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PMC3137274 | core_pubmed_pmc | Metabolism and Pharmacokinetics of San-Huang-Xie-Xin-Tang, a Polyphenol-Rich Chinese Medicine Formula, in Rats and Ex-Vivo Antioxidant Activity | Metabolism and Pharmacokinetics of San-Huang-Xie-Xin-Tang, a Polyphenol-Rich Chinese Medicine Formula, in Rats and Ex-Vivo Antioxidant Activity Abstract San-Huang-Xie-Xin-Tang (SHXXT), a widely used Chinese herbal formula, consists of rhizomes of Rheum officinale , roots of Scutellaria baicalensis and rhizomes of Copti... |
PMC6510378 | core_pubmed_pmc | Safety, Pharmacokinetics, and Pharmacodynamics of ASP3662, a Novel 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor, in Healthy Young and Elderly Subjects | Safety, Pharmacokinetics, and Pharmacodynamics of ASP3662, a Novel 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor, in Healthy Young and Elderly Subjects Abstract Abstract Inhibition of the enzyme 11 β ‐hydroxysteroid dehydrogenase type 1 (11β‐HSD1) represents a potential mechanism for improving pain conditions. ASP3... |
PMC4598212 | core_pubmed_pmc | Micellar emulsions composed of mPEG-PCL/MCT as novel nanocarriers for systemic delivery of genistein: a comparative study with micelles | Micellar emulsions composed of mPEG-PCL/MCT as novel nanocarriers for systemic delivery of genistein: a comparative study with micelles Abstract Abstract Polymeric micelles receive considerable attention as drug delivery vehicles, depending on the versatility in drug solubilization and targeting therapy. However, their... |
PMC6681065 | core_pubmed_pmc | CK‐2127107 amplifies skeletal muscle response to nerve activation in humans | CK‐2127107 amplifies skeletal muscle response to nerve activation in humans Abstract ABSTRACT Introduction Three studies evaluated safety, tolerability, pharmacokinetics, and pharmacodynamics of CK‐2127107 (CK‐107), a next‐generation fast skeletal muscle troponin activator (FSTA), in healthy participants. We tested the... |
PMC4839326 | core_pubmed_pmc | Characterization of the first-in-class T-cell-engaging bispecific single-chain antibody for targeted immunotherapy of solid tumors expressing the oncofetal protein claudin 6 | Characterization of the first-in-class T-cell-engaging bispecific single-chain antibody for targeted immunotherapy of solid tumors expressing the oncofetal protein claudin 6 Abstract abstract The fetal tight junction molecule claudin 6 (CLDN6) is virtually absent from any normal tissue, whereas it is aberrantly and fre... |
PMC9228468 | core_pubmed_pmc | Relevance of Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors in Routine Clinical Practice: A Pilot Study | Relevance of Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors in Routine Clinical Practice: A Pilot Study Abstract Abstract Introduction: The main goal of treatment in cancer patients is to achieve the highest therapeutic effectiveness with the least iatrogenic toxicity. Tyrosine kinase inhibitors (TKIs) are a... |
PMC8940756 | core_pubmed_pmc | A longitudinal model for the Mayo Clinical Score and its sub-components in patients with ulcerative colitis | A longitudinal model for the Mayo Clinical Score and its sub-components in patients with ulcerative colitis Abstract Clinical trials in patients with ulcerative colitis (UC) face the challenge of high and variable placebo response rates. The Mayo Clinical Score (MCS) is used widely as the primary endpoint in clinical t... |
PMC3760445 | core_pubmed_pmc | ABCB1 haplotypes do not influence transport or efficacy of tyrosine kinase inhibitors in vitro | ABCB1 haplotypes do not influence transport or efficacy of tyrosine kinase inhibitors in vitro Abstract Single-nucleotide polymorphisms (SNPs) in the gene coding for the efflux-transport protein ABCB1 (P-glycoprotein) are commonly inherited as haplotypes. ABCB1 SNPs and haplotypes have been suggested to influence the p... |
PMC6023238 | core_pubmed_pmc | Randomized, placebo controlled phase I trial of safety, pharmacokinetics, pharmacodynamics and acceptability of tenofovir and tenofovir plus levonorgestrel vaginal rings in women | Randomized, placebo controlled phase I trial of safety, pharmacokinetics, pharmacodynamics and acceptability of tenofovir and tenofovir plus levonorgestrel vaginal rings in women Abstract To prevent the global health burdens of human immunodeficiency virus [HIV] and unintended/mistimed pregnancies, we developed an intr... |
PMC10090862 | core_pubmed_pmc | Improving the predictive power of xenograft and syngeneic anti-tumour studies using mice humanised for pathways of drug metabolism | Improving the predictive power of xenograft and syngeneic anti-tumour studies using mice humanised for pathways of drug metabolism Abstract Drug development is an expensive and time-consuming process, with only a small fraction of drugs gaining regulatory approval from the often many thousands of candidates identified ... |
PMC6925736 | core_pubmed_pmc | Development of a HPLC-MS/MS Method to Determine the 13 Elements of Semen Cuscutae and Application to a Pharmacokinetic Study in Rats | Development of a HPLC-MS/MS Method to Determine the 13 Elements of Semen Cuscutae and Application to a Pharmacokinetic Study in Rats Abstract This study developed a method for simultaneous determination of 13 elements of Semen Cuscutae (quercitrin, quercetin, hyperoside, caffeic acid, chlorogenic acid, luteolin, apigen... |
PMC9230547 | core_pubmed_pmc | Model-Based Prediction of Acid Suppression and Proposal of a New Dosing Regimen of Fexuprazan in Humans | Model-Based Prediction of Acid Suppression and Proposal of a New Dosing Regimen of Fexuprazan in Humans Abstract Fexuprazan is a potassium-competitive acid blocker (P-CAB). The compounds in this newly developed drug family suppress intragastric acidity. As there are already other acid-suppressing drugs on the market, s... |
PMC8093170 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of High-Dose Piperacillin–Tazobactam in Obese Patients | Pharmacokinetics and Pharmacodynamics of High-Dose Piperacillin–Tazobactam in Obese Patients Abstract Background and Objective Standard piperacillin–tazobactam (P-T) dosing may be suboptimal in obesity, but high-dose regimens have not been studied. We prospectively evaluated the pharmacokinetics and pharmacodynamics of... |
PMC6952755 | core_pubmed_pmc | A Randomized Clinical Trial Evaluating the Efficacy of Colistin Loading Dose in Critically Ill Children | A Randomized Clinical Trial Evaluating the Efficacy of Colistin Loading Dose in Critically Ill Children Abstract Objective: Pharmacokinetic and clinical studies recommend applying loading dose of colistin for the treatment of severe infections in the critically ill adults. Pharmacokinetic studies of colistin in childre... |
PMC10314623 | core_pubmed_pmc | Phase 1 dose-escalation study of SEA-CD40: a non-fucosylated CD40 agonist, in advanced solid tumors and lymphomas | Phase 1 dose-escalation study of SEA-CD40: a non-fucosylated CD40 agonist, in advanced solid tumors and lymphomas Abstract Background SEA-CD40 is an investigational, non-fucosylated, humanized monoclonal IgG 1 antibody that activates CD40, an immune-activating tumor necrosis factor receptor superfamily member. SEA-CD40... |
PMC9231190 | core_pubmed_pmc | The Natural Alkaloid Tryptanthrin Induces Apoptosis-like Death in Leishmania spp. | The Natural Alkaloid Tryptanthrin Induces Apoptosis-like Death in Leishmania spp. Abstract Abstract Leishmaniasis is a vector-borne disease against which there are no approved vaccines, and the treatment is based on highly toxic drugs. The alkaloids consist of a chemical class of natural nitrogen-containing substances ... |
PMC7291522 | core_pubmed_pmc | Effects of concomitant use of prasugrel with edoxaban on bleeding time, pharmacodynamics, and pharmacokinetics of edoxaban in healthy elderly Japanese male subjects: a clinical pharmacology study | Effects of concomitant use of prasugrel with edoxaban on bleeding time, pharmacodynamics, and pharmacokinetics of edoxaban in healthy elderly Japanese male subjects: a clinical pharmacology study Abstract Background Dual therapy with a direct oral anticoagulant (DOAC) plus a P2Y 12 receptor inhibitor is recommended in ... |
PMC7266804 | core_pubmed_pmc | Physiologically Based Dissolution Testing in a Drug Development Process—a Case Study of a Successful Application in a Bioequivalence Study of Trazodone ER Formulations Under Fed Conditions | Physiologically Based Dissolution Testing in a Drug Development Process—a Case Study of a Successful Application in a Bioequivalence Study of Trazodone ER Formulations Under Fed Conditions Abstract Abstract Development of generic extended-release (ER) formulations is challenging. Especially under fed conditions, the ri... |
PMC9366561 | core_pubmed_pmc | Effectiveness, nephrotoxicity, and therapeutic drug monitoring of polymyxin B in nosocomial pneumonia among critically ill patients | Effectiveness, nephrotoxicity, and therapeutic drug monitoring of polymyxin B in nosocomial pneumonia among critically ill patients Abstract Abstract Objectives We aimed to assess the effectiveness and nephrotoxicity of polymyxin B in critically ill patients with nosocomial pneumonia and to evaluate the utility of its ... |
PMC4988406 | core_pubmed_pmc | Correlating drug–target kinetics and in vivo pharmacodynamics: long residence time inhibitors of the FabI enoyl-ACP reductase † †Electronic supplementary information (ESI) available: Derivation of PK/PD models. See DOI: 10.1039/c6sc01000h | Correlating drug–target kinetics and in vivo pharmacodynamics: long residence time inhibitors of the FabI enoyl-ACP reductase † †Electronic supplementary information (ESI) available: Derivation of PK/PD models. See DOI: 10.1039/c6sc01000h Abstract A mechanistic PK/PD model that enables predictions of in vivo drug activ... |
PMC11954114 | core_pubmed_pmc | Therapeutic role of fluconazole in immunocompetent patients with pulmonary cryptococcosis: A case report | Therapeutic role of fluconazole in immunocompetent patients with pulmonary cryptococcosis: A case report Abstract Abstract The present investigation examines the potential for customized treatment of pulmonary cryptococcosis using fluconazole in an immunocompetent individual. Therapeutic drug monitoring (TDM) was utili... |
PMC9369086 | core_pubmed_pmc | Alteration of the Nucleotide Excision Repair (NER) Pathway in Soft Tissue Sarcoma | Alteration of the Nucleotide Excision Repair (NER) Pathway in Soft Tissue Sarcoma Abstract Abstract Clinical responses to anticancer therapies in advanced soft tissue sarcoma (STS) are unluckily restricted to a small subgroup of patients. Much of the inter-individual variability in treatment efficacy is as result of po... |
PMC8842743 | core_pubmed_pmc | Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species | Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species Abstract Background: The development of beta-site amyloid-beta precursor protein cleaving enzyme (BACE) 1 inhibitors for the treatment of Alzheimer’s disease requires optimization ... |
PMC3485142 | core_pubmed_pmc | Comparison of Suprachoroidal Drug Delivery with Subconjunctival and Intravitreal Routes Using Noninvasive Fluorophotometry | Comparison of Suprachoroidal Drug Delivery with Subconjunctival and Intravitreal Routes Using Noninvasive Fluorophotometry Abstract Abstract Purpose To determine whether exposure of sodium fluorescein (NaF) to the choroid-retina region in the posterior segment of the eye is greater with suprachoroidal injection when co... |
PMC5522970 | core_pubmed_pmc | Population Pharmacokinetic Characteristics of Amikacin in Suspected Cases of Neonatal Sepsis in a Low-Resource African Setting: A Prospective Nonrandomized Single-Site Study | Population Pharmacokinetic Characteristics of Amikacin in Suspected Cases of Neonatal Sepsis in a Low-Resource African Setting: A Prospective Nonrandomized Single-Site Study Abstract Abstract Background Amikacin exhibits marked pharmacokinetic (PK) variability and is commonly used in combination with other drugs in the... |
PMC5627010 | core_pubmed_pmc | Pharmacodynamic Evaluation and PK/PD-Based Dose Prediction of Tulathromycin: A Potential New Indication for Streptococcus suis Infection | Pharmacodynamic Evaluation and PK/PD-Based Dose Prediction of Tulathromycin: A Potential New Indication for Streptococcus suis Infection Abstract Abstract Tulathromycin is the first member of the triamilide antimicrobial drugs that has been registered in more than 30 countries. The goal of this study is to provide a po... |
PMC8009239 | core_pubmed_pmc | Study protocol of a phase 1 clinical trial establishing the safety of intrapleural administration of liposomal curcumin: curcumin as a palliative treatment for malignant pleural effusion (IPAL-MPE) | Study protocol of a phase 1 clinical trial establishing the safety of intrapleural administration of liposomal curcumin: curcumin as a palliative treatment for malignant pleural effusion (IPAL-MPE) Abstract Abstract Introduction This is a phase 1, open-label, single-centre, uncontrolled, dose-escalation study to evalua... |
PMC12338083 | core_pubmed_pmc | First‐In‐Human, Randomized, Placebo‐Controlled, SAD and MAD Trial to Evaluate Safety, Tolerability, and PK/PD Modeling of Potravitug in Healthy Adults | First‐In‐Human, Randomized, Placebo‐Controlled, SAD and MAD Trial to Evaluate Safety, Tolerability, and PK/PD Modeling of Potravitug in Healthy Adults Abstract ABSTRACT BK polyomavirus (BKPyV) affects 10%–30% of kidney‐transplant recipients receiving immunosuppressive therapy, potentially leading to nephropathy, graft ... |
PMC5702902 | core_pubmed_pmc | Integration of Genome Scale Metabolic Networks and Gene Regulation of Metabolic Enzymes With Physiologically Based Pharmacokinetics | Integration of Genome Scale Metabolic Networks and Gene Regulation of Metabolic Enzymes With Physiologically Based Pharmacokinetics Abstract The scope of physiologically based pharmacokinetic (PBPK) modeling can be expanded by assimilation of the mechanistic models of intracellular processes from systems biology field.... |
PMC8763961 | core_pubmed_pmc | Model-Based Anticancer Effect of Botulinum Neurotoxin Type A1 on Syngeneic Melanoma Mice | Model-Based Anticancer Effect of Botulinum Neurotoxin Type A1 on Syngeneic Melanoma Mice Abstract Abstract In recent, Botulinum Neurotoxin A1 (BoNT/A1) has been suggested as a potential anticancer agent due to neuronal innervation in tumor cells. Although potential BoNT/A1’s mechanism of action for the tumor suppressio... |
PMC12290790 | core_pubmed_pmc | PET imaging of the serotonin 1A receptor in major depressive disorder: Hierarchical multivariate analysis of [ 11 C]WAY100635 overcomes outcome measure discrepancies | PET imaging of the serotonin 1A receptor in major depressive disorder: Hierarchical multivariate analysis of [ 11 C]WAY100635 overcomes outcome measure discrepancies Abstract Abstract The serotonin 1A receptor has been linked to both the pathophysiology of major depressive disorder (MDD) and the antidepressant action o... |
PMC9812893 | core_pubmed_pmc | Antibody–Drug Conjugate Sacituzumab Govitecan Drives Efficient Tissue Penetration and Rapid Intracellular Drug Release | Antibody–Drug Conjugate Sacituzumab Govitecan Drives Efficient Tissue Penetration and Rapid Intracellular Drug Release Abstract Abstract Antibody–drug conjugates (ADC) are a rapidly growing class of targeted cancer treatments, but the field has experienced significant challenges from their complex design. This study ex... |
PMC4492748 | core_pubmed_pmc | Pharmacokinetic study of metopimazine by oral route in children | Pharmacokinetic study of metopimazine by oral route in children Abstract Abstract Metopimazine (MPZ) is an antiemetic considered as a currently used drug. In France, it has become the leading antiemetic mediator due to its good tolerance, however, its pharmacokinetics has never previously been studied in children. MPZ ... |
PMC11585863 | core_pubmed_pmc | Pharmacokinetics of Siddha Antidiabetic Polyherbal Formulation Madhumega Chooranam in Healthy Volunteers | Pharmacokinetics of Siddha Antidiabetic Polyherbal Formulation Madhumega Chooranam in Healthy Volunteers Abstract Abstract Background Madhumega Chooranam (MMC), a traditional Siddha polyherbal formulation, is used for diabetes management. Understanding its pharmacokinetics is crucial for evaluating its efficacy and saf... |
PMC6906348 | core_pubmed_pmc | A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma | A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma Abstract Background: The objectives of this phase II study were to determine the clinical activity of the MET tyrosine kinase inhibitor capmatinib (INC280) in patients with MET-dysregu... |
PMC5673907 | core_pubmed_pmc | Oral Apolipoprotein A‐I Mimetic D‐4F Lowers HDL‐Inflammatory Index in High‐Risk Patients: A First‐in‐Human Multiple‐Dose, Randomized Controlled Trial | Oral Apolipoprotein A‐I Mimetic D‐4F Lowers HDL‐Inflammatory Index in High‐Risk Patients: A First‐in‐Human Multiple‐Dose, Randomized Controlled Trial Abstract Abstract A single dose of the apolipoprotein (apo)A‐I mimetic peptide D‐4F rendered high‐density lipoprotein (HDL) less inflammatory, motivating the first multip... |
PMC10108555 | core_pubmed_pmc | Preclinical evaluation of ISH0339, a tetravalent broadly neutralizing bispecific antibody against SARS-CoV-2 with long-term protection | Preclinical evaluation of ISH0339, a tetravalent broadly neutralizing bispecific antibody against SARS-CoV-2 with long-term protection Abstract Abstract Background: Ending the global COVID-19 pandemic requires efficacious therapies against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Nevertheless, the ... |
PMC4629098 | core_pubmed_pmc | Preclinical investigation of the pharmacokinetics, metabolism, and protein and red blood cell binding of DRDE-07: a prophylactic agent against sulphur mustard | Preclinical investigation of the pharmacokinetics, metabolism, and protein and red blood cell binding of DRDE-07: a prophylactic agent against sulphur mustard Abstract Abstract DRDE-07, a newly synthesized amifostine analog currently under clinical investigation in a phase I trial, is a potent antidote against sulfur m... |
PMC4604150 | core_pubmed_pmc | Improved Safety, Bioavailability and Pharmacokinetics of Zidovudine through Lactoferrin Nanoparticles during Oral Administration in Rats | Improved Safety, Bioavailability and Pharmacokinetics of Zidovudine through Lactoferrin Nanoparticles during Oral Administration in Rats Abstract Zidovudine (AZT) is one of the most referred antiretroviral drug. In spite of its higher bioavailability (50–75%) the most important reason of its cessation are bone marrow s... |
PMC3595641 | core_pubmed_pmc | Surface-Modified HK:siRNA Nanoplexes with Enhanced Pharmacokinetics and Tumor Growth Inhibition | Surface-Modified HK:siRNA Nanoplexes with Enhanced Pharmacokinetics and Tumor Growth Inhibition Abstract We characterized in this study the pharmacokinetics and antitumor efficacy of histidine-lysine (HK):siRNA nanoplexes modified with PEG and a cyclic RGD (cRGD) ligand targeting αvβ3 and αvβ5 integrins. With noninvasi... |
PMC9614802 | core_pubmed_pmc | Antibiotic stewardship for nurses: Using e-learning modules to bridge the education gap | Antibiotic stewardship for nurses: Using e-learning modules to bridge the education gap Abstract Abstract Objective: The Centers for Disease Control and Prevention has called for an interdisciplinary approach to antibiotic stewardship implementation that includes front-line nurses. The literature to date has identified... |
PMC12845265 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Digoxin in Adult and Pediatric Patients with Heart Failure | Physiologically Based Pharmacokinetic Modeling of Digoxin in Adult and Pediatric Patients with Heart Failure Abstract Background/Objectives : Digoxin is a cardiotonic agent with a narrow therapeutic window and a high risk of toxicity. The current clinical use is based on an empirically FDA-recommended regimen which has... |
PMC10084052 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Fudosteine in Healthy Chinese Volunteers Under Fasting and Fed Conditions: A 4‐Way Replicate Crossover Study | Pharmacokinetics and Bioequivalence of Fudosteine in Healthy Chinese Volunteers Under Fasting and Fed Conditions: A 4‐Way Replicate Crossover Study Abstract Abstract The bioequivalence of a generic fudosteine tablet vs a brand‐named fudosteine tablet under fasting and fed conditions was evaluated in this study. This ra... |
PMC8505283 | core_pubmed_pmc | Etomidate and its Analogs: A Review of Pharmacokinetics and Pharmacodynamics | Etomidate and its Analogs: A Review of Pharmacokinetics and Pharmacodynamics Abstract Abstract Etomidate is a hypnotic agent that is used for the induction of anesthesia. It produces its effect by acting as a positive allosteric modulator on the γ-aminobutyric acid type A receptor and thus enhancing the effect of the i... |
PMC8800899 | core_pubmed_pmc | A pharmacokinetics study of proposed bevacizumab biosimilar MYL-1402O vs EU-bevacizumab and US-bevacizumab | A pharmacokinetics study of proposed bevacizumab biosimilar MYL-1402O vs EU-bevacizumab and US-bevacizumab Abstract Purpose Bevacizumab is a recombinant humanized monoclonal antibody that inhibits vascular endothelial growth factor-specific angiogenesis in some cancers. MYL-1402O is a proposed bevacizumab biosimilar. M... |
PMC11983587 | core_pubmed_pmc | Preparation, quality evaluation and preliminary pharmacokinetic-pharmacodynamic studies of synephrine dry powder inhaler | Preparation, quality evaluation and preliminary pharmacokinetic-pharmacodynamic studies of synephrine dry powder inhaler Abstract Abstract Acute lung injury (ALI) is a lung disease characterized by pulmonary edema caused by an excessive inflammatory response within the lungs and disruption of the alveolar capillary bar... |
PMC9227536 | core_pubmed_pmc | Prediction of Pharmacokinetics of IDP-73152 in Humans Using Physiologically-Based Pharmacokinetics | Prediction of Pharmacokinetics of IDP-73152 in Humans Using Physiologically-Based Pharmacokinetics Abstract Abstract IDP-73152, a novel peptide deformylase inhibitor with an antibacterial effect against Gram-positive bacteria, is in phase I development. The objective of this study was to develop a physiologically-based... |
PMC12871250 | core_pubmed_pmc | Synchrony is a robust iEEG biomarker for antiseizure medication load in epileptic patients | Synchrony is a robust iEEG biomarker for antiseizure medication load in epileptic patients Abstract With new, minimally invasive continuous EEG and wearable monitoring systems for epilepsy nearing regulatory approval, there is a rush to determine how to make these devices most useful to patients. One application is to ... |
PMC9304170 | core_pubmed_pmc | Chloromethyl Glycosides as Versatile Synthons to Prepare Glycosyloxymethyl‐Prodrugs | Chloromethyl Glycosides as Versatile Synthons to Prepare Glycosyloxymethyl‐Prodrugs Abstract Abstract This work investigates the addition of monosaccharides to marketed drugs to improve their pharmacokinetic properties for oral absorption. To this end, a set of chloromethyl glycoside synthons were developed to prepare ... |
PMC6549574 | core_pubmed_pmc | Pharmacogenomic considerations for antiplatelet agents: the era of precision medicine in stroke prevention and neurointerventional practice | Pharmacogenomic considerations for antiplatelet agents: the era of precision medicine in stroke prevention and neurointerventional practice Abstract Abstract Antiplatelet drugs are widely utilized in the setting of primary stroke prevention, secondary stroke prevention, and neuroendovascular device-related stroke preve... |
PMC12030627 | core_pubmed_pmc | Radioiodinated Bicyclic RGD Peptide Derivatives for Enhanced Tumor Accumulation | Radioiodinated Bicyclic RGD Peptide Derivatives for Enhanced Tumor Accumulation Abstract Background/Objectives : Integrin α V β 3 plays a crucial role in tumor angiogenesis and cancer progression, making it a key target for radiolabeled probes used in imaging and therapy. A previously developed probe, [ 125 I]bcRGD, ex... |
PMC3332339 | core_pubmed_pmc | Switching from enoxaparin to dabigatran etexilate: pharmacokinetics, pharmacodynamics, and safety profile | Switching from enoxaparin to dabigatran etexilate: pharmacokinetics, pharmacodynamics, and safety profile Abstract Purpose Dabigatran etexilate is an oral, reversible, direct thrombin inhibitor licensed for the prevention of venous thromboembolism and stroke prevention in patients with atrial fibrillation. The aim of t... |
PMC8004468 | core_pubmed_pmc | Optimal empiric treatment for KPC-2-producing Klebsiella pneumoniae infections in critically ill patients with normal or decreased renal function using Monte Carlo simulation | Optimal empiric treatment for KPC-2-producing Klebsiella pneumoniae infections in critically ill patients with normal or decreased renal function using Monte Carlo simulation Abstract Abstract Background Limited clinical studies describe the pharmacodynamics of fosfomycin (FOS), tigecycline (TGC) and colistin methanesu... |
PMC10410440 | core_pubmed_pmc | Preclinical PK investigation of a novel IDO1/TDO dual inhibitor—SHR9146 in mouse plasma and tissues by LC-MS/MS | Preclinical PK investigation of a novel IDO1/TDO dual inhibitor—SHR9146 in mouse plasma and tissues by LC-MS/MS Abstract Abstract Purpose The aim of the present study was to establish a liquid chromatography–tandem mass spectrometry (LC-MS/MS) method for the determination of SHR9146, a novel IDO1/TDO dual inhibitor, in... |
PMC6763420 | core_pubmed_pmc | Isolation, analysis and in vitro assessment of CYP3A4 inhibition by methylxanthines extracted from Pu-erh and Bancha tea leaves | Isolation, analysis and in vitro assessment of CYP3A4 inhibition by methylxanthines extracted from Pu-erh and Bancha tea leaves Abstract Abstract Methylxanthines, purine alkaloids found in plants, are found in beverages (coffee, tea, cocoa) and foods (chocolate and other cocoa-containing foods) commonly consumed worldw... |
PMC7922031 | core_pubmed_pmc | Pharmacokinetics of the CYP3A4 and CYP2B6 Inducer Carbamazepine and Its Drug–Drug Interaction Potential: A Physiologically Based Pharmacokinetic Modeling Approach | Pharmacokinetics of the CYP3A4 and CYP2B6 Inducer Carbamazepine and Its Drug–Drug Interaction Potential: A Physiologically Based Pharmacokinetic Modeling Approach Abstract The anticonvulsant carbamazepine is frequently used in the long-term therapy of epilepsy and is a known substrate and inducer of cytochrome P450 (CY... |
PMC11280093 | core_pubmed_pmc | Liver Fibrosis Stages Affect Organic Cation Transporter 1/2 Activities in Hepatitis C Virus-Infected Patients | Liver Fibrosis Stages Affect Organic Cation Transporter 1/2 Activities in Hepatitis C Virus-Infected Patients Abstract Abstract This study aims to evaluate the impact of liver fibrosis stages of chronic infection with hepatitis C virus (HCV) on the in vivo activity of organic cation transporters (hepatic OCT1 and renal... |
PMC9898255 | core_pubmed_pmc | Yoghurt as a deglutition aid for oral medication: effects on famotidine powder dissolution rate and pharmacokinetics | Yoghurt as a deglutition aid for oral medication: effects on famotidine powder dissolution rate and pharmacokinetics Abstract Deglutition aid foods are used to help patients with dysphagia take oral medications. Yoghurt is occasionally used to help swallow medications; however, its influence on pharmacokinetics is poor... |
PMC12296807 | core_pubmed_pmc | Predictors of Plasma Levels of Direct Oral Anticoagulants Among Patients with Atrial Fibrillation in Need of Elective Cardiac Procedures | Predictors of Plasma Levels of Direct Oral Anticoagulants Among Patients with Atrial Fibrillation in Need of Elective Cardiac Procedures Abstract Background The withdrawal timing of direct oral anticoagulants (DOACs) among patients in need of elective invasive surgery is based on DOAC pharmacokinetics in order to perfo... |
PMC7271501 | core_pubmed_pmc | Comparative evaluation of efficacy, pharmacodynamics, and safety of Hetero’s adalimumab (Mabura®, Hetero Biopharma Ltd.) and reference adalimumab (Humira®, Abbvie Inc.) in patients with active rheumatoid arthritis on concomitant methotrexate therapy | Comparative evaluation of efficacy, pharmacodynamics, and safety of Hetero’s adalimumab (Mabura®, Hetero Biopharma Ltd.) and reference adalimumab (Humira®, Abbvie Inc.) in patients with active rheumatoid arthritis on concomitant methotrexate therapy Abstract Background Our study aimed to compare efficacy and safety of ... |
PMC10836110 | core_pubmed_pmc | Comparable Efficacy of Oral Bendamustine versus Intravenous Administration in Treating Hematologic Malignancies | Comparable Efficacy of Oral Bendamustine versus Intravenous Administration in Treating Hematologic Malignancies Abstract Purpose: The purpose of this study was to analyze potential differences in antitumor efficacy and pharmacokinetics between intravenous (IV) bendamustine (BEN) and a novel orally administered bendamus... |
PMC8971958 | core_pubmed_pmc | Pharmacodynamic Thresholds for Beta-Lactam Antibiotics: A Story of Mouse Versus Man | Pharmacodynamic Thresholds for Beta-Lactam Antibiotics: A Story of Mouse Versus Man Abstract Abstract Beta-lactams remain a critical member of our antibiotic armamentarium and are among the most commonly prescribed antibiotic classes in the inpatient setting. For these agents, the percentage of time that the free conce... |
PMC6044135 | core_pubmed_pmc | Pharmacokinetics and bioavailability of chromium malate and its influence on trace metals absorption after oral or intravenous administration | Pharmacokinetics and bioavailability of chromium malate and its influence on trace metals absorption after oral or intravenous administration Abstract Abstract OBJECTIVES: In our preliminary study, chromium malate could decrease the blood glucose level in mice with diabetes and exhibits good benefits in treating glycom... |
PMC8663981 | core_pubmed_pmc | Drug-drug interactions in polypharmacy patients: The impact of renal impairment | Drug-drug interactions in polypharmacy patients: The impact of renal impairment Abstract Chronic kidney disease (CKD) is a long-term condition characterized by a gradual loss of kidney functions, usually accompanied by other comorbidities including cardiovascular diseases (hypertension, heart failure and stroke) and di... |
PMC8713164 | core_pubmed_pmc | Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II | Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II Abstract Abstract Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a plethora of target proteins. In this function, TNKS1/2 also impact the WNT/β-catenin and Hippo signaling pathways that are involved... |
PMC3848746 | core_pubmed_pmc | Ceftolozane/tazobactam: a novel antipseudomonal cephalosporin and β-lactamase-inhibitor combination | Ceftolozane/tazobactam: a novel antipseudomonal cephalosporin and β-lactamase-inhibitor combination Abstract Abstract The management of infections caused by multidrug-resistant Gram-negative bacteria, particularly Pseudomonas aeruginosa , continues to be a significant challenge to clinicians. Ceftolozane/tazobactam is ... |
PMC10816067 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Analysis of the Oxacephem Antibiotic Flomoxef against Extended-Spectrum β-Lactamase-Producing Enterobacterales from Dogs | Pharmacokinetic and Pharmacodynamic Analysis of the Oxacephem Antibiotic Flomoxef against Extended-Spectrum β-Lactamase-Producing Enterobacterales from Dogs Abstract Abstract Flomoxef (FMX) may be a potential alternative to carbapenems for dogs infected with Enterobacterales-producing extended-spectrum β-lactamase (ESB... |
PMC9864769 | core_pubmed_pmc | Identification of Lignan Compounds as New 6-Phosphogluconate Dehydrogenase Inhibitors for Lung Cancer | Identification of Lignan Compounds as New 6-Phosphogluconate Dehydrogenase Inhibitors for Lung Cancer Abstract Abstract Targeting pentose phosphate pathway (PPP) enzymes has emerged as a promising strategy to combat cancer. 6-Phosphogluconate dehydrogenase (6-PGD), the third critical enzyme of the PPP, catalyzes oxidat... |
PMC12338864 | core_pubmed_pmc | Modifications in FLAP 's second cytosolic loop influence 5‐ LOX interaction, inhibitor binding, and leukotriene formation | Modifications in FLAP 's second cytosolic loop influence 5‐ LOX interaction, inhibitor binding, and leukotriene formation Abstract Leukotrienes, synthesized via the 5‐lipoxygenase (5‐LOX) pathway in the arachidonic acid cascade, are critical in inflammation. Effective leukotriene production requires interaction between... |
PMC5215074 | core_pubmed_pmc | Impact of the mode of protraction of basal insulin therapies on their pharmacokinetic and pharmacodynamic properties and resulting clinical outcomes | Impact of the mode of protraction of basal insulin therapies on their pharmacokinetic and pharmacodynamic properties and resulting clinical outcomes Abstract Manufacturers of insulin products for diabetes therapy have long sought ways to modify the absorption rate of exogenously administered insulins in an effort to be... |
PMC11876733 | core_pubmed_pmc | Safety, Dosimetry, and Feasibility of [ 68 Ga]Ga-PSMA-R2 as an Imaging Agent in Patients with Biochemical Recurrence or Metastatic Prostate Cancer | Safety, Dosimetry, and Feasibility of [ 68 Ga]Ga-PSMA-R2 as an Imaging Agent in Patients with Biochemical Recurrence or Metastatic Prostate Cancer Abstract Prostate-specific membrane antigen (PSMA) is highly expressed in most prostate cancers (PCs). PET and CT imaging studies using 68 Ga-labeled PSMA ligands demonstrat... |
PMC9163677 | core_pubmed_pmc | Safety, Pharmacokinetics/Pharmacodynamics, and Absolute Bioavailability of Dexmedetomidine Hydrochloride Nasal Spray in Healthy Subjects: A Randomized, Parallel, Escalating Dose Study | Safety, Pharmacokinetics/Pharmacodynamics, and Absolute Bioavailability of Dexmedetomidine Hydrochloride Nasal Spray in Healthy Subjects: A Randomized, Parallel, Escalating Dose Study Abstract Abstract Background: The present study evaluated the safety, pharmacokinetics/pharmacodynamics (PK/PD), and absolute bioavailab... |
PMC4260119 | core_pubmed_pmc | Single- and Multiple-Dose Pharmacokinetics and Absolute Bioavailability of Tedizolid | Single- and Multiple-Dose Pharmacokinetics and Absolute Bioavailability of Tedizolid Abstract Abstract Objectives Tedizolid phosphate is a novel antibacterial under investigation for the treatment of gram-positive infections. This study was conducted to assess the pharmacokinetics, safety, and tolerability of intraveno... |
PMC6587716 | core_pubmed_pmc | Omadacycline Enters the Ring: A New Antimicrobial Contender | Omadacycline Enters the Ring: A New Antimicrobial Contender Abstract Omadacycline is a novel aminomethylcycline approved for the treatment of community‐acquired bacterial pneumonia and acute bacterial skin and skin structure infections. This article reviews existing data pertaining to the biochemistry, mechanism of act... |
PMC9123937 | core_pubmed_pmc | The Effects of a Novel Curcumin Derivative Loaded Long-Circulating Solid Lipid Nanoparticle on the MHCC-97H Liver Cancer Cells and Pharmacokinetic Behavior | The Effects of a Novel Curcumin Derivative Loaded Long-Circulating Solid Lipid Nanoparticle on the MHCC-97H Liver Cancer Cells and Pharmacokinetic Behavior Abstract Abstract Purpose The objective of this study was to develop long-circulating solid lipid nanoparticles (LSLN) containing a novel curcumin (CU) derivative (... |
PMC7818513 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Oral Venglustat in Healthy Volunteers | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Oral Venglustat in Healthy Volunteers Abstract Abstract Venglustat is a small‐molecule glucosylceramide synthase (GCS) inhibitor designed to reduce the production of glucosylceramide (GL‐1) and thus is expected to substantially reduce formation of glucosyl... |
PMC3994916 | core_pubmed_pmc | Effect of Administration Route on the Pharmacokinetics of Cobalamin in Elderly Patients: A Randomized Controlled Trial | Effect of Administration Route on the Pharmacokinetics of Cobalamin in Elderly Patients: A Randomized Controlled Trial Abstract Abstract Background The gold standard for cobalamin deficiency treatment is administration of cobalamin by intramuscular injection. The injection is painful and inconvenient, particularly for ... |
PMC4692299 | core_pubmed_pmc | Fidaxomicin: A novel agent for the treatment of Clostridium difficile infection | Fidaxomicin: A novel agent for the treatment of Clostridium difficile infection Abstract Oral vancomycin and oral metronidazole have several limitations with regard to their use in the treatment of Clostridium difficile infections (CDIs); however, oral vancomycin has been considered the gold standard in clinical trials... |
PMC5039492 | core_pubmed_pmc | Odanacatib, a Cathepsin K Cysteine Protease Inhibitor, Kills Hookworm In Vivo | Odanacatib, a Cathepsin K Cysteine Protease Inhibitor, Kills Hookworm In Vivo Abstract Hookworm infection is chief among soil-transmitted helminthiases (STHs) for the chronic morbidly inflicted. Deworming via mass drug administration (MDA) programs most often employs single doses of benzimidazole drugs to which resista... |
PMC5608907 | core_pubmed_pmc | Split dosing of artemisinins does not improve antimalarial therapeutic efficacy | Split dosing of artemisinins does not improve antimalarial therapeutic efficacy Abstract Abstract It has been suggested recently, based on pharmacokinetic-pharmacodynamic modelling exercises, that twice daily dosing of artemisinins increases malaria parasite killing and so could “dramatically enhance and restore drug e... |
PMC5379148 | core_pubmed_pmc | A phase I study of intravenous and oral rucaparib in combination with chemotherapy in patients with advanced solid tumours | A phase I study of intravenous and oral rucaparib in combination with chemotherapy in patients with advanced solid tumours Abstract Abstract Background: This study evaluated safety, pharmacokinetics, and clinical activity of intravenous and oral rucaparib, a poly(ADP-ribose) polymerase inhibitor, combined with chemothe... |
PMC9281365 | core_pubmed_pmc | Prophylactic evaluation of verubecestat on disease‐ and symptom‐modifying effects in 5XFAD mice | Prophylactic evaluation of verubecestat on disease‐ and symptom‐modifying effects in 5XFAD mice Abstract Abstract Introduction Alzheimer's disease (AD) is the most common form of dementia. Beta‐secretase (BACE) inhibitors have been proposed as potential therapeutic interventions; however, initiating treatment once dise... |
PMC9234538 | core_pubmed_pmc | High value of 64 Cu as a tool to evaluate the restoration of physiological copper excretion after gene therapy in Wilson’s disease | High value of 64 Cu as a tool to evaluate the restoration of physiological copper excretion after gene therapy in Wilson’s disease Abstract Abstract Wilson’s disease (WD) is an inherited disorder of copper metabolism associated with mutations in ATP7B gene. We have shown that the administration of an adeno-associated v... |
PMC6154603 | core_pubmed_pmc | Study on the Rationality for Antiviral Activity of Flos Lonicerae Japonicae -Fructus Forsythiae Herb Couple Preparations Improved by Chito-Oligosaccharide via Integral Pharmacokinetics | Study on the Rationality for Antiviral Activity of Flos Lonicerae Japonicae -Fructus Forsythiae Herb Couple Preparations Improved by Chito-Oligosaccharide via Integral Pharmacokinetics Abstract Abstract In the present study, the rationality for the antiviral effect (H1N1 virus) of Flos Lonicerae Japonicae (FLJ, named J... |
PMC9540503 | core_pubmed_pmc | Quantitative Proteomics of Hepatic Drug‐Metabolizing Enzymes and Transporters in Patients With Colorectal Cancer Metastasis | Quantitative Proteomics of Hepatic Drug‐Metabolizing Enzymes and Transporters in Patients With Colorectal Cancer Metastasis Abstract Abstract The impact of liver cancer metastasis on protein abundance of 22 drug‐metabolizing enzymes (DMEs) and 25 transporters was investigated using liquid chromatography‐tandem accurate... |
PMC7164646 | core_pubmed_pmc | Toward precision prescribing for methadone: Determinants of methadone deposition | Toward precision prescribing for methadone: Determinants of methadone deposition Abstract Abstract Background Despite the World Health Organization listing methadone as an essential medication, effective dose selection is challenging, especially in racial and ethnic minority populations. Subtherapeutic doses can result... |
PMC12307536 | core_pubmed_pmc | Relugolix in Combination with Androgen Receptor Pathway Inhibitors in the Treatment of Metastatic Prostate Cancer: A Clinical Perspective | Relugolix in Combination with Androgen Receptor Pathway Inhibitors in the Treatment of Metastatic Prostate Cancer: A Clinical Perspective Abstract Abstract Relugolix, an oral gonadotropin-releasing hormone (GnRH) receptor antagonist, has been established as an effective androgen deprivation therapy (ADT) for advanced p... |
PMC3687236 | core_pubmed_pmc | Formulation and evaluation of buccal film of Ivabradine hydrochloride for the treatment of stable angina pectoris | Formulation and evaluation of buccal film of Ivabradine hydrochloride for the treatment of stable angina pectoris Abstract Background: Ivabradine hydrochloride is an anti-anginal drug with a biological half-life of about 2 h, and repeated daily administration is needed to maintain effective plasma level. Present invest... |
PMC6223696 | core_pubmed_pmc | Gabapentin and Pregabalin and Risk of Atrial Fibrillation in the Elderly: A Population-Based Cohort Study in an Electronic Prescription Database | Gabapentin and Pregabalin and Risk of Atrial Fibrillation in the Elderly: A Population-Based Cohort Study in an Electronic Prescription Database Abstract Abstract Introduction Gabapentin and pregabalin are widely prescribed to elderly people, but data on their pharmacokinetics, safety, and efficacy in this population a... |
PMC5292974 | core_pubmed_pmc | MOD-4023, a long-acting carboxy-terminal peptide-modified human growth hormone: results of a Phase 2 study in growth hormone-deficient adults | MOD-4023, a long-acting carboxy-terminal peptide-modified human growth hormone: results of a Phase 2 study in growth hormone-deficient adults Abstract Objective Growth hormone (GH) replacement therapy currently requires daily injections, which may cause distress and low compliance. C-terminal peptide (CTP)-modified gro... |
PMC12819607 | core_pubmed_pmc | Mitochondrial dysfunction and apoptotic signaling induced by the combined action of 2-aminoethyl dihydrogen phosphate and methyl-β-cyclodextrin in melanoma cells | Mitochondrial dysfunction and apoptotic signaling induced by the combined action of 2-aminoethyl dihydrogen phosphate and methyl-β-cyclodextrin in melanoma cells Abstract Abstract Melanoma cells exhibit remarkable metabolic adaptability, sustained by lipid enrichment and mitochondrial resilience that enable survival un... |
PMC9959744 | core_pubmed_pmc | Identification of and Mechanistic Insights into SARS-CoV-2 Main Protease Non-Covalent Inhibitors: An In-Silico Study | Identification of and Mechanistic Insights into SARS-CoV-2 Main Protease Non-Covalent Inhibitors: An In-Silico Study Abstract Abstract The indispensable role of the SARS-CoV-2 main protease (Mpro) in the viral replication cycle and its dissimilarity to human proteases make Mpro a promising drug target. In order to iden... |
PMC11439918 | core_pubmed_pmc | Impact of oil type on the development and oral bioavailability of self-nanoemulsifying drug delivery systems containing simvastatin | Impact of oil type on the development and oral bioavailability of self-nanoemulsifying drug delivery systems containing simvastatin Abstract The aim of this work is to develop and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) containing simvastatin to increase its oral bioavailability. Formulation EO 5 (... |
PMC8808992 | core_pubmed_pmc | Randomized double-blind clinical trial comparing safety and efficacy of the biosimilar BCD-021 with reference bevacizumab | Randomized double-blind clinical trial comparing safety and efficacy of the biosimilar BCD-021 with reference bevacizumab Abstract Abstract Background BCD-021 is a bevacizumab biosimilar which was shown to be equivalent to reference bevacizumab in a wide panel of physicochemical studies as well as preclinical studies i... |
PMC8053373 | core_pubmed_pmc | Clinically Significant Drug Interactions Between Psychotropic Agents and Repurposed COVID-19 Therapies | Clinically Significant Drug Interactions Between Psychotropic Agents and Repurposed COVID-19 Therapies Abstract Abstract As many patients with underlying psychiatric disorders may be infected with COVID-19, and COVID-19-affected subjects may frequently experience a new onset of psychiatric manifestations, concomitant u... |
PMC4124053 | core_pubmed_pmc | Apoptosis and the FLIP and NF-kappa B proteins as pharmacodynamic criteria for biosimilar TNF-alpha antagonists | Apoptosis and the FLIP and NF-kappa B proteins as pharmacodynamic criteria for biosimilar TNF-alpha antagonists Abstract Abstract Various criteria are necessary to assess the efficacy and safety of biological medications in order to grant companies the right to register these medications with the appropriate bodies tha... |
PMC11660682 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic analysis of sulbactam against Acinetobacter baumannii pneumonia: establishing in vivo efficacy targets in the epithelial lining fluid | Pharmacokinetic/pharmacodynamic analysis of sulbactam against Acinetobacter baumannii pneumonia: establishing in vivo efficacy targets in the epithelial lining fluid Abstract Abstract Background Sulbactam is an effective therapy for Acinetobacter baumannii infections. Previous sulbactam pharmacokinetics/pharmacodynamic... |
PMC7996486 | core_pubmed_pmc | What Is the Best Predictor of Phenobarbital Pharmacokinetics to Use for Initial Dosing in Neonates? | What Is the Best Predictor of Phenobarbital Pharmacokinetics to Use for Initial Dosing in Neonates? Abstract Abstract Phenobarbital is a first-line treatment of various seizure types in newborns. Dosage individualization maximizing the proportion of patients with drug levels in therapeutic range or sufficient treatment... |
PMC4931879 | core_pubmed_pmc | Robust Translation of γ -Secretase Modulator Pharmacology across Preclinical Species and Human Subjects | Robust Translation of γ -Secretase Modulator Pharmacology across Preclinical Species and Human Subjects Abstract Abstract The amyloid- β peptide (A β )—in particular, the 42–amino acid form, A β 1-42—is thought to play a key role in the pathogenesis of Alzheimer’s disease (AD). Thus, several therapeutic modalities aimi... |
PMC12896375 | core_pubmed_pmc | A Generalized Minimal PBPK ‐ PD Model of Bispecific Antibodies: Case Studies and Applications in Drug Development | A Generalized Minimal PBPK ‐ PD Model of Bispecific Antibodies: Case Studies and Applications in Drug Development Abstract ABSTRACT Bispecific antibodies (bsAbs), for which each arm binds a distinct molecular target, are developed to engage soluble and cell surface targets in different therapeutic indications. Three ke... |
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