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PMC5101708
core_pubmed_pmc
Low heritability in pharmacokinetics of talinolol: a pharmacogenetic twin study on the heritability of the pharmacokinetics of talinolol, a putative probe drug of MDR1 and other membrane transporters
Low heritability in pharmacokinetics of talinolol: a pharmacogenetic twin study on the heritability of the pharmacokinetics of talinolol, a putative probe drug of MDR1 and other membrane transporters Abstract Background Efflux transporters like MDR1 and MRP2 may modulate the pharmacokinetics of about 50 % of all drugs....
PMC5618157
core_pubmed_pmc
The Role of Disulfide Bond Replacements in Analogues of the Tarantula Toxin ProTx-II and Their Effects on Inhibition of the Voltage-Gated Sodium Ion Channel Na v 1.7
The Role of Disulfide Bond Replacements in Analogues of the Tarantula Toxin ProTx-II and Their Effects on Inhibition of the Voltage-Gated Sodium Ion Channel Na v 1.7 Abstract Spider venom toxins, such as Protoxin-II (ProTx-II), have recently received much attention as selective Na v 1.7 channel blockers, with potential...
PMC12783437
core_pubmed_pmc
Secukinumab in the Treatment of Moderate‐to‐Severe Hidradenitis Suppurativa: Pooled Pharmacokinetics and Safety Results From the SUNSHINE and SUNRISE Phase 3 Studies
Secukinumab in the Treatment of Moderate‐to‐Severe Hidradenitis Suppurativa: Pooled Pharmacokinetics and Safety Results From the SUNSHINE and SUNRISE Phase 3 Studies Abstract ABSTRACT Background Secukinumab, a fully human, monoclonal antibody targeting interleukin‐17A, is approved for moderate‐to‐severe HS in adults. T...
PMC10902014
core_pubmed_pmc
Pharmacodynamic effects of the PARP inhibitor talazoparib (MDV3800, BMN 673) in patients with BRCA -mutated advanced solid tumors
Pharmacodynamic effects of the PARP inhibitor talazoparib (MDV3800, BMN 673) in patients with BRCA -mutated advanced solid tumors Abstract Abstract Purpose Talazoparib is an inhibitor of the poly (ADP-ribose) polymerase (PARP) family of enzymes and is FDA-approved for patients with (suspected) deleterious germline BRCA...
PMC6283804
core_pubmed_pmc
Biodistribution, pharmacokinetics, and organ-level dosimetry for 188 Re-AHDD-Lipiodol radioembolization based on quantitative post-treatment SPECT/CT scans
Biodistribution, pharmacokinetics, and organ-level dosimetry for 188 Re-AHDD-Lipiodol radioembolization based on quantitative post-treatment SPECT/CT scans Abstract Background Rhenium-188-labelled-Lipiodol radioembolization is a safe and cost-effective treatment for primary liver cancer. In order to determine correlati...
PMC6321138
core_pubmed_pmc
Food Bioactive Compounds and Their Interference in Drug Pharmacokinetic/Pharmacodynamic Profiles
Food Bioactive Compounds and Their Interference in Drug Pharmacokinetic/Pharmacodynamic Profiles Abstract Preclinical and clinical studies suggest that many food molecules could interact with drug transporters and metabolizing enzymes through different mechanisms, which are predictive of what would be observed clinical...
PMC8777709
core_pubmed_pmc
Real-Time Optimization of Pharmacodynamic Target Attainment at Infection Site during Treatment of Post-Neurosurgical Ventriculitis Caused by Carbapenem-Resistant Gram Negatives with Ceftazidime–Avibactam-Based Regimens: A Report of Two Cases
Real-Time Optimization of Pharmacodynamic Target Attainment at Infection Site during Treatment of Post-Neurosurgical Ventriculitis Caused by Carbapenem-Resistant Gram Negatives with Ceftazidime–Avibactam-Based Regimens: A Report of Two Cases Abstract Abstract We present two cases of post-neurosurgical ventriculitis cau...
PMC11646372
core_pubmed_pmc
Determination of Nemonoxacin in Small Volumes of Rat Plasma and Bile by a Novel HPLC-Fluorescence Assay and Its Application to Disposition and Biliary Excretion Kinetics
Determination of Nemonoxacin in Small Volumes of Rat Plasma and Bile by a Novel HPLC-Fluorescence Assay and Its Application to Disposition and Biliary Excretion Kinetics Abstract Background Nemonoxacin is a novel non-fluorinated quinolone antibiotic for the treatment of community-acquired pneumonia. To investigate the ...
PMC9243301
core_pubmed_pmc
An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma
An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma Abstract Relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, has been well studied in the treatment of endometriosis symptomatic. It is mainly metabolized by the CYP3A subfamily of P450 enzymes, while minorly ...
PMC5559493
core_pubmed_pmc
Increased Body Exposure to New Anti-Trypanosomal Through Nanoencapsulation
Increased Body Exposure to New Anti-Trypanosomal Through Nanoencapsulation Abstract Lychnopholide, a lipophilic sesquiterpene lactone, is efficacious in mice at the acute and chronic phases of Chagas disease. Conventional poly-ε-caprolactone (PCL) and long-circulating poly(D,L-lactide)- block -polyethylene glycol (PLA-...
PMC3506129
core_pubmed_pmc
Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors
Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors Abstract Inhibitors of checkpoint kinase 1 (CHK1) are of current interest as potential antitumor agents, but the most advanced inhibitor series reported to date are not orally bioavailable. A novel...
PMC9792776
core_pubmed_pmc
Potential drug-drug interaction of olverembatinib (HQP1351) using physiologically based pharmacokinetic models
Potential drug-drug interaction of olverembatinib (HQP1351) using physiologically based pharmacokinetic models Abstract Olverembatinib (HQP1351) is a third-generation BCR-ABL tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia (CML) (including T315I-mutant disease), exhibits drug-drug interaction (D...
PMC10440559
core_pubmed_pmc
Erianin: A phytoestrogen with therapeutic potential
Erianin: A phytoestrogen with therapeutic potential Abstract Erianin, a phytoestrogen with therapeutic potential, is one of the major active components of Dendrobll caulis. Erianin has a variety of pharmacological effects, such as anti-tumor, anti-inflammatory, anti-diabetic retinopathy, anti-psoriasis, and antibacteri...
PMC8307065
core_pubmed_pmc
Is Hypoxia a Factor Influencing PSMA-Directed Radioligand Therapy?—An In Silico Study on the Role of Chronic Hypoxia in Prostate Cancer
Is Hypoxia a Factor Influencing PSMA-Directed Radioligand Therapy?—An In Silico Study on the Role of Chronic Hypoxia in Prostate Cancer Abstract Abstract Simple Summary Tumor hypoxia is considered a critical factor associated with the resistance of conventional radiotherapy, where the X-ray-induced free radicals lead t...
PMC8309057
core_pubmed_pmc
The Role of Mathematical Models in Immuno-Oncology: Challenges and Future Perspectives
The Role of Mathematical Models in Immuno-Oncology: Challenges and Future Perspectives Abstract Immuno-oncology (IO) focuses on the ability of the immune system to detect and eliminate cancer cells. Since the approval of the first immune checkpoint inhibitor, immunotherapies have become a major player in oncology treat...
PMC5059567
core_pubmed_pmc
Valproic Acid, a Histone Deacetylase Inhibitor, in Combination with Paclitaxel for Anaplastic Thyroid Cancer: Results of a Multicenter Randomized Controlled Phase II/III Trial
Valproic Acid, a Histone Deacetylase Inhibitor, in Combination with Paclitaxel for Anaplastic Thyroid Cancer: Results of a Multicenter Randomized Controlled Phase II/III Trial Abstract Anaplastic thyroid cancer (ATC) has a median survival less than 5 months and, to date, no effective therapy exists. Taxanes have recent...
PMC11940229
core_pubmed_pmc
How Plant Polyhydroxy Flavonoids Can Hinder the Metabolism of Cytochrome 3A4
How Plant Polyhydroxy Flavonoids Can Hinder the Metabolism of Cytochrome 3A4 Abstract Abstract Background/Objectives : Recent interest in dietary components and their effects on xenobiotic metabolism has highlighted their role in modulating drug pharmacokinetics. Cytochrome P450 3A4, a key isoform of the cytochrome P45...
PMC4007078
core_pubmed_pmc
The c-Abl inhibitor, Nilotinib, protects dopaminergic neurons in a preclinical animal model of Parkinson's disease
The c-Abl inhibitor, Nilotinib, protects dopaminergic neurons in a preclinical animal model of Parkinson's disease Abstract Abstract c-Abl is activated in the brain of Parkinson's disease (PD) patients and in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-intoxicated mice where it inhibits parkin through tyrosine ...
PMC4894244
core_pubmed_pmc
A Randomized, Double-Blind, Double-Dummy Study to Evaluate the Intranasal Human Abuse Potential and Pharmacokinetics of a Novel Extended-Release Abuse-Deterrent Formulation of Oxycodone
A Randomized, Double-Blind, Double-Dummy Study to Evaluate the Intranasal Human Abuse Potential and Pharmacokinetics of a Novel Extended-Release Abuse-Deterrent Formulation of Oxycodone Abstract Abstract Objective . Evaluate the human abuse potential (HAP) of an experimental, microsphere-in-capsule formulation of exten...
PMC10974776
core_pubmed_pmc
In Vivo Pharmacokinetic Study of Polygonatum cyrtonema Polysaccharide DPC1 after Oral and Intraperitoneal Administration
In Vivo Pharmacokinetic Study of Polygonatum cyrtonema Polysaccharide DPC1 after Oral and Intraperitoneal Administration Abstract Abstract (1) Background: Polygonatum cyrtonema is a medicinal plant, and its polysaccharides are used for immunomodulation and the treatment of hyperglycemia. Investigation of the tissue dis...
PMC4900597
core_pubmed_pmc
Evaluation of the Effects of Pasireotide LAR Administration on Lymphocele Prevention after Axillary Node Dissection for Breast Cancer: Results of a Randomized Non-Comparative Phase 2 Study
Evaluation of the Effects of Pasireotide LAR Administration on Lymphocele Prevention after Axillary Node Dissection for Breast Cancer: Results of a Randomized Non-Comparative Phase 2 Study Abstract Objective The aim of this study was to assess the efficacy (response rate centered on 80%) of a somatostatin analog with h...
PMC6769095
core_pubmed_pmc
Population Pharmacokinetics of Risankizumab in Healthy Volunteers and Subjects with Moderate to Severe Plaque Psoriasis: Integrated Analyses of Phase I–III Clinical Trials
Population Pharmacokinetics of Risankizumab in Healthy Volunteers and Subjects with Moderate to Severe Plaque Psoriasis: Integrated Analyses of Phase I–III Clinical Trials Abstract Abstract Background and Objective Risankizumab is an anti-interleukin (IL)-23 monoclonal antibody being developed for treatment of moderate...
PMC12618442
core_pubmed_pmc
Modulating inflammation and oxidative stress in rheumatoid arthritis: a systematic review of nutraceutical interventions
Modulating inflammation and oxidative stress in rheumatoid arthritis: a systematic review of nutraceutical interventions Abstract Rheumatoid arthritis is a chronic autoimmune disease characterized by persistent synovial inflammation and progressive joint destruction. The gut microbiome has emerged as a key factor in th...
PMC5739562
core_pubmed_pmc
ATTACK, a novel bispecific T cell-recruiting antibody with trivalent EGFR binding and monovalent CD3 binding for cancer immunotherapy
ATTACK, a novel bispecific T cell-recruiting antibody with trivalent EGFR binding and monovalent CD3 binding for cancer immunotherapy Abstract ABSTRACT The redirection of T cell activity using bispecific antibodies is one of the most promising cancer immunotherapy approaches currently in development, but it is limited ...
PMC4349534
core_pubmed_pmc
Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxine in male Shiba goats
Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxine in male Shiba goats Abstract In the present study, we examined the oral pharmacokinetics of the acidic drugs, diclofenac (DF) and sulfamonomethoxine (SMM), which have different physicochemical properties, in Shiba goats. DF and SMM were intrav...
PMC7142831
core_pubmed_pmc
Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes
Preparation, characterization, pharmacokinetics and anticancer effects of PEGylated β-elemene liposomes Abstract Objective: This study aimed to develop a new polyethylene glycol (PEG)ylated β-elemene liposome (PEG-Lipo-β-E) and evaluate its characterization, pharmacokinetics, antitumor effects and safety in vitro and i...
PMC5890695
core_pubmed_pmc
Plasma and breast milk pharmacokinetics of emtricitabine, tenofovir and lamivudine using dried blood and breast milk spots in nursing African mother–infant pairs
Plasma and breast milk pharmacokinetics of emtricitabine, tenofovir and lamivudine using dried blood and breast milk spots in nursing African mother–infant pairs Abstract Abstract Background Breast milk transfer of first-line ART from mother to infant is not fully understood. Objectives To determine the concentrations ...
PMC12056735
core_pubmed_pmc
New nicotinamide–thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and in silico and in vitro evaluation †
New nicotinamide–thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and in silico and in vitro evaluation † Abstract Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development. In t...
PMC7396196
core_pubmed_pmc
Bradykinin 1 Receptor Antagonist BI1026706 Does Not Reduce Central Retinal Thickness in Center-Involved Diabetic Macular Edema
Bradykinin 1 Receptor Antagonist BI1026706 Does Not Reduce Central Retinal Thickness in Center-Involved Diabetic Macular Edema Abstract Purpose The bradykinin 1 receptor may be important in inflammatory retinal vascular leakage in diabetic macular edema. BI 1026706 is an antagonist of bradykinin 1 receptor that has dem...
PMC9381909
core_pubmed_pmc
The area under the effect curve as an efficacy determinant for anti‐infectives
The area under the effect curve as an efficacy determinant for anti‐infectives Abstract Abstract Pharmacokinetic/pharmacodynamic (PK/PD) indices making use of area under the curve, maximum concentration, and the duration that in vivo drug concentration is maintained above a critical level are commonly applied to clinic...
PMC11042912
core_pubmed_pmc
System Pharmacological Approach to Investigate and Validate Multitargeted and Therapeutic Effect of Furocoumarins of Apium graveolens L. for Treatment of Kidney Disease
System Pharmacological Approach to Investigate and Validate Multitargeted and Therapeutic Effect of Furocoumarins of Apium graveolens L. for Treatment of Kidney Disease Abstract Abstract Background System pharmacological approaches play important roles in drug discovery and development and in biomolecular exploration t...
PMC3847553
core_pubmed_pmc
Kinetic properties of “dual” orexin receptor antagonists at OX 1 R and OX 2 R orexin receptors
Kinetic properties of “dual” orexin receptor antagonists at OX 1 R and OX 2 R orexin receptors Abstract Abstract Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in clinical settings and thorough investigations of p...
PMC11403593
core_pubmed_pmc
Randomised, phase 1/2a trial of ION-827359, an antisense oligonucleotide inhibitor of ENaC
Randomised, phase 1/2a trial of ION-827359, an antisense oligonucleotide inhibitor of ENaC Abstract Abstract Background Hyperactivity of epithelial sodium channel (ENaC) with increased sodium absorption is a feature of cystic fibrosis (CF). ION-827359 is a 2.5-generation antisense oligonucleotide targeted to reduce ENa...
PMC12930602
core_pubmed_pmc
Population pharmacokinetics of a single bolus of ciprofol in Chinese pediatric patients
Population pharmacokinetics of a single bolus of ciprofol in Chinese pediatric patients Abstract Background Ciprofol is a recently developed sedative similar to propofol, but there is a lack of bolus pharmacokinetic data for ciprofol in children. Improved knowledge of ciprofol pharmacokinetics (PK) in children could he...
PMC5038257
core_pubmed_pmc
HIV-1 Coinfection Does Not Reduce Exposure to Rifampin, Isoniazid, and Pyrazinamide in South African Tuberculosis Outpatients
HIV-1 Coinfection Does Not Reduce Exposure to Rifampin, Isoniazid, and Pyrazinamide in South African Tuberculosis Outpatients Abstract There are contrasting data in the literature about antituberculosis plasma drug concentrations in HIV-1-coinfected patients. We report the pharmacokinetics of rifampin, isoniazid, and p...
PMC5906006
core_pubmed_pmc
The somatostatin receptor 2 antagonist 64 Cu-NODAGA-JR11 outperforms 64 Cu-DOTA-TATE in a mouse xenograft model
The somatostatin receptor 2 antagonist 64 Cu-NODAGA-JR11 outperforms 64 Cu-DOTA-TATE in a mouse xenograft model Abstract Abstract Copper-64 is an attractive radionuclide for PET imaging and is frequently used in clinical applications. The aim of this study was to perform a side-by-side comparison of the in vitro and in...
PMC12843740
core_pubmed_pmc
Suzetrigine, a Na V 1.8 Inhibitor as a Novel Approach for Pain Therapy—A Medicinal and Chemical Drug Profile
Suzetrigine, a Na V 1.8 Inhibitor as a Novel Approach for Pain Therapy—A Medicinal and Chemical Drug Profile Abstract Abstract Suzetrigine was approved by the US American Food and Drug Administration in 2025 as the first oral, non-opioid, selective inhibitor of Na V 1.8 sodium channel for the treatment of acute pain. T...
PMC8707499
core_pubmed_pmc
Computer-Based Drug Design of Positive Modulators of Store-Operated Calcium Channels to Prevent Synaptic Dysfunction in Alzheimer’s Disease
Computer-Based Drug Design of Positive Modulators of Store-Operated Calcium Channels to Prevent Synaptic Dysfunction in Alzheimer’s Disease Abstract Store-operated calcium entry (SOCE) constitutes a fine-tuning mechanism responsible for the replenishment of intracellular stores. Hippocampal SOCE is regulated by store-o...
PMC7818442
core_pubmed_pmc
The Oral Bioavailability and Metabolism of Midazolam in Stable Critically Ill Children: A Pharmacokinetic Microtracing Study
The Oral Bioavailability and Metabolism of Midazolam in Stable Critically Ill Children: A Pharmacokinetic Microtracing Study Abstract Midazolam is metabolized by the developmentally regulated intestinal and hepatic drug‐metabolizing enzyme cytochrome P450 (CYP) 3A4/5. It is frequently administered orally to children, y...
PMC8685769
core_pubmed_pmc
Curcumin Nanoparticles Inhibiting Ferroptosis for the Enhanced Treatment of Intracerebral Hemorrhage
Curcumin Nanoparticles Inhibiting Ferroptosis for the Enhanced Treatment of Intracerebral Hemorrhage Abstract Background Intracerebral hemorrhage (ICH) is a form of severe stroke, the pathology of which is tied closely to a recently discovered form of programmed cell death known as ferroptosis. Curcumin (Cur) is a comm...
PMC9796478
core_pubmed_pmc
Population Pharmacokinetics of Tralokinumab in Adult Subjects With Moderate to Severe Atopic Dermatitis
Population Pharmacokinetics of Tralokinumab in Adult Subjects With Moderate to Severe Atopic Dermatitis Abstract Abstract Tralokinumab is the first biologic therapy for moderate‐to‐severe atopic dermatitis (AD) that specifically neutralizes interleukin‐13 activity, a key driver of AD signs and symptoms. Tralokinumab is...
PMC4354399
core_pubmed_pmc
A pharmacokinetic and pharmacodynamic drug interaction between rosuvastatin and valsartan in healthy subjects
A pharmacokinetic and pharmacodynamic drug interaction between rosuvastatin and valsartan in healthy subjects Abstract Purpose Valsartan, an angiotensin-receptor blocker, and rosuvastatin, a competitive inhibitor of the 3-hydroxy-3-methylglutaryl coenzyme A reductase, are frequently coadministered to treat patients wit...
PMC11707736
core_pubmed_pmc
Current State and New Horizons in Applications of Physiologically Based Biopharmaceutics Modeling (PBBM): A Workshop Report
Current State and New Horizons in Applications of Physiologically Based Biopharmaceutics Modeling (PBBM): A Workshop Report Abstract This report summarizes the proceedings for Day 3 of the workshop titled “ Physiologically Based Biopharmaceutics Modeling (PBBM) Best Practices for Drug Product Quality: Regulatory and In...
PMC8466382
core_pubmed_pmc
What Matters in Piglets’ Exposure to Antibiotics Administered through Drinking Water?
What Matters in Piglets’ Exposure to Antibiotics Administered through Drinking Water? Abstract A number of drugs are given in drinking water in piglet farming, although this way of administering drugs leads to significant and uncontrolled variability in exposures. Three main explanations for this variability have been ...
PMC10206227
core_pubmed_pmc
Characterization of pharmacogenomic variants in a Brazilian admixed cohort of elderly individuals based on whole-genome sequencing data
Characterization of pharmacogenomic variants in a Brazilian admixed cohort of elderly individuals based on whole-genome sequencing data Abstract Abstract Introduction: Research in the field of pharmacogenomics (PGx) aims to identify genetic variants that modulate response to drugs, through alterations in their pharmaco...
PMC10964632
core_pubmed_pmc
A phase II study of belumosudil for chronic graft-versus-host disease in patients who failed at least one line of systemic therapy in China
A phase II study of belumosudil for chronic graft-versus-host disease in patients who failed at least one line of systemic therapy in China Abstract Background Chronic graft-versus-host disease (cGVHD) is an immune-related disorder that is the most common complication post-allogenic hematopoietic stem cell transplant. ...
PMC4519271
core_pubmed_pmc
Comparative Pharmacokinetics and Allometric Scaling of Carboplatin in Different Avian Species
Comparative Pharmacokinetics and Allometric Scaling of Carboplatin in Different Avian Species Abstract The use of chemotherapeutics as a possible treatment strategy in avian oncology is steadily increasing over the last years. Despite this, literature reports regarding dosing strategies and pharmacokinetic behaviour of...
PMC12389332
core_pubmed_pmc
Development of PBPK Population Model for End-Stage Renal Disease Patients to Inform OATP1B-, BCRP-, P-gp-, and CYP3A4-Mediated Drug Disposition with Individual Influencing Factors
Development of PBPK Population Model for End-Stage Renal Disease Patients to Inform OATP1B-, BCRP-, P-gp-, and CYP3A4-Mediated Drug Disposition with Individual Influencing Factors Abstract Background/Objective: Physiologically based pharmacokinetic (PBPK) modeling is a powerful tool for predicting pharmacokinetics (PK)...
PMC11860141
core_pubmed_pmc
General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics
General Anesthetics: Aspects of Chirality, Pharmacodynamics, and Pharmacokinetics Abstract The introduction of general anesthetics in the mid-19th century is considered one of the greatest contributions to medical practice. It was the first time that complicated surgical interventions became feasible, without putting a...
PMC12508180
core_pubmed_pmc
Pharmaceutical and biomedical challenges for crew autonomy in health preservation during future exploration missions
Pharmaceutical and biomedical challenges for crew autonomy in health preservation during future exploration missions Abstract Human space missions beyond Low Earth Orbit (LEO), such as to the Moon and Mars, will require increased crew autonomy in health management, due to communication delays and limited resupply. Thes...
PMC4518096
core_pubmed_pmc
Design and Comparative Evaluation of In-vitro Drug Release, Pharmacokinetics and Gamma Scintigraphic Analysis of Controlled Release Tablets Using Novel pH Sensitive Starch and Modified Starch- acrylate Graft Copolymer Matrices
Design and Comparative Evaluation of In-vitro Drug Release, Pharmacokinetics and Gamma Scintigraphic Analysis of Controlled Release Tablets Using Novel pH Sensitive Starch and Modified Starch- acrylate Graft Copolymer Matrices Abstract The present investigation deals with the development of controlled release tablets o...
PMC10993776
core_pubmed_pmc
Advancing the utilization of real‐world data and real‐world evidence in clinical pharmacology and translational research—Proceedings from the ASCPT 2023 preconference workshop
Advancing the utilization of real‐world data and real‐world evidence in clinical pharmacology and translational research—Proceedings from the ASCPT 2023 preconference workshop Abstract Abstract Real‐world data (RWD) and real‐world evidence (RWE) are now being routinely used in epidemiology, clinical practice, and post‐...
PMC4241044
core_pubmed_pmc
An open-label study to estimate the effect of steady-state erythromycin on the pharmacokinetics, pharmacodynamics, and safety of a single dose of rivaroxaban in subjects with renal impairment and normal renal function
An open-label study to estimate the effect of steady-state erythromycin on the pharmacokinetics, pharmacodynamics, and safety of a single dose of rivaroxaban in subjects with renal impairment and normal renal function Abstract Two previously conducted rivaroxaban studies showed that, separately, renal impairment (RI) a...
PMC6571683
core_pubmed_pmc
Pharmacodynamics of Five Anthraquinones (Aloe-emodin, Emodin, Rhein, Chysophanol, and Physcion) and Reciprocal Pharmacokinetic Interaction in Rats with Cerebral Ischemia
Pharmacodynamics of Five Anthraquinones (Aloe-emodin, Emodin, Rhein, Chysophanol, and Physcion) and Reciprocal Pharmacokinetic Interaction in Rats with Cerebral Ischemia Abstract (1) Background: Rhubarb anthraquinones—a class of components with neuroprotective function—can be used to alleviate cerebral ischemia reperfu...
PMC10766906
core_pubmed_pmc
A novel, small-volume subcutaneous furosemide formulation delivered by an abdominal patch infusor device in patients with heart failure: results of two phase I studies
A novel, small-volume subcutaneous furosemide formulation delivered by an abdominal patch infusor device in patients with heart failure: results of two phase I studies Abstract Abstract Aims Subcutaneous (SC) furosemide has potential advantages over intravenous (IV) furosemide by enabling self-administration or adminis...
PMC10610097
core_pubmed_pmc
The Combination of Predictive Factors of Pharmacokinetic Origin Associates with Enhanced Disease Control during Treatment of Pediatric Crohn’s Disease with Infliximab
The Combination of Predictive Factors of Pharmacokinetic Origin Associates with Enhanced Disease Control during Treatment of Pediatric Crohn’s Disease with Infliximab Abstract Abstract Infliximab (IFX) concentrations are a predictive factor (PF) of pharmacokinetic (PK) origin in the treatment of Crohn’s disease (CD). W...
PMC3062127
core_pubmed_pmc
Effect of esomeprazole on the pharmacokinetics of carbamazepine
Effect of esomeprazole on the pharmacokinetics of carbamazepine Abstract Abstract Objective: Present study was carried out to evaluate effect of esomeprazole on the pharmacokinetics of carbamazepine in rabbits. Materials and Methods: Study was conducted at Department of Pharmacology, Postgraduate Institute of Medical E...
PMC12714604
core_pubmed_pmc
Association of pharmacokinetic biomarkers with early immune recovery following HLA-haploidentical hematopoietic cell transplantation
Association of pharmacokinetic biomarkers with early immune recovery following HLA-haploidentical hematopoietic cell transplantation Abstract Background Prophylactic immunosuppressants for graft-versus-host disease (GVHD) in allogeneic hematopoietic cell transplantation (alloHCT), including post-transplant cyclophospha...
PMC9598364
core_pubmed_pmc
The Combination of Amoxicillin and 1,8-Cineole Improves the Bioavailability and the Therapeutic Effect of Amoxicillin in a Rabbit Model
The Combination of Amoxicillin and 1,8-Cineole Improves the Bioavailability and the Therapeutic Effect of Amoxicillin in a Rabbit Model Abstract In this study, the effectiveness of the combination therapy of 1,8-cineole with amoxicillin (AMX) and clavulanic acid (Clav) was investigated. For this, the pharmacokinetic be...
PMC8441157
core_pubmed_pmc
Drug-drug interactions between palbociclib and proton pump inhibitors may significantly affect clinical outcome of metastatic breast cancer patients
Drug-drug interactions between palbociclib and proton pump inhibitors may significantly affect clinical outcome of metastatic breast cancer patients Abstract Abstract Background Proton-pump-inhibitors (PPIs) are frequently prescribed for the management of anticancer drug-related gastrointestinal symptoms. Palbociclib i...
PMC11381307
core_pubmed_pmc
In vitro mechanistic study on mycophenolate mofetil drug interactions: effect of prednisone, cyclosporine, and others
In vitro mechanistic study on mycophenolate mofetil drug interactions: effect of prednisone, cyclosporine, and others Abstract Abstract Objective The metabolism- and transporter-based drug-drug interactions (DDIs) between mycophenolate mofetil (MMF) and co-administered medications may be key factors for the high indivi...
PMC7641258
core_pubmed_pmc
Pharmacological principles guiding prolonged glucocorticoid treatment in ARDS
Pharmacological principles guiding prolonged glucocorticoid treatment in ARDS Abstract Current literature addressing the pharmacological principles guiding glucocorticoid (GC) administration in ARDS is scant. This paucity of information may have led to the heterogeneity of treatment protocols and misinterpretation of a...
PMC5404566
core_pubmed_pmc
Age, Weight, and CYP2D6 Genotype Are Major Determinants of Primaquine Pharmacokinetics in African Children
Age, Weight, and CYP2D6 Genotype Are Major Determinants of Primaquine Pharmacokinetics in African Children Abstract ABSTRACT Low-dose primaquine is recommended to prevent Plasmodium falciparum malaria transmission in areas threatened by artemisinin resistance and areas aiming for malaria elimination. Community treatmen...
PMC8195918
core_pubmed_pmc
Evaluation of the Pharmacokinetic Interaction and Safety of Atogepant Co-Administered with Acetaminophen or Naproxen in Healthy Participants: A Randomized Trial
Evaluation of the Pharmacokinetic Interaction and Safety of Atogepant Co-Administered with Acetaminophen or Naproxen in Healthy Participants: A Randomized Trial Abstract Abstract Background Atogepant is an oral calcitonin gene-related peptide (CGRP) receptor antagonist in development for preventive treatment of migrain...
PMC3224713
core_pubmed_pmc
Long-circulating delivery of bioactive polysaccharide from radix ophiopogonis by PEGylation
Long-circulating delivery of bioactive polysaccharide from radix ophiopogonis by PEGylation Abstract Background Radix ophiopogonis polysaccharide (ROP) has been found to be effective against myocardial ischemia. One of main problems with its use is its short in-vivo half-life, which makes the development of an effectiv...
PMC10053806
core_pubmed_pmc
Building a Human Physiologically Based Pharmacokinetic Model for Aflatoxin B1 to Simulate Interactions with Drugs
Building a Human Physiologically Based Pharmacokinetic Model for Aflatoxin B1 to Simulate Interactions with Drugs Abstract Mycotoxins such as aflatoxin B1 (AFB1) are secondary fungal metabolites present in food commodities and part of one’s daily exposure, especially in certain regions, e.g., sub-Saharan Africa. AFB1 i...
PMC12624433
core_pubmed_pmc
Atomoxetine Drug Properties for Repurposing as a Candidate Alzheimer’s Disease Therapeutic Agent
Atomoxetine Drug Properties for Repurposing as a Candidate Alzheimer’s Disease Therapeutic Agent Abstract Ongoing Alzheimer’s disease (AD) drug development research addresses the need for therapeutic agents that can ameliorate cognitive symptoms and attenuate the course of AD synaptic deficits and neurodegeneration. Th...
PMC5419648
core_pubmed_pmc
Pharmacokinetic modeling of gentamicin in treatment of infective endocarditis: Model development and validation of existing models
Pharmacokinetic modeling of gentamicin in treatment of infective endocarditis: Model development and validation of existing models Abstract Gentamicin shows large variations in half-life and volume of distribution (Vd) within and between individuals. Thus, monitoring and accurately predicting serum levels are required ...
PMC5765392
core_pubmed_pmc
Exposure‐response relationship of certolizumab pegol induction and maintenance therapy in patients with Crohn's disease
Exposure‐response relationship of certolizumab pegol induction and maintenance therapy in patients with Crohn's disease Abstract Summary Background Therapeutic drug monitoring may optimize therapy for Crohn's disease (CD). Aim To use a population pharmacokinetic model that accounts for the time‐varying nature of covari...
PMC5511024
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and tolerability of verinurad, a selective uric acid reabsorption inhibitor, in healthy adult male subjects
Pharmacokinetics, pharmacodynamics, and tolerability of verinurad, a selective uric acid reabsorption inhibitor, in healthy adult male subjects Abstract Abstract Purpose Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for the treatment of gout and asymptomatic hyperuricemia....
PMC10867190
core_pubmed_pmc
Determination of glomerular filtration rate “en passant” after high doses of iohexol for computed tomography in intensive care medicine—a proof of concept
Determination of glomerular filtration rate “en passant” after high doses of iohexol for computed tomography in intensive care medicine—a proof of concept Abstract Accurate assessment of renal function is of great clinical and scientific importance, as it is an important pharmacokinetic covariate of pivotal drugs. The ...
PMC10301887
core_pubmed_pmc
Intranasal Microemulsion as an Innovative and Promising Alternative to the Oral Route in Improving Stiripentol Brain Targeting
Intranasal Microemulsion as an Innovative and Promising Alternative to the Oral Route in Improving Stiripentol Brain Targeting Abstract Stiripentol (STP) is a new-generation antiepileptic only available for oral administration. However, it is extremely unstable in acidic environments and undergoes gastrointestinal slow...
PMC8185251
core_pubmed_pmc
Pharmacokinetics and Safety of an Intravitreal Humanized Anti-VEGF-A Monoclonal Antibody (PRO-169), a Biosimilar Candidate to Bevacizumab
Pharmacokinetics and Safety of an Intravitreal Humanized Anti-VEGF-A Monoclonal Antibody (PRO-169), a Biosimilar Candidate to Bevacizumab Abstract Abstract Background PRO-169 is a biosimilar candidate to bevacizumab (BEV), a monoclonal antibody (mAb) that inhibits vascular endothelial growth factor-A (VEGF-A) developed...
PMC3072488
core_pubmed_pmc
Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
Why pharmacokinetic differences among oral triptans have little clinical importance: a comment Abstract Abstract Triptans, selective 5-HT1B/1D receptor agonists, are specific drugs for the acute treatment of migraine that have the same mechanism of action. Here, it is discussed why the differences among kinetic paramet...
PMC11155381
core_pubmed_pmc
Crafting Docetaxel-Loaded Albumin Nanoparticles Through a Novel Thermal-Driven Self-Assembly/Microfluidic Combination Technology: Formulation, Process Optimization, Stability, and Bioavailability
Crafting Docetaxel-Loaded Albumin Nanoparticles Through a Novel Thermal-Driven Self-Assembly/Microfluidic Combination Technology: Formulation, Process Optimization, Stability, and Bioavailability Abstract Background The commercial docetaxel (DTX) formulation causes severe side effects due to polysorbate 80 and ethanol....
PMC4111663
core_pubmed_pmc
Enhanced oral absorption and therapeutic effect of acetylpuerarin based on D-α-tocopheryl polyethylene glycol 1000 succinate nanoemulsions
Enhanced oral absorption and therapeutic effect of acetylpuerarin based on D-α-tocopheryl polyethylene glycol 1000 succinate nanoemulsions Abstract Abstract Background Acetylpuerarin (AP), because of its lower water solubility, shows poor absorption that hinders its therapeutic application. Thus, the aim of this study ...
PMC4448982
core_pubmed_pmc
LP-925219 maximizes urinary glucose excretion in mice by inhibiting both renal SGLT1 and SGLT2
LP-925219 maximizes urinary glucose excretion in mice by inhibiting both renal SGLT1 and SGLT2 Abstract Abstract Sodium-glucose cotransporter 2 (SGLT2) inhibitors are a new class of oral anti-diabetic agents that improve glycemic control by inhibiting SGLT2-mediated renal glucose reabsorption. Currently available agent...
PMC11315818
core_pubmed_pmc
A Randomized, Open-Label, Phase I, Single-Dose Study of Antisense Oligonucleotide, Vupanorsen, in Chinese Adults with Elevated Triglycerides
A Randomized, Open-Label, Phase I, Single-Dose Study of Antisense Oligonucleotide, Vupanorsen, in Chinese Adults with Elevated Triglycerides Abstract Abstract Background Vupanorsen is a GalNAc 3 -conjugated antisense oligonucleotide targeting angiopoietin-like 3 (ANGPTL3) mRNA shown to reduce atherogenic lipoproteins i...
PMC12730041
core_pubmed_pmc
Peri-Operative Dosage and Therapeutic Concentrations of Cefazolin Administered for Surgical Site Infection Prophylaxis in Elective Surgery—A Systematic Review
Peri-Operative Dosage and Therapeutic Concentrations of Cefazolin Administered for Surgical Site Infection Prophylaxis in Elective Surgery—A Systematic Review Abstract Background/Objectives : Cefazolin is commonly administered for surgical antibiotic prophylaxis. This review aims to examine whether target unbound plasm...
PMC10271881
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Kukoamine B in Healthy Volunteers: A Randomized, Double-Blind, Placebo-Controlled, Multiple-Dose Phase I Study
Safety, Tolerability, and Pharmacokinetics of Kukoamine B in Healthy Volunteers: A Randomized, Double-Blind, Placebo-Controlled, Multiple-Dose Phase I Study Abstract Abstract Introduction Kukoamine B (KB) is a novel sepsis therapeutic drug targeting lipopolysaccharide and CpG DNA. This study aims to evaluate the safety...
PMC8308683
core_pubmed_pmc
Pharmacokinetic Properties of the Novel Synthetic Cannabinoid 5F-APINAC and Its Influence on Metabolites Associated with Neurotransmission in Rabbit Plasma
Pharmacokinetic Properties of the Novel Synthetic Cannabinoid 5F-APINAC and Its Influence on Metabolites Associated with Neurotransmission in Rabbit Plasma Abstract The strong psychoactive effects of synthetic cannabinoids raise the need for the deeper studying of their neurometabolic effects. The pharmacokinetic prope...
PMC9902557
core_pubmed_pmc
PANTHER: AZD8931, inhibitor of EGFR, ERBB2 and ERBB3 signalling, combined with FOLFIRI: a Phase I/II study to determine the importance of schedule and activity in colorectal cancer
PANTHER: AZD8931, inhibitor of EGFR, ERBB2 and ERBB3 signalling, combined with FOLFIRI: a Phase I/II study to determine the importance of schedule and activity in colorectal cancer Abstract Background Epidermal growth factor receptor (EGFR) is a therapeutic target to which HER2/HER3 activation may contribute resistance...
PMC7026992
core_pubmed_pmc
Intrapulmonary concentrations of meropenem administered by continuous infusion in critically ill patients with nosocomial pneumonia: a randomized pharmacokinetic trial
Intrapulmonary concentrations of meropenem administered by continuous infusion in critically ill patients with nosocomial pneumonia: a randomized pharmacokinetic trial Abstract Background Optimal antimicrobial drug exposure in the lung is required for successful treatment outcomes for nosocomial pneumonia. Little is kn...
PMC8139433
core_pubmed_pmc
Tailored Pharmacokinetic model to predict drug trapping in long-term anesthesia
Tailored Pharmacokinetic model to predict drug trapping in long-term anesthesia Abstract Abstract Introduction In long-term induced general anesthesia cases such as those uniquely defined by the ongoing Covid-19 pandemic context, the clearance of hypnotic and analgesic drugs from the body follows anomalous diffusion wi...
PMC7076407
core_pubmed_pmc
Retinal Cell Protection in Ocular Excitotoxicity Diseases. Possible Alternatives Offered by Microparticulate Drug Delivery Systems and Future Prospects
Retinal Cell Protection in Ocular Excitotoxicity Diseases. Possible Alternatives Offered by Microparticulate Drug Delivery Systems and Future Prospects Abstract Abstract Excitotoxicity seems to play a critical role in ocular neurodegeneration. Excess-glutamate-mediated retinal ganglion cells death is the principal caus...
PMC4792355
core_pubmed_pmc
Single-dose pharmacokinetics and safety of azilsartan medoxomil in children and adolescents with hypertension as compared to healthy adults
Single-dose pharmacokinetics and safety of azilsartan medoxomil in children and adolescents with hypertension as compared to healthy adults Abstract Purpose This open-label, multicenter, single-dose study characterized the pharmacokinetics and short-term safety of azilsartan medoxomil (AZL-M) in hypertensive pediatric ...
PMC11881572
core_pubmed_pmc
Prediction of higher ceftazidime–avibactam concentrations in the human renal interstitium compared with unbound plasma using a minimal physiologically based pharmacokinetic model developed in rats and pigs through microdialysis
Prediction of higher ceftazidime–avibactam concentrations in the human renal interstitium compared with unbound plasma using a minimal physiologically based pharmacokinetic model developed in rats and pigs through microdialysis Abstract ABSTRACT Last resort antibiotics, like ceftazidime–avibactam (CZA), were used to tr...
PMC6304886
core_pubmed_pmc
Sinusoidal Obstruction Syndrome (SOS) in Multiple Myeloma with Renal Failure
Sinusoidal Obstruction Syndrome (SOS) in Multiple Myeloma with Renal Failure Abstract SOS is a rare complication of stem cell transplantation and has significant morbidity and mortality. We present three cases of SOS and highlight underlying risk factors for its development, such as impaired clearance of alkylating age...
PMC8364686
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses of BI 187004, an inhibitor of 11beta-hydroxysteroid dehydrogenase-1, in healthy male volunteers with overweight or obesity
Safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses of BI 187004, an inhibitor of 11beta-hydroxysteroid dehydrogenase-1, in healthy male volunteers with overweight or obesity Abstract Abstract Background The study characterizes safety, tolerability, pharmacokinetic and pharmacodynamic profi...
PMC12162304
core_pubmed_pmc
Integrated UPLC–MS/MS and UPLC–Q–TOF–MS/MS analysis to reveal pharmacokinetics, tissue distribution, metabolism, and excretion of sipeimine in rats
Integrated UPLC–MS/MS and UPLC–Q–TOF–MS/MS analysis to reveal pharmacokinetics, tissue distribution, metabolism, and excretion of sipeimine in rats Abstract Abstract Background and Objective Fritillaria Bulbus is a traditional Chinese medicine used to treat respiratory diseases such as cough, expectoration, and asthma ...
PMC6770524
core_pubmed_pmc
Novel Human Bispecific Aptamer–Antibody Conjugates for Efficient Cancer Cell Killing
Novel Human Bispecific Aptamer–Antibody Conjugates for Efficient Cancer Cell Killing Abstract Monoclonal antibodies have been approved by the Food and Drug Administration for the treatment of various human cancers. More recently, oligonucleotide aptamers have risen increasing attention for cancer therapy thanks to thei...
PMC9303465
core_pubmed_pmc
Venetoclax exposure‐efficacy and exposure‐safety relationships in patients with treatment‐naïve acute myeloid leukemia who are ineligible for intensive chemotherapy
Venetoclax exposure‐efficacy and exposure‐safety relationships in patients with treatment‐naïve acute myeloid leukemia who are ineligible for intensive chemotherapy Abstract Abstract This study evaluated venetoclax population pharmacokinetics (popPK) in patients with treatment‐naïve acute myeloid leukemia and assessed ...
PMC9046195
core_pubmed_pmc
Safety and serum distribution of anti-SARS-CoV-2 monoclonal antibody MAD0004J08 after intramuscular injection
Safety and serum distribution of anti-SARS-CoV-2 monoclonal antibody MAD0004J08 after intramuscular injection Abstract Abstract The emerging threat represented by SARS-CoV-2 variants, demands the development of therapies for better clinical management of COVID-19. MAD0004J08 is a potent Fc-engineered monoclonal antibod...
PMC11764037
core_pubmed_pmc
Nebulized aminoglycosides for ventilator-associated pneumonia: Methodological considerations and lessons from experimental studies
Nebulized aminoglycosides for ventilator-associated pneumonia: Methodological considerations and lessons from experimental studies Abstract Aminoglycosides are concentration-dependent antibiotics exerting a bactericidal effect when concentrations at the site of infection are equal to or greater than 5 times the minimum...
PMC11881624
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Milvexian in Healthy Chinese Adults
Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Milvexian in Healthy Chinese Adults Abstract Background Milvexian is a small molecule, selective factor XIa (FXIa) inhibitor being developed as an oral anticoagulant. This study assessed the pharmacokinetics, pharmacodynamics (activated partial thromboplas...
PMC12728533
core_pubmed_pmc
Computational Identification and Anti-Inflammatory Evaluation of T19093 as a TLR4/MD2 Inhibitor
Computational Identification and Anti-Inflammatory Evaluation of T19093 as a TLR4/MD2 Inhibitor Abstract Abstract Background The TLR4 (Toll-like receptor 4)/MD2 (Myeloid differentiation protein-2) is a crucial target for developing novel anti-inflammatory drugs. Nevertheless, current inhibitors often have significant a...
PMC12086410
core_pubmed_pmc
Proposed Denosumab Biosimilar SB16 vs Reference Denosumab in Postmenopausal Osteoporosis: Phase 3 Results Up to Month 12
Proposed Denosumab Biosimilar SB16 vs Reference Denosumab in Postmenopausal Osteoporosis: Phase 3 Results Up to Month 12 Abstract Abstract Context SB16 is a proposed biosimilar to reference denosumab (DEN; brand name: Prolia). Objective This phase 3 randomized, double-blind, multicenter study evaluated the biosimilarit...
PMC11007141
core_pubmed_pmc
Innovative research methodologies in the EU regulatory framework: an analysis of EMA qualification procedures from a pediatric perspective
Innovative research methodologies in the EU regulatory framework: an analysis of EMA qualification procedures from a pediatric perspective Abstract Abstract Introduction The European Medicines Agency (EMA) offers scientific advice to support the qualification procedure of novel methodologies, such as preclinical and in...
PMC9303191
core_pubmed_pmc
Bacterial growth dynamics and pharmacokinetic–pharmacodynamic relationships of rifampicin and bedaquiline in BALB/c mice
Bacterial growth dynamics and pharmacokinetic–pharmacodynamic relationships of rifampicin and bedaquiline in BALB/c mice Abstract Abstract Background and Purpose Translational efforts in the evaluation of novel anti‐tubercular drugs demand better integration of pharmacokinetic–pharmacodynamic data arising from preclini...
PMC11330186
core_pubmed_pmc
Physiologically‐based pharmacokinetic modeling of pantoprazole to evaluate the role of CYP2C19 genetic variation and obesity in the pediatric population
Physiologically‐based pharmacokinetic modeling of pantoprazole to evaluate the role of CYP2C19 genetic variation and obesity in the pediatric population Abstract Abstract Pantoprazole is a proton pump inhibitor indicated for the treatment of gastroesophageal reflux disease, a condition that disproportionately affects c...