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PMC12130796 | core_pubmed_pmc | A Phase I Study of Nilotinib in Combination with Paclitaxel in Patients with Advanced Solid Tumors | A Phase I Study of Nilotinib in Combination with Paclitaxel in Patients with Advanced Solid Tumors Abstract Abstract Purpose: We assessed the safety, maximum tolerated dose, and recommended phase 2 dose (RP2D), efficacy, pharmacokinetics, and pharmacodynamics of the nilotinib–paclitaxel combination in 44 patients with ... |
PMC5754937 | core_pubmed_pmc | Investigation of in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetics of paromomycin: Influence on oral bioavailability | Investigation of in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetics of paromomycin: Influence on oral bioavailability Abstract Abstract OBJECTIVE: The objective of this study is to investigate in vitro Caco2 permeability, metabolism and in vivo pharmacokinetic (PK) properties of p... |
PMC9556364 | core_pubmed_pmc | The effect of rifampin on the pharmacokinetics of famitinib in healthy subjects | The effect of rifampin on the pharmacokinetics of famitinib in healthy subjects Abstract Abstract Background Famitinib is an oral, small-molecule, multi-targeted tyrosine kinase inhibitor under clinical investigation for the treatment of solid tumors. As famitinib is metabolized mainly by cytochrome P450 3A4 (CYP3A4), ... |
PMC8452731 | core_pubmed_pmc | Flow cytometry method for absolute counting and single-cell phenotyping of mycobacteria | Flow cytometry method for absolute counting and single-cell phenotyping of mycobacteria Abstract Abstract Detection and accurate quantitation of viable Mycobacterium tuberculosis is fundamental to understanding mycobacterial pathogenicity, tuberculosis (TB) disease progression and outcomes; TB transmission; drug action... |
PMC10619024 | core_pubmed_pmc | Longitudinal evaluation of the biodistribution and cellular internalization of the bispecific CD3xTRP1 antibody in syngeneic mouse tumor models | Longitudinal evaluation of the biodistribution and cellular internalization of the bispecific CD3xTRP1 antibody in syngeneic mouse tumor models Abstract Background CD3 bispecific antibodies (CD3-bsAbs) require binding of both a tumor-associated surface antigen and CD3 for their immunotherapeutic effect. Their efficacy ... |
PMC4020540 | core_pubmed_pmc | Hyperammonemia Associated with Valproic Acid Concentrations | Hyperammonemia Associated with Valproic Acid Concentrations Abstract Valproic acid, a branched short-chain fatty acid, has numerous action mechanisms which turn it into a broad spectrum anticonvulsant drug and make its use possible in some other pathologies such as bipolar disorder. It is extensively metabolized in liv... |
PMC12272314 | core_pubmed_pmc | Impact of Model‐Informed Drug Development on Drug Development Cycle Times and Clinical Trial Cost | Impact of Model‐Informed Drug Development on Drug Development Cycle Times and Clinical Trial Cost Abstract Abstract Model‐informed drug development (MIDD) integrates data to quantify benefit/risk informing objective drug discovery and development decisions. An additional critical benefit of MIDD is postulated to be imp... |
PMC3436077 | core_pubmed_pmc | The influence of active transport systems on morphine -6-glucuronide transport in MDCKII and MDCK-PGP cells | The influence of active transport systems on morphine -6-glucuronide transport in MDCKII and MDCK-PGP cells Abstract Abstract Background and the purpose of the study Morphine-6-glucuronide (M6G) is a potent metabolite of morphine which has high penetration into the brain despite its high polarity, which could be the re... |
PMC8268181 | core_pubmed_pmc | Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits | Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits Abstract Objective Malaria is a major global health concern with the urgent need for new treatment alternatives due to the alarming increase of drug-resistant Plasmodium strains. Chalcones and its derivatives are ... |
PMC10431048 | core_pubmed_pmc | Population pharmacokinetic analysis of sparsentan in healthy volunteers and patients with focal segmental glomerulosclerosis | Population pharmacokinetic analysis of sparsentan in healthy volunteers and patients with focal segmental glomerulosclerosis Abstract Abstract Sparsentan is a single‐molecule dual endothelin angiotensin receptor antagonist (DEARA) currently under investigation as a treatment for focal segmental glomerulosclerosis (FSGS... |
PMC10800975 | core_pubmed_pmc | Anti-seizure effects of JNJ-54175446 in the intra-amygdala kainic acid model of drug-resistant temporal lobe epilepsy in mice | Anti-seizure effects of JNJ-54175446 in the intra-amygdala kainic acid model of drug-resistant temporal lobe epilepsy in mice Abstract Abstract There remains a need for new drug targets for treatment-resistant temporal lobe epilepsy. The ATP-gated P2X7 receptor coordinates neuroinflammatory responses to tissue injury. ... |
PMC5310137 | core_pubmed_pmc | Development and validation of bioanalytical UHPLC-UV method for simultaneous analysis of unchanged fenofibrate and its metabolite fenofibric acid in rat plasma: Application to pharmacokinetics | Development and validation of bioanalytical UHPLC-UV method for simultaneous analysis of unchanged fenofibrate and its metabolite fenofibric acid in rat plasma: Application to pharmacokinetics Abstract Abstract A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been... |
PMC12944386 | core_pubmed_pmc | Cyclodextrin Polymer Complexation Improves the Tolerability of Parenteral Oestradiol | Cyclodextrin Polymer Complexation Improves the Tolerability of Parenteral Oestradiol Abstract Abstract Background : Menopause is characterised by a decline in oestrogen levels, leading to physical and psychological symptoms that significantly affect quality of life. Current parenteral oestradiol ester therapies, while ... |
PMC10583239 | core_pubmed_pmc | A comprehensive evaluation in clinic and physiologically‐based pharmacokinetic modeling and simulation to confirm lack of cytochrome P450–mediated drug–drug interaction potential for pomotrelvir | A comprehensive evaluation in clinic and physiologically‐based pharmacokinetic modeling and simulation to confirm lack of cytochrome P450–mediated drug–drug interaction potential for pomotrelvir Abstract Abstract Pomotrelvir is a new chemical entity and potent direct‐acting antiviral inhibitor of the main protease of c... |
PMC11905873 | core_pubmed_pmc | Bioavailability, Metabolism, and Excretion of [ 14 C]‐Tazemetostat in Patients With B‐Cell Lymphomas or Advanced Solid Tumors | Bioavailability, Metabolism, and Excretion of [ 14 C]‐Tazemetostat in Patients With B‐Cell Lymphomas or Advanced Solid Tumors Abstract Abstract This open‐label, multicenter study ( NCT03010982 ) evaluated the absolute bioavailability, characterized the disposition and metabolism, and investigated the metabolic profile ... |
PMC9544063 | core_pubmed_pmc | A phase 1 study to evaluate the safety, tolerability and pharmacokinetics of TAK‐041 in healthy participants and patients with stable schizophrenia | A phase 1 study to evaluate the safety, tolerability and pharmacokinetics of TAK‐041 in healthy participants and patients with stable schizophrenia Abstract Abstract Aims TAK‐041 (NBI‐1065846), an orally available, investigational, small molecule agonist of GPR139, an orphan G‐protein‐coupled receptor, has shown promis... |
PMC10832602 | core_pubmed_pmc | Target attainment of intravenous lefamulin for treatment of acute bacterial skin and skin structure infections | Target attainment of intravenous lefamulin for treatment of acute bacterial skin and skin structure infections Abstract Abstract Objectives Lefamulin is a pleuromutilin antibiotic approved for the treatment of community-acquired bacterial pneumonia (CABP). Its spectrum of activity, good penetration into soft tissues an... |
PMC5032877 | core_pubmed_pmc | Posaconazole Pharmacokinetics in Healthy Cats after Oral and Intravenous Administration | Posaconazole Pharmacokinetics in Healthy Cats after Oral and Intravenous Administration Abstract Background Posaconazole is the most active available azole antifungal drug, but absorption and pharmacokinetics are not available to guide dosing regimens in cats. Objective To determine the pharmacokinetics of posaconazole... |
PMC9065259 | core_pubmed_pmc | Susceptibility to Adrenal Crisis Is Associated With Differences in Cortisol Excretion in Patients With Secondary Adrenal Insufficiency | Susceptibility to Adrenal Crisis Is Associated With Differences in Cortisol Excretion in Patients With Secondary Adrenal Insufficiency Abstract Objective To compare cortisol pharmacokinetics and pharmacodynamics mapped through several glucocorticoid sensitive pathways in patients on hydrocortisone substitution with or ... |
PMC7529626 | core_pubmed_pmc | A Pharmacokinetic Study of Methylphenidate Hydrochloride Multilayer Extended-Release Capsules (Aptensio XR ® ) in Preschool-Aged Children with Attention-Deficit/Hyperactivity Disorder | A Pharmacokinetic Study of Methylphenidate Hydrochloride Multilayer Extended-Release Capsules (Aptensio XR ® ) in Preschool-Aged Children with Attention-Deficit/Hyperactivity Disorder Abstract Objective This was a single-dose, one-period, multicenter, pharmacokinetic (PK) study to evaluate the PK of methylphenidate (MP... |
PMC11638672 | core_pubmed_pmc | A loading dose of clofazimine to rapidly achieve steady-state-like concentrations in patients with nontuberculous mycobacterial disease | A loading dose of clofazimine to rapidly achieve steady-state-like concentrations in patients with nontuberculous mycobacterial disease Abstract Abstract Objectives Clofazimine is a promising drug for the treatment of nontuberculous mycobacterial (NTM) diseases. Accumulation of clofazimine to reach steady-state plasma ... |
PMC12678924 | core_pubmed_pmc | Gepants: targeting the CGRP pathway for migraine relief | Gepants: targeting the CGRP pathway for migraine relief Abstract Background Calcitonin gene–related peptide (CGRP) receptor antagonist (collectively known as gepant) have emerged as effective therapies for both acute migraine treatment and preventive management. Several new agents (atogepant, ubrogepant, rimegepant, an... |
PMC11578123 | core_pubmed_pmc | Pharmacometrics in obstetrics and maternal–fetal medicine research: Bridging gaps in maternal and fetal pharmacology | Pharmacometrics in obstetrics and maternal–fetal medicine research: Bridging gaps in maternal and fetal pharmacology Modeling MATERNAL AND FETAL PBPK MODELS Maternal PBPK models have evolved significantly to describe gestational‐dependent changes across trimesters, enhancing our understanding of how predicted maternal ... |
PMC6893510 | core_pubmed_pmc | Towards Therapeutic Alternatives for Mercury Neurotoxicity in the Amazon: Unraveling the Pre-Clinical Effects of the Superfruit Açaí ( Euterpe oleracea , Mart.) as Juice for Human Consumption | Towards Therapeutic Alternatives for Mercury Neurotoxicity in the Amazon: Unraveling the Pre-Clinical Effects of the Superfruit Açaí ( Euterpe oleracea , Mart.) as Juice for Human Consumption Abstract Abstract Methylmercury (MeHg) exposure is a serious problem of public health, especially in the Amazon. Exposure in riv... |
PMC6389346 | core_pubmed_pmc | Blood‐Based Biomarkers of Quinpirole Pharmacology: Cluster‐Based PK / PD and Metabolomics to Unravel the Underlying Dynamics in Rat Plasma and Brain | Blood‐Based Biomarkers of Quinpirole Pharmacology: Cluster‐Based PK / PD and Metabolomics to Unravel the Underlying Dynamics in Rat Plasma and Brain Abstract Abstract A key challenge in the development of central nervous system drugs is the availability of drug target specific blood‐based biomarkers. As a new approach,... |
PMC5024008 | core_pubmed_pmc | Pharmacokinetics and Dose Recommendations for Cyclosporine and Tacrolimus When Coadministered With ABT‐450, Ombitasvir, and Dasabuvir | Pharmacokinetics and Dose Recommendations for Cyclosporine and Tacrolimus When Coadministered With ABT‐450, Ombitasvir, and Dasabuvir Abstract Short abstract The authors describe the drug–drug interaction profile of the he patitis C direct‐acting antiviral agents ABT‐450, ombitasvir, and dasabuvir with cyclosporine A a... |
PMC10515777 | core_pubmed_pmc | Structure-based discovery of CFTR potentiators and inhibitors | Structure-based discovery of CFTR potentiators and inhibitors Abstract The cystic fibrosis transmembrane conductance regulator (CFTR) is a crucial ion channel whose loss of function leads to cystic fibrosis, while its hyperactivation leads to secretory diarrhea. Small molecules that improve CFTR folding (correctors) or... |
PMC8636098 | core_pubmed_pmc | Predicting New Anti-Norovirus Inhibitor With the Help of Machine Learning Algorithms and Molecular Dynamics Simulation–Based Model | Predicting New Anti-Norovirus Inhibitor With the Help of Machine Learning Algorithms and Molecular Dynamics Simulation–Based Model Abstract Hepatitis C virus (HCV) inhibitors are essential in the treatment of human norovirus (HuNoV). This study aimed to map out HCV NS5B RNA-dependent RNA polymerase inhibitors that coul... |
PMC10514301 | core_pubmed_pmc | A viral RNA-dependent RNA polymerase inhibitor VV116 broadly inhibits human coronaviruses and has synergistic potency with 3CLpro inhibitor nirmatrelvir | A viral RNA-dependent RNA polymerase inhibitor VV116 broadly inhibits human coronaviruses and has synergistic potency with 3CLpro inhibitor nirmatrelvir Abstract During the ongoing pandemic, providing treatment consisting of effective, low-cost oral antiviral drugs at an early stage of SARS-CoV-2 infection has been a p... |
PMC10013357 | core_pubmed_pmc | Lack of pharmacokinetic interaction between derazantinib and naringin in rats | Lack of pharmacokinetic interaction between derazantinib and naringin in rats Abstract Abstract Context Derazantinib—an orally bioavailable, ATP competitive, multikinase inhibitor—has strong activity against fibroblast growth factor receptors (FGFR)2, FGFR1, and FGFR3 kinases. It has preliminary antitumor activity in p... |
PMC10209927 | core_pubmed_pmc | Mechanochemical Synthesis of Thiazolidinone-Triazoles Derivatives as Antidiabetic Agents: Pharmacokinetics, Molecular Docking, and In Vitro Antidiabetic Properties | Mechanochemical Synthesis of Thiazolidinone-Triazoles Derivatives as Antidiabetic Agents: Pharmacokinetics, Molecular Docking, and In Vitro Antidiabetic Properties Abstract Abstract Mechanochemistry is an eco-friendly and solventless method. In the present study, the surface of a custom-made closed mortar and pestle is... |
PMC9415412 | core_pubmed_pmc | Computer-Aided Screening of Phytoconstituents from Ocimum tenuiflorum against Diabetes Mellitus Targeting DPP4 Inhibition: A Combination of Molecular Docking, Molecular Dynamics, and Pharmacokinetics Approaches | Computer-Aided Screening of Phytoconstituents from Ocimum tenuiflorum against Diabetes Mellitus Targeting DPP4 Inhibition: A Combination of Molecular Docking, Molecular Dynamics, and Pharmacokinetics Approaches Abstract Abstract Diabetes mellitus is a major global health concern in the current scenario which is chiefly... |
PMC10636818 | core_pubmed_pmc | Panax japonicus C.A. Meyer: a comprehensive review on botany, phytochemistry, pharmacology, pharmacokinetics and authentication | Panax japonicus C.A. Meyer: a comprehensive review on botany, phytochemistry, pharmacology, pharmacokinetics and authentication Abstract Abstract Background Panax japonicu s C.A. Meyer (Zhujieshen) is widely used in traditional medicine as a tonic hemostatic and anti-inflammatory agent in China, Japan, and Korea. Furth... |
PMC7861408 | core_pubmed_pmc | Higher plasma drug levels in elderly people living with HIV treated with darunavir | Higher plasma drug levels in elderly people living with HIV treated with darunavir Abstract Abstract Background The proportion of elderly people living with HIV-1 (PLHIV) is rising. In older patients, comorbidities and concomitant medications are more frequent, increasing the risk of potential drug-drug interactions (P... |
PMC10014059 | core_pubmed_pmc | Investigation of simplified physiologically‐based pharmacokinetic models in rat and human | Investigation of simplified physiologically‐based pharmacokinetic models in rat and human Abstract Abstract Whole‐body physiologically‐based pharmacokinetic (PBPK) models have many applications in drug research and development. It is often necessary to inform these models with animal or clinical data, updating model pa... |
PMC12064631 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Prusogliptin (DBPR108), a Once-Daily Dipeptidyl Peptidase-4 Inhibitor, in Patients with Type 2 Diabetes | Pharmacokinetics and Pharmacodynamics of Prusogliptin (DBPR108), a Once-Daily Dipeptidyl Peptidase-4 Inhibitor, in Patients with Type 2 Diabetes Abstract Abstract Background and Objective DBPR108 (prusogliptin) is a novel, orally bioavailable dipeptidyl peptidase-4 (DPP‐4) inhibitor. This study investigated the pharmac... |
PMC12789420 | core_pubmed_pmc | Solvent dependent bioactivity and spectroscopic characterization of neovestitol from Nigerian propolis using experimental and computational methods | Solvent dependent bioactivity and spectroscopic characterization of neovestitol from Nigerian propolis using experimental and computational methods Abstract In this study, Neovestitol (NVT) isolated from Imo propolis was characterized, revealing its chemical structure and confirming its identity through nuclear magneti... |
PMC11456700 | core_pubmed_pmc | A Comparative Study of DC Beads, Callispheres and Multimodal Imaging Nano-Assembled Microspheres Loaded with Irinotecan in Vitro | A Comparative Study of DC Beads, Callispheres and Multimodal Imaging Nano-Assembled Microspheres Loaded with Irinotecan in Vitro Abstract Abstract Introduction: In recent years, the development of drug-eluting embolization beads that can be imaged has become a hot research topic in regard to meeting clinical needs. In ... |
PMC11452091 | core_pubmed_pmc | Road-traffic noise exposure and coronary atherosclerosis in the Swedish CArdioPulmonary bioImage Study (SCAPIS) | Road-traffic noise exposure and coronary atherosclerosis in the Swedish CArdioPulmonary bioImage Study (SCAPIS) Abstract Abstract Background: Road-traffic noise may influence the development of cardiovascular events such as stroke and myocardial infarction, but etiological mechanisms remain unclear. This study aimed to... |
PMC7345246 | core_pubmed_pmc | Considerations for Optimizing Dosing of Immunoglobulins Based on Pharmacokinetic Evidence | Considerations for Optimizing Dosing of Immunoglobulins Based on Pharmacokinetic Evidence Abstract Abstract Immunoglobulins (IGs) are widely used for the treatment of immunodeficiency syndromes and several autoimmune diseases. In neonates, IGs have been used for the treatment of alloimmune thrombocytopenia, in neonatal... |
PMC8152774 | core_pubmed_pmc | Refractory symptoms in paediatric palliative care: can ketamine help? | Refractory symptoms in paediatric palliative care: can ketamine help? Abstract Background One of the main challenges for paediatric palliative care (PPC) is the management of concomitant, different and severe symptoms that frequently affect the quality of life of PPC patients and are often refractory to commonly used p... |
PMC7831863 | core_pubmed_pmc | Role of favipiravir in the treatment of COVID-19 | Role of favipiravir in the treatment of COVID-19 Abstract Abstract The coronavirus disease-2019 (COVID-19) outbreak all over the world has led the researchers to strive to develop drugs or vaccines to prevent or halt the progression of this ailment. To hasten the treatment process, repurposed drugs are being evaluated.... |
PMC11106099 | core_pubmed_pmc | Relative Bioavailability of Dolutegravir (DTG) and Emtricitabine/Tenofovir Alafenamide Fumarate (F/TAF) Administered as Paediatric Tablet Formulations in Healthy Volunteers | Relative Bioavailability of Dolutegravir (DTG) and Emtricitabine/Tenofovir Alafenamide Fumarate (F/TAF) Administered as Paediatric Tablet Formulations in Healthy Volunteers Abstract Background and objective Within the UNIVERSAL project (RIA2019PD-2882) we aim to develop a paediatric dolutegravir (DTG)/emtricitabine (FT... |
PMC11638087 | core_pubmed_pmc | Model-based translation of results from in vitro to in vivo experiments for afabicin activity against Staphylococcus aureus | Model-based translation of results from in vitro to in vivo experiments for afabicin activity against Staphylococcus aureus Abstract Abstract Background Translation of experimental data on antibiotic activity typically relies on pharmacokinetic/pharmacodynamic (PK/PD) indices. Model-based approaches, considering the fu... |
PMC9893638 | core_pubmed_pmc | Population pharmacokinetics of buprenorphine and naloxone sublingual combination in Chinese healthy volunteers and patients with opioid use disorder: Model-based dose optimization | Population pharmacokinetics of buprenorphine and naloxone sublingual combination in Chinese healthy volunteers and patients with opioid use disorder: Model-based dose optimization Abstract The sublingual combination of buprenorphine (BUP) and naloxone (NLX) is a new treatment option for opioid use disorder (OUD) and is... |
PMC9381913 | core_pubmed_pmc | Multi‐phase multi‐layer mechanistic dermal absorption (MPML MechDermA) model to predict local and systemic exposure of drug products applied on skin | Multi‐phase multi‐layer mechanistic dermal absorption (MPML MechDermA) model to predict local and systemic exposure of drug products applied on skin Abstract Abstract Physiologically‐based pharmacokinetic models combine knowledge about physiology, drug product properties, such as physicochemical parameters, absorption,... |
PMC9306831 | core_pubmed_pmc | Intrapulmonary Pharmacokinetic Modeling and Simulation of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Patients With Pneumonia and Healthy Subjects | Intrapulmonary Pharmacokinetic Modeling and Simulation of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Patients With Pneumonia and Healthy Subjects Abstract Abstract Cefiderocol is a siderophore cephalosporin for the treatment of infections caused by gram‐negative bacteria including carbapenem‐resistant stra... |
PMC11002946 | core_pubmed_pmc | Drug Exposure of Long-Acting Cabotegravir and Rilpivirine in Older People With Human Immunodeficiency Virus: A Pharmacokinetic Modeling Study | Drug Exposure of Long-Acting Cabotegravir and Rilpivirine in Older People With Human Immunodeficiency Virus: A Pharmacokinetic Modeling Study Abstract Abstract Background The life expectancy of people with human immunodeficiency virus (PWH) has significantly increased, thanks to combined antiretrovirals with improved p... |
PMC8196871 | core_pubmed_pmc | Molecular Imaging and Preclinical Studies of Radiolabeled Long-Term RGD Peptides in U-87 MG Tumor-Bearing Mice | Molecular Imaging and Preclinical Studies of Radiolabeled Long-Term RGD Peptides in U-87 MG Tumor-Bearing Mice Abstract The Arg–Gly–Asp (RGD) peptide shows a high affinity for α v β 3 integrin, which is overexpressed in new tumor blood vessels and many types of tumor cells. The radiolabeled RGD peptide has been studied... |
PMC12153896 | core_pubmed_pmc | Pharmacokinetic Profile of Two Active Dipyrone Metabolites, 4-Methylaminoantipyrine (MAA) and 4-Aminoantipyrine (AA), Following Intravenous Administration in Dogs: A Preliminary Study | Pharmacokinetic Profile of Two Active Dipyrone Metabolites, 4-Methylaminoantipyrine (MAA) and 4-Aminoantipyrine (AA), Following Intravenous Administration in Dogs: A Preliminary Study Abstract Simple Summary Dipyrone is widely used to control pain. However, although the standard dose for routine use is 25 mg·kg −1 , no... |
PMC12944088 | core_pubmed_pmc | Nanotechnology-Enabled Precision Therapy for Lung Cancer in Never-Smokers | Nanotechnology-Enabled Precision Therapy for Lung Cancer in Never-Smokers Abstract Lung cancer in never-smokers (LCINS) represents a distinct clinical entity driven by dominant oncogenic alterations and characterized by a low tumor mutational burden. Although tyrosine kinase inhibitors (TKIs) achieve high initial respo... |
PMC7457350 | core_pubmed_pmc | Ertapenem and Faropenem against Mycobacterium tuberculosis : in vitro testing and comparison by macro and microdilution | Ertapenem and Faropenem against Mycobacterium tuberculosis : in vitro testing and comparison by macro and microdilution Abstract Background Interest in carbapenems has been rising in the last few years due to the emergence of drug resistant tuberculosis. Ertapenem (ETP), given once a day parenteral, and faropenem (FAR)... |
PMC7217817 | core_pubmed_pmc | Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug–Drug Interactions Using Physiologically Based Pharmacokinetic Modeling | Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug–Drug Interactions Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Introduction Elagolix is approved for the management of moderate-to-severe pain associated with endometriosis. The aim of this analysis was to develop a phys... |
PMC12466486 | core_pubmed_pmc | Postβ-Lactamase-Inhibiting Effect of Sulbactam in Combination with Ceftriaxone on Extended-Spectrum-β-Lactamase-Producing Escherichia coli | Postβ-Lactamase-Inhibiting Effect of Sulbactam in Combination with Ceftriaxone on Extended-Spectrum-β-Lactamase-Producing Escherichia coli Abstract Background/Objectives : Extended-spectrum β-lactamase (ESBL)-producing Escherichia coli poses a significant global health challenge, as it leads to antimicrobial treatment ... |
PMC3393068 | core_pubmed_pmc | Newer agents in antiplatelet therapy: a review | Newer agents in antiplatelet therapy: a review Abstract Abstract Antiplatelet therapy remains the mainstay in preventing aberrant platelet activation in pathophysiological conditions such as myocardial infarction, ischemia, and stroke. Although there has been significant advancement in antiplatelet therapeutic approach... |
PMC4821390 | core_pubmed_pmc | Nanomedicine developments in the treatment of metastatic pancreatic cancer: focus on nanoliposomal irinotecan | Nanomedicine developments in the treatment of metastatic pancreatic cancer: focus on nanoliposomal irinotecan Abstract Abstract Nanoliposomal irinotecan (nal-IRI) was originally developed using an efficient and high-loading capacity system to encapsulate irinotecan within a liposomal carrier, producing a therapeutic ag... |
PMC5323192 | core_pubmed_pmc | Involvement of let-7 microRNA for the therapeutic effects of Rhenium-188-embedded liposomal nanoparticles on orthotopic human head and neck cancer model | Involvement of let-7 microRNA for the therapeutic effects of Rhenium-188-embedded liposomal nanoparticles on orthotopic human head and neck cancer model Abstract Human head and neck squamous cell carcinoma (HNSCC) is usually treated by surgical resection with adjuvant radio-chemotherapy. In this study, we examined whet... |
PMC12567511 | core_pubmed_pmc | Engineered Phage-Guided Nanotherapeutic Systems for Precision Antibacterial Therapy: Hacking Bacterial Resistance Mechanisms | Engineered Phage-Guided Nanotherapeutic Systems for Precision Antibacterial Therapy: Hacking Bacterial Resistance Mechanisms Abstract Antibiotic resistance (ABR) poses a critical global public health challenge necessitating immediate action. Without prompt interventions, infections caused by antibiotic-resistant bacter... |
PMC11293488 | core_pubmed_pmc | Uncovering the Role of Direct Oral Anticoagulants in Stroke Prevention for Atrial Fibrillation: A Review of the Literature | Uncovering the Role of Direct Oral Anticoagulants in Stroke Prevention for Atrial Fibrillation: A Review of the Literature Abstract Abstract Atrial fibrillation (AF) is a predominant contributor to morbidity and mortality, and stroke prevention remains the mainstay for the management of AF. The precise mechanism involv... |
PMC7384162 | core_pubmed_pmc | Effects of Lasmiditan on Cardiovascular Parameters and Pharmacokinetics in Healthy Subjects Receiving Oral Doses of Propranolol | Effects of Lasmiditan on Cardiovascular Parameters and Pharmacokinetics in Healthy Subjects Receiving Oral Doses of Propranolol Abstract Abstract Lasmiditan ( LY573144 /COL‐144) is a high‐affinity, centrally penetrant, selective 5‐HT 1F receptor agonist currently under investigation for acute treatment of migraine. Alt... |
PMC5345593 | core_pubmed_pmc | Safety, Efficacy, and Exposure–Response of Voriconazole in Pediatric Patients With Invasive Aspergillosis, Invasive Candidiasis or Esophageal Candidiasis | Safety, Efficacy, and Exposure–Response of Voriconazole in Pediatric Patients With Invasive Aspergillosis, Invasive Candidiasis or Esophageal Candidiasis Abstract Abstract Background: Data on safety and efficacy of voriconazole for invasive aspergillosis (IA) and invasive candidiasis/esophageal candidiasis (IC/EC) in p... |
PMC9659104 | core_pubmed_pmc | Pharmacogenetics of Drug Metabolism: The Role of Gene Polymorphism in the Regulation of Doxorubicin Safety and Efficacy | Pharmacogenetics of Drug Metabolism: The Role of Gene Polymorphism in the Regulation of Doxorubicin Safety and Efficacy Abstract Simple Summary The effectiveness and safety of the anti-cancer agent doxorubicin (anthracycline group medicine) depend on the metabolism and retention of the drug in the human organism. Polym... |
PMC4574824 | core_pubmed_pmc | Effects of food on pharmacokinetics of immediate release oral formulations of aspirin, dipyrone, paracetamol and NSAIDs – a systematic review | Effects of food on pharmacokinetics of immediate release oral formulations of aspirin, dipyrone, paracetamol and NSAIDs – a systematic review Abstract Aims It is common to advise that analgesics, and especially non-steroidal anti-inflammatory drugs (NSAIDs), be taken with food to reduce unwanted gastrointestinal advers... |
PMC6247400 | core_pubmed_pmc | The clinical toxicology of caffeine: A review and case study | The clinical toxicology of caffeine: A review and case study Abstract Caffeine is a widely recognized psychostimulant compound with a long history of consumption by humans. While it has received a significant amount of attention there is still much to be learned with respect to its toxicology in humans, especially in c... |
PMC12872935 | core_pubmed_pmc | Real-world study of adverse events associated with ceftazidime/avibactam based on the U.S. Food and Drug Administration adverse event reporting system database | Real-world study of adverse events associated with ceftazidime/avibactam based on the U.S. Food and Drug Administration adverse event reporting system database Abstract Abstract Objective Ceftazidime/avibactam (CZA), a combination of the third-generation cephalosporin ceftazidime and the novel, non-β-lactam β-lactamase... |
PMC4230487 | core_pubmed_pmc | Use of a physiologically-based pharmacokinetic model to simulate artemether dose adjustment for overcoming the drug-drug interaction with efavirenz | Use of a physiologically-based pharmacokinetic model to simulate artemether dose adjustment for overcoming the drug-drug interaction with efavirenz Abstract Purpose To treat malaria, HIV-infected patients normally receive artemether (80 mg twice daily) concurrently with antiretroviral therapy and drug-drug interactions... |
PMC12619615 | core_pubmed_pmc | Contezolid for the Super-Elderly: Balancing Efficacy and Safety Through Pharmacokinetic Insights | Contezolid for the Super-Elderly: Balancing Efficacy and Safety Through Pharmacokinetic Insights Abstract Background Contezolid is a new oxazolidinone antibacterial agent, and its pharmacokinetic (PK) characteristics and safety in super-elderly patients remain poorly understood. Methods Contezolid PK parameters were an... |
PMC11541526 | core_pubmed_pmc | Synthesis of Tryptamine-Thiazolidin-4-one Derivatives and the Combined In Silico and In Vitro Evaluation of their Biological Activity and Cytotoxicity | Synthesis of Tryptamine-Thiazolidin-4-one Derivatives and the Combined In Silico and In Vitro Evaluation of their Biological Activity and Cytotoxicity Abstract Abstract Tryptamine, a monoamine alkaloid with an indole ring structure, is derived from the decarboxylation of the amino acid tryptophan, which is present in f... |
PMC5832324 | core_pubmed_pmc | Pharmacogenomics of Chemically Distinct Classes of Keap1-Nrf2 Activators Identify Common and Unique Gene, Protein, and Pathway Responses In Vivo | Pharmacogenomics of Chemically Distinct Classes of Keap1-Nrf2 Activators Identify Common and Unique Gene, Protein, and Pathway Responses In Vivo Abstract Abstract The Kelch-like erythroid-associated protein 1 (Keap1)–NF-E2-related factor 2 (Nrf2) signaling pathway is the subject of several clinical trials evaluating th... |
PMC9668967 | core_pubmed_pmc | The progressive ratio and fixed ratio 1 schedules of cocaine self-administration in rats convey the same information | The progressive ratio and fixed ratio 1 schedules of cocaine self-administration in rats convey the same information Abstract Progressive ratio (PR) schedules of drug delivery are used to determine the ‘motivational’ state of an animal and drug ‘reinforcing efficacy’. This widely held interpretation is supported mainly... |
PMC6225502 | core_pubmed_pmc | Epacadostat Plus Pembrolizumab in Patients With Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037) | Epacadostat Plus Pembrolizumab in Patients With Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037) Abstract Purpose Tumors may evade immunosurveillance through upregulation of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme. Epacadostat is a potent and highly s... |
PMC10290391 | core_pubmed_pmc | Targeted degradation of ⍺-synuclein aggregates in Parkinson’s disease using the AUTOTAC technology | Targeted degradation of ⍺-synuclein aggregates in Parkinson’s disease using the AUTOTAC technology Abstract Background There are currently no disease-modifying therapeutics for Parkinson’s disease (PD). Although extensive efforts were undertaken to develop therapeutic approaches to delay the symptoms of PD, untreated α... |
PMC10329437 | core_pubmed_pmc | Recommendations of Gentamicin Dose Based on Different Pharmacokinetic/Pharmacodynamic Targets for Intensive Care Adult Patients: A Redefining Approach | Recommendations of Gentamicin Dose Based on Different Pharmacokinetic/Pharmacodynamic Targets for Intensive Care Adult Patients: A Redefining Approach Abstract Background In addition to the maximum plasma concentration (C max ) to the minimum inhibitory concentration (MIC) ratio, the 24-hour area under the concentratio... |
PMC9292737 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Burosumab in Adult and Pediatric Patients With X‐linked Hypophosphatemia | Population Pharmacokinetics and Pharmacodynamics of Burosumab in Adult and Pediatric Patients With X‐linked Hypophosphatemia Abstract Abstract Burosumab is a fully human monoclonal antibody against fibroblast growth factor 23, which has been approved to treat X‐linked hypophosphatemia (XLH) in adult and pediatric patie... |
PMC7938004 | core_pubmed_pmc | Pharmacokinetics of Intravitreal Vancomycin and Ceftazidime in Silicone Oil-Filled Macaque Eyes | Pharmacokinetics of Intravitreal Vancomycin and Ceftazidime in Silicone Oil-Filled Macaque Eyes Abstract Purpose This study evaluated the pharmacokinetics of intravitreal vancomycin and ceftazidime in the aqueous humor of macaque eyes filled with silicone oil in the vitreous cavity. Methods Intravitreal vancomycin (1 m... |
PMC3419350 | core_pubmed_pmc | CYP2C19 polymorphism affects single-dose pharmacokinetics of oral pantoprazole in healthy volunteers | CYP2C19 polymorphism affects single-dose pharmacokinetics of oral pantoprazole in healthy volunteers Abstract Abstract Objectives Pantoprazole is metabolized by cytochrome P450 2 C19, which shows genetic polymorphism. The effect of CYP2C19 polymorphism on single-dose pharmacokinetics of oral pantoprazole in healthy vol... |
PMC8422741 | core_pubmed_pmc | Pharmacokinetics of loxoprofen in a self-administered overdose in a Japanese patient admitted to hospital | Pharmacokinetics of loxoprofen in a self-administered overdose in a Japanese patient admitted to hospital Abstract Abstract Background Loxoprofen is a propionic acid derivative and is the most widely prescribed non-steroidal anti-inflammatory drug in Japan. Loxoprofen is generally considered to be relatively nontoxic. ... |
PMC4831483 | core_pubmed_pmc | Variability in plasma concentration of cefotaxime in critically ill patients in an Intensive Care Unit of India and its pharmacodynamic outcome: A nonrandomized, prospective, open-label, analytical study | Variability in plasma concentration of cefotaxime in critically ill patients in an Intensive Care Unit of India and its pharmacodynamic outcome: A nonrandomized, prospective, open-label, analytical study Abstract Abstract Background: Cefotaxime is a widely utilized cephalosporin in most intensive care units of India. H... |
PMC10220743 | core_pubmed_pmc | Pharmacokinetic Feasibility of Stability-Enhanced Solid-State (SESS) Tenofovir Disoproxil Free Base Crystal | Pharmacokinetic Feasibility of Stability-Enhanced Solid-State (SESS) Tenofovir Disoproxil Free Base Crystal Abstract Abstract Tenofovir (TEV) is a nucleotide reverse transcriptase inhibitor used against human immunodeficiency virus (HIV) reverse transcriptase. To improve the poor bioavailability of TEV, TEV disoproxil ... |
PMC12568129 | core_pubmed_pmc | Computational Modelling Suggests Bacteriostatic Saline Does Not Reverse Botulinum Toxin-Induced Brow Ptosis | Computational Modelling Suggests Bacteriostatic Saline Does Not Reverse Botulinum Toxin-Induced Brow Ptosis Abstract Abstract Anecdotal reports have recently circulated suggesting that intramuscular injection of bacteriostatic saline (BS)—which contains benzyl alcohol (BnOH)—can reverse botulinum toxin type A (BoNTA)-i... |
PMC4033275 | core_pubmed_pmc | SPARC independent drug delivery and antitumour effects of nab -paclitaxel in genetically engineered mice | SPARC independent drug delivery and antitumour effects of nab -paclitaxel in genetically engineered mice Abstract Abstract Design Pharmacokinetic and pharmacodynamic parameters of cremophor-paclitaxel, nab -paclitaxel (human-albumin-bound paclitaxel, Abraxane) and a novel mouse-albumin-bound paclitaxel ( m-nab -paclita... |
PMC6542779 | core_pubmed_pmc | Tobramycin Clearance Is Best Described by Renal Function Estimates in Obese and Non-obese Individuals: Results of a Prospective Rich Sampling Pharmacokinetic Study | Tobramycin Clearance Is Best Described by Renal Function Estimates in Obese and Non-obese Individuals: Results of a Prospective Rich Sampling Pharmacokinetic Study Abstract Purpose Tobramycin is an aminoglycoside antibiotic of which the 24 h exposure correlates with efficacy. Recently, we found that clearance of the am... |
PMC12609022 | core_pubmed_pmc | Pharmacological Management of Oral and Esophageal Candidiasis: A Clinical Pharmacotherapy Perspective | Pharmacological Management of Oral and Esophageal Candidiasis: A Clinical Pharmacotherapy Perspective Abstract Abstract Candida spp. are common components of normal microbiota in the oral cavity. However, Candida albicans can be a primary cause of superficial infections in the oral cavity and esophagus, especially in i... |
PMC5328523 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of MEDI8897, the Respiratory Syncytial Virus Prefusion F-Targeting Monoclonal Antibody with an Extended Half-Life, in Healthy Adults | Safety, Tolerability, and Pharmacokinetics of MEDI8897, the Respiratory Syncytial Virus Prefusion F-Targeting Monoclonal Antibody with an Extended Half-Life, in Healthy Adults Abstract ABSTRACT Prevention of respiratory syncytial virus (RSV) illness in infants is a major public health priority, but there is no approved... |
PMC5744692 | core_pubmed_pmc | High-Throughput Analysis of Ovarian Cycle Disruption by Mixtures of Aromatase Inhibitors | High-Throughput Analysis of Ovarian Cycle Disruption by Mixtures of Aromatase Inhibitors Abstract Background: Combining computational toxicology with ExpoCast exposure estimates and ToxCast™ assay data gives us access to predictions of human health risks stemming from exposures to chemical mixtures. Objectives: We expl... |
PMC6532162 | core_pubmed_pmc | Clinically relevant pharmacokinetic knowledge on antibiotic dosing among intensive care professionals is insufficient: a cross-sectional study | Clinically relevant pharmacokinetic knowledge on antibiotic dosing among intensive care professionals is insufficient: a cross-sectional study Abstract Abstract Background Antibiotic exposure in intensive care patients with sepsis is frequently inadequate and is associated with poorer outcomes. Antibiotic dosing is cha... |
PMC9579625 | core_pubmed_pmc | FORWARDS-1: an adaptive, single-blind, placebo-controlled ascending dose study of acute baclofen on safety parameters in opioid dependence during methadone-maintenance treatment—a pharmacokinetic-pharmacodynamic study | FORWARDS-1: an adaptive, single-blind, placebo-controlled ascending dose study of acute baclofen on safety parameters in opioid dependence during methadone-maintenance treatment—a pharmacokinetic-pharmacodynamic study Abstract Abstract Background Treatment of opiate addiction with opiate substitution treatment (e.g. me... |
PMC9312177 | core_pubmed_pmc | Intermittent Short-Term Infusion vs. Continuous Infusion of Piperacillin: Steady State Concentrations in Porcine Cervical Spine Tissue Evaluated by Microdialysis | Intermittent Short-Term Infusion vs. Continuous Infusion of Piperacillin: Steady State Concentrations in Porcine Cervical Spine Tissue Evaluated by Microdialysis Abstract Background: Piperacillin is a central drug in the treatment of Pseudomonas aeruginosa spondylodiscitis. Intermittent short-term infusion (STI) remain... |
PMC11604993 | core_pubmed_pmc | Late-stage (radio)fluorination of alkyl phosphonates via electrophilic activation | Late-stage (radio)fluorination of alkyl phosphonates via electrophilic activation Abstract Constructing organic fluorophosphines, vital drug skeletons, through the direct fluorination of readily available alkyl phosphonates has been impeded due to the intrinsic low electrophilicity of P V and the high bond energy of P═... |
PMC12309592 | core_pubmed_pmc | BEBT-209, a primary CDK4 selective inhibitor, for the treatment of HR+/HER2- advanced breast cancer (BECTOP1): a phase 1, multicentre, open-label study | BEBT-209, a primary CDK4 selective inhibitor, for the treatment of HR+/HER2- advanced breast cancer (BECTOP1): a phase 1, multicentre, open-label study Abstract Abstract Purpose Several cyclin-dependent kinase 4/6 (CDK4/6) inhibitors have been approved for the treatment of hormone receptor-positive (HR+) and human epid... |
PMC12772413 | core_pubmed_pmc | Phytochemical Profiling, Molecular Docking, ADMET Analysis of Zingiber Officinale Peel Extract for the Biogenic Synthesis of ZnO and Fe-Doped ZnO Nanoparticles with Antibacterial and Photocatalytic Potential | Phytochemical Profiling, Molecular Docking, ADMET Analysis of Zingiber Officinale Peel Extract for the Biogenic Synthesis of ZnO and Fe-Doped ZnO Nanoparticles with Antibacterial and Photocatalytic Potential Abstract Abstract Industrial dye effluents are the predominant source of water pollution, while the increasing p... |
PMC11628175 | core_pubmed_pmc | Exploring the Inhibitory Potential of M. pendans Compounds Against N -Acetylglucosamine (Mur) Receptor: In Silico Insights Into Antibacterial Activity and Drug-Likeness | Exploring the Inhibitory Potential of M. pendans Compounds Against N -Acetylglucosamine (Mur) Receptor: In Silico Insights Into Antibacterial Activity and Drug-Likeness Abstract Abstract Oral diseases are often caused by bacterial infections, making the inhibition of receptors like N -acetylglucosamine critical in prev... |
PMC10191064 | core_pubmed_pmc | PEGylated Tween 80-functionalized chitosan-lipidic nano-vesicular hybrids for heightening nose-to-brain delivery and bioavailability of metoclopramide | PEGylated Tween 80-functionalized chitosan-lipidic nano-vesicular hybrids for heightening nose-to-brain delivery and bioavailability of metoclopramide Abstract Abstract A PEGylated Tween 80–functionalized chitosan–lipidic (PEG-T-Chito-Lip) nano-vesicular hybrid was developed for intranasal administration as an alternat... |
PMC5118988 | core_pubmed_pmc | Pharmacokinetics of the New Hepatitis C Virus NS3 Protease Inhibitor Narlaprevir following Single-Dose Use with or without Ritonavir in Patients with Liver Cirrhosis | Pharmacokinetics of the New Hepatitis C Virus NS3 Protease Inhibitor Narlaprevir following Single-Dose Use with or without Ritonavir in Patients with Liver Cirrhosis Abstract In this study we sought to evaluate narlaprevir (NVR) pharmacokinetics (PK) after a single dose with or without ritonavir (RTV) in cirrhotic vers... |
PMC6907063 | core_pubmed_pmc | The Herb-Drug Pharmacokinetic Interaction of Fluoxetine and Its Metabolite Norfluoxetine with a Traditional Chinese Medicine in Rats by LC-MS/MS | The Herb-Drug Pharmacokinetic Interaction of Fluoxetine and Its Metabolite Norfluoxetine with a Traditional Chinese Medicine in Rats by LC-MS/MS Abstract Abstract Background Fluoxetine (FLU) is the first-line and widely used medication for depression. The combination of Chaihu Shugan san (CSGS) and FLU is commonly used... |
PMC11858960 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Model of CYP2D6 Associated Interaction Between Venlafaxine and Strong Inhibitor Bupropion—The Influence of Age-Relevant Changes and Inhibitory Dose to Classify Therapeutical Success and Harm | Physiologically Based Pharmacokinetic Model of CYP2D6 Associated Interaction Between Venlafaxine and Strong Inhibitor Bupropion—The Influence of Age-Relevant Changes and Inhibitory Dose to Classify Therapeutical Success and Harm Abstract Background/Objectives: Venlafaxine (VEN) is commonly used in young and elderly pat... |
PMC3699390 | core_pubmed_pmc | A multicenter, open-label, phase 2 study of lenalidomide plus low-dose dexamethasone in Chinese patients with relapsed/refractory multiple myeloma: the MM-021 trial | A multicenter, open-label, phase 2 study of lenalidomide plus low-dose dexamethasone in Chinese patients with relapsed/refractory multiple myeloma: the MM-021 trial Abstract Background There is an unmet need for treatment options in Chinese patients with relapsed or refractory multiple myeloma (RRMM). Lenalidomide plus... |
PMC9010267 | core_pubmed_pmc | Population pharmacokinetic modeling and simulations of berotralstat for prophylactic treatment of attacks of hereditary angioedema | Population pharmacokinetic modeling and simulations of berotralstat for prophylactic treatment of attacks of hereditary angioedema Abstract Abstract Hereditary angioedema (HAE) is an autosomal dominant disorder characterized by recurrent episodes of swelling of the skin, larynx, gastrointestinal tract, genitals, and ex... |
PMC12409652 | core_pubmed_pmc | Effect of Meloxicam on the Pharmacokinetics of Cefquinome in Endotoxemic Sheep | Effect of Meloxicam on the Pharmacokinetics of Cefquinome in Endotoxemic Sheep Abstract ABSTRACT Objective The objective of this study was to investigate the effect of meloxicam on the pharmacokinetics of cefquinome in experimental endotoxemic sheep. In addition, the MIC of cefquinome was determined against Escherichia... |
PMC9798760 | core_pubmed_pmc | Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique | Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique Abstract The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble dru... |
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