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PMC11052790
core_pubmed_pmc
Time Course of the Interaction Between Oral Short-Term Ritonavir Therapy with Three Factor Xa Inhibitors and the Activity of CYP2D6, CYP2C19, and CYP3A4 in Healthy Volunteers
Time Course of the Interaction Between Oral Short-Term Ritonavir Therapy with Three Factor Xa Inhibitors and the Activity of CYP2D6, CYP2C19, and CYP3A4 in Healthy Volunteers Abstract Abstract Background We investigated the effect of a 5-day low-dose ritonavir therapy, as it is used in the treatment of COVID-19 with ni...
PMC6227840
core_pubmed_pmc
Pharmacokinetics of Vancomycin in Patients with Different Renal Function Levels
Pharmacokinetics of Vancomycin in Patients with Different Renal Function Levels Abstract Abstract There are many determinants of vancomycin clearance, but these have not been analyzed separately in populations with different levels of renal function, which could be why some important factors have been missed. The aim o...
PMC12191815
core_pubmed_pmc
Genetic Mechanisms of Antimicrobial Non-Susceptibility to Novel Fluoroquinolone Delafloxacin Among Bulgarian Clinical Isolates of Streptococcus agalactiae
Genetic Mechanisms of Antimicrobial Non-Susceptibility to Novel Fluoroquinolone Delafloxacin Among Bulgarian Clinical Isolates of Streptococcus agalactiae Abstract Delafloxacin is one of the newest fluoroquinolones with a unique structure, determining better pharmacokinetic and pharmacodynamic properties, a better safe...
PMC8709907
core_pubmed_pmc
Preclinical and clinical evaluation of German-sourced ONC201 for the treatment of H3K27M-mutant diffuse intrinsic pontine glioma
Preclinical and clinical evaluation of German-sourced ONC201 for the treatment of H3K27M-mutant diffuse intrinsic pontine glioma Abstract Abstract Background Diffuse intrinsic pontine glioma (DIPG) is a fatal childhood brainstem tumor for which radiation is the only treatment. Case studies report a clinical response to...
PMC8614650
core_pubmed_pmc
Effects of Growth Medium and Inoculum Size on Pharmacodynamics Activity of Marbofloxacin against Staphylococcus aureus Isolated from Caprine Clinical Mastitis
Effects of Growth Medium and Inoculum Size on Pharmacodynamics Activity of Marbofloxacin against Staphylococcus aureus Isolated from Caprine Clinical Mastitis Abstract Abstract Staphylococcus aureus ( S. aureus ) is an important pathogen that causes clinical mastitis in goats and produces infections difficult to cure. ...
PMC10763448
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of perfluoropropane after intra-venous bolus injection of perflutren lipid microsphere injection (DEFINITY®) in healthy Chinese volunteers
Pharmacokinetics and pharmacodynamics of perfluoropropane after intra-venous bolus injection of perflutren lipid microsphere injection (DEFINITY®) in healthy Chinese volunteers Abstract Background and objective Definity is an ultrasound contrast agent consisting of phospholipids-encapsulated perfluoropropane (PFP), als...
PMC10444824
core_pubmed_pmc
Predicting the molecular mechanism-driven progression of breast cancer through comprehensive network pharmacology and molecular docking approach
Predicting the molecular mechanism-driven progression of breast cancer through comprehensive network pharmacology and molecular docking approach Abstract Abstract Identification of key regulators is a critical step toward discovering biomarker that participate in BC. A gene expression dataset of breast cancer patients ...
PMC6339746
core_pubmed_pmc
Quantification of Lappaconitine in Mouse Blood by UPLC-MS/MS and Its Application to a Pharmacokinetic Study
Quantification of Lappaconitine in Mouse Blood by UPLC-MS/MS and Its Application to a Pharmacokinetic Study Abstract Lappaconitine is extracted from Aconitum sinomontanum Nakai, which belongs to the Ranunculaceae. Lappaconitine is as a diterpenoid alkaloid used as a nonaddictive analgesic. To assure the rational use of...
PMC12594730
core_pubmed_pmc
QT interval prolongation: clinical assessment, risk factors and quantitative pharmacological considerations
QT interval prolongation: clinical assessment, risk factors and quantitative pharmacological considerations Abstract Abstract Prolongation of the QT interval in the ECG is a critical finding that signifies an extended duration from the onset of ventricular depolarization to the end of ventricular repolarization. It can...
PMC7417410
core_pubmed_pmc
Population pharmacokinetics–pharmacodynamics of sunitinib in pediatric patients with solid tumors
Population pharmacokinetics–pharmacodynamics of sunitinib in pediatric patients with solid tumors Abstract Purpose The safety profile of sunitinib in children, including the impact of sunitinib exposure on safety endpoints, was assessed using population pharmacokinetic (PK) and pharmacokinetic–pharmacodynamic (PK–PD) m...
PMC10640521
core_pubmed_pmc
Patient Factors Influencing Intraocular Penetration of Brimonidine-Related Eye Drops in Adults: A Post Hoc Pooled Analysis
Patient Factors Influencing Intraocular Penetration of Brimonidine-Related Eye Drops in Adults: A Post Hoc Pooled Analysis Abstract Introduction The factors related to the ocular penetration of drugs after the administration of eye drops in humans have not been examined in detail. Therefore, this study assessed the inf...
PMC8743345
core_pubmed_pmc
Cysteamine bitartrate delayed‐release capsules control leukocyte cystine levels and promote statural growth and kidney health in an open‐label study of treatment‐naïve patients <6 years of age with nephropathic cystinosis
Cysteamine bitartrate delayed‐release capsules control leukocyte cystine levels and promote statural growth and kidney health in an open‐label study of treatment‐naïve patients <6 years of age with nephropathic cystinosis Abstract Abstract Nephropathic cystinosis is a rare autosomal recessive lysosomal storage disease ...
PMC8212709
core_pubmed_pmc
A Phase I, Randomized, Double‐Blind, Placebo‐Controlled, Single‐Dose and Multiple‐Rising‐Dose Study of the BTK Inhibitor TAK‐020 in Healthy Subjects
A Phase I, Randomized, Double‐Blind, Placebo‐Controlled, Single‐Dose and Multiple‐Rising‐Dose Study of the BTK Inhibitor TAK‐020 in Healthy Subjects Abstract Abstract Bruton’s tyrosine kinase (BTK) is a target for treatment of hematologic malignancies and autoimmune diseases. TAK‐020 is a highly selective covalent BTK ...
PMC6708059
core_pubmed_pmc
Convergence of Cell Pharmacology and Drug Delivery
Convergence of Cell Pharmacology and Drug Delivery Abstract Summary Cellular therapy is enabling new approaches to tackle significant unmet needs in areas such as regenerative medicine and immunotherapy. The pharmacology of cell therapeutics becomes of critical importance to assure that these new drugs work reproducibl...
PMC3880470
core_pubmed_pmc
Pharmacokinetics of Mirabegron, a β 3 -Adrenoceptor Agonist for Treatment of Overactive Bladder, in Healthy Japanese Male Subjects: Results from Single- and Multiple-Dose Studies
Pharmacokinetics of Mirabegron, a β 3 -Adrenoceptor Agonist for Treatment of Overactive Bladder, in Healthy Japanese Male Subjects: Results from Single- and Multiple-Dose Studies Abstract Abstract Background Mirabegron is a human β 3 -adrenoceptor agonist for the treatment of overactive bladder. The pharmacokinetic pro...
PMC10665782
core_pubmed_pmc
Evaluation of the inhibitory effect of azoles on pharmacokinetics of lenvatinib in rats both in vivo and in vitro by UPLC‐MS/MS
Evaluation of the inhibitory effect of azoles on pharmacokinetics of lenvatinib in rats both in vivo and in vitro by UPLC‐MS/MS Abstract Abstract Background Lenvatinib is a multitargeted tyrosine kinase inhibitor used in the treatment of a variety of solid tumors. This study aims to investigate the potential pharmacoki...
PMC9540480
core_pubmed_pmc
Applying Modeling and Simulations for Rational Dose Selection of Novel Toll‐Like Receptor 7/8 Inhibitor Enpatoran for Indications of High Medical Need
Applying Modeling and Simulations for Rational Dose Selection of Novel Toll‐Like Receptor 7/8 Inhibitor Enpatoran for Indications of High Medical Need Abstract Dual toll‐like receptor (TLR) 7 and TLR8 inhibitor enpatoran is under investigation as a treatment for lupus and coronavirus disease 2019 (COVID‐19) pneumonia. ...
PMC9944491
core_pubmed_pmc
Haemophilia A: A Review of Clinical Manifestations, Treatment, Mutations, and the Development of Inhibitors
Haemophilia A: A Review of Clinical Manifestations, Treatment, Mutations, and the Development of Inhibitors Abstract The purpose of this narrative review was to provide an overview that allows readers to improve their understanding of hemophilia A, which is considered a genetic disease with a high impact on the quality...
PMC10858190
core_pubmed_pmc
Mitigating non-genetic resistance to checkpoint inhibition based on multiple states of immune exhaustion
Mitigating non-genetic resistance to checkpoint inhibition based on multiple states of immune exhaustion Abstract Abstract Despite the revolutionary impact of immune checkpoint inhibition on cancer therapy, the lack of response in a subset of patients, as well as the emergence of resistance, remain significant challeng...
PMC5911476
core_pubmed_pmc
Novel Antimicrobials for the Treatment of Clostridium difficile Infection
Novel Antimicrobials for the Treatment of Clostridium difficile Infection Abstract Abstract The current picture of Clostridium difficile infection (CDI) is alarming with a mortality rate ranging between 3% and 15% and a CDI recurrence rate ranging from 12% to 40%. Despite the great efforts made over the past 10 years t...
PMC12129139
core_pubmed_pmc
Obesity-related drug-metabolizing enzyme expression alterations in the human liver
Obesity-related drug-metabolizing enzyme expression alterations in the human liver Abstract Abstract Objective: Implications of obesity extend beyond the association with various health conditions, impacting physiological changes that affect the liver and the activity of metabolizing enzymes. Given the prevalence of ob...
PMC10130658
core_pubmed_pmc
Sinapis Semen: A review on phytochemistry, pharmacology, toxicity, analytical methods and pharmacokinetics
Sinapis Semen: A review on phytochemistry, pharmacology, toxicity, analytical methods and pharmacokinetics Abstract Abstract Sinapis Semen (SS), the dried mature seed of Sinapis alba L. and Brassica juncea (L.) Czern. et Coss., is one of the traditional Chinese medicinal materials with a wide range of pharmacological e...
PMC10769996
core_pubmed_pmc
Characterization of the Pharmacokinetics and Mass Balance of a Single Oral Dose of Trofinetide in Healthy Male Subjects
Characterization of the Pharmacokinetics and Mass Balance of a Single Oral Dose of Trofinetide in Healthy Male Subjects Abstract Background and Objective Trofinetide is the first drug to be approved for the treatment of Rett syndrome, a neurodevelopmental disorder. The purpose of the study is to fully characterize the ...
PMC7292816
core_pubmed_pmc
Effective Removal of Dabigatran by Idarucizumab or Hemodialysis: A Physiologically Based Pharmacokinetic Modeling Analysis
Effective Removal of Dabigatran by Idarucizumab or Hemodialysis: A Physiologically Based Pharmacokinetic Modeling Analysis Abstract Abstract Background Application of idarucizumab and hemodialysis are options to reverse the action of the oral anticoagulant dabigatran in emergency situations. Objectives The objectives o...
PMC12228451
core_pubmed_pmc
Development and validation of an innovative approach to estimating FVIII levels and designing personalised doses in the prophylactic treatment of haemophilia A: based on the principle of the two-compartment model
Development and validation of an innovative approach to estimating FVIII levels and designing personalised doses in the prophylactic treatment of haemophilia A: based on the principle of the two-compartment model Abstract Abstract Objective To predict the level at a specified time and design personalised dosing, we pro...
PMC3975707
core_pubmed_pmc
The effect of food on the pharmacokinetics of oral fluralaner in dogs
The effect of food on the pharmacokinetics of oral fluralaner in dogs Abstract Background Fluralaner is a novel systemic ectoparasiticide for dogs providing long-acting flea- and tick-control after a single oral dose. The pharmacokinetics of orally administered drugs may be influenced by feeding. This study investigate...
PMC10535516
core_pubmed_pmc
The Use of Tricaine Methanesulfonate (MS-222) in Asian Seabass ( Lates calcarifer ) at Different Temperatures: Study of Optimal Doses, Minimum Effective Concentration, Blood Biochemistry, Immersion Pharmacokinetics, and Tissue Distributions
The Use of Tricaine Methanesulfonate (MS-222) in Asian Seabass ( Lates calcarifer ) at Different Temperatures: Study of Optimal Doses, Minimum Effective Concentration, Blood Biochemistry, Immersion Pharmacokinetics, and Tissue Distributions Abstract Abstract Simple Summary The optimal use of tricaine methanesulfonate (...
PMC9298630
core_pubmed_pmc
Shenmai-Yin decreased the clearance of nifedipine in rats: The involvement of time-dependent inhibition of nifedipine oxidation
Shenmai-Yin decreased the clearance of nifedipine in rats: The involvement of time-dependent inhibition of nifedipine oxidation Abstract The traditional Chinese herbal formula Shenmai-Yin (SY) and nifedipine have both been used to treat patients with cardiovascular disorders. Nifedipine is primarily oxidized by cytochr...
PMC7076055
core_pubmed_pmc
[ 89 Zr]Zr-cetuximab PET/CT as biomarker for cetuximab monotherapy in patients with RAS wild-type advanced colorectal cancer
[ 89 Zr]Zr-cetuximab PET/CT as biomarker for cetuximab monotherapy in patients with RAS wild-type advanced colorectal cancer Abstract Abstract Purpose One-third of patients with RAS wild-type mCRC do not benefit from anti-EGFR monoclonal antibodies. This might be a result of variable pharmacokinetics and insufficient t...
PMC7499189
core_pubmed_pmc
Importance of Stability Analysis When Using Nonlinear Semimechanistic Models to Describe Drug‐Induced Hematotoxicity
Importance of Stability Analysis When Using Nonlinear Semimechanistic Models to Describe Drug‐Induced Hematotoxicity Abstract Abstract Stability analysis, often overlooked in pharmacometrics, is essential to explore dynamical systems. The model developed by Friberg et al . 1 to describe drug‐induced hematotoxicity is w...
PMC6304248
core_pubmed_pmc
Novel SN38 derivative-based liposome as anticancer prodrug: an in vitro and in vivo study
Novel SN38 derivative-based liposome as anticancer prodrug: an in vitro and in vivo study Abstract Abstract Background Many novel drug delivery systems have been extensively studied to exploit the full therapeutic potential of SN38, which is one of the most potent antitumor analogs of camptothecins (CPTs), whose clinic...
PMC5895137
core_pubmed_pmc
CSL112 (Apolipoprotein A-I [Human]) Enhances Cholesterol Efflux Similarly in Healthy Individuals and Stable Atherosclerotic Disease Patients
CSL112 (Apolipoprotein A-I [Human]) Enhances Cholesterol Efflux Similarly in Healthy Individuals and Stable Atherosclerotic Disease Patients Abstract Supplemental Digital Content is available in the text. Keywords: apolipoproteins, atherosclerosis, clinical trial, coronary disease, high density lipoprotein-1 Abstract O...
PMC4356204
core_pubmed_pmc
Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug
Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug Abstract Objectives Bedaquiline is the first drug of a new class approved for the treatment of TB in decades. Bedaquiline is metabolized by cytochrome P450 (CYP) 3A4 to a less-active M2 metabolite. Its terminal half-life i...
PMC7745756
core_pubmed_pmc
Recommendations for Dosing of Repurposed COVID-19 Medications in Patients with Renal and Hepatic Impairment
Recommendations for Dosing of Repurposed COVID-19 Medications in Patients with Renal and Hepatic Impairment Abstract Introduction In December 2019, an outbreak of a novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) began, resulting in a number of antivirals and immune modulators being repurposed to tre...
PMC6878905
core_pubmed_pmc
Effects of CYP3A4 Polymorphisms on Drug Addiction Risk Among the Chinese Han Population
Effects of CYP3A4 Polymorphisms on Drug Addiction Risk Among the Chinese Han Population Abstract Background: Cytochrome P450 3A4 ( CYP3A4 ) regulates pharmacokinetic and pharmacodynamic interactions during the process of drug absorption and metabolism, suggesting CYP3A4 plays an important role in drug addiction. Howeve...
PMC10337722
core_pubmed_pmc
Barium silicate nanoparticles, an efficient catalyst for one-pot green synthesis of α-benzyl amino coumarin derivatives as potential chemotherapeutic agents †
Barium silicate nanoparticles, an efficient catalyst for one-pot green synthesis of α-benzyl amino coumarin derivatives as potential chemotherapeutic agents † Abstract Abstract A new, simple, and efficient method for synthesis of α-benzyl amino coumarin and its derivatives (1–24) is described via a one-pot, three-compo...
PMC11067698
core_pubmed_pmc
Assessment of Efficacy and Safety of Zagotenemab
Assessment of Efficacy and Safety of Zagotenemab Abstract Abstract Background and Objectives Zagotenemab (LY3303560), a monoclonal antibody that preferentially targets misfolded, extracellular, aggregated tau, was assessed in the PERISCOPE-ALZ phase 2 study to determine its ability to slow cognitive and functional decl...
PMC9894673
core_pubmed_pmc
Pharmacokinetic Alterations Associated with Critical Illness
Pharmacokinetic Alterations Associated with Critical Illness Abstract Abstract Haemodynamic, metabolic, and biochemical derangements in critically ill patients affect drug pharmacokinetics and pharmacodynamics making dose optimisation particularly challenging. Appropriate therapeutic dosing depends on the knowledge of ...
PMC5834087
core_pubmed_pmc
Assessment of nivolumab benefit–risk profile of a 240-mg flat dose relative to a 3-mg/kg dosing regimen in patients with advanced tumors
Assessment of nivolumab benefit–risk profile of a 240-mg flat dose relative to a 3-mg/kg dosing regimen in patients with advanced tumors Abstract Abstract Background Nivolumab 3 mg/kg every 2 weeks (Q2W) has shown benefit versus the standard of care in melanoma, non-small cell lung cancer (NSCLC), and renal cell carcin...
PMC9852958
core_pubmed_pmc
Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses
Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses Abstract According to in vitro and in vivo investigations, firocoxib (FX), a second-generation coxib, is a highly selective COX-2 inhibitor in horses. With a COX-1/COX-2 IC 50 ratio of 643 in horses, FX spares the COX-1 ...
PMC9110059
core_pubmed_pmc
Mechanistic Models of COVID-19: Insights into Disease Progression, Vaccines, and Therapeutics
Mechanistic Models of COVID-19: Insights into Disease Progression, Vaccines, and Therapeutics Abstract Abstract The COVID-19 pandemic has severely impacted health systems and economies worldwide. Significant global efforts are therefore ongoing to improve vaccine efficacies, optimize vaccine deployment, and develop new...
PMC10329699
core_pubmed_pmc
Pharmacokinetics, biodistribution and toxicology of novel cell-penetrating peptides
Pharmacokinetics, biodistribution and toxicology of novel cell-penetrating peptides Abstract Abstract Cell-penetrating peptides (CPPs) have been used in basic and preclinical research in the past 30 years to facilitate drug delivery into target cells. However, translation toward the clinic has not been successful so fa...
PMC11867924
core_pubmed_pmc
Exposure‐Efficacy Analysis and Dopamine D2 Receptor Occupancy in Adults with Schizophrenia after Treatment with the Monthly Intramuscular Injectable Risperidone ISM
Exposure‐Efficacy Analysis and Dopamine D2 Receptor Occupancy in Adults with Schizophrenia after Treatment with the Monthly Intramuscular Injectable Risperidone ISM Abstract Abstract Dopamine D2 receptor occupancy (D2RO) significantly influences the clinical effectiveness and safety of many antipsychotic drugs. Maintai...
PMC9239973
core_pubmed_pmc
Vitamin K1 inhibits ferroptosis and counteracts a detrimental effect of phenprocoumon in experimental acute kidney injury
Vitamin K1 inhibits ferroptosis and counteracts a detrimental effect of phenprocoumon in experimental acute kidney injury Abstract Ferroptosis, a type of iron-dependent programmed cell death distinct from apoptosis, necroptosis, and other types of cell death, is characterized by lipid peroxidation, reactive oxygen spec...
PMC10482275
core_pubmed_pmc
Pharmacokinetics of Moxidectin combined with Albendazole or Albendazole plus Diethylcarbamazine for Bancroftian Filariasis
Pharmacokinetics of Moxidectin combined with Albendazole or Albendazole plus Diethylcarbamazine for Bancroftian Filariasis Abstract Abstract Moxidectin (MOX) is a milbemycin endectocide recently approved by the U.S. FDA for the treatment of onchocerciasis in persons at least 12 years of age. MOX has been shown to have ...
PMC10720512
core_pubmed_pmc
Semi-mechanistic population pharmacokinetic/pharmacodynamic modeling of a Plasmodium elongation factor 2 inhibitor cabamiquine for prevention and cure of malaria
Semi-mechanistic population pharmacokinetic/pharmacodynamic modeling of a Plasmodium elongation factor 2 inhibitor cabamiquine for prevention and cure of malaria Abstract ABSTRACT Cabamiquine is a novel antimalarial agent that demonstrates the potential for chemoprevention and treatment of malaria. In this article, the...
PMC6272970
core_pubmed_pmc
Natural Deep Eutectic Solvents (NADES) as a Tool for Bioavailability Improvement: Pharmacokinetics of Rutin Dissolved in Proline/Glycine after Oral Administration in Rats: Possible Application in Nutraceuticals
Natural Deep Eutectic Solvents (NADES) as a Tool for Bioavailability Improvement: Pharmacokinetics of Rutin Dissolved in Proline/Glycine after Oral Administration in Rats: Possible Application in Nutraceuticals Abstract There is a need for innovation in plant-derived pharmaceuticals, food supplements and nutraceutical ...
PMC11043595
core_pubmed_pmc
In vitro pharmacokinetics/pharmacodynamics of FL058 (a novel beta-lactamase inhibitor) combined with meropenem against carbapenemase-producing Enterobacterales
In vitro pharmacokinetics/pharmacodynamics of FL058 (a novel beta-lactamase inhibitor) combined with meropenem against carbapenemase-producing Enterobacterales Abstract Objective: FL058 is a novel beta-lactamase inhibitor with a broad spectrum of activity and a favorable safety profile. The objective of this study was ...
PMC11207335
core_pubmed_pmc
In Vitro Metabolism and Transport Characteristics of Zastaprazan
In Vitro Metabolism and Transport Characteristics of Zastaprazan Abstract Zastaprazan (JP-1366), a novel potassium-competitive acid blocker, is a new drug for the treatment of erosive esophagitis. JP-1366 is highly metabolized in human, mouse, and dog hepatocytes but moderately metabolized in rat and monkey hepatocytes...
PMC3032523
core_pubmed_pmc
Potent antitumoral activity of TRAIL through generation of tumor-targeted single-chain fusion proteins
Potent antitumoral activity of TRAIL through generation of tumor-targeted single-chain fusion proteins Abstract Abstract In an attempt to improve TRAIL's (tumor necrosis factor-related apoptosis-inducing ligand) tumor selective activity a variant was designed, in which the three TRAIL protomers are expressed as a singl...
PMC7728716
core_pubmed_pmc
Pharmacokinetics and Tissue Levels of Pantoprazole in Neonatal Calves After Intravenous Administration
Pharmacokinetics and Tissue Levels of Pantoprazole in Neonatal Calves After Intravenous Administration Abstract Abstract Background: Neonatal calves are at risk of developing abomasal ulceration, but there is a lack of pharmacokinetic data for potential anti-ulcerative therapies, such as pantoprazole, in ruminant speci...
PMC4702416
core_pubmed_pmc
Randomized, active-controlled, comparative phase 3 efficacy and safety equivalence trial of Ovaleap® (recombinant human follicle-stimulating hormone) in infertile women using assisted reproduction technology (ART)
Randomized, active-controlled, comparative phase 3 efficacy and safety equivalence trial of Ovaleap® (recombinant human follicle-stimulating hormone) in infertile women using assisted reproduction technology (ART) Abstract Abstract Background Pharmacokinetic studies with XM17 (Ovaleap®), a recombinant human follicle-st...
PMC3047975
core_pubmed_pmc
Pharmacology, efficacy and safety of liraglutide in the management of type 2 diabetes
Pharmacology, efficacy and safety of liraglutide in the management of type 2 diabetes Abstract Liraglutide is a glucagon-like peptide-1 analog with pharmacokinetic properties suitable for once-daily administration approved by the Food and Drug Administration for the treatment of patients with type 2 diabetes. Clinical ...
PMC12715044
core_pubmed_pmc
Spatial Pharmacokinetic and Pharmacodynamic Modeling in Airway Mucus
Spatial Pharmacokinetic and Pharmacodynamic Modeling in Airway Mucus Abstract Background and Objectives Diseases such as cystic fibrosis (CF) and non-CF bronchiectasis can cause extensive mucus formation in the lung, which may affect drug distribution and effects. As such, quantitative understanding of drug distributio...
PMC7371857
core_pubmed_pmc
Modeling Pathway Dynamics of the Skeletal Muscle Response to Intravenous Methylprednisolone (MPL) Administration in Rats: Dosing and Tissue Effects
Modeling Pathway Dynamics of the Skeletal Muscle Response to Intravenous Methylprednisolone (MPL) Administration in Rats: Dosing and Tissue Effects Abstract Abstract A model-based approach for the assessment of pathway dynamics is explored to characterize metabolic and signaling pathway activity changes characteristic ...
PMC8866227
core_pubmed_pmc
Losartan Blocks Osteosarcoma-Elicited Monocyte Recruitment, and Combined With the Kinase Inhibitor Toceranib, Exerts Significant Clinical Benefit in Canine Metastatic Osteosarcoma
Losartan Blocks Osteosarcoma-Elicited Monocyte Recruitment, and Combined With the Kinase Inhibitor Toceranib, Exerts Significant Clinical Benefit in Canine Metastatic Osteosarcoma Abstract Abstract Purpose: There is increasing recognition that progress in immuno-oncology could be accelerated by evaluating immune-based ...
PMC6611044
core_pubmed_pmc
Pharmacokinetic analysis of new synthetic antimalarial N-251
Pharmacokinetic analysis of new synthetic antimalarial N-251 Abstract Abstract Background With the emergence and growing number of drug-resistant Plasmodium falciparum , a new drug for malaria control must be urgently developed. The new antimalarial synthetic compound N-251 was recently discovered. As an endoperoxide s...
PMC5999140
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Evolocumab, a PCSK9 Inhibitor
Clinical Pharmacokinetics and Pharmacodynamics of Evolocumab, a PCSK9 Inhibitor Abstract Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) increases plasma low-density lipoprotein cholesterol (LDL-C) by decreasing expression of the LDL receptor on hepatic cells. Evolocumab is a human monoclonal immunoglobu...
PMC9325164
core_pubmed_pmc
Perspectives of Positively Charged Nanocrystals of Tedizolid Phosphate as a Topical Ocular Application in Rabbits
Perspectives of Positively Charged Nanocrystals of Tedizolid Phosphate as a Topical Ocular Application in Rabbits Abstract The aim of this study was the successful utilization of the positively charged nanocrystals (NCs) of Tedizolid Phosphate (TZP) (0.1% w / v ) for topical ocular applications. TZP belongs to the 1, 3...
PMC11972901
core_pubmed_pmc
Minocycline Susceptibility of Carbapenem-Resistant Acinetobacter baumannii Blood Isolates from a Single Center in Korea: Role of tetB in Resistance
Minocycline Susceptibility of Carbapenem-Resistant Acinetobacter baumannii Blood Isolates from a Single Center in Korea: Role of tetB in Resistance Abstract Background Carbapenem-resistant Acinetobacter baumannii (CRAB) represents a devastating and growing global threat, calling for new antibiotic treatments. In Korea,...
PMC4338135
core_pubmed_pmc
Ozanezumab Dose Selection for Amyotrophic Lateral Sclerosis by Pharmacokinetic-Pharmacodynamic Modelling of Immunohistochemistry Data from Patient Muscle Biopsies
Ozanezumab Dose Selection for Amyotrophic Lateral Sclerosis by Pharmacokinetic-Pharmacodynamic Modelling of Immunohistochemistry Data from Patient Muscle Biopsies Abstract Amyotrophic Lateral Sclerosis (ALS) is a rare and fatal neurodegenerative disease with a high unmet medical need. In this context, a potential thera...
PMC6458767
core_pubmed_pmc
Transcriptional changes in response to ketamine ester-analogs SN 35210 and SN 35563 in the rat brain
Transcriptional changes in response to ketamine ester-analogs SN 35210 and SN 35563 in the rat brain Abstract Abstract Background Ketamine ester analogs, SN 35210 and SN 35563, demonstrate different pharmacological profiles to ketamine in animal models. Both confer hypnosis with predictably rapid offset yet, paradoxica...
PMC8300337
core_pubmed_pmc
Nonlinear Mixed-Effect Pharmacokinetic Modeling and Distribution of Doxycycline in Healthy Female Donkeys after Multiple Intragastric Dosing–Preliminary Investigation
Nonlinear Mixed-Effect Pharmacokinetic Modeling and Distribution of Doxycycline in Healthy Female Donkeys after Multiple Intragastric Dosing–Preliminary Investigation Abstract Simple Summary Rational use of antibiotic is of most importance for human and animal health. Donkeys have differences in metabolism compared to ...
PMC2984539
core_pubmed_pmc
How pharmacokinetic and pharmacodynamic principles pave the way for optimal basal insulin therapy in type 2 diabetes
How pharmacokinetic and pharmacodynamic principles pave the way for optimal basal insulin therapy in type 2 diabetes Abstract This pedagogical review illustrates the differences between pharmacokinetic (PK) and pharmacodynamic (PD) measures, using insulin therapy as the primary example. The main conclusion is that PD p...
PMC12382683
core_pubmed_pmc
Pharmacokinetics of Tolfenamic Acid Administered Orally and Intravenously at Different Doses in Pekin Ducks ( Anas platyrhynchos domestica )
Pharmacokinetics of Tolfenamic Acid Administered Orally and Intravenously at Different Doses in Pekin Ducks ( Anas platyrhynchos domestica ) Abstract Simple Summary This study examined how tolfenamic acid behaves in Pekin ducks when given either intravenously or orally at different doses. The key findings showed that w...
PMC8880217
core_pubmed_pmc
Model-Based Equivalent Dose Optimization to Develop New Donepezil Patch Formulation
Model-Based Equivalent Dose Optimization to Develop New Donepezil Patch Formulation Abstract Abstract Donepezil patch was developed to replace the original oral formulation. To accurately describe the pharmacokinetics of donepezil and investigate compatible doses between two formulations, a population pharmacokinetic m...
PMC3931386
core_pubmed_pmc
The Pharmacogenetics of Type 2 Diabetes: A Systematic Review
The Pharmacogenetics of Type 2 Diabetes: A Systematic Review Abstract Abstract OBJECTIVE We performed a systematic review to identify which genetic variants predict response to diabetes medications. RESEARCH DESIGN AND METHODS We performed a search of electronic databases (PubMed, EMBASE, and Cochrane Database) and a m...
PMC9144241
core_pubmed_pmc
Cannabidiol and Cannabidiol Metabolites: Pharmacokinetics, Interaction with Food, and Influence on Liver Function
Cannabidiol and Cannabidiol Metabolites: Pharmacokinetics, Interaction with Food, and Influence on Liver Function Abstract Cannabidiol (CBD) is widely available and marketed as having therapeutic properties. Over-the-counter CBD is unregulated, many of the therapeutic claims lack scientific support, and controversy exi...
PMC10188378
core_pubmed_pmc
Ustekinumab Trough Concentrations Are Associated with Biochemical Outcomes in Patients with Crohn’s Disease
Ustekinumab Trough Concentrations Are Associated with Biochemical Outcomes in Patients with Crohn’s Disease Abstract Objective It is unknown whether ustekinumab (UST) levels can predict clinical outcomes in Crohn’s disease (CD) patients. We assessed the exposure–response relationship of UST trough concentrations with b...
PMC11934747
core_pubmed_pmc
Pharmacokinetics of post-transplant cyclophosphamide and its associations with clinical outcomes in pediatric haploidentical hematopoietic stem cell transplantation
Pharmacokinetics of post-transplant cyclophosphamide and its associations with clinical outcomes in pediatric haploidentical hematopoietic stem cell transplantation Abstract Abstract Background Post-transplantation cyclophosphamide (PTCy) has paved the way for the increased use of alternative donors, including haploide...
PMC4213378
core_pubmed_pmc
Pharmacokinetics and Efficacy of the Spleen Tyrosine Kinase Inhibitor R406 after Ocular Delivery for Retinoblastoma
Pharmacokinetics and Efficacy of the Spleen Tyrosine Kinase Inhibitor R406 after Ocular Delivery for Retinoblastoma Abstract Purpose Retinoblastoma is a childhood cancer of the retina. Clinical trials have shown that local delivery of broad spectrum chemotherapeutic agents is efficacious. Recent studies characterizing ...
PMC9704759
core_pubmed_pmc
Dosing time optimization of antihypertensive medications by including the circadian rhythm in pharmacokinetic-pharmacodynamic models
Dosing time optimization of antihypertensive medications by including the circadian rhythm in pharmacokinetic-pharmacodynamic models Abstract Abstract Blood pressure (BP) follows a circadian variation, increasing during active hours, showing a small postprandial valley and a deeper decrease during sleep. Nighttime redu...
PMC7690806
core_pubmed_pmc
Formulation and Nanotechnology-Based Approaches for Solubility and Bioavailability Enhancement of Zerumbone
Formulation and Nanotechnology-Based Approaches for Solubility and Bioavailability Enhancement of Zerumbone Abstract About 40–70% of drug molecules in the clinical development pipeline suffer from one of either low aqueous solubility, poor absorption, or extremely low bioavailability. Approximately 75% of the world pop...
PMC10008152
core_pubmed_pmc
Intravenously administered interleukin-7 to reverse lymphopenia in patients with septic shock: a double-blind, randomized, placebo-controlled trial
Intravenously administered interleukin-7 to reverse lymphopenia in patients with septic shock: a double-blind, randomized, placebo-controlled trial Abstract Abstract Background Profound lymphopenia is an independent predictor of adverse clinical outcomes in sepsis. Interleukin-7 (IL-7) is essential for lymphocyte proli...
PMC5420810
core_pubmed_pmc
Screening of conventional anticonvulsants in a genetic mouse model of epilepsy
Screening of conventional anticonvulsants in a genetic mouse model of epilepsy Abstract Abstract Objective Epilepsy is a common neurological disorder that affects 1% of the population. Approximately, 30% of individuals with epilepsy are refractory to treatment, highlighting the need for novel therapies. Conventional an...
PMC3986720
core_pubmed_pmc
Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice
Induction of Drug Transporters Alters Disposition of Risperidone - A Study in Mice Abstract Abstract Pharmacokinetic interactions, e.g. modulation of drug transporters like P-glycoprotein at the blood-brain barrier, can be a reason for treatment non-response. This study focuses on the influence of induction of drug tra...
PMC6497258
core_pubmed_pmc
Empirical models for anatomical and physiological changes in a human mother and fetus during pregnancy and gestation
Empirical models for anatomical and physiological changes in a human mother and fetus during pregnancy and gestation Abstract Abstract Many parameters treated as constants in traditional physiologically based pharmacokinetic models must be formulated as time-varying quantities when modeling pregnancy and gestation due ...
PMC7993257
core_pubmed_pmc
Predicting Resolvin D1 Pharmacokinetics in Humans with Physiologically‐Based Pharmacokinetic Modeling
Predicting Resolvin D1 Pharmacokinetics in Humans with Physiologically‐Based Pharmacokinetic Modeling Abstract Sjögren’s syndrome (SS) is an autoimmune disease with no effective treatment options. Resolvin D1 (RvD1) belongs to a class of lipid‐based specialized pro‐resolving mediators that showed efficacy in preclinica...
PMC9796419
core_pubmed_pmc
Effect Compartment Model for the Evaluation of Tolerance to Psychological Highness Following Smoking Marijuana
Effect Compartment Model for the Evaluation of Tolerance to Psychological Highness Following Smoking Marijuana Abstract Abstract The purpose of this study is to evaluate the development of tolerance, using a population modeling approach, in recreational marijuana users after acute pulmonary administration of tetrahydro...
PMC5354739
core_pubmed_pmc
Pharmacogenetic analysis of high-dose methotrexate treatment in children with osteosarcoma
Pharmacogenetic analysis of high-dose methotrexate treatment in children with osteosarcoma Abstract Inter-individual differences in toxic symptoms and pharmacokinetics of high-dose methotrexate (MTX) treatment may be caused by genetic variants in the MTX pathway. Correlations between polymorphisms and pharmacokinetic p...
PMC11645446
core_pubmed_pmc
Pharmacokinetic study of polymyxin B in healthy subjects and subjects with renal insufficiency
Pharmacokinetic study of polymyxin B in healthy subjects and subjects with renal insufficiency Abstract Abstract Polymyxin B is a viable option for treating antibiotic‐resistant infections; however, current data on its pharmacokinetics, particularly in patients with renal insufficiency, remain inconclusive and necessit...
PMC9780658
core_pubmed_pmc
Safety of oral nemonoxacin: A systematic review of clinical trials and postmarketing surveillance
Safety of oral nemonoxacin: A systematic review of clinical trials and postmarketing surveillance Abstract Abstract Background: Postmarketing safety analysis is an effective supplement for new drugs in clinical practice. Therefore, we aimed to systematically assess the safety of oral nemonoxacin malate, the first appro...
PMC10747454
core_pubmed_pmc
The Complexity of Bariatric Patient’s Pharmacotherapy: Sildenafil Biopharmaceutics and Pharmacokinetics before vs. after Gastric Sleeve/Bypass
The Complexity of Bariatric Patient’s Pharmacotherapy: Sildenafil Biopharmaceutics and Pharmacokinetics before vs. after Gastric Sleeve/Bypass Abstract Abstract Postbariatric altered gastrointestinal (GI) anatomy/physiology may significantly harm oral drug absorption and overall bioavailability. In this work, sildenafi...
PMC11685455
core_pubmed_pmc
Computational biology assisted exploration of phytochemicals derived natural inhibitors to block BZLF1 gene activation of Epstein–Bar virus in host
Computational biology assisted exploration of phytochemicals derived natural inhibitors to block BZLF1 gene activation of Epstein–Bar virus in host Abstract Abstract The Epstein–Barr virus (EBV) is widespread and has been related to a variety of malignancies as well as infectious mononucleosis. Despite the lack of a va...
PMC6656941
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Modeling of Fluconazole Using Plasma and Cerebrospinal Fluid Samples From Preterm and Term Infants
Physiologically‐Based Pharmacokinetic Modeling of Fluconazole Using Plasma and Cerebrospinal Fluid Samples From Preterm and Term Infants Abstract Abstract Fluconazole is used to treat hematogenous Candida meningoencephalitis in preterm and term infants. To characterize plasma and central nervous system exposure, an adu...
PMC7195756
core_pubmed_pmc
Niosomes of active Fumaria officinalis phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action
Niosomes of active Fumaria officinalis phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action Abstract Background Fumaria officinalis ( F. officinalis, FO) has been used in many inflammatory and painful-ailments. The main aim of this work is to perform an in-depth bio-guided...
PMC12655709
core_pubmed_pmc
Artificial Intelligence (AI) in Pharmaceutical Formulation and Dosage Calculations
Artificial Intelligence (AI) in Pharmaceutical Formulation and Dosage Calculations Abstract Artificial intelligence (AI) is reforming pharmaceutical sciences by renovating traditional drug formulation and dosage calculation approaches. This review provides a comprehensive overview of how AI technologies, such as machin...
PMC5620576
core_pubmed_pmc
Pharmacokinetic and Toxicodynamic Characterization of a Novel Doxorubicin Derivative
Pharmacokinetic and Toxicodynamic Characterization of a Novel Doxorubicin Derivative Abstract Doxorubicin (Dox) is an effective anti-cancer medication with poor oral bioavailability and systemic toxicities. DoxQ was developed by conjugating Dox to the lymphatically absorbed antioxidant quercetin to improve Dox’s bioava...
PMC3082021
core_pubmed_pmc
Increasing tumoral 5-fluorouracil concentrations during a 5-day continuous infusion: a microdialysis study
Increasing tumoral 5-fluorouracil concentrations during a 5-day continuous infusion: a microdialysis study Abstract Abstract Purpose Response to anticancer therapy is believed to be directly related to the concentration of the anticancer drug in the tumor itself. Assessment of intra-tumor drug pharmacokinetics can be h...
PMC3609526
core_pubmed_pmc
Enhanced Absorption of Insulin Aspart as the Result of a Dispersed Injection Strategy Tested in a Randomized Trial in Type 1 Diabetic Patients
Enhanced Absorption of Insulin Aspart as the Result of a Dispersed Injection Strategy Tested in a Randomized Trial in Type 1 Diabetic Patients Abstract Abstract OBJECTIVE We investigated the impact of two different injection strategies on the pharmacokinetics and pharmacodynamics of insulin aspart in vivo in an open-la...
PMC6522576
core_pubmed_pmc
Teaching an Old Class New Tricks: A Novel Semi-Synthetic Aminoglycoside, Plazomicin
Teaching an Old Class New Tricks: A Novel Semi-Synthetic Aminoglycoside, Plazomicin Abstract The emergence of multi-drug resistant (MDR) Gram-negative pathogens has become a serious worldwide health concern. Gram-negative bacteria such as Enterobacteriaceae ( Klebsiella pneumoniae , Escherichia coli , Enterobacter spp....
PMC11944414
core_pubmed_pmc
Leveraging Omeprazole PBPK/PD Modeling to Inform Drug–Drug Interactions and Specific Recommendations for Pediatric Labeling
Leveraging Omeprazole PBPK/PD Modeling to Inform Drug–Drug Interactions and Specific Recommendations for Pediatric Labeling Abstract Background/Objectives: Omeprazole is widely used for managing gastrointestinal disorders like GERD, ulcers, and H. pylori infections. However, its use in pediatrics presents challenges du...
PMC9111087
core_pubmed_pmc
Quantitative methods and modeling to assess COVID‐19‐interrupted in vivo pharmacokinetic bioequivalence studies with two reference batches
Quantitative methods and modeling to assess COVID‐19‐interrupted in vivo pharmacokinetic bioequivalence studies with two reference batches Abstract Abstract The coronavirus disease 2019 (COVID‐19) has presented unprecedented challenges to the generic drug development, including interruptions in bioequivalence (BE) stud...
PMC11971949
core_pubmed_pmc
Optimizing Tacrolimus Dosing During Hospitalization After Kidney Transplantation: A Comparative Model Analysis
Optimizing Tacrolimus Dosing During Hospitalization After Kidney Transplantation: A Comparative Model Analysis Abstract Background The optimization of tacrolimus dosing during the early postoperative hospitalization period is essential to prevent rejection, minimize nephrotoxicity, and minimize the risk of opportunisti...
PMC5897417
core_pubmed_pmc
Comparative Pharmacokinetics of Gallic Acid After Oral Administration of Gallic Acid Monohydrate in Normal and Isoproterenol-Induced Myocardial Infarcted Rats
Comparative Pharmacokinetics of Gallic Acid After Oral Administration of Gallic Acid Monohydrate in Normal and Isoproterenol-Induced Myocardial Infarcted Rats Abstract Gallic acid (GA) is a polyphenolic natural product widely distributed in food, beverage, and traditional Chinese herbs with beneficial effects on the ca...
PMC6512037
core_pubmed_pmc
Evaluation of the Effects of Astragalus membranaceus on the Pharmacokinetics of Pemetrexed Disodium and Gemcitabine in Rats by a Simple High-Performance Liquid Chromatography/UV Method
Evaluation of the Effects of Astragalus membranaceus on the Pharmacokinetics of Pemetrexed Disodium and Gemcitabine in Rats by a Simple High-Performance Liquid Chromatography/UV Method Abstract Abstract Combination therapy is opted as a potential therapeutic strategy for cancer treatment. Astragalus membranaceus combin...
PMC12816657
core_pubmed_pmc
Hyaluronic acid capped cubosomes co-loaded with antitumor agents towards the treatment of colorectal cancer
Hyaluronic acid capped cubosomes co-loaded with antitumor agents towards the treatment of colorectal cancer Abstract Abstract Colorectal cancer (CRC) is the 3rd most lethal type of cancer-linked deaths worldwide. Combination chemotherapy offers a better therapeutic response against CRC than single drug therapy. The pur...
PMC8391092
core_pubmed_pmc
Effect of Obesity on Clinical Failure of Patients Treated With β-Lactams
Effect of Obesity on Clinical Failure of Patients Treated With β-Lactams Abstract Abstract Background Altered pharmacokinetics in obese patients raise concerns over worse clinical outcomes. This study assessed whether obese patients receiving a β-lactam have worse clinical outcomes compared to nonobese patients and to ...
PMC5104339
core_pubmed_pmc
Model Linking Plasma and Intracellular Tenofovir/Emtricitabine with Deoxynucleoside Triphosphates
Model Linking Plasma and Intracellular Tenofovir/Emtricitabine with Deoxynucleoside Triphosphates Abstract The coformulation of the nucleos(t)ide analogs (NA) tenofovir (TFV) disoproxil fumarate (TDF) and emtricitabine (FTC) is approved for HIV-infection treatment and prevention. Plasma TFV and FTC undergo complicated ...
PMC5833774
core_pubmed_pmc
Pharmacokinetics, distribution and anti-tumor efficacy of liposomal mitoxantrone modified with a luteinizing hormone-releasing hormone receptor-specific peptide
Pharmacokinetics, distribution and anti-tumor efficacy of liposomal mitoxantrone modified with a luteinizing hormone-releasing hormone receptor-specific peptide Abstract Abstract Background A previous study developed a novel luteinizing hormone-releasing hormone (LHRH) receptor-targeted liposome. The aim of this study ...