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PMC12471285 | core_pubmed_pmc | Redefining Breast Cancer Care by Harnessing Computational Drug Repositioning | Redefining Breast Cancer Care by Harnessing Computational Drug Repositioning Abstract Abstract Breast cancer faces significant therapeutic challenges, particularly for triple-negative breast cancer (TNBC), due to limited targeted therapies and drug resistance. Drug repositioning leverages existing safety and pharmacoki... |
PMC5543190 | core_pubmed_pmc | IRIS study: a phase II study of the steroid sulfatase inhibitor Irosustat when added to an aromatase inhibitor in ER-positive breast cancer patients | IRIS study: a phase II study of the steroid sulfatase inhibitor Irosustat when added to an aromatase inhibitor in ER-positive breast cancer patients Abstract Abstract Purpose Irosustat is a first-generation, orally active, irreversible steroid sulfatase inhibitor. We performed a multicentre, open label phase II trial o... |
PMC12680786 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Long‐Acting FGF21 Analog Zalfermin | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Long‐Acting FGF21 Analog Zalfermin Abstract ABSTRACT This first‐in‐human study investigated the safety, pharmacokinetics, and pharmacodynamics of the long‐acting fibroblast growth factor 21 (FGF21) analog zalfermin. Healthy male participants ( n ... |
PMC11912797 | core_pubmed_pmc | Pharmacokinetic variability and significance of therapeutic drug monitoring for broad-spectrum antimicrobials in critically ill patients | Pharmacokinetic variability and significance of therapeutic drug monitoring for broad-spectrum antimicrobials in critically ill patients Abstract Critically ill patients are susceptible to serious infections due to their compromised conditions and extensive use of medical devices, often requiring empiric broad-spectrum... |
PMC4879477 | core_pubmed_pmc | Prospective Design of Anti‐Transferrin Receptor Bispecific Antibodies for Optimal Delivery into the Human Brain | Prospective Design of Anti‐Transferrin Receptor Bispecific Antibodies for Optimal Delivery into the Human Brain Abstract Abstract Anti‐transferrin receptor (TfR)‐based bispecific antibodies have shown promise for boosting antibody uptake in the brain. Nevertheless, there are limited data on the molecular properties, in... |
PMC11499514 | core_pubmed_pmc | A Pooled Analysis of Eight Clinical Studies Suggests a Link Between Influenza-Like Symptoms and Pharmacodynamics of the Toll-Like Receptor-7 Agonist Vesatolimod | A Pooled Analysis of Eight Clinical Studies Suggests a Link Between Influenza-Like Symptoms and Pharmacodynamics of the Toll-Like Receptor-7 Agonist Vesatolimod Abstract Abstract Introduction Vesatolimod is a Toll-like receptor-7 (TLR7) agonist in clinical development as part of a combination regimen for human immunode... |
PMC5346879 | core_pubmed_pmc | Scaling clearance in paediatric pharmacokinetics: All models are wrong, which are useful? | Scaling clearance in paediatric pharmacokinetics: All models are wrong, which are useful? Abstract Abstract Linked Articles This article is commented on in the editorial by Holford NHG and Anderson BJ. Why standards are useful for predicting doses. Br J Clin Pharmacol 2017; 83: 685–7. doi: 10.1111/bcp.13230 Aim When di... |
PMC6430158 | core_pubmed_pmc | Assessing CYP2C19 Ontogeny in Neonates and Infants Using Physiologically Based Pharmacokinetic Models: Impact of Enzyme Maturation Versus Inhibition | Assessing CYP2C19 Ontogeny in Neonates and Infants Using Physiologically Based Pharmacokinetic Models: Impact of Enzyme Maturation Versus Inhibition Abstract Abstract The objective of this study was to develop pediatric physiologically based pharmacokinetic (PBPK) models for pantoprazole and esomeprazole. Pediatric PBP... |
PMC11976807 | core_pubmed_pmc | Dynamic Assessment of Local Abdominal Tissue Concentrations of Cisplatin During a HIPEC Procedure: Insights from a Porcine Model | Dynamic Assessment of Local Abdominal Tissue Concentrations of Cisplatin During a HIPEC Procedure: Insights from a Porcine Model Abstract Abstract Background This study aimed to establish a feasible large porcine model for dynamic assessment of cisplatin concentrations in carcinomatosis-relevant abdominal tissues using... |
PMC11992659 | core_pubmed_pmc | The pharmacokinetics of brensocatib in participants with renal impairment following a single oral administration | The pharmacokinetics of brensocatib in participants with renal impairment following a single oral administration Abstract Aim Brensocatib is an oral, selective, competitive and reversible dipeptidyl peptidase 1 inhibitor in development for the treatment of bronchiectasis. This study evaluated the pharmacokinetics (PKs)... |
PMC12460387 | core_pubmed_pmc | Model-informed identification of optimised dosing strategies for meropenem in critically ill patients receiving SLEDD: an observational study | Model-informed identification of optimised dosing strategies for meropenem in critically ill patients receiving SLEDD: an observational study Abstract Purpose An increasing number of critically ill patients receive slow extended daily dialysis (SLEDD) due to their pathophysiology while suffering from sepsis, necessitat... |
PMC11199538 | core_pubmed_pmc | A phase I, randomized study to evaluate the safety, tolerability, and pharmacokinetics of mefunidone in healthy subjects | A phase I, randomized study to evaluate the safety, tolerability, and pharmacokinetics of mefunidone in healthy subjects Abstract Background Mefunidone is a novel synthetic compound and is better when compared to pirfenidone for the anti-fibrotic treatment of renal fibrosis in end-stage renal disease. We conducted this... |
PMC9428924 | core_pubmed_pmc | Stealth Liposomal Chemotherapeutic Agent for Triple Negative Breast Cancer with Improved Pharmacokinetics | Stealth Liposomal Chemotherapeutic Agent for Triple Negative Breast Cancer with Improved Pharmacokinetics Abstract Triple-negative breast cancer is one of the most lethal cancers. Chemotherapeutics for targeting CDK4 and CDK6 like Palbociclib (PAB) in triple-negative breast cancer was widely explored. However, poor bio... |
PMC3448612 | core_pubmed_pmc | In Silico Investigations of the Anti-Catabolic Effects of Pamidronate and Denosumab on Multiple Myeloma-Induced Bone Disease | In Silico Investigations of the Anti-Catabolic Effects of Pamidronate and Denosumab on Multiple Myeloma-Induced Bone Disease Abstract It is unclear whether the new anti-catabolic agent denosumab represents a viable alternative to the widely used anti-catabolic agent pamidronate in the treatment of Multiple Myeloma (MM)... |
PMC8695459 | core_pubmed_pmc | Cytotoxicity of targeted PLGA nanoparticles: a systematic review † | Cytotoxicity of targeted PLGA nanoparticles: a systematic review † Abstract Recent advances in nanotechnology have contributed tremendously to the development and revolutionizing of drug delivery systems in the field of nanomedicine. In particular, targeting nanoparticles based on biodegradable poly(lactic- co -glycoli... |
PMC4588373 | core_pubmed_pmc | Efficacy of two-time prophylactic intravenous administration of tazobactam/piperacillin for transrectal ultrasound-guided needle biopsy of the prostate | Efficacy of two-time prophylactic intravenous administration of tazobactam/piperacillin for transrectal ultrasound-guided needle biopsy of the prostate Abstract Abstract Background Prevalence of fluoroquinolone (FQ)-resistant Escherichia coli has been recently increasing worldwide. We analyzed the incidence and charact... |
PMC10664005 | core_pubmed_pmc | Design, synthesis and in silico evaluation of newer 1,4-dihydropyridine based amlodipine bio-isosteres as promising antihypertensive agents † | Design, synthesis and in silico evaluation of newer 1,4-dihydropyridine based amlodipine bio-isosteres as promising antihypertensive agents † Abstract Hypertension remains a major global health concern, prompting ongoing research into innovative therapeutic approaches. This research encompasses the strategic design, sy... |
PMC11064475 | core_pubmed_pmc | Accelerating therapeutics development during a pandemic: population pharmacokinetics of the long-acting antibody combination AZD7442 (tixagevimab/cilgavimab) in the prophylaxis and treatment of COVID-19 | Accelerating therapeutics development during a pandemic: population pharmacokinetics of the long-acting antibody combination AZD7442 (tixagevimab/cilgavimab) in the prophylaxis and treatment of COVID-19 Abstract ABSTRACT AZD7442 is a combination of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-neutralizi... |
PMC7804201 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics integration of danofloxacin against Eschrichia coli in piglet ileum ultrafiltration probe model | Pharmacokinetics and pharmacodynamics integration of danofloxacin against Eschrichia coli in piglet ileum ultrafiltration probe model Abstract Improper use of antibiotics results in poor treatment and severe bacterial resistance. In this study, ultrafiltration probes were successfully placed in the ileum of piglets wit... |
PMC7891373 | core_pubmed_pmc | Pharmacokinetic Comparison of Capsule and Tablet Formulations of Opicapone in Healthy Japanese Subjects: Phase 1 Study | Pharmacokinetic Comparison of Capsule and Tablet Formulations of Opicapone in Healthy Japanese Subjects: Phase 1 Study Abstract Abstract Opicapone, a peripheral, long‐acting catechol‐O‐methyltransferase inhibitor has been shown to improve wearing‐off phenomenon in randomized, double‐blind studies. This study compared t... |
PMC8113290 | core_pubmed_pmc | [ 11 C]MODAG-001—towards a PET tracer targeting α-synuclein aggregates | [ 11 C]MODAG-001—towards a PET tracer targeting α-synuclein aggregates Abstract Purpose Deposition of misfolded alpha-synuclein (αSYN) aggregates in the human brain is one of the major hallmarks of synucleinopathies. However, a target-specific tracer to detect pathological aggregates of αSYN remains lacking. Here, we r... |
PMC10589167 | core_pubmed_pmc | Optimization of Q.Clear reconstruction for dynamic 18 F PET imaging | Optimization of Q.Clear reconstruction for dynamic 18 F PET imaging Abstract Abstract Background Q.Clear, a Bayesian penalized likelihood reconstruction algorithm, has shown high potential in improving quantitation accuracy in PET systems. The Q.Clear algorithm controls noise during the iterative reconstruction through... |
PMC8705362 | core_pubmed_pmc | Cytochrome P450 and P-gp Mediated Herb-Drug Interactions and Molecular Docking Studies of Garcinol | Cytochrome P450 and P-gp Mediated Herb-Drug Interactions and Molecular Docking Studies of Garcinol Abstract Abstract Garcinol is an active constituent of Garcinia indica and Garcinia cambogia . Recent studies have proven that garcinol has anti-inflammatory, anti-cancer, and anti-oxidant activities. The objective of thi... |
PMC5602130 | core_pubmed_pmc | Food and Sex-Related Impacts on the Pharmacokinetics of a Single-Dose of Ginsenoside Compound K in Healthy Subjects | Food and Sex-Related Impacts on the Pharmacokinetics of a Single-Dose of Ginsenoside Compound K in Healthy Subjects Abstract Background and Objectives: Ginsenoside compound K (CK) is a candidate drug for rheumatoid arthritis therapy. This clinical trial was designed to evaluate the effects of food and sex on the pharma... |
PMC4718910 | core_pubmed_pmc | A phase II study of afatinib, an irreversible ErbB family blocker, added to letrozole in patients with estrogen receptor-positive hormone-refractory metastatic breast cancer progressing on letrozole | A phase II study of afatinib, an irreversible ErbB family blocker, added to letrozole in patients with estrogen receptor-positive hormone-refractory metastatic breast cancer progressing on letrozole Abstract Abstract Phase II, open-label study assessing the efficacy and safety of the ErbB family blocker afatinib combin... |
PMC4909762 | core_pubmed_pmc | Pharmacotherapy of Pain in the Older Population: The Place of Opioids | Pharmacotherapy of Pain in the Older Population: The Place of Opioids Abstract Abstract Pain is a common symptom in older people. It is possible that pain is underreported in older persons due to an incorrect belief that it is an inevitable part of aging. Opioid analgesics are potent medications, with confirmed efficac... |
PMC3751891 | core_pubmed_pmc | Systematic Pharmacogenomics Analysis of a Malay Whole Genome: Proof of Concept for Personalized Medicine | Systematic Pharmacogenomics Analysis of a Malay Whole Genome: Proof of Concept for Personalized Medicine Abstract Abstract Background With a higher throughput and lower cost in sequencing, second generation sequencing technology has immense potential for translation into clinical practice and in the realization of phar... |
PMC5023994 | core_pubmed_pmc | Does age affect gastric emptying time? A model‐based meta‐analysis of data from premature neonates through to adults | Does age affect gastric emptying time? A model‐based meta‐analysis of data from premature neonates through to adults Abstract Abstract Purpose . Gastric emptying (GE) is often reported to be slower and more irregular in premature neonates than in older children and adults. The aim of this study was to investigate the i... |
PMC7945371 | core_pubmed_pmc | Low-dose amikacin in the treatment of Multidrug-resistant Tuberculosis (MDR-TB) | Low-dose amikacin in the treatment of Multidrug-resistant Tuberculosis (MDR-TB) Abstract Abstract Background The World Health Organization recommends intravenous amikacin for the treatment of MDR-TB at a dose of 15 mg/kg. However, higher doses are associated with significant toxicity. Methods Patients with MDR-TB treat... |
PMC11051385 | core_pubmed_pmc | The Impact of Augmented Renal Clearance on Vancomycin Pharmacokinetics and Pharmacodynamics in Critically Ill Patients | The Impact of Augmented Renal Clearance on Vancomycin Pharmacokinetics and Pharmacodynamics in Critically Ill Patients Abstract Abstract Augmented renal clearance (ARC), defined as a creatinine clearance (CrCl) > 130 mL/min/1.73 m 2 , is observed in 30–65% of critically ill patients. When following standard dosage guid... |
PMC11015084 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic modeling of cortical dopamine concentrations after quetiapine lipid core nanocapsules administration to schizophrenia phenotyped rats | Pharmacokinetic/pharmacodynamic modeling of cortical dopamine concentrations after quetiapine lipid core nanocapsules administration to schizophrenia phenotyped rats Abstract Abstract Schizophrenia (SCZ) response to pharmacological treatment is highly variable. Quetiapine (QTP) administered as QTP lipid core nanocapsul... |
PMC11979702 | core_pubmed_pmc | Computational analysis of Ayurvedic metabolites for potential treatment of drug-resistant Candida auris | Computational analysis of Ayurvedic metabolites for potential treatment of drug-resistant Candida auris Abstract Abstract This study explored the effectiveness of secondary metabolites of referred traditional Ayurvedic plants in treating fungal infections, particularly targeting Candida auris . Recognized as a global h... |
PMC4652348 | core_pubmed_pmc | Pharmacokinetics and safety of cyclophosphamide and docetaxel in a hemodialysis patient with early stage breast cancer: a case report | Pharmacokinetics and safety of cyclophosphamide and docetaxel in a hemodialysis patient with early stage breast cancer: a case report Abstract Abstract Background Standardized chemotherapy used in cancer patients with severe kidney insufficiency is ineffective. Although there are some pharmacokinetic studies on cycloph... |
PMC9515697 | core_pubmed_pmc | Ivermectin induces cell cycle arrest and caspase-dependent apoptosis in human urothelial carcinoma cells | Ivermectin induces cell cycle arrest and caspase-dependent apoptosis in human urothelial carcinoma cells Abstract Abstract Bladder carcinoma is one of the most common malignancies worldwide, and >90% of all bladder cancers are classified as urothelial carcinomas (UC). Surgery, radiotherapy, chemotherapy, targeted thera... |
PMC5686265 | core_pubmed_pmc | Phase 1 study of darolutamide (ODM-201): a new-generation androgen receptor antagonist, in Japanese patients with metastatic castration-resistant prostate cancer | Phase 1 study of darolutamide (ODM-201): a new-generation androgen receptor antagonist, in Japanese patients with metastatic castration-resistant prostate cancer Abstract Abstract Purpose This trial assessed the safety, pharmacokinetics, and efficacy of darolutamide (ODM-201), a new-generation nonsteroidal androgen rec... |
PMC9298689 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of Abelacimab (MAA868), a novel dual inhibitor of Factor XI and Factor XIa | Pharmacokinetics and pharmacodynamics of Abelacimab (MAA868), a novel dual inhibitor of Factor XI and Factor XIa Abstract Abstract Background Factor XI (FXI) inhibition offers the promise of hemostasis‐sparing anticoagulation for the prevention and treatment of thromboembolic events. Abelacimab (MAA868) is a novel full... |
PMC12410058 | core_pubmed_pmc | Global assessment of partial artemisinin resistance: multicenter trial across Kenya, Peru, and Thailand in patients with uncomplicated Plasmodium falciparum malaria | Global assessment of partial artemisinin resistance: multicenter trial across Kenya, Peru, and Thailand in patients with uncomplicated Plasmodium falciparum malaria Abstract Objectives: Artemisinin-resistant Plasmodium falciparum challenges the effectiveness of all artemisinin-based combination therapies. Methods: We c... |
PMC5684285 | core_pubmed_pmc | Influence of genetic co-factors on the population pharmacokinetic model for clopidogrel and its active thiol metabolite | Influence of genetic co-factors on the population pharmacokinetic model for clopidogrel and its active thiol metabolite Abstract Purpose A high interindividual variability is observed in the pharmacokinetics of clopidogrel, a widely used antiplatelet drug. In the present study, a joint parent-metabolite population phar... |
PMC6951457 | core_pubmed_pmc | Target‐Mediated Drug Disposition Pharmacokinetic/Pharmacodynamic Model‐Informed Dose Selection for the First‐in‐Human Study of AVB‐S6‐500 | Target‐Mediated Drug Disposition Pharmacokinetic/Pharmacodynamic Model‐Informed Dose Selection for the First‐in‐Human Study of AVB‐S6‐500 Abstract Abstract AVB‐S6‐500 neutralized growth arrest‐specific 6 (GAS6) protein and effectively inhibited AXL signaling in preclinical cancer models. A target‐mediated drug disposit... |
PMC6878998 | core_pubmed_pmc | Co-Delivery of Prednisolone and Curcumin in Human Serum Albumin Nanoparticles for Effective Treatment of Rheumatoid Arthritis | Co-Delivery of Prednisolone and Curcumin in Human Serum Albumin Nanoparticles for Effective Treatment of Rheumatoid Arthritis Abstract Background Prednisolone (PD) is extremely effective for treating rheumatoid arthritis (RA). However, it distributes nonspecifically throughout the body and its use is associated with se... |
PMC8625191 | core_pubmed_pmc | Population Pharmacokinetics of Meropenem in Critically Ill Korean Patients and Effects of Extracorporeal Membrane Oxygenation | Population Pharmacokinetics of Meropenem in Critically Ill Korean Patients and Effects of Extracorporeal Membrane Oxygenation Abstract Limited studies have investigated population pharmacokinetic (PK) models and optimal dosage regimens of meropenem for critically ill adult patients using the probability of target attai... |
PMC11417994 | core_pubmed_pmc | Cyclohexanediamine Triazole (CHDT) Functionalization Enables Labeling of Target Molecules with Al 18 F/ 68 Ga/ 111 In | Cyclohexanediamine Triazole (CHDT) Functionalization Enables Labeling of Target Molecules with Al 18 F/ 68 Ga/ 111 In Abstract The Al 18 F-labeling approach offers a one-step access to radiofluorinated biomolecules by mimicking the labeling process for radiometals. Although these labeling conditions are considered to b... |
PMC6462747 | core_pubmed_pmc | BAY 1213790, a fully human IgG1 antibody targeting coagulation factor XI a: First evaluation of safety, pharmacodynamics, and pharmacokinetics | BAY 1213790, a fully human IgG1 antibody targeting coagulation factor XI a: First evaluation of safety, pharmacodynamics, and pharmacokinetics Abstract Abstract Background Coagulation factor XI ( FXI ) contributes to the development of thrombosis but appears to play only a minor role in hemostasis and is therefore an a... |
PMC12178835 | core_pubmed_pmc | A Dose Too Far: Valacyclovir’s Surprising Side Effect | A Dose Too Far: Valacyclovir’s Surprising Side Effect Abstract Valacyclovir, a prodrug of acyclovir, is a widely prescribed antiviral medication known for its efficacy in treating herpes infections. Although generally considered safe, rare cases of psychiatric adverse effects, including psychosis, have been reported. T... |
PMC5834589 | core_pubmed_pmc | Pharmacokinetics of Oral and Intravenous Paracetamol (Acetaminophen) When Co-Administered with Intravenous Morphine in Healthy Adult Subjects | Pharmacokinetics of Oral and Intravenous Paracetamol (Acetaminophen) When Co-Administered with Intravenous Morphine in Healthy Adult Subjects Abstract Background and Objective Several features favor paracetamol (acetaminophen) administration by the intravenous rather than the oral route in the postoperative setting. Th... |
PMC8067398 | core_pubmed_pmc | An Efficient Method for the Differentiation of Human iPSC-Derived Endoderm toward Enterocytes and Hepatocytes | An Efficient Method for the Differentiation of Human iPSC-Derived Endoderm toward Enterocytes and Hepatocytes Abstract The endoderm, differentiated from human induced pluripotent stem cells (iPSCs), can differentiate into the small intestine and liver, which are vital for drug absorption and metabolism. The development... |
PMC12680638 | core_pubmed_pmc | Discovering bioactive pharmaceuticals from natural products for type 2 diabetes mellitus using network pharmacology, molecular docking, and molecular dynamics | Discovering bioactive pharmaceuticals from natural products for type 2 diabetes mellitus using network pharmacology, molecular docking, and molecular dynamics Abstract Abstract Type 2 diabetes mellitus (T2DM) is a global health challenge that requires new therapeutic approaches. Natural compounds from botanical sources... |
PMC12375329 | core_pubmed_pmc | Design, Synthesis and Anti-Inflammation Evaluation of N -Acyl Tryptophan Derivatives as Promising P2Y 14 R Antagonists Against Lipopolysaccharide-Induced Acute Lung Injury | Design, Synthesis and Anti-Inflammation Evaluation of N -Acyl Tryptophan Derivatives as Promising P2Y 14 R Antagonists Against Lipopolysaccharide-Induced Acute Lung Injury Abstract Purpose The P2Y 14 receptor (P2Y 14 R) is closely associated with several inflammatory diseases in humans. Although several P2Y 14 R antago... |
PMC6169240 | core_pubmed_pmc | Simultaneous Determination of Columbianadin and Its Metabolite Columbianetin in Rat Plasma by LC-MS/MS: Application to Pharmacokinetics of Columbianadin after Oral Administration | Simultaneous Determination of Columbianadin and Its Metabolite Columbianetin in Rat Plasma by LC-MS/MS: Application to Pharmacokinetics of Columbianadin after Oral Administration Abstract Abstract Columbianadin and its metabolite columbianetin exhibited the anti-inflammatory, analgesic, calcium channel blocking and ant... |
PMC10769797 | core_pubmed_pmc | A Phase I Dose-Escalation Study of LY3405105, a Covalent Inhibitor of Cyclin-Dependent Kinase 7, Administered to Patients With Advanced Solid Tumors | A Phase I Dose-Escalation Study of LY3405105, a Covalent Inhibitor of Cyclin-Dependent Kinase 7, Administered to Patients With Advanced Solid Tumors Abstract Abstract Background This study aimed to evaluate the safety, pharmacokinetics (PKs), and preliminary activity of LY3405105, a covalent inhibitor of cyclin-depende... |
PMC3249746 | core_pubmed_pmc | Pharmacokinetic Evaluation of Paclitaxel in South Indian Cancer Patients: A Prospective Study | Pharmacokinetic Evaluation of Paclitaxel in South Indian Cancer Patients: A Prospective Study Abstract Paclitaxel is a promising drug in the treatment of different solid tumors. It exhibits nonlinear pharmacokinetics, particularly when administered as a constant rate infusion for shorter duration (e.g., 3 h). Because o... |
PMC10332326 | core_pubmed_pmc | Phase Ib/II Study of a Liposomal Formulation of Eribulin (E7389-LF) plus Nivolumab in Patients with Advanced Solid Tumors: Results from Phase Ib | Phase Ib/II Study of a Liposomal Formulation of Eribulin (E7389-LF) plus Nivolumab in Patients with Advanced Solid Tumors: Results from Phase Ib Abstract Purpose: To determine a recommended dose of liposomal eribulin (E7389-LF) in combination with nivolumab in patients with advanced solid tumors, and to evaluate the sa... |
PMC10725889 | core_pubmed_pmc | Integrated network pharmacology and metabolomics reveal the mechanisms of Jasminum elongatum in anti-ulcerative colitis | Integrated network pharmacology and metabolomics reveal the mechanisms of Jasminum elongatum in anti-ulcerative colitis Abstract Jasminum elongatum (JE), an ethnic Chinese medicine, is widely used in the Lingnan region of China, because of its analgesic and antidiarrheal action, as well as its anti-inflammatory effects... |
PMC12300028 | core_pubmed_pmc | Diastereoselective Synthesis and Biological Evaluation of Spiro[chromane-2,4′-pyrimidin]-2′(3′ H )-ones as Novel Antimicrobial and Antioxidant Agents | Diastereoselective Synthesis and Biological Evaluation of Spiro[chromane-2,4′-pyrimidin]-2′(3′ H )-ones as Novel Antimicrobial and Antioxidant Agents Abstract This study reports an improved diastereoselective synthesis of substituted spiro[chromane-2,4′-pyrimidin]-2′(3′ H )-ones via the acid-catalyzed condensation of 6... |
PMC10648923 | core_pubmed_pmc | Simplified urine-based method to detect rifampin underexposure in adults with tuberculosis: a prospective diagnostic accuracy study | Simplified urine-based method to detect rifampin underexposure in adults with tuberculosis: a prospective diagnostic accuracy study Abstract ABSTRACT Variable pharmacokinetics of rifampin in tuberculosis (TB) treatment can lead to poor outcomes. Urine spectrophotometry is simpler and more accessible than recommended se... |
PMC7579232 | core_pubmed_pmc | Pomegranate Juice does not Affect the Bioavailability of Cyclosporine in Healthy Thai Volunteers | Pomegranate Juice does not Affect the Bioavailability of Cyclosporine in Healthy Thai Volunteers Abstract Background It is still controversial whether pomegranate causes drug interactions. Pomegranate juice has been shown to inhibit CYP3A in-vitro and animal studies. The co-administration of pomegranate juice with cycl... |
PMC8471929 | core_pubmed_pmc | Gene Expression and Protein Abundance of Hepatic Drug Metabolizing Enzymes in Liver Pathology | Gene Expression and Protein Abundance of Hepatic Drug Metabolizing Enzymes in Liver Pathology Abstract Hepatic drug metabolizing enzymes (DMEs) markedly affect drug pharmacokinetics. Because liver diseases may alter enzymatic function and in turn drug handling and clinical efficacy, we investigated DMEs expression in d... |
PMC10771754 | core_pubmed_pmc | TQB2450 in patients with advanced malignant tumors: results from a phase I dose-escalation and expansion study | TQB2450 in patients with advanced malignant tumors: results from a phase I dose-escalation and expansion study Abstract Abstract Background: Immune checkpoint inhibitor therapy has demonstrated impressive clinical benefits in multiple tumor types. TQB2450, a novel monoclonal antibody targeting programmed cell death lig... |
PMC10064968 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Ruxolitinib: A Review | Pharmacokinetics and Pharmacodynamics of Ruxolitinib: A Review Abstract Abstract Background and Objective Ruxolitinib is a tyrosine kinase inhibitor targeting the Janus kinase (JAK) and signal transducer and activator of transcription (STAT) pathways. Ruxolitinib is used to treat myelofibrosis, polycythemia vera and st... |
PMC12223915 | core_pubmed_pmc | Serum Pharmacology Combined with Network Pharmacology Reveals the Effects and Mechanisms of Ganmai Dazao Decoction in the Treatment of Depression | Serum Pharmacology Combined with Network Pharmacology Reveals the Effects and Mechanisms of Ganmai Dazao Decoction in the Treatment of Depression Abstract Abstract Ganmai Dazao Decoction (GMZ) is a famous classic traditional Chinese medicine compound prescription for the treatment of depression and has a good clinical ... |
PMC7062864 | core_pubmed_pmc | The Steps to Therapeutic Drug Monitoring: A Structured Approach Illustrated With Imatinib | The Steps to Therapeutic Drug Monitoring: A Structured Approach Illustrated With Imatinib Abstract Abstract Pharmacometric methods have hugely benefited from progress in analytical and computer sciences during the past decades, and play nowadays a central role in the clinical development of new medicinal drugs. It is t... |
PMC12306963 | core_pubmed_pmc | The Individual and Interactive Effects of Alpha-Pinene and Delta-9-Tetrahydrocannabinol in Healthy Adults | The Individual and Interactive Effects of Alpha-Pinene and Delta-9-Tetrahydrocannabinol in Healthy Adults Abstract Abstract Introduction Cannabis contains hundreds of chemical constituents beyond delta-9-tetrahydrocannabinol (Δ9-THC), which is thought to be the primary driver of most of its acute pharmacodynamic effect... |
PMC6643060 | core_pubmed_pmc | Pharmacokinetics of the Yougui pill in experimental autoimmune encephalomyelitis model rats and its pharmacological activity in vitro | Pharmacokinetics of the Yougui pill in experimental autoimmune encephalomyelitis model rats and its pharmacological activity in vitro Abstract Purpose To determine the pharmacokinetic properties and pharmacological activity of the Yougui pill (YGP), which is a well-known Chinese medicine formula. Methods An ultra-perfo... |
PMC7060842 | core_pubmed_pmc | Dexmedetomidine Pharmacokinetics in Neonates with Hypoxic-Ischemic Encephalopathy Receiving Hypothermia | Dexmedetomidine Pharmacokinetics in Neonates with Hypoxic-Ischemic Encephalopathy Receiving Hypothermia Abstract Abstract Dexmedetomidine is a promising sedative and analgesic for newborns with hypoxic-ischemic encephalopathy (HIE) undergoing therapeutic hypothermia (TH). Pharmacokinetics and safety of dexmedetomidine ... |
PMC10215193 | core_pubmed_pmc | Evaluation of Dosing Guidelines for Gentamicin in Neonates and Children | Evaluation of Dosing Guidelines for Gentamicin in Neonates and Children Abstract Abstract Although aminoglycosides are frequently prescribed to neonates and children, the ability to reach effective and safe target concentrations with the currently used dosing regimens remains unclear. This study aims to evaluate the ta... |
PMC3419955 | core_pubmed_pmc | Phase I dose-escalation study of aflibercept in combination with docetaxel and cisplatin in patients with advanced solid tumours | Phase I dose-escalation study of aflibercept in combination with docetaxel and cisplatin in patients with advanced solid tumours Abstract Background: This phase I cohort study investigated aflibercept (vascular endothelial growth factor (VEGF) trap) plus docetaxel and cisplatin in patients with advanced solid tumours. ... |
PMC10689903 | core_pubmed_pmc | Swedish multicentre study of target attainments with β-lactams in the ICU: which MIC parameter should be used? | Swedish multicentre study of target attainments with β-lactams in the ICU: which MIC parameter should be used? Abstract Abstract Background Therapeutic drug monitoring (TDM) has been suggested to optimize antimicrobial target attainment, typically using 100%T >MIC , in β-lactam treatment in the ICU. The MIC parameter u... |
PMC12269393 | core_pubmed_pmc | A multiscale physiologically based pharmacokinetic model to support mRNA-encoded BiTE therapy in cancer treatment | A multiscale physiologically based pharmacokinetic model to support mRNA-encoded BiTE therapy in cancer treatment Abstract Abstract In the field of cancer therapy, bispecific T cell engagers (BiTEs) have demonstrated significant potential. However, their clinical application is constrained by challenges in production a... |
PMC12455781 | core_pubmed_pmc | Development and validation of a sustainable spectrofluorimetric method for simultaneous quantification of amlodipine and aspirin using genetic algorithm-enhanced partial least squares regression | Development and validation of a sustainable spectrofluorimetric method for simultaneous quantification of amlodipine and aspirin using genetic algorithm-enhanced partial least squares regression Abstract The widespread clinical utilization of amlodipine-aspirin combinations, despite potential pharmacodynamic interactio... |
PMC11305208 | core_pubmed_pmc | Bioavailability of dronedarone tablets administered with or without food in healthy participants | Bioavailability of dronedarone tablets administered with or without food in healthy participants Abstract Abstract Study objective There is inadequate awareness of the effect of food on the bioavailability of dronedarone. We report results from two phase 1 studies assessing the effect of food on dronedarone's bioavaila... |
PMC5386126 | core_pubmed_pmc | Effect of B-complex vitamins on the antifatigue activity and bioavailability of ginsenoside Re after oral administration | Effect of B-complex vitamins on the antifatigue activity and bioavailability of ginsenoside Re after oral administration Abstract Background Both ginsenoside Re and B-complex vitamins are widely used as nutritional supplements. They are often taken together so as to fully utilize their antifatigue and refreshing effect... |
PMC6211014 | core_pubmed_pmc | Association Between PM 2.5 and Daily Hospital Admissions for Heart Failure: A Time-Series Analysis in Beijing | Association Between PM 2.5 and Daily Hospital Admissions for Heart Failure: A Time-Series Analysis in Beijing Abstract Abstract There is little evidence that acute exposure to fine particulate matter (PM 2.5 ) impacts the rate of hospitalization for congestive heart failure (CHF) in developing countries. The primary pu... |
PMC5110617 | core_pubmed_pmc | The effect of Fisher information matrix approximation methods in population optimal design calculations | The effect of Fisher information matrix approximation methods in population optimal design calculations Abstract With the increasing popularity of optimal design in drug development it is important to understand how the approximations and implementations of the Fisher information matrix (FIM) affect the resulting optim... |
PMC4108102 | core_pubmed_pmc | Evaluation of Daptomycin Non-Susceptible Staphylococcus aureus for Stability, Population Profiles, mprF Mutations, and Daptomycin Activity | Evaluation of Daptomycin Non-Susceptible Staphylococcus aureus for Stability, Population Profiles, mprF Mutations, and Daptomycin Activity Abstract Introduction Despite studies examining daptomycin non-susceptible (DNS) Staphylococcus aureus , examination of the stability and population profiles is limited. The objecti... |
PMC9986446 | core_pubmed_pmc | Development, testing, parameterisation, and calibration of a human PBPK model for the plasticiser, di-(2-ethylhexyl) terephthalate (DEHTP) using in silico , in vitro and human biomonitoring data | Development, testing, parameterisation, and calibration of a human PBPK model for the plasticiser, di-(2-ethylhexyl) terephthalate (DEHTP) using in silico , in vitro and human biomonitoring data Abstract Abstract A physiologically based pharmacokinetic model for di-(2-ethylhexyl) terephthalate (DEHTP) based on a refine... |
PMC8093546 | core_pubmed_pmc | Gastric floating tablet improves the bioavailability and reduces the hypokalemia effect of gossypol in vivo | Gastric floating tablet improves the bioavailability and reduces the hypokalemia effect of gossypol in vivo Abstract Abstract Gossypol (Gos) is a natural polyphenolic compound that has shown a number of valuable biological properties such as antifertility, antioxidation, and antitumor activities. However, the clinical ... |
PMC4520130 | core_pubmed_pmc | Targeting anti-apoptotic Bcl-2 by AT-101 to increase radiation efficacy: data from in vitro and clinical pharmacokinetic studies in head and neck cancer | Targeting anti-apoptotic Bcl-2 by AT-101 to increase radiation efficacy: data from in vitro and clinical pharmacokinetic studies in head and neck cancer Abstract Abstract Background Pro-survival Bcl-2 family members can promote cancer development and contribute to treatment resistance. Head and neck squamous cell carci... |
PMC12944153 | core_pubmed_pmc | Evaluating the Impact of CYP2D6 Phenotype on Fluvoxamine Pharmacokinetics in Geriatric Patients Using Physiologically Based Pharmacokinetic Modeling | Evaluating the Impact of CYP2D6 Phenotype on Fluvoxamine Pharmacokinetics in Geriatric Patients Using Physiologically Based Pharmacokinetic Modeling Abstract Background/Objectives : Fluvoxamine is commonly prescribed for depressive disorders in elderly patients, a population that frequently exhibits variable drug respo... |
PMC8525652 | core_pubmed_pmc | Circadian Effects of Drug Responses | Circadian Effects of Drug Responses Abstract Circadian rhythms describe physiological systems that repeat themselves with a cycle of approximately 24 h. Our understanding of the cellular and molecular origins of these oscillations has improved dramatically, allowing us to appreciate the significant role these oscillati... |
PMC12065682 | core_pubmed_pmc | Drug dissolution problems in ostomy patients: a chart review and patient interview analysis | Drug dissolution problems in ostomy patients: a chart review and patient interview analysis Abstract Purpose The pharmacokinetic properties of peroral drugs, e.g. considering dissolution, release and absorption, can be influenced by a shortened transit time after ostomy placement. Its aim was to find unexpected undisso... |
PMC8289197 | core_pubmed_pmc | Diabetic Retinopathy in the Aging Population: A Perspective of Pathogenesis and Treatment | Diabetic Retinopathy in the Aging Population: A Perspective of Pathogenesis and Treatment Abstract Abstract The elderly population in the United States is projected to almost double by the year 2050. In addition, the numbers of diabetics are rising, along with its most common complication, diabetic retinopathy (DR). To... |
PMC8711562 | core_pubmed_pmc | Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug–Drug Interaction | Simultaneous Determination of Loratadine and Its Metabolite Desloratadine in Beagle Plasma by LC-MS/MS and Application for Pharmacokinetics Study of Loratadine Tablets and Omeprazole‑Induced Drug–Drug Interaction Abstract Background Loratadine (LTD) is a Biopharmaceutical Classification System II basic drug with pH-sen... |
PMC9007951 | core_pubmed_pmc | Systematically evaluating DOTATATE and FDG as PET immuno-imaging tracers of cardiovascular inflammation | Systematically evaluating DOTATATE and FDG as PET immuno-imaging tracers of cardiovascular inflammation Abstract In recent years, cardiovascular immuno-imaging by positron emission tomography (PET) has undergone tremendous progress in preclinical settings. Clinically, two approved PET tracers hold great potential for i... |
PMC6463033 | core_pubmed_pmc | Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants | Pharmacogenomics of Novel Direct Oral Anticoagulants: Newly Identified Genes and Genetic Variants Abstract Direct oral anticoagulants (DOAC) have shown an upward prescribing trend in recent years due to favorable pharmacokinetics and pharmacodynamics without requirement for routine coagulation monitoring. However, rece... |
PMC12158726 | core_pubmed_pmc | Population pharmacokinetic analysis of rivaroxaban in healthy volunteers and patients with radiofrequency ablation of non-valvular atrial fibrillation in China | Population pharmacokinetic analysis of rivaroxaban in healthy volunteers and patients with radiofrequency ablation of non-valvular atrial fibrillation in China Abstract Abstract Aims This study aimed to develop a population pharmacokinetic (PopPK) model of rivaroxaban in healthy volunteers and patients with radiofreque... |
PMC4900982 | core_pubmed_pmc | Onset of Glycemic and Weight Outcomes in Patients Initiating Exenatide Once Weekly: The Relationship of Exenatide Exposure with Efficacy over the First 24 Weeks of Treatment | Onset of Glycemic and Weight Outcomes in Patients Initiating Exenatide Once Weekly: The Relationship of Exenatide Exposure with Efficacy over the First 24 Weeks of Treatment Abstract Abstract Introduction Exenatide is gradually released from exenatide once weekly (QW) microspheres, and at steady state, consistently con... |
PMC7300169 | core_pubmed_pmc | Influence of sampling schedules on [ 177 Lu]Lu-PSMA dosimetry | Influence of sampling schedules on [ 177 Lu]Lu-PSMA dosimetry Abstract Abstract Background Individualized dosimetry is recommended for [ 177 Lu]Lu-PSMA radioligand therapy (RLT) which is resource-intensive and protocols are often not optimized. Therefore, a simulation study was performed focusing on the determination o... |
PMC6323662 | core_pubmed_pmc | A phase I, randomized, observer-blinded, single and multiple ascending-dose study to investigate the safety, pharmacokinetics, and immunogenicity of BITS7201A, a bispecific antibody targeting IL-13 and IL-17, in healthy volunteers | A phase I, randomized, observer-blinded, single and multiple ascending-dose study to investigate the safety, pharmacokinetics, and immunogenicity of BITS7201A, a bispecific antibody targeting IL-13 and IL-17, in healthy volunteers Abstract Background Inhibition of interleukin (IL)-13, a Type 2 inflammatory mediator in ... |
PMC12588639 | core_pubmed_pmc | Pharmacokinetic Characterization of Rituximab in Patients with Glomerular Diseases | Pharmacokinetic Characterization of Rituximab in Patients with Glomerular Diseases Abstract Supplemental Digital Content is Available in the Text. Background: Rituximab is commonly used to treat patients with primary glomerular diseases; however, its pharmacokinetics in this population have not been fully described yet... |
PMC11735518 | core_pubmed_pmc | Ocrelizumab dose selection for treatment of pediatric relapsing–remitting multiple sclerosis: results of the OPERETTA I study | Ocrelizumab dose selection for treatment of pediatric relapsing–remitting multiple sclerosis: results of the OPERETTA I study Abstract Background The presented study identified the appropriate ocrelizumab dosing regimen for patients with pediatric-onset multiple sclerosis (POMS). Methods Patients with POMS aged 10–17 y... |
PMC6590663 | core_pubmed_pmc | Liraglutide effects in a paediatric (7‐11 y) population with obesity: A randomized, double‐blind, placebo‐controlled, short‐term trial to assess safety, tolerability, pharmacokinetics, and pharmacodynamics | Liraglutide effects in a paediatric (7‐11 y) population with obesity: A randomized, double‐blind, placebo‐controlled, short‐term trial to assess safety, tolerability, pharmacokinetics, and pharmacodynamics Abstract Summary Background Childhood obesity is a major public health concern with limited treatment options. Obj... |
PMC5718031 | core_pubmed_pmc | Intestinally-restricted Janus Kinase inhibition: a potential approach to maximize the therapeutic index in inflammatory bowel disease therapy | Intestinally-restricted Janus Kinase inhibition: a potential approach to maximize the therapeutic index in inflammatory bowel disease therapy Abstract Abstract Background An unmet need remains for safe and effective treatments to induce and maintain remission in inflammatory bowel disease (IBD) patients. The Janus kina... |
PMC7958319 | core_pubmed_pmc | Sensitive, High-Throughput Liquid Chromatography-Tandem Mass Spectrometry Analysis of Atorvastatin and Its Pharmacologically Active Metabolites in Serum for Supporting Precision Pharmacotherapy | Sensitive, High-Throughput Liquid Chromatography-Tandem Mass Spectrometry Analysis of Atorvastatin and Its Pharmacologically Active Metabolites in Serum for Supporting Precision Pharmacotherapy Abstract The antihyerlipidemic drug atorvastatin (ATR) is used worldwide as part of the strategy to prevent cardiovascular eve... |
PMC11372059 | core_pubmed_pmc | Pharmacokinetic model-based assessment of factor IX prophylaxis treatment regimens in severe hemophilia B | Pharmacokinetic model-based assessment of factor IX prophylaxis treatment regimens in severe hemophilia B Abstract Abstract An important aspect of improving care for people with hemophilia B (HB) is developing optimal treatment strategies. Here we aimed to provide in-silico evidence, comparing the estimated optimal pos... |
PMC11352038 | core_pubmed_pmc | In Vitro and In Silico Studies of the Antimicrobial Activity of Prenylated Phenylpropanoids of Green Propolis and Their Derivatives against Oral Bacteria | In Vitro and In Silico Studies of the Antimicrobial Activity of Prenylated Phenylpropanoids of Green Propolis and Their Derivatives against Oral Bacteria Abstract Abstract Artepillin C, drupanin, and plicatin B are prenylated phenylpropanoids that naturally occur in Brazilian green propolis. In this study, these compou... |
PMC9121888 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of verinurad with and without allopurinol in healthy Asian, Chinese, and non‐Asian participants | Pharmacokinetics, pharmacodynamics, and safety of verinurad with and without allopurinol in healthy Asian, Chinese, and non‐Asian participants Abstract Abstract Verinurad is a selective inhibitor of uric acid transporter 1 (URAT1). Here, we assessed the safety, pharmacokinetics, and pharmacodynamics of verinurad + allo... |
PMC6384561 | core_pubmed_pmc | Deltamethrin Residues in Milk and Cheese of Lactating Goats ( Capra hircus ) | Deltamethrin Residues in Milk and Cheese of Lactating Goats ( Capra hircus ) Abstract Abstract The distribution of pyrethroid insecticide deltamethrin (DLM) in goat milk and cheese (caciotta) following pour-on administration at the sheep dosage (DLMS-10 mL/60 kg body weight) and double dosage (DLMD-20 mL/60 kg body wei... |
PMC9054874 | core_pubmed_pmc | Pharmacokinetics of metronomic temozolomide in cerebrospinal fluid of children with malignant central nervous system tumors | Pharmacokinetics of metronomic temozolomide in cerebrospinal fluid of children with malignant central nervous system tumors Abstract Purpose Although temozolomide is widely used in the treatment of childhood central nervous system (CNS) tumors, information on its pharmacokinetic profile in the brain or cerebrospinal fl... |
PMC10748184 | core_pubmed_pmc | The Pharmacokinetics of CPZEN-45, a Novel Anti-Tuberculosis Drug, in Guinea Pigs | The Pharmacokinetics of CPZEN-45, a Novel Anti-Tuberculosis Drug, in Guinea Pigs Abstract CPZEN-45 is a novel compound with activity against drug-susceptible and drug-resistant tuberculosis (TB). The present study was undertaken to determine the best dose and dosing regimen of inhalable CPZEN-45 powders to use in effic... |
PMC9603770 | core_pubmed_pmc | Broad-Spectrum Inhibitors against Class A, B, and C Type β-Lactamases to Block the Hydrolysis against Antibiotics: Kinetics and Structural Characterization | Broad-Spectrum Inhibitors against Class A, B, and C Type β-Lactamases to Block the Hydrolysis against Antibiotics: Kinetics and Structural Characterization Abstract ABSTRACT The emergence of antibiotic resistance has led to a global crisis for the physician to handle infection control issues. All antibiotics, including... |
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