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PMC7338550
core_pubmed_pmc
Pharmacodynamic and Metabolomics Studies on the Effect of Kouyanqing Granule in the Treatment of Phenol-Induced Oral Ulcer Worsened by Sleep Deprivation
Pharmacodynamic and Metabolomics Studies on the Effect of Kouyanqing Granule in the Treatment of Phenol-Induced Oral Ulcer Worsened by Sleep Deprivation Abstract Oral ulcers are the most prevalent oral mucosal diseases globally, and no specific treatment schemes are currently available due to the complexity of oral ulc...
PMC9099131
core_pubmed_pmc
Evaluation of the pharmacokinetics of trazpiroben (TAK‐906) in the presence and absence of the proton pump inhibitor esomeprazole
Evaluation of the pharmacokinetics of trazpiroben (TAK‐906) in the presence and absence of the proton pump inhibitor esomeprazole Abstract Abstract Trazpiroben, a dopamine D 2 /D 3 receptor antagonist under development to treat gastroparesis, displays decreasing solubility with increasing pH. This single‐sequence, open...
PMC8537252
core_pubmed_pmc
Dose- and Sex-Dependent Changes in Hemoglobin Oxygen Affinity by the Micronutrient 5-Hydroxymethylfurfural and α-Ketoglutaric Acid
Dose- and Sex-Dependent Changes in Hemoglobin Oxygen Affinity by the Micronutrient 5-Hydroxymethylfurfural and α-Ketoglutaric Acid Abstract Abstract 5-Hydroxymethylfurfural (5-HMF) is known to increase hemoglobin oxygen affinity (Hb–O 2 affinity) and to induce a left shift of the oxygen dissociation curve (ODC). It is ...
PMC5827733
core_pubmed_pmc
Integration of genome-scale metabolic networks into whole-body PBPK models shows phenotype-specific cases of drug-induced metabolic perturbation
Integration of genome-scale metabolic networks into whole-body PBPK models shows phenotype-specific cases of drug-induced metabolic perturbation Abstract Drug-induced perturbations of the endogenous metabolic network are a potential root cause of cellular toxicity. A mechanistic understanding of such unwanted side effe...
PMC6542580
core_pubmed_pmc
Quality Improvement Project to Reduce Drug-Related Problems (DRPs) and Potentially Inappropriate Medications (PIMs) in Geriatrics Cardiac Clinic in Saudi Arabia
Quality Improvement Project to Reduce Drug-Related Problems (DRPs) and Potentially Inappropriate Medications (PIMs) in Geriatrics Cardiac Clinic in Saudi Arabia Abstract Background Elderly people have a high risk of potentially inappropriate medications (PIMs) and drug-related problems (DRPs) due to polypharmacy, physi...
PMC7719361
core_pubmed_pmc
Fasting Status and Circadian Variation Must be Considered When Performing AUC‐based Therapeutic Drug Monitoring of Tacrolimus in Renal Transplant Recipients
Fasting Status and Circadian Variation Must be Considered When Performing AUC‐based Therapeutic Drug Monitoring of Tacrolimus in Renal Transplant Recipients Abstract Therapeutic drug monitoring (TDM) is mandatory for the immunosuppressive drug tacrolimus (Tac). For clinical applicability, TDM is performed using morning...
PMC8348927
core_pubmed_pmc
Development, Validation, and Application of the LC-MS/MS Method for Determination of 4-Acetamidobenzoic Acid in Pharmacokinetic Pilot Studies in Pigs
Development, Validation, and Application of the LC-MS/MS Method for Determination of 4-Acetamidobenzoic Acid in Pharmacokinetic Pilot Studies in Pigs Abstract Abstract Each drug has pharmacokinetics that must be defined for the substance to be used in humans and animals. Currently, one of the basic analytical tools for...
PMC9796890
core_pubmed_pmc
Individualised prophylaxis based on personalised target trough FVIII level optimised clinical outcomes in paediatric patients with severe haemophilia A
Individualised prophylaxis based on personalised target trough FVIII level optimised clinical outcomes in paediatric patients with severe haemophilia A Abstract Abstract Introduction As standard care of severe haemophilia A (SHA), prophylaxis should be individualised. Aim This study aimed to investigate the effectivene...
PMC5739138
core_pubmed_pmc
Cancer Chemopreventive Effects of Boswellia sacra Gum Resin Hydrodistillates on Invasive Urothelial Cell Carcinoma: Report of a Case
Cancer Chemopreventive Effects of Boswellia sacra Gum Resin Hydrodistillates on Invasive Urothelial Cell Carcinoma: Report of a Case Abstract A 52-year-old Hispanic male presented with hematuria and was later diagnosed with a large invasive high-grade urothelial cell carcinoma (UCC) of the urinary bladder, but with amb...
PMC10514109
core_pubmed_pmc
OCE-205, A Novel, Selective Vasopressin Receptor Mixed Agonist-Antagonist: Safety, Tolerability, and Pharmacokinetics/Pharmacodynamics from a Phase 1 Study in Healthy Volunteers
OCE-205, A Novel, Selective Vasopressin Receptor Mixed Agonist-Antagonist: Safety, Tolerability, and Pharmacokinetics/Pharmacodynamics from a Phase 1 Study in Healthy Volunteers Abstract Abstract Background OCE-205, a novel, selective vasopressin V1a receptor mixed agonist/antagonist with no V2 receptor activity, may t...
PMC12951577
core_pubmed_pmc
Discovery of EGT710, an Oral Nonpeptidomimetic Reversible Covalent SARS-CoV‑2 Main Protease Inhibitor
Discovery of EGT710, an Oral Nonpeptidomimetic Reversible Covalent SARS-CoV‑2 Main Protease Inhibitor Abstract Abstract The coronavirus main protease (3CL pro , M pro , nsp5) is a highly conserved cysteine protease unique to the Coronaviridae family, including SARS-CoV-2, and is a validated target for the treatment of ...
PMC6019389
core_pubmed_pmc
Computational quantum chemistry, molecular docking, and ADMET predictions of imidazole alkaloids of Pilocarpus microphyllus with schistosomicidal properties
Computational quantum chemistry, molecular docking, and ADMET predictions of imidazole alkaloids of Pilocarpus microphyllus with schistosomicidal properties Abstract Schistosomiasis affects million people and its control is widely dependent on a single drug, praziquantel. Computational chemistry has led to the developm...
PMC10427982
core_pubmed_pmc
Transfer and biotransformation of the COVID-19 prodrug molnupiravir and its metabolite β-D-N4-hydroxycytidine across the blood-placenta barrier
Transfer and biotransformation of the COVID-19 prodrug molnupiravir and its metabolite β-D-N4-hydroxycytidine across the blood-placenta barrier Abstract Summary Background Molnupiravir is an orally bioavailable prodrug of the nucleoside analogue β-D-N4-hydroxycytidine (NHC) and is used to treat coronavirus disease 2019...
PMC12314526
core_pubmed_pmc
Azenosertib Is a Potent and Selective WEE1 Kinase Inhibitor with Broad Antitumor Activity Across a Range of Solid Tumors
Azenosertib Is a Potent and Selective WEE1 Kinase Inhibitor with Broad Antitumor Activity Across a Range of Solid Tumors Abstract Abstract Genomic instability and accumulation of DNA damage are hallmarks of tumor development and progression. To ensure the maintenance of genomic integrity, cells rely on a coordinated DN...
PMC3497345
core_pubmed_pmc
Tanshinones: Sources, Pharmacokinetics and Anti-Cancer Activities
Tanshinones: Sources, Pharmacokinetics and Anti-Cancer Activities Abstract Abstract Tanshinones are a class of abietane diterpene compound isolated from Salvia miltiorrhiza (Danshen or Tanshen in Chinese), a well-known herb in Traditional Chinese Medicine (TCM). Since they were first identified in the 1930s, more than ...
PMC10815480
core_pubmed_pmc
Agri-Food Waste Recycling for Healthy Remedies: Biomedical Potential of Nutraceuticals from Unripe Tomatoes ( Solanum lycopersicum L.)
Agri-Food Waste Recycling for Healthy Remedies: Biomedical Potential of Nutraceuticals from Unripe Tomatoes ( Solanum lycopersicum L.) Abstract Abstract Unripe tomatoes represent an agri-food waste resulting from industrial by-processing products of tomatoes, yielding products with a high content of bioactive compounds...
PMC8940246
core_pubmed_pmc
A Computational Framework for Studying Gut-Brain Axis in Autism Spectrum Disorder
A Computational Framework for Studying Gut-Brain Axis in Autism Spectrum Disorder Abstract Abstract Introduction The integrity of the intestinal epithelium is crucial for human health and is harmed in autism spectrum disorder (ASD). An aberrant gut microbial composition resulting in gut-derived metabolic toxins was fou...
PMC7382813
core_pubmed_pmc
Herb–drug interactions between the medicinal mushrooms Lingzhi and Yunzhi and cytotoxic anticancer drugs: a systematic review
Herb–drug interactions between the medicinal mushrooms Lingzhi and Yunzhi and cytotoxic anticancer drugs: a systematic review Abstract Abstract Background Lingzhi and Yunzhi are medicinal mushrooms commonly used with cytotoxic chemotherapy in cancer patients in Asian countries. The current systematic review aims to ide...
PMC10188103
core_pubmed_pmc
Effect of flowing water on the pharmacokinetic properties of norfloxacin in channel catfish ( Ictalurus punctatus ) after single‐dose oral administration
Effect of flowing water on the pharmacokinetic properties of norfloxacin in channel catfish ( Ictalurus punctatus ) after single‐dose oral administration Abstract Abstract Background The recirculating aquaculture system (RAS) is a widely used, water‐saving and efficient aquaculture model. However, bacterial diseases ar...
PMC6824349
core_pubmed_pmc
Pharmacokinetics of Prolonged-Release Once-Daily Formulations of Tacrolimus in De Novo Kidney Transplant Recipients: A Randomized, Parallel-Group, Open-Label, Multicenter Study
Pharmacokinetics of Prolonged-Release Once-Daily Formulations of Tacrolimus in De Novo Kidney Transplant Recipients: A Randomized, Parallel-Group, Open-Label, Multicenter Study Abstract Abstract Introduction Different prolonged-release formulations of tacrolimus are available. To date, the pharmacokinetic (PK) profile ...
PMC5063900
core_pubmed_pmc
A phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-063, a selective PDE10A inhibitor
A phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-063, a selective PDE10A inhibitor Abstract Abstract Rationale Schizophrenia is a complex neuropsychiatric disorder characterized, in part, by impaired dopamine signaling. TAK-063 is a selective inhibitor of phosphodiesterase 10A,...
PMC7184160
core_pubmed_pmc
Phase 1 trial of vorolanib (CM082) in combination with everolimus in patients with advanced clear-cell renal cell carcinoma
Phase 1 trial of vorolanib (CM082) in combination with everolimus in patients with advanced clear-cell renal cell carcinoma Abstract Abstract Background Vorolanib (X-82, CM082) is a multi-target tyrosine kinase inhibitor. This study aimed to evaluate the tolerability, safety, pharmacokinetics and antitumor activities o...
PMC9032858
core_pubmed_pmc
GC-MS Profiling, Vibriocidal, Antioxidant, Antibiofilm, and Anti-Quorum Sensing Properties of Carum carvi L. Essential Oil: In Vitro and In Silico Approaches
GC-MS Profiling, Vibriocidal, Antioxidant, Antibiofilm, and Anti-Quorum Sensing Properties of Carum carvi L. Essential Oil: In Vitro and In Silico Approaches Abstract Abstract The main objectives of the present study were to investigate anti- Vibrio spp., antibiofilms, and anti-quorum-sensing (anti-QS) properties of ca...
PMC9689687
core_pubmed_pmc
Sex and Age Influence on Association of CYP450 Polymorphism with Midazolam Levels in Critically Ill Children
Sex and Age Influence on Association of CYP450 Polymorphism with Midazolam Levels in Critically Ill Children Abstract Abstract Midazolam is a drug that is metabolized by cytochrome P450 (CYP450) enzymes, particularly CYP3A4 and CYP3A5. The present study aimed to determine the sex and age influence on association of CYP...
PMC7601100
core_pubmed_pmc
Pharmacokinetic Principles and Their Application to Central Nervous System Tumors
Pharmacokinetic Principles and Their Application to Central Nervous System Tumors Abstract Abstract Despite increasing knowledge of the biologic drivers of central nervous system tumors, most targeted agents trialed to date have not shown activity against these tumors in clinical trials. To effectively treat central ne...
PMC12811158
core_pubmed_pmc
Anti-cryptosporidial efficacy of tricyclic carbazole aminoalcohols in vitro and in vivo
Anti-cryptosporidial efficacy of tricyclic carbazole aminoalcohols in vitro and in vivo Abstract Cryptosporidiosis is a major cause of diarrheal disease in humans and animals, yet there are no fully effective drugs, particularly for immunocompromised patients. Carbazole aminoalcohols (CAAs) are a relatively unexplored ...
PMC8290241
core_pubmed_pmc
ADME gene polymorphisms do not influence the pharmacokinetics of docetaxel: Results from a population pharmacokinetic study in Indian cancer patients
ADME gene polymorphisms do not influence the pharmacokinetics of docetaxel: Results from a population pharmacokinetic study in Indian cancer patients Abstract Abstract Background Pharmacokinetics (PK) of docetaxel is characterized by high inter‐individual variability (IIV). While covariate models that explain the PK va...
PMC10806122
core_pubmed_pmc
Pharmacokinetics of recombinant human annexin A5 (SY-005) in patients with severe COVID-19
Pharmacokinetics of recombinant human annexin A5 (SY-005) in patients with severe COVID-19 Abstract Objective: Annexin A5 is a phosphatidylserine binding protein with anti-inflammatory, anticoagulant and anti-apoptotic properties. Preclinical studies have shown that annexin A5 inhibits pro-inflammatory responses and im...
PMC8481692
core_pubmed_pmc
Quantitative Multiparametric MRI as an Imaging Biomarker for the Prediction of Breast Cancer Receptor Status and Molecular Subtypes
Quantitative Multiparametric MRI as an Imaging Biomarker for the Prediction of Breast Cancer Receptor Status and Molecular Subtypes Abstract Abstract Objectives To assess breast cancer receptor status and molecular subtypes by using the CAIPIRINHA-Dixon-TWIST-VIBE and readout-segmented echo-planar diffusion weighted im...
PMC4602450
core_pubmed_pmc
High Phenobarbital Clearance During Continuous Renal Replacement Therapy
High Phenobarbital Clearance During Continuous Renal Replacement Therapy Abstract Abstract Phenobarbital is an old antiepileptic drug used in severe epilepsy. Despite this, little is written about the need for dose adjustments in renal replacement therapy. Most sources recommend a moderately increased dose guided by th...
PMC12478598
core_pubmed_pmc
Pharmacokinetics and Safety of Pelacarsen, a GalNAc 3 ‐Conjugated Antisense Oligonucleotide Targeting Apo(a), in Participants With Mild Hepatic Impairment
Pharmacokinetics and Safety of Pelacarsen, a GalNAc 3 ‐Conjugated Antisense Oligonucleotide Targeting Apo(a), in Participants With Mild Hepatic Impairment Abstract ABSTRACT Pelacarsen, an antisense oligonucleotide, directly inhibits plasma lipoprotein(a) production; however, it remains unknown whether hepatic impairmen...
PMC10548181
core_pubmed_pmc
EGFR and PI3K/m-TOR inhibitors: design, microwave assisted synthesis and anticancer activity of thiazole–coumarin hybrids †
EGFR and PI3K/m-TOR inhibitors: design, microwave assisted synthesis and anticancer activity of thiazole–coumarin hybrids † Abstract Abstract A series of thiazoline and thiazolidinone-based 4-hydroxycoumarin derivatives were synthesized using both conventional synthesis procedures and microwave-assisted techniques. The...
PMC12481716
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, immunogenicity and pharmacodynamics of 9MW1911, an anti-ST2 monoclonal antibody: results from a first-in-human phase 1 study
Safety, tolerability, pharmacokinetics, immunogenicity and pharmacodynamics of 9MW1911, an anti-ST2 monoclonal antibody: results from a first-in-human phase 1 study Abstract Background 9MW1911 is a high-affinity human IgG4 monoclonal antibody targeting ST2, the human IL-33 receptor. It may have anti-inflammatory effect...
PMC8969250
core_pubmed_pmc
Pharmacokinetics studies of eugenol in Pacific white shrimp ( Litopenaeus vannamei ) after immersion bath
Pharmacokinetics studies of eugenol in Pacific white shrimp ( Litopenaeus vannamei ) after immersion bath Abstract Abstract Background Eugenol is the most commonly used plant anesthetic to relieve the stressors during various aquaculture procedures. This study aims to investigate the pharmacokinetics of eugenol in Paci...
PMC7144330
core_pubmed_pmc
2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors
2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors Abstract Abstract A novel 2-thiopyrimidine/chalcone hybrid was designed, synthesised, and evaluated for their cytotoxic activities against three different cell lines, K-562, MCF-7, and HT-29. The...
PMC12085675
core_pubmed_pmc
In silico screening of naturally derived dietary compounds as potential butyrylcholinesterase inhibitors for Alzheimer’s disease treatment
In silico screening of naturally derived dietary compounds as potential butyrylcholinesterase inhibitors for Alzheimer’s disease treatment Abstract Abstract Alzheimer’s disease (AD) is a progressive neurodegenerative condition that causes a substantial decline in cognitive functions and affects memory, thinking abiliti...
PMC11739751
core_pubmed_pmc
A Novel Step‐Up Dosage Regimen for Enhancing the Benefit‐to‐Risk Ratio of Mosunetuzumab in Relapsed or Refractory Follicular Lymphoma
A Novel Step‐Up Dosage Regimen for Enhancing the Benefit‐to‐Risk Ratio of Mosunetuzumab in Relapsed or Refractory Follicular Lymphoma Abstract Abstract Mosunetuzumab, a T‐cell engaging bispecific antibody targeting CD20xCD3, is approved for treating relapsed/refractory follicular lymphoma. This research supports the ap...
PMC7408157
core_pubmed_pmc
Approaches to Dose Finding in Neonates, Illustrating the Variability between Neonatal Drug Development Programs
Approaches to Dose Finding in Neonates, Illustrating the Variability between Neonatal Drug Development Programs Abstract Drug dosing in neonates should be based on integrated knowledge concerning the disease to be treated, the physiological characteristics of the neonate, and the pharmacokinetics (PK) and pharmacodynam...
PMC7298054
core_pubmed_pmc
Predicted effect of ticagrelor on the pharmacokinetics of dabigatran etexilate using physiologically based pharmacokinetic modeling
Predicted effect of ticagrelor on the pharmacokinetics of dabigatran etexilate using physiologically based pharmacokinetic modeling Abstract Dabigatran etexilate (DABE) is a direct oral anticoagulant (DOAC) and may be combined with ticagrelor, a P2Y 12 inhibitor with antiplatelet effects. This combination of antiplatel...
PMC3682108
core_pubmed_pmc
Efficacy and safety of intravenous daptomycin in Japanese patients with skin and soft tissue infections
Efficacy and safety of intravenous daptomycin in Japanese patients with skin and soft tissue infections Abstract Daptomycin is a lipopeptide antibiotic active against gram-positive organisms and recently approved for marketing in Japan. This study investigates the efficacy and safety of daptomycin in Japanese patients ...
PMC10698746
core_pubmed_pmc
Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent
Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent Abstract Lenacapavir (LEN) is a picomolar first-in-class capsid inhibitor of human immunodeficiency virus type 1 (HIV-1) with a mult...
PMC7825190
core_pubmed_pmc
Examination of Physiologically‐Based Pharmacokinetic Models of Rosuvastatin
Examination of Physiologically‐Based Pharmacokinetic Models of Rosuvastatin Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) modeling is increasingly used to predict drug disposition and drug–drug interactions (DDIs). However, accurately predicting the pharmacokinetics of transporter substrates and transp...
PMC3909249
core_pubmed_pmc
A phase 1 study of the BCL2-targeted deoxyribonucleic acid inhibitor (DNAi) PNT2258 in patients with advanced solid tumors
A phase 1 study of the BCL2-targeted deoxyribonucleic acid inhibitor (DNAi) PNT2258 in patients with advanced solid tumors Abstract Purpose Maximum tolerated dose, safety, pharmacokinetics, and pharmacodynamics were assessed in this phase 1 study of PNT2258, a BCL-2-targeted liposomal formulation of a 24-base DNA oligo...
PMC12025118
core_pubmed_pmc
Ethnic Sensitivity Assessment of Mosunetuzumab Pharmacokinetics and Pharmacodynamics in Chinese Patients With Relapsed or Refractory Follicular Lymphoma
Ethnic Sensitivity Assessment of Mosunetuzumab Pharmacokinetics and Pharmacodynamics in Chinese Patients With Relapsed or Refractory Follicular Lymphoma Abstract ABSTRACT Mosunetuzumab, a CD20 × CD3 T‐cell‐engaging bispecific antibody, redirects T cells to eliminate malignant B cells. The purpose of YO43555 was to asse...
PMC4153969
core_pubmed_pmc
A Novel Suspension Formulation Enhances Intestinal Absorption of Macromolecules Via Transient and Reversible Transport Mechanisms
A Novel Suspension Formulation Enhances Intestinal Absorption of Macromolecules Via Transient and Reversible Transport Mechanisms Abstract Purpose Medium chain fatty acid salts promote absorption by increasing paracellular permeability of the intestinal epithelium. Novel oily suspension (OS) formulation disperses a pow...
PMC11661530
core_pubmed_pmc
Pharmacogenetics of colorectal cancer in a third-level hospital in Valencia
Pharmacogenetics of colorectal cancer in a third-level hospital in Valencia Abstract Abstract Objectives Genetic variants with associated pharmacokinetic and pharmacodynamic effects have an impact on the development of adverse drug reactions and survival of patients with colorectal cancer. Methods A selection of geneti...
PMC8258972
core_pubmed_pmc
Stereoselective ketamine effect on cardiac output: a population pharmacokinetic/pharmacodynamic modelling study in healthy volunteers
Stereoselective ketamine effect on cardiac output: a population pharmacokinetic/pharmacodynamic modelling study in healthy volunteers Abstract Abstract Background Ketamine has cardiac excitatory side-effects. Currently, data on the effects of ketamine and metabolite concentrations on cardiac output are scarce. We there...
PMC9539985
core_pubmed_pmc
Treatment of anemia associated with chronic kidney disease with the HIF prolyl hydroxylase inhibitor enarodustat: A review of the evidence
Treatment of anemia associated with chronic kidney disease with the HIF prolyl hydroxylase inhibitor enarodustat: A review of the evidence Abstract Abstract Enarodustat, a newly developed hypoxia‐inducible factor prolyl hydroxylase inhibitor, is used in clinical practice in Japan. Several clinical studies showed that e...
PMC7250461
core_pubmed_pmc
Estimation of Drug Pharmacokinetics from Breast Feeding: A Simple Method Based on Meta-analysis
Estimation of Drug Pharmacokinetics from Breast Feeding: A Simple Method Based on Meta-analysis Abstract Background: In resource-limited settings, breastfeeding is the healthiest source of nutrition for newborns. For economic/cultural reasons, breastfeeding is the preferred option for the majority of mothers, including...
PMC5762620
core_pubmed_pmc
Quantification of neomangiferin in rat plasma by liquid chromatography–tandem mass spectrometry and its application to bioavailability study ☆
Quantification of neomangiferin in rat plasma by liquid chromatography–tandem mass spectrometry and its application to bioavailability study ☆ Abstract Abstract Neomangiferin, a natural C-glucosyl xanthone, has recently received a great deal of attention due to its multiple biological activities. In this study, a rapid...
PMC11509893
core_pubmed_pmc
Acacetin, a Natural Flavone with Potential in Improving Liver Disease Based on Its Anti-Inflammation, Anti-Cancer, Anti-Infection and Other Effects
Acacetin, a Natural Flavone with Potential in Improving Liver Disease Based on Its Anti-Inflammation, Anti-Cancer, Anti-Infection and Other Effects Abstract Liver disease is a global public problem, and the cost of its therapy is a large financial burden to governments. It is well known that drug therapy plays a critic...
PMC4153582
core_pubmed_pmc
Development of a Physiologically Based Model to Describe the Pharmacokinetics of Methylphenidate in Juvenile and Adult Humans and Nonhuman Primates
Development of a Physiologically Based Model to Describe the Pharmacokinetics of Methylphenidate in Juvenile and Adult Humans and Nonhuman Primates Abstract The widespread usage of methylphenidate (MPH) in the pediatric population has received considerable attention due to its potential effect on child development. For...
PMC11864782
core_pubmed_pmc
A review of mathematical modeling of bone remodeling from a systems biology perspective
A review of mathematical modeling of bone remodeling from a systems biology perspective Abstract Abstract Bone remodeling is an essential, delicately balanced physiological process of coordinated activity of bone cells that remove and deposit new bone tissue in the adult skeleton. Due to the complex nature of this proc...
PMC10043546
core_pubmed_pmc
Safety and Tolerability of Antimicrobial Agents in the Older Patient
Safety and Tolerability of Antimicrobial Agents in the Older Patient Abstract Abstract Older patients are at high risk of infections, which often present atypically and are associated with high morbidity and mortality. Antimicrobial treatment in older individuals with infectious diseases represents a clinical challenge...
PMC11636299
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetics of Intravenous Sodium Taurodeoxycholate, HY209, a GPCR19 Agonist Inhibiting Inflammasomal Activation
Safety, Tolerability and Pharmacokinetics of Intravenous Sodium Taurodeoxycholate, HY209, a GPCR19 Agonist Inhibiting Inflammasomal Activation Abstract Background HY209 is a synthesized sodium taurodeoxycholate (TDCA) that is expected to serve as a novel treatment for sepsis by inhibiting the inflammasomal activation t...
PMC8624081
core_pubmed_pmc
Transplant Prognosis in Kidney Transplant Recipients with Diabetes under Mycophenolic Acid-Focused Therapeutic Drug Monitoring
Transplant Prognosis in Kidney Transplant Recipients with Diabetes under Mycophenolic Acid-Focused Therapeutic Drug Monitoring Abstract Abstract Mycophenolate mofetil is a key immunosuppressant that is metabolized into mycophenolic acid (MPA). The prognostic impact of MPA-focused therapeutic drug monitoring on allograf...
PMC10512912
core_pubmed_pmc
Impact of amiodarone use on metoprolol concentrations, α‐OH ‐metoprolol concentrations, metoprolol dosing and heart rate: A cross‐sectional study
Impact of amiodarone use on metoprolol concentrations, α‐OH ‐metoprolol concentrations, metoprolol dosing and heart rate: A cross‐sectional study Abstract Abstract Small studies suggest that amiodarone is a weak inhibitor of cytochrome P450 (CYP) 2D6. Inhibition of CYP2D6 leads to increases in concentrations of drugs m...
PMC8633703
core_pubmed_pmc
Gender Variations in Pharmacokinetics of Paracetamol in Hausa/Fulani Ethnic group in Northwest Nigeria – A Two-stage Approach
Gender Variations in Pharmacokinetics of Paracetamol in Hausa/Fulani Ethnic group in Northwest Nigeria – A Two-stage Approach Abstract Abstract Background: Paracetamol is one of the most commonly used drugs worldwide and has been linked to drug-related liver damage, even when taken at recommended doses. Ingesting the u...
PMC6543612
core_pubmed_pmc
Intracranial antitumor responses of nivolumab and ipilimumab: a pharmacodynamic and pharmacokinetic perspective, a scoping systematic review
Intracranial antitumor responses of nivolumab and ipilimumab: a pharmacodynamic and pharmacokinetic perspective, a scoping systematic review Abstract Abstract Background Recently, two phase II trials showed intracranial activity of the immune checkpoint inhibitors nivolumab and ipilimumab in patients with melanoma brai...
PMC10225205
core_pubmed_pmc
FIGHT‐102: A phase 1 study of pemigatinib in Japanese patients with advanced malignancies
FIGHT‐102: A phase 1 study of pemigatinib in Japanese patients with advanced malignancies Abstract Abstract Background FIGHT‐102 was a phase 1, dose‐escalation, dose‐expansion study of pemigatinib in Japanese patients with advanced solid tumors. Here, we report safety, tolerability, and preliminary efficacy of pemigati...
PMC12402800
core_pubmed_pmc
Preclinical Modeling of Navtemadlin Pharmacokinetics, Pharmacodynamics, and Efficacy in IDH–Wild-type Glioblastoma
Preclinical Modeling of Navtemadlin Pharmacokinetics, Pharmacodynamics, and Efficacy in IDH–Wild-type Glioblastoma Abstract Abstract Purpose: Navtemadlin is a potent small-molecule inhibitor of MDM2, which has completed a phase 0 window-of-opportunity study in glioblastoma (GBM). To optimally interpret the clinical dat...
PMC9291755
core_pubmed_pmc
The Effect of Food on the Pharmacokinetics of the Potassium‐Competitive Acid Blocker Vonoprazan
The Effect of Food on the Pharmacokinetics of the Potassium‐Competitive Acid Blocker Vonoprazan Abstract Abstract Herein, we report a food‐effect study of vonoprazan, an oral potassium‐competitive acid blocker. In a phase 1, randomized, open‐label, crossover study, healthy subjects received a single 20‐mg dose of vonop...
PMC12707156
core_pubmed_pmc
A Phase I Dose-Escalation Study of the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Oral Dose of Tigulixostat
A Phase I Dose-Escalation Study of the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Oral Dose of Tigulixostat Abstract Aim Tigulixostat is a promising selective xanthine oxidase inhibitor under clinical development for the treatment of hyperuricemia. The aim of this study was to evaluate the pharmacokinet...
PMC8082176
core_pubmed_pmc
Pharmacokinetics, Bioavailability, Excretion and Metabolism Studies of Akebia Saponin D in Rats: Causes of the Ultra-Low Oral Bioavailability and Metabolic Pathway
Pharmacokinetics, Bioavailability, Excretion and Metabolism Studies of Akebia Saponin D in Rats: Causes of the Ultra-Low Oral Bioavailability and Metabolic Pathway Abstract Background: Akebia saponin D (ASD) has a variety of biological activities and great medicinal potential, but its oral bioavailability is so low as ...
PMC12710159
core_pubmed_pmc
Andrias Davidianus Peptide Hydrogel Enables Sustained SR9011 Release to Promote Efferocytosis and Alleviate Colitis
Andrias Davidianus Peptide Hydrogel Enables Sustained SR9011 Release to Promote Efferocytosis and Alleviate Colitis Abstract Abstract Ulcerative colitis (UC) is a chronic inflammatory disorder marked by epithelial barrier disruption and defective resolution of inflammation. Although epithelial apoptosis and impaired ef...
PMC7266983
core_pubmed_pmc
Individualized Dosing With High Inter-Occasion Variability Is Correctly Handled With Model-Informed Precision Dosing—Using Rifampicin as an Example
Individualized Dosing With High Inter-Occasion Variability Is Correctly Handled With Model-Informed Precision Dosing—Using Rifampicin as an Example Abstract Abstract Rifampicin exhibits complexities in its pharmacokinetics (PK), including high inter-occasion variability (IOV), which is challenging for dose individualiz...
PMC9914177
core_pubmed_pmc
New antibiotics for the treatment of nonfermenting Gram-negative bacteria
New antibiotics for the treatment of nonfermenting Gram-negative bacteria Abstract Purpose of review To discuss the current literature on novel agents for the treatment of carbapenem-resistant nonfermenting Gram-negative bacteria (NF-GNB) infections. Recent findings Some novel agents have recently become available that...
PMC7027977
core_pubmed_pmc
Exposure–Response Analyses for Upadacitinib Efficacy and Safety in the Crohn's Disease CELEST Study and Bridging to the Extended‐Release Formulation
Exposure–Response Analyses for Upadacitinib Efficacy and Safety in the Crohn's Disease CELEST Study and Bridging to the Extended‐Release Formulation Abstract Upadacitinib plasma concentrations, efficacy, and safety data from 216 subjects with moderate‐to‐severe active Crohn's disease (CD) from the 16‐week induction per...
PMC11294067
core_pubmed_pmc
Impact of the Reference Multiple-Time-Point Dosimetry Protocol on the Validity of Single-Time-Point Dosimetry for [ 177 Lu]Lu-PSMA-I&T Therapy
Impact of the Reference Multiple-Time-Point Dosimetry Protocol on the Validity of Single-Time-Point Dosimetry for [ 177 Lu]Lu-PSMA-I&T Therapy Abstract Abstract Internal dosimetry supports safe and effective patient management during radionuclide therapy. Yet, it is associated with high clinical workload, costs, and pa...
PMC10153433
core_pubmed_pmc
Antihypertensive drugs and brain function: mechanisms underlying therapeutically beneficial and harmful neuropsychiatric effects
Antihypertensive drugs and brain function: mechanisms underlying therapeutically beneficial and harmful neuropsychiatric effects Abstract Abstract A bidirectional relationship exists between hypertension and psychiatric disorders, including unipolar and bipolar depression, anxiety, post-traumatic stress disorder (PTSD)...
PMC9291514
core_pubmed_pmc
Unanticipated CNS Safety Signal in a Placebo‐Controlled, Randomized Trial of Co‐Administered Atovaquone‐Proguanil and Amodiaquine
Unanticipated CNS Safety Signal in a Placebo‐Controlled, Randomized Trial of Co‐Administered Atovaquone‐Proguanil and Amodiaquine Abstract Abstract Atovaquone‐proguanil (ATV‐PG) plus amodiaquine (AQ) has been considered as a potential replacement for sulfadoxine‐pyrimethamine plus AQ for seasonal malaria chemopreventio...
PMC2911773
core_pubmed_pmc
A multi-center, randomized, double-blind, parallel, placebo-controlled trial to evaluate the efficacy, safety, and pharmacokinetics of intravenous ibuprofen for the treatment of fever in critically ill and non-critically ill adults
A multi-center, randomized, double-blind, parallel, placebo-controlled trial to evaluate the efficacy, safety, and pharmacokinetics of intravenous ibuprofen for the treatment of fever in critically ill and non-critically ill adults Abstract Abstract Introduction Hospitalized patients are often unable to ingest or toler...
PMC11096448
core_pubmed_pmc
Physiologically based pharmacokinetic modeling to predict the pharmacokinetics of codeine in different CYP2D6 phenotypes
Physiologically based pharmacokinetic modeling to predict the pharmacokinetics of codeine in different CYP2D6 phenotypes Abstract Objectives Codeine, a prodrug used as an opioid agonist, is metabolized to the active product morphine by CYP2D6. This study aimed to establish physiologically based pharmacokinetic (PBPK) m...
PMC6139604
core_pubmed_pmc
A feasibility study prior to an international multicentre paediatric study to assess pharmacokinetic/pharmacodynamic sampling and sample preparation procedures, logistics and bioanalysis
A feasibility study prior to an international multicentre paediatric study to assess pharmacokinetic/pharmacodynamic sampling and sample preparation procedures, logistics and bioanalysis Abstract Abstract Background Variability in pre-analytical procedures such as blood sampling, sample preparation and transport can su...
PMC11011161
core_pubmed_pmc
Linezolid Population Pharmacokinetic Model in Plasma and Cerebrospinal Fluid Among Patients With Tuberculosis Meningitis
Linezolid Population Pharmacokinetic Model in Plasma and Cerebrospinal Fluid Among Patients With Tuberculosis Meningitis Abstract Abstract Background Linezolid is evaluated in novel treatment regimens for tuberculous meningitis (TBM). Linezolid pharmacokinetics have not been characterized in this population, particular...
PMC8694443
core_pubmed_pmc
Ecological HPLC method for analyzing an antidiabetic drug in real rat plasma samples and studying the effects of concurrently administered fenugreek extract on its pharmacokinetics
Ecological HPLC method for analyzing an antidiabetic drug in real rat plasma samples and studying the effects of concurrently administered fenugreek extract on its pharmacokinetics Abstract Currently, the total number of diabetic people worldwide is constantly increasing. Metformin (MET) is known to be a first-line ant...
PMC7573825
core_pubmed_pmc
Population Pharmacokinetics of Vancomycin in Kidney Transplant Recipients: Model Building and Parameter Optimization
Population Pharmacokinetics of Vancomycin in Kidney Transplant Recipients: Model Building and Parameter Optimization Abstract Abstract Background Depending on the renal function of patients and many other influencing factors, studies on vancomycin pharmacokinetics show significant inter- and intra-individual variabilit...
PMC4199974
core_pubmed_pmc
Evaluation of the pharmacokinetic and pharmacodynamic drug interactions between cilnidipine and valsartan, in healthy volunteers
Evaluation of the pharmacokinetic and pharmacodynamic drug interactions between cilnidipine and valsartan, in healthy volunteers Abstract Purpose Although cilnidipine and valsartan are widely coadministered to patients with hypertension, their drug–drug interaction potential has not been investigated. This study compar...
PMC9780811
core_pubmed_pmc
Determination of the Pharmacokinetics and Pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a Cross-Over Cynomolgus Macaque Model of Mycobacterium tuberculosis Infection
Determination of the Pharmacokinetics and Pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a Cross-Over Cynomolgus Macaque Model of Mycobacterium tuberculosis Infection Abstract Abstract Innovative cross-over study designs were explored in non-human primate (NHP) studies to determine the value ...
PMC6161852
core_pubmed_pmc
Safety and pharmacokinetics of single, dual, and triple antiretroviral drug formulations delivered by pod-intravaginal rings designed for HIV-1 prevention: A Phase I trial
Safety and pharmacokinetics of single, dual, and triple antiretroviral drug formulations delivered by pod-intravaginal rings designed for HIV-1 prevention: A Phase I trial Abstract Abstract Background Intravaginal rings (IVRs) for HIV pre-exposure prophylaxis (PrEP) theoretically overcome some adherence concerns associ...
PMC8528301
core_pubmed_pmc
Vitamin D levels do not cause vitamin-drug interactions with dexamethasone or dasatinib in mice
Vitamin D levels do not cause vitamin-drug interactions with dexamethasone or dasatinib in mice Abstract Abstract Vitamin D 3 (VD 3 ) induces intestinal CYP3A that metabolizes orally administered anti-leukemic chemotherapeutic substrates dexamethasone (DEX) and dasatinib potentially causing a vitamin-drug interaction. ...
PMC10343793
core_pubmed_pmc
Implications of Pharmacokinetic Potentials of Pioglitazone Enantiomers in Rat Plasma Mediated through Glucose Uptake Assay
Implications of Pharmacokinetic Potentials of Pioglitazone Enantiomers in Rat Plasma Mediated through Glucose Uptake Assay Abstract Abstract Pioglitazone, a PPAR-gamma activator used to diagnose hyperglycemia, was studied for its stereoselective deposition and active enantiomers in female albino Wistar rats. In accorda...
PMC10582672
core_pubmed_pmc
Keverprazan, a novel potassium‐competitive acid blocker: Multiple oral doses safety, tolerability, pharmacokinetics, and pharmacodynamics in healthy subjects
Keverprazan, a novel potassium‐competitive acid blocker: Multiple oral doses safety, tolerability, pharmacokinetics, and pharmacodynamics in healthy subjects Abstract Abstract Keverprazan, a novel potassium‐competitive acid blocker, was approved for treating acid‐related diseases. This study aimed to analyze the safety...
PMC12634510
core_pubmed_pmc
From molecules to medicine: a systematic review of Gastrodia elata’s bioactive metabolites and therapeutic potential
From molecules to medicine: a systematic review of Gastrodia elata’s bioactive metabolites and therapeutic potential Abstract Abstract The dried tuber of Gastrodia elata (GE), a perennial orchid with a 2,200-year medicinal history documented in the Shennong Bencaojing (200 BCE), remains a cornerstone of traditional Chi...
PMC9047015
core_pubmed_pmc
Pharmacokinetics and Tissue Residue Profiles of Enrofloxacin in Crucian Carp ( Carassius auratus gibelio ) Following Single and Multiple Oral Administration
Pharmacokinetics and Tissue Residue Profiles of Enrofloxacin in Crucian Carp ( Carassius auratus gibelio ) Following Single and Multiple Oral Administration Abstract Abstract The pharmacokinetics, tissue distribution, and elimination of enrofloxacin (ENR) and its metabolite ciprofloxacin (CIP) were investigated to the ...
PMC11509227
core_pubmed_pmc
A Simple Eco-Friendly HPLC-PDA Method for the Simultaneous Determination of Paclitaxel and Seliciclib in Plasma Samples for Assessing Their Pharmacodynamics and Pharmacokinetics in Combination Therapy for Uterine Sarcoma
A Simple Eco-Friendly HPLC-PDA Method for the Simultaneous Determination of Paclitaxel and Seliciclib in Plasma Samples for Assessing Their Pharmacodynamics and Pharmacokinetics in Combination Therapy for Uterine Sarcoma Abstract Background/Objectives : Uterine sarcoma, a rare cancer originating in the smooth muscle of...
PMC11290884
core_pubmed_pmc
The impact of alcohol and illicit substance use on the pharmacokinetics of first-line TB drugs
The impact of alcohol and illicit substance use on the pharmacokinetics of first-line TB drugs Abstract Abstract Background In South Africa, an estimated 11% of the population have high alcohol use, a major risk factor for TB. Alcohol and other substance use are also associated with poor treatment response, with a pote...
PMC10139987
core_pubmed_pmc
A biomarker of opioid-induced respiratory toxicity in experimental studies
A biomarker of opioid-induced respiratory toxicity in experimental studies Abstract Summary Opioids are commonly used painkillers and drugs of abuse and have serious toxic effects including potentially lethal respiratory depression. It remains unknown which respiratory parameter is the most sensitive biomarker of opioi...
PMC11761243
core_pubmed_pmc
Chemometric Methods—A Valuable Tool for Investigating the Interactions Between Antifungal Drugs (Including Antifungal Antibiotics) and Food
Chemometric Methods—A Valuable Tool for Investigating the Interactions Between Antifungal Drugs (Including Antifungal Antibiotics) and Food Abstract Background/Objectives: Developing antifungal drugs with lower potential for interactions with food may help to optimize treatment and reduce the risk of antimicrobial resi...
PMC6889584
core_pubmed_pmc
Relationship between the effects of food on the pharmacokinetics of oral antineoplastic drugs and their physicochemical properties
Relationship between the effects of food on the pharmacokinetics of oral antineoplastic drugs and their physicochemical properties Abstract Abstract Background Food is known to affect drug absorption by delaying gastric emptying time, altering gastrointestinal pH, stimulating bile flow, increasing splanchnic blood flow...
PMC4368747
core_pubmed_pmc
Validation of a Rapid and Sensitive LC-MS/MS Method for Determination of Exemestane and Its Metabolites, 17β-Hydroxyexemestane and 17β-Hydroxyexemestane-17-O-β-D-Glucuronide: Application to Human Pharmacokinetics Study
Validation of a Rapid and Sensitive LC-MS/MS Method for Determination of Exemestane and Its Metabolites, 17β-Hydroxyexemestane and 17β-Hydroxyexemestane-17-O-β-D-Glucuronide: Application to Human Pharmacokinetics Study Abstract Abstract A novel, rapid and sensitive liquid chromatography-tandem mass spectrometric (LC-MS...
PMC9710314
core_pubmed_pmc
The Influence of Cannabidiol on the Pharmacokinetics of Methylphenidate in Healthy Subjects
The Influence of Cannabidiol on the Pharmacokinetics of Methylphenidate in Healthy Subjects Abstract Introduction Cannabidiol (CBD) is a widely utilized nonpsychoactive cannabinoid available as an over-the-counter supplement, a component of medical cannabis, and a prescriptive treatment of childhood epilepsies. In vitr...
PMC9996316
core_pubmed_pmc
Chemically modified aptamers for improving binding affinity to the target proteins via enhanced non-covalent bonding
Chemically modified aptamers for improving binding affinity to the target proteins via enhanced non-covalent bonding Abstract Nucleic acid aptamers are ssDNA or ssRNA fragments that specifically recognize targets. However, the pharmacodynamic properties of natural aptamers consisting of 4 naturally occurring nucleoside...
PMC10421376
core_pubmed_pmc
Simultaneous Determination of Five Iridoids of Picrorhiza scrophulariiflora in Rat Plasma Using UHPLC-ESI-MS/MS
Simultaneous Determination of Five Iridoids of Picrorhiza scrophulariiflora in Rat Plasma Using UHPLC-ESI-MS/MS Abstract In this study, we developed an ultra-performance liquid chromatography-electrospray tandem quadrupole mass spectrometry (UHPLC-ESI-MS/MS) method to simultaneously determine Picroside-I, Picroside-II,...
PMC9633523
core_pubmed_pmc
Phase 1 Study to Assess the Safety and Pharmacokinetics of Elexacaftor/Tezacaftor/Ivacaftor in Subjects Without Cystic Fibrosis With Moderate Hepatic Impairment
Phase 1 Study to Assess the Safety and Pharmacokinetics of Elexacaftor/Tezacaftor/Ivacaftor in Subjects Without Cystic Fibrosis With Moderate Hepatic Impairment Abstract Background and Objective Elexacaftor/tezacaftor/ivacaftor is highly effective in treating people with cystic fibrosis (pwCF) who have ≥ 1 responsive m...
PMC9598710
core_pubmed_pmc
Health Benefits and Pharmacological Properties of Stigmasterol
Health Benefits and Pharmacological Properties of Stigmasterol Abstract Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmaste...
PMC11447946
core_pubmed_pmc
Guiding the starting dose of the once-daily formulation of tacrolimus in “ de novo” adult renal transplant patients: a population approach
Guiding the starting dose of the once-daily formulation of tacrolimus in “ de novo” adult renal transplant patients: a population approach Abstract Abstract Aims The once-daily extended-release tacrolimus formulation (ER-Tac) has demonstrated similar efficacy and safety to the twice-daily immediate-release formulation ...
PMC8856561
core_pubmed_pmc
Pharmacological and genetic activation of cAMP synthesis disrupts cholesterol utilization in Mycobacterium tuberculosis
Pharmacological and genetic activation of cAMP synthesis disrupts cholesterol utilization in Mycobacterium tuberculosis Abstract There is a growing appreciation for the idea that bacterial utilization of host-derived lipids, including cholesterol, supports Mycobacterium tuberculosis (Mtb) pathogenesis. This has generat...
PMC9476642
core_pubmed_pmc
A reliable and rapid pharmacokinetic study of pueraria isoflavones using pueraria reference extractive substance in beagle plasma: Application to study of Yufeng Ningxin Tablets
A reliable and rapid pharmacokinetic study of pueraria isoflavones using pueraria reference extractive substance in beagle plasma: Application to study of Yufeng Ningxin Tablets Abstract Objective In order to evaluate the reliability and feasibility of pueraria reference extractive substance (RES) used in biological sa...
PMC3065798
core_pubmed_pmc
Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats
Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats Abstract Nanoemulsions stabilized by traditional emulsifiers raise toxicological concerns for long-term treatment. The present work investigates the po...