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PMC7468728 | core_pubmed_pmc | Natural Sources, Pharmacokinetics, Biological Activities and Health Benefits of Hydroxycinnamic Acids and Their Metabolites | Natural Sources, Pharmacokinetics, Biological Activities and Health Benefits of Hydroxycinnamic Acids and Their Metabolites Abstract Hydroxycinnamic acids (HCAs) are important natural phenolic compounds present in high concentrations in fruits, vegetables, cereals, coffee, tea and wine. Many health beneficial effects h... |
PMC5132082 | core_pubmed_pmc | Impact of Renal Impairment on the Pharmacokinetics of Apremilast and Metabolite M12 | Impact of Renal Impairment on the Pharmacokinetics of Apremilast and Metabolite M12 Abstract Abstract The pharmacokinetics of apremilast and its major metabolite M12 were evaluated in subjects with varying degrees of renal impairment. Men and women with renal impairment (estimated glomerular filtration rate, 60‒89 mL/m... |
PMC9425464 | core_pubmed_pmc | Antifungal pharmacodynamics: Latin America's perspective | Antifungal pharmacodynamics: Latin America's perspective Abstract Abstract The current increment of invasive fungal infections and the availability of new broad-spectrum antifungal agents has increased the use of these agents by non-expert practitioners, without an impact on mortality. To improve efficacy while minimiz... |
PMC7849011 | core_pubmed_pmc | Defining the Antimalarial Activity of Cipargamin in Healthy Volunteers Experimentally Infected with Blood-Stage Plasmodium falciparum | Defining the Antimalarial Activity of Cipargamin in Healthy Volunteers Experimentally Infected with Blood-Stage Plasmodium falciparum Abstract The spiroindolone cipargamin, a new antimalarial compound that inhibits Plasmodium ATP4, is currently in clinical development. This study aimed to characterize the antimalarial ... |
PMC11533097 | core_pubmed_pmc | Simulating realistic patient profiles from pharmacokinetic models by a machine learning postprocessing correction of residual variability | Simulating realistic patient profiles from pharmacokinetic models by a machine learning postprocessing correction of residual variability Abstract Abstract We address the problem of model misspecification in population pharmacokinetics (PopPK), by modeling residual unexplained variability (RUV) by machine learning (ML)... |
PMC9620261 | core_pubmed_pmc | Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of ENO1 -Deleted Cancers | Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of ENO1 -Deleted Cancers Abstract Abstract Cancers harboring homozygous deletion of the glycolytic enzyme enolase 1 ( ENO1 ) are selectively vulnerable to inhibition of the paralogous isoform, enolase 2 (ENO2). A previous work d... |
PMC11852066 | core_pubmed_pmc | Bridging the Gap: A Systematic Review with Expert Opinion on the Use of Dalbavancin for In-Label and Off-Label Indications in Pediatric Patients | Bridging the Gap: A Systematic Review with Expert Opinion on the Use of Dalbavancin for In-Label and Off-Label Indications in Pediatric Patients Abstract Abstract Objectives: The aim of this work was to perform a systematic review assessing the pharmacokinetic/pharmacodynamic (PK/PD) properties of dalbavancin and the c... |
PMC10789575 | core_pubmed_pmc | Effect of High-Fat Meal on the Pharmacokinetics and Safety of Valsartan/Amlodipine Fixed Dose Combination Tablets in Healthy Subjects | Effect of High-Fat Meal on the Pharmacokinetics and Safety of Valsartan/Amlodipine Fixed Dose Combination Tablets in Healthy Subjects Abstract Background The objective of this study was to evaluate the effect of a high-fat meal on the pharmacokinetics and safety of 80/5 mg valsartan/amlodipine tablets in healthy subjec... |
PMC12001258 | core_pubmed_pmc | Modeling and Simulation of Acetaminophen Pharmacokinetics and Hepatic Biomarkers After Overdoses of Extended‐Release and Immediate‐Release Formulations in Healthy Adults Using the Quantitative Systems Toxicology Software Platform DILIsym | Modeling and Simulation of Acetaminophen Pharmacokinetics and Hepatic Biomarkers After Overdoses of Extended‐Release and Immediate‐Release Formulations in Healthy Adults Using the Quantitative Systems Toxicology Software Platform DILIsym Abstract ABSTRACT Acetaminophen (APAP) has been formulated as immediate‐, modified... |
PMC12169384 | core_pubmed_pmc | Pharmacodynamic interactions between seletracetam and antiseizure comedications in the human photosensitivity model | Pharmacodynamic interactions between seletracetam and antiseizure comedications in the human photosensitivity model Abstract Abstract We recently reported that seletracetam (SEL), a highly potent derivative of levetiracetam (LEV), reduces or abolishes the photoparoxysmal electroencephalographic response (PPR) to interm... |
PMC8085964 | core_pubmed_pmc | Clinically relevant enantiomer specific R‐ and S‐praziquantel pharmacokinetic drug‐drug interactions with efavirenz and ritonavir | Clinically relevant enantiomer specific R‐ and S‐praziquantel pharmacokinetic drug‐drug interactions with efavirenz and ritonavir Abstract Abstract We conducted a clinical study to determine the effect of efavirenz and ritonavir on the pharmacokinetics of R‐ and S‐PZQ in healthy male participants. This was toward evalu... |
PMC10112269 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Target Attainment Analyses Evaluating Omadacycline Dosing Regimens for the Treatment of Patients with Community-Acquired Bacterial Pneumonia Arising from Streptococcus pneumoniae and Haemophilus influenzae | Pharmacokinetic-Pharmacodynamic Target Attainment Analyses Evaluating Omadacycline Dosing Regimens for the Treatment of Patients with Community-Acquired Bacterial Pneumonia Arising from Streptococcus pneumoniae and Haemophilus influenzae Abstract ABSTRACT Omadacycline, a novel aminomethylcycline with in vitro activity ... |
PMC11222283 | core_pubmed_pmc | Clinical Pharmacokinetic and Pharmacodynamic Profile of Vericiguat | Clinical Pharmacokinetic and Pharmacodynamic Profile of Vericiguat Abstract Abstract Vericiguat is an oral soluble guanylate cyclase stimulator and enhances the cyclic guanosine monophosphate pathway independently of nitric oxide as well as synergistically in normal- and low-nitric oxide conditions. This review describ... |
PMC6155825 | core_pubmed_pmc | Preparative Scale Resolution of Enantiomers Enables Accelerated Drug Discovery and Development | Preparative Scale Resolution of Enantiomers Enables Accelerated Drug Discovery and Development Abstract Abstract The provision of pure enantiomers is of increasing importance not only for the pharmaceutical industry but also for agro-chemistry and biotechnology. In drug discovery and development, the enantiomers of a c... |
PMC10006169 | core_pubmed_pmc | A phase I trial of LXS196, a protein kinase C (PKC) inhibitor, for metastatic uveal melanoma | A phase I trial of LXS196, a protein kinase C (PKC) inhibitor, for metastatic uveal melanoma Abstract Background Up to 50% of patients with uveal melanoma develop metastases (MUM) with a poor prognosis and median overall survival of approximately 1 year. Methods This phase I study evaluated the safety, tolerability, ph... |
PMC10770825 | core_pubmed_pmc | Pharmacokinetics and bioavailability of a new long-acting insulin analog in healthy Chinese volunteers: an open, randomized, single-dose, two-period and two-sequence cross-over study | Pharmacokinetics and bioavailability of a new long-acting insulin analog in healthy Chinese volunteers: an open, randomized, single-dose, two-period and two-sequence cross-over study Abstract Abstract Objectives: INS068 is a novel, soluble, and long-acting insulin analog. In this study, we evaluated the pharmacokinetic... |
PMC12119865 | core_pubmed_pmc | Structure-based design of potent and selective inhibitors of the HECT ligase NEDD4 | Structure-based design of potent and selective inhibitors of the HECT ligase NEDD4 Abstract Among the human E3 ubiquitin ligases, NEDD4 (Neural precursor cell expressed developmentally down-regulated 4) plays a critical role in development and cancer, making it a compelling therapeutic target. However, no specific NEDD... |
PMC9276400 | core_pubmed_pmc | Extended-release tofacitinib for refractory Behçet disease | Extended-release tofacitinib for refractory Behçet disease Abstract Abstract Rationale: Although single-cytokine inhibitors can be considered in treating severe or refractory Behçet disease (BD), these biologic agents are associated with potential therapeutic failure due to the multi-cytokine pathogenesis involving Th1... |
PMC5247822 | core_pubmed_pmc | Pharmacokinetics and in vitro efficacy of salicylic acid after oral administration of acetylsalicylic acid in horses | Pharmacokinetics and in vitro efficacy of salicylic acid after oral administration of acetylsalicylic acid in horses Abstract Background Although acetylsalicylic acid (ASA) is not frequently used as a therapeutic agent in horses, its metabolite SA is of special interest in equestrianism since it is a natural component ... |
PMC8352633 | core_pubmed_pmc | Individualized Drugs’ Selection by Evaluation of Drug Properties, Pharmacogenomics and Clinical Parameters: Performance of a Bioinformatic Tool Compared to a Clinically Established Counselling Process | Individualized Drugs’ Selection by Evaluation of Drug Properties, Pharmacogenomics and Clinical Parameters: Performance of a Bioinformatic Tool Compared to a Clinically Established Counselling Process Abstract Abstract Purpose Inefficacy and safety concerns are main medications’ problems, especially in the case of poly... |
PMC10561543 | core_pubmed_pmc | Recurrent toxic epidermal necrolysis with two different drugs in a patient with chronic kidney disease–A case report with an atypical presentation | Recurrent toxic epidermal necrolysis with two different drugs in a patient with chronic kidney disease–A case report with an atypical presentation Abstract Abstract Toxic epidermal necrolysis (TEN) is a dermatologic emergency usually attributed to drugs. Recurrent episodes of TEN are more common in the pediatric popula... |
PMC11578137 | core_pubmed_pmc | Population pharmacokinetics of amodiaquine and piperaquine in African pregnant women with uncomplicated Plasmodium falciparum infections | Population pharmacokinetics of amodiaquine and piperaquine in African pregnant women with uncomplicated Plasmodium falciparum infections Abstract Abstract Artemisinin‐based combination therapy (ACT) is the first‐line recommended treatment for uncomplicated malaria. Pharmacokinetic (PK) properties in pregnant women are ... |
PMC12645622 | core_pubmed_pmc | Development of a novel 18F-labeled radiotracer targeting granzyme B for imaging early tumor responses to immunotherapy | Development of a novel 18F-labeled radiotracer targeting granzyme B for imaging early tumor responses to immunotherapy Abstract Abstract Background Immunotherapy has emerged as a promising avenue for malignant tumors treatment, but methods to validate its in vivo antitumor activity remain limited. Granzyme B, a key med... |
PMC10564204 | core_pubmed_pmc | Antifungal Activity of N-Arylbenzoquinaldinium Derivatives against a Clinical Strain of M. canis | Antifungal Activity of N-Arylbenzoquinaldinium Derivatives against a Clinical Strain of M. canis Abstract Abstract Background: Microsporum canis (Bodin, 1902) is a dermatophyte, which is widely represented in the developing and the developed world alike. Commonly transmitted from domestic animals it is particularly dan... |
PMC10222860 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of β-Cryptoxanthin Supplementation in Healthy Women: A Double-Blind, Randomized, Placebo-Controlled Clinical Trial | Safety, Tolerability, and Pharmacokinetics of β-Cryptoxanthin Supplementation in Healthy Women: A Double-Blind, Randomized, Placebo-Controlled Clinical Trial Abstract Background: β-cryptoxanthin is a dietary carotenoid for which there have been few studies on the safety and pharmacokinetics following daily oral supplem... |
PMC4743204 | core_pubmed_pmc | Three-times-weekly, post-dialysis cefepime therapy in patients on maintenance hemodialysis: a retrospective study | Three-times-weekly, post-dialysis cefepime therapy in patients on maintenance hemodialysis: a retrospective study Abstract Background In hemodialysis patients, post-dialysis treatment with intravenous antibiotics permits even severe infections to be managed on an outpatient basis. Cefepime is a fourth-generation cephal... |
PMC9612372 | core_pubmed_pmc | Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives | Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives Abstract Since their introduction to pharmacotherapy, proton pump inhibitors (PPIs) have been widely used in the treatment of numerous diseases manifested by excessive secretion of gastric acid. Despite that, t... |
PMC10672774 | core_pubmed_pmc | Development of a Predictive Statistical Pharmacological Model for Local Anesthetic Agent Effects with Bayesian Hierarchical Model Parameter Estimation | Development of a Predictive Statistical Pharmacological Model for Local Anesthetic Agent Effects with Bayesian Hierarchical Model Parameter Estimation Abstract As an alternative to animal use, computer simulations are useful for predicting pharmacokinetics and cardiovascular activities. For this purpose, we constructed... |
PMC12641132 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Italy and Spain: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Italy and Spain: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine the antibiotic susceptibility of community-acquired respiratory tract infection (CA-RTI) Strept... |
PMC6925539 | core_pubmed_pmc | Effect of Hemodynamic Changes in Plasma Propofol Concentrations Associated with Knee-Chest Position in Spinal Surgery: A Prospective Study | Effect of Hemodynamic Changes in Plasma Propofol Concentrations Associated with Knee-Chest Position in Spinal Surgery: A Prospective Study Abstract Abstract Background Anesthesia induction and maintenance with propofol can be guided by target-controlled infusion (TCI) systems using pharmacokinetic (Pk) models. Physiolo... |
PMC11434809 | core_pubmed_pmc | Drug Nanocrystals in Oral Absorption: Factors That Influence Pharmacokinetics | Drug Nanocrystals in Oral Absorption: Factors That Influence Pharmacokinetics Abstract Abstract Despite the safety and convenience of oral administration, poorly water-soluble drugs compromise absorption and bioavailability. These drugs can exhibit low dissolution rates, variability between fed and fasted states, diffi... |
PMC9228315 | core_pubmed_pmc | Simultaneous Characterization and Determination of Warfarin and Its Hydroxylation Metabolites in Rat Plasma by Chiral Liquid Chromatography-Tandem Mass Spectrometry | Simultaneous Characterization and Determination of Warfarin and Its Hydroxylation Metabolites in Rat Plasma by Chiral Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract Warfarin is extensively used for venous thromboembolism and other coagulopathies. In clinical settings, warfarin is administered as a mix... |
PMC12641131 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2020–21 in Vietnam: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2020–21 in Vietnam: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives Antibiotic susceptibility determination of Streptococcus pneumoniae and Haemophilus influenzae from community-acquir... |
PMC7368963 | core_pubmed_pmc | Botanical and Traditional Uses and Phytochemical, Pharmacological, Pharmacokinetic, and Toxicological Characteristics of Ziziphi Spinosae Semen : A Review | Botanical and Traditional Uses and Phytochemical, Pharmacological, Pharmacokinetic, and Toxicological Characteristics of Ziziphi Spinosae Semen : A Review Abstract Ziziphi Spinosae Semen (ZS, the seeds of Ziziphus jujuba Mill . var. spinosa (Bunge) Hu ex H. F. Chou) is used as a traditional Chinese medicine referred to... |
PMC11315406 | core_pubmed_pmc | Phase II Efficacy and Safety of 80 mg Osimertinib in Patients With Leptomeningeal Metastases Associated With Epidermal Growth Factor Receptor Mutation–Positive Non–Small Cell Lung Cancer (BLOSSOM) | Phase II Efficacy and Safety of 80 mg Osimertinib in Patients With Leptomeningeal Metastases Associated With Epidermal Growth Factor Receptor Mutation–Positive Non–Small Cell Lung Cancer (BLOSSOM) Abstract PURPOSE Leptomeningeal metastases (LMs) exhibit a high incidence in patients with epidermal growth factor receptor... |
PMC10825021 | core_pubmed_pmc | Exposure–response analysis using time-to-event data for bevacizumab biosimilar SB8 and the reference bevacizumab | Exposure–response analysis using time-to-event data for bevacizumab biosimilar SB8 and the reference bevacizumab Abstract Abstract Purpose: This analysis aimed to characterize the exposure–response relationship of bevacizumab in non-small-cell lung cancer (NSCLC) and evaluate the efficacy of SB8, a bevacizumab biosimil... |
PMC9928570 | core_pubmed_pmc | Computational Study of Bis-(1-(Benzoyl)-3-Methyl Thiourea) Platinum (II) Complex Derivatives as Anticancer Candidates | Computational Study of Bis-(1-(Benzoyl)-3-Methyl Thiourea) Platinum (II) Complex Derivatives as Anticancer Candidates Abstract Abstract Background The increasing incidence of cancer every year has resulted in cancer becoming one of the most common causes of death in the world. The most common types of cancer are breast... |
PMC11742240 | core_pubmed_pmc | In vitro evaluation of using ceftazidime/avibactam against carbapenem-resistant Acinetobacter baumannii | In vitro evaluation of using ceftazidime/avibactam against carbapenem-resistant Acinetobacter baumannii Abstract Abstract Objective: Carbapenem-resistant Acinetobacter baumannii (CRAB) is a global concern as effective treatments are very limited. We previously used a modified susceptibility testing approach to predict ... |
PMC6113706 | core_pubmed_pmc | Andecaliximab [Anti-matrix Metalloproteinase-9] Induction Therapy for Ulcerative Colitis: A Randomised, Double-Blind, Placebo-Controlled, Phase 2/3 Study in Patients With Moderate to Severe Disease | Andecaliximab [Anti-matrix Metalloproteinase-9] Induction Therapy for Ulcerative Colitis: A Randomised, Double-Blind, Placebo-Controlled, Phase 2/3 Study in Patients With Moderate to Severe Disease Abstract Abstract Background and Aims Matrix metalloproteinase-9 [MMP9] is implicated in the pathogenesis of ulcerative co... |
PMC10874764 | core_pubmed_pmc | Effect of Rhei Radix et Rhizoma and Eupolyphaga Steleophaga on liver protection mechanism based on pharmacokinetics and metabonomics | Effect of Rhei Radix et Rhizoma and Eupolyphaga Steleophaga on liver protection mechanism based on pharmacokinetics and metabonomics Abstract Abstract Objective Based on metabonomics technology of high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS) and hydrogen nuclear magnetic resonance spectroscopy ... |
PMC4670010 | core_pubmed_pmc | Using Akaike's information theoretic criterion in mixed-effects modeling of pharmacokinetic data: a simulation study | Using Akaike's information theoretic criterion in mixed-effects modeling of pharmacokinetic data: a simulation study Abstract Abstract Akaike's information theoretic criterion for model discrimination (AIC) is often stated to "overfit", i.e., it selects models with a higher dimension than the dimension of the model tha... |
PMC7070814 | core_pubmed_pmc | Dosage Regimens for Meropenem in Children with Pseudomonas Infections Do Not Meet Serum Concentration Targets | Dosage Regimens for Meropenem in Children with Pseudomonas Infections Do Not Meet Serum Concentration Targets Abstract There have been literature reports that some recommended meropenem dosage regimens may fail to meet therapeutic targets in some high‐risk children and adults. We evaluated this observation in children ... |
PMC8182383 | core_pubmed_pmc | MicroRNA-sensitive oncolytic measles virus for chemovirotherapy of pancreatic cancer | MicroRNA-sensitive oncolytic measles virus for chemovirotherapy of pancreatic cancer Abstract Advanced pancreatic cancer is characterized by few treatment options and poor outcomes. Oncolytic virotherapy and chemotherapy involve complementary pharmacodynamics and could synergize to improve therapeutic efficacy. Likewis... |
PMC7070804 | core_pubmed_pmc | Predicting In Vivo Efficacy from In Vitro Data: Quantitative Systems Pharmacology Modeling for an Epigenetic Modifier Drug in Cancer | Predicting In Vivo Efficacy from In Vitro Data: Quantitative Systems Pharmacology Modeling for an Epigenetic Modifier Drug in Cancer Abstract Reliably predicting in vivo efficacy from in vitro data would facilitate drug development by reducing animal usage and guiding drug dosing in human clinical trials. However, such... |
PMC8961117 | core_pubmed_pmc | Phase I, multicenter, open-label study of intravenous VCN-01 oncolytic adenovirus with or without nab-paclitaxel plus gemcitabine in patients with advanced solid tumors | Phase I, multicenter, open-label study of intravenous VCN-01 oncolytic adenovirus with or without nab-paclitaxel plus gemcitabine in patients with advanced solid tumors Abstract Background VCN-01 is an oncolytic adenovirus (Ad5 based) designed to replicate in cancer cells with dysfunctional RB1 pathway, express hyaluro... |
PMC12389586 | core_pubmed_pmc | Anticancer Activity of Paclitaxel-Loaded Mesoporous Silica Nanoparticles in B16F10 Melanoma-Bearing Mice | Anticancer Activity of Paclitaxel-Loaded Mesoporous Silica Nanoparticles in B16F10 Melanoma-Bearing Mice Abstract Background/Objectives : Paclitaxel (PTX) faces clinical limitations in melanoma treatment due to poor solubility, P-glycoprotein (P-gp)-mediated efflux, and systemic toxicity. This study aimed to develop PT... |
PMC10754736 | core_pubmed_pmc | Oral Versus Subcutaneous Methotrexate in Immune-Mediated Inflammatory Disorders: an Update of the Current Literature | Oral Versus Subcutaneous Methotrexate in Immune-Mediated Inflammatory Disorders: an Update of the Current Literature Abstract Purpose This review aims to critically evaluate the potential benefit of either oral or subcutaneous administration of methotrexate (MTX) in various immune-mediated inflammatory disorders (IMIDs... |
PMC9311849 | core_pubmed_pmc | Population Pharmacokinetics of Temocillin Administered by Continuous Infusion in Patients with Septic Shock Associated with Intra-Abdominal Infection and Ascitic Fluid Effusion | Population Pharmacokinetics of Temocillin Administered by Continuous Infusion in Patients with Septic Shock Associated with Intra-Abdominal Infection and Ascitic Fluid Effusion Abstract Abstract Temocillin is active against Gram-negative bacteria, including many extended-spectrum β-lactamase (ESBL)-producing Enterobact... |
PMC10461390 | core_pubmed_pmc | Impact of clinical pharmacist-led intervention for drug-related problems in neonatal intensive care unit a randomized controlled trial | Impact of clinical pharmacist-led intervention for drug-related problems in neonatal intensive care unit a randomized controlled trial Abstract Introduction: Drug-related problems (DRPs) incidence is higher in neonatal intensive care units (NICUs), compared to other pediatric wards due to aspects like off-label medicat... |
PMC3737112 | core_pubmed_pmc | Identification of resistance of Plasmodium falciparum to artesunate-mefloquine combination in an area along the Thai-Myanmar border: integration of clinico-parasitological response, systemic drug exposure, and in vitro parasite sensitivity | Identification of resistance of Plasmodium falciparum to artesunate-mefloquine combination in an area along the Thai-Myanmar border: integration of clinico-parasitological response, systemic drug exposure, and in vitro parasite sensitivity Abstract Abstract Background A markedly high failure rate of three-day artesunat... |
PMC4948716 | core_pubmed_pmc | Cancer pharmacogenomics, challenges in implementation, and patient-focused perspectives | Cancer pharmacogenomics, challenges in implementation, and patient-focused perspectives Abstract Cancer pharmacogenomics is an evolving landscape and has the potential to significantly impact cancer care and precision medicine. Harnessing and understanding the genetic code of both the patient (germline) and the tumor (... |
PMC8949893 | core_pubmed_pmc | Chemical Synthesis, Pharmacokinetic Properties and Biological Effects of JM-00266, a Putative Non-Brain Penetrant Cannabinoid Receptor 1 Inverse Agonist | Chemical Synthesis, Pharmacokinetic Properties and Biological Effects of JM-00266, a Putative Non-Brain Penetrant Cannabinoid Receptor 1 Inverse Agonist Abstract Abstract Targeting cannabinoid 1 receptors (CB1R) with peripherally restricted antagonists (or inverse agonists) shows promise to improve metabolic disorders ... |
PMC8780797 | core_pubmed_pmc | T908 Polymeric Micelles Improved the Uptake of Sgc8-c Aptamer Probe in Tumor-Bearing Mice: A Co-Association Study between the Probe and Preformed Nanostructures | T908 Polymeric Micelles Improved the Uptake of Sgc8-c Aptamer Probe in Tumor-Bearing Mice: A Co-Association Study between the Probe and Preformed Nanostructures Abstract Abstract Aptamers are oligonucleotides that have the characteristic of recognizing a target with high affinity and specificity. Based on our previous ... |
PMC4004800 | core_pubmed_pmc | Preclinical evaluation of marketed sodium channel blockers in a rat model of myotonia discloses promising antimyotonic drugs | Preclinical evaluation of marketed sodium channel blockers in a rat model of myotonia discloses promising antimyotonic drugs Abstract Abstract Although the sodium channel blocker mexiletine is considered the first-line drug in myotonia, some patients experiment adverse effects, while others do not gain any benefit. Oth... |
PMC12638300 | core_pubmed_pmc | Design and evaluation of octopromycin-derived peptides as multifunctional antimicrobial agents against multidrug-resistant pathogens | Design and evaluation of octopromycin-derived peptides as multifunctional antimicrobial agents against multidrug-resistant pathogens Abstract Octopromycin (OPM), an antimicrobial peptide from Octopus minor , shows potent activity against multidrug-resistant (MDR) Acinetobacter baumannii . Guided by the structure–activi... |
PMC10582666 | core_pubmed_pmc | Pharmacokinetics, safety, and tolerability of BMS‐986263, a lipid nanoparticle containing HSP47 siRNA, in participants with hepatic impairment | Pharmacokinetics, safety, and tolerability of BMS‐986263, a lipid nanoparticle containing HSP47 siRNA, in participants with hepatic impairment Abstract Abstract BMS‐986263 is a retinoid‐conjugated lipid nanoparticle delivering small interfering RNA designed to inhibit synthesis of HSP47 protein, a collagen‐specific cha... |
PMC4467253 | core_pubmed_pmc | Absence of QTc Prolongation with Domperidone: A Randomized, Double-Blind, Placebo- and Positive-Controlled Thorough QT/QTc Study in Healthy Volunteers | Absence of QTc Prolongation with Domperidone: A Randomized, Double-Blind, Placebo- and Positive-Controlled Thorough QT/QTc Study in Healthy Volunteers Abstract Abstract Domperidone effects on QTc duration were assessed in a single-center, double-blind, four-way crossover study of 44 healthy participants randomized to o... |
PMC8085606 | core_pubmed_pmc | Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment | Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment Abstract Aim Diabetic (type-2) is a metabolic disease characterized by increased blood glucose level from the normal level. In the present study, apigenin (AG) loaded lipid vesicles (bilosomes: BIL) was prepared, optimized... |
PMC10045242 | core_pubmed_pmc | A Comprehensive Review on Chemical Synthesis and Chemotherapeutic Potential of 3-Heteroaryl Fluoroquinolone Hybrids | A Comprehensive Review on Chemical Synthesis and Chemotherapeutic Potential of 3-Heteroaryl Fluoroquinolone Hybrids Abstract Abstract Fluoroquinolones have been studied for more than half a century. Since the 1960s, four generations of these synthetic antibiotics have been created and successfully introduced into clini... |
PMC5811607 | core_pubmed_pmc | Development of a primary human Small Intestine-on-a-Chip using biopsy-derived organoids | Development of a primary human Small Intestine-on-a-Chip using biopsy-derived organoids Abstract Here we describe a method for fabricating a primary human Small Intestine-on-a-Chip (Intestine Chip) containing epithelial cells isolated from healthy regions of intestinal biopsies. The primary epithelial cells are expande... |
PMC4470182 | core_pubmed_pmc | Review of Tolvaptan’s Pharmacokinetic and Pharmacodynamic Properties and Drug Interactions | Review of Tolvaptan’s Pharmacokinetic and Pharmacodynamic Properties and Drug Interactions Abstract Tolvaptan is an arginine vasopressin (AVP) antagonist that acts to increase excretion of free water (aquaresis) in patients without introducing electrolyte abnormalities or worsening renal function. It works via blockade... |
PMC8880588 | core_pubmed_pmc | In-Silico Screening of Novel Synthesized Thienopyrimidines Targeting Fms Related Receptor Tyrosine Kinase-3 and Their In-Vitro Biological Evaluation | In-Silico Screening of Novel Synthesized Thienopyrimidines Targeting Fms Related Receptor Tyrosine Kinase-3 and Their In-Vitro Biological Evaluation Abstract The present investigation describes the design strategy and synthesis of novel thienopyrimidine compounds in addition to their anticancer activity targeting tyros... |
PMC12847619 | core_pubmed_pmc | In silico prediction, molecular docking and simulation of natural flavonoid apigenin and xanthoangelol E against human metapneumovirus | In silico prediction, molecular docking and simulation of natural flavonoid apigenin and xanthoangelol E against human metapneumovirus Abstract Human metapneumovirus (hMPV) is one of the potential pandemic pathogens, and it is a concern for elderly subjects and immunocompromised patients. There is no vaccine or specifi... |
PMC6709459 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Intravenous Durlobactam and Sulbactam in Subjects with Renal Impairment and Healthy Matched Control Subjects | Pharmacokinetics, Safety, and Tolerability of Intravenous Durlobactam and Sulbactam in Subjects with Renal Impairment and Healthy Matched Control Subjects Abstract Sulbactam-durlobactam is being developed for the treatment of infections caused by Acinetobacter baumannii , including those caused by multidrug- and carbap... |
PMC8349134 | core_pubmed_pmc | Identification of lead compounds from large natural product library targeting 3C-like protease of SARS-CoV-2 using E-pharmacophore modelling, QSAR and molecular dynamics simulation | Identification of lead compounds from large natural product library targeting 3C-like protease of SARS-CoV-2 using E-pharmacophore modelling, QSAR and molecular dynamics simulation Abstract COVID-19 is a novel disease caused by SARS-CoV-2 and has made a catastrophic impact on the global economy. As it is, there is no o... |
PMC10772894 | core_pubmed_pmc | Use of direct oral anticoagulants for venous thromboembolism treatment at extremes of body weight, renal and liver function: an illustrated review | Use of direct oral anticoagulants for venous thromboembolism treatment at extremes of body weight, renal and liver function: an illustrated review Abstract Abstract Direct oral anticoagulants (DOACs) have been a welcome addition to clinical practice due to the practical advantages they confer over traditional anticoagu... |
PMC11434838 | core_pubmed_pmc | Subcellular Drug Distribution: Exploring Organelle-Specific Characteristics for Enhanced Therapeutic Efficacy | Subcellular Drug Distribution: Exploring Organelle-Specific Characteristics for Enhanced Therapeutic Efficacy Abstract Abstract The efficacy and potential toxicity of drug treatments depends on the drug concentration at its site of action, intricately linked to its distribution within diverse organelles of mammalian ce... |
PMC7539608 | core_pubmed_pmc | Improving the therapeutic index in adoptive cell therapy: key factors that impact efficacy | Improving the therapeutic index in adoptive cell therapy: key factors that impact efficacy Abstract The therapeutic index (TI) is a quantitative assessment of a drug safety proportional to its effectiveness. The estimation is intuitive when the engagement of the product with its target is dependent on stable chemistry ... |
PMC7150936 | core_pubmed_pmc | Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A | Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A Abstract Abstract The physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, su... |
PMC8066100 | core_pubmed_pmc | Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization | Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization Abstract Abstract Green nanotechnology utilizes the principles of green chemistry to formulate eco-friendly nanocarrier systems to mitigate patient... |
PMC10718122 | core_pubmed_pmc | Comparative Efficacy and Safety of Super-Bioavailable Itraconazole-130 mg Once Daily in Obese and Non-Obese Patients of Glabrous Tinea | Comparative Efficacy and Safety of Super-Bioavailable Itraconazole-130 mg Once Daily in Obese and Non-Obese Patients of Glabrous Tinea Abstract Background: Obesity is considered one of the risk factors for dermatophytosis and warrants systemic therapy. Itraconazole is the most commonly used antifungal, but owing to pha... |
PMC9306230 | core_pubmed_pmc | Favipiravir and/or nitazoxanide: a randomized, double-blind, placebo-controlled trial of early therapy in COVID-19 in health workers, their household members, and patients treated at IMSS (FANTAZE) | Favipiravir and/or nitazoxanide: a randomized, double-blind, placebo-controlled trial of early therapy in COVID-19 in health workers, their household members, and patients treated at IMSS (FANTAZE) Abstract Background The 2020 pandemic of SARS-CoV-2 causing COVID-19 disease is an unprecedented global emergency. COVID-1... |
PMC5605383 | core_pubmed_pmc | Study on pharmacokinetics and tissue distribution of single dose oral tryptanthrin in Kunming mice by validated reversed-phase high-performance liquid chromatography with ultraviolet detection | Study on pharmacokinetics and tissue distribution of single dose oral tryptanthrin in Kunming mice by validated reversed-phase high-performance liquid chromatography with ultraviolet detection Abstract Abstract Background Tryptanthrin is a major active constituent of several Chinese herbal plants, such as Isatidis radi... |
PMC9791134 | core_pubmed_pmc | Kir4.1 channel activation in NG2 glia contributes to remyelination in ischemic stroke | Kir4.1 channel activation in NG2 glia contributes to remyelination in ischemic stroke Abstract Summary Background Stroke is one of the most common neurological diseases in the world and is clinically manifested by transient or permanent brain dysfunction. It has a high mortality and disability rate, which severely affe... |
PMC4779096 | core_pubmed_pmc | An Integrated Strategy for Implementation of Dried Blood Spots in Clinical Development Programs | An Integrated Strategy for Implementation of Dried Blood Spots in Clinical Development Programs Abstract Dried blood spot (DBS) sample collection has gained increased interest across the pharmaceutical industry as a potential alternative to plasma for pharmacokinetic (PK) evaluations. However, regulatory guidelines and... |
PMC4244809 | core_pubmed_pmc | Applications of linking PBPK and PD models to predict the impact of genotypic variability, formulation differences, differences in target binding capacity and target site drug concentrations on drug responses and variability | Applications of linking PBPK and PD models to predict the impact of genotypic variability, formulation differences, differences in target binding capacity and target site drug concentrations on drug responses and variability Abstract Abstract This study aimed to demonstrate the added value of integrating prior in vitro... |
PMC10059750 | core_pubmed_pmc | Glycosylation and Lipidation Strategies: Approaches for Improving Antimicrobial Peptide Efficacy | Glycosylation and Lipidation Strategies: Approaches for Improving Antimicrobial Peptide Efficacy Abstract Abstract Antimicrobial peptides (AMPs) have recently gained attention as a viable solution for combatting antibiotic resistance due to their numerous advantages, including their broad-spectrum activity, low propens... |
PMC4754004 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic relationship of anesthetic drugs: from modeling to clinical use | Pharmacokinetic-pharmacodynamic relationship of anesthetic drugs: from modeling to clinical use Abstract Abstract Anesthesia is a combination of unconsciousness, amnesia, and analgesia, expressed in sleeping patients by limited reaction to noxious stimulations. It is achieved by several classes of drugs, acting mainly ... |
PMC10605826 | core_pubmed_pmc | In Vivo Application of Carboranes for Boron Neutron Capture Therapy (BNCT): Structure, Formulation and Analytical Methods for Detection | In Vivo Application of Carboranes for Boron Neutron Capture Therapy (BNCT): Structure, Formulation and Analytical Methods for Detection Abstract Simple Summary Boron neutron capture therapy (BNCT) is an emerging anticancer treatment. The success of BNCT relies on the delivery of adequate quantities of 10 B to tumor cel... |
PMC10095881 | core_pubmed_pmc | Papaverine: A Miraculous Alkaloid from Opium and Its Multimedicinal Application | Papaverine: A Miraculous Alkaloid from Opium and Its Multimedicinal Application Abstract The pharmacological actions of benzylisoquinoline alkaloids are quite substantial, and have recently attracted much attention. One of the principle benzylisoquinoline alkaloids has been found in the unripe seed capsules of Papaver ... |
PMC9312304 | core_pubmed_pmc | Concentration-Dependent Activity of Pazufloxacin against Pseudomonas aeruginosa : An In Vivo Pharmacokinetic/Pharmacodynamic Study | Concentration-Dependent Activity of Pazufloxacin against Pseudomonas aeruginosa : An In Vivo Pharmacokinetic/Pharmacodynamic Study Abstract The bacterium Pseudomonas aeruginosa is known to be associated with nosocomial infections around the world. Pazufloxacin, a potent DNA gyrase inhibitor, is known to be an effective... |
PMC11963596 | core_pubmed_pmc | Usefulness of a hub and spoke TDM-guided expert clinical pharmacological advice program of dalbavancin for optimizing very long-term curative or suppressive treatment of chronic staphylococcal infections | Usefulness of a hub and spoke TDM-guided expert clinical pharmacological advice program of dalbavancin for optimizing very long-term curative or suppressive treatment of chronic staphylococcal infections Abstract ABSTRACT A hub and spoke model for optimizing long-term treatment of chronic staphylococcal infections with... |
PMC10540618 | core_pubmed_pmc | Pre-clinical investigation of liquid sirolimus for local drug delivery | Pre-clinical investigation of liquid sirolimus for local drug delivery Abstract Abstract Introduction Sirolimus is currently being explored as an alternative drug to paclitaxel for the treatment of peripheral artery disease (PAD). To date, sirolimus has only been used as drug coatings for stents and balloons and no stu... |
PMC7057431 | core_pubmed_pmc | Poor outcome with anti-programmed death-ligand 1 (PD-L1) antibody due to poor pharmacokinetic properties in PD-1/PD-L1 blockade-sensitive mouse models | Poor outcome with anti-programmed death-ligand 1 (PD-L1) antibody due to poor pharmacokinetic properties in PD-1/PD-L1 blockade-sensitive mouse models Abstract Abstract Background Recently, antiprogrammed cell death protein 1 (aPD-1) and antiprogrammed death-ligand 1 (aPD-L1) monoclonal antibodies (mAbs) have been appr... |
PMC6121755 | core_pubmed_pmc | Focus on biosimilar etanercept – bioequivalence and interchangeability | Focus on biosimilar etanercept – bioequivalence and interchangeability Abstract Abstract Background The recent approval of reference etanercept (re-ETN) biosimilars SB4, GP2015, and HD203 produced relevant changes in the management of rheumatoid arthritis (RA), psoriatic arthritis, and ankylosing spondylitis due to the... |
PMC6189912 | core_pubmed_pmc | Microfluidic-Based Multi-Organ Platforms for Drug Discovery | Microfluidic-Based Multi-Organ Platforms for Drug Discovery Abstract Development of predictive multi-organ models before implementing costly clinical trials is central for screening the toxicity, efficacy, and side effects of new therapeutic agents. Despite significant efforts that have been recently made to develop bi... |
PMC7686626 | core_pubmed_pmc | Simultaneous determination of calycosin, prim- O -glucosylcimifugin, and paeoniflorin in rat plasma by HPLC-MS/MS: application in the pharmacokinetic analysis of HQCF | Simultaneous determination of calycosin, prim- O -glucosylcimifugin, and paeoniflorin in rat plasma by HPLC-MS/MS: application in the pharmacokinetic analysis of HQCF Abstract Objective This study aimed to develop and validate a high-performance liquid chromatography–tandem mass spectrometry method to simultaneously de... |
PMC3913846 | core_pubmed_pmc | A first-in-human dose-escalation study of ME-143, a second generation NADH oxidase inhibitor, in patients with advanced solid tumors | A first-in-human dose-escalation study of ME-143, a second generation NADH oxidase inhibitor, in patients with advanced solid tumors Abstract Summary Background ME-143, a second-generation tumor-specific NADH oxidase inhibitor, is broadly active against human cancers in vitro and in vivo . This first-in-human dose-esca... |
PMC10746576 | core_pubmed_pmc | Vincristine-based nanoformulations: a preclinical and clinical studies overview | Vincristine-based nanoformulations: a preclinical and clinical studies overview Abstract Vincristine (VCR) is a chemotherapeutic agent obtained from natural alkaloid plant source Catharanthus roseus. VCR has been significantly useful in treatments of lung cancer, lymphocyte-based leukaemia, glioblastomas and acute myel... |
PMC7011789 | core_pubmed_pmc | In silico identification of promiscuous scaffolds as potential inhibitors of 1-deoxy- d -xylulose 5-phosphate reductoisomerase for treatment of Falciparum malaria | In silico identification of promiscuous scaffolds as potential inhibitors of 1-deoxy- d -xylulose 5-phosphate reductoisomerase for treatment of Falciparum malaria Abstract Abstract Context: Malaria remains one of the prevalent infectious diseases worldwide. Plasmodium falciparum 1-deoxy- d -xylulose-5-phosphate reducto... |
PMC3899455 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Immunogenicity of Belatacept in Adult Kidney Transplant Recipients | Pharmacokinetics, Pharmacodynamics, and Immunogenicity of Belatacept in Adult Kidney Transplant Recipients Abstract Abstract Background and Objectives Belatacept is a first-in-class, selective co-stimulation blocker recently approved for the prophylaxis of organ rejection in adult kidney transplant recipients. The obje... |
PMC10544008 | core_pubmed_pmc | MTX-13, a Novel PTK7-Directed Antibody–Drug Conjugate with Widened Therapeutic Index Shows Sustained Tumor Regressions for a Broader Spectrum of PTK7-Positive Tumors | MTX-13, a Novel PTK7-Directed Antibody–Drug Conjugate with Widened Therapeutic Index Shows Sustained Tumor Regressions for a Broader Spectrum of PTK7-Positive Tumors Abstract Abstract Protein tyrosine kinase 7 (PTK7) is a Wnt signaling pathway protein implicated in cancer development and metastasis. When using a potent... |
PMC6511943 | core_pubmed_pmc | Structure-Guided Drug Design of 6-Substituted Adenosine Analogues as Potent Inhibitors of Mycobacterium tuberculosis Adenosine Kinase | Structure-Guided Drug Design of 6-Substituted Adenosine Analogues as Potent Inhibitors of Mycobacterium tuberculosis Adenosine Kinase Abstract Abstract Mycobacterium tuberculosis adenosine kinase (MtbAdoK) is an essential enzyme of Mtb and forms part of the purine salvage pathway within mycobacteria. Evidence suggests ... |
PMC6958579 | core_pubmed_pmc | Drug related problems in admitted geriatric patients: the impact of clinical pharmacist interventions | Drug related problems in admitted geriatric patients: the impact of clinical pharmacist interventions Abstract Abstract Background Geriatric patients are at high risk of Drug Related Problems (DRPs) due to multi- morbidity associated polypharmacy, age related physiologic changes, pharmacokinetic and pharmacodynamics al... |
PMC3046530 | core_pubmed_pmc | Steady-state mycophenolate mofetil pharmacokinetic parameters enable prediction of systemic lupus erythematosus clinical flares: an observational cohort study | Steady-state mycophenolate mofetil pharmacokinetic parameters enable prediction of systemic lupus erythematosus clinical flares: an observational cohort study Abstract Abstract Introduction The aim of this study was to determine whether mycophenolate mofetil (MMF) pharmacokinetics (PK) under combined MMF and prednisone... |
PMC5425488 | core_pubmed_pmc | Disease–Drug Interaction of Sarilumab and Simvastatin in Patients with Rheumatoid Arthritis | Disease–Drug Interaction of Sarilumab and Simvastatin in Patients with Rheumatoid Arthritis Abstract Introduction Elevated interleukin (IL)-6 occurs in patients with active rheumatoid arthritis (RA), which has been shown to lead to a decrease in cytochrome P450 (CYP) enzyme activity and alterations in drug concentratio... |
PMC9325633 | core_pubmed_pmc | Antimicrobial Alkaloids from Marine-Derived Fungi as Drug Leads versus COVID-19 Infection: A Computational Approach to Explore their Anti-COVID-19 Activity and ADMET Properties | Antimicrobial Alkaloids from Marine-Derived Fungi as Drug Leads versus COVID-19 Infection: A Computational Approach to Explore their Anti-COVID-19 Activity and ADMET Properties Abstract Therapeutic strategies based upon enzyme inhibition have recently gained higher attention in treating hazardous ailments. Herein, the ... |
PMC9250196 | core_pubmed_pmc | A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors | A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors Abstract Background Glutamate signaling activates MAPK and PI3K/AKT pathways in tumor cells. Treatment with riluzole, a glutamate release inhibitor,... |
PMC12167911 | core_pubmed_pmc | Pharmacokinetic Model‐Informed Precision Dosing of Natalizumab in Multiple Sclerosis | Pharmacokinetic Model‐Informed Precision Dosing of Natalizumab in Multiple Sclerosis Abstract ABSTRACT Intravenous natalizumab is an effective treatment for relapsing–remitting multiple sclerosis. However, the standard treatment interval of 4 weeks may be excessive for many patients. Personalized interval extension usi... |
PMC9835671 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacokinetic/Pharmacodynamic Target Attainment Analyses for Dalbavancin in Pediatric Patients | Population Pharmacokinetic and Pharmacokinetic/Pharmacodynamic Target Attainment Analyses for Dalbavancin in Pediatric Patients Abstract Background: Dalbavancin, approved for the treatment of pediatric and adult patients with acute bacterial skin and skin structure infections, has a terminal half-life of >14 days allow... |
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