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PMC9545191
core_pubmed_pmc
Dapagliflozin Pharmacokinetics Is Similar in Adults With Type 1 and Type 2 Diabetes Mellitus
Dapagliflozin Pharmacokinetics Is Similar in Adults With Type 1 and Type 2 Diabetes Mellitus Abstract Abstract Dapagliflozin improves glycemic control in patients with type 2 diabetes mellitus (T2DM) and is approved in Japanese patients with type 1 diabetes mellitus (T1DM) with inadequate glycemic control. The objectiv...
PMC9045325
core_pubmed_pmc
Fluconazole Population Pharmacokinetics after Fosfluconazole Administration and Dosing Optimization in Extremely Low-Birth-Weight Infants
Fluconazole Population Pharmacokinetics after Fosfluconazole Administration and Dosing Optimization in Extremely Low-Birth-Weight Infants Abstract ABSTRACT A prospective single-center study was conducted to characterize the pharmacokinetics (PK) of fluconazole (FLCZ) in extremely low-birth-weight infants (ELBWIs) who r...
PMC6704567
core_pubmed_pmc
Anti-PD-1 monoclonal antibody MEDI0680 in a phase I study of patients with advanced solid malignancies
Anti-PD-1 monoclonal antibody MEDI0680 in a phase I study of patients with advanced solid malignancies Abstract Background The safety, efficacy, pharmacokinetics, and pharmacodynamics of the anti-programmed cell death-1 antibody MEDI0680 were evaluated in a phase I, multicenter, dose-escalation study in advanced solid ...
PMC7894400
core_pubmed_pmc
Population pharmacokinetic model with time‐varying clearance for lorlatinib using pooled data from patients with non‐small cell lung cancer and healthy participants
Population pharmacokinetic model with time‐varying clearance for lorlatinib using pooled data from patients with non‐small cell lung cancer and healthy participants Abstract Abstract Lorlatinib, a selective inhibitor of anaplastic lymphoma kinase (ALK) and c‐ROS oncogene 1 (ROS1) tyrosine kinase, is indicated for the t...
PMC9474582
core_pubmed_pmc
Model-informed approach for risk management of bleeding toxicities for bintrafusp alfa, a bifunctional fusion protein targeting TGF-β and PD-L1
Model-informed approach for risk management of bleeding toxicities for bintrafusp alfa, a bifunctional fusion protein targeting TGF-β and PD-L1 Abstract Abstract Purpose Bintrafusp alfa (BA) is a bifunctional fusion protein composed of the extracellular domain of the transforming growth factor-β (TGF-β) receptor II fus...
PMC10020863
core_pubmed_pmc
Project Optimus, an FDA initiative: Considerations for cancer drug development internationally, from an academic perspective
Project Optimus, an FDA initiative: Considerations for cancer drug development internationally, from an academic perspective Abstract Modern cancer therapeutics are increasingly targeted, bringing the promise of new and improved activity, alongside better tolerability. However, while many are indeed resulting in dramat...
PMC8663962
core_pubmed_pmc
Pharmacogenomics and circadian rhythms as mediators of cardiovascular drug-drug interactions
Pharmacogenomics and circadian rhythms as mediators of cardiovascular drug-drug interactions Abstract Abstract This article summarizes the current literature and documents new evidence concerning drug-drug interactions (DDI) stemming from pharmacogenomic and circadian rhythm determinants of therapies used to treat comm...
PMC6539080
core_pubmed_pmc
Simultaneous Determination and Pharmacokinetic Characterization of Glycyrrhizin, Isoliquiritigenin, Liquiritigenin, and Liquiritin in Rat Plasma Following Oral Administration of Glycyrrhizae Radix Extract
Simultaneous Determination and Pharmacokinetic Characterization of Glycyrrhizin, Isoliquiritigenin, Liquiritigenin, and Liquiritin in Rat Plasma Following Oral Administration of Glycyrrhizae Radix Extract Abstract Abstract Glycyrrhizae Radix is widely used as herbal medicine and is effective against inflammation, vario...
PMC9695821
core_pubmed_pmc
Synthesis and Evaluation of NF-κB Inhibitory Activity of Mollugin Derivatives
Synthesis and Evaluation of NF-κB Inhibitory Activity of Mollugin Derivatives Abstract Abstract (1) Background: Nuclear factor κB (NF-κB) is an important transcriptional regulator that regulates the inflammatory pathway and plays a key role in cellular inflammatory and immune responses. The presence of a high concentra...
PMC11835428
core_pubmed_pmc
Semimechanistic Population PK/PD Modeling of Axatilimab in Healthy Participants and Patients With Solid Tumors or Chronic Graft‐Versus‐Host Disease
Semimechanistic Population PK/PD Modeling of Axatilimab in Healthy Participants and Patients With Solid Tumors or Chronic Graft‐Versus‐Host Disease Abstract Axatilimab, a high‐affinity humanized immunoglobulin G4 monoclonal antibody against colony‐stimulating factor 1 receptor (CSF‐1R), is approved for the treatment of...
PMC5351340
core_pubmed_pmc
The Pharmacokinetic Exposure to Fexofenadine is Volume‐Dependently Reduced in Healthy Subjects Following Oral Administration With Apple Juice
The Pharmacokinetic Exposure to Fexofenadine is Volume‐Dependently Reduced in Healthy Subjects Following Oral Administration With Apple Juice Abstract Abstract Pharmacokinetic exposures to fexofenadine (FEX) are reduced by apple juice (AJ); however, the relationship between the AJ volume and the degree of AJ‐FEX intera...
PMC8698904
core_pubmed_pmc
Drug Delivery Challenges in Brain Disorders across the Blood–Brain Barrier: Novel Methods and Future Considerations for Improved Therapy
Drug Delivery Challenges in Brain Disorders across the Blood–Brain Barrier: Novel Methods and Future Considerations for Improved Therapy Abstract Abstract Due to the physiological and structural properties of the blood–brain barrier (BBB), the delivery of drugs to the brain poses a unique challenge in patients with cen...
PMC10747608
core_pubmed_pmc
Bovine Serum Albumin Nanoparticles Enhanced the Intranasal Bioavailability of Silybin in Rats
Bovine Serum Albumin Nanoparticles Enhanced the Intranasal Bioavailability of Silybin in Rats Abstract Abstract Silybin (SLB), an important flavonoid from silymarin, displays significant hepatoprotective, anticancer, antioxidant, and neuroprotective effects. However, its therapeutic efficacy is limited by its low solub...
PMC9405042
core_pubmed_pmc
Pharmacodynamics of Flucloxacillin in a Neutropenic Murine Thigh Infection Model: A Piece of the Puzzle towards Evidence-Based Dosing
Pharmacodynamics of Flucloxacillin in a Neutropenic Murine Thigh Infection Model: A Piece of the Puzzle towards Evidence-Based Dosing Abstract For decades, flucloxacillin has been used to treat methicillin-susceptible Staphylococcus aureus (MSSA). Little is still known about its pharmacodynamics (PD). The present study...
PMC5763286
core_pubmed_pmc
Constraint-based perturbation analysis with cluster Newton method: a case study of personalized parameter estimations with irinotecan whole-body physiologically based pharmacokinetic model
Constraint-based perturbation analysis with cluster Newton method: a case study of personalized parameter estimations with irinotecan whole-body physiologically based pharmacokinetic model Abstract Background Drug development considering individual varieties among patients becomes crucial to improve clinical developmen...
PMC11851067
core_pubmed_pmc
An open-label Phase 2a study to assess the safety and tolerability of trimetazidine in patients with amyotrophic lateral sclerosis
An open-label Phase 2a study to assess the safety and tolerability of trimetazidine in patients with amyotrophic lateral sclerosis Abstract Abstract Metabolic imbalance is associated with amyotrophic lateral sclerosis progression. Impaired glucose oxidation and increased reliance on fatty acid oxidation contribute to r...
PMC9812024
core_pubmed_pmc
Prediction of the Contribution Ratio of a Target Metabolic Enzyme to Clearance from Chemical Structure Information
Prediction of the Contribution Ratio of a Target Metabolic Enzyme to Clearance from Chemical Structure Information Abstract Abstract The contribution ratio of metabolic enzymes such as cytochrome P450 to in vivo clearance (fraction metabolized: fm) is a pharmacokinetic index that is particularly important for the quant...
PMC12002994
core_pubmed_pmc
Mechanistic intracellular PK/PD modeling to inform development strategies for small interfering RNA therapeutics
Mechanistic intracellular PK/PD modeling to inform development strategies for small interfering RNA therapeutics Abstract Small interfering RNA (siRNA) therapeutics provide a targeted approach to silence disease-related genes, with notable success in liver-targeting applications. However, the quantitative effects of si...
PMC6430159
core_pubmed_pmc
Target‐Mediated Drug Disposition Model for Bispecific Antibodies: Properties, Approximation, and Optimal Dosing Strategy
Target‐Mediated Drug Disposition Model for Bispecific Antibodies: Properties, Approximation, and Optimal Dosing Strategy Abstract Bispecific antibodies (BsAbs) bind to two different targets, and create two binary and one ternary complex ( TC ). These molecules have shown promise as immuno‐oncology drugs, and the TC is ...
PMC11416114
core_pubmed_pmc
Target Attainment and Population Pharmacokinetics of Nirmatrelvir/Ritonavir in Critically Ill Adult Patients
Target Attainment and Population Pharmacokinetics of Nirmatrelvir/Ritonavir in Critically Ill Adult Patients Abstract Background The population pharmacokinetics of nirmatrelvir/ritonavir (NIR/RIT) has not yet been described for critically ill adult patient. Purpose This was a prospective observational population pharma...
PMC11502913
core_pubmed_pmc
A phase 1 dose escalation of pritumumab in patients with refractory or recurrent gliomas or brain metastases
A phase 1 dose escalation of pritumumab in patients with refractory or recurrent gliomas or brain metastases Abstract Abstract Background This phase 1 ( NCT04396717 ) open-label, multicenter study, evaluated Pritumumab, a IgG1 monoclonal antibody, in patients with gliomas and brain metastases. The primary objective was...
PMC11315830
core_pubmed_pmc
Antibody–Drug Conjugates in the Pipeline for Treatment of Melanoma: Target and Pharmacokinetic Considerations
Antibody–Drug Conjugates in the Pipeline for Treatment of Melanoma: Target and Pharmacokinetic Considerations Abstract Abstract Melanoma is an aggressive, rapidly developing form of skin cancer that affects about 22 per 100,000 individuals. Treatment options for melanoma patients are limited and typically involve surgi...
PMC10101109
core_pubmed_pmc
Efficacy of Zidovudine-Amikacin Combination Therapy In Vitro and in a Rat Tissue Cage Infection Model against Amikacin-Resistant, Multidrug-Resistant Enterobacteriales
Efficacy of Zidovudine-Amikacin Combination Therapy In Vitro and in a Rat Tissue Cage Infection Model against Amikacin-Resistant, Multidrug-Resistant Enterobacteriales Abstract ABSTRACT Multidrug-resistant (MDR) Enterobacteriales infections have become an urgent global threat to public health. The aim of this study was...
PMC8305691
core_pubmed_pmc
Pharmacokinetics, Biodistribution, and Biosafety of PEGylated Gold Nanoparticles In Vivo
Pharmacokinetics, Biodistribution, and Biosafety of PEGylated Gold Nanoparticles In Vivo Abstract Abstract Despite the obvious advantages of gold nanoparticles for biomedical applications, controversial and incomplete toxicological data hamper their widespread use. Here, we present the results from an in vivo toxicity ...
PMC9924181
core_pubmed_pmc
Risdiplam in Patients Previously Treated with Other Therapies for Spinal Muscular Atrophy: An Interim Analysis from the JEWELFISH Study
Risdiplam in Patients Previously Treated with Other Therapies for Spinal Muscular Atrophy: An Interim Analysis from the JEWELFISH Study Abstract Abstract Introduction Risdiplam is a survival of motor neuron 2 ( SMN2 ) splicing modifier for the treatment of patients with spinal muscular atrophy (SMA). The JEWELFISH stud...
PMC12942462
core_pubmed_pmc
Envarsus Versus Advagraf in De Novo Kidney Transplant Recipients: A Comparative Pharmacokinetic Study
Envarsus Versus Advagraf in De Novo Kidney Transplant Recipients: A Comparative Pharmacokinetic Study Abstract Abstract Background: Comparative real-world data on the pharmacokinetics of once-daily tacrolimus formulations in de novo kidney transplantation remain limited. We compared tacrolimus exposure and dosing requi...
PMC8013631
core_pubmed_pmc
Efficacy and safety of vancomycin loading doses in critically ill patients with methicillin-resistant Staphylococcus aureus infection
Efficacy and safety of vancomycin loading doses in critically ill patients with methicillin-resistant Staphylococcus aureus infection Abstract Background: While vancomycin loading doses may facilitate earlier pharmacokinetic–pharmacodynamic target attainment, the impact of loading doses on clinical outcomes remains und...
PMC3522110
core_pubmed_pmc
Pharmacokinetics and Relative Bioavailability of Flavonoids between Two Dosage Forms of Gegen-Qinlian-Tang in Rats
Pharmacokinetics and Relative Bioavailability of Flavonoids between Two Dosage Forms of Gegen-Qinlian-Tang in Rats Abstract Abstract Gegen-Qinlian-Tang (GQT), a popular Chinese medicine prescription, consists of Puerariae Radix, Scutellariae Radix, Coptidis Rhizoma, and Glycyrrhizae Radix. This study investigated the p...
PMC12964424
core_pubmed_pmc
Pharmacokinetics and preliminary data on safety of meloxicam subcutaneous extended-release formulation in Sprague–Dawley rats
Pharmacokinetics and preliminary data on safety of meloxicam subcutaneous extended-release formulation in Sprague–Dawley rats Abstract Abstract Introduction Nonsteroidal anti-inflammatory drugs (NSAIDs) play a critical role in managing pain and inflammation in veterinary medicine. Meloxicam, a widely used NSAID, is com...
PMC9401513
core_pubmed_pmc
First-in-Human Study of PF-06647020 (Cofetuzumab Pelidotin), an Antibody–Drug Conjugate Targeting Protein Tyrosine Kinase 7, in Advanced Solid Tumors
First-in-Human Study of PF-06647020 (Cofetuzumab Pelidotin), an Antibody–Drug Conjugate Targeting Protein Tyrosine Kinase 7, in Advanced Solid Tumors Abstract Abstract Purpose: We investigated safety, tolerability, pharmacokinetics, and antitumor activity of the protein tyrosine kinase 7 (PTK7)-targeted, auristatin-bas...
PMC5855550
core_pubmed_pmc
Pharmacokinetic Study of Bioactive Flavonoids in the Traditional Japanese Medicine Keigairengyoto Exerting Antibacterial Effects against Staphylococcus aureus
Pharmacokinetic Study of Bioactive Flavonoids in the Traditional Japanese Medicine Keigairengyoto Exerting Antibacterial Effects against Staphylococcus aureus Abstract Abstract Recent studies have demonstrated that flavonoid glucuronides can be deconjugated to the active form aglycone by β-glucuronidase-expressing macr...
PMC7338818
core_pubmed_pmc
Wide variation in tissue, systemic, and drain fluid exposure after oxaliplatin-based HIPEC: results of the GUTOX study
Wide variation in tissue, systemic, and drain fluid exposure after oxaliplatin-based HIPEC: results of the GUTOX study Abstract Abstract Purpose In this exploratory study, the effect of postprocedural flushing with crystalloids after oxaliplatin-based hyperthermic intraperitoneal chemotherapy (HIPEC) on platinum concen...
PMC12642000
core_pubmed_pmc
Physiologically Based Pharmacokinetic Model for Prediction of Immunoglobulins Exposure in Pregnant Women
Physiologically Based Pharmacokinetic Model for Prediction of Immunoglobulins Exposure in Pregnant Women Abstract Background : Physiologically based pharmacokinetic (PBPK) modeling is applied to address clinical pharmacology issues including dose selection and exposure assessments for special populations (e.g., pediatr...
PMC11975176
core_pubmed_pmc
Lack of Pharmacokinetic Drug–Drug Interactions Between Bepirovirsen and Nucleos(t)ide Analogs
Lack of Pharmacokinetic Drug–Drug Interactions Between Bepirovirsen and Nucleos(t)ide Analogs Abstract Abstract Bepirovirsen is an antisense oligonucleotide currently in Phase 3 development to treat chronic hepatitis B virus (HBV) infection. Given the importance of coadministration of bepirovirsen and standard‐of‐care ...
PMC10302878
core_pubmed_pmc
Long-Acting Opioid Analgesics for Acute Pain: Pharmacokinetic Evidence Reviewed
Long-Acting Opioid Analgesics for Acute Pain: Pharmacokinetic Evidence Reviewed Abstract Simple Summary Pharmacokinetic (PK) studies measure the time for a dose of a drug to reach therapeutic levels in a patient’s blood or tissues. This data provides a simple and precise method to compare the response to drugs made by ...
PMC12353791
core_pubmed_pmc
Targeting the angiopoietin-like protein 3/8 complex with a monoclonal antibody in patients with mixed hyperlipidemia: a phase 1 trial
Targeting the angiopoietin-like protein 3/8 complex with a monoclonal antibody in patients with mixed hyperlipidemia: a phase 1 trial Abstract The angiopoietin-like protein 3/8 complex (ANGPTL3/8) inhibits lipoprotein lipase (LPL) activity, primarily in oxidative tissues, and does so more potently than ANGPTL3, making ...
PMC6188068
core_pubmed_pmc
In situ misemgel as a multifunctional dual-absorption platform for nasal delivery of raloxifene hydrochloride: formulation, characterization, and in vivo performance
In situ misemgel as a multifunctional dual-absorption platform for nasal delivery of raloxifene hydrochloride: formulation, characterization, and in vivo performance Abstract Abstract Background Raloxifene hydrochloride (RLX) is approved by the US Food and Drug Administration for the treatment and prevention of osteopo...
PMC9515533
core_pubmed_pmc
Initial sirolimus dosage recommendations for pediatric patients with PIK3CD mutation-related immunodeficiency disease
Initial sirolimus dosage recommendations for pediatric patients with PIK3CD mutation-related immunodeficiency disease Abstract Abstract Sirolimus is used to treat pediatric patients with PIK3CD mutation-related immunodeficiency disease. However, the initial dosages of sirolimus remain undecided. The present study aims ...
PMC8032623
core_pubmed_pmc
Prediction of the dose range for adverse neurological effects of amiodarone in patients from an in vitro toxicity test by in vitro–in vivo extrapolation
Prediction of the dose range for adverse neurological effects of amiodarone in patients from an in vitro toxicity test by in vitro–in vivo extrapolation Abstract Abstract Amiodarone is an antiarrhythmic agent inducing adverse effects on the nervous system, among others. We applied physiologically based pharmacokinetic ...
PMC10700596
core_pubmed_pmc
Docking for EP4R antagonists active against inflammatory pain
Docking for EP4R antagonists active against inflammatory pain Abstract The lipid prostaglandin E 2 (PGE 2 ) mediates inflammatory pain by activating G protein-coupled receptors, including the prostaglandin E2 receptor 4 (EP4R). Nonsteroidal anti-inflammatory drugs (NSAIDs) reduce nociception by inhibiting prostaglandin...
PMC12764621
core_pubmed_pmc
Predicting the toxicity-efficacy ratio of venetoclax in real-world patients
Predicting the toxicity-efficacy ratio of venetoclax in real-world patients Abstract Abstract This study investigates the pharmacokinetic variability and exposure-response relationships of Venetoclax (VEN) in adult patients with acute myeloid leukemia (AML) who are ineligible for intensive chemotherapy. The study was c...
PMC9805719
core_pubmed_pmc
Pharmacokinetics of a Fixed-Dose Combination of Teneligliptin Hydrochloride Hydrate and Modified-Release Metformin Under Fasting and Fed Conditions in Healthy Subjects
Pharmacokinetics of a Fixed-Dose Combination of Teneligliptin Hydrochloride Hydrate and Modified-Release Metformin Under Fasting and Fed Conditions in Healthy Subjects Abstract Abstract Purpose This study was performed to compare the pharmacokinetics of two fixed-dose combination (FDC) formulations of teneligliptin com...
PMC12868987
core_pubmed_pmc
Anthelmintic Efficacy of Rosemary Oil and Its Nanoemulsion Against the Monogenean Parasite, Zeuxapta seriolae , in Yellowtail Kingfish ( Seriola lalandi )
Anthelmintic Efficacy of Rosemary Oil and Its Nanoemulsion Against the Monogenean Parasite, Zeuxapta seriolae , in Yellowtail Kingfish ( Seriola lalandi ) Abstract This study evaluated the anthelmintic efficacy of rosemary oil delivered as a nanoemulsion compared with regular rosemary oil against the monogenean parasit...
PMC12819339
core_pubmed_pmc
Enhancement of oral bioavailability of risedronate through xyloglucan rafts
Enhancement of oral bioavailability of risedronate through xyloglucan rafts Abstract Bisphosphonates irritate the stomach and oesophagus and have a very limited absorption. The purpose of this study was to increase risedronate (RDN) oral bioavailability by causing a raft to form in the stomach. The creation of a raft p...
PMC12304831
core_pubmed_pmc
Pharmacokinetics of betamethasone in pre‐eclampsia: An in vivo and ex vivo study
Pharmacokinetics of betamethasone in pre‐eclampsia: An in vivo and ex vivo study Abstract Aims To enhance understanding of betamethasone and its metabolites' pharmacokinetics in pregnancy, specifically early‐onset pre‐eclampsia, through a population pharmacokinetic model. Additionally, to investigate the placental meta...
PMC12397115
core_pubmed_pmc
Safety and dosimetry of [ 177 Lu]Lu-DOTA-TATE in adolescent patients with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours, or pheochromocytomas and paragangliomas: Primary analysis of the Phase II NETTER-P study
Safety and dosimetry of [ 177 Lu]Lu-DOTA-TATE in adolescent patients with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours, or pheochromocytomas and paragangliomas: Primary analysis of the Phase II NETTER-P study Abstract Purpose NETTER-P, an open-label Phase II study, evaluated the safety a...
PMC9753331
core_pubmed_pmc
Comparison of the neuromuscular effects of two infusion rates of rocuronium in anesthetized pigs
Comparison of the neuromuscular effects of two infusion rates of rocuronium in anesthetized pigs Abstract Abstract Background: Neuromuscular blocking agents are frequently administered to pigs used for research. In humans, administration of the drugs is not without risk and may result in accidental awareness under gene...
PMC3855985
core_pubmed_pmc
Simultaneous Determination of Volatile Constituents from Acorus tatarinowii Schott in Rat Plasma by Gas Chromatography-Mass Spectrometry with Selective Ion Monitoring and Application in Pharmacokinetic Study
Simultaneous Determination of Volatile Constituents from Acorus tatarinowii Schott in Rat Plasma by Gas Chromatography-Mass Spectrometry with Selective Ion Monitoring and Application in Pharmacokinetic Study Abstract A sensitive and specific gas chromatographic-mass spectrometry with selected ion monitoring (GC-MS/SIM)...
PMC10230557
core_pubmed_pmc
Feasibility study of a clinical decision support system for polymedicated patients in primary care
Feasibility study of a clinical decision support system for polymedicated patients in primary care Abstract Abstract Age‐related changes in pharmacokinetics and pharmacodynamics, multimorbidity, frailty, and cognitive impairment represent challenges for drug treatments. Moreover, older adults are commonly exposed to po...
PMC6835498
core_pubmed_pmc
Pharmacokinetic Study of Bioactive Glycopeptide from Strongylocentrotus droebachiensis After Intranasal Administration to Rats Using Biomarker Approach
Pharmacokinetic Study of Bioactive Glycopeptide from Strongylocentrotus droebachiensis After Intranasal Administration to Rats Using Biomarker Approach Abstract A glycopeptide fraction (GPF) from internal organs of green sea urchins ( Strongylocentrotus droebachiensis Müller, Strongylocentrotidae) has been reported to ...
PMC4831541
core_pubmed_pmc
A Pharmacokinetic and Pharmacodynamic Study on Intravenous Cefazedone Sodium in Patients with Community-acquired Pneumonia
A Pharmacokinetic and Pharmacodynamic Study on Intravenous Cefazedone Sodium in Patients with Community-acquired Pneumonia Abstract Abstract Background: As a time-dependent antibiotic, the time of cefazedone concentration exceeds the minimum inhibitory concentration (MIC) is the key pharmacokinetic-pharmacodynamic (PK-...
PMC6728954
core_pubmed_pmc
Safety of an extended-release injectable moxidectin suspension formulation (ProHeart ® 12) in dogs
Safety of an extended-release injectable moxidectin suspension formulation (ProHeart ® 12) in dogs Abstract Abstract Background The safety of ProHeart® 12 (PH 12; extended-release injectable suspension; 10% moxidectin in glyceryl tristearate microspheres) was evaluated in four studies using Beagle dogs and one study us...
PMC4541546
core_pubmed_pmc
RGD-modified liposomes enhance efficiency of aclacinomycin A delivery: evaluation of their effect in lung cancer
RGD-modified liposomes enhance efficiency of aclacinomycin A delivery: evaluation of their effect in lung cancer Abstract In this study, long-circulating Arg-Gly-Asp (RGD)-modified aclacinomycin A (ACM) liposomes were prepared by thin film hydration method. Their morphology, particle size, encapsulation efficiency, and...
PMC9819214
core_pubmed_pmc
Development and Validation of an Efficient and Highly Sensitive Enzyme-Linked Immunosorbent Assay for Alemtuzumab Quantification in Human Serum and Plasma
Development and Validation of an Efficient and Highly Sensitive Enzyme-Linked Immunosorbent Assay for Alemtuzumab Quantification in Human Serum and Plasma Abstract Supplemental Digital Content is Available in the Text. Background: Alemtuzumab is a humanized monoclonal antibody that targets the CD52 glycoprotein express...
PMC10167634
core_pubmed_pmc
A model-based approach for a practical dosing strategy for the short, intensive treatment regimen for paediatric tuberculous meningitis
A model-based approach for a practical dosing strategy for the short, intensive treatment regimen for paediatric tuberculous meningitis Abstract Following infection with Mycobacterium tuberculosis , young children are at high risk of developing severe forms of tuberculosis (TB) disease, including TB meningitis (TBM), w...
PMC8297997
core_pubmed_pmc
Efficacy, Safety and Tolerability of a New 10% Intravenous Immunoglobulin for the Treatment of Primary Immunodeficiencies
Efficacy, Safety and Tolerability of a New 10% Intravenous Immunoglobulin for the Treatment of Primary Immunodeficiencies Abstract We report here the results of a phase 3 study to assess the efficacy, safety, and tolerability of GC5107, a new 10% liquid intravenous immunoglobulin (IVIG) in preventing serious bacterial ...
PMC4004401
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects
Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects Abstract Aim The aim of the study was to evaluate the pharmacokinetics (PK) of inhaled and intravenous (i.v.) fluticasone furoate (FF) in healthy Caucasian, Chinese, Japanese and Korean subj...
PMC12032411
core_pubmed_pmc
Acute dose-dependent effects and self-guided titration of continuous N,N- dimethyltryptamine infusions in a double-blind placebo-controlled study in healthy participants
Acute dose-dependent effects and self-guided titration of continuous N,N- dimethyltryptamine infusions in a double-blind placebo-controlled study in healthy participants Abstract Abstract N,N -dimethyltryptamine (DMT) is a serotonergic psychedelic that is known for its short-lasting effects when administered intravenou...
PMC7803377
core_pubmed_pmc
Thresholds for post-rebound SHIV control after CCR5 gene-edited autologous hematopoietic cell transplantation
Thresholds for post-rebound SHIV control after CCR5 gene-edited autologous hematopoietic cell transplantation Abstract Autologous, CCR5 gene-edited hematopoietic stem and progenitor cell (HSPC) transplantation is a promising strategy for achieving HIV remission. However, only a fraction of HSPCs can be edited ex vivo t...
PMC11732916
core_pubmed_pmc
Impact of different parametric Patlak imaging approaches and comparison with a 2-tissue compartment pharmacokinetic model with a long axial field-of-view (LAFOV) PET/CT in oncological patients
Impact of different parametric Patlak imaging approaches and comparison with a 2-tissue compartment pharmacokinetic model with a long axial field-of-view (LAFOV) PET/CT in oncological patients Abstract Abstract Aim The recently introduced Long-Axial-Field-of-View (LAFOV) PET-CT scanners allow for the first-time whole-b...
PMC5099547
core_pubmed_pmc
Edoxaban drug–drug interactions with ketoconazole, erythromycin, and cyclosporine
Edoxaban drug–drug interactions with ketoconazole, erythromycin, and cyclosporine Abstract Aims Edoxaban, a novel factor Xa inhibitor, is a substrate of cytochrome P450 3 A4 (CYP3A4) and the efflux transporter P‐glycoprotein (P‐gp). Three edoxaban drug–drug interaction studies examined the effects of P‐gp inhibitors wi...
PMC12736838
core_pubmed_pmc
PopPK and PBPK Models Guide Meropenem Dosing in Critically Ill Children with Augmented Renal Clearance
PopPK and PBPK Models Guide Meropenem Dosing in Critically Ill Children with Augmented Renal Clearance Abstract Abstract Background: Meropenem (MEM) is frequently prescribed for the empirical management of severe infections in the pediatric intensive care unit (PICU). Critically ill children exhibit substantial pharmac...
PMC3733166
core_pubmed_pmc
Stereoselective binding of chiral drugs to plasma proteins
Stereoselective binding of chiral drugs to plasma proteins Abstract Abstract Chiral drugs show distinct biochemical and pharmacological behaviors in the human body. The binding of chiral drugs to plasma proteins usually exhibits stereoselectivity, which has a far-reaching influence on their pharmacological activities a...
PMC12520463
core_pubmed_pmc
Translation of a Human‐Based Malaria‐on‐a‐Chip Phenotypic Disease Model for In Vivo Applications
Translation of a Human‐Based Malaria‐on‐a‐Chip Phenotypic Disease Model for In Vivo Applications Abstract Abstract In 2023 malaria claimed ≈600000 lives, with 90% of those deaths attributed to the Plasmodium falciparum parasite. This resurgence in mortality emphasizes the necessity of adopting alternative models to acc...
PMC7717654
core_pubmed_pmc
Incessant Automatic Atrial Tachycardia in a Neonate Successfully Treated with Nadolol and Closely Spaced Doses of Flecainide: A Case Report
Incessant Automatic Atrial Tachycardia in a Neonate Successfully Treated with Nadolol and Closely Spaced Doses of Flecainide: A Case Report Abstract Abstract Supraventricular tachyarrhythmia (SVT) is the most common type of arrhythmia in childhood. Management can be challenging with an associated risk of mortality. A f...
PMC4748848
core_pubmed_pmc
Pharmacokinetic/Toxicity Properties of the New Anti-Staphylococcal Lead Compound SK-03-92
Pharmacokinetic/Toxicity Properties of the New Anti-Staphylococcal Lead Compound SK-03-92 Abstract Abstract Because of the potential of a new anti-staphylococcal lead compound SK-03-92 as a topical antibiotic, a patch, or an orally active drug, we sought to determine its safety profile and oral bioavailability. SK-03-9...
PMC12291358
core_pubmed_pmc
Targeting rheumatoid arthritis: a molecular perspective on biologic therapies and clinical progress
Targeting rheumatoid arthritis: a molecular perspective on biologic therapies and clinical progress Abstract Abstract To surpass challenges with traditional approaches to treat Rheumatoid arthritis (RA), an improved understanding of molecular-level pathogenesis brought forth targeted therapy with biologics as a great p...
PMC10459361
core_pubmed_pmc
Development and Validation of a Novel UHPLC-MS/MS Method for the Quantification of Plinabulin in Plasma and Its Application in a Pharmacokinetic Study with Leukopenic Rats
Development and Validation of a Novel UHPLC-MS/MS Method for the Quantification of Plinabulin in Plasma and Its Application in a Pharmacokinetic Study with Leukopenic Rats Abstract Plinabulin, a new antitumor drug developed from marine natural products that targets microtubules in cancer cells, is currently being teste...
PMC12609199
core_pubmed_pmc
Using Machine Learning for the Discovery and Development of Multitarget Flavonoid-Based Functional Products in MASLD
Using Machine Learning for the Discovery and Development of Multitarget Flavonoid-Based Functional Products in MASLD Abstract Abstract Metabolic dysfunction-associated steatotic liver disease (MASLD) represents a multifactorial condition requiring multi-target therapeutic strategies beyond traditional single-marker app...
PMC10614688
core_pubmed_pmc
The role of radiolabeling in BNCT tracers for enhanced dosimetry and treatment planning
The role of radiolabeling in BNCT tracers for enhanced dosimetry and treatment planning Abstract Abstract Positron emission tomography (PET) and single photon emission computed tomography (SPECT) are potent technologies for non-invasive imaging of pharmacological and biochemical processes in both preclinical and advanc...
PMC12655440
core_pubmed_pmc
Potential Modulation of Polygoni Cuspidati Rhizoma et Radix on Breast Cancer Resistance Protein and Marked Alteration on Methotrexate Pharmacokinetics
Potential Modulation of Polygoni Cuspidati Rhizoma et Radix on Breast Cancer Resistance Protein and Marked Alteration on Methotrexate Pharmacokinetics Abstract Abstract Background/Objectives : Polygoni Cuspidati Rhizoma et Radix (PCRR) is an herb and a source of a resveratrol-containing dietary supplement. Breast cance...
PMC12968486
core_pubmed_pmc
Pharmacokinetics and Safety of a Single Subcutaneous or Intramuscular Dose of Ketamine in Healthy Horses
Pharmacokinetics and Safety of a Single Subcutaneous or Intramuscular Dose of Ketamine in Healthy Horses Abstract ABSTRACT Pharmacokinetics (PK) of intramuscular (IM) and subcutaneous (SC) ketamine in horses has not been described. This study aimed to evaluate the PK and safety of ketamine and its metabolites after a s...
PMC8711110
core_pubmed_pmc
Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole
Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole Abstract Abstract Purpose Proton pump inhibitors (PPIs) are used for the treatment of acid-related disorders. Demands for enhanced stability and faster onset led to the...
PMC10609725
core_pubmed_pmc
Challenges in Permeability Assessment for Oral Drug Product Development
Challenges in Permeability Assessment for Oral Drug Product Development Abstract Drug permeation across the intestinal epithelium is a prerequisite for successful oral drug delivery. The increased interest in oral administration of peptides, as well as poorly soluble and poorly permeable compounds such as drugs for tar...
PMC9155601
core_pubmed_pmc
Population pharmacokinetics of intravenous cefotaxime indicates that higher doses are required for critically ill children
Population pharmacokinetics of intravenous cefotaxime indicates that higher doses are required for critically ill children Abstract Abstract Background Cefotaxime is frequently used in critically ill children, however pharmacokinetic (PK) studies to support adequate dosing in this patient population are limited. Object...
PMC8308703
core_pubmed_pmc
Therapeutic Drug Monitoring of Busulfan in Patients Undergoing Hematopoietic Cell Transplantation: A Pilot Single-Center Study in Taiwan
Therapeutic Drug Monitoring of Busulfan in Patients Undergoing Hematopoietic Cell Transplantation: A Pilot Single-Center Study in Taiwan Abstract Abstract Busulfan has been used as a conditioning regimen in allogeneic hematopoietic cell stem transplantation (HSCT). Owing to a large inter-individual variation in pharmac...
PMC10157140
core_pubmed_pmc
Genetic polymorphism related to ethambutol outcomes and susceptibility to toxicity
Genetic polymorphism related to ethambutol outcomes and susceptibility to toxicity Abstract The World Health Organization (WHO) stated that ensuring access to effective and optimal treatment is a key component to eradicate tuberculosis (TB) through the End TB Strategy. Personalized medicine that depends on the genetic ...
PMC6880852
core_pubmed_pmc
Efficacy and safety of switching from rituximab to biosimilar CT-P10 in rheumatoid arthritis: 72-week data from a randomized Phase 3 trial
Efficacy and safety of switching from rituximab to biosimilar CT-P10 in rheumatoid arthritis: 72-week data from a randomized Phase 3 trial Abstract Abstract Objective To evaluate the efficacy and safety of CT-P10, a rituximab biosimilar after a single switch, during a multinational, randomized, double-blind Phase 3 tri...
PMC3215871
core_pubmed_pmc
Preclinical evaluation of the antitumor activity of bortezomib in combination with vitamin C or with epigallocatechin gallate, a component of green tea
Preclinical evaluation of the antitumor activity of bortezomib in combination with vitamin C or with epigallocatechin gallate, a component of green tea Abstract Abstract Purpose To investigate whether clinically relevant levels of epigallocatechin gallate (EGCG, a component of green tea) or vitamin C (ascorbic acid) co...
PMC3513214
core_pubmed_pmc
Pharmacogenetics in breast cancer: steps toward personalized medicine in breast cancer management
Pharmacogenetics in breast cancer: steps toward personalized medicine in breast cancer management Abstract There is wide individual variability in the pharmacokinetics, pharmacodynamics, and tolerance to anticancer drugs within the same ethnic group and even greater variability among different ethnicities. Pharmacogeno...
PMC11381276
core_pubmed_pmc
Preclinical pharmacokinetic studies and prediction of human PK profiles for Deg-AZM, a clinical-stage new transgelin agonist
Preclinical pharmacokinetic studies and prediction of human PK profiles for Deg-AZM, a clinical-stage new transgelin agonist Abstract Introduction Deglycosylated azithromycin (Deg-AZM), a newly developed Class I drug with good therapeutic effects on slow transit constipation, is a small-molecule transgelin agonist that...
PMC7606183
core_pubmed_pmc
A modeling informed quantitative approach to salvage clinical trials interrupted due to COVID‐19
A modeling informed quantitative approach to salvage clinical trials interrupted due to COVID‐19 Abstract Abstract Many ongoing Alzheimer's disease central nervous system clinical trials are being disrupted and halted due to the COVID‐19 pandemic. They are often of a long duration’ are very complex; and involve many st...
PMC9921003
core_pubmed_pmc
Biogenic Selenium Nanoparticles in Biomedical Sciences: Properties, Current Trends, Novel Opportunities and Emerging Challenges in Theranostic Nanomedicine
Biogenic Selenium Nanoparticles in Biomedical Sciences: Properties, Current Trends, Novel Opportunities and Emerging Challenges in Theranostic Nanomedicine Abstract Selenium is an important dietary supplement and an essential trace element incorporated into selenoproteins with growth-modulating properties and cytotoxic...
PMC11513893
core_pubmed_pmc
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations
Discovery of Oral Degraders of the ROS1 Fusion Protein with Potent Activity against Secondary Resistance Mutations Abstract Abstract The development of therapeutic resistance in the majority of patients limits the long-term benefit of ROS1 inhibitor treatment. On-target mutations of the ROS1 kinase domain confer resist...
PMC9245605
core_pubmed_pmc
Nanocrytals-Mediated Oral Drug Delivery: Enhanced Bioavailability of Amiodarone
Nanocrytals-Mediated Oral Drug Delivery: Enhanced Bioavailability of Amiodarone Abstract The aim of this study was to improve the saturation solubility, dissolution profile and oral bioavailability of amiodarone hydrochloride (AMH), a highly lipophilic drug. Stabilizer (Pluronic F-127)-coated AMH nanocrystals (AMH-NCs)...
PMC9032118
core_pubmed_pmc
Squalene-Based Nano-Assemblies Improve the Pro-Autophagic Activity of Trehalose
Squalene-Based Nano-Assemblies Improve the Pro-Autophagic Activity of Trehalose Abstract The disaccharide trehalose is a well-established autophagy inducer, but its therapeutic application is severely hampered by its low potency and poor pharmacokinetic profile. Thus, we targeted the rational design and synthesis of tr...
PMC4846999
core_pubmed_pmc
Pharmacokinetic comparison of different flubendazole formulations in pigs: A further contribution to its development as a macrofilaricide molecule
Pharmacokinetic comparison of different flubendazole formulations in pigs: A further contribution to its development as a macrofilaricide molecule Abstract Despite the well established ivermectin activity against microfilaria, the success of human filariasis control programmes requires the use of a macrofilaricide comp...
PMC12208385
core_pubmed_pmc
Safety, Pharmacokinetics, and Clinical Efficacy of ADS051, a Neutrophil Modulator, in Ulcerative Colitis: Results of a Randomized Phase 1b Trial
Safety, Pharmacokinetics, and Clinical Efficacy of ADS051, a Neutrophil Modulator, in Ulcerative Colitis: Results of a Randomized Phase 1b Trial Abstract INTRODUCTION: Ulcerative colitis (UC) is characterized by colonic inflammation, with neutrophils playing a key role in UC activity, prognosis, and response to therapi...
PMC10517705
core_pubmed_pmc
Beta-Blockers and Their Current Role in Maternal and Neonatal Health: A Narrative Review of the Literature
Beta-Blockers and Their Current Role in Maternal and Neonatal Health: A Narrative Review of the Literature Abstract Beta-blockers are a class of medications that act on beta-adrenergic receptors and are categorized as cardio-selective and non-selective. They are principally used to treat cardiovascular conditions such ...
PMC12971278
core_pubmed_pmc
A Standardized Culture Medium for Comparative Drug Efficacy Evaluation Across Plasmodium and Babesia Species
A Standardized Culture Medium for Comparative Drug Efficacy Evaluation Across Plasmodium and Babesia Species Abstract The discovery of broad-spectrum antiparasitic agents relies on the ability to evaluate drug efficacy under harmonized in vitro conditions across related species. However, current drug screening pipeline...
PMC9155642
core_pubmed_pmc
Efficacy of Cipargamin (KAE609) in a Randomized, Phase II Dose-Escalation Study in Adults in Sub-Saharan Africa With Uncomplicated Plasmodium falciparum Malaria
Efficacy of Cipargamin (KAE609) in a Randomized, Phase II Dose-Escalation Study in Adults in Sub-Saharan Africa With Uncomplicated Plasmodium falciparum Malaria Abstract Abstract Background Cipargamin (KAE609) is a potent antimalarial in a phase II trial. Here we report efficacy, pharmacokinetics, and resistance marker...
PMC3584253
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Properties of Canakinumab, a Human Anti-Interleukin-1β Monoclonal Antibody
Pharmacokinetic and Pharmacodynamic Properties of Canakinumab, a Human Anti-Interleukin-1β Monoclonal Antibody Abstract Canakinumab is a high-affinity human monoclonal anti-interleukin-1β (IL-1β) antibody of the IgG1/κ isotype designed to bind and neutralize the activity of human IL-1β, a pro-inflammatory cytokine. Can...
PMC3177244
core_pubmed_pmc
Multimodal Bacteriochlorophyll Theranostic Agent
Multimodal Bacteriochlorophyll Theranostic Agent Abstract Abstract The complimentary ability of different noninvasive imaging technologies with therapeutic modalities can be used in tandem providing high-resolution and highly sensitive imaging of events at the molecular and cellular level providing a means for image-gu...
PMC12036611
core_pubmed_pmc
Model-Informed Precision Dosing of Levamlodipine Besylate in Smoking Patients
Model-Informed Precision Dosing of Levamlodipine Besylate in Smoking Patients Abstract Object To quantitatively investigate the influence of various factors, including nicotine, demographics, biochemical index, and genetic polymorphisms of PAHs and drug metabolising enzymes, on the steady-state trough concentrations of...
PMC3082038
core_pubmed_pmc
Phase I, pharmacokinetic, and biological studies of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, administered after meals with solid tumors
Phase I, pharmacokinetic, and biological studies of TSU-68, a novel multiple receptor tyrosine kinase inhibitor, administered after meals with solid tumors Abstract Abstract Purpose TSU-68 is a low molecular weight inhibitor of the tyrosine kinases for vascular endothelial growth factor receptor 2, platelet-derived gro...
PMC3671111
core_pubmed_pmc
A Phase I, open-label, randomized, crossover study in three parallel groups to evaluate the effect of Rifampicin, Ketoconazole, and Omeprazole on the pharmacokinetics of THC/CBD oromucosal spray in healthy volunteers
A Phase I, open-label, randomized, crossover study in three parallel groups to evaluate the effect of Rifampicin, Ketoconazole, and Omeprazole on the pharmacokinetics of THC/CBD oromucosal spray in healthy volunteers Abstract Abstract Abstract This Phase I study aimed to assess the potential drug-drug interactions (pha...
PMC11655785
core_pubmed_pmc
Effect of bariatric surgery on the pharmacokinetics of drugs used for attention‐deficit hyperactivity disorder—A case series
Effect of bariatric surgery on the pharmacokinetics of drugs used for attention‐deficit hyperactivity disorder—A case series Abstract Abstract Background Changes in gastrointestinal physiology following bariatric surgery may affect the pharmacokinetics of drugs. Data on the impact of bariatric surgery on drugs used for...
PMC11042421
core_pubmed_pmc
Quantifying trade-offs between therapeutic efficacy and resistance dissemination for enrofloxacin dose regimens in cattle
Quantifying trade-offs between therapeutic efficacy and resistance dissemination for enrofloxacin dose regimens in cattle Abstract Abstract The use of antimicrobial drugs in food-producing animals increases the selection pressure on pathogenic and commensal bacteria to become resistant. This study aims to evaluate the ...
PMC6953120
core_pubmed_pmc
Characterization of a Fiber Bundle-Based Real-Time Ultrasound/Photoacoustic Imaging System and Its In Vivo Functional Imaging Applications
Characterization of a Fiber Bundle-Based Real-Time Ultrasound/Photoacoustic Imaging System and Its In Vivo Functional Imaging Applications Abstract Abstract Photoacoustic (PA) imaging is an attractive technology for imaging biological tissues because it can capture both functional and structural information with satisf...
PMC11990732
core_pubmed_pmc
The Molecular Recognition of Lurasidone by Human Serum Albumin: A Combined Experimental and Computational Approach
The Molecular Recognition of Lurasidone by Human Serum Albumin: A Combined Experimental and Computational Approach Abstract Lurasidone (LUR) is an antipsychotic drug whose interaction with human serum albumin (HSA) plays a crucial role in its pharmacokinetic and pharmacodynamic properties. A thorough understanding of L...