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PMC5953989 | core_pubmed_pmc | Pharmacodynamic modeling of cardiac biomarkers in breast cancer patients treated with anthracycline and trastuzumab regimens | Pharmacodynamic modeling of cardiac biomarkers in breast cancer patients treated with anthracycline and trastuzumab regimens Abstract Trastuzumab is associated with cardiotoxicity, manifesting as a decrease of the left-ventricular ejection fraction (LVEF). Administration of anthracyclines prior to trastuzumab increases... |
PMC6755487 | core_pubmed_pmc | Pharmacokinetics of ropivacaine in elderly patients receiving fascia iliaca compartment block | Pharmacokinetics of ropivacaine in elderly patients receiving fascia iliaca compartment block Abstract Abstract Local anesthetic of ropivacaine was demonstrated to reduce the postoperative pain in elderly patients. This study investigated the pharmacokinetics of ropivacaine at different concentrations in elderly patien... |
PMC9671373 | core_pubmed_pmc | Computational analysis of 5-fluorouracil anti-tumor activity in colon cancer using a mechanistic pharmacokinetic/pharmacodynamic model | Computational analysis of 5-fluorouracil anti-tumor activity in colon cancer using a mechanistic pharmacokinetic/pharmacodynamic model Abstract Abstract 5-Fluorouracil (5-FU) is a standard chemotherapeutic agent to treat solid cancers such as breast, colon, head, and neck. Computational modeling plays an essential role... |
PMC9299819 | core_pubmed_pmc | Meropenem pharmacokinetics in critically ill patients with or without burn treated with or without continuous veno‐venous haemofiltration | Meropenem pharmacokinetics in critically ill patients with or without burn treated with or without continuous veno‐venous haemofiltration Abstract Introduction Severe burn injury involves widespread skin and tissue damage leading to systemic inflammation, hypermetabolism and multi‐organ failure. The hypermetabolic phas... |
PMC7845031 | core_pubmed_pmc | Safety of natural anthraquinone emodin: an assessment in mice | Safety of natural anthraquinone emodin: an assessment in mice Abstract Background Emodin, a natural anthraquinone, has shown potential as an effective therapeutic agent in the treatment of many diseases including cancer. However, its clinical development is hindered by uncertainties surrounding its potential toxicity. ... |
PMC4875998 | core_pubmed_pmc | Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin | Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin Abstract RNA virus infections can lead to the onset of severe diseases such as fever with haemorrhage, multiorgan failure, and mortality. The emergence and reemergence of RNA viruses continue to pose a significant public health threat worldwide with p... |
PMC11865242 | core_pubmed_pmc | A single point mutation on FLT3L-Fc protein increases the risk of immunogenicity | A single point mutation on FLT3L-Fc protein increases the risk of immunogenicity Abstract Abstract Introduction As a crucial asset for human health and modern medicine, an increasing number of biotherapeutics are entering the clinic. However, due to their complexity, these drugs have a higher potential to be immunogeni... |
PMC5587199 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics of oral omaveloxolone (RTA 408), a synthetic triterpenoid, in a first-in-human trial of patients with advanced solid tumors | Safety, pharmacokinetics, and pharmacodynamics of oral omaveloxolone (RTA 408), a synthetic triterpenoid, in a first-in-human trial of patients with advanced solid tumors Abstract Abstract Background Omaveloxolone is a semisynthetic oleanane triterpenoid that potently activates Nrf2 with subsequent antioxidant function... |
PMC5543507 | core_pubmed_pmc | Phase I study of glasdegib ( PF ‐04449913), an oral smoothened inhibitor, in Japanese patients with select hematologic malignancies | Phase I study of glasdegib ( PF ‐04449913), an oral smoothened inhibitor, in Japanese patients with select hematologic malignancies Abstract The hedgehog signaling pathway regulates multiple morphogenetic processes during embryogenesis. Aberrant activation of the hedgehog pathway signal transduction in adult tissues is... |
PMC6901225 | core_pubmed_pmc | Prevalence of drug–drug interaction in atrial fibrillation patients based on a large claims data | Prevalence of drug–drug interaction in atrial fibrillation patients based on a large claims data Abstract This study aimed to compare and determine the prevalence of drug–drug interaction (DDI) and bleeding rate in atrial fibrillation (AF) patients receiving anticoagulants in a clinical setting. We used large claims da... |
PMC11832029 | core_pubmed_pmc | Safety, Pharmacokinetics and Target Engagement of a Novel Brain Penetrant RIPK1 Inhibitor (SIR9900) in Healthy Adults and Elderly Participants | Safety, Pharmacokinetics and Target Engagement of a Novel Brain Penetrant RIPK1 Inhibitor (SIR9900) in Healthy Adults and Elderly Participants Abstract ABSTRACT Receptor‐interacting serine/threonine kinase 1 (RIPK1) regulates inflammatory signaling and induces apoptosis and necroptosis. Pharmacological inhibition of RI... |
PMC9091613 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of VIS649 (Sibeprenlimab), an APRIL-Neutralizing IgG 2 Monoclonal Antibody, in Healthy Volunteers | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of VIS649 (Sibeprenlimab), an APRIL-Neutralizing IgG 2 Monoclonal Antibody, in Healthy Volunteers Abstract Introduction VIS649 (sibeprenlimab), a humanized IgG 2 monoclonal antibody that inhibits APRIL, is being developed as a potential treatment for IgA neph... |
PMC5534040 | core_pubmed_pmc | Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans ( Cygnus atratus ) | Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans ( Cygnus atratus ) Abstract Background The objective of this study is to investigate pharmacokinetics and dose regimens of cefquinome in black swans following intravenous (IV) and intramuscular (IM) administratio... |
PMC4488474 | core_pubmed_pmc | The Effect of Rifampin on the Pharmacokinetics of Edoxaban in Healthy Adults | The Effect of Rifampin on the Pharmacokinetics of Edoxaban in Healthy Adults Abstract Abstract Background and Objective The oral direct factor Xa inhibitor edoxaban is a P-glycoprotein (P-gp) substrate metabolized via carboxylesterase-1 and cytochrome P450 (CYP) 3A4/5. The effect of rifampin-induced induction of P-gp a... |
PMC5648081 | core_pubmed_pmc | First-in-Man Evaluation of 124 I-PGN650: A PET Tracer for Detecting Phosphatidylserine as a Biomarker of the Solid Tumor Microenvironment | First-in-Man Evaluation of 124 I-PGN650: A PET Tracer for Detecting Phosphatidylserine as a Biomarker of the Solid Tumor Microenvironment Abstract Abstract Purpose: PGN650 is a F(ab′) 2 antibody fragment that targets phosphatidylserine (PS), a marker normally absent that becomes exposed on tumor cells and tumor vascula... |
PMC10415223 | core_pubmed_pmc | A physiologically based pharmacokinetic model of cefepime to predict its pharmacokinetics in healthy, pediatric and disease populations | A physiologically based pharmacokinetic model of cefepime to predict its pharmacokinetics in healthy, pediatric and disease populations Abstract The physiologically based pharmacokinetic modeling (PBPK) approach can predict drug pharmacokinetics (PK) by combining changes in blood flow and pathophysiological alterations... |
PMC8048531 | core_pubmed_pmc | Phase 1 Studies to Define the Safety, Tolerability, and Pharmacokinetic and Pharmacodynamic Profiles of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone in Healthy Volunteers | Phase 1 Studies to Define the Safety, Tolerability, and Pharmacokinetic and Pharmacodynamic Profiles of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone in Healthy Volunteers Abstract Abstract Apararenone is a long‐acting, nonsteroidal mineralocorticoid receptor antagonist (MRA). The safety, tolerabil... |
PMC10582325 | core_pubmed_pmc | Coadministration of bedaquiline and pyrifazimine reduce exposure to toxic metabolite N-desmethyl bedaquiline | Coadministration of bedaquiline and pyrifazimine reduce exposure to toxic metabolite N-desmethyl bedaquiline Abstract Abstract Background: A new, effective anti-tuberculosis (TB) regimen containing bedaquiline (BDQ) and pyrifazimine (TBI-166) has been recommended for a phase IIb clinical trial. Preclinical drug–drug in... |
PMC4118627 | core_pubmed_pmc | Expression, purification, and characterization of rhTyrRS | Expression, purification, and characterization of rhTyrRS Abstract Abstract Background Aminoacyl-tRNA synthetases (AARSs) catalyze the first step of protein synthesis. Emerging evidence indicates that AARSs may have additional functions, playing a role in signal transduction pathways regulating thrombopoiesis and infla... |
PMC9289467 | core_pubmed_pmc | A Novel Multifunctional 5,6-Dimethoxy-Indanone-Chalcone-Carbamate Hybrids Alleviates Cognitive Decline in Alzheimer’s Disease by Dual Inhibition of Acetylcholinesterase and Inflammation | A Novel Multifunctional 5,6-Dimethoxy-Indanone-Chalcone-Carbamate Hybrids Alleviates Cognitive Decline in Alzheimer’s Disease by Dual Inhibition of Acetylcholinesterase and Inflammation Abstract Abstract Backgrounds Alzheimer’s disease (AD) is a multifactorial neurodegenerative disease. The treatment of AD through mult... |
PMC9377148 | core_pubmed_pmc | Relationship Between Linezolid Exposure and the Typical Clinical Laboratory Safety and Bacterial Clearance in Chinese Pediatric Patients | Relationship Between Linezolid Exposure and the Typical Clinical Laboratory Safety and Bacterial Clearance in Chinese Pediatric Patients Abstract Abstract Objectives: There have been limited studies concerning the safety and efficacy of linezolid (LZD) in children. This study aimed to evaluate the association between L... |
PMC10286764 | core_pubmed_pmc | A phase 1b/2 clinical study of marstacimab, targeting human tissue factor pathway inhibitor, in haemophilia | A phase 1b/2 clinical study of marstacimab, targeting human tissue factor pathway inhibitor, in haemophilia Abstract Summary A phase 1b/2, three‐month study of marstacimab, a human monoclonal antibody targeting tissue factor pathway inhibitor (TFPI), was conducted in participants with haemophilia A or B, with or withou... |
PMC6274205 | core_pubmed_pmc | Simultaneous Determination of Four Tanshinones by UPLC-TQ/MS and Their Pharmacokinetic Application after Administration of Single Ethanol Extract of Danshen Combined with Water Extract in Normal and Adenine-Induced Chronic Renal Failure Rats | Simultaneous Determination of Four Tanshinones by UPLC-TQ/MS and Their Pharmacokinetic Application after Administration of Single Ethanol Extract of Danshen Combined with Water Extract in Normal and Adenine-Induced Chronic Renal Failure Rats Abstract Salvia miltiorrhiza , one of the major traditional Chinese medicines,... |
PMC9996834 | core_pubmed_pmc | Global estimates and determinants of antituberculosis drug pharmacokinetics in children and adolescents: a systematic review and individual patient data meta-analysis | Global estimates and determinants of antituberculosis drug pharmacokinetics in children and adolescents: a systematic review and individual patient data meta-analysis Abstract Abstract Background Suboptimal exposure to antituberculosis (anti-TB) drugs has been associated with unfavourable treatment outcomes. We aimed t... |
PMC7969127 | core_pubmed_pmc | Development of a Gestational and Lactational Physiologically Based Pharmacokinetic (PBPK) Model for Perfluorooctane Sulfonate (PFOS) in Rats and Humans and Its Implications in the Derivation of Health-Based Toxicity Values | Development of a Gestational and Lactational Physiologically Based Pharmacokinetic (PBPK) Model for Perfluorooctane Sulfonate (PFOS) in Rats and Humans and Its Implications in the Derivation of Health-Based Toxicity Values Abstract Background: There is a great concern on potential adverse effects of exposure to perfluo... |
PMC7319013 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and pharmacodynamics of the anti‐CD38 cytolytic antibody TAK‐079 in healthy subjects | Safety, tolerability, pharmacokinetics and pharmacodynamics of the anti‐CD38 cytolytic antibody TAK‐079 in healthy subjects Abstract Aims This investigation characterised tolerability, pharmacokinetics and pharmacodynamics of the anti‐CD38 antibody TAK‐079. Methods A randomised, double‐blind, placebo‐controlled trial o... |
PMC7816587 | core_pubmed_pmc | Inhibition of drug-metabolizing enzymes by Qingfei Paidu decoction: Implication of herb-drug interactions in COVID-19 pharmacotherapy | Inhibition of drug-metabolizing enzymes by Qingfei Paidu decoction: Implication of herb-drug interactions in COVID-19 pharmacotherapy Abstract Abstract Corona Virus Disease 2019 (COVID-19) has spread all over the world and brings significantly negative effects on human health. To fight against COVID-19 in a more effici... |
PMC11429322 | core_pubmed_pmc | Precision Dosing of Meropenem in Adults with Normal Renal Function: Insights from a Population Pharmacokinetic and Monte Carlo Simulation Study | Precision Dosing of Meropenem in Adults with Normal Renal Function: Insights from a Population Pharmacokinetic and Monte Carlo Simulation Study Abstract This study aimed to develop a population pharmacokinetic (PK) model for meropenem in healthy adults and explore optimal dosing regimens for patients with normal renal ... |
PMC9715618 | core_pubmed_pmc | The pharmacokinetics profiles, pharmacological properties, and toxicological risks of dehydroevodiamine: A review | The pharmacokinetics profiles, pharmacological properties, and toxicological risks of dehydroevodiamine: A review Abstract Abstract Dehydroevodiamine (DHE) is a quinazoline alkaloid isolated from Evodiae Fructus (EF, Wuzhuyu in Chinese, Rutaceae family), a well-known traditional Chinese medicine (TCM) which is clinical... |
PMC6134108 | core_pubmed_pmc | Nystatin-like Pseudonocardia polyene B1, a novel disaccharide-containing antifungal heptaene antibiotic | Nystatin-like Pseudonocardia polyene B1, a novel disaccharide-containing antifungal heptaene antibiotic Abstract Abstract Polyene macrolides such as nystatin A1 and amphotericin B belong to a large family of very valuable antifungal polyketide compounds typically produced by soil actinomycetes. Recently, nystatin-like ... |
PMC10466232 | core_pubmed_pmc | Pharmacokinetics of meloxicam in pigeons after single intravenous, oral, and intramuscular administration | Pharmacokinetics of meloxicam in pigeons after single intravenous, oral, and intramuscular administration Abstract Abstract This study aimed to determine the pharmacokinetics of meloxicam in pigeons. Twenty-four 7-wk-old meat pigeons ( Columba livia ) were randomly divided into 3 groups (PO, IM, and IV) and given a sin... |
PMC12916870 | core_pubmed_pmc | Antibody–Antibiotic Conjugates: Mechanisms, Clinical Progress, and Next‐Generation Strategies Against Multidrug‐Resistant Bacterial Infections | Antibody–Antibiotic Conjugates: Mechanisms, Clinical Progress, and Next‐Generation Strategies Against Multidrug‐Resistant Bacterial Infections Abstract ABSTRACT The rise of multidrug‐resistant (MDR) bacterial pathogens presents a critical challenge to global health, highlighting the need for innovative therapeutic stra... |
PMC11016567 | core_pubmed_pmc | Safety, Tolerability, and Pharmacodynamics of the ADAMTS ‐5 Nanobody M6495 : Two Phase 1, Single‐Center , Double‐Blind , Randomized, Placebo‐Controlled Studies in Healthy Subjects and Patients With Osteoarthritis | Safety, Tolerability, and Pharmacodynamics of the ADAMTS ‐5 Nanobody M6495 : Two Phase 1, Single‐Center , Double‐Blind , Randomized, Placebo‐Controlled Studies in Healthy Subjects and Patients With Osteoarthritis Abstract Objective To assess the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of single and mul... |
PMC11279916 | core_pubmed_pmc | Application of 99m Tc-Labeled WL12 Peptides as a Tumor PD-L1-Targeted SPECT Imaging Agent: Kit Formulation, Preclinical Evaluation, and Study on the Influence of Coligands | Application of 99m Tc-Labeled WL12 Peptides as a Tumor PD-L1-Targeted SPECT Imaging Agent: Kit Formulation, Preclinical Evaluation, and Study on the Influence of Coligands Abstract Abstract With the development of PD-1/PD-L1 immune checkpoint inhibitor therapy, the ability to monitor PD-L1 expression in the tumor micro... |
PMC12910643 | core_pubmed_pmc | Diastereomeric Branched-Ester dBET1 Analogs Exhibit Conformation-Dependent Differences in Passive Membrane Permeability | Diastereomeric Branched-Ester dBET1 Analogs Exhibit Conformation-Dependent Differences in Passive Membrane Permeability Abstract Proteolysis-targeting chimeras (PROTACs) represent a promising therapeutic modality, but their clinical translation is often hindered by poor pharmacokinetic properties associated with their ... |
PMC12274254 | core_pubmed_pmc | Physiologically-based pharmacokinetic model for predicting drug-drug interactions perpetrated by posaconazole in healthy subjects with normal weight and obesity: Concomitant use and washout | Physiologically-based pharmacokinetic model for predicting drug-drug interactions perpetrated by posaconazole in healthy subjects with normal weight and obesity: Concomitant use and washout Abstract Abstract Posaconazole is an effective broad-spectrum triazole antifungal used as prophylaxis or to treat invasive Aspergi... |
PMC12127401 | core_pubmed_pmc | Gastrodin: a potential natural product for the prevention and treatment of cerebral ischemia-reperfusion injury | Gastrodin: a potential natural product for the prevention and treatment of cerebral ischemia-reperfusion injury Abstract Ethnopharmacological relevance Gastrodin is the main bioactive metabolite of Gastrodia elata Blume of traditional Chinese medicine, which has pharmacological effects such as anti-inflammatory, antiox... |
PMC10147368 | core_pubmed_pmc | An integrated computational approach towards novel drugs discovery against polyketide synthase 13 thioesterase domain of Mycobacterium tuberculosis | An integrated computational approach towards novel drugs discovery against polyketide synthase 13 thioesterase domain of Mycobacterium tuberculosis Abstract The acquired drug resistance by Mycobacterium tuberculosis (M. tuberculosis) to antibiotics urges the need for developing novel anti- M. tuberculosis drugs that po... |
PMC11792745 | core_pubmed_pmc | Quantitation of the DNA-dependent protein kinase inhibitor peposertib (M3814) and metabolite in human plasma by LC–MS/MS | Quantitation of the DNA-dependent protein kinase inhibitor peposertib (M3814) and metabolite in human plasma by LC–MS/MS Abstract Abstract The DNA-dependent protein kinase (DNA-PK) is an abundant nuclear protein that mediates DNA double-strand break repair by nonhomologous end joining (NHEJ). As such, DNA-PK is critica... |
PMC10416407 | core_pubmed_pmc | An extension of the BioAssay Ontology to include pharmacokinetic/pharmacodynamic terminology for the enrichment of scientific workflows | An extension of the BioAssay Ontology to include pharmacokinetic/pharmacodynamic terminology for the enrichment of scientific workflows Abstract Abstract With the capacity to produce and record data electronically, Scientific research and the data associated with it have grown at an unprecedented rate. However, despite... |
PMC9441134 | core_pubmed_pmc | First-in-Human Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Rapidly Developed SARS-CoV-2 Therapeutic Antibody, AOD01, in Healthy Adults | First-in-Human Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Rapidly Developed SARS-CoV-2 Therapeutic Antibody, AOD01, in Healthy Adults Abstract Abstract Introduction AOD01 is a novel, fully human immunoglobulin (Ig) G1 neutralizing monoclonal antibody that was developed as a ther... |
PMC11788250 | core_pubmed_pmc | Multi‐organ kinetic modeling for Na[ 18 F]F pre‐clinical total‐body PET studies | Multi‐organ kinetic modeling for Na[ 18 F]F pre‐clinical total‐body PET studies Abstract Abstract Background Total‐body positron emission tomography (PET), already well‐established in the pre‐clinical setting, makes it possible to study multi‐parameters in biological systems as a whole, rather than focusing on single t... |
PMC12129013 | core_pubmed_pmc | Targeting AGE-RAGE Signaling Pathway with Hujin Decoction Ameliorates MAFLD in HepG2 Cells | Targeting AGE-RAGE Signaling Pathway with Hujin Decoction Ameliorates MAFLD in HepG2 Cells Abstract Abstract Purpose To explore the mechanism and substance basis of HJD for the treatment of MAFLD based on system pharmacology. Patients and Methods The ingredients of HJD in vitro and in vivo were detected by UPLC-MS/MS, ... |
PMC10803696 | core_pubmed_pmc | Physiologically based radiopharmacokinetic (PBRPK) modeling to simulate and analyze radiopharmaceutical therapies: studies of non-linearities, multi-bolus injections, and albumin binding | Physiologically based radiopharmacokinetic (PBRPK) modeling to simulate and analyze radiopharmaceutical therapies: studies of non-linearities, multi-bolus injections, and albumin binding Abstract Background We aimed to develop a publicly shared computational physiologically based pharmacokinetic (PBPK) model to reliabl... |
PMC4619308 | core_pubmed_pmc | Model-based adaptive phase I trial design of post-transplant decitabine maintenance in myelodysplastic syndrome | Model-based adaptive phase I trial design of post-transplant decitabine maintenance in myelodysplastic syndrome Abstract Background This report focuses on the adaptive phase I trial design aimed to find the clinically applicable dose for decitabine maintenance treatment after allogeneic hematopoietic stem cell transpla... |
PMC3762800 | core_pubmed_pmc | CK2 Inhibitor CX-4945 Blocks TGF-β1-Induced Epithelial-to-Mesenchymal Transition in A549 Human Lung Adenocarcinoma Cells | CK2 Inhibitor CX-4945 Blocks TGF-β1-Induced Epithelial-to-Mesenchymal Transition in A549 Human Lung Adenocarcinoma Cells Abstract Background The epithelial-to-mesenchymal transition (EMT) is a major phenotype of cancer metastasis and invasion. As a druggable cancer target, the inhibition of protein kinase CK2 (formally... |
PMC11964176 | core_pubmed_pmc | First-in-Human Phase I Study of a CD16A Bispecific Innate Cell Engager, AFM24, Targeting EGFR-Expressing Solid Tumors | First-in-Human Phase I Study of a CD16A Bispecific Innate Cell Engager, AFM24, Targeting EGFR-Expressing Solid Tumors Abstract Abstract Purpose: Innate immune cell–based therapies have shown promising antitumor activity against solid and hematologic malignancies. AFM24, a bispecific innate cell engager, binds CD16A on ... |
PMC5591809 | core_pubmed_pmc | Successful Use of [ 14 C]Paracetamol Microdosing to Elucidate Developmental Changes in Drug Metabolism | Successful Use of [ 14 C]Paracetamol Microdosing to Elucidate Developmental Changes in Drug Metabolism Abstract Abstract Background We previously showed the practical and ethical feasibility of using [ 14 C]-microdosing for pharmacokinetic studies in children. We now aimed to show that this approach can be used to eluc... |
PMC9476706 | core_pubmed_pmc | Integrating pharmacokinetics and network analysis to investigate the mechanism of Moutan Cortex in blood-heat and blood stasis syndrome | Integrating pharmacokinetics and network analysis to investigate the mechanism of Moutan Cortex in blood-heat and blood stasis syndrome Abstract Abstract Background Raw Moutan Cortex (RMC) has been used in China and other Asian countries for thousands of years. Its medical application is the treatment of cooling blood ... |
PMC6983174 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution of Anwuligan in Rats after Intravenous and Intragastric Administration by Liquid Chromatography-Mass Spectrometry | Pharmacokinetics and Tissue Distribution of Anwuligan in Rats after Intravenous and Intragastric Administration by Liquid Chromatography-Mass Spectrometry Abstract Anwuligan, a natural 2,3-dibenzylbutane lignan from the nutmeg mace of Myristica fragans , has been proved to possess a broad range of pharmacological effec... |
PMC11884763 | core_pubmed_pmc | Phase 2b program with sonlicromanol in patients with mitochondrial disease due to m.3243A>G mutation | Phase 2b program with sonlicromanol in patients with mitochondrial disease due to m.3243A>G mutation Abstract Abstract Mitochondrial disease incorporates a group of rare conditions with no approved treatment to date, except for Leber hereditary optic neuropathy. Therapeutic options to alleviate the symptoms of mitochon... |
PMC12298228 | core_pubmed_pmc | Modeling the Influence of CYP2C9 and ABCB1 Gene Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Losartan | Modeling the Influence of CYP2C9 and ABCB1 Gene Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Losartan Abstract Abstract Background/Objectives: Hypertension is a pathological condition characterized by elevated systolic and/or diastolic blood pressure. A range of pharmacotherapeutic agents are available... |
PMC11891644 | core_pubmed_pmc | Safety and Antitumor Activity of a Novel aCD25 Treg Depleter RG6292 as a Single Agent and in Combination with Atezolizumab in Patients with Solid Tumors | Safety and Antitumor Activity of a Novel aCD25 Treg Depleter RG6292 as a Single Agent and in Combination with Atezolizumab in Patients with Solid Tumors Abstract Abstract Purpose: Therapeutic depletion of immunosuppressive regulatory T cells (Treg) may overcome resistance to cancer immunotherapies. RG6292 is an anti-CD... |
PMC4501287 | core_pubmed_pmc | Critical appraisal of dabigatran in the treatment of deep vein thrombosis and pulmonary embolism | Critical appraisal of dabigatran in the treatment of deep vein thrombosis and pulmonary embolism Abstract Objective To compare the safety and efficacy of dabigatran to warfarin for the treatment of deep vein thrombosis and pulmonary embolism. Background Venous thromboembolism (VTE) is a disease comprised of two conditi... |
PMC6940354 | core_pubmed_pmc | Comparative Assessment of the New PDE7 Inhibitor – GRMS-55 and Lisofylline in Animal Models of Immune-Related Disorders: A PK/PD Modeling Approach | Comparative Assessment of the New PDE7 Inhibitor – GRMS-55 and Lisofylline in Animal Models of Immune-Related Disorders: A PK/PD Modeling Approach Abstract Purpose This study aimed to assess the activity of two phosphodiesterase (PDE) inhibitors, namely GRMS-55 and racemic lisofylline ((±)-LSF)) in vitro and in animal ... |
PMC7230214 | core_pubmed_pmc | Interindividual Variability of Apixaban Plasma Concentrations: Influence of Clinical and Genetic Factors in a Real-Life Cohort of Atrial Fibrillation Patients | Interindividual Variability of Apixaban Plasma Concentrations: Influence of Clinical and Genetic Factors in a Real-Life Cohort of Atrial Fibrillation Patients Abstract Abstract (1) Background: Prescribing apixaban for stroke prevention has significantly increased in patients with non-valvular atrial fibrillation (NVAF)... |
PMC12583444 | core_pubmed_pmc | Computational and pharmacophore-based study of Camellia sinensis phytochemicals targeting BRAF in melanoma | Computational and pharmacophore-based study of Camellia sinensis phytochemicals targeting BRAF in melanoma Abstract Melanoma is the deadliest kind and most invasive form of skin cancer caused by exposure to UV light and mutation in BRAF signaling protein. Plant-derived phytochemicals have several anticancer properties ... |
PMC8959905 | core_pubmed_pmc | Evaluation and Application of Population Pharmacokinetic Models for Identifying Delayed Methotrexate Elimination in Patients With Primary Central Nervous System Lymphoma | Evaluation and Application of Population Pharmacokinetic Models for Identifying Delayed Methotrexate Elimination in Patients With Primary Central Nervous System Lymphoma Abstract Abstract Objective: Several population pharmacokinetic (popPK) models have been developed to determine the sources of methotrexate (MTX) PK v... |
PMC7716044 | core_pubmed_pmc | Human equivalent dose of oral 4-aminopyridine differentiates nerve crush injury from transection injury and improves post-injury function in mice | Human equivalent dose of oral 4-aminopyridine differentiates nerve crush injury from transection injury and improves post-injury function in mice Abstract Abstract 4-Aminopyridine (4-AP), an FDA-approved drug for the symptomatic treatment of multiple sclerosis, is used to improve neuromuscular function in patients with... |
PMC11739593 | core_pubmed_pmc | Safety and efficacy of trifluridine/tipiracil +/− bevacizumab plus XB2001 (anti-IL-1α antibody): a single-center phase 1 trial | Safety and efficacy of trifluridine/tipiracil +/− bevacizumab plus XB2001 (anti-IL-1α antibody): a single-center phase 1 trial Abstract Abstract In the tumour microenvironment, IL-1α promotes neoangiogenesis, matrix remodelling, tumour proliferation, chemoresistance, and metastases. Highly expressed in human colorectal... |
PMC12598559 | core_pubmed_pmc | Absorption characteristics and in vivo behavior of astaxanthin isomers: insights from the administration of highly purified (all- E )-, (9 Z )-, and (13 Z )-astaxanthin in male mice | Absorption characteristics and in vivo behavior of astaxanthin isomers: insights from the administration of highly purified (all- E )-, (9 Z )-, and (13 Z )-astaxanthin in male mice Abstract Astaxanthin, a xanthophyll carotenoid with potent antioxidant properties, exists in multiple geometrical isomers whose difference... |
PMC5303333 | core_pubmed_pmc | Dental management of patients taking novel oral anticoagulants (NOAs): Dabigatran | Dental management of patients taking novel oral anticoagulants (NOAs): Dabigatran Abstract Abstract Background A new group of oral anticoagulants (dabigatran, rivaroxaban, apixaban and edoxaban) with clear advantages over classic dicoumarin oral anticoagulants (warfarin and acenocoumarol) has been developed in recent y... |
PMC4234270 | core_pubmed_pmc | A Phase 1 Study of 131 I-CLR1404 in Patients with Relapsed or Refractory Advanced Solid Tumors: Dosimetry, Biodistribution, Pharmacokinetics, and Safety | A Phase 1 Study of 131 I-CLR1404 in Patients with Relapsed or Refractory Advanced Solid Tumors: Dosimetry, Biodistribution, Pharmacokinetics, and Safety Abstract Abstract Introduction 131 I-CLR1404 is a small molecule that combines a tumor-targeting moiety with a therapeutic radioisotope. The primary aim of this phase ... |
PMC5487860 | core_pubmed_pmc | RPC4046, A Novel Anti-interleukin-13 Antibody, Blocks IL-13 Binding to IL-13 α1 and α2 Receptors: A Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation First-in-Human Study | RPC4046, A Novel Anti-interleukin-13 Antibody, Blocks IL-13 Binding to IL-13 α1 and α2 Receptors: A Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation First-in-Human Study Abstract Abstract Introduction A unique anti-interleukin (IL)-13 monoclonal antibody, RPC4046, was generated on the basis of differential... |
PMC6374939 | core_pubmed_pmc | Stereoselectivity evaluation of chiral chitosan microspheres delivery system containing rac-KET in vitro and in vivo | Stereoselectivity evaluation of chiral chitosan microspheres delivery system containing rac-KET in vitro and in vivo Abstract Abstract The influence of chiral excipient D-chitosan (CS) on the stereoselective release of racemic ketoprofen (rac-KET) microspheres has been investigated in comparison to those microspheres c... |
PMC8529037 | core_pubmed_pmc | Effects of Cytochrome P450 and Transporter Polymorphisms on the Bioavailability and Safety of Dutasteride and Tamsulosin | Effects of Cytochrome P450 and Transporter Polymorphisms on the Bioavailability and Safety of Dutasteride and Tamsulosin Abstract Abstract Dutasteride and tamsulosin are one of the first-line combination therapies for the management of benign prostatic hyperplasia (BPH). Despite being more effective than monotherapies,... |
PMC5876239 | core_pubmed_pmc | Anti-gout Potential of Malaysian Medicinal Plants | Anti-gout Potential of Malaysian Medicinal Plants Abstract Gout is a type of arthritis that causes painful inflammation in one or more joints. In gout, elevation of uric acid in the blood triggers the formation of crystals, causing joint pain. Malaysia is a mega-biodiversity country that is rich in medicinal plants spe... |
PMC9547536 | core_pubmed_pmc | An open-access data set of pig skin anatomy and physiology for modelling purposes | An open-access data set of pig skin anatomy and physiology for modelling purposes Abstract Abstract The use of animal as opposed to human skin for in vitro permeation testing (IVPT) is an alternative, which can reduce logistical and economic issues. However, this surrogate also has ethical considerations and may not pr... |
PMC10499368 | core_pubmed_pmc | Calcifediol in the management of vitamin D deficiency-related skeletal and extraskeletal diseases: overview and clinical cases | Calcifediol in the management of vitamin D deficiency-related skeletal and extraskeletal diseases: overview and clinical cases Abstract Abstract As well as being essential for musculoskeletal health, vitamin D is involved in numerous other physiological processes. Poor vitamin D status is linked to a wide range of dise... |
PMC4342764 | core_pubmed_pmc | Single-dose new insulin glargine 300 U/ml provides prolonged, stable glycaemic control in Japanese and European people with type 1 diabetes | Single-dose new insulin glargine 300 U/ml provides prolonged, stable glycaemic control in Japanese and European people with type 1 diabetes Abstract Aims Two single-dose studies were conducted in Japan and Europe to compare the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of new insulin glargine 300 U/ml (Gla... |
PMC7540588 | core_pubmed_pmc | Ultra rapid lispro lowers postprandial glucose and more closely matches normal physiological glucose response compared to other rapid insulin analogues: A phase 1 randomized, crossover study | Ultra rapid lispro lowers postprandial glucose and more closely matches normal physiological glucose response compared to other rapid insulin analogues: A phase 1 randomized, crossover study Abstract Abstract Aims To compare the pharmacokinetic (PK) and glucodynamic (GD) characteristics of ultra rapid lispro (URLi; Eli... |
PMC12486195 | core_pubmed_pmc | Pharmacokinetic and Bioequivalence Evaluation of Two Sitagliptin Tablets With Different Salts in Healthy Subjects | Pharmacokinetic and Bioequivalence Evaluation of Two Sitagliptin Tablets With Different Salts in Healthy Subjects Abstract Abstract The objective of the current study was to evaluate the rate and extent of absorption of a test formulation (sitagliptin hydrochloride) and a reference formulation (sitagliptin phosphate). ... |
PMC10644045 | core_pubmed_pmc | Advances in the pharmacological effects and molecular mechanisms of emodin in the treatment of metabolic diseases | Advances in the pharmacological effects and molecular mechanisms of emodin in the treatment of metabolic diseases Abstract Abstract Rhubarb palmatum L. , Polygonum multijiorum Thunb ., and Polygonum cuspidatum Sieb. Et Zucc. are traditional Chinese medicines that have been used for thousands of years. They are formulat... |
PMC9653313 | core_pubmed_pmc | Optimization of Drug Therapy for Heart Failure With Reduced Ejection Fraction Based on Gender | Optimization of Drug Therapy for Heart Failure With Reduced Ejection Fraction Based on Gender Abstract Purpose of Review Over the last decades, several classes of drugs have been introduced for the treatment of patients with heart failure with reduced ejection fraction (HFrEF). Their use has been supported by randomize... |
PMC8187405 | core_pubmed_pmc | Nicotine delivery and relief of craving after consumption of European JUUL e-cigarettes prior and after pod modification | Nicotine delivery and relief of craving after consumption of European JUUL e-cigarettes prior and after pod modification Abstract Abstract The emergence of e-cigarettes on the consumer market led to a tremendous rise in e-cigarette consumption among adolescents in the United States. The success of JUUL and other pod sy... |
PMC5036424 | core_pubmed_pmc | A Population Pharmacokinetic Model for Vancomycin in Adult Patients Receiving Extracorporeal Membrane Oxygenation Therapy | A Population Pharmacokinetic Model for Vancomycin in Adult Patients Receiving Extracorporeal Membrane Oxygenation Therapy Abstract Abstract The literature on the pharmacokinetics of vancomycin in patients undergoing extracorporeal membrane oxygenation (ECMO) therapy is sparse. A population pharmacokinetic (PK) model fo... |
PMC8513424 | core_pubmed_pmc | Early phase clinical studies of AR‐42, a histone deacetylase inhibitor, for neurofibromatosis type 2‐associated vestibular schwannomas and meningiomas | Early phase clinical studies of AR‐42, a histone deacetylase inhibitor, for neurofibromatosis type 2‐associated vestibular schwannomas and meningiomas Abstract Abstract Objectives Two pilot studies of AR‐42, a pan‐histone deacetylase inhibitor, in human neurofibromatosis type 2 (NF2), vestibular schwannomas (VS), and m... |
PMC9860936 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Effects of Polyclonal Antibodies against SARS-CoV2 in Mice | Pharmacokinetic and Pharmacodynamic Effects of Polyclonal Antibodies against SARS-CoV2 in Mice Abstract Abstract Despite ongoing vaccination efforts to prevent SARS-CoV-2 infections, treatment tools are still necessary to address the ongoing COVID-19 pandemic. We report here that COVID-HIGIV, a human immunoglobulin pro... |
PMC7785388 | core_pubmed_pmc | Establishment and Validation of a Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of Tigecycline in Critically Ill Patients | Establishment and Validation of a Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of Tigecycline in Critically Ill Patients Abstract Utilizing tigecycline-d9 as an internal standard (IS), we establish and validate a simple, effective, and rapid liquid chromatography-tandem mass spectrometry ... |
PMC9333413 | core_pubmed_pmc | Optimal dosing of cefotaxime and desacetylcefotaxime for critically ill paediatric patients. Can we use microsampling? | Optimal dosing of cefotaxime and desacetylcefotaxime for critically ill paediatric patients. Can we use microsampling? Abstract Abstract Objectives To describe the population pharmacokinetics of cefotaxime and desacetylcefotaxime in critically ill paediatric patients and provide dosing recommendations. We also sought t... |
PMC11530482 | core_pubmed_pmc | Population Pharmacokinetics of Casirivimab and Imdevimab in Pediatric and Adult Non-Infected Individuals, Pediatric and Adult Ambulatory or Hospitalized Patients or Household Contacts of Patients Infected with SARS-COV-2 | Population Pharmacokinetics of Casirivimab and Imdevimab in Pediatric and Adult Non-Infected Individuals, Pediatric and Adult Ambulatory or Hospitalized Patients or Household Contacts of Patients Infected with SARS-COV-2 Abstract Introduction Casirivimab (CAS) and imdevimab (IMD) are two fully human monoclonal antibodi... |
PMC7854954 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Central Nervous System Pharmacokinetics of CDK4/6 Inhibitors to Guide Selection of Drug and Dosing Regimen for Brain Cancer Treatment | Physiologically Based Pharmacokinetic Modeling of Central Nervous System Pharmacokinetics of CDK4/6 Inhibitors to Guide Selection of Drug and Dosing Regimen for Brain Cancer Treatment Abstract Abstract A better understanding of the human central nervous system (CNS) pharmacokinetics is critical to the selection of the ... |
PMC5702158 | core_pubmed_pmc | Cohort-specific imputation of gene expression improves prediction of warfarin dose for African Americans | Cohort-specific imputation of gene expression improves prediction of warfarin dose for African Americans Abstract Background Genome-wide association studies are useful for discovering genotype–phenotype associations but are limited because they require large cohorts to identify a signal, which can be population-specifi... |
PMC3658022 | core_pubmed_pmc | Bioanalytical method validation: An updated review | Bioanalytical method validation: An updated review Abstract The development of sound bioanalytical method(s) is of paramount importance during the process of drug discovery and development, culminating in a marketing approval. The objective of this paper is to review the sample preparation of drug in biological matrix ... |
PMC7550310 | core_pubmed_pmc | Innovative Approaches for Pharmacology Studies in Pregnant and Lactating Women: A Viewpoint and Lessons from HIV | Innovative Approaches for Pharmacology Studies in Pregnant and Lactating Women: A Viewpoint and Lessons from HIV Abstract Medication use during pregnancy in the absence of pharmacokinetic and safety data is common, particularly for antiretrovirals, as pregnant women are not usually included in clinical trials leading t... |
PMC7673921 | core_pubmed_pmc | Baicalin Liposome Alleviates Lipopolysaccharide-Induced Acute Lung Injury in Mice via Inhibiting TLR4/JNK/ERK/NF- κ B Pathway | Baicalin Liposome Alleviates Lipopolysaccharide-Induced Acute Lung Injury in Mice via Inhibiting TLR4/JNK/ERK/NF- κ B Pathway Abstract Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are challenging diseases with the high mortality in a clinical setting. Baicalin (BA) is the main effective consti... |
PMC9835136 | core_pubmed_pmc | A pharmacokinetic–pharmacodynamic model for chemoprotective agents against malaria | A pharmacokinetic–pharmacodynamic model for chemoprotective agents against malaria Abstract Abstract Chemoprophylactics are a vital tool in the fight against malaria. They can be used to protect populations at risk, such as children younger than the age of 5 in areas of seasonal malaria transmission or pregnant women. ... |
PMC8752107 | core_pubmed_pmc | Prediction of cytochromes P450 3A and 2C19 modulation by both inflammation and drug interactions using physiologically based pharmacokinetics | Prediction of cytochromes P450 3A and 2C19 modulation by both inflammation and drug interactions using physiologically based pharmacokinetics Abstract Abstract Xenobiotics can interact with cytochromes P450 (CYPs), resulting in drug–drug interactions, but CYPs can also contribute to drug–disease interactions, especiall... |
PMC7877864 | core_pubmed_pmc | A Dynamic Quantitative Systems Pharmacology Model of Inflammatory Bowel Disease: Part 2 – Application to Current Therapies in Crohn’s Disease | A Dynamic Quantitative Systems Pharmacology Model of Inflammatory Bowel Disease: Part 2 – Application to Current Therapies in Crohn’s Disease Abstract Abstract Inflammatory bowel disease (IBD) is a heterogeneic disease with a variety of treatments targeting different mechanisms. A multistate, mechanistic, mathematical ... |
PMC11233281 | core_pubmed_pmc | Effect of Activated Charcoal on Mavacamten Pharmacokinetics in Healthy Participants | Effect of Activated Charcoal on Mavacamten Pharmacokinetics in Healthy Participants Abstract Objective To assess the effect of activated charcoal on the single-dose pharmacokinetics of mavacamten when administered 2 h or 6 h after mavacamten dosing. Methods In this open-label, randomized, parallel-group study, healthy ... |
PMC6472623 | core_pubmed_pmc | Next generation physiologically based kinetic (NG-PBK) models in support of regulatory decision making | Next generation physiologically based kinetic (NG-PBK) models in support of regulatory decision making Abstract Highlights • PBK models have helped to facilitate quantitative in vitro to in vivo extrapolation. • PBK modelling has the potential to play a significant role in reducing animal testing. • It is critical to a... |
PMC5323819 | core_pubmed_pmc | SiRNA Crosslinked Nanoparticles for the Treatment of Inflammation‐induced Liver Injury | SiRNA Crosslinked Nanoparticles for the Treatment of Inflammation‐induced Liver Injury Abstract RNA interference mediated by small interfering RNA (siRNA) provides a powerful tool for gene regulation, and has a broad potential as a promising therapeutic strategy. However, therapeutics based on siRNA have had limited cl... |
PMC4875959 | core_pubmed_pmc | Liraglutide in Type 2 Diabetes Mellitus: Clinical Pharmacokinetics and Pharmacodynamics | Liraglutide in Type 2 Diabetes Mellitus: Clinical Pharmacokinetics and Pharmacodynamics Abstract Abstract Liraglutide is an acylated glucagon-like peptide-1 analogue with 97 % amino acid homology with native glucagon-like peptide-1 and greatly protracted action. It is widely used for the treatment of type 2 diabetes me... |
PMC4839654 | core_pubmed_pmc | Sustained Effect of Hyaluronic Acid in Subcutaneous Administration to the Cochlear Spiral Ganglion | Sustained Effect of Hyaluronic Acid in Subcutaneous Administration to the Cochlear Spiral Ganglion Abstract Abstract The spatiotemporal distribution of drugs in the inner ear cannot be precisely evaluated because of its small area and complex structure. In the present study, we used hyaluronic acid (HA)-dispersed lucif... |
PMC5903241 | core_pubmed_pmc | Effect of the angiotensin receptor–neprilysin inhibitor sacubitril/valsartan on the pharmacokinetics and pharmacodynamics of a single dose of furosemide | Effect of the angiotensin receptor–neprilysin inhibitor sacubitril/valsartan on the pharmacokinetics and pharmacodynamics of a single dose of furosemide Abstract Aims Sacubitril/valsartan is indicated for the treatment of heart failure and reduced ejection fraction (HFrEF). Furosemide, a loop diuretic commonly used for... |
PMC12816464 | core_pubmed_pmc | VAL-083 is effective in patients with newly-diagnosed MGMT-unmethylated glioblastoma: report of phase II study | VAL-083 is effective in patients with newly-diagnosed MGMT-unmethylated glioblastoma: report of phase II study Abstract Purpose Unmethylated MGMT is a validated biomarker for temozolomide (TMZ) resistance and poor prognosis in glioblastoma. VAL-083 (dianhydrogalactitol; DAG) is a DNA-targeting agent that forms interstr... |
PMC4728292 | core_pubmed_pmc | Semiphysiologically based pharmacokinetic model for midazolam and CYP3A mediated metabolite 1‐OH‐midazolam in morbidly obese and weight loss surgery patients | Semiphysiologically based pharmacokinetic model for midazolam and CYP3A mediated metabolite 1‐OH‐midazolam in morbidly obese and weight loss surgery patients Abstract Abstract This study aimed to describe the pharmacokinetics of midazolam and its cytochrome P450 3A (CYP3A) mediated metabolite 1‐OH‐midazolam in morbidly... |
PMC7343180 | core_pubmed_pmc | Model-Based Approach for Establishing the Predicted Clinical Response of a Delayed-Release and Extended-Release Methylphenidate for the Treatment of Attention-Deficit/Hyperactivity Disorder | Model-Based Approach for Establishing the Predicted Clinical Response of a Delayed-Release and Extended-Release Methylphenidate for the Treatment of Attention-Deficit/Hyperactivity Disorder Abstract Supplemental digital content is available in the text. Abstract Purpose/Background HLD200 is an evening-dosed, delayed-re... |
PMC2880981 | core_pubmed_pmc | Correlation of pharmacodynamic activity, pharmacokinetics, and anti-product antibody responses to anti-IL-21R antibody therapeutics following IV administration to cynomolgus monkeys | Correlation of pharmacodynamic activity, pharmacokinetics, and anti-product antibody responses to anti-IL-21R antibody therapeutics following IV administration to cynomolgus monkeys Abstract Abstract Background Anti-IL-21R antibodies are potential therapeutics for the treatment of autoimmune diseases. This study evalua... |
PMC6447882 | core_pubmed_pmc | Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice | Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice Abstract Abstract The efficacy of methotrexate (MTX) as an antimetabolite chemotherapeutic agent highly depends on its blood circulation half-life. In our previous study, different conjugates of MTX (MTX-PEG) were synthesized... |
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