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PMC5216559 | core_pubmed_pmc | Deflazacort: therapeutic index, relative potency and equivalent doses versus other corticosteroids | Deflazacort: therapeutic index, relative potency and equivalent doses versus other corticosteroids Abstract Background Deflazacort is a synthetic corticosteroid characterized by a favourable pharmacokinetic profile, peculiar pharmacodynamic properties and a good safety profile. However, to the best of our knowledge, no... |
PMC4706275 | core_pubmed_pmc | Modeling Testosterone Circadian Rhythm in Hypogonadal Males: Effect of Age and Circannual Variations | Modeling Testosterone Circadian Rhythm in Hypogonadal Males: Effect of Age and Circannual Variations Abstract The objective of this study was to characterize the baseline circadian rhythm of testosterone levels in hypogonadal men. A total of 859 baseline profiles of testosterone from hypogonadal men were included in th... |
PMC9676507 | core_pubmed_pmc | Implications of rituximab pharmacokinetic and pharmacodynamic alterations in various immune-mediated glomerulopathies and potential anti-CD20 therapy alternatives | Implications of rituximab pharmacokinetic and pharmacodynamic alterations in various immune-mediated glomerulopathies and potential anti-CD20 therapy alternatives Abstract The specific B-cell depleting anti-CD20 monoclonal antibody rituximab (RTX) is effective in terms of the treatment of various immune-mediated glomer... |
PMC8397660 | core_pubmed_pmc | Quantitative Systems Pharmacology Modeling of Avadomide-Induced Neutropenia Enables Virtual Clinical Dose and Schedule Finding Studies | Quantitative Systems Pharmacology Modeling of Avadomide-Induced Neutropenia Enables Virtual Clinical Dose and Schedule Finding Studies Abstract Abstract Avadomide is a cereblon E3 ligase modulator and a potent antitumor and immunomodulatory agent. Avadomide trials are challenged by neutropenia as a major adverse event ... |
PMC9463365 | core_pubmed_pmc | Mechanisms of antibiotic action shape the fitness landscapes of resistance mutations | Mechanisms of antibiotic action shape the fitness landscapes of resistance mutations Abstract Highlights • A multiscale model links bacterial growth with molecular mechanisms of antibiotics. • The model estimates molecular parameters from population-scale experimental data. • Antibiotic mechanism influences the fitness... |
PMC12196480 | core_pubmed_pmc | Quasipaa spinosa-Derived Parvalbumin Attenuates Exercise-Induced Fatigue via Calcium Homeostasis and Oxidative Stress Modulation in Exhaustively Trained Mice | Quasipaa spinosa-Derived Parvalbumin Attenuates Exercise-Induced Fatigue via Calcium Homeostasis and Oxidative Stress Modulation in Exhaustively Trained Mice Abstract Background: Quasipaa spinosa crude extract (QSce), a natural source rich in proteins such as parvalbumin (PV), has been traditionally used to promote phy... |
PMC12374431 | core_pubmed_pmc | Multilevel Analysis Reveals the Critical Role of Cell Death-Related Molecules and Drugs in Temporomandibular Disorders | Multilevel Analysis Reveals the Critical Role of Cell Death-Related Molecules and Drugs in Temporomandibular Disorders Abstract Abstract Background Temporomandibular disorder (TMD) is the most common maxillofacial musculoskeletal disease involving various conditions such as chewing muscle disorders, disc displacement a... |
PMC5940791 | core_pubmed_pmc | Synergistic combination of two antimicrobial agents closing each other’s mutant selection windows to prevent antimicrobial resistance | Synergistic combination of two antimicrobial agents closing each other’s mutant selection windows to prevent antimicrobial resistance Abstract Abstract Antimicrobial resistance seriously threatened human health. Combination therapy is generally an effective strategy to fight resistance, while some data on its effects a... |
PMC7317899 | core_pubmed_pmc | Impact of dose‐escalation schemes and drug discontinuation on weight loss outcomes with liraglutide 3.0 mg: A model‐based approach | Impact of dose‐escalation schemes and drug discontinuation on weight loss outcomes with liraglutide 3.0 mg: A model‐based approach Abstract Abstract Aims To investigate the impact on weight loss of the treatment changes in overweight or obese people that may be needed in case of gastrointestinal (GI) tolerability issue... |
PMC10053761 | core_pubmed_pmc | Identification of Transporter Polymorphisms Influencing Metformin Pharmacokinetics in Healthy Volunteers | Identification of Transporter Polymorphisms Influencing Metformin Pharmacokinetics in Healthy Volunteers Abstract Abstract For patients with type 2 diabetes, metformin is the most often recommended drug. However, there are substantial individual differences in the pharmacological response to metformin. To investigate t... |
PMC6521822 | core_pubmed_pmc | Identification and Assessment of Potential Drug-Drug Interactions in Intensive Care Unit Patients | Identification and Assessment of Potential Drug-Drug Interactions in Intensive Care Unit Patients Abstract ABSTRACT Context Intensive care unit (ICU) patients suffer from various comorbidities and usually receive complex pharmacotherapy which increases the risk of drug-drug interactions (DDIs). Aim To identify and asse... |
PMC6010493 | core_pubmed_pmc | Exposure–response analysis of alectinib in crizotinib-resistant ALK-positive non-small cell lung cancer | Exposure–response analysis of alectinib in crizotinib-resistant ALK-positive non-small cell lung cancer Abstract Purpose Alectinib is a selective and potent anaplastic lymphoma kinase (ALK) inhibitor that is active in the central nervous system (CNS). Alectinib demonstrated robust efficacy in a pooled analysis of two s... |
PMC6000956 | core_pubmed_pmc | Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors | Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors Abstract Background Pixatimod (PG545) is a novel clinical-stage immunomodulatory agent capable of inhibiting the infiltration of tumor-associated macrophages (TAMs) yet also st... |
PMC5486072 | core_pubmed_pmc | Emerging Role of the Spleen in the Pharmacokinetics of Monoclonal Antibodies, Nanoparticles and Exosomes | Emerging Role of the Spleen in the Pharmacokinetics of Monoclonal Antibodies, Nanoparticles and Exosomes Abstract After being absorbed, drugs distribute in the body in part to reach target tissues, in part to be disposed in tissues where they do not exert clinically-relevant effects. Therapeutically-relevant effects ar... |
PMC10117697 | core_pubmed_pmc | A Phase 1 Study of Oral Vitamin D 3 in Boys and Young Men With X-Linked Adrenoleukodystrophy | A Phase 1 Study of Oral Vitamin D 3 in Boys and Young Men With X-Linked Adrenoleukodystrophy Abstract Background and Objectives There are no therapies for preventing cerebral demyelination in X-linked adrenoleukodystrophy (ALD). Higher plasma vitamin D levels have been linked to lower risk of inflammatory brain lesions... |
PMC12490974 | core_pubmed_pmc | Lipid-Coated Mesoporous Silica Particles for pH-Sensitive Tumor-Targeted Paclitaxel: Development, Characterization | Lipid-Coated Mesoporous Silica Particles for pH-Sensitive Tumor-Targeted Paclitaxel: Development, Characterization Abstract Nanoparticle carriers can selectively deliver the drug cargo to tumor cells, thus having the ability to prevent early drug release, reduce non-specific cell binding, and prolong in vivo drug reten... |
PMC7493140 | core_pubmed_pmc | An open label study of the safety and efficacy of a single dose of weekly chloroquine and azithromycin administered for malaria prophylaxis in healthy adults challenged with 7G8 chloroquine-resistant Plasmodium falciparum in a controlled human malaria infection model | An open label study of the safety and efficacy of a single dose of weekly chloroquine and azithromycin administered for malaria prophylaxis in healthy adults challenged with 7G8 chloroquine-resistant Plasmodium falciparum in a controlled human malaria infection model Abstract Abstract Background Malaria remains the top... |
PMC10036418 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Model of Brain Delivery of Plasma Protein Bound Drugs | Physiologically Based Pharmacokinetic Model of Brain Delivery of Plasma Protein Bound Drugs Abstract Abstract Introduction A physiologically based pharmacokinetic (PBPK) model is developed that focuses on the kinetic parameters of drug association and dissociation with albumin, alpha-1 acid glycoprotein (AGP), and brai... |
PMC12078333 | core_pubmed_pmc | Pharmacokinetic evaluation and bioavailability of KPT-335 (Verdinexor) in cats | Pharmacokinetic evaluation and bioavailability of KPT-335 (Verdinexor) in cats Abstract Abstract KPT-335 (Verdinexor) is a novel, orally bioavailable selective inhibitor of nuclear export that has gained significant attention in pharmaceutical research due to its potential anti-tumor and antiviral effects. This study a... |
PMC11406679 | core_pubmed_pmc | Analysis of Biogenic Amines and Small Molecule Metabolites in Human Diabetic Wound Ulcer Exudate | Analysis of Biogenic Amines and Small Molecule Metabolites in Human Diabetic Wound Ulcer Exudate Abstract Diabetic foot ulcers (DFUs) pose a significant challenge in wound care due to their chronic nature and impaired healing processes. This study examines the biogenic amines and small molecule metabolites present in D... |
PMC11273281 | core_pubmed_pmc | B-Cell Maturation Antigen/CD19 Dual-Targeting Immunotherapy in Newly Diagnosed Multiple Myeloma | B-Cell Maturation Antigen/CD19 Dual-Targeting Immunotherapy in Newly Diagnosed Multiple Myeloma Abstract Key Points Question What are the safety, pharmacokinetic, and survival outcomes of B-cell maturation antigen (BCMA)/CD19 dual-targeting chimeric antigen receptor (CAR) T-cell therapy in individuals with high-risk ne... |
PMC11882431 | core_pubmed_pmc | Effect of hypoalbuminemia on drug pharmacokinetics | Effect of hypoalbuminemia on drug pharmacokinetics Abstract Abstract Hypoalbuminemia, defined as serum albumin levels below 35 g/L, is common in patients with conditions such as nephrotic syndrome, cirrhosis, or sepsis. This review examines the impact of hypoalbuminemia on the pharmacokinetics of selected drugs—such as... |
PMC7531524 | core_pubmed_pmc | A minimal physiologically based pharmacokinetic model to characterize colon TNF suppression and treatment effects of an anti-TNF monoclonal antibody in a mouse inflammatory bowel disease model | A minimal physiologically based pharmacokinetic model to characterize colon TNF suppression and treatment effects of an anti-TNF monoclonal antibody in a mouse inflammatory bowel disease model Abstract ABSTRACT Biotherapeutic drugs against tumor necrosis factor (TNF) are effective treatments for moderate to severe infl... |
PMC12769651 | core_pubmed_pmc | Meta-analysis of levamisole absorption and disposition across diverse species using a minimal physiologically-based pharmacokinetic model | Meta-analysis of levamisole absorption and disposition across diverse species using a minimal physiologically-based pharmacokinetic model Abstract Abstract Purpose Pharmacokinetic (PK) data for levamisole, an important immunostimulant and antiparasitic agent, were identified in 18 species providing sufficient PK data f... |
PMC5316407 | core_pubmed_pmc | In vivo imaging of systemic transport and elimination of xenobiotics and endogenous molecules in mice | In vivo imaging of systemic transport and elimination of xenobiotics and endogenous molecules in mice Abstract Abstract We describe a two-photon microscopy-based method to evaluate the in vivo systemic transport of compounds. This method comprises imaging of the intact liver, kidney and intestine, the main organs respo... |
PMC12927693 | core_pubmed_pmc | Lack of Modulation of In Vivo Activity of Organic Anion Transporters 1 and 3 in Pregnancy Using Furosemide as a Probe | Lack of Modulation of In Vivo Activity of Organic Anion Transporters 1 and 3 in Pregnancy Using Furosemide as a Probe Abstract Abstract Pregnancy induces physiological changes that can alter drug disposition, yet little is known about their impact on renal transporters such as organic anion transporters 1 and 3 (OAT1/3... |
PMC12913803 | core_pubmed_pmc | Adjunct EF-M2 therapy improves clinical activity, steroid-sparing, and macrophage-linked biomarkers in feline chronic enteropathy: A randomized, double-blind, and placebo-controlled trial | Adjunct EF-M2 therapy improves clinical activity, steroid-sparing, and macrophage-linked biomarkers in feline chronic enteropathy: A randomized, double-blind, and placebo-controlled trial Abstract ABSTRACT Background and Aim: Feline chronic enteropathy (CE), often manifesting along the triaditis-axis with concurrent pa... |
PMC4847232 | core_pubmed_pmc | Pharmacokinetic properties of intramuscular versus oral syrup paracetamol in Plasmodium falciparum malaria | Pharmacokinetic properties of intramuscular versus oral syrup paracetamol in Plasmodium falciparum malaria Abstract Abstract Background Fever is an inherent symptom of malaria in both adults and children. Paracetamol (acetaminophen) is the recommended antipyretic as it is inexpensive, widely available and has a good sa... |
PMC10561745 | core_pubmed_pmc | OSWG Recommended Approaches to the Nonclinical Pharmacokinetic (ADME) Characterization of Therapeutic Oligonucleotides | OSWG Recommended Approaches to the Nonclinical Pharmacokinetic (ADME) Characterization of Therapeutic Oligonucleotides Abstract Abstract This white paper summarizes the recommendations of the absorption, distribution, metabolism, and excretion (ADME) Subcommittee of the Oligonucleotide Safety Working Group for the char... |
PMC7590462 | core_pubmed_pmc | The effect of the glucosylceramide synthase inhibitor lucerastat on cardiac repolarization: results from a thorough QT study in healthy subjects | The effect of the glucosylceramide synthase inhibitor lucerastat on cardiac repolarization: results from a thorough QT study in healthy subjects Abstract Background Fabry disease is a rare inherited glycosphingolipid storage disorder caused by deleterious mutations in the GLA gene coding for the lysosomal enzyme α-gala... |
PMC11540123 | core_pubmed_pmc | Benchmark Dose for Dioxin Based on Gestational Diabetes Mellitus Using Coexposure Statistical Methods and an Optimized Physiologically Based Toxicokinetic Model | Benchmark Dose for Dioxin Based on Gestational Diabetes Mellitus Using Coexposure Statistical Methods and an Optimized Physiologically Based Toxicokinetic Model Abstract Dioxins are ubiquitous endocrine-disrupting substances, but determining the effects and benchmark doses in situations of coexposure is highly challeng... |
PMC11704051 | core_pubmed_pmc | MAT2A inhibitor AG-270/S095033 in patients with advanced malignancies: a phase I trial | MAT2A inhibitor AG-270/S095033 in patients with advanced malignancies: a phase I trial Abstract Abstract Homozygous MTAP deletion occurs in ~15% of cancers, making them vulnerable to decreases in the concentration of S-adenosylmethionine (SAM). AG-270/S095033 is an oral, potent, reversible inhibitor of methionine adeno... |
PMC11596549 | core_pubmed_pmc | Bupropion Increased More than Five Times the Systemic Exposure to Aripiprazole: An In Vivo Study in Wistar albino Rats | Bupropion Increased More than Five Times the Systemic Exposure to Aripiprazole: An In Vivo Study in Wistar albino Rats Abstract Abstract Background/Objectives : In psychiatric disorders, antipsychotics and antidepressant medication are often administered together. Aripiprazole, a third-generation antipsychotic drug, is... |
PMC6802206 | core_pubmed_pmc | Evaluation of Small Molecule Drug Uptake in Patient-Derived Prostate Cancer Explants by Mass Spectrometry | Evaluation of Small Molecule Drug Uptake in Patient-Derived Prostate Cancer Explants by Mass Spectrometry Abstract Patient-derived explant (PDE) culture of solid tumors is increasingly being applied to preclinical evaluation of novel therapeutics and for biomarker discovery. In this technique, treatments are added to c... |
PMC9787453 | core_pubmed_pmc | Mannosylated Systems for Targeted Delivery of Antibacterial Drugs to Activated Macrophages | Mannosylated Systems for Targeted Delivery of Antibacterial Drugs to Activated Macrophages Abstract Abstract Macrophages are a promising target for drug delivery to influence macrophage-associated processes in the body, namely due to the presence of resistant microorganisms in macrophages. In this work, a series of man... |
PMC11784162 | core_pubmed_pmc | First-in-human, multicenter, open-label, phase I study of ATOR-1017 (evunzekibart), a 4-1BB antibody, in patients with advanced solid malignancies | First-in-human, multicenter, open-label, phase I study of ATOR-1017 (evunzekibart), a 4-1BB antibody, in patients with advanced solid malignancies Abstract Abstract Background ATOR-1017 (evunzekibart) is a human agonistic immunoglobulin G4 antibody targeting the costimulatory receptor 4-1BB (CD137). ATOR-1017 activates... |
PMC9424659 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of daptomycin dose optimization in pediatric patients with renal impairment | Physiologically based pharmacokinetic modeling of daptomycin dose optimization in pediatric patients with renal impairment Abstract Background and Objective: Daptomycin is used to treat Gram-positive infections in adults and children and its dosing varies among different age groups. We focused on the pharmacokinetics o... |
PMC4230815 | core_pubmed_pmc | A framework incorporating the impact of exposure scenarios and application conditions on risk assessment of chemicals applied to skin | A framework incorporating the impact of exposure scenarios and application conditions on risk assessment of chemicals applied to skin Abstract Abstract Purpose 1. To develop a framework for exposure calculation via the dermal route to meet the needs of 21st century toxicity testing and refine current approaches; 2. To ... |
PMC9099209 | core_pubmed_pmc | Tissue Distribution, Excretion, and Interaction With Human Serum Albumin of Total Bioflavonoid Extract From Selaginella doederleinii | Tissue Distribution, Excretion, and Interaction With Human Serum Albumin of Total Bioflavonoid Extract From Selaginella doederleinii Abstract Selaginella doederleinii Hieron is a traditional Chinese medicinal herb widely used to treat different cancers. Previously, we showed that the total bioflavonoid extract of S. do... |
PMC4207554 | core_pubmed_pmc | Anticancer efficacy and absorption, distribution, metabolism, and toxicity studies of Aspergiolide A in early drug development | Anticancer efficacy and absorption, distribution, metabolism, and toxicity studies of Aspergiolide A in early drug development Abstract Abstract Since the first anthracycline was discovered, many other related compounds have been studied in order to overcome its defects and improve efficacy. In the present paper, we in... |
PMC11682177 | core_pubmed_pmc | Vancomycin administration and AUC/MIC in patients with acute kidney injury on hemodialysis (HD): randomized clinical trial | Vancomycin administration and AUC/MIC in patients with acute kidney injury on hemodialysis (HD): randomized clinical trial Abstract The pharmacokinetics and pharmacodynamics (PK/PD) of vancomycin change during HD, increasing the risk of subtherapeutic concentrations. The aim of this study was to evaluate during and aft... |
PMC7358525 | core_pubmed_pmc | Characterization of PF-6142, a Novel, Non-Catecholamine Dopamine Receptor D1 Agonist, in Murine and Nonhuman Primate Models of Dopaminergic Activation | Characterization of PF-6142, a Novel, Non-Catecholamine Dopamine Receptor D1 Agonist, in Murine and Nonhuman Primate Models of Dopaminergic Activation Abstract Selective activation of dopamine D1 receptors remains a promising pro-cognitive therapeutic strategy awaiting robust clinical investigation. PF-6142 is a key ex... |
PMC6152676 | core_pubmed_pmc | Pharmacokinetics and Tissue Distribution Kinetics of Puerarin in Rats Using Indirect Competitive ELISA | Pharmacokinetics and Tissue Distribution Kinetics of Puerarin in Rats Using Indirect Competitive ELISA Abstract Abstract Puerarin (PUE) is a compound isolated from the roots of Pueraria lobata . We studied the pharmacokinetics and tissue distribution kinetics of PUE in Sprague-Dawley rats following intraperitoneal admi... |
PMC4282122 | core_pubmed_pmc | Evaluation of a Novel Nicotine Inhaler Device: Part 1—Arterial and Venous Pharmacokinetics | Evaluation of a Novel Nicotine Inhaler Device: Part 1—Arterial and Venous Pharmacokinetics Abstract Introduction: In the United Kingdom, licensed nicotine-containing products can be recommended to reduce the harm associated with smoking. Many smokers find currently available nicotine replacement products unsatisfactory... |
PMC7673685 | core_pubmed_pmc | The scientific basis of rational prescribing. A guide to precision clinical pharmacology based on the WHO 6-step method | The scientific basis of rational prescribing. A guide to precision clinical pharmacology based on the WHO 6-step method Abstract Abstract Background and methods This opinion paper expanded on the WHO “six-step approach to optimal pharmacotherapy,” by detailed exploration of the underlying pharmacological and pathophysi... |
PMC10921956 | core_pubmed_pmc | High-throughput glycolytic inhibitor discovery targeting glioblastoma by graphite dots–assisted LDI mass spectrometry | High-throughput glycolytic inhibitor discovery targeting glioblastoma by graphite dots–assisted LDI mass spectrometry Abstract Abstract Malignant tumors will become vulnerable if their uncontrolled biosynthesis and energy consumption engaged in metabolic reprogramming can be cut off. Here, we report finding a glycolyti... |
PMC3909979 | core_pubmed_pmc | Formulation and Evaluation of Fixed-Dose Combination of Bilayer Gastroretentive Matrix Tablet Containing Atorvastatin as Fast-Release and Atenolol as Sustained-Release | Formulation and Evaluation of Fixed-Dose Combination of Bilayer Gastroretentive Matrix Tablet Containing Atorvastatin as Fast-Release and Atenolol as Sustained-Release Abstract Abstract The objective of the present study was to develop bilayer tablets of atorvastatin and atenolol that are characterized by initial fast-... |
PMC7825188 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model to Predict Potential Drug–Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor | A Physiologically Based Pharmacokinetic Model to Predict Potential Drug–Drug Interactions and Inform Dosing of Acumapimod, an Oral p38 MAPK Inhibitor Abstract Abstract Acumapimod, an investigational oral p38 mitogen‐activated protein kinase inhibitor for treatment during severe acute exacerbations of chronic obstructiv... |
PMC11246689 | core_pubmed_pmc | Genetic variants of ABCB1 and CES1 genes on dabigatran metabolism in the Kazakh population | Genetic variants of ABCB1 and CES1 genes on dabigatran metabolism in the Kazakh population Abstract Abstract Background: Allelic variants of genes encoding enzymes of the esterase system ( CES1 ) and P-glycoprotein ( ABCB1 ) can change the metabolism and pharmacokinetics of dabigatran. Therefore, they act as determinin... |
PMC8596596 | core_pubmed_pmc | Biperiden Challenge Model in Healthy Elderly as Proof‐of‐Pharmacology Tool: A Randomized, Placebo‐Controlled Trial | Biperiden Challenge Model in Healthy Elderly as Proof‐of‐Pharmacology Tool: A Randomized, Placebo‐Controlled Trial Abstract Abstract Selective M 1 muscarinic acetylcholine receptor (mAChR) agonists are being developed as symptomatic treatment for neurodegenerative and neuropsychiatric disorders that lead to cognitive d... |
PMC11330180 | core_pubmed_pmc | A pharmacokinetic framework describing antibiotic adsorption to cardiopulmonary bypass devices | A pharmacokinetic framework describing antibiotic adsorption to cardiopulmonary bypass devices Abstract Abstract Cardiopulmonary bypass (CPB) can alter pharmacokinetic (PK) parameters and the drug may adsorb to the CPB device, altering exposure. Cefazolin is a beta‐lactam antibiotic used for antimicrobial prophylaxis d... |
PMC11725097 | core_pubmed_pmc | Thio-ProTide strategy: A novel H 2 S donor–drug conjugate (DDC) alleviates hepatic injury via innate lysosomal targeting | Thio-ProTide strategy: A novel H 2 S donor–drug conjugate (DDC) alleviates hepatic injury via innate lysosomal targeting Abstract Abstract Hydrogen sulfide (H 2 S) is a gas signaling molecule with versatile bioactivities; however, its exploitation for disease treatment appears challenging. This study describes the desi... |
PMC8104087 | core_pubmed_pmc | Serum Creatinine and Serum Cystatin C are Both Relevant Renal Markers to Estimate Vancomycin Clearance in Critically Ill Neonates | Serum Creatinine and Serum Cystatin C are Both Relevant Renal Markers to Estimate Vancomycin Clearance in Critically Ill Neonates Abstract Abstract Purpose: Serum creatinine (SCr) is used as a marker of kidney function to guide dosing of renally eliminated drugs. Serum Cystatin C (S-CysC) has been suggested as a more r... |
PMC7862523 | core_pubmed_pmc | Exploration of Reduced Doses and Short-Cycle Therapy for Darunavir/Cobicistat in Patients with HIV Using Population Pharmacokinetic Modeling and Simulations | Exploration of Reduced Doses and Short-Cycle Therapy for Darunavir/Cobicistat in Patients with HIV Using Population Pharmacokinetic Modeling and Simulations Abstract Background and objectives Protease inhibitors such as darunavir are an important therapeutic option in the anti-human immunodeficiency virus arsenal. Curr... |
PMC7873432 | core_pubmed_pmc | Challenges of Psychiatry Drug Development and the Role of Human Pharmacology Models in Early Development—A Drug Developer's Perspective | Challenges of Psychiatry Drug Development and the Role of Human Pharmacology Models in Early Development—A Drug Developer's Perspective Abstract Psychiatric diseases have the lowest probability of success in clinical drug development. This presents not only an issue to address the unmet medical needs of patients, but a... |
PMC8743212 | core_pubmed_pmc | The influence of immune stress induced by Escherichia coli lipopolysaccharide on the pharmacokinetics of danofloxacin in broilers | The influence of immune stress induced by Escherichia coli lipopolysaccharide on the pharmacokinetics of danofloxacin in broilers Abstract This study aimed to determine whether the challenge from Escherichia coli ( E. coli ) lipopolysaccharide ( LPS ) affects the pharmacokinetics of danofloxacin in broilers. Twenty 1-d... |
PMC8462653 | core_pubmed_pmc | The influence of edema on the bisoprolol blood concentration after bisoprolol dermal patch application | The influence of edema on the bisoprolol blood concentration after bisoprolol dermal patch application Abstract Abstract Background: Beta-blocking is important for critically ill patients. Although some patients are required to continue taking beta-blockers after they no longer need critical care, some of these patient... |
PMC7076237 | core_pubmed_pmc | Phase I trial of WEE1 inhibition with chemotherapy and radiotherapy as adjuvant treatment, and a window of opportunity trial with cisplatin in patients with head and neck cancer: the WISTERIA trial protocol | Phase I trial of WEE1 inhibition with chemotherapy and radiotherapy as adjuvant treatment, and a window of opportunity trial with cisplatin in patients with head and neck cancer: the WISTERIA trial protocol Abstract Introduction Patients with head and neck squamous cell carcinoma with locally advanced disease often req... |
PMC5412900 | core_pubmed_pmc | Drug interaction between tacrolimus and nilotinib in a patient with chronic myeloid leukemia after renal transplant | Drug interaction between tacrolimus and nilotinib in a patient with chronic myeloid leukemia after renal transplant Abstract Key Clinical Message Nilotinib, a BCR ‐ ABL tyrosine kinase inhibitor, is a known inhibitor of CYP 3A4 and could increase the concentration of drugs metabolized by CYP 3A4. An immunosuppressive d... |
PMC11869703 | core_pubmed_pmc | Developing a PK-PD model for propofol in exhaled air and the BIS following fospropofol disodium in beagles | Developing a PK-PD model for propofol in exhaled air and the BIS following fospropofol disodium in beagles Abstract Background Fospropofol, a water-soluble prodrug of propofol, is metabolized into propofol by alkaline phosphatase after administration. This study aimed to develop a pharmacokinetic-pharmacodynamic (PK-PD... |
PMC10254625 | core_pubmed_pmc | Phase I trial of KN046, a novel bispecific antibody targeting PD-L1 and CTLA-4 in patients with advanced solid tumors | Phase I trial of KN046, a novel bispecific antibody targeting PD-L1 and CTLA-4 in patients with advanced solid tumors Abstract Abstract Background KN046 is a novel bispecific antibody targeting programmed death ligand 1 (PD-L1) and cytotoxic T lymphocyte-associated protein 4 (CTLA-4). This multicenter phase I trial inv... |
PMC5374376 | core_pubmed_pmc | Polypharmacy in Zoological Medicine | Polypharmacy in Zoological Medicine Abstract Abstract Polypharmacy is a term that describes the inappropriate, concurrent use of multiple drugs in an individual patient. Zoological medicine practitioners must take approved agents (veterinary or human) and extrapolate their use to non-approved species often with little ... |
PMC3070480 | core_pubmed_pmc | A Computational Systems Biology Software Platform for Multiscale Modeling and Simulation: Integrating Whole-Body Physiology, Disease Biology, and Molecular Reaction Networks | A Computational Systems Biology Software Platform for Multiscale Modeling and Simulation: Integrating Whole-Body Physiology, Disease Biology, and Molecular Reaction Networks Abstract Today, in silico studies and trial simulations already complement experimental approaches in pharmaceutical R&D and have become indispens... |
PMC9010254 | core_pubmed_pmc | Translational findings for odronextamab: From preclinical research to a first‐in‐human study in patients with CD20+ B‐cell malignancies | Translational findings for odronextamab: From preclinical research to a first‐in‐human study in patients with CD20+ B‐cell malignancies Abstract Abstract Odronextamab is a fully‐human IgG4‐based CD20xCD3 bispecific antibody that binds to CD3 on T cells and CD20 on B cells, triggering T‐cell‐mediated cytotoxicity indepe... |
PMC4432106 | core_pubmed_pmc | The impact of composite AUC estimates on the prediction of systemic exposure in toxicology experiments | The impact of composite AUC estimates on the prediction of systemic exposure in toxicology experiments Abstract Current toxicity protocols relate measures of systemic exposure (i.e. AUC, C max ) as obtained by non-compartmental analysis to observed toxicity. A complicating factor in this practice is the potential bias ... |
PMC11450095 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Systemic Corticosteroids in Autoimmune and Inflammatory Diseases: A Review of Current Evidence | Pharmacokinetics and Pharmacodynamics of Systemic Corticosteroids in Autoimmune and Inflammatory Diseases: A Review of Current Evidence Abstract Abstract Background and Objective Systemic corticosteroids have a long history of use in the treatment of autoimmune and inflammatory diseases. Both efficacy and safety show l... |
PMC6558040 | core_pubmed_pmc | Factors Affecting Combination Trial Success (FACTS): Investigator Survey Results on Early-Phase Combination Trials | Factors Affecting Combination Trial Success (FACTS): Investigator Survey Results on Early-Phase Combination Trials Abstract Abstract Experimental therapeutic oncology agents are often combined to circumvent tumor resistance to individual agents. However, most combination trials fail to demonstrate sufficient safety and... |
PMC7033327 | core_pubmed_pmc | Putative multiple reaction monitoring strategy for the comparative pharmacokinetics of postoral administration Renshen–Yuanzhi compatibility through liquid chromatography–tandem mass spectrometry | Putative multiple reaction monitoring strategy for the comparative pharmacokinetics of postoral administration Renshen–Yuanzhi compatibility through liquid chromatography–tandem mass spectrometry Abstract Abstract Background Exploring the pharmacokinetic (PK) changes of various active components of single herbs and the... |
PMC11877154 | core_pubmed_pmc | Chronotherapeutic considerations of benzodiazepine administration for agitation management in the emergency department | Chronotherapeutic considerations of benzodiazepine administration for agitation management in the emergency department Abstract Abstract Objective Agitation in the emergency department (ED) affects up to 2.6% of encounters, posing significant risks to patients and caregivers. This review investigates the impact of circ... |
PMC11234030 | core_pubmed_pmc | An insight into the anticancer potentials of lignan arctiin: A comprehensive review of molecular mechanisms | An insight into the anticancer potentials of lignan arctiin: A comprehensive review of molecular mechanisms Abstract Abstract Natural products are being developed as possible treatment options due to the rising prevalence of cancer and the harmful side effects of synthetic medications. Arctiin is a naturally occurring ... |
PMC9662714 | core_pubmed_pmc | Atractylodes lancea for cholangiocarcinoma: Modulatory effects on CYP1A2 and CYP3A1 and pharmacokinetics in rats and biodistribution in mice | Atractylodes lancea for cholangiocarcinoma: Modulatory effects on CYP1A2 and CYP3A1 and pharmacokinetics in rats and biodistribution in mice Abstract Abstract Atractylodes lancea (Thunb.) DC. ( A . lancea : AL) is a promising candidate for the treatment of cholangiocarcinoma (bile duct cancer). The study investigated (... |
PMC10975434 | core_pubmed_pmc | Cannabinoid-Induced Inhibition of Morphine Glucuronidation and the Potential for In Vivo Drug–Drug Interactions | Cannabinoid-Induced Inhibition of Morphine Glucuronidation and the Potential for In Vivo Drug–Drug Interactions Abstract Abstract Opioids are commonly prescribed for the treatment of chronic pain. Approximately 50% of adults who are prescribed opioids for pain co-use cannabis with their opioid treatment. Morphine is pr... |
PMC5388421 | core_pubmed_pmc | Phosphorylation-specific status of RNAi triggers in pharmacokinetic and biodistribution analyses | Phosphorylation-specific status of RNAi triggers in pharmacokinetic and biodistribution analyses Abstract Abstract The RNA interference (RNAi)-based therapeutic ARC-520 for chronic hepatitis B virus (HBV) infection consists of a melittin-derived peptide conjugated to N-acetylgalactosamine for hepatocyte targeting and e... |
PMC5560534 | core_pubmed_pmc | Comparing efficacies of moxifloxacin, levofloxacin and gatifloxacin in tuberculosis granulomas using a multi-scale systems pharmacology approach | Comparing efficacies of moxifloxacin, levofloxacin and gatifloxacin in tuberculosis granulomas using a multi-scale systems pharmacology approach Abstract Abstract Granulomas are complex lung lesions that are the hallmark of tuberculosis (TB). Understanding antibiotic dynamics within lung granulomas will be vital to imp... |
PMC9632061 | core_pubmed_pmc | Pharmacokinetics/Pharmacodynamics and tolerability of cefiderocol in the clinical setting | Pharmacokinetics/Pharmacodynamics and tolerability of cefiderocol in the clinical setting Abstract Abstract Cefiderocol is a new cephalosporin with a catechol in its chemical structure faciliting its access to the interior of bacteria through iron channels. In addition, it is broadly stable to beta-lactamases. The phar... |
PMC6204840 | core_pubmed_pmc | Extending human IgG half-life using structure-guided design | Extending human IgG half-life using structure-guided design Abstract ABSTRACT Engineering of antibodies for improved pharmacokinetics through enhanced binding to the neonatal Fc receptor (FcRn) has been demonstrated in transgenic mice, non-human primates and humans. Traditionally, such approaches have largely relied on... |
PMC8520753 | core_pubmed_pmc | Population pharmacokinetic analysis of rivaroxaban in children and comparison to prospective physiologically‐based pharmacokinetic predictions | Population pharmacokinetic analysis of rivaroxaban in children and comparison to prospective physiologically‐based pharmacokinetic predictions Abstract Abstract Rivaroxaban has been investigated in the EINSTEIN‐Jr program for the treatment of acute venous thromboembolism (VTE) in children aged 0 to 18 years and in the ... |
PMC7373711 | core_pubmed_pmc | Optimising the dose of clonidine to achieve sedation in intensive care unit patients with population pharmacokinetics | Optimising the dose of clonidine to achieve sedation in intensive care unit patients with population pharmacokinetics Abstract Abstract Aims The aim of this study was to investigate the population pharmacokinetics (PK) of clonidine in intensive care unit (ICU) patients in order to develop a dosing regimen for sedation.... |
PMC12816420 | core_pubmed_pmc | Enhancing Severe Neutropenia Prediction: PKPD ‐Informed Labeling for Machine Learning Models Trained on Real‐World Data | Enhancing Severe Neutropenia Prediction: PKPD ‐Informed Labeling for Machine Learning Models Trained on Real‐World Data Abstract Accurately labeling outcomes in real‐world data for machine learning is challenging due to data sparsity and imbalances. This study developed and evaluated a pharmacokinetic–pharmacodynamic (... |
PMC4892995 | core_pubmed_pmc | Phase 1 Study of ABT‐751 in Combination With CAPIRI (Capecitabine and Irinotecan) and Bevacizumab in Patients With Advanced Colorectal Cancer | Phase 1 Study of ABT‐751 in Combination With CAPIRI (Capecitabine and Irinotecan) and Bevacizumab in Patients With Advanced Colorectal Cancer Abstract Abstract ABT‐751 is an orally bioavailable sulfonamide with antimitotic properties. A nonrandomized phase 1 dose‐escalation study of ABT‐751 in combination with CAPIRI (... |
PMC11747318 | core_pubmed_pmc | Proximal tubule-on-chip as a model for predicting cation transport and drug transporter dynamics | Proximal tubule-on-chip as a model for predicting cation transport and drug transporter dynamics Abstract Deciphering the sources of variability in drug responses requires to understand the processes modulating drug pharmacokinetics. However, pharmacological research suffers from poor reproducibility across clinical, a... |
PMC5520933 | core_pubmed_pmc | LISPRO mitigates β -amyloid and associated pathologies in Alzheimer’s mice | LISPRO mitigates β -amyloid and associated pathologies in Alzheimer’s mice Abstract Lithium has been marketed in the United States of America since the 1970s as a treatment for bipolar disorder. More recently, studies have shown that lithium can improve cognitive decline associated with Alzheimer’s disease (AD). Howeve... |
PMC12737236 | core_pubmed_pmc | Selection of Solubility Enhancement Technologies for S-892216, a Novel COVID-19 Drug Candidate | Selection of Solubility Enhancement Technologies for S-892216, a Novel COVID-19 Drug Candidate Abstract Background/Objectives : S-892216 is a poorly water-soluble drug developed as a novel oral treatment for COVID-19, although its oral absorption is low. For Phase 1 (Ph1) studies and commercial use, both oral solution ... |
PMC12888850 | core_pubmed_pmc | Monthly dalbavancin dosing for suppressive therapy: a pharmacokinetic estimation analysis and case series | Monthly dalbavancin dosing for suppressive therapy: a pharmacokinetic estimation analysis and case series Abstract ABSTRACT Retained hardware/prosthetic infections frequently require antimicrobial suppression therapy. Treatment options are often limited by resistance, allergies, and dosing frequencies. Dalbavancin (DAL... |
PMC9259115 | core_pubmed_pmc | β-Lactam Therapeutic Drug Monitoring in Critically Ill Patients: Weighing the Challenges and Opportunities to Assess Clinical Value | β-Lactam Therapeutic Drug Monitoring in Critically Ill Patients: Weighing the Challenges and Opportunities to Assess Clinical Value Abstract Abstract OBJECTIVE: β-lactams are the cornerstone of empiric and targeted antibiotic therapy for critically ill patients. Recently, there have been calls to use β-lactam therapeut... |
PMC5132138 | core_pubmed_pmc | The Pharmacokinetics and Pharmacodynamics of Prasugrel and Clopidogrel in Healthy Japanese Volunteers | The Pharmacokinetics and Pharmacodynamics of Prasugrel and Clopidogrel in Healthy Japanese Volunteers Abstract Abstract The dosing regimen of prasugrel adjusted for Japanese patients was compared with that of clopidogrel by analyzing the pharmacokinetics and pharmacodynamics in 40 healthy Japanese subjects in a randomi... |
PMC12788065 | core_pubmed_pmc | Dose-Sparing Efficacy of d-Limonene with Low-Dose Allopurinol in a Dual Model of Hyperuricemia and Gouty Arthritis in Rats | Dose-Sparing Efficacy of d-Limonene with Low-Dose Allopurinol in a Dual Model of Hyperuricemia and Gouty Arthritis in Rats Abstract Abstract Background: d -Limonene (LIM) is a food-derived monoterpenoid phytocompound predominantly found in citrus peels, endowed with potent antioxidant and anti-inflammatory properties, ... |
PMC9704642 | core_pubmed_pmc | Potential SARS-CoV-2 RdRp inhibitors of cytidine derivatives: Molecular docking, molecular dynamic simulations, ADMET, and POM analyses for the identification of pharmacophore sites | Potential SARS-CoV-2 RdRp inhibitors of cytidine derivatives: Molecular docking, molecular dynamic simulations, ADMET, and POM analyses for the identification of pharmacophore sites Abstract The RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 is one of the optimum targets for antiviral drug design and development. Th... |
PMC7734772 | core_pubmed_pmc | Pharmacokinetic study of a novel oral formulation of S-adenosylmethionine (MSI-195) in healthy subjects: dose escalation, food effect and comparison to a commercial nutritional supplement product | Pharmacokinetic study of a novel oral formulation of S-adenosylmethionine (MSI-195) in healthy subjects: dose escalation, food effect and comparison to a commercial nutritional supplement product Abstract Background A novel, high bioavailability oral, enteric coated tablet formulation of S-adenosylmethionine (MSI-195) ... |
PMC9788450 | core_pubmed_pmc | Management of Anti-Seizure Medications during Pregnancy: Advancements in The Past Decade | Management of Anti-Seizure Medications during Pregnancy: Advancements in The Past Decade Abstract Management of seizures often involves continuous medication use throughout a patient’s life, including when a patient is pregnant. The physiological changes during pregnancy can lead to altered drug exposure to anti-seizur... |
PMC6198747 | core_pubmed_pmc | Enantiospecific pharmacokinetics and drug–drug interactions of primaquine and blood-stage antimalarial drugs | Enantiospecific pharmacokinetics and drug–drug interactions of primaquine and blood-stage antimalarial drugs Abstract Abstract Objectives Characterization of the pharmacokinetic properties of the enantiomers of primaquine and carboxyprimaquine following administration of racemic primaquine given alone and in combinatio... |
PMC8246029 | core_pubmed_pmc | Antisense Inhibition of Angiotensinogen With IONIS-AGT-L Rx | Antisense Inhibition of Angiotensinogen With IONIS-AGT-L Rx Abstract Highlights • Targeting AGT is a novel approach to inhibit the RAAS pathway. • AGT is primarily synthesized in the liver. • IONIS-AGT-L Rx is an ASO directed to hepatocyte-derived AGT. • In 2 phase 2 trials as monotherapy and as an add-on to 2 to 3 med... |
PMC6704358 | core_pubmed_pmc | A PK/PD Analysis of Circulating Biomarkers and Their Relationship to Tumor Response in Atezolizumab‐Treated non‐small Cell Lung Cancer Patients | A PK/PD Analysis of Circulating Biomarkers and Their Relationship to Tumor Response in Atezolizumab‐Treated non‐small Cell Lung Cancer Patients Abstract Abstract To assess circulating biomarkers as predictors of antitumor response to atezolizumab (anti‐programmed death‐ligand 1 (PD‐L1), Tecentriq) serum pharmacokinetic... |
PMC10427527 | core_pubmed_pmc | Model-Informed Support of Dose Selection for Prophylactic Treatment with Dalcinonacog Alfa in Adult and Paediatric Hemophilia B Patients | Model-Informed Support of Dose Selection for Prophylactic Treatment with Dalcinonacog Alfa in Adult and Paediatric Hemophilia B Patients Abstract Abstract Introduction Dalcinonacog alfa (DalcA), a novel subcutaneously administered recombinant human factor IX (FIX) variant is being developed for adult and paediatric pat... |
PMC4464579 | core_pubmed_pmc | Use of in-silico assays to characterize the ADMET profile and identify potential therapeutic targets of fusarochromanone, a novel anti-cancer agent | Use of in-silico assays to characterize the ADMET profile and identify potential therapeutic targets of fusarochromanone, a novel anti-cancer agent Abstract Abstract Purpose For 30 years nature has provided a plethora of natural products with potential meaningful anti-cancer activity. Fusarochromanone (FC101a) is a sma... |
PMC6445413 | core_pubmed_pmc | Tuberculosis drugs’ distribution and emergence of resistance in patient’s lung lesions: A mechanistic model and tool for regimen and dose optimization | Tuberculosis drugs’ distribution and emergence of resistance in patient’s lung lesions: A mechanistic model and tool for regimen and dose optimization Abstract Abstract Background The sites of mycobacterial infection in the lungs of tuberculosis (TB) patients have complex structures and poor vascularization, which obst... |
PMC9137512 | core_pubmed_pmc | Validation and Application of an HPLC-UV Method for Routine Therapeutic Drug Monitoring of Dalbavancin | Validation and Application of an HPLC-UV Method for Routine Therapeutic Drug Monitoring of Dalbavancin Abstract Abstract Dalbavancin is emerging as a promising alternative in the ambulant treatment of gram-positive infections that require long-term antibiotic treatment such as osteomyelitis, prosthetic joint infections... |
PMC12435975 | core_pubmed_pmc | Safety and Pharmacokinetics of MK ‐8527 in Adults Without HIV | Safety and Pharmacokinetics of MK ‐8527 in Adults Without HIV Abstract ABSTRACT MK‐8527 is a nucleoside reverse transcriptase translocation inhibitor (NRTTI) in clinical development. Two Phase 1 trials evaluated single (trial A) and multiple (trial B) ascending doses of MK‐8527 in adults without HIV. In trial A, 34 par... |
PMC10460728 | core_pubmed_pmc | Physiologically-based pharmacokinetic modeling to predict drug-drug interaction of enzalutamide with combined P-gp and CYP3A substrates | Physiologically-based pharmacokinetic modeling to predict drug-drug interaction of enzalutamide with combined P-gp and CYP3A substrates Abstract Enzalutamide is known to strongly induce cytochrome P450 3A4 (CYP3A4). Furthermore, enzalutamide showed induction and inhibition of P-glycoprotein (P-gp) in in vitro studies. ... |
PMC5459446 | core_pubmed_pmc | A phase I study of single-agent perifosine for recurrent or refractory pediatric CNS and solid tumors | A phase I study of single-agent perifosine for recurrent or refractory pediatric CNS and solid tumors Abstract The PI3K/Akt/mTOR signaling pathway is aberrantly activated in various pediatric tumors. We conducted a phase I study of the Akt inhibitor perifosine in patients with recurrent/refractory pediatric CNS and sol... |
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