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PMC12389355 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling to Assess Perpetrator and Victim Cytochrome P450 2C Induction Risk | Physiologically Based Pharmacokinetic Modeling to Assess Perpetrator and Victim Cytochrome P450 2C Induction Risk Abstract Abstract Background: Accurate assessment of CYP2C induction-mediated drug–drug interactions (DDIs) remains a challenge, despite the importance of CYP2C enzymes in drug metabolism. Limitations in av... |
PMC6880552 | core_pubmed_pmc | Comparative evaluation of drug information leaflets for non-steroidal anti-inflammatory drugs in Palestine: local versus imported products | Comparative evaluation of drug information leaflets for non-steroidal anti-inflammatory drugs in Palestine: local versus imported products Abstract Background Drug information leaflets (DILs) are written for patients and health care providers to show how to use the medications safely and effectively, in order to reach ... |
PMC5488121 | core_pubmed_pmc | Elucidating the Aβ42 Anti-Aggregation Mechanism of Action of Tramiprosate in Alzheimer’s Disease: Integrating Molecular Analytical Methods, Pharmacokinetic and Clinical Data | Elucidating the Aβ42 Anti-Aggregation Mechanism of Action of Tramiprosate in Alzheimer’s Disease: Integrating Molecular Analytical Methods, Pharmacokinetic and Clinical Data Abstract Abstract Background Amyloid beta (Aβ) oligomers play a critical role in the pathogenesis of Alzheimer’s disease (AD) and represent a prom... |
PMC12333010 | core_pubmed_pmc | Predicting Δ‑9-Tetrahydrocannabinol-Induced Psychoactive and Cognitive Effects: A PBPK–PD Approach to Quantifying Feeling High and Reduced Alertness | Predicting Δ‑9-Tetrahydrocannabinol-Induced Psychoactive and Cognitive Effects: A PBPK–PD Approach to Quantifying Feeling High and Reduced Alertness Abstract Abstract The increasing use of cannabis for medicinal and recreational purposes highlights the need to understand its psychoactive effects. Δ-9-tetrahydrocannabin... |
PMC8829947 | core_pubmed_pmc | Three-Dimensional Structure and Optimization of the Metallo-β-Lactamase Inhibitor Aspergillomarasmine A | Three-Dimensional Structure and Optimization of the Metallo-β-Lactamase Inhibitor Aspergillomarasmine A Abstract The aminopolycarboxylic acid aspergillomarasmine A (AMA) is a natural Zn 2+ metallophore and inhibitor of metallo-β-lactamases (MBLs) which reverses β-lactam resistance. The first crystal structure of an AMA... |
PMC8875124 | core_pubmed_pmc | Mechanistically Coupled PK (MCPK) Model to Describe Enzyme Induction and Occupancy Dependent DDI of Dabrafenib Metabolism | Mechanistically Coupled PK (MCPK) Model to Describe Enzyme Induction and Occupancy Dependent DDI of Dabrafenib Metabolism Abstract Abstract Dabrafenib inhibits the cell proliferation of metastatic melanoma with the oncogenic BRAF(V600)-mutation. However, dabrafenib monotherapy is associated with pERK reactivation, drug... |
PMC10085907 | core_pubmed_pmc | Evaluation of CYP2C19-Mediated Pharmacokinetic Drug Interaction of Tegoprazan, Compared with Vonoprazan or Esomeprazole | Evaluation of CYP2C19-Mediated Pharmacokinetic Drug Interaction of Tegoprazan, Compared with Vonoprazan or Esomeprazole Abstract Abstract Background and Objective CYP2C19-mediated drug interactions of acid-reducing agents are clinically important given the high possibility of concomitant administration with CYP2C19 sub... |
PMC12314112 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Single‐Dose Dazukibart in Healthy Adults in China and Japan: Results From 2 Randomized, Double‐Blind, Phase 1 Studies | Pharmacokinetics, Safety, and Tolerability of Single‐Dose Dazukibart in Healthy Adults in China and Japan: Results From 2 Randomized, Double‐Blind, Phase 1 Studies Abstract Abstract Dazukibart is a humanized monoclonal antibody selectively targeting interferon‐β. The pharmacokinetics (PK), safety, tolerability, and imm... |
PMC5318554 | core_pubmed_pmc | Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery | Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery Abstract Introduction In spite of advances in understanding and technology, postoperative pain remains poorly treated fo... |
PMC10967119 | core_pubmed_pmc | Accelerated lymph flow from infusion of crystalloid fluid during general anesthesia | Accelerated lymph flow from infusion of crystalloid fluid during general anesthesia Abstract Abstract Background Kinetic analysis of crystalloid fluid yields a central distribution volume ( V c ) of the same size as the expected plasma volume (approximately 3 L) except during general anesthesia during which V c might b... |
PMC7578131 | core_pubmed_pmc | Incorporating Pharmacometrics into Pharmacoeconomic Models: Applications from Drug Development | Incorporating Pharmacometrics into Pharmacoeconomic Models: Applications from Drug Development Abstract Abstract Pharmacometrics is the science of quantifying the relationship between the pharmacokinetics and pharmacodynamics of drugs in combination with disease models and trial information to aid in drug development a... |
PMC4820900 | core_pubmed_pmc | Population pharmacokinetic analysis and dosing regimen optimization of penicillin G in patients with infective endocarditis | Population pharmacokinetic analysis and dosing regimen optimization of penicillin G in patients with infective endocarditis Abstract Abstract Background This study was designed to evaluate the population pharmacokinetics (popPK) of penicillin G in patients with infective endocarditis and establish a dosage regimen base... |
PMC11686335 | core_pubmed_pmc | Phase 3 Study of Talazoparib Plus Enzalutamide Versus Placebo Plus Enzalutamide as First‐Line Treatment in Patients With Metastatic Castration‐Resistant Prostate Cancer: TALAPRO‐2 Japanese Subgroup Analysis | Phase 3 Study of Talazoparib Plus Enzalutamide Versus Placebo Plus Enzalutamide as First‐Line Treatment in Patients With Metastatic Castration‐Resistant Prostate Cancer: TALAPRO‐2 Japanese Subgroup Analysis Abstract ABSTRACT Background In TALAPRO‐2, the poly(ADP‐ribose) polymerase inhibitor talazoparib plus the androge... |
PMC3249745 | core_pubmed_pmc | High Performance Liquid Chromatographic Fluorescence Detection Method for the Quantification of Rivastigmine in Rat Plasma and Brain: Application to Preclinical Pharmacokinetic Studies in Rats | High Performance Liquid Chromatographic Fluorescence Detection Method for the Quantification of Rivastigmine in Rat Plasma and Brain: Application to Preclinical Pharmacokinetic Studies in Rats Abstract Abstract A highly sensitive and selective high performance liquid chromatographic fluorescence detection method has be... |
PMC12729822 | core_pubmed_pmc | Cefiderocol as a Successful Therapy for Osteomyelitis Due to XDR Pseudomonas aeruginosa : A Case Report and Literature Review | Cefiderocol as a Successful Therapy for Osteomyelitis Due to XDR Pseudomonas aeruginosa : A Case Report and Literature Review Abstract Abstract Background : Carbapenem-resistant Enterobacterales and difficult-to-treat resistance (DTR) Pseudomonas aeruginosa are a growing public health issue. Cefiderocol demonstrated ac... |
PMC11622299 | core_pubmed_pmc | Pharmacology Knowledge Among Nurses Working in Nursing Homes in Norway: A Cross-Sectional Study | Pharmacology Knowledge Among Nurses Working in Nursing Homes in Norway: A Cross-Sectional Study Abstract Abstract Introduction The administration of drugs is an important part of nurses’ professional practice. A basic knowledge of pharmacological principles is required to make accurate decisions about drug management a... |
PMC10674765 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Modeling of Midazolam in Pediatric Surgery | Pharmacokinetic–Pharmacodynamic Modeling of Midazolam in Pediatric Surgery Abstract Midazolam (MDZ) is used for sedation in surgical procedures; its clinical effect is related to its receptor affinity and the dose administered. Therefore, a pharmacokinetic–pharmacodynamic (PK-PD) population model of MDZ in pediatric pa... |
PMC10056485 | core_pubmed_pmc | Local Liver Irradiation Concurrently Versus Sequentially with Cabozantinib on the Pharmacokinetics and Biodistribution in Rats | Local Liver Irradiation Concurrently Versus Sequentially with Cabozantinib on the Pharmacokinetics and Biodistribution in Rats Abstract The aim of this study was to evaluate the radiotherapy (RT)-pharmacokinetics (PK) effect of cabozantinib in concurrent or sequential regimens with external beam radiotherapy (EBRT) or ... |
PMC12883205 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic-efficacy modeling of the MDM2 inhibitor brigimadlin in glioblastoma patient-derived xenografts | Pharmacokinetic-pharmacodynamic-efficacy modeling of the MDM2 inhibitor brigimadlin in glioblastoma patient-derived xenografts Abstract Abstract Background Murine double minute 2 (MDM2) inhibitors reactivate wild-type p53 and are a promising therapy for glioblastoma, IDH-wildtype (GBM). Brigimadlin is a highly potent M... |
PMC4309630 | core_pubmed_pmc | Metabolism-related pharmacokinetic drug−drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations | Metabolism-related pharmacokinetic drug−drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations Abstract Abstract Drug−drug interactions (DDIs) occur when a patient's response to the drug is modified by administration or co-exposure to another drug. The main cytochrome P... |
PMC9263896 | core_pubmed_pmc | Advantages of ketamine in pediatric anesthesia | Advantages of ketamine in pediatric anesthesia Abstract Abstract Although ketamine is primarily used for induction and maintenance of general anesthesia, it also presents sedative, amnestic, anesthetics, analgesic, antihyperalgesia, neuroprotective, anti-inflammatory, immunomodulant, and antidepressant effects. Its uni... |
PMC3147094 | core_pubmed_pmc | Comparative bioavailability studies of citric acid and malonic acid based aspirin effervescent tablets | Comparative bioavailability studies of citric acid and malonic acid based aspirin effervescent tablets Abstract Abstract Purpose: The present investigation is aimed at comparing the pharmacokinetic profile (Bioavailability) of aspirin in tablet formulations, which were prepared by using different effervescent excipient... |
PMC4403850 | core_pubmed_pmc | Antifungal wound penetration of amphotericin and voriconazole in combat-related injuries: case report | Antifungal wound penetration of amphotericin and voriconazole in combat-related injuries: case report Abstract Background Survivors of combat trauma can have long and challenging recoveries, which may be complicated by infection. Invasive fungal infections are a rare but serious complication with limited treatment opti... |
PMC11347457 | core_pubmed_pmc | Efficacy and Safety of Salvage-line Nivolumab Monotherapy for Advanced Esophageal Squamous Cell Carcinoma: Comparison of 240 mg Versus 480 mg Doses | Efficacy and Safety of Salvage-line Nivolumab Monotherapy for Advanced Esophageal Squamous Cell Carcinoma: Comparison of 240 mg Versus 480 mg Doses Abstract Abstract Background Nivolumab monotherapy is the standard second-line treatment for advanced esophageal squamous cell carcinoma (ESCC) after failure of platinum-ba... |
PMC3231940 | core_pubmed_pmc | Disposition, metabolism and mass balance of [ 14 C]apremilast following oral administration | Disposition, metabolism and mass balance of [ 14 C]apremilast following oral administration Abstract Abstract Apremilast is a novel, orally available small molecule that specifically inhibits PDE4and thus modulates multiple pro- and anti-inflammatory mediators, and is currently under clinical development for the treatm... |
PMC8445792 | core_pubmed_pmc | A study on catalytic and non-catalytic sites of H5N1 and H1N1 neuraminidase as the target for chalcone inhibitors | A study on catalytic and non-catalytic sites of H5N1 and H1N1 neuraminidase as the target for chalcone inhibitors Abstract The H1N1 pandemic in 2009 and the H5N1 outbreak in 2005 have shocked the world as millions of people were infected and hundreds of thousands died due to the infections by the influenza virus. Oselt... |
PMC6225483 | core_pubmed_pmc | PD-1/PD-L1 pathway and angiogenesis dual recognizable nanoparticles for enhancing chemotherapy of malignant cancer | PD-1/PD-L1 pathway and angiogenesis dual recognizable nanoparticles for enhancing chemotherapy of malignant cancer Abstract Abstract Although the cancer immunotherapy represents one of the most promising strategies for cancer treatment, the PD-1/PD-L1 pathway, which involves a receptor-ligand interaction, can induced i... |
PMC8703774 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model for In Vivo Alpha Particle Generators Targeting Neuroendocrine Tumors in Mice | A Physiologically Based Pharmacokinetic Model for In Vivo Alpha Particle Generators Targeting Neuroendocrine Tumors in Mice Abstract In vivo alpha particle generators have great potential for the treatment of neuroendocrine tumors in alpha-emitter-based peptide receptor radionuclide therapy (α-PRRT). Quantitative pharm... |
PMC9213765 | core_pubmed_pmc | Mortality burden attributable to high and low ambient temperatures in China and its provinces: Results from the Global Burden of Disease Study 2019 | Mortality burden attributable to high and low ambient temperatures in China and its provinces: Results from the Global Burden of Disease Study 2019 Abstract Summary Background Non-optimal temperatures are associated with mortality risk, yet the heterogeneity of temperature-attributable mortality burden across subnation... |
PMC10195017 | core_pubmed_pmc | Translational Studies Using the MALT1 Inhibitor ( S )-Mepazine to Induce Treg Fragility and Potentiate Immune Checkpoint Therapy in Cancer | Translational Studies Using the MALT1 Inhibitor ( S )-Mepazine to Induce Treg Fragility and Potentiate Immune Checkpoint Therapy in Cancer Abstract Introduction Regulatory T cells (Tregs) play a critical role in the maintenance of immune homeostasis but also protect tumors from immune-mediated growth control or rejecti... |
PMC8832229 | core_pubmed_pmc | Evaluation of the Safety, Tolerability, and Pharmacokinetic Profiles of TP0473292 (TS-161), A Prodrug of a Novel Orthosteric mGlu2/3 Receptor Antagonist TP0178894, in Healthy Subjects and Its Antidepressant-Like Effects in Rodents | Evaluation of the Safety, Tolerability, and Pharmacokinetic Profiles of TP0473292 (TS-161), A Prodrug of a Novel Orthosteric mGlu2/3 Receptor Antagonist TP0178894, in Healthy Subjects and Its Antidepressant-Like Effects in Rodents Abstract Abstract Background TP0473292 (the active ingredient of TS-161) is a prodrug of ... |
PMC12736537 | core_pubmed_pmc | Bridging Literature and Real-World Evidence: External Evaluation and Development of Fluoxetine Population Pharmacokinetics Model | Bridging Literature and Real-World Evidence: External Evaluation and Development of Fluoxetine Population Pharmacokinetics Model Abstract Abstract Background: Fluoxetine is widely prescribed to treat depression but exhibits high inter-individual and inter-ethnic pharmacokinetic (PK) variability. Most published populati... |
PMC11768344 | core_pubmed_pmc | An Injectable Oil-Based Depot Formulation of N -Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation | An Injectable Oil-Based Depot Formulation of N -Acyloxymethyl Prodrug of Ropivacaine for Long-Acting Local Analgesia: Formulation Development and In Vitro/In Vivo Evaluation Abstract Objectives: The development of novel long-acting injectables for local anesthetics is necessary to effectively manage the acute postopera... |
PMC11576895 | core_pubmed_pmc | A minimal physiologically based pharmacokinetic model to study the combined effect of antibody size, charge, and binding affinity to FcRn/antigen on antibody pharmacokinetics | A minimal physiologically based pharmacokinetic model to study the combined effect of antibody size, charge, and binding affinity to FcRn/antigen on antibody pharmacokinetics Abstract Abstract Protein therapeutics have revolutionized the treatment of a wide range of diseases. While they have distinct physicochemical ch... |
PMC12641053 | core_pubmed_pmc | Characterization of a Long-Acting Anti-Human MASP-2 Antibody for the Treatment of Complement-Related Diseases | Characterization of a Long-Acting Anti-Human MASP-2 Antibody for the Treatment of Complement-Related Diseases Abstract Purpose The complement system is an important component of the innate immune system, which is essential for orchestrating host defense and regulating inflammation. However, overactivation of the comple... |
PMC4305367 | core_pubmed_pmc | A phase 1 multiple-dose study of orteronel in Japanese patients with castration-resistant prostate cancer | A phase 1 multiple-dose study of orteronel in Japanese patients with castration-resistant prostate cancer Abstract Abstract Purpose Orteronel (TAK-700) is a non-steroidal, selective, reversible inhibitor of 17,20-lyase. We evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor effect of o... |
PMC6449572 | core_pubmed_pmc | Pharmacokinetics and tolerability of lefamulin following intravenous and oral dosing | Pharmacokinetics and tolerability of lefamulin following intravenous and oral dosing Abstract Abstract Objectives To explore the pharmacokinetics (PK) of oral and intravenous (iv) lefamulin after single and multiple doses, and the effect of food on bioavailability. Methods Lefamulin PK was examined in four studies. In ... |
PMC10466002 | core_pubmed_pmc | Full-profile pharmacokinetics, anticancer activity and toxicity of an extended release trivalent PEGylated irinotecan prodrug | Full-profile pharmacokinetics, anticancer activity and toxicity of an extended release trivalent PEGylated irinotecan prodrug Abstract Abstract Irinotecan is an anticancer topoisomerase I inhibitor that acts as a prodrug of the active metabolite, SN-38. Unfortunately, the limited utility of irinotecan is attributed to ... |
PMC11469437 | core_pubmed_pmc | Determination of QLNC-3A6 in canine plasma by UHPLC-MS/MS and its application in pharmacokinetic studies | Determination of QLNC-3A6 in canine plasma by UHPLC-MS/MS and its application in pharmacokinetic studies Abstract Abstract Multi-targeted tyrosine kinase inhibitor QLNC-3A6 Di-maleate, a structurally novel small molecule compound, has therapeutic efficacy for the treatment of canine cutaneous mast cell tumor (CMCT) cau... |
PMC3499303 | core_pubmed_pmc | The assay design used for measurement of therapeutic antibody concentrations can affect pharmacokinetic parameters | The assay design used for measurement of therapeutic antibody concentrations can affect pharmacokinetic parameters Abstract To interpret pharmacokinetic (PK) data of biotherapeutics, it is critical to understand which drug species is being measured by the PK assay. For therapeutic antibodies, it is generally accepted t... |
PMC7761534 | core_pubmed_pmc | BCS Class IV Oral Drugs and Absorption Windows: Regional-Dependent Intestinal Permeability of Furosemide | BCS Class IV Oral Drugs and Absorption Windows: Regional-Dependent Intestinal Permeability of Furosemide Abstract Biopharmaceutical classification system (BCS) class IV drugs (low-solubility low-permeability) are generally poor drug candidates, yet, ~5% of oral drugs on the market belong to this class. While solubility... |
PMC11500360 | core_pubmed_pmc | Improved Dissolution Time and Oral Bioavailability of Pioglitazone Using Liquisolid Tablets: Formulation, In Vitro Characterization, and In Vivo Pharmacokinetics in Rabbits | Improved Dissolution Time and Oral Bioavailability of Pioglitazone Using Liquisolid Tablets: Formulation, In Vitro Characterization, and In Vivo Pharmacokinetics in Rabbits Abstract Abstract In the current study, it was intended to prepare liquisolid tablets of pioglitazone HCl to improve the bioavailability and dissol... |
PMC10068424 | core_pubmed_pmc | Development of an optimized and practical pharmacokinetics/pharmacodynamics analysis method for aztreonam/nacubactam against carbapenemase-producing K. pneumoniae | Development of an optimized and practical pharmacokinetics/pharmacodynamics analysis method for aztreonam/nacubactam against carbapenemase-producing K. pneumoniae Abstract Abstract Background Nacubactam, a new β-lactamase inhibitor with antibacterial activity, is being developed as a single drug to be co-administered w... |
PMC10716325 | core_pubmed_pmc | Pharmacokinetics of cannabidiol-/cannabidiolic acid-rich hemp oil in juvenile cynomolgus macaques ( Macaca fascicularis ) | Pharmacokinetics of cannabidiol-/cannabidiolic acid-rich hemp oil in juvenile cynomolgus macaques ( Macaca fascicularis ) Abstract Abstract Introduction Cannabinoids are increasingly popular in human and veterinary medicine and have been studied as an alternative treatment for a wide range of disorders. The goal of thi... |
PMC7020319 | core_pubmed_pmc | Where Do PBPK Models Stand in Pharmacometrics and Systems Pharmacology? | Where Do PBPK Models Stand in Pharmacometrics and Systems Pharmacology? Modeling Status of PBPK and QSP The origins of PBPK models can be traced back to the work of Teorell in 1937. 1 For many decades, PBPK models have been used by environmental toxicologists. Typically, these models shared some specific characteristic... |
PMC7132603 | core_pubmed_pmc | Gender effect on the pharmacokinetics of thymoquinone: Preclinical investigation and in silico modeling in male and female rats | Gender effect on the pharmacokinetics of thymoquinone: Preclinical investigation and in silico modeling in male and female rats Abstract Abstract Thymoquinone is the most biologically active constituent of Nigella sativa (black seed). A monoterpene compound chemically known as 2-methyl-5-isopropyl-1, 4-quinone. In this... |
PMC7599602 | core_pubmed_pmc | Pharmacokinetics and Protective Effects of Tartary Buckwheat Flour Extracts against Ethanol-Induced Liver Injury in Rats | Pharmacokinetics and Protective Effects of Tartary Buckwheat Flour Extracts against Ethanol-Induced Liver Injury in Rats Abstract Abstract The grains of Tartary buckwheat ( Fagopyrum esculentum ) are traditionally consumed on a daily basis and are used in the preparation of diverse processed foods owing to the high con... |
PMC11983664 | core_pubmed_pmc | Preclinical Pharmacokinetic Assessment of a Promising Vasorelaxant, Analgesic, and Anti‐Inflammatory Prototype 5‐[1‐(4‐Fluorophenyl)‐1H‐pyrazol‐4‐yl]‐2H‐tetrazole (LQFM020) Through Selective Bioanalytical HPLC‐PDA‐Based Method | Preclinical Pharmacokinetic Assessment of a Promising Vasorelaxant, Analgesic, and Anti‐Inflammatory Prototype 5‐[1‐(4‐Fluorophenyl)‐1H‐pyrazol‐4‐yl]‐2H‐tetrazole (LQFM020) Through Selective Bioanalytical HPLC‐PDA‐Based Method Abstract ABSTRACT A simple and selective high‐performance liquid chromatography bioanalytical... |
PMC10870243 | core_pubmed_pmc | Investigation of pharmacokinetic drug interaction between clesacostat and DGAT2 inhibitor ervogastat in healthy adult participants | Investigation of pharmacokinetic drug interaction between clesacostat and DGAT2 inhibitor ervogastat in healthy adult participants Abstract Abstract Co‐administration of clesacostat (acetyl‐CoA carboxylase inhibitor, PF‐05221304) and ervogastat (diacylglycerol O‐acyltransferase inhibitor, PF‐06865571) in laboratory mod... |
PMC6680488 | core_pubmed_pmc | An ImmunoPEGliposome for Targeted Antimalarial Combination Therapy at the Nanoscale | An ImmunoPEGliposome for Targeted Antimalarial Combination Therapy at the Nanoscale Abstract Abstract Combination therapies, where two drugs acting through different mechanisms are administered simultaneously, are one of the most efficient approaches currently used to treat malaria infections. However, the different ph... |
PMC12546829 | core_pubmed_pmc | Pharmacokinetic, docking, and DFT analyses reveal Moringa oleifera phytochemicals as inhibitors of HIF-1α/VEGF/GLUT1 signaling pathway in breast cancer | Pharmacokinetic, docking, and DFT analyses reveal Moringa oleifera phytochemicals as inhibitors of HIF-1α/VEGF/GLUT1 signaling pathway in breast cancer Abstract Abstract Breast cancer is among the most heterogeneous and aggressive malignancies. Hypoxia-driven activation of Hypoxia-inducible factor-1 alpha (HIF-1α) in b... |
PMC4288003 | core_pubmed_pmc | Toward Prospective Prediction of Pharmacokinetics in OATP1B1 Genetic Variant Populations | Toward Prospective Prediction of Pharmacokinetics in OATP1B1 Genetic Variant Populations Abstract Physiologically based pharmacokinetic (PBPK) models are increasingly being used to provide human pharmacokinetic (PK) predictions for organic anion-transporting polypeptide (OATP) substrates based on in vitro assay data. A... |
PMC8145041 | core_pubmed_pmc | Aminoglycosides in the Intensive Care Unit: What Is New in Population PK Modeling? | Aminoglycosides in the Intensive Care Unit: What Is New in Population PK Modeling? Abstract Abstract Background: Although aminoglycosides are often used as treatment for Gram-negative infections, optimal dosing regimens remain unclear, especially in ICU patients. This is due to a large between- and within-subject varia... |
PMC5071756 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo‐Controlled Studies in Healthy Volunteers | Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo‐Controlled Studies in Healthy Volunteers Abstract Abstract We evaluated the pharmacokinetics (PK), safety, and tolerability of a novel oral CRTh2 antagonist, fevipiprant (QA... |
PMC12741916 | core_pubmed_pmc | Genotype–Specific Safety and Pharmacokinetics of Cannabidiol in Healthy Volunteers | Genotype–Specific Safety and Pharmacokinetics of Cannabidiol in Healthy Volunteers Abstract ABSTRACT Cannabidiol (CBD) use has increased in America due to its widespread availability. Cannabidiol is metabolized by multiple polymorphic enzymes including CYP3A, CYP2C9, and CYP2C19. We sought to evaluate the genotype‐spec... |
PMC5937082 | core_pubmed_pmc | Prediction of Lipophilicity and Pharmacokinetics of Chloroacetamides by Chemometric Approach | Prediction of Lipophilicity and Pharmacokinetics of Chloroacetamides by Chemometric Approach Abstract In this study, the existence of biological potential of selected N -(substituted phenyl)-2-chloroacetamides was examined none empirically, as was the possibility of applying simple experimental technique in predicting ... |
PMC12316791 | core_pubmed_pmc | Insulin icodec: A novel once-weekly formulation for the treatment of type 1 and type 2 diabetes mellitus | Insulin icodec: A novel once-weekly formulation for the treatment of type 1 and type 2 diabetes mellitus Abstract Insulin icodec is a novel once-weekly basal insulin analog subcutaneous injection seeking approval by the United States Food and Drug Administration (FDA) for use in both type 1 and type 2 diabetes mellitus... |
PMC6149943 | core_pubmed_pmc | Preparation of honokiol nanoparticles by liquid antisolvent precipitation technique, characterization, pharmacokinetics, and evaluation of inhibitory effect on HepG2 cells | Preparation of honokiol nanoparticles by liquid antisolvent precipitation technique, characterization, pharmacokinetics, and evaluation of inhibitory effect on HepG2 cells Abstract Abstract Background Honokiol is a bioactive lignanoid and has been utilized in traditional Chinese medicine for a long time. It exhibits se... |
PMC7070889 | core_pubmed_pmc | Relationship Between Plasma Concentrations and Clinical Effects of Cariprazine in Patients With Schizophrenia or Bipolar Mania | Relationship Between Plasma Concentrations and Clinical Effects of Cariprazine in Patients With Schizophrenia or Bipolar Mania Abstract Abstract Population pharmacokinetic/pharmacodynamic modeling (via NONMEM) was used to describe longitudinal exposure‐response relationships for total cariprazine (sum of cariprazine an... |
PMC6691755 | core_pubmed_pmc | Pharmacodynamics, safety, and immunogenicity of Pelmeg ® , a pegfilgrastim biosimilar in healthy subjects | Pharmacodynamics, safety, and immunogenicity of Pelmeg ® , a pegfilgrastim biosimilar in healthy subjects Abstract Abstract A pharmacodynamics (PD) and immunogenicity study was conducted to investigate biosimilarity of Pelmeg ® , a pegfilgrastim biosimilar to EU‐authorized Neulasta ® . The multiple‐dose, randomized, do... |
PMC6719321 | core_pubmed_pmc | Effect of Oral Semaglutide on the Pharmacokinetics of Lisinopril, Warfarin, Digoxin, and Metformin in Healthy Subjects | Effect of Oral Semaglutide on the Pharmacokinetics of Lisinopril, Warfarin, Digoxin, and Metformin in Healthy Subjects Abstract Abstract Background Oral semaglutide is a tablet co-formulation of the human glucagon-like peptide-1 (GLP-1) analog semaglutide with the absorption enhancer sodium N -(8-[2-hydroxybenzoyl] ami... |
PMC12011663 | core_pubmed_pmc | Analysis of Sirolimus Blood Concentration and Influencing Factors in Pediatric Patients: Implications for Individualized Drug Therapy | Analysis of Sirolimus Blood Concentration and Influencing Factors in Pediatric Patients: Implications for Individualized Drug Therapy Abstract Background and Objective The purpose of this study is to investigate the status of blood concentration of sirolimus (SRL), explore the factors influencing SRL drug blood concent... |
PMC7497671 | core_pubmed_pmc | Phase 1 study of the MDM2 antagonist RO6839921 in patients with acute myeloid leukemia | Phase 1 study of the MDM2 antagonist RO6839921 in patients with acute myeloid leukemia Abstract In acute myeloid leukemia (AML), TP53 mutations and dysregulation of wild-type p53 is common and supports an MDM2 antagonist as a therapy. RO6839921 is an inactive pegylated prodrug of the oral MDM2 antagonist idasanutlin (a... |
PMC6515238 | core_pubmed_pmc | Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics | Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics Abstract A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a – 5h , have been synthesized, characterized by 1 H-NMR and 13 C-NMR, and evaluated for th... |
PMC7764268 | core_pubmed_pmc | Cardamonin Exerts Antitumor Effect on Human Hepatocellular Carcinoma Xenografts in Athymic Nude Mice through Inhibiting NF-κβ Pathway | Cardamonin Exerts Antitumor Effect on Human Hepatocellular Carcinoma Xenografts in Athymic Nude Mice through Inhibiting NF-κβ Pathway Abstract Abstract Cardamonin (CADMN) exerts an in vitro antiproliferative and apoptotic actions against human hepatocellular carcinoma cells (HepG2). This study aimed to investigate the ... |
PMC10300709 | core_pubmed_pmc | Demonstration of the Early Cardiac Bioavailability of a Non-Specific Cell-Targeted Peptide Using Radionuclide-Based Imaging In Vivo | Demonstration of the Early Cardiac Bioavailability of a Non-Specific Cell-Targeted Peptide Using Radionuclide-Based Imaging In Vivo Abstract The cardiac bioavailability of peptide drugs that inhibit harmful intracellular protein–protein interactions in cardiovascular diseases remains a challenging task in drug developm... |
PMC9396688 | core_pubmed_pmc | Influence of trazodone on the pharmacodynamics and pharmacokinetics of pioglitazone | Influence of trazodone on the pharmacodynamics and pharmacokinetics of pioglitazone Abstract Abstract BACKGROUND: These days, poly pharmacy is very common for the treatment of multiple diseases and majority of drugs were metabolized with CYP 450 enzymes. Diabetes mellitus is such a disorder, which requires continuous t... |
PMC3996108 | core_pubmed_pmc | Pharmacodynamics of cisatracurium in the intensive care unit: an observational study | Pharmacodynamics of cisatracurium in the intensive care unit: an observational study Abstract Background Data from previous studies indicate that optimal conditions for intubation are met 120 seconds after administration of 0.15 mg.kg -1 cisatracurium (ED95 × 3) following the induction of anesthesia. The aim of this st... |
PMC3942296 | core_pubmed_pmc | Preclinical and clinical phase I studies of a new recombinant Filgrastim (BK0023) in comparison with Neupogen ® | Preclinical and clinical phase I studies of a new recombinant Filgrastim (BK0023) in comparison with Neupogen ® Abstract Background Filgrastim or methionyl-granulocyte colony-stimulating factor (Met-G-CSF), is a recombinant therapeutic protein widely used to treat severe neutropenia caused by myelosuppressive drugs in ... |
PMC4404468 | core_pubmed_pmc | Whole-body organ-level and kidney micro-dosimetric evaluations of 64 Cu-loaded HER2/ErbB2-targeted liposomal doxorubicin ( 64 Cu-MM-302) in rodents and primates | Whole-body organ-level and kidney micro-dosimetric evaluations of 64 Cu-loaded HER2/ErbB2-targeted liposomal doxorubicin ( 64 Cu-MM-302) in rodents and primates Abstract Background Features of the tumor microenvironment influence the efficacy of cancer nanotherapeutics. The ability to directly radiolabel nanotherapeuti... |
PMC9309443 | core_pubmed_pmc | A highly D 3 R-selective and efficacious partial agonist ( S )-ABS01-113 compared to its D 3 R-selective antagonist enantiomer ( R )-ABS01-113 as potential treatments for opioid use disorder | A highly D 3 R-selective and efficacious partial agonist ( S )-ABS01-113 compared to its D 3 R-selective antagonist enantiomer ( R )-ABS01-113 as potential treatments for opioid use disorder Abstract The non-medical use of opioids has become a national crisis in the USA. Developing non-opioid pharmacotherapies for cont... |
PMC6831654 | core_pubmed_pmc | Influence of midazolam-related genetic polymorphism on conscious sedation during upper gastrointestinal endoscopy in a Korean population | Influence of midazolam-related genetic polymorphism on conscious sedation during upper gastrointestinal endoscopy in a Korean population Abstract Genetic polymorphism can result in abnormal pharmacodynamics that subsequently leads to the individual variance in sedative effects and adverse reactions. The aim of this stu... |
PMC12937503 | core_pubmed_pmc | Model‐Informed Dosing Regimen of Sugemalimab for European Patients With Non‐Small Cell Lung Cancer: Bridging From Asian Clinical Data | Model‐Informed Dosing Regimen of Sugemalimab for European Patients With Non‐Small Cell Lung Cancer: Bridging From Asian Clinical Data Abstract ABSTRACT Model‐informed drug development (MIDD) framework was employed to bridge sugemalimab dosing from an Asian population to European patients with non‐small cell lung cancer... |
PMC8637357 | core_pubmed_pmc | Safety and tolerability of escalating cannabinoid doses in healthy cats | Safety and tolerability of escalating cannabinoid doses in healthy cats Abstract Abstract Objectives The aim of this study was to determine the safety and tolerability of escalating doses of orally delivered cannabis oils predominant in cannabidiol (CBD), tetrahydrocannabinol (THC), or both CBD and THC in healthy cats.... |
PMC3909452 | core_pubmed_pmc | Population pharmacokinetics of azithromycin and chloroquine in healthy adults and paediatric malaria subjects following oral administration of fixed-dose azithromycin and chloroquine combination tablets | Population pharmacokinetics of azithromycin and chloroquine in healthy adults and paediatric malaria subjects following oral administration of fixed-dose azithromycin and chloroquine combination tablets Abstract Abstract Background Population pharmacokinetics (PK) of azithromycin (AZ) and chloroquine (CQ) following adm... |
PMC6130451 | core_pubmed_pmc | Effects of glycyrrhizin on the pharmacokinetics of asiatic acid in rats and its potential mechanism | Effects of glycyrrhizin on the pharmacokinetics of asiatic acid in rats and its potential mechanism Abstract Abstract Context: Asiatic acid has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the effects of glycyrrhizin on the pharmacokinetics of asiatic acid in r... |
PMC9586895 | core_pubmed_pmc | Esomeprazole and apixaban pharmacokinetic interactions in healthy rats | Esomeprazole and apixaban pharmacokinetic interactions in healthy rats Abstract Abstract Esomeprazole is used in various clinical settings where a decrease in gastric acid production is desired since it is a proton pump inhibitor. Apixaban, an anticoagulant, is used to reduce the risk of stroke in patients with certain... |
PMC4207069 | core_pubmed_pmc | Clinical significance of pharmacogenomic studies in tardive dyskinesia associated with patients with psychiatric disorders | Clinical significance of pharmacogenomic studies in tardive dyskinesia associated with patients with psychiatric disorders Abstract Abstract Pharmacogenomics is the study of the effects of genetic polymorphisms on medication pharmacokinetics and pharmacodynamics. It offers advantages in predicting drug efficacy and/or ... |
PMC11182756 | core_pubmed_pmc | Enhanced Dissolution and Bioavailability of Curcumin Nanocrystals Prepared by Hot Melt Extrusion Technology | Enhanced Dissolution and Bioavailability of Curcumin Nanocrystals Prepared by Hot Melt Extrusion Technology Abstract Purpose Curcumin nanocrystals (Cur-NCs) were prepared by hot melt extrusion (HME) technology to improve the dissolution and bioavailability of curcumin (Cur). Methods Cur-NCs with different drug-carrier ... |
PMC6814091 | core_pubmed_pmc | Oral antibiotics for neonatal infections: a systematic review and meta-analysis | Oral antibiotics for neonatal infections: a systematic review and meta-analysis Abstract Abstract Background Worldwide many neonates suffer from bacterial infections. Adequate treatment is important but is associated with prolonged hospitalization for intravenous administration. In older children, oral switch therapy h... |
PMC8099445 | core_pubmed_pmc | Identification of high‐dimensional omics‐derived predictors for tumor growth dynamics using machine learning and pharmacometric modeling | Identification of high‐dimensional omics‐derived predictors for tumor growth dynamics using machine learning and pharmacometric modeling Abstract Abstract Pharmacometric modeling can capture tumor growth inhibition (TGI) dynamics and variability. These approaches do not usually consider covariates in high‐dimensional s... |
PMC9616540 | core_pubmed_pmc | Population pharmacokinetic/pharmacodynamic study suggests continuous infusion of ceftaroline daily dose in ventilated critical care patients with early-onset pneumonia and augmented renal clearance | Population pharmacokinetic/pharmacodynamic study suggests continuous infusion of ceftaroline daily dose in ventilated critical care patients with early-onset pneumonia and augmented renal clearance Abstract Abstract Objectives Ceftaroline could be suitable to treat early-onset ventilator-associated pneumonia (VAP) beca... |
PMC7907647 | core_pubmed_pmc | Development of a Physiologically Based Pharmacokinetic Model for Hydroxychloroquine and Its Application in Dose Optimization in Specific COVID-19 Patients | Development of a Physiologically Based Pharmacokinetic Model for Hydroxychloroquine and Its Application in Dose Optimization in Specific COVID-19 Patients Abstract Abstract In Feb 2020, we developed a physiologically-based pharmacokinetic (PBPK) model of hydroxychloroquine (HCQ) and integrated in vitro anti-viral effec... |
PMC5011848 | core_pubmed_pmc | The effects of oral and topical corticosteroid in rabbit corneas | The effects of oral and topical corticosteroid in rabbit corneas Abstract Background To determine the most effective route of administration of corticosteroids in the treatment of ocular surface disease, by characterizing the difference between oral prednisolone and topical dexamethasone administration using an animal ... |
PMC11762572 | core_pubmed_pmc | Clinical Pharmacokinetics of Psilocin After Psilocybin Administration: A Systematic Review and Post-Hoc Analysis | Clinical Pharmacokinetics of Psilocin After Psilocybin Administration: A Systematic Review and Post-Hoc Analysis Abstract Background and Objective Psilocybin is currently being extensively studied as a potential therapeutic agent for multiple psychiatric disorders. Here, a systematic literature review of all published ... |
PMC4177650 | core_pubmed_pmc | Prediction of In - silico ADME Properties of 1,2-O-Isopropylidene Aldohexose Derivatives | Prediction of In - silico ADME Properties of 1,2-O-Isopropylidene Aldohexose Derivatives Abstract Retention behaviour of molecules mostly depends on their chemical structure. Retention data of biologically active molecules could be an indirect relationship between their structure and biological or pharmacological activ... |
PMC8037587 | core_pubmed_pmc | Sex-Related Differences in Drugs with Anti-Inflammatory Properties | Sex-Related Differences in Drugs with Anti-Inflammatory Properties Abstract There is increasing evidence of sex differences in the action of anti-inflammatory drugs, with women being at significantly higher risk of adverse effects. Nevertheless, clinicians’ awareness of the implications of these sex differences on dosi... |
PMC10129950 | core_pubmed_pmc | A Bioequivalence Study of Ezetimibe/Rosuvastatin Fixed Dose Combination (10 mg/10 mg) Versus the Individual Formulations Taken Concomitantly | A Bioequivalence Study of Ezetimibe/Rosuvastatin Fixed Dose Combination (10 mg/10 mg) Versus the Individual Formulations Taken Concomitantly Abstract Abstract Introduction This study evaluated the bioequivalence of ezetimibe/rosuvastatin fixed dose combination compared to the concomitant administration of individual fo... |
PMC11820055 | core_pubmed_pmc | Human Pharmacokinetic Profiling and Comparative Analysis of Mangiferin and Its Monosodium Derivative from Mangifera indica Extracts Using UHPLC-MS/MS with 1 H NMR and MALDI-TOF Confirmation | Human Pharmacokinetic Profiling and Comparative Analysis of Mangiferin and Its Monosodium Derivative from Mangifera indica Extracts Using UHPLC-MS/MS with 1 H NMR and MALDI-TOF Confirmation Abstract Mangiferin, a glucosyl xanthone, is a plant metabolite with promising nootropic and ergogenic properties. However, its po... |
PMC8300700 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Analysis of Tedizolid Phosphate Compared to Linezolid for the Treatment of Infections Caused by Gram-Positive Bacteria | Pharmacokinetic/Pharmacodynamic Analysis of Tedizolid Phosphate Compared to Linezolid for the Treatment of Infections Caused by Gram-Positive Bacteria Abstract Tedizolid and linezolid have antibacterial activity against the most important acute bacterial skin and skin-structure infection (ABSSSIs) pathogens. The object... |
PMC12634351 | core_pubmed_pmc | Evaluation of the pharmacokinetics, pharmacodynamics, and liver ultrasound imaging characteristics of a novel perfluoropropane microbubble in Chinese volunteers | Evaluation of the pharmacokinetics, pharmacodynamics, and liver ultrasound imaging characteristics of a novel perfluoropropane microbubble in Chinese volunteers Abstract Background and Objective Perfluoropropane (PFP), a lipidbased microbubble preparation, is a novel ultrasound contrast agent. This study aims to evalua... |
PMC7051931 | core_pubmed_pmc | Population Pharmacokinetic and Exposure–Response Analysis of Finerenone: Insights Based on Phase IIb Data and Simulations to Support Dose Selection for Pivotal Trials in Type 2 Diabetes with Chronic Kidney Disease | Population Pharmacokinetic and Exposure–Response Analysis of Finerenone: Insights Based on Phase IIb Data and Simulations to Support Dose Selection for Pivotal Trials in Type 2 Diabetes with Chronic Kidney Disease Abstract Background Finerenone (BAY 94-8862) is a potent non-steroidal, selective mineralocorticoid recept... |
PMC11614658 | core_pubmed_pmc | Evaluation of pharmacokinetics and relative bioavailability of pentoxifylline and its metabolite in beagle dogs following different formulations | Evaluation of pharmacokinetics and relative bioavailability of pentoxifylline and its metabolite in beagle dogs following different formulations Abstract Abstract A single-oral-dose, two-period cross-over study with a 5-day washout period under fed condition was conducted in six beagle dogs to explore the pharmacokinet... |
PMC8085977 | core_pubmed_pmc | Exposure–response modeling of peficitinib efficacy in patients with rheumatoid arthritis | Exposure–response modeling of peficitinib efficacy in patients with rheumatoid arthritis Abstract Abstract The aim was to analyze the relationship between peficitinib exposure and efficacy response according to American College of Rheumatology (ACR) 20 criteria and 28‐joint disease activity score based on C‐reactive pr... |
PMC10272300 | core_pubmed_pmc | Bounded integer model‐based analysis of psoriasis area and severity index in patients with moderate‐to‐severe plaque psoriasis receiving BI 730357 | Bounded integer model‐based analysis of psoriasis area and severity index in patients with moderate‐to‐severe plaque psoriasis receiving BI 730357 Abstract Abstract BI 730357 is investigated as an oral treatment of plaque psoriasis. We analyzed the impact of three dosage regimens on the Psoriasis Area and Severity Inde... |
PMC5926077 | core_pubmed_pmc | In vitro antibacterial effect of fosfomycin combination therapy against colistin-resistant Klebsiella pneumoniae | In vitro antibacterial effect of fosfomycin combination therapy against colistin-resistant Klebsiella pneumoniae Abstract Objectives Colistin is still a “last-resort” antibiotic used to manage human infections due to multidrug-resistant (MDR) Klebsiella pneumoniae . However, colistin-resistant K. pneumoniae (CR-Kp) iso... |
PMC12189085 | core_pubmed_pmc | Pharmacokinetics of Isavuconazole During Extracorporeal Membrane Oxygenation Support in Critically Ill Patients: A Case Series | Pharmacokinetics of Isavuconazole During Extracorporeal Membrane Oxygenation Support in Critically Ill Patients: A Case Series Abstract Abstract Background/Objectives: Extracorporeal membrane oxygenation (ECMO) is increasingly used in critically ill patients, but may significantly alter the pharmacokinetics (PK) of ant... |
PMC3235899 | core_pubmed_pmc | Cyclosporine: A Commentary on Brand versus Generic Formulation Exchange | Cyclosporine: A Commentary on Brand versus Generic Formulation Exchange Abstract Abstract The evidence for conversion from brand name to generic equivalent cyclosporine is conflicting. Cyclosporine is a narrow therapeutic-range drug for which small variations in exposure may have severe clinical consequences for transp... |
PMC10989016 | core_pubmed_pmc | Identifying and mathematically modeling the time-course of extracellular metabolic markers associated with resistance to ceftolozane/tazobactam in Pseudomonas aeruginosa | Identifying and mathematically modeling the time-course of extracellular metabolic markers associated with resistance to ceftolozane/tazobactam in Pseudomonas aeruginosa Abstract ABSTRACT Extracellular bacterial metabolites have potential as markers of bacterial growth and resistance emergence but have not been evaluat... |
PMC6479676 | core_pubmed_pmc | A Rapid UPLC-MS Method for Quantification of Gomisin D in Rat Plasma and Its Application to a Pharmacokinetic and Bioavailability Study | A Rapid UPLC-MS Method for Quantification of Gomisin D in Rat Plasma and Its Application to a Pharmacokinetic and Bioavailability Study Abstract Gomisin D, a lignan compound isolated from Fructus Schisandra , is a potential antidiabetic and anti-Alzheimer’s agent. Recently, gomisin D was used as a quality marker of som... |
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