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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...