mim8, a novel factor VIIIa mimetic bispecific antibody, shows favorable safety and pharmacokinetics in healthy adults Abstract Abstract Background Mim8 (denecimig) is a novel activated coagulation factor VIII-mimetic bispecific antibody that assembles with activated coagulation FIX and FX on the platelet membrane surfa... |
PMC5971586 | core_pubmed_pmc | Pharmacokinetics of Intravenous Posaconazole in Critically Ill Patients | Pharmacokinetics of Intravenous Posaconazole in Critically Ill Patients Abstract ABSTRACT To date, there is no information on the intravenous (i.v.) posaconazole pharmacokinetics for intensive care unit (ICU) patients. This prospective observational study aimed to describe the pharmacokinetics of a single dose of i.v. ... |
PMC6680440 | core_pubmed_pmc | Effects of Gut Microbiota on the Bioavailability of Bioactive Compounds from Ginkgo Leaf Extracts | Effects of Gut Microbiota on the Bioavailability of Bioactive Compounds from Ginkgo Leaf Extracts Abstract Ginkgo leaf extract (GLE) is a popular herbal medicine and dietary supplement for the treatment of various diseases, including cardiovascular disease. GLE contains a variety of secondary plant metabolites, such as... |
PMC4965013 | core_pubmed_pmc | Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond | Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond Abstract A major cause of the paucity of new starting points for drug discovery is the lack of interaction between academia and industry. Much of the global resource in biology is present in universities, whereas the f... |
PMC8175879 | core_pubmed_pmc | Interpretation of volume kinetics in terms of pharmacokinetic principles | Interpretation of volume kinetics in terms of pharmacokinetic principles Abstract Abstract Volume kinetics is the pharmacokinetics of infusion fluids and describes the distribution and elimination of infused volume. Generally, pharmacokinetic parameters can be estimated by measuring the concentration of a drug. However... |
PMC7526406 | core_pubmed_pmc | Optimal regimens based on PK/PD cutoff evaluation of ceftiofur against Actinobacillus pleuropneumoniae in swine | Optimal regimens based on PK/PD cutoff evaluation of ceftiofur against Actinobacillus pleuropneumoniae in swine Abstract Abstract Background Actinobacillus pleuropneumoniae formerly known as Haemophilus pleuropneumoniae , can cause pleuropneumoniae in pigs, which lead to significant mortality. Ceftiofur was the first c... |
PMC11834528 | core_pubmed_pmc | Quantifying antibody binding: techniques and therapeutic implications | Quantifying antibody binding: techniques and therapeutic implications Abstract ABSTRACT The binding kinetics of an antibody for its target antigen represent key determinants of its biological function and success as a novel biotherapeutic. Defining these interactions and kinetics is critical for understanding the pharm... |
PMC8779982 | core_pubmed_pmc | FDA-Approved Oximes and Their Significance in Medicinal Chemistry | FDA-Approved Oximes and Their Significance in Medicinal Chemistry Abstract Despite the scientific advancements, organophosphate (OP) poisoning continues to be a major threat to humans, accounting for nearly one million poisoning cases every year leading to at least 20,000 deaths worldwide. Oximes represent the most imp... |
PMC7091414 | core_pubmed_pmc | Preclinical safety and efficacy of a new recombinant FIX drug product for treatment of hemophilia B | Preclinical safety and efficacy of a new recombinant FIX drug product for treatment of hemophilia B Abstract Baxter has developed a new recombinant factor IX (rFIX) drug product (BAX326) for treating patients with hemophilia B, or congenital FIX deficiency. An extensive preclinical program evaluated the pharmacokinetic... |
PMC6691757 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of Pelmeg ® , a pegfilgrastim biosimilar in healthy subjects | Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of Pelmeg ® , a pegfilgrastim biosimilar in healthy subjects Abstract Abstract A pharmacokinetics (PK)/pharmacodynamics (PD) study (EudraCT number 2015‐002966‐21) was conducted to investigate the biosimilarity of Pelmeg ® (pegfilgrastim), a biosimilar to EU... |
PMC9875447 | core_pubmed_pmc | Phosphorothioated amino-AS1411 aptamer functionalized stealth nanoliposome accelerates bio-therapeutic threshold of apigenin in neoplastic rat liver: a mechanistic approach | Phosphorothioated amino-AS1411 aptamer functionalized stealth nanoliposome accelerates bio-therapeutic threshold of apigenin in neoplastic rat liver: a mechanistic approach Abstract Abstract Hepatocellular carcinoma (HCC) is a leading cause of death globally. Even though the progressive invention of some very potent th... |
PMC12655633 | core_pubmed_pmc | Simultaneous Quantification of Multiple Analytes in Rat Plasma by UHPLC–MS/MS Following Oral Administration of Gastrodiae Rhizoma Extract for Pharmacokinetic Evaluation | Simultaneous Quantification of Multiple Analytes in Rat Plasma by UHPLC–MS/MS Following Oral Administration of Gastrodiae Rhizoma Extract for Pharmacokinetic Evaluation Abstract Abstract Gastrodiae Rhizoma (GR) is known to have a medicinal and food-based homology. It is used to treat infantile convulsion, epilepsy, spa... |
PMC12853717 | core_pubmed_pmc | Multiple linear regression modeling with values below a lower limit of quantification – a statistical method comparison | Multiple linear regression modeling with values below a lower limit of quantification – a statistical method comparison Abstract Background Missing values occur in almost all real-world medical data. Sometimes, more information is available for the missing values due to technical measurement limits. This was also the c... |
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