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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... |
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