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PMC5572409
core_pubmed_pmc
Translational Pharmacometric Evaluation of Typical Antibiotic Broad‐Spectrum Combination Therapies Against Staphylococcus Aureus Exploiting In Vitro Information
Translational Pharmacometric Evaluation of Typical Antibiotic Broad‐Spectrum Combination Therapies Against Staphylococcus Aureus Exploiting In Vitro Information Abstract Abstract Broad‐spectrum antibiotic combination therapy is frequently applied due to increasing resistance development of infective pathogens. The obje...
PMC9442045
core_pubmed_pmc
Dose-dependent reduction of lymphocyte count and heart rate after multiple administration of LC51-0255, a novel sphingosine-1-phosphate receptor 1 modulator, in healthy subjects
Dose-dependent reduction of lymphocyte count and heart rate after multiple administration of LC51-0255, a novel sphingosine-1-phosphate receptor 1 modulator, in healthy subjects Abstract Aim: Sphingosine-1-phosphate receptor mediates the egress of lymphocytes from lymphoid organs, and its inhibition results in a decrea...
PMC11430653
core_pubmed_pmc
Model-Informed Radiopharmaceutical Therapy Optimization: A Study on the Impact of PBPK Model Parameters on Physical, Biological, and Statistical Measures in 177 Lu-PSMA Therapy
Model-Informed Radiopharmaceutical Therapy Optimization: A Study on the Impact of PBPK Model Parameters on Physical, Biological, and Statistical Measures in 177 Lu-PSMA Therapy Abstract Abstract Simple Summary This study investigates the influence of various pharmacokinetic parameters on 177 Lu-PSMA therapies via physi...
PMC5447332
core_pubmed_pmc
A Phase Ib Study of the Dual PI3K/mTOR Inhibitor Dactolisib (BEZ235) Combined with Everolimus in Patients with Advanced Solid Malignancies
A Phase Ib Study of the Dual PI3K/mTOR Inhibitor Dactolisib (BEZ235) Combined with Everolimus in Patients with Advanced Solid Malignancies Abstract Background The combination of everolimus and the imidazoquinoline derivative, BEZ235 (dactolisib), a dual PI3K/mTOR inhibitor, demonstrated synergy in a preclinical model. ...
PMC11310660
core_pubmed_pmc
In silico evaluation of potential breast cancer receptor antagonists from GC-MS and HPLC identified compounds in Pleurotus ostreatus extracts †
In silico evaluation of potential breast cancer receptor antagonists from GC-MS and HPLC identified compounds in Pleurotus ostreatus extracts † Abstract Abstract Introduction : Pharmacotherapeutic targets for breast cancer include the estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor...
PMC12466427
core_pubmed_pmc
Unlocking Antimicrobial Peptides from Marine Invertebrates: A Comprehensive Review of Antimicrobial Discovery
Unlocking Antimicrobial Peptides from Marine Invertebrates: A Comprehensive Review of Antimicrobial Discovery Abstract Unlike other animals, marine invertebrates lack an adaptive immune system and instead rely on innate immunity as their first line of defense. A key component of this innate response is the production o...
PMC6700602
core_pubmed_pmc
Decreased Disposition of Anticancer Drugs Predominantly Eliminated via the Liver in Patients with Renal Failure
Decreased Disposition of Anticancer Drugs Predominantly Eliminated via the Liver in Patients with Renal Failure Abstract Background: Evidence has revealed that renal impairment can affect the systemic exposure of drugs which are predominantly eliminated via the liver. The modulation of drug-metabolizing enzymes and tra...
PMC10545503
core_pubmed_pmc
Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children
Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children Abstract Abstract Background Levofloxacin is used for treatment and prevention of rifampicin-resistant (RR)-TB in children. Recent data showed higher exposures with 100 mg dispersible compared with non-d...
PMC5572358
core_pubmed_pmc
Integrating In Vitro , Modeling, and In Vivo Approaches to Investigate Warfarin Bioequivalence
Integrating In Vitro , Modeling, and In Vivo Approaches to Investigate Warfarin Bioequivalence Abstract We demonstrate the use of modeling and simulation to investigate bioequivalence (BE) concerns raised about generic warfarin products. To test the hypothesis that the loss of isopropyl alcohol and slow dissolution in ...
PMC6218153
core_pubmed_pmc
Pharmacokinetics in Rat of P8, a Peptide Drug Candidate for the Treatment of Alzheimer’s Disease: Stability and Delivery to the Brain 1
Pharmacokinetics in Rat of P8, a Peptide Drug Candidate for the Treatment of Alzheimer’s Disease: Stability and Delivery to the Brain 1 Abstract Abstract Strategies to achieve a therapy for Alzheimer’s disease (AD) aimed at reducing the effects of amyloid-β (Aβ) have largely involved inhibiting or modifying the activit...
PMC8359378
core_pubmed_pmc
ONO‐7684 a novel oral FXIa inhibitor: Safety, tolerability, pharmacokinetics and pharmacodynamics in a first‐in‐human study
ONO‐7684 a novel oral FXIa inhibitor: Safety, tolerability, pharmacokinetics and pharmacodynamics in a first‐in‐human study Abstract Aims The objectives of this study were to investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of ONO‐7684, a novel activated fact...
PMC9482569
core_pubmed_pmc
Influence of N-acetyltransferase 2 ( NAT2 ) genotype/single nucleotide polymorphisms on clearance of isoniazid in tuberculosis patients: a systematic review of population pharmacokinetic models
Influence of N-acetyltransferase 2 ( NAT2 ) genotype/single nucleotide polymorphisms on clearance of isoniazid in tuberculosis patients: a systematic review of population pharmacokinetic models Abstract Purpose Significant pharmacokinetic variabilities have been reported for isoniazid across various populations. We aim...
PMC11843977
core_pubmed_pmc
Investigation of Antibody Pharmacokinetics in Male Reproductive System and Its Characterization Using a Translational PBPK Model
Investigation of Antibody Pharmacokinetics in Male Reproductive System and Its Characterization Using a Translational PBPK Model Abstract Abstract Objectives: To investigate the pharmacokinetics (PK) of the monoclonal antibody (mAb) in male reproductive tissues and develop a translational physiologically based pharmaco...
PMC12209996
core_pubmed_pmc
A Randomized Phase 1 Study Evaluating Pharmacokinetics, Safety, and Tolerability of a High‐Concentration, Long‐Acting Cabotegravir Formulation in Adults Without HIV
A Randomized Phase 1 Study Evaluating Pharmacokinetics, Safety, and Tolerability of a High‐Concentration, Long‐Acting Cabotegravir Formulation in Adults Without HIV Abstract Abstract Long‐acting (LA) cabotegravir 200‐mg/mL (CAB200) injections are approved for HIV‐1 prevention and as a complete LA HIV‐1 treatment regime...
PMC4932617
core_pubmed_pmc
Rapid and ultra-rapid metabolizers with CYP2C19 *17 polymorphism do not respond to standard therapy with proton pump inhibitors
Rapid and ultra-rapid metabolizers with CYP2C19 *17 polymorphism do not respond to standard therapy with proton pump inhibitors Abstract Abstract Introduction and objective Polymorphisms in genes encoding drug metabolizing enzymes may lead to varied enzyme activity and inter-individual variability in drug efficacy and/...
PMC9260901
core_pubmed_pmc
Impact of Composition and Morphology of Ketoconazole-Loaded Solid Lipid Nanoparticles on Intestinal Permeation and Gastroplus-Based Prediction Studies
Impact of Composition and Morphology of Ketoconazole-Loaded Solid Lipid Nanoparticles on Intestinal Permeation and Gastroplus-Based Prediction Studies Abstract Abstract Ketoconazole (KTZ) is a potential oral antifungal agent to control systemic and local infections. This study addresses the impact of composition (tween...
PMC11163776
core_pubmed_pmc
Clinical application of voriconazole in pediatric patients: a systematic review
Clinical application of voriconazole in pediatric patients: a systematic review Abstract Abstract The purpose of this study was to review the literature on the clinical use of voriconazole (VRC) in pediatric patients. MEDLINE, Embase, PubMed, Web of Science, and Cochrane Library were searched from January 1, 2000, to A...
PMC9160101
core_pubmed_pmc
In Vitro ADME and Preclinical Pharmacokinetics of Ulotaront, a TAAR1/5-HT 1A Receptor Agonist for the Treatment of Schizophrenia
In Vitro ADME and Preclinical Pharmacokinetics of Ulotaront, a TAAR1/5-HT 1A Receptor Agonist for the Treatment of Schizophrenia Abstract Abstract Purpose Ulotaront (SEP-363856) is a TAAR1 agonist with 5-HT 1A agonist activity currently in clinical development for the treatment of schizophrenia. The objectives of the c...
PMC8956318
core_pubmed_pmc
Predicting transdermal fentanyl delivery using physics-based simulations for tailored therapy based on the age
Predicting transdermal fentanyl delivery using physics-based simulations for tailored therapy based on the age Abstract Abstract Transdermal fentanyl patches are an effective alternative to the sustained release of oral morphine for chronic pain management. Due to the narrow therapeutic range of fentanyl, the concentra...
PMC10052077
core_pubmed_pmc
Novel Approach for the Approximation of Vitamin D 3 Pharmacokinetics from In Vivo Absorption Studies
Novel Approach for the Approximation of Vitamin D 3 Pharmacokinetics from In Vivo Absorption Studies Abstract Abstract The changing environment and modified lifestyles have meant that many vitamins and minerals are deficient in a significant portion of the human population. Therefore, supplementation is a viable nutrit...
PMC8256626
core_pubmed_pmc
An Evidence-Based Multidisciplinary Approach Focused at Creating Algorithms for Targeted Therapy of BSIs, cUTIs, and cIAIs Caused by Enterobacterales in Critically Ill Adult Patients
An Evidence-Based Multidisciplinary Approach Focused at Creating Algorithms for Targeted Therapy of BSIs, cUTIs, and cIAIs Caused by Enterobacterales in Critically Ill Adult Patients Abstract Abstract Prompt implementation of appropriate targeted antibiotic therapy represents a valuable approach in improving clinical a...
PMC7913287
core_pubmed_pmc
Antioxidant-Rich Woodfordia fruticosa Leaf Extract Alleviates Depressive-Like Behaviors and Impede Hyperglycemia
Antioxidant-Rich Woodfordia fruticosa Leaf Extract Alleviates Depressive-Like Behaviors and Impede Hyperglycemia Abstract Abstract Dhaiphul ( Woodfordia fruticosa ) is a frequently demanded plant in South-East Asian regions for its diverse medicinal values. This study was proposed to examine antioxidant, antidiabetic, ...
PMC11573875
core_pubmed_pmc
Impact of Continuous Infusion Meropenem PK/PD Target Attainment on C-Reactive Protein Dynamics in Critically Ill Patients With Documented Gram-Negative Hospital-Acquired or Ventilator-Associated Pneumonia
Impact of Continuous Infusion Meropenem PK/PD Target Attainment on C-Reactive Protein Dynamics in Critically Ill Patients With Documented Gram-Negative Hospital-Acquired or Ventilator-Associated Pneumonia Abstract Background and Objective Population pharmacokinetic/pharmacodynamic (PK/PD) modelling of antibiotics inclu...
PMC12419554
core_pubmed_pmc
From PICU to NICU: Extrapolating Meropenem Exposure From Pediatric to Neonatal Intensive Care Patients
From PICU to NICU: Extrapolating Meropenem Exposure From Pediatric to Neonatal Intensive Care Patients Abstract Abstract We previously developed a population pharmacokinetic (PopPK) model for meropenem in pediatric intensive care unit patients accounting for effect of body size, maturation, and kidney function on clear...
PMC4534804
core_pubmed_pmc
Pharmacokinetics of a multicomponent herbal preparation in healthy Chinese and African volunteers
Pharmacokinetics of a multicomponent herbal preparation in healthy Chinese and African volunteers Abstract K-601 is an herbal formulation for influenza consisting of Lonicera japonica , Isatis indigotica , Rheum palmatum , Phellodendron chinense , and Scutellaria baicalensis . In this work, we characterized the chemica...
PMC5952280
core_pubmed_pmc
Development of a vancomycin dosing approach for critically ill patients receiving hybrid hemodialysis using Monte Carlo simulation
Development of a vancomycin dosing approach for critically ill patients receiving hybrid hemodialysis using Monte Carlo simulation Abstract Objectives: Prolonged intermittent renal replacement therapy is an increasingly popular treatment for acute kidney injury in critically ill patients that runs at different flow rat...
PMC4281365
core_pubmed_pmc
Remifentanil, Fentanyl, or the Combination in Surgical Procedures in the United States: Predictors of Use in Patients with Organ Impairment or Obesity
Remifentanil, Fentanyl, or the Combination in Surgical Procedures in the United States: Predictors of Use in Patients with Organ Impairment or Obesity Abstract Abstract Introduction Remifentanil has a rapid onset and short duration of action, predictable pharmacokinetic/pharmacodynamic profile, and unlike fentanyl, doe...
PMC8361729
core_pubmed_pmc
Predictive Performance of Physiology‐Based Pharmacokinetic Dose Estimates for Pediatric Trials: Evaluation With 10 Bayer Small‐Molecule Compounds in Children
Predictive Performance of Physiology‐Based Pharmacokinetic Dose Estimates for Pediatric Trials: Evaluation With 10 Bayer Small‐Molecule Compounds in Children Abstract Abstract Development and guidance of dosing schemes in children have been supported by physiology‐based pharmacokinetic (PBPK) modeling for many years. P...
PMC8592505
core_pubmed_pmc
Scientific and regulatory evaluation of empirical pharmacometric models: An application of the risk informed credibility assessment framework
Scientific and regulatory evaluation of empirical pharmacometric models: An application of the risk informed credibility assessment framework Abstract Abstract Empirical pharmacometric models are part of practically every regulatory submission for a new drug. The use of the models often exceeds descriptory roles and th...
PMC12014410
core_pubmed_pmc
Characterizing circulating biomarkers for childhood dementia disorders: A scoping review of clinical trials
Characterizing circulating biomarkers for childhood dementia disorders: A scoping review of clinical trials Abstract Abstract Childhood dementias, a group of neurological disorders are characterised by neurocognitive decline, with physical and psychosocial impacts for individuals. With therapy available for <5 ​% of ch...
PMC6942373
core_pubmed_pmc
Malfunctioning sufentanil intrathecal pain pump: a case report
Malfunctioning sufentanil intrathecal pain pump: a case report Abstract Abstract Background Sufentanil is a potent opioid uncommonly used to manage pain and is rarely administered via an intrathecal pain pump system. Case presentation This case illustrates the use of intrathecal sufentanil in a 50-year-old Caucasian ma...
PMC7565282
core_pubmed_pmc
Challenges in Antifungal Therapy in Diabetes Mellitus
Challenges in Antifungal Therapy in Diabetes Mellitus Abstract Abstract Diabetic patients have an increased propensity to Candida sp. infections due to disease-related immunosuppression and various other physiological alterations. The incidence of candidiasis has increased in number over the years and is linked to sign...
PMC4771886
core_pubmed_pmc
Application of PK/PD Modeling in Veterinary Field: Dose Optimization and Drug Resistance Prediction
Application of PK/PD Modeling in Veterinary Field: Dose Optimization and Drug Resistance Prediction Abstract Abstract Among veterinary drugs, antibiotics are frequently used. The true mean of antibiotic treatment is to administer dose of drug that will have enough high possibility of attaining the preferred curative ef...
PMC5434881
core_pubmed_pmc
Physiologically based pharmacokinetic model for ethyl tertiary ‐butyl ether and tertiary ‐butyl alcohol in rats: Contribution of binding to α2u–globulin in male rats and high‐exposure nonlinear kinetics to toxicity and cancer outcomes
Physiologically based pharmacokinetic model for ethyl tertiary ‐butyl ether and tertiary ‐butyl alcohol in rats: Contribution of binding to α2u–globulin in male rats and high‐exposure nonlinear kinetics to toxicity and cancer outcomes Abstract Abstract In cancer bioassays, inhalation, but not drinking water exposure to...
PMC10786958
core_pubmed_pmc
Impact of Key Components of Intensified Ceftaroline Dosing on Pharmacokinetic/Pharmacodynamic Target Attainment
Impact of Key Components of Intensified Ceftaroline Dosing on Pharmacokinetic/Pharmacodynamic Target Attainment Abstract Abstract Background and Objective Ceftaroline fosamil is a β-lactam antibiotic approved as a 600 mg twice daily dose (≤1 h infusion, ‘standard dosing’) or a 600 mg thrice daily dose (2 h infusion) to...
PMC9145563
core_pubmed_pmc
Recent Advances in Translational Pharmacokinetics and Pharmacodynamics Prediction of Therapeutic Antibodies Using Modeling and Simulation
Recent Advances in Translational Pharmacokinetics and Pharmacodynamics Prediction of Therapeutic Antibodies Using Modeling and Simulation Abstract Abstract Therapeutic monoclonal antibodies (mAbs) have been a promising therapeutic approach for several diseases and a wide variety of mAbs are being evaluated in clinical ...
PMC7352719
core_pubmed_pmc
A Phase 1 Study of mTORC1/2 Inhibitor BI 860585 as a Single Agent or with Exemestane or Paclitaxel in Patients with Advanced Solid Tumors
A Phase 1 Study of mTORC1/2 Inhibitor BI 860585 as a Single Agent or with Exemestane or Paclitaxel in Patients with Advanced Solid Tumors Abstract This phase 1 trial (NCT01938846) determined the maximum tolerated dose (MTD) of the mTOR serine/threonine kinase inhibitor, BI 860585, as monotherapy and with exemestane or ...
PMC5715633
core_pubmed_pmc
Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics
Development of triptolide-nanoemulsion gels for percutaneous administration: physicochemical, transport, pharmacokinetic and pharmacodynamic characteristics Abstract Abstract Background This work aimed to provide useful information on the use of nanoemulsions for the percutaneous administration of triptolide. Lipid nan...
PMC12426918
core_pubmed_pmc
Late-Stage Serine Modification Enables Noncanonical Peptide Synthesis
Late-Stage Serine Modification Enables Noncanonical Peptide Synthesis Abstract Abstract Noncanonical amino acids play a critical role in enhancing drug efficacy, specificity, pharmacokinetics, and other key therapeutic properties. However, their incorporation into peptides or small molecules often presents significant ...
PMC10508808
core_pubmed_pmc
A Nanopore sequencing-based pharmacogenomic panel to personalize tuberculosis drug dosing
A Nanopore sequencing-based pharmacogenomic panel to personalize tuberculosis drug dosing Abstract Rationale: Standardized dosing of anti-tubercular (TB) drugs leads to variable plasma drug levels, which are associated with adverse drug reactions, delayed treatment response, and relapse. Mutations in genes affecting dr...
PMC10248928
core_pubmed_pmc
An exploration on retro-construction of plasma drug concentration-time curves from corresponding urine excretion data and single-point plasma concentrations using a simplified and idealized method
An exploration on retro-construction of plasma drug concentration-time curves from corresponding urine excretion data and single-point plasma concentrations using a simplified and idealized method Abstract Background Despite the availability of various tools of modeling and simulation, clinical pediatric pharmacokineti...
PMC11573813
core_pubmed_pmc
Phase 1 Studies of the Anti-Tau Monoclonal Antibody JNJ-63733657 in Healthy Participants and Participants with Alzheimer’s Disease
Phase 1 Studies of the Anti-Tau Monoclonal Antibody JNJ-63733657 in Healthy Participants and Participants with Alzheimer’s Disease Abstract Background JNJ-63733657 (posdinemab) is a humanized IgG1/kappa monoclonal anti-phospho tau antibody that binds with high affinity to phosphorylated amino acid 217 (pT217) in the pr...
PMC12049125
core_pubmed_pmc
Preclinical Investigations of a Novel PEGylated Long-Acting Human Growth Hormone
Preclinical Investigations of a Novel PEGylated Long-Acting Human Growth Hormone Abstract Purpose The daily administration of recombinant human growth hormone (rhGH) replacement therapies via subcutaneous (SC) injections can be burdensome for patients. Long-acting Growth hormone (GH) formulation could reduce injection ...
PMC9504927
core_pubmed_pmc
Use of Real‐World Data and Physiologically‐Based Pharmacokinetic Modeling to Characterize Enoxaparin Disposition in Children With Obesity
Use of Real‐World Data and Physiologically‐Based Pharmacokinetic Modeling to Characterize Enoxaparin Disposition in Children With Obesity Abstract Abstract Dosing guidance for children with obesity is often unknown despite the fact that nearly 20% of US children are classified as obese. Enoxaparin, a commonly prescribe...
PMC12269164
core_pubmed_pmc
Qingrehuoxue formula enhances anti-PD-1 immunotherapy in NSCLC by remodeling the tumor immune microenvironment via TREM2 signaling
Qingrehuoxue formula enhances anti-PD-1 immunotherapy in NSCLC by remodeling the tumor immune microenvironment via TREM2 signaling Abstract Objective This study evaluated the anti-cancer effect of the Qingrehuoxue Formula (QRHXF) and explored its synergistic mechanisms with anti-programmed cell death protein 1 (anti-PD...
PMC12933224
core_pubmed_pmc
Clinical assessment of mocravimod as a victim of drug–drug interactions via CYP3A4 metabolism and transporters
Clinical assessment of mocravimod as a victim of drug–drug interactions via CYP3A4 metabolism and transporters Abstract Abstract Mocravimod, a novel immunomodulator targeting sphingosine‐1‐phosphate receptor (S1PR), is being developed as a maintenance treatment for patients with acute myeloid leukemia undergoing alloge...
PMC8107873
core_pubmed_pmc
Update on the use of sildenafil in neonatal pulmonary hypertension: a narrative review of the history, current administration, and future directions
Update on the use of sildenafil in neonatal pulmonary hypertension: a narrative review of the history, current administration, and future directions Abstract Pulmonary hypertension (PH) is a life-threatening syndrome in neonates and has multiple and varied etiologies. However, few clinical studies have systematically e...
PMC12348194
core_pubmed_pmc
Aryl-Substituted Dihydro-Pyrimidines Effecting Kinesin Eg5 as Novel Approach for Cancer Treatment
Aryl-Substituted Dihydro-Pyrimidines Effecting Kinesin Eg5 as Novel Approach for Cancer Treatment Abstract Cancer is one of the most lethal diseases of this century. Unfortunately, many anticancer agents have harsh side effects or fail to work against cancer any longer due to tolerance. Dihydropyrimidinones are promisi...
PMC8957250
core_pubmed_pmc
A physiologically-based pharmacokinetic model of oseltamivir phosphate and its carboxylate metabolite for rats and humans
A physiologically-based pharmacokinetic model of oseltamivir phosphate and its carboxylate metabolite for rats and humans Abstract Oseltamivir phosphate (OP, Tamiflu®) is a widely used prodrug for the treatment of influenza viral infections. Orally administered OP is rapidly hydrolyzed by the carboxylesterases in anima...
PMC9632654
core_pubmed_pmc
Effects of amikacin, polymyxin-B, and sulbactam combination on the pharmacodynamic indices of mutant selection against multi-drug resistant Acinetobacter baumannii
Effects of amikacin, polymyxin-B, and sulbactam combination on the pharmacodynamic indices of mutant selection against multi-drug resistant Acinetobacter baumannii Abstract Amikacin and polymyxins as monotherapies are ineffective against multidrug-resistant Acinetobacter baumannii at the clinical dose. When polymyxins,...
PMC11004265
core_pubmed_pmc
Randomized, placebo‐controlled, double‐blind phase I trial of co‐administered pyronaridine and piperaquine in healthy adults of sub‐Saharan origin
Randomized, placebo‐controlled, double‐blind phase I trial of co‐administered pyronaridine and piperaquine in healthy adults of sub‐Saharan origin Abstract Abstract Drug resistance to sulfadoxine‐pyrimethamine and amodiaquine threatens the efficacy of malaria chemoprevention interventions in children and pregnant women...
PMC3364689
core_pubmed_pmc
Quantitative Property-Property Relationship for Screening-Level Prediction of Intrinsic Clearance of Volatile Organic Chemicals in Rats and Its Integration within PBPK Models to Predict Inhalation Pharmacokinetics in Humans
Quantitative Property-Property Relationship for Screening-Level Prediction of Intrinsic Clearance of Volatile Organic Chemicals in Rats and Its Integration within PBPK Models to Predict Inhalation Pharmacokinetics in Humans Abstract Abstract The objectives of this study were (i) to develop a screening-level Quantitativ...
PMC7457412
core_pubmed_pmc
Penetration of topical diclofenac into synovial tissue and fluid of osteoarthritic knees: a multicenter, randomized, placebo-controlled, pharmacokinetic study
Penetration of topical diclofenac into synovial tissue and fluid of osteoarthritic knees: a multicenter, randomized, placebo-controlled, pharmacokinetic study Abstract Abstract Background: Topical diclofenac, a nonsteroidal anti-inflammatory drug, has proven efficacy and safety in the management of osteoarthritis pain....
PMC7600685
core_pubmed_pmc
Recent Progress of Nanocarrier-Based Therapy for Solid Malignancies
Recent Progress of Nanocarrier-Based Therapy for Solid Malignancies Abstract Abstract Simple Summary Although conventional anti-cancer drugs have been the footstone in the fight against cancer, yet they are far from optimal due to issues related with indiscriminate destruction of normal cells, multidrug resistance, and...
PMC8002702
core_pubmed_pmc
Population Pharmacokinetic Modelling of Orally Administered Doxycycline to Rabbits at Different Ages
Population Pharmacokinetic Modelling of Orally Administered Doxycycline to Rabbits at Different Ages Abstract Abstract Doxycycline is a well-tolerated tetracycline antibiotic, registered for use in rabbits and administered for treatment of bacterial infections in this animal species. Nevertheless, the available pharmac...
PMC6187751
core_pubmed_pmc
Levodopa in Parkinson’s Disease: Current Status and Future Developments
Levodopa in Parkinson’s Disease: Current Status and Future Developments Abstract Abstract Background Ever since the pioneering reports in the 60s, L-3,4-Dioxyphenylalanine (levodopa) has represented the gold standard for the treatment of Parkinson’s Disease (PD). However, long-term levodopa (LD) treatment is frequently...
PMC12722385
core_pubmed_pmc
89 Zr-labeled PSMA ligands for pharmacokinetic PET imaging and dosimetry of PSMA-617 and PSMA-I&T: a preclinical evaluation and first in man
89 Zr-labeled PSMA ligands for pharmacokinetic PET imaging and dosimetry of PSMA-617 and PSMA-I&T: a preclinical evaluation and first in man Abstract Abstract Rationale Prolonged in vivo evaluation of PSMA tracers could improve tumor imaging and patient selection for 177 Lu-PSMA-617 and 177 Lu-PSMA-I&T. In this study, ...
PMC10912742
core_pubmed_pmc
New light on ω-3 polyunsaturated fatty acids and diabetes debate: a population pharmacokinetic-pharmacodynamic modelling and intake threshold study
New light on ω-3 polyunsaturated fatty acids and diabetes debate: a population pharmacokinetic-pharmacodynamic modelling and intake threshold study Abstract Objective ω-3 polyunsaturated fatty acids (PUFA) are a key modifiable factor in the intervention of type 2 diabetes, yet recommendations for dietary consumption of...
PMC7942514
core_pubmed_pmc
Evaluation of the safety and efficacy of XAV-19 in patients with COVID-19-induced moderate pneumonia: study protocol for a randomized, double-blinded, placebo-controlled phase 2 (2a and 2b) trial
Evaluation of the safety and efficacy of XAV-19 in patients with COVID-19-induced moderate pneumonia: study protocol for a randomized, double-blinded, placebo-controlled phase 2 (2a and 2b) trial Abstract Background Early inhibition of entry and replication of the severe acute respiratory syndrome coronavirus 2 (SARS-C...
PMC11771711
core_pubmed_pmc
Effect of Food on the Pharmacokinetics, Safety, and Tolerability of Budesonide Oral Suspension in Healthy Adult Participants: A Randomized Phase 1 Study
Effect of Food on the Pharmacokinetics, Safety, and Tolerability of Budesonide Oral Suspension in Healthy Adult Participants: A Randomized Phase 1 Study Abstract Abstract Budesonide oral suspension (BOS) is a swallowed corticosteroid indicated for 12‐week therapy in eosinophilic esophagitis with minimal systemic exposu...
PMC8791798
core_pubmed_pmc
A Phase 1 study of GDC ‐0134, a dual leucine zipper kinase inhibitor, in ALS
A Phase 1 study of GDC ‐0134, a dual leucine zipper kinase inhibitor, in ALS Abstract Abstract Objective Dual leucine zipper kinase (DLK), which regulates the c‐Jun N‐terminal kinase pathway involved in axon degeneration and apoptosis following neuronal injury, is a potential therapeutic target in amyotrophic lateral s...
PMC9385056
core_pubmed_pmc
Physiologically based modelling of the antiplatelet effect of aspirin: A tool to characterize drug responsiveness and inform precision dosing
Physiologically based modelling of the antiplatelet effect of aspirin: A tool to characterize drug responsiveness and inform precision dosing Abstract A computational approach involving mathematical modeling and in silico experiments was used to characterize the determinants of extent and duration of platelet cyclooxyg...
PMC9360108
core_pubmed_pmc
Population pharmacokinetic modelling of imatinib in healthy subjects receiving a single dose of 400 mg
Population pharmacokinetic modelling of imatinib in healthy subjects receiving a single dose of 400 mg Abstract Purpose Imatinib is indicated for treatment of CML, GIST, etc. The population pharmacokinetics (popPK) of imatinib in patients under long-term treatment are reported in literature. Data obtained from bioequiv...
PMC5688484
core_pubmed_pmc
Considerations for using minocycline vs doxycycline for treatment of canine heartworm disease
Considerations for using minocycline vs doxycycline for treatment of canine heartworm disease Abstract Background Doxycycline has been considered the first drug of choice for treating Wolbachia, a member of the Rickettsiaceae, which has a symbiotic relationship with filarial worms, including heartworms. Wolbachia , is ...
PMC6151713
core_pubmed_pmc
Effect of Sipjeondaebo-Tang on the Pharmacokinetics of S-1, an Anticancer Agent, in Rats Evaluated by Population Pharmacokinetic Modeling
Effect of Sipjeondaebo-Tang on the Pharmacokinetics of S-1, an Anticancer Agent, in Rats Evaluated by Population Pharmacokinetic Modeling Abstract Abstract S-1 (TS-1 ® ) is an oral fluoropyrimidine anticancer agent containing tegafur, oteracil, and gimeracil. Sipjeondaebo-tang (SDT) is a traditional oriental herbal med...
PMC12171220
core_pubmed_pmc
Finerenone in diabetic kidney disease: a new frontier for slowing disease progression
Finerenone in diabetic kidney disease: a new frontier for slowing disease progression Abstract Diabetic kidney disease (DKD) represents a substantial health burden for patients with type 2 diabetes mellitus (T2DM), markedly increasing morbidity and mortality. The cornerstone of DKD treatment remains renin-angiotensin s...
PMC8142937
core_pubmed_pmc
Pharmacokinetics of Linezolid Dose Adjustment for Creatinine Clearance in Critically Ill Patients: A Multicenter, Prospective, Open-Label, Observational Study
Pharmacokinetics of Linezolid Dose Adjustment for Creatinine Clearance in Critically Ill Patients: A Multicenter, Prospective, Open-Label, Observational Study Abstract Purpose The aim of this study is to use a population pharmacokinetic (PK) approach to evaluate the optimal dosing strategy for linezolid (LNZ) in critic...
PMC5221548
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic evaluation according to absorption differences in three formulations of ibuprofen
Pharmacokinetic and pharmacodynamic evaluation according to absorption differences in three formulations of ibuprofen Abstract Objective Prostaglandin E 2 (PGE 2 ) synthesis is modulated by COX2. Changes in PGE 2 could be used to quantify the COX2 inhibition after ibuprofen administration. This study investigated the p...
PMC5215471
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD‐6972 in healthy subjects and subjects with type 2 diabetes mellitus
Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD‐6972 in healthy subjects and subjects with type 2 diabetes mellitus Abstract Abstract Aim To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple doses of a novel, oral g...
PMC5574242
core_pubmed_pmc
A non-controlled, single arm, open label, phase II study of intravenous and intratumoral administration of ParvOryx in patients with metastatic, inoperable pancreatic cancer: ParvOryx02 protocol
A non-controlled, single arm, open label, phase II study of intravenous and intratumoral administration of ParvOryx in patients with metastatic, inoperable pancreatic cancer: ParvOryx02 protocol Abstract Abstract Background Metastatic pancreatic cancer has a dismal prognosis, with a mean six-month progression-free surv...
PMC3038594
core_pubmed_pmc
Linear low-dose extrapolation for noncancer health effects is the exception, not the rule
Linear low-dose extrapolation for noncancer health effects is the exception, not the rule Abstract Abstract The nature of the exposure-response relationship has a profound influence on risk analyses. Several arguments have been proffered as to why all exposure-response relationships for both cancer and noncarcinogenic ...
PMC7898688
core_pubmed_pmc
A single‐dose euglycaemic clamp study in two cohorts to compare the exposure of SAR341402 (insulin aspart) Mix 70/30 with US ‐ and European‐ approved versions of insulin aspart Mix 70/30 and SAR341402 rapid‐acting solution in subjects with type 1 diabetes
A single‐dose euglycaemic clamp study in two cohorts to compare the exposure of SAR341402 (insulin aspart) Mix 70/30 with US ‐ and European‐ approved versions of insulin aspart Mix 70/30 and SAR341402 rapid‐acting solution in subjects with type 1 diabetes Abstract Abstract Aim To compare the pharmacokinetic exposure of...
PMC7300403
core_pubmed_pmc
The underlying mechanisms of lorlatinib penetration across the blood ‐ brain barrier and the distribution characteristics of lorlatinib in the brain
The underlying mechanisms of lorlatinib penetration across the blood ‐ brain barrier and the distribution characteristics of lorlatinib in the brain Abstract Abstract Objective To clarify the distribution of lorlatinib in the brain and elucidate the molecular mechanisms of lorlatinib penetration across the blood‐brain ...
PMC6989237
core_pubmed_pmc
Development of a physiologically-based pharmacokinetic model for cyclosporine in Asian children with renal impairment
Development of a physiologically-based pharmacokinetic model for cyclosporine in Asian children with renal impairment Abstract Abstract This study aimed to assess the pharmacokinetics of cyclosporine A (CsA) in Asian children with renal impairment (RI) by developing a physiologically-based pharmacokinetic (PBPK) model ...
PMC9303412
core_pubmed_pmc
Pharmacokinetics and Concentration‐Response of Dupilumab in Patients With Seasonal Allergic Rhinitis
Pharmacokinetics and Concentration‐Response of Dupilumab in Patients With Seasonal Allergic Rhinitis Abstract Abstract Patients with moderate to severe allergic rhinitis may benefit from subcutaneous immunotherapy (SCIT), despite the risk of systemic allergic reaction. Dupilumab is a fully human monoclonal antibody tha...
PMC5007398
core_pubmed_pmc
Assessment of Blood-Brain Barrier Permeability by Dynamic Contrast-Enhanced MRI in Transient Middle Cerebral Artery Occlusion Model after Localized Brain Cooling in Rats
Assessment of Blood-Brain Barrier Permeability by Dynamic Contrast-Enhanced MRI in Transient Middle Cerebral Artery Occlusion Model after Localized Brain Cooling in Rats Abstract Objective The purpose of this study was to evaluate the effects of localized brain cooling on blood-brain barrier (BBB) permeability followin...
PMC12143337
core_pubmed_pmc
Integrating pharmacokinetics and network pharmacology to decipher the efficacy of Fufang Qinlan oral liquid on post infectious cough
Integrating pharmacokinetics and network pharmacology to decipher the efficacy of Fufang Qinlan oral liquid on post infectious cough Abstract Abstract Background and aim Fufang Qinlan oral liquid (QLOL) is a traditional Chinese medicine formula used to treat fevers, sore throats and cough. This study was to evaluate QL...
PMC12746520
core_pubmed_pmc
Cannabidiol Lacks Direct Effect on Cortical Excitability: A Randomized, Double Blind, Placebo Controlled, 3‐Way Crossover Trial
Cannabidiol Lacks Direct Effect on Cortical Excitability: A Randomized, Double Blind, Placebo Controlled, 3‐Way Crossover Trial Abstract Cannabidiol (CBD) is approved as an adjunctive treatment of seizures associated with Dravet syndrome, Lennox–Gastaut Syndrome, and tuberous sclerosis. Its therapeutic and adverse effe...
PMC12882758
core_pubmed_pmc
Reducing the Burden of Interaction Studies in Cancer Patients Using a Stable Isotopically Labeled Microtracer: A Proof‐of‐Concept Study with Alectinib
Reducing the Burden of Interaction Studies in Cancer Patients Using a Stable Isotopically Labeled Microtracer: A Proof‐of‐Concept Study with Alectinib Abstract Abstract Traditional drug‐food interaction studies of oral anticancer agents have a high patient burden. A patient‐friendly alternative approach to studying foo...
PMC10005323
core_pubmed_pmc
Bio-Actives from Natural Products with Potential Cardioprotective Properties: Isolation, Identification, and Pharmacological Actions of Apigenin, Quercetin, and Silibinin
Bio-Actives from Natural Products with Potential Cardioprotective Properties: Isolation, Identification, and Pharmacological Actions of Apigenin, Quercetin, and Silibinin Abstract Abstract Cardiovascular diseases (CVDs) are the leading cause of morbidity and mortality worldwide. As a result, pharmaceutical and non-phar...
PMC9788704
core_pubmed_pmc
Preparation and characterization of morphine gelatine microspheres
Preparation and characterization of morphine gelatine microspheres Abstract ABSTRACT Morphine is a widely used opioid analgesic. However, standard morphine dosages and administration methods exhibit a short half-life and pose a risk of respiratory depression. Sustained-release microspheres can deliver prolonged efficac...
PMC6585620
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling for Olaparib Dosing Recommendations: Bridging Formulations, Drug Interactions, and Patient Populations
Physiologically Based Pharmacokinetic Modeling for Olaparib Dosing Recommendations: Bridging Formulations, Drug Interactions, and Patient Populations Abstract We report physiologically based pharmacokinetic‐modeling analyses to determine olaparib (tablet or capsule) drug–drug interactions (DDIs). Verified DDI simulatio...
PMC4631705
core_pubmed_pmc
Animal and human mucosal tissue models to study HIV biomedical interventions: can we predict success?
Animal and human mucosal tissue models to study HIV biomedical interventions: can we predict success? Abstract Introduction Preclinical testing plays an integral role in the development of HIV prevention modalities. Several models are used including humanized mice, non-human primates and human mucosal tissue cultures. ...
PMC12855771
core_pubmed_pmc
Comparing the pharmacokinetics of GS-441524 after intravenous and oral administration of remdesivir in New Zealand cats with feline infectious peritonitis
Comparing the pharmacokinetics of GS-441524 after intravenous and oral administration of remdesivir in New Zealand cats with feline infectious peritonitis Abstract Objectives The aim of the study was to compare the pharmacokinetics of GS-441524 after intravenous (IV) and oral administration of compounded remdesivir (RD...
PMC6853151
core_pubmed_pmc
A Modeling Framework to Characterize Cytokine Release upon T‐Cell–Engaging Bispecific Antibody Treatment: Methodology and Opportunities
A Modeling Framework to Characterize Cytokine Release upon T‐Cell–Engaging Bispecific Antibody Treatment: Methodology and Opportunities Abstract T‐cell–engaging bispecific antibodies (T‐BsAbs) are an important class of antibody therapeutics in immuno‐oncology. T‐BsAbs simultaneously bind to CD 3 on T cells and a tumor‐...
PMC7399966
core_pubmed_pmc
Influence of Renal Function and Age on the Pharmacokinetics of Levofloxacin in Patients with Bone and Joint Infections
Influence of Renal Function and Age on the Pharmacokinetics of Levofloxacin in Patients with Bone and Joint Infections Abstract Abstract Despite its efficacy and toxicity being exposure-related, levofloxacin pharmacokinetics in patients with bone and joint infections has been poorly described to date, so the possible n...
PMC11822261
core_pubmed_pmc
Emapalumab in Patients With Macrophage Activation Syndrome Associated With Still's Disease: A Population Pharmacokinetic/Pharmacodynamic Analysis
Emapalumab in Patients With Macrophage Activation Syndrome Associated With Still's Disease: A Population Pharmacokinetic/Pharmacodynamic Analysis Abstract ABSTRACT Macrophage activation syndrome (MAS) is a life‐threatening form of secondary haemophagocytic lymphohistiocytosis (HLH) associated with rheumatic diseases, m...
PMC8931505
core_pubmed_pmc
Associations of Fentanyl, Sufentanil, and Remifentanil With Length of Stay and Mortality Among Mechanically Ventilated Patients: A Registry-Based Cohort Study
Associations of Fentanyl, Sufentanil, and Remifentanil With Length of Stay and Mortality Among Mechanically Ventilated Patients: A Registry-Based Cohort Study Abstract Background: As the first-line treatment for mechanically ventilated patients with critical illness, fentanyl and its analogs (e.g., sufentanil and remif...
PMC8157038
core_pubmed_pmc
Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation
Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation Abstract The reduced therapeutic efficacy of rizatriptan in migraine treatment is primarily due to low oral bioavailability and extensive first pass metabolism. The purpose of this investigation was to optimize the thin mucoadhesiv...
PMC4213839
core_pubmed_pmc
Effect of a soluble prebiotic fiber, NUTRIOSE, on the absorption of ginsenoside Rd in rats orally administered ginseng
Effect of a soluble prebiotic fiber, NUTRIOSE, on the absorption of ginsenoside Rd in rats orally administered ginseng Abstract Abstract Background There is limited understanding of the effect of dietary components on the absorption of ginsenosides and their metabolites into the blood. Methods This study investigated t...
PMC8013748
core_pubmed_pmc
Neglecting Plasma Protein Binding in COVID‐19 Patients Leads to a Wrong Interpretation of Lopinavir Overexposure
Neglecting Plasma Protein Binding in COVID‐19 Patients Leads to a Wrong Interpretation of Lopinavir Overexposure Abstract Abstract Boffito et al . recalled the critical importance to correctly interpret protein binding. Changes of lopinavir pharmacokinetics in coronavirus disease 2019 (COVID‐19) are a perfect illustrat...
PMC4865535
core_pubmed_pmc
Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation
Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation Abstract Purpose Dolutegravir (DTG) is primarily metabolized by UGT1A1 with CYP3A as a minor route. Carbamazepine (CBZ) is a potent inducer of these enzymes; thus, the effect of oral extended-release CBZ on DTG pharmacokinetics (PK) was ...
PMC11993286
core_pubmed_pmc
Model‐Informed Selection of the Recommended Phase 2 Dosage for Anti‐TIGIT Immunotherapy Leveraging co‐Expressed PD‐1 Inhibitor Target Engagement
Model‐Informed Selection of the Recommended Phase 2 Dosage for Anti‐TIGIT Immunotherapy Leveraging co‐Expressed PD‐1 Inhibitor Target Engagement Abstract Abstract Refining dose projections requires a deep understanding of drug‐target relationships at the site of action, which is often challenging to achieve. Here we pr...
PMC11362038
core_pubmed_pmc
Alpinia officinarum Hance: a comprehensive review of traditional uses, phytochemistry, pharmacokinetic and pharmacology
Alpinia officinarum Hance: a comprehensive review of traditional uses, phytochemistry, pharmacokinetic and pharmacology Abstract The dried root and rhizome of Alpinia officinarum Hance ( A. officinarum ) have been widely used in traditional Chinese medicine for thousands of years to alleviate pain, promote digestion, w...
PMC6656473
core_pubmed_pmc
A Phase I/II Open‐Label Study of Nivolumab in Previously Treated Advanced or Recurrent Nasopharyngeal Carcinoma and Other Solid Tumors
A Phase I/II Open‐Label Study of Nivolumab in Previously Treated Advanced or Recurrent Nasopharyngeal Carcinoma and Other Solid Tumors Abstract Abstract Lessons Learned. Nivolumab treatment at doses of 3 mg/kg once every 2 weeks (Q2W), 240 mg Q2W, and 360 mg once every 3 weeks was well tolerated in the Chinese populati...
PMC12823299
core_pubmed_pmc
Tutorial on Causal Mediation Analysis for Pharmacometricians
Tutorial on Causal Mediation Analysis for Pharmacometricians Abstract ABSTRACT Mediation analyses can support biomarker development by quantifying the part of the total treatment effect on clinical outcome that is mediated by the biomarker. Given that pharmacometricians are often involved in the analysis of biomarker d...
PMC8370238
core_pubmed_pmc
Blocking Bacterial Naphthohydroquinone Oxidation and ADP-Ribosylation Improves Activity of Rifamycins against Mycobacterium abscessus
Blocking Bacterial Naphthohydroquinone Oxidation and ADP-Ribosylation Improves Activity of Rifamycins against Mycobacterium abscessus Abstract ABSTRACT Rifampicin is an effective drug for treating tuberculosis (TB) but is not used to treat Mycobacterium abscessus infections due to poor in vitro activity. While rifabuti...
PMC4580724
core_pubmed_pmc
Pharmacokinetic Drug Interaction Studies with Enzalutamide
Pharmacokinetic Drug Interaction Studies with Enzalutamide Abstract Background and Objectives Two phase I drug interaction studies were performed with oral enzalutamide, which is approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Methods A parallel-treatment design ( n = 41) was used...
PMC3137875
core_pubmed_pmc
Bioactive Markers Based Pharmacokinetic Evaluation of Extracts of a Traditional Medicinal Plant, Piper sarmentosum
Bioactive Markers Based Pharmacokinetic Evaluation of Extracts of a Traditional Medicinal Plant, Piper sarmentosum Abstract Abstract In vitro assays are economical and easy to perform but to establish relevance of their results to real clinical outcome in animals or human, pharmacokinetics is prerequisite. Despite vari...
PMC4679385
core_pubmed_pmc
Chemotherapy in Elderly Patients with Gastric Cancer
Chemotherapy in Elderly Patients with Gastric Cancer Abstract Abstract Gastric cancer (GC) is one of the most frequent malignant diseases in the elderly. Systemic chemotherapy showed an improvement of quality of life and survival benefit compared to supportive care alone in patients with advanced GC. Because comorbidit...