id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC12090809
core_pubmed_pmc
Safety, pharmacokinetics, and biological activity of CD4-mimetic BNM-III-170 in SHIV-infected rhesus macaques
Safety, pharmacokinetics, and biological activity of CD4-mimetic BNM-III-170 in SHIV-infected rhesus macaques Abstract ABSTRACT Anti-HIV-1 antibodies capable of mediating ADCC are elicited by the majority of people with HIV-1 and preferentially target the “open,” CD4-bound conformation of HIV-1 envelope glycoproteins (...
PMC10447267
core_pubmed_pmc
Assessment of the potential of the MET inhibitor tepotinib to affect the pharmacokinetics of CYP3A4 and P-gp substrates
Assessment of the potential of the MET inhibitor tepotinib to affect the pharmacokinetics of CYP3A4 and P-gp substrates Abstract Tepotinib is a highly selective, potent, mesenchymal-epithelial transition factor (MET) inhibitor, approved for the treatment of non-small cell lung cancer harboring MET exon 14 skipping alte...
PMC7779054
core_pubmed_pmc
PK-DB: pharmacokinetics database for individualized and stratified computational modeling
PK-DB: pharmacokinetics database for individualized and stratified computational modeling Abstract Abstract A multitude of pharmacokinetics studies have been published. However, due to the lack of an open database, pharmacokinetics data, as well as the corresponding meta-information, have been difficult to access. We p...
PMC8287637
core_pubmed_pmc
Using mixed-effects modeling to estimate decay kinetics of response to SARS-CoV-2 infection
Using mixed-effects modeling to estimate decay kinetics of response to SARS-CoV-2 infection Abstract Abstract The duration of natural immunity in response to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a matter of some debate in the literature at present. For example, in a recent publication charact...
PMC7477452
core_pubmed_pmc
Safety, Efficacy, Pharmacokinetic and Pharmacodynamic evaluation of YF-H-2015005 for mobilizing Hematopoietic stem cells in Non-Hodgkin's Lymphoma Patients
Safety, Efficacy, Pharmacokinetic and Pharmacodynamic evaluation of YF-H-2015005 for mobilizing Hematopoietic stem cells in Non-Hodgkin's Lymphoma Patients Abstract Background: Targeting the interaction between SDF1 and CXCR4 may provide an opportunity to intervene in the hematopoietic stem cell mobilization process. A...
PMC11533098
core_pubmed_pmc
A physiologically‐based pharmacokinetic modeling approach for dosing amiodarone in children on ECMO
A physiologically‐based pharmacokinetic modeling approach for dosing amiodarone in children on ECMO Abstract Abstract Extracorporeal membrane oxygenation (ECMO) is a cardiopulmonary bypass device commonly used to treat cardiac arrest in children. The American Heart Association guidelines for cardiopulmonary resuscitati...
PMC4501444
core_pubmed_pmc
Pharmacokinetic comparison of sustained- and immediate-release formulations of cilostazol after multiple oral doses in fed healthy male Korean volunteers
Pharmacokinetic comparison of sustained- and immediate-release formulations of cilostazol after multiple oral doses in fed healthy male Korean volunteers Abstract Background A new extended-release form of cilostazol has recently been developed. This study was conducted to compare the pharmacokinetic characteristics of ...
PMC9271669
core_pubmed_pmc
The Potential Use of Antibiotics Against Helicobacter pylori Infection: Biopharmaceutical Implications
The Potential Use of Antibiotics Against Helicobacter pylori Infection: Biopharmaceutical Implications Abstract Abstract Helicobacter pylori ( H. pylori ) is a notorious, recalcitrant and silent germ, which can cause a variety of debilitating stomach diseases, including gastric and duodenal ulcers and gastric cancer. T...
PMC12871814
core_pubmed_pmc
Development of Physiologically Based Liver Distribution Model that Incorporates Intracellular Lipid Partitioning and Binding to Fatty Acid Binding Protein 1 (FABP1)
Development of Physiologically Based Liver Distribution Model that Incorporates Intracellular Lipid Partitioning and Binding to Fatty Acid Binding Protein 1 (FABP1) Abstract Steady-state volume of distribution ( V ss ) can be predicted using tissue-to-plasma partition coefficients K p and tissue volumes. K p values are...
PMC10747965
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling in Neonates: Current Status and Future Perspectives
Physiologically Based Pharmacokinetic Modeling in Neonates: Current Status and Future Perspectives Abstract Abstract Rational drug use in special populations is a clinical problem that doctors and pharma-cists must consider seriously. Neonates are the most physiologically immature and vulnerable to drug dosing. There i...
PMC8981429
core_pubmed_pmc
Pharmacokinetic changes for newer antiepileptic drugs and seizure control during pregnancy
Pharmacokinetic changes for newer antiepileptic drugs and seizure control during pregnancy Abstract Abstract Objective To investigate pharmacokinetic changes in newer antiepileptic drugs (AEDs) and assess seizure frequencies and risk factors of increased seizures during pregnancy in women with epilepsy (WWE). Methods A...
PMC12800558
core_pubmed_pmc
Anesthetic implications of psychotropic medications: a narrative review
Anesthetic implications of psychotropic medications: a narrative review Abstract Abstract Psychotropic medications are widely used in the treatment of mental and nonmental disorders such as chronic pain and other off-label indications. With the increase in comorbidities of mental and physical illnesses, anesthesiologis...
PMC3406004
core_pubmed_pmc
Modeling of Pharmacokinetics of Cocaine in Human Reveals the Feasibility for Development of Enzyme Therapies for Drugs of Abuse
Modeling of Pharmacokinetics of Cocaine in Human Reveals the Feasibility for Development of Enzyme Therapies for Drugs of Abuse Abstract A promising strategy for drug abuse treatment is to accelerate the drug metabolism by administration of a drug-metabolizing enzyme. The question is how effectively an enzyme can actua...
PMC7705402
core_pubmed_pmc
Dosing Considerations for Antibodies Against COVID-19
Dosing Considerations for Antibodies Against COVID-19 Abstract At present, no cure is available for COVID-19 but vaccines, antiviral drugs, immunoglobulins, or the combination of immunoglobulins with antiviral drugs have been suggested and are in clinical trials. The purpose of this paper is to discuss the role of a ph...
PMC4351431
core_pubmed_pmc
Pharmacokinetics of diluted (U20) insulin aspart compared with standard (U100) in children aged 3–6 years with type 1 diabetes during closed-loop insulin delivery: a randomised clinical trial
Pharmacokinetics of diluted (U20) insulin aspart compared with standard (U100) in children aged 3–6 years with type 1 diabetes during closed-loop insulin delivery: a randomised clinical trial Abstract Abstract Aims/hypothesis The aim of this study was to compare the pharmacokinetics of two different concentrations of i...
PMC11319329
core_pubmed_pmc
Design of new α-glucosidase inhibitors based on the bis-4-hydroxycoumarin skeleton: Synthesis, evaluation, and in silico studies
Design of new α-glucosidase inhibitors based on the bis-4-hydroxycoumarin skeleton: Synthesis, evaluation, and in silico studies Abstract Abstract In this work, we have reported the design, synthesis, in vitro, and in silico enzymatic evaluation of new bis-4-hydroxycoumarin-based phenoxy-1,2,3-triazole- N -phenylacetam...
PMC7883310
core_pubmed_pmc
Bioequivalence of intramuscular and subcutaneous peginterferon beta-1a: results of a phase I, open-label crossover study in healthy volunteers
Bioequivalence of intramuscular and subcutaneous peginterferon beta-1a: results of a phase I, open-label crossover study in healthy volunteers Abstract Abstract Background: Peginterferon beta-1a administered every 2 weeks via subcutaneous (SC) injection is approved to treat adult patients with relapsing-remitting multi...
PMC10675857
core_pubmed_pmc
Risk adjustment model for tuberculosis compared to non-tuberculosis mycobacterium or latent tuberculosis infection: Center for Personalized Precision Medicine of Tuberculosis (cPMTb) cohort database
Risk adjustment model for tuberculosis compared to non-tuberculosis mycobacterium or latent tuberculosis infection: Center for Personalized Precision Medicine of Tuberculosis (cPMTb) cohort database Abstract Background The Center for Personalized Precision Medicine of Tuberculosis (cPMTb) was constructed to develop per...
PMC6717060
core_pubmed_pmc
Results from a Phase 1 Study of Sodium Selenite in Combination with Palliative Radiation Therapy in Patients with Metastatic Cancer
Results from a Phase 1 Study of Sodium Selenite in Combination with Palliative Radiation Therapy in Patients with Metastatic Cancer Abstract In preclinical studies, selenite had single agent activity and radiosensitized tumors in vivo. Here we report results from a Phase 1 trial in 15 patients with metastatic cancer tr...
PMC5907431
core_pubmed_pmc
Effect site concentration of propofol at induction and recovery of anaesthesia - A correlative dose-response study
Effect site concentration of propofol at induction and recovery of anaesthesia - A correlative dose-response study Abstract Background and Aims: Sound knowledge about effect site concentration (Ce) of propofol aids in smooth induction, maintenance and early recovery. We studied the correlation between Ce of propofol at...
PMC7884331
core_pubmed_pmc
Targeting Salmonella Typhimurium Invasion and Intracellular Survival Using Pyrogallol
Targeting Salmonella Typhimurium Invasion and Intracellular Survival Using Pyrogallol Abstract Abstract Salmonella enterica serovar Typhimurium, an intracellular pathogen, evades the host immune response mechanisms to cause gastroenteritis in animals and humans. After invading the host cells, the bacteria proliferate i...
PMC9405298
core_pubmed_pmc
The Effect of Different Colistin Dosing Regimens on Nephrotoxicity: A Cohort Study
The Effect of Different Colistin Dosing Regimens on Nephrotoxicity: A Cohort Study Abstract (1) Background: It is not known whether different daily dosing schemes have different effects on colistin nephrotoxicity. We examined the effect of once- versus twice- or thrice-daily doses of colistin on renal function. (2) Met...
PMC9709912
core_pubmed_pmc
Selective Inhibitor Design for Kinase Homologs Using Multiobjective Monte Carlo Tree Search
Selective Inhibitor Design for Kinase Homologs Using Multiobjective Monte Carlo Tree Search Abstract Designing highly selective molecules for a drug target protein is a challenging task in drug discovery. This task can be regarded as a multiobjective problem that simultaneously satisfies criteria for various objectives...
PMC4432110
core_pubmed_pmc
Using sensitivity equations for computing gradients of the FOCE and FOCEI approximations to the population likelihood
Using sensitivity equations for computing gradients of the FOCE and FOCEI approximations to the population likelihood Abstract The first order conditional estimation (FOCE) method is still one of the parameter estimation workhorses for nonlinear mixed effects (NLME) modeling used in population pharmacokinetics and phar...
PMC8522761
core_pubmed_pmc
Relationship between Plasma and Intracellular Concentrations of Bedaquiline and Its M2 Metabolite in South African Patients with Rifampin-Resistant Tuberculosis
Relationship between Plasma and Intracellular Concentrations of Bedaquiline and Its M2 Metabolite in South African Patients with Rifampin-Resistant Tuberculosis Abstract ABSTRACT Bedaquiline is recommended for the treatment of all patients with rifampin-resistant tuberculosis (RR-TB). Bedaquiline accumulates within cel...
PMC6497337
core_pubmed_pmc
The MOVEMENT Trial
The MOVEMENT Trial Abstract Abstract Background Morphine administration is a strong predictor of delayed onset of action of orally administered ticagrelor in patients with ST‐segment–elevation myocardial infarction, likely because of impaired gastrointestinal motility. The aim of this study was to evaluate whether the ...
PMC12869162
core_pubmed_pmc
Cergutuzumab Amunaleukin in Combination with Atezolizumab in Patients with Carcinoembryonic Antigen–Positive Advanced/Metastatic Solid Tumors
Cergutuzumab Amunaleukin in Combination with Atezolizumab in Patients with Carcinoembryonic Antigen–Positive Advanced/Metastatic Solid Tumors Abstract Abstract Purpose: Cergutuzumab amunaleukin (CA) is an immunocytokine comprising a variant form of interleukin 2 (IL2) [constructed to avoid CD25 binding and regulatory T...
PMC12403246
core_pubmed_pmc
Antimicrobial susceptibility of Legionella gormanii : species-specific ECOFFs, distinct MICs for rifampin versus Legionella pneumophila
Antimicrobial susceptibility of Legionella gormanii : species-specific ECOFFs, distinct MICs for rifampin versus Legionella pneumophila Abstract Background Legionella gormanii (L. gormanii) is an emerging pathogen causing legionellosis, yet it is much less studied than the predominant species, L. pneumophila . Clinical...
PMC3153011
core_pubmed_pmc
Stereoselective Inhibition of the hERG1 Potassium Channel
Stereoselective Inhibition of the hERG1 Potassium Channel Abstract Abstract A growing number of drugs have been shown to prolong cardiac repolarization, predisposing individuals to life-threatening ventricular arrhythmias known as Torsades de Pointes . Most of these drugs are known to interfere with the human ether à-g...
PMC8395812
core_pubmed_pmc
Selective Serotonin Reuptake Inhibitors and Adverse Effects: A Narrative Review
Selective Serotonin Reuptake Inhibitors and Adverse Effects: A Narrative Review Abstract Abstract Depression is the most prevalent psychiatric disorder in the world, affecting 4.4% of the global population. Despite an array of treatment modalities, depressive disorders remain difficult to manage due to many factors. Be...
PMC10410082
core_pubmed_pmc
Individualized antibiotic dosage regimens for patients with augmented renal clearance
Individualized antibiotic dosage regimens for patients with augmented renal clearance Abstract Abstract Objectives: Augmented renal clearance (ARC) is a state of enhanced renal function commonly observed in 30%–65% of critically ill patients despite normal serum creatinine levels. Using unadjusted standard dosing regim...
PMC12487286
core_pubmed_pmc
Preclinical assessment of pharmacokinetics and anticonvulsant activity of CBDTech, a novel orally administered cannabidiol (CBD) formulation for seizure and epilepsy
Preclinical assessment of pharmacokinetics and anticonvulsant activity of CBDTech, a novel orally administered cannabidiol (CBD) formulation for seizure and epilepsy Abstract Abstract Oral cannabidiol (CBD) product use is increasing despite suboptimal pharmacokinetics (PK) of currently available formulations. This stud...
PMC12698292
core_pubmed_pmc
Residual Effects of Acute and Subchronic Zolpidem Treatments on Attentional Processes in Aged Female Rats
Residual Effects of Acute and Subchronic Zolpidem Treatments on Attentional Processes in Aged Female Rats Abstract ABSTRACT Rational Zolpidem, a hypnotic Z‐drug commonly prescribed to promote sleep, is predominantly used over the age of 50. In this elderly population, adverse behavioral disturbances, impaired driving p...
PMC5402624
core_pubmed_pmc
Low body weight and body mass index may be associated with musculoskeletal pain following imatinib discontinuation in chronic myeloid leukemia
Low body weight and body mass index may be associated with musculoskeletal pain following imatinib discontinuation in chronic myeloid leukemia Abstract Abstract It is difficult to predict musculoskeletal pain as a withdrawal syndrome following the discontinuation of imatinib (IM) in patients with chronic myeloid leukem...
PMC8666106
core_pubmed_pmc
2-Phenoxyacetamide derivatives as SARS-CoV-2 main protease inhibitor: In silico studies
2-Phenoxyacetamide derivatives as SARS-CoV-2 main protease inhibitor: In silico studies Abstract 2-Phenoxyacetamide group has been identified as one of markers in the discovery and development of SARS-CoV-2 antiviral agent through its main protease (M pro ) inhibition pathway. This study aims to study a series of 2-phe...
PMC11884701
core_pubmed_pmc
Predictors of clozapine concentration and psychiatric symptoms in patients with schizophrenia
Predictors of clozapine concentration and psychiatric symptoms in patients with schizophrenia Abstract Clozapine has superior efficacy to other antipsychotics, especially in patients with treatment-resistant schizophrenia. However, its pharmacokinetics and pharmacodynamics vary largely among patients. We aimed to evalu...
PMC12103860
core_pubmed_pmc
Quality by Design Formulation Approach for the Development of Orodispersible Tablets of Dexlansoprazole
Quality by Design Formulation Approach for the Development of Orodispersible Tablets of Dexlansoprazole Abstract Purpose Dexlansoprazole (DX) is a commercially available proton pump inhibitor (PPI). It is an oral delayed-release (DR) formulation that takes 1–2 h to reach the systemic circulation. To overcome the delaye...
PMC7007440
core_pubmed_pmc
Population Pharmacokinetics of Intravenous Salbutamol in Children with Refractory Status Asthmaticus
Population Pharmacokinetics of Intravenous Salbutamol in Children with Refractory Status Asthmaticus Abstract Abstract Background Intravenous salbutamol is used to treat children with refractory status asthmaticus, however insufficient pharmacokinetic data are available to guide initial and subsequent dosing recommenda...
PMC12249819
core_pubmed_pmc
Structure-Based Discovery of Orthosteric Non-Peptide GLP-1R Agonists via Integrated Virtual Screening and Molecular Dynamics
Structure-Based Discovery of Orthosteric Non-Peptide GLP-1R Agonists via Integrated Virtual Screening and Molecular Dynamics Abstract The development of orally bioavailable non-peptidomimetic glucagon-like peptide-1 receptor agonists (GLP-1RAs) offers a promising therapeutic avenue for the treatment of type 2 diabetes ...
PMC9231369
core_pubmed_pmc
Relation between Plasma Trough Concentration of Pazopanib and Progression-Free Survival in Metastatic Soft Tissue Sarcoma Patients
Relation between Plasma Trough Concentration of Pazopanib and Progression-Free Survival in Metastatic Soft Tissue Sarcoma Patients Abstract Abstract Background: Pazopanib (PAZ) is an oral angiogenesis inhibitor approved to treat soft tissue sarcoma (STS) but associated with a large interpatient pharmacokinetic (PK) var...
PMC3592920
core_pubmed_pmc
Reduced Susceptibility of Plasmodium falciparum to Artesunate in Southern Myanmar
Reduced Susceptibility of Plasmodium falciparum to Artesunate in Southern Myanmar Abstract Background Plasmodium falciparum resistance to artemisinins, the first line treatment for malaria worldwide, has been reported in western Cambodia. Resistance is characterized by significantly delayed clearance of parasites follo...
PMC6282763
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of Multiple Rising Doses of BI 655064, an Antagonistic Anti‐CD40 Antibody, in Healthy Subjects: A Potential Novel Treatment for Autoimmune Diseases
Safety, Pharmacokinetics, and Pharmacodynamics of Multiple Rising Doses of BI 655064, an Antagonistic Anti‐CD40 Antibody, in Healthy Subjects: A Potential Novel Treatment for Autoimmune Diseases Abstract Abstract BI 655064 is a humanized antagonistic anti‐cluster of differentiation (CD) 40 monoclonal antibody that sele...
PMC8758692
core_pubmed_pmc
Extension of human GCSF serum half-life by the fusion of albumin binding domain
Extension of human GCSF serum half-life by the fusion of albumin binding domain Abstract Abstract Granulocyte colony stimulating factor (GCSF) can decrease mortality of patients undergo chemotherapy through increasing neutrophil counts. Many strategies have been developed to improve its blood circulating time. Albumin ...
PMC9395490
core_pubmed_pmc
An open-label, crossover study to compare different formulations and evaluate effect of food on pharmacokinetics of pimitespib in patients with advanced solid tumors
An open-label, crossover study to compare different formulations and evaluate effect of food on pharmacokinetics of pimitespib in patients with advanced solid tumors Abstract Abstract This study compared the bioavailability of two pimitespib formulations (Formulations A and B), evaluated the food effect on Formulation ...
PMC12297723
core_pubmed_pmc
Development and application of an LC–MS/MS method for quantification of fosmidomycin in human and rat plasma
Development and application of an LC–MS/MS method for quantification of fosmidomycin in human and rat plasma Abstract Background Malaria still poses a significant burden on global health, with millions of cases reported annually and rising resistance to current treatments, emphasizing the need for new therapeutic strat...
PMC9853254
core_pubmed_pmc
INBRX-120, a CD8α-targeted detuned IL-2 that selectively expands and activates tumoricidal effector cells for safe and durable in vivo responses
INBRX-120, a CD8α-targeted detuned IL-2 that selectively expands and activates tumoricidal effector cells for safe and durable in vivo responses Abstract Background As a major driver of lymphocyte proliferation and activation interleukin 2 (IL-2) is a crucial mediator for antitumor responses. Despite promising activity...
PMC11884746
core_pubmed_pmc
Pharmacokinetics of two pharmaceutical presentations of benznidazole in adult Trypanosoma cruzi infected population
Pharmacokinetics of two pharmaceutical presentations of benznidazole in adult Trypanosoma cruzi infected population Abstract Abstract BACKGROUND Benznidazole (BNZ) is the primary treatment for Chagas disease. While pharmacokinetic studies of BNZ began in the 1970s, its metabolism and excretion are not fully understood....
PMC5226997
core_pubmed_pmc
Effects of cytochrome P450 (CYP3A4 and CYP2C19) inhibition and induction on the exposure of selumetinib, a MEK1/2 inhibitor, in healthy subjects: results from two clinical trials
Effects of cytochrome P450 (CYP3A4 and CYP2C19) inhibition and induction on the exposure of selumetinib, a MEK1/2 inhibitor, in healthy subjects: results from two clinical trials Abstract Purpose Two phase I, open-label trials in healthy subjects assessed whether co-administration with CYP3A4/CYP2C19 inhibitors, itraco...
PMC4532346
core_pubmed_pmc
Characterization of preclinical in vitro and in vivo pharmacokinetics properties for KBP-7018, a new tyrosine kinase inhibitor candidate for treatment of idiopathic pulmonary fibrosis
Characterization of preclinical in vitro and in vivo pharmacokinetics properties for KBP-7018, a new tyrosine kinase inhibitor candidate for treatment of idiopathic pulmonary fibrosis Abstract Abstract KBP-7018 is a novel selective tyrosine kinase inhibitor with potential for the treatment of idiopathic pulmonary fibro...
PMC11311898
core_pubmed_pmc
Phase 1, placebo-controlled, single ascending dose trial to evaluate the safety, pharmacokinetics and effect on altered states of consciousness of intranasal BPL-003 (5-methoxy- N,N -dimethyltryptamine benzoate) in healthy participants
Phase 1, placebo-controlled, single ascending dose trial to evaluate the safety, pharmacokinetics and effect on altered states of consciousness of intranasal BPL-003 (5-methoxy- N,N -dimethyltryptamine benzoate) in healthy participants Abstract Abstract Aims: To investigate the safety, tolerability, pharmacokinetics (P...
PMC8129716
core_pubmed_pmc
Comprehensive PBPK model to predict drug interaction potential of Zanubrutinib as a victim or perpetrator
Comprehensive PBPK model to predict drug interaction potential of Zanubrutinib as a victim or perpetrator Abstract Abstract A physiologically based pharmacokinetic (PBPK) model was developed to evaluate and predict (1) the effect of concomitant cytochrome P450 3A (CYP3A) inhibitors or inducers on the exposures of zanub...
PMC7557484
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial
Pharmacokinetics and pharmacodynamics of intranasal remimazolam—a randomized controlled clinical trial Abstract Abstract Purpose Remimazolam is a novel and ultra-short-acting sedative currently developed for intravenous use in procedural sedation, general anesthesia, and ICU sedation. However, intravenous administratio...
PMC11563356
core_pubmed_pmc
Associations between urinary phytoestrogen mixed metabolites and osteoarthritis risk
Associations between urinary phytoestrogen mixed metabolites and osteoarthritis risk Abstract Abstract Background This study aims to explore the relationship between urinary phytoestrogen mixed metabolites and the risk of osteoarthritis (OA). Methods Using data from the National Health and Nutrition Examination Survey ...
PMC5382562
core_pubmed_pmc
Preclinical development of a humanized neutralizing antibody targeting HGF
Preclinical development of a humanized neutralizing antibody targeting HGF Abstract Hepatocyte growth factor (HGF) and its receptor, cMET, play critical roles in cell proliferation, angiogenesis and invasion in a wide variety of cancers. We therefore examined the anti-tumor activity of the humanized monoclonal anti-HGF...
PMC11054066
core_pubmed_pmc
View on Metformin: Antidiabetic and Pleiotropic Effects, Pharmacokinetics, Side Effects, and Sex-Related Differences
View on Metformin: Antidiabetic and Pleiotropic Effects, Pharmacokinetics, Side Effects, and Sex-Related Differences Abstract Abstract Metformin is a synthetic biguanide used as an antidiabetic drug in type 2 diabetes mellitus, achieved by studying the bioactive metabolites of Galega officinalis L. It is also used off-...
PMC5844872
core_pubmed_pmc
Glyco-engineered Long Acting FGF21 Variant with Optimal Pharmaceutical and Pharmacokinetic Properties to Enable Weekly to Twice Monthly Subcutaneous Dosing
Glyco-engineered Long Acting FGF21 Variant with Optimal Pharmaceutical and Pharmacokinetic Properties to Enable Weekly to Twice Monthly Subcutaneous Dosing Abstract Abstract Pharmacological administration of FGF21 analogues has shown robust body weight reduction and lipid profile improvement in both dysmetabolic animal...
PMC11674395
core_pubmed_pmc
Updates on the Activity, Efficacy and Emerging Mechanisms of Resistance to Cefiderocol
Updates on the Activity, Efficacy and Emerging Mechanisms of Resistance to Cefiderocol Abstract In recent years, novel antimicrobials have been developed to counter the emergence of antimicrobial resistance and provide effective therapeutic options against multidrug-resistant (MDR) Gram-negative bacilli (GNB). Cefidero...
PMC9381674
core_pubmed_pmc
Effects of Itraconazole and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Milvexian, A Factor XIa Inhibitor
Effects of Itraconazole and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Milvexian, A Factor XIa Inhibitor Abstract Introduction Modulation of Factor XIa (FXIa) may provide a novel mechanism for systemic anticoagulation with the potential to improve the risk-benefit profile observed with existing anticoagu...
PMC9085911
core_pubmed_pmc
Pharmacokinetic and excretion study of three alkaloids in rats using UPLC-MS/MS after oral administration of menispermi rhizoma capsules †
Pharmacokinetic and excretion study of three alkaloids in rats using UPLC-MS/MS after oral administration of menispermi rhizoma capsules † Abstract A sensitive, specific and rapid ultra-performance liquid chromatography tandem mass spectrometry method (UPLC-MS/MS) was developed for simultaneous determination of three m...
PMC12567995
core_pubmed_pmc
Building Sub-Saharan African PBPK Populations Reveals Critical Data Gaps: A Case Study on Aflatoxin B1
Building Sub-Saharan African PBPK Populations Reveals Critical Data Gaps: A Case Study on Aflatoxin B1 Abstract Abstract Physiologically based pharmacokinetic (PBPK) models allow to simulate the behaviour of compounds in diverse physiological populations. However, the categorization of individuals into distinct populat...
PMC4868728
core_pubmed_pmc
Tea nanoparticle, a safe and biocompatible nanocarrier, greatly potentiates the anticancer activity of doxorubicin
Tea nanoparticle, a safe and biocompatible nanocarrier, greatly potentiates the anticancer activity of doxorubicin Abstract Abstract An infusion-dialysis based procedure has been developed as an approach to isolate organic nanoparticles from green tea. Tea nanoparticle (TNP) can effectively load doxorubicin (DOX) via e...
PMC7468366
core_pubmed_pmc
Physiologically based pharmacokinetic–pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans
Physiologically based pharmacokinetic–pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans Abstract Vonoprazan is characterized as having a long-lasting antisecretory effect on gastric acid....
PMC12881041
core_pubmed_pmc
Population Pharmacokinetics of Levosimendan and its Metabolites OR-1855 and OR-1896 in Critically Ill Adults, Neonates and Infants on Veno-Arterial ECMO
Population Pharmacokinetics of Levosimendan and its Metabolites OR-1855 and OR-1896 in Critically Ill Adults, Neonates and Infants on Veno-Arterial ECMO Abstract Abstract Background and Objective Levosimendan is an inotrope and vasodilator agent commonly used in critical care, particularly to facilitate weaning from ve...
PMC10269072
core_pubmed_pmc
Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model
Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model Abstract ABSTRACT The development of new combinations of antimalarial drugs is urgently needed to prevent the spread of parasites resistant to drugs in clinical use and contribute to the control and eradica...
PMC4521867
core_pubmed_pmc
Activity Profile of an FDA-Approved Compound Library against Schistosoma mansoni
Activity Profile of an FDA-Approved Compound Library against Schistosoma mansoni Abstract Background As plans to expand mass drug treatment campaigns to fight schistosomiasis form, worries about reliance on praziquantel as the sole available treatment motivate the investigation for novel antischistosomal compounds. Dru...
PMC12582174
core_pubmed_pmc
A First-in-Human Study of Givastomig, a CLDN18.2 and 4-1BB Bispecific Antibody, as Monotherapy in Patients with CLDN18.2-Positive Advanced or Metastatic Solid Tumors
A First-in-Human Study of Givastomig, a CLDN18.2 and 4-1BB Bispecific Antibody, as Monotherapy in Patients with CLDN18.2-Positive Advanced or Metastatic Solid Tumors Abstract Abstract Purpose: Givastomig is a bispecific antibody that targets CLDN18.2 and conditionally activates local 4-1BB–expressing T cells. This firs...
PMC6600784
core_pubmed_pmc
Preclinical Pharmacokinetic and Safety Studies of Copper-Diacetyl-Bis( N 4 -Methylthiosemicarbazone) (Cu-ATSM): Translational Studies for Internal Radiotherapy
Preclinical Pharmacokinetic and Safety Studies of Copper-Diacetyl-Bis( N 4 -Methylthiosemicarbazone) (Cu-ATSM): Translational Studies for Internal Radiotherapy Abstract Hypoxia plays important roles in the prognosis of malignant brain tumors such as glioblastoma because it causes drug delivery deficiencies and the indu...
PMC7511286
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetics of Vidofludimus calcium (IMU-838) After Single and Multiple Ascending Oral Doses in Healthy Male Subjects
Safety, Tolerability and Pharmacokinetics of Vidofludimus calcium (IMU-838) After Single and Multiple Ascending Oral Doses in Healthy Male Subjects Abstract Background and Objective Vidofludimus is a potent and selective inhibitor of human mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). The clinical efficacy...
PMC7153885
core_pubmed_pmc
Pharmacokinetics and safety after once and twice a day doses of meclizine hydrochloride administered to children with achondroplasia
Pharmacokinetics and safety after once and twice a day doses of meclizine hydrochloride administered to children with achondroplasia Abstract Abstract Achondroplasia (ACH) is the most common short-limbed skeletal dysplasia caused by activating mutations in the fibroblast growth factor receptor 3 ( FGFR3 ) gene. We iden...
PMC12131014
core_pubmed_pmc
Oxidant-free cross-dehydrogenative oxyalkylation enables late-stage functionalization of drugs
Oxidant-free cross-dehydrogenative oxyalkylation enables late-stage functionalization of drugs Abstract Abstract Late-stage functionalization is an attractive strategy that allows chemists to bypass lengthy synthetic processes, facilitating the rapid generation of drug analogs with potentially enhanced pharmacokinetic ...
PMC3984826
core_pubmed_pmc
The Effects of Acute Hydrogen Sulfide Poisoning on Cytochrome P450 Isoforms Activity in Rats
The Effects of Acute Hydrogen Sulfide Poisoning on Cytochrome P450 Isoforms Activity in Rats Abstract Hydrogen sulfide (H 2 S) is the second leading cause of toxin related death (after carbon monoxide) in the workplace. H 2 S is absorbed by the upper respiratory tract mucosa, and it causes histotoxic hypoxemia and resp...
PMC12653867
core_pubmed_pmc
Pharmacokinetics and Exposure–Response During Infliximab Induction Therapy in Pediatric IBD Using Point-of-Care Assay
Pharmacokinetics and Exposure–Response During Infliximab Induction Therapy in Pediatric IBD Using Point-of-Care Assay Abstract Background : Pharmacokinetic therapeutic failure with infliximab during induction therapy can pose a significant challenge for clinicians. The objective of this study was to conduct population ...
PMC4840291
core_pubmed_pmc
MDM2 Inhibition Sensitizes Prostate Cancer Cells to Androgen Ablation and Radiotherapy in a p53-Dependent Manner 1 2
MDM2 Inhibition Sensitizes Prostate Cancer Cells to Androgen Ablation and Radiotherapy in a p53-Dependent Manner 1 2 Abstract PURPOSE: Increased murine double minute 2 (MDM2) expression, independent of p53 status, is associated with increased cancer-specific mortality for men with prostate cancer treated with radiother...
PMC12750218
core_pubmed_pmc
Characterization of the Interaction between Human α 1 ‑Acid Glycoprotein and Apremilast Enantiomers: HPLC, Isothermal Titration Calorimetry, Ultracentrifugation, and Docking Studies
Characterization of the Interaction between Human α 1 ‑Acid Glycoprotein and Apremilast Enantiomers: HPLC, Isothermal Titration Calorimetry, Ultracentrifugation, and Docking Studies Abstract The interactions between human α 1 -acid glycoprotein (AGP) and the enantiomers of apremilast (APR) were investigated by using a ...
PMC12481680
core_pubmed_pmc
Development of carboximidamide small molecule nanogels as potent antimicrobial functional drug delivery systems
Development of carboximidamide small molecule nanogels as potent antimicrobial functional drug delivery systems Abstract The escalating threat of multidrug-resistant (MDR) bacterial infections necessitates innovative antimicrobial strategies with enhanced potency, selectivity, and pharmacokinetic profiles. In this stud...
PMC9764074
core_pubmed_pmc
Small molecule-based immunomodulators for cancer therapy
Small molecule-based immunomodulators for cancer therapy Abstract Immunotherapy has led to a paradigm shift in the treatment of cancer. Current cancer immunotherapies are mostly antibody-based, thus possessing advantages in regard to pharmacodynamics ( e.g ., specificity and efficacy). However, they have limitations in...
PMC9662205
core_pubmed_pmc
Model enhanced reinforcement learning to enable precision dosing: A theoretical case study with dosing of propofol
Model enhanced reinforcement learning to enable precision dosing: A theoretical case study with dosing of propofol Abstract Abstract Extending the potential of precision dosing requires evaluating methodologies offering more flexibility and higher degree of personalization. Reinforcement learning (RL) holds promise in ...
PMC10419712
core_pubmed_pmc
Therapeutic Drug Monitoring of Direct Oral Anticoagulants in Patients with Extremely Low and High Body Weight—Pilot Study
Therapeutic Drug Monitoring of Direct Oral Anticoagulants in Patients with Extremely Low and High Body Weight—Pilot Study Abstract Phase III clinical trials for individual direct oral anticoagulants (DOACs) contained a limited representation of subjects with abnormal body weight, which were mostly limited to a BMI > 40...
PMC6618134
core_pubmed_pmc
Single‐Dose Pharmacokinetics and Safety of Solriamfetol in Participants With Normal or Impaired Renal Function and With End‐Stage Renal Disease Requiring Hemodialysis
Single‐Dose Pharmacokinetics and Safety of Solriamfetol in Participants With Normal or Impaired Renal Function and With End‐Stage Renal Disease Requiring Hemodialysis Abstract Abstract Solriamfetol (JZP‐110), a selective dopamine and norepinephrine reuptake inhibitor with wake‐promoting effects, is renally excreted ∼90...
PMC3108694
core_pubmed_pmc
Glargine and detemir: Safety and efficacy profiles of the long-acting basal insulin analogs
Glargine and detemir: Safety and efficacy profiles of the long-acting basal insulin analogs Abstract Abstract Diabetes mellitus is a growing public health concern in the US and worldwide. Insulin therapy is the cornerstone of diabetes therapy, and the use of basal insulins will increase as clinicians strive to help the...
PMC5801534
core_pubmed_pmc
Development and evaluation of exemestane-loaded lyotropic liquid crystalline gel formulations
Development and evaluation of exemestane-loaded lyotropic liquid crystalline gel formulations Abstract Abstract Introduction: The use of liquid crystalline (LC) gel formulations for drug delivery has considerably improved the current delivery methods in terms of bioavailability and efficacy. The purpose of this study w...
PMC9138011
core_pubmed_pmc
Combined PK/PD Index May Be a More Appropriate PK/PD Index for Cefoperazone/Sulbactam against Acinetobacter baumannii in Patients with Hospital-Acquired Pneumonia
Combined PK/PD Index May Be a More Appropriate PK/PD Index for Cefoperazone/Sulbactam against Acinetobacter baumannii in Patients with Hospital-Acquired Pneumonia Abstract Cefoperazone/sulbactam (CPZ/SUL) is a β-lactam and β-lactamase inhibitor combination therapy for the treatment of respiratory tract infections. Usin...
PMC4807048
core_pubmed_pmc
High Performance Liquid Chromatographic Assay for the Simultaneous Determination of Posaconazole and Vincristine in Rat Plasma
High Performance Liquid Chromatographic Assay for the Simultaneous Determination of Posaconazole and Vincristine in Rat Plasma Abstract Purpose . Developing a validated HPLC-DAD method for simultaneous determination of posaconazole (PSZ) and vincristine (VCR) in rat plasma. Methods . PSZ, VCR, and itraconazole (ITZ) we...
PMC5605788
core_pubmed_pmc
Repurposing Lesogaberan to Promote Human Islet Cell Survival and β -Cell Replication
Repurposing Lesogaberan to Promote Human Islet Cell Survival and β -Cell Replication Abstract The activation of β -cell's A- and B-type gamma-aminobutyric acid receptors (GABA A -Rs and GABA B -Rs) can promote their survival and replication, and the activation of α -cell GABA A -Rs promotes their conversion into β -cel...
PMC6120654
core_pubmed_pmc
Efficacy of cloxacillin versus cefazolin for methicillin-susceptible Staphylococcus aureus bacteraemia (CloCeBa): study protocol for a randomised, controlled, non-inferiority trial
Efficacy of cloxacillin versus cefazolin for methicillin-susceptible Staphylococcus aureus bacteraemia (CloCeBa): study protocol for a randomised, controlled, non-inferiority trial Abstract Introduction Methicillin-susceptible Staphylococcus aureus (MSSA) bacteraemia is a common and severe disease responsible for appro...
PMC5672931
core_pubmed_pmc
Phase 1 safety, pharmacokinetic and pharmacodynamic study of the cyclin-dependent kinase inhibitor dinaciclib administered every three weeks in patients with advanced malignancies
Phase 1 safety, pharmacokinetic and pharmacodynamic study of the cyclin-dependent kinase inhibitor dinaciclib administered every three weeks in patients with advanced malignancies Abstract Background: Dinaciclib is a potent inhibitor of cell cycle and transcriptional cyclin-dependent kinases. This Phase 1 study evaluat...
PMC9370311
core_pubmed_pmc
Resveratrol Effects on the Reproductive System in Ovariectomized Rats: Deciphering Possible Mechanisms
Resveratrol Effects on the Reproductive System in Ovariectomized Rats: Deciphering Possible Mechanisms Abstract Phytoestrogen resveratrol (R) has been demonstrated to benefit human reproductive health. However, R bioavailability and pharmacokinetics are still problematic under oral supplementation. We used an experimen...
PMC4780231
core_pubmed_pmc
Addressing Early Life Sensitivity Using Physiologically Based Pharmacokinetic Modeling and In Vitro to In Vivo Extrapolation
Addressing Early Life Sensitivity Using Physiologically Based Pharmacokinetic Modeling and In Vitro to In Vivo Extrapolation Abstract Physiologically based pharmacokinetic (PBPK) modeling can provide an effective way to utilize in vitro and in silico based information in modern risk assessment for children and other po...
PMC6625463
core_pubmed_pmc
Pharmacokinetic changes and therapeutic drug monitoring of lamotrigine during pregnancy
Pharmacokinetic changes and therapeutic drug monitoring of lamotrigine during pregnancy Abstract Abstract Objectives To evaluate the pharmacokinetic changes in lamotrigine (LTG) from prepregnancy to postpartum and to assess the impact of therapeutic drug monitoring (TDM) on seizure management during pregnancy in a Chin...
PMC11176942
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, efficacy, and safety of ravulizumab in pediatric paroxysmal nocturnal hemoglobinuria
Pharmacokinetics, pharmacodynamics, efficacy, and safety of ravulizumab in pediatric paroxysmal nocturnal hemoglobinuria Abstract Key Points • PNH is a rare blood disease that can affect children, with symptoms that may result in fatal complications if left untreated. • In children with PNH ravulizumab controlled termi...
PMC11793854
core_pubmed_pmc
Optimal Transport Based Graph Kernels for Drug Property Prediction
Optimal Transport Based Graph Kernels for Drug Property Prediction Abstract Objective: The development of pharmaceutical agents relies heavily on optimizing their pharmacodynamics, pharmacokinetics, and toxicological properties, collectively known as ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity)...
PMC3797319
core_pubmed_pmc
Comparison between the pharmacokinetics of meranzin hydrate in a rat model of chronic depression and in controls following the oral administration of Chaihu-Shugan-San
Comparison between the pharmacokinetics of meranzin hydrate in a rat model of chronic depression and in controls following the oral administration of Chaihu-Shugan-San Abstract Abstract Previous studies have shown that meranzin hydrate (MH) may be beneficial in depressive disorders. However, to the best of our knowledg...
PMC12784360
core_pubmed_pmc
Cemiplimab in Japanese patients with advanced non-small cell lung cancer
Cemiplimab in Japanese patients with advanced non-small cell lung cancer Abstract Abstract Background EMPOWER-Lung 1 and EMPOWER-Lung 3 (phase 3 studies) demonstrated survival benefits for cemiplimab with/without chemotherapy in global (non-Japanese) patients with advanced non-small cell lung cancer (aNSCLC). This sing...
PMC6771248
core_pubmed_pmc
Pretargeted radioimmunotherapy and SPECT imaging of peritoneal carcinomatosis using bioorthogonal click chemistry: probe selection and first proof-of-concept
Pretargeted radioimmunotherapy and SPECT imaging of peritoneal carcinomatosis using bioorthogonal click chemistry: probe selection and first proof-of-concept Abstract Rationale : Pretargeted radioimmunotherapy (PRIT) based upon bioorthogonal click chemistry has been investigated for the first time in the context of per...
PMC12497927
core_pubmed_pmc
Pharmacokinetics and safety of eptinezumab in children and adolescents with migraine
Pharmacokinetics and safety of eptinezumab in children and adolescents with migraine Abstract Abstract Objective The primary objective was to characterize the pharmacokinetics (PK) and safety of eptinezumab in children and adolescents with migraine. Background Migraine in children and adolescents is a prevalent and pot...
PMC8872245
core_pubmed_pmc
Successful Treatment of Bacteremia and Ventilator-Associated Pneumonia Caused by KPC/OXA-48-like Klebsiella pneumoniae Co-Producer with a Continuous Infusion of High-Dose Meropenem Plus Fosfomycin Guided by Real-Time Therapeutic Drug Monitoring
Successful Treatment of Bacteremia and Ventilator-Associated Pneumonia Caused by KPC/OXA-48-like Klebsiella pneumoniae Co-Producer with a Continuous Infusion of High-Dose Meropenem Plus Fosfomycin Guided by Real-Time Therapeutic Drug Monitoring Abstract Abstract Bacteremia and ventilator-associated pneumonia due to a p...
PMC9883662
core_pubmed_pmc
Physiologically-based pharmacokinetic modeling to predict drug-drug interactions of dabigatran etexilate and rivaroxaban in the Chinese older adults
Physiologically-based pharmacokinetic modeling to predict drug-drug interactions of dabigatran etexilate and rivaroxaban in the Chinese older adults Abstract Highlights • Exposure of anticoagulants in Chinese older adults is 21–88% greater than in Chinese adults. • Aging has no drastic impact on drug interaction extent...
PMC6499228
core_pubmed_pmc
Dose Characterization of the Investigational Anticancer Drug Tigilanol Tiglate (EBC-46) in the Local Treatment of Canine Mast Cell Tumors
Dose Characterization of the Investigational Anticancer Drug Tigilanol Tiglate (EBC-46) in the Local Treatment of Canine Mast Cell Tumors Abstract Mast cell tumor (MCT) is the most common cutaneous neoplasm in dogs and wide surgical resection is the current first-line treatment. However, recurrence is common and often ...
PMC12510642
core_pubmed_pmc
Population pharmacokinetic-pharmacodynamic analysis of benznidazole monotherapy and combination therapy with fosravuconazole in chronic Chagas disease (BENDITA)
Population pharmacokinetic-pharmacodynamic analysis of benznidazole monotherapy and combination therapy with fosravuconazole in chronic Chagas disease (BENDITA) Abstract Introduction The currently recommended 8-week daily benznidazole regimen for Chagas disease is poorly tolerated. While shorter benznidazole monotherap...
PMC9644353
core_pubmed_pmc
Study protocol for locoregional precision treatment of hepatocellular carcinoma with transarterial chemoembolisation (TACTida), a clinical study: idarubicin dose selection, tissue response and survival
Study protocol for locoregional precision treatment of hepatocellular carcinoma with transarterial chemoembolisation (TACTida), a clinical study: idarubicin dose selection, tissue response and survival Abstract Abstract Introduction Hepatocellular carcinoma (HCC) is a common cause of cancer-related death, often detecte...