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PMC10694292 | core_pubmed_pmc | Increased sinusoidal export of drug glucuronides is a compensative mechanism in liver cirrhosis of mice | Increased sinusoidal export of drug glucuronides is a compensative mechanism in liver cirrhosis of mice Abstract Rationale: Liver cirrhosis is known to affect drug pharmacokinetics, but the functional assessment of the underlying pathophysiological alterations in drug metabolism is difficult. Methods: Cirrhosis in mice... |
PMC2889891 | core_pubmed_pmc | Pharmacokinetic properties and antitumor efficacy of the 5-fluorouracil loaded PEG-hydrogel | Pharmacokinetic properties and antitumor efficacy of the 5-fluorouracil loaded PEG-hydrogel Abstract Abstract Background We have studied the in vitro and in vivo utility of polyethylene glycol (PEG)-hydrogels for the development of an anticancer drug 5-fluorouracil (5-FU) delivery system. Methods A 5-FU-loaded PEG-hydr... |
PMC4709389 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach | Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach Abstract Abstract Purpose Acotiamide, a gastroprokinetic agent used to treat functional dyspepsia, is tran... |
PMC8023329 | core_pubmed_pmc | Effect of hepatic impairment on pharmacokinetics, safety, and tolerability of lemborexant | Effect of hepatic impairment on pharmacokinetics, safety, and tolerability of lemborexant Abstract Abstract Lemborexant, a dual orexin receptor antagonist, is approved in the United States, Japan, and Canada for the treatment of insomnia in adults. This phase I, multicenter, open‐label, parallel‐group study assessed th... |
PMC7540321 | core_pubmed_pmc | Physiological parameter values for physiologically based pharmacokinetic models in food‐producing animals. Part I: Cattle and swine | Physiological parameter values for physiologically based pharmacokinetic models in food‐producing animals. Part I: Cattle and swine Abstract Abstract Physiologically based pharmacokinetic (PBPK) models for chemicals in food animals are a useful tool in estimating chemical tissue residues and withdrawal intervals. Physi... |
PMC11597430 | core_pubmed_pmc | An In Silico Approach to Discover Efficient Natural Inhibitors to Tie Up Epstein–Barr Virus Infection | An In Silico Approach to Discover Efficient Natural Inhibitors to Tie Up Epstein–Barr Virus Infection Abstract Epstein–Barr virus (EBV), also known as human herpesvirus 4, is a member of the herpes virus family. EBV is a widespread virus and causes infectious mononucleosis, which manifests with symptoms such as fever, ... |
PMC7679260 | core_pubmed_pmc | Antispasmodic effects of the essential oil of Croton zehnteneri , anethole, and estragole, on tracheal smooth muscle | Antispasmodic effects of the essential oil of Croton zehnteneri , anethole, and estragole, on tracheal smooth muscle Abstract Croton zehntneri is a plant well adapted to the semi-arid climate of northeastern region of Brazil. The essential oil of C. zehntneri (EOCz) has been described to have several pharmacologic prop... |
PMC11576624 | core_pubmed_pmc | Assessing the performance of QSP models: biology as the driver for validation | Assessing the performance of QSP models: biology as the driver for validation Abstract Validation of a quantitative model is a critical step in establishing confidence in the model’s suitability for whatever analysis it was designed. While processes for validation are well-established in the statistical sciences, the f... |
PMC7529773 | core_pubmed_pmc | Pharmacokinetic prediction of an antibody in mice based on an in vitro cell-based approach using target receptor-expressing cells | Pharmacokinetic prediction of an antibody in mice based on an in vitro cell-based approach using target receptor-expressing cells Abstract Abstract In vivo pharmacokinetics (PK) studies using mice and monkeys are the main approaches for evaluating and predicting the PK of antibodies, and there is a strong demand for me... |
PMC3933742 | core_pubmed_pmc | Neuroprotective Properties of Citicoline: Facts, Doubts and Unresolved Issues | Neuroprotective Properties of Citicoline: Facts, Doubts and Unresolved Issues Abstract Citicoline is the generic name of the pharmaceutical substance that chemically is cytidine-5′-diphosphocholine (CDP-choline), which is identical to the natural intracellular precursor of phospholipid phosphatidylcholine. Following in... |
PMC12061681 | core_pubmed_pmc | Tacrolimus exposure during the three-month period following allogeneic stem cell transplantation predicts overall survival | Tacrolimus exposure during the three-month period following allogeneic stem cell transplantation predicts overall survival Abstract Abstract Objectives The objective of this study was to investigate the relationship between both short-term and long-term tacrolimus exposure and overall survival after allogeneic stem cel... |
PMC6270898 | core_pubmed_pmc | Trends in Protein-Based Biosensor Assemblies for Drug Screening and Pharmaceutical Kinetic Studies | Trends in Protein-Based Biosensor Assemblies for Drug Screening and Pharmaceutical Kinetic Studies Abstract Abstract The selection of natural and chemical compounds for potential applications in new pharmaceutical formulations constitutes a time-consuming procedure in drug screening. To overcome this issue, new devices... |
PMC8605568 | core_pubmed_pmc | Genetic analysis of pharmacogenomic VIP variants in the Wa population from Yunnan Province of China | Genetic analysis of pharmacogenomic VIP variants in the Wa population from Yunnan Province of China Abstract Background The variation of drug responses and target does among individuals is mostly determined by genes. With the development of pharmacogenetics and pharmacogenomics, the differences in drug response between... |
PMC6814631 | core_pubmed_pmc | Development of In Vitro – In Vivo Correlation for Upadacitinib Extended-Release Tablet Formulation | Development of In Vitro – In Vivo Correlation for Upadacitinib Extended-Release Tablet Formulation Abstract Abstract Upadacitinib is a selective Janus Kinase 1 inhibitor which is being developed for the treatment of several inflammatory diseases including rheumatoid arthritis. Upadacitinib was evaluated in Phase 3 stud... |
PMC5055906 | core_pubmed_pmc | Prediction of drug interaction between oral adsorbent AST-120 and concomitant drugs based on the in vitro dissolution and in vivo absorption behavior of the drugs | Prediction of drug interaction between oral adsorbent AST-120 and concomitant drugs based on the in vitro dissolution and in vivo absorption behavior of the drugs Abstract Purpose AST-120 is used to decrease the abundance of serum uremic toxins in treatment of chronic kidney disease; however, it could also adsorb conco... |
PMC9706570 | core_pubmed_pmc | A Reactive Oxygen Species-Scavenging ‘Stealth’ Polymer, Poly(thioglycidyl glycerol), Outperforms Poly(ethylene glycol) in Protein Conjugates and Nanocarriers and Enhances Protein Stability to Environmental and Biological Stressors | A Reactive Oxygen Species-Scavenging ‘Stealth’ Polymer, Poly(thioglycidyl glycerol), Outperforms Poly(ethylene glycol) in Protein Conjugates and Nanocarriers and Enhances Protein Stability to Environmental and Biological Stressors Abstract Abstract This study addresses well-known shortcomings of poly(ethylene glycol) (... |
PMC12615732 | core_pubmed_pmc | A large-scale human toxicogenomics resource for drug-induced liver injury prediction | A large-scale human toxicogenomics resource for drug-induced liver injury prediction Abstract Abstract Drug-Induced Liver Injury (DILI) remains one of the most critical challenges in drug development, causing patient safety concerns, clinical trial failures and drug withdrawals. We introduce ToxPredictor , a toxicogeno... |
PMC5604705 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of AMG 811, an anti-interferon-γ monoclonal antibody, in SLE subjects without or with lupus nephritis | Safety, pharmacokinetics and pharmacodynamics of AMG 811, an anti-interferon-γ monoclonal antibody, in SLE subjects without or with lupus nephritis Abstract Abstract Objective To evaluate safety, pharmacokinetics and pharmacodynamics of anti-interferon (IFN)-γ monoclonal antibody AMG 811 in subjects with SLE without or... |
PMC12165791 | core_pubmed_pmc | Tebentafusp elicits on-target cutaneous immune responses driven by cytotoxic T cells in uveal melanoma patients | Tebentafusp elicits on-target cutaneous immune responses driven by cytotoxic T cells in uveal melanoma patients Abstract BACKGROUND Tebentafusp is the first T cell receptor–based bispecific protein approved for clinical use in HLA-A*02:01 + adult patients with unresectable/metastatic uveal melanoma. It redirects T cell... |
PMC6017738 | core_pubmed_pmc | A Comparative Pharmacokinetic Study by UHPLC-MS/MS of Main Active Compounds after Oral Administration of Zushima-Gancao Extract in Normal and Adjuvant-Induced Arthritis Rats | A Comparative Pharmacokinetic Study by UHPLC-MS/MS of Main Active Compounds after Oral Administration of Zushima-Gancao Extract in Normal and Adjuvant-Induced Arthritis Rats Abstract A sensitive and rapid ultra high-performance liquid-chromatography tandem mass spectrometry (UHPLC-MS/MS) method has been applied to inve... |
PMC9401557 | core_pubmed_pmc | Mogamulizumab in Combination with Nivolumab in a Phase I/II Study of Patients with Locally Advanced or Metastatic Solid Tumors | Mogamulizumab in Combination with Nivolumab in a Phase I/II Study of Patients with Locally Advanced or Metastatic Solid Tumors Abstract Abstract Purpose: The aim of the study was to determine safety, antitumor activity, and pharmacodynamic profile of mogamulizumab, an anti-CCR4 monoclonal antibody targeting effector re... |
PMC11943233 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Simulation of Muscle Relaxation Antagonistic Conditions for Post-Operative Recurarization Prevention | Pharmacokinetic–Pharmacodynamic Simulation of Muscle Relaxation Antagonistic Conditions for Post-Operative Recurarization Prevention Abstract Abstract Background/Objectives: No study has simulated rocuronium (Rb) effect-site concentrations (Ce_Rb) using real-time data—such as Rb concentrations, train-of-four (TOF) coun... |
PMC6200719 | core_pubmed_pmc | Imaging of Pseudomonas aeruginosa infection with Ga-68 labelled pyoverdine for positron emission tomography | Imaging of Pseudomonas aeruginosa infection with Ga-68 labelled pyoverdine for positron emission tomography Abstract Abstract Pseudomonas aeruginosa is an increasingly prevalent opportunistic pathogen that causes a variety of life-threatening nosocomial infections. Novel strategies for the development of new antibacter... |
PMC10187420 | core_pubmed_pmc | Transcriptomic signature, bioactivity and safety of a non-hepatoxic analgesic generating AM404 in the mid-brain PAG region | Transcriptomic signature, bioactivity and safety of a non-hepatoxic analgesic generating AM404 in the mid-brain PAG region Abstract Abstract The safe and effective management of pain is a critical healthcare and societal need. The potential for misuse and addiction associated with opioids, nephrotoxicity, and gastroint... |
PMC11881576 | core_pubmed_pmc | Population pharmacokinetics and pulmonary modeling of eravacycline and the determination of microbiological breakpoint and cutoff of PK/PD | Population pharmacokinetics and pulmonary modeling of eravacycline and the determination of microbiological breakpoint and cutoff of PK/PD Abstract ABSTRACT Eravacycline is a broad-spectrum fluorocycline currently approved for complicated intra-abdominal infections (cIAIs). In lung-infection models, it is effective aga... |
PMC6579883 | core_pubmed_pmc | Semi-Mechanistic Modeling of Florfenicol Time-Kill Curves and in silico Dose Fractionation for Calf Respiratory Pathogens | Semi-Mechanistic Modeling of Florfenicol Time-Kill Curves and in silico Dose Fractionation for Calf Respiratory Pathogens Abstract An important application of time-kill curve (TKC) assays is determination of the nature of the best PK/PD index ( f AUC/MIC or f T% > MIC) and its target value for predicting clinical effic... |
PMC5407619 | core_pubmed_pmc | Non invasive imaging assessment of the biodistribution of GSK2849330, an ADCC and CDC optimized anti HER3 mAb, and its role in tumor macrophage recruitment in human tumor-bearing mice | Non invasive imaging assessment of the biodistribution of GSK2849330, an ADCC and CDC optimized anti HER3 mAb, and its role in tumor macrophage recruitment in human tumor-bearing mice Abstract The purpose of this work was to use various molecular imaging techniques to non-invasively assess GSK2849330 (anti HER3 ADCC an... |
PMC9296590 | core_pubmed_pmc | Population pharmacokinetics of tenofovir, emtricitabine and intracellular metabolites in transgender women | Population pharmacokinetics of tenofovir, emtricitabine and intracellular metabolites in transgender women Abstract Aims Transgender women (TGW) have been underrepresented in trials and use gender‐affirming hormonal therapies (GAHT) that may alter renal function by significantly increasing creatinine clearance. Populat... |
PMC12479631 | core_pubmed_pmc | TDM-Based Tailored Dosing of Durvalumab in Lung Cancer Patients: A Comprehensive Population Pharmacokinetic–Pharmacoeconomic Evaluation | TDM-Based Tailored Dosing of Durvalumab in Lung Cancer Patients: A Comprehensive Population Pharmacokinetic–Pharmacoeconomic Evaluation Abstract Abstract Background The increasing use of immune checkpoint inhibitors, such as durvalumab, places a significant financial burden on healthcare systems, strains hospital capac... |
PMC4580629 | core_pubmed_pmc | Auto-Induction Effect of Chloroxoquinoline on the Cytochrome P450 Enzymes of Rats Associated with CYP 3A and 1A | Auto-Induction Effect of Chloroxoquinoline on the Cytochrome P450 Enzymes of Rats Associated with CYP 3A and 1A Abstract To investigate the auto-induction of cytochrome P450 (CYP450) by Chloroxoquinoline (CXL), a novel anticancer drug. Three experiments related to the induction of CYP450 were performed: a) In vitro use... |
PMC4769423 | core_pubmed_pmc | Tolerability in man following inhalation dosing of the selective TLR7 agonist, AZD8848 | Tolerability in man following inhalation dosing of the selective TLR7 agonist, AZD8848 Abstract Abstract Background Many patients with asthma have a T-helper type 2 (Th2) driven inflammation of the lung, whereas toll-like receptor 7 (TLR7) agonists, by inducing type I interferons, inhibit Th2 responses. In man, oral or... |
PMC12057358 | core_pubmed_pmc | Distribution of ganciclovir in the porcine central nervous system | Distribution of ganciclovir in the porcine central nervous system Abstract ABSTRACT Ganciclovir is often used compassionately for encephalitis due to cytomegalovirus (CMV) and human herpes virus 6b (HHV-6b). Ganciclovir pharmacokinetic studies in the central nervous system (CNS) generally rely on single measurements in... |
PMC8705537 | core_pubmed_pmc | Total Body Irradiation Forever? Optimising Chemotherapeutic Options for Irradiation-Free Conditioning for Paediatric Acute Lymphoblastic Leukaemia | Total Body Irradiation Forever? Optimising Chemotherapeutic Options for Irradiation-Free Conditioning for Paediatric Acute Lymphoblastic Leukaemia Abstract Total-body irradiation (TBI) based conditioning prior to allogeneic hematopoietic stem cell transplantation (HSCT) is generally regarded as the gold-standard for ch... |
PMC6471806 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of the artesunate–mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children | Population pharmacokinetics and pharmacodynamics of the artesunate–mefloquine fixed dose combination for the treatment of uncomplicated falciparum malaria in African children Abstract Abstract Background The World Health Organization (WHO) recommends combinations of an artemisinin derivative plus an anti-malarial drug ... |
PMC5045556 | core_pubmed_pmc | Development of a mechanism-based pharmacokinetic/pharmacodynamic model to characterize the thermoregulatory effects of serotonergic drugs in mice | Development of a mechanism-based pharmacokinetic/pharmacodynamic model to characterize the thermoregulatory effects of serotonergic drugs in mice Abstract Abstract We have shown recently that concurrent harmaline, a monoamine oxidase-A inhibitor (MAOI), potentiates serotonin (5-HT) receptor agonist 5-methoxy- N,N -dime... |
PMC12848337 | core_pubmed_pmc | Phase 1 study of rogocekib in patients with relapsed or refractory hematologic malignancies | Phase 1 study of rogocekib in patients with relapsed or refractory hematologic malignancies Abstract Key Points • Rogocekib (CTX-712), a pan–CDC2-like kinase inhibitor, showed tolerable safety in relapsed/refractory AML and higher-risk MDS. • The overall response rate was 42.9%, with promising activity in patients, inc... |
PMC6071124 | core_pubmed_pmc | Pharmacokinetics of Salicylic Acid Following Intravenous and Oral Administration of Sodium Salicylate in Sheep | Pharmacokinetics of Salicylic Acid Following Intravenous and Oral Administration of Sodium Salicylate in Sheep Abstract Simple Summary Scarcity of non-steroidal anti-inflammatory drugs (NSAID) to minimise the pain in sheep instigated the current study. The aim of this study was to know the pharmacokinetic parameters of... |
PMC7768337 | core_pubmed_pmc | First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia | First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia Abstract PURPOSE Iadademstat is a novel, highly potent, and selective inhibitor of LSD1 (KDM1A), with preclinical in vitro and in vivo antileukemic ... |
PMC10820197 | core_pubmed_pmc | Potentially Harmful Excipients: State of the Art for Oral Liquid Forms Used in Neonatology and Pediatrics Units | Potentially Harmful Excipients: State of the Art for Oral Liquid Forms Used in Neonatology and Pediatrics Units Abstract Abstract The pediatric population exhibits an important age-dependent heterogeneity in pharmacokinetics and pharmacodynamics parameters, resulting in differences in drug efficacy and toxicity compare... |
PMC7831558 | core_pubmed_pmc | Repositioning chloroquine as antiviral prophylaxis against COVID-19: potential and challenges | Repositioning chloroquine as antiviral prophylaxis against COVID-19: potential and challenges Abstract Highlights • Chloroquine (CQ) has in vitro evidence of potential efficacy against SARS-CoV-2 (virus causing COVID-19) and particularly effective at early stages of infection when viral load is low. • CQ can achieve mi... |
PMC12136075 | core_pubmed_pmc | Anti-Tyrosinase and Radical Scavenging Activities of Selected Cassipourea Plants and Isolated 7-Methoxygeranin A: Traditional Use as Skin Lighteners | Anti-Tyrosinase and Radical Scavenging Activities of Selected Cassipourea Plants and Isolated 7-Methoxygeranin A: Traditional Use as Skin Lighteners Abstract Abstract Background In rural areas of KwaZulu-Natal and Eastern Cape Provinces, South Africa, women have traditionally used bark extracts from Cassipourea flanaga... |
PMC4964175 | core_pubmed_pmc | SCISSOR—Spinal Cord Injury Study on Small molecule-derived Rho inhibition: a clinical study protocol | SCISSOR—Spinal Cord Injury Study on Small molecule-derived Rho inhibition: a clinical study protocol Abstract Introduction The approved analgesic and anti-inflammatory drugs ibuprofen and indometacin block the small GTPase RhoA, a key enzyme that impedes axonal sprouting after axonal damage. Inhibition of the Rho pathw... |
PMC7843372 | core_pubmed_pmc | Case Report: Variable Pharmacokinetic Profile of Eculizumab in an aHUS Patient | Case Report: Variable Pharmacokinetic Profile of Eculizumab in an aHUS Patient Abstract Abstract Background With the introduction of eculizumab, a C5-inhibitor, morbidity and mortality improved significantly for patients with atypical hemolytic uremic syndrome (aHUS). In view of the high costs, actual needs of the drug... |
PMC9103606 | core_pubmed_pmc | Hydroxychloroquine Blood Concentrations Can Be Clinically Relevant Also After Drug Discontinuation | Hydroxychloroquine Blood Concentrations Can Be Clinically Relevant Also After Drug Discontinuation Abstract Abstract Background and Objective Hydroxychloroquine was widely used during the severe acute respiratory syndrome coronavirus 2 pandemic as an antiviral drug. Most previous pharmacokinetic/pharmacodynamic studies... |
PMC6820606 | core_pubmed_pmc | Alternative dosing regimens for atezolizumab: an example of model-informed drug development in the postmarketing setting | Alternative dosing regimens for atezolizumab: an example of model-informed drug development in the postmarketing setting Abstract Purpose To determine the exposure–response (ER) relationships between atezolizumab exposure and efficacy or safety in patients with advanced non-small cell lung cancer (NSCLC) or urothelial ... |
PMC9021690 | core_pubmed_pmc | Can First-Dose Therapeutic Drug Monitoring Predict the Steady State Area Under the Blood Concentration-Time Curve of Busulfan in Pediatric Patients Undergoing Hematopoietic Stem Cell Transplantation? | Can First-Dose Therapeutic Drug Monitoring Predict the Steady State Area Under the Blood Concentration-Time Curve of Busulfan in Pediatric Patients Undergoing Hematopoietic Stem Cell Transplantation? Abstract Abstract Busulfan has high intra-individual variability and possible time-dependent changes in clearance, which... |
PMC12649303 | core_pubmed_pmc | A Novel Maturation Equation for Hepatic Clearance Across Preterm, Term Neonates, Children, and Adults: Application to Paracetamol and Its Metabolite | A Novel Maturation Equation for Hepatic Clearance Across Preterm, Term Neonates, Children, and Adults: Application to Paracetamol and Its Metabolite Abstract Abstract A preterm and term neonate to adult (PTNA) maturation equation was introduced recently to describe the glomerular filtration rate maturation from birth t... |
PMC3404091 | core_pubmed_pmc | Synergy between Vancomycin and Nafcillin against Staphylococcus aureus in an In Vitro Pharmacokinetic/Pharmacodynamic Model | Synergy between Vancomycin and Nafcillin against Staphylococcus aureus in an In Vitro Pharmacokinetic/Pharmacodynamic Model Abstract Abstract Introduction Continued pressure from glycopeptide use has led to non-susceptible strains of Staphylococcus aureus including heterogeneously vancomycin-intermediate S. aureus (hVI... |
PMC11020314 | core_pubmed_pmc | Impact of attaining aggressive vs. conservative PK/PD target on the clinical efficacy of beta-lactams for the treatment of Gram-negative infections in the critically ill patients: a systematic review and meta-analysis | Impact of attaining aggressive vs. conservative PK/PD target on the clinical efficacy of beta-lactams for the treatment of Gram-negative infections in the critically ill patients: a systematic review and meta-analysis Abstract Abstract Background To perform a systematic review with meta-analysis with the dual intent of... |
PMC6971844 | core_pubmed_pmc | Mobilized peripheral blood: an updated perspective | Mobilized peripheral blood: an updated perspective Abstract Enforced egress of hematopoietic stem cells (HSCs) out of the bone marrow (BM) into the peripheral circulation, termed mobilization, has come a long way since its discovery over four decades ago. Mobilization research continues to be driven by the need to opti... |
PMC8585822 | core_pubmed_pmc | Geographical Variability in Paromomycin Pharmacokinetics Does Not Explain Efficacy Differences between Eastern African and Indian Visceral Leishmaniasis Patients | Geographical Variability in Paromomycin Pharmacokinetics Does Not Explain Efficacy Differences between Eastern African and Indian Visceral Leishmaniasis Patients Abstract Abstract Introduction Intramuscular paromomycin monotherapy to treat visceral leishmaniasis (VL) has been shown to be effective for Indian patients, ... |
PMC8915826 | core_pubmed_pmc | Evaluation of Inhalation Exposures and Potential Health Impacts of Ingredient Mixtures Using in vitro to in vivo Extrapolation | Evaluation of Inhalation Exposures and Potential Health Impacts of Ingredient Mixtures Using in vitro to in vivo Extrapolation Abstract Abstract In vitro methods offer opportunities to provide mechanistic insight into bioactivity as well as human-relevant toxicological assessments compared to animal testing. One of the... |
PMC7297490 | core_pubmed_pmc | Transitions between infused and oral prostacyclin pathway agents in pulmonary arterial hypertension: key considerations | Transitions between infused and oral prostacyclin pathway agents in pulmonary arterial hypertension: key considerations Abstract Prostacyclin pathway agents are a critical treatment for patients with pulmonary arterial hypertension. Seven prostacyclin pathway agents are available, including agents administered by paren... |
PMC6916274 | core_pubmed_pmc | Oral ferroportin inhibitor VIT‐2763: First‐in‐human, phase 1 study in healthy volunteers | Oral ferroportin inhibitor VIT‐2763: First‐in‐human, phase 1 study in healthy volunteers Abstract Abstract Restriction of iron availability by ferroportin inhibition is a novel approach to treating non‐transfusion‐dependent thalassemia (β‐thalassemia intermedia). This first‐in‐human, Phase I study ( https://www.clinica... |
PMC12830148 | core_pubmed_pmc | Hydroxyurea pharmacokinetics in children with sickle cell anemia across different global populations | Hydroxyurea pharmacokinetics in children with sickle cell anemia across different global populations Abstract Key Points • Interpatient differences in hydroxyurea dosing for children with SCA are predicted by drug PK. • Hydroxyurea PK parameters in children with SCA from the United States, Africa, and the Caribbean pre... |
PMC10519932 | core_pubmed_pmc | Physiologically-based pharmacokinetic modeling for optimal dosage prediction of olaparib when co-administered with CYP3A4 modulators and in patients with hepatic/renal impairment | Physiologically-based pharmacokinetic modeling for optimal dosage prediction of olaparib when co-administered with CYP3A4 modulators and in patients with hepatic/renal impairment Abstract This study aimed to develop a physiologically-based pharmacokinetic (PBPK) model to predict the maximum plasma concentration (C max ... |
PMC12588651 | core_pubmed_pmc | Utility of a TDM-Guided Expert Clinical Pharmacological Advice Program for Optimizing the Use of Novel Beta-Lactam/Beta-Lactamase Inhibitor Combinations and Cefiderocol in a Tertiary University Hospital: An Interim Analysis | Utility of a TDM-Guided Expert Clinical Pharmacological Advice Program for Optimizing the Use of Novel Beta-Lactam/Beta-Lactamase Inhibitor Combinations and Cefiderocol in a Tertiary University Hospital: An Interim Analysis Abstract Supplemental Digital Content is Available in the Text. Key Words: expert clinical pharm... |
PMC9545781 | core_pubmed_pmc | Human pharmacokinetics of XBD173 and etifoxine distinguish their potential for pharmacodynamic effects mediated by translocator protein | Human pharmacokinetics of XBD173 and etifoxine distinguish their potential for pharmacodynamic effects mediated by translocator protein Abstract Abstract XBD173 and etifoxine are translocator protein (TSPO) ligands that modulate inflammatory responses in preclinical models. Limited human pharmacokinetic data is availab... |
PMC12177174 | core_pubmed_pmc | A phase 1 study evaluating the safety, tolerability, and pharmacokinetics of the porcupine inhibitor, AZD5055 | A phase 1 study evaluating the safety, tolerability, and pharmacokinetics of the porcupine inhibitor, AZD5055 Abstract Summary Excessive Wnt signaling contributes to the development of fibrotic diseases and cancer. Here, we report the findings of a phase 1 study evaluating AZD5055, an orally administered porcupine inhi... |
PMC6422639 | core_pubmed_pmc | Under‐representation of elderly in clinical trials: An analysis of the initial approval documents in the Food and Drug Administration database | Under‐representation of elderly in clinical trials: An analysis of the initial approval documents in the Food and Drug Administration database Abstract Abstract Aims To evaluate the availability of pharmacokinetic, safety and efficacy analyses specifically targeted at elderly, prior to the authorization of drugs. Metho... |
PMC10810027 | core_pubmed_pmc | Real-Time Imaging of Single Retinal Cell Apoptosis in a Non-Human Primate Ocular Hypertension Model | Real-Time Imaging of Single Retinal Cell Apoptosis in a Non-Human Primate Ocular Hypertension Model Abstract Purpose To evaluate the feasibility of using DARC (detection of apoptosing retinal cells) technology as a biomarker for preclinical assessment of glaucomatous damage in a non-human primate (NHP) model of ocular ... |
PMC5991393 | core_pubmed_pmc | Pharmacokinetic properties of a novel inosine analog, 4′-cyano-2′-deoxyinosine, after oral administration in rats | Pharmacokinetic properties of a novel inosine analog, 4′-cyano-2′-deoxyinosine, after oral administration in rats Abstract Abstract 4′-cyano-2′-deoxyinosine (SK14-061a), a novel nucleoside analog based on inosine, has antiviral activity against the human immunodeficiency virus type 1 that has the ability to acquire res... |
PMC12070208 | core_pubmed_pmc | Population Pharmacokinetic Model for the Use of Intravenous or Subcutaneous Infliximab in Patients with Inflammatory Bowel Disease: Real-World Data from a Prospective Cohort Study | Population Pharmacokinetic Model for the Use of Intravenous or Subcutaneous Infliximab in Patients with Inflammatory Bowel Disease: Real-World Data from a Prospective Cohort Study Abstract Background/Aims Infliximab treatment failure in patients with inflammatory bowel disease may result from sub-optimal infliximab tro... |
PMC5076779 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of an orally disintegrating tablet formulation of dexlansoprazole | Pharmacokinetics and pharmacodynamics of an orally disintegrating tablet formulation of dexlansoprazole Abstract Background: The pharmacokinetics and pharmacodynamics of a novel orally disintegrating tablet (ODT) formulation of delayed-release dexlansoprazole 30 mg was evaluated versus the dexlansoprazole 30 mg capsule... |
PMC3912854 | core_pubmed_pmc | Raltegravir for HIV-1 infected children and adolescents: efficacy, safety, and pharmacokinetics | Raltegravir for HIV-1 infected children and adolescents: efficacy, safety, and pharmacokinetics Abstract Raltegravir was the first HIV integrase strand-transfer inhibitor to be approved by the US FDA, in October 2007, for the treatment of HIV-1 infection in combination with other antiretroviral agents. Raltegravir can ... |
PMC12845319 | core_pubmed_pmc | Clinical Characteristics, Long-Term Pharmacokinetics, and Outcomes in Kidney Transplant Recipients from an African Tertiary Centre: A 10-Year Single-Centre Retrospective Review | Clinical Characteristics, Long-Term Pharmacokinetics, and Outcomes in Kidney Transplant Recipients from an African Tertiary Centre: A 10-Year Single-Centre Retrospective Review Abstract Background: Kidney transplantation outcomes in resource-limited settings remain underreported. This 10-year retrospective review exami... |
PMC9280727 | core_pubmed_pmc | Micelles as potential drug delivery systems for colorectal cancer treatment | Micelles as potential drug delivery systems for colorectal cancer treatment Abstract Abstract Despite the significant progress in cancer therapy, colorectal cancer (CRC) remains one of the most fatal malignancies worldwide. Chemotherapy is currently the mainstay therapeutic modality adopted for CRC treatment. However, ... |
PMC3460023 | core_pubmed_pmc | Pharmacokinetics of cyclosporin - a microemulsion in children with idiopathic nephrotic syndrome | Pharmacokinetics of cyclosporin - a microemulsion in children with idiopathic nephrotic syndrome Abstract Abstract OBJECTIVE: We present a prospective study of a microemulsion of cyclosporin to treat idiopathic nephrotic syndrome in ten children with normal renal function who presented cyclosporin trough levels between... |
PMC6057249 | core_pubmed_pmc | Pharmacokinetics of colistin in patients with multidrug-resistant Gram-negative infections: A pilot study | Pharmacokinetics of colistin in patients with multidrug-resistant Gram-negative infections: A pilot study Abstract Abstract Background & objectives: There is little information concerning intravenously (i.v.) administered colistin in patients with multidrug-resistant (MDR) Gram-negative infections. Thus, this pilot pro... |
PMC9525106 | core_pubmed_pmc | Intestinal permeability of agaro-oligosaccharides: Transport across Caco-2 cell monolayers and pharmacokinetics in rats | Intestinal permeability of agaro-oligosaccharides: Transport across Caco-2 cell monolayers and pharmacokinetics in rats Abstract Abstract Agaro-oligosaccharides (AOSs), even-numbered oligosaccharides prepared from agar, are applied to various food, including supplements, drinks, and jellies because of their biological ... |
PMC3388254 | core_pubmed_pmc | Two-stage model-based design of cancer phase I dose escalation trials: evaluation using the phase I program of barasertib (AZD1152) | Two-stage model-based design of cancer phase I dose escalation trials: evaluation using the phase I program of barasertib (AZD1152) Abstract Summary Introduction Modeling and simulation of pharmacokinetics and pharmacodynamics has previously been shown to be potentially useful in designing Phase I programs of novel ant... |
PMC12108447 | core_pubmed_pmc | Impact of Timing of Beta-Lactam Therapeutic Drug Monitoring and Therapy Adjustment in Critically Ill Patients | Impact of Timing of Beta-Lactam Therapeutic Drug Monitoring and Therapy Adjustment in Critically Ill Patients Abstract Purpose: To assess the impact of beta-lactam therapeutic drug monitoring (TDM) timing and therapy adjustment on clinical cure and 30-day mortality. Methods: This was a prospective study of critically i... |
PMC8144741 | core_pubmed_pmc | Safety and Pharmacokinetics of a Tenofovir Alafenamide Fumarate-Emtricitabine based Oral Antiretroviral Regimen for Prevention of HIV Acquisition in Women: A Randomized Controlled Trial | Safety and Pharmacokinetics of a Tenofovir Alafenamide Fumarate-Emtricitabine based Oral Antiretroviral Regimen for Prevention of HIV Acquisition in Women: A Randomized Controlled Trial Abstract Background Daily oral emtricitabine (FTC, F)/tenofovir disoproxil fumarate (TDF) combination is approved for HIV pre-exposure... |
PMC5871563 | core_pubmed_pmc | Safety and tolerability of a novel, polyclonal human anti-MERS coronavirus antibody produced from transchromosomic cattle: a phase 1 randomised, double-blind, single-dose-escalation study | Safety and tolerability of a novel, polyclonal human anti-MERS coronavirus antibody produced from transchromosomic cattle: a phase 1 randomised, double-blind, single-dose-escalation study Abstract Summary Background Middle East respiratory syndrome (MERS) is a severe respiratory illness with an overall mortality of 35%... |
PMC11054797 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Side Effects of Midazolam: A Review and Case Example | Pharmacokinetics, Pharmacodynamics, and Side Effects of Midazolam: A Review and Case Example Abstract Abstract Midazolam, a short-acting benzodiazepine, is widely used to alleviate patient anxiety, enhance compliance, and aid in anesthesia. While its side effects are typically dose-dependent and manageable with vigilan... |
PMC6899822 | core_pubmed_pmc | A Phase 1, Open‐Label, Pharmacokinetic Trial to Investigate Possible Drug‐Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects | A Phase 1, Open‐Label, Pharmacokinetic Trial to Investigate Possible Drug‐Drug Interactions Between Clobazam, Stiripentol, or Valproate and Cannabidiol in Healthy Subjects Abstract Abstract GW Pharmaceuticals’ formulation of highly purified cannabidiol oral solution is approved in the United States for seizures associa... |
PMC3043256 | core_pubmed_pmc | Marginal increase of sunitinib exposure by grapefruit juice | Marginal increase of sunitinib exposure by grapefruit juice Abstract Purpose The drug label of sunitinib includes a warning for concomitant use of grapefruit juice (GJ) but clinical evidence for this drug interaction is lacking. The aim of this study is to determine the effect of GJ, a potent intestinal cytochrome P450... |
PMC4386948 | core_pubmed_pmc | Artemether-lumefantrine co-administration with antiretrovirals: population pharmacokinetics and dosing implications | Artemether-lumefantrine co-administration with antiretrovirals: population pharmacokinetics and dosing implications Abstract AIM Drug–drug interactions between antimalarial and antiretroviral drugs may influence antimalarial treatment outcomes. The aim of this study was to investigate the potential drug–drug interactio... |
PMC6864662 | core_pubmed_pmc | Comparative Pharmacokinetics of Gallic Acid, Protocatechuic Acid, and Quercitrin in Normal and Pyelonephritis Rats after Oral Administration of a Polygonum capitatum Extract | Comparative Pharmacokinetics of Gallic Acid, Protocatechuic Acid, and Quercitrin in Normal and Pyelonephritis Rats after Oral Administration of a Polygonum capitatum Extract Abstract Polygonum capitatum Buch.-Ham. ex D. Don is traditionally used by Hmong for the treatment of urinary tract infections and pyelonephritis.... |
PMC4186453 | core_pubmed_pmc | Use of a novel rapid and resource-efficient cassette dosing approach to determine the pharmacokinetics and CNS distribution of small molecule 7-transmembrane receptor allosteric modulators in rat | Use of a novel rapid and resource-efficient cassette dosing approach to determine the pharmacokinetics and CNS distribution of small molecule 7-transmembrane receptor allosteric modulators in rat Abstract Approaches to efficiently and accurately define the pharmacokinetics (PK) of large sets of small molecules in roden... |
PMC2809247 | core_pubmed_pmc | Co-administration of fluconazole increases nevirapine concentrations in HIV-infected Ugandans | Co-administration of fluconazole increases nevirapine concentrations in HIV-infected Ugandans Abstract Abstract Background Data from retrospective studies have suggested that there may be an interaction between fluconazole and nevirapine, increasing nevirapine concentrations and potentially leading to hepatotoxicity. M... |
PMC10222464 | core_pubmed_pmc | Pharmacokinetic Study and Metabolite Identification of CAM106 in Rats by Validated UHPLC-MS/MS | Pharmacokinetic Study and Metabolite Identification of CAM106 in Rats by Validated UHPLC-MS/MS Abstract Given the limitations of existing antiviral drugs and vaccines, there is still an urgent need for new anti-influenza drugs. CAM106, a rupestonic acid derivative, was studied for its potent antiviral activity and show... |
PMC5642551 | core_pubmed_pmc | A new donors’ CYP3A5 and recipients’ CYP3A4 cluster predicting tacrolimus disposition, and new-onset hypertension in Chinese liver transplant patients | A new donors’ CYP3A5 and recipients’ CYP3A4 cluster predicting tacrolimus disposition, and new-onset hypertension in Chinese liver transplant patients Abstract Aim The purpose of the current study was to investigate individualized therapy of tacrolimus (Tac), as well as complications after liver transplantation (LT) wi... |
PMC10204800 | core_pubmed_pmc | Deuterated buprenorphine retains pharmacodynamic properties of buprenorphine and resists metabolism to the active metabolite norbuprenorphine in rats | Deuterated buprenorphine retains pharmacodynamic properties of buprenorphine and resists metabolism to the active metabolite norbuprenorphine in rats Abstract Introduction: An active metabolite of buprenorphine ( BUP ), called norbuprenorphine ( NorBUP ), is implicated in neonatal opioid withdrawal syndrome when BUP is... |
PMC12599041 | core_pubmed_pmc | The role of gut microbiota tyrosine decarboxylases in levodopa pharmacokinetics: insights from a levodopa challenge test | The role of gut microbiota tyrosine decarboxylases in levodopa pharmacokinetics: insights from a levodopa challenge test Abstract Background The gut microbiota is known to influence levodopa metabolism in the intestinal tract, primarily through the action of tyrosine decarboxylase, an enzyme encoded by the tyrosine dec... |
PMC4875923 | core_pubmed_pmc | Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination | Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination Abstract Introduction The co-existence of malaria with bacterial infections is common in the tropics, hence the concurrent use of antimalarials and antibiotics. Objective This study aimed to investigate the effect on pharmac... |
PMC6175414 | core_pubmed_pmc | Tracking the Sugar Rush: Incorporating Continuous Glucose Monitoring Into Multisite Early Clinical Research With Type 2 Diabetes Subjects | Tracking the Sugar Rush: Incorporating Continuous Glucose Monitoring Into Multisite Early Clinical Research With Type 2 Diabetes Subjects Abstract Abstract Continuous glucose monitoring (CGM) systems allow patients with diabetes mellitus to closely track glucose concentrations over several days, identify trends in gluc... |
PMC6839502 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects Abstract PF-06751979 is a selective inhibitor of the beta-site amyloid precursor protein cleaving enzyme-1, which is ... |
PMC8877499 | core_pubmed_pmc | Ganciclovir Pharmacokinetics and Individualized Dosing Based on Covariate in Lung Transplant Recipients | Ganciclovir Pharmacokinetics and Individualized Dosing Based on Covariate in Lung Transplant Recipients Abstract Abstract The aim of this prospective study was to evaluate the pharmacokinetics of ganciclovir in lung transplant recipients, to explore its covariates, and to propose an individualized dosing regimen. Ganci... |
PMC5516238 | core_pubmed_pmc | Oral drug absorption in pediatrics: the intestinal wall, its developmental changes and current tools for predictions | Oral drug absorption in pediatrics: the intestinal wall, its developmental changes and current tools for predictions Abstract Abstract The dissolution, intestinal absorption and presystemic metabolism of a drug depend on its physicochemical characteristics but also on numerous physiological (e.g. gastrointestinal pH, v... |
PMC7759025 | core_pubmed_pmc | Screening for a Potential Therapeutic Agent from the Herbal Formula in the 4 th Edition of the Chinese National Guidelines for the Initial-Stage Management of COVID-19 via Molecular Docking | Screening for a Potential Therapeutic Agent from the Herbal Formula in the 4 th Edition of the Chinese National Guidelines for the Initial-Stage Management of COVID-19 via Molecular Docking Abstract Background COVID-19 caused by SARS-CoV-2 infection has been spreading through many countries since the end of 2019. The 4... |
PMC7254798 | core_pubmed_pmc | Insight into the Loading and Release Properties of MCM-48/Biopolymer Composites as Carriers for 5-Fluorouracil: Equilibrium Modeling and Pharmacokinetic Studies | Insight into the Loading and Release Properties of MCM-48/Biopolymer Composites as Carriers for 5-Fluorouracil: Equilibrium Modeling and Pharmacokinetic Studies Abstract Abstract The effect of the integration between MCM-48 and some biopolymers (starch, chitosan, and β-cyclodextrin) on enhancing the pharmaceutical prop... |
PMC7142887 | core_pubmed_pmc | Galleria mellonella for the Evaluation of Antifungal Efficacy against Medically Important Fungi, a Narrative Review | Galleria mellonella for the Evaluation of Antifungal Efficacy against Medically Important Fungi, a Narrative Review Abstract Abstract The treatment of invasive fungal infections remains challenging and the emergence of new fungal pathogens as well as the development of resistance to the main antifungal drugs highlight ... |
PMC10196430 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of tacrolimus for food–drug and CYP3A drug–drug–gene interaction predictions | Physiologically based pharmacokinetic modeling of tacrolimus for food–drug and CYP3A drug–drug–gene interaction predictions Abstract Abstract The immunosuppressant and narrow therapeutic index drug tacrolimus is metabolized mainly via cytochrome P450 (CYP) 3A4 and CYP3A5. For its pharmacokinetics (PK), high inter‐ and ... |
PMC11772993 | core_pubmed_pmc | The graded heat-health risk forecast and early warning with full-season coverage across China: a predicting model development and evaluation study | The graded heat-health risk forecast and early warning with full-season coverage across China: a predicting model development and evaluation study Abstract Summary Background Due to global climate change, high temperature and heatwaves have become critical issues that pose a threat to human health. An effective early w... |
PMC3414211 | core_pubmed_pmc | Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption | Lipid-based liquid crystalline nanoparticles as oral drug delivery vehicles for poorly water-soluble drugs: cellular interaction and in vivo absorption Abstract Background Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as novel drug-delivery systems for improving the bioavailabilit... |
PMC7496896 | core_pubmed_pmc | Regional Differences in Penetration of the Protein Stabilizer Trimethoprim (TMP) in the Rat Central Nervous System | Regional Differences in Penetration of the Protein Stabilizer Trimethoprim (TMP) in the Rat Central Nervous System Abstract Abstract Regulating gene expression at the protein level is becoming increasingly important for answering basic questions in neurobiology. Several techniques using destabilizing domains (DD) on tr... |
PMC9774644 | core_pubmed_pmc | Population Pharmacokinetic Analysis Proves Superiority of Continuous Infusion in PK/PD Target Attainment with Oxacillin in Staphylococcal Infections | Population Pharmacokinetic Analysis Proves Superiority of Continuous Infusion in PK/PD Target Attainment with Oxacillin in Staphylococcal Infections Abstract Considering its very short elimination half-life, the approved oxacillin dosage might not be sufficient to maintain the pharmacokinetic/pharmacodynamics (PK/PD) t... |
PMC10711279 | core_pubmed_pmc | Overcoming the clinical challenges of traditional ayahuasca: a first-in-human trial exploring novel routes of administration of N,N-Dimethyltryptamine and harmine | Overcoming the clinical challenges of traditional ayahuasca: a first-in-human trial exploring novel routes of administration of N,N-Dimethyltryptamine and harmine Abstract Abstract Recently, the Amazonian plant medicine “ayahuasca”—containing the psychedelic compound N,N-dimethyltryptamine (DMT) and numerous β-carbolin... |
PMC9393097 | core_pubmed_pmc | Population-Based Pharmacokinetics and Dose Optimization of Imipenem in Vietnamese Critically-Ill Patients | Population-Based Pharmacokinetics and Dose Optimization of Imipenem in Vietnamese Critically-Ill Patients Abstract Purpose The purpose of this study was to characterize the population-based pharmacokinetic (POP-PK) profile of imipenem in Vietnamese adult patients and to assess the probability of target attainment (PTA)... |
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