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PMC4045546
core_pubmed_pmc
Quantification of Neocortical Slice Diffusion Characteristics Using Pharmacokinetic and Pharmacodynamic Modelling
Quantification of Neocortical Slice Diffusion Characteristics Using Pharmacokinetic and Pharmacodynamic Modelling Abstract Pharmacological brain slice experiments are complicated by the need to ensure adequate drug delivery deep into the healthy layers of the tissue. Because tissue slices have no blood supply, this is ...
PMC11925807
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics Evaluation of Ivonescimab, a Novel Bispecific Antibody Targeting PD‐1 and VEGF, in Chinese Patients With Advanced Solid Tumors
Safety, Pharmacokinetics, and Pharmacodynamics Evaluation of Ivonescimab, a Novel Bispecific Antibody Targeting PD‐1 and VEGF, in Chinese Patients With Advanced Solid Tumors Abstract ABSTRACT Background Ivonescimab (AK112) is a first‐in‐class bispecific antibody that simultaneously targets programmed death‐1 (PD‐1) and...
PMC4623742
core_pubmed_pmc
Synergistic anti-tumor therapy by a comb-like multifunctional antibody nanoarray with exceptionally potent activity
Synergistic anti-tumor therapy by a comb-like multifunctional antibody nanoarray with exceptionally potent activity Abstract Simultaneously blocking multiple mediators offers new hope for the treatment of complex diseases. However, the curative potential of current combination therapy by chronological administration of...
PMC11487780
core_pubmed_pmc
Association between exposure to proton pump inhibitors and delirium: a descriptive and disproportionality analysis of VigiBase
Association between exposure to proton pump inhibitors and delirium: a descriptive and disproportionality analysis of VigiBase Abstract Abstract Abstract Objectives Proton pump inhibitor (PPI) exposure can lead to hyponatraemia, which is a common cause of delirium. An association between PPI exposure and delirium witho...
PMC9399108
core_pubmed_pmc
Determining drug dose in the era of targeted therapies: playing it (un)safe?
Determining drug dose in the era of targeted therapies: playing it (un)safe? Abstract Abstract Targeted therapies against phosphatidylinositol 3-kinase (PI3K), Bruton’s tyrosine kinase (BTK), and B-cell lymphoma-2 (BCL-2) are approved for chronic lymphocytic leukemia (CLL). Since approval of the first-in-class drugs, n...
PMC5428631
core_pubmed_pmc
A previously published propofol–remifentanil response surface model does not predict patient response well in video-assisted thoracic surgery
A previously published propofol–remifentanil response surface model does not predict patient response well in video-assisted thoracic surgery Abstract Abstract Modern anesthesia usually employs a hypnotic and an analgesic to produce synergistic sedation and analgesia. Two remifentanil–propofol interaction response surf...
PMC10247930
core_pubmed_pmc
The effects of novel macrocyclic chelates on the targeting properties of the 68 Ga-labeled Gastrin releasing peptide receptor antagonist RM2
The effects of novel macrocyclic chelates on the targeting properties of the 68 Ga-labeled Gastrin releasing peptide receptor antagonist RM2 Abstract Background The gastrin-releasing peptide receptor (GRPr) is a molecular target for the visualization of prostate cancer. Bombesin (BN) analogs are short peptides with a h...
PMC9866283
core_pubmed_pmc
Pharmacokinetic Study of Triptolide Nanocarrier in Transdermal Drug Delivery System—Combination of Experiment and Mathematical Modeling
Pharmacokinetic Study of Triptolide Nanocarrier in Transdermal Drug Delivery System—Combination of Experiment and Mathematical Modeling Abstract Compared with traditional oral and injection administration, the transdermal administration of traditional Chinese medicine has distinctive characteristics and advantages, whi...
PMC6865853
core_pubmed_pmc
Lymphocyte pharmacodynamics are not associated with autoimmunity or efficacy after alemtuzumab
Lymphocyte pharmacodynamics are not associated with autoimmunity or efficacy after alemtuzumab Abstract Objective To examine the association between peripheral blood lymphocyte pharmacodynamics and autoimmune adverse events (AEs) or return of disease activity in alemtuzumab-treated patients with relapsing-remitting MS....
PMC5494778
core_pubmed_pmc
Comparative Pharmacokinetics and Bioavailability of Three Ephedrines in Rat after Oral Administration of Unprocessed and Honey-Fried Ephedra Extract by Response Surface Experimental Design
Comparative Pharmacokinetics and Bioavailability of Three Ephedrines in Rat after Oral Administration of Unprocessed and Honey-Fried Ephedra Extract by Response Surface Experimental Design Abstract Abstract Ephedra have been used as a common traditional Chinese medicine for thousands of years. However, the perspiration...
PMC8032567
core_pubmed_pmc
An open-label, positron emission tomography study of the striatal D 2 /D 3 receptor occupancy and pharmacokinetics of single-dose oral brexpiprazole in healthy participants
An open-label, positron emission tomography study of the striatal D 2 /D 3 receptor occupancy and pharmacokinetics of single-dose oral brexpiprazole in healthy participants Abstract Abstract Purpose The aim of this Phase 1, open-label, positron emission tomography (PET) study was to determine the degree of striatal D 2...
PMC7719375
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of TD‐0714, a Novel Potent Neprilysin Inhibitor in Healthy Adult and Elderly Subjects
Safety, Pharmacokinetics, and Pharmacodynamics of TD‐0714, a Novel Potent Neprilysin Inhibitor in Healthy Adult and Elderly Subjects Abstract TD‐0714 is an orally active, potent, and selective inhibitor of human neprilysin (NEP) in development for the treatment of chronic heart failure. Oral administration of TD‐0714 i...
PMC5765031
core_pubmed_pmc
Biotransformation and tissue distribution of protopine and allocryptopine and effects of Plume Poppy Total Alkaloid on liver drug-metabolizing enzymes
Biotransformation and tissue distribution of protopine and allocryptopine and effects of Plume Poppy Total Alkaloid on liver drug-metabolizing enzymes Abstract Abstract In this study, the biotransformation in the plasma, urine and feces of rats following oral administration of protopine (PRO) and allocryptopine (ALL)we...
PMC10148140
core_pubmed_pmc
Repositioning Cannabinoids and Terpenes as Novel EGFR-TKIs Candidates for Targeted Therapy Against Cancer: A virtual screening model using CADD and biophysical simulations
Repositioning Cannabinoids and Terpenes as Novel EGFR-TKIs Candidates for Targeted Therapy Against Cancer: A virtual screening model using CADD and biophysical simulations Abstract Abstract This study examines the potential of Cannabis sativa L. plants to be repurposed as therapeutic agents for cancer treatment through...
PMC10976160
core_pubmed_pmc
Comparative Pharmacokinetics Research of 13 Bioactive Components of Jieyu Pills in Control and Attention Deficit Hyperactivity Disorder Model Rats Based on UPLC-Orbitrap Fusion MS
Comparative Pharmacokinetics Research of 13 Bioactive Components of Jieyu Pills in Control and Attention Deficit Hyperactivity Disorder Model Rats Based on UPLC-Orbitrap Fusion MS Abstract Jieyu Pills (JYPs), a Chinese medicine consisting of 10 herbal elements, have displayed promising clinical effectiveness and low by...
PMC12385050
core_pubmed_pmc
Novel Neuroactive Steroid Analogs and Voltage-Dependent Blockers of Ca V 3.2 Currents, B372 and YX23, Are Effective Anti-Nociceptives with Diminished Sedative Properties in Intact Female Mice
Novel Neuroactive Steroid Analogs and Voltage-Dependent Blockers of Ca V 3.2 Currents, B372 and YX23, Are Effective Anti-Nociceptives with Diminished Sedative Properties in Intact Female Mice Abstract Although opioids are effective in treating pain, they cause serious side effects. The use of regional anesthesia, altho...
PMC9312011
core_pubmed_pmc
Prophylactic Anti-Osteoporotic Effect of Matricaria chamomilla L. Flower Using Steroid-Induced Osteoporosis in Rat Model and Molecular Modelling Approaches
Prophylactic Anti-Osteoporotic Effect of Matricaria chamomilla L. Flower Using Steroid-Induced Osteoporosis in Rat Model and Molecular Modelling Approaches Abstract Abstract The anti-osteoporotic activity of ethanol extract from the Matricaria chamomilla L. flower was evaluated using steroid-induced osteoporosis in a r...
PMC3833229
core_pubmed_pmc
A dose-escalating phase I of imatinib mesylate with fixed dose of metronomic cyclophosphamide in targeted olid tumours
A dose-escalating phase I of imatinib mesylate with fixed dose of metronomic cyclophosphamide in targeted olid tumours Abstract Abstract Background: Preclinical findings suggest that imatinib mesylate (IM) and metronomic cyclophosphamide (MC) combination provides synergistic antiangiogenic activity on both pericytes an...
PMC7507140
core_pubmed_pmc
Image‐guided mathematical modeling for pharmacological evaluation of nanomaterials and monoclonal antibodies
Image‐guided mathematical modeling for pharmacological evaluation of nanomaterials and monoclonal antibodies Abstract Abstract While plasma concentration kinetics has traditionally been the predictor of drug pharmacological effects, it can occasionally fail to represent kinetics at the site of action, particularly for ...
PMC12203789
core_pubmed_pmc
Escherichia coli producing AmpC DHA-1 bacteraemia in neutropenic leukemic patient: continuous infusion ceftazidime/avibactam as a carbapenem sparing regimen
Escherichia coli producing AmpC DHA-1 bacteraemia in neutropenic leukemic patient: continuous infusion ceftazidime/avibactam as a carbapenem sparing regimen Abstract Abstract Background Escherichia coli resistant to third-generation cephalosporins, primarily due to the production of ESBLs and AmpC β-lactamases, poses a...
PMC4641511
core_pubmed_pmc
Membrane-stabilizing copolymers confer marked protection to dystrophic skeletal muscle in vivo
Membrane-stabilizing copolymers confer marked protection to dystrophic skeletal muscle in vivo Abstract Abstract Duchenne muscular dystrophy (DMD) is a fatal disease of striated muscle deterioration. A unique therapeutic approach for DMD is the use of synthetic membrane stabilizers to protect the fragile dystrophic sar...
PMC10121042
core_pubmed_pmc
A single-dose, randomized crossover study in healthy Chinese subjects to evaluate pharmacokinetics and bioequivalence of two capsules of calcium dobesilate 0.5 g under fasting and fed conditions
A single-dose, randomized crossover study in healthy Chinese subjects to evaluate pharmacokinetics and bioequivalence of two capsules of calcium dobesilate 0.5 g under fasting and fed conditions Abstract Objectives To compare the rate and extent of absorption of a launched generic calcium dobesilate capsule versus the ...
PMC6709789
core_pubmed_pmc
Effect of hepatic and renal impairment on the pharmacokinetics of olanzapine and samidorphan given in combination as a bilayer tablet
Effect of hepatic and renal impairment on the pharmacokinetics of olanzapine and samidorphan given in combination as a bilayer tablet Abstract Abstract Background A combination of olanzapine and samidorphan (OLZ/SAM) is in development to provide the established antipsychotic efficacy of olanzapine while mitigating olan...
PMC10892410
core_pubmed_pmc
[ 18 F]Fluspidine—A PET Tracer for Imaging of σ 1 Receptors in the Central Nervous System
[ 18 F]Fluspidine—A PET Tracer for Imaging of σ 1 Receptors in the Central Nervous System Abstract Abstract σ 1 receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer’s disease, and depression. Spirocyclic piperidines represent a promising class of pote...
PMC12393001
core_pubmed_pmc
Who to Enroll in Parkinson Disease Prevention Trials?
Who to Enroll in Parkinson Disease Prevention Trials? Abstract Therapies that prevent the occurrence of Parkinson disease (PD) (primary prevention) or mitigate the progression of symptoms in those with early disease (secondary prevention) are a critical unmet need in disease management. Despite great promise, PD preven...
PMC5967376
core_pubmed_pmc
An ex vivo human aqueous humor-concentration comparison of two commercial bromfenac formulations
An ex vivo human aqueous humor-concentration comparison of two commercial bromfenac formulations Abstract Purpose The purpose of this study was to quantify the concentration of bromfenac in the aqueous humor utilizing high-performance liquid chromatography mass spectrometry between two commercial nonsteroidal anti-infl...
PMC8841436
core_pubmed_pmc
Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168)
Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168) Abstract Abstract Bruton’s tyrosine kinase (BTK), expressed in B cells and cells of innate immunity, including microglia, is an essential signaling element downstream of the B‐cell receptor and Fc‐...
PMC11060137
core_pubmed_pmc
A Phase I Study of KIN-3248, an Irreversible Small-molecule Pan-FGFR Inhibitor, in Patients with Advanced FGFR2/3-driven Solid Tumors
A Phase I Study of KIN-3248, an Irreversible Small-molecule Pan-FGFR Inhibitor, in Patients with Advanced FGFR2/3-driven Solid Tumors Abstract Abstract Purpose: Despite efficacy of approved FGFR inhibitors, emergence of polyclonal secondary mutations in the FGFR kinase domain leads to acquired resistance. KIN-3248 is a...
PMC5762490
core_pubmed_pmc
Analytical methods for determination of terbinafine hydrochloride in pharmaceuticals and biological materials ☆
Analytical methods for determination of terbinafine hydrochloride in pharmaceuticals and biological materials ☆ Abstract Terbinafine is a new powerful antifungal agent indicated for both oral and topical treatment of mycosessince. It is highly effective in the treatment of determatomycoses. The chemical and pharmaceuti...
PMC9219867
core_pubmed_pmc
Evaluation of a Meropenem and Piperacillin Monitoring Program in Intensive Care Unit Patients Calls for the Regular Assessment of Empirical Targets and Easy-to-Use Dosing Decision Tools
Evaluation of a Meropenem and Piperacillin Monitoring Program in Intensive Care Unit Patients Calls for the Regular Assessment of Empirical Targets and Easy-to-Use Dosing Decision Tools Abstract Abstract The drug concentrations targeted in meropenem and piperacillin/tazobactam therapy also depend on the susceptibility ...
PMC9870685
core_pubmed_pmc
Evaluating the Efficacy, Toxicity and Pharmacokinetic Profile of Oral Busulfan in Allogeneic Stem Cell Transplant Patients
Evaluating the Efficacy, Toxicity and Pharmacokinetic Profile of Oral Busulfan in Allogeneic Stem Cell Transplant Patients Abstract Background: Oral busulfan and intravenous cyclophosphamide (Bu/Cy) are common myeloablative preparations used in allogeneic hematopoietic stem cell transplantation (HSCT). Herein, we inves...
PMC7642461
core_pubmed_pmc
Pharmacokinetic and Efficacy Study of Acyclovir Against Cyprinid Herpesvirus 3 in Cyprinus carpio
Pharmacokinetic and Efficacy Study of Acyclovir Against Cyprinid Herpesvirus 3 in Cyprinus carpio Abstract Cyprinid Herpesvirus 3 (CyHV-3), more commonly known as Koi Herpesvirus (KHV), is a re-emergent virus causing acute systemic infection with high mortality rates in koi fish ( Cyprinus carpio ). Survivors from outb...
PMC8010964
core_pubmed_pmc
Randomized and dose-escalation trials of recombinant human serum albumin /granulocyte colony-stimulating factor in patients with breast cancer receiving anthracycline-containing chemotherapy
Randomized and dose-escalation trials of recombinant human serum albumin /granulocyte colony-stimulating factor in patients with breast cancer receiving anthracycline-containing chemotherapy Abstract Abstract Background To evaluate the efficacy and safety of recombinant human serum albumin /granulocyte colony-stimulati...
PMC9090356
core_pubmed_pmc
PLGA sustained-release microspheres loaded with an insoluble small-molecule drug: microfluidic-based preparation, optimization, characterization, and evaluation in vitro and in vivo
PLGA sustained-release microspheres loaded with an insoluble small-molecule drug: microfluidic-based preparation, optimization, characterization, and evaluation in vitro and in vivo Abstract Abstract Microspheres play an important role in controlling drug delivery and release rate accurately. To realize the sustainable...
PMC5652740
core_pubmed_pmc
Inhibition of HIV-1 infection in humanized mice and metabolic stability of protein phosphatase-1-targeting small molecule 1E7-03
Inhibition of HIV-1 infection in humanized mice and metabolic stability of protein phosphatase-1-targeting small molecule 1E7-03 Abstract Abstract We recently identified the protein phosphatase-1 - targeting compound, 1E7-03 which inhibited HIV-1 in vitro . Here, we investigated the effect of 1E7-03 on HIV-1 infection ...
PMC10433970
core_pubmed_pmc
Neutropenic Rat Thigh Infection Model for Evaluation of the Pharmacokinetics/Pharmacodynamics of Anti-Infectives
Neutropenic Rat Thigh Infection Model for Evaluation of the Pharmacokinetics/Pharmacodynamics of Anti-Infectives Abstract ABSTRACT The neutropenic mouse infection model is extensively used to characterize the pharmacokinetics/pharmacodynamics (PK/PD) of anti-infective agents. However, it is difficult to evaluate agents...
PMC9019179
core_pubmed_pmc
The use of pharmacogenetics to increase the safety of colorectal cancer patients treated with fluoropyrimidines
The use of pharmacogenetics to increase the safety of colorectal cancer patients treated with fluoropyrimidines Abstract Abstract Fluoropyrimidines (FP) are given in the combination treatment of the advanced disease or as monotherapy in the neo-adjuvant and adjuvant treatment of colorectal cancerand other solid tumors ...
PMC4817977
core_pubmed_pmc
The qEEG Signature of Selective NMDA NR2B Negative Allosteric Modulators; A Potential Translational Biomarker for Drug Development
The qEEG Signature of Selective NMDA NR2B Negative Allosteric Modulators; A Potential Translational Biomarker for Drug Development Abstract Abstract The antidepressant activity of the N-methyl-D-aspartate (NMDA) receptor channel blocker, ketamine, has led to the investigation of negative allosteric modulators (NAMs) se...
PMC10049354
core_pubmed_pmc
Anti-Inflammatory Effects and Photo- and Neuro-Protective Properties of BIO203, a New Amide Conjugate of Norbixin, in Development for the Treatment of Age-Related Macular Degeneration (AMD)
Anti-Inflammatory Effects and Photo- and Neuro-Protective Properties of BIO203, a New Amide Conjugate of Norbixin, in Development for the Treatment of Age-Related Macular Degeneration (AMD) Abstract 9′- cis -norbixin (norbixin/BIO201) protects RPE cells against phototoxicity induced by blue light and N -retinylidene- N...
PMC7988592
core_pubmed_pmc
Pharmacogenetics–Based Preliminary Algorithm to Predict the Incidence of Infection in Patients Receiving Cytotoxic Chemotherapy for Hematological Malignancies: A Discovery Cohort
Pharmacogenetics–Based Preliminary Algorithm to Predict the Incidence of Infection in Patients Receiving Cytotoxic Chemotherapy for Hematological Malignancies: A Discovery Cohort Abstract Abstract Introduction: Infections in hematological cancer patients are common and usually life-threatening; avoiding them could decr...
PMC11581693
core_pubmed_pmc
Efficacy and Safety of Remdesivir in People With Impaired Kidney Function Hospitalized for COVID-19 Pneumonia: A Randomized Clinical Trial
Efficacy and Safety of Remdesivir in People With Impaired Kidney Function Hospitalized for COVID-19 Pneumonia: A Randomized Clinical Trial Abstract Abstract Background Few antiviral therapies have been studied in patients with coronavirus disease 2019 (COVID-19) and kidney impairment. Herein, the efficacy, safety, and ...
PMC7384059
core_pubmed_pmc
Bioequivalence and Bioavailability of an Orodispersible Tablet of Sildenafil Citrate in Healthy Chinese Male Subjects
Bioequivalence and Bioavailability of an Orodispersible Tablet of Sildenafil Citrate in Healthy Chinese Male Subjects Abstract Abstract Sildenafil citrate is approved to treat erectile dysfunction. An orally disintegrating tablet (ODT) of sildenafil citrate that does not require swallowing or administration with fluids...
PMC12247986
core_pubmed_pmc
A structure-based modelling approach identifies effective drug combinations for RAS-mutant acute myeloid leukemia
A structure-based modelling approach identifies effective drug combinations for RAS-mutant acute myeloid leukemia Abstract Abstract Mutations activating RAS/RAF/MEK/ERK signaling are associated with poor outcome in acute myeloid leukemia (AML), but therapeutic targeting of this pathway is challenging. Here, we employ a...
PMC6983510
core_pubmed_pmc
Lidocaine as treatment for neonatal seizures: Evaluation of previously developed population pharmacokinetic models and dosing regimen
Lidocaine as treatment for neonatal seizures: Evaluation of previously developed population pharmacokinetic models and dosing regimen Abstract Aims Lidocaine is used to treat neonatal seizures refractory to other anticonvulsants. It is effective, but also associated with cardiac toxicity. Previous studies have reported...
PMC5062580
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and efficacy of a small-molecule SMN2 splicing modifier in mouse models of spinal muscular atrophy
Pharmacokinetics, pharmacodynamics, and efficacy of a small-molecule SMN2 splicing modifier in mouse models of spinal muscular atrophy Abstract Spinal muscular atrophy (SMA) is caused by the loss or mutation of both copies of the survival motor neuron 1 ( SMN1 ) gene. The related SMN2 gene is retained, but due to alter...
PMC8615430
core_pubmed_pmc
β-Dystroglycan Restoration and Pathology Progression in the Dystrophic mdx Mouse: Outcome and Implication of a Clinically Oriented Study with a Novel Oral Dasatinib Formulation
β-Dystroglycan Restoration and Pathology Progression in the Dystrophic mdx Mouse: Outcome and Implication of a Clinically Oriented Study with a Novel Oral Dasatinib Formulation Abstract ROS-activated cSrc tyrosine kinase (TK) promotes the degradation of β-dystroglycan (β-DG), a dystrophin-glycoprotein complex component...
PMC12455456
core_pubmed_pmc
Pharmacokinetics and 180‐day safety of diazepam nasal spray in pediatric patients with epilepsy aged 2–5 years
Pharmacokinetics and 180‐day safety of diazepam nasal spray in pediatric patients with epilepsy aged 2–5 years Abstract Abstract Objective Benzodiazepine immediate‐use seizure medications (ISMs; also called rescue therapies) are used to treat seizure clusters/acute repetitive seizures in patients with epilepsy. In the ...
PMC12444152
core_pubmed_pmc
Association between tacrolimus blood levels and biopsy-proven acute cellular rejection in adult heart transplant recipients
Association between tacrolimus blood levels and biopsy-proven acute cellular rejection in adult heart transplant recipients Abstract Abstract Background Acute cellular rejection (ACR) is a common complication following heart transplantation (HTx). This study examined the association between tacrolimus whole-blood conce...
PMC4977286
core_pubmed_pmc
Inhibition of P-Glycoprotein and Multidrug Resistance-Associated Protein 2 Regulates the Hepatobiliary Excretion and Plasma Exposure of Thienorphine and Its Glucuronide Conjugate
Inhibition of P-Glycoprotein and Multidrug Resistance-Associated Protein 2 Regulates the Hepatobiliary Excretion and Plasma Exposure of Thienorphine and Its Glucuronide Conjugate Abstract Thienorphine (TNP) is a novel partial opioid agonist that has completed phase II clinical evaluation as a promising drug candidate f...
PMC10142183
core_pubmed_pmc
Optimization of polymyxin B regimens for the treatment of carbapenem-resistant organism nosocomial pneumonia: a real-world prospective study
Optimization of polymyxin B regimens for the treatment of carbapenem-resistant organism nosocomial pneumonia: a real-world prospective study Abstract Abstract Background Polymyxin B is the first-line therapy for Carbapenem-resistant organism (CRO) nosocomial pneumonia. However, clinical data for its pharmacokinetic/pha...
PMC12686966
core_pubmed_pmc
Da‐Bu‐Yin‐Wan and Qian‐Zheng‐San Alleviate Parkinson's Disease by Activating the Keap1/Nrf2/ HO ‐1 Pathway to Positively Regulate Oxidative Stress
Da‐Bu‐Yin‐Wan and Qian‐Zheng‐San Alleviate Parkinson's Disease by Activating the Keap1/Nrf2/ HO ‐1 Pathway to Positively Regulate Oxidative Stress Abstract ABSTRACT Background Parkinson's disease (PD) is a neurodegenerative disorder that worsens progressively. Different pathological mechanisms are involved in the progr...
PMC5546485
core_pubmed_pmc
Impact of chronic unpredicted mild stress-induced depression on repaglinide fate via glucocorticoid signaling pathway
Impact of chronic unpredicted mild stress-induced depression on repaglinide fate via glucocorticoid signaling pathway Abstract Abstract Chronic unpredicted mild stress (CUMS)-induced depression could alter the pharmacokinetics of many drugs in rats, however, the underlying mechanism is not clear. In this work we studie...
PMC5695007
core_pubmed_pmc
pH-Sensitive Nano-Complexes Overcome Drug Resistance and Inhibit Metastasis of Breast Cancer by Silencing Akt Expression
pH-Sensitive Nano-Complexes Overcome Drug Resistance and Inhibit Metastasis of Breast Cancer by Silencing Akt Expression Abstract Abstract The therapy of breast cancer is encumbered by drug resistance and metastasis, which can be due to a defective PI3K/AKT/mTOR signaling pathway. This study was aimed at improving the ...
PMC8541586
core_pubmed_pmc
In Silico Identification and Validation of Organic Triazole Based Ligands as Potential Inhibitory Drug Compounds of SARS-CoV-2 Main Protease
In Silico Identification and Validation of Organic Triazole Based Ligands as Potential Inhibitory Drug Compounds of SARS-CoV-2 Main Protease Abstract Abstract The SARS-CoV-2 virus is highly contagious to humans and has caused a pandemic of global proportions. Despite worldwide research efforts, efficient targeted thera...
PMC12196119
core_pubmed_pmc
Multifunctional Evaluation of Graphene Oxide–Sulfonamide Nanoconjugates: Antimicrobial, Antibiofilm, Cytocompatibility and Xenobiotic Metabolism Gene Expression Insight
Multifunctional Evaluation of Graphene Oxide–Sulfonamide Nanoconjugates: Antimicrobial, Antibiofilm, Cytocompatibility and Xenobiotic Metabolism Gene Expression Insight Abstract The clinical utility of sulfonamide antibiotics is increasingly challenged by antimicrobial resistance and pharmacokinetic limitations. In thi...
PMC5883056
core_pubmed_pmc
Virtual screening, Docking, ADMET and System Pharmacology studies on Garcinia caged Xanthone derivatives for Anticancer activity
Virtual screening, Docking, ADMET and System Pharmacology studies on Garcinia caged Xanthone derivatives for Anticancer activity Abstract Abstract Caged xanthones are bioactive compounds mainly derived from the Garcinia genus. In this study, a structure-activity relationship (SAR) of caged xanthones and their derivativ...
PMC6267706
core_pubmed_pmc
Exposure–response analysis and simulation of lenvatinib safety and efficacy in patients with radioiodine-refractory differentiated thyroid cancer
Exposure–response analysis and simulation of lenvatinib safety and efficacy in patients with radioiodine-refractory differentiated thyroid cancer Abstract Abstract Purpose Once-daily lenvatinib 24 mg is the approved dose for radioiodine-refractory differentiated thyroid cancer. In a phase 3 trial with lenvatinib, the s...
PMC8698120
core_pubmed_pmc
Multi-Injection Pharmacokinetics of Meloxicam in Kemp’s Ridley (Lepidochelys kempii ) and Green ( Chelonia mydas ) Sea Turtles after Subcutaneous Administration
Multi-Injection Pharmacokinetics of Meloxicam in Kemp’s Ridley (Lepidochelys kempii ) and Green ( Chelonia mydas ) Sea Turtles after Subcutaneous Administration Abstract Abstract Simple Summary Drug dosing in sea turtles is often extrapolated from other reptiles, mammals, and humans. A more accurate way to determine th...
PMC10941517
core_pubmed_pmc
Bioavailability of three novel oral, sustained‐release pellets, relative to an immediate‐release tablet containing 500 mg flucytosine: A randomized, open‐label, crossover study in healthy volunteers
Bioavailability of three novel oral, sustained‐release pellets, relative to an immediate‐release tablet containing 500 mg flucytosine: A randomized, open‐label, crossover study in healthy volunteers Abstract Abstract The opportunistic fungal infection cryptococcal meningoencephalitis is a major cause of death among peo...
PMC12304414
core_pubmed_pmc
Optimizing the Use of Cabotegravir Plus Rilpivirine Long-acting Therapy in HIV Care: Evidence, Implementation, and Unanswered Questions
Optimizing the Use of Cabotegravir Plus Rilpivirine Long-acting Therapy in HIV Care: Evidence, Implementation, and Unanswered Questions Abstract Abstract Cabotegravir plus rilpivirine long-acting (CAB + RPV-LA) injectable therapy marks a major milestone in HIV care, offering an efficacious, well-tolerated alternative t...
PMC6624406
core_pubmed_pmc
Methadone and buprenorphine pharmacokinetics and pharmacodynamics when coadministered with fostemsavir to opioid‐dependent, human immunodeficiency virus seronegative participants
Methadone and buprenorphine pharmacokinetics and pharmacodynamics when coadministered with fostemsavir to opioid‐dependent, human immunodeficiency virus seronegative participants Abstract Aims Regional human immunodeficiency virus (HIV) prevalence rates are high in people with history of injection drug use, including t...
PMC6969938
core_pubmed_pmc
The 1,10-Phenanthroline Ligand Enhances the Antiproliferative Activity of DNA-Intercalating Thiourea-Pd(II) and -Pt(II) Complexes Against Cisplatin-Sensitive and -Resistant Human Ovarian Cancer Cell Lines
The 1,10-Phenanthroline Ligand Enhances the Antiproliferative Activity of DNA-Intercalating Thiourea-Pd(II) and -Pt(II) Complexes Against Cisplatin-Sensitive and -Resistant Human Ovarian Cancer Cell Lines Abstract Abstract Ovarian cancer is the most lethal gynecological malignancy, often because of the frequent insurge...
PMC11773107
core_pubmed_pmc
Physiologically based pharmacokinetic modelling to predict potential drug–drug interactions of dersimelagon (MT‐7117)
Physiologically based pharmacokinetic modelling to predict potential drug–drug interactions of dersimelagon (MT‐7117) Abstract Abstract Aims Dersimelagon is a novel, investigational, orally administered, selective agonist of the melanocortin‐1 receptor that has demonstrated efficacy at increasing symptom‐free light exp...
PMC11653594
core_pubmed_pmc
Model-informed drug discovery and development approaches to inform clinical trial design and regulatory decisions: A primer for the MENA region
Model-informed drug discovery and development approaches to inform clinical trial design and regulatory decisions: A primer for the MENA region Abstract Model-Informed Drug Discovery and Development (MID3) represents a transformative approach in pharmaceutical research, integrating quantitative models to inform and opt...
PMC8230242
core_pubmed_pmc
Therapeutic Drug Monitoring of Second- and Third-Generation Antipsychotic Drugs—Influence of Smoking Behavior and Inflammation on Pharmacokinetics
Therapeutic Drug Monitoring of Second- and Third-Generation Antipsychotic Drugs—Influence of Smoking Behavior and Inflammation on Pharmacokinetics Abstract Abstract Both inflammation and smoking can influence a drug’s pharmacokinetic properties, i.e., its liberation, absorption, distribution, metabolism, and eliminatio...
PMC8161238
core_pubmed_pmc
Enrofloxacin Dose Optimization for the Treatment of Colibacillosis in Broiler Chickens Using a Drinking Behaviour Pharmacokinetic Model
Enrofloxacin Dose Optimization for the Treatment of Colibacillosis in Broiler Chickens Using a Drinking Behaviour Pharmacokinetic Model Abstract Enrofloxacin is frequently administered via drinking water for the treatment of colibacillosis in broiler chickens. However, the EMA/CVMP has urged to re-evaluate historically...
PMC8707652
core_pubmed_pmc
Intratracheally Inhalable Nifedipine-Loaded Chitosan-PLGA Nanocomposites as a Promising Nanoplatform for Lung Targeting: Snowballed Protection via Regulation of TGF-β/β-Catenin Pathway in Bleomycin-Induced Pulmonary Fibrosis
Intratracheally Inhalable Nifedipine-Loaded Chitosan-PLGA Nanocomposites as a Promising Nanoplatform for Lung Targeting: Snowballed Protection via Regulation of TGF-β/β-Catenin Pathway in Bleomycin-Induced Pulmonary Fibrosis Abstract Abstract Pulmonary fibrosis is a serious ailment that may progress to lung remodeling ...
PMC9224574
core_pubmed_pmc
Pharmacokinetics and Clinical Implications of Two Non-Tablet Oral Formulations of L-Thyroxine in Patients with Hypothyroidism
Pharmacokinetics and Clinical Implications of Two Non-Tablet Oral Formulations of L-Thyroxine in Patients with Hypothyroidism Abstract Background: Increased knowledge of the pharmacokinetic characteristics of orally administered levothyroxine (L-T 4 ) has improved individualization of dosing regimens. However, up to 40...
PMC8801490
core_pubmed_pmc
Non-vitamin K Antagonist Oral Anticoagulants and Drug-Food Interactions: Implications for Clinical Practice and Potential Role of Probiotics and Prebiotics
Non-vitamin K Antagonist Oral Anticoagulants and Drug-Food Interactions: Implications for Clinical Practice and Potential Role of Probiotics and Prebiotics Abstract Non-vitamin K antagonist oral anticoagulants (NOACs) are a therapeutic option to prevent stroke in patients with atrial fibrillation (AF). In fact, NOACs h...
PMC5485718
core_pubmed_pmc
Genomewide Association Study Identifies Novel Genetic Loci That Modify Antiplatelet Effects and Pharmacokinetics of Clopidogrel
Genomewide Association Study Identifies Novel Genetic Loci That Modify Antiplatelet Effects and Pharmacokinetics of Clopidogrel Abstract Abstract Genetic variants in the pharmacokinetic (PK) mechanism are the main underlying factors affecting the antiplatelet response to clopidogrel. Using a genomewide association stud...
PMC5589177
core_pubmed_pmc
The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits
The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits Abstract There is interest in pharmacologic preconditioning for end-organ protection by targeting the HIF system. This can be accomplished by inhibition of prolyl 4-hydroxylase (PHD). GSK3...
PMC11213752
core_pubmed_pmc
A Post-Marketing Surveillance Study of Nusinersen for Spinal Muscular Atrophy in Routine Medical Practice in China: Interim Results
A Post-Marketing Surveillance Study of Nusinersen for Spinal Muscular Atrophy in Routine Medical Practice in China: Interim Results Abstract Abstract Introduction Spinal muscular atrophy (SMA) is a rare, autosomal recessive, neuromuscular disease that leads to progressive muscular weakness and atrophy. Nusinersen, an a...
PMC11462178
core_pubmed_pmc
Changes in fluconazole pharmacokinetics can impact on antifungal effectiveness in critically ill burn patients: a Pharmacokinetic-Pharmacodynamic (PK/PD) approach
Changes in fluconazole pharmacokinetics can impact on antifungal effectiveness in critically ill burn patients: a Pharmacokinetic-Pharmacodynamic (PK/PD) approach Abstract Highlights • Fluconazole pharmacokinetics is significantly altered in critically ill burn patients. • Half-life and total body clearance were correl...
PMC12702928
core_pubmed_pmc
Improved exposure of curcumin-loaded nanocapsules: drug quantification in LPS-induced Drosophila melanogaster and pharmacokinetics in Wistar rats
Improved exposure of curcumin-loaded nanocapsules: drug quantification in LPS-induced Drosophila melanogaster and pharmacokinetics in Wistar rats Abstract Abstract Introduction Curcumin (CUR) has broad pharmacological potential; however, its clinical efficacy is hindered by low aqueous solubility, extensive presystemic...
PMC9631576
core_pubmed_pmc
Using stroma-anchoring cytokines to augment ADCC: a phase 1 trial of F16IL2 and BI 836858 for posttransplant AML relapse
Using stroma-anchoring cytokines to augment ADCC: a phase 1 trial of F16IL2 and BI 836858 for posttransplant AML relapse Abstract Key Points F16-monoclonal antibody–mediated delivery of IL-2 to the leukemia-modified stroma induced an expansion and activation of NK cells. F16IL2/BI 836858 combination therapy showed a ma...
PMC9056898
core_pubmed_pmc
Study on mechanism of elemene reversing tumor multidrug resistance based on luminescence pharmacokinetics in tumor cells in vitro and in vivo
Study on mechanism of elemene reversing tumor multidrug resistance based on luminescence pharmacokinetics in tumor cells in vitro and in vivo Abstract Abstract While elemene (ELE) can reverse tumor multidrug resistance (MDR), the mechanisms for ELE reversing MDR remain unclear. Numerous studies have suggested that the ...
PMC9961245
core_pubmed_pmc
Pharmacokinetics of Tamoxifen and Its Major Metabolites and the Effect of the African Ancestry Specific CYP2D6*17 Variant on the Formation of the Active Metabolite, Endoxifen
Pharmacokinetics of Tamoxifen and Its Major Metabolites and the Effect of the African Ancestry Specific CYP2D6*17 Variant on the Formation of the Active Metabolite, Endoxifen Abstract Abstract Tamoxifen (TAM) is widely used in the treatment of hormone receptor-positive breast cancer. TAM is metabolized into the active ...
PMC11361749
core_pubmed_pmc
A noninvasive BCG skin challenge model for assessing tuberculosis vaccine efficacy
A noninvasive BCG skin challenge model for assessing tuberculosis vaccine efficacy Abstract We report here on the characterisation in mice of a noninvasive bacille Calmette-Guérin (BCG) skin challenge model for assessing tuberculosis (TB) vaccine efficacy. Controlled human infection models (CHIMs) are valuable tools fo...
PMC3388068
core_pubmed_pmc
Pharmacokinetics of Quinacrine Efflux from Mouse Brain via the P-glycoprotein Efflux Transporter
Pharmacokinetics of Quinacrine Efflux from Mouse Brain via the P-glycoprotein Efflux Transporter Abstract The lipophilic cationic compound quinacrine has been used as an antimalarial drug for over 75 years but its pharmacokinetic profile is limited. Here, we report on the pharmacokinetic properties of quinacrine in mic...
PMC12072227
core_pubmed_pmc
Item Response Modeling and Artificial Neural Network for Differentiation of Parkinson's Patients and Subjects Without Evidence of Dopaminergic Deficit
Item Response Modeling and Artificial Neural Network for Differentiation of Parkinson's Patients and Subjects Without Evidence of Dopaminergic Deficit Abstract ABSTRACT Approximately 15% of patients suspected of having Parkinson's disease (PD) present dopamine active transporter (DaT) scans without evidence of dopamine...
PMC12625610
core_pubmed_pmc
Revised therapeutic window for vancomycin in pediatric patients: evidence from a retrospective therapeutic drug monitoring study
Revised therapeutic window for vancomycin in pediatric patients: evidence from a retrospective therapeutic drug monitoring study Abstract Objective Methicillin-resistant Staphylococcus aureus (MRSA) infections among children are escalating annually. Vancomycin serves as the frontline therapeutic agent against MRSA infe...
PMC8301564
core_pubmed_pmc
A population pharmacodynamic Markov mixed‐effects model for determining remimazolam‐induced sedation when co‐administered with fentanyl in procedural sedation
A population pharmacodynamic Markov mixed‐effects model for determining remimazolam‐induced sedation when co‐administered with fentanyl in procedural sedation Abstract ABSTRACT The clinical effects of remimazolam (an investigational, ultra‐short acting benzodiazepine being studied in procedural sedation) were measured ...
PMC12012080
core_pubmed_pmc
Development of a PBPK model of psilocybin/psilocin from Psilocybe cubensis (magic mushroom) in mice, rats, and humans
Development of a PBPK model of psilocybin/psilocin from Psilocybe cubensis (magic mushroom) in mice, rats, and humans Abstract Psilocybin is an active alkaloid found in magic mushrooms ( Psilocybe cubensis ). It is classified as a Class I Psychoactive Substance due to its psychoactive properties. Recent research has su...
PMC5471578
core_pubmed_pmc
UPLC-Tandem Mass Spectrometry Method for Simultaneous Determination of Fluoxetine, Risperidone, and Its Active Metabolite 9-Hydroxyrisperidone in Plasma: Application to Pharmacokinetics Study in Rats
UPLC-Tandem Mass Spectrometry Method for Simultaneous Determination of Fluoxetine, Risperidone, and Its Active Metabolite 9-Hydroxyrisperidone in Plasma: Application to Pharmacokinetics Study in Rats Abstract Risperidone (RIS) is used as an antipsychotic drug alone or with other drugs, like fluoxetine (FLX). A simple m...
PMC11460996
core_pubmed_pmc
Pharmacokinetics and safety of TBAJ-876, a novel antimycobacterial diarylquinoline, in healthy subjects
Pharmacokinetics and safety of TBAJ-876, a novel antimycobacterial diarylquinoline, in healthy subjects Abstract ABSTRACT TBAJ-876, a second-generation diarylquinoline with greater antimycobacterial activity and a potentially better safety profile compared with bedaquiline, is under development for the treatment of dru...
PMC4110066
core_pubmed_pmc
Controlling on-demand gastric acidity in obese subjects: a randomized, controlled trial comparing a single dose of 20 mg rabeprazole and 20 mg omeprazole
Controlling on-demand gastric acidity in obese subjects: a randomized, controlled trial comparing a single dose of 20 mg rabeprazole and 20 mg omeprazole Abstract Background Obesity is associated with a risk of gastroesophageal reflux disease. The pharmacodynamic efficacy of proton pump inhibitors has not been specific...
PMC4335872
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Analysis of Spiroindolone Analogs and KAE609 in a Murine Malaria Model
Pharmacokinetic-Pharmacodynamic Analysis of Spiroindolone Analogs and KAE609 in a Murine Malaria Model Abstract Abstract Limited information is available on the pharmacokinetic (PK) and pharmacodynamic (PD) parameters driving the efficacy of antimalarial drugs. Our objective in this study was to determine dose-response...
PMC11860999
core_pubmed_pmc
Model-informed development of a cost-saving dosing regimen for enfortumab vedotin
Model-informed development of a cost-saving dosing regimen for enfortumab vedotin Abstract Abstract Aim Enfortumab vedotin is an antibody-drug conjugate (ADC) that has been approved for locally advanced or metastatic urothelial cancer, as monotherapy and in combination with pembrolizumab, and has shown significant bene...
PMC9881080
core_pubmed_pmc
Curcumin, Resveratrol and Cannabidiol as Natural Key Prototypes in Drug Design for Neuroprotective Agents
Curcumin, Resveratrol and Cannabidiol as Natural Key Prototypes in Drug Design for Neuroprotective Agents Abstract Abstract Nowadays, neurodegenerative diseases (NDs), such as Parkinson’s disease (PD), Alzheimer’s disease (AD), Huntington’s disease (HD), and amyotrophic lateral sclerosis (ALS), represent a great challe...
PMC12194734
core_pubmed_pmc
The Alkaloid Caulerpin Exhibits Potent and Selective Anti-Inflammatory Activity Through Interaction with the Glucocorticoid Receptor
The Alkaloid Caulerpin Exhibits Potent and Selective Anti-Inflammatory Activity Through Interaction with the Glucocorticoid Receptor Abstract Abstract Inflammation plays a central role in various pathological conditions, necessitating the search for safer and more effective anti-inflammatory agents. This study investig...
PMC11542455
core_pubmed_pmc
Review of the novel antifungal drug olorofim (F901318)
Review of the novel antifungal drug olorofim (F901318) Abstract There is clearly a need for novel antifungal agents, not only concerning spectrum, but also oral bioavailability, tolerability, and drug-drug interactions. There is growing concern for antifungal resistance for current available antifungals, mainly driven ...
PMC5075067
core_pubmed_pmc
Population Pharmacokinetics and Dosing Regimen Optimization of Meropenem in Cerebrospinal Fluid and Plasma in Patients with Meningitis after Neurosurgery
Population Pharmacokinetics and Dosing Regimen Optimization of Meropenem in Cerebrospinal Fluid and Plasma in Patients with Meningitis after Neurosurgery Abstract Abstract Meropenem is used to manage postneurosurgical meningitis, but its population pharmacokinetics (PPK) in plasma and cerebrospinal fluid (CSF) in this ...
PMC7378673
core_pubmed_pmc
Longitudinal Pharmacokinetic-Pharmacodynamic Biomarkers Correlate With Treatment Outcome in Drug-Sensitive Pulmonary Tuberculosis: A Population Pharmacokinetic-Pharmacodynamic Analysis
Longitudinal Pharmacokinetic-Pharmacodynamic Biomarkers Correlate With Treatment Outcome in Drug-Sensitive Pulmonary Tuberculosis: A Population Pharmacokinetic-Pharmacodynamic Analysis Abstract Abstract Background This study aims to explore relationships between baseline demographic covariates, plasma antibiotic exposu...
PMC5823863
core_pubmed_pmc
Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes
Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes Abstract Fundamental equations for determining pharmacological parameters, such as the binding affinity of a ligand for its target receptor, assume a homogeneous distribution of ligand, with concentrations in the immediate vicinity of t...
PMC7032200
core_pubmed_pmc
Development of cryptotanshinone-loaded pellets for angina chronotherapy: In vitro / in vivo prediction and evaluation ☆
Development of cryptotanshinone-loaded pellets for angina chronotherapy: In vitro / in vivo prediction and evaluation ☆ Abstract The clinical manifestations of variant angina is unevenly distributed during the 24 h, thus the in vivo performance of drugs should be tailored according to the angina circadian rhythm. Crypt...
PMC5656713
core_pubmed_pmc
Effects of Ketoconazole on the Pharmacokinetics of Mifepristone, a Competitive Glucocorticoid Receptor Antagonist, in Healthy Men
Effects of Ketoconazole on the Pharmacokinetics of Mifepristone, a Competitive Glucocorticoid Receptor Antagonist, in Healthy Men Abstract Abstract Introduction Mifepristone, a competitive glucocorticoid receptor antagonist approved for Cushing syndrome, and ketoconazole, an antifungal and steroidogenesis inhibitor, ar...
PMC9166902
core_pubmed_pmc
Folate Decorated Multifunctional Biodegradable Nanoparticles for Gastric Carcinoma Active Targeting Theranostics
Folate Decorated Multifunctional Biodegradable Nanoparticles for Gastric Carcinoma Active Targeting Theranostics Abstract Abstract Introduction Gastric cancer remains a major clinical issue and little progress has been made in the treatment of gastric cancer patients during recent decades. Nanoparticles provide a versa...
PMC12227894
core_pubmed_pmc
Pharmacokinetic Variability of Amlodipine Serum Concentration and Effect on Blood Pressure in Patients Treated for Hypertension
Pharmacokinetic Variability of Amlodipine Serum Concentration and Effect on Blood Pressure in Patients Treated for Hypertension Abstract ABSTRACT We investigated the effects of age, sex, BMI, total number of prescribed daily pills, common biomarkers, and CYP3A4/5 polymorphisms on dose‐adjusted amlodipine concentration ...
PMC4150159
core_pubmed_pmc
Late Aminophylline Reversal of Regadenoson Stress Testing in Patients with End Stage Renal Disease
Late Aminophylline Reversal of Regadenoson Stress Testing in Patients with End Stage Renal Disease Abstract Regadenoson is a widely used and well-tolerated vasodilator agent for pharmacologic stress myocardial perfusing imaging. In patients at higher risk of adverse reactions such as those with end stage renal disease,...
PMC12057336
core_pubmed_pmc
Impact of hepatic impairment and renal failure on the pharmacokinetics of linezolid and its metabolites: contribution of hepatic metabolism and renal excretion
Impact of hepatic impairment and renal failure on the pharmacokinetics of linezolid and its metabolites: contribution of hepatic metabolism and renal excretion Abstract ABSTRACT Linezolid, an oxazolidinone antibiotic, is used in patients with liver or kidney disease. However, the effects and mechanisms of hepatic impai...