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PMC4057332
core_pubmed_pmc
Critical appraisal of pemetrexed in the treatment of NSCLC and metastatic pulmonary nodules
Critical appraisal of pemetrexed in the treatment of NSCLC and metastatic pulmonary nodules Abstract Pemetrexed, a new multitarget antifolate antineoplastic agent, has significantly improved the overall survival in nonsquamous non-small-cell lung cancer patients. Presently, pemetrexed is recommended for first line trea...
PMC5772397
core_pubmed_pmc
Antibacterial effect evaluation of moxalactam against extended-spectrum β-lactamase-producing Escherichia coli and Klebsiella pneumoniae with in vitro pharmacokinetics/pharmacodynamics simulation
Antibacterial effect evaluation of moxalactam against extended-spectrum β-lactamase-producing Escherichia coli and Klebsiella pneumoniae with in vitro pharmacokinetics/pharmacodynamics simulation Abstract Objectives The aim of this study was to evaluate the bactericidal effects of moxalactam (MOX), cefotaxime (CTX), an...
PMC7733004
core_pubmed_pmc
Inclusion of non-inferiority analysis in superiority-based clinical trials with single-arm, two-stage Simon's design
Inclusion of non-inferiority analysis in superiority-based clinical trials with single-arm, two-stage Simon's design Abstract Introduction Non-inferiority (NI) analysis is not usually considered in the early phases of clinical development. In some negative phase II trials, a post-hoc NI analysis justified additional ph...
PMC10574112
core_pubmed_pmc
Development of a New Benzofuran–Pyrazole–Pyridine-Based Molecule for the Management of Osteoarthritis
Development of a New Benzofuran–Pyrazole–Pyridine-Based Molecule for the Management of Osteoarthritis Abstract Abstract Osteoarthritis is a substantial burden for patients with the disease. The known medications for the disease target the mitigation of the disease’s symptoms. So, drug development for the management of ...
PMC12472637
core_pubmed_pmc
Use of TLC and Computational Methods to Determine Lipophilicity Parameters of Selected Neuroleptics: Comparison of Experimental and Theoretical Studies
Use of TLC and Computational Methods to Determine Lipophilicity Parameters of Selected Neuroleptics: Comparison of Experimental and Theoretical Studies Abstract Abstract Background: Compound lipophilicity is a fundamental physicochemical property for determining the pharmacokinetic and pharmacodynamic profiles of thera...
PMC11481554
core_pubmed_pmc
Integration of genomic and pharmacokinetic data to predict clinical outcomes in HIV-associated cryptococcal meningitis
Integration of genomic and pharmacokinetic data to predict clinical outcomes in HIV-associated cryptococcal meningitis Abstract ABSTRACT Cryptococcal meningitis causes an estimated 112,000 global deaths per annum. Genomic and phenotypic features of the infecting strain of Cryptococcus spp. have been associated with out...
PMC7276966
core_pubmed_pmc
Amikacin pharmacokinetic/pharmacodynamic in intensive care unit: a prospective database
Amikacin pharmacokinetic/pharmacodynamic in intensive care unit: a prospective database Abstract Background Aminoglycosides have a concentration-dependent therapeutic effect when peak serum concentration ( C max ) reaches eight to tenfold the minimal inhibitory concentration (MIC). With an amikacin MIC of 8 mg/L, the C...
PMC12054466
core_pubmed_pmc
Development of N,P-doped carbon quantum dots as a green fluorescent probe for fexofenadine determination: mechanistic studies, Box–Behnken optimization, and pharmacokinetic application †
Development of N,P-doped carbon quantum dots as a green fluorescent probe for fexofenadine determination: mechanistic studies, Box–Behnken optimization, and pharmacokinetic application † Abstract A sensitive and selective fluorescence quenching method based on nitrogen and phosphorus co-doped carbon quantum dots (N,P C...
PMC11703413
core_pubmed_pmc
Do CYP2D6 genotypes affect oxycodone dose, pharmacokinetics, pain, and adverse effects in cancer?
Do CYP2D6 genotypes affect oxycodone dose, pharmacokinetics, pain, and adverse effects in cancer? Abstract ABSTRACT Aims To examine the associations between CYP2D6 and CYP3A4 polymorphisms, plasma oxycodone and metabolite concentrations, and oxycodone response (dose, pain scores, and adverse effects) in people with pai...
PMC4833300
core_pubmed_pmc
Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade
Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade Abstract Chagas disease is a significant health problem in Latin America and the available treatments have significant issues in terms of toxicity and efficacy. There is thus an urgent need...
PMC6321466
core_pubmed_pmc
Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats
Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats Abstract Abstract The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a no...
PMC6058476
core_pubmed_pmc
Novel application of pluronic lecithin organogels (PLOs) for local delivery of synergistic combination of docetaxel and cisplatin to improve therapeutic efficacy against ovarian cancer
Novel application of pluronic lecithin organogels (PLOs) for local delivery of synergistic combination of docetaxel and cisplatin to improve therapeutic efficacy against ovarian cancer Abstract Abstract The synergistic combination of docetaxel (DTX) and cisplatin (CIS) by local drug delivery with a pluronic lecithin or...
PMC4249579
core_pubmed_pmc
Open-Label Crossover Study of Primaquine and Dihydroartemisinin-Piperaquine Pharmacokinetics in Healthy Adult Thai Subjects
Open-Label Crossover Study of Primaquine and Dihydroartemisinin-Piperaquine Pharmacokinetics in Healthy Adult Thai Subjects Abstract Dihydroartemisinin-piperaquine is an artemisinin-based combination treatment (ACT) recommended by the WHO for uncomplicated Plasmodium falciparum malaria, and it is being used increasingl...
PMC9257283
core_pubmed_pmc
Dogs as a Natural Animal Model of Epilepsy
Dogs as a Natural Animal Model of Epilepsy Abstract Epilepsy is a common neurological disease in both humans and domestic dogs, making dogs an ideal translational model of epilepsy. In both species, epilepsy is a complex brain disease characterized by an enduring predisposition to generate spontaneous recurrent epilept...
PMC12706821
core_pubmed_pmc
Chronic Alcoholism and Propofol Demand: The Impact of Alcohol Tolerance in Painless Gastrointestinal Endoscopy
Chronic Alcoholism and Propofol Demand: The Impact of Alcohol Tolerance in Painless Gastrointestinal Endoscopy Abstract ABSTRACT Background and Aim Existing research suggests that chronic alcohol consumption may increase propofol requirements during anesthesia, though findings remain inconsistent. This study investigat...
PMC9148946
core_pubmed_pmc
A new perspective to improve the treatment of Lianhuaqingwen on COVID-19 and prevent the environmental health risk of medication
A new perspective to improve the treatment of Lianhuaqingwen on COVID-19 and prevent the environmental health risk of medication Abstract Abstract Lianhuaqingwen (LH), one traditional Chinese medicine (TCM), has been used to treat the coronavirus disease 2019 (COVID-19), but its ecotoxicity with potential human health ...
PMC9740829
core_pubmed_pmc
Salvianolic Acid B Strikes Back: New Evidence in the Modulation of Expression and Activity of Matrix Metalloproteinase 9 in MDA-MB-231 Human Breast Cancer Cells
Salvianolic Acid B Strikes Back: New Evidence in the Modulation of Expression and Activity of Matrix Metalloproteinase 9 in MDA-MB-231 Human Breast Cancer Cells Abstract Abstract Salvianolic acid B (SalB) is a bioactive compound from Salviae miltiorrhizae , one of the most important traditional herbal medicines widely ...
PMC5171718
core_pubmed_pmc
Using anti-poly(ethylene glycol) bioparticles for the quantitation of PEGylated nanoparticles
Using anti-poly(ethylene glycol) bioparticles for the quantitation of PEGylated nanoparticles Abstract Abstract Attachment of polyethylene glycol (PEG) molecules to nanoparticles (PEGylation) is a widely-used method to improve the stability, biocompatibility and half-life of nanomedicines. However, the evaluation of th...
PMC6867604
core_pubmed_pmc
A comparison of genetic sampling methodologies for candidate-gene analyses
A comparison of genetic sampling methodologies for candidate-gene analyses Abstract Much of the recent gains in knowledge regarding the influence of patient genetics on medication pharmacokinetics (drug absorption, distribution, metabolism and elimination) how patients process medications) and pharmacodynamics (drug re...
PMC8167066
core_pubmed_pmc
A Biosimilarity Study Between QX001S and Ustekinumab in Healthy Chinese Male Subjects
A Biosimilarity Study Between QX001S and Ustekinumab in Healthy Chinese Male Subjects Abstract Abstract Objective: To evaluate the tolerance, variability, and pharmacokinetics (PK) of QX001S, a biosimilar for ustekinumab, in healthy Chinese men. Methods: One hundred and seventy-eight healthy men were recruited in this ...
PMC3997354
core_pubmed_pmc
Genetic Polymorphism of Cytochrome P450 4F2, Vitamin E Level and Histological Response in Adults and Children with Nonalcoholic Fatty Liver Disease Who Participated in PIVENS and TONIC Clinical Trials
Genetic Polymorphism of Cytochrome P450 4F2, Vitamin E Level and Histological Response in Adults and Children with Nonalcoholic Fatty Liver Disease Who Participated in PIVENS and TONIC Clinical Trials Abstract Abstract Vitamin E improved liver histology in children and adults with NAFLD who participated in TONIC and PI...
PMC12011604
core_pubmed_pmc
Potential inappropriate medications and drug–drug interactions in adverse drug reactions in the elderly: a retrospective study in a pharmacovigilance database
Potential inappropriate medications and drug–drug interactions in adverse drug reactions in the elderly: a retrospective study in a pharmacovigilance database Abstract Abstract Introduction Potential inappropriate medications (PIMs) and potential drug–drug interactions (pDDIs) are important factors leading to adverse d...
PMC5629131
core_pubmed_pmc
Pharmacokinetics of Bevacizumab in Three Patients Under the Age of 3 Years with CNS Malignancies
Pharmacokinetics of Bevacizumab in Three Patients Under the Age of 3 Years with CNS Malignancies Abstract Abstract Background Bevacizumab is a recombinant antibody that is increasingly used in pediatric malignancies. The pharmacokinetics of bevacizumab in pediatric patients have been shown to be influenced by tumor loc...
PMC9298541
core_pubmed_pmc
[ 68 Ga]Ga-DOTA-Siglec-9 Detects Pharmacodynamic Changes of FAP-Targeted IL2 Variant Immunotherapy in B16-FAP Melanoma Mice
[ 68 Ga]Ga-DOTA-Siglec-9 Detects Pharmacodynamic Changes of FAP-Targeted IL2 Variant Immunotherapy in B16-FAP Melanoma Mice Abstract Abstract Vascular adhesion protein-1 (VAP-1) is an inflammation-inducible adhesion molecule, which supports contact between leukocytes and inflamed endothelium. There is evidence that VAP...
PMC12927183
core_pubmed_pmc
PM 2.5 and its chemical components interact with hypoxia to increase the risk of hospitalization for peripheral arterial disease
PM 2.5 and its chemical components interact with hypoxia to increase the risk of hospitalization for peripheral arterial disease Abstract Abstract This study investigated the combined effects of fine particulate matter (PM 2.5 ) exposure and ambient oxygen (O 2 ) availability on peripheral artery disease (PAD) hospital...
PMC12386638
core_pubmed_pmc
Caffeine in Aging Brains: Cognitive Enhancement, Neurodegeneration, and Emerging Concerns About Addiction
Caffeine in Aging Brains: Cognitive Enhancement, Neurodegeneration, and Emerging Concerns About Addiction Abstract This narrative review examines the effects of caffeine on brain health in older adults, with particular attention to its potential for dependence—an often-overlooked issue in geriatric care. Caffeine acts ...
PMC6398875
core_pubmed_pmc
Phase I study of alpelisib (BYL719), an α‐specific PI3K inhibitor, in Japanese patients with advanced solid tumors
Phase I study of alpelisib (BYL719), an α‐specific PI3K inhibitor, in Japanese patients with advanced solid tumors Abstract This phase I study aimed to determine tolerability and preliminary efficacy of single‐agent alpelisib (BYL719) in Japanese patients with advanced solid malignancies. The primary objective of the s...
PMC12339841
core_pubmed_pmc
Exploring Human Use of Monoclonal Antibodies Against Critical Bacteria: A Scoping Review of Clinical Trials
Exploring Human Use of Monoclonal Antibodies Against Critical Bacteria: A Scoping Review of Clinical Trials Abstract Abstract Introduction The global spread of multidrug-resistant organisms (MDROs), particularly the World Health Organization (WHO) priority pathogens, poses a major challenge to infection treatment, nece...
PMC5351312
core_pubmed_pmc
Efficiency of Ipratropium Bromide and Albuterol Deposition in the Lung Delivered via a Soft Mist Inhaler or Chlorofluorocarbon Metered‐Dose Inhaler
Efficiency of Ipratropium Bromide and Albuterol Deposition in the Lung Delivered via a Soft Mist Inhaler or Chlorofluorocarbon Metered‐Dose Inhaler Abstract The propellant‐free Combivent Respimat Soft Mist Inhaler (CVT‐R) was developed to replace the chlorofluorocarbon‐propelled Combivent metered‐dose inhaler (CVT‐MDI)...
PMC9297106
core_pubmed_pmc
Phase I study of intraperitoneal aerosolized nanoparticle albumin based paclitaxel (NAB-PTX) for unresectable peritoneal metastases
Phase I study of intraperitoneal aerosolized nanoparticle albumin based paclitaxel (NAB-PTX) for unresectable peritoneal metastases Abstract Summary Background Pressurized intraperitoneal aerosolized chemotherapy (PIPAC) is a novel method to treat patients with peritoneal metastases (PM). We aimed to study the tolerabi...
PMC8934763
core_pubmed_pmc
Opioids and Falls Risk in Older Adults: A Narrative Review
Opioids and Falls Risk in Older Adults: A Narrative Review Abstract Abstract Pain treatment is important in older adults but may result in adverse events such as falls. Opioids are effective for nociceptive pain but the evidence for neuropathic pain is weak. Nevertheless, both pain and opioids may increase the risk of ...
PMC8969529
core_pubmed_pmc
Safety, antiviral activity and pharmacokinetics of JNJ-64530440, a novel capsid assembly modulator, as 4 week monotherapy in treatment-naive patients with chronic hepatitis B virus infection
Safety, antiviral activity and pharmacokinetics of JNJ-64530440, a novel capsid assembly modulator, as 4 week monotherapy in treatment-naive patients with chronic hepatitis B virus infection Abstract Abstract Objectives We investigated JNJ-64530440 (a hepatitis B virus capsid assembly modulator) safety, antiviral activ...
PMC12735687
core_pubmed_pmc
Therapeutic Potentials of Phytochemicals in Pancreatitis: Targeting Calcium Signaling, Ferroptosis, microRNAs, and Inflammation with Drug-Likeness Evaluation
Therapeutic Potentials of Phytochemicals in Pancreatitis: Targeting Calcium Signaling, Ferroptosis, microRNAs, and Inflammation with Drug-Likeness Evaluation Abstract Background: Pancreatitis, encompassing acute (AP), severe acute (SAP), and chronic (CP) forms, is a life-threatening inflammatory disorder with limited t...
PMC7344705
core_pubmed_pmc
Influence of Single Nucleotide Polymorphisms on Rifampin Pharmacokinetics in Tuberculosis Patients
Influence of Single Nucleotide Polymorphisms on Rifampin Pharmacokinetics in Tuberculosis Patients Abstract Rifampin (RF) is metabolized in the liver into an active metabolite 25-desacetylrifampin and excreted almost equally via biliary and renal routes. Various influx and efflux transporters influence RF disposition d...
PMC5286864
core_pubmed_pmc
A multicenter, randomized, open-label, active-comparator trial to determine the efficacy, safety, and pharmacokinetics of intravenous ibuprofen for treatment of fever in hospitalized pediatric patients
A multicenter, randomized, open-label, active-comparator trial to determine the efficacy, safety, and pharmacokinetics of intravenous ibuprofen for treatment of fever in hospitalized pediatric patients Abstract Background Oral antipyretics are commonly used to treat pediatric patients who develop fevers. However, patie...
PMC12370230
core_pubmed_pmc
Human oral pharmacokinetics of 4-hydroxy isoleucine and dosage simulation studies for predicting its pharmacodynamics in diabetes
Human oral pharmacokinetics of 4-hydroxy isoleucine and dosage simulation studies for predicting its pharmacodynamics in diabetes Abstract Abstract INTRODUCTION: 4-hydroxy isoleucine (4-HIL), a potent glucose-lowering agent and insulin secretagogue, is widely available in nutraceutical market as fenugreek seed extract ...
PMC8598283
core_pubmed_pmc
High unbound flucloxacillin fraction in critically ill patients
High unbound flucloxacillin fraction in critically ill patients Abstract Abstract Objectives To describe the unbound and total flucloxacillin pharmacokinetics in critically ill patients and to define optimal dosing strategies. Patients and methods Observational multicentre study including a total of 33 adult ICU patien...
PMC8146514
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Cefepime in Adults with Hematological Malignancies and Febrile Neutropenia after Chemotherapy
Pharmacokinetics and Pharmacodynamics of Cefepime in Adults with Hematological Malignancies and Febrile Neutropenia after Chemotherapy Abstract Patients with chemotherapy-induced febrile neutropenia (CIFN) may have changes in the pharmacokinetics (PK) compared to patients without malignancies or neutropenia. Those chan...
PMC3934590
core_pubmed_pmc
Nanostructured lipid carriers as a novel oral delivery system for triptolide: induced changes in pharmacokinetics profile associated with reduced toxicity in male rats
Nanostructured lipid carriers as a novel oral delivery system for triptolide: induced changes in pharmacokinetics profile associated with reduced toxicity in male rats Abstract Abstract After oral administration in rodents, triptolide (TP), a diterpenoid triepoxide compound, active as anti-inflammatory, immunosuppressi...
PMC4716584
core_pubmed_pmc
A Systems Pharmacology Model for Predicting Effects of Factor Xa Inhibitors in Healthy Subjects: Assessment of Pharmacokinetics and Binding Kinetics
A Systems Pharmacology Model for Predicting Effects of Factor Xa Inhibitors in Healthy Subjects: Assessment of Pharmacokinetics and Binding Kinetics Abstract Factor Xa (FXa) emerged as a promising target for effective anticoagulation and several FXa inhibitors are now available for the prevention of venous thromboembol...
PMC10481892
core_pubmed_pmc
Comparability strategy and demonstration for post-approval production cell line change of a bevacizumab biosimilar IBI305
Comparability strategy and demonstration for post-approval production cell line change of a bevacizumab biosimilar IBI305 Abstract Abstract High-producing cell line could improve the affordability and availability of biotherapeutic products. A post-approval production cell line change, low-titer CHO-K1S to high-titer C...
PMC5107195
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Follicle-Stimulating Hormone in Healthy Women Receiving Single and Multiple Doses of Highly Purified Human Menotrophin and Urofollitrophin
Pharmacokinetics and Pharmacodynamics of Follicle-Stimulating Hormone in Healthy Women Receiving Single and Multiple Doses of Highly Purified Human Menotrophin and Urofollitrophin Abstract Abstract Background and Objective Highly purified human menotrophin and urofollitrophin preparations obtained from human urine via ...
PMC8606893
core_pubmed_pmc
Optimization of Initial Dose Regimen for Sirolimus in Pediatric Patients With Lymphangioma
Optimization of Initial Dose Regimen for Sirolimus in Pediatric Patients With Lymphangioma Abstract Sirolimus is an effective oral treatment for pediatric patients with lymphangioma. The present clinical study in 15 children (0.12–16.39 years of age) examines the effects of underlying factors on sirolimus concentration...
PMC11739741
core_pubmed_pmc
Effects of GLPG3970 on Sulfasalazine and Methotrexate Pharmacokinetics in Healthy Adults: Two Open‐Label, Phase I, Drug–Drug Interaction Studies
Effects of GLPG3970 on Sulfasalazine and Methotrexate Pharmacokinetics in Healthy Adults: Two Open‐Label, Phase I, Drug–Drug Interaction Studies Abstract Abstract GLPG3970 is a selective salt‐inducible kinase 2/3 inhibitor intended for the treatment of inflammatory diseases. In vitro studies suggest GLPG3970 strongly i...
PMC7510565
core_pubmed_pmc
Pharmacodynamic effects of the K + binder patiromer in a novel chronic hyperkalemia model in spontaneously hypertensive rats
Pharmacodynamic effects of the K + binder patiromer in a novel chronic hyperkalemia model in spontaneously hypertensive rats Abstract Abstract Currently described hyperkalemia (HK) animal models are typically acute and cause significant distress and mortality to the animals, warranting new approaches for studying chron...
PMC9174400
core_pubmed_pmc
Bioequivalence Studies of New Generic Formulations of Vildagliptin and Fixed-Drug Combination of Vildagliptin and Metformin Versus Respective Originator Products in Healthy Volunteers
Bioequivalence Studies of New Generic Formulations of Vildagliptin and Fixed-Drug Combination of Vildagliptin and Metformin Versus Respective Originator Products in Healthy Volunteers Abstract Introduction Vildagliptin and metformin are two well-established oral antidiabetics with a complementary mechanism of action. T...
PMC8313639
core_pubmed_pmc
Novel ways to monitor immunosuppression in pediatric kidney transplant recipients—underlying concepts and emerging data
Novel ways to monitor immunosuppression in pediatric kidney transplant recipients—underlying concepts and emerging data Abstract Abstract After pediatric kidney transplantation, immunosuppressive therapy is given to avoid acute and chronic rejections. However, the immunosuppression causes an increased risk of severe vi...
PMC11883507
core_pubmed_pmc
Mucositis Pain and Its Temporal Relationship to White Cell Count
Mucositis Pain and Its Temporal Relationship to White Cell Count Abstract ABSTRACT Background Children who have received chemotherapy and/or radiotherapy treatment resulting in neutropenia can suffer painful mucositis. We explored the relationship between pain score and white cell count in children with mucositis due t...
PMC11705542
core_pubmed_pmc
Non-linear oral bioavailability and clinical pharmacokinetics of high-dose Andrographis paniculata ethanolic extract: relevant dosage implications for COVID-19 treatment
Non-linear oral bioavailability and clinical pharmacokinetics of high-dose Andrographis paniculata ethanolic extract: relevant dosage implications for COVID-19 treatment Abstract Abstract Aim Insufficient quality control and limited dissolution of Andrographis paniculata extract capsules restricts their bioavailability...
PMC11635514
core_pubmed_pmc
Analyzing the Effect of Resveratrol on Pharmacokinetics of Antituberculosis Drug Bedaquiline in Rats by a Novel UPLC-MS/MS Approach
Analyzing the Effect of Resveratrol on Pharmacokinetics of Antituberculosis Drug Bedaquiline in Rats by a Novel UPLC-MS/MS Approach Abstract Abstract Bedaquiline (BDQ), a diarylquinoline compound, is an inhibitor of mycobacterial ATP synthase, specifically with FDA approval as a treatment for multidrug-resistant tuberc...
PMC4168221
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Profiles of Canagliflozin in Japanese Patients with Type 2 Diabetes Mellitus and Moderate Renal Impairment
Pharmacokinetic and Pharmacodynamic Profiles of Canagliflozin in Japanese Patients with Type 2 Diabetes Mellitus and Moderate Renal Impairment Abstract Abstract Background and Objectives This study examined the effects of moderate renal impairment on the pharmacokinetics and pharmacodynamics of canagliflozin in Japanes...
PMC7181550
core_pubmed_pmc
A Three-Part, Randomised Study to Investigate the Safety, Tolerability, Pharmacokinetics and Mode of Action of BC 007, Neutraliser of Pathogenic Autoantibodies Against G-Protein Coupled Receptors in Healthy, Young and Elderly Subjects
A Three-Part, Randomised Study to Investigate the Safety, Tolerability, Pharmacokinetics and Mode of Action of BC 007, Neutraliser of Pathogenic Autoantibodies Against G-Protein Coupled Receptors in Healthy, Young and Elderly Subjects Abstract Background and Objective BC 007 is a substance with a novel and innovative m...
PMC11399637
core_pubmed_pmc
Pharmacokinetic modeling of sulfamethoxazole-trimethoprim and sulfadiazine-trimethoprim combinations in broilers
Pharmacokinetic modeling of sulfamethoxazole-trimethoprim and sulfadiazine-trimethoprim combinations in broilers Abstract Sulfonamides ( S ) are old bacteriostatic antibiotics which are widely prescribed in combination with trimethoprim ( TMP ) for the treatment of various diseases in food-producing animals such as pou...
PMC7442270
core_pubmed_pmc
Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide Acetate Treatment for Central Precocious Puberty
Phase 3 Trial of a Small-volume Subcutaneous 6-Month Duration Leuprolide Acetate Treatment for Central Precocious Puberty Abstract Abstract Context Gonadotropin-releasing hormone agonists (GnRHas) are standard of care for central precocious puberty (CPP). A 6-month subcutaneous injection has recently been approved by t...
PMC9124358
core_pubmed_pmc
Exposure–response analysis of adverse events associated with molibresib and its active metabolites in patients with solid tumors
Exposure–response analysis of adverse events associated with molibresib and its active metabolites in patients with solid tumors Abstract Abstract Molibresib (GSK525762) is an investigational orally bioavailable small‐molecule bromodomain and extraterminal (BET) protein inhibitor for the treatment of advanced solid tum...
PMC3403474
core_pubmed_pmc
Factors Important to the Prioritization and Development of Successful Topical Microbicides for HIV-1
Factors Important to the Prioritization and Development of Successful Topical Microbicides for HIV-1 Abstract Significant advancements in topical microbicide development have occurred since the prevention strategy was first described as a means to inhibit the sexual transmission of HIV-1. The lack of clinical efficacy ...
PMC9387934
core_pubmed_pmc
Randomized single oral dose phase 1 study of safety, tolerability, and pharmacokinetics of Iminosugar UV-4 Hydrochloride (UV-4B) in healthy subjects
Randomized single oral dose phase 1 study of safety, tolerability, and pharmacokinetics of Iminosugar UV-4 Hydrochloride (UV-4B) in healthy subjects Abstract Background UV-4 ( N -(9’-methoxynonyl)-1-deoxynojirimycin, also called M O N-DNJ) is an iminosugar small-molecule oral drug candidate with in vitro antiviral acti...
PMC10398811
core_pubmed_pmc
Nivolumab with or without ipilimumab in pediatric patients with high-grade CNS malignancies: Safety, efficacy, biomarker, and pharmacokinetics—CheckMate 908
Nivolumab with or without ipilimumab in pediatric patients with high-grade CNS malignancies: Safety, efficacy, biomarker, and pharmacokinetics—CheckMate 908 Abstract Abstract Background Therapeutic options are limited in pediatric CNS malignancies. CheckMate 908 ( NCT03130959 ) is an open-label, sequential-arm, phase 1...
PMC6310871
core_pubmed_pmc
A Systematic Evaluation of Effect of Adherence Patterns on the Sample Size and Power of a Clinical Study
A Systematic Evaluation of Effect of Adherence Patterns on the Sample Size and Power of a Clinical Study Abstract Abstract The objective of our study was to evaluate the effect of adherence patterns on the sample size and power of a clinical trial. Simulations from a population pharmacokinetic/pharmacodynamic (PK/PD) m...
PMC8837505
core_pubmed_pmc
Two heads are better than one: current landscape of integrating QSP and machine learning
Two heads are better than one: current landscape of integrating QSP and machine learning Abstract Quantitative systems pharmacology (QSP) modeling is applied to address essential questions in drug development, such as the mechanism of action of a therapeutic agent and the progression of disease. Meanwhile, machine lear...
PMC6470842
core_pubmed_pmc
Physiologically-Based Pharmacokinetic Modeling for Drug-Drug Interactions of Procainamide and N -Acetylprocainamide with Cimetidine, an Inhibitor of rOCT2 and rMATE1, in Rats
Physiologically-Based Pharmacokinetic Modeling for Drug-Drug Interactions of Procainamide and N -Acetylprocainamide with Cimetidine, an Inhibitor of rOCT2 and rMATE1, in Rats Abstract Previous observations demonstrated that cimetidine decreased the clearance of procainamide (PA) and/or N -acetylprocainamide (NAPA; the ...
PMC9169874
core_pubmed_pmc
Sex Differences in Blood–Brain Barrier Transport of Psychotropic Drugs
Sex Differences in Blood–Brain Barrier Transport of Psychotropic Drugs Abstract Abstract Treatment of neuropsychiatric disorders relies on the effective delivery of therapeutic molecules to the target organ, the brain. The blood–brain barrier (BBB) hinders such delivery and proteins acting as transporters actively regu...
PMC9931437
core_pubmed_pmc
Semimechanistic modeling of copeptin and aldosterone kinetics and dynamics in response to rehydration treatment for diabetic ketoacidosis in children
Semimechanistic modeling of copeptin and aldosterone kinetics and dynamics in response to rehydration treatment for diabetic ketoacidosis in children Abstract Abstract Diabetic ketoacidosis (DKA), a frequent complication of type 1 diabetes (T1D), is characterized by hyperosmolar hypovolemia. The response of water‐regul...
PMC11098153
core_pubmed_pmc
Covariate modeling in pharmacometrics: General points for consideration
Covariate modeling in pharmacometrics: General points for consideration Abstract Abstract Modeling the relationships between covariates and pharmacometric model parameters is a central feature of pharmacometric analyses. The information obtained from covariate modeling may be used for dose selection, dose individualiza...
PMC12823303
core_pubmed_pmc
Exposure–Response Modeling of Monthly Migraine Days for Efficacy of Atogepant in Patients With Episodic or Chronic Migraine
Exposure–Response Modeling of Monthly Migraine Days for Efficacy of Atogepant in Patients With Episodic or Chronic Migraine Abstract ABSTRACT This work aimed to develop an appropriate model to evaluate the exposure–response relationship (ERR) for monthly migraine days (MMD) in atogepant's key migraine prevention clinic...
PMC10824694
core_pubmed_pmc
Pharmacological profiling of a berbamine derivative for lymphoma treatment
Pharmacological profiling of a berbamine derivative for lymphoma treatment Abstract Key Points • PA4 is a potent CAMKIIγ inhibitor. • In vivo efficacy, pharmacokinetic, and toxicity assays suggest that PA4 is a candidate for future drug development. Abstract Ca 2+ /calmodulin-dependent protein kinase II γ (CAMKIIγ) has...
PMC11644310
core_pubmed_pmc
Improve Solubility and Develop Personalized Itraconazole Dosages via Forming Amorphous Solid Dispersions with Hydrophilic Polymers Utilizing HME and 3D Printing Technologies
Improve Solubility and Develop Personalized Itraconazole Dosages via Forming Amorphous Solid Dispersions with Hydrophilic Polymers Utilizing HME and 3D Printing Technologies Abstract Itraconazole (ITZ), a broad-spectrum triazole antifungal agent, exhibits remarkable pharmacodynamic and pharmacokinetic properties. Howev...
PMC11473376
core_pubmed_pmc
Hierarchical deep compartment modeling: A workflow to leverage machine learning and Bayesian inference for hierarchical pharmacometric modeling
Hierarchical deep compartment modeling: A workflow to leverage machine learning and Bayesian inference for hierarchical pharmacometric modeling Abstract Abstract Population pharmacokinetic (PK) modeling serves as the cornerstone for understanding drug behavior within a specific population. It integrates subject covaria...
PMC12287013
core_pubmed_pmc
Adverse effects of antiseizure medications: a review of the impact of pharmacogenetics and drugs interactions in clinical practice
Adverse effects of antiseizure medications: a review of the impact of pharmacogenetics and drugs interactions in clinical practice Abstract Abstract Epilepsy is a chronic and debilitating neurological disorder characterized by the occurrence of spontaneous and recurrent seizures. Despite the availability of several ant...
PMC11993961
core_pubmed_pmc
A phase I/II trial evaluating the safety of increased-dose S- 1 with oxaliplatin and nivolumab in HER2-negative advanced gastric cancer
A phase I/II trial evaluating the safety of increased-dose S- 1 with oxaliplatin and nivolumab in HER2-negative advanced gastric cancer Abstract Abstract Background We developed and refined an S-1 dosage formula based on renal function, sex, and body surface area (BSA) to achieve the target area under the concentration...
PMC5846071
core_pubmed_pmc
Strategies for clinical development of monoclonal antibodies beyond first-in-human trials: tested doses and rationale for dose selection
Strategies for clinical development of monoclonal antibodies beyond first-in-human trials: tested doses and rationale for dose selection Abstract Background: Our previous survey on first-in-human trials (FIHT) of monoclonal antibodies (mAbs) showed that, due to their limited toxicity, the recommended phase II dose (RP2...
PMC9124111
core_pubmed_pmc
Biological and Immune Responses to Current Anti-SARS-CoV-2 mRNA Vaccines beyond Anti-Spike Antibody Production
Biological and Immune Responses to Current Anti-SARS-CoV-2 mRNA Vaccines beyond Anti-Spike Antibody Production Abstract Several vaccine strategies are now available to fight the current SARS-CoV-2 pandemic. Those based on the administration of lipid-complexed messenger(m)RNA molecules represent the last frontiers in te...
PMC3505375
core_pubmed_pmc
A Single-Dose Study of Denosumab in Patients With Various Degrees of Renal Impairment
A Single-Dose Study of Denosumab in Patients With Various Degrees of Renal Impairment Abstract This 16-week study evaluated pharmacokinetics and pharmacodynamics of denosumab in 55 subjects with renal function ranging from normal to dialysis-dependent kidney failure. Participants received a single 60-mg subcutaneous do...
PMC12178318
core_pubmed_pmc
First‐in‐human phase 1 study of KHK2455 monotherapy and in combination with mogamulizumab in patients with advanced solid tumors
First‐in‐human phase 1 study of KHK2455 monotherapy and in combination with mogamulizumab in patients with advanced solid tumors Abstract Abstract Background Indoleamine 2,3‐dioxygenase 1 (IDO1) is a heme‐containing enzyme that degrades tryptophan (Trp) to kynurenine (Kyn), which suppresses effector T cells and reduces...
PMC11880188
core_pubmed_pmc
Pharmacokinetics of Nivolumab and Erythropoietin in a Rat Model of Diet-Induced Obesity
Pharmacokinetics of Nivolumab and Erythropoietin in a Rat Model of Diet-Induced Obesity Abstract Purpose To investigate how obesity affects the pharmacokinetics of biologics in a rat model. Method Male Long-Evans rats were fed a high-fat diet from the age of 3 weeks and development of obesity was monitored by measuring...
PMC12920379
core_pubmed_pmc
A true theranostic pair – 44/47 Sc-labeled GRPR antagonist shows great promise for managing prostate and breast cancer
A true theranostic pair – 44/47 Sc-labeled GRPR antagonist shows great promise for managing prostate and breast cancer Abstract Purpose This study investigates the theranostic potential of a 44/47 Sc-labeled antagonist targeting the gastrin-releasing peptide receptor (GRPR) in prostate and breast tumors. Methods A stat...
PMC3907542
core_pubmed_pmc
Contribution of Baicalin on the Plasma Protein Binding Displacement and CYP3A Activity Inhibition to the Pharmacokinetic Changes of Nifedipine in Rats In Vivo and In Vitro
Contribution of Baicalin on the Plasma Protein Binding Displacement and CYP3A Activity Inhibition to the Pharmacokinetic Changes of Nifedipine in Rats In Vivo and In Vitro Abstract Abstract Baicalin purified from the root of Radix scutellariae is widely used in clinical practices. This study aimed to evaluate the effec...
PMC10182447
core_pubmed_pmc
Mode of binding, kinetic and thermodynamic properties of a lipid-like drug (Fingolimod) interacting with Human Serum Albumin
Mode of binding, kinetic and thermodynamic properties of a lipid-like drug (Fingolimod) interacting with Human Serum Albumin Abstract Introduction: Fingolimod is a drug that is used to treat multiple sclerosis (MS). It has pH-dependent solubility and low solubility when buffering agents are present. Multi-spectroscopic...
PMC3895290
core_pubmed_pmc
Buparvaquone loaded solid lipid nanoparticles for targeted delivery in theleriosis
Buparvaquone loaded solid lipid nanoparticles for targeted delivery in theleriosis Abstract Abstract Background: Buparvaquone (BPQ), a hydroxynaphthoquinone derivative, has been investigated for the treatment of many infections and is recommended as the gold standard for the treatment of theileriosis. Theileriosis, an ...
PMC6124477
core_pubmed_pmc
Asenapine pharmacokinetics and tolerability in a pediatric population
Asenapine pharmacokinetics and tolerability in a pediatric population Abstract Purpose This study aimed to characterize the pharmacokinetic (PK) properties, safety, and tolerability of asenapine, and to develop a population PK model in pediatric patients with schizophrenia, bipolar disorder, or other psychiatric disord...
PMC4906519
core_pubmed_pmc
Pharmacogenetics-Guided Phase I Study of Capecitabine on an Intermittent Schedule in Patients with Advanced or Metastatic Solid Tumours
Pharmacogenetics-Guided Phase I Study of Capecitabine on an Intermittent Schedule in Patients with Advanced or Metastatic Solid Tumours Abstract Abstract The FDA-approved starting dosage of capecitabine is 1,250 mg/m 2 , and market research indicates that U.S. physicians routinely prescribe 1,000 mg/m 2 . Retrospective...
PMC8079248
core_pubmed_pmc
A National Survey of Attitudes and Practices of Physicians Relating to Therapeutic Drug Monitoring and Clinical Pharmacokinetic Service: Strategies for Enhancing Patient’s Care in Saudi Arabia
A National Survey of Attitudes and Practices of Physicians Relating to Therapeutic Drug Monitoring and Clinical Pharmacokinetic Service: Strategies for Enhancing Patient’s Care in Saudi Arabia Abstract Purpose The aim of the study was to evaluate physicians’ perception of the concept of pharmacokinetics and therapeutic...
PMC7802642
core_pubmed_pmc
Study protocol of RESCUE-ALS: A Phase 2, r andomised, double-blind, placebo-controlled study in e arly s ymptomatic amyotrophic lateral sclerosis patients to assess bioenergetic c atalysis with CNM-A u 8 as a mechanism to slow diseas e progression
Study protocol of RESCUE-ALS: A Phase 2, r andomised, double-blind, placebo-controlled study in e arly s ymptomatic amyotrophic lateral sclerosis patients to assess bioenergetic c atalysis with CNM-A u 8 as a mechanism to slow diseas e progression Abstract Introduction Amyotrophic lateral sclerosis (ALS) is an adult-on...
PMC11005050
core_pubmed_pmc
MELLODDY: Cross-pharma Federated Learning at Unprecedented Scale Unlocks Benefits in QSAR without Compromising Proprietary Information
MELLODDY: Cross-pharma Federated Learning at Unprecedented Scale Unlocks Benefits in QSAR without Compromising Proprietary Information Abstract Abstract Federated multipartner machine learning has been touted as an appealing and efficient method to increase the effective training data volume and thereby the predictivit...
PMC6309143
core_pubmed_pmc
Association between genetic polymorphisms of CYP2C9 and VKORC1 and safety and efficacy of warfarin: Results of a 5 years audit
Association between genetic polymorphisms of CYP2C9 and VKORC1 and safety and efficacy of warfarin: Results of a 5 years audit Abstract Abstract Objective Genetic polymorphisms of CYP2C9 and VKORC1 play major role in pharmacokinetics and pharmacodynamics of warfarin, respectively. Purpose of our study was to assess the...
PMC8241047
core_pubmed_pmc
Atorvastatin-loaded micelles with bone-targeted ligand for the treatment of osteoporosis
Atorvastatin-loaded micelles with bone-targeted ligand for the treatment of osteoporosis Abstract Abstract Osteoporosis is a common bone disorder where the declined bone mass is far more than normal physiological status and usually associated with enhanced fracture risk, reduced bone strength and even deteriorated qual...
PMC9415049
core_pubmed_pmc
Health Benefits and Pharmacological Aspects of Chrysoeriol
Health Benefits and Pharmacological Aspects of Chrysoeriol Abstract A flavone, chrysoeriol is synthetized in several plant species. It comes from several natural sources, especially medicinal plants. The identification and isolation of this compound has been carried out and verified by several research teams using diff...
PMC8424225
core_pubmed_pmc
In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives
In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives Abstract Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs. However, construction of in vitro and in vivo correlations (IVIVCs) for LBFs ...
PMC9608191
core_pubmed_pmc
Development and Validation of a HPLC–MS/MS Method to Measure Nifuroxazide and Its Application in Healthy and Glioblastoma-Bearing Mice
Development and Validation of a HPLC–MS/MS Method to Measure Nifuroxazide and Its Application in Healthy and Glioblastoma-Bearing Mice Abstract Abstract Nifuroxazide (NAZ), a nitrofuran derivative used to treat diarrhea, has been recently shown to possess anticancer activity. However, its pharmacokinetic profile is poo...
PMC11366162
core_pubmed_pmc
High adsorption capacity of hemoperfusion on imipenem in critically ill patients with septic shock: a case report
High adsorption capacity of hemoperfusion on imipenem in critically ill patients with septic shock: a case report Abstract Abstract Background Sepsis is a life-threatening organ dysfunction caused by an excessive host response to infection, manifested by elevated levels of inflammatory cytokines. At present, the use of...
PMC3205122
core_pubmed_pmc
Phase I dose escalation safety study of nanoparticulate paclitaxel (CTI 52010) in normal dogs
Phase I dose escalation safety study of nanoparticulate paclitaxel (CTI 52010) in normal dogs Abstract Background Paclitaxel is highly effective in the treatment of many cancers in humans, but cannot be routinely used in dogs as currently formulated due to the exquisite sensitivity of this species to surfactant-solubil...
PMC7764481
core_pubmed_pmc
Chemotherapy and Targeted Agents in the Treatment of Elderly Patients with Metastatic Colorectal Cancer
Chemotherapy and Targeted Agents in the Treatment of Elderly Patients with Metastatic Colorectal Cancer Abstract Abstract Colorectal cancer (CRC) is one of the main causes of cancer death in the elderly. The older patients constitute a heterogeneous group in terms of functional status, comorbidities, and aging-related ...
PMC4168027
core_pubmed_pmc
Management of Non-Vitamin K Antagonist Oral Anticoagulants in the Perioperative Setting
Management of Non-Vitamin K Antagonist Oral Anticoagulants in the Perioperative Setting Abstract Abstract The field of oral anticoagulation has evolved with the arrival of non-vitamin K antagonist oral anticoagulants (NOACs) including an anti-IIa agent (dabigatran etexilate) and anti-Xa agents (rivaroxaban and apixaban...
PMC9780544
core_pubmed_pmc
A Phase 1 pharmacokinetic study of a single-dose bioadhesive clindamycin 2% gel for bacterial vaginosis
A Phase 1 pharmacokinetic study of a single-dose bioadhesive clindamycin 2% gel for bacterial vaginosis Abstract Abstract Objectives To evaluate pharmacokinetics (PK) of a single dose of an investigational 2% clindamycin phosphate vaginal gel in healthy women by assessment of plasma and vaginal clindamycin concentratio...
PMC12928122
core_pubmed_pmc
Population Pharmacokinetics of Vancomycin in Critically Ill Patients Undergoing Continuous Renal Replacement Therapy: Influence of Adsorptive Membranes
Population Pharmacokinetics of Vancomycin in Critically Ill Patients Undergoing Continuous Renal Replacement Therapy: Influence of Adsorptive Membranes Abstract ABSTRACT Vancomycin is commonly used to treat Staphylococcus aureus infections. In critically ill patients receiving continuous renal replacement therapy (CRRT...
PMC10912063
core_pubmed_pmc
Preclinical characterisation of gallium-68 labeled ferrichrome siderophore stereoisomers for PET imaging applications
Preclinical characterisation of gallium-68 labeled ferrichrome siderophore stereoisomers for PET imaging applications Abstract Background Siderophores are small iron-binding molecules produced by microorganisms to facilitate iron acquisition from the environment. Radiolabelled siderophores offer a promising solution fo...
PMC8485331
core_pubmed_pmc
Sorption of Neuropsychopharmaca in Microfluidic Materials for In Vitro Studies
Sorption of Neuropsychopharmaca in Microfluidic Materials for In Vitro Studies Abstract Abstract Sorption ( i.e. , adsorption and absorption) of small-molecule compounds to polydimethylsiloxane (PDMS) is a widely acknowledged phenomenon. However, studies to date have largely been conducted under atypical conditions for...
PMC9628577
core_pubmed_pmc
Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells
Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells Abstract SARS coronavirus 2 (SARS-CoV-2) has caused an ongoing global pandemic with significant mortality and morbidity. At this time, the only FDA-approved therapeutic for COVID-19 is remdesivir, a broad-spectrum antivi...
PMC11377867
core_pubmed_pmc
Phase I Study of Simlukafusp Alfa (FAP-IL2v) with or without Atezolizumab in Japanese Patients with Advanced Solid Tumors
Phase I Study of Simlukafusp Alfa (FAP-IL2v) with or without Atezolizumab in Japanese Patients with Advanced Solid Tumors Abstract Abstract Purpose: The aim of the study was to evaluate the safety/tolerability and pharmacokinetics of simlukafusp alfa (FAP-IL2v), an immunocytokine containing an anti-fibroblast activatio...
PMC4416384
core_pubmed_pmc
Population pharmacokinetic and pharmacodynamic modeling of transformed binary effect data of triflusal in healthy Korean male volunteers: a randomized, open-label, multiple dose, crossover study
Population pharmacokinetic and pharmacodynamic modeling of transformed binary effect data of triflusal in healthy Korean male volunteers: a randomized, open-label, multiple dose, crossover study Abstract Background Triflusal is a drug that inhibits platelet aggregation. In this study we investigated the dose-exposure-r...