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PMC6929995 | core_pubmed_pmc | Rod-shape theranostic nanoparticles facilitate antiretroviral drug biodistribution and activity in human immunodeficiency virus susceptible cells and tissues | Rod-shape theranostic nanoparticles facilitate antiretroviral drug biodistribution and activity in human immunodeficiency virus susceptible cells and tissues Abstract Human immunodeficiency virus theranostics facilitates the development of long acting (LA) antiretroviral drugs (ARVs) by defining drug-particle cell depo... |
PMC6771872 | core_pubmed_pmc | Fast‐acting insulin aspart in people with type 2 diabetes: Earlier onset and greater initial exposure and glucose‐lowering effect compared with insulin aspart | Fast‐acting insulin aspart in people with type 2 diabetes: Earlier onset and greater initial exposure and glucose‐lowering effect compared with insulin aspart Abstract Abstract Aims To investigate the pharmacokinetic/pharmacodynamic properties of fast‐acting insulin aspart (faster aspart) versus insulin aspart (IAsp) i... |
PMC11963601 | core_pubmed_pmc | Clinical outcomes and pharmacokinetics/pharmacodynamics of intravenous polymyxin B treatment for various site carbapenem-resistant gram-negative bacterial infections: a prospective observational multicenter study | Clinical outcomes and pharmacokinetics/pharmacodynamics of intravenous polymyxin B treatment for various site carbapenem-resistant gram-negative bacterial infections: a prospective observational multicenter study Abstract ABSTRACT Polymyxin B, a last resort for carbapenem-resistant gram-negative bacteria (CRGNB) infect... |
PMC6792482 | core_pubmed_pmc | Phase I trial of TAK‐385 in hormone treatment‐naïve Japanese patients with nonmetastatic prostate cancer | Phase I trial of TAK‐385 in hormone treatment‐naïve Japanese patients with nonmetastatic prostate cancer Abstract Abstract This open‐label, phase I dose‐finding study evaluated the gonadotropin‐releasing hormone antagonist, TAK‐385, in Japanese patients with nonmetastatic prostate cancer. In a two‐part design, patients... |
PMC7022474 | core_pubmed_pmc | Characterization of the Prion Protein Binding Properties of Antisense Oligonucleotides | Characterization of the Prion Protein Binding Properties of Antisense Oligonucleotides Abstract Abstract Antisense oligonucleotides (ASOs) designed to lower prion protein (PrP) expression in the brain through RNase H1-mediated degradation of PrP RNA are in development as prion disease therapeutics. ASOs were previously... |
PMC11659896 | core_pubmed_pmc | Design, Synthesis, and Evaluation of Trihalomethyl Ketone Derivatives of Neocarzilin A as Improved Antimetastatic Agents | Design, Synthesis, and Evaluation of Trihalomethyl Ketone Derivatives of Neocarzilin A as Improved Antimetastatic Agents Abstract Vesicle Amine Transport-1 (VAT1) is a protein that is overexpressed in many cancers, including breast cancer, glioblastoma, and angiosarcoma. High VAT1 expression correlates with poor overal... |
PMC12473689 | core_pubmed_pmc | Drug Metabolism and Pharmacokinetics of Oxazolo[4,5- c ]quinoline Analogs as Novel Interleukin-33 Inhibitors | Drug Metabolism and Pharmacokinetics of Oxazolo[4,5- c ]quinoline Analogs as Novel Interleukin-33 Inhibitors Abstract Background/Objectives : Interleukin-33 (IL-33) is crucial in immune-mediated diseases like asthma. Targeting the IL-33/ST2 pathway holds therapeutic promise. This study characterized the pharmacokinetic... |
PMC7022972 | core_pubmed_pmc | Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat | Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat Abstract Abstract Tetrodotoxin (TTX) was identified as a latent neurotoxin that has a significant analgesia effect. It was rapidly absorbed and excreted in rat after intramuscular (i.m.) injection. To maintain the effect, frequent injections ... |
PMC7797213 | core_pubmed_pmc | Vascular effects of serelaxin in patients with stable coronary artery disease: a randomized placebo-controlled trial | Vascular effects of serelaxin in patients with stable coronary artery disease: a randomized placebo-controlled trial Abstract Abstract Aims The effects of serelaxin, a recombinant form of human relaxin-2 peptide, on vascular function in the coronary microvascular and systemic macrovascular circulation remain largely un... |
PMC3020311 | core_pubmed_pmc | The use of the SAEM algorithm in MONOLIX software for estimation of population pharmacokinetic-pharmacodynamic-viral dynamics parameters of maraviroc in asymptomatic HIV subjects | The use of the SAEM algorithm in MONOLIX software for estimation of population pharmacokinetic-pharmacodynamic-viral dynamics parameters of maraviroc in asymptomatic HIV subjects Abstract Using simulated viral load data for a given maraviroc monotherapy study design, the feasibility of different algorithms to perform p... |
PMC11795045 | core_pubmed_pmc | Characterizing the plasma protein binding profiles of chemistry diversified antisense oligonucleotides in human and mouse plasma using an ultrafiltration method | Characterizing the plasma protein binding profiles of chemistry diversified antisense oligonucleotides in human and mouse plasma using an ultrafiltration method Abstract Introduction Plasma protein binding plays a significant role in influencing the pharmacokinetic and pharmacodynamic properties of drugs. This study fo... |
PMC9654380 | core_pubmed_pmc | Pharmacodynamic Interactions between Puerarin and Metformin in Type-2 Diabetic Rats | Pharmacodynamic Interactions between Puerarin and Metformin in Type-2 Diabetic Rats Abstract Herb–drug interactions are vital in effectively managing type-2-diabetes complications. Puerarin is a natural isoflavonoid in the Pueraria genus, and its pharmacological activities, including antidiabetic activity, are well est... |
PMC12925283 | core_pubmed_pmc | The toxicology of orally administered Δ 9 -tetrahydrocannabinol in sheep | The toxicology of orally administered Δ 9 -tetrahydrocannabinol in sheep Abstract Introduction As part of a larger study to assess the potential value of industrial hemp biomass (the low Δ 9 -tetrahydrocannabinol (Δ 9 -THC) variety of Cannabis sativa L.) as a feed for ruminants, a pharmacokinetics study of Δ 9 -THC, on... |
PMC7690812 | core_pubmed_pmc | Bioavailability of Orally Administered Active Lipid Compounds from four Different Greenshell™ Mussel Formats | Bioavailability of Orally Administered Active Lipid Compounds from four Different Greenshell™ Mussel Formats Abstract Abstract Greenshell™ mussel (GSM, Perna canaliculus ) is New Zealand’s most important aquaculture species. They are a good source of long chain-polyunsaturated fatty acids ( n -3 LC PUFA). Beyond a trad... |
PMC12078936 | core_pubmed_pmc | In-silico discovery of type-2 diabetes-causing host key genes that are associated with the complexity of monkeypox and repurposing common drugs | In-silico discovery of type-2 diabetes-causing host key genes that are associated with the complexity of monkeypox and repurposing common drugs Abstract Abstract Monkeypox (Mpox) is a major global human health threat after COVID-19. Its treatment becomes complicated with type-2 diabetes (T2D). It may happen due to the ... |
PMC6966186 | core_pubmed_pmc | Population Pharmacokinetics of Ipilimumab in Combination With Nivolumab in Patients With Advanced Solid Tumors | Population Pharmacokinetics of Ipilimumab in Combination With Nivolumab in Patients With Advanced Solid Tumors Abstract Abstract Ipilimumab is a fully human monoclonal antibody approved for the treatment of melanoma as monotherapy and for the treatment of melanoma, renal cell carcinoma, and colorectal cancer in combina... |
PMC8359405 | core_pubmed_pmc | Comprehensive evaluation of microneedle‐based intradermal adalimumab delivery vs . subcutaneous administration: results of a randomized controlled clinical trial | Comprehensive evaluation of microneedle‐based intradermal adalimumab delivery vs . subcutaneous administration: results of a randomized controlled clinical trial Abstract Abstract Aims To evaluate feasibility of intradermal (i.d.) adalimumab administration using hollow microneedles, and to compare a single i.d. dose of... |
PMC7193498 | core_pubmed_pmc | Relationship between factor VIII activity, bleeds and individual characteristics in severe hemophilia A patients | Relationship between factor VIII activity, bleeds and individual characteristics in severe hemophilia A patients Abstract Abstract Pharmacokinetic-based prophylaxis of replacement factor VIII (FVIII) products has been encouraged in recent years, but the relationship between exposure (factor VIII activity) and response ... |
PMC8521403 | core_pubmed_pmc | Effect of efavirenz-based ART on the pharmacokinetics of rifampicin and its primary metabolite in patients coinfected with TB and HIV | Effect of efavirenz-based ART on the pharmacokinetics of rifampicin and its primary metabolite in patients coinfected with TB and HIV Abstract Abstract Objectives To evaluate the effects of concomitant efavirenz-based ART and genetic polymorphism on the variability in rifampicin and 25-desacetylrifampicin pharmacokinet... |
PMC8327158 | core_pubmed_pmc | PEGylated AdipoRon derivatives improve glucose and lipid metabolism under insulinopenic and high-fat diet conditions | PEGylated AdipoRon derivatives improve glucose and lipid metabolism under insulinopenic and high-fat diet conditions Abstract Abstract The pleiotropic actions of adiponectin in improving cell survival and metabolism have motivated the development of small-molecule therapeutic agents for treating diabetes and lipotoxici... |
PMC10054914 | core_pubmed_pmc | Prediction of the Drug–Drug Interaction Potential between Tegoprazan and Amoxicillin/Clarithromycin Using the Physiologically Based Pharmacokinetic and Pharmacodynamic Model | Prediction of the Drug–Drug Interaction Potential between Tegoprazan and Amoxicillin/Clarithromycin Using the Physiologically Based Pharmacokinetic and Pharmacodynamic Model Abstract Abstract Tegoprazan is a novel potassium-competitive acid blocker. This study investigated the effect of drug–drug interaction on the pha... |
PMC6733293 | core_pubmed_pmc | Development and characterization of liposomal formulation of bortezomib | Development and characterization of liposomal formulation of bortezomib Abstract Abstract Bortezomib is a proteasome inhibitor used for the treatment of multiple myeloma. The poor pharmacokinetic profile and off-target adverse effects provide a strong incentive to develop drug delivery systems for bortezomib. In the pa... |
PMC9231303 | core_pubmed_pmc | Pharmacokinetic–Pharmacometabolomic Approach in Early-Phase Clinical Trials: A Way Forward for Targeted Therapy in Type 2 Diabetes | Pharmacokinetic–Pharmacometabolomic Approach in Early-Phase Clinical Trials: A Way Forward for Targeted Therapy in Type 2 Diabetes Abstract Abstract Pharmacometabolomics in early phase clinical trials demonstrate the metabolic profiles of a subject responding to a drug treatment in a controlled environment, whereas pha... |
PMC6454998 | core_pubmed_pmc | A phase 1, open-label, single-arm study evaluating the ocular safety of OTX-101 and systemic absorption of cyclosporine in healthy human volunteers | A phase 1, open-label, single-arm study evaluating the ocular safety of OTX-101 and systemic absorption of cyclosporine in healthy human volunteers Abstract Purpose To evaluate the ocular safety of OTX-101 0.09% – a novel, nanomicellar, clear, aqueous solution of cyclosporine (CsA) – and to determine the systemic expos... |
PMC12796165 | core_pubmed_pmc | Personalized chronotherapy in glioblastoma: integrating circadian profiling and PK–PD modelling to optimize temozolomide timing | Personalized chronotherapy in glioblastoma: integrating circadian profiling and PK–PD modelling to optimize temozolomide timing Abstract Glioblastoma (GBM) remains one of the most lethal brain tumors, with limited benefit from current standard therapies, including temozolomide (TMZ). Chronotherapy—aligning treatment wi... |
PMC11152740 | core_pubmed_pmc | Analysis of the pharmacokinetics and efficacy of RBD1016 – A GalNAc-siRNA targeting Hepatitis B Virus X gene using semi-mechanistic PK/PD model | Analysis of the pharmacokinetics and efficacy of RBD1016 – A GalNAc-siRNA targeting Hepatitis B Virus X gene using semi-mechanistic PK/PD model Abstract Abstract Small interference RNA (siRNA) is a class of short double-stranded RNA molecules that cause mRNA degradation through an RNA interference mechanism and is a pr... |
PMC5094503 | core_pubmed_pmc | Confirmation of Biosimilarity in a Pharmacokinetic/Pharmacodynamic Study in Healthy Volunteers for an Analytically Highly Similar Pegfilgrastim | Confirmation of Biosimilarity in a Pharmacokinetic/Pharmacodynamic Study in Healthy Volunteers for an Analytically Highly Similar Pegfilgrastim Abstract Abstract A phase 1 pharmacokinetic (PK) and pharmacodynamic (PD) study was conducted to demonstrate similarity of a proposed pegfilgrastim biosimilar to its reference ... |
PMC7092621 | core_pubmed_pmc | Efficient Delivery of Triptolide Plus a miR-30-5p Inhibitor Through the Use of Near Infrared Laser Responsive or CADY Modified MSNs for Efficacy in Rheumatoid Arthritis Therapeutics | Efficient Delivery of Triptolide Plus a miR-30-5p Inhibitor Through the Use of Near Infrared Laser Responsive or CADY Modified MSNs for Efficacy in Rheumatoid Arthritis Therapeutics Abstract Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease for which treatment focuses on suppressing an overactive i... |
PMC4112823 | core_pubmed_pmc | Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study | Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study Abstract Abstract Background Alternatives to treatment for malaria treatment of travellers are needed in the USA and in Europe for travellers who return with severe malaria infections. The obj... |
PMC11373227 | core_pubmed_pmc | First-in-human, randomized, double-blind, placebo-controlled, single and multiple ascending doses clinical study to assess the safety, tolerability, and pharmacokinetics of cipargamin administered intravenously in healthy adults | First-in-human, randomized, double-blind, placebo-controlled, single and multiple ascending doses clinical study to assess the safety, tolerability, and pharmacokinetics of cipargamin administered intravenously in healthy adults Abstract ABSTRACT This first-in-human study assessed safety, tolerability, and pharmacokine... |
PMC11995007 | core_pubmed_pmc | Clinical and Translational Results from PORTER, a Multicohort Phase I Platform Trial of Combination Immunotherapy in Metastatic Castration-Resistant Prostate Cancer | Clinical and Translational Results from PORTER, a Multicohort Phase I Platform Trial of Combination Immunotherapy in Metastatic Castration-Resistant Prostate Cancer Abstract Abstract Purpose: Current immune checkpoint therapies offer limited benefits for metastatic castration-resistant prostate cancer. Novel combinatio... |
PMC11560753 | core_pubmed_pmc | Comparative pharmacokinetics of porcine and human anti-influenza hemagglutinin monoclonal antibodies in outbred pigs and minipigs | Comparative pharmacokinetics of porcine and human anti-influenza hemagglutinin monoclonal antibodies in outbred pigs and minipigs Abstract Abstract Assessing the pharmacokinetics of monoclonal antibodies (mAbs) in relevant animal models is essential for designing improved formulations and developing mAb delivery platfo... |
PMC7598109 | core_pubmed_pmc | Comparative pharmacokinetics of chlortetracycline, tetracycline, minocycline, and tigecycline in broiler chickens | Comparative pharmacokinetics of chlortetracycline, tetracycline, minocycline, and tigecycline in broiler chickens Abstract Abstract Tetracyclines continue to be important antimicrobials in veterinary medicine. However, the pharmacokinetics ( PK ) of tigecycline ( TIG ) and minocycline ( MIN ) in broiler chickens has no... |
PMC6204872 | core_pubmed_pmc | Distinct features of rabbit and human adipose-derived mesenchymal stem cells: implications for biotechnology and translational research | Distinct features of rabbit and human adipose-derived mesenchymal stem cells: implications for biotechnology and translational research Abstract Introduction Owing to their similarity with humans, rabbits are useful for multiple applications in biotechnology and translational research from basic to preclinical studies.... |
PMC10691958 | core_pubmed_pmc | The Pharmacokinetics, Safety and Tolerability of Aclidinium Bromide 400 μg Administered by Inhalation as Single and Multiple (Twice Daily) Doses in Healthy Chinese Participants | The Pharmacokinetics, Safety and Tolerability of Aclidinium Bromide 400 μg Administered by Inhalation as Single and Multiple (Twice Daily) Doses in Healthy Chinese Participants Abstract Abstract Purpose To date, aclidinium pharmacokinetic (PK) studies have focused on Caucasian populations, and no data are available for... |
PMC4394617 | core_pubmed_pmc | Modeling and Simulation Approaches for Cardiovascular Function and Their Role in Safety Assessment | Modeling and Simulation Approaches for Cardiovascular Function and Their Role in Safety Assessment Abstract Systems pharmacology modeling and pharmacokinetic-pharmacodynamic (PK/PD) analysis of drug-induced effects on cardiovascular (CV) function plays a crucial role in understanding the safety risk of new drugs. The a... |
PMC10824963 | core_pubmed_pmc | Linoleate-pazopanib conjugation as active pharmacological ingredient to abolish hepatocellular carcinoma growth | Linoleate-pazopanib conjugation as active pharmacological ingredient to abolish hepatocellular carcinoma growth Abstract Abstract Small molecule compounds targeting multiple kinases involved in neoangiogenesis have shown survival benefits in patients with unresectable hepatocellular carcinoma (HCC). Nonetheless, despit... |
PMC9640280 | core_pubmed_pmc | Pimavanserin Exposure-Response Analyses in Patients With Schizophrenia | Pimavanserin Exposure-Response Analyses in Patients With Schizophrenia Abstract Abstract Purpose/Background Pimavanserin is a selective serotonin 5-HT 2A receptor inverse agonist/antagonist being investigated in patients with negative symptoms of schizophrenia. This analysis aimed to characterize exposure-response rela... |
PMC3400037 | core_pubmed_pmc | Application of a single-objective, hybrid genetic algorithm approach to pharmacokinetic model building | Application of a single-objective, hybrid genetic algorithm approach to pharmacokinetic model building Abstract Abstract A limitation in traditional stepwise population pharmacokinetic model building is the difficulty in handling interactions between model components. To address this issue, a method was previously intr... |
PMC12220247 | core_pubmed_pmc | Paxlovid for the treatment of severe or critical COVID-19 in children | Paxlovid for the treatment of severe or critical COVID-19 in children Abstract Abstract Background Paxlovid, known for its efficacy against SARS-CoV-2, is currently limited in its use for treating pediatric COVID-19, particularly in severe or critical cases. Methods We conducted a study within a single-center, prospect... |
PMC6457131 | core_pubmed_pmc | Intranasal insulin therapy reverses hippocampal dendritic injury and cognitive impairment in a model of HIV-associated neurocognitive disorders in EcoHIV-infected mice | Intranasal insulin therapy reverses hippocampal dendritic injury and cognitive impairment in a model of HIV-associated neurocognitive disorders in EcoHIV-infected mice Abstract Supplemental Digital Content is available in the text Keywords: EcoHIV, fear conditioning, HIV-associated neurocognitive impairment, insulin, i... |
PMC9932319 | core_pubmed_pmc | In vitro to in vivo acetaminophen hepatotoxicity extrapolation using classical schemes, pharmacodynamic models and a multiscale spatial-temporal liver twin | In vitro to in vivo acetaminophen hepatotoxicity extrapolation using classical schemes, pharmacodynamic models and a multiscale spatial-temporal liver twin Abstract Abstract In vitro to in vivo extrapolation represents a critical challenge in toxicology. In this paper we explore extrapolation strategies for acetaminoph... |
PMC11612344 | core_pubmed_pmc | Molecular docking and in silico analysis of the pharmacokinetics, toxicological profile and differential gene expression of bioactive compounds from Cyrtopodium glutiniferum | Molecular docking and in silico analysis of the pharmacokinetics, toxicological profile and differential gene expression of bioactive compounds from Cyrtopodium glutiniferum Abstract The genus Cyrtopodium , from the Orchidaceae family, is widely used for its therapeutic properties in the treatment of tuberculosis, absc... |
PMC8919711 | core_pubmed_pmc | Acute Effects of Liothyronine Administration on Cardiovascular System and Energy Metabolism in Healthy Volunteers | Acute Effects of Liothyronine Administration on Cardiovascular System and Energy Metabolism in Healthy Volunteers Abstract Context The pharmacokinetics of liothyronine causes concerns for cardiovascular toxicity. While the effects of sustained increase in serum T3 concentrations are well described, little is known on t... |
PMC7877830 | core_pubmed_pmc | Coproporphyrin I Can Serve as an Endogenous Biomarker for OATP1B1 Inhibition: Assessment Using a Glecaprevir/Pibrentasvir Clinical Study | Coproporphyrin I Can Serve as an Endogenous Biomarker for OATP1B1 Inhibition: Assessment Using a Glecaprevir/Pibrentasvir Clinical Study Abstract Abstract Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 are involved in the disposition of a variety of commonly prescribed drugs. The evaluation of OATP1B1/1B... |
PMC7083463 | core_pubmed_pmc | Quantification of total and unbound cefuroxime in plasma by ultra‐performance liquid chromatography tandem mass spectrometry in a cohort of critically ill patients with hypoalbuminemia and renal failure | Quantification of total and unbound cefuroxime in plasma by ultra‐performance liquid chromatography tandem mass spectrometry in a cohort of critically ill patients with hypoalbuminemia and renal failure Abstract Abstract Background Pharmacokinetic studies of cefuroxime by ultra‐performance liquid chromatography tandem ... |
PMC5375969 | core_pubmed_pmc | Influence of Ivabradine on the Anticonvulsant Action of Four Classical Antiepileptic Drugs Against Maximal Electroshock-Induced Seizures in Mice | Influence of Ivabradine on the Anticonvulsant Action of Four Classical Antiepileptic Drugs Against Maximal Electroshock-Induced Seizures in Mice Abstract Abstract Although the role of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels in neuronal excitability and synaptic transmission is still unclear, ... |
PMC11621205 | core_pubmed_pmc | Semi-mechanistic population pharmacokinetic modeling of DZIF-10c, a neutralizing antibody against SARS-Cov-2: predicting systemic and lung exposure following inhaled and intravenous administration | Semi-mechanistic population pharmacokinetic modeling of DZIF-10c, a neutralizing antibody against SARS-Cov-2: predicting systemic and lung exposure following inhaled and intravenous administration Abstract DZIF-10c (BI 767551) is a recombinant human monoclonal antibody of the IgG1 kappa isotype. It acts as a SARS-CoV-2... |
PMC6768916 | core_pubmed_pmc | Population pharmacokinetics of fedratinib in patients with myelofibrosis, polycythemia vera, and essential thrombocythemia | Population pharmacokinetics of fedratinib in patients with myelofibrosis, polycythemia vera, and essential thrombocythemia Abstract Abstract Purpose Fedratinib (SAR302503, TG101348) is an orally administered Janus kinase (JAK) 2-selective inhibitor that is being developed for the treatment of patients with myelofibrosi... |
PMC3813201 | core_pubmed_pmc | Comparative Pharmacokinetics of Levofloxacin in Healthy Volunteers and in Patients Suffering from Typhoid Fever | Comparative Pharmacokinetics of Levofloxacin in Healthy Volunteers and in Patients Suffering from Typhoid Fever Abstract Abstract The aim of this study was to characterize the effect of typhoid fever on pharmacokinetic parameters of levofloxacin (LF) and compare the pharmacokinetic parameters of the said antibiotic in ... |
PMC8195962 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine | Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine Abstract Introduction Lasmiditan is a selective serotonin (5-HT1F) receptor agonist approved in the US for the acute treatment ofmigraine in adults. This phase I, open-label, two-cohort study assessed the pharmacokinetics (PK),... |
PMC9101560 | core_pubmed_pmc | Hyperoside: A Review of Its Structure, Synthesis, Pharmacology, Pharmacokinetics and Toxicity | Hyperoside: A Review of Its Structure, Synthesis, Pharmacology, Pharmacokinetics and Toxicity Abstract Abstract Hyperoside is an active ingredient in plants, such as Hypericum monogynum in Hypericaceae, Crataegus pinnatifida in Rosaceae and Polygonum aviculare in Polygonaceae. Its pharmacologic effects include preventi... |
PMC11933424 | core_pubmed_pmc | An automated classification pipeline for tables in pharmacokinetic literature | An automated classification pipeline for tables in pharmacokinetic literature Abstract Pharmacokinetic (PK) models are essential for optimising drug candidate selection and dosing regimens in drug development. Preclinical and population PK models benefit from integrating prior knowledge from existing compounds. While t... |
PMC4070054 | core_pubmed_pmc | Evaluation of novel Saquinavir analogs for resistance mutation compatibility and potential as an HIV-Protease inhibitor drug | Evaluation of novel Saquinavir analogs for resistance mutation compatibility and potential as an HIV-Protease inhibitor drug Abstract A fundamental issue related to therapy of HIV-1 infection is the emergence of viral mutations which severely limits the long term efficiency of the HIV-protease (HIV-PR) inhibitors. Deve... |
PMC5189627 | core_pubmed_pmc | A Phase I Study of the Safety and Pharmacokinetics of Higher-Dose Icotinib in Patients With Advanced Non-Small Cell Lung Cancer | A Phase I Study of the Safety and Pharmacokinetics of Higher-Dose Icotinib in Patients With Advanced Non-Small Cell Lung Cancer Abstract Abstract Lessons Learned This phase I study evaluated the maximum tolerated dose, dose-limiting toxicities, safety, pharmacokinetics, and efficacy of icotinib with a starting dose of ... |
PMC4014136 | core_pubmed_pmc | The role of prothrombin complex concentrates in reversal of target specific anticoagulants | The role of prothrombin complex concentrates in reversal of target specific anticoagulants Abstract Abstract Over the past several years a new era for patients requiring anticoagulation has arrived. The approval of new target specific oral anticoagulants offers practitioners several advantages over traditionally used v... |
PMC5442105 | core_pubmed_pmc | Preparation, characterization and pharmacokinetics of cyadox nanosuspension | Preparation, characterization and pharmacokinetics of cyadox nanosuspension Abstract An increase in number of newly developed synthetic drugs displays bioavailability constraints because of poor water solubility. Nanosuspensions formulation may help to overwhelm these problems by increasing dissolution velocity and sat... |
PMC10794771 | core_pubmed_pmc | Pharmacokinetics of florfenicol and its metabolite florfenicol amine in the plasma, urine, and feces of fattening male donkeys following single oral administration | Pharmacokinetics of florfenicol and its metabolite florfenicol amine in the plasma, urine, and feces of fattening male donkeys following single oral administration Abstract Florfenicol (FF) is a commonly used antibacterial agent in animals. We investigated the pharmacokinetics of FF and its metabolite florfenicol amine... |
PMC5070617 | core_pubmed_pmc | Characterization and Bioavailability of Wogonin by Different Administration Routes in Beagles | Characterization and Bioavailability of Wogonin by Different Administration Routes in Beagles Abstract Abstract Background With the gradually accumulating research on pharmacological activity of wogonin, the in vitro analysis research on wogonin has become more and more popular, but there are very few reports about in ... |
PMC10179782 | core_pubmed_pmc | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation | Clarithromycin-Loaded Submicron-Sized Carriers: Pharmacokinetics and Pharmacodynamic Evaluation Abstract Abstract The current study aims to improve clarithromycin bioavailability and effectiveness in complicated intra-abdominal infection management. Therefore, clarithromycin-loaded submicron dual lipid carriers (CLA-DL... |
PMC6851181 | core_pubmed_pmc | Pharmacokinetic parameters of ifosfamide in mouse pre-administered with grapefruit juice or naringin | Pharmacokinetic parameters of ifosfamide in mouse pre-administered with grapefruit juice or naringin Abstract Grapefruit juice (GFJ) and naringin when consumed previously or together with medications may alter their bioavailavility and consequently the clinical effect. Ifosfamide (IF) is an antitumoral agent prescribed... |
PMC11473700 | core_pubmed_pmc | An enhanced intracellular delivery platform based on a distant diphtheria toxin homolog that evades pre-existing antitoxin antibodies | An enhanced intracellular delivery platform based on a distant diphtheria toxin homolog that evades pre-existing antitoxin antibodies Abstract Targeted intracellular delivery of therapeutic proteins remains a significant unmet challenge in biotechnology. A promising approach is to leverage the intrinsic capabilities of... |
PMC5760933 | core_pubmed_pmc | Quantitation of bivalirudin, a novel anticoagulant peptide, in human plasma by LC–MS/MS: Method development, validation and application to pharmacokinetics | Quantitation of bivalirudin, a novel anticoagulant peptide, in human plasma by LC–MS/MS: Method development, validation and application to pharmacokinetics Abstract Abstract A rapid and sensitive method based on liquid chromatography–tandem mass spectrometry (LC–MS/MS) for the determination of a novel anticoagulant pep... |
PMC9317288 | core_pubmed_pmc | Adverse Drug Reactions in Relation to Clozapine Plasma Levels: A Systematic Review | Adverse Drug Reactions in Relation to Clozapine Plasma Levels: A Systematic Review Abstract Abstract Clozapine is the gold standard for treatment-resistant schizophrenia. Serious and even life-threatening adverse effects, mostly granulocytopenia, myocarditis, and constipation, are of great clinical concern and constitu... |
PMC3652823 | core_pubmed_pmc | Improvement of Intestinal Absorption of Forsythoside A and Chlorogenic Acid by Different Carboxymethyl Chitosan and Chito-oligosaccharide, Application to Flos Lonicerae - Fructus Forsythiae Herb Couple Preparations | Improvement of Intestinal Absorption of Forsythoside A and Chlorogenic Acid by Different Carboxymethyl Chitosan and Chito-oligosaccharide, Application to Flos Lonicerae - Fructus Forsythiae Herb Couple Preparations Abstract The current study aims to investigate the effect of chitosan derivatives on the intestinal absor... |
PMC12272481 | core_pubmed_pmc | Effectorless Fc-fusion improves FLT3L drug-like properties for cancer immunotherapy combinations | Effectorless Fc-fusion improves FLT3L drug-like properties for cancer immunotherapy combinations Abstract Summary Background Conventional dendritic cells (cDCs), are central to antitumour immunity, but their low prevalence in tumours limits the efficacy of immunotherapies. FLT3L is a key growth factor regulating cDCs d... |
PMC11738990 | core_pubmed_pmc | A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models | A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models Abstract Abstract Idiopathic pulmonary fibrosis (IPF) is an aggressive interstitial lung disease with a high mortality rate. Putative drug targets in IPF have failed to translate into effective therapies at the clinical level. We identi... |
PMC12246932 | core_pubmed_pmc | HORNBILL: A First-in-Human Phase I/IIa Study of the Safety, Tolerability, and Early Pharmacodynamics of BI 764524 for Diabetic Macular Ischemia | HORNBILL: A First-in-Human Phase I/IIa Study of the Safety, Tolerability, and Early Pharmacodynamics of BI 764524 for Diabetic Macular Ischemia Abstract Abstract Objective To report safety and early pharmacodynamic results from a first-in-human trial of intravitreal (IVT) anti-semaphorin 3A antibody in participants wit... |
PMC3561686 | core_pubmed_pmc | Pharmacokinetic Interaction Between Prasugrel and Ritonavir in Healthy Volunteers | Pharmacokinetic Interaction Between Prasugrel and Ritonavir in Healthy Volunteers Abstract Abstract The new anti-aggregating agent prasugrel is bioactivated by cytochromes P450 (CYP) 3A and 2B6. Ritonavir is a potent CYP3A inhibitor and was shown in vitro as a CYP2B6 inhibitor. The aim of this open-label cross-over stu... |
PMC11574399 | core_pubmed_pmc | Phase I study of a recombinant attenuated oncolytic virus, MEDI5395 (NDV–GM-CSF), administered systemically in combination with durvalumab in patients with advanced solid tumors | Phase I study of a recombinant attenuated oncolytic virus, MEDI5395 (NDV–GM-CSF), administered systemically in combination with durvalumab in patients with advanced solid tumors Abstract Abstract Background MEDI5395 is a recombinant attenuated Newcastle disease virus engineered to express a human granulocyte-macrophage... |
PMC8246794 | core_pubmed_pmc | Pharmacologic effects of oseltamivir in immunocompromised adult patients as assessed by population PK/PD analysis and drug‐disease modelling for dosing regimen optimization | Pharmacologic effects of oseltamivir in immunocompromised adult patients as assessed by population PK/PD analysis and drug‐disease modelling for dosing regimen optimization Abstract Aim Pharmacologic effects were analysed to determine a dose recommendation for oseltamivir in immunocompromised (IC) adults with influenza... |
PMC9467298 | core_pubmed_pmc | Study on Integrated Pharmacokinetics of the Component-Based Chinese Medicine of Ginkgo biloba Leaves Based on Nanocrystalline Solid Dispersion Technology | Study on Integrated Pharmacokinetics of the Component-Based Chinese Medicine of Ginkgo biloba Leaves Based on Nanocrystalline Solid Dispersion Technology Abstract Abstract Background To improve the dissolution and bioavailability of the component-based Chinese medicine of Ginkgo biloba leaves (GBCCM), a novel nanocryst... |
PMC5845054 | core_pubmed_pmc | A generic whole body physiologically based pharmacokinetic model for therapeutic proteins in PK-Sim | A generic whole body physiologically based pharmacokinetic model for therapeutic proteins in PK-Sim Abstract Proteins are an increasingly important class of drugs used as therapeutic as well as diagnostic agents. A generic physiologically based pharmacokinetic (PBPK) model was developed in order to represent at whole b... |
PMC8576757 | core_pubmed_pmc | Chemistry, Biosynthesis, Physicochemical and Biological Properties of Rubiadin: A Promising Natural Anthraquinone for New Drug Discovery and Development | Chemistry, Biosynthesis, Physicochemical and Biological Properties of Rubiadin: A Promising Natural Anthraquinone for New Drug Discovery and Development Abstract Abstract Anthraquinones (AQs) are found in a variety of consumer products, including foods, nutritional supplements, drugs, and traditional medicines, and hav... |
PMC6115778 | core_pubmed_pmc | Toxicity and Pharmacokinetic Studies of Lidocaine and Its Active Metabolite, Monoethylglycinexylidide, in Goat Kids | Toxicity and Pharmacokinetic Studies of Lidocaine and Its Active Metabolite, Monoethylglycinexylidide, in Goat Kids Abstract Abstract Simple Summary Disbudding is becoming a routine husbandry procedure in goat farms even though it is a painful procedure without appropriate pain relief. One of the ways to alleviate or m... |
PMC12300523 | core_pubmed_pmc | Development and Validation of Bioanalytical LC–MS/MS Method for Pharmacokinetic Assessment of Amoxicillin and Clavulanate in Human Plasma | Development and Validation of Bioanalytical LC–MS/MS Method for Pharmacokinetic Assessment of Amoxicillin and Clavulanate in Human Plasma Abstract Background/Objectives : We developed and validated a robust and simple LC–MS/MS method for the simultaneous quantification of amoxicillin and clavulanate in human plasma rel... |
PMC4669428 | core_pubmed_pmc | Comparison of different serum sample extraction methods and their suitability for mass spectrometry analysis | Comparison of different serum sample extraction methods and their suitability for mass spectrometry analysis Abstract Mass spectrometry has been widely used, particularly in pharmacokinetic investigations and for therapeutic drug monitoring purposes. Like any other analytical method some difficulties exist in employing... |
PMC3599276 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study | Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study Abstract Abstract Background The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma patho... |
PMC2996318 | core_pubmed_pmc | Modeling Mechanisms of In Vivo Variability in Methotrexate Accumulation and Folate Pathway Inhibition in Acute Lymphoblastic Leukemia Cells | Modeling Mechanisms of In Vivo Variability in Methotrexate Accumulation and Folate Pathway Inhibition in Acute Lymphoblastic Leukemia Cells Abstract Methotrexate (MTX) is widely used for the treatment of childhood acute lymphoblastic leukemia (ALL). The accumulation of MTX and its active metabolites, methotrexate polyg... |
PMC11734454 | core_pubmed_pmc | In vivo brain delivery of BBB-enabled iduronate 2-sulfatase in rats | In vivo brain delivery of BBB-enabled iduronate 2-sulfatase in rats Abstract Background Iduronate-2-sulfatase (IDS) deficiency (MPS II; Hunter syndrome) is a disorder that exhibits peripheral and CNS pathology. The blood brain barrier (BBB) prevents systemic enzyme replacement therapy (ERT) from alleviating CNS patholo... |
PMC4072877 | core_pubmed_pmc | In vivo interactions of continuous flucloxacillin infusion and high-dose oral rifampicin in the serum of 15 patients with bone and soft tissue infections due to Staphylococcus aureus - a methodological and pilot study | In vivo interactions of continuous flucloxacillin infusion and high-dose oral rifampicin in the serum of 15 patients with bone and soft tissue infections due to Staphylococcus aureus - a methodological and pilot study Abstract Background Increased antibiotic resistance against Staphylococcus aureus and low penetration ... |
PMC4861370 | core_pubmed_pmc | Phase I Study of the Prolactin Receptor Antagonist LFA102 in Metastatic Breast and Castration-Resistant Prostate Cancer | Phase I Study of the Prolactin Receptor Antagonist LFA102 in Metastatic Breast and Castration-Resistant Prostate Cancer Abstract Abstract Lessons Learned Despite evidence for a role for prolactin signaling in breast and prostate tumorigenesis, a prolactin receptor-binding monoclonal antibody has not produced clinical e... |
PMC11142125 | core_pubmed_pmc | Comparative analysis of within-host dynamics of acute infection and viral rebound dynamics in postnatally SHIV-infected ART-treated infant rhesus macaques | Comparative analysis of within-host dynamics of acute infection and viral rebound dynamics in postnatally SHIV-infected ART-treated infant rhesus macaques Abstract Viral dynamics of acute HIV infection and HIV rebound following suspension of antiretroviral therapy may be qualitatively similar but must differ given, for... |
PMC4911330 | core_pubmed_pmc | Anthelmintic closantel enhances bacterial killing of polymyxin B against multidrug-resistant Acinetobacter baumannii | Anthelmintic closantel enhances bacterial killing of polymyxin B against multidrug-resistant Acinetobacter baumannii Abstract Polymyxins, an old class of antibiotics, are currently used as the last resort for the treatment of multidrug-resistant (MDR) Acinetobacter baumannii . However, recent pharmacokinetic and pharma... |
PMC4779506 | core_pubmed_pmc | Characterization of IXINITY® (Trenonacog Alfa), a Recombinant Factor IX with Primary Sequence Corresponding to the Threonine-148 Polymorph | Characterization of IXINITY® (Trenonacog Alfa), a Recombinant Factor IX with Primary Sequence Corresponding to the Threonine-148 Polymorph Abstract Abstract The goal of these studies was to extensively characterize the first recombinant FIX therapeutic corresponding to the threonine-148 (Thr-148) polymorph, IXINITY (tr... |
PMC5418314 | core_pubmed_pmc | First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors | First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors Abstract Summary Introduction This was an open-label, dose escalation (3 + 3 design), Phase I study of SOR-C13 in patients with advanced tumors of epithelial origin. Primary objectives were to assess safet... |
PMC4599715 | core_pubmed_pmc | Improvement of in vivo efficacy of recombinant human erythropoietin by encapsulation in PEG–PLA micelle | Improvement of in vivo efficacy of recombinant human erythropoietin by encapsulation in PEG–PLA micelle Abstract To improve the pharmacokinetics and stability of recombinant human erythropoietin (rhEPO), rhEPO was successfully formulated into poly(ethylene glycol)–poly(d,l-lactide) (PEG–PLA) di-block copolymeric micell... |
PMC9811456 | core_pubmed_pmc | NPP-669, a Novel Broad-Spectrum Antiviral Therapeutic with Excellent Cellular Uptake, Antiviral Potency, Oral Bioavailability, Preclinical Efficacy, and a Promising Safety Margin | NPP-669, a Novel Broad-Spectrum Antiviral Therapeutic with Excellent Cellular Uptake, Antiviral Potency, Oral Bioavailability, Preclinical Efficacy, and a Promising Safety Margin Abstract DNA viruses are responsible for many diseases in humans. Current treatments are often limited by toxicity, as in the case of cidofov... |
PMC12112975 | core_pubmed_pmc | Sedative Agents, Synthetic Torpor, and Long-Haul Space Travel—A Systematic Review | Sedative Agents, Synthetic Torpor, and Long-Haul Space Travel—A Systematic Review Abstract Abstract Background: With renewed interest in long-duration space missions, there is growing exploration into synthetic torpor as a countermeasure to mitigate physiological stressors. Sedative agents, particularly those used in c... |
PMC7076355 | core_pubmed_pmc | Semi-Mechanism-Based Pharmacokinetic-Toxicodynamic Model of Oxaliplatin-Induced Acute and Chronic Neuropathy | Semi-Mechanism-Based Pharmacokinetic-Toxicodynamic Model of Oxaliplatin-Induced Acute and Chronic Neuropathy Abstract Oxaliplatin (L-OHP) is widely prescribed for treating gastroenterological cancer. L-OHP-induced peripheral neuropathy is a critical toxic effect that limits the dosage of L-OHP. An ideal chemotherapeuti... |
PMC10907863 | core_pubmed_pmc | Preclinical evaluation of engineered L-asparaginase variants to improve the treatment of Acute Lymphoblastic Leukemia | Preclinical evaluation of engineered L-asparaginase variants to improve the treatment of Acute Lymphoblastic Leukemia Abstract Highlights • When compared to the wild-type EcA, KHY-17 and KHYW-17 EcA variants had comparable asparaginase activity at 37 °C. Both the variants showed approximately 24-fold lower glutaminase ... |
PMC3881071 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of febuxostat under fasting conditions in healthy individuals | Pharmacokinetics and pharmacodynamics of febuxostat under fasting conditions in healthy individuals Abstract The aim of the present study was to investigate the pharmacokinetic and pharmacodynamic characteristics of febuxostat following the administration of single and multiple oral doses under fasting conditions to he... |
PMC10610861 | core_pubmed_pmc | Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) | Strategies in the Design and Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) Abstract Abstract AIDS ( acquired immunodeficiency syndrome ) is a potentially life-threatening infectious disease caused by human immunodeficiency virus (HIV). To date, thousands of people have lost their lives annuall... |
PMC4716096 | core_pubmed_pmc | Pharmacokinetics of tacrolimus according to body composition in recipients of kidney transplants | Pharmacokinetics of tacrolimus according to body composition in recipients of kidney transplants Abstract Abstract Background Currently, the dosage of tacrolimus used after transplantation is based on the patient's body weight. However, there is a low correlation between body weight and body composition in kidney trans... |
PMC7066709 | core_pubmed_pmc | The McCAVE Trial: Vanucizumab plus mFOLFOX‐6 Versus Bevacizumab plus mFOLFOX‐6 in Patients with Previously Untreated Metastatic Colorectal Carcinoma (mCRC) | The McCAVE Trial: Vanucizumab plus mFOLFOX‐6 Versus Bevacizumab plus mFOLFOX‐6 in Patients with Previously Untreated Metastatic Colorectal Carcinoma (mCRC) Abstract Abstract Background Bevacizumab, a VEGF‐A inhibitor, in combination with chemotherapy, has proven to increase progression‐free survival (PFS) and overall s... |
PMC8667992 | core_pubmed_pmc | Ceftriaxone-induced Encephalopathy: A Pharmacokinetic Approach | Ceftriaxone-induced Encephalopathy: A Pharmacokinetic Approach Abstract We report a case of ceftriaxone-induced encephalopathy correlated with a high concentration of the drug in cerebrospinal fluid (CSF). Cephalosporin neurotoxicity is increasingly reported, especially in association with fourth-generation cephalospor... |
PMC5117956 | core_pubmed_pmc | Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats | Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats Abstract Abstract Background The intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicate... |
PMC8230268 | core_pubmed_pmc | The Role of PK/PD Analysis in the Development and Evaluation of Antimicrobials | The Role of PK/PD Analysis in the Development and Evaluation of Antimicrobials Abstract Pharmacokinetic/pharmacodynamic (PK/PD) analysis has proved to be very useful to establish rational dosage regimens of antimicrobial agents in human and veterinary medicine. Actually, PK/PD studies are included in the European Medic... |
PMC9755924 | core_pubmed_pmc | Phase III dose selection of marzeptacog alfa (activated) informed by population pharmacokinetic modeling: A novel hemostatic drug | Phase III dose selection of marzeptacog alfa (activated) informed by population pharmacokinetic modeling: A novel hemostatic drug Abstract Abstract Marzeptacog alfa (activated) (MarzAA) is an activated recombinant human FVII (rFVIIa) variant developed as subcutaneous (s.c.) administration for the treatment or preventio... |
PMC12220787 | core_pubmed_pmc | Effect of CYP2D6 and ABCB1 polymorphisms on pharmacokinetics and efficacy of aripiprazole in pediatric tic disorders | Effect of CYP2D6 and ABCB1 polymorphisms on pharmacokinetics and efficacy of aripiprazole in pediatric tic disorders Abstract Background Aripiprazole (ARI) is the first-line treatment for tic disorders (TD). Cytochrome P450(CYP)2D6 (CYP2D6) and ATP-binding cassette, sub-family B, member 1 (ABCB1) transporter are involv... |
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