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PMC6377538 | core_pubmed_pmc | Treatment of multiple brain metastases using gadolinium nanoparticles and radiotherapy: NANO-RAD, a phase I study protocol | Treatment of multiple brain metastases using gadolinium nanoparticles and radiotherapy: NANO-RAD, a phase I study protocol Abstract Introduction Occurrence of multiple brain metastases is a critical evolution of many cancers with significant neurological and overall survival consequences, despite new targeted therapy a... |
PMC11892667 | core_pubmed_pmc | Bexotegrast Shows Dose-Dependent Integrin α v β 6 Receptor Occupancy in Lungs of Participants with Idiopathic Pulmonary Fibrosis: A Phase 2, Open-Label Clinical Trial | Bexotegrast Shows Dose-Dependent Integrin α v β 6 Receptor Occupancy in Lungs of Participants with Idiopathic Pulmonary Fibrosis: A Phase 2, Open-Label Clinical Trial Abstract Rationale Idiopathic pulmonary fibrosis (IPF) is a chronic and progressive disease characterized by dyspnea and loss of lung function. Transform... |
PMC10459320 | core_pubmed_pmc | Dried Blood Spots in Neonatal Studies: A Computational Analysis for the Role of the Hematocrit Effect | Dried Blood Spots in Neonatal Studies: A Computational Analysis for the Role of the Hematocrit Effect Abstract Abstract Dried blood spot (DBS) microsampling is extensively employed in newborn screening (NBS) and neonatal studies. However, the impact of variable neonatal hematocrit (Ht) values on the results can be a so... |
PMC10509356 | core_pubmed_pmc | Nonlinear Mixed Effects Modeling of Glucagon Kinetics in Healthy Subjects | Nonlinear Mixed Effects Modeling of Glucagon Kinetics in Healthy Subjects Abstract Objective: To date, the lack of a model of glucagon kinetics precluded the possibility of estimating and studying glucagon secretion in vivo, e.g., using deconvolution, as done for other hormones like insulin and C-peptide. Here, we used... |
PMC11227971 | core_pubmed_pmc | Exploring the clinical transition of engineered exosomes designed for intracellular delivery of therapeutic proteins | Exploring the clinical transition of engineered exosomes designed for intracellular delivery of therapeutic proteins Abstract Abstract Extracellular vesicles, particularly exosomes, have emerged as promising drug delivery systems owing to their unique advantages, such as biocompatibility, immune tolerability, and targe... |
PMC8635670 | core_pubmed_pmc | In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model | In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model Abstract Abstract Context Metformin is an important oral anti-hyperglycemic used in diabetes. Polylactic-co-glycolic acid (PLGA) has been widely used due to its reliability in control... |
PMC3532155 | core_pubmed_pmc | Continuous infusion of antibiotics in the critically ill: The new holy grail for beta-lactams and vancomycin? | Continuous infusion of antibiotics in the critically ill: The new holy grail for beta-lactams and vancomycin? Abstract Abstract The alarming global rise of antimicrobial resistance combined with the lack of new antimicrobial agents has led to a renewed interest in optimization of our current antibiotics. Continuous inf... |
PMC4854994 | core_pubmed_pmc | The PK/PD Interactions of Doxycycline against Mycoplasma gallisepticum | The PK/PD Interactions of Doxycycline against Mycoplasma gallisepticum Abstract Abstract Mycoplasma gallisepticum is one of the most important pathogens that cause chronic respiratory disease in chicken. This study investigated the antibacterial activity of doxycycline against M. gallisepticum strain S6. In static time... |
PMC10239799 | core_pubmed_pmc | Effect of molecular distillation on the anti-inflammatory activity and neurotoxicity of Asarum essential oil | Effect of molecular distillation on the anti-inflammatory activity and neurotoxicity of Asarum essential oil Abstract Abstract Asarum essential oil (AEO) has been shown to have good pharmacological activities for the anti-inflammatory and analgesic effects, but increasing the dose may cause toxicity. Therefore, we stud... |
PMC6157691 | core_pubmed_pmc | A Semi‐Mechanistic Population Pharmacokinetic Model of Nusinersen: An Antisense Oligonucleotide for the Treatment of Spinal Muscular Atrophy | A Semi‐Mechanistic Population Pharmacokinetic Model of Nusinersen: An Antisense Oligonucleotide for the Treatment of Spinal Muscular Atrophy Abstract Abstract A pharmacokinetic (PK) model was developed for nusinersen, an antisense oligonucleotide (ASO) that is the first approved treatment for spinal muscular atrophy (S... |
PMC11848289 | core_pubmed_pmc | Targeting aldose reductase using natural African compounds as promising agents for managing diabetic complications | Targeting aldose reductase using natural African compounds as promising agents for managing diabetic complications Abstract Abstract Background Diabetes remains a leading cause of morbidity and mortality due to various complications induced by hyperglycemia. Inhibiting Aldose Reductase (AR), an enzyme that converts glu... |
PMC10398509 | core_pubmed_pmc | Comparative cardiac effects of antimalarial drug halofantrine with or without concomitant administration of kolanut or fluconazole in healthy volunteers | Comparative cardiac effects of antimalarial drug halofantrine with or without concomitant administration of kolanut or fluconazole in healthy volunteers Abstract Background There is rekindled interest in the cardiotoxicity of antimalarial medicines. Halofantrine is associated with QT interval prolongation. Fluconazole ... |
PMC3785161 | core_pubmed_pmc | In vivo pharmacokinetic comparisons of ferulic acid and puerarin after oral administration of monomer, medicinal substance aqueous extract and Nao-De-Sheng to rats | In vivo pharmacokinetic comparisons of ferulic acid and puerarin after oral administration of monomer, medicinal substance aqueous extract and Nao-De-Sheng to rats Abstract Background: Nao-De-Sheng decoction (NDS), a traditional Chinese medicine (TCM) prescription containing Radix puerariae lobatae , Floscarthami , Rad... |
PMC12159125 | core_pubmed_pmc | An Adult Population Pharmacokinetic Model to Simulate Subcutaneous Administration of a Fixed Dose of Furosemide in Adolescents with Heart Failure and Volume Overload | An Adult Population Pharmacokinetic Model to Simulate Subcutaneous Administration of a Fixed Dose of Furosemide in Adolescents with Heart Failure and Volume Overload Abstract Background Subcutaneous furosemide administered with the On-Body Infusor could be useful in children with heart failure (HF) and congestion due t... |
PMC10051808 | core_pubmed_pmc | A Validated Chiral LC–MS/MS Method for the Enantioselective Determination of (S)-(+)- and (R)-(-)-Ibuprofen in Dog Plasma: Its Application to a Pharmacokinetic Study | A Validated Chiral LC–MS/MS Method for the Enantioselective Determination of (S)-(+)- and (R)-(-)-Ibuprofen in Dog Plasma: Its Application to a Pharmacokinetic Study Abstract Abstract The purpose of this study was to develop a method for simultaneously separating ibuprofen enantiomers using electrospray ionization (ESI... |
PMC5321810 | core_pubmed_pmc | Multiscale modeling reveals inhibitory and stimulatory effects of caffeine on acetaminophen‐induced toxicity in humans | Multiscale modeling reveals inhibitory and stimulatory effects of caffeine on acetaminophen‐induced toxicity in humans Abstract Acetaminophen (APAP) is a widely used analgesic drug that is frequently co‐administered with caffeine (CAF) in the treatment of pain. It is well known that APAP may cause severe liver injury a... |
PMC12472646 | core_pubmed_pmc | Pharmacological Effects and Mechanisms of Tanshinone IIA in Bone Injury Repair | Pharmacological Effects and Mechanisms of Tanshinone IIA in Bone Injury Repair Abstract Tanshinone IIA (T-IIA), a fat-soluble diterpene quinone extracted from Salvia miltiorrhiza , is widely recognized for its multiple pharmacological properties, including anti-inflammatory, antioxidant, anti-fibrotic, and anti-tumor e... |
PMC6522057 | core_pubmed_pmc | Analysis of PK11195 concentrations in rodent whole blood and tissue samples by rapid and reproducible chromatographic method to support target-occupancy PET studies | Analysis of PK11195 concentrations in rodent whole blood and tissue samples by rapid and reproducible chromatographic method to support target-occupancy PET studies Abstract Abstract In Positron Emission Tomography (PET) research, it is important to assess not only pharmacokinetics of a radiotracer in vivo , but also o... |
PMC3173470 | core_pubmed_pmc | A Systems Approach for Tumor Pharmacokinetics | A Systems Approach for Tumor Pharmacokinetics Abstract Recent advances in genome inspired target discovery, small molecule screens, development of biological and nanotechnology have led to the introduction of a myriad of new differently sized agents into the clinic. The differences in small and large molecule delivery ... |
PMC11526779 | core_pubmed_pmc | Identification of acetylcholinesterase inhibitors from traditional medicinal plants for Alzheimer's disease using in silico and machine learning approaches † | Identification of acetylcholinesterase inhibitors from traditional medicinal plants for Alzheimer's disease using in silico and machine learning approaches † Abstract Acetylcholinesterase (AChE) holds significance in Alzheimer's disease (AD), where cognitive impairment correlates with insufficient acetylcholine levels.... |
PMC12339406 | core_pubmed_pmc | Preclinical Evaluation of the Oral Toxicity, Genotoxicity, and Safety Pharmacology of LPM4870108, a Novel Potent Tropomyosin Receptor Kinase Inhibitor | Preclinical Evaluation of the Oral Toxicity, Genotoxicity, and Safety Pharmacology of LPM4870108, a Novel Potent Tropomyosin Receptor Kinase Inhibitor Abstract ABSTRACT Tropomyosin receptor kinase (Trk) inhibitors are an essential class of anticancer drugs treating NTRK gene fusions‐positive cancer. However, the potent... |
PMC8602248 | core_pubmed_pmc | Identifying an optimal dihydroartemisinin-piperaquine dosing regimen for malaria prevention in young Ugandan children | Identifying an optimal dihydroartemisinin-piperaquine dosing regimen for malaria prevention in young Ugandan children Abstract Intermittent preventive treatment (IPT) with dihydroartemisinin-piperaquine (DP) is highly protective against malaria in children, but is not standard in malaria-endemic countries. Optimal DP d... |
PMC8651971 | core_pubmed_pmc | A Randomized, Double-Blind, Placebo-Controlled, First-in-Human Clinical Trial to Assess Safety, Tolerability, and Pharmacokinetics of LY-CovMab, a Potent Human Neutralizing Antibody Against SARS-CoV-2 | A Randomized, Double-Blind, Placebo-Controlled, First-in-Human Clinical Trial to Assess Safety, Tolerability, and Pharmacokinetics of LY-CovMab, a Potent Human Neutralizing Antibody Against SARS-CoV-2 Abstract Abstract Introduction We aimed to evaluate the safety, tolerability, pharmacokinetics, and immunogenicity of a... |
PMC9206391 | core_pubmed_pmc | Topical Ocular Anti-TNFα Agent Licaminlimab in the Treatment of Acute Anterior Uveitis: A Randomized Phase II Pilot Study | Topical Ocular Anti-TNFα Agent Licaminlimab in the Treatment of Acute Anterior Uveitis: A Randomized Phase II Pilot Study Abstract Purpose Licaminlimab is a new anti-TNFα antibody fragment for topical ocular application. This phase II study assessed the tolerability, treatment effect, and pharmacokinetics of licaminlim... |
PMC8760698 | core_pubmed_pmc | Bioactivities and mechanisms of natural medicines in the management of pulmonary arterial hypertension | Bioactivities and mechanisms of natural medicines in the management of pulmonary arterial hypertension Abstract Abstract Pulmonary arterial hypertension (PAH) is a progressive and rare disease without obvious clinical symptoms that shares characteristics with pulmonary vascular remodeling. Right heart failure in the te... |
PMC6278537 | core_pubmed_pmc | Simultaneous Determination and Pharmacokinetics Study of Six Triterpenes in Rat Plasma by UHPLC-MS/MS after Oral Administration of Sanguisorba officinalis L. Extract | Simultaneous Determination and Pharmacokinetics Study of Six Triterpenes in Rat Plasma by UHPLC-MS/MS after Oral Administration of Sanguisorba officinalis L. Extract Abstract A selective and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed and validated ... |
PMC11707850 | core_pubmed_pmc | Efficacy and Safety of Ciprofol for Anesthesia in Painless Colonoscopy with Varying Body Mass Indices Patients: A Prospective, Single-Center, Observational Study | Efficacy and Safety of Ciprofol for Anesthesia in Painless Colonoscopy with Varying Body Mass Indices Patients: A Prospective, Single-Center, Observational Study Abstract Abstract Background Ciprofol, a novel intravenous anesthetic derived from propofol, exhibits high lipophilicity. Its pharmacokinetics and pharmacodyn... |
PMC8484168 | core_pubmed_pmc | A phase 1, open-label, drug–drug interaction study of rucaparib with rosuvastatin and oral contraceptives in patients with advanced solid tumors | A phase 1, open-label, drug–drug interaction study of rucaparib with rosuvastatin and oral contraceptives in patients with advanced solid tumors Abstract Abstract Purpose This study aimed at evaluating the effect of rucaparib on the pharmacokinetics of rosuvastatin and oral contraceptives in patients with advanced soli... |
PMC9952313 | core_pubmed_pmc | Repurposing β-Lactams for the Treatment of Mycobacterium kansasii Infections: An In Vitro Study | Repurposing β-Lactams for the Treatment of Mycobacterium kansasii Infections: An In Vitro Study Abstract Abstract Mycobacterium kansasii ( Mkn ) causes tuberculosis-like lung infection in both immunocompetent and immunocompromised patients. Current standard therapy against Mkn infection is lengthy and difficult to adhe... |
PMC8583628 | core_pubmed_pmc | A Phase Ib Study of Sotrastaurin, a PKC Inhibitor, and Alpelisib, a PI3Kα Inhibitor, in Patients with Metastatic Uveal Melanoma | A Phase Ib Study of Sotrastaurin, a PKC Inhibitor, and Alpelisib, a PI3Kα Inhibitor, in Patients with Metastatic Uveal Melanoma Abstract Abstract Simple Summary Uveal melanoma is a rare subset of melanoma characterized by the presence of early initiating GNAQ/11 mutations, with downstream activation of several pathways... |
PMC6923804 | core_pubmed_pmc | The pharmacology and therapeutic applications of monoclonal antibodies | The pharmacology and therapeutic applications of monoclonal antibodies Abstract Abstract Monoclonal antibodies (mAbs) have emerged as a major class of therapeutic agents on the market. To date, approximately 80 mAbs have been granted marketing approval. In 2018, 12 new mAbs were approved by the FDA, representing 20% of... |
PMC7418953 | core_pubmed_pmc | Simultaneous separation of naproxen and 6-O-desmethylnaproxen metabolite in saliva samples by liquid chromatography–tandem mass spectrometry: Pharmacokinetic study of naproxen alone and associated with esomeprazole | Simultaneous separation of naproxen and 6-O-desmethylnaproxen metabolite in saliva samples by liquid chromatography–tandem mass spectrometry: Pharmacokinetic study of naproxen alone and associated with esomeprazole Abstract Naproxen is a widely used non-steroidal anti-inflammatory drug for the control of postoperative ... |
PMC10720493 | core_pubmed_pmc | Subcutaneous infusion of high-dose benzathine penicillin G is safe, tolerable, and suitable for less-frequent dosing for rheumatic heart disease secondary prophylaxis: a phase 1 open-label population pharmacokinetic study | Subcutaneous infusion of high-dose benzathine penicillin G is safe, tolerable, and suitable for less-frequent dosing for rheumatic heart disease secondary prophylaxis: a phase 1 open-label population pharmacokinetic study Abstract ABSTRACT Since 1955, the recommended strategy for rheumatic heart disease (RHD) secondary... |
PMC3813230 | core_pubmed_pmc | Optimal Aminoglycoside Therapy Following the Sepsis: How Much Is Too Much? | Optimal Aminoglycoside Therapy Following the Sepsis: How Much Is Too Much? Abstract Abstract Severe sepsis and septic shock are major problems as the result of high rates morbidity and mortality in intensive care units (ICUs). In the presence of septic shock, each hour of delay in the administration of effective antibi... |
PMC6444840 | core_pubmed_pmc | Controlled infusion of intravenous cardiac drugs using global optimization | Controlled infusion of intravenous cardiac drugs using global optimization Abstract OBJECTIVES: The objective of the study is to develop an automatic drug infusion control system during cardiovascular surgery. MATERIALS AND METHODS: Based on the clinical drug dosage analysis, the modeling of cardiovascular system with ... |
PMC4602247 | core_pubmed_pmc | The relationship between infliximab concentrations, antibodies to infliximab and disease activity in Crohn's disease | The relationship between infliximab concentrations, antibodies to infliximab and disease activity in Crohn's disease Abstract Objective Although low infliximab trough concentrations and antibodies to infliximab (ATI) are associated with poor outcomes in patients with Crohn's disease (CD), the clinical relevance of ATI ... |
PMC12189505 | core_pubmed_pmc | Intravenous Clarithromycin in Critically Ill Adults: A Population Pharmacokinetic Study | Intravenous Clarithromycin in Critically Ill Adults: A Population Pharmacokinetic Study Abstract Background: Clarithromycin is a commonly used macrolide antibiotic. Infection is a major source of mortality and morbidity in critical care units. Pharmacokinetics may vary during critical illness and suboptimal antimicrobi... |
PMC7019851 | core_pubmed_pmc | Estimation of the Minimum Effective Dose of Dietary Supplement Crocetin for Prevention of Myopia Progression in Mice | Estimation of the Minimum Effective Dose of Dietary Supplement Crocetin for Prevention of Myopia Progression in Mice Abstract Abstract The natural carotenoid crocetin has been reported to suppress phenotypes of an experimental myopia model in mice. We investigated the minimum effective dose to prevent myopia progressio... |
PMC9304220 | core_pubmed_pmc | The Pharmacoeconomic Benefits of Pemetrexed Dose Individualization in Patients With Lung Cancer | The Pharmacoeconomic Benefits of Pemetrexed Dose Individualization in Patients With Lung Cancer Abstract Abstract Neutropenia is a dose‐related treatment‐limiting and costly adverse event of pemetrexed. We postulate that individualized dosing reduces the incidence of neutropenia. The aims of this study were (i) to inve... |
PMC8948873 | core_pubmed_pmc | Effects of Injection Volume and Route of Administration on Dolutegravir In Situ Forming Implant Pharmacokinetics | Effects of Injection Volume and Route of Administration on Dolutegravir In Situ Forming Implant Pharmacokinetics Abstract Abstract Due to the versatility of the in situ forming implant (ISFI) drug delivery system, it is crucial to understand the effects of formulation parameters for clinical translation. We utilized ul... |
PMC12537934 | core_pubmed_pmc | Artificial intelligence coupled to pharmacometrics modelling to tailor malaria and tuberculosis treatment in Africa | Artificial intelligence coupled to pharmacometrics modelling to tailor malaria and tuberculosis treatment in Africa Abstract Abstract Africa’s vast genetic diversity poses challenges for optimising drug treatments in the continent, which is exacerbated by the fact that drug discovery and development efforts have histor... |
PMC6468233 | core_pubmed_pmc | Enantioselective Box Behenken Optimized HPLC-DAD Method for the Simultaneous Estimation of Alogliptin Enantiomorphs in Pharmaceutical Formulations and their Pharmacokinetic Study in Rat Plasma | Enantioselective Box Behenken Optimized HPLC-DAD Method for the Simultaneous Estimation of Alogliptin Enantiomorphs in Pharmaceutical Formulations and their Pharmacokinetic Study in Rat Plasma Abstract Purpose: A stereoselective high performance liquid chromatographic analytical method with photodiode array detector wa... |
PMC4629955 | core_pubmed_pmc | Critical appraisal of rituximab in the maintenance treatment of advanced follicular lymphoma | Critical appraisal of rituximab in the maintenance treatment of advanced follicular lymphoma Abstract Rituximab is an IgG1, chimeric monoclonal antibody specifically designed to recognize the CD20 antigen expressed on the surface of normal and malignant B-lymphocytes, from the B-cell precursor to the mature B-cells of ... |
PMC11760439 | core_pubmed_pmc | Intra- and Interspecies Conjugal Transfer of Plasmids in Gram-Negative Bacteria | Intra- and Interspecies Conjugal Transfer of Plasmids in Gram-Negative Bacteria Abstract Abstract Background/Objectives: Plasmid-mediated resistance is a significant mechanism that contributes to the gradual decrease in the efficacy of antibiotics from various classes, including carbapenems. The aim of this study is to... |
PMC12521056 | core_pubmed_pmc | Population Pharmacokinetic and Exposure‐Response Analyses of Ibrutinib Combined With Bendamustine and Rituximab in Patients With Mantle Cell Lymphoma | Population Pharmacokinetic and Exposure‐Response Analyses of Ibrutinib Combined With Bendamustine and Rituximab in Patients With Mantle Cell Lymphoma Abstract ABSTRACT Efficacy and safety of ibrutinib 560 mg once daily or placebo combined with bendamustine and rituximab (BR) were assessed in patients with mantle cell l... |
PMC10054735 | core_pubmed_pmc | Preparation, Characterization and Evaluation of Flavonolignan Silymarin Effervescent Floating Matrix Tablets for Enhanced Oral Bioavailability | Preparation, Characterization and Evaluation of Flavonolignan Silymarin Effervescent Floating Matrix Tablets for Enhanced Oral Bioavailability Abstract Abstract The convenient and highly compliant route for the delivery of active pharmaceutical ingredients is the tablet. A versatile platform of tablets is available for... |
PMC3746791 | core_pubmed_pmc | Synthesis of novel tetravalent galactosylated DTPA-DSPE and study on hepatocyte-targeting efficiency in vitro and in vivo | Synthesis of novel tetravalent galactosylated DTPA-DSPE and study on hepatocyte-targeting efficiency in vitro and in vivo Abstract Abstract For the purposes of obtaining a hepatocyte-selective drug delivery system, a novel tetravalent galactosylated diethylenetriaminepentaacetic acid-distearoyl phosphatidylethanolamine... |
PMC7766014 | core_pubmed_pmc | Combining Chemistry and Engineering for Hepatocellular Carcinoma: Nano-Scale and Smaller Therapies | Combining Chemistry and Engineering for Hepatocellular Carcinoma: Nano-Scale and Smaller Therapies Abstract Abstract Primary liver cancer, or hepatocellular carcinoma (HCC), is a major worldwide cause of death from carcinoma. Most patients are not candidates for surgery and medical therapies, including new immunotherap... |
PMC10218444 | core_pubmed_pmc | Nanoemulsions of Hydroxysafflor Yellow A for Enhancing Physicochemical and In Vivo Performance | Nanoemulsions of Hydroxysafflor Yellow A for Enhancing Physicochemical and In Vivo Performance Abstract Abstract Stroke was always a disease that threatened human life and health worldwide. We reported the synthesis of a new type of hyaluronic acid-modified multi-walled carbon nanotube. Then, we produced hydroxysafflor... |
PMC9500859 | core_pubmed_pmc | Pharmacokinetics and Anti-Diabetic Studies of Gliclazide Nanosuspension | Pharmacokinetics and Anti-Diabetic Studies of Gliclazide Nanosuspension Abstract Gliclazide (GCZ), an antidiabetic medication, has poor solubility and limited oral bioavailability due to substantial first-pass metabolism. Thus, the purpose of the current study was to optimize and formulate a GCZ nanosuspension (NS) emp... |
PMC10951222 | core_pubmed_pmc | Exemestane plus everolimus and palbociclib in metastatic breast cancer: clinical response and genomic/transcriptomic determinants of resistance in a phase I/II trial | Exemestane plus everolimus and palbociclib in metastatic breast cancer: clinical response and genomic/transcriptomic determinants of resistance in a phase I/II trial Abstract Abstract The landscape of cyclin-dependent kinase 4/6 inhibitor (CDK4/6i) resistance is still being elucidated and the optimal subsequent therapy... |
PMC5524955 | core_pubmed_pmc | An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection | An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection Abstract Abstract Traditional Chinese medicine (TCM) treatment can be valuable therapeutic strategies. However, the active components and action mechanism... |
PMC7971003 | core_pubmed_pmc | A multi-scale pipeline linking drug transcriptomics with pharmacokinetics predicts in vivo interactions of tuberculosis drugs | A multi-scale pipeline linking drug transcriptomics with pharmacokinetics predicts in vivo interactions of tuberculosis drugs Abstract Abstract Tuberculosis (TB) is the deadliest infectious disease worldwide. The design of new treatments for TB is hindered by the large number of candidate drugs, drug combinations, dosi... |
PMC5627448 | core_pubmed_pmc | Pharmacokinetics of carfilzomib in patients with advanced malignancies and varying degrees of hepatic impairment: an open-label, single-arm, phase 1 study | Pharmacokinetics of carfilzomib in patients with advanced malignancies and varying degrees of hepatic impairment: an open-label, single-arm, phase 1 study Abstract Abstract Background Carfilzomib is approved in the United States and Europe for treatment of relapsed or refractory multiple myeloma (MM). This study evalua... |
PMC8123827 | core_pubmed_pmc | Development and Validation of a Sensitive, Specific and Reproducible UPLC-MS/MS Method for the Quantification of OJT007, A Novel Anti-Leishmanial Agent: Application to a Pharmacokinetic Study | Development and Validation of a Sensitive, Specific and Reproducible UPLC-MS/MS Method for the Quantification of OJT007, A Novel Anti-Leishmanial Agent: Application to a Pharmacokinetic Study Abstract Abstract OJT007 is a methionine aminopeptidase 1 (MetAP1) inhibitor with potent anti-proliferative effects against Leis... |
PMC9953489 | core_pubmed_pmc | Nonlinear Adaptive Optimal Controller Design for Anti-Angiogenic Tumor Treatment | Nonlinear Adaptive Optimal Controller Design for Anti-Angiogenic Tumor Treatment Abstract Abstract Angiogenesis is an important process in tumor growth as it represents the regime when the tumor recruits blood vessels from the surrounding tissue to support further tumor growth. Anti-angiogenic treatments aim to shrink ... |
PMC8405607 | core_pubmed_pmc | Pharmacokinetic–pharmacodynamic guided optimisation of dose and schedule of CGM097, an HDM2 inhibitor, in preclinical and clinical studies | Pharmacokinetic–pharmacodynamic guided optimisation of dose and schedule of CGM097, an HDM2 inhibitor, in preclinical and clinical studies Abstract Background CGM097 inhibits the p53-HDM2 interaction leading to downstream p53 activation. Preclinical in vivo studies support clinical exploration while providing prelimina... |
PMC8886150 | core_pubmed_pmc | The Blind Spot of Pharmacology: A Scoping Review of Drug Metabolism in Prematurely Born Children | The Blind Spot of Pharmacology: A Scoping Review of Drug Metabolism in Prematurely Born Children Abstract The limit for possible survival after extremely preterm birth has steadily improved and consequently, more premature neonates with increasingly lower gestational age at birth now require care. This specialized care... |
PMC10779093 | core_pubmed_pmc | Unraveling the Multifaceted Roles of Extracellular Vesicles: Insights into Biology, Pharmacology, and Pharmaceutical Applications for Drug Delivery | Unraveling the Multifaceted Roles of Extracellular Vesicles: Insights into Biology, Pharmacology, and Pharmaceutical Applications for Drug Delivery Abstract Abstract Extracellular vesicles (EVs) are nanoparticles released from various cell types that have emerged as powerful new therapeutic option for a variety of dise... |
PMC12024584 | core_pubmed_pmc | Modulation of Lonp1 Activity by Small Compounds | Modulation of Lonp1 Activity by Small Compounds Abstract The Lon protease homolog 1 (LONP1) is an ATP-dependent mitochondrial protease essential for maintaining proteostasis, bioenergetics, and cellular homeostasis. LONP1 plays a pivotal role in protein quality control, mitochondrial DNA maintenance, and oxidative phos... |
PMC12185632 | core_pubmed_pmc | Population Cellular Kinetics of Idecabtagene Vicleucel in Patients with Triple-Class–Exposed Relapsed/Refractory Multiple Myeloma | Population Cellular Kinetics of Idecabtagene Vicleucel in Patients with Triple-Class–Exposed Relapsed/Refractory Multiple Myeloma Abstract Background Idecabtagene vicleucel (ide-cel, ABECMA) is an autologous, B-cell maturation antigen (BCMA)-directed, chimeric antigen receptor (CAR) T-cell therapy. The current modeling... |
PMC6980640 | core_pubmed_pmc | The pharmacokinetic parameters and the effect of a single and repeated doses of memantine on gastric myoelectric activity in experimental pigs | The pharmacokinetic parameters and the effect of a single and repeated doses of memantine on gastric myoelectric activity in experimental pigs Abstract Abstract Background Memantine, currently available for the treatment of Alzheimer's disease, is an uncompetitive antagonist of the N-methyl-D-aspartate type of glutamat... |
PMC9160115 | core_pubmed_pmc | A Novel Faster-Acting, Dry Powder-Based, Naloxone Intranasal Formulation for Opioid Overdose | A Novel Faster-Acting, Dry Powder-Based, Naloxone Intranasal Formulation for Opioid Overdose Abstract Abstract Objective To examine the pharmacokinetics and safety of FMXIN001, a new intranasal powder-based naloxone formulation, in comparison to Narcan® nasal liquid spray. Methods FMXIN001, was developed by blending dr... |
PMC3191504 | core_pubmed_pmc | Pharmacokinetics and clinical activity of very low-dose alemtuzumab in transplantation for acute leukemia | Pharmacokinetics and clinical activity of very low-dose alemtuzumab in transplantation for acute leukemia Abstract The optimal dose of in vivo -administrated alemtuzumab in the allogeneic transplantation setting has not been defined. We report our experience on 37 patients with high-risk diseases, mainly acute leukemia... |
PMC9320886 | core_pubmed_pmc | Daily Intraperitoneal Administration of Rosiglitazone Does Not Improve Lung Function or Alveolarization in Preterm Rabbits Exposed to Hyperoxia | Daily Intraperitoneal Administration of Rosiglitazone Does Not Improve Lung Function or Alveolarization in Preterm Rabbits Exposed to Hyperoxia Abstract Thiazolidinediones (TZDs) are potent PPARγ agonists that have been shown to attenuate alveolar simplification after prolonged hyperoxia in term rodent models of bronch... |
PMC6389873 | core_pubmed_pmc | The Role of Adherence Thresholds for Development and Performance Aspects of a Prediction Model for Direct Oral Anticoagulation Adherence | The Role of Adherence Thresholds for Development and Performance Aspects of a Prediction Model for Direct Oral Anticoagulation Adherence Abstract Patients who do not sufficiently adhere to their dosing regimens will, ultimately, do not get the full benefit of their medication. For example, if direct oral anticoagulants... |
PMC4816807 | core_pubmed_pmc | Safety and Upper Respiratory Pharmacokinetics of the Hemagglutinin Stalk-Binding Antibody VIS410 Support Treatment and Prophylaxis Based on Population Modeling of Seasonal Influenza A Outbreaks | Safety and Upper Respiratory Pharmacokinetics of the Hemagglutinin Stalk-Binding Antibody VIS410 Support Treatment and Prophylaxis Based on Population Modeling of Seasonal Influenza A Outbreaks Abstract Abstract Background Seasonal influenza is a major public health concern in vulnerable populations. Here we investigat... |
PMC12280776 | core_pubmed_pmc | Donanemab (LY3002813) Phase 1b Study in Alzheimer's Disease: Rapid and Sustained Reduction of Brain Amyloid Measured by Florbetapir F18 Imaging | Donanemab (LY3002813) Phase 1b Study in Alzheimer's Disease: Rapid and Sustained Reduction of Brain Amyloid Measured by Florbetapir F18 Imaging Abstract Abstract Background Donanemab (LY3002813) is an IgG1 antibody directed at an N-terminal pyroglutamate of amyloid beta epitope that is present only in brain amyloid pla... |
PMC9311151 | core_pubmed_pmc | Anticonvulsive properties of soticlestat, a novel cholesterol 24‐hydroxylase inhibitor | Anticonvulsive properties of soticlestat, a novel cholesterol 24‐hydroxylase inhibitor Abstract Abstract Objective The formation of 24 S ‐hydroxycholesterol is a brain‐specific mechanism of cholesterol catabolism catalyzed by cholesterol 24‐hydroxylase (CYP46A1, also known as CH24H). CH24H has been implicated in variou... |
PMC12548419 | core_pubmed_pmc | An orally available 4 ' -fluorouridine prodrug inhibits SFTSV and LCMV infection | An orally available 4 ' -fluorouridine prodrug inhibits SFTSV and LCMV infection Abstract ABSTRACT Bunyaviruses, a subset of segmented negative-sense RNA viruses, include pathogenic species capable of zoonotic transmission to humans via arthropod vectors and rodent hosts. Pathogenic bunyavirus infections can cause seve... |
PMC12703924 | core_pubmed_pmc | Comparative pharmacokinetic and bioequivalence of nine oral ivermectin formulations in dogs | Comparative pharmacokinetic and bioequivalence of nine oral ivermectin formulations in dogs Abstract Abstract Importance Canine heartworm disease remains a major global health issue. Despite the wide availability of ivermectin (IVM) formulations, pharmacokinetic and bioequivalence data are limited. Objective This study... |
PMC8420755 | core_pubmed_pmc | Murine cancer cachexia models replicate elevated catabolic pembrolizumab clearance in humans | Murine cancer cachexia models replicate elevated catabolic pembrolizumab clearance in humans Abstract Abstract Background Monoclonal antibody (mAb) immune checkpoint inhibitor (ICI) therapies have dramatically impacted oncology this past decade. However, only about one‐third of patients respond to treatment, and biomar... |
PMC9025623 | core_pubmed_pmc | Antibiotic Therapy for Prosthetic Joint Infections: An Overview | Antibiotic Therapy for Prosthetic Joint Infections: An Overview Abstract Abstract Prosthetic joint infection (PJI) is a severe complication after arthroplasty. Its management combines surgical intervention, whose type depends on the clinical situation, and prolonged high-dose antibiotics adapted to the responsible micr... |
PMC10145013 | core_pubmed_pmc | Comparison of Compartmental and Non-Compartmental Analysis to Detect Biopharmaceutical Similarity of Intravenous Nanomaterial-Based Rifabutin Formulations | Comparison of Compartmental and Non-Compartmental Analysis to Detect Biopharmaceutical Similarity of Intravenous Nanomaterial-Based Rifabutin Formulations Abstract Pharmacometric analysis is often used to quantify the differences and similarities between formulation prototypes. In the regulatory framework, it plays a s... |
PMC10819767 | core_pubmed_pmc | An ADAM10 Exosite Inhibitor Is Efficacious in an In Vivo Collagen-Induced Arthritis Model | An ADAM10 Exosite Inhibitor Is Efficacious in an In Vivo Collagen-Induced Arthritis Model Abstract Abstract Rheumatoid arthritis is a systemic autoimmune inflammatory disease that affects millions of people worldwide. There are multiple disease-modifying anti-rheumatic drugs available; however, many patients do not res... |
PMC7866082 | core_pubmed_pmc | Design and Synthesis of Novel Imidazole Derivatives Possessing Triazole Pharmacophore with Potent Anticancer Activity, and In Silico ADMET with GSK-3β Molecular Docking Investigations | Design and Synthesis of Novel Imidazole Derivatives Possessing Triazole Pharmacophore with Potent Anticancer Activity, and In Silico ADMET with GSK-3β Molecular Docking Investigations Abstract A library of novel imidazole-1,2,3-triazole hybrids were designed and synthesized based on the hybrid pharmacophore approach. T... |
PMC11729431 | core_pubmed_pmc | Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling of Erythroferrone in Anemic Rats with Chronic Kidney Disease and Chemotherapy-Induced Anemia: An Early Biomarker for Hemoglobin Response and rHuEPO Hyporesponsiveness | Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling of Erythroferrone in Anemic Rats with Chronic Kidney Disease and Chemotherapy-Induced Anemia: An Early Biomarker for Hemoglobin Response and rHuEPO Hyporesponsiveness Abstract Erythroferrone (ERFE) has emerged as a potential biomarker for the erythropoiesis respo... |
PMC5054534 | core_pubmed_pmc | Species Comparison of Pre-systemic Bioactivation of Vicagrel, a New Acetate Derivative of Clopidogrel | Species Comparison of Pre-systemic Bioactivation of Vicagrel, a New Acetate Derivative of Clopidogrel Abstract Previously we have found vicagrel, a new acetate derivative of clopidogrel, underwent hydrolysis to 2-oxo-clopidogrel and subsequent conversions to its pharmacological active metabolite (AM) and inactive carbo... |
PMC3272225 | core_pubmed_pmc | Effect of Mycophenolate Mofetil on Plasma Bioelements in Renal Transplant Recipients | Effect of Mycophenolate Mofetil on Plasma Bioelements in Renal Transplant Recipients Abstract The proper concentrations of plasma bioelements may favorably reduce the incidence of metabolic disorders, which often occur during immunosuppressive therapy. Mycophenolate mofetil (MMF) is currently one of the most frequently... |
PMC8746970 | core_pubmed_pmc | Determination of the Peptide AWRK6 in Rat Plasma by Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) and Its Application to Pharmacokinetics | Determination of the Peptide AWRK6 in Rat Plasma by Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) and Its Application to Pharmacokinetics Abstract AWRK6 was a synthesized peptide developed based on the natural occurring peptide dybowskin-2CDYa, which was discovered in frog skin in our previous study. Here, ... |
PMC8958973 | core_pubmed_pmc | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning Abstract Recent events demonstrated that organophosphorus nerve agents are a serious threat for civilian and military populations. The current therapy includes a pyridinium aldoxime reactivator to restore the enzymatic act... |
PMC5048606 | core_pubmed_pmc | Validated determination method of tramadol and its desmethylates in human plasma using an isocratic LC-MS/MS and its clinical application to patients with cancer pain or non-cancer pain | Validated determination method of tramadol and its desmethylates in human plasma using an isocratic LC-MS/MS and its clinical application to patients with cancer pain or non-cancer pain Abstract Background This study aimed to develop a simultaneous determination method for tramadol and its desmethylates in human plasma... |
PMC6592555 | core_pubmed_pmc | Development of a physiologically-based pharmacokinetic pediatric brain model for prediction of cerebrospinal fluid drug concentrations and the influence of meningitis | Development of a physiologically-based pharmacokinetic pediatric brain model for prediction of cerebrospinal fluid drug concentrations and the influence of meningitis Abstract Different pediatric physiologically-based pharmacokinetic (PBPK) models have been described incorporating developmental changes that influence p... |
PMC7011679 | core_pubmed_pmc | The Possibility of Therapeutic Drug Monitoring of the Most Important Interactions in Nursing Homes | The Possibility of Therapeutic Drug Monitoring of the Most Important Interactions in Nursing Homes Abstract Abstract Background Therapeutic drug monitoring is a relevant tool in drug treatment of elderly patients. The aim of this study was to assess the possibility of therapeutic drug monitoring of the most important p... |
PMC8691013 | core_pubmed_pmc | Exploring population pharmacokinetic models in patients treated with vancomycin during continuous venovenous haemodiafiltration (CVVHDF) | Exploring population pharmacokinetic models in patients treated with vancomycin during continuous venovenous haemodiafiltration (CVVHDF) Abstract Background Therapeutic antibiotic dose monitoring can be particularly challenging in septic patients requiring renal replacement therapy. Our aim was to conduct an explorator... |
PMC11706425 | core_pubmed_pmc | PBPK modeling: What is the role of CYP3A4 expression in the gastrointestinal tract to accurately predict first‐pass metabolism? | PBPK modeling: What is the role of CYP3A4 expression in the gastrointestinal tract to accurately predict first‐pass metabolism? Abstract Abstract Gastrointestinal first‐pass metabolism plays an important role in bioavailability and in drug–drug interactions. Physiologically‐based pharmacokinetic (PBPK) modeling is a po... |
PMC3329467 | core_pubmed_pmc | Stereoselective Regulations of P-Glycoprotein by Ginsenoside Rh2 Epimers and the Potential Mechanisms From the View of Pharmacokinetics | Stereoselective Regulations of P-Glycoprotein by Ginsenoside Rh2 Epimers and the Potential Mechanisms From the View of Pharmacokinetics Abstract Abstract Chirality is an interesting topic and it is meaningful to explore the interactions between chiral small molecules and stereoselective biomacromolecules, with pre-clin... |
PMC10880554 | core_pubmed_pmc | Opportunities and Challenges for Inhalable Nanomedicine Formulations in Respiratory Diseases: A Review | Opportunities and Challenges for Inhalable Nanomedicine Formulations in Respiratory Diseases: A Review Abstract Abstract Lungs experience frequent interactions with the external environment and have an abundant supply of blood; therefore, they are susceptible to invasion by pathogenic microorganisms and tumor cells. Ho... |
PMC10568689 | core_pubmed_pmc | Predictive Models Based on Molecular Images and Molecular Descriptors for Drug Screening | Predictive Models Based on Molecular Images and Molecular Descriptors for Drug Screening Abstract Various toxicity and pharmacokinetic evaluations as screening experiments are needed at the drug discovery stage. Currently, to reduce the use of animal experiments and developmental expenses, the development of high-perfo... |
PMC9774413 | core_pubmed_pmc | When and How to Use MIC in Clinical Practice? | When and How to Use MIC in Clinical Practice? Abstract Bacterial resistance to antibiotics continues to be a global public health problem. The choice of the most effective antibiotic and the use of an adapted dose in the initial phase of the infection are essential to limit the emergence of resistance. This will depend... |
PMC6927930 | core_pubmed_pmc | Meta-Analysis of Pharmacokinetic Studies of Nanobiomaterials for the Prediction of Excretion Depending on Particle Characteristics | Meta-Analysis of Pharmacokinetic Studies of Nanobiomaterials for the Prediction of Excretion Depending on Particle Characteristics Abstract The growth in development and use of nanobiomaterials (NBMs) has raised questions regarding their possible distribution in the environment. Because most NBMs are not yet available ... |
PMC10535808 | core_pubmed_pmc | Translational Pharmacokinetic/Pharmacodynamic Modeling and Simulation of Oxaliplatin and Irinotecan in Colorectal Cancer | Translational Pharmacokinetic/Pharmacodynamic Modeling and Simulation of Oxaliplatin and Irinotecan in Colorectal Cancer Abstract Abstract Despite the recent advances in this field, there are limited methods for translating organoid-based study results to clinical response. The goal of this study was to develop a pharm... |
PMC8129715 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling to predict drug interactions of lemborexant with CYP3A inhibitors | Physiologically‐based pharmacokinetic modeling to predict drug interactions of lemborexant with CYP3A inhibitors Abstract Abstract Lemborexant, a recently approved dual orexin receptor antagonist for treatment of adults with insomnia, is eliminated primarily by cytochrome P450 (CYP)3A metabolism. The recommended dose o... |
PMC12263744 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Intranasal Diacetylmorphine in Heroin-Assisted Treatment for Severe Opioid Use Disorder | Pharmacokinetics and Pharmacodynamics of Intranasal Diacetylmorphine in Heroin-Assisted Treatment for Severe Opioid Use Disorder Abstract Background Intranasal diacetylmorphine (IN DAM) represents a promising new route of administration, which is currently under investigation as a novel treatment approach for opioid us... |
PMC6287190 | core_pubmed_pmc | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome | Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome Abstract Abstract Apart from well-known functions of bile acids in digestion and solubilization of lipophilic nutrients and drugs in the small intestine, the emerging evidence from the past two decades identified the... |
PMC7545998 | core_pubmed_pmc | A snake toxin as a theranostic agent for the type 2 vasopressin receptor | A snake toxin as a theranostic agent for the type 2 vasopressin receptor Abstract Rationale: MQ1, a snake toxin which targets with high nanomolar affinity and absolute selectivity for the type 2 vasopressin receptor (V2R), is a drug candidate for renal diseases and a molecular probe for imaging cells or organs expressi... |
PMC6369428 | core_pubmed_pmc | Efflux Inhibitor Bicalutamide Increases Oral Bioavailability of the Poorly Soluble Efflux Substrate Docetaxel in Co-Amorphous Anti-Cancer Combination Therapy | Efflux Inhibitor Bicalutamide Increases Oral Bioavailability of the Poorly Soluble Efflux Substrate Docetaxel in Co-Amorphous Anti-Cancer Combination Therapy Abstract Many anti-cancer drugs are difficult to formulate into an oral dosage form because they are both poorly water-soluble and show poor permeability, the lat... |
PMC10712305 | core_pubmed_pmc | The effect of icotinib or apatinib on the pharmacokinetic profile of oxycodone in rats and the underlying mechanism | The effect of icotinib or apatinib on the pharmacokinetic profile of oxycodone in rats and the underlying mechanism Abstract Abstract This study aimed to investigate the interactions between icotinib/apatinib and oxycodone in rats and to unveil the underlying mechanism. An ultra-performance liquid chromatography–tandem... |
PMC10384157 | core_pubmed_pmc | Pharmacokinetics of Curcumin Delivered by Nanoparticles and the Relationship with Antitumor Efficacy: A Systematic Review | Pharmacokinetics of Curcumin Delivered by Nanoparticles and the Relationship with Antitumor Efficacy: A Systematic Review Abstract Abstract Curcumin is a polyphenolic compound, derived from Curcuma longa, and it has several pharmacological effects such as antioxidant, anti-inflammatory, and antitumor. Although it is a ... |
PMC12119998 | core_pubmed_pmc | Computational and biological modeling of IGF1R inhibition for multifocal medulloblastoma | Computational and biological modeling of IGF1R inhibition for multifocal medulloblastoma Abstract Background Leptomeningeal metastasis in medulloblastoma poses challenges for effective treatments due to the blood–brain barrier (BBB), which may be addressed through intrathecal or intraventricular drug delivery. However,... |
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