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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...