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PMC9310021 | core_pubmed_pmc | Pharmacodynamic Target Assessment and PK/PD Cutoff Determination for Gamithromycin Against Streptococcus suis in Piglets | Pharmacodynamic Target Assessment and PK/PD Cutoff Determination for Gamithromycin Against Streptococcus suis in Piglets Abstract Abstract Gamithromycin is a long-acting azalide antibiotic that has been developed recently for the treatment of swine respiratory diseases. In this study, the pharmacokinetic/pharmacodynami... |
PMC5469595 | core_pubmed_pmc | Phase I Dose‐Escalation Study of Ramucirumab in Chinese Patients with Advanced Solid Tumors | Phase I Dose‐Escalation Study of Ramucirumab in Chinese Patients with Advanced Solid Tumors Abstract Abstract Lessons Learned. Ramucirumab was well tolerated in Chinese patients with advanced solid tumors, and adverse events were manageable in this study. Pharmacokinetics characteristics in Chinese patients were simila... |
PMC12256174 | core_pubmed_pmc | Next-Generation Oral Delivery Systems: Phytosomal Hinokitiol Tablets via REGEMAT 3D Bioprinter-Based 3D Printing for Enhanced Bioavailability | Next-Generation Oral Delivery Systems: Phytosomal Hinokitiol Tablets via REGEMAT 3D Bioprinter-Based 3D Printing for Enhanced Bioavailability Abstract Abstract The administration of hinokitiol, a natural bioactive compound with promising therapeutic potential, particularly against breast cancer, faces notable challenge... |
PMC9952184 | core_pubmed_pmc | Implementing Vancomycin Population Pharmacokinetic Models: An App for Individualized Antibiotic Therapy in Critically Ill Patients | Implementing Vancomycin Population Pharmacokinetic Models: An App for Individualized Antibiotic Therapy in Critically Ill Patients Abstract In individualized therapy, the Bayesian approach integrated with population pharmacokinetic models (PopPK) for predictions together with therapeutic drug monitoring (TDM) to mainta... |
PMC4574835 | core_pubmed_pmc | Population pharmacokinetics of dolutegravir in HIV-infected treatment-naive patients | Population pharmacokinetics of dolutegravir in HIV-infected treatment-naive patients Abstract Abstract Aim Dolutegravir is the newest integrase inhibitor approved for HIV treatment and has demonstrated potent antiviral activity in patient populations with a broad range of treatment experience. This analysis aimed to ch... |
PMC11846486 | core_pubmed_pmc | Population Pharmacokinetics-Based Evaluation of Ceftazidime-Avibactam Dosing Regimens in Critically and Non-Critically Ill Patients With Carbapenem-Resistant Klebsiella pneumoniae | Population Pharmacokinetics-Based Evaluation of Ceftazidime-Avibactam Dosing Regimens in Critically and Non-Critically Ill Patients With Carbapenem-Resistant Klebsiella pneumoniae Abstract Abstract Purpose This study aimed to describe the population pharmacokinetics (PopPK) of ceftazidime-avibactam (CAZ-AVI) in adult p... |
PMC8018285 | core_pubmed_pmc | New Human Follitropin Preparations: How Glycan Structural Differences May Affect Biochemical and Biological Function and Clinical Effect | New Human Follitropin Preparations: How Glycan Structural Differences May Affect Biochemical and Biological Function and Clinical Effect Abstract It is well accepted that pituitary follitropin is secreted into the circulation as a mixture of variants, which differ not in primary structure but rather at the level of gly... |
PMC7033524 | core_pubmed_pmc | Pharmacokinetics of TKM-130803 in Sierra Leonean patients with Ebola virus disease: plasma concentrations exceed target levels, with drug accumulation in the most severe patients | Pharmacokinetics of TKM-130803 in Sierra Leonean patients with Ebola virus disease: plasma concentrations exceed target levels, with drug accumulation in the most severe patients Abstract Abstract Background TKM-130803 is a specific anti-EBOV therapeutic comprised of two small interfering RNAs (siRNA) siLpol-2 and siVP... |
PMC5340825 | core_pubmed_pmc | A Two-Period Open-Label, Single-Dose Crossover Study in Healthy Volunteers to Evaluate the Drug–Drug Interaction Between Cimetidine and Inhaled Extrafine CHF 5993 | A Two-Period Open-Label, Single-Dose Crossover Study in Healthy Volunteers to Evaluate the Drug–Drug Interaction Between Cimetidine and Inhaled Extrafine CHF 5993 Abstract Abstract Background and Objectives CHF 5993 is an extrafine ‘triple therapy’ combination of the long-acting muscarinic antagonist glycopyrronium bro... |
PMC12298552 | core_pubmed_pmc | Prediction of Monoclonal Antibody Pharmacokinetics in Pediatric Populations Using PBPK Modeling and Simulation | Prediction of Monoclonal Antibody Pharmacokinetics in Pediatric Populations Using PBPK Modeling and Simulation Abstract Abstract Background : Accurately determining pediatric dosing is essential prior to initiating clinical trials or administering medications in routine clinical settings. In children, ethical considera... |
PMC10140984 | core_pubmed_pmc | Neonatal Pharmacokinetics and Biodistribution of Polymeric Nanoparticles and Effect of Surfactant | Neonatal Pharmacokinetics and Biodistribution of Polymeric Nanoparticles and Effect of Surfactant Abstract Abstract The development of therapeutics for pediatric use has advanced in the last few decades, yet the off-label use of adult medications in pediatrics remains a significant clinical problem. Nano-based medicine... |
PMC9021973 | core_pubmed_pmc | Safety, Pharmacokinetics and Pharmacodynamics of Spectrum Yellow Oil in Healthy Participants | Safety, Pharmacokinetics and Pharmacodynamics of Spectrum Yellow Oil in Healthy Participants Abstract Abstract Due to a lack of published pharmacokinetic (PK) and/or pharmacodynamic (PD) data, decision-making surrounding appropriate dosing of cannabis used for medical purposes is limited. This multiple-dose study evalu... |
PMC7078782 | core_pubmed_pmc | Simultaneous Determination of Parecoxib and Its Metabolite Valdecoxib Concentrations in Beagle Plasma by UPLC-MS/MS and Application for Pharmacokinetics Study | Simultaneous Determination of Parecoxib and Its Metabolite Valdecoxib Concentrations in Beagle Plasma by UPLC-MS/MS and Application for Pharmacokinetics Study Abstract Abstract A method for the simultaneous determination of parecoxib and its metabolite valdecoxib in beagle plasma by UPLC-MS/MS was developed and validat... |
PMC10536666 | core_pubmed_pmc | New Antimicrobials for Gram-Positive Sustained Infections: A Comprehensive Guide for Clinicians | New Antimicrobials for Gram-Positive Sustained Infections: A Comprehensive Guide for Clinicians Abstract Antibiotic resistance is a public health problem with increasingly alarming data being reported. Gram-positive bacteria are among the protagonists of severe nosocomial and community infections. The objective of this... |
PMC6549717 | core_pubmed_pmc | Pharmacokinetics, safety, and efficacy of tapentadol oral solution for treating moderate to severe pain in pediatric patients | Pharmacokinetics, safety, and efficacy of tapentadol oral solution for treating moderate to severe pain in pediatric patients Abstract Abstract Background: This trial is part of the global pediatric clinical development program investigating the administration of the strong analgesic tapentadol in children and adolesce... |
PMC12964675 | core_pubmed_pmc | Design, synthesis, and biological profiling of fluorinated cannabidiol and cannabigerol derivatives as promising therapeutic agents | Design, synthesis, and biological profiling of fluorinated cannabidiol and cannabigerol derivatives as promising therapeutic agents Abstract Background Cannabidiol (CBD) and cannabigerol (CBG) are non-psychotropic phytocannabinoids that have significant, broad-spectrum therapeutic potential in a variety of pharmacologi... |
PMC8674000 | core_pubmed_pmc | Unraveling pleiotropic effects of rifampicin by using physiologically based pharmacokinetic modeling: Assessing the induction magnitude of P‐glycoprotein–cytochrome P450 3A4 dual substrates | Unraveling pleiotropic effects of rifampicin by using physiologically based pharmacokinetic modeling: Assessing the induction magnitude of P‐glycoprotein–cytochrome P450 3A4 dual substrates Abstract Abstract Rifampicin induces both P‐glycoprotein (P‐gp) and cytochrome P450 3A4 (CYP3A4) through regulating common nuclear... |
PMC8422304 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of investigational regimens’ drugs in the TB-PRACTECAL clinical trial (the PRACTECAL-PKPD study): a prospective nested study protocol in a randomised controlled trial | Population pharmacokinetics and pharmacodynamics of investigational regimens’ drugs in the TB-PRACTECAL clinical trial (the PRACTECAL-PKPD study): a prospective nested study protocol in a randomised controlled trial Abstract Introduction Drug-resistant tuberculosis (TB) remains a global health threat, with little over ... |
PMC5808039 | core_pubmed_pmc | Phase I open-label study of afatinib plus vinorelbine in patients with solid tumours overexpressing EGFR and/or HER2 | Phase I open-label study of afatinib plus vinorelbine in patients with solid tumours overexpressing EGFR and/or HER2 Abstract Abstract Background: This phase Ib study evaluated afatinib plus vinorelbine in patients with advanced solid tumours overexpressing epidermal growth factor receptor (EGFR) and/or human EGFR 2 (H... |
PMC6524914 | core_pubmed_pmc | Choice of Renal Function Estimator Influences Adverse Outcomes with Dabigatran Etexilate in Patients with Atrial Fibrillation | Choice of Renal Function Estimator Influences Adverse Outcomes with Dabigatran Etexilate in Patients with Atrial Fibrillation Abstract Background Clinical significance of dosing dabigatran with different estimates of renal function for treatment of atrial fibrillation (AF) is unknown. Renal function is routinely estima... |
PMC7826463 | core_pubmed_pmc | Pamiparib dose escalation in Chinese patients with non‐mucinous high‐grade ovarian cancer or advanced triple‐negative breast cancer | Pamiparib dose escalation in Chinese patients with non‐mucinous high‐grade ovarian cancer or advanced triple‐negative breast cancer Abstract Abstract Background The recommended phase 2 dose (RP2D) of pamiparib, an investigational PARP1/2 inhibitor, was established as 60 mg twice daily (BID) in a first‐in‐human (FIH) st... |
PMC3355859 | core_pubmed_pmc | Preliminary Clinical and Pharmacologic Investigation of Photodynamic Therapy with the Silicon Phthalocyanine Photosensitizer Pc 4 for Primary or Metastatic Cutaneous Cancers | Preliminary Clinical and Pharmacologic Investigation of Photodynamic Therapy with the Silicon Phthalocyanine Photosensitizer Pc 4 for Primary or Metastatic Cutaneous Cancers Abstract Photodynamic therapy (PDT) for cutaneous malignancies has been found to be an effective treatment with a range of photosensitizers. The p... |
PMC7797177 | core_pubmed_pmc | Pharmacological basis for the potential role of Azithromycin and Doxycycline in management of COVID-19 | Pharmacological basis for the potential role of Azithromycin and Doxycycline in management of COVID-19 Abstract Abstract A novel corona virus SARS-CoV-2 has led to an outbreak of the highly infectious pandemic COVID-19 complicated viral pneumonia. Patients with risk factors frequently develop secondary infections where... |
PMC12959123 | core_pubmed_pmc | A genomics-informed mechanism-based pharmacokinetic/pharmacodynamic model of cefiderocol and ceftazidime/avibactam against carbapenem-resistant Achromobacter xylosoxidans | A genomics-informed mechanism-based pharmacokinetic/pharmacodynamic model of cefiderocol and ceftazidime/avibactam against carbapenem-resistant Achromobacter xylosoxidans Abstract ABSTRACT Achromobacter xylosoxidans harbors robust intrinsic and acquired resistance mechanisms and is responsible for severe nosocomial inf... |
PMC9730333 | core_pubmed_pmc | Eight pharmacokinetic genetic variants are not associated with the risk of bleeding from direct oral anticoagulants in non-valvular atrial fibrillation patients | Eight pharmacokinetic genetic variants are not associated with the risk of bleeding from direct oral anticoagulants in non-valvular atrial fibrillation patients Abstract Background: Atrial fibrillation (AF) is the leading cause of ischemic stroke and treatment has focused on reducing this risk through anticoagulation. ... |
PMC8026479 | core_pubmed_pmc | Trilaciclib dose selection: an integrated pharmacokinetic and pharmacodynamic analysis of preclinical data and Phase Ib/IIa studies in patients with extensive-stage small cell lung cancer | Trilaciclib dose selection: an integrated pharmacokinetic and pharmacodynamic analysis of preclinical data and Phase Ib/IIa studies in patients with extensive-stage small cell lung cancer Abstract Abstract Purpose Trilaciclib is a first-in-class CDK4/6 inhibitor that transiently arrests hematopoietic stem and progenito... |
PMC9623328 | core_pubmed_pmc | Multiple-dose up-titration study to evaluate the pharmacokinetics, safety and antitumor activity of apatinib in advanced gastric adenocarcinoma | Multiple-dose up-titration study to evaluate the pharmacokinetics, safety and antitumor activity of apatinib in advanced gastric adenocarcinoma Abstract Background and purpose The objective of this study was to investigate the pharmacokinetics, safety, and antitumor activity of apatinib, a vascular endothelial growth f... |
PMC4092878 | core_pubmed_pmc | In silico comparative characterization of pharmacogenomic missense variants | In silico comparative characterization of pharmacogenomic missense variants Abstract Abstract Background Missense pharmacogenomic (PGx) variants refer to amino acid substitutions that potentially affect the pharmacokinetic (PK) or pharmacodynamic (PD) response to drug therapies. The PGx variants, as compared to disease... |
PMC5446025 | core_pubmed_pmc | A multicentre randomised controlled trial to compare the pharmacokinetics, efficacy and safety of CT-P10 and innovator rituximab in patients with rheumatoid arthritis | A multicentre randomised controlled trial to compare the pharmacokinetics, efficacy and safety of CT-P10 and innovator rituximab in patients with rheumatoid arthritis Abstract Abstract Objective To demonstrate pharmacokinetic equivalence of CT-P10 and innovator rituximab (RTX) in patients with rheumatoid arthritis (RA)... |
PMC8555527 | core_pubmed_pmc | Nonclinical safety evaluation, pharmacokinetics, and target engagement of Lu AF82422, a monoclonal IgG1 antibody against alpha-synuclein in development for treatment of synucleinopathies | Nonclinical safety evaluation, pharmacokinetics, and target engagement of Lu AF82422, a monoclonal IgG1 antibody against alpha-synuclein in development for treatment of synucleinopathies Abstract ABSTRACT Alpha-synuclein is a 15 kDa protein associated with neurodegenerative diseases such as Parkinson disease and multip... |
PMC4710599 | core_pubmed_pmc | Impact of Exposure Uncertainty on the Association between Perfluorooctanoate and Preeclampsia in the C8 Health Project Population | Impact of Exposure Uncertainty on the Association between Perfluorooctanoate and Preeclampsia in the C8 Health Project Population Abstract Background Uncertainty in exposure estimates from models can result in exposure measurement error and can potentially affect the validity of epidemiological studies. We recently use... |
PMC4705890 | core_pubmed_pmc | Phase I trial of EpCAM-targeting immunotoxin MOC31PE, alone and in combination with cyclosporin | Phase I trial of EpCAM-targeting immunotoxin MOC31PE, alone and in combination with cyclosporin Abstract Abstract Background: A phase I trial was performed to determine the maximum tolerated dose (MTD), safety, pharmacokinetics and immunogenicity of the anti-EpCAM immunotoxin (IT) MOC31PE in cancer patients. An importa... |
PMC3949712 | core_pubmed_pmc | Phase I Study of GC1008 (Fresolimumab): A Human Anti-Transforming Growth Factor-Beta (TGFβ) Monoclonal Antibody in Patients with Advanced Malignant Melanoma or Renal Cell Carcinoma | Phase I Study of GC1008 (Fresolimumab): A Human Anti-Transforming Growth Factor-Beta (TGFβ) Monoclonal Antibody in Patients with Advanced Malignant Melanoma or Renal Cell Carcinoma Abstract Abstract Background In advanced cancers, transforming growth factor-beta (TGFβ) promotes tumor growth and metastases and suppresse... |
PMC6550132 | core_pubmed_pmc | Pharmacokinetic study of the oral fluorouracil antitumor agent S‐1 in patients with impaired renal function | Pharmacokinetic study of the oral fluorouracil antitumor agent S‐1 in patients with impaired renal function Abstract Abstract Although dose reduction of S‐1 is recommended for patients with impaired renal function, dose modification for such patients has not been prospectively evaluated. The aim of the present study wa... |
PMC5920042 | core_pubmed_pmc | KH176 Safeguards Mitochondrial Diseased Cells from Redox Stress-Induced Cell Death by Interacting with the Thioredoxin System/Peroxiredoxin Enzyme Machinery | KH176 Safeguards Mitochondrial Diseased Cells from Redox Stress-Induced Cell Death by Interacting with the Thioredoxin System/Peroxiredoxin Enzyme Machinery Abstract Abstract A deficient activity of one or more of the mitochondrial oxidative phosphorylation (OXPHOS) enzyme complexes leads to devastating diseases, with ... |
PMC5119957 | core_pubmed_pmc | A Phase 1 study of intravenous infusions of tigecycline in patients with acute myeloid leukemia | A Phase 1 study of intravenous infusions of tigecycline in patients with acute myeloid leukemia Abstract Abstract Acute myeloid leukemia ( AML ) cells meet the higher energy, metabolic, and signaling demands of the cell by increasing mitochondrial biogenesis and mitochondrial protein translation. Blocking mitochondrial... |
PMC8628143 | core_pubmed_pmc | SARS-CoV-2 Neutralization in Convalescent Plasma and Commercial Lots of Plasma-Derived Immunoglobulin | SARS-CoV-2 Neutralization in Convalescent Plasma and Commercial Lots of Plasma-Derived Immunoglobulin Abstract Introduction Patients with primary or secondary immunodeficiency (PID or SID) face increased insecurity and discomfort in the light of the COVID-19 pandemic, not knowing if and to what extent their comorbiditi... |
PMC8376139 | core_pubmed_pmc | Population pharmacokinetics of belantamab mafodotin, a BCMA‐targeting agent in patients with relapsed/refractory multiple myeloma | Population pharmacokinetics of belantamab mafodotin, a BCMA‐targeting agent in patients with relapsed/refractory multiple myeloma Abstract Abstract Belantamab mafodotin (belamaf) is an antibody–drug conjugate (ADC) targeting B‐cell maturation antigen (BCMA). Nonlinear mixed‐effects models were developed to characterize... |
PMC5362750 | core_pubmed_pmc | Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19 | Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19 Abstract The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putati... |
PMC8955737 | core_pubmed_pmc | Mechanism of Soy Isoflavone Daidzein-Induced Female-Specific Anorectic Effect | Mechanism of Soy Isoflavone Daidzein-Induced Female-Specific Anorectic Effect Abstract Epidemiological studies suggest that regular intake of soy isoflavone exerts a preventive effect on postmenopausal obesity and other forms of dysmetabolism. Estrogens inhibit eating behavior. Soy isoflavones may act as estrogen agoni... |
PMC10518600 | core_pubmed_pmc | A phase I, first-in-human study to evaluate the safety and tolerability, pharmacokinetics, and pharmacodynamics of MRG-001 in healthy subjects | A phase I, first-in-human study to evaluate the safety and tolerability, pharmacokinetics, and pharmacodynamics of MRG-001 in healthy subjects Abstract Summary Preclinical studies demonstrate that pharmacological mobilization and recruitment of endogenous bone marrow stem cells and immunoregulatory cells by a fixed-dos... |
PMC4429008 | core_pubmed_pmc | Inhaled anti-infective chemotherapy for respiratory tract infections: Successes, challenges and the road ahead ☆ | Inhaled anti-infective chemotherapy for respiratory tract infections: Successes, challenges and the road ahead ☆ Abstract Abstract One of the most common causes of illnesses in humans is from respiratory tract infections caused by bacterial, viral or fungal pathogens. Inhaled anti-infective drugs are crucial for the pr... |
PMC9398229 | core_pubmed_pmc | Pharmacokinetic, pharmacodynamic, and transcriptomic analysis of chronic levetiracetam treatment in 5XFAD mice: A MODEL‐AD preclinical testing core study | Pharmacokinetic, pharmacodynamic, and transcriptomic analysis of chronic levetiracetam treatment in 5XFAD mice: A MODEL‐AD preclinical testing core study Abstract Abstract Introduction Hyperexcitability and epileptiform activity are commonplace in Alzheimer's disease (AD) patients and associated with impaired cognitive... |
PMC3002823 | core_pubmed_pmc | In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation | In Vivo Bioavailability and Therapeutic Assessment of Host-Guest Inclusion Phenomena for the Hydrophobic Molecule Etodolac: Pharmacodynamic and Pharmacokinetic Evaluation Abstract Abstract The aim of present investigation was 1) to evaluate the in vivo bioavailability of an Etodolac (ETD)-β-cyclodextrin (β-CD) inclusio... |
PMC9863155 | core_pubmed_pmc | Optimizing Antiviral Dosing for HSV and CMV Treatment in Immunocompromised Patients | Optimizing Antiviral Dosing for HSV and CMV Treatment in Immunocompromised Patients Abstract Herpes simplex virus (HSV) and cytomegalovirus (CMV) are DNA viruses that are common among humans. Severely immunocompromised patients are at increased risk of developing HSV or CMV disease due to a weakened immune system. Anti... |
PMC10586285 | core_pubmed_pmc | Biological Evaluation of Xanthene and Thioxanthene Derivatives as Antioxidant, Anticancer, and COX Inhibitors | Biological Evaluation of Xanthene and Thioxanthene Derivatives as Antioxidant, Anticancer, and COX Inhibitors Abstract Abstract Xanthene and thioxanthene analogues have been investigated for their potential as anticancer and anti-inflammatory agents. Additionally, cysteine analogues have been found to possess antioxida... |
PMC12855360 | core_pubmed_pmc | COMT inhibition with entacapone for patients with Parkinson’s disease and motor complications: the novelty of continuous infusion | COMT inhibition with entacapone for patients with Parkinson’s disease and motor complications: the novelty of continuous infusion Abstract Enhancing levodopa efficacy through peripheral COMT inhibition and using continuous infusion are both established strategies for managing motor fluctuations. Both approaches aim to ... |
PMC9915104 | core_pubmed_pmc | Impact of Extracorporeal Membrane Oxygenation in an Infant Treated with Vancomycin: A Case Report | Impact of Extracorporeal Membrane Oxygenation in an Infant Treated with Vancomycin: A Case Report Abstract Abstract Vancomycin is a glycopeptide antibiotic used for prophylaxis and treatment of infections caused by methicillin-resistant Staphylococcus aureus. Although major organ sizes and functions mature during infan... |
PMC4900737 | core_pubmed_pmc | Outcomes of 50 Patients With Ewing Sarcoma Family of Tumors Treated at a Single Institution in Taiwan | Outcomes of 50 Patients With Ewing Sarcoma Family of Tumors Treated at a Single Institution in Taiwan Abstract Abstract To identify the prognostic factors and long-term outcome of the Ewing sarcoma family of tumors (ESFT), data on 50 patients with ESFT treated at Taipei Veterans General Hospital between February 1991 a... |
PMC7542311 | core_pubmed_pmc | Comparison of CYP2C9 Activity in Ethiopian and Non-Ethiopian Jews Using Phenytoin as a Probe | Comparison of CYP2C9 Activity in Ethiopian and Non-Ethiopian Jews Using Phenytoin as a Probe Abstract The pharmacokinetics of CYP2C9 substrates is characterized by substantial interethnic variability. The objective of the study was to compare CYP2C9 activity by using Phenytoin Metabolic Ratio (PMR) between Ethiopian an... |
PMC5648738 | core_pubmed_pmc | Effect of Semaglutide on the Pharmacokinetics of Metformin, Warfarin, Atorvastatin and Digoxin in Healthy Subjects | Effect of Semaglutide on the Pharmacokinetics of Metformin, Warfarin, Atorvastatin and Digoxin in Healthy Subjects Abstract Background and Objective Semaglutide is a glucagon-like peptide-1 analogue in development for the once-weekly treatment of type 2 diabetes mellitus. Its effect on the rate and extent of absorption... |
PMC12877310 | core_pubmed_pmc | A First‐In‐Human Randomized Controlled Phase 1 Study Assessing the Safety and Tolerability of Topical TCP ‐25 Gel in Epidermal Suction Blister Wounds | A First‐In‐Human Randomized Controlled Phase 1 Study Assessing the Safety and Tolerability of Topical TCP ‐25 Gel in Epidermal Suction Blister Wounds Abstract ABSTRACT Inflammation and infection remain unmet challenges in wounds of various etiologies, delaying healing, impacting quality of life, and increasing healthca... |
PMC5767720 | core_pubmed_pmc | Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats | Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats Abstract Abstract Mephedrone (MEPH) is a synthetic cathinone derivative with effects that mimic MDMA and/or cocaine. Our study in male Wistar rats provides detailed investigations of MEPH’s and its primary me... |
PMC8197803 | core_pubmed_pmc | Study Protocol: Phase I Dose Escalation Study of Oxaliplatin, Cisplatin and Doxorubicin Applied as PIPAC in Patients with Peritoneal Metastases | Study Protocol: Phase I Dose Escalation Study of Oxaliplatin, Cisplatin and Doxorubicin Applied as PIPAC in Patients with Peritoneal Metastases Abstract Pressurized Intra-Peritoneal Aerosol Chemotherapy (PIPAC) is a novel laparoscopic intraperitoneal chemotherapy approach offered in selected patients affected by non-re... |
PMC7205744 | core_pubmed_pmc | Anti-seizure therapy with a long-term, implanted intra-cerebroventricular delivery system for drug-resistant epilepsy: A first-in-man study | Anti-seizure therapy with a long-term, implanted intra-cerebroventricular delivery system for drug-resistant epilepsy: A first-in-man study Abstract Background A clinical feasibility study was undertaken at a single center of long-term intra-cerebroventricular drug delivery of the anti-seizure medication valproic acid,... |
PMC6226118 | core_pubmed_pmc | Tutorial on Monoclonal Antibody Pharmacokinetics and Its Considerations in Early Development | Tutorial on Monoclonal Antibody Pharmacokinetics and Its Considerations in Early Development Abstract Abstract The tutorial introduces the readers to the fundamentals of antibody pharmacokinetics (PK) in the context of drug development. Topics covered include an overview of antibody development, PK characteristics, and... |
PMC12419008 | core_pubmed_pmc | In vitro potency and pharmacokinetics of APG777, a novel anti–IL-13 mAb | In vitro potency and pharmacokinetics of APG777, a novel anti–IL-13 mAb Abstract Abstract Background IL-13 plays a key role in the induction and perpetuation of type 2 immune responses associated with the development of atopic dermatitis and other chronic inflammatory diseases. mAbs targeting IL-13 have demonstrated ef... |
PMC10572049 | core_pubmed_pmc | Utility of physiologically based pharmacokinetic modeling to predict inter-antibody variability in monoclonal antibody pharmacokinetics in mice | Utility of physiologically based pharmacokinetic modeling to predict inter-antibody variability in monoclonal antibody pharmacokinetics in mice Abstract ABSTRACT In this investigation, we tested the hypothesis that a physiologically based pharmacokinetic (PBPK) model incorporating measured in vitro metrics of off-targe... |
PMC3862411 | core_pubmed_pmc | Comparative tissue pharmacokinetics and efficacy of moxidectin, abamectin and ivermectin in lambs infected with resistant nematodes: Impact of drug treatments on parasite P-glycoprotein expression ☆ | Comparative tissue pharmacokinetics and efficacy of moxidectin, abamectin and ivermectin in lambs infected with resistant nematodes: Impact of drug treatments on parasite P-glycoprotein expression ☆ Abstract Abstract The high level of resistance to the macrocyclic lactones has encouraged the search for strategies to op... |
PMC6225292 | core_pubmed_pmc | Simultaneous Determination of Aesculin, Aesculetin, Fraxetin, Fraxin and Polydatin in Beagle Dog Plasma by UPLC-ESI-MS/MS and Its Application in a Pharmacokinetic Study after Oral Administration Extracts of Ledum palustre L. | Simultaneous Determination of Aesculin, Aesculetin, Fraxetin, Fraxin and Polydatin in Beagle Dog Plasma by UPLC-ESI-MS/MS and Its Application in a Pharmacokinetic Study after Oral Administration Extracts of Ledum palustre L. Abstract Abstract A rapid, simple and sensitive ultra-performance liquid chromatography-electro... |
PMC7577013 | core_pubmed_pmc | Meeting Report: PMDA Public Workshop on Pharmacometrics at Japan | Meeting Report: PMDA Public Workshop on Pharmacometrics at Japan Discussion DISCUSSION The draft guideline for ER analysis has been finalized based on views exchanged in the workshop that was held just after the completion of public consultation on “Guideline for drug exposure‐response analysis (draft)” conducted by th... |
PMC8390591 | core_pubmed_pmc | Interstitial washdown and vascular albumin refill during fluid infusion: novel kinetic analysis from three clinical trials | Interstitial washdown and vascular albumin refill during fluid infusion: novel kinetic analysis from three clinical trials Abstract Abstract Background and aims Increased capillary filtration may paradoxically accelerate vascular refill of both fluid and albumin from the interstitial space, which is claimed to be edema... |
PMC11208962 | core_pubmed_pmc | A Nanopore Sequencing-based Pharmacogenomic Panel to Personalize Tuberculosis Drug Dosing | A Nanopore Sequencing-based Pharmacogenomic Panel to Personalize Tuberculosis Drug Dosing Abstract Abstract Rationale Standardized dosing of antitubercular drugs leads to variable plasma drug levels, which are associated with adverse drug reactions, delayed treatment response, and relapse. Mutations in genes affecting ... |
PMC12452960 | core_pubmed_pmc | Population Pharmacokinetics and Covariate Analysis of Methotrexate in Pediatric Acute Lymphoblastic Leukemia | Population Pharmacokinetics and Covariate Analysis of Methotrexate in Pediatric Acute Lymphoblastic Leukemia Abstract Abstract Purpose The current study was designed to develop and validate a population pharmacokinetic (PPK) model of methotrexate (MTX) in pediatric patients with acute lymphoblastic leukemia (ALL). We a... |
PMC12804822 | core_pubmed_pmc | Establishing FDA-approved oncology drugs as GPR176 inhibitor through homology modelling, molecular docking, MMGBSA, DFT, and molecular dynamics simulation | Establishing FDA-approved oncology drugs as GPR176 inhibitor through homology modelling, molecular docking, MMGBSA, DFT, and molecular dynamics simulation Abstract Abstract The GPR176 protein is a cell membrane protein implicated in human diseases, especially cancers. Numerous studies have highlighted its overexpressio... |
PMC9697781 | core_pubmed_pmc | 18 F-Radiolabeled Translocator Protein (TSPO) PET Tracers: Recent Development of TSPO Radioligands and Their Application to PET Study | 18 F-Radiolabeled Translocator Protein (TSPO) PET Tracers: Recent Development of TSPO Radioligands and Their Application to PET Study Abstract Abstract Translocator protein 18 kDa (TSPO) is a transmembrane protein in the mitochondrial membrane, which has been identified as a peripheral benzodiazepine receptor. TSPO is ... |
PMC12408558 | core_pubmed_pmc | Model-based prediction of nanoparticle and dissolved form ratios using total concentration data: a case study of SNB-101 | Model-based prediction of nanoparticle and dissolved form ratios using total concentration data: a case study of SNB-101 Abstract Abstract Introduction Irinotecan (CPT-11), a topoisomerase I inhibitor, serves as a prodrug for SN-38, its active metabolite with significantly higher cytotoxic potency. Despite its clinical... |
PMC4120019 | core_pubmed_pmc | Clinical Translation in the Virtual Liver Network | Clinical Translation in the Virtual Liver Network Abstract Abstract The liver is the central detoxifying organ, continuously removing xenobiotics from the vascular system. Given its role in drug metabolism, a functional understanding of liver physiology is crucial to optimizing drug efficacy and patient safety. The Vir... |
PMC10057980 | core_pubmed_pmc | Pharmacokinetics of Orally Applied Cannabinoids and Medical Marijuana Extracts in Mouse Nervous Tissue and Plasma: Relevance for Pain Treatment | Pharmacokinetics of Orally Applied Cannabinoids and Medical Marijuana Extracts in Mouse Nervous Tissue and Plasma: Relevance for Pain Treatment Abstract Abstract Cannabis sativa plants contain a multitude of bioactive substances, which show broad variability between different plant strains. Of the more than a hundred n... |
PMC5761216 | core_pubmed_pmc | Simultaneous determination of borneol and its metabolite in rat plasma by GC–MS and its application to pharmacokinetic study | Simultaneous determination of borneol and its metabolite in rat plasma by GC–MS and its application to pharmacokinetic study Abstract Abstract A gas chromatography mass spectrometry (GC–MS) method has been developed and fully validated for the simultaneous determination of natural borneol (NB) and its metabolite, camph... |
PMC8452291 | core_pubmed_pmc | Precision dosing of intravenous busulfan in pediatric hematopoietic stem cell transplantation: Results from a multicenter population pharmacokinetic study | Precision dosing of intravenous busulfan in pediatric hematopoietic stem cell transplantation: Results from a multicenter population pharmacokinetic study Abstract Abstract Busulfan (Bu) is a common component of conditioning regimens before hematopoietic stem cell transplantation (HSCT) and is known for high interpatie... |
PMC4460047 | core_pubmed_pmc | Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats | Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats Abstract Palmitoylethanolamide (PEA) has antinflammatory and antinociceptive properties widely exploited in veterinary and human medicine, despite its poor pharmacokinetics. Looking for prodrugs t... |
PMC3322481 | core_pubmed_pmc | Population Pharmacokinetics of Vancomycin in Thai Patients | Population Pharmacokinetics of Vancomycin in Thai Patients Abstract Population pharmacokinetics of vancomycin in Thai adult patients was determined by non-linear mixed-effects approach using 319 vancomycin serum concentrations from 212 patients. The data were best fitted by a two-compartment model and it was used to ex... |
PMC12138820 | core_pubmed_pmc | Estimation and Validation of an Effective Ergothioneine Dose for Improved Sleep Quality Using Physiologically Based Pharmacokinetic Model | Estimation and Validation of an Effective Ergothioneine Dose for Improved Sleep Quality Using Physiologically Based Pharmacokinetic Model Abstract ABSTRACT A four‐week administration of 20 mg/day ergothioneine (EGT), a strong antioxidant, improves sleep quality; however, its effect at lower doses remains unclear. This ... |
PMC11728531 | core_pubmed_pmc | Preparation and In Vitro/In Vivo Characterization of Mixed-Micelles-Loaded Dissolving Microneedles for Sustained Release of Indomethacin | Preparation and In Vitro/In Vivo Characterization of Mixed-Micelles-Loaded Dissolving Microneedles for Sustained Release of Indomethacin Abstract Abstract Background/Objectives: Indomethacin (IDM) is commonly used to treat chronic inflammatory diseases such as rheumatoid arthritis and osteoarthritis. However, long-term... |
PMC12497388 | core_pubmed_pmc | LC-MS/MS Method for Simultaneous Quantification of Three Oxazolidinone Antimicrobials in Human Plasma: Application to Therapeutic Drug Monitoring | LC-MS/MS Method for Simultaneous Quantification of Three Oxazolidinone Antimicrobials in Human Plasma: Application to Therapeutic Drug Monitoring Abstract Background Oxazolidinone antimicrobials, which are effective against multidrug-resistant gram-positive pathogens, face challenges of variable efficacy and safety owi... |
PMC6212553 | core_pubmed_pmc | Baicalein Enhances the Oral Bioavailability and Hepatoprotective Effects of Silybin Through the Inhibition of Efflux Transporters BCRP and MRP2 | Baicalein Enhances the Oral Bioavailability and Hepatoprotective Effects of Silybin Through the Inhibition of Efflux Transporters BCRP and MRP2 Abstract Abstract Although hepatoprotective properties of silybin are well documented, the clinical therapeutic efficacy is limited by its low bioavailability due to absorption... |
PMC7834647 | core_pubmed_pmc | Is it possible to use Proton Pump Inhibitors in COVID-19 treatment and prophylaxis? | Is it possible to use Proton Pump Inhibitors in COVID-19 treatment and prophylaxis? Abstract Abstract Coronaviruses (CoV), discovered after 1960, caused human life-threatening outbreaks. SARS-CoV2, which appeared in Wuhan, China in December 2019, causing Severe Acute Respiratory Syndrome and has different features than... |
PMC11476483 | core_pubmed_pmc | Review of drug-drug interactions in patients with prostate cancer | Review of drug-drug interactions in patients with prostate cancer Abstract Objective The objective of this review is to provide an overview of common drug-drug interactions (DDIs) associated with prostate cancer treatments and outline recommendations for managing polypharmacy. Data sources A literature search of PubMed... |
PMC11496754 | core_pubmed_pmc | Drug–drug interactions between letermovir and tacrolimus in Japanese renal transplant recipients simulated using a physiologically based pharmacokinetic model | Drug–drug interactions between letermovir and tacrolimus in Japanese renal transplant recipients simulated using a physiologically based pharmacokinetic model Abstract Letermovir (LET) is a novel antiviral agent recently approved for cytomegalovirus (CMV) prophylaxis of renal transplant patients in Japan. However, its ... |
PMC9393037 | core_pubmed_pmc | Long-Circulation and Brain Targeted Isoliquiritigenin Micelle Nanoparticles: Formation, Characterization, Tissue Distribution, Pharmacokinetics and Effects for Ischemic Stroke | Long-Circulation and Brain Targeted Isoliquiritigenin Micelle Nanoparticles: Formation, Characterization, Tissue Distribution, Pharmacokinetics and Effects for Ischemic Stroke Abstract Abstract Purpose We designed a novel isoliquiritigenin (ISL) loaded micelle prepared with DSPE-PEG 2000 as the drug carrier modified wi... |
PMC2904846 | core_pubmed_pmc | High fludarabine exposure and relationship with treatment-related mortality after nonmyeloablative hematopoietic cell transplantation | High fludarabine exposure and relationship with treatment-related mortality after nonmyeloablative hematopoietic cell transplantation Abstract Despite its common use in nonmyeloablative preparative regimens, the pharmacokinetics of fludarabine are poorly characterized in hematopoietic cell transplantation (HCT) recipie... |
PMC4944512 | core_pubmed_pmc | Pharmacokinetics of ranitidine in preterm and term neonates with gastroesophageal reflux | Pharmacokinetics of ranitidine in preterm and term neonates with gastroesophageal reflux Abstract Abstract Background The aim of this study was to determine the effect of gestational age on pharmacokinetics of ranitidine in newborns with gastroesophageal reflux. Methods A prospective, descriptive and pharmacokinetic st... |
PMC12147034 | core_pubmed_pmc | Identification of alkynyl nicotinamide HSN748 as a RET solvent-front mutant inhibitor with intracranial efficacy † | Identification of alkynyl nicotinamide HSN748 as a RET solvent-front mutant inhibitor with intracranial efficacy † Abstract RET solvent-front G810C/R/S mutations confer resistance to the currently approved RET protein tyrosine kinase inhibitors (TKIs) selpercatinib and pralsetinib. Moreover, RET fusion-positive lung ad... |
PMC12195665 | core_pubmed_pmc | A Label-Free Liquid Chromatography–Tandem Mass Spectrometry Method for the Quantitative Analysis of Exosome Pharmacokinetics In Vivo | A Label-Free Liquid Chromatography–Tandem Mass Spectrometry Method for the Quantitative Analysis of Exosome Pharmacokinetics In Vivo Abstract Abstract Background: Exosomes are nanoscale extracellular vesicles actively secreted by cells that play critical roles in disease biomarker discovery, drug delivery, and direct t... |
PMC9730379 | core_pubmed_pmc | Computational model of CAR T-cell immunotherapy dissects and predicts leukemia patient responses at remission, resistance, and relapse | Computational model of CAR T-cell immunotherapy dissects and predicts leukemia patient responses at remission, resistance, and relapse Abstract Background Adaptive CD19-targeted chimeric antigen receptor (CAR) T-cell transfer has become a promising treatment for leukemia. Although patient responses vary across differen... |
PMC9573218 | core_pubmed_pmc | Vardenafil-Loaded Bilosomal Mucoadhesive Sponge for Buccal Delivery: Optimization, Characterization, and In Vivo Evaluation | Vardenafil-Loaded Bilosomal Mucoadhesive Sponge for Buccal Delivery: Optimization, Characterization, and In Vivo Evaluation Abstract Vardenafil (VDF) is a relatively new phosphodiesterase-5 inhibitor that has limited oral bioavailability (≈15%). The objective of this study was to develop bilosome-based mucoadhesive buc... |
PMC6959213 | core_pubmed_pmc | Survey on Polypharmacy and Drug-Drug Interactions Among Elderly People with Cardiovascular Diseases at Yekatit 12 Hospital, Addis Ababa, Ethiopia | Survey on Polypharmacy and Drug-Drug Interactions Among Elderly People with Cardiovascular Diseases at Yekatit 12 Hospital, Addis Ababa, Ethiopia Abstract Background Elderly people are most commonly associated with cardiac disease. Cardiovascular diseases are interlinked with co-morbidities which require multiple drug ... |
PMC11889410 | core_pubmed_pmc | Agents for Change: Artificial Intelligent Workflows for Quantitative Clinical Pharmacology and Translational Sciences | Agents for Change: Artificial Intelligent Workflows for Quantitative Clinical Pharmacology and Translational Sciences Abstract ABSTRACT Artificial intelligence (AI) is making a significant impact across various industries, including healthcare, where it is driving innovation and increasing efficiency. In the fields of ... |
PMC8146254 | core_pubmed_pmc | Fluorophores Use in Pituitary Surgery: A Pharmacokinetics and Pharmacodynamics Appraisal | Fluorophores Use in Pituitary Surgery: A Pharmacokinetics and Pharmacodynamics Appraisal Abstract (1) Background: Despite many surgical and technological advances, pituitary adenoma surgery is still burdened by non-negligible rates of incomplete tumor resection, mainly due to difficulties in differentiating pathology f... |
PMC9050769 | core_pubmed_pmc | Population Pharmacokinetic Model for Tramadol and O -desmethyltramadol in Older Patients | Population Pharmacokinetic Model for Tramadol and O -desmethyltramadol in Older Patients Abstract Background and Objectives Tramadol is commonly prescribed to manage chronic pain in older patients. However, there is a gap in the literature describing the pharmacokinetic parameters for tramadol and its active metabolite... |
PMC8856114 | core_pubmed_pmc | Evodiamine decreased the systemic exposure of pravastatin in non-alcoholic steatohepatitis rats due to the up-regulation of hepatic OATPs | Evodiamine decreased the systemic exposure of pravastatin in non-alcoholic steatohepatitis rats due to the up-regulation of hepatic OATPs Abstract Abstract Context Patients with non-alcoholic steatohepatitis (NASH) may have a simultaneous intake of pravastatin and evodiamine-containing herbs. Objective The effect of ev... |
PMC7687240 | core_pubmed_pmc | A Single‐Dose, Open‐Label, Randomized, Two‐Way Crossover Study in Healthy Japanese Participants to Evaluate the Bioequivalence and the Food Effect on the Pharmacokinetics of Daprodustat | A Single‐Dose, Open‐Label, Randomized, Two‐Way Crossover Study in Healthy Japanese Participants to Evaluate the Bioequivalence and the Food Effect on the Pharmacokinetics of Daprodustat Abstract Abstract Daprodustat is a prolyl hydroxylase inhibitor that stimulates erythropoiesis in a manner similar to the natural resp... |
PMC12566730 | core_pubmed_pmc | Resensitizing the Untreatable: Zidovudine and Polymyxin Combinations to Combat Pan-Drug-Resistant Klebsiella pneumoniae | Resensitizing the Untreatable: Zidovudine and Polymyxin Combinations to Combat Pan-Drug-Resistant Klebsiella pneumoniae Abstract Background: The emergence of pan-drug-resistant (PDR) Klebsiella pneumoniae has compromised the efficacy of last-line agents, leaving few therapeutic options. Repurposing zidovudine, an FDA-a... |
PMC7151237 | core_pubmed_pmc | Preparation, Characterization, and In Vivo Pharmacokinetic Evaluation of Polyvinyl Alcohol and Polyvinyl Pyrrolidone Blended Hydrogels for Transdermal Delivery of Donepezil HCl | Preparation, Characterization, and In Vivo Pharmacokinetic Evaluation of Polyvinyl Alcohol and Polyvinyl Pyrrolidone Blended Hydrogels for Transdermal Delivery of Donepezil HCl Abstract Abstract Transdermal delivery systems are emerging platforms for the delivery of donepezil hydrochloride (DH) for treating Alzheimer’s... |
PMC7053720 | core_pubmed_pmc | Mathematical modeling and parameter estimation of levodopa motor response in patients with parkinson disease | Mathematical modeling and parameter estimation of levodopa motor response in patients with parkinson disease Abstract Abstract Parkinson disease (PD) is characterized by a clear beneficial motor response to levodopa (LD) treatment. However, with disease progression and longer LD exposure, drug-related motor fluctuation... |
PMC7291256 | core_pubmed_pmc | A Randomized Comparison of Plasma Levobupivacaine Concentrations Following Thoracic Epidural Analgesia and Subpleural Paravertebral Analgesia in Open Thoracic Surgery | A Randomized Comparison of Plasma Levobupivacaine Concentrations Following Thoracic Epidural Analgesia and Subpleural Paravertebral Analgesia in Open Thoracic Surgery Abstract Background: The aim of this study was to compare plasma levobupivacaine concentrations in thoracic epidural and subpleural paravertebral analges... |
PMC10905521 | core_pubmed_pmc | Phase I Trial of First-line Bintrafusp Alfa in Patients with Locally Advanced or Persistent/Recurrent/Metastatic Cervical Cancer | Phase I Trial of First-line Bintrafusp Alfa in Patients with Locally Advanced or Persistent/Recurrent/Metastatic Cervical Cancer Abstract Abstract Purpose: Bintrafusp alfa, a first-in-class bifunctional fusion protein composed of the extracellular domain of TGFβ receptor II (a TGFβ “trap”) fused to a human IgG1 mAb blo... |
PMC7692355 | core_pubmed_pmc | Effects of Intestinal Microbiota on Pharmacokinetics of Crocin and Crocetin in Male Sprague-Dawley Rats | Effects of Intestinal Microbiota on Pharmacokinetics of Crocin and Crocetin in Male Sprague-Dawley Rats Abstract Abstract In addition to the hepatic metabolism, the role of intestinal microbiota in drug metabolism has been considered important in the biotransformation of xenobiotics. Crocin and its aglycone, crocetin, ... |
PMC8964335 | core_pubmed_pmc | Co-Administration with Voriconazole Doubles the Exposure of Ruxolitinib in Patients with Hematological Malignancies | Co-Administration with Voriconazole Doubles the Exposure of Ruxolitinib in Patients with Hematological Malignancies Abstract Background Ruxolitinib is newly approved for glucocorticoid-refractory acute graft-versus-host disease (GVHD) in patients undergoing allo-geneic hematopoietic stem-cell transplantation (allo-HSCT... |
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