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PMC4236622 | core_pubmed_pmc | Nonclinical pharmacokinetics and activity of etirinotecan pegol (NKTR-102), a long-acting topoisomerase 1 inhibitor, in multiple cancer models | Nonclinical pharmacokinetics and activity of etirinotecan pegol (NKTR-102), a long-acting topoisomerase 1 inhibitor, in multiple cancer models Abstract Abstract Purpose The aim of the study was to demonstrate the activity of etirinotecan pegol, a polymer conjugate of irinotecan, in multiple human tumor models and to es... |
PMC7944986 | core_pubmed_pmc | Safety and activity of the TGFβ receptor I kinase inhibitor galunisertib plus the anti-PD-L1 antibody durvalumab in metastatic pancreatic cancer | Safety and activity of the TGFβ receptor I kinase inhibitor galunisertib plus the anti-PD-L1 antibody durvalumab in metastatic pancreatic cancer Abstract Abstract Background We assessed the safety, efficacy, and pharmacokinetics of the transforming growth factor beta (TGFβ) receptor inhibitor galunisertib co-administer... |
PMC6490911 | core_pubmed_pmc | Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies | Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies Abstract Background Linezolid is increasingly important for multidrug-resistant tuberculosis (MDR-TB) treatment. However, among children with MDR-TB, ther... |
PMC4418347 | core_pubmed_pmc | Pharmacokinetics of the Dual Melatonin Receptor Agonist Tasimelteon in Subjects With Hepatic or Renal Impairment | Pharmacokinetics of the Dual Melatonin Receptor Agonist Tasimelteon in Subjects With Hepatic or Renal Impairment Abstract Tasimelteon is a circadian regulator that resets the master clock in the suprachiasmatic nuclei of the hypothalamus by binding to both melatonin MT 1 and MT 2 receptors making it a dual melatonin re... |
PMC6324384 | core_pubmed_pmc | Acute Effects of Smoked and Vaporized Cannabis in Healthy Adults Who Infrequently Use Cannabis | Acute Effects of Smoked and Vaporized Cannabis in Healthy Adults Who Infrequently Use Cannabis Abstract Key Points Question How does smoked and vaporized cannabis acutely influence subjective drug effects, cognitive and psychomotor performance, and cardiovascular measures in healthy adults who infrequently use cannabis... |
PMC7940353 | core_pubmed_pmc | Model-Informed Precision Dosing of Antibiotics in Pediatric Patients: A Narrative Review | Model-Informed Precision Dosing of Antibiotics in Pediatric Patients: A Narrative Review Abstract Optimal pharmacotherapy in pediatric patients with suspected infections requires understanding and integration of relevant data on the antibiotic, bacterial pathogen, and patient characteristics. Because of age-related phy... |
PMC6099542 | core_pubmed_pmc | [ 18 F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model | [ 18 F]FEPPA a TSPO Radioligand: Optimized Radiosynthesis and Evaluation as a PET Radiotracer for Brain Inflammation in a Peripheral LPS-Injected Mouse Model Abstract [ 18 F]FEPPA is a specific ligand for the translocator protein of 18 kDa (TSPO) used as a positron emission tomography (PET) biomarker for glial activati... |
PMC12484386 | core_pubmed_pmc | Effects of Hepatic or Renal Impairment on Pharmacokinetics of Fruquintinib | Effects of Hepatic or Renal Impairment on Pharmacokinetics of Fruquintinib Abstract Abstract Fruquintinib (FRUZAQLA TM ) is a highly selective tyrosine kinase inhibitor of all three vascular endothelial growth factor receptors (‐1, ‐2, and ‐3). Two Phase 1, open‐label, single‐dose studies investigated the impact of hep... |
PMC10681527 | core_pubmed_pmc | Skipping a pillar does not make for strong foundations: Pharmacokinetic‐pharmacodynamic reasoning behind the shape of dose–response relationships in oncology | Skipping a pillar does not make for strong foundations: Pharmacokinetic‐pharmacodynamic reasoning behind the shape of dose–response relationships in oncology Abstract Abstract Dose–response analysis is often applied to the quantification of drug‐effect especially for slowly responding disease end points where a compari... |
PMC7955752 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Single and Multiple Ascending Doses of Benfotiamine in Healthy Subjects | Safety, Tolerability and Pharmacokinetics of Single and Multiple Ascending Doses of Benfotiamine in Healthy Subjects Abstract Abstract Purpose Safety, tolerability and pharmacokinetics of single and multiple ascending doses (SADs/MADs) of benfotiamine were assessed after oral administration in two randomized, double-bl... |
PMC3766998 | core_pubmed_pmc | Comparative Plasma Exposure of Albendazole after Administration of Rapidly Disintegrating Tablets in Dogs | Comparative Plasma Exposure of Albendazole after Administration of Rapidly Disintegrating Tablets in Dogs Abstract The main objectives of this study were (a) to evaluate the in vitro performance of the rapid disintegration tablets as a way to improve the solid dispersions and (b) to study the in vivo pharmacokinetics o... |
PMC6911901 | core_pubmed_pmc | Pharmacokinetic Parameters of Quinine in Healthy Subjects and in Patients with Uncomplicated Malaria in Nigeria: Analysis of Data using a Population Approach | Pharmacokinetic Parameters of Quinine in Healthy Subjects and in Patients with Uncomplicated Malaria in Nigeria: Analysis of Data using a Population Approach Abstract Highlights • Varied disposition imparts on the tolerance and safety of quinine, and thus constitutes a major limiting consideration for its dosing in unc... |
PMC9146975 | core_pubmed_pmc | Virtual Screening Based on Machine Learning Explores Mangrove Natural Products as KRAS G12C Inhibitors | Virtual Screening Based on Machine Learning Explores Mangrove Natural Products as KRAS G12C Inhibitors Abstract Mangrove secondary metabolites have many unique biological activities. We identified lead compounds among them that might target KRAS G12C . KRAS is considered to be closely related to various cancers. A vari... |
PMC12209837 | core_pubmed_pmc | Liposomal amphotericin B prophylaxis in paediatrics: a systematic review | Liposomal amphotericin B prophylaxis in paediatrics: a systematic review Abstract Abstract Background Liposomal amphotericin B (LAmB) is widely used for prophylaxis in paediatric patients at high risk of invasive fungal diseases (IFD) but its use is off-label and there is significant variability in dosage and frequency... |
PMC7886476 | core_pubmed_pmc | Prediction of expiratory desflurane and sevoflurane concentrations in lung-healthy patients utilizing cardiac output and alveolar ventilation matched pharmacokinetic models | Prediction of expiratory desflurane and sevoflurane concentrations in lung-healthy patients utilizing cardiac output and alveolar ventilation matched pharmacokinetic models Abstract Supplemental Digital Content is available in the text Keywords: computer simulation, Inhalation anesthesia, pharmacokinetic model, physiol... |
PMC7700809 | core_pubmed_pmc | Low dose of emetine as potential anti-SARS-CoV-2 virus therapy: preclinical in vitro inhibition and in vivo pharmacokinetic evidences | Low dose of emetine as potential anti-SARS-CoV-2 virus therapy: preclinical in vitro inhibition and in vivo pharmacokinetic evidences Abstract The global pandemic of COVID-19 has attracted extensive drug searching interets for the new coronavirus SARS-CoV-2. Although currently several of clinically used “old” drugs hav... |
PMC11677946 | core_pubmed_pmc | Investigating the Potential of Ufasomes Laden with Nintedanib as an Optimized Targeted Lung Nanoparadigm for Accentuated Tackling of Idiopathic Pulmonary Fibrosis | Investigating the Potential of Ufasomes Laden with Nintedanib as an Optimized Targeted Lung Nanoparadigm for Accentuated Tackling of Idiopathic Pulmonary Fibrosis Abstract Abstract Background/objectives : Idiopathic pulmonary fibrosis (IPF) is a prevalent interstitial lung disease that typically progresses gradually, l... |
PMC6459237 | core_pubmed_pmc | Phase I, First‐in‐Human, Dose‐Escalation Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Vorolanib in Patients with Advanced Solid Tumors | Phase I, First‐in‐Human, Dose‐Escalation Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Vorolanib in Patients with Advanced Solid Tumors Abstract Abstract Lessons Learned. Pharmacokinetic results underscore that the vorolanib (X‐82) study design was successful without the need for further dose esca... |
PMC12067867 | core_pubmed_pmc | Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein | Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein Abstract Abstract Background The administration of recombinant interleukin 2 (IL-2) in oncology is frequently hampered by dose-limiting toxicities, including potentially lethal vascular leak syndrome. Antibody-... |
PMC10944885 | core_pubmed_pmc | Population pharmacokinetic model for oral ORIN1001 in Chinese patients with advanced solid tumors | Population pharmacokinetic model for oral ORIN1001 in Chinese patients with advanced solid tumors Abstract Background: ORIN1001, a first-in-class oral IRE1-α endoribonuclease inhibitor to block the activation of XBP1, is currently in clinical development for inhibiting tumor growth and enhancing the effect of chemical ... |
PMC3930089 | core_pubmed_pmc | Semiphysiological versus Empirical Modelling of the Population Pharmacokinetics of Free and Total Cefazolin during Pregnancy | Semiphysiological versus Empirical Modelling of the Population Pharmacokinetics of Free and Total Cefazolin during Pregnancy Abstract Abstract This work describes a first population pharmacokinetic (PK) model for free and total cefazolin during pregnancy, which can be used for dose regimen optimization. Secondly, analy... |
PMC12024234 | core_pubmed_pmc | Antioxidant, Anti-Inflammatory, and Oral Bioavailability of Novel Sulfonamide Derivatives of Gallic Acid | Antioxidant, Anti-Inflammatory, and Oral Bioavailability of Novel Sulfonamide Derivatives of Gallic Acid Abstract Gallic acid (GA) is known for its antioxidant and anti-inflammatory properties, yet its clinical potential is hindered due to poor oral bioavailability. This study investigates novel GA sulfonamide derivati... |
PMC7441710 | core_pubmed_pmc | Opioids and alpha-2-agonists for analgesia and sedation in newborn infants: protocol of a systematic review | Opioids and alpha-2-agonists for analgesia and sedation in newborn infants: protocol of a systematic review Abstract Background Hospitalized newborn infants may require analgesia and sedation either for the management of procedural pain, during or after surgery, and other painful conditions. The benefits and harms of o... |
PMC6974130 | core_pubmed_pmc | The Effect of UGT1A9, CYP2B6 and CYP2C9 Genes Polymorphism on Propofol Pharmacokinetics in Children | The Effect of UGT1A9, CYP2B6 and CYP2C9 Genes Polymorphism on Propofol Pharmacokinetics in Children Abstract Abstract Purpose This study was conducted to determine the effect of UGT1A9 98T>C, CYP2B6 516G>T and CYP2C9 430C>T genetic polymorphisms on the pharmacokinetics of propofol in children of different sexes and age... |
PMC12182312 | core_pubmed_pmc | Comparison of Bioavailability of Nitrates and Nitrites in 3 Species of Amaranthus : A Randomized, Double-Blind, Placebo-Controlled, 4-Way Crossover Study in Healthy Subjects Under Fasting Conditions | Comparison of Bioavailability of Nitrates and Nitrites in 3 Species of Amaranthus : A Randomized, Double-Blind, Placebo-Controlled, 4-Way Crossover Study in Healthy Subjects Under Fasting Conditions Abstract Background Amaranthus is a significant source of dietary nitrates, which have been known to improve aerobic capa... |
PMC8539993 | core_pubmed_pmc | Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine | Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine Abstract This work aimed to develop a three-dimensional printed (3DP) tablet containing glimepiride (GLMP) and/or rosuvastatin (RSV) for treatment of dyslipidemia i... |
PMC5593164 | core_pubmed_pmc | Does Secretory Clearance Follow Glomerular Filtration Rate in Chronic Kidney Diseases? Reconsidering the Intact Nephron Hypothesis | Does Secretory Clearance Follow Glomerular Filtration Rate in Chronic Kidney Diseases? Reconsidering the Intact Nephron Hypothesis Abstract Abstract Drug‐dose modification in chronic kidney disease (CKD) utilizes glomerular filtration rate (GFR) with the implicit assumption that multiple renal excretory processes decli... |
PMC4552778 | core_pubmed_pmc | Pharmacokinetics of micafungin in subjects with severe hepatic dysfunction | Pharmacokinetics of micafungin in subjects with severe hepatic dysfunction Abstract Abstract Micafungin is an echinocandin with potent activity against a broad range of fungal species, including Candida species. The pharmacokinetic and safety profiles of micafungin have been evaluated in individuals with mild-to-modera... |
PMC10269399 | core_pubmed_pmc | A spatiotemporal computational model of focused ultrasound heat-induced nano-sized drug delivery system in solid tumors | A spatiotemporal computational model of focused ultrasound heat-induced nano-sized drug delivery system in solid tumors Abstract Abstract Focused Ultrasound (FUS)-triggered nano-sized drug delivery, as a smart stimuli-responsive system for treating solid tumors, is computationally investigated to enhance localized deli... |
PMC4768397 | core_pubmed_pmc | Optimal dose of gemcitabine for the treatment of biliary tract or pancreatic cancer in patients with liver dysfunction | Optimal dose of gemcitabine for the treatment of biliary tract or pancreatic cancer in patients with liver dysfunction Abstract A clear consensus does not exist about whether the initial dose of gemcitabine, an essential anticancer antimetabolite, should be reduced in patients with liver dysfunction. Adult patients wit... |
PMC12030717 | core_pubmed_pmc | Whole-Body Physiologically Based Pharmacokinetic Modeling Framework for Tissue Target Engagement of CD3 Bispecific Antibodies | Whole-Body Physiologically Based Pharmacokinetic Modeling Framework for Tissue Target Engagement of CD3 Bispecific Antibodies Abstract Abstract Background : T-cell-engaging bispecific (TCB) antibodies represent a promising therapy that utilizes T-cells to eliminate cancer cells independently of the major histocompatibi... |
PMC8841437 | core_pubmed_pmc | First‐in‐human study of milvexian, an oral, direct, small molecule factor XIa inhibitor | First‐in‐human study of milvexian, an oral, direct, small molecule factor XIa inhibitor Abstract Abstract Milvexian (BMS‐986177/JNJ‐70033093) is a small molecule, active‐site inhibitor of factor XIa (FXIa) being developed to prevent and treat thrombotic events. The safety, tolerability, pharmacokinetics (PKs), and phar... |
PMC9101287 | core_pubmed_pmc | In Vitro–In Vivo Correlation of Tianeptine Sodium Sustained-Release Dual-Layer Tablets | In Vitro–In Vivo Correlation of Tianeptine Sodium Sustained-Release Dual-Layer Tablets Abstract Abstract Tianeptine tablets are currently marketed to be designed for immediate-release tablets. The tianeptine has a short half-life, making it difficult to design for sustained-release tablets and achieve bioequivalence wi... |
PMC7024189 | core_pubmed_pmc | Simultaneous Quantitation of S(+)- and R(−)-Baclofen and Its Metabolite in Human Plasma and Cerebrospinal Fluid using LC–APCI–MS/MS: An Application for Clinical Studies | Simultaneous Quantitation of S(+)- and R(−)-Baclofen and Its Metabolite in Human Plasma and Cerebrospinal Fluid using LC–APCI–MS/MS: An Application for Clinical Studies Abstract Abstract Baclofen is a racemic mixture that is commonly used for the treatment for spasticity. However, the optimal dose and dosing interval t... |
PMC12028293 | core_pubmed_pmc | Pharmacokinetic Characterization of Labetalol in Pregnancy (The CLIP Study): A Prospective Observational Longitudinal Pharmacokinetic/Pharmacodynamic Cohort Study During Pregnancy and Postpartum | Pharmacokinetic Characterization of Labetalol in Pregnancy (The CLIP Study): A Prospective Observational Longitudinal Pharmacokinetic/Pharmacodynamic Cohort Study During Pregnancy and Postpartum Abstract Background/Objectives: Hypertensive disorders of pregnancy are a leading cause of pregnancy-related deaths in the Un... |
PMC9981362 | core_pubmed_pmc | Ustekinumab for steroid-refractory pancolitis in a biologically naive child: A case report and literature review | Ustekinumab for steroid-refractory pancolitis in a biologically naive child: A case report and literature review Abstract Ustekinumab is not recommended for the treatment of children with inflammatory bowel disease, but its off-label use is increasing despite a lack of pediatric pharmacokinetic data. The purpose of thi... |
PMC11304707 | core_pubmed_pmc | Pharmacokinetics and safety of GST-HG171, a novel 3CL protease inhibitor, in Chinese subjects with impaired and normal liver function | Pharmacokinetics and safety of GST-HG171, a novel 3CL protease inhibitor, in Chinese subjects with impaired and normal liver function Abstract ABSTRACT GST-HG171 is a potent, broad-spectrum, orally bioavailable small-molecule 3C-like (3CL) protease inhibitor that was recently approved for treating mild to moderate coro... |
PMC8773391 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Profile of a Novel Phospholipid Aspirin Formulation | Pharmacokinetic and Pharmacodynamic Profile of a Novel Phospholipid Aspirin Formulation Abstract Aspirin is one of the most widely used medicines. Although aspirin is commonly utilized for the treatment of several medical conditions, its broadest uptake is for the prevention of recurrent ischemic events in patients wit... |
PMC9298840 | core_pubmed_pmc | A Model‐Based Framework to Inform the Dose Selection and Study Design of Emicizumab for Pediatric Patients With Hemophilia A | A Model‐Based Framework to Inform the Dose Selection and Study Design of Emicizumab for Pediatric Patients With Hemophilia A Abstract Abstract Emicizumab is a bispecific antibody mimicking the cofactor function of activated coagulation factor VIII to prevent bleeds in patients with hemophilia A. The dose selection for ... |
PMC9415283 | core_pubmed_pmc | Pharmacokinetic Interaction between Atorvastatin and Omega-3 Fatty Acid in Healthy Volunteers | Pharmacokinetic Interaction between Atorvastatin and Omega-3 Fatty Acid in Healthy Volunteers Abstract Abstract The interaction between statins and omega-3 fatty acids remains controversial. The aim of this phase 1 trial was to evaluate the pharmacokinetics of drug-drug interaction between atorvastatin and omega-3 fatt... |
PMC11759765 | core_pubmed_pmc | A Quantitative Examination and Comparison of the Ability of Australian Gentamicin Dosing Guidelines to Achieve Target Therapeutic Concentrations in Neonates | A Quantitative Examination and Comparison of the Ability of Australian Gentamicin Dosing Guidelines to Achieve Target Therapeutic Concentrations in Neonates Abstract Abstract Background: Effective gentamicin dosing is crucial to the survival of neonates with suspected sepsis but requires a careful balance between attai... |
PMC9324075 | core_pubmed_pmc | Assessment of Antibiotic Pharmacokinetics, Molecular Biomarkers and Clinical Status in Critically Ill Adults Diagnosed with Community-Acquired Pneumonia and Receiving Intravenous Piperacillin/Tazobactam and Hydrocortisone over the First Five Days of Intensive Care: An Observational Study (STROBE Compliant) | Assessment of Antibiotic Pharmacokinetics, Molecular Biomarkers and Clinical Status in Critically Ill Adults Diagnosed with Community-Acquired Pneumonia and Receiving Intravenous Piperacillin/Tazobactam and Hydrocortisone over the First Five Days of Intensive Care: An Observational Study (STROBE Compliant) Abstract Sev... |
PMC9628234 | core_pubmed_pmc | Advances and challenges in using nirmatrelvir and its derivatives against SARS-CoV-2 infection | Advances and challenges in using nirmatrelvir and its derivatives against SARS-CoV-2 infection Abstract Abstract On December 22, 2021, the United States Food and Drug Administration approved the first main protease inhibitor, i.e., oral antiviral nirmatrelvir (PF-07321332)/ritonavir (Paxlovid), for the treatment of ear... |
PMC4047837 | core_pubmed_pmc | Evaluation of ceftiofur–PHBV microparticles in rats | Evaluation of ceftiofur–PHBV microparticles in rats Abstract Despite the high number of antibiotics used for the treatment of infectious disease in animals, the development of slow release formulations presents a significant challenge, particularly in using novel biomaterials with low cost. In this report, we studied t... |
PMC4705248 | core_pubmed_pmc | Comparative pharmacokinetics of a proliposome formulation of Ginkgo biloba extract and Ginaton in rats by a sensitive ultra performance liquid chromatography–tandem mass spectrometry method | Comparative pharmacokinetics of a proliposome formulation of Ginkgo biloba extract and Ginaton in rats by a sensitive ultra performance liquid chromatography–tandem mass spectrometry method Abstract As a novel oral drug delivery system, proliposome was applied to improve the solubility of active components of Ginkgo bi... |
PMC12547354 | core_pubmed_pmc | Network Modeling of Biomarker Systems in Liver Steatosis and Fibrosis | Network Modeling of Biomarker Systems in Liver Steatosis and Fibrosis Abstract ABSTRACT Metabolic dysfunction‐associated fatty liver disease causes hepatic fat accumulation (steatosis) and fibrosis, which can be measured with ultrasound elastography imaging. The dependencies of elastography‐derived hepatic steatosis an... |
PMC6033168 | core_pubmed_pmc | Greater early postprandial suppression of endogenous glucose production and higher initial glucose disappearance is achieved with fast‐acting insulin aspart compared with insulin aspart | Greater early postprandial suppression of endogenous glucose production and higher initial glucose disappearance is achieved with fast‐acting insulin aspart compared with insulin aspart Abstract Abstract Aim To investigate the mechanisms behind the lower postprandial glucose (PPG) concentrations achieved with fast‐acti... |
PMC4863535 | core_pubmed_pmc | Biochronomer™ technology and the development of APF530, a sustained release formulation of granisetron | Biochronomer™ technology and the development of APF530, a sustained release formulation of granisetron Abstract Abstract Granisetron and other 5-hydroxytryptamine type 3 (5-HT 3 ) receptor antagonists are first-line agents for preventing chemotherapy-induced nausea and vomiting (CINV). Current treatment guidelines pref... |
PMC11946194 | core_pubmed_pmc | Rational Design, Synthesis, and Biological Evaluation of Novel Thiazole/Thiazolidinones Multitarget Anti-Human Immunodeficiency Virus Molecules | Rational Design, Synthesis, and Biological Evaluation of Novel Thiazole/Thiazolidinones Multitarget Anti-Human Immunodeficiency Virus Molecules Abstract Background: HIV-1 RT inhibitors were the first drugs approved to treat AIDS and remain key components of highly active antiretroviral therapy (HAART). While HAART effe... |
PMC9379957 | core_pubmed_pmc | Phytochemical Characterization, Functional Nutrition, and Anti-Diabetic Potentials of Leptadenia hastata (pers) Decne Leaves: In Silico and In Vitro Studies | Phytochemical Characterization, Functional Nutrition, and Anti-Diabetic Potentials of Leptadenia hastata (pers) Decne Leaves: In Silico and In Vitro Studies Abstract The geometrical increase in diabetes mellitus (DM) and the undesirable side effects of synthetic drugs have intensified efforts to search for an effective... |
PMC8810372 | core_pubmed_pmc | Chemotherapeutic potential of hesperetin for cancer treatment, with mechanistic insights: A comprehensive review | Chemotherapeutic potential of hesperetin for cancer treatment, with mechanistic insights: A comprehensive review Abstract Background Cancer has become a significant concern in the medical sector with increasing disease complexity. Although some available conventional treatments are still a blessing for cancer patients,... |
PMC10131217 | core_pubmed_pmc | Plasma concentration of atorvastatin metabolites correlates with low‐density lipoprotein cholesterol reduction in patients with coronary heart disease | Plasma concentration of atorvastatin metabolites correlates with low‐density lipoprotein cholesterol reduction in patients with coronary heart disease Abstract Abstract In this exploratory study from a randomized double‐blinded crossover trial including 70 patients with coronary heart disease and self‐perceived muscula... |
PMC10070214 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Single and Multiple Doses of Mirogabalin in Healthy Chinese Participants: A Randomized, Double-Blind, Placebo-Controlled Study | Safety, Tolerability and Pharmacokinetics of Single and Multiple Doses of Mirogabalin in Healthy Chinese Participants: A Randomized, Double-Blind, Placebo-Controlled Study Abstract Introduction Mirogabalin is a treatment option for patients with neuropathic pain; however, safety, tolerability, and pharmacokinetics (PK)... |
PMC10154887 | core_pubmed_pmc | Pharmacokinetic and dose‐finding study of osimertinib in patients with impaired renal function and low body weight | Pharmacokinetic and dose‐finding study of osimertinib in patients with impaired renal function and low body weight Abstract Abstract The safety of osimertinib is limited in patients with severe or moderate renal impairment, or low body weight. This study aimed to investigate the safety, pharmacokinetics (PK) and recomm... |
PMC9124353 | core_pubmed_pmc | Erdafitinib’s effect on serum phosphate justifies its pharmacodynamically guided dosing in patients with cancer | Erdafitinib’s effect on serum phosphate justifies its pharmacodynamically guided dosing in patients with cancer Abstract Abstract A population pharmacokinetic (PK)–pharmacodynamic (PD) model was developed using data from 345 patients with cancer. The population PK‐PD model evaluated the effect of erdafitinib total and ... |
PMC5425333 | core_pubmed_pmc | Variants in Pharmacokinetic Transporters and Glycemic Response to Metformin: A Metgen Meta‐Analysis | Variants in Pharmacokinetic Transporters and Glycemic Response to Metformin: A Metgen Meta‐Analysis Abstract Abstract Therapeutic response to metformin, a first‐line drug for type 2 diabetes (T2D), is highly variable, in part likely due to genetic factors. To date, metformin pharmacogenetic studies have mainly focused ... |
PMC5364005 | core_pubmed_pmc | Treatment adherence in patients with type 2 diabetes mellitus correlates with different coping styles, low perception of self-influence on disease, and depressive symptoms | Treatment adherence in patients with type 2 diabetes mellitus correlates with different coping styles, low perception of self-influence on disease, and depressive symptoms Abstract Background Insulin analogs are regarded as more convenient to use than human insulin; however, they require a different administration sche... |
PMC9292930 | core_pubmed_pmc | Low immunogenicity of emicizumab in persons with haemophilia A | Low immunogenicity of emicizumab in persons with haemophilia A Abstract Abstract Introduction Emicizumab is a humanised, bispecific monoclonal antibody mimicking the cofactor function of activated factor (F)VIII. It is indicated for routine prophylaxis of bleeding episodes in persons with haemophilia A (PwHA) with/with... |
PMC11303286 | core_pubmed_pmc | In silico and in vitro chemometrics, cell toxicity and permeability of naringenin 8-sulphonate and derivatives | In silico and in vitro chemometrics, cell toxicity and permeability of naringenin 8-sulphonate and derivatives Abstract Background Sulphur containing natural compounds are among the most biologically relevant metabolites in vivo . Naringenin 8-sulphonate from Parinari excelsa Sabine was evaluated in a previous work, de... |
PMC3400177 | core_pubmed_pmc | Clinical pharmacokinetics of vancomycin in the neonate: a review | Clinical pharmacokinetics of vancomycin in the neonate: a review Abstract Abstract Neonatal sepsis is common and is a major cause of morbidity and mortality. Vancomycin is the preferred treatment of several neonatal staphylococcal infections. The aim of this study was to review published data on vancomycin pharmacokine... |
PMC9137037 | core_pubmed_pmc | Preclinical Studies of a Novel Human PD-1 B-Cell Peptide Cancer Vaccine PD1-Vaxx From BALB/c Mice to Beagle Dogs and to Non-Human Primates (Cynomolgus Monkeys) | Preclinical Studies of a Novel Human PD-1 B-Cell Peptide Cancer Vaccine PD1-Vaxx From BALB/c Mice to Beagle Dogs and to Non-Human Primates (Cynomolgus Monkeys) Abstract Abstract Immunotherapy with monoclonal antibodies to checkpoint inhibitors against the PD-1/PD-L1 signaling pathway is a landmark achievement in cancer... |
PMC6407740 | core_pubmed_pmc | Phase I Study of BI 853520, an Inhibitor of Focal Adhesion Kinase, in Patients with Advanced or Metastatic Nonhematologic Malignancies | Phase I Study of BI 853520, an Inhibitor of Focal Adhesion Kinase, in Patients with Advanced or Metastatic Nonhematologic Malignancies Abstract Background Overexpression/activation of focal adhesion kinase (FAK) in human malignancies has led to its evaluation as a therapeutic target. We report the first-in-human phase ... |
PMC9536304 | core_pubmed_pmc | Effect of chronic unpredicted mild stress-induced depression on clopidogrel pharmacokinetics in rats | Effect of chronic unpredicted mild stress-induced depression on clopidogrel pharmacokinetics in rats Abstract Background Clopidogrel is widely used to prevent and treat cardiovascular atherosclerosis and thrombosis. However, disturbance in the expression and activity of liver cytochrome metabolic enzymes significantly ... |
PMC5384759 | core_pubmed_pmc | Maternal Pharmacokinetics and Fetal Disposition of (±)-Citalopram during Mouse Pregnancy | Maternal Pharmacokinetics and Fetal Disposition of (±)-Citalopram during Mouse Pregnancy Abstract While selective-serotonin reuptake inhibitor (SSRI) antidepressants are commonly prescribed in the treatment of depression, their use during pregnancy leads to fetal drug exposures. According to recent reports, such exposu... |
PMC8569471 | core_pubmed_pmc | Pharmacokinetics of Orally Administered Prednisolone in Alpacas | Pharmacokinetics of Orally Administered Prednisolone in Alpacas Abstract This study aimed to determine the pharmacokinetics of prednisolone following intravenous and oral administration in healthy adult alpacas. Healthy adult alpacas were given prednisolone (IV, n = 4), as well as orally (PO, n = 6). Prednisolone was a... |
PMC8275539 | core_pubmed_pmc | Navigating the Regulatory Landscape to Develop Pediatric Oncology Drugs: Expert Opinion Recommendations | Navigating the Regulatory Landscape to Develop Pediatric Oncology Drugs: Expert Opinion Recommendations Abstract Regulatory changes have been enacted in the United States (US) and European Union (EU) to encourage the development of new treatments for pediatric cancer. Here, we review some of the factors that have hampe... |
PMC6881786 | core_pubmed_pmc | Serum Testosterone and Cortisol Concentrations After Single-Dose Administration of 100-Mg Transdermal Testosterone in Healthy Men | Serum Testosterone and Cortisol Concentrations After Single-Dose Administration of 100-Mg Transdermal Testosterone in Healthy Men Abstract Abstract The growing interest in testosterone's effects on men's social behaviors, in particular aggressive, risk-taking, or status maintenance behaviors, is accompanied by a paucit... |
PMC3224467 | core_pubmed_pmc | Colistin: recent data on pharmacodynamics properties and clinical efficacy in critically ill patients | Colistin: recent data on pharmacodynamics properties and clinical efficacy in critically ill patients Abstract Recent clinical studies performed in a large number of patients showed that colistin "forgotten" for several decades revived for the management of infections due to multidrug-resistant (MDR) Gram-negative bact... |
PMC5139813 | core_pubmed_pmc | Fidaxomicin for the Treatment of Clostridium Difficile Infection in the Pediatric Population - Not Quite So Soon Yet | Fidaxomicin for the Treatment of Clostridium Difficile Infection in the Pediatric Population - Not Quite So Soon Yet Abstract Fidaxomicin is a new narrow spectrum macrocyclic antibiotic. It inhibits bacterial RNA polymerase and eradicates C difficile with minimal effect on normal intestinal flora. The US FDA granted or... |
PMC8359335 | core_pubmed_pmc | Physiological parameter values for physiologically based pharmacokinetic models in food‐producing animals. Part II: Chicken and turkey | Physiological parameter values for physiologically based pharmacokinetic models in food‐producing animals. Part II: Chicken and turkey Abstract Abstract Physiologically based pharmacokinetic (PBPK) models are growing in popularity due to human food safety concerns and for estimating drug residue distribution and estima... |
PMC6875703 | core_pubmed_pmc | Evaluation of pharmacokinetics and safety of cetuximab with cisplatin/carboplatin in patients with advanced solid tumor: Result from phase II studies | Evaluation of pharmacokinetics and safety of cetuximab with cisplatin/carboplatin in patients with advanced solid tumor: Result from phase II studies Abstract Abstract The pharmacokinetics and potential drug–drug interactions between cetuximab and cisplatin or carboplatin from two studies (JXBA and JXBB) were evaluated... |
PMC8037586 | core_pubmed_pmc | Synthesis and Enantioselective Pharmacokinetic/Pharmacodynamic Analysis of New CNS-Active Sulfamoylphenyl Carbamate Derivatives | Synthesis and Enantioselective Pharmacokinetic/Pharmacodynamic Analysis of New CNS-Active Sulfamoylphenyl Carbamate Derivatives Abstract Abstract We recently reported a new class of carbamate derivatives as anticonvulsants. Among these, 3-methylpentyl(4-sulfamoylphenyl)carbamate (MSPC) stood out as the most potent comp... |
PMC11221101 | core_pubmed_pmc | In silico exploration of anti-prostate cancer compounds from differential expressed genes | In silico exploration of anti-prostate cancer compounds from differential expressed genes Abstract Abstract Prostate cancer (PCa) is a complex and biologically diverse disease with no curative treatment options at present. This study aims to utilize computational methods to explore potential anti-PCa compounds based on... |
PMC6393897 | core_pubmed_pmc | An LC-MS/MS Method for Simultaneous Determination of the Toxic and Active Components of Cortex Periplocae in Rat Plasma and Application to a Pharmacokinetic Study | An LC-MS/MS Method for Simultaneous Determination of the Toxic and Active Components of Cortex Periplocae in Rat Plasma and Application to a Pharmacokinetic Study Abstract A sensitive and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to simultaneously determine the ... |
PMC11946465 | core_pubmed_pmc | Preclinical Characterization of Efficacy and Pharmacodynamic Properties of Finotonlimab, a Humanized Anti-PD-1 Monoclonal Antibody | Preclinical Characterization of Efficacy and Pharmacodynamic Properties of Finotonlimab, a Humanized Anti-PD-1 Monoclonal Antibody Abstract Abstract Background/Objectives: Finotonlimab (SCTI10A) is a humanized anti-PD-1 antibody tested in Phase III trials for several solid tumor types. Methods : This study characterize... |
PMC5643369 | core_pubmed_pmc | Pharmacokinetic Profiles of Ticagrelor Orodispersible Tablets in Healthy Western and Japanese Subjects | Pharmacokinetic Profiles of Ticagrelor Orodispersible Tablets in Healthy Western and Japanese Subjects Abstract Background and Objectives Ticagrelor is an antiplatelet agent for patients with acute coronary syndrome or a history of myocardial infarction. Two studies compared pharmacokinetic profiles of orodispersible (... |
PMC10041964 | core_pubmed_pmc | A case report of brain abscess caused by carbapenem-resistant Klebsiella pneumoniae | A case report of brain abscess caused by carbapenem-resistant Klebsiella pneumoniae Abstract ABSTRACT The treatment of infections caused by carbapenem-resistant Klebsiella pneumoniae (CR-Kp) strains is difficult due to the limited antimicrobial options and high mortality. There are many reports on intracranial infectio... |
PMC12038220 | core_pubmed_pmc | Pharmacokinetics, Efficacy, and Safety of Upadacitinib in Pediatric Patients With Polyarticular‐Course Juvenile Idiopathic Arthritis: An Interim Analysis of an Open‐Label, Phase 1 Trial | Pharmacokinetics, Efficacy, and Safety of Upadacitinib in Pediatric Patients With Polyarticular‐Course Juvenile Idiopathic Arthritis: An Interim Analysis of an Open‐Label, Phase 1 Trial Abstract Objective This work aimed to evaluate the pharmacokinetics, efficacy, and safety of upadacitinib, an oral selective JAK inhib... |
PMC4047585 | core_pubmed_pmc | Comparison of pharmacokinetic behavior of two iridoid glycosides in rat plasma after oral administration of crude Cornus officinals and its jiuzhipin by high performance liquid chromatography triple quadrupole mass spectrometry combined with multiple reactions monitoring mode | Comparison of pharmacokinetic behavior of two iridoid glycosides in rat plasma after oral administration of crude Cornus officinals and its jiuzhipin by high performance liquid chromatography triple quadrupole mass spectrometry combined with multiple reactions monitoring mode Abstract Objective: The present study exami... |
PMC4422865 | core_pubmed_pmc | Semi-mechanistic Multiple-Analyte Pharmacokinetic Model for an Antibody-Drug-Conjugate in Cynomolgus Monkeys | Semi-mechanistic Multiple-Analyte Pharmacokinetic Model for an Antibody-Drug-Conjugate in Cynomolgus Monkeys Abstract Purpose A semi-mechanistic multiple-analyte population pharmacokinetics (PK) model was developed to describe the complex relationship between the different analytes of monomethyl auristatin E (MMAE) con... |
PMC7688542 | core_pubmed_pmc | Population pharmacokinetics of regorafenib in solid tumours: Exposure in clinical practice considering enterohepatic circulation and food intake | Population pharmacokinetics of regorafenib in solid tumours: Exposure in clinical practice considering enterohepatic circulation and food intake Abstract Abstract Aim Regorafenib is an oral multikinase inhibitor with clinical efficacy in a range of advanced solid tumours. A population pharmacokinetic (PK) model was dev... |
PMC5882782 | core_pubmed_pmc | Innovative Nanoparticles Enhance N -Palmitoylethanolamide Intraocular Delivery | Innovative Nanoparticles Enhance N -Palmitoylethanolamide Intraocular Delivery Abstract Abstract Nanostructured lipid carriers (NLCs) loaded with palmitoylethanolamide (PEA) were formulated with the aim to enhance ocular bioavailability of PEA, particularly to the back of the eye. Technological characterization (e.g., ... |
PMC4706584 | core_pubmed_pmc | Population pharmacokinetic and exposure–response analysis for trastuzumab administered using a subcutaneous “manual syringe” injection or intravenously in women with HER2-positive early breast cancer | Population pharmacokinetic and exposure–response analysis for trastuzumab administered using a subcutaneous “manual syringe” injection or intravenously in women with HER2-positive early breast cancer Abstract Abstract Purpose To characterize the population pharmacokinetics (PKs) of subcutaneous (SC) and intravenous (IV... |
PMC5418443 | core_pubmed_pmc | First-in-human phase 1 of YS110, a monoclonal antibody directed against CD26 in advanced CD26-expressing cancers | First-in-human phase 1 of YS110, a monoclonal antibody directed against CD26 in advanced CD26-expressing cancers Abstract Abstract Background: YS110 is a humanised IgG1 monoclonal antibody with high affinity to the CD26 antigen. YS110 demonstrated preclinical anti-tumour effects without significant side effects. Method... |
PMC7522226 | core_pubmed_pmc | Resveratrol stereoselectively affected (±)warfarin pharmacokinetics and enhanced the anticoagulation effect | Resveratrol stereoselectively affected (±)warfarin pharmacokinetics and enhanced the anticoagulation effect Abstract Abstract Resveratrol (RVT) has various beneficial bioactivities and popularly used as a dietary supplement. RVT showed inhibitions on CYP1A2/2C9/3A4, breast cancer resistance protein (BCRP), and some con... |
PMC12319425 | core_pubmed_pmc | A Comparative Study of Sugammadex and Neostigmine: A Bibliometric Analysis of the Past 15 Years | A Comparative Study of Sugammadex and Neostigmine: A Bibliometric Analysis of the Past 15 Years Abstract Abstract Purpose Sugammadex is a novel selective relaxant binding agent for aminosteroid neuromuscular blocking agents (NMBAs). However, existing literature reveals major knowledge gaps regarding its current applica... |
PMC5461644 | core_pubmed_pmc | Novel SGLT 2 inhibitor: first‐in‐man studies of antisense compound is associated with unexpected renal effects | Novel SGLT 2 inhibitor: first‐in‐man studies of antisense compound is associated with unexpected renal effects Abstract Abstract The antisense compound ISIS 388626 selectively inhibits renal glucose reabsorption by inhibiting the sodium–glucose cotransporter‐2 ( SGLT 2) mRNA expression. It is developed as an insulin‐in... |
PMC4480847 | core_pubmed_pmc | Safety, pharmacodynamics, and pharmacokinetics of multiple oral doses of delta-9-tetrahydrocannabinol in older persons with dementia | Safety, pharmacodynamics, and pharmacokinetics of multiple oral doses of delta-9-tetrahydrocannabinol in older persons with dementia Abstract Abstract Rationale Data on safety, pharmacodynamics, and pharmacokinetics of tetrahydrocannabinol (THC) are lacking in dementia patients. Methods In this randomized, double-blind... |
PMC11835432 | core_pubmed_pmc | TMS and EEG Pharmacodynamic Effects of a Selective Sphingosine‐1‐Phosphate Subtype 1 Receptor Agonist on Cortical Excitability in Healthy Subjects | TMS and EEG Pharmacodynamic Effects of a Selective Sphingosine‐1‐Phosphate Subtype 1 Receptor Agonist on Cortical Excitability in Healthy Subjects Abstract Abstract Current anti‐epileptic drugs lack efficacy, cause many side effects and one third of all patients are treatment‐resistant. Drugs targeting the sphingosine‐... |
PMC10674911 | core_pubmed_pmc | Bombesins: A New Frontier in Hybrid Compound Development | Bombesins: A New Frontier in Hybrid Compound Development Abstract Recently, bombesin (BN) and its analogs have attracted much attention as excellent anticancer agents because they interact with specific receptors widely distributed on the surface of various cancer cells. However, their biological properties proceed far... |
PMC6269848 | core_pubmed_pmc | Metal Complexes of Quinolone Antibiotics and Their Applications: An Update | Metal Complexes of Quinolone Antibiotics and Their Applications: An Update Abstract Abstract Quinolones are synthetic broad-spectrum antibiotics with good oral absorption and excellent bioavailability. Due to the chemical functions found on their nucleus (a carboxylic acid function at the 3-position, and in most cases ... |
PMC8761875 | core_pubmed_pmc | Methyl β-D-galactopyranoside esters as potential inhibitors for SARS-CoV-2 protease enzyme: synthesis, antimicrobial, PASS, molecular docking, molecular dynamics simulations and quantum computations | Methyl β-D-galactopyranoside esters as potential inhibitors for SARS-CoV-2 protease enzyme: synthesis, antimicrobial, PASS, molecular docking, molecular dynamics simulations and quantum computations Abstract Carbohydrate esters are significant in medicinal chemistry because of their efficacy for the synthesis of biolog... |
PMC11054906 | core_pubmed_pmc | A Population Pharmacokinetic Study to Compare a Novel Empagliflozin L-Proline Formulation with Its Conventional Formulation in Healthy Subjects | A Population Pharmacokinetic Study to Compare a Novel Empagliflozin L-Proline Formulation with Its Conventional Formulation in Healthy Subjects Abstract Abstract Empagliflozin is a sodium–glucose cotransporter 2 (SGLT2) inhibitor that is commonly used for the treatment of type 2 diabetes mellitus (T2DM). CKD-370 was ne... |
PMC6262174 | core_pubmed_pmc | Resveratrol Brain Delivery for Neurological Disorders Prevention and Treatment | Resveratrol Brain Delivery for Neurological Disorders Prevention and Treatment Abstract Resveratrol (RES) is a natural polyphenolic non-flavonoid compound present in grapes, mulberries, peanuts, rhubarb and in several other plants. Numerous health effects have been related with its intake, such as anti-carcinogenic, an... |
PMC6901059 | core_pubmed_pmc | Spray-Dried Silica Xerogel Nanoparticles as a Promising Gastroretentive Carrier System for the Management of Chemotherapy-Induced Nausea and Vomiting | Spray-Dried Silica Xerogel Nanoparticles as a Promising Gastroretentive Carrier System for the Management of Chemotherapy-Induced Nausea and Vomiting Abstract Abstract Purpose The current work aimed to develop spray-dried silica xerogel nanoparticles (SXNs) as a gastroretentive carrier for the dual delivery of chloramb... |
PMC12659736 | core_pubmed_pmc | LUMIADE 3: Therapeutic Equivalence of Denosumab Biosimilar FKS518 to Reference Product in Postmenopausal Osteoporosis | LUMIADE 3: Therapeutic Equivalence of Denosumab Biosimilar FKS518 to Reference Product in Postmenopausal Osteoporosis Abstract Abstract Objectives To demonstrate therapeutic equivalence of the proposed denosumab biosimilar FKS518 to the originator denosumab (US-licensed Prolia®, reference product), a potent antiresorpt... |
PMC12292961 | core_pubmed_pmc | Microbial Crosstalk with Therapy: Pharmacomicrobiomics in AML—One Step Closer to Personalized Medicine | Microbial Crosstalk with Therapy: Pharmacomicrobiomics in AML—One Step Closer to Personalized Medicine Abstract Abstract Increasing evidence demonstrates the mutualistic connection between the microbiome and acute myeloid leukemia (AML) treatment. Drugs disrupt the microbial balance and, conversely, changes in the micr... |
PMC4354355 | core_pubmed_pmc | Serotonin versus catecholamine deficiency: behavioral and neural effects of experimental depletion in remitted depression | Serotonin versus catecholamine deficiency: behavioral and neural effects of experimental depletion in remitted depression Abstract Abstract Despite immense efforts into development of new antidepressant drugs, the increases of serotoninergic and catecholaminergic neurotransmission have remained the two major pharmacody... |
PMC11215542 | core_pubmed_pmc | Antifungal drug penetration in soft tissue abscesses: a comparative analysis | Antifungal drug penetration in soft tissue abscesses: a comparative analysis Abstract Abstract Background Invasive fungal infections (IFIs) are severe and difficult-to-treat infections affecting immunocompromised patients. Antifungal drug penetration at the site of infection is critical for outcome and may be difficult... |
PMC8891099 | core_pubmed_pmc | Finerenone Dose-Exposure-Response for the Primary Kidney Outcome in FIDELIO-DKD Phase III: Population Pharmacokinetic and Time-to-Event Analysis | Finerenone Dose-Exposure-Response for the Primary Kidney Outcome in FIDELIO-DKD Phase III: Population Pharmacokinetic and Time-to-Event Analysis Abstract Abstract Background Finerenone is a nonsteroidal selective mineralocorticoid receptor antagonist that recently demonstrated efficacy in delaying chronic kidney diseas... |
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