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PMC9645340 | core_pubmed_pmc | Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment | Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment Abstract Abstract The effect of moderate hepatic impairment on the pharmacokinetics (PK), safety, and tolerability of the dual endothelin receptor antagonist aproci... |
PMC11102648 | core_pubmed_pmc | The pharmacokinetics and pharmacodynamics of ibogaine in opioid use disorder patients | The pharmacokinetics and pharmacodynamics of ibogaine in opioid use disorder patients Abstract Abstract Objective: Ibogaine is a hallucinogenic drug that may be used to treat opioid use disorder (OUD). The relationships between pharmacokinetics (PKs) of ibogaine and its metabolites and their clinical effects on side ef... |
PMC8854656 | core_pubmed_pmc | Alpinetin: A Review of Its Pharmacology and Pharmacokinetics | Alpinetin: A Review of Its Pharmacology and Pharmacokinetics Abstract Abstract Flavonoids isolated from medicinal herbs have been utilized as valuable health-care agents due to their virous biological applications. Alpinetin is a natural flavonoid that emerges in many widely used medicinal plants, and has been frequent... |
PMC6539708 | core_pubmed_pmc | A Theoretical Physiologically‐Based Pharmacokinetic Approach to Ascertain Covariates Explaining the Large Interpatient Variability in Tacrolimus Disposition | A Theoretical Physiologically‐Based Pharmacokinetic Approach to Ascertain Covariates Explaining the Large Interpatient Variability in Tacrolimus Disposition Abstract Physiologically‐based pharmacokinetic ( PBPK ) modeling allows assessment of the covariates contributing to the large pharmacokinetic ( PK ) variability o... |
PMC11112299 | core_pubmed_pmc | Clinical pharmacokinetics and pharmacodynamics of venetoclax, a selective B‐cell lymphoma‐2 inhibitor | Clinical pharmacokinetics and pharmacodynamics of venetoclax, a selective B‐cell lymphoma‐2 inhibitor Abstract Abstract Venetoclax, a highly potent BCL‐2 inhibitor, is indicated for treatment of some hematologic malignancies as monotherapy, and/or in combination with other agents. Venetoclax pharmacokinetics has been e... |
PMC12454520 | core_pubmed_pmc | Elranatamab Fixed Dosing: A Safe, Effective, and Convenient Dosing Approach | Elranatamab Fixed Dosing: A Safe, Effective, and Convenient Dosing Approach Abstract Background Bispecific T-cell engagers (TCEs) are a promising modality for cancer treatment, and evaluation of dosing strategies, including utilization of body weight–based versus fixed dosing, is essential to ensure optimal therapeutic... |
PMC11435314 | core_pubmed_pmc | An Investigational Study on the Role of CYP2D6 , CYP3A4 and UGT s Genetic Variation on Fesoterodine Pharmacokinetics in Young Healthy Volunteers | An Investigational Study on the Role of CYP2D6 , CYP3A4 and UGT s Genetic Variation on Fesoterodine Pharmacokinetics in Young Healthy Volunteers Abstract Abstract Introduction: Fesoterodine is one of the most widely used antimuscarinic drugs to treat an overactive bladder. Fesoterodine is extensively hydrolyzed by este... |
PMC3585954 | core_pubmed_pmc | Pharmacokinetics, Safety and Tolerability of Bencycloquidium Bromide, a Novel Selective Muscarinic M1/M3 Receptor Antagonist, After Single and Multiple Intranasal Doses in Healthy Chinese Subjects | Pharmacokinetics, Safety and Tolerability of Bencycloquidium Bromide, a Novel Selective Muscarinic M1/M3 Receptor Antagonist, After Single and Multiple Intranasal Doses in Healthy Chinese Subjects Abstract Abstract Background: Bencycloquidium bromide (BCQB) is a novel, potent and selective muscarinic M1/M3 receptor ant... |
PMC9338184 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics and Initial Pharmacodynamics of a Subcommissural Organ-Spondin-Derived Peptide: A Randomized, Placebo-Controlled, Double-Blind, Single Ascending Dose First-in-Human Study | Safety, Tolerability, Pharmacokinetics and Initial Pharmacodynamics of a Subcommissural Organ-Spondin-Derived Peptide: A Randomized, Placebo-Controlled, Double-Blind, Single Ascending Dose First-in-Human Study Abstract Introduction This randomized, double-blind, placebo-controlled study in healthy volunteers assessed t... |
PMC7282067 | core_pubmed_pmc | Drug dosing in the critically ill obese patient—a focus on sedation, analgesia, and delirium | Drug dosing in the critically ill obese patient—a focus on sedation, analgesia, and delirium Abstract Practice guidelines provide clear evidence-based recommendations for the use of drug therapy to manage pain, agitation, and delirium associated with critical illness. Dosing recommendations however are often based on s... |
PMC7408862 | core_pubmed_pmc | Drug Tissue Distribution of TUDCA From a Biodegradable Suprachoroidal Implant versus Intravitreal or Systemic Delivery in the Pig Model | Drug Tissue Distribution of TUDCA From a Biodegradable Suprachoroidal Implant versus Intravitreal or Systemic Delivery in the Pig Model Abstract Abstract Purpose To determine local ocular tissue levels of the bile acid, tauroursodeoxycholic acid (TUDCA), in the pig model using oral, intravenous (IV), intravitreal injec... |
PMC9465247 | core_pubmed_pmc | Improved pharmacokinetics of tenofovir ester prodrugs strengthened the inhibition of HBV replication and the rebalance of hepatocellular metabolism in preclinical models | Improved pharmacokinetics of tenofovir ester prodrugs strengthened the inhibition of HBV replication and the rebalance of hepatocellular metabolism in preclinical models Abstract Abstract Tenofovir (TFV) ester prodrugs, a class of nucleotide analogs (NAs), are the first-line clinical anti-hepatitis B virus (HBV) drugs ... |
PMC8584740 | core_pubmed_pmc | A Practical Guide to Therapeutic Drug Monitoring of Biologic Medications for Inflammatory Bowel Disease | A Practical Guide to Therapeutic Drug Monitoring of Biologic Medications for Inflammatory Bowel Disease Abstract Therapeutic drug monitoring (TDM) is a useful strategy to optimize biologic medications for inflammatory bowel disease not responsive to standard dosing regimens. TDM is cost effective for anti-tumor necrosi... |
PMC8224624 | core_pubmed_pmc | Assessment of Antibody Stability in a Novel Protein-Free Serum Model | Assessment of Antibody Stability in a Novel Protein-Free Serum Model Abstract Therapeutic proteins can degrade upon administration as they are subjected to a variety of stresses in human body compartments. In vivo degradation may cause undesirable pharmacokinetic/pharmacodynamic profiles. Pre-clinical in vitro models h... |
PMC12030157 | core_pubmed_pmc | Development of Rapidly Dissolving Microneedles Integrated with Valsartan-Loaded Nanoliposomes for Transdermal Drug Delivery: In Vitro and Ex Vivo Evaluation | Development of Rapidly Dissolving Microneedles Integrated with Valsartan-Loaded Nanoliposomes for Transdermal Drug Delivery: In Vitro and Ex Vivo Evaluation Abstract Abstract Background: Hypertension (HTN) is recognized as a major risk factor for cardiovascular disease, chronic kidney disease, and peripheral artery dis... |
PMC12072229 | core_pubmed_pmc | Evaluation of Adefovir PBPK Model to Assess Biomarker‐Informed OAT1 Drug–Drug Interaction and Effect of Chronic Kidney Disease | Evaluation of Adefovir PBPK Model to Assess Biomarker‐Informed OAT1 Drug–Drug Interaction and Effect of Chronic Kidney Disease Abstract ABSTRACT Evaluation of transporter‐mediated drug–drug interactions (DDI) with endogenous biomarkers, coupled with physiologically‐based pharmacokinetic modeling (PBPK) is envisioned to... |
PMC8451076 | core_pubmed_pmc | Natural Nano-Drug Delivery System in Coptidis Rhizoma Extract with Modified Berberine Hydrochloride Pharmacokinetics | Natural Nano-Drug Delivery System in Coptidis Rhizoma Extract with Modified Berberine Hydrochloride Pharmacokinetics Abstract Purpose This study aimed to evaluate the pharmaceutical and pharmacokinetic effects of the natural nanoparticles (Nnps) isolated from Coptidis Rhizoma extract on berberine hydrochloride (BBR) an... |
PMC8423479 | core_pubmed_pmc | Infant Exposure to Dolutegravir Through Placental and Breast Milk Transfer: A Population Pharmacokinetic Analysis of DolPHIN-1 | Infant Exposure to Dolutegravir Through Placental and Breast Milk Transfer: A Population Pharmacokinetic Analysis of DolPHIN-1 Abstract Abstract Background Rapid reduction in human immunodeficiency virus (HIV) load is paramount to prevent peripartum transmission in women diagnosed late in pregnancy. We investigated dol... |
PMC6831561 | core_pubmed_pmc | Pharmacological and Behavioral Effects of the Synthetic Cannabinoid AKB48 in Rats | Pharmacological and Behavioral Effects of the Synthetic Cannabinoid AKB48 in Rats Abstract AKB48 is a designer drug belonging to the indazole synthetic cannabinoids class, illegally sold as herbal blend, incense, or research chemicals for their psychoactive cannabis-like effects. In the present study, we investigated t... |
PMC8726625 | core_pubmed_pmc | The impact of immunogenicity on therapeutic antibody pharmacokinetics: A preclinical evaluation of the effect of immune complex formation and antibody effector function on clearance | The impact of immunogenicity on therapeutic antibody pharmacokinetics: A preclinical evaluation of the effect of immune complex formation and antibody effector function on clearance Abstract ABSTRACT The occurrence of an immune response against therapeutic proteins poses a major risk for the development of biologics an... |
PMC6128722 | core_pubmed_pmc | A comprehensive review on Brigatinib – A wonder drug for targeted cancer therapy in non-small cell lung cancer | A comprehensive review on Brigatinib – A wonder drug for targeted cancer therapy in non-small cell lung cancer Abstract The mortality rate in patients suffering from non-small cell lung cancer (NSCLC) is quite high. This type of cancer mainly occurs due to rearrangements in the anaplastic lymphoma kinase (ALK) gene whi... |
PMC11475343 | core_pubmed_pmc | Degradable Bottlebrush Polypeptides and the Impact of their Architecture on Cell Uptake, Pharmacokinetics, and Biodistribution In Vivo | Degradable Bottlebrush Polypeptides and the Impact of their Architecture on Cell Uptake, Pharmacokinetics, and Biodistribution In Vivo Abstract Abstract Bottlebrush polymers are highly promising as unimolecular nanomedicines due to their unique control over the critical parameters of size, shape and chemical function. ... |
PMC7746298 | core_pubmed_pmc | Population pharmacokinetics of ivermectin for the treatment of scabies in Indigenous Australian children | Population pharmacokinetics of ivermectin for the treatment of scabies in Indigenous Australian children Abstract Ivermectin is a broad-spectrum antiparasitic agent used for the treatment and control of neglected tropical diseases. In Australia, ivermectin is primarily used for scabies and is licensed in children aged ... |
PMC6268535 | core_pubmed_pmc | Rapid and Sensitive LC-MS/MS Method for the Determination of Metoprolol in Beagle Dog Plasma with a Simple Protein Precipitation Treatment and Its Pharmacokinetic Applications | Rapid and Sensitive LC-MS/MS Method for the Determination of Metoprolol in Beagle Dog Plasma with a Simple Protein Precipitation Treatment and Its Pharmacokinetic Applications Abstract Abstract A rapid LC-MS/MS method with good accuracy and sensitivity was developed and validated for the pharmacokinetics study of metop... |
PMC8928849 | core_pubmed_pmc | Evaluation of the inhibitory effect of quercetin on the pharmacokinetics of tucatinib in rats by a novel UPLC–MS/MS assay | Evaluation of the inhibitory effect of quercetin on the pharmacokinetics of tucatinib in rats by a novel UPLC–MS/MS assay Abstract Abstract Context Tucatinib (CYP2C8 substrate) and quercetin (CYP2C8 inhibitor) are two common drugs for the treatment of cancer. However, the effect of quercetin on the metabolism of tucati... |
PMC7089330 | core_pubmed_pmc | Exploration of structural and physicochemical requirements and search of virtual hits for aminopeptidase N inhibitors | Exploration of structural and physicochemical requirements and search of virtual hits for aminopeptidase N inhibitors Abstract Abstract Aminopeptidase N (APN) inhibitors have been reported to be effective in treating of life threatening diseases including cancer. Validated ligand- and structure-based pharmacophore mapp... |
PMC11428266 | core_pubmed_pmc | Risk Factors Associated with Antibiotic Exposure Variability in Critically Ill Patients: A Systematic Review | Risk Factors Associated with Antibiotic Exposure Variability in Critically Ill Patients: A Systematic Review Abstract Abstract (1) Background: Knowledge about the behavior of antibiotics in critically ill patients has been increasing in recent years. Some studies have concluded that a high percentage may be outside the... |
PMC12754995 | core_pubmed_pmc | Give weekly adalimumab a chance before discontinuing it: a retrospective clinical and pharmacokinetic analysis in pediatric rheumatology | Give weekly adalimumab a chance before discontinuing it: a retrospective clinical and pharmacokinetic analysis in pediatric rheumatology Abstract Abstract Background Subcutaneous adalimumab is the preferred treatment for most children with juvenile idiopathic arthritis (JIA) and non-infectious uveitis, usually administ... |
PMC10178888 | core_pubmed_pmc | Topical Treatment for Retinal Degenerative Pathologies: A Systematic Review | Topical Treatment for Retinal Degenerative Pathologies: A Systematic Review Abstract The topical administration of medicines is the preferred route in ocular therapy, at least for the anterior segment of the eye. However, the eye’s inherent functional and biological barriers all work against the active pharmaceutical i... |
PMC5336418 | core_pubmed_pmc | PK/PD Target Attainment With Ceftolozane/Tazobactam Using Monte Carlo Simulation in Patients With Various Degrees of Renal Function, Including Augmented Renal Clearance and End-Stage Renal Disease | PK/PD Target Attainment With Ceftolozane/Tazobactam Using Monte Carlo Simulation in Patients With Various Degrees of Renal Function, Including Augmented Renal Clearance and End-Stage Renal Disease Abstract Abstract Introduction Ceftolozane/tazobactam is an antibacterial agent with potent in vitro activity against Gram-... |
PMC5397556 | core_pubmed_pmc | Database of Optimized Proteomic Quantitative Methods for Human Drug Disposition‐Related Proteins for Applications in Physiologically Based Pharmacokinetic Modeling | Database of Optimized Proteomic Quantitative Methods for Human Drug Disposition‐Related Proteins for Applications in Physiologically Based Pharmacokinetic Modeling Abstract Abstract The purpose of this study was to create an open access repository of validated liquid chromatography tandem mass spectrometry (LC‐MS/MS) m... |
PMC10632074 | core_pubmed_pmc | Pretreatment albumin is a prognostic and predictive biomarker for response to atezolizumab across solid tumors | Pretreatment albumin is a prognostic and predictive biomarker for response to atezolizumab across solid tumors Abstract Abstract Objectives Reliable predictive biomarkers for response to immune checkpoint inhibition (ICI) are lacking. Pretreatment serum albumin, a known prognostic and predictive factor in ICI‐treated p... |
PMC11205493 | core_pubmed_pmc | Development and Validation of a Simple and Reliable HPLC-UV Method for Determining Gemcitabine Levels: Application in Pharmacokinetic Analysis | Development and Validation of a Simple and Reliable HPLC-UV Method for Determining Gemcitabine Levels: Application in Pharmacokinetic Analysis Abstract Background and Objectives : Gemcitabine has been used to treat various solid cancers, including, since 1997, metastatic pancreatic cancer. Here, we developed an HPLC-UV... |
PMC6839879 | core_pubmed_pmc | Three-dimensional (3D) brain microphysiological system for organophosphates and neurochemical agent toxicity screening | Three-dimensional (3D) brain microphysiological system for organophosphates and neurochemical agent toxicity screening Abstract Abstract We investigated a potential use of a 3D tetraculture brain microphysiological system (BMPS) for neurotoxic chemical agent screening. This platform consists of neuronal tissue with ext... |
PMC9686672 | core_pubmed_pmc | Defining Exposure Predictors of Meropenem That Are Associated with Improved Survival for Severe Bacterial Infection: A Preclinical PK/PD Study in Sepsis Rat Model | Defining Exposure Predictors of Meropenem That Are Associated with Improved Survival for Severe Bacterial Infection: A Preclinical PK/PD Study in Sepsis Rat Model Abstract Abstract Background : The pharmacokinetic/pharmacodynamic (PK/PD) index of carbapenems that best correlates with in vivo antimicrobial activity is p... |
PMC6839911 | core_pubmed_pmc | Axitinib in Combination With Toripalimab, a Humanized Immunoglobulin G 4 Monoclonal Antibody Against Programmed Cell Death-1, in Patients With Metastatic Mucosal Melanoma: An Open-Label Phase IB Trial | Axitinib in Combination With Toripalimab, a Humanized Immunoglobulin G 4 Monoclonal Antibody Against Programmed Cell Death-1, in Patients With Metastatic Mucosal Melanoma: An Open-Label Phase IB Trial Abstract PURPOSE Metastatic mucosal melanoma responds poorly to anti–programmed cell death-1 (PD-1) monotherapy. Vascul... |
PMC7511284 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Studies of Elacestrant, A Novel Oral Selective Estrogen Receptor Degrader, in Healthy Post-Menopausal Women | Pharmacokinetic and Pharmacodynamic Studies of Elacestrant, A Novel Oral Selective Estrogen Receptor Degrader, in Healthy Post-Menopausal Women Abstract Background and Objectives Advanced estrogen receptor-positive (ER+) breast cancer is currently treated with endocrine therapy. Elacestrant is a novel, nonsteroidal, se... |
PMC8920105 | core_pubmed_pmc | Evaluation of pharmacokinetics of warfarin from validated pharmacokinetic-pharmacodynamic model | Evaluation of pharmacokinetics of warfarin from validated pharmacokinetic-pharmacodynamic model Abstract Abstract Background Pharmacokinetics of warfarin has not been described in our population. We derived the pharmacokinetic parameters from a validated pharmacokinetic-pharmacodynamic model. Methods Patients receiving... |
PMC7792585 | core_pubmed_pmc | Trospium Chloride Transport by Mouse Drug Carriers of the Slc22 and Slc47 Families | Trospium Chloride Transport by Mouse Drug Carriers of the Slc22 and Slc47 Families Abstract Abstract Background: The muscarinic receptor antagonist trospium chloride (TCl) is used for pharmacotherapy of the overactive bladder syndrome. TCl is a hydrophilic positively charged drug. Therefore, it has low permeability thr... |
PMC12196407 | core_pubmed_pmc | Biological and Biosimilar Medicines in Contemporary Pharmacotherapy for Metabolic Syndrome | Biological and Biosimilar Medicines in Contemporary Pharmacotherapy for Metabolic Syndrome Abstract Abstract The discovery of new drugs offers valuable alternatives, particularly for treating diseases that are resistant to existing therapies or involving complex, multi-organ conditions such as metabolic syndrome. Altho... |
PMC8941010 | core_pubmed_pmc | Pharmacokinetics, Safety, Efficacy, and Biomarker Profiles During Nemolizumab Treatment of Atopic Dermatitis in Adolescents | Pharmacokinetics, Safety, Efficacy, and Biomarker Profiles During Nemolizumab Treatment of Atopic Dermatitis in Adolescents Abstract Abstract Introduction Nemolizumab, a new monoclonal antibody that targets the receptor alpha of the neuroimmune cytokine interleukin-31 (IL-31), has shown efficacy in atopic dermatitis (A... |
PMC12445431 | core_pubmed_pmc | Efficacy of Topical Non-Selective and COX-2 Selective NSAIDs in Accelerating Resolution of Acute Central Serous Chorioretinopathy: A Retrospective Analysis | Efficacy of Topical Non-Selective and COX-2 Selective NSAIDs in Accelerating Resolution of Acute Central Serous Chorioretinopathy: A Retrospective Analysis Abstract Abstract Purpose To evaluate whether topical nonsteroidal anti-inflammatory drugs (NSAIDs) accelerate the resolution of acute central serous chorioretinopa... |
PMC12881975 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of desoxycorticosterone pivalate in dogs with hypoadrenocorticism | Pharmacokinetics and pharmacodynamics of desoxycorticosterone pivalate in dogs with hypoadrenocorticism Abstract Abstract Background Desoxycorticosterone pivalate (DOCP) is commonly used to treat mineralocorticoid deficiency in dogs with hypoadrenocorticism (HA). Hypothesis/Objective To determine the pharmacokinetics a... |
PMC12587601 | core_pubmed_pmc | Population pharmacokinetics of ritonavir as a booster of lopinavir, atazanavir, or darunavir in African children with HIV | Population pharmacokinetics of ritonavir as a booster of lopinavir, atazanavir, or darunavir in African children with HIV Abstract ABSTRACT Ritonavir is important in antiretroviral therapy (ART) because it is used to boost the drug exposure of its fellow protease inhibitors (PIs). While PIs are commonly used in childre... |
PMC11476770 | core_pubmed_pmc | Molecular Mechanisms Affecting Statin Pharmacokinetics after Bariatric Surgery | Molecular Mechanisms Affecting Statin Pharmacokinetics after Bariatric Surgery Abstract Abstract According to recent data, one in eight people in the world struggle with obesity. Obesity management is increasingly dependent on bariatric surgical interventions, as the combination of lifestyle modifications and pharmacot... |
PMC12828233 | core_pubmed_pmc | Systemic distribution of tricyclo-DNA antisense oligonucleotide following intratracheal instillation in the mouse | Systemic distribution of tricyclo-DNA antisense oligonucleotide following intratracheal instillation in the mouse Abstract Abstract This study evaluated intratracheal (IT) instillation as an alternative route for systemic delivery of therapeutic tricyclo-DNA antisense oligonucleotides (tcDNA-ASOs), using the Duchenne m... |
PMC10957775 | core_pubmed_pmc | Integrated chemical characterization, metabolite profiling, and pharmacokinetics analysis of Zhijun Tangshen Decoction by UPLC-Q/TOF-MS | Integrated chemical characterization, metabolite profiling, and pharmacokinetics analysis of Zhijun Tangshen Decoction by UPLC-Q/TOF-MS Abstract Abstract Diabetic nephropathy (DN) is the main cause of end-stage renal disease worldwide and a major public issue affecting the health of people. Therefore, it is essential t... |
PMC6771557 | core_pubmed_pmc | Effect of a single dose of insulin glargine/lixisenatide fixed ratio combination (iGlarLixi) on postprandial glucodynamic response in Japanese patients with type 2 diabetes mellitus: A phase I randomized trial | Effect of a single dose of insulin glargine/lixisenatide fixed ratio combination (iGlarLixi) on postprandial glucodynamic response in Japanese patients with type 2 diabetes mellitus: A phase I randomized trial Abstract Abstract This report describes novel clinical data assessing the pharmacodynamics of insulin glargine... |
PMC9201829 | core_pubmed_pmc | Hierarchical Virtual Screening Based on Rocaglamide Derivatives to Discover New Potential Anti-Skin Cancer Agents | Hierarchical Virtual Screening Based on Rocaglamide Derivatives to Discover New Potential Anti-Skin Cancer Agents Abstract Skin Cancer (SC) is among the most common type of cancers worldwide. The search for SC therapeutics using molecular modeling strategies as well as considering natural plant-derived products seems t... |
PMC11568537 | core_pubmed_pmc | Adverse drug reactions and its associated factors among geriatric hospitalized patients at selected comprehensive specialized hospitals of the Amhara Region, Ethiopia: a multicenter prospective cohort study | Adverse drug reactions and its associated factors among geriatric hospitalized patients at selected comprehensive specialized hospitals of the Amhara Region, Ethiopia: a multicenter prospective cohort study Abstract Abstract Background Adverse drug reactions are more prevalent in geriatric patients and are frequently a... |
PMC11052088 | core_pubmed_pmc | The Conventional and Breakthrough Tool for the Study of L-Glutamate Transporters | The Conventional and Breakthrough Tool for the Study of L-Glutamate Transporters Abstract Abstract In our recent report, we clarified the direct interaction between the excitatory amino acid transporter (EAAT) 1/2 and polyunsaturated fatty acids (PUFAs) by applying electrophysiological and molecular biological techniqu... |
PMC12151970 | core_pubmed_pmc | Clinical Pharmacokinetics and Safety of a New HIV-1 Capsid Inhibitor, VH4004280, After Oral Administration in Adults Without HIV | Clinical Pharmacokinetics and Safety of a New HIV-1 Capsid Inhibitor, VH4004280, After Oral Administration in Adults Without HIV Abstract Introduction The pharmacokinetics, drug–drug interaction potential, and safety of a new HIV-1 capsid inhibitor, VH4004280 (VH-280), are described in this first-time-in-human study. M... |
PMC6056420 | core_pubmed_pmc | A novel calix[4]pyrrole derivative as a potential anticancer agent that forms genotoxic adducts with DNA | A novel calix[4]pyrrole derivative as a potential anticancer agent that forms genotoxic adducts with DNA Abstract Abstract meso -( p -acetamidophenyl)-calixpyrrole 3 was found to exhibit remarkable cytotoxicity towards A549 cancer cells. A comparative study including the isomer of 3 meso -( m -acetamidophenyl)-calixpyr... |
PMC11990080 | core_pubmed_pmc | Essential Oil of Lippia origanoides Kunth: Nanoformulation, Anticholinesterase Activity, and Molecular Docking | Essential Oil of Lippia origanoides Kunth: Nanoformulation, Anticholinesterase Activity, and Molecular Docking Abstract Abstract This study investigates the therapeutic potential of Lippia origanoides essential oil (LOEO) in neurological and pharmaceutical applications. The chemical composition of LOEO was analyzed usi... |
PMC3101238 | core_pubmed_pmc | Omeprazole Inhibits Proliferation and Modulates Autophagy in Pancreatic Cancer Cells | Omeprazole Inhibits Proliferation and Modulates Autophagy in Pancreatic Cancer Cells Abstract Background Omeprazole has recently been described as a modulator of tumour chemoresistance, although its underlying molecular mechanisms remain controversial. Since pancreatic tumours are highly chemoresistant, a logical step ... |
PMC10250344 | core_pubmed_pmc | Generating immunogenomic data-guided virtual patients using a QSP model to predict response of advanced NSCLC to PD-L1 inhibition | Generating immunogenomic data-guided virtual patients using a QSP model to predict response of advanced NSCLC to PD-L1 inhibition Abstract Generating realistic virtual patients from a limited amount of patient data is one of the major challenges for quantitative systems pharmacology modeling in immuno-oncology. Quantit... |
PMC7570662 | core_pubmed_pmc | In Vivo Pharmacokinetic Analysis Utilizing Non-Targeted and Targeted Mass Spectrometry and In Vitro Assay against Transient Receptor Potential Channels of Maobushisaishinto and Its Constituent Asiasari Radix | In Vivo Pharmacokinetic Analysis Utilizing Non-Targeted and Targeted Mass Spectrometry and In Vitro Assay against Transient Receptor Potential Channels of Maobushisaishinto and Its Constituent Asiasari Radix Abstract Abstract The Japanese traditional medicine maobushisaishinto (MBST) has been prescribed for treating up... |
PMC8092647 | core_pubmed_pmc | Assessment of carbapenems in a mouse model of Mycobacterium tuberculosis infection | Assessment of carbapenems in a mouse model of Mycobacterium tuberculosis infection Abstract We present further study of a subset of carbapenems, arising from a previously reported machine learning approach, with regard to their mouse pharmacokinetic profiling and subsequent study in a mouse model of sub-acute Mycobacte... |
PMC7894404 | core_pubmed_pmc | Model‐Informed Pediatric Dose Selection for Dapagliflozin by Incorporating Developmental Changes | Model‐Informed Pediatric Dose Selection for Dapagliflozin by Incorporating Developmental Changes Abstract Abstract This analysis reports a quantitative modeling and simulation approach for oral dapagliflozin, a primarily uridine diphosphate‐glucuronosyltransferase (UGT)–metabolized human sodium‐glucose cotransporter 2 ... |
PMC8986735 | core_pubmed_pmc | Translational Modeling Identifies Synergy between Nanoparticle-Delivered miRNA-22 and Standard-of-Care Drugs in Triple-Negative Breast Cancer | Translational Modeling Identifies Synergy between Nanoparticle-Delivered miRNA-22 and Standard-of-Care Drugs in Triple-Negative Breast Cancer Abstract Purpose Downregulation of miRNA-22 in triple-negative breast cancer (TNBC) is associated with upregulation of eukaryotic elongation 2 factor kinase (eEF2K) protein, whic... |
PMC10275282 | core_pubmed_pmc | Jitteriness/anxiety syndrome caused by coadministration of celecoxib, a selective COX‐2 inhibitor, with escitalopram and trazodone in a patient with depression and spondylolisthesis | Jitteriness/anxiety syndrome caused by coadministration of celecoxib, a selective COX‐2 inhibitor, with escitalopram and trazodone in a patient with depression and spondylolisthesis Abstract Abstract Antidepressant‐induced jitteriness/anxiety syndrome is characterized as anxiety, agitation, panic attacks, insomnia, irr... |
PMC5971579 | core_pubmed_pmc | Overcoming the Resistance Hurdle: Pharmacokinetic-Pharmacodynamic Target Attainment Analyses for Rezafungin (CD101) against Candida albicans and Candida glabrata | Overcoming the Resistance Hurdle: Pharmacokinetic-Pharmacodynamic Target Attainment Analyses for Rezafungin (CD101) against Candida albicans and Candida glabrata Abstract ABSTRACT Rezafungin (CD101) is a novel echinocandin antifungal agent with activity against Aspergillus and Candida species, including azole- and echi... |
PMC12497527 | core_pubmed_pmc | Elucidating the Therapeutic Mechanism of Danggui Liuhuang Decoction in Hyperthyroid Kidney Disease: An Integration of Network Pharmacology and Metabolomics | Elucidating the Therapeutic Mechanism of Danggui Liuhuang Decoction in Hyperthyroid Kidney Disease: An Integration of Network Pharmacology and Metabolomics Abstract Abstract Background and Objective: Danggui Liuhuang decoction (DLD) demonstrates pharmacological efficacy in the treatment of hyperthyroid kidney disease (... |
PMC9485022 | core_pubmed_pmc | A population pharmacokinetic model of remdesivir and its major metabolites based on published mean values from healthy subjects | A population pharmacokinetic model of remdesivir and its major metabolites based on published mean values from healthy subjects Abstract Abstract Remdesivir is a direct-acting anti-viral agent. It was originally evaluated against filoviruses. However, during the COVID-19 pandemic, it was investigated due to its anti-vi... |
PMC7070801 | core_pubmed_pmc | A Double‐Blind, Phase I, Single Ascending Dose Study to Assess the Safety, Pharmacokinetics, and Pharmacodynamics of BOS161721 in Healthy Subjects | A Double‐Blind, Phase I, Single Ascending Dose Study to Assess the Safety, Pharmacokinetics, and Pharmacodynamics of BOS161721 in Healthy Subjects Abstract Abstract The purpose of this study was to assess the safety, tolerability, pharmacokinetics, pharmacodynamics, and immunogenicity of BOS161721, a humanized immunogl... |
PMC7229136 | core_pubmed_pmc | Pharmacokinetics of Ambroxol Sustained Release (Mucosolvan ® Retard) Compared with Other Formulations in Healthy Volunteers | Pharmacokinetics of Ambroxol Sustained Release (Mucosolvan ® Retard) Compared with Other Formulations in Healthy Volunteers Abstract Abstract Introduction Ambroxol is used in the treatment of acute and chronic respiratory conditions characterized by abnormal mucus secretion and impaired mucus transport and is available... |
PMC9786172 | core_pubmed_pmc | Determination of Leuprolide–Fatty Acid Conjugate in Rat Plasma Using LC-MS/MS and Its Pharmacokinetics after Subcutaneous Administration in Rats | Determination of Leuprolide–Fatty Acid Conjugate in Rat Plasma Using LC-MS/MS and Its Pharmacokinetics after Subcutaneous Administration in Rats Abstract Abstract Leuprolide is a synthetic nonapeptide drug (pyroGlu-His-Trp-Ser-Tyr- d -Leu-Leu-Arg-Pro-NHEt) that acts as a gonadotropin-releasing hormone agonist. The cont... |
PMC11155132 | core_pubmed_pmc | A Phase 1, randomized, double-blind, placebo-controlled, single- and multiple-dose escalation study to evaluate the safety and pharmacokinetics/pharmacodynamics of PF-06835375, a C-X-C chemokine receptor type 5 directed antibody, in patients with systemic lupus erythematosus or rheumatoid arthritis | A Phase 1, randomized, double-blind, placebo-controlled, single- and multiple-dose escalation study to evaluate the safety and pharmacokinetics/pharmacodynamics of PF-06835375, a C-X-C chemokine receptor type 5 directed antibody, in patients with systemic lupus erythematosus or rheumatoid arthritis Abstract Abstract Ba... |
PMC8666568 | core_pubmed_pmc | The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS | The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS Abstract Objective: A robust, quick, and reliable ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS) method for the quantification of erdafitinib in beagle dog plasma was developed... |
PMC6585706 | core_pubmed_pmc | Evaluation of Food and Spherical Carbon Adsorbent Effects on the Pharmacokinetics of Roxadustat in Healthy Nonelderly Adult Male Japanese Subjects | Evaluation of Food and Spherical Carbon Adsorbent Effects on the Pharmacokinetics of Roxadustat in Healthy Nonelderly Adult Male Japanese Subjects Abstract Abstract Roxadustat is a hypoxia‐inducible factor prolyl hydroxylase inhibitor in late‐stage clinical development for the treatment of anemia in chronic kidney dise... |
PMC10459069 | core_pubmed_pmc | Comparative Serum and Brain Pharmacokinetics of Quercetin after Oral and Nasal Administration to Rats as Lyophilized Complexes with β-Cyclodextrin Derivatives and Their Blends with Mannitol/Lecithin Microparticles | Comparative Serum and Brain Pharmacokinetics of Quercetin after Oral and Nasal Administration to Rats as Lyophilized Complexes with β-Cyclodextrin Derivatives and Their Blends with Mannitol/Lecithin Microparticles Abstract Abstract Quercetin (Que) is one of the most studied flavonoids with strong antioxidant properties... |
PMC9010250 | core_pubmed_pmc | Effect of food on capsule and granule formulations of selumetinib | Effect of food on capsule and granule formulations of selumetinib Abstract Abstract Selumetinib is an oral, potent, and highly selective allosteric MEK1/2 inhibitor approved for the treatment of pediatric patients (aged ≥2 years) with neurofibromatosis type 1 who have symptomatic, inoperable plexiform neurofibromas. A ... |
PMC9098584 | core_pubmed_pmc | Phase I trial of ATM inhibitor M3541 in combination with palliative radiotherapy in patients with solid tumors | Phase I trial of ATM inhibitor M3541 in combination with palliative radiotherapy in patients with solid tumors Abstract Background . Ataxia telangiectasia mutated (ATM) kinase orchestrates DNA double strand break (DSB) repair; ATM inhibitors may therefore enhance the therapeutic effect of DSB-inducing treatments such a... |
PMC6639421 | core_pubmed_pmc | Assessment of Demographic and Socio-Behavioral Factors on Adherence to HIV Pre-Exposure Prophylaxis Using a Markov Modeling Approach | Assessment of Demographic and Socio-Behavioral Factors on Adherence to HIV Pre-Exposure Prophylaxis Using a Markov Modeling Approach Abstract Purpose: Adherence is important for the effectiveness of human immunodeficiency virus (HIV) preexposure prophylaxis (PrEP). The objective of the current work is to assess the imp... |
PMC9189214 | core_pubmed_pmc | Allicin affects the pharmacokinetics of sulfadiazine and florfenicol by downregulating the expression of jejunum P-gp and BCRP in broilers | Allicin affects the pharmacokinetics of sulfadiazine and florfenicol by downregulating the expression of jejunum P-gp and BCRP in broilers Abstract Allicin, one of the main bioactive compounds in garlic, is an excellent feed additive. It is unknown whether allicin affects the expression of P-gp and BCRP, 2 important AB... |
PMC12284239 | core_pubmed_pmc | Multi-Target Synergy Against Acute Lung Injury: Systems Pharmacology Decoding Dahuang-Huangqin Herb Pair’s Therapeutic Mechanism | Multi-Target Synergy Against Acute Lung Injury: Systems Pharmacology Decoding Dahuang-Huangqin Herb Pair’s Therapeutic Mechanism Abstract Abstract Aim This study investigates the therapeutic mechanisms of Radix et Rhizoma Rhei-Scutellaria baicalensis Georgi (DH-HQ) herb pair against acute lung injury (ALI) using integr... |
PMC9807490 | core_pubmed_pmc | Preclinical exploration of combined glucagon inhibition and liver-preferential insulin for treatment of diabetes using in vitro assays and rat and mouse models | Preclinical exploration of combined glucagon inhibition and liver-preferential insulin for treatment of diabetes using in vitro assays and rat and mouse models Abstract Aims/hypothesis Normalisation of blood glucose in individuals with diabetes is recommended to reduce development of diabetic complications. However, ri... |
PMC3261664 | core_pubmed_pmc | Targeting the Endothelin Axis with Atrasentan, in combination with IFN-alpha, in metastatic renal cell carcinoma | Targeting the Endothelin Axis with Atrasentan, in combination with IFN-alpha, in metastatic renal cell carcinoma Abstract Abstract Background: The endothelin system is involved in tumour growth. Atrasentan, a selective endothelin-A-receptor antagonist, blocks endothelin signalling. This phase I trial studied combining ... |
PMC5761055 | core_pubmed_pmc | Comparative pharmacokinetics of five saponins after intravenous administration of TSFS injection and TSFS injection plus TFFG in rats under different physiological states | Comparative pharmacokinetics of five saponins after intravenous administration of TSFS injection and TSFS injection plus TFFG in rats under different physiological states Abstract Abstract Sanqi is a popular traditional Chinese medicine and commonly used for promoting blood circulation and removing blood stasis. Notogi... |
PMC10141516 | core_pubmed_pmc | Development of Clinically Optimized Sitagliptin and Dapagliflozin Complex Tablets: Pre-Formulation, Formulation, and Human Bioequivalence Studies | Development of Clinically Optimized Sitagliptin and Dapagliflozin Complex Tablets: Pre-Formulation, Formulation, and Human Bioequivalence Studies Abstract The purpose of this study is to derive an optimal drug release formulation with human clinical bioequivalence in developing a sitagliptin phosphate monohydrate-dapag... |
PMC7520421 | core_pubmed_pmc | A model-based analysis identifies differences in phenotypic resistance between in vitro and in vivo: implications for translational medicine within tuberculosis | A model-based analysis identifies differences in phenotypic resistance between in vitro and in vivo: implications for translational medicine within tuberculosis Abstract Abstract Proper characterization of drug effects on Mycobacterium tuberculosis relies on the characterization of phenotypically resistant bacteria to ... |
PMC11006409 | core_pubmed_pmc | Safety and Tolerability of the APOL1 Inhibitor, Inaxaplin, following Single- and Multiple-Ascending Doses in Healthy Adults | Safety and Tolerability of the APOL1 Inhibitor, Inaxaplin, following Single- and Multiple-Ascending Doses in Healthy Adults Abstract Abstract Introduction Toxic gain-of-function Apolipoprotein L1 ( APOL1 ) variants contribute to the development of proteinuric nephropathies collectively referred to as APOL1-mediated kid... |
PMC12309453 | core_pubmed_pmc | Pharmacodynamic effects of early aspirin withdrawal after percutaneous coronary intervention in patients with atrial fibrillation treated with ticagrelor or prasugrel | Pharmacodynamic effects of early aspirin withdrawal after percutaneous coronary intervention in patients with atrial fibrillation treated with ticagrelor or prasugrel Abstract ABSTRACT Dual antithrombotic therapy (DAT) without aspirin reduces bleeding compared with triple antithrombotic therapy (TAT) in patients with a... |
PMC5324641 | core_pubmed_pmc | Clinical Pharmacology of Delafloxacin in Patients With Hepatic Impairment | Clinical Pharmacology of Delafloxacin in Patients With Hepatic Impairment Abstract Abstract Delafloxacin is a novel anionic fluoroquinolone with robust activity against Gram‐positive, Gram‐negative, atypical, and anaerobic bacteria, including methicillin‐resistant S aureus . Delafloxacin is currently being studied for ... |
PMC10081578 | core_pubmed_pmc | Dose optimization of vancomycin in obese patients: A systematic review | Dose optimization of vancomycin in obese patients: A systematic review Abstract Abstract Background: Dose optimization of vancomycin plays a substantial role in drug pharmacokinetics because of the increased incidence of obesity worldwide. This systematic review was aimed to highlight the current dosing strategy of van... |
PMC6624439 | core_pubmed_pmc | Pharmacokinetics of Intranasally Administered Dexmedetomidine in Chinese Children | Pharmacokinetics of Intranasally Administered Dexmedetomidine in Chinese Children Abstract Background: Intranasal application is a comfortable, effective, nearly non-invasive, and easy route of administration in children. To date, there is, however, only one pharmacokinetic study on intranasal dexmedetomidine in pediat... |
PMC10607223 | core_pubmed_pmc | Impact of Sex and Genetic Variation in Relevant Pharmacogenes on the Pharmacokinetics and Safety of Valsartan, Olmesartan and Hydrochlorothiazide | Impact of Sex and Genetic Variation in Relevant Pharmacogenes on the Pharmacokinetics and Safety of Valsartan, Olmesartan and Hydrochlorothiazide Abstract Drug combination therapy is the most common pharmacological strategy for hypertension management. No pharmacogenetic biomarkers for guiding hypertension pharmacother... |
PMC4076864 | core_pubmed_pmc | Chronopharmacodynamics of drugs in toxicological aspects: A short review for clinical pharmacists and pharmacy practitioners | Chronopharmacodynamics of drugs in toxicological aspects: A short review for clinical pharmacists and pharmacy practitioners Abstract Abstract For many decades, researchers are aware of the importance of circadian rhythm in physiological/biochemical properties and drug metabolism. Chronopharmacology is the study of how... |
PMC10583249 | core_pubmed_pmc | Multivariate modeling of magnetic resonance biomarkers and clinical outcome measures for Duchenne muscular dystrophy clinical trials | Multivariate modeling of magnetic resonance biomarkers and clinical outcome measures for Duchenne muscular dystrophy clinical trials Abstract Abstract Although regulatory agencies encourage inclusion of imaging biomarkers in clinical trials for Duchenne muscular dystrophy (DMD), industry receives minimal guidance on ho... |
PMC9917302 | core_pubmed_pmc | Polymorphisms Affecting the Response to Novel Antiepileptic Drugs | Polymorphisms Affecting the Response to Novel Antiepileptic Drugs Abstract Epilepsy is one of the most frequent chronic neurologic disorders that affects nearly 1% of the population worldwide, especially in developing countries. Currently, several antiepileptic drugs (AEDs) are available for its therapy, and although t... |
PMC12309645 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic evaluation of sulbactam‐durlobactam in a critically ill patient on continuous venovenous hemofiltration infected with carbapenem‐resistant Acinetobacter baumannii‐calcoaceticus complex | Pharmacokinetic and pharmacodynamic evaluation of sulbactam‐durlobactam in a critically ill patient on continuous venovenous hemofiltration infected with carbapenem‐resistant Acinetobacter baumannii‐calcoaceticus complex Abstract Abstract Background Drug databases currently do not provide dosing guidance for sulbactam‐... |
PMC10789452 | core_pubmed_pmc | Low-dose naltrexone for treatment of pain in patients with fibromyalgia: a randomized, double-blind, placebo-controlled, crossover study | Low-dose naltrexone for treatment of pain in patients with fibromyalgia: a randomized, double-blind, placebo-controlled, crossover study Abstract Supplemental Digital Content is Available in the Text. Keywords: Low-dose naltrexone, Fibromyalgia patients, Chronic pain, RCT Abstract Introduction: Fibromyalgia (FM) is a c... |
PMC10559696 | core_pubmed_pmc | Total intravenous anesthesia management with simultaneous use of remimazolam and propofol: A case series of three patients | Total intravenous anesthesia management with simultaneous use of remimazolam and propofol: A case series of three patients Abstract Abstract Remimazolam is an ultra-short-acting benzodiazepine anesthetic agent. Because of pharmacodynamic interactions in the sedation effect between benzodiazepines and propofol, the comb... |
PMC6609630 | core_pubmed_pmc | A repository of protein abundance data of drug metabolizing enzymes and transporters for applications in physiologically based pharmacokinetic (PBPK) modelling and simulation | A repository of protein abundance data of drug metabolizing enzymes and transporters for applications in physiologically based pharmacokinetic (PBPK) modelling and simulation Abstract Abstract Population factors such as age, gender, ethnicity, genotype and disease state can cause inter-individual variability in pharmac... |
PMC9381908 | core_pubmed_pmc | Population pharmacokinetic model for once‐daily intravenous busulfan in pediatric subjects describing time‐associated clearance | Population pharmacokinetic model for once‐daily intravenous busulfan in pediatric subjects describing time‐associated clearance Abstract Abstract This study aimed to characterize the population pharmacokinetics (PK) of busulfan focusing on how busulfan clearance (CL) changes over time during once‐daily administration a... |
PMC5066743 | core_pubmed_pmc | Phase 1 Study of Safety, Tolerability, and Pharmacokinetics of PTC299, an Inhibitor of Stress‐Regulated Protein Translation | Phase 1 Study of Safety, Tolerability, and Pharmacokinetics of PTC299, an Inhibitor of Stress‐Regulated Protein Translation Abstract Abstract PTC299 is a novel small molecule that specifically blocks the production of protein from selected mRNAs that under certain conditions use noncanonical ribosomal translational pat... |
PMC9228520 | core_pubmed_pmc | Structural Elucidation of Rift Valley Fever Virus L Protein towards the Discovery of Its Potential Inhibitors | Structural Elucidation of Rift Valley Fever Virus L Protein towards the Discovery of Its Potential Inhibitors Abstract Abstract Rift valley fever virus (RVFV) is the causative agent of a viral zoonosis that causes a significant clinical burden in domestic and wild ruminants. Major outbreaks of the virus occur in livest... |
PMC3530871 | core_pubmed_pmc | Anti hyperglycaemic study of natural inhibitors for Insulin receptor | Anti hyperglycaemic study of natural inhibitors for Insulin receptor Abstract Diabetes is a metabolic disorder associated with either improper functioning of the beta-cells or wherein cells fail to use insulin properly. Insulin, the principal hormone regulates uptake of glucose from the blood into most of the cells exc... |
PMC10880038 | core_pubmed_pmc | The effect of genetic variants in the transcription factor TSPYL family on the CYP3A4 mediated cyclosporine metabolism in kidney transplant patients | The effect of genetic variants in the transcription factor TSPYL family on the CYP3A4 mediated cyclosporine metabolism in kidney transplant patients Abstract Abstract CYP3A4 activity shows considerable interindividual variability. Although studies indicate 60%–80% is heritable, common single nucleotide variants (SNVs) ... |
PMC12154015 | core_pubmed_pmc | A Novel Approach for the Activity Assessment of L-Asparaginase Formulations When Dealing with Complex Biological Samples | A Novel Approach for the Activity Assessment of L-Asparaginase Formulations When Dealing with Complex Biological Samples Abstract Abstract Majority of commercial L-asparaginase (L-ASNase) activity assays are based on coupled enzymatic reaction, which converts aspartate into pyruvate, subsequently reacting with the prob... |
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