id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC6014264
core_pubmed_pmc
Effect of pore size and morphology of activated charcoal prepared from midribs of Elaeis guineensis on adsorption of poisons using metronidazole and Escherichia coli O157:H7 as a case study
Effect of pore size and morphology of activated charcoal prepared from midribs of Elaeis guineensis on adsorption of poisons using metronidazole and Escherichia coli O157:H7 as a case study Abstract Abstract Agricultural waste obtained from Elaeis guineensis mid ribs can provide a veritable source of materials which ca...
PMC11151742
core_pubmed_pmc
Transcutaneous auricular vagus nerve stimulation may benefit from the addition of N-acetylcysteine to facilitate motor learning in infants of diabetic mothers failing oral feeds
Transcutaneous auricular vagus nerve stimulation may benefit from the addition of N-acetylcysteine to facilitate motor learning in infants of diabetic mothers failing oral feeds Abstract Objective This study aims to determine if pretreating with enteral N-acetylcysteine (NAC) improves CNS oxidative stress and facilitat...
PMC12888661
core_pubmed_pmc
Optimizing ribociclib dosing in breast cancer with brain metastasis patients using a physiologically based pharmacokinetic model
Optimizing ribociclib dosing in breast cancer with brain metastasis patients using a physiologically based pharmacokinetic model Abstract Objective This study aimed to determine the optimal dosing strategy for ribociclib (RIB) in patients with breast cancer and brain metastasis (BCBM) by using a developed and validated...
PMC5058661
core_pubmed_pmc
Effects of aging on the effectiveness of smoking cessation medication
Effects of aging on the effectiveness of smoking cessation medication Abstract Abstract Background Considering the pharmacokinetic and pharmacodynamic aspects of different medications, it is plausible that the age of a smoker could affect the half-life of these drugs. The aim of this study was to compare the effectiven...
PMC8653087
core_pubmed_pmc
An Open Label, Adaptive, Phase 1 Trial of High‐Dose Oral Nitazoxanide in Healthy Volunteers: An Antiviral Candidate for SARS‐CoV‐2
An Open Label, Adaptive, Phase 1 Trial of High‐Dose Oral Nitazoxanide in Healthy Volunteers: An Antiviral Candidate for SARS‐CoV‐2 Abstract Abstract Repurposing approved drugs may rapidly establish effective interventions during a public health crisis. This has yielded immunomodulatory treatments for severe coronavirus...
PMC8399089
core_pubmed_pmc
Monolayer platform using human biopsy-derived duodenal organoids for pharmaceutical research
Monolayer platform using human biopsy-derived duodenal organoids for pharmaceutical research Abstract Abstract The human small intestine is the key organ for absorption, metabolism, and excretion of orally administered drugs. To preclinically predict these reactions in drug discovery research, a cell model that can pre...
PMC9276671
core_pubmed_pmc
A first-in-human Phase I dose-escalation trial of the novel therapeutic peptide, ALM201, demonstrates a favourable safety profile in unselected patients with ovarian cancer and other advanced solid tumours
A first-in-human Phase I dose-escalation trial of the novel therapeutic peptide, ALM201, demonstrates a favourable safety profile in unselected patients with ovarian cancer and other advanced solid tumours Abstract Background We aimed to assess the safety, tolerability and pharmacokinetics of a novel anti-angiogenic pe...
PMC5813016
core_pubmed_pmc
Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor
Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor Abstract Abstract Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a therapeutic strategy for neurologic and psychiatric diseases due to the fundamental role of D1Rs in m...
PMC10222948
core_pubmed_pmc
Intraperitoneally Administered Vancomycin in Patients with Peritoneal Dialysis-Associated Peritonitis: Population Pharmacokinetics and Dosing Implications
Intraperitoneally Administered Vancomycin in Patients with Peritoneal Dialysis-Associated Peritonitis: Population Pharmacokinetics and Dosing Implications Abstract Abstract Peritonitis is a limiting complication of peritoneal dialysis, which is treated by intraperitoneal administration of antibiotics. Various dosing st...
PMC11919261
core_pubmed_pmc
Semi‐mechanistic population PK/PD model to aid clinical understanding of myelodysplastic syndromes following treatment with Venetoclax and Azacitidine
Semi‐mechanistic population PK/PD model to aid clinical understanding of myelodysplastic syndromes following treatment with Venetoclax and Azacitidine Abstract Abstract Myelodysplastic syndromes (MDS) represent a group of bone marrow disorders involving cytopenias, hypercellular bone marrow, and dysplastic hematopoieti...
PMC10859787
core_pubmed_pmc
Population pharmacokinetics and exposure‐response analyses for efficacy and safety of upadacitinib in patients with axial spondyloarthritis
Population pharmacokinetics and exposure‐response analyses for efficacy and safety of upadacitinib in patients with axial spondyloarthritis Abstract Abstract Upadacitinib is an orally administered, selective, Janus kinase inhibitor that is approved for several auto‐immune conditions, such as axial spondyloarthritis, an...
PMC10146264
core_pubmed_pmc
Safety, Pharmacokinetic and Pharmacodynamic Evaluation of Teverelix for the Treatment of Hormone-Sensitive Advanced Prostate Cancer: Phase 2 Loading-Dose-Finding Studies
Safety, Pharmacokinetic and Pharmacodynamic Evaluation of Teverelix for the Treatment of Hormone-Sensitive Advanced Prostate Cancer: Phase 2 Loading-Dose-Finding Studies Abstract Background and objectives: Teverelix drug product (DP) is a gonadotropin-releasing hormone antagonist in development for the treatment of pat...
PMC8532831
core_pubmed_pmc
MPC-Based Prediction of Anti-Mutant Effectiveness of Antibiotic Combinations: In Vitro Model Study with Daptomycin and Gentamicin against Staphylococcus aureus
MPC-Based Prediction of Anti-Mutant Effectiveness of Antibiotic Combinations: In Vitro Model Study with Daptomycin and Gentamicin against Staphylococcus aureus Abstract To explore whether combined treatments with daptomycin and gentamicin can prevent the development of Staphylococcus aureus resistance, and whether the ...
PMC11568778
core_pubmed_pmc
Spiral volumetric optoacoustic and ultrasound (SVOPUS) tomography of mice
Spiral volumetric optoacoustic and ultrasound (SVOPUS) tomography of mice Abstract Optoacoustic (OA) tomography is a powerful noninvasive preclinical imaging tool enabling high resolution whole-body visualization of biodistribution and dynamics of molecular agents. The technique yet lacks endogenous soft-tissue contras...
PMC12352012
core_pubmed_pmc
Moxifloxacin-Induced Seizures: A Case Report
Moxifloxacin-Induced Seizures: A Case Report Abstract Abstract Fluoroquinolones are widely used antibiotics due to their broad-spectrum activity and favorable pharmacokinetic properties. However, increasing evidence has raised concerns about their neurotoxic potential, particularly in vulnerable populations. We present...
PMC11946590
core_pubmed_pmc
Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial
Bioequivalence Study of Two Oral Methocarbamol Formulations in Healthy Subjects Under Fasting Conditions: A Randomized, Open-Label, Crossover Clinical Trial Abstract Objective: This study aimed to assess the bioequivalence of two oral methocarbamol formulations, as follows: the test (T) methocarbamol 1500 mg tablets an...
PMC6383175
core_pubmed_pmc
Bioequivalence of 2 Naproxen Sodium Tablet Formulations in Healthy Male and Female Volunteers
Bioequivalence of 2 Naproxen Sodium Tablet Formulations in Healthy Male and Female Volunteers Abstract Highlights • This study compared the relative bioavailability of naproxen sodium when administered as a currently-marketed reference product (Aleve ® naproxen sodium 220 mg, Bayer B.V. ) and a new test product (naprox...
PMC12089089
core_pubmed_pmc
Plant polysaccharides influence tumor development based on epigenetics: a review
Plant polysaccharides influence tumor development based on epigenetics: a review Abstract Abstract Plant polysaccharides have emerged as pivotal epigenetic modulators in oncology, offering multi-target therapeutic potential to address toxicity and drug resistance limitations of conventional therapies. This review integ...
PMC7393056
core_pubmed_pmc
Evaluation of Cyclosporine Pharmacokinetic, Monitoring, and Dosing Parameters for GVHD Prophylaxis in Hematopoietic Stem Cell Transplant (HSCT) Recipients
Evaluation of Cyclosporine Pharmacokinetic, Monitoring, and Dosing Parameters for GVHD Prophylaxis in Hematopoietic Stem Cell Transplant (HSCT) Recipients Abstract Allogeneic hematopoietic stem cell transplantation (AHSCT) is a major method of treatment for different hematologic and congenital disease. Graft versus hos...
PMC11879792
core_pubmed_pmc
Pharmacokinetics and bioequivalence of two formulations of the S-1 (tegafur/gimeracil/oxonate) capsule in Chinese cancer patients under fasting and fed conditions: a multicenter, randomized, open-label, single-dose, double-cycle crossover study
Pharmacokinetics and bioequivalence of two formulations of the S-1 (tegafur/gimeracil/oxonate) capsule in Chinese cancer patients under fasting and fed conditions: a multicenter, randomized, open-label, single-dose, double-cycle crossover study Abstract Objective S-1, an oral multicomponent capsule containing tegafur, ...
PMC8158765
core_pubmed_pmc
Rational Design of Novel Inhibitors of α-Glucosidase: An Application of Quantitative Structure Activity Relationship and Structure-Based Virtual Screening
Rational Design of Novel Inhibitors of α-Glucosidase: An Application of Quantitative Structure Activity Relationship and Structure-Based Virtual Screening Abstract α-Glucosidase is considered a prime drug target for Diabetes Mellitus and its inhibitors are used to delay carbohydrate digestion for the treatment of diabe...
PMC12879251
core_pubmed_pmc
Body composition and anti-neoplastic treatment in adult and older subjects - A systematic review
Body composition and anti-neoplastic treatment in adult and older subjects - A systematic review Abstract Background T he estimation of the risk of poor tolerance and overdose of antineoplastic agents protocols represents a major challenge in oncology, particularly in older patients. We hypothesize that age-related mod...
PMC8097779
core_pubmed_pmc
Establishment of a population pharmacokinetics model of vancomycin in 94 infants with septicemia and its application in individualized therapy
Establishment of a population pharmacokinetics model of vancomycin in 94 infants with septicemia and its application in individualized therapy Abstract Abstract Background We aim to develop a population pharmacokinetics (PopPK) model of vancomycin for the treatment of septicemia in infants younger than one year. Factor...
PMC6277878
core_pubmed_pmc
Cannabinoids and Pain: New Insights From Old Molecules
Cannabinoids and Pain: New Insights From Old Molecules Abstract Abstract Cannabis has been used for medicinal purposes for thousands of years. The prohibition of cannabis in the middle of the 20th century has arrested cannabis research. In recent years there is a growing debate about the use of cannabis for medical pur...
PMC5904239
core_pubmed_pmc
Evidence-Based Design of Fixed-Dose Combinations: Principles and Application to Pediatric Anti-Tuberculosis Therapy
Evidence-Based Design of Fixed-Dose Combinations: Principles and Application to Pediatric Anti-Tuberculosis Therapy Abstract Abstract Background and Objectives Fixed-dose combination formulations where several drugs are included in one tablet are important for the implementation of many long-term multidrug therapies. T...
PMC7496299
core_pubmed_pmc
Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans
Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans Abstract Objective To evaluate the potential for pharmacokinetic interaction and the safety and tolerability when ubrogepant and sumatriptan are coadministered in a Phase 1 study in ...
PMC9150140
core_pubmed_pmc
Effect of alcohol coadministration on the pharmacodynamics, pharmacokinetics, and safety of lemborexant: A randomized, placebo-controlled crossover study
Effect of alcohol coadministration on the pharmacodynamics, pharmacokinetics, and safety of lemborexant: A randomized, placebo-controlled crossover study Abstract Background: Lemborexant is a dual orexin receptor antagonist approved to treat insomnia in adults in several countries including the USA, Canada, and Japan. ...
PMC5859165
core_pubmed_pmc
Insight into the interaction of inhaled corticosteroids with human serum albumin: A spectroscopic-based study
Insight into the interaction of inhaled corticosteroids with human serum albumin: A spectroscopic-based study Abstract Abstract It is well known that the safety and efficacy profile of an inhaled cortocosteroid (ICS) is influenced by the pharmacokinetic properties and associated pharmacodynamic effects of the drug. Fre...
PMC7318034
core_pubmed_pmc
Safety, Pharmacokinetics, and Drug-Drug Interaction Potential of Intravenous Durlobactam, a β-Lactamase Inhibitor, in Healthy Subjects
Safety, Pharmacokinetics, and Drug-Drug Interaction Potential of Intravenous Durlobactam, a β-Lactamase Inhibitor, in Healthy Subjects Abstract Durlobactam (DUR; also known as ETX2514) is a novel β-lactamase inhibitor with broad activity against Ambler class A, C, and D β-lactamases. Addition of DUR to sulbactam (SUL) ...
PMC12122562
core_pubmed_pmc
Phase 1 studies of the indenoisoquinolines LMP776 and LMP744 in patients with solid tumors and lymphomas
Phase 1 studies of the indenoisoquinolines LMP776 and LMP744 in patients with solid tumors and lymphomas Abstract Purpose Indenoisoquinolines are a class of topoisomerase I (TOP1) inhibitors designed to overcome clinical limitations of camptothecins. Three indenoisoquinolines (LMP400, LMP776, and LMP744) demonstrated a...
PMC3480420
core_pubmed_pmc
Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”): The Influence of Gender and Genetics (CYP2D6, COMT, 5-HTT)
Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”): The Influence of Gender and Genetics (CYP2D6, COMT, 5-HTT) Abstract Abstract The synthetic psychostimulant MDMA (±3,4-methylenedioxymethamphetamine, ecstasy) acts as an indirect serotonin, dopamine, and norepinephrine agonist and as a mechani...
PMC4721819
core_pubmed_pmc
Pharmacokinetics of Chiral Dendrimer-Triamine-Coordinated Gd-MRI Contrast Agents Evaluated by in Vivo MRI and Estimated by in Vitro QCM
Pharmacokinetics of Chiral Dendrimer-Triamine-Coordinated Gd-MRI Contrast Agents Evaluated by in Vivo MRI and Estimated by in Vitro QCM Abstract Recently, we developed novel chiral dendrimer-triamine-coordinated Gd-MRI contrast agents (Gd-MRI CAs), which showed longitudinal relaxivity ( r 1 ) values about four times hi...
PMC4772838
core_pubmed_pmc
Unintended Pregnancies Observed With Combined Use of the Levonorgestrel Contraceptive Implant and Efavirenz-based Antiretroviral Therapy: A Three-Arm Pharmacokinetic Evaluation Over 48 Weeks
Unintended Pregnancies Observed With Combined Use of the Levonorgestrel Contraceptive Implant and Efavirenz-based Antiretroviral Therapy: A Three-Arm Pharmacokinetic Evaluation Over 48 Weeks Abstract Women receiving efavirenz-based antiretroviral therapy plus a contraceptive implant had significantly lower levonorgestr...
PMC11936797
core_pubmed_pmc
Molecular determinants of neuroprotection in blood-brain interfaces of the cynomolgus monkey
Molecular determinants of neuroprotection in blood-brain interfaces of the cynomolgus monkey Abstract Abstract The blood-brain barrier (BBB) formed by the cerebral microvessel endothelium and the blood-CSF barrier (BCSFB) formed by the choroid plexus epithelium impact the cerebral bioavailability of drugs and endogenou...
PMC6900553
core_pubmed_pmc
Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor
Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor Abstract EGFR tyrosine kinase inhibitor (EGFR-TKI) has been used successfully in clinic for the treatment of solid tumors. In the present study, we reported the discovery of WS-157 from our in-house diverse compound library, which was va...
PMC11707343
core_pubmed_pmc
Formulation development and evaluation, in silico PBPK modeling and in vivo pharmacodynamic studies of clozapine matrix type transdermal patches
Formulation development and evaluation, in silico PBPK modeling and in vivo pharmacodynamic studies of clozapine matrix type transdermal patches Abstract Clozapine is a potent serotonin receptor antagonist and commonly used for the treatment of Schizophrenia. The study aimed to develop and optimize the transdermal matr...
PMC11106138
core_pubmed_pmc
Time-Varying Clearance in Milrinone Pharmacokinetics from Premature Neonates to Adolescents
Time-Varying Clearance in Milrinone Pharmacokinetics from Premature Neonates to Adolescents Abstract Abstract Background and Objectives Milrinone is an inotrope and vasodilator used for prophylaxis or treatment of low cardiac output syndrome after weaning from cardiopulmonary bypass (CPB). It is renally eliminated and ...
PMC6481230
core_pubmed_pmc
Breaking the cycle
Breaking the cycle Abstract Abstract Objective To infer molecular effectors of therapeutic effects and adverse events for dimethyl fumarate (DMF) in patients with relapsing-remitting MS (RRMS) using untargeted plasma metabolomics. Methods Plasma from 27 patients with RRMS was collected at baseline and 6 weeks after ini...
PMC9818258
core_pubmed_pmc
Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors in the Treatment of Advanced Renal Cancer
Therapeutic Drug Monitoring of Tyrosine Kinase Inhibitors in the Treatment of Advanced Renal Cancer Abstract Abstract Simple Summary The rational, benefits and limits of therapeutic drug monitoring as a routine practice are discussed for the seven tyrosine kinase inhibitor compounds currently used to treat advanced ren...
PMC9376161
core_pubmed_pmc
High efficacy of tamoxifen-loaded L-lysine coated magnetic iron oxide nanoparticles in cell cycle arrest and anti-cancer activity for breast cancer therapy
High efficacy of tamoxifen-loaded L-lysine coated magnetic iron oxide nanoparticles in cell cycle arrest and anti-cancer activity for breast cancer therapy Abstract Abstract Introduction: Due to the side effects of drugs, the development of nanoscale drug delivery systems has led to a significant improvement in medicin...
PMC9798452
core_pubmed_pmc
Transporter and metabolizer gene polymorphisms affect fluoroquinolone pharmacokinetic parameters
Transporter and metabolizer gene polymorphisms affect fluoroquinolone pharmacokinetic parameters Abstract Abstract Tuberculosis (TB) is an infectious disease that occurs globally. Treatment of TB has been hindered by problems with multidrug-resistant strains (MDR-TB). Fluoroquinolones are one of the main drugs used for...
PMC9760361
core_pubmed_pmc
Development and In vivo Pharmacokinetic and Pharmacodynamic Evaluation of an Oral Innovative Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan Formulation for Enhanced Bioavailability
Development and In vivo Pharmacokinetic and Pharmacodynamic Evaluation of an Oral Innovative Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan Formulation for Enhanced Bioavailability Abstract Abstract Background: Irbesartan (IR) is used in the treatment of hypertension, heart failure, and nephropathy in Type II...
PMC12494115
core_pubmed_pmc
Pharmacological Phase I Clinical Trials in Pediatric Brain Tumors (1990–2024): A Historical Perspective
Pharmacological Phase I Clinical Trials in Pediatric Brain Tumors (1990–2024): A Historical Perspective Abstract Abstract Central nervous system (CNS) tumors are the most common solid tumors in pediatric patients and the leading cause of childhood cancer-related mortality. Their rarity compared to adult cancers has mad...
PMC10420079
core_pubmed_pmc
Differences in the pharmacokinetics and steady-state blood concentrations of orally administered lenvatinib in adult and juvenile rats
Differences in the pharmacokinetics and steady-state blood concentrations of orally administered lenvatinib in adult and juvenile rats Abstract Abstract Objective: The aim of this study was to compare the pharmacokinetics and steady-state serum concentrations of lenvatinib in adult and juvenile rats. Experimental study...
PMC5387939
core_pubmed_pmc
Feasibility of melatonin for prevention of delirium in critically ill patients: a protocol for a multicentre, randomised, placebo-controlled study
Feasibility of melatonin for prevention of delirium in critically ill patients: a protocol for a multicentre, randomised, placebo-controlled study Abstract Abstract Introduction Delirium is highly prevalent in the intensive care unit (ICU) and is associated with adverse clinical outcomes. At this time, there is no drug...
PMC11831872
core_pubmed_pmc
Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry
Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry Abstract Abstract Relieving severe pains is an unmet medical need, in which opioids are of prime importance and in the focus of pharmaceutical companies. The objective of this study is to characterize the physicochemical proper...
PMC9047688
core_pubmed_pmc
Population pharmacokinetics of piperacillin/tazobactam in critically ill Korean patients and the effects of extracorporeal membrane oxygenation
Population pharmacokinetics of piperacillin/tazobactam in critically ill Korean patients and the effects of extracorporeal membrane oxygenation Abstract Abstract Objectives To explore extracorporeal membrane oxygenation (ECMO)-related alterations of the pharmacokinetics (PK) of piperacillin/tazobactam and determine an ...
PMC6974970
core_pubmed_pmc
Pharmacokinetics of plasma lopinavir and ritonavir in tuberculosis–HIV co-infected African adult patients also receiving rifabutin 150 or 300 mg three times per week
Pharmacokinetics of plasma lopinavir and ritonavir in tuberculosis–HIV co-infected African adult patients also receiving rifabutin 150 or 300 mg three times per week Abstract Background To evaluate the pharmacokinetic of plasma lopinavir (LPV) and ritonavir (RTV) when co-administered with three times weekly (TPW) rifab...
PMC10222987
core_pubmed_pmc
In Vivo Antiviral Activity of Baloxavir against PA/I38T-Substituted Influenza A Viruses at Clinically Relevant Doses
In Vivo Antiviral Activity of Baloxavir against PA/I38T-Substituted Influenza A Viruses at Clinically Relevant Doses Abstract Although the prevalence of polymerase acidic (PA)/I38T strains of influenza virus with reduced susceptibility to baloxavir acid is low, there is a possibility of emergence under selective pressu...
PMC3849266
core_pubmed_pmc
In Vitro and In Vivo Evaluation of a 18 F-Labeled High Affinity NOTA Conjugated Bombesin Antagonist as a PET Ligand for GRPR-Targeted Tumor Imaging
In Vitro and In Vivo Evaluation of a 18 F-Labeled High Affinity NOTA Conjugated Bombesin Antagonist as a PET Ligand for GRPR-Targeted Tumor Imaging Abstract Abstract Expression of the gastrin-releasing peptide receptor (GRPR) in prostate cancer suggests that this receptor can be used as a potential molecular target to ...
PMC12629152
core_pubmed_pmc
Study on the Screening of Anti‐Osteoporosis Components in Processed Epimedium‐Based on Spectrum‐Effect Analysis
Study on the Screening of Anti‐Osteoporosis Components in Processed Epimedium‐Based on Spectrum‐Effect Analysis Abstract ABSTRACT Epimedium (EP) is a traditional Chinese medicine that has been used to treat osteoporosis for several years, but its mechanism of action is unclear. We used ultrahigh‐performance liquid chro...
PMC6304835
core_pubmed_pmc
Bioinformatic and Metabolomic Analysis Reveal Intervention Effects of Chicory in a Quail Model of Hyperuricemia
Bioinformatic and Metabolomic Analysis Reveal Intervention Effects of Chicory in a Quail Model of Hyperuricemia Abstract Background . Hyperuricemia (HUA) is a kind of a metabolic disease that seriously threatens human health worldwide. Chicory, a natural herbal medicine, has an obvious effect of reducing uric acid. The...
PMC7811981
core_pubmed_pmc
The Effect of Verapamil, a P-gp Inhibitor, on the Pharmacokinetics, Safety, and Tolerability of Omadacycline in Healthy Adults: A Phase I, Open-Label, Single-Sequence Study
The Effect of Verapamil, a P-gp Inhibitor, on the Pharmacokinetics, Safety, and Tolerability of Omadacycline in Healthy Adults: A Phase I, Open-Label, Single-Sequence Study Abstract Background Omadacycline is a semisynthetic aminomethylcycline antibacterial derived from the tetracycline class. It is approved in the USA...
PMC8929097
core_pubmed_pmc
Permeability of Gemcitabine and PBPK Modeling to Assess Oral Administration
Permeability of Gemcitabine and PBPK Modeling to Assess Oral Administration Abstract Abstract Gemcitabine is a nucleoside analog effective against several solid tumors. Standard treatment consists of an intravenous infusion over 30 min. This is an invasive, uncomfortable and often painful method, involving recurring vi...
PMC7359852
core_pubmed_pmc
Naturally Occurring Cardenolides Affecting Schistosoma mansoni
Naturally Occurring Cardenolides Affecting Schistosoma mansoni Abstract Schistosomiasis is a neglected tropical disease of considerable public health burden. We recently discovered a micromolar activity of several cardenolides against newly transformed schistosomula (NTS) of the parasitic flatworm Schistosoma mansoni i...
PMC11383896
core_pubmed_pmc
Identification of novel natural compounds against CFTR p.Gly628Arg pathogenic variant
Identification of novel natural compounds against CFTR p.Gly628Arg pathogenic variant Abstract Abstract Cystic fibrosis transmembrane conductance regulator (CFTR) protein is an ion channel found in numerous epithelia and controls the flow of water and salt across the epithelium. The aim of our study to find natural com...
PMC3817375
core_pubmed_pmc
Application of Physiologically Based Pharmacokinetic Modeling to Predict Acetaminophen Metabolism and Pharmacokinetics in Children
Application of Physiologically Based Pharmacokinetic Modeling to Predict Acetaminophen Metabolism and Pharmacokinetics in Children Abstract Acetaminophen (APAP) is a widely used analgesic and antipyretic drug that undergoes extensive phase I and II metabolism. To better understand the kinetics of this process and to ch...
PMC10319279
core_pubmed_pmc
The Comparative Bioavailability of Fluticasone and Azelastine Delivered as a Single Fixed Dose Combination (MP-AzeFlu) in Comparison to Two Different Formulations of Azelastine and Fluticasone Propionate Following Intranasal Administration in Healthy Chinese Volunteers
The Comparative Bioavailability of Fluticasone and Azelastine Delivered as a Single Fixed Dose Combination (MP-AzeFlu) in Comparison to Two Different Formulations of Azelastine and Fluticasone Propionate Following Intranasal Administration in Healthy Chinese Volunteers Abstract Objective Two studies (Study I and Study ...
PMC6748616
core_pubmed_pmc
Discovery of high affinity, pan-allelic, and pan-mammalian reactive antibodies against the myeloid checkpoint receptor SIRPα
Discovery of high affinity, pan-allelic, and pan-mammalian reactive antibodies against the myeloid checkpoint receptor SIRPα Abstract ABSTRACT Targeting the CD47-signal-regulatory protein α (SIRPα) pathway represents a novel therapeutic approach to enhance anti-cancer immunity by promoting both innate and adaptive immu...
PMC5555689
core_pubmed_pmc
The use of 18 F-Fluoro-deoxy-glucose positron emission tomography ( 18 F-FDG PET) as a non-invasive pharmacodynamic biomarker to determine the minimally pharmacologically active dose of AZD8835, a novel PI3Kα inhibitor
The use of 18 F-Fluoro-deoxy-glucose positron emission tomography ( 18 F-FDG PET) as a non-invasive pharmacodynamic biomarker to determine the minimally pharmacologically active dose of AZD8835, a novel PI3Kα inhibitor Abstract Abstract Background The phosphatidyl inositol 3 kinase (PI3K), AKT and mammalian target of r...
PMC12666428
core_pubmed_pmc
Tailored management of chronic bacterial prostatitis with sequential fluoroquinolones and adverse effect mitigation strategies: A case report
Tailored management of chronic bacterial prostatitis with sequential fluoroquinolones and adverse effect mitigation strategies: A case report Abstract Chronic bacterial prostatitis (CBP) presents diagnostic and therapeutic challenges, particularly in patients with drug allergies and atypical symptom profiles. This case...
PMC6487098
core_pubmed_pmc
Effect of Short-Course Oral Ciprofloxacin on Isoflavone Pharmacokinetics following Soy Milk Ingestion in Healthy Postmenopausal Women
Effect of Short-Course Oral Ciprofloxacin on Isoflavone Pharmacokinetics following Soy Milk Ingestion in Healthy Postmenopausal Women Abstract Abstract Soy isoflavones have several potential benefits related to postmenopausal health. Isoflavone glycosides, found predominantly in nonfermented soy products, e.g., soy mil...
PMC11676624
core_pubmed_pmc
Therapeutic Drug Monitoring of Low Methotrexate Doses for Drug Exposure and Adherence Assessment—Pre-Analytical Variables, Bioanalytical Issues, and Current Clinical Applications
Therapeutic Drug Monitoring of Low Methotrexate Doses for Drug Exposure and Adherence Assessment—Pre-Analytical Variables, Bioanalytical Issues, and Current Clinical Applications Abstract Methotrexate (MTX) is an antifolic agent used in the first line of anti-inflammatory disease treatment and some oncologic issues. Th...
PMC12777573
core_pubmed_pmc
Population pharmacokinetics and dose optimization of piperacillin-tazobactam in premature and term neonates with severe infections
Population pharmacokinetics and dose optimization of piperacillin-tazobactam in premature and term neonates with severe infections Abstract ABSTRACT Piperacillin-tazobactam is widely used off-label in neonates for the empirical treatment of severe infections, resulting in diverse dosing regimens across clinical setting...
PMC12223600
core_pubmed_pmc
Pharmacokinetic Simulation of Optimal Lopinavir and Ritonavir Dose Combination for COVID-19: Boosting Lopinavir With Ritonavir
Pharmacokinetic Simulation of Optimal Lopinavir and Ritonavir Dose Combination for COVID-19: Boosting Lopinavir With Ritonavir Abstract Background/Aim Lopinavir (LPV) combined with ritonavir (LPV/r) was initially developed to treat human immunodeficiency virus (HIV) infection and was subsequently repurposed to treat co...
PMC6804494
core_pubmed_pmc
Structural simplification: an efficient strategy in lead optimization
Structural simplification: an efficient strategy in lead optimization Abstract Abstract The trend toward designing large hydrophobic molecules for lead optimization is often associated with poor drug-likeness and high attrition rates in drug discovery and development. Structural simplification is a powerful strategy fo...
PMC9286649
core_pubmed_pmc
Sarecycline treatment for acne vulgaris: Rationale for weight‐based dosing and limited impact of food intake on clinical efficacy
Sarecycline treatment for acne vulgaris: Rationale for weight‐based dosing and limited impact of food intake on clinical efficacy Abstract Abstract Tetracycline‐class antibiotics are frequently prescribed by dermatologists, commonly for acne vulgaris. Gastrointestinal absorption of first and second‐generation tetracycl...
PMC10987731
core_pubmed_pmc
The pharmacokinetics and pharmacodynamics of fentanyl administered via transdermal patch in horses
The pharmacokinetics and pharmacodynamics of fentanyl administered via transdermal patch in horses Abstract Introduction Understanding the pharmacokinetics and pharmacodynamics of fentanyl in horses is crucial for optimizing pain management strategies in veterinary medicine. Methods Six adult horses were enrolled in a ...
PMC10193918
core_pubmed_pmc
Hyaluronic acid-based nanoparticles to deliver drugs to the ocular posterior segment
Hyaluronic acid-based nanoparticles to deliver drugs to the ocular posterior segment Abstract Abstract Ocular posterior segment diseases such as uveitis, X-linked juvenile retinoschisis, or age-related macular degeneration usually result in progressive and irreversible vision loss. Although intravitreal injection is th...
PMC7236601
core_pubmed_pmc
Pharmacodynamic Response to Anti-thyroid Drugs in Graves' Hyperthyroidism
Pharmacodynamic Response to Anti-thyroid Drugs in Graves' Hyperthyroidism Abstract Objective: Graves' disease is the commonest cause of hyperthyroidism in populations with sufficient dietary iodine intake. Anti-thyroid drugs (ATD) are often used as the initial treatment for Graves' hyperthyroidism, however there is a p...
PMC5053726
core_pubmed_pmc
The novel tankyrase inhibitor (AZ1366) enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance
The novel tankyrase inhibitor (AZ1366) enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance Abstract Background Dysregulation of the canonical Wnt signaling pathway has been implicated in colorectal cancer (CRC) development as well as incipient stages of malignant transformat...
PMC11263240
core_pubmed_pmc
Pharmacokinetic Modeling of the Effect of Tariquidar on Ondansetron Disposition into the Central Nervous System
Pharmacokinetic Modeling of the Effect of Tariquidar on Ondansetron Disposition into the Central Nervous System Abstract Purpose Serotonin (5-HT 3 ) receptor antagonists are promising agents for treatment of neuropathic pain. However, insufficient drug exposure at the central nervous system (CNS) might result in lack o...
PMC6630319
core_pubmed_pmc
Flaxseed Lignans as Important Dietary Polyphenols for Cancer Prevention and Treatment: Chemistry, Pharmacokinetics, and Molecular Targets
Flaxseed Lignans as Important Dietary Polyphenols for Cancer Prevention and Treatment: Chemistry, Pharmacokinetics, and Molecular Targets Abstract Abstract Cancer causes considerable morbidity and mortality across the world. Socioeconomic, environmental, and lifestyle factors contribute to the increasing cancer prevale...
PMC3185019
core_pubmed_pmc
Cellular pharmacokinetic and pharmacodynamic analyses of ethacrynic acid: Implications in topical drug delivery in the eye
Cellular pharmacokinetic and pharmacodynamic analyses of ethacrynic acid: Implications in topical drug delivery in the eye Abstract Purpose Ethacrynic acid (ECA) is a potential trabecular meshwork (TM) drug that has shown promising results in preclinical studies for treatment of primary open-angle glaucoma. However, to...
PMC6857112
core_pubmed_pmc
Influence of the OATP Polymorphism on the Population Pharmacokinetics of Methotrexate in Chinese Patients
Influence of the OATP Polymorphism on the Population Pharmacokinetics of Methotrexate in Chinese Patients Abstract Background: The Pharmacokinetics of Methotrexate (MTX) has been reported to show significant inter-subject variability. MTX is metabolized by SHMT1 and transported by OATP1B1 and OATP1B3 both of which show...
PMC5896717
core_pubmed_pmc
Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan‐Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors
Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan‐Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors Abstract Abstract Lessons Learned. A phase I study of the pan‐class I phosphoinositide 3‐kinase inhibitor pilaralisib (in capsule formulation) in advanced solid tumors established the maximum toler...
PMC9789683
core_pubmed_pmc
Effect of Rifampicin on the Pharmacokinetics of Evogliptin in Healthy Volunteers
Effect of Rifampicin on the Pharmacokinetics of Evogliptin in Healthy Volunteers Abstract Abstract Purpose Evogliptin (DA-1229) is a novel, potent, and selective dipeptidyl peptidase 4 (DPP-4) inhibitor for treating type 2 diabetes mellitus. This study investigates the effect of rifampicin on evogliptin pharmacokinetic...
PMC12964354
core_pubmed_pmc
A Review of Alpha‑2 Adrenergic Agents Implicated in Opioid Use Disorder
A Review of Alpha‑2 Adrenergic Agents Implicated in Opioid Use Disorder Abstract Opioid use disorder (OUD) has been recognized for many years as a leading public health emergency in the United States, costing almost 80,000 Americans their lives in 2023. Recently, fentanyl, the predominant synthetic opioid implicated in...
PMC11241800
core_pubmed_pmc
Aprotinin (II): Inhalational Administration for the Treatment of COVID-19 and Other Viral Conditions
Aprotinin (II): Inhalational Administration for the Treatment of COVID-19 and Other Viral Conditions Abstract Aprotinin is a broad-spectrum inhibitor of human proteases that has been approved for the treatment of bleeding in single coronary artery bypass surgery because of its potent antifibrinolytic actions. Following...
PMC10684710
core_pubmed_pmc
The Pharmacokinetics of the Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone
The Pharmacokinetics of the Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone Abstract Abstract Finerenone, a selective and nonsteroidal antagonist of the mineralocorticoid receptor, has received regulatory approval with the indication of cardiorenal protection in patients with chronic kidney disease associ...
PMC4936002
core_pubmed_pmc
OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens
OptiMal-PK: an internet-based, user-friendly interface for the mathematical-based design of optimized anti-malarial treatment regimens Abstract Abstract Background The search for highly effective anti-malarial therapies has gathered pace and recent years have seen a number of promising single and combined therapies rea...
PMC7814539
core_pubmed_pmc
Plasma levels of a methadone constant rate infusion and their corresponding effects on thermal and mechanical nociceptive thresholds in dogs
Plasma levels of a methadone constant rate infusion and their corresponding effects on thermal and mechanical nociceptive thresholds in dogs Abstract Background The present study aimed to collect pharmacokinetic data of a methadone continuous rate infusion (CRI) and to investigate its effect on mechanical and thermal n...
PMC8035073
core_pubmed_pmc
Comparison of pharmacokinetics of omega-3 fatty acid supplements in monoacylglycerol or ethyl ester in humans: a randomized controlled trial
Comparison of pharmacokinetics of omega-3 fatty acid supplements in monoacylglycerol or ethyl ester in humans: a randomized controlled trial Abstract Background A diet low in omega-3 fatty acids (n-3 FA) results in low plasma concentrations of docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), the two main lon...
PMC9583757
core_pubmed_pmc
Effect of drug-to-lipid ratio on nanodisc-based tenofovir drug delivery to the brain for HIV-1 infection
Effect of drug-to-lipid ratio on nanodisc-based tenofovir drug delivery to the brain for HIV-1 infection Abstract Background Combination antiretroviral therapy has significantly advanced HIV-1 infection treatment. However, HIV-1 remains persistent in the brain; the inaccessibility of the blood–brain barrier allows for ...
PMC8624019
core_pubmed_pmc
In Vitro Pharmacokinetic/Pharmacodynamic Modelling and Simulation of Amphotericin B against Candida auris
In Vitro Pharmacokinetic/Pharmacodynamic Modelling and Simulation of Amphotericin B against Candida auris Abstract Abstract The aims of this study were to characterize the antifungal activity of amphotericin B against Candida auris in a static in vitro system and to evaluate different dosing schedules and MIC scenarios...
PMC5871679
core_pubmed_pmc
Gut Microbiota-Regulated Pharmacokinetics of Berberine and Active Metabolites in Beagle Dogs After Oral Administration
Gut Microbiota-Regulated Pharmacokinetics of Berberine and Active Metabolites in Beagle Dogs After Oral Administration Abstract Abstract Berberine (BBR) is considered a multi-target drug that has significant advantages. In contrast to its significant pharmacological effects in clinic, the plasma level of BBR is very lo...
PMC5590451
core_pubmed_pmc
Nonstandard Finite Difference Method Applied to a Linear Pharmacokinetics Model
Nonstandard Finite Difference Method Applied to a Linear Pharmacokinetics Model Abstract We extend the nonstandard finite difference method of solution to the study of pharmacokinetic–pharmacodynamic models. Pharmacokinetic (PK) models are commonly used to predict drug concentrations that drive controlled intravenous (...
PMC9913742
core_pubmed_pmc
Feeding Management and Albendazole Pharmacokinetics in Pigs
Feeding Management and Albendazole Pharmacokinetics in Pigs Abstract Abstract Simple Summary Helminth parasite infections have a significant impact on the efficiency of swine production as a consequence of the reduced feed conversion and weight gain and the condemnation of affected organs after slaughter. Parasite cont...
PMC10338611
core_pubmed_pmc
Predicting Chemotherapy Distribution into Breast Milk for Breastfeeding Women Using a Population Pharmacokinetic Approach
Predicting Chemotherapy Distribution into Breast Milk for Breastfeeding Women Using a Population Pharmacokinetic Approach Abstract Background and Objective Information on the distribution of chemotherapeutic drugs to breast milk is scarce, and reports are limited to small sample sizes. Anecdotal pharmacokinetic data ha...
PMC6418145
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic actions of clozapine-N-oxide, clozapine, and compound 21 in DREADD-based chemogenetics in mice
Pharmacokinetic and pharmacodynamic actions of clozapine-N-oxide, clozapine, and compound 21 in DREADD-based chemogenetics in mice Abstract Muscarinic Designer Receptors Exclusively Activated by Designer Drugs (DREADD) gated by clozapine-N-oxide (CNO) allow selective G-protein cascade activation in genetically specifie...
PMC8724961
core_pubmed_pmc
Pharmacokinetics and analytical determination of acyclovir in Asian elephant calves ( Elephas maximus )
Pharmacokinetics and analytical determination of acyclovir in Asian elephant calves ( Elephas maximus ) Abstract Highlights • Pharmacokinetic and bioavailability data of acyclovir following intravenous and oral administration are reported for Asian elephant calves. • Data represent the first comprehensive LC-MS/MS anal...
PMC7775851
core_pubmed_pmc
Development of a UHPLC-MS/MS method for the quantification of ilaprazole enantiomers in rat plasma and its pharmacokinetic application
Development of a UHPLC-MS/MS method for the quantification of ilaprazole enantiomers in rat plasma and its pharmacokinetic application Abstract In Korea and China, ilaprazole is a widely used proton pump inhibitor in the treatment of gastric ulcers. In this study, a specific and sensitive LC-MS/MS method has been devel...
PMC11480897
core_pubmed_pmc
Challenges and Opportunities for Consideration of Efavirenz Drug Repurposing for Alzheimer’s Disease Therapeutics
Challenges and Opportunities for Consideration of Efavirenz Drug Repurposing for Alzheimer’s Disease Therapeutics Abstract Therapeutic research and development for Alzheimer’s disease (AD) has been an area of intense research to alleviate memory loss and neurodegeneration. There is growing interest in drug repositionin...
PMC10432867
core_pubmed_pmc
A long‐acting GDF15 analog causes robust, sustained weight loss and reduction of food intake in an obese nonhuman primate model
A long‐acting GDF15 analog causes robust, sustained weight loss and reduction of food intake in an obese nonhuman primate model Abstract Abstract Growth Differentiation Factor‐15 (GDF15) is a circulating polypeptide linked to cellular stress and metabolic adaptation. GDF15's half‐life is ~3 h and activates the glial ce...
PMC9809415
core_pubmed_pmc
Formulation and characterization of lamotrigine nasal insert targeted brain for enhanced epilepsy treatment
Formulation and characterization of lamotrigine nasal insert targeted brain for enhanced epilepsy treatment Abstract Abstract Lamotrigine. (LMT) is a triazine drug has an antiepileptic effect but with low water solubility, dissolution rate and thus therapeutic effect. Spanlastics are nano-vesicular carriers’ act as sit...
PMC10304221
core_pubmed_pmc
Pharmacokinetic and Biomarker Quantification Studies on Vancomycin-Loaded PEGylated Liposomes and Its Potential to Reduce Vancomycin-Induced Kidney Injury: A Rat Study
Pharmacokinetic and Biomarker Quantification Studies on Vancomycin-Loaded PEGylated Liposomes and Its Potential to Reduce Vancomycin-Induced Kidney Injury: A Rat Study Abstract Abstract Vancomycin is a commonly used antibiotic in hospital settings, especially against Methicillin-resistant staphylococcus aureus (MRSA). ...
PMC12091844
core_pubmed_pmc
Corrin Ring Modification in Peptide Drug Development – a Brief History of “Corrination”
Corrin Ring Modification in Peptide Drug Development – a Brief History of “Corrination” Abstract Abstract Recently, the term “corrination” was coined to describe the conjugate modification of a peptide, protein, small molecule, or radionuclide with a corrin ring‐containing molecule. By exploiting the innate chemicophys...
PMC11194020
core_pubmed_pmc
Targeted Delivery of Macrophage Membrane Biomimetic Liposomes Through Intranasal Administration for Treatment of Ischemic Stroke
Targeted Delivery of Macrophage Membrane Biomimetic Liposomes Through Intranasal Administration for Treatment of Ischemic Stroke Abstract Abstract Purpose Ginsenoside Rg3 (Rg3) and Panax notoginseng saponins (PNS) can be used for ischemic stroke treatment, however, the lack of targeting to the ischemic region limits th...
PMC12678931
core_pubmed_pmc
Cardamonin as a potential anticancer agent: Preclinical insights and clinical implications
Cardamonin as a potential anticancer agent: Preclinical insights and clinical implications Abstract Cardamonin is a natural chalcone that has been extensively investigated for its anticancer activity. However, its clinical relevance is still not explicit, limiting its progression into clinical trials and highlighting a...
PMC8560754
core_pubmed_pmc
Bridging the gap between in silico and in vivo by modeling opioid disposition in a kidney proximal tubule microphysiological system
Bridging the gap between in silico and in vivo by modeling opioid disposition in a kidney proximal tubule microphysiological system Abstract Abstract Opioid overdose, dependence, and addiction are a major public health crisis. Patients with chronic kidney disease (CKD) are at high risk of opioid overdose, therefore nov...