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PMC11256651 | core_pubmed_pmc | Adipose-derived stem cell exosomes loaded with icariin alleviates rheumatoid arthritis by modulating macrophage polarization in rats | Adipose-derived stem cell exosomes loaded with icariin alleviates rheumatoid arthritis by modulating macrophage polarization in rats Abstract Rheumatoid arthritis (RA) is a chronic autoimmune disease marked by synovitis and cartilage destruction. The active compound, icariin (ICA), derived from the herb Epimedium, exhi... |
PMC12802965 | core_pubmed_pmc | Systematic review of antimicrobial pharmacokinetic/pharmacodynamic indices in murine thigh and hollow fibre dose fractionation studies analysed with a standard method | Systematic review of antimicrobial pharmacokinetic/pharmacodynamic indices in murine thigh and hollow fibre dose fractionation studies analysed with a standard method Abstract Abstract Background Pre-clinical models are commonly used to determine human antibiotic dosage regimens using pharmacokinetic/pharmacodynamic (P... |
PMC5502055 | core_pubmed_pmc | Phase II study of lanreotide autogel in Japanese patients with unresectable or metastatic well-differentiated neuroendocrine tumors | Phase II study of lanreotide autogel in Japanese patients with unresectable or metastatic well-differentiated neuroendocrine tumors Abstract Summary Background Lanreotide is a long-acting somatostatin analog with demonstrated efficacy against enteropancreatic neuroendocrine tumor (NET) in the phase III (CLARINET) study... |
PMC4435632 | core_pubmed_pmc | Phase 1 study of ixazomib, an investigational proteasome inhibitor, in advanced non-hematologic malignancies | Phase 1 study of ixazomib, an investigational proteasome inhibitor, in advanced non-hematologic malignancies Abstract Summary Purpose Ixazomib is an investigational proteasome inhibitor with demonstrated antitumor activity in xenograft models of multiple myeloma (MM), lymphoma, and solid tumors. This open-label, phase ... |
PMC5936012 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of nanoceria systemic distribution in rats suggests dose- and route-dependent biokinetics | Physiologically based pharmacokinetic modeling of nanoceria systemic distribution in rats suggests dose- and route-dependent biokinetics Abstract Abstract Background Cerium dioxide nanoparticles (nanoceria) are increasingly being used in a variety of products as catalysts, coatings, and polishing agents. Furthermore, t... |
PMC12094080 | core_pubmed_pmc | Dose Optimization of rhIL‐7‐hyFc for Patients With Lymphopenia Using a Neonatal Fc Receptor‐Mediated Recycling‐Based and Target‐Mediated Drug Disposition Pharmacokinetic Model | Dose Optimization of rhIL‐7‐hyFc for Patients With Lymphopenia Using a Neonatal Fc Receptor‐Mediated Recycling‐Based and Target‐Mediated Drug Disposition Pharmacokinetic Model Abstract ABSTRACT Recombinant human interleukin‐7 hybrid Fc (rhIL‐7‐hyFc) is a homodimer of rhIL‐7 fused to a hyFc. Exogenous IL‐7 promotes T ce... |
PMC11330188 | core_pubmed_pmc | A novel Bayesian generative approach for estimating tumor dynamics from published studies | A novel Bayesian generative approach for estimating tumor dynamics from published studies Abstract Abstract Tumor growth inhibition (TGI) modeling attempts to describe the time course changes in tumor size for patients undergoing cancer therapy. TGI models present several advantages over traditional exposure–response m... |
PMC7293270 | core_pubmed_pmc | Robust combination of liver stereotactic body radiotherapy modulates pharmacokinetics of sorafenib toward preferable parameters | Robust combination of liver stereotactic body radiotherapy modulates pharmacokinetics of sorafenib toward preferable parameters Abstract To evaluate the effect and mechanism of radiotherapy (RT)–sorafenib pharmacokinetics (PK) in different regimens with conventional or high dose irradiation. Between February 2012 and D... |
PMC10183356 | core_pubmed_pmc | Optimization, and biological evaluation of 3- O - β -chacotriosyl betulinic acid amide derivatives as novel small-molecule Omicron | Optimization, and biological evaluation of 3- O - β -chacotriosyl betulinic acid amide derivatives as novel small-molecule Omicron Abstract SARS-CoV-2 Omicron viruses possess a high antigenic shift, and the approved anti-SARS-CoV-2 drugs are extremely limited, which makes the development of new antiviral drugs for the ... |
PMC10748779 | core_pubmed_pmc | Incomplete Data and Potential Risks of Drugs in People with Obesity | Incomplete Data and Potential Risks of Drugs in People with Obesity Abstract Abstract Purpose of Review To provide examples of knowledge gaps in current pharmaceutical treatments for people with obesity and call for changes to regulatory and pharmaceutical clinical research requirements during the drug discovery and de... |
PMC11621354 | core_pubmed_pmc | Repurposing raltegravir for reducing inflammation and treating cancer: a bioinformatics analysis | Repurposing raltegravir for reducing inflammation and treating cancer: a bioinformatics analysis Abstract Abstract Inflammation is a defensive mechanism that safeguards the human body against detrimental stimuli. Within this intricate process, ADAM17, a zinc-dependent metalloprotease, emerges as an indispensable elemen... |
PMC6657354 | core_pubmed_pmc | Optimized administration of hetIL-15 expands lymphocytes and minimizes toxicity in rhesus macaques | Optimized administration of hetIL-15 expands lymphocytes and minimizes toxicity in rhesus macaques Abstract The common γ-chain cytokine interleukin-15 (IL-15) plays a significant role in regulating innate and adaptive lymphocyte homeostasis and can stimulate anti-tumor activity of leukocytes. We have previously shown t... |
PMC4583105 | core_pubmed_pmc | Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers | Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers Abstract Abstract Nanostructured lipid carriers (NLCs) have been one of the systems of choice for improving the oral bioavailability of drugs with poor water solubility. In the present study, lovastatin (LVT)-loaded NLCs (LVT-NLCs)... |
PMC3950581 | core_pubmed_pmc | Soybean greatly reduces valproic acid plasma concentrations: A food–drug interaction study | Soybean greatly reduces valproic acid plasma concentrations: A food–drug interaction study Abstract The aim of this study was to investigate the effects of soy on the pharmacokinetics and pharmacodynamics of valproic acid (VPA). In a preclinical study, rats were pretreated with two different amounts of soy extract for ... |
PMC3502230 | core_pubmed_pmc | Fourth World Antibody-Drug Conjugate Summit | Fourth World Antibody-Drug Conjugate Summit Abstract Abstract The 4th World Antibody Drug Conjugate (WADC) Summit, organized by Hanson Wade was held on February 29‑March 1, 2012 in Frankfurt, Germany, which was also the location for the Antibody Drug Conjugate Summit Europe held in February 2011. During the one year be... |
PMC6055665 | core_pubmed_pmc | Determining the optimal dose of atrasentan by evaluating the exposure‐response relationships of albuminuria and bodyweight | Determining the optimal dose of atrasentan by evaluating the exposure‐response relationships of albuminuria and bodyweight Abstract This study aimed to identify the optimal dose of the endothelin‐1 receptor antagonist atrasentan with maximal albuminuria reduction and minimal signs of sodium retention, as manifested by ... |
PMC12030734 | core_pubmed_pmc | Albaconazole Polymeric Nanocapsules for Treating Trypanosoma cruzi Infections | Albaconazole Polymeric Nanocapsules for Treating Trypanosoma cruzi Infections Abstract The therapeutic management of Chagas disease requires new medicines because the standard-of-care drugs available induce adverse effects and have limited efficacy. In this study, we developed a formulation of albaconazole (ABZ) loaded... |
PMC12834011 | core_pubmed_pmc | Intravital microscopy for nanomedicine: investigating nanoparticle–tissue interactions in the native state | Intravital microscopy for nanomedicine: investigating nanoparticle–tissue interactions in the native state Abstract Abstract Nanomedicine is an evolving field that employs nanoparticles (NPs) for drug delivery systems, molecular imaging, and therapeutic interventions. However, characterizing NP–cell interactions poses ... |
PMC7032160 | core_pubmed_pmc | Development and validation of a UPLC–MS/MS assay for the determination of gemcitabine and its L-carnitine ester derivative in rat plasma and its application in oral pharmacokinetics | Development and validation of a UPLC–MS/MS assay for the determination of gemcitabine and its L-carnitine ester derivative in rat plasma and its application in oral pharmacokinetics Abstract Abstract A simple and rapid UPLC–MS/MS method to simultaneously determine gemcitabine and its L-carnitine ester derivative (2'-de... |
PMC9612038 | core_pubmed_pmc | High-altitude Hypoxia Influences the Activities of the Drug-Metabolizing Enzyme CYP3A1 and the Pharmacokinetics of Four Cardiovascular System Drugs | High-altitude Hypoxia Influences the Activities of the Drug-Metabolizing Enzyme CYP3A1 and the Pharmacokinetics of Four Cardiovascular System Drugs Abstract (1) Background: High-altitude hypoxia has been shown to affect the pharmacokinetic properties of drugs. Although there is a high incidence of cardiovascular diseas... |
PMC5686643 | core_pubmed_pmc | Alterations in Hydrocortisone Pharmacokinetics in a Patient With Congenital Adrenal Hyperplasia Following Bariatric Surgery | Alterations in Hydrocortisone Pharmacokinetics in a Patient With Congenital Adrenal Hyperplasia Following Bariatric Surgery Abstract Management of adult patients with classic congenital adrenal hyperplasia (CAH) is challenging and often complicated by obesity, metabolic syndrome, and adverse cardiovascular risk. Altera... |
PMC10361978 | core_pubmed_pmc | Association between CYP2B6 genetic variability and cyclophosphamide therapy in pediatric patients with neuroblastoma | Association between CYP2B6 genetic variability and cyclophosphamide therapy in pediatric patients with neuroblastoma Abstract Abstract Cyclophosphamide, an oxazaphosphorine prodrug is frequently used in treatment of neuroblastoma, which is one of the most prevalent solid organ malignancies in infants and young children... |
PMC10818372 | core_pubmed_pmc | Is Gender an Important Factor in the Precision Medicine Approach to Levocetirizine? | Is Gender an Important Factor in the Precision Medicine Approach to Levocetirizine? Abstract Abstract Currently, there is insufficient information on the variability in levocetirizine pharmacometrics among individuals, a crucial aspect for establishing its clinical use. The gender differences in pharmacokinetics and th... |
PMC4846778 | core_pubmed_pmc | PK‐PD modeling of individual lesion FDG‐PET response to predict overall survival in patients with sunitinib‐treated gastrointestinal stromal tumor | PK‐PD modeling of individual lesion FDG‐PET response to predict overall survival in patients with sunitinib‐treated gastrointestinal stromal tumor Abstract Pharmacometric models were developed to characterize the relationships between lesion‐level tumor metabolic activity, as assessed by the maximum standardized uptake... |
PMC12895649 | core_pubmed_pmc | Behavioral abnormalities in older patients with chronic renal function decline following administration of compound paracetamol and amantadine hydrochloride capsules | Behavioral abnormalities in older patients with chronic renal function decline following administration of compound paracetamol and amantadine hydrochloride capsules Abstract Abstract Background Compound paracetamol and amantadine hydrochloride capsules are commonly used over-the-counter medications at the primary care... |
PMC12083018 | core_pubmed_pmc | A review on the ethnopharmacology, metabolites, pharmacological uses, and toxicology of Ficus hirta (Moraceae) Vahl | A review on the ethnopharmacology, metabolites, pharmacological uses, and toxicology of Ficus hirta (Moraceae) Vahl Abstract Abstract Ficus hirta Vahl, a member of the Moraceae family and genus Ficus , is a traditional medicinal plant with diverse metabolites. Traditionally, Ficus hirta Vahl has been used in Asian coun... |
PMC8402143 | core_pubmed_pmc | Effects of 1α,25-Dihydroxyvitamin D 3 on the Pharmacokinetics of Procainamide and Its Metabolite N-Acetylprocainamide, Organic Cation Transporter Substrates, in Rats with PBPK Modeling Approach | Effects of 1α,25-Dihydroxyvitamin D 3 on the Pharmacokinetics of Procainamide and Its Metabolite N-Acetylprocainamide, Organic Cation Transporter Substrates, in Rats with PBPK Modeling Approach Abstract Abstract In this study, possible changes in the expression of rat organic cationic transporters (rOCTs) and rat multi... |
PMC3528733 | core_pubmed_pmc | Efficacy, Safety and Anticancer Activity of Protein Nanoparticle-Based Delivery of Doxorubicin through Intravenous Administration in Rats | Efficacy, Safety and Anticancer Activity of Protein Nanoparticle-Based Delivery of Doxorubicin through Intravenous Administration in Rats Abstract Abstract Background and Aims Doxorubicin is a potent anticancer drug and a major limiting factor that hinders therapeutic use as its high levels of systemic circulation ofte... |
PMC4323218 | core_pubmed_pmc | Developing a Molecular Roadmap of Drug-Food Interactions | Developing a Molecular Roadmap of Drug-Food Interactions Abstract Recent research has demonstrated that consumption of food -especially fruits and vegetables- can alter the effects of drugs by interfering either with their pharmacokinetic or pharmacodynamic processes. Despite the recognition of such drug-food associati... |
PMC3218416 | core_pubmed_pmc | Computer aided screening and evaluation of herbal therapeutics against MRSA infections | Computer aided screening and evaluation of herbal therapeutics against MRSA infections Abstract Abstract Methicillin resistant Staphylococcus aureus (MRSA), a pathogenic bacterium that causes life threatening outbreaks such as community-onset and nosocomial infections has emerged as ‘superbug’. The organism developed r... |
PMC7059968 | core_pubmed_pmc | Population modeling of tumor growth curves and the reduced Gompertz model improve prediction of the age of experimental tumors | Population modeling of tumor growth curves and the reduced Gompertz model improve prediction of the age of experimental tumors Abstract Abstract Tumor growth curves are classically modeled by means of ordinary differential equations. In analyzing the Gompertz model several studies have reported a striking correlation b... |
PMC12257260 | core_pubmed_pmc | Pharmacokinetics and Bioavailability of Single‐Dose Intramuscular and Intravenous Administration of Thiafentanil in Goats ( Capra hircus ) | Pharmacokinetics and Bioavailability of Single‐Dose Intramuscular and Intravenous Administration of Thiafentanil in Goats ( Capra hircus ) Abstract ABSTRACT Thiafentanil is a popular opioid agonist used for wildlife chemical immobilisation. Its effects are quickly and completely reversed by the antagonist naltrexone. S... |
PMC4906052 | core_pubmed_pmc | Oseltamivir PK/PD Modeling and Simulation to Evaluate Treatment Strategies against Influenza-Pneumococcus Coinfection | Oseltamivir PK/PD Modeling and Simulation to Evaluate Treatment Strategies against Influenza-Pneumococcus Coinfection Abstract Abstract Influenza pandemics and seasonal outbreaks have shown the potential of Influenza A virus (IAV) to enhance susceptibility to a secondary infection with the bacterial pathogen Streptococ... |
PMC10675397 | core_pubmed_pmc | Physiologically Based Pharmacokinetics Modeling in the Neonatal Population—Current Advances, Challenges, and Opportunities | Physiologically Based Pharmacokinetics Modeling in the Neonatal Population—Current Advances, Challenges, and Opportunities Abstract Physiologically based pharmacokinetic (PBPK) modeling is an approach to predicting drug pharmacokinetics, using knowledge of the human physiology involved and drug physiochemical propertie... |
PMC3502539 | core_pubmed_pmc | Rationale for short course primaquine in Africa to interrupt malaria transmission | Rationale for short course primaquine in Africa to interrupt malaria transmission Abstract Following the recent successes of malaria control in sub-Saharan Africa, the gametocytocidal drug primaquine needs evaluation as a tool to further reduce the transmission of Plasmodium falciparum malaria. The drug has scarcely be... |
PMC5846849 | core_pubmed_pmc | Pharmacogenomics in epilepsy | Pharmacogenomics in epilepsy Abstract Highlights • Genetic variation can influence response to antiepileptic drug (AED) treatment through various effector processes. • Metabolism of many AEDs is mediated by the cytochrome P450 (CYP) family; some of the CYPs have allelic variants that may affect serum AED concentrations... |
PMC4732456 | core_pubmed_pmc | Asparaginase pharmacokinetics and implications of therapeutic drug monitoring | Asparaginase pharmacokinetics and implications of therapeutic drug monitoring Abstract Asparaginase is widely used in chemotherapeutic regimens for the treatment of acute lymphoblastic leukemia (ALL) and has led to a substantial improvement in cure rates, especially in children. Optimal therapeutic effects depend on a ... |
PMC3949558 | core_pubmed_pmc | Population pharmacokinetics of olprinone in healthy male volunteers | Population pharmacokinetics of olprinone in healthy male volunteers Abstract Abstract Background Olprinone decreases the cardiac preload and/or afterload because of its vasodilatory effect and increases myocardial contractility by inhibiting phosphodiesterase III. Purpose The objective of this study was to characterize... |
PMC5328660 | core_pubmed_pmc | Enhancing the oral bioavailability of biochanin A by encapsulation in mixed micelles containing Pluronic F127 and Plasdone S630 | Enhancing the oral bioavailability of biochanin A by encapsulation in mixed micelles containing Pluronic F127 and Plasdone S630 Abstract Biochanin A (BCA), a natural dietary isoflavone, has been reported to show anticancer activities. However, its low biological availability and poor aqueous solubility limit its useful... |
PMC12267664 | core_pubmed_pmc | Drug Interaction PBPK Modeling: Review of the Literature Exposes the Need for Increased Verification of Model Inputs and Outputs as Part of Credibility Assessment | Drug Interaction PBPK Modeling: Review of the Literature Exposes the Need for Increased Verification of Model Inputs and Outputs as Part of Credibility Assessment Abstract ABSTRACT In vitro data are routinely used to support both static and physiologically based pharmacokinetic (PBPK) model‐based drug–drug interaction ... |
PMC8626637 | core_pubmed_pmc | Successful Prediction of Human Fetal Exposure to P-Glycoprotein Substrate Drugs Using the Proteomics-Informed Relative Expression Factor Approach and PBPK Modeling and Simulation | Successful Prediction of Human Fetal Exposure to P-Glycoprotein Substrate Drugs Using the Proteomics-Informed Relative Expression Factor Approach and PBPK Modeling and Simulation Abstract Abstract Many women take drugs during their pregnancy to treat a variety of clinical conditions. To optimize drug efficacy and reduc... |
PMC3750949 | core_pubmed_pmc | Pharmacokinetics and thrombolytic effects of the recombinant tissue-type plasminogen activator in horses | Pharmacokinetics and thrombolytic effects of the recombinant tissue-type plasminogen activator in horses Abstract Abstract Background To test the efficacy of the recombinant tissue-type plasminogen activator (rt-PA) alteplase in horses, the thrombolytic effect was tested in in vitro generated equine thrombi. The extent... |
PMC7449161 | core_pubmed_pmc | Nonstationary Pharmacokinetics of Caspofungin in ICU Patients | Nonstationary Pharmacokinetics of Caspofungin in ICU Patients Abstract Standard dosing of caspofungin in critically ill patients has been reported to result in lower drug exposure, which can lead to subtherapeutic 24-h area under the curve to MIC (AUC 0–24 /MIC) ratios. The aim of the study was to investigate the popul... |
PMC6587412 | core_pubmed_pmc | A population pharmacokinetic study of benzathine benzylpenicillin G administration in children and adolescents with rheumatic heart disease: new insights for improved secondary prophylaxis strategies | A population pharmacokinetic study of benzathine benzylpenicillin G administration in children and adolescents with rheumatic heart disease: new insights for improved secondary prophylaxis strategies Abstract Abstract Background Benzathine benzylpenicillin G (BPG) is recommended as secondary prophylaxis to prevent recu... |
PMC4806669 | core_pubmed_pmc | Treating Diabetes Mellitus: Pharmacophore Based Designing of Potential Drugs from Gymnema sylvestre against Insulin Receptor Protein | Treating Diabetes Mellitus: Pharmacophore Based Designing of Potential Drugs from Gymnema sylvestre against Insulin Receptor Protein Abstract Abstract Diabetes mellitus (DM) is one of the most prevalent metabolic disorders which can affect the quality of life severely. Injectable insulin is currently being used to trea... |
PMC12886327 | core_pubmed_pmc | Human metabolism and pharmacological profiling of protonitazepyne and metonitazepyne, two highly potent nitazenes: prediction of main metabolite activity based on µ-opioid receptor docking simulations | Human metabolism and pharmacological profiling of protonitazepyne and metonitazepyne, two highly potent nitazenes: prediction of main metabolite activity based on µ-opioid receptor docking simulations Abstract Abstract Nitazenes have recently surfaced the illicit opioid market, causing numerous intoxications and fatali... |
PMC6054689 | core_pubmed_pmc | CYP2C9 and OATP1B1 genetic polymorphisms affect the metabolism and transport of glimepiride and gliclazide | CYP2C9 and OATP1B1 genetic polymorphisms affect the metabolism and transport of glimepiride and gliclazide Abstract The therapeutic use of glimepiride and gliclazide shows substantial inter-individual variation in pharmacokinetics and pharmacodynamics in human populations, which might be caused by genetic differences a... |
PMC4574542 | core_pubmed_pmc | Artemether-lumefantrine treatment of uncomplicated Plasmodium falciparum malaria: a systematic review and meta-analysis of day 7 lumefantrine concentrations and therapeutic response using individual patient data | Artemether-lumefantrine treatment of uncomplicated Plasmodium falciparum malaria: a systematic review and meta-analysis of day 7 lumefantrine concentrations and therapeutic response using individual patient data Abstract Abstract Background Achieving adequate antimalarial drug exposure is essential for curing malaria. ... |
PMC12414727 | core_pubmed_pmc | Treatment modifiers and predictors of risperidone response in dementia: An individual participant data meta‐analysis of six randomized controlled trials | Treatment modifiers and predictors of risperidone response in dementia: An individual participant data meta‐analysis of six randomized controlled trials Abstract Abstract INTRODUCTION Risperidone is approved for behaviors and psychological symptoms of dementia (BPSD), despite modest efficacy and known risks. Identifyin... |
PMC11717999 | core_pubmed_pmc | Influence of ABCB1 polymorphisms on aripiprazole and dehydroaripiprazole plasma concentrations | Influence of ABCB1 polymorphisms on aripiprazole and dehydroaripiprazole plasma concentrations Abstract Abstract Aripiprazole (ARI) is an atypical antipsychotic which is a substrate of P-glycoprotein (P-gp), a transmembrane glycoprotein that plays a crucial role in eliminating potentially harmful compounds from the org... |
PMC6838446 | core_pubmed_pmc | SPARC dependent collagen deposition and gemcitabine delivery in a genetically engineered mouse model of pancreas cancer | SPARC dependent collagen deposition and gemcitabine delivery in a genetically engineered mouse model of pancreas cancer Abstract Background Pancreatic ductal adenocarcinoma (PDAC) is characterised by extensive matrix deposition that has been implicated in impaired drug delivery and therapeutic resistance. Secreted prot... |
PMC12031437 | core_pubmed_pmc | A Preliminary Evaluation of the Comparative Efficacy of Gel-Based and Oil-Based CBD on Hematologic and Biochemical Responses in Dogs | A Preliminary Evaluation of the Comparative Efficacy of Gel-Based and Oil-Based CBD on Hematologic and Biochemical Responses in Dogs Abstract Simple Summary Cannabidiol (CBD) is increasingly used in dogs to alleviate stress, pain, and inflammation. However, oral administration has limitations due to poor bioavailabilit... |
PMC7467447 | core_pubmed_pmc | Implementation of a Reference-Scaled Average Bioequivalence Approach for Highly Variable Acetylsalicylic Acid in Fixed-Dose Combination with Clopidogrel Versus Enteric Aspirin in Chinese Subjects Under Fasting Conditions: A Phase 1, Open-Label, Randomized, Crossover Study | Implementation of a Reference-Scaled Average Bioequivalence Approach for Highly Variable Acetylsalicylic Acid in Fixed-Dose Combination with Clopidogrel Versus Enteric Aspirin in Chinese Subjects Under Fasting Conditions: A Phase 1, Open-Label, Randomized, Crossover Study Abstract Abstract Introduction Dual antiplatele... |
PMC12706403 | core_pubmed_pmc | LSTM‐Based Prediction of Human PK Profiles and Parameters for Intravenous Small Molecule Drugs Using ADME and Physicochemical Properties | LSTM‐Based Prediction of Human PK Profiles and Parameters for Intravenous Small Molecule Drugs Using ADME and Physicochemical Properties Abstract ABSTRACT Accurate prediction of human pharmacokinetics (PK) for lead compounds is one of the critical determinants of successful drug development. Traditional methods for PK ... |
PMC4425236 | core_pubmed_pmc | Pharmacokinetics of mitragynine in man | Pharmacokinetics of mitragynine in man Abstract Abstract Background Kratom, known botanically as Mitragyna speciosa (Korth.), is an indigenous tree in Southeast Asia. Kratom is currently easily available worldwide via special shops and the Internet to use as a drug of abuse, opioid alternative, or pain killer. So far, ... |
PMC11775066 | core_pubmed_pmc | The Influence of High Body Mass Index (BMI > 35 kg/m 2 ) on Apixaban Plasma Concentration in Patients with Atrial Fibrillation | The Influence of High Body Mass Index (BMI > 35 kg/m 2 ) on Apixaban Plasma Concentration in Patients with Atrial Fibrillation Abstract Purpose Apixaban, a direct oral anticoagulant is administered for stroke prevention in atrial fibrillation patients. Dosing adjustment is guided by renal function, age, and body weight... |
PMC8302242 | core_pubmed_pmc | An artificial neural network−pharmacokinetic model and its interpretation using Shapley additive explanations | An artificial neural network−pharmacokinetic model and its interpretation using Shapley additive explanations Abstract Abstract We developed a method to apply artificial neural networks (ANNs) for predicting time‐series pharmacokinetics (PKs), and an interpretable the ANN‐PK model, which can explain the evidence of pre... |
PMC5989765 | core_pubmed_pmc | The safety, tolerability, and pharmacokinetic profile of GSK 2838232, a novel 2nd generation HIV maturation inhibitor, as assessed in healthy subjects | The safety, tolerability, and pharmacokinetic profile of GSK 2838232, a novel 2nd generation HIV maturation inhibitor, as assessed in healthy subjects Abstract Abstract This work aimed to assess the safety, tolerability, pharmacokinetics ( PK ), and relative bioavailability of GSK 2838232, an investigational HIV matura... |
PMC4171493 | core_pubmed_pmc | Investigation of 6-[ 18 F]-Fluoromaltose as a Novel PET Tracer for Imaging Bacterial Infection | Investigation of 6-[ 18 F]-Fluoromaltose as a Novel PET Tracer for Imaging Bacterial Infection Abstract Despite advances in the field of nuclear medicine, the imaging of bacterial infections has remained a challenge. The existing reagents suffer from poor sensitivity and specificity. In this study we investigate the po... |
PMC11260762 | core_pubmed_pmc | Pharmacokinetic drug–drug interactions of JBPOS0101 mediated by cytochrome P450 3A4 and UDP‐glucuronosyltransferases | Pharmacokinetic drug–drug interactions of JBPOS0101 mediated by cytochrome P450 3A4 and UDP‐glucuronosyltransferases Abstract Abstract JBPOS0101 is a new antiepileptic drug and is a substrate of UDP‐glucuronosyltransferases (UGTs) in in vitro test. In vitro experiments showed different results regarding whether JBPOS01... |
PMC4303928 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Safety of Peginterferon Beta-Ia in Subjects with Normal or Impaired Renal Function | Pharmacokinetics, Pharmacodynamics, and Safety of Peginterferon Beta-Ia in Subjects with Normal or Impaired Renal Function Abstract Peginterferon beta-1a was efficacious in a Phase 3 relapsing multiple sclerosis trial, and its safety profile was consistent with other beta interferons. This study evaluated the impact of... |
PMC12564180 | core_pubmed_pmc | Investigation of the Relevance of CYP3A4 Inhibition on the Pharmacokinetics of the Novel P2X3 Antagonist Filapixant: Results of In Vitro Explorations and a Fixed-Sequence Clinical Trial with Itraconazole in Healthy Volunteers | Investigation of the Relevance of CYP3A4 Inhibition on the Pharmacokinetics of the Novel P2X3 Antagonist Filapixant: Results of In Vitro Explorations and a Fixed-Sequence Clinical Trial with Itraconazole in Healthy Volunteers Abstract Hypersensitized P2X3 receptor signaling has been described to play a role in several ... |
PMC5038291 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model of Isoniazid and Its Application in Individualizing Tuberculosis Chemotherapy | A Physiologically Based Pharmacokinetic Model of Isoniazid and Its Application in Individualizing Tuberculosis Chemotherapy Abstract Abstract Due to its high early bactericidal activity, isoniazid (INH) plays an essential role in tuberculosis treatment. Genetic polymorphisms of N -acetyltransferase type 2 (NAT2) cause ... |
PMC3564460 | core_pubmed_pmc | A Phase 1, randomized, open-label crossover study to evaluate the safety and pharmacokinetics of 400 mg albaconazole administered to healthy participants as a tablet formulation versus a capsule formulation | A Phase 1, randomized, open-label crossover study to evaluate the safety and pharmacokinetics of 400 mg albaconazole administered to healthy participants as a tablet formulation versus a capsule formulation Abstract Background Albaconazole is a novel triazole being developed for the oral treatment of fungal diseases. O... |
PMC6825114 | core_pubmed_pmc | Factors Influencing the Safety and Efficiency of Antifungal Prophylaxis with Posaconazole in Children with Hematological Diseases: From Genetics to Polypharmacotherapy | Factors Influencing the Safety and Efficiency of Antifungal Prophylaxis with Posaconazole in Children with Hematological Diseases: From Genetics to Polypharmacotherapy Abstract Abstract The aim of this study was to determine the impact of ABCB1 polymorphism, BMI, age and drug co-administration on safety and efficiency ... |
PMC11077034 | core_pubmed_pmc | Pharmacokinetics and antioxidant activity of dihydrocaffeic acid grafted chitosan nanomicelles loaded with chicoric acid in broilers | Pharmacokinetics and antioxidant activity of dihydrocaffeic acid grafted chitosan nanomicelles loaded with chicoric acid in broilers Abstract Chicoric acid ( CA ) is a natural nutrient found in plants, showcasing diverse biological activities, including anti-inflammatory and antioxidant properties. Despite its valuable... |
PMC4829506 | core_pubmed_pmc | Dispositions of enrofloxacin and its major metabolite ciprofloxacin in Thai swamp buffaloes | Dispositions of enrofloxacin and its major metabolite ciprofloxacin in Thai swamp buffaloes Abstract Given the limited information available in this species, the aim of this study was to investigate the pharmacokinetic characteristics of enrofloxacin (ER) and its major metabolite ciprofloxacin (CP) in buffaloes, Bubalu... |
PMC12098388 | core_pubmed_pmc | Optimization of meropenem dosing regimens in critically ill patients with augmented renal clearance | Optimization of meropenem dosing regimens in critically ill patients with augmented renal clearance Abstract Abstract The pharmacokinetics of meropenem are significantly altered in patients with augmented renal clearance (ARC), resulting in suboptimal plasma concentrations. The objective of this study is to investigate... |
PMC6177703 | core_pubmed_pmc | Target site pharmacokinetics of doxycycline for rosacea in healthy volunteers is independent of the food effect | Target site pharmacokinetics of doxycycline for rosacea in healthy volunteers is independent of the food effect Abstract Abstract Aims Doxycycline (DFD‐09) oral capsules 40 mg are approved for the treatment of inflammatory lesions of rosacea. Unlike the food‐induced lowering of doxycycline's peak plasma concentration (... |
PMC5064996 | core_pubmed_pmc | The promises of quantitative systems pharmacology modelling for drug development | The promises of quantitative systems pharmacology modelling for drug development Abstract Recent growth in annual new therapeutic entity (NTE) approvals by the U.S. Food and Drug Administration (FDA) suggests a positive trend in current research and development (R&D) output. Prior to this, the cost of each NTE was cons... |
PMC10006245 | core_pubmed_pmc | CYP2C9 Polymorphisms and the Risk of Cardiovascular Events in Patients Treated with Clopidogrel: Combined Data from the POPular Genetics and POPular AGE Trials | CYP2C9 Polymorphisms and the Risk of Cardiovascular Events in Patients Treated with Clopidogrel: Combined Data from the POPular Genetics and POPular AGE Trials Abstract Background The cytochrome P450 (CYP) 2C9 enzyme plays a role in the metabolization of clopidogrel. Carriage of a CYP2C9 loss-of-function (LoF) allele h... |
PMC10016219 | core_pubmed_pmc | Brief History of Opioids in Perioperative and Periprocedural Medicine to Inform the Future | Brief History of Opioids in Perioperative and Periprocedural Medicine to Inform the Future Abstract Background: Opioids and derivatives of opium had been used as analgesics for thousands of years before the introduction of inhalational anesthetic agents. Once these early volatile agents were in widespread use, opioids ... |
PMC6717342 | core_pubmed_pmc | Novel analytical methods to interpret large sequencing data from small sample sizes | Novel analytical methods to interpret large sequencing data from small sample sizes Abstract Abstract Background Targeted therapies have greatly improved cancer patient prognosis. For instance, chronic myeloid leukemia is now well treated with imatinib, a tyrosine kinase inhibitor. Around 80% of the patients reach comp... |
PMC11860126 | core_pubmed_pmc | X-Ray Irradiation Induces Oxidative Stress and Upregulates Intestinal Nrf2-Mrp2 Pathway, Leading to Decreased Intestinal Absorption of Valsartan | X-Ray Irradiation Induces Oxidative Stress and Upregulates Intestinal Nrf2-Mrp2 Pathway, Leading to Decreased Intestinal Absorption of Valsartan Abstract Abstract Background: It has been documented that radiation can influence the pharmacokinetics of chemotherapy drugs, yet the underlying mechanisms remain poorly under... |
PMC11402040 | core_pubmed_pmc | PF-06952229, a selective TGF-β-R1 inhibitor: preclinical development and a first-in-human, phase I, dose-escalation study in advanced solid tumors | PF-06952229, a selective TGF-β-R1 inhibitor: preclinical development and a first-in-human, phase I, dose-escalation study in advanced solid tumors Abstract Background PF-06952229 is a selective small-molecule inhibitor of transforming growth factor-β (TGF-β) receptor 1. We evaluated its antitumor activity in preclinica... |
PMC5038304 | core_pubmed_pmc | Amikacin Optimal Exposure Targets in the Hollow-Fiber System Model of Tuberculosis | Amikacin Optimal Exposure Targets in the Hollow-Fiber System Model of Tuberculosis Abstract Aminoglycosides such as amikacin are currently used for the treatment of multidrug-resistant tuberculosis (MDR-TB). However, formal pharmacokinetic/pharmacodynamic (PK/PD) studies to identify amikacin exposures and dosing schedu... |
PMC10797295 | core_pubmed_pmc | Deep learning for automatic organ and tumor segmentation in nanomedicine pharmacokinetics | Deep learning for automatic organ and tumor segmentation in nanomedicine pharmacokinetics Abstract Rationale : Multimodal imaging provides important pharmacokinetic and dosimetry information during nanomedicine development and optimization. However, accurate quantitation is time-consuming, resource intensive, and requi... |
PMC8979486 | core_pubmed_pmc | Augmented Renal Clearance in Severe Infections—An Important Consideration in Vancomycin Dosing: A Narrative Review | Augmented Renal Clearance in Severe Infections—An Important Consideration in Vancomycin Dosing: A Narrative Review Abstract Abstract Vancomycin is a hydrophilic antibiotic widely used in severe infections, including bacteremia and central nervous system (CNS) infections caused by Gram-positive bacteria such as methicil... |
PMC11179706 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of imatinib and N ‐desmethyl imatinib for drug–drug interaction predictions | Physiologically based pharmacokinetic modeling of imatinib and N ‐desmethyl imatinib for drug–drug interaction predictions Abstract Abstract The first‐generation tyrosine kinase inhibitor imatinib has revolutionized the development of targeted cancer therapy and remains among the frontline treatments, for example, agai... |
PMC10823479 | core_pubmed_pmc | First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT 6 Agents with a Beneficial Neuroprotective Profile against Alzheimer’s Disease | First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT 6 Agents with a Beneficial Neuroprotective Profile against Alzheimer’s Disease Abstract Abstract Alzheimer’s disease (AD) has a complex and not-fully-understood etiology. Recently, the serotonin receptor 5-HT 6 emerged as a promising target for AD treatm... |
PMC11863741 | core_pubmed_pmc | Synergistic activity of nootropic herbs as potent therapeutics for Alzheimer's disease: A cheminformatics, pharmacokinetics, and system pharmacology approach | Synergistic activity of nootropic herbs as potent therapeutics for Alzheimer's disease: A cheminformatics, pharmacokinetics, and system pharmacology approach Abstract Background Alzheimer's disease (AD) is a progressive neurodegenerative disorder, which subdues over 55 million people and finding a cure, still remains d... |
PMC7540988 | core_pubmed_pmc | Lorlatinib in previously treated anaplastic lymphoma kinase‐rearranged non–small cell lung cancer: Japanese subgroup analysis of a global study | Lorlatinib in previously treated anaplastic lymphoma kinase‐rearranged non–small cell lung cancer: Japanese subgroup analysis of a global study Abstract Abstract Lorlatinib is a potent, brain‐penetrant, third‐generation anaplastic lymphoma kinase (ALK)/ROS proto‐oncogene 1 (ROS1) tyrosine kinase inhibitor (TKI) that is... |
PMC5908314 | core_pubmed_pmc | Pharmacogenetics-based area-under-curve model can predict efficacy and adverse events from axitinib in individual patients with advanced renal cell carcinoma | Pharmacogenetics-based area-under-curve model can predict efficacy and adverse events from axitinib in individual patients with advanced renal cell carcinoma Abstract Abstract We investigated the relationship between axitinib pharmacogenetics and clinical efficacy/adverse events in advanced renal cell carcinoma (RCC) a... |
PMC4208661 | core_pubmed_pmc | SGLT2 inhibitors act from the extracellular surface of the cell membrane | SGLT2 inhibitors act from the extracellular surface of the cell membrane Abstract Abstract SGLT2 inhibitors are a new class of drugs that have been recently developed to treat type II diabetes. They lower glucose levels by inhibiting the renal Na + /glucose cotransporter SGLT2, thereby increasing the amount of glucose ... |
PMC5100660 | core_pubmed_pmc | Evaluation of a novel autoinjector for subcutaneous self-administration of belimumab in systemic lupus erythematosus | Evaluation of a novel autoinjector for subcutaneous self-administration of belimumab in systemic lupus erythematosus Abstract Objective: To study self-administration and pharmacokinetics (PK) of subcutaneous (SC) belimumab in patients with systemic lupus erythematosus (SLE). Methods: Patients previously treated with be... |
PMC9904295 | core_pubmed_pmc | Novel Pt(IV) prodrug self-assembled nanoparticles with enhanced blood circulation stability and improved antitumor capacity of oxaliplatin for cancer therapy | Novel Pt(IV) prodrug self-assembled nanoparticles with enhanced blood circulation stability and improved antitumor capacity of oxaliplatin for cancer therapy Abstract Abstract Pt(IV) compounds are regarded as prodrugs of active Pt(II) drugs (i.e. cisplatin, carboplatin, and oxaliplatin) and burgeoned as the most ideal ... |
PMC8735617 | core_pubmed_pmc | Pharmacokinetics of a 503B outsourcing facility-produced theophylline in dogs | Pharmacokinetics of a 503B outsourcing facility-produced theophylline in dogs Abstract Abstract Theophylline is an important drug for treatment of canine chronic bronchitis and bradyarrhythmias, but new products require validation since pharmacokinetics in dogs can vary by formulation. A new, 503B outsourcing facility-... |
PMC11769258 | core_pubmed_pmc | Snake Venom Pharmacokinetics and Acute Toxic Outcomes Following Daboia siamensis Envenoming: Experimental and Clinical Correlations | Snake Venom Pharmacokinetics and Acute Toxic Outcomes Following Daboia siamensis Envenoming: Experimental and Clinical Correlations Abstract An understanding of snake venom pharmacokinetics is essential for determining clinical outcomes of envenoming and developing therapeutic approaches to the treatment of envenoming,... |
PMC3555879 | core_pubmed_pmc | ABCB1 Variation and Treatment Response in AIDS Patients: Initial Results of the Henan Cohort | ABCB1 Variation and Treatment Response in AIDS Patients: Initial Results of the Henan Cohort Abstract Abstract HIV/AIDS has the highest mortality among infectious diseases in China. In ongoing efforts to alleviate this crisis, the national government has placed great emphasis on efforts in Henan province where HIV-infe... |
PMC4048666 | core_pubmed_pmc | Method of variability optimization in pharmacokinetic data analysis | Method of variability optimization in pharmacokinetic data analysis Abstract For many drugs administered per os , high variability in the concentration–time (C–T) values from first sampling to the phase of distribution may cause difficulty in pharmacokinetic analysis. Therefore, the aim of this study was to propose a m... |
PMC8199036 | core_pubmed_pmc | Improved Tumor-Targeting with Peptidomimetic Analogs of Minigastrin 177 Lu-PP-F11N | Improved Tumor-Targeting with Peptidomimetic Analogs of Minigastrin 177 Lu-PP-F11N Abstract Simple Summary Several radiolabeled peptides targeting CCK2R-positive types of cancer (such as medullary thyroid cancer and small cell lung cancer) have been reported in the last 25 years, some of which have entered clinical tri... |
PMC5288422 | core_pubmed_pmc | Analytical Methods for Determining Third and Fourth Generation Fluoroquinolones: A Review | Analytical Methods for Determining Third and Fourth Generation Fluoroquinolones: A Review Abstract Abstract Abstract Fluoroquinolones of the third and fourth generation posses wide bactericidal activity. Monitoring concentrations of antibacterial agents provides effective therapy and prevents the increase of bacterial ... |
PMC12220524 | core_pubmed_pmc | Infections and mortality in ICU patients undergoing continuous renal replacement therapy: a retrospective cohort study | Infections and mortality in ICU patients undergoing continuous renal replacement therapy: a retrospective cohort study Abstract Background Critically ill patients receiving continuous renal replacement therapy (CRRT) are at increased risk for multidrug-resistant infections and infection-related mortality. Altered pharm... |
PMC8396642 | core_pubmed_pmc | Investigation of Bemethyl Biotransformation Pathways by Combination of LC–MS/HRMS and In Silico Methods | Investigation of Bemethyl Biotransformation Pathways by Combination of LC–MS/HRMS and In Silico Methods Abstract Abstract Bemethyl is an actoprotector, an antihypoxant, and a moderate psychostimulant. Even though the therapeutic effectiveness of bemethyl is well documented, there is a gap in knowledge regarding its met... |
PMC6973014 | core_pubmed_pmc | Randomized Population Pharmacokinetic Analysis and Safety of Intravenous Acetaminophen for Acute Postoperative Pain in Neonates and Infants | Randomized Population Pharmacokinetic Analysis and Safety of Intravenous Acetaminophen for Acute Postoperative Pain in Neonates and Infants Abstract Abstract Intravenous administration of acetaminophen is an alternative to the oral and rectal routes, which may be contraindicated in particular clinical settings. This ra... |
PMC12661794 | core_pubmed_pmc | Bioinformatics analysis of Rickettsia typhi autoimmune associations and screening of Streptomyces-derived inhibitors | Bioinformatics analysis of Rickettsia typhi autoimmune associations and screening of Streptomyces-derived inhibitors Abstract Background Rickettsia typhi is the causative agent of epidemic murine typhus and Rocky Mountain spotted fever. The infection can affect multiple vital organs, including the heart, lungs, kidneys... |
PMC6331591 | core_pubmed_pmc | Deducing Mucosal Pharmacokinetics and Pharmacodynamics of the Anti-HIV Molecule Tenofovir from Measurements in Blood | Deducing Mucosal Pharmacokinetics and Pharmacodynamics of the Anti-HIV Molecule Tenofovir from Measurements in Blood Abstract Abstract Microbicide pharmacokinetic (PK) studies typically sample drug in luminal fluid, mucosal tissue, and blood. Blood measurements can be conducted most frequently, serially within subjects... |
PMC12484717 | core_pubmed_pmc | North American Society for Pediatric Gastroenterology, Hepatology, and Nutrition position paper on the therapeutic drug monitoring in pediatric inflammatory bowel disease | North American Society for Pediatric Gastroenterology, Hepatology, and Nutrition position paper on the therapeutic drug monitoring in pediatric inflammatory bowel disease Abstract Abstract Inflammatory bowel diseases (IBD) require effective therapies to prevent morbidity and maintain quality of life. The introduction o... |
PMC12930287 | core_pubmed_pmc | Assessment and Benchmarking of Model Informed Approaches in Drug Development for Hemoglobinopathies: A Review of Scientific Advices From January 2000 to December 2024 | Assessment and Benchmarking of Model Informed Approaches in Drug Development for Hemoglobinopathies: A Review of Scientific Advices From January 2000 to December 2024 Abstract ABSTRACT Despite the fact that modeling and simulation are now recognized as promising innovative methodologies, their use in the context of dev... |
PMC12914733 | core_pubmed_pmc | Multiscale physiologically-based model of age-dependent CD4+ T-lymphocyte homeostasis | Multiscale physiologically-based model of age-dependent CD4+ T-lymphocyte homeostasis Abstract Objective To develop a mechanistic physiologically-based model describing CD4 + T-lymphocyte homeostasis across the human lifespan, incorporating maturation, differentiation, migration aspects and the impact of age on distinc... |
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