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PMC12899015 | core_pubmed_pmc | Ibogaine: Therapeutic Potential, Cardiac Safety, and Translational Perspectives in the Treatment of Substance Use Disorders—A Scoping Review | Ibogaine: Therapeutic Potential, Cardiac Safety, and Translational Perspectives in the Treatment of Substance Use Disorders—A Scoping Review Abstract Abstract Substance Use Disorder (SUD) constitutes a major and persistent global public health burden, accounting for approximately 600,000 deaths annually, largely driven... |
PMC9978582 | core_pubmed_pmc | Bronchopulmonary disposition of IV cefepime/taniborbactam (2–0.5 g) administered over 2 h in healthy adult subjects | Bronchopulmonary disposition of IV cefepime/taniborbactam (2–0.5 g) administered over 2 h in healthy adult subjects Abstract Abstract Introduction Taniborbactam (formerly VNRX-5133) is an investigational β-lactamase inhibitor in clinical development in combination with cefepime for the treatment of MDR Gram-negative pa... |
PMC9228987 | core_pubmed_pmc | Antiproliferative Activity of a New Quinazolin-4(3 H )-One Derivative via Targeting Aurora Kinase A in Non-Small Cell Lung Cancer | Antiproliferative Activity of a New Quinazolin-4(3 H )-One Derivative via Targeting Aurora Kinase A in Non-Small Cell Lung Cancer Abstract Abstract Non-small cell lung cancer (NSCLC) is the most common lung cancer subtype. Although chemotherapy and targeted therapy are used for the treatment of patients with NSCLC, the... |
PMC11412846 | core_pubmed_pmc | Exploring pharmacokinetic variability of palbociclib in HR+/HER2- metastatic breast cancer: a focus on age, renal function, and drug–gene interactions | Exploring pharmacokinetic variability of palbociclib in HR+/HER2- metastatic breast cancer: a focus on age, renal function, and drug–gene interactions Abstract Palbociclib, an oral inhibitor of cyclin-dependent kinase 4 and 6, is approved for the treatment of metastatic breast cancer. This study investigated the influe... |
PMC10394516 | core_pubmed_pmc | The pharmacokinetic profile of brensocatib and its effect on pharmacodynamic biomarkers including NE, PR3, and CatG in various rodent species | The pharmacokinetic profile of brensocatib and its effect on pharmacodynamic biomarkers including NE, PR3, and CatG in various rodent species Abstract Abstract Brensocatib is a novel, oral, selective, reversible inhibitor of dipeptidyl peptidase 1 (DPP1), which activates several neutrophil serine proteases (NSPs), incl... |
PMC9097888 | core_pubmed_pmc | Review: Role of Model-Informed Drug Development Approaches in the Lifecycle of Drug Development and Regulatory Decision-Making | Review: Role of Model-Informed Drug Development Approaches in the Lifecycle of Drug Development and Regulatory Decision-Making Abstract Abstract Model-informed drug development (MIDD) is a powerful approach to support drug development and regulatory review. There is a rich history of MIDD applications at the U.S. Food ... |
PMC10239661 | core_pubmed_pmc | Simulation of optimal dose regimens of photoactivated curcumin for antimicrobial resistance pneumonia in COVID-19 patients: A modeling approach | Simulation of optimal dose regimens of photoactivated curcumin for antimicrobial resistance pneumonia in COVID-19 patients: A modeling approach Abstract Abstract Background Secondary antimicrobial resistance bacterial (AMR) pneumonia could lead to an increase in mortality in COVID-19 patients, particularly of geriatric... |
PMC9229424 | core_pubmed_pmc | Remifentanil requirement for i-gel insertion is reduced in male patients with Parkinson’s disease undergoing deep brain stimulator implantation: an up-and-down sequential allocation trial | Remifentanil requirement for i-gel insertion is reduced in male patients with Parkinson’s disease undergoing deep brain stimulator implantation: an up-and-down sequential allocation trial Abstract Abstract Background Laryngeal mask airways have been widely used in clinical practice. The aim of this study was to investi... |
PMC10220404 | core_pubmed_pmc | Development and validation of an LC-MS/MS method to quantify ceftaroline in microdialysate samples from plasma and brain: Application to a preclinical pharmacokinetic investigation | Development and validation of an LC-MS/MS method to quantify ceftaroline in microdialysate samples from plasma and brain: Application to a preclinical pharmacokinetic investigation Abstract Abstract A bioanalytical LC–MS/MS method was developed and validated to determine ceftaroline in microdialysate samples from plasm... |
PMC4425551 | core_pubmed_pmc | Pioglitazone Increases Whole Body Insulin Sensitivity in Obese, Insulin-Resistant Rhesus Monkeys | Pioglitazone Increases Whole Body Insulin Sensitivity in Obese, Insulin-Resistant Rhesus Monkeys Abstract Abstract Hyperinsulinemic-euglycemic clamps are considered the "gold standard" for assessing whole body insulin sensitivity. When used in combination with tracer dilution techniques and physiological insulin concen... |
PMC5513836 | core_pubmed_pmc | A 6-month mixed-effect pharmacokinetic model for post-transplant intravenous anti-hepatitis B immunoglobulin prophylaxis | A 6-month mixed-effect pharmacokinetic model for post-transplant intravenous anti-hepatitis B immunoglobulin prophylaxis Abstract Background Although individualized dosage regimens for anti-hepatitis B immunoglobulin (HBIG) therapy have been suggested, the pharmacokinetic profile and factors influencing the basis for i... |
PMC11387650 | core_pubmed_pmc | PharmaBench: Enhancing ADMET benchmarks with large language models | PharmaBench: Enhancing ADMET benchmarks with large language models Abstract Accurately predicting ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) properties early in drug development is essential for selecting compounds with optimal pharmacokinetics and minimal toxicity. Existing ADMET-related ben... |
PMC8901234 | core_pubmed_pmc | Safety, Pharmacokinetics and Pharmacodynamics of the Selective Glucocorticoid Receptor Modulator Velsecorat (AZD7594) Following Inhalation in Healthy Volunteers | Safety, Pharmacokinetics and Pharmacodynamics of the Selective Glucocorticoid Receptor Modulator Velsecorat (AZD7594) Following Inhalation in Healthy Volunteers Abstract Abstract Introduction Velsecorat (AZD7594) is a non-steroidal, selective, glucocorticoid receptor modulator (SGRM), being developed for the treatment ... |
PMC8538061 | core_pubmed_pmc | Pharmacokinetic Variability and Target Attainment of Fluconazole in Critically Ill Patients | Pharmacokinetic Variability and Target Attainment of Fluconazole in Critically Ill Patients Abstract Background : Fluconazole is one of the oldest antifungal drugs. Previous studies have raised concerns considering variability in exposure and inadequate target attainment in critically ill patients. The current study ai... |
PMC9541555 | core_pubmed_pmc | Delayed concentration effect models for dabigatran anticoagulation | Delayed concentration effect models for dabigatran anticoagulation Abstract Abstract Introduction Dabigatran is an anticoagulant with potential use during cardiopulmonary bypass in children and adults. The pharmacokinetic–pharmacodynamic relationship for dabigatran anticoagulation effect was investigated in an intact a... |
PMC7093595 | core_pubmed_pmc | Model-Based Simulation of Maintenance Therapy of Childhood Acute Lymphoblastic Leukemia | Model-Based Simulation of Maintenance Therapy of Childhood Acute Lymphoblastic Leukemia Abstract Acute lymphoblastic leukemia is the most common malignancy in childhood. Successful treatment requires initial high-intensity chemotherapy, followed by low-intensity oral maintenance therapy with oral 6-mercaptopurine (6MP)... |
PMC6028884 | core_pubmed_pmc | Population Pharmacokinetics of Upadacitinib in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I and II Clinical Trials | Population Pharmacokinetics of Upadacitinib in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I and II Clinical Trials Abstract Background and Objectives Upadacitinib is a janus kinase (JAK) 1 inhibitor being developed for the treatment of rheumatoid arthritis (RA) and other inflammatory dis... |
PMC5385193 | core_pubmed_pmc | A Pooled Analysis of Clinical Pharmacology Trials Investigating the Pharmacokinetic and Pharmacodynamic Characteristics of Fast-Acting Insulin Aspart in Adults with Type 1 Diabetes | A Pooled Analysis of Clinical Pharmacology Trials Investigating the Pharmacokinetic and Pharmacodynamic Characteristics of Fast-Acting Insulin Aspart in Adults with Type 1 Diabetes Abstract Abstract Background Fast-acting insulin aspart (faster aspart) is insulin aspart (IAsp) in a new formulation aiming to mimic the f... |
PMC4674575 | core_pubmed_pmc | Genetic Resistance Determinants, In Vitro Time-Kill Curve Analysis and Pharmacodynamic Functions for the Novel Topoisomerase II Inhibitor ETX0914 (AZD0914) in Neisseria gonorrhoeae | Genetic Resistance Determinants, In Vitro Time-Kill Curve Analysis and Pharmacodynamic Functions for the Novel Topoisomerase II Inhibitor ETX0914 (AZD0914) in Neisseria gonorrhoeae Abstract Abstract Resistance in Neisseria gonorrhoeae to all available therapeutic antimicrobials has emerged and new efficacious drugs for... |
PMC11920349 | core_pubmed_pmc | Imputation of missing clock times – application to procalcitonin concentration time course after birth | Imputation of missing clock times – application to procalcitonin concentration time course after birth Abstract Abstract The time course of biomarkers (e.g., acute phase proteins) are typically described using days relative to events of interest, such as surgery or birth, without specifying the sample time. This limits... |
PMC4632083 | core_pubmed_pmc | No effect on pharmacokinetics of tamoxifen and 4-hydroxytamoxifen by multiple doses of red clover capsule in rats | No effect on pharmacokinetics of tamoxifen and 4-hydroxytamoxifen by multiple doses of red clover capsule in rats Abstract Tamoxifen is used in clinical practice for breast cancer patients and to prevent osteoporosis. Red clover ( Trifolium pratense ) preparations are consumed worldwide as dietary supplements for relie... |
PMC9323086 | core_pubmed_pmc | Comparative Pharmacokinetics of Three Bioactive Diterpenoids of Rabdosia serra Extract in Normal and Con A-Induced Liver Injury Rats Using UPLC-MS/MS | Comparative Pharmacokinetics of Three Bioactive Diterpenoids of Rabdosia serra Extract in Normal and Con A-Induced Liver Injury Rats Using UPLC-MS/MS Abstract Rabdosia serra (Maxim.) Hara ( R. serra ), one of the source plants of “Xihuangcao”, has been widely used as a Chinese folk herb with the concomitant function of... |
PMC9454848 | core_pubmed_pmc | BMS-986158, a Small Molecule Inhibitor of the Bromodomain and Extraterminal Domain Proteins, in Patients with Selected Advanced Solid Tumors: Results from a Phase 1/2a Trial | BMS-986158, a Small Molecule Inhibitor of the Bromodomain and Extraterminal Domain Proteins, in Patients with Selected Advanced Solid Tumors: Results from a Phase 1/2a Trial Abstract Simple Summary Bromodomain and extraterminal domain (BET) proteins can regulate cancer-related genes to make tumors grow. BMS-986158, an ... |
PMC5702344 | core_pubmed_pmc | The Clinical Pharmacokinetics and Pharmacodynamics of Warfarin When Combined with Compound Danshen: A Case Study for Combined Treatment of Coronary Heart Diseases with Atrial Fibrillation | The Clinical Pharmacokinetics and Pharmacodynamics of Warfarin When Combined with Compound Danshen: A Case Study for Combined Treatment of Coronary Heart Diseases with Atrial Fibrillation Abstract Warfarin is used as anticoagulant and Compound Danshen prescription (CDP) is able to promote blood circulation. The combina... |
PMC7179319 | core_pubmed_pmc | Fourteen-Day Bactericidal Activity, Safety, and Pharmacokinetics of Linezolid in Adults with Drug-Sensitive Pulmonary Tuberculosis | Fourteen-Day Bactericidal Activity, Safety, and Pharmacokinetics of Linezolid in Adults with Drug-Sensitive Pulmonary Tuberculosis Abstract Linezolid is increasingly used for the treatment of tuberculosis resistant to first-line agents, but the most effective dosing strategy is yet unknown. From November 2014 to Novemb... |
PMC10919156 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics in healthy Chinese volunteers treated with SC0062, a highly selective endothelin‐A receptor antagonist | Safety, pharmacokinetics, and pharmacodynamics in healthy Chinese volunteers treated with SC0062, a highly selective endothelin‐A receptor antagonist Abstract Abstract This study evaluated the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and food effects (FE) of SC0062, a highly active endothelin... |
PMC7407796 | core_pubmed_pmc | What Are the Current Approaches to Optimising Antimicrobial Dosing in the Intensive Care Unit? | What Are the Current Approaches to Optimising Antimicrobial Dosing in the Intensive Care Unit? Abstract Abstract Antimicrobial dosing in the intensive care unit (ICU) can be problematic due to various challenges including unique physiological changes observed in critically ill patients and the presence of pathogens wit... |
PMC12202198 | core_pubmed_pmc | Pharmacokinetics and Safety of Fenofibrate in Participants with Mild Hepatic Impairment or with Advanced Fibrosis due to Metabolic‐Associated Fatty Liver Disease | Pharmacokinetics and Safety of Fenofibrate in Participants with Mild Hepatic Impairment or with Advanced Fibrosis due to Metabolic‐Associated Fatty Liver Disease Abstract Abstract Fenofibrate is contraindicated in patients with advanced hepatic fibrosis due to limited clinical data. We evaluated the pharmacokinetics an... |
PMC9268243 | core_pubmed_pmc | Metabolic Behaviors of Aconitum Alkaloids in Different Concentrations of Aconiti Lateralis Radix Praeparata and Effects of Aconitine in Healthy Human and Long QT Syndrome Cardiomyocytes | Metabolic Behaviors of Aconitum Alkaloids in Different Concentrations of Aconiti Lateralis Radix Praeparata and Effects of Aconitine in Healthy Human and Long QT Syndrome Cardiomyocytes Abstract Aconiti Lateralis Radix Praeparata ( Fu Zi ) is the processed lateral root of Aconitum carmichaelii Debx, which is widely use... |
PMC8470654 | core_pubmed_pmc | Antimicrobial Properties of Antidepressants and Antipsychotics—Possibilities and Implications | Antimicrobial Properties of Antidepressants and Antipsychotics—Possibilities and Implications Abstract Abstract The spreading of antibiotic resistance is responsible annually for over 700,000 deaths worldwide, and the prevision is that this number will increase exponentially. The identification of new antimicrobial tre... |
PMC7016994 | core_pubmed_pmc | Quantitative Predictive Modelling Approaches to Understanding Rheumatoid Arthritis: A Brief Review | Quantitative Predictive Modelling Approaches to Understanding Rheumatoid Arthritis: A Brief Review Abstract Rheumatoid arthritis is a chronic autoimmune disease that is a major public health challenge. The disease is characterised by inflammation of synovial joints and cartilage erosion, which lead to chronic pain, poo... |
PMC7819157 | core_pubmed_pmc | TAT-modified serum albumin nanoparticles for sustained-release of tetramethylpyrazine and improved targeting to spinal cord injury | TAT-modified serum albumin nanoparticles for sustained-release of tetramethylpyrazine and improved targeting to spinal cord injury Abstract Abstract Background Spinal Cord injury (SCI) is a kind of severe traumatic disease. The inflammatory response is a significant feature after SCI. Tetramethylpyrazine (TMP), a peren... |
PMC7595962 | core_pubmed_pmc | Drug–Drug Interactions between Direct Oral Anticoagulants and Hepatitis C Direct-Acting Antiviral Agents: Looking for Evidence Through a Systematic Review | Drug–Drug Interactions between Direct Oral Anticoagulants and Hepatitis C Direct-Acting Antiviral Agents: Looking for Evidence Through a Systematic Review Abstract Background Direct oral anticoagulants (DOACs), as substrates of cytochrome P450 (CYP) 3A4 and/or P-glycoprotein, are susceptible to drug–drug interactions (... |
PMC10750411 | core_pubmed_pmc | Drug transport by red blood cells | Drug transport by red blood cells Abstract This review focuses on the role of human red blood cells (RBCs) as drug carriers. First, a general introduction about RBC physiology is provided, followed by the presentation of several cases in which RBCs act as natural carriers of drugs. This is due to the presence of severa... |
PMC9692583 | core_pubmed_pmc | Inferring Therapeutic Targets in Candida albicans and Possible Inhibition through Natural Products: A Binding and Physiological Based Pharmacokinetics Snapshot | Inferring Therapeutic Targets in Candida albicans and Possible Inhibition through Natural Products: A Binding and Physiological Based Pharmacokinetics Snapshot Abstract Abstract Despite being responsible for invasive infections, fungal pathogens have been underrepresented in computer aided therapeutic target mining and... |
PMC8241167 | core_pubmed_pmc | Loratadine bioavailability via buccal transferosomal gel: formulation, statistical optimization, in vitro / in vivo characterization, and pharmacokinetics in human volunteers | Loratadine bioavailability via buccal transferosomal gel: formulation, statistical optimization, in vitro / in vivo characterization, and pharmacokinetics in human volunteers Abstract Abstract Loratadine (LTD) is an antihistaminic drug that suffers limited solubility, poor oral bioavailability (owing to extensive first... |
PMC8610051 | core_pubmed_pmc | Calcipotriene/betamethasone dipropionate foam: primary evidence supporting its use in patients with psoriasis vulgaris. A narrative review | Calcipotriene/betamethasone dipropionate foam: primary evidence supporting its use in patients with psoriasis vulgaris. A narrative review Abstract Psoriasis vulgaris is a chronic, immune-mediated disorder, which has a substantial impact on all aspects of patients’ quality of life. In most patients, the disease is mild... |
PMC7187247 | core_pubmed_pmc | Clinical Pharmacology and Safety of Trifarotene, a First‐in‐Class RARγ‐Selective Topical Retinoid | Clinical Pharmacology and Safety of Trifarotene, a First‐in‐Class RARγ‐Selective Topical Retinoid Abstract Abstract Trifarotene is a new drug with retinoic acid receptor activity and selectivity for retinoic acid receptor‐γ. The reported studies aimed at assessing the clinical pharmacology and safety of trifarotene. Th... |
PMC10143068 | core_pubmed_pmc | Injectable In-Situ Forming Depot Based on PLGA and PLGA-PEG-PLGA for Sustained-Release of Risperidone: In Vitro Evaluation and Pharmacokinetics in Rabbits | Injectable In-Situ Forming Depot Based on PLGA and PLGA-PEG-PLGA for Sustained-Release of Risperidone: In Vitro Evaluation and Pharmacokinetics in Rabbits Abstract Abstract In the current research, novel drug delivery systems based on in situ forming gel (ISFG) (PLGA-PEG-PLGA) and in situ forming implant (ISFI) (PLGA) ... |
PMC9660608 | core_pubmed_pmc | Optimisation of treatments for oral Neisseria gonorrhoeae infection: Pharmacokinetics Study (STI-PK project) – study protocol for non-randomised clinical trial | Optimisation of treatments for oral Neisseria gonorrhoeae infection: Pharmacokinetics Study (STI-PK project) – study protocol for non-randomised clinical trial Abstract Introduction Neisseria gonorrhoeae infections are common and incidence increasing. Oropharyngeal infections are associated with greater treatment failu... |
PMC9401457 | core_pubmed_pmc | Pharmacokinetics, Safety, and Efficacy of Trastuzumab Deruxtecan with Concomitant Ritonavir or Itraconazole in Patients with HER2-Expressing Advanced Solid Tumors | Pharmacokinetics, Safety, and Efficacy of Trastuzumab Deruxtecan with Concomitant Ritonavir or Itraconazole in Patients with HER2-Expressing Advanced Solid Tumors Abstract Abstract Purpose: To evaluate drug–drug interactions between the human epidermal growth factor receptor 2 (HER2)–targeted antibody-drug conjugate tr... |
PMC6914903 | core_pubmed_pmc | Mitochondrial Dysfunction and Alpha-Lipoic Acid: Beneficial or Harmful in Alzheimer's Disease? | Mitochondrial Dysfunction and Alpha-Lipoic Acid: Beneficial or Harmful in Alzheimer's Disease? Abstract Alzheimer's disease (AD) is a neurodegenerative disorder characterised by impairments in the cognitive domains associated with orientation, recording, and memory. This pathology results from an abnormal deposition of... |
PMC9609737 | core_pubmed_pmc | Design, Preparation, and Evaluation of Osthol Poly-Butyl-Cyanoacrylate Nanoparticles with Improved In Vitro Anticancer Activity in Neuroblastoma Treatment | Design, Preparation, and Evaluation of Osthol Poly-Butyl-Cyanoacrylate Nanoparticles with Improved In Vitro Anticancer Activity in Neuroblastoma Treatment Abstract Abstract Osthol (osthole), known as a neuroprotective drug, has shown potent anticancer activity. However, the potential clinical application of osthol is l... |
PMC6767974 | core_pubmed_pmc | Minimum Inhibitory Concentration Distribution of Fluconazole Against Cryptococcus Species and the Fluconazole Exposure Prediction Model | Minimum Inhibitory Concentration Distribution of Fluconazole Against Cryptococcus Species and the Fluconazole Exposure Prediction Model Abstract Abstract Background Fluconazole is lifesaving for treatment and prevention of cryptococcosis; however, optimal dosing is unknown. Initial fluconazole doses of 100 mg to 2000 m... |
PMC5433145 | core_pubmed_pmc | Perioperative management of patients on direct oral anticoagulants | Perioperative management of patients on direct oral anticoagulants Abstract Direct oral anticoagulants (DOACs) have been licensed worldwide for several years for various indications. Each year, 10–15% of patients on oral anticoagulants will undergo an invasive procedure and expert groups have issued several guidelines ... |
PMC2965873 | core_pubmed_pmc | Phase I and pharmacological study of the broad-spectrum tyrosine kinase inhibitor JNJ-26483327 in patients with advanced solid tumours | Phase I and pharmacological study of the broad-spectrum tyrosine kinase inhibitor JNJ-26483327 in patients with advanced solid tumours Abstract Abstract Background: JNJ-26483327 is an oral, potent, multi-targeted tyrosine kinase inhibitor, inhibiting kinases of epidermal growth factor receptor (EGFR)-1, -2 and -4, rear... |
PMC4919269 | core_pubmed_pmc | Renal PET-imaging with 11 C-metformin in a transgenic mouse model for chronic kidney disease | Renal PET-imaging with 11 C-metformin in a transgenic mouse model for chronic kidney disease Abstract Abstract Background Organic cation transporters (OCTs) in the renal proximal tubule are important for the excretion of both exo- and endogenous compounds, and chronic kidney disease (CKD) alter the expression of OCT. M... |
PMC7237449 | core_pubmed_pmc | Multi-objective optimization of tumor response to drug release from vasculature-bound nanoparticles | Multi-objective optimization of tumor response to drug release from vasculature-bound nanoparticles Abstract Abstract The pharmacokinetics of nanoparticle-borne drugs targeting tumors depends critically on nanoparticle design. Empirical approaches to evaluate such designs in order to maximize treatment efficacy are tim... |
PMC5761007 | core_pubmed_pmc | Bioanalytical method development and validation of milnacipran in rat plasma by LC–MS/MS detection and its application to a pharmacokinetic study | Bioanalytical method development and validation of milnacipran in rat plasma by LC–MS/MS detection and its application to a pharmacokinetic study Abstract Abstract A simple, sensitive and specific liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed for the quantification of milnacipran (MC) i... |
PMC7113567 | core_pubmed_pmc | Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits ( Oryctolagus cuniculus ) | Pharmacokinetic profiles of levofloxacin after intravenous, intramuscular and subcutaneous administration to rabbits ( Oryctolagus cuniculus ) Abstract Levofloxacin pharmacokinetic profiles were evaluated in 6 healthy female rabbits after intravenous (I/V), intramuscular (I/M), or subcutaneous (S/C) administration rout... |
PMC8147021 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic modelling of atazanavir in hair among adolescents on antiretroviral treatment in Zimbabwe | Pharmacokinetic-pharmacodynamic modelling of atazanavir in hair among adolescents on antiretroviral treatment in Zimbabwe Abstract Abstract Background Drug potency is a pharmacological parameter defining dose or concentration of drug required to obtain 50% of the drug’s maximal effect. Pharmacokinetic-pharmacodynamic m... |
PMC5642474 | core_pubmed_pmc | Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt’s lymphoma anti-tumor activity | Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt’s lymphoma anti-tumor activity Abstract Abstract Tumors frequently display a glycolytic phenotype with increased flux through glycolysis and concomitant synthesis of lactate. To maintain glycolytic flux and prevent intracellular... |
PMC10234445 | core_pubmed_pmc | Healthy volunteers in first‐in‐human oncology drug development for small molecules | Healthy volunteers in first‐in‐human oncology drug development for small molecules Abstract This review provides tools to consider the inclusion of healthy volunteers (HVs) in first‐in‐human (FIH) oncology clinical trials with small molecules, including targeted and immunomodulatory agents, a strategy that was not envi... |
PMC12896398 | core_pubmed_pmc | The Phase Ib VenObi CNS Study: Chemotherapy-Free Treatment with Venetoclax and Obinutuzumab for Relapsed/Refractory Primary Large B-Cell Lymphoma of the Central Nervous System | The Phase Ib VenObi CNS Study: Chemotherapy-Free Treatment with Venetoclax and Obinutuzumab for Relapsed/Refractory Primary Large B-Cell Lymphoma of the Central Nervous System Abstract Simple Summary Despite substantial advances in the treatment of primary large B-cell lymphoma of the central nervous system (PCNSL), up... |
PMC12445920 | core_pubmed_pmc | Correlation Between Chimeric Antigen Receptor T‐Cell Pharmacokinetic Data Measured by Flow Cytometry and Quantitative Polymerase Chain Reaction | Correlation Between Chimeric Antigen Receptor T‐Cell Pharmacokinetic Data Measured by Flow Cytometry and Quantitative Polymerase Chain Reaction Abstract ABSTRACT Chimeric antigen receptor (CAR)‐T cells have antitumor efficacy in hematological and solid malignancies. Unlike small molecules or antibodies, CAR‐T cells hav... |
PMC5859368 | core_pubmed_pmc | Acute Pharmacological Effects of 2C-B in Humans: An Observational Study | Acute Pharmacological Effects of 2C-B in Humans: An Observational Study Abstract Abstract 2,5-dimethoxy-4-bromophenethylamine (2C-B) is a psychedelic phenylethylamine derivative, structurally similar to mescaline. It is a serotonin 5-hydroxytryptamine-2A (5-HT 2A ), 5-hydroxytryptamine-2B (5-HT 2B ), and 5-hydroxytrypt... |
PMC4335822 | core_pubmed_pmc | Randomized study of teriflunomide effects on immune responses to neoantigen and recall antigens | Randomized study of teriflunomide effects on immune responses to neoantigen and recall antigens Abstract Objective: To evaluate immune responses to neoantigen and recall antigens in healthy subjects treated with teriflunomide. Methods: This was a randomized, double-blind, placebo-controlled study. Subjects received ora... |
PMC8743917 | core_pubmed_pmc | Quantitative analysis of efficacy and safety of LABA/LAMA fixed-dose combinations in the treatment of stable COPD | Quantitative analysis of efficacy and safety of LABA/LAMA fixed-dose combinations in the treatment of stable COPD Abstract Abstract Objective: This study aimed to quantitatively compare the efficacy and safety of long-acting β2-agonist (LABA)/long-acting muscarinic antagonist (LAMA) fixed-dose combinations (FDCs) for t... |
PMC8201069 | core_pubmed_pmc | Rekindling of a Masterful Precedent; Bacteriophage: Reappraisal and Future Pursuits | Rekindling of a Masterful Precedent; Bacteriophage: Reappraisal and Future Pursuits Abstract Antibiotic resistance is exuberantly becoming a deleterious health problem world-wide. Seeking innovative approaches is necessary in order to circumvent such a hazard. An unconventional fill-in to antibiotics is bacteriophage. ... |
PMC9250213 | core_pubmed_pmc | Population pharmacokinetic modeling of CSF to blood clearance: prospective tracer study of 161 patients under work-up for CSF disorders | Population pharmacokinetic modeling of CSF to blood clearance: prospective tracer study of 161 patients under work-up for CSF disorders Abstract Abstract Background Quantitative measurements of cerebrospinal fluid to blood clearance has previously not been established for neurological diseases. Possibly, variability in... |
PMC9958968 | core_pubmed_pmc | Unveiling the Pharmacological and Nanotechnological Facets of Daidzein: Present State-of-the-Art and Future Perspectives | Unveiling the Pharmacological and Nanotechnological Facets of Daidzein: Present State-of-the-Art and Future Perspectives Abstract Herbal drugs have been attracting much scientific interest in the last few decades and nowadays, phytoconstituents-based research is in progress to disclose their unidentified medicinal pote... |
PMC4169032 | core_pubmed_pmc | Immune suppression in cynomolgus monkeys by XPro9523 | Immune suppression in cynomolgus monkeys by XPro9523 Abstract Abstract The CTLA4-Ig fusion proteins abatacept and belatacept are clinically proven immunosuppressants used for rheumatoid arthritis and renal transplant, respectively. Given that both biologics are typically administered chronically by infusion, a need exi... |
PMC11676034 | core_pubmed_pmc | First Clinical Application of Aztreonam–Avibactam in Treating Carbapenem-Resistant Enterobacterales: Insights from Therapeutic Drug Monitoring and Pharmacokinetic Simulations | First Clinical Application of Aztreonam–Avibactam in Treating Carbapenem-Resistant Enterobacterales: Insights from Therapeutic Drug Monitoring and Pharmacokinetic Simulations Abstract Background : A novel fixed combination of aztreonam (ATM) and avibactam (AVI) offers promising potential to treat infections with carbap... |
PMC9653239 | core_pubmed_pmc | Assessing the relative importance of bacterial resistance, persistence and hyper-mutation for antibiotic treatment failure | Assessing the relative importance of bacterial resistance, persistence and hyper-mutation for antibiotic treatment failure Abstract Abstract To curb the rising threat of antimicrobial resistance, we need to understand the routes to antimicrobial treatment failure. Bacteria can survive treatment by using both genetic an... |
PMC7186811 | core_pubmed_pmc | Calculated initial parenteral treatment of bacterial infections: Pharmacokinetics and pharmacodynamics | Calculated initial parenteral treatment of bacterial infections: Pharmacokinetics and pharmacodynamics Abstract This is the third chapter of the guideline “Calculated initial parenteral treatment of bacterial infections in adults – update 2018” in the 2 nd updated version. The German guideline by the Paul-Ehrlich-Gesel... |
PMC3889826 | core_pubmed_pmc | Development of a Paediatric Population-Based Model of the Pharmacokinetics of Rivaroxaban | Development of a Paediatric Population-Based Model of the Pharmacokinetics of Rivaroxaban Abstract Abstract Background Venous thromboembolism has been increasingly recognised as a clinical problem in the paediatric population. Guideline recommendations for antithrombotic therapy in paediatric patients are based mainly ... |
PMC12117666 | core_pubmed_pmc | Integrating Pharmacokinetics and Quantitative Systems Pharmacology Approaches in Generative Drug Design | Integrating Pharmacokinetics and Quantitative Systems Pharmacology Approaches in Generative Drug Design Abstract Integrated understanding of pharmacokinetics (PK) and pharmacodynamics (PD) is a key aspect of successful drug discovery. Yet in generative computational drug design, the focus often lies on optimizing poten... |
PMC4561049 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of GSK961081 (Batefenterol), a Muscarinic Antagonist and β 2 -Agonist, in Moderate-to-Severe COPD Patients: Substudy of a Randomized Trial | Population Pharmacokinetics and Pharmacodynamics of GSK961081 (Batefenterol), a Muscarinic Antagonist and β 2 -Agonist, in Moderate-to-Severe COPD Patients: Substudy of a Randomized Trial Abstract GSK961081 (batefenterol) is a novel bifunctional molecule composed of a muscarinic antagonist and a β 2 ‐agonist. The aims ... |
PMC6617844 | core_pubmed_pmc | American Society for Clinical Pharmacology and Therapeutics 2019 Annual Meeting Pre‐Conferences | American Society for Clinical Pharmacology and Therapeutics 2019 Annual Meeting Pre‐Conferences Modeling PBPK Pre‐Conference The full‐day PBPK pre‐conference was cosponsored by the ASCPT and the US Food and Drug Administration (FDA) and cochaired by Liang Zhao, PhD, US FDA, and Ping Zhao, PhD, Bill & Melinda Gates Foun... |
PMC9166662 | core_pubmed_pmc | Biotransformation and transplacental transfer of the anti-viral remdesivir and predominant metabolite, GS-441524 in pregnant rats | Biotransformation and transplacental transfer of the anti-viral remdesivir and predominant metabolite, GS-441524 in pregnant rats Abstract Summary Background Remdesivir was the first prodrug approved to treat coronavirus disease 2019 (COVID-19) and has the potential to be used during pregnancy. However, it is not known... |
PMC12348896 | core_pubmed_pmc | Targeting Oxidative Stress in Acute Pancreatitis: A Critical Review of Antioxidant Strategies | Targeting Oxidative Stress in Acute Pancreatitis: A Critical Review of Antioxidant Strategies Abstract Acute pancreatitis (AP) is among the most frequent gastroenterology emergencies, with hospital admission rates on the rise in recent decades. However, a specific treatment for this condition is still lacking. Mitochon... |
PMC6017933 | core_pubmed_pmc | Development and Validation of a HPLC-ESI-MS/MS Method for Simultaneous Quantification of Fourteen Alkaloids in Mouse Plasma after Oral Administration of the Extract of Corydalis yanhusuo Tuber: Application to Pharmacokinetic Study | Development and Validation of a HPLC-ESI-MS/MS Method for Simultaneous Quantification of Fourteen Alkaloids in Mouse Plasma after Oral Administration of the Extract of Corydalis yanhusuo Tuber: Application to Pharmacokinetic Study Abstract The tuber of Corydalis yanhusuo is a famous traditional Chinese medicine and fou... |
PMC7984375 | core_pubmed_pmc | Safety, Tolerability, and Dose Proportionality of a Novel Transdermal Fentanyl Matrix Patch and Bioequivalence With a Matrix Fentanyl Patch: Two Phase 1 Single‐Center Open‐Label, Randomized Crossover Studies in Healthy Japanese Volunteers | Safety, Tolerability, and Dose Proportionality of a Novel Transdermal Fentanyl Matrix Patch and Bioequivalence With a Matrix Fentanyl Patch: Two Phase 1 Single‐Center Open‐Label, Randomized Crossover Studies in Healthy Japanese Volunteers Abstract Abstract Two open‐label, single‐dose, randomized crossover studies were ... |
PMC3043235 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic analysis of adjuvant pegylated interferon α-2b in patients with resected high-risk melanoma | Pharmacokinetic/pharmacodynamic analysis of adjuvant pegylated interferon α-2b in patients with resected high-risk melanoma Abstract Abstract Purpose High-dose pegylated interferon α-2b (peginterferon α-2b) significantly decreased disease recurrence in patients with resected stage III melanoma in a clinical study. We i... |
PMC11768278 | core_pubmed_pmc | Nose-to-Brain Delivery of Chitosan-Grafted Leciplexes for Promoting the Bioavailability and Antidepressant Efficacy of Mirtazapine: In Vitro Assessment and Animal Studies | Nose-to-Brain Delivery of Chitosan-Grafted Leciplexes for Promoting the Bioavailability and Antidepressant Efficacy of Mirtazapine: In Vitro Assessment and Animal Studies Abstract Abstract Background/Objectives : Mirtazapine (MRZ) is a psychotropic drug prescribed to manage serious sorts of depression. By virtue of its... |
PMC9756784 | core_pubmed_pmc | LC–MS/MS method for simultaneous quantification of ten antibiotics in human plasma for routine therapeutic drug monitoring | LC–MS/MS method for simultaneous quantification of ten antibiotics in human plasma for routine therapeutic drug monitoring Abstract Highlights • Simultaneous quantification of ten antimicrobials in human plasma by LC–MS/MS utilizing a SIL-IS for each analyte. • Therapeutic drug monitoring of antimicrobials in clinical ... |
PMC9305464 | core_pubmed_pmc | TSH receptor specific monoclonal autoantibody K1‐70 TM targeting of the TSH receptor in subjects with Graves' disease and Graves' orbitopathy—Results from a phase I clinical trial | TSH receptor specific monoclonal autoantibody K1‐70 TM targeting of the TSH receptor in subjects with Graves' disease and Graves' orbitopathy—Results from a phase I clinical trial Abstract Abstract Objectives In Graves' disease (GD), autoantibodies to the thyroid stimulating hormone receptor (TSHR) cause hyperthyroidis... |
PMC12602602 | core_pubmed_pmc | Eco Friendly and Budget Smart: An Economic and Environmental Evaluation of Alternative PD-1 and PD-L1 Inhibitor Dosing Regimens | Eco Friendly and Budget Smart: An Economic and Environmental Evaluation of Alternative PD-1 and PD-L1 Inhibitor Dosing Regimens Abstract Abstract Background Immune checkpoint inhibitors (ICIs) are clinically beneficial but associated with high costs that represent a growing challenge for healthcare budgets and may affe... |
PMC5340788 | core_pubmed_pmc | Predicting drug–drug interactions through drug structural similarities and interaction networks incorporating pharmacokinetics and pharmacodynamics knowledge | Predicting drug–drug interactions through drug structural similarities and interaction networks incorporating pharmacokinetics and pharmacodynamics knowledge Abstract Drug–drug interactions (DDIs) may lead to adverse effects and potentially result in drug withdrawal from the market. Predicting DDIs during drug developm... |
PMC10186381 | core_pubmed_pmc | Comparative Bioavailability Study of a Novel Multi-Day Patch Formulation of Rivastigmine (Twice Weekly) with Exelon ® Transdermal Patch (Daily)- A Randomized Clinical Trial | Comparative Bioavailability Study of a Novel Multi-Day Patch Formulation of Rivastigmine (Twice Weekly) with Exelon ® Transdermal Patch (Daily)- A Randomized Clinical Trial Abstract Background : Rivastigmine, a reversible AChEI for symptomatic treatment of mild to moderately severe Alzheimer’s dementia, is administered... |
PMC8659019 | core_pubmed_pmc | Evaluation of The Antioxidant, Antimicrobial, and Anticancer Activities of Dicliptera bupleuroides Isolated Compounds Using In Vitro and In Silico Studies | Evaluation of The Antioxidant, Antimicrobial, and Anticancer Activities of Dicliptera bupleuroides Isolated Compounds Using In Vitro and In Silico Studies Abstract Abstract Phytochemical investigation of chloroform fraction (DBC) and ethyl acetate fraction (DBE) of D. bupleuroides (Acanthaceae) resulted in the isolatio... |
PMC4870186 | core_pubmed_pmc | A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro | A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro Abstract Dovitinib (TKI258) is a small molecule multi-kinase inhibitor currently in clinical phase I/II/III development for the treatment of various types of cancers. This drug has a safe and effective ... |
PMC10712105 | core_pubmed_pmc | Single protein encapsulated SN38 for tumor-targeting treatment | Single protein encapsulated SN38 for tumor-targeting treatment Abstract Background The alkaloid camptothecin analog SN38 is a potent antineoplastic agent, but cannot be used directly for clinical application due to its poor water solubility. Currently, the prodrug approach on SN38 has resulted in 3 FDA-approved cancer ... |
PMC11520922 | core_pubmed_pmc | Improving the Thrombocytopenia Adverse Reaction of Belinostat Using Human Serum Albumin Nanoparticles | Improving the Thrombocytopenia Adverse Reaction of Belinostat Using Human Serum Albumin Nanoparticles Abstract Abstract Background Belinostat, a histone deacetylase inhibitor used for hematological cancer treatments, however, it caused thrombocytopenia, poor solubility, and rapid clearance. To mitigate these issues, hu... |
PMC12311710 | core_pubmed_pmc | Nutritional Supplementation Benefits in Caenorhabditis elegans under Developmental Disruption and Stress Conditions | Nutritional Supplementation Benefits in Caenorhabditis elegans under Developmental Disruption and Stress Conditions Abstract Abstract Autism spectrum disorder (ASD) is a developmental and neurological condition that impacts an individual’s behavior, communication, social interaction, and learning abilities. This diseas... |
PMC5442600 | core_pubmed_pmc | Pharmacokinetics of Recombinant Human Soluble Thrombomodulin in Disseminated Intravascular Coagulation Patients with Acute Renal Dysfunction | Pharmacokinetics of Recombinant Human Soluble Thrombomodulin in Disseminated Intravascular Coagulation Patients with Acute Renal Dysfunction Abstract Summary Recombinant human soluble thrombomodulin (ART-123) is a novel anticoagulant for patients with disseminated intravascular coagulation (DIC). It is widely used in c... |
PMC10022826 | core_pubmed_pmc | SeDeM expert system with I-optimal mixture design for oral multiparticulate drug delivery: An encapsulated floating minitablets of loxoprofen Na and its in silico physiologically based pharmacokinetic modeling | SeDeM expert system with I-optimal mixture design for oral multiparticulate drug delivery: An encapsulated floating minitablets of loxoprofen Na and its in silico physiologically based pharmacokinetic modeling Abstract Abstract Introduction: A SeDeM expert tool-driven I-optimal mixture design has been used to develop a... |
PMC12756207 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Viral Pharmacodynamics of the Monoclonal Antibody Sotrovimab Administered via Intramuscular Injection in Participants with Early, Mild-to-Moderate COVID-19: A Randomized Clinical Trial | Safety, Tolerability, Pharmacokinetics, and Viral Pharmacodynamics of the Monoclonal Antibody Sotrovimab Administered via Intramuscular Injection in Participants with Early, Mild-to-Moderate COVID-19: A Randomized Clinical Trial Abstract Abstract Background and Objectives New coronavirus disease 2019 (COVID-19) therape... |
PMC4977083 | core_pubmed_pmc | Preparation of novel biodegradable ropivacaine microspheres and evaluation of their efficacy in sciatic nerve block in mice | Preparation of novel biodegradable ropivacaine microspheres and evaluation of their efficacy in sciatic nerve block in mice Abstract In this study, ropivacaine chitosan-loaded microspheres for subcutaneous administration were developed. The systems were characterized in terms of surface morphology, particle size, encap... |
PMC4407821 | core_pubmed_pmc | Pharmacokinetics of quercetin-loaded nanodroplets with ultrasound activation and their use for bioimaging | Pharmacokinetics of quercetin-loaded nanodroplets with ultrasound activation and their use for bioimaging Abstract Bubble formulations have both diagnostic and therapeutic applications. However, research on nanobubbles/nanodroplets remains in the initial stages. In this study, a nanodroplet formulation was prepared and... |
PMC8453264 | core_pubmed_pmc | Comparative Effects of Metamizole (Dipyrone) and Naproxen on Renal Function and Prostacyclin Synthesis in Salt-Depleted Healthy Subjects - A Randomized Controlled Parallel Group Study | Comparative Effects of Metamizole (Dipyrone) and Naproxen on Renal Function and Prostacyclin Synthesis in Salt-Depleted Healthy Subjects - A Randomized Controlled Parallel Group Study Abstract Abstract Aim: The objective was to investigate the effect of metamizole on renal function in healthy, salt-depleted volunteers.... |
PMC8939912 | core_pubmed_pmc | Predicting Individual Changes in Terminal Half-Life After Switching to Extended Half-Life Concentrates in Patients With Severe Hemophilia | Predicting Individual Changes in Terminal Half-Life After Switching to Extended Half-Life Concentrates in Patients With Severe Hemophilia Abstract Abstract Predicting individual effects of switching from standard half-life (SHL) to extended half-life (EHL) FVIII/FIX concentrates is pivotal in clinical care, but large-s... |
PMC11526018 | core_pubmed_pmc | Risk-stratified treatment for drug-susceptible pulmonary tuberculosis | Risk-stratified treatment for drug-susceptible pulmonary tuberculosis Abstract The Phase 3 randomized controlled trial, TBTC Study 31/ACTG A5349 ( NCT02410772 ) demonstrated that a 4-month rifapentine-moxifloxacin regimen for drug-susceptible pulmonary tuberculosis was safe and effective. The primary efficacy outcome w... |
PMC10098929 | core_pubmed_pmc | Removing race and body surface area indexation for estimated kidney function based drug dosing: Aminoglycosides as justification of these principles | Removing race and body surface area indexation for estimated kidney function based drug dosing: Aminoglycosides as justification of these principles Abstract Abstract Study Objective The use of race in medicine can contribute to health inequity. Updated equations for estimated glomerular filtration rate (eGFR) without ... |
PMC12761352 | core_pubmed_pmc | Enhanced Tear Film Concentrations of Cefazolin and Chloramphenicol Using Cross‐Linked Hyaluronic Acid in Canine Eyes | Enhanced Tear Film Concentrations of Cefazolin and Chloramphenicol Using Cross‐Linked Hyaluronic Acid in Canine Eyes Abstract ABSTRACT Objective To evaluate the impact of two excipients, 1.4% polyvinyl alcohol (PVA) and 0.75% cross‐linked hyaluronic acid (XHA), on tear film concentrations of cefazolin and chloramphenic... |
PMC7547810 | core_pubmed_pmc | Effects of Fluorescent Diamond Particles FDP-NV-800nm on Essential Biochemical Functions of Primary Human Umbilical Vein Cells and Human Hepatic Cell Line, HepG-2 in vitro (Part VI): Acute Biocompatibility Studies | Effects of Fluorescent Diamond Particles FDP-NV-800nm on Essential Biochemical Functions of Primary Human Umbilical Vein Cells and Human Hepatic Cell Line, HepG-2 in vitro (Part VI): Acute Biocompatibility Studies Abstract Background Recently, we reported the safety and biocompatibility of fluorescent diamond particles... |
PMC11990745 | core_pubmed_pmc | Sirtuins and Resveratrol in Cardiorenal Diseases: A Narrative Review of Mechanisms and Therapeutic Potential | Sirtuins and Resveratrol in Cardiorenal Diseases: A Narrative Review of Mechanisms and Therapeutic Potential Abstract Abstract Aging is a very complex process, and it has been linked with Sirtuins. Sirtuin enzymes are a family of deacetylases that are related to caloric restriction and aging by modulating energy metabo... |
PMC12823295 | core_pubmed_pmc | Managing Drug–Drug Interactions Involving the Non‐Prescription Opioid Loperamide Through Physiologically Based Pharmacokinetic Modeling | Managing Drug–Drug Interactions Involving the Non‐Prescription Opioid Loperamide Through Physiologically Based Pharmacokinetic Modeling Abstract ABSTRACT Loperamide is a widely used nonprescription peripherally acting opioid indicated for diarrhea. Loperamide undergoes extensive first‐pass metabolism, primarily by cyto... |
PMC11718471 | core_pubmed_pmc | Impact of setting distinct target blood glucose levels on endogenous insulin suppression and pharmacodynamics of insulin preparations | Impact of setting distinct target blood glucose levels on endogenous insulin suppression and pharmacodynamics of insulin preparations Abstract BACKGROUND Insulin therapy plays a crucial role in managing diabetes. Regulatory guidelines mandate assessing the pharmacokinetics (PK) and pharmacodynamics (PD) of new insulin ... |
PMC12854426 | core_pubmed_pmc | Population pharmacokinetics model of pyrazinamide to optimize tuberculosis treatment: An interethnic cohort study of diabetes mellitus effect on drug exposure | Population pharmacokinetics model of pyrazinamide to optimize tuberculosis treatment: An interethnic cohort study of diabetes mellitus effect on drug exposure Abstract Abstract Diabetes mellitus (DM), a common comorbidity in tuberculosis (TB) patients, can alter the pharmacokinetics (PK) of TB drugs. Additionally, clin... |
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