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PMC9386120
core_pubmed_pmc
The effect of phenobarbital treatment on behavioral comorbidities and on the composition and function of the fecal microbiome in dogs with idiopathic epilepsy
The effect of phenobarbital treatment on behavioral comorbidities and on the composition and function of the fecal microbiome in dogs with idiopathic epilepsy Abstract Phenobarbital (PB) is one of the most important antiseizure drugs (ASDs) to treat canine idiopathic epilepsy (IE). The effect of PB on the taxonomic cha...
PMC12853878
core_pubmed_pmc
Do the redefined EUCAST susceptibility categories warrant adjustment of paediatric antibiotic dosages? Pragmatic physiologically based pharmacokinetic modelling of four commonly used agents
Do the redefined EUCAST susceptibility categories warrant adjustment of paediatric antibiotic dosages? Pragmatic physiologically based pharmacokinetic modelling of four commonly used agents Abstract Abstract Background and objective With the redefinition of the EUCAST ‘I’ susceptibility category, from ‘intermediate’ to...
PMC11561580
core_pubmed_pmc
Optimizing Lumefantrine Dosing for Young Children in High-Malaria-Burden Countries Using Pharmacokinetic-Pharmacodynamic Simulations
Optimizing Lumefantrine Dosing for Young Children in High-Malaria-Burden Countries Using Pharmacokinetic-Pharmacodynamic Simulations Abstract Abstract Background Artemether-lumefantrine is the most widely used treatment for uncomplicated malaria and it is dosed based on weight bands according to World Health Organizati...
PMC9715596
core_pubmed_pmc
Buprenorphine exposure levels to optimize treatment outcomes in opioid use disorder
Buprenorphine exposure levels to optimize treatment outcomes in opioid use disorder Abstract Abstract The severity of the ongoing opioid crisis, recently exacerbated by the COVID-19 pandemic, emphasizes the importance for individuals suffering from opioid use disorder (OUD) to have access to and receive efficacious, ev...
PMC6598480
core_pubmed_pmc
Effects of puerarin on the pharmacokinetics of triptolide in rats
Effects of puerarin on the pharmacokinetics of triptolide in rats Abstract Abstract Context: Puerarin and triptolide are sometimes used together for the treatment of disease in Chinese clinics; however, the drug–drug interaction between puerarin and triptolide is still unknown. Objective: This study investigates the ef...
PMC9257044
core_pubmed_pmc
Therapeutic Drug Monitoring of Ceftazidime-Avibactam Concentrations in Carbapenem-Resistant K. pneumoniae- Infected Patients With Different Kidney Statuses
Therapeutic Drug Monitoring of Ceftazidime-Avibactam Concentrations in Carbapenem-Resistant K. pneumoniae- Infected Patients With Different Kidney Statuses Abstract Aims: Carbapenem-resistant K. pneumoniae (CRKP) is the most common carbapenem-resistant Enterobacteriaceae with high mortality. Ceftazidime-avibactam (CAZ-...
PMC8241022
core_pubmed_pmc
Controllable continuous sub-tenon drug delivery of dexamethasone disodium phosphate to ocular posterior segment in rabbit
Controllable continuous sub-tenon drug delivery of dexamethasone disodium phosphate to ocular posterior segment in rabbit Abstract Abstract Corticosteroids have been used for treatment of posterior segment eye diseases, but the delivery of drug to the posterior segments is still a problem to resolve. In our study, we e...
PMC12780488
core_pubmed_pmc
An Overview of Liquid Chromatography–Mass Spectrometry (LC–MS) Methods for the Quantification of Antibody‐Drug Conjugates
An Overview of Liquid Chromatography–Mass Spectrometry (LC–MS) Methods for the Quantification of Antibody‐Drug Conjugates Abstract ABSTRACT Antibody‐drug conjugates (ADCs) are innovative drugs composed of cytotoxic molecules (payload) linked to antibodies, that selectively target and kill cancer cells upon internalizat...
PMC6154486
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery
Pharmacokinetic and pharmacodynamic studies of etodolac loaded vesicular gels on rats by transdermal delivery Abstract Background The present study includes the development of liposomal and ethosomal gels for transdermal delivery to overcome the side effects associated with oral route. Methods The liposomes and ethosom...
PMC12084224
core_pubmed_pmc
Artificial intelligence generated 3D body composition predicts dose modifications in patients undergoing neoadjuvant chemotherapy for rectal cancer
Artificial intelligence generated 3D body composition predicts dose modifications in patients undergoing neoadjuvant chemotherapy for rectal cancer Abstract Purpose Chemotherapy administration is a balancing act between giving enough to achieve the desired tumour response while limiting adverse effects. Chemotherapy do...
PMC5582369
core_pubmed_pmc
Tenapanor administration and the activity of the H + ‐coupled transporter PepT1 in healthy volunteers
Tenapanor administration and the activity of the H + ‐coupled transporter PepT1 in healthy volunteers Abstract Aim Tenapanor (RDX5791/AZD1722), an inhibitor of gastrointestinal Na + /H + exchanger NHE3, is being evaluated for the treatment of patients with constipation‐predominant irritable bowel syndrome and the treat...
PMC12943722
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modelling of Hydroxyurea in Patients with Sickle Cell Disease: A Special Focus on Lactating Women and Breastfed Infants to Inform Safe Dosing and Breastfeeding Strategies
Physiologically Based Pharmacokinetic Modelling of Hydroxyurea in Patients with Sickle Cell Disease: A Special Focus on Lactating Women and Breastfed Infants to Inform Safe Dosing and Breastfeeding Strategies Abstract Abstract Background/Objectives : Hydroxyurea is currently the standard disease-modifying therapy for r...
PMC10786959
core_pubmed_pmc
A Comprehensive Review of the Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Nirmatrelvir/Ritonavir
A Comprehensive Review of the Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Nirmatrelvir/Ritonavir Abstract Abstract Nirmatrelvir is a potent and selective inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease that is used as an oral antiviral coronavirus di...
PMC12630006
core_pubmed_pmc
Influence of Potential Pharmacodynamic Drug Interactions in Pharmacotherapy of Coronary Heart Disease with Comorbid Conditions on Treatment Adherence: A Cross-Sectional Study of a Ukrainian Patient Cohort
Influence of Potential Pharmacodynamic Drug Interactions in Pharmacotherapy of Coronary Heart Disease with Comorbid Conditions on Treatment Adherence: A Cross-Sectional Study of a Ukrainian Patient Cohort Abstract Purpose Coronary heart disease (CHD) is accompanied by a high level of comorbidity, which necessitates the...
PMC12656350
core_pubmed_pmc
Arzanol: A Review of Chemical Properties and Biological Activities
Arzanol: A Review of Chemical Properties and Biological Activities Abstract Abstract Arzanol, a prenylated phloroglucinol–α-pyrone heterodimer, displays a broad range of pharmacological properties. This review compiles findings from 2007 to 2025 on its chemistry, conformational behavior, bioactivities, molecular target...
PMC4461093
core_pubmed_pmc
Profile of ceftolozane/tazobactam and its potential in the treatment of complicated intra-abdominal infections
Profile of ceftolozane/tazobactam and its potential in the treatment of complicated intra-abdominal infections Abstract Drug-resistant pathogens have gained a foothold especially in the most vulnerable patient populations, hospitalized and immunocompromised individuals. Furthermore, extended-spectrum β-lactamase and ca...
PMC9011188
core_pubmed_pmc
Ivermectin Plasma Concentration in Iberian Ibex ( Capra pyrenaica ) Following Oral Administration: A Pilot Study
Ivermectin Plasma Concentration in Iberian Ibex ( Capra pyrenaica ) Following Oral Administration: A Pilot Study Abstract Sarcoptic mange is considered the main driver of demographic declines occurred in the last decades in Iberian ibex ( Capra pyrenaica ) populations. Mass treatment campaigns by administration of in-f...
PMC6681021
core_pubmed_pmc
Dose-Dependent Pharmacokinetics of Tofacitinib in Rats: Influence of Hepatic and Intestinal First-Pass Metabolism
Dose-Dependent Pharmacokinetics of Tofacitinib in Rats: Influence of Hepatic and Intestinal First-Pass Metabolism Abstract This study investigated the pharmacokinetics of tofacitinib in rats and the effects of first-pass metabolism on tofacitinib pharmacokinetics. Intravenous administration of 5, 10, 20, and 50 mg/kg t...
PMC12645405
core_pubmed_pmc
Dosing Optimization of Lamotrigine in Peripregnancy Epilepsy Through PopPK Modelling and Simulation
Dosing Optimization of Lamotrigine in Peripregnancy Epilepsy Through PopPK Modelling and Simulation Abstract Purpose Lamotrigine demonstrates substantial interindividual pharmacokinetic variability during pregnancy, though the underlying mechanisms remain incompletely understood. The study aimed to develop a population...
PMC12358299
core_pubmed_pmc
Pirana and Integrated PMX Tools, a Workbench for NONMEM, NLME, pyDarwin, and RsNLME
Pirana and Integrated PMX Tools, a Workbench for NONMEM, NLME, pyDarwin, and RsNLME Abstract ABSTRACT Keizer initially described Pirana as a workbench designed to streamline management of NONMEM modeling, visualization, and analysis. Initial versions of Pirana integrated tools included NONMEM and PSN. As new tools have...
PMC3834941
core_pubmed_pmc
Pharmacokinetic Evaluation of a DSPE-PEG 2000 Micellar Formulation of Ridaforolimus in Rat
Pharmacokinetic Evaluation of a DSPE-PEG 2000 Micellar Formulation of Ridaforolimus in Rat Abstract The rapamycin analog, ridaforolimus, has demonstrated potent anti-proliferative effects in cancer treatment, and it currently is being evaluated in a range of clinical cancer studies. Ridaforolimus is an extremely lipoph...
PMC4440724
core_pubmed_pmc
Robust and Reproducible Quantification of the Extent of Chest Radiographic Abnormalities (And It’s Free!)
Robust and Reproducible Quantification of the Extent of Chest Radiographic Abnormalities (And It’s Free!) Abstract Abstract Rationale Objective, reproducible quantification of the extent of abnormalities seen on a chest radiograph would improve the user-friendliness of a previously proposed severity scoring system for ...
PMC5207541
core_pubmed_pmc
VKORC1 and CYP2C9 polymorphisms related to adverse events in case-control cohort of anticoagulated patients
VKORC1 and CYP2C9 polymorphisms related to adverse events in case-control cohort of anticoagulated patients Abstract Abstract Vitamin K antagonists (VKAs) are highly effective but have a narrow therapeutic index and require routine monitoring of the INR. The primary aim of pharmacogenetics (PGx) is to optimize patient ...
PMC11897418
core_pubmed_pmc
The Single‐Dose Pharmacokinetics of a Compounded Levetiracetam Formulation and Bioequivalence to a Commercial Formulation in Healthy Dogs
The Single‐Dose Pharmacokinetics of a Compounded Levetiracetam Formulation and Bioequivalence to a Commercial Formulation in Healthy Dogs Abstract ABSTRACT Levetiracetam (LEV) is an anti‐epileptic drug used extra‐label in dogs. Commercially available extended‐release formulations (LEV‐ER), administered twice daily, can...
PMC9010270
core_pubmed_pmc
Imeglimin population pharmacokinetics and dose adjustment predictions for renal impairment in Japanese and Western patients with type 2 diabetes
Imeglimin population pharmacokinetics and dose adjustment predictions for renal impairment in Japanese and Western patients with type 2 diabetes Abstract Abstract Imeglimin is an orally administered first‐in‐class drug to treat type 2 diabetes mellitus (T2DM) and is mainly excreted unchanged by the kidneys. The present...
PMC10235566
core_pubmed_pmc
Tolerability and pharmacokinetics of intravenous allopregnanolone with and without midazolam pretreatment in two healthy dogs
Tolerability and pharmacokinetics of intravenous allopregnanolone with and without midazolam pretreatment in two healthy dogs Abstract Abstract The neurosteroid allopregnanolone (ALLO) is under investigation as a treatment for benzodiazepine‐refractory status epilepticus (SE). Here, we assess the cardiopulmonary safety...
PMC5056674
core_pubmed_pmc
Application of Physiologically Based Absorption Modeling to Characterize the Pharmacokinetic Profiles of Oral Extended Release Methylphenidate Products in Adults
Application of Physiologically Based Absorption Modeling to Characterize the Pharmacokinetic Profiles of Oral Extended Release Methylphenidate Products in Adults Abstract A previously presented physiologically-based pharmacokinetic model for immediate release (IR) methylphenidate (MPH) was extended to characterize the ...
PMC7877841
core_pubmed_pmc
Quantitative Clinical Pharmacology of T‐Cell Engaging Bispecifics: Current Perspectives and Opportunities
Quantitative Clinical Pharmacology of T‐Cell Engaging Bispecifics: Current Perspectives and Opportunities Abstract T‐cell directing/engaging bispecifics (TDBs) enable a powerful mode of action by activating T‐cells through the creation of artificial immune synapses. Their pharmacological response involves the dynamic i...
PMC5209692
core_pubmed_pmc
A four-compartment PBPK heart model accounting for cardiac metabolism - model development and application
A four-compartment PBPK heart model accounting for cardiac metabolism - model development and application Abstract Abstract In the field of cardiac drug efficacy and safety assessment, information on drug concentration in heart tissue is desirable. Because measuring drug concentrations in human cardiac tissue is challe...
PMC12201673
core_pubmed_pmc
Biomarkers of mRNA vaccine efficacy derived from mechanistic modeling of tumor-immune interactions
Biomarkers of mRNA vaccine efficacy derived from mechanistic modeling of tumor-immune interactions Abstract The success of mRNA vaccines against infectious diseases such as COVID-19 has opened new avenues for their application in oncology. In cancer immunotherapy, mRNA vaccines—typically encapsulated in lipid nanoparti...
PMC6373417
core_pubmed_pmc
Development and In Vivo Evaluation of Ziyuglycoside I–Loaded Self-Microemulsifying Formulation for Activity of Increasing Leukocyte
Development and In Vivo Evaluation of Ziyuglycoside I–Loaded Self-Microemulsifying Formulation for Activity of Increasing Leukocyte Abstract Ziyuglycoside I (ZgI), a major effective ingredient of Sanguisorba officinalis L, has shown good activity in increasing leukocyte of myelosuppression mice. However, oral ZgI thera...
PMC8560717
core_pubmed_pmc
Drug discovery and development scheme for liver-targeting bridged nucleic acid antisense oligonucleotides
Drug discovery and development scheme for liver-targeting bridged nucleic acid antisense oligonucleotides Abstract Antisense oligonucleotides (ASOs) containing bridged nucleic acids (BNAs) have been proven to be very powerful. However, ensuring a reliable discovery and translational development scheme for this class of...
PMC10010323
core_pubmed_pmc
TAK-676: A Novel Stimulator of Interferon Genes (STING) Agonist Promoting Durable IFN-dependent Antitumor Immunity in Preclinical Studies
TAK-676: A Novel Stimulator of Interferon Genes (STING) Agonist Promoting Durable IFN-dependent Antitumor Immunity in Preclinical Studies Abstract Oncology therapies targeting the immune system have improved patient outcomes across a wide range of tumor types, but resistance due to an inadequate T-cell response in a su...
PMC8449800
core_pubmed_pmc
A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug–Drug Interactions With Antiretroviral and Antituberculosis Treatment
A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug–Drug Interactions With Antiretroviral and Antituberculosis Treatment Abstract Depot medroxyprogesterone acetate is an injectable hormonal contraceptive, widely used by women of childbearing potential living with HIV and/or tuberculos...
PMC12812941
core_pubmed_pmc
Enhanced CYP2C19-mediated drug-drug interaction risk with escitalopram in geriatric populations
Enhanced CYP2C19-mediated drug-drug interaction risk with escitalopram in geriatric populations Abstract Introduction Escitalopram (S-CIT) is commonly prescribed for depression and anxiety in older patients. Previous research has reported that the effect of CYP2C19 polymorphism on S-CIT pharmacokinetics is more pronoun...
PMC5856878
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of the Epidermal Growth Factor Receptor Inhibitor Panitumumab in the Treatment of Colorectal Cancer
Clinical Pharmacokinetics and Pharmacodynamics of the Epidermal Growth Factor Receptor Inhibitor Panitumumab in the Treatment of Colorectal Cancer Abstract Despite progress in the treatment of metastatic colorectal cancer (mCRC) in the last 15 years, it is still a condition with a relatively low 5-year survival rate. P...
PMC11458338
core_pubmed_pmc
Individual pharmacokinetic parameter estimation of gentamicin in an obese hemodialysis patient using non-linear mixed effect model
Individual pharmacokinetic parameter estimation of gentamicin in an obese hemodialysis patient using non-linear mixed effect model Abstract This study aimed to estimate individual pharmacokinetic (PK) parameters in an obese hemodialysis (HD) patient receiving gentamicin and to assess the impact of obesity on gentamicin...
PMC7132596
core_pubmed_pmc
UPLC–MS/MS assay for quantification of an inhibitor of kinases (Foretinib) in plasma: Application to a pharmacokinetic study in rats
UPLC–MS/MS assay for quantification of an inhibitor of kinases (Foretinib) in plasma: Application to a pharmacokinetic study in rats Abstract Abstract Foretinib, an oral multikinase inhibitor, is known to have anti-tumor effects against cancers. The doses and the levels of foretinib vary based on the type of cancer to ...
PMC11434788
core_pubmed_pmc
Development, Stability, and In Vitro/In Vivo Studies of Volatile Oil Pickering Emulsion Stabilized by Modified Amber
Development, Stability, and In Vitro/In Vivo Studies of Volatile Oil Pickering Emulsion Stabilized by Modified Amber Abstract Volatile oil stabilization strategies based on encapsulation with a large number of excipients limit further applications. The primary objective of this study is to improve the stability of vola...
PMC11098163
core_pubmed_pmc
Population longitudinal analysis of Gait Profile Score and North Star Ambulatory Assessment in children with Duchenne muscular dystrophy
Population longitudinal analysis of Gait Profile Score and North Star Ambulatory Assessment in children with Duchenne muscular dystrophy Abstract Abstract Duchenne muscular dystrophy (DMD) is a rare X‐linked recessive disorder characterized by loss‐of‐function mutations in the gene encoding dystrophin. These mutations ...
PMC5591805
core_pubmed_pmc
Population Pharmacokinetics of Cladribine in Patients with Multiple Sclerosis
Population Pharmacokinetics of Cladribine in Patients with Multiple Sclerosis Abstract Purpose The aims of this study were to characterize the concentration–time course of cladribine (CdA) and its main metabolite 2-chloroadenine (CAde), estimate interindividual variability in pharmacokinetics (PK), and identify covaria...
PMC11504871
core_pubmed_pmc
Target Attainment and Population Pharmacokinetics of Cefazolin in Patients with Invasive Staphylococcus aureus Infections: A Prospective Cohort Study
Target Attainment and Population Pharmacokinetics of Cefazolin in Patients with Invasive Staphylococcus aureus Infections: A Prospective Cohort Study Abstract This study aimed to determine cefazolin target attainment in patients with invasive Staphylococcus aureus ( S. aureus ) infections and to develop a population ph...
PMC11502491
core_pubmed_pmc
Minimum effective dose of clemastine in a mouse model of preterm white matter injury
Minimum effective dose of clemastine in a mouse model of preterm white matter injury Abstract Background Preterm white matter injury (PWMI) is the most common cause of brain injury in premature neonates. PWMI involves a differentiation arrest of oligodendrocytes, the myelinating cells of the central nervous system. Cle...
PMC10333628
core_pubmed_pmc
Idiopathic pulmonary fibrosis therapy development: a clinical pharmacology perspective
Idiopathic pulmonary fibrosis therapy development: a clinical pharmacology perspective Abstract Abstract Drug development for idiopathic pulmonary fibrosis (IPF) has been challenging due to poorly understood disease etiology, unpredictable disease progression, highly heterogeneous patient populations, and a lack of rob...
PMC10222093
core_pubmed_pmc
Model-Based Analysis of In Vivo Release Data of Levonorgestrel Implants: Projecting Long-Term Systemic Exposure
Model-Based Analysis of In Vivo Release Data of Levonorgestrel Implants: Projecting Long-Term Systemic Exposure Abstract Abstract Levonorgestrel (LNG) is a progestin used in many contraceptive formulations, including subcutaneous implants. There is an unmet need for developing long-acting formulations for LNG. To devel...
PMC7187405
core_pubmed_pmc
The Pharmacokinetics and Relative Bioavailability of Mepolizumab 100 mg Liquid Formulation Administered Subcutaneously to Healthy Participants: A Randomized Trial
The Pharmacokinetics and Relative Bioavailability of Mepolizumab 100 mg Liquid Formulation Administered Subcutaneously to Healthy Participants: A Randomized Trial Abstract Abstract This study compared the pharmacokinetic (PK) profile of a new liquid formulation of mepolizumab with the established lyophilized formulatio...
PMC7983940
core_pubmed_pmc
Quantitative Systems Pharmacology Approaches for Immuno‐Oncology: Adding Virtual Patients to the Development Paradigm
Quantitative Systems Pharmacology Approaches for Immuno‐Oncology: Adding Virtual Patients to the Development Paradigm Abstract Drug development in oncology commonly exploits the tools of molecular biology to gain therapeutic benefit through reprograming of cellular responses. In immuno‐oncology (IO) the aim is to direc...
PMC8184152
core_pubmed_pmc
Nemiralisib in Patients with an Acute Exacerbation of COPD: Placebo-Controlled, Dose-Ranging Study
Nemiralisib in Patients with an Acute Exacerbation of COPD: Placebo-Controlled, Dose-Ranging Study Abstract Abstract Background Management of acute exacerbations of chronic obstructive pulmonary disease (COPD) is sometimes inadequate leading to either prolonged duration and/or an increased risk of recurrent exacerbatio...
PMC6166769
core_pubmed_pmc
Mechanisms and the clinical relevance of complex drug–drug interactions
Mechanisms and the clinical relevance of complex drug–drug interactions Abstract As a result of an increasing aging population, the number of individuals taking multiple medications simultaneously has grown considerably. For these individuals, taking multiple medications has increased the risk of undesirable drug–drug ...
PMC6067669
core_pubmed_pmc
Plasma concentrations of fenbendazole (FBZ) and oxfendazole in alpacas ( Lama pacos ) after single intravenous and oral dosing of FBZ
Plasma concentrations of fenbendazole (FBZ) and oxfendazole in alpacas ( Lama pacos ) after single intravenous and oral dosing of FBZ Abstract The objective of this study was to determine plasma pharmacokinetics and bioavailability of fenbendazole (FBZ) and oxfendazole (OFZ) after intravenous (iv) and oral administrati...
PMC6264278
core_pubmed_pmc
Corydaline Inhibits Multiple Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes
Corydaline Inhibits Multiple Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes Abstract Abstract Corydaline is a bioactive alkaloid with various antiacetylcholinesterase, antiallergic, and antinociceptive activities found in the medicinal herb Corydalis Tubers. The inhibitory p...
PMC12461970
core_pubmed_pmc
Enoxolone pharmacokinetics, tissue distribution, and residue depletion in largemouth bass ( Micropterus salmoides )
Enoxolone pharmacokinetics, tissue distribution, and residue depletion in largemouth bass ( Micropterus salmoides ) Abstract Enoxolone, a hydrolyzed component of Chinese herbal medicine, has shown efficacy against Flavobacterium columnare in largemouth bass ( Micropterus salmoides ). However, its pharmacokinetics and m...
PMC10187109
core_pubmed_pmc
Izokibep: Preclinical development and first-in-human study of a novel IL-17A neutralizing Affibody molecule in patients with plaque psoriasis
Izokibep: Preclinical development and first-in-human study of a novel IL-17A neutralizing Affibody molecule in patients with plaque psoriasis Abstract ABSTRACT Psoriasis, an immune-mediated inflammatory disease, affects nearly 125 million people globally. The interleukin (IL)-17A homodimer is a key driver of psoriasis ...
PMC10144056
core_pubmed_pmc
Application of Computing as a High-Practicability and -Efficiency Auxiliary Tool in Nanodrugs Discovery
Application of Computing as a High-Practicability and -Efficiency Auxiliary Tool in Nanodrugs Discovery Abstract Research and development (R&D) of nanodrugs is a long, complex and uncertain process. Since the 1960s, computing has been used as an auxiliary tool in the field of drug discovery. Many cases have proven the ...
PMC11962430
core_pubmed_pmc
Impact of CYP3A4 and ABCB1 genetic variants on tacrolimus dosing in Greek kidney transplant recipients
Impact of CYP3A4 and ABCB1 genetic variants on tacrolimus dosing in Greek kidney transplant recipients Abstract Background Tacrolimus, an approved first-line calcineurin inhibitor, is widely prescribed in organ transplantation to prevent allograft rejection. Its narrow therapeutic index requires precise management to a...
PMC3494424
core_pubmed_pmc
Phase I study of axitinib combined with paclitaxel, docetaxel or capecitabine in patients with advanced solid tumours
Phase I study of axitinib combined with paclitaxel, docetaxel or capecitabine in patients with advanced solid tumours Abstract Background: Axitinib, a potent and selective second-generation inhibitor of vascular endothelial growth factor receptors, enhanced the efficacy of chemotherapy in human xenograft tumour models....
PMC2875439
core_pubmed_pmc
Oral Insulin: A Comparison With Subcutaneous Regular Human Insulin in Patients With Type 2 Diabetes
Oral Insulin: A Comparison With Subcutaneous Regular Human Insulin in Patients With Type 2 Diabetes Abstract Abstract OBJECTIVE To determine the pharmacokinetic and pharmacodynamic properties of an oral insulin (OI) formulation compared with subcutaneously injected regular human insulin (RHI). RESEARCH DESIGN AND METHO...
PMC11179697
core_pubmed_pmc
Comparison of dose selection based on target engagement versus inhibition of receptor–ligand interaction for checkpoint inhibitors
Comparison of dose selection based on target engagement versus inhibition of receptor–ligand interaction for checkpoint inhibitors Abstract Abstract Immune checkpoint inhibitors block the interaction between a receptor on one cell and its ligand on another cell, thus preventing the transduction of an immunosuppressive ...
PMC10820138
core_pubmed_pmc
Drug Exposure and Susceptibility of Pyrazinamide Correlate with Treatment Response in Pyrazinamide-Susceptible Patients with Multidrug-Resistant Tuberculosis
Drug Exposure and Susceptibility of Pyrazinamide Correlate with Treatment Response in Pyrazinamide-Susceptible Patients with Multidrug-Resistant Tuberculosis Abstract Abstract Exploring the influence of pyrazinamide exposure and susceptibility on treatment response is crucial for optimizing the management of multidrug-...
PMC7518978
core_pubmed_pmc
Engineered tissues and strategies to overcome challenges in drug development
Engineered tissues and strategies to overcome challenges in drug development Abstract Abstract Current preclinical studies in drug development utilize high-throughput in vitro screens to identify drug leads, followed by both in vitro and in vivo models to predict lead candidates' pharmacokinetic and pharmacodynamic pro...
PMC4070457
core_pubmed_pmc
Determination of Oral Bioavailability of Fusaric Acid in Male Sprague-Dawley Rats
Determination of Oral Bioavailability of Fusaric Acid in Male Sprague-Dawley Rats Abstract Head and neck squamous cell cancer accounts for 3 % of new cancer cases and 2 % of cancer mortality annually in the United States. Current treatment options for most head and neck cancers continue to be surgical excision with or ...
PMC12706424
core_pubmed_pmc
A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe
A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe Abstract ABSTRACT Efavirenz induces and inhibits multiple drug‐metabolizing enzymes, contributing to significant drug–drug interactions. This study quantified the impact of mult...
PMC5012553
core_pubmed_pmc
Biodistribution and Pharmacokinetics Study of siRNA-loaded Anti-NTSR1-mAb-functionalized Novel Hybrid Nanoparticles in a Metastatic Orthotopic Murine Lung Cancer Model
Biodistribution and Pharmacokinetics Study of siRNA-loaded Anti-NTSR1-mAb-functionalized Novel Hybrid Nanoparticles in a Metastatic Orthotopic Murine Lung Cancer Model Abstract Abstract Small interfering RNA (siRNA) is effective in silencing critical molecular pathways in cancer. The use of this tool as a treatment mod...
PMC11448508
core_pubmed_pmc
Therapeutic antibodies in oncology: an immunopharmacological overview
Therapeutic antibodies in oncology: an immunopharmacological overview Abstract Abstract The biotechnological development of monoclonal antibodies and their immunotherapeutic use in oncology have grown exponentially in the last decade, becoming the first-line therapy for some types of cancer. Their mechanism of action i...
PMC11463156
core_pubmed_pmc
Ethnic sensitivity analyses of pharmacokinetics, efficacy and safety in polycythemia vera treatment with ropeginterferon alfa-2b
Ethnic sensitivity analyses of pharmacokinetics, efficacy and safety in polycythemia vera treatment with ropeginterferon alfa-2b Abstract Abstract Ropeginterferon alfa-2b (Ropeg) is approved for the treatment of adults with polycythemia vera (PV). This report aims to analyze the ethnic sensitivity of Ropeg for the trea...
PMC12683211
core_pubmed_pmc
Advances in Conductive Nanomaterials for Cardiac Arrhythmia and Future Directions in Bioevaluation Strategies
Advances in Conductive Nanomaterials for Cardiac Arrhythmia and Future Directions in Bioevaluation Strategies Abstract Abstract Cardiac arrhythmia (CA), characterized by irregular heart rhythms, affects nearly 90% of individuals with cardiovascular diseases. Commonly triggered by myocardial infarction (MI) or ion chann...
PMC4318893
core_pubmed_pmc
11β-Hydroxysteroid Dehydrogenase Activity in the Brain Does Not Contribute to Systemic Interconversion of Cortisol and Cortisone in Healthy Men
11β-Hydroxysteroid Dehydrogenase Activity in the Brain Does Not Contribute to Systemic Interconversion of Cortisol and Cortisone in Healthy Men Abstract Abstract Context and Objective: 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) catalyses regeneration of cortisol in liver, adipose tissue, and skeletal muscle, mak...
PMC5357096
core_pubmed_pmc
Effect of nitazoxanide on albendazole pharmacokinetics in cerebrospinal fluid and plasma in rats
Effect of nitazoxanide on albendazole pharmacokinetics in cerebrospinal fluid and plasma in rats Abstract Background: Although albendazole is the drug-of-choice for the treatment of neurocysticercosis, its efficacy is limited due to its low bioavailability. An alternative for optimizing pharmacological treatment is thr...
PMC9747118
core_pubmed_pmc
Population‐based cellular kinetic characterization of ciltacabtagene autoleucel in subjects with relapsed or refractory multiple myeloma
Population‐based cellular kinetic characterization of ciltacabtagene autoleucel in subjects with relapsed or refractory multiple myeloma Abstract Abstract The aims of this work were to develop a population pharmacokinetic (PK) model for chimeric antigen receptor (CAR) transgene after single intravenous infusion adminis...
PMC4326208
core_pubmed_pmc
Pharmacokinetic model of unfractionated heparin during and after cardiopulmonary bypass in cardiac surgery
Pharmacokinetic model of unfractionated heparin during and after cardiopulmonary bypass in cardiac surgery Abstract Abstract Background Unfractionated heparin (UFH) is widely used as a reversible anti-coagulant in cardiopulmonary bypass (CPB). However, the pharmacokinetic characteristics of UFH in CPB surgeries remain ...
PMC10615937
core_pubmed_pmc
Safety, pharmacokinetics, and efficacy of belantamab mafodotin monotherapy in Japanese patients with relapsed or refractory multiple myeloma: DREAMM-11
Safety, pharmacokinetics, and efficacy of belantamab mafodotin monotherapy in Japanese patients with relapsed or refractory multiple myeloma: DREAMM-11 Abstract Abstract Belantamab mafodotin, a B-cell maturation antigen-targeting antibody–drug conjugate (ADC), was investigated in Japanese patients with relapsed/refract...
PMC5760995
core_pubmed_pmc
Method development and validation of Guanfacine in rat plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study
Method development and validation of Guanfacine in rat plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study Abstract Abstract A selective, sensitive and high-throughput liquid chromatography–tandem mass spectrometry (LC–ESI-MS/MS) method has been developed and validated for t...
PMC7187627
core_pubmed_pmc
Multiple-Ascending-Dose Phase 1 Clinical Study of the Safety, Tolerability, and Pharmacokinetics of CRS3123, a Narrow-Spectrum Agent with Minimal Disruption of Normal Gut Microbiota
Multiple-Ascending-Dose Phase 1 Clinical Study of the Safety, Tolerability, and Pharmacokinetics of CRS3123, a Narrow-Spectrum Agent with Minimal Disruption of Normal Gut Microbiota Abstract CRS3123 is a novel small molecule that potently inhibits methionyl-tRNA synthetase of Clostridioides difficile , inhibiting C. di...
PMC3463859
core_pubmed_pmc
Integrating Experimentation and Quantitative Modeling to Enhance Discovery of Beta Amyloid Lowering Therapeutics for Alzheimer’s Disease
Integrating Experimentation and Quantitative Modeling to Enhance Discovery of Beta Amyloid Lowering Therapeutics for Alzheimer’s Disease Abstract Abstract Drug discovery can benefit from a proactive-knowledge-attainment philosophy which strategically integrates experimentation and pharmacokinetic/pharmacodynamic (PK/PD...
PMC3131558
core_pubmed_pmc
Plitidepsin Has a Safe Cardiac Profile: A Comprehensive Analysis
Plitidepsin Has a Safe Cardiac Profile: A Comprehensive Analysis Abstract Abstract Plitidepsin is a cyclic depsipeptide of marine origin in clinical development in cancer patients. Previously, some depsipeptides have been linked to increased cardiac toxicity. Clinical databases were searched for cardiac adverse events ...
PMC4326489
core_pubmed_pmc
Efficacy and pharmacokinetic evaluation of a novel anti-malarial compound (NP046) in a mouse model
Efficacy and pharmacokinetic evaluation of a novel anti-malarial compound (NP046) in a mouse model Abstract Abstract Background Even though malaria is a completely preventable and treatable disease, it remains a threat to human life and a burden to the global economy due to the emergence of multiple-drug resistant mala...
PMC11106956
core_pubmed_pmc
Population pharmacokinetics of primaquine and its metabolites in African males
Population pharmacokinetics of primaquine and its metabolites in African males Abstract Background Primaquine (PQ) is the prototype 8-aminoquinoline drug, a class which targets gametocytes and hypnozoites. The World Health Organization (WHO) recommends adding a single low dose of primaquine to the standard artemisinin-...
PMC3610115
core_pubmed_pmc
Study of the pharmacokinetic changes of Tramadol in diabetic rats
Study of the pharmacokinetic changes of Tramadol in diabetic rats Abstract Abstract Background Besides the pathological states, diabetes mellitus may also alter the hepatic biotransformation of pharmaceutical agents. It is advantageous to understand the effect of diabetes on the pharmacokinetic of drugs. The objective ...
PMC11404262
core_pubmed_pmc
Effect of henagliflozin on left ventricular mass index in dialysis patients with HFpEF (HELD-HF): protocol for a multicentre, randomised, double-blind, placebo-controlled trial
Effect of henagliflozin on left ventricular mass index in dialysis patients with HFpEF (HELD-HF): protocol for a multicentre, randomised, double-blind, placebo-controlled trial Abstract Abstract Introduction Heart failure with preserved ejection fraction (HFpEF) is a prevalent comorbidity among patients with end-stage ...
PMC9712457
core_pubmed_pmc
Exploring the potential mechanism of Fritiliariae Irrhosae Bulbus on ischemic stroke based on network pharmacology and experimental validation
Exploring the potential mechanism of Fritiliariae Irrhosae Bulbus on ischemic stroke based on network pharmacology and experimental validation Abstract Abstract Objective: To study the potential targets and molecular mechanisms of Fritiliariae Irrhosae Bulbus (FIB) in the treatment of ischemic strokes based on a networ...
PMC5247555
core_pubmed_pmc
Pharmacokinetics, Biotransformation, and Excretion of [ 14 C]Etelcalcetide (AMG 416) Following a Single Microtracer Intravenous Dose in Patients with Chronic Kidney Disease on Hemodialysis
Pharmacokinetics, Biotransformation, and Excretion of [ 14 C]Etelcalcetide (AMG 416) Following a Single Microtracer Intravenous Dose in Patients with Chronic Kidney Disease on Hemodialysis Abstract Abstract Etelcalcetide (AMG 416) is a novel synthetic peptide calcium-sensing receptor activator in clinical development a...
PMC7838024
core_pubmed_pmc
A facile and universal method to achieve liposomal remote loading of non-ionizable drugs with outstanding safety profiles and therapeutic effect
A facile and universal method to achieve liposomal remote loading of non-ionizable drugs with outstanding safety profiles and therapeutic effect Abstract Liposomes have made remarkable achievements as drug delivery vehicles in the clinic. Liposomal products mostly benefited from remote drug loading techniques that succ...
PMC10175964
core_pubmed_pmc
A multi‐purpose Japanese phase I study in the global development of vupanorsen: Randomized, placebo‐controlled, single‐ascending dose study in adults
A multi‐purpose Japanese phase I study in the global development of vupanorsen: Randomized, placebo‐controlled, single‐ascending dose study in adults Abstract Abstract Vupanorsen (PF‐07285557) is a second‐generation tri‐ N ‐acetyl galactosamine (GalNAc 3 )‐antisense oligonucleotide targeted to angiopoietin‐like 3 (ANGP...
PMC9457773
core_pubmed_pmc
Pharmacokinetic Interactions between Canagliflozin and Sorafenib or Lenvatinib in Rats
Pharmacokinetic Interactions between Canagliflozin and Sorafenib or Lenvatinib in Rats Abstract Abstract Hepatocellular carcinoma (HCC) and type 2 diabetes mellitus (T2DM) are common clinical conditions, and T2DM is an independent risk factor for HCC. Sorafenib and lenvatinib, two multi-targeted tyrosine kinase inhibit...
PMC4112050
core_pubmed_pmc
Population pharmacokinetics of trastuzumab emtansine (T-DM1), a HER2-targeted antibody–drug conjugate, in patients with HER2-positive metastatic breast cancer: clinical implications of the effect of covariates
Population pharmacokinetics of trastuzumab emtansine (T-DM1), a HER2-targeted antibody–drug conjugate, in patients with HER2-positive metastatic breast cancer: clinical implications of the effect of covariates Abstract Abstract Purpose Trastuzumab emtansine (T-DM1) is an antibody–drug conjugate comprising the humanized...
PMC12129583
core_pubmed_pmc
A pre-post quasi-experimental study of the impact of TDM-guided aggressive pharmacokinetic/pharmacodynamic target attainment of continuous infusion ceftolozane/tazobactam monotherapy in treating severe Pseudomonas aeruginosa infections: a strategy useful for raising the bar?
A pre-post quasi-experimental study of the impact of TDM-guided aggressive pharmacokinetic/pharmacodynamic target attainment of continuous infusion ceftolozane/tazobactam monotherapy in treating severe Pseudomonas aeruginosa infections: a strategy useful for raising the bar? Abstract Abstract Objectives To assess the c...
PMC4432908
core_pubmed_pmc
Clinical and pharmacokinetic evaluation of S-ketamine for intravenous general anaesthesia in horses undergoing field castration
Clinical and pharmacokinetic evaluation of S-ketamine for intravenous general anaesthesia in horses undergoing field castration Abstract Background Intravenous anaesthetic drugs are the primary means for producing general anaesthesia in equine practice. The ideal drug for intravenous anaesthesia has high reliability an...
PMC10405310
core_pubmed_pmc
Safety, efficacy and pharmacokinetics of palivizumab in off-label neonates, infants, and young children at risk for serious respiratory syncytial virus infection: a multicenter phase II clinical trial
Safety, efficacy and pharmacokinetics of palivizumab in off-label neonates, infants, and young children at risk for serious respiratory syncytial virus infection: a multicenter phase II clinical trial Abstract Summary Background Pediatric patients with certain rare diseases are at increased risk of severe respiratory s...
PMC9135659
core_pubmed_pmc
Pitavastatin-Incorporated Nanoparticles for Chronic Limb Threatening Ischemia: A Phase I/IIa Clinical Trial
Pitavastatin-Incorporated Nanoparticles for Chronic Limb Threatening Ischemia: A Phase I/IIa Clinical Trial Abstract Abstract Aim: To assess the results of a phase I/IIa open-label dose-escalation clinical trial of 5-day repeated intramuscular administration of pitavastatin-incorporated poly (lactic-co-glycolic acid) n...
PMC12155186
core_pubmed_pmc
GLP-1 Analogues in the Neurobiology of Addiction: Translational Insights and Therapeutic Perspectives
GLP-1 Analogues in the Neurobiology of Addiction: Translational Insights and Therapeutic Perspectives Abstract Glucagon-like peptide-1 receptor agonists, originally developed for the treatment of metabolic disorders, have recently emerged as promising candidates for the management of substance use disorders. This revie...
PMC9075506
core_pubmed_pmc
A selective and sensitive UFLC-MS/MS method for the simultaneous determination of five alkaloids from Piper longum L. and its application in the pharmacokinetic study of 6-OHDA-induced Parkinson's disease rats
A selective and sensitive UFLC-MS/MS method for the simultaneous determination of five alkaloids from Piper longum L. and its application in the pharmacokinetic study of 6-OHDA-induced Parkinson's disease rats Abstract Abstract The alkaloids from Piper longum L. (PLA) mainly contain piperine (PPR), piperlongumine (PPL)...
PMC11179669
core_pubmed_pmc
Enhanced Pharmacokinetics of Celastrol via Long-Circulating Liposomal Delivery for Intravenous Administration
Enhanced Pharmacokinetics of Celastrol via Long-Circulating Liposomal Delivery for Intravenous Administration Abstract Abstract Background Rheumatoid Arthritis (RA) involves prolonged inflammation of the synovium, damaging joints and causing stiffness and deformity. Celastrol (Cel), derived from the Chinese herbal medi...
PMC2805799
core_pubmed_pmc
Dosage and formulation issues: oral vitamin E therapy in children
Dosage and formulation issues: oral vitamin E therapy in children Abstract Purpose Oral vitamin E is used in several childhood diseases, but dosage recommendations differ. Few oral products have a marketing authorization for therapeutic use in children. Preliminary data indicate differences in bioavailability among the...
PMC5190058
core_pubmed_pmc
Combination of gemcitabine-containing magnetoliposome and oxaliplatin-containing magnetoliposome in breast cancer treatment: A possible mechanism with potential for clinical application
Combination of gemcitabine-containing magnetoliposome and oxaliplatin-containing magnetoliposome in breast cancer treatment: A possible mechanism with potential for clinical application Abstract Breast cancer is a major global health problem with high incidence and case fatality rates. The use of magnetoliposomes has b...
PMC10534335
core_pubmed_pmc
Bedaquiline-Loaded Solid Lipid Nanoparticles Drug Delivery in the Management of Non-Small-Cell Lung Cancer (NSCLC)
Bedaquiline-Loaded Solid Lipid Nanoparticles Drug Delivery in the Management of Non-Small-Cell Lung Cancer (NSCLC) Abstract Abstract Non-small-cell lung cancer (NSCLC) mortality and new case rates are both on the rise. Most patients have fewer treatment options accessible due to side effects from drugs and the emergenc...
PMC10855066
core_pubmed_pmc
Anti-Inflammatory and Antioxidant Pyrrolo[3,4- d ]pyridazinone Derivatives Interact with DNA and Bind to Plasma Proteins—Spectroscopic and In Silico Studies
Anti-Inflammatory and Antioxidant Pyrrolo[3,4- d ]pyridazinone Derivatives Interact with DNA and Bind to Plasma Proteins—Spectroscopic and In Silico Studies Abstract Abstract From the point of view of the search for new pharmaceuticals, pyridazinone derivatives are a very promising group of compounds. In our previous w...
PMC6226122
core_pubmed_pmc
No Pharmacokinetic Interactions Between Elbasvir or Grazoprevir and Methadone in Participants Receiving Maintenance Opioid Agonist Therapy
No Pharmacokinetic Interactions Between Elbasvir or Grazoprevir and Methadone in Participants Receiving Maintenance Opioid Agonist Therapy Abstract Abstract We conducted two phase I trials to evaluate the pharmacokinetic interactions between elbasvir (EBR), grazoprevir (GZR), and methadone (MK‐8742‐P010 and MK‐5172‐P03...
PMC4211354
core_pubmed_pmc
Effects of breakpoint changes on carbapenem susceptibility rates of Enterobacteriaceae : Results from the SENTRY Antimicrobial Surveillance Program, United States, 2008 to 2012
Effects of breakpoint changes on carbapenem susceptibility rates of Enterobacteriaceae : Results from the SENTRY Antimicrobial Surveillance Program, United States, 2008 to 2012 Abstract Antibiotic susceptibility breakpoints are determined at the time of clinical approval for a given drug, but may need to be revised to ...
PMC4776683
core_pubmed_pmc
The effect of modulated electro-hyperthermia on the pharmacokinetic properties of nefopam in healthy volunteers: A randomised, single-dose, crossover open-label study
The effect of modulated electro-hyperthermia on the pharmacokinetic properties of nefopam in healthy volunteers: A randomised, single-dose, crossover open-label study Abstract Abstract Purpose : Nefopam is a widely available analgesic for the management of pain. The aim of this study was to reveal the effect of regiona...
PMC6351946
core_pubmed_pmc
Breast Cancer and Exposure to Organochlorines in the CECILE Study: Associations with Plasma Levels Measured at the Time of Diagnosis and Estimated during Adolescence
Breast Cancer and Exposure to Organochlorines in the CECILE Study: Associations with Plasma Levels Measured at the Time of Diagnosis and Estimated during Adolescence Abstract Exposure to environmental chemicals with hormonal effects, such as organochlorine compounds (OCs), during developmental periods of breast cells m...