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PMC6590358
core_pubmed_pmc
Systemic Tofacitinib Concentrations in Adult Patients With Atopic Dermatitis Treated With 2% Tofacitinib Ointment and Application to Pediatric Study Planning
Systemic Tofacitinib Concentrations in Adult Patients With Atopic Dermatitis Treated With 2% Tofacitinib Ointment and Application to Pediatric Study Planning Abstract Abstract Atopic dermatitis is a chronic eczematous, pruritic, inflammatory skin condition affecting children and adults. Tofacitinib is a Janus kinase in...
PMC10974694
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of anti‐IL‐4Rα antibody SHR ‐1819 in healthy subjects: A randomized, controlled phase I study
Safety, pharmacokinetics, and pharmacodynamics of anti‐IL‐4Rα antibody SHR ‐1819 in healthy subjects: A randomized, controlled phase I study Abstract Abstract SHR‐1819 is a novel anti‐IL‐4Rα monoclonal antibody currently under clinical development for use in patients with type 2 inflammatory diseases. In this randomize...
PMC9469698
core_pubmed_pmc
A population PK–PD model of YH4808, a novel P‐CAB, and intragastric pH that incorporated negative feedback by increased intragastric pH onto the systemic exposure to YH4808
A population PK–PD model of YH4808, a novel P‐CAB, and intragastric pH that incorporated negative feedback by increased intragastric pH onto the systemic exposure to YH4808 Abstract Abstract YH4808 is a novel potassium‐competitive acid blocker that is under clinical development to treat patients with gastroesophageal r...
PMC10145512
core_pubmed_pmc
A Systematic Review of Clinical Pharmacokinetics of Inhaled Antiviral
A Systematic Review of Clinical Pharmacokinetics of Inhaled Antiviral Abstract Abstract Background and Objectives : The study of clinical pharmacokinetics of inhaled antivirals is particularly important as it helps one to understand the therapeutic efficacy of these drugs and how best to use them in the treatment of re...
PMC9219807
core_pubmed_pmc
A Simple Method for the Prediction of Human Concentration–Time Profiles and Pharmacokinetics of Antibody–Drug Conjugates (ADC) from Rats or Monkeys
A Simple Method for the Prediction of Human Concentration–Time Profiles and Pharmacokinetics of Antibody–Drug Conjugates (ADC) from Rats or Monkeys Abstract Abstract Knowledge of human concentration–time profiles from animal data can be useful during early drug development. The objective of this study is to predict hum...
PMC8377511
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of RT234 (Vardenafil Inhalation Powder): A First-in-Human, Ascending Single- and Multiple-Dose Study in Healthy Subjects
Safety, Tolerability, and Pharmacokinetics of RT234 (Vardenafil Inhalation Powder): A First-in-Human, Ascending Single- and Multiple-Dose Study in Healthy Subjects Abstract Background: RT234 (vardenafil inhalation powder) is being developed for pulmonary administration “as needed”, to acutely improve exercise tolerance...
PMC7036132
core_pubmed_pmc
Effects of the Salt-Processing Method on the Pharmacokinetics and Tissue Distribution of Orally Administered Morinda officinalis How. Extract
Effects of the Salt-Processing Method on the Pharmacokinetics and Tissue Distribution of Orally Administered Morinda officinalis How. Extract Abstract Abstract Salt processing, which involves steaming with salt water, directs herbs into the kidney channel. After being salt processed, kidney invigorating effects occur. ...
PMC9965536
core_pubmed_pmc
Integrating In Vitro Biopharmaceutics into Physiologically Based Biopharmaceutic Model (PBBM) to Predict Food Effect of BCS IV Zwitterionic Drug (GSK3640254)
Integrating In Vitro Biopharmaceutics into Physiologically Based Biopharmaceutic Model (PBBM) to Predict Food Effect of BCS IV Zwitterionic Drug (GSK3640254) Abstract Abstract A strategy followed to integrate in vitro solubility and permeability data into a PBBM model to predict the food effect of a BCS IV zwitterionic...
PMC4460031
core_pubmed_pmc
Nevirapine Concentration in Hair Samples Is a Strong Predictor of Virologic Suppression in a Prospective Cohort of HIV-Infected Patients
Nevirapine Concentration in Hair Samples Is a Strong Predictor of Virologic Suppression in a Prospective Cohort of HIV-Infected Patients Abstract Effective antiretroviral (ARV) therapy depends on adequate drug exposure, yet methods to assess ARV exposure are limited. Concentrations of ARV in hair are the product of ste...
PMC3728816
core_pubmed_pmc
Vasopressin vs Terlipressin in Treatment of Refractory Shock
Vasopressin vs Terlipressin in Treatment of Refractory Shock Abstract Arginine vasopressin (AVP) and its synthetic, long-acting analog terlipressin (TP) are potent alternative vasoconstrictors in the treatment of septic patients with catecholamine-refractive vasodilatatory shock. Recent clinical data suggest that early...
PMC4531525
core_pubmed_pmc
Pharmacokinetics of fluticasone furoate, umeclidinium, and vilanterol as a triple therapy in healthy volunteers
Pharmacokinetics of fluticasone furoate, umeclidinium, and vilanterol as a triple therapy in healthy volunteers Abstract Abstract Objective: Two single-center, four-way, single-dose, crossover studies assessed the systemic exposure, systemic pharmacodynamics (PD), and safety profile of the closed triple fluticasone fur...
PMC12660201
core_pubmed_pmc
Morusin as a drug candidate: opportunities, limitations, and the path toward clinical translation
Morusin as a drug candidate: opportunities, limitations, and the path toward clinical translation Abstract Prenylflavonoids are widespread in plants, which are considered valuable sources of natural polyphenolic compounds with isoprenyl groups, including flavones, flavanones, chalcones and aurones. Among the notable pr...
PMC10943695
core_pubmed_pmc
Neutrophil elastase as a versatile cleavage enzyme for activation of αvβ3 integrin-targeted small molecule drug conjugates with different payload classes in the tumor microenvironment
Neutrophil elastase as a versatile cleavage enzyme for activation of αvβ3 integrin-targeted small molecule drug conjugates with different payload classes in the tumor microenvironment Abstract Abstract Introduction: The development of bioconjugates for the targeted delivery of anticancer agents is gaining momentum afte...
PMC11662891
core_pubmed_pmc
Retention of indoxyl sulfate in different genotypes of ABCC2 may explain variation in tacrolimus pharmacokinetics
Retention of indoxyl sulfate in different genotypes of ABCC2 may explain variation in tacrolimus pharmacokinetics Abstract Abstract Background Microbiota-derived toxins indoxyl sulfate and hippuric acid were previously reported to be associated with altered pharmacokinetics of the immunosuppressant tacrolimus in liver ...
PMC10005075
core_pubmed_pmc
Study on Absorption, Distribution and Excretion of a New Candidate Compound XYY-CP1106 against Alzheimer’s Disease in Rats by LC-MS/MS
Study on Absorption, Distribution and Excretion of a New Candidate Compound XYY-CP1106 against Alzheimer’s Disease in Rats by LC-MS/MS Abstract XYY-CP1106, a candidate compound synthesized from a hybrid of hydroxypyridinone and coumarin, has been shown to be remarkably effective in treating Alzheimer’s disease. A simpl...
PMC7902330
core_pubmed_pmc
Pharmacokinetic study of traditional Japanese Kampo medicine shimotsuto used to treat gynecological diseases in rats
Pharmacokinetic study of traditional Japanese Kampo medicine shimotsuto used to treat gynecological diseases in rats Abstract Abstract Shimotsuto is a traditional Japanese Kampo medicine used to treat gynecological diseases, such as irregular menstruation, in addition to oversensitivity to cold and chilblains. Part of ...
PMC9772935
core_pubmed_pmc
Clinical Impact of Melphalan Pharmacokinetics on Transplantation Outcomes in Children Undergoing Hematopoietic Stem Cell Transplantation
Clinical Impact of Melphalan Pharmacokinetics on Transplantation Outcomes in Children Undergoing Hematopoietic Stem Cell Transplantation Abstract Melphalan is widely used for hematopoietic stem cell transplantation (HSCT) conditioning. However, the relationship between its pharmacokinetic (PK) and transplantation outco...
PMC3857037
core_pubmed_pmc
Factors and Mechanisms for Pharmacokinetic Differences between Pediatric Population and Adults
Factors and Mechanisms for Pharmacokinetic Differences between Pediatric Population and Adults Abstract Abstract Many physiologic differences between children and adults may result in age-related changes in pharmacokinetics and pharmacodynamics. Factors such as gastric pH and emptying time, intestinal transit time, imm...
PMC10383245
core_pubmed_pmc
Transdermal Flunixin Meglumine as a Pain Relief in Donkeys: A Pharmacokinetics Pilot Study
Transdermal Flunixin Meglumine as a Pain Relief in Donkeys: A Pharmacokinetics Pilot Study Abstract Recent approval of transdermal flunixin meglumine (FM) (Banamine ® ) in cattle has opened the door for the drug’s potential application in other species. Transdermal FM could provide a safe and effective form of pain rel...
PMC11770821
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of an innovative psychedelic N,N-dimethyltryptamine/harmine formulation in healthy participants: a randomized controlled trial
Pharmacokinetics and pharmacodynamics of an innovative psychedelic N,N-dimethyltryptamine/harmine formulation in healthy participants: a randomized controlled trial Abstract Abstract Background Recent interest in the clinical use of psychedelics has highlighted plant-derived medicines like ayahuasca showing rapid-actin...
PMC7393820
core_pubmed_pmc
Machine learning reveals that Mycobacterium tuberculosis genotypes and anatomic disease site impacts drug resistance and disease transmission among patients with proven extra-pulmonary tuberculosis
Machine learning reveals that Mycobacterium tuberculosis genotypes and anatomic disease site impacts drug resistance and disease transmission among patients with proven extra-pulmonary tuberculosis Abstract Abstract Background There is a general dearth of information on extrapulmonary tuberculosis (EPTB). Here, we inve...
PMC12315901
core_pubmed_pmc
Safety Profile of Intravenous Ferulic Acid Nanoparticles: Acute Toxicity and Neurological Effects in Sprague-Dawley Rats
Safety Profile of Intravenous Ferulic Acid Nanoparticles: Acute Toxicity and Neurological Effects in Sprague-Dawley Rats Abstract Abstract Background Ferulic acid (FA) exhibits therapeutic potential for various disorders, but its clinical application is hindered by poor bioavailability and solubility. This study aimed ...
PMC6192681
core_pubmed_pmc
An enzymatic approach reverses nicotine dependence, decreases compulsive-like intake, and prevents relapse
An enzymatic approach reverses nicotine dependence, decreases compulsive-like intake, and prevents relapse Abstract Abstract Tobacco use disorder is the leading cause of disease and preventable death worldwide, but current medications that are based on pharmacodynamics have low efficacy. Novel pharmacokinetic approache...
PMC6146116
core_pubmed_pmc
SMMDB: a web-accessible database for small molecule modulators and their targets involved in neurological diseases
SMMDB: a web-accessible database for small molecule modulators and their targets involved in neurological diseases Abstract Abstract High-throughput screening and better understanding of small molecule’s structure–activity relationship (SAR) using computational biology techniques have greatly expanded the face of drug ...
PMC7211195
core_pubmed_pmc
The influence of the coadministration of the p-glycoprotein modulator elacridar on the pharmacokinetics of lapatinib and its distribution in the brain and cerebrospinal fluid
The influence of the coadministration of the p-glycoprotein modulator elacridar on the pharmacokinetics of lapatinib and its distribution in the brain and cerebrospinal fluid Abstract Summary Background Lapatinib is a small-molecule tyrosine kinase inhibitor of human epidermal receptor 2 (HER2) and EGFR that has curren...
PMC10354316
core_pubmed_pmc
Rationale and evidence for the use of new beta-lactam/beta-lactamase inhibitor combinations and cefiderocol in critically ill patients
Rationale and evidence for the use of new beta-lactam/beta-lactamase inhibitor combinations and cefiderocol in critically ill patients Abstract Background Healthcare-associated infections involving Gram-negative bacteria (GNB) with difficult-to-treat resistance (DTR) phenotype are associated with impaired patient-cente...
PMC12018549
core_pubmed_pmc
Exposure–response relationship of niraparib in maintenance therapy for recurrent ovarian cancer: ancillary analysis of the French GINECO–NiQoLe study
Exposure–response relationship of niraparib in maintenance therapy for recurrent ovarian cancer: ancillary analysis of the French GINECO–NiQoLe study Abstract Abstract Background Interindividual variability in pharmacokinetics may influence clinical outcomes of niraparib in patients with platinum-sensitive recurrent ov...
PMC12737763
core_pubmed_pmc
Precision Glyco-Modulation of Macrophages with EF-M2 (Immutalon TM ) Improves Function and Lowers Inflammatory Biomarkers in Aging Dogs: A Double-Blind, Placebo-Controlled Trial
Precision Glyco-Modulation of Macrophages with EF-M2 (Immutalon TM ) Improves Function and Lowers Inflammatory Biomarkers in Aging Dogs: A Double-Blind, Placebo-Controlled Trial Abstract Simple Summary Older dogs often slow down and lose “vitality” because of low-grade, chronic inflammation. EF-M2 is a protein-based tr...
PMC6220428
core_pubmed_pmc
Dolutegravir/rilpivirine for the treatment of HIV-1 infection
Dolutegravir/rilpivirine for the treatment of HIV-1 infection Abstract Abstract Much progress has been made in the development of antiretroviral therapies (ARTs) for HIV-1 infection. Beginning a little over a decade ago, single tablet combination regimens (STRs) became available, and subsequently, newer STR formulation...
PMC8550862
core_pubmed_pmc
OATP1B1 Plays an Important Role in the Transport and Treatment Efficacy of Sorafenib in Hepatocellular Carcinoma
OATP1B1 Plays an Important Role in the Transport and Treatment Efficacy of Sorafenib in Hepatocellular Carcinoma Abstract Background Sorafenib is an anticancer drug used in the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. It is a substrate for the human OATP1B1. This study is ai...
PMC12069994
core_pubmed_pmc
Effect of ABCB1 SNP polymorphisms on the plasma concentrations and clinical outcomes of rivaroxaban in Chinese NVAF patients: a population pharmacokinetic-based study
Effect of ABCB1 SNP polymorphisms on the plasma concentrations and clinical outcomes of rivaroxaban in Chinese NVAF patients: a population pharmacokinetic-based study Abstract Abstract Background This study utilized a population pharmacokinetic (PPK) approach to assess the influence of ABCB1 genetic polymorphisms on th...
PMC10099546
core_pubmed_pmc
Population Pharmacokinetics of Tenecteplase in Patients With Acute Myocardial Infarction and Application to Patients With Acute Ischemic Stroke
Population Pharmacokinetics of Tenecteplase in Patients With Acute Myocardial Infarction and Application to Patients With Acute Ischemic Stroke Abstract Abstract The pharmacokinetics (PK) of tenecteplase in patients with acute ischemic stroke has not been extensively studied. This study aimed to describe PK characteris...
PMC5121396
core_pubmed_pmc
Xpert MTB/RIF Assay Shows Faster Clearance of Mycobacterium tuberculosis DNA with Higher Levels of Rifapentine Exposure
Xpert MTB/RIF Assay Shows Faster Clearance of Mycobacterium tuberculosis DNA with Higher Levels of Rifapentine Exposure Abstract Abstract The Xpert MTB/RIF assay is both sensitive and specific as a diagnostic test. Xpert also reports quantitative output in cycle threshold ( C T ) values, which may provide a dynamic mea...
PMC9784628
core_pubmed_pmc
Impact of Early Intrapatient Variability of Tacrolimus Concentrations on the Risk of Graft-Versus-Host Disease after Allogeneic Stem Cell Transplantation Using High-Dose Post-Transplant Cyclophosphamide
Impact of Early Intrapatient Variability of Tacrolimus Concentrations on the Risk of Graft-Versus-Host Disease after Allogeneic Stem Cell Transplantation Using High-Dose Post-Transplant Cyclophosphamide Abstract Abstract Tacrolimus (Tac) is a pivotal immunosuppressant agent used to prevent graft-versus-host disease (GV...
PMC7719391
core_pubmed_pmc
Dose‐Dependent Acute Effects of Everolimus Administration on Immunological, Neuroendocrine and Psychological Parameters in Healthy Men
Dose‐Dependent Acute Effects of Everolimus Administration on Immunological, Neuroendocrine and Psychological Parameters in Healthy Men Abstract Abstract The rapamycin analogue everolimus (EVR) is a potent inhibitor of the mammalian target of rapamycin (mTOR) and clinically used to prevent allograft rejections as well a...
PMC11835429
core_pubmed_pmc
Population Pharmacokinetic/Pharmacodynamic and Exposure‐Response Modeling Analyses of Sotatercept in Healthy Participants and Patients with Pulmonary Arterial Hypertension
Population Pharmacokinetic/Pharmacodynamic and Exposure‐Response Modeling Analyses of Sotatercept in Healthy Participants and Patients with Pulmonary Arterial Hypertension Abstract Sotatercept is a breakthrough, first‐in‐class biologic, recently approved by the Food and Drug Administration (FDA) for the treatment of pu...
PMC10630019
core_pubmed_pmc
A Systematic Review of Phytochemistry, Nutritional Composition, and Pharmacologic Application of Species of the Genus Viola in Noncommunicable Diseases (NCDs)
A Systematic Review of Phytochemistry, Nutritional Composition, and Pharmacologic Application of Species of the Genus Viola in Noncommunicable Diseases (NCDs) Abstract Viola L. is the largest genus of the Violaceae family with more than 500 species across the globe. The present extensive literature survey revealed Viol...
PMC7183808
core_pubmed_pmc
Omadacycline as a promising new agent for the treatment of infections with Mycobacterium abscessus
Omadacycline as a promising new agent for the treatment of infections with Mycobacterium abscessus Abstract Abstract Background Despite intensive treatment regimens, the outcome of Mycobacterium abscessus infections is extremely poor and thus novel treatment regimens are needed. Although tigecycline seems to be one of ...
PMC8664670
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Desmoteplase
Clinical Pharmacokinetics and Pharmacodynamics of Desmoteplase Abstract Desmoteplase is a bat ( Desmodus rotundus ) saliva-derived fibrinolytic enzyme resembling a urokinase and tissue plasminogen activator. It is highly dependent on fibrin and has some neuroprotective attributes. Intravenous administration of desmotep...
PMC6258891
core_pubmed_pmc
Central pharmacodynamic activity of solanezumab in mild Alzheimer's disease dementia
Central pharmacodynamic activity of solanezumab in mild Alzheimer's disease dementia Abstract Abstract Introduction Solanezumab treatment was previously shown to significantly increase total (bound + unbound) cerebrospinal fluid (CSF) levels of amyloid β (Aβ) 1–40 and Aβ 1–42 in patients with mild to moderate Alzheimer...
PMC7913839
core_pubmed_pmc
The Minimum Inhibitory Concentration of Antibiotics: Methods, Interpretation, Clinical Relevance
The Minimum Inhibitory Concentration of Antibiotics: Methods, Interpretation, Clinical Relevance Abstract Inefficiency of medical therapies used in order to cure patients with bacterial infections requires not only to actively look for new therapeutic strategies but also to carefully select antibiotics based on variety...
PMC7383501
core_pubmed_pmc
Pharmacokinetic and dose‐finding studies on efpeglenatide in patients with type 2 diabetes
Pharmacokinetic and dose‐finding studies on efpeglenatide in patients with type 2 diabetes Abstract Abstract Aim To assess the efficacy, safety and pharmacokinetic/pharmacodynamic properties of efpeglenatide, a long‐acting glucagon‐like peptide‐1 receptor agonist, in patients with type 2 diabetes (T2D). Research design...
PMC4552636
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution, and Anti-Lipogenic/Adipogenic Effects of Allyl-Isothiocyanate Metabolites
Pharmacokinetics, Tissue Distribution, and Anti-Lipogenic/Adipogenic Effects of Allyl-Isothiocyanate Metabolites Abstract Allyl-isothiocyanate (AITC) is an organosulfur phytochemical found in abundance in common cruciferous vegetables such as mustard, wasabi, and cabbage. Although AITC is metabolized primarily through ...
PMC4284384
core_pubmed_pmc
Quantitative Measurement of the Target-Mediated Internalization Kinetics of Biopharmaceuticals
Quantitative Measurement of the Target-Mediated Internalization Kinetics of Biopharmaceuticals Abstract Purpose Measurement of internalization of biopharmaceuticals targeting cell surface proteins can greatly facilitate drug development. The objective of this study was to develop a reliable method for determination of ...
PMC10398856
core_pubmed_pmc
Discovery of Hybrid Thiouracil–Coumarin Conjugates as Potential Novel Anti-SARS-CoV-2 Agents Targeting the Virus’s Polymerase “RdRp” as a Confirmed Interacting Biomolecule
Discovery of Hybrid Thiouracil–Coumarin Conjugates as Potential Novel Anti-SARS-CoV-2 Agents Targeting the Virus’s Polymerase “RdRp” as a Confirmed Interacting Biomolecule Abstract The coronavirus (COVID-19) pandemic, along with its various strains, has emerged as a global health crisis that has severely affected human...
PMC7325314
core_pubmed_pmc
Assessment of Maternal and Fetal Dolutegravir Exposure by Integrating Ex Vivo Placental Perfusion Data and Physiologically‐Based Pharmacokinetic Modeling
Assessment of Maternal and Fetal Dolutegravir Exposure by Integrating Ex Vivo Placental Perfusion Data and Physiologically‐Based Pharmacokinetic Modeling Abstract Antiretroviral therapy during pregnancy reduces the risk of vertical HIV‐1 transmission. However, drug dosing is challenging as pharmacokinetics (PK) may be ...
PMC10859324
core_pubmed_pmc
Obesity: a gender-view
Obesity: a gender-view Abstract Purpose There is a growing awareness of the importance of understanding gender differences in obesity. The aim of this short review was to revise the current evidence on anthropometric characteristics and nutritional and pharmacological aspects of obesity from a gender perspective. Metho...
PMC4050360
core_pubmed_pmc
Biological conversion of aripiprazole lauroxil - An N -acyloxymethyl aripiprazole prodrug
Biological conversion of aripiprazole lauroxil - An N -acyloxymethyl aripiprazole prodrug Abstract N -acyloxyalkylation of NH -acidic compounds can be a prodrug approach for e.g. tertiary or some N -heterocyclic amines and secondary amides and have the potential to modify the properties of the parent drug for specific ...
PMC8257471
core_pubmed_pmc
Rifampin Reduces the Plasma Concentrations of Oral and Intravenous Hydromorphone in Healthy Volunteers
Rifampin Reduces the Plasma Concentrations of Oral and Intravenous Hydromorphone in Healthy Volunteers Abstract BACKGROUND: Several opioids are metabolized by the inducible cytochrome P450 (CYP) 3A isozymes. Coadministration with strong inducers of drug metabolism, such as rifampin, can dramatically reduce systemic exp...
PMC12574446
core_pubmed_pmc
Blood Pressure Reduction During Anesthetic Induction with Remimazolam versus Propofol in Elderly Patients: Pharmacodynamic Modeling of Remimazolam
Blood Pressure Reduction During Anesthetic Induction with Remimazolam versus Propofol in Elderly Patients: Pharmacodynamic Modeling of Remimazolam Abstract Purpose Remimazolam, a novel hypnotic agent, has demonstrated superior hemodynamic stability compared with propofol during general anesthesia, particularly in elder...
PMC10689914
core_pubmed_pmc
In vitro synergy of the combination of sulbactam-durlobactam and cefepime at clinically relevant concentrations against A. baumannii , P. aeruginosa and Enterobacterales
In vitro synergy of the combination of sulbactam-durlobactam and cefepime at clinically relevant concentrations against A. baumannii , P. aeruginosa and Enterobacterales Abstract Abstract Background Sulbactam-durlobactam is a potent combination active against Acinetobacter baumannii ; however, it lacks activity against...
PMC10956049
core_pubmed_pmc
Safety, efficacy, and pharmacokinetics of nirmatrelvir and ritonavir in patients with severe COVID-19 and renal impairment: A case report
Safety, efficacy, and pharmacokinetics of nirmatrelvir and ritonavir in patients with severe COVID-19 and renal impairment: A case report Abstract Nirmatrelvir/ritonavir (N/r) has received emergency use authorization for mild-to-moderate COVID-19 treatment in adult and pediatric patients (aged and weighing at least 12 ...
PMC8463036
core_pubmed_pmc
Allometric scaling of therapeutic monoclonal antibodies in preclinical and clinical settings
Allometric scaling of therapeutic monoclonal antibodies in preclinical and clinical settings Abstract ABSTRACT Constant technological advancement enabled the production of therapeutic monoclonal antibodies (mAbs) and will continue to contribute to their rapid expansion. Compared to small-molecule drugs, mAbs have favor...
PMC7218526
core_pubmed_pmc
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy Abstract Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein o...
PMC5667771
core_pubmed_pmc
Pyrazinamide clearance is impaired among HIV/tuberculosis patients with high levels of systemic immune activation
Pyrazinamide clearance is impaired among HIV/tuberculosis patients with high levels of systemic immune activation Abstract Pyrazinamide is the main driver of sterilizing effect in the standard regimen in adults and older children, and this effect is concentration-dependent. Tuberculosis patients co-infected with human ...
PMC9836147
core_pubmed_pmc
Awareness on current status of usage of ritonavir in the management of covid among dental students
Awareness on current status of usage of ritonavir in the management of covid among dental students Abstract Abstract Ritonavir's pharmacodynamics raise questions regarding whether medication concentrations high enough to block the SARS-CoV-2 proteases can be obtained. Ritonavir may have a therapeutic benefit at any sta...
PMC10980240
core_pubmed_pmc
From Flora to Pharmaceuticals: 100 new additions to angiosperms of Gafargaon subdistrict in Bangladesh and unraveling antidiabetic drug candidates targeting DPP4 through in silico approach
From Flora to Pharmaceuticals: 100 new additions to angiosperms of Gafargaon subdistrict in Bangladesh and unraveling antidiabetic drug candidates targeting DPP4 through in silico approach Abstract Addition to the angiosperm flora provides essential insights into the biodiversity of a region, contributing to ecological...
PMC10051381
core_pubmed_pmc
Therapeutic Drug Monitoring of Vedolizumab in Inflammatory Bowel Disease Patients during Maintenance Treatment—TUMMY Study
Therapeutic Drug Monitoring of Vedolizumab in Inflammatory Bowel Disease Patients during Maintenance Treatment—TUMMY Study Abstract Abstract There are limited data on therapeutic drug monitoring (TDM) in inflammatory bowel disease (IBD) patients treated with vedolizumab (VDZ). Although an exposure–response relation has...
PMC7670518
core_pubmed_pmc
Regression of Atherosclerosis in ApoE−/− Mice Via Modulation of Monocyte Recruitment and Phenotype, Induced by Weekly Dosing of a Novel “Cytotopic” Anti‐Thrombin Without Prolonged Anticoagulation
Regression of Atherosclerosis in ApoE−/− Mice Via Modulation of Monocyte Recruitment and Phenotype, Induced by Weekly Dosing of a Novel “Cytotopic” Anti‐Thrombin Without Prolonged Anticoagulation Abstract Abstract Background Anticoagulants induce atherosclerosis regression in animal models but exploiting this clinicall...
PMC4363860
core_pubmed_pmc
Sensitization of Gram-negative bacteria to rifampin and OAK combinations
Sensitization of Gram-negative bacteria to rifampin and OAK combinations Abstract While individually inefficient against Gram-negative bacteria, in-vitro combinations of rifampin and OAK were mutually synergistic since sub-minimal inhibitory concentrations of one compound have potentiated the other by 2–4 orders of mag...
PMC11687410
core_pubmed_pmc
Model‐based interspecies interpretation of botulinum neurotoxin type A on muscle‐contraction inhibition
Model‐based interspecies interpretation of botulinum neurotoxin type A on muscle‐contraction inhibition Abstract Abstract Botulinum neurotoxins (BoNTs) are commonly used in therapeutic and cosmetic applications. One such neurotoxin, BoNT type A (BoNT/A), has been studied widely for its effects on muscle function and co...
PMC10572397
core_pubmed_pmc
Effect of Food on the Pharmacokinetics of Tenofovir Amibufenamide: A Phase I, Randomized, Open-Label, Two-Period Crossover Trial in Healthy Adult Subjects
Effect of Food on the Pharmacokinetics of Tenofovir Amibufenamide: A Phase I, Randomized, Open-Label, Two-Period Crossover Trial in Healthy Adult Subjects Abstract Abstract Purpose Tenofovir amibufenamide (TMF) is a novel nucleotide reverse transcriptase inhibitor. The aim of this study was to investigate the effect of...
PMC8116206
core_pubmed_pmc
Herb-drug interaction in the protective effect of Alpinia officinarum against gastric injury induced by indomethacin based on pharmacokinetic, tissue distribution and excretion studies in rats
Herb-drug interaction in the protective effect of Alpinia officinarum against gastric injury induced by indomethacin based on pharmacokinetic, tissue distribution and excretion studies in rats Abstract Abstract Alpinia officinarum Hance of the Chinese traditional herb for the treatment of emesis, abdominal pain and dia...
PMC6598168
core_pubmed_pmc
Development and validation of an LC-MS/MS method for tyrphostin A9
Development and validation of an LC-MS/MS method for tyrphostin A9 Abstract Abstract Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as ...
PMC3428318
core_pubmed_pmc
Pharmacodynamics of Antimicrobials against Mycoplasma mycoides mycoides Small Colony, the Causative Agent of Contagious Bovine Pleuropneumonia
Pharmacodynamics of Antimicrobials against Mycoplasma mycoides mycoides Small Colony, the Causative Agent of Contagious Bovine Pleuropneumonia Abstract Abstract Background Mycoplasma mycoides subspecies mycoides Small Colony ( Mmm SC) is the causative agent of Contagious Bovine Pleuropneumonia (CBPP), a disease of subs...
PMC4548739
core_pubmed_pmc
Efficacy and safety of the long-acting β 2 -agonist olodaterol over 4 weeks in Japanese patients with chronic obstructive pulmonary disease
Efficacy and safety of the long-acting β 2 -agonist olodaterol over 4 weeks in Japanese patients with chronic obstructive pulmonary disease Abstract Abstract Background Olodaterol is a novel long-acting β 2 -agonist with proven ≥24-hour duration of action in preclinical and clinical studies. Objective This randomized, ...
PMC8246766
core_pubmed_pmc
Pharmacokinetics of Belimumab in Children With Systemic Lupus Erythematosus
Pharmacokinetics of Belimumab in Children With Systemic Lupus Erythematosus Abstract Abstract The phase 2 placebo‐controlled, double‐blind PLUTO trial characterized the pharmacokinetics of belimumab plus standard systemic lupus erythematosus (SLE) therapy in patients with childhood‐onset SLE (cSLE) and demonstrated sim...
PMC12180593
core_pubmed_pmc
Model-Informed Precision Dosing of Remimazolam in General Anesthesia Patients
Model-Informed Precision Dosing of Remimazolam in General Anesthesia Patients Abstract Purpose This study aimed to characterize the pharmacokinetics/pharmacodynamics (PK/PD) of remimazolam in patients under general anesthesia using a population analysis and to develop a web-based dashboard tool that directly displays t...
PMC11089243
core_pubmed_pmc
The first selective VAP-1 inhibitor in China, TT-01025-CL: safety, tolerability, pharmacokinetics, and pharmacodynamics of single- and multiple-ascending doses
The first selective VAP-1 inhibitor in China, TT-01025-CL: safety, tolerability, pharmacokinetics, and pharmacodynamics of single- and multiple-ascending doses Abstract Abstract Introduction: TT-01025-CL is an oral, irreversible small molecule that potently inhibits vascular adhesion protein-1 (VAP-1) for the treatment...
PMC11701949
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Neonatal Fc Receptor Inhibitor Rozanolixizumab: An Ethnic Sensitivity Study in Healthy Japanese, Chinese, and White Participants
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Neonatal Fc Receptor Inhibitor Rozanolixizumab: An Ethnic Sensitivity Study in Healthy Japanese, Chinese, and White Participants Abstract Abstract Rozanolixizumab is an anti‐human neonatal Fc receptor humanized immunoglobulin (Ig) G4 monoclonal antibod...
PMC5321639
core_pubmed_pmc
Design and pharmacodynamics of recombinant NZ2114 histidine mutants with improved activity against methicillin-resistant Staphylococcus aureus
Design and pharmacodynamics of recombinant NZ2114 histidine mutants with improved activity against methicillin-resistant Staphylococcus aureus Abstract NZ2114 is a promising candidate for therapeutic application owing to its potent activity to Staphylococcus aureus . Our objective was to identify NZ2114 derivatives wit...
PMC12304798
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of HSK31858, a novel oral dipeptidyl peptidase‐1 inhibitor, in healthy volunteers: An integrated phase 1, randomized, double‐blind, placebo‐controlled, single‐ and multiple‐ascending dose study
Safety, tolerability, pharmacokinetics and pharmacodynamics of HSK31858, a novel oral dipeptidyl peptidase‐1 inhibitor, in healthy volunteers: An integrated phase 1, randomized, double‐blind, placebo‐controlled, single‐ and multiple‐ascending dose study Abstract Abstract Aim Dipeptidyl peptidase‐1 (DPP‐1) inhibitors ha...
PMC11284144
core_pubmed_pmc
A phase 1, randomized, double-blind, placebo-controlled, dose escalation study to evaluate the safety, tolerability, pharmacokinetics and immunogenicity of SHR-1905, a long-acting anti-thymic stromal lymphopoietin antibody, in healthy subjects
A phase 1, randomized, double-blind, placebo-controlled, dose escalation study to evaluate the safety, tolerability, pharmacokinetics and immunogenicity of SHR-1905, a long-acting anti-thymic stromal lymphopoietin antibody, in healthy subjects Abstract Abstract Introduction Thymic stromal lymphopoietin (TSLP) is integr...
PMC8951011
core_pubmed_pmc
Effect of Caffeine and Flavonoids on the Binding of Tigecycline to Human Serum Albumin: A Spectroscopic Study and Molecular Docking
Effect of Caffeine and Flavonoids on the Binding of Tigecycline to Human Serum Albumin: A Spectroscopic Study and Molecular Docking Abstract Abstract Human serum albumin (HSA) has a very significant role in the transport of drugs, in their pharmacokinetic and pharmacodynamic properties, as well as the unbound concentra...
PMC9137536
core_pubmed_pmc
Drug Regimens of Novel Antibiotics in Critically Ill Patients with Varying Renal Functions: A Rapid Review
Drug Regimens of Novel Antibiotics in Critically Ill Patients with Varying Renal Functions: A Rapid Review Abstract Abstract There is currently an increase in the emergence of multidrug-resistant bacteria (MDR) worldwide, requiring the development of novel antibiotics. However, it is not only the choice of antibiotic t...
PMC4504870
core_pubmed_pmc
Absorption, distribution and excretion of intravenously injected 68 Ge/ 68 Ga generator eluate in healthy rats, and estimation of human radiation dosimetry
Absorption, distribution and excretion of intravenously injected 68 Ge/ 68 Ga generator eluate in healthy rats, and estimation of human radiation dosimetry Abstract Abstract Background This study evaluated the absorption, distribution, and excretion of Gallium-68 ( 68 Ga) radionuclide after a single intravenous (i.v.) ...
PMC8647693
core_pubmed_pmc
Genital Mucosal Drug Concentrations and anti-HIV Activity in Tenofovir-Based PrEP Products: Intravaginal Ring vs. Oral Administration
Genital Mucosal Drug Concentrations and anti-HIV Activity in Tenofovir-Based PrEP Products: Intravaginal Ring vs. Oral Administration Abstract Supplemental Digital Content is Available in the Text. Objective: To describe and compare systemic and local pharmacokinetics (PK) and cervicovaginal (CV) pharmacodynamics (PD) ...
PMC6966182
core_pubmed_pmc
Probenecid‐Boosted Tenofovir: A Physiologically‐Based Pharmacokinetic Model‐Informed Strategy for On‐Demand HIV Preexposure Prophylaxis
Probenecid‐Boosted Tenofovir: A Physiologically‐Based Pharmacokinetic Model‐Informed Strategy for On‐Demand HIV Preexposure Prophylaxis Abstract Abstract Multiple doses of tenofovir disoproxil fumarate (TDF) together with emtricitabine is effective for HIV preexposure prophylaxis (PrEP). TDF is converted to tenofovir (...
PMC12902727
core_pubmed_pmc
Model‐Informed Abatacept Dose Recommendation in Pediatric Patients With Acute Graft Versus Host Disease
Model‐Informed Abatacept Dose Recommendation in Pediatric Patients With Acute Graft Versus Host Disease Abstract Abstract This study uses a population pharmacokinetic (PPK) approach to provide abatacept dosing recommendations in pediatric patients 2 to < 6 years of age receiving unrelated donor hematopoietic stem cell ...
PMC12495782
core_pubmed_pmc
Exploratory high-throughput screening of repurposed drugs for canine lymphoid malignancies
Exploratory high-throughput screening of repurposed drugs for canine lymphoid malignancies Abstract Abstract Background Lymphoid malignancies are common in dogs. However, the limitations of existing chemotherapy highlight the need for alternative therapies. Drug repositioning is a promising approach for discovering new...
PMC5814527
core_pubmed_pmc
Access to the CNS: Biomarker Strategies for Dopaminergic Treatments
Access to the CNS: Biomarker Strategies for Dopaminergic Treatments Abstract Abstract Despite substantial research carried out over the last decades, it remains difficult to understand the wide range of pharmacological effects of dopaminergic agents. The dopaminergic system is involved in several neurological disorders...
PMC8793782
core_pubmed_pmc
Post-hoc Analysis of Pharmacodynamics and Single-Agent Activity of CD3xCD123 Bispecific Antibody APVO436 in Relapsed/Refractory AML and MDS Resistant to HMA or Venetoclax Plus HMA
Post-hoc Analysis of Pharmacodynamics and Single-Agent Activity of CD3xCD123 Bispecific Antibody APVO436 in Relapsed/Refractory AML and MDS Resistant to HMA or Venetoclax Plus HMA Abstract Abstract APVO436 is a recombinant bispecific antibody designed to direct host cytotoxic T-cells to CD123-expressing blast cells in ...
PMC6714928
core_pubmed_pmc
Effects of Obesity on Warfarin Reversal With Vitamin K
Effects of Obesity on Warfarin Reversal With Vitamin K Abstract Abstract Phytonadione (vitamin K1, VK) is fat soluble and may be sequestered by adipose tissue, thus potentially altering drug distribution in obese patients requiring warfarin reversal. This single-center retrospective cohort study aimed to determine the ...
PMC4041784
core_pubmed_pmc
Stereoselective Property of 20( S )-Protopanaxadiol Ocotillol Type Epimers Affects Its Absorption and Also the Inhibition of P-Glycoprotein
Stereoselective Property of 20( S )-Protopanaxadiol Ocotillol Type Epimers Affects Its Absorption and Also the Inhibition of P-Glycoprotein Abstract Abstract Stereoselectivity has been proved to be tightly related to drug action including pharmacodynamics and pharmacokinetics. (20S,24R)-epoxy-dammarane-3,12,25-triol (2...
PMC11868361
core_pubmed_pmc
Repeated Switching Between CT-P17 and EU Reference Adalimumab in Patients with Moderate-to-Severe Chronic Plaque Psoriasis: A Randomized, Double-Blind, Active-Controlled, Phase 3, Interchangeability Study
Repeated Switching Between CT-P17 and EU Reference Adalimumab in Patients with Moderate-to-Severe Chronic Plaque Psoriasis: A Randomized, Double-Blind, Active-Controlled, Phase 3, Interchangeability Study Abstract Abstract Introduction This study aimed to demonstrate the interchangeability of biosimilar CT-P17 and Euro...
PMC5799260
core_pubmed_pmc
Genetic variability affects absolute and relative potencies and kinetics of the anesthetics isoflurane and sevoflurane in Drosophila melanogaster
Genetic variability affects absolute and relative potencies and kinetics of the anesthetics isoflurane and sevoflurane in Drosophila melanogaster Abstract Abstract Genetic variability affects the response to numerous xenobiotics but its role in the clinically-observed irregular responses to general anesthetics remains ...
PMC6702932
core_pubmed_pmc
Pharmacokinetics of combination antiparasitic drug preparation for dogs and cats in the form of spot-on solution
Pharmacokinetics of combination antiparasitic drug preparation for dogs and cats in the form of spot-on solution Abstract Abstract Objective: The object of the study was to examine the major pharmacokinetic parameters after a single application of a complex drug preparation for veterinary use based on fipronil, praziqu...
PMC6617747
core_pubmed_pmc
Monoclonal Antibodies and Fc‐Fusion Proteins for Pediatric Use: Dosing, Immunogenicity, and Modeling and Simulation in Data Submitted to the US Food and Drug Administration
Monoclonal Antibodies and Fc‐Fusion Proteins for Pediatric Use: Dosing, Immunogenicity, and Modeling and Simulation in Data Submitted to the US Food and Drug Administration Abstract Abstract The experience with the use of monoclonal antibodies and Fc‐fusion proteins (mAb/Fc) in the pediatric population is limited. The ...
PMC4753396
core_pubmed_pmc
In vivo evaluation of different alterations of redox status by studying pharmacokinetics of nitroxides using magnetic resonance techniques
In vivo evaluation of different alterations of redox status by studying pharmacokinetics of nitroxides using magnetic resonance techniques Abstract Free radicals, particularly reactive oxygen species (ROS), are involved in various pathologies, injuries related to radiation, ischemia-reperfusion or ageing. Unfortunately...
PMC12086322
core_pubmed_pmc
Pharmacodynamic Effect of Different Dosage Regimes of Oseltamivir in Severe Influenza Patients Requiring Mechanical Ventilation: A Multicentre Randomised Controlled Trial
Pharmacodynamic Effect of Different Dosage Regimes of Oseltamivir in Severe Influenza Patients Requiring Mechanical Ventilation: A Multicentre Randomised Controlled Trial Abstract ABSTRACT Background and Objectives This randomised controlled trial evaluated whether higher doses of oseltamivir would improve virological ...
PMC4492732
core_pubmed_pmc
The distribution and clearance of (2S,6S)-hydroxynorketamine, an active ketamine metabolite, in Wistar rats
The distribution and clearance of (2S,6S)-hydroxynorketamine, an active ketamine metabolite, in Wistar rats Abstract Abstract The distribution, clearance, and bioavailability of (2S,6S)-hydroxynorketamine has been studied in the Wistar rat. The plasma and brain tissue concentrations over time of (2S,6S)-hydroxynorketam...
PMC12657313
core_pubmed_pmc
A comparison of theacrine and methylliberine with caffeine as salivary markers for determining gastric emptying
A comparison of theacrine and methylliberine with caffeine as salivary markers for determining gastric emptying Abstract Gastric emptying is a critical determinant of the pharmacokinetics of orally administered drugs. A key limitation in studies using caffeine as a marker for gastric emptying is the requirement for pri...
PMC7356959
core_pubmed_pmc
Quantification of Pharmacokinetic Profiles of PD-1/PD-L1 Antibodies by Validated ELISAs
Quantification of Pharmacokinetic Profiles of PD-1/PD-L1 Antibodies by Validated ELISAs Abstract Abstract Immunotherapy has changed the paradigm of cancer treatments. In this way, several combinatorial strategies based on monoclonal antibodies (mAb) such as anti (a)-PD-1 or anti (a)-PD-L1 are often reported to yield pr...
PMC3967138
core_pubmed_pmc
Tacrolimus Pharmacokinetic and Pharmacogenomic Differences between Adults and Pediatric Solid Organ Transplant Recipients
Tacrolimus Pharmacokinetic and Pharmacogenomic Differences between Adults and Pediatric Solid Organ Transplant Recipients Abstract Tacrolimus is a calcineurin inhibitor immunosuppressant that has seen considerable use in both adult and pediatric solid organ transplant recipients. Though there is much pharmacokinetic da...
PMC6789481
core_pubmed_pmc
A Comparative Pharmacokinetic Analysis of Oral and Subcutaneous Meloxicam Administered to Postpartum Dairy Cows
A Comparative Pharmacokinetic Analysis of Oral and Subcutaneous Meloxicam Administered to Postpartum Dairy Cows Abstract The dairy industry needs evidence-based solutions to mitigate painful procedures and conditions in dairy cattle. The objective of this study was to compare the pharmacokinetic properties of orally ve...
PMC8663927
core_pubmed_pmc
Pharmacokinetic drug interactions of integrase strand transfer inhibitors
Pharmacokinetic drug interactions of integrase strand transfer inhibitors Abstract The integrase strand transfer inhibitor (INSTI)-containing regimens are currently considered as the first-line treatment of human immunodeficiency virus (HIV) infection. Although possessing a common mechanism of action to inhibit HIV int...
PMC6429202
core_pubmed_pmc
Drug-1,3,4-Thiadiazole Conjugates as Novel Mixed-Type Inhibitors of Acetylcholinesterase: Synthesis, Molecular Docking, Pharmacokinetics, and ADMET Evaluation
Drug-1,3,4-Thiadiazole Conjugates as Novel Mixed-Type Inhibitors of Acetylcholinesterase: Synthesis, Molecular Docking, Pharmacokinetics, and ADMET Evaluation Abstract Abstract A small library of new drug-1,3,4-thiazidazole hybrid compounds ( 3a – 3i ) was synthesized, characterized, and assessed for their acetyl choli...
PMC12566120
core_pubmed_pmc
In Vitro Metabolism of a Benzofuran-Substituted Nitazene: Ethyleneoxynitazene
In Vitro Metabolism of a Benzofuran-Substituted Nitazene: Ethyleneoxynitazene Abstract Abstract Background/Objectives : New synthetic opioids (NSOs) like nitazenes pose significant public health risks due to their high potency and increasing prevalence. Ethyleneoxynitazene, a benzofuran-containing nitazene, recently em...
PMC9292591
core_pubmed_pmc
Assessment of the safe and efficacious dose of the selective progesterone receptor modulator vilaprisan for the treatment of patients with uterine fibroids by exposure–response modelling and simulation
Assessment of the safe and efficacious dose of the selective progesterone receptor modulator vilaprisan for the treatment of patients with uterine fibroids by exposure–response modelling and simulation Abstract Aims We report population pharmacokinetic (popPK) and exposure–response (E–R) analyses for efficacy (induced ...
PMC9434412
core_pubmed_pmc
Phase I, first-in-human study of MSC-1 (AZD0171), a humanized anti-leukemia inhibitory factor monoclonal antibody, for advanced solid tumors
Phase I, first-in-human study of MSC-1 (AZD0171), a humanized anti-leukemia inhibitory factor monoclonal antibody, for advanced solid tumors Abstract Abstract Background Activation of leukemia inhibitory factor (LIF) is linked to an immunosuppressive tumor microenvironment (TME), with a strong association between LIF e...