id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC5593171
core_pubmed_pmc
New Paradigm for Translational Modeling to Predict Long‐term Tuberculosis Treatment Response
New Paradigm for Translational Modeling to Predict Long‐term Tuberculosis Treatment Response Abstract Abstract Disappointing results of recent tuberculosis chemotherapy trials suggest that knowledge gained from preclinical investigations was not utilized to maximal effect. A mouse‐to‐human translational pharmacokinetic...
PMC9958448
core_pubmed_pmc
Rohitukine content across the geographical distribution of Dysoxylum binectariferum Hook F. and its natural derivatives as potential sources of CDK inhibitors
Rohitukine content across the geographical distribution of Dysoxylum binectariferum Hook F. and its natural derivatives as potential sources of CDK inhibitors Abstract Dysoxylum binectariferum is an important medicinal plant distributed in the Western Ghats of India. The species has gained international importance for ...
PMC7811989
core_pubmed_pmc
Effect of Kidney Function and Dialysis on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor
Effect of Kidney Function and Dialysis on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Abstract Abstract Background and Objectives Roxadustat is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor for anemia in chronic kidney d...
PMC12905028
core_pubmed_pmc
Deconvoluting Gut Versus Liver Cytochrome P450 3A4 Function: Drug Probes, Biomarkers, and Tissue Biopsy
Deconvoluting Gut Versus Liver Cytochrome P450 3A4 Function: Drug Probes, Biomarkers, and Tissue Biopsy Abstract Abstract Cytochrome P450 3A4 (CYP3A4) is an important drug‐metabolizing enzyme, whose function is impacted by age, sex, body weight, pregnancy, and disease. It is also the site of major drug interactions inv...
PMC10376460
core_pubmed_pmc
Novel aldo-keto reductase 1C3 inhibitor affects androgen metabolism but not ovarian function in healthy women: a phase 1 study
Novel aldo-keto reductase 1C3 inhibitor affects androgen metabolism but not ovarian function in healthy women: a phase 1 study Abstract Abstract Objective Aldo-keto reductase 1C3 (AKR1C3) has been postulated to be involved in androgen, progesterone, and estrogen metabolism. Aldo-keto reductase 1C3 inhibition has been p...
PMC10653991
core_pubmed_pmc
Enzyme‐Triggered Intestine‐Specific Targeting Adhesive Platform for Universal Oral Drug Delivery
Enzyme‐Triggered Intestine‐Specific Targeting Adhesive Platform for Universal Oral Drug Delivery Abstract Abstract Patient adherence to chronic therapies can be suboptimal, leading to poor therapeutic outcomes. Dosage forms that enable reduction in dosing frequency stand to improve patient adherence. Variation in gastr...
PMC12811727
core_pubmed_pmc
Ameliorative Effects of Ethyl-Acetate Extract of Bidens pilosa on Oxidative Stress and Reproductive Impairment in Bisphenol A-Exposed Male Mice: Insight from In-silico, Invitro and In-vivo Studies
Ameliorative Effects of Ethyl-Acetate Extract of Bidens pilosa on Oxidative Stress and Reproductive Impairment in Bisphenol A-Exposed Male Mice: Insight from In-silico, Invitro and In-vivo Studies Abstract Background Bisphenol A (BPA), a ubiquitous environmental pollutant, is known to induce oxidative stress and disrup...
PMC5903252
core_pubmed_pmc
First‐in‐human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS‐962212, a direct, reversible, small molecule factor XIa inhibitor in non‐Japanese and Japanese healthy subjects
First‐in‐human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS‐962212, a direct, reversible, small molecule factor XIa inhibitor in non‐Japanese and Japanese healthy subjects Abstract Abstract Aims The aims of the present study were to assess the safety, pharmacokinetics (PK) and pharmacodynami...
PMC10273764
core_pubmed_pmc
Safety and tolerability study of sotrovimab (VIR-7831) prophylaxis against COVID-19 infection in immunocompromised individuals with impaired SARS-CoV-2 humoral immunity
Safety and tolerability study of sotrovimab (VIR-7831) prophylaxis against COVID-19 infection in immunocompromised individuals with impaired SARS-CoV-2 humoral immunity Abstract Background Multiple vaccines have been approved since August 2021 to prevent infection with SARS-CoV-2; however, 20–40% of immunocompromised p...
PMC7751226
core_pubmed_pmc
Capsular Polysaccharide From Bacteroides fragilis Protects Against Ulcerative Colitis in an Undegraded Form
Capsular Polysaccharide From Bacteroides fragilis Protects Against Ulcerative Colitis in an Undegraded Form Abstract Abstract The prominent human symbiont Bacteroides fragilis protects animals from intestinal diseases, such as ulcerative colitis, and its capsular polysaccharide plays a key role in reducing inflammation...
PMC10035389
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of TAK-931, a Cell Division Cycle 7 Inhibitor, in Patients with Advanced Solid Tumors: A Phase I First-in-Human Study
Safety, Tolerability, and Pharmacokinetics of TAK-931, a Cell Division Cycle 7 Inhibitor, in Patients with Advanced Solid Tumors: A Phase I First-in-Human Study Abstract Abstract Purpose: We conducted a first-in-human, dose-escalation study, to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and ...
PMC9732253
core_pubmed_pmc
Inhibition of the Phosphatidylinositol-3 Kinase Pathway Using Bimiralisib in Loss-of-Function NOTCH1 -Mutant Head and Neck Cancer
Inhibition of the Phosphatidylinositol-3 Kinase Pathway Using Bimiralisib in Loss-of-Function NOTCH1 -Mutant Head and Neck Cancer Abstract Abstract Background PI3K/mTOR inhibition leads to apoptosis of NOTCH1 -mutant head and neck squamous cell carcinoma (HNSCC) cells. We tested the efficacy of the PI3K/mTOR inhibitor ...
PMC5787171
core_pubmed_pmc
Pharmacokinetics of Single Oral Dose Extended‐Release Levetiracetam in Healthy Cats
Pharmacokinetics of Single Oral Dose Extended‐Release Levetiracetam in Healthy Cats Abstract Abstract Background Repeated PO dosing of anti‐epileptic drugs may contribute to poor compliance in treated cats. Intermediate‐release levetiracetam has been used safely in cats, but must be given q8h to maintain serum concentr...
PMC12626903
core_pubmed_pmc
Zaleplon nanospanlastics loaded transdermal patches: formulation, optimization, ex-vivo permeation, and in-vivo studies
Zaleplon nanospanlastics loaded transdermal patches: formulation, optimization, ex-vivo permeation, and in-vivo studies Abstract Zaleplon (ZLP) is a commonly used sedative-hypnotic drug that has low oral bioavailability because of its poor water solubility and extensive hepatic metabolism. This study aimed to encapsula...
PMC8185372
core_pubmed_pmc
A Prospective Investigation of Bispecific CD19/22 CAR T Cell Therapy in Patients With Relapsed or Refractory B Cell Non-Hodgkin Lymphoma
A Prospective Investigation of Bispecific CD19/22 CAR T Cell Therapy in Patients With Relapsed or Refractory B Cell Non-Hodgkin Lymphoma Abstract Abstract Background The use of T cells expressing chimeric antigen receptor (CAR T) engineered to target CD19 constitutes breakthrough treatment for relapsed or refractory B ...
PMC8589829
core_pubmed_pmc
Pharmacokinetic and molecular docking studies to design antimalarial compounds targeting Actin I
Pharmacokinetic and molecular docking studies to design antimalarial compounds targeting Actin I Abstract Abstract Objective: Malaria is an ancient disease that still causes more than 200 million of cases 7 with high mortality globally. Identification of new drug targets and development of novel antimalarial drugs with...
PMC9541386
core_pubmed_pmc
Effect of Colonic Absorption on the Pharmacokinetic Properties of Delayed‐Release and Extended‐Release Methylphenidate: In Vivo, In Vitro, and Modeling Evaluations
Effect of Colonic Absorption on the Pharmacokinetic Properties of Delayed‐Release and Extended‐Release Methylphenidate: In Vivo, In Vitro, and Modeling Evaluations Abstract Abstract Most stimulants used to treat attention‐deficit/hyperactivity disorder are administered in the morning and absorbed in the upper gastroint...
PMC9393588
core_pubmed_pmc
Pharmacokinetics of menbutone after intravenous and intramuscular administration to sheep
Pharmacokinetics of menbutone after intravenous and intramuscular administration to sheep Abstract Abstract Menbutone is a drug currently approved in several European Union (EU) countries to treat digestive disorders in different animal species. The objective of this study was to establish the pharmacokinetic parameter...
PMC11262688
core_pubmed_pmc
New pharmacodynamic parameters linked with ibrutinib responses in chronic lymphocytic leukemia: Prospective study in real-world patients and mathematical modeling
New pharmacodynamic parameters linked with ibrutinib responses in chronic lymphocytic leukemia: Prospective study in real-world patients and mathematical modeling Abstract Abstract Background One of the first clinical observations of ibrutinib activity in the treatment of chronic lymphocytic leukemia (CLL) is a rapid d...
PMC11738769
core_pubmed_pmc
Bioequivalence study of fluticasone propionate nebuliser suspensions in healthy Chinese subjects
Bioequivalence study of fluticasone propionate nebuliser suspensions in healthy Chinese subjects Abstract Abstract Background Fluticasone propionate is a synthetic trifluoro-substituted glucocorticoid, a highly selective glucocorticoid receptor agonist. Fluticasone propionate nebuliser suspensions is an inhaled cortico...
PMC3817378
core_pubmed_pmc
Longitudinal Modeling of the Relationship Between Mean Plasma Glucose and HbA1c Following Antidiabetic Treatments
Longitudinal Modeling of the Relationship Between Mean Plasma Glucose and HbA1c Following Antidiabetic Treatments Abstract Abstract Late-phase clinical trials within diabetes generally have a duration of 12–24 weeks, where 12 weeks may be too short to reach steady-state glycated hemoglobin (HbA1c). The main determinant...
PMC12623593
core_pubmed_pmc
Population Pharmacokinetic–Based Strategies for Switching Patients with Schizophrenia Between Long-Acting Injectable Formulations of Risperidone: R064766 or RBP-7000 to TV-46000
Population Pharmacokinetic–Based Strategies for Switching Patients with Schizophrenia Between Long-Acting Injectable Formulations of Risperidone: R064766 or RBP-7000 to TV-46000 Abstract Abstract Introduction This analysis used pharmacokinetic (PK) modeling to characterize dosing conversions and switching strategies fr...
PMC11644218
core_pubmed_pmc
The Deuterium Oxide Dilution Method to Quantify Human Milk Intake Volume of Infants: A Systematic Review—A Contribution from the ConcePTION Project
The Deuterium Oxide Dilution Method to Quantify Human Milk Intake Volume of Infants: A Systematic Review—A Contribution from the ConcePTION Project Abstract Abstract Background: Global health organizations recommend breastfeeding, but maternal pharmacotherapy can disrupt this due to safety concerns. Physiologically bas...
PMC8688832
core_pubmed_pmc
A Comparative Study of the Respiratory Neonatal Outcomes Utilizing Dexamethasone Sodium Phosphate versus a Mixture of Betamethasone Dipropionate and Betamethasone Sodium Phosphate as an Antenatal Corticosteroid Therapy
A Comparative Study of the Respiratory Neonatal Outcomes Utilizing Dexamethasone Sodium Phosphate versus a Mixture of Betamethasone Dipropionate and Betamethasone Sodium Phosphate as an Antenatal Corticosteroid Therapy Abstract Objective The aim of this study is to compare the respiratory neonatal outcomes utilizing an...
PMC6742946
core_pubmed_pmc
Exposure–Response Analysis of Overall Survival for Tremelimumab in Unresectable Malignant Mesothelioma: The Confounding Effect of Disease Status
Exposure–Response Analysis of Overall Survival for Tremelimumab in Unresectable Malignant Mesothelioma: The Confounding Effect of Disease Status Abstract Tremelimumab, an anti‐cytotoxic T‐lymphocyte antigen‐4 monoclonal antibody that enhances T‐cell activation, was evaluated in a randomized, double‐blind, placebo‐contr...
PMC7485953
core_pubmed_pmc
Genetic Diversity in Drug Transporters: Impact in African Populations
Genetic Diversity in Drug Transporters: Impact in African Populations Abstract Abstract Polymorphisms in drug transporters, like the adenosine triposphate‒binding cassette (ABC) and solute carrier (SLC) superfamilies, may contribute to the observed diversity in drug response in African patients. This review aims to pro...
PMC8227653
core_pubmed_pmc
Polypharmacy and Malnutrition Management of Elderly Perioperative Patients with Cancer: A Systematic Review
Polypharmacy and Malnutrition Management of Elderly Perioperative Patients with Cancer: A Systematic Review Abstract Malnutrition, which commonly occurs in perioperative patients with cancer, leads to decreased muscle mass, hypoalbuminemia, and edema, thereby increasing the patient’s risk of various complications. Thus...
PMC12188534
core_pubmed_pmc
Microemulsion Gels of Tapentadol Hydrochloride: Statistical Analysis of Pharmacokinetics and Skin Irritation Studies
Microemulsion Gels of Tapentadol Hydrochloride: Statistical Analysis of Pharmacokinetics and Skin Irritation Studies Abstract Abstract Background: The present study aimed to overcome the drawbacks of tapentadol through the oral route and to assess the significance of microemulsion gels for transdermal delivery via phar...
PMC12433215
core_pubmed_pmc
Drug-Drug Interactions and Initial Dosage Optimization of Quetiapine in Patients with Depression: A Real-World Study
Drug-Drug Interactions and Initial Dosage Optimization of Quetiapine in Patients with Depression: A Real-World Study Abstract Abstract Objective Quetiapine has been used for treating patients with depression; however, drug-drug interactions (DDIs) deeply limit its individualized administration. This study explored DDIs...
PMC7778723
core_pubmed_pmc
Ivermectin as a potential drug for treatment of COVID-19: an in-sync review with clinical and computational attributes
Ivermectin as a potential drug for treatment of COVID-19: an in-sync review with clinical and computational attributes Abstract Introduction COVID-19 cases are on surge; however, there is no efficient treatment or vaccine that can be used for its management. Numerous clinical trials are being reviewed for use of differ...
PMC8666623
core_pubmed_pmc
Sensitive LC-MS/MS Methods for Amphotericin B Analysis in Cerebrospinal Fluid, Plasma, Plasma Ultrafiltrate, and Urine: Application to Clinical Pharmacokinetics
Sensitive LC-MS/MS Methods for Amphotericin B Analysis in Cerebrospinal Fluid, Plasma, Plasma Ultrafiltrate, and Urine: Application to Clinical Pharmacokinetics Abstract Neurocryptococcosis, a meningoencephalitis caused by Cryptococcus spp, is treated with amphotericin B (AmB) combined with fluconazole. The integrity o...
PMC6523871
core_pubmed_pmc
Biodistribution and Physiologically-Based Pharmacokinetic Modeling of Gold Nanoparticles in Mice with Interspecies Extrapolation
Biodistribution and Physiologically-Based Pharmacokinetic Modeling of Gold Nanoparticles in Mice with Interspecies Extrapolation Abstract Abstract Gold nanoparticles (AuNPs) are a focus of growing medical research applications due to their unique chemical, electrical and optical properties. Because of uncertain toxicit...
PMC12735454
core_pubmed_pmc
Oral Therapy for Infective Endocarditis: Where Do We Stand?
Oral Therapy for Infective Endocarditis: Where Do We Stand? Abstract Abstract Standard therapy for infective endocarditis (IE) usually requires 4–6 weeks of intravenous (IV) antibiotics, ensuring sustained bactericidal concentrations, yet resulting in prolonged hospitalization and increased cost of care. These challeng...
PMC4673178
core_pubmed_pmc
Trop-2 is a novel target for solid cancer therapy with sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC) *
Trop-2 is a novel target for solid cancer therapy with sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC) * Abstract Trop-2 is a novel target for ADC therapy because of its high expression by many solid cancers. The rational development of IMMU-132 represents a paradigm shift as an ADC that binds a well...
PMC7212882
core_pubmed_pmc
Efficacy and pharmacodynamics of niraparib in BRCA-mutant and wild-type intracranial triple-negative breast cancer murine models
Efficacy and pharmacodynamics of niraparib in BRCA-mutant and wild-type intracranial triple-negative breast cancer murine models Abstract Abstract Background Despite the poor prognosis of triple-negative breast cancer (TNBC) brain metastases, there are no approved systemic therapies. We explored the DNA-damaging poly(A...
PMC8259816
core_pubmed_pmc
Baicalein inhibits the pharmacokinetics of simvastatin in rats via regulating the activity of CYP3A4
Baicalein inhibits the pharmacokinetics of simvastatin in rats via regulating the activity of CYP3A4 Abstract Abstract Context Baicalein and simvastatin possess similar pharmacological activities and indications. The risk of their co-administration was unclear. Objective The interaction between baicalein and simvastati...
PMC7175153
core_pubmed_pmc
Testing the Pharmacokinetic Interactions of 24 Colonic Flavonoid Metabolites with Human Serum Albumin and Cytochrome P450 Enzymes
Testing the Pharmacokinetic Interactions of 24 Colonic Flavonoid Metabolites with Human Serum Albumin and Cytochrome P450 Enzymes Abstract Flavonoids are abundant polyphenols in nature. They are extensively biotransformed in enterocytes and hepatocytes, where conjugated (methyl, sulfate, and glucuronide) metabolites ar...
PMC10793675
core_pubmed_pmc
Development and pharmacokinetic assessment of a fully canine anti-PD-1 monoclonal antibody for comparative translational research in dogs with spontaneous tumors
Development and pharmacokinetic assessment of a fully canine anti-PD-1 monoclonal antibody for comparative translational research in dogs with spontaneous tumors Abstract ABSTRACT PD-1 checkpoint inhibitors have revolutionized the treatment of patients with different cancer histologies including melanoma, renal cell ca...
PMC12378435
core_pubmed_pmc
The effect of intraoperative excessive bleeding on the pharmacokinetics of ampicillin and sulbactam in recipients of living donor liver transplantation in Japan
The effect of intraoperative excessive bleeding on the pharmacokinetics of ampicillin and sulbactam in recipients of living donor liver transplantation in Japan Abstract Abstract Objective Guidelines recommend redosing with intravenous prophylactic antibiotics when excessive bleeding exceeds 1500 mL during surgery base...
PMC6099731
core_pubmed_pmc
A Microdialysis in Adjuvant Arthritic Rats for Pharmacokinetics–Pharmacodynamics Modeling Study of Geniposide with Determination of Drug Concentration and Efficacy Levels in Dialysate
A Microdialysis in Adjuvant Arthritic Rats for Pharmacokinetics–Pharmacodynamics Modeling Study of Geniposide with Determination of Drug Concentration and Efficacy Levels in Dialysate Abstract Abstract Microdialysis, a sampling method for pharmacokinetics–pharmacodynamics (PK–PD) modeling in preclinical and clinical st...
PMC6896236
core_pubmed_pmc
Severe Acute Malnutrition Results in Lower Lumefantrine Exposure in Children Treated With Artemether‐Lumefantrine for Uncomplicated Malaria
Severe Acute Malnutrition Results in Lower Lumefantrine Exposure in Children Treated With Artemether‐Lumefantrine for Uncomplicated Malaria Abstract Severe acute malnutrition ( SAM ) has been reported to be associated with increased malaria morbidity in Sub‐Saharan African children and may affect the pharmacology of an...
PMC5787466
core_pubmed_pmc
Accelerated bottom-up drug design platform enables the discovery of novel stearoyl-CoA desaturase 1 inhibitors for cancer therapy
Accelerated bottom-up drug design platform enables the discovery of novel stearoyl-CoA desaturase 1 inhibitors for cancer therapy Abstract Here we present an innovative computational-based drug discovery strategy, coupled with machine-based learning and functional assessment, for the rational design of novel small mole...
PMC12691610
core_pubmed_pmc
Keeping the horse with the cart: are we underdosing tazobactam even when using continuous-infusion ceftolozane/tazobactam for effectively preventing resistance development by ESBL-producing Enterobacterales?
Keeping the horse with the cart: are we underdosing tazobactam even when using continuous-infusion ceftolozane/tazobactam for effectively preventing resistance development by ESBL-producing Enterobacterales? Abstract ABSTRACT Ceftolozane/tazobactam is widely used against extended-spectrum β-lactamase (ESBL)-producing E...
PMC6822546
core_pubmed_pmc
Pharmacokinetic Interaction of Green Rooibos Extract With Atorvastatin and Metformin in Rats
Pharmacokinetic Interaction of Green Rooibos Extract With Atorvastatin and Metformin in Rats Abstract An aspalathin-rich green rooibos extract (Afriplex GRT™) has demonstrated anti-diabetic and hypolipidemic properties, while also moderately inhibiting CYP3A4 activity, suggesting a potential for herb–drug interaction. ...
PMC3764307
core_pubmed_pmc
Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability
Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability Abstract Introduction Human immunodeficiency virus (HIV) type-1 non-nucleoside and nucleoside reverse transcriptase inhibitors (NNRTIs) are key drugs of highly active antiretroviral therapy (HAART) i...
PMC10100937
core_pubmed_pmc
Safety and Feasibility Assessment of a Pharmacy-Driven AUC/MIC Vancomycin Dosing Protocol in a Multicenter Hospital System
Safety and Feasibility Assessment of a Pharmacy-Driven AUC/MIC Vancomycin Dosing Protocol in a Multicenter Hospital System Abstract ABSTRACT Vancomycin is used for Gram-positive infections, including methicillin-resistant Staphylococcus aureus . The 2020 vancomycin guidelines described by M. J. Rybak, J. Le, T. P. Lodi...
PMC10930353
core_pubmed_pmc
Assessing Pharmacokinetic Correlates of Escitalopram-Related Adverse Drug Reactions
Assessing Pharmacokinetic Correlates of Escitalopram-Related Adverse Drug Reactions Abstract Supplemental Digital Content is Available in the Text. Background: To assess the pharmacokinetic correlates of reported adverse drug reactions (ADRs) under antidepressant treatment with escitalopram (ESC) using a large therapeu...
PMC10339700
core_pubmed_pmc
Systems‐based digital twins to help characterize clinical dose–response and propose predictive biomarkers in a Phase I study of bispecific antibody, mosunetuzumab, in NHL
Systems‐based digital twins to help characterize clinical dose–response and propose predictive biomarkers in a Phase I study of bispecific antibody, mosunetuzumab, in NHL Abstract Abstract Phase I oncology clinical trials often comprise a limited number of patients representing different disease subtypes who are divide...
PMC7250365
core_pubmed_pmc
Hepatic Transcript Profiles of Cytochrome P450 Genes Predict Sex Differences in Drug Metabolism
Hepatic Transcript Profiles of Cytochrome P450 Genes Predict Sex Differences in Drug Metabolism Abstract Safety assessments of new drug candidates are an important part of the drug development and approval process. Often, possible sex-associated susceptibilities are not adequately addressed, and better assessment tools...
PMC12823293
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling in Patients With Hepatic Impairment: Are Changes in Bosutinib Exposure Profiles Driven by Altered Absorption or Distribution?
Physiologically Based Pharmacokinetic Modeling in Patients With Hepatic Impairment: Are Changes in Bosutinib Exposure Profiles Driven by Altered Absorption or Distribution? Abstract ABSTRACT Bosutinib is an orally available Src/Abl tyrosine kinase inhibitor and has been approved for the treatment of patients with Ph + ...
PMC8294837
core_pubmed_pmc
Imlifidase Desensitization in Crossmatch-positive, Highly Sensitized Kidney Transplant Recipients: Results of an International Phase 2 Trial (Highdes)
Imlifidase Desensitization in Crossmatch-positive, Highly Sensitized Kidney Transplant Recipients: Results of an International Phase 2 Trial (Highdes) Abstract Supplemental Digital Content is available in the text. Background. Highly HLA sensitized patients have limited access to life-saving kidney transplantation beca...
PMC6494745
core_pubmed_pmc
A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: Lessons learned from a human laboratory investigation
A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: Lessons learned from a human laboratory investigation Abstract Abstract Previous studies suggest that GABA-B receptor agonism may represent an effective pharmacological approach to treat addictive disorders. Baclo...
PMC12926606
core_pubmed_pmc
As-Needed Medication Use for Agitation Across Valproic Acid Formulations
As-Needed Medication Use for Agitation Across Valproic Acid Formulations Abstract Abstract Background Pharmacokinetic differences between immediate-, delayed- and extended-release (IR, DR, ER) formulations of valproic acid (VPA) may impact therapeutic outcomes. As-needed, pro re nata (PRN) medications may serve as prox...
PMC8381972
core_pubmed_pmc
Evaluation of herb-drug interaction of ambrisentan with shikonin based on UPLC-MS/MS
Evaluation of herb-drug interaction of ambrisentan with shikonin based on UPLC-MS/MS Abstract Abstract Context Ambrisentan is an oral endothelin-receptor antagonist (ERA). However, there is no report on the interaction between ambrisentan and shikonin. Objective To investigate the effect of shikonin on ambrisentan meta...
PMC6585622
core_pubmed_pmc
Genomic Variation and Pharmacokinetics in Old Age: A Quantitative Review of Age‐ vs. Genotype‐Related Differences
Genomic Variation and Pharmacokinetics in Old Age: A Quantitative Review of Age‐ vs. Genotype‐Related Differences Abstract Older persons may particularly benefit from pharmacogenetic diagnostics, but there is little clinical evidence on that question. We quantitatively analyzed the effects of age and genotype in drugs ...
PMC12749239
core_pubmed_pmc
Effects of Acacetin on the Pharmacokinetics of Diazepam in vivo and in vitro
Effects of Acacetin on the Pharmacokinetics of Diazepam in vivo and in vitro Abstract Background Herb-drug interactions (HDIs) have garnered significant attention in recent years. Objectives To investigate the effects of acacetin on the pharmacokinetics of diazepam both in vivo and in vitro. Methods Rat liver microsome...
PMC11442724
core_pubmed_pmc
Assessing the effect of therapeutic level of oxytetracycline dihydrate on pharmacokinetics and biosafety in Oncorhynchus mykiss (Walbaum, 1792)
Assessing the effect of therapeutic level of oxytetracycline dihydrate on pharmacokinetics and biosafety in Oncorhynchus mykiss (Walbaum, 1792) Abstract Abstract The aim of the experiment was to investigate the pharmacokinetics of oxytetracycline dihydrate after a single oral administration of 80 mg kg −1 day −1 in rai...
PMC9989164
core_pubmed_pmc
Pharmacological and toxicological studies of a novel goserelin acetate extended-release microspheres in rats
Pharmacological and toxicological studies of a novel goserelin acetate extended-release microspheres in rats Abstract LY01005 is an investigational new drug product of goserelin acetate which is formulated as extended-release microspheres for intramuscular injection. To support the proposed clinical trials and marketin...
PMC11221861
core_pubmed_pmc
ABCG2 polymorphism and rivaroxaban pharmacokinetics in healthy individuals after a single dose
ABCG2 polymorphism and rivaroxaban pharmacokinetics in healthy individuals after a single dose Abstract Rivaroxaban is a direct factor Xa inhibitor. Its interindividual variability is large and may be connected to the occurrence of adverse drug reactions or drug inefficacy. Pharmacogenetics studies concentrating on the...
PMC12670091
core_pubmed_pmc
First-in-human study of a thorium-227-labeled mesothelin-targeting antibody-chelator conjugate (MSLN-TTC), in patients with malignant mesothelioma and other solid tumors
First-in-human study of a thorium-227-labeled mesothelin-targeting antibody-chelator conjugate (MSLN-TTC), in patients with malignant mesothelioma and other solid tumors Abstract Abstract Introduction BAY 2287411 [ 227 Th-anetumab corixetan; mesothelin-targeting antibody-chelator conjugate (MSLN-TTC)] is a targeted alp...
PMC3044563
core_pubmed_pmc
Prevalence of potential drug interactions in patients in an intensive care unit of a university hospital in Brazil
Prevalence of potential drug interactions in patients in an intensive care unit of a university hospital in Brazil Abstract OBJECTIVES: To investigate the prevalence of potential drug interactions at the intensive care unit of a university hospital in Brazil and to analyze their clinical significance. METHODS: This cro...
PMC5956996
core_pubmed_pmc
In vivo imaging biomarkers of neuroinflammation in the development and assessment of stroke therapies - towards clinical translation
In vivo imaging biomarkers of neuroinflammation in the development and assessment of stroke therapies - towards clinical translation Abstract Abstract Modulation of the inflammatory microenvironment after stroke opens a new avenue for the development of novel neurorestorative therapies in stroke. Understanding the spat...
PMC11243439
core_pubmed_pmc
Revisiting and Updating the Interaction between Human Serum Albumin and the Non-Steroidal Anti-Inflammatory Drugs Ketoprofen and Ketorolac
Revisiting and Updating the Interaction between Human Serum Albumin and the Non-Steroidal Anti-Inflammatory Drugs Ketoprofen and Ketorolac Abstract Abstract Ketoprofen (KTF) and ketorolac (KTL) are among the most primarily used non-steroidal anti-inflammatory drugs (NSAIDs) in humans to alleviate moderate pain and to t...
PMC12863475
core_pubmed_pmc
Discovery of a novel Keap1 inhibitor for neurodegeneration through virtual screening and molecular dynamics simulations
Discovery of a novel Keap1 inhibitor for neurodegeneration through virtual screening and molecular dynamics simulations Abstract Oxidative stress is a key feature of Alzheimer’s disease (AD) and other neurodegenerative disorders. The Kelch-like ECH-associated protein 1 (Keap1)–nuclear factor erythroid 2–related factor ...
PMC6360486
core_pubmed_pmc
Safety and tolerability of inebilizumab (MEDI-551), an anti-CD19 monoclonal antibody, in patients with relapsing forms of multiple sclerosis: Results from a phase 1 randomised, placebo-controlled, escalating intravenous and subcutaneous dose study
Safety and tolerability of inebilizumab (MEDI-551), an anti-CD19 monoclonal antibody, in patients with relapsing forms of multiple sclerosis: Results from a phase 1 randomised, placebo-controlled, escalating intravenous and subcutaneous dose study Abstract Abstract Background: B cells may be involved in the pathophysio...
PMC11653581
core_pubmed_pmc
Effect of changes in skin properties due to diabetes mellitus on the titration period of transdermal fentanyl: single-center retrospective study and diabetic animal model study
Effect of changes in skin properties due to diabetes mellitus on the titration period of transdermal fentanyl: single-center retrospective study and diabetic animal model study Abstract Abstract Background In the dose titration of transdermal fentanyl to prevent unrelieved pain, it is important to consider not only dos...
PMC12613457
core_pubmed_pmc
Evaluating the Use of Nasal Epinephrine in Anaphylaxis: Current Status
Evaluating the Use of Nasal Epinephrine in Anaphylaxis: Current Status Abstract The use of epinephrine auto-injectors is life-saving in serious allergic reactions such as out-of-hospital anaphylaxis. However, several factors limit their use, including patients not obtaining their prescriptions, the difficulty of carryi...
PMC7602181
core_pubmed_pmc
Dalbavancin, Vancomycin and Daptomycin Alone and in Combination with Cefazolin against Resistant Phenotypes of Staphylococcus aureus in a Pharmacokinetic/Pharmacodynamic Model
Dalbavancin, Vancomycin and Daptomycin Alone and in Combination with Cefazolin against Resistant Phenotypes of Staphylococcus aureus in a Pharmacokinetic/Pharmacodynamic Model Abstract The most efficacious antimicrobial therapy to aid in the successful elimination of resistant S. aureus infections is unknown. In this s...
PMC9972364
core_pubmed_pmc
Pharmacokinetic study on the effect of ligustrazine–tangeretin co‐administration on the pharmacokinetics of ligustrazine and its potential mechanism in rats
Pharmacokinetic study on the effect of ligustrazine–tangeretin co‐administration on the pharmacokinetics of ligustrazine and its potential mechanism in rats Abstract Abstract Both ligustrazine and tangeretin are usually prescribed in the treatment of cardiovascular diseases, which makes their co‐administration possible...
PMC10526140
core_pubmed_pmc
Understanding the Clinical Use of Levosimendan and Perspectives on its Future in Oncology
Understanding the Clinical Use of Levosimendan and Perspectives on its Future in Oncology Abstract Abstract Drug repurposing, also known as repositioning or reprofiling, has emerged as a promising strategy to accelerate drug discovery and development. This approach involves identifying new medical indications for exist...
PMC4865545
core_pubmed_pmc
A clinically relevant pharmacokinetic interaction between cyclosporine and imatinib
A clinically relevant pharmacokinetic interaction between cyclosporine and imatinib Abstract Abstract Purpose Cyclosporine A (CsA) and imatinib are both CYP3A4 and P-glycoprotein substrates. Concomitant use after hematopoietic stem cell transplantation (HSCT) for chronic myeloid leukemia (CML) or Philadelphia chromosom...
PMC6732512
core_pubmed_pmc
Co-crystals as a new approach to multimodal analgesia and the treatment of pain
Co-crystals as a new approach to multimodal analgesia and the treatment of pain Abstract Abstract Pain is highly prevalent, but frequently untreated or under-treated, and health care professionals are faced with a range of treatment challenges. Multimodal therapy is recommended and can be achieved using open combinatio...
PMC6597607
core_pubmed_pmc
A Pediatric Covariate Function for CYP3A-Mediated Midazolam Clearance Can Scale Clearance of Selected CYP3A Substrates in Children
A Pediatric Covariate Function for CYP3A-Mediated Midazolam Clearance Can Scale Clearance of Selected CYP3A Substrates in Children Abstract Recently a framework was presented to assess whether pediatric covariate models for clearance can be extrapolated between drugs sharing elimination pathways, based on extraction ra...
PMC7769078
core_pubmed_pmc
Polymeric Nanoparticles-Based Brain Delivery with Improved Therapeutic Efficacy of Ginkgolide B in Parkinson’s Disease
Polymeric Nanoparticles-Based Brain Delivery with Improved Therapeutic Efficacy of Ginkgolide B in Parkinson’s Disease Abstract Purpose Ginkgolide B (GB) is a terpene lactone derivative of Ginkgo biloba that is believed to function in a neuroprotective manner ideal for treating Parkinson’s disease (PD). Despite its pro...
PMC11693449
core_pubmed_pmc
New reverse sum Revan indices for physicochemical and pharmacokinetic properties of anti-filovirus drugs
New reverse sum Revan indices for physicochemical and pharmacokinetic properties of anti-filovirus drugs Abstract Abstract Ebola and Marburg viruses, biosafety level 4 pathogens, cause severe hemorrhaging and organ failure with high mortality. Although some FDA-approved vaccines or therapeutics like Ervebo for Zaire Eb...
PMC9270751
core_pubmed_pmc
Comparison of 8 weeks standard treatment (rifampicin plus clarithromycin) vs. 4 weeks standard plus amoxicillin/clavulanate treatment [RC8 vs. RCA4] to shorten Buruli ulcer disease therapy (the BLMs4BU trial): study protocol for a randomized controlled multi-centre trial in Benin
Comparison of 8 weeks standard treatment (rifampicin plus clarithromycin) vs. 4 weeks standard plus amoxicillin/clavulanate treatment [RC8 vs. RCA4] to shorten Buruli ulcer disease therapy (the BLMs4BU trial): study protocol for a randomized controlled multi-centre trial in Benin Abstract Abstract Background Buruli ulc...
PMC5894414
core_pubmed_pmc
Withdrawal of Amoxicillin and Penicillin G Procaine from Milk after Intramammary Administration in Dairy Cows with Mastitis
Withdrawal of Amoxicillin and Penicillin G Procaine from Milk after Intramammary Administration in Dairy Cows with Mastitis Abstract Abstract Introduction There are many veterinary products containing β-lactam antibiotics which are used for mastitis treatment in cows. The aim of the study was to determine whether masti...
PMC6491995
core_pubmed_pmc
Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma
Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma Abstract Abstract High‐risk neuroblastoma, a predominantly TP53 wild‐type (wt) tumour, is incurable in >50% patients supporting the use of MDM2 antagonists as novel therapeutics. Id...
PMC12629135
core_pubmed_pmc
Preclinical Evaluation of a Pilocarpine–(R)-Lipoic Acid Eye Drop for Presbyopia
Preclinical Evaluation of a Pilocarpine–(R)-Lipoic Acid Eye Drop for Presbyopia Abstract Abstract Purpose Presbyopia is a progressive, age-related loss of near vision. Although current therapies offer symptomatic relief, they fail to target the underlying pathology. These studies investigated a novel dual-mechanism eye...
PMC5760943
core_pubmed_pmc
Validated LC–MS/MS method for simultaneous determination of SIM and its acid form in human plasma and cell lysate: Pharmacokinetic application
Validated LC–MS/MS method for simultaneous determination of SIM and its acid form in human plasma and cell lysate: Pharmacokinetic application Abstract Simvastatin (SIM) is a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor widely used in hyperlipidemia therapy. SIM has recently been studied for its anticancer...
PMC7292814
core_pubmed_pmc
Unbound Plasma, Total Plasma, and Whole-Blood Tacrolimus Pharmacokinetics Early After Thoracic Organ Transplantation
Unbound Plasma, Total Plasma, and Whole-Blood Tacrolimus Pharmacokinetics Early After Thoracic Organ Transplantation Abstract Background and Objective Abstract Therapeutic drug monitoring of tacrolimus whole-blood concentrations is standard care in thoracic organ transplantation. Nevertheless, toxicity may appear with ...
PMC7488503
core_pubmed_pmc
Design, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152): a novel triple angiokinase inhibitor for cancer therapy
Design, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152): a novel triple angiokinase inhibitor for cancer therapy Abstract Angiokinases, such as vascular endothelial-, fibroblast- and platelet-derived growth factor receptors...
PMC11927737
core_pubmed_pmc
Tixagevimab/cilgavimab or placebo for COVID-19 in ACTIV-2: Safety, pharmacokinetics and neutralizing and anti-drug antibodies
Tixagevimab/cilgavimab or placebo for COVID-19 in ACTIV-2: Safety, pharmacokinetics and neutralizing and anti-drug antibodies Abstract Summary Monoclonal antibodies have potential as rapidly developable agents for treatment and prevention of emerging viruses. The ACTIV-2 trial randomized persons with mild-moderate COVI...
PMC9298621
core_pubmed_pmc
The regulation of drug-metabolizing enzymes and membrane transporters by inflammation: Evidences in inflammatory diseases and age-related disorders
The regulation of drug-metabolizing enzymes and membrane transporters by inflammation: Evidences in inflammatory diseases and age-related disorders Abstract Abstract Drug-metabolizing enzymes (DMEs) and membrane transporters play important roles in the absorption, distribution, metabolism, and excretion processes that ...
PMC7485944
core_pubmed_pmc
Effect of Rifampin‐Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel
Effect of Rifampin‐Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel Abstract Abstract In vitro studies have indicated that the P2Y12 receptor antagonist selatogrel is a substrate of organic anion‐transporting‐polypeptide (OATP)1B1 and OATP1B3 that a...
PMC9324789
core_pubmed_pmc
The Effect of CYP2D6 Phenotypes on the Pharmacokinetics of Propafenone: A Systematic Review and Meta-Analysis
The Effect of CYP2D6 Phenotypes on the Pharmacokinetics of Propafenone: A Systematic Review and Meta-Analysis Abstract Abstract Propafenone (PPF) is a class 1C antiarrhythmic agent mainly metabolized by cytochrome (CYP) 2D6, CYP1A2, and CYP3A4. Previous studies have shown that CYP2D6 polymorphism influences the pharmac...
PMC9199891
core_pubmed_pmc
Evaluation of the relationship between polymorphisms in CYP2C19 and the single‐dose pharmacokinetics of omeprazole in healthy Chinese volunteers: A multicenter study
Evaluation of the relationship between polymorphisms in CYP2C19 and the single‐dose pharmacokinetics of omeprazole in healthy Chinese volunteers: A multicenter study Abstract Abstract The aim of this study was to evaluate the relationship between polymorphisms in CYP2C19 and the single‐dose pharmacokinetics (PKs) of om...
PMC4965482
core_pubmed_pmc
Lack of pharmacokinetic drug–drug interaction between ramucirumab and paclitaxel in a phase II study of patients with advanced malignant solid tumors
Lack of pharmacokinetic drug–drug interaction between ramucirumab and paclitaxel in a phase II study of patients with advanced malignant solid tumors Abstract Purpose The objective of this phase II study was to evaluate pharmacokinetic interaction potential between ramucirumab and paclitaxel in patients with advanced c...
PMC12756197
core_pubmed_pmc
Bioequivalence Study of Bedaquiline and Sirturo ® in Healthy Chinese Subjects Under Fasting and Postprandial Conditions: A Randomized, Open-Label, Single-Dose, Crossover Trial
Bioequivalence Study of Bedaquiline and Sirturo ® in Healthy Chinese Subjects Under Fasting and Postprandial Conditions: A Randomized, Open-Label, Single-Dose, Crossover Trial Abstract Background and Objective Multidrug-resistant tuberculosis remains a major global health challenge, and bedaquiline has become an essent...
PMC9875039
core_pubmed_pmc
Viral clearance, pharmacokinetics and tolerability of ensovibep in patients with mild to moderate COVID‐19: A phase 2a, open‐label, single‐dose escalation study
Viral clearance, pharmacokinetics and tolerability of ensovibep in patients with mild to moderate COVID‐19: A phase 2a, open‐label, single‐dose escalation study Abstract Abstract Aim To assess viral clearance, pharmacokinetics, tolerability and symptom evolution following ensovibep administration in symptomatic COVID‐1...
PMC9852841
core_pubmed_pmc
Expanding the toolbox of metabolically stable lipid prodrug strategies
Expanding the toolbox of metabolically stable lipid prodrug strategies Abstract Nucleoside- and nucleotide-based therapeutics are indispensable treatment options for patients suffering from malignant and viral diseases. These agents are most commonly administered to patients as prodrugs to maximize bioavailability and ...
PMC9116478
core_pubmed_pmc
Population Pharmacokinetics of Caspofungin and Dose Simulations in Heart Transplant Recipients
Population Pharmacokinetics of Caspofungin and Dose Simulations in Heart Transplant Recipients Abstract ABSTRACT The effect of heart transplantation (HTx) on the pharmacokinetics (PK) of caspofungin is not well-characterized. The aim of this study was to investigate the population PK of caspofungin in HTx and non-HTx p...
PMC3589632
core_pubmed_pmc
Population pharmacokinetic modeling of Sepantronium bromide (YM155), a small molecule survivin suppressant, in patients with non-small cell lung cancer, hormone refractory prostate cancer, or unresectable stage III or IV melanoma
Population pharmacokinetic modeling of Sepantronium bromide (YM155), a small molecule survivin suppressant, in patients with non-small cell lung cancer, hormone refractory prostate cancer, or unresectable stage III or IV melanoma Abstract Summary Purpose Population pharmacokinetics (PK) of sepantronium bromide (YM155) ...
PMC8604835
core_pubmed_pmc
Systemic exposure following intravitreal administration of therapeutic agents: an integrated pharmacokinetic approach. 1. THR-149
Systemic exposure following intravitreal administration of therapeutic agents: an integrated pharmacokinetic approach. 1. THR-149 Abstract Intravitreal (IVT) injection of pharmacological agents is an established and widely used procedure for the treatment of many posterior segment of the eye diseases. IVT injections pe...
PMC6030425
core_pubmed_pmc
Development of growth equations from longitudinal studies of body weight and height in the full term and preterm neonate: From birth to four years postnatal age
Development of growth equations from longitudinal studies of body weight and height in the full term and preterm neonate: From birth to four years postnatal age Abstract Abstract Physiologically based pharmacokinetic (PBPK) models are developed from compound‐independent information to describe important anatomical and ...
PMC8148219
core_pubmed_pmc
Machine Learning Establishes Single-Cell Calcium Dynamics as an Early Indicator of Antibiotic Response
Machine Learning Establishes Single-Cell Calcium Dynamics as an Early Indicator of Antibiotic Response Abstract Changes in bacterial physiology necessarily precede cell death in response to antibiotics. Herein we investigate the early disruption of Ca 2+ homeostasis as a marker for antibiotic response. Using a machine ...
PMC9228144
core_pubmed_pmc
Probability of Target Attainment of Tobramycin Treatment in Acute and Chronic Pseudomonas aeruginosa Lung Infection Based on Preclinical Population Pharmacokinetic Modeling
Probability of Target Attainment of Tobramycin Treatment in Acute and Chronic Pseudomonas aeruginosa Lung Infection Based on Preclinical Population Pharmacokinetic Modeling Abstract Abstract Biofilms and infectious process may alter free antimicrobial concentrations at the site of infection. Tobramycin (TOB), an aminog...
PMC12657739
core_pubmed_pmc
Phase I trial of neratinib plus palbociclib in advanced cancers with HER family alterations
Phase I trial of neratinib plus palbociclib in advanced cancers with HER family alterations Abstract Abstract Background Aberrations in the human epidermal growth factor receptor (HER) and cyclin-dependent kinase 4/6 pathways drive tumor growth. While neratinib, a pan-HER kinase inhibitor, and palbociclib, a cyclin-dep...
PMC8284446
core_pubmed_pmc
Safety, Tolerability, and Population Pharmacokinetics of Intravenous and Oral Isavuconazonium Sulfate in Pediatric Patients
Safety, Tolerability, and Population Pharmacokinetics of Intravenous and Oral Isavuconazonium Sulfate in Pediatric Patients Abstract ABSTRACT Isavuconazole, administered as the water-soluble prodrug isavuconazonium sulfate, is a new triazole agent used to treat invasive fungal infections. This phase 1 study evaluated t...
PMC12115253
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Biologic Case Studies in Monkeys and Humans Reveals the Necessity of an Additional Clearance Term
Physiologically Based Pharmacokinetic Modeling of Biologic Case Studies in Monkeys and Humans Reveals the Necessity of an Additional Clearance Term Abstract Abstract Background/Objectives : Physiologically based pharmacokinetic (PBPK) modeling is an important tool in biologic drug development. However, a standardized m...