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PMC7504675
core_pubmed_pmc
Pharmacogenomics of Antibiotics
Pharmacogenomics of Antibiotics Abstract Although the introduction of antibiotics in medicine has resulted in one of the most successful events and in a major breakthrough to reduce morbidity and mortality caused by infectious disease, response to these agents is not always predictable, leading to differences in their ...
PMC12061181
core_pubmed_pmc
Anti-cancer activity elucidation of geissolosimine as an MDM2-p53 interaction inhibitor: An in-silico study
Anti-cancer activity elucidation of geissolosimine as an MDM2-p53 interaction inhibitor: An in-silico study Abstract Abstract For cancer treatment, Inhibition of murine double minute (MDM2) & p53 interaction is considered an attractive therapeutic approach. In this study, we performed an integrated virtual screening ( ...
PMC10723688
core_pubmed_pmc
Delineating Pixantrone Maleate’s adroit activity against cervical cancer proteins through multitargeted docking-based MM\GBSA, QM-DFT and MD simulation
Delineating Pixantrone Maleate’s adroit activity against cervical cancer proteins through multitargeted docking-based MM\GBSA, QM-DFT and MD simulation Abstract Abstract Cervical cancer poses a substantial worldwide health challenge, especially in low- and middle-income nations, caused by high-risk types of human papil...
PMC9086831
core_pubmed_pmc
Effects of Lisdexamfetamine, a Prodrug of D-Amphetamine, on Locomotion, Spatial Cognitive Processing and Neurochemical Profiles in Rats: A Comparison With Immediate-Release Amphetamine
Effects of Lisdexamfetamine, a Prodrug of D-Amphetamine, on Locomotion, Spatial Cognitive Processing and Neurochemical Profiles in Rats: A Comparison With Immediate-Release Amphetamine Abstract D-amphetamine has been used to enhance cognitive performance over the last few decades. Due to the rapid absorption after admi...
PMC6882433
core_pubmed_pmc
Blood concentrations of small extracellular vesicles are determined by a balance between abundant secretion and rapid clearance
Blood concentrations of small extracellular vesicles are determined by a balance between abundant secretion and rapid clearance Abstract ABSTRACT Small extracellular vesicles (sEVs) are important mediators of cell–cell communication with respect to diverse physiological processes. To further understand their physiologi...
PMC10332652
core_pubmed_pmc
Area-Under-Curve–Guided Versus Trough-Guided Monitoring of Vancomycin and Its Impact on Nephrotoxicity: A Systematic Review and Meta-Analysis
Area-Under-Curve–Guided Versus Trough-Guided Monitoring of Vancomycin and Its Impact on Nephrotoxicity: A Systematic Review and Meta-Analysis Abstract Supplemental Digital Content is Available in the Text. Key Words: vancomycin, therapeutic drug monitoring, area under curve, trough Background: Conventionally, vancomyci...
PMC8580130
core_pubmed_pmc
Galbofloxacin: a xenometal-antibiotic with potent in vitro and in vivo efficacy against S. aureus †
Galbofloxacin: a xenometal-antibiotic with potent in vitro and in vivo efficacy against S. aureus † Abstract Siderophore-antibiotic drug conjugates are considered potent tools to deliver and potentiate the antibacterial activity of antibiotics, but only few have seen preclinical and clinical success. Here, we introduce...
PMC4432109
core_pubmed_pmc
Development and application of an aggregate adherence metric derived from population pharmacokinetics to inform clinical trial enrichment
Development and application of an aggregate adherence metric derived from population pharmacokinetics to inform clinical trial enrichment Abstract Abstract Nonadherence to prescribed medication is a common barrier to effective treatment, and current options to determine adherence are limited. This study describes devel...
PMC7151110
core_pubmed_pmc
On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development
On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development Abstract Abstract A small-scale biphasic dissolution setup and a small-scale dissolution-permeation (D-P) setup were evaluated for their usefulness in simulating the ...
PMC12177163
core_pubmed_pmc
Phase I Study of the Anti-interleukin 33 Fragment Antigen-Binding Region RO7303359 in Geographic Atrophy Secondary to Age-Related Macular Degeneration
Phase I Study of the Anti-interleukin 33 Fragment Antigen-Binding Region RO7303359 in Geographic Atrophy Secondary to Age-Related Macular Degeneration Abstract Abstract Purpose Interleukin (IL) 33 is a potent proinflammatory cytokine and a potential target in age-related macular degeneration (AMD) pathophysiology. This...
PMC5132046
core_pubmed_pmc
Pharmacokinetics and Safety of Defibrotide in Healthy Japanese Subjects
Pharmacokinetics and Safety of Defibrotide in Healthy Japanese Subjects Methods Study Design This study had a randomized, single‐blind, placebo‐controlled study design. The 20 subjects were randomly divided into 2 groups. From each group, 8 subjects received either a 3.0 or 6.25 mg/kg dose of DF, and 2 subjects receive...
PMC5727322
core_pubmed_pmc
A phase I/II pharmacokinetics/pharmacodynamics study of irinotecan combined with S−1 for recurrent/metastatic breast cancer in patients with selected UGT1A1 genotypes (the JBCRG‐M01 study)
A phase I/II pharmacokinetics/pharmacodynamics study of irinotecan combined with S−1 for recurrent/metastatic breast cancer in patients with selected UGT1A1 genotypes (the JBCRG‐M01 study) Abstract Abstract S‐1 and irinotecan combination is attractive for breast cancer refractory to anthracyclines and taxanes. Patients...
PMC5005780
core_pubmed_pmc
Dosing Recommendations of Aripiprazole Depot with Strong Cytochrome P450 3A4 Inhibitors: A Relapse Risk
Dosing Recommendations of Aripiprazole Depot with Strong Cytochrome P450 3A4 Inhibitors: A Relapse Risk Abstract Abstract A 50-year-old male patient with comorbid human immunodeficiency virus developed a relapse of bipolar disorder after a switch from oral aripiprazole 10 mg/day to intramuscular aripiprazole depot 200 ...
PMC7318031
core_pubmed_pmc
Population Pharmacokinetic Analyses for Omadacycline Using Phase 1 and 3 Data
Population Pharmacokinetic Analyses for Omadacycline Using Phase 1 and 3 Data Abstract Omadacycline, a novel aminomethylcycline antibiotic with activity against Gram-positive and -negative organisms, including tetracycline-resistant pathogens, received FDA approval in October 2018 for the treatment of patients with acu...
PMC12592380
core_pubmed_pmc
Exploring Cadaba fruticosa bioactive compounds for oral cancer an in silico and in vitro approach
Exploring Cadaba fruticosa bioactive compounds for oral cancer an in silico and in vitro approach Abstract Abstract This study evaluates the efficacy of phytotherapy in treating oral cancer. This study evaluated the phytocompounds extracted from Cadaba fruticosa for anticancer potential using GC–MS analysis. A total of...
PMC12709667
core_pubmed_pmc
Evaluation of the Pharmacokinetics, Disposition, and Metabolism of Miricorilant, a Novel Glucocorticoid Receptor Modulator for the Treatment of Metabolic Dysfunction‐Associated Steatohepatitis in Nonclinical and Clinical Studies
Evaluation of the Pharmacokinetics, Disposition, and Metabolism of Miricorilant, a Novel Glucocorticoid Receptor Modulator for the Treatment of Metabolic Dysfunction‐Associated Steatohepatitis in Nonclinical and Clinical Studies Abstract Abstract Miricorilant is a novel selective glucocorticoid receptor (GR) modulator ...
PMC7473713
core_pubmed_pmc
Alcohol’s Unique Effects on Cognition in Women: A 2020 (Re)view to Envision Future Research and Treatment
Alcohol’s Unique Effects on Cognition in Women: A 2020 (Re)view to Envision Future Research and Treatment Abstract Alcohol use and misuse is increasing among women. Although the prevalence of drinking remains higher in men than women, the gender gap is narrowing. This narrative review focuses on the cognitive sequelae ...
PMC9486086
core_pubmed_pmc
Development of a UPLC-MS/MS method for the determination of orelabrutinib in rat plasma and its application in pharmacokinetics
Development of a UPLC-MS/MS method for the determination of orelabrutinib in rat plasma and its application in pharmacokinetics Abstract The aim of the present study was to establish an ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the determination of orelabrutinib in rat pla...
PMC5501685
core_pubmed_pmc
LASSIM—A network inference toolbox for genome-wide mechanistic modeling
LASSIM—A network inference toolbox for genome-wide mechanistic modeling Abstract Recent technological advancements have made time-resolved, quantitative, multi-omics data available for many model systems, which could be integrated for systems pharmacokinetic use. Here, we present la rge- s cale si mulation m odeling (L...
PMC7117434
core_pubmed_pmc
The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies
The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies Abstract Highlights • GS-441524 inhibited replication of serotype II FIP virus (FIPV) in CRFK cell cultures at an EC50 of approximately 1 uM and no toxicity at 100 uM. • G...
PMC9545147
core_pubmed_pmc
Impact of Sulfur Fumigation on Ginger: Chemical and Biological Evidence
Impact of Sulfur Fumigation on Ginger: Chemical and Biological Evidence Abstract Abstract We previously found that sulfur fumigation, a commonly used controversial method for the post-harvest handling of ginger, induces the generation of a compound in ginger, which was speculated to be a sulfur-containing derivative of...
PMC7043204
core_pubmed_pmc
Ethnic Differences in Hematologic Toxicity from Imatinib in Patients with Gastrointestinal Stromal Cell Tumor (GIST): Coincidence or a Real Phenomenon
Ethnic Differences in Hematologic Toxicity from Imatinib in Patients with Gastrointestinal Stromal Cell Tumor (GIST): Coincidence or a Real Phenomenon Abstract Objectives: There is a wide variability in the pharmacokinetics, pharmacodynamics and tolerance of anticancer drugs based on ethnicity. GIST is a rare cancer, (...
PMC6713240
core_pubmed_pmc
Pharmacokinetic Properties of Rivaroxaban in Healthy Human Subjects
Pharmacokinetic Properties of Rivaroxaban in Healthy Human Subjects Abstract Abstract Direct oral anticoagulants (DOACs) have predictable pharmacokinetics and pharmacodynamics, limited potential for drug to drug interactions, and can be given at fixed doses without the need for routine coagulation monitoring, which mak...
PMC8690270
core_pubmed_pmc
Safety and Efficacy of Tocilizumab 4 or 8 mg/kg in Hospitalized Patients With Moderate to Severe Coronavirus Disease 2019 Pneumonia: A Randomized Clinical Trial
Safety and Efficacy of Tocilizumab 4 or 8 mg/kg in Hospitalized Patients With Moderate to Severe Coronavirus Disease 2019 Pneumonia: A Randomized Clinical Trial Abstract Abstract Background Tocilizumab, an interleukin 6 receptor (IL-6R) antagonist monoclonal antibody, has shown efficacy in patients with coronavirus dis...
PMC7698073
core_pubmed_pmc
Fungal Enzyme l -Lysine α-Oxidase Affects the Amino Acid Metabolism in the Brain and Decreases the Polyamine Level
Fungal Enzyme l -Lysine α-Oxidase Affects the Amino Acid Metabolism in the Brain and Decreases the Polyamine Level Abstract The fungal glycoprotein l -lysine α-oxidase (LO) catalyzes the oxidative deamination of l -lysine ( l -lys). LO may be internalized in the intestine and shows antitumor, antibacterial, and antivir...
PMC3392829
core_pubmed_pmc
Atacicept in combination with MMF and corticosteroids in lupus nephritis: results of a prematurely terminated trial
Atacicept in combination with MMF and corticosteroids in lupus nephritis: results of a prematurely terminated trial Abstract Introduction Atacicept is a soluble, fully human, recombinant fusion protein that inhibits B cell-stimulating factors APRIL (a proliferation-inducing ligand) and BLyS (B-lymphocyte stimulator). T...
PMC7584801
core_pubmed_pmc
Clinical pharmacology applications in clinical drug development and clinical care: A focus on Saudi Arabia
Clinical pharmacology applications in clinical drug development and clinical care: A focus on Saudi Arabia Abstract Drug development, from preclinical to clinical studies, is a lengthy and complex process. There is an increased interest in the Kingdom of Saudi Arabia (KSA) to promote innovation, research and local cont...
PMC10133543
core_pubmed_pmc
Safety, tolerance, and pharmacokinetics of salvianolic acid B in healthy Chinese volunteers: A randomized, double-blind, placebo-controlled phase 1 clinical trial
Safety, tolerance, and pharmacokinetics of salvianolic acid B in healthy Chinese volunteers: A randomized, double-blind, placebo-controlled phase 1 clinical trial Abstract Background: Salvianolic acid B (Sal B) is one of the main active ingredients of Sa lvia miltiorrhiza Bunge . In China, many traditional Chinese medi...
PMC11272469
core_pubmed_pmc
Comparing the adverse effects of ketamine and esketamine between genders using FAERS data
Comparing the adverse effects of ketamine and esketamine between genders using FAERS data Abstract Background Ketamine was developed as an anesthetic. Esketamine is the isolated S-enantiomer of racemic ketamine. They provide new avenues for the treatment of depression, especially treatment-resistant depression. Conside...
PMC12872673
core_pubmed_pmc
Absorption, Metabolism, Distribution and Excretion (ADME) and Absolute Bioavailability Assessment of Zongertinib in Healthy Male Volunteers
Absorption, Metabolism, Distribution and Excretion (ADME) and Absolute Bioavailability Assessment of Zongertinib in Healthy Male Volunteers Abstract Abstract Background and Objectives Zongertinib is an irreversible tyrosine kinase inhibitor that selectively inhibits human epidermal growth factor receptor 2 (HER2) while...
PMC10092043
core_pubmed_pmc
Pharmacodynamic Biomarkers Evidentiary Considerations for Biosimilar Development and Approval
Pharmacodynamic Biomarkers Evidentiary Considerations for Biosimilar Development and Approval Abstract Abstract A biosimilar is a biological product that is highly similar to and has no clinically meaningful differences from a US Food and Drug Administration (FDA)‐approved reference product. The development and approva...
PMC5953987
core_pubmed_pmc
Guiding dose adjustment of amlodipine after co-administration with ritonavir containing regimens using a physiologically-based pharmacokinetic/pharmacodynamic model
Guiding dose adjustment of amlodipine after co-administration with ritonavir containing regimens using a physiologically-based pharmacokinetic/pharmacodynamic model Abstract Abstract Amlodipine, a commonly prescribed anti-hypertensive drug, shows increased systemic exposure with cytochrome P450 (CYP) 3A inhibitors. Rit...
PMC9290951
core_pubmed_pmc
Population Pharmacokinetic Modeling and Simulations to Evaluate a Potential Dose Regimen of Testosterone Undecanoate in Hypogonadal Males
Population Pharmacokinetic Modeling and Simulations to Evaluate a Potential Dose Regimen of Testosterone Undecanoate in Hypogonadal Males Abstract Abstract Intramuscular testosterone undecanoate is indicated as testosterone replacement in adult males with a deficiency in or absence of endogenous testosterone (hypogonad...
PMC8175963
core_pubmed_pmc
Pharmacodynamic Evaluation of Dosing, Bacterial Kill, and Resistance Suppression for Zoliflodacin Against Neisseria gonorrhoeae in a Dynamic Hollow Fiber Infection Model
Pharmacodynamic Evaluation of Dosing, Bacterial Kill, and Resistance Suppression for Zoliflodacin Against Neisseria gonorrhoeae in a Dynamic Hollow Fiber Infection Model Abstract Antimicrobial resistance in Neisseria gonorrhoeae is threatening the treatment and control of gonorrhea globally, and new treatment options a...
PMC11903094
core_pubmed_pmc
Vitamin D: are all compounds equal?
Vitamin D: are all compounds equal? Abstract ABSTRACT Vitamin D is a pre-hormone essential for maintaining mineral homeostasis and also plays significant roles in bone, cardiovascular and renal health. Vitamin D deficiency is prevalent in the general population, and even more so in chronic kidney disease (CKD) patients...
PMC4452163
core_pubmed_pmc
Phase I study of tivantinib in Japanese patients with advanced hepatocellular carcinoma: Distinctive pharmacokinetic profiles from other solid tumors
Phase I study of tivantinib in Japanese patients with advanced hepatocellular carcinoma: Distinctive pharmacokinetic profiles from other solid tumors Abstract A c-Met inhibitor tivantinib is a candidate anticancer agent for patients with hepatocellular carcinoma (HCC), and CYP2C19 is the key metabolic enzyme for tivant...
PMC3917320
core_pubmed_pmc
Basic Concepts in Population Modeling, Simulation, and Model-Based Drug Development: Part 3—Introduction to Pharmacodynamic Modeling Methods
Basic Concepts in Population Modeling, Simulation, and Model-Based Drug Development: Part 3—Introduction to Pharmacodynamic Modeling Methods Abstract Abstract Population pharmacodynamic (PD) models describe the time course of drug effects, relating exposure to response, and providing a more robust understanding of drug...
PMC12030383
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Bioequivalence of Test Insulin Glargine Versus Reference Preparation (Lantus ® ) in Healthy Male Volunteers—By Euglycemic Clamp Technique
Pharmacokinetics, Pharmacodynamics, and Bioequivalence of Test Insulin Glargine Versus Reference Preparation (Lantus ® ) in Healthy Male Volunteers—By Euglycemic Clamp Technique Abstract The aim of this study was to evaluate the pharmacokinetics (PK), pharmacodynamics (PD), and safety of two insulin glargine preparatio...
PMC8932690
core_pubmed_pmc
A phase I, first‐in‐human, randomized dose‐escalation study of anti‐activated factor XII monoclonal antibody garadacimab
A phase I, first‐in‐human, randomized dose‐escalation study of anti‐activated factor XII monoclonal antibody garadacimab Abstract Abstract Factor XII (FXII) is the principal initiator of the plasma contact system and has proinflammatory and prothrombotic activities. This single‐center, first‐in‐human phase I study aime...
PMC8235938
core_pubmed_pmc
Progress in Redirecting Antiparasitic Drugs for Cancer Treatment
Progress in Redirecting Antiparasitic Drugs for Cancer Treatment Abstract Abstract Drug repurposing is a feasible strategy in developing novel medications. Regarding the cancer field, scientists are continuously making efforts to redirect conventional drugs into cancer treatment. This approach aims at exploring new app...
PMC5278894
core_pubmed_pmc
Virological efficacy of 24-week fozivudine-based regimen in ART-naive patients from Tanzania and Côte d’Ivoire
Virological efficacy of 24-week fozivudine-based regimen in ART-naive patients from Tanzania and Côte d’Ivoire Abstract Supplemental Digital Content is available in the text Objective: Use of zidovudine (ZDV) in antiretroviral therapy is limited by toxicity and twice daily (b.i.d.) dosing. Fozivudine (FZD) is a ZDV pro...
PMC5514236
core_pubmed_pmc
The effect of using a robust optimality criterion in model based adaptive optimization
The effect of using a robust optimality criterion in model based adaptive optimization Abstract Abstract Optimizing designs using robust (global) optimality criteria has been shown to be a more flexible approach compared to using local optimality criteria. Additionally, model based adaptive optimal design (MBAOD) may b...
PMC4592532
core_pubmed_pmc
Connecting the Dots: Linking Osteocyte Activity and Therapeutic Modulation of Sclerostin by Extending a Multiscale Systems Model
Connecting the Dots: Linking Osteocyte Activity and Therapeutic Modulation of Sclerostin by Extending a Multiscale Systems Model Abstract The goal of this work was to extend a mathematical, multiscale systems model of bone function, remodeling, and health in order to explore hypotheses related to therapeutic modulation...
PMC3928458
core_pubmed_pmc
Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation Abstract The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-solu...
PMC12823319
core_pubmed_pmc
Pharmacokinetic Model Selection for Personalized Infliximab Dosing in IBD
Pharmacokinetic Model Selection for Personalized Infliximab Dosing in IBD Abstract ABSTRACT Infliximab, a monoclonal antibody used for immune‐mediated diseases, shows high interpatient pharmacokinetic variability. Prolonged exposure increases the risk of adverse effects and costs, making dose personalization essential ...
PMC10863324
core_pubmed_pmc
Whole-body galactose oxidation as a robust functional assay to assess the efficacy of gene-based therapies in a mouse model of Galactosemia
Whole-body galactose oxidation as a robust functional assay to assess the efficacy of gene-based therapies in a mouse model of Galactosemia Abstract Despite the implementation of lifesaving newborn screening programs and a galactose-restricted diet, many patients with classic galactosemia develop long-term debilitating...
PMC10623319
core_pubmed_pmc
Pharmacokinetics of immunosuppressive agents during hemoperfusion in a sheep model
Pharmacokinetics of immunosuppressive agents during hemoperfusion in a sheep model Abstract Introduction Hemoadsorption shows promising signals in organ preservation and post lung transplantation. However, its potential impact on the pharmacokinetics of immunosuppressant drugs (ID) is still unknown. Methods In this int...
PMC11367382
core_pubmed_pmc
Sabatolimab in combination with spartalizumab in patients with non-small cell lung cancer or melanoma who received prior treatment with anti-PD-1/PD-L1 therapy: a phase 2 multicentre study
Sabatolimab in combination with spartalizumab in patients with non-small cell lung cancer or melanoma who received prior treatment with anti-PD-1/PD-L1 therapy: a phase 2 multicentre study Abstract Abstract Objective This study evaluates the safety/efficacy of sabatolimab plus spartalizumab in patients with melanoma or...
PMC9306898
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of Etavopivat (FT‐4202), an Allosteric Activator of Pyruvate Kinase‐R, in Healthy Adults: A Randomized, Placebo‐Controlled, Double‐Blind, First‐in‐Human Phase 1 Trial
Safety, Pharmacokinetics, and Pharmacodynamics of Etavopivat (FT‐4202), an Allosteric Activator of Pyruvate Kinase‐R, in Healthy Adults: A Randomized, Placebo‐Controlled, Double‐Blind, First‐in‐Human Phase 1 Trial Abstract Abstract Etavopivat (FT‐4202) is an orally administered, small‐molecule allosteric activator of e...
PMC8366046
core_pubmed_pmc
Scoping insight on antiviral drugs against COVID-19
Scoping insight on antiviral drugs against COVID-19 Abstract Abstract Background COVID-19 is an ongoing viral pandemic produced by SARS-CoV-2. In light of in vitro efficacy, several medications were repurposed for its management. During clinical use, many of these medications produced inconsistent results or had varyin...
PMC9096090
core_pubmed_pmc
Can Old Animals Reveal New Targets? The Aging and Degenerating Brain as a New Precision Medicine Opportunity for Epilepsy
Can Old Animals Reveal New Targets? The Aging and Degenerating Brain as a New Precision Medicine Opportunity for Epilepsy Abstract Older people represent the fastest growing group with epilepsy diagnosis. For example, cerebrovascular disease may underlie roughly 30–50% of epilepsy in older adults and seizures are also ...
PMC11123338
core_pubmed_pmc
The Effects of Dobutamine in Septic Shock: An Updated Narrative Review of Clinical and Experimental Studies
The Effects of Dobutamine in Septic Shock: An Updated Narrative Review of Clinical and Experimental Studies Abstract Abstract The key objective in the hemodynamic treatment of septic shock is the optimization of tissue perfusion and oxygenation. This is usually achieved by the utilization of fluids, vasopressors, and i...
PMC10649008
core_pubmed_pmc
Pharmacokinetics and safety of a single dose of telavancin in pediatric subjects 2–17 years of age
Pharmacokinetics and safety of a single dose of telavancin in pediatric subjects 2–17 years of age Abstract ABSTRACT Antimicrobial resistance increases infection morbidity in both adults and children, necessitating the development of new therapeutic options. Telavancin, an antibiotic approved in the United States for c...
PMC5827532
core_pubmed_pmc
Triphenylphosphonium Moiety Modulates Proteolytic Stability and Potentiates Neuroprotective Activity of Antioxidant Tetrapeptides in Vitro
Triphenylphosphonium Moiety Modulates Proteolytic Stability and Potentiates Neuroprotective Activity of Antioxidant Tetrapeptides in Vitro Abstract Although delocalized lipophilic cations have been identified as effective cellular and mitochondrial carriers for a range of natural and synthetic drug molecules, little is...
PMC9504753
core_pubmed_pmc
Exposure–Response Analysis of Osimertinib in Patients with Advanced Non-Small-Cell Lung Cancer
Exposure–Response Analysis of Osimertinib in Patients with Advanced Non-Small-Cell Lung Cancer Abstract Abstract High interindividual variability (IIV) of the clinical response to epidermal growth factor receptor (EGFR) inhibitors such as osimertinib in non-small-cell lung cancer (NSCLC) might be related to the IIV in ...
PMC6528723
core_pubmed_pmc
Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids
Novel nanomicelle formulation to enhance bioavailability and stability of curcuminoids Abstract Abstract Objective(s): Curcuminoids, comprising curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), are bioactive phytochemicals with numerous pharmacological effects. Oral biological availability of curcumino...
PMC7689240
core_pubmed_pmc
Pan‐cancer population pharmacokinetics and exposure‐safety and ‐efficacy analyses of atezolizumab in patients with high tumor mutational burden
Pan‐cancer population pharmacokinetics and exposure‐safety and ‐efficacy analyses of atezolizumab in patients with high tumor mutational burden Abstract Abstract We retrospectively investigated the pharmacokinetics and exposure‐efficacy/safety relationships of single‐agent atezolizumab based on tissue tumor mutational ...
PMC9210879
core_pubmed_pmc
Advances in the clinical application of oxycodone in the perioperative period
Advances in the clinical application of oxycodone in the perioperative period Abstract Abstract To review the research progress of pure opioid receptor agonist oxycodone. The research progress of oxycodone in terms of pharmacokinetics, pharmacodynamics, adverse reactions, clinical application, combined medication and n...
PMC8302244
core_pubmed_pmc
Population pharmacokinetic modeling of molibresib and its active metabolites in patients with solid tumors: A semimechanistic autoinduction model
Population pharmacokinetic modeling of molibresib and its active metabolites in patients with solid tumors: A semimechanistic autoinduction model Abstract Abstract Molibresib (GSK525762) is an investigational, orally bioavailable, small‐molecule bromodomain and extraterminal (BET) protein inhibitor for the treatment of...
PMC3004635
core_pubmed_pmc
Opioid chronopharmacology: influence of timing of infusion on fentanyl’s analgesic efficacy in healthy human volunteers
Opioid chronopharmacology: influence of timing of infusion on fentanyl’s analgesic efficacy in healthy human volunteers Abstract Abstract Chronopharmacology studies the effect of the timing of drug administration on drug effect. Here, we measured the influence of 4 timing moments on fentanyl-induced antinociception in ...
PMC5788590
core_pubmed_pmc
The pharmacokinetic-pharmacodynamic modeling and cut-off values of tildipirosin against Haemophilus parasuis
The pharmacokinetic-pharmacodynamic modeling and cut-off values of tildipirosin against Haemophilus parasuis Abstract Abstract The goal of this study was to establish the epidemiological, pharmacodynamic cut-off values, optimal dose regimens for tildipirosin against Haemophilus parasuis . The minimum inhibitory concent...
PMC4778235
core_pubmed_pmc
Development of Validated Bioanalytical HPLC-UV Method for Simultaneous Estimation of Amlodipine and Atorvastatin in Rat Plasma
Development of Validated Bioanalytical HPLC-UV Method for Simultaneous Estimation of Amlodipine and Atorvastatin in Rat Plasma Abstract A simple, economical and robust analytical high-performance liquid chromatography-ultraviolet method was developed and validated for simultaneous chromatographic elution of two cardiov...
PMC7360824
core_pubmed_pmc
Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects
Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects Abstract Purpose To evaluate the tolerability, safety, pharmacokinetics and drug interaction of cefotaxime sodium–tazobactam sodi...
PMC12439015
core_pubmed_pmc
Relationship between Dose, Factor IX Activity Levels and Bleeding Probability for rIX‐FP Prophylaxis in Hemophilia B: A Repeated Time‐to‐Event Analysis
Relationship between Dose, Factor IX Activity Levels and Bleeding Probability for rIX‐FP Prophylaxis in Hemophilia B: A Repeated Time‐to‐Event Analysis Abstract Abstract In hemophilia B, pharmacokinetic (PK)‐guided dosing of extended half‐life factor IX (EHL‐FIX) concentrates can secure targeted FIX exposure. Target FI...
PMC4470194
core_pubmed_pmc
Targeted Therapy of FLT3 in Treatment of AML—Current Status and Future Directions
Targeted Therapy of FLT3 in Treatment of AML—Current Status and Future Directions Abstract Internal tandem duplications (ITDs) of the gene encoding the Fms-Like Tyrosine kinase-3 (FLT3) receptor are present in approximately 25% of patients with acute myeloid leukemia (AML). The mutation is associated with poor prognosi...
PMC12511377
core_pubmed_pmc
Molecular docking and pharmacokinetics of benzimidazole-based FtsZ inhibitors for tuberculosis
Molecular docking and pharmacokinetics of benzimidazole-based FtsZ inhibitors for tuberculosis Abstract Abstract Benzimidazole derivatives are privileged heterocyclic scaffolds with broad-spectrum pharmacological activities, notably antitubercular and antibacterial. In particular, 1,2-disubstituted benzimidazoles have ...
PMC10938783
core_pubmed_pmc
A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation
A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation Abstract Background Phosphoinositide 3-kinases (PI3Ks) are critical regulators of diverse cellular functions and have emerged as promising targets in cancer therapy. Despite significant progress, ex...
PMC8580050
core_pubmed_pmc
Improvement of the antimicrobial potency, pharmacokinetic and pharmacodynamic properties of albicidin by incorporation of nitrogen atoms †
Improvement of the antimicrobial potency, pharmacokinetic and pharmacodynamic properties of albicidin by incorporation of nitrogen atoms † Abstract Abstract The worrisome development and spread of multidrug-resistant bacteria demands new antibacterial agents with strong bioactivities particularly against Gram-negative ...
PMC8861431
core_pubmed_pmc
Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling
Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling Abstract Abstract Hypoxia-activated prodrugs are bioactivated in oxygen-deficient tumour regions and represent a novel strategy to exploit this pharmacological sanctuary for therapeutic gain. The appro...
PMC12238781
core_pubmed_pmc
Optimization of Preemptive Therapy for Cytomegalovirus Infections With Valganciclovir Based on Therapeutic Drug Monitoring: Protocol for a Phase II, Single-Center, Single-Arm Trial
Optimization of Preemptive Therapy for Cytomegalovirus Infections With Valganciclovir Based on Therapeutic Drug Monitoring: Protocol for a Phase II, Single-Center, Single-Arm Trial Abstract Background Valganciclovir (VGCV) is the first-line drug for preemptive therapy of cytomegalovirus (CMV) infections. However, even ...
PMC3140810
core_pubmed_pmc
Evaluation of CYP450 inhibitory effects and steady-state pharmacokinetics of genistein in combination with cholecalciferol and citrated zinc bisglycinate in postmenopausal women
Evaluation of CYP450 inhibitory effects and steady-state pharmacokinetics of genistein in combination with cholecalciferol and citrated zinc bisglycinate in postmenopausal women Abstract Abstract Background The combination of genistein 27 mg, cholecalciferol 200 IU, citrated zinc bisglycinate (4 mg elemental zinc) 20 m...
PMC8072262
core_pubmed_pmc
Simultaneous Optimization of Oral and Transdermal Nanovesicles for Bioavailability Enhancement of Ivabradine Hydrochloride
Simultaneous Optimization of Oral and Transdermal Nanovesicles for Bioavailability Enhancement of Ivabradine Hydrochloride Abstract Abstract Purpose Ivabradine hydrochloride is selective pacemaker current (I f ) ion channel inhibitor used in case of chronic heart failure (CHF) with superior efficacy and lower side effe...
PMC8537691
core_pubmed_pmc
Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP
Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP Abstract Abstract Folium Sennae (FS), a popular laxative (Senna), contains polyphenolic anthranoids, whose conjugation metabolites are probable modulators of multidrug resistance-associated proteins (MRPs) and breast cancer...
PMC7577234
core_pubmed_pmc
Functional humanization of immunoglobulin heavy constant gamma 1 Fc domain human FCGRT transgenic mice
Functional humanization of immunoglobulin heavy constant gamma 1 Fc domain human FCGRT transgenic mice Abstract ABSTRACT A major asset of many monoclonal antibody (mAb)-based biologics is their persistence in circulation. The MHC class I family Fc receptor, FCGRT, is primarily responsible for this extended pharmacokine...
PMC11592880
core_pubmed_pmc
Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors Abstract Tamibarotene is a synthetic retinoid that inhibits tumor cell proliferation and promotes differentiation. We previously reported on the safety and tolerability of tamibarotene in patients...
PMC12742169
core_pubmed_pmc
MOdel-informed precision dosing (MIPD) of ustekinumab and VEdolizumab in inflammatory bowel disease: protocol for an Independent randomised, controlled, multicentre Trial (MOVE-IT)
MOdel-informed precision dosing (MIPD) of ustekinumab and VEdolizumab in inflammatory bowel disease: protocol for an Independent randomised, controlled, multicentre Trial (MOVE-IT) Abstract Abstract Introduction Biologic therapies, such as vedolizumab (VDZ) and ustekinumab (UST), offer effective treatment options for i...
PMC7589779
core_pubmed_pmc
Toward Drug-Like Multispecific Antibodies by Design
Toward Drug-Like Multispecific Antibodies by Design Abstract Abstract The success of antibody therapeutics is strongly influenced by their multifunctional nature that couples antigen recognition mediated by their variable regions with effector functions and half-life extension mediated by a subset of their constant reg...
PMC2861178
core_pubmed_pmc
Basic PK/PD principles of drug effects in circular/proliferative systems for disease modelling
Basic PK/PD principles of drug effects in circular/proliferative systems for disease modelling Abstract Abstract Disease progression modelling can provide information about the time course and outcome of pharmacological intervention on the disease. The basic PK/PD principles of proliferative and circular systems within...
PMC12597959
core_pubmed_pmc
Gamified interventions to educate healthcare professionals on the rational use of antimicrobials
Gamified interventions to educate healthcare professionals on the rational use of antimicrobials Abstract Abstract Background Antimicrobial resistance [AMR] is a global health problem. It is important to train health care professionals on the rational use of antimicrobials to curb AMR. Methods This prospective interven...
PMC11359531
core_pubmed_pmc
Establishment of Dissolution Test Method for Multi-Components in Traditional Chinese Medicine Preparations Based on In Vitro–In Vivo Correlation
Establishment of Dissolution Test Method for Multi-Components in Traditional Chinese Medicine Preparations Based on In Vitro–In Vivo Correlation Abstract Abstract In this study, a multi-component integrated dissolution evaluation system of Yuanhu Zhitong tablets (YZTs) was established based on in vitro and in vivo corr...
PMC9474278
core_pubmed_pmc
Pharmacokinetics of the most commonly used antihypertensive drugs throughout pregnancy methyldopa, labetalol, and nifedipine: a systematic review
Pharmacokinetics of the most commonly used antihypertensive drugs throughout pregnancy methyldopa, labetalol, and nifedipine: a systematic review Abstract Purpose Antihypertensive drugs are among the most prescribed drugs during pregnancy. Methyldopa, labetalol, and nifedipine have been perceived safe to use during pre...
PMC11271312
core_pubmed_pmc
Enhanced disulphide bond stability contributes to the once-weekly profile of insulin icodec
Enhanced disulphide bond stability contributes to the once-weekly profile of insulin icodec Abstract Insulin icodec is a once-weekly insulin analogue that has a long half-life of approximately 7 days, making it suitable for once weekly dosing. The Insulin icodec molecule was developed based on the hypothesis that lower...
PMC11021729
core_pubmed_pmc
Association of exposure to multiple perfluoroalkyl and polyfluoroalkyl substances and glucose metabolism in National Health and Nutrition Examination Survey 2017–2018
Association of exposure to multiple perfluoroalkyl and polyfluoroalkyl substances and glucose metabolism in National Health and Nutrition Examination Survey 2017–2018 Abstract Abstract Objective To investigate the relationships between perfluoroalkyl and polyfluoroalkyl substances (PFASs) exposure and glucose metabolis...
PMC7485951
core_pubmed_pmc
Pharmacodynamic Effects of Topical Omiganan in Patients With Mild to Moderate Atopic Dermatitis in a Randomized, Placebo‐Controlled, Phase II Trial
Pharmacodynamic Effects of Topical Omiganan in Patients With Mild to Moderate Atopic Dermatitis in a Randomized, Placebo‐Controlled, Phase II Trial Abstract Omiganan is an indolicidin analog with antimicrobial properties that could be beneficial for patients with atopic dermatitis. In this randomized, double‐blind, pla...
PMC5992319
core_pubmed_pmc
Reduction of glycemic variability with Degludec insulin in patients with unstable diabetes
Reduction of glycemic variability with Degludec insulin in patients with unstable diabetes Abstract Summary Introduction Degludec (IDeg) is an ultralong-acting insulin, with stable pharmacodynamic profile which leads to lower fluctuations in glucose levels. The effect of IDeg has not been specifically assessed in patie...
PMC8819907
core_pubmed_pmc
Phase I pharmacokinetic study of single agent trametinib in patients with advanced cancer and hepatic dysfunction
Phase I pharmacokinetic study of single agent trametinib in patients with advanced cancer and hepatic dysfunction Abstract Abstract Background Trametinib is an oral MEK 1/2 inhibitor, with a single agent recommended phase 2 dose (RP2D) of 2 mg daily (QD). This study was designed to evaluate RP2D, maximum tolerated dose...
PMC8599380
core_pubmed_pmc
Population Pharmacokinetic Analysis from First-in-Human Data for HDAC Inhibitor, REC-2282 (AR-42), in Patients with Solid Tumors and Hematologic Malignancies: A Case Study for Evaluating Flat vs. Body Size Normalized Dosing
Population Pharmacokinetic Analysis from First-in-Human Data for HDAC Inhibitor, REC-2282 (AR-42), in Patients with Solid Tumors and Hematologic Malignancies: A Case Study for Evaluating Flat vs. Body Size Normalized Dosing Abstract Background and Objectives REC-2282 is a novel histone deacetylase inhibitor that has sh...
PMC7064329
core_pubmed_pmc
Population pharmacokinetic and exposure‐response analysis of eptinezumab in the treatment of episodic and chronic migraine
Population pharmacokinetic and exposure‐response analysis of eptinezumab in the treatment of episodic and chronic migraine Abstract Abstract Eptinezumab is a humanized mAb that targets calcitonin gene‐related peptide and is under regulatory review for the prevention of episodic and chronic migraine (EM, CM). It is impo...
PMC12665028
core_pubmed_pmc
Randomized, phase I studies to evaluate the safety, tolerability, and pharmacokinetics of an inhaled, TMEM16A potentiator, GDC-6988, in healthy subjects
Randomized, phase I studies to evaluate the safety, tolerability, and pharmacokinetics of an inhaled, TMEM16A potentiator, GDC-6988, in healthy subjects Abstract Abstract Background: Respiratory diseases such as cystic fibrosis (CF), chronic obstructive pulmonary disease, and non-CF bronchiectasis are significant globa...
PMC6785660
core_pubmed_pmc
Quantitative systems toxicology (QST) reproduces species differences in PF‐04895162 liver safety due to combined mitochondrial and bile acid toxicity
Quantitative systems toxicology (QST) reproduces species differences in PF‐04895162 liver safety due to combined mitochondrial and bile acid toxicity Abstract Abstract Many compounds that appear promising in preclinical species, fail in human clinical trials due to safety concerns. The FDA has strongly encouraged the a...
PMC12110325
core_pubmed_pmc
Exploring Conscious Sedation in Pediatric Oral Surgery: A Non-Randomized Clinical Trial on Safety and Efficacy
Exploring Conscious Sedation in Pediatric Oral Surgery: A Non-Randomized Clinical Trial on Safety and Efficacy Abstract Abstract Background: Conscious sedation is a well-established technique used in pediatric dentistry that reduces perioperative stress and pain while maintaining verbal contact with the patient. It is ...
PMC6343132
core_pubmed_pmc
Effect of Cilostazol on the Pharmacokinetics of Simvastatin in Healthy Subjects
Effect of Cilostazol on the Pharmacokinetics of Simvastatin in Healthy Subjects Abstract Abstract Purpose We evaluated potential drug-drug interactions between cilostazol and simvastatin, both CYP3A substrates, in healthy subjects. Methods An open-label, two-period, fixed-sequence clinical study was conducted. Seventee...
PMC10398387
core_pubmed_pmc
UPLC-MS/MS method for Icariin and metabolites in whole blood of C57 mice: development, validation, and pharmacokinetics study
UPLC-MS/MS method for Icariin and metabolites in whole blood of C57 mice: development, validation, and pharmacokinetics study Abstract Icariin, a Chinese medicinal herb with significant effects on Alzheimer’s disease, lacks pharmacokinetic data in mice. To address this, a UPLC-MS/MS method was developed and validated f...
PMC5915681
core_pubmed_pmc
Phase I/II evaluation of RV1001, a novel PI3Kδ inhibitor, in spontaneous canine lymphoma
Phase I/II evaluation of RV1001, a novel PI3Kδ inhibitor, in spontaneous canine lymphoma Abstract Background RV1001 is a novel, potent, and selective PI3Kδ inhibitor. The purpose of this study was to evaluate the safety and efficacy of RV1001 in canine Non-Hodgkin lymphoma (NHL). Methods and results Inhibition of endog...
PMC6359546
core_pubmed_pmc
Simultaneous Quantitation of a Novel α 1 /β 1 -Blocker TJ0711 and Its Two Metabolites in Dog Plasma Using LC-MS/MS and Its Application to a Pharmacokinetic Study after Intravenous Infusion
Simultaneous Quantitation of a Novel α 1 /β 1 -Blocker TJ0711 and Its Two Metabolites in Dog Plasma Using LC-MS/MS and Its Application to a Pharmacokinetic Study after Intravenous Infusion Abstract Abstract TJ0711∙HCl, which is a novel α 1 /β 1 adrenoceptor blocking agent with a ratio of 1:1 for α 1 /β 1 , is designed ...
PMC7038779
core_pubmed_pmc
Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study
Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study Abstract Introduction Solid lipid nanoparticles (SLNs) are considered a promising system in enhancing the oral bioavailability of poorly water-soluble drugs; owing to their intrins...
PMC11393876
core_pubmed_pmc
A Novel Monoclonal Antibody against PD-1 for the Treatment of Viral Oncogene-Induced Tumors or Other Cancer
A Novel Monoclonal Antibody against PD-1 for the Treatment of Viral Oncogene-Induced Tumors or Other Cancer Abstract Simple Summary Viral infection poses cancer risk and the PD-1/PD-L1 immune check point plays a critical role in this process. Despite the success of the existing anti-PD-1 and PD-L1 antibodies, significa...
PMC5649209
core_pubmed_pmc
Targeting Mediators of Smoking Persistence with Intranasal Insulin
Targeting Mediators of Smoking Persistence with Intranasal Insulin Abstract Abstract Rapid-acting, non-irritating nasal treatment options for smoking cessation pharmacotherapy are lacking. The halt in development is due, in part, to difficulty in delivering compounds across the blood brain barrier. Recently, in both hu...
PMC10778029
core_pubmed_pmc
Fungal Diseases in Elasmobranchs and Their Possible Treatment with a Special Mention to Azole Antifungal Agents
Fungal Diseases in Elasmobranchs and Their Possible Treatment with a Special Mention to Azole Antifungal Agents Abstract Abstract Simple Summary Fungal diseases, despite their low incidence in fish, appear to be lethal in many teleost and elasmobranch species. There are many fungi involved, including Paecilomyces spp.,...
PMC11284822
core_pubmed_pmc
TG6050, an oncolytic vaccinia virus encoding interleukin-12 and anti-CTLA-4 antibody, favors tumor regression via profound immune remodeling of the tumor microenvironment
TG6050, an oncolytic vaccinia virus encoding interleukin-12 and anti-CTLA-4 antibody, favors tumor regression via profound immune remodeling of the tumor microenvironment Abstract Abstract Background TG6050 was designed as an improved oncolytic vector, combining the intrinsic properties of vaccinia virus to selectively...