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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...