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PMC12149789 | core_pubmed_pmc | Pharmacotherapy research landscape and knowledge gaps of opioids in maternal and pediatric populations | Pharmacotherapy research landscape and knowledge gaps of opioids in maternal and pediatric populations Abstract Abstract The use and misuse of opioids has surged in the past decade, with nearly half of the users being female. Although opioid use is lower among pregnant women, trends mirror the general population. While... |
PMC7520022 | core_pubmed_pmc | Treating schizophrenia with cariprazine: from clinical research to clinical practice. Real world experiences and recommendations from an International Panel | Treating schizophrenia with cariprazine: from clinical research to clinical practice. Real world experiences and recommendations from an International Panel Abstract Abstract Background Management of schizophrenia is sub-optimal in many patients. Targeting negative symptoms, among the most debilitating aspects of schiz... |
PMC12120100 | core_pubmed_pmc | Synthesis, anticancer evaluation, and electrochemical investigation of new chiral pyrazolo[4,3- e ]tetrazolo[1,5- b ][1,2,4]triazine sulfonamides | Synthesis, anticancer evaluation, and electrochemical investigation of new chiral pyrazolo[4,3- e ]tetrazolo[1,5- b ][1,2,4]triazine sulfonamides Abstract Abstract Pyrazolo[4,3- e ]tetrazolo[1,5- b ]triazine sulfonamides ( MM -compounds) represent a novel class of heterocyclic compounds with promising anticancer potent... |
PMC9085981 | core_pubmed_pmc | Opioid Use Disorder Curriculum: Preclerkship Pharmacology Case-Based Learning Session | Opioid Use Disorder Curriculum: Preclerkship Pharmacology Case-Based Learning Session Abstract Introduction During the first year of the COVID-19 pandemic, over 93,000 Americans lost their lives to a preventable overdose. Medications for opioid use disorder (OUD) have been shown to decrease mortality in OUD but are und... |
PMC11075158 | core_pubmed_pmc | Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration | Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration Abstract Abstract Background and purporse The combination of alginate and gum acacia in previous studies showed good results in inhibiting ketoconazole precipitation due to the supersatu... |
PMC8846628 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of tadalafil to inform pediatric dose selection in children with pulmonary arterial hypertension | Physiologically based pharmacokinetic modeling of tadalafil to inform pediatric dose selection in children with pulmonary arterial hypertension Abstract Abstract Tadalafil, a phosphodiesterase 5 inhibitor, is being investigated as a treatment for pulmonary arterial hypertension (PAH) in children aged 6 months to less t... |
PMC7335700 | core_pubmed_pmc | Major Neurologic Adverse Drug Reactions, Potential Drug–Drug Interactions and Pharmacokinetic Aspects of Drugs Used in COVID-19 Patients with Stroke: A Narrative Review | Major Neurologic Adverse Drug Reactions, Potential Drug–Drug Interactions and Pharmacokinetic Aspects of Drugs Used in COVID-19 Patients with Stroke: A Narrative Review Abstract Abstract Stroke has been considered as one of the underlying diseases that increases the probability of severe infection and mortality. Meanwh... |
PMC10658550 | core_pubmed_pmc | Pharmacokinetics of pimobendan after oral administration to dogs with myxomatous mitral valve disease | Pharmacokinetics of pimobendan after oral administration to dogs with myxomatous mitral valve disease Abstract Abstract Background Pimobendan is an important therapy for dogs with myxomatous mitral valve disease (MMVD). The pharmacokinetics are reported in healthy dogs but not in dogs with heart disease. Hypothesis/Obj... |
PMC7475792 | core_pubmed_pmc | Plazomicin: a new aminoglycoside in the fight against antimicrobial resistance | Plazomicin: a new aminoglycoside in the fight against antimicrobial resistance Abstract Objective: To review the mechanism of action, mechanisms of resistance, in vitro activity, pharmacokinetics, pharmacodynamics, and clinical data for a novel aminoglycoside. Data sources: A PubMed search was performed from January 20... |
PMC6850605 | core_pubmed_pmc | The oral Janus kinase/spleen tyrosine kinase inhibitor ASN002 demonstrates efficacy and improves associated systemic inflammation in patients with moderate‐to‐severe atopic dermatitis: results from a randomized double‐blind placebo‐controlled study † | The oral Janus kinase/spleen tyrosine kinase inhibitor ASN002 demonstrates efficacy and improves associated systemic inflammation in patients with moderate‐to‐severe atopic dermatitis: results from a randomized double‐blind placebo‐controlled study † Abstract Summary Background ASN002 is an oral dual inhibitor of Janus... |
PMC12891084 | core_pubmed_pmc | Optimising anti-seizure medication timing using a dynamic network model of seizure rhythms | Optimising anti-seizure medication timing using a dynamic network model of seizure rhythms Abstract Epileptic seizures and interictal discharges exhibit robust circadian and multidien rhythms, yet the interaction between these biological cycles and anti-seizure medication (ASM) pharmacology remains poorly understood. H... |
PMC4989015 | core_pubmed_pmc | A population approach to characterise amisulpride pharmacokinetics in older people and Alzheimer’s disease | A population approach to characterise amisulpride pharmacokinetics in older people and Alzheimer’s disease Abstract Abstract Introduction Current prescribing guidelines for the antipsychotic amisulpride are based largely on pharmacokinetic (PK) studies in young adults, and there is a relative absence of data on older p... |
PMC7063935 | core_pubmed_pmc | Patterns of Medication Exposure in Children on Extracorporeal Membrane Oxygenation: A Step in Prioritizing Future Pharmacologic Studies | Patterns of Medication Exposure in Children on Extracorporeal Membrane Oxygenation: A Step in Prioritizing Future Pharmacologic Studies Abstract Supplemental Digital Content is available in the text. Keywords: critical care, drug utilization, extracorporeal life support, pediatrics, pharmacokinetics, review literature ... |
PMC12830199 | core_pubmed_pmc | A Phase I Randomized Trial of Topical Insulin for Glaucoma: Safety and Efficacy Outcomes | A Phase I Randomized Trial of Topical Insulin for Glaucoma: Safety and Efficacy Outcomes Abstract Purpose Insulin is neuroprotective in mouse and nonhuman primate models of glaucoma. Here we evaluate the safety and efficacy of topical insulin in human patients with glaucoma. Methods This prospective study of once-daily... |
PMC5226282 | core_pubmed_pmc | Application of a systems pharmacology model for translational prediction of hERG‐mediated QTc prolongation | Application of a systems pharmacology model for translational prediction of hERG‐mediated QTc prolongation Abstract Abstract Drug‐induced QTc interval prolongation ( Δ QTc) is a main surrogate for proarrhythmic risk assessment. A higher in vivo than in vitro potency for hERG‐mediated QTc prolongation has been suggested... |
PMC5369137 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Responses to Clopidogrel: Evidences and Perspectives | Pharmacokinetic and Pharmacodynamic Responses to Clopidogrel: Evidences and Perspectives Abstract Abstract Clopidogrel has significantly reduced the incidence of recurrent atherothrombotic events in patients with acute coronary syndrome (ACS) and in those undergoing percutaneous coronary intervention (PCI). However, re... |
PMC9755925 | core_pubmed_pmc | Bayesian forecasting of tumor size metrics and overall survival | Bayesian forecasting of tumor size metrics and overall survival Abstract Abstract The tumor size ratio (TSR), time‐to‐tumor growth (TTG), and tumor growth rate (kG) are frequently suggested as model‐based predictors of overall survival (OS) for different types of tumors. When the tumor metrics are applied in forecastin... |
PMC6271545 | core_pubmed_pmc | Comparative Pharmacokinetics Study of Sinomenine in Rats after Oral Administration of Sinomenine Monomer and Sinomenium Acutum Extract | Comparative Pharmacokinetics Study of Sinomenine in Rats after Oral Administration of Sinomenine Monomer and Sinomenium Acutum Extract Abstract Abstract Various products containing sinomenine monomer and extracts of Sinomenium acutum have been widely applied in clinical treatments. The goal of the present study was to ... |
PMC9230590 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution of Enavogliflozin in Mice and Rats | Pharmacokinetics and Tissue Distribution of Enavogliflozin in Mice and Rats Abstract This study investigated the pharmacokinetics and tissue distribution of enavogliflozin, a novel sodium-glucose cotransporter 2 inhibitor that is currently in phase three clinical trials. Enavogliflozin showed dose-proportional pharmaco... |
PMC12277756 | core_pubmed_pmc | A phase I study to evaluate the effect of high-dose carbidopa on levodopa pharmacokinetics | A phase I study to evaluate the effect of high-dose carbidopa on levodopa pharmacokinetics Abstract Abstract Levodopa is the gold standard treatment for Parkinson’s disease. However, a high unmet medical need exists for longer-lasting oral levodopa formulations to achieve sustained motor improvement with reduced risk o... |
PMC7446256 | core_pubmed_pmc | The PEritoneal SUrface CAlculator (PESUCA): A new tool to quantify the resected peritoneal surface area after cytoreductive surgery | The PEritoneal SUrface CAlculator (PESUCA): A new tool to quantify the resected peritoneal surface area after cytoreductive surgery Abstract Abstract Background The body surface area (BSA) is taken as a measure for the effective contact area for dosing in hyperthermic intraperitoneal chemotherapy (HIPEC). Currently, th... |
PMC9326883 | core_pubmed_pmc | Concurrent administration of anticancer chemotherapy drug and herbal medicine on the perspective of pharmacokinetics | Concurrent administration of anticancer chemotherapy drug and herbal medicine on the perspective of pharmacokinetics Abstract Abstract With an increasing number of cancer patients seeking an improved quality of life, complementary and alternative therapies are becoming more common ways to achieve such improvements. The... |
PMC7168150 | core_pubmed_pmc | The Effect of Different Antibiotic Regimens on Bacterial Resistance: A Systematic Review | The Effect of Different Antibiotic Regimens on Bacterial Resistance: A Systematic Review Abstract Abstract Background and objectives: Infections caused by resistant bacteria are a growing public health problem that is linked to many different causes, among them the antibiotics’ incorrect use plays an important role. Ac... |
PMC7296558 | core_pubmed_pmc | Scalable in silico Simulation of Transdermal Drug Permeability: Application of BIOiSIM Platform | Scalable in silico Simulation of Transdermal Drug Permeability: Application of BIOiSIM Platform Abstract Abstract Introduction Transdermal drug delivery is gaining popularity as an alternative to traditional routes of administration. It can increase patient compliance because of its painless and noninvasive nature, aid... |
PMC4791456 | core_pubmed_pmc | Impact of New Genomic Technologies on Understanding Adverse Drug Reactions | Impact of New Genomic Technologies on Understanding Adverse Drug Reactions Abstract Abstract It is well established that variations in genes can alter the pharmacokinetic and pharmacodynamic profile of a drug and immunological responses to it. Early advances in pharmacogenetics were made with traditional genetic techni... |
PMC9099467 | core_pubmed_pmc | Combining Pharmacokinetics and Vibrational Spectroscopy: MCR-ALS Hard-and-Soft Modelling of Drug Uptake In Vitro Using Tailored Kinetic Constraints | Combining Pharmacokinetics and Vibrational Spectroscopy: MCR-ALS Hard-and-Soft Modelling of Drug Uptake In Vitro Using Tailored Kinetic Constraints Abstract Abstract Raman microspectroscopy is a label-free technique which is very suited for the investigation of pharmacokinetics of cellular uptake, mechanisms of interac... |
PMC6708181 | core_pubmed_pmc | Phase I study of samalizumab in chronic lymphocytic leukemia and multiple myeloma: blockade of the immune checkpoint CD200 | Phase I study of samalizumab in chronic lymphocytic leukemia and multiple myeloma: blockade of the immune checkpoint CD200 Abstract Purpose Samalizumab is a novel recombinant humanized monoclonal antibody that targets CD200, an immunoregulatory cell surface member of the immunoglobulin superfamily that dampens excessiv... |
PMC11279950 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic Modeling and In Vitro–In Vivo Correlation of TV-46000 (Risperidone LAI): Prediction from Dog to Human | Physiologically-Based Pharmacokinetic Modeling and In Vitro–In Vivo Correlation of TV-46000 (Risperidone LAI): Prediction from Dog to Human Abstract The interest in the development and therapeutic application of long-acting injectable products for chronic or long-term treatments has experienced exponential growth in re... |
PMC12458139 | core_pubmed_pmc | A General Analytic Approach to Predicting the Best Antibiotic Dosing Regimen | A General Analytic Approach to Predicting the Best Antibiotic Dosing Regimen Abstract Determining optimal antibiotic dosing strategies is complex. Clinically, some antibiotics work best in continuous low doses, while others require high repeated pulses. However, the best approach for any antibiotic and bacterial infect... |
PMC10921134 | core_pubmed_pmc | Pharmacokinetic enhancement of marbofloxacin by alpha-1-monolaurin pre-treatment in broiler chickens | Pharmacokinetic enhancement of marbofloxacin by alpha-1-monolaurin pre-treatment in broiler chickens Abstract The present study investigated the prospect of improvement in pharmacokinetic (PK) parameters of marbofloxacin due to alpha-1-monolaurin pre-treatment in broiler chickens. Two groups of broilers were administer... |
PMC12882757 | core_pubmed_pmc | Verekitug, a Novel Antibody Antagonist to the TSLP Receptor in Adults with Asthma: A 32‐Week Randomized Phase 1b Multiple Ascending‐Dose Trial | Verekitug, a Novel Antibody Antagonist to the TSLP Receptor in Adults with Asthma: A 32‐Week Randomized Phase 1b Multiple Ascending‐Dose Trial Abstract Verekitug, a novel, high‐affinity, fully human monoclonal antibody targeting thymic stromal lymphopoietin receptor (TSLPR), is in development as a potential treatment f... |
PMC6767767 | core_pubmed_pmc | An Evidence-Based Review On The Use Of Perampanel For The Treatment Of Focal-Onset Seizures In Pediatric Patients | An Evidence-Based Review On The Use Of Perampanel For The Treatment Of Focal-Onset Seizures In Pediatric Patients Abstract Abstract Perampanel, a non-competitive AMPA receptor antagonist, is a once-daily oral antiepileptic drug approved for the treatment of focal seizures and primary generalized tonic–clonic seizures i... |
PMC9545894 | core_pubmed_pmc | A sensitive LC‐MS/MS method for quantification of phenytoin and its major metabolite with application to in vivo investigations of intravenous and intranasal phenytoin delivery | A sensitive LC‐MS/MS method for quantification of phenytoin and its major metabolite with application to in vivo investigations of intravenous and intranasal phenytoin delivery Abstract Phenytoin is a powerful antiseizure drug with complex pharmacokinetic properties, making it an interesting model drug to use in precli... |
PMC11583740 | core_pubmed_pmc | Genotype-specific effects of elamipretide in patients with primary mitochondrial myopathy: a post hoc analysis of the MMPOWER-3 trial | Genotype-specific effects of elamipretide in patients with primary mitochondrial myopathy: a post hoc analysis of the MMPOWER-3 trial Abstract Background As previously published, the MMPOWER-3 clinical trial did not demonstrate a significant benefit of elamipretide treatment in a genotypically diverse population of adu... |
PMC11603672 | core_pubmed_pmc | Characterizing the pharmacological interaction of the antimalarial combination artefenomel-piperaquine in healthy volunteers with induced blood-stage Plasmodium falciparum to predict efficacy in patients with malaria | Characterizing the pharmacological interaction of the antimalarial combination artefenomel-piperaquine in healthy volunteers with induced blood-stage Plasmodium falciparum to predict efficacy in patients with malaria Abstract Background The combination antimalarial artefenomel-piperaquine failed to achieve target effic... |
PMC10583250 | core_pubmed_pmc | Optimized infusion rates for N,N‐dimethyltryptamine to achieve a target psychedelic intensity based on a modeling and simulation framework | Optimized infusion rates for N,N‐dimethyltryptamine to achieve a target psychedelic intensity based on a modeling and simulation framework Abstract Abstract N,N‐dimethyltryptamine (DMT) is a psychedelic compound that is being studied as a therapeutic option in various psychiatric disorders. Due to its short half‐life, ... |
PMC8246819 | core_pubmed_pmc | Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants | Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants Abstract Abstract Macimorelin is an orally active growth hormone secretagogue indicated for the diagnosis of adult growth hormone deficiency. The primary objective of this study was to evaluate the effect of ... |
PMC7560225 | core_pubmed_pmc | Population Pharmacokinetics of Continuous-Infusion Meropenem in Febrile Neutropenic Patients with Hematologic Malignancies: Dosing Strategies for Optimizing Empirical Treatment against Enterobacterales and P. aeruginosa | Population Pharmacokinetics of Continuous-Infusion Meropenem in Febrile Neutropenic Patients with Hematologic Malignancies: Dosing Strategies for Optimizing Empirical Treatment against Enterobacterales and P. aeruginosa Abstract Abstract A population pharmacokinetic analysis of continuous infusion (CI) meropenem was co... |
PMC6958509 | core_pubmed_pmc | Anticancer Ruthenium(III) Complexes and Ru(III)-Containing Nanoformulations: An Update on the Mechanism of Action and Biological Activity | Anticancer Ruthenium(III) Complexes and Ru(III)-Containing Nanoformulations: An Update on the Mechanism of Action and Biological Activity Abstract The great advances in the studies on metal complexes for the treatment of different cancer forms, starting from the pioneering works on platinum derivatives, have fostered a... |
PMC10795579 | core_pubmed_pmc | Macrophage metallothioneins participate in the antileishmanial activity of antimonials | Macrophage metallothioneins participate in the antileishmanial activity of antimonials Abstract Host cell functions that participate in the pharmacokinetics and pharmacodynamics (PK/PD) of drugs against intracellular pathogen infections are critical for drug efficacy. In this study, we investigated whether macrophage m... |
PMC5914156 | core_pubmed_pmc | Pharmacokinetics of immediate release, extended release, and gastric retentive gabapentin formulations in healthy adults | Pharmacokinetics of immediate release, extended release, and gastric retentive gabapentin formulations in healthy adults Abstract Objective: Gabapentin immediate release (GBP-IR), gabapentin gastric retentive (GBP-GR), and the prodrug gabapentin enacarbil extended release formulation (GEn) have been approved for manage... |
PMC4553980 | core_pubmed_pmc | Persistent Staphylococcus aureus Bacteremia | Persistent Staphylococcus aureus Bacteremia Abstract Abstract Persistent Staphylococcus aureus bacteremia (SAB) that fails to respond to appropriate antibiotic therapy is associated with poor outcomes. Comprehensive prospective studies on risk factors and outcomes of persistent bacteremia are limited. We investigated o... |
PMC10708275 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution and Excretion of Demethyleneberberine, a Metabolite of Berberine, in Rats and Mice | Pharmacokinetics, Tissue Distribution and Excretion of Demethyleneberberine, a Metabolite of Berberine, in Rats and Mice Abstract Abstract Demethyleneberberine is an active component extracted from the Chinese herbal drug Cortex Phellodendri. It is also a metabolite of berberine in animals and humans. However, the phar... |
PMC11246403 | core_pubmed_pmc | Pre-Clinical Studies of a Novel Bispecific Fusion Protein Targeting C3b and VEGF in Neovascular and Nonexudative AMD Models | Pre-Clinical Studies of a Novel Bispecific Fusion Protein Targeting C3b and VEGF in Neovascular and Nonexudative AMD Models Abstract Introduction KNP-301 is a bi-specific fragment crystallizable region (Fc) fusion protein, which inhibits both C3b and vascular endothelial growth factor (VEGF) simultaneously for patients... |
PMC5754413 | core_pubmed_pmc | Mass balance, metabolic disposition, and pharmacokinetics of a single oral dose of regorafenib in healthy human subjects | Mass balance, metabolic disposition, and pharmacokinetics of a single oral dose of regorafenib in healthy human subjects Abstract Abstract Purpose To evaluate the mass balance, metabolic disposition, and pharmacokinetics of a single dose of regorafenib in healthy volunteers. In addition, in vitro metabolism of regorafe... |
PMC12485673 | core_pubmed_pmc | Structure-Guided Development of a Potent BioA Inhibitor Validates Biotin Synthesis Inhibition as a Therapeutic Strategy for Tuberculosis | Structure-Guided Development of a Potent BioA Inhibitor Validates Biotin Synthesis Inhibition as a Therapeutic Strategy for Tuberculosis Abstract Structure-guided optimization was applied to develop a potent and selective inhibitor of the aminotransferase BioA, a key enzyme in bacterial biotin biosynthesis. Strategic m... |
PMC10564155 | core_pubmed_pmc | Association of smoking cigarettes, age, and sex with serum concentrations of olanzapine in patients with schizophrenia | Association of smoking cigarettes, age, and sex with serum concentrations of olanzapine in patients with schizophrenia Abstract Introduction Olanzapine is an atypical antipsychotic drug which is effective in the treatment of schizophrenia. Cigarette smoking, age, and sex could be related to the pharmacokinetics and ser... |
PMC11919382 | core_pubmed_pmc | Development of an oral regimen of unithiol for the treatment of snakebite envenoming: a phase 1 open-label dose-escalation safety trial and pharmacokinetic analysis in healthy Kenyan adults | Development of an oral regimen of unithiol for the treatment of snakebite envenoming: a phase 1 open-label dose-escalation safety trial and pharmacokinetic analysis in healthy Kenyan adults Abstract Summary Background Viperidae snakes are responsible for many of the 94,000 deaths caused by snakebite envenoming each yea... |
PMC3485666 | core_pubmed_pmc | The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate | The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate Abstract BACKGROUND AND PURPOSE BAF312 is a next-generation sphingosine 1-phosphate (S1P) receptor modulator, selective for S1P 1 and S1P 5 receptors. S1P 1 receptors are esse... |
PMC5167316 | core_pubmed_pmc | Phase I/II Trial of Sorafenib in Combination with Vinorelbine as First-Line Chemotherapy for Metastatic Breast Cancer | Phase I/II Trial of Sorafenib in Combination with Vinorelbine as First-Line Chemotherapy for Metastatic Breast Cancer Abstract Background Preclinical models have reported a synergistic interaction between sorafenib and vinorelbine. We investigated the toxicity, efficacy, and pharmacokinetics interaction of this combina... |
PMC5761005 | core_pubmed_pmc | Pharmacokinetic study of inosiplex tablets in healthy Chinese volunteers by hyphenated HPLC and tandem MS techniques | Pharmacokinetic study of inosiplex tablets in healthy Chinese volunteers by hyphenated HPLC and tandem MS techniques Abstract Abstract Inosiplex is a compound formulation composed of inosine and p-acetaminobenzoic acid (PABA) salt of N,N-dimethylamino-2-propanol (DIP). This study was to investigate the clinical plasma ... |
PMC5638427 | core_pubmed_pmc | Formulation and pharmacology of long-acting cabotegravir | Formulation and pharmacology of long-acting cabotegravir Abstract Abstract Purpose of review Long-acting cabotegravir may provide a novel therapeutic option for both the treatment and prevention of HIV-1 infection that does not necessitate adherence to a daily regimen. The present review will highlight the unique formu... |
PMC12730968 | core_pubmed_pmc | Integrating New Approach Methodologies (NAMs) into Preclinical Regulatory Evaluation of Oncology Drugs | Integrating New Approach Methodologies (NAMs) into Preclinical Regulatory Evaluation of Oncology Drugs Abstract Abstract Traditional animal-based preclinical models, including xenografts and genetically engineered mice, have been used for assessing pharmacodynamics, toxicity, efficacy, and safety for decades. Despite t... |
PMC6921215 | core_pubmed_pmc | Targeting Repeated Regions Unique to a Gene Is an Effective Strategy for Discovering Potent and Efficacious Antisense Oligonucleotides | Targeting Repeated Regions Unique to a Gene Is an Effective Strategy for Discovering Potent and Efficacious Antisense Oligonucleotides Abstract Abstract Well-validated strategies for discovering potent and efficacious antisense oligonucleotides are central to realize the full therapeutic potential of RNA therapy. In th... |
PMC10117888 | core_pubmed_pmc | Evaluation of the drug-drug interaction potential of the novel hepatitis B and D virus entry inhibitor bulevirtide at OATP1B in healthy volunteers | Evaluation of the drug-drug interaction potential of the novel hepatitis B and D virus entry inhibitor bulevirtide at OATP1B in healthy volunteers Abstract Introduction: Bulevirtide is a first-in-class antiviral drug to treat chronic hepatitis B/D. We investigated the drug-drug interaction potential and pharmacokinetic... |
PMC11110266 | core_pubmed_pmc | Evaluation of Apixaban standard dosing in underweight patients with non-valvular atrial fibrillation: a retrospective cohort study | Evaluation of Apixaban standard dosing in underweight patients with non-valvular atrial fibrillation: a retrospective cohort study Abstract Background Recent guidelines recommend using direct oral anticoagulants (DOACs) as first-line agents in patients with non-valvular atrial fibrillation (NVAF). Research is currently... |
PMC5907193 | core_pubmed_pmc | Comparison of electroencephalographic changes in response to acute electrical and thermal stimuli with the tail flick and hot plate test in rats administered with opiorphin | Comparison of electroencephalographic changes in response to acute electrical and thermal stimuli with the tail flick and hot plate test in rats administered with opiorphin Abstract Background The objective of this study was to compare the changes in the electroencephalogram (EEG) in response to noxious stimuli with ta... |
PMC8975668 | core_pubmed_pmc | Preparation and Safety Evaluation of Centella asiatica Total Glycosides Nitric Oxide Gel and Its Therapeutic Effect on Diabetic Cutaneous Ulcers | Preparation and Safety Evaluation of Centella asiatica Total Glycosides Nitric Oxide Gel and Its Therapeutic Effect on Diabetic Cutaneous Ulcers Abstract Abstract Diabetic cutaneous ulcers (DCU) are a chronic and refractory complication of diabetes mellitus, which can lead to amputation or even death in extreme cases. ... |
PMC7689899 | core_pubmed_pmc | Cannabidiol efficacy independent of clobazam: Meta‐analysis of four randomized controlled trials | Cannabidiol efficacy independent of clobazam: Meta‐analysis of four randomized controlled trials Abstract Abstract Objective The efficacy of cannabidiol (CBD) with and without concomitant clobazam (CLB) was evaluated in stratified analyses of four large randomized controlled trials, two in Lennox‐Gastaut syndrome, and ... |
PMC11357484 | core_pubmed_pmc | Investigating Changes in Pharmacokinetics of Steroidal Alkaloids from a Hydroethanolic Fritillariae thunbergii Bulbus Extract in 2,4-Dinitrobenzene Sulfonic Acid-Induced Colitis Rats | Investigating Changes in Pharmacokinetics of Steroidal Alkaloids from a Hydroethanolic Fritillariae thunbergii Bulbus Extract in 2,4-Dinitrobenzene Sulfonic Acid-Induced Colitis Rats Abstract Fritillariae thunbergii Bulbus (FTB), a member of the Liliaceae family, has a long history of use in many herbal formulations fo... |
PMC8374393 | core_pubmed_pmc | Complete preclinical platform for intravitreal chemotherapy drug discovery for retinoblastoma: Assessment of pharmacokinetics, toxicity and efficacy using a rabbit model | Complete preclinical platform for intravitreal chemotherapy drug discovery for retinoblastoma: Assessment of pharmacokinetics, toxicity and efficacy using a rabbit model Abstract Abstract Current melphalan-based intravitreal chemotherapy regimens for retinoblastoma vitreous seeds are effective, but cause significant oc... |
PMC12799528 | core_pubmed_pmc | Characterization of fecal deglucuronidation activity in healthy subjects and in patients treated with fecal microbiota transplantation | Characterization of fecal deglucuronidation activity in healthy subjects and in patients treated with fecal microbiota transplantation Abstract Abstract Gut bacterial β -glucuronidase (GUS) enzymes contribute to the intestinal toxicity and/or enterohepatic recycling of glucuronidated compounds by cleaving glucuronide c... |
PMC6631517 | core_pubmed_pmc | Novel Amphiphilic Cyclobutene and Cyclobutane cis -C 18 Fatty Acid Derivatives Inhibit Mycobacterium avium subsp. paratuberculosis Growth | Novel Amphiphilic Cyclobutene and Cyclobutane cis -C 18 Fatty Acid Derivatives Inhibit Mycobacterium avium subsp. paratuberculosis Growth Abstract Mycobacterium avium subspecies paratuberculosis (Map) is the etiologic agent of Johne’s disease in ruminants and has been associated with Crohn’s disease in humans. An effec... |
PMC10600059 | core_pubmed_pmc | Targeting Dalbavancin Inoculum Effect: Adjunctive Single Dose of Daptomycin | Targeting Dalbavancin Inoculum Effect: Adjunctive Single Dose of Daptomycin Abstract Introduction Daptomycin (DAP) has proven to be a viable alternative amid vancomycin resistance; however, the use of DAP post vancomycin treatment has led to the development of DAP non-susceptible (DNS) strains. Dalbavancin (DAL), a nov... |
PMC10506772 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of JNJ-1802, a Pan-serotype Dengue Direct Antiviral Small Molecule, in a Phase 1, Double-Blind, Randomized, Dose-Escalation Study in Healthy Volunteers | Safety, Tolerability, and Pharmacokinetics of JNJ-1802, a Pan-serotype Dengue Direct Antiviral Small Molecule, in a Phase 1, Double-Blind, Randomized, Dose-Escalation Study in Healthy Volunteers Abstract Abstract Background Dengue is a growing global health threat with no specific antiviral drugs available for treatmen... |
PMC12654983 | core_pubmed_pmc | Is Fentanyl Rebound an Intrinsic Feature of Naloxone Reversal? | Is Fentanyl Rebound an Intrinsic Feature of Naloxone Reversal? Abstract Abstract Background/Objectives : The drug development response to the unique pharmacology of fentanyl, which drives the current opioid epidemic, has primarily focused on increasing naloxone doses and employing longer-acting antidotes. While having ... |
PMC11359093 | core_pubmed_pmc | MB09, a denosumab biosimilar candidate: Biosimilarity demonstration in a phase I study in healthy subjects | MB09, a denosumab biosimilar candidate: Biosimilarity demonstration in a phase I study in healthy subjects Abstract Abstract This was a Phase I, randomized, double‐blinded, three‐arm, single‐dose, parallel study aimed to demonstrate pharmacokinetic (PK) similarity between MB09 (a denosumab biosimilar candidate) and ref... |
PMC9744694 | core_pubmed_pmc | Evaluating Islatravir Administered Via Microneedle Array Patch for Long-Acting HIV Pre-exposure Prophylaxis Using Physiologically Based Pharmacokinetic Modelling | Evaluating Islatravir Administered Via Microneedle Array Patch for Long-Acting HIV Pre-exposure Prophylaxis Using Physiologically Based Pharmacokinetic Modelling Abstract Abstract Background and Objectives Technologies for long-acting administration of antiretrovirals (ARVs) for the prevention and treatment of HIV are ... |
PMC8474375 | core_pubmed_pmc | Daratumumab Plus Atezolizumab in Previously Treated Advanced or Metastatic NSCLC: Brief Report on a Randomized, Open-Label, Phase 1b/2 Study (LUC2001 JNJ-54767414) | Daratumumab Plus Atezolizumab in Previously Treated Advanced or Metastatic NSCLC: Brief Report on a Randomized, Open-Label, Phase 1b/2 Study (LUC2001 JNJ-54767414) Abstract Abstract Introduction The programmed death-ligand 1 inhibitor atezolizumab improves progression-free survival (PFS) and overall survival (OS) for p... |
PMC10140824 | core_pubmed_pmc | Estimation of Pediatric Dosage of Antimalarial Drugs, Using Pharmacokinetic and Physiological Approach | Estimation of Pediatric Dosage of Antimalarial Drugs, Using Pharmacokinetic and Physiological Approach Abstract Most of the individuals who die of malaria in sub–Saharan Africa are children. It is, therefore, important for this age group to have access to the right treatment and correct dose. Artemether—lumefantrine is... |
PMC12866164 | core_pubmed_pmc | DF6215, an α-optimized IL-2-Fc fusion, expands immune effectors and drives robust preclinical anti-tumor activity | DF6215, an α-optimized IL-2-Fc fusion, expands immune effectors and drives robust preclinical anti-tumor activity Abstract Summary DF6215 is a rationally engineered interleukin-2 (IL-2) Fc-fusion protein developed to overcome efficacy and safety limitations of traditional IL-2 cancer immunotherapy. Unlike non-alpha (no... |
PMC11875147 | core_pubmed_pmc | Predicting tuberculosis drug efficacy in preclinical and clinical models from in vitro data | Predicting tuberculosis drug efficacy in preclinical and clinical models from in vitro data Abstract Summary Multiple in vitro potency assays are used to evaluate compounds against Mycobacterium tuberculosis , but a consensus on clinically relevant assays is lacking. We aimed to identify an in vitro assay signature tha... |
PMC3880288 | core_pubmed_pmc | Computational Modeling of 3D Tumor Growth and Angiogenesis for Chemotherapy Evaluation | Computational Modeling of 3D Tumor Growth and Angiogenesis for Chemotherapy Evaluation Abstract Abstract Solid tumors develop abnormally at spatial and temporal scales, giving rise to biophysical barriers that impact anti-tumor chemotherapy. This may increase the expenditure and time for conventional drug pharmacokinet... |
PMC12295472 | core_pubmed_pmc | Current Challenges in the Treatment of Invasive Aspergillosis in Geriatric Patients | Current Challenges in the Treatment of Invasive Aspergillosis in Geriatric Patients Abstract Background: Invasive aspergillosis (IA) is a severe fungal infection increasingly affecting elderly patients with chronic respiratory diseases and prolonged corticosteroid use. Methods: We evaluated clinical, biochemical, and f... |
PMC12823321 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling of the PARP Inhibitor Niraparib | Physiologically‐Based Pharmacokinetic Modeling of the PARP Inhibitor Niraparib Abstract ABSTRACT A physiologically‐based pharmacokinetic (PBPK) model of niraparib and its primary metabolite using a relevant virtual cancer population is reported here. A series of in vitro experiments using liver S9, microsomes, and hepa... |
PMC12011715 | core_pubmed_pmc | Regulatory mechanism of ABCB1 transcriptional repression by HDAC5 in rat hepatocytes under hypoxic environment | Regulatory mechanism of ABCB1 transcriptional repression by HDAC5 in rat hepatocytes under hypoxic environment Abstract Abstract Objective Previous research has demonstrated that the hypoxic environment at high altitudes significantly alters the pharmacokinetics of many drugs, reducing their efficacy and increasing adv... |
PMC11092382 | core_pubmed_pmc | A review on the pharmacology, pharmacokinetics and toxicity of sophocarpine | A review on the pharmacology, pharmacokinetics and toxicity of sophocarpine Abstract Abstract Sophocarpine is a natural compound that belongs to the quinolizidine alkaloid family, and has a long history of use and widespread distribution in traditional Chinese herbal medicines such as Sophora alopecuroides L., Sophora ... |
PMC12714856 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model for the Prediction of Plasma and Bone Tissue Exposure after Prophylactic Administration of Ampicillin/Sulbactam in Patients with Osteonecrosis of the Jaw | A Physiologically Based Pharmacokinetic Model for the Prediction of Plasma and Bone Tissue Exposure after Prophylactic Administration of Ampicillin/Sulbactam in Patients with Osteonecrosis of the Jaw Abstract Abstract Background and Objective The combination of ampicillin (AMP) together with sulbactam (SBC) is a widely... |
PMC7179297 | core_pubmed_pmc | Preclinical Antimalarial Combination Study of M5717, a Plasmodium falciparum Elongation Factor 2 Inhibitor, and Pyronaridine, a Hemozoin Formation Inhibitor | Preclinical Antimalarial Combination Study of M5717, a Plasmodium falciparum Elongation Factor 2 Inhibitor, and Pyronaridine, a Hemozoin Formation Inhibitor Abstract Antimalarial drug resistance in the Plasmodium falciparum parasite poses a constant challenge for drug development. To mitigate this risk, new antimalaria... |
PMC6283801 | core_pubmed_pmc | Dibenzazepine Agents in Epilepsy: How Does Eslicarbazepine Acetate Differ? | Dibenzazepine Agents in Epilepsy: How Does Eslicarbazepine Acetate Differ? Abstract Abstract Carbamazepine (CBZ), oxcarbazepine (OXC), and eslicarbazepine acetate (ESL) belong to the dibenzazepine family of antiepileptic drugs and are all thought to primarily act as sodium channel blockers (SCBs). However, ESL is struc... |
PMC9051541 | core_pubmed_pmc | Design, in silico studies, and synthesis of new 1,8-naphthyridine-3-carboxylic acid analogues and evaluation of their H1R antagonism effects † | Design, in silico studies, and synthesis of new 1,8-naphthyridine-3-carboxylic acid analogues and evaluation of their H1R antagonism effects † Abstract New 1,8-naphthyridine-3-carboxylic acid derivatives were designed, synthesized and evaluated for their in vivo antihistaminic activity on guinea pig trachea by using ch... |
PMC7070302 | core_pubmed_pmc | Measuring Sulforaphane and Its Metabolites in Human Plasma: A High Throughput Method | Measuring Sulforaphane and Its Metabolites in Human Plasma: A High Throughput Method Abstract (1) Background: There is increasing understanding of the potential health benefits of cruciferous vegetables. In particular sulforaphane (SFN), found in broccoli, and its metabolites sulforaphane-glutathione (SFN-GSH), sulfora... |
PMC8646198 | core_pubmed_pmc | The influence of excessive consumption of liquorice on phenprocoumon (Marcumar®): a case report | The influence of excessive consumption of liquorice on phenprocoumon (Marcumar®): a case report Abstract Abstract Here, the case of a 92-year-old female patient, who was diagnosed with atrial fibrillation and treated with phenprocoumon (Marcumar®), is reported. Pre-existing comorbidities were arterial hypertension, cor... |
PMC12664837 | core_pubmed_pmc | A review: advances of resveratrol co-delivery biomaterials-based system in anti-tumor therapy | A review: advances of resveratrol co-delivery biomaterials-based system in anti-tumor therapy Abstract Resveratrol (3,5,4′-trihydroxy-trans-stilbene), a natural polyphenol, has garnered significant attention in oncology for its multifaceted antitumor mechanisms, including apoptosis induction, angiogenesis suppression, ... |
PMC5821365 | core_pubmed_pmc | Population nutrikinetics of green tea extract | Population nutrikinetics of green tea extract Abstract Green tea polyphenols may contribute to the prevention of cancer and other diseases. To learn more about the pharmacokinetics and interindividual variation of green tea polyphenols after oral intake in humans we performed a population nutrikinetic study of standard... |
PMC8837058 | core_pubmed_pmc | Combination of CLEC4M rs868875 G-Carriership and ABO O Genotypes May Predict Faster Decay of FVIII Infused in Hemophilia A Patients | Combination of CLEC4M rs868875 G-Carriership and ABO O Genotypes May Predict Faster Decay of FVIII Infused in Hemophilia A Patients Abstract Abstract The C-type lectin CLEC4M binds and internalizes factor VIII (FVIII). Common CLEC4M variants have been associated with FVIII pharmacokinetic (PK) profiles in hemophilia A ... |
PMC12195914 | core_pubmed_pmc | A Review on New Frontiers in Drug-Drug Interaction Predictions and Safety Evaluations with In Vitro Cellular Models | A Review on New Frontiers in Drug-Drug Interaction Predictions and Safety Evaluations with In Vitro Cellular Models Abstract Abstract The characterization of a drug’s ADME (absorption, distribution, metabolism, and excretion) profile is crucial for accurately determining its safety and efficacy. The rising prevalence o... |
PMC11992656 | core_pubmed_pmc | Use of population pharmacokinetic‐pharmacodynamic modelling to inform antimalarial dose optimization in infants | Use of population pharmacokinetic‐pharmacodynamic modelling to inform antimalarial dose optimization in infants Abstract Abstract Infants bear a significant malaria burden but are usually excluded from participating in early dose optimization studies that inform dosing regimens of antimalarial therapy. Unlike older chi... |
PMC11927960 | core_pubmed_pmc | Multiparameter ranking of carbazoles for anti-trypanosome lead discovery | Multiparameter ranking of carbazoles for anti-trypanosome lead discovery Abstract Abstract The criteria for the progression of hits in the discovery of leads for human African trypanosomiasis (HAT), a neglected disease caused by the microbial eukaryote Trypanosoma brucei , are not standardized. Hits are advanced upon m... |
PMC8294601 | core_pubmed_pmc | Pharmacokinetics of enoxaparin in COVID-19 critically ill patients | Pharmacokinetics of enoxaparin in COVID-19 critically ill patients Abstract Abstract Background In intensive-care unit (ICU) patients, pathophysiological changes may affect the pharmacokinetics of enoxaparin and result in underdosing. Objectives To develop a pharmacokinetic model of enoxaparin to predict the time-expos... |
PMC9076297 | core_pubmed_pmc | Intermittent Hypoxia Inhibits Hepatic CYP1a2 Expression and Delays Aminophylline Metabolism | Intermittent Hypoxia Inhibits Hepatic CYP1a2 Expression and Delays Aminophylline Metabolism Abstract Abstract Purpose In this study, we aimed to determine the effects of intermittent hypoxia (IH) on hepatic cytochrome P450 1A2 (CYP1A2) expression and the pharmacokinetics of CYP1A2-mediated aminophylline and warfarin in... |
PMC6422671 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and effect on serum uric acid of the myeloperoxidase inhibitor AZD4831 in a randomized, placebo‐controlled, phase I study in healthy volunteers | Safety, tolerability, pharmacokinetics and effect on serum uric acid of the myeloperoxidase inhibitor AZD4831 in a randomized, placebo‐controlled, phase I study in healthy volunteers Abstract Abstract Aims Myeloperoxidase activity can contribute to impaired vascular endothelial function and fibrosis in chronic inflamma... |
PMC8878013 | core_pubmed_pmc | Circumventing Doxorubicin Resistance Using Elastin-like Polypeptide Biopolymer-Mediated Drug Delivery | Circumventing Doxorubicin Resistance Using Elastin-like Polypeptide Biopolymer-Mediated Drug Delivery Abstract Although doxorubicin (dox), an anthracycline antibiotic, is widely used and effective in treating cancer, its treatment efficiency is limited by low blood plasma solubility, poor pharmacokinetics, and adverse ... |
PMC11288853 | core_pubmed_pmc | Identifying plant-derived antiviral alkaloids as dual inhibitors of SARS-CoV-2 main protease and spike glycoprotein through computational screening | Identifying plant-derived antiviral alkaloids as dual inhibitors of SARS-CoV-2 main protease and spike glycoprotein through computational screening Abstract COVID-19 is currently considered the ninth-deadliest pandemic, spreading through direct or indirect contact with infected individuals. It has imposed a consistent ... |
PMC12966353 | core_pubmed_pmc | Extended absorption, implications: Rethinking alcohol pharmacokinetics in forensic calculations | Extended absorption, implications: Rethinking alcohol pharmacokinetics in forensic calculations Abstract Forensic toxicologists routinely perform pharmacokinetic calculations for alcohol, such as retrograde extrapolation calculations that rely on assumptions about when alcohol absorption is complete. However, examinati... |
PMC12000915 | core_pubmed_pmc | Transferrin and Borneol-Enhanced Liposomes for Targeted Rapamycin Delivery in TBI | Transferrin and Borneol-Enhanced Liposomes for Targeted Rapamycin Delivery in TBI Abstract Background The therapeutic potential of rapamycin (RAPA) for traumatic brain injury (TBI) is limited by its low bioavailability and poor penetration across the blood-brain barrier (BBB). We developed transferrin-modified rapamyci... |
PMC8607802 | core_pubmed_pmc | Computational Pharmacokinetics Report, ADMET Study and Conceptual DFT‐Based Estimation of the Chemical Reactivity Properties of Marine Cyclopeptides | Computational Pharmacokinetics Report, ADMET Study and Conceptual DFT‐Based Estimation of the Chemical Reactivity Properties of Marine Cyclopeptides Abstract Abstract Homophymines A–E and A1–E1 are bioactive natural cyclodepsipeptides with a complex molecular architecture. These molecules could have a potential use as ... |
PMC11301252 | core_pubmed_pmc | Ivermectin therapy for young children with scabies infection: a multicentre phase 2 non-randomized trial | Ivermectin therapy for young children with scabies infection: a multicentre phase 2 non-randomized trial Abstract Summary Background Ivermectin, an effective treatment for scabies, is not licensed for children weighing <15 kg. Pharmacokinetic modelling has shown a 3 mg dose in young children (2–4 years, weighing 10–14 ... |
PMC12310023 | core_pubmed_pmc | Anti- Cryptosporidium efficacy of BKI-1708, an inhibitor of Cryptosporidium calcium-dependent protein kinase 1 | Anti- Cryptosporidium efficacy of BKI-1708, an inhibitor of Cryptosporidium calcium-dependent protein kinase 1 Abstract Abstract Background Diarrheal pathogens, such as Cryptosporidium, impose a heavy burden of disease in resource-limited regions. Cryptosporidiosis often causes chronic infection in immunocompromised pe... |
PMC12479678 | core_pubmed_pmc | Challenging Traditional ADME Assumptions for Physiologically Based Pharmacokinetic Models for Intravenous Administration of Iron–Carbohydrate Nanomedicines: Potential Utility of Gold Nanoparticle Models as a Roadmap | Challenging Traditional ADME Assumptions for Physiologically Based Pharmacokinetic Models for Intravenous Administration of Iron–Carbohydrate Nanomedicines: Potential Utility of Gold Nanoparticle Models as a Roadmap Abstract Abstract Intravenous iron–carbohydrate complexes are a class of nanomedicines that are widely u... |
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