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PMC6354162 | core_pubmed_pmc | Development of a MD-LC-MS/MS Method to Analyze 3 Bioactive Compounds in Huoxuezhitong Rubber Patch and Application to a Pharmacokinetic Study in Rats | Development of a MD-LC-MS/MS Method to Analyze 3 Bioactive Compounds in Huoxuezhitong Rubber Patch and Application to a Pharmacokinetic Study in Rats Abstract Abstract Huoxuezhitong rubber patch, a well-known traditional Chinese medicine (TCM) prescription, is utilized to treat pain and inflammation. In this study, a m... |
PMC12789875 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Single Doses of ABBV‐916, an Anti‐Amyloid Antibody, in Healthy Participants | Safety, Tolerability, and Pharmacokinetics of Single Doses of ABBV‐916, an Anti‐Amyloid Antibody, in Healthy Participants Abstract ABSTRACT Amyloid‐beta (Aβ) plaque brain clearance is one of the promising disease‐modifying treatment approaches to slow cognitive decline in Alzheimer's disease (AD). ABBV‐916, an anti‐amy... |
PMC6585654 | core_pubmed_pmc | Impact on HbA1c and body weight of switching from other GLP‐1 receptor agonists to semaglutide: A model‐based approach | Impact on HbA1c and body weight of switching from other GLP‐1 receptor agonists to semaglutide: A model‐based approach Abstract Abstract Aims Semaglutide is a glucagon‐like peptide‐1 (GLP‐1) analogue approved for the treatment of type 2 diabetes. The impact of switching treatment from another GLP‐1 receptor agonist (GL... |
PMC5069300 | core_pubmed_pmc | Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide | Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide Abstract Abstract Two novel oral drugs that target androgen signaling have recently become available for the treatment of metastatic castration-resistant prostate cancer (mC... |
PMC10748085 | core_pubmed_pmc | Body Surface Area-Based Dosing of Mycophenolate Mofetil in Pediatric Hematopoietic Stem Cell Transplant Recipients: A Prospective Population Pharmacokinetic Study | Body Surface Area-Based Dosing of Mycophenolate Mofetil in Pediatric Hematopoietic Stem Cell Transplant Recipients: A Prospective Population Pharmacokinetic Study Abstract Mycophenolate mofetil (MMF) is commonly used for acute graft-versus-host disease (aGVHD) after allogeneic hematopoietic stem cell transplantation (H... |
PMC6559771 | core_pubmed_pmc | Solutol ® HS15+pluronicF127 and Solutol ® HS15+pluronicL61 mixed micelle systems for oral delivery of genistein | Solutol ® HS15+pluronicF127 and Solutol ® HS15+pluronicL61 mixed micelle systems for oral delivery of genistein Abstract Abstract Purpose: We aimed to prepare two oral drug delivery systems consisting of polyoxyl 15 hydroxystearate (HS15) with pluronicF127 (F127) and HS15 with pluronicL61 (L61) to overcome the challeng... |
PMC10003857 | core_pubmed_pmc | Impact of Pomegranate Juice on the Pharmacokinetics of CYP3A4- and CYP2C9-Mediated Drugs Metabolism: A Preclinical and Clinical Review | Impact of Pomegranate Juice on the Pharmacokinetics of CYP3A4- and CYP2C9-Mediated Drugs Metabolism: A Preclinical and Clinical Review Abstract The Punica granatum L. (pomegranate) fruit juice contains large amounts of polyphenols, mainly tannins such as ellagitannin, punicalagin, and punicalin, and flavonoids such as ... |
PMC7035259 | core_pubmed_pmc | T-13 and T-26, the novel taxanes with improved oral bioavailability in rats | T-13 and T-26, the novel taxanes with improved oral bioavailability in rats Abstract Abstract In an attempt to improve the oral bioavailability of taxanes, a series of new analogues were synthesized and tested in a panel of human tumor cell lines and cellular permeability assays. Compounds T-13 and T-26 showed potent c... |
PMC12324101 | core_pubmed_pmc | Structure-based identification of bioactive compounds as trace amine-associated receptor 1 agonists for the therapeutic management of major depressive disorder | Structure-based identification of bioactive compounds as trace amine-associated receptor 1 agonists for the therapeutic management of major depressive disorder Abstract The global burden of major depressive disorder (MDD) drives ongoing efforts to develop safer and more targeted treatment strategies. Modern advances ha... |
PMC6161670 | core_pubmed_pmc | Cereblon modulator iberdomide induces degradation of the transcription factors Ikaros and Aiolos: immunomodulation in healthy volunteers and relevance to systemic lupus erythematosus | Cereblon modulator iberdomide induces degradation of the transcription factors Ikaros and Aiolos: immunomodulation in healthy volunteers and relevance to systemic lupus erythematosus Abstract Objectives IKZF1 and IKZF3 ( encoding transcription factors Ikaros and Aiolos) are susceptibility loci for systemic lupus erythe... |
PMC6977225 | core_pubmed_pmc | Modern pharmacological treatment of obese patients | Modern pharmacological treatment of obese patients Abstract Abstract There are many angles to consider in drug treatment of obese patients. On the one hand, some specific weight loss drugs are available, on the other, several drugs are associated with unintentional weight changes. When treating an obese patient for any... |
PMC10357448 | core_pubmed_pmc | Design of Glycoengineered IL-4 Antagonists Employing Chemical and Biosynthetic Glycosylation | Design of Glycoengineered IL-4 Antagonists Employing Chemical and Biosynthetic Glycosylation Abstract Interleukin-4 (IL-4) plays a key role in atopic diseases. It coordinates T-helper cell differentiation to subtype 2, thereby directing defense toward humoral immunity. Together with Interleukin-13, IL-4 further induces... |
PMC5908825 | core_pubmed_pmc | A Pharmacometric Analysis of Patient-Reported Outcomes in Breast Cancer Patients Through Item Response Theory | A Pharmacometric Analysis of Patient-Reported Outcomes in Breast Cancer Patients Through Item Response Theory Abstract Purpose An item response theory (IRT) pharmacometric framework is presented to characterize Functional Assessment of Cancer Therapy-Breast (FACT-B) data in locally-advanced or metastatic breast cancer ... |
PMC2819904 | core_pubmed_pmc | Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles | Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles Abstract Efforts to improve the oral bioavailability of cyclosporine A (CyA) remains a challenge in the field of drug delivery. In this study, glyceryl monooleate (GM... |
PMC12968514 | core_pubmed_pmc | Pharmacokinetic Parameters of Oral Firocoxib, Oral Meloxicam, and Transdermal Flunixin in Meat Type Goats | Pharmacokinetic Parameters of Oral Firocoxib, Oral Meloxicam, and Transdermal Flunixin in Meat Type Goats Abstract ABSTRACT The objective of this study was to determine and compare the pharmacokinetics of oral firocoxib, oral meloxicam, and transdermal flunixin (TD) in 44 adult, male castrated, crossbred goats. Pharmac... |
PMC10436462 | core_pubmed_pmc | Targeting FSCN1 with an oral small-molecule inhibitor for treating ocular neovascularization | Targeting FSCN1 with an oral small-molecule inhibitor for treating ocular neovascularization Abstract Abstract Background Ocular neovascularization is a leading cause of blindness and visual impairment. While intravitreal anti-VEGF agents can be effective, they do have several drawbacks, such as endophthalmitis and dru... |
PMC10005657 | core_pubmed_pmc | The Metabolites and Mechanism Analysis of Genistin against Hyperlipidemia via the UHPLC-Q-Exactive Orbitrap Mass Spectrometer and Metabolomics | The Metabolites and Mechanism Analysis of Genistin against Hyperlipidemia via the UHPLC-Q-Exactive Orbitrap Mass Spectrometer and Metabolomics Abstract Genistin, an isoflavone, has been reported to have multiple activities. However, its improvement of hyperlipidemia is still unclear, and the same is true with regard to... |
PMC11422154 | core_pubmed_pmc | Development of a novel intramuscular liposomal injection for advanced meloxicam delivery: Preparation, characterization, in vivo pharmacokinetics, pharmacodynamics, and pain assessment in an orthopedic pain model | Development of a novel intramuscular liposomal injection for advanced meloxicam delivery: Preparation, characterization, in vivo pharmacokinetics, pharmacodynamics, and pain assessment in an orthopedic pain model Abstract Pain produces several physiological, and degenerative complications. This study aimed to formulate... |
PMC11297089 | core_pubmed_pmc | CPL-01, an investigational long-acting ropivacaine, demonstrates safety and efficacy in open inguinal hernia repair | CPL-01, an investigational long-acting ropivacaine, demonstrates safety and efficacy in open inguinal hernia repair Abstract Background There is an unmet medical need for effective nonopioid analgesics that can decrease pain while reducing systemic opioid use. CPL-01, an extended-release injectable formulation of ropiv... |
PMC12722941 | core_pubmed_pmc | Effects of bolus injection rate on the pharmacodynamics and pharmacokinetics of propofol, etomidate and sufentanil in rats | Effects of bolus injection rate on the pharmacodynamics and pharmacokinetics of propofol, etomidate and sufentanil in rats Abstract Introduction The preclinical phase of innovative drug research and development involves a comprehensive assessment of multiple variables that may influence therapeutic outcomes and safety ... |
PMC10740422 | core_pubmed_pmc | Pharmacokinetics, Tissue Residues, and Withdrawal Times of Oxytetracycline in Rainbow Trout ( Oncorhynchus mykiss ) after Single- and Multiple-Dose Oral Administration | Pharmacokinetics, Tissue Residues, and Withdrawal Times of Oxytetracycline in Rainbow Trout ( Oncorhynchus mykiss ) after Single- and Multiple-Dose Oral Administration Abstract Simple Summary Determination of the pharmacokinetics of oxytetracycline (OTC) at single and multiple oral doses revealed its long half-life, ve... |
PMC8476882 | core_pubmed_pmc | Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Genetic Variants: In Vitro Functional Characterization and Association With Circulating Concentrations of Endogenous Substrates | Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Genetic Variants: In Vitro Functional Characterization and Association With Circulating Concentrations of Endogenous Substrates Abstract Organic anion transporting polypeptide 2B1 (OATP2B1, gene SLCO2B1 ) is an uptake transporter that is thought to determine drug dis... |
PMC3713598 | core_pubmed_pmc | Renal Protective Role of Xiexin Decoction with Multiple Active Ingredients Involves Inhibition of Inflammation through Downregulation of the Nuclear Factor- κ B Pathway in Diabetic Rats | Renal Protective Role of Xiexin Decoction with Multiple Active Ingredients Involves Inhibition of Inflammation through Downregulation of the Nuclear Factor- κ B Pathway in Diabetic Rats Abstract In Chinese medicine, Xiexin decoction (XXD) has been used for the clinical treatment of diabetes for at least 1700 years. The... |
PMC11771652 | core_pubmed_pmc | Pharmacodynamic Exposure–Response Analysis of Fracture Count Data Following Treatment with Burosumab in Patients with XLH | Pharmacodynamic Exposure–Response Analysis of Fracture Count Data Following Treatment with Burosumab in Patients with XLH Abstract Abstract X‐linked hypophosphatemia (XLH) is a rare genetic disorder caused by excessive fibroblast growth factor 23 (FGF23), leading to low serum phosphate levels resulting in increased ris... |
PMC10202199 | core_pubmed_pmc | The Influence of Cytochrome P450 Polymorphisms on Pharmacokinetic Profiles and Treatment Outcomes Among Malaria Patients in Sub-Saharan Africa: A Systematic Review | The Influence of Cytochrome P450 Polymorphisms on Pharmacokinetic Profiles and Treatment Outcomes Among Malaria Patients in Sub-Saharan Africa: A Systematic Review Abstract Background Sub-Saharan Africa (SSA) population is genetically diverse and heterogenous thus variability in drug response among individuals is predi... |
PMC5395234 | core_pubmed_pmc | Spectrophotometric and molecular modelling studies on in vitro interaction of tyrosine kinase inhibitor linifanib with bovine serum albumin | Spectrophotometric and molecular modelling studies on in vitro interaction of tyrosine kinase inhibitor linifanib with bovine serum albumin Abstract Linifanib (LNF) possess antitumor activity and acts by inhibiting receptor tyrosine kinase VEGF and PDGF. The interaction of BSA with the drug can provide valuable informa... |
PMC10975777 | core_pubmed_pmc | Advancing Precision Medicine: A Review of Innovative In Silico Approaches for Drug Development, Clinical Pharmacology and Personalized Healthcare | Advancing Precision Medicine: A Review of Innovative In Silico Approaches for Drug Development, Clinical Pharmacology and Personalized Healthcare Abstract The landscape of medical treatments is undergoing a transformative shift. Precision medicine has ushered in a revolutionary era in healthcare by individualizing diag... |
PMC9235044 | core_pubmed_pmc | Computational exploration of maternal embryonic leucine zipper kinase (MELK) as a cancer drug target | Computational exploration of maternal embryonic leucine zipper kinase (MELK) as a cancer drug target Abstract Maternal embryonic leucine zipper kinase (MELK) is of vital importance due to its significant role in cancer development and its association with poor prognosis in different cancers. Here, we employed several c... |
PMC3033367 | core_pubmed_pmc | Pharmacodynamic Modeling of Anti-Cancer Activity of Tetraiodothyroacetic Acid in a Perfused Cell Culture System | Pharmacodynamic Modeling of Anti-Cancer Activity of Tetraiodothyroacetic Acid in a Perfused Cell Culture System Abstract Abstract Unmodified or as a poly[lactide-co-glycolide] nanoparticle, tetraiodothyroacetic acid (tetrac) acts at the integrin αvβ3 receptor on human cancer cells to inhibit tumor cell proliferation an... |
PMC8602549 | core_pubmed_pmc | Apixaban Pharmacokinetics and Pharmacodynamics in Subjects with Mild or Moderate Hepatic Impairment | Apixaban Pharmacokinetics and Pharmacodynamics in Subjects with Mild or Moderate Hepatic Impairment Abstract Abstract Background Hepatic impairment can impact apixaban pharmacokinetics and pharmacodynamics by decreasing cytochrome P450-mediated metabolism and factor X production. Objective This study evaluated the effe... |
PMC11729890 | core_pubmed_pmc | Probabilistic nested model selection in pharmacokinetic analysis of DCE-MRI data in animal model of cerebral tumor | Probabilistic nested model selection in pharmacokinetic analysis of DCE-MRI data in animal model of cerebral tumor Abstract Abstract Best current practice in the analysis of dynamic contrast enhanced (DCE)-MRI is to employ a voxel-by-voxel model selection from a hierarchy of nested models. This nested model selection (... |
PMC8414630 | core_pubmed_pmc | Sodium-Glucose Cotransporter 2 (SGLT-2) Inhibitors: Delving Into the Potential Benefits of Cardiorenal Protection Beyond the Treatment of Type-2 Diabetes Mellitus | Sodium-Glucose Cotransporter 2 (SGLT-2) Inhibitors: Delving Into the Potential Benefits of Cardiorenal Protection Beyond the Treatment of Type-2 Diabetes Mellitus Abstract Abstract Diabetes mellitus is a leading cause of morbidity and mortality and a significant risk factor for the early onset of chronic kidney disease... |
PMC12115012 | core_pubmed_pmc | Isoetin from Isoetaceae Exhibits Superior Pentatransferase Inhibition in Breast Cancer: Comparative Computational Profiling with FDA-Approved Tucatinib | Isoetin from Isoetaceae Exhibits Superior Pentatransferase Inhibition in Breast Cancer: Comparative Computational Profiling with FDA-Approved Tucatinib Abstract Background: Breast cancer, the most prevalent cancer among women globally, develops primarily in the breast’s ducts or lobules. Drug resistance is a significan... |
PMC6787836 | core_pubmed_pmc | Nanoparticles in the Treatment of Infections Caused by Multidrug-Resistant Organisms | Nanoparticles in the Treatment of Infections Caused by Multidrug-Resistant Organisms Abstract Abstract Nanotechnology using nanoscale materials is increasingly being utilized for clinical applications, especially as a new paradigm for infectious diseases. Infections caused by multidrug-resistant organisms (MDROs) are e... |
PMC8510649 | core_pubmed_pmc | Microbial Therapeutics in Neurocognitive and Psychiatric Disorders | Microbial Therapeutics in Neurocognitive and Psychiatric Disorders Abstract Microbial therapeutics, which include gut biotics and fecal transplantation, are interventions designed to improve the gut microbiome. Gut biotics can be considered as the administration of direct microbial populations. The delivery of this can... |
PMC5561493 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Bortezomib in Pediatric Leukemia Patients: Model‐Based Support for Body Surface Area‐Based Dosing Over the 2‐ to 16‐Year Age Range | Population Pharmacokinetic Analysis of Bortezomib in Pediatric Leukemia Patients: Model‐Based Support for Body Surface Area‐Based Dosing Over the 2‐ to 16‐Year Age Range Abstract Abstract This population analysis described the pharmacokinetics of bortezomib after twice‐weekly, repeat‐dose, intravenous administration in... |
PMC3892687 | core_pubmed_pmc | Topological augmentation to infer hidden processes in biological systems | Topological augmentation to infer hidden processes in biological systems Abstract Abstract Motivation: A common problem in understanding a biochemical system is to infer its correct structure or topology. This topology consists of all relevant state variables—usually molecules and their interactions. Here we present a ... |
PMC4228482 | core_pubmed_pmc | The co-use of conventional drugs and herbs among patients in Norwegian general practice: a cross-sectional study | The co-use of conventional drugs and herbs among patients in Norwegian general practice: a cross-sectional study Abstract Abstract Background Different patient groups are known to use herbal remedies and conventional drugs concomitantly (co-use). This poses a potential risk of herb-drug interaction through altering the... |
PMC10746618 | core_pubmed_pmc | Assessing Dose-Exposure–Response Relationships of Miltefosine in Adults and Children using Physiologically-Based Pharmacokinetic Modeling Approach | Assessing Dose-Exposure–Response Relationships of Miltefosine in Adults and Children using Physiologically-Based Pharmacokinetic Modeling Approach Abstract Abstract Objectives Miltefosine is the first and only oral medication to be successfully utilized as an antileishmanial agent. However, the drug is associated with ... |
PMC12649201 | core_pubmed_pmc | β-Lactam/β-Lactamase Inhibitor Combinations in Sepsis-Associated Acute Kidney Injury and Renal Replacement Therapy | β-Lactam/β-Lactamase Inhibitor Combinations in Sepsis-Associated Acute Kidney Injury and Renal Replacement Therapy Abstract Sepsis-associated acute kidney injury (SA-AKI) often requires renal replacement therapy (RRT), which markedly alters antimicrobial pharmacokinetics (PK) and pharmacodynamics (PD). Novel β-lactam/β... |
PMC11539713 | core_pubmed_pmc | CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency | CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency Abstract Abstract Background The most widely used anti-malarial drug artemisinin (ART) is metabolized extensively, but the therapeutic capacity of its major metabolite remains unknown. Whether the major metabolite ... |
PMC9762530 | core_pubmed_pmc | Association Between Body Mass Index and Response to Disease-Modifying Therapies in Patients With Relapsing-Remitting Multiple Sclerosis at King Abdulaziz University Hospital: A Retrospective Study | Association Between Body Mass Index and Response to Disease-Modifying Therapies in Patients With Relapsing-Remitting Multiple Sclerosis at King Abdulaziz University Hospital: A Retrospective Study Abstract Abstract Background Multiple sclerosis (MS) is an immune-mediated inflammatory disease that attacks myelinated axo... |
PMC12491529 | core_pubmed_pmc | Sedative potential of palmatine chloride in thiopental sodium-induced chicks: evidence from in vivo and in Silico studies | Sedative potential of palmatine chloride in thiopental sodium-induced chicks: evidence from in vivo and in Silico studies Abstract The aim of this study is to assess the sedative impact of palmatine chloride (PME) in thiopental sodium-induced sleeping chicks and its underlying molecular mechanism by using in vivo and i... |
PMC12296705 | core_pubmed_pmc | In Vivo and Bioinformatics Evaluation of Nine Traditional Chinese Medicine Compounds Targeting Acetylcholinesterase and Butyrylcholinesterase Enzymes in Alzheimer’s Disease | In Vivo and Bioinformatics Evaluation of Nine Traditional Chinese Medicine Compounds Targeting Acetylcholinesterase and Butyrylcholinesterase Enzymes in Alzheimer’s Disease Abstract Background Alzheimer’s disease (AD) is characterized by cholinergic dysfunction and oxidative stress, creating a need for the development ... |
PMC4023067 | core_pubmed_pmc | Pharmacokinetics and bioavailability of single dose ibuprofen and pseudoephedrine alone or in combination: a randomized three-period, cross-over trial in healthy Indian volunteers | Pharmacokinetics and bioavailability of single dose ibuprofen and pseudoephedrine alone or in combination: a randomized three-period, cross-over trial in healthy Indian volunteers Abstract Objective: To compare the bioavailability of single dose ibuprofen 200 mg and pseudoephedrine hydrochloride 30 mg administered alon... |
PMC10779128 | core_pubmed_pmc | Development and Characterization of 99m Tc-scFvD2B as a Potential Radiopharmaceutical for SPECT Imaging of Prostate Cancer | Development and Characterization of 99m Tc-scFvD2B as a Potential Radiopharmaceutical for SPECT Imaging of Prostate Cancer Abstract Previously, we demonstrated that the 177 Lu-labeled single-chain variable fragment of an anti-prostate-specific membrane antigen (PSMA) IgG D2B antibody (scFvD2B) showed higher prostate ca... |
PMC5360941 | core_pubmed_pmc | Simultaneous Determination and Pharmacokinetic Study of Quercetin, Luteolin, and Apigenin in Rat Plasma after Oral Administration of Matricaria chamomilla L. Extract by HPLC-UV | Simultaneous Determination and Pharmacokinetic Study of Quercetin, Luteolin, and Apigenin in Rat Plasma after Oral Administration of Matricaria chamomilla L. Extract by HPLC-UV Abstract A simple and sensitive HPLC-UV method has been developed for the simultaneous determination of quercetin, luteolin, and apigenin in ra... |
PMC11925552 | core_pubmed_pmc | Delayed Onset of Spinal Anesthesia in a Chronic Opioid User Undergoing Cesarean Section | Delayed Onset of Spinal Anesthesia in a Chronic Opioid User Undergoing Cesarean Section Abstract Delayed onset of spinal anesthesia can pose challenges during cesarean section (CS) in patients with a history of chronic opioid use. We present a case of delayed onset of spinal anesthesia in a patient with chronic opioid ... |
PMC12743846 | core_pubmed_pmc | Ibrutinib oral suspension bioavailability and compatibility for optimal enteral administration route | Ibrutinib oral suspension bioavailability and compatibility for optimal enteral administration route Abstract Abstract Background: Ibrutinib is the only Bruton tyrosine kinase inhibitor (BTKi) with once-daily oral capsule, tablet, and oral suspension formulations approved in the United States across indications of chro... |
PMC6534336 | core_pubmed_pmc | Pharmacokinetics of oral and subcutaneous meloxicam: Effect on indicators of pain and inflammation after knife castration in weaned beef calves | Pharmacokinetics of oral and subcutaneous meloxicam: Effect on indicators of pain and inflammation after knife castration in weaned beef calves Abstract Abstract Oral meloxicam is labelled for reducing pain and inflammation associated with castration in cattle in Canada, however, subcutaneous meloxicam is only labelled... |
PMC9911583 | core_pubmed_pmc | Single-time-point dosimetry using model selection and nonlinear mixed-effects modelling: a proof of concept | Single-time-point dosimetry using model selection and nonlinear mixed-effects modelling: a proof of concept Abstract Purpose This project aims to develop and evaluate a method for accurately determining time-integrated activities (TIAs) in single-time-point (STP) dosimetry for molecular radiotherapy. It performs a mode... |
PMC10102643 | core_pubmed_pmc | A mass balance study of [ 14 C]SHR6390 (dalpiciclib), a selective and potent CDK4/6 inhibitor in humans | A mass balance study of [ 14 C]SHR6390 (dalpiciclib), a selective and potent CDK4/6 inhibitor in humans Abstract SHR6390 (dalpiciclib) is a selective and effective cyclin-dependent kinase (CDK) 4/6 inhibitor and an effective cancer therapeutic agent. On 31 December 2021, the new drug application was approved by Nationa... |
PMC9570606 | core_pubmed_pmc | Nanogels as Potential Delivery Vehicles in Improving the Therapeutic Efficacy of Phytopharmaceuticals | Nanogels as Potential Delivery Vehicles in Improving the Therapeutic Efficacy of Phytopharmaceuticals Abstract Nanogel is a promising drug delivery approach to improve the pharmacokinetics and pharmacodynamic prospect of phytopharmaceuticals. In the present review, phytopharmaceuticals with astonishing therapeutic util... |
PMC12890086 | core_pubmed_pmc | Modeling viral shedding and symptom outcomes in oseltamivir-treated experimental influenza infection | Modeling viral shedding and symptom outcomes in oseltamivir-treated experimental influenza infection Abstract Abstract Influenza remains a global public health concern, and although the antiviral drug oseltamivir is widely used to treat infections, questions regarding its actual antiviral efficacy and clinical benefits... |
PMC8975796 | core_pubmed_pmc | Clinical Pharmacokinetics of the Androgen Receptor Inhibitor Darolutamide in Healthy Subjects and Patients with Hepatic or Renal Impairment | Clinical Pharmacokinetics of the Androgen Receptor Inhibitor Darolutamide in Healthy Subjects and Patients with Hepatic or Renal Impairment Abstract Background Darolutamide is a second-generation androgen receptor inhibitor approved for the treatment of nonmetastatic castration-resistant prostate cancer at a dosage of ... |
PMC11597736 | core_pubmed_pmc | Drug Interaction-Informed Approaches to Inflammatory Bowel Disease Management | Drug Interaction-Informed Approaches to Inflammatory Bowel Disease Management Abstract Inflammatory bowel disease (IBD) is a complex and chronic condition that requires the use of various pharmacological agents for its management. Despite advancements in IBD research, the multifaceted mechanisms involved continue to po... |
PMC3967229 | core_pubmed_pmc | Largazole Pharmacokinetics in Rats by LC-MS/MS | Largazole Pharmacokinetics in Rats by LC-MS/MS Abstract A highly sensitive and specific LC-MS/MS method for the quantitation of largazole thiol, the active species of the marine-derived preclinical histone deacetylase inhibitor, largazole (prodrug), was developed and validated. Largazole thiol was extracted with ethyl ... |
PMC11930985 | core_pubmed_pmc | Bemcentinib as monotherapy and in combination with low-dose cytarabine in acute myeloid leukemia patients unfit for intensive chemotherapy: a phase 1b/2a trial | Bemcentinib as monotherapy and in combination with low-dose cytarabine in acute myeloid leukemia patients unfit for intensive chemotherapy: a phase 1b/2a trial Abstract Abstract Beyond first line, the prognosis of relapsed/refractory (R/R) acute myeloid leukemia (AML) patients is poor with limited treatment options. Be... |
PMC11641021 | core_pubmed_pmc | Understanding the Preclinical Efficacy of Antibody–Drug Conjugates | Understanding the Preclinical Efficacy of Antibody–Drug Conjugates Abstract Antibody–drug conjugates (ADCs) represent a therapeutic modality that guides chemotherapies to tumoral cells by using antibodies against tumor-associated antigens (TAAs). The antibody and the chemotherapy or payload are attached by a chemical s... |
PMC12026224 | core_pubmed_pmc | Real World Posaconazole Pharmacokinetic Data in Paediatric Stem Cell Transplant Recipients | Real World Posaconazole Pharmacokinetic Data in Paediatric Stem Cell Transplant Recipients Abstract Abstract Background: Invasive fungal disease is a significant cause of morbidity and mortality in allogeneic hematopoietic stem cell transplant (alloHSCT) recipients. Posaconazole, a broad-spectrum triazole, is widely us... |
PMC6318406 | core_pubmed_pmc | Improving Anti-Cancer Potentiality and Bioavailability of Gallic Acid by Designing Polymeric Nanocomposite Formulation | Improving Anti-Cancer Potentiality and Bioavailability of Gallic Acid by Designing Polymeric Nanocomposite Formulation Abstract Objective: In this study, we investigated the in vivo antitumor activity and pharmacokinetic characteristics of encapsulated GA-NC (gallic acid nanocomposite) in normal and hepatocellular carc... |
PMC7948397 | core_pubmed_pmc | A novel soluble complement receptor 1 fragment with enhanced therapeutic potential | A novel soluble complement receptor 1 fragment with enhanced therapeutic potential Abstract Abstract Human complement receptor 1 (HuCR1) is a pivotal regulator of complement activity, acting on all three complement pathways as a membrane-bound receptor of C3b/C4b, C3/C5 convertase decay accelerator, and cofactor for fa... |
PMC10376517 | core_pubmed_pmc | Real-Life Experience of Continuously Infused Ceftolozane/Tazobactam in Patients with Bronchiectasis and Multidrug-Resistant Pseudomonas aeruginosa Infection in the Outpatient Setting | Real-Life Experience of Continuously Infused Ceftolozane/Tazobactam in Patients with Bronchiectasis and Multidrug-Resistant Pseudomonas aeruginosa Infection in the Outpatient Setting Abstract (1) Background: Ceftolozane/tazobactam (C/T) is a novel β-lactam/β-lactamase inhibitor with excellent activity against the multi... |
PMC11827725 | core_pubmed_pmc | Prediction of lacosamide concentrations to support dose optimization during pregnancy | Prediction of lacosamide concentrations to support dose optimization during pregnancy Abstract Abstract Objective We aimed to quantify and predict lacosamide exposure during pregnancy by developing a pregnancy physiologically‐based pharmacokinetic model, allowing the prediction of potential dose increases to support ma... |
PMC9244803 | core_pubmed_pmc | Development and Optimization of Bifunctional Fusion Proteins to Locally Modulate Complement Activation in Diseased Tissue | Development and Optimization of Bifunctional Fusion Proteins to Locally Modulate Complement Activation in Diseased Tissue Abstract Abstract Sustained complement activation is an underlying pathologic driver in many inflammatory and autoimmune diseases. Currently approved anti-complement therapies are directed at the sy... |
PMC7103015 | core_pubmed_pmc | G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer | G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer Abstract Abstract Purpose The combination of targeting the CDK4/6 and estrogen receptor (ER) signaling pathways with palbociclib and fulvestrant is a proven... |
PMC8419828 | core_pubmed_pmc | Computational approach towards the design of artemisinin–thymoquinone hybrids against main protease of SARS-COV-2 | Computational approach towards the design of artemisinin–thymoquinone hybrids against main protease of SARS-COV-2 Abstract Abstract Background The sanitary emergency installed in the world, generated by the pandemic of COVID-19, instigates the search for scientific strategies to mitigate the damage caused by the diseas... |
PMC11206183 | core_pubmed_pmc | Determination of ertapenem in plasma and ascitic fluid by UHPLC-MS/MS in cirrhotic patients with spontaneous bacterial peritonitis | Determination of ertapenem in plasma and ascitic fluid by UHPLC-MS/MS in cirrhotic patients with spontaneous bacterial peritonitis Abstract Abstract Objectives Spontaneous bacterial peritonitis is a frequent severe complication in cirrhotic patients with ascites. Carbapenem antibiotics are currently the treatment of ch... |
PMC7100491 | core_pubmed_pmc | Ellagic Acid, Kaempferol, and Quercetin from Acacia nilotica : Promising Combined Drug With Multiple Mechanisms of Action | Ellagic Acid, Kaempferol, and Quercetin from Acacia nilotica : Promising Combined Drug With Multiple Mechanisms of Action Abstract The pharmacological activity of Acacia nilotica ’s phytochemical constituents was confirmed with evidence-based studies, but the determination of exact targets that they bind and the mechan... |
PMC12300161 | core_pubmed_pmc | Population Pharmacokinetics and Model-Informed Precision Dosing of Clobazam Based on the Developmental and Genetic Characteristics of Children with Epilepsy | Population Pharmacokinetics and Model-Informed Precision Dosing of Clobazam Based on the Developmental and Genetic Characteristics of Children with Epilepsy Abstract Background/Objectives: This study aimed to characterize the pharmacokinetic profiles of clobazam (CLB) and its active metabolite, N-desmethylclobazam (N-C... |
PMC8616484 | core_pubmed_pmc | Intra-Tumoral Pharmacokinetics of Pazopanib in Combination with Radiotherapy in Patients with Non-Metastatic Soft-Tissue Sarcoma | Intra-Tumoral Pharmacokinetics of Pazopanib in Combination with Radiotherapy in Patients with Non-Metastatic Soft-Tissue Sarcoma Abstract Abstract Simple Summary Pazopanib plasma levels have been associated with treatment efficacy. Since pazopanib targets receptors present on cells in the vicinity of the tumor and on t... |
PMC3664353 | core_pubmed_pmc | Mathematical modelling to restore circulating IGF-1 concentrations in children with Crohn's disease-induced growth failure: a pharmacokinetic study | Mathematical modelling to restore circulating IGF-1 concentrations in children with Crohn's disease-induced growth failure: a pharmacokinetic study Abstract Objectives Children with Crohn's disease grow poorly, and inflammation depresses the response of insulin-like growth factor-1 (IGF-1) to growth hormone. Correcting... |
PMC8491704 | core_pubmed_pmc | Pharmacokinetic study of Tangwang Mingmu granule for the management of diabetic retinopathy based on network pharmacology | Pharmacokinetic study of Tangwang Mingmu granule for the management of diabetic retinopathy based on network pharmacology Abstract Abstract Context Tangwang Mingmu granule (TWMM), a traditional Chinese medicine, has been widely used in the treatment of diabetic retinopathy (DR), the most common microvascular complicati... |
PMC10175981 | core_pubmed_pmc | Age associations with tacrolimus and mycophenolic acid pharmacokinetics in stable Black and White kidney transplant recipients: Implications for health inequities | Age associations with tacrolimus and mycophenolic acid pharmacokinetics in stable Black and White kidney transplant recipients: Implications for health inequities Abstract Abstract Tacrolimus (TAC) and mycophenolic acid (MPA) provide maintenance immunosuppression and is dosed empirically in elderly kidney transplant re... |
PMC4383224 | core_pubmed_pmc | Pharmacoinformatics approach for investigation of alternative potential hepatitis C virus nonstructural protein 5B inhibitors | Pharmacoinformatics approach for investigation of alternative potential hepatitis C virus nonstructural protein 5B inhibitors Abstract Abstract Hepatitis C virus (HCV) is one of the major viruses affecting the world today. It is a highly variable virus, having a rapid reproduction and evolution rate. The variability of... |
PMC12334480 | core_pubmed_pmc | Impact of Batoclimab Treatment on LDL-C with and Without Coadministration of Atorvastatin: Results from a Phase I Randomized Study in Healthy Participants | Impact of Batoclimab Treatment on LDL-C with and Without Coadministration of Atorvastatin: Results from a Phase I Randomized Study in Healthy Participants Abstract Introduction Batoclimab is an anti-neonatal fragment crystallizable receptor monoclonal antibody in clinical development for the treatment of autoimmune dis... |
PMC9762804 | core_pubmed_pmc | Receptor occupancy assessment and interpretation in terms of quantitative systems pharmacology: nivolumab case study | Receptor occupancy assessment and interpretation in terms of quantitative systems pharmacology: nivolumab case study Abstract ABSTRACT Receptor occupancy assays applied in clinical studies provide insights into pharmacokinetic-pharmacodynamic relationships for therapeutic antibodies. When measured by different assays, ... |
PMC8914346 | core_pubmed_pmc | Vincristine dosing, drug exposure and therapeutic drug monitoring in neonate and infant cancer patients | Vincristine dosing, drug exposure and therapeutic drug monitoring in neonate and infant cancer patients Abstract Abstract Background The anticancer drug vincristine is associated with potentially dose-limiting side-effects, including neurotoxicity and myelosuppression. However, there currently exists a lack of publishe... |
PMC5625156 | core_pubmed_pmc | Coffee inhibition of CYP 3A4 in vitro was not translated to a grapefruit‐like pharmacokinetic interaction clinically | Coffee inhibition of CYP 3A4 in vitro was not translated to a grapefruit‐like pharmacokinetic interaction clinically Abstract Abstract Grapefruit can augment oral medication bioavailability through irreversible (mechanism‐based) inhibition of intestinal CYP 3A4. Supplementary data from our recent coffee–drug interactio... |
PMC6099482 | core_pubmed_pmc | Pharmacokinetics of Mycophenolate Mofetil and Development of Limited Sampling Strategy in Early Kidney Transplant Recipients | Pharmacokinetics of Mycophenolate Mofetil and Development of Limited Sampling Strategy in Early Kidney Transplant Recipients Abstract Abstract The mycophenolate mofetil (MMF) dose management for optimization of post-transplant treatment especially the early postoperative phase has been well recognized. MMF is a pro-dru... |
PMC6567274 | core_pubmed_pmc | Vive la Difference ! The Effects of Natural and Conventional Wines on Blood Alcohol Concentrations: A Randomized, Triple-Blind, Controlled Study | Vive la Difference ! The Effects of Natural and Conventional Wines on Blood Alcohol Concentrations: A Randomized, Triple-Blind, Controlled Study Abstract Abstract Different alcoholic beverages can have different effects on blood alcohol concentration (BAC) and neurotoxicity, even when equalized for alcohol content by v... |
PMC4901288 | core_pubmed_pmc | Significant pharmacokinetic differences of berberine are attributable to variations in gut microbiota between Africans and Chinese | Significant pharmacokinetic differences of berberine are attributable to variations in gut microbiota between Africans and Chinese Abstract We investigated the influence of gut microbiotal metabolism on the pharmacokinetics of berberine in healthy male Africans and Chinese. The C max and AUC in the Africans were 2.67-f... |
PMC3377357 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Modeling of Metabolic Pathways of Bromochloromethane in Rats | Physiologically Based Pharmacokinetic (PBPK) Modeling of Metabolic Pathways of Bromochloromethane in Rats Abstract Abstract Bromochloromethane (BCM) is a volatile compound and a by-product of disinfection of water by chlorination. Physiologically based pharmacokinetic (PBPK) models are used in risk assessment applicati... |
PMC12569255 | core_pubmed_pmc | [ 11 C]Fentanyl: radiosynthesis and preclinical pet imaging for its pharmacokinetics | [ 11 C]Fentanyl: radiosynthesis and preclinical pet imaging for its pharmacokinetics Abstract Abstract Background Fentanyl is a potent synthetic opioid widely used for pain management and anesthesia, but the high prevalence of its misuse and its key contribution to overdose fatalities in the United States have made it ... |
PMC6821220 | core_pubmed_pmc | Safety and Pharmacokinetics of Glecaprevir/Pibrentasvir in Adults With Chronic Genotype 1–6 Hepatitis C Virus Infections and Compensated Liver Disease | Safety and Pharmacokinetics of Glecaprevir/Pibrentasvir in Adults With Chronic Genotype 1–6 Hepatitis C Virus Infections and Compensated Liver Disease Abstract Abstract Background Untreated, chronic hepatitis C virus (HCV) infection may lead to progressive liver damage, which can be mitigated by successful treatment. T... |
PMC10862980 | core_pubmed_pmc | A unifying model to explain high nirmatrelvir therapeutic efficacy against SARS-CoV-2, despite low post-exposure prophylaxis efficacy and frequent viral rebound | A unifying model to explain high nirmatrelvir therapeutic efficacy against SARS-CoV-2, despite low post-exposure prophylaxis efficacy and frequent viral rebound Abstract In a pivotal trial (EPIC-HR), a 5-day course of oral ritonavir-boosted nirmatrelvir, given early during symptomatic SARS-CoV-2 infection (within three... |
PMC10960464 | core_pubmed_pmc | In vivo antimalarial effect of 1-hydroxy-5,6,7-trimethoxyxanthone isolated from Mammea siamensis T. Anders. flowers: pharmacokinetic and acute toxicity studies | In vivo antimalarial effect of 1-hydroxy-5,6,7-trimethoxyxanthone isolated from Mammea siamensis T. Anders. flowers: pharmacokinetic and acute toxicity studies Abstract Background The potent antiplasmodial activity of 1-hydroxy-5,6,7-trimethoxyxanthone (HTX), isolated from Mammea siamensis T. Anders. flowers, has previ... |
PMC10704090 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of ciprofol emulsion in Chinese subjects with normal or impaired renal function | Pharmacokinetics, pharmacodynamics, and safety of ciprofol emulsion in Chinese subjects with normal or impaired renal function Abstract Background: Ciprofol, a novel sedative–hypnotic drug, has been approved for its use in inducing and maintaining general anesthesia, as well as for providing sedation. Methods: In this ... |
PMC8079061 | core_pubmed_pmc | Effects of dacomitinib on the pharmacokinetics of poziotinib in vivo and in vitro | Effects of dacomitinib on the pharmacokinetics of poziotinib in vivo and in vitro Abstract Abstract Context Dacomitinib and poziotinib, irreversible ErbB family blockers, are often used for treatment of non-small cell lung cancer (NSCLC) in the clinic. Objective This study investigates the effect of dacomitinib on the ... |
PMC3124792 | core_pubmed_pmc | An ANN model for treatment prediction in HBV patients | An ANN model for treatment prediction in HBV patients Abstract Abstract Two types of antiviral treatments, namely, interferon and nucleoside/nucleotide analogues are available for hepatitis infections. The selection of drug and dose determined using known pharmacokinetics and pharmacodynamics data is important. The lac... |
PMC5813242 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic correlations in the development of ginger extract as an anticancer agent | Pharmacokinetic-pharmacodynamic correlations in the development of ginger extract as an anticancer agent Abstract Abstract Anticancer efficacy of ginger phenolics (GPs) has been demonstrated in various in vitro assays and xenograft mouse models. However, only sub-therapeutic plasma concentrations of GPs were detected i... |
PMC9099026 | core_pubmed_pmc | Multi-Omics Integration in Mice With Parkinson’s Disease and the Intervention Effect of Cyanidin-3- O -Glucoside | Multi-Omics Integration in Mice With Parkinson’s Disease and the Intervention Effect of Cyanidin-3- O -Glucoside Abstract Abstract Background Parkinson’s disease (PD) is a multifactorial degenerative disease of the central nervous system, which affects mostly older adults. To date, research has focused on the progressi... |
PMC10609730 | core_pubmed_pmc | Pharmacokinetics and Anti-Tumor Efficacy of PEGylated Liposomes Co-Loaded with Cisplatin and Mifepristone | Pharmacokinetics and Anti-Tumor Efficacy of PEGylated Liposomes Co-Loaded with Cisplatin and Mifepristone Abstract Abstract Although cisplatin is an effective chemotherapy drug used against many types of cancer, it has poor bioavailability, produces severe adverse effects, and frequently leads to tumor resistance. Cons... |
PMC12368874 | core_pubmed_pmc | The Impact of Conjugation Mode and Site on Tubulysin Antibody‐Drug‐Conjugate Efficacy and Stability | The Impact of Conjugation Mode and Site on Tubulysin Antibody‐Drug‐Conjugate Efficacy and Stability Abstract Antibody‐drug conjugates (ADCs) represent a prominent class of biotherapeutics engineered to selectively deliver cytotoxic payloads to tumors, thereby facilitating targeted cell killing. While first‐generation A... |
PMC3910846 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacogenetic Analysis of Nevirapine in Hypersensitive and Tolerant HIV-Infected Patients from Malawi | Population Pharmacokinetic and Pharmacogenetic Analysis of Nevirapine in Hypersensitive and Tolerant HIV-Infected Patients from Malawi Abstract Abstract We modeled nevirapine (NVP) pharmacokinetics in HIV-infected Malawian patients to assess the relationship between drug exposure and patient characteristics, genetic po... |
PMC8064303 | core_pubmed_pmc | Population Pharmacokinetics of Piperacillin in Non-Critically Ill Patients with Bacteremia Caused by Enterobacteriaceae | Population Pharmacokinetics of Piperacillin in Non-Critically Ill Patients with Bacteremia Caused by Enterobacteriaceae Abstract This study analyzes the pharmacokinetic variability of piperacillin in non-critically ill patients with Enterobacteriaceae bloodstream infections (EBSI) and explores predicted clinical outcom... |
PMC6781287 | core_pubmed_pmc | Impact of GSTA1 Polymorphisms on Busulfan Oral Clearance in Adult Patients Undergoing Hematopoietic Stem Cell Transplantation | Impact of GSTA1 Polymorphisms on Busulfan Oral Clearance in Adult Patients Undergoing Hematopoietic Stem Cell Transplantation Abstract Background: Busulfan pharmacokinetics exhibit large inter-subject variability. Our objective was to evaluate the influence of glutathione S-transferase A1 ( GSTA1 ) gene variants on bus... |
PMC9775652 | core_pubmed_pmc | Concomitant Administration of Red Ginseng Extract with Lactic Acid Bacteria Increases the Plasma Concentration of Deglycosylated Ginsenosides in Healthy Human Subjects | Concomitant Administration of Red Ginseng Extract with Lactic Acid Bacteria Increases the Plasma Concentration of Deglycosylated Ginsenosides in Healthy Human Subjects Abstract With the increased frequency of red ginseng extract (RGE) and lactic acid bacteria (LAB) co-administration, we aimed to investigate the interac... |
PMC12199096 | core_pubmed_pmc | Paracetamol and its metabolites in children and adults with spinal muscular atrophy – a population pharmacokinetic model | Paracetamol and its metabolites in children and adults with spinal muscular atrophy – a population pharmacokinetic model Abstract Abstract Aims The aim of the study was to investigate whether differences in paracetamol pharmacokinetics (PK) between spinal muscular atrophy (SMA) patients and healthy controls (HC) could ... |
PMC8293327 | core_pubmed_pmc | Characterizing Errors in Pharmacokinetic Parameters from Analyzing Quantitative Abbreviated DCE-MRI Data in Breast Cancer | Characterizing Errors in Pharmacokinetic Parameters from Analyzing Quantitative Abbreviated DCE-MRI Data in Breast Cancer Abstract Abstract This study characterizes the error that results when performing quantitative analysis of abbreviated dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) data of the brea... |
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