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PMC4195667
core_pubmed_pmc
Personalized Tacrolimus Dose Requirement by CYP3A5 but Not ABCB1 or ACE Genotyping in Both Recipient and Donor after Pediatric Liver Transplantation
Personalized Tacrolimus Dose Requirement by CYP3A5 but Not ABCB1 or ACE Genotyping in Both Recipient and Donor after Pediatric Liver Transplantation Abstract Tacrolimus (TAC) is the backbone of an immunosuppressive drug used in most solid organ transplant recipients. A single nucleotide polymorphism (SNP) at position 6...
PMC4259998
core_pubmed_pmc
Population Pharmacokinetics of Intravenous Artesunate: A Pooled Analysis of Individual Data From Patients With Severe Malaria
Population Pharmacokinetics of Intravenous Artesunate: A Pooled Analysis of Individual Data From Patients With Severe Malaria Abstract Abstract There are ~660,000 deaths from severe malaria each year. Intravenous artesunate (i.v. ARS) is the first-line treatment in adults and children. To optimize the dosing regimen of...
PMC12679194
core_pubmed_pmc
Investigating the pharmaceutical substances and action mechanisms of Changmaxifeng granules against tic disorders
Investigating the pharmaceutical substances and action mechanisms of Changmaxifeng granules against tic disorders Abstract Abstract BACKGROUND Tic disorders (TDs) are a type of neurological and psychiatric disorder characterized by vocal or motor tics in the head, body, or limbs. Clinical studies have shown that Changm...
PMC11459961
core_pubmed_pmc
Systemic absorption and safety of topical terbinafine hydrochloride 10% solution (MOB015B): a phase 1 maximal usage trial in patients with moderate-to-severe onychomycosis
Systemic absorption and safety of topical terbinafine hydrochloride 10% solution (MOB015B): a phase 1 maximal usage trial in patients with moderate-to-severe onychomycosis Abstract ABSTRACT Topical antifungals may be considered to treat onychomycosis with minimal risk of systemic side effects. In this study, we assess ...
PMC11509103
core_pubmed_pmc
Differential Cytoprotective Effect of Resveratrol and Its Derivatives: Focus on Antioxidant and Autophagy-Inducing Effects
Differential Cytoprotective Effect of Resveratrol and Its Derivatives: Focus on Antioxidant and Autophagy-Inducing Effects Abstract Abstract Numerous beneficial effects of resveratrol were reported; however, its pharmacological profile is contradictious. Previously, we have demonstrated that resveratrol has a dose-depe...
PMC8211846
core_pubmed_pmc
Identification of optimal dosing schedules of dacomitinib and osimertinib for a phase I/II trial in advanced EGFR -mutant non-small cell lung cancer
Identification of optimal dosing schedules of dacomitinib and osimertinib for a phase I/II trial in advanced EGFR -mutant non-small cell lung cancer Abstract Despite the clinical success of the third-generation EGFR inhibitor osimertinib as a first-line treatment of EGFR -mutant non-small cell lung cancer (NSCLC), resi...
PMC7588963
core_pubmed_pmc
1,1-Difluoroethane Detection Time in Blood after Inhalation Abuse Estimated by Monte Carlo PBPK Modeling
1,1-Difluoroethane Detection Time in Blood after Inhalation Abuse Estimated by Monte Carlo PBPK Modeling Abstract (1) Background: Inhalant abuse and misuse are still widespread problems. 1,1-Difluoroethane abuse is reported to be potentially fatal and to cause acute and chronic adverse health effects. Lab testing for d...
PMC5357639
core_pubmed_pmc
In vivo Efficacy and Pharmacokinetics of Optimized Apidaecin Analogs
In vivo Efficacy and Pharmacokinetics of Optimized Apidaecin Analogs Abstract Proline-rich antimicrobial peptides (PrAMPs) represent promising alternative therapeutic options for the treatment of multidrug-resistant bacterial infections. PrAMPs are predominantly active against Gram-negative bacteria by inhibiting prote...
PMC6618770
core_pubmed_pmc
Pharmacokinetics and Target Attainment of Ceftobiprole in Asian and Non‐Asian Subjects
Pharmacokinetics and Target Attainment of Ceftobiprole in Asian and Non‐Asian Subjects Abstract Abstract Ceftobiprole is a broad‐spectrum cephalosporin. The objective of this study was to test the hypothesis that the pharmacokinetics (PK) and exposure of ceftobiprole in Asian subjects are similar to those in non‐Asian ...
PMC8930902
core_pubmed_pmc
Randomized Pharmacokinetic Study of a Highly Purified Human Chorionic Gonadotropin and of a Recombinant Human Chorionic Gonadotropin Following Single Subcutaneous Administration in Healthy Women
Randomized Pharmacokinetic Study of a Highly Purified Human Chorionic Gonadotropin and of a Recombinant Human Chorionic Gonadotropin Following Single Subcutaneous Administration in Healthy Women Abstract Abstract Background and Objectives Exogenous human chorionic gonadotropin (hCG) acts on the final phase of the folli...
PMC7493358
core_pubmed_pmc
Failure of target attainment of beta-lactam antibiotics in critically ill patients and associated risk factors: a two-center prospective study (EXPAT)
Failure of target attainment of beta-lactam antibiotics in critically ill patients and associated risk factors: a two-center prospective study (EXPAT) Abstract Background Early and appropriate antibiotic dosing is associated with improved clinical outcomes in critically ill patients, yet target attainment remains a cha...
PMC8520751
core_pubmed_pmc
Pharmacometrics meets statistics—A synergy for modern drug development
Pharmacometrics meets statistics—A synergy for modern drug development Abstract Abstract Modern drug development problems are very complex and require integration of various scientific fields. Traditionally, statistical methods have been the primary tool for design and analysis of clinical trials. Increasingly, pharmac...
PMC3152769
core_pubmed_pmc
Pentoxifylline as an adjunct therapy in children with cerebral malaria
Pentoxifylline as an adjunct therapy in children with cerebral malaria Abstract Background Pentoxifylline (PTX) affects many processes that may contribute to the pathogenesis of severe malaria and it has been shown to reduce the duration of coma in children with cerebral malaria. This pilot study was performed to asses...
PMC6192596
core_pubmed_pmc
Nanotracing and cavity-ring down spectroscopy: A new ultrasensitive approach in large molecule drug disposition studies
Nanotracing and cavity-ring down spectroscopy: A new ultrasensitive approach in large molecule drug disposition studies Abstract New therapeutic biological entities such as bispecific antibodies targeting tissue or specific cell populations form an increasingly important part of the drug development portfolio. However,...
PMC8632367
core_pubmed_pmc
Tissue Type Differences in ABCB1 Expression and Paclitaxel Tissue Pharmacokinetics in Patients With Esophageal Cancer
Tissue Type Differences in ABCB1 Expression and Paclitaxel Tissue Pharmacokinetics in Patients With Esophageal Cancer Abstract Background: Data from previous work suggests that there is no correlation between systemic (plasma) paclitaxel exposure and efficacy in patients treated for esophageal cancer. In this trial, we...
PMC3995995
core_pubmed_pmc
Development of an Adverse Drug Reaction Risk Assessment Score among Hospitalized Patients with Chronic Kidney Disease
Development of an Adverse Drug Reaction Risk Assessment Score among Hospitalized Patients with Chronic Kidney Disease Abstract Background Adverse drug reactions (ADRs) represent a major burden on the healthcare system. Chronic kidney disease (CKD) patients are particularly vulnerable to ADRs because they are usually on...
PMC9325261
core_pubmed_pmc
Developing New Treatments for COVID-19 through Dual-Action Antiviral/Anti-Inflammatory Small Molecules and Physiologically Based Pharmacokinetic Modeling
Developing New Treatments for COVID-19 through Dual-Action Antiviral/Anti-Inflammatory Small Molecules and Physiologically Based Pharmacokinetic Modeling Abstract Abstract Broad-spectrum antiviral agents that are effective against many viruses are difficult to develop, as the key molecules, as well as the biochemical p...
PMC8989052
core_pubmed_pmc
The novel bronchodilator navafenterol: a phase 2a, multicentre, randomised, double-blind, placebo-controlled crossover trial in COPD
The novel bronchodilator navafenterol: a phase 2a, multicentre, randomised, double-blind, placebo-controlled crossover trial in COPD Abstract Abstract Background Navafenterol (AZD8871) belongs to a new class of bronchodilator, the single-molecule muscarinic antagonist and β-agonist, developed for the treatment of COPD....
PMC12064635
core_pubmed_pmc
Model-Informed Dose Optimization of Pazopanib in Real-World Patients with Cancer
Model-Informed Dose Optimization of Pazopanib in Real-World Patients with Cancer Abstract Abstract Background and Objectives Pazopanib is approved for metastatic renal cell carcinoma (mRCC) and soft tissue sarcoma (STS) in a dose of 800 mg once daily (QD) taken under fasted conditions. In clinical practice, approximate...
PMC6461749
core_pubmed_pmc
Phase 1 dose-finding and pharmacokinetic study of eribulin-liposomal formulation in patients with solid tumours
Phase 1 dose-finding and pharmacokinetic study of eribulin-liposomal formulation in patients with solid tumours Abstract Abstract Background This phase 1 study examined the safety, tolerability, pharmacokinetics and preliminary efficacy of eribulin-liposomal formulation (eribulin-LF) in patients with advanced solid tum...
PMC7047841
core_pubmed_pmc
Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate
Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate Abstract Introduction Enrofloxacin is used in the treatment of a wide variety of bacterial infections in mammals. However, its poor solubility limits the clinical use. Methods In order to improve the solubility of enrofloxacin, the enroflo...
PMC12854914
core_pubmed_pmc
Early Evidence of Safety, Clinical Benefit, and Pharmacokinetics of Roflumilast Cream 0.3% Once Daily for Treatment of Mild or Moderate Plaque Psoriasis in Children Aged 2–11 Years
Early Evidence of Safety, Clinical Benefit, and Pharmacokinetics of Roflumilast Cream 0.3% Once Daily for Treatment of Mild or Moderate Plaque Psoriasis in Children Aged 2–11 Years Abstract ABSTRACT Two 4‐week, phase 2, open‐label, maximal usage pharmacokinetic (PK) and safety studies of once‐daily roflumilast cream 0....
PMC7564037
core_pubmed_pmc
Nonclinical safety, tolerance and pharmacodynamics evaluation for meplazumab treating chloroquine-resistant Plasmodium falciparum
Nonclinical safety, tolerance and pharmacodynamics evaluation for meplazumab treating chloroquine-resistant Plasmodium falciparum Abstract Meplazumab is an anti-CD147 humanized IgG2 antibody. The purpose of this study was to characterize the nonclinical safety, tolerance and efficacy evaluation of meplazumab treating c...
PMC11774110
core_pubmed_pmc
Effects of Food on the Pharmacokinetics and Safety of HA121-28 Tablet, a Novel Multi-Targeting Tyrosine Kinase Inhibitor, in Healthy Chinese Subjects: A Phase I Clinical Trial
Effects of Food on the Pharmacokinetics and Safety of HA121-28 Tablet, a Novel Multi-Targeting Tyrosine Kinase Inhibitor, in Healthy Chinese Subjects: A Phase I Clinical Trial Abstract Purpose HA121-28, a novel multi-targeting tyrosine kinase inhibitor, has dual efficacy against tumor growth and neovascularization. The...
PMC4961081
core_pubmed_pmc
Multiscale Systems‐Pharmacology Pipeline to Assess the Prophylactic Efficacy of NRTIs Against HIV‐1
Multiscale Systems‐Pharmacology Pipeline to Assess the Prophylactic Efficacy of NRTIs Against HIV‐1 Abstract While HIV‐1 continues to spread, the use of antivirals in preexposure prophylaxis (PrEP) has recently been suggested. Here we present a modular systems pharmacology modeling pipeline, predicting PrEP efficacy of...
PMC9686508
core_pubmed_pmc
Continuous Piperacillin-Tazobactam Infusion Improves Clinical Outcomes in Critically Ill Patients with Sepsis: A Retrospective, Single-Centre Study
Continuous Piperacillin-Tazobactam Infusion Improves Clinical Outcomes in Critically Ill Patients with Sepsis: A Retrospective, Single-Centre Study Abstract Continuous infusion of beta-lactam antibiotics has emerged as an alternative for the treatment of sepsis because of the favourable pharmacokinetics of continuous i...
PMC10898943
core_pubmed_pmc
A Case Report of a Patient with Soaring Clozapine Levels after Developing a Urinary Tract Infection
A Case Report of a Patient with Soaring Clozapine Levels after Developing a Urinary Tract Infection Abstract Abstract Clozapine is an antipsychotic medicine used to treat mental illnesses that is resistant to therapy. It can induce dose-dependent adverse effects such as increased susceptibility to infections and hemato...
PMC6964137
core_pubmed_pmc
Phase Ib Study of Combination Therapy with MEK Inhibitor Binimetinib and Phosphatidylinositol 3‐Kinase Inhibitor Buparlisib in Patients with Advanced Solid Tumors with RAS/RAF Alterations
Phase Ib Study of Combination Therapy with MEK Inhibitor Binimetinib and Phosphatidylinositol 3‐Kinase Inhibitor Buparlisib in Patients with Advanced Solid Tumors with RAS/RAF Alterations Abstract Abstract Background This multicenter, open‐label, phase Ib study investigated the safety and efficacy of binimetinib (MEK i...
PMC8300326
core_pubmed_pmc
The interaction of alpha-mangostin and its derivatives against main protease enzyme in COVID-19 using in silico methods
The interaction of alpha-mangostin and its derivatives against main protease enzyme in COVID-19 using in silico methods Abstract Abstract More than 111 million people worldwide have been affected by the COVID-19 outbreak caused by SARS-CoV-2. The main therapeutic target of COVID-19 is main protease (Mpro). It plays a k...
PMC11901792
core_pubmed_pmc
Chemical Composition and Larvicidal Activity Against Aedes aegypti of the Leaf Essential Oils from Croton blanchetianus
Chemical Composition and Larvicidal Activity Against Aedes aegypti of the Leaf Essential Oils from Croton blanchetianus Abstract The Aedes aegypti mosquito is the primary vector of dengue, a neglected disease and a serious public health problem in tropical countries. The control of this vector has been carried out usin...
PMC10226671
core_pubmed_pmc
RLS-0071 Moderated Elevated Myeloperoxidase Level and Activity in an Asymptomatic Subject in Clinical Trial RLS-0071-101
RLS-0071 Moderated Elevated Myeloperoxidase Level and Activity in an Asymptomatic Subject in Clinical Trial RLS-0071-101 Abstract Patient: Female, 21-year-old Final Diagnosis: Healthy Symptoms: Asymptomatic Clinical Procedure: Clinical trial Specialty: Immunology Objective: Unknown etiology Background: RLS-0071 is a du...
PMC10389201
core_pubmed_pmc
A model-based quantitative analysis of efficacy and associated factors of platelet rich plasma treatment for osteoarthritis
A model-based quantitative analysis of efficacy and associated factors of platelet rich plasma treatment for osteoarthritis Abstract Objective: While platelet rich plasma (PRP) has been extensively studied in treating osteoarthritis (OA), there has been an ongoing debate regarding the efficacy of PRP and the optimal su...
PMC12110728
core_pubmed_pmc
Pharmacokinetic and Exposure–Response Modeling Support Body Surface Area‐Based Dosing of Farletuzumab Ecteribulin in Japanese Patients with Solid Tumors
Pharmacokinetic and Exposure–Response Modeling Support Body Surface Area‐Based Dosing of Farletuzumab Ecteribulin in Japanese Patients with Solid Tumors Abstract Abstract The first‐in‐human, Phase 1 Study 101 showed antitumor activity and a tolerable safety profile of farletuzumab ecteribulin in Japanese patients with ...
PMC4503439
core_pubmed_pmc
Dose-Independent ADME Properties and Tentative Identification of Metabolites of α-Mangostin from Garcinia mangostana in Mice by Automated Microsampling and UPLC-MS/MS Methods
Dose-Independent ADME Properties and Tentative Identification of Metabolites of α-Mangostin from Garcinia mangostana in Mice by Automated Microsampling and UPLC-MS/MS Methods Abstract Abstract The information about a marker compound's pharmacokinetics in herbal products including the characteristics of absorption, dist...
PMC3590589
core_pubmed_pmc
Optimized siRNA-PEG Conjugates for Extended Blood Circulation and Reduced Urine Excretion in Mice
Optimized siRNA-PEG Conjugates for Extended Blood Circulation and Reduced Urine Excretion in Mice Abstract Some of the main concerns with in vivo application of naked small interfering RNA are rapid degradation and urinary excretion resulting in a short plasma half-life. In this study we investigated how conjugation of...
PMC7181426
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Peficitinib (ASP015K) in Healthy Male Caucasian and Japanese Subjects
Pharmacokinetics, Pharmacodynamics, and Safety of Peficitinib (ASP015K) in Healthy Male Caucasian and Japanese Subjects Abstract Background and Objective Peficitinib pharmacokinetics and pharmacodynamics have been characterized mainly in Caucasian subjects. This study investigated the pharmacokinetics, pharmacodynamics...
PMC10731587
core_pubmed_pmc
Quantitative systems pharmacology model of erythropoiesis to simulate therapies targeting anemia due to chronic kidney disease
Quantitative systems pharmacology model of erythropoiesis to simulate therapies targeting anemia due to chronic kidney disease Abstract Anemia induced by chronic kidney disease (CKD) has multiple underlying mechanistic causes and generally worsens as CKD progresses. Erythropoietin (EPO) is a key endogenous protein whic...
PMC5397563
core_pubmed_pmc
Morphine Pharmacodynamics in Mechanically Ventilated Preterm Neonates Undergoing Endotracheal Suctioning
Morphine Pharmacodynamics in Mechanically Ventilated Preterm Neonates Undergoing Endotracheal Suctioning Abstract To date, morphine pharmacokinetics (PKs) are well quantified in neonates, but results about its efficacy are ambiguous. This work presents an analysis of a previously published study on pain measurements in...
PMC9263204
core_pubmed_pmc
Strategies to Reduce Mortality Among Children Living With HIV and Children Exposed to HIV but Are Uninfected, Admitted With Severe Acute Malnutrition at Mulago Hospital, Uganda (REDMOTHIV): A Mixed Methods Study
Strategies to Reduce Mortality Among Children Living With HIV and Children Exposed to HIV but Are Uninfected, Admitted With Severe Acute Malnutrition at Mulago Hospital, Uganda (REDMOTHIV): A Mixed Methods Study Abstract Background Children living with HIV (CLHIV) and children who are exposed to HIV but uninfected (CHE...
PMC12166440
core_pubmed_pmc
The effect of black tea and water temperature on the disintegration of gelatine and HPMC capsules, tested with the paddle device, GastroDuo and in vivo pharmacokinetics: Much ado about little
The effect of black tea and water temperature on the disintegration of gelatine and HPMC capsules, tested with the paddle device, GastroDuo and in vivo pharmacokinetics: Much ado about little Abstract Fluid co-administered with oral medication directly affects its behaviour. Often, people use fluids other than water wh...
PMC4598208
core_pubmed_pmc
Maraviroc: a review of its use in HIV infection and beyond
Maraviroc: a review of its use in HIV infection and beyond Abstract The human immunodeficiency virus-1 (HIV-1) enters target cells by binding its envelope glycoprotein gp120 to the CD4 receptor and/or coreceptors such as C-C chemokine receptor type 5 (CCR5; R5) and C-X-C chemokine receptor type 4 (CXCR4; X4), and R5-tr...
PMC5020340
core_pubmed_pmc
Predicting lung dosimetry of inhaled particleborne benzo[a]pyrene using physiologically based pharmacokinetic modeling
Predicting lung dosimetry of inhaled particleborne benzo[a]pyrene using physiologically based pharmacokinetic modeling Abstract Abstract Benzo[a]pyrene (BaP) is a by-product of incomplete combustion of fossil fuels and plant/wood products, including tobacco. A physiologically based pharmacokinetic (PBPK) model for BaP ...
PMC6118139
core_pubmed_pmc
Therapeutic implications of nano-encapsulated rifabutin, azithromycin & ethambutol against experimental Mycobacterium avium infection in mice
Therapeutic implications of nano-encapsulated rifabutin, azithromycin & ethambutol against experimental Mycobacterium avium infection in mice Abstract Background & objectives: Mycobacterium avium causes atypical infection in both immunocompetent and immunocompromised individuals. Conventional chemotherapy for M. avium ...
PMC10448909
core_pubmed_pmc
A First-in-human, Dose-escalation Study of the Methionine Aminopeptidase 2 Inhibitor M8891 in Patients with Advanced Solid Tumors
A First-in-human, Dose-escalation Study of the Methionine Aminopeptidase 2 Inhibitor M8891 in Patients with Advanced Solid Tumors Abstract Abstract Methionine aminopeptidase 2 (MetAP2) is essential to endothelial cell growth and proliferation during tumor angiogenesis. M8891 is a novel orally bioavailable, potent, sele...
PMC9331863
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Analysis of Dalbavancin for Long-Term Treatment of Subacute and/or Chronic Infectious Diseases: The Major Role of Therapeutic Drug Monitoring
Population Pharmacokinetic and Pharmacodynamic Analysis of Dalbavancin for Long-Term Treatment of Subacute and/or Chronic Infectious Diseases: The Major Role of Therapeutic Drug Monitoring Abstract Abstract A population pharmacokinetic analysis of dalbavancin was conducted in patients with different infection sites. No...
PMC11966180
core_pubmed_pmc
Enhanced Absorption and Safety of MuscleBlaze CreAMP™: A Comparative Analysis With Regular Micronized Creatine Monohydrate in Healthy Male Adults
Enhanced Absorption and Safety of MuscleBlaze CreAMP™: A Comparative Analysis With Regular Micronized Creatine Monohydrate in Healthy Male Adults Abstract Background Creatine monohydrate is a widely utilized dietary supplement in sports nutrition, valued for its role in enhancing muscle energy availability, power outpu...
PMC6955413
core_pubmed_pmc
Physiologically based pharmacokinetic evaluation of cefuroxime in perioperative antibiotic prophylaxis
Physiologically based pharmacokinetic evaluation of cefuroxime in perioperative antibiotic prophylaxis Abstract Abstract Aims Adequate plasma concentrations of antibiotics during surgery are essential for the prevention of surgical site infections. We examined the pharmacokinetics of 1.5 g cefuroxime administered durin...
PMC12371256
core_pubmed_pmc
A Randomized, Open‐Label, Single‐Dose, Parallel‐Group Bioequivalence Study of Ferric Carboxymaltose Injection Under Fasting Conditions in Chinese Adult Subjects With Iron Deficiency Anemia
A Randomized, Open‐Label, Single‐Dose, Parallel‐Group Bioequivalence Study of Ferric Carboxymaltose Injection Under Fasting Conditions in Chinese Adult Subjects With Iron Deficiency Anemia Abstract ABSTRACT The objectives of this study were to compare the pharmacokinetics and safety profiles of the test (T) preparation...
PMC3957867
core_pubmed_pmc
Pharmacokinetics of Orally Administered Oseltamivir in Healthy Obese and Nonobese Thai Subjects
Pharmacokinetics of Orally Administered Oseltamivir in Healthy Obese and Nonobese Thai Subjects Abstract Oseltamivir is the most widely used anti-influenza drug. In the 2009 H1N1 pandemic, in which the influenza viruses were oseltamivir sensitive, obesity was identified as a risk factor for severe disease and unfavorab...
PMC11369432
core_pubmed_pmc
Study on the uptake of Gastrodin in the liver
Study on the uptake of Gastrodin in the liver Abstract Abstract Background Gastrodin is the active monomer of the Chinese herb Rhizoma Gastrodiae with the largest quantity of active components. Gastrodin is commonly used in the treatment of central nervous system disorders such as headaches and epilepsy due to its seda...
PMC12038836
core_pubmed_pmc
Total Synthesis and Pharmacological Evaluation of Phochrodines A–C
Total Synthesis and Pharmacological Evaluation of Phochrodines A–C Abstract The first syntheses of the Phomopsis -isolated natural products phochrodines A–C are reported. Functional group manipulations on a key 5 H -chromeno[4,3- b ]pyridine intermediate, itself synthesized from intramolecular Suzuki–Miyaura coupling, ...
PMC7136080
core_pubmed_pmc
Evaluation of pharmacokinetic interactions between amoxicillin, clarithromycin, and the potassium-competitive acid blocker YH4808 in healthy subjects
Evaluation of pharmacokinetic interactions between amoxicillin, clarithromycin, and the potassium-competitive acid blocker YH4808 in healthy subjects Abstract Abstract YH4808 is a novel potassium-competitive acid blocker that was developed as a therapeutic agent for gastric acid-related diseases; it may replace proton ...
PMC9930093
core_pubmed_pmc
Supramolecular Phenylalanine-Derived Hydrogels for the Sustained Release of Functional Proteins
Supramolecular Phenylalanine-Derived Hydrogels for the Sustained Release of Functional Proteins Abstract Abstract Protein-based therapeutics have emerged as next-generation pharmaceutical agents for oncology, bone regeneration, autoimmune disorders, viral infections, and other diseases. The clinical application of prot...
PMC11502236
core_pubmed_pmc
Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2D6 , ADRB1 , ADRB2 , ADRA2C , GRK4 , and GRK5 Genotypes and Beta-Blocker Therapy
Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2D6 , ADRB1 , ADRB2 , ADRA2C , GRK4 , and GRK5 Genotypes and Beta-Blocker Therapy Abstract Beta-blockers are widely used medications for a variety of indications, including heart failure, myocardial infarction, cardiac arrhythmias, and hyperten...
PMC5572360
core_pubmed_pmc
Supervised Machine‐Learning Reveals That Old and Obese People Achieve Low Dapsone Concentrations
Supervised Machine‐Learning Reveals That Old and Obese People Achieve Low Dapsone Concentrations Abstract The human species is becoming increasingly obese. Dapsone, which is extensively used across the globe for dermatological disorders, arachnid bites, and for treatment of several bacterial, fungal, and parasitic dise...
PMC6105874
core_pubmed_pmc
Pharmacokinetics of rifampicin in adult TB patients and healthy volunteers: a systematic review and meta-analysis
Pharmacokinetics of rifampicin in adult TB patients and healthy volunteers: a systematic review and meta-analysis Abstract Abstract Objectives The objectives of this study were to explore inter-study heterogeneity in the pharmacokinetics (PK) of orally administered rifampicin, to derive summary estimates of rifampicin ...
PMC12352996
core_pubmed_pmc
Physiologically-Based Pharmacokinetics and Empirical Pharmacodynamic Modeling for Pediatric Henagliflozin Dosing: Clinical Insights for Chinese Patients
Physiologically-Based Pharmacokinetics and Empirical Pharmacodynamic Modeling for Pediatric Henagliflozin Dosing: Clinical Insights for Chinese Patients Abstract Abstract Objective: This study aimed to present a quantitative modeling and simulation approach for oral henagliflozin, a selective sodium-glucose cotransport...
PMC9893258
core_pubmed_pmc
Synthesis, Characterization, Pharmacogenomics, and Molecular Simulation of Pyridinium Type of Ionic Liquids and Their Applications
Synthesis, Characterization, Pharmacogenomics, and Molecular Simulation of Pyridinium Type of Ionic Liquids and Their Applications Abstract Abstract Substituted pyridinium bromides are prepared by conventional and solvent-free greener methods. The solvent-free solid-phase (greener) method is superior to the conventiona...
PMC12439002
core_pubmed_pmc
Comparison of Regression and Categorical Analysis for Pharmacokinetic Data From Renal Impairment Studies
Comparison of Regression and Categorical Analysis for Pharmacokinetic Data From Renal Impairment Studies Abstract The US Food and Drug Administration 2024 guidance prefers regression analysis over categorical analysis for pharmacokinetic data for studies that assess pharmacokinetics in patients with impaired renal func...
PMC5590147
core_pubmed_pmc
Intrinsic fluorescence of the clinically approved multikinase inhibitor nintedanib reveals lysosomal sequestration as resistance mechanism in FGFR-driven lung cancer
Intrinsic fluorescence of the clinically approved multikinase inhibitor nintedanib reveals lysosomal sequestration as resistance mechanism in FGFR-driven lung cancer Abstract Background Studying the intracellular distribution of pharmacological agents, including anticancer compounds, is of central importance in biomedi...
PMC3516836
core_pubmed_pmc
Image Guided Biodistribution and Pharmacokinetic Studies of Theranostics
Image Guided Biodistribution and Pharmacokinetic Studies of Theranostics Abstract Abstract Image guided technique is playing an increasingly important role in the investigation of the biodistribution and pharmacokinetics of drugs or drug delivery systems in various diseases, especially cancers. Besides anatomical imagi...
PMC8894322
core_pubmed_pmc
Nanomedicine Ex Machina: Between Model-Informed Development and Artificial Intelligence
Nanomedicine Ex Machina: Between Model-Informed Development and Artificial Intelligence Abstract Abstract Today, a growing number of computational aids and simulations are shaping model-informed drug development. Artificial intelligence, a family of self-learning algorithms, is only the latest emerging trend applied by...
PMC8662762
core_pubmed_pmc
Rezafungin Versus Caspofungin in a Phase 2, Randomized, Double-blind Study for the Treatment of Candidemia and Invasive Candidiasis: The STRIVE Trial
Rezafungin Versus Caspofungin in a Phase 2, Randomized, Double-blind Study for the Treatment of Candidemia and Invasive Candidiasis: The STRIVE Trial Abstract Abstract Background Rezafungin (RZF) is a novel echinocandin exhibiting distinctive pharmacokinetics/pharmacodynamics. STRIVE was a phase 2, double-blind, random...
PMC5828556
core_pubmed_pmc
Steady-State Clozapine and Norclozapine Pharmacokinetics in Maori and European Patients
Steady-State Clozapine and Norclozapine Pharmacokinetics in Maori and European Patients Abstract Abstract Background Clozapine is the most effective drug for treatment-resistant schizophrenia, but its use is limited by toxicity. Because ethnicity has been reported to affect clozapine metabolism, we compared its steady ...
PMC10786955
core_pubmed_pmc
Digoxin Pharmacokinetics in Patients with Obesity Before and After a Gastric Bypass or a Strict Diet Compared with Normal Weight Individuals
Digoxin Pharmacokinetics in Patients with Obesity Before and After a Gastric Bypass or a Strict Diet Compared with Normal Weight Individuals Abstract Background and Objective Several drugs on the market are substrates for P-glycoprotein (P-gp), an efflux transporter highly expressed in barrier tissues such as the intes...
PMC6446180
core_pubmed_pmc
Randomised, double-blind, phase III study comparing the infliximab biosimilar, PF-06438179/GP1111, with reference infliximab: efficacy, safety and immunogenicity from week 30 to week 54
Randomised, double-blind, phase III study comparing the infliximab biosimilar, PF-06438179/GP1111, with reference infliximab: efficacy, safety and immunogenicity from week 30 to week 54 Abstract Abstract Objective To investigate the efficacy, safety and immunogenicity of PF-06438179/GP1111 (PF-SZ-IFX) compared with Eur...
PMC10237409
core_pubmed_pmc
Trotabresib, an oral potent bromodomain and extraterminal inhibitor, in patients with high-grade gliomas: A phase I, “window-of-opportunity” study
Trotabresib, an oral potent bromodomain and extraterminal inhibitor, in patients with high-grade gliomas: A phase I, “window-of-opportunity” study Abstract Abstract Background The bromodomain and extraterminal protein (BET) inhibitor trotabresib has demonstrated antitumor activity in patients with advanced solid tumors...
PMC6306117
core_pubmed_pmc
Pharmacokinetic Study of Sirolimus-Eluting BioResorbable Vascular Scaffold System for Treatment of De Novo Native Coronary Lesions: A Sub-Study of MeRes-1 Trial
Pharmacokinetic Study of Sirolimus-Eluting BioResorbable Vascular Scaffold System for Treatment of De Novo Native Coronary Lesions: A Sub-Study of MeRes-1 Trial Abstract Background MeRes100™ (Meril Life Sciences Pvt. Ltd., Vapi, India) is a novel sirolimus-eluting bioresorbable vascular scaffold (BRS). The purpose of t...
PMC3435480
core_pubmed_pmc
FUNCTIONAL CHARACTERIZATION OF ABCC2 PROMOTER POLYMORPHISMS AND ALLELE SPECIFIC EXPRESSION
FUNCTIONAL CHARACTERIZATION OF ABCC2 PROMOTER POLYMORPHISMS AND ALLELE SPECIFIC EXPRESSION Abstract Multidrug resistance protein 2 (MRP2, ABCC2) is an efflux membrane transporter highly expressed in liver, kidney and intestine with important physiological and pharmacological roles. The goal of this study was to investi...
PMC4720030
core_pubmed_pmc
Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells
Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells Abstract Metabotropic glutamate receptor 4 (mGluR4) possesses immune modulatory properties in vivo , such that a positive allosteric modulator (PAM) of the receptor confers protection on mi...
PMC8597115
core_pubmed_pmc
Base and Covariate Population Pharmacokinetic Analyses of Dupilumab in Adolescents and Children ≥6 to <12 Years of Age Using Phase 3 Data
Base and Covariate Population Pharmacokinetic Analyses of Dupilumab in Adolescents and Children ≥6 to <12 Years of Age Using Phase 3 Data Abstract Abstract Population pharmacokinetic (PK) base and covariate analyses were conducted using data from adolescents with moderate‐to‐severe atopic dermatitis (AD) and children ≥...
PMC8776711
core_pubmed_pmc
Impact of Sampling Time Variability on Tacrolimus Dosage Regimen in Pediatric Primary Nephrotic Syndrome: Single-Center, Prospective, Observational Study
Impact of Sampling Time Variability on Tacrolimus Dosage Regimen in Pediatric Primary Nephrotic Syndrome: Single-Center, Prospective, Observational Study Abstract Background: Tacrolimus (TAC) is an important immunosuppressant for children with primary nephrotic syndrome (PNS). The relationship between sampling time var...
PMC9395610
core_pubmed_pmc
Spectrum effect correlation of yangyin tongnao granules on cerebral ischemia-reperfusion injury rats
Spectrum effect correlation of yangyin tongnao granules on cerebral ischemia-reperfusion injury rats Abstract Yangyin Tongnao Granules (YYTNG), as traditional Chinese medicine (TCM) compound preparation, have a good curative effect on cerebral ischemia-reperfusion injury. This study aimed to investigate the relationshi...
PMC10457821
core_pubmed_pmc
Amorphous Solid Dispersion as Drug Delivery Vehicles in Cancer
Amorphous Solid Dispersion as Drug Delivery Vehicles in Cancer Abstract Cancer treatment has improved over the past decades, but a major challenge lies in drug formulation, specifically for oral administration. Most anticancer drugs have poor water solubility which can affect their bioavailability. This causes suboptim...
PMC4774801
core_pubmed_pmc
Pharmacokinetic interaction of curcumin and glibenclamide in diabetic rats
Pharmacokinetic interaction of curcumin and glibenclamide in diabetic rats Abstract Abstract Aim: The aim was to assess the pharmacokinetic (PK) interaction of curcumin and glibenclamide (GL) in diabetic rats. Materials and Methods: Sprague-Dawley rats induced with diabetes were divided into 2 groups of six rats in eac...
PMC12691640
core_pubmed_pmc
Unlocking potentials: the impact of meropenem, meropenem-vaborbactam, and ceftazidime-avibactam in combating carbapenem-resistant Enterobacter cloacae
Unlocking potentials: the impact of meropenem, meropenem-vaborbactam, and ceftazidime-avibactam in combating carbapenem-resistant Enterobacter cloacae Abstract ABSTRACT Carbapenem-resistant Enterobacterales (CREs) are recognized as an urgent public threat by the Centers for Disease Control and Prevention. This study as...
PMC7306027
core_pubmed_pmc
Single dose epidural hydromorphone in labour pain: maternal pharmacokinetics and neonatal exposure
Single dose epidural hydromorphone in labour pain: maternal pharmacokinetics and neonatal exposure Abstract Abstract Introduction Epidural hydromorphone could be useful in obstetric analgesia as there is a need for a more water-soluble opioid than sufentanil or fentanyl with prolonged analgesic effect. To our knowledge...
PMC8879496
core_pubmed_pmc
Anticoronaviral Activity of the Natural Phloroglucinols, Dryocrassin ABBA and Filixic Acid ABA from the Rhizome of Dryopteris crassirhizoma by Targeting the Main Protease of SARS-CoV-2
Anticoronaviral Activity of the Natural Phloroglucinols, Dryocrassin ABBA and Filixic Acid ABA from the Rhizome of Dryopteris crassirhizoma by Targeting the Main Protease of SARS-CoV-2 Abstract The rhizome of Dryopteris crassirhizoma Nakai. (Dryopteridaceae) has been used in traditional medicine in East Asia and has re...
PMC12389431
core_pubmed_pmc
Phytocannabinoids as Novel SGLT2 Modulators for Renal Glucose Reabsorption in Type 2 Diabetes Management
Phytocannabinoids as Novel SGLT2 Modulators for Renal Glucose Reabsorption in Type 2 Diabetes Management Abstract Abstract Background : Sodium–glucose cotransporter 2 (SGLT2) inhibitors have transformed type 2 diabetes mellitus (T2DM) management by promoting glucosuria, lowering glycated hemoglobin (HbA1c), blood press...
PMC6332382
core_pubmed_pmc
Pharmacokinetics of Ginkgolide B after Oral Administration of Three Different Ginkgolide B Formulations in Beagle Dogs
Pharmacokinetics of Ginkgolide B after Oral Administration of Three Different Ginkgolide B Formulations in Beagle Dogs Abstract Ginkgolide B (GB), an important active constituent of Ginkgo biloba extract, has been used in clinical applications for the treatment of dementia, cerebral insufficiency or related cognitive d...
PMC7992283
core_pubmed_pmc
A novel sustained‐release cysteamine bitartrate formulation for the treatment of cystinosis: Pharmacokinetics and safety in healthy male volunteers
A novel sustained‐release cysteamine bitartrate formulation for the treatment of cystinosis: Pharmacokinetics and safety in healthy male volunteers Abstract Abstract The strict intake regimen of cysteamine bitartrate formulations, associated with side effects, is a concern for the treatment compliance in cystinosis the...
PMC3970101
core_pubmed_pmc
A Cell-Based Pharmacokinetics Assay for Evaluating Tubulin-Binding Drugs
A Cell-Based Pharmacokinetics Assay for Evaluating Tubulin-Binding Drugs Abstract Abstract Increasing evidence reveals that traditional pharmacokinetics parameters based on plasma drug concentrations are insufficient to reliably demonstrate accurate pharmacological effects of drugs in target organs or cells in vivo. Th...
PMC12242391
core_pubmed_pmc
Evaluation of drug-drug interaction potentials between JP-1366 and celecoxib using physiologically based pharmacokinetic modeling
Evaluation of drug-drug interaction potentials between JP-1366 and celecoxib using physiologically based pharmacokinetic modeling Abstract Abstract Zastaprazan (JP-1366) is a new potassium-competitive acid blocker being developed for treating gastrointestinal reflux disease. It is an orally administered small molecule ...
PMC12298542
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of (R)-Ketamine Hydrochloride Injection, a Novel Rapid-Acting Antidepressant, in Healthy Chinese Subjects
Pharmacokinetics, Safety, and Tolerability of (R)-Ketamine Hydrochloride Injection, a Novel Rapid-Acting Antidepressant, in Healthy Chinese Subjects Abstract Abstract Objectives : (R)-ketamine hydrochloride injection is a novel, rapid-acting antidepressant for the treatment of treatment-resistant depression. The aim of...
PMC6108095
core_pubmed_pmc
Evaluating the safety, tolerability, pharmacokinetics and efficacy of clofazimine in cryptosporidiosis (CRYPTOFAZ): study protocol for a randomized controlled trial
Evaluating the safety, tolerability, pharmacokinetics and efficacy of clofazimine in cryptosporidiosis (CRYPTOFAZ): study protocol for a randomized controlled trial Abstract Abstract Background Cryptosporidium infection and diarrhea (cryptosporidiosis) is a life-threatening infection in persons with HIV and also in chi...
PMC5771593
core_pubmed_pmc
A non-linear pharmacokinetic-pharmacodynamic relationship of metformin in healthy volunteers: An open-label, parallel group, randomized clinical study
A non-linear pharmacokinetic-pharmacodynamic relationship of metformin in healthy volunteers: An open-label, parallel group, randomized clinical study Abstract Abstract Background The aim of this study was to explore the pharmacokinetic-pharmacodynamic (PK-PD) relationship of metformin on glucose levels after the admin...
PMC3825677
core_pubmed_pmc
Efficacy of Retigabine in Adjunctive Treatment of Partial Onset Seizures in Adults
Efficacy of Retigabine in Adjunctive Treatment of Partial Onset Seizures in Adults Abstract Objective To evaluate efficacy and tolerability of retigabine (ezogabine, US adopted name) in the adjunctive treatment of partial-onset seizures in adults. Retigabine is the first anticonvulsant in its class, decreasing neuronal...
PMC5382042
core_pubmed_pmc
Fludarabine with pharmacokinetically-guided IV busulfan is superior to fixed-dose delivery in pretransplant conditioning of AML/MDS patients
Fludarabine with pharmacokinetically-guided IV busulfan is superior to fixed-dose delivery in pretransplant conditioning of AML/MDS patients Abstract We hypothesized that IV Busulfan (Bu) dosing could be safely intensified through pharmacokinetic (PK-) dose guidance to minimize the inter-patient variability in systemic...
PMC8116427
core_pubmed_pmc
Pharmacokinetics of Levornidazole Tablet in Healthy Chinese Subjects and Proposed Dosing Regimen Based on Pharmacokinetic/Pharmacodynamic Analysis
Pharmacokinetics of Levornidazole Tablet in Healthy Chinese Subjects and Proposed Dosing Regimen Based on Pharmacokinetic/Pharmacodynamic Analysis Abstract Abstract Introduction Levornidazole is a novel nitroimidazole antimicrobial agent active against anaerobes. We aimed to investigate the pharmacokinetic (PK) profile...
PMC8658702
core_pubmed_pmc
Arterial Hypertension in Aortic Valve Stenosis: A Critical Update
Arterial Hypertension in Aortic Valve Stenosis: A Critical Update Abstract Aortic stenosis (AS) is a very common valve disease and is associated with high mortality once it becomes symptomatic. Arterial hypertension (HT) has a high prevalence among patients with AS leading to worse left ventricle remodeling and faster ...
PMC12844682
core_pubmed_pmc
Pharmacokinetics and Childhood Obesity: Pathophysiological Basis and Challenges in Choosing the Ideal Body Size Descriptor
Pharmacokinetics and Childhood Obesity: Pathophysiological Basis and Challenges in Choosing the Ideal Body Size Descriptor Abstract Abstract Despite the progressive increase in obesity and associated chronic diseases in children, there is limited evidence on the optimal dosage of most medications for obese children and...
PMC8245786
core_pubmed_pmc
Comparative Studies on Multi-Component Pharmacokinetics of Polygonum multiflorum Thunb Extract After Oral Administration in Different Rat Models
Comparative Studies on Multi-Component Pharmacokinetics of Polygonum multiflorum Thunb Extract After Oral Administration in Different Rat Models Abstract Abstract The clinical use of Polygonum multiflorum Thunb (PM) has been restricted or banned in many countries, due to its hepatotoxic adverse effects. Its toxicity re...
PMC12844686
core_pubmed_pmc
Efficacy and Safety of SA001 in Patients with Primary Sjögren’s Syndrome: A Randomized, Double-Blind, Placebo-Controlled Trial
Efficacy and Safety of SA001 in Patients with Primary Sjögren’s Syndrome: A Randomized, Double-Blind, Placebo-Controlled Trial Abstract Abstract Background/Objectives : SA001, a mofetil-ester prodrug of rebamipide, was developed to enhance gastrointestinal absorption and systemic exposure, which was confirmed in a prio...
PMC11568852
core_pubmed_pmc
Effect-Site Concentration of Remimazolam by Age Groups During Target-Controlled Infusion for Total Intravenous Anesthesia: A Retrospective Comparative Study
Effect-Site Concentration of Remimazolam by Age Groups During Target-Controlled Infusion for Total Intravenous Anesthesia: A Retrospective Comparative Study Abstract Purpose Pharmacokinetic and pharmacodynamic (PKPD) models exist for remimazolam, but data for target-controlled infusion (TCI) are limited. The Schüttler ...
PMC6882847
core_pubmed_pmc
Pharmacogenetics of amfepramone in healthy Mexican subjects reveals potential markers for tailoring pharmacotherapy of obesity: results of a randomised trial
Pharmacogenetics of amfepramone in healthy Mexican subjects reveals potential markers for tailoring pharmacotherapy of obesity: results of a randomised trial Abstract Amfepramone (AFP) is an appetite-suppressant drug used in the treatment of obesity. Nonetheless, studies on interindividual pharmacokinetic variability a...
PMC11493442
core_pubmed_pmc
Sensory-Motor Neuropathy in Mfn2 T105M Knock-in Mice and Its Reversal by a Novel Piperine-Derived Mitofusin Activator
Sensory-Motor Neuropathy in Mfn2 T105M Knock-in Mice and Its Reversal by a Novel Piperine-Derived Mitofusin Activator Abstract Mitochondrial dysfunction is a hallmark of many genetic neurodegenerative diseases, but therapeutic options to reverse mitochondrial dysfunction are limited. While recent studies support the po...
PMC5394133
core_pubmed_pmc
Pharmacokinetic Properties of Fast-Acting Insulin Aspart Administered in Different Subcutaneous Injection Regions
Pharmacokinetic Properties of Fast-Acting Insulin Aspart Administered in Different Subcutaneous Injection Regions Abstract Abstract Background Fast-acting insulin aspart (faster aspart) is insulin aspart set in a new formulation with faster initial absorption after subcutaneous administration. This study investigated t...
PMC6360331
core_pubmed_pmc
Population Pharmacokinetic Estimates Suggest Elevated Clearance and Distribution Volume of Desethylamodiaquine in Pediatric Patients with Sickle Cell Disease Treated with Artesunate-Amodiaquine
Population Pharmacokinetic Estimates Suggest Elevated Clearance and Distribution Volume of Desethylamodiaquine in Pediatric Patients with Sickle Cell Disease Treated with Artesunate-Amodiaquine Abstract Abstract Background There is limited information on the safety or efficacy of currently recommended antimalarial drug...
PMC7962407
core_pubmed_pmc
A randomized, placebo-controlled experimental medicine study of RIPK1 inhibitor GSK2982772 in patients with moderate to severe rheumatoid arthritis
A randomized, placebo-controlled experimental medicine study of RIPK1 inhibitor GSK2982772 in patients with moderate to severe rheumatoid arthritis Abstract Abstract Background Receptor-interacting protein kinase 1 (RIPK1) is a key mediator of inflammation through cell death and proinflammatory cytokine production. Thi...
PMC7617887
core_pubmed_pmc
A novel LC-MS/MS method for the determination of favipiravir ribofuranosyl-5’-triphosphate (T-705-RTP) in human peripheral mononuclear cells
A novel LC-MS/MS method for the determination of favipiravir ribofuranosyl-5’-triphosphate (T-705-RTP) in human peripheral mononuclear cells Abstract Favipiravir is a broad-spectrum antiviral that is metabolised intracellularly into the active form, favipiravir ribofuranosyl-5’-triphosphate (F-RTP). Measurement of the ...