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PMC5343769 | core_pubmed_pmc | N -Glycoprofiling Analysis for Carbohydrate Composition and Site-Occupancy Determination in a Poly-Glycosylated Protein: Human Thyrotropin of Different Origins | N -Glycoprofiling Analysis for Carbohydrate Composition and Site-Occupancy Determination in a Poly-Glycosylated Protein: Human Thyrotropin of Different Origins Abstract Abstract Human thyrotropin (hTSH) is a glycoprotein with three potential glycosylation sites: two in the α-subunit and one in the β-subunit. These site... |
PMC9598655 | core_pubmed_pmc | Combination Regimens with Colistin Sulfate versus Colistin Sulfate Monotherapy in the Treatment of Infections Caused by Carbapenem-Resistant Gram-Negative Bacilli | Combination Regimens with Colistin Sulfate versus Colistin Sulfate Monotherapy in the Treatment of Infections Caused by Carbapenem-Resistant Gram-Negative Bacilli Abstract Carbapenem-resistant organisms (CRO) have become a global concern because of the limited antibiotic treatment options for CRO infections. Colistin s... |
PMC4909673 | core_pubmed_pmc | Besifloxacin: Efficacy and Safety in Treatment and Prevention of Ocular Bacterial Infections | Besifloxacin: Efficacy and Safety in Treatment and Prevention of Ocular Bacterial Infections Abstract This comprehensive review summarizes the mechanism of action, pharmacokinetics, efficacy, and safety of besifloxacin ophthalmic suspension, 0.6% and examines its role in the treatment of ocular surface bacterial infect... |
PMC10180502 | core_pubmed_pmc | Mechanochemical Synthesis and Molecular Docking Studies of New Azines Bearing Indole as Anticancer Agents | Mechanochemical Synthesis and Molecular Docking Studies of New Azines Bearing Indole as Anticancer Agents Abstract Abstract The development of new approaches for the synthesis of new bioactive heterocyclic derivatives is of the utmost importance for pharmaceutical industry. In this regard, the present study reports the... |
PMC12012807 | core_pubmed_pmc | Phase I study of oral metronomic gemcitabine (D07001) in patients with advanced solid tumors | Phase I study of oral metronomic gemcitabine (D07001) in patients with advanced solid tumors Abstract Abstract Background D07001-F4 is an absorption-enhanced oral gemcitabine developed in liquid formulation and adjusted to D07001-softgel capsules. We conducted 2 phase 1 studies to evaluate the dose-limiting toxicity (D... |
PMC2990578 | core_pubmed_pmc | Phase II trial of sagopilone, a novel epothilone analog in metastatic melanoma | Phase II trial of sagopilone, a novel epothilone analog in metastatic melanoma Abstract Abstract Background: Sagopilone is a novel fully synthetic epothilone with promising preclinical activity and a favourable toxicity profile in phase I testing. Methods: A phase II pharmacokinetic and efficacy trial was conducted in ... |
PMC5892672 | core_pubmed_pmc | Bioequivalent pharmacokinetics for generic and originator hepatitis C direct-acting antivirals | Bioequivalent pharmacokinetics for generic and originator hepatitis C direct-acting antivirals Abstract Abstract Mass production of low-cost, generic direct-acting antivirals (DAAs) will be required to achieve targets of eliminating hepatitis C (HCV) by 2030. The pharmaceutical companies Gilead and Bristol-Myers Squibb... |
PMC8309207 | core_pubmed_pmc | Comparison of Pharmacokinetics and Anti-Pulmonary Fibrosis-Related Effects of Sulforaphane and Sulforaphane N -acetylcysteine | Comparison of Pharmacokinetics and Anti-Pulmonary Fibrosis-Related Effects of Sulforaphane and Sulforaphane N -acetylcysteine Abstract Abstract Sulforaphane (SFN), belonging to the isothiocyanate family, has received attention owing to its beneficial activities, including chemopreventive and antifibrotic effects. As su... |
PMC11978648 | core_pubmed_pmc | Comparison of the pharmacokinetic variations of different concentrations of ropivacaine used for serratus anterior plane block in patients undergoing thoracoscopic lobectomy: a population pharmacokinetics analysis | Comparison of the pharmacokinetic variations of different concentrations of ropivacaine used for serratus anterior plane block in patients undergoing thoracoscopic lobectomy: a population pharmacokinetics analysis Abstract Objective Ropivacaine serratus anterior plane block is widely used in clinical analgesia in patie... |
PMC4931877 | core_pubmed_pmc | The γ -Secretase Modulator, BMS-932481, Modulates A β Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers | The γ -Secretase Modulator, BMS-932481, Modulates A β Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers Abstract Abstract The pharmacokinetics, pharmacodynamics, safety, and tolerability of BMS-932481, a γ -secretase modulator (GSM), were tested in healthy young and elderly volunteers after single an... |
PMC8608957 | core_pubmed_pmc | Pain Relieving and Neuroprotective Effects of Non-opioid Compound, DDD-028, in the Rat Model of Paclitaxel-Induced Neuropathy | Pain Relieving and Neuroprotective Effects of Non-opioid Compound, DDD-028, in the Rat Model of Paclitaxel-Induced Neuropathy Abstract Abstract Chemotherapy-induced neuropathy (CIN) is a major dose-limiting side effect of anticancer therapy that can compel therapy discontinuation. Inadequate analgesic efficacy of curre... |
PMC7448256 | core_pubmed_pmc | Simultaneous Determination of Six Uncaria Alkaloids in Mouse Blood by UPLC–MS/MS and Its Application in Pharmacokinetics and Bioavailability | Simultaneous Determination of Six Uncaria Alkaloids in Mouse Blood by UPLC–MS/MS and Its Application in Pharmacokinetics and Bioavailability Abstract A specific ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed for the simultaneous determination of six Uncaria alkalo... |
PMC4383552 | core_pubmed_pmc | Pharmacokinetics and Bioavailability of a Therapeutic Enzyme (Idursulfase) in Cynomolgus Monkeys after Intrathecal and Intravenous Administration | Pharmacokinetics and Bioavailability of a Therapeutic Enzyme (Idursulfase) in Cynomolgus Monkeys after Intrathecal and Intravenous Administration Abstract Intravenous enzyme replacement therapy with iduronate-2-sulfatase is an approved treatment for Hunter syndrome, however, conventional intravenous delivery cannot tre... |
PMC10707468 | core_pubmed_pmc | Pharmacokinetics of Novel Dopamine Transporter Inhibitor CE-123 and Modafinil with a Focus on Central Nervous System Distribution | Pharmacokinetics of Novel Dopamine Transporter Inhibitor CE-123 and Modafinil with a Focus on Central Nervous System Distribution Abstract S -CE-123, a novel dopamine transporter inhibitor, has emerged as a potential candidate for cognitive enhancement. The objective of this study was to compare the tissue distribution... |
PMC9800192 | core_pubmed_pmc | Pharmacodynamics and acute toxicity studies of Shangke Jiegu tablet with or without cinnabar | Pharmacodynamics and acute toxicity studies of Shangke Jiegu tablet with or without cinnabar Abstract Purpose To evaluate the function of cinnabar in Shangke Jiegu tablet (SKJGT) via pharmacodynamics and toxicity investigations to determine whether cinnabar should be removed from SKJGT. Materials and methods The pharma... |
PMC9024597 | core_pubmed_pmc | The Biological Fate of a Novel Anticancer Drug Candidate TNBG-5602: Metabolic Profile, Interaction with CYP450, and Pharmacokinetics in Rats | The Biological Fate of a Novel Anticancer Drug Candidate TNBG-5602: Metabolic Profile, Interaction with CYP450, and Pharmacokinetics in Rats Abstract TNBG-5602, a novel anticancer drug candidate, may induce the expression of PPARγ, causing targeted lipotoxicity in cancer tissues. In this study, the in vivo metabolism i... |
PMC11746922 | core_pubmed_pmc | Penetration of linezolid and tedizolid in cerebrospinal fluid of mouse and impact of blood–brain barrier disruption | Penetration of linezolid and tedizolid in cerebrospinal fluid of mouse and impact of blood–brain barrier disruption Abstract Abstract Penetration of antimicrobial treatments into the cerebrospinal fluid is essential to successfully treat infections of the central nervous system. This penetration is hindered by differen... |
PMC10435304 | core_pubmed_pmc | A Pharmacokinetic Study of Different Quercetin Formulations in Healthy Participants: A Diet-Controlled, Crossover, Single- and Multiple-Dose Pilot Study | A Pharmacokinetic Study of Different Quercetin Formulations in Healthy Participants: A Diet-Controlled, Crossover, Single- and Multiple-Dose Pilot Study Abstract Abstract This study aimed to evaluate the blood concentrations of quercetin in healthy participants after the administration of different formulations in sing... |
PMC9962277 | core_pubmed_pmc | In Vivo Pharmacodynamics of Calophyllum soulattri as Antiobesity with In Silico Molecular Docking and ADME/Pharmacokinetic Prediction Studies | In Vivo Pharmacodynamics of Calophyllum soulattri as Antiobesity with In Silico Molecular Docking and ADME/Pharmacokinetic Prediction Studies Abstract This study aims to determine the antiobesity activity of Calophyllum soulattri leaves extract (CSLE) on high fat diet-fed rats (HFD) and to predict the molecular docking... |
PMC6182381 | core_pubmed_pmc | Population Pharmacokinetics and Exposure-Response Relationships of Naldemedine | Population Pharmacokinetics and Exposure-Response Relationships of Naldemedine Abstract Purpose To characterize population pharmacokinetic (PK) of naldemedine, to identify factors which influence naldemedine PK, and to evaluate their clinical relevancy based on exposure-response relationships. Methods A population PK m... |
PMC8448163 | core_pubmed_pmc | A Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Oral Doses of V-7404 in Healthy Adult Volunteers | A Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Oral Doses of V-7404 in Healthy Adult Volunteers Abstract ABSTRACT V-7404, a direct-acting enterovirus (EV) 3C protease inhibitor, is being developed as a treatment option for serious EV infections, including infections in immunode... |
PMC6912358 | core_pubmed_pmc | Increased Paracetamol Bioavailability after Sleeve Gastrectomy: A Crossover Pre- vs. Post-Operative Clinical Trial | Increased Paracetamol Bioavailability after Sleeve Gastrectomy: A Crossover Pre- vs. Post-Operative Clinical Trial Abstract Oral drug bioavailability may be significantly altered after laparoscopic sleeve gastrectomy (LSG), the most popular bariatric procedure worldwide. Paracetamol (acetaminophen) is the post-bariatri... |
PMC12196137 | core_pubmed_pmc | Parallel In Vitro and In Silico Studies of the Anti-Inflammatory Activity of Bioactive Compounds Found in Different Ethanolic Extracts of Bracts from B. x buttiana (var. Rose): A Comparative Analysis | Parallel In Vitro and In Silico Studies of the Anti-Inflammatory Activity of Bioactive Compounds Found in Different Ethanolic Extracts of Bracts from B. x buttiana (var. Rose): A Comparative Analysis Abstract Background/Objectives: Bougainvillea x buttiana is used in traditional Mexican medicine to treat various diseas... |
PMC4772585 | core_pubmed_pmc | Population pharmacokinetics of a three-day chloroquine treatment in patients with Plasmodium vivax infection on the Thai-Myanmar border | Population pharmacokinetics of a three-day chloroquine treatment in patients with Plasmodium vivax infection on the Thai-Myanmar border Abstract Abstract Background A three-day course of chloroquine remains a standard treatment of Plasmodium vivax infection in Thailand with satisfactory clinical efficacy and tolerabili... |
PMC7438818 | core_pubmed_pmc | Estimation of Equipotent Doses for Anti‐Inflammatory Effects of Prednisolone and AZD9567, an Oral Selective Nonsteroidal Glucocorticoid Receptor Modulator | Estimation of Equipotent Doses for Anti‐Inflammatory Effects of Prednisolone and AZD9567, an Oral Selective Nonsteroidal Glucocorticoid Receptor Modulator Abstract AZD9567 is a potent and selective nonsteroidal oral glucocorticoid receptor modulator. It is developed as an anti‐inflammatory drug with improved safety pro... |
PMC6658277 | core_pubmed_pmc | Safety of Intranasal Ketamine for Reducing Uncontrolled Cancer-Related Pain: Protocol of a Phase I/II Clinical Trial | Safety of Intranasal Ketamine for Reducing Uncontrolled Cancer-Related Pain: Protocol of a Phase I/II Clinical Trial Abstract Background Approximately 12 million Americans are affected with cancer. Of these, 53% experience pain at all stages of cancer. Pain may remain uncontrolled despite high-dose opioid therapy, and ... |
PMC8619450 | core_pubmed_pmc | Pharmaceutical Aspects of Nanocarriers for Smart Anticancer Therapy | Pharmaceutical Aspects of Nanocarriers for Smart Anticancer Therapy Abstract Abstract Drug delivery to tumor sites using nanotechnology has been demonstrated to overcome the drawbacks of conventional anticancer drugs. Altering the surface shape and geometry of nanocomposites alters their chemical properties, which can ... |
PMC10272070 | core_pubmed_pmc | Treatment of critically ill patients with cefiderocol for infections caused by multidrug-resistant pathogens: review of the evidence | Treatment of critically ill patients with cefiderocol for infections caused by multidrug-resistant pathogens: review of the evidence Abstract Abstract Appropriate antibiotic treatment for critically ill patients with serious Gram-negative infections in the intensive care unit is crucial to minimize morbidity and mortal... |
PMC10893163 | core_pubmed_pmc | Can 3D Printed Tablets Be Bioequivalent and How to Test It: A PBPK Model Based Virtual Bioequivalence Study for Ropinirole Modified Release Tablets | Can 3D Printed Tablets Be Bioequivalent and How to Test It: A PBPK Model Based Virtual Bioequivalence Study for Ropinirole Modified Release Tablets Abstract As the field of personalized dosing develops, the pharmaceutical manufacturing industry needs to offer flexibility in terms of tailoring the drug release and stren... |
PMC4713720 | core_pubmed_pmc | Population pharmacokinetics and pharmacogenetics of once daily tacrolimus formulation in stable liver transplant recipients | Population pharmacokinetics and pharmacogenetics of once daily tacrolimus formulation in stable liver transplant recipients Abstract Purpose The once daily formulation of tacrolimus is an important immunosuppressive drug. Interpatient variability in metabolism has been related to genetic variation in CYP3A4 and CYP3A5 ... |
PMC6502747 | core_pubmed_pmc | Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7 inhibitor and clinical candidate, DTP3 | Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7 inhibitor and clinical candidate, DTP3 Abstract Highlights • DTP3 eliminates any viable MM cells in mice upon i.v. bolus administration. • DTP3 exhibits highly favourable PK and ADME profiles, with long plasma half life. • DTP3 had no adv... |
PMC10107991 | core_pubmed_pmc | A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron (PF‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus | A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of danuglipron (PF‐06882961), an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in Japanese adults with type 2 diabetes mellitus Abstract Abstract Aims This study investigated the safety, tolerability, pharmacokin... |
PMC12555095 | core_pubmed_pmc | Pharmacokinetics and Safety of Fezolinetant in Women with Hepatic or Renal Impairment | Pharmacokinetics and Safety of Fezolinetant in Women with Hepatic or Renal Impairment Abstract Abstract The neurokinin 3 receptor antagonist fezolinetant is an approved treatment for vasomotor symptoms due to menopause. The impacts of hepatic and renal impairment on the pharmacokinetics and safety of a single oral dose... |
PMC9016807 | core_pubmed_pmc | Metabolic, Pharmacokinetic, and Activity Profile of the Liver Stage Antimalarial (RC-12) | Metabolic, Pharmacokinetic, and Activity Profile of the Liver Stage Antimalarial (RC-12) Abstract The catechol derivative RC-12 (WR 27653) ( 1 ) is one of the few non-8-aminoquinolines with good activity against hypnozoites in the gold-standard Plasmodium cynomolgi –rhesus monkey ( Macaca mulatta ) model, but in a smal... |
PMC12519509 | core_pubmed_pmc | Assessment of QT Interval Prolongation Using Concentration– QT Modeling for Iptacopan, an Oral Complement Factor B Inhibitor, in Healthy Individuals | Assessment of QT Interval Prolongation Using Concentration– QT Modeling for Iptacopan, an Oral Complement Factor B Inhibitor, in Healthy Individuals Abstract ABSTRACT To assess cardiac and safety parameters of iptacopan (an oral, selective, reversible, small‐molecule factor B inhibitor), we conducted a phase I, single ... |
PMC11041979 | core_pubmed_pmc | Novel Carbon Dots Derived from Moutan Cortex Significantly Improve the Solubility and Bioavailability of Mangiferin | Novel Carbon Dots Derived from Moutan Cortex Significantly Improve the Solubility and Bioavailability of Mangiferin Abstract Background Mangiferin (MA), a bioactive C-glucosyl xanthone with a wide range of interesting therapeutic properties, has recently attracted considerable attention. However, its application in bio... |
PMC6150229 | core_pubmed_pmc | Simultaneous Determination of Twenty-Five Compounds in Rat Plasma Using Ultra-High Performance Liquid Chromatography-Polarity Switching Tandem Mass Spectrometry and Its Application to a Pharmacokinetic Study | Simultaneous Determination of Twenty-Five Compounds in Rat Plasma Using Ultra-High Performance Liquid Chromatography-Polarity Switching Tandem Mass Spectrometry and Its Application to a Pharmacokinetic Study Abstract Abstract An attempt was made to characterize the pharmacokinetic profiles of Qishen Keli (QSKL) that ha... |
PMC11903821 | core_pubmed_pmc | In silico discovery of potential novel anti-tuberculosis drug candidates from phytoconstituents of Chlorophytum borivilianum and Asparagus racemosus | In silico discovery of potential novel anti-tuberculosis drug candidates from phytoconstituents of Chlorophytum borivilianum and Asparagus racemosus Abstract Tuberculosis (TB), caused by Mycobacterium tuberculosis , remains a significant global health challenge, particularly in developing nations. Side effects and incr... |
PMC10907882 | core_pubmed_pmc | Identification and neuroprotective properties of NA‐184, a calpain‐2 inhibitor | Identification and neuroprotective properties of NA‐184, a calpain‐2 inhibitor Abstract Abstract Our laboratory has shown that calpain‐2 activation in the brain following acute injury is directly related to neuronal damage and the long‐term functional consequences of the injury, while calpain‐1 activation is generally ... |
PMC8047996 | core_pubmed_pmc | Impact of extreme weight loss on factor VIII concentrate pharmacokinetics in haemophilia | Impact of extreme weight loss on factor VIII concentrate pharmacokinetics in haemophilia Abstract We explored the effects of extreme weight loss after gastric bypass surgery on factor VIII concentrate pharmacokinetic (PK) parameters in a patient with haemophilia A. We present a 32-year-old man with severe haemophilia A... |
PMC7241266 | core_pubmed_pmc | Prevention of Adrenal Crisis: Cortisol Responses to Major Stress Compared to Stress Dose Hydrocortisone Delivery | Prevention of Adrenal Crisis: Cortisol Responses to Major Stress Compared to Stress Dose Hydrocortisone Delivery Abstract Abstract Context Patients with adrenal insufficiency require increased hydrocortisone cover during major stress to avoid a life-threatening adrenal crisis. However, current treatment recommendations... |
PMC4921109 | core_pubmed_pmc | A clinical drug–drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib | A clinical drug–drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib Abstract Abstract Purpose The Hedgehog pathway inhibitor vismodegib exhibits pH-dependent solubility,... |
PMC9936208 | core_pubmed_pmc | Incorporation of rapid association/dissociation processes in tissues into the monkey and human physiologically based pharmacokinetic models for manganese | Incorporation of rapid association/dissociation processes in tissues into the monkey and human physiologically based pharmacokinetic models for manganese Abstract Abstract In earlier physiologically based pharmacokinetic (PBPK) models for manganese (Mn), the kinetics of transport of Mn into and out of tissues were prim... |
PMC9428150 | core_pubmed_pmc | Mechanistic PK-PD model of alendronate treatment of postmenopausal osteoporosis predicts bone site-specific response | Mechanistic PK-PD model of alendronate treatment of postmenopausal osteoporosis predicts bone site-specific response Abstract Abstract Alendronate is the most widely used drug for postmenopausal osteoporosis (PMO). It inhibits bone resorption, affecting osteoclasts. Pharmacokinetics (PK) and pharmacodynamics (PD) of al... |
PMC9377751 | core_pubmed_pmc | DS-7300a, a DNA Topoisomerase I Inhibitor, DXd-Based Antibody–Drug Conjugate Targeting B7-H3, Exerts Potent Antitumor Activities in Preclinical Models | DS-7300a, a DNA Topoisomerase I Inhibitor, DXd-Based Antibody–Drug Conjugate Targeting B7-H3, Exerts Potent Antitumor Activities in Preclinical Models Abstract Abstract B7-H3 is overexpressed in various solid tumors and has been considered as an attractive target for cancer therapy. Here, we report the development of D... |
PMC5428680 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration | Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration Abstract Abstract Tuberculosis (TB) treatment is long and complex, typically involving a combination of drugs taken for 6 months. Improved drug regimens to shorten and... |
PMC9442941 | core_pubmed_pmc | IMI2-PainCare-BioPain-RCT2 protocol: a randomized, double-blind, placebo-controlled, crossover, multicenter trial in healthy subjects to investigate the effects of lacosamide, pregabalin, and tapentadol on biomarkers of pain processing observed by non-invasive neurophysiological measurements of human spinal cord and br... | IMI2-PainCare-BioPain-RCT2 protocol: a randomized, double-blind, placebo-controlled, crossover, multicenter trial in healthy subjects to investigate the effects of lacosamide, pregabalin, and tapentadol on biomarkers of pain processing observed by non-invasive neurophysiological measurements of human spinal cord and br... |
PMC6943327 | core_pubmed_pmc | Effects of anemoside B4 on pharmacokinetics of florfenicol and mRNA expression of CXR, MDR1, CYP3A37 and UGT1E in broilers | Effects of anemoside B4 on pharmacokinetics of florfenicol and mRNA expression of CXR, MDR1, CYP3A37 and UGT1E in broilers Abstract Abstract Pulsatillae radix , a traditional Chinese medicine (TCM), is often used in combination with florfenicol for treatment of intestinal infection in Chinese veterinary clinics. Anemos... |
PMC7997407 | core_pubmed_pmc | Pharmacokinetic Analysis of Carnosic Acid and Carnosol in Standardized Rosemary Extract and the Effect on the Disease Activity Index of DSS-Induced Colitis | Pharmacokinetic Analysis of Carnosic Acid and Carnosol in Standardized Rosemary Extract and the Effect on the Disease Activity Index of DSS-Induced Colitis Abstract Rosemary extract (RE) is an approved food preservative in the European Union and contains dietary phytochemicals that are beneficial for gastrointestinal h... |
PMC5503500 | core_pubmed_pmc | Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation | Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation Abstract Abstract Nanodrug delivery systems have been widely reviewed for their use in several drug formulations to improve bioavailability, sust... |
PMC10610014 | core_pubmed_pmc | Drug–Drug Interactions between Tamsulosin and Mirabegron in Healthy Individuals Do Not Affect Pharmacokinetics and Hemodynamic Parameters Significantly | Drug–Drug Interactions between Tamsulosin and Mirabegron in Healthy Individuals Do Not Affect Pharmacokinetics and Hemodynamic Parameters Significantly Abstract Overactive bladder (OAB) is characterized by urinary urgency and increased urinary frequency, substantially affecting quality of life. Tamsulosin and mirabegro... |
PMC10801101 | core_pubmed_pmc | Prediction of Novel Natural Small Molecules From Schinus molle as an Inhibitor of PI3K Protein Target in Cancer Cells Using In Silico Screening | Prediction of Novel Natural Small Molecules From Schinus molle as an Inhibitor of PI3K Protein Target in Cancer Cells Using In Silico Screening Abstract Abstract Introduction Cancer continues to pose a significant challenge in medical research. Phytochemicals derived from plants have emerged as a promising avenue for p... |
PMC4522836 | core_pubmed_pmc | Simultaneous determination of four active components in rat plasma by ultra-high performance liquid chromatography tandem-mass spectrometry/mass spectrometry and its application to a pharmacokinetic study after oral administration of Callicarpa nudiflora extract | Simultaneous determination of four active components in rat plasma by ultra-high performance liquid chromatography tandem-mass spectrometry/mass spectrometry and its application to a pharmacokinetic study after oral administration of Callicarpa nudiflora extract Abstract Abstract Background: Callicarpa nudiflora has be... |
PMC3809924 | core_pubmed_pmc | Evaluation of the pharmacokinetics and pharmacodynamics of ticagrelor co-administered with aspirin in healthy volunteers | Evaluation of the pharmacokinetics and pharmacodynamics of ticagrelor co-administered with aspirin in healthy volunteers Abstract The results of two independent, randomized, two-period crossover, single-center studies, conducted to assess the pharmacokinetics of ticagrelor ± aspirin, inhibition of platelet aggregation ... |
PMC10726352 | core_pubmed_pmc | Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers | Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers Abstract Transcriptional deregulation is a hallmark of many cancers and is exemplified by genomic amplifications of the MYC family of oncogenes, which occur in at least 20% of all solid tumors in ad... |
PMC10960609 | core_pubmed_pmc | Pharmacokinetic behaviour and pharmacokinetic–pharmacodynamic integration of doxycycline in rainbow trout ( Oncorhynchus mykiss ) after intravascular, intramuscular and oral administrations | Pharmacokinetic behaviour and pharmacokinetic–pharmacodynamic integration of doxycycline in rainbow trout ( Oncorhynchus mykiss ) after intravascular, intramuscular and oral administrations Abstract Abstract Objective Doxycycline (DO) has been used in fish for a long time, but there are some factors that have not yet b... |
PMC6363730 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Modeling for Coptisine Challenge of Inflammation in LPS-Stimulated Rats | Pharmacokinetic-Pharmacodynamic Modeling for Coptisine Challenge of Inflammation in LPS-Stimulated Rats Abstract Abstract Pro-inflammatory factors are important indicators for assessing inflammation severity and drug efficacy. Coptisine has been reported to inhibit LPS-induced TNF-α and NO production. In this study, we... |
PMC11925827 | core_pubmed_pmc | In-Hospital Management of Hyperglycemia: The Role of Insulin Degludec | In-Hospital Management of Hyperglycemia: The Role of Insulin Degludec Abstract Abstract Introduction Hyperglycemia is a common and challenging condition in hospitalized patients both with and without a history of diabetes. Managing hyperglycemia effectively is critical in reducing complications, mortality, and the leng... |
PMC9541946 | core_pubmed_pmc | A review of the pharmacokinetics, efficacy and safety of high‐purity factor X for the prophylactic treatment of hereditary factor X deficiency | A review of the pharmacokinetics, efficacy and safety of high‐purity factor X for the prophylactic treatment of hereditary factor X deficiency Abstract Abstract Introduction Hereditary factor X (FX) deficiency (FXD) is a rare autosomal recessive bleeding disorder. Plasma‐derived FX (pdFX) is a high‐purity FX concentrat... |
PMC6879437 | core_pubmed_pmc | Engineered antibodies: new possibilities for brain PET? | Engineered antibodies: new possibilities for brain PET? Abstract Almost 50 million people worldwide are affected by Alzheimer’s disease (AD), the most common neurodegenerative disorder. Development of disease-modifying therapies would benefit from reliable, non-invasive positron emission tomography (PET) biomarkers for... |
PMC11792010 | core_pubmed_pmc | Molecular Docking Appraisal of Pleurotus ostreatus Phytochemicals as Potential Inhibitors of PI3K/Akt Pathway for Breast Cancer Treatment | Molecular Docking Appraisal of Pleurotus ostreatus Phytochemicals as Potential Inhibitors of PI3K/Akt Pathway for Breast Cancer Treatment Abstract Introduction: Breast cancer (BC) is a heterogeneous disease involving a network of numerous extracellular signal transduction pathways. The phosphoinositide 3-kinase (PI3K)/... |
PMC6214181 | core_pubmed_pmc | Revisiting cefditoren for the treatment of community-acquired infections caused by human-adapted respiratory pathogens in adults | Revisiting cefditoren for the treatment of community-acquired infections caused by human-adapted respiratory pathogens in adults Abstract Abstract Fifteen years after its licensure, this revision assesses the role of cefditoren facing the current pharmacoepidemiology of resistances in respiratory human-adapted pathogen... |
PMC7511144 | core_pubmed_pmc | Population Pharmacokinetics of Hydroxychloroquine in COVID-19 Patients: Implications for Dose Optimization | Population Pharmacokinetics of Hydroxychloroquine in COVID-19 Patients: Implications for Dose Optimization Abstract Background and Objective In the absence of characterization on pharmacokinetics and reference concentrations for hydroxychloroquine in COVID-19 patients, the dose and treatment duration for hydrochloroqui... |
PMC9316317 | core_pubmed_pmc | Reducing the Kidney Uptake of High Contrast CXCR4 PET Imaging Agents via Linker Modifications | Reducing the Kidney Uptake of High Contrast CXCR4 PET Imaging Agents via Linker Modifications Abstract Abstract Purpose: The C-X-C chemokine receptor 4 (CXCR4) is highly expressed in many subtypes of cancers, notably in several kidney-based malignancies. We synthesized, labeled, and assessed a series of radiotracers ba... |
PMC12258651 | core_pubmed_pmc | Determination and disposition of meta -iodobenzylguanidine in plasma and heart of transporter-deficient mice by UPLC-MS/MS | Determination and disposition of meta -iodobenzylguanidine in plasma and heart of transporter-deficient mice by UPLC-MS/MS Abstract A simple LC-MS/MS method for the quantitative determination of the norepinephrine analogue meta -iodobenzyl-guanidine (mIBG) was developed and validated for mouse plasma and tissues, inclu... |
PMC5938375 | core_pubmed_pmc | Is IQG-607 a Potential Metallodrug or Metallopro-Drug With a Defined Molecular Target in Mycobacterium tuberculosis ? | Is IQG-607 a Potential Metallodrug or Metallopro-Drug With a Defined Molecular Target in Mycobacterium tuberculosis ? Abstract The emergence of strains of Mycobacterium tuberculosis resistant to isoniazid (INH) has underscored the need for the development of new anti-tuberculosis agents. INH is activated by the mycobac... |
PMC12737397 | core_pubmed_pmc | Repurposing FDA-Approved Drugs as Hendra Virus RNA-Dependent RNA Polymerase Inhibitors: A Comprehensive Computational Drug Discovery Approach | Repurposing FDA-Approved Drugs as Hendra Virus RNA-Dependent RNA Polymerase Inhibitors: A Comprehensive Computational Drug Discovery Approach Abstract Abstract Hendra virus (HeV) is a highly pathogenic zoonotic paramyxovirus that poses a serious threat to human and equine health, yet no approved antivirals or vaccines ... |
PMC12801877 | core_pubmed_pmc | GB5, a synergistic phytotherapy for type 2 diabetes mellitus management: an integrated polyherbal approach from phytochemical profiling to network pharmacology | GB5, a synergistic phytotherapy for type 2 diabetes mellitus management: an integrated polyherbal approach from phytochemical profiling to network pharmacology Abstract Abstract Background Type 2 diabetes mellitus (T2DM) remains a global health burden characterized by insulin resistance, persistent hyperglycaemia, and ... |
PMC12227205 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Remimazolam for Procedural Sedation in Children and Adolescents | Pharmacokinetics and Pharmacodynamics of Remimazolam for Procedural Sedation in Children and Adolescents Abstract Abstract Background: Remimazolam is not approved for use in pediatric patients. The pharmacokinetics of remimazolam have been reported to be similar to those of adult patients after scaling for body size. T... |
PMC5914314 | core_pubmed_pmc | Human Abuse Potential of the New Opioid Analgesic Molecule NKTR-181 Compared with Oxycodone | Human Abuse Potential of the New Opioid Analgesic Molecule NKTR-181 Compared with Oxycodone Abstract Abstract Objective Evaluate the human abuse potential, pharmacokinetics, pharmacodynamics, and safety of NKTR-181, a novel mu-opioid agonist molecule, relative to oxycodone. Design This randomized, single-center, double... |
PMC12806588 | core_pubmed_pmc | When are novel methods for analyzing complex chemical mixtures in epidemiology beneficial? | When are novel methods for analyzing complex chemical mixtures in epidemiology beneficial? Abstract Estimating the health impacts of exposure to a mixture of chemicals poses many statistical challenges: multiple correlated exposure variables, moderate to high dimensionality, and possible nonlinear and interactive healt... |
PMC4591485 | core_pubmed_pmc | Pharmacokinetics of single oral dose trazodone: a randomized, two-period, cross-over trial in healthy, adult, human volunteers under fed condition | Pharmacokinetics of single oral dose trazodone: a randomized, two-period, cross-over trial in healthy, adult, human volunteers under fed condition Abstract Abstract Objective: To assess the bioequivalence of single dose trazodone hydrochloride USP 100 mg tablets administered as an oral dose under fed condition. Methods... |
PMC7407622 | core_pubmed_pmc | Population Pharmacokinetics of Vincristine Related to Infusion Duration and Peripheral Neuropathy in Pediatric Oncology Patients | Population Pharmacokinetics of Vincristine Related to Infusion Duration and Peripheral Neuropathy in Pediatric Oncology Patients Abstract Vincristine (VCR) is frequently used in pediatric oncology and can be administered intravenously through push injections or 1 h infusions. The effects of administration duration on p... |
PMC9298070 | core_pubmed_pmc | Lack of a Clinically Meaningful Drug Interaction Between the HIV‐1 Antiretroviral Agents Islatravir, Dolutegravir, and Tenofovir Disoproxil Fumarate | Lack of a Clinically Meaningful Drug Interaction Between the HIV‐1 Antiretroviral Agents Islatravir, Dolutegravir, and Tenofovir Disoproxil Fumarate Abstract Abstract Islatravir, an investigational nucleoside reverse transcriptase translocation inhibitor, is in clinical development for the treatment and prevention of H... |
PMC4720707 | core_pubmed_pmc | A population pharmacokinetic model for R- and S-citalopram and desmethylcitalopram in Alzheimer’s disease patients with agitation | A population pharmacokinetic model for R- and S-citalopram and desmethylcitalopram in Alzheimer’s disease patients with agitation Abstract Abstract The citalopram for Alzheimer’s disease trial evaluated citalopram for the management for agitation in Alzheimer’s disease patients. Sparse data was available from this elde... |
PMC6332156 | core_pubmed_pmc | Comparative Pharmacokinetics Study of Icariin and Icariside II in Rats | Comparative Pharmacokinetics Study of Icariin and Icariside II in Rats Abstract To explore the pharmacokinetic properties of icariin (ICA) and icariside II (ICA II) following intragastric and intravenous administration in rats, a rapid and sensitive method by using ultra-performance liquid chromatography–tandem mass sp... |
PMC7719387 | core_pubmed_pmc | Population Pharmacokinetics of Metoclopramide in Infants, Children, and Adolescents | Population Pharmacokinetics of Metoclopramide in Infants, Children, and Adolescents Abstract Abstract Metoclopramide is commonly used for gastroesophageal reflux. The aims of the present study were to develop a pediatric population pharmacokinetic (PopPK) model, which was applied to simulate the metoclopramide exposure... |
PMC8517077 | core_pubmed_pmc | Indoles Derived From Glucobrassicin: Cancer Chemoprevention by Indole-3-Carbinol and 3,3'-Diindolylmethane | Indoles Derived From Glucobrassicin: Cancer Chemoprevention by Indole-3-Carbinol and 3,3'-Diindolylmethane Abstract Hydrolysis of glucobrassicin by plant or bacterial myrosinase produces multiple indoles predominantly indole-3-carbinol (I3C). I3C and its major in vivo product, 3,3'-diindolylmethane (DIM), are effective... |
PMC7003501 | core_pubmed_pmc | Preclinical Pharmacokinetics of Lamivudine and Its Interaction with Schisandra chinensis Extract in Rats | Preclinical Pharmacokinetics of Lamivudine and Its Interaction with Schisandra chinensis Extract in Rats Abstract Schisandra chinensis (Turcz.) Baill. ( S. chinensis ) extract and its active ingredient, schizandrin, have been used as a botanical medicine and dietary supplement for the treatment of hepatitis. Lamivudine... |
PMC12957794 | core_pubmed_pmc | Hyperthermia-targeted rectal delivery of thermosensitive liposomal doxorubicin via intra-arterial and intravenous administration | Hyperthermia-targeted rectal delivery of thermosensitive liposomal doxorubicin via intra-arterial and intravenous administration Abstract Introduction Lyso-thermosensitive liposomal doxorubicin (LTLD) is a thermosensitive nanomedicine designed to release doxorubicin rapidly at mild hyperthermic temperatures. Unlike sys... |
PMC6321364 | core_pubmed_pmc | Pharmacokinetic Profile of Kaurenoic Acid after Oral Administration of Araliae Continentalis Radix Extract Powder to Humans | Pharmacokinetic Profile of Kaurenoic Acid after Oral Administration of Araliae Continentalis Radix Extract Powder to Humans Abstract The objective of this study was to characterize pharmacokinetics (PKs) of kaurenoic acid (KAU) after administration of the clinical usual dose of Araliae Continentalis Radix extract powde... |
PMC10787705 | core_pubmed_pmc | Bioequivalence Study of Two Tablet Formulations of Clonazepam 2 mg: A Randomized, Open-Label, Crossover Study in Healthy Mexican Volunteers Under Fasting Conditions | Bioequivalence Study of Two Tablet Formulations of Clonazepam 2 mg: A Randomized, Open-Label, Crossover Study in Healthy Mexican Volunteers Under Fasting Conditions Abstract Introduction The prevalence of neurological disorders is high among the Mexican population. Clonazepam is primarily indicated to treat panic disor... |
PMC5694508 | core_pubmed_pmc | Phase I trial and pharmacokinetic study of tanibirumab, a fully human monoclonal antibody to vascular endothelial growth factor receptor 2, in patients with refractory solid tumors | Phase I trial and pharmacokinetic study of tanibirumab, a fully human monoclonal antibody to vascular endothelial growth factor receptor 2, in patients with refractory solid tumors Abstract Summary Background Tanibirumab is a fully human monoclonal antibody to vascular endothelial growth factor receptor 2 (VEGFR-2). We... |
PMC8219220 | core_pubmed_pmc | Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators | Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators Abstract Abstract Organophosphorus poisoning caused by some pesticides and nerve agents is a life-threating condition that must be swiftly addressed to avoid casualties. Despite the ... |
PMC9075024 | core_pubmed_pmc | A simple LC-MS/MS method for pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol at a low dose | A simple LC-MS/MS method for pharmacokinetic study of carvedilol and 4/-hydroxyphenyl carvedilol at a low dose Abstract Background and purpose: The study was aimed at validating a simple, rapid, and low-cost LC-MS/MS method for carvedilol and 4 / -hydroxyphenyl carvedilol assay in human plasma. The validated method was... |
PMC6775169 | core_pubmed_pmc | A pharmacokinetic model of lead absorption and calcium competitive dynamics | A pharmacokinetic model of lead absorption and calcium competitive dynamics Abstract Lead is a naturally-occurring element. It has been known to man for a long time, and it is one of the longest established poisons. The current consensus is that no level of lead exposure should be deemed “safe”. New evidence regarding ... |
PMC12661886 | core_pubmed_pmc | A phase 1/2 study of DS-1594 menin inhibitor in relapsed/refractory acute leukemias | A phase 1/2 study of DS-1594 menin inhibitor in relapsed/refractory acute leukemias Abstract Abstract Several menin inhibitors are in development targeting menin dependent leukemias, however available preclinical results show variable level of activity. We report the phase 1 portion (to establish a recommended phase 2 ... |
PMC12705286 | core_pubmed_pmc | Allosteric ligand-driven smart nanoconjugates for mutation-selective EGFR targeting: A precision approach to overcoming tyrosine kinase inhibitor resistance | Allosteric ligand-driven smart nanoconjugates for mutation-selective EGFR targeting: A precision approach to overcoming tyrosine kinase inhibitor resistance Abstract The development of targeted therapies against epidermal growth factor receptor (EGFR) has transformed the clinical management of EGFR-driven malignancies,... |
PMC8259838 | core_pubmed_pmc | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats | Study on the pharmacokinetics, tissue distribution and excretion of laurolitsine from Litsea glutinosa in Sprague-Dawley rats Abstract Abstract Context Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective To investigate the pharmacokinetics,... |
PMC12099050 | core_pubmed_pmc | Pharmacokinetics, toxicities, and tissue concentrations of belotecan sprayed by rotational intraperitoneal pressurized aerosol chemotherapy in a pig model | Pharmacokinetics, toxicities, and tissue concentrations of belotecan sprayed by rotational intraperitoneal pressurized aerosol chemotherapy in a pig model Abstract Abstract Objective We evaluated the pharmacokinetics, tissue concentrations, and toxicities of belotecan during rotational intraperitoneal pressurized aeros... |
PMC12925024 | core_pubmed_pmc | The interplay between serotonin syndrome and syndrome of inappropriate antidiuresis: a fatal case of acute hyponatremia during treatment with duloxetine, chlorphenamine, amitriptyline, and L-tryptophan | The interplay between serotonin syndrome and syndrome of inappropriate antidiuresis: a fatal case of acute hyponatremia during treatment with duloxetine, chlorphenamine, amitriptyline, and L-tryptophan Abstract Serotonin syndrome (SS) and hyponatremia are severe, potentially life-threatening adverse reactions to seroto... |
PMC12597572 | core_pubmed_pmc | Development and analysis of a remimazolam pharmacokinetics and pharmacodynamics model with proposed dosing and concentrations for anaesthesia and sedation | Development and analysis of a remimazolam pharmacokinetics and pharmacodynamics model with proposed dosing and concentrations for anaesthesia and sedation Abstract Abstract Background Pharmacokinetic–pharmacodynamic (PK–PD) models of remimazolam and their covariate relationships are useful for understanding drug dispos... |
PMC10651637 | core_pubmed_pmc | CYP2C19 genotypes and osteoporotic fractures in long‐term users of proton pump inhibitors: A hospital‐based study | CYP2C19 genotypes and osteoporotic fractures in long‐term users of proton pump inhibitors: A hospital‐based study Abstract Abstract Proton pump inhibitors (PPIs) are commonly prescribed medications. The existing data suggest that individuals at a high risk of fractures have been exposed to high doses of PPIs for prolon... |
PMC12119765 | core_pubmed_pmc | Unveiling the potential of copper-61 vs. gallium-68 for SSTR PET imaging | Unveiling the potential of copper-61 vs. gallium-68 for SSTR PET imaging Abstract Abstract Purpose In recent years, copper-61 has attracted considerable attention from both physicists and radiochemists due to its favorable physical decay properties for PET imaging and its ease of production at any cyclotron center prod... |
PMC9300558 | core_pubmed_pmc | Exposure–response analyses for the MET inhibitor tepotinib including patients in the pivotal VISION trial: support for dosage recommendations | Exposure–response analyses for the MET inhibitor tepotinib including patients in the pivotal VISION trial: support for dosage recommendations Abstract Purpose Tepotinib is a highly selective MET inhibitor approved for treatment of non-small cell lung cancer (NSCLC) harboring MET ex14 skipping alterations. Analyses pres... |
PMC9545531 | core_pubmed_pmc | Pharmacodynamic modelling and exposure–response assessment of inebilizumab in subjects with neuromyelitis optica spectrum disorders | Pharmacodynamic modelling and exposure–response assessment of inebilizumab in subjects with neuromyelitis optica spectrum disorders Abstract Aims Neuromyelitis optica spectrum disorders (NMOSD) is an autoantibody‐mediated, B cell‐driven disease. Inebilizumab is a humanized, affinity‐optimized, afucosylated IgG1 κ monoc... |
PMC10857686 | core_pubmed_pmc | Influence of genetic polymorphisms in vascular endothelial-related genes on the clinical outcome of axitinib in patients with metastatic renal cell carcinoma | Influence of genetic polymorphisms in vascular endothelial-related genes on the clinical outcome of axitinib in patients with metastatic renal cell carcinoma Abstract ABSTRACT Objective Axitinib is an oral multi-target tyrosine kinase inhibitor used for the treatment of renal cell carcinoma (RCC). Because of the severe... |
PMC8179178 | core_pubmed_pmc | Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation † | Click activated protodrugs against cancer increase the therapeutic potential of chemotherapy through local capture and activation † Abstract Abstract A desired goal of targeted cancer treatments is to achieve high tumor specificity with minimal side effects. Despite recent advances, this remains difficult to achieve in... |
PMC7494236 | core_pubmed_pmc | Self-Assembled Dual-Targeted Epirubicin-Hybrid Polydopamine Nanoparticles for Combined Chemo-Photothermal Therapy of Triple-Negative Breast Cancer | Self-Assembled Dual-Targeted Epirubicin-Hybrid Polydopamine Nanoparticles for Combined Chemo-Photothermal Therapy of Triple-Negative Breast Cancer Abstract Abstract Purpose Folic acid and cyclic arginylglycylaspartic acid peptides were introduced to the surface of negatively charged lipid-coated hybrid polydopamine-cys... |
PMC11602950 | core_pubmed_pmc | The effect of severe renal impairment on the pharmacokinetics, safety and tolerability of mitiperstat | The effect of severe renal impairment on the pharmacokinetics, safety and tolerability of mitiperstat Abstract Abstract Aims Mitiperstat is a novel, highly potent myeloperoxidase inhibitor being evaluated in patients with cardio‐metabolic disease (phase 2). These patients often have impaired renal function, which may a... |
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