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PMC11602703 | core_pubmed_pmc | Enhanced anticancer effect of thymidylate synthase dimer disrupters by promoting intracellular accumulation | Enhanced anticancer effect of thymidylate synthase dimer disrupters by promoting intracellular accumulation Abstract Abstract Introduction Thymidylate synthase (TS) plays a crucial role in cellular growth, proliferation, DNA synthesis, and repair, thus gaining attention for targeted therapies in cancer. TS overexpressi... |
PMC7557213 | core_pubmed_pmc | Model-Informed Drug Discovery and Development in Pulmonary Delivery: Biopharmaceutical Pharmacometric Modeling for Formulation Evaluation of Pulmonary Suspensions | Model-Informed Drug Discovery and Development in Pulmonary Delivery: Biopharmaceutical Pharmacometric Modeling for Formulation Evaluation of Pulmonary Suspensions Abstract For respiratory conditions, targeted drug delivery to the lungs could produce higher local concentrations with reduced risk of adverse events compar... |
PMC4239983 | core_pubmed_pmc | Bridging the gap: a review of dose investigations in paediatric investigation plans | Bridging the gap: a review of dose investigations in paediatric investigation plans Abstract Abstract Aims In the EU, development of new medicines for children should follow a prospectively agreed paediatric investigation plan (PIP). Finding the right dose for children is crucial but challenging due to the variability ... |
PMC9041855 | core_pubmed_pmc | Efficacy assessment of a novel endolysin PlyAZ3a T for the treatment of ceftriaxone-resistant pneumococcal meningitis in an infant rat model | Efficacy assessment of a novel endolysin PlyAZ3a T for the treatment of ceftriaxone-resistant pneumococcal meningitis in an infant rat model Abstract Abstract Background Treatment failure in pneumococcal meningitis due to antibiotic resistance is an increasing clinical challenge and alternatives to antibiotics warrant ... |
PMC5761010 | core_pubmed_pmc | Optimization and validation of a fast RP–HPLC method for the determination of dobutamine in rat plasma: Pharmacokinetic studies in healthy rat subjects | Optimization and validation of a fast RP–HPLC method for the determination of dobutamine in rat plasma: Pharmacokinetic studies in healthy rat subjects Abstract Abstract A novel isocratic reverse phase high performance liquid chromatography (RP–HPLC) with photo diode array (PDA) detection method for the determination o... |
PMC10759924 | core_pubmed_pmc | Differential Detection of Amyloid Aggregates in Old Animals Using Gold Nanorods by Computerized Tomography: A Pharmacokinetic and Bioaccumulation Study | Differential Detection of Amyloid Aggregates in Old Animals Using Gold Nanorods by Computerized Tomography: A Pharmacokinetic and Bioaccumulation Study Abstract Introduction The development of new materials and tools for radiology is key to the implementation of this diagnostic technique in clinics. In this work, we ev... |
PMC4435036 | core_pubmed_pmc | Antihypertensive Drugs Metabolism: An Update to Pharmacokinetic Profiles and Computational Approaches | Antihypertensive Drugs Metabolism: An Update to Pharmacokinetic Profiles and Computational Approaches Abstract Drug discovery and development is a high-risk enterprise that requires significant investments in capital, time and scientific expertise. The studies of xenobiotic metabolism remain as one of the main topics i... |
PMC8640522 | core_pubmed_pmc | Estimation of Mycophenolic Acid Exposure in Heart Transplant Recipients by Population Pharmacokinetic and Limited Sampling Strategies | Estimation of Mycophenolic Acid Exposure in Heart Transplant Recipients by Population Pharmacokinetic and Limited Sampling Strategies Abstract Purpose: The aim of this study is i) to establish a strategy to estimate the area under the curve of the dosing interval (AUC 0–12h ) of mycophenolic acid (MPA) in the heart tra... |
PMC3822020 | core_pubmed_pmc | The comparison of predictive performance in bispectral index prediction during target effect-site controlled infusion of propofol using different blood effect-site equilibration rate constants in the same pharmacokinetic model | The comparison of predictive performance in bispectral index prediction during target effect-site controlled infusion of propofol using different blood effect-site equilibration rate constants in the same pharmacokinetic model Abstract Background Blood-brain equilibration rate constant ( k e0 ) is derived from either p... |
PMC8931745 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, Safety, Tolerability, and Immunogenicity of the QX002N anti-IL-17 Monoclonal Antibody: A Phase I, Randomized, Double-Blind, Single Ascending Dose Study in Healthy Chinese Volunteers | Pharmacokinetics, Pharmacodynamics, Safety, Tolerability, and Immunogenicity of the QX002N anti-IL-17 Monoclonal Antibody: A Phase I, Randomized, Double-Blind, Single Ascending Dose Study in Healthy Chinese Volunteers Abstract Background: The innovative injection of interleukin 17 A (IL-17A) monoclonal antibody QX002N ... |
PMC11771648 | core_pubmed_pmc | Pharmacokinetics and Safety of Intravenous Candidate Biosimilar CT‐P47 and Reference Tocilizumab: A Randomized, Double‐Blind, Phase 1 Study | Pharmacokinetics and Safety of Intravenous Candidate Biosimilar CT‐P47 and Reference Tocilizumab: A Randomized, Double‐Blind, Phase 1 Study Abstract Abstract CT‐P47 is a candidate biosimilar of tocilizumab. This 12‐week, randomized, double‐blind, parallel‐design, phase 1 study aimed to demonstrate pharmacokinetic (PK) ... |
PMC12706420 | core_pubmed_pmc | Optimizing Ibrutinib Posology in Chronic Lymphocytic Leukemia Using a Semi‐Mechanistic Pharmacometric Framework | Optimizing Ibrutinib Posology in Chronic Lymphocytic Leukemia Using a Semi‐Mechanistic Pharmacometric Framework Abstract ABSTRACT Ibrutinib, a Bruton's tyrosine kinase (Btk) inhibitor, is a key therapy for chronic lymphocytic leukemia (CLL). In clinical practice, adverse events, such as hypertension, frequently necessi... |
PMC3853718 | core_pubmed_pmc | A first-in-human, phase 1, dose-escalation study of dinaciclib, a novel cyclin-dependent kinase inhibitor, administered weekly in subjects with advanced malignancies | A first-in-human, phase 1, dose-escalation study of dinaciclib, a novel cyclin-dependent kinase inhibitor, administered weekly in subjects with advanced malignancies Abstract Background Dinaciclib, a small-molecule, cyclin-dependent kinase inhibitor, inhibits cell cycle progression and proliferation in various tumor ce... |
PMC5750658 | core_pubmed_pmc | A High-Performance Liquid Chromatography Assay Method for the Determination of Lidocaine in Human Serum | A High-Performance Liquid Chromatography Assay Method for the Determination of Lidocaine in Human Serum Abstract Abstract Here we report on the development of a selective and sensitive high-performance liquid chromatographic method for the determination of lidocaine in human serum. The extraction of lidocaine and proca... |
PMC11844199 | core_pubmed_pmc | Population Pharmacokinetics of Prolonged Infusion for Meropenem: Tailoring Dosing Recommendations for Chinese Critically Ill Patients on Continuous Renal Replacement Therapy with Consideration for Renal Function | Population Pharmacokinetics of Prolonged Infusion for Meropenem: Tailoring Dosing Recommendations for Chinese Critically Ill Patients on Continuous Renal Replacement Therapy with Consideration for Renal Function Abstract Abstract Objective Extended meropenem infusion is increasingly employed to enhance clinical outcome... |
PMC10812724 | core_pubmed_pmc | Translational PK/PD for the Development of Novel Antibiotics—A Drug Developer’s Perspective | Translational PK/PD for the Development of Novel Antibiotics—A Drug Developer’s Perspective Abstract Antibiotic development traditionally involved large Phase 3 programs, preceded by Phase 2 studies. Recognizing the high unmet medical need for new antibiotics and, in some cases, challenges to conducting large clinical ... |
PMC9305226 | core_pubmed_pmc | Similar Pharmacokinetics and Pharmacodynamics of Biosimilar SAR342434 Insulin Lispro and Japan‐Approved Humalog Insulin Lispro in Healthy Japanese Subjects | Similar Pharmacokinetics and Pharmacodynamics of Biosimilar SAR342434 Insulin Lispro and Japan‐Approved Humalog Insulin Lispro in Healthy Japanese Subjects Abstract Abstract This phase 1 study compared the pharmacokinetic (PK) and glucose pharmacodynamic (PD) characteristics of biosimilar SAR342434 insulin lispro and J... |
PMC8065677 | core_pubmed_pmc | A Model-Based Pharmacokinetic/Pharmacodynamic Analysis of the Combination of Amoxicillin and Monophosphoryl Lipid A Against S. pneumoniae in Mice | A Model-Based Pharmacokinetic/Pharmacodynamic Analysis of the Combination of Amoxicillin and Monophosphoryl Lipid A Against S. pneumoniae in Mice Abstract Abstract Combining amoxicillin with the immunostimulatory toll-like receptor 4 agonist monophosphoryl lipid A (MPLA) represents an innovative approach for enhancing ... |
PMC10331411 | core_pubmed_pmc | Formulation, optimization, in-vivo biodistribution studies and histopathological safety assessment of duloxetine HCl-loaded ultra-elastic nanovesicles for antidepressant effect after intranasal and transdermal delivery | Formulation, optimization, in-vivo biodistribution studies and histopathological safety assessment of duloxetine HCl-loaded ultra-elastic nanovesicles for antidepressant effect after intranasal and transdermal delivery Abstract Abstract Duloxetine hydrochloride (DUL) is a BCS class-II antidepressant drug, acting via se... |
PMC12518165 | core_pubmed_pmc | No Evidence of QTc Interval Prolongation With Baxdrostat Treatment: Concentration–QTc Modeling Assessment | No Evidence of QTc Interval Prolongation With Baxdrostat Treatment: Concentration–QTc Modeling Assessment Abstract ABSTRACT Baxdrostat is a novel, highly potent, selective, competitive inhibitor of human aldosterone synthase currently under development for the treatment of uncontrolled and resistant hypertension and ch... |
PMC5947295 | core_pubmed_pmc | Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics | Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics Abstract Abstract The relative bioavailability of lanabecestat administered as 2 tablet formulations versus an oral solution was invest... |
PMC12569559 | core_pubmed_pmc | Extrapolation of lung pharmacokinetics of bedaquiline across species using physiologically‐based pharmacokinetic modelling | Extrapolation of lung pharmacokinetics of bedaquiline across species using physiologically‐based pharmacokinetic modelling Abstract Aims Bedaquiline (BDQ) is a first‐in‐class diarylquinoline (DARQ) and a potent anti‐tuberculosis drug, vital in combating multi‐drug resistant tuberculosis (TB). Understanding its lung pha... |
PMC7993267 | core_pubmed_pmc | Digitally Enabled, Patient‐Centric Clinical Trials: Shifting the Drug Development Paradigm | Digitally Enabled, Patient‐Centric Clinical Trials: Shifting the Drug Development Paradigm Abstract The rapidly advancing field of digital health technologies provides a great opportunity to radically transform the way clinical trials are conducted and to shift the clinical trial paradigm from a site‐centric to a patie... |
PMC5997598 | core_pubmed_pmc | In Vivo Pharmacokinetics of Bromfenac Ophthalmic Solution 0.075%, Bromfenac Ophthalmic Solution 0.07%, and Nepafenac/Amfenac Ophthalmic Suspension 0.3% in Rabbits | In Vivo Pharmacokinetics of Bromfenac Ophthalmic Solution 0.075%, Bromfenac Ophthalmic Solution 0.07%, and Nepafenac/Amfenac Ophthalmic Suspension 0.3% in Rabbits Abstract Introduction Little is known of the ocular distribution characteristics of currently branded non-steroidal anti-inflammatory drugs (NSAIDs) in the U... |
PMC11146679 | core_pubmed_pmc | Machine Learning and Artificial Intelligence in PK‐PD Modeling: Fad, Friend, or Foe? | Machine Learning and Artificial Intelligence in PK‐PD Modeling: Fad, Friend, or Foe? Modeling MACHINE LEARNING AND PK AND PK ‐ PD MODEL DEVELOPMENT PK‐PD modelers leverage various AI‐based tools in their daily routine and this has without doubt contributed to increased productivity. For example, AI‐driven programming t... |
PMC12481195 | core_pubmed_pmc | Human Abuse Potential of Oral NKTR-181 in Recreational Opioid Users: A Randomized, Double-Blind, Crossover Study | Human Abuse Potential of Oral NKTR-181 in Recreational Opioid Users: A Randomized, Double-Blind, Crossover Study Abstract Abstract Objective To evaluate the human abuse potential, pharmacokinetics, pharmacodynamics, and safety of oral NKTR-181 (oxycodegol), a novel full mu-opioid receptor agonist, relative to oral oxyc... |
PMC5014080 | core_pubmed_pmc | Eltoprazine counteracts l -DOPA-induced dyskinesias in Parkinson’s disease: a dose-finding study | Eltoprazine counteracts l -DOPA-induced dyskinesias in Parkinson’s disease: a dose-finding study Abstract See Bezard and Carta for a scientific commentary on this article (doi: 10.1093/brain/awu407 ). In a double-blind placebo-controlled study, Svenningsson et al. test a single oral dose of eltoprazine—a serotonin 5-HT... |
PMC5430090 | core_pubmed_pmc | The positive clinical therapeutically effects of Escin on advanced thyroid cancer | The positive clinical therapeutically effects of Escin on advanced thyroid cancer Abstract Abstract The incidences of thyroid cancer keep rising worldwide over the past few decades. Although most thyroid cancers are indolent and highly curable, the treatment for advanced thyroid cancer remains challengeable in clinical... |
PMC12473248 | core_pubmed_pmc | Optimizing Dose Conversion from IR-Tac to LCP-Tac Formulations in Renal Transplant Recipients: A Population Pharmacokinetic Modeling Study | Optimizing Dose Conversion from IR-Tac to LCP-Tac Formulations in Renal Transplant Recipients: A Population Pharmacokinetic Modeling Study Abstract Background/Objectives : Tacrolimus dosing remains challenging due to its narrow therapeutic index and high inter- and intra-patient variability. The extended-release once-d... |
PMC5524914 | core_pubmed_pmc | Physiologically-based modelling in mice suggests an aggravated loss of clearance capacity after toxic liver damage | Physiologically-based modelling in mice suggests an aggravated loss of clearance capacity after toxic liver damage Abstract Abstract Diseases and toxins may lead to death of active liver tissue, resulting in a loss of total clearance capacity at the whole-body level. However, it remains difficult to study, whether the ... |
PMC10847229 | core_pubmed_pmc | Levetiracetam modulates brain metabolic networks and transcriptomic signatures in the 5XFAD mouse model of Alzheimer’s disease | Levetiracetam modulates brain metabolic networks and transcriptomic signatures in the 5XFAD mouse model of Alzheimer’s disease Abstract Introduction Subcritical epileptiform activity is associated with impaired cognitive function and is commonly seen in patients with Alzheimer’s disease (AD). The anti-convulsant, levet... |
PMC7655531 | core_pubmed_pmc | Systematic Review and Pharmacological Considerations for Chloroquine and Its Analogs in the Treatment for COVID-19 | Systematic Review and Pharmacological Considerations for Chloroquine and Its Analogs in the Treatment for COVID-19 Abstract Abstract COVID-19 has been announced pandemic by WHO and over 17,000,000 people infected (Till April 21st 2020). The disease is currently under control in China, with a curative rate of 86.8%. Chl... |
PMC11483047 | core_pubmed_pmc | A novel ultra-performance liquid chromatography detection method development and validation for paclitaxel and its major metabolite in human plasma | A novel ultra-performance liquid chromatography detection method development and validation for paclitaxel and its major metabolite in human plasma Abstract BACKGROUND: Paclitaxel is a promising anticancer drug for patients with ovarian, breast, lung, gastrointestinal, genitourinary, prostate, and head-and-neck cancers... |
PMC12300661 | core_pubmed_pmc | A Semi-Mechanistic Mathematical Model of Immune Tolerance Induction to Support Preclinical Studies of Human Monoclonal Antibodies in Rats | A Semi-Mechanistic Mathematical Model of Immune Tolerance Induction to Support Preclinical Studies of Human Monoclonal Antibodies in Rats Abstract Background/Objectives: The administration of human monoclonal antibodies (mAb) in preclinical pharmacokinetics and toxicology studies often triggers an immune response, lead... |
PMC3889677 | core_pubmed_pmc | Circulating proteins as potential biomarkers of sunitinib and interferon-α efficacy in treatment-naïve patients with metastatic renal cell carcinoma | Circulating proteins as potential biomarkers of sunitinib and interferon-α efficacy in treatment-naïve patients with metastatic renal cell carcinoma Abstract Abstract Purpose We investigated potential biomarkers of efficacy in a phase III trial of sunitinib versus interferon-alpha (IFN-α), first-line in metastatic rena... |
PMC12339818 | core_pubmed_pmc | Targeted drug monitoring in oncology for personalized treatment with use of next generation analytics | Targeted drug monitoring in oncology for personalized treatment with use of next generation analytics Abstract Therapeutic drug monitoring (TDM) is a clinical procedure aimed at maintaining plasma drug concentrations within a specific therapeutic range, thereby maximizing the safety and efficacy of pharmacological ther... |
PMC10754982 | core_pubmed_pmc | Isavuconazole for Treating Invasive Mould Disease in Solid Organ Transplant Recipients | Isavuconazole for Treating Invasive Mould Disease in Solid Organ Transplant Recipients Abstract Solid organ transplant (SOT) recipients have a higher risk of developing invasive mould diseases (IMD). Isavuconazole is a novel broad-spectrum azole active against Aspergillus spp. and Mucor, well tolerated, with an excelle... |
PMC5739632 | core_pubmed_pmc | A population pharmacokinetic model for individualised dosage regimens of vancomycin in Chinese neonates and young infants | A population pharmacokinetic model for individualised dosage regimens of vancomycin in Chinese neonates and young infants Abstract Population pharmacokinetic (PPK) modelling is an easy and impartment method for estimating drug concentration for use inindividualized therapy, especially for young patients and to help pro... |
PMC10216553 | core_pubmed_pmc | Association between Food/UGT2B7 Polymorphisms and Pharmacokinetics/Pharmacodynamics Properties of Indapamide in Healthy Humans | Association between Food/UGT2B7 Polymorphisms and Pharmacokinetics/Pharmacodynamics Properties of Indapamide in Healthy Humans Abstract Abstract Indapamide is an effective and safe antihypertensive medication showing a beneficial effect in combination with other antihypertensive agents regarding morbidity and mortality... |
PMC8389032 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Adequacy of Novel β-Lactam/β-Lactamase Inhibitors against Gram-Negative Bacterial in Critically Ill Patients | Pharmacokinetic/Pharmacodynamic Adequacy of Novel β-Lactam/β-Lactamase Inhibitors against Gram-Negative Bacterial in Critically Ill Patients Abstract Abstract The optimal regimens of novel β-lactam/β-lactamase inhibitors (BLBLIs), ceftazidime/avibactam, ceftolozane/tazobactam, and meropenem/vaborbactam, are not well de... |
PMC12930024 | core_pubmed_pmc | Pharmacokinetic profiles of sertraline in pregnancy as a predictor of postpartum depressive symptoms | Pharmacokinetic profiles of sertraline in pregnancy as a predictor of postpartum depressive symptoms Abstract Aim To characterize pharmacokinetic changes of sertraline and its metabolite during pregnancy and postpartum, and their relationship to maternal postpartum depressive symptoms. Methods This was a prospective ob... |
PMC3210072 | core_pubmed_pmc | Future prospects in the treatment of erectile dysfunction: focus on avanafil | Future prospects in the treatment of erectile dysfunction: focus on avanafil Abstract Abstract The treatment of erectile dysfunction (ED) has been revolutionized in the last 15 years with the introduction of type 5 phosphodiesterase (PDE5) inhibitors. Their efficacy, safety, and ease of administration have made them fi... |
PMC6635391 | core_pubmed_pmc | A zwitterionic near-infrared fluorophore for real-time ureter identification during laparoscopic abdominopelvic surgery | A zwitterionic near-infrared fluorophore for real-time ureter identification during laparoscopic abdominopelvic surgery Abstract Abstract Iatrogenic injury of the ureters is a feared complication of abdominal surgery. Zwitterionic near-infrared fluorophores are molecules with geometrically-balanced, electrically-neutra... |
PMC8410448 | core_pubmed_pmc | Simultaneous Quantification of Four Ginsenosides in Rat Plasma and Its Application to a Comparative Pharmacokinetic Study in Normal and Depression Rats Using UHPLC-MS/MS | Simultaneous Quantification of Four Ginsenosides in Rat Plasma and Its Application to a Comparative Pharmacokinetic Study in Normal and Depression Rats Using UHPLC-MS/MS Abstract Abstract A sensitive method has been developed for simultaneous determination of ginsenoside Rh 1 (G-Rh 1 ), ginsenoside Rb 1 (G-Rb 1 ), gins... |
PMC10168112 | core_pubmed_pmc | Population Pharmacokinetic Model and Dosing Simulation of Meropenem Using Measured Creatinine Clearance for Patients with Sepsis | Population Pharmacokinetic Model and Dosing Simulation of Meropenem Using Measured Creatinine Clearance for Patients with Sepsis Abstract Supplemental Digital Content is Available in the Text. Purpose: Creatinine clearance (CCr) and pharmacokinetic parameters are markedly affected by pathophysiological changes in patie... |
PMC8698194 | core_pubmed_pmc | Personalized Antibiotic Therapy for the Critically Ill: Implementation Strategies and Effects on Clinical Outcome of Piperacillin Therapeutic Drug Monitoring—A Descriptive Retrospective Analysis | Personalized Antibiotic Therapy for the Critically Ill: Implementation Strategies and Effects on Clinical Outcome of Piperacillin Therapeutic Drug Monitoring—A Descriptive Retrospective Analysis Abstract Therapeutic drug monitoring (TDM) is increasingly relevant for an individualized antibiotic therapy and subsequently... |
PMC12781651 | core_pubmed_pmc | The scientific basis of synergy in traditional Chinese medicine: physicochemical, pharmacokinetic, and pharmacodynamic perspectives | The scientific basis of synergy in traditional Chinese medicine: physicochemical, pharmacokinetic, and pharmacodynamic perspectives Abstract Traditional Chinese medicine, with millennia of history, demonstrates significant therapeutic efficacy against diverse diseases. A key characteristic of traditional Chinese medici... |
PMC10052041 | core_pubmed_pmc | The Progress and Pitfalls of Pharmacogenetics-Based Precision Medicine in Schizophrenia Spectrum Disorders: A Systematic Review and Meta-Analysis | The Progress and Pitfalls of Pharmacogenetics-Based Precision Medicine in Schizophrenia Spectrum Disorders: A Systematic Review and Meta-Analysis Abstract Abstract The inadequate efficacy and adverse effects of antipsychotics severely affect the recovery of patients with schizophrenia spectrum disorders (SSD). We repor... |
PMC12018249 | core_pubmed_pmc | A mechanistic quantitative systems pharmacology model platform for translational efficacy evaluation and checkpoint combination design of bispecific immuno-modulatory antibodies | A mechanistic quantitative systems pharmacology model platform for translational efficacy evaluation and checkpoint combination design of bispecific immuno-modulatory antibodies Abstract Abstract Over the past 2 decades, tumor immunotherapies have witnessed remarkable advancements, especially with the emergence of immu... |
PMC7876946 | core_pubmed_pmc | Extrapyramidal side effects in first-episode schizophrenia treated with flupenthixol decanoate | Extrapyramidal side effects in first-episode schizophrenia treated with flupenthixol decanoate Abstract Background Concern for the development of extrapyramidal side effects (EPSEs) represents a barrier to the routine use of long-acting injectable (LAI) antipsychotic medication in patients with first-episode schizophre... |
PMC9306698 | core_pubmed_pmc | Evaluation of sex differences in the pharmacokinetics of oral sumatriptan in healthy Korean subjects using population pharmacokinetic modeling | Evaluation of sex differences in the pharmacokinetics of oral sumatriptan in healthy Korean subjects using population pharmacokinetic modeling Abstract Abstract Sumatriptan was introduced in 1983, as the first of the triptans, selective 5‐hydroxytryptamine (5‐HT 1B/1D ) receptor agonists, to treat moderate to severe mi... |
PMC12299188 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Simulation of Tofacitinib in Humans Using Extrapolation from Single-Species Renal Failure Model | Physiologically Based Pharmacokinetic Simulation of Tofacitinib in Humans Using Extrapolation from Single-Species Renal Failure Model Abstract Abstract Background/Objectives: Tofacitinib is a Janus kinase 1 and 3 inhibitor that was developed to treat rheumatoid arthritis. Accordingly, this study aimed to predict plasma... |
PMC11513306 | core_pubmed_pmc | Hepatotoxicity of antipsychotics: an exploratory pharmacoepidemiologic and pharmacodynamic study integrating FAERS data and in vitro receptor-binding affinities | Hepatotoxicity of antipsychotics: an exploratory pharmacoepidemiologic and pharmacodynamic study integrating FAERS data and in vitro receptor-binding affinities Abstract Abstract Introduction Antipsychotic psychopharmacotherapy is associated with the risk of drug-induced liver injury (DILI). However, understanding spec... |
PMC7046954 | core_pubmed_pmc | Methotrexate effect on immunogenicity and long-term maintenance of adalimumab in axial spondyloarthritis: a multicentric randomised trial | Methotrexate effect on immunogenicity and long-term maintenance of adalimumab in axial spondyloarthritis: a multicentric randomised trial Abstract Abstract Objectives Anti-drug antibodies (ADA) are responsible for decreased adalimumab efficacy in axial spondyloarthritis (SpA). We aimed to evaluate the ability of methot... |
PMC9657932 | core_pubmed_pmc | Enhancing an Oxidative “Trojan Horse” Action of Vitamin C with Arsenic Trioxide for Effective Suppression of KRAS-Mutant Cancers: A Promising Path at the Bedside | Enhancing an Oxidative “Trojan Horse” Action of Vitamin C with Arsenic Trioxide for Effective Suppression of KRAS-Mutant Cancers: A Promising Path at the Bedside Abstract Abstract The turn-on mutations of the KRAS gene, coding a small GTPase coupling growth factor signaling, are contributing to nearly 25% of all human ... |
PMC12162307 | core_pubmed_pmc | Dachengqi decoction for the treatment of acute pancreatitis: a comprehensive analysis based on metabolites, pharmacokinetics, and metabolites efficacy mechanisms | Dachengqi decoction for the treatment of acute pancreatitis: a comprehensive analysis based on metabolites, pharmacokinetics, and metabolites efficacy mechanisms Abstract Dachengqi decoction (DCQD) is a traditional Chinese medicine formula consisting of three botanical drugs and one mineral drug. It has anti-inflammato... |
PMC9678390 | core_pubmed_pmc | The impact of sphingosine-1-phosphate receptor modulators on COVID-19 and SARS-CoV-2 vaccination | The impact of sphingosine-1-phosphate receptor modulators on COVID-19 and SARS-CoV-2 vaccination Abstract Abstract Background Sphingosine-one phosphate receptor (S1PR) modulation inhibits S1PR1-mediated lymphocyte migration, lesion formation and positively-impacts on active multiple sclerosis (MS). These S1PR modulator... |
PMC7856802 | core_pubmed_pmc | Pharmacokinetics of duloxetine self-administered in overdose with quetiapine and other antipsychotic drugs in a Japanese patient admitted to hospital | Pharmacokinetics of duloxetine self-administered in overdose with quetiapine and other antipsychotic drugs in a Japanese patient admitted to hospital Abstract Background Combinations of antidepressant duloxetine (at doses of 40–60 mg/day) and other antipsychotics are frequently used in clinical treatment; however, seve... |
PMC5660441 | core_pubmed_pmc | In silico repurposing of antipsychotic drugs for Alzheimer’s disease | In silico repurposing of antipsychotic drugs for Alzheimer’s disease Abstract Abstract Background Alzheimer’s disease (AD) is the most prevalent form of dementia and represents one of the highest unmet requirements in medicine today. There is shortage of novel molecules entering into market because of poor pharmacokine... |
PMC8384516 | core_pubmed_pmc | Comparison of Pharmacokinetics and Tissue Distribution Characteristics of Three Diterpenoid Esters in Crude and Prepared Semen Euphorbiae | Comparison of Pharmacokinetics and Tissue Distribution Characteristics of Three Diterpenoid Esters in Crude and Prepared Semen Euphorbiae Abstract Abstract Background Semen Euphorbiae (SE) and Semen Euphorbiae Pulveratum (SEP) have a long history of medicinal use. SEP is the processed product of SE; both ancient and mo... |
PMC4541541 | core_pubmed_pmc | Pooled post hoc analysis of population pharmacokinetics of oxycodone and acetaminophen following a single oral dose of biphasic immediate-release/extended-release oxycodone/acetaminophen tablets | Pooled post hoc analysis of population pharmacokinetics of oxycodone and acetaminophen following a single oral dose of biphasic immediate-release/extended-release oxycodone/acetaminophen tablets Abstract This analysis evaluated the single-dose population pharmacokinetics (PK) of biphasic immediate-release (IR)/extended... |
PMC3631866 | core_pubmed_pmc | Renal Glucose Handling | Renal Glucose Handling Abstract OBJECTIVE Ipragliflozin, a sodium-glucose cotransporter 2 inhibitor, stimulates glycosuria and lowers glycemia in patients with type 2 diabetes (T2DM). The objective of this study was to assess the pharmacodynamics of ipragliflozin in T2DM patients with impaired renal function. RESEARCH ... |
PMC7998731 | core_pubmed_pmc | Pharmacokinetic Characterization of Supinoxin and Its Physiologically Based Pharmacokinetic Modeling in Rats | Pharmacokinetic Characterization of Supinoxin and Its Physiologically Based Pharmacokinetic Modeling in Rats Abstract Supinoxin is a novel anticancer drug candidate targeting the Y593 phospho-p68 RNA helicase, by exhibiting antiproliferative activity and/or suppression of tumor growth. This study aimed to characterize ... |
PMC12027796 | core_pubmed_pmc | A Pharmacokinetic–Pharmacodynamic Study of Protosappanoside D, a Component Derived from Biancaea decapetala Extracts, for Its Anti-Inflammatory Effects | A Pharmacokinetic–Pharmacodynamic Study of Protosappanoside D, a Component Derived from Biancaea decapetala Extracts, for Its Anti-Inflammatory Effects Abstract Abstract Biancaea decapetala (Roth) O. Deg. (Fabaceae), traditionally used by the Hmong people to treat rheumatoid arthritis (RA), has not been extensively stu... |
PMC9299763 | core_pubmed_pmc | Population pharmacokinetics of clonazepam in saliva and plasma: Steps towards noninvasive pharmacokinetic studies in vulnerable populations | Population pharmacokinetics of clonazepam in saliva and plasma: Steps towards noninvasive pharmacokinetic studies in vulnerable populations Abstract Aim Traditional studies focusing on the relationship between pharmacokinetics (PK) and pharmacodynamics necessitate blood draws, which are too invasive for children or oth... |
PMC5672925 | core_pubmed_pmc | A phase I/II study of KW-2478, an Hsp90 inhibitor, in combination with bortezomib in patients with relapsed/refractory multiple myeloma | A phase I/II study of KW-2478, an Hsp90 inhibitor, in combination with bortezomib in patients with relapsed/refractory multiple myeloma Abstract Abstract Background: KW-2478 is a novel non-ansamycin Hsp90 inhibitor with modest single-agent activity in relapsed/refractory myeloma but which shows synergistic antimyeloma ... |
PMC11914140 | core_pubmed_pmc | Rapid quantification and PK-PD modeling of rocuronium bromide in beagles using portable mass spectrometer | Rapid quantification and PK-PD modeling of rocuronium bromide in beagles using portable mass spectrometer Abstract Abstract Monitoring rocuronium bromide (Rocur) concentrations is crucial for assessing muscle relaxation in clinical anesthesia. However, no suitable instruments are currently available. This study explore... |
PMC12441064 | core_pubmed_pmc | Fungal metabolite Ochratoxin A inhibits MrkD1P of multidrug-resistant Klebsiella pneumoniae : Integrated computational and in vitro validation | Fungal metabolite Ochratoxin A inhibits MrkD1P of multidrug-resistant Klebsiella pneumoniae : Integrated computational and in vitro validation Abstract Multidrug-resistant (MDR) Klebsiella pneumoniae poses a significant global health concern, particularly in hospital setting where it causes severe and hard-to-treat inf... |
PMC12816413 | core_pubmed_pmc | Strategy for Identifying Rational Sensitivity Analysis Using PBPK Modeling for Precipitant Drug–Drug Interaction Predictions | Strategy for Identifying Rational Sensitivity Analysis Using PBPK Modeling for Precipitant Drug–Drug Interaction Predictions Abstract Physiology Based Pharmacokinetic (PBPK) modeling is an established essential tool for predicting and/or analyzing drug–drug interactions (DDI). Uncertainty and variability associated wit... |
PMC5344954 | core_pubmed_pmc | NC-6004 Phase I study in combination with gemcitabine for advanced solid tumors and population PK/PD analysis | NC-6004 Phase I study in combination with gemcitabine for advanced solid tumors and population PK/PD analysis Abstract Abstract Objectives This study was an open-label phase I study to confirm the safety and tolerability of NC-6004 in combination with gemcitabine in Japanese patients with advanced solid tumors and to a... |
PMC6704728 | core_pubmed_pmc | Population pharmacokinetics of tofacitinib in patients with psoriatic arthritis | Population pharmacokinetics of tofacitinib in patients with psoriatic arthritis Abstract Objective: Tofacitinib is an oral Janus kinase inhibitor for the treatment of psoriatic arthritis (PsA). This analysis characterized the pharmacokinetics (PK) of tofacitinib in adult patients with active PsA and evaluated the impac... |
PMC11541066 | core_pubmed_pmc | Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis | Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis Abstract Introduction Lymphocyte depletion via anti-CD52 monoclonal antibody (mAb) therapy is an effective treatment strategy for relapsing–remitting multiple sclerosis (MS) but i... |
PMC11542727 | core_pubmed_pmc | Favipiravir pharmacokinetics in Thai adults with mild COVID‐19: A sub‐study of interpatient variability and ethnic differences in exposure | Favipiravir pharmacokinetics in Thai adults with mild COVID‐19: A sub‐study of interpatient variability and ethnic differences in exposure Abstract Abstract This sub‐study sought to characterize the pharmacokinetics (PK) of favipiravir (FPV) within Thai adults and quantitatively assess differences in exposure to those ... |
PMC5999141 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Telavancin Compared with the Other Glycopeptides | Clinical Pharmacokinetics and Pharmacodynamics of Telavancin Compared with the Other Glycopeptides Abstract Telavancin was discovered by modifying the chemical structure of vancomycin and belongs to the group of lipoglycopeptides. It employs its antimicrobial potential through two distinct mechanisms of action: inhibit... |
PMC6957157 | core_pubmed_pmc | Pharmacokinetics, absolute bioavailability and tolerability of ketamine after intranasal administration to dexmedetomidine sedated dogs | Pharmacokinetics, absolute bioavailability and tolerability of ketamine after intranasal administration to dexmedetomidine sedated dogs Abstract Intranasal ketamine has recently gained interest in human medicine, not only for its sedative, anaesthetic or analgesic properties, but also in the management of treatment res... |
PMC8841461 | core_pubmed_pmc | Population pharmacokinetic/pharmacodynamic assessment of imipenem/cilastatin/relebactam in patients with hospital‐acquired/ventilator‐associated bacterial pneumonia | Population pharmacokinetic/pharmacodynamic assessment of imipenem/cilastatin/relebactam in patients with hospital‐acquired/ventilator‐associated bacterial pneumonia Abstract Abstract In the phase III RESTORE‐IMI 2 study (ClinicalTrials.gov: NCT02493764 ), the combination antibacterial agent imipenem/cilastatin/relebact... |
PMC7105400 | core_pubmed_pmc | Comparison of In Vivo Pharmacokinetics and Pharmacodynamics of Vancomycin Products Available in Korea | Comparison of In Vivo Pharmacokinetics and Pharmacodynamics of Vancomycin Products Available in Korea Abstract Abstract Purpose Few studies have been investigated the in vivo efficacy of generic vancomycin products available outside of the United States. In this study, we aimed to compare the in vivo pharmacokinetics (... |
PMC9319272 | core_pubmed_pmc | Simultaneous LC-ESI-MS/MS Quantification of Levosimendan and Its Metabolites for Therapeutic Drug Monitoring of Cardiac Surgery Patients | Simultaneous LC-ESI-MS/MS Quantification of Levosimendan and Its Metabolites for Therapeutic Drug Monitoring of Cardiac Surgery Patients Abstract Levosimendan is used in severe chronic cardiac insufficiency, also within the peri-operative setting. Real-life pharmacokinetic data in surgical patients is lacking, making t... |
PMC7534664 | core_pubmed_pmc | Beyond Deterministic Models in Drug Discovery and Development | Beyond Deterministic Models in Drug Discovery and Development Abstract Abstract The model-informed drug discovery and development paradigm is now well established among the pharmaceutical industry and regulatory agencies. This success has been mainly due to the ability of pharmacometrics to bring together different mod... |
PMC12511513 | core_pubmed_pmc | Baicalin nano-micelles for dry eye disease: LC–MS/MS method validation, pharmacokinetics and pharmacodynamics in preclinical models | Baicalin nano-micelles for dry eye disease: LC–MS/MS method validation, pharmacokinetics and pharmacodynamics in preclinical models Abstract This study aimed to establish a method for quantifying baicalin (BC) in rabbit ocular tissues and plasma, and evaluate the pharmacological efficacy and pharmacokinetic properties ... |
PMC5353912 | core_pubmed_pmc | Intra-individual variability of mycophenolic acid concentration according to renal function in liver transplant recipients receiving mycophenolate monotherapy | Intra-individual variability of mycophenolic acid concentration according to renal function in liver transplant recipients receiving mycophenolate monotherapy Abstract Backgrounds/Aims Mycophenolate mofetil (MMF) has wide inter- and intra-individual variability of mycophenolic acid (MPA) after liver transplantation (LT... |
PMC6058612 | core_pubmed_pmc | Uncovering the regional localization of inhaled salmeterol retention in the lung | Uncovering the regional localization of inhaled salmeterol retention in the lung Abstract Abstract Treatment of respiratory disease with a drug delivered via inhalation is generally held as being beneficial as it provides direct access to the lung target site with a minimum systemic exposure. There is however only limi... |
PMC3212724 | core_pubmed_pmc | MEGen: A Physiologically Based Pharmacokinetic Model Generator | MEGen: A Physiologically Based Pharmacokinetic Model Generator Abstract Abstract Physiologically based pharmacokinetic models are being used in an increasing number of different areas. However, they are perceived as complex, data hungry, resource intensive, and time consuming. In addition, model validation and verifica... |
PMC7956253 | core_pubmed_pmc | Simulation of the In Vivo Fate of Polymeric Nanoparticles Traced by Environment-Responsive Near-Infrared Dye: A Physiologically Based Pharmacokinetic Modelling Approach | Simulation of the In Vivo Fate of Polymeric Nanoparticles Traced by Environment-Responsive Near-Infrared Dye: A Physiologically Based Pharmacokinetic Modelling Approach Abstract The application of physiologically based pharmacokinetic models to nanoparticles is still very restricted and challenging, owing to the compli... |
PMC9588096 | core_pubmed_pmc | Dose Adjustment of Concomitant Antiseizure Medications During Cenobamate Treatment: Expert Opinion Consensus Recommendations | Dose Adjustment of Concomitant Antiseizure Medications During Cenobamate Treatment: Expert Opinion Consensus Recommendations Abstract Introduction Our objective was to provide expert consensus recommendations to improve treatment tolerability through dose adjustments of concomitant antiseizure medications (ASMs) during... |
PMC8062952 | core_pubmed_pmc | Targeting synovial fibroblast proliferation in rheumatoid arthritis (TRAFIC): an open-label, dose-finding, phase 1b trial | Targeting synovial fibroblast proliferation in rheumatoid arthritis (TRAFIC): an open-label, dose-finding, phase 1b trial Abstract Summary Background Current rheumatoid arthritis therapies target immune inflammation and are subject to ceiling effects. Seliciclib is an orally available cyclin-dependent kinase inhibitor ... |
PMC10990645 | core_pubmed_pmc | Associations of Combined Exposure to Metabolic and Inflammatory Indicators with Thyroid Nodules in Adults: A Nested Case-Control Study | Associations of Combined Exposure to Metabolic and Inflammatory Indicators with Thyroid Nodules in Adults: A Nested Case-Control Study Abstract Objective To explore associations of combined exposure to metabolic/inflammatory indicators with thyroid nodules. Methods We reviewed personal data for health screenings from 2... |
PMC10099850 | core_pubmed_pmc | A meta‐analysis of methotrexate polyglutamates in relation to efficacy and toxicity of methotrexate in inflammatory arthritis, colitis and dermatitis | A meta‐analysis of methotrexate polyglutamates in relation to efficacy and toxicity of methotrexate in inflammatory arthritis, colitis and dermatitis Abstract Abstract Aims In immune‐mediated inflammatory diseases (IMIDs), early symptom control is a key therapeutic goal. Methotrexate (MTX) is the first‐line treatment a... |
PMC2878603 | core_pubmed_pmc | Pharmacokinetics, immunogenicity and bioactivity of the therapeutic antibody catumaxomab intraperitoneally administered to cancer patients | Pharmacokinetics, immunogenicity and bioactivity of the therapeutic antibody catumaxomab intraperitoneally administered to cancer patients Abstract Abstract AIMS Catumaxomab is the first EMEA approved trifunctional anti-EpCAM×anti-CD3 antibody for the treatment of cancer patients with malignant ascites. A phase II phar... |
PMC8147617 | core_pubmed_pmc | Population Pharmacokinetics of Primaquine in the Korean Population | Population Pharmacokinetics of Primaquine in the Korean Population Abstract Abstract While primaquine has long been used for malaria treatment, treatment failure is common. This study aims to develop a population pharmacokinetic model of primaquine and its metabolite, carboxyprimaquine, and examine factors influencing ... |
PMC9574748 | core_pubmed_pmc | Designing phase I oncology dose escalation using dose–exposure–toxicity models as a complementary approach to model‐based dose–toxicity models | Designing phase I oncology dose escalation using dose–exposure–toxicity models as a complementary approach to model‐based dose–toxicity models Abstract Abstract One of the objectives of oncology phase I dose‐escalation studies has been to determine the maximum tolerated dose (MTD). Although MTD is no longer set as the ... |
PMC10673377 | core_pubmed_pmc | Molecular Insight into the Pharmacological Potential of Clerodendrum minahassae Leaf Extract for Type-2 Diabetes Management Using the Network Pharmacology Approach | Molecular Insight into the Pharmacological Potential of Clerodendrum minahassae Leaf Extract for Type-2 Diabetes Management Using the Network Pharmacology Approach Abstract Abstract Background and Objectives: The increasing occurrence and prevalence of type-2 diabetes mellitus (T2DM) have led to a growing interest in r... |
PMC12917758 | core_pubmed_pmc | Therapeutic drug monitoring of adalimumab in hidradenitis suppurativa: a prospective observational study | Therapeutic drug monitoring of adalimumab in hidradenitis suppurativa: a prospective observational study Abstract Abstract Background Adalimumab (ADA) is an effective treatment for moderate to severe hidradenitis suppurativa (HS). However, nearly half of patients receiving the standard dose may lose response. Objective... |
PMC3218893 | core_pubmed_pmc | Infliximab in ankylosing spondylitis: alone or in combination with methotrexate? A pharmacokinetic comparative study | Infliximab in ankylosing spondylitis: alone or in combination with methotrexate? A pharmacokinetic comparative study Abstract Abstract Introduction Methotrexate (MTX) has been shown to modify infliximab pharmacokinetics in rheumatoid arthritis. However, its combination with infliximab in the treatment of ankylosing spo... |
PMC9016006 | core_pubmed_pmc | A Multi‑Center, Open‑Label, Single‑Arm Trial to Evaluate the Efficacy, Pharmacokinetics, and Safety and Tolerability of IGSC 20% in Subjects with Primary Immunodeficiency | A Multi‑Center, Open‑Label, Single‑Arm Trial to Evaluate the Efficacy, Pharmacokinetics, and Safety and Tolerability of IGSC 20% in Subjects with Primary Immunodeficiency Abstract Purpose The purpose of this phase 3 study was to evaluate the efficacy, pharmacokinetics (PK), and safety of Immune Globulin Subcutaneous (H... |
PMC12217474 | core_pubmed_pmc | Population pharmacokinetic analyses for telavancin using data from healthy subjects and patients with infections | Population pharmacokinetic analyses for telavancin using data from healthy subjects and patients with infections Abstract ABSTRACT Telavancin is an intravenously administered lipoglycopeptide antibiotic active against clinically relevant gram-positive pathogens. In these analyses, a population pharmacokinetic (PK) mode... |
PMC7307925 | core_pubmed_pmc | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design Abstract The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs. In this article, we report a novel method to screen for ionizable molecules... |
PMC9684194 | core_pubmed_pmc | Thrombin generation assays to personalize treatment in bleeding and thrombotic diseases | Thrombin generation assays to personalize treatment in bleeding and thrombotic diseases Abstract Abstract Treatment of bleeding and thrombotic disorders is highly standardized and based on evidence-based medicine guidelines. These evidence-based treatment schemes are well accepted but may lead to either insufficient tr... |
PMC7409647 | core_pubmed_pmc | Pharmacokinetic and metabolomic analyses of Mangiferin calcium salt in rat models of type 2 diabetes and non-alcoholic fatty liver disease | Pharmacokinetic and metabolomic analyses of Mangiferin calcium salt in rat models of type 2 diabetes and non-alcoholic fatty liver disease Abstract Abstract Background Non-alcoholic fatty liver is one of the most common comorbidities of diabetes. It can cause disturbance of glucose and lipid metabolism in the body, gra... |
PMC11390206 | core_pubmed_pmc | In Silico Study of Coumarins: Wedelolactone as a Potential Inhibitor of the Spike Protein of the SARS-CoV-2 Variants | In Silico Study of Coumarins: Wedelolactone as a Potential Inhibitor of the Spike Protein of the SARS-CoV-2 Variants Abstract Abstract Despite the rigorous global efforts to control SARS-CoV-2 transmission, it continues to pose a serious threat to humans with the frequent emergence of new variants. Thus, robust therape... |
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