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PMC6732506 | core_pubmed_pmc | Genetic polymorphisms of CYP3A5, CHRM2, and ZNF498 and their association with epilepsy susceptibility: a pharmacogenetic and case–control study | Genetic polymorphisms of CYP3A5, CHRM2, and ZNF498 and their association with epilepsy susceptibility: a pharmacogenetic and case–control study Abstract Abstract Background A total of 50 million persons were diagnosed worldwide with epilepsy. One-third of them are experiencing debilitating seizures despite optimum anti... |
PMC10009698 | core_pubmed_pmc | AV-101, a novel inhaled dry-powder formulation of imatinib, in healthy adult participants: a phase 1 single and multiple ascending dose study | AV-101, a novel inhaled dry-powder formulation of imatinib, in healthy adult participants: a phase 1 single and multiple ascending dose study Abstract Abstract Background Oral imatinib has been shown to be effective, but poorly tolerated, in patients with advanced pulmonary arterial hypertension (PAH). To maintain effi... |
PMC10582660 | core_pubmed_pmc | Co‐consuming green tea with raloxifene decreases raloxifene systemic exposure in healthy adult participants | Co‐consuming green tea with raloxifene decreases raloxifene systemic exposure in healthy adult participants Abstract Abstract Green tea is a popular beverage worldwide. The abundant green tea catechin (−)‐epigallocatechin gallate (EGCG) is a potent in vitro inhibitor of intestinal UDP‐glucuronosyltransferase (UGT) acti... |
PMC6587462 | core_pubmed_pmc | Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy‐Induced Nausea and Vomiting | Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy‐Induced Nausea and Vomiting Abstract Abstract NEPA is the first fixed‐combination antiemetic composed of the neurokinin‐1 receptor antagonist netupitant (netupi... |
PMC9835139 | core_pubmed_pmc | An introduction to causal inference for pharmacometricians | An introduction to causal inference for pharmacometricians Abstract Abstract As formal causal inference begins to play a greater role in disciplines that intersect with pharmacometrics, such as biostatistics, epidemiology, and artificial intelligence/machine learning, pharmacometricians may increasingly benefit from a ... |
PMC10675329 | core_pubmed_pmc | Enhancing Pharmacokinetics and Pharmacodynamics of Rosuvastatin Calcium through the Development and Optimization of Fast-Dissolving Films | Enhancing Pharmacokinetics and Pharmacodynamics of Rosuvastatin Calcium through the Development and Optimization of Fast-Dissolving Films Abstract Abstract Rosuvastatin (RSV) is a widely used cholesterol-lowering medication, but its limited bioavailability due to its susceptibility to stomach pH and extensive first-pas... |
PMC8224376 | core_pubmed_pmc | Modelling Hydrocortisone Pharmacokinetics on a Subcutaneous Pulsatile Infusion Replacement Strategy in Patients with Adrenocortical Insufficiency | Modelling Hydrocortisone Pharmacokinetics on a Subcutaneous Pulsatile Infusion Replacement Strategy in Patients with Adrenocortical Insufficiency Abstract In the context of glucocorticoid (GC) therapeutics, recent studies have utilised a subcutaneous hydrocortisone (HC) infusion pump programmed to deliver multiple HC p... |
PMC11365236 | core_pubmed_pmc | In silico, in vitro, and in vivo acute and sub-acute toxicity profiling of whole plant methanol extract of Equisetum diffusum D. Don from the sub-Himalayan West Bengal, India, having ethnobotanical uses | In silico, in vitro, and in vivo acute and sub-acute toxicity profiling of whole plant methanol extract of Equisetum diffusum D. Don from the sub-Himalayan West Bengal, India, having ethnobotanical uses Abstract Background Equisetum diffusum D. Don commonly known as ‘Himalayan horsetail’, has been traditionally used in... |
PMC9600142 | core_pubmed_pmc | Coming of Age for BTK Inhibitor Therapy: A Review of Zanubrutinib in Waldenström Macroglobulinemia | Coming of Age for BTK Inhibitor Therapy: A Review of Zanubrutinib in Waldenström Macroglobulinemia Abstract Waldenström macroglobulinemia (WM) is a rare form of non-Hodgkin B-cell lymphoma with a variable clinical presentation that can impact a patient’s quality of life by causing anemia, peripheral neuropathy, serum h... |
PMC8117330 | core_pubmed_pmc | Dexketoprofen Pharmacokinetics is not Significantly Altered by Genetic Polymorphism | Dexketoprofen Pharmacokinetics is not Significantly Altered by Genetic Polymorphism Abstract Dexketoprofen is the (S)-(+)-enantiomer of racemic ketoprofen, a nonsteroidal anti-inflammatory drug used for the management of different types of pain. To the best of our knowledge, no article was published to date on dexketop... |
PMC8224802 | core_pubmed_pmc | Assessment of Metabolic Interaction between Repaglinide and Quercetin via Mixed Inhibition in the Liver: In Vitro and In Vivo | Assessment of Metabolic Interaction between Repaglinide and Quercetin via Mixed Inhibition in the Liver: In Vitro and In Vivo Abstract Repaglinide (RPG), a rapid-acting meglitinide analog, is an oral hypoglycemic agent for patients with type 2 diabetes mellitus. Quercetin (QCT) is a well-known antioxidant and antidiabe... |
PMC10077952 | core_pubmed_pmc | The N‐Acetylgalactosamine ‐conjugated small interfering RNA inclisiran can be coadministered safely with atorvastatin in cynomolgus monkeys resulting in additive low‐density lipoprotein cholesterol reductions | The N‐Acetylgalactosamine ‐conjugated small interfering RNA inclisiran can be coadministered safely with atorvastatin in cynomolgus monkeys resulting in additive low‐density lipoprotein cholesterol reductions Abstract Abstract Inclisiran, a small interfering RNA, selectively inhibits proprotein convertase subtilisin/ke... |
PMC7015742 | core_pubmed_pmc | Imatinib, sunitinib and pazopanib: From flat‐fixed dosing towards a pharmacokinetically guided personalized dose | Imatinib, sunitinib and pazopanib: From flat‐fixed dosing towards a pharmacokinetically guided personalized dose Abstract Abstract Tyrosine kinase inhibitors (TKIs) are anti‐cancer drugs that target tyrosine kinases, enzymes that are involved in multiple cellular processes. Currently, multiple oral TKIs have been intro... |
PMC8442892 | core_pubmed_pmc | Rare genetic variability in human drug target genes modulates drug response and can guide precision medicine | Rare genetic variability in human drug target genes modulates drug response and can guide precision medicine Abstract Abstract Interindividual variability in drug response constitutes a major concern in pharmacotherapy. While polymorphisms in genes involved in drug disposition have been extensively studied, drug target... |
PMC8423465 | core_pubmed_pmc | High-Dose Oral and Intravenous Rifampicin for the Treatment of Tuberculous Meningitis in Predominantly Human Immunodeficiency Virus (HIV)-Positive Ugandan Adults: A Phase II Open-Label Randomized Controlled Trial | High-Dose Oral and Intravenous Rifampicin for the Treatment of Tuberculous Meningitis in Predominantly Human Immunodeficiency Virus (HIV)-Positive Ugandan Adults: A Phase II Open-Label Randomized Controlled Trial Abstract Abstract Background High-dose rifampicin may improve outcomes of tuberculous meningitis (TBM). Lit... |
PMC5064970 | core_pubmed_pmc | The pharmacokinetics, bioavailability and excretion of bergapten after oral and intravenous administration in rats using high performance liquid chromatography with fluorescence detection | The pharmacokinetics, bioavailability and excretion of bergapten after oral and intravenous administration in rats using high performance liquid chromatography with fluorescence detection Abstract A sensitive, specific, reproducible and optimized high performance liquid chromatography with fluorescence detection (HPLC-... |
PMC7600799 | core_pubmed_pmc | The Development and Validation of a Novel “Dual Cocktail” Probe for Cytochrome P450s and Transporter Functions to Evaluate Pharmacokinetic Drug-Drug and Herb-Drug Interactions | The Development and Validation of a Novel “Dual Cocktail” Probe for Cytochrome P450s and Transporter Functions to Evaluate Pharmacokinetic Drug-Drug and Herb-Drug Interactions Abstract This study was designed to develop and validate a 10 probe drug cocktail named “Dual Cocktail”, composed of caffeine (Cyp1a2 in rat and... |
PMC9167594 | core_pubmed_pmc | Subcutaneously-Administered Infliximab in the Management of Rheumatoid Arthritis: A Short Narrative Review of Current Clinical Evidence | Subcutaneously-Administered Infliximab in the Management of Rheumatoid Arthritis: A Short Narrative Review of Current Clinical Evidence Abstract Abstract The first subcutaneous (SC) formulation of infliximab CT-P13 has been authorized for the treatment of rheumatoid arthritis (RA) in Europe in 2019. Later, in 2020, app... |
PMC12847311 | core_pubmed_pmc | Intraoperative hypotension trajectories and their predictive value for major postoperative complications: a retrospective cohort study | Intraoperative hypotension trajectories and their predictive value for major postoperative complications: a retrospective cohort study Abstract Abstract Background Intraoperative hypotension (IOH) is a common hemodynamic disturbance during major non-cardiac surgery, yet the prognostic significance of different temporal... |
PMC2810279 | core_pubmed_pmc | Two-stage model-based clinical trial design to optimize phase I development of novel anticancer agents | Two-stage model-based clinical trial design to optimize phase I development of novel anticancer agents Abstract Summary Background The phase I program of anticancer agents usually consists of multiple dose escalation studies to select a safe dose for various administration schedules. We hypothesized that pharmacokineti... |
PMC12107730 | core_pubmed_pmc | Multiplex LC–MS/MS assay for simultaneous quantification of artesunate and its active metabolite dihydroartemisinin with pyronaridine, proguanil, cycloguanil, and clindamycin in pharmacokinetic studies | Multiplex LC–MS/MS assay for simultaneous quantification of artesunate and its active metabolite dihydroartemisinin with pyronaridine, proguanil, cycloguanil, and clindamycin in pharmacokinetic studies Abstract Abstract Background Malaria, especially caused by Plasmodium falciparum , remains a major global health conce... |
PMC12027966 | core_pubmed_pmc | Rehmanniae Radix Praeparata in Blood Deficiency Syndrome: UPLC-Q-TOF-MS Profiling, Network Pharmacology, and PI3K-AKT Activation | Rehmanniae Radix Praeparata in Blood Deficiency Syndrome: UPLC-Q-TOF-MS Profiling, Network Pharmacology, and PI3K-AKT Activation Abstract Abstract This study investigated the therapeutic mechanism of Rehmanniae Radix Praeparata (RRP) in treating blood deficiency syndrome (BDS) through integrated chemical analysis and p... |
PMC5325427 | core_pubmed_pmc | Phase Ib/II randomized, open-label study of doxorubicin and cyclophosphamide with or without low-dose, short-course sunitinib in the pre-operative treatment of breast cancer | Phase Ib/II randomized, open-label study of doxorubicin and cyclophosphamide with or without low-dose, short-course sunitinib in the pre-operative treatment of breast cancer Abstract Abstract Background Prolonged anti-angiogenic therapy destroys tumor vasculature, whereas vascular-normalizing doses may enhance intra-tu... |
PMC8737424 | core_pubmed_pmc | Aspects of high-performance and bio-acceptable magnetic nanoparticles for biomedical application | Aspects of high-performance and bio-acceptable magnetic nanoparticles for biomedical application Abstract Abstract This review covers extensively the synthesis & surface modification, characterization, and application of magnetic nanoparticles. For biomedical applications, consideration should be given to factors such ... |
PMC7400126 | core_pubmed_pmc | Bacteriophages and the One Health Approach to Combat Multidrug Resistance: Is This the Way? | Bacteriophages and the One Health Approach to Combat Multidrug Resistance: Is This the Way? Abstract Abstract Antimicrobial resistance necessitates action to reduce and eliminate infectious disease, ensure animal and human health, and combat emerging diseases. Species such as Acinetobacter baumanniii , vancomycin resis... |
PMC4377464 | core_pubmed_pmc | Herb-Drug Pharmacokinetic Interaction of a Traditional Chinese Medicine Jia-Wei-Xiao-Yao-San with 5-Fluorouracil in the Blood and Brain of Rat Using Microdialysis | Herb-Drug Pharmacokinetic Interaction of a Traditional Chinese Medicine Jia-Wei-Xiao-Yao-San with 5-Fluorouracil in the Blood and Brain of Rat Using Microdialysis Abstract According to a survey from the National Health Insurance Research Database (NHIRD), Jia-Wei-Xiao-Yao-San (JWXYS) is the most popular Chinese medicin... |
PMC12794725 | core_pubmed_pmc | Comparative pharmacokinetics of voriconazole between elderly and young adult patients: a population pharmacokinetic study | Comparative pharmacokinetics of voriconazole between elderly and young adult patients: a population pharmacokinetic study Abstract ABSTRACT Background Voriconazole (VCZ) belongs to the class of broad-spectrum antifungal agents, and it is commonly used for the treatment of serious fungal infections. Safe and effective t... |
PMC6368728 | core_pubmed_pmc | Ambroxol as a novel disease-modifying treatment for Parkinson’s disease dementia: protocol for a single-centre, randomized, double-blind, placebo-controlled trial | Ambroxol as a novel disease-modifying treatment for Parkinson’s disease dementia: protocol for a single-centre, randomized, double-blind, placebo-controlled trial Abstract Abstract Background Currently there are no disease-modifying treatments for Parkinson’s disease dementia (PDD), a condition linked to aggregation of... |
PMC5404495 | core_pubmed_pmc | A generic 89 Zr labeling method to quantify the in vivo pharmacokinetics of liposomal nanoparticles with positron emission tomography | A generic 89 Zr labeling method to quantify the in vivo pharmacokinetics of liposomal nanoparticles with positron emission tomography Abstract Abstract Liposomal nanoparticles are versatile drug delivery vehicles that show great promise in cancer therapy. In an effort to quantitatively measure their in vivo pharmacokin... |
PMC9006844 | core_pubmed_pmc | Dual checkpoint targeting of B7-H3 and PD-1 with enoblituzumab and pembrolizumab in advanced solid tumors: interim results from a multicenter phase I/II trial | Dual checkpoint targeting of B7-H3 and PD-1 with enoblituzumab and pembrolizumab in advanced solid tumors: interim results from a multicenter phase I/II trial Abstract Background Availability of checkpoint inhibitors has created a paradigm shift in the management of patients with solid tumors. Despite this, most patien... |
PMC11565514 | core_pubmed_pmc | Allele frequencies and genotype distribution of three metformin transporter polymorphisms in Mexican population and their application in pharmacogenomics of type 2 diabetes | Allele frequencies and genotype distribution of three metformin transporter polymorphisms in Mexican population and their application in pharmacogenomics of type 2 diabetes Abstract Abstract Background Metformin is the first-line antidiabetic therapy for type 2 diabetes in Mexico, despite recent recommendations highlig... |
PMC7772935 | core_pubmed_pmc | Plant-Derived Compounds as a Tool for the Control of Gastrointestinal Nematodes: Modulation of Abamectin Pharmacological Action by Carvone | Plant-Derived Compounds as a Tool for the Control of Gastrointestinal Nematodes: Modulation of Abamectin Pharmacological Action by Carvone Abstract Abstract The combination of synthetic anthelmintics and bioactive phytochemicals may be a pharmacological tool for improving nematode control in livestock. Carvone (R-CNE) ... |
PMC8604237 | core_pubmed_pmc | Population pharmacokinetics and exposure‐response analyses of teduglutide in adult and pediatric patients with short bowel syndrome | Population pharmacokinetics and exposure‐response analyses of teduglutide in adult and pediatric patients with short bowel syndrome Abstract Abstract Teduglutide is a recombinant analog of human glucagon‐like peptide‐2 that regulates the functional and structural integrity of the cells lining the gastrointestinal tract... |
PMC11489451 | core_pubmed_pmc | Canagliflozin Pharmacokinetics at Steady State in Patients on Maintenance Hemodialysis | Canagliflozin Pharmacokinetics at Steady State in Patients on Maintenance Hemodialysis Results Results We screened 17 eligible participants on maintenance hemodialysis. Ten patients agreed to participate and received 100 mg of canagliflozin for 9 days. Eight of these 10 patients agreed to participate in the second phas... |
PMC12199991 | core_pubmed_pmc | Pharmacokinetics of Orally Administered Phenazopyridine in Goats With Obstructive Urolithiasis | Pharmacokinetics of Orally Administered Phenazopyridine in Goats With Obstructive Urolithiasis Abstract ABSTRACT Background Phenazopyridine is used for ancillary pain management in the treatment of goats with obstructive urolithiasis. However, there are no published studies on the pharmacokinetics, safety, or efficacy ... |
PMC10975571 | core_pubmed_pmc | Pharmakokinetics of Mistletoe Lectins after Intravenous Application of a Mistletoe Product in Healthy Subjects | Pharmakokinetics of Mistletoe Lectins after Intravenous Application of a Mistletoe Product in Healthy Subjects Abstract Abstract Mistletoe lectins (ML) have cytotoxic and immunomodulating properties, and subcutaneously applied mistletoe products (MP) containing ML have approval for supportive cancer treatment. MP are a... |
PMC10672446 | core_pubmed_pmc | Screening of Phytochemical, Antimicrobial, and Antioxidant Properties of Juncus acutus from Northeastern Morocco | Screening of Phytochemical, Antimicrobial, and Antioxidant Properties of Juncus acutus from Northeastern Morocco Abstract Abstract Juncus acutus , acknowledged through its indigenous nomenclature “samar”, is part of the Juncaceae taxonomic lineage, bearing considerable import as a botanical reservoir harboring conceiva... |
PMC9693798 | core_pubmed_pmc | Liposomal amphotericin B—the past | Liposomal amphotericin B—the past Abstract Abstract The discovery of amphotericin B, a polyene antifungal compound, in the 1950s, and the formulation of this compound in a liposomal drug delivery system, has resulted in decades of use in systemic fungal infections. The use of liposomal amphotericin B formulation is ref... |
PMC3168911 | core_pubmed_pmc | Prescribing Medications in Patients with Decompensated Liver Cirrhosis | Prescribing Medications in Patients with Decompensated Liver Cirrhosis Abstract Abstract Patients with decompensated liver cirrhosis have various serious complications which require multiple drugs for therapeutic or prophylactic use. Majority of the drugs are primarily metabolized and excreted by hepatobiliary system; ... |
PMC4211672 | core_pubmed_pmc | A Multi-Compartment Single and Multiple Dose Pharmacokinetic Comparison of Rectally Applied Tenofovir 1% Gel and Oral Tenofovir Disoproxil Fumarate | A Multi-Compartment Single and Multiple Dose Pharmacokinetic Comparison of Rectally Applied Tenofovir 1% Gel and Oral Tenofovir Disoproxil Fumarate Abstract This Phase 1, randomized, two-site (United States), double-blind, placebo-controlled study enrolled 18 sexually abstinent men and women. All received a single 300-... |
PMC8800998 | core_pubmed_pmc | L-carnitine does not improve valproic acid poisoning management: a cohort study with toxicokinetics and concentration/effect relationships | L-carnitine does not improve valproic acid poisoning management: a cohort study with toxicokinetics and concentration/effect relationships Abstract Background Valproic acid (VPA) poisoning is responsible for life-threatening neurological and metabolic impairments. Despite only low-level evidence of effectiveness, L-car... |
PMC11191922 | core_pubmed_pmc | Ivosidenib in Chinese patients with relapsed or refractory isocitrate dehydrogenase 1 mutated acute myeloid leukemia: a registry study | Ivosidenib in Chinese patients with relapsed or refractory isocitrate dehydrogenase 1 mutated acute myeloid leukemia: a registry study Abstract Abstract Ivosidenib, an isocitrate dehydrogenase 1 ( IDH1 ) inhibitor, has demonstrated clinical benefits in a pivotal study (AG120-C-001) in patients with IDH1 -mutated (m IDH... |
PMC7188913 | core_pubmed_pmc | Precision Dosing Priority Criteria: Drug, Disease, and Patient Population Variables | Precision Dosing Priority Criteria: Drug, Disease, and Patient Population Variables Abstract The administered dose of a drug modulates whether patients will experience optimal effectiveness, toxicity including death, or no effect at all. Dosing is particularly important for diseases and/or drugs where the drug can decr... |
PMC9399017 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Lucitanib in Patients with Advanced Cancer | Population Pharmacokinetic Modeling of Lucitanib in Patients with Advanced Cancer Abstract Abstract Background Lucitanib is an oral, potent, selective inhibitor of the tyrosine kinase activity of vascular endothelial growth factor receptors 1‒3, fibroblast growth factor receptors 1‒3, and platelet-derived growth factor... |
PMC4629124 | core_pubmed_pmc | Pharmacokinetics of propafenone hydrochloride sustained-release capsules in male beagle dogs | Pharmacokinetics of propafenone hydrochloride sustained-release capsules in male beagle dogs Abstract Abstract This paper describes the development and validation of a liquid chromatography–mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propa... |
PMC12913765 | core_pubmed_pmc | LOAd703-induced tumor microenvironment gene engineering in combination with atezolizumab in metastatic malignant melanoma: a phase I/II trial | LOAd703-induced tumor microenvironment gene engineering in combination with atezolizumab in metastatic malignant melanoma: a phase I/II trial Abstract This phase I/II study evaluated the capacity of tumor microenvironment (TME) gene engineering by intratumoral injection of a viral vector encoding a designed CD40L and 4... |
PMC11845724 | core_pubmed_pmc | A preliminary exploration of liver microsomes and PBPK to uncover the impact of CYP3A4/5 and CYP2C19 on tacrolimus and voriconazole drug-drug interactions | A preliminary exploration of liver microsomes and PBPK to uncover the impact of CYP3A4/5 and CYP2C19 on tacrolimus and voriconazole drug-drug interactions Abstract Solid transplant recipients are at increased risk for invasive aspergillosis. Tacrolimus and Voriconazole is one of the most frequently utilized treatments ... |
PMC5303260 | core_pubmed_pmc | Efficacy, safety and pharmacokinetics of simeprevir and TMC647055/ritonavir with or without ribavirin and JNJ-56914845 in HCV genotype 1 infection | Efficacy, safety and pharmacokinetics of simeprevir and TMC647055/ritonavir with or without ribavirin and JNJ-56914845 in HCV genotype 1 infection Abstract Abstract Background A Phase 2a, open-label study ( NCT01724086 ) was conducted to assess the efficacy and safety of a once-daily, 2-direct-acting-antiviral-agent (2... |
PMC11054600 | core_pubmed_pmc | Comprehensive Therapeutic Approaches to Tuberculous Meningitis: Pharmacokinetics, Combined Dosing, and Advanced Intrathecal Therapies | Comprehensive Therapeutic Approaches to Tuberculous Meningitis: Pharmacokinetics, Combined Dosing, and Advanced Intrathecal Therapies Abstract Abstract Tuberculous meningitis (TBM) presents a critical neurologic emergency characterized by high mortality and morbidity rates, necessitating immediate therapeutic intervent... |
PMC6664151 | core_pubmed_pmc | Pharmacokinetics of hard micronized progesterone capsules via vaginal or oral route compared with soft micronized capsules in healthy postmenopausal women: a randomized open-label clinical study | Pharmacokinetics of hard micronized progesterone capsules via vaginal or oral route compared with soft micronized capsules in healthy postmenopausal women: a randomized open-label clinical study Abstract Purpose This study aimed to evaluate the pharmacokinetics of hard micronized progesterone capsules (Yimaxin) via the... |
PMC3123696 | core_pubmed_pmc | Efficacy and safety of motesanib, an oral inhibitor of VEGF, PDGF, and Kit receptors, in patients with imatinib-resistant gastrointestinal stromal tumors | Efficacy and safety of motesanib, an oral inhibitor of VEGF, PDGF, and Kit receptors, in patients with imatinib-resistant gastrointestinal stromal tumors Abstract Purpose This multicenter phase 2 study assessed the tolerability and efficacy of motesanib, an oral inhibitor of Kit, platelet-derived growth factor receptor... |
PMC5548886 | core_pubmed_pmc | A first‐in‐human phase I, multicenter, open‐label, dose‐escalation study of the oral RAF/VEGFR‐2 inhibitor (RAF265) in locally advanced or metastatic melanoma independent from BRAF mutation status | A first‐in‐human phase I, multicenter, open‐label, dose‐escalation study of the oral RAF/VEGFR‐2 inhibitor (RAF265) in locally advanced or metastatic melanoma independent from BRAF mutation status Abstract Abstract To establish the maximum tolerated dose ( MTD ), dose‐limiting toxicities ( DLT ), safety profile, and an... |
PMC7167374 | core_pubmed_pmc | A precision medicine framework using artificial intelligence for the identification and confirmation of genomic biomarkers of response to an Alzheimer's disease therapy: Analysis of the blarcamesine (ANAVEX2‐73) Phase 2a clinical study | A precision medicine framework using artificial intelligence for the identification and confirmation of genomic biomarkers of response to an Alzheimer's disease therapy: Analysis of the blarcamesine (ANAVEX2‐73) Phase 2a clinical study Abstract Abstract Introduction The search for drugs to treat Alzheimer's disease (AD... |
PMC7098963 | core_pubmed_pmc | Pharmacophore-Based Virtual Screening Toward the Discovery of Novel Anti-echinococcal Compounds | Pharmacophore-Based Virtual Screening Toward the Discovery of Novel Anti-echinococcal Compounds Abstract Abstract Echinococcosis is a serious helminthic zoonosis with a great impact on human health and livestock husbandry. However, the clinically used drugs (benzimidazoles) have a low cure rate, so alternative drugs ar... |
PMC11247113 | core_pubmed_pmc | Population pharmacokinetics of adebrelimab – Support of alternative flat dose regimen in extensive‐stage small‐cell lung cancer | Population pharmacokinetics of adebrelimab – Support of alternative flat dose regimen in extensive‐stage small‐cell lung cancer Abstract Abstract Adebrelimab, a novel anti‐PD‐L1 antibody, has been approved by the National Medical Products Administration of China as an intravenous infusion for use in combination with ca... |
PMC9223854 | core_pubmed_pmc | Proteolysis Targeting Chimeric Molecules: Tuning Molecular Strategies for a Clinically Sound Listening | Proteolysis Targeting Chimeric Molecules: Tuning Molecular Strategies for a Clinically Sound Listening Abstract From seminal evidence in the early 2000s, the opportunity to drive the specific knockdown of a protein of interest (POI) through pharmacological entities called Proteolysis Targeting Chimeric molecules, or PR... |
PMC6923423 | core_pubmed_pmc | Influence of OATP1B1 and BCRP polymorphisms on the pharmacokinetics and pharmacodynamics of rosuvastatin in elderly and young Korean subjects | Influence of OATP1B1 and BCRP polymorphisms on the pharmacokinetics and pharmacodynamics of rosuvastatin in elderly and young Korean subjects Abstract Abstract A lack of information regarding whether genetic polymorphisms of SLCO1B1 and ABCG 2 affect the pharmacokinetics (PKs)/pharmacodynamics (PDs) of rosuvastatin in ... |
PMC8620410 | core_pubmed_pmc | Pseudomonas aeruginosa Susceptibility in Spain: Antimicrobial Activity and Resistance Suppression Evaluation by PK/PD Analysis | Pseudomonas aeruginosa Susceptibility in Spain: Antimicrobial Activity and Resistance Suppression Evaluation by PK/PD Analysis Abstract Pseudomonas aeruginosa remains one of the major causes of healthcare-associated infection in Europe; in 2019, 12.5% of invasive isolates of P. aeruginosa in Spain presented combined re... |
PMC11812195 | core_pubmed_pmc | A phase 2 randomized, double-blind trial of ART-001, a selective PI3Kα inhibitor, for the treatment of slow-flow vascular malformations | A phase 2 randomized, double-blind trial of ART-001, a selective PI3Kα inhibitor, for the treatment of slow-flow vascular malformations Abstract Background In patients with slow-flow vascular malformations (SFVMs) including venous malformations (VM), lymphatic malformations (LM) or Klippel–Trenaunay Syndrome (KTS), som... |
PMC12356974 | core_pubmed_pmc | GX-I7, a long-acting IL-7, safely and effectively increased peripheral CD8 + /CD4 + T cells and TILs in patients with locally advanced or metastatic solid tumours | GX-I7, a long-acting IL-7, safely and effectively increased peripheral CD8 + /CD4 + T cells and TILs in patients with locally advanced or metastatic solid tumours Abstract Background GX-I7 (rhIL-7-hyFc, efineptakin alfa) is a hybrid Fc-fused long-acting interleukin-7 (IL-7) with the aim of correcting T-cell deficiency,... |
PMC6533572 | core_pubmed_pmc | Elucidation of the Differences in Cinobufotalin’s Pharmacokinetics Between Normal and Diethylnitrosamine-Injured Rats: The Role of P-Glycoprotein | Elucidation of the Differences in Cinobufotalin’s Pharmacokinetics Between Normal and Diethylnitrosamine-Injured Rats: The Role of P-Glycoprotein Abstract Cinobufotalin is one of the major anti-tumor components isolated from toad venom and has been used in the clinical therapy of hepatocellular carcinoma (HCC), known a... |
PMC3513969 | core_pubmed_pmc | Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin | Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin Abstract Abstract Red yeast rice (RYR) can reduce cholesterol through its active component, lovastatin. This study was to investigate the pharmacokinetic properties of lovastatin in R... |
PMC6827426 | core_pubmed_pmc | Influence of Charge, Hydrophobicity, and Size on Vitreous Pharmacokinetics of Large Molecules | Influence of Charge, Hydrophobicity, and Size on Vitreous Pharmacokinetics of Large Molecules Abstract Abstract Purpose Development of therapeutics for retinal disease with improved durability is hampered by inadequate understanding of pharmacokinetic (PK) drivers following intravitreal injection. Previous work shows t... |
PMC5071622 | core_pubmed_pmc | Pharmacokinetics of H002, a novel S1PR 1 modulator, and its metabolites in rat blood using liquid chromatography–tandem mass spectrometry | Pharmacokinetics of H002, a novel S1PR 1 modulator, and its metabolites in rat blood using liquid chromatography–tandem mass spectrometry Abstract A rapid and sensitive liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed and validated for the simultaneous determination of H002 and its phospho... |
PMC5024096 | core_pubmed_pmc | Focused Ultrasound-Induced Blood-Brain Barrier Opening: Association with Mechanical Index and Cavitation Index Analyzed by Dynamic Contrast-Enhanced Magnetic-Resonance Imaging | Focused Ultrasound-Induced Blood-Brain Barrier Opening: Association with Mechanical Index and Cavitation Index Analyzed by Dynamic Contrast-Enhanced Magnetic-Resonance Imaging Abstract Focused ultrasound (FUS) with microbubbles can temporally open the blood-brain barrier (BBB), and the cavitation activities of microbub... |
PMC7079113 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic bioequivalence of proposed biosimilar MYL‐1501D with US and European insulin glargine formulations in patients with type 1 diabetes mellitus | Pharmacokinetic and pharmacodynamic bioequivalence of proposed biosimilar MYL‐1501D with US and European insulin glargine formulations in patients with type 1 diabetes mellitus Abstract Abstract Aims To report phase 1 bioequivalence results comparing MYL‐1501D, US reference insulin glargine (US IG), and European refere... |
PMC12125420 | core_pubmed_pmc | Yinling Qushi Granule as a therapeutic agent for metabolic syndrome: pharmacological, molecular targets, and pharmacokinetic insights | Yinling Qushi Granule as a therapeutic agent for metabolic syndrome: pharmacological, molecular targets, and pharmacokinetic insights Abstract Metabolic Syndrome (MetS) is a globally prevalent condition with unclear underlying mechanisms. Current treatments primarily focus on alleviating individual symptoms, lacking lo... |
PMC9661317 | core_pubmed_pmc | Comparison of Steady-State Pharmacokinetics of Donepezil Transdermal Delivery System with Oral Donepezil | Comparison of Steady-State Pharmacokinetics of Donepezil Transdermal Delivery System with Oral Donepezil Abstract Abstract Background: Donepezil is approved for treatment of dementia of the Alzheimer type and is currently available only in tablet forms in the United States. Objective: To compare steady-state pharmacoki... |
PMC10717981 | core_pubmed_pmc | Development and characterization of NILK-2301, a novel CEACAM5xCD3 κλ bispecific antibody for immunotherapy of CEACAM5-expressing cancers | Development and characterization of NILK-2301, a novel CEACAM5xCD3 κλ bispecific antibody for immunotherapy of CEACAM5-expressing cancers Abstract Background T-cell retargeting to eliminate CEACAM5-expressing cancer cells via CEACAM5xCD3 bispecific antibodies (BsAbs) showed limited clinical activity so far, mostly due ... |
PMC4280029 | core_pubmed_pmc | LC–MS/MS determination and pharmacokinetic study of columbianadin in rat plasma after intravenous administration of pure columbianadin | LC–MS/MS determination and pharmacokinetic study of columbianadin in rat plasma after intravenous administration of pure columbianadin Abstract Background Columbianadin, one of the active coumarins, is isolated from Radix Angelicae pubescentis which has been used as a traditional Chinese medicine for the treatment of r... |
PMC5797931 | core_pubmed_pmc | Population Pharmacokinetic Modeling of a Desmopressin Oral Lyophilisate in Growing Piglets as a Model for the Pediatric Population | Population Pharmacokinetic Modeling of a Desmopressin Oral Lyophilisate in Growing Piglets as a Model for the Pediatric Population Abstract Abstract Desmopressin is used to treat primary nocturnal enuresis in children. Over the years, various formulations of desmopressin were commercialized of which the sublingual melt... |
PMC11677527 | core_pubmed_pmc | Predicting Pharmacokinetics of Active Constituents in Spatholobi caulis by Using Physiologically Based Pharmacokinetic Models | Predicting Pharmacokinetics of Active Constituents in Spatholobi caulis by Using Physiologically Based Pharmacokinetic Models Abstract Background/Objectives: Spatholobi Caulis (SPC) is a medicinal plant that mainly grows in China and Southeast Asian countries and commonly used in clinics; the pharmacokinetic characteri... |
PMC6585621 | core_pubmed_pmc | Clopidogrel Increases Dasabuvir Exposure With or Without Ritonavir, and Ritonavir Inhibits the Bioactivation of Clopidogrel | Clopidogrel Increases Dasabuvir Exposure With or Without Ritonavir, and Ritonavir Inhibits the Bioactivation of Clopidogrel Abstract Dasabuvir is mainly metabolized by cytochrome P450 (CYP) 2C8 and is predominantly used in a regimen containing ritonavir. Ritonavir and clopidogrel are inhibitors of CYP3A4 and CYP2C8, re... |
PMC12415939 | core_pubmed_pmc | Penicillin and Gentamicin Concentrations in the Uterine Fluid of Non‐Pregnant Mares Following a Single Intrauterine Infusion | Penicillin and Gentamicin Concentrations in the Uterine Fluid of Non‐Pregnant Mares Following a Single Intrauterine Infusion Abstract ABSTRACT Despite their widespread clinical use, there is limited pharmacokinetic data for many equine intrauterine antimicrobials. This study aimed to measure the concentration of gentam... |
PMC8804354 | core_pubmed_pmc | Population Pharmacokinetic Modeling and Simulation of TQ-B3101 to Inform Dosing in Pediatric Patients With Solid Tumors | Population Pharmacokinetic Modeling and Simulation of TQ-B3101 to Inform Dosing in Pediatric Patients With Solid Tumors Abstract Abstract Background: TQ-B3101 is a novel kinase inhibitor currently in development for the treatment of advanced malignant solid tumor and relapsed or refractory ALK-positive anaplastic large... |
PMC4755745 | core_pubmed_pmc | Bidirectional interactions between indomethacin and the murine intestinal microbiota | Bidirectional interactions between indomethacin and the murine intestinal microbiota Abstract The vertebrate gut microbiota have been implicated in the metabolism of xenobiotic compounds, motivating studies of microbe-driven metabolism of clinically important drugs. Here, we studied interactions between the microbiota ... |
PMC7076457 | core_pubmed_pmc | Species Differences in Stereoselective Pharmacokinetics of HSG4112, A New Anti-Obesity Agent | Species Differences in Stereoselective Pharmacokinetics of HSG4112, A New Anti-Obesity Agent Abstract HSG4112, a racemic drug, is a new anti-obesity agent. In this study, the stereoselective pharmacokinetics of HSG4112 were investigated in rats and dogs, and the underlying mechanism was investigated. The plasma concent... |
PMC8861296 | core_pubmed_pmc | AI Models to Assist Vancomycin Dosage Titration | AI Models to Assist Vancomycin Dosage Titration Abstract Abstract Background: Effective treatment using antibiotic vancomycin requires close monitoring of serum drug levels due to its narrow therapeutic index. In the current practice, physicians use various dosing algorithms for dosage titration, but these algorithms r... |
PMC8585037 | core_pubmed_pmc | Comparative Neuropharmacology and Pharmacokinetics of Methamphetamine and Its Thiophene Analog Methiopropamine in Rodents | Comparative Neuropharmacology and Pharmacokinetics of Methamphetamine and Its Thiophene Analog Methiopropamine in Rodents Abstract Methiopropamine is a novel psychoactive substance (NPS) that is associated with several cases of clinical toxicity, yet little information is available regarding its neuropharmacological pr... |
PMC6385179 | core_pubmed_pmc | Changes in microbiome diversity following beta-lactam antibiotic treatment are associated with therapeutic versus subtherapeutic antibiotic exposure in cystic fibrosis | Changes in microbiome diversity following beta-lactam antibiotic treatment are associated with therapeutic versus subtherapeutic antibiotic exposure in cystic fibrosis Abstract Abstract In persons with cystic fibrosis (CF), decreased airway microbial diversity is associated with lower lung function. Conflicting data ex... |
PMC9211078 | core_pubmed_pmc | Population Pharmacokinetics of Tigecycline: A Systematic Review | Population Pharmacokinetics of Tigecycline: A Systematic Review Abstract Abstract Although tigecycline is widely used in clinical practice, its efficiency and optimal dosage regimens remain controversial. The purpose of this article was to help guide tigecycline dosing in different patient subpopulations through compar... |
PMC10771435 | core_pubmed_pmc | Minimally sufficient experimental design using identifiability analysis | Minimally sufficient experimental design using identifiability analysis Abstract Abstract Mathematical models are increasingly being developed and calibrated in tandem with data collection, empowering scientists to intervene in real time based on quantitative model predictions. Well-designed experiments can help augmen... |
PMC6682562 | core_pubmed_pmc | Safety and Tolerability of Adjunctive Brivaracetam in Pediatric Patients < 16 Years with Epilepsy: An Open-Label Trial | Safety and Tolerability of Adjunctive Brivaracetam in Pediatric Patients < 16 Years with Epilepsy: An Open-Label Trial Abstract Objective This trial evaluated the short-term safety and tolerability, steady-state pharmacokinetics, and preliminary efficacy of brivaracetam oral solution in children aged 1 month to < 16 ye... |
PMC8876868 | core_pubmed_pmc | Diurnal Variability of Platelet Aggregation in Patients with Myocardial Infarction Treated with Prasugrel and Ticagrelor | Diurnal Variability of Platelet Aggregation in Patients with Myocardial Infarction Treated with Prasugrel and Ticagrelor Abstract Background: Contemporary antiplatelet treatment in acute myocardial infarction (AMI) is based on one of two P2Y12 receptor inhibitors, prasugrel or ticagrelor. The aim of this study was to c... |
PMC8880729 | core_pubmed_pmc | Anti-Diabetic Activity of Bioactive Compound Extracted from Spondias mangifera Fruit: In-Vitro and Molecular Docking Approaches | Anti-Diabetic Activity of Bioactive Compound Extracted from Spondias mangifera Fruit: In-Vitro and Molecular Docking Approaches Abstract Spondias mangifera is a drupaceous fruit popular for its flavour and health advantages. There is little scientific knowledge about S. mangifera , despite its widespread usage in tradi... |
PMC4628089 | core_pubmed_pmc | The Pharmacokinetics of the CYP3A Substrate Midazolam in Morbidly Obese Patients Before and One Year After Bariatric Surgery | The Pharmacokinetics of the CYP3A Substrate Midazolam in Morbidly Obese Patients Before and One Year After Bariatric Surgery Abstract Purpose Bariatric surgery is nowadays commonly applied as treatment for morbid obesity (BMI > 40 kg/m 2 ). As information about the effects of this procedure on a drug’s pharmacokinetics... |
PMC11115456 | core_pubmed_pmc | Infection and Prophylaxis During Normothermic Liver Perfusion: Audit of Incidence and Pharmacokinetics of Antimicrobial Therapy | Infection and Prophylaxis During Normothermic Liver Perfusion: Audit of Incidence and Pharmacokinetics of Antimicrobial Therapy Abstract Abstract Background. Ex situ normothermic liver perfusion (NMP) in a blood-based perfusate is associated with a risk of microbe growth, resulting in life-threatening posttransplant se... |
PMC6114101 | core_pubmed_pmc | Safety and efficacy of the bumped kinase inhibitor BKI-1553 in pregnant sheep experimentally infected with Neospora caninum tachyzoites | Safety and efficacy of the bumped kinase inhibitor BKI-1553 in pregnant sheep experimentally infected with Neospora caninum tachyzoites Abstract Abstract Neospora caninum is one of the main causes of abortion in cattle, and recent studies have highlighted its relevance as an abortifacient in small ruminants. Vaccines o... |
PMC11364066 | core_pubmed_pmc | IL-2-armored peptide-major histocompatibility class I bispecific antibodies redirect antiviral effector memory CD8+ T cells to induce potent anti-cancer cytotoxic activity with limited cytokine release | IL-2-armored peptide-major histocompatibility class I bispecific antibodies redirect antiviral effector memory CD8+ T cells to induce potent anti-cancer cytotoxic activity with limited cytokine release Abstract ABSTRACT T cell engagers (TCEs) are becoming an integral class of biological therapeutic owing to their highl... |
PMC6930491 | core_pubmed_pmc | Electrophysiology and Behavioral Assessment of the New Molecule SMe1EC2M3 as a Representative of the Future Class of Triple Reuptake Inhibitors | Electrophysiology and Behavioral Assessment of the New Molecule SMe1EC2M3 as a Representative of the Future Class of Triple Reuptake Inhibitors Abstract SMe1EC2M3 is a pyridoindole derivative related to the neuroleptic drug carbidine. Based on the structural similarities of SMe1EC2M3 and known serotonin (5-HT), norepin... |
PMC7271942 | core_pubmed_pmc | A Randomized Trial of Modified-Release Versus Immediate-Release Tolvaptan in ADPKD | A Randomized Trial of Modified-Release Versus Immediate-Release Tolvaptan in ADPKD Abstract Introduction Tolvaptan, for treatment of autosomal dominant polycystic kidney disease (ADPKD), is provided as immediate-release (IR) tablets administered twice daily in split-dose regimens to suppress urine osmolality to <300 mO... |
PMC3627016 | core_pubmed_pmc | Pharmacokinetics of Coadministration of Guanfacine Extended Release and Methylphenidate Extended Release | Pharmacokinetics of Coadministration of Guanfacine Extended Release and Methylphenidate Extended Release Abstract Abstract Background α 2 -Adrenoceptor agonists are used adjunctively to psychostimulants in treating attention-deficit/hyperactivity disorder (ADHD) when psychostimulants alone do not sufficiently reduce sy... |
PMC12709922 | core_pubmed_pmc | Physiologically based pharmacokinetic (PBPK) modeling of drug-drug interactions between suraxavir marboxil and CYP3A4 inhibitors: Quantitative prediction of pharmacokinetic effects on active metabolite GP1707D07 | Physiologically based pharmacokinetic (PBPK) modeling of drug-drug interactions between suraxavir marboxil and CYP3A4 inhibitors: Quantitative prediction of pharmacokinetic effects on active metabolite GP1707D07 Abstract Abstract Suraxavir marboxil (GP681) is a promising novel prodrug influenza polymerase acidic (PA) i... |
PMC11783638 | core_pubmed_pmc | Different behaviour of target-controlled infusion pumps despite apparently using the same Schnider pharmacokinetic model | Different behaviour of target-controlled infusion pumps despite apparently using the same Schnider pharmacokinetic model Abstract Abstract BACKGROUND Target-controlled infusion (TCI) pumps deliver an initial bolus of drug to achieve a preset drug target concentration quickly. OBJECTIVE We investigated whether differenc... |
PMC5519571 | core_pubmed_pmc | Sex-Divergent Clinical Outcomes and Precision Medicine: An Important New Role for Institutional Review Boards and Research Ethics Committees | Sex-Divergent Clinical Outcomes and Precision Medicine: An Important New Role for Institutional Review Boards and Research Ethics Committees Abstract Abstract The efforts toward individualized medicine have constantly increased in an attempt to improve treatment options. These efforts have led to the development of sma... |
PMC9235074 | core_pubmed_pmc | Empirical treatment against cytomegalovirus and tuberculosis in HIV-infected infants with severe pneumonia: study protocol for a multicenter, open-label randomized controlled clinical trial | Empirical treatment against cytomegalovirus and tuberculosis in HIV-infected infants with severe pneumonia: study protocol for a multicenter, open-label randomized controlled clinical trial Abstract Background Pneumonia is the primary cause of death among HIV-infected children in Africa, with mortality rates as high as... |
PMC3686537 | core_pubmed_pmc | PEGylated interferon beta-1a in the treatment of multiple sclerosis – an update | PEGylated interferon beta-1a in the treatment of multiple sclerosis – an update Abstract Current standard immunomodulatory therapy with interferons (IFNs) for relapsing–remitting multiple sclerosis (MS) exhibits proven, but limited, efficacy and increased side effects due to the need of frequent application of the drug... |
PMC11230209 | core_pubmed_pmc | RNAi-mediated silencing of SOD1 profoundly extends survival and functional outcomes in ALS mice | RNAi-mediated silencing of SOD1 profoundly extends survival and functional outcomes in ALS mice Abstract Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative condition, with 20% of familial and 2–3% of sporadic cases linked to mutations in the cytosolic superoxide dismutase (SOD1) gene. Mutant SOD1 protein ... |
PMC5718430 | core_pubmed_pmc | An open-label, non-randomized study of the pharmacokinetics of the nutritional supplement nicotinamide riboside (NR) and its effects on blood NAD+ levels in healthy volunteers | An open-label, non-randomized study of the pharmacokinetics of the nutritional supplement nicotinamide riboside (NR) and its effects on blood NAD+ levels in healthy volunteers Abstract Objectives The co-primary objectives of this study were to determine the human pharmacokinetics (PK) of oral NR and the effect of NR on... |
PMC9658985 | core_pubmed_pmc | Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats | Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats Abstract Meloxicam (MLX) is currently used in the therapeutic management of both acute and chronic inflammatory disorders such as pain, injuries, osteoarthritis, and... |
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