id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC4759704 | core_pubmed_pmc | Quantitative prediction and clinical evaluation of an unexplored herb–drug interaction mechanism in healthy volunteers | Quantitative prediction and clinical evaluation of an unexplored herb–drug interaction mechanism in healthy volunteers Abstract Quantitative prediction of herb–drug interaction risk remains challenging. A quantitative framework to assess a potential interaction was used to evaluate a mechanism not previously tested in ... |
PMC12234879 | core_pubmed_pmc | Microneedle-based integrated pharmacokinetic and pharmacodynamic evaluation platform for personalized medicine | Microneedle-based integrated pharmacokinetic and pharmacodynamic evaluation platform for personalized medicine Abstract Abstract Precision and personalized medicine for disease management necessitates real-time, continuous monitoring of biomarkers and therapeutic drugs to adjust treatment regimens based on individual p... |
PMC6262252 | core_pubmed_pmc | Glutathione depleting drugs, antioxidants and intestinal calcium absorption | Glutathione depleting drugs, antioxidants and intestinal calcium absorption Abstract Glutathione (GSH) is a tripeptide that constitutes one of the main intracellular reducing compounds. The normal content of GSH in the intestine is essential to optimize the intestinal Ca 2+ absorption. The use of GSH depleting drugs su... |
PMC9023454 | core_pubmed_pmc | In vivo dose–response analysis to acetylcholine: pharmacodynamic assessment by polarized reflectance spectroscopy | In vivo dose–response analysis to acetylcholine: pharmacodynamic assessment by polarized reflectance spectroscopy Abstract Abstract Transdermal iontophoresis offers an in vivo alternative to the strain-gauge model for measurement of vascular function but is limited due to lack of technical solutions for outcome assessm... |
PMC9399604 | core_pubmed_pmc | Expert consensus statement on therapeutic drug monitoring and individualization of linezolid | Expert consensus statement on therapeutic drug monitoring and individualization of linezolid Abstract Abstract Linezolid is an oxazolidinone antibacterial drug, and its therapeutic drug monitoring and individualized treatment have been challenged since its approval. With the in-depth clinical research of linezolid, we ... |
PMC12862098 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modeling of Donidalorsen, an Antisense Oligonucleotide in Development for Prophylaxis of Hereditary Angioedema | Population Pharmacokinetic/Pharmacodynamic Modeling of Donidalorsen, an Antisense Oligonucleotide in Development for Prophylaxis of Hereditary Angioedema Abstract ABSTRACT Hereditary angioedema (HAE) is a rare disorder linked to kallikrein‐kinin system dysregulation, which leads to uncontrolled activation of plasma pre... |
PMC12362582 | core_pubmed_pmc | Linker Methylation as a Strategy to Enhance PROTAC Oral Bioavailability: Insights from Molecular Properties and Conformational Analysis | Linker Methylation as a Strategy to Enhance PROTAC Oral Bioavailability: Insights from Molecular Properties and Conformational Analysis Abstract In this study, we profiled 11 structurally related von Hippel–Lindau (VHL)-based proteolysis-targeting chimeras (PROTACs), evaluating in vivo pharmacokinetics in mice (oral bi... |
PMC2984425 | core_pubmed_pmc | Safety and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor YN968D1 in patients with advanced malignancies | Safety and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor YN968D1 in patients with advanced malignancies Abstract Abstract Background YN968D1 (Apatinib) selectively inhibits phosphorylation of VEGFR-2 and tumor angiogenesis in mice model. The study was conducted to determine... |
PMC9176062 | core_pubmed_pmc | Phase Ib study of combinations of avadomide (CC‐122), CC‐223, CC‐292, and rituximab in patients with relapsed/refractory diffuse large B‐cell lymphoma | Phase Ib study of combinations of avadomide (CC‐122), CC‐223, CC‐292, and rituximab in patients with relapsed/refractory diffuse large B‐cell lymphoma Abstract Abstract There is a need for additional treatment options for patients with relapsed or refractory diffuse large B‐cell lymphoma (DLBCL) who do not benefit from... |
PMC7187594 | core_pubmed_pmc | A Population Pharmacokinetic Model-Guided Evaluation of Ceftolozane-Tazobactam Dosing in Critically Ill Patients Undergoing Continuous Venovenous Hemodiafiltration | A Population Pharmacokinetic Model-Guided Evaluation of Ceftolozane-Tazobactam Dosing in Critically Ill Patients Undergoing Continuous Venovenous Hemodiafiltration Abstract The aim of this work was to describe optimized dosing regimens of ceftolozane-tazobactam for critically ill patients receiving continuous venovenou... |
PMC6964011 | core_pubmed_pmc | Health effects of nutrients and environmental pollutants in Baltic herring and salmon: a quantitative benefit-risk assessment | Health effects of nutrients and environmental pollutants in Baltic herring and salmon: a quantitative benefit-risk assessment Abstract Abstract Background Health risks linked with dioxin in fish remain a complex policy issue. Fatty Baltic fish contain persistent pollutants, but they are otherwise healthy food. We studi... |
PMC2898330 | core_pubmed_pmc | Development of a Two-part Strategy to Identify a Therapeutic Human Bispecific Antibody That Inhibits IgE Receptor Signaling * | Development of a Two-part Strategy to Identify a Therapeutic Human Bispecific Antibody That Inhibits IgE Receptor Signaling * Abstract The development of bispecific antibodies as therapeutic agents for human diseases has great clinical potential, but broad application has been hindered by the difficulty of identifying ... |
PMC6950274 | core_pubmed_pmc | Impact of Nicotine Replacement and Electronic Nicotine Delivery Systems on Fetal Brain Development | Impact of Nicotine Replacement and Electronic Nicotine Delivery Systems on Fetal Brain Development Abstract Abstract Maternal tobacco smoking during pregnancy remains a major public health issue. The neurotoxic properties of nicotine are associated with fetal neurodevelopmental disorders and perinatal morbimortality. R... |
PMC8740605 | core_pubmed_pmc | Single Oral Doses of MK-8507, a Novel Non-Nucleoside Reverse Transcriptase Inhibitor, Suppress HIV-1 RNA for a Week | Single Oral Doses of MK-8507, a Novel Non-Nucleoside Reverse Transcriptase Inhibitor, Suppress HIV-1 RNA for a Week Abstract Background: MK-8507 is a novel HIV-1 non-nucleoside reverse transcriptase inhibitor being developed for treatment of HIV-1 infection. MK-8507 has high antiviral potency in vitro and pharmacokinet... |
PMC12341096 | core_pubmed_pmc | A randomized trial to evaluate the pharmacokinetics, pharmacodynamics, and safety of vadadustat in patients with anemia associated with chronic kidney disease receiving hemodialysis | A randomized trial to evaluate the pharmacokinetics, pharmacodynamics, and safety of vadadustat in patients with anemia associated with chronic kidney disease receiving hemodialysis Abstract Abstract Background Vadadustat is an oral hypoxia-inducible factor prolyl hydroxylase inhibitor for treatment of anemia in dialys... |
PMC12774958 | core_pubmed_pmc | A phase 1, first-in-human, dose escalation study of JNJ-80038114, a PSMAxCD3 bispecific antibody, in participants with metastatic castration-resistant prostate cancer | A phase 1, first-in-human, dose escalation study of JNJ-80038114, a PSMAxCD3 bispecific antibody, in participants with metastatic castration-resistant prostate cancer Abstract Abstract Purpose Prostate-specific membrane antigen (PSMA) has been identified as a therapeutic target for metastatic castration-resistant prost... |
PMC6061410 | core_pubmed_pmc | Multiple Rising Doses of Oral BI 425809, a GlyT1 Inhibitor, in Young and Elderly Healthy Volunteers: A Randomised, Double-Blind, Phase I Study Investigating Safety and Pharmacokinetics | Multiple Rising Doses of Oral BI 425809, a GlyT1 Inhibitor, in Young and Elderly Healthy Volunteers: A Randomised, Double-Blind, Phase I Study Investigating Safety and Pharmacokinetics Abstract Abstract Background and Objective Schizophrenia and Alzheimer’s disease are characterised by abnormalities in glutamatergic pa... |
PMC11497128 | core_pubmed_pmc | Combining mathematical modeling, in vitro data and clinical target expression to support bispecific antibody binding affinity selection: a case example with FAP-4-1BBL | Combining mathematical modeling, in vitro data and clinical target expression to support bispecific antibody binding affinity selection: a case example with FAP-4-1BBL Abstract Abstract The majority of bispecific costimulatory antibodies in cancer immunotherapy are capable of exerting tumor-specific T-cell activation b... |
PMC10618730 | core_pubmed_pmc | Targeted Nanofitin-drug Conjugates Achieve Efficient Tumor Delivery and Therapeutic Effect in an EGFR pos Mouse Xenograft Model | Targeted Nanofitin-drug Conjugates Achieve Efficient Tumor Delivery and Therapeutic Effect in an EGFR pos Mouse Xenograft Model Abstract Abstract Adjusting the molecular size, the valency and the pharmacokinetics of drug conjugates are as many leverages to improve their therapeutic window, notably by affecting tumor pe... |
PMC8996499 | core_pubmed_pmc | Comparative bioavailability study following a single dose intravenous and buccal administration of remdesivir in rabbits | Comparative bioavailability study following a single dose intravenous and buccal administration of remdesivir in rabbits Abstract Abstract As remdesivir, the first FDA-approved drug for SARS-CoV-2 infection, can be used only for hospitalized patients due to intravenous administration, there is an urgent need of effecti... |
PMC9482958 | core_pubmed_pmc | Natural Products-Based Nanoformulations: A New Approach Targeting CSCs to Cancer Therapy | Natural Products-Based Nanoformulations: A New Approach Targeting CSCs to Cancer Therapy Abstract Abstract Cancer stem cells (CSCs) lead to the occurrence and progression of cancer due to their strong tumorigenic, self-renewal, and multidirectional differentiation abilities. Existing cancer treatment methods cannot eff... |
PMC6470838 | core_pubmed_pmc | Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban | Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban Abstract Concomitant use of rivaroxaban with non-dihydropyridine calcium channel blockers (non-DHPs) might lead to an increase of systemic rivaroxaban exposure and anticoagulant effects in relation to the inhibition of metabo... |
PMC12342022 | core_pubmed_pmc | Advancing precision medicine therapeutics for Parkinson’s utilizing a shared quantitative systems pharmacology model and framework | Advancing precision medicine therapeutics for Parkinson’s utilizing a shared quantitative systems pharmacology model and framework Abstract Abstract A rich pipeline of therapeutic candidates is advancing for Parkinson’s disease, many of which are targeting the underlying pathophysiology of disease. Emerging evidence gr... |
PMC5119973 | core_pubmed_pmc | Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models | Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models Abstract Abstract Regorafenib is an orally administered inhibitor of protein kinases involved in tumor angiogenesis, oncogenesis, and maintenance of the tumor microenvironment. Phase III studies showed that regorafenib has e... |
PMC4580473 | core_pubmed_pmc | Mitotic Checkpoint Kinase Mps1 Has a Role in Normal Physiology which Impacts Clinical Utility | Mitotic Checkpoint Kinase Mps1 Has a Role in Normal Physiology which Impacts Clinical Utility Abstract Cell cycle checkpoint intervention is an effective therapeutic strategy for cancer when applied to patients predisposed to respond and the treatment is well-tolerated. A critical cell cycle process that could be targe... |
PMC10489817 | core_pubmed_pmc | 2-Alkyl-Substituted-4-Amino-Thieno[2,3- d ]Pyrimidines: Anti-Proliferative Properties to In Vitro Breast Cancer Models | 2-Alkyl-Substituted-4-Amino-Thieno[2,3- d ]Pyrimidines: Anti-Proliferative Properties to In Vitro Breast Cancer Models Abstract Abstract Thienopyrimidines are structural analogs of quinazolines, and the creation of new 2-alkyl derivatives of ethyl 4-aminothienopyrimidine-6-carboxylates for the study of their anti-proli... |
PMC8852670 | core_pubmed_pmc | Is pharmacokinetic-guided dosing of desmopressin and von Willebrand factor-containing concentrates in individuals with von Willebrand disease or low von Willebrand factor reliable and feasible? A protocol for a multicentre, non-randomised, open label cohort trial, the OPTI-CLOT: to WiN study | Is pharmacokinetic-guided dosing of desmopressin and von Willebrand factor-containing concentrates in individuals with von Willebrand disease or low von Willebrand factor reliable and feasible? A protocol for a multicentre, non-randomised, open label cohort trial, the OPTI-CLOT: to WiN study Abstract Abstract Introduct... |
PMC12426406 | core_pubmed_pmc | Semi-mechanistic population pharmacokinetic model incorporating glutathione S-transferase activity for personalized busulfan dosing in pediatric allogeneic hematopoietic cell transplantation | Semi-mechanistic population pharmacokinetic model incorporating glutathione S-transferase activity for personalized busulfan dosing in pediatric allogeneic hematopoietic cell transplantation Abstract Abstract Background Busulfan is known for its high inter- and intra-individual pharmacokinetics/pharmacodynamics (PK/PD)... |
PMC10534486 | core_pubmed_pmc | Effects of Hyperlipidemia on the Pharmacokinetics of Tofacitinib, a JAK 1/3 Inhibitor, in Rats | Effects of Hyperlipidemia on the Pharmacokinetics of Tofacitinib, a JAK 1/3 Inhibitor, in Rats Abstract Tofacitinib, an inhibitor of Janus kinases (JAKs) 1 and 3, has been shown to be effective in the treatment of rheumatoid arthritis. The incidence of hyperlipidemia has been found to be higher in patients with rheumat... |
PMC8427954 | core_pubmed_pmc | The relationship between the effect-site concentration of propofol and sedation scale in children: a pharmacodynamic modeling study | The relationship between the effect-site concentration of propofol and sedation scale in children: a pharmacodynamic modeling study Abstract Abstract Background Continuous infusion of propofol has been used to achieve sedation in children. However, the relationship between the effect-site concentration ( C e ) of propo... |
PMC8097474 | core_pubmed_pmc | In Vitro Activity and In Vivo Efficacy of Cefiderocol against Stenotrophomonas maltophilia | In Vitro Activity and In Vivo Efficacy of Cefiderocol against Stenotrophomonas maltophilia Abstract Cefiderocol is a novel siderophore cephalosporin antibiotic with broad coverage against difficult-to-treat Gram-negative bacteria, including those resistant to carbapenems. Its activity against Stenotrophomonas maltophil... |
PMC7187334 | core_pubmed_pmc | Phase 1 Pharmacokinetic Study of AZD5718 in Healthy Volunteers: Effects of Coadministration With Rosuvastatin, Formulation and Food on Oral Bioavailability | Phase 1 Pharmacokinetic Study of AZD5718 in Healthy Volunteers: Effects of Coadministration With Rosuvastatin, Formulation and Food on Oral Bioavailability Abstract Abstract AZD5718 is a first‐in‐class small‐molecule anti‐inflammatory drug with the potential to reduce the residual risk of cardiovascular events after my... |
PMC5318338 | core_pubmed_pmc | Saliva Versus Plasma Bioequivalence of Azithromycin in Humans: Validation of Class I Drugs of the Salivary Excretion Classification System | Saliva Versus Plasma Bioequivalence of Azithromycin in Humans: Validation of Class I Drugs of the Salivary Excretion Classification System Abstract Aim The aim of this study was to compare human pharmacokinetics and bioequivalence metrics in saliva versus plasma for azithromycin as a model class I drug of the Salivary ... |
PMC10353880 | core_pubmed_pmc | Creation of a Didactic Clinical Pharmacology Lecture Series for Internal Medicine Residents | Creation of a Didactic Clinical Pharmacology Lecture Series for Internal Medicine Residents Abstract Abstract Introduction: One of the noted areas of weakness for internal medicine residents is pharmacology. However, there is little data documenting the creation and effect of a comprehensive pharmacology didactic progr... |
PMC7140755 | core_pubmed_pmc | Split First Dose Administration of Intravenous Daratumumab for the Treatment of Multiple Myeloma (MM): Clinical and Population Pharmacokinetic Analyses | Split First Dose Administration of Intravenous Daratumumab for the Treatment of Multiple Myeloma (MM): Clinical and Population Pharmacokinetic Analyses Abstract Abstract Introduction Daratumumab, a human immunoglobulin Gκ monoclonal antibody targeting CD38, is approved as monotherapy and in combination with standard-of... |
PMC11096517 | core_pubmed_pmc | Review of the pharmacokinetics of French maritime pine bark extract (Pycnogenol ® ) in humans | Review of the pharmacokinetics of French maritime pine bark extract (Pycnogenol ® ) in humans Abstract Abstract The French maritime pine bark extract Pycnogenol ® is a proprietary product from Pinus pinaster Aiton. It complies with the quality specifications in the United States Pharmacopeia monograph “Pine extract” in... |
PMC10725270 | core_pubmed_pmc | Population pharmacokinetics of ivermectin after mass drug administration in lymphatic filariasis endemic communities of Tanzania | Population pharmacokinetics of ivermectin after mass drug administration in lymphatic filariasis endemic communities of Tanzania Abstract Abstract Ivermectin (IVM) is a drug of choice used with albendazole for mass drug administration (MDA) to halt transmission of lymphatic filariasis. We investigated IVM pharmacokinet... |
PMC12110111 | core_pubmed_pmc | The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review | The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review Abstract Background: To date, it remains unclear which oral doses and preparation forms of melatonin should be ... |
PMC12394248 | core_pubmed_pmc | Pharmacokinetic Bioequivalence, Safety, and Immunogenicity of DMB-3115, an Ustekinumab Biosimilar, and EU- and US-Stelara in Healthy Adult Participants: A Randomized, Double-Blind, Single-Dose Study | Pharmacokinetic Bioequivalence, Safety, and Immunogenicity of DMB-3115, an Ustekinumab Biosimilar, and EU- and US-Stelara in Healthy Adult Participants: A Randomized, Double-Blind, Single-Dose Study Abstract Abstract Introduction The aim of this study was to investigate the pharmacokinetic bioequivalence between DMB-31... |
PMC10146305 | core_pubmed_pmc | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation Abstract Olmesartan medoxomil (OLM) is a first-line antihypertensive drug with low oral bioavailability (28.6%). This study aimed to develop oleogel formulations to decrease OLM side effects and b... |
PMC7390499 | core_pubmed_pmc | Genetics and major depressive disorder: clinical implications for disease risk, prognosis and treatment | Genetics and major depressive disorder: clinical implications for disease risk, prognosis and treatment Abstract Abstract In the post-genomic era, genetics has led to limited clinical applications in the diagnosis and treatment of major depressive disorder (MDD). Variants in genes coding for cytochrome enzymes are incl... |
PMC9866558 | core_pubmed_pmc | Amphotericin B Nano-Assemblies Circumvent Intrinsic Toxicity and Ensure Superior Protection in Experimental Visceral Leishmaniasis with Feeble Toxic Manifestation | Amphotericin B Nano-Assemblies Circumvent Intrinsic Toxicity and Ensure Superior Protection in Experimental Visceral Leishmaniasis with Feeble Toxic Manifestation Abstract Abstract In spite of its high effectiveness in the treatment of both leishmaniasis as well as a range of fungal infections, the free form of the pol... |
PMC7966506 | core_pubmed_pmc | Cannabidiol in Pharmacoresistant Epilepsy: Clinical Pharmacokinetic Data From an Expanded Access Program | Cannabidiol in Pharmacoresistant Epilepsy: Clinical Pharmacokinetic Data From an Expanded Access Program Abstract Background and Aim: Data on the clinical pharmacokinetics of cannabidiol (CBD) are scanty. We explored the effect of demographic and clinical variables on plasma concentrations of purified CBD in patients w... |
PMC10339692 | core_pubmed_pmc | Population pharmacokinetics, enzyme occupancy, and 24 S ‐hydroxycholesterol modeling of soticlestat, a novel cholesterol 24‐hydroxylase inhibitor, in healthy adults | Population pharmacokinetics, enzyme occupancy, and 24 S ‐hydroxycholesterol modeling of soticlestat, a novel cholesterol 24‐hydroxylase inhibitor, in healthy adults Abstract Abstract Soticlestat is a first‐in‐class, selective inhibitor of cholesterol 24‐hydroxylase (CH24H), which catabolizes cholesterol to 24 S ‐hydrox... |
PMC11229810 | core_pubmed_pmc | The impact of mild therapeutic hypothermia on platelet reactivity in comatose survivors of cardiac arrest with acute myocardial infarction treated with ticagrelor | The impact of mild therapeutic hypothermia on platelet reactivity in comatose survivors of cardiac arrest with acute myocardial infarction treated with ticagrelor Abstract Abstract Background The aim of the study was to assess the antiplatelet effect of ticagrelor in patients with myocardial infarction (MI) after out-o... |
PMC8650721 | core_pubmed_pmc | Tripterygium hypoglauc um (Lévl.) Hutch and Its Main Bioactive Components: Recent Advances in Pharmacological Activity, Pharmacokinetics and Potential Toxicity | Tripterygium hypoglauc um (Lévl.) Hutch and Its Main Bioactive Components: Recent Advances in Pharmacological Activity, Pharmacokinetics and Potential Toxicity Abstract Abstract Tripterygium hypoglaucum (Lévl.) Hutch (THH) is believed to play an important role in health care and disease treatment according to tradition... |
PMC11961231 | core_pubmed_pmc | A Phase 1b PK/PD Study to Demonstrate Antigen Elimination with RLYB212, A Monoclonal Anti-HPA-1a Antibody for FNAIT Prevention | A Phase 1b PK/PD Study to Demonstrate Antigen Elimination with RLYB212, A Monoclonal Anti-HPA-1a Antibody for FNAIT Prevention Abstract Background Fetal and neonatal alloimmune thrombocytopenia (FNAIT) is a rare bleeding disorder of the fetus/newborn caused by development of maternal alloantibodies against fetal human ... |
PMC12657850 | core_pubmed_pmc | Pharmacokinetics of therapies approved for spinal muscular atrophy: A narrative review of current evidence | Pharmacokinetics of therapies approved for spinal muscular atrophy: A narrative review of current evidence Abstract Abstract Spinal muscular atrophy is a severe neuromuscular disorder caused by mutations in the survival motor neuron 1 gene, leading to progressive motor neuron degeneration. Over the past decade, disease... |
PMC11646760 | core_pubmed_pmc | Cardiovascular toxicity risk assessment of tyrosine kinase inhibitors: a pharmacovigilance study using the VigiBase database | Cardiovascular toxicity risk assessment of tyrosine kinase inhibitors: a pharmacovigilance study using the VigiBase database Abstract Abstract Introduction Advances in the early detection and treatment of cancer have significantly improved the prognosis of patients with cancer. Tyrosine kinase inhibitors (TKIs) are eff... |
PMC3586876 | core_pubmed_pmc | Relationship between Patient Demographic Characteristics, Valproic Acid Dosage and Clearance in Adult Iranian Patients | Relationship between Patient Demographic Characteristics, Valproic Acid Dosage and Clearance in Adult Iranian Patients Abstract Abstract Objective(s) As there are conflicting findings regarding the clearance-dose and patient characteristics relationships for valproic acid (VPA), this study was conducted to investigate ... |
PMC5514907 | core_pubmed_pmc | Targeting of the breast cancer microenvironment with a potent and linkable oxindole based antiangiogenic small molecule | Targeting of the breast cancer microenvironment with a potent and linkable oxindole based antiangiogenic small molecule Abstract The clinical efficacy of antiangiogenic small molecules ( e.g ., sunitinib) in breast carcinoma has largely failed with substantial off-target toxicity. We rationally designed and evaluated p... |
PMC12453228 | core_pubmed_pmc | Volume kinetics of crystalloid and colloid solutions administered to healthy anesthetized cats | Volume kinetics of crystalloid and colloid solutions administered to healthy anesthetized cats Abstract This prospective experimental study evaluated the disposition of a crystalloid and a colloid solution in 10 healthy cats under general anesthesia. Each cat was randomly assigned to receive either 20 mL/kg of a balanc... |
PMC12304071 | core_pubmed_pmc | The Impact of Drug Properties and Severity of Obesity on Renal Drug Clearance Through Glomerular Filtration and Active Tubular Secretion: A Systematic Analysis Using PBPK Modeling | The Impact of Drug Properties and Severity of Obesity on Renal Drug Clearance Through Glomerular Filtration and Active Tubular Secretion: A Systematic Analysis Using PBPK Modeling Abstract Objective The influence of obesity on renal drug clearance (CLr) remains difficult to predict. This study quantifies obesity-relate... |
PMC4215875 | core_pubmed_pmc | Aldehyde Tag Coupled with HIPS Chemistry Enables the Production of ADCs Conjugated Site-Specifically to Different Antibody Regions with Distinct in Vivo Efficacy and PK Outcomes | Aldehyde Tag Coupled with HIPS Chemistry Enables the Production of ADCs Conjugated Site-Specifically to Different Antibody Regions with Distinct in Vivo Efficacy and PK Outcomes Abstract It is becoming increasingly clear that site-specific conjugation offers significant advantages over conventional conjugation chemistr... |
PMC6373577 | core_pubmed_pmc | Lack of UGT polymorphism association with idasanutlin pharmacokinetics in solid tumor patients | Lack of UGT polymorphism association with idasanutlin pharmacokinetics in solid tumor patients Abstract Abstract Purpose Idasanutlin is a selective small-molecule MDM2 antagonist. It activates the tumor suppressor TP53 and is in phase 3 clinical trial for acute myeloid leukemia. Nonclinical studies have shown that gluc... |
PMC4917521 | core_pubmed_pmc | Bioequivalence Study of Two Long-Acting Formulations of Oxytetracycline Following Intramuscular Administration in Bovines | Bioequivalence Study of Two Long-Acting Formulations of Oxytetracycline Following Intramuscular Administration in Bovines Abstract Abstract The aim of this study was to evaluate the bioequivalence of two commercial long-acting formulations based on oxytetracycline (OTC) hydrochloride between the reference formulation (... |
PMC6533040 | core_pubmed_pmc | Pharmacokinetic comparison of a diverse panel of non-targeting human antibodies as matched IgG1 and IgG2 isotypes in rodents and non-human primates | Pharmacokinetic comparison of a diverse panel of non-targeting human antibodies as matched IgG1 and IgG2 isotypes in rodents and non-human primates Abstract Abstract In this study we compared the pharmacokinetic profile of four unrelated antibodies, which do not bind to mammalian antigens, in IgG1 and IgG2 frameworks i... |
PMC8596792 | core_pubmed_pmc | Population Pharmacokinetics of Olanzapine and Samidorphan When Administered in Combination in Healthy Subjects and Patients With Schizophrenia | Population Pharmacokinetics of Olanzapine and Samidorphan When Administered in Combination in Healthy Subjects and Patients With Schizophrenia Abstract Abstract A combination of olanzapine and samidorphan was recently approved by the US Food and Drug Administration for the treatment of patients with schizophrenia or bi... |
PMC8116426 | core_pubmed_pmc | Intranasal Allopregnanolone Confers Rapid Seizure Protection: Evidence for Direct Nose-to-Brain Delivery | Intranasal Allopregnanolone Confers Rapid Seizure Protection: Evidence for Direct Nose-to-Brain Delivery Abstract Abstract Allopregnanolone, a positive modulator of GABA A receptors with antiseizure activity, has potential in the treatment of seizure emergencies. Instillation of allopregnanolone in 40% sulfobutylether-... |
PMC5548977 | core_pubmed_pmc | Safety and activity of IT-139, a ruthenium-based compound, in patients with advanced solid tumours: a first-in-human, open-label, dose-escalation phase I study with expansion cohort | Safety and activity of IT-139, a ruthenium-based compound, in patients with advanced solid tumours: a first-in-human, open-label, dose-escalation phase I study with expansion cohort Abstract Objective This phase I clinical study ( NCT01415297 ) evaluated the safety, tolerability, maximum-tolerated dose (MTD), pharmacok... |
PMC12842986 | core_pubmed_pmc | Can Fascaplysins Be Considered Analogs of Indolo[2,3- a ]pyrrolo[3,4- c ]carbazoles? Comparison of Biosynthesis, Biological Activity and Therapeutic Potential | Can Fascaplysins Be Considered Analogs of Indolo[2,3- a ]pyrrolo[3,4- c ]carbazoles? Comparison of Biosynthesis, Biological Activity and Therapeutic Potential Abstract For the first time, a comparative analysis has been conducted to elucidate the biosynthesis of three families of natural products—staurosporines/rebecca... |
PMC10224436 | core_pubmed_pmc | Effect of Food on the Pediatric Dispersible Tablet Formulations of TRIUMEQ and DOVATO in Healthy Adult Participants | Effect of Food on the Pediatric Dispersible Tablet Formulations of TRIUMEQ and DOVATO in Healthy Adult Participants Abstract Abstract This randomized food effect study in healthy adult participants examined dispersible tablet formulations of fixed-dose combinations of dolutegravir/abacavir/lamivudine (TRIUMEQ) and dolu... |
PMC9017349 | core_pubmed_pmc | Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones | Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones Abstract ABSTRACT Described here is a series of spiropyrimidinetrione (SPT) compounds with activity against Mycobacterium tuberculosis through inhibition of DNA gyra... |
PMC10035960 | core_pubmed_pmc | Daytime variation in non-cardiac surgery impacts the recovery after general anesthesia | Daytime variation in non-cardiac surgery impacts the recovery after general anesthesia Abstract Abstract Background Circadian rhythm involved with physiology has been reported to affect pharmacokinetics or pharmacodynamics. We hypothesized that circadian variations in physiology disturb anesthesia and eventually affect... |
PMC12251549 | core_pubmed_pmc | Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics | Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics Abstract Abstract The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated th... |
PMC8688925 | core_pubmed_pmc | Inhibition of Podocytes DPP4 Activity Is a Potential Mechanism of Lobeliae Chinensis Herba in Treating Diabetic Kidney Disease | Inhibition of Podocytes DPP4 Activity Is a Potential Mechanism of Lobeliae Chinensis Herba in Treating Diabetic Kidney Disease Abstract Diabetic kidney disease (DKD) is the leading cause of end-stage renal disease and has become a serious public health problem worldwide. Dipeptidyl peptidase-4 (DPP4) inhibitors, an eme... |
PMC11363325 | core_pubmed_pmc | A Novel Prodrug Strategy Based on Reversibly Degradable Guanidine Imides for High Oral Bioavailability and Prolonged Pharmacokinetics of Broad-Spectrum Anti-influenza Agents | A Novel Prodrug Strategy Based on Reversibly Degradable Guanidine Imides for High Oral Bioavailability and Prolonged Pharmacokinetics of Broad-Spectrum Anti-influenza Agents Abstract We present orally administrable prodrugs ( OSC-GCDI s) of guanidino oseltamivir carboxylate ( GOC ) based on guanidine cyclic diimide (GC... |
PMC6337617 | core_pubmed_pmc | In Vivo Glycan Engineering via the Mannosidase I Inhibitor (Kifunensine) Improves Efficacy of Rituximab Manufactured in Nicotiana benthamiana Plants | In Vivo Glycan Engineering via the Mannosidase I Inhibitor (Kifunensine) Improves Efficacy of Rituximab Manufactured in Nicotiana benthamiana Plants Abstract N-glycosylation has been shown to affect the pharmacokinetic properties of several classes of biologics, including monoclonal antibodies, blood factors, and lysos... |
PMC4432104 | core_pubmed_pmc | Reporting guidelines for population pharmacokinetic analyses | Reporting guidelines for population pharmacokinetic analyses Abstract Abstract The purpose of this work was to develop a consolidated set of guiding principles for reporting of population pharmacokinetic (PK) analyses based on input from a survey of practitioners as well as discussions between industry, consulting and ... |
PMC6440571 | core_pubmed_pmc | Emerging Role of Organ‐on‐a‐Chip Technologies in Quantitative Clinical Pharmacology Evaluation | Emerging Role of Organ‐on‐a‐Chip Technologies in Quantitative Clinical Pharmacology Evaluation Abstract The recently enacted Prescription Drug User Fee Act ( PDUFA ) VI includes in its performance goals “enhancing regulatory science and expediting drug development.” The key elements in “enhancing regulatory decision to... |
PMC11865925 | core_pubmed_pmc | Simulation of a field condition to evaluate the risk of enrofloxacin-resistant Pasteurella multocida strain selection in food producing rabbits treated via drinking water | Simulation of a field condition to evaluate the risk of enrofloxacin-resistant Pasteurella multocida strain selection in food producing rabbits treated via drinking water Abstract Introduction Pasteurella multocida is a key bacterial agent involved in most respiratory disorders in rabbits. The objective of this study w... |
PMC11280286 | core_pubmed_pmc | Pharmacokinetic Evaluation of Oral Viscous Budesonide in Paediatric Patients with Eosinophilic Oesophagitis in Repaired Oesophageal Atresia | Pharmacokinetic Evaluation of Oral Viscous Budesonide in Paediatric Patients with Eosinophilic Oesophagitis in Repaired Oesophageal Atresia Abstract Eosinophilic oesophagitis is a long-term complication of oesophageal atresia (EA), an uncommon condition that affects approximately 1 in 3500 infants. An exploratory, open... |
PMC3612327 | core_pubmed_pmc | Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin | Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin Abstract Background & objectives: Moxifloxacin (MFX) is reported to have promising antimycobacterial activity, and has a potential to shorten tuberculosis (TB) treatment. We undertook this study to examine the influence of rifampicin ... |
PMC7891419 | core_pubmed_pmc | Effect of Hepatic Impairment on Cobimetinib Pharmacokinetics: The Complex Interplay Between Physiological Changes and Drug Characteristics | Effect of Hepatic Impairment on Cobimetinib Pharmacokinetics: The Complex Interplay Between Physiological Changes and Drug Characteristics Abstract Abstract Cobimetinib is a kinase inhibitor indicated for use in combination with vemurafenib for treatment of unresectable/metastatic melanoma with specific BRAF mutations.... |
PMC11425750 | core_pubmed_pmc | Current status and usefulness of therapeutic drug monitoring implementation of theophylline in elderly patients based on a nationwide database study and modeling approach | Current status and usefulness of therapeutic drug monitoring implementation of theophylline in elderly patients based on a nationwide database study and modeling approach Abstract Objectives: Theophylline is used in the treatment of chronic obstructive pulmonary disease but readily causes symptoms of intoxication and e... |
PMC9922174 | core_pubmed_pmc | Meeting the Unmet Need in the Management of MDR Gram-Positive Infections with Oral Bactericidal Agent Levonadifloxacin | Meeting the Unmet Need in the Management of MDR Gram-Positive Infections with Oral Bactericidal Agent Levonadifloxacin Abstract Levonadifloxacin (intravenous) and its oral prodrug alalevonadifloxacin are broad-spectrum antibacterial agents developed for the treatment of difficult-to-treat infections caused by multidrug... |
PMC7985098 | core_pubmed_pmc | Anti-inflammatory Action of Statins in Cardiovascular Disease: the Role of Inflammasome and Toll-Like Receptor Pathways | Anti-inflammatory Action of Statins in Cardiovascular Disease: the Role of Inflammasome and Toll-Like Receptor Pathways Abstract Atherosclerosis is one type of cardiovascular disease (CVD) in which activation of the NLRP3 inflammasome and toll-like receptor (TLR) pathways is implicated. One of the most effective treatm... |
PMC8219870 | core_pubmed_pmc | Prednisolone in Dogs—Plasma Exposure and White Blood Cell Response | Prednisolone in Dogs—Plasma Exposure and White Blood Cell Response Abstract Glucocorticoids such as prednisolone are commonly used in dogs but there is sparse quantitative pharmacokinetic and pharmacodynamic information of this drug in this species. The objective of this study was to quantitatively characterize the con... |
PMC10860804 | core_pubmed_pmc | Ranibizumab Biosimilars in Treating Retinal Disorders: A Cost-Effective Revolution? | Ranibizumab Biosimilars in Treating Retinal Disorders: A Cost-Effective Revolution? Abstract Abstract Ranibizumab, is a humanized, monoclonal antibody fragment that binds and inactivates vascular endothelial growth factor-A (VEGF-A) and VEGF-B. One of the main indications for an intravitreal treatment with ranibizumab ... |
PMC4150927 | core_pubmed_pmc | Population Pharmacokinetics and Antimalarial Pharmacodynamics of Piperaquine in Patients With Plasmodium vivax Malaria in Thailand | Population Pharmacokinetics and Antimalarial Pharmacodynamics of Piperaquine in Patients With Plasmodium vivax Malaria in Thailand Abstract Abstract Dihydroartemisinin-piperaquine is an effective drug in the treatment of Plasmodium falciparum and P. vivax malaria. The objective of this study was to evaluate the populat... |
PMC4184702 | core_pubmed_pmc | The potent and selective α 4 β 2*/ α 6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-(( S )Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile | The potent and selective α 4 β 2*/ α 6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-(( S )Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile Abstract Preclinical and clinical studies demonstrated that the inhib... |
PMC5346382 | core_pubmed_pmc | Effects of FMO3 Polymorphisms on Pharmacokinetics of Sulindac in Chinese Healthy Male Volunteers | Effects of FMO3 Polymorphisms on Pharmacokinetics of Sulindac in Chinese Healthy Male Volunteers Abstract Sulindac is a nonsteroidal anti-inflammatory drug, which is clinically used for the ailments of various inflammations. This study investigated the allele frequencies of FMO3 E158K and E308G and evaluated the influe... |
PMC4261612 | core_pubmed_pmc | Prediction of brain clozapine and norclozapine concentrations in humans from a scaled pharmacokinetic model for rat brain and plasma pharmacokinetics | Prediction of brain clozapine and norclozapine concentrations in humans from a scaled pharmacokinetic model for rat brain and plasma pharmacokinetics Abstract Abstract Background Clozapine is highly effective in treatment-resistant schizophrenia, although, there remains significant variability in the response to this d... |
PMC4130225 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution Study of Chlorogenic Acid from Lonicerae Japonicae Flos Following Oral Administrations in Rats | Pharmacokinetics and Tissue Distribution Study of Chlorogenic Acid from Lonicerae Japonicae Flos Following Oral Administrations in Rats Abstract Chlorogenic acid (ChA) is proposed as the major bioactive compounds of Lonicerae Japonicae Flos (LJF). Forty-two Wistar rats were randomly divided into seven groups to investi... |
PMC4863280 | core_pubmed_pmc | Effect of antiretroviral drugs on the pharmacodynamics of gliclazide with respect to glucose–insulin homeostasis in animal models | Effect of antiretroviral drugs on the pharmacodynamics of gliclazide with respect to glucose–insulin homeostasis in animal models Abstract The objective of this study was to investigate the effect of oral administration of antiretroviral drugs (indinavir, ritonavir, atazanavir, efavirenz and nevirapine) on the pharmaco... |
PMC9098589 | core_pubmed_pmc | Integrated multiple analytes and semi-mechanistic population pharmacokinetic model of tusamitamab ravtansine, a DM4 anti-CEACAM5 antibody-drug conjugate | Integrated multiple analytes and semi-mechanistic population pharmacokinetic model of tusamitamab ravtansine, a DM4 anti-CEACAM5 antibody-drug conjugate Abstract Tusamitamab ravtansine (SAR408701) is an antibody-drug conjugate (ADC), combining a humanized monoclonal antibody (IgG1) targeting carcinoembryonic antigen-re... |
PMC8706516 | core_pubmed_pmc | Spray-Dried Powder Formulation of Capreomycin Designed for Inhaled Tuberculosis Therapy | Spray-Dried Powder Formulation of Capreomycin Designed for Inhaled Tuberculosis Therapy Abstract Abstract Multi-drug-resistant tuberculosis (MDR-TB) is a huge public health problem. The treatment regimen of MDR-TB requires prolonged chemotherapy with multiple drugs including second-line anti-TB agents associated with s... |
PMC7744018 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of allopregnanolone as a regenerative therapeutic for Alzheimer's disease: A single and multiple ascending dose phase 1b/2a clinical trial | Safety, tolerability, and pharmacokinetics of allopregnanolone as a regenerative therapeutic for Alzheimer's disease: A single and multiple ascending dose phase 1b/2a clinical trial Abstract Abstract Introduction Allopregnanolone is an endogenous neurosteroid with the potential to be a novel regenerative therapeutic fo... |
PMC11450984 | core_pubmed_pmc | Safety and pharmacokinetic properties of a new formulation of parenteral artesunate in healthy Thai volunteers | Safety and pharmacokinetic properties of a new formulation of parenteral artesunate in healthy Thai volunteers Abstract Abstract Background Parenteral artesunate is the first-line therapy for severe malaria. Artesunate, in its current formulation, must be prepared immediately before administration by first dissolving i... |
PMC11879162 | core_pubmed_pmc | Activity of Rezafungin Against Echinocandin Non–wild type Candida glabrata Clinical Isolates From a Global Surveillance Program | Activity of Rezafungin Against Echinocandin Non–wild type Candida glabrata Clinical Isolates From a Global Surveillance Program Abstract Abstract Among 1463 Candida glabrata isolates collected in 39 US hospitals, 91 (6.2%) were non–wild type to ≥1 echinocandins (ECH-NWT) when tested by the Clinical and Laboratory Stand... |
PMC4690642 | core_pubmed_pmc | Comparative pharmacokinetics and pharmacodynamics of a PEGylated recombinant human growth hormone and daily recombinant human growth hormone in growth hormone-deficient children | Comparative pharmacokinetics and pharmacodynamics of a PEGylated recombinant human growth hormone and daily recombinant human growth hormone in growth hormone-deficient children Abstract Objective Recombinant human growth hormone (rhGH) replacement therapy in children generally requires daily subcutaneous (sc) injectio... |
PMC12749025 | core_pubmed_pmc | Pharmacodynamic interactions among meropenem ciprofloxacin and gentamicin in an in-vitro model | Pharmacodynamic interactions among meropenem ciprofloxacin and gentamicin in an in-vitro model Abstract Meropenem, gentamicin and ciprofloxacin are often used together as empiric broad-spectrum therapy in different combinations. Recent regulations regarding the use of quinolones mean that greater justification is requi... |
PMC10335304 | core_pubmed_pmc | ALESIA 5-Year Update: Alectinib at 600 mg Twice Daily Gives Lorlatinib a Run for Its Money in Asia | ALESIA 5-Year Update: Alectinib at 600 mg Twice Daily Gives Lorlatinib a Run for Its Money in Asia Abstract Abstract Alectinib, a next-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI), has demonstrated superior progression-free survival over crizotinib with both 300 mg twice daily (J-ALEX) or... |
PMC5677298 | core_pubmed_pmc | Squarticles as the nanoantidotes to sequester the overdosed antidepressant for detoxification | Squarticles as the nanoantidotes to sequester the overdosed antidepressant for detoxification Abstract The increasing death rate caused by drug overdose points to an urgent demand for the development of novel detoxification therapy. In an attempt to detoxify tricyclic antidepressant overdose, we prepared a lipid nanoem... |
PMC10747822 | core_pubmed_pmc | Bioanalysis of the Ex Vivo Labile PACE4 Inhibitory Peptide Ac-[ d- Leu]LLLRVK-Amba in Whole Blood Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Quantification | Bioanalysis of the Ex Vivo Labile PACE4 Inhibitory Peptide Ac-[ d- Leu]LLLRVK-Amba in Whole Blood Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Quantification Abstract The calcium-dependent serine endoprotease PACE4 is evaluated as a therapeutic target for prostate cancer. The peptide Ac-[ d -L... |
PMC10658592 | core_pubmed_pmc | Population pharmacokinetic analysis of enrofloxacin and its active metabolite ciprofloxacin after intravenous injection to cats with reduced kidney function | Population pharmacokinetic analysis of enrofloxacin and its active metabolite ciprofloxacin after intravenous injection to cats with reduced kidney function Abstract Abstract Background It is unknown if enrofloxacin accumulates in plasma of cats with reduced kidney function. Hypothesis To determine if enrofloxacin and ... |
PMC6492070 | core_pubmed_pmc | Impact of Subacute Exposure to T-2 Toxin and Zearalenone on the Pharmacokinetics of Midazolam as CYP3A Probe Drug in a Porcine Animal Model: A Pilot Study | Impact of Subacute Exposure to T-2 Toxin and Zearalenone on the Pharmacokinetics of Midazolam as CYP3A Probe Drug in a Porcine Animal Model: A Pilot Study Abstract Cytochrome P450 enzymes (CYP) are important catalyzing proteins involved in the biotransformation of endogenous and xenobiotic compounds. However, their exp... |
PMC10687399 | core_pubmed_pmc | Pharmacokinetic differences in nicotine and nicotine salts mediate reinforcement-related behavior: an animal model study | Pharmacokinetic differences in nicotine and nicotine salts mediate reinforcement-related behavior: an animal model study Abstract Since their introduction in the United States and Europe in 2007, electronic cigarettes (E-Cigs) have become increasingly popular among smokers. Nicotine, a key component in both tobacco and... |
PMC8401109 | core_pubmed_pmc | Janus Kinase Inhibitors and Coronavirus Disease (COVID)-19: Rationale, Clinical Evidence and Safety Issues | Janus Kinase Inhibitors and Coronavirus Disease (COVID)-19: Rationale, Clinical Evidence and Safety Issues Abstract We are witnessing a paradigm shift in drug development and clinical practice to fight the novel coronavirus disease (COVID-19), and a number of clinical trials have been or are being testing various pharm... |
PMC9652439 | core_pubmed_pmc | Manufacturing‐dependent change in biological activity of the TLR4 agonist GSK1795091 and implications for lipid A analog development | Manufacturing‐dependent change in biological activity of the TLR4 agonist GSK1795091 and implications for lipid A analog development Abstract Abstract A phase I trial ( NCT03447314 ; 204686) evaluated the safety and efficacy of GSK1795091, a Toll‐like receptor 4 (TLR4) agonist, in combination with immunotherapy (GSK317... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.