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PMC4215876
core_pubmed_pmc
Dose Schedule Optimization and the Pharmacokinetic Driver of Neutropenia
Dose Schedule Optimization and the Pharmacokinetic Driver of Neutropenia Abstract Toxicity often limits the utility of oncology drugs, and optimization of dose schedule represents one option for mitigation of this toxicity. Here we explore the schedule-dependency of neutropenia, a common dose-limiting toxicity. To this...
PMC5737438
core_pubmed_pmc
Impact of enhanced metabolic stability on pharmacokinetics and pharmacodynamics of GalNAc–siRNA conjugates
Impact of enhanced metabolic stability on pharmacokinetics and pharmacodynamics of GalNAc–siRNA conjugates Abstract Abstract Covalent attachment of a synthetic triantennary N -acetylagalactosamine (GalNAc) ligand to chemically modified siRNA has enabled asialoglycoprotein (ASGPR)-mediated targeted delivery of therapeut...
PMC10106809
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Esomezol DR, a New Dual Delayed-Release Formulation of Esomeprazole 20 Mg or 40 Mg, in Healthy Subjects
Pharmacokinetics and Pharmacodynamics of Esomezol DR, a New Dual Delayed-Release Formulation of Esomeprazole 20 Mg or 40 Mg, in Healthy Subjects Abstract Abstract Background Esomeprazole, a proton pump inhibitor (PPI), is widely used to treat acid-related disorders, but it has short plasma half-life which can cause ins...
PMC5058548
core_pubmed_pmc
Regulatory T Cell Responses in Participants with Type 1 Diabetes after a Single Dose of Interleukin-2: A Non-Randomised, Open Label, Adaptive Dose-Finding Trial
Regulatory T Cell Responses in Participants with Type 1 Diabetes after a Single Dose of Interleukin-2: A Non-Randomised, Open Label, Adaptive Dose-Finding Trial Abstract Abstract Background Interleukin-2 (IL-2) has an essential role in the expansion and function of CD4 + regulatory T cells (Tregs). Tregs reduce tissue ...
PMC11152307
core_pubmed_pmc
Phase 1 randomized trials to assess safety, pharmacokinetics, and vaginal bleeding associated with use of extended duration dapivirine and levonorgestrel vaginal rings
Phase 1 randomized trials to assess safety, pharmacokinetics, and vaginal bleeding associated with use of extended duration dapivirine and levonorgestrel vaginal rings Abstract Abstract Background Vaginal rings formulated to deliver two drugs simultaneously have potential as user-controlled, long-acting methods for dua...
PMC5901821
core_pubmed_pmc
Development and Validation of an LC-MS/MS Method and Comparison with a GC-MS Method to Measure Phenytoin in Human Brain Dialysate, Blood, and Saliva
Development and Validation of an LC-MS/MS Method and Comparison with a GC-MS Method to Measure Phenytoin in Human Brain Dialysate, Blood, and Saliva Abstract Abstract Phenytoin (PHT) is one of the most often used critical dose drugs, where insufficient or excessive dosing can have severe consequences such as seizures o...
PMC11166842
core_pubmed_pmc
Insight into the mechanism of action of ORG27569 at the cannabinoid type one receptor utilising a unified mathematical model
Insight into the mechanism of action of ORG27569 at the cannabinoid type one receptor utilising a unified mathematical model Abstract Allosteric modulation of CB 1 is therapeutically advantageous compared to orthosteric activation as it potentially offers reduced on-target adverse effects. ORG27569 is an allosteric mod...
PMC12361215
core_pubmed_pmc
Pragmatic and contextualized methods selection for safety assessment of infant systemic exposure through human milk: the Milk4baby decision tree approach - a contribution from the concePTION project
Pragmatic and contextualized methods selection for safety assessment of infant systemic exposure through human milk: the Milk4baby decision tree approach - a contribution from the concePTION project Abstract More than 50% of women take at least one medication during lactation. However, 54% of drugs in the LactMed datab...
PMC12185616
core_pubmed_pmc
Population Pharmacokinetic Analysis of Enalapril and Enalaprilat in Newly Treated Children with Heart Failure: Implications for Safe Dosing of Enalapril (LENA Studies)
Population Pharmacokinetic Analysis of Enalapril and Enalaprilat in Newly Treated Children with Heart Failure: Implications for Safe Dosing of Enalapril (LENA Studies) Abstract Background Enalapril orodispersible minitablets (ODMT) have been authorised by the European Medicines Agency for the treatment of heart failure...
PMC6677897
core_pubmed_pmc
Effect of protracted dexamethasone exposure and its withdrawal on rocuronium-induced neuromuscular blockade and sugammadex reversal: an ex vivo rat study
Effect of protracted dexamethasone exposure and its withdrawal on rocuronium-induced neuromuscular blockade and sugammadex reversal: an ex vivo rat study Abstract Studies have reported that protracted dexamethasone treatment induces resistance to nondepolarizing neuromuscular blocking agents (NMBAs) and the association...
PMC11882694
core_pubmed_pmc
Critical Care Pharmacology of Antiretroviral Therapy in Adults
Critical Care Pharmacology of Antiretroviral Therapy in Adults Abstract Abstract The clinical pharmacology of antiretroviral therapy (ART) in critical care presents unique challenges due to the complex interplay between HIV infection, critical illness, and drug management. This comprehensive review examines the pharmac...
PMC7032178
core_pubmed_pmc
A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen
A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen Abstract Until now, there are no publications about the preformulation studies on (S)-zaltoprofen ((S)-ZPF). Hence, we first investigated the solubility of (S)-ZPF, screened solubilizers and performed the pharmac...
PMC6989234
core_pubmed_pmc
Mechanistic ligand-receptor interaction model: operational model of agonism
Mechanistic ligand-receptor interaction model: operational model of agonism Abstract This tutorial explains the basic principles of mechanistic ligand-receptor interaction model, which is an operational model of agonism. A growing number of agonist drugs, especially immune oncology drugs, is currently being developed. ...
PMC9931426
core_pubmed_pmc
Learn–confirm in model‐informed drug development: Assessing an immunogenicity quantitative systems pharmacology platform
Learn–confirm in model‐informed drug development: Assessing an immunogenicity quantitative systems pharmacology platform Abstract Abstract Immunogenicity against therapeutic proteins frequently causes attrition owing to its potential impact on pharmacokinetics, pharmacodynamics, efficacy, and safety. Predicting immunog...
PMC9521615
core_pubmed_pmc
Clinical effects and pharmacokinetics of nebulized lidocaine in healthy horses
Clinical effects and pharmacokinetics of nebulized lidocaine in healthy horses Abstract Background Nebulized lidocaine appears promising as a novel corticosteroid-sparing therapeutic for equine asthma, but its safety and pharmacokinetic behavior have yet to be confirmed. Objective To describe the effect of nebulized li...
PMC6004370
core_pubmed_pmc
Pharmacokinetics of Human Red Blood Cell Microparticles Prepared Using High-Pressure Extrusion Method
Pharmacokinetics of Human Red Blood Cell Microparticles Prepared Using High-Pressure Extrusion Method Abstract Red blood cell microparticles (RMPs) is a high potency hemostatic agent, which may serve as a viable therapeutic approach. They generate thrombin in vitro and effective in arresting bleeding in animal bleeding...
PMC12853871
core_pubmed_pmc
Exploring the opportunity for therapeutic drug monitoring (TDM) and precision dose antimicrobials in an outpatient antimicrobial therapy (OPAT) service: a prospective observational study
Exploring the opportunity for therapeutic drug monitoring (TDM) and precision dose antimicrobials in an outpatient antimicrobial therapy (OPAT) service: a prospective observational study Abstract Abstract Objectives Notwithstanding the wide uptake of outpatient antimicrobial therapy (OPAT) in the UK, there is a paucity...
PMC8927801
core_pubmed_pmc
Beyond Circulating Tumor Cell Enumeration: Cell-Based Liquid Biopsy to Assess Protein Biomarkers and Cancer Genomics Using the RareCyte ® Platform
Beyond Circulating Tumor Cell Enumeration: Cell-Based Liquid Biopsy to Assess Protein Biomarkers and Cancer Genomics Using the RareCyte ® Platform Abstract Abstract The practice of medicine has steadily employed less invasive methods to obtain information derived from the tumor to guide clinical management of patients....
PMC6495018
core_pubmed_pmc
Clinical Pharmacokinetics, Pharmacodynamics, Safety and Efficacy of Liposomal Amphotericin B
Clinical Pharmacokinetics, Pharmacodynamics, Safety and Efficacy of Liposomal Amphotericin B Abstract Abstract Since its introduction in the 1990s, liposomal amphotericin B (LAmB) continues to be an important agent for the treatment of invasive fungal diseases caused by a wide variety of yeasts and molds. This liposoma...
PMC11683177
core_pubmed_pmc
A Randomized, Parallel, Open‐Label, Single‐Dose and Multiple‐Dose Clinical Trial to Investigate the Pharmacokinetic, Pharmacodynamic, and Safety Profiles of Obicetrapib in Healthy Participants in China
A Randomized, Parallel, Open‐Label, Single‐Dose and Multiple‐Dose Clinical Trial to Investigate the Pharmacokinetic, Pharmacodynamic, and Safety Profiles of Obicetrapib in Healthy Participants in China Abstract Abstract Obicetrapib is a selective cholesteryl ester transfer protein (CETP) inhibitor. Previous research ha...
PMC11167383
core_pubmed_pmc
Systematic review of drug-drug interactions of delta-9-tetrahydrocannabinol, cannabidiol, and Cannabis
Systematic review of drug-drug interactions of delta-9-tetrahydrocannabinol, cannabidiol, and Cannabis Abstract Background The recent exponential increase in legalized medical and recreational cannabis, development of medical cannabis programs, and production of unregulated over-the-counter products (e.g., cannabidiol ...
PMC2952772
core_pubmed_pmc
Dose finding of melatonin for chronic idiopathic childhood sleep onset insomnia: an RCT
Dose finding of melatonin for chronic idiopathic childhood sleep onset insomnia: an RCT Abstract Abstract Rationale Pharmacokinetics of melatonin in children might differ from that in adults. Objectives This study aims to establish a dose–response relationship for melatonin in advancing dim light melatonin onset (DLMO)...
PMC8986118
core_pubmed_pmc
Pharmacokinetics of oral moxidectin in individuals with Onchocerca volvulus infection
Pharmacokinetics of oral moxidectin in individuals with Onchocerca volvulus infection Abstract Background Onchocerciasis (“river blindness”), is a neglected tropical disease caused by the filarial nematode Onchocerca volvulus and transmitted to humans through repeated bites by infective blackflies of the genus Simulium...
PMC12348926
core_pubmed_pmc
Potential of Quercetin as a Promising Therapeutic Agent Against Type 2 Diabetes
Potential of Quercetin as a Promising Therapeutic Agent Against Type 2 Diabetes Abstract Abstract Quercetin (QE) is a naturally occurring flavonoid found in many fruits, vegetables, and other plant-based foods. It is recognized for its diverse pharmacological activities. Among its many therapeutic potentials, its antid...
PMC9415969
core_pubmed_pmc
Efficient Sustained-Release Nanoparticle Delivery System Protects Nigral Neurons in a Toxin Model of Parkinson’s Disease
Efficient Sustained-Release Nanoparticle Delivery System Protects Nigral Neurons in a Toxin Model of Parkinson’s Disease Abstract Parkinson’s disease (PD) is a serious neurodegenerative disease wherein the progressive destruction of dopaminergic neurons results in a series of related movement disorders. Effective oral ...
PMC9369162
core_pubmed_pmc
Substrates of the Human Brain Proton-Organic Cation Antiporter and Comparison with Organic Cation Transporter 1 Activities
Substrates of the Human Brain Proton-Organic Cation Antiporter and Comparison with Organic Cation Transporter 1 Activities Abstract Abstract Many organic cations (OCs) may be transported through membranes by a genetically still uncharacterized proton-organic cation (H + OC) antiporter. Here, we characterized an extende...
PMC9507282
core_pubmed_pmc
The Impact of Pharmacokinetic-Guided Prophylaxis on Clinical Outcomes and Healthcare Resource Utilization in Hemophilia A Patients: Real-World Evidence from the CHESS II Study
The Impact of Pharmacokinetic-Guided Prophylaxis on Clinical Outcomes and Healthcare Resource Utilization in Hemophilia A Patients: Real-World Evidence from the CHESS II Study Abstract Abstract Background Using a pharmacokinetic (PK)-guided approach to personalize the dose and frequency of prophylactic treatment can he...
PMC10192880
core_pubmed_pmc
Evaluation and clinical implications of interactions between compound Danshen dropping pill and warfarin associated with the epoxide hydrolase gene
Evaluation and clinical implications of interactions between compound Danshen dropping pill and warfarin associated with the epoxide hydrolase gene Abstract Abstract Introduction: In clinical practice, warfarin is often combined with Compound Danshen dripping pill (CDDP) for the treatment of cardiovascular diseases. Ho...
PMC12292754
core_pubmed_pmc
Mapping the Global Research on Drug–Drug Interactions: A Multidecadal Evolution Through AI-Driven Terminology Standardization
Mapping the Global Research on Drug–Drug Interactions: A Multidecadal Evolution Through AI-Driven Terminology Standardization Abstract The significant burden of polypharmacy in clinical settings contrasts sharply with the narrow research focus on drug–drug interactions (DDIs), revealing an important gap in understandin...
PMC8867285
core_pubmed_pmc
Randomised study evaluating the pharmacodynamics of emixustat hydrochloride in subjects with macular atrophy secondary to Stargardt disease
Randomised study evaluating the pharmacodynamics of emixustat hydrochloride in subjects with macular atrophy secondary to Stargardt disease Abstract Background/Aims Stargardt disease is a rare, inherited, degenerative disease of the retina that is the most common type of hereditary macular dystrophy. Currently, no appr...
PMC9874752
core_pubmed_pmc
Ocrelizumab Concentration Is a Good Predictor of SARS‐CoV‐2 Vaccination Response in Patients with Multiple Sclerosis
Ocrelizumab Concentration Is a Good Predictor of SARS‐CoV‐2 Vaccination Response in Patients with Multiple Sclerosis Abstract Abstract Ocrelizumab, an anti‐CD20 monoclonal antibody, counteracts induction of humoral immune responses after severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2) vaccinations in patie...
PMC12376128
core_pubmed_pmc
In vitro and In Vivo Drug Metabolism Analysis of BPI-460372 - A Covalent TEAD1/3/4 Inhibitor
In vitro and In Vivo Drug Metabolism Analysis of BPI-460372 - A Covalent TEAD1/3/4 Inhibitor Abstract Background BPI-460372 is an orally available, covalent, irreversible small molecule inhibitor of the transcriptional enhanced associate domain (TEAD) 1/3/4, which is currently in clinical development for the treatment ...
PMC4048194
core_pubmed_pmc
A Study of the Relationship between Serum Bile Acids and Propranolol Pharmacokinetics and Pharmacodynamics in Patients with Liver Cirrhosis and in Healthy Controls
A Study of the Relationship between Serum Bile Acids and Propranolol Pharmacokinetics and Pharmacodynamics in Patients with Liver Cirrhosis and in Healthy Controls Abstract Abstract The main objectives of the study were to determine the exposure and bioavailability of oral propranolol and to investigate their associati...
PMC9810283
core_pubmed_pmc
A New Complex Design of Fe (II) Isoleucine Dithiocarbamate as a Novel Anticancer and Antivirus against SARSCOV-2 (COVID-19)
A New Complex Design of Fe (II) Isoleucine Dithiocarbamate as a Novel Anticancer and Antivirus against SARSCOV-2 (COVID-19) Abstract Background: This study was carried out to synthesize a new complex of Fe(II) with isoleucine dithiocarbamate ligand and to determine its potential as an anticancer and antiviral agent for...
PMC8253134
core_pubmed_pmc
Characterization of brusatol self-microemulsifying drug delivery system and its therapeutic effect against dextran sodium sulfate-induced ulcerative colitis in mice
Characterization of brusatol self-microemulsifying drug delivery system and its therapeutic effect against dextran sodium sulfate-induced ulcerative colitis in mice Abstract Abstract Brusatol (BR) is one of the main bioactive components derived from Brucea javanica , a medicinal herb historically used in the treatment ...
PMC6522096
core_pubmed_pmc
Development and Evaluation of an 18 F-Radiolabeled Monocyclam Derivative for Imaging CXCR4 Expression
Development and Evaluation of an 18 F-Radiolabeled Monocyclam Derivative for Imaging CXCR4 Expression Abstract Abstract In humans, C–X–C chemokine receptor type 4 (CXCR4) is a protein that is encoded by the CXCR4 gene and binds the ligand CXCL12 (also known as SDF-1). The CXCR4–CXCL12 interaction in cancer elicits biol...
PMC12864542
core_pubmed_pmc
A Systematic Review on Functional Bioactive Compound Atractylone: Natural Source, Pharmacological Properties and Mechanisms Insights
A Systematic Review on Functional Bioactive Compound Atractylone: Natural Source, Pharmacological Properties and Mechanisms Insights Abstract ABSTRACT Traditional Chinese medicine (TCM) has garnered considerable attention due to its multifaceted therapeutic potential, characterized by a broad spectrum of pharmacologica...
PMC11786019
core_pubmed_pmc
The Role of Candidate Polymorphisms in Drug Transporter Genes on High‐Dose Methotrexate in the Consolidation Phase of the AIEOP‐BFM ALL 2009 Protocol
The Role of Candidate Polymorphisms in Drug Transporter Genes on High‐Dose Methotrexate in the Consolidation Phase of the AIEOP‐BFM ALL 2009 Protocol Abstract ABSTRACT High‐dose methotrexate (HD‐MTX) infusions are commonly used to consolidate remission in children with acute lymphoblastic leukemia (ALL). We investigate...
PMC11676367
core_pubmed_pmc
The Role of Pharmacometrics in Advancing the Therapies for Autoimmune Diseases
The Role of Pharmacometrics in Advancing the Therapies for Autoimmune Diseases Abstract Autoimmune diseases (AIDs) are a group of disorders in which the immune system attacks the body’s own tissues, leading to chronic inflammation and organ damage. These diseases are difficult to treat due to variability in drug PK amo...
PMC7648747
core_pubmed_pmc
Application of physiologically based pharmacokinetic modeling for sertraline dosing recommendations in pregnancy
Application of physiologically based pharmacokinetic modeling for sertraline dosing recommendations in pregnancy Abstract Abstract Pregnancy is a period of significant change that impacts physiological and metabolic status leading to alterations in the disposition of drugs. Uncertainty in drug dosing in pregnancy can l...
PMC8839434
core_pubmed_pmc
Fisetin as a Senotherapeutic Agent: Biopharmaceutical Properties and Crosstalk between Cell Senescence and Neuroprotection
Fisetin as a Senotherapeutic Agent: Biopharmaceutical Properties and Crosstalk between Cell Senescence and Neuroprotection Abstract Abstract Like other organs, brain functions diminish with age. Furthermore, for a variety of neurological disorders—including Alzheimer’s disease—age is one of the higher-risk factors. Sin...
PMC12063204
core_pubmed_pmc
Phase 1 Study Evaluating the Pharmacokinetics, Dose Proportionality, Bioavailability, and Tolerability of Subcutaneous Levothyroxine Sodium (XP‐8121)
Phase 1 Study Evaluating the Pharmacokinetics, Dose Proportionality, Bioavailability, and Tolerability of Subcutaneous Levothyroxine Sodium (XP‐8121) Abstract ABSTRACT Levothyroxine sodium has been the cornerstone of hypothyroidism management worldwide, with daily oral administration (PO) recognized as standard of care...
PMC11080464
core_pubmed_pmc
Physiologically Based Biopharmaceutics Modeling (PBBM): Best Practices for Drug Product Quality, Regulatory and Industry Perspectives: 2023 Workshop Summary Report
Physiologically Based Biopharmaceutics Modeling (PBBM): Best Practices for Drug Product Quality, Regulatory and Industry Perspectives: 2023 Workshop Summary Report Abstract Abstract Physiologically based biopharmaceutics modeling (PBBM) is used to elevate drug product quality by providing a more accurate and holistic u...
PMC12196172
core_pubmed_pmc
Pharmacodynamic Evaluation of Adjuvant Targets: Low Molecular Weight PBP7/8 Effects on β-Lactam Activity Against Carbapenem-Resistant Acinetobacter Baumannii
Pharmacodynamic Evaluation of Adjuvant Targets: Low Molecular Weight PBP7/8 Effects on β-Lactam Activity Against Carbapenem-Resistant Acinetobacter Baumannii Abstract Background/Objectives: The increasing occurrence of carbapenem resistance A. baumannii (CRAB) has forced clinicians to seek out alternative options with ...
PMC4282310
core_pubmed_pmc
Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety
Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety Abstract Abstract Dual antiplatelet therapy, composed of aspirin plus a P2Y 12 -receptor antagonist, is the cornerstone of treatment for patients with acute coronary syndrome (ACS). A number of U.S. Food and Drug Administration–approved P2Y 1...
PMC6515699
core_pubmed_pmc
Treatment of internuclear ophthalmoparesis in multiple sclerosis with fampridine: A randomized double‐blind, placebo‐controlled cross‐over trial
Treatment of internuclear ophthalmoparesis in multiple sclerosis with fampridine: A randomized double‐blind, placebo‐controlled cross‐over trial Abstract Summary Aim To examine whether the velocity of saccadic eye movements in internuclear ophthalmoparesis ( INO ) improves with fampridine treatment in patients with mul...
PMC8147976
core_pubmed_pmc
Partitioning and Spatial Distribution of Drugs in Ocular Surface Tissues
Partitioning and Spatial Distribution of Drugs in Ocular Surface Tissues Abstract Abstract Ocular drug absorption after eye drop instillation has been widely studied, but partitioning phenomena and spatial drug distribution are poorly understood. We investigated partitioning of seven beta-blocking drugs in corneal epit...
PMC9270100
core_pubmed_pmc
A New Paradigm of Cardio-Hematological Monitoring in Chronic Myeloid Leukemia Patients Treated With Tyrosine Kinase Inhibitors
A New Paradigm of Cardio-Hematological Monitoring in Chronic Myeloid Leukemia Patients Treated With Tyrosine Kinase Inhibitors Abstract Abstract Significant progress has been achieved in treating patients with onco-hematological diseases, including chronic myeloid leukemia (CML). This is primarily associated with the d...
PMC9898395
core_pubmed_pmc
Upadacitinib Population Pharmacokinetics and Exposure-Response Relationships in Ulcerative Colitis Patients
Upadacitinib Population Pharmacokinetics and Exposure-Response Relationships in Ulcerative Colitis Patients Abstract Abstract Background and Objective Upadacitinib, an oral selective and reversible Janus kinase (JAK) inhibitor, showed favorable efficacy and safety in patients with moderate-to-severe ulcerative colitis ...
PMC3969656
core_pubmed_pmc
High-performance liquid chromatography determination and pharmacokinetics of coumarin compounds after oral administration of Samul-Tang to rats
High-performance liquid chromatography determination and pharmacokinetics of coumarin compounds after oral administration of Samul-Tang to rats Abstract Abstract Background: Samul-tang has been traditionally used for the treatment of cardiovascular, gynecologic, cutaneous, and chronic inflammation disorders. Although c...
PMC6137116
core_pubmed_pmc
Acetaminophen as a Renoprotective Adjunctive Treatment in Patients With Severe and Moderately Severe Falciparum Malaria: A Randomized, Controlled, Open-Label Trial
Acetaminophen as a Renoprotective Adjunctive Treatment in Patients With Severe and Moderately Severe Falciparum Malaria: A Randomized, Controlled, Open-Label Trial Abstract Abstract Background Acute kidney injury independently predicts mortality in falciparum malaria. It is unknown whether acetaminophen’s capacity to i...
PMC10469274
core_pubmed_pmc
Translational predictions of phase 2a first-in-patient efficacy studies for antituberculosis drugs
Translational predictions of phase 2a first-in-patient efficacy studies for antituberculosis drugs Abstract Abstract Background: Phase 2a trials in tuberculosis typically use early bactericidal activity (EBA), the decline in sputum CFU over 14 days, as the primary end-point for testing the efficacy of drugs as monother...
PMC7598804
core_pubmed_pmc
A phase I study of pharmacokinetics of trastuzumab emtansine in Chinese patients with locally advanced inoperable or metastatic human epidermal growth factor receptor 2-positive breast cancer who have received prior trastuzumab-based therapy
A phase I study of pharmacokinetics of trastuzumab emtansine in Chinese patients with locally advanced inoperable or metastatic human epidermal growth factor receptor 2-positive breast cancer who have received prior trastuzumab-based therapy Abstract Abstract Background: Trastuzumab emtansine (T-DM1) is an antibody–dru...
PMC6333674
core_pubmed_pmc
Bovine Mucosal Heparins Are Comparable to Porcine Mucosal Heparin at USP Potency Adjusted Levels
Bovine Mucosal Heparins Are Comparable to Porcine Mucosal Heparin at USP Potency Adjusted Levels Abstract Abstract Introduction: Bovine mucosal heparins (BMH) are currently being developed for re-introduction for both medical and surgical indications. BMH active pharmaceutical ingredient (API) exhibits a somewhat weake...
PMC6001845
core_pubmed_pmc
Effect of food on the pharmacokinetic characteristics of a single oral dose of LCB01-0371, a novel oxazolidinone antibiotic
Effect of food on the pharmacokinetic characteristics of a single oral dose of LCB01-0371, a novel oxazolidinone antibiotic Abstract Background LCB01-0371 is a novel oxazolidinone antibiotic that blocks protein production by binding to bacterial 23S ribosomes. This antibiotic is active against Gram-positive bacteria. T...
PMC7417114
core_pubmed_pmc
Repurposing of Kinase Inhibitors for Treatment of COVID-19
Repurposing of Kinase Inhibitors for Treatment of COVID-19 Abstract The outbreak of COVID-19, the pandemic disease caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has spurred an intense search for treatments by the scientific community. In the absence of a vaccine, the goal is to target the ...
PMC12612935
core_pubmed_pmc
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug–Drug Interaction In Vitro
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug–Drug Interaction In Vitro Abstract Abstract The OATP1B3 transporter is responsible for the hepatic uptake of multiple drugs and their metabolites. The single-nucleotide polymorphism (SNP) of OATP1B3 may be essential for interindividual variability in...
PMC3001221
core_pubmed_pmc
A Systematic, Updated Review on the Antidepressant Agomelatine Focusing on its Melatonergic Modulation
A Systematic, Updated Review on the Antidepressant Agomelatine Focusing on its Melatonergic Modulation Abstract Objective: To present an updated, comprehensive review on clinical and pre-clinical studies on agomelatine. Method: A MEDLINE, Psycinfo and Web of Science search (1966-May 2009) was performed using the follow...
PMC12341704
core_pubmed_pmc
Development of VNX-101, an adeno-associated virus with less immunogenicity and efficient long-term expression of a CD19 T cell engager
Development of VNX-101, an adeno-associated virus with less immunogenicity and efficient long-term expression of a CD19 T cell engager Abstract Abstract We previously described the use of recombinant adeno-associated virus (AAV) gene therapy to achieve off-the-shelf, long-term in vivo T cell engagement for CD19+ B cell...
PMC12329412
core_pubmed_pmc
Study of the mass balance, biotransformation, and safety of [ 14 C]IBI351 in healthy Chinese subjects
Study of the mass balance, biotransformation, and safety of [ 14 C]IBI351 in healthy Chinese subjects Abstract Abstract IBI351, a synthetic compound, exerts its anti-tumor effects by specifically, covalently, and irreversibly modifying the 12th cysteine residue of KRAS G12C. However, the pharmacokinetic profile of IBI3...
PMC8838889
core_pubmed_pmc
The System Profile of Renal Drug Transporters in Tubulointerstitial Fibrosis Model and Consequent Effect on Pharmacokinetics
The System Profile of Renal Drug Transporters in Tubulointerstitial Fibrosis Model and Consequent Effect on Pharmacokinetics Abstract Abstract With the widespread clinical use of drug combinations, the incidence of drug–drug interactions (DDI) has significantly increased, accompanied by a variety of adverse reactions. ...
PMC10514205
core_pubmed_pmc
Identifying an optimal fludarabine exposure for improved outcomes after axi-cel therapy for aggressive B-cell non-Hodgkin lymphoma
Identifying an optimal fludarabine exposure for improved outcomes after axi-cel therapy for aggressive B-cell non-Hodgkin lymphoma Abstract Key Points • Previous studies showed that fludarabine PK exposure is associated with key outcomes in pediatric patients after tisagenlecleucel. • In adults receiving axi-cel, an es...
PMC3355935
core_pubmed_pmc
Insulin Analogs and Cancer
Insulin Analogs and Cancer Abstract Today, insulin analogs are used in millions of diabetic patients. Insulin analogs have been developed to achieve more physiological insulin replacement in terms of time-course of the effect. Modifications in the amino acid sequence of the insulin molecule change the pharmacokinetics ...
PMC12313457
core_pubmed_pmc
Cardiac safety of bedaquiline, delamanid and moxifloxacin co-administered with or without varying doses of sutezolid or delpazolid for the treatment of drug-susceptible TB
Cardiac safety of bedaquiline, delamanid and moxifloxacin co-administered with or without varying doses of sutezolid or delpazolid for the treatment of drug-susceptible TB Abstract Abstract Introduction Many drugs for the treatment of TB prolong the QTc interval, which is associated with an increased risk of developing...
PMC8920403
core_pubmed_pmc
Sorafenib-loaded nanostructured lipid carriers for topical ocular therapy of corneal neovascularization: development, in-vitro and in vivo study
Sorafenib-loaded nanostructured lipid carriers for topical ocular therapy of corneal neovascularization: development, in-vitro and in vivo study Abstract Abstract Sorafenib (SRB), a multikinase inhibitor, is effective in reducing experimental corneal neovascularization (CNV) after oral administration; however, its ther...
PMC9667119
core_pubmed_pmc
Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes
Alfaxalone population pharmacokinetics in the rat: Model application for pharmacokinetic and pharmacodynamic design in inbred and outbred strains and sexes Abstract Abstract The translation of new injectable anesthetic drugs from rodent to humans remains slow, despite the realization that reliance on the volatile agent...
PMC6061088
core_pubmed_pmc
Projected 24-hour post-dose ocular itching scores post-treatment with olopatadine 0.7% versus 0.2%
Projected 24-hour post-dose ocular itching scores post-treatment with olopatadine 0.7% versus 0.2% Abstract Olopatadine is an antihistamine and mast cell stabilizer used for treating allergic conjunctivitis. Olopatadine 0.7% has been recently approved for daily dosing in the US, which supersedes the previously approved...
PMC10385846
core_pubmed_pmc
Relationship between Pharmacokinetic Profile and Clinical Efficacy Data of Three Different Forms of Locally Applied Flurbiprofen in the Mouth/Throat
Relationship between Pharmacokinetic Profile and Clinical Efficacy Data of Three Different Forms of Locally Applied Flurbiprofen in the Mouth/Throat Abstract Abstract This study aimed to link pharmacokinetic (PK) data from different flurbiprofen preparations for the treatment of sore throat with published data to eluci...
PMC4960810
core_pubmed_pmc
Utilizing native fluorescence imaging, modeling and simulation to examine pharmacokinetics and therapeutic regimen of a novel anticancer prodrug
Utilizing native fluorescence imaging, modeling and simulation to examine pharmacokinetics and therapeutic regimen of a novel anticancer prodrug Abstract Abstract Background Success of cancer prodrugs relying on a foreign gene requires specific delivery of the gene to the cancer, and improvements such as higher level g...
PMC6075885
core_pubmed_pmc
Pharmacokinetics of Doripenem in Healthy Koreans and Monte Carlo Simulations to Explore Optimal Dosage Regimens in Patients With Normal and Enhanced Renal Function
Pharmacokinetics of Doripenem in Healthy Koreans and Monte Carlo Simulations to Explore Optimal Dosage Regimens in Patients With Normal and Enhanced Renal Function Abstract Supplemental Digital Content is Available in the Text. Background: Dose adjustment is often required in patients with normal or enhanced renal func...
PMC8421735
core_pubmed_pmc
Optimized Dosing Regimens of Meropenem in Septic Children Receiving Extracorporeal Life Support
Optimized Dosing Regimens of Meropenem in Septic Children Receiving Extracorporeal Life Support Abstract Objectives: To develop a population pharmacokinetic model of meropenem in children with sepsis receiving extracorporeal life support (ECLS) and optimize the dosage regimen based on investigating the probability of t...
PMC7921458
core_pubmed_pmc
A clinical trial of non-invasive imaging with an anti-HIV antibody labelled with copper-64 in people living with HIV and uninfected controls
A clinical trial of non-invasive imaging with an anti-HIV antibody labelled with copper-64 in people living with HIV and uninfected controls Abstract Background A research priority in finding a cure for HIV is to establish methods to accurately locate and quantify where and how HIV persists in people living with HIV (P...
PMC11954688
core_pubmed_pmc
Effect of Hepatic Impairment or Renal Impairment on the Pharmacokinetics of Aficamten
Effect of Hepatic Impairment or Renal Impairment on the Pharmacokinetics of Aficamten Abstract Abstract Background and Objective Aficamten, a small-molecule, selective cardiac myosin inhibitor, is under development for the treatment of symptomatic obstructive hypertrophic cardiomyopathy (oHCM). Aficamten is primarily e...
PMC8024918
core_pubmed_pmc
Bacteriophage uptake by mammalian cell layers represents a potential sink that may impact phage therapy
Bacteriophage uptake by mammalian cell layers represents a potential sink that may impact phage therapy Abstract Summary It is increasingly apparent that bacteriophages, viruses that infect bacteria and more commonly referred to as simply phages, have tropisms outside their bacterial hosts. Using live tissue culture ce...
PMC8618844
core_pubmed_pmc
Mathematical Modeling of Within-Host, Untreated, Cytomegalovirus Infection Dynamics after Allogeneic Transplantation
Mathematical Modeling of Within-Host, Untreated, Cytomegalovirus Infection Dynamics after Allogeneic Transplantation Abstract Abstract Cytomegalovirus (CMV) causes significant morbidity and mortality in recipients of allogeneic hematopoietic cell transplantation (HCT). Whereas insights gained from mathematical modeling...
PMC4950695
core_pubmed_pmc
Evaluation of the paediatric dose of chloroquine in the treatment of Plasmodium vivax malaria
Evaluation of the paediatric dose of chloroquine in the treatment of Plasmodium vivax malaria Abstract Background Chloroquine (CQ) continues to be the first-line medication used worldwide in the treatment of Plasmodium vivax malaria. The dose recommended by the World Health Organization is 25 mg/kg independently of the...
PMC10825484
core_pubmed_pmc
The atorvastatin metabolite pattern in muscle tissue and blood plasma is associated with statin muscle side effects in patients with coronary heart disease; An exploratory case-control study
The atorvastatin metabolite pattern in muscle tissue and blood plasma is associated with statin muscle side effects in patients with coronary heart disease; An exploratory case-control study Abstract Abstract Background and aims Statin-associated muscle symptoms (SAMS) is a prevalent cause of statin discontinuation. It...
PMC10042773
core_pubmed_pmc
The Pharmacokinetics and Target Attainment of Antimicrobial Drugs Throughout Pregnancy: Part III Non-penicillin and Non-cephalosporin Drugs
The Pharmacokinetics and Target Attainment of Antimicrobial Drugs Throughout Pregnancy: Part III Non-penicillin and Non-cephalosporin Drugs Abstract Abstract Introduction Understanding the pharmacokinetics (PK) of antimicrobial drugs in pregnant women is crucial to provide effective and safe treatment. This study is pa...
PMC12702011
core_pubmed_pmc
Recent advances in mass spectrometry-based bioanalytical methods for endogenous biomarkers analysis in transporter-mediated drug-drug interactions
Recent advances in mass spectrometry-based bioanalytical methods for endogenous biomarkers analysis in transporter-mediated drug-drug interactions Abstract Drug-drug interactions (DDI) are a critical concern in drug development and clinical practice. A new molecular entity often requires numerous clinical DDI studies t...
PMC4714695
core_pubmed_pmc
Phase I trial of volasertib, a Polo‐like kinase inhibitor, in Japanese patients with acute myeloid leukemia
Phase I trial of volasertib, a Polo‐like kinase inhibitor, in Japanese patients with acute myeloid leukemia Abstract This phase I trial conducted in Japanese patients with acute myeloid leukemia evaluated the safety, maximum tolerated dose and pharmacokinetics of volasertib (BI 6727), a selective Polo‐like kinase inhib...
PMC3658019
core_pubmed_pmc
Bioanalysis in drug discovery and development
Bioanalysis in drug discovery and development Abstract Abstract Recent years have witnessed the introduction of several high-quality review articles into the literature covering various scientific and technical aspects of bioanalysis. Now it is widely accepted that bioanalysis is an integral part of the pharmacokinetic...
PMC11318863
core_pubmed_pmc
Analyzing the worldwide progression of COVID-19 cases and deaths using nonlinear mixed-effects model
Analyzing the worldwide progression of COVID-19 cases and deaths using nonlinear mixed-effects model Abstract COVID-19 is an infectious disease that continues to spread worldwide. A precise estimation of the cases and deaths due to COVID-19 would allow for appropriate consideration of healthcare resource allocation, pu...
PMC9229330
core_pubmed_pmc
Population Pharmacokinetics of Busulfan and Its Metabolite Sulfolane in Patients with Myelofibrosis Undergoing Hematopoietic Stem Cell Transplantation
Population Pharmacokinetics of Busulfan and Its Metabolite Sulfolane in Patients with Myelofibrosis Undergoing Hematopoietic Stem Cell Transplantation Abstract Abstract For patients with myelofibrosis, allogeneic hematopoietic stem cell transplantation (allo-HSCT) remains the only curative treatment to date. Busulfan-b...
PMC9199882
core_pubmed_pmc
Pharmacokinetic drug interactions of asciminib with the sensitive cytochrome P450 probe substrates midazolam, warfarin, and repaglinide in healthy participants
Pharmacokinetic drug interactions of asciminib with the sensitive cytochrome P450 probe substrates midazolam, warfarin, and repaglinide in healthy participants Abstract Abstract Asciminib, a first‐in‐class BCR‐ABL1 inhibitor that works by Specifically Targeting the ABL Myristoyl Pocket (STAMP), is a new treatment optio...
PMC10300336
core_pubmed_pmc
Nanotechnology-based radiation therapy to cure cancer and the challenges in its clinical applications
Nanotechnology-based radiation therapy to cure cancer and the challenges in its clinical applications Abstract Radiation therapy against cancer frequently fails to attain the desired outcomes because of several restricting aspects. Radiation therapy is not a targeted antitumor treatment, and it poses serious threats to...
PMC3021701
core_pubmed_pmc
Regulatory scientific advice in drug development: does company size make a difference?
Regulatory scientific advice in drug development: does company size make a difference? Abstract Purpose To assess whether the content of Scientific Advice (SA) questions addressed to a national drug regulatory agency is associated with company size. This may help to increase understanding about the knowledge, strategic...
PMC6398889
core_pubmed_pmc
Phase II trial of aflibercept with FOLFIRI as a second‐line treatment for Japanese patients with metastatic colorectal cancer
Phase II trial of aflibercept with FOLFIRI as a second‐line treatment for Japanese patients with metastatic colorectal cancer Abstract Abstract Aflibercept targets vascular endothelial growth factor. The present study involved assessing the efficacy, safety and pharmacokinetics of aflibercept plus 5‐fluorouracil/levofo...
PMC7830469
core_pubmed_pmc
Review of Clinical Questions Submitted to Norwegian Drug Information Centres Concerning Administration and Dosage to Older Patients of Relevance to Patient-Centric Care
Review of Clinical Questions Submitted to Norwegian Drug Information Centres Concerning Administration and Dosage to Older Patients of Relevance to Patient-Centric Care Abstract Abstract Patient-centric care entails optimising healthcare provision to patients based on their perspective and opinion. It involves appropri...
PMC7007418
core_pubmed_pmc
Population Pharmacokinetics of an Anti-PD-L1 Antibody, Durvalumab in Patients with Hematologic Malignancies
Population Pharmacokinetics of an Anti-PD-L1 Antibody, Durvalumab in Patients with Hematologic Malignancies Abstract Background and Objectives Durvalumab, a human monoclonal antibody targeting programmed cell death ligand 1, has been approved for urothelial carcinoma and stage III non-small cell lung cancer by the US F...
PMC6046601
core_pubmed_pmc
Phase 3, single‐arm, multicenter study of dabigatran etexilate for secondary prevention of venous thromboembolism in children: Rationale and design
Phase 3, single‐arm, multicenter study of dabigatran etexilate for secondary prevention of venous thromboembolism in children: Rationale and design Abstract Abstract Background Anticoagulant therapy for venous thromboembolism (VTE) in children is largely based on treatment recommendations for adults. However, differenc...
PMC7831362
core_pubmed_pmc
Activity of murine surrogate antibodies for durvalumab and tremelimumab lacking effector function and the ability to deplete regulatory T cells in mouse models of cancer
Activity of murine surrogate antibodies for durvalumab and tremelimumab lacking effector function and the ability to deplete regulatory T cells in mouse models of cancer Abstract ABSTRACT Preclinical studies of PD-L1 and CTLA-4 blockade have relied heavily on mouse syngeneic tumor models with intact immune systems, whi...
PMC6099349
core_pubmed_pmc
Development of a Molecular Signature to Monitor Pharmacodynamic Responses Mediated by In Vivo Administration of Glucocorticoids
Development of a Molecular Signature to Monitor Pharmacodynamic Responses Mediated by In Vivo Administration of Glucocorticoids Abstract Objective To develop an objective, readily measurable pharmacodynamic biomarker of glucocorticoid (GC) activity. Methods Genes modulated by prednisolone were identified from in vitro ...
PMC12272317
core_pubmed_pmc
Modeling and Simulation to Inform Apixaban Dosing in Pediatrics With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma Treated With Asparaginase
Modeling and Simulation to Inform Apixaban Dosing in Pediatrics With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma Treated With Asparaginase Abstract Apixaban could be a potential treatment option for the prevention of venous thromboembolism (VTE) in children with acute lymphoblastic leukemia (ALL) or lymphobl...
PMC6945238
core_pubmed_pmc
Impact of the host environment on the antitubercular action of pyrazinamide
Impact of the host environment on the antitubercular action of pyrazinamide Abstract Abstract Pyrazinamide remains the only drug in the tuberculosis pharmacopeia to drastically shorten first-line therapy from nine to six months. Due to its unparalleled ability to sterilize non-replicating bacilli and reduce relapse rat...
PMC7718703
core_pubmed_pmc
Accidental apixaban intoxication in a 23-month-old child: a case report
Accidental apixaban intoxication in a 23-month-old child: a case report Abstract Abstract Background Direct oral anticoagulants, such as apixaban, are increasingly used in everyday practice in order to treat or prevent thromboembolic diseases. To date, there is no available data about apixaban pharmacokinetics in child...
PMC3495014
core_pubmed_pmc
Dynamic tumor modeling of the dose–response relationship for everolimus in metastatic renal cell carcinoma using data from the phase 3 RECORD-1 trial
Dynamic tumor modeling of the dose–response relationship for everolimus in metastatic renal cell carcinoma using data from the phase 3 RECORD-1 trial Abstract Background The phase 3 RECORD-1 trial ( NCT00410124 ) established the efficacy and safety of everolimus in patients with metastatic renal cell carcinoma (mRCC) w...
PMC10457872
core_pubmed_pmc
Tigecycline Absorption Improved by Selected Excipients
Tigecycline Absorption Improved by Selected Excipients Abstract Abstract To investigate the effects of (2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD), (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), tocopherol polyethylene glycol 1000 succinate (TPGS), sodium desoxycholate (SDOCH), trimethyl chitosan (TMC), and sodium caprate ...
PMC11944824
core_pubmed_pmc
Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System of Cannabidiol for Enhanced Solubility and Bioavailability
Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System of Cannabidiol for Enhanced Solubility and Bioavailability Abstract Abstract Background/Objectives: This study aims to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) to enhance the solubility and oral bioavailability of ca...
PMC11655386
core_pubmed_pmc
Translational PK–PD model for in vivo CAR‐T‐cell therapy delivered using CAR mRNA‐loaded polymeric nanoparticle vector
Translational PK–PD model for in vivo CAR‐T‐cell therapy delivered using CAR mRNA‐loaded polymeric nanoparticle vector Abstract Abstract Autologous chimeric antigen receptor (CAR) T‐cell therapy has demonstrated remarkable response rates, yet its widespread implementation is hindered by logistical, financial, and physi...
PMC7083170
core_pubmed_pmc
Structure‐Based Design and Synthesis of Piperidinol‐Containing Molecules as New Mycobacterium abscessus Inhibitors
Structure‐Based Design and Synthesis of Piperidinol‐Containing Molecules as New Mycobacterium abscessus Inhibitors Abstract Abstract Non‐tuberculous mycobacterium (NTM) infections, such as those caused by Mycobacterium abscessus , are increasing globally. Due to their intrinsic drug resistance, M. abscessus pulmonary i...