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PMC7497078 | core_pubmed_pmc | Evaluation of Pharmacokinetics and Dose Proportionality of Diazepam After Intranasal Administration of NRL‐1 to Healthy Volunteers | Evaluation of Pharmacokinetics and Dose Proportionality of Diazepam After Intranasal Administration of NRL‐1 to Healthy Volunteers Abstract Abstract NRL‐1 is a novel intranasal formulation of diazepam that is being evaluated as rescue medication in patients with epilepsy who experience bouts of increased seizure activi... |
PMC7376288 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Response of Luspatercept, an Erythroid Maturation Agent, in Anemic Patients With Myelodysplastic Syndromes | Population Pharmacokinetics and Exposure–Response of Luspatercept, an Erythroid Maturation Agent, in Anemic Patients With Myelodysplastic Syndromes Abstract Luspatercept is a recombinant fusion protein that enhances late‐stage erythroid maturation. This report describes the population pharmacokinetics and exposure–resp... |
PMC10157364 | core_pubmed_pmc | Preclinical Evaluation of ON203, A Novel Bioengineered mAb Targeting Oxidized Macrophage Migration Inhibitory Factor as an Anticancer Therapeutic | Preclinical Evaluation of ON203, A Novel Bioengineered mAb Targeting Oxidized Macrophage Migration Inhibitory Factor as an Anticancer Therapeutic Abstract Abstract High levels of macrophage migration inhibitory factor (MIF) in patients with cancer are associated with poor prognosis. Its redox-dependent conformational i... |
PMC12823316 | core_pubmed_pmc | Neural Controlled Differential Equation and Its Application in Pharmacokinetics and Pharmacodynamics | Neural Controlled Differential Equation and Its Application in Pharmacokinetics and Pharmacodynamics Abstract ABSTRACT With the recent advances in machine learning (ML) and artificial intelligence (AI), data‐driven modeling approaches for pharmacokinetics (PK) and pharmacodynamics (PD) have gained popularity due to the... |
PMC3693428 | core_pubmed_pmc | Fluticasone Furoate, a Novel Inhaled Corticosteroid, Demonstrates Prolonged Lung Absorption Kinetics in Man Compared with Inhaled Fluticasone Propionate | Fluticasone Furoate, a Novel Inhaled Corticosteroid, Demonstrates Prolonged Lung Absorption Kinetics in Man Compared with Inhaled Fluticasone Propionate Abstract Abstract Background Fluticasone furoate (FF; GW685698 ) is a novel inhaled corticosteroid that is active at 24 h and under development for once-daily administ... |
PMC6699497 | core_pubmed_pmc | Validated UPLC-MS/MS method for quantification of fruquintinib in rat plasma and its application to pharmacokinetic study | Validated UPLC-MS/MS method for quantification of fruquintinib in rat plasma and its application to pharmacokinetic study Abstract Abstract A new, simple, and sensitive ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for quantification of fruquintinib was established to assess the ph... |
PMC5613184 | core_pubmed_pmc | Population Pharmacokinetics/Pharmacodynamics of 3,4‐Diaminopyridine Free Base in Patients With Lambert‐Eaton Myasthenia | Population Pharmacokinetics/Pharmacodynamics of 3,4‐Diaminopyridine Free Base in Patients With Lambert‐Eaton Myasthenia Abstract Lambert‐Eaton myasthenia (LEM) is a rare autoimmune disorder associated with debilitating muscle weakness. There are limited treatment options and 3,4‐diaminopyridine (3,4‐DAP) free base is a... |
PMC11292879 | core_pubmed_pmc | Influence of aging on opioid dosing for perioperative pain management: a focus on pharmacokinetics | Influence of aging on opioid dosing for perioperative pain management: a focus on pharmacokinetics Abstract Abstract The older population continues to grow in all countries, and surgeons are encountering older patients more frequently. The management of postoperative pain in older patients can be a difficult task. Opio... |
PMC10126531 | core_pubmed_pmc | Population Pharmacokinetics and Probability of Target Attainment Analysis of Nadroparin in Different Stages of COVID-19 | Population Pharmacokinetics and Probability of Target Attainment Analysis of Nadroparin in Different Stages of COVID-19 Abstract Abstract Background and Objective The risk of thrombotic complications in critical patients with COVID-19 remains extremely high, and multicenter trials failed to prove a survival benefit of ... |
PMC9611668 | core_pubmed_pmc | Controversial Interactions of Tacrolimus with Dietary Supplements, Herbs and Food | Controversial Interactions of Tacrolimus with Dietary Supplements, Herbs and Food Abstract Tacrolimus is an immunosuppressive calcineurin inhibitor used to prevent rejection in allogeneic organ transplant recipients, such as kidney, liver, heart or lung. It is metabolized in the liver, involving the cytochrome P450 (CY... |
PMC6921606 | core_pubmed_pmc | Mass Spectrometry Imaging Demonstrates the Regional Brain Distribution Patterns of Three First-Line Antiretroviral Drugs | Mass Spectrometry Imaging Demonstrates the Regional Brain Distribution Patterns of Three First-Line Antiretroviral Drugs Abstract Abstract HIV in the central nervous system (CNS) contributes to the development of HIV-associated neurological disorders (HAND), even with chronic antiretroviral therapy. In order for antire... |
PMC3234127 | core_pubmed_pmc | Combining antihypertensive and antihyperlipidemic agents – optimizing cardiovascular risk factor management | Combining antihypertensive and antihyperlipidemic agents – optimizing cardiovascular risk factor management Abstract Clinical guidelines now recognize the importance of a multifactorial approach to managing cardiovascular (CV) risk. This idea was taken a step further with the concept of the Polypill™. There are, howeve... |
PMC9292820 | core_pubmed_pmc | First‐in‐human trial to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of STR‐324, a dual enkephalinase inhibitor for pain management | First‐in‐human trial to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of STR‐324, a dual enkephalinase inhibitor for pain management Abstract Aim Dual enkephalinase inhibitors (DENKIs) are involved in the regulation of nociception via opioid receptors. The novel compound STR‐324 belongs to the ... |
PMC10421490 | core_pubmed_pmc | Antioxidant, Volatile Compounds; Antimicrobial, Anti-Inflammatory, and Dermatoprotective Properties of Cedrus atlantica (Endl.) Manetti Ex Carriere Essential Oil: In Vitro and In Silico Investigations | Antioxidant, Volatile Compounds; Antimicrobial, Anti-Inflammatory, and Dermatoprotective Properties of Cedrus atlantica (Endl.) Manetti Ex Carriere Essential Oil: In Vitro and In Silico Investigations Abstract Abstract Cedrus atlantica (Endl.) Manetti ex Carriere is an endemic tree possessing valuable health benefits w... |
PMC5555058 | core_pubmed_pmc | Evaluation of evidence for pharmacokinetics-pharmacodynamics-based dose optimization of antimicrobials for treating Gram-negative infections in neonates | Evaluation of evidence for pharmacokinetics-pharmacodynamics-based dose optimization of antimicrobials for treating Gram-negative infections in neonates Abstract Abstract Background & objectives: Neonates present a special subgroup of population in whom optimization of antimicrobial dosing can be particularly challengi... |
PMC6585844 | core_pubmed_pmc | Open‐Label, Dose‐Escalation, Phase 1 Study of Safety and Single and Multiple‐Dose Pharmacokinetics of Dichlorphenamide in Healthy Volunteers | Open‐Label, Dose‐Escalation, Phase 1 Study of Safety and Single and Multiple‐Dose Pharmacokinetics of Dichlorphenamide in Healthy Volunteers Abstract Abstract Single‐and multiple‐dose pharmacokinetics and safety were investigated in this phase 1 study of dichlorphenamide, a carbonic anhydrase inhibitor approved in the ... |
PMC9546314 | core_pubmed_pmc | Does difference between label and actual potency of factor VIII concentrate affect pharmacokinetic‐guided dosing of replacement therapy in haemophilia A? | Does difference between label and actual potency of factor VIII concentrate affect pharmacokinetic‐guided dosing of replacement therapy in haemophilia A? Abstract Abstract Background To account for interindividual variability in the pharmacokinetics (PK) of factor concentrates, PK‐guided dosing is increasingly implemen... |
PMC9867512 | core_pubmed_pmc | Data-Driven Approaches Used for Compound Library Design for the Treatment of Parkinson’s Disease | Data-Driven Approaches Used for Compound Library Design for the Treatment of Parkinson’s Disease Abstract Abstract Parkinson’s disease (PD) is the second most common neurodegenerative disease in older individuals worldwide. Pharmacological treatment for such a disease consists of drugs such as monoamine oxidase B (MAO-... |
PMC11676928 | core_pubmed_pmc | Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data | Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data Abstract Abstract Background/Objectives: Early stages of diabetic retinopathy are currently considered an unmet medical need due to the lack of effective treatments beyond proper monitoring and control of glycemia and blood pressure. Sitaglip... |
PMC9504371 | core_pubmed_pmc | Revisiting Cerebrospinal Fluid Flow Direction and Rate in Physiologically Based Pharmacokinetic Model | Revisiting Cerebrospinal Fluid Flow Direction and Rate in Physiologically Based Pharmacokinetic Model Abstract Abstract The bidirectional pulsatile movement of cerebrospinal fluid (CSF), instead of the traditionally believed unidirectional and constant CSF circulation, has been demonstrated. In the present study, the s... |
PMC7511473 | core_pubmed_pmc | Pharmacokinetics and Safety of Dabigatran Etexilate after Single and Multiple Oral Doses in Healthy Chinese Subjects | Pharmacokinetics and Safety of Dabigatran Etexilate after Single and Multiple Oral Doses in Healthy Chinese Subjects Abstract Abstract Background and Objective Dabigatran etexilate is a non-vitamin K antagonist oral anticoagulant (NOAC) that is used to prevent stroke and systemic embolism in adults with nonvalvular atr... |
PMC11423992 | core_pubmed_pmc | TFAB002s, novel CD20-targeting T cell-dependent bispecific Fab-FabCH3 antibodies, exhibit potent antitumor efficacy against malignant B-cell lymphoma | TFAB002s, novel CD20-targeting T cell-dependent bispecific Fab-FabCH3 antibodies, exhibit potent antitumor efficacy against malignant B-cell lymphoma Abstract Abstract B-cell lymphoma, clinically, comprises a heterogeneous group of malignancies that encompass various subtypes. CD20 is an optimal target for therapeutic ... |
PMC10148758 | core_pubmed_pmc | Pathogen-based target attainment of optimized continuous infusion dosing regimens of piperacillin-tazobactam and meropenem in surgical ICU patients: a prospective single center observational study | Pathogen-based target attainment of optimized continuous infusion dosing regimens of piperacillin-tazobactam and meropenem in surgical ICU patients: a prospective single center observational study Abstract Background Several studies have indicated that commonly used piperacillin-tazobactam (TZP) and meropenem (MEM) dos... |
PMC9521280 | core_pubmed_pmc | A pharmacodynamic investigation to assess the synergism of orbifloxacin and propyl gallate against Escherichia coli | A pharmacodynamic investigation to assess the synergism of orbifloxacin and propyl gallate against Escherichia coli Abstract Abstract Escherichia coli ( E. coli ) infections are becoming increasingly difficult to treat, as antibiotic-resistant variants proliferate. Studies on novel methods to combat the spread of resis... |
PMC12696360 | core_pubmed_pmc | Safety and clinical outcomes of pembrolizumab standard-interval dosing versus extended-interval dosing in patients with breast cancer | Safety and clinical outcomes of pembrolizumab standard-interval dosing versus extended-interval dosing in patients with breast cancer Abstract Abstract Introduction Extended-interval (EI) dosing of pembrolizumab (400 mg IV every 6 weeks) was approved across all solid tumors based on pharmacokinetic modeling and exposur... |
PMC6572291 | core_pubmed_pmc | DPYD and Fluorouracil-Based Chemotherapy: Mini Review and Case Report | DPYD and Fluorouracil-Based Chemotherapy: Mini Review and Case Report Abstract 5-Fluorouracil remains a foundational component of chemotherapy for solid tumour malignancies. While considered a generally safe and effective chemotherapeutic, 5-fluorouracil has demonstrated severe adverse event rates of up to 30%. Underst... |
PMC7854423 | core_pubmed_pmc | Anticonvulsant Effectiveness and Neurotoxicity Profile of 4-butyl-5-[(4-chloro-2-methylphenoxy)methyl]-2,4-dihydro-3 H -1,2,4-triazole-3-thione (TPL-16) in Mice | Anticonvulsant Effectiveness and Neurotoxicity Profile of 4-butyl-5-[(4-chloro-2-methylphenoxy)methyl]-2,4-dihydro-3 H -1,2,4-triazole-3-thione (TPL-16) in Mice Abstract Protective (antiseizure) effects of 4-butyl-5-[(4-chloro-2-methylphenoxy)-methyl]-2,4-dihydro-3 H -1,2,4-triazole-3-thione (TPL-16) and acute neurotox... |
PMC7281310 | core_pubmed_pmc | Pharmacokinetic Analysis of Epithelial/Endothelial Cell Barriers in Microfluidic Bilayer Devices with an Air–Liquid Interface | Pharmacokinetic Analysis of Epithelial/Endothelial Cell Barriers in Microfluidic Bilayer Devices with an Air–Liquid Interface Abstract Abstract As the range of applications of organs-on-chips is broadening, the evaluation of aerosol-based therapies using a lung-on-a-chip model has become an attractive approach. Inhalat... |
PMC7226106 | core_pubmed_pmc | Population Pharmacokinetics/Pharmacodynamics of Dabrafenib Plus Trametinib in Patients with BRAF-Mutated Metastatic Melanoma | Population Pharmacokinetics/Pharmacodynamics of Dabrafenib Plus Trametinib in Patients with BRAF-Mutated Metastatic Melanoma Abstract Patients treated with dabrafenib/trametinib (DAB/TRA) exhibit a large interindividual variability in clinical outcomes. The aims of this study were to characterize the pharmacokinetics o... |
PMC9420618 | core_pubmed_pmc | A Retrospective Cohort Study of the Efficacy, Safety, and Clinical Value of 6-TG versus 6-MP Maintenance Therapy in Children with Acute Lymphoblastic Leukemia | A Retrospective Cohort Study of the Efficacy, Safety, and Clinical Value of 6-TG versus 6-MP Maintenance Therapy in Children with Acute Lymphoblastic Leukemia Abstract Abstract Objective To explore the efficacy, safety, and clinical value of 6-TG versus 6-MP when treating childhood acute lymphoblastic leukemia (ALL). M... |
PMC6130456 | core_pubmed_pmc | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport Abstract Abstract Context: Diclofenac and celastrol are always used together for the treatment of rheumatoid arthritis; the herb–drug interaction potential between diclofenac and celastrol is still unknown. Objective: This study invest... |
PMC12297353 | core_pubmed_pmc | Identification of potential VP40 inhibitor of Marburg virus through molecular docking, pharmacokinetic analysis and molecular dynamics simulation | Identification of potential VP40 inhibitor of Marburg virus through molecular docking, pharmacokinetic analysis and molecular dynamics simulation Abstract Abstract West Africa has been experiencing a resurgence of Marburg virus disease (MVD), a zoonotic pathogen that causes severe hemorrhagic fever in both humans and p... |
PMC9383688 | core_pubmed_pmc | Development and evaluation of a bovine lung-on-chip (bLOC) to study bovine respiratory diseases | Development and evaluation of a bovine lung-on-chip (bLOC) to study bovine respiratory diseases Abstract Purpose Current air-liquid interface (ALI) models of bovine proximal airways have their limitations. They do not simulate blood flow necessary to mimic systemic drug administration, and repeated sampling requires mu... |
PMC11357675 | core_pubmed_pmc | Stimulating the Antitumor Immune Response Using Immunocytokines: A Preclinical and Clinical Overview | Stimulating the Antitumor Immune Response Using Immunocytokines: A Preclinical and Clinical Overview Abstract Abstract Cytokines are immune modulators which can enhance the immune response and have been proven to be an effective class of immunotherapy. Nevertheless, the clinical use of cytokines in cancer treatment has... |
PMC8752527 | core_pubmed_pmc | A Drug–Drug Interaction Study to Investigate the Effect of Nintedanib on the Pharmacokinetics of Microgynon (Ethinylestradiol and Levonorgestrel) in Female Patients with Systemic Sclerosis-Associated Interstitial Lung Disease | A Drug–Drug Interaction Study to Investigate the Effect of Nintedanib on the Pharmacokinetics of Microgynon (Ethinylestradiol and Levonorgestrel) in Female Patients with Systemic Sclerosis-Associated Interstitial Lung Disease Abstract Background and Objectives Nintedanib is a tyrosine kinase inhibitor approved for the ... |
PMC8183773 | core_pubmed_pmc | Bendamustine treatment of Chinese patients with relapsed indolent non-Hodgkin lymphoma: a multicenter, open-label, single-arm, phase 3 study | Bendamustine treatment of Chinese patients with relapsed indolent non-Hodgkin lymphoma: a multicenter, open-label, single-arm, phase 3 study Abstract Abstract Background: Bendamustine was approved in China on May 26th, 2019 by the National Medical Product Administration for the treatment of indolent B-cell non-Hodgkin ... |
PMC9007606 | core_pubmed_pmc | Model‐based meta‐analysis of salbutamol pharmacokinetics and practical implications for doping control | Model‐based meta‐analysis of salbutamol pharmacokinetics and practical implications for doping control Abstract Abstract Salbutamol was included in the prohibited list of the World Anti‐Doping Agency (WADA) in 2004. Although systemic intake is banned, inhalation for asthma is permitted but with dosage restrictions. The... |
PMC2846148 | core_pubmed_pmc | New atypical antipsychotics for schizophrenia: iloperidone | New atypical antipsychotics for schizophrenia: iloperidone Abstract Abstract The optimal treatment of schizophrenia poses a challenge to develop more effective treatments and safer drugs, to overcome poor compliance, discontinuation and frequent switching with available antipsychotics. Iloperidone is a new dopamine typ... |
PMC5988193 | core_pubmed_pmc | Impact of body weight, low energy diet and gastric bypass on drug bioavailability, cardiovascular risk factors and metabolic biomarkers: protocol for an open, non-randomised, three-armed single centre study (COCKTAIL) | Impact of body weight, low energy diet and gastric bypass on drug bioavailability, cardiovascular risk factors and metabolic biomarkers: protocol for an open, non-randomised, three-armed single centre study (COCKTAIL) Abstract Introduction Roux-en-Y gastric bypass (GBP) is associated with changes in cardiometabolic ris... |
PMC12969023 | core_pubmed_pmc | Retinal organoid screening reveals ABT-737 and luminespib as potential agents against a cone- precursor-derived subtype of retinoblastoma | Retinal organoid screening reveals ABT-737 and luminespib as potential agents against a cone- precursor-derived subtype of retinoblastoma Abstract Abstract Retinoblastoma (Rb) features proliferating cone precursors, particularly those in the G2/M phase, as a major driver population revealed by recent single-cell transc... |
PMC9292875 | core_pubmed_pmc | Concentration‐QT modelling shows no evidence of clinically significant QT interval prolongation with capivasertib at expected therapeutic concentrations | Concentration‐QT modelling shows no evidence of clinically significant QT interval prolongation with capivasertib at expected therapeutic concentrations Abstract Pharmacokinetics‐matched digital electrocardiogram data ( n = 503 measurements from 180 patients) collected in a first‐in‐human, multi‐part, dose‐escalation (... |
PMC10319141 | core_pubmed_pmc | Imidazoquinolines with improved pharmacokinetic properties induce a high IFNα to TNFα ratio in vitro and in vivo | Imidazoquinolines with improved pharmacokinetic properties induce a high IFNα to TNFα ratio in vitro and in vivo Abstract Abstract TLR Agonists have promising activity in preclinical models of viral infection and cancer. However, clinical use is only in topical application. Systemic uses of TLR-ligands such as Resiquim... |
PMC8674001 | core_pubmed_pmc | Tutorial for $DESIGN in NONMEM: Clinical trial evaluation and optimization | Tutorial for $DESIGN in NONMEM: Clinical trial evaluation and optimization Abstract Abstract This NONMEM tutorial shows how to evaluate and optimize clinical trial designs, using algorithms developed in design software, such as PopED and PFIM 4.0. Parameter precision and model parameter estimability is obtained by asse... |
PMC4026633 | core_pubmed_pmc | Systems Pharmacology Models Can Be Used to Understand Complex Pharmacokinetic-Pharmacodynamic Behavior: An Example Using 5-Lipoxygenase Inhibitors | Systems Pharmacology Models Can Be Used to Understand Complex Pharmacokinetic-Pharmacodynamic Behavior: An Example Using 5-Lipoxygenase Inhibitors Abstract Zileuton, a 5-lipoxygenase (5LO) inhibitor, displays complex pharmaokinetic (PK)-pharmacodynamic (PD) behavior. Available clinical data indicate a lack of dose–bron... |
PMC6241247 | core_pubmed_pmc | Development and Application of an UHPLC-MS/MS Method for Comparative Pharmacokinetic Study of Eight Major Bioactive Components from Yin Chen Hao Tang in Normal and Acute Liver Injured Rats | Development and Application of an UHPLC-MS/MS Method for Comparative Pharmacokinetic Study of Eight Major Bioactive Components from Yin Chen Hao Tang in Normal and Acute Liver Injured Rats Abstract Yin Chen Hao Tang (YCHT) is one of the most famous hepatoprotective herbal formulas in China, but its pharmacokinetic inve... |
PMC10082801 | core_pubmed_pmc | Heroin and its metabolites: relevance to heroin use disorder | Heroin and its metabolites: relevance to heroin use disorder Abstract Heroin is an opioid agonist commonly abused for its rewarding effects. Since its synthesis at the end of the nineteenth century, its popularity as a recreational drug has ebbed and flowed. In the last three decades, heroin use has increased again, an... |
PMC5358997 | core_pubmed_pmc | Fixed-dose combination orally disintegrating tablets to treat cardiovascular disease: formulation, in vitro characterization and physiologically based pharmacokinetic modeling to assess bioavailability | Fixed-dose combination orally disintegrating tablets to treat cardiovascular disease: formulation, in vitro characterization and physiologically based pharmacokinetic modeling to assess bioavailability Abstract Cardiovascular disease (CVD) is the leading cause of death among men and women worldwide. In CVD, hypertensio... |
PMC4360666 | core_pubmed_pmc | Target Mediated Drug Disposition Model of CPHPC in Patients with Systemic Amyloidosis | Target Mediated Drug Disposition Model of CPHPC in Patients with Systemic Amyloidosis Abstract The amyloid deposits that cause disease in systemic amyloidosis always contain the normal plasma protein, serum amyloid P (SAP) component. SAP is the target of a novel immunotherapy approach now being developed to eliminate a... |
PMC10410934 | core_pubmed_pmc | DosEmi study protocol: a phase IV, multicentre, open-label, crossover study to evaluate non-inferiority of pharmacokinetic-guided reduced dosing compared with conventional dosing of emicizumab in people with haemophilia A | DosEmi study protocol: a phase IV, multicentre, open-label, crossover study to evaluate non-inferiority of pharmacokinetic-guided reduced dosing compared with conventional dosing of emicizumab in people with haemophilia A Abstract Introduction Emicizumab effectively prevents bleeding in people with haemophilia A (PwHA)... |
PMC12583985 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of the Long‐Acting SARS‐CoV‐2–Neutralizing Monoclonal Antibody Combination AZD7442 (Tixagevimab/Cilgavimab) in Healthy Chinese Adults | Safety, Tolerability, and Pharmacokinetics of the Long‐Acting SARS‐CoV‐2–Neutralizing Monoclonal Antibody Combination AZD7442 (Tixagevimab/Cilgavimab) in Healthy Chinese Adults Abstract Abstract AZD7442, a combination of extended half‐life monoclonal antibodies tixagevimab and cilgavimab, was shown to neutralize previo... |
PMC11299271 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic modelling of Saxagliptin and its active metabolite, 5-hydroxy Saxagliptin in rats with Type 2 Diabetes Mellitus | Pharmacokinetic/Pharmacodynamic modelling of Saxagliptin and its active metabolite, 5-hydroxy Saxagliptin in rats with Type 2 Diabetes Mellitus Abstract Abstract Background and purposes It is unclear whether the parent Saxagliptin (SAX) in vivo is the same as that in vitro, which is twice that of 5-hydroxy Saxagliptin ... |
PMC12568586 | core_pubmed_pmc | Mass spectrometry-guided discovery of novel GCPII inhibitor scaffolds | Mass spectrometry-guided discovery of novel GCPII inhibitor scaffolds Abstract Abstract Introduction There is an unmet need for therapeutics with a novel mechanism to address Q9 symptoms associated with conditions where aberrant glutamatergic neurotransmission is presumed pathogenic. One enzyme of potential relevance i... |
PMC3371467 | core_pubmed_pmc | Propofol pharmacokinetics in China: A multicentric study | Propofol pharmacokinetics in China: A multicentric study Abstract Objective: A multicenter population pharmacokinetics study of propofol was performed to establish a new population model. Materials and Methods: Three thousand two hundred and fifty-nine blood samples of 220 participants were measured by HPLC-UV or HPLC-... |
PMC11306728 | core_pubmed_pmc | When to consider intra-target microdosing: physiologically based pharmacokinetic modeling approach to quantitatively identify key factors for observing target engagement | When to consider intra-target microdosing: physiologically based pharmacokinetic modeling approach to quantitatively identify key factors for observing target engagement Abstract Abstract Intra-Target Microdosing (ITM), integral to Phase 0 clinical studies, offers a novel approach in drug development, effectively bridg... |
PMC10619015 | core_pubmed_pmc | First-in-human phase I/Ib study of NIZ985, a recombinant heterodimer of IL-15 and IL-15Rα, as a single agent and in combination with spartalizumab in patients with advanced and metastatic solid tumors | First-in-human phase I/Ib study of NIZ985, a recombinant heterodimer of IL-15 and IL-15Rα, as a single agent and in combination with spartalizumab in patients with advanced and metastatic solid tumors Abstract Background Preclinically, interleukin-15 (IL-15) monotherapy promotes antitumor immune responses, which are en... |
PMC7927850 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis | Population Pharmacokinetic Analysis of Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis Abstract A population pharmacokinetic (PopPK) model of delamanid in patients with pulmonary multidrug-resistant tuberculosis (MDR-TB) was developed using data from four delamanid clinical trials. The final PopPK... |
PMC5890607 | core_pubmed_pmc | Randomized, dose-ranging safety trial of cannabidiol in Dravet syndrome | Randomized, dose-ranging safety trial of cannabidiol in Dravet syndrome Abstract Abstract Objective To evaluate the safety and preliminary pharmacokinetics of a pharmaceutical formulation of purified cannabidiol (CBD) in children with Dravet syndrome. Methods Patients aged 4–10 years were randomized 4:1 to CBD (5, 10, ... |
PMC7260122 | core_pubmed_pmc | Phase I study of vemurafenib in children with recurrent or progressive BRAF V600E mutant brain tumors: Pacific Pediatric Neuro-Oncology Consortium study (PNOC-002) | Phase I study of vemurafenib in children with recurrent or progressive BRAF V600E mutant brain tumors: Pacific Pediatric Neuro-Oncology Consortium study (PNOC-002) Abstract Background: BRAF V600E mutation is present in a subset of pediatric brain tumors. Vemurafenib is an oral, selective ATP-competitive inhibitor of BR... |
PMC11605291 | core_pubmed_pmc | Mass balance, metabolism, and pharmacokinetics of [ 14 C]amdizalisib, a clinical-stage novel oral selective PI3Kδ inhibitor for the treatment of non-hodgkin’s lymphoma, in healthy Chinese volunteers | Mass balance, metabolism, and pharmacokinetics of [ 14 C]amdizalisib, a clinical-stage novel oral selective PI3Kδ inhibitor for the treatment of non-hodgkin’s lymphoma, in healthy Chinese volunteers Abstract Abstract Introduction Amdizalisib (HMPL-689) is an ATP-competitive PI3Kδ inhibitor currently under investigation... |
PMC11307025 | core_pubmed_pmc | Effectiveness of Continuous Dopaminergic Therapies in Parkinson’s Disease: A Review of L-DOPA Pharmacokinetics/Pharmacodynamics | Effectiveness of Continuous Dopaminergic Therapies in Parkinson’s Disease: A Review of L-DOPA Pharmacokinetics/Pharmacodynamics Abstract Abstract Background: Parkinson’s disease (PD) is characterized by striatal dopamine deficiency. Since dopamine cannot cross the digestive and blood-brain barriers, its precursor, levo... |
PMC10319623 | core_pubmed_pmc | Optimizing the Use of Beta-Lactam Antibiotics in Clinical Practice: A Test of Time | Optimizing the Use of Beta-Lactam Antibiotics in Clinical Practice: A Test of Time Abstract Abstract Despite their limitations, the pharmacokinetics (PK) and pharmacodynamics (PD) indices form the basis for our current understanding regarding antibiotic development, selection, and dose optimization. Application of PK-P... |
PMC7946689 | core_pubmed_pmc | Galactose-Modified PH-Sensitive Niosomes for Controlled Release and Hepatocellular Carcinoma Target Delivery of Tanshinone IIA | Galactose-Modified PH-Sensitive Niosomes for Controlled Release and Hepatocellular Carcinoma Target Delivery of Tanshinone IIA Abstract Increasing the drug tumor-specific accumulation and controlling their release is considered one of the most effective ways to increase the efficacy of drugs. Here, we developed a vesic... |
PMC9693583 | core_pubmed_pmc | Effect of Pd 2 Spermine on Mice Brain-Liver Axis Metabolism Assessed by NMR Metabolomics | Effect of Pd 2 Spermine on Mice Brain-Liver Axis Metabolism Assessed by NMR Metabolomics Abstract Abstract Cisplatin (cDDP)-based chemotherapy is often limited by severe deleterious effects (nephrotoxicity, hepatotoxicity and neurotoxicity). The polynuclear palladium(II) compound Pd 2 Spermine (Pd 2 Spm) has emerged as... |
PMC9423109 | core_pubmed_pmc | Design of Montelukast Nanocrystalline Suspension for Parenteral Prolonged Delivery | Design of Montelukast Nanocrystalline Suspension for Parenteral Prolonged Delivery Abstract Abstract Background Montelukast (MTK), a representative leukotriene receptor antagonist, is currently being investigated as a potential candidate for treating Alzheimer’s disease. For potent and effective dosing in elderly patie... |
PMC10242497 | core_pubmed_pmc | A novel polymer-conjugated human IL-15 improves efficacy of CD19-targeted CAR T-cell immunotherapy | A novel polymer-conjugated human IL-15 improves efficacy of CD19-targeted CAR T-cell immunotherapy Abstract Key Points • Polymer-conjugated IL-15 (NKTR-255) induced CD8 + and CD4 + T-cell and natural killer cell proliferation in nonhuman primates. • NKTR-255 enhanced the efficacy of human CD19 CAR T cells in a xenogene... |
PMC9857301 | core_pubmed_pmc | Immunogenicity With Ranibizumab Biosimilar SB11 (Byooviz) and Reference Product Lucentis and Association With Efficacy, Safety, and Pharmacokinetics | Immunogenicity With Ranibizumab Biosimilar SB11 (Byooviz) and Reference Product Lucentis and Association With Efficacy, Safety, and Pharmacokinetics Abstract Key Points Question How is immunogenicity to ranibizumab products associated with efficacy, safety, and pharmacokinetic (PK) profiles in patients with neovascular... |
PMC6151663 | core_pubmed_pmc | Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years | Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years Abstract Background : Poor pharmacokinetic profiles and resistance are the main two drawbacks from which currently used antiviral agents suffer, thus make them excellent targets for research, especially in t... |
PMC9359405 | core_pubmed_pmc | Investigation of the “Nose-to-Brain” Pathways in Intranasal HupA Nanoemulsions and Evaluation of Their in vivo Pharmacokinetics and Brain-Targeting Ability | Investigation of the “Nose-to-Brain” Pathways in Intranasal HupA Nanoemulsions and Evaluation of Their in vivo Pharmacokinetics and Brain-Targeting Ability Abstract Purpose While developing huperzine A (HupA) to explore new approaches to treating Alzheimer’s disease (AD), intranasal administration was proposed as an al... |
PMC4157019 | core_pubmed_pmc | Liquid Chromatography Tandem Mass/Mass Spectrometry for the Quantification of Fudosteine in Human Serum without Precolumn Derivatization | Liquid Chromatography Tandem Mass/Mass Spectrometry for the Quantification of Fudosteine in Human Serum without Precolumn Derivatization Abstract A quantitative analysis method for fudosteine in human serum by high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI/MS/MS) was e... |
PMC8773721 | core_pubmed_pmc | A Small Molecule–Drug Conjugate (SMDC) Consisting of a Modified Camptothecin Payload Linked to an α V ß 3 Binder for the Treatment of Multiple Cancer Types | A Small Molecule–Drug Conjugate (SMDC) Consisting of a Modified Camptothecin Payload Linked to an α V ß 3 Binder for the Treatment of Multiple Cancer Types Abstract Abstract Simple Summary Many cancer drugs are cytotoxic, which means that they kill cancer cells effectively but are also toxic to normal cells. To overcom... |
PMC11932312 | core_pubmed_pmc | Assessing the Application of Physiologically Based Pharmacokinetic Models in Acute Chemical Incidents | Assessing the Application of Physiologically Based Pharmacokinetic Models in Acute Chemical Incidents Abstract Chemical release incidents in the United States involve hazardous chemicals that can harm nearby communities. A historical tracking of these chemical release incidents from 1991 to 2014 across up to 16 states ... |
PMC6060990 | core_pubmed_pmc | Population Pharmacokinetic Analysis and Model-Based Simulations of Aripiprazole for a 1-Day Initiation Regimen for the Long-Acting Antipsychotic Aripiprazole Lauroxil | Population Pharmacokinetic Analysis and Model-Based Simulations of Aripiprazole for a 1-Day Initiation Regimen for the Long-Acting Antipsychotic Aripiprazole Lauroxil Abstract Background and Objectives Aripiprazole lauroxil (AL), a long-acting injectable antipsychotic for the treatment of schizophrenia, requires 21 day... |
PMC11668332 | core_pubmed_pmc | Chitosan-Based Nanocapsules as a Delivery System of Hydrophobic Carnosic Acid, A Model Neuroprotective Drug | Chitosan-Based Nanocapsules as a Delivery System of Hydrophobic Carnosic Acid, A Model Neuroprotective Drug Abstract Introduction Since the population of Europe is rapidly aging, the number of cases of neurodegenerative diseases sharply increases. One of the most significant limitations of current neurodegenerative dis... |
PMC10956312 | core_pubmed_pmc | Brivaracetam and topiramate serum levels during pregnancy and delivery: a case report and a review of literature | Brivaracetam and topiramate serum levels during pregnancy and delivery: a case report and a review of literature Abstract Background An increasing use of newer antiseizure medication (ASM) such as SV2A ligand brivaracetam is observed. However, data on newer antiseizure medication and therapeutic drug monitoring during ... |
PMC10053003 | core_pubmed_pmc | Study on Pharmacokinetics and Metabolic Profiles of Novel Potential PLK-1 Inhibitors by UHPLC-MS/MS Combined with UHPLC-Q-Orbitrap/HRMS | Study on Pharmacokinetics and Metabolic Profiles of Novel Potential PLK-1 Inhibitors by UHPLC-MS/MS Combined with UHPLC-Q-Orbitrap/HRMS Abstract Abstract PLK-1 (Polo-like kinase-1) plays an essential role in cytokinesis, and its aberrant expression is considered to be keenly associated with a wide range of cancers. It ... |
PMC5641942 | core_pubmed_pmc | Oral and intravenous pharmacokinetics of taurine in sprague‐dawley rats: the influence of dose and the possible involvement of the proton‐coupled amino acid transporter, PAT1, in oral taurine absorption | Oral and intravenous pharmacokinetics of taurine in sprague‐dawley rats: the influence of dose and the possible involvement of the proton‐coupled amino acid transporter, PAT1, in oral taurine absorption Abstract Abstract Taurine is involved in various physiological processes, and one of the most abundant amino acids in... |
PMC7158207 | core_pubmed_pmc | Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling | Evaluating the Role of Solubility in Oral Absorption of Poorly Water‐Soluble Drugs Using Physiologically‐Based Pharmacokinetic Modeling Abstract Abstract Poor aqueous solubility and dissolution of drug candidates drive key decisions on lead series optimization during drug discovery, on formulation optimization, and cli... |
PMC3236496 | core_pubmed_pmc | IT-141, a Polymer Micelle Encapsulating SN-38, Induces Tumor Regression in Multiple Colorectal Cancer Models | IT-141, a Polymer Micelle Encapsulating SN-38, Induces Tumor Regression in Multiple Colorectal Cancer Models Abstract Polymer micelles are promising drug delivery vehicles for the delivery of anticancer agents to tumors. Often, anticancer drugs display potent cytotoxic effects towards cancer cells but are too hydrophob... |
PMC5663900 | core_pubmed_pmc | Shengjiang Xiexin Decoction Alters Pharmacokinetics of Irinotecan by Regulating Metabolic Enzymes and Transporters: A Multi-Target Therapy for Alleviating the Gastrointestinal Toxicity | Shengjiang Xiexin Decoction Alters Pharmacokinetics of Irinotecan by Regulating Metabolic Enzymes and Transporters: A Multi-Target Therapy for Alleviating the Gastrointestinal Toxicity Abstract Shengjiang Xiexin decoction (SXD), a classic traditional Chinese medical formula chronicled in Shang Han Lun , is used in mode... |
PMC8950239 | core_pubmed_pmc | Magnetic Solid Nanoparticles and Their Counterparts: Recent Advances towards Cancer Theranostics | Magnetic Solid Nanoparticles and Their Counterparts: Recent Advances towards Cancer Theranostics Abstract Abstract Cancer is currently a leading cause of death worldwide. The World Health Organization estimates an increase of 60% in the global cancer incidence in the next two decades. The inefficiency of the currently ... |
PMC10005590 | core_pubmed_pmc | Characterization, Antioxidant Potential, and Pharmacokinetics Properties of Phenolic Compounds from Native Australian Herbs and Fruits | Characterization, Antioxidant Potential, and Pharmacokinetics Properties of Phenolic Compounds from Native Australian Herbs and Fruits Abstract In recent decades, plant bioactive phenolic compounds gained much attention due to their various health benefits. Therefore, this study aimed to analyze native Australian river... |
PMC9797307 | core_pubmed_pmc | Measurement of Pharmacokinetics and Tissue Distribution of Four Compounds from Nauclea officinalis in Rat Plasma and Tissues through HPLC-MS/MS | Measurement of Pharmacokinetics and Tissue Distribution of Four Compounds from Nauclea officinalis in Rat Plasma and Tissues through HPLC-MS/MS Abstract A rapid, sensitive, selective, and accurate HPLC–MS/MS method was developed and validated for the simultaneous determination of chlorogenic acid, naucleactonin C, khae... |
PMC4622559 | core_pubmed_pmc | Dose dependent pharmacokinetics, tissue distribution, and anti-tumor efficacy of a humanized monoclonal antibody against DLL4 in mice | Dose dependent pharmacokinetics, tissue distribution, and anti-tumor efficacy of a humanized monoclonal antibody against DLL4 in mice Abstract Abstract Delta-like-4 ligand (DLL4) plays an important role in vascular development and is widely expressed on the vasculature of normal and tumor tissues. Anti-DLL4 is a humani... |
PMC9143054 | core_pubmed_pmc | Common UGT1A6 Variant Alleles Determine Acetaminophen Pharmacokinetics in Man | Common UGT1A6 Variant Alleles Determine Acetaminophen Pharmacokinetics in Man Abstract Acetaminophen (paracetamol) is a widely used drug that causes adverse drug events that are often dose-dependent and related to plasma drug concentrations. Acetaminophen metabolism strongly depends on UGT1A enzymes. We aimed to invest... |
PMC7598194 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic (PBPK) Modeling Providing Insights into Fentanyl Pharmacokinetics in Adults and Pediatric Patients | Physiologically-Based Pharmacokinetic (PBPK) Modeling Providing Insights into Fentanyl Pharmacokinetics in Adults and Pediatric Patients Abstract Abstract Fentanyl is widely used for analgesia, sedation, and anesthesia both in adult and pediatric populations. Yet, only few pharmacokinetic studies of fentanyl in pediatr... |
PMC10222203 | core_pubmed_pmc | Differential Blood–Brain Barrier Transport and Cell Uptake of Cyclic Peptides In Vivo and In Vitro | Differential Blood–Brain Barrier Transport and Cell Uptake of Cyclic Peptides In Vivo and In Vitro Abstract Abstract The blood–brain barrier (BBB) poses major challenges to drug delivery to the CNS. SFTI-1 and kalata B1 are cyclic cell-penetrating peptides (cCPPs) with high potential to be used as scaffolds for drug de... |
PMC11106201 | core_pubmed_pmc | Population Pharmacokinetics of Sacituzumab Govitecan in Patients with Metastatic Triple-Negative Breast Cancer and Other Solid Tumors | Population Pharmacokinetics of Sacituzumab Govitecan in Patients with Metastatic Triple-Negative Breast Cancer and Other Solid Tumors Abstract Background and Objective Sacituzumab govitecan (SG) is an antibody–drug conjugate composed of an antibody with affinity for Trop-2 coupled to SN-38 via hydrolyzable linker. SG i... |
PMC8980857 | core_pubmed_pmc | Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors Using Dried Blood Microsamples | Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors Using Dried Blood Microsamples Abstract Abstract Therapeutic drug monitoring (TDM) of tyrosine kinase inhibitors (TKIs) is not yet performed routinely in the standard care of oncology patients, although it offers a high potential to improve treatment outcome and... |
PMC11812941 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic analysis of geographic atrophy lesion area in patients receiving pegcetacoplan treatment or sham | Pharmacokinetic/pharmacodynamic analysis of geographic atrophy lesion area in patients receiving pegcetacoplan treatment or sham Abstract Abstract Pegcetacoplan is a complement C3/C3b inhibitor indicated for the treatment of geographic atrophy (GA). A population pharmacokinetic (PK)/pharmacodynamic (PD) analysis of peg... |
PMC10256675 | core_pubmed_pmc | Comparison of Three Renal Function Formulas for Ganciclovir/Valganciclovir Dose Individualization in CMV-Infected Solid Organ Transplantation Patients Using a Population Approach | Comparison of Three Renal Function Formulas for Ganciclovir/Valganciclovir Dose Individualization in CMV-Infected Solid Organ Transplantation Patients Using a Population Approach Abstract Abstract Background and Objective The gold standard treatment of established cytomegalovirus infection or prevention in solid organ ... |
PMC12309868 | core_pubmed_pmc | In Vitro and Clinical Evaluations of UGT1A1‐, P‐gp‐, OATP1B1‐, and BCRP‐Mediated Drug–Drug Interactions of Belumosudil, a Potent ROCK2 Inhibitor | In Vitro and Clinical Evaluations of UGT1A1‐, P‐gp‐, OATP1B1‐, and BCRP‐Mediated Drug–Drug Interactions of Belumosudil, a Potent ROCK2 Inhibitor Abstract Abstract Belumosudil is an oral selective rho‐associated coiled‐coil containing protein kinase 2 inhibitor, approved as a treatment for chronic graft‐versus‐host dise... |
PMC10499419 | core_pubmed_pmc | A phase I randomized, double‐blinded , placebo‐controlled study assessing the safety and pharmacokinetics of RIPK1 inhibitor GFH312 in healthy subjects | A phase I randomized, double‐blinded , placebo‐controlled study assessing the safety and pharmacokinetics of RIPK1 inhibitor GFH312 in healthy subjects Abstract Abstract Receptor‐interacting protein kinase 1 (RIPK1) mediates necroptosis and inflammation in various pathophysiologies, emerging as a pharmacological target... |
PMC9678504 | core_pubmed_pmc | The status of TKI/acid-suppressant concomitant use in 44 hospitals in China: A cross-sectional descriptive study | The status of TKI/acid-suppressant concomitant use in 44 hospitals in China: A cross-sectional descriptive study Abstract Abstract The irrational use of tyrosine kinase inhibitors (TKIs) has attracted increasing attention, especially because of drug–drug interactions. The objective of this study was to analyze TKI pres... |
PMC3255418 | core_pubmed_pmc | Determination of pregabalin in human plasma by electrospray ionisation tandem mass spectroscopy | Determination of pregabalin in human plasma by electrospray ionisation tandem mass spectroscopy Abstract Abstract A rapid, precise, specific, and accurate Electrospray Ionisation Tandem Mass Spectrometry (ESI-MS / MS) method has been developed and subsequently validated, for the determination of pregabalin (PB) in huma... |
PMC11319150 | core_pubmed_pmc | In silico studies on leishmanicide activity of limonoids and fatty acids from Carapa guianensis Aubl | In silico studies on leishmanicide activity of limonoids and fatty acids from Carapa guianensis Aubl Abstract The oil of Carapa guianensis showed leishmanicidal activity, with its activity being related to limonoids, but fatty acids are the major constituents of this oil. The present study evaluated the physicochemical... |
PMC9313867 | core_pubmed_pmc | Disease Modeling and Model‐Based Meta‐Analyses to Define a New Direction for a Phase III Program of Gantenerumab in Alzheimer’s Disease | Disease Modeling and Model‐Based Meta‐Analyses to Define a New Direction for a Phase III Program of Gantenerumab in Alzheimer’s Disease Abstract Selecting the right dose is a significant challenge in designing clinical development programs, especially for slowly progressing diseases lacking predictive biomarkers of eff... |
PMC5117585 | core_pubmed_pmc | A phase I dose-escalation study of PEP02 (irinotecan liposome injection) in combination with 5-fluorouracil and leucovorin in advanced solid tumors | A phase I dose-escalation study of PEP02 (irinotecan liposome injection) in combination with 5-fluorouracil and leucovorin in advanced solid tumors Abstract Abstract Background PEP02 (also known as MM-398, nal-IRI) is a novel nanoparticle formulation of irinotecan encapsulated in liposomes. The aims of this study were ... |
PMC12121518 | core_pubmed_pmc | Regulatory Effects of Betonica macrantha Extract, Known as Mountain Tea, on miRNA Expression and Its Pharmacokinetic Properties | Regulatory Effects of Betonica macrantha Extract, Known as Mountain Tea, on miRNA Expression and Its Pharmacokinetic Properties Abstract ABSTRACT The aim of this study is to investigate the anticancer potential of Betonica macrantha extract on MDA‐MB‐231 breast cancer cells, its regulatory effects on miRNA expression, ... |
PMC4567061 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of orally administered acetylenic tricyclic bis (cyanoenone), a highly potent Nrf2 activator with a reversible covalent mode of action | Pharmacokinetics and pharmacodynamics of orally administered acetylenic tricyclic bis (cyanoenone), a highly potent Nrf2 activator with a reversible covalent mode of action Abstract Abstract The acetylenic tricyclic bis (cyanoenone) TBE-31 is a highly potent cysteine targeting compound with a reversible covalent mode o... |
PMC12883143 | core_pubmed_pmc | Quantitative Evaluation of Model‐Informed Drug Development Implementation in China's Approved Innovative Drugs: From Policy to Practice (2018–2024) | Quantitative Evaluation of Model‐Informed Drug Development Implementation in China's Approved Innovative Drugs: From Policy to Practice (2018–2024) Abstract ABSTRACT Model‐informed drug development (MIDD) has emerged as a cornerstone paradigm in global pharmaceutical innovation. Historically underutilized in China, MID... |
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