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PMC10847213 | core_pubmed_pmc | Evaluation of the Effect of Lorlatinib on CYP2B6, CYP2C9, UGT, and P-Glycoprotein Substrates in Patients with Advanced Non-Small Cell Lung Cancer | Evaluation of the Effect of Lorlatinib on CYP2B6, CYP2C9, UGT, and P-Glycoprotein Substrates in Patients with Advanced Non-Small Cell Lung Cancer Abstract Background and Objective Lorlatinib is a tyrosine kinase inhibitor approved for the treatment of advanced anaplastic lymphoma kinase–positive non-small cell lung can... |
PMC9808944 | core_pubmed_pmc | Safety of AFM11 in the treatment of patients with B-cell malignancies: findings from two phase 1 studies | Safety of AFM11 in the treatment of patients with B-cell malignancies: findings from two phase 1 studies Abstract Background The prognosis for patients with relapsed and/or refractory (R/R) non-Hodgkin’s lymphoma (NHL) or acute lymphoblastic leukaemia (ALL) remains poor, with existing treatments having significant side... |
PMC12827616 | core_pubmed_pmc | Unveiling abietic Acid’s therapeutic potential: a narrative review on structure-activity relationship, pharmacological properties, pharmacokinetics, and toxicological considerations | Unveiling abietic Acid’s therapeutic potential: a narrative review on structure-activity relationship, pharmacological properties, pharmacokinetics, and toxicological considerations Abstract Abietic acid (AA) is a carboxylic acid and a tricyclic diterpenoid that is found in a variety of coniferous resins. Its promising... |
PMC4833932 | core_pubmed_pmc | Cytotoxicity and cell cycle arrest induced by andrographolide lead to programmed cell death of MDA-MB-231 breast cancer cell line | Cytotoxicity and cell cycle arrest induced by andrographolide lead to programmed cell death of MDA-MB-231 breast cancer cell line Abstract Background Breast cancer is considered as an increasing major life-threatening concern among the malignancies encountered globally in females. Traditional therapy is far from satisf... |
PMC12379162 | core_pubmed_pmc | Value Addition to African Natural Product-Based Drug Discovery Initiatives | Value Addition to African Natural Product-Based Drug Discovery Initiatives Abstract Natural products are vital to drug discovery, yet Africa’s vast biodiversity remains underutilized. This perspective examines barriers limiting Africa’s impactsuch as weak infrastructure, limited translational capacity, and minimal int... |
PMC9723010 | core_pubmed_pmc | Leptomeningeal Metastases: New Opportunities in the Modern Era | Leptomeningeal Metastases: New Opportunities in the Modern Era Abstract Leptomeningeal metastases arise from cancer cell entry into the subarachnoid space, inflicting significant neurologic morbidity and mortality across a wide range of malignancies. The modern era of cancer therapeutics has seen an explosion of molecu... |
PMC8359440 | core_pubmed_pmc | Enantiomer‐specific pharmacokinetics of D,L‐3‐hydroxybutyrate: Implications for the treatment of multiple acyl‐CoA dehydrogenase deficiency | Enantiomer‐specific pharmacokinetics of D,L‐3‐hydroxybutyrate: Implications for the treatment of multiple acyl‐CoA dehydrogenase deficiency Abstract Abstract D,L‐3‐hydroxybutyrate (D,L‐3‐HB, a ketone body) treatment has been described in several inborn errors of metabolism, including multiple acyl‐CoA dehydrogenase def... |
PMC3266258 | core_pubmed_pmc | Fast Multispectral Optoacoustic Tomography (MSOT) for Dynamic Imaging of Pharmacokinetics and Biodistribution in Multiple Organs | Fast Multispectral Optoacoustic Tomography (MSOT) for Dynamic Imaging of Pharmacokinetics and Biodistribution in Multiple Organs Abstract The characterization of pharmacokinetic and biodistribution profiles is an essential step in the development process of new candidate drugs or imaging agents. Simultaneously, the ass... |
PMC10582389 | core_pubmed_pmc | Widespread in vivo efficacy of The-0504: A conditionally-activatable nanoferritin for tumor-agnostic targeting of CD71-expressing cancers | Widespread in vivo efficacy of The-0504: A conditionally-activatable nanoferritin for tumor-agnostic targeting of CD71-expressing cancers Abstract Abstract Background Cancer is still among the leading causes of death all over the world. Improving chemotherapy and minimizing associated toxicities are major unmet medical... |
PMC3670507 | core_pubmed_pmc | Phase I study of tremelimumab (CP-675 206) plus PF-3512676 (CPG 7909) in patients with melanoma or advanced solid tumours | Phase I study of tremelimumab (CP-675 206) plus PF-3512676 (CPG 7909) in patients with melanoma or advanced solid tumours Abstract Background: Tremelimumab, a fully human cytotoxic T-lymphocyte antigen 4 monoclonal antibody, and PF-3512676, a Toll-like receptor-9 agonist, are targeted immune modulators that elicit dura... |
PMC10285615 | core_pubmed_pmc | Synthesis and biological evaluation of novel β-lactam-metallo β-lactamase inhibitors † | Synthesis and biological evaluation of novel β-lactam-metallo β-lactamase inhibitors † Abstract Abstract β-lactamases are enzymes that deactivate β-lactam antibiotics through a hydrolysis mechanism. There are two known types of β-lactamases: serine β-lactamases (SBLs) and metallo β-lactamases (MBLs). The two existing s... |
PMC9868327 | core_pubmed_pmc | Design of an adaptive randomized clinical trial of intravenous citrulline for sickle cell pain crisis in the emergency department | Design of an adaptive randomized clinical trial of intravenous citrulline for sickle cell pain crisis in the emergency department Abstract Abstract Background Vaso-occlusive pain crisis (VOC) is the most frequent cause for Emergency Department (ED) visits and hospital admissions for patients with sickle cell disease (S... |
PMC12161439 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of two dosing regimens of antenatal corticosteroids: protocol for a prospective nested study in a randomised controlled trial | Population pharmacokinetics and pharmacodynamics of two dosing regimens of antenatal corticosteroids: protocol for a prospective nested study in a randomised controlled trial Abstract Abstract Introduction Antenatal corticosteroid (ACS) regimens have remained unchanged since the initial trials in 1972, with the optimal... |
PMC8039805 | core_pubmed_pmc | Structure-based identification of SARS-CoV-2 main protease inhibitors from anti-viral specific chemical libraries: an exhaustive computational screening approach | Structure-based identification of SARS-CoV-2 main protease inhibitors from anti-viral specific chemical libraries: an exhaustive computational screening approach Abstract Abstract Worldwide coronavirus disease 2019 (COVID-19) outbreak is still threatening global health since its outbreak first reported in the late 2019... |
PMC3617128 | core_pubmed_pmc | Pharmacometabolomic Approach to Predict QT Prolongation in Guinea Pigs | Pharmacometabolomic Approach to Predict QT Prolongation in Guinea Pigs Abstract Drug-induced torsades de pointes (TdP), a life-threatening arrhythmia associated with prolongation of the QT interval, has been a significant reason for withdrawal of several medicines from the market. Prolongation of the QT interval is con... |
PMC10132043 | core_pubmed_pmc | Repeat Ivermectin Mass Drug Administrations for Malaria Control II: Protocol for a Double-blind, Cluster-Randomized, Placebo-Controlled Trial for the Integrated Control of Malaria | Repeat Ivermectin Mass Drug Administrations for Malaria Control II: Protocol for a Double-blind, Cluster-Randomized, Placebo-Controlled Trial for the Integrated Control of Malaria Abstract Abstract Background The gains made against malaria have stagnated since 2015, threatened further by increasing resistance to insect... |
PMC3978528 | core_pubmed_pmc | Development of a Physiologically-Based Pharmacokinetic Model of the Rat Central Nervous System | Development of a Physiologically-Based Pharmacokinetic Model of the Rat Central Nervous System Abstract Abstract Central nervous system (CNS) drug disposition is dictated by a drug’s physicochemical properties and its ability to permeate physiological barriers. The blood–brain barrier (BBB), blood-cerebrospinal fluid b... |
PMC11962451 | core_pubmed_pmc | Flycodes enable simultaneous preclinical analysis for dozens of antibodies in single cassette–dosed mice | Flycodes enable simultaneous preclinical analysis for dozens of antibodies in single cassette–dosed mice Abstract Significance During discovery and development of protein-based biotherapeutics, extensive preclinical animal testing is required for assessment of drug behavior, efficacy, and safety. Generally, numerous an... |
PMC10777233 | core_pubmed_pmc | Antibiotics in anesthesia and critical care | Antibiotics in anesthesia and critical care Abstract Abstract Sepsis is life-threatening organ dysfunction due to a dysregulated host response to an underlying acute infection. Sepsis is a major worldwide healthcare problem. An annual estimated 48.9 million incident cases of sepsis is reported, with 11 million (20%) se... |
PMC8813547 | core_pubmed_pmc | Therapeutic dilemmas in addressing SARS-CoV-2 infection: Favipiravir versus Remdesivir | Therapeutic dilemmas in addressing SARS-CoV-2 infection: Favipiravir versus Remdesivir Abstract Coronavirus disease 2019 (COVID-19) represents an unmet clinical need, due to a high mortality rate, rapid mutation rate in the virus, increased chances of reinfection, lack of effectiveness of repurposed drugs and economic ... |
PMC3615532 | core_pubmed_pmc | Drug and Disease Model Resources: A Consortium to Create Standards and Tools to Enhance Model-Based Drug Development | Drug and Disease Model Resources: A Consortium to Create Standards and Tools to Enhance Model-Based Drug Development Abstract Abstract Model-based drug development (MBDD) is accepted as a vital approach in understanding patients' drug-related benefit and risk by integrating quantitative information integration from div... |
PMC5783989 | core_pubmed_pmc | Validation of a Model Predicting Anti-infective Lung Penetration in the Epithelial Lining Fluid of Humans | Validation of a Model Predicting Anti-infective Lung Penetration in the Epithelial Lining Fluid of Humans Methods Methods We searched the PubMed database and relevant microbiology conference abstracts for clinical studies reporting anti-infective ELF and plasma concentrations in humans between year 2011 and 2017. We al... |
PMC10644327 | core_pubmed_pmc | A randomized, double‐blind phase 1b study evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of the NLRP3 inhibitor selnoflast in patients with moderate to severe active ulcerative colitis | A randomized, double‐blind phase 1b study evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of the NLRP3 inhibitor selnoflast in patients with moderate to severe active ulcerative colitis Abstract Abstract Background The NLRP3 inflammasome drives release of pro‐inflammatory cytokines including ... |
PMC10747499 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modelling of Cabotegravir Microarray Patches in Rats and Humans | Physiologically Based Pharmacokinetic Modelling of Cabotegravir Microarray Patches in Rats and Humans Abstract Microarray patches (MAPs) are currently under investigation as a self-administered, pain-free alternative used to achieve long-acting (LA) drug delivery. Cabotegravir is a potent antiretroviral that has demons... |
PMC7248076 | core_pubmed_pmc | A biomathematical model of human erythropoiesis and iron metabolism | A biomathematical model of human erythropoiesis and iron metabolism Abstract Abstract Anaemia therapy or perisurgical support of erythropoiesis often require both, EPO and iron medication. However, excessive iron medication can result in iron overload and it is challenging to control haemoglobin levels in a desired ran... |
PMC5994321 | core_pubmed_pmc | Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects | Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects Abstract Propofol is an intravenous short-acting anesthetic widely used to induce and maintain general anesthesia and to provide procedural sedation. The potential for propofol dependency and abuse has been recognized, and seve... |
PMC11224070 | core_pubmed_pmc | Development of a target concentration intervention to individualize paroxysmal nocturnal hemoglobinuria treatment with pegcetacoplan | Development of a target concentration intervention to individualize paroxysmal nocturnal hemoglobinuria treatment with pegcetacoplan Abstract Abstract Pegcetacoplan (Aspaveli®/Empaveli™) is a factor C3 inhibitor that is approved for the treatment of paroxysmal nocturnal hemoglobinuria. An individualized dosing strategy... |
PMC8968060 | core_pubmed_pmc | Arsenic trioxide for acute promyelocytic leukemia in a patient on chronic hemodialysis | Arsenic trioxide for acute promyelocytic leukemia in a patient on chronic hemodialysis Abstract Acute promyelocytic leukemia (APL) is a rare acute leukemia generally considered curable with all-trans retinoic acid (ATRA) and arsenic trioxide (ATO). Some patients have co-morbidities that may limit the use of these agent... |
PMC11145865 | core_pubmed_pmc | Evaluation the kill rate and mutant selection window of danofloxacin against Actinobacillus pleuropneumoniae in a peristaltic pump model | Evaluation the kill rate and mutant selection window of danofloxacin against Actinobacillus pleuropneumoniae in a peristaltic pump model Abstract Background Actinobacillus pleuropneumoniae is a serious pathogen in pigs. The abundant application of antibiotics has resulted in the gradual emergence of drugresistant bacte... |
PMC11307714 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of a Novel Human Hepatitis B Virus Capsid Assembly Modulator Canocapavir: A Randomized First-in-Human Study | Safety, Tolerability, and Pharmacokinetics of a Novel Human Hepatitis B Virus Capsid Assembly Modulator Canocapavir: A Randomized First-in-Human Study Abstract Background and Aims Canocapavir (ZM-H1505R) is a small-molecule hepatitis B virus capsid assembly modulator with a novel pyrazole structure. This is the first-i... |
PMC7957728 | core_pubmed_pmc | Quantitative Dynamic 18 F-FDG PET/CT in Survival Prediction of Metastatic Melanoma under PD-1 Inhibitors | Quantitative Dynamic 18 F-FDG PET/CT in Survival Prediction of Metastatic Melanoma under PD-1 Inhibitors Abstract Abstract Simple Summary The reliable and early during-the-course-of-treatment assessment of tumor response to the novel immunotherapeutic agents is a matter of debate, posing relevant challenges to conventi... |
PMC9781129 | core_pubmed_pmc | Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats | Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats Abstract Abstract Tetrahydroisoquinolines have been widely investigated for the treatment of arrhythmias. 1−(3′−bromophenyl)−heliamine (BH), an anti−arrhythmias agent, is a synthetic tetrahydroisoquinoline. This study focuses on... |
PMC7485950 | core_pubmed_pmc | Population and Noncompartmental Pharmacokinetics of Sodium Oxybate Support Weight‐Based Dosing in Children and Adolescents With Narcolepsy With Cataplexy | Population and Noncompartmental Pharmacokinetics of Sodium Oxybate Support Weight‐Based Dosing in Children and Adolescents With Narcolepsy With Cataplexy Abstract Abstract The pharmacokinetics (PKs) of sodium oxybate (SXB) was evaluated in a subset of participants from a study of SXB treatment in children (aged 7–11 ye... |
PMC6090978 | core_pubmed_pmc | A phase II clinical trial of the Aurora and angiogenic kinase inhibitor ENMD-2076 for previously treated, advanced, or metastatic triple-negative breast cancer | A phase II clinical trial of the Aurora and angiogenic kinase inhibitor ENMD-2076 for previously treated, advanced, or metastatic triple-negative breast cancer Abstract Background Triple-negative breast cancer (TNBC) remains an aggressive breast cancer subtype with limited treatment options. ENMD-2076 is a small-molecu... |
PMC12658823 | core_pubmed_pmc | Targeting SUMOylation with Anacardic Acid Derivatives: Novel Insights into EGF Pathway Dysregulation in Cancer Using an In Silico Approach | Targeting SUMOylation with Anacardic Acid Derivatives: Novel Insights into EGF Pathway Dysregulation in Cancer Using an In Silico Approach Abstract SUMOylation is a critical post-translational modification pathway implicated in various ailments, such as diabetes, neurodegenerative disorders, infectious diseases, and ca... |
PMC8582555 | core_pubmed_pmc | Application of High-Z Gold Nanoparticles in Targeted Cancer Radiotherapy—Pharmacokinetic Modeling, Monte Carlo Simulation and Radiobiological Effect Modeling | Application of High-Z Gold Nanoparticles in Targeted Cancer Radiotherapy—Pharmacokinetic Modeling, Monte Carlo Simulation and Radiobiological Effect Modeling Abstract Simple Summary High-Z gold nanoparticles show potential as radiosensitizers in the radiotherapy of cancer. In this paper, we introduce the benefits and p... |
PMC4814628 | core_pubmed_pmc | Achievement of Vancomycin Therapeutic Goals in Critically Ill Patients: Early Individualization May Be Beneficial | Achievement of Vancomycin Therapeutic Goals in Critically Ill Patients: Early Individualization May Be Beneficial Abstract Objective. The aim of our study was to assess and validate the effectiveness of early dose adjustment of vancomycin based on first dose monitoring in achieving target recommended goal in critically... |
PMC9371077 | core_pubmed_pmc | A QbD Approach to Design and to Optimize the Self-Emulsifying Resveratrol–Phospholipid Complex to Enhance Drug Bioavailability through Lymphatic Transport | A QbD Approach to Design and to Optimize the Self-Emulsifying Resveratrol–Phospholipid Complex to Enhance Drug Bioavailability through Lymphatic Transport Abstract Highlights The FTIR, DSC, and the XRD characterization confirmed the successful complex formation between resveratrol and phospholipid. The optimal SEDDS fo... |
PMC12307566 | core_pubmed_pmc | Teclistamab Dosing in Responders: Modeling and Simulation Results from the MajesTEC-1 Study in Relapsed/Refractory Multiple Myeloma | Teclistamab Dosing in Responders: Modeling and Simulation Results from the MajesTEC-1 Study in Relapsed/Refractory Multiple Myeloma Abstract Background Based on the phase I/II MajesTEC-1 study, the B-cell maturation antigen (BCMA) and cluster of differentiation (CD)3 bispecific antibody, teclistamab, is approved for re... |
PMC6278279 | core_pubmed_pmc | Effects of Red Ginseng Extract on the Pharmacokinetics and Elimination of Methotrexate via Mrp2 Regulation | Effects of Red Ginseng Extract on the Pharmacokinetics and Elimination of Methotrexate via Mrp2 Regulation Abstract We aimed to investigate the effects of red ginseng extract (RGE) on the expression of efflux transporters and to study the pharmacokinetics of representative substrate. For this, rats received single or r... |
PMC10754993 | core_pubmed_pmc | Optimization of pharmacological interventions in the guinea pig animal model—a new approach to calculate the perilymph volume of the scala tympani | Optimization of pharmacological interventions in the guinea pig animal model—a new approach to calculate the perilymph volume of the scala tympani Abstract Abstract Objective The guinea pig serves as a well-established animal model for inner ear research, offering valuable insights into the anatomy, physiology, and the... |
PMC8418037 | core_pubmed_pmc | Immunomodulatory effect of standardized C. asiatica extract on a promotion of regulatory T cells in rats | Immunomodulatory effect of standardized C. asiatica extract on a promotion of regulatory T cells in rats Abstract Abstract Background ECa 233 is a standardized extract of C. asiatica containing the triterpenoid glycosides, madecassoside to asiaticoside in the ratio of (1.5 ± 0.5):1. Anti-inflammatory activities of ECa ... |
PMC4366384 | core_pubmed_pmc | Pharmacokinetics (PK), Pharmacodynamics (PD) and Integrated PK/PD Modeling of a Novel Long Acting FGF21 Clinical Candidate PF-05231023 in Diet-Induced Obese and Leptin-Deficient Obese Mice | Pharmacokinetics (PK), Pharmacodynamics (PD) and Integrated PK/PD Modeling of a Novel Long Acting FGF21 Clinical Candidate PF-05231023 in Diet-Induced Obese and Leptin-Deficient Obese Mice Abstract Pharmacological administration of fibroblast growth factor 21 (FGF21) improves metabolic profile in preclinical species an... |
PMC5053749 | core_pubmed_pmc | Changes in cytochrome P450s-mediated drug clearance in patients with hepatocellular carcinoma in vitro and in vivo : a bottom-up approach | Changes in cytochrome P450s-mediated drug clearance in patients with hepatocellular carcinoma in vitro and in vivo : a bottom-up approach Abstract Abstract Hepatocellular carcinoma (HCC) accompanied by severe liver dysfunction is a serious disease, which results in altered hepatic clearance. Generally, maintenance dose... |
PMC4926482 | core_pubmed_pmc | Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers | Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers Abstract Abstract R-α-lipoic acid (R-LA) is a cofactor of mitochondrial enzymes and a very strong antioxidant. R-LA is available as a functional food ingredient but is unstable against heat or acid. Stabilized R-LA was prepared through c... |
PMC4919356 | core_pubmed_pmc | Measurements of Deposition, Lung Surface Area and Lung Fluid for Simulation of Inhaled Compounds | Measurements of Deposition, Lung Surface Area and Lung Fluid for Simulation of Inhaled Compounds Abstract Modern strategies in drug development employ in silico techniques in the design of compounds as well as estimations of pharmacokinetics, pharmacodynamics and toxicity parameters. The quality of the results depends ... |
PMC11881275 | core_pubmed_pmc | In vitro and in silico evaluation of synthetic compounds derived from bi-triazoles against asexual and sexual forms of Plasmodium falciparum | In vitro and in silico evaluation of synthetic compounds derived from bi-triazoles against asexual and sexual forms of Plasmodium falciparum Abstract Background Despite advances in malaria chemotherapy, the disease continues to claim thousands of lives annually. Addressing this issue requires the discovery of new compo... |
PMC11830758 | core_pubmed_pmc | Simultaneous Determination of Multiple Acid-Suppressing Drugs by UPLC-MS/MS Method and Application for Pharmacokinetics Study | Simultaneous Determination of Multiple Acid-Suppressing Drugs by UPLC-MS/MS Method and Application for Pharmacokinetics Study Abstract Background Proton pump inhibitors (PPIs) and potassium competitive acid blockers (P-CABs) are widely used to treat acid-related diseases (ARDs). Precisely quantifying their plasma level... |
PMC5440538 | core_pubmed_pmc | Efficacy and safety of paricalcitol in children with stages 3 to 5 chronic kidney disease | Efficacy and safety of paricalcitol in children with stages 3 to 5 chronic kidney disease Abstract Abstract Background Elevated intact parathyroid hormone (iPTH) levels can contribute to morbidity and mortality in children with chronic kidney disease (CKD). We evaluated the pharmacokinetics, efficacy, and safety of ora... |
PMC9992188 | core_pubmed_pmc | PBPK modeling to evaluate maximum tolerated doses: A case study with 3-chloroallyl alcohol | PBPK modeling to evaluate maximum tolerated doses: A case study with 3-chloroallyl alcohol Abstract Abstract Introduction: A physiologically based pharmacokinetic (PBPK) model for 3-chloroallyl alcohol (3-CAA) was developed and used to evaluate the design of assays for the in vivo genotoxicity of 3-CAA. Methods: Model ... |
PMC5974002 | core_pubmed_pmc | Clinical Pharmacokinetic and Pharmacodynamic Profile of Riociguat | Clinical Pharmacokinetic and Pharmacodynamic Profile of Riociguat Abstract Abstract Oral riociguat is a soluble guanylate cyclase (sGC) stimulator that targets the nitric oxide (NO)–sGC–cyclic guanosine monophosphate pathway with a dual mode of action: directly by stimulating sGC, and indirectly by increasing the sensi... |
PMC5514005 | core_pubmed_pmc | Development of a sandwich enzyme-linked immunosorbent assay for dTMP-GH fusion protein by rational immunogen selection | Development of a sandwich enzyme-linked immunosorbent assay for dTMP-GH fusion protein by rational immunogen selection Abstract dTMP-GH is a chimeric protein containing a tandem dimer of thrombopoietin mimetic peptide (dTMP) fused to human growth hormone (hGH) prepared previously by our team. It shows significant bioac... |
PMC10720796 | core_pubmed_pmc | Exploring the complex relationship between vitamin K, gut microbiota, and warfarin variability in cardiac surgery patients | Exploring the complex relationship between vitamin K, gut microbiota, and warfarin variability in cardiac surgery patients Abstract Background and objectives: Due to the high individual variability of anticoagulant warfarin, this study aimed to investigate the effects of vitamin K concentration and gut microbiota on in... |
PMC7023481 | core_pubmed_pmc | A Mechanistic Physiologically-Based Biopharmaceutics Modeling (PBBM) Approach to Assess the In Vivo Performance of an Orally Administered Drug Product: From IVIVC to IVIVP | A Mechanistic Physiologically-Based Biopharmaceutics Modeling (PBBM) Approach to Assess the In Vivo Performance of an Orally Administered Drug Product: From IVIVC to IVIVP Abstract The application of in silico modeling to predict the in vivo outcome of an oral drug product is gaining a lot of interest. Fully relying on... |
PMC8764296 | core_pubmed_pmc | Self-Assembled Micellar Glutaminase Allosteric Inhibitor for Effective Therapeutic Intervention | Self-Assembled Micellar Glutaminase Allosteric Inhibitor for Effective Therapeutic Intervention Abstract Introduction Kidney-type glutaminase (KGA) has been an important anti-tumor drug target, and KGA allosteric inhibitors attracted much interest for their superior enzymatic specificity with good drug safety profiles.... |
PMC12687824 | core_pubmed_pmc | Mechanistic model of phase-transitioning therapeutics injected into poroelastic tissue for improved targeting of superficial tumors | Mechanistic model of phase-transitioning therapeutics injected into poroelastic tissue for improved targeting of superficial tumors Abstract Abstract The development of new drugs and drug delivery systems relies heavily on careful acquisition and interpretation of large amounts of experimental data, to identify and sel... |
PMC9989027 | core_pubmed_pmc | An overview of clinical cerebral microdialysis in acute brain injury | An overview of clinical cerebral microdialysis in acute brain injury Abstract Cerebral microdialysis may be used in patients with severe brain injury to monitor their cerebral physiology. In this article we provide a concise synopsis with illustrations and original images of catheter types, their structure, and how the... |
PMC10085897 | core_pubmed_pmc | Population Pharmacokinetics and Dosing Simulations of Ampicillin and Sulbactam in Hospitalised Adult Patients | Population Pharmacokinetics and Dosing Simulations of Ampicillin and Sulbactam in Hospitalised Adult Patients Abstract Background The pharmacokinetic variability of ampicillin-sulbactam in adults has not been extensively described, particularly in patients with a reduced renal function (i.e., < 60 mL/min). Objective Th... |
PMC4937626 | core_pubmed_pmc | Evaluation of bioequivalence of five 0.1 mg dutasteride capsules compared to one 0.5 mg dutasteride capsule: a randomized study in healthy male volunteers | Evaluation of bioequivalence of five 0.1 mg dutasteride capsules compared to one 0.5 mg dutasteride capsule: a randomized study in healthy male volunteers Abstract Abstract Objective To evaluate the bioequivalence of five 0.1 mg dutasteride capsules to one 0.5 mg dutasteride capsule in healthy adult male subjects under... |
PMC11100960 | core_pubmed_pmc | Combined ROS Sensitive Folate Receptor Targeted Micellar Formulations of Curcumin Effective Against Rheumatoid Arthritis in Rat Model | Combined ROS Sensitive Folate Receptor Targeted Micellar Formulations of Curcumin Effective Against Rheumatoid Arthritis in Rat Model Abstract Introduction Rheumatoid arthritis (RA) is an inflammatory immune-mediated disease that involves synovitis, cartilage destruction, and even joint damage. Traditional agents used ... |
PMC10014056 | core_pubmed_pmc | A “middle‐out approach” for the prediction of human drug disposition from preclinical data using simplified physiologically based pharmacokinetic (PBPK) models | A “middle‐out approach” for the prediction of human drug disposition from preclinical data using simplified physiologically based pharmacokinetic (PBPK) models Abstract Abstract Simplified physiologically based pharmacokinetic (PBPK) models using estimated tissue‐to‐unbound plasma partition coefficients (Kpus) were pre... |
PMC7041323 | core_pubmed_pmc | A Randomized, Double-Blinded, Placebo-Controlled, Dose-Escalation Phase 1 Study of Aerosolized Pirfenidone Delivered via the PARI Investigational eFlow Nebulizer in Volunteers and Patients with Idiopathic Pulmonary Fibrosis | A Randomized, Double-Blinded, Placebo-Controlled, Dose-Escalation Phase 1 Study of Aerosolized Pirfenidone Delivered via the PARI Investigational eFlow Nebulizer in Volunteers and Patients with Idiopathic Pulmonary Fibrosis Abstract Background: This clinical trial evaluated the pharmacokinetics and safety/tolerability ... |
PMC11273447 | core_pubmed_pmc | Extended Pharmacokinetics Improve Site-Specific Prodrug Activation Using Radiation | Extended Pharmacokinetics Improve Site-Specific Prodrug Activation Using Radiation Abstract Radiotherapy is commonly used to treat cancer, and localized energy deposited by radiotherapy has the potential to chemically uncage prodrugs; however, it has been challenging to demonstrate prodrug activation that is both susta... |
PMC10480607 | core_pubmed_pmc | Network pharmacology-guided and TCM theory-supported in vitro and in vivo component identification of Naoluoxintong | Network pharmacology-guided and TCM theory-supported in vitro and in vivo component identification of Naoluoxintong Abstract Naoluoxintong (NLXT) has been used to treat ischemic stroke (IS) in China for more than two hundred years. However, the pharmacodynamic material basis of NLXT has not been fully studied. Under th... |
PMC7054494 | core_pubmed_pmc | Ocular and Systemic Pharmacokinetics of Brimonidine and Timolol After Topical Administration in Rabbits: Comparison Between Fixed-Combination and Single Drugs | Ocular and Systemic Pharmacokinetics of Brimonidine and Timolol After Topical Administration in Rabbits: Comparison Between Fixed-Combination and Single Drugs Abstract Introduction This study was aimed to compare ocular tissue distribution and systemic exposure of brimonidine and timolol after single topical administra... |
PMC11204409 | core_pubmed_pmc | Targeted Liposomal Drug Delivery: Overview of the Current Applications and Challenges | Targeted Liposomal Drug Delivery: Overview of the Current Applications and Challenges Abstract Abstract In drug development, it is not uncommon that an active substance exhibits efficacy in vitro but lacks the ability to specifically reach its target in vivo. As a result, targeted drug delivery has become a primary foc... |
PMC8846629 | core_pubmed_pmc | Step‐by‐step comparison of ordinary differential equation and agent‐based approaches to pharmacokinetic‐pharmacodynamic models | Step‐by‐step comparison of ordinary differential equation and agent‐based approaches to pharmacokinetic‐pharmacodynamic models Abstract Abstract Mathematical models in oncology aid in the design of drugs and understanding of their mechanisms of action by simulation of drug biodistribution, drug effects, and interaction... |
PMC4627342 | core_pubmed_pmc | Lapatinib promotes the incidence of hepatotoxicity by increasing chemotherapeutic agent accumulation in hepatocytes | Lapatinib promotes the incidence of hepatotoxicity by increasing chemotherapeutic agent accumulation in hepatocytes Abstract Lapatinib has been used in combination with capecitabine or paclitaxel to treat patients with progressive HER2-overexpressing metastatic breast cancer (MBC). Unfortunately, an increased incidence... |
PMC8966223 | core_pubmed_pmc | A PBPK Model of Ternary Cyclodextrin Complex of ST-246 Was Built to Achieve a Reasonable IV Infusion Regimen for the Treatment of Human Severe Smallpox | A PBPK Model of Ternary Cyclodextrin Complex of ST-246 Was Built to Achieve a Reasonable IV Infusion Regimen for the Treatment of Human Severe Smallpox Abstract ST-246 is an oral drug against pathogenic orthopoxvirus infections. An intravenous formulation is required for some critical patients. A ternary complex of ST-... |
PMC4351929 | core_pubmed_pmc | Population pharmacokinetic modeling of the Qishe pill in three major traditional Chinese medicine-defined constitutional types of healthy Chinese subjects: study protocol for a randomized controlled trial | Population pharmacokinetic modeling of the Qishe pill in three major traditional Chinese medicine-defined constitutional types of healthy Chinese subjects: study protocol for a randomized controlled trial Abstract Abstract Background High incidences of neck pain morbidity are challenging in various situations for popul... |
PMC5944200 | core_pubmed_pmc | Determination of Tobramycin in M 9 Medium by LC-MS/MS: Signal Enhancement by Trichloroacetic Acid | Determination of Tobramycin in M 9 Medium by LC-MS/MS: Signal Enhancement by Trichloroacetic Acid Abstract Abstract It is well known that ion-pairing reagents cause ion suppression in LC-MS/MS methods. Here, we report that trichloroacetic acid increases the MS signal of tobramycin. To support studies of an in vitro pha... |
PMC12579034 | core_pubmed_pmc | Cenegermin for the Treatment of Moderate or Severe Neurotrophic Keratopathy: Results from a Prospective, Phase IV, Open-Label Study in China | Cenegermin for the Treatment of Moderate or Severe Neurotrophic Keratopathy: Results from a Prospective, Phase IV, Open-Label Study in China Abstract Introduction Neurotrophic keratopathy (NK) is a rare degenerative disease that can lead to epithelial breakdown, corneal ulceration, and potentially perforation and visio... |
PMC12149175 | core_pubmed_pmc | Dose-dependent immunotoxic mechanisms of celastrol via modulation of the PI3K-Akt signaling pathway | Dose-dependent immunotoxic mechanisms of celastrol via modulation of the PI3K-Akt signaling pathway Abstract Ethnopharmacological relevance Celastrol, a bioactive compound from Tripterygium wilfordii Hook.f. , is known for its anti-inflammatory and immunomodulatory effects, but its immunotoxicity is underexplored. This... |
PMC3820275 | core_pubmed_pmc | CYP2A6 Genotype but not Age Determines Cotinine Half-life in Infants and Children | CYP2A6 Genotype but not Age Determines Cotinine Half-life in Infants and Children Abstract The formation of cotinine, the main proximate metabolite and a biomarker of nicotine exposure, is mediated primarily by CYP2A6. Our aim was to determine if higher cotinine levels in young children exposed to secondhand smoke (SHS... |
PMC8746472 | core_pubmed_pmc | Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms | Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms Abstract Grifolin is a volatile compound contained in essential oils of several medicinal plants. Several studies show that this substance has been the subject of numerous pharmacological investigations, which have yielded interesting results. Grifo... |
PMC6005348 | core_pubmed_pmc | Betahistine Treatment in a Cat Model of Vestibular Pathology: Pharmacokinetic and Pharmacodynamic Approaches | Betahistine Treatment in a Cat Model of Vestibular Pathology: Pharmacokinetic and Pharmacodynamic Approaches Abstract Abstract This study is a pharmacokinetic (PK) and pharmacodynamics (PD) approach using betahistine doses levels in unilateral vestibular neurectomized cats (UVN) comparable to those used in humans for t... |
PMC11997996 | core_pubmed_pmc | Development of [ 99m Tc]TcO-ABX474: Design, Synthesis, and Biological Evaluation of PSMA-Binding Technetium-99m Radioligands for SPECT Imaging of Prostate Cancer | Development of [ 99m Tc]TcO-ABX474: Design, Synthesis, and Biological Evaluation of PSMA-Binding Technetium-99m Radioligands for SPECT Imaging of Prostate Cancer Abstract A current global limitation to the timely and equitable patient access to PSMA-based therapies for prostate cancer (PCa) is the insufficient PET capa... |
PMC6601550 | core_pubmed_pmc | An in vitro FcRn- dependent transcytosis assay as a screening tool for predictive assessment of nonspecific clearance of antibody therapeutics in humans | An in vitro FcRn- dependent transcytosis assay as a screening tool for predictive assessment of nonspecific clearance of antibody therapeutics in humans Abstract ABSTRACT A cell-based assay employing Madin–Darby canine kidney cells stably expressing human neonatal Fc receptor (FcRn) heavy chain and β2-microglobulin gen... |
PMC4715717 | core_pubmed_pmc | Activity and Toxicity of Intravenous Erwinia Asparaginase Following Allergy to E . coli ‐Derived Asparaginase in Children and Adolescents With Acute Lymphoblastic Leukemia | Activity and Toxicity of Intravenous Erwinia Asparaginase Following Allergy to E . coli ‐Derived Asparaginase in Children and Adolescents With Acute Lymphoblastic Leukemia Abstract Abstract Background Erwinia asparaginase is antigenically distinct from E.coli ‐derived asparaginase and may be used after E.coli ‐derived ... |
PMC12617562 | core_pubmed_pmc | Design and pharmacodynamic study of live biotherapeutic products with efficient degradation of branched‐chain amino acids | Design and pharmacodynamic study of live biotherapeutic products with efficient degradation of branched‐chain amino acids Abstract Abstract The homeostasis of branched‐chain amino acids (BCAAs) plays a crucial role in maintaining health, and the accumulation of BCAAs can lead to various diseases. Therefore, exogenous d... |
PMC8660086 | core_pubmed_pmc | Herb-Drug Interaction Between Xiyanping Injection and Lopinavir/Ritonavir, Two Agents Used in COVID-19 Pharmacotherapy | Herb-Drug Interaction Between Xiyanping Injection and Lopinavir/Ritonavir, Two Agents Used in COVID-19 Pharmacotherapy Abstract The global epidemic outbreak of the coronavirus disease 2019 (COVID-19), which exhibits high infectivity, resulted in thousands of deaths due to the lack of specific drugs. Certain traditional... |
PMC12439289 | core_pubmed_pmc | Predicting Drug Transfer Into Human Milk With the Simcyp Simulator: A Contribution From the ConcePTION Project | Predicting Drug Transfer Into Human Milk With the Simcyp Simulator: A Contribution From the ConcePTION Project Abstract ABSTRACT Physiologically‐based pharmacokinetic (PBPK) modeling can support decision‐making on maternal medication use during breastfeeding. This study aimed to enhance lactation PBPK models in two way... |
PMC12603884 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Modeling of Clonidine and Midazolam for Sedation in Pediatric Intensive Care | Pharmacokinetic and Pharmacodynamic Modeling of Clonidine and Midazolam for Sedation in Pediatric Intensive Care Abstract ABSTRACT Background Clonidine and midazolam are routinely used in the pediatric intensive care unit for pain and sedation management, but target concentration and optimal dose are poorly defined for... |
PMC12624468 | core_pubmed_pmc | Using a PBPK Model Incorporating Lymphatic Absorption to Predict Food Effect, Multiple Dosing, and Hepatic Impairment of Cannabidiol | Using a PBPK Model Incorporating Lymphatic Absorption to Predict Food Effect, Multiple Dosing, and Hepatic Impairment of Cannabidiol Abstract ABSTRACT Cannabidiol (CBD) is one of the most extensively studied cannabinoids and is used for myriad conditions. Its oral pharmacokinetics are complex, exhibiting non‐linear abs... |
PMC6325194 | core_pubmed_pmc | Effect of Rifampin-Isoniazid-Containing Antituberculosis Therapy on Efavirenz Pharmacokinetics in HIV-Infected Children 3 to 14 Years Old | Effect of Rifampin-Isoniazid-Containing Antituberculosis Therapy on Efavirenz Pharmacokinetics in HIV-Infected Children 3 to 14 Years Old Abstract We compared efavirenz pharmacokinetic (PK) parameters in children with tuberculosis (TB)/human immunodeficiency virus (HIV) coinfection on and off first-line antituberculosi... |
PMC9337276 | core_pubmed_pmc | Assessment of the pharmacokinetics, removal rate of hemodialysis, and safety of lactulose in hemodialysis patients | Assessment of the pharmacokinetics, removal rate of hemodialysis, and safety of lactulose in hemodialysis patients Abstract Lactulose is often used to treat hepatic encephalopathy or constipation, and also exhibits benefits to chronic renal insufficiency due to reduce nitrogen-related products in serum. The present stu... |
PMC12135038 | core_pubmed_pmc | Enantiomeric Excess Bupivacaine in a Lavender Oil NLC Tested in a Melanoma Model: Prolonged Release and Anticancer Effect | Enantiomeric Excess Bupivacaine in a Lavender Oil NLC Tested in a Melanoma Model: Prolonged Release and Anticancer Effect Abstract Recent studies have highlighted the potential of local anesthetics (LA) as adjuvants in cancer treatment, specifically by increasing survival rates when used in surgical excisions. However,... |
PMC7811992 | core_pubmed_pmc | Population Pharmacokinetics of Cariprazine and its Major Metabolites | Population Pharmacokinetics of Cariprazine and its Major Metabolites Abstract Abstract Background and Objectives Cariprazine, a dopamine D 3 -preferring D 3 /D 2 receptor partial agonist, is approved for the treatment of adults with schizophrenia (1.5–6 mg/day) and manic/mixed (3–6 mg/day) episodes associated with bipo... |
PMC11324906 | core_pubmed_pmc | Dynamic PET reveals compartmentalized brain and lung tissue antibiotic exposures of tuberculosis drugs | Dynamic PET reveals compartmentalized brain and lung tissue antibiotic exposures of tuberculosis drugs Abstract Abstract Tuberculosis (TB) remains a leading cause of death, but antibiotic treatments for tuberculous meningitis, the deadliest form of TB, are based on those developed for pulmonary TB and not optimized for... |
PMC5516185 | core_pubmed_pmc | Assessment of the Pharmacokinetics, Pharmacodynamics, and Safety of Single Doses of TV‐1106, a Long‐Acting Growth Hormone, in Healthy Japanese and Caucasian Subjects | Assessment of the Pharmacokinetics, Pharmacodynamics, and Safety of Single Doses of TV‐1106, a Long‐Acting Growth Hormone, in Healthy Japanese and Caucasian Subjects Abstract Abstract TV‐1106 is a human serum albumin genetically fused to recombinant human growth hormone, designed to provide a long‐acting alternative to... |
PMC3160557 | core_pubmed_pmc | Predictive ability of a semi-mechanistic model for neutropenia in the development of novel anti-cancer agents: two case studies | Predictive ability of a semi-mechanistic model for neutropenia in the development of novel anti-cancer agents: two case studies Abstract Summary In cancer chemotherapy neutropenia is a common dose-limiting toxicity. An ability to predict the neutropenic effects of cytotoxic agents based on proposed trial designs and mo... |
PMC6437521 | core_pubmed_pmc | Pooled Population Pharmacokinetic Analysis of Tribendimidine for the Treatment of Opisthorchis viverrini Infections | Pooled Population Pharmacokinetic Analysis of Tribendimidine for the Treatment of Opisthorchis viverrini Infections Abstract Opisthorchiasis, caused by the foodborne trematode Opisthorchis viverrini , affects more than 8 million people in Southeast Asia. In the framework of a phase 2b clinical trial conducted in Lao Pe... |
PMC4559581 | core_pubmed_pmc | Pharmacokinetics, Safety, and Cardiovascular Tolerability of Phenylephrine HCl 10, 20, and 30 mg After a Single Oral Administration in Healthy Volunteers | Pharmacokinetics, Safety, and Cardiovascular Tolerability of Phenylephrine HCl 10, 20, and 30 mg After a Single Oral Administration in Healthy Volunteers Abstract Abstract Background and Objectives Phenylephrine HCl 10 mg has been used as a nasal decongestant for over 50 years, yet only limited pharmacokinetic and meta... |
PMC10748010 | core_pubmed_pmc | Utility of Physiologically Based Pharmacokinetic Modeling to Investigate the Impact of Physiological Changes of Pregnancy and Cancer on Oncology Drug Pharmacokinetics | Utility of Physiologically Based Pharmacokinetic Modeling to Investigate the Impact of Physiological Changes of Pregnancy and Cancer on Oncology Drug Pharmacokinetics Abstract Abstract Background: The treatment of cancer during pregnancy remains challenging with knowledge gaps in drug dosage, safety, and efficacy due t... |
PMC11749819 | core_pubmed_pmc | First-in-human phase I trial of the bispecific CD47 inhibitor and CD40 agonist Fc-fusion protein, SL-172154 in patients with platinum-resistant ovarian cancer | First-in-human phase I trial of the bispecific CD47 inhibitor and CD40 agonist Fc-fusion protein, SL-172154 in patients with platinum-resistant ovarian cancer Abstract Abstract Background SL-172154 is a hexameric fusion protein adjoining the extracellular domain of SIRPα to the extracellular domain of CD40L via an iner... |
PMC6588111 | core_pubmed_pmc | Rheological Properties, Dissolution Kinetics, and Ocular Pharmacokinetics of Loteprednol Etabonate (Submicron) Ophthalmic Gel 0.38% | Rheological Properties, Dissolution Kinetics, and Ocular Pharmacokinetics of Loteprednol Etabonate (Submicron) Ophthalmic Gel 0.38% Abstract Abstract Purpose: To evaluate rheological properties, in vitro dissolution, and in vivo ocular pharmacokinetics of loteprednol etabonate (LE) (submicron) ophthalmic gel 0.38%. Met... |
PMC4478180 | core_pubmed_pmc | Injectable Coformulations in Diabetology | Injectable Coformulations in Diabetology Abstract Abstract Coformulations are a novel pharmaceutical development in diabetology. They are composed of two medicinal products, both of which maintain their distinct pharmacokinetic and pharmacodynamic properties. Currently available coformulations include combinations of b... |
PMC12855527 | core_pubmed_pmc | Near, far, wherever you are: phenotype-related variation in pharmacogenomic effect sizes across the psychiatric drug literature | Near, far, wherever you are: phenotype-related variation in pharmacogenomic effect sizes across the psychiatric drug literature Abstract Abstract Background Pharmacogenomics is viewed as one route to understanding inter-individual variability in drug response. However, clinical uptake in psychiatry is slower than in ot... |
PMC12114988 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Filapixant, a Highly Selective P2X3 Receptor Antagonist, in an Ascending-Single-Dose First-in-Human Study | Safety, Tolerability, and Pharmacokinetics of Filapixant, a Highly Selective P2X3 Receptor Antagonist, in an Ascending-Single-Dose First-in-Human Study Abstract Background/Objectives: P2X3 receptor antagonists have been suggested as a potential treatment for urogenital, respiratory and pain conditions. This first-in-hu... |
PMC5848258 | core_pubmed_pmc | Antiviral Activity, Safety, and Exposure–Response Relationships of GSK3532795, a Second-Generation Human Immunodeficiency Virus Type 1 Maturation Inhibitor, Administered as Monotherapy or in Combination With Atazanavir With or Without Ritonavir in a Phase 2a Randomized, Dose-Ranging, Controlled Trial ( AI468002 ) | Antiviral Activity, Safety, and Exposure–Response Relationships of GSK3532795, a Second-Generation Human Immunodeficiency Virus Type 1 Maturation Inhibitor, Administered as Monotherapy or in Combination With Atazanavir With or Without Ritonavir in a Phase 2a Randomized, Dose-Ranging, Controlled Trial ( AI468002 ) Abstr... |
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