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PMC11888580 | core_pubmed_pmc | Leveraging Patient-Reported Outcome Measures for Optimal Dose Selection in Early Phase Cancer Trials | Leveraging Patient-Reported Outcome Measures for Optimal Dose Selection in Early Phase Cancer Trials Abstract Abstract While patient-reported outcome measures are regularly incorporated into phase 3 clinical trials, they have been infrequently used in early phase trials. However, the patient’s perspective is vital to f... |
PMC8742635 | core_pubmed_pmc | Evaluation of atezolizumab immunogenicity: Clinical pharmacology (part 1) | Evaluation of atezolizumab immunogenicity: Clinical pharmacology (part 1) Abstract Abstract Baseline patient characteristics and prognostic factors are important considerations in oncology when evaluating the impact of immunogenicity on pharmacokinetics (PK) and efficacy. Here, we assessed the impact of anti‐drug antib... |
PMC11117394 | core_pubmed_pmc | A Novel Approach to Integrate Human Biomonitoring Data with Model Predicted Dietary Exposures: A Crop Protection Chemical Case Study Using Lambda-Cyhalothrin | A Novel Approach to Integrate Human Biomonitoring Data with Model Predicted Dietary Exposures: A Crop Protection Chemical Case Study Using Lambda-Cyhalothrin Abstract Abstract The appropriate use of human biomonitoring data to model population chemical exposures is challenging, especially for rapidly metabolized chemic... |
PMC7183132 | core_pubmed_pmc | Volume kinetic analysis of fluid retention after induction of general anesthesia | Volume kinetic analysis of fluid retention after induction of general anesthesia Abstract Abstract Background Induction of general anesthesia increases the hemodilution resulting from infusion of crystalloid fluid, which is believed to be due to slower distribution caused by arterial hypotension. When normal distributi... |
PMC12042691 | core_pubmed_pmc | Exploring neuropharmacokinetics: mechanisms, models, and clinical implications | Exploring neuropharmacokinetics: mechanisms, models, and clinical implications Abstract Neuropharmacokinetics is an emerging field dedicated to understanding the pharmacokinetics of drugs within the central nervous system (CNS), with a particular emphasis on overcoming the challenges posed by the blood-brain barrier. T... |
PMC4993270 | core_pubmed_pmc | Pharmacokinetic profile of defibrotide in patients with renal impairment | Pharmacokinetic profile of defibrotide in patients with renal impairment Abstract Hepatic veno-occlusive disease, also called sinusoidal obstruction syndrome (VOD/SOS), is an unpredictable, potentially life-threatening complication of hematopoietic stem cell transplant conditioning. Severe VOD/SOS, generally associated... |
PMC12451837 | core_pubmed_pmc | The Efficiency of Plant Extracts in the Prevention of Gastric Cancer: A Systematic Review | The Efficiency of Plant Extracts in the Prevention of Gastric Cancer: A Systematic Review Abstract ABSTRACT Background and Aims Gastric cancer is a global health concern with high morbidity and mortality. This systematic review evaluates the potential of plant extracts in the prevention of gastric cancer by analyzing t... |
PMC12579074 | core_pubmed_pmc | Targeting IL-6 Receptor Signaling with Satralizumab in Thyroid Eye Disease: Design of the Phase 3 SatraGO-1 and SatraGO-2 Trials | Targeting IL-6 Receptor Signaling with Satralizumab in Thyroid Eye Disease: Design of the Phase 3 SatraGO-1 and SatraGO-2 Trials Abstract Abstract Introduction Thyroid eye disease (TED) is a rare, autoimmune, orbital inflammatory disorder that is disfiguring, debilitating, and potentially sight-threatening. There is an... |
PMC11252221 | core_pubmed_pmc | Pharmacokinetics and safety of mavacamten in healthy Chinese participants with different CYP2C19 phenotypes | Pharmacokinetics and safety of mavacamten in healthy Chinese participants with different CYP2C19 phenotypes Abstract Abstract Obstructive hypertrophic cardiomyopathy (oHCM) is a subtype of HCM characterized by left ventricular outflow tract obstruction resulting from cardiac muscle hypertrophy and anatomic alterations ... |
PMC9777743 | core_pubmed_pmc | Dalbavancin in clinical practice in Spain: a 2 year retrospective study | Dalbavancin in clinical practice in Spain: a 2 year retrospective study Abstract Abstract Objectives Dalbavancin is approved for the treatment of acute bacterial skin and skin-structure infections (ABSSSIs) in adults. Its unique pharmacokinetic properties allow daily dosing to be avoided. The objective was to describe ... |
PMC12467535 | core_pubmed_pmc | In Vivo Characterization of ONL1204, a Small Peptide Inhibitor of the Fas Receptor, as a Potential Neuroprotective Therapy for Geographic Atrophy and Dry Age-Related Macular Degeneration | In Vivo Characterization of ONL1204, a Small Peptide Inhibitor of the Fas Receptor, as a Potential Neuroprotective Therapy for Geographic Atrophy and Dry Age-Related Macular Degeneration Abstract Background : Age-related macular degeneration (AMD) is a major cause of irreversible vision loss in the developed world, and... |
PMC11944829 | core_pubmed_pmc | A Narrative Review on Higenamine: Pharmacological Properties and Clinical Applications | A Narrative Review on Higenamine: Pharmacological Properties and Clinical Applications Abstract Background: Higenamine, a bioactive alkaloid derived from plants such as Aconitum and Annona squamosa , has been traditionally used in Chinese medicine for treating heart diseases like bradycardia, arrhythmia, and heart fail... |
PMC11613628 | core_pubmed_pmc | Covalent Targeting of Histidine Residues with Aryl Fluorosulfates: Application to Mcl-1 BH3 Mimetics | Covalent Targeting of Histidine Residues with Aryl Fluorosulfates: Application to Mcl-1 BH3 Mimetics Abstract Covalent drugs provide pharmacodynamic and pharmacokinetic advantages over reversible agents. However, covalent strategies have been developed mostly to target cysteine (Cys) residues, which are rarely found in... |
PMC9325750 | core_pubmed_pmc | A curated binary pattern multitarget dataset of focused ATP-binding cassette transporter inhibitors | A curated binary pattern multitarget dataset of focused ATP-binding cassette transporter inhibitors Abstract Multitarget datasets that correlate bioactivity landscapes of small-molecules toward different related or unrelated pharmacological targets are crucial for novel drug design and discovery. ATP-binding cassette (... |
PMC4990596 | core_pubmed_pmc | Tracking Cefoperazone/Sulbactam Resistance Development In vivo in A. baumannii Isolated from a Patient with Hospital-Acquired Pneumonia by Whole-Genome Sequencing | Tracking Cefoperazone/Sulbactam Resistance Development In vivo in A. baumannii Isolated from a Patient with Hospital-Acquired Pneumonia by Whole-Genome Sequencing Abstract Cefoperazone/sulbactam has been shown to be efficacious for the treatment of infections caused by Acinetobacter baumannii ; however, the mechanism u... |
PMC6182466 | core_pubmed_pmc | A Mechanism-Based Population Pharmacokinetic Analysis Assessing the Feasibility of Efavirenz Dose Reduction to 400 mg in Pregnant Women | A Mechanism-Based Population Pharmacokinetic Analysis Assessing the Feasibility of Efavirenz Dose Reduction to 400 mg in Pregnant Women Abstract Abstract Background Reducing the dose of efavirenz can improve safety, reduce costs, and increase access for patients with HIV infection. According to the World Health Organiz... |
PMC6266947 | core_pubmed_pmc | Pharmacokinetics of Sublingually Delivered Fentanyl in Head and Neck Cancer Patients Treated with Curatively Aimed Chemo or Bioradiotherapy | Pharmacokinetics of Sublingually Delivered Fentanyl in Head and Neck Cancer Patients Treated with Curatively Aimed Chemo or Bioradiotherapy Abstract Abstract Over 90% of patients treated for head and neck cancer with curatively aimed chemo or bioradiotherapy will develop painful mucositis and xerostomia. Sublingually d... |
PMC7443729 | core_pubmed_pmc | Optimization of flucloxacillin dosing regimens in critically ill patients using population pharmacokinetic modelling of total and unbound concentrations | Optimization of flucloxacillin dosing regimens in critically ill patients using population pharmacokinetic modelling of total and unbound concentrations Abstract Abstract Background Initial appropriate anti-infective therapy is associated with improved outcomes in patients with severe infections. In critically ill pati... |
PMC8875672 | core_pubmed_pmc | Development and Validation of Open-Source R Package HMCtdm for Therapeutic Drug Monitoring | Development and Validation of Open-Source R Package HMCtdm for Therapeutic Drug Monitoring Abstract Most therapeutic drug monitoring (TDM) packages are based on the maximum a posteriori (MAP) estimation. In this study, HMCtdm, a new TDM package, was developed using a Hamiltonian Monte Carlo (HMC) simulation. The estima... |
PMC5768421 | core_pubmed_pmc | Lactoferrin-modified rotigotine nanoparticles for enhanced nose-to-brain delivery: LESA-MS/MS-based drug biodistribution, pharmacodynamics, and neuroprotective effects | Lactoferrin-modified rotigotine nanoparticles for enhanced nose-to-brain delivery: LESA-MS/MS-based drug biodistribution, pharmacodynamics, and neuroprotective effects Abstract Abstract Introduction Efficient delivery of rotigotine into the brain is crucial for obtaining maximum therapeutic efficacy for Parkinson’s dis... |
PMC5063153 | core_pubmed_pmc | A thorough QTc study demonstrates that olmesartan medoxomil does not prolong the QTc interval | A thorough QTc study demonstrates that olmesartan medoxomil does not prolong the QTc interval Abstract Abstract Two studies (ROADMAP and ORIENT) evaluating the renoprotective effects of olmesartan medoxomil (OM) in patients with type 2 diabetes suggested OM is associated with increased cardiovascular mortality. We cond... |
PMC10076747 | core_pubmed_pmc | Drug exposure during pregnancy: Current understanding and approaches to measure maternal-fetal drug exposure | Drug exposure during pregnancy: Current understanding and approaches to measure maternal-fetal drug exposure Abstract Prescription drug use is prevalent during pregnancy, yet there is limited knowledge about maternal-fetal safety and efficacy of this drug use because pregnant individuals have historically been excluded... |
PMC5004172 | core_pubmed_pmc | Prions efficiently cross the intestinal barrier after oral administration: Study of the bioavailability, and cellular and tissue distribution in vivo | Prions efficiently cross the intestinal barrier after oral administration: Study of the bioavailability, and cellular and tissue distribution in vivo Abstract Abstract Natural forms of prion diseases frequently originate by oral (p.o.) infection. However, quantitative information on the gastro-intestinal (GI) absorptio... |
PMC6270099 | core_pubmed_pmc | Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs | Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs Abstract Abstract Liguzinediol (LZDO) ester prodrugs 3 – 5 were synthesized and evaluated in vitro and in vivo for their potential use in prolonging the half-life of the parent drug LZDO ( 1a ) in vivo . Prodrugs 3 – 5 were found... |
PMC8026416 | core_pubmed_pmc | Extrapolation of pharmacokinetics and pharmacodynamics of sunitinib in children with gastrointestinal stromal tumors | Extrapolation of pharmacokinetics and pharmacodynamics of sunitinib in children with gastrointestinal stromal tumors Abstract Abstract Purpose The starting dose of sunitinib in children with gastrointestinal stromal tumors (GIST) was extrapolated based on data in adults with GIST or solid tumors and children with solid... |
PMC6603215 | core_pubmed_pmc | Exploring the Use of Pegylated Liposomal Doxorubicin (Caelyx ® ) as Pressurized Intraperitoneal Aerosol Chemotherapy | Exploring the Use of Pegylated Liposomal Doxorubicin (Caelyx ® ) as Pressurized Intraperitoneal Aerosol Chemotherapy Abstract Abstract Background: Peritoneal carcinomatosis is a common metastatic pattern in ovarian, gastric, colorectal, and appendiceal cancer; systemic chemotherapy is the current standard of care for p... |
PMC10135278 | core_pubmed_pmc | All Roads Lead to Rome: Enhancing the Probability of Target Attainment with Different Pharmacokinetic/Pharmacodynamic Modelling Approaches | All Roads Lead to Rome: Enhancing the Probability of Target Attainment with Different Pharmacokinetic/Pharmacodynamic Modelling Approaches Abstract In light of rising antimicrobial resistance and a decreasing number of antibiotics with novel modes of action, it is of utmost importance to accelerate development of novel... |
PMC6025247 | core_pubmed_pmc | Pharmacokinetics of Tedizolid and Pseudoephedrine Administered Alone or in Combination in Healthy Volunteers | Pharmacokinetics of Tedizolid and Pseudoephedrine Administered Alone or in Combination in Healthy Volunteers Abstract Therapeutic doses of tedizolid phosphate, an oxazolidinone antibiotic, lack monoamine oxidase inhibition in vivo, potentially resulting in an improved safety profile versus other oxazolidinones. This ra... |
PMC7932974 | core_pubmed_pmc | Sphingosine 1-phosphate Receptor Modulator Therapy for Multiple Sclerosis: Differential Downstream Receptor Signalling and Clinical Profile Effects | Sphingosine 1-phosphate Receptor Modulator Therapy for Multiple Sclerosis: Differential Downstream Receptor Signalling and Clinical Profile Effects Abstract Lysophospholipids are a class of bioactive lipid molecules that produce their effects through various G protein-coupled receptors (GPCRs). Sphingosine 1-phosphate ... |
PMC11647205 | core_pubmed_pmc | First-in-Human Dose-Escalation Study of the First-in-Class PDE3A–SLFN12 Complex Inducer BAY 2666605 in Patients with Advanced Solid Tumors Coexpressing SLFN12 and PDE3A | First-in-Human Dose-Escalation Study of the First-in-Class PDE3A–SLFN12 Complex Inducer BAY 2666605 in Patients with Advanced Solid Tumors Coexpressing SLFN12 and PDE3A Abstract Abstract Purpose: The study aims to evaluate the safety, tolerability, and pharmacokinetics of BAY 2666605, a velcrin that induces complex for... |
PMC11357179 | core_pubmed_pmc | Guidance on Selecting Optimal Steady-State Tacrolimus Concentrations for Continuous IV Perfusion: Insights from Physiologically Based Pharmacokinetic Modeling | Guidance on Selecting Optimal Steady-State Tacrolimus Concentrations for Continuous IV Perfusion: Insights from Physiologically Based Pharmacokinetic Modeling Abstract Abstract Introduction : The dose–response relationships of tacrolimus have been primarily assessed through trough concentrations during intermittent adm... |
PMC10215448 | core_pubmed_pmc | The Antimicrobial Effects of Colistin Encapsulated in Chelating Complex Micelles for the Treatment of Multi-Drug-Resistant Gram-Negative Bacteria: A Pharmacokinetic Study | The Antimicrobial Effects of Colistin Encapsulated in Chelating Complex Micelles for the Treatment of Multi-Drug-Resistant Gram-Negative Bacteria: A Pharmacokinetic Study Abstract Abstract Background: Infections caused by multi-drug-resistant Gram-negative bacteria (MDR-GNB) are an emerging problem globally. Colistin i... |
PMC11179703 | core_pubmed_pmc | Quantitative evaluation of trastuzumab deruxtecan pharmacokinetics and pharmacodynamics in mouse models of varying degrees of HER2 expression | Quantitative evaluation of trastuzumab deruxtecan pharmacokinetics and pharmacodynamics in mouse models of varying degrees of HER2 expression Abstract Abstract Trastuzumab deruxtecan (T‐DXd; DS‐8201; ENHERTU®) is a human epithelial growth factor receptor 2 (HER2)‐directed antibody drug conjugate (ADC) with demonstrated... |
PMC11204537 | core_pubmed_pmc | Dosing Cefazolin for Surgical Site Infection Prophylaxis in Adolescent Idiopathic Scoliosis Surgery: Intermittent Bolus or Continuous Infusion?—A Pilot Study | Dosing Cefazolin for Surgical Site Infection Prophylaxis in Adolescent Idiopathic Scoliosis Surgery: Intermittent Bolus or Continuous Infusion?—A Pilot Study Abstract Abstract Background: Cefazolin may minimize the risk of surgical site infection (SSI) following posterior spinal fusion (PSF) for adolescent idiopathic s... |
PMC9513393 | core_pubmed_pmc | Revealing the mechanism of raw and vinegar-processed Curcuma aromatica Salisb. [Zingiberaceae] regulates primary dysmenorrhea in rats via integrated metabolomics | Revealing the mechanism of raw and vinegar-processed Curcuma aromatica Salisb. [Zingiberaceae] regulates primary dysmenorrhea in rats via integrated metabolomics Abstract Primary dysmenorrhea (PDM) is a common disorder among women around the world. Two processed products of Curcuma aromatica Salisb. [Zingiberaceae] (CA... |
PMC8830040 | core_pubmed_pmc | Population pharmacokinetic analysis and dosage recommendations for digoxin in Japanese patients with atrial fibrillation and heart failure using real-world data | Population pharmacokinetic analysis and dosage recommendations for digoxin in Japanese patients with atrial fibrillation and heart failure using real-world data Abstract Background Digoxin is an important treatment option for reducing the ventricular rate in patients with atrial fibrillation (AF) and heart failure (HF)... |
PMC8093178 | core_pubmed_pmc | Population Pharmacokinetics of Sunitinib and its Active Metabolite SU012662 in Pediatric Patients with Gastrointestinal Stromal Tumors or Other Solid Tumors | Population Pharmacokinetics of Sunitinib and its Active Metabolite SU012662 in Pediatric Patients with Gastrointestinal Stromal Tumors or Other Solid Tumors Abstract Abstract Background and Objective Population pharmacokinetic analysis explored the pharmacokinetics of sunitinib and its primary active metabolite, SU0126... |
PMC4540731 | core_pubmed_pmc | Are Physiologically Based Pharmacokinetic Models Reporting the Right C max ? Central Venous Versus Peripheral Sampling Site | Are Physiologically Based Pharmacokinetic Models Reporting the Right C max ? Central Venous Versus Peripheral Sampling Site Abstract Physiologically based pharmacokinetic (PBPK) models can over-predict maximum plasma concentrations (C max ) following intravenous administration. A proposed explanation is that invariably... |
PMC3113376 | core_pubmed_pmc | A comparative study of the pharmacokinetics of traditional and automated dosing/blood sampling systems using gabapentin | A comparative study of the pharmacokinetics of traditional and automated dosing/blood sampling systems using gabapentin Abstract Objective: The present study was undertaken to investigate the pharmacokinetics (PKs) of gabapentin as determined by traditional manual blood sampling and by using an automated dosing/blood s... |
PMC8638037 | core_pubmed_pmc | Individualized treatment of breast cancer with chronic renal failure: A case report and review of literature | Individualized treatment of breast cancer with chronic renal failure: A case report and review of literature Abstract BACKGROUND Studies have shown that patients with chronic renal failure (CRF) are more likely to suffer from breast cancer and other malignant tumors. To our knowledge, CRF can reduce drug excretion, the... |
PMC6559177 | core_pubmed_pmc | Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation | Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation Abstract Abstract Study Objectives To present results from in vivo studies underlying the preclinical development of lemborexant (E2006), a novel dual orexin (hypocretin) receptor antagonist fo... |
PMC5880335 | core_pubmed_pmc | Pharmacokinetics-adapted Busulfan-based myeloablative conditioning before unrelated umbilical cord blood transplantation for myeloid malignancies in children | Pharmacokinetics-adapted Busulfan-based myeloablative conditioning before unrelated umbilical cord blood transplantation for myeloid malignancies in children Abstract Abstract Unrelated umbilical cord blood transplantation (UCBT) is an alternative to provide transplants in children with acute leukemia or myelodysplasti... |
PMC8886296 | core_pubmed_pmc | Role of Dexamethasone and Methylprednisolone Corticosteroids in Coronavirus Disease 2019 Hospitalized Patients: A Review | Role of Dexamethasone and Methylprednisolone Corticosteroids in Coronavirus Disease 2019 Hospitalized Patients: A Review Abstract The WHO announced coronavirus disease 2019 (COVID-19) as a pandemic disease globally on March 11, 2020, after it emerged in China. The emergence of COVID-19 has lasted over a year, and despi... |
PMC6189138 | core_pubmed_pmc | Anti-tumour activity of a first-in-class agent NUC-1031 in patients with advanced cancer: results of a phase I study | Anti-tumour activity of a first-in-class agent NUC-1031 in patients with advanced cancer: results of a phase I study Abstract Abstract Background Gemcitabine is used to treat a wide range of tumours, but its efficacy is limited by cancer cell resistance mechanisms. NUC-1031, a phosphoramidate modification of gemcitabin... |
PMC12594320 | core_pubmed_pmc | A systematic comparison of patient information leaflets from local and multinational pharmaceutical companies: Assessing content quality and completeness | A systematic comparison of patient information leaflets from local and multinational pharmaceutical companies: Assessing content quality and completeness Abstract Abstract Background It is necessary to provide essential information to patients regarding medication to ensure safe and effective use. Patient Information L... |
PMC5762495 | core_pubmed_pmc | Development of an LC–MS/MS method for the quantitation of deoxyglycychloxazol in rat plasma and its application in pharmacokinetic study ☆ | Development of an LC–MS/MS method for the quantitation of deoxyglycychloxazol in rat plasma and its application in pharmacokinetic study ☆ Abstract Abstract Deoxyglycychloxazol (TY501) is a glycyrrhetinic acid derivative which exhibits high anti-inflammatory activity and reduced pseudoaldosteronism compared to glycyrrh... |
PMC6412143 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of a single dose Nilotinib in individuals with Parkinson's disease | Pharmacokinetics and pharmacodynamics of a single dose Nilotinib in individuals with Parkinson's disease Abstract Abstract Nilotinib is a broad‐based tyrosine kinase inhibitor with the highest affinity to inhibit Abelson (c‐Abl) and discoidin domain receptors (DDR1/2). Preclinical evidence indicates that Nilotinib redu... |
PMC9303624 | core_pubmed_pmc | Bimekizumab for the treatment of moderate‐to‐severe plaque psoriasis: efficacy, safety, pharmacokinetics, pharmacodynamics and transcriptomics from a phase IIa, randomized, double‐blind multicentre study * | Bimekizumab for the treatment of moderate‐to‐severe plaque psoriasis: efficacy, safety, pharmacokinetics, pharmacodynamics and transcriptomics from a phase IIa, randomized, double‐blind multicentre study * Abstract Summary Background Bimekizumab is a monoclonal antibody that selectively inhibits both interleukin (IL)‐1... |
PMC7021089 | core_pubmed_pmc | Pharmacokinetics and safety of aztreonam/avibactam for the treatment of complicated intra-abdominal infections in hospitalized adults: results from the REJUVENATE study | Pharmacokinetics and safety of aztreonam/avibactam for the treatment of complicated intra-abdominal infections in hospitalized adults: results from the REJUVENATE study Abstract Abstract Objectives To investigate pharmacokinetics (PK) and safety (primary objectives) and efficacy (secondary objective) of the investigati... |
PMC3263649 | core_pubmed_pmc | Variability in the Responsiveness to Low-Dose Aspirin: Pharmacological and Disease-Related Mechanisms | Variability in the Responsiveness to Low-Dose Aspirin: Pharmacological and Disease-Related Mechanisms Abstract Abstract The main pharmacological aspects of pharmacodynamics (PD) and pharmacokinetics (PK) of aspirin as antiplatelet agent were unravelled between the late sixties and the eighties, and low-dose aspirin giv... |
PMC4874602 | core_pubmed_pmc | Bedaquiline and Pyrazinamide Treatment Responses Are Affected by Pulmonary Lesion Heterogeneity in Mycobacterium tuberculosis Infected C3HeB/FeJ Mice | Bedaquiline and Pyrazinamide Treatment Responses Are Affected by Pulmonary Lesion Heterogeneity in Mycobacterium tuberculosis Infected C3HeB/FeJ Mice Abstract BALB/c and Swiss mice are routinely used to validate the effectiveness of tuberculosis drug regimens, although these mouse strains fail to develop human-like pul... |
PMC9119441 | core_pubmed_pmc | Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice | Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice Abstract Abstract Drug repurposing has the advantage of shortening regulatory preclinical development steps. Here, we screened a library of drug compounds, already registered in one or several geographical areas, to identify those exhibiting a... |
PMC11434791 | core_pubmed_pmc | Pharmacokinetic Models of Tafenoquine: Insights for Optimal Malaria Treatment Strategies | Pharmacokinetic Models of Tafenoquine: Insights for Optimal Malaria Treatment Strategies Abstract Tafenoquine (TQ) is a new 8-aminoquinoline antimalarial drug developed by the US Army for Plasmodium vivax malaria treatment. Modeling and simulation are essential tools for drug development and improving rationality in ph... |
PMC6658769 | core_pubmed_pmc | First-Time-in-Human Study and Prediction of Early Bactericidal Activity for GSK3036656, a Potent Leucyl-tRNA Synthetase Inhibitor for Tuberculosis Treatment | First-Time-in-Human Study and Prediction of Early Bactericidal Activity for GSK3036656, a Potent Leucyl-tRNA Synthetase Inhibitor for Tuberculosis Treatment Abstract This first-time-in-human (FTIH) study evaluated the safety, tolerability, pharmacokinetics, and food effect of single and repeat oral doses of GSK3036656,... |
PMC12735571 | core_pubmed_pmc | DoE- and PBBM-Driven Formulation Development of an Extended-Release Donepezil Tablet | DoE- and PBBM-Driven Formulation Development of an Extended-Release Donepezil Tablet Abstract Background/Objectives : This study explores the integration of Design of Experiments (DoE) with Physiologically Based Biopharmaceutics Modeling (PBBM) to streamline the development of extended-release (XR) formulations. Using ... |
PMC8996404 | core_pubmed_pmc | The pharmacokinetics of buserelin after intramuscular administration in pigs and cows | The pharmacokinetics of buserelin after intramuscular administration in pigs and cows Abstract Background Buserelin is a luteinizing hormone releasing hormone (LHRH) agonist used for the treatment of hormone-dependent diseases in males and females. However, the pharmacokinetics of buserelin in pigs and cows are not ful... |
PMC11208791 | core_pubmed_pmc | Quantification of Rhodojaponin II and Rhodojaponin III in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry | Quantification of Rhodojaponin II and Rhodojaponin III in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Abstract Abstract An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed to determine the concentrations of Rhodojaponin II and Rhodojap... |
PMC12043107 | core_pubmed_pmc | Preclinical pharmacokinetics, distribution, metabolism and excretion of disitamab vedotin | Preclinical pharmacokinetics, distribution, metabolism and excretion of disitamab vedotin Abstract Abstract Background and purpose Disitamab vedotin is an antibody-drug conjugate (ADC) composed of a humanized IgG1 monoclonal antibody (mAb) targeting HER2 conjugated to monomethyl auristatin E(MMAE) via a cleavable dipep... |
PMC9540401 | core_pubmed_pmc | What is the value of faster acting prandial insulin? Focus on ultra rapid lispro | What is the value of faster acting prandial insulin? Focus on ultra rapid lispro Abstract Abstract Rapid‐acting insulins (RAIs) have been instrumental in the management of diabetes because of their improved postprandial glucose (PPG) control compared with regular human insulin. However, their absorption rate and time a... |
PMC8672039 | core_pubmed_pmc | Integrated Network Pharmacology and Lipidomics to Reveal the Inhibitory Effect of Qingfei Oral Liquid on Excessive Autophagy in RSV-Induced Lung Inflammation | Integrated Network Pharmacology and Lipidomics to Reveal the Inhibitory Effect of Qingfei Oral Liquid on Excessive Autophagy in RSV-Induced Lung Inflammation Abstract Abstract Background: Respiratory syncytial virus (RSV) can cause varying degrees of lung inflammation in children. Qingfei Oral Liquid (QF) is effective ... |
PMC9545268 | core_pubmed_pmc | Sexually transmitted doping: The impact of urine contamination of semen | Sexually transmitted doping: The impact of urine contamination of semen Abstract Abstract The high sensitivity of antidoping detection tests creates the possibility of inadvertent doping due to an athlete's unknowing ingestion of contaminated environmental sources such as dietary supplements, food, or drinks. Recently,... |
PMC3738144 | core_pubmed_pmc | Phase 1 study of lenvatinib combined with carboplatin and paclitaxel in patients with non-small-cell lung cancer | Phase 1 study of lenvatinib combined with carboplatin and paclitaxel in patients with non-small-cell lung cancer Abstract Background: This dose-finding study evaluated lenvatinib, an oral multitargeted receptor tyrosine kinase inhibitor, in combination with carboplatin/paclitaxel in chemotherapy-naïve non-small-cell lu... |
PMC11495133 | core_pubmed_pmc | On placental and lactational transfer of IgG‐based therapeutic proteins – Current understanding and knowledge gaps from a clinical pharmacology perspective | On placental and lactational transfer of IgG‐based therapeutic proteins – Current understanding and knowledge gaps from a clinical pharmacology perspective Abstract Abstract Maternal medication use may expose the developing fetus through placental transfer or the infant through lactational transfer. Because pregnant an... |
PMC11701965 | core_pubmed_pmc | A Phase 1 Study to Evaluate the Pharmacokinetic Drug‐Drug Interaction Between Islatravir and Methadone in Participants on Stable Methadone Therapy | A Phase 1 Study to Evaluate the Pharmacokinetic Drug‐Drug Interaction Between Islatravir and Methadone in Participants on Stable Methadone Therapy Abstract Abstract Islatravir is a nucleoside reverse transcriptase translocation inhibitor in development for the treatment of HIV‐1. People living with HIV‐1 receiving meth... |
PMC5131886 | core_pubmed_pmc | Bridging Sunitinib Exposure to Time‐to‐Tumor Progression in Hepatocellular Carcinoma Patients With Mathematical Modeling of an Angiogenic Biomarker | Bridging Sunitinib Exposure to Time‐to‐Tumor Progression in Hepatocellular Carcinoma Patients With Mathematical Modeling of an Angiogenic Biomarker Abstract Hepatocellular carcinoma (HCC) is third in cancer‐related causes of death worldwide and its treatment is a significant unmet medical need. Sunitinib is a selective... |
PMC5116175 | core_pubmed_pmc | Estimation of tulathromycin depletion in plasma and milk after subcutaneous injection in lactating goats using a nonlinear mixed-effects pharmacokinetic modeling approach | Estimation of tulathromycin depletion in plasma and milk after subcutaneous injection in lactating goats using a nonlinear mixed-effects pharmacokinetic modeling approach Abstract Background Extra-label use of tulathromycin in lactating goats is common and may cause violative residues in milk. The objective of this stu... |
PMC11191404 | core_pubmed_pmc | Reversible Chemical Modification of Antibody Effector Function Mitigates Unwanted Systemic Immune Activation | Reversible Chemical Modification of Antibody Effector Function Mitigates Unwanted Systemic Immune Activation Abstract Abstract Antibody effector functions including antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) are mediated through the interaction of the antibody Fc region with Fcγ receptors p... |
PMC12625083 | core_pubmed_pmc | Postmarketing Assessment of Antibody–Drug Conjugates: Proof‐of‐Concept Using Model‐Based Meta‐Analysis and a Clinical Utility Index Approach | Postmarketing Assessment of Antibody–Drug Conjugates: Proof‐of‐Concept Using Model‐Based Meta‐Analysis and a Clinical Utility Index Approach Abstract ABSTRACT Antibody–drug conjugates (ADCs) are a promising class of targeted cancer therapies. However, they need careful dose optimization to maximize effectiveness and mi... |
PMC11898576 | core_pubmed_pmc | Anticholinesterase and carbonic anhydrase inhibitory activities of natural carnosic acid derivatives: A comprehensive in vitro and in silico study | Anticholinesterase and carbonic anhydrase inhibitory activities of natural carnosic acid derivatives: A comprehensive in vitro and in silico study Abstract Abstract This study investigates the anticholinesterase (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and carbonic anhydrase (CAI and CAII) inhibit... |
PMC4981156 | core_pubmed_pmc | Quantification of simvastatin in mice plasma by near-infrared and chemometric analysis of spectral data | Quantification of simvastatin in mice plasma by near-infrared and chemometric analysis of spectral data Abstract Time and cost saving is an essential requirement in pharmacokinetics and bioequivalence studies. The aim of this study is to use a simple, fast, and nondestructive near-infrared transmission spectroscopic me... |
PMC8228202 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Meropenem by Extended or Continuous Infusion in Low Body Weight Critically Ill Patients | Pharmacokinetics and Pharmacodynamics of Meropenem by Extended or Continuous Infusion in Low Body Weight Critically Ill Patients Abstract Abstract Background : Pathophysiological changes such as extreme body weights in critically ill patients with severe infections may alter the pharmacokinetics (PK) of antimicrobials,... |
PMC8926166 | core_pubmed_pmc | Pharmacometric Analysis of Intranasal and Intravenous Nalbuphine to Optimize Pain Management in Infants | Pharmacometric Analysis of Intranasal and Intravenous Nalbuphine to Optimize Pain Management in Infants Abstract Abstract Objectives The objective of this pharmacometric (PMX) study was to (i) characterize population pharmacokinetics (PPK) and exposure-pain response associations following intranasal (0.1 mg/kg) or intr... |
PMC9417013 | core_pubmed_pmc | Molecular docking, simulation and binding free energy analysis of small molecules as Pf HT1 inhibitors | Molecular docking, simulation and binding free energy analysis of small molecules as Pf HT1 inhibitors Abstract Abstract Antimalarial drug resistance has thrown a spanner in the works of malaria elimination. New drugs are required for ancillary support of existing malaria control efforts. Plasmodium falciparum requires... |
PMC4462042 | core_pubmed_pmc | GHB Pharmacology and Toxicology: Acute Intoxication, Concentrations in Blood and Urine in Forensic Cases and Treatment of the Withdrawal Syndrome | GHB Pharmacology and Toxicology: Acute Intoxication, Concentrations in Blood and Urine in Forensic Cases and Treatment of the Withdrawal Syndrome Abstract Abstract The illicit recreational drug of abuse, γ-hydroxybutyrate (GHB) is a potent central nervous system depressant and is often encountered during forensic inves... |
PMC9818079 | core_pubmed_pmc | Adherence to the CDK 4/6 Inhibitor Palbociclib and Omission of Dose Management Supported by Pharmacometric Modelling as Part of the OpTAT Study | Adherence to the CDK 4/6 Inhibitor Palbociclib and Omission of Dose Management Supported by Pharmacometric Modelling as Part of the OpTAT Study Abstract Simple Summary Medication adherence to CDK4/6 inhibitors such as palbociclib, prescribed as a cyclic oral anticancer therapy in women diagnosed with advanced breast ca... |
PMC12281427 | core_pubmed_pmc | Overcoming multidrug resistance in gastrointestinal cancers with a CDH17-targeted ADC conjugated to a DNA topoisomerase inhibitor | Overcoming multidrug resistance in gastrointestinal cancers with a CDH17-targeted ADC conjugated to a DNA topoisomerase inhibitor Abstract Summary Cadherin 17 (CDH17) has emerged as a promising target for gastrointestinal (GI) cancers, which are often complicated by multidrug resistance (MDR) and recurrence. In this st... |
PMC7996972 | core_pubmed_pmc | TBDBT: A TB DataBase Template for collection of harmonized TB clinical research data in REDCap, facilitating data standardisation for inter-study comparison and meta-analyses | TBDBT: A TB DataBase Template for collection of harmonized TB clinical research data in REDCap, facilitating data standardisation for inter-study comparison and meta-analyses Abstract Clinical tuberculosis research, both within research groups and across research ecosystems, is often undertaken in isolation using bespo... |
PMC11648756 | core_pubmed_pmc | Complex immunogenicity assessment in caplacizumab-treated patients with immune-mediated thrombotic thrombocytopenic purpura who have received plasma exchange | Complex immunogenicity assessment in caplacizumab-treated patients with immune-mediated thrombotic thrombocytopenic purpura who have received plasma exchange Abstract Background International Society on Thrombosis and Haemostasis guidelines for immune-mediated thrombotic thrombocytopenic purpura (iTTP) treatment recomm... |
PMC10060561 | core_pubmed_pmc | Acori Tatarinowii Rhizoma: A comprehensive review of its chemical composition, pharmacology, pharmacokinetics and toxicity | Acori Tatarinowii Rhizoma: A comprehensive review of its chemical composition, pharmacology, pharmacokinetics and toxicity Abstract Acori Tatarinowii Rhizoma (ATR, Shi Chang Pu in Chinese), a natural product with multiple targets in various diseases. This review provides the comprehensive summary of the chemical compos... |
PMC5861163 | core_pubmed_pmc | Analysis of different innovative formulations of curcumin for improved relative oral bioavailability in human subjects | Analysis of different innovative formulations of curcumin for improved relative oral bioavailability in human subjects Abstract Abstract Purpose The optimal health benefits of curcumin are limited by its low solubility in water and corresponding poor intestinal absorption. Cyclodextrins (CD) can form inclusion complexe... |
PMC11333285 | core_pubmed_pmc | Inhibition of lysine acetyltransferase KAT6 in ER + HER2 − metastatic breast cancer: a phase 1 trial | Inhibition of lysine acetyltransferase KAT6 in ER + HER2 − metastatic breast cancer: a phase 1 trial Abstract Abstract Inhibition of histone lysine acetyltransferases (KATs) KAT6A and KAT6B has shown antitumor activity in estrogen receptor-positive (ER + ) breast cancer preclinical models. PF-07248144 is a selective ca... |
PMC4715838 | core_pubmed_pmc | Caffeine enhances the antidepressant-like activity of common antidepressant drugs in the forced swim test in mice | Caffeine enhances the antidepressant-like activity of common antidepressant drugs in the forced swim test in mice Abstract Abstract Caffeine is the most widely used behaviorally active drug in the world which exerts its activity on central nervous system through adenosine receptors. Worrying data indicate that excessiv... |
PMC8948897 | core_pubmed_pmc | Growth Optimization and Secondary Metabolites Evaluation of Anabaena variabilis for Acetylcholinesterase Inhibition Activity | Growth Optimization and Secondary Metabolites Evaluation of Anabaena variabilis for Acetylcholinesterase Inhibition Activity Abstract Abstract Cyanobacteria comprise a good natural resource of a potential variety of neuro-chemicals, including acetylcholinesterase inhibitors essential for Alzheimer’s disease treatment. ... |
PMC9316855 | core_pubmed_pmc | Synthesis and Systematic Study on the Effect of Different PEG Units on Stability of PEGylated, Integrin-αvβ6-Specific A20FMDV2 Analogues in Rat Serum and Human Plasma | Synthesis and Systematic Study on the Effect of Different PEG Units on Stability of PEGylated, Integrin-αvβ6-Specific A20FMDV2 Analogues in Rat Serum and Human Plasma Abstract A20FMDV2 is a 20-mer peptide that exhibits high selectivity and affinity for the tumour-related αvβ6 integrin that can compete with extracellula... |
PMC12035591 | core_pubmed_pmc | Pharmacokinetic characterization and exposure–response relationship of crovalimab in the COMMODORE 1, 2 and 3 and COMPOSER trials of patients with paroxysmal nocturnal haemoglobinuria | Pharmacokinetic characterization and exposure–response relationship of crovalimab in the COMMODORE 1, 2 and 3 and COMPOSER trials of patients with paroxysmal nocturnal haemoglobinuria Abstract Abstract Aims Crovalimab is a novel C5 inhibitor administered first intravenously and then subcutaneously in patients with paro... |
PMC7341313 | core_pubmed_pmc | Anthelmintic Efficacy and Pharmacokinetics of Ivermectin Paste after Oral Administration in Mules Infected by Cyathostomins | Anthelmintic Efficacy and Pharmacokinetics of Ivermectin Paste after Oral Administration in Mules Infected by Cyathostomins Abstract Abstract Simple Summary Mules and donkeys are often treated as horses from a therapeutic point of view. This approach could be dangerous due to species differences in drug pharmacokinetic... |
PMC5021044 | core_pubmed_pmc | Dose‐escalation study of tabalumab with bortezomib and dexamethasone in Japanese patients with multiple myeloma | Dose‐escalation study of tabalumab with bortezomib and dexamethasone in Japanese patients with multiple myeloma Abstract B‐cell activating factor ( BAFF ) promotes the survival and adhesion of multiple myeloma ( MM ) cells. Tabalumab ( LY 2127399) is an anti‐ BAFF monoclonal antibody. This phase 1, multicenter, open‐la... |
PMC11098162 | core_pubmed_pmc | Pharmacokinetics and exposure–safety relationship of ciprofol for sedation in mechanically ventilated patients in the intensive care unit | Pharmacokinetics and exposure–safety relationship of ciprofol for sedation in mechanically ventilated patients in the intensive care unit Abstract Abstract Ciprofol (HSK3486) is a newly developed, highly selective γ‐aminobutyric acid‐A (GABA A ) receptor potentiator that is recently approved for a new indication of sed... |
PMC10087067 | core_pubmed_pmc | Characterizing complex and competing drug–drug interactions between the antiviral regimen of glecaprevir and pibrentasvir with rifampin or carbamazepine | Characterizing complex and competing drug–drug interactions between the antiviral regimen of glecaprevir and pibrentasvir with rifampin or carbamazepine Abstract Abstract The fixed‐dose combination of the direct acting antivirals glecaprevir (GLE) and pibrentasvir (PIB) is an oral, once‐daily treatment for all six majo... |
PMC3758109 | core_pubmed_pmc | Efficient 18 F-Labeling of Synthetic Exendin-4 Analogues for Imaging Beta Cells | Efficient 18 F-Labeling of Synthetic Exendin-4 Analogues for Imaging Beta Cells Abstract A number of exendin derivatives have been developed to target glucagon-like peptide 1 (GLP-1) receptors on beta cells in vivo. Modifications of exendin analogues have been shown to have significant effects on pharmacokinetics and, ... |
PMC4577263 | core_pubmed_pmc | Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers | Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers Abstract Abstract The aim of this study is to prepare fluvastatin nanostructured lipid carriers (FLV-NLCs) in order to find an innovative way to alleviate FLV-associated disadvantages. The limitations include poor solubility and exte... |
PMC11938982 | core_pubmed_pmc | NALIRIFOX in Japanese treatment-naïve patients with metastatic pancreatic adenocarcinoma: an open-label, phase II trial design | NALIRIFOX in Japanese treatment-naïve patients with metastatic pancreatic adenocarcinoma: an open-label, phase II trial design Abstract ABSTRACT This is a single arm, open label trial to assess the safety and efficacy of NALIRIFOX in Japanese participants who have not previously received therapy for metastatic adenocar... |
PMC7719369 | core_pubmed_pmc | hIL‐7‐hyFc, A Long‐Acting IL‐7, Increased Absolute Lymphocyte Count in Healthy Subjects | hIL‐7‐hyFc, A Long‐Acting IL‐7, Increased Absolute Lymphocyte Count in Healthy Subjects Abstract A low lymphocyte count puts immune‐compromised patients at risk of mortality. hIL‐7‐hyFc is a homodimeric interleukin‐7 (IL‐7), a potent T‐cell amplifier, fused to the hybridizing IgD/IgG4 immunoglobulin domain. We performe... |
PMC10050386 | core_pubmed_pmc | Population PK/PD modelling of meropenem in preterm newborns based on therapeutic drug monitoring data | Population PK/PD modelling of meropenem in preterm newborns based on therapeutic drug monitoring data Abstract Background: Preterm neonates rarely participate in clinical trials, this leads to lack of adequate information on pharmacokinetics for most drugs in this population. Meropenem is used in neonates to treat seve... |
PMC11173459 | core_pubmed_pmc | The Discovery of Selective Protein Arginine Methyltransferase 5 Inhibitors in the Management of β-Thalassemia through Computational Methods | The Discovery of Selective Protein Arginine Methyltransferase 5 Inhibitors in the Management of β-Thalassemia through Computational Methods Abstract Abstract β-Thalassemia is an inherited genetic disorder associated with β-globin chain synthesis, which ultimately becomes anemia. Adenosine-2,3-dialdehyde, by inhibiting ... |
PMC3743329 | core_pubmed_pmc | A quick review of carbamazepine pharmacokinetics in epilepsy from 1953 to 2012 | A quick review of carbamazepine pharmacokinetics in epilepsy from 1953 to 2012 Abstract Background: Carbamazepine has been used as AEDs since 1965, and is most effective against partial seizures. Two basic mechanisms of action have been proposed: 1) enhancement of sodium channel inactivation by reducing high-frequency ... |
PMC6175298 | core_pubmed_pmc | A Randomized, First‐in‐Human, Healthy Volunteer Trial of sutimlimab, a Humanized Antibody for the Specific Inhibition of the Classical Complement Pathway | A Randomized, First‐in‐Human, Healthy Volunteer Trial of sutimlimab, a Humanized Antibody for the Specific Inhibition of the Classical Complement Pathway Abstract Aberrant activation of the classical complement pathway is the common underlying pathophysiology of orphan diseases such as bullous pemphigoid, antibody‐medi... |
PMC3207826 | core_pubmed_pmc | Phase I Evaluation of STA-1474, a Prodrug of the Novel HSP90 Inhibitor Ganetespib, in Dogs with Spontaneous Cancer | Phase I Evaluation of STA-1474, a Prodrug of the Novel HSP90 Inhibitor Ganetespib, in Dogs with Spontaneous Cancer Abstract Abstract Background The novel water soluble compound STA-1474 is metabolized to ganetespib (formerly STA-9090), a potent HSP90 inhibitor previously shown to kill canine tumor cell lines in vitro a... |
PMC5512459 | core_pubmed_pmc | Pharmacodynamic Monitoring of RO5459072, a Small Molecule Inhibitor of Cathepsin S | Pharmacodynamic Monitoring of RO5459072, a Small Molecule Inhibitor of Cathepsin S Abstract Abstract Major histocompatibility complex class II (MHCII)-restricted antigen priming of CD4 + T cells is both involved in adaptive immune responses and the pathogenesis of autoimmune diseases. Degradation of invariant chain Ii,... |
PMC8172506 | core_pubmed_pmc | Improved Decision-Making Confidence Using Item-Based Pharmacometric Model: Illustration with a Phase II Placebo-Controlled Trial | Improved Decision-Making Confidence Using Item-Based Pharmacometric Model: Illustration with a Phase II Placebo-Controlled Trial Abstract Abstract This study aimed to illustrate how a new methodology to assess clinical trial outcome measures using a longitudinal item response theory–based model (IRM) could serve as an ... |
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