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PMC3615930 | core_pubmed_pmc | Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study | Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study Abstract Abstract Background The combination of umeclidinium (UMEC), a long-acting muscarinic receptor antagonist, and vilanterol (VI), a selective long-acting β 2 agonist, is in development for the tre... |
PMC5647335 | core_pubmed_pmc | Controlling the bioactivity of a peptide hormone in vivo by reversible self-assembly | Controlling the bioactivity of a peptide hormone in vivo by reversible self-assembly Abstract The use of peptides as therapeutic agents is undergoing a renaissance with the expectation of new drugs with enhanced levels of efficacy and safety. Their clinical potential will be only fully realised once their physicochemic... |
PMC10981579 | core_pubmed_pmc | Ezabenlimab (BI 754091), an anti-PD-1 antibody, in patients with advanced solid tumours | Ezabenlimab (BI 754091), an anti-PD-1 antibody, in patients with advanced solid tumours Abstract Abstract Background Ezabenlimab (BI 754091) is a humanised monoclonal antibody targeting programmed cell death protein-1. We report results from open-label, dose-escalation/expansion, Phase I trials that evaluated the safet... |
PMC5914018 | core_pubmed_pmc | N-of-1 trials in the clinical care of patients in developing countries: a systematic review | N-of-1 trials in the clinical care of patients in developing countries: a systematic review Abstract Abstract Background N-of-1 trials have a potential role in promoting patient-centered medicine in developing countries. However, there is limited academic literature regarding the use of N-of-1 trials in the clinical ca... |
PMC9579398 | core_pubmed_pmc | A proof of concept using the Ussing chamber methodology to study pediatric intestinal drug transport and age‐dependent differences in absorption | A proof of concept using the Ussing chamber methodology to study pediatric intestinal drug transport and age‐dependent differences in absorption Abstract Abstract Little is known about the impact of age on the processes governing human intestinal drug absorption. The Ussing chamber is a system to study drug transport a... |
PMC7654938 | core_pubmed_pmc | Single-Dose Pharmacokinetics and Pharmacodynamics of IPX203 in Patients With Advanced Parkinson Disease: A Comparison With Immediate-Release Carbidopa-Levodopa and With Extended-Release Carbidopa-Levodopa Capsules | Single-Dose Pharmacokinetics and Pharmacodynamics of IPX203 in Patients With Advanced Parkinson Disease: A Comparison With Immediate-Release Carbidopa-Levodopa and With Extended-Release Carbidopa-Levodopa Capsules Abstract Objective IPX203 is an investigational oral extended-release capsule formulation of carbidopa-lev... |
PMC5075098 | core_pubmed_pmc | Preclinical Evaluation of the Stability, Safety, and Efficacy of CD101, a Novel Echinocandin | Preclinical Evaluation of the Stability, Safety, and Efficacy of CD101, a Novel Echinocandin Abstract Abstract Fungal infections pose a significant public health burden with high morbidity and mortality. CD101 is a novel echinocandin under development for the treatment and prevention of systemic Candida infections. Pre... |
PMC7032964 | core_pubmed_pmc | Treatment response and disease progression | Treatment response and disease progression Abstract Abstract This tutorial defines the concepts of disease progression in the context of clinical pharmacology. Disease progression describes the natural history of disease, such as pain, or biomarker of drug response, such as blood pressure. The action of a drug, such as... |
PMC11891907 | core_pubmed_pmc | Nanomedicine Innovations for Lung Cancer Diagnosis and Therapy | Nanomedicine Innovations for Lung Cancer Diagnosis and Therapy Abstract Lung cancer remains a challenge within the realm of oncology. Characterized by late-stage diagnosis and resistance to conventional treatments, the currently available therapeutic strategies encompass surgery, radiotherapy, chemotherapy, immunothera... |
PMC12678371 | core_pubmed_pmc | Preclinical pharmacokinetic characterization of (R)-ketamine injection, a novel antidepressant glutamatergic agent | Preclinical pharmacokinetic characterization of (R)-ketamine injection, a novel antidepressant glutamatergic agent Abstract Introduction Ketamine is a significant class of antidepressant drugs, and the pharmacokinetic and pharmacodynamic characteristics of its enantiomers exhibit differences. Among them, intravenous in... |
PMC5221883 | core_pubmed_pmc | Pharmacokinetics of Lidocaine Hydrochloride Administered with or without Adrenaline for the Paravertebral Brachial Plexus Block in Dogs | Pharmacokinetics of Lidocaine Hydrochloride Administered with or without Adrenaline for the Paravertebral Brachial Plexus Block in Dogs Abstract Adrenaline is known to prolong the duration of local anesthesia but its effects on the pharmacokinetic processes of local anesthetic drugs are not fully understood. Our object... |
PMC7867377 | core_pubmed_pmc | Phytochemistry, Bioactivities, Pharmacokinetics and Toxicity Prediction of Selaginella repanda with Its Anticancer Potential against Human Lung, Breast and Colorectal Carcinoma Cell Lines | Phytochemistry, Bioactivities, Pharmacokinetics and Toxicity Prediction of Selaginella repanda with Its Anticancer Potential against Human Lung, Breast and Colorectal Carcinoma Cell Lines Abstract In this study, we investigated the bioactive potential (antibacterial and antioxidant), anticancer activity and detailed ph... |
PMC6224495 | core_pubmed_pmc | Localising functionalised gold-nanoparticles in murine spinal cords by X-ray fluorescence imaging and background-reduction through spatial filtering for human-sized objects | Localising functionalised gold-nanoparticles in murine spinal cords by X-ray fluorescence imaging and background-reduction through spatial filtering for human-sized objects Abstract Accurate in vivo localisation of minimal amounts of functionalised gold-nanoparticles, enabling e.g . early-tumour diagnostics and pharmac... |
PMC5651340 | core_pubmed_pmc | First-in-human, double-blind, placebo-controlled, single-dose escalation study of aducanumab (BIIB037) in mild-to-moderate Alzheimer's disease | First-in-human, double-blind, placebo-controlled, single-dose escalation study of aducanumab (BIIB037) in mild-to-moderate Alzheimer's disease Abstract Introduction Aducanumab (BIIB037), a human monoclonal antibody selective for aggregated forms of amyloid beta, is being investigated as a disease-modifying treatment fo... |
PMC11835422 | core_pubmed_pmc | Clinical and Physiologically Based Pharmacokinetic Model Evaluations of Adagrasib Drug–Drug Interactions | Clinical and Physiologically Based Pharmacokinetic Model Evaluations of Adagrasib Drug–Drug Interactions Abstract Abstract Adagrasib is a potent, highly selective, orally available, small molecule, covalent inhibitor of G12C mutated KRAS. As both a substrate and strong inhibitor of cytochrome P450 (CYP) 3A4, adagrasib ... |
PMC9017385 | core_pubmed_pmc | Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants | Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants Abstract ABSTRACT Fostemsavir is a prodrug of temsavir, a first-in-class att... |
PMC9090854 | core_pubmed_pmc | Predicting Viable Skin Concentration: Modelling the Subpapillary Plexus | Predicting Viable Skin Concentration: Modelling the Subpapillary Plexus Abstract Abstract The skin concentration of a substance after a topical application or exposure determines both local treatment outcomes and the dermal toxicity assessment of various products. However, quantifying the time course of those concentra... |
PMC10439066 | core_pubmed_pmc | Hepatotoxicity of AKR1C3 Inhibitor BAY1128688: Findings from an Early Terminated Phase IIa Trial for the Treatment of Endometriosis | Hepatotoxicity of AKR1C3 Inhibitor BAY1128688: Findings from an Early Terminated Phase IIa Trial for the Treatment of Endometriosis Abstract Introduction BAY1128688 is a selective inhibitor of aldo-keto reductase family 1 member C3 (AKR1C3), an enzyme implicated in the pathology of endometriosis and other disorders. In... |
PMC6951463 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Analysis of Intravenous Zanamivir in Healthy Adults and Hospitalized Adult and Pediatric Subjects With Influenza | Population Pharmacokinetic/Pharmacodynamic Analysis of Intravenous Zanamivir in Healthy Adults and Hospitalized Adult and Pediatric Subjects With Influenza Abstract Abstract Zanamivir is a potent and highly selective inhibitor of influenza neuraminidase in which the inhibition of this enzyme prevents the virus from inf... |
PMC12625128 | core_pubmed_pmc | A model‐informed clinical trial simulation tool with a graphical user interface for Duchenne muscular dystrophy | A model‐informed clinical trial simulation tool with a graphical user interface for Duchenne muscular dystrophy Abstract Abstract Quantitative model‐based clinical trial simulation tools play a critical role in informing study designs through simulation before actual execution. These tools help drug developers explore ... |
PMC8100460 | core_pubmed_pmc | CYP3A5 and UGT1A9 Polymorphisms Influence Immunosuppressive Therapy in Pediatric Kidney Transplant Recipients | CYP3A5 and UGT1A9 Polymorphisms Influence Immunosuppressive Therapy in Pediatric Kidney Transplant Recipients Abstract Abstract Background: Tacrolimus (TAC) and mycophenolic acid (MPA) are the main immunosuppressive drugs used in pediatric kidney transplantation. Single nucleotide polymorphisms (SNPs) in metabolizing e... |
PMC9102399 | core_pubmed_pmc | Comparative Study of Preparation, Evaluation, and Pharmacokinetics in Beagle Dogs of Curcumin β-Cyclodextrin Inclusion Complex, Curcumin Solid Dispersion, and Curcumin Phospholipid Complex | Comparative Study of Preparation, Evaluation, and Pharmacokinetics in Beagle Dogs of Curcumin β-Cyclodextrin Inclusion Complex, Curcumin Solid Dispersion, and Curcumin Phospholipid Complex Abstract Curcumin is a natural acidic polyphenol extracted from turmeric with a wide range of biological and pharmacological effect... |
PMC10209603 | core_pubmed_pmc | Pharmacokinetics and effect of maslinic acid with physical exercise on grip strength and trunk muscle mass in healthy Japanese individuals | Pharmacokinetics and effect of maslinic acid with physical exercise on grip strength and trunk muscle mass in healthy Japanese individuals Abstract Abstract Age-related changes in physical function are closely associated with daily activity impairment among the elderly. Continuous maslinic acid intake may improve skele... |
PMC7044683 | core_pubmed_pmc | United States Pharmacopeia (USP) comprehensive review of the hepatotoxicity of green tea extracts | United States Pharmacopeia (USP) comprehensive review of the hepatotoxicity of green tea extracts Abstract Abstract As part of the United States Pharmacopeia’s ongoing review of dietary supplement safety data, a new comprehensive systematic review on green tea extracts (GTE) has been completed. GTEs may contain hepatot... |
PMC6934983 | core_pubmed_pmc | A New Model to Describe the Single-dose Pharmacokinetics of Bevacizumab and Predict Its Multiple-Dose Pharmacokinetics in Beagle Dogs | A New Model to Describe the Single-dose Pharmacokinetics of Bevacizumab and Predict Its Multiple-Dose Pharmacokinetics in Beagle Dogs Abstract Abstract Complex pharmacokinetic (PK) properties including nonlinear elimination were encountered by some monoclonal antibodies (mAbs), and classic compartment models sometimes ... |
PMC8128043 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics in the treatment of cutaneous leishmaniasis – challenges and opportunities | Pharmacokinetics and pharmacodynamics in the treatment of cutaneous leishmaniasis – challenges and opportunities Abstract Pharmacological efficacy is obtained when adequate concentrations of a potent drug reach the target site. In cutaneous leishmaniasis, a heterogeneous disease characterised by a variety of skin manif... |
PMC9909811 | core_pubmed_pmc | In Silico Characterization of Withania coagulans Bioactive Compounds as Potential Inhibitors of Hydroxymethylglutaryl (HMG-CoA) Reductase of Mus musculus | In Silico Characterization of Withania coagulans Bioactive Compounds as Potential Inhibitors of Hydroxymethylglutaryl (HMG-CoA) Reductase of Mus musculus Abstract Abstract Hypercholesterolemia is a mediator for the etiology of cardiovascular diseases, which are characterized as the global leading cause of mortality. We... |
PMC10982099 | core_pubmed_pmc | Explaining in-vitro to in-vivo efficacy correlations in oncology pre-clinical development via a semi-mechanistic mathematical model | Explaining in-vitro to in-vivo efficacy correlations in oncology pre-clinical development via a semi-mechanistic mathematical model Abstract Abstract In-vitro to in-vivo correlations (IVIVC), relating in-vitro parameters like IC 50 to in-vivo drug exposure in plasma and tumour growth, are widely used in oncology for ex... |
PMC10269516 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics, and immunogenicity of an anti-SARS-CoV-2 monoclonal antibody HFB30132A after single dose intravenous administration in healthy Chinese subjects: a phase 1, randomized, double-blind, placebo-controlled study | Safety, tolerability, pharmacokinetics, and immunogenicity of an anti-SARS-CoV-2 monoclonal antibody HFB30132A after single dose intravenous administration in healthy Chinese subjects: a phase 1, randomized, double-blind, placebo-controlled study Abstract Objective: The pandemic of coronavirus disease 2019 (COVID-19) c... |
PMC12473409 | core_pubmed_pmc | PBPK/PD Model of Vancomycin in Sepsis: Linking Interstitial Exposure in Perfusion-Limited Tissues to MRSA Infection | PBPK/PD Model of Vancomycin in Sepsis: Linking Interstitial Exposure in Perfusion-Limited Tissues to MRSA Infection Abstract Abstract Objective : This study aims to evaluate free vancomycin concentrations in tissues of septic patients that received empirical doses. Methods : A PBPK model was built in PK-Sim to simulate... |
PMC9978475 | core_pubmed_pmc | Comparison of Yizhiqingxin formula extraction methods and their pharmacodynamic differences | Comparison of Yizhiqingxin formula extraction methods and their pharmacodynamic differences Abstract Objectives This study compared different extraction methods of Yizhiqingxin formula (YQF) and its neuroprotective effects based on pharmacodynamic indices such as learning and memory ability, brain tissue histopathology... |
PMC9695976 | core_pubmed_pmc | Simultaneous Determination of Moxifloxacin Hydrochloride and Dexamethasone Sodium Phosphate in Rabbit Ocular Tissues and Plasma by LC-MS/MS: Application for Pharmacokinetics Studies | Simultaneous Determination of Moxifloxacin Hydrochloride and Dexamethasone Sodium Phosphate in Rabbit Ocular Tissues and Plasma by LC-MS/MS: Application for Pharmacokinetics Studies Abstract Treatment of ocular infection involves pharmacotherapy with steroids and antibiotic drops, such as moxifloxacin hydrochloride (MF... |
PMC8775521 | core_pubmed_pmc | Biguanide Pharmaceutical Formulations and the Applications of Bile Acid-Based Nano Delivery in Chronic Medical Conditions | Biguanide Pharmaceutical Formulations and the Applications of Bile Acid-Based Nano Delivery in Chronic Medical Conditions Abstract Biguanides, particularly the widely prescribed drug metformin, have been marketed for many decades and have well-established absorption profiles. They are commonly administered via the oral... |
PMC5035790 | core_pubmed_pmc | First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas | First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas Abstract This phase I study evaluated the safety, tolerability, and pharmacokinetics of copanlisib, an intravenously administer... |
PMC10432884 | core_pubmed_pmc | First‐in‐human trial to assess safety, tolerability, pharmacokinetics, and pharmacodynamics of zagociguat (CY6463), a CNS‐penetrant soluble guanylyl cyclase stimulator | First‐in‐human trial to assess safety, tolerability, pharmacokinetics, and pharmacodynamics of zagociguat (CY6463), a CNS‐penetrant soluble guanylyl cyclase stimulator Abstract Abstract Soluble guanylate cyclase (sGC) and its product, cyclic guanosine monophosphate, play a role in learning and memory formation. Zagocig... |
PMC7188401 | core_pubmed_pmc | Preclinical characterization of the ADME properties of a surrogate anti-IL-36R monoclonal antibody antagonist in mouse serum and tissues | Preclinical characterization of the ADME properties of a surrogate anti-IL-36R monoclonal antibody antagonist in mouse serum and tissues Abstract ABSTRACT The decision to pursue a monoclonal antibody (mAb) as a therapeutic for disease intervention requires the assessment of many factors, such as target-biology, includi... |
PMC10863906 | core_pubmed_pmc | Topiramate dosage optimization for effective antiseizure management via population pharmacokinetic modeling | Topiramate dosage optimization for effective antiseizure management via population pharmacokinetic modeling Abstract Abstract Objective Despite the suggested topiramate serum level of 5–20 mg/L, numerous institutions have observed substantial drug response at lower levels. We aim to investigate the correlation between ... |
PMC5107207 | core_pubmed_pmc | Development of a Whole-Body Physiologically Based Pharmacokinetic Approach to Assess the Pharmacokinetics of Drugs in Elderly Individuals | Development of a Whole-Body Physiologically Based Pharmacokinetic Approach to Assess the Pharmacokinetics of Drugs in Elderly Individuals Abstract Abstract Background Because of the vulnerability and frailty of elderly adults, clinical drug development has traditionally been biased towards young and middle-aged adults.... |
PMC5944589 | core_pubmed_pmc | Big Data Toolsets to Pharmacometrics: Application of Machine Learning for Time‐to‐Event Analysis | Big Data Toolsets to Pharmacometrics: Application of Machine Learning for Time‐to‐Event Analysis Abstract Abstract Additional value can be potentially created by applying big data tools to address pharmacometric problems. The performances of machine learning (ML) methods and the Cox regression model were evaluated base... |
PMC6471907 | core_pubmed_pmc | Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability | Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability Abstract Abstract Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug del... |
PMC6030392 | core_pubmed_pmc | Improved Brain Penetration and Antitumor Efficacy of Temozolomide by Inhibition of ABCB1 and ABCG2 1 | Improved Brain Penetration and Antitumor Efficacy of Temozolomide by Inhibition of ABCB1 and ABCG2 1 Abstract The anticancer drug temozolomide is the only drug with proven activity against high-grade gliomas and has therefore become a part of the standard treatment of these tumors. P-glycoprotein (P-gp; ABCB1) and brea... |
PMC12645117 | core_pubmed_pmc | Limitations and Innovative Application Methods of Surfactants for Solubilization of Poorly Water-Soluble Drugs | Limitations and Innovative Application Methods of Surfactants for Solubilization of Poorly Water-Soluble Drugs Abstract Poor solubility of drugs leads to poor bioavailability and therapeutic efficiency. A large proportion of drugs that are not developed and marketed for use by patients are due to their extremely low so... |
PMC4584421 | core_pubmed_pmc | Safety, pharmacokinetic and pharmacodynamic properties of TV-1106, a long-acting GH treatment for GH deficiency | Safety, pharmacokinetic and pharmacodynamic properties of TV-1106, a long-acting GH treatment for GH deficiency Abstract Background TV-1106 (Teva Pharmaceuticals) is a genetically fused recombinant protein of human GH (hGH) and human serum albumin, in development for treatment of GH deficiency (GHD). TV-1106 is expecte... |
PMC8398354 | core_pubmed_pmc | The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity | The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity Abstract Designer benzodiazepines (DBZDs) represent a serious health concern and are increasingly reported in polydrug consumption-related fatalities. When new DBZDs are ide... |
PMC12884390 | core_pubmed_pmc | Mechanistic and therapeutic dimensions of DcR3-mediated immunomodulation in sepsis | Mechanistic and therapeutic dimensions of DcR3-mediated immunomodulation in sepsis Abstract Sepsis is a life-threatening syndrome characterized by dysregulated host-immune responses, progressing through hyperinflammatory and immunosuppressive stages. Decoy receptor 3 (DcR3), a soluble member of the TNF receptor superfa... |
PMC8272888 | core_pubmed_pmc | Repurposing FDA-approved drugs against multiple proteins of SARS-CoV-2: An in silico study | Repurposing FDA-approved drugs against multiple proteins of SARS-CoV-2: An in silico study Abstract Abstract The current crisis of the COVID-19 pandemic around the world has been devastating as many lives have been lost to the novel SARS CoV-2 virus. Thus, there is an urgent need for the right therapeutic drug to curb ... |
PMC5626687 | core_pubmed_pmc | Evaluation of the heterogeneous tissue distribution of erlotinib in lung cancer using matrix-assisted laser desorption ionization mass spectrometry imaging | Evaluation of the heterogeneous tissue distribution of erlotinib in lung cancer using matrix-assisted laser desorption ionization mass spectrometry imaging Abstract Although drug distribution in tumor tissues has a significant impact on efficacy, conventional pharmacokinetic analysis has some limitations with regard to... |
PMC11337614 | core_pubmed_pmc | Targeting gut-microbiota for gastric cancer treatment: a systematic review | Targeting gut-microbiota for gastric cancer treatment: a systematic review Abstract Background Preclinical research has identified the mechanisms via which bacteria influence cancer treatment outcomes. Clinical studies have demonstrated the potential to modify the microbiome in cancer treatment. Herein, we systematical... |
PMC5125732 | core_pubmed_pmc | PBPK modeling and simulation in drug research and development | PBPK modeling and simulation in drug research and development Abstract Abstract Physiologically based pharmacokinetic (PBPK) modeling and simulation can be used to predict the pharmacokinetic behavior of drugs in humans using preclinical data. It can also explore the effects of various physiologic parameters such as ag... |
PMC12767388 | core_pubmed_pmc | Targeting NRF2 With Isoeugenol: A Promising Small Molecule for Neurodegenerative, Metabolic, and Chronic Inflammatory Disorders | Targeting NRF2 With Isoeugenol: A Promising Small Molecule for Neurodegenerative, Metabolic, and Chronic Inflammatory Disorders Abstract Oxidative stress, driven by an imbalance between oxidants and antioxidants, disrupts redox homeostasis and contributes to the development of chronic diseases, including cancer, diabet... |
PMC6853277 | core_pubmed_pmc | Using mechanistic physiologically-based pharmacokinetic models to assess prenatal drug exposure: Thalidomide versus efavirenz as case studies | Using mechanistic physiologically-based pharmacokinetic models to assess prenatal drug exposure: Thalidomide versus efavirenz as case studies Abstract Abstract Maternofoetal physiologically-based pharmacokinetic models integrating multi-compartmental maternal and foetal units were developed using Simbiology® to estimat... |
PMC8940759 | core_pubmed_pmc | A series acceleration algorithm for the gamma-Pareto (type I) convolution and related functions of interest for pharmacokinetics | A series acceleration algorithm for the gamma-Pareto (type I) convolution and related functions of interest for pharmacokinetics Abstract Abstract The gamma-Pareto type I convolution (GPC type I) distribution, which has a power function tail, was recently shown to describe the disposition kinetics of metformin in dogs ... |
PMC9868173 | core_pubmed_pmc | Pharmacological activities and mechanisms of action of hypophyllanthin: A review | Pharmacological activities and mechanisms of action of hypophyllanthin: A review Abstract Abstract Hypophyllanthin is a major lignan present in various Phyllanthus species and has been used as one of the bioactive chemical markers for quality control purposes as it contributes to their diverse pharmacological activitie... |
PMC12910213 | core_pubmed_pmc | A prospective feasibility study evaluating the implementation of model-informed precision dosing in critically ill children | A prospective feasibility study evaluating the implementation of model-informed precision dosing in critically ill children Abstract Achieving optimal antibiotic exposure in critically ill pediatric patients is difficult due to (their) dynamic physiology and variability. Conventional weight-based regimens often fail to... |
PMC9345828 | core_pubmed_pmc | The Options for Neuraxial Drug Administration | The Options for Neuraxial Drug Administration Abstract Neuraxial drug administration, i.e., the injection of drugs into the epidural or intrathecal space to produce anesthesia or analgesia, is a technique developed more than 120 years ago. Today, it still is widely used in daily practice in anesthesiology and in acute ... |
PMC11742280 | core_pubmed_pmc | A phase I study of MLN4924 and belinostat in relapsed/refractory acute myeloid leukemia or myelodysplastic syndrome | A phase I study of MLN4924 and belinostat in relapsed/refractory acute myeloid leukemia or myelodysplastic syndrome Abstract Purpose Relapsed and/or refractory acute myeloid leukemia and high-risk myelodysplastic syndrome continue to have a poor prognosis with limited treatment options despite advancements in rational ... |
PMC10652308 | core_pubmed_pmc | Efficacy and safety of abemaciclib alone and with PI3K/mTOR inhibitor LY3023414 or galunisertib versus chemotherapy in previously treated metastatic pancreatic adenocarcinoma: A randomized controlled trial | Efficacy and safety of abemaciclib alone and with PI3K/mTOR inhibitor LY3023414 or galunisertib versus chemotherapy in previously treated metastatic pancreatic adenocarcinoma: A randomized controlled trial Abstract Abstract Background Pancreatic ductal adenocarcinomas (PDAC) are characterized by frequent cell cycle pat... |
PMC9964875 | core_pubmed_pmc | A Rapid and Sensitive UHPLC–MS/MS Method for Determination of Chlorogenic Acid and Its Application to Distribution and Neuroprotection in Rat Brain | A Rapid and Sensitive UHPLC–MS/MS Method for Determination of Chlorogenic Acid and Its Application to Distribution and Neuroprotection in Rat Brain Abstract Chlorogenic acid (5-CQA) is a phenolic natural product that has been reported to improve neurobehavioral disorders and brain injury. However, its pharmacokinetics ... |
PMC11521577 | core_pubmed_pmc | Supratherapeutic International Normalized Ratio in a Patient on Warfarin Following Initiation of Brexpiprazole Pharmacotherapy: A Case Report | Supratherapeutic International Normalized Ratio in a Patient on Warfarin Following Initiation of Brexpiprazole Pharmacotherapy: A Case Report Abstract Abstract Many medications have established interactions with warfarin, potentially affecting international normalized ratio (INR) levels and increasing the risk of bleed... |
PMC12592267 | core_pubmed_pmc | Changes in the Fraction Metabolized in Children Younger than Four Years; When is Clearance Scaling for the Dominant Elimination Route in Adults Appropriate? | Changes in the Fraction Metabolized in Children Younger than Four Years; When is Clearance Scaling for the Dominant Elimination Route in Adults Appropriate? Abstract Introduction A common approach to scaling clearance from adults to children is to apply a maturation function for the dominant elimination pathway in adul... |
PMC11581887 | core_pubmed_pmc | Combined carbapenem resulted in a 4.48-fold increase in valproic acid clearance: a population pharmacokinetic model in Chinese children and adults with epilepsy or after neurosurgery | Combined carbapenem resulted in a 4.48-fold increase in valproic acid clearance: a population pharmacokinetic model in Chinese children and adults with epilepsy or after neurosurgery Abstract Abstract Our study aims to explore the pharmacokinetics of valproic acid (VPA) in Chinese patients with epilepsy or after neuros... |
PMC7819529 | core_pubmed_pmc | Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing | Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing Abstract Abstract Background The weight-band dosing in tuberculosis treatment regimen has been implemented in clinical practice for decades. Patients will receive different number of fixed dose combination tablets according to their weight-band. Howev... |
PMC12271520 | core_pubmed_pmc | Ceftazidime–Avibactam Pharmacokinetic Comparative In Vivo/In Vitro Study in a Critically Ill Children Under High‐Volume Continuous Venovenous Hemodiafiltration | Ceftazidime–Avibactam Pharmacokinetic Comparative In Vivo/In Vitro Study in a Critically Ill Children Under High‐Volume Continuous Venovenous Hemodiafiltration Abstract ABSTRACT Ceftazidime–avibactam is a novel cephalosporin/beta‐lactamase inhibitor combination developed to address increasing antimicrobial resistance. ... |
PMC6534253 | core_pubmed_pmc | Stereoselective pharmacokinetic and pharmacodynamic analysis of a CNS-active sulphamoylphenyl carbamate derivative | Stereoselective pharmacokinetic and pharmacodynamic analysis of a CNS-active sulphamoylphenyl carbamate derivative Abstract Abstract 3-Methylpentyl(4-sulphamoylphenyl)carbamate (MSPC) came as the most potent compound out of a new series of carbamates composed of phenyl-ethanol or branched aliphatic alcohols, and 4-benz... |
PMC11250107 | core_pubmed_pmc | Pharmacokinetics of Generic Pediatric Dolutegravir Dispersible Tablet in Thai Young Children Living With HIV Weighing Below Twenty Kilograms | Pharmacokinetics of Generic Pediatric Dolutegravir Dispersible Tablet in Thai Young Children Living With HIV Weighing Below Twenty Kilograms Abstract Abstract Introduction: Dolutegravir (DTG) dispersible tablet (DTG-DT) is a pediatric-friendly formulation. We aimed to describe the pharmacokinetics and virologic respons... |
PMC4932535 | core_pubmed_pmc | Non-Steroidal Anti-Inflammatory Drugs and Aspirin Therapy for the Treatment of Acute and Recurrent Idiopathic Pericarditis | Non-Steroidal Anti-Inflammatory Drugs and Aspirin Therapy for the Treatment of Acute and Recurrent Idiopathic Pericarditis Abstract Abstract Aspirin (ASA) and non-steroidal anti-inflammatory drugs (NSAIDs) are a mainstay of therapy for the treatment of idiopathic pericarditis (IP). A comprehensive review consisting of ... |
PMC12037436 | core_pubmed_pmc | Stable self-assembled oral metformin-bridged nanocochleates against hepatocellular carcinoma | Stable self-assembled oral metformin-bridged nanocochleates against hepatocellular carcinoma Abstract Abstract Despite its established anti-diabetic activity, Metformin hydrochloride (MET) has been repurposed for the management of hepatocellular carcinoma (HCC). Owing to MET high aqueous solubility and poor oral permea... |
PMC9478891 | core_pubmed_pmc | PBPK-PD modeling for the preclinical development and clinical translation of tau antibodies for Alzheimer’s disease | PBPK-PD modeling for the preclinical development and clinical translation of tau antibodies for Alzheimer’s disease Abstract Disrupted tau proteostasis and transneuronal spread is a pathological hallmark of Alzheimer’s disease. Neurodegenerative diseases remain an unmet medical need and novel disease modifying therapeu... |
PMC7982536 | core_pubmed_pmc | Individualizing Therapy in CIDP: A Mini-Review Comparing the Pharmacokinetics of Ig With SCIg and IVIg | Individualizing Therapy in CIDP: A Mini-Review Comparing the Pharmacokinetics of Ig With SCIg and IVIg Abstract Immunoglobulin (Ig) therapy is a first-line treatment for CIDP, which can be administered intravenously (IVIg) or subcutaneously (SCIg) and is often required long term. The differences between these modes of ... |
PMC7070803 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Intramuscular and Oral Betamethasone and Dexamethasone in Reproductive Age Women in India | Pharmacokinetics and Pharmacodynamics of Intramuscular and Oral Betamethasone and Dexamethasone in Reproductive Age Women in India Abstract High‐dose betamethasone and dexamethasone are standard of care treatments for women at risk of preterm delivery to improve neonatal respiratory and mortality outcomes. The dose in ... |
PMC7513528 | core_pubmed_pmc | Lung function, pharmacokinetics, and tolerability of inhaled indacaterol maleate and acetate in asthma patients | Lung function, pharmacokinetics, and tolerability of inhaled indacaterol maleate and acetate in asthma patients Abstract Background Indacaterol maleate delivered with the Breezhaler® inhalation device is a long-acting β 2 -agonist approved for chronic obstructive pulmonary disease. In the development of a once daily, i... |
PMC9329868 | core_pubmed_pmc | Is Silver the New Gold? A Systematic Review of the Preclinical Evidence of Its Use in Bone Substitutes as Antiseptic | Is Silver the New Gold? A Systematic Review of the Preclinical Evidence of Its Use in Bone Substitutes as Antiseptic Abstract Antibiotic-laden bone substitutes represent a viable option in the treatment of bone and joint infections with bone defects. In particular, the addition of silver ions or silver nanoparticles to... |
PMC9311525 | core_pubmed_pmc | Towards Improved Management of Tuberculous Bloodstream Infections: Pharmacokinetic Considerations with Suggestions for Better Treatment Outcomes | Towards Improved Management of Tuberculous Bloodstream Infections: Pharmacokinetic Considerations with Suggestions for Better Treatment Outcomes Abstract Mycobacterium tuberculosis is the leading cause of sepsis among HIV-infected adults, yet effective treatment remains a challenge. Efficacy of antituberculous drugs is... |
PMC12587311 | core_pubmed_pmc | Early Higher Plasma Regorafenib Concentration Predicts Shorter PFS in Japanese Patients With mCRC | Early Higher Plasma Regorafenib Concentration Predicts Shorter PFS in Japanese Patients With mCRC Abstract ABSTRACT The pharmacokinetics of regorafenib and its active metabolites, M2 and M5, vary widely among individual patients. However, the relationship between these plasma concentrations and therapeutic efficacy rem... |
PMC12334468 | core_pubmed_pmc | Application of Physiologically-Based Pharmacokinetic (PBPK) Model in Drug Development and in Dietary Phytochemicals | Application of Physiologically-Based Pharmacokinetic (PBPK) Model in Drug Development and in Dietary Phytochemicals Abstract Abstract Purpose of review Physiologically-based pharmacokinetic (PBPK) modeling is a powerful tool to understand drug movements throughout the human body. Unlike classical PK methods that often ... |
PMC8252714 | core_pubmed_pmc | Ibuprofen enantiomers in premature neonates with patent ductus arteriosus: Preliminary data on an unexpected pharmacokinetic profile of S (+)‐ibuprofen | Ibuprofen enantiomers in premature neonates with patent ductus arteriosus: Preliminary data on an unexpected pharmacokinetic profile of S (+)‐ibuprofen Abstract Abstract S (+)‐ibuprofen ( S ‐IBU) and R (−)‐ibuprofen ( R ‐IBU) concentrations were measured in 16 neonates with patent ductus arteriosus during a cycle of th... |
PMC10772478 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of cannabis‐based medicine in a patient population included in a randomized, placebo‐controlled, clinical trial | Pharmacokinetics and pharmacodynamics of cannabis‐based medicine in a patient population included in a randomized, placebo‐controlled, clinical trial Abstract Abstract Information on the pharmacokinetics (PK) and pharmacodynamics (PD) of orally administered cannabis‐based medicine (CBM) in capsule formulation in patien... |
PMC5418449 | core_pubmed_pmc | Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy | Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy Abstract Abstract Background: The main role of the cell cycle is to enable error-free DNA replication, chromosome segregation and cytokinesis. One of the best characterise... |
PMC8425638 | core_pubmed_pmc | In vivo trafficking of a tumor-targeting IgE antibody: molecular imaging demonstrates rapid hepatobiliary clearance compared to IgG counterpart | In vivo trafficking of a tumor-targeting IgE antibody: molecular imaging demonstrates rapid hepatobiliary clearance compared to IgG counterpart Abstract ABSTRACT IgE antibodies elicit powerful immune responses, recruiting effector cells to tumors more efficiently and with greater cytotoxicity than IgG antibodies. Conse... |
PMC12712391 | core_pubmed_pmc | The Second Mitochondria‐Derived Activator of Caspases Mimetic BI 891065 in Patients With Advanced Solid Tumors: Results From Two Phase I Studies | The Second Mitochondria‐Derived Activator of Caspases Mimetic BI 891065 in Patients With Advanced Solid Tumors: Results From Two Phase I Studies Abstract ABSTRACT Introduction BI 891065, a second mitochondria‐derived activator of caspases mimetic targets the inhibitor of apoptosis (IAP) family member cIAP1. We describe... |
PMC8465969 | core_pubmed_pmc | The Effect of Cannabis-Based Medicine on Neuropathic Pain and Spasticity in Patients with Multiple Sclerosis and Spinal Cord Injury: Study Protocol of a National Multicenter Double-Blinded, Placebo-Controlled Trial | The Effect of Cannabis-Based Medicine on Neuropathic Pain and Spasticity in Patients with Multiple Sclerosis and Spinal Cord Injury: Study Protocol of a National Multicenter Double-Blinded, Placebo-Controlled Trial Abstract Disease or acquired damage to the central nervous system frequently causes disabling spasticity ... |
PMC12757702 | core_pubmed_pmc | Enhanced Vatiquinone Bioavailability With Fatty Meals and Optimal Dosing Schedule | Enhanced Vatiquinone Bioavailability With Fatty Meals and Optimal Dosing Schedule Abstract ABSTRACT Vatiquinone, a 15‐lipoxygenase (LO) inhibitor, is an orally bioavailable small molecule being developed for the treatment of Friedreich's ataxia, a disorder characterized by high levels of oxidative stress and dysregulat... |
PMC12314501 | core_pubmed_pmc | Thigh Injections of Cabotegravir + Rilpivirine in Virally Suppressed Adults With HIV-1: A Substudy of the Phase 3b ATLAS-2M Study | Thigh Injections of Cabotegravir + Rilpivirine in Virally Suppressed Adults With HIV-1: A Substudy of the Phase 3b ATLAS-2M Study Abstract Abstract Background Cabotegravir + rilpivirine (CAB + RPV) administered via intramuscular gluteal injections is the first complete long-acting regimen for maintaining human immunode... |
PMC10343629 | core_pubmed_pmc | In Silico Studies of Novel Vemurafenib Derivatives as BRAF Kinase Inhibitors | In Silico Studies of Novel Vemurafenib Derivatives as BRAF Kinase Inhibitors Abstract BRAF inhibitors have improved the treatment of advanced or metastatic melanoma in patients that harbor a BRAF T1799A mutation. Because of new insights into the role of aberrant glycosylation in drug resistance, we designed and studied... |
PMC12789425 | core_pubmed_pmc | Discovery of thiadiazole-based small-molecule inhibitors of SARS-CoV-2 spike-ACE2 interaction through integrated computational prediction and experimental validation | Discovery of thiadiazole-based small-molecule inhibitors of SARS-CoV-2 spike-ACE2 interaction through integrated computational prediction and experimental validation Abstract Abstract The SARS-CoV-2 spike protein enables viral entry by binding to the human ACE2 receptor, making it a critical target for antiviral interv... |
PMC5644636 | core_pubmed_pmc | Mechanisms of Drug Resistance in Veterinary Oncology—A Review with an Emphasis on Canine Lymphoma | Mechanisms of Drug Resistance in Veterinary Oncology—A Review with an Emphasis on Canine Lymphoma Abstract Abstract Drug resistance (DR) is the major limiting factor in the successful treatment of systemic neoplasia with cytotoxic chemotherapy. DR can be either intrinsic or acquired, and although the development and cl... |
PMC7139065 | core_pubmed_pmc | An approach to antibiotic treatment in patients with sepsis | An approach to antibiotic treatment in patients with sepsis Abstract Abstract Sepsis is a medical emergency and life-threatening condition due to a dysregulated host response to infection, which is time-dependent and associated with unacceptably high mortality. Thus, when treating suspicious or confirmed cases of sepsi... |
PMC8282371 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution of Combined Triptolide and Paeoniflorin Regimen for Percutaneous Administration in Rats Assessed by Liquid Chromatography-Tandem Mass Spectrometry | Pharmacokinetics and Tissue Distribution of Combined Triptolide and Paeoniflorin Regimen for Percutaneous Administration in Rats Assessed by Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract Triptolide (TP) has shown potential in rheumatoid arthritis (RA) treatment, but the narrow therapeutic window limi... |
PMC9652429 | core_pubmed_pmc | Human radiolabeled mass balance studies supporting the FDA approval of new drugs | Human radiolabeled mass balance studies supporting the FDA approval of new drugs Abstract Abstract Human radiolabeled mass balance studies are an important component of the clinical pharmacology programs supporting the development of new investigational drugs. These studies allow for understanding of the absorption, di... |
PMC4685605 | core_pubmed_pmc | Historical Context and Recent Advances in Exposure-Response Estimation for Deriving Occupational Exposure Limits | Historical Context and Recent Advances in Exposure-Response Estimation for Deriving Occupational Exposure Limits Abstract Abstract Virtually no occupational exposure standards specify the level of risk for the prescribed exposure, and most occupational exposure limits are not based on quantitative risk assessment (QRA)... |
PMC10026531 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Exposure‐Response Analysis for Aripiprazole Once Monthly in Subjects With Schizophrenia | Population Pharmacokinetic Modeling and Exposure‐Response Analysis for Aripiprazole Once Monthly in Subjects With Schizophrenia Abstract Abstract An intramuscular formulation of aripiprazole monohydrate dosed once monthly (AOM) was developed to address nonadherence with the approved oral tablets. A 3‐compartment linear... |
PMC11652822 | core_pubmed_pmc | Harnessing Pharmacogenomics in Clinical Research on Psychedelic‐Assisted Therapy | Harnessing Pharmacogenomics in Clinical Research on Psychedelic‐Assisted Therapy Abstract Abstract Psychedelics have recently re‐emerged as potential treatments for various psychiatric conditions that impose major public health costs and for which current treatment options have limited efficacy. At the same time, perso... |
PMC10805834 | core_pubmed_pmc | Population pharmacokinetic modeling of ilaprazole in healthy subjects and patients with duodenal ulcer in China | Population pharmacokinetic modeling of ilaprazole in healthy subjects and patients with duodenal ulcer in China Abstract Abstract Aims: This study aimed to develop a population pharmacokinetic (PopPK) model of ilaprazole in healthy subjects and patients with duodenal ulcer in Chinese and investigate the effect of poten... |
PMC6616216 | core_pubmed_pmc | Clinical Pharmacokinetics of a Lipid-Based Formulation of Risperidone, VAL401: Analysis of a Single Dose in an Open-Label Trial of Late-Stage Cancer Patients | Clinical Pharmacokinetics of a Lipid-Based Formulation of Risperidone, VAL401: Analysis of a Single Dose in an Open-Label Trial of Late-Stage Cancer Patients Abstract Abstract Background and Objectives A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperi... |
PMC11818058 | core_pubmed_pmc | Combinatorial Effects of Cisplatin and PARP Inhibitor Olaparib on Survival, Intestinal Integrity, and Microbiome Modulation in Murine Model | Combinatorial Effects of Cisplatin and PARP Inhibitor Olaparib on Survival, Intestinal Integrity, and Microbiome Modulation in Murine Model Abstract This study investigated the effects of the poly (ADP-ribose) polymerase (PARP) inhibitor Olaparib, alone and in combination with cisplatin, on intestinal integrity, surviv... |
PMC12389047 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Piperacillin/Tazobactam in Healthy Adults and Exploration of Optimal Dosing Strategies | Population Pharmacokinetic Modeling of Piperacillin/Tazobactam in Healthy Adults and Exploration of Optimal Dosing Strategies Abstract Abstract Background/Objectives: Current dosing recommendations for piperacillin/tazobactam suggest adjustments only for patients with creatinine clearance (CrCl) below 40 mL/min, potent... |
PMC11658602 | core_pubmed_pmc | In vivo imaging and pharmacokinetics of percutaneously injected ultrasound and X-ray imageable thermosensitive hydrogel loaded with doxorubicin versus free drug in swine | In vivo imaging and pharmacokinetics of percutaneously injected ultrasound and X-ray imageable thermosensitive hydrogel loaded with doxorubicin versus free drug in swine Abstract Intratumoral injections often lack visibility, leading to unpredictable outcomes such as incomplete tumor coverage, off-target drug delivery ... |
PMC10869334 | core_pubmed_pmc | In vitro pharmacokinetics/pharmacodynamics of the β-lactamase inhibitor, durlobactam, in combination with sulbactam against Acinetobacter baumannii-calcoaceticus complex | In vitro pharmacokinetics/pharmacodynamics of the β-lactamase inhibitor, durlobactam, in combination with sulbactam against Acinetobacter baumannii-calcoaceticus complex Abstract ABSTRACT Infections caused by Acinetobacter baumannii are increasingly multidrug resistant and associated with high rates of morbidity and mo... |
PMC7970330 | core_pubmed_pmc | Towards a mechanistic understanding of reciprocal drug–microbiome interactions | Towards a mechanistic understanding of reciprocal drug–microbiome interactions Abstract Abstract Broad‐spectrum antibiotics target multiple gram‐positive and gram‐negative bacteria, and can collaterally damage the gut microbiota. Yet, our knowledge of the extent of damage, the antibiotic activity spectra, and the resis... |
PMC12587533 | core_pubmed_pmc | A first-in-human phase I study to evaluate the safety, tolerability, and pharmacokinetics of a novel anti-influenza agent suraxavir marboxil in healthy Chinese subjects | A first-in-human phase I study to evaluate the safety, tolerability, and pharmacokinetics of a novel anti-influenza agent suraxavir marboxil in healthy Chinese subjects Abstract ABSTRACT Suraxavir marboxil (GP681) is a prodrug of a novel polymerase acidic protein inhibitor, and its metabolite GP1707D07 prevents the rep... |
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