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PMC11754052 | core_pubmed_pmc | Key considerations based on pharmacokinetic/pharmacodynamic in the design of antibody-drug conjugates | Key considerations based on pharmacokinetic/pharmacodynamic in the design of antibody-drug conjugates Abstract Background Antibody-drug conjugate (ADC) is an anticancer drug that links toxins to specifically targeted antibodies via linkers, offering the advantages of high target specificity and high cytotoxicity. Howev... |
PMC11148161 | core_pubmed_pmc | Integrated PBPK-EO modeling of osimertinib to predict plasma concentrations and intracranial EGFR engagement in patients with brain metastases | Integrated PBPK-EO modeling of osimertinib to predict plasma concentrations and intracranial EGFR engagement in patients with brain metastases Abstract Abstract The purpose of this study was to develop and validate a physiologically based pharmacokinetic (PBPK) model combined with an EGFR occupancy (EO) model for osime... |
PMC8712803 | core_pubmed_pmc | Antithrombotic and anticoagulation therapies in cardiogenic shock: a critical review of the published literature | Antithrombotic and anticoagulation therapies in cardiogenic shock: a critical review of the published literature Abstract Abstract Cardiogenic shock (CS) is a complex multifactorial clinical syndrome, developing as a continuum, and progressing from the initial insult (underlying cause) to the subsequent occurrence of o... |
PMC10458693 | core_pubmed_pmc | Metabotropic Glutamate Receptor Subtype 5 Positron-Emission-Tomography Radioligands as a Tool for Central Nervous System Drug Development: Between Progress and Setbacks | Metabotropic Glutamate Receptor Subtype 5 Positron-Emission-Tomography Radioligands as a Tool for Central Nervous System Drug Development: Between Progress and Setbacks Abstract Abstract The metabotropic glutamate receptor subtype 5 (mGluR5) is a class C G-protein-coupled receptor (GPCR) that has been implicated in var... |
PMC11103495 | core_pubmed_pmc | In situ single-cell therapeutic response imaging facilitated by the TRIPODD fluorescence imaging platform | In situ single-cell therapeutic response imaging facilitated by the TRIPODD fluorescence imaging platform Abstract Abstract Purpose : Small molecule drugs such as tyrosine kinase inhibitors (TKIs) targeting tumoral molecular dependencies have become standard of care for numerous cancer types. Notably, epidermal growth ... |
PMC11154452 | core_pubmed_pmc | Population Pharmacokinetic Modeling for Twice-Daily Intravenous Busulfan in a Large Cohort of Pediatric Patients Undergoing Hematopoietic Stem Cell Transplantation—A 10-Year Single-Center Experience | Population Pharmacokinetic Modeling for Twice-Daily Intravenous Busulfan in a Large Cohort of Pediatric Patients Undergoing Hematopoietic Stem Cell Transplantation—A 10-Year Single-Center Experience Abstract Abstract Reaching target exposure of busulfan-based conditioning prior to hematopoietic stem cell transplantatio... |
PMC8533539 | core_pubmed_pmc | Capillary Electrophoresis–Mass Spectrometry with Multisegment Injection and In-Capillary Preconcentration for High-Throughput and Sensitive Determination of Therapeutic Decapeptide Triptorelin in Pharmaceutical and Biological Matrices | Capillary Electrophoresis–Mass Spectrometry with Multisegment Injection and In-Capillary Preconcentration for High-Throughput and Sensitive Determination of Therapeutic Decapeptide Triptorelin in Pharmaceutical and Biological Matrices Abstract Abstract A capillary electrophoresis–tandem mass spectrometry method with a ... |
PMC5462973 | core_pubmed_pmc | Tacrolimus Updated Guidelines through popPK Modeling: How to Benefit More from CYP3A Pre-emptive Genotyping Prior to Kidney Transplantation | Tacrolimus Updated Guidelines through popPK Modeling: How to Benefit More from CYP3A Pre-emptive Genotyping Prior to Kidney Transplantation Abstract Tacrolimus (Tac) is a profoundly effective immunosuppressant that reduces the risk of rejection after solid organ transplantation. However, its use is hampered by its narr... |
PMC5108082 | core_pubmed_pmc | Pharmacokinetics, toxicity, and cytochrome P450 modulatory activity of plumbagin | Pharmacokinetics, toxicity, and cytochrome P450 modulatory activity of plumbagin Abstract Background The antimalarial activity of plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone), a naturally occurring naphthoquinone widely distributed in the Plumbaginaceae family has previously been demonstrated in vitro (good activi... |
PMC10547636 | core_pubmed_pmc | Maturation of Paracetamol Elimination Routes in Preterm Neonates Born Below 32 Weeks of Gestation | Maturation of Paracetamol Elimination Routes in Preterm Neonates Born Below 32 Weeks of Gestation Abstract Abstract Purpose Despite being off-label, intravenous paracetamol (PCM) is increasingly used to control mild-to-moderate pain in preterm neonates. Here we aim to quantify the maturation of paracetamol elimination ... |
PMC11129190 | core_pubmed_pmc | Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility | Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility Abstract Cardiac myosin activation has been shown to be a viable approach for the treatment of heart failure with reduced ejection fraction. Here, we repor... |
PMC7329795 | core_pubmed_pmc | In vitro inhibition of human cytochrome P450 enzymes by the novel atypical antipsychotic drug asenapine: a prediction of possible drug–drug interactions | In vitro inhibition of human cytochrome P450 enzymes by the novel atypical antipsychotic drug asenapine: a prediction of possible drug–drug interactions Abstract Background Inhibition of cytochrome P450 (CYP) enzymes is the most common cause of harmful drug–drug interactions. The present study aimed at examining the in... |
PMC11598963 | core_pubmed_pmc | Pharmacokinetics of Meloxicam in Different Animal Species: A Comprehensive Review | Pharmacokinetics of Meloxicam in Different Animal Species: A Comprehensive Review Abstract Simple Summary Meloxicam has been extensively used in human beings and animals for ameliorating pain and inflammation associated with a wide range of disorders such as osteoarthritis, acute respiratory infection or mastitis, due ... |
PMC12612075 | core_pubmed_pmc | A new, patient-friendly, needleless methotrexate administration method using the pyro-drive jet injector in rats | A new, patient-friendly, needleless methotrexate administration method using the pyro-drive jet injector in rats Abstract Methotrexate (MTX) is the anchor first-line drug for the treatment of rheumatoid arthritis (RA) in the RA guidelines of the ACR, JCR and EULAR. In the guidelines, MTX is primarily administered orall... |
PMC6697721 | core_pubmed_pmc | A population pharmacokinetic model for simvastatin and its metabolites in children and adolescents | A population pharmacokinetic model for simvastatin and its metabolites in children and adolescents Abstract Purpose Poor adherence to dietary/behaviour modifications as interventions for hypercholesterolemia in paediatric patients often necessitates the initiation of statin therapy. The aim of this study was to develop... |
PMC10514130 | core_pubmed_pmc | Impact of Bariatric Surgery in the Short and Long Term: A Need for Time-Dependent Dosing of Drugs | Impact of Bariatric Surgery in the Short and Long Term: A Need for Time-Dependent Dosing of Drugs Abstract Abstract Sparse information is available on pharmacokinetic changes of drugs over time after bariatric surgery. By reviewing the literature on the short- and long-term pharmacokinetic changes of drugs, several pat... |
PMC3777223 | core_pubmed_pmc | Confirmation of diosmetin 3- O -glucuronide as major metabolite of diosmin in humans, using micro-liquid-chromatography–mass spectrometry and ion mobility mass spectrometry | Confirmation of diosmetin 3- O -glucuronide as major metabolite of diosmin in humans, using micro-liquid-chromatography–mass spectrometry and ion mobility mass spectrometry Abstract Abstract Diosmin is a flavonoid often administered in the treatment of chronic venous insufficiency, hemorrhoids, and related affections. ... |
PMC8358626 | core_pubmed_pmc | Variation in Target Attainment of Beta‐Lactam Antibiotic Dosing Between International Pediatric Formularies | Variation in Target Attainment of Beta‐Lactam Antibiotic Dosing Between International Pediatric Formularies Abstract As antimicrobial susceptibility of common bacterial pathogens decreases, ensuring optimal dosing may preserve the use of older antibiotics in order to limit the spread of resistance to newer agents. Beta... |
PMC9476668 | core_pubmed_pmc | Comparative pharmacokinetics of baicalin and geniposide in juvenile and adult rats after oral administration of Qingkailing Granules | Comparative pharmacokinetics of baicalin and geniposide in juvenile and adult rats after oral administration of Qingkailing Granules Abstract Objective To explore the effect of age on Qingkailing Granules disposition by comparing the pharmacokinetics of geniposide and baicalin in juvenile and adult rats. Methods A simp... |
PMC5847232 | core_pubmed_pmc | Impact of mathematical pharmacology on practice and theory: four case studies | Impact of mathematical pharmacology on practice and theory: four case studies Abstract Abstract Drug-discovery has become a complex discipline in which the amount of knowledge about human biology, physiology, and biochemistry have increased. In order to harness this complex body of knowledge mathematics can play a crit... |
PMC12263743 | core_pubmed_pmc | Model-Informed Precision Dosing of Eculizumab in Patients with Paroxysmal Nocturnal Hemoglobinuria | Model-Informed Precision Dosing of Eculizumab in Patients with Paroxysmal Nocturnal Hemoglobinuria Abstract Background and Objective Eculizumab is an expensive therapeutic monoclonal antibody inhibiting complement C5 and approved for various indications, including the rare disease paroxysmal nocturnal hemoglobinuria. E... |
PMC11302283 | core_pubmed_pmc | Ronapreve (REGN-CoV; casirivimab and imdevimab) reduces the viral burden and alters the pulmonary response to the SARS-CoV-2 Delta variant (B.1.617.2) in K18-hACE2 mice using an experimental design reflective of a treatment use case | Ronapreve (REGN-CoV; casirivimab and imdevimab) reduces the viral burden and alters the pulmonary response to the SARS-CoV-2 Delta variant (B.1.617.2) in K18-hACE2 mice using an experimental design reflective of a treatment use case Abstract ABSTRACT With some exceptions, global policymakers have recommended against th... |
PMC12288676 | core_pubmed_pmc | Pharmacokinetics of apixaban in patients undergoing pancreaticoduodenectomy (PAP-UP) | Pharmacokinetics of apixaban in patients undergoing pancreaticoduodenectomy (PAP-UP) Abstract Abstract Objective: The impact of pancreaticoduodenectomy on absorption of drugs in the duodenum remains largely unknown. We aim to characterize the pharmacokinetics of apixaban in patients who had previously undergone pancrea... |
PMC7067712 | core_pubmed_pmc | Evaluation of Fosphenytoin Therapeutic Drug Monitoring in the Neurocritical Care Unit | Evaluation of Fosphenytoin Therapeutic Drug Monitoring in the Neurocritical Care Unit Abstract Abstract Objective The aim of this study was to determine whether the current method of calculating a fosphenytoin reloading dose results in a therapeutic free phenytoin level on subsequent days. Methods Medical records of pa... |
PMC8879580 | core_pubmed_pmc | Population Pharmacokinetics of Amikacin in Patients on Veno-Arterial Extracorporeal Membrane Oxygenation | Population Pharmacokinetics of Amikacin in Patients on Veno-Arterial Extracorporeal Membrane Oxygenation Abstract Veno-arterial extracorporeal membrane oxygenation (V-A ECMO) support leads to complex pharmacokinetic alterations, whereas adequate drug dosing is paramount for efficacy and absence of toxicity in criticall... |
PMC7310382 | core_pubmed_pmc | Parasite clearance, cure rate, post-treatment prophylaxis and safety of standard 3-day versus an extended 6-day treatment of artemether–lumefantrine and a single low-dose primaquine for uncomplicated Plasmodium falciparum malaria in Bagamoyo district, Tanzania: a randomized controlled trial | Parasite clearance, cure rate, post-treatment prophylaxis and safety of standard 3-day versus an extended 6-day treatment of artemether–lumefantrine and a single low-dose primaquine for uncomplicated Plasmodium falciparum malaria in Bagamoyo district, Tanzania: a randomized controlled trial Abstract Abstract Background... |
PMC10686957 | core_pubmed_pmc | Oral and Intravenous Amoxicillin Dosing Recommendations in Neonates: A Pooled Population Pharmacokinetic Study | Oral and Intravenous Amoxicillin Dosing Recommendations in Neonates: A Pooled Population Pharmacokinetic Study Abstract Abstract Background There is a lack of evidence on oral amoxicillin pharmacokinetics and exposure in neonates with possible serious bacterial infection (pSBI). We aimed to describe amoxicillin disposi... |
PMC10338556 | core_pubmed_pmc | Bioequivalence of Intravenous Alteplase from Two Different Manufacturing Processes in Healthy Male Volunteers: Results from a Two-Stage, Adaptive-Design Study | Bioequivalence of Intravenous Alteplase from Two Different Manufacturing Processes in Healthy Male Volunteers: Results from a Two-Stage, Adaptive-Design Study Abstract Objective Alteplase is a recombinant tissue plasminogen activator used for thrombolytic treatment in several indications and is currently approved in Eu... |
PMC6060311 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic properties of orally administered torsemide in healthy horses | Pharmacokinetic and pharmacodynamic properties of orally administered torsemide in healthy horses Abstract Abstract Background Diuretic treatment is the mainstay for management of congestive heart failure in horses, and its use has been restricted to injectable medications because no currently data supports the use of ... |
PMC11830948 | core_pubmed_pmc | Population Pharmacokinetic of Epidural Sufentanil in Labouring Women: A Multicentric, Prospective, Observational Study | Population Pharmacokinetic of Epidural Sufentanil in Labouring Women: A Multicentric, Prospective, Observational Study Abstract Purpose The effects of sufentanil-ropivacaine combination on the parturient women and the course of labor have been well documented. However, there is little information regarding the time-dep... |
PMC7854758 | core_pubmed_pmc | On the effect of antiresorptive drugs on the bone remodeling of the mandible after dental implantation: a mathematical model | On the effect of antiresorptive drugs on the bone remodeling of the mandible after dental implantation: a mathematical model Abstract Abstract Bone remodeling identifies the process of permanent bone change with new bone formation and old bone resorption. Understanding this process is essential in many applications, su... |
PMC3813505 | core_pubmed_pmc | AfroDb: A Select Highly Potent and Diverse Natural Product Library from African Medicinal Plants | AfroDb: A Select Highly Potent and Diverse Natural Product Library from African Medicinal Plants Abstract Computer-aided drug design (CADD) often involves virtual screening (VS) of large compound datasets and the availability of such is vital for drug discovery protocols. We assess the bioactivity and “drug-likeness” o... |
PMC12562088 | core_pubmed_pmc | Bidirectional Endothelial Feedback Drives Turing-Vascular Patterning and Drug-Resistance Niches: A Hybrid PDE-Agent-Based Study | Bidirectional Endothelial Feedback Drives Turing-Vascular Patterning and Drug-Resistance Niches: A Hybrid PDE-Agent-Based Study Abstract Abstract We present a hybrid partial differential equation-agent-based model (PDE-ABM). In our framework, tumor cells secrete tumor angiogenic factor (TAF), while endothelial cells ch... |
PMC8541629 | core_pubmed_pmc | Towards Advances in Medicinal Plant Antimicrobial Activity: A Review Study on Challenges and Future Perspectives | Towards Advances in Medicinal Plant Antimicrobial Activity: A Review Study on Challenges and Future Perspectives Abstract The increasing incidence of drug- resistant pathogens raises an urgent need to identify and isolate new bioactive compounds from medicinal plants using standardized modern analytical procedures. Med... |
PMC10182160 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Voclosporin | Clinical Pharmacokinetics and Pharmacodynamics of Voclosporin Abstract Abstract Voclosporin is an approved option for the long-term treatment of lupus nephritis. We aimed to provide a narrative review of the pharmacokinetics and pharmacodynamics of voclosporin. In addition, we derived values for pharmacokinetic and pha... |
PMC10515181 | core_pubmed_pmc | Ternary Mixture of Pentanamide in Solvent Analogy with Halogenated Phenol: Experimental, Theoretical, and In Silico Biological Studies | Ternary Mixture of Pentanamide in Solvent Analogy with Halogenated Phenol: Experimental, Theoretical, and In Silico Biological Studies Abstract Abstract This research describes the preparation of mixtures of new halogen-substituted phenol derivatives and their effects due to linkages with a fatty amide (pentanamide). T... |
PMC6693729 | core_pubmed_pmc | A Pilot Study of Vinorelbine Safety and Pharmacokinetics in Patients with Varying Degrees of Liver Dysfunction | A Pilot Study of Vinorelbine Safety and Pharmacokinetics in Patients with Varying Degrees of Liver Dysfunction Abstract Vinorelbine tartrate is a semi‐synthetic vinca alkaloid and an inhibitor of microtubule polymerization with demonstrated antitumor properties across a spectrum of cancers. The pharmacokinetics of vino... |
PMC12135072 | core_pubmed_pmc | Improved anti-breast cancer activity through structural modification of fused pyran derivatives and mechanistic investigations † | Improved anti-breast cancer activity through structural modification of fused pyran derivatives and mechanistic investigations † Abstract Novel fused pyran derivatives were synthesized and evaluated for anticancer activity against MCF7 (ATCC – HTB-22, breast), A549 (ATCC – CCL-185, lung), and HCT116 (ATCC – CCL-247, co... |
PMC12347667 | core_pubmed_pmc | The Role of Landiolol in Coronary Artery Disease: Insights into Acute Coronary Syndromes, Stable Coronary Artery Disease and Computed Tomography Coronary Angiography | The Role of Landiolol in Coronary Artery Disease: Insights into Acute Coronary Syndromes, Stable Coronary Artery Disease and Computed Tomography Coronary Angiography Abstract Coronary artery disease (CAD) constitutes a major contributor to morbidity, mortality and healthcare burden worldwide. Recent innovations in imag... |
PMC12881681 | core_pubmed_pmc | Mechanism-based inactivation of human aldehyde oxidase by erlotinib: Mechanistic insights from structural analogs and molecular docking | Mechanism-based inactivation of human aldehyde oxidase by erlotinib: Mechanistic insights from structural analogs and molecular docking Abstract Aldehyde oxidase (AOX1) is a cytosolic molybdo-flavoenzyme that metabolizes azaheterocyclic drugs. Erlotinib and gefitinib are azaheterocyclic drugs. We deployed structural an... |
PMC5944576 | core_pubmed_pmc | NI‐0801, an anti‐chemokine (C‐X‐C motif) ligand 10 antibody, in patients with primary biliary cholangitis and an incomplete response to ursodeoxycholic acid | NI‐0801, an anti‐chemokine (C‐X‐C motif) ligand 10 antibody, in patients with primary biliary cholangitis and an incomplete response to ursodeoxycholic acid Abstract NI‐0801 is a fully human monoclonal antibody against chemokine (C‐X‐C motif) ligand 10 (CXCL10), which is involved in the recruitment of inflammatory T ce... |
PMC8923208 | core_pubmed_pmc | Considerations for the Use of Phage Therapy in Clinical Practice | Considerations for the Use of Phage Therapy in Clinical Practice Abstract ABSTRACT Increasing antimicrobial resistance and medical device-related infections have led to a renewed interest in phage therapy as an alternative or adjunct to conventional antimicrobials. Expanded access and compassionate use cases have risen... |
PMC9291886 | core_pubmed_pmc | Oral drug dosing following bariatric surgery: General concepts and specific dosing advice | Oral drug dosing following bariatric surgery: General concepts and specific dosing advice Abstract Bariatric or weight‐loss surgery is a popular option for weight reduction. Depending on the surgical procedure, gastric changes like decreased transit time and volume and increased pH, decreased absorption surface in the ... |
PMC5916261 | core_pubmed_pmc | Comparison of tadalafil pharmacokinetics after administration of a new orodispersible film versus a film-coated tablet | Comparison of tadalafil pharmacokinetics after administration of a new orodispersible film versus a film-coated tablet Abstract Abstract Background An orodispersible film (ODF) of tadalafil may provide increased convenience for erectile dysfunction (ED) patients as compared to conventional tablet formulations. In this ... |
PMC8161445 | core_pubmed_pmc | Clinical Pharmacology of Antibody-Drug Conjugates | Clinical Pharmacology of Antibody-Drug Conjugates Abstract Antibody-drug conjugates (ADCs) are biopharmaceutical products where a monoclonal antibody is linked to a biologically active drug (a small molecule) forming a conjugate. Since the approval of first ADC (Gemtuzumab ozogamicin (trade name: Mylotarg)) for the tre... |
PMC9290673 | core_pubmed_pmc | TDM is dead. Long live TCI! | TDM is dead. Long live TCI! Abstract Twenty years ago, target concentration intervention (TCI) was distinguished from therapeutic drug monitoring (TDM). It was proposed that TCI would bring more clinical benefit because of the precision of the approach and the ability to link TCI to principles of pharmacokinetics and p... |
PMC11812939 | core_pubmed_pmc | Implementing a Bayesian approach using Stan with Torsten: Population pharmacokinetics analysis of somatrogon | Implementing a Bayesian approach using Stan with Torsten: Population pharmacokinetics analysis of somatrogon Abstract Abstract Fully Bayesian approaches are not commonly implemented for population pharmacokinetic (PK) modeling. In this paper, we evaluate the use of Stan with R and Torsten for population PK modeling of ... |
PMC11379596 | core_pubmed_pmc | Improvement of NaCas/DGMO complex emulsion on resveratrol stability, in vitro bioaccessibility, in vivo bioavailability and gut microbiota | Improvement of NaCas/DGMO complex emulsion on resveratrol stability, in vitro bioaccessibility, in vivo bioavailability and gut microbiota Abstract Evaluation for biological impact of food emulsions is fundamental for their application. In present study, we utilized a NaCas-DGMO (sodium caseinate-decylglycerol monoolea... |
PMC5808101 | core_pubmed_pmc | Darunavir/cobicistat showing similar effectiveness as darunavir/ritonavir monotherapy despite lower trough concentrations | Darunavir/cobicistat showing similar effectiveness as darunavir/ritonavir monotherapy despite lower trough concentrations Abstract Abstract Introduction When darunavir ( DRV ) 800 mg is boosted with 150 mg cobicistat ( DRV cobi ), DRV trough concentration (C trough ) is about 30% lower as compared to 100 mg ritonavir (... |
PMC10937073 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Tenapanor in Healthy Chinese and Caucasian Volunteers: A Randomized, Open-Label, Single-Center, Placebo-Controlled Phase 1 Study | Pharmacokinetics, Safety, and Tolerability of Tenapanor in Healthy Chinese and Caucasian Volunteers: A Randomized, Open-Label, Single-Center, Placebo-Controlled Phase 1 Study Abstract Background Tenapanor is a locally acting selective sodium-hydrogen exchanger 3 inhibitor with the potential to treat sodium/phosphorus a... |
PMC12710366 | core_pubmed_pmc | Model-informed development of bacteriophage therapy: bridging in vitro and in vivo efficacy against multidrug-resistant Pseudomonas aeruginosa | Model-informed development of bacteriophage therapy: bridging in vitro and in vivo efficacy against multidrug-resistant Pseudomonas aeruginosa Abstract ABSTRACT Bacteriophages are emerging as promising alternatives to antibiotics for multidrug-resistant (MDR) infections. However, their unique pharmacokinetic and pharma... |
PMC12115173 | core_pubmed_pmc | The Cordyceps Genus as a Potential Source of Bioactive Compounds for Adjuvant Cancer Therapy: A Network Pharmacology Approach | The Cordyceps Genus as a Potential Source of Bioactive Compounds for Adjuvant Cancer Therapy: A Network Pharmacology Approach Abstract Abstract Background/Objectives: Cancer remains one of the leading causes of mortality globally, underscoring the need for novel therapeutic strategies capable of targeting multiple mole... |
PMC11703399 | core_pubmed_pmc | Artificial intelligence-driven prediction and validation of blood–brain barrier permeability and absorption, distribution, metabolism, excretion profiles in natural product research laboratory compounds | Artificial intelligence-driven prediction and validation of blood–brain barrier permeability and absorption, distribution, metabolism, excretion profiles in natural product research laboratory compounds Abstract Introduction Our previous research demonstrated that a large language model (LLM) based on the transformer a... |
PMC5680437 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of insulin glargine–insulin glulisine basal-bolus and twice-daily premixed analog insulin in type 1 diabetes mellitus patients during three standardized meals | Pharmacokinetics and pharmacodynamics of insulin glargine–insulin glulisine basal-bolus and twice-daily premixed analog insulin in type 1 diabetes mellitus patients during three standardized meals Abstract Highlights • Insulin glargine/glulisine PK in T1DM is similar to healthy insulin responses. • Insulin glargine/glu... |
PMC3867868 | core_pubmed_pmc | Elimination Kinetics of Ethanol in a 5-Week-Old Infant and a Literature Review of Infant Ethanol Pharmacokinetics | Elimination Kinetics of Ethanol in a 5-Week-Old Infant and a Literature Review of Infant Ethanol Pharmacokinetics Abstract Primary ethanol metabolism occurs through alcohol dehydrogenase, but minor metabolic pathways such as the P450 enzymes CYP2E1 and CYP1A2 and the enzyme catalase exist. These enzymes have distinct d... |
PMC4804322 | core_pubmed_pmc | Nonclinical analysis of the safety, pharmacodynamics, and pharmacokinetics of plasma‐derived human FXIII concentrate in animals | Nonclinical analysis of the safety, pharmacodynamics, and pharmacokinetics of plasma‐derived human FXIII concentrate in animals Abstract Abstract Factor XIII ( FXIII ) is a coagulation protein which plays a major role in hemostasis by covalently cross‐linking fibrin molecules, thereby stabilizing the blood clot and inc... |
PMC4387250 | core_pubmed_pmc | A phase I study of farletuzumab, a humanized anti-folate receptor α monoclonal antibody, in patients with solid tumors | A phase I study of farletuzumab, a humanized anti-folate receptor α monoclonal antibody, in patients with solid tumors Abstract Summary Farletuzumab is a humanized monoclonal antibody against folate receptor α (FRA). The purpose of the study is to assess safety and tolerability, the pharmacokinetic (PK) profile, and pr... |
PMC9544005 | core_pubmed_pmc | A single LC‐MS/MS validated method for tulathromycin quantification in plasma, seminal plasma, and urine to be applied in a pharmacokinetic study in bull | A single LC‐MS/MS validated method for tulathromycin quantification in plasma, seminal plasma, and urine to be applied in a pharmacokinetic study in bull Abstract Abstract Tulathromycin is a macrolide antibiotic generally used for the treatment of respiratory diseases in cattle and swine. This work proposes an improvem... |
PMC8112893 | core_pubmed_pmc | Niclosamide inhalation powder made by thin-film freezing: Multi-dose tolerability and exposure in rats and pharmacokinetics in hamsters | Niclosamide inhalation powder made by thin-film freezing: Multi-dose tolerability and exposure in rats and pharmacokinetics in hamsters Abstract Abstract In this work, we have developed and tested a dry powder form of niclosamide made by thin-film freezing (TFF) and administered it by inhalation to rats and hamsters to... |
PMC5623357 | core_pubmed_pmc | Cohort profile of a study on outcomes related to tuberculosis and antiretroviral drug concentrations in Uganda: design, methods and patient characteristics of the SOUTH study | Cohort profile of a study on outcomes related to tuberculosis and antiretroviral drug concentrations in Uganda: design, methods and patient characteristics of the SOUTH study Abstract Purpose Tuberculosis (TB) is a leading cause of death among people living with HIV in sub-Saharan Africa. Several factors influence the ... |
PMC7523358 | core_pubmed_pmc | A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia | A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia Abstract Background Combined inhibition of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) complexes may be an efficient treatment for acute leukemia. The primary obj... |
PMC12217485 | core_pubmed_pmc | Influence of patient characteristics and oral lead-in on long-acting cabotegravir and rilpivirine pharmacokinetics and outcomes in people with HIV: a real-world study | Influence of patient characteristics and oral lead-in on long-acting cabotegravir and rilpivirine pharmacokinetics and outcomes in people with HIV: a real-world study Abstract ABSTRACT Factors influencing suboptimal pharmacokinetics (PK) of long-acting (LA) cabotegravir (CAB) and rilpivirine (RPV) in people with HIV (P... |
PMC6110008 | core_pubmed_pmc | Pharmacokinetics and Bioavailability Study of Monocrotaline in Mouse Blood by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry | Pharmacokinetics and Bioavailability Study of Monocrotaline in Mouse Blood by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract Background and Aims The present study aimed to develop a simple and sensitive method for quantitative determination of monocrotaline (MCT) in mouse blood emplo... |
PMC12321411 | core_pubmed_pmc | Pharmacokinetics Study of Herb–Drug Interaction of Berberine and Glipizide in Beagle Dogs Using UPLC-MS/MS | Pharmacokinetics Study of Herb–Drug Interaction of Berberine and Glipizide in Beagle Dogs Using UPLC-MS/MS Abstract Abstract Based on the establishment and validation of a UPLC-MS/MS method for detecting glipizide in beagle plasma, the herb–drug interaction (HDI) between berberine and glipizide was studied. After gradi... |
PMC9590231 | core_pubmed_pmc | Ivabradine toxicity: a case report | Ivabradine toxicity: a case report Abstract Background We describe a case of symptomatic bradycardia resulting from ivabradine toxicity by measurement of ivabradine levels, of which there are limited reports in the literature. Case presentation A 43-year-old White female presented with several days of near syncope and ... |
PMC7158967 | core_pubmed_pmc | Comparative evaluation of 68 Ga-labelled TATEs: the impact of chelators on imaging | Comparative evaluation of 68 Ga-labelled TATEs: the impact of chelators on imaging Abstract Abstract Background 68 Ga-labelled peptides targeting somatostatin receptor 2 (SSTR2) have demonstrated encouraging results in managing patients with neuroendocrine tumours (NETs). In addition to metal chelation, bifunctional ch... |
PMC5635303 | core_pubmed_pmc | Clonazepam-associated Bradycardia in a Disabled Elderly Woman with Multiple Complications | Clonazepam-associated Bradycardia in a Disabled Elderly Woman with Multiple Complications Abstract Abstract We herein report an 87-year-old woman who was taking clonazepam at 1.5 mg/day. She was hospitalized with an old cerebral infarction complicated with symptomatic epilepsy, dementia, dyslipidemia, and chronic chole... |
PMC11996792 | core_pubmed_pmc | First-in-human study of CPL’116 – a dual JAK/ROCK inhibitor – in healthy subjects | First-in-human study of CPL’116 – a dual JAK/ROCK inhibitor – in healthy subjects Abstract Abstract Background CPL’116 is a novel Janus kinase (JAK) and Rho-associated coiled-coil containing protein kinase (ROCK) dual inhibitor and a promising drug candidate for the treatment of inflammatory and fibrotic diseases. We c... |
PMC12756461 | core_pubmed_pmc | Pharmacokinetics and safety of the antitumor drug everolimus in healthy Chinese subjects: a single-dose, open-label, randomized, two-sequence, two-period crossover, phase I bioequivalence study | Pharmacokinetics and safety of the antitumor drug everolimus in healthy Chinese subjects: a single-dose, open-label, randomized, two-sequence, two-period crossover, phase I bioequivalence study Abstract Abstract Purpose It aims to evaluate the pharmacokinetic (PK) similarity and safety of everolimus in whole blood unde... |
PMC7563461 | core_pubmed_pmc | Effect of CYP3A5 on the Once-Daily Tacrolimus Conversion in Stable Liver Transplant Patients | Effect of CYP3A5 on the Once-Daily Tacrolimus Conversion in Stable Liver Transplant Patients Abstract Abstract Cytochrome P450 ( CYP ) 3A5 polymorphism influences tacrolimus metabolism, but its effect on the drug pharmacokinetics in liver transplant recipients switched to once-daily extended-release formulation remains... |
PMC10211256 | core_pubmed_pmc | Visual prediction and parameter optimization of viral dynamics in the mucus milieu of the upper airway based on CFPD-HCD analysis | Visual prediction and parameter optimization of viral dynamics in the mucus milieu of the upper airway based on CFPD-HCD analysis Abstract Background and Objective Respiratory diseases caused by viruses are a major human health problem. To better control the infection and understand the pathogenesis of these diseases, ... |
PMC9369865 | core_pubmed_pmc | Aliskiren Hemifumarate Proliposomes for Improved Oral Drug Delivery: Formulation Development, In Vitro and In Vivo Permeability Testing | Aliskiren Hemifumarate Proliposomes for Improved Oral Drug Delivery: Formulation Development, In Vitro and In Vivo Permeability Testing Abstract Abstract The objective of this study was to develop proliposomal formulations for a poorly bioavailable drug, aliskiren hemifumarate (AKH). A solvent evaporation method was us... |
PMC5344941 | core_pubmed_pmc | Phase 1 study of new formulation of patritumab (U3-1287) Process 2, a fully human anti-HER3 monoclonal antibody in combination with erlotinib in Japanese patients with advanced non-small cell lung cancer | Phase 1 study of new formulation of patritumab (U3-1287) Process 2, a fully human anti-HER3 monoclonal antibody in combination with erlotinib in Japanese patients with advanced non-small cell lung cancer Abstract Abstract Background This phase 1 study evaluated the safety, tolerability, pharmacokinetics and efficacy of... |
PMC3598976 | core_pubmed_pmc | Potent in vivo anti-malarial activity and representative snapshot pharmacokinetic evaluation of artemisinin-quinoline hybrids | Potent in vivo anti-malarial activity and representative snapshot pharmacokinetic evaluation of artemisinin-quinoline hybrids Abstract Abstract Background Because Plasmodium falciparum displays increase tolerance against the recommended artemisinin combination therapies (ACT), new classes of anti-malarial drugs are urg... |
PMC5956998 | core_pubmed_pmc | Tumour-homing chimeric polypeptide-conjugated polypyrrole nanoparticles for imaging-guided synergistic photothermal and chemical therapy of cancer | Tumour-homing chimeric polypeptide-conjugated polypyrrole nanoparticles for imaging-guided synergistic photothermal and chemical therapy of cancer Abstract Abstract Near-infrared (NIR)-absorbing conjugated polymer nanoparticles are interesting for imaging-guided combination therapy, especially for synergistic photother... |
PMC7165255 | core_pubmed_pmc | Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties | Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties Abstract Since in vitro studies and a preliminary clinical report suggested the efficacy of chloroquine for COVID-19-associated pneumonia, there is increasing interest in this old antimalarial drug. In this article, we discuss ... |
PMC5694424 | core_pubmed_pmc | Pharmacokinetic Effects of Antidrug Antibodies Occurring in Healthy Subjects After a Single Dose of Intravenous Infliximab | Pharmacokinetic Effects of Antidrug Antibodies Occurring in Healthy Subjects After a Single Dose of Intravenous Infliximab Abstract Background Infliximab pharmacokinetic studies have been performed in patients receiving chronic infliximab therapy. In these patients, infliximab antidrug antibodies (ADAs) increase inflix... |
PMC4807896 | core_pubmed_pmc | Pharmacokinetics and safety of olodaterol administered with the Respimat Soft Mist inhaler in subjects with impaired hepatic or renal function | Pharmacokinetics and safety of olodaterol administered with the Respimat Soft Mist inhaler in subjects with impaired hepatic or renal function Abstract Abstract Purpose In two trials, the influences of hepatic and renal impairment on the pharmacokinetics of olodaterol, a novel long-acting inhaled β 2 -agonist for treat... |
PMC12614974 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Once-Monthly Oral Islatravir: A Phase 2a Study in Participants at Low Risk for Acquiring Human Immunodeficiency Virus Type 1 | Safety, Tolerability, and Pharmacokinetics of Once-Monthly Oral Islatravir: A Phase 2a Study in Participants at Low Risk for Acquiring Human Immunodeficiency Virus Type 1 Abstract Abstract Background Islatravir, a nucleoside reverse transcriptase translocation inhibitor, exhibits high potency against human immunodefici... |
PMC9945836 | core_pubmed_pmc | Immunosuppression by hydroxychloroquine: mechanistic proof in in vitro experiments but limited systemic activity in a randomized placebo-controlled clinical pharmacology study | Immunosuppression by hydroxychloroquine: mechanistic proof in in vitro experiments but limited systemic activity in a randomized placebo-controlled clinical pharmacology study Abstract Based on its wide range of immunosuppressive properties, hydroxychloroquine (HCQ) is used for the treatment of several autoimmune disea... |
PMC6631119 | core_pubmed_pmc | Nasal Administration and Plasma Pharmacokinetics of Parathyroid Hormone Peptide PTH 1-34 for the Treatment of Osteoporosis | Nasal Administration and Plasma Pharmacokinetics of Parathyroid Hormone Peptide PTH 1-34 for the Treatment of Osteoporosis Abstract Abstract Nasal delivery of large peptides such as parathyroid 1-34 (PTH 1-34) can benefit from a permeation enhancer to promote absorption across the nasal mucosa into the bloodstream. Pre... |
PMC12968511 | core_pubmed_pmc | The Need for a Revision of Fluoroquinolone Breakpoints for Interpretation of Antimicrobial Susceptibility Testing of Feline Bacterial Isolates | The Need for a Revision of Fluoroquinolone Breakpoints for Interpretation of Antimicrobial Susceptibility Testing of Feline Bacterial Isolates Abstract ABSTRACT The fluoroquinolone antimicrobial agents, enrofloxacin and marbofloxacin, were approved in the United States for cats in 1990 and 2001, respectively. In 2023, ... |
PMC8048864 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling Combined with Swiss HIV Cohort Study Data Supports No Dose Adjustment of Bictegravir in Elderly Individuals Living With HIV | Physiologically‐Based Pharmacokinetic Modeling Combined with Swiss HIV Cohort Study Data Supports No Dose Adjustment of Bictegravir in Elderly Individuals Living With HIV Abstract Clinical studies in aging people living with HIV (PLWH) are sparse for the novel integrase inhibitor bictegravir, leading to some uncertaint... |
PMC10192144 | core_pubmed_pmc | A Phase I, First-in-Human Study of PRL3-zumab in Advanced, Refractory Solid Tumors and Hematological Malignancies | A Phase I, First-in-Human Study of PRL3-zumab in Advanced, Refractory Solid Tumors and Hematological Malignancies Abstract Background Phosphatase of regenerating liver-3 (PRL-3) is involved in cellular processes driving metastasis, cell proliferation, invasion, motility and survival. It has been shown to be upregulated... |
PMC6331894 | core_pubmed_pmc | Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy | Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy Abstract The majority of anticancer drugs have poor aqueous solubility, produce adverse effects in healthy tissue, and thus impose major limitations on both clinical efficacy and therapeutic safety of cancer c... |
PMC9898326 | core_pubmed_pmc | Pilot Pharmacokinetic Study in Healthy Adults Using Intravascular Microdialysis Catheters Modified for Use in Paediatric Patients to Assess Vancomycin Blood Levels | Pilot Pharmacokinetic Study in Healthy Adults Using Intravascular Microdialysis Catheters Modified for Use in Paediatric Patients to Assess Vancomycin Blood Levels Abstract Abstract Background and Objective Exhaustive pharmacokinetic (PK) studies in paediatric patients are unavailable for most antibiotics and feasibili... |
PMC12317981 | core_pubmed_pmc | Using five exposure metrics to explore the association between ambient PM 2.5 and the hospital admissions for COPD in Tianshui city, China | Using five exposure metrics to explore the association between ambient PM 2.5 and the hospital admissions for COPD in Tianshui city, China Abstract Abstract Numerous studies have identified air pollutant as a primary risk factor for chronic obstructive pulmonary disease (COPD), particularly for fine particulate matter ... |
PMC5867473 | core_pubmed_pmc | Computer-aided design of temozolomide derivatives based on alkylglycerone phosphate synthase structure with isothiocyanate and their pharmacokinetic/toxicity prediction and anti-tumor activity in vitro | Computer-aided design of temozolomide derivatives based on alkylglycerone phosphate synthase structure with isothiocyanate and their pharmacokinetic/toxicity prediction and anti-tumor activity in vitro Abstract Despite the development of temozolomide (TMZ), a novel type of glioma therapeutic drug, malignant glioma rema... |
PMC6822839 | core_pubmed_pmc | A Randomized, Crossover Study on the Effect of Food on the Pharmacokinetic Characteristics of Morphine ARER (MorphaBond™ ER), an Abuse-Deterrent Formulation of Extended-Release Morphine | A Randomized, Crossover Study on the Effect of Food on the Pharmacokinetic Characteristics of Morphine ARER (MorphaBond™ ER), an Abuse-Deterrent Formulation of Extended-Release Morphine Abstract Abstract Introduction Food can alter the pharmacokinetics of certain abuse-deterrent formulations. Morphine ARER is an oral a... |
PMC5845053 | core_pubmed_pmc | Pharmacokinetics of dexmedetomidine during analgosedation in ICU patients | Pharmacokinetics of dexmedetomidine during analgosedation in ICU patients Abstract Dexmedetomidine (DEX) is a fairly new alfa 2 -agonist which has been increasingly used in recent years for analgosedation, mostly because it offers a unique ability of providing both moderate level of sedation and analgesia without respi... |
PMC9809015 | core_pubmed_pmc | Randomized, open-label, phase 2a study to evaluate the contribution of artefenomel to the clinical and parasiticidal activity of artefenomel plus ferroquine in African patients with uncomplicated Plasmodium falciparum malaria | Randomized, open-label, phase 2a study to evaluate the contribution of artefenomel to the clinical and parasiticidal activity of artefenomel plus ferroquine in African patients with uncomplicated Plasmodium falciparum malaria Abstract Background The contribution of artefenomel to the clinical and parasiticidal activity... |
PMC7479006 | core_pubmed_pmc | Effect of high-fat diet on the pharmacokinetics and safety of flumatinib in healthy Chinese subjects | Effect of high-fat diet on the pharmacokinetics and safety of flumatinib in healthy Chinese subjects Abstract Purpose To evaluate the effect of a high-fat diet on the pharmacokinetics and safety of flumatinib mesylate tablets in healthy Chinese subjects. Methods This study was a randomized, open-label, single-dose, two... |
PMC6968538 | core_pubmed_pmc | Pharmacological limitations of phage therapy | Pharmacological limitations of phage therapy Abstract Abstract Clinical trial results of phage treatment of bacterial infections show a low to moderate efficacy, and the variation in infection clearance between subjects within studies is often large. Phage therapy is complicated and introduces many additional component... |
PMC12784611 | core_pubmed_pmc | Rhapontigenin alleviates cellular senescence and physiological aging by upregulating sirt1 and promoting autophagy | Rhapontigenin alleviates cellular senescence and physiological aging by upregulating sirt1 and promoting autophagy Abstract Abstract Background Aging is characterized by cellular senescence, inflammation, and physiological decline. Currently available antiaging therapies often have limitations due to their toxicity and... |
PMC9328652 | core_pubmed_pmc | A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides | A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides Abstract Background and Purpose Efficacy of current antimalarial treatments is declining as a result of increasing antimalarial drug resistance, so new and potent antimalarial drugs are urgently needed. Azithromycin, an azalide antibioti... |
PMC5973957 | core_pubmed_pmc | Population exposure–response analysis of cabozantinib efficacy and safety endpoints in patients with renal cell carcinoma | Population exposure–response analysis of cabozantinib efficacy and safety endpoints in patients with renal cell carcinoma Abstract Abstract Background In the phase III METEOR trial, tyrosine kinase inhibitor cabozantinib significantly improved progression-free survival (PFS), objective response rate (ORR), and overall ... |
PMC4786599 | core_pubmed_pmc | A dose escalating phase I study of GLPG0187, a broad spectrum integrin receptor antagonist, in adult patients with progressive high-grade glioma and other advanced solid malignancies | A dose escalating phase I study of GLPG0187, a broad spectrum integrin receptor antagonist, in adult patients with progressive high-grade glioma and other advanced solid malignancies Abstract Summary Background Integrin signaling is an attractive target for anti-cancer treatment. GLPG0187 is a broad spectrum integrin r... |
PMC7363910 | core_pubmed_pmc | Pharmacokinetics and safety of IBI301 versus rituximab in patients with CD20 + B-cell lymphoma: a multicenter, randomized, double-blind, parallel-controlled study | Pharmacokinetics and safety of IBI301 versus rituximab in patients with CD20 + B-cell lymphoma: a multicenter, randomized, double-blind, parallel-controlled study Abstract Abstract This multicenter, randomized, double-blind, parallel-controlled trial aimed to compare the pharmacokinetics (PK) of IBI301 with rituximab i... |
PMC11111557 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of drug‒drug interactions in hospitalized older adults treated with direct oral anticoagulants | Pharmacokinetics and pharmacodynamics of drug‒drug interactions in hospitalized older adults treated with direct oral anticoagulants Abstract Purpose Polypharmacy is a frequent situation in older adults that increases the risk of drug-drug interactions (DDIs), both pharmacokinetic (PK) and pharmacodynamic (PD). Direct ... |
PMC10071157 | core_pubmed_pmc | A phase Ia dose-escalation trial of Ametumumab (a fully human monoclonal antibody against epidermal growth factor receptor) in patients with advanced solid malignancies | A phase Ia dose-escalation trial of Ametumumab (a fully human monoclonal antibody against epidermal growth factor receptor) in patients with advanced solid malignancies Abstract Abstract Background: Epidermal growth factor receptor (EGFR) is a well-known target for cancer treatment. However, the authorized anti-EGFR mo... |
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