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PMC3626541 | core_pubmed_pmc | A first in human, safety, pharmacokinetics, and clinical activity phase I study of once weekly administration of the Hsp90 inhibitor ganetespib (STA-9090) in patients with solid malignancies | A first in human, safety, pharmacokinetics, and clinical activity phase I study of once weekly administration of the Hsp90 inhibitor ganetespib (STA-9090) in patients with solid malignancies Abstract Background This phase I study investigated the maximum tolerated dose (MTD), safety, pharmacokinetics and antitumor acti... |
PMC9028393 | core_pubmed_pmc | Tigecycline Dosing Strategies in Critically Ill Liver-Impaired Patients | Tigecycline Dosing Strategies in Critically Ill Liver-Impaired Patients Abstract Abstract This study investigated tigecycline exposure in critically ill patients from a population pharmacokinetic perspective to support rational dosing in intensive care unit (ICU) patients with acute and chronic liver impairment. A clin... |
PMC8400696 | core_pubmed_pmc | Development, Characterization, and In Vivo Evaluation of a Novel Aptamer (Anti-MUC1/Y) for Breast Cancer Therapy | Development, Characterization, and In Vivo Evaluation of a Novel Aptamer (Anti-MUC1/Y) for Breast Cancer Therapy Abstract MUC1, the transmembrane glycoprotein Mucin 1, is usually found to be overexpressed in a variety of epithelial cancers playing an important role in disease progression. MUC1 isoforms such as MUC1/Y, ... |
PMC9101701 | core_pubmed_pmc | Computational studies on potential new anti-Covid-19 agents with a multi-target mode of action | Computational studies on potential new anti-Covid-19 agents with a multi-target mode of action Abstract Abstract A compound that could inhibit multiple targets associated with SARS-CoV-2 infection would prove to be a drug of choice against the virus. Human receptor-ACE2, receptor binding domain (RBD) of SARS-CoV-2 S-pr... |
PMC4928348 | core_pubmed_pmc | Combination therapy in cancer: effects of angiogenesis inhibitors on drug pharmacokinetics and pharmacodynamics | Combination therapy in cancer: effects of angiogenesis inhibitors on drug pharmacokinetics and pharmacodynamics Abstract Abstract Validated preclinical studies have provided evidence that anti-vascular endothelial growth factor (VEGF) compounds enhance the activity of subsequent antitumor therapy, but the mechanism of ... |
PMC12324405 | core_pubmed_pmc | Tigecycline pharmacodynamics in the hollow fiber system of Mycobacterium avium -complex lung disease, and the utility of MICs and time-kill studies in drug development | Tigecycline pharmacodynamics in the hollow fiber system of Mycobacterium avium -complex lung disease, and the utility of MICs and time-kill studies in drug development Abstract Abstract Background: Guideline-based therapy (GBT) drugs for Mycobacterium avium-complex (MAC) lung disease (LD) were chosen in part because th... |
PMC10955605 | core_pubmed_pmc | The impact of skin color and tone on histamine iontophoresis and Doppler flowmetry measurements as a pharmacodynamic biomarker | The impact of skin color and tone on histamine iontophoresis and Doppler flowmetry measurements as a pharmacodynamic biomarker Abstract Abstract The phenotypical manifestations of asthma among children are diverse and exhibit varying responses to therapeutic interventions. There is a need to develop objective biomarker... |
PMC8652414 | core_pubmed_pmc | The More, the Merrier…? Antipsychotic Polypharmacy Treatment Strategies in Schizophrenia From a Pharmacology Perspective | The More, the Merrier…? Antipsychotic Polypharmacy Treatment Strategies in Schizophrenia From a Pharmacology Perspective Abstract Antipsychotic polypharmacy/drug combination treatment (APP) is a remarkably common practice in the schizophrenia context, given the lack of general support in treatment Guidelines. There is ... |
PMC5094543 | core_pubmed_pmc | In Vitro and In Vivo Characterization of a Fully Felinized Therapeutic Anti‐Nerve Growth Factor Monoclonal Antibody for the Treatment of Pain in Cats | In Vitro and In Vivo Characterization of a Fully Felinized Therapeutic Anti‐Nerve Growth Factor Monoclonal Antibody for the Treatment of Pain in Cats Abstract Abstract Background Limited options are available for the treatment of pain in cats. Monoclonal antibodies (mAbs) that neutralize nerve growth factor (NGF) have ... |
PMC6060940 | core_pubmed_pmc | A pilot study to determine the occurrence of concomitant diseases and drug intake in patients on antituberculosis therapy | A pilot study to determine the occurrence of concomitant diseases and drug intake in patients on antituberculosis therapy Abstract Abstract Introduction: Altered pharmacokinetics of antituberculosis (anti-TB) drugs due to interaction with non-TB medications or concomitant diseases may lead to suboptimal plasma levels o... |
PMC11330225 | core_pubmed_pmc | Dose–exposure–efficacy response of intravenous immunoglobulin G 10% in multifocal motor neuropathy | Dose–exposure–efficacy response of intravenous immunoglobulin G 10% in multifocal motor neuropathy Abstract Abstract Objective Multifocal motor neuropathy is a rare chronic immune‐mediated neuropathy with impaired grip strength representing a common symptom. While intravenous immunoglobulin G is an effective treatment ... |
PMC11706429 | core_pubmed_pmc | Physiology‐based pharmacokinetic model with relative transcriptomics to evaluate tissue distribution and receptor occupancy of anifrolumab | Physiology‐based pharmacokinetic model with relative transcriptomics to evaluate tissue distribution and receptor occupancy of anifrolumab Abstract Abstract Type I interferons contribute to the pathogenesis of several autoimmune disorders, including systemic lupus erythematosus (SLE), systemic sclerosis, cutaneous lupu... |
PMC12258201 | core_pubmed_pmc | Rationale and design of the GLADE study: a randomized, multicenter, double-blind, placebo-controlled trial evaluating the safety and efficacy of gestrinone subdermal bioabsorbable pellet in endometriosis-related pelvic pain | Rationale and design of the GLADE study: a randomized, multicenter, double-blind, placebo-controlled trial evaluating the safety and efficacy of gestrinone subdermal bioabsorbable pellet in endometriosis-related pelvic pain Abstract Abstract Background Pelvic pain secondary to endometriosis is a disabling condition. Th... |
PMC7198115 | core_pubmed_pmc | Model-Informed Drug Development for Malaria Therapeutics | Model-Informed Drug Development for Malaria Therapeutics Abstract Abstract Malaria is a critical public health problem resulting in substantial morbidity and mortality, particularly in developing countries. Owing to the development of resistance toward current therapies, novel approaches to accelerate the development e... |
PMC7114774 | core_pubmed_pmc | Pharmacokinetic Comparisons of Different Combinations of Yigan Jiangzhi Formula in Rats: Simultaneous Determination of Fourteen Components by UPLC-MS/MS | Pharmacokinetic Comparisons of Different Combinations of Yigan Jiangzhi Formula in Rats: Simultaneous Determination of Fourteen Components by UPLC-MS/MS Abstract A rapid, specific, and sensitive analysis for simultaneous determination of fourteen components (daidzein, fermononetin, apigenin, luteolin, puerarin, ononin,... |
PMC6030804 | core_pubmed_pmc | Sites of gastrointestinal lesion induced by mycophenolate mofetil: a comparison with enteric-coated mycophenolate sodium in rats | Sites of gastrointestinal lesion induced by mycophenolate mofetil: a comparison with enteric-coated mycophenolate sodium in rats Abstract Background Immunosuppressant drugs for renal transplant mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS) cause gastrointestinal (GI) disorders. The specif... |
PMC6056278 | core_pubmed_pmc | Nuclear Factor of Activated T Cell-regulated Cytokine Gene Expression for Adjustment of Tacrolimus in Kidney Transplant Recipients: A Randomized Controlled Pilot Trial | Nuclear Factor of Activated T Cell-regulated Cytokine Gene Expression for Adjustment of Tacrolimus in Kidney Transplant Recipients: A Randomized Controlled Pilot Trial Abstract Background The aim of this pilot study was to assess the feasibility of a pharmacodynamics assay that measures Nuclear Factor of Activated T Ce... |
PMC5975598 | core_pubmed_pmc | Defining the potency of amikacin against Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa , and Acinetobacter baumannii derived from Chinese hospitals using CLSI and inhalation-based breakpoints | Defining the potency of amikacin against Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa , and Acinetobacter baumannii derived from Chinese hospitals using CLSI and inhalation-based breakpoints Abstract Objectives We report the in vitro activity of amikacin and comparators against Gram-negative bacteria... |
PMC5864138 | core_pubmed_pmc | Development of Tizanidine HCl-Meloxicam loaded mucoadhesive buccal films: In-vitro and in-vivo evaluation | Development of Tizanidine HCl-Meloxicam loaded mucoadhesive buccal films: In-vitro and in-vivo evaluation Abstract The purpose of the study was to develop Tizanidine HCl (TZN) and Meloxicam (MLX) loaded bilayer mucoadhesive films intended for buccal administration, aiming to enhance the bioavailability. Bilayer films w... |
PMC8141531 | core_pubmed_pmc | NKTR-358: A novel regulatory T-cell stimulator that selectively stimulates expansion and suppressive function of regulatory T cells for the treatment of autoimmune and inflammatory diseases | NKTR-358: A novel regulatory T-cell stimulator that selectively stimulates expansion and suppressive function of regulatory T cells for the treatment of autoimmune and inflammatory diseases Abstract Impaired interleukin-2 (IL-2) production and regulatory T-cell dysfunction have been implicated as immunological mechanis... |
PMC8536065 | core_pubmed_pmc | Strategies to Control Human Health Risks Arising from Antibiotics in the Environment: Molecular Modification of QNs for Enhanced Plant–Microbial Synergistic Degradation | Strategies to Control Human Health Risks Arising from Antibiotics in the Environment: Molecular Modification of QNs for Enhanced Plant–Microbial Synergistic Degradation Abstract Abstract In the present work, a comprehensive screening and evaluation system was established to improve the plant–microbial synergistic degra... |
PMC12392212 | core_pubmed_pmc | Intraperitoneally Administered Vancomycin Results in Suboptimal Serum and Peritoneal Effluent Drug Levels in Patients with PD-related Peritonitis | Intraperitoneally Administered Vancomycin Results in Suboptimal Serum and Peritoneal Effluent Drug Levels in Patients with PD-related Peritonitis Abstract Abstract Background Intraperitoneal vancomycin is commonly used to treat peritoneal dialysis (PD)-related peritonitis. Therapeutic drug level monitoring helps optimi... |
PMC9772231 | core_pubmed_pmc | Preparation, characterization and in-vivo efficacy study of glatiramer acetate (GA)-hydrogel-microparticles as novel drug delivery system for GA in RRMS | Preparation, characterization and in-vivo efficacy study of glatiramer acetate (GA)-hydrogel-microparticles as novel drug delivery system for GA in RRMS Abstract Relapsing Remitting Multiple Sclerosis is a chronic Central nervous system autoimmune disease. There is no absolute treatment for MS and the available remedie... |
PMC9807524 | core_pubmed_pmc | Drug formulation augments the therapeutic response of carboplatin administered through a lymphatic drug delivery system | Drug formulation augments the therapeutic response of carboplatin administered through a lymphatic drug delivery system Abstract Abstract Treatment of metastatic lymph nodes (LNs) is challenging due to their unique architecture and biophysical traits. Systemic chemotherapy fails to impede tumor progression in LNs due t... |
PMC12845014 | core_pubmed_pmc | Affinity- and Format-Dependent Pharmacokinetics of 89 Zr-Labeled Albumin-Binding VHH Constructs | Affinity- and Format-Dependent Pharmacokinetics of 89 Zr-Labeled Albumin-Binding VHH Constructs Abstract Abstract Background/Objectives: NANOBODY ® molecules (VHHs) are attractive vectors for radiopharmaceuticals due to their small size and high target affinity, but rapid clearance and pronounced kidney retention limit... |
PMC6572387 | core_pubmed_pmc | The Influence of Dimerization on the Pharmacokinetics and Activity of an Antibacterial Enzyme Lysostaphin | The Influence of Dimerization on the Pharmacokinetics and Activity of an Antibacterial Enzyme Lysostaphin Abstract The increasing prevalence of antibiotic-resistant strains of pathogenic bacteria is a major healthcare problem. Antibacterial lysins are enzymes that cleave the peptidoglycan of the bacterial cell wall. Th... |
PMC8602566 | core_pubmed_pmc | A Novel Hydroxamic Acid-Based Curcumin Derivative as Potent Histone Deacetylase Inhibitor for the Treatment of Glioblastoma | A Novel Hydroxamic Acid-Based Curcumin Derivative as Potent Histone Deacetylase Inhibitor for the Treatment of Glioblastoma Abstract Abstract Glioblastoma (GBM) is one of the most common primary and deadliest malignant brain tumor with chemoresistance and poor prognosis. There is a lack of effective chemotherapeutic dr... |
PMC4508765 | core_pubmed_pmc | Prenatal mercury exposure, autism, and developmental delay, using pharmacokinetic combination of newborn blood concentrations and questionnaire data: a case control study | Prenatal mercury exposure, autism, and developmental delay, using pharmacokinetic combination of newborn blood concentrations and questionnaire data: a case control study Abstract Abstract Background Methylmercury (MeHg), known for well over a century as a neurotoxin in adults, has more recently been studied for potent... |
PMC12430005 | core_pubmed_pmc | Methylation Enables Sensitive LC-MS/MS Quantification of Ciclopirox in a Mouse Pharmacokinetics Study | Methylation Enables Sensitive LC-MS/MS Quantification of Ciclopirox in a Mouse Pharmacokinetics Study Abstract Abstract Ciclopirox (CPX), a topical antifungal agent of the N-hydroxypyridone class, has gained renewed interest for its potential anticancer, antiviral, antibacterial, and neuroprotective effects. However, d... |
PMC12406663 | core_pubmed_pmc | Inhibition of efflux pumps by FDA-approved drugs oxiconazole and sertaconazole restores antibiotic susceptibility in multidrug-resistant S. aureus | Inhibition of efflux pumps by FDA-approved drugs oxiconazole and sertaconazole restores antibiotic susceptibility in multidrug-resistant S. aureus Abstract ABSTRACT Antibiotic resistance in Staphylococcus aureus causes major concern worldwide. In S. aureus , efflux pumps are mostly responsible for the development of mu... |
PMC3336852 | core_pubmed_pmc | Effect of intermittent hypobaric hypoxia on efficacy & clearance of drugs | Effect of intermittent hypobaric hypoxia on efficacy & clearance of drugs Abstract Abstract Background & objectives: People travelling to high altitude for occupational, recreational or religious purposes are mostly healthy and fit but sometimes they use drugs for common ailments like influenza, acute mountain sickness... |
PMC11557650 | core_pubmed_pmc | Evaluation of Drug–Drug Interaction Potential of Talquetamab, a T-Cell-Redirecting GPRC5D × CD3 Bispecific Antibody, as a Result of Cytokine Release Syndrome in Patients with Relapsed/Refractory Multiple Myeloma in MonumenTAL-1, Using a Physiologically Based Pharmacokinetic Model | Evaluation of Drug–Drug Interaction Potential of Talquetamab, a T-Cell-Redirecting GPRC5D × CD3 Bispecific Antibody, as a Result of Cytokine Release Syndrome in Patients with Relapsed/Refractory Multiple Myeloma in MonumenTAL-1, Using a Physiologically Based Pharmacokinetic Model Abstract Background Cytokine release sy... |
PMC11258331 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and pharmacodynamics of milvexian with aspirin and/or clopidogrel in healthy participants | Safety, tolerability, pharmacokinetics and pharmacodynamics of milvexian with aspirin and/or clopidogrel in healthy participants Abstract Abstract Milvexian, an oral activated Factor XI (FXIa) inhibitor, is in clinical studies where it may be combined with antiplatelet agents, including aspirin and/or clopidogrel, to p... |
PMC11596062 | core_pubmed_pmc | Substrate Specificity of ABCB Transporters Predicted by Docking Simulations Can Be Confirmed by Experimental Tests | Substrate Specificity of ABCB Transporters Predicted by Docking Simulations Can Be Confirmed by Experimental Tests Abstract Abstract ATP-binding cassette (ABC) transporters, particularly those of subfamily B, are involved in cell detoxification, multidrug resistance, drug treatment pharmacodynamics, and also ecological... |
PMC9182407 | core_pubmed_pmc | Development and Validation of an HPLC-UV Method for the Quantification of 4′-Hydroxydiclofenac Using Salicylic Acid: Future Applications for Measurement of In Vitro Drug–Drug Interaction in Rat Liver Microsomes | Development and Validation of an HPLC-UV Method for the Quantification of 4′-Hydroxydiclofenac Using Salicylic Acid: Future Applications for Measurement of In Vitro Drug–Drug Interaction in Rat Liver Microsomes Abstract Abstract Salicylic acid is a key compound in nonsteroidal anti-inflammatory drugs that has been rece... |
PMC6432247 | core_pubmed_pmc | An Osteoconductive Antibiotic Bone Eluting Putty with a Custom Polymer Matrix | An Osteoconductive Antibiotic Bone Eluting Putty with a Custom Polymer Matrix Abstract With the rising tide of antibiotic resistant bacteria, extending the longevity of the current antibiotic arsenal is becoming a necessity. Developing local, controlled release antibiotic strategies, particularly for difficult to penet... |
PMC5529735 | core_pubmed_pmc | Pharmacokinetics of Sulfadoxine and Pyrimethamine for Intermittent Preventive Treatment of Malaria During Pregnancy and After Delivery | Pharmacokinetics of Sulfadoxine and Pyrimethamine for Intermittent Preventive Treatment of Malaria During Pregnancy and After Delivery Abstract Abstract Sulfadoxine/pyrimethamine is recommended for intermittent preventative treatment of malaria during pregnancy. Data from 98 women during pregnancy and 77 after delivery... |
PMC12403563 | core_pubmed_pmc | Efficacy of carrimycin against Mycobacterium avium complex in vitro and in vivo | Efficacy of carrimycin against Mycobacterium avium complex in vitro and in vivo Abstract ABSTRACT Mycobacterium avium complex (MAC) is one of the principal pathogenic strains among nontuberculous mycobacteria . Current antibiotics have poor microbiological responses, and repurposed antibiotics are a way to meet clinica... |
PMC11823673 | core_pubmed_pmc | Population pharmacokinetics of piperacillin-tazobactam in the plasma and cerebrospinal fluid of critically ill patients | Population pharmacokinetics of piperacillin-tazobactam in the plasma and cerebrospinal fluid of critically ill patients Abstract ABSTRACT Ventriculitis in neurocritical care patients leads to significant morbidity and mortality. Antibiotic dose optimization targeting pharmacokinetic/pharmacodynamic (PK/PD) exposures as... |
PMC4857741 | core_pubmed_pmc | A novel small molecule ameliorates ocular neovascularisation and synergises with anti-VEGF therapy | A novel small molecule ameliorates ocular neovascularisation and synergises with anti-VEGF therapy Abstract Ocular neovascularisation underlies blinding eye diseases such as retinopathy of prematurity, proliferative diabetic retinopathy, and wet age-related macular degeneration. These diseases cause irreversible vision... |
PMC6147237 | core_pubmed_pmc | A Combined In Vitro/In Silico Approach to Identifying Off-Target Receptor Toxicity | A Combined In Vitro/In Silico Approach to Identifying Off-Target Receptor Toxicity Abstract Summary Many xenobiotics can bind to off-target receptors and cause toxicity via the dysregulation of downstream transcription factors. Identification of subsequent off-target toxicity in these chemicals has often required exten... |
PMC12796862 | core_pubmed_pmc | Mesenchymal stromal cell–derived extracellular vesicles in regenerative medicine: Standardisation, bioengineering and clinical translation | Mesenchymal stromal cell–derived extracellular vesicles in regenerative medicine: Standardisation, bioengineering and clinical translation Abstract Abstract Mesenchymal stromal cell-derived extracellular vesicles (MSC-EVs) have emerged as promising cell-free therapeutics that recapitulate key paracrine functions of MSC... |
PMC8731131 | core_pubmed_pmc | Molecular Docking of Phytochemicals Targeting GFRs as Therapeutic Sites for Cancer: an In Silico Study | Molecular Docking of Phytochemicals Targeting GFRs as Therapeutic Sites for Cancer: an In Silico Study Abstract Drug delivery in a safe manner is a major challenge in the drug development process. Growth factor receptors (GFRs) are known to have profound roles in the growth and progression of cancerous cells making the... |
PMC8163711 | core_pubmed_pmc | Nebivolol attenuates the anticonvulsant action of carbamazepine and phenobarbital against the maximal electroshock-induced seizures in mice | Nebivolol attenuates the anticonvulsant action of carbamazepine and phenobarbital against the maximal electroshock-induced seizures in mice Abstract Background Due to co-occurrence of seizures and cardiovascular disorders, nebivolol, a widely used selective β 1 -blocker with vasodilatory properties, may be co-administe... |
PMC12902976 | core_pubmed_pmc | Nobiletin Ameliorates Doxorubicin-Induced Nephrotoxicity by Targeting Oxidative Stress, Inflammatory, and Apoptotic Pathways: Combined In Vivo and In Silico Insights | Nobiletin Ameliorates Doxorubicin-Induced Nephrotoxicity by Targeting Oxidative Stress, Inflammatory, and Apoptotic Pathways: Combined In Vivo and In Silico Insights Abstract Abstract Doxorubicin (DOX), although effective as a chemotherapeutic agent, induces significant nephrotoxicity, limiting its clinical application... |
PMC9495429 | core_pubmed_pmc | Advancing pediatric antimicrobial stewardship: Has pharmacodynamic dosing for gram-negative infections taken effect? | Advancing pediatric antimicrobial stewardship: Has pharmacodynamic dosing for gram-negative infections taken effect? Abstract Objective: To characterize pharmacodynamic dosing strategies used at children’s hospitals using a national survey. Design: Survey. Setting: Children’s hospitals. Participants: Volunteer sample o... |
PMC9762419 | core_pubmed_pmc | In Vitro Screening and MD Simulations of Thiourea Derivatives against SARS-CoV-2 in Association with Multidrug Resistance ABCB1 Transporter | In Vitro Screening and MD Simulations of Thiourea Derivatives against SARS-CoV-2 in Association with Multidrug Resistance ABCB1 Transporter Abstract Abstract Severe acute respiratory syndrome corona virus 2 (SARS-CoV-2) is considered a global public health concern since it causes high morbidity and mortality. Recently,... |
PMC6572512 | core_pubmed_pmc | Application of Pharmacometrics in Pharmacotherapy: Open-Source Software for Vancomycin Therapeutic Drug Management | Application of Pharmacometrics in Pharmacotherapy: Open-Source Software for Vancomycin Therapeutic Drug Management Abstract Abstract The population pharmacokinetic (PK) parameters that are implemented in therapeutic drug management (TDM) software were generally obtained from a Western population and might not be adequa... |
PMC7877840 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Cenerimod, A Selective S1P 1 R Modulator, Are Not Affected by Ethnicity in Healthy Asian and White Subjects | Pharmacokinetics and Pharmacodynamics of Cenerimod, A Selective S1P 1 R Modulator, Are Not Affected by Ethnicity in Healthy Asian and White Subjects Abstract Abstract Cenerimod is a sphingosine‐1‐phosphate 1 receptor (S1P 1 R) modulator in phase II development for treatment of systemic lupus erythematosus. Its pharmaco... |
PMC6907056 | core_pubmed_pmc | The Effect of Acupoint Application of Sinomenine for Rheumatoid Arthritis Measured by Microdialysis and UPLC-MS/MS | The Effect of Acupoint Application of Sinomenine for Rheumatoid Arthritis Measured by Microdialysis and UPLC-MS/MS Abstract Abstract Objective This study aimed to investigate the treatment effects of acupoint application of sinomenine in rheumatoid arthritis (RA). RA models were constructed using male New Zealand rabbi... |
PMC9106168 | core_pubmed_pmc | Lung cancer targeting efficiency of Silibinin loaded Poly Caprolactone /Pluronic F68 Inhalable nanoparticles: In vitro and In vivo study | Lung cancer targeting efficiency of Silibinin loaded Poly Caprolactone /Pluronic F68 Inhalable nanoparticles: In vitro and In vivo study Abstract Abstract Silibinin (SB) is shown to have an anticancer properties. However, its clinical therapeutic effects have been restricted due to its low water solubility and poor abs... |
PMC11130313 | core_pubmed_pmc | Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy | Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy Abstract Abstract Hypertrophic cardiomyopathy (HCM) remains the most common cardiomyopathy in humans and cats with few preclinical pharmacologic interventional studies. Small-molecule ... |
PMC5007274 | core_pubmed_pmc | A phase I dose-escalation study of LY2875358, a bivalent MET antibody, given as monotherapy or in combination with erlotinib or gefitinib in Japanese patients with advanced malignancies | A phase I dose-escalation study of LY2875358, a bivalent MET antibody, given as monotherapy or in combination with erlotinib or gefitinib in Japanese patients with advanced malignancies Abstract Summary Background MET is a tyrosine kinase receptor involved in the regulation of cell proliferation and migration. Reported... |
PMC12684063 | core_pubmed_pmc | Sodium Valproate-Associated Thrombocytopenia in Antiepileptic Drug Polypharmacy: A Case Report and Review of the Literature | Sodium Valproate-Associated Thrombocytopenia in Antiepileptic Drug Polypharmacy: A Case Report and Review of the Literature Abstract Patient: Male, 31-year-old Final Diagnosis: Sodium valproate-associated thrombocytopenia Symptoms: Thrombocytopenia Clinical Procedure: — Specialty: Hematology Objective: Diagnostic/thera... |
PMC9686470 | core_pubmed_pmc | Population Pharmacokinetics of Prophylactic Cefazolin in Cardiac Surgery with Standard and Minimally Invasive Extracorporeal Circulation | Population Pharmacokinetics of Prophylactic Cefazolin in Cardiac Surgery with Standard and Minimally Invasive Extracorporeal Circulation Abstract The objectives of this study were to develop a population pharmacokinetic model of prophylactically administered cefazolin in patients undergoing cardiac surgery with and wit... |
PMC6756255 | core_pubmed_pmc | Optimizing Mycophenolic Acid Exposure in Kidney Transplant Recipients: Time for Target Concentration Intervention | Optimizing Mycophenolic Acid Exposure in Kidney Transplant Recipients: Time for Target Concentration Intervention Abstract The immunosuppressive agent mycophenolate is used extensively in kidney transplantation, yet dosing strategy applied varies markedly from fixed dosing (“one-dose-fits-all”), to mycophenolic acid (M... |
PMC12198324 | core_pubmed_pmc | Carfentanil stabilizes µ opioid receptor conformations that are ultra-efficient in inhibiting cAMP, resistant to naloxone or nalmefene but sensitive to naltrexone | Carfentanil stabilizes µ opioid receptor conformations that are ultra-efficient in inhibiting cAMP, resistant to naloxone or nalmefene but sensitive to naltrexone Abstract The highly potent opioid carfentanil (CAR) represents a growing health risk. CAR acts via G i/o -coupled µ opioid receptors (µOR) and exhibits ultra... |
PMC10014156 | core_pubmed_pmc | Pharmacometrics: A New Era of Pharmacotherapy and Drug Development in Low- and Middle-Income Countries | Pharmacometrics: A New Era of Pharmacotherapy and Drug Development in Low- and Middle-Income Countries Abstract Pharmacotherapy, in many cases, is practiced at a suboptimal level of performance in low- and middle-income countries (LMICs) although stupendous amounts of data are available regularly. The process of drug d... |
PMC11172649 | core_pubmed_pmc | Nonclinical Evaluation of Single-Mutant E. coli Asparaginases Obtained by Double-Mutant Deconvolution: Improving Toxicological, Immune and Inflammatory Responses | Nonclinical Evaluation of Single-Mutant E. coli Asparaginases Obtained by Double-Mutant Deconvolution: Improving Toxicological, Immune and Inflammatory Responses Abstract Acute lymphoblastic leukaemia is currently treated with bacterial L-asparaginase; however, its side effects raise the need for the development of imp... |
PMC6430157 | core_pubmed_pmc | Pediatric Dosing of Ganciclovir and Valganciclovir: How Model‐Based Simulations Can Prevent Underexposure and Potential Treatment Failure | Pediatric Dosing of Ganciclovir and Valganciclovir: How Model‐Based Simulations Can Prevent Underexposure and Potential Treatment Failure Abstract Abstract Intravenous ganciclovir and oral valganciclovir are effective in the prevention and treatment of pediatric cytomegalovirus (CMV) infection but various dosing regime... |
PMC6733418 | core_pubmed_pmc | In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats | In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats Abstract The objective of this study was to evaluate in vitro and in vivo drug release from in situ forming gels prepared with poloxamer 338 (P338) and/or 407 (P407) in N-me... |
PMC5814546 | core_pubmed_pmc | Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer’s Disease | Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer’s Disease Abstract Background ALZ-801 is an orally available, valine-conjugated prodrug of tramiprosate. Tramiprosate, the active agent, is a small-molecule β-amyloid (Aβ) anti-oligomer and agg... |
PMC10491825 | core_pubmed_pmc | Endoglin inhibitor TRC105 with or without bevacizumab for bevacizumab-refractory glioblastoma (ENDOT): a multicenter phase II trial | Endoglin inhibitor TRC105 with or without bevacizumab for bevacizumab-refractory glioblastoma (ENDOT): a multicenter phase II trial Abstract Abstract Background Glioblastoma (GBM), the most lethal primary brain tumor, has limited treatment options upon recurrence after chemoradiation and bevacizumab. TRC105 (carotuxima... |
PMC2854692 | core_pubmed_pmc | Gcg-XTEN: An Improved Glucagon Capable of Preventing Hypoglycemia without Increasing Baseline Blood Glucose | Gcg-XTEN: An Improved Glucagon Capable of Preventing Hypoglycemia without Increasing Baseline Blood Glucose Abstract Abstract Objective While the majority of current diabetes treatments focus on reducing blood glucose levels, hypoglycemia represents a significant risk associated with insulin treatment. Glucagon plays a... |
PMC6244972 | core_pubmed_pmc | Translational PK-PD modeling analysis of MCLA-128, a HER2/HER3 bispecific monoclonal antibody, to predict clinical efficacious exposure and dose | Translational PK-PD modeling analysis of MCLA-128, a HER2/HER3 bispecific monoclonal antibody, to predict clinical efficacious exposure and dose Abstract Summary Introduction MCLA-128 is a bispecific monoclonal antibody targeting the HER2 and HER3 receptors. Pharmacokinetics (PK) and pharmacodynamics (PD) of MCLA-128 h... |
PMC9322208 | core_pubmed_pmc | Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat | Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat Abstract Abstract Tangeretin, 4′,5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to poss... |
PMC5669010 | core_pubmed_pmc | HIV treatment simplification to elvitegravir/cobicistat/emtricitabine/tenofovir disproxil fumarate (E/C/F/TDF) plus darunavir: a pharmacokinetic study | HIV treatment simplification to elvitegravir/cobicistat/emtricitabine/tenofovir disproxil fumarate (E/C/F/TDF) plus darunavir: a pharmacokinetic study Abstract Background As a simplification strategy for treatment-experienced HIV-infected patients who have achieved virologic suppression on a multi-drug, multi-class ant... |
PMC12460146 | core_pubmed_pmc | Impact of metabolic enzyme activity variability on dabrafenib disposition | Impact of metabolic enzyme activity variability on dabrafenib disposition Abstract Introduction The systemic exposure of dabrafenib correlates with its adverse drug reactions. A thorough understanding of its pharmacokinetic profile is crucial for precise clinical application. Methods An optimized liver microsomal incub... |
PMC3980549 | core_pubmed_pmc | Effect of Carum carvi , a herbal bioenhancer on pharmacokinetics of antitubercular drugs: A study in healthy human volunteers | Effect of Carum carvi , a herbal bioenhancer on pharmacokinetics of antitubercular drugs: A study in healthy human volunteers Abstract Abstract Aim and Objectives: The present study was undertaken in 20 healthy human volunteers to evaluate the effect of a herbal bioenhancer, Carum carvi on pharmacokinetics of rifampici... |
PMC11007094 | core_pubmed_pmc | A comprehensive review of the botany, phytochemistry, pharmacology, and toxicology of Murrayae Folium et Cacumen | A comprehensive review of the botany, phytochemistry, pharmacology, and toxicology of Murrayae Folium et Cacumen Abstract Ethnopharmacological relevance: Murrayae Folium et Cacumen (MFC) is a plant considered to be a traditional Chinese medicine with culinary value as well. The dry leaves and twigs of Murraya paniculat... |
PMC6321737 | core_pubmed_pmc | Enantioselective Drug Recognition by Drug Transporters | Enantioselective Drug Recognition by Drug Transporters Abstract Abstract Drug transporters mediate the absorption, tissue distribution, and excretion of drugs. The cDNAs of P-glycoprotein, multidrug resistance proteins (MRPs/ABCC), breast cancer resistance protein (BCRP/ABCG2), peptide transporters (PEPTs/SLC15), proto... |
PMC7351521 | core_pubmed_pmc | Assessment of a Model-Informed Precision Dosing Platform Use in Routine Clinical Care for Personalized Busulfan Therapy in the Pediatric Hematopoietic Cell Transplantation (HCT) Population | Assessment of a Model-Informed Precision Dosing Platform Use in Routine Clinical Care for Personalized Busulfan Therapy in the Pediatric Hematopoietic Cell Transplantation (HCT) Population Abstract Abstract Introduction Population pharmacokinetic (PK) studies demonstrate model-based dosing for busulfan that incorporate... |
PMC12350181 | core_pubmed_pmc | Mirikizumab Pharmacokinetics and Exposure‐Response in Patients With Moderately‐To‐Severely Active Crohn's Disease: Results From Two Randomized Studies | Mirikizumab Pharmacokinetics and Exposure‐Response in Patients With Moderately‐To‐Severely Active Crohn's Disease: Results From Two Randomized Studies Abstract ABSTRACT Mirikizumab is a humanized anti–interleukin‐23‐p19 monoclonal antibody approved for both moderately‐to‐severely active ulcerative colitis and moderatel... |
PMC7579887 | core_pubmed_pmc | ASP5094, a humanized monoclonal antibody against integrin alpha-9, did not show efficacy in patients with rheumatoid arthritis refractory to methotrexate: results from a phase 2a, randomized, double-blind, placebo-controlled trial | ASP5094, a humanized monoclonal antibody against integrin alpha-9, did not show efficacy in patients with rheumatoid arthritis refractory to methotrexate: results from a phase 2a, randomized, double-blind, placebo-controlled trial Abstract Abstract Background Rheumatoid arthritis (RA) is a chronic, debilitating autoimm... |
PMC11054939 | core_pubmed_pmc | Development and Validation of a Capillary Zone Electrophoresis–Tandem Mass Spectrometry Method for Simultaneous Quantification of Eight β-Lactam Antibiotics and Two β-Lactamase Inhibitors in Plasma Samples | Development and Validation of a Capillary Zone Electrophoresis–Tandem Mass Spectrometry Method for Simultaneous Quantification of Eight β-Lactam Antibiotics and Two β-Lactamase Inhibitors in Plasma Samples Abstract Monitoring plasma concentrations of β-lactam antibiotics is crucial, particularly in critically ill patie... |
PMC3401188 | core_pubmed_pmc | Staphylococcus aureus in Continuous Culture: A Tool for the Rational Design of Antibiotic Treatment Protocols | Staphylococcus aureus in Continuous Culture: A Tool for the Rational Design of Antibiotic Treatment Protocols Abstract Abstract In vitro measures of the pharmacodynamics of antibiotics that account for the factors anticipated for bacteria in infected patients are central to the rational design of antibiotic treatment p... |
PMC11206727 | core_pubmed_pmc | Population Pharmacokinetic Analysis and Simulation of Alternative Dosing Regimens for Biosimilars to Adalimumab and Etanercept in Patients with Rheumatoid Arthritis | Population Pharmacokinetic Analysis and Simulation of Alternative Dosing Regimens for Biosimilars to Adalimumab and Etanercept in Patients with Rheumatoid Arthritis Abstract Efficacy to biologics in rheumatoid arthritis (RA) patients is variable and is likely influenced by each patient’s circulating drug levels. Using ... |
PMC11954733 | core_pubmed_pmc | Influence of Ageing on the Pharmacodynamics and Pharmacokinetics of Chronically Administered Medicines in Geriatric Patients: A Review | Influence of Ageing on the Pharmacodynamics and Pharmacokinetics of Chronically Administered Medicines in Geriatric Patients: A Review Abstract Abstract As people age, the efficiency of various regulatory processes that ensure proper communication between cells and organs tends to decline. This deterioration can lead t... |
PMC5825030 | core_pubmed_pmc | Effect of contrast material injection duration on arterial enhancement at CT in patients with various cardiac indices: Analysis using computer simulation | Effect of contrast material injection duration on arterial enhancement at CT in patients with various cardiac indices: Analysis using computer simulation Abstract Abstract Arterial peak enhancement on contrast-enhanced CT (CECT) images is thought to be higher in patients with low cardiac function. Using computer simula... |
PMC9546310 | core_pubmed_pmc | First‐in‐human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics | First‐in‐human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics Abstract Abstract Aims Neuronal hypersensitisation due to adenosine triphosphate‐dependent P2X3 receptor signalling plays a significant role in several disorders including chronic cou... |
PMC6589987 | core_pubmed_pmc | Pharmacokinetics and tolerability of inhaled levodopa from a new dry-powder inhaler in patients with Parkinson’s disease | Pharmacokinetics and tolerability of inhaled levodopa from a new dry-powder inhaler in patients with Parkinson’s disease Abstract Abstract Background: Inhaled levodopa may quickly resolve off periods in Parkinson’s disease. Our aim was to determine the pharmacokinetics and tolerability of a new levodopa dry-powder inha... |
PMC5768937 | core_pubmed_pmc | Metabolic and hepatic effects of liraglutide, obeticholic acid and elafibranor in diet-induced obese mouse models of biopsy-confirmed nonalcoholic steatohepatitis | Metabolic and hepatic effects of liraglutide, obeticholic acid and elafibranor in diet-induced obese mouse models of biopsy-confirmed nonalcoholic steatohepatitis Abstract AIM To evaluate the pharmacodynamics of compounds in clinical development for nonalcoholic steatohepatitis (NASH) in obese mouse models of biopsy-co... |
PMC9623849 | core_pubmed_pmc | Potent and biostable inhibitors of the main protease of SARS-CoV-2 | Potent and biostable inhibitors of the main protease of SARS-CoV-2 Abstract Summary Potent and biostable inhibitors of the main protease (M pro ) of SARS-CoV-2 were designed and synthesized based on an active hit compound 5h ( 2 ). Our strategy was based not only on the introduction of fluorine atoms into the inhibitor... |
PMC5613109 | core_pubmed_pmc | Therapeutic Potential and Pharmaceutical Development of Thymoquinone: A Multitargeted Molecule of Natural Origin | Therapeutic Potential and Pharmaceutical Development of Thymoquinone: A Multitargeted Molecule of Natural Origin Abstract Thymoquinone, a monoterpene molecule is chemically known as 2-methyl-5-isopropyl-1, 4-benzoquinone. It is abundantly present in seeds of Nigella sativa L. that is popularly known as black cumin or b... |
PMC6528491 | core_pubmed_pmc | A Single Dose of Baicalin Has No Clinically Significant Effect on the Pharmacokinetics of Cyclosporine A in Healthy Chinese Volunteers | A Single Dose of Baicalin Has No Clinically Significant Effect on the Pharmacokinetics of Cyclosporine A in Healthy Chinese Volunteers Abstract Abstract Despite its narrow therapeutic window and large interindividual variability, cyclosporine A (CsA) is the first-line therapy following organ transplantation. Metabolize... |
PMC12951872 | core_pubmed_pmc | Single vs Dual Lactose-Polyethylene Glycol 3000 Microcarrier Systems for Pulmonary Salmeterol and Fluticasone Targeted Delivery | Single vs Dual Lactose-Polyethylene Glycol 3000 Microcarrier Systems for Pulmonary Salmeterol and Fluticasone Targeted Delivery Abstract Background Agglomeration/microparticulation of anti-asthmatic/anti-inflammatory salmeterol (SX) and fluticasone (FP) in a single vehicle rendered inefficient pulmonary drug redispersi... |
PMC8215331 | core_pubmed_pmc | Study design of a randomised, placebo-controlled trial of nintedanib in children and adolescents with fibrosing interstitial lung disease | Study design of a randomised, placebo-controlled trial of nintedanib in children and adolescents with fibrosing interstitial lung disease Abstract Abstract Childhood interstitial lung disease (chILD) comprises >200 rare respiratory disorders, with no currently approved therapies and variable prognosis. Nintedanib reduc... |
PMC9087009 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modelling to Investigate Baricitinib and Tofacitinib Dosing Recommendations for COVID‐19 in Geriatrics | Physiologically‐Based Pharmacokinetic Modelling to Investigate Baricitinib and Tofacitinib Dosing Recommendations for COVID‐19 in Geriatrics Abstract Janus kinase (JAK) inhibitors baricitinib and tofacitinib are recommended by the US National Institutes of Health as immunomodulatory drugs for coronavirus disease 2019 (... |
PMC11024357 | core_pubmed_pmc | Assessment of omeprazole and famotidine effects on the pharmacokinetics of tacrolimus in patients following kidney transplant–randomized controlled trial | Assessment of omeprazole and famotidine effects on the pharmacokinetics of tacrolimus in patients following kidney transplant–randomized controlled trial Abstract Abstract Tacrolimus is metabolized in the liver with the participation of the CYP3A4 and CYP3A5 enzymes. Proton pump inhibitors are used in kidney transplant... |
PMC6590294 | core_pubmed_pmc | Vedolizumab exposure levels and clinical outcomes in ulcerative colitis: determining the potential for dose optimisation | Vedolizumab exposure levels and clinical outcomes in ulcerative colitis: determining the potential for dose optimisation Abstract Summary Background Prospectively designed studies assessing the exposure‐response profile of vedolizumab are lacking. Observational exposure‐response data for vedolizumab are limited and hav... |
PMC12559832 | core_pubmed_pmc | Optimizing Perioperative Management Strategies in Uveitic Cataract Surgery: A Survey of Expert Practices | Optimizing Perioperative Management Strategies in Uveitic Cataract Surgery: A Survey of Expert Practices Abstract Abstract Objectives To evaluate the current practices in uveitic cataract surgery based on expert opinions and identify areas of agreement and divergence. Materials and Methods A descriptive, cross-sectiona... |
PMC4488184 | core_pubmed_pmc | Biocomparison of Three Formulations of the S1P 1 Receptor Modulator Ponesimod in Healthy Subjects | Biocomparison of Three Formulations of the S1P 1 Receptor Modulator Ponesimod in Healthy Subjects Abstract Background Ponesimod is a potent selective sphingosine-1-phosphate receptor 1 (S1P 1 ) modulator, which leads to a reduction in circulating lymphocytes, reflecting their sequestration within lymphoid organs. Modul... |
PMC9279632 | core_pubmed_pmc | In vitro and in vivo characterization of erythrosin B and derivatives against Zika virus | In vitro and in vivo characterization of erythrosin B and derivatives against Zika virus Abstract Zika virus (ZIKV) causes significant human diseases without specific therapy. Previously we found erythrosin B, an FDA-approved food additive, inhibited viral NS2B−NS3 interactions, leading to inhibition of ZIKV infection ... |
PMC9782009 | core_pubmed_pmc | Solvent Free Twin Screw Processed Silybin Nanophytophospholipid: In Silico, In Vitro and In Vivo Insights | Solvent Free Twin Screw Processed Silybin Nanophytophospholipid: In Silico, In Vitro and In Vivo Insights Abstract Silybin (SIL) is a polyphenolic phytoconstituent that is commonly used to treat liver disorders. It is difficult to fabricate an orally delivered SIL product due to its low oral bioavailability (0.95%). Th... |
PMC12196290 | core_pubmed_pmc | Investigation of the ABCB1 Gene Polymorphism and Food Effects on the Avatrombopag Pharmacokinetics in Chinese Individuals: A Population Pharmacokinetic/Pharmacodynamic Analysis | Investigation of the ABCB1 Gene Polymorphism and Food Effects on the Avatrombopag Pharmacokinetics in Chinese Individuals: A Population Pharmacokinetic/Pharmacodynamic Analysis Abstract Abstract Background/Objectives: Avatrombopag (AVA), a thrombopoietin receptor agonist used to treat thrombocytopenia in patients with ... |
PMC10193296 | core_pubmed_pmc | Precision antiplatelet therapy | Precision antiplatelet therapy Abstract A State of the Art lecture titled “Personalizing Antiplatelet Therapy Based on Platelet Turnover and Metabolic Phenotype” was presented by Bianca Rocca at the International Society on Thrombosis and Haemostasis (ISTH) Congress in 2022. Increased variability in drug response may b... |
PMC4777261 | core_pubmed_pmc | Slow drug delivery decreased total body clearance and altered bioavailability of immediate‐ and controlled‐release oxycodone formulations | Slow drug delivery decreased total body clearance and altered bioavailability of immediate‐ and controlled‐release oxycodone formulations Abstract Abstract Oxycodone is a commonly used analgesic with a large body of pharmacokinetic data from various immediate‐release or controlled‐release formulations, under different ... |
PMC5363244 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Analysis of Subcutaneous Tocilizumab in Patients With Rheumatoid Arthritis From 2 Randomized, Controlled Trials: SUMMACTA and BREVACTA | Pharmacokinetic and Pharmacodynamic Analysis of Subcutaneous Tocilizumab in Patients With Rheumatoid Arthritis From 2 Randomized, Controlled Trials: SUMMACTA and BREVACTA Abstract Abstract Tocilizumab is a humanized anti–interleukin‐6 receptor antibody for treating rheumatoid arthritis. Pharmacokinetic/pharmacodynamic ... |
PMC3731829 | core_pubmed_pmc | The impact of mathematical modeling on the understanding of diabetes and related complications | The impact of mathematical modeling on the understanding of diabetes and related complications Abstract Abstract Diabetes is a chronic and complex multifactorial disease caused by persistent hyperglycemia and for which underlying pathogenesis is still not completely understood. The mathematical modeling of glucose home... |
PMC7313537 | core_pubmed_pmc | INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models | INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models Abstract Alterations in fibroblast growth factor receptor (FGFR) genes have been identified as potential driver oncogenes. Pharmacological targeting of... |
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