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PMC9784770
core_pubmed_pmc
Development of an Oral Isoliquiritigenin Self-Nano-Emulsifying Drug Delivery System (ILQ-SNEDDS) for Effective Treatment of Eosinophilic Esophagitis Induced by Food Allergy
Development of an Oral Isoliquiritigenin Self-Nano-Emulsifying Drug Delivery System (ILQ-SNEDDS) for Effective Treatment of Eosinophilic Esophagitis Induced by Food Allergy Abstract Abstract Isoliquiritigenin (ILQ) is a natural flavonoid with various pharmacological activities. In this study, we optimized the preparati...
PMC4452035
core_pubmed_pmc
Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag
Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag Abstract Purpose Targeting the prostacyclin pathway is an effective treatment option for pulmonary arterial hypertension (PAH). Patients with PAH have a deficiency of prostacyclin and prostacyclin synthase. Selexipag is an or...
PMC6153548
core_pubmed_pmc
Safety, tolerability, and preliminary activity of IMGN529, a CD37-targeted antibody-drug conjugate, in patients with relapsed or refractory B-cell non-Hodgkin lymphoma: a dose-escalation, phase I study
Safety, tolerability, and preliminary activity of IMGN529, a CD37-targeted antibody-drug conjugate, in patients with relapsed or refractory B-cell non-Hodgkin lymphoma: a dose-escalation, phase I study Abstract Summary Background CD37 is expressed on B-cell lymphoid malignancies, thus making it an attractive candidate ...
PMC10951188
core_pubmed_pmc
Population Pharmacokinetic Analysis to Support and Facilitate Switching from Risperidone Formulations to Rykindo in Patients with Schizophrenia
Population Pharmacokinetic Analysis to Support and Facilitate Switching from Risperidone Formulations to Rykindo in Patients with Schizophrenia Abstract Abstract Introduction RYKINDO® (Rykindo) is a novel, long-acting injectable risperidone formulation administered biweekly (Q2W) through intramuscular gluteal injection...
PMC5306145
core_pubmed_pmc
Impact of saturable distribution in compartmental PK models: dynamics and practical use
Impact of saturable distribution in compartmental PK models: dynamics and practical use Abstract We explore the impact of saturable distribution over the central and the peripheral compartment in pharmacokinetic models, whilst assuming that back flow into the central compartiment is linear. Using simulations and analyt...
PMC6449574
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In vivo pharmacodynamics of lefamulin, the first systemic pleuromutilin for human use, in a neutropenic murine thigh infection model
In vivo pharmacodynamics of lefamulin, the first systemic pleuromutilin for human use, in a neutropenic murine thigh infection model Abstract Abstract Objectives To characterize the pharmacokinetics (PK) and pharmacodynamics (PD) of lefamulin in the neutropenic murine thigh infection model to ascertain (i) which PK/PD ...
PMC8658697
core_pubmed_pmc
Managing the Unpredictable: Mechanistic Analysis and Clinical Recommendations for Lamotrigine Treatment after Bariatric Surgery
Managing the Unpredictable: Mechanistic Analysis and Clinical Recommendations for Lamotrigine Treatment after Bariatric Surgery Abstract Abstract Bariatric surgery may alter the absorption and overall bioavailability of oral drugs. Lamotrigine is a major antiepileptic and mood stabilizer, that its use after bariatric s...
PMC10223580
core_pubmed_pmc
Benzisothiazolinone: Pharmacokinetics, Tissue Distribution, and Mass Balance Studies in Rats
Benzisothiazolinone: Pharmacokinetics, Tissue Distribution, and Mass Balance Studies in Rats Abstract Humans are continuously exposed to benzisothiazolinone (BIT), which is used as a preservative, through multiple routes. BIT is known to be a sensitizer; in particular, dermal contact or aerosol inhalation could affect ...
PMC12028845
core_pubmed_pmc
Exploring the In Vivo Fate of β-1, 3/1, 6-Glucan Using Quantitative Tandem Mass Spectrometry Based on a Structure-Specific Fragment
Exploring the In Vivo Fate of β-1, 3/1, 6-Glucan Using Quantitative Tandem Mass Spectrometry Based on a Structure-Specific Fragment Abstract Abstract β-glucan, a promising drug candidate for immuno-antitumor therapy, holds tremendous potential for clinical applications. However, the absence of highly sensitive quantita...
PMC12676308
core_pubmed_pmc
A Validated LC–MS/MS Method for the Determination of Sulindac and Its Metabolite Su-EP‑C in Human Plasma and Their Pharmacokinetic Application in Healthy Volunteers
A Validated LC–MS/MS Method for the Determination of Sulindac and Its Metabolite Su-EP‑C in Human Plasma and Their Pharmacokinetic Application in Healthy Volunteers Abstract A rapid, specific, and sensitive LC–MS/MS method for the determination of sulindac and its metabolite Su-EP-C in human EDTA-K2 plasma was develope...
PMC12245748
core_pubmed_pmc
Prophylaxis of Gout Flares in Patients with Renal Impairment: Dosing Adjustments with Colchicine Oral Solution Informed by a Pharmacokinetic Model
Prophylaxis of Gout Flares in Patients with Renal Impairment: Dosing Adjustments with Colchicine Oral Solution Informed by a Pharmacokinetic Model Abstract Abstract Introduction Patients receiving the standard prophylaxis dose of colchicine for gout flares are at increased risk for developing toxicity if there are pre-...
PMC9114261
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An Introduction to Biosimilars for the Treatment of Retinal Diseases: A Narrative Review
An Introduction to Biosimilars for the Treatment of Retinal Diseases: A Narrative Review Abstract Biological therapies have revolutionized the treatment of disease across a number of therapeutic areas including retinal diseases. However, on occasion, such treatments may be relatively more expensive compared to small mo...
PMC7020547
core_pubmed_pmc
The gender-related variability in the pharmacokinetics and antiplasmodial activity of naphthoquine in rodents
The gender-related variability in the pharmacokinetics and antiplasmodial activity of naphthoquine in rodents Abstract Abstract Background Naphthoquine (NQ) is a suitable partner anti-malarial for the artemisinin-based combination therapy (ACT), which is recommended to be taken orally as a single-dose regimen. The meta...
PMC12024218
core_pubmed_pmc
Efficacy of Ceftobiprole and Daptomycin at Bone Concentrations Against Methicillin-Resistant Staphylococcus aureus Biofilm: Results of a Dynamic In Vitro PK/PD Model
Efficacy of Ceftobiprole and Daptomycin at Bone Concentrations Against Methicillin-Resistant Staphylococcus aureus Biofilm: Results of a Dynamic In Vitro PK/PD Model Abstract Abstract Background : The presence of biofilms and low antimicrobial concentrations in bone tissue make prosthetic joint infections (PJI) difficu...
PMC8650113
core_pubmed_pmc
Clinical Validation of a Volumetric Absorptive Micro-Sampling Device for Pharmacokinetic Studies With Tranexamic Acid
Clinical Validation of a Volumetric Absorptive Micro-Sampling Device for Pharmacokinetic Studies With Tranexamic Acid Abstract We assessed the accuracy of tranexamic acid (TXA) concentrations measured in capillary whole blood using volumetric absorptive micro-sampling (VAMS) devices. Paired venous and VAMS capillary bl...
PMC8918863
core_pubmed_pmc
Single-treatment tumor ablation with photodynamic liposomal irinotecan sucrosulfate
Single-treatment tumor ablation with photodynamic liposomal irinotecan sucrosulfate Abstract Highlights • A liposomal formulation of irinotecan that contains a non-exchangeable, embedded photosensitizer gives rise to enhanced serum stability and rapid light-triggered release when sucrosulfate is used as a trapping agen...
PMC10991832
core_pubmed_pmc
Phase 1, first-in-human study of TYRP1-TCB (RO7293583), a novel TYRP1-targeting CD3 T-cell engager, in metastatic melanoma: active drug monitoring to assess the impact of immune response on drug exposure
Phase 1, first-in-human study of TYRP1-TCB (RO7293583), a novel TYRP1-targeting CD3 T-cell engager, in metastatic melanoma: active drug monitoring to assess the impact of immune response on drug exposure Abstract Introduction Although checkpoint inhibitors (CPIs) have improved outcomes for patients with metastatic mela...
PMC3818833
core_pubmed_pmc
Clinical Pharmacology of Furosemide in Neonates: A Review
Clinical Pharmacology of Furosemide in Neonates: A Review Abstract Furosemide is the diuretic most used in newborn infants. It blocks the Na + -K + -2Cl − symporter in the thick ascending limb of the loop of Henle increasing urinary excretion of Na + and Cl − . This article aimed to review the published data on the cli...
PMC5312726
core_pubmed_pmc
Pharmacokinetics, efficacy, and safety of a plasma-derived VWF/FVIII concentrate (VONCENTO) for on-demand and prophylactic treatment in patients with von Willebrand disease (SWIFT-VWD study)
Pharmacokinetics, efficacy, and safety of a plasma-derived VWF/FVIII concentrate (VONCENTO) for on-demand and prophylactic treatment in patients with von Willebrand disease (SWIFT-VWD study) Abstract Supplemental Digital Content is available in the text Keywords: annual bleeding rate, haemostatic efficacy, haemostatic ...
PMC12226763
core_pubmed_pmc
A probabilistic model of behavioural emergence from general anaesthesia in mice
A probabilistic model of behavioural emergence from general anaesthesia in mice Abstract Abstract Background Time to emergence from general anaesthesia is highly variable between individuals. This variability has been attributed to individual differences in anaesthetic sensitivity. However, this hypothesis has not been...
PMC9441481
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Risk assessment and molecular mechanism study of drug-drug interactions between rivaroxaban and tyrosine kinase inhibitors mediated by CYP2J2/3A4 and BCRP/P-gp
Risk assessment and molecular mechanism study of drug-drug interactions between rivaroxaban and tyrosine kinase inhibitors mediated by CYP2J2/3A4 and BCRP/P-gp Abstract Cancer patients generally has a high risk of thrombotic diseases. However, anticoagulant therapy always aggravates bleeding risks. Rivaroxaban is one o...
PMC9823043
core_pubmed_pmc
Population Pharmacokinetic–Pharmacodynamic Modeling and Probability of Target Attainment Analysis of Rocuronium and Sugammadex in Children Undergoing Surgery
Population Pharmacokinetic–Pharmacodynamic Modeling and Probability of Target Attainment Analysis of Rocuronium and Sugammadex in Children Undergoing Surgery Abstract Background and Objectives Probability of target attainment (PTA) curves are commonly used to support dose recommendations of antibiotics for different pa...
PMC12913916
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In vitro inhibitory effects of gentamicin and ceftiofur against Trypanosoma evansi : Promising antibiotic alternatives for equine trypanosomosis in Thailand
In vitro inhibitory effects of gentamicin and ceftiofur against Trypanosoma evansi : Promising antibiotic alternatives for equine trypanosomosis in Thailand Abstract ABSTRACT Background and Aim: Trypanosoma evansi infection (Surra) remains a major constraint to equine health and productivity in Thailand. The only avail...
PMC11267250
core_pubmed_pmc
Cinnamaldehyde: Pharmacokinetics, anticancer properties and therapeutic potential (Review)
Cinnamaldehyde: Pharmacokinetics, anticancer properties and therapeutic potential (Review) Abstract Cancer incidence is increasing globally, presenting a growing public health challenge. While anticancer drugs are crucial in treatment, their limitations, including poor targeting ability and high toxicity, hinder effect...
PMC6601554
core_pubmed_pmc
Neonatal Fc receptor expression in macrophages is indispensable for IgG homeostasis
Neonatal Fc receptor expression in macrophages is indispensable for IgG homeostasis Abstract ABSTRACT The maintenance of the homeostasis of immunoglobulin G (IgG) represents a fundamental aspect of humoral immunity that has direct relevance to the successful delivery of antibody-based therapeutics. The ubiquitously exp...
PMC11494130
core_pubmed_pmc
Study on bioequivalence and influence of obesity-related indicators on pharmacokinetics and pharmacodynamics for insulin degludec in healthy subjects
Study on bioequivalence and influence of obesity-related indicators on pharmacokinetics and pharmacodynamics for insulin degludec in healthy subjects Abstract Abstract This study aimed to evaluate the bioequivalence between test and reference insulin degludec (IDeg) and the effects of body composition on pharmacokineti...
PMC10434993
core_pubmed_pmc
Integrated transcriptomic and metabolomic profiles reveal the protective mechanism of modified Danggui Buxue decoction on radiation-induced leukopenia in mice
Integrated transcriptomic and metabolomic profiles reveal the protective mechanism of modified Danggui Buxue decoction on radiation-induced leukopenia in mice Abstract Leukopenia caused by radiation hinders the continuous treatment of cancers. Danggui Buxue Decoction (DBD) has been widely used in clinical owing to low ...
PMC9441576
core_pubmed_pmc
Cytochrome P450-mediated antiseizure medication interactions influence apoptosis, modulate the brain BAX/Bcl-X L ratio and aggravate mitochondrial stressors in human pharmacoresistant epilepsy
Cytochrome P450-mediated antiseizure medication interactions influence apoptosis, modulate the brain BAX/Bcl-X L ratio and aggravate mitochondrial stressors in human pharmacoresistant epilepsy Abstract Abstract Polytherapy with antiseizure medications (ASMs) is often used to control seizures in patients suffering from ...
PMC11224448
core_pubmed_pmc
Exploring the pharmacokinetics and tolerability of cyclooxygenase inhibitor ampiroxicam: a phase I study on single and multiple oral doses
Exploring the pharmacokinetics and tolerability of cyclooxygenase inhibitor ampiroxicam: a phase I study on single and multiple oral doses Abstract Introduction: Ampiroxicam is a long-acting, non-steroidal anti-inflammatory drug that selectively inhibits human cyclooxygenase, effectively mitigating fever, pain, and inf...
PMC3431551
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Potential Effects of Chlorpyrifos on Fetal Growth Outcomes: Implications for Risk Assessment
Potential Effects of Chlorpyrifos on Fetal Growth Outcomes: Implications for Risk Assessment Abstract Abstract Chlorpyrifos (CPF) is one of the most widely used organophosphate insecticides in the United States. By December 2000, nearly all residential uses were voluntarily canceled, so that today, CPF is only used to ...
PMC5219696
core_pubmed_pmc
Optimal dosage of cefmetazole for intraoperative antimicrobial prophylaxis in patients undergoing surgery for colorectal cancer
Optimal dosage of cefmetazole for intraoperative antimicrobial prophylaxis in patients undergoing surgery for colorectal cancer Abstract Background Few studies have reported the dosage of cefmetazole (CMZ) for intraoperative antimicrobial prophylaxis in patients underwent surgery for colorectal cancer. We therefore exa...
PMC9866112
core_pubmed_pmc
Chetomin, a SARS-CoV-2 3C-like Protease (3CL pro ) Inhibitor: In Silico Screening, Enzyme Docking, Molecular Dynamics and Pharmacokinetics Analysis
Chetomin, a SARS-CoV-2 3C-like Protease (3CL pro ) Inhibitor: In Silico Screening, Enzyme Docking, Molecular Dynamics and Pharmacokinetics Analysis Abstract The emergence of the Coronavirus Disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has led to over 6 million ...
PMC11570272
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Leveraging long-acting IL-15 agonists for intratumoral delivery and enhanced antimetastatic activity
Leveraging long-acting IL-15 agonists for intratumoral delivery and enhanced antimetastatic activity Abstract Introduction IL-15 agonists hold promise as immunotherapeutics due to their ability to induce the proliferation and expansion of cytotoxic immune cells including natural killer (NK) and CD8 + T cells. However, ...
PMC9427151
core_pubmed_pmc
Randomized Trial of Metformin With Anti-Tuberculosis Drugs for Early Sputum Conversion in Adults With Pulmonary Tuberculosis
Randomized Trial of Metformin With Anti-Tuberculosis Drugs for Early Sputum Conversion in Adults With Pulmonary Tuberculosis Abstract Abstract Background Metformin, by reducing intracellular Mycobacterium tuberculosis growth, can be considered an adjunctive therapy to anti-tuberculosis treatment (ATT). We determined wh...
PMC9305466
core_pubmed_pmc
Exposure‐response relationships for the efficacy and safety of filgotinib and its metabolite GS‐829845 in subjects with rheumatoid arthritis based on phase 2 and phase 3 studies
Exposure‐response relationships for the efficacy and safety of filgotinib and its metabolite GS‐829845 in subjects with rheumatoid arthritis based on phase 2 and phase 3 studies Abstract Aims Filgotinib is a potent, oral, JAK1‐preferential inhibitor for the treatment of rheumatoid arthritis (RA). This report describes ...
PMC5698573
core_pubmed_pmc
Population pharmacokinetic meta‐analysis of ramucirumab in cancer patients
Population pharmacokinetic meta‐analysis of ramucirumab in cancer patients Abstract Abstract Aims Ramucirumab is a human IgG1 monoclonal antibody that specifically binds vascular endothelial growth factor receptor‐2 (VEGFR‐2) and blocks binding of VEGF‐A, VEGF‐C and VEGF‐D. The objective of the analysis was to characte...
PMC8679136
core_pubmed_pmc
Serum etanercept concentrations in relation to disease activity and treatment response assessed by ultrasound, biomarkers and clinical disease activity scores: results from a prospective observational study of patients with rheumatoid arthritis
Serum etanercept concentrations in relation to disease activity and treatment response assessed by ultrasound, biomarkers and clinical disease activity scores: results from a prospective observational study of patients with rheumatoid arthritis Abstract Abstract Objectives To identify the therapeutic range for etanerce...
PMC8932710
core_pubmed_pmc
Optimizing moxidectin dosing for Strongyloides stercoralis infections: Insights from pharmacometric modeling
Optimizing moxidectin dosing for Strongyloides stercoralis infections: Insights from pharmacometric modeling Abstract Abstract Moxidectin is a frontrunner drug candidate in the treatment of strongyloidiasis. A dose of 8 mg is recommended to treat this indication, which shows a reasonably good efficacy and tolerability ...
PMC9465605
core_pubmed_pmc
Investigating brain uptake of a non-targeting monoclonal antibody after intravenous and intracerebroventricular administration
Investigating brain uptake of a non-targeting monoclonal antibody after intravenous and intracerebroventricular administration Abstract Abstract Monoclonal antibodies play an important role in the treatment of various diseases. However, the development of these drugs against neurological disorders where the drug target...
PMC7409122
core_pubmed_pmc
Rapid and Sensitive Quantification of Osimertinib in Human Plasma Using a Fully Validated MALDI–IM–MS/MS Assay
Rapid and Sensitive Quantification of Osimertinib in Human Plasma Using a Fully Validated MALDI–IM–MS/MS Assay Abstract Abstract The third-generation tyrosine kinase inhibitor (TKI), osimertinib, has revolutionized the treatment of patients with non-small cell lung carcinoma with epidermal growth factor receptor (EGFR)...
PMC10043960
core_pubmed_pmc
Identification of RdRp inhibitors against SARS-CoV-2 through E-pharmacophore-based virtual screening, molecular docking and MD simulations approaches
Identification of RdRp inhibitors against SARS-CoV-2 through E-pharmacophore-based virtual screening, molecular docking and MD simulations approaches Abstract Abstract The outbreak of novel Coronavirus, an enduring pandemic declared by WHO, has consequences to an alarming ongoing public health menace which has already ...
PMC11651187
core_pubmed_pmc
Subcutaneous ocrelizumab in multiple sclerosis: Results of the Phase 1b OCARINA I study
Subcutaneous ocrelizumab in multiple sclerosis: Results of the Phase 1b OCARINA I study Abstract Abstract Objective Subcutaneous ocrelizumab is being developed to provide treatment flexibility and additional choice to patients with multiple sclerosis. OCARINA I ( NCT03972306 ) is an open‐label, multicenter, Phase 1b, d...
PMC2955962
core_pubmed_pmc
Single-Dose Pharmacokinetics of Fentanyl Buccal Soluble Film
Single-Dose Pharmacokinetics of Fentanyl Buccal Soluble Film Abstract Abstract Objective The objectives of the study were to determine the absolute bioavailability of fentanyl from fentanyl buccal soluble film, estimate the percentage of a fentanyl dose absorbed through the buccal mucosa, and compare the bioavailabilit...
PMC9442038
core_pubmed_pmc
Pharmacokinetics of baicalin and oroxyloside in plasma and different tissues of rats after transnasal aerosol inhalation and intravenous injection of Tanreqing
Pharmacokinetics of baicalin and oroxyloside in plasma and different tissues of rats after transnasal aerosol inhalation and intravenous injection of Tanreqing Abstract To avoid adverse drug reactions associated with injection, off-label nebulization of Tanreqing (TRQ) injection is often used in China to treat respirat...
PMC7566410
core_pubmed_pmc
Characterizing the non-linear pharmacokinetics of miltefosine in paediatric visceral leishmaniasis patients from Eastern Africa
Characterizing the non-linear pharmacokinetics of miltefosine in paediatric visceral leishmaniasis patients from Eastern Africa Abstract Abstract Background Conventional miltefosine dosing (2.5 mg/kg/day) for treatment of visceral leishmaniasis (VL) is less effective in children than in adults. A higher allometric dose...
PMC6018554
core_pubmed_pmc
2-[2-(4-(trifluoromethyl)phenylamino)thiazol-4-yl]acetic acid (Activator-3) is a potent activator of AMPK
2-[2-(4-(trifluoromethyl)phenylamino)thiazol-4-yl]acetic acid (Activator-3) is a potent activator of AMPK Abstract AMPK is considered as a potential high value target for metabolic disorders. Here, we present the molecular modeling, in vitro and in vivo characterization of Activator-3, 2-[2-(4-(trifluoromethyl)phenylam...
PMC4618644
core_pubmed_pmc
Interrogating the relationship between rat in vivo tissue distribution and drug property data for >200 structurally unrelated molecules
Interrogating the relationship between rat in vivo tissue distribution and drug property data for >200 structurally unrelated molecules Abstract The ability to explain distribution patterns from drug physicochemical properties and binding characteristics has been explored for more than 200 compounds by interrogating da...
PMC7591012
core_pubmed_pmc
Repurposing Drugs for COVID-19: Pharmacokinetics and Pharmacogenomics of Chloroquine and Hydroxychloroquine
Repurposing Drugs for COVID-19: Pharmacokinetics and Pharmacogenomics of Chloroquine and Hydroxychloroquine Abstract Background A new coronavirus SARS-CoV-2 has been identified as the etiological agent of the severe acute respiratory syndrome, COVID-19, the source and cause of the 2019–20 coronavirus pandemic. Hydroxyc...
PMC11311427
core_pubmed_pmc
Determinants of Interpatient Variability in Treosulfan Pharmacokinetics in AML Patients Undergoing Autologous Stem Cell Transplantation
Determinants of Interpatient Variability in Treosulfan Pharmacokinetics in AML Patients Undergoing Autologous Stem Cell Transplantation Abstract Limited data on treosulfan pharmacokinetics in adults, particularly regarding autologous stem cell transplantation (ASCT) in acute myeloid leukemia (AML), is available to date...
PMC12859171
core_pubmed_pmc
Pharmacokinetics and Customized Dosing of Vancomycin in Adult Patients With Hematological Malignancies: Status, Challenges, and Opportunities
Pharmacokinetics and Customized Dosing of Vancomycin in Adult Patients With Hematological Malignancies: Status, Challenges, and Opportunities Abstract ABSTRACT Vancomycin (VAN) remains the first‐line treatment for methicillin‐resistant, multidrug‐resistant gram‐positive bacterial infections, even among cancer patients....
PMC8974913
core_pubmed_pmc
Therapeutic Drug Monitoring of Anti-Thymocyte Globulin in Allogeneic Stem Cell Transplantation: Proof of Concept
Therapeutic Drug Monitoring of Anti-Thymocyte Globulin in Allogeneic Stem Cell Transplantation: Proof of Concept Abstract Anti-thymocyte globulin (ATG), a polyclonal antibody, is used in allogeneic hematopoietic cell transplantation (HCT) to prevent graft-vs.-host-disease (GvHD) and graft failure (GF). Overexposure to ...
PMC11706424
core_pubmed_pmc
Population pharmacokinetics and pharmacodynamics of edoxaban in pediatric patients
Population pharmacokinetics and pharmacodynamics of edoxaban in pediatric patients Abstract Abstract Edoxaban is an orally active inhibitor of activated factor X (FXa). Population pharmacokinetic (PK) and pharmacodynamic (PD) analyses were performed to characterize the PK and PK–PD relationships of edoxaban in pediatri...
PMC6471205
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics Modeling and Simulation Systems to Support the Development and Regulation of Liposomal Drugs
Pharmacokinetics and Pharmacodynamics Modeling and Simulation Systems to Support the Development and Regulation of Liposomal Drugs Abstract Liposomal formulations have been developed to improve the therapeutic index of encapsulated drugs by altering the balance of on- and off-targeted distribution. The improved therape...
PMC5345807
core_pubmed_pmc
Formulation and PEGylation optimization of the therapeutic PEGylated phenylalanine ammonia lyase for the treatment of phenylketonuria
Formulation and PEGylation optimization of the therapeutic PEGylated phenylalanine ammonia lyase for the treatment of phenylketonuria Abstract Phenylketonuria (PKU) is a genetic metabolic disease in which the decrease or loss of phenylalanine hydroxylase (PAH) activity results in elevated, neurotoxic levels of phenylal...
PMC4089556
core_pubmed_pmc
Systems biology modeling of omics data: effect of cyclosporine a on the Nrf2 pathway in human renal cells
Systems biology modeling of omics data: effect of cyclosporine a on the Nrf2 pathway in human renal cells Abstract Background Incorporation of omic data streams for building improved systems biology models has great potential for improving their predictions of biological outcomes. We have recently shown that cyclospori...
PMC11577668
core_pubmed_pmc
The relation between inflammatory biomarkers and drug pharmacokinetics in the critically ill patients: a scoping review
The relation between inflammatory biomarkers and drug pharmacokinetics in the critically ill patients: a scoping review Abstract Background The level of inflammation alters drug pharmacokinetics (PK) in critically ill patients. This might compromise treatment efficacy. Understanding the specific effects of inflammation...
PMC8152995
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Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010–2020 Review
Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010–2020 Review Abstract Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a curable airborne disease currently treated using a drug regimen consisting of four drugs. Global TB control has bee...
PMC2835511
core_pubmed_pmc
Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations
Pharmacokinetics of oseltamivir: an oral antiviral for the treatment and prophylaxis of influenza in diverse populations Abstract Abstract Influenza is a transmissible viral pathogen that continues to cause substantial morbidity and mortality. Oseltamivir is an orally administered antiviral medication that selectively ...
PMC10366144
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Computational reactive–diffusive modeling for stratification and prognosis determination of patients with breast cancer receiving Olaparib
Computational reactive–diffusive modeling for stratification and prognosis determination of patients with breast cancer receiving Olaparib Abstract Abstract Mathematical models based on partial differential equations (PDEs) can be exploited to handle clinical data with space/time dimensions, e.g. tumor growth challenge...
PMC6767014
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Catalpol in Diabetes and its Complications: A Review of Pharmacology, Pharmacokinetics, and Safety
Catalpol in Diabetes and its Complications: A Review of Pharmacology, Pharmacokinetics, and Safety Abstract Abstract This review aimed to provide a general view of catalpol in protection against diabetes and diabetic complications, as well as its pharmacokinetics and safety concerns. The following databases were consul...
PMC12104602
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Efficacy and safety of rituximab biosimilar (DRL_RI) versus MabThera ® in low-tumor-burden follicular lymphoma: the FLINTER study
Efficacy and safety of rituximab biosimilar (DRL_RI) versus MabThera ® in low-tumor-burden follicular lymphoma: the FLINTER study Abstract Abstract Background and objectives: This phase III study (RI-01-006; FLINTER) was conducted to demonstrate equivalent efficacy of DRL_RI to EU-approved rituximab (MabThera ® ) in pa...
PMC11920723
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Pharmacokinetics of Milbemycin Oxime in Pekingese Dogs after Single Oral and Intravenous Administration
Pharmacokinetics of Milbemycin Oxime in Pekingese Dogs after Single Oral and Intravenous Administration Abstract ABSTRACT Objective This study aimed to characterize the pharmacokinetic profiles of milbemycin oxime in Pekingese dogs following a single oral (PO) and intravenous (IV) dose. Six clinically healthy Pekingese...
PMC4032641
core_pubmed_pmc
An evaluation of the potential for drug–drug interactions between bendamustine and rituximab in indolent non-Hodgkin lymphoma and mantle cell lymphoma
An evaluation of the potential for drug–drug interactions between bendamustine and rituximab in indolent non-Hodgkin lymphoma and mantle cell lymphoma Abstract Purpose Bendamustine plus rituximab has been reported to be effective in treating lymphoid malignancies. This analysis investigated the potential for drug–drug ...
PMC12558648
core_pubmed_pmc
Haemodynamic Changes After Prophylactic Doses of Ephedrine, Phenylephrine, Norepinephrine Versus Placebo During Induction of General Anaesthesia: A Randomised Trial
Haemodynamic Changes After Prophylactic Doses of Ephedrine, Phenylephrine, Norepinephrine Versus Placebo During Induction of General Anaesthesia: A Randomised Trial Abstract ABSTRACT Background Ephedrine, phenylephrine, and norepinephrine are commonly used to manage hypotension during the induction of anaesthesia. The ...
PMC5188417
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Effect of Tea Polyphenol Compounds on Anticancer Drugs in Terms of Anti-Tumor Activity, Toxicology, and Pharmacokinetics
Effect of Tea Polyphenol Compounds on Anticancer Drugs in Terms of Anti-Tumor Activity, Toxicology, and Pharmacokinetics Abstract Multidrug resistance and various adverse side effects have long been major problems in cancer chemotherapy. Recently, chemotherapy has gradually transitioned from mono-substance therapy to m...
PMC11358572
core_pubmed_pmc
Validation of the C-X-C chemokine receptor 3 (CXCR3) as a target for PET imaging of T cell activation
Validation of the C-X-C chemokine receptor 3 (CXCR3) as a target for PET imaging of T cell activation Abstract Abstract Purpose CXCR3 is expressed on activated T cells and plays a crucial role in T-cell recruitment to the tumor microenvironment (TME) during cell-based and immune checkpoint inhibitor (ICI) immunotherapy...
PMC6927769
core_pubmed_pmc
Development of a quantitative relationship between CAR-affinity, antigen abundance, tumor cell depletion and CAR-T cell expansion using a multiscale systems PK-PD model
Development of a quantitative relationship between CAR-affinity, antigen abundance, tumor cell depletion and CAR-T cell expansion using a multiscale systems PK-PD model Abstract ABSTRACT The development of mechanism-based, multiscale pharmacokinetic–pharmacodynamic (PK-PD) models for chimeric antigen receptor (CAR)-T c...
PMC2817937
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Management of hyperuricemia in gout: focus on febuxostat
Management of hyperuricemia in gout: focus on febuxostat Abstract Abstract Gout is the most common inflammatory arthritis in an elderly population, and can be diagnosed with absolute certainty by polarization microscopy. However, diagnosis may be challenging because atypical presentations are more common in the elderly...
PMC10451047
core_pubmed_pmc
A review of evidence, antimicrobial stability, and feasibility considerations for OPAT continuous infusion
A review of evidence, antimicrobial stability, and feasibility considerations for OPAT continuous infusion Abstract Abstract Outpatient parenteral antimicrobial therapy (OPAT) has been widely used in clinical practice for many decades because of its associated cost savings, reductions in inpatient hospital days, and de...
PMC11267906
core_pubmed_pmc
Development of an eco-friendly capillary electrophoresis method for the simultaneous determination of piperacillin, tazobactam and ibuprofen in plasma samples: application to a pharmacokinetic study in rats
Development of an eco-friendly capillary electrophoresis method for the simultaneous determination of piperacillin, tazobactam and ibuprofen in plasma samples: application to a pharmacokinetic study in rats Abstract Abstract Piperacillin (PIP) and tazobactam (TAZ) are broad-spectrum beta-lactam antimicrobial agents, wh...
PMC12374684
core_pubmed_pmc
Acute High Dose Melatonin for Encephalopathy of the Newborn (ACUMEN) Study: a protocol for a multicentre phase 1 safety trial of melatonin to augment therapeutic hypothermia for moderate/severe hypoxic ischaemic encephalopathy
Acute High Dose Melatonin for Encephalopathy of the Newborn (ACUMEN) Study: a protocol for a multicentre phase 1 safety trial of melatonin to augment therapeutic hypothermia for moderate/severe hypoxic ischaemic encephalopathy Abstract Abstract Introduction Neonatal death and later disability remain common sequelae of ...
PMC8082684
core_pubmed_pmc
Hepatic Cytochrome P450 Abundance and Activity in the Developing and Adult Göttingen Minipig: Pivotal Data for PBPK Modeling
Hepatic Cytochrome P450 Abundance and Activity in the Developing and Adult Göttingen Minipig: Pivotal Data for PBPK Modeling Abstract The Göttingen Minipig is gaining ground as nonrodent species in safety testing of drugs for pediatric indications. Due to developmental changes in pharmacokinetics and pharmacodynamics, ...
PMC11622436
core_pubmed_pmc
Pyrazinamide Safety, Efficacy, and Dosing for Treating Drug-Susceptible Pulmonary Tuberculosis: A Phase 3, Randomized Controlled Clinical Trial
Pyrazinamide Safety, Efficacy, and Dosing for Treating Drug-Susceptible Pulmonary Tuberculosis: A Phase 3, Randomized Controlled Clinical Trial Abstract Abstract Rationale Optimizing pyrazinamide dosing is critical to improve treatment efficacy while minimizing toxicity during tuberculosis treatment. Study 31/AIDS Clin...
PMC11836603
core_pubmed_pmc
Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition
Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition Abstract Abstract The benzodiazines (phthalazine, quinazoline, quinoxaline, and cinnoline) have emerged as attractive scaffolds for creating novel anticancer drugs. These nitrogen-containing heterocycles are intriguing because...
PMC9291057
core_pubmed_pmc
Safety, pharmacokinetics and quantitative EEG modulation of TAK‐071, a novel muscarinic M1 receptor positive allosteric modulator, in healthy subjects
Safety, pharmacokinetics and quantitative EEG modulation of TAK‐071, a novel muscarinic M1 receptor positive allosteric modulator, in healthy subjects Abstract Abstract Aims TAK‐071 is a muscarinic M 1 receptor positive allosteric modulator designed to have low cooperativity with acetylcholine. This was a first‐in‐huma...
PMC12736120
core_pubmed_pmc
First-in-Human Phase I Clinical Trial of SLC-391, a Novel and Selective AXL Inhibitor, in Patients with Advanced Solid Tumours
First-in-Human Phase I Clinical Trial of SLC-391, a Novel and Selective AXL Inhibitor, in Patients with Advanced Solid Tumours Abstract Abstract Background/Objectives: AXL, a receptor tyrosine kinase of the TAM family, has emerged as a key target in cancer therapy due to its role in tumour growth, metastasis, immune ev...
PMC6413744
core_pubmed_pmc
In vitro activity and pharmacodynamic/pharmacokinetic parameters of clarithromycin and azithromycin: why they matter in the treatment of respiratory tract infections
In vitro activity and pharmacodynamic/pharmacokinetic parameters of clarithromycin and azithromycin: why they matter in the treatment of respiratory tract infections Abstract Abstract Clarithromycin and azithromycin are second-generation macrolides established and widely used for treating a range of upper and lower res...
PMC11687557
core_pubmed_pmc
Dynamics of thrombin generation: Filling the gap between the system pharmacology theory and clinical practice in clinical pharmacology and therapeutics
Dynamics of thrombin generation: Filling the gap between the system pharmacology theory and clinical practice in clinical pharmacology and therapeutics Abstract Abstract Mathematical models of thrombin generation (TG) that have been developed are based on a systems biology approach. Although this approach provides impo...
PMC9820191
core_pubmed_pmc
Half-Life Extension and Biodistribution Modulation of Biotherapeutics via Red Blood Cell Hitch-Hiking with Novel Anti-Band 3 Single-Domain Antibodies
Half-Life Extension and Biodistribution Modulation of Biotherapeutics via Red Blood Cell Hitch-Hiking with Novel Anti-Band 3 Single-Domain Antibodies Abstract Small therapeutic proteins are receiving increased interest as therapeutic drugs; however, their clinical success has been limited due to their rapid elimination...
PMC9299061
core_pubmed_pmc
Acute Effects of Psilocybin After Escitalopram or Placebo Pretreatment in a Randomized, Double‐Blind, Placebo‐Controlled, Crossover Study in Healthy Subjects
Acute Effects of Psilocybin After Escitalopram or Placebo Pretreatment in a Randomized, Double‐Blind, Placebo‐Controlled, Crossover Study in Healthy Subjects Abstract The psychedelic psilocybin is being investigated for the treatment of depression and anxiety. Unclear is whether antidepressant treatments interact with ...
PMC7563358
core_pubmed_pmc
Prolonging the Half-Life of Histone Deacetylase Inhibitor Belinostat via 50 nm Scale Liposomal Subcutaneous Delivery System for Peripheral T-Cell Lymphoma
Prolonging the Half-Life of Histone Deacetylase Inhibitor Belinostat via 50 nm Scale Liposomal Subcutaneous Delivery System for Peripheral T-Cell Lymphoma Abstract Abstract Simple Summary Belinostat is the novel histone deacetylase inhibitors (HDACis) for treatment for peripheral T-cell lymphoma (PTCL). However, the ha...
PMC8004922
core_pubmed_pmc
Sex Differences on Mitotane Concentration and Treatment Outcome in Patients with Adrenocortical Carcinoma
Sex Differences on Mitotane Concentration and Treatment Outcome in Patients with Adrenocortical Carcinoma Abstract Abstract (1) Background: In clinical settings, data regarding sex are rarely investigated. In women, factors such as body size and composition, hormonal variations, metabolism, and access to care systems a...
PMC8596611
core_pubmed_pmc
Maternal-Fetal Pharmacology of Drugs: A Review of Current Status of the Application of Physiologically Based Pharmacokinetic Models
Maternal-Fetal Pharmacology of Drugs: A Review of Current Status of the Application of Physiologically Based Pharmacokinetic Models Abstract Abstract Pregnancy and the postpartum period are associated with several physiological changes that can alter the pharmacokinetics (PK) and pharmacodynamics (PD) of drugs. For cer...
PMC10517157
core_pubmed_pmc
Comparative acute effects of mescaline, lysergic acid diethylamide, and psilocybin in a randomized, double-blind, placebo-controlled cross-over study in healthy participants
Comparative acute effects of mescaline, lysergic acid diethylamide, and psilocybin in a randomized, double-blind, placebo-controlled cross-over study in healthy participants Abstract Mescaline, lysergic acid diethylamide (LSD), and psilocybin are classic serotonergic psychedelics. A valid, direct comparison of the effe...
PMC12758690
core_pubmed_pmc
Uric acid levels mediate the association between four dietary indices and kidney stones in US adults: A cross-sectional study of NHANES 2007–2018
Uric acid levels mediate the association between four dietary indices and kidney stones in US adults: A cross-sectional study of NHANES 2007–2018 Abstract Background Diet and uric acid are closely linked to the formation of kidney stones. However, the specific dietary indices associated with kidney stone risk and the m...
PMC4069131
core_pubmed_pmc
Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers
Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers Abstract Context Diacerein (DCN) has low aqueous solubility (3.197 mg/L) and, consequently, low oral bioavailability (35%–56%). To increase both the solubility and dissolution rate of D...
PMC8885946
core_pubmed_pmc
Pharmacokinetics of Diazepam and Its Metabolites in Urine of Chinese Participants
Pharmacokinetics of Diazepam and Its Metabolites in Urine of Chinese Participants Abstract Background Urine is conventionally used as a specimen to document diazepam-related crimes; however, few reports have described the pharmacokinetics of diazepam and its metabolites in urine. Objective This study aimed to investiga...
PMC12289749
core_pubmed_pmc
Quantifying clinical and genetic factors influencing rate and severity of autosomal dominant tubulointerstitial kidney disease progression
Quantifying clinical and genetic factors influencing rate and severity of autosomal dominant tubulointerstitial kidney disease progression Abstract Abstract Autosomal dominant tubulointerstitial kidney disease (ADTKD), caused by mutations in UMOD and MUC1 genes, leads to tubular damage and fibrosis, ultimately resultin...
PMC12553364
core_pubmed_pmc
Interaction between crizotinib and tropifexor through in vitro and in vivo studies
Interaction between crizotinib and tropifexor through in vitro and in vivo studies Abstract In the context of cancer treatment, the employment of multiple drug therapies frequently results in a high prevalence of drug-drug interaction (DDI) in clinical practice. Crizotinib is a tyrosine kinase inhibitor (TKI) used to t...
PMC11788651
core_pubmed_pmc
Safety and Tolerability of Letetresgene Autoleucel (GSK3377794): Pilot Studies in Patients with Advanced Non–Small Cell Lung Cancer
Safety and Tolerability of Letetresgene Autoleucel (GSK3377794): Pilot Studies in Patients with Advanced Non–Small Cell Lung Cancer Abstract Abstract Purpose: The study aims to evaluate the safety, tolerability, and antitumor response of letetresgene autoleucel (lete-cel), genetically modified autologous T cells expres...
PMC9283668
core_pubmed_pmc
Natural and commercial antibiotic comparison with drugs modeling cell integrity cell stability of Bio-Kinetics changes under morphological topographies cells with lower toxicological characteristics for multidrug resistances problem
Natural and commercial antibiotic comparison with drugs modeling cell integrity cell stability of Bio-Kinetics changes under morphological topographies cells with lower toxicological characteristics for multidrug resistances problem Abstract Antibacterial drug-resistant strains are a serious problem of bacterial treatm...
PMC9043603
core_pubmed_pmc
Application of an Accessible Interface for Pharmacokinetic Modeling and In Vitro to In Vivo Extrapolation
Application of an Accessible Interface for Pharmacokinetic Modeling and In Vitro to In Vivo Extrapolation Abstract Regulatory toxicology testing has traditionally relied on in vivo methods to inform decision-making. However, scientific, practical, and ethical considerations have led to an increased interest in the use ...
PMC8020364
core_pubmed_pmc
Physiologically-based pharmacokinetic model for clozapine in Korean patients with schizophrenia
Physiologically-based pharmacokinetic model for clozapine in Korean patients with schizophrenia Abstract Clozapine has been used as a treatment of schizophrenia. Despite its large interindividual variability, few reports addressed the physiologically-based pharmacokinetic modeling and simulation (PBPK M&S) of clozapine...
PMC9623018
core_pubmed_pmc
Blood–brain barrier and brain structural changes in lung cancer patients with non-brain metastases
Blood–brain barrier and brain structural changes in lung cancer patients with non-brain metastases Abstract Purpose To explore the relationship between blood-brain barrier (BBB) leakage and brain structure in non-brain metastasis lung cancer (LC) by magnetic resonance imaging (MRI) as well as to indicate the possibilit...
PMC7689835
core_pubmed_pmc
Population Pharmacokinetic Analysis of Quizartinib in Healthy Volunteers and Patients With Relapsed/Refractory Acute Myeloid Leukemia
Population Pharmacokinetic Analysis of Quizartinib in Healthy Volunteers and Patients With Relapsed/Refractory Acute Myeloid Leukemia Abstract Abstract Quizartinib is an FMS‐like tyrosine kinase 3 (FLT3) inhibitor that has shown robust clinical activity in patients with FLT3‐ internal tandem duplication–mutated relapse...
PMC5303336
core_pubmed_pmc
Managing patients taking edoxaban in dentistry
Managing patients taking edoxaban in dentistry Abstract Background Anticoagulation therapy is used in several conditions to prevent or treat thromboembolism. A new group of oral anticoagulants with clear advantages over classic dicoumarin oral anticoagulants (warfarin and acenocoumarol) has been developed in recent yea...
PMC6585996
core_pubmed_pmc
Effect of a High‐Fat Meal on the Pharmacokinetics of the HIV Integrase Inhibitor Cabotegravir
Effect of a High‐Fat Meal on the Pharmacokinetics of the HIV Integrase Inhibitor Cabotegravir Abstract Abstract Cabotegravir is an integrase inhibitor in clinical development for the treatment and prevention of HIV infection using oral tablets for short‐term, lead‐in use before subsequent administration of a long‐actin...
PMC6354309
core_pubmed_pmc
Daptomycin dosing in obese patients: analysis of the use of adjusted body weight versus actual body weight
Daptomycin dosing in obese patients: analysis of the use of adjusted body weight versus actual body weight Abstract Background: Food and Drug Administration–approved daptomycin dosing uses actual body weight, despite limited dosing information for obese patients. Studies report alterations in daptomycin pharmacokinetic...
PMC7127355
core_pubmed_pmc
Pharmacokinetic study of luteolin, apigenin, chrysoeriol and diosmetin after oral administration of Flos Chrysanthemi extract in rats
Pharmacokinetic study of luteolin, apigenin, chrysoeriol and diosmetin after oral administration of Flos Chrysanthemi extract in rats Abstract Abstract Flos Chrysanthemi (the flower of Chrysanthemum morifolium Ramat.) is widely used in China as a food and traditional Chinese medicine for many diseases. Luteolin and api...
PMC5845055
core_pubmed_pmc
gPKPDSim: a SimBiology ® -based GUI application for PKPD modeling in drug development
gPKPDSim: a SimBiology ® -based GUI application for PKPD modeling in drug development Abstract Abstract Modeling and simulation (M&S) is increasingly used in drug development to characterize pharmacokinetic-pharmacodynamic (PKPD) relationships and support various efforts such as target feasibility assessment, molecule ...