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PMC8918144
core_pubmed_pmc
Biosimilar Pegfilgrastim-cbqv Demonstrated Similar Immunogenicity to Pegfilgrastim in Healthy Subjects Across Three Randomized Clinical Studies
Biosimilar Pegfilgrastim-cbqv Demonstrated Similar Immunogenicity to Pegfilgrastim in Healthy Subjects Across Three Randomized Clinical Studies Abstract Introduction Biologic therapeutics can trigger immune responses in patients. As part of the totality of evidence that is required for regulatory approval of biosimilar...
PMC8885761
core_pubmed_pmc
Optimization of supercritical-CO 2 extraction and pharmacokinetics in SD rats of alkaloids form Sophora moorcroftiana seed
Optimization of supercritical-CO 2 extraction and pharmacokinetics in SD rats of alkaloids form Sophora moorcroftiana seed Abstract The total alkaloids extracted from the seeds of Sophora moorcroftiana (TAs-SM) have the potential to treat alveolar echinococcosis, a disease included by the WHO in a list of 17 key neglec...
PMC10222456
core_pubmed_pmc
Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug–Drug Interactions between Elexacaftor/Tezacaftor/Ivacaftor and Tacrolimus in Lung Transplant Recipients
Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug–Drug Interactions between Elexacaftor/Tezacaftor/Ivacaftor and Tacrolimus in Lung Transplant Recipients Abstract Elexacaftor/tezacaftor/ivacaftor (ETI) treatment has potential benefits in lung transplant recipients, including improvements in ...
PMC7577018
core_pubmed_pmc
Novel Mechanistic PBPK Model to Predict Renal Clearance in Varying Stages of CKD by Incorporating Tubular Adaptation and Dynamic Passive Reabsorption
Novel Mechanistic PBPK Model to Predict Renal Clearance in Varying Stages of CKD by Incorporating Tubular Adaptation and Dynamic Passive Reabsorption Abstract Chronic kidney disease (CKD) has significant effects on renal clearance (CL r ) of drugs. Physiologically‐based pharmacokinetic (PBPK) models have been used to p...
PMC11998014
core_pubmed_pmc
Application of Machine Learning and Mechanistic Modeling to Predict Intravenous Pharmacokinetic Profiles in Humans
Application of Machine Learning and Mechanistic Modeling to Predict Intravenous Pharmacokinetic Profiles in Humans Abstract Accurate prediction of new compounds’ pharmacokinetic (PK) profile in humans is crucial for drug discovery. Traditional methods, including allometric scaling and mechanistic modeling, rely on para...
PMC11990089
core_pubmed_pmc
Determination and Disposition of the Aromatase Inhibitor Exemestane in CYP3A-Deficient Mice
Determination and Disposition of the Aromatase Inhibitor Exemestane in CYP3A-Deficient Mice Abstract Abstract Exemestane, a steroidal aromatase inhibitor prescribed for post-menopausal women with estrogen receptor-positive breast cancer, is associated with debilitating musculoskeletal side effects and exhibits consider...
PMC10088084
core_pubmed_pmc
N,N‐dimethyltryptamine affects electroencephalography response in a concentration‐dependent manner—A pharmacokinetic/pharmacodynamic analysis
N,N‐dimethyltryptamine affects electroencephalography response in a concentration‐dependent manner—A pharmacokinetic/pharmacodynamic analysis Abstract Abstract N,N‐dimethyltryptamine (DMT) is a psychedelic substance and is being used as a research tool in investigations of the neurobiology behind the human consciousnes...
PMC9434437
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Etrolizumab in Children With Moderately to Severely Active Ulcerative Colitis or Crohn’s Disease: Results from a Phase 1 Randomized Trial
Pharmacokinetics, Pharmacodynamics, and Safety of Etrolizumab in Children With Moderately to Severely Active Ulcerative Colitis or Crohn’s Disease: Results from a Phase 1 Randomized Trial Abstract Abstract Background Etrolizumab, a humanized anti-β7 antibody, has not been studied in children. Here, we evaluate the phar...
PMC11993836
core_pubmed_pmc
Pharmacokinetics and safety of topical fluralaner in koalas (Phascolarctos cinereus )
Pharmacokinetics and safety of topical fluralaner in koalas (Phascolarctos cinereus ) Abstract Abstract Sarcoptic mange (etiological agent Sarcoptes scabiei ) is among the most important parasitic diseases of some marsupial species and has been an emerging disease of koalas, causing welfare and conservation implication...
PMC12888887
core_pubmed_pmc
Preclinical pharmacokinetics/pharmacodynamics studies defining the role of ethambutol in Mycobacterium kansasii lung disease
Preclinical pharmacokinetics/pharmacodynamics studies defining the role of ethambutol in Mycobacterium kansasii lung disease Abstract ABSTRACT Rifampin, isoniazid, and ethambutol are the backbone of the regimen used to treat Mycobacterium kansasii- complex (MKC) lung disease. However, ethambutol pharmacokinetics/pharma...
PMC9996548
core_pubmed_pmc
A phase IV study evaluating QT interval, pharmacokinetics, and safety following fractionated dosing of gemtuzumab ozogamicin in patients with relapsed/refractory CD33-positive acute myeloid leukemia
A phase IV study evaluating QT interval, pharmacokinetics, and safety following fractionated dosing of gemtuzumab ozogamicin in patients with relapsed/refractory CD33-positive acute myeloid leukemia Abstract Abstract Purpose Gemtuzumab ozogamicin (GO) is indicated for treatment of relapsed/refractory (R/R) acute myeloi...
PMC10311440
core_pubmed_pmc
A model-based head-to-head comparison of single-agent lurbinectedin in the pivotal ATLANTIS Study
A model-based head-to-head comparison of single-agent lurbinectedin in the pivotal ATLANTIS Study Abstract Abstract Introduction Lurbinectedin is a selective inhibitor of oncogenic transcription U.S. Food and Drug Administration (FDA)-approved for patients with relapsed small cell lung cancer (SCLC) as monotherapy at 3...
PMC7983888
core_pubmed_pmc
Clinical and Model‐Based Evaluation of the Effect of Glasdegib on Cardiac Repolarization From a Randomized Thorough QT Study
Clinical and Model‐Based Evaluation of the Effect of Glasdegib on Cardiac Repolarization From a Randomized Thorough QT Study Abstract Abstract Glasdegib is a potent, selective oral inhibitor of the Hedgehog signaling pathway. This phase 1 double‐blind thorough QT study ( NCT03162900 ) evaluated the effects of glasdegib...
PMC7720366
core_pubmed_pmc
In silico study of thymohydroquinone interaction with blood–brain barrier disrupting proteins
In silico study of thymohydroquinone interaction with blood–brain barrier disrupting proteins Abstract Abstract Aim: To evaluate the inhibitory interaction of thymohydroquinone against blood–brain barrier (BBB)-associated neuropsychiatric and neurodegenerative disorders. Materials & methods: An elaborated in silico stu...
PMC11597066
core_pubmed_pmc
Species Differences in Ezetimibe Glucuronidation
Species Differences in Ezetimibe Glucuronidation Abstract Background: Peclinical and clinical studies have revealed that ezetimibe, an approved cholesterol-absorption inhibitor, is rapidly and extensively metabolized to a more potent metabolite, ezetimibe glucuronide. Since different species are commonly used in the ph...
PMC11994961
core_pubmed_pmc
In Vivo pharmacokinetic interactions of ribociclib with rivaroxaban and apixaban in rats: implications for increased drug exposure and dose adjustments
In Vivo pharmacokinetic interactions of ribociclib with rivaroxaban and apixaban in rats: implications for increased drug exposure and dose adjustments Abstract Background Apixaban (API) and rivaroxaban (RIVA) are orally available inhibitors of coagulation factor Xa and are commonly used to treat cancer-related venous ...
PMC12814313
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effect of Bexicaserin in Healthy Participants: A First‐in‐Human Randomized, Double‐Blind, Placebo‐Controlled Single Ascending Dose Escalation Phase 1 Study
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effect of Bexicaserin in Healthy Participants: A First‐in‐Human Randomized, Double‐Blind, Placebo‐Controlled Single Ascending Dose Escalation Phase 1 Study Abstract Abstract Bexicaserin (LP352) is a selective 5‐hydroxytryptamine 2C (5‐HT 2C ) superagoni...
PMC11490238
core_pubmed_pmc
Prediction of Pharmacokinetic Drug–Drug Interactions Involving Anlotinib as a Victim by Using Physiologically Based Pharmacokinetic Modeling
Prediction of Pharmacokinetic Drug–Drug Interactions Involving Anlotinib as a Victim by Using Physiologically Based Pharmacokinetic Modeling Abstract Background Anlotinib was approved as a third line therapy for advanced non-small cell lung cancer in China. However, the impact of concurrent administration of various cl...
PMC11449957
core_pubmed_pmc
Identification of mycobacterial Thymidylate kinase inhibitors: a comprehensive pharmacophore, machine learning, molecular docking, and molecular dynamics simulation studies
Identification of mycobacterial Thymidylate kinase inhibitors: a comprehensive pharmacophore, machine learning, molecular docking, and molecular dynamics simulation studies Abstract Abstract Thymidylate kinase (TMK) is a pivotal enzyme in Mycobacterium tuberculosis (Mtb), crucial for phosphorylating thymidine monophosp...
PMC6377964
core_pubmed_pmc
Evidence on Integrating Pharmacokinetics to Find Truly Therapeutic Agent for Alzheimer's Disease: Comparative Pharmacokinetics and Disposition Kinetics Profiles of Stereoisomers Isorhynchophylline and Rhynchophylline in Rats
Evidence on Integrating Pharmacokinetics to Find Truly Therapeutic Agent for Alzheimer's Disease: Comparative Pharmacokinetics and Disposition Kinetics Profiles of Stereoisomers Isorhynchophylline and Rhynchophylline in Rats Abstract Isorhynchophylline (IRN) and rhynchophylline (RN), a pair of stereoisomers, are tetrac...
PMC4823318
core_pubmed_pmc
Effects of Age, Sex, and Race on the Safety and Pharmacokinetics of Single and Multiple Doses of Azilsartan Medoxomil in Healthy Subjects
Effects of Age, Sex, and Race on the Safety and Pharmacokinetics of Single and Multiple Doses of Azilsartan Medoxomil in Healthy Subjects Abstract Background and Objective Azilsartan medoxomil (AZL-M) is an angiotensin II receptor blocker approved to treat hypertension. After oral dosing, AZL-M is quickly hydrolyzed to...
PMC8134639
core_pubmed_pmc
A bispecific antibody agonist of the IL-2 heterodimeric receptor preferentially promotes in vivo expansion of CD8 and NK cells
A bispecific antibody agonist of the IL-2 heterodimeric receptor preferentially promotes in vivo expansion of CD8 and NK cells Abstract The use of recombinant interleukin-2 (IL-2) as a therapeutic protein has been limited by significant toxicities despite its demonstrated ability to induce durable tumor-regression in c...
PMC7506135
core_pubmed_pmc
Comparative Pharmacokinetics of Meloxicam Between Healthy Post-partum vs. Mid-lactation Dairy Cattle
Comparative Pharmacokinetics of Meloxicam Between Healthy Post-partum vs. Mid-lactation Dairy Cattle Abstract Lactating dairy cattle are at risk for various painful conditions throughout their life, such as lameness, parturition, mastitis, and metabolic disorders. These conditions necessitate adequate methods of analge...
PMC10624750
core_pubmed_pmc
Comparison of In Vitro Corneal Permeation and In Vivo Ocular Bioavailability in Rabbits of Three Marketed Latanoprost Formulations
Comparison of In Vitro Corneal Permeation and In Vivo Ocular Bioavailability in Rabbits of Three Marketed Latanoprost Formulations Abstract Abstract Background and Objective All latanoprost formulations currently available for the treatment of glaucoma or ocular hypertension contain the same concentration of latanopros...
PMC12290309
core_pubmed_pmc
Albiflorin on Neuropsychiatric and Neurodegenerative Disorders: A Systematic Review
Albiflorin on Neuropsychiatric and Neurodegenerative Disorders: A Systematic Review Abstract ABSTRACT Aims Albiflorin, a key compound from Paeonia lactiflora , has shown therapeutic potential in neuropsychiatric and neurodegenerative disorders (NPDs and NDDs), especially depression and Alzheimer's disease (AD). This re...
PMC6182932
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics and Pharmacogenetics of Tacrolimus in Kidney Transplantation
Pharmacokinetics, Pharmacodynamics and Pharmacogenetics of Tacrolimus in Kidney Transplantation Abstract Background: Tacrolimus (Tac, or FK506), a calcineurin inhibitor (CNI), is the first-line immu-nosuppressant which consists of the footstone as immunosuppressive regimens in kidney transplantation. However, the drug ...
PMC3116006
core_pubmed_pmc
Clinical, Pharmacokinetic, and Pharmacogenetic Determinants of Clopidogrel Resistance in Korean Patients with Acute Coronary Syndrome
Clinical, Pharmacokinetic, and Pharmacogenetic Determinants of Clopidogrel Resistance in Korean Patients with Acute Coronary Syndrome Abstract Abstract Background Clopidogrel has been widely used to prevent recurrent ischemia in patients with acute coronary syndrome (ACS). However, inter-individual variability in respo...
PMC12222399
core_pubmed_pmc
Improved FAPI-radiopharmaceutical pharmacokinetics from the perspectives of a dose escalation study
Improved FAPI-radiopharmaceutical pharmacokinetics from the perspectives of a dose escalation study Abstract Abstract Purpose This study explores the use of fibroblast activation protein inhibitors (FAPI) targeting radiopharmaceuticals as a new approach for pan-cancer treatment, focusing on key factors affecting their ...
PMC3639233
core_pubmed_pmc
Dynamical modeling of drug effect using hybrid systems
Dynamical modeling of drug effect using hybrid systems Abstract Drug discovery today is a complex, expensive, and time-consuming process with high attrition rate. A more systematic approach is needed to combine innovative approaches in order to lead to more effective and efficient drug development. This article provide...
PMC11272695
core_pubmed_pmc
Systematic evaluation of high-throughput PBK modelling strategies for the prediction of intravenous and oral pharmacokinetics in humans
Systematic evaluation of high-throughput PBK modelling strategies for the prediction of intravenous and oral pharmacokinetics in humans Abstract Physiologically based kinetic (PBK) modelling offers a mechanistic basis for predicting the pharmaco-/toxicokinetics of compounds and thereby provides critical information for...
PMC6790709
core_pubmed_pmc
Alternative Magnesium Sulfate Dosing Regimens for Women With Preeclampsia: A Population Pharmacokinetic Exposure‐Response Modeling and Simulation Study
Alternative Magnesium Sulfate Dosing Regimens for Women With Preeclampsia: A Population Pharmacokinetic Exposure‐Response Modeling and Simulation Study Abstract Abstract Magnesium sulfate is the anticonvulsant of choice for eclampsia prophylaxis and treatment; however, the recommended dosing regimens are costly and cum...
PMC10771556
core_pubmed_pmc
PEGylated therapeutics in the clinic
PEGylated therapeutics in the clinic Abstract Abstract The covalent attachment of polyethylene glycol (PEG) to therapeutic agents, termed PEGylation, is a well‐established and clinically proven drug delivery approach to improve the pharmacokinetics and pharmacodynamics of drugs. Specifically, PEGylation can improve the...
PMC4445693
core_pubmed_pmc
Pharmacokinetics and skin-tissue penetration of daptomycin in rats
Pharmacokinetics and skin-tissue penetration of daptomycin in rats Abstract Background Daptomycin is recommended for complicated skin and skin-structure infections. However, information on the penetration of daptomycin into skin is limited. Therefore, the aim of this in vivo investigation was to determine the pharmacok...
PMC4675819
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic study of triptolide-loaded liposome hydrogel patch under microneedles on rats with collagen-induced arthritis
Pharmacokinetic and pharmacodynamic study of triptolide-loaded liposome hydrogel patch under microneedles on rats with collagen-induced arthritis Abstract Triptolide (TP), a major active component of Tripterygium wilfordii Hook.F. (TWHF), is used to treat rheumatoid arthritis (RA). However, it has a narrow therapeutic ...
PMC3901587
core_pubmed_pmc
Disposition of Erlotinib and Its Metabolite OSI420 in a Patient with High Bilirubin Levels
Disposition of Erlotinib and Its Metabolite OSI420 in a Patient with High Bilirubin Levels Abstract Abstract Erlotinib is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for the treatment of non-small cell lung cancer and when combined with gemcitabine for pancreatic cancer. Dose redu...
PMC9085669
core_pubmed_pmc
Detecting Validated Intracellular ROS Generation with 18 F-dihydroethidine-Based PET
Detecting Validated Intracellular ROS Generation with 18 F-dihydroethidine-Based PET Abstract Abstract Purpose To determine the sensitivity of the 18 F-radiolabelled dihydroethidine analogue ([ 18 F]DHE) to ROS in a validated ex vivo model of tissue oxidative stress. Procedures The sensitivity of [ 18 F]DHE to various ...
PMC10672071
core_pubmed_pmc
Drug–Drug Interactions Involving Dexamethasone in Clinical Practice: Myth or Reality?
Drug–Drug Interactions Involving Dexamethasone in Clinical Practice: Myth or Reality? Abstract Abstract Concomitant administration of multiple drugs frequently causes severe pharmacokinetic or pharmacodynamic drug–drug interactions (DDIs) resulting in the possibility of enhanced toxicity and/or treatment failure. The a...
PMC9609824
core_pubmed_pmc
Pharmacokinetic Herb-Drug Interactions of Glipizide with Andrographis paniculata (Burm. f.) and Andrographolide in Normal and Diabetic Rats by Validated HPLC Method
Pharmacokinetic Herb-Drug Interactions of Glipizide with Andrographis paniculata (Burm. f.) and Andrographolide in Normal and Diabetic Rats by Validated HPLC Method Abstract Co-administered medicinal herbs can modify a drug’s pharmacokinetics (PK), effectiveness, and toxicity. Andrographis paniculata (Burm. f.) ethanol...
PMC8402031
core_pubmed_pmc
No Time Dependence of Ciprofloxacin Pharmacokinetics in Critically Ill Adults: Comparison of Individual and Population Analyses
No Time Dependence of Ciprofloxacin Pharmacokinetics in Critically Ill Adults: Comparison of Individual and Population Analyses Abstract Abstract The aim of this prospective PK study was to evaluate the pharmacokinetics of ciprofloxacin dosed within the first 36 h (early phase) and after 3 days of treatment (delayed ph...
PMC9263537
core_pubmed_pmc
Population pharmacokinetic of paracetamol and atorvastatin with co‐administration of semaglutide
Population pharmacokinetic of paracetamol and atorvastatin with co‐administration of semaglutide Abstract Abstract Semaglutide is a glucagon‐like‐peptide‐1 (GLP‐1) analogue marketed for once‐weekly subcutaneous administration for type 2 diabetes mellitus. Like other long‐acting GLP‐1 analogues, semaglutide reduces gast...
PMC8953841
core_pubmed_pmc
Orally Administered, Biodegradable and Biocompatible Hydroxypropyl–β–Cyclodextrin Grafted Poly(methacrylic acid) Hydrogel for pH Sensitive Sustained Anticancer Drug Delivery
Orally Administered, Biodegradable and Biocompatible Hydroxypropyl–β–Cyclodextrin Grafted Poly(methacrylic acid) Hydrogel for pH Sensitive Sustained Anticancer Drug Delivery Abstract Abstract In the current study, a pH sensitive intelligent hydroxypropyl–β–cyclodextrin-based polymeric network (HP-β-CD-g-MAA) was develo...
PMC5014782
core_pubmed_pmc
Population Pharmacokinetics and Exposure–Response (Efficacy and Safety/Tolerability) of Empagliflozin in Patients with Type 2 Diabetes
Population Pharmacokinetics and Exposure–Response (Efficacy and Safety/Tolerability) of Empagliflozin in Patients with Type 2 Diabetes Abstract Abstract Introduction The aim of the analysis was to characterize the population pharmacokinetics (PKs) and exposure–response (E–R) for efficacy (fasting plasma glucose, glycat...
PMC12558857
core_pubmed_pmc
Syzygium aromaticum (clove buds) as a natural antibacterial agent: a promising alternative to combat multidrug-resistant bacteria
Syzygium aromaticum (clove buds) as a natural antibacterial agent: a promising alternative to combat multidrug-resistant bacteria Abstract Abstract Antibiotic resistance is a critical threat to modern medicine, necessitating new strategies against multi-drug resistant bacteria (MDR). This narrative review evaluates the...
PMC4869351
core_pubmed_pmc
The pharmacokinetics of mianserin suppositories for rectal administration in dogs and healthy volunteers: a pilot study
The pharmacokinetics of mianserin suppositories for rectal administration in dogs and healthy volunteers: a pilot study Abstract Abstract Background We formulated mianserin suppositories for the treatment of delirium and evaluated their pharmacokinetics by measuring plasma drug concentrations in dogs and healthy human ...
PMC10746103
core_pubmed_pmc
Development of a HPLC-MS/MS Method to Assess the Pharmacokinetics and Tumour Distribution of the Dimethylarginine Dimethylaminohydrolase 1 Inhibitors ZST316 and L-257 in a Xenograft Model of Triple-Negative Breast Cancer in Mice
Development of a HPLC-MS/MS Method to Assess the Pharmacokinetics and Tumour Distribution of the Dimethylarginine Dimethylaminohydrolase 1 Inhibitors ZST316 and L-257 in a Xenograft Model of Triple-Negative Breast Cancer in Mice Abstract Abstract We describe the development and validation of an HPLC-MS/MS method to ass...
PMC5368957
core_pubmed_pmc
Influence of age on intestinal bile acid transport in C57BL/6 mice
Influence of age on intestinal bile acid transport in C57BL/6 mice Abstract Abstract Intestinal and hepatic bile acid transporters are important for enterohepatic bile acid circulation and pharmacokinetics. Based on previous literature, we hypothesized that the expression of bile acid transporters and intestinal bile a...
PMC10427511
core_pubmed_pmc
A phase 1 study in healthy participants to characterize the safety and pharmacology of inclacumab, a fully human anti-P-selectin antibody, in development for treatment of sickle cell disease
A phase 1 study in healthy participants to characterize the safety and pharmacology of inclacumab, a fully human anti-P-selectin antibody, in development for treatment of sickle cell disease Abstract Purpose We evaluated the safety, pharmacokinetics (PK), pharmacodynamics (PD), and immunogenicity of intravenous (IV) in...
PMC6105165
core_pubmed_pmc
A phase I study of LY3164530, a bispecific antibody targeting MET and EGFR, in patients with advanced or metastatic cancer
A phase I study of LY3164530, a bispecific antibody targeting MET and EGFR, in patients with advanced or metastatic cancer Abstract Abstract Purpose The phase I study characterized the safety, pharmacokinetics, anti-tumor activity, and recommended phase II dose/schedule of LY3164530 in patients with advanced or metasta...
PMC12411485
core_pubmed_pmc
Flavonoids in atopic dermatitis: mechanisms, delivery innovations, and translational strategies
Flavonoids in atopic dermatitis: mechanisms, delivery innovations, and translational strategies Abstract Abstract Objective To provide a comprehensive narrative synthesis of recent advances in the pharmacological actions and therapeutic potential of natural flavonoids in atopic dermatitis (AD), with emphasis on their m...
PMC12938469
core_pubmed_pmc
Next-Generation HIV-1 Therapeutics in Co-Endemic Settings
Next-Generation HIV-1 Therapeutics in Co-Endemic Settings Abstract The development of next-generation HIV-1 therapeutics, including ultralong-acting antivirals, novel mechanistic classes, and curative immunotherapies, promises to overcome the limitations of lifelong, daily antiretroviral therapy (ART). However, the rea...
PMC3720542
core_pubmed_pmc
Population pharmacokinetics of mefloquine, piperaquine and artemether-lumefantrine in Cambodian and Tanzanian malaria patients
Population pharmacokinetics of mefloquine, piperaquine and artemether-lumefantrine in Cambodian and Tanzanian malaria patients Abstract Abstract Background Inter-individual variability in plasma concentration-time profiles might contribute to differences in anti-malarial treatment response. This study investigated the ...
PMC8048069
core_pubmed_pmc
Contribution of Population Pharmacokinetics of Glycopeptides and Antifungals to Dosage Adaptation in Paediatric Onco-hematological Malignancies: A Review
Contribution of Population Pharmacokinetics of Glycopeptides and Antifungals to Dosage Adaptation in Paediatric Onco-hematological Malignancies: A Review Abstract Abstract The response to medications in children differs not only in comparison to adults but also between children of the different age groups and according...
PMC11812940
core_pubmed_pmc
Exploration of the potential impact of batch‐to‐batch variability on the establishment of pharmacokinetic bioequivalence for inhalation powder drug products
Exploration of the potential impact of batch‐to‐batch variability on the establishment of pharmacokinetic bioequivalence for inhalation powder drug products Abstract Abstract Batch‐to‐batch variability in inhalation powder has been identified as a potential challenge in the development of generic versions. This study e...
PMC10284613
core_pubmed_pmc
Pharmacokinetics of baricitinib in critically ill COVID-19 patients
Pharmacokinetics of baricitinib in critically ill COVID-19 patients Abstract Abstract Background The use of the selective Janus Kinase 1/2 inhibitor baricitinib has shown a survival benefit in mechanically ventilated COVID-19 patients but this is not without adverse drug reactions. Although critically ill patients are ...
PMC8094082
core_pubmed_pmc
Individualized dosing guidelines for PEGasparaginase and factors influencing the clearance: a population pharmacokinetic model
Individualized dosing guidelines for PEGasparaginase and factors influencing the clearance: a population pharmacokinetic model Abstract Considerable inter- and intra-patient variability exist in serum activity levels of PEGasparaginase, essential for pediatric acute lymphoblastic leukemia (ALL) treatment. A population ...
PMC12481524
core_pubmed_pmc
Population pharmacokinetic modeling of sulfadimethoxine, sulfadiazine and sulfamethoxazole combined to trimethoprim in pigs
Population pharmacokinetic modeling of sulfadimethoxine, sulfadiazine and sulfamethoxazole combined to trimethoprim in pigs Abstract Abstract Sulfonamides (S) are old antibiotics combined with trimethoprim (TMP) for synergistic effects against pathogens responsible for a variety of infections in food-producing animals....
PMC12633417
core_pubmed_pmc
Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters –in vitro investigations and physiologically based pharmacokinetic modelling
Dicloxacillin and flucloxacillin inhibit hepatic uptake transporters –in vitro investigations and physiologically based pharmacokinetic modelling Abstract Abstract Dicloxacillin and flucloxacillin are β-lactamase-resistant penicillin antibiotics that have been in clinical use for over 50 years. While both antibiotics a...
PMC5064158
core_pubmed_pmc
Optimal Clinical Doses of Faropenem, Linezolid, and Moxifloxacin in Children With Disseminated Tuberculosis: Goldilocks
Optimal Clinical Doses of Faropenem, Linezolid, and Moxifloxacin in Children With Disseminated Tuberculosis: Goldilocks Abstract Background. When treated with the same antibiotic dose, children achieve different 0- to 24-hour area under the concentration-time curves (AUC 0–24 ) because of maturation and between-child p...
PMC11678797
core_pubmed_pmc
A Repurposed Drug Selection Pipeline to Identify CNS-Penetrant Drug Candidates for Glioblastoma
A Repurposed Drug Selection Pipeline to Identify CNS-Penetrant Drug Candidates for Glioblastoma Abstract Background: Glioblastoma is an aggressive and incurable type of brain cancer. Little progress has been made in the development of effective new therapies in the past decades. The blood–brain barrier (BBB) and drug e...
PMC11434810
core_pubmed_pmc
Powder Self-Emulsifying Drug Delivery System for Mitotane: In Vitro and In Vivo Evaluation
Powder Self-Emulsifying Drug Delivery System for Mitotane: In Vitro and In Vivo Evaluation Abstract Abstract Drug Delivery Systems (DDSs) of known drugs are prominent candidates for new and more effective treatments of various diseases, as they may increase drug solubility, dissolution velocity, and bioavailability. Mi...
PMC8476623
core_pubmed_pmc
Effect of CYP3A4 metabolism on sex differences in the pharmacokinetics and pharmacodynamics of zolpidem
Effect of CYP3A4 metabolism on sex differences in the pharmacokinetics and pharmacodynamics of zolpidem Abstract Abstract To investigate pharmacokinetic and pharmacodynamic differences of zolpidem between males and females and their causes, including CYP3A4 activity. A single oral dose of zolpidem (10 mg) was administe...
PMC4938879
core_pubmed_pmc
Physiologically Based Pharmacokinetic (PBPK) Model for Biodistribution of Radiolabeled Peptides in Patients with Neuroendocrine Tumours
Physiologically Based Pharmacokinetic (PBPK) Model for Biodistribution of Radiolabeled Peptides in Patients with Neuroendocrine Tumours Abstract Abstract Objective(s): The objectives of this work was to assess the benefits of the application of Physiologically Based Pharmacokinetic (PBPK) models in patients with differ...
PMC7746945
core_pubmed_pmc
Pharmacokinetics, safety, and tolerability of olaparib and temozolomide for recurrent glioblastoma: results of the phase I OPARATIC trial
Pharmacokinetics, safety, and tolerability of olaparib and temozolomide for recurrent glioblastoma: results of the phase I OPARATIC trial Abstract Abstract Background The poly(ADP-ribose) polymerase (PARP) inhibitor olaparib potentiated radiation and temozolomide (TMZ) chemotherapy in preclinical glioblastoma models bu...
PMC11561736
core_pubmed_pmc
Enhanced in vivo Stability and Antitumor Efficacy of PEGylated Liposomes of Paclitaxel Palmitate Prodrug
Enhanced in vivo Stability and Antitumor Efficacy of PEGylated Liposomes of Paclitaxel Palmitate Prodrug Abstract Abstract Purpose The clinical use of paclitaxel (PTX) in cancer treatment is limited by its poor water solubility, significant toxicity, and adverse effects. This study aimed to propose a straightforward an...
PMC6106931
core_pubmed_pmc
Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer’s disease: randomized, double-blind, placebo-controlled study
Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer’s disease: randomized, double-blind, placebo-controlled study Abstract Abstract Background β-Secretase enzyme (BACE) inhibition has been proposed as a priority treatment mechanism for Alzheimer’s disease (AD), but t...
PMC7318259
core_pubmed_pmc
Exposure–response relationships for the sodium‐glucose co‐transporter‐2 inhibitor dapagliflozin with regard to renal risk markers
Exposure–response relationships for the sodium‐glucose co‐transporter‐2 inhibitor dapagliflozin with regard to renal risk markers Abstract Abstract Aims To quantitate the consistency of an individual's plasma exposure to dapagliflozin upon re‐exposure, and to investigate whether the individual's systemic exposure to da...
PMC9725750
core_pubmed_pmc
The clinical pharmacology of tafenoquine in the radical cure of Plasmodium vivax malaria: An individual patient data meta-analysis
The clinical pharmacology of tafenoquine in the radical cure of Plasmodium vivax malaria: An individual patient data meta-analysis Abstract Abstract Tafenoquine is a newly licensed antimalarial drug for the radical cure of Plasmodium vivax malaria. The mechanism of action and optimal dosing are uncertain. We pooled ind...
PMC11600623
core_pubmed_pmc
Population pharmacokinetic analysis of quizartinib in patients with newly diagnosed FLT3‐internal‐tandem‐duplication‐positive acute myeloid leukemia
Population pharmacokinetic analysis of quizartinib in patients with newly diagnosed FLT3‐internal‐tandem‐duplication‐positive acute myeloid leukemia Abstract Abstract The population pharmacokinetics (PK) of quizartinib and its pharmacologically active metabolite AC886 have been previously described in healthy volunteer...
PMC3799537
core_pubmed_pmc
Strategies to Minimize Antibiotic Resistance
Strategies to Minimize Antibiotic Resistance Abstract Abstract Antibiotic resistance can be reduced by using antibiotics prudently based on guidelines of antimicrobial stewardship programs (ASPs) and various data such as pharmacokinetic (PK) and pharmacodynamic (PD) properties of antibiotics, diagnostic testing, antimi...
PMC8020855
core_pubmed_pmc
Bayesian estimation of pharmacokinetic parameters: an important component to include in the teaching of clinical pharmacokinetics and therapeutic drug monitoring
Bayesian estimation of pharmacokinetic parameters: an important component to include in the teaching of clinical pharmacokinetics and therapeutic drug monitoring Abstract Abstract Bayesian estimation of pharmacokinetic parameters (PKP), as discussed in this review, provides a powerful approach towards the individualiza...
PMC11206811
core_pubmed_pmc
Population Pharmacokinetics of Dasatinib in Healthy Subjects
Population Pharmacokinetics of Dasatinib in Healthy Subjects Abstract Background and Objectives: Dasatinib is one of the tyrosine kinase inhibitors. The main use of these agents is inhibition of cancerous cell proliferation. The therapeutic importance of tyrosine kinase inhibitors raises the necessity of many types of ...
PMC7990796
core_pubmed_pmc
Efficacy of a Combined Antiplatelet Therapy Is Not Affected by a Simultaneous Binding of Cangrelor and PSB 0777 to Albumin
Efficacy of a Combined Antiplatelet Therapy Is Not Affected by a Simultaneous Binding of Cangrelor and PSB 0777 to Albumin Abstract Concurrent administration of two drugs may complicate the management of acute coronary syndromes: competitive drug displacement diminishes drug binding and alters drug pharmacodynamics. We...
PMC4644980
core_pubmed_pmc
The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer’s disease amyloid-β peptides
The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer’s disease amyloid-β peptides Abstract Known γ-secretase inhibitors or modulators display an undesirable pharmacokinetic profile and toxicity and have therefore not been successful in clinical trials for Alzheimer’s disease (AD)...
PMC6920808
core_pubmed_pmc
Preclinical Evaluation of UDCA-Containing Oral Formulation in Mice for the Treatment of Wet Age-Related Macular Degeneration
Preclinical Evaluation of UDCA-Containing Oral Formulation in Mice for the Treatment of Wet Age-Related Macular Degeneration Abstract Abstract As a posterior ocular disease, wet age-related macular degeneration (WAMD) has been known to be related to vision loss, accompanying ocular complications. The intravitreous inje...
PMC3717157
core_pubmed_pmc
A phase I study of intravenous aflibercept with FOLFIRI in Japanese patients with previously treated metastatic colorectal cancer
A phase I study of intravenous aflibercept with FOLFIRI in Japanese patients with previously treated metastatic colorectal cancer Abstract Summary Aflibercept, a recombinant fusion protein, is a potent inhibitor of vascular endothelial growth factor (VEGF)-A, VEGF-B, and the placental growth factor (PlGF). The present ...
PMC9053011
core_pubmed_pmc
An open‐label, dose‐escalation study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single doses of GSK2586881 in participants with pulmonary arterial hypertension
An open‐label, dose‐escalation study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single doses of GSK2586881 in participants with pulmonary arterial hypertension Abstract Abstract Preclinical and early clinical studies suggest that angiotensin‐converting enzyme type 2 activity may be ...
PMC8999552
core_pubmed_pmc
An Up-to-Date Article Regarding Particularities of Drug Treatment in Patients with Chronic Heart Failure
An Up-to-Date Article Regarding Particularities of Drug Treatment in Patients with Chronic Heart Failure Abstract Since the prevalence of heart failure (HF) increases with age, HF is now one of the most common reasons for the hospitalization of elderly people. Although the treatment strategies and overall outcomes of H...
PMC6960190
core_pubmed_pmc
Systemic Evaluation on the Pharmacokinetics of Platinum-Based Anticancer Drugs From Animal to Cell Level: Based on Total Platinum and Intact Drugs
Systemic Evaluation on the Pharmacokinetics of Platinum-Based Anticancer Drugs From Animal to Cell Level: Based on Total Platinum and Intact Drugs Abstract Cisplatin, carboplatin, and oxaliplatin are the common platinum-based anticancer drugs widely used in the chemotherapeutic treatment of solid tumors in clinic. Howe...
PMC11345836
core_pubmed_pmc
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19 Abstract Abstract Despite the record-breaking discovery, development and approval of vaccines and antiviral therapeutics such as Paxlovid, coronavirus disease 2019 (COVID-19) remained the fourth leading cause of...
PMC5952257
core_pubmed_pmc
Developments in Glycopeptide Antibiotics
Developments in Glycopeptide Antibiotics Abstract Glycopeptide antibiotics (GPAs) are a key weapon in the fight against drug resistant bacteria, with vancomycin still a mainstream therapy against serious Gram-positive infections more than 50 years after it was first introduced. New, more potent semisynthetic derivative...
PMC10414718
core_pubmed_pmc
Tarlatamab, a First-in-Class DLL3-Targeted Bispecific T-Cell Engager, in Recurrent Small-Cell Lung Cancer: An Open-Label, Phase I Study
Tarlatamab, a First-in-Class DLL3-Targeted Bispecific T-Cell Engager, in Recurrent Small-Cell Lung Cancer: An Open-Label, Phase I Study Abstract PURPOSE Small-cell lung cancer (SCLC) is an aggressive malignancy with limited treatments. Delta-like ligand 3 (DLL3) is aberrantly expressed in most SCLC. Tarlatamab (AMG 757...
PMC3198383
core_pubmed_pmc
A Multi-Compartment, Single and Multiple Dose Pharmacokinetic Study of the Vaginal Candidate Microbicide 1% Tenofovir Gel
A Multi-Compartment, Single and Multiple Dose Pharmacokinetic Study of the Vaginal Candidate Microbicide 1% Tenofovir Gel Abstract Background Tenofovir (TFV) gel is being evaluated as a microbicide with pericoital and daily regimens. To inhibit viral replication locally, an adequate concentration in the genital tract i...
PMC10670065
core_pubmed_pmc
Anticarcinogenic Potency of EF24: An Overview of Its Pharmacokinetics, Efficacy, Mechanism of Action, and Nanoformulation for Drug Delivery
Anticarcinogenic Potency of EF24: An Overview of Its Pharmacokinetics, Efficacy, Mechanism of Action, and Nanoformulation for Drug Delivery Abstract Simple Summary This study summarizes the current state of knowledge about the anticancer potential of the curcumin analog EF24, including its pharmacokinetic profile, ther...
PMC3215663
core_pubmed_pmc
Canalization effect in the coagulation cascade and the interindividual variability of oral anticoagulant response. a simulation Study
Canalization effect in the coagulation cascade and the interindividual variability of oral anticoagulant response. a simulation Study Abstract Background Increasing the predictability and reducing the rate of side effects of oral anticoagulant treatment (OAT) requires further clarification of the cause of about 50% of ...
PMC12387580
core_pubmed_pmc
Marine-Derived Polymers–Polysaccharides as Promising Natural Therapeutics for Atherosclerotic Cardiovascular Disease
Marine-Derived Polymers–Polysaccharides as Promising Natural Therapeutics for Atherosclerotic Cardiovascular Disease Abstract Atherosclerotic cardiovascular disease (ASCVD) remains a leading cause of morbidity and mortality worldwide, driven by dyslipidemia, chronic inflammation, oxidative stress, and endothelial dysfu...
PMC9931434
core_pubmed_pmc
Oncolytic viral kinetics mechanistic modeling of Talimogene Laherparepvec (T‐VEC) a first‐in‐class oncolytic viral therapy in patients with advanced melanoma
Oncolytic viral kinetics mechanistic modeling of Talimogene Laherparepvec (T‐VEC) a first‐in‐class oncolytic viral therapy in patients with advanced melanoma Abstract Abstract Talimogene Laherparepvec (T‐VEC) is a first‐in‐class oncolytic virotherapy approved for the treatment of unresectable melanoma recurrent after i...
PMC5573754
core_pubmed_pmc
Impact of an alternative steroid on the relative bioavailability and bioequivalence of a novel versus the originator formulation of abiraterone acetate
Impact of an alternative steroid on the relative bioavailability and bioequivalence of a novel versus the originator formulation of abiraterone acetate Abstract Abstract Purpose The originator abiraterone acetate (OAA) formulation is used for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Thi...
PMC8123347
core_pubmed_pmc
Predicting Absorption-Distribution Properties of Neuroprotective Phosphine-Borane Compounds Using In Silico Modeling and Machine Learning
Predicting Absorption-Distribution Properties of Neuroprotective Phosphine-Borane Compounds Using In Silico Modeling and Machine Learning Abstract Phosphine-borane complexes are novel chemical entities with preclinical efficacy in neuronal and ophthalmic disease models. In vitro and in vivo studies showed that the meta...
PMC6077530
core_pubmed_pmc
The Bioavailability and Pharmacokinetics of Silymarin SMEDDS Formulation Study in Healthy Thai Volunteers
The Bioavailability and Pharmacokinetics of Silymarin SMEDDS Formulation Study in Healthy Thai Volunteers Abstract Abstract The present study aimed to determine the pharmacokinetic parameters and bioavailability of silymarin 140 mg SMEDDS formulation. An open-label, single-dose pharmacokinetic study was conducted. Twel...
PMC11315837
core_pubmed_pmc
A Semi-Mechanistic Population Pharmacokinetic Model of Noscapine in Healthy Subjects Considering Hepatic First-Pass Extraction and CYP2C9 Genotypes
A Semi-Mechanistic Population Pharmacokinetic Model of Noscapine in Healthy Subjects Considering Hepatic First-Pass Extraction and CYP2C9 Genotypes Abstract Introduction Noscapine is a commonly used cough suppressant, with ongoing research on its anti-inflammatory and anti-tumor properties. The drug has a pronounced ph...
PMC9260974
core_pubmed_pmc
Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions
Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions Abstract Purpose The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study...
PMC7277861
core_pubmed_pmc
A Comprehensive Review of the Phytochemical, Pharmacological, and Toxicological Properties of Tribulus terrestris L.
A Comprehensive Review of the Phytochemical, Pharmacological, and Toxicological Properties of Tribulus terrestris L. Abstract The general spread of Tribulus terrestris L. (South Africa, Australia, Europe, and India), the high content of active ingredients (in particular sterol saponins, as well as flavonoids, tannins, ...
PMC6130657
core_pubmed_pmc
In vitro and ex vivo approach for anti-urolithiatic potential of bioactive fractions of gokhru with simultaneous HPLC analysis of six major metabolites and their exploration in rat plasma
In vitro and ex vivo approach for anti-urolithiatic potential of bioactive fractions of gokhru with simultaneous HPLC analysis of six major metabolites and their exploration in rat plasma Abstract Abstract Context: Tribulus terrestris L. (Zygophyllaceae) fruits have long been used in traditional systems of medicine for...
PMC9646544
core_pubmed_pmc
Safety and efficacy of daratumumab in Chinese patients with relapsed or refractory multiple myeloma: a phase 1, dose-escalation study (MMY1003)
Safety and efficacy of daratumumab in Chinese patients with relapsed or refractory multiple myeloma: a phase 1, dose-escalation study (MMY1003) Abstract Daratumumab monotherapy demonstrated favorable safety and efficacy in relapsed/refractory multiple myeloma (RRMM) patients in the global phase 1/2 GEN501 and phase 2 S...
PMC9581391
core_pubmed_pmc
“Rogue” neutrophil-subset [DEspR+CD11b+/CD66b+] immunotype is an actionable therapeutic target for neutrophilic inflammation-mediated tissue injury – studies in human, macaque and rat LPS-inflammation models
“Rogue” neutrophil-subset [DEspR+CD11b+/CD66b+] immunotype is an actionable therapeutic target for neutrophilic inflammation-mediated tissue injury – studies in human, macaque and rat LPS-inflammation models Abstract Abstract Background and objective The correlation (Rs > 0.7) of neutrophils expressing the dual endothe...
PMC11510348
core_pubmed_pmc
Comparative Pharmacokinetics of Sustained-Release versus Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study
Comparative Pharmacokinetics of Sustained-Release versus Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study Abstract Abstract Background: Exogenous melatonin, a nutraceutical for maintaining a healthy sleep–wake cycle and managing sleep disorders, requires large, ...
PMC9330804
core_pubmed_pmc
Machine Learning and Pharmacometrics for Prediction of Pharmacokinetic Data: Differences, Similarities and Challenges Illustrated with Rifampicin
Machine Learning and Pharmacometrics for Prediction of Pharmacokinetic Data: Differences, Similarities and Challenges Illustrated with Rifampicin Abstract Abstract Pharmacometrics (PM) and machine learning (ML) are both valuable for drug development to characterize pharmacokinetics (PK) and pharmacodynamics (PD). Pharm...
PMC6032903
core_pubmed_pmc
Evaluation of Flexible Tacrolimus Drug Concentration Monitoring Approach in Patients Receiving Extended‐Release Once‐Daily Tacrolimus Tablets
Evaluation of Flexible Tacrolimus Drug Concentration Monitoring Approach in Patients Receiving Extended‐Release Once‐Daily Tacrolimus Tablets Abstract Abstract The majority of United States kidney transplant patients are treated with tacrolimus, a drug effective in preventing graft rejection, but with a narrow therapeu...
PMC7193063
core_pubmed_pmc
Quantitative analysis of the effect of fraction of inspired oxygen on peripheral oxygen saturation in healthy volunteers
Quantitative analysis of the effect of fraction of inspired oxygen on peripheral oxygen saturation in healthy volunteers Abstract Background The international organization for standardization (ISO) 80601-2-61 dictates that the accuracy of a pulse oximeter should be assessed by a controlled desaturation study. We aimed ...
PMC6095608
core_pubmed_pmc
Efavirenz reduces renal excretion of lamivudine in rats by inhibiting organic cation transporters (OCT, Oct) and multidrug and toxin extrusion proteins (MATE, Mate)
Efavirenz reduces renal excretion of lamivudine in rats by inhibiting organic cation transporters (OCT, Oct) and multidrug and toxin extrusion proteins (MATE, Mate) Abstract Abstract Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor used in first-line combination antiretroviral therapy (cART). It is u...