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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... |
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