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PMC5034095
core_pubmed_pmc
A randomized safety and pharmacokinetic trial of daily tenofovir 1% gel in term and near-term pregnancy
A randomized safety and pharmacokinetic trial of daily tenofovir 1% gel in term and near-term pregnancy Abstract Abstract Introduction Vaginal tenofovir (TFV) 1% gel may reduce incident HIV-1 and herpes simplex virus 2 infection. Pregnancy may increase risk of HIV acquisition, and incident HIV in pregnancy potentiates ...
PMC4262094
core_pubmed_pmc
A Randomized Study of the Relative Pharmacokinetics, Pharmacodynamics, and Safety of Alirocumab, a Fully Human Monoclonal Antibody to PCSK9, After Single Subcutaneous Administration at Three Different Injection Sites in Healthy Subjects
A Randomized Study of the Relative Pharmacokinetics, Pharmacodynamics, and Safety of Alirocumab, a Fully Human Monoclonal Antibody to PCSK9, After Single Subcutaneous Administration at Three Different Injection Sites in Healthy Subjects Abstract Aims We investigated the relative pharmacokinetics, pharmacodynamics, and ...
PMC5525553
core_pubmed_pmc
A Pharmacodynamic Analysis of Choroidal Neovascularization in a Porcine Model Using Three Targeted Drugs
A Pharmacodynamic Analysis of Choroidal Neovascularization in a Porcine Model Using Three Targeted Drugs Abstract Purpose To compare the efficacy of microneedle-delivered suprachoroidal (SC) pazopanib to intravitreal (Ivit) delivery of pazopanib, bevacizumab, or a fusion protein hI-con1 versus vehicle controls on choro...
PMC12735885
core_pubmed_pmc
A Systematic Review and Meta-Analysis of Doxazosin Pharmacokinetics in Healthy and Diseased Populations
A Systematic Review and Meta-Analysis of Doxazosin Pharmacokinetics in Healthy and Diseased Populations Abstract Abstract Background: Doxazosin, an α 1 -adrenergic antagonist, is commonly used in the management of hypertension and benign prostatic hyperplasia (BPH). Pharmacokinetic (PK) variability across populations m...
PMC7529331
core_pubmed_pmc
Pharmacokinetic, pharmacodynamic, and neurochemical investigations of lamotrigine‐pentylenetetrazole kindled mice to ascertain it as a reliable model for clinical drug‐resistant epilepsy
Pharmacokinetic, pharmacodynamic, and neurochemical investigations of lamotrigine‐pentylenetetrazole kindled mice to ascertain it as a reliable model for clinical drug‐resistant epilepsy Abstract Abstract Background Pentylenetetrazole kindling has long been used for the screening of investigational antiseizure drugs. T...
PMC4260137
core_pubmed_pmc
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES Abstract The factor Xa inhibitor apixaban is one of the novel anticoagulants to emerge as alternatives to long-standing standards of care that include low-molecular-weight heparin and warfarin. The development of apixaban reflects a strategy to optimize the clinical pharmacolo...
PMC11064047
core_pubmed_pmc
Tailoring of Bilosomal Nanogel for Augmenting the Off-Label Use of Sildenafil Citrate in Pediatric Pulmonary Hypertension
Tailoring of Bilosomal Nanogel for Augmenting the Off-Label Use of Sildenafil Citrate in Pediatric Pulmonary Hypertension Abstract Pediatric pulmonary hypertension is a serious syndrome with significant morbidity and mortality. Sildenafil is widely used off-label in pediatric patients with pulmonary arterial hypertensi...
PMC7713806
core_pubmed_pmc
Accuracy assessment of a PION TCI pump based on international standards
Accuracy assessment of a PION TCI pump based on international standards Abstract Abstract Background Inaccuracies associated with target-controlled infusion (TCI) delivery systems are attributable to both software and hardware issues, as well as pharmacokinetic variability. However, little is known about the inaccuracy...
PMC11465679
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of a single intravenous dose of SHR-1707 in healthy adult subjects: two randomized, double-blind, single-ascending-dose, phase 1 studies
Safety, tolerability, pharmacokinetics and pharmacodynamics of a single intravenous dose of SHR-1707 in healthy adult subjects: two randomized, double-blind, single-ascending-dose, phase 1 studies Abstract Abstract Background SHR-1707 is a novel humanized anti-Aβ IgG1 monoclonal antibody that binds to Aβ fibrils and mo...
PMC9660540
core_pubmed_pmc
Phase Ia/b, Open-Label, Multicenter Study of AZD4635 (an Adenosine A2A Receptor Antagonist) as Monotherapy or Combined with Durvalumab, in Patients with Solid Tumors
Phase Ia/b, Open-Label, Multicenter Study of AZD4635 (an Adenosine A2A Receptor Antagonist) as Monotherapy or Combined with Durvalumab, in Patients with Solid Tumors Abstract Abstract Purpose: To evaluate AZD4635, an adenosine A 2A receptor antagonist, as monotherapy or in combination with durvalumab in patients with a...
PMC11744960
core_pubmed_pmc
Urinary phthalate metabolites associated with increased prevalence of gallstone disease in U.S. adults: data from the NHANES study
Urinary phthalate metabolites associated with increased prevalence of gallstone disease in U.S. adults: data from the NHANES study Abstract Background Phthalate exposure has been hypothesized to influence cholesterol metabolism and gallstone pathogenesis, but previous studies are limited. We aimed to examine the associ...
PMC8346919
core_pubmed_pmc
A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Pharmacodynamic Effects of VX-150, a Highly Selective Na V 1.8 Inhibitor, in Healthy Male Adults
A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Pharmacodynamic Effects of VX-150, a Highly Selective Na V 1.8 Inhibitor, in Healthy Male Adults Abstract Abstract Objective To evaluate the analgesic potential, safety, tolerability, and pharmacokinetics of VX-150, a pro-drug of a...
PMC9702083
core_pubmed_pmc
Pharmacodynamic evaluation of lefamulin in the treatment of gonorrhea using a hollow fiber infection model simulating Neisseria gonorrhoeae infections
Pharmacodynamic evaluation of lefamulin in the treatment of gonorrhea using a hollow fiber infection model simulating Neisseria gonorrhoeae infections Abstract The emergence and spread of antimicrobial resistance in Neisseria gonorrhoeae is seriously threatening the treatment and control of gonorrhea globally. Novel tr...
PMC3640601
core_pubmed_pmc
Advances in antiplatelet technologies to improve cardiovascular disease morbidity and mortality: a review of ticagrelor
Advances in antiplatelet technologies to improve cardiovascular disease morbidity and mortality: a review of ticagrelor Abstract Antiplatelet therapy is widely used with proven benefit for the prevention of further ischemic cardiac complications in patients with acute coronary syndrome. Treatment guidelines for acute c...
PMC3899448
core_pubmed_pmc
Pharmacokinetics, Safety and Tolerability of Rotigotine Transdermal Patch in Healthy Japanese and Caucasian Subjects
Pharmacokinetics, Safety and Tolerability of Rotigotine Transdermal Patch in Healthy Japanese and Caucasian Subjects Abstract Abstract Background and Objectives Rotigotine is a dopamine receptor agonist with activity across the D 1 through to D 5 receptors as well as select serotonergic and adrenergic sites; continuous...
PMC12399214
core_pubmed_pmc
Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects
Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects Abstract Invasive fungal infections (IFIs) have become prominent global health threats, escalating the burden on public health systems. The increasing occurrence of invasive fungal infections is due primarily to the extensive application of ...
PMC4269818
core_pubmed_pmc
Ibuprofen Sodium Is Absorbed Faster than Standard Ibuprofen Tablets: Results of Two Open-Label, Randomized, Crossover Pharmacokinetic Studies
Ibuprofen Sodium Is Absorbed Faster than Standard Ibuprofen Tablets: Results of Two Open-Label, Randomized, Crossover Pharmacokinetic Studies Abstract Abstract Background A novel ibuprofen (IBU) formulation, Advil ® Film-Coated Tablets (IBU Na ), was developed. Objective Pharmacokinetic comparison of IBU Na versus othe...
PMC7214649
core_pubmed_pmc
Semimechanistic Modeling to Guide Venetoclax Coadministration with Ritonavir and Digoxin
Semimechanistic Modeling to Guide Venetoclax Coadministration with Ritonavir and Digoxin Abstract Venetoclax is a cytochrome P450, family 3, subfamily A (CYP3A) substrate and was shown to inhibit P‐gp efflux transporters in vitro . To quantify the impact of CYP3A inhibition by ritonavir on venetoclax disposition and P‐...
PMC8374068
core_pubmed_pmc
A Critical Review of the Evidence That Metformin Is a Putative Anti-Aging Drug That Enhances Healthspan and Extends Lifespan
A Critical Review of the Evidence That Metformin Is a Putative Anti-Aging Drug That Enhances Healthspan and Extends Lifespan Abstract The numerous beneficial health outcomes associated with the use of metformin to treat patients with type 2 diabetes (T2DM), together with data from pre-clinical studies in animals includ...
PMC11942484
core_pubmed_pmc
A Novel Recombinant Human FGF21 Analog with High Glycosylation Has a Prolonged Half-Life and Affects Glycemic and Body Weight Control
A Novel Recombinant Human FGF21 Analog with High Glycosylation Has a Prolonged Half-Life and Affects Glycemic and Body Weight Control Abstract Fibroblast growth factor 21 (FGF21), a hormone-like protein, plays a crucial role in enhancing glucose and lipid metabolism, offering promising therapeutic avenues for condition...
PMC11787782
core_pubmed_pmc
Pharmacodynamic Modeling of Warfarin Dosing Algorithm for Cardiovascular Patients in Indonesia: A Tailored Method to Anticoagulation Therapy
Pharmacodynamic Modeling of Warfarin Dosing Algorithm for Cardiovascular Patients in Indonesia: A Tailored Method to Anticoagulation Therapy Abstract Abstract Purpose Warfarin is an anticoagulant drug widely used for treating thromboembolism-related conditions. The main challenge with this drug is the high variability ...
PMC6897292
core_pubmed_pmc
Development, Testing, Parameterization, and Calibration of a Human Physiologically Based Pharmacokinetic Model for the Plasticizer, Hexamoll ® Diisononyl-Cyclohexane-1, 2-Dicarboxylate Using In Silico , In Vitro , and Human Biomonitoring Data
Development, Testing, Parameterization, and Calibration of a Human Physiologically Based Pharmacokinetic Model for the Plasticizer, Hexamoll ® Diisononyl-Cyclohexane-1, 2-Dicarboxylate Using In Silico , In Vitro , and Human Biomonitoring Data Abstract A physiologically based pharmacokinetic model for Hexamoll ® diisono...
PMC8519033
core_pubmed_pmc
Liraglutide pharmacokinetics and exposure‐response in adolescents with obesity
Liraglutide pharmacokinetics and exposure‐response in adolescents with obesity Abstract Summary Background Obesity in adolescence presents a major public health challenge, often leading to obesity in adulthood with associated chronic disease. Objectives This study aimed to perform a population pharmacokinetic and expos...
PMC7612404
core_pubmed_pmc
Concentration-Response Relationships of Dolutegravir and Efavirenz with Weight Change After Starting Antiretroviral Therapy
Concentration-Response Relationships of Dolutegravir and Efavirenz with Weight Change After Starting Antiretroviral Therapy Abstract Abstract Aim Dolutegravir is associated with more weight gain than efavirenz in people starting antiretroviral therapy (ART). We investigated the concentration-response relationships of e...
PMC12130374
core_pubmed_pmc
Phase I Study of Sorafenib Combined with Gemcitabine and Carboplatin in Patients with Advanced Solid Tumors
Phase I Study of Sorafenib Combined with Gemcitabine and Carboplatin in Patients with Advanced Solid Tumors Abstract Abstract Introduction A combination of targeted anticancer drugs with cytotoxic therapy can potentially overcome multidrug resistance. The multi-target kinase inhibitor sorafenib demonstrates synergistic...
PMC6937755
core_pubmed_pmc
A phase 1, randomized, open-label, single-dose study to assess the relative bioavailability of a subcutaneous dose of FKB327 when administered using a prefilled syringe, a prefilled auto-injector, or a vial with disposable syringe in healthy subjects
A phase 1, randomized, open-label, single-dose study to assess the relative bioavailability of a subcutaneous dose of FKB327 when administered using a prefilled syringe, a prefilled auto-injector, or a vial with disposable syringe in healthy subjects Abstract Abstract Background/objective FKB327 is a biosimilar of the ...
PMC6743242
core_pubmed_pmc
A Review of Controlled Drug Delivery Systems Based on Cells and Cell Membranes
A Review of Controlled Drug Delivery Systems Based on Cells and Cell Membranes Abstract Novel drug delivery systems have ameliorated drugs’ pharmacokinetics and declined undesired ramifications while led to a better patient compliance by extending the time of release. In fact, although there has been a multitude of enc...
PMC8070284
core_pubmed_pmc
Pharmacokinetic Characterization of LW6, a Novel Hypoxia-Inducible Factor-1α (HIF-1α) Inhibitor in Mice
Pharmacokinetic Characterization of LW6, a Novel Hypoxia-Inducible Factor-1α (HIF-1α) Inhibitor in Mice Abstract Abstract LW6, an (aryloxyacetylamino)benzoic acid derivative, was recently identified to be an inhibitor of hypoxia-inducible factor-1α (HIF-1α), which is an attractive target for cancer therapeutics. Althou...
PMC6273138
core_pubmed_pmc
Inhibitory Effects of Aschantin on Cytochrome P450 and Uridine 5′-diphospho-glucuronosyltransferase Enzyme Activities in Human Liver Microsomes
Inhibitory Effects of Aschantin on Cytochrome P450 and Uridine 5′-diphospho-glucuronosyltransferase Enzyme Activities in Human Liver Microsomes Abstract Abstract Aschantin is a bioactive neolignan found in Magnolia flos with antiplasmodial, Ca 2+ -antagonistic, platelet activating factor-antagonistic, and chemopreventi...
PMC12517267
core_pubmed_pmc
Acceptability of 100-mg moxifloxacin in children with rifampicin-resistant TB in three high-burden countries
Acceptability of 100-mg moxifloxacin in children with rifampicin-resistant TB in three high-burden countries Abstract SUMMARY BACKGROUND Routinely, a 400-mg tablet of moxifloxacin is used in children with rifampicin-resistant TB (RR-TB), but it has very poor acceptability. We describe the acceptability of a 100-mg disp...
PMC6182726
core_pubmed_pmc
Physiologically based pharmacokinetic-quantitative systems toxicology and safety (PBPK-QSTS) modeling approach applied to predict the variability of amitriptyline pharmacokinetics and cardiac safety in populations and in individuals
Physiologically based pharmacokinetic-quantitative systems toxicology and safety (PBPK-QSTS) modeling approach applied to predict the variability of amitriptyline pharmacokinetics and cardiac safety in populations and in individuals Abstract Abstract The physiologically based pharmacokinetic (PBPK) models allow for pre...
PMC10761441
core_pubmed_pmc
Kinetically-derived maximal dose (KMD) indicates lack of human carcinogenicity of ethylbenzene
Kinetically-derived maximal dose (KMD) indicates lack of human carcinogenicity of ethylbenzene Abstract Abstract The kinetically-derived maximal dose (KMD) is defined as the maximal external dose at which kinetics are unchanged relative to lower doses, e.g., doses at which kinetic processes are not saturated. Toxicity ...
PMC10215112
core_pubmed_pmc
The Clinical Pharmacology and Therapeutic Evaluation of Non-Steroidal Anti-Inflammatory Drugs in Adult Horses
The Clinical Pharmacology and Therapeutic Evaluation of Non-Steroidal Anti-Inflammatory Drugs in Adult Horses Abstract Simple Summary Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed in equine practice for a variety of painful or inflammatory conditions. This review discusses the clinical pharmaco...
PMC5094513
core_pubmed_pmc
Palmitoylethanolamide for the treatment of pain: pharmacokinetics, safety and efficacy
Palmitoylethanolamide for the treatment of pain: pharmacokinetics, safety and efficacy Abstract Abstract Palmitoylethanolamide (PEA) has been suggested to have useful analgesic properties and to be devoid of unwanted effects. Here, we have examined critically this contention, and discussed available data concerning the...
PMC8712478
core_pubmed_pmc
Mechanisms of the Rapid Effects of Ketamine on Depression and Sleep Disturbances: A Narrative Review
Mechanisms of the Rapid Effects of Ketamine on Depression and Sleep Disturbances: A Narrative Review Abstract Abstract Recently, sleep has been recognized as a crucial factor for health and longevity. The daily sleep/wake cycle provides the basis of biorhythm, which controls whole-body homeostasis and homeodynamics. Sl...
PMC12414074
core_pubmed_pmc
Malnutrition and Its Effect on Drug Pharmacokinetics: A Clinical Perspective
Malnutrition and Its Effect on Drug Pharmacokinetics: A Clinical Perspective Abstract Abstract Malnutrition significantly alters the pharmacokinetics of medications, particularly in vulnerable populations such as children, pregnant women, elderly individuals, and individuals in low- and middle-income countries. These p...
PMC6765692
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Evaluation of Dexlansoprazole Infusion Injection Compared with Lansoprazole in Healthy Chinese Adults
Pharmacokinetic/Pharmacodynamic Evaluation of Dexlansoprazole Infusion Injection Compared with Lansoprazole in Healthy Chinese Adults Abstract Background and Objective This study was performed in healthy Chinese subjects to evaluate the safety and pharmacokinetic/pharmacodynamic characteristics of a novel injection for...
PMC9221162
core_pubmed_pmc
Low-Dose Metronomic Topotecan and Pazopanib (TOPAZ) in Children with Relapsed or Refractory Solid Tumors: A C17 Canadian Phase I Clinical Trial
Low-Dose Metronomic Topotecan and Pazopanib (TOPAZ) in Children with Relapsed or Refractory Solid Tumors: A C17 Canadian Phase I Clinical Trial Abstract Abstract Simple Summary Low-dose continuous oral chemotherapy may work together with targeted tyrosine kinase inhibitors to target a cancer’s ability to promote new bl...
PMC11347695
core_pubmed_pmc
Under-representation of older Indian persons with cancer in clinical trials
Under-representation of older Indian persons with cancer in clinical trials Abstract Abstract Objective Older patients with cancer have traditionally been under-represented in global clinical trials. There are no data from India regarding this issue. Methods and analysis This was a retrospective analysis done at our in...
PMC3449383
core_pubmed_pmc
E-Pharmacophore mapping and docking studies on Vitamin D receptor (VDR)
E-Pharmacophore mapping and docking studies on Vitamin D receptor (VDR) Abstract Abstract Small structured chemical molecules are importance in the field of molecular medicine since their pharmacokinetic and pharmacodynamic properties are predictable and because of its ability to bind with target molecules and execute ...
PMC9876276
core_pubmed_pmc
The pharmacokinetics and pharmacodynamics of cefquinome against Streptococcus agalactiae in a murine mastitis model
The pharmacokinetics and pharmacodynamics of cefquinome against Streptococcus agalactiae in a murine mastitis model Abstract Abstract Cefquinome is a new generation cephalosporin that is effective in the treatment of mastitis in animals. In this study, we evaluated the associations between the specific pharmacokinetics...
PMC2889733
core_pubmed_pmc
Preclinical PK and PD Studies on 2′- O -Methyl-phosphorothioate RNA Antisense Oligonucleotides in the mdx Mouse Model
Preclinical PK and PD Studies on 2′- O -Methyl-phosphorothioate RNA Antisense Oligonucleotides in the mdx Mouse Model Abstract Abstract Antisense oligonucleotides (AONs) are being developed as RNA therapeutic molecules for Duchenne muscular dystrophy. For oligonucleotides with the 2′- O -methyl-phosphorothioate (2OMePS...
PMC7038312
core_pubmed_pmc
Mechanistic Modeling of Mycobacterium tuberculosis Infection in Murine Models for Drug and Vaccine Efficacy Studies
Mechanistic Modeling of Mycobacterium tuberculosis Infection in Murine Models for Drug and Vaccine Efficacy Studies Abstract Tuberculosis (TB) drug, regimen, and vaccine development rely heavily on preclinical animal experiments, and quantification of bacterial and immune response dynamics is essential for understandin...
PMC4745832
core_pubmed_pmc
Randomized clinical trial: pharmacokinetics and safety of multimatrix mesalamine for treatment of pediatric ulcerative colitis
Randomized clinical trial: pharmacokinetics and safety of multimatrix mesalamine for treatment of pediatric ulcerative colitis Abstract Abstract Background Limited data are available on mesalamine (5-aminosalicylic acid; 5-ASA) use in pediatric ulcerative colitis (UC). Aim To evaluate pharmacokinetic and safety profile...
PMC11718548
core_pubmed_pmc
Microneedles as a Promising Technology for Disease Monitoring and Drug Delivery: A Review
Microneedles as a Promising Technology for Disease Monitoring and Drug Delivery: A Review Abstract The delivery of molecules, such as DNA, RNA, peptides, and certain hydrophilic drugs, across the epidermal barrier poses a significant obstacle. Microneedle technology has emerged as a prominent area of focus in biomedica...
PMC10719490
core_pubmed_pmc
A first‐in‐human phase I study of SHR‐1906, a humanized monoclonal antibody against connective tissue growth factor, in healthy participants
A first‐in‐human phase I study of SHR‐1906, a humanized monoclonal antibody against connective tissue growth factor, in healthy participants Abstract Abstract New therapeutic targets and drugs are urgently needed to halt the fibrosing process in idiopathic pulmonary fibrosis (IPF). SHR‐1906 is a novel fully humanized m...
PMC9633485
core_pubmed_pmc
Microdialysis of Drug and Drug Metabolite: a Comprehensive In Vitro Analysis for Voriconazole and Voriconazole N -oxide
Microdialysis of Drug and Drug Metabolite: a Comprehensive In Vitro Analysis for Voriconazole and Voriconazole N -oxide Abstract Purpose Voriconazole is a therapeutically challenging antifungal drug associated with high interindividual pharmacokinetic variability. As a prerequisite to performing clinical trials using t...
PMC7220402
core_pubmed_pmc
Pharmacokinetic evaluation of MFF in combinations with tacrolimus and cyclosporine. Findings of C 0 and AUC
Pharmacokinetic evaluation of MFF in combinations with tacrolimus and cyclosporine. Findings of C 0 and AUC Abstract Abstract We hypothesized that area under the concentration time curve (AUC (0-12) ) is more accurate pharmacokinetic predictor vs trough level of mycophenolic acid (C 0 ). Study was performed at the Univ...
PMC9750107
core_pubmed_pmc
Efficacy and Safety of Alirocumab in Children and Adolescents With Homozygous Familial Hypercholesterolemia: Phase 3, Multinational Open-Label Study
Efficacy and Safety of Alirocumab in Children and Adolescents With Homozygous Familial Hypercholesterolemia: Phase 3, Multinational Open-Label Study Abstract Background: Despite progress in treating homozygous familial hypercholesterolemia, most patients do not achieve low-density lipoprotein cholesterol (LDL-C) target...
PMC5613062
core_pubmed_pmc
A phase I dose-escalation study of Selumetinib in combination with Erlotinib or Temsirolimus in patients with advanced solid tumors
A phase I dose-escalation study of Selumetinib in combination with Erlotinib or Temsirolimus in patients with advanced solid tumors Abstract Summary Background Combinations of molecularly targeted agents may provide optimal anti-tumor activity and improve clinical outcomes for patients with advanced cancers. Selumetini...
PMC7591420
core_pubmed_pmc
Phase Ib Trial of the PI3K Inhibitor Copanlisib Combined with the Allosteric MEK Inhibitor Refametinib in Patients with Advanced Cancer
Phase Ib Trial of the PI3K Inhibitor Copanlisib Combined with the Allosteric MEK Inhibitor Refametinib in Patients with Advanced Cancer Abstract Background Dual inhibition of PI3K and MAPK signaling is conceptually a promising anticancer therapy. Objective This phase 1b trial investigated the safety, maximum tolerated ...
PMC5610536
core_pubmed_pmc
Effect of Rifampin on the Single-Dose Pharmacokinetics of Oral Cabotegravir in Healthy Subjects
Effect of Rifampin on the Single-Dose Pharmacokinetics of Oral Cabotegravir in Healthy Subjects Abstract ABSTRACT Drug-drug interactions between antiretroviral medications and rifampin complicate the treatment of HIV and tuberculosis coinfection. This study evaluated the effect of rifampin on the pharmacokinetics of or...
PMC9599027
core_pubmed_pmc
Individual Pharmacotherapy Management (IPM)—IV: Optimized Usage of Approved Antimicrobials Addressing Under-Recognized Adverse Drug Reactions and Drug-Drug Interactions in Polypharmacy
Individual Pharmacotherapy Management (IPM)—IV: Optimized Usage of Approved Antimicrobials Addressing Under-Recognized Adverse Drug Reactions and Drug-Drug Interactions in Polypharmacy Abstract Abstract Antimicrobial therapy is often a life-saving medical intervention for inpatients and outpatients. Almost all medical ...
PMC6025223
core_pubmed_pmc
A Phase II Study of Pelareorep (REOLYSIN ® ) in Combination with Gemcitabine for Patients with Advanced Pancreatic Adenocarcinoma
A Phase II Study of Pelareorep (REOLYSIN ® ) in Combination with Gemcitabine for Patients with Advanced Pancreatic Adenocarcinoma Abstract Abstract Pancreatic ductal adenocarcinoma (PDAC) has a poor prognosis, with 1 and 5-year survival rates of ~18% and 7% respectively. FOLFIRINOX or gemcitabine in combination with na...
PMC12934543
core_pubmed_pmc
Population Pharmacokinetics Analysis of Talazoparib and Enzalutamide Combination Therapy for Patients With Metastatic Castration‐Resistant Prostate Cancer
Population Pharmacokinetics Analysis of Talazoparib and Enzalutamide Combination Therapy for Patients With Metastatic Castration‐Resistant Prostate Cancer Abstract Abstract The poly(ADP‐ribose) polymerase inhibitor talazoparib, combined with the androgen receptor inhibitor enzalutamide is approved for patients with hom...
PMC3467880
core_pubmed_pmc
Pharmacodynamic responses of exogenous epinephrine during mandibular third molar surgery
Pharmacodynamic responses of exogenous epinephrine during mandibular third molar surgery Abstract Abstract Background: The systemic effects attributable to the injection of dental local anesthetic solutions have been the subject of discussion for many years. Aim and Objective: The aim of the present study was to invest...
PMC8307098
core_pubmed_pmc
Synthesis and Bioinformatic Characterization of New Schiff Bases with Possible Applicability in Brain Disorders
Synthesis and Bioinformatic Characterization of New Schiff Bases with Possible Applicability in Brain Disorders Abstract (1) Background: The research aims to find new treatments for neurodegenerative diseases, in particular, Alzheimer’s disease. (2) Methods: This article presents a bioinformatics and pathology study of...
PMC8810887
core_pubmed_pmc
Citrate pharmacokinetics in critically ill liver failure patients receiving CRRT
Citrate pharmacokinetics in critically ill liver failure patients receiving CRRT Abstract Abstract Citrate has been proposed as anticoagulation of choice in continuous renal replacement therapy (CRRT). However, little is known about the pharmacokinetics (PK) and metabolism of citrate in liver failure patients who requi...
PMC11035515
core_pubmed_pmc
Drug–Drug Interaction Studies of Esmethadone (REL-1017) Involving CYP3A4- and CYP2D6-Mediated Metabolism
Drug–Drug Interaction Studies of Esmethadone (REL-1017) Involving CYP3A4- and CYP2D6-Mediated Metabolism Abstract Abstract Background and Objective Esmethadone (dextromethadone; d-methadone; S-methadone (+)-methadone; REL-1017) is the opioid inactive dextro-isomer of racemic methadone. Esmethadone is a low potency N-me...
PMC6842130
core_pubmed_pmc
Fluorophotometric Assessment of Tear Volume and Turnover Rate in Healthy Dogs and Cats
Fluorophotometric Assessment of Tear Volume and Turnover Rate in Healthy Dogs and Cats Abstract Abstract Purpose: The study establishes normative data of tear volume (TV) and tear turnover rate (TTR) in healthy dogs and cats, 2 species commonly used for translational research in ophthalmology. Methods: Thirty-six dogs ...
PMC10836316
core_pubmed_pmc
First-in-Human Phase I Study of Minnelide in Patients With Advanced Gastrointestinal Cancers: Safety, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity
First-in-Human Phase I Study of Minnelide in Patients With Advanced Gastrointestinal Cancers: Safety, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity Abstract Abstract Background Minnelide is a water-soluble prodrug of triptolide. Triptolide is an anticancer agent that targets cancer resistance through sever...
PMC11897840
core_pubmed_pmc
Prolonged Elimination of Lamotrigine After Suicidal Overdose: A Case Report
Prolonged Elimination of Lamotrigine After Suicidal Overdose: A Case Report Abstract Lamotrigine (LTG) is an antiepileptic drug that stabilizes neuronal membranes by inhibiting excitatory neurotransmitter release, thereby reducing neuronal excitation. Various factors can contribute to its metabolic dysfunction. A 22-ye...
PMC4270037
core_pubmed_pmc
Mycophenolic acid AUC in Thai kidney transplant recipients receiving low dose mycophenolate and its association with UGT2B7 polymorphisms
Mycophenolic acid AUC in Thai kidney transplant recipients receiving low dose mycophenolate and its association with UGT2B7 polymorphisms Abstract Abstract Background Despite use of a lower mycophenolate dose in Thai kidney transplant patients, acceptable graft and patient outcomes can be achieved. We therefore examine...
PMC5788216
core_pubmed_pmc
Development of Nanoemulsion Based Gel Loaded with Phytoconstituents for the Treatment of Urinary Tract Infection and in Vivo Biodistribution Studies
Development of Nanoemulsion Based Gel Loaded with Phytoconstituents for the Treatment of Urinary Tract Infection and in Vivo Biodistribution Studies Abstract Purpose: A nanoemulsion based gel containing Polyphenon 60 (P60) and cranberry (CRB) has been developed to deliver via intravaginal route for the treatment of uri...
PMC5887840
core_pubmed_pmc
Population Pharmacokinetics of Durvalumab in Cancer Patients and Association With Longitudinal Biomarkers of Disease Status
Population Pharmacokinetics of Durvalumab in Cancer Patients and Association With Longitudinal Biomarkers of Disease Status Abstract Abstract The objectives of this analysis were to develop a population pharmacokinetics (PK) model of durvalumab, an anti‐PD‐L1 antibody, and quantify the impact of baseline and time‐varyi...
PMC6863819
core_pubmed_pmc
Effect of food on the pharmacokinetics and therapeutic efficacy of 4-phenylbutyrate in progressive familial intrahepatic cholestasis
Effect of food on the pharmacokinetics and therapeutic efficacy of 4-phenylbutyrate in progressive familial intrahepatic cholestasis Abstract Abstract Progressive familial intrahepatic cholestasis (PFIC), a rare inherited disorder, progresses to liver failure in childhood. We have shown that sodium 4-phenylbutyrate (Na...
PMC10671645
core_pubmed_pmc
The Interplay of Permeability, Metabolism, Transporters, and Dosing in Determining the Dynamics of the Tissue/Plasma Partition Coefficient and Volume of Distribution—A Theoretical Investigation Using Permeability-Limited, Physiologically Based Pharmacokinetic Modeling
The Interplay of Permeability, Metabolism, Transporters, and Dosing in Determining the Dynamics of the Tissue/Plasma Partition Coefficient and Volume of Distribution—A Theoretical Investigation Using Permeability-Limited, Physiologically Based Pharmacokinetic Modeling Abstract A permeability-limited physiologically bas...
PMC12103781
core_pubmed_pmc
Phase I study of the safety, tolerability, and potential therapeutic dose of OMT-110 for patients with refractory metastatic Colorectal Cancer
Phase I study of the safety, tolerability, and potential therapeutic dose of OMT-110 for patients with refractory metastatic Colorectal Cancer Abstract Background OMT-110 is a repositioned drug candidate for the treatment of metastatic colorectal cancer (mCRC). This phase I study aimed to determine the appropriate dose...
PMC4288327
core_pubmed_pmc
Unraveling bisphenol A pharmacokinetics using physiologically based pharmacokinetic modeling
Unraveling bisphenol A pharmacokinetics using physiologically based pharmacokinetic modeling Abstract Abstract Physiologically based pharmacokinetic (PBPK) models integrate both chemical- and system-specific information into a mathematical framework, offering a mechanistic approach to predict the internal dose metrics ...
PMC5565246
core_pubmed_pmc
Potential drug–drug interactions in inpatients treated at the Internal Medicine ward of Tikur Anbessa Specialized Hospital
Potential drug–drug interactions in inpatients treated at the Internal Medicine ward of Tikur Anbessa Specialized Hospital Abstract Purpose Although the concomitant use of multiple drugs often increases therapeutic effectiveness, certain combinations result in unwanted drug–drug interactions (DDIs). Most interactions g...
PMC11289455
core_pubmed_pmc
JNJ-77242113, a highly potent, selective peptide targeting the IL-23 receptor, provides robust IL-23 pathway inhibition upon oral dosing in rats and humans
JNJ-77242113, a highly potent, selective peptide targeting the IL-23 receptor, provides robust IL-23 pathway inhibition upon oral dosing in rats and humans Abstract The interleukin (IL)-23 pathway is a pathogenic driver in psoriasis, psoriatic arthritis, and inflammatory bowel disease. Currently, no oral therapeutics s...
PMC6044797
core_pubmed_pmc
Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs
Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs Abstract Abstract Investigation into the pharmacokinetic profile of esomeprazole was conducted using eight healthy dogs after intravenous (IV) and oral (po) administration in a two-part randomized crossover study. The dogs we...
PMC9393138
core_pubmed_pmc
The use of a modified Delphi technique to develop a critical appraisal tool for clinical pharmacokinetic studies
The use of a modified Delphi technique to develop a critical appraisal tool for clinical pharmacokinetic studies Abstract Abstract Background Critical appraisal aids in assessing the quality of scientific literature, which is central to the practice of evidence-based medicine. Several tools and guidelines are available...
PMC7292875
core_pubmed_pmc
Intra-tumoral drug concentration mapping within solid tumor micro-milieu using in-vitro model and doxorubicin as a model drug
Intra-tumoral drug concentration mapping within solid tumor micro-milieu using in-vitro model and doxorubicin as a model drug Abstract Abstract In contrast to plasma pharmacokinetics, intratumoral pharmacokinetics of doxorubicin (DOX) determines its spatial anti-tumoral activity. Three-dimensional multicellular layers ...
PMC6668111
core_pubmed_pmc
Development of a human immuno-oncology therapeutic agent targeting HER2: targeted delivery of granzyme B
Development of a human immuno-oncology therapeutic agent targeting HER2: targeted delivery of granzyme B Abstract Abstract Background Immunotherapeutic approaches designed to augment T and B cell mediated killing of tumor cells has met with clinical success in recent years suggesting tremendous potential for treatment ...
PMC10800708
core_pubmed_pmc
Efficacies and ADME properties of redox active methylene blue and phenoxazine analogues for use in new antimalarial triple drug combinations with amino-artemisinins
Efficacies and ADME properties of redox active methylene blue and phenoxazine analogues for use in new antimalarial triple drug combinations with amino-artemisinins Abstract Abstract Efforts to develop new artemisinin triple combination therapies effective against artemisinin-tolerant strains of Plasmodium falciparum b...
PMC10681508
core_pubmed_pmc
PK/PD model‐informed dose selection for oncology phase I expansion: Case study based on PF‐06939999, a PRMT5 inhibitor
PK/PD model‐informed dose selection for oncology phase I expansion: Case study based on PF‐06939999, a PRMT5 inhibitor Abstract Abstract The optimal dose for targeted oncology therapeutics is often not the maximum tolerated dose. Pharmacokinetic/pharmacodynamic (PK/PD) modeling can be an effective tool to integrate cli...
PMC9587772
core_pubmed_pmc
Ask Your Provider About Cannabis: Increasing Nurse Practitioner Knowledge and Confidence
Ask Your Provider About Cannabis: Increasing Nurse Practitioner Knowledge and Confidence Abstract Abstract Introduction: Nurse practitioners (NPs) are authorizing providers for medical cannabis in many states, and may serve as a primary care clinician. We report findings from a nationally distributed 2-h continuing edu...
PMC10585000
core_pubmed_pmc
Mediation and longitudinal analysis to interpret the association between clozapine pharmacokinetics, pharmacogenomics, and absolute neutrophil count
Mediation and longitudinal analysis to interpret the association between clozapine pharmacokinetics, pharmacogenomics, and absolute neutrophil count Abstract Clozapine is effective at reducing symptoms of treatment-resistant schizophrenia, but it can also induce several adverse outcomes including neutropenia and agranu...
PMC10792358
core_pubmed_pmc
A Phase I/II Study of GSK525762 Combined with Fulvestrant in Patients with Hormone Receptor–positive/HER2-negative Advanced or Metastatic Breast Cancer
A Phase I/II Study of GSK525762 Combined with Fulvestrant in Patients with Hormone Receptor–positive/HER2-negative Advanced or Metastatic Breast Cancer Abstract Abstract Purpose: Endocrine-based therapy is the initial primary treatment option for hormone receptor–positive and human epidermal growth factor receptor 2-ne...
PMC4329422
core_pubmed_pmc
Clinical Pharmacology of Paracetamol in Neonates: A Review
Clinical Pharmacology of Paracetamol in Neonates: A Review Abstract Paracetamol is commonly used to control mild-to-moderate pain or to reduce opioid exposure as part of multimodal analgesia, and is the only compound recommended to treat fever in neonates. Paracetamol clearance is lower in neonates than in children and...
PMC10304400
core_pubmed_pmc
Prevalence and Risk Factors Associated with Potentially Inappropriate Prescribing According to STOPP-2 Criteria among Discharged Older Patients—An Observational Retrospective Study
Prevalence and Risk Factors Associated with Potentially Inappropriate Prescribing According to STOPP-2 Criteria among Discharged Older Patients—An Observational Retrospective Study Abstract Pharmacokinetic and pharmacodynamic changes associated with old age, along with multimorbidity and polypharmacy might lead to inap...
PMC9003587
core_pubmed_pmc
Drug interaction between carbamazepine and other antiepileptic drugs in Tunisian epileptic patients
Drug interaction between carbamazepine and other antiepileptic drugs in Tunisian epileptic patients Abstract Summary Introduction: Carbamazepine could be used on monotherapy or associated to other antiepileptic drugs (AED). In these cases, drug interactions should be taken into account. Aim: To assess the influence of ...
PMC7689089
core_pubmed_pmc
Regorafenib combined with PD1 blockade increases CD8 T-cell infiltration by inducing CXCL10 expression in hepatocellular carcinoma
Regorafenib combined with PD1 blockade increases CD8 T-cell infiltration by inducing CXCL10 expression in hepatocellular carcinoma Abstract Abstract Background and purpose Combining inhibitors of vascular endothelial growth factor and the programmed cell death protein 1 (PD1) pathway has shown efficacy in multiple canc...
PMC9599747
core_pubmed_pmc
Association of SLC22A1 , SLC22A2 , SLC47A1 , and SLC47A2 Polymorphisms with Metformin Efficacy in Type 2 Diabetic Patients
Association of SLC22A1 , SLC22A2 , SLC47A1 , and SLC47A2 Polymorphisms with Metformin Efficacy in Type 2 Diabetic Patients Abstract Abstract Response to metformin, first-line therapy for type 2 diabetes mellitus (T2DM), exists interindividual variation. Considering that transporters belonging to the solute carrier (SLC...
PMC6156772
core_pubmed_pmc
Can Population Modelling Principles be Used to Identify Key PBPK Parameters for Paediatric Clearance Predictions? An Innovative Application of Optimal Design Theory
Can Population Modelling Principles be Used to Identify Key PBPK Parameters for Paediatric Clearance Predictions? An Innovative Application of Optimal Design Theory Abstract Purpose Physiologically-based pharmacokinetic (PBPK) models are essential in drug development, but require parameters that are not always obtainab...
PMC9539103
core_pubmed_pmc
Pharmacokinetics of butorphanol following intravenous and intramuscular administration in donkeys: A preliminary study
Pharmacokinetics of butorphanol following intravenous and intramuscular administration in donkeys: A preliminary study Abstract Abstract The pharmacokinetics of butorphanol after intravenous (IVB) and intramuscular (IMB) administration in donkeys were determined in this preliminary study. Healthy male gelded donkeys ( ...
PMC3157216
core_pubmed_pmc
Feasibility of Imaging Myelin Lesions in Multiple Sclerosis
Feasibility of Imaging Myelin Lesions in Multiple Sclerosis Abstract The goal of this study was to provide a feasibility assessment for PET imaging of multiple sclerosis (MS) lesions based on their decreased myelin content relative to the surrounding normal-appearing brain tissue. The imaging agent evaluated for this p...
PMC11144913
core_pubmed_pmc
Better together: nanoscale co-delivery systems of therapeutic agents for high-performance cancer therapy
Better together: nanoscale co-delivery systems of therapeutic agents for high-performance cancer therapy Abstract Combination therapies can enhance the sensitivity of cancer to drugs, lower drug doses, and reduce side effects in cancer treatment. However, differences in the physicochemical properties and pharmacokineti...
PMC3409044
core_pubmed_pmc
Multiple concurrent collagenase clostridium histolyticum injections to dupuytren’s cords: an exploratory study
Multiple concurrent collagenase clostridium histolyticum injections to dupuytren’s cords: an exploratory study Abstract Abstract Background Dupuytren’s contracture (DC) is a progressive fibroproliferative disorder characterized by development of nodules and collagen cords within the palmar fascia of the hand. Collagena...
PMC3889701
core_pubmed_pmc
Clinical Pharmacokinetic and Pharmacodynamic Profile of Rivaroxaban
Clinical Pharmacokinetic and Pharmacodynamic Profile of Rivaroxaban Abstract Rivaroxaban is an oral, direct Factor Xa inhibitor that targets free and clot-bound Factor Xa and Factor Xa in the prothrombinase complex. It is absorbed rapidly, with maximum plasma concentrations being reached 2–4 h after tablet intake. Oral...
PMC3828005
core_pubmed_pmc
Basic Concepts in Physiologically Based Pharmacokinetic Modeling in Drug Discovery and Development
Basic Concepts in Physiologically Based Pharmacokinetic Modeling in Drug Discovery and Development Modeling Different PK Model Types: Classical Vs. PBPK Models Mathematical models are frequently used to help understand the PK of drugs following intravenous (i.v.) and oral dosing in animals and humans. Models describing...
PMC7707836
core_pubmed_pmc
Challenges in the management of chronic hypoparathyroidism
Challenges in the management of chronic hypoparathyroidism Abstract Abstract The first adjunctive hormone therapy for chronic hypoparathyroidism, recombinant human parathyroid hormone (1–84) (rhPTH(1–84)) was approved by the FDA in January 2015. Since the approval of rhPTH(1–84), growing interest has developed in other...
PMC8479189
core_pubmed_pmc
Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer
Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer Abstract Background Zimberelimab (GLS-010) is a novel fully human monoclonal immunoglobulin G4 (IgG4) against the programmed cell death-1 (PD-1) receptor. Aim To evaluate the affinity, compet...
PMC11567709
core_pubmed_pmc
Patiromer Does Not Alter Tacrolimus Pharmacokinetics in Kidney Transplant Recipients When Administered Three Hours Post–Tacrolimus
Patiromer Does Not Alter Tacrolimus Pharmacokinetics in Kidney Transplant Recipients When Administered Three Hours Post–Tacrolimus Abstract Background. Hyperkalemia is common in kidney transplant (KTx) recipients. Patiromer, a potassium-binding polymer used to treat acute and chronic hyperkalemia, has the potential to ...
PMC11620509
core_pubmed_pmc
How to use meropenem in pediatric patients undergoing CKRT? Integrated meropenem pharmacokinetic model for critically ill children
How to use meropenem in pediatric patients undergoing CKRT? Integrated meropenem pharmacokinetic model for critically ill children Abstract ABSTRACT Standard dosing could fail to achieve adequate systemic concentrations in ICU children or may lead to toxicity in children with acute kidney injury. The population pharmac...
PMC12501462
core_pubmed_pmc
Abelacimab for Acute Pulmonary Embolism: Translating Dual FXI/XIa Inhibition from Mechanism to Clinical Prospects
Abelacimab for Acute Pulmonary Embolism: Translating Dual FXI/XIa Inhibition from Mechanism to Clinical Prospects Abstract Abstract Acute pulmonary embolism (PE) remains a life-threatening condition. A critical therapeutic dilemma exists for a significant proportion of patients at high bleeding risk(approximately 30%-5...
PMC4858031
core_pubmed_pmc
Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing
Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing Abstract Background Levetiracetam is an anticonvulsant used for control of canine epilepsy. An extended release preparation should improve dosing convenience. Objectives To determine the disposition of extended release levetir...
PMC8476547
core_pubmed_pmc
Epigenetic derepression converts PPARγ into a druggable target in triple-negative and endocrine-resistant breast cancers
Epigenetic derepression converts PPARγ into a druggable target in triple-negative and endocrine-resistant breast cancers Abstract Clinical trials repurposing peroxisome proliferator-activated receptor-gamma (PPARγ) agonists as anticancer agents have exhibited lackluster efficacy across a variety of tumor types. Here, w...
PMC12358302
core_pubmed_pmc
Prognostic Value of a Joint K‐PD Model With Tumor Size Dynamics and CA‐125 Kinetics in Recurrent Ovarian Cancer Patients: BOLD Phase II GINECO Study
Prognostic Value of a Joint K‐PD Model With Tumor Size Dynamics and CA‐125 Kinetics in Recurrent Ovarian Cancer Patients: BOLD Phase II GINECO Study Abstract ABSTRACT In patients with recurrent advanced ovarian cancer, there is a need for companion tests to guide the development of innovative chemotherapy‐free treatmen...