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PMC12419557 | core_pubmed_pmc | Pharmacokinetic study of the synthetic cannabinoid, 5F-MDMB-PICA, in male Wistar rats | Pharmacokinetic study of the synthetic cannabinoid, 5F-MDMB-PICA, in male Wistar rats Abstract BACKGROUND: This research focused on establishing a highly sensitive and reliable gas chromatography–mass spectrometry (GC-MS) method for detecting and quantifying 5F-MDMB-PICA in rat plasma, as well as thoroughly assessing i... |
PMC8832728 | core_pubmed_pmc | Clinical pharmacokinetics of quinine and its relationship with treatment outcomes in children, pregnant women, and elderly patients, with uncomplicated and complicated malaria: a systematic review | Clinical pharmacokinetics of quinine and its relationship with treatment outcomes in children, pregnant women, and elderly patients, with uncomplicated and complicated malaria: a systematic review Abstract Background Standard dosage regimens of quinine formulated for adult patients with uncomplicated and complicated ma... |
PMC3221672 | core_pubmed_pmc | Evaluation of an AAV2-Based Rapamycin-Regulated Glial Cell Line-Derived Neurotrophic Factor (GDNF) Expression Vector System | Evaluation of an AAV2-Based Rapamycin-Regulated Glial Cell Line-Derived Neurotrophic Factor (GDNF) Expression Vector System Abstract Effective regulation of transgene product in anatomically circumscribed brain tissue is dependent on the pharmacokinetics of the regulating agent, the kinetics of transcriptional activati... |
PMC6306054 | core_pubmed_pmc | Preparation and characterization of nimodipine-loaded nanostructured lipid systems for enhanced solubility and bioavailability | Preparation and characterization of nimodipine-loaded nanostructured lipid systems for enhanced solubility and bioavailability Abstract Abstract Purpose Nimodipine (NMP) is a clinical dihydropyridine calcium antagonist. However, the clinical application of NMP is limited by poor water solubility and low oral bioavailab... |
PMC8949582 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling and Simulation to Predict the Plasma Concentration Profile of Doxorubicin | Physiologically Based Pharmacokinetic Modelling and Simulation to Predict the Plasma Concentration Profile of Doxorubicin Abstract Doxorubicin (DOX) is still an important anticancer agent despite its tricky pharmacokinetics (PK) and toxicity potential. The advent of systems pharmacology enables the construction of PK m... |
PMC8979756 | core_pubmed_pmc | Evaluation of food effects on the pharmacokinetics of Pelargonium sidoides and Coptis with each bioactive compound berberine and epicatechin after a single oral dose of an expectorant and antitussive agent UI026 in healthy subjects | Evaluation of food effects on the pharmacokinetics of Pelargonium sidoides and Coptis with each bioactive compound berberine and epicatechin after a single oral dose of an expectorant and antitussive agent UI026 in healthy subjects Abstract UI026 is an expectorant and antitussive agent which is a new combination of Pel... |
PMC3792958 | core_pubmed_pmc | Olomoucine II, but Not Purvalanol A, Is Transported by Breast Cancer Resistance Protein (ABCG2) and P-Glycoprotein (ABCB1) | Olomoucine II, but Not Purvalanol A, Is Transported by Breast Cancer Resistance Protein (ABCG2) and P-Glycoprotein (ABCB1) Abstract Purine cyclin-dependent kinase inhibitors have been recognized as promising candidates for the treatment of various cancers; nevertheless, data regarding interaction of these substances wi... |
PMC8069016 | core_pubmed_pmc | Matrix Effects of the Hydroethanolic Extract of Calyces of Physalis peruviana L. on Rutin Pharmacokinetics in Wistar Rats Using Population Modeling | Matrix Effects of the Hydroethanolic Extract of Calyces of Physalis peruviana L. on Rutin Pharmacokinetics in Wistar Rats Using Population Modeling Abstract Abstract Rutin is the rutinose conjugate of quercetin. It presents several biological activities and is the major flavonoid in the hydroalcoholic extract of the ca... |
PMC11372519 | core_pubmed_pmc | Remimazolam in intensive care unit: Potential applications and considerations | Remimazolam in intensive care unit: Potential applications and considerations Abstract Abstract This manuscript explores the potential use of Remimazolam in the intensive care unit (ICU) and critical care units, considering its pharmacological characteristics, clinical applications, advantages, and comparative effectiv... |
PMC7913794 | core_pubmed_pmc | Design, Synthesis, and In Silico Multitarget Pharmacological Simulations of Acid Bioisosteres with a Validated In Vivo Antihyperglycemic Effect | Design, Synthesis, and In Silico Multitarget Pharmacological Simulations of Acid Bioisosteres with a Validated In Vivo Antihyperglycemic Effect Abstract Substituted phenylacetic ( 1–3 ), phenylpropanoic ( 4–6 ), and benzylidenethiazolidine-2,4-dione ( 7–9 ) derivatives were designed according to a multitarget unified p... |
PMC12693367 | core_pubmed_pmc | Methylphenidate, Sleep, and the “Stimulant Paradox” in Adult ADHD: A Conceptual Framework for Integrating Chronopharmacotherapy and Coaching | Methylphenidate, Sleep, and the “Stimulant Paradox” in Adult ADHD: A Conceptual Framework for Integrating Chronopharmacotherapy and Coaching Abstract This conceptual narrative review explores the intricate dynamics of the ‘stimulant paradox’ in adult ADHD, highlighting the timing-dependent trade-offs associated with st... |
PMC3834939 | core_pubmed_pmc | Protein Adsorption Patterns and Analysis on IV Nanoemulsions—The Key Factor Determining the Organ Distribution | Protein Adsorption Patterns and Analysis on IV Nanoemulsions—The Key Factor Determining the Organ Distribution Abstract Intravenous nanoemulsions have been on the market for parenteral nutrition since the 1950s; meanwhile, they have also been used successfully for IV drug delivery. To be well tolerable, the emulsions s... |
PMC6954127 | core_pubmed_pmc | A phase 3, open-label, multicenter study of a 6-month pre-mixed depot formulation of leuprolide mesylate in advanced prostate cancer patients | A phase 3, open-label, multicenter study of a 6-month pre-mixed depot formulation of leuprolide mesylate in advanced prostate cancer patients Abstract Objectives To determine the safety, efficacy and pharmacokinetic (PK) profile of a pre-mixed depot formulation of leuprolide mesylate subcutaneous injectable suspension ... |
PMC4712254 | core_pubmed_pmc | Effects of Cytochrome P450 Inhibition and Induction on the Phenotyping Metrics of the Basel Cocktail: A Randomized Crossover Study | Effects of Cytochrome P450 Inhibition and Induction on the Phenotyping Metrics of the Basel Cocktail: A Randomized Crossover Study Abstract Abstract Background and Objective Activity of human cytochrome P450 enzymes (CYPs) shows high inter-and intra-individual variability, which is determined by genetic and non-genetic... |
PMC12615164 | core_pubmed_pmc | Gliadel use in a pregnant patient with malignant glioma: a case report | Gliadel use in a pregnant patient with malignant glioma: a case report Abstract Malignant gliomas during pregnancy represent a rare and complex clinical challenge, with limited data to guide management. We report a case of a 35-year-old woman with World Health Organization (WHO) grade III anaplastic astrocytoma who pre... |
PMC5595942 | core_pubmed_pmc | Food intake and darunavir plasma concentrations in people living with HIV in an outpatient setting | Food intake and darunavir plasma concentrations in people living with HIV in an outpatient setting Abstract Aims Patients receiving darunavir are advised to take it concomitantly with food. The objectives of the present cross‐sectional study were to evaluate the actual concomitant food intake of patients visiting an HI... |
PMC7890197 | core_pubmed_pmc | Clinical Pharmacology of Clazosentan, a Selective Endothelin A Receptor Antagonist for the Prevention and Treatment of aSAH-Related Cerebral Vasospasm | Clinical Pharmacology of Clazosentan, a Selective Endothelin A Receptor Antagonist for the Prevention and Treatment of aSAH-Related Cerebral Vasospasm Abstract Abstract Aneurysmal subarachnoid hemorrhage (aSAH) may lead to cerebral vasospasm and is associated with significant morbidity and mortality. It represents a ma... |
PMC8026785 | core_pubmed_pmc | The pharmacokinetics of [ 18 F]UCB-H revisited in the healthy non-human primate brain | The pharmacokinetics of [ 18 F]UCB-H revisited in the healthy non-human primate brain Abstract Background Positron Emission Tomography (PET) imaging of the Synaptic Vesicle glycoprotein (SV) 2A is a new tool to quantify synaptic density. [ 18 F]UCB-H was one of the first promising SV2A-ligands to be labelled and used i... |
PMC12473654 | core_pubmed_pmc | Strategic Objectives of Nanotechnology-Driven Repurposing in Radiopharmacy—Implications for Radiopharmaceutical Repurposing (Beyond Oncology) | Strategic Objectives of Nanotechnology-Driven Repurposing in Radiopharmacy—Implications for Radiopharmaceutical Repurposing (Beyond Oncology) Abstract Abstract The integration of nanotechnology into drug repurposing strategies is redefining the development landscape for diagnostic, therapeutic, and theranostic agents. ... |
PMC4488346 | core_pubmed_pmc | Rational Design and Adaptive Management of Combination Therapies for Hepatitis C Virus Infection | Rational Design and Adaptive Management of Combination Therapies for Hepatitis C Virus Infection Abstract Abstract Recent discoveries of direct acting antivirals against Hepatitis C virus (HCV) have raised hopes of effective treatment via combination therapies. Yet rapid evolution and high diversity of HCV populations,... |
PMC5955381 | core_pubmed_pmc | SN38-loaded <100 nm targeted liposomes for improving poor solubility and minimizing burst release and toxicity: in vitro and in vivo study | SN38-loaded <100 nm targeted liposomes for improving poor solubility and minimizing burst release and toxicity: in vitro and in vivo study Abstract Abstract Background SN38 (7-ethyl-10-hydroxycamptothecin) is a camptothecin derivative acts against various tumors. However, SN38 is hydrolyzed in the physiological environ... |
PMC5573988 | core_pubmed_pmc | Dose‐finding methods for Phase I clinical trials using pharmacokinetics in small populations | Dose‐finding methods for Phase I clinical trials using pharmacokinetics in small populations Abstract Abstract The aim of phase I clinical trials is to obtain reliable information on safety, tolerability, pharmacokinetics (PK), and mechanism of action of drugs with the objective of determining the maximum tolerated dos... |
PMC12162334 | core_pubmed_pmc | Congrong Shujing Granules ameliorates mitochondrial associated membranes to against MPP + -induced neurological damage in the cellular model of Parkinson’s disease | Congrong Shujing Granules ameliorates mitochondrial associated membranes to against MPP + -induced neurological damage in the cellular model of Parkinson’s disease Abstract Abstract Context Congrong-Shujing Granules (CRSJG) are known to protect dopaminergic neurons in Parkinson’s disease (PD), and the mechanism may be ... |
PMC10830452 | core_pubmed_pmc | Aerosolized delivery of ESKAPE pathogens for murine pneumonia models | Aerosolized delivery of ESKAPE pathogens for murine pneumonia models Abstract Murine pneumonia models for ESKAPE pathogens serve to evaluate novel antibacterials or to investigate immunological responses. The majority of published models uses intranasal or to a limited extent the intratracheal instillation to challenge... |
PMC3239365 | core_pubmed_pmc | A randomized, double-blind study of AMG 108 (a fully human monoclonal antibody to IL-1R1) in patients with osteoarthritis of the knee | A randomized, double-blind study of AMG 108 (a fully human monoclonal antibody to IL-1R1) in patients with osteoarthritis of the knee Abstract Abstract Introduction AMG 108 is a fully human, immunoglobulin subclass G2 (IgG2) monoclonal antibody that binds the human interleukin-1 (IL-1) receptor type 1, inhibiting the a... |
PMC8635734 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate | Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate Abstract Abstract Delicaflavone (DF), a natural active ingredient from Selaginella doederleinii Hieron, has been reported to have favorable anticancer effects and is thus considered a potenti... |
PMC8056730 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of BI 655064 in phase 1 clinical trials in healthy Chinese and Japanese subjects | Safety, pharmacokinetics and pharmacodynamics of BI 655064 in phase 1 clinical trials in healthy Chinese and Japanese subjects Abstract Abstract Aims To evaluate the safety, pharmacokinetics and pharmacodynamics of BI 655064 in healthy Chinese and Japanese subjects after administration of single doses of 80‐240 mg and ... |
PMC12813654 | core_pubmed_pmc | A Thorough QT Study to Assess the Effects of Milvexian on Cardiac Repolarization in Healthy Participants | A Thorough QT Study to Assess the Effects of Milvexian on Cardiac Repolarization in Healthy Participants Abstract Abstract Milvexian is an oral factor XIa inhibitor in development for prevention of major thromboembolic conditions. This randomized, double‐blind, placebo‐ and positive‐controlled, multiple‐dose, four‐peri... |
PMC10391552 | core_pubmed_pmc | Immunomodulatory effects and mechanisms of the extracts and secondary compounds of Zingiber and Alpinia species: a review | Immunomodulatory effects and mechanisms of the extracts and secondary compounds of Zingiber and Alpinia species: a review Abstract Abstract Zingiber and Alpinia species (family: Zingiberaceae) are popularly used in food as spices and flavoring agents and in ethnomedicine to heal numerous diseases, including immune-rela... |
PMC4969531 | core_pubmed_pmc | Enhanced Absorption Study of Ginsenoside Compound K (20- O - β -(D-Glucopyranosyl)-20(S)-protopanaxadiol) after Oral Administration of Fermented Red Ginseng Extract (HYFRG ™ ) in Healthy Korean Volunteers and Rats | Enhanced Absorption Study of Ginsenoside Compound K (20- O - β -(D-Glucopyranosyl)-20(S)-protopanaxadiol) after Oral Administration of Fermented Red Ginseng Extract (HYFRG ™ ) in Healthy Korean Volunteers and Rats Abstract To evaluate the pharmacokinetics of compound K after oral administration of HYFRG and RG in human... |
PMC11078975 | core_pubmed_pmc | Population pharmacokinetic modelling of primaquine exposures in lactating women and breastfed infants | Population pharmacokinetic modelling of primaquine exposures in lactating women and breastfed infants Abstract Current guidelines advise against primaquine treatment for breastfeeding mothers to avoid the potential for haemolysis in infants with G6PD deficiency. To predict the haemolytic risk, the amount of drug receiv... |
PMC5869873 | core_pubmed_pmc | Effect of alisertib, an investigational aurora a kinase inhibitor on the QTc interval in patients with advanced malignancies | Effect of alisertib, an investigational aurora a kinase inhibitor on the QTc interval in patients with advanced malignancies Abstract Summary Aims A primary objective of this study was to investigate the effect of single and multiple doses of alisertib, an investigational Aurora A kinase inhibitor, on the QTc interval ... |
PMC12821350 | core_pubmed_pmc | The colloidal stability of albumin-based drug delivery systems has a profound effect on tumoricidal activity | The colloidal stability of albumin-based drug delivery systems has a profound effect on tumoricidal activity Abstract ABSTRACT Human serum albumin (HSA) has attracted significant attention in drug delivery since the approval of Abraxane in 2005. Abraxane is a nanoparticle albumin-bound paclitaxel (nab-PTX) formulation.... |
PMC8847640 | core_pubmed_pmc | Study on Pharmacokinetic Interactions Between HS-10234 and Emtricitabine in Healthy Subjects: An Open-Label, Two-Sequence, Self-Controlled Phase I Trial | Study on Pharmacokinetic Interactions Between HS-10234 and Emtricitabine in Healthy Subjects: An Open-Label, Two-Sequence, Self-Controlled Phase I Trial Abstract Introduction HS-10234, a novel prodrug of tenofovir (TFV), functions by inhibiting nucleotide reverse transcriptase against retroviral infections including he... |
PMC3405875 | core_pubmed_pmc | Intracellular delivery mechanism and brain delivery kinetics of biodegradable cationic bovine serum albumin-conjugated polymersomes | Intracellular delivery mechanism and brain delivery kinetics of biodegradable cationic bovine serum albumin-conjugated polymersomes Abstract Background A novel brain drug delivery system using cationic bovine serum albumin (CBSA)-conjugated biodegradable polymersomes (CBSA-PO) was prepared, and its intracellular delive... |
PMC7182240 | core_pubmed_pmc | Safety, Efficacy and Pharmacokinetics of Anidulafungin in Patients 1 Month to <2 Years of Age With Invasive Candidiasis, Including Candidemia | Safety, Efficacy and Pharmacokinetics of Anidulafungin in Patients 1 Month to <2 Years of Age With Invasive Candidiasis, Including Candidemia Abstract Abstract Nineteen patients 1 month to <2 years of age with (n = 16) or at high risk of (n = 3) invasive candidiasis received anidulafungin for 5–35 days (3 mg/kg day 1, ... |
PMC10313034 | core_pubmed_pmc | Poria cocos compounds targeting neuropeptide Y1 receptor (Y 1 R) for weight management: A computational ligand- and structure-based study with molecular dynamics simulations identified beta-amyrin acetate as a putative Y 1 R inhibitor | Poria cocos compounds targeting neuropeptide Y1 receptor (Y 1 R) for weight management: A computational ligand- and structure-based study with molecular dynamics simulations identified beta-amyrin acetate as a putative Y 1 R inhibitor Abstract Abstract Poria cocos (PC) is a medicinal herb frequently used in weight-loss... |
PMC11947739 | core_pubmed_pmc | Optimized 5‐HT 2b inhibitors for neuropsychiatric syndromes with cognitive dysfunction | Optimized 5‐HT 2b inhibitors for neuropsychiatric syndromes with cognitive dysfunction Abstract Abstract INTRODUCTION Neuropsychiatric syndromes such as anxiety and agitation are clinical presentations common to diverse neurodegenerative diseases and brain injury sequelae. They are a concern due to the impact on cognit... |
PMC7941787 | core_pubmed_pmc | A hierarchical model for estimating the exposure-response curve by combining multiple studies of acute lower respiratory infections in children and household fine particulate matter air pollution | A hierarchical model for estimating the exposure-response curve by combining multiple studies of acute lower respiratory infections in children and household fine particulate matter air pollution Abstract Supplemental Digital Content is available in the text. Background: Adverse health effects of household air pollutio... |
PMC9575570 | core_pubmed_pmc | Precise quantitative evaluation of pharmacokinetics of cisplatin using a radio-platinum tracer in tumor-bearing mice | Precise quantitative evaluation of pharmacokinetics of cisplatin using a radio-platinum tracer in tumor-bearing mice Abstract Objective The platinum-based antineoplastic drug cisplatin is commonly used for chemotherapy in clinics. This work aims to demonstrate a radio-platinum tracer is useful for precisely quantifying... |
PMC8301546 | core_pubmed_pmc | Model‐based approach to sampling optimization in studies of antibacterial drugs for infants and young children | Model‐based approach to sampling optimization in studies of antibacterial drugs for infants and young children Abstract Abstract Clinical trials for pediatric indications and new pediatric drugs face challenges, including the limited blood volume due to the patients’ small bodies. In Japan, the Evaluation Committee on ... |
PMC4539082 | core_pubmed_pmc | Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway | Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway Abstract Abstract Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological processes. TGF-β plays an important role in tumorigenesis and contributes... |
PMC12070635 | core_pubmed_pmc | The safety, tolerability, pharmacokinetics, and pharmacodynamics of nebulized pegylated interferon α-2b in healthy adults: a randomized phase 1 trial | The safety, tolerability, pharmacokinetics, and pharmacodynamics of nebulized pegylated interferon α-2b in healthy adults: a randomized phase 1 trial Abstract Background Interferons (IFNs) are proteins that combat viruses and regulate the immune system. Studies have demonstrated that aerosol inhalation of IFNα is both ... |
PMC9322451 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults | Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults Abstract Abstract Brensocatib, an investigational first‐in‐class, small‐molecule, orally bioavailable, selective, and reversible dipeptidyl peptidase... |
PMC3265736 | core_pubmed_pmc | Effect of trabectedin on the QT interval in patients with advanced solid tumor malignancies | Effect of trabectedin on the QT interval in patients with advanced solid tumor malignancies Abstract Abstract Purpose The primary objective of this study was to access the potential effects of trabectedin on the QT/QTc interval in patients with locally advanced or metastatic solid tumors. Methods Patients ( n = 75) who... |
PMC10385742 | core_pubmed_pmc | Quetiapine Albumin Nanoparticles as an Efficacious Platform for Brain Deposition and Potentially Improved Antipsychotic Activity | Quetiapine Albumin Nanoparticles as an Efficacious Platform for Brain Deposition and Potentially Improved Antipsychotic Activity Abstract Abstract Quetiapine (QP) is a second-generation short-acting antipsychotic drug extensively metabolized in the liver, producing pharmacologically inactive metabolites and leading to ... |
PMC6413363 | core_pubmed_pmc | Simultaneous Determination of Five Chromones of Radix Saposhnikoviae Extract in Rat Plasma by UPLC-MS/MS: Application to a Comparative Pharmacokinetic Study in Normal and Febrile Rats | Simultaneous Determination of Five Chromones of Radix Saposhnikoviae Extract in Rat Plasma by UPLC-MS/MS: Application to a Comparative Pharmacokinetic Study in Normal and Febrile Rats Abstract Abstract A rapid and sensitive quantitative analytical method was established for the simultaneous determination of five chromo... |
PMC5987854 | core_pubmed_pmc | Evaluation of the Pharmacodynamic Effects of the Potassium Binder RDX7675 in Mice | Evaluation of the Pharmacodynamic Effects of the Potassium Binder RDX7675 in Mice Abstract Abstract Introduction: Hyperkalemia is a common complication in patients with heart failure or chronic kidney disease, particularly those who are taking inhibitors of the renin–angiotensin–aldosterone system. RDX7675, the calcium... |
PMC11762434 | core_pubmed_pmc | Evaluation of the Effect of Risankizumab on the Pharmacokinetics of Cytochrome P450 Substrates in Patients with Moderately to Severely Active Ulcerative Colitis or Crohn’s Disease | Evaluation of the Effect of Risankizumab on the Pharmacokinetics of Cytochrome P450 Substrates in Patients with Moderately to Severely Active Ulcerative Colitis or Crohn’s Disease Abstract Background and Objective The objective of this study was to characterize the effects of risankizumab on the pharmacokinetics of cyt... |
PMC9468555 | core_pubmed_pmc | Investigation of CYP3A induction by PF ‐05251749 in early clinical development: comparison of linear slope physiologically based pharmacokinetic prediction and biomarker response | Investigation of CYP3A induction by PF ‐05251749 in early clinical development: comparison of linear slope physiologically based pharmacokinetic prediction and biomarker response Abstract Abstract PF‐05251749 is a dual inhibitor of casein kinase 1 δ/ε under clinical development to treat disruption of circadian rhythm i... |
PMC6540003 | core_pubmed_pmc | Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats | Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats Abstract Herein, the effect of silymarin pretreatment on the pharmacokinetics of simvastatin in rats was evaluated. To ensure the accuracy of the results, a rapid and sensitive UPLC–MS/MS method was established for sim... |
PMC12072225 | core_pubmed_pmc | Using Pharmacokinetic and Pharmacodynamic Analysis to Optimize the Dosing Regimens of Fanastomig (EMB‐02) in Patients With Advanced Solid Tumors | Using Pharmacokinetic and Pharmacodynamic Analysis to Optimize the Dosing Regimens of Fanastomig (EMB‐02) in Patients With Advanced Solid Tumors Abstract ABSTRACT Fanastomig (also known as EMB‐02) is a bispecific antibody targeting programmed cell death protein‐1(PD‐1) and lymphocyte activation gene‐3 (LAG‐3), develope... |
PMC6080103 | core_pubmed_pmc | QSAR Modeling of Histamine H 3 R Antagonists/inverse Agonists as Future Drugs for Neurodegenerative Diseases | QSAR Modeling of Histamine H 3 R Antagonists/inverse Agonists as Future Drugs for Neurodegenerative Diseases Abstract Abstract Background Histamine H 3 receptor (H 3 R) is associated with several neuropsychological diseases, and thus it is an important target involved in several CNS disorders, such as narcolepsy, atten... |
PMC9637468 | core_pubmed_pmc | GRWR Correlates with the Metabolism of Tacrolimus after Pediatric Living Donor Liver Transplantation According to Donor CYP3A5 Polymorphism | GRWR Correlates with the Metabolism of Tacrolimus after Pediatric Living Donor Liver Transplantation According to Donor CYP3A5 Polymorphism Abstract Abstract Objectives Tacrolimus is characterized by high pharmacokinetic variability in combination with a narrow therapeutic range. However, influence of donor CYP3A5 geno... |
PMC10040605 | core_pubmed_pmc | Population pharmacokinetics of tigecycline in critically ill patients | Population pharmacokinetics of tigecycline in critically ill patients Abstract Abstract Objective: In critically ill patients, the change of pathophysiological status may affect the pharmacokinetic (PK) process of drugs. The purpose of this study was to develop a PK model for tigecycline in critically ill patients, ide... |
PMC9920178 | core_pubmed_pmc | Mesoporous Silica Nanoparticles Coated with Carboxymethyl Chitosan for 5-Fluorouracil Ocular Delivery: Characterization, In Vitro and In Vivo Studies | Mesoporous Silica Nanoparticles Coated with Carboxymethyl Chitosan for 5-Fluorouracil Ocular Delivery: Characterization, In Vitro and In Vivo Studies Abstract This study investigates the development of topically applied non-invasive amino-functionalized silica nanoparticles (AMSN) and O-Carboxymethyl chitosan-coated AM... |
PMC5651313 | core_pubmed_pmc | Quantitative disease progression model of α‐1 proteinase inhibitor therapy on computed tomography lung density in patients with α‐1 antitrypsin deficiency | Quantitative disease progression model of α‐1 proteinase inhibitor therapy on computed tomography lung density in patients with α‐1 antitrypsin deficiency Abstract Aims Early‐onset emphysema attributed to α‐1 antitrypsin deficiency (AATD) is frequently overlooked and undertreated. RAPID‐RCT/RAPID‐OLE, the largest clini... |
PMC12521396 | core_pubmed_pmc | Adverse drug reaction profiles of histone deacetylase inhibitors | Adverse drug reaction profiles of histone deacetylase inhibitors Abstract The safety and tolerability of histone deacetylase inhibitors (HDACIs) were always a matter of concern. This study aimed to explore the global observational adverse drug reaction (ADR) profiles of the HDACIs: vorinostat, belinostat, panobinostat,... |
PMC3829787 | core_pubmed_pmc | Pharmacokinetics of Remifentanil: a three-compartmental modeling approach | Pharmacokinetics of Remifentanil: a three-compartmental modeling approach Abstract Abstract Remifentanil is a new opioid derivative drug characterized by a fast onset and by a short time of action, since it is rapidly degraded by esterases in blood and other tissues. Its pharmacokinetic and pharmacodynamics properties ... |
PMC9714380 | core_pubmed_pmc | Development and characterization of a novel human CD137 agonistic antibody with anti‐tumor activity and a good safety profile in non‐human primates | Development and characterization of a novel human CD137 agonistic antibody with anti‐tumor activity and a good safety profile in non‐human primates Abstract CD137 (4‐1BB, TNFRSF9), an inducible T‐cell costimulatory receptor, is expressed on activated T cells, activated NK cells, Treg cells, and several innate immune ce... |
PMC3170473 | core_pubmed_pmc | Mechanism-Based Pharmacokinetic–Pharmacodynamic Modeling of the Dopamine D 2 Receptor Occupancy of Olanzapine in Rats | Mechanism-Based Pharmacokinetic–Pharmacodynamic Modeling of the Dopamine D 2 Receptor Occupancy of Olanzapine in Rats Abstract Abstract Purpose A mechanism-based PK-PD model was developed to predict the time course of dopamine D 2 receptor occupancy (D 2 RO) in rat striatum following administration of olanzapine, an at... |
PMC11017206 | core_pubmed_pmc | Sources of pharmacokinetic and pharmacodynamic variability and clinical pharmacology studies of antiseizure medications in the pediatric population | Sources of pharmacokinetic and pharmacodynamic variability and clinical pharmacology studies of antiseizure medications in the pediatric population Abstract Abstract Multiple treatment options exist for children with epilepsy, including surgery, dietary therapies, neurostimulation, and antiseizure medications (ASMs). A... |
PMC5463067 | core_pubmed_pmc | Methionine tumor starvation by erythrocyte‐encapsulated methionine gamma‐lyase activity controlled with per os vitamin B6 | Methionine tumor starvation by erythrocyte‐encapsulated methionine gamma‐lyase activity controlled with per os vitamin B6 Abstract Abstract Erymet is a new therapy resulting from the encapsulation of a methionine gamma‐lyase (MGL; EC number 4.4.1.11) in red blood cells (RBC). The aim of this study was to evaluate eryme... |
PMC12494056 | core_pubmed_pmc | Towards precision dosing of vancomycin in patients with allogeneic hematopoietic stem cell transplantation: a comparison of published population pharmacokinetic models | Towards precision dosing of vancomycin in patients with allogeneic hematopoietic stem cell transplantation: a comparison of published population pharmacokinetic models Abstract ABSTRACT Patients undergoing allogeneic hematopoietic stem cell transplantation (allo-HSCT) often receive vancomycin as antibiotic treatment us... |
PMC6585761 | core_pubmed_pmc | Tramadol Hydrochloride at Steady State Lacks Clinically Relevant QTc Interval Increases in Healthy Adults | Tramadol Hydrochloride at Steady State Lacks Clinically Relevant QTc Interval Increases in Healthy Adults Abstract Abstract We evaluated the effects of therapeutic and supratherapeutic doses of tramadol hydrochloride on the corrected QT (QTc) interval in healthy adults (aged 18‐55 years) in a randomized, phase I, doubl... |
PMC8112988 | core_pubmed_pmc | A Multicenter Study of Docetaxel at a Dose of 100 mg/m 2 in Japanese Patients with Advanced or Recurrent Breast Cancer | A Multicenter Study of Docetaxel at a Dose of 100 mg/m 2 in Japanese Patients with Advanced or Recurrent Breast Cancer Abstract Objective This study examined the pharmacokinetics, safety and anti-tumor activity of docetaxel at a dose of 100 mg/m 2 in Japanese patients with advanced or recurrent breast cancer. Methods J... |
PMC12450378 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling and Dose Optimization of Linezolid in Pediatric Patients With Renal Impairment | Physiologically Based Pharmacokinetic Modeling and Dose Optimization of Linezolid in Pediatric Patients With Renal Impairment Abstract Abstract Objective Linezolid (LZD), a commonly used antimicrobial agent in clinical practice, has not undergone adequate pharmacokinetic (PK) assessment in pediatric populations with re... |
PMC3292503 | core_pubmed_pmc | Transarterial chemoembolization plus or minus intravenous bevacizumab in the treatment of hepatocellular cancer: A pilot study | Transarterial chemoembolization plus or minus intravenous bevacizumab in the treatment of hepatocellular cancer: A pilot study Abstract Background Stimulation of vascular endothelial growth factor (VEGF) has been observed following transarterial chemoembolization (TACE) in hepatocellular cancer (HCC) and may contribute... |
PMC11738623 | core_pubmed_pmc | Integrated serum pharmacochemistry, pharmacokinetics, and network analysis to explore active components of BuShao Tiaozhi Capsule on hyperlipidemia | Integrated serum pharmacochemistry, pharmacokinetics, and network analysis to explore active components of BuShao Tiaozhi Capsule on hyperlipidemia Abstract Abstract BuShao Tiaozhi Capsule (BSTZC), a novel drug in China, has been used to treat hyperlipidemia (HLP) in clinical practice for many years. Despite our previo... |
PMC12185581 | core_pubmed_pmc | Population Pharmacokinetic Analysis of an Octreotide Depot (CAM2029) in the Treatment of Acromegaly | Population Pharmacokinetic Analysis of an Octreotide Depot (CAM2029) in the Treatment of Acromegaly Abstract Abstract Introduction Octreotide is a first-generation somatostatin receptor ligand (SRL) approved for acromegaly treatment. CAM2029 is a sustained-release subcutaneous octreotide injection designed to improve t... |
PMC8124935 | core_pubmed_pmc | Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation | Investigation of Antifungal Properties of Synthetic Dimethyl-4-Bromo-1-(Substituted Benzoyl) Pyrrolo[1,2-a] Quinoline-2,3-Dicarboxylates Analogues: Molecular Docking Studies and Conceptual DFT-Based Chemical Reactivity Descriptors and Pharmacokinetics Evaluation Abstract Abstract Candida albicans , an opportunistic fun... |
PMC11768932 | core_pubmed_pmc | Pharmacokinetic Evaluation of Neutral Sphinghomyelinase2 (nSMase2) Inhibitor Prodrugs in Mice and Dogs | Pharmacokinetic Evaluation of Neutral Sphinghomyelinase2 (nSMase2) Inhibitor Prodrugs in Mice and Dogs Abstract Background : Extracellular vesicles (EVs) can carry pathological cargo, contributing to disease progression. The enzyme neutral sphingomyelinase 2 (nSMase2) plays a critical role in EV biogenesis, making it a... |
PMC8600545 | core_pubmed_pmc | Action of mefloquine/amitriptyline THN101 combination on neuropathic mechanical hypersensitivity in mice | Action of mefloquine/amitriptyline THN101 combination on neuropathic mechanical hypersensitivity in mice Abstract Supplemental Digital Content is Available in the Text. Mefloquine/amitriptyline THN101 combination reduces cuff-induced neuropathic hypersensitivity by recruiting noradrenergic descending pathways and α 2 a... |
PMC3561611 | core_pubmed_pmc | Effect of Concomitant Administration of Trospium Chloride Extended Release on the Steady-State Pharmacokinetics of Metformin in Healthy Adults | Effect of Concomitant Administration of Trospium Chloride Extended Release on the Steady-State Pharmacokinetics of Metformin in Healthy Adults Abstract Abstract Background Overactive bladder (OAB) is often associated with a number of co-morbid medical conditions, including diabetes mellitus. This may necessitate severa... |
PMC5686655 | core_pubmed_pmc | Serum Testosterone Concentrations Remain Stable Between Injections in Patients Receiving Subcutaneous Testosterone | Serum Testosterone Concentrations Remain Stable Between Injections in Patients Receiving Subcutaneous Testosterone Abstract Abstract Purpose: Intramuscular (IM) testosterone is the most common modality for testosterone therapy of both male hypogonadism and female-to-male (FTM) gender transition. However, IM injections ... |
PMC11574258 | core_pubmed_pmc | Formulation development, characterization, and mechanistic PBPK modeling of metoclopramide loaded halloysite nanotube (HNT) based drug-in-adhesive type transdermal drug delivery system | Formulation development, characterization, and mechanistic PBPK modeling of metoclopramide loaded halloysite nanotube (HNT) based drug-in-adhesive type transdermal drug delivery system Abstract Abstract Metoclopramide is an antiemetic agent prescribed for motion sickness, cancer chemotherapy, and pregnancy. The present... |
PMC11099671 | core_pubmed_pmc | Pharmacokinetics and Effects on Saliva Flow of Sublingual and Oral Atropine in Clozapine-Treated and Healthy Adults: An Interventional Cross-Over Study | Pharmacokinetics and Effects on Saliva Flow of Sublingual and Oral Atropine in Clozapine-Treated and Healthy Adults: An Interventional Cross-Over Study Abstract Abstract Background: Sublingual atropine is an effective treatment of clozapine-induced hypersalivation. This study aims to investigate the pharmacokinetics of... |
PMC10386943 | core_pubmed_pmc | Clinical Pharmacology of Brigatinib: A Next-Generation Anaplastic Lymphoma Kinase Inhibitor | Clinical Pharmacology of Brigatinib: A Next-Generation Anaplastic Lymphoma Kinase Inhibitor Abstract Abstract Brigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor designed to overcome mechanisms of resistance associated with crizotinib, is approved for the treatment of ALK -positive advanced or meta... |
PMC12030190 | core_pubmed_pmc | Alectinib-Loaded Chitosan–Alginate Nanoparticles: A Novel Synthesis Method with In Vitro and In Vivo Evaluations | Alectinib-Loaded Chitosan–Alginate Nanoparticles: A Novel Synthesis Method with In Vitro and In Vivo Evaluations Abstract Abstract Background/Objectives : Non-small cell lung cancer (NSCLC) constitutes over 84% of all lung cancer cases and is a leading cause of cancer-related mortality globally. Alectinib, a second-gen... |
PMC12159872 | core_pubmed_pmc | Navigating the complexities of drug development for metallo-β-lactamase inhibitors | Navigating the complexities of drug development for metallo-β-lactamase inhibitors Abstract Abstract The rising antibiotic resistance rates, especially among carbapenem-resistant Enterobacterales with metallo-β-lactamases (MBLs), highlight the urgent need for effective MBL inhibitors (MBLIs). Navigating the complexitie... |
PMC12469574 | core_pubmed_pmc | Pharmacogenetics Approach for Personalized Tacrolimus Dosing in Heart Transplantation: A Case Report and Literature Review | Pharmacogenetics Approach for Personalized Tacrolimus Dosing in Heart Transplantation: A Case Report and Literature Review Abstract Background: Tacrolimus is a cornerstone of immunosuppressive therapy following heart transplantation. Despite routine therapeutic drug monitoring (TDM), substantial interindividual variabi... |
PMC11470537 | core_pubmed_pmc | N-alkylation of amines for the synthesis of potential antiviral agents: A structural modification approach | N-alkylation of amines for the synthesis of potential antiviral agents: A structural modification approach Abstract The threat of emerging viral outbreaks has increased the need for fast and effective development of therapeutics against emerging pathogens. One approach is to modify the structure of existing therapeutic... |
PMC12382608 | core_pubmed_pmc | Preliminary Pharmacokinetic Analysis of Tramadol and Its Metabolite O-Desmethyltramadol in Boa ( Boa constrictor constrictor ) | Preliminary Pharmacokinetic Analysis of Tramadol and Its Metabolite O-Desmethyltramadol in Boa ( Boa constrictor constrictor ) Abstract Simple Summary Tramadol is commonly used for pain relief in both humans and animals; however, its pharmacokinetics in reptiles, especially snakes, are not well understood. Pharmacokine... |
PMC10923241 | core_pubmed_pmc | Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity | Scopoletin: a review of its pharmacology, pharmacokinetics, and toxicity Abstract Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, p... |
PMC11187260 | core_pubmed_pmc | Unraveling the interconversion pharmacokinetics and oral bioavailability of the major ginger constituents: [6]-gingerol, [6]-shogaol, and zingerone after single-dose administration in rats | Unraveling the interconversion pharmacokinetics and oral bioavailability of the major ginger constituents: [6]-gingerol, [6]-shogaol, and zingerone after single-dose administration in rats Abstract Abstract Background The available in vitro evidences suggest the inherent instability and interconvertibility of -gingerol... |
PMC4128677 | core_pubmed_pmc | Somatostatin Analogues for Receptor Targeted Photodynamic Therapy | Somatostatin Analogues for Receptor Targeted Photodynamic Therapy Abstract Abstract Photodynamic therapy (PDT) is an established treatment modality, used mainly for anticancer therapy that relies on the interaction of photosensitizer, light and oxygen. For the treatment of pathologies in certain anatomical sites, impro... |
PMC4564187 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Characterisation of an Anti-Mouse TNF Receptor 1 Domain Antibody Formatted for In Vivo Half-Life Extension | Pharmacokinetic and Pharmacodynamic Characterisation of an Anti-Mouse TNF Receptor 1 Domain Antibody Formatted for In Vivo Half-Life Extension Abstract Tumour Necrosis Factor-α (TNF-α) inhibition has been transformational in the treatment of patients with inflammatory disease, e.g. rheumatoid arthritis. Intriguingly, T... |
PMC4619821 | core_pubmed_pmc | Inhibition of P-Selectin and PSGL-1 Using Humanized Monoclonal Antibodies Increases the Sensitivity of Multiple Myeloma Cells to Bortezomib | Inhibition of P-Selectin and PSGL-1 Using Humanized Monoclonal Antibodies Increases the Sensitivity of Multiple Myeloma Cells to Bortezomib Abstract Multiple myeloma (MM) is a plasma cell malignancy localized in the bone marrow. Despite the introduction of novel therapies majority of MM patients relapse. We have previo... |
PMC10376825 | core_pubmed_pmc | Voriconazole Pharmacokinetics in Critically Ill Patients and Extracorporeal Membrane Oxygenation Support: A Retrospective Comparative Case-Control Study | Voriconazole Pharmacokinetics in Critically Ill Patients and Extracorporeal Membrane Oxygenation Support: A Retrospective Comparative Case-Control Study Abstract Abstract Voriconazole, an antifungal agent, displays high intra- and inter-individual variability. The predictive pharmacokinetic (PK) index requires a minimu... |
PMC12424289 | core_pubmed_pmc | Programmable Nanostructure Assembly of a Paclitaxel Derivative Enables Tunable Anticancer Therapy via Hydrogen Bond Engineering | Programmable Nanostructure Assembly of a Paclitaxel Derivative Enables Tunable Anticancer Therapy via Hydrogen Bond Engineering Abstract Precise control of the morphology of self-assembling drugs is critical for optimizing their pharmacokinetics and therapeutic efficacy. However, adapting a single drug for diverse ther... |
PMC4875922 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of FAAH Inhibitor V158866: A Double-Blind, Randomised, Placebo-Controlled Phase I Study in Healthy Volunteers | Safety, Tolerability and Pharmacokinetics of FAAH Inhibitor V158866: A Double-Blind, Randomised, Placebo-Controlled Phase I Study in Healthy Volunteers Abstract Background and Objective The inhibition of fatty acid amide hydrolase 1 (FAAH) has been proposed as a novel mechanism for treating pain syndromes by increasing... |
PMC5623731 | core_pubmed_pmc | Phase I/ II study of pralatrexate in Japanese patients with relapsed or refractory peripheral T‐cell lymphoma | Phase I/ II study of pralatrexate in Japanese patients with relapsed or refractory peripheral T‐cell lymphoma Abstract Pralatrexate is a novel antifolate approved in the USA for the treatment of relapsed or refractory peripheral T‐cell lymphoma. To assess its safety, efficacy, and pharmacokinetics in Japanese patients ... |
PMC9529013 | core_pubmed_pmc | Pharmacokinetics of Herb-Drug Interactions of Plumbagin and Tazemetostat in Rats by UPLC-MS/MS | Pharmacokinetics of Herb-Drug Interactions of Plumbagin and Tazemetostat in Rats by UPLC-MS/MS Abstract Objective A sensitive and rapid UPLC-MS/MS method for determination of tazemetostat in rat plasma was developed, and the pharmacokinetics of herb-drug interactions (HDIs) of plumbagin (PLB) and tazemetostat was inves... |
PMC12456800 | core_pubmed_pmc | Dual efficacy-toxicity of Chelidonii Herba in chronic obstructive pulmonary disease: Integrated network pharmacology, immune profiling and molecular docking | Dual efficacy-toxicity of Chelidonii Herba in chronic obstructive pulmonary disease: Integrated network pharmacology, immune profiling and molecular docking Abstract Abstract Objective To investigate the pharmacodynamic material basis, multi-target mechanisms of Chelidonii Herba in treating chronic obstructive pulmonar... |
PMC12389038 | core_pubmed_pmc | Significant Improvement in Bioavailability and Therapeutic Efficacy of Mebendazole Oral Nano-Systems Assessed in a Murine Model with Extreme Phenotypes of Susceptibility to Trichinella spiralis | Significant Improvement in Bioavailability and Therapeutic Efficacy of Mebendazole Oral Nano-Systems Assessed in a Murine Model with Extreme Phenotypes of Susceptibility to Trichinella spiralis Abstract This study aimed to analyze whether the enhancement of the biopharmaceutical efficiency of mebendazole, a poorly wate... |
PMC9637881 | core_pubmed_pmc | Physiologically based pharmacokinetic (PBPK) modeling of the role of CYP2D6 polymorphism for metabolic phenotyping with dextromethorphan | Physiologically based pharmacokinetic (PBPK) modeling of the role of CYP2D6 polymorphism for metabolic phenotyping with dextromethorphan Abstract Abstract The cytochrome P450 2D6 (CYP2D6) is a key xenobiotic-metabolizing enzyme involved in the clearance of many drugs. Genetic polymorphisms in CYP2D6 contribute to the l... |
PMC12096718 | core_pubmed_pmc | First dose target attainment with extended infusion regimens of piperacillin and meropenem | First dose target attainment with extended infusion regimens of piperacillin and meropenem Abstract Abstract Background Standard dosing regimens of meropenem and piperacillin-tazobactam frequently fail to achieve targeted plasma concentrations in critically ill patients. Extended or continuous regimens are often used t... |
PMC12583980 | core_pubmed_pmc | First‐in‐Human Study of Merotocin, a Short‐Acting Peptidic Oxytocin Receptor Agonist for Lactation Support | First‐in‐Human Study of Merotocin, a Short‐Acting Peptidic Oxytocin Receptor Agonist for Lactation Support Abstract Abstract Endogenous oxytocin plays an important role in lactation, but its effectiveness as an exogenous galactagogue has been modest due to dose‐limiting side effects related to off‐target effects at the... |
PMC8243370 | core_pubmed_pmc | Therapeutic Effectiveness and Safety of Repurposing Drugs for the Treatment of COVID-19: Position Standing in 2021 | Therapeutic Effectiveness and Safety of Repurposing Drugs for the Treatment of COVID-19: Position Standing in 2021 Abstract Abstract COVID-19, transmitted by SARS-CoV-2, is one of the most serious pandemic situations in the history of mankind, and has already infected a huge population across the globe. This horrendous... |
PMC11966027 | core_pubmed_pmc | Randomized crossover clinical studies to assess abuse liability and nicotine pharmacokinetics of Velo Oral Nicotine pouches | Randomized crossover clinical studies to assess abuse liability and nicotine pharmacokinetics of Velo Oral Nicotine pouches Abstract Abstract Introduction Oral nicotine pouches (ONPs) are a newer category of smokeless tobacco products containing pharmaceutical-grade nicotine but no tobacco leaf. These products have the... |
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