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PMC9424636
core_pubmed_pmc
Population pharmacokinetic/pharmacodynamic analysis of AK111, an IL-17A monoclonal antibody, in subjects with moderate-to-severe plaque psoriasis
Population pharmacokinetic/pharmacodynamic analysis of AK111, an IL-17A monoclonal antibody, in subjects with moderate-to-severe plaque psoriasis Abstract AK111 is an innovative IL-17A antibody, presenting high affinity to IL-17A and showing similar pharmacokinetic (PK) characteristics to those of typical immunoglobuli...
PMC10440360
core_pubmed_pmc
Herbal concoction Unveiled: A computational analysis of phytochemicals' pharmacokinetic and toxicological profiles using novel approach methodologies (NAMs)
Herbal concoction Unveiled: A computational analysis of phytochemicals' pharmacokinetic and toxicological profiles using novel approach methodologies (NAMs) Abstract Highlights • Herbal syrups have sparked interest among traditional medicine practitioners and contemporary healthcare providers. • Limited knowledge exist...
PMC7256126
core_pubmed_pmc
A large multicentre, randomized, double‐blind, cross‐over study in healthy volunteers to compare pharmacokinetics, pharmacodynamics and safety of a pegfilgrastim biosimilar with its US‐ and EU‐reference biologics
A large multicentre, randomized, double‐blind, cross‐over study in healthy volunteers to compare pharmacokinetics, pharmacodynamics and safety of a pegfilgrastim biosimilar with its US‐ and EU‐reference biologics Abstract Abstract Aims Recombinant PEGylated human granulocyte colony‐stimulating factor (pegfilgrastim) is...
PMC8367884
core_pubmed_pmc
A randomized, single-dose, pharmacokinetic equivalence study comparing MB02 (proposed biosimilar) and reference bevacizumab in healthy Japanese male volunteers
A randomized, single-dose, pharmacokinetic equivalence study comparing MB02 (proposed biosimilar) and reference bevacizumab in healthy Japanese male volunteers Abstract Purpose MB02 is a biosimilar to bevacizumab that has demonstrated similar physicochemical and functional properties in in vitro studies to the referenc...
PMC8449641
core_pubmed_pmc
Modeling and Simulation for Individualized Therapy of Amisulpride in Chinese Patients with Schizophrenia: Focus on Interindividual Variability, Therapeutic Reference Range and the Laboratory Alert Level
Modeling and Simulation for Individualized Therapy of Amisulpride in Chinese Patients with Schizophrenia: Focus on Interindividual Variability, Therapeutic Reference Range and the Laboratory Alert Level Abstract Abstract Purpose To explain the high inter-individual variability (IIV) and the frequency of exceeding the t...
PMC12886820
core_pubmed_pmc
Bioequivalence assessment between two formulations of a film-coated fixed-dose combination of metformin and vildagliptin (850/50mg) in healthy Tunisian subjects under fed conditions
Bioequivalence assessment between two formulations of a film-coated fixed-dose combination of metformin and vildagliptin (850/50mg) in healthy Tunisian subjects under fed conditions Abstract Abstract In Tunisia, bioequivalence studies have been required for generic drug approval since 2008. This study aimed to assess t...
PMC8245857
core_pubmed_pmc
A comprehensive review of integrative pharmacology-based investigation: A paradigm shift in traditional Chinese medicine
A comprehensive review of integrative pharmacology-based investigation: A paradigm shift in traditional Chinese medicine Abstract Abstract Over the past decade, traditional Chinese medicine (TCM) has widely embraced systems biology and its various data integration approaches to promote its modernization. Thus, integrat...
PMC11666613
core_pubmed_pmc
Acute kidney injury is associated with abnormal cefepime exposure among critically ill children and young adults
Acute kidney injury is associated with abnormal cefepime exposure among critically ill children and young adults Abstract Background Elevated cefepime blood concentrations can cause neurotoxicity in adults. The consequences of elevated cefepime concentrations among pediatric patients are unknown. Future exploration of ...
PMC10975284
core_pubmed_pmc
Hyperlipidemia Increases Nalbuphine Brain Accumulation with Multiple Dosing without Affecting Its Analgesic Response—Its Respiratory Depression Potential Should Be Investigated in Future Studies
Hyperlipidemia Increases Nalbuphine Brain Accumulation with Multiple Dosing without Affecting Its Analgesic Response—Its Respiratory Depression Potential Should Be Investigated in Future Studies Abstract Abstract Nalbuphine is associated with a significant risk of respiratory depression. Its central nervous system entr...
PMC11291776
core_pubmed_pmc
The development of 177 Lu-DOTA-CC-PSMA following a unified “Click Chemistry” protocol of synthesizing metal nuclide-conjugated radiopharmaceuticals
The development of 177 Lu-DOTA-CC-PSMA following a unified “Click Chemistry” protocol of synthesizing metal nuclide-conjugated radiopharmaceuticals Abstract Abstract Background Currently, the synthesis pathway of metal nuclide-labeled radiopharmaceuticals is mainly divided into two steps: first, connecting the chelator...
PMC12588057
core_pubmed_pmc
Association of CYP2B6 and OPRM1 Genotypes with Methadone Dose Requirements and Serum Concentrations in a Vietnamese Cohorts
Association of CYP2B6 and OPRM1 Genotypes with Methadone Dose Requirements and Serum Concentrations in a Vietnamese Cohorts Abstract Abstract To characterize the prevalence of CYP2B6 and OPRM1 gene polymorphisms and evaluate their associations with serum methadone concentrations and dose requirements in Vietnamese pati...
PMC5555446
core_pubmed_pmc
Evaluation of the Potential for Drug Interactions With Patiromer in Healthy Volunteers
Evaluation of the Potential for Drug Interactions With Patiromer in Healthy Volunteers Abstract Introduction: Patiromer is a potassium-binding polymer that is not systemically absorbed; however, it may bind coadministered oral drugs in the gastrointestinal tract, potentially reducing their absorption. Methods: Twelve r...
PMC12916242
core_pubmed_pmc
Glycoprotein Non‐Metastatic Melanoma Protein B (GPNMB): A Translational Pharmacodynamic Biomarker for PIKfyve Inhibition With VRG50635
Glycoprotein Non‐Metastatic Melanoma Protein B (GPNMB): A Translational Pharmacodynamic Biomarker for PIKfyve Inhibition With VRG50635 Abstract ABSTRACT Glycoprotein non‐metastatic melanoma protein B (GPNMB) was investigated as a pharmacodynamic (PD) biomarker for PIKfyve inhibition across translational studies ex vivo...
PMC9333035
core_pubmed_pmc
Real-life comparison of three intravitreal antibiotic drug regimens in endophthalmitis
Real-life comparison of three intravitreal antibiotic drug regimens in endophthalmitis Abstract Abstract Purpose: Real-life comparison of three intravitreal drug regimens used in cases of endophthalmitis at a tertiary care center in India. Methods: In this prospective, comparative study, patients of bacterial endophtha...
PMC12119792
core_pubmed_pmc
Metabolomic reprogramming of the tumor microenvironment by dual arginase inhibitor OATD-02 boosts anticancer immunity
Metabolomic reprogramming of the tumor microenvironment by dual arginase inhibitor OATD-02 boosts anticancer immunity Abstract Abstract Metabolic reprogramming within the tumor microenvironment (TME) plays a central role in cancer progression and immune evasion, with L-arginine metabolism emerging as a key regulatory a...
PMC3831268
core_pubmed_pmc
Current Advances in Mathematical Modeling of Anti-Cancer Drug Penetration into Tumor Tissues
Current Advances in Mathematical Modeling of Anti-Cancer Drug Penetration into Tumor Tissues Abstract Abstract Delivery of anti-cancer drugs to tumor tissues, including their interstitial transport and cellular uptake, is a complex process involving various biochemical, mechanical, and biophysical factors. Mathematical...
PMC6422941
core_pubmed_pmc
Microdialysis Determination of Cefquinome Pharmacokinetics in Murine Thigh From Healthy, Neutropenic, and Actinobacillus pleuropneumoniae- Infected Mice
Microdialysis Determination of Cefquinome Pharmacokinetics in Murine Thigh From Healthy, Neutropenic, and Actinobacillus pleuropneumoniae- Infected Mice Abstract This study was aimed at applying microdialysis to explore cefquinome pharmacokinetics in thigh and plasma of healthy, neutropenic, and Actinobacillus pleuropn...
PMC11303223
core_pubmed_pmc
Role of ursolic acid in preventing gastrointestinal cancer: recent trends and future perspectives
Role of ursolic acid in preventing gastrointestinal cancer: recent trends and future perspectives Abstract Gastrointestinal malignancies are one of the major worldwide health concerns. In the present review, we have assessed the plausible therapeutic implication of Ursolic Acid (UA) against gastrointestinal cancer. By ...
PMC4639751
core_pubmed_pmc
Development of 1- N - 11 C-Methyl- l - and - d -Tryptophan for pharmacokinetic imaging of the immune checkpoint inhibitor 1-Methyl-Tryptophan
Development of 1- N - 11 C-Methyl- l - and - d -Tryptophan for pharmacokinetic imaging of the immune checkpoint inhibitor 1-Methyl-Tryptophan Abstract Abstract 1-Methyl-tryptophan (1MTrp) is known as a specific inhibitor targeting the immune- checkpoint protein indoleamine-2,3-dioxygenase, in two stereoisomers of levor...
PMC12959111
core_pubmed_pmc
Ceftazidime/avibactam and aztreonam combined with an aminoglycoside combat metallo-β-lactamase-producing Klebsiella pneumoniae
Ceftazidime/avibactam and aztreonam combined with an aminoglycoside combat metallo-β-lactamase-producing Klebsiella pneumoniae Abstract ABSTRACT There is an urgent need for additional therapeutic solutions to treat serious bacterial infections caused by metallo-β-lactamase (MBL)-producing Klebsiella pneumoniae . Aztreo...
PMC5593169
core_pubmed_pmc
Leveraging a Clinical Phase Ib Proof‐of‐Concept Study for the GPR40 Agonist MK‐8666 in Patients With Type 2 Diabetes for Model‐Informed Phase II Dose Selection
Leveraging a Clinical Phase Ib Proof‐of‐Concept Study for the GPR40 Agonist MK‐8666 in Patients With Type 2 Diabetes for Model‐Informed Phase II Dose Selection Abstract Abstract GPR40 mediates free fatty acid–induced insulin secretion in beta cells. We investigated the safety, pharmacokinetics, and glucose response of ...
PMC8831370
core_pubmed_pmc
Modelling Shows the Negative Impact of Age Dependent Pharmacokinetics on the Efficacy of Oxytetracycline in Young Steers
Modelling Shows the Negative Impact of Age Dependent Pharmacokinetics on the Efficacy of Oxytetracycline in Young Steers Abstract Abstract The effect of age dependent pharmacokinetics (PK) on the clinical efficacy of oxytetracycline (OTC) against Bovine Respiratory Disease (BRD) in beef cattle was studied, using a Phys...
PMC11728498
core_pubmed_pmc
In Vitro Evaluation, Chemical Profiling, and In Silico ADMET Prediction of the Pharmacological Activities of Artemisia absinthium Root Extract
In Vitro Evaluation, Chemical Profiling, and In Silico ADMET Prediction of the Pharmacological Activities of Artemisia absinthium Root Extract Abstract Artemisia absinthium L., is a plant with established pharmacological properties, but the A. absinthium root extract (AARE) remains unexplored. The aim of this study was...
PMC11150716
core_pubmed_pmc
Sertraline, citalopram and paroxetine in lactation: passage into breastmilk and infant exposure
Sertraline, citalopram and paroxetine in lactation: passage into breastmilk and infant exposure Abstract Objectives This study aimed to investigate the plasma and breastmilk concentrations for sertraline, citalopram and paroxetine for assessment of the Milk/Plasma (M/P) ratio and Absolute Infant Dose (AID), and to dete...
PMC11646944
core_pubmed_pmc
Quantitative systems toxicology modeling in pharmaceutical research and development: An industry‐wide survey and selected case study examples
Quantitative systems toxicology modeling in pharmaceutical research and development: An industry‐wide survey and selected case study examples Abstract Abstract Quantitative systems toxicology (QST) models are increasingly being applied for predicting and understanding toxicity liabilities in pharmaceutical research and...
PMC11194834
core_pubmed_pmc
Teaching an old drug new tricks: Regulatory insights for the repurposing of hemin in cardiovascular disease
Teaching an old drug new tricks: Regulatory insights for the repurposing of hemin in cardiovascular disease Abstract Abstract Drug repurposing has gained significant interest in recent years due to the high costs associated with de novo drug development; however, comprehensive pharmacological information is needed for ...
PMC7032087
core_pubmed_pmc
The effect of cephalexin in influencing the pharmacokinetics of a novel drug – 5′-valyl-cytarabine hydrochloride
The effect of cephalexin in influencing the pharmacokinetics of a novel drug – 5′-valyl-cytarabine hydrochloride Abstract The aim of this study is to investigate the pharmacokinetics of 5′-valyl-cytarabine hydrochloride (OPC) when co-administered with cephalexin, which are both the substrates of PepT1. The drugs were a...
PMC8879428
core_pubmed_pmc
The Potential Application of Extracellular Vesicles from Liquid Biopsies for Determination of Pharmacogene Expression
The Potential Application of Extracellular Vesicles from Liquid Biopsies for Determination of Pharmacogene Expression Abstract Pharmacogenomics (PGx) entails the study of heritability of drug response. This may include both variability in genes related to pharmacokinetics (drug absorption, distribution, metabolism and ...
PMC12075688
core_pubmed_pmc
GDF8 and activin A are the key negative regulators of muscle mass in postmenopausal females: a randomized phase I trial
GDF8 and activin A are the key negative regulators of muscle mass in postmenopausal females: a randomized phase I trial Abstract Abstract Evolutionary pressures to protect against food scarcity likely resulted in highly-conserved pathways designed to minimize energy expenditure, one of which involves the minimization o...
PMC10800819
core_pubmed_pmc
Randomized controlled trial on healthy volunteers of pharmacokinetic and antimicrobial activity of a novel hydrogel-containing chlorhexidine dressing to prevent catheter-related bloodstream infection
Randomized controlled trial on healthy volunteers of pharmacokinetic and antimicrobial activity of a novel hydrogel-containing chlorhexidine dressing to prevent catheter-related bloodstream infection Abstract Introduction Catheter-related blood stream infection (CRBSI) is one of the most relevant complications associat...
PMC12337022
core_pubmed_pmc
Randomized, Double-Blind, Crossover Study Comparing the Bioavailability of 4 Ashwagandha ( Withania somnifera (L.) Dunal) Extracts in Healthy Adults Under Fasting Condition
Randomized, Double-Blind, Crossover Study Comparing the Bioavailability of 4 Ashwagandha ( Withania somnifera (L.) Dunal) Extracts in Healthy Adults Under Fasting Condition Abstract Abstract Background Withania somnifera (L.) Dunal, commonly known as ashwagandha, is a well-known plant in ayurvedic medicine, widely valu...
PMC12641781
core_pubmed_pmc
Insights into Hepatic, Neuronal, and hERG Channel Safety of Plant-Derived Active Compounds
Insights into Hepatic, Neuronal, and hERG Channel Safety of Plant-Derived Active Compounds Abstract Abstract Curcumin (CUR), atractylodin (ATD), α-mangostin (αMG), ethyl-p-methoxycinnamate (EPMC), ligustilide (LIG), and β-eudesmol (BEU) are commonly used in Thai traditional medicine formulations. This study evaluated t...
PMC5402955
core_pubmed_pmc
Respiratory syncytial virus-neutralizing serum antibody titers in infants following palivizumab prophylaxis with an abbreviated dosing regimen
Respiratory syncytial virus-neutralizing serum antibody titers in infants following palivizumab prophylaxis with an abbreviated dosing regimen Abstract Background Monthly injections of palivizumab during the respiratory syncytial virus (RSV) season in at-risk infants reduces RSV-associated hospitalizations. However, th...
PMC2875720
core_pubmed_pmc
Role of triple fixed combination valsartan, amlodipine and hydrochlorothiazide in controlling blood pressure
Role of triple fixed combination valsartan, amlodipine and hydrochlorothiazide in controlling blood pressure Abstract Abstract Hypertension is one of the main risk factors for the development of cardiovascular diseases and the search for new therapeutic strategies aimed at optimizing its control remains an ongoing rese...
PMC3139423
core_pubmed_pmc
Experimental Adjustment on Drug Interactions through Intestinal CYP3A Activity in Rat: Impacts of Kampo Medicines Repeat Administered
Experimental Adjustment on Drug Interactions through Intestinal CYP3A Activity in Rat: Impacts of Kampo Medicines Repeat Administered Abstract Abstract To provide the information that is necessary for making the proper use of kampo medicines, we have proposed the adequate methodology focused on the following issues: (i...
PMC8402437
core_pubmed_pmc
Biopharmaceutics 4.0, Advanced Pre-Clinical Development of mRNA-Encoded Monoclonal Antibodies to Immunosuppressed Murine Models
Biopharmaceutics 4.0, Advanced Pre-Clinical Development of mRNA-Encoded Monoclonal Antibodies to Immunosuppressed Murine Models Abstract Abstract Administration of mRNA against SARS-CoV-2 has demonstrated sufficient efficacy, tolerability and clinical potential to disrupt the vaccination field. A multiple-arm, cohort r...
PMC9148397
core_pubmed_pmc
Preparation, characterization, and biodistribution of glutathione PEGylated nanoliposomal doxorubicin for brain drug delivery with a post-insertion approach
Preparation, characterization, and biodistribution of glutathione PEGylated nanoliposomal doxorubicin for brain drug delivery with a post-insertion approach Abstract Objective(s): Brain cancer treatments have mainly failed due to their inability to cross the blood-brain barrier. Several studies have confirmed the prese...
PMC12963251
core_pubmed_pmc
Penicillin Concentrations in Oropharyngeal and Frontal Sinus Tissue Following Intravenous Bolus and Continuous Infusion - An Experimental Porcine Study
Penicillin Concentrations in Oropharyngeal and Frontal Sinus Tissue Following Intravenous Bolus and Continuous Infusion - An Experimental Porcine Study Abstract Abstract Background and Purpose Studies have documented that continuous infusion is superior to bolus infusion in providing longer time with drug concentration...
PMC12564157
core_pubmed_pmc
Structural and Pharmacological Insights into Propranolol: An Integrated Crystallographic Perspective
Structural and Pharmacological Insights into Propranolol: An Integrated Crystallographic Perspective Abstract Propranolol is a non-selective β-adrenergic receptor antagonist widely used in cardiovascular and neurological therapy. Its naphthalene-based structure contributes to its high lipophilicityand central nervous s...
PMC12796535
core_pubmed_pmc
Dual FLT3/PIM inhibitor dapolsertib in acute myeloid leukemia: results from the phase 1/2 DIAMOND-01 trial
Dual FLT3/PIM inhibitor dapolsertib in acute myeloid leukemia: results from the phase 1/2 DIAMOND-01 trial Abstract Key Points • Dapolsertib (MEN1703) is a dual kinase inhibitor of proviral integration site for PIM and FLT3 kinases. • Dapolsertib has a manageable safety profile and activity in a phase 1/2 study in pati...
PMC12361636
core_pubmed_pmc
First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7 ‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity
First‐In‐Human Study of Safety, Tolerability, Efficacy, and Pharmacokinetics of CPNE7 ‐Derived Peptide (Selcopintide) for Dentin Hypersensitivity Abstract ABSTRACT Dentin hypersensitivity is characterized by transient, sharp pain resulting from dentin exposure due to enamel or cementum loss. Current treatments, which p...
PMC11394851
core_pubmed_pmc
Spectral Characteristics, In Silico Perspectives, Density Functional Theory (DFT), and Therapeutic Potential of Green-Extracted Phycocyanin from Spirulina
Spectral Characteristics, In Silico Perspectives, Density Functional Theory (DFT), and Therapeutic Potential of Green-Extracted Phycocyanin from Spirulina Abstract Abstract Phycocyanin (PC) is a naturally occurring green pigment in Spirulina. It was extracted by ultrasonic extraction using green technology, and its str...
PMC7993260
core_pubmed_pmc
Impact of Green Tea Catechin Ingestion on the Pharmacokinetics of Lisinopril in Healthy Volunteers
Impact of Green Tea Catechin Ingestion on the Pharmacokinetics of Lisinopril in Healthy Volunteers Abstract Abstract Lisinopril, a highly hydrophilic long‐acting angiotensin‐converting enzyme inhibitor, is frequently prescribed for the treatment of hypertension and congestive heart failure. Green tea consumption may re...
PMC5066862
core_pubmed_pmc
Bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers
Bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers Abstract Abstract Background Dronabinol, a pharmaceutical Δ-9-tetrahydrocannabinol, was originally developed as an oral capsule. This study evaluated the bioavailability of a new formulation, dronabinol oral solution, ver...
PMC9137619
core_pubmed_pmc
Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol Abstract Trans -resveratrol, a polyphenolic phytoalexin found in various plant sources, has been the focus of increasing attention in recent years because of its role in the prevention of many human diseases, and particularly beca...
PMC6835970
core_pubmed_pmc
Curcumin, Gut Microbiota, and Neuroprotection
Curcumin, Gut Microbiota, and Neuroprotection Abstract Abstract Curcumin, a nontoxic, naturally occurring polyphenol, has been recently proposed for the management of neurodegenerative and neurological diseases. However, a discrepancy exists between the well-documented pharmacological activities that curcumin seems to ...
PMC9743148
core_pubmed_pmc
Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1–4 inhibitor in patients with advanced solid tumors
Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1–4 inhibitor in patients with advanced solid tumors Abstract Background: Futibatinib is an oral, irreversible, highly selective fibroblast growth factor receptor (FGFR)1–4 inhibitor with potent preclinical activity against tumors harbor...
PMC10803517
core_pubmed_pmc
Pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 tartrate, a novel G protein-biased μ-opioid receptor agonist, in healthy Chinese subjects
Pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 tartrate, a novel G protein-biased μ-opioid receptor agonist, in healthy Chinese subjects Abstract Abstract Objective: YZJ-4729 is a novel G protein-biased μ-opioid receptor agonist for the treatment of acute pain in adult patients who require ...
PMC4449878
core_pubmed_pmc
Physicochemical and Biological Characterization of a Biosimilar Trastuzumab
Physicochemical and Biological Characterization of a Biosimilar Trastuzumab Abstract According to the World Health Organization, the incidence of malignant neoplasms and endocrine, blood, and immune disorders will increase in the upcoming decades along with the demand of affordable treatments. In response to this need,...
PMC7687070
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic effects of ravulizumab and eculizumab on complement component 5 in adults with paroxysmal nocturnal haemoglobinuria: results of two phase 3 randomised, multicentre studies
Pharmacokinetic and pharmacodynamic effects of ravulizumab and eculizumab on complement component 5 in adults with paroxysmal nocturnal haemoglobinuria: results of two phase 3 randomised, multicentre studies Abstract Abstract Ravulizumab, a novel long‐acting complement component 5 (C5) inhibitor administered every 8 we...
PMC11433732
core_pubmed_pmc
Disposition of Oral Nalbuphine and Its Metabolites in Healthy Subjects and Subjects with Hepatic Impairment: Preliminary Modeling Results Using a Continuous Intestinal Absorption Model with Enterohepatic Recirculation
Disposition of Oral Nalbuphine and Its Metabolites in Healthy Subjects and Subjects with Hepatic Impairment: Preliminary Modeling Results Using a Continuous Intestinal Absorption Model with Enterohepatic Recirculation Abstract Abstract Nalbuphine (NAL) is a mixed κ-agonist/μ-antagonist opioid with extensive first-pass ...
PMC9844344
core_pubmed_pmc
Vancomycin Flight Simulator: A Team-Based Learning Exercise
Vancomycin Flight Simulator: A Team-Based Learning Exercise Abstract BACKGROUND: Team-based learning (TBL) encourages learners to think critically to solve problems they will face in practice. Pharmacokinetic dosing and monitoring are complex skills requiring the application of learned knowledge. The study sought to as...
PMC11032463
core_pubmed_pmc
Theoretical considerations and empirical predictions of the pharmaco- and population dynamics of heteroresistance
Theoretical considerations and empirical predictions of the pharmaco- and population dynamics of heteroresistance Abstract Significance This mathematical modeling and computer-simulation study quantitatively explores two broadly different, previously undescribed, classes of heteroresistance. In our analysis of the prop...
PMC6994552
core_pubmed_pmc
Investigating Stochastic Differential Equations Modelling for Levodopa Infusion in Patients with Parkinson’s Disease
Investigating Stochastic Differential Equations Modelling for Levodopa Infusion in Patients with Parkinson’s Disease Abstract Background and Objectives Levodopa concentration in patients with Parkinson’s disease is frequently modelled with ordinary differential equations (ODEs). Here, we investigate a pharmacokinetic m...
PMC10915720
core_pubmed_pmc
Population pharmacokinetics, enzyme occupancy, and pharmacodynamic modeling of soticlestat in patients with developmental and epileptic encephalopathies
Population pharmacokinetics, enzyme occupancy, and pharmacodynamic modeling of soticlestat in patients with developmental and epileptic encephalopathies Abstract Abstract Soticlestat (TAK‐935) is a first‐in‐class, selective inhibitor of cholesterol 24‐hydroxylase (CH24H) under phase III development for the treatment of...
PMC8742638
core_pubmed_pmc
A microdosing framework for absolute bioavailability assessment of poorly soluble drugs: A case study on cold‐labeled venetoclax, from chemistry to the clinic
A microdosing framework for absolute bioavailability assessment of poorly soluble drugs: A case study on cold‐labeled venetoclax, from chemistry to the clinic Abstract Abstract This work presents an end‐to‐end approach for assessing the absolute bioavailability of highly hydrophobic, poorly water‐soluble compounds that...
PMC4076857
core_pubmed_pmc
Chronopharmacokinetics of drugs in toxicological aspects: A short review for pharmacy practitioners
Chronopharmacokinetics of drugs in toxicological aspects: A short review for pharmacy practitioners Abstract Abstract A rough 24-hour cycle driven endogenously in biochemical, physiological or behavioral processes is called circadian rhythm. Chronobiology is the study of biological temporal rhythms. For decades, we kno...
PMC8404633
core_pubmed_pmc
Prediction of potential drug interactions between repurposed COVID-19 and antitubercular drugs: an integrational approach of drug information software and computational techniques data
Prediction of potential drug interactions between repurposed COVID-19 and antitubercular drugs: an integrational approach of drug information software and computational techniques data Abstract Introduction: Tuberculosis is a major respiratory disease globally with a higher prevalence in Asian and African countries tha...
PMC4749816
core_pubmed_pmc
Circulating Carbonic Anhydrase IX and Antiangiogenic Therapy in Breast Cancer
Circulating Carbonic Anhydrase IX and Antiangiogenic Therapy in Breast Cancer Abstract Abstract Introduction . Carbonic anhydrase IX (CAIX) is a hypoxia regulated metalloenzyme integral to maintaining cellular pH. Increased CAIX expression is associated with poor prognosis in breast cancer. To explore CAIX as a biomark...
PMC6234689
core_pubmed_pmc
Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril Abstract Abstract Background and objectives The study investigated the intravitreal safety and vitreous disposition of lisinopril, an angiotensin converting enzyme inhibitor in rabbits for its projected use in retin...
PMC12314194
core_pubmed_pmc
A machine learning approach to population pharmacokinetic modelling automation
A machine learning approach to population pharmacokinetic modelling automation Abstract Abstract Background Population pharmacokinetic (PopPK) models are crucial for understanding drug behaviour across populations, yet traditional development is often labour-intensive and slow. This study demonstrates an automated, out...
PMC10485568
core_pubmed_pmc
Safety and pharmacodynamics of a single infusion of danavorexton in adults with idiopathic hypersomnia
Safety and pharmacodynamics of a single infusion of danavorexton in adults with idiopathic hypersomnia Abstract Abstract Study Objectives Idiopathic hypersomnia (IH) is a chronic disorder characterized by excessive daytime sleepiness unexplained by another disorder or drug/medication use. Although the orexin system pla...
PMC11001372
core_pubmed_pmc
Pharmacokinetic analysis of ceftazidime and cefazolin in the treatment of continuous ambulatory peritoneal dialysis-related peritonitis
Pharmacokinetic analysis of ceftazidime and cefazolin in the treatment of continuous ambulatory peritoneal dialysis-related peritonitis Abstract Abstract Objective Peritoneal dialysis-related peritonitis (PDRP) presents a significant challenge for nephrologists. Continuous intraperitoneal cefazolin and ceftazidime are ...
PMC12692349
core_pubmed_pmc
Coprogen B from Talaromyces marneffei ΔsreA : Rapid Iron Chelation and Favorable Partitioning to Deferoxamine
Coprogen B from Talaromyces marneffei ΔsreA : Rapid Iron Chelation and Favorable Partitioning to Deferoxamine Abstract Abstract Iron (Fe) chelators are used to treat iron-overloaded disorders, metal detoxification, radionuclides, and molecular imaging; however, they can cause side effects. In this study, we identified ...
PMC8518425
core_pubmed_pmc
Malaria PK/PD and the Role Pharmacometrics Can Play in the Global Health Arena: Malaria Treatment Regimens for Vulnerable Populations
Malaria PK/PD and the Role Pharmacometrics Can Play in the Global Health Arena: Malaria Treatment Regimens for Vulnerable Populations Abstract Abstract Malaria is an infectious disease which disproportionately effects children and pregnant women. These vulnerable populations are often excluded from clinical trials resu...
PMC11522197
core_pubmed_pmc
Selecting the Best Pharmacokinetic Models for a Priori Model-Informed Precision Dosing with Model Ensembling
Selecting the Best Pharmacokinetic Models for a Priori Model-Informed Precision Dosing with Model Ensembling Abstract Abstract Background and Objective When utilizing population pharmacokinetic (popPK) models for a priori dosage individualization, selecting the best model is crucial to obtain adequate doses. We develop...
PMC10655782
core_pubmed_pmc
SHIP1 therapeutic target enablement: Identification and evaluation of inhibitors for the treatment of late‐onset Alzheimer's disease
SHIP1 therapeutic target enablement: Identification and evaluation of inhibitors for the treatment of late‐onset Alzheimer's disease Abstract Abstract INTRODUCTION The risk of developing Alzheimer's disease is associated with genes involved in microglial function. Inositol polyphosphate‐5‐phosphatase ( INPP5D ), which ...
PMC5915608
core_pubmed_pmc
Modeling Composite Assessment Data Using Item Response Theory
Modeling Composite Assessment Data Using Item Response Theory Abstract Abstract Composite assessments aim to combine different aspects of a disease in a single score and are utilized in a variety of therapeutic areas. The data arising from these evaluations are inherently discrete with distinct statistical properties. ...
PMC9881082
core_pubmed_pmc
How to Optimize the Effectiveness and Safety of Parkinson’s Disease Therapy? – A Systematic Review of Drugs Interactions with Food and Dietary Supplements
How to Optimize the Effectiveness and Safety of Parkinson’s Disease Therapy? – A Systematic Review of Drugs Interactions with Food and Dietary Supplements Abstract Abstract Background : Despite increasing worldwide incidence of Parkinson’s disease, the therapy is still suboptimal due to the diversified clinical manifes...
PMC12376451
core_pubmed_pmc
Pulmonary and neurobehavioral efficacies of AVR-48, a TLR4 modulator, in a preterm lamb model of bronchopulmonary dysplasia
Pulmonary and neurobehavioral efficacies of AVR-48, a TLR4 modulator, in a preterm lamb model of bronchopulmonary dysplasia Abstract Background AVR-48 is a small molecule that modulates toll-like receptor 4 (TLR4) activity, changing macrophage phenotype from pro- to anti-inflammatory and increasing the anti-inflammator...
PMC6349788
core_pubmed_pmc
A pharmacokinetic study of radiprodil oral suspension in healthy adults comparing conventional venous blood sampling with two microsampling techniques
A pharmacokinetic study of radiprodil oral suspension in healthy adults comparing conventional venous blood sampling with two microsampling techniques Abstract Abstract In this phase I, single‐center, open‐label study of ten heathy adults (18‐45 years; NCT02647697), the PK, safety, and tolerability profile of radiprodi...
PMC12104636
core_pubmed_pmc
Phase 1b/2 study of ADG106, a 4-1BB/CD137 agonist, in combination with toripalimab in patients with advanced solid tumors
Phase 1b/2 study of ADG106, a 4-1BB/CD137 agonist, in combination with toripalimab in patients with advanced solid tumors Abstract Summary This phase 1b/2 clinical trial ( NCT04775680 ) evaluated the safety, efficacy, pharmacokinetics and pharmacodynamics of ADG106, a ligand-blocking agonistic antibody targeting CD137 ...
PMC11128198
core_pubmed_pmc
Phase 1 trial evaluating safety and pharmacokinetics of HIV-1 broadly neutralizing mAbs 10E8VLS and VRC07-523LS
Phase 1 trial evaluating safety and pharmacokinetics of HIV-1 broadly neutralizing mAbs 10E8VLS and VRC07-523LS Abstract BACKGROUND Broadly neutralizing monoclonal antibodies (bNAbs) represent a promising strategy for HIV-1 immunoprophylaxis and treatment. 10E8VLS and VRC07-523LS are bNAbs that target the highly conser...
PMC9928626
core_pubmed_pmc
Phase Ib Study of Telisotuzumab Vedotin in Combination With Erlotinib in Patients With c-Met Protein–Expressing Non–Small-Cell Lung Cancer
Phase Ib Study of Telisotuzumab Vedotin in Combination With Erlotinib in Patients With c-Met Protein–Expressing Non–Small-Cell Lung Cancer Abstract PURPOSE Overexpression of c-Met protein and epidermal growth factor receptor ( EGFR ) mutations can co-occur in non–small-cell lung cancer (NSCLC), providing strong rationa...
PMC4159312
core_pubmed_pmc
Single dose pharmacokinetic equivalence study of two gabapentin preparations in healthy subjects
Single dose pharmacokinetic equivalence study of two gabapentin preparations in healthy subjects Abstract Abstract Background The current study was conducted to find out whether two oral preparations of 300 mg gabapentin (the test and reference capsules) were bioequivalent. Subjects and methods This was a randomized, s...
PMC8833767
core_pubmed_pmc
Pharmacokinetic Profile of Doxycycline in Koala Plasma after Weekly Subcutaneous Injections for the Treatment of Chlamydiosis
Pharmacokinetic Profile of Doxycycline in Koala Plasma after Weekly Subcutaneous Injections for the Treatment of Chlamydiosis Abstract Abstract Simple Summary Doxycycline is an antimicrobial used for treating chlamydial infections in various species, including the koala. The dose and route of administration used initia...
PMC10014057
core_pubmed_pmc
Disease progression modeling of the North Star Ambulatory Assessment for Duchenne Muscular Dystrophy
Disease progression modeling of the North Star Ambulatory Assessment for Duchenne Muscular Dystrophy Abstract Abstract Duchenne muscular dystrophy (DMD) is a rare genetic disorder caused by decreased or absent dystrophin gene leading to progressive muscle degeneration and weakness in young boys. Disease progression mod...
PMC9503885
core_pubmed_pmc
Monitoring of Ex Vivo Cyclosporin a Activity in Healthy Volunteers Using T Cell Function Assays in Relation to Whole Blood and Cellular Pharmacokinetics
Monitoring of Ex Vivo Cyclosporin a Activity in Healthy Volunteers Using T Cell Function Assays in Relation to Whole Blood and Cellular Pharmacokinetics Abstract Abstract Therapeutic drug monitoring (TDM) of calcineurin inhibitors (i.e., tacrolimus and cyclosporin A) is standard of care after solid organ transplantatio...
PMC9509526
core_pubmed_pmc
Faster Insulin Aspart for Continuous Subcutaneous Insulin Infusion: Is It Worth It?
Faster Insulin Aspart for Continuous Subcutaneous Insulin Infusion: Is It Worth It? Abstract Abstract Introduction Faster insulin aspart (fASP) is the new formulation of insulin aspart (ASP) with a left-shifted pharmacokinetic profile, allowing better control of early postprandial hyperglycemia and a reduction in the r...
PMC9401544
core_pubmed_pmc
Results from Phase I Extension Study Assessing Pexidartinib Treatment in Six Cohorts with Solid Tumors including TGCT, and Abnormal CSF1 Transcripts in TGCT
Results from Phase I Extension Study Assessing Pexidartinib Treatment in Six Cohorts with Solid Tumors including TGCT, and Abnormal CSF1 Transcripts in TGCT Abstract Abstract Purpose: To assess the response to pexidartinib treatment in six cohorts of adult patients with advanced, incurable solid tumors associated with ...
PMC7670682
core_pubmed_pmc
The effect of grape seed and green tea extracts on the pharmacokinetics of imatinib and its main metabolite, N -desmethyl imatinib, in rats
The effect of grape seed and green tea extracts on the pharmacokinetics of imatinib and its main metabolite, N -desmethyl imatinib, in rats Abstract Background Imatinib is mainly metabolized by CYP3A4 and to a lesser extent by other isoenzymes, with N -desmethyl imatinib being its major equipotent metabolite. Being a C...
PMC3590652
core_pubmed_pmc
Single-nucleotide polymorphisms associated with outcome in metastatic renal cell carcinoma treated with sunitinib
Single-nucleotide polymorphisms associated with outcome in metastatic renal cell carcinoma treated with sunitinib Abstract Background: There are no validated markers that predict response in metastatic renal cell cancer (RCC) patients treated with sunitinib. We aim to study the impact of single-nucleotide polymorphisms...
PMC6496162
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Assessment of the Hepatic and Bone Marrow Toxicities of the New Trypanoside Fexinidazole
Pharmacokinetic-Pharmacodynamic Assessment of the Hepatic and Bone Marrow Toxicities of the New Trypanoside Fexinidazole Abstract Fexinidazole is a novel oral treatment for human African trypanosomiasis caused by Trypanosoma brucei gambiense ( g -HAT). Fexinidazole also has activity against T. cruzi , the causative age...
PMC9468570
core_pubmed_pmc
Model‐informed drug development for immuno‐oncology agonistic anti‐GITR antibody GWN323 : Dose selection based on MABEL and biologically active dose
Model‐informed drug development for immuno‐oncology agonistic anti‐GITR antibody GWN323 : Dose selection based on MABEL and biologically active dose Abstract Abstract GWN323, an agonistic human anti‐GITR (glucocorticoid‐induced TNFR‐related protein) IgG1 antibody, was studied clinically as an immuno‐oncology therapeuti...
PMC10239260
core_pubmed_pmc
Cannabidiol-Decorated Berberine-Loaded Microemulsions Improve IBS-D Therapy Through Ketogenic Diet-Induced Cannabidiol Receptors Overexpression
Cannabidiol-Decorated Berberine-Loaded Microemulsions Improve IBS-D Therapy Through Ketogenic Diet-Induced Cannabidiol Receptors Overexpression Abstract Abstract Background Berberine (BR) shows promise as a candidate for treating irritable bowel syndrome with diarrhea (IBS-D). However, the undesired physicochemical pro...
PMC4705292
core_pubmed_pmc
Improvement of oral availability of ginseng fruit saponins by a proliposome delivery system containing sodium deoxycholate
Improvement of oral availability of ginseng fruit saponins by a proliposome delivery system containing sodium deoxycholate Abstract Abstract Ginseng fruit saponins (GFS) extracted from the ginseng fruit are the bioactive triterpenoid saponin components. The aim of the present study was to develop a drug delivery system...
PMC10057831
core_pubmed_pmc
In Silico Study of Different Thrombolytic Agents for Fibrinolysis in Acute Ischemic Stroke
In Silico Study of Different Thrombolytic Agents for Fibrinolysis in Acute Ischemic Stroke Abstract Alteplase is the only FDA-approved drug for thrombolysis in acute ischemic stroke (AIS). Meanwhile, several thrombolytic drugs are deemed to be promising candidates to substitute alteplase. This paper evaluates the effic...
PMC11597563
core_pubmed_pmc
Amphiphilic Oligonucleotide Derivatives—Promising Tools for Therapeutics
Amphiphilic Oligonucleotide Derivatives—Promising Tools for Therapeutics Abstract Abstract Recent advances in genetics and nucleic acid chemistry have created fundamentally new tools, both for practical applications in therapy and diagnostics and for fundamental genome editing tasks. Nucleic acid-based therapeutic agen...
PMC12430303
core_pubmed_pmc
Design and Evaluation of Indole-Based Schiff Bases as α-Glucosidase Inhibitors: CNN-Enhanced Docking, MD Simulations, ADMET Profiling, and SAR Analysis
Design and Evaluation of Indole-Based Schiff Bases as α-Glucosidase Inhibitors: CNN-Enhanced Docking, MD Simulations, ADMET Profiling, and SAR Analysis Abstract Abstract Type 2 diabetes mellitus (T2DM) remains a global health challenge, prompting the development of novel α-glucosidase inhibitors (AGIs) to regulate post...
PMC8956787
core_pubmed_pmc
Enhanced pharmacokinetics and reduced bleeds in boys with hemophilia A after switching to Kovaltry from other standard half‐life factor VIII concentrates
Enhanced pharmacokinetics and reduced bleeds in boys with hemophilia A after switching to Kovaltry from other standard half‐life factor VIII concentrates Abstract Abstract Background BAY81‐8973 (Kovaltry; Bayer, Berkeley, CA, USA) was reported with enhanced pharmacokinetic (PK) profiles compared with some other standar...
PMC12025311
core_pubmed_pmc
Recent Advancements Towards the Use of Vitamin D Isoforms and the Development of Their Synthetic Analogues as New Therapeutics
Recent Advancements Towards the Use of Vitamin D Isoforms and the Development of Their Synthetic Analogues as New Therapeutics Abstract Abstract Vitamin D and its metabolites are essential in various physiological processes, including muscle strength, metabolism, antifibrotic activity, and immune regulation. Researcher...
PMC5938355
core_pubmed_pmc
Utility of a Novel Three-Dimensional and Dynamic (3DD) Cell Culture System for PK/PD Studies: Evaluation of a Triple Combination Therapy at Overcoming Anti-HER2 Treatment Resistance in Breast Cancer
Utility of a Novel Three-Dimensional and Dynamic (3DD) Cell Culture System for PK/PD Studies: Evaluation of a Triple Combination Therapy at Overcoming Anti-HER2 Treatment Resistance in Breast Cancer Abstract Abstract Background: Emergence of Human epidermal growth factor receptor 2 (HER2) therapy resistance in HER2-pos...
PMC7092464
core_pubmed_pmc
Identification of essential oils with activity against stationary phase Staphylococcus aureus
Identification of essential oils with activity against stationary phase Staphylococcus aureus Abstract Abstract Background Staphylococcus aureus is the most dominant human pathogen, responsible for a variety of chronic and severe infections. There is mounting evidence that persisters are associated with treatment failu...
PMC4007257
core_pubmed_pmc
Preparation and Characterisation of Nevirapine Oral Nanosuspensions
Preparation and Characterisation of Nevirapine Oral Nanosuspensions Abstract Abstract The objective of this study was to prepare and characterise nevirapine nanosuspensions so as to improve the dissolution rate of nevirapine. Nevirapine is a nonnucleoside reverse transcriptase inhibitor of immunodeficiency virus type-1...
PMC5563350
core_pubmed_pmc
Improved Pharmacokinetics with BAY 81-8973 Versus Antihemophilic Factor (Recombinant) Plasma/Albumin-Free Method: A Randomized Pharmacokinetic Study in Patients with Severe Hemophilia A
Improved Pharmacokinetics with BAY 81-8973 Versus Antihemophilic Factor (Recombinant) Plasma/Albumin-Free Method: A Randomized Pharmacokinetic Study in Patients with Severe Hemophilia A Abstract Abstract Background BAY 81-8973 is a full-length, unmodified, recombinant human factor VIII (FVIII) for the treatment of hemo...
PMC12406668
core_pubmed_pmc
Assessment of TB47 as a potential novel therapeutic agent: in vitro and in vivo efficacy against Mycobacterium leprae
Assessment of TB47 as a potential novel therapeutic agent: in vitro and in vivo efficacy against Mycobacterium leprae Abstract ABSTRACT Leprosy is a chronic infectious disease caused by Mycobacterium leprae and Mycobacterium lepromatosis . The treatment typically involves multidrug therapy comprising dapsone, clofazimi...
PMC7494911
core_pubmed_pmc
Translational pharmacology of an inhaled small molecule αvβ6 integrin inhibitor for idiopathic pulmonary fibrosis
Translational pharmacology of an inhaled small molecule αvβ6 integrin inhibitor for idiopathic pulmonary fibrosis Abstract Abstract The αvβ6 integrin plays a key role in the activation of transforming growth factor-β (TGFβ), a pro-fibrotic mediator that is pivotal to the development of idiopathic pulmonary fibrosis (IP...
PMC12882759
core_pubmed_pmc
Integrated Population Pharmacokinetic, Pharmacodynamic, and Safety Analyses to Inform Dosage Selection in the Clinical Development of the ATR Inhibitor Tuvusertib
Integrated Population Pharmacokinetic, Pharmacodynamic, and Safety Analyses to Inform Dosage Selection in the Clinical Development of the ATR Inhibitor Tuvusertib Abstract We present model‐informed selection of the recommended dose for expansion (RDE) of investigational oral ATR inhibitor tuvusertib, by integrating cli...
PMC6779903
core_pubmed_pmc
d-a-Tocopheryl Polyethylene Glycol 1000 Succinate and a small-molecule Survivin suppressant synergistically induce apoptosis in SKBR3 breast cancer cells
d-a-Tocopheryl Polyethylene Glycol 1000 Succinate and a small-molecule Survivin suppressant synergistically induce apoptosis in SKBR3 breast cancer cells Abstract Breast cancer is the second in mortality rate malignancy among women. Despite the many advances in breast cancer treatment, there is still a need to improve ...
PMC12795952
core_pubmed_pmc
Synthesis and Pharmacokinetics of Nanosized NH 2 ‑UiO‑66 (Zr) Metal-Organic Frameworks
Synthesis and Pharmacokinetics of Nanosized NH 2 ‑UiO‑66 (Zr) Metal-Organic Frameworks Abstract The application of porous nanomaterials in drug delivery offers a promising strategy to mitigate the adverse side effects of chemotherapy. In this study, we report the synthesis of nanosized NH 2 -UiO-66 (Zr) metal-organic f...