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PMC7899927
core_pubmed_pmc
Pharmacokinetics of buprenorphine in pregnant sheep after intravenous injection
Pharmacokinetics of buprenorphine in pregnant sheep after intravenous injection Abstract Abstract Buprenorphine is a semi‐synthetic opioid, widely used in the maintenance treatment for opioid‐dependent pregnant women. Limited data exist on the pharmacokinetics of buprenorphine in pregnancy. We conducted a pharmacokinet...
PMC9762503
core_pubmed_pmc
Validation of a simplified-geometry model of inhaled formoterol pharmacodynamics in asthmatic patients
Validation of a simplified-geometry model of inhaled formoterol pharmacodynamics in asthmatic patients Abstract PharmacoKinetics (PK) and PharmacoDynamics (PD) mathematical models of inhaled bronchodilators represent useful tools for understanding the mechanisms of drug action and for the individuation of therapy regim...
PMC11638344
core_pubmed_pmc
Effect of SLC22A1 polymorphism on the pharmacokinetics of proguanil in Korean: A semi‐physiologic population pharmacokinetic approach
Effect of SLC22A1 polymorphism on the pharmacokinetics of proguanil in Korean: A semi‐physiologic population pharmacokinetic approach Abstract Abstract Proguanil, an antimalarial drug, undergoes hepatic uptake by the polymorphic organic cation transporter 1 (OCT1) and is subsequently metabolized by the cytochrome P‐450...
PMC8668201
core_pubmed_pmc
Average IGF-1 Prediction for Once-Weekly Lonapegsomatropin in Children With Growth Hormone Deficiency
Average IGF-1 Prediction for Once-Weekly Lonapegsomatropin in Children With Growth Hormone Deficiency Abstract Abstract Context Serum insulin-like growth factor 1 (IGF-1) levels are relatively constant in somatropin-treated children with growth hormone deficiency (GHD), and guide dose adjustments for clinical efficacy ...
PMC8874959
core_pubmed_pmc
Unlike Chloroquine, Mefloquine Inhibits SARS-CoV-2 Infection in Physiologically Relevant Cells
Unlike Chloroquine, Mefloquine Inhibits SARS-CoV-2 Infection in Physiologically Relevant Cells Abstract Despite the development of specific therapies against severe acute respiratory coronavirus 2 (SARS-CoV-2), the continuous investigation of the mechanism of action of clinically approved drugs could provide new inform...
PMC7049282
core_pubmed_pmc
Peripheral Opioid Receptor Antagonists for Opioid-Induced Constipation: A Primer on Pharmacokinetic Variabilities with a Focus on Drug Interactions
Peripheral Opioid Receptor Antagonists for Opioid-Induced Constipation: A Primer on Pharmacokinetic Variabilities with a Focus on Drug Interactions Abstract Abstract Opioid analgesics remain a treatment option for refractory acute and chronic pain, despite their potential risk for abuse and adverse events (AEs). Opioid...
PMC4838684
core_pubmed_pmc
Multicentre open-label randomised controlled trial to compare colistin alone with colistin plus meropenem for the treatment of severe infections caused by carbapenem-resistant Gram-negative infections (AIDA): a study protocol
Multicentre open-label randomised controlled trial to compare colistin alone with colistin plus meropenem for the treatment of severe infections caused by carbapenem-resistant Gram-negative infections (AIDA): a study protocol Abstract Abstract Introduction The emergence of antibiotic-resistant bacteria has driven renew...
PMC6477053
core_pubmed_pmc
Treatment of Infections Due to MDR Gram-Negative Bacteria
Treatment of Infections Due to MDR Gram-Negative Bacteria Abstract Abstract The treatment of multidrug-resistant Gram-negative bacteria (MDR-GNB) infections in critically ill patients presents many challenges. Since an effective treatment should be administered as soon as possible, resistance to many antimicrobial clas...
PMC8363684
core_pubmed_pmc
Safety and Pharmacokinetics of HTL0018318, a Novel M 1 Receptor Agonist, Given in Combination with Donepezil at Steady State: A Randomized Trial in Healthy Elderly Subjects
Safety and Pharmacokinetics of HTL0018318, a Novel M 1 Receptor Agonist, Given in Combination with Donepezil at Steady State: A Randomized Trial in Healthy Elderly Subjects Abstract Introduction HTL0018318 is a selective muscarinic M 1 receptor partial agonist under development for the symptomatic treatment of dementia...
PMC8879427
core_pubmed_pmc
Phytochemical and In Silico ADME/Tox Analysis of Eruca sativa Extract with Antioxidant, Antibacterial and Anticancer Potential against Caco-2 and HCT-116 Colorectal Carcinoma Cell Lines
Phytochemical and In Silico ADME/Tox Analysis of Eruca sativa Extract with Antioxidant, Antibacterial and Anticancer Potential against Caco-2 and HCT-116 Colorectal Carcinoma Cell Lines Abstract Abstract Eruca sativa Mill. ( E. sativa ) leaves recently grabbed the attention of scientific communities around the world du...
PMC8079654
core_pubmed_pmc
Natalizumab Pharmacokinetics and -Dynamics and Serum Neurofilament in Patients With Multiple Sclerosis
Natalizumab Pharmacokinetics and -Dynamics and Serum Neurofilament in Patients With Multiple Sclerosis Abstract Abstract Background: Natalizumab (NAT) is a high-efficacy treatment for relapsing remitting multiple sclerosis (RRMS). However, it is associated with an increased risk of progressive multifocal leukoencephalo...
PMC4055585
core_pubmed_pmc
Pharmacokinetics of Anti-HBV Polyoxometalate in Rats
Pharmacokinetics of Anti-HBV Polyoxometalate in Rats Abstract Polyoxometalates are non-nucleoside analogs that have been proven to exhibit broad-spectrum antiviral activity. In particular, Cs 2 K 4 Na[SiW 9 Nb 3 O 40 ].H 2 O 1 shows low toxicity and high activity against HBV. The preclinical pharmacokinetics of Compoun...
PMC5412848
core_pubmed_pmc
Cefiderocol, a Siderophore Cephalosporin for Gram‐Negative Bacterial Infections: Pharmacokinetics and Safety in Subjects With Renal Impairment
Cefiderocol, a Siderophore Cephalosporin for Gram‐Negative Bacterial Infections: Pharmacokinetics and Safety in Subjects With Renal Impairment Abstract Abstract Cefiderocol, a new injectable siderophore cephalosporin antibiotic, has promising in vitro and in vivo activity against Gram‐negative bacteria including multid...
PMC4356686
core_pubmed_pmc
Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation Abstract Abstract Background The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticul...
PMC11455733
core_pubmed_pmc
Preclinical and Toxicology Assessment of ALW-II-41-27, an Inhibitor of the Eph Receptor A2 (EphA2)
Preclinical and Toxicology Assessment of ALW-II-41-27, an Inhibitor of the Eph Receptor A2 (EphA2) Abstract Abstract Background and Objective The EphA2 receptor inhibitor ALW-II-41-27 has proven to be an effective in vitro antagonist of Pneumocystis β-glucan-induced proinflammatory signaling. This suggests its potentia...
PMC6442103
core_pubmed_pmc
Single dose oral ranolazine pharmacokinetics in patients receiving maintenance hemodialysis
Single dose oral ranolazine pharmacokinetics in patients receiving maintenance hemodialysis Abstract Abstract Purpose: Ranolazine is a novel anti-angina treatment approved in the United States for chronic stable angina. Ranolazine pharmacokinetics have not been studied previously in patients who receive maintenance hem...
PMC12347919
core_pubmed_pmc
Mephedrone and Its Metabolites: A Narrative Review
Mephedrone and Its Metabolites: A Narrative Review Abstract New psychoactive substances (NPSs) have emerged as a significant global public health challenge due to their ability to mimic traditional drugs. Among these, mephedrone has gained attention because of its widespread use and associated toxicities. This review p...
PMC11052795
core_pubmed_pmc
Pharmacological Basis of Differences in Dose Response, Dose Equivalence, and Duration of Action of Inhaled Corticosteroids
Pharmacological Basis of Differences in Dose Response, Dose Equivalence, and Duration of Action of Inhaled Corticosteroids Abstract Introduction Asthma treatment guidelines classify inhaled corticosteroid (ICS) regimens as low, medium, or high dose. However, efficacy and safety are not independently assessed accordingl...
PMC11260750
core_pubmed_pmc
The potential therapeutic value of the natural plant compounds matrine and oxymatrine in cardiovascular diseases
The potential therapeutic value of the natural plant compounds matrine and oxymatrine in cardiovascular diseases Abstract Abstract Matrine (MT) and Oxymatrine (OMT) are two natural alkaloids derived from plants. These bioactive compounds are notable for their diverse pharmacological effects and have been extensively st...
PMC5927802
core_pubmed_pmc
Pharmacokinetics, safety, and tolerability of the 2‐ and 3‐direct‐acting antiviral combination of AL‐335, odalasvir, and simeprevir in healthy subjects
Pharmacokinetics, safety, and tolerability of the 2‐ and 3‐direct‐acting antiviral combination of AL‐335, odalasvir, and simeprevir in healthy subjects Abstract Abstract This Phase I, open‐label, two‐group, fixed‐sequence study evaluated the pharmacokinetics and safety of AL‐335, odalasvir, and simeprevir in healthy su...
PMC12887773
core_pubmed_pmc
Safety and pharmacokinetics of sulfasalazine and its metabolite sulfapyridine for treatment of preterm preeclampsia in Australia (SIP): an early phase, unblinded, single-arm, proof of concept clinical trial
Safety and pharmacokinetics of sulfasalazine and its metabolite sulfapyridine for treatment of preterm preeclampsia in Australia (SIP): an early phase, unblinded, single-arm, proof of concept clinical trial Abstract Summary Background Preeclampsia is a hypertensive pregnancy disorder marked by systemic inflammation and...
PMC10391520
core_pubmed_pmc
Intravenous Magnesium: Prompt Use for Asthma in Children Treated in the Emergency Department (IMPACT-ED): Protocol for a Multicenter Pilot Randomized Controlled Trial
Intravenous Magnesium: Prompt Use for Asthma in Children Treated in the Emergency Department (IMPACT-ED): Protocol for a Multicenter Pilot Randomized Controlled Trial Abstract Background Children managed for asthma in an emergency department (ED) may be less likely to be hospitalized if they receive intravenous magnesi...
PMC10503830
core_pubmed_pmc
Tumor Response to Stroma-Modifying Therapy: Magnetic Resonance Imaging Findings in Early-Phase Clinical Trials of Pegvorhyaluronidase alpha (PEGPH20)
Tumor Response to Stroma-Modifying Therapy: Magnetic Resonance Imaging Findings in Early-Phase Clinical Trials of Pegvorhyaluronidase alpha (PEGPH20) Abstract Pre-clinical and clinical studies have shown that PEGPH20 depletes intratumoral hyaluronic acid (HA), which is linked to high interstitial fluid pressures and po...
PMC11494920
core_pubmed_pmc
A mechanistic PK/PD model of AZD0171 (anti‐LIF) to support Phase II dose selection
A mechanistic PK/PD model of AZD0171 (anti‐LIF) to support Phase II dose selection Abstract Abstract AZD0171 (INN: Falbikitug) is being developed as a humanized monoclonal antibody (mAb), immunoglobulin G subclass 1 (IgG1), which binds specifically to the immunosuppressive human cytokine leukemia inhibitory factor (LIF...
PMC11266035
core_pubmed_pmc
Pharmacokinetic study of Q808 in rhesus monkey using liquid chromatography–tandem mass spectrometry
Pharmacokinetic study of Q808 in rhesus monkey using liquid chromatography–tandem mass spectrometry Abstract Abstract Background Q808 is a novel antiepileptic agent currently in development. In this study, we established and validated a LC-MS/MS method for the quantification of Q808 in Rhesus monkey plasma. Furthermore...
PMC4676620
core_pubmed_pmc
Impact of volume expansion on the efficacy and pharmacokinetics of liposome bupivacaine
Impact of volume expansion on the efficacy and pharmacokinetics of liposome bupivacaine Abstract Abstract Liposome bupivacaine is a prolonged-release liposomal formulation of bupivacaine indicated for single-dose infiltration into the surgical site to produce postsurgical analgesia of longer duration than traditional l...
PMC7835195
core_pubmed_pmc
68 Ga-labelled desferrioxamine-B for bacterial infection imaging
68 Ga-labelled desferrioxamine-B for bacterial infection imaging Abstract Purpose With the increase of especially hospital-acquired infections, timely and accurate diagnosis of bacterial infections is crucial for effective patient care. Molecular imaging has the potential for specific and sensitive detection of infecti...
PMC12865225
core_pubmed_pmc
Dicloxacillin and Flucloxacillin Inhibit Hepatic Uptake Transporters—In Vitro Investigations and Physiologically Based Pharmacokinetic Modeling
Dicloxacillin and Flucloxacillin Inhibit Hepatic Uptake Transporters—In Vitro Investigations and Physiologically Based Pharmacokinetic Modeling Abstract ABSTRACT Dicloxacillin and flucloxacillin are β‐lactamase‐resistant penicillin antibiotics that have been in clinical use for over 50 years. While both antibiotics are...
PMC8406631
core_pubmed_pmc
A Retinoid X Receptor Agonist Directed to the Large Intestine Ameliorates T-Cell-Mediated Colitis in Mice
A Retinoid X Receptor Agonist Directed to the Large Intestine Ameliorates T-Cell-Mediated Colitis in Mice Abstract Retinoid X receptor (RXR) is a nuclear receptor that heterodimerizes with several nuclear receptors, integrating ligand-mediated signals across the heterodimers. Synthetic RXR agonists have been developed ...
PMC5568018
core_pubmed_pmc
Pharmacokinetics and Safety of Vortioxetine in Pediatric Patients
Pharmacokinetics and Safety of Vortioxetine in Pediatric Patients Abstract Abstract Objective: The primary objectives of this study were to evaluate the pharmacokinetics (PK) and tolerability of single and multiple doses of vortioxetine in children and adolescents with a depressive or anxiety disorder and to provide su...
PMC7662502
core_pubmed_pmc
Pharmaceutical Excipients and Drug Metabolism: A Mini-Review
Pharmaceutical Excipients and Drug Metabolism: A Mini-Review Abstract Conclusions from previously reported articles have revealed that many commonly used pharmaceutical excipients, known to be pharmacologically inert, show effects on drug transporters and/or metabolic enzymes. Thus, the pharmacokinetics (absorption, di...
PMC10681545
core_pubmed_pmc
Mechanistically modeling peripheral cytokine dynamics following bispecific dosing in solid tumors
Mechanistically modeling peripheral cytokine dynamics following bispecific dosing in solid tumors Abstract Abstract Bispecific antibodies exhibit proven clinical benefit, and many bispecifics are currently in clinical development for oncology. Cytokine release syndrome (CRS) is a common clinical adverse effect observed...
PMC7821183
core_pubmed_pmc
Increased Induction Infliximab Clearance Predicts Early Antidrug Antibody Detection
Increased Induction Infliximab Clearance Predicts Early Antidrug Antibody Detection Abstract Abstract Treatment of patients with biologics such as infliximab may trigger development of antidrug antibodies, which are associated with faster drug clearance, reduced treatment efficacy, and increased risk of infusion‐relate...
PMC12238500
core_pubmed_pmc
The effects of high-altitude hypoxic environment on the pharmacokinetics and respiratory function of remimazolam: an experimental study in rats
The effects of high-altitude hypoxic environment on the pharmacokinetics and respiratory function of remimazolam: an experimental study in rats Abstract This study investigated the impact of high-altitude hypoxic environment on the pharmacokinetics and respiratory effects of remimazolam in a rat model. Forty Sprague-Da...
PMC7340670
core_pubmed_pmc
Phase I study of TAS-115, a novel oral multi-kinase inhibitor, in patients with advanced solid tumors
Phase I study of TAS-115, a novel oral multi-kinase inhibitor, in patients with advanced solid tumors Abstract Summary TAS-115 is a novel MET, VEGFR, FMS and PDGFR inhibitor, developed to improve the continuity of drug administration with a relatively short half-life. We assessed its tolerability, safety, pharmacokinet...
PMC3185947
core_pubmed_pmc
Erlotinib ‘dosing-to-rash’: a phase II intrapatient dose escalation and pharmacologic study of erlotinib in previously treated advanced non-small cell lung cancer
Erlotinib ‘dosing-to-rash’: a phase II intrapatient dose escalation and pharmacologic study of erlotinib in previously treated advanced non-small cell lung cancer Abstract Background: To evaluate the anticancer activity of erlotinib in patients with previously treated, advanced non-small cell lung cancer (NSCLC) whose ...
PMC6754336
core_pubmed_pmc
Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine
Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine Abstract Abstract Introduction: Cariprazine, a dopamine D 3 -preferring D 3 /D 2 receptor partial agonist and serotonin 5-HT 1A receptor partial agonist, has two major human metabolites, desmethyl-cariprazine (DCAR)...
PMC7463902
core_pubmed_pmc
Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation
Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation Abstract Abstract The aim of this study was to control the dissolution rate and permeability of cilostazol. To enhance the dissolution rate of the active pharmaceutical ingredient (API), hot-melt extrusion (HME...
PMC10256642
core_pubmed_pmc
Pharmacokinetics and Safety of Cotadutide, a GLP-1 and Glucagon Receptor Dual Agonist, in Individuals with Renal Impairment: A Single-Dose, Phase I, Bridging Study
Pharmacokinetics and Safety of Cotadutide, a GLP-1 and Glucagon Receptor Dual Agonist, in Individuals with Renal Impairment: A Single-Dose, Phase I, Bridging Study Abstract Background and Objective Cotadutide is a balanced glucagon-like peptide-1 and glucagon receptor dual agonist under development for the treatment of...
PMC5663168
core_pubmed_pmc
Food significantly reduces plasma concentrations of first-line anti-tuberculosis drugs
Food significantly reduces plasma concentrations of first-line anti-tuberculosis drugs Abstract Abstract Background & objectives: Concomitant feeding and anti-tuberculosis (TB) drug administration are likely to reduce nausea and enhance compliance to treatment. However, food could lower plasma drug concentrations. This...
PMC12338885
core_pubmed_pmc
Pharmacokinetics of dexamethasone in tuberculosis meningitis
Pharmacokinetics of dexamethasone in tuberculosis meningitis Abstract Introduction Dexamethasone is recommended as adjunctive therapy for tuberculosis meningitis (TBM). Co-administration with rifampicin is expected to reduce dexamethasone exposure in TBM, an effect that may be more pronounced with the higher rifampicin...
PMC8131695
core_pubmed_pmc
Pharmacokinetics of anti-infective agents during CytoSorb hemoadsorption
Pharmacokinetics of anti-infective agents during CytoSorb hemoadsorption Abstract Abstract Cytokine hemoadsorption might be beneficial in patients with sepsis. However, its effect on anti-infective agents' disposition remains largely unknown. We sought to determine the influence of hemoadsorption on the pharmacokinetic...
PMC11184600
core_pubmed_pmc
Systematic Quantitative Analysis of Fetal Dexamethasone Exposure and Fetal Lung Maturation in Pregnant Animals: Model Informed Dexamethasone Precision Dose Study
Systematic Quantitative Analysis of Fetal Dexamethasone Exposure and Fetal Lung Maturation in Pregnant Animals: Model Informed Dexamethasone Precision Dose Study Abstract Abstract Dexamethasone (DEX) was applied in neonatal respiratory distress syndrome treatment of pregnant women. We established a pharmacokinetics (PK...
PMC4062834
core_pubmed_pmc
Prediction of Clinical Irrelevance of PK Differences in Atorvastatin Using PK/PD Models Derived From Literature-Based Meta-Analyses
Prediction of Clinical Irrelevance of PK Differences in Atorvastatin Using PK/PD Models Derived From Literature-Based Meta-Analyses Abstract Abstract To support the development of a fixed-dose combination (FDC) of ezetimibe and atorvastatin for the treatment of dyslipidemia, bioequivalence (BE) studies were conducted a...
PMC7695871
core_pubmed_pmc
Chitosan-Coated Hydroxypropylmethyl Cellulose Microparticles of Levodopa (and Carbidopa): In Vitro and Rat Model Kinetic Characteristics
Chitosan-Coated Hydroxypropylmethyl Cellulose Microparticles of Levodopa (and Carbidopa): In Vitro and Rat Model Kinetic Characteristics Abstract Background Parkinson's disease is a neurodegenerative disorder, and a major cause of disability. Levodopa, a prodrug of dopamine, remains the gold standard in the pharmacolog...
PMC4235724
core_pubmed_pmc
Can We Prevent Antimicrobial Resistance by Using Antimicrobials Better?
Can We Prevent Antimicrobial Resistance by Using Antimicrobials Better? Abstract Abstract Since their development over 60 years ago, antimicrobials have become an integral part of healthcare practice worldwide. Recently, this has been put in jeopardy by the emergence of widespread antimicrobial resistance, which is one...
PMC7028795
core_pubmed_pmc
Safety, Pharmacokinetics, and Clinical Activity of Adavosertib in Combination with Chemotherapy in Asian Patients with Advanced Solid Tumors: Phase Ib Study
Safety, Pharmacokinetics, and Clinical Activity of Adavosertib in Combination with Chemotherapy in Asian Patients with Advanced Solid Tumors: Phase Ib Study Abstract Abstract Background The WEE1 inhibitor adavosertib (AZD1775) has been investigated in Western patients. Objective This open-label Phase Ib study ( NCT0234...
PMC12567882
core_pubmed_pmc
Anticancer Activity of Snake Venom Against Breast Cancer: A Scoping Review
Anticancer Activity of Snake Venom Against Breast Cancer: A Scoping Review Abstract Abstract Breast cancer remains a leading cause of cancer-related mortality worldwide, necessitating innovative therapeutic approaches. This scoping review summarizes experimental evidence on the anticancer activity of snake venom and it...
PMC8102622
core_pubmed_pmc
Ibudilast (MN-166) in amyotrophic lateral sclerosis- an open label, safety and pharmacodynamic trial
Ibudilast (MN-166) in amyotrophic lateral sclerosis- an open label, safety and pharmacodynamic trial Abstract Highlights • No significant reduction in brain glial activation measured by PBR28-PET SUVR. • No significant reduction in serum neurofilament light levels over 36–40 weeks. • Adverse event related dose reductio...
PMC8940812
core_pubmed_pmc
Population pharmacokinetic model selection assisted by machine learning
Population pharmacokinetic model selection assisted by machine learning Abstract A fit-for-purpose structural and statistical model is the first major requirement in population pharmacometric model development. In this manuscript we discuss how this complex and computationally intensive task could benefit from supervis...
PMC8108689
core_pubmed_pmc
Delivering clinical trials at home: protocol, design and implementation of a direct-to-family paediatric lupus trial
Delivering clinical trials at home: protocol, design and implementation of a direct-to-family paediatric lupus trial Abstract Abstract Introduction Direct-to-family clinical trials efficiently provide data while reducing the participation burden for children and their families. Although these trials can offer significa...
PMC4015666
core_pubmed_pmc
Identification and comparison of insulin pharmacokinetics injected with a new 4‐mm needle vs 6‐ and 8‐mm needles accounting for endogenous insulin and C‐peptide secretion kinetics in non‐diabetic adult males
Identification and comparison of insulin pharmacokinetics injected with a new 4‐mm needle vs 6‐ and 8‐mm needles accounting for endogenous insulin and C‐peptide secretion kinetics in non‐diabetic adult males Abstract Abstract Aims/Introduction Many patients with diabetes now use 5‐, 6‐ or 8‐mm needles for insulin injec...
PMC5427923
core_pubmed_pmc
A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy
A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy Abstract CC Chemokine Receptor 2 (CCR2) and its endogenous ligand CCL2 are involved in a number of diseases, including atherosclerosis. Several CCR2 antagonists have been developed as potential therapeutic agents,...
PMC11330181
core_pubmed_pmc
Tipifarnib physiologically‐based pharmacokinetic modeling to assess drug–drug interaction, organ impairment, and biopharmaceutics in healthy subjects and cancer patients
Tipifarnib physiologically‐based pharmacokinetic modeling to assess drug–drug interaction, organ impairment, and biopharmaceutics in healthy subjects and cancer patients Abstract Abstract A physiologically‐based pharmacokinetic (PBPK) model for tipifarnib, which included mechanistic absorption, was built and verified b...
PMC6431676
core_pubmed_pmc
Pharmacokinetic and Pharmacogenetic Factors Contributing to Platelet Function Recovery After Single Dose of Ticagrelor in Healthy Subjects
Pharmacokinetic and Pharmacogenetic Factors Contributing to Platelet Function Recovery After Single Dose of Ticagrelor in Healthy Subjects Abstract Abstract Objectives: This study aimed to elucidate the contribution of candidate single nucleotide polymorphisms (SNPs) related to pharmacokinetics on the recovery of plate...
PMC12586038
core_pubmed_pmc
The efficacy, safety, and pharmacokinetics/pharmacodynamics of telitacicept following efgartigimod in generalized myasthenia gravis: protocol of a randomized controlled trial
The efficacy, safety, and pharmacokinetics/pharmacodynamics of telitacicept following efgartigimod in generalized myasthenia gravis: protocol of a randomized controlled trial Abstract Introduction Several biologic agents have emerged as novel therapeutic options for patients with generalized myasthenia gravis (gMG); ho...
PMC10136204
core_pubmed_pmc
Low-Dose Immunotherapy: Is It Just an Illusion?
Low-Dose Immunotherapy: Is It Just an Illusion? Abstract Abstract The development and use of immunotherapy in the last decade have led to a drastic improvement in results in the onco-haematological field. This has implied, on the one hand, the need for clinicians to manage a new type of adverse event and, on the other ...
PMC4452638
core_pubmed_pmc
Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer
Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer Abstract Abstract Background Due to its high expression in prostate cancer, PSMA (prostate-specific membrane antigen) represents an ideal target for both diagnostic imaging and endoradio...
PMC9326882
core_pubmed_pmc
Association of antioxidant nutraceuticals and acetaminophen (paracetamol): Friend or foe?
Association of antioxidant nutraceuticals and acetaminophen (paracetamol): Friend or foe? Abstract Abstract Acetaminophen (paracetamol or APAP) is an analgesic and antipyretic drug that can induce oxidative stress-mediated hepatotoxicity at high doses. Several studies reported that antioxidant nutraceuticals, in partic...
PMC10974834
core_pubmed_pmc
Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention
Preclinical and Early Clinical Development of Tenofovir Alafenamide/Elvitegravir Topical Inserts for Effective On-Demand Vaginal and Rectal HIV Prevention Abstract HIV/AIDS remains a global public health issue, and products available for the prevention of HIV infections are limited, especially those for short-acting, o...
PMC3968084
core_pubmed_pmc
Rivaroxaban as an oral anticoagulant for stroke prevention in atrial fibrillation
Rivaroxaban as an oral anticoagulant for stroke prevention in atrial fibrillation Abstract Atrial fibrillation (AF) is the most common cardiac arrhythmia in the developed world and is associated with a fivefold increase in the risk of stroke, accounting for up to 15% of strokes in the general population. The European S...
PMC6699558
core_pubmed_pmc
Pharmacokinetic data on high dose baclofen administration in unhealthy alcohol user in the ICU
Pharmacokinetic data on high dose baclofen administration in unhealthy alcohol user in the ICU Abstract In the intensive care unit, alcohol intake above the NIAAA recommendations regardless of the existence of an Alcohol Use Disorder (AUD), was associated with an increased risk of death and longer time on ventilator. T...
PMC9486669
core_pubmed_pmc
Pharmacological characterization of geraniol in sheep and its potential use in the control of gastrointestinal nematodes
Pharmacological characterization of geraniol in sheep and its potential use in the control of gastrointestinal nematodes Abstract Highlights • Geraniol is a monoterpene which showed in vitro antiparasitic effect. • The oxidative metabolism of albendazole is reduced by geraniol in vitro. • There were not in vivo pharmac...
PMC4491360
core_pubmed_pmc
Phase I study of ipilimumab in phased combination with paclitaxel and carboplatin in Japanese patients with non-small-cell lung cancer
Phase I study of ipilimumab in phased combination with paclitaxel and carboplatin in Japanese patients with non-small-cell lung cancer Abstract Summary Background Ipilimumab is an antibody that targets the cytotoxic T-lymphocyte antigen-4 to potentiate an antitumor response. Adding ipilimumab 10 mg/kg to paclitaxel (PT...
PMC8128801
core_pubmed_pmc
Coadministration of tizanidine and ciprofloxacin: a retrospective analysis of the WHO pharmacovigilance database
Coadministration of tizanidine and ciprofloxacin: a retrospective analysis of the WHO pharmacovigilance database Abstract Purpose Tizanidine, an alpha-adrenergic substance with antinociceptive and antihypertensive effects, is extensively metabolized via cytochrome P450 (CYP) 1A2. Therefore, coadministration with potent...
PMC8641324
core_pubmed_pmc
Results of a Double-Blind, Randomized, Placebo-Controlled Phase 1 Study to Evaluate the Safety and Pharmacokinetics of Anti-Zika Virus Immunoglobulin
Results of a Double-Blind, Randomized, Placebo-Controlled Phase 1 Study to Evaluate the Safety and Pharmacokinetics of Anti-Zika Virus Immunoglobulin Abstract ABSTRACT. Zika virus (ZIKV) is transmitted primarily through infected Aedes aegypti or Aedes albopictus mosquitoes. ZIKV infection during pregnancy was linked to...
PMC8146490
core_pubmed_pmc
HIV-1 Tat and Morphine Differentially Disrupt Pyramidal Cell Structure and Function and Spatial Learning in Hippocampal Area CA1: Continuous versus Interrupted Morphine Exposure
HIV-1 Tat and Morphine Differentially Disrupt Pyramidal Cell Structure and Function and Spatial Learning in Hippocampal Area CA1: Continuous versus Interrupted Morphine Exposure Abstract Abstract About half the people infected with human immunodeficiency virus (HIV) have neurocognitive deficits that often include memor...
PMC12276727
core_pubmed_pmc
Elranatamab for Relapsed/Refractory Multiple Myeloma With Severe Renal Impairment Requiring Hemodialysis
Elranatamab for Relapsed/Refractory Multiple Myeloma With Severe Renal Impairment Requiring Hemodialysis Abstract ABSTRACT Relapsed/refractory multiple myeloma (RRMM) patients with dialysis‐dependent renal impairment face limited therapeutic options due to exclusion from clinical trials, a lack of evidence‐based guidel...
PMC8994040
core_pubmed_pmc
Therapeutic Drug Monitoring of Antimicrobial Drugs in Neonates: An Opinion Article
Therapeutic Drug Monitoring of Antimicrobial Drugs in Neonates: An Opinion Article Abstract Background: Neonatal infections are associated with high morbidity and mortality rates. Optimal treatment of these infections requires knowledge of neonatal pharmacology and integration of neonatal developmental pharmacokinetics...
PMC11504488
core_pubmed_pmc
Linezolid Pharmacokinetics in Critically Ill Patients: Continuous Versus Intermittent Infusion
Linezolid Pharmacokinetics in Critically Ill Patients: Continuous Versus Intermittent Infusion Abstract Abstract Background: Linezolid has been found to have considerable interindividual variability, especially in critically ill patients, which can lead to suboptimal plasma concentration. To overcome this shortcoming, ...
PMC10809906
core_pubmed_pmc
A low-volume LC/MS method for highly sensitive monitoring of phenoxymethylpenicillin, benzylpenicillin, and probenecid in human serum †
A low-volume LC/MS method for highly sensitive monitoring of phenoxymethylpenicillin, benzylpenicillin, and probenecid in human serum † Abstract Abstract Background : The optimization of antimicrobial dosing plays a crucial role in improving the likelihood of achieving therapeutic success while reducing the risks assoc...
PMC5620572
core_pubmed_pmc
Development and Evaluation of Topical Gabapentin Formulations
Development and Evaluation of Topical Gabapentin Formulations Abstract Abstract Topical delivery of gabapentin is desirable to treat peripheral neuropathic pain conditions whilst avoiding systemic side effects. To date, reports of topical gabapentin delivery in vitro have been variable and dependent on the skin model e...
PMC11253127
core_pubmed_pmc
NfL concentration in CSF is a quantitative marker of the rate of neurodegeneration in aging and Huntington's disease: a semi-mechanistic model-based analysis
NfL concentration in CSF is a quantitative marker of the rate of neurodegeneration in aging and Huntington's disease: a semi-mechanistic model-based analysis Abstract Abstract The concentrations of neurofilament light chain (NfL) in cerebrospinal fluid (CSF) and plasma have become key biomarkers of many neurodegenerati...
PMC9483500
core_pubmed_pmc
Impact of model misspecification on model-based tests in PK studies with parallel design: real case and simulation studies
Impact of model misspecification on model-based tests in PK studies with parallel design: real case and simulation studies Abstract Abstract This article evaluates the performance of pharmacokinetic (PK) equivalence testing between two formulations of a drug through the Two-One Sided Tests (TOST) by a model-based appro...
PMC3432029
core_pubmed_pmc
Pharmacokinetics of Peptide Mediated Delivery of Anticancer Drug Ellipticine
Pharmacokinetics of Peptide Mediated Delivery of Anticancer Drug Ellipticine Abstract The amino acid pairing peptide EAK16-II (EAK) has shown the ability to stabilize the hydrophobic anticancer agent ellipticine (EPT) in aqueous solution. In this study, we investigate pharmacokinetics of the formulation of EAK-EPT comp...
PMC8918743
core_pubmed_pmc
Therapeutic drug monitoring of vancomycin in neurosurgery patients, from trough concentration to area under the curve: a retrospective single center cohort study in a tertiary hospital
Therapeutic drug monitoring of vancomycin in neurosurgery patients, from trough concentration to area under the curve: a retrospective single center cohort study in a tertiary hospital Abstract Objective To evaluate the effect of therapeutic drug monitoring (TDM) of vancomycin in neurosurgery patients. Methods In this ...
PMC12820277
core_pubmed_pmc
Expanding the payload scope in antibody-drug conjugates by delivery of hydroxy-containing drugs through self-immolative phosphoramidates
Expanding the payload scope in antibody-drug conjugates by delivery of hydroxy-containing drugs through self-immolative phosphoramidates Abstract Despite recent advances in targeted drug delivery, approved Antibody-Drug-Conjugates (ADCs) are still limited by the delivery of a restricted set of payloads with limited mod...
PMC9800720
core_pubmed_pmc
Size-advantage of monovalent nanobodies against the macrophage mannose receptor for deep tumor penetration and tumor-associated macrophage targeting
Size-advantage of monovalent nanobodies against the macrophage mannose receptor for deep tumor penetration and tumor-associated macrophage targeting Abstract Rationale: Nanobodies (Nbs) have emerged as an elegant alternative to the use of conventional monoclonal antibodies in cancer therapy, but a detailed microscopic ...
PMC5788896
core_pubmed_pmc
Geraniol Pharmacokinetics, Bioavailability and Its Multiple Effects on the Liver Antioxidant and Xenobiotic-Metabolizing Enzymes
Geraniol Pharmacokinetics, Bioavailability and Its Multiple Effects on the Liver Antioxidant and Xenobiotic-Metabolizing Enzymes Abstract Geraniol is a natural monoterpene showing anti-inflammatory, antioxidant, neuroprotective and anticancer effects. No pharmacokinetic and bioavailability data on geraniol are currentl...
PMC12521047
core_pubmed_pmc
Continuous‐Time Markov Population PK/PD Modeling of Longitudinal EASI Categorical Score in Atopic Dermatitis Treated With Rocatinlimab, an Anti‐OX40 Monoclonal Antibody
Continuous‐Time Markov Population PK/PD Modeling of Longitudinal EASI Categorical Score in Atopic Dermatitis Treated With Rocatinlimab, an Anti‐OX40 Monoclonal Antibody Abstract ABSTRACT Rocatinlimab (AMG 451/KHK4083) is a potential T‐cell rebalancing therapy that inhibits and reduces the number of pathogenic T cells b...
PMC11728838
core_pubmed_pmc
Novel Lipid Formulation Increases Absorption of Oral Cannabidiol (CBD)
Novel Lipid Formulation Increases Absorption of Oral Cannabidiol (CBD) Abstract Abstract Background : Cannabidiol (CBD) is an approved treatment for childhood epilepsies and a candidate treatment for several other CNS disorders. However, it has poor oral bioavailability. We investigated the effect of a novel lipid form...
PMC12647572
core_pubmed_pmc
Changes in blood concentration of tranexamic acid in dialysis and non-dialysis patients undergoing cardiac surgery: a prospective observational cohort study
Changes in blood concentration of tranexamic acid in dialysis and non-dialysis patients undergoing cardiac surgery: a prospective observational cohort study Abstract Abstract The pharmacokinetics of tranexamic acid (TXA), used during cardiopulmonary bypass (CPB) surgery, in patients receiving maintenance hemodialysis r...
PMC6044342
core_pubmed_pmc
Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate
Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate Abstract Background Biopharmaceutics classification system class II drugs have low solubility, which limits their extent and speed of absorption after oral administration. Ove...
PMC6360625
core_pubmed_pmc
Influences of Corydalis decumbens on the Activities of CYP450 Enzymes in Rats with a Cocktail Approach
Influences of Corydalis decumbens on the Activities of CYP450 Enzymes in Rats with a Cocktail Approach Abstract Abstract Corydalis decumbens , a Traditional Chinese Medicine, has been widely used for the alternative and/or complementary therapy of hypertension, arrhythmias rheumatoid arthritis, sciatica, stroke, hemipl...
PMC3969514
core_pubmed_pmc
Use of a linearization approximation facilitating stochastic model building
Use of a linearization approximation facilitating stochastic model building Abstract The objective of this work was to facilitate the development of nonlinear mixed effects models by establishing a diagnostic method for evaluation of stochastic model components. The random effects investigated were between subject, bet...
PMC9734231
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of PARP Inhibitors in Oncology
Pharmacokinetics and Pharmacodynamics of PARP Inhibitors in Oncology Abstract Olaparib, niraparib, rucaparib, and talazoparib are poly (ADP-ribose) polymerase (PARP) inhibitors approved for the treatment of ovarian, breast, pancreatic, and/or prostate cancer. Poly (ADP-ribose) polymerase inhibitors are potent inhibitor...
PMC9305196
core_pubmed_pmc
Emapalumab in primary haemophagocytic lymphohistiocytosis and the pathogenic role of interferon gamma: A pharmacometric model‐based approach
Emapalumab in primary haemophagocytic lymphohistiocytosis and the pathogenic role of interferon gamma: A pharmacometric model‐based approach Abstract Aim Primary haemophagocytic lymphohistiocytosis (HLH) is a rare, life‐threatening, hyperinflammatory syndrome generally occurring in early childhood. The monoclonal antib...
PMC11417140
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of the factor XIa ‐inhibiting antibody osocimab in healthy male East Asian volunteers: Results from two phase 1 studies
Pharmacokinetics and pharmacodynamics of the factor XIa ‐inhibiting antibody osocimab in healthy male East Asian volunteers: Results from two phase 1 studies Abstract Abstract The pharmacokinetics, pharmacodynamics, immunogenicity, and safety of osocimab single doses in healthy Chinese and Japanese volunteers over 149 ...
PMC12063479
core_pubmed_pmc
Elexacaftor/Tezacaftor/Ivacaftor Population Pharmacokinetics in Pediatric Patients With Cystic Fibrosis
Elexacaftor/Tezacaftor/Ivacaftor Population Pharmacokinetics in Pediatric Patients With Cystic Fibrosis Abstract ABSTRACT Elexacaftor/tezacaftor/ivacaftor (ETI) significantly improves treatment outcomes for people with cystic fibrosis (pwCF) with at least one F508del allele. In 2023, the Food and Drug Administration ap...
PMC11841632
core_pubmed_pmc
Population Pharmacokinetic Modeling of Cefepime, Meropenem, and Piperacillin-Tazobactam in Patients With Cystic Fibrosis
Population Pharmacokinetic Modeling of Cefepime, Meropenem, and Piperacillin-Tazobactam in Patients With Cystic Fibrosis Abstract Abstract Background Patients with cystic fibrosis (CF) experience recurrent bacterial pulmonary exacerbations. Management of these infections is increasingly challenging due to decreased ant...
PMC4783977
core_pubmed_pmc
Systems Pharmacology in Small Molecular Drug Discovery
Systems Pharmacology in Small Molecular Drug Discovery Abstract Drug discovery is a risky, costly and time-consuming process depending on multidisciplinary methods to create safe and effective medicines. Although considerable progress has been made by high-throughput screening methods in drug design, the cost of develo...
PMC8926483
core_pubmed_pmc
Aducanumab Therapy to Treat Alzheimer's Disease: A Narrative Review
Aducanumab Therapy to Treat Alzheimer's Disease: A Narrative Review Abstract Background Aducanumab, a new monoclonal antibody that targets β -amyloid aggregates, has been granted conditional approval by the U.S. FDA for treatment of mild Alzheimer's disease (AD). The approval of this drug without a confirmed significan...
PMC3153698
core_pubmed_pmc
Tacrolimus and 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: An interaction study in CYP3A5 non-expressors, renal transplant recipients
Tacrolimus and 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: An interaction study in CYP3A5 non-expressors, renal transplant recipients Abstract Abstract Objectives: Atherosclerosis is a significant factor affecting long-term outcome in renal transplant recipients. Studies have been conducted to determine...
PMC12819747
core_pubmed_pmc
A high content (30%) stable doxycycline hyclate drinking-water solution for broilers: preparation, stability, and bioequivalence
A high content (30%) stable doxycycline hyclate drinking-water solution for broilers: preparation, stability, and bioequivalence Abstract Introduction Doxycycline is a semi-synthetic tetracycline antibiotic with broad-spectrum antimicrobial activity. Under intensive animal husbandry, commercially available doxycycline ...
PMC10974343
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics: A Comprehensive Analysis of the Absorption, Distribution, Metabolism, and Excretion of Psychiatric Drugs
Pharmacokinetics and Pharmacodynamics: A Comprehensive Analysis of the Absorption, Distribution, Metabolism, and Excretion of Psychiatric Drugs Abstract Abstract The two main classifications of antidepressant medications are selective norepinephrine reuptake inhibitors (SNRIs) and selective serotonin reuptake inhibitor...
PMC11404436
core_pubmed_pmc
Gene polymorphism impact on opioid analgesic usage
Gene polymorphism impact on opioid analgesic usage Abstract Abstract Acute pain, moderate-to-severe cancer pain, and persistent malignant pain are all frequently treated with opioids. It is regarded as one of the main tenets of analgesic treatment. The relationship between human opioid sensitivity and genetic polymorph...
PMC8746447
core_pubmed_pmc
Two Possible Strategies for Drug Modification of Gemcitabine and Future Contributions to Personalized Medicine
Two Possible Strategies for Drug Modification of Gemcitabine and Future Contributions to Personalized Medicine Abstract Abstract Drug repurposing is an emerging strategy, which uses already approved drugs for new medical indications. One such drug is gemcitabine, an anticancer drug that only works at high doses since a...
PMC3944781
core_pubmed_pmc
Tobramycin exposure from active calcium sulfate bone graft substitute
Tobramycin exposure from active calcium sulfate bone graft substitute Abstract Background Bone graft substitute such as calcium sulfate are frequently used as carrier material for local antimicrobial therapy in orthopedic surgery. This study aimed to assess the systemic absorption and disposition of tobramycin in patie...
PMC6985042
core_pubmed_pmc
Biorelevant In Vitro Release Testing and In Vivo Study of Extended-Release Niacin Hydrophilic Matrix Tablets
Biorelevant In Vitro Release Testing and In Vivo Study of Extended-Release Niacin Hydrophilic Matrix Tablets Abstract Niacin (nicotinic acid, NA) is administered orally as an antihyperlipidemic agent in extended-release (ER) tablets in high doses. Due to rapid absorption and extensive metabolism (non-linear pharmacokin...
PMC10350899
core_pubmed_pmc
Tolerability and Efficacy of a 10:25 Preparation of Δ9-Tetrahydrocannabinol and Cannabidiol for Treatment of Chronic Back or Neck Pain: A Multiple-Dose Escalation Study
Tolerability and Efficacy of a 10:25 Preparation of Δ9-Tetrahydrocannabinol and Cannabidiol for Treatment of Chronic Back or Neck Pain: A Multiple-Dose Escalation Study Abstract Abstract Introduction The aim was to demonstrate the safety and tolerability of cannabidiol (CBD) with Δ9-THC in patients with moderate to sev...