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PMC7990753 | core_pubmed_pmc | PolyQ-expanded ataxin-3 protein levels in peripheral blood mononuclear cells correlate with clinical parameters in SCA3: a pilot study | PolyQ-expanded ataxin-3 protein levels in peripheral blood mononuclear cells correlate with clinical parameters in SCA3: a pilot study Abstract Abstract In view of upcoming clinical trials, quantitative molecular markers accessible in peripheral blood are of critical importance as prognostic or pharmacodynamic markers ... |
PMC8383732 | core_pubmed_pmc | Genetics, Epigenetics, and Gender Impact in Axial-Spondyloarthritis Susceptibility: An Update on Genetic Polymorphisms and Their Sex Related Associations | Genetics, Epigenetics, and Gender Impact in Axial-Spondyloarthritis Susceptibility: An Update on Genetic Polymorphisms and Their Sex Related Associations Abstract Abstract Spondyloarthritis (SpA) is a group of chronic inflammatory rheumatic disease that can be divided into predominantly axial or predominantly periphera... |
PMC9784495 | core_pubmed_pmc | Pharmacokinetic Comparison of Ginsenosides between Fermented and Non-Fermented Red Ginseng in Healthy Volunteers | Pharmacokinetic Comparison of Ginsenosides between Fermented and Non-Fermented Red Ginseng in Healthy Volunteers Abstract Fermentation of red ginseng (RG) produces fermented red ginseng (FRG), thereby increasing the relative amount of downstream ginsenosides, including compound Y (CY), F2, Rh2, compound K (CK), compoun... |
PMC12932228 | core_pubmed_pmc | Honey and cancer: from traditional medicine to modern adjuvant therapy | Honey and cancer: from traditional medicine to modern adjuvant therapy Abstract Abstract Cancer remains one of the principal causes of death worldwide, with conventional treatments like chemotherapy and radiotherapy often exhibiting high toxicity, resistance, and relapse rates. These constraints have sparked new invest... |
PMC3654174 | core_pubmed_pmc | Sifalimumab, a Human Anti–Interferon-α Monoclonal Antibody, in Systemic Lupus Erythematosus: A Phase I Randomized, Controlled, Dose-Escalation Study | Sifalimumab, a Human Anti–Interferon-α Monoclonal Antibody, in Systemic Lupus Erythematosus: A Phase I Randomized, Controlled, Dose-Escalation Study Abstract Abstract Objective To evaluate the safety and tolerability of multiple intravenous (IV) doses of sifalimumab in adults with moderate-to-severe systemic lupus eryt... |
PMC11510446 | core_pubmed_pmc | Establishing a Relationship between In Vitro Potency in Cell-Based Assays and Clinical Efficacious Concentrations for Approved GLP-1 Receptor Agonists | Establishing a Relationship between In Vitro Potency in Cell-Based Assays and Clinical Efficacious Concentrations for Approved GLP-1 Receptor Agonists Abstract Abstract Background: Glucagon-like peptide-1 receptor agonists (GLP-1RAs) play an important role in the treatment of type 2 diabetes (T2D) and obesity. The rela... |
PMC8001195 | core_pubmed_pmc | Pharmacogenetics of Carbamazepine and Valproate: Focus on Polymorphisms of Drug Metabolizing Enzymes and Transporters | Pharmacogenetics of Carbamazepine and Valproate: Focus on Polymorphisms of Drug Metabolizing Enzymes and Transporters Abstract Abstract Pharmacogenomics can identify polymorphisms in genes involved in drug pharmacokinetics and pharmacodynamics determining differences in efficacy and safety and causing inter-individual ... |
PMC7015744 | core_pubmed_pmc | Comparison of pharmacokinetics, safety and tolerability of secukinumab administered subcutaneously using different delivery systems in healthy volunteers and in psoriasis patients | Comparison of pharmacokinetics, safety and tolerability of secukinumab administered subcutaneously using different delivery systems in healthy volunteers and in psoriasis patients Abstract Aims The aim of the study was to compare the pharmacokinetics (PK), safety and tolerability of secukinumab with different devices f... |
PMC10873430 | core_pubmed_pmc | Drug-drug interaction perpetrators of oxycodone in patients with cancer: frequency and clinical relevance | Drug-drug interaction perpetrators of oxycodone in patients with cancer: frequency and clinical relevance Abstract Aim Oxycodone is known to have numerous drug-drug interactions (DDIs) that can potentially decrease efficacy or lead to adverse drug reactions (ADRs). However, there is limited research on the frequency of... |
PMC3317240 | core_pubmed_pmc | Application of Physiologically Based Pharmacokinetic Models in Chemical Risk Assessment | Application of Physiologically Based Pharmacokinetic Models in Chemical Risk Assessment Abstract Post-exposure risk assessment of chemical and environmental stressors is a public health challenge. Linking exposure to health outcomes is a 4-step process: exposure assessment, hazard identification, dose response assessme... |
PMC11597346 | core_pubmed_pmc | Evaluation of Drug–Drug Interactions Between Clarithromycin and Direct Oral Anticoagulants Using Physiologically Based Pharmacokinetic Models | Evaluation of Drug–Drug Interactions Between Clarithromycin and Direct Oral Anticoagulants Using Physiologically Based Pharmacokinetic Models Abstract Abstract Objective: This study assessed the pharmacokinetic (PK) interactions between clarithromycin (a P-glycoprotein [P-gp] inhibitor) and four direct oral anticoagula... |
PMC7248953 | core_pubmed_pmc | Assessment of Pharmacokinetics and Metabolism Profiles of SCH 58261 in Rats Using Liquid Chromatography–Mass Spectrometric Method | Assessment of Pharmacokinetics and Metabolism Profiles of SCH 58261 in Rats Using Liquid Chromatography–Mass Spectrometric Method Abstract 5-Amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c) pyrimidine (SCH 58261) is one of the new chemical entities that has been developed as an adenosine A 2A r... |
PMC7917713 | core_pubmed_pmc | Estimation of the In Vivo Release of Amiodarone From the Pharmacokinetics of Its Active Metabolite and Correlation With Its In Vitro Release | Estimation of the In Vivo Release of Amiodarone From the Pharmacokinetics of Its Active Metabolite and Correlation With Its In Vitro Release Abstract Due to its very low water solubility and complex pharmacokinetics, a reliable point-to-point correlation of its in vitro release with its pharmacokinetics has not been ac... |
PMC8634237 | core_pubmed_pmc | Assessing the safety, tolerability and efficacy of PLGA-based immunomodulatory nanoparticles in patients with advanced NY-ESO-1-positive cancers: a first-in-human phase I open-label dose-escalation study protocol | Assessing the safety, tolerability and efficacy of PLGA-based immunomodulatory nanoparticles in patients with advanced NY-ESO-1-positive cancers: a first-in-human phase I open-label dose-escalation study protocol Abstract Abstract Introduction The undiminished need for more effective cancer treatments stimulates the de... |
PMC12483284 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Oxcarbazepine to Characterize Its Disposition in Children with Obesity | Physiologically Based Pharmacokinetic Modeling of Oxcarbazepine to Characterize Its Disposition in Children with Obesity Abstract Abstract Oxcarbazepine (OXC) is a second‐generation antiseizure medication, effective through its active metabolite, 10‐mono‐hydroxy derivative (MHD). OXC is used as adjunctive therapy for f... |
PMC12728616 | core_pubmed_pmc | Regioselective Glycosylation of Fluorine-18-Labeled Sorbitol for Enhanced Bacterial Detection In Vivo Using PET | Regioselective Glycosylation of Fluorine-18-Labeled Sorbitol for Enhanced Bacterial Detection In Vivo Using PET Abstract Precise and rapid detection of bacterial infection in vivo remains a significant challenge in clinical practice. In response to this challenge, several pathogen-specific positron emission tomography ... |
PMC4324687 | core_pubmed_pmc | A single-dose mass balance and metabolite-profiling study of vemurafenib in patients with metastatic melanoma | A single-dose mass balance and metabolite-profiling study of vemurafenib in patients with metastatic melanoma Abstract Vemurafenib, a selective inhibitor of oncogenic BRAF kinase carrying the V600 mutation, is approved for treatment of advanced BRAF mutation–positive melanoma. This study characterized mass balance, met... |
PMC8167741 | core_pubmed_pmc | Pharmacokinetics of oral pridinol: Results of a randomized, crossover bioequivalence trial in healthy subjects | Pharmacokinetics of oral pridinol: Results of a randomized, crossover bioequivalence trial in healthy subjects Abstract Abstract Objectives: To establish the relative bioavailability and to assess bioequivalence of oral, immediate-release tablets containing pridinol and to determine the pharmacokinetic properties of th... |
PMC6707041 | core_pubmed_pmc | Ultra-High-Precision, in-vivo Pharmacokinetic Measurements Highlight the Need for and a Route Toward More Highly Personalized Medicine | Ultra-High-Precision, in-vivo Pharmacokinetic Measurements Highlight the Need for and a Route Toward More Highly Personalized Medicine Abstract Abstract Clinical drug dosing would, ideally, be informed by high-precision, patient-specific data on drug metabolism. The direct determination of patient-specific drug pharmac... |
PMC11015457 | core_pubmed_pmc | Revealing the active ingredients and mechanism of P. sibiricumm in non-small-cell lung cancer based on UPLC-Q-TOF-MS/MS, network pharmacology, and molecular docking | Revealing the active ingredients and mechanism of P. sibiricumm in non-small-cell lung cancer based on UPLC-Q-TOF-MS/MS, network pharmacology, and molecular docking Abstract Abstract The alcohol extraction of P. sibiricum has exhibited significant inhibitory effects on the production of free radicals and the proliferat... |
PMC3232103 | core_pubmed_pmc | Population pharmacokinetics of oral high-dose busulfan in adult patients undergoing hematopoietic stem cell transplantation | Population pharmacokinetics of oral high-dose busulfan in adult patients undergoing hematopoietic stem cell transplantation Abstract Abstract Background and the purpose of the study Many factors have been reported that contribute to the wide intra- and inter-patient variability of Busulfan (Bu) disposition. The purpose... |
PMC10716275 | core_pubmed_pmc | Evaluation of pharmacological and pharmacokinetic herb-drug interaction between irinotecan hydrochloride injection and Kangai injection in colorectal tumor-bearing mice and healthy rats | Evaluation of pharmacological and pharmacokinetic herb-drug interaction between irinotecan hydrochloride injection and Kangai injection in colorectal tumor-bearing mice and healthy rats Abstract Abstract Introduction: Kangai (KA) injection, a Chinese herbal injection, is often used in combination with irinotecan (CPT-1... |
PMC3356221 | core_pubmed_pmc | Preclinical evaluation of injectable sirolimus formulated with polymeric nanoparticle for cancer therapy | Preclinical evaluation of injectable sirolimus formulated with polymeric nanoparticle for cancer therapy Abstract Abstract Nanoparticles are useful delivery vehicles for promising drug candidates that face obstacles for clinical applicability. Sirolimus, an inhibitor of mammalian target of rapamycin has gained attentio... |
PMC7818112 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Dalteparin in Pediatric Patients With Venous Thromboembolism | Population Pharmacokinetic Analysis of Dalteparin in Pediatric Patients With Venous Thromboembolism Abstract Abstract This article describes the population pharmacokinetics (PK) of dalteparin in pediatric patients with venous thromboembolism (VTE). A prospective multicenter open‐label study was conducted in children wh... |
PMC7577146 | core_pubmed_pmc | Population Pharmacokinetics of Caspofungin among Extracorporeal Membrane Oxygenation Patients during the Postoperative Period of Lung Transplantation | Population Pharmacokinetics of Caspofungin among Extracorporeal Membrane Oxygenation Patients during the Postoperative Period of Lung Transplantation Abstract Little is known about the influence of extracorporeal membrane oxygenation (ECMO) on the pharmacokinetics (PK) of caspofungin. The aim of this study was to descr... |
PMC9318546 | core_pubmed_pmc | Novel Therapies to Address Unmet Needs in ITP | Novel Therapies to Address Unmet Needs in ITP Abstract Abstract Primary immune thrombocytopenia (ITP) is an autoimmune disorder that causes low platelet counts and subsequent bleeding risk. Although current corticosteroid-based ITP therapies are able to improve platelet counts, up to 70% of subjects with an ITP diagnos... |
PMC10575992 | core_pubmed_pmc | A Phase 1 Study of Ensitrelvir Fumaric Acid Tablets Evaluating the Safety, Pharmacokinetics and Food Effect in Healthy Adult Populations | A Phase 1 Study of Ensitrelvir Fumaric Acid Tablets Evaluating the Safety, Pharmacokinetics and Food Effect in Healthy Adult Populations Abstract Abstract Background A reported clinical pharmacokinetics and safety study of suspension formulation of ensitrelvir, a therapeutic agent used in severe acute respiratory syndr... |
PMC7187570 | core_pubmed_pmc | Intracellular Pharmacodynamic Modeling Is Predictive of the Clinical Activity of Fluoroquinolones against Tuberculosis | Intracellular Pharmacodynamic Modeling Is Predictive of the Clinical Activity of Fluoroquinolones against Tuberculosis Abstract Clinical studies of new antitubercular drugs are costly and time-consuming. Owing to the extensive tuberculosis (TB) treatment periods, the ability to identify drug candidates based on their p... |
PMC8177785 | core_pubmed_pmc | Abemaciclib in combination with endocrine therapy for East Asian patients with HR+, HER2− advanced breast cancer: MONARCH 2 & 3 trials | Abemaciclib in combination with endocrine therapy for East Asian patients with HR+, HER2− advanced breast cancer: MONARCH 2 & 3 trials Abstract Abstract This post hoc analysis of MONARCH 2 and MONARCH 3 assesses the efficacy, safety, and pharmacokinetics (PK) of abemaciclib in combination with endocrine therapy (ET) in... |
PMC3425973 | core_pubmed_pmc | Personalising docetaxel and G-CSF schedules in cancer patients by a clinically validated computational model | Personalising docetaxel and G-CSF schedules in cancer patients by a clinically validated computational model Abstract Background: This study was aimed to develop a new method for personalising chemotherapeutic and granulocyte colony-stimulating factor (G-CSF) combined schedules, and use it for suggesting efficacious ch... |
PMC9224772 | core_pubmed_pmc | Sex-Based Difference in the Effect of Metoprolol on Heart Rate and Bradycardia in a Population-Based Setting | Sex-Based Difference in the Effect of Metoprolol on Heart Rate and Bradycardia in a Population-Based Setting Abstract Abstract Background: Metoprolol, a beta-blocker, is used to reduce the heart rate. Although it has been demonstrated that the metoprolol plasma concentration is higher in women than in men, the same dos... |
PMC4689335 | core_pubmed_pmc | Evaluation of HDL-modulating interventions for cardiovascular risk reduction using a systems pharmacology approach [S] | Evaluation of HDL-modulating interventions for cardiovascular risk reduction using a systems pharmacology approach [S] Abstract Abstract The recent failures of cholesteryl ester transport protein inhibitor drugs to decrease CVD risk, despite raising HDL cholesterol (HDL-C) levels, suggest that pharmacologic increases i... |
PMC4336683 | core_pubmed_pmc | The protocol of the Oslo Study of Clonidine in Elderly Patients with Delirium; LUCID: a randomised placebo-controlled trial | The protocol of the Oslo Study of Clonidine in Elderly Patients with Delirium; LUCID: a randomised placebo-controlled trial Abstract Background Delirium affects 15% of hospitalised patients and is linked with poor outcomes, yet few pharmacological treatment options exist. One hypothesis is that delirium may in part res... |
PMC12713449 | core_pubmed_pmc | Structure-Based Discovery of Potent and Selective Small-Molecule α5β1 Integrin Inhibitors for Asthma Therapy | Structure-Based Discovery of Potent and Selective Small-Molecule α5β1 Integrin Inhibitors for Asthma Therapy Abstract Abstract Integrin α5β1 is the principal fibronectin-binding integrin in airway smooth muscle (ASM), and its modulation attenuates airway narrowing induced by asthmagenic cytokines in mouse models of all... |
PMC4086932 | core_pubmed_pmc | Analysis of Combination Drug Therapy to Develop Regimens with Shortened Duration of Treatment for Tuberculosis | Analysis of Combination Drug Therapy to Develop Regimens with Shortened Duration of Treatment for Tuberculosis Abstract Abstract Rationale Tuberculosis remains a worldwide problem, particularly with the advent of multi-drug resistance. Shortening therapy duration for Mycobacterium tuberculosis is a major goal, requirin... |
PMC3928318 | core_pubmed_pmc | A randomized, double-blind, placebo-controlled, multiple-dose, parallel-group clinical trial to assess the effects of teduglutide on gastric emptying of liquids in healthy subjects | A randomized, double-blind, placebo-controlled, multiple-dose, parallel-group clinical trial to assess the effects of teduglutide on gastric emptying of liquids in healthy subjects Abstract Abstract Background Teduglutide, a recombinant analog of human glucagon-like peptide (GLP)-2, is a novel therapy recently approved... |
PMC11676667 | core_pubmed_pmc | Pharmacokinetics of Oral Cannabinoid Δ8-Tetrahydrocannabivarin and Its Main Metabolites in Healthy Participants | Pharmacokinetics of Oral Cannabinoid Δ8-Tetrahydrocannabivarin and Its Main Metabolites in Healthy Participants Abstract Background: Tetrahydrocannabivarin (THCV) is a phytocannabinoid commonly found in cannabis with potential pharmacological properties; however, its post-acute pharmacokinetics (PK) in humans have not ... |
PMC7336703 | core_pubmed_pmc | COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms | COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms Abstract Abstract SARS-CoV-2 infection is required for COVID-19, but many signs and symptoms of COVID-19 differ from common acute viral diseases. Currently, there are no pre- or post-exposure prophylactic COVID-19 medical countermeasures. Clinical data suggest... |
PMC6272035 | core_pubmed_pmc | In vivo and in vitro assessment of mirtazapine pharmacokinetics in cats with liver disease | In vivo and in vitro assessment of mirtazapine pharmacokinetics in cats with liver disease Abstract Background Liver disease (LD) prolongs mirtazapine half‐life in humans, but it is unknown if this occurs in cats with LD and healthy cats. Hypothesis/Objectives To determine pharmacokinetics of administered orally mirtaz... |
PMC6278009 | core_pubmed_pmc | Reviewing the role of healthy volunteer studies in drug development | Reviewing the role of healthy volunteer studies in drug development Abstract Background With the exception of genotoxic oncology drugs, first-in-human, Phase 1 clinical studies of investigational drugs have traditionally been conducted in healthy volunteers (HVs). The primary goal of these studies is to investigate the... |
PMC5131889 | core_pubmed_pmc | Cardiovascular Safety Assessment in Early‐Phase Clinical Studies: A Meta‐Analytical Comparison of Exposure‐Response Models | Cardiovascular Safety Assessment in Early‐Phase Clinical Studies: A Meta‐Analytical Comparison of Exposure‐Response Models Abstract Abstract Exposure‐response analysis of QT interval in clinical studies has been proposed as a thorough QT study alternative. Many exposure‐response model structures have been proposed for ... |
PMC9619254 | core_pubmed_pmc | Estimation of Kidney Function in Patients With Multiple Myeloma: Implications for Lenalidomide Dosing | Estimation of Kidney Function in Patients With Multiple Myeloma: Implications for Lenalidomide Dosing Abstract Abstract Background Lenalidomide is an immunomodulatory drug used to treat multiple myeloma that requires renal dosing adjustment based on Cockcroft-Gault (CG). Various equations to estimate kidney function ex... |
PMC8469644 | core_pubmed_pmc | Drug Release Profiles of Mitomycin C Encapsulated Quantum Dots–Chitosan Nanocarrier System for the Possible Treatment of Non-Muscle Invasive Bladder Cancer | Drug Release Profiles of Mitomycin C Encapsulated Quantum Dots–Chitosan Nanocarrier System for the Possible Treatment of Non-Muscle Invasive Bladder Cancer Abstract Nanotechnology-based drug delivery systems are an emerging technology for the targeted delivery of chemotherapeutic agents in cancer therapy with low/no to... |
PMC12455318 | core_pubmed_pmc | The Kinetics of Bedaquiline Diffusion in Tuberculous Cavities Open a Window for the Emergence of Resistance | The Kinetics of Bedaquiline Diffusion in Tuberculous Cavities Open a Window for the Emergence of Resistance Abstract Abstract Background Cavitary tuberculosis is difficult to cure and constitutes a site of relapse. Bedaquiline has been a wonder drug in the treatment of multidrug-resistant tuberculosis, but emergence of... |
PMC10425307 | core_pubmed_pmc | Evaluation of the pharmacokinetics, dosimetry, and therapeutic efficacy for the α-particle-emitting transarterial radioembolization (αTARE) agent [ 225 Ac]Ac-DOTA-TDA-Lipiodol ® against hepatic tumors | Evaluation of the pharmacokinetics, dosimetry, and therapeutic efficacy for the α-particle-emitting transarterial radioembolization (αTARE) agent [ 225 Ac]Ac-DOTA-TDA-Lipiodol ® against hepatic tumors Abstract Background The liver is a common site for metastatic disease for a variety of cancers, including colorectal ca... |
PMC11802679 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of a Novel Anti-obesity Agent, S-309309, in Healthy Adults with or Without Obesity | Safety, Tolerability, and Pharmacokinetics of a Novel Anti-obesity Agent, S-309309, in Healthy Adults with or Without Obesity Abstract Abstract Background Anti-obesity medications are recommended for patients who do not achieve and maintain weight loss despite lifestyle interventions. S-309309 is a novel oral inhibitor... |
PMC7803744 | core_pubmed_pmc | CYP3A4 mediated pharmacokinetics drug interaction potential of Maha-Yogaraj Gugglu and E, Z guggulsterone | CYP3A4 mediated pharmacokinetics drug interaction potential of Maha-Yogaraj Gugglu and E, Z guggulsterone Abstract Maha yogaraja guggulu (MYG) is a classical herbomineral polyherbal formulation being widely used since centuries. The aim of this study was to investigate the effect of MYG formulation and its major consti... |
PMC6069276 | core_pubmed_pmc | A Physiologically-Based Pharmacokinetic Modeling Approach Using Biomonitoring Data in Order to Assess the Contribution of Drinking Water for the Achievement of an Optimal Fluoride Dose for Dental Health in Children | A Physiologically-Based Pharmacokinetic Modeling Approach Using Biomonitoring Data in Order to Assess the Contribution of Drinking Water for the Achievement of an Optimal Fluoride Dose for Dental Health in Children Abstract Abstract Due to an optimal fluoride concentration in drinking water advised for caries preventio... |
PMC10906076 | core_pubmed_pmc | A Design-Conversed Strategy Establishes the Performance Safe Space for Doxorubicin Nanosimilars | A Design-Conversed Strategy Establishes the Performance Safe Space for Doxorubicin Nanosimilars Abstract Abstract Nanomedicines exhibit multifaceted performances, yet their biopharmaceutics remain poorly understood and present several challenges in the translation from preclinical to clinical research. To address this ... |
PMC8538929 | core_pubmed_pmc | Micafungin Is an Efficient Treatment of Multi Drug-Resistant Candida glabrata Urosepsis: A Case Report | Micafungin Is an Efficient Treatment of Multi Drug-Resistant Candida glabrata Urosepsis: A Case Report Abstract Abstract Candiduria is a common nosocomial infection in hospitalized patients, which may progress into life-threatening candidemia. Successful treatment of urosepsis requires early and effective antifungal th... |
PMC3535401 | core_pubmed_pmc | Phase 1 study of trebananib (AMG 386), an angiogenesis targeting angiopoietin-1/2 antagonist, in Japanese patients with advanced solid tumors | Phase 1 study of trebananib (AMG 386), an angiogenesis targeting angiopoietin-1/2 antagonist, in Japanese patients with advanced solid tumors Abstract Purpose To evaluate the safety, tolerability, pharmacokinetics, and antitumor activity of trebananib (AMG 386)—a first-in-class angiopoietin-1/2 antagonist peptide-Fc fu... |
PMC11124525 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Correlation Analysis of Rhodiola crenulata in Rats with Myocardial Ischemia | Pharmacokinetic–Pharmacodynamic Correlation Analysis of Rhodiola crenulata in Rats with Myocardial Ischemia Abstract Abstract The pharmacokinetics (PK) of Rhodiola crenulata in rats were studied, and pharmacokinetic–pharmacodynamic (PK-PD) correlation analysis was performed to elucidate their time–concentration–effect ... |
PMC9643609 | core_pubmed_pmc | Targeting SAMHD1 with hydroxyurea in first‐line cytarabine‐based therapy of newly diagnosed acute myeloid leukaemia: Results from the HEAT‐AML trial | Targeting SAMHD1 with hydroxyurea in first‐line cytarabine‐based therapy of newly diagnosed acute myeloid leukaemia: Results from the HEAT‐AML trial Abstract Abstract Background Treatment of newly diagnosed acute myeloid leukaemia (AML) is based on combination chemotherapy with cytarabine (ara‐C) and anthracyclines. Fi... |
PMC10674226 | core_pubmed_pmc | Challenges Related to Acquisition of Physiological Data for Physiologically Based Pharmacokinetic (PBPK) Models in Postpartum, Lactating Women and Breastfed Infants—A Contribution from the ConcePTION Project | Challenges Related to Acquisition of Physiological Data for Physiologically Based Pharmacokinetic (PBPK) Models in Postpartum, Lactating Women and Breastfed Infants—A Contribution from the ConcePTION Project Abstract Physiologically based pharmacokinetic (PBPK) modelling is a bottom-up approach to predict pharmacokinet... |
PMC11597839 | core_pubmed_pmc | Aniline Derivatives Containing 1-Substituted 1,2,3-Triazole System as Potential Drug Candidates: Pharmacokinetic Profile Prediction, Lipophilicity Analysis Using Experimental and In Silico Studies | Aniline Derivatives Containing 1-Substituted 1,2,3-Triazole System as Potential Drug Candidates: Pharmacokinetic Profile Prediction, Lipophilicity Analysis Using Experimental and In Silico Studies Abstract Abstract Background : The triazole ring is an attractive structural unit in medicinal chemistry, and chemical comp... |
PMC6039205 | core_pubmed_pmc | Pharmacokinetics of RP5063 Following Single Doses to Normal Healthy Volunteers and Multiple Doses Over 10 Days to Stable Schizophrenic Patients | Pharmacokinetics of RP5063 Following Single Doses to Normal Healthy Volunteers and Multiple Doses Over 10 Days to Stable Schizophrenic Patients Abstract Abstract RP5063, a multimodal dopamine (D)–serotonin (5‐HT) stabilizer, possesses high affinity for D 2/3/4 and 5‐HT 1A/2A/2B/2C/6/7 receptors and moderate affinity fo... |
PMC5724491 | core_pubmed_pmc | Efficacy and tolerability of the new autoinjected suspension of exenatide once weekly versus exenatide twice daily in patients with type 2 diabetes | Efficacy and tolerability of the new autoinjected suspension of exenatide once weekly versus exenatide twice daily in patients with type 2 diabetes Abstract Aims To simplify administration of aqueous exenatide once weekly, which requires reconstitution, the exenatide microspheres have been reformulated in a ready‐to‐us... |
PMC7281216 | core_pubmed_pmc | The Therapeutic Effectiveness of Full Spectrum Hemp Oil Using a Chronic Neuropathic Pain Model | The Therapeutic Effectiveness of Full Spectrum Hemp Oil Using a Chronic Neuropathic Pain Model Abstract Background: Few models exist that can control for placebo and expectancy effects commonly observed in clinical trials measuring ‘ Cannabis ’ pharmacodynamics. We used the Foramen Rotundum Inflammatory Constriction Tr... |
PMC3005107 | core_pubmed_pmc | Understanding pharmacokinetics using realistic computational models of fluid dynamics: biosimulation of drug distribution within the CSF space for intrathecal drugs | Understanding pharmacokinetics using realistic computational models of fluid dynamics: biosimulation of drug distribution within the CSF space for intrathecal drugs Abstract We introduce how biophysical modeling in pharmaceutical research and development, combining physiological observations at the tissue, organ and sy... |
PMC11956005 | core_pubmed_pmc | 2FA-Platform Generates Dual Fatty Acid-Conjugated GLP-1 Receptor Agonist TE-8105 with Enhanced Diabetes, Obesity, and NASH Efficacy Compared to Semaglutide | 2FA-Platform Generates Dual Fatty Acid-Conjugated GLP-1 Receptor Agonist TE-8105 with Enhanced Diabetes, Obesity, and NASH Efficacy Compared to Semaglutide Abstract Conjugating two fatty acids (2FAs) to peptide drugs can improve pharmacokinetics and therapeutic effects. However, optimizing FA spacing, chain combination... |
PMC7871676 | core_pubmed_pmc | Safety and related factors of treatment with long-term atypical antipsychotic in Chinese patients with schizophrenia: observational study | Safety and related factors of treatment with long-term atypical antipsychotic in Chinese patients with schizophrenia: observational study Abstract Abstract Background Atypical antipsychotics as first-line drugs have been used in patients with schizophrenia in China and abroad. However, its safety still needs to be eval... |
PMC6885504 | core_pubmed_pmc | The Effects of Clarithromycin on the Pharmacokinetics of Apixaban in Healthy Volunteers: A Single-Sequence Crossover Study | The Effects of Clarithromycin on the Pharmacokinetics of Apixaban in Healthy Volunteers: A Single-Sequence Crossover Study Abstract Abstract Background This was an open-label, phase I, nonrandomized, single-sequence, crossover study to evaluate the effect of concomitant administration of multiple doses of clarithromyci... |
PMC5360744 | core_pubmed_pmc | Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate | Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate Abstract Background To determine the concentration after a single dose of generic 0.05% difluprednate and commercial difluprednate in th... |
PMC10449972 | core_pubmed_pmc | Population Target-Mediated Pharmacokinetic/Pharmacodynamic Modeling to Evaluate SPI-62 Exposure and Hepatic 11β-Hydroxysteroid Dehydrogenase Type 1 (HSD-1) Inhibition in Healthy Adults | Population Target-Mediated Pharmacokinetic/Pharmacodynamic Modeling to Evaluate SPI-62 Exposure and Hepatic 11β-Hydroxysteroid Dehydrogenase Type 1 (HSD-1) Inhibition in Healthy Adults Abstract Abstract Introduction SPI-62 is a small-molecule 11β-hydroxysteroid dehydrogenase type 1 (HSD-1) inhibitor exhibiting complica... |
PMC8839776 | core_pubmed_pmc | Safety Profile of Rapamycin Perfluorocarbon Nanoparticles for Preventing Cisplatin-Induced Kidney Injury | Safety Profile of Rapamycin Perfluorocarbon Nanoparticles for Preventing Cisplatin-Induced Kidney Injury Abstract Cancer treatment-induced toxicities may restrict maximal effective dosing for treatment and cancer survivors’ quality of life. It is critical to develop novel strategies that mitigate treatment-induced toxi... |
PMC6651109 | core_pubmed_pmc | Preparation and In Vitro/In Vivo Characterization of Polymeric Nanoparticles Containing Methotrexate to Improve Lymphatic Delivery | Preparation and In Vitro/In Vivo Characterization of Polymeric Nanoparticles Containing Methotrexate to Improve Lymphatic Delivery Abstract Abstract Methotrexate (MTX) is a folic acid antagonist used as an effective drug to treat various kinds of cancers. However, MTX has limited use in cancer chemotherapy due to its a... |
PMC6989269 | core_pubmed_pmc | Digital therapeutics and clinical pharmacology | Digital therapeutics and clinical pharmacology Abstract Abstract Digital therapeutics (DTx) is a new subsection of digital health that is primarily driven by software and will be of great interest to clinical pharmacologists. In this article, an overview of DTx, including definition, position in the landscape of therap... |
PMC5545752 | core_pubmed_pmc | Defining the optimal dose of rifapentine for pulmonary tuberculosis: Exposure–response relations from two phase II clinical trials | Defining the optimal dose of rifapentine for pulmonary tuberculosis: Exposure–response relations from two phase II clinical trials Abstract Abstract Rifapentine is a highly active antituberculosis antibiotic with treatment‐shortening potential; however, exposure–response relations and the dose needed for maximal bacter... |
PMC4288002 | core_pubmed_pmc | Prediction of Metabolic Interactions With Oxycodone via CYP2D6 and CYP3A Inhibition Using a Physiologically Based Pharmacokinetic Model | Prediction of Metabolic Interactions With Oxycodone via CYP2D6 and CYP3A Inhibition Using a Physiologically Based Pharmacokinetic Model Abstract Evaluation of a potential risk of metabolic drug–drug interactions (DDI) is of high importance in the clinical setting. In this study, a physiologically based pharmacokinetic ... |
PMC6103319 | core_pubmed_pmc | Evaluation of the antibacterial activity of tilmicosin-SLN against Streptococcus agalactiae : in vitro and in vivo studies | Evaluation of the antibacterial activity of tilmicosin-SLN against Streptococcus agalactiae : in vitro and in vivo studies Abstract Abstract Background Streptococcus and Staphylococcus are the major contagious organisms causing dairy cow mastitis. Our previous studies have demonstrated that solid lipid nanoparticles (S... |
PMC7143661 | core_pubmed_pmc | Disambiguating “Mechanisms” in Pharmacy: Lessons from Mechanist Philosophy of Science | Disambiguating “Mechanisms” in Pharmacy: Lessons from Mechanist Philosophy of Science Abstract Talk of mechanisms is ubiquitous in the natural sciences. Interdisciplinary fields such as biochemistry and pharmacy frequently discuss mechanisms with the assistance of diagrams. Such diagrams usually depict entities as stru... |
PMC7391639 | core_pubmed_pmc | Plasma concentrations of eleven cannabinoids in cattle following oral administration of industrial hemp ( Cannabis sativa ) | Plasma concentrations of eleven cannabinoids in cattle following oral administration of industrial hemp ( Cannabis sativa ) Abstract Abstract Cannabinoid production for medicinal purposes has renewed interest in utilizing byproducts of industrial hemp (IH) as a feed source for livestock. However, the presence of bioact... |
PMC10974824 | core_pubmed_pmc | Validated LC-MS/MS Assay for the Quantitative Determination of Fenretinide in Plasma and Tumor and Its Application in a Pharmacokinetic Study in Mice of a Novel Oral Nanoformulation of Fenretinide | Validated LC-MS/MS Assay for the Quantitative Determination of Fenretinide in Plasma and Tumor and Its Application in a Pharmacokinetic Study in Mice of a Novel Oral Nanoformulation of Fenretinide Abstract We describe the development and validation of a HPLC-MS/MS method to assess the pharmacokinetics and tumor distrib... |
PMC7779995 | core_pubmed_pmc | Fosfomycin Dosing Regimens based on Monte Carlo Simulation for Treated Carbapenem-Resistant Enterobacteriaceae Infection | Fosfomycin Dosing Regimens based on Monte Carlo Simulation for Treated Carbapenem-Resistant Enterobacteriaceae Infection Abstract Abstract Background Infections by Carbapenem-Resistant Enterobacteriaceae (CRE) remain a leading cause of death in critically ill patients. Fosfomycin has been regarded as an alternative the... |
PMC10820281 | core_pubmed_pmc | Personalized Prophylaxis with myPKFiT CE : A Real-World Cost-Effectiveness Analysis in Haemophilia A Patients | Personalized Prophylaxis with myPKFiT CE : A Real-World Cost-Effectiveness Analysis in Haemophilia A Patients Abstract Background and Objectives: This study aimed to assess the effectiveness and costs associated with pharmacokinetics-driven (PK) prophylaxis based on the myPKFiT ® device in patients affected by hemophil... |
PMC12747374 | core_pubmed_pmc | Integrating bioactivity and molecular simulations to explore the pharmacological landscape of Lagerstroemia speciosa leaf extract | Integrating bioactivity and molecular simulations to explore the pharmacological landscape of Lagerstroemia speciosa leaf extract Abstract Abstract Natural resources are vital for identifying novel treatments for noncommunicable diseases and multidrug-resistant pathogens. Lagerstroemia speciosa (L. speciosa) Linn. is t... |
PMC4019625 | core_pubmed_pmc | Folate receptor-targeted liposomes enhanced the antitumor potency of imatinib through the combination of active targeting and molecular targeting | Folate receptor-targeted liposomes enhanced the antitumor potency of imatinib through the combination of active targeting and molecular targeting Abstract Purpose Imatinib inhibits platelet-derived growth factor receptor (PDGFR), and evidence shows that PDGFR participates in the development and progression of cervical ... |
PMC10622832 | core_pubmed_pmc | Hyperbaric oxygen therapy counteracts Pseudomonas aeruginosa biofilm micro-compartment phenomenon in murine thermal wounds | Hyperbaric oxygen therapy counteracts Pseudomonas aeruginosa biofilm micro-compartment phenomenon in murine thermal wounds Abstract Abstract Background Biofilm antibiotic tolerance is partly explained by the behavior of a biofilm as an independent pharmacokinetic micro-compartment. Hyperbaric oxygen therapy has been sh... |
PMC10397395 | core_pubmed_pmc | A sustained-release phospholipid-based phase separation gel loaded with berberine for treating rheumatoid arthritis | A sustained-release phospholipid-based phase separation gel loaded with berberine for treating rheumatoid arthritis Abstract Berberine (BBR) has a long history of use in the treatment of Rheumatoid arthritis (RA) and is considered one of the most promising natural product for the treatment of RA. However, oral administ... |
PMC5394143 | core_pubmed_pmc | Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults | Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults Abstract Abstract Background and Objectives Osilodrostat (LCI699) is an adrenal steroidogenesis inhibitor currently in late-phase clinical development as a potentia... |
PMC5527439 | core_pubmed_pmc | Interactions between antidiabetic drugs and herbs: an overview of mechanisms of action and clinical implications | Interactions between antidiabetic drugs and herbs: an overview of mechanisms of action and clinical implications Abstract Abstract Diabetes is a complex condition with a variety of causes and pathophysiologies. The current single target approach has not provided ideal clinical outcomes for the treatment of the disease ... |
PMC9786574 | core_pubmed_pmc | Binge and high‐intensity drinking—Associations with intravenous alcohol self‐administration and underlying risk factors | Binge and high‐intensity drinking—Associations with intravenous alcohol self‐administration and underlying risk factors Abstract Abstract Some styles of alcohol consumption are riskier than others. How the level and rate of alcohol exposure contribute to the increased risk of alcohol use disorder is unclear, but likely... |
PMC10796454 | core_pubmed_pmc | Pharmacokinetics and tolerability of a veterinary phenobarbital product in healthy dogs | Pharmacokinetics and tolerability of a veterinary phenobarbital product in healthy dogs Abstract Abstract Introduction Phenobarbital has been used for many decades in both human and veterinary epileptic patients. Many formulations for a particular drug exist, most of which are marketed for humans. Recently a veterinary... |
PMC6105794 | core_pubmed_pmc | Pharmacokinetics of Piperaquine and Safety Profile of Dihydroartemisinin-Piperaquine Coadministered with Antiretroviral Therapy in Malaria-Uninfected HIV-Positive Malawian Adults | Pharmacokinetics of Piperaquine and Safety Profile of Dihydroartemisinin-Piperaquine Coadministered with Antiretroviral Therapy in Malaria-Uninfected HIV-Positive Malawian Adults Abstract There are limited data on the pharmacokinetic and safety profiles of dihydroartemisinin-piperaquine (DHA-PQ) among human immunodefic... |
PMC3697147 | core_pubmed_pmc | Treatment of Acute Tacrolimus Toxicity with Phenytoin in Solid Organ Transplant Recipients | Treatment of Acute Tacrolimus Toxicity with Phenytoin in Solid Organ Transplant Recipients Abstract The pharmacokinetics of tacrolimus are influenced by many factors, including genetic variability, acute infections, liver dysfunction, and interacting medications, which can result in elevated concentrations. The most ap... |
PMC10614689 | core_pubmed_pmc | Efficient PD-L1 imaging of murine glioblastoma with FUS-aided immunoPET by leveraging FcRn-antibody interaction | Efficient PD-L1 imaging of murine glioblastoma with FUS-aided immunoPET by leveraging FcRn-antibody interaction Abstract Rationale: The passage of antibodies through the blood-brain barrier (BBB) and the blood-tumoral barrier (BTB) is determinant not only to increase the immune checkpoint inhibitors efficacy but also t... |
PMC7086090 | core_pubmed_pmc | External Validation of a Pharmacokinetic Model of Propofol for Target-Controlled Infusion in Children under Two Years Old | External Validation of a Pharmacokinetic Model of Propofol for Target-Controlled Infusion in Children under Two Years Old Abstract Background Previously, a linked pharmacokinetic-pharmacodynamic model (the Kim model) of propofol with concurrent infusion of remifentanil was developed for children aged 2–12 years. There ... |
PMC12655235 | core_pubmed_pmc | Folic Acid-Decorated Lipidic Nanocapsules Co-Loaded with Atorvastatin and Curcumin to Enhance Glioma Targeting in Mice | Folic Acid-Decorated Lipidic Nanocapsules Co-Loaded with Atorvastatin and Curcumin to Enhance Glioma Targeting in Mice Abstract Abstract Background : Glioma remains an intractable and highly aggressive brain tumor, mainly due to the daunting obstacle presented by the blood–brain barrier (BBB). To overcome this challeng... |
PMC12872032 | core_pubmed_pmc | Steroid–tacrolimus drug–drug interaction and the effect of CYP3A genotypes | Steroid–tacrolimus drug–drug interaction and the effect of CYP3A genotypes Abstract Aims: Tacrolimus, metabolized by CYP3A4 and CYP3A5 enzymes, is susceptible to drug–drug interactions (DDI). Steroids induce CYP3A genes to increase tacrolimus clearance, but the effect is variable. We hypothesized that the extent of the... |
PMC7582433 | core_pubmed_pmc | Prediction of Cyclosporin-Mediated Drug Interaction Using Physiologically Based Pharmacokinetic Model Characterizing Interplay of Drug Transporters and Enzymes | Prediction of Cyclosporin-Mediated Drug Interaction Using Physiologically Based Pharmacokinetic Model Characterizing Interplay of Drug Transporters and Enzymes Abstract Abstract Uptake transporter organic anion transporting polypeptides (OATPs), efflux transporters (P-gp, BCRP and MRP2) and cytochrome P450 enzymes (CYP... |
PMC9610909 | core_pubmed_pmc | Simultaneous Analysis of a Combination of Anti-Hypertensive Drugs, Fimasartan, Amlodipine, and Hydrochlorothiazide, in Rats Using LC-MS/MS and Subsequent Application to Pharmacokinetic Drug Interaction with Red Ginseng Extract | Simultaneous Analysis of a Combination of Anti-Hypertensive Drugs, Fimasartan, Amlodipine, and Hydrochlorothiazide, in Rats Using LC-MS/MS and Subsequent Application to Pharmacokinetic Drug Interaction with Red Ginseng Extract Abstract Abstract Fimasartan, amlodipine, and hydrochlorothiazide are commonly used in combin... |
PMC5627754 | core_pubmed_pmc | Ocular pharmacokinetics and tolerability of bimatoprost ophthalmic solutions administered once or twice daily in rabbits, and clinical dosing implications | Ocular pharmacokinetics and tolerability of bimatoprost ophthalmic solutions administered once or twice daily in rabbits, and clinical dosing implications Abstract Abstract Purpose Fixed-combination medications can benefit patients requiring multiple agents to lower their intraocular pressure (IOP), but combining agent... |
PMC10742527 | core_pubmed_pmc | The Risk of Drug Interactions in Older Primary Care Patients after Hospital Discharge: The Role of Drug Reconciliation | The Risk of Drug Interactions in Older Primary Care Patients after Hospital Discharge: The Role of Drug Reconciliation Abstract Abstract Introduction: Drug–drug interactions (DDIs) represent an important clinical problem, particularly in older patients, due to polytherapy, comorbidity, and physiological changes in phar... |
PMC5137824 | core_pubmed_pmc | Effects of renal impairment on the pharmacokinetics of orally administered deferiprone | Effects of renal impairment on the pharmacokinetics of orally administered deferiprone Abstract Abstract Aims In light of the growing recognition of renal disease in thalassemia, it is important to understand the impact of renal impairment on the pharmacokinetics of iron chelators. This study evaluated the pharmacokine... |
PMC11597886 | core_pubmed_pmc | Phytochemical Characterization Utilizing HS-SPME/GC-MS: Exploration of the Antioxidant and Enzyme Inhibition Properties of Essential Oil from Saudi Artemisia absinthium L. | Phytochemical Characterization Utilizing HS-SPME/GC-MS: Exploration of the Antioxidant and Enzyme Inhibition Properties of Essential Oil from Saudi Artemisia absinthium L. Abstract Abstract Background/Objectives: This study aimed to analyze the chemical composition and biological activities of Artemisia absinthium L. e... |
PMC12973224 | core_pubmed_pmc | Stearic acid-modified PSMA-targeting peptide–drug conjugate for long-acting prostate cancer therapy | Stearic acid-modified PSMA-targeting peptide–drug conjugate for long-acting prostate cancer therapy Abstract Prostate-specific membrane antigen (PSMA)-targeting peptide–drug conjugates (PDCs) offer promise for the treatment of PSMA-positive prostate cancer, but their applications are limited by rapid clearance, poor ph... |
PMC7540326 | core_pubmed_pmc | Higher Dosage of Ciprofloxacin Necessary in Critically Ill Patients: A New Dosing Algorithm Based on Renal Function and Pathogen Susceptibility | Higher Dosage of Ciprofloxacin Necessary in Critically Ill Patients: A New Dosing Algorithm Based on Renal Function and Pathogen Susceptibility Abstract The objective of the present study was to develop a dosing algorithm for ciprofloxacin based on both renal function and pathogen susceptibility in critically ill patie... |
PMC3063866 | core_pubmed_pmc | Systematic Evaluation of the Descriptive and Predictive Performance of Paediatric Morphine Population Models | Systematic Evaluation of the Descriptive and Predictive Performance of Paediatric Morphine Population Models Abstract Purpose A framework for the evaluation of paediatric population models is proposed and applied to two different paediatric population pharmacokinetic models for morphine. One covariate model was based o... |
PMC7507898 | core_pubmed_pmc | Therapeutic efficacy and safety of a human fusion construct targeting the TWEAK receptor Fn14 and containing a modified granzyme B | Therapeutic efficacy and safety of a human fusion construct targeting the TWEAK receptor Fn14 and containing a modified granzyme B Abstract Background Antibody-drug conjugates are an exceptional and useful therapeutic tool for multiple diseases, particularly for cancer treatment. We previously showed that the fusion of... |
PMC7662174 | core_pubmed_pmc | Pharmacokinetics of antiretroviral and tuberculosis drugs in children with HIV/TB co-infection: a systematic review | Pharmacokinetics of antiretroviral and tuberculosis drugs in children with HIV/TB co-infection: a systematic review Abstract Abstract Introduction Management of concomitant use of ART and TB drugs is difficult because of the many drug–drug interactions (DDIs) between the medications. This systematic review provides an ... |
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