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PMC10987370 | core_pubmed_pmc | Superior bioavailability of the calcium salt form of β-hydroxy-β-methylbutyrate compared with the free acid form | Superior bioavailability of the calcium salt form of β-hydroxy-β-methylbutyrate compared with the free acid form Abstract We investigated the bioavailability of the calcium salt (HMB-Ca) and the free acid (HMB-FA) forms of β-hydroxy-β-methylbutyrate (HMB). Sixteen young individuals received the following treatments on ... |
PMC8061644 | core_pubmed_pmc | Tumescent Anesthesia for Dermatosurgical Procedures Other Than Liposuction | Tumescent Anesthesia for Dermatosurgical Procedures Other Than Liposuction Abstract Abstract Context: Tumescent local anesthesia is a form of local anesthesia, which is a technique in which a dilute local anesthetic solution is injected into the subcutaneous tissue until it becomes firm and tense. Originally developed ... |
PMC8263851 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of single- and multiple-dose intravenous ceftobiprole in healthy Chinese participants | Pharmacokinetics, pharmacodynamics, and safety of single- and multiple-dose intravenous ceftobiprole in healthy Chinese participants Abstract Background Ceftobiprole is a novel β-lactam cephalosporin with activity against Gram-positive and -negative bacteria. The aim of the present study was to investigate the pharmaco... |
PMC11881578 | core_pubmed_pmc | Pharmacokinetics and bioequivalence of a molnupiravir tablet formulation compared with the molnupiravir capsule formulation in healthy adult participants—a randomized, open-label, three-period, crossover study | Pharmacokinetics and bioequivalence of a molnupiravir tablet formulation compared with the molnupiravir capsule formulation in healthy adult participants—a randomized, open-label, three-period, crossover study Abstract ABSTRACT Molnupiravir, a prodrug of β-D-N 4 -hydroxycytidine (NHC), is administered orally as four 20... |
PMC11656427 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling to predict the effect of risperidone on aripiprazole pharmacokinetics in subjects with different CYP2D6 genotypes and individuals with hepatic impairment | Physiologically based pharmacokinetic modeling to predict the effect of risperidone on aripiprazole pharmacokinetics in subjects with different CYP2D6 genotypes and individuals with hepatic impairment Abstract Abstract Background: Aripiprazole and risperidone, widely used atypical antipsychotics, are commonly adjunctiv... |
PMC5933357 | core_pubmed_pmc | Pharmacokinetic characteristics of telaprevir in healthy Korean male subjects and comparisons with Japanese | Pharmacokinetic characteristics of telaprevir in healthy Korean male subjects and comparisons with Japanese Abstract Introduction Telaprevir, a reversible selective inhibitor of viral protease and a potential blocker of viral replication, is indicated for the treatment of hepatitis C virus genotype 1 infection. In this... |
PMC10359578 | core_pubmed_pmc | Dose escalation randomised study of efmarodocokin alfa in healthy volunteers and patients with ulcerative colitis | Dose escalation randomised study of efmarodocokin alfa in healthy volunteers and patients with ulcerative colitis Abstract Background The interleukin-22 cytokine (IL-22) has demonstrated efficacy in preclinical colitis models with non-immunosuppressive mechanism of action. Efmarodocokin alfa (UTTR1147A) is a fusion pro... |
PMC5787161 | core_pubmed_pmc | Effect of Intravenous Administration of Cobalt Chloride to Horses on Clinical and Hemodynamic Variables | Effect of Intravenous Administration of Cobalt Chloride to Horses on Clinical and Hemodynamic Variables Abstract Abstract Background Cobalt chloride (CoCl 2 ) is administered to racehorses to enhance performance. The purpose of this study was to evaluate the clinical, cardiovascular, and endocrine effects of parenteral... |
PMC10100262 | core_pubmed_pmc | Synthesis of a Bifunctional Cross‐Bridged Chelating Agent, Peptide Conjugation, and Comparison of 68 Ga Labeling and Complex Stability Characteristics with Established Chelators | Synthesis of a Bifunctional Cross‐Bridged Chelating Agent, Peptide Conjugation, and Comparison of 68 Ga Labeling and Complex Stability Characteristics with Established Chelators Abstract Abstract [ 68 Ga]Ga 3+ can be introduced into receptor‐specific peptidic carriers via different chelators to obtain radiotracers for ... |
PMC3567458 | core_pubmed_pmc | A Detailed Physiologically Based Model to Simulate the Pharmacokinetics and Hormonal Pharmacodynamics of Enalapril on the Circulating Endocrine Renin-Angiotensin-Aldosterone System | A Detailed Physiologically Based Model to Simulate the Pharmacokinetics and Hormonal Pharmacodynamics of Enalapril on the Circulating Endocrine Renin-Angiotensin-Aldosterone System Abstract Abstract The renin-angiotensin-aldosterone system (RAAS) plays a key role in the pathogenesis of cardiovascular disorders includin... |
PMC11552514 | core_pubmed_pmc | Optimizing Pharmacological and Immunological Properties of Therapeutic Proteins Through PEGylation: Investigating Key Parameters and Their Impact | Optimizing Pharmacological and Immunological Properties of Therapeutic Proteins Through PEGylation: Investigating Key Parameters and Their Impact Abstract Abstract Protein PEGylation represents a significant technological advancement in the development of protein-based therapeutics and is widely used to reduce immunoge... |
PMC9145467 | core_pubmed_pmc | Cost-Effectiveness of Therapeutic Drug Monitoring of Anti-TNF Therapy in Inflammatory Bowel Disease: A Systematic Review | Cost-Effectiveness of Therapeutic Drug Monitoring of Anti-TNF Therapy in Inflammatory Bowel Disease: A Systematic Review Abstract Abstract Infliximab and adalimumab are monoclonal antibodies against tumor necrosis factor (anti-TNF) used to manage inflammatory bowel disease (IBD). Therapeutic Drug Monitoring (TDM) has b... |
PMC8828610 | core_pubmed_pmc | Survey of tumorigenic sensitivity in 6-month rasH2-Tg mice studies compared with 2-year rodent assays | Survey of tumorigenic sensitivity in 6-month rasH2-Tg mice studies compared with 2-year rodent assays Abstract The pharmacokinetic endpoint of a 25-fold increase in human exposure is one of the specified criteria for high-dose selection for 2-year carcinogenicity studies in rodents according to ICH S1C(R2). However, th... |
PMC7774078 | core_pubmed_pmc | Contribution of Uptake and Efflux Transporters to Oral Pharmacokinetics of Furosemide | Contribution of Uptake and Efflux Transporters to Oral Pharmacokinetics of Furosemide Abstract Furosemide is a widely used diuretic for treating excessive fluid accumulation caused by disease conditions like heart failure and liver cirrhosis. Furosemide tablet formulation exhibits variable pharmacokinetics (PK) with bi... |
PMC4051715 | core_pubmed_pmc | Poly(styrene)-b-poly(DL-lactide) copolymer-based nanoparticles for anticancer drug delivery | Poly(styrene)-b-poly(DL-lactide) copolymer-based nanoparticles for anticancer drug delivery Abstract Poly(styrene)-b-poly(DL-lactide) (PS-PDLLA) copolymer-based nanoparticles (NPs) of a narrow size distribution, negative zeta potential, and spherical shape were fabricated for the delivery of docetaxel (DCT). The partic... |
PMC4521485 | core_pubmed_pmc | Measuring windows of selection for anti-malarial drug treatments | Measuring windows of selection for anti-malarial drug treatments Abstract Background The long half-lives of malaria ‘partner’ drugs are a potent force selecting for drug resistance. Clinical trials can quantify this effect by estimating a window of selection (WoS), defined as the amount of time post-treatment when drug... |
PMC12742193 | core_pubmed_pmc | Pretargeted brain PET imaging reveals amyloid-β pathology using a TCO-modified antibody and a fluorine-18-labeled tetrazine | Pretargeted brain PET imaging reveals amyloid-β pathology using a TCO-modified antibody and a fluorine-18-labeled tetrazine Abstract Abstract Background Antibody-based positron emission tomography (PET) imaging holds great promise for visualizing disease-related proteins in the brain. However, its clinical utility is l... |
PMC11724663 | core_pubmed_pmc | Development of Solid Self-Nanoemulsifying Drug Delivery System of Rhein to Improve Biopharmaceutical Performance: Physiochemical Characterization, and Pharmacokinetic Evaluation | Development of Solid Self-Nanoemulsifying Drug Delivery System of Rhein to Improve Biopharmaceutical Performance: Physiochemical Characterization, and Pharmacokinetic Evaluation Abstract Abstract Introduction Rhein, a natural bioactive lipophilic compound with numerous pharmacological activities, faces limitations in c... |
PMC11320734 | core_pubmed_pmc | A Highly Potent, Orally Bioavailable Pyrazole-Derived Cannabinoid CB2 Receptor- Selective Full Agonist for In Vivo Studies | A Highly Potent, Orally Bioavailable Pyrazole-Derived Cannabinoid CB2 Receptor- Selective Full Agonist for In Vivo Studies Abstract Abstract The cannabinoid CB2 receptor (CB2R) is a potential therapeutic target for distinct forms of tissue injury and inflammatory diseases. To thoroughly investigate the role of CB2R in ... |
PMC9055260 | core_pubmed_pmc | An unexpected single crystal structure of nickel(II) complex: Spectral, DFT, NLO, magnetic and molecular docking studies | An unexpected single crystal structure of nickel(II) complex: Spectral, DFT, NLO, magnetic and molecular docking studies Abstract Abstract This work explores the study of a synthesized nickel complex as a possible inhibitor against the main protease (Mpro) of the recent emerging coronavirus disease (COVID-19). Overall,... |
PMC10486870 | core_pubmed_pmc | Effect of Xylazine on Pharmacokinetics and Physiological Efficacy of Intravenous Carprofen in Castrated Goats Kids | Effect of Xylazine on Pharmacokinetics and Physiological Efficacy of Intravenous Carprofen in Castrated Goats Kids Abstract Simple Summary The castration of male goats is one of the most common livestock management procedures to reduce aggression and sexual behavior by lowering testosterone levels, prevent unwanted pre... |
PMC8558816 | core_pubmed_pmc | MTORC1 signaling as a biomarker in major depressive disorder and its pharmacological modulation by novel rapid-acting antidepressants | MTORC1 signaling as a biomarker in major depressive disorder and its pharmacological modulation by novel rapid-acting antidepressants Abstract Major depressive disorder (MDD) is a multifactorial psychiatric disorder with obscure pathophysiology. A biomarker-based approach in combination with standardized interview-base... |
PMC9862396 | core_pubmed_pmc | Development of a Physiologically Based Pharmacokinetic Model for Tegoprazan: Application for the Prediction of Drug–Drug Interactions with CYP3A4 Perpetrators | Development of a Physiologically Based Pharmacokinetic Model for Tegoprazan: Application for the Prediction of Drug–Drug Interactions with CYP3A4 Perpetrators Abstract Tegoprazan is a novel potassium-competitive acid blocker (P-CAB) developed by CJ Healthcare (Korea) for the treatment of gastroesophageal reflux disease... |
PMC9145021 | core_pubmed_pmc | Brain-Targeted Intranasal Delivery of Zotepine Microemulsion: Pharmacokinetics and Pharmacodynamics | Brain-Targeted Intranasal Delivery of Zotepine Microemulsion: Pharmacokinetics and Pharmacodynamics Abstract Abstract The purpose of our study was to improve the solubility, bioavailability, and efficacy of zotepine (ZTP) by brain-targeted intranasal delivery of microemulsion (ME) and its physicochemical properties, th... |
PMC11587652 | core_pubmed_pmc | Inhalation of itraconazole mitigates bleomycin-induced lung fibrosis via regulating SPP1 and C3 signaling pathway pivotal in the interaction between phagocytic macrophages and diseased fibroblasts | Inhalation of itraconazole mitigates bleomycin-induced lung fibrosis via regulating SPP1 and C3 signaling pathway pivotal in the interaction between phagocytic macrophages and diseased fibroblasts Abstract Background Idiopathic pulmonary fibrosis (IPF) stands as a significant contributor to global mortality rates. Pres... |
PMC6033159 | core_pubmed_pmc | Individualized immunoglobulin therapy in chronic immune‐mediated peripheral neuropathies * | Individualized immunoglobulin therapy in chronic immune‐mediated peripheral neuropathies * Abstract Abstract Despite the well‐recognized importance of immunoglobulin therapy individualization during the treatment of chronic inflammatory demyelinating polyneuropathy (CIDP), the pathway to best achieve optimization is un... |
PMC10807299 | core_pubmed_pmc | Intranasal Naloxone Repeat Dosing Strategies and Fentanyl Overdose | Intranasal Naloxone Repeat Dosing Strategies and Fentanyl Overdose Abstract Key Points Question How long does it take for different repeat dosing strategies of intranasal naloxone to increase naloxone plasma concentration after fentanyl overdose? Findings This crossover randomized clinical trial included 21 healthy par... |
PMC4058004 | core_pubmed_pmc | Concomitant use of tamoxifen and endoxifen in postmenopausal early breast cancer: prediction of plasma levels by physiologically-based pharmacokinetic modeling | Concomitant use of tamoxifen and endoxifen in postmenopausal early breast cancer: prediction of plasma levels by physiologically-based pharmacokinetic modeling Abstract Abstract Purpose To overcome cytochrome P450 2D6 (CYP2D6) mediated tamoxifen resistance in postmenopausal early breast cancer, CYP2D6 phenotype-adjuste... |
PMC12114923 | core_pubmed_pmc | Nanostructured Lipoxin A4: Understanding Its Biological Behavior and Impact on Alzheimer’s Disease (Proof of Concept) | Nanostructured Lipoxin A4: Understanding Its Biological Behavior and Impact on Alzheimer’s Disease (Proof of Concept) Abstract Background/Objectives : Lipoxins, particularly Lipoxin A4 (LXA4), are endogenous lipid mediators with potent anti-inflammatory and pro-resolving properties, making them promising candidates for... |
PMC6510352 | core_pubmed_pmc | Influence of concomitant medication on plasma concentration of amiodarone in patients with atrial fibrillation - a pilot study | Influence of concomitant medication on plasma concentration of amiodarone in patients with atrial fibrillation - a pilot study Abstract Background Although amiodarone is a drug with many side effects, it is one of the most commonly used drugs in the treatment and prophylaxis of supraventricular and ventricular arrhythm... |
PMC8540251 | core_pubmed_pmc | In-Vitro Efficacy of Cefiderocol in Carbapenem-Non-Susceptible Gram-Negative Bacilli of Different Genotypes in Sub-Region of North Rhine Westphalia, Germany | In-Vitro Efficacy of Cefiderocol in Carbapenem-Non-Susceptible Gram-Negative Bacilli of Different Genotypes in Sub-Region of North Rhine Westphalia, Germany Abstract Abstract In the last two decades, the worldwide dissemination of multidrug-resistant Gram-negative bacteria (MDR-GNB) has continued. Therapy options for s... |
PMC10725262 | core_pubmed_pmc | Population pharmacokinetics of molnupiravir in adults with COVID ‐19: Lack of clinically important exposure variation across individuals | Population pharmacokinetics of molnupiravir in adults with COVID ‐19: Lack of clinically important exposure variation across individuals Abstract Abstract Effective antiviral treatments for coronavirus disease 2019 (COVID‐19) are needed to reduce the morbidity and mortality associated with severe acute respiratory synd... |
PMC12355014 | core_pubmed_pmc | Folinic Acid Prophylaxis and Dose Adjustments Enable Safe Treatment with Pemetrexed in Patients with Renal Impairment | Folinic Acid Prophylaxis and Dose Adjustments Enable Safe Treatment with Pemetrexed in Patients with Renal Impairment Abstract Abstract Pemetrexed is a cornerstone in chemo(immunotherapy) of non‐small cell lung cancer and mesothelioma; however, it is contraindicated in patients with renal impairment due to severe toxic... |
PMC8251533 | core_pubmed_pmc | Relationship Between Oral Semaglutide Tablet Erosion and Pharmacokinetics: A Pharmacoscintigraphic Study | Relationship Between Oral Semaglutide Tablet Erosion and Pharmacokinetics: A Pharmacoscintigraphic Study Abstract Abstract Semaglutide, a glucagon‐like peptide‐1 (GLP‐1) analogue, has been coformulated in a tablet with the absorption enhancer, sodium N‐(8‐[2‐hydroxybenzoyl] amino) caprylate (SNAC). We investigated tabl... |
PMC4444108 | core_pubmed_pmc | Xanthohumol Inhibits Notch Signaling and Induces Apoptosis in Hepatocellular Carcinoma | Xanthohumol Inhibits Notch Signaling and Induces Apoptosis in Hepatocellular Carcinoma Abstract Despite improvement in therapeutic strategies, median survival in advanced hepatocellular carcinoma (HCC) remains less than one year. Therefore, molecularly targeted compounds with less toxic profiles are needed. Xanthohumol... |
PMC12212770 | core_pubmed_pmc | Selection of anesthetic agents for obstructive jaundice: An update for anesthesiologists | Selection of anesthetic agents for obstructive jaundice: An update for anesthesiologists Abstract Abstract Obstructive jaundice is induced by complete or partial obstruction of the common bile duct, which causes bile to overflow from the digestive system into the circulatory system. Clinically, such patients often requ... |
PMC7662460 | core_pubmed_pmc | Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects | Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects Abstract Abstract In the golden age of pharmaceutical nanocarriers, we are witnessing a maturation stage of the original concepts and ideas. There is no doubt that nanoformulations are extremely valuable tools for drug delivery a... |
PMC12621564 | core_pubmed_pmc | Rivaroxaban in Chinese children with giant coronary artery aneurysms after Kawasaki disease | Rivaroxaban in Chinese children with giant coronary artery aneurysms after Kawasaki disease Abstract Abstract Background Data on the use of rivaroxaban in children with giant coronary artery aneurysm (GCAA) after Kawasaki disease (KD) remain limited. Objectives This study evaluated the feasibility of rivaroxaban in Chi... |
PMC11477000 | core_pubmed_pmc | Enantioselective Binding of Proton Pump Inhibitors to Alpha1-Acid Glycoprotein and Human Serum Albumin—A Chromatographic, Spectroscopic, and In Silico Study | Enantioselective Binding of Proton Pump Inhibitors to Alpha1-Acid Glycoprotein and Human Serum Albumin—A Chromatographic, Spectroscopic, and In Silico Study Abstract Abstract The enantioselective binding of three proton pump inhibitors (PPIs)—omeprazole, rabeprazole, and lansoprazole—to two key plasma proteins, α1-acid... |
PMC11787235 | core_pubmed_pmc | Population Pharmacokinetic Modeling to Support Trofinetide Dosing for the Treatment of Rett Syndrome | Population Pharmacokinetic Modeling to Support Trofinetide Dosing for the Treatment of Rett Syndrome Abstract Introduction Oral trofinetide administered using a body weight-banded dosing regimen was approved in the US for the treatment of Rett syndrome (RTT) in patients aged ≥ 2 years. This approval was principally bas... |
PMC2939789 | core_pubmed_pmc | Open-label, phase I dose-escalation study of sodium selenate, a novel activator of PP2A, in patients with castration-resistant prostate cancer | Open-label, phase I dose-escalation study of sodium selenate, a novel activator of PP2A, in patients with castration-resistant prostate cancer Abstract Background: Angiogenesis is fundamental to the progression of many solid tumours including prostate cancer. Sodium selenate is a small, water-soluble, orally bioavailab... |
PMC10295794 | core_pubmed_pmc | Pharmacokinetic Analysis of Zonarol, a Marine Algal Hydroquinone, in Mice Using HPLC with Fluorescence Detection | Pharmacokinetic Analysis of Zonarol, a Marine Algal Hydroquinone, in Mice Using HPLC with Fluorescence Detection Abstract Zonarol, which was discovered in the brown algae Dictyopteris undulata, has antibiotic, antioxidative, anti-inflammatory, and neuroprotective hydroquinone properties. Additionally, a daily treatment... |
PMC5189989 | core_pubmed_pmc | Metoprolol Dose Equivalence in Adult Men and Women Based on Gender Differences: Pharmacokinetic Modeling and Simulations | Metoprolol Dose Equivalence in Adult Men and Women Based on Gender Differences: Pharmacokinetic Modeling and Simulations Abstract Abstract Recent meta-analyses and publications over the past 15 years have provided evidence showing there are considerable gender differences in the pharmacokinetics of metoprolol. Througho... |
PMC10306236 | core_pubmed_pmc | Optimizing tuberculosis treatment efficacy: Comparing the standard regimen with Moxifloxacin-containing regimens | Optimizing tuberculosis treatment efficacy: Comparing the standard regimen with Moxifloxacin-containing regimens Abstract Abstract Tuberculosis (TB) continues to be one of the deadliest infectious diseases in the world, causing ~1.5 million deaths every year. The World Health Organization initiated an End TB Strategy t... |
PMC11947405 | core_pubmed_pmc | Accuracy and precision analyses of single-time-point dosimetry utilising physiologically-based pharmacokinetic modelling and non-linear mixed-effects modelling | Accuracy and precision analyses of single-time-point dosimetry utilising physiologically-based pharmacokinetic modelling and non-linear mixed-effects modelling Abstract Abstract Purpose The aim of this study was to investigate the accuracy and precision of single-time-point (STP) dosimetry using a physiologically-based... |
PMC12806149 | core_pubmed_pmc | Microbiota‐gut‐brain axis multi‐organ chip construction and applications in drug evaluation | Microbiota‐gut‐brain axis multi‐organ chip construction and applications in drug evaluation Abstract Abstract The theoretical framework of the microbiota‐gut‐brain axis (MGBA) elucidates the influence of gut microbiota (GM) on the central nervous system (CNS) and offers novel approaches for diagnosing and treating neur... |
PMC9700536 | core_pubmed_pmc | Clinical Validation of the Covariates Pharmacokinetic Model for Propofol in an Adult Population | Clinical Validation of the Covariates Pharmacokinetic Model for Propofol in an Adult Population Abstract Abstract Background and Objective Pharmacokinetic or pharmacokinetic-pharmacodynamic models have been instrumental in facilitating the clinical use of propofol in target-controlled infusion systems in anaesthetic pr... |
PMC8093904 | core_pubmed_pmc | In silico and in vitro screening of licensed antimalarial drugs for repurposing as inhibitors of hepatitis E virus | In silico and in vitro screening of licensed antimalarial drugs for repurposing as inhibitors of hepatitis E virus Abstract Abstract Hepatitis E virus (HEV) infection is emerging in Cameroon and represents one of the most common causes of acute hepatitis and jaundice. Moreover, earlier reports showed evidence of falcip... |
PMC11343830 | core_pubmed_pmc | Can we Predict Drug Excretion into Saliva? A Systematic Review and Analysis of Physicochemical Properties | Can we Predict Drug Excretion into Saliva? A Systematic Review and Analysis of Physicochemical Properties Abstract Abstract Background and Objectives Saliva is a patient-friendly matrix for therapeutic drug monitoring (TDM) but is infrequently used in routine care. This is due to the uncertainty of saliva-based TDM res... |
PMC12415080 | core_pubmed_pmc | Digital twins in nuclear medicine: A proposition of a modular pipeline for dosimetry protocol optimization in molecular radiotherapy | Digital twins in nuclear medicine: A proposition of a modular pipeline for dosimetry protocol optimization in molecular radiotherapy Abstract Introduction: Digital twins (DTs) are emerging tools for simulating and optimizing therapeutic protocols in personalized nuclear medicine. In this paper, we present a modular pip... |
PMC3731824 | core_pubmed_pmc | Influence of a priori Information, Designs, and Undetectable Data on Individual Parameters Estimation and Prediction of Hepatitis C Treatment Outcome | Influence of a priori Information, Designs, and Undetectable Data on Individual Parameters Estimation and Prediction of Hepatitis C Treatment Outcome Abstract Hepatitis C viral kinetic analysis based on nonlinear mixed effect models can be used to individualize treatment. For that purpose, it is necessary to obtain pre... |
PMC6723418 | core_pubmed_pmc | Pharmacokinetic Profile and Anti-Adhesive Effect of Oxaliplatin-PLGA Microparticle-Loaded Hydrogels in Rats for Colorectal Cancer Treatment | Pharmacokinetic Profile and Anti-Adhesive Effect of Oxaliplatin-PLGA Microparticle-Loaded Hydrogels in Rats for Colorectal Cancer Treatment Abstract Abstract Colorectal cancer (CRC) is one of the most malignant and fatal cancers worldwide. Although cytoreductive surgery combined with chemotherapy is considered a promis... |
PMC4055422 | core_pubmed_pmc | Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies | Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies Abstract Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from n... |
PMC4435089 | core_pubmed_pmc | A pharmacokinetic comparison of two voriconazole formulations and the effect of CYP2C19 polymorphism on their pharmacokinetic profiles | A pharmacokinetic comparison of two voriconazole formulations and the effect of CYP2C19 polymorphism on their pharmacokinetic profiles Abstract Abstract Purpose SYP-1018 is a lyophilized polymeric nanoparticle formulation of voriconazole that is under development for intravenous dosing. This study compared the pharmaco... |
PMC10227503 | core_pubmed_pmc | Genetic polymorphisms influencing deferasirox pharmacokinetics, efficacy, and adverse drug reactions: a systematic review and meta-analysis | Genetic polymorphisms influencing deferasirox pharmacokinetics, efficacy, and adverse drug reactions: a systematic review and meta-analysis Abstract Objective: Deferasirox is an iron-chelating agent prescribed to patients with iron overload. Due to the interindividual variability of deferasirox responses reported in va... |
PMC8041391 | core_pubmed_pmc | Clinical Pharmacology Regulatory Sciences in Drug Development and Precision Medicine: Current Status and Emerging Trends | Clinical Pharmacology Regulatory Sciences in Drug Development and Precision Medicine: Current Status and Emerging Trends Abstract Abstract In the regulatory setting, clinical pharmacology focuses on the impact of intrinsic and extrinsic factors on inter-patient and intra-subject variability in drug exposure and respons... |
PMC12823777 | core_pubmed_pmc | Examining the Reliability of Model‐Based Meta‐Analysis (MBMA) Outcomes: A Simulation Study | Examining the Reliability of Model‐Based Meta‐Analysis (MBMA) Outcomes: A Simulation Study Abstract ABSTRACT Model‐based meta‐analysis (MBMA) can be utilized to synthesize literature data and predict drug efficacy, particularly suitable for constructing external comparator arms for non‐randomized controlled trials (NRC... |
PMC9645377 | core_pubmed_pmc | A rotaxane-based platform for tailoring the pharmacokinetics of cancer-targeted radiotracers † | A rotaxane-based platform for tailoring the pharmacokinetics of cancer-targeted radiotracers † Abstract Abstract Radiolabelled monoclonal antibodies (mAbs) are a cornerstone of molecular diagnostic imaging and targeted radioimmunotherapy in nuclear medicine, but one of the major challenges in the field is to identify w... |
PMC11706430 | core_pubmed_pmc | Nonlinear mixed‐effects modeling as a method for causal inference to predict exposures under desired within‐subject dose titration schemes | Nonlinear mixed‐effects modeling as a method for causal inference to predict exposures under desired within‐subject dose titration schemes Abstract Abstract The ICH E9 (R1) guidance and the related estimand framework propose to clearly define and separate the clinical question of interest formulated as estimand from th... |
PMC8195421 | core_pubmed_pmc | High risk of early sub-therapeutic penicillin concentrations after intramuscular benzathine penicillin G injections in Ethiopian children and adults with rheumatic heart disease | High risk of early sub-therapeutic penicillin concentrations after intramuscular benzathine penicillin G injections in Ethiopian children and adults with rheumatic heart disease Abstract Abstract Introduction Intramuscular benzathine penicillin G (BPG) injections are a cornerstone of secondary prophylaxis to prevent ac... |
PMC11312558 | core_pubmed_pmc | Quantitative Analysis of the Effect of Neuromuscular Blockade on Motor-Evoked Potentials in Patients Undergoing Brain Tumor Removal Surgery: A Prospective, Single-Arm, Open-Label Observational Study | Quantitative Analysis of the Effect of Neuromuscular Blockade on Motor-Evoked Potentials in Patients Undergoing Brain Tumor Removal Surgery: A Prospective, Single-Arm, Open-Label Observational Study Abstract Abstract Background : We aimed to elucidate the quantitative relationship between the neuromuscular blockade dep... |
PMC9494998 | core_pubmed_pmc | Plasma Protein Binding Rate and Pharmacokinetics of Lekethromycin in Rats | Plasma Protein Binding Rate and Pharmacokinetics of Lekethromycin in Rats Abstract Abstract Lekethromycin (LKMS), a novel macrolide lactone, is still unclear regarding its absorption. Thus, we conducted this study to investigate the characteristics of LKMS in rats. We chose the ultrafiltration method to measure the pla... |
PMC10583240 | core_pubmed_pmc | Population pharmacokinetic analyses for belzutifan to inform dosing considerations and labeling | Population pharmacokinetic analyses for belzutifan to inform dosing considerations and labeling Abstract Abstract Belzutifan (Welireg, Merck & Co., Inc., Rahway, NJ, USA) is an oral, potent inhibitor of hypoxia‐inducible factor 2α, approved for the treatment of certain patients with von Hippel–Lindau (VHL) disease‐asso... |
PMC11468994 | core_pubmed_pmc | Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents | Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents Abstract Abstract Nanogels open up access to a wide range of applications and offer among others hopeful approaches for use in the field of biomedicine. This review provides a brief overview of current developments of nanogels in gene... |
PMC12221915 | core_pubmed_pmc | Virtual screening, molecular dynamics simulations, and in vitro analysis of Sophora flavescens -derived aloperine against Haemonchus contortus | Virtual screening, molecular dynamics simulations, and in vitro analysis of Sophora flavescens -derived aloperine against Haemonchus contortus Abstract Abstract Introduction The resistance of Haemonchus contortus to ivermectin (IVM) poses a significant economic threat to the global livestock industry. This necessitates... |
PMC12479965 | core_pubmed_pmc | In vitro investigation of Datura innoxia phytocompounds against Mycobacterium tuberculosis H37Ra strain in association with in silico studies | In vitro investigation of Datura innoxia phytocompounds against Mycobacterium tuberculosis H37Ra strain in association with in silico studies Abstract Tuberculosis (TB) is a recurrent and progressive bacterial disease caused by Mycobacterium tuberculosis ( Mtb ), posing a significant challenge globally due to its drug ... |
PMC12920200 | core_pubmed_pmc | Metabolic control of neuroinflammation: focus on itaconate and its derivatives in CNS disorders | Metabolic control of neuroinflammation: focus on itaconate and its derivatives in CNS disorders Abstract The activation of microglia, which are the resident immune cells of the central nervous system (CNS), underpins the pathogenesis of neuroinflammatory and neurodegenerative diseases. Metabolic reprogramming has recen... |
PMC4365270 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamic properties of oral DEBIO1143 (AT-406) in patients with advanced cancer: results of a first-in-man study | Safety, pharmacokinetics, and pharmacodynamic properties of oral DEBIO1143 (AT-406) in patients with advanced cancer: results of a first-in-man study Abstract Purpose To assess safety/tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and antitumor activity of DEBIO1143, an antagonist of inhibitor apoptosis pr... |
PMC9558510 | core_pubmed_pmc | Monitoring of Dabrafenib and Trametinib in Serum and Self-Sampled Capillary Blood in Patients with BRAFV600-Mutant Melanoma | Monitoring of Dabrafenib and Trametinib in Serum and Self-Sampled Capillary Blood in Patients with BRAFV600-Mutant Melanoma Abstract Abstract Simple Summary In melanoma patients treated with dabrafenib and trametinib, dose reductions and treatment discontinuations related to adverse events (AE) occur frequently. Howeve... |
PMC12694723 | core_pubmed_pmc | Pharmacokinetic Evidence Supporting Subcutaneous Use of Protein C Concentrate in Patients with Protein C Deficiency | Pharmacokinetic Evidence Supporting Subcutaneous Use of Protein C Concentrate in Patients with Protein C Deficiency Abstract Background Protein C concentrate (Ceprotin®; Baxalta US Inc., a Takeda company, Cambridge, MA; Takeda Manufacturing Austria AG, Vienna, Austria) is approved for intravenous (IV) use in severe con... |
PMC12686243 | core_pubmed_pmc | Synthesis and preclinical evaluation of FAP-targeting radiotracers for PET and optical imaging | Synthesis and preclinical evaluation of FAP-targeting radiotracers for PET and optical imaging Abstract Abstract Background Successful treatment of solid cancers relies on precise diagnosis, e.g. using noninvasive molecular imaging, followed by surgical removal and/or chemo/immunotherapy. Despite advances in pre-operat... |
PMC7434864 | core_pubmed_pmc | Lysine Acetyltransferase Inhibitors From Natural Sources | Lysine Acetyltransferase Inhibitors From Natural Sources Abstract Abstract Acetylation of histone and non-histone protein lysine residues has been widely described as a critical modulator of several cell functions in humans. Lysine acetyltransferases (KATs) catalyse the transfer of acetyl groups on substrate proteins a... |
PMC4527054 | core_pubmed_pmc | Estimation of the plasma effect site equilibration rate constant of sufentanil in children using the time to peak effect of heart rate and blood pressure | Estimation of the plasma effect site equilibration rate constant of sufentanil in children using the time to peak effect of heart rate and blood pressure Abstract Abstract Objectives: Although targeting the effect site concentration may offer advantages over the traditional forms of administering intravenous anesthetic... |
PMC4882768 | core_pubmed_pmc | Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer | Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer Abstract Abstract Background: Rucaparib is an orally available potent selective small-molecule inhibitor ... |
PMC8216120 | core_pubmed_pmc | Denosumab biosimilar in postmenopausal osteoporotic women: A randomized, assessor-blind, active-controlled clinical trial | Denosumab biosimilar in postmenopausal osteoporotic women: A randomized, assessor-blind, active-controlled clinical trial Abstract Abstract OBJECTIVE: The study assessed the efficacy, safety, pharmacokinetic (PK), and immunogenicity profiles of denosumab-biosimilar and denosumab-reference in postmenopausal osteoporotic... |
PMC7969273 | core_pubmed_pmc | Low-dose oral hydroxychloroquine led to impaired vision in a child with renal failure | Low-dose oral hydroxychloroquine led to impaired vision in a child with renal failure Abstract Abstract Introduction: Hydroxychloroquine (HCQ) has received much attention in the treatment of coronavirus disease 2019 recently. However, it can cause irreversible vision loss. Few cases have been reported in pediatric pati... |
PMC11944646 | core_pubmed_pmc | PK/PD of Positively Charged ADC in Mice | PK/PD of Positively Charged ADC in Mice Abstract Background/Objectives : Antibody–drug conjugates (ADCs) show significant promise in oncology but often suffer from a narrow therapeutic window. Introducing a positive charge on the antibody is one proposed strategy to enhance tumor distribution and efficacy of ADC. Accor... |
PMC9982223 | core_pubmed_pmc | Cardiac Toxicity of Alectinib in Patients With ALK+ Lung Cancer | Cardiac Toxicity of Alectinib in Patients With ALK+ Lung Cancer Abstract Abstract Background Anaplastic lymphoma kinase (ALK) translocations in metastatic non-small cell lung cancer (3% to 7%) predict for response to ALK-inhibitors (eg, alectinib, first line), resulting in a 5-year survival rate of ∼60% and median prog... |
PMC11368715 | core_pubmed_pmc | Influence of C-reactive protein on the pharmacokinetics of voriconazole in relation to the CYP2C19 genotype: a population pharmacokinetics analysis | Influence of C-reactive protein on the pharmacokinetics of voriconazole in relation to the CYP2C19 genotype: a population pharmacokinetics analysis Abstract Abstract Voriconazole is a broad-spectrum triazole antifungal agent. A number of studies have revealed that the impact of C-reactive protein (CRP) on voriconazole ... |
PMC3262369 | core_pubmed_pmc | The pharmacokinetics of valganciclovir prophylaxis in pediatric solid organ transplant patients at risk for Epstein–Barr virus disease | The pharmacokinetics of valganciclovir prophylaxis in pediatric solid organ transplant patients at risk for Epstein–Barr virus disease Abstract Abstract Antiviral prophylaxis with valganciclovir is used frequently in pediatric solid organ transplant patients to prevent Epstein–Barr virus (EBV)-induced infections and ti... |
PMC11130324 | core_pubmed_pmc | Quantitative systems pharmacology modeling of HER2-positive metastatic breast cancer for translational efficacy evaluation and combination assessment across therapeutic modalities | Quantitative systems pharmacology modeling of HER2-positive metastatic breast cancer for translational efficacy evaluation and combination assessment across therapeutic modalities Abstract HER2-positive (HER2 + ) metastatic breast cancer (mBC) is highly aggressive and a major threat to human health. Despite the signifi... |
PMC11098151 | core_pubmed_pmc | Using forest plots to interpret covariate effects in pharmacometric models | Using forest plots to interpret covariate effects in pharmacometric models Abstract Abstract The inclusion of covariates in pharmacometric models is important due to their ability to explain variability in drug exposure and response. Clear communication of the impact of covariates is needed to support informed decision... |
PMC3704234 | core_pubmed_pmc | Erythropoiesis stimulating agents: approaches to modulate activity | Erythropoiesis stimulating agents: approaches to modulate activity Abstract Abstract Recombinant human erythropoietin (rHuEPO), such as the approved agents epoetin alfa and epoetin beta, has been used successfully for over 20 years to treat anemia in millions of patients. However, due to the relatively short half-life ... |
PMC7945683 | core_pubmed_pmc | Effect of severe renal impairment on pharmacokinetics, safety, and tolerability of lemborexant | Effect of severe renal impairment on pharmacokinetics, safety, and tolerability of lemborexant Abstract Abstract The primary aim of this study was to examine the effect of severe renal impairment (SRI) on the pharmacokinetics of lemborexant, a dual orexin receptor antagonist indicated for the treatment of insomnia. A p... |
PMC4366519 | core_pubmed_pmc | Stereochemical bias introduced during RNA synthesis modulates the activity of phosphorothioate siRNAs | Stereochemical bias introduced during RNA synthesis modulates the activity of phosphorothioate siRNAs Abstract An established means of improving the pharmacokinetics properties of oligoribonucleotides (ORNs) is to exchange their phosphodiester linkages for phosphorothioates (PSs). However, this strategy has not been pu... |
PMC12298949 | core_pubmed_pmc | Pharmacokinetic Analysis of the Bioavailability of AQUATURM ® , a Water-Soluble Curcumin Formulation, in Comparison to a Conventional Curcumin Tablet, in Human Subjects | Pharmacokinetic Analysis of the Bioavailability of AQUATURM ® , a Water-Soluble Curcumin Formulation, in Comparison to a Conventional Curcumin Tablet, in Human Subjects Abstract Abstract Background/Objectives: Curcumin, the principal bioactive component of Curcuma longa, is known for its anti-inflammatory, antioxidant,... |
PMC9798748 | core_pubmed_pmc | Using a Mathematical Modeling To Simulate Pharmacokinetics and Urinary Glucose Excretion of Luseogliflozin and Explore the Role of SGLT1/2 in Renal Glucose Reabsorption | Using a Mathematical Modeling To Simulate Pharmacokinetics and Urinary Glucose Excretion of Luseogliflozin and Explore the Role of SGLT1/2 in Renal Glucose Reabsorption Abstract Abstract (1) Purpose: To develop a mathematical model combining physiologically based pharmacokinetic and urinary glucose excretion (PBPK-UGE)... |
PMC3053444 | core_pubmed_pmc | Performance Evaluation of PETbox: A Low Cost Bench Top Preclinical PET Scanner | Performance Evaluation of PETbox: A Low Cost Bench Top Preclinical PET Scanner Abstract Purpose PETbox is a low cost bench top preclinical PET scanner dedicated to pharmacokinetic and pharmacodynamic mouse studies. A prototype system was developed at our institute, and this manuscript characterizes the performance of t... |
PMC11854238 | core_pubmed_pmc | A prior information-based multi-population multi-objective optimization for estimating 18 F-FDG PET/CT pharmacokinetics of hepatocellular carcinoma | A prior information-based multi-population multi-objective optimization for estimating 18 F-FDG PET/CT pharmacokinetics of hepatocellular carcinoma Abstract Background 18 F fluoro-D-glucose ( 18 F-FDG) positron emission tomography/computed tomography (PET/CT) pharmacokinetics is an approach for efficiently quantifying ... |
PMC9054915 | core_pubmed_pmc | Assessment of cytochrome P450 3A4-mediated drug–drug interactions for ipatasertib using a fit-for-purpose physiologically based pharmacokinetic model | Assessment of cytochrome P450 3A4-mediated drug–drug interactions for ipatasertib using a fit-for-purpose physiologically based pharmacokinetic model Abstract Purpose Ipatasertib, a potent and highly selective small-molecule inhibitor of AKT, is currently under investigation for treatment of cancer. Ipatasertib is a su... |
PMC6978430 | core_pubmed_pmc | Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use | Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use Abstract Quercetin (3,3′,4′,5,7-pentahydroxyflavone) is a naturally derived flavonoid that is commonly found in fruits and vegetables. There is mounting evidence to suggest that quercetin has potential anticancer effects and ap... |
PMC12072214 | core_pubmed_pmc | Using the Simcyp R Package for PBPK Simulation Workflows With the Simcyp Simulator | Using the Simcyp R Package for PBPK Simulation Workflows With the Simcyp Simulator Abstract ABSTRACT Physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) modeling aims to understand how a drug is absorbed, distributed, metabolized, excreted, and acts in a human or animal body. The Simcyp Simulator is a w... |
PMC9467945 | core_pubmed_pmc | Machines that help machines to help patients: optimising antimicrobial dosing in patients receiving extracorporeal membrane oxygenation and renal replacement therapy using dosing software | Machines that help machines to help patients: optimising antimicrobial dosing in patients receiving extracorporeal membrane oxygenation and renal replacement therapy using dosing software Abstract Abstract Intensive care unit (ICU) patients with end-organ failure will require specialised machines or extracorporeal ther... |
PMC12128073 | core_pubmed_pmc | Prediction of Vancomycin Area Under the Curve With Trough Concentrations Only: Performance Evaluation of Pediatric Population Pharmacokinetic Models | Prediction of Vancomycin Area Under the Curve With Trough Concentrations Only: Performance Evaluation of Pediatric Population Pharmacokinetic Models Abstract Abstract Background In pediatric patients, vancomycin plays a pivotal role in combating infections, necessitating precise therapeutic drug monitoring to ensure ef... |
PMC12031376 | core_pubmed_pmc | Ex Vivo Pharmacokinetic/Pharmacodynamic Integration Model of Cefquinome Against Escherichia coli in Foals | Ex Vivo Pharmacokinetic/Pharmacodynamic Integration Model of Cefquinome Against Escherichia coli in Foals Abstract Simple Summary Bacterial infection is a major cause of death in foals. Escherichia coli ( E. coli ) is a Gram-negative bacterium that causes sepsis, which can be life-threatening in horses. Cefquinome has ... |
PMC9714317 | core_pubmed_pmc | An adaptive phase II/III safety and efficacy randomized controlled trial of single day or three-day fixed-dose albendazole-ivermectin co-formulation versus albendazole for the treatment of Trichuris trichiura and other STH infections. ALIVE trial protocol | An adaptive phase II/III safety and efficacy randomized controlled trial of single day or three-day fixed-dose albendazole-ivermectin co-formulation versus albendazole for the treatment of Trichuris trichiura and other STH infections. ALIVE trial protocol Abstract Background: Soil-transmitted helminths (STH) are target... |
PMC12163019 | core_pubmed_pmc | Zabedosertib, a novel interleukin-1 receptor-associated kinase-4 inhibitor, shows a favorable pharmacokinetic and safety profile across multiple phase 1 studies | Zabedosertib, a novel interleukin-1 receptor-associated kinase-4 inhibitor, shows a favorable pharmacokinetic and safety profile across multiple phase 1 studies Abstract Introduction Zabedosertib, the interleukin-1 receptor-associated kinase-4 (IRAK4) inhibitor, is in clinical development as an oral therapeutic for imm... |
PMC11630552 | core_pubmed_pmc | Safety and efficacy of selumetinib in pediatric and adult patients with neurofibromatosis type 1 and plexiform neurofibroma | Safety and efficacy of selumetinib in pediatric and adult patients with neurofibromatosis type 1 and plexiform neurofibroma Abstract Abstract Background The MEK inhibitor, selumetinib, reduces plexiform neurofibroma (PN) in pediatric patients with neurofibromatosis type 1 (NF1). Its safety and efficacy in adults with P... |
PMC5371981 | core_pubmed_pmc | Untargeted metabolomics analysis reveals key pathways responsible for the synergistic killing of colistin and doripenem combination against Acinetobacter baumannii | Untargeted metabolomics analysis reveals key pathways responsible for the synergistic killing of colistin and doripenem combination against Acinetobacter baumannii Abstract Combination therapy is deployed for the treatment of multidrug-resistant Acinetobacter baumannii , as it can rapidly develop resistance to current ... |
PMC6585632 | core_pubmed_pmc | Pharmacokinetic Study of Rucaparib in Patients With Advanced Solid Tumors | Pharmacokinetic Study of Rucaparib in Patients With Advanced Solid Tumors Abstract Abstract The phase 1‐2 study CO‐338‐010 (Study 10; NCT01482715 ) is evaluating single‐agent rucaparib, a poly(ADP‐ribose) polymerase inhibitor, administered orally to patients with an advanced solid tumor. In the dose escalation phase (P... |
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