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PMC8251570 | core_pubmed_pmc | A Phase 1 Study to Investigate the Effects of Cortexolone 17α‐Propionate, Also Known as Clascoterone, on the QT Interval Using the Meal Effect to Demonstrate ECG Assay Sensitivity | A Phase 1 Study to Investigate the Effects of Cortexolone 17α‐Propionate, Also Known as Clascoterone, on the QT Interval Using the Meal Effect to Demonstrate ECG Assay Sensitivity Abstract Abstract Cortexolone 17α‐propionate, also known as clascoterone, is a potent androgen receptor inhibitor intended for the topical t... |
PMC9495723 | core_pubmed_pmc | Current Uncertainties and Future Challenges Regarding NAD+ Boosting Strategies | Current Uncertainties and Future Challenges Regarding NAD+ Boosting Strategies Abstract Abstract Precursors of nicotinamide adenine dinucleotide (NAD+), modulators of enzymes of the NAD+ biosynthesis pathways and inhibitors of NAD+ consuming enzymes, are the main boosters of NAD+. Increasing public awareness and intere... |
PMC3376429 | core_pubmed_pmc | Pleiotropic effects of pitavastatin | Pleiotropic effects of pitavastatin Abstract Abstract 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are established first line treatments for hypercholesterolaemia. In addition to the direct effects of statins in reducing concentrations of atherogenic low density lipoprotein cholesterol... |
PMC11812945 | core_pubmed_pmc | A tutorial on pharmacometric Markov models | A tutorial on pharmacometric Markov models Abstract Abstract The Markov chain is a stochastic process in which the future value of a variable is conditionally independent of the past, given its present value. Data with Markovian features are characterized by: frequent observations relative to the expected changes in va... |
PMC7119008 | core_pubmed_pmc | Intranasal epinephrine effects on epinephrine pharmacokinetics and heart rate in a nasal congestion canine model | Intranasal epinephrine effects on epinephrine pharmacokinetics and heart rate in a nasal congestion canine model Abstract Background Histamine release and vasodilation during an allergic reaction can alter the pharmacokinetics of drugs administered via the intranasal (IN) route. The current study evaluated the effects ... |
PMC10507317 | core_pubmed_pmc | Population pharmacokinetics of Amisulpride in Chinese patients with schizophrenia with external validation: the impact of renal function | Population pharmacokinetics of Amisulpride in Chinese patients with schizophrenia with external validation: the impact of renal function Abstract Introduction: Amisulpride is primarily eliminated via the kidneys. Given the clear influence of renal clearance on plasma concentration, we aimed to explicitly examine the im... |
PMC12167912 | core_pubmed_pmc | A Pragmatic Approach to Handling Censored Data Below the Lower Limit of Quantification in Pharmacokinetic Modeling | A Pragmatic Approach to Handling Censored Data Below the Lower Limit of Quantification in Pharmacokinetic Modeling Abstract ABSTRACT Proper handling of data below the lower limit of quantification (BLQ) is crucial for accurate pharmacokinetic parameter estimation. The M3 method proposed by Beal uses a likelihood‐based ... |
PMC3006138 | core_pubmed_pmc | Fexinidazole – A New Oral Nitroimidazole Drug Candidate Entering Clinical Development for the Treatment of Sleeping Sickness | Fexinidazole – A New Oral Nitroimidazole Drug Candidate Entering Clinical Development for the Treatment of Sleeping Sickness Abstract Background Human African trypanosomiasis (HAT), also known as sleeping sickness, is a fatal parasitic disease caused by trypanosomes. Current treatment options for HAT are scarce, toxic,... |
PMC11470857 | core_pubmed_pmc | Pharmacokinetics and clinical outcomes of low-dose nivolumab relative to conventional dose in patients with advanced cancer | Pharmacokinetics and clinical outcomes of low-dose nivolumab relative to conventional dose in patients with advanced cancer Abstract Abstract Purpose Nivolumab is approved at various doses, including 3 mg/kg, 240 mg and 480 mg flat doses at various dosing intervals. The concept of low-dose immunotherapy is gaining trac... |
PMC6550498 | core_pubmed_pmc | Double-blind, randomized, placebo-controlled study of trofinetide in pediatric Rett syndrome | Double-blind, randomized, placebo-controlled study of trofinetide in pediatric Rett syndrome Abstract Abstract Objective To determine safety, tolerability, and pharmacokinetics of trofinetide and evaluate its efficacy in female children/adolescents with Rett syndrome (RTT), a debilitating neurodevelopmental condition f... |
PMC6949133 | core_pubmed_pmc | Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability | Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability Abstract The relative contribution of hepatic compared with intestinal oxidative metabolism is a crucial factor in drug oral bioavailability and therapeutic efficacy. Oxidative metabolis... |
PMC11303472 | core_pubmed_pmc | Assessment of body mass-related covariates for rifampicin pharmacokinetics in healthy Caucasian volunteers | Assessment of body mass-related covariates for rifampicin pharmacokinetics in healthy Caucasian volunteers Abstract Purpose Currently, body weight-based dosing of rifampicin is recommended. But lately, fat-free mass (FFM) was reported to be superior to body weight (BW). The present evaluation aimed to assess the influe... |
PMC3099639 | core_pubmed_pmc | Pseudocontinuous arterial spin labeling reveals dissociable effects of morphine and alcohol on regional cerebral blood flow | Pseudocontinuous arterial spin labeling reveals dissociable effects of morphine and alcohol on regional cerebral blood flow Abstract Abstract We have examined sensitivity and specificity of pseudocontinuous arterial spin labeling (PCASL) to detect global and regional changes in cerebral blood flow (CBF) in response to ... |
PMC4577253 | core_pubmed_pmc | Exposure–outcome analysis in depressed patients treated with paroxetine using population pharmacokinetics | Exposure–outcome analysis in depressed patients treated with paroxetine using population pharmacokinetics Abstract Purpose This study investigated population pharmacokinetics of paroxetine, and then performed an integrated analysis of exposure and clinical outcome using population pharmacokinetic parameter estimates in... |
PMC3411319 | core_pubmed_pmc | Pharmacokinetics and Toxicity in Rats and Monkeys of coDbait: A Therapeutic Double-stranded DNA Oligonucleotide Conjugated to Cholesterol | Pharmacokinetics and Toxicity in Rats and Monkeys of coDbait: A Therapeutic Double-stranded DNA Oligonucleotide Conjugated to Cholesterol Abstract Abstract Increased DNA repair activity in cancer cells is one of their primary mechanisms of resistance to current radio- and chemotherapies. The molecule coDbait is the fir... |
PMC4947517 | core_pubmed_pmc | Biases affecting injected doses of an experimental drug during clinical trials | Biases affecting injected doses of an experimental drug during clinical trials Abstract Background During clinical trials, researchers rarely question nominal doses specified on labels of investigational products, overlooking the potential for inaccuracies that may result when calculating pharmacokinetic and pharmacody... |
PMC12074391 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic modeling of benznidazole and its antitrypanosomal activity in a murine model of chronic Chagas disease | Pharmacokinetic-pharmacodynamic modeling of benznidazole and its antitrypanosomal activity in a murine model of chronic Chagas disease Abstract Abstract Background There is an urgent need for improved treatments for Chagas disease, a neglected tropical infection caused by the protozoan parasite Trypanosoma cruzi . Benz... |
PMC9290990 | core_pubmed_pmc | The New S7B/E14 Question and Answer Draft Guidance for Industry: Contents and Commentary | The New S7B/E14 Question and Answer Draft Guidance for Industry: Contents and Commentary Abstract Abstract In August 2020, the International Council on Harmonisation (ICH) released a new draft document, which for the first time combined nonclinical (S7B) and clinical (E14) Questions and Answers (Q&As) into 1 document. ... |
PMC12227458 | core_pubmed_pmc | Pharmacokinetics of Intraperitoneal Lidocaine for Sustained Postoperative Analgesia in Adults | Pharmacokinetics of Intraperitoneal Lidocaine for Sustained Postoperative Analgesia in Adults Abstract Abstract Background and Objective Intraperitoneal lidocaine is an emerging strategy for analgesia following abdominal surgery but its pharmacokinetics are poorly quantified. We aimed to develop a pharmacokinetic model... |
PMC7153848 | core_pubmed_pmc | Dose escalation PET imaging for safety and effective therapy dose optimization of a bispecific antibody | Dose escalation PET imaging for safety and effective therapy dose optimization of a bispecific antibody Abstract ABSTRACT Selecting the dose for efficacy and first-in-human studies of bispecific antibodies (BsAbs) is a challenging process. Herein, positron emission tomography (PET) imaging with 89 Zr-labeled IBI322, an... |
PMC5993275 | core_pubmed_pmc | Effects of smoking and body mass index on the exposure of fentanyl in patients with cancer | Effects of smoking and body mass index on the exposure of fentanyl in patients with cancer Abstract The transdermal fentanyl patch is widely used to treat cancer-related pain despite its wide inter- and intrapatient variability in pharmacokinetics. The aim of this study was to investigate whether smoking and body size ... |
PMC11246974 | core_pubmed_pmc | Pharmacokinetics of Sofosbuvir/Velpatasvir and efficacy of an alternate‐day treatment in hemodialysis patients with chronic hepatitis C infection | Pharmacokinetics of Sofosbuvir/Velpatasvir and efficacy of an alternate‐day treatment in hemodialysis patients with chronic hepatitis C infection Abstract Abstract Sofosbuvir/Velpatasvir (SOF/VEL) is a combination drug used for chronic hepatitis C (HCV) infection. However, limited information exists regarding the pharm... |
PMC11157419 | core_pubmed_pmc | Pharmacokinetics of single‐dose rivaroxaban under fed state in obese vs. non‐obese subjects: An open‐label controlled clinical trial (RIVOBESE‐PK) | Pharmacokinetics of single‐dose rivaroxaban under fed state in obese vs. non‐obese subjects: An open‐label controlled clinical trial (RIVOBESE‐PK) Abstract Abstract The evidence of rivaroxaban's pharmacokinetics in obese compared with non‐obese populations remains inconclusive. We aimed to compare the pharmacokinetic p... |
PMC10689296 | core_pubmed_pmc | Comparative Effectiveness of Different Anticoagulation Strategies in Atrial Fibrillation and Renal Dysfunction: A Systematic Review | Comparative Effectiveness of Different Anticoagulation Strategies in Atrial Fibrillation and Renal Dysfunction: A Systematic Review Abstract Abstract Atrial fibrillation (AF) is a common cardiac arrhythmia that increases the risk of stroke and thromboembolism. Anticoagulation therapy can reduce this risk, but the optim... |
PMC7080151 | core_pubmed_pmc | Preventive and therapeutic strategies in critically ill patients with highly resistant bacteria | Preventive and therapeutic strategies in critically ill patients with highly resistant bacteria Abstract The antibiotic pipeline continues to diminish and the majority of the public remains unaware of this critical situation. The cause of the decline of antibiotic development is multifactorial and currently most ICUs a... |
PMC11782835 | core_pubmed_pmc | Pharmacokinetics, safety and efficacy of elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide in children with HIV aged from 2 years and weighing at least 14 kg | Pharmacokinetics, safety and efficacy of elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide in children with HIV aged from 2 years and weighing at least 14 kg Abstract Abstract Introduction Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (E/C/F/TAF) was efficacious and well tolerated in children/ad... |
PMC5445237 | core_pubmed_pmc | Population Pharmacokinetics, Pharmacodynamics, and Exploratory Exposure–Response Analyses of Apixaban in Subjects Treated for Venous Thromboembolism | Population Pharmacokinetics, Pharmacodynamics, and Exploratory Exposure–Response Analyses of Apixaban in Subjects Treated for Venous Thromboembolism Abstract Apixaban is approved for treatment of venous thromboembolism (VTE) and prevention of recurrence. Population pharmacokinetics, pharmacokinetics–pharmacodynamics (a... |
PMC11052879 | core_pubmed_pmc | ‘Totality of Evidence’ Approach in the Development of GP2017, an Approved Adalimumab Biosimilar | ‘Totality of Evidence’ Approach in the Development of GP2017, an Approved Adalimumab Biosimilar Abstract Abstract Introduction Hyrimoz ® , (GP2017 [SDZ-ADL]), is a biosimilar to Humira ® (REF-ADL). SDZ-ADL was approved in 2018 by both the United States Food and Drug Administration (US FDA) and European Medicines Agency... |
PMC12907776 | core_pubmed_pmc | A Randomized, Double‐Blind, Placebo‐Controlled, Multiple Ascending Dose Phase 1 Study of Firsekibart in Chinese Healthy Participants | A Randomized, Double‐Blind, Placebo‐Controlled, Multiple Ascending Dose Phase 1 Study of Firsekibart in Chinese Healthy Participants Abstract Abstract Firsekibart is an anti‐IL‐1β monoclonal antibody for treating acute gout flares in adults. This randomized, double‐blind, placebo‐controlled study assessed the safety, p... |
PMC10542493 | core_pubmed_pmc | Theoretical Considerations and Empirical Predictions of the Pharmaco- and Population Dynamics of Heteroresistance | Theoretical Considerations and Empirical Predictions of the Pharmaco- and Population Dynamics of Heteroresistance Abstract Antibiotics are considered one of the most important contributions to clinical medicine in the last 100 years. Due to the use and overuse of these drugs, there have been increasing frequencies of i... |
PMC11799083 | core_pubmed_pmc | Evaluation of different PK/PD ratios of three enrofloxacin preparations on the clinical response of pneumonic calves | Evaluation of different PK/PD ratios of three enrofloxacin preparations on the clinical response of pneumonic calves Abstract Importance Enrofloxacin preparations are available for administration daily or every 3 days. This study presents clinical evidence to define which preparation is adequate to treat clinical cases... |
PMC10141822 | core_pubmed_pmc | Bioprospecting phytochemicals of Rosmarinus officinalis L. for targeting SARS-CoV-2 main protease (M pro ): a computational study | Bioprospecting phytochemicals of Rosmarinus officinalis L. for targeting SARS-CoV-2 main protease (M pro ): a computational study Abstract Abstract Context The persistent spread of highly contagious COVID-19 disease is one of the deadliest occurrences in the history of mankind. Despite the distribution of numerous effi... |
PMC11393542 | core_pubmed_pmc | Novel Combinations of Immunotherapies or DNA Damage Repair Inhibitors in Platinum-Refractory Extensive-Stage Small Cell Lung Cancer: The Phase II BALTIC Study | Novel Combinations of Immunotherapies or DNA Damage Repair Inhibitors in Platinum-Refractory Extensive-Stage Small Cell Lung Cancer: The Phase II BALTIC Study Abstract Abstract Purpose: The phase II, multiarm, signal-searching BALTIC study ( NCT02937818 ) assessed novel treatment combinations for platinum-refractory/re... |
PMC12407664 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, efficacy and drug resistance selection of injectable long-acting lenacapavir pre-exposure prophylaxis (PrEP) against HIV | Pharmacokinetics, pharmacodynamics, efficacy and drug resistance selection of injectable long-acting lenacapavir pre-exposure prophylaxis (PrEP) against HIV Abstract Abstract Oral pre-exposure prophylaxis (PrEP) denotes an effective strategy to reduce the risk of HIV infection. However, many individuals encounter diffi... |
PMC9846493 | core_pubmed_pmc | Pharmacokinetic analysis of linezolid for multidrug resistant tuberculosis at a tertiary care centre in Mumbai, India | Pharmacokinetic analysis of linezolid for multidrug resistant tuberculosis at a tertiary care centre in Mumbai, India Abstract Linezolid is an oxazolidinone used to treat multidrug-resistant tuberculosis (MDR-TB), including in the recently-endorsed shorter 6-month treatment regimens. Due to its narrow therapeutic index... |
PMC5658289 | core_pubmed_pmc | A Translational Systems Pharmacology Model for Aβ Kinetics in Mouse, Monkey, and Human | A Translational Systems Pharmacology Model for Aβ Kinetics in Mouse, Monkey, and Human Abstract Abstract A mechanistic model of amyloid beta production, degradation, and distribution was constructed for mouse, monkey, and human, calibrated and externally verified across multiple datasets. Simulations of single‐dose ava... |
PMC10192147 | core_pubmed_pmc | A Systematic Evaluation of Cost-Saving Dosing Regimens for Therapeutic Antibodies and Antibody-Drug Conjugates for the Treatment of Lung Cancer | A Systematic Evaluation of Cost-Saving Dosing Regimens for Therapeutic Antibodies and Antibody-Drug Conjugates for the Treatment of Lung Cancer Abstract Background Expensive novel anticancer drugs put a serious strain on healthcare budgets, and the associated drug expenses limit access to life-saving treatments worldwi... |
PMC5874844 | core_pubmed_pmc | Absolute Oral Bioavailability of Creatine Monohydrate in Rats: Debunking a Myth | Absolute Oral Bioavailability of Creatine Monohydrate in Rats: Debunking a Myth Abstract Abstract Creatine is an ergogenic compound used by athletes to enhance performance. Supplementation with creatine monohydrate (CM) has been suggested for musculoskeletal and neurological disorders. Until now, little is known about ... |
PMC11511332 | core_pubmed_pmc | Efficacy of Ciprofloxacin in Treating Gram-Negative Infections: Does Obesity Matter? | Efficacy of Ciprofloxacin in Treating Gram-Negative Infections: Does Obesity Matter? Abstract Background: Obesity is considered a health issue associated with increased morbidity and a risk factor for multiple conditions, such as type 2 diabetes, cardiovascular diseases and infections. It may affect the pharmacokinetic... |
PMC10387630 | core_pubmed_pmc | Changes of colistin pharmacokinetics in critically ill patients due to the extracorporeal membrane oxygenation: protocol for the COL-ECMO2022 trial – a prospective, non-randomised, open-label phase IV pharmacokinetic clinical trial | Changes of colistin pharmacokinetics in critically ill patients due to the extracorporeal membrane oxygenation: protocol for the COL-ECMO2022 trial – a prospective, non-randomised, open-label phase IV pharmacokinetic clinical trial Abstract Introduction Colistin is a lipopeptide antibiotic administered as an inactive p... |
PMC10780092 | core_pubmed_pmc | Pharmacological Properties of Shionone: Potential Anti-Inflammatory Phytochemical against Different Diseases | Pharmacological Properties of Shionone: Potential Anti-Inflammatory Phytochemical against Different Diseases Abstract Shionone is a triterpenoid that is the primary constituent of an important ancient Chinese medicine named Radix Asteris. It has emerged as an attractive candidate against different important diseases, i... |
PMC7762536 | core_pubmed_pmc | The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats | The Impact of Polymer Size and Cleavability on the Intravenous Pharmacokinetics of PEG-Based Hyperbranched Polymers in Rats Abstract Abstract A better understanding of the impact of molecular size and linkers is important for PEG-based hyperbranched polymers (HBPs) intended as tailored drug delivery vehicles. This stud... |
PMC6983027 | core_pubmed_pmc | Pharmacokinetic Comparison of Epinastine Using Developed Human Plasma Assays | Pharmacokinetic Comparison of Epinastine Using Developed Human Plasma Assays Abstract Abstract The purpose of the study was to develop two new methods, HPLC-UV and UPLC-MS/MS, for quantifying epinastine in human plasma and to compare pharmacokinetic (PK) parameters obtained using them. Even in the same sample, there ma... |
PMC9150776 | core_pubmed_pmc | Application of a Physiologically Based Pharmacokinetic Approach to Predict Theophylline Pharmacokinetics Using Virtual Non-Pregnant, Pregnant, Fetal, Breast-Feeding, and Neonatal Populations | Application of a Physiologically Based Pharmacokinetic Approach to Predict Theophylline Pharmacokinetics Using Virtual Non-Pregnant, Pregnant, Fetal, Breast-Feeding, and Neonatal Populations Abstract Perinatal pharmacology is influenced by a myriad of physiological variables that are changing dynamically. The influence... |
PMC8659147 | core_pubmed_pmc | Chalcone Scaffolds, Bioprecursors of Flavonoids: Chemistry, Bioactivities, and Pharmacokinetics | Chalcone Scaffolds, Bioprecursors of Flavonoids: Chemistry, Bioactivities, and Pharmacokinetics Abstract Chalcones are secondary metabolites belonging to the flavonoid (C 6 -C 3 -C 6 system) family that are ubiquitous in edible and medicinal plants, and they are bioprecursors of plant flavonoids. Chalcones and their na... |
PMC5482735 | core_pubmed_pmc | Towards better dose individualisation: metabolic phenotyping to predict cabazitaxel pharmacokinetics in men with prostate cancer | Towards better dose individualisation: metabolic phenotyping to predict cabazitaxel pharmacokinetics in men with prostate cancer Abstract Background: Cabazitaxel is approved for treatment of castration-resistant metastatic prostate cancer. The current dosing strategy of cabazitaxel is based on body surface area (BSA). ... |
PMC8297514 | core_pubmed_pmc | Totality of Evidence Supporting the Use of ABP 980, a Trastuzumab Biosimilar: Practical Considerations | Totality of Evidence Supporting the Use of ABP 980, a Trastuzumab Biosimilar: Practical Considerations Abstract ABP 980 (KANJINTI™, Amgen, Thousand Oaks, CA, USA; Amgen Europe B.V., The Netherlands) is a biosimilar to trastuzumab (Herceptin ® ), a monoclonal antibody that selectively binds human epidermal growth factor... |
PMC12155695 | core_pubmed_pmc | Modeling the Ocular Pharmacokinetics and Pharmacodynamics of Ranibizumab for Improved Understanding and Data Collection Strategies in Ocular Diseases | Modeling the Ocular Pharmacokinetics and Pharmacodynamics of Ranibizumab for Improved Understanding and Data Collection Strategies in Ocular Diseases Abstract Abstract Purpose Improving our understanding of the ocular pharmacokinetics and pharmacodynamics of anti-vascular endothelial growth factor (VEGF) therapies, suc... |
PMC11279564 | core_pubmed_pmc | Advances in Nanomedicine for Precision Insulin Delivery | Advances in Nanomedicine for Precision Insulin Delivery Abstract Diabetes mellitus, which comprises a group of metabolic disorders affecting carbohydrate metabolism, is characterized by improper glucose utilization and excessive production, leading to hyperglycemia. The global prevalence of diabetes is rising, with pro... |
PMC9078533 | core_pubmed_pmc | A UPLC-MS/MS method for simultaneous quantification of pairs of oleanene- and ursane-type triterpenoid saponins and their major metabolites in mice plasma and its application to a comparative pharmacokinetic study | A UPLC-MS/MS method for simultaneous quantification of pairs of oleanene- and ursane-type triterpenoid saponins and their major metabolites in mice plasma and its application to a comparative pharmacokinetic study Abstract Ilexhainanoside D (IhD) and Ilexsaponin A 1 (IsA) are a pair of oleanene- and ursane-type triterp... |
PMC9501900 | core_pubmed_pmc | Cranberry Ingestion Modulated Drug Transporters and Metabolizing Enzymes: Gefitinib Used as a Probe Substrate in Rats | Cranberry Ingestion Modulated Drug Transporters and Metabolizing Enzymes: Gefitinib Used as a Probe Substrate in Rats Abstract Abstract Cranberry, a polyphenol-rich functional food, is commonly used for the prophylaxis of urinary tract infections. Gefitinib, an anticancer agent clinically prescribed to treat non-small-... |
PMC3414821 | core_pubmed_pmc | Phenol-Explorer 2.0: a major update of the Phenol-Explorer database integrating data on polyphenol metabolism and pharmacokinetics in humans and experimental animals | Phenol-Explorer 2.0: a major update of the Phenol-Explorer database integrating data on polyphenol metabolism and pharmacokinetics in humans and experimental animals Abstract Abstract Phenol-Explorer, launched in 2009, is the only comprehensive web-based database on the content in foods of polyphenols, a major class of... |
PMC8401636 | core_pubmed_pmc | Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films | Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films Abstract Abstract The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfe... |
PMC3447615 | core_pubmed_pmc | Development and Characterization of Pharmacokinetic Parameters of Fast-Dissolving Films Containing Levocetirizine | Development and Characterization of Pharmacokinetic Parameters of Fast-Dissolving Films Containing Levocetirizine Abstract Abstract A fast-dissolving film containing levocetirizine, a non-sedative antihistamine drug, was developed using pullulan, xanthan gum, propylene glycol, and tween 80 as the base materials. The dr... |
PMC9561726 | core_pubmed_pmc | External evaluation of published population pharmacokinetic models of posaconazole | External evaluation of published population pharmacokinetic models of posaconazole Abstract Population pharmacokinetic (PopPK) models of posaconazole have been established to promote the precision dosing. However, the performance of these models extrapolated to other centers has not been evaluated. This study aimed to ... |
PMC10155250 | core_pubmed_pmc | In silico study of potential SARS-CoV-2 antagonist from Clitoria ternatea | In silico study of potential SARS-CoV-2 antagonist from Clitoria ternatea Abstract Objectives: In this study, we implemented a structure-based virtual screening protocol in search of natural bioactive compounds in Clitoria ternatea that could inhibit the viral M pro . Methods: A library of twelve main bioactive compoun... |
PMC5354496 | core_pubmed_pmc | Targeted Fcγ Receptor (FcγR)-mediated Clearance by a Biparatopic Bispecific Antibody * | Targeted Fcγ Receptor (FcγR)-mediated Clearance by a Biparatopic Bispecific Antibody * Abstract Abstract Soluble ligands have commonly been targeted by antibody therapeutics for cancers and other diseases. Although monoclonal antibodies targeting such ligands can block their interactions with their cognate receptors, t... |
PMC6398794 | core_pubmed_pmc | Non-inferiority double-blind randomised controlled trial comparing gabapentin versus tramadol for the treatment of chronic neuropathic or mixed pain in children and adolescents: the GABA-1 trial—a study protocol | Non-inferiority double-blind randomised controlled trial comparing gabapentin versus tramadol for the treatment of chronic neuropathic or mixed pain in children and adolescents: the GABA-1 trial—a study protocol Abstract Introduction Gabapentin is currently used ‘off-label’ in children and adolescents with chronic neur... |
PMC6021635 | core_pubmed_pmc | Personalizing Polymyxin B Dosing Using an Adaptive Feedback Control Algorithm | Personalizing Polymyxin B Dosing Using an Adaptive Feedback Control Algorithm Abstract ABSTRACT Polymyxin B is used as an antibiotic of last resort for patients with multidrug-resistant Gram-negative bacterial infections; however, it carries a significant risk of nephrotoxicity. Herein we present a polymyxin B therapeu... |
PMC12910641 | core_pubmed_pmc | Design, Synthesis, and Pharmacokinetic Profiling of Fluorinated Reversible N ‑Alkyl Carbamate Derivatives of Psilocin for Sub-Hallucinogenic Brain Exposure | Design, Synthesis, and Pharmacokinetic Profiling of Fluorinated Reversible N ‑Alkyl Carbamate Derivatives of Psilocin for Sub-Hallucinogenic Brain Exposure Abstract Psilocybin, the phosphorylated prodrug of psilocin, holds therapeutic promise across a range of neuropsychiatric conditions, yet its clinical utility is co... |
PMC6481997 | core_pubmed_pmc | Pharmacokinetics, Safety, and Efficacy of an Allometric Miltefosine Regimen for the Treatment of Visceral Leishmaniasis in Eastern African Children: An Open-label, Phase II Clinical Trial | Pharmacokinetics, Safety, and Efficacy of an Allometric Miltefosine Regimen for the Treatment of Visceral Leishmaniasis in Eastern African Children: An Open-label, Phase II Clinical Trial Abstract Abstract Background Convenient, safe, and effective treatments for visceral leishmaniasis in Eastern African children are l... |
PMC10681487 | core_pubmed_pmc | How large must a dose‐optimization trial be? | How large must a dose‐optimization trial be? Abstract Abstract Recently promulgated Draft Guidance from the US Food and Drug Administration Oncology Center of Excellence (OCE) recommends randomized, parallel dose–response trials for “dose optimization,” but with vaguely stated aims that engage none of the statistical p... |
PMC4359179 | core_pubmed_pmc | Saliva Versus Plasma Bioequivalence of Rusovastatin in Humans: Validation of Class III Drugs of the Salivary Excretion Classification System | Saliva Versus Plasma Bioequivalence of Rusovastatin in Humans: Validation of Class III Drugs of the Salivary Excretion Classification System Abstract Abstract Bioequivalence of rusovastatin in healthy human volunteers was done using saliva and plasma matrices in order to investigate the robustness of using saliva inste... |
PMC5883402 | core_pubmed_pmc | SPIRE – combining SGI-110 with cisplatin and gemcitabine chemotherapy for solid malignancies including bladder cancer: study protocol for a phase Ib/randomised IIa open label clinical trial | SPIRE – combining SGI-110 with cisplatin and gemcitabine chemotherapy for solid malignancies including bladder cancer: study protocol for a phase Ib/randomised IIa open label clinical trial Abstract Abstract Background Urothelial bladder cancer (UBC) accounts for 10,000 new diagnoses and 5000 deaths annually in the UK ... |
PMC12379323 | core_pubmed_pmc | Effects of simultaneous administration of local anesthetics on seizure induced threshold: an experimental study in rats | Effects of simultaneous administration of local anesthetics on seizure induced threshold: an experimental study in rats Abstract Abstract Background The effect of the simultaneous administration of local anesthetics, whether synergistic, additive, or antagonistic, has not yet been established. This study investigated t... |
PMC7115413 | core_pubmed_pmc | Enfuvirtide−PEG conjugate: A potent HIV fusion inhibitor with improved pharmacokinetic properties | Enfuvirtide−PEG conjugate: A potent HIV fusion inhibitor with improved pharmacokinetic properties Abstract Enfuvirtide (ENF) is a clinically used peptide drug for the treatment of HIV infections, but its poor pharmacokinetic profile ( T 1/2 = 1.5 h in rats) and low aqueous solubility make the therapy expensive and inco... |
PMC10264951 | core_pubmed_pmc | Developing a mechanistic understanding of the nonlinear pharmacokinetics of letermovir and prospective drug interaction with everolimus using physiological‐based pharmacokinetic modeling | Developing a mechanistic understanding of the nonlinear pharmacokinetics of letermovir and prospective drug interaction with everolimus using physiological‐based pharmacokinetic modeling Abstract Abstract Letermovir is approved for use in cytomegalovirus‐seropositive hematopoietic stem cell transplant recipients and is... |
PMC12001667 | core_pubmed_pmc | A Modern Overview of the Potential Therapeutic Effects of Psilocybin in the Treatment of Depressive Disorders, Treatment-Resistant Depression, and End-of-Life Distress | A Modern Overview of the Potential Therapeutic Effects of Psilocybin in the Treatment of Depressive Disorders, Treatment-Resistant Depression, and End-of-Life Distress Abstract The purpose of this review is to provide a comprehensive overview of the current findings and data on the therapeutic effects of psilocybin, a ... |
PMC10377123 | core_pubmed_pmc | Pharmacological Potential of Betulin as a Multitarget Compound | Pharmacological Potential of Betulin as a Multitarget Compound Abstract Abstract Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has pro... |
PMC8399770 | core_pubmed_pmc | The Manifesto of Pharmacoenosis: Merging HIV Pharmacology into Pathocoenosis and Syndemics in Developing Countries | The Manifesto of Pharmacoenosis: Merging HIV Pharmacology into Pathocoenosis and Syndemics in Developing Countries Abstract Pathocoenosis and syndemics theories have emerged in the last decades meeting the frequent need of better understanding interconnections and reciprocal influences that coexistent communicable and ... |
PMC7794570 | core_pubmed_pmc | Understanding the antiviral effects of RNAi-based therapy in HBeAg-positive chronic hepatitis B infection | Understanding the antiviral effects of RNAi-based therapy in HBeAg-positive chronic hepatitis B infection Abstract The RNA interference (RNAi) drug ARC-520 was shown to be effective in reducing serum hepatitis B virus (HBV) DNA, hepatitis B e antigen (HBeAg) and hepatitis B surface antigen (HBsAg) in HBeAg-positive pat... |
PMC5108498 | core_pubmed_pmc | Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats | Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats Abstract The aim of the study was to improve the oral absorption of the compound 25-OCH 3 -PPD with poor hydrophilicity and lipo... |
PMC10912931 | core_pubmed_pmc | A multi-center interventional study to assess pharmacokinetics, effectiveness, and tolerability of prolonged-release tacrolimus after pediatric kidney transplantation: study protocol for a prospective, open-label, randomized, two-phase, two-sequence, single dose, crossover, phase III b trial | A multi-center interventional study to assess pharmacokinetics, effectiveness, and tolerability of prolonged-release tacrolimus after pediatric kidney transplantation: study protocol for a prospective, open-label, randomized, two-phase, two-sequence, single dose, crossover, phase III b trial Abstract Abstract Backgroun... |
PMC5849192 | core_pubmed_pmc | First-in-human phase 1 study of the BTK inhibitor GDC-0853 in relapsed or refractory B-cell NHL and CLL | First-in-human phase 1 study of the BTK inhibitor GDC-0853 in relapsed or refractory B-cell NHL and CLL Abstract Abstract GDC-0853 is a selective, reversible, and non-covalent inhibitor of Bruton’s tyrosine kinase (BTK) that does not require interaction with the Cys481 residue for activity. In this first-in-human phase... |
PMC9964742 | core_pubmed_pmc | An Overview of Physiologically-Based Pharmacokinetic Models for Forensic Science | An Overview of Physiologically-Based Pharmacokinetic Models for Forensic Science Abstract Abstract A physiologically-based pharmacokinetic (PBPK) model represents the structural components of the body with physiologically relevant compartments connected via blood flow rates described by mathematical equations to determ... |
PMC8426283 | core_pubmed_pmc | A resource of high-quality and versatile nanobodies for drug delivery | A resource of high-quality and versatile nanobodies for drug delivery Abstract Summary Therapeutic and diagnostic efficacies of small biomolecules and chemical compounds are hampered by suboptimal pharmacokinetics. Here, we developed a repertoire of robust and high-affinity antihuman serum albumin nanobodies (Nb HSA ) ... |
PMC4382528 | core_pubmed_pmc | An Update on Pharmacological, Pharmacokinetic Properties and Drug–Drug Interactions of Rotigotine Transdermal System in Parkinson’s Disease and Restless Legs Syndrome | An Update on Pharmacological, Pharmacokinetic Properties and Drug–Drug Interactions of Rotigotine Transdermal System in Parkinson’s Disease and Restless Legs Syndrome Abstract This narrative review reports on the pharmacological and pharmacokinetic properties of rotigotine, a non-ergolinic D 3 /D 2 /D 1 dopamine recept... |
PMC12844840 | core_pubmed_pmc | Mathematical Modeling in Drug Metabolism and Pharmacokinetics: Correct In Vitro, Not Always Valid In Vivo | Mathematical Modeling in Drug Metabolism and Pharmacokinetics: Correct In Vitro, Not Always Valid In Vivo Abstract Abstract Background/Objectives : Chemical and metabolic kinetics have historically been derived from mass balance differential equations expressed in terms of amounts, and this framework was later extended... |
PMC11985910 | core_pubmed_pmc | Targeting vascular adhesion protein-1 and myeloperoxidase with a dual inhibitor SNT-8370 in preclinical models of inflammatory disease | Targeting vascular adhesion protein-1 and myeloperoxidase with a dual inhibitor SNT-8370 in preclinical models of inflammatory disease Abstract Inflammatory diseases are a major source of morbidity and mortality world-wide, the pathogenesis of which are characterised by the interplay of key pro-inflammatory and oxidati... |
PMC4282435 | core_pubmed_pmc | The effects of alcohol on the pharmacokinetics and pharmacodynamics of the selective mu-opioid receptor antagonist GSK1521498 in healthy subjects | The effects of alcohol on the pharmacokinetics and pharmacodynamics of the selective mu-opioid receptor antagonist GSK1521498 in healthy subjects Abstract Abstract The mu-opioid system has a key role in hedonic and motivational processes critical to substance addiction. However, existing mu-opioid antagonists have had ... |
PMC10427764 | core_pubmed_pmc | Influence of the microbiota on the effectiveness and toxicity of oncological therapies, with a focus on chemotherapy | Influence of the microbiota on the effectiveness and toxicity of oncological therapies, with a focus on chemotherapy Abstract Abstract Recent studies have highlighted a possible correlation between microbiota composition and the pathogenesis of various oncological diseases. Also, many bacterial groups are now directly ... |
PMC6656940 | core_pubmed_pmc | Evaluation of the Drug–Drug Interaction Potential of Acalabrutinib and Its Active Metabolite, ACP ‐5862, Using a Physiologically‐Based Pharmacokinetic Modeling Approach | Evaluation of the Drug–Drug Interaction Potential of Acalabrutinib and Its Active Metabolite, ACP ‐5862, Using a Physiologically‐Based Pharmacokinetic Modeling Approach Abstract Acalabrutinib, a selective, covalent Bruton tyrosine kinase inhibitor, is a CYP 3A substrate and weak CYP 3A/ CYP 2C8 inhibitor. A physiologic... |
PMC9902179 | core_pubmed_pmc | A Double-blind, Placebo-controlled, Randomized, Single Ascending, and Multiple Dose Phase 1 Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral Dose Isomyosamine Capsules in Healthy Adult Subjects | A Double-blind, Placebo-controlled, Randomized, Single Ascending, and Multiple Dose Phase 1 Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral Dose Isomyosamine Capsules in Healthy Adult Subjects Abstract Background Aging is tightly linked to chronic disease, frailty, and death. Multi-morbidity, d... |
PMC12081248 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling supports investigation of potential drug-drug interactions in the pre- and early post-hematopoietic stem cell transplantation stages | Physiologically based pharmacokinetic modeling supports investigation of potential drug-drug interactions in the pre- and early post-hematopoietic stem cell transplantation stages Abstract Introduction Drug-drug interactions (DDIs) are an important issue in medication safety and a potential cause of adverse drug events... |
PMC12777811 | core_pubmed_pmc | Cannabidiol lymphatic transport after oral administration assessed using a novel thoracic lymph duct cannulated conscious pig model | Cannabidiol lymphatic transport after oral administration assessed using a novel thoracic lymph duct cannulated conscious pig model Abstract ABSTRACT Lymphatic transport of drugs after oral administration is an important physiological process in highly lipophilic compounds, such as cannabidiol (CBD). The majority of ly... |
PMC5498655 | core_pubmed_pmc | Virtual Clinical Studies to Examine the Probability Distribution of the AUC at Target Tissues Using Physiologically-Based Pharmacokinetic Modeling: Application to Analyses of the Effect of Genetic Polymorphism of Enzymes and Transporters on Irinotecan Induced Side Effects | Virtual Clinical Studies to Examine the Probability Distribution of the AUC at Target Tissues Using Physiologically-Based Pharmacokinetic Modeling: Application to Analyses of the Effect of Genetic Polymorphism of Enzymes and Transporters on Irinotecan Induced Side Effects Abstract Abstract Purpose To establish a physio... |
PMC10864214 | core_pubmed_pmc | Efficacy and safety of stapokibart (CM310) in uncontrolled seasonal allergic rhinitis (MERAK): an investigator-initiated, placebo-controlled, randomised, double-blind, phase 2 trial | Efficacy and safety of stapokibart (CM310) in uncontrolled seasonal allergic rhinitis (MERAK): an investigator-initiated, placebo-controlled, randomised, double-blind, phase 2 trial Abstract Summary Background There is no trial to assess the benefits of periodically using biologics during the pollen season in patients ... |
PMC3468918 | core_pubmed_pmc | Translocating the blood-brain barrier using electrostatics | Translocating the blood-brain barrier using electrostatics Abstract Abstract Mammalian cell membranes regulate homeostasis, protein activity, and cell signaling. The charge at the membrane surface has been correlated with these key events. Although mammalian cells are known to be slightly anionic, quantitative informat... |
PMC8397907 | core_pubmed_pmc | Staphylococcus haemolyticus meningitis and bacteremia in an allogenic stem cell transplant patient | Staphylococcus haemolyticus meningitis and bacteremia in an allogenic stem cell transplant patient Abstract Abstract Staphylococcus haemolyticus is a rare cause of bacterial meningitis and most commonly occurs as a nosocomial infection in patients’ post-neurosurgery. We report a patient post-allogenic stem cell transpl... |
PMC3955335 | core_pubmed_pmc | Selective androgen receptor modulators for the treatment of late onset male hypogonadism | Selective androgen receptor modulators for the treatment of late onset male hypogonadism Abstract Abstract Several testosterone preparations are used in the treatment of hypogonadism in the ageing male. These therapies differ in their convenience, flexibility, regional availability and expense but share their pharmacok... |
PMC10975960 | core_pubmed_pmc | Pharmacokinetic Modeling of Bepotastine for Determination of Optimal Dosage Regimen in Pediatric Patients with Allergic Rhinitis or Urticaria | Pharmacokinetic Modeling of Bepotastine for Determination of Optimal Dosage Regimen in Pediatric Patients with Allergic Rhinitis or Urticaria Abstract Bepotastine, a second-generation antihistamine for allergic rhinitis and urticaria, is widely used in all age groups but lacks appropriate dosing guidelines for pediatri... |
PMC10609273 | core_pubmed_pmc | Radiosynthesis and Early Evaluation of a Positron Emission Tomography Imaging Probe [ 18 F]AGAL Targeting Alpha-Galactosidase A Enzyme for Fabry Disease | Radiosynthesis and Early Evaluation of a Positron Emission Tomography Imaging Probe [ 18 F]AGAL Targeting Alpha-Galactosidase A Enzyme for Fabry Disease Abstract Abstract Success of gene therapy relies on the durable expression and activity of transgene in target tissues. In vivo molecular imaging approaches using posi... |
PMC4551560 | core_pubmed_pmc | Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment | Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment Abstract Abstract Chemokine receptors belong to the class of G protein-coupled receptors and are important in the host defense against infections and inflammation. However, aberra... |
PMC8866828 | core_pubmed_pmc | Pharmacogenetics in Primary Headache Disorders | Pharmacogenetics in Primary Headache Disorders Abstract Abstract Primary headache disorders, such as migraine, tension-type headache (TTH), and cluster headache, belong to the most common neurological disorders affecting a high percentage of people worldwide. Headache induces a high burden for the affected individuals ... |
PMC3321555 | core_pubmed_pmc | Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part I: Program Implementation and Lessons Learned | Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part I: Program Implementation and Lessons Learned Abstract Abstract Concerns have been raised regarding environmental manganese exposure since high exposures have been associated with neurological disorders. The USA Environmental Protection Agency... |
PMC3842690 | core_pubmed_pmc | Main considerable factors for correct laboratory test interpretation under DOA treatment | Main considerable factors for correct laboratory test interpretation under DOA treatment Abstract Summary To avoid misinterpretation and mismanagement clinicians should be aware of the interference of new direct oral anticoagulants (DOA) on coagulation assays. A variety of oral anticoagulants targeting specific coagula... |
PMC6413453 | core_pubmed_pmc | Long-term relationship between everolimus blood concentration and clinical outcomes in Japanese patients with metastatic renal cell carcinoma: a prospective study | Long-term relationship between everolimus blood concentration and clinical outcomes in Japanese patients with metastatic renal cell carcinoma: a prospective study Abstract Background Everolimus is an oral inhibitor of mammalian target of rapamycin, approved for metastatic renal cell carcinoma (mRCC). Recently, personal... |
PMC9266550 | core_pubmed_pmc | The 2-hydroxy-3-(4-aryl-1-piperazinyl)propyl Phthalimide Derivatives as Prodrugs—Spectroscopic and Theoretical Binding Studies with Plasma Proteins | The 2-hydroxy-3-(4-aryl-1-piperazinyl)propyl Phthalimide Derivatives as Prodrugs—Spectroscopic and Theoretical Binding Studies with Plasma Proteins Abstract Abstract Many publications in databases deal with the interactions of new drugs with albumin. However, it is not only albumin that is responsible for binding pharm... |
PMC11307027 | core_pubmed_pmc | Impact of Physical Exercise on Levodopa Therapy Across Parkinson’s Disease Stages | Impact of Physical Exercise on Levodopa Therapy Across Parkinson’s Disease Stages Abstract Abstract Background: Levodopa is the gold standard of treatment in Parkinson’s disease (PD). Its clinical effect changes as the disease progresses. Wearing off is a frequent first manifestation of motor fluctuations. Some patient... |
PMC5792431 | core_pubmed_pmc | Anti-Rift Valley fever virus activity in vitro , pre-clinical pharmacokinetics and oral bioavailability of benzavir-2, a broad-acting antiviral compound | Anti-Rift Valley fever virus activity in vitro , pre-clinical pharmacokinetics and oral bioavailability of benzavir-2, a broad-acting antiviral compound Abstract Rift Valley fever virus (RVFV) is a mosquito-borne hemorrhagic fever virus affecting both humans and animals with severe morbidity and mortality and is classi... |
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