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PMC8456852 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of Abacavir/Dolutegravir/Lamivudine Combination Tablets in Healthy Japanese Study Participants | Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of Abacavir/Dolutegravir/Lamivudine Combination Tablets in Healthy Japanese Study Participants Abstract Abstract Pharmacokinetics, safety, and tolerability of abacavir 600 mg/dolutegravir 50 mg/lamivudine 300 mg were assessed in this phase 1, single‐arm, ... |
PMC8597022 | core_pubmed_pmc | Quantitative Clinical Pharmacology Supports the Bridging From i.v. Dosing and Approval of s.c. Rituximab in B‐Cell Hematological Malignancies | Quantitative Clinical Pharmacology Supports the Bridging From i.v. Dosing and Approval of s.c. Rituximab in B‐Cell Hematological Malignancies Abstract Abstract A fixed‐dose subcutaneous (s.c.) formulation of the anti‐CD20 antibody, rituximab, has been developed to address safety, infusion time, and patient comfort conc... |
PMC12408595 | core_pubmed_pmc | Locked nucleic acid-modified antisense oligonucleotides attenuate scar hyperplasia through targeted inhibition of CTGF | Locked nucleic acid-modified antisense oligonucleotides attenuate scar hyperplasia through targeted inhibition of CTGF Abstract Abstract Connective tissue growth factor (CTGF) is notably upregulated in scar tissue, making it a promising target for therapeutic intervention. Here, we have designed and screened an antisen... |
PMC9501983 | core_pubmed_pmc | Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions | Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions Abstract Abstract The dapivirine (DPV) vaginal ring was developed by the nonprofit International Partnership for Microbicides (IPM) for reducing the risk of HIV infection. A clinical study (IPM 028) showed that concomitant... |
PMC8948700 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery | Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery Abstract Abstract Nose-to-brain drug delivery has been of great interest for the treatment of many central nervous system (CNS) diseases and psychiatric disorders over past decades.... |
PMC3286592 | core_pubmed_pmc | Pharmacokinetics, metabolism and excretion of [ 14 C]-lenalidomide following oral administration in healthy male subjects | Pharmacokinetics, metabolism and excretion of [ 14 C]-lenalidomide following oral administration in healthy male subjects Abstract Abstract Purpose Assessment of the absorption, metabolism and excretion of [ 14 C]-lenalidomide in healthy male subjects following a single oral dose. Methods Six healthy male subjects were... |
PMC7244958 | core_pubmed_pmc | Effect of You-Gui Yin on the Activities of Seven Cytochrome P450 Isozymes in Rats | Effect of You-Gui Yin on the Activities of Seven Cytochrome P450 Isozymes in Rats Abstract Abstract You-Gui Yin (YGY) is a traditional Chinese medicine (TCM) decoction composed of eight Chinese herbs. The interaction between TCM and Western medicine has attracted much attention nowadays. It is therefore necessary to st... |
PMC6270976 | core_pubmed_pmc | Pharmacokinetic Study in Mice of Galphimine-A, an Anxiolytic Compound from Galphimia glauca | Pharmacokinetic Study in Mice of Galphimine-A, an Anxiolytic Compound from Galphimia glauca Abstract Abstract The aim of this study was to obtain pharmacokinetic data for the anxiolytic compound galphimine-A (G–A) from Galphimia glauca . G–A is the most abundant anxiolytic compound in this plant, while Galphimine-E (G–... |
PMC12291801 | core_pubmed_pmc | The Changing Landscape of Antibiotic Treatment: Reevaluating Treatment Length in the Age of New Agents | The Changing Landscape of Antibiotic Treatment: Reevaluating Treatment Length in the Age of New Agents Abstract Abstract Background: The landscape of antimicrobial therapy is undergoing a profound transformation; the contemporary arsenal of antimicrobials, particularly those with extended half-lives and enhanced tissue... |
PMC11652423 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Rusfertide, a Hepcidin Mimetic, Following Subcutaneous Administration of a Lyophilized Powder Formulation in Healthy Volunteers | Pharmacokinetics and Pharmacodynamics of Rusfertide, a Hepcidin Mimetic, Following Subcutaneous Administration of a Lyophilized Powder Formulation in Healthy Volunteers Abstract Background and Objective Hepcidin, an endogenous peptide hormone, binds to ferroportin and is the master regulator of iron trafficking. Rusfer... |
PMC10674549 | core_pubmed_pmc | Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin | Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin Abstract Abstract Permeability has an important effect on drug absorption. In this study, the effect of different concentrations of sodium sulfobutyl ether-β-cyclodextrin (SBE-β-CD) on the absorption of ranitidine... |
PMC11679925 | core_pubmed_pmc | Metabolomic Profile Modification in the Cerebellum of Mice Repeatedly Exposed to Khat and Treated with β-Lactamase Inhibitor, Clavulanic Acid | Metabolomic Profile Modification in the Cerebellum of Mice Repeatedly Exposed to Khat and Treated with β-Lactamase Inhibitor, Clavulanic Acid Abstract Background/Objectives: Catha edulis, commonly known as khat, is used for its psychoactive effects and is considered a natural amphetamine. The current study investigated... |
PMC4427609 | core_pubmed_pmc | Impact of streptozotocin on altering normal glucose homeostasis during insulin testing in diabetic rats compared to normoglycemic rats | Impact of streptozotocin on altering normal glucose homeostasis during insulin testing in diabetic rats compared to normoglycemic rats Abstract Streptozotocin (STZ) is currently the most used diabetogenic agent in testing insulin and new antidiabetic drugs in animals. Due to the toxic and disruptive nature of STZ on or... |
PMC12936328 | core_pubmed_pmc | In silico analysis of Anacardium occidentale phytochemicals: pharmacokinetics, molecular docking, and dynamics of Cryptococcus neoformans enzymes | In silico analysis of Anacardium occidentale phytochemicals: pharmacokinetics, molecular docking, and dynamics of Cryptococcus neoformans enzymes Abstract Abstract This study evaluated in silico the antifungal potential of phytochemicals from the leaves of Anacardium occidentale (cashew tree) against key enzymatic targ... |
PMC8799530 | core_pubmed_pmc | A Review of the Totality of Evidence for the Development and Approval of ABP 710 (AVSOLA), an Infliximab Biosimilar | A Review of the Totality of Evidence for the Development and Approval of ABP 710 (AVSOLA), an Infliximab Biosimilar Abstract Abstract ABP 710 (AVSOLA ® ) is a biosimilar to infliximab reference product (RP), a monoclonal antibody targeting tumor necrosis factor alpha (TNFα). It is approved in the USA and Canada for all... |
PMC12191122 | core_pubmed_pmc | The Perioperative Use of Dexmedetomidine in Paediatric Patients | The Perioperative Use of Dexmedetomidine in Paediatric Patients Abstract Abstract Background/Objectives : Dexmedetomidine, an alpha-2 adrenergic agonist, has gained significant attention for its sedative, analgesic, and anxiolytic properties in paediatric anaesthesia. This review explores its pharmacokinetics and pharm... |
PMC9249725 | core_pubmed_pmc | Repeat subcutaneous administration of casirivimab and imdevimab in adults is well-tolerated and prevents the occurrence of COVID-19 | Repeat subcutaneous administration of casirivimab and imdevimab in adults is well-tolerated and prevents the occurrence of COVID-19 Abstract Objectives A phase 1, double-blind, placebo-controlled trial was conducted to evaluate the safety, tolerability, and exploratory efficacy of repeat monthly doses of subcutaneous (... |
PMC9965021 | core_pubmed_pmc | Inclisiran—Safety and Effectiveness of Small Interfering RNA in Inhibition of PCSK-9 | Inclisiran—Safety and Effectiveness of Small Interfering RNA in Inhibition of PCSK-9 Abstract Dyslipidemia is listed among important cardiovascular disease risk factors. Treating lipid disorders is difficult, and achieving desirable levels of LDL-cholesterol (LDL-C) is essential in both the secondary and primary preven... |
PMC9774142 | core_pubmed_pmc | Next-Generation Polymyxin Class of Antibiotics: A Ray of Hope Illuminating a Dark Road | Next-Generation Polymyxin Class of Antibiotics: A Ray of Hope Illuminating a Dark Road Abstract Abstract Although new-generation antimicrobials, in particular β-lactam/β-lactamase inhibitors, have largely replaced polymyxins in carbapenem-resistant Gram-negative bacterial infections, polymyxins are still needed for car... |
PMC9227765 | core_pubmed_pmc | Molnupiravir and Its Active Form, EIDD-1931, Show Potent Antiviral Activity against Enterovirus Infections In Vitro and In Vivo | Molnupiravir and Its Active Form, EIDD-1931, Show Potent Antiviral Activity against Enterovirus Infections In Vitro and In Vivo Abstract Enterovirus infections can cause hand, foot, and mouth disease (HFDM), aseptic meningitis, encephalitis, myocarditis, and acute flaccid myelitis, leading to death of infants and young... |
PMC8518967 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Bedaquiline‐Clarithromycin for Dose Selection Against Pulmonary Nontuberculous Mycobacteria Based on a Phase 1, Randomized, Pharmacokinetic Study | Population Pharmacokinetic Analysis of Bedaquiline‐Clarithromycin for Dose Selection Against Pulmonary Nontuberculous Mycobacteria Based on a Phase 1, Randomized, Pharmacokinetic Study Abstract Abstract Based on the in vitro profile of bedaquiline against mycobacterial species, it is being investigated for clinical eff... |
PMC9063953 | core_pubmed_pmc | BREEZE: Open‐label clinical study to evaluate the safety and tolerability of treprostinil inhalation powder as Tyvaso DPI™ in patients with pulmonary arterial hypertension | BREEZE: Open‐label clinical study to evaluate the safety and tolerability of treprostinil inhalation powder as Tyvaso DPI™ in patients with pulmonary arterial hypertension Abstract Abstract Inhaled treprostinil is an approved therapy for pulmonary arterial hypertension (PAH) and pulmonary hypertension associated with i... |
PMC12406660 | core_pubmed_pmc | Pharmacokinetics of first-line tuberculosis drugs rifampin, isoniazid, ethambutol, and pyrazinamide during pregnancy and postpartum with and without efavirenz-based antiretroviral treatment: IMPAACT P1026s study | Pharmacokinetics of first-line tuberculosis drugs rifampin, isoniazid, ethambutol, and pyrazinamide during pregnancy and postpartum with and without efavirenz-based antiretroviral treatment: IMPAACT P1026s study Abstract ABSTRACT The pharmacokinetics (PK) of antituberculosis drugs may be altered by both pregnancy-induc... |
PMC11998771 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Effects of the Muscarinic M 1 Positive Allosteric Modulator VU0467319 for Alzheimer’s disease: A Single Ascending-Dose Study in Healthy Participants | Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Effects of the Muscarinic M 1 Positive Allosteric Modulator VU0467319 for Alzheimer’s disease: A Single Ascending-Dose Study in Healthy Participants Abstract Abstract The development of cholinergic neurotransmitter based cognitive enhancers for Alzheimer’s disea... |
PMC4062493 | core_pubmed_pmc | Failure of Miltefosine Treatment for Visceral Leishmaniasis in Children and Men in South-East Asia | Failure of Miltefosine Treatment for Visceral Leishmaniasis in Children and Men in South-East Asia Abstract Background High frequency of relapse in miltefosine-treated visceral leishmaniasis (VL) patients in India and Nepal followed up for twelve months. Objective To identify epidemiological and clinical risk factors f... |
PMC5579760 | core_pubmed_pmc | The Nephrotoxicity of Vancomycin | The Nephrotoxicity of Vancomycin Abstract Abstract Vancomycin use is often associated with nephrotoxicity. It remains uncertain, however, to what extent vancomycin is directly responsible, as numerous potential risk factors for acute kidney injury frequently coexist. Herein, we critically examine available data in adul... |
PMC8388768 | core_pubmed_pmc | Efficacy and Safety of Continuous Infusion of Vancomycin in Children: A Systematic Review | Efficacy and Safety of Continuous Infusion of Vancomycin in Children: A Systematic Review Abstract Vancomycin is used to treat a wide variety of infections within the pediatric population. In adults, continuous infusion of vancomycin (CIV) has been evaluated as an alternative to intermittent infusion of vancomycin (IIV... |
PMC4873860 | core_pubmed_pmc | Strain differences in cytochrome P450 mRNA and protein expression, and enzymatic activity among Sprague Dawley, Wistar, Brown Norway and Dark Agouti rats | Strain differences in cytochrome P450 mRNA and protein expression, and enzymatic activity among Sprague Dawley, Wistar, Brown Norway and Dark Agouti rats Abstract Abstract Rat cytochrome P450 (CYP) exhibits inter-strain differences, but their analysis has been scattered across studies under different conditions. To ide... |
PMC10904689 | core_pubmed_pmc | First-in-Human Safety, Tolerability, and Pharmacokinetics of Single-Dose Kukoamine B Mesylate in Healthy Subjects: A Randomized, Double-Blind, Placebo-Controlled Phase I Study | First-in-Human Safety, Tolerability, and Pharmacokinetics of Single-Dose Kukoamine B Mesylate in Healthy Subjects: A Randomized, Double-Blind, Placebo-Controlled Phase I Study Abstract Introduction Kukoamine B mesylate (KB) is a mesylate chrysamine B targeting lipopolysaccharides and CpG DNA, two potential treatment ta... |
PMC4457799 | core_pubmed_pmc | Development of Sustained Release “NanoFDC (Fixed Dose Combination)” for Hypertension – An Experimental Study | Development of Sustained Release “NanoFDC (Fixed Dose Combination)” for Hypertension – An Experimental Study Abstract Objectives The present study was planned to formulate, characterize and evaluate the pharmacokinetics of a novel “NanoFDC” comprising three commonly prescribed anti-hypertensive drugs, hydrochlorothiazi... |
PMC10768346 | core_pubmed_pmc | Differential distribution of linezolid in diseased and nondiseased bones in patients with spinal tuberculosis | Differential distribution of linezolid in diseased and nondiseased bones in patients with spinal tuberculosis Abstract Background Linezolid exhibits antibacterial activity against sensitive and drug-resistant strains of Mycobacterium tuberculosis . Knowledge on the distribution of linezolid in different types of bones ... |
PMC6131668 | core_pubmed_pmc | Computational Modeling of Electrophysiology and Pharmacotherapy of Atrial Fibrillation: Recent Advances and Future Challenges | Computational Modeling of Electrophysiology and Pharmacotherapy of Atrial Fibrillation: Recent Advances and Future Challenges Abstract Abstract The pathophysiology of atrial fibrillation (AF) is broad, with components related to the unique and diverse cellular electrophysiology of atrial myocytes, structural complexity... |
PMC10087078 | core_pubmed_pmc | Physiologically‐based pharmacokinetic model to investigate the effect of pregnancy on risperidone and paliperidone pharmacokinetics: Application to a pregnant woman and her neonate | Physiologically‐based pharmacokinetic model to investigate the effect of pregnancy on risperidone and paliperidone pharmacokinetics: Application to a pregnant woman and her neonate Abstract Abstract This study aimed to determine the effects of pregnancy and ontogeny on risperidone and paliperidone pharmacokinetics by a... |
PMC7686355 | core_pubmed_pmc | A randomised controlled single-centre open-label pharmacokinetic study to examine various approaches of nicotine delivery using electronic cigarettes | A randomised controlled single-centre open-label pharmacokinetic study to examine various approaches of nicotine delivery using electronic cigarettes Abstract Smokers who switch completely to e-cigarettes may reduce their relative risk of tobacco-related disease. Effective nicotine delivery from e-cigarettes is importa... |
PMC8489377 | core_pubmed_pmc | Population Pharmacokinetics Modeling of Vancomycin Among Chinese Infants With Normal and Augmented Renal Function | Population Pharmacokinetics Modeling of Vancomycin Among Chinese Infants With Normal and Augmented Renal Function Abstract There have been good amounts of population pharmacokinetics (PPK) models of vancomycin for Chinese pediatric patients, but none of them had a special focus on modeling infant population with differ... |
PMC11869203 | core_pubmed_pmc | Acetalax and Bisacodyl for the Treatment of Triple-Negative Breast Cancer: A Combined Molecular and Preclinical Study | Acetalax and Bisacodyl for the Treatment of Triple-Negative Breast Cancer: A Combined Molecular and Preclinical Study Abstract Abstract The recalcitrant nature of triple-negative breast cancer (TNBC) calls for novel treatments. Acetalax (oxyphenisatin acetate) and bisacodyl, which have been and are extensively used ora... |
PMC6738359 | core_pubmed_pmc | Pharmacokinetics of Sublingual Buprenorphine Tablets Following Single and Multiple Doses in Chinese Participants With and Without Opioid Use Disorder | Pharmacokinetics of Sublingual Buprenorphine Tablets Following Single and Multiple Doses in Chinese Participants With and Without Opioid Use Disorder Abstract Background Two phase I studies assessed the pharmacokinetics of buprenorphine, its metabolite norbuprenorphine, and naloxone following administration of buprenor... |
PMC5012102 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Profiles of Tiamulin in an Experimental Intratracheal Infection Model of Mycoplasma gallisepticum | Pharmacokinetic/Pharmacodynamic Profiles of Tiamulin in an Experimental Intratracheal Infection Model of Mycoplasma gallisepticum Abstract Mycoplasma gallisepticum is the most important pathogen in poultry among four pathogenic Mycoplasma species. Tiamulin is a pleuromutilin antibiotic that shows a great activity again... |
PMC12612264 | core_pubmed_pmc | In silico and in vitro evaluation of drug-like properties and anticancer potential of novel 5-fluorouracil derivatives | In silico and in vitro evaluation of drug-like properties and anticancer potential of novel 5-fluorouracil derivatives Abstract Abstract The development of more effective and safer anticancer agents remains a critical focus in cancer therapy. While biologics are gaining attention, small molecules continue to play a sig... |
PMC10885622 | core_pubmed_pmc | Mechanism of action, resistance, interaction, pharmacokinetics, pharmacodynamics, and safety of fostemsavir | Mechanism of action, resistance, interaction, pharmacokinetics, pharmacodynamics, and safety of fostemsavir Abstract The Food and Drug Administration (FDA) has licensed many antiretroviral medications to treat human immunodeficiency virus type 1 (HIV-1), however, treatment options for people with multi-drug resistant H... |
PMC4773073 | core_pubmed_pmc | The Antiviral Activity of Approved and Novel Drugs against HIV-1 Mutations Evaluated under the Consideration of Dose-Response Curve Slope | The Antiviral Activity of Approved and Novel Drugs against HIV-1 Mutations Evaluated under the Consideration of Dose-Response Curve Slope Abstract Objectives This study was designed to identify common HIV-1 mutation complexes affecting the slope of inhibition curve, and to propose a new parameter incorporating both the... |
PMC12451478 | core_pubmed_pmc | Bench to Bedside Modeling of mRNA Encoding IgG Using a Multiscale Mechanistic Pharmacokinetic‐Toxicokinetic ( PK ‐ TK ) Model: A Case Study With Anti‐Claudin 18.2 | Bench to Bedside Modeling of mRNA Encoding IgG Using a Multiscale Mechanistic Pharmacokinetic‐Toxicokinetic ( PK ‐ TK ) Model: A Case Study With Anti‐Claudin 18.2 Abstract ABSTRACT In vivo expression of mRNA‐encoded antibodies offers a novel platform for targeted therapies. However, translating preclinical findings to ... |
PMC3982980 | core_pubmed_pmc | Effects of Calibration Approaches on the Accuracy for LC–MS Targeted Quantification of Therapeutic Protein | Effects of Calibration Approaches on the Accuracy for LC–MS Targeted Quantification of Therapeutic Protein Abstract LC–MS provides a promising alternative to ligand-binding assays for quantification of therapeutic proteins and biomarkers. As LC–MS methodology is based on the analysis of proteolytic peptides, calibratio... |
PMC10087228 | core_pubmed_pmc | Pharmacokinetic and Bioequivalence Study of Eldecalcitol Soft Capsules in Healthy Chinese Subjects | Pharmacokinetic and Bioequivalence Study of Eldecalcitol Soft Capsules in Healthy Chinese Subjects Abstract Abstract Eldecalcitol is a novel active vitamin D 3 1,25(OH) 2 D 3 derivative used in the treatment of osteoporosis. To investigate and compare the pharmacokinetic and bioequivalent profiles of two eldecalcitol s... |
PMC7053273 | core_pubmed_pmc | High Risk of Drug–drug interactions among Hospitalized Patients with kidney Diseases at a Nigerian Teaching Hospital: A Call for Action | High Risk of Drug–drug interactions among Hospitalized Patients with kidney Diseases at a Nigerian Teaching Hospital: A Call for Action Abstract Background: Potential drug–drug interactions (DDIs) are increasingly common in clinical practice, especially among individuals with chronic conditions, such as chronic kidney ... |
PMC9909726 | core_pubmed_pmc | Development and application of a simple pharmacokinetic model that quantitatively describes the distribution and elimination of the commonly measured proteins | Development and application of a simple pharmacokinetic model that quantitatively describes the distribution and elimination of the commonly measured proteins Abstract Abstract Increased plasma concentrations of a variety of cellular enzymes (alanine transaminase, aspartate aminotransferase, alkaline phosphatase, amyla... |
PMC12087683 | core_pubmed_pmc | IQ Survey Results on Current Industry Practices: Part 2—Quantitative Evaluations of Immunogenicity Assessment | IQ Survey Results on Current Industry Practices: Part 2—Quantitative Evaluations of Immunogenicity Assessment Abstract All biotherapeutics have the potential to induce an immunogenic response and generate anti‐drug antibodies (ADAs), especially when administered as multiple doses over prolonged periods. However, a clin... |
PMC8945640 | core_pubmed_pmc | Population pharmacokinetic modeling of factor concentrates in hemophilia: an overview and evaluation of best practice | Population pharmacokinetic modeling of factor concentrates in hemophilia: an overview and evaluation of best practice Abstract Abstract The accuracy of pharmacokinetic (PK)-guided dosing depends on the clinical and laboratory data used to construct a population PK model, as well as the patient’s individual PK profile. ... |
PMC6950567 | core_pubmed_pmc | Evaluation of Marine Diindolinonepyrane in Vitro and in Vivo: Permeability Characterization in Caco-2 Cells Monolayer and Pharmacokinetic Properties in Beagle Dogs | Evaluation of Marine Diindolinonepyrane in Vitro and in Vivo: Permeability Characterization in Caco-2 Cells Monolayer and Pharmacokinetic Properties in Beagle Dogs Abstract Abstract A marine fibrinolytic compound was studied for use in thrombolytic therapy. Firstly, the absorption and transportation characteristics of ... |
PMC4332344 | core_pubmed_pmc | EEG entropy measures in anesthesia | EEG entropy measures in anesthesia Abstract Highlights: ► Twelve entropy indices were systematically compared in monitoring depth of anesthesia and detecting burst suppression. ► Renyi permutation entropy performed best in tracking EEG changes associated with different anesthesia states. ► Approximate Entropy and Sampl... |
PMC11068909 | core_pubmed_pmc | Changes of PK/PD of Meropenem in patients with abdominal septic shock and exploration of clinical rational administration plan: a prospective exploratory study | Changes of PK/PD of Meropenem in patients with abdominal septic shock and exploration of clinical rational administration plan: a prospective exploratory study Abstract This study aimed to explore the changes of pharmacokinetic parameters after meropenem in patients with abdominal septic shock after gastrointestinal pe... |
PMC10363979 | core_pubmed_pmc | Effects of bergapten on the pharmacokinetics of macitentan in rats both in vitro and in vivo | Effects of bergapten on the pharmacokinetics of macitentan in rats both in vitro and in vivo Abstract Macitentan was approved by the United States Food and Drug Administration (FDA) in 2013 for the treatment of pulmonary arterial hypertension (PAH). Bergapten is a furanocoumarin that is abundant in Umbelliferae and Rut... |
PMC6032847 | core_pubmed_pmc | Subcutaneous Abatacept in Patients With Polyarticular‐Course Juvenile Idiopathic Arthritis | Subcutaneous Abatacept in Patients With Polyarticular‐Course Juvenile Idiopathic Arthritis Abstract Abstract Objective To investigate the pharmacokinetics, effectiveness, and safety of subcutaneous (SC) abatacept treatment over 24 months in patients with polyarticular‐course juvenile idiopathic arthritis (JIA). Methods... |
PMC9122897 | core_pubmed_pmc | SHR1032, a novel STING agonist, stimulates anti-tumor immunity and directly induces AML apoptosis | SHR1032, a novel STING agonist, stimulates anti-tumor immunity and directly induces AML apoptosis Abstract Abstract Stimulator of interferon genes (STING) activation induces type I interferons and pro-inflammatory cytokines which stimulate tumor antigen cross presentation and the adaptive immune responses against tumor... |
PMC3600759 | core_pubmed_pmc | Modeling and Simulation as a Tool to Bridge Efficacy and Safety Data in Special Populations | Modeling and Simulation as a Tool to Bridge Efficacy and Safety Data in Special Populations Abstract The registration and approval of novel medicines have traditionally been based on evidence arising from large prospective trials. Such an approach is often not possible or unsuitable to evaluate the benefit-risk balance... |
PMC7870595 | core_pubmed_pmc | Evaluation of the impact of renal impairment on the pharmacokinetics of glasdegib in otherwise healthy volunteers | Evaluation of the impact of renal impairment on the pharmacokinetics of glasdegib in otherwise healthy volunteers Abstract Purpose Glasdegib is being developed for indications in myeloid malignancies. The effect of renal impairment on the pharmacokinetics (PK) of a single, oral, 100-mg glasdegib dose under fasted condi... |
PMC3861362 | core_pubmed_pmc | Single- and multiple-dose pharmacokinetics, pharmacodynamics, and safety of apixaban in healthy Chinese subjects | Single- and multiple-dose pharmacokinetics, pharmacodynamics, and safety of apixaban in healthy Chinese subjects Abstract Background The pharmacokinetics (PK), pharmacodynamics (PD), and safety of apixaban were assessed in healthy Chinese subjects in this randomized, placebo-controlled, double-blind, single-sequence, s... |
PMC6790582 | core_pubmed_pmc | The first‐generation phosphodiesterase 5 inhibitors and their pharmacokinetic issue | The first‐generation phosphodiesterase 5 inhibitors and their pharmacokinetic issue Abstract Abstract Background Erectile dysfunction (ED) is a relatively frequent disease that negatively impacts the overall quality of life, well‐being, and relationships. Although the use of phosphodiesterase 5 inhibitors (PDE5is) has ... |
PMC12564961 | core_pubmed_pmc | Pharmacokinetics and Monitoring of Methotrexate in Adults with Acute Lymphoblastic Leukaemia: A 10-Year Follow-Up at an Italian Centre | Pharmacokinetics and Monitoring of Methotrexate in Adults with Acute Lymphoblastic Leukaemia: A 10-Year Follow-Up at an Italian Centre Abstract Abstract Background : High-dose methotrexate (HDMTX) is widely used for acute lymphoblastic leukaemia (ALL), but its pharmacokinetic (PK) variability and toxicity require thera... |
PMC6657537 | core_pubmed_pmc | Different Levels of Incomplete Terminal Pathway Inhibition by Eculizumab and the Clinical Response of PNH Patients | Different Levels of Incomplete Terminal Pathway Inhibition by Eculizumab and the Clinical Response of PNH Patients Abstract Abstract Background: Eculizumab blocks the lytic complement pathway by inhibiting C5 and has become the standard of care for certain complement-mediated diseases. Previously, we have shown that st... |
PMC6039200 | core_pubmed_pmc | Initial Clinical Experience of RP5063 Following Single Doses in Normal Healthy Volunteers and Multiple Doses in Patients with Stable Schizophrenia | Initial Clinical Experience of RP5063 Following Single Doses in Normal Healthy Volunteers and Multiple Doses in Patients with Stable Schizophrenia Abstract Abstract RP5063 is a multimodal dopamine (D)‐serotonin (5‐HT) stabilizer with a high affinity for D 2/3/4 and 5‐HT 1A/2A/2B/7 receptors and moderate affinity for th... |
PMC5606553 | core_pubmed_pmc | Phase I trial of the androgen receptor modulator CR1447 in breast cancer patients | Phase I trial of the androgen receptor modulator CR1447 in breast cancer patients Abstract Abstract CR1447 (4-hydroxytestosterone, 4-OHT) binds to the androgen receptor and has antiproliferative activity in both ER-positive and ER-negative/AR-positive breast cancer cells in preclinical studies. The objective of this fi... |
PMC8976459 | core_pubmed_pmc | Sputum lipoarabinomannan (LAM) as a biomarker to determine sputum mycobacterial load: exploratory and model-based analyses of integrated data from four cohorts | Sputum lipoarabinomannan (LAM) as a biomarker to determine sputum mycobacterial load: exploratory and model-based analyses of integrated data from four cohorts Abstract Background Despite the high global disease burden of tuberculosis (TB), the disease caused by Mycobacterium tuberculosis ( Mtb ) infection, novel treat... |
PMC10892093 | core_pubmed_pmc | Cannabinoid-Induced Stereoselective Inhibition of R-S-Oxazepam Glucuronidation: Cannabinoid–Oxazepam Drug Interactions | Cannabinoid-Induced Stereoselective Inhibition of R-S-Oxazepam Glucuronidation: Cannabinoid–Oxazepam Drug Interactions Abstract Benzodiazepines (BZDs) such as oxazepam are commonly prescribed depressant drugs known for their anxiolytic, hypnotic, muscle relaxant, and anticonvulsant effects and are frequently used in co... |
PMC12587577 | core_pubmed_pmc | Cefazolin population pharmacokinetics in children undergoing maintenance hemodialysis for kidney failure | Cefazolin population pharmacokinetics in children undergoing maintenance hemodialysis for kidney failure Abstract ABSTRACT We aimed to develop a population pharmacokinetic model of cefazolin in children undergoing maintenance hemodialysis for kidney failure and simulate dosing regimens to optimize patients’ exposure. C... |
PMC7254109 | core_pubmed_pmc | First in human dose calculation of a single-chain bispecific antibody targeting glioma using the MABEL approach | First in human dose calculation of a single-chain bispecific antibody targeting glioma using the MABEL approach Abstract Background First-in-human (FIH) clinical trials require careful selection of a safe yet biologically relevant starting dose. Typically, such starting doses are selected based on toxicity studies in a... |
PMC12030314 | core_pubmed_pmc | Biomarker-Driven Pharmacokinetics and Efficacy of Polymyxin B in Critically Ill Patients with XDR-GN Pneumonia | Biomarker-Driven Pharmacokinetics and Efficacy of Polymyxin B in Critically Ill Patients with XDR-GN Pneumonia Abstract Background: Achieving pharmacokinetic/pharmacodynamic (PK/PD) targets is critical for improving treatment success, particularly in critically ill patients. This study investigates the role of inflamma... |
PMC11814229 | core_pubmed_pmc | Fermented sugarcane juice-derived probiotic Levilactobacillus brevis RAMULAB54 enhances lipid metabolism and glucose homeostasis through PPAR-γ activation | Fermented sugarcane juice-derived probiotic Levilactobacillus brevis RAMULAB54 enhances lipid metabolism and glucose homeostasis through PPAR-γ activation Abstract Abstract The gut microbiota plays a significant role in metabolic disorders such as diabetes and obesity, with the peroxisome proliferator-activated recepto... |
PMC3384888 | core_pubmed_pmc | Native and Complexed IGF-1: Biodistribution and Pharmacokinetics in Infantile Neuronal Ceroid Lipofuscinosis | Native and Complexed IGF-1: Biodistribution and Pharmacokinetics in Infantile Neuronal Ceroid Lipofuscinosis Abstract Abstract Infantile neuronal ceroid lipofuscinosis (INCL) is a severe neurodegenerative disorder of childhood characterized by selective death of cortical neurons. Insulin-like growth factor 1 (IGF-1) is... |
PMC9872700 | core_pubmed_pmc | Comparison of Pharmacokinetics of the GalNAc-Conjugated Antisense Oligonucleotide GSK3389404 in Participants with Chronic Hepatitis B Infection across the Asia-Pacific Region | Comparison of Pharmacokinetics of the GalNAc-Conjugated Antisense Oligonucleotide GSK3389404 in Participants with Chronic Hepatitis B Infection across the Asia-Pacific Region Abstract ABSTRACT GSK3389404, an N-acetyl galactosamine-conjugated antisense oligonucleotide (ASO), was in clinical development for chronic hepat... |
PMC6778862 | core_pubmed_pmc | Effect of Naoxintong Capsules on the Activities of CYP450 and Metabolism of Metoprolol Tartrate in Rats Evaluated by Probe Cocktail and Pharmacokinetic Methods | Effect of Naoxintong Capsules on the Activities of CYP450 and Metabolism of Metoprolol Tartrate in Rats Evaluated by Probe Cocktail and Pharmacokinetic Methods Abstract Abstract Naoxintong capsule (NXT), a prescribed Chinese medicine, has been used clinically for more than 20 years and is widely received by patients. W... |
PMC6420786 | core_pubmed_pmc | Effects of formulation types on pharmacodynamics of warfarin in patients with cerebral infarction and dysphagia | Effects of formulation types on pharmacodynamics of warfarin in patients with cerebral infarction and dysphagia Abstract Abstract Purpose The purpose of this study was to investigate the effects of the type of formulation on the efficacy of warfarin. Materials and methods The electronic medical records of patients with... |
PMC11949333 | core_pubmed_pmc | Pharmacogenetics and adverse drug reports: Insights from a United Kingdom national pharmacovigilance database | Pharmacogenetics and adverse drug reports: Insights from a United Kingdom national pharmacovigilance database Abstract Abstract Background Adverse drug reactions (ADRs) harm patients and are costly for healthcare systems. Genetic variation contributes to variability in medication response and prospective knowledge of t... |
PMC10290285 | core_pubmed_pmc | Sex-biased gene expression and gene-regulatory networks of sex-biased adverse event drug targets and drug metabolism genes | Sex-biased gene expression and gene-regulatory networks of sex-biased adverse event drug targets and drug metabolism genes Abstract Abstract Background: Previous pharmacovigilance studies and a retroactive review of cancer clinical trial studies identified that women were more likely to experience drug adverse events (... |
PMC7767385 | core_pubmed_pmc | Meropenem Plasma and Interstitial Soft Tissue Concentrations in Obese and Nonobese Patients—A Controlled Clinical Trial | Meropenem Plasma and Interstitial Soft Tissue Concentrations in Obese and Nonobese Patients—A Controlled Clinical Trial Abstract Background: This controlled clinical study aimed to investigate the impact of obesity on plasma and tissue pharmacokinetics of meropenem. Methods: Obese (body mass index (BMI) ≥ 35 kg/m 2 ) a... |
PMC3896903 | core_pubmed_pmc | Perturbation of mitiglinide metabolism by chronic unpredicted mild stress in rats | Perturbation of mitiglinide metabolism by chronic unpredicted mild stress in rats Abstract Abstract Many diabetic patients complicated with wild to severe depression. It is unclear in diabetic medication whether depression perturbs the drug metabolic process of the hypoglycemic agents or not. The present study was desi... |
PMC12167923 | core_pubmed_pmc | Precision Dosing in Presence of Multiobjective Therapies by Integrating Reinforcement Learning and PK‐PD Models: Application to Givinostat Treatment of Polycythemia Vera | Precision Dosing in Presence of Multiobjective Therapies by Integrating Reinforcement Learning and PK‐PD Models: Application to Givinostat Treatment of Polycythemia Vera Abstract ABSTRACT Precision dosing aims to optimize and customize pharmacological treatment at the individual level. The integration of pharmacometric... |
PMC12122123 | core_pubmed_pmc | First‐in‐human safety, tolerability, pharmacokinetics and pilot food‐effect study of the candidate antimalarial compound MMV367 | First‐in‐human safety, tolerability, pharmacokinetics and pilot food‐effect study of the candidate antimalarial compound MMV367 Abstract Abstract Aim To evaluate the safety, tolerability and pharmacokinetics in healthy participants of orally administered MMV367 (GSK3772701), a novel antimalarial interfering with Plasmo... |
PMC11969998 | core_pubmed_pmc | Pharmacokinetics modulation in solid tumors through thrombin-embedded nanomedicine | Pharmacokinetics modulation in solid tumors through thrombin-embedded nanomedicine Abstract Abstract The development of anti-tumor nanomedicines grapples with the critical challenge of achieving sustained retention and massive intratumoral distributions of chemotherapeutics. Herein, we attempted multifaceted prodrug na... |
PMC7151673 | core_pubmed_pmc | Cystatin C: A Primer for Pharmacists | Cystatin C: A Primer for Pharmacists Abstract Abstract Pharmacists are at the forefront of dosing and monitoring medications eliminated by or toxic to the kidney. To evaluate the effectiveness and safety of these medications, accurate measurement of kidney function is paramount. The mainstay of kidney assessment for dr... |
PMC12534112 | core_pubmed_pmc | Wuweizisu B for cancer treatment from multitarget mechanisms to precision delivery strategies (Review) | Wuweizisu B for cancer treatment from multitarget mechanisms to precision delivery strategies (Review) Abstract Wuweizisu B (WSB), a bioactive lignan derived from Schisandra chinensis , has shown promise as a multi-target anticancer agent with unique therapeutic advantages over conventional therapies. The present revie... |
PMC4790952 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Two Formulations of Febuxostat 40-Mg and 80-Mg Tablets: A Randomized, Open-Label, 4-Way Crossover Study in Healthy Chinese Male Volunteers | Pharmacokinetics and Bioequivalence of Two Formulations of Febuxostat 40-Mg and 80-Mg Tablets: A Randomized, Open-Label, 4-Way Crossover Study in Healthy Chinese Male Volunteers Abstract The present study aimed to investigate the pharmacokinetic properties of febuxostat in healthy Chinese male volunteers and evaluate w... |
PMC9793106 | core_pubmed_pmc | Impact of oral administration of single strain Lactococcus lactis spp. cremoris on immune responses to keyhole limpet hemocyanin immunization and gut microbiota: A randomized placebo-controlled trial in healthy volunteers | Impact of oral administration of single strain Lactococcus lactis spp. cremoris on immune responses to keyhole limpet hemocyanin immunization and gut microbiota: A randomized placebo-controlled trial in healthy volunteers Abstract Introduction Lactococcus lactis spp. cremoris has been associated with promising immunomo... |
PMC8620940 | core_pubmed_pmc | The Pharmacokinetic Profile and Bioavailability of Enteral N-Acetylcysteine in Intensive Care Unit | The Pharmacokinetic Profile and Bioavailability of Enteral N-Acetylcysteine in Intensive Care Unit Abstract Abstract Background and Objectives : N-acetylcysteine (NAC) is a mucolytic agent used to prevent ventilator-associated pneumonia in intensive care units. This study aimed to evaluate the oral bioavailability of N... |
PMC12670184 | core_pubmed_pmc | Recent Advances in Machine Learning Models for Predicting Toxicity of Inorganic Nanoparticles | Recent Advances in Machine Learning Models for Predicting Toxicity of Inorganic Nanoparticles Abstract Nanoparticles (NPs) such as engineered inorganic NPs (metals, metal oxides, carbon materials, etc.) can induce cytotoxicity in normal biological systems when used for disease treatment or when exposed to the environme... |
PMC8395454 | core_pubmed_pmc | Importance and Considerations of Antibody Engineering in Antibody-Drug Conjugates Development from a Clinical Pharmacologist’s Perspective | Importance and Considerations of Antibody Engineering in Antibody-Drug Conjugates Development from a Clinical Pharmacologist’s Perspective Abstract Antibody-drug conjugates (ADCs) appear to be in a developmental boom, with five FDA approvals in the last two years and a projected market value of over $4 billion by 2024.... |
PMC3092713 | core_pubmed_pmc | Integration of population pharmacokinetics and pharmacogenetics: an aid to optimal nevirapine dose selection in HIV-infected individuals | Integration of population pharmacokinetics and pharmacogenetics: an aid to optimal nevirapine dose selection in HIV-infected individuals Abstract Background Nevirapine is metabolized by CYP2B6 and polymorphisms within the CYP2B6 gene partly explain inter-patient variability in pharmacokinetics. The aim of this study wa... |
PMC5049785 | core_pubmed_pmc | Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling | Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling Abstract Background Artemisinin resistance observed in Southeast Asia threatens the continued use of artemisinin-based combination therapy in endemic countries. Additionally, the diversity of chemic... |
PMC8836179 | core_pubmed_pmc | Transport Turnover Rates for Human OCT2 and MATE1 Expressed in Chinese Hamster Ovary Cells | Transport Turnover Rates for Human OCT2 and MATE1 Expressed in Chinese Hamster Ovary Cells Abstract MATE1 (multidrug and toxin extruder 1) and OCT2 (organic cation transporter 2) play critical roles in organic cation excretion by the human kidney. The transporter turnover rate (TOR) is relevant to understanding both th... |
PMC9274742 | core_pubmed_pmc | A multimodal imaging workflow for monitoring CAR T cell therapy against solid tumor from whole-body to single-cell level | A multimodal imaging workflow for monitoring CAR T cell therapy against solid tumor from whole-body to single-cell level Abstract CAR T cell research in solid tumors often lacks spatiotemporal information and therefore, there is a need for a molecular tomography to facilitate high-throughput preclinical monitoring of C... |
PMC11968489 | core_pubmed_pmc | The impact of circadian rhythm disruption on oxaliplatin tolerability and pharmacokinetics in Cry1 −/− Cry2 −/− mice under constant darkness | The impact of circadian rhythm disruption on oxaliplatin tolerability and pharmacokinetics in Cry1 −/− Cry2 −/− mice under constant darkness Abstract Abstract Circadian rhythms, the 24-h oscillations of biological activities guided by the molecular clock, play a pivotal role in regulating various physiological processe... |
PMC7508607 | core_pubmed_pmc | Phase I EnACT Trial of the Safety and Tolerability of a Novel Oral Formulation of Amphotericin B | Phase I EnACT Trial of the Safety and Tolerability of a Novel Oral Formulation of Amphotericin B Abstract Amphotericin B deoxycholate (AMB) has substantial toxicities. A novel encochleated amphotericin B deoxycholate (cAMB) formulation has oral bioavailability, efficacy in an animal model, and minimal toxicity due to t... |
PMC7419402 | core_pubmed_pmc | Remimazolam Has Low Oral Bioavailability and No Potential for Misuse in Drug-Facilitated Sexual Assaults, with or Without Alcohol: Results from Two Randomised Clinical Trials | Remimazolam Has Low Oral Bioavailability and No Potential for Misuse in Drug-Facilitated Sexual Assaults, with or Without Alcohol: Results from Two Randomised Clinical Trials Abstract Abstract Background and Objectives Remimazolam is a new ultra-short-acting benzodiazepine currently being developed for intravenous use ... |
PMC5338811 | core_pubmed_pmc | Antimicrobial use in paediatric patients in a teaching hospital in Ethiopia | Antimicrobial use in paediatric patients in a teaching hospital in Ethiopia Abstract Background Antibiotics use in in children are different from adults due to a lack of data on pharmacokinetics, pharmacodynamics, efficacy and safety of drugs, different physiological spectrum, pediatrics populations being vulnerable to... |
PMC7468908 | core_pubmed_pmc | Inhibitory Effects of Quercetin and Its Main Methyl, Sulfate, and Glucuronic Acid Conjugates on Cytochrome P450 Enzymes, and on OATP, BCRP and MRP2 Transporters | Inhibitory Effects of Quercetin and Its Main Methyl, Sulfate, and Glucuronic Acid Conjugates on Cytochrome P450 Enzymes, and on OATP, BCRP and MRP2 Transporters Abstract Abstract Quercetin is a flavonoid, its glycosides and aglycone are found in significant amounts in several plants and dietary supplements. Because of ... |
PMC5865657 | core_pubmed_pmc | Association analysis of SNPs present in plasma with adverse events and population pharmacokinetics in Chinese sunitinib treated patients with renal cell carcinoma | Association analysis of SNPs present in plasma with adverse events and population pharmacokinetics in Chinese sunitinib treated patients with renal cell carcinoma Abstract Background Sunitinib is a tyrosine kinase inhibitor with effective therapeutic outcomes in patients with renal-cell carcinoma. The study were to ana... |
PMC5928880 | core_pubmed_pmc | Glucocorticoids Inhibit Oncogenic RUNX1-ETO in Acute Myeloid Leukemia with Chromosome Translocation t(8;21) | Glucocorticoids Inhibit Oncogenic RUNX1-ETO in Acute Myeloid Leukemia with Chromosome Translocation t(8;21) Abstract Acute myeloid leukemia (AML) is a major blood cancer with poor prognosis. New therapies are needed to target oncogene-driven leukemia stem cells, which account for relapse and resistance. Chromosome tran... |
PMC9978593 | core_pubmed_pmc | Plasma concentration of orally administered amoxicillin and clindamycin in patients receiving haemodialysis | Plasma concentration of orally administered amoxicillin and clindamycin in patients receiving haemodialysis Abstract Abstract Objectives In the randomized controlled trial PANTHEM, the prophylactic effect of oral amoxicillin or clindamycin is investigated in patients receiving chronic haemodialysis (HD). However, data ... |
PMC11627180 | core_pubmed_pmc | Translational findings support regimen selection for first‐in‐human study of ubamatamab (MUC16 × CD3 bispecific antibody) in patients with recurrent ovarian cancer | Translational findings support regimen selection for first‐in‐human study of ubamatamab (MUC16 × CD3 bispecific antibody) in patients with recurrent ovarian cancer Abstract Abstract Ubamatamab, a Mucin 16 (MUC16) × cluster of differentiation 3 (CD3) bispecific antibody that promotes T‐cell‐mediated cytotoxicity of MUC1... |
PMC5114200 | core_pubmed_pmc | Lithium in Bipolar Disorder: Optimizing Therapy Using Prolonged-Release Formulations | Lithium in Bipolar Disorder: Optimizing Therapy Using Prolonged-Release Formulations Abstract Lithium has been a gold standard in the treatment of bipolar disorder (BD) for several decades. Despite a general reduction in the use of lithium over the past several years, it is effective in the management of both manic and... |
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