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PMC9017382
core_pubmed_pmc
Single Ascending-Dose Study To Evaluate the Safety, Tolerability, and Pharmacokinetics of Sutezolid in Healthy Adult Subjects
Single Ascending-Dose Study To Evaluate the Safety, Tolerability, and Pharmacokinetics of Sutezolid in Healthy Adult Subjects Abstract ABSTRACT The primary objective of the study was to evaluate the safety and tolerability of single oral doses of sutezolid tablets administered under fasting conditions in healthy adult ...
PMC11769521
core_pubmed_pmc
Investigations of Long-Acting Formulations in Children, Adolescents, and Pregnant Women: A Systematic Review
Investigations of Long-Acting Formulations in Children, Adolescents, and Pregnant Women: A Systematic Review Abstract Background/Objectives: Long-acting and extended-release drug delivery strategies have greatly improved treatment for a variety of medical conditions. Special populations, specifically infants, children,...
PMC12030730
core_pubmed_pmc
Using Physiologically Based Pharmacokinetic Models for Assessing Pharmacokinetic Drug–Drug Interactions in Patients with Chronic Heart Failure Taking Narrow Therapeutic Window Drugs
Using Physiologically Based Pharmacokinetic Models for Assessing Pharmacokinetic Drug–Drug Interactions in Patients with Chronic Heart Failure Taking Narrow Therapeutic Window Drugs Abstract Abstract Background: Pharmacotherapy of chronic heart failure (CHF) with a reduced ejection fraction includes a combination of dr...
PMC10149097
core_pubmed_pmc
In silico Study of Antiviral Activity of Polyphenol Compounds from Ocimum basilicum by Molecular Docking, ADMET, and Drug-Likeness Analysis
In silico Study of Antiviral Activity of Polyphenol Compounds from Ocimum basilicum by Molecular Docking, ADMET, and Drug-Likeness Analysis Abstract Abstract Aim The SARS-CoV-2 virus is a disease that has mild to severe effects on patients, which can even lead to death. One of the enzymes that act as DNA replication is...
PMC9398717
core_pubmed_pmc
Comparison of Pharmacokinetic Profiles of 14 Major Bioactive Components in Normal and Arthritic Model Rats after Oral Administration of Angelicae pubescentis Radix by UPLC-MS/MS
Comparison of Pharmacokinetic Profiles of 14 Major Bioactive Components in Normal and Arthritic Model Rats after Oral Administration of Angelicae pubescentis Radix by UPLC-MS/MS Abstract An ultraperformance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was established to simultaneously determine 14...
PMC11220307
core_pubmed_pmc
Cadmium nanocluster as a safe nanocarrier: biodistribution in BALB/c mice and application to carry crocin to breast cancer cell lines
Cadmium nanocluster as a safe nanocarrier: biodistribution in BALB/c mice and application to carry crocin to breast cancer cell lines Abstract Abstract Aim: Metal nanoclusters are emerging nanomaterials applicable for drug delivery. Here, the toxicity and oxidative stress induction of divalent cationic cadmium (Cd 2+ )...
PMC5680251
core_pubmed_pmc
Differential T Cell Signaling Pathway Activation by Tacrolimus and Belatacept after Kidney Transplantation: Post Hoc Analysis of a Randomised-Controlled Trial
Differential T Cell Signaling Pathway Activation by Tacrolimus and Belatacept after Kidney Transplantation: Post Hoc Analysis of a Randomised-Controlled Trial Abstract Abstract Pharmacokinetic immunosuppressive drug monitoring poorly correlates with clinical outcomes after solid organ transplantation. A promising metho...
PMC10525617
core_pubmed_pmc
The Significance of Bayesian Pharmacokinetics in Dosing for Critically Ill Patients: A Primer for Clinicians Using Vancomycin as an Example
The Significance of Bayesian Pharmacokinetics in Dosing for Critically Ill Patients: A Primer for Clinicians Using Vancomycin as an Example Abstract Abstract Antibiotic use is becoming increasingly challenging with the emergence of multidrug-resistant organisms. Pharmacokinetic (PK) alterations result from complex path...
PMC12521730
core_pubmed_pmc
Quantitative dual-isotope preclinical SPECT/CT imaging and biodistribution of the mercury-197m/g theranostic pair with [ 197m/g Hg]HgCl 2 and a [ 197m/g Hg]Hg-tetrathiol complex as a platform for radiopharmaceutical development
Quantitative dual-isotope preclinical SPECT/CT imaging and biodistribution of the mercury-197m/g theranostic pair with [ 197m/g Hg]HgCl 2 and a [ 197m/g Hg]Hg-tetrathiol complex as a platform for radiopharmaceutical development Abstract Abstract Background Mercury-197m ( 197m Hg, t 1/2 = 23.8 h) and mercury-197g ( 197g...
PMC10843171
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and toxicity of a PD-1-targeted IL-15 in cynomolgus monkeys
Pharmacokinetics, pharmacodynamics, and toxicity of a PD-1-targeted IL-15 in cynomolgus monkeys Abstract PF-07209960 is a novel bispecific fusion protein composed of an anti-PD-1 antibody and engineered IL-15 cytokine mutein with reduced binding affinity to its receptors. The pharmacokinetics (PK), pharmacodynamics (PD...
PMC4068511
core_pubmed_pmc
Individualization of Piperacillin Dosing for Critically Ill Patients: Dosing Software To Optimize Antimicrobial Therapy
Individualization of Piperacillin Dosing for Critically Ill Patients: Dosing Software To Optimize Antimicrobial Therapy Abstract Abstract Piperacillin-tazobactam is frequently used for empirical and targeted therapy of infections in critically ill patients. Considerable pharmacokinetic (PK) variability is observed in c...
PMC9316995
core_pubmed_pmc
Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis
Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis Abstract Abstract This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol mono...
PMC3899768
core_pubmed_pmc
SLC28A3 genotype and gemcitabine rate of infusion affect dFdCTP metabolite disposition in patients with solid tumours
SLC28A3 genotype and gemcitabine rate of infusion affect dFdCTP metabolite disposition in patients with solid tumours Abstract Background: Gemcitabine is used for the treatment of several solid tumours and exhibits high inter-individual pharmacokinetic variability. In this study, we explore possible predictive covariat...
PMC10749543
core_pubmed_pmc
Olanzapine Pharmacokinetics: A Clinical Review of Current Insights and Remaining Questions
Olanzapine Pharmacokinetics: A Clinical Review of Current Insights and Remaining Questions Abstract Abstract Olanzapine is one of the most widely used antipsychotics since its initial approval by the US Food and Drug Administration in 1996 and has undergone extensive pharmacokinetic study. Despite being utilized in cli...
PMC7598278
core_pubmed_pmc
A Novel Co-Crystal of Bexarotene and Ligustrazine Improves Pharmacokinetics and Tissue Distribution of Bexarotene in SD Rats
A Novel Co-Crystal of Bexarotene and Ligustrazine Improves Pharmacokinetics and Tissue Distribution of Bexarotene in SD Rats Abstract Bexarotene (BEX), a specific retinoic acid X receptor (RXR) agonist granted by Food and Drug Administration (FDA) approval for the clinical treatment of T cell lymphoma, has now been fou...
PMC4217108
core_pubmed_pmc
Glycol chitosan nanoparticles as specialized cancer therapeutic vehicles: Sequential delivery of doxorubicin and Bcl-2 siRNA
Glycol chitosan nanoparticles as specialized cancer therapeutic vehicles: Sequential delivery of doxorubicin and Bcl-2 siRNA Abstract Abstract Conventional chemotherapy is plagued with adverse side effects because cancer treatments are subject to numerous variations, most predominantly from drug resistance. Accordingly...
PMC12574322
core_pubmed_pmc
Less frequent intravenous dosing of nemvaleukin alfa in patients with advanced solid tumors: the phase 1/2 ARTISTRY-3 trial
Less frequent intravenous dosing of nemvaleukin alfa in patients with advanced solid tumors: the phase 1/2 ARTISTRY-3 trial Abstract Abstract Background Intravenous (IV) nemvaleukin alfa (nemvaleukin, ALKS 4230) administered daily on days 1-5 in 21‑day cycles demonstrated antitumor activity and manageable safety in hea...
PMC9459822
core_pubmed_pmc
Exosome-Containing Extracellular Vesicles Contribute to the Transport of Resveratrol Metabolites in the Bloodstream: A Human Pharmacokinetic Study
Exosome-Containing Extracellular Vesicles Contribute to the Transport of Resveratrol Metabolites in the Bloodstream: A Human Pharmacokinetic Study Abstract Abstract Exosomes are extracellular vesicles (EVs) that regulate intercellular signaling by transferring small RNAs, proteins, nucleic acids, lipids, and other meta...
PMC9694402
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution of 13 C-Labeled Succinic Acid in Mice
Pharmacokinetics and Tissue Distribution of 13 C-Labeled Succinic Acid in Mice Abstract Abstract Succinic acid is widely used as a food additive, and its effects on sepsis, cancer, ataxia, and obesity were recently reported. Dietary drug exposure studies have been conducted to evaluate the in vivo efficacy of succinic ...
PMC10583682
core_pubmed_pmc
An improved PKPD modeling approach to characterize the pharmacodynamic interaction over time between ceftazidime/avibactam and colistin from in vitro time-kill experiments against multidrug-resistant Klebsiella pneumoniae isolates
An improved PKPD modeling approach to characterize the pharmacodynamic interaction over time between ceftazidime/avibactam and colistin from in vitro time-kill experiments against multidrug-resistant Klebsiella pneumoniae isolates Abstract ABSTRACT In contrast to the checkerboard method, bactericidal experiments [time-...
PMC12430943
core_pubmed_pmc
Dual-route levofloxacin delivery following revision surgery: a synergistic intravenous/intra-articular strategy for enhanced bactericidal effect against prosthetic Pseudomonas aeruginosa infections
Dual-route levofloxacin delivery following revision surgery: a synergistic intravenous/intra-articular strategy for enhanced bactericidal effect against prosthetic Pseudomonas aeruginosa infections Abstract Purpose: Pseudomonas aeruginosa (PA)-associated periprosthetic joint infection (PJI) is notoriously difficult to ...
PMC6513110
core_pubmed_pmc
Optimization of florfenicol dose against Piscirickettsia salmonis in Salmo salar through PK/PD studies
Optimization of florfenicol dose against Piscirickettsia salmonis in Salmo salar through PK/PD studies Abstract Salmonid Rickettsial Septicemia (SRS) is the disease of greatest economic importance in the Chilean salmon farming industry, causing high mortality in fish during the final stage of their productive cycle at ...
PMC8858243
core_pubmed_pmc
A Pharmacokinetic Study of Native E.coli Asparaginase for Acute Lymphoblastic Leukemia Treated with ThaiPOG Protocol
A Pharmacokinetic Study of Native E.coli Asparaginase for Acute Lymphoblastic Leukemia Treated with ThaiPOG Protocol Abstract Abstract Background: Asparaginase is one of the essential chemotherapies used to treat acute lymphoblastic leukemia (ALL). Asparaginase antibody production may cause a subtherapeutic level and r...
PMC9146469
core_pubmed_pmc
Cannabidiol (CBD) Dosing: Plasma Pharmacokinetics and Effects on Accumulation in Skeletal Muscle, Liver and Adipose Tissue
Cannabidiol (CBD) Dosing: Plasma Pharmacokinetics and Effects on Accumulation in Skeletal Muscle, Liver and Adipose Tissue Abstract Oral cannabidiol (CBD) consumption is widespread in North America and Europe, as it has analgesic, neuroprotective and antitumor effects. Although oral CBD consumption in humans affords be...
PMC7894406
core_pubmed_pmc
PBPK Model of Coproporphyrin I: Evaluation of the Impact of SLCO1B1 Genotype, Ethnicity, and Sex on its Inter‐Individual Variability
PBPK Model of Coproporphyrin I: Evaluation of the Impact of SLCO1B1 Genotype, Ethnicity, and Sex on its Inter‐Individual Variability Abstract Coproporphyrin I (CPI) is an endogenous biomarker of OATP1B activity and associated drug‐drug interactions. In this study, a minimal physiologically‐based pharmacokinetic model w...
PMC6175093
core_pubmed_pmc
Lack of Impact by SCY‐078, a First‐in‐Class Oral Fungicidal Glucan Synthase Inhibitor, on the Pharmacokinetics of Rosiglitazone, a Substrate for CYP450 2C8, Supports the Low Risk for Clinically Relevant Metabolic Drug‐Drug Interactions
Lack of Impact by SCY‐078, a First‐in‐Class Oral Fungicidal Glucan Synthase Inhibitor, on the Pharmacokinetics of Rosiglitazone, a Substrate for CYP450 2C8, Supports the Low Risk for Clinically Relevant Metabolic Drug‐Drug Interactions Abstract Abstract SCY‐078, the first in a new class of β 1,3‐glucan synthesis inhibi...
PMC3082698
core_pubmed_pmc
Modelling and simulation as research tools in paediatric drug development
Modelling and simulation as research tools in paediatric drug development Abstract Abstract Purpose Although practical and ethical constraints impose special requirements for the evaluation of treatment safety and efficacy in children, the main issue remains the empirical basis for patient stratification and dose selec...
PMC6438786
core_pubmed_pmc
Physicochemical, pharmacokinetics, and histological evaluation of new naproxen-quercetin co-lyophilizate to diminish drug-induced gastric irritations in rats
Physicochemical, pharmacokinetics, and histological evaluation of new naproxen-quercetin co-lyophilizate to diminish drug-induced gastric irritations in rats Abstract Quercetin (QUE) is a flavonoid found in several plants and commonly distributed in edible vegetables and fruits. To evaluate the effect of co-lyophilizat...
PMC7305075
core_pubmed_pmc
In vivo assessment of the drug interaction between sorafenib and paracetamol in rats
In vivo assessment of the drug interaction between sorafenib and paracetamol in rats Abstract Abstract Purpose Sorafenib is a multi-targeted tyrosine kinase inhibitor (TKI) used for the treatment of advanced renal cell carcinoma, hepatocellular carcinoma and radioactive iodine resistant thyroid carcinoma. Neoplastic di...
PMC3218575
core_pubmed_pmc
Biodistribution and pharmacokinetics of 188 Re-liposomes and their comparative therapeutic efficacy with 5-fluorouracil in C26 colonic peritoneal carcinomatosis mice
Biodistribution and pharmacokinetics of 188 Re-liposomes and their comparative therapeutic efficacy with 5-fluorouracil in C26 colonic peritoneal carcinomatosis mice Abstract Abstract Background Nanoliposomes are designed as carriers capable of packaging drugs through passive targeting tumor sites by enhanced permeabil...
PMC9122788
core_pubmed_pmc
Phase I study of ribociclib and everolimus in children with newly diagnosed DIPG and high-grade glioma: A CONNECT pediatric neuro-oncology consortium report
Phase I study of ribociclib and everolimus in children with newly diagnosed DIPG and high-grade glioma: A CONNECT pediatric neuro-oncology consortium report Abstract Abstract Background Genomic aberrations in the cell cycle and PI3K/Akt/mTOR pathways have been reported in diffuse intrinsic pontine glioma (DIPG) and hig...
PMC10888695
core_pubmed_pmc
Unveiling Novel Urease Inhibitors for Helicobacter pylori : A Multi-Methodological Approach from Virtual Screening and ADME to Molecular Dynamics Simulations
Unveiling Novel Urease Inhibitors for Helicobacter pylori : A Multi-Methodological Approach from Virtual Screening and ADME to Molecular Dynamics Simulations Abstract Helicobacter pylori ( Hp ) infections pose a global health challenge demanding innovative therapeutic strategies by which to eradicate them. Urease, a ke...
PMC3520048
core_pubmed_pmc
mTOR Inhibitors in Tuberous Sclerosis Complex
mTOR Inhibitors in Tuberous Sclerosis Complex Abstract Abstract Tuberous sclerosis complex (TSC) is a genetic multiple organ system disorder that is characterized by the development of tumor-like lesions (hamartomas) and neurodevelopmental disorders. Mutations in the TSC1 and TSC2 tumor suppressor genes occur in the ma...
PMC10482267
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of aficamten in healthy Chinese participants: a randomized, double-blind, placebo-controlled, phase 1 study
Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of aficamten in healthy Chinese participants: a randomized, double-blind, placebo-controlled, phase 1 study Abstract Abstract Objectives: Aficamten is a selective, small-molecule allosteric inhibitor of cardiac sarcomere being dev...
PMC9309445
core_pubmed_pmc
A Randomized Pharmacokinetic Study in Healthy Male Subjects Comparing a High-concentration, Citrate-free SB5 Formulation (40 mg/0.4 ml) and Prior SB5 (Adalimumab Biosimilar)
A Randomized Pharmacokinetic Study in Healthy Male Subjects Comparing a High-concentration, Citrate-free SB5 Formulation (40 mg/0.4 ml) and Prior SB5 (Adalimumab Biosimilar) Abstract Introduction SB5 is an approved biosimilar of adalimumab, a monoclonal anti-tumor necrosis factor (anti-TNF) antibody. This study compare...
PMC12930065
core_pubmed_pmc
A phase I dose-escalation study of Lobaplatin combined with paclitaxel in platinum-sensitive recurrent ovarian epithelial carcinoma: preliminary safety and tolerability supporting clinical trial dosing
A phase I dose-escalation study of Lobaplatin combined with paclitaxel in platinum-sensitive recurrent ovarian epithelial carcinoma: preliminary safety and tolerability supporting clinical trial dosing Abstract Highlights • MTD was 30 mg/m 2 ; Grade 4 neutropenia occurred at 35 mg/m 2 . (60 characters) • LBP–TAX achiev...
PMC3127977
core_pubmed_pmc
No relevant cardiac, pharmacokinetic or safety interactions between roflumilast and inhaled formoterol in healthy subjects: an open-label, randomised, actively controlled study
No relevant cardiac, pharmacokinetic or safety interactions between roflumilast and inhaled formoterol in healthy subjects: an open-label, randomised, actively controlled study Abstract Abstract Background Roflumilast is an oral, selective phosphodiesterase 4 inhibitor with anti-inflammatory effects in chronic obstruct...
PMC9335946
core_pubmed_pmc
Tubeimoside-1: A review of its antitumor effects, pharmacokinetics, toxicity, and targeting preparations
Tubeimoside-1: A review of its antitumor effects, pharmacokinetics, toxicity, and targeting preparations Abstract Abstract Tubeimoside-1 (TBMS-1), a natural triterpenoid saponin found in traditional Chinese herbal medicine Bolbostemmatis Rhizoma, is present in numerous Chinese medicine preparations. This review aims to...
PMC5651060
core_pubmed_pmc
Evaluating Adherence of Health-Care Team to Standard Guideline of Colistin Use at Intensive Care Units of a Referral Hospital in Shiraz, Southwest of Iran
Evaluating Adherence of Health-Care Team to Standard Guideline of Colistin Use at Intensive Care Units of a Referral Hospital in Shiraz, Southwest of Iran Abstract Abstract Purpose: To evaluate colistin use according to global standard drug consumption in intensive care units of a referral hospital in Shiraz, Iran Meth...
PMC10962211
core_pubmed_pmc
Pharmacokinetics and relative bioavailability study of two cefquinome sulfate intramammary infusions in cow milk
Pharmacokinetics and relative bioavailability study of two cefquinome sulfate intramammary infusions in cow milk Abstract Abstract In this study, two intramammary infusions of cefquinome sulfate were investigated for pharmacokinetics and bioavailability. Twelve lactating cows for each group were administered an effecti...
PMC12353801
core_pubmed_pmc
A generative AI-discovered TNIK inhibitor for idiopathic pulmonary fibrosis: a randomized phase 2a trial
A generative AI-discovered TNIK inhibitor for idiopathic pulmonary fibrosis: a randomized phase 2a trial Abstract Despite substantial progress in artificial intelligence (AI) for generative chemistry, few novel AI-discovered or AI-designed drugs have reached human clinical trials. Here we present the results of the fir...
PMC10010692
core_pubmed_pmc
Opicapone Pharmacokinetics and Effects on Catechol- O -Methyltransferase Activity and Levodopa Pharmacokinetics in Patients With Parkinson Disease Receiving Carbidopa/Levodopa
Opicapone Pharmacokinetics and Effects on Catechol- O -Methyltransferase Activity and Levodopa Pharmacokinetics in Patients With Parkinson Disease Receiving Carbidopa/Levodopa Abstract Objectives Levodopa (LD) administered with dopa decarboxylase inhibitor is predominantly metabolized in the periphery by catechol- O -m...
PMC9676153
core_pubmed_pmc
Neurobiological substrates of chronic low back pain (CLBP): a brain [ 99m Tc]Tc-ECD SPECT study
Neurobiological substrates of chronic low back pain (CLBP): a brain [ 99m Tc]Tc-ECD SPECT study Abstract Background Recent neuroimaging studies have demonstrated pathological mechanisms related to cerebral neuroplasticity in chronic low back pain (CLBP). Few studies have compared cerebral changes between patients with ...
PMC10817838
core_pubmed_pmc
Advances in pediatric acute kidney injury pharmacology and nutrition: a report from the 26th Acute Disease Quality Initiative (ADQI) consensus conference
Advances in pediatric acute kidney injury pharmacology and nutrition: a report from the 26th Acute Disease Quality Initiative (ADQI) consensus conference Abstract Background In the past decade, there have been substantial advances in our understanding of pediatric AKI. Despite this progress, large gaps remain in our un...
PMC6161283
core_pubmed_pmc
Pharmacokinetic Drug-Drug Interaction and Responsible Mechanism between Memantine and Cimetidine
Pharmacokinetic Drug-Drug Interaction and Responsible Mechanism between Memantine and Cimetidine Abstract Abstract A sensitive and simple chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to evaluate memantine in rat plasma. Memantine and propranolol (internal standard) in rat plasma was extracted...
PMC9718561
core_pubmed_pmc
Multi-functional chitosan copolymer modified nanocrystals as oral andrographolide delivery systems for enhanced bioavailability and anti-inflammatory efficacy
Multi-functional chitosan copolymer modified nanocrystals as oral andrographolide delivery systems for enhanced bioavailability and anti-inflammatory efficacy Abstract Abstract Modifying nanocrystals with functional materials have been common strategy to enlarge the enhancing ability on oral absorption via nanocrystals...
PMC3945293
core_pubmed_pmc
Phase I study of sunitinib plus S-1 and cisplatin in Japanese patients with advanced or metastatic gastric cancer
Phase I study of sunitinib plus S-1 and cisplatin in Japanese patients with advanced or metastatic gastric cancer Abstract Summary Background This phase I, dose-finding study evaluated the maximum tolerated dose (MTD), safety, pharmacokinetics, and antitumor activity of sunitinib plus S-1/cisplatin in Japanese patients...
PMC4791805
core_pubmed_pmc
Immunodynamics: a cancer immunotherapy trials network review of immune monitoring in immuno-oncology clinical trials
Immunodynamics: a cancer immunotherapy trials network review of immune monitoring in immuno-oncology clinical trials Abstract The efficacy of PD-1/PD-L1 targeted therapies in addition to anti-CTLA-4 solidifies immunotherapy as a modality to add to the anticancer arsenal. Despite raising the bar of clinical efficacy, im...
PMC3665191
core_pubmed_pmc
Alternative medicine and anesthesia: Implications and considerations in daily practice
Alternative medicine and anesthesia: Implications and considerations in daily practice Abstract Abstract Nowadays, herbal medicines are widely used by most of the people, including the pre-surgical population. These medicines may pose numerous challenges during perioperative care. The objective of the current literatur...
PMC6450621
core_pubmed_pmc
Changes of drug pharmacokinetics mediated by downregulation of kidney organic cation transporters Mate1 and Oct2 in a rat model of hyperuricemia
Changes of drug pharmacokinetics mediated by downregulation of kidney organic cation transporters Mate1 and Oct2 in a rat model of hyperuricemia Abstract The effects of hyperuricemia on the expression of kidney drug transporters and on the pharmacokinetics of several substrate drugs were examined. We first established ...
PMC9706588
core_pubmed_pmc
Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review
Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review Abstract Abstract Rationale: Physiologically based pharmacokinetic (PBPK) and population pharmacokinetic (PK) modelling approaches are widely accepted in non-radiopharmaceutical drug development and r...
PMC5595947
core_pubmed_pmc
Metoprolol‐pridopidine drug–drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease
Metoprolol‐pridopidine drug–drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease Abstract Abstract Aims Pridopidine is an oral drug in clinical development for treatment of patients with Huntington's disease. This study examined the interactions of pridopidine wi...
PMC10454053
core_pubmed_pmc
β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes
β-Caryophyllene-Loaded Microemulsion-Based Topical Hydrogel: A Promising Carrier to Enhance the Analgesic and Anti-Inflammatory Outcomes Abstract Abstract Musculoskeletal pain and inflammation can vary from localised pain like pain in the shoulders and neck to widespread pain like fibromyalgia, and as per estimates, ar...
PMC7069473
core_pubmed_pmc
Implications for IV posaconazole dosing in the era of obesity
Implications for IV posaconazole dosing in the era of obesity Abstract Abstract Background The prevalence of obesity has shown a dramatic increase over recent decades. Obesity is associated with underdosing of antimicrobial drugs for prophylaxis and treatment. Posaconazole is a broad-spectrum triazole antifungal drug l...
PMC8301585
core_pubmed_pmc
First‐in‐human study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of ALPN‐101, a dual CD28/ICOS antagonist, in healthy adult subjects
First‐in‐human study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of ALPN‐101, a dual CD28/ICOS antagonist, in healthy adult subjects Abstract Abstract ALPN‐101 (ICOSL vIgD‐Fc) is an Fc fusion protein of a human inducible T cell costimulatory ligand (ICOSL) variant immunoglobulin domain (vIgD) de...
PMC3313063
core_pubmed_pmc
Successfully Improving Ocular Drug Delivery Using the Cationic Nanoemulsion, Novasorb
Successfully Improving Ocular Drug Delivery Using the Cationic Nanoemulsion, Novasorb Abstract Topical ophthalmic delivery of active ingredients can be achieved using cationic nanoemulsions. In the last decade, Novagali Pharma has successfully developed and marketed Novasorb, an advanced pharmaceutical technology for t...
PMC6235261
core_pubmed_pmc
Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs
Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs Abstract Two chemotypes were examined in vitro with CYPs 3A4 and 2C19 by molecular docking, metabolic profiles, and intrinsic clearance deuterium isotope effects wit...
PMC10885499
core_pubmed_pmc
External validation of the modified Marsh and Schnider models for medium-chain triglyceride propofol in target-controlled infusion anesthesia
External validation of the modified Marsh and Schnider models for medium-chain triglyceride propofol in target-controlled infusion anesthesia Abstract Abstract Background Propofol formulated with medium- and long-chain triglycerides (MCT/LCT propofol) has rapidly replaced propofol formulated with long-chain triglycerid...
PMC8633954
core_pubmed_pmc
Serum Predose Metabolic Profiling for Prediction of Rosuvastatin Pharmacokinetic Parameters in Healthy Volunteers
Serum Predose Metabolic Profiling for Prediction of Rosuvastatin Pharmacokinetic Parameters in Healthy Volunteers Abstract Rosuvastatin is a well-known lipid-lowering agent generally used for hypercholesterolemia treatment and coronary artery disease prevention. There is a substantial inter-individual variability in th...
PMC8194902
core_pubmed_pmc
Pharmacokinetic modelling to estimate intracellular favipiravir ribofuranosyl-5′-triphosphate exposure to support posology for SARS-CoV-2
Pharmacokinetic modelling to estimate intracellular favipiravir ribofuranosyl-5′-triphosphate exposure to support posology for SARS-CoV-2 Abstract Abstract Objectives Favipiravir has discrepant activity against SARS-CoV-2 in vitro , concerns about teratogenicity and pill burden, and an unknown optimal dose. This analys...
PMC5513855
core_pubmed_pmc
Bioequivalence of generic alendronate sodium tablets (70 mg) to Fosamax ® tablets (70 mg) in fasting, healthy volunteers: a randomized, open-label, three-way, reference-replicated crossover study
Bioequivalence of generic alendronate sodium tablets (70 mg) to Fosamax ® tablets (70 mg) in fasting, healthy volunteers: a randomized, open-label, three-way, reference-replicated crossover study Abstract Abstract Purpose The aim of this study was to evaluate the bioequivalence of a generic product 70 mg alendronate so...
PMC9706587
core_pubmed_pmc
Development of functional nanomedicines for tumor associated macrophages-focused cancer immunotherapy
Development of functional nanomedicines for tumor associated macrophages-focused cancer immunotherapy Abstract Abstract Clinical cancer immunotherapies are usually impeded by tumor immunosuppression driven by tumor associated macrophages (TAMs). Thus, TAMs can be considered as a promising therapeutic target for improve...
PMC8166202
core_pubmed_pmc
Polyphenolic-Rich Compounds From Dillenia pentagyna (Roxb.) Attenuates the Doxorubicin-Induced Cardiotoxicity: A High-Frequency Ultrasonography Assisted Approach
Polyphenolic-Rich Compounds From Dillenia pentagyna (Roxb.) Attenuates the Doxorubicin-Induced Cardiotoxicity: A High-Frequency Ultrasonography Assisted Approach Abstract Cardiovascular complications are the foremost concern in patients undergoing anticancer therapy . There is an unmet need to address the problems aris...
PMC8945304
core_pubmed_pmc
Antithymocyte globulin exposure in CD34 + T-cell–depleted allogeneic hematopoietic cell transplantation
Antithymocyte globulin exposure in CD34 + T-cell–depleted allogeneic hematopoietic cell transplantation Abstract Key Points In CD34 + TCD allogeneic-HCT, optimum post-HCT rATG exposure decreases NRM driven by faster CD4 + IR and improves survival. Personalized rATG exposure using a PK-directed strategy may improve surv...
PMC12963244
core_pubmed_pmc
Assessment of Vancomycin Penetration into Cerebrospinal Fluid in Patients with Ventriculitis Using a Physiologically Based Pharmacokinetic Approach
Assessment of Vancomycin Penetration into Cerebrospinal Fluid in Patients with Ventriculitis Using a Physiologically Based Pharmacokinetic Approach Abstract Introduction Vancomycin is an antimicrobial agent for treating central nervous system (CNS) infections caused by Gram-positive bacteria. Due to practical and ethic...
PMC6587702
core_pubmed_pmc
Rifampicin Alters Metformin Plasma Exposure but Not Blood Glucose Levels in Diabetic Tuberculosis Patients
Rifampicin Alters Metformin Plasma Exposure but Not Blood Glucose Levels in Diabetic Tuberculosis Patients Abstract The pharmacokinetic (PK) and clinical implications of combining metformin with rifampicin are relevant to increasing numbers of patients with diabetic tuberculosis ( TB ) across the world and are yet uncl...
PMC12888277
core_pubmed_pmc
Association between heavy metals exposure and depression: findings of the NHANES from 2003 to 2020
Association between heavy metals exposure and depression: findings of the NHANES from 2003 to 2020 Abstract Abstract Background Heavy metals are recognized neurotoxicants implicated in depression, yet limited research examines combined metal impacts. This study aimed to investigate the joint effect of heavy metals on d...
PMC8472364
core_pubmed_pmc
Pharmacokinetics of Levodopa and 3-O-Methyldopa in Parkinsonian Patients Treated with Levodopa and Ropinirole and in Patients with Motor Complications
Pharmacokinetics of Levodopa and 3-O-Methyldopa in Parkinsonian Patients Treated with Levodopa and Ropinirole and in Patients with Motor Complications Abstract Abstract Parkinson’s disease (PD) is a progressive, neurodegenerative disorder primarily affecting dopaminergic neuronal systems, with impaired motor function a...
PMC9946004
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of a Novel Vancomycin Derivative LYSC98 in a Murine Thigh Infection Model Against Staphylococcus aureus
Pharmacokinetics and Pharmacodynamics of a Novel Vancomycin Derivative LYSC98 in a Murine Thigh Infection Model Against Staphylococcus aureus Abstract Introduction LYSC98 is a novel vancomycin derivative used for gram-positive bacterial infections. Here we compared the antibacterial activity of LYSC98 with vancomycin a...
PMC10649908
core_pubmed_pmc
Ophthalmic Bimatoprost-Loaded Niosomal In Situ Gel: Preparation, Optimization, and In Vivo Pharmacodynamics Study
Ophthalmic Bimatoprost-Loaded Niosomal In Situ Gel: Preparation, Optimization, and In Vivo Pharmacodynamics Study Abstract Abstract This study aimed at formulating the antiglaucoma agent, Bimatoprost (BMT), into niosomal in situ gel (BMT-ISG) for ocular delivery. Niosomes containing cholesterol/span 60 entrapping BMT w...
PMC9132812
core_pubmed_pmc
Mapping the current evidence on the anesthetic management of adult patients with neuromuscular disorders—a scoping review
Mapping the current evidence on the anesthetic management of adult patients with neuromuscular disorders—a scoping review Abstract Abstract Purpose Patients with neuromuscular disorders (NMDs) are at increased risk of perioperative complications. The objective of this scoping review was to examine emerging evidence fro...
PMC3509396
core_pubmed_pmc
Enantiospecific ketoprofen concentrations in plasma after oral and intramuscular administration in growing pigs
Enantiospecific ketoprofen concentrations in plasma after oral and intramuscular administration in growing pigs Abstract Background Ketoprofen is a non-steroidal anti-inflammatory drug which has been widely used for domestic animals. Orally administered racemic ketoprofen has been reported to be absorbed well in pigs, ...
PMC10145343
core_pubmed_pmc
Current Update on Role of Hesperidin in Inflammatory Lung Diseases: Chemistry, Pharmacology, and Drug Delivery Approaches
Current Update on Role of Hesperidin in Inflammatory Lung Diseases: Chemistry, Pharmacology, and Drug Delivery Approaches Abstract Abstract Inflammation is a common feature of many respiratory diseases, such as pneumonia, asthma, pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), lung cancer, acute lung ...
PMC5263138
core_pubmed_pmc
Putative Membrane-Bound Transporters MFSD14A and MFSD14B Are Neuronal and Affected by Nutrient Availability
Putative Membrane-Bound Transporters MFSD14A and MFSD14B Are Neuronal and Affected by Nutrient Availability Abstract Characterization of orphan transporters is of importance due to their involvement in cellular homeostasis but also in pharmacokinetics and pharmacodynamics. The tissue and cellular localization, as well ...
PMC6352369
core_pubmed_pmc
17p deletion strongly influences rituximab elimination in chronic lymphocytic leukemia
17p deletion strongly influences rituximab elimination in chronic lymphocytic leukemia Abstract Chronic lymphocytic leukemia (CLL) is the most common type of leukemia and the anti-CD20 monoclonal antibody, rituximab, represents the therapeutic gold standard for more than 2 decades in this pathology, when used in combin...
PMC12925031
core_pubmed_pmc
A study to evaluate the impact of PB-119 injection (a pegylated exenatide formulation) on the pharmacokinetic profiles of Digoxin and Warfarin sodium in healthy subjects
A study to evaluate the impact of PB-119 injection (a pegylated exenatide formulation) on the pharmacokinetic profiles of Digoxin and Warfarin sodium in healthy subjects Abstract Objective: To evaluate the impact of multiple-dose PB-119 injection (a pegylated exenatide formulation) on the pharmacokinetics of single-dos...
PMC12193675
core_pubmed_pmc
In-silico study of approved drugs as potential inhibitors against 3CLpro and other viral proteins of CoVID-19
In-silico study of approved drugs as potential inhibitors against 3CLpro and other viral proteins of CoVID-19 Abstract Abstract The global pandemic, due to the emergence of COVID-19, has created a public health crisis. It has a huge morbidity rate that was never comprehended in the recent decades. Despite numerous effo...
PMC12079095
core_pubmed_pmc
A Phase I Dose-Escalation Study of the HIF-2 Alpha Inhibitor DFF332 in Patients with Advanced Clear-Cell Renal Cell Carcinoma
A Phase I Dose-Escalation Study of the HIF-2 Alpha Inhibitor DFF332 in Patients with Advanced Clear-Cell Renal Cell Carcinoma Abstract Abstract Purpose: Mutations or silencing of the von Hippel–Lindau tumor suppressor gene accumulate hypoxia-inducible factors (HIF). HIF-2α is implicated in the oncogenesis of ∼50% of pa...
PMC6099360
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic profile of the sodium‐glucose co‐transporter‐2 inhibitor empagliflozin in young people with Type 2 diabetes: a randomized trial
Pharmacokinetic and pharmacodynamic profile of the sodium‐glucose co‐transporter‐2 inhibitor empagliflozin in young people with Type 2 diabetes: a randomized trial Abstract Abstract Aims To assess the pharmacokinetic and pharmacodynamic profile of a single dose of empagliflozin in young people with Type 2 diabetes to i...
PMC7089466
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Considerations for Drugs Binding to Alpha-1-Acid Glycoprotein
Pharmacokinetic and Pharmacodynamic Considerations for Drugs Binding to Alpha-1-Acid Glycoprotein Abstract According to the free drug hypothesis only the unbound drug is available to act at physiological sites of action, and as such the importance of plasma protein binding primarily resides in its impact on pharmacokin...
PMC8096729
core_pubmed_pmc
Estimation of Ontogeny Functions for Renal Transporters Using a Combined Population Pharmacokinetic and Physiology-Based Pharmacokinetic Approach: Application to OAT1,3
Estimation of Ontogeny Functions for Renal Transporters Using a Combined Population Pharmacokinetic and Physiology-Based Pharmacokinetic Approach: Application to OAT1,3 Abstract To date, information on the ontogeny of renal transporters is limited. Here, we propose to estimate the in vivo functional ontogeny of transpo...
PMC4039091
core_pubmed_pmc
Pharmacokinetic Changes and Dosing Modification of Aminoglycosides in Critically Ill Obese Patients: A Literature Review
Pharmacokinetic Changes and Dosing Modification of Aminoglycosides in Critically Ill Obese Patients: A Literature Review Abstract Abstract The objective of the paper is to review the literature and provide recommendations for use of aminoglycoside antibiotics in critically ill obese patients. Literature search in PubMe...
PMC12393660
core_pubmed_pmc
A Phase 0 Window of Opportunity Trial of LB100, a Protein Phosphatase 2A Inhibitor, in Patients with Recurrent Gliomas
A Phase 0 Window of Opportunity Trial of LB100, a Protein Phosphatase 2A Inhibitor, in Patients with Recurrent Gliomas Abstract Abstract Background: LB100 is a protein phosphatase 2A (PP2A) inhibitor. Glioma models show inhibition of PP2A by LB100 causes cell death. Whether LB100 crosses the human blood brain barrier (...
PMC8683664
core_pubmed_pmc
In vivo pharmacokinetic study of remdesivir dry powder for inhalation in hamsters
In vivo pharmacokinetic study of remdesivir dry powder for inhalation in hamsters Abstract Remdesivir dry powder for inhalation was previously developed using thin film freezing (TFF). A single-dose 24-h pharmacokinetic study in hamsters demonstrated that pulmonary delivery of TFF remdesivir can achieve plasma remdesiv...
PMC5908175
core_pubmed_pmc
Nonclinical comparability studies of recombinant human arylsulfatase A addressing manufacturing process changes
Nonclinical comparability studies of recombinant human arylsulfatase A addressing manufacturing process changes Abstract Recombinant human arylsulfatase A (rhASA) is in clinical development for the treatment of patients with metachromatic leukodystrophy (MLD). Manufacturing process changes were introduced to improve ro...
PMC7851041
core_pubmed_pmc
Characterizing dynamics of serum creatinine and creatinine clearance in extremely low birth weight neonates during the first 6 weeks of life
Characterizing dynamics of serum creatinine and creatinine clearance in extremely low birth weight neonates during the first 6 weeks of life Abstract Abstract Background Characterizing the dynamics of serum creatinine concentrations (Scr) and associated creatinine clearance (CLcr) as a measure of kidney function in ext...
PMC7946667
core_pubmed_pmc
Effect of ceritinib on the pharmacokinetics of coadministered CYP3A and 2C9 substrates: a phase I, multicenter, drug–drug interaction study in patients with ALK + advanced tumors
Effect of ceritinib on the pharmacokinetics of coadministered CYP3A and 2C9 substrates: a phase I, multicenter, drug–drug interaction study in patients with ALK + advanced tumors Abstract Abstract Purpose Ceritinib is an ALK receptor tyrosine kinase inhibitor approved as first- and second-line treatment in adult patien...
PMC5315724
core_pubmed_pmc
Towards a Model-Based Dose Recommendation for Doxorubicin in Children
Towards a Model-Based Dose Recommendation for Doxorubicin in Children Abstract Following the publication of our paper regarding a population-based model of doxorubicin pharmacokinetics in children in Clinical Pharmacokinetics last year (Voller et al. 54:1139–1149, 2015 ), we have received many inquiries on the practica...
PMC8871704
core_pubmed_pmc
Amikacin Therapy in Japanese Pediatric Patients: Narrative Review
Amikacin Therapy in Japanese Pediatric Patients: Narrative Review Abstract Abstract Children show a very wide range of physical development processes. These changes impact pharmacokinetic (PK) variability in pediatric patients. Most PK studies have been conducted on the Caucasian population. Therefore, whether current ...
PMC4222830
core_pubmed_pmc
EMPIRICUS micafungin versus placebo during nosocomial sepsis in Candida multi-colonized ICU patients with multiple organ failures: study protocol for a randomized controlled trial
EMPIRICUS micafungin versus placebo during nosocomial sepsis in Candida multi-colonized ICU patients with multiple organ failures: study protocol for a randomized controlled trial Abstract Abstract Background The potential interest of antifungal treatment of non-immunocompromized patients with sepsis, extra-digestive C...
PMC5874838
core_pubmed_pmc
Pharmacokinetics and Scintigraphic Imaging of the Hypoxia-Imaging Agent [ 123 I]IAZA in Healthy Adults Following Exercise-Based Cardiac Stress †
Pharmacokinetics and Scintigraphic Imaging of the Hypoxia-Imaging Agent [ 123 I]IAZA in Healthy Adults Following Exercise-Based Cardiac Stress † Abstract The objective of this work is to evaluate the potential effect of cardiac stress exercise on the accumulation of [ 123 I]IAZA, a radiopharmaceutical used to image foc...
PMC6096965
core_pubmed_pmc
Pharmacokinetics of a Single Dose of Azilsartan in Pediatric Patients: A Phase 3, Open-Label, Multicenter Study
Pharmacokinetics of a Single Dose of Azilsartan in Pediatric Patients: A Phase 3, Open-Label, Multicenter Study Abstract Introduction Azilsartan is an angiotensin II receptor blocker indicated for the treatment of patients with hypertension. The efficacy and safety of azilsartan are established in adults, but have not ...
PMC5529745
core_pubmed_pmc
Advanced Methods for Dose and Regimen Finding During Drug Development: Summary of the EMA/EFPIA Workshop on Dose Finding (London 4–5 December 2014)
Advanced Methods for Dose and Regimen Finding During Drug Development: Summary of the EMA/EFPIA Workshop on Dose Finding (London 4–5 December 2014) Abstract Abstract Inadequate dose selection for confirmatory trials is currently still one of the most challenging issues in drug development, as illustrated by high rates ...
PMC8518515
core_pubmed_pmc
Grapiprant: A snapshot of the current knowledge
Grapiprant: A snapshot of the current knowledge Abstract Abstract Grapiprant is the pioneer member of the novel piprant class, a potent and specific antagonist of the prostaglandin E2 receptor 4. It has been approved in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in dogs ...
PMC10820135
core_pubmed_pmc
Pharmacokinetic, Tissue Distribution, Metabolite, and Toxicity Evaluation of the Matrine Derivative, (6aS, 10S, 11aR, 11bR, 11cS)-10-Methylaminododecahydro-3a, 7a-Diaza-benzo (de) Anthracene-8-thione
Pharmacokinetic, Tissue Distribution, Metabolite, and Toxicity Evaluation of the Matrine Derivative, (6aS, 10S, 11aR, 11bR, 11cS)-10-Methylaminododecahydro-3a, 7a-Diaza-benzo (de) Anthracene-8-thione Abstract MASM, a structurally modified derivative of matrine, exhibits superior efficacy in reducing inflammation and li...
PMC12321715
core_pubmed_pmc
Co-administration of nobiletin and tetrahydrocurcumin enhanced the cytotoxicity to breast cancer through inhibiting CYP1A1 enzyme: from the perspective of pharmacokinetic interactions
Co-administration of nobiletin and tetrahydrocurcumin enhanced the cytotoxicity to breast cancer through inhibiting CYP1A1 enzyme: from the perspective of pharmacokinetic interactions Abstract Background & objectives The introduction of traditional Chinese medicine to the treatment of breast cancer increases the risk o...
PMC12662413
core_pubmed_pmc
Daily mosnodenvir dosing as dengue prophylaxis in a human infection model
Daily mosnodenvir dosing as dengue prophylaxis in a human infection model Abstract Abstract Background: Antiviral prophylaxis or treatment is unavailable for dengue. We evaluated the antiviral activity, safety and pharmacokinetics of repeated oral doses of mosnodenvir (JNJ-64281802), a pan-serotype dengue antiviral, as...
PMC3280623
core_pubmed_pmc
Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings
Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings Abstract Abstract Integrase inhibitors represent an important new class of antiretroviral drugs. Elvitegravir, the second available integrase inhibitor to be submitted for regulatory approval appears to be...
PMC11218975
core_pubmed_pmc
The evolution of antimicrobial peptide resistance in Pseudomonas aeruginosa is severely constrained by random peptide mixtures
The evolution of antimicrobial peptide resistance in Pseudomonas aeruginosa is severely constrained by random peptide mixtures Abstract Abstract The prevalence of antibiotic-resistant pathogens has become a major threat to public health, requiring swift initiatives for discovering new strategies to control bacterial in...
PMC5445230
core_pubmed_pmc
Evaluating Dosage Optimality for Tofacitinib, an Oral Janus Kinase Inhibitor, in Plaque Psoriasis, and the Influence of Body Weight
Evaluating Dosage Optimality for Tofacitinib, an Oral Janus Kinase Inhibitor, in Plaque Psoriasis, and the Influence of Body Weight Abstract Abstract Tofacitinib is an oral Janus kinase inhibitor. An integrated analysis was conducted to evaluate dosage optimality for tofacitinib in patients with moderate‐to‐severe plaq...