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PMC11800098
core_pubmed_pmc
Challenges and opportunities to address the emerging burden of targeted therapies in ovarian cancer
Challenges and opportunities to address the emerging burden of targeted therapies in ovarian cancer Abstract Highlights • Ovarian cancer management leads to significant patient out of pocket expenditure. • Patients may experience financial toxicity during the course of treatment. • Targeted therapies may increase treat...
PMC11349847
core_pubmed_pmc
A Novel Formulation of Ketorolac Tromethamine (NTM-001) in Continuous Infusion in Adults with and without Renal Impairment: A Randomized Controlled Pharmacologic Study
A Novel Formulation of Ketorolac Tromethamine (NTM-001) in Continuous Infusion in Adults with and without Renal Impairment: A Randomized Controlled Pharmacologic Study Abstract Abstract Introduction There is a medical need for a safe, effective nonopioid postoperative analgesic for older subjects, including those with ...
PMC8613160
core_pubmed_pmc
Population Cellular Kinetics of Lisocabtagene Maraleucel, an Autologous CD19-Directed Chimeric Antigen Receptor T-Cell Product, in Patients with Relapsed/Refractory Large B-Cell Lymphoma
Population Cellular Kinetics of Lisocabtagene Maraleucel, an Autologous CD19-Directed Chimeric Antigen Receptor T-Cell Product, in Patients with Relapsed/Refractory Large B-Cell Lymphoma Abstract Abstract Background and Objectives Lisocabtagene maraleucel (liso-cel) is a CD19-directed, defined composition, 4-1BB chimer...
PMC4281073
core_pubmed_pmc
Comparison of Drug Release and Pharmacokinetics after Transarterial Chemoembolization Using Diverse Lipiodol Emulsions and Drug-Eluting Beads
Comparison of Drug Release and Pharmacokinetics after Transarterial Chemoembolization Using Diverse Lipiodol Emulsions and Drug-Eluting Beads Abstract In many studies for chemoembolization of hepatocellular carcinoma, the Lipiodol emulsion preparation protocols, especially the mixing steps, were unclear or even unrevea...
PMC6273216
core_pubmed_pmc
Inhibitors of the Hydrolytic Enzyme Dimethylarginine Dimethylaminohydrolase (DDAH): Discovery, Synthesis and Development
Inhibitors of the Hydrolytic Enzyme Dimethylarginine Dimethylaminohydrolase (DDAH): Discovery, Synthesis and Development Abstract Dimethylarginine dimethylaminohydrolase (DDAH) is a highly conserved hydrolytic enzyme found in numerous species, including bacteria, rodents, and humans. In humans, the DDAH-1 isoform is kn...
PMC6587326
core_pubmed_pmc
Delayed insulin absorption correlates with alterations in subcutaneous depot kinetics in rats with diet‐induced obesity
Delayed insulin absorption correlates with alterations in subcutaneous depot kinetics in rats with diet‐induced obesity Abstract Summary Objective Obesity is associated with delayed insulin absorption upon subcutaneous (s.c.) dosing in humans. The aim of this study was to investigate whether alterations in depot struct...
PMC12110642
core_pubmed_pmc
Drugs Used in “Chemsex”/Sexualized Drug Behaviour—Overview of the Related Clinical Psychopharmacological Issues
Drugs Used in “Chemsex”/Sexualized Drug Behaviour—Overview of the Related Clinical Psychopharmacological Issues Abstract Background : “Chemsex” involves the intake of a range of drugs (e.g., synthetic cathinones, gamma-hydroxybutyric acid/gamma-butyrolactone (GHB/GBL), ketamine, methamphetamine, “poppers”, type V phosp...
PMC3197614
core_pubmed_pmc
Drug Discovery for Duchenne Muscular Dystrophy via Utrophin Promoter Activation Screening
Drug Discovery for Duchenne Muscular Dystrophy via Utrophin Promoter Activation Screening Abstract Abstract Background Duchenne muscular dystrophy (DMD) is a devastating muscle wasting disease caused by mutations in dystrophin, a muscle cytoskeletal protein. Utrophin is a homologue of dystrophin that can functionally c...
PMC4467261
core_pubmed_pmc
Effects of Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on Pharmacokinetic Parameters of Rosiglitazone in Healthy Subjects
Effects of Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on Pharmacokinetic Parameters of Rosiglitazone in Healthy Subjects Abstract Background Icosapent ethyl is a high-purity form of eicosapentaenoic acid ethyl ester approved to reduce triglyceride levels in adults with triglycerides ≥500 mg/dL. Candidates for ...
PMC12823317
core_pubmed_pmc
Comparison of Metformin PBPK Models Incorporating Placental Transfer to Predict Fetal and Maternal Exposure
Comparison of Metformin PBPK Models Incorporating Placental Transfer to Predict Fetal and Maternal Exposure Abstract ABSTRACT Physiologically based pharmacokinetic (PBPK) modeling of placental drug transfer is an evolving tool for predicting fetal drug exposure. In this study, a pregnancy‐specific metformin PBPK model ...
PMC12034913
core_pubmed_pmc
Severe Impact of Omeprazole Timing on pH‐Sensitive Dasatinib Absorption: Unveiling Substantial Drug–Drug Interaction
Severe Impact of Omeprazole Timing on pH‐Sensitive Dasatinib Absorption: Unveiling Substantial Drug–Drug Interaction Abstract Abstract The absorption and bioavailability of most tyrosine kinase inhibitors are affected by gastrointestinal pH as they are weak basic lipophilic drugs. Hence, concomitant use of acid reducin...
PMC9220178
core_pubmed_pmc
Preclinical Characterization of Antioxidant Quinolyl Nitrone QN23 as a New Candidate for the Treatment of Ischemic Stroke
Preclinical Characterization of Antioxidant Quinolyl Nitrone QN23 as a New Candidate for the Treatment of Ischemic Stroke Abstract Abstract Nitrones are encouraging drug candidates for the treatment of oxidative stress-driven diseases such as acute ischemic stroke (AIS). In a previous study, we found a promising quinol...
PMC3718992
core_pubmed_pmc
A predictive pharmacokinetic–pharmacodynamic model of tumor growth kinetics in xenograft mice after administration of anticancer agents given in combination
A predictive pharmacokinetic–pharmacodynamic model of tumor growth kinetics in xenograft mice after administration of anticancer agents given in combination Abstract Abstract Purpose In clinical oncology, combination treatments are widely used and increasingly preferred over single drug administrations. A better charac...
PMC11687222
core_pubmed_pmc
Prediction and analysis of toxic and side effects of tigecycline based on deep learning
Prediction and analysis of toxic and side effects of tigecycline based on deep learning Abstract Abstract Background In recent years, with the increase of antibiotic resistance, tigecycline has attracted much attention as a new broad-spectrum glycylcycline antibiotic. It is widely used in the treatment of complex skin ...
PMC5403958
core_pubmed_pmc
From PK/PD to QSP: Understanding the Dynamic Effect of Cholesterol-Lowering Drugs on Atherosclerosis Progression and Stratified Medicine
From PK/PD to QSP: Understanding the Dynamic Effect of Cholesterol-Lowering Drugs on Atherosclerosis Progression and Stratified Medicine Abstract Current computational and mathematical tools are demonstrating the high value of using systems modeling approaches (e.g. Quantitative Systems Pharmacology) to understand the ...
PMC11015073
core_pubmed_pmc
Understanding CYP3A4 and P‐gp mediated drug–drug interactions through PBPK modeling – Case example of pralsetinib
Understanding CYP3A4 and P‐gp mediated drug–drug interactions through PBPK modeling – Case example of pralsetinib Abstract Abstract Pralsetinib, a potent and selective inhibitor of oncogenic RET fusion and RET mutant proteins, is a substrate of the drug metabolizing enzyme CYP3A4 and a substrate of the efflux transport...
PMC8754504
core_pubmed_pmc
Meropenem Target Attainment and Population Pharmacokinetics in Critically Ill Septic Patients with Preserved or Increased Renal Function
Meropenem Target Attainment and Population Pharmacokinetics in Critically Ill Septic Patients with Preserved or Increased Renal Function Abstract Abstract Purpose Critically ill patients with preserved or increased renal function have been shown to be at risk of underexposure to meropenem. Although many meropenem popul...
PMC7531749
core_pubmed_pmc
Evaluation of Renal Anionic Secretion Following Living-donor and Deceased-donor Renal Transplantation: A Clinical Pharmacokinetic Study of Cefoxitin Microdosing
Evaluation of Renal Anionic Secretion Following Living-donor and Deceased-donor Renal Transplantation: A Clinical Pharmacokinetic Study of Cefoxitin Microdosing Abstract Background. Renal transplantation is the treatment of choice for patients with end-stage renal disease. Because kidneys are the primary excretory orga...
PMC11018886
core_pubmed_pmc
Differential impact of fentanyl and morphine doses on ticagrelor-induced platelet inhibition in ST-segment elevation myocardial infarction: a subgroup analysis from the PERSEUS randomized trial
Differential impact of fentanyl and morphine doses on ticagrelor-induced platelet inhibition in ST-segment elevation myocardial infarction: a subgroup analysis from the PERSEUS randomized trial Abstract Abstract Introduction Among patients with ST-segment elevation myocardial infarction (STEMI) treated with primary per...
PMC12755803
core_pubmed_pmc
The Peak Plasma Concentration (Cmax)/Minimum Inhibitory Concentration (MIC) of bedaquiline and levofloxacin with special attention to the sputum conversion in the treatment of multidrug-resistant tuberculosis in Indonesia
The Peak Plasma Concentration (Cmax)/Minimum Inhibitory Concentration (MIC) of bedaquiline and levofloxacin with special attention to the sputum conversion in the treatment of multidrug-resistant tuberculosis in Indonesia Abstract Background Tuberculosis in Indonesia remains a serious public health concern, as the coun...
PMC12635367
core_pubmed_pmc
Pharmacological risks of khat–oral antidiabetic drug interactions among patients at Gondar university referral hospital
Pharmacological risks of khat–oral antidiabetic drug interactions among patients at Gondar university referral hospital Abstract Background Khat (Catha edulis), a psychoactive plant commonly chewed in Ethiopia, is known to influence drug metabolism through its active compound, cathinone. Among patients with T2DM, concu...
PMC9051383
core_pubmed_pmc
Human IgG1 Fc pH-dependent optimization from a constant pH molecular dynamics simulation analysis †
Human IgG1 Fc pH-dependent optimization from a constant pH molecular dynamics simulation analysis † Abstract The binding of IgG Fc with FcRn enables the long circulating half-life of IgG, where the Fc–FcRn complex interacts in a pH-dependent manner. This complex shows stronger interaction at pH ≤ 6.5 and weaker interac...
PMC11408209
core_pubmed_pmc
Insights from pharmacovigilance and pharmacodynamics on cardiovascular safety signals of NSAIDs
Insights from pharmacovigilance and pharmacodynamics on cardiovascular safety signals of NSAIDs Abstract Background and Aim Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat fever, pain, and inflammation. Concerns regarding their cardiovascular safety have been raised. However, the underlying me...
PMC11068998
core_pubmed_pmc
Metabolism and drug interactions of Korean ginseng based on the pharmacokinetic properties of ginsenosides: Current status and future perspectives
Metabolism and drug interactions of Korean ginseng based on the pharmacokinetic properties of ginsenosides: Current status and future perspectives Abstract Orally administered ginsenosides, the major active components of ginseng, have been shown to be biotransformed into a number of metabolites by gastric juice, digest...
PMC10955127
core_pubmed_pmc
Next generation risk assessment: an ab initio case study to assess the systemic safety of the cosmetic ingredient, benzyl salicylate, after dermal exposure
Next generation risk assessment: an ab initio case study to assess the systemic safety of the cosmetic ingredient, benzyl salicylate, after dermal exposure Abstract We performed an ab initio next-generation risk assessment (NGRA) for a fragrance ingredient, benzyl salicylate (BSal), to demonstrate how cosmetic ingredie...
PMC6154636
core_pubmed_pmc
Using UPLC-MS/MS for Characterization of Active Components in Extracts of Yupingfeng and Application to a Comparative Pharmacokinetic Study in Rat Plasma after Oral Administration
Using UPLC-MS/MS for Characterization of Active Components in Extracts of Yupingfeng and Application to a Comparative Pharmacokinetic Study in Rat Plasma after Oral Administration Abstract Yupingfeng (YPF), a famous traditional Chinese medicine, which contains a large array of compounds, has been effectually used in he...
PMC10033663
core_pubmed_pmc
Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats—pharmacokinetics, effects on behaviour and thermoregulation
Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats—pharmacokinetics, effects on behaviour and thermoregulation Abstract Introduction: N -2-methoxy-benzylated (“NBOMe”) analogues of phenethylamine are a group of new psychoactive substances (NPS) with reported strong psychedelic effects in sub-milligram ...
PMC8184532
core_pubmed_pmc
Population pharmacokinetic modelling to quantify the magnitude of drug-drug interactions between amlodipine and antiretroviral drugs
Population pharmacokinetic modelling to quantify the magnitude of drug-drug interactions between amlodipine and antiretroviral drugs Abstract Abstract Purpose Drug-drug interactions (DDIs) with antiretroviral drugs (ARVs) represent an important issue in elderly people living with HIV (PLWH). Amlodipine is a commonly pr...
PMC8992239
core_pubmed_pmc
Pharmacokinetics of ß-d-N4-Hydroxycytidine, the Parent Nucleoside of Prodrug Molnupiravir, in Nonplasma Compartments of Patients With Severe Acute Respiratory Syndrome Coronavirus 2 Infection
Pharmacokinetics of ß-d-N4-Hydroxycytidine, the Parent Nucleoside of Prodrug Molnupiravir, in Nonplasma Compartments of Patients With Severe Acute Respiratory Syndrome Coronavirus 2 Infection Abstract Abstract ß-d-N4-hydroxycytidine (NHC), the parent nucleoside of molnupiravir, a COVID-19 antiviral, was quantified at S...
PMC3284992
core_pubmed_pmc
Expression of recombinant human coagulation factors VII (rFVII) and IX (rFIX) in various cell types, glycosylation analysis, and pharmacokinetic comparison
Expression of recombinant human coagulation factors VII (rFVII) and IX (rFIX) in various cell types, glycosylation analysis, and pharmacokinetic comparison Conclusion Results and conclusions Identical protein structures and minor differences in post-translational modifications between rFVII from BHK, CHO, HEK293 cells,...
PMC10321182
core_pubmed_pmc
Chirality of antidepressive drugs: an overview of stereoselectivity
Chirality of antidepressive drugs: an overview of stereoselectivity Abstract Abstract Stereochemistry plays an important role in drug design because the enantiomers of a drug frequently vary in their biological action and pharmacokinetic profiles. Racemates of a drug with either an inactive or an unsafe enantiomer can ...
PMC12823309
core_pubmed_pmc
Generating Control Groups for Organ Impairment Studies: A Case‐Study Comparing Statistical and Population Pharmacokinetic‐Based Matching Approaches
Generating Control Groups for Organ Impairment Studies: A Case‐Study Comparing Statistical and Population Pharmacokinetic‐Based Matching Approaches Abstract ABSTRACT A common challenge in conducting phase 1 studies that assess the impact of organ impairment on the pharmacokinetics of a drug is the recruitment of a demo...
PMC5009137
core_pubmed_pmc
Comparable pharmacodynamics, efficacy, and safety of linagliptin 5 mg among Japanese, Asian and white patients with type 2 diabetes
Comparable pharmacodynamics, efficacy, and safety of linagliptin 5 mg among Japanese, Asian and white patients with type 2 diabetes Abstract Abstract Aims/Introduction The efficacy and safety of drugs can vary between different races or ethnic populations because of differences in the relationship of dose to exposure, ...
PMC12346198
core_pubmed_pmc
Valine–Niclosamide for Treatment of Androgen Receptor Splice Variant-Positive Hepatocellular Carcinoma
Valine–Niclosamide for Treatment of Androgen Receptor Splice Variant-Positive Hepatocellular Carcinoma Abstract Simple Summary Hepatocellular carcinoma (HCC) is the predominant form of liver cancer and a leading cause of global cancer-related mortality. At present, the current front-line systemic therapies for advanced...
PMC3263612
core_pubmed_pmc
Development of an Oral Form of Azacytidine: 2′3′5′Triacetyl-5-Azacytidine
Development of an Oral Form of Azacytidine: 2′3′5′Triacetyl-5-Azacytidine Abstract Abstract Myelodysplastic syndromes (MDSs) represent a group of incurable stem-cell malignancies which are predominantly treated by supportive care. Epigenetic silencing through promoter methylation of a number of genes is present in poor...
PMC6440611
core_pubmed_pmc
Systemic pharmacokinetic/pharmacodynamic analysis of intravitreal aflibercept injection in patients with retinal diseases
Systemic pharmacokinetic/pharmacodynamic analysis of intravitreal aflibercept injection in patients with retinal diseases Abstract Objective Explore relationships between systemic exposure to intravitreal aflibercept injection (IAI) and systemic pharmacodynamic effects via post hoc analyses of clinical trials of IAI fo...
PMC7977154
core_pubmed_pmc
Eribulin, Child-Pugh score, and liver-function tests: lessons from pivotal breast cancer studies 301 and 305
Eribulin, Child-Pugh score, and liver-function tests: lessons from pivotal breast cancer studies 301 and 305 Abstract Background The recommended starting dose of eribulin in patients with hepatic impairment is based on the Child-Pugh score, largely informed by a pharmacokinetic study of 18 patients. In the pivotal stud...
PMC6058531
core_pubmed_pmc
Inhalation delivery of topotecan is superior to intravenous exposure for suppressing lung cancer in a preclinical model
Inhalation delivery of topotecan is superior to intravenous exposure for suppressing lung cancer in a preclinical model Abstract Abstract Intravenous (IV) topotecan is approved for the treatment of various malignancies including lung cancer but its clinical use is greatly undermined by severe hematopoietic toxicity. We...
PMC3849647
core_pubmed_pmc
Pharmacokinetics and biodistribution of the cyclin-dependent kinase inhibitor -CR8- in mice
Pharmacokinetics and biodistribution of the cyclin-dependent kinase inhibitor -CR8- in mice Abstract Background CR8 is a second generation inhibitor of cyclin-dependent kinases derived from roscovitine. CR8 was shown to be 50–100 fold more potent than roscovitine in inducing apoptosis in different tumor cell lines. In ...
PMC4444337
core_pubmed_pmc
Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model
Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model Abstract Abstract Background The study assessed the antiviral activity of TMC353121, a respiratory syncytial virus (RSV) fusion inhibitor, in a preclinical non-human primate challenge model with a viral s...
PMC4746214
core_pubmed_pmc
Pharmacokinetic Bioequivalence, Safety, and Immunogenicity of DMB-3111, a Trastuzumab Biosimilar, and Trastuzumab in Healthy Japanese Adult Males: Results of a Randomized Trial
Pharmacokinetic Bioequivalence, Safety, and Immunogenicity of DMB-3111, a Trastuzumab Biosimilar, and Trastuzumab in Healthy Japanese Adult Males: Results of a Randomized Trial Abstract Background DMB-3111 is a biosimilar trastuzumab drug being jointly developed by Meiji Seika Pharma (Japan) and Dong-A Socio Holdings (...
PMC11684502
core_pubmed_pmc
Efficacy and safety of vancomycin compared with those of alternative treatments for methicillin‐resistant Staphylococcus aureus infections: An umbrella review
Efficacy and safety of vancomycin compared with those of alternative treatments for methicillin‐resistant Staphylococcus aureus infections: An umbrella review Abstract Abstract Objective To summarize the evidence on the efficacy and safety of vancomycin compared with those of alternative treatments in adult patients wi...
PMC12006663
core_pubmed_pmc
Subcutaneous Ocrelizumab in Patients With Multiple Sclerosis
Subcutaneous Ocrelizumab in Patients With Multiple Sclerosis Abstract Abstract Background and Objectives IV-administered ocrelizumab (OCR) is approved for the treatment of relapsing and primary progressive multiple sclerosis (RMS/PPMS). OCARINA II ( NCT05232825 ) was designed to demonstrate noninferiority in drug expos...
PMC9293150
core_pubmed_pmc
Phase 1/2a, open‐label, multicenter study of RM‐1929 photoimmunotherapy in patients with locoregional, recurrent head and neck squamous cell carcinoma
Phase 1/2a, open‐label, multicenter study of RM‐1929 photoimmunotherapy in patients with locoregional, recurrent head and neck squamous cell carcinoma Abstract Abstract Background Recurrent head and neck squamous cell carcinoma (rHNSCC) represents a significant global health burden with an unmet medical need. In this s...
PMC9998565
core_pubmed_pmc
Evaluation of the Influence of Sildenafil on the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Vericiguat in Healthy Adults
Evaluation of the Influence of Sildenafil on the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Vericiguat in Healthy Adults Abstract Background and Objective Vericiguat is approved for the treatment of patients with heart failure with ejection fraction < 45%. Sildenafil, indicated for the treatment of...
PMC11143530
core_pubmed_pmc
Pharmacokinetic enhancement of oncolytic virus M1 by inhibiting JAK‒STAT pathway
Pharmacokinetic enhancement of oncolytic virus M1 by inhibiting JAK‒STAT pathway Abstract Oncolytic viruses (OVs), a group of replication-competent viruses that can selectively infect and kill cancer cells while leaving healthy cells intact, are emerging as promising living anticancer agents. Unlike traditional drugs c...
PMC11263918
core_pubmed_pmc
Comparative study of the effects of antitussive drugs in a canine acute cough model
Comparative study of the effects of antitussive drugs in a canine acute cough model Abstract Abstract Background Cough is a common clinical complaint in small animal practice with limited treatment options for chronic underlying conditions. Objectives The present study aimed to evaluate the efficacy of three antitussiv...
PMC12937467
core_pubmed_pmc
TDM-Guided Dalbavancin Treatment for Complex Staphylococcus aureus Osteoarticular Infections in Children
TDM-Guided Dalbavancin Treatment for Complex Staphylococcus aureus Osteoarticular Infections in Children Abstract Abstract Background/Objectives : Dalbavancin is approved for pediatric acute bacterial skin and skin structure infections (ABSSSIs), yet real-world practice frequently necessitates off-label use for deep-se...
PMC10015565
core_pubmed_pmc
Influence of Murraya koenigii extract on diabetes induced rat brain aging
Influence of Murraya koenigii extract on diabetes induced rat brain aging Abstract Abstract Food supplements are used to improve cognitive functions in age-related dementia. This study was designed to determine the Murraya koenigii leaves’ effect on Alloxan-induced cognitive impairment in diabetic rats and the contents...
PMC7306095
core_pubmed_pmc
Allylmethylsulfide, a Sulfur Compound Derived from Garlic, Attenuates Isoproterenol-Induced Cardiac Hypertrophy in Rats
Allylmethylsulfide, a Sulfur Compound Derived from Garlic, Attenuates Isoproterenol-Induced Cardiac Hypertrophy in Rats Abstract Allylmethylsulfide (AMS) is a novel sulfur metabolite found in the garlic-fed serum of humans and animals. In the present study, we have observed that AMS is safe on chronic administration an...
PMC10508491
core_pubmed_pmc
A physiologically‐based pharmacokinetic model for tuberculosis drug disposition at extrapulmonary sites
A physiologically‐based pharmacokinetic model for tuberculosis drug disposition at extrapulmonary sites Abstract Abstract Tuberculosis (TB) is a leading cause of mortality attributed to an infectious agent. TB primarily targets the lungs, but in about 16% cases can affect other organs as well, giving rise to extrapulmo...
PMC10996858
core_pubmed_pmc
Pharmacokinetic of two oral doses of a 1:20 THC:CBD cannabis herbal extract in cats
Pharmacokinetic of two oral doses of a 1:20 THC:CBD cannabis herbal extract in cats Abstract Abstract Objective To determine the pharmacokinetics (PK) of two oral doses of a Cannabis herbal extract (CHE) containing 1:20 THC:CBD in 12 healthy Domestic Shorthair cats. Methods Single-dose PK were assessed after oral admin...
PMC10443535
core_pubmed_pmc
Pharmacokinetic Study of Enteric-Coated Sustained-Release Aspirin Tablets in Healthy Chinese Participants
Pharmacokinetic Study of Enteric-Coated Sustained-Release Aspirin Tablets in Healthy Chinese Participants Abstract Abstract Purpose To study and compare the pharmacokinetic characteristics of enteric-coated sustained-release (EcSr) aspirin tablets with enteric-coated (Ec) aspirin tablets (Bayer S.p.A) in healthy Chines...
PMC9573392
core_pubmed_pmc
From cis -Lobeline to trans -Lobeline: Study on the Pharmacodynamics and Isomerization Factors
From cis -Lobeline to trans -Lobeline: Study on the Pharmacodynamics and Isomerization Factors Abstract Abstract Lobeline is an alkaloid derived from the leaves of an Indian tobacco plant ( Lobelia inflata ), which has been prepared by chemical synthesis. It is classified as a partial nicotinic agonist and has a long h...
PMC10750039
core_pubmed_pmc
Clinical development of antivirals against SARS-CoV-2 and its variants
Clinical development of antivirals against SARS-CoV-2 and its variants Abstract Highlight • Developing antivirals is important for the treatment of coronavirus diseases, • Many viral factors and host factors serve as targets for developing antivirals, • Many repurposed antivirals did not demonstrate great efficacy in c...
PMC10296334
core_pubmed_pmc
Pharmacokinetics of Antibacterial Agents in the Elderly: The Body of Evidence
Pharmacokinetics of Antibacterial Agents in the Elderly: The Body of Evidence Abstract Abstract Infections are important factors contributing to the morbidity and mortality among elderly patients. High rates of consumption of antimicrobial agents by the elderly may result in increased risk of toxic reactions, deteriora...
PMC9000669
core_pubmed_pmc
Design, Synthesis, Pharmacodynamic and In Silico Pharmacokinetic Evaluation of Some Novel Biginelli-Derived Pyrimidines and Fused Pyrimidines as Calcium Channel Blockers
Design, Synthesis, Pharmacodynamic and In Silico Pharmacokinetic Evaluation of Some Novel Biginelli-Derived Pyrimidines and Fused Pyrimidines as Calcium Channel Blockers Abstract Some new pyrimidine derivatives comprising arylsulfonylhydrazino, ethoxycarbonylhydrazino, thiocarbamoylhydrazino and substituted hydrazone a...
PMC2834613
core_pubmed_pmc
Antenatal allopurinol for reduction of birth asphyxia induced brain damage (ALLO-Trial); a randomized double blind placebo controlled multicenter study
Antenatal allopurinol for reduction of birth asphyxia induced brain damage (ALLO-Trial); a randomized double blind placebo controlled multicenter study Abstract Background Hypoxic-ischaemic encephalopathy is associated with development of cerebral palsy and cognitive disability later in life and is therefore one of the...
PMC7076672
core_pubmed_pmc
Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates
Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates Abstract 13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resi...
PMC7144358
core_pubmed_pmc
Determination of KD025 (SLx-2119), a Selective ROCK2 Inhibitor, in Rat Plasma by High-Performance Liquid Chromatography-Tandem Mass Spectrometry and Its Pharmacokinetic Application
Determination of KD025 (SLx-2119), a Selective ROCK2 Inhibitor, in Rat Plasma by High-Performance Liquid Chromatography-Tandem Mass Spectrometry and Its Pharmacokinetic Application Abstract Abstract KD025 (SLx-2119), the first specific Rho-associated protein kinase 2 (ROCK2) inhibitor, is a potential new drug candidate...
PMC3717159
core_pubmed_pmc
LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models
LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models Abstract Summary The HGF/MET signaling pathway regulates a wide variety of normal cellular functions that can be subverted to support n...
PMC7919379
core_pubmed_pmc
Cytotoxicity Evaluation of Chloroquine and Hydroxychloroquine in Multiple Cell Lines and Tissues by Dynamic Imaging System and Physiologically Based Pharmacokinetic Model
Cytotoxicity Evaluation of Chloroquine and Hydroxychloroquine in Multiple Cell Lines and Tissues by Dynamic Imaging System and Physiologically Based Pharmacokinetic Model Abstract Abstract Chloroquine (CQ) and hydroxychloroquine (HCQ) have been challenged in treating COVID-19 patients and still under debate due to the ...
PMC9050387
core_pubmed_pmc
The development and validation of an HPLC-MS/MS method for the determination of eriocitrin in rat plasma and its application to a pharmacokinetic study
The development and validation of an HPLC-MS/MS method for the determination of eriocitrin in rat plasma and its application to a pharmacokinetic study Abstract Abstract Eriocitrin is one of the major active constituents of lemon fruit, and it possesses strong antioxidant, lipid-lowering, anticancer and anti-inflammato...
PMC8739161
core_pubmed_pmc
Safety, antitumor activity, and pharmacokinetics of dostarlimab, an anti-PD-1, in patients with advanced solid tumors: a dose–escalation phase 1 trial
Safety, antitumor activity, and pharmacokinetics of dostarlimab, an anti-PD-1, in patients with advanced solid tumors: a dose–escalation phase 1 trial Abstract Abstract Purpose New immuno-oncology therapies targeting programmed cell death receptor 1 (PD-1) have improved patient outcomes in a broad range of cancers. The...
PMC8785535
core_pubmed_pmc
Early vigabatrin augmenting GABA-ergic pathways in post-anoxic status epilepticus (VIGAB-STAT) phase IIa clinical trial study protocol
Early vigabatrin augmenting GABA-ergic pathways in post-anoxic status epilepticus (VIGAB-STAT) phase IIa clinical trial study protocol Abstract Abstract Background Nearly one in three unconscious cardiac arrest survivors experience post-anoxic status epilepticus (PASE). Historically, PASE has been deemed untreatable re...
PMC9796721
core_pubmed_pmc
Do we become better prescribers after graduation: A 1‐year international follow‐up study among junior doctors
Do we become better prescribers after graduation: A 1‐year international follow‐up study among junior doctors Abstract Aim The aim of this study was to investigate how the prescribing knowledge and skills of junior doctors in the Netherlands and Belgium develop in the year after graduation. We also analysed differences...
PMC6628352
core_pubmed_pmc
In Vivo Evaluation of Dual-Targeted Nanoparticles Encapsulating Paclitaxel and Everolimus
In Vivo Evaluation of Dual-Targeted Nanoparticles Encapsulating Paclitaxel and Everolimus Abstract A synergistic combination of paclitaxel (PTX) and everolimus (EVER) can allow for lower drug doses, reducing the toxicities associated with PTX, while maintaining therapeutic efficacy. Polymeric nanoparticles (NPs) of hig...
PMC8139681
core_pubmed_pmc
Phase I Trial on Arterial Embolization with Hypoxia Activated Tirapazamine for Unresectable Hepatocellular Carcinoma
Phase I Trial on Arterial Embolization with Hypoxia Activated Tirapazamine for Unresectable Hepatocellular Carcinoma Abstract Abstract Background Tirapazamine (TPZ) is a hypoxia activated drug that may be synergistic with transarterial embolization (TAE). The primary objective was to evaluate the safety of combining TP...
PMC10398570
core_pubmed_pmc
Physiologically-based pharmacokinetic modeling for single and multiple dosing regimens of ceftriaxone in healthy and chronic kidney disease populations: a tool for model-informed precision dosing
Physiologically-based pharmacokinetic modeling for single and multiple dosing regimens of ceftriaxone in healthy and chronic kidney disease populations: a tool for model-informed precision dosing Abstract Introduction: Ceftriaxone is one of commonly prescribed beta-lactam antibiotics with several label and off-label cl...
PMC9306994
core_pubmed_pmc
Assessment of Effects of Investigational TAK‐931, an Oral Cell Division Cycle 7 Kinase Inhibitor on the QTc Intervals in Patients With Advanced Solid Tumors
Assessment of Effects of Investigational TAK‐931, an Oral Cell Division Cycle 7 Kinase Inhibitor on the QTc Intervals in Patients With Advanced Solid Tumors Abstract Abstract TAK‐931, a novel, selective, small‐molecule inhibitor of cell division cycle 7 has been investigated in multiple clinical trials in patients with...
PMC4819942
core_pubmed_pmc
A phase I pharmacokinetics study comparing PF-06439535 (a potential biosimilar) with bevacizumab in healthy male volunteers
A phase I pharmacokinetics study comparing PF-06439535 (a potential biosimilar) with bevacizumab in healthy male volunteers Abstract Abstract Purpose This study compared the pharmacokinetics of PF-06439535, a potential bevacizumab biosimilar, to bevacizumab sourced from the European Union (bevacizumab-EU) and USA (beva...
PMC12944511
core_pubmed_pmc
Integrated Computational Investigation of Cannabis sativa Phytoconstituents as Putative Multi-Target Inhibitors in Skin Cancer: A Molecular Docking, Dynamics, and ADMET Profiling Study
Integrated Computational Investigation of Cannabis sativa Phytoconstituents as Putative Multi-Target Inhibitors in Skin Cancer: A Molecular Docking, Dynamics, and ADMET Profiling Study Abstract Abstract Background : Skin cancer progression is driven by the dysregulation of key oncogenic signaling pathways, including EG...
PMC5659777
core_pubmed_pmc
Clinical efficacy and pharmacokinetics of meloxicam in Mediterranean buffalo calves ( Bubalus bubalis )
Clinical efficacy and pharmacokinetics of meloxicam in Mediterranean buffalo calves ( Bubalus bubalis ) Abstract Abstract The aims of the investigation were to establish for the first time (i) clinical efficacy and (ii) pharmacokinetic profile of meloxicam intravenously (IV) administered in male Mediterranean buffalo c...
PMC7819284
core_pubmed_pmc
PK/PD Study of Mycophenolate Mofetil in Children With Systemic Lupus Erythematosus to Inform Model-Based Precision Dosing
PK/PD Study of Mycophenolate Mofetil in Children With Systemic Lupus Erythematosus to Inform Model-Based Precision Dosing Abstract Objectives: To evaluate the mycophenolic acid [MPA, the active form of mycophenolate mofetil (MMF)] pharmacokinetic parameters in relation to clinical response to identify target exposure r...
PMC6412495
core_pubmed_pmc
Urine Caffeine Concentration in Doping Control Samples from 2004 to 2015
Urine Caffeine Concentration in Doping Control Samples from 2004 to 2015 Abstract Abstract The ergogenic effect of caffeine is well-established, but the extent of its consumption in sport is unknown at the present. The use of caffeine was considered “prohibited” until 2004, but this stimulant was moved from the List of...
PMC4300410
core_pubmed_pmc
A randomised trial of the pharmacodynamic and pharmacokinetic effects of ticagrelor compared with clopidogrel in Hispanic patients with stable coronary artery disease
A randomised trial of the pharmacodynamic and pharmacokinetic effects of ticagrelor compared with clopidogrel in Hispanic patients with stable coronary artery disease Abstract Abstract The objective was to compare the pharmacodynamic (PD) and pharmacokinetic (PK) effects of ticagrelor with clopidogrel among subjects of...
PMC3760091
core_pubmed_pmc
Interaction of Carbamazepine with Herbs, Dietary Supplements, and Food: A Systematic Review
Interaction of Carbamazepine with Herbs, Dietary Supplements, and Food: A Systematic Review Abstract Abstract Background . Carbamazepine (CBZ) is a first-line antiepileptic drug which may be prone to drug interactions. Systematic review of herb- and food-drug interactions on CBZ is warranted to provide guidance for med...
PMC7157624
core_pubmed_pmc
Plasma Concentration Rise after the Intramuscular Administration of High Dose Medetomidine (0.13 mg/kg) for Semen Collection in Cats
Plasma Concentration Rise after the Intramuscular Administration of High Dose Medetomidine (0.13 mg/kg) for Semen Collection in Cats Abstract Abstract High dose medetomidine 0.13 mg/kg can be used for semen collection in cats with variable results in terms of quantity and quality. Therefore, a variation in terms of dis...
PMC5161048
core_pubmed_pmc
Role of cephalosporins in the era of Clostridium difficile infection
Role of cephalosporins in the era of Clostridium difficile infection Abstract Abstract The incidence of Clostridium difficile infection (CDI) in Europe has increased markedly since 2000. Previous meta-analyses have suggested a strong association between cephalosporin use and CDI, and many national programmes on CDI con...
PMC8301571
core_pubmed_pmc
Clinical pharmacology and dosing regimen optimization of neonatal opioid withdrawal syndrome treatments
Clinical pharmacology and dosing regimen optimization of neonatal opioid withdrawal syndrome treatments Abstract Abstract In this paper, we review the management of neonatal opioid withdrawal syndrome (NOWS) and clinical pharmacology of primary treatment agents in NOWS, including morphine, methadone, buprenorphine, clo...
PMC9943892
core_pubmed_pmc
Phase 1 Study of the Selective c-MET Inhibitor, HS-10241, in Patients With Advanced Solid Tumors
Phase 1 Study of the Selective c-MET Inhibitor, HS-10241, in Patients With Advanced Solid Tumors Abstract Abstract Introduction c-MET is an important therapeutic target for various cancers; however, the People’s Republic of China currently retails only one specific c-MET inhibitor. Our preclinical study has revealed th...
PMC10620926
core_pubmed_pmc
Development of a Method for Multisensory Stripping Voltammetry in the Analysis of Medical Preparations
Development of a Method for Multisensory Stripping Voltammetry in the Analysis of Medical Preparations Abstract For the effective dosage of newly developed ophthalmic drugs, an assessment of the dynamics of their concentration in lacrimal fluid over time is required. To express the detection and identification of drugs...
PMC8461112
core_pubmed_pmc
Efficacy predictors of omalizumab in Chinese patients with moderate-to-severe allergic asthma: Findings from a post-hoc analysis of a randomised phase III study ☆
Efficacy predictors of omalizumab in Chinese patients with moderate-to-severe allergic asthma: Findings from a post-hoc analysis of a randomised phase III study ☆ Abstract Abstract Background Omalizumab has demonstrated efficacy as an add-on therapy in Chinese patients with moderate-to-severe allergic asthma. This post...
PMC11678373
core_pubmed_pmc
Pharmacokinetic Interaction Between Olaparib and Regorafenib in an Animal Model
Pharmacokinetic Interaction Between Olaparib and Regorafenib in an Animal Model Abstract Abstract Background: Olaparib (OLA) and regorafenib (REG) are metabolized by the CYP3A4 isoenzyme of cytochrome P450. Both drugs are also substrates and inhibitors of the membrane transporters P-glycoprotein and BCRP. Therefore, th...
PMC5969050
core_pubmed_pmc
Influence of aprepitant on the pharmacodynamics and pharmacokinetics of gliclazide in rats and rabbits
Influence of aprepitant on the pharmacodynamics and pharmacokinetics of gliclazide in rats and rabbits Abstract Abstract Background Concomitant drug administration is a general phenomenon in patients with chronic diseases such as diabetes mellitus. Among the currently available oral antidiabetic drugs, gliclazide is a ...
PMC9199878
core_pubmed_pmc
High intrapatient variability of tacrolimus exposure associated with poorer outcomes in liver transplantation
High intrapatient variability of tacrolimus exposure associated with poorer outcomes in liver transplantation Abstract Abstract Tacrolimus (TAC) is a dose‐dependent immunosuppressor with considerable intrapatient variability (IPV) in its pharmacokinetics. The aim of this work is to ascertain the association between TAC...
PMC10456934
core_pubmed_pmc
Deciphering Molecular Aspects of Potential α -Glucosidase Inhibitors within Aspergillus terreus : A Computational Odyssey of Molecular Docking-Coupled Dynamics Simulations and Pharmacokinetic Profiling
Deciphering Molecular Aspects of Potential α -Glucosidase Inhibitors within Aspergillus terreus : A Computational Odyssey of Molecular Docking-Coupled Dynamics Simulations and Pharmacokinetic Profiling Abstract Hyperglycemia, as a hallmark of the metabolic malady diabetes mellitus, has been an overwhelming healthcare b...
PMC9781104
core_pubmed_pmc
Prediction of Drug–Drug–Gene Interaction Scenarios of ( E )-Clomiphene and Its Metabolites Using Physiologically Based Pharmacokinetic Modeling
Prediction of Drug–Drug–Gene Interaction Scenarios of ( E )-Clomiphene and Its Metabolites Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Clomiphene, a selective estrogen receptor modulator (SERM), has been used for the treatment of anovulation for more than 50 years. However, since ( E )-clomip...
PMC11505437
core_pubmed_pmc
Ceftazidime–Avibactam Versus Polymyxin-Based Combination Therapies: A Study on 30-Day Mortality in Carbapenem-Resistant Enterobacterales Bloodstream Infections in an OXA-48-Endemic Region †
Ceftazidime–Avibactam Versus Polymyxin-Based Combination Therapies: A Study on 30-Day Mortality in Carbapenem-Resistant Enterobacterales Bloodstream Infections in an OXA-48-Endemic Region † Abstract Abstract Background : Ceftazidime–avibactam (CAZ-AVI) is recommended as first-line treatment for Oxacillinase-48 (OXA-48)...
PMC12423363
core_pubmed_pmc
Estimands for Early‐Phase Dose Optimization Trials in Oncology
Estimands for Early‐Phase Dose Optimization Trials in Oncology Abstract ABSTRACT Phase I dose escalation trials in oncology generally aim to find the maximum tolerated dose. However, with the advent of molecular‐targeted therapies and antibody drug conjugates, dose‐limiting toxicities are less frequently observed, givi...
PMC11046337
core_pubmed_pmc
Abatacept Pharmacokinetics and Exposure Response in Patients Hospitalized With COVID-19
Abatacept Pharmacokinetics and Exposure Response in Patients Hospitalized With COVID-19 Abstract Key Points Question Is abatacept exposure associated with clinical outcomes in patients with severe COVID-19? Findings In this secondary analysis of abatacept pharmacokinetics and exposure-response data for 395 hospitalized...
PMC8455721
core_pubmed_pmc
Association of partial systemic exposure and abuse potential for opioid analgesics with abuse deterrence labeling claims supporting product-specific guidance
Association of partial systemic exposure and abuse potential for opioid analgesics with abuse deterrence labeling claims supporting product-specific guidance Abstract Background Over the past decade, U.S. FDA has approved 10 opioid analgesics in abuse-deterrent formulations (ADFs). ADFs are intended to reduce abuse of ...
PMC6479889
core_pubmed_pmc
Fritillariae Thunbergii Bulbus: Traditional Uses, Phytochemistry, Pharmacodynamics, Pharmacokinetics and Toxicity
Fritillariae Thunbergii Bulbus: Traditional Uses, Phytochemistry, Pharmacodynamics, Pharmacokinetics and Toxicity Abstract Abstract Fritillariae Thunbergii Bulbus (FTB) has been widely used as an antitussive herb for thousands of years in China. However, FTB’s traditional uses, chemical compounds and pharmacological ac...
PMC11812503
core_pubmed_pmc
Data-based regression models for predicting remifentanil pharmacokinetics
Data-based regression models for predicting remifentanil pharmacokinetics Abstract Background and Aims: Remifentanil is a powerful synthetic opioid drug with a short initiation and period of action, making it an ultra-short-acting opioid. It is delivered as an intravenous infusion during surgical procedures for pain ma...
PMC7883216
core_pubmed_pmc
Pharmacokinetics of exogenous GIP(1-42) in C57Bl/6 mice; Extremely rapid degradation but marked variation between available assays
Pharmacokinetics of exogenous GIP(1-42) in C57Bl/6 mice; Extremely rapid degradation but marked variation between available assays Abstract Highlights • Peptide hormone GIP shows an extremely short half-life of 90 s in mice. • Administration of GIP yields a very low ratio of intact:total peptide. • Co-administration wi...
PMC11784458
core_pubmed_pmc
Ex vivo assessment of sulbactam-durlobactam clearance during continuous renal replacement therapy to guide dosing recommendations
Ex vivo assessment of sulbactam-durlobactam clearance during continuous renal replacement therapy to guide dosing recommendations Abstract ABSTRACT Sulbactam-durlobactam is approved for the treatment of hospital-acquired and ventilator-associated bacterial pneumonia caused by susceptible isolates of Acinetobacter bauma...
PMC7557909
core_pubmed_pmc
Mitochondrial DNA damage as a potential biomarker of LRRK2 kinase activity in LRRK2 Parkinson’s disease
Mitochondrial DNA damage as a potential biomarker of LRRK2 kinase activity in LRRK2 Parkinson’s disease Abstract Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for the treatment of Parkinson’s disease (PD) and LRRK2 kinase inhibitors are currently being tested in early phase clinical trials. In ...
PMC12160614
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Immunogenicity Profiles of a Single‐Dose JYB1904 in Healthy Chinese Participants: A Phase Ia, Randomized, Double‐Blind, Placebo‐Controlled Study
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Immunogenicity Profiles of a Single‐Dose JYB1904 in Healthy Chinese Participants: A Phase Ia, Randomized, Double‐Blind, Placebo‐Controlled Study Abstract ABSTRACT Allergic asthma, characterized by airborne allergen sensitivity and Th2 immune responses, is a ...
PMC8437624
core_pubmed_pmc
Aminoquinolines as Translational Models for Drug Repurposing: Anticancer Adjuvant Properties and Toxicokinetic-Related Features
Aminoquinolines as Translational Models for Drug Repurposing: Anticancer Adjuvant Properties and Toxicokinetic-Related Features Abstract Abstract The indiscriminate consumption of antimalarials against coronavirus disease-2019 emphasizes the longstanding clinical weapons of medicines. In this work, we conducted a revie...
PMC11912621
core_pubmed_pmc
Comparative bioavailability study of two oral formulations of amoxicillin-clavulanic acid in healthy dogs
Comparative bioavailability study of two oral formulations of amoxicillin-clavulanic acid in healthy dogs Abstract Background Amoxicillin-clavulanic acid combination (AMX-CA) is a widely used oral antibiotic for companion animals. In Thailand, various AMX-CA formulations are available. This study aimed to evaluate and ...