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PMC3035000
core_pubmed_pmc
Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats
Different Influences on Tacrolimus Pharmacokinetics by Coadministrations of Zhi Ke and Zhi Shi in Rats Abstract Abstract Tacrolimus, an immunosuppressant with narrow therapeutic window, has been used widely in transplant patients. Grapefruit juice and pomelo have been reported to increase the blood levels of tacrolimus...
PMC10033566
core_pubmed_pmc
Systemic exposure to cisplatin and paclitaxel after intraperitoneal chemotherapy in ovarian cancer
Systemic exposure to cisplatin and paclitaxel after intraperitoneal chemotherapy in ovarian cancer Abstract Purpose To determine the systemic exposure to cisplatin and paclitaxel after adjuvant intraperitoneal administration in patients with advanced ovarian cancer who underwent primary debulking surgery. This could pr...
PMC7663170
core_pubmed_pmc
Antinociceptive Interaction and Pharmacokinetics of the Combination Treatments of Methyleugenol Plus Diclofenac or Ketorolac
Antinociceptive Interaction and Pharmacokinetics of the Combination Treatments of Methyleugenol Plus Diclofenac or Ketorolac Abstract Abstract Although nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the main types of drugs used to treat pain, they have several adverse effects, and such effects can be reduced ...
PMC4752255
core_pubmed_pmc
Comparison of Active Drug Concentrations in the Pulmonary Epithelial Lining Fluid and Interstitial Fluid of Calves Injected with Enrofloxacin, Florfenicol, Ceftiofur, or Tulathromycin
Comparison of Active Drug Concentrations in the Pulmonary Epithelial Lining Fluid and Interstitial Fluid of Calves Injected with Enrofloxacin, Florfenicol, Ceftiofur, or Tulathromycin Abstract Abstract Bacterial pneumonia is the most common reason for parenteral antimicrobial administration to beef cattle in the United...
PMC7261230
core_pubmed_pmc
Safety issues and harmful pharmacological interactions of nutritional supplements in Duchenne muscular dystrophy: considerations for Standard of Care and emerging virus outbreaks
Safety issues and harmful pharmacological interactions of nutritional supplements in Duchenne muscular dystrophy: considerations for Standard of Care and emerging virus outbreaks Abstract At the moment, little treatment options are available for Duchenne muscular dystrophy (DMD). The absence of the dystrophin protein l...
PMC8829821
core_pubmed_pmc
Awareness of Gadolinium Toxicity Among Non-radiologists in Saudi Arabia
Awareness of Gadolinium Toxicity Among Non-radiologists in Saudi Arabia Abstract Introduction and aim Gadolinium toxicity has been accompanied by side effects among patients scanned with MRI, especially patients with chronic renal insufficiency. The toxicity, pharmacokinetics, and pharmacodynamics of gadolinium-based c...
PMC7688195
core_pubmed_pmc
Physiologically Based Pharmacokinetic Models of Probenecid and Furosemide to Predict Transporter Mediated Drug-Drug Interactions
Physiologically Based Pharmacokinetic Models of Probenecid and Furosemide to Predict Transporter Mediated Drug-Drug Interactions Abstract Purpose To provide whole-body physiologically based pharmacokinetic (PBPK) models of the potent clinical organic anion transporter (OAT) inhibitor probenecid and the clinical OAT vic...
PMC4011913
core_pubmed_pmc
Quantitative cumulative biodistribution of antibodies in mice
Quantitative cumulative biodistribution of antibodies in mice Abstract The neonatal Fc receptor (FcRn) plays an important and well-known role in antibody recycling in endothelial and hematopoietic cells and thus it influences the systemic pharmacokinetics (PK) of immunoglobulin G (IgG). However, considerably less is kn...
PMC12460347
core_pubmed_pmc
Modulating the gut-immune axis to alleviate rheumatoid arthritis: mechanistic insights and therapeutic potential of traditional Chinese medicine
Modulating the gut-immune axis to alleviate rheumatoid arthritis: mechanistic insights and therapeutic potential of traditional Chinese medicine Abstract Abstract Rheumatoid arthritis (RA), a chronic autoimmune disorder marked by systemic inflammation and joint destruction, remains challenging to treat due to the limit...
PMC6589536
core_pubmed_pmc
Interactions between antidepressants, sleep aids and selected breast cancer therapy
Interactions between antidepressants, sleep aids and selected breast cancer therapy Abstract Abstract Depression and insomnia are very significant pathologies in cancer patients as they contribute to the patient’s overall cure and quality of life. Moreover, untreated depression and ongoing insomnia are associated with ...
PMC11324770
core_pubmed_pmc
A novel in vitro high-content imaging assay for the prediction of drug-induced lung toxicity
A novel in vitro high-content imaging assay for the prediction of drug-induced lung toxicity Abstract The development of inhaled drugs for respiratory diseases is frequently impacted by lung pathology in non-clinical safety studies. To enable design of novel candidate drugs with the right safety profile, predictive in ...
PMC9716937
core_pubmed_pmc
Evaluation of the Effect of Eslicarbazepine Acetate on the Pharmacokinetics of Perampanel in Rats by Isotope-Dilution-UHPLC-MS/MS
Evaluation of the Effect of Eslicarbazepine Acetate on the Pharmacokinetics of Perampanel in Rats by Isotope-Dilution-UHPLC-MS/MS Abstract Abstract Purpose The present study aimed to establish and validate an isotope-dilution-UHPLC-MS/MS method for the determination of perampanel (PER) concentration and investigate the...
PMC9241942
core_pubmed_pmc
A Vancomycin HPLC Assay for Use in Gut Microbiome Research
A Vancomycin HPLC Assay for Use in Gut Microbiome Research Abstract ABSTRACT The human microbiome project has revolutionized our understanding of the interaction between commensal microbes and human health. By far, the biggest perturbation of the microbiome involves use of broad-spectrum antibiotics excreted in the gut...
PMC6618313
core_pubmed_pmc
Pharmacokinetics and Safety of CSL112 (Apolipoprotein A‐I [Human]) in Adults With Moderate Renal Impairment and Normal Renal Function
Pharmacokinetics and Safety of CSL112 (Apolipoprotein A‐I [Human]) in Adults With Moderate Renal Impairment and Normal Renal Function Abstract Abstract CSL112 (Apolipoprotein A‐I [human]) is an intravenous preparation of apolipoprotein A‐I (apoA‐I), formulated with phosphatidylcholine (PC) and stabilized with sucrose, ...
PMC9557946
core_pubmed_pmc
Intermittent MEK inhibition for the treatment of metastatic uveal melanoma
Intermittent MEK inhibition for the treatment of metastatic uveal melanoma Abstract Introduction Uveal melanoma (UM) is associated with poor outcomes in the metastatic setting and harbors activating mutations resulting in upregulation of MAPK signaling in almost all cases. The efficacy of selumetinib, an oral allosteri...
PMC10033538
core_pubmed_pmc
Analysis of 2′-hydroxyflavanone (2HF) in mouse whole blood by HPLC–MS/MS for the determination of pharmacokinetic parameters
Analysis of 2′-hydroxyflavanone (2HF) in mouse whole blood by HPLC–MS/MS for the determination of pharmacokinetic parameters Abstract Given the lack of investments, structure, and difficulty of metabolite isolation, promising natural product studies do not progress to preclinical studies, such as pharmacokinetics. 2′-H...
PMC11088545
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Oral BI 1358894 in Healthy Japanese Male Volunteers
Safety, Tolerability, and Pharmacokinetics of Oral BI 1358894 in Healthy Japanese Male Volunteers Abstract Abstract Background and Objectives BI 1358894, a novel small-molecule inhibitor of transient receptor potential canonical ion channels, is under development for treatment of major depressive disorder. Phase I tria...
PMC6421050
core_pubmed_pmc
Acmella oleracea (L) R. K. Jansen Reproductive Toxicity in Zebrafish: An In Vivo and In Silico Assessment
Acmella oleracea (L) R. K. Jansen Reproductive Toxicity in Zebrafish: An In Vivo and In Silico Assessment Abstract The plant species Acmella oleracea L. is used in the north of Brazil for the treatment of a range of illnesses, such as tuberculosis, flu, cough, and rheumatism and as an anti-inflammatory agent; besides, ...
PMC7984335
core_pubmed_pmc
A Randomized, Double‐Blind, Parallel‐Group, Phase 1 Clinical Trial Comparing the Pharmacokinetic, Safety, and Immunogenicity of the Biosimilar HS016 and the Originator Adalimumab in Chinese Healthy Male Subjects
A Randomized, Double‐Blind, Parallel‐Group, Phase 1 Clinical Trial Comparing the Pharmacokinetic, Safety, and Immunogenicity of the Biosimilar HS016 and the Originator Adalimumab in Chinese Healthy Male Subjects Abstract Abstract A comparison of the immunogenicity, safety, and pharmacokinetic properties of HS016 and it...
PMC10626537
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic studies of nicotine in rat brain: a simultaneous investigation of nicotine metabolites and the release of neurotransmitters in vivo
Pharmacokinetic and pharmacodynamic studies of nicotine in rat brain: a simultaneous investigation of nicotine metabolites and the release of neurotransmitters in vivo Abstract Abstract Introduction: The body’s ability to metabolize nicotine and the disposition of nicotine in the brain are important determinants of its...
PMC4204050
core_pubmed_pmc
Traditional Herbal Medicine for the Control of Tropical Diseases
Traditional Herbal Medicine for the Control of Tropical Diseases Abstract Throughout history, traditional herbal medicine has afforded a rich repository of remedies with diverse chemical structures and bioactivities against several health disorders. A common issue of herbal medicine is the limitation of information on ...
PMC4511448
core_pubmed_pmc
Actionable pharmacogenetic markers for prediction and prognosis in breast cancer
Actionable pharmacogenetic markers for prediction and prognosis in breast cancer Abstract Abstract Breast cancer is a heterogeneous disease that necessitates proper patient classification to direct surgery, pharmacotherapy, and radiotherapy. Despite patients within the same subgroup receiving similar pharmacotherapy, s...
PMC3885379
core_pubmed_pmc
Pharmacokinetics, Brain Delivery, and Efficacy in Brain Tumor-Bearing Mice of Glutathione Pegylated Liposomal Doxorubicin (2B3-101)
Pharmacokinetics, Brain Delivery, and Efficacy in Brain Tumor-Bearing Mice of Glutathione Pegylated Liposomal Doxorubicin (2B3-101) Abstract Brain cancer is a devastating disease affecting many people worldwide. Effective treatment with chemotherapeutics is limited due to the presence of the blood-brain barrier (BBB) t...
PMC7067713
core_pubmed_pmc
Prediction of Clearance in Children from Adults Following Drug–Drug Interaction Studies: Application of Age-Dependent Exponent Model
Prediction of Clearance in Children from Adults Following Drug–Drug Interaction Studies: Application of Age-Dependent Exponent Model Abstract Abstract Background and Objective Pharmacokinetic drug–drug interaction (DDI) studies are conducted in adult subjects during drug development but there are limited studies that h...
PMC12964523
core_pubmed_pmc
Reshaping study design for faster extrapolation‐based drug approval in pediatric inflammatory bowel diseases: An ESPGHAN–NASPGHAN position paper
Reshaping study design for faster extrapolation‐based drug approval in pediatric inflammatory bowel diseases: An ESPGHAN–NASPGHAN position paper Abstract Abstract Children with inflammatory bowel diseases (IBD) have limited access to the available advanced therapies, given the lengthy gap between adult and pediatric ap...
PMC8840040
core_pubmed_pmc
Pharmacokinetic Characterization of the DDAH1 Inhibitors ZST316 and ZST152 in Mice Using a HPLC-MS/MS Method
Pharmacokinetic Characterization of the DDAH1 Inhibitors ZST316 and ZST152 in Mice Using a HPLC-MS/MS Method Abstract Abstract The pharmacokinetic profile of ZST316 and ZST152, arginine analogues with inhibitory activity towards human dimethylarginine dimethylaminohydrolase-1 (DDAH1), was investigated in mice using a n...
PMC4049886
core_pubmed_pmc
Once-weekly albiglutide in the management of type 2 diabetes: patient considerations
Once-weekly albiglutide in the management of type 2 diabetes: patient considerations Abstract Abstract This review describes the pharmacologic, pharmacokinetic, and pharmacodynamic properties of albiglutide, as well as its clinical efficacy and safety. Albiglutide is a novel, once-weekly, injectable glucagon-like pepti...
PMC8532682
core_pubmed_pmc
In Vivo Pharmacodynamics of β-Lactams/Nacubactam against Carbapenem-Resistant and/or Carbapenemase-Producing Enterobacter cloacae and Klebsiella pneumoniae in Murine Pneumonia Model
In Vivo Pharmacodynamics of β-Lactams/Nacubactam against Carbapenem-Resistant and/or Carbapenemase-Producing Enterobacter cloacae and Klebsiella pneumoniae in Murine Pneumonia Model Abstract Carbapenem-resistant Enterobacterales (CRE) and carbapenemase-producing Enterobacterales (CPE) have become global threats. CRE− a...
PMC4999603
core_pubmed_pmc
Model‐Based Assessment of Alternative Study Designs in Pediatric Trials. Part II: Bayesian Approaches
Model‐Based Assessment of Alternative Study Designs in Pediatric Trials. Part II: Bayesian Approaches Abstract Abstract This study presents a pharmacokinetic‐pharmacodynamic based clinical trial simulation framework for evaluating the performance of a fixed‐sample Bayesian design (BD) and two alternative Bayesian seque...
PMC3405895
core_pubmed_pmc
Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation Abstract The aim of this research work was to investigate the potential of lecithin nanoparticles (LNs) in improving the oral bioavailability of docetaxel. Docetaxel-loaded LNs (DTX-LNs) were prepared fro...
PMC5689141
core_pubmed_pmc
Pharmacokinetic study of single- and multiple-dosing with metolazone tablets in healthy Chinese population
Pharmacokinetic study of single- and multiple-dosing with metolazone tablets in healthy Chinese population Abstract Abstract Background Metolazone is a diuretic, saluretic and antihypertensive chemical compound from the quinazoline category that possesses medicinal features similar to those of other thiazide diuretic d...
PMC7320194
core_pubmed_pmc
Exploiting metabolic acidosis in solid cancers using a tumor-agnostic pH-activatable nanoprobe for fluorescence-guided surgery
Exploiting metabolic acidosis in solid cancers using a tumor-agnostic pH-activatable nanoprobe for fluorescence-guided surgery Abstract Abstract Cancer cell metabolism leads to a uniquely acidic microenvironment in solid tumors, but exploiting the labile extracellular pH differences between cancer and normal tissues fo...
PMC7889463
core_pubmed_pmc
Covid-19 treatment: Investigation on the phytochemical constituents of Vernonia amygdalina as potential Coronavirus-2 inhibitors
Covid-19 treatment: Investigation on the phytochemical constituents of Vernonia amygdalina as potential Coronavirus-2 inhibitors Abstract The upsurge in the current cases of COVID-19 poses a major threat on human health and population all over the globe. The emergence of new infectious diseases and increase in frequenc...
PMC6243994
core_pubmed_pmc
24-hour levodopa-carbidopa intestinal gel may reduce troublesome dyskinesia in advanced Parkinson’s disease
24-hour levodopa-carbidopa intestinal gel may reduce troublesome dyskinesia in advanced Parkinson’s disease Abstract Levodopa-carbidopa intestinal gel (LCIG) is effective for the control of motor fluctuations in Parkinson’s disease (PD). The objective of this study is to report the reduction of dyskinesias after transi...
PMC9028825
core_pubmed_pmc
Microbiological, Clinical, and PK/PD Features of the New Anti-Gram-Negative Antibiotics: β-Lactam/β-Lactamase Inhibitors in Combination and Cefiderocol—An All-Inclusive Guide for Clinicians
Microbiological, Clinical, and PK/PD Features of the New Anti-Gram-Negative Antibiotics: β-Lactam/β-Lactamase Inhibitors in Combination and Cefiderocol—An All-Inclusive Guide for Clinicians Abstract Abstract Bacterial resistance mechanisms are continuously and rapidly evolving. This is particularly true for Gram-negati...
PMC10065864
core_pubmed_pmc
The inhibitory and inducing effects of ritonavir on hepatic and intestinal CYP3A and other drug-handling proteins
The inhibitory and inducing effects of ritonavir on hepatic and intestinal CYP3A and other drug-handling proteins Abstract Ritonavir, originally developed as HIV protease inhibitor, is widely used as a booster in several HIV pharmacotherapy regimens and more recently in Covid-19 treatment (e.g., Paxlovid). Its boosting...
PMC6792402
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic predictions and clinical outcomes of patients with augmented renal clearance and Pseudomonas aeruginosa bacteremia and/or pneumonia treated with extended infusion cefepime versus extended infusion piperacillin/tazobactam
Pharmacokinetic/pharmacodynamic predictions and clinical outcomes of patients with augmented renal clearance and Pseudomonas aeruginosa bacteremia and/or pneumonia treated with extended infusion cefepime versus extended infusion piperacillin/tazobactam Abstract Abstract Aim: We sought to correlate pharmacokinetic (PK)/...
PMC11049849
core_pubmed_pmc
The Biologic IRL201805 Alters Immune Tolerance Leading to Prolonged Pharmacodynamics and Efficacy in Rheumatoid Arthritis Patients
The Biologic IRL201805 Alters Immune Tolerance Leading to Prolonged Pharmacodynamics and Efficacy in Rheumatoid Arthritis Patients Abstract Abstract A homologue of binding immunoglobulin protein/BiP—IRL201805 alters the function of immune cells in pre-clinical in vivo and in vitro studies. The aim of the study was to s...
PMC10458336
core_pubmed_pmc
Cinnamon modulates the pharmacodynamic & pharmacokinetic of amlodipine in hypertensive rats
Cinnamon modulates the pharmacodynamic & pharmacokinetic of amlodipine in hypertensive rats Abstract The objective of this study was to investigate the effects of cinnamon on the pharmacodynamic (PD) & pharmacokinetic (PK) of amlodipine in hypertensive rats. The hypertensive control group of Wistar rats received L-NAME...
PMC7285759
core_pubmed_pmc
Safety, Pharmacokinetics, and Mosquito‐Lethal Effects of Ivermectin in Combination With Dihydroartemisinin‐Piperaquine and Primaquine in Healthy Adult Thai Subjects
Safety, Pharmacokinetics, and Mosquito‐Lethal Effects of Ivermectin in Combination With Dihydroartemisinin‐Piperaquine and Primaquine in Healthy Adult Thai Subjects Abstract Abstract Mass administration of antimalarial drugs and ivermectin are being considered as potential accelerators of malaria elimination. The safet...
PMC12597537
core_pubmed_pmc
Curcumin enhances the oral bioavailability of testosterone by inhibiting its intestinal metabolism
Curcumin enhances the oral bioavailability of testosterone by inhibiting its intestinal metabolism Abstract Abstract Hypogonadism, characterized by low testosterone blood levels, affects 3%–5% of males worldwide. Oral testosterone undecanoate (TU) is emerging as a key route of administration due to its better ease of a...
PMC10668788
core_pubmed_pmc
Antimicrobial Activities of Aztreonam-Avibactam and Comparator Agents against Enterobacterales Analyzed by ICU and Non-ICU Wards, Infection Sources, and Geographic Regions: ATLAS Program 2016–2020
Antimicrobial Activities of Aztreonam-Avibactam and Comparator Agents against Enterobacterales Analyzed by ICU and Non-ICU Wards, Infection Sources, and Geographic Regions: ATLAS Program 2016–2020 Abstract Abstract Increasing antimicrobial resistance among multidrug-resistant (MDR), extended-spectrum β-lactamase (ESBL)...
PMC10088252
core_pubmed_pmc
Safety, efficacy and pharmacokinetics of BPI-9016M in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic non-small-cell lung cancer: a phase Ib study
Safety, efficacy and pharmacokinetics of BPI-9016M in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic non-small-cell lung cancer: a phase Ib study Abstract Background As a potential target receptor tyrosine kinase, mesenchymal-epithelial transition factor ( MET ) exhib...
PMC11096172
core_pubmed_pmc
CEA-CD3 bispecific antibody cibisatamab with or without atezolizumab in patients with CEA-positive solid tumours: results of two multi-institutional Phase 1 trials
CEA-CD3 bispecific antibody cibisatamab with or without atezolizumab in patients with CEA-positive solid tumours: results of two multi-institutional Phase 1 trials Abstract Abstract Cibisatamab is a bispecific antibody-based construct targeting carcinoembryonic antigen (CEA) on tumour cells and CD3 epsilon chain as a T...
PMC5831157
core_pubmed_pmc
Pharmacokinetics and safety of oral glyburide in dogs with acute spinal cord injury
Pharmacokinetics and safety of oral glyburide in dogs with acute spinal cord injury Abstract Background Glyburide (also known as glibenclamide) is effective in reducing the severity of tissue destruction and improving functional outcome after experimental spinal cord injury in rodents and so has promise as a therapy in...
PMC5756296
core_pubmed_pmc
Perspective on the Genetic Response to Antiparasitics: A Review Article
Perspective on the Genetic Response to Antiparasitics: A Review Article Abstract Background: Drugs’ pharmacokinetics and pharmacodynamics can be affected by diverse genetic variations, within which simple nucleotide polymorphisms (SNPs) are the most common. Genetic variability is one of the factors that could explain q...
PMC9493307
core_pubmed_pmc
A high throughput method for Monitoring of Sorafenib, regorafenib, cabozantinib and their metabolites with UPLC-MS/MS in rat plasma
A high throughput method for Monitoring of Sorafenib, regorafenib, cabozantinib and their metabolites with UPLC-MS/MS in rat plasma Abstract As multi-targeted tyrosine kinase inhibitors, sorafenib, regorafenib and cabozantinib are widely used in hepatocellular carcinoma (HCC) for systemic therapies with anti-proliferat...
PMC7183491
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Posaconazole
Pharmacokinetics and Pharmacodynamics of Posaconazole Abstract Posaconazole is typically used for preventing invasive yeast and mold infections such as invasive aspergillosis in high-risk immunocompromised patients. The oral suspension was the first released formulation and many pharmacokinetic and pharmacodynamic stud...
PMC3513229
core_pubmed_pmc
Individualized immunosuppression in transplant patients: potential role of pharmacogenetics
Individualized immunosuppression in transplant patients: potential role of pharmacogenetics Abstract The immunosuppressive drugs used to prevent the rejection of transplanted organs have a narrow therapeutic index. Under treatment results in episodes of rejection leading to either damage or loss of the organ. Over immu...
PMC10691926
core_pubmed_pmc
The role of antidrug antibodies in ustekinumab therapy and the impact of methotrexate
The role of antidrug antibodies in ustekinumab therapy and the impact of methotrexate Abstract Abstract Objective We investigated the impact of concomitant MTX on ustekinumab (UST) levels and antidrug antibody (ADA) formation in PsA and evaluated consequences in pharmacodynamics and pharmacokinetics. Methods We conduct...
PMC12667466
core_pubmed_pmc
An Effective Oral Drug Delivery Route for Pharmacokinetic Complications: Spirulina Lipid Nanotechnology System
An Effective Oral Drug Delivery Route for Pharmacokinetic Complications: Spirulina Lipid Nanotechnology System Abstract Abstract Irritable bowel syndrome (IBS) is a prevalent gastrointestinal disorder characterized by mental manifestations, abdominal pain, and alterations in defecation habits. The incidence rate in som...
PMC9303766
core_pubmed_pmc
A Population Pharmacokinetic Model of Vonoprazan: Evaluating the Effects of Race, Disease Status, and Other Covariates on Exposure
A Population Pharmacokinetic Model of Vonoprazan: Evaluating the Effects of Race, Disease Status, and Other Covariates on Exposure Abstract Abstract Vonoprazan, a potassium‐competitive acid blocker, is under investigation in the United States and Europe for the treatment of erosive esophagitis and Helicobacter pylori i...
PMC6307495
core_pubmed_pmc
Fenofibrate modified-release pellets with lag phase and high oral bioavailability
Fenofibrate modified-release pellets with lag phase and high oral bioavailability Abstract Purpose Fenofibrate and statin combination therapy is highly recommended by the current clinical guidelines for treatment of mixed dyslipidemia. In this study, an innovative delayed-release preparation of fenofibrate was designed...
PMC8471814
core_pubmed_pmc
Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats
Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats Abstract Abstract Candesartan cilexetil (CC) is an antihypertensive drug. It has low solubility and faces hepatic first-pass metabolism after oral ingestion. We formulated bioadhesive buccal films and studied the respec...
PMC12806658
core_pubmed_pmc
Acid-suppressive effect of tegoprazan 12.5 mg BID: a phase 1 comparative study with tegoprazan 25 mg QD and famotidine 20 mg BID
Acid-suppressive effect of tegoprazan 12.5 mg BID: a phase 1 comparative study with tegoprazan 25 mg QD and famotidine 20 mg BID Abstract Abstract Tegoprazan is a potassium-competitive acid blocker that directly inhibits the gastric proton pump, whereas famotidine is a histamine-2 receptor antagonist that indirectly su...
PMC10855649
core_pubmed_pmc
GT-00AxIL15, a Novel Tumor-Targeted IL-15-Based Immunocytokine for the Treatment of TA-MUC1-Positive Solid Tumors: Preclinical In Vitro and In Vivo Pharmacodynamics and Biodistribution Studies
GT-00AxIL15, a Novel Tumor-Targeted IL-15-Based Immunocytokine for the Treatment of TA-MUC1-Positive Solid Tumors: Preclinical In Vitro and In Vivo Pharmacodynamics and Biodistribution Studies Abstract GT-00AxIL15 is a novel interleukin-15-based immunocytokine targeting a tumor-specific, glycosylated epitope of MUC1 (T...
PMC11743450
core_pubmed_pmc
Bergenin, a bioactive flavonoid: advancements in the prospects of anticancer mechanism, pharmacokinetics and nanoformulations
Bergenin, a bioactive flavonoid: advancements in the prospects of anticancer mechanism, pharmacokinetics and nanoformulations Abstract Abstract The natural world is a vast reservoir of exceptionally varied and inventive chemical compositions. Natural products are used as initial compounds to create combinatorial librar...
PMC11199305
core_pubmed_pmc
The Use of Microdosing for In vivo Phenotyping of Cytochrome P450 Enzymes: Where Do We Stand? A Narrative Review
The Use of Microdosing for In vivo Phenotyping of Cytochrome P450 Enzymes: Where Do We Stand? A Narrative Review Abstract Abstract Cytochrome P450 (CYP) enzymes play a central role in the elimination of approximately 80% of all clinically used drugs. Differences in CYP enzyme activity between individuals can contribute...
PMC5174014
core_pubmed_pmc
Effect of various anticoagulants on the bioanalysis of drugs in rat blood: implication for pharmacokinetic studies of anticancer drugs
Effect of various anticoagulants on the bioanalysis of drugs in rat blood: implication for pharmacokinetic studies of anticancer drugs Abstract Abstract Background Pharmacokinetic studies are vital in development and optimization of drugs. While blood samples can be collected either in EDTA, heparin or citrate containi...
PMC6286374
core_pubmed_pmc
Using a three-compartment model improves the estimation of iohexol clearance to assess glomerular filtration rate
Using a three-compartment model improves the estimation of iohexol clearance to assess glomerular filtration rate Abstract Abstract Plasma clearance of iohexol is a key tool to precisely determine glomerular filtration rate (GFR) in clinical research and clinical practice. Despite evidence that iohexol pharmacokinetics...
PMC12546633
core_pubmed_pmc
Erdafitinib suppresses pathological retinal angiogenesis via dual targeting of FGFR and VEGFR2 signaling
Erdafitinib suppresses pathological retinal angiogenesis via dual targeting of FGFR and VEGFR2 signaling Abstract Pathological retinal angiogenesis drives vision loss in diseases like proliferative diabetic retinopathy (PDR) and retinal vein occlusion (RVO). Erdafitinib, a pan-fibroblast growth factor receptor (FGFR) i...
PMC11993295
core_pubmed_pmc
Pharmacokinetic Modeling and Model‐Based Hypothesis Generation for Dose Optimization of Clonidine in Neonates With Neonatal Opioid Withdrawal Syndrome
Pharmacokinetic Modeling and Model‐Based Hypothesis Generation for Dose Optimization of Clonidine in Neonates With Neonatal Opioid Withdrawal Syndrome Abstract Abstract The No‐POPPY study ( NCT03396588 ), a double‐blind, randomized trial compared morphine with clonidine therapy for neonatal opioid withdrawal syndrome (...
PMC11904481
core_pubmed_pmc
A phase I, first-in-human trial of KO-947, an ERK1/2 inhibitor, in patients with advanced solid tumors
A phase I, first-in-human trial of KO-947, an ERK1/2 inhibitor, in patients with advanced solid tumors Abstract Background KO-947, a potent, intravenously administered, extracellular signal-regulated kinase (ERK) inhibitor, has demonstrated activity in preclinical models. This phase I trial of KO-947 evaluated maximum ...
PMC10649009
core_pubmed_pmc
The role of rifampicin within the treatment of Mycobacterium avium pulmonary disease
The role of rifampicin within the treatment of Mycobacterium avium pulmonary disease Abstract ABSTRACT Rifampicin is recommended for the treatment of Mycobacterium avium complex pulmonary disease alongside azithromycin and ethambutol. We evaluated the azithromycin-ethambutol backbone with and without rifampicin in an i...
PMC12064623
core_pubmed_pmc
Impact of Hypothermic Temperature Control on Plasma and Soft Tissue Pharmacokinetics of Penicillin/Beta-Lactamase Inhibitor Combinations in Patients Resuscitated After Cardiac Arrest
Impact of Hypothermic Temperature Control on Plasma and Soft Tissue Pharmacokinetics of Penicillin/Beta-Lactamase Inhibitor Combinations in Patients Resuscitated After Cardiac Arrest Abstract Background and Objectives Penicillin/beta-lactamase inhibitors are often used to treat aspiration pneumonia in patients resuscit...
PMC11935520
core_pubmed_pmc
Direct oral anticoagulants versus warfarin in adult heart transplant recipients
Direct oral anticoagulants versus warfarin in adult heart transplant recipients Abstract Abstract Background Direct oral anticoagulants (DOACs) have transformed the field of anticoagulation, offering more predictable pharmacokinetic and pharmacodynamic characteristics when compared to traditional warfarin therapy. DOAC...
PMC12162790
core_pubmed_pmc
Cross-species translational modelling of targeted therapeutic oligonucleotides using physiologically based pharmacokinetics
Cross-species translational modelling of targeted therapeutic oligonucleotides using physiologically based pharmacokinetics Abstract Oligonucleotide therapeutics hold promise for targeted gene silencing, yet achieving optimal tissue-specific delivery remains challenging. This study introduces a mechanistic whole-body p...
PMC5371884
core_pubmed_pmc
Comparison of the Pharmacokinetic Properties of Hemoglobin-Based Oxygen Carriers
Comparison of the Pharmacokinetic Properties of Hemoglobin-Based Oxygen Carriers Abstract Abstract Hemoglobin (Hb) is an ideal material for use in the development of an oxygen carrier in view of its innate biological properties. However, the vascular retention of free Hb is too short to permit a full therapeutic effect...
PMC11206988
core_pubmed_pmc
Study on the Effect of Pharmaceutical Excipient PEG400 on the Pharmacokinetics of Baicalin in Cells Based on MRP2, MRP3, and BCRP Efflux Transporters
Study on the Effect of Pharmaceutical Excipient PEG400 on the Pharmacokinetics of Baicalin in Cells Based on MRP2, MRP3, and BCRP Efflux Transporters Abstract Abstract Pharmaceutical excipient PEG400 is a common component of traditional Chinese medicine compound preparations. Studies have demonstrated that pharmaceutic...
PMC6055887
core_pubmed_pmc
Development of novel rosuvastatin nanostructured lipid carriers for oral delivery in an animal model
Development of novel rosuvastatin nanostructured lipid carriers for oral delivery in an animal model Abstract Objective The aim of this study was to prepare rosuvastatin nanostructured lipid carriers (RST-NLCs) in order to increase the bioavailability of RST. Materials and methods RST-NLCs were prepared by hot melt hig...
PMC11897362
core_pubmed_pmc
Transient destabilization of whole brain dynamics induced by N,N-Dimethyltryptamine (DMT)
Transient destabilization of whole brain dynamics induced by N,N-Dimethyltryptamine (DMT) Abstract Abstract The transition towards the brain state induced by psychedelic drugs is frequently neglected in favor of a static description of their acute effects. We use a time-dependent whole-brain model to reproduce large-sc...
PMC5848842
core_pubmed_pmc
Preclinical pharmacokinetics, interspecies scaling, and pharmacokinetics of a Phase I clinical trial of TTAC-0001, a fully human monoclonal antibody against vascular endothelial growth factor 2
Preclinical pharmacokinetics, interspecies scaling, and pharmacokinetics of a Phase I clinical trial of TTAC-0001, a fully human monoclonal antibody against vascular endothelial growth factor 2 Abstract Abstract Background VEGF is a highly selective mitogen that serves as the central regulator of tumor angiogenesis by ...
PMC12039930
core_pubmed_pmc
Combined Mulberry Leaf Polysaccharide-Caged Liposomes for Effective Oral Drug Delivery in Rat Model
Combined Mulberry Leaf Polysaccharide-Caged Liposomes for Effective Oral Drug Delivery in Rat Model Abstract Introduction Mulberry leaf polysaccharide (MLP) has gained attention as a potential anti-diabetic agent for lowering blood glucose and improving insulin sensitivity. However, the low gastrointestinal stability a...
PMC6452316
core_pubmed_pmc
Optimal Treatments for Severe Malaria and the Threat Posed by Artemisinin Resistance
Optimal Treatments for Severe Malaria and the Threat Posed by Artemisinin Resistance Abstract Abstract Background Standard treatment for severe malaria is with artesunate; patient survival in the 24 hours immediately posttreatment is the key objective. Clinical trials use clearance rates of circulating parasites as the...
PMC8835015
core_pubmed_pmc
Powering Research through Innovative Methods for Mixtures in Epidemiology (PRIME) Program: Novel and Expanded Statistical Methods
Powering Research through Innovative Methods for Mixtures in Epidemiology (PRIME) Program: Novel and Expanded Statistical Methods Abstract Abstract Humans are exposed to a diverse mixture of chemical and non-chemical exposures across their lifetimes. Well-designed epidemiology studies as well as sophisticated exposure ...
PMC6359039
core_pubmed_pmc
Pharmacokinetics, Tissue Distribution, Plasma Protein Binding Studies of 10-Dehydroxyl-12-Demethoxy-Conophylline, a Novel Anti-Tumor Candidate, in Rats
Pharmacokinetics, Tissue Distribution, Plasma Protein Binding Studies of 10-Dehydroxyl-12-Demethoxy-Conophylline, a Novel Anti-Tumor Candidate, in Rats Abstract 10-Dehydroxyl-12-demethoxy-conophylline is a natural anticancer candidate. The motivation of this study was to explore the pharmacokinetic profiles, tissue dis...
PMC11848832
core_pubmed_pmc
Phase Ib Study of Immunocytokine Simlukafusp Alfa (FAP-IL2v) Combined with Pembrolizumab for Treatment of Advanced and/or Metastatic Melanoma
Phase Ib Study of Immunocytokine Simlukafusp Alfa (FAP-IL2v) Combined with Pembrolizumab for Treatment of Advanced and/or Metastatic Melanoma Abstract Abstract Purpose: This study explored the combination of fibroblast activation protein (FAP) IL2 variant (FAP-IL2v), a novel immune-cytokine, with pembrolizumab in patie...
PMC11782592
core_pubmed_pmc
Adaptation of an in vitro one-compartment pharmacodynamic chemostat for testing efficacy of ceftazidime against Burkholderia pseudomallei outside a BSL3 facility
Adaptation of an in vitro one-compartment pharmacodynamic chemostat for testing efficacy of ceftazidime against Burkholderia pseudomallei outside a BSL3 facility Abstract Non-clinical pharmacokinetic-pharmacodynamic (PKPD) models are crucial in the initial design of drug-dosage regimens and in drug development but has ...
PMC5022189
core_pubmed_pmc
A Phase II pilot trial to evaluate safety and efficacy of ferroquine against early Plasmodium falciparum in an induced blood-stage malaria infection study
A Phase II pilot trial to evaluate safety and efficacy of ferroquine against early Plasmodium falciparum in an induced blood-stage malaria infection study Abstract Abstract Background Ferroquine ( SSR97193 ) is a candidate anti-malarial currently undergoing clinical trials for malaria. To better understand its pharmaco...
PMC12764708
core_pubmed_pmc
Evaluation of [ 89 Zr]Zr-girentuximab PET imaging of clear cell renal cell carcinoma in Chinese patients: a Phase 1 clinical study (ZIRDOSE-CP)
Evaluation of [ 89 Zr]Zr-girentuximab PET imaging of clear cell renal cell carcinoma in Chinese patients: a Phase 1 clinical study (ZIRDOSE-CP) Abstract Abstract Background Results from a multinational Phase 3 study demonstrated high accuracy and a favorable safety and tolerability profile of [ 89 Zr]Zr-girentuximab PE...
PMC8525888
core_pubmed_pmc
Targeted mass-spectrometry-based assays enable multiplex quantification of receptor tyrosine kinase, MAP kinase, and AKT signaling
Targeted mass-spectrometry-based assays enable multiplex quantification of receptor tyrosine kinase, MAP kinase, and AKT signaling Abstract Summary A primary goal of the US National Cancer Institute's Ras initiative at the Frederick National Laboratory for Cancer Research is to develop methods to quantify RAS signaling...
PMC4818938
core_pubmed_pmc
Naïve-pooled pharmacokinetic analysis of pyrazinamide, isoniazid and rifampicin in plasma and cerebrospinal fluid of Vietnamese children with tuberculous meningitis
Naïve-pooled pharmacokinetic analysis of pyrazinamide, isoniazid and rifampicin in plasma and cerebrospinal fluid of Vietnamese children with tuberculous meningitis Abstract Background Among the various forms of TB, tuberculous meningitis (TBM) is the most severe, with about 30 % mortality and 50 % of survivors left wi...
PMC10757118
core_pubmed_pmc
HS ‐10352 in hormone receptor‐positive, HER2 ‐negative advanced breast cancer: A phase 1 dose‐escalation trial
HS ‐10352 in hormone receptor‐positive, HER2 ‐negative advanced breast cancer: A phase 1 dose‐escalation trial Abstract Abstract Background Approximately 40% of patients with hormone receptor (HR)‐positive and human epidermal growth factor receptor 2 (HER2)‐negative advanced breast cancer (ABC) exhibit PIK3CA mutations...
PMC11049954
core_pubmed_pmc
Association of CYP3A4-392A/G, CYP3A5-6986A/G, and ABCB1-3435C/T Polymorphisms with Tacrolimus Dose, Serum Concentration, and Biochemical Parameters in Mexican Patients with Kidney Transplant
Association of CYP3A4-392A/G, CYP3A5-6986A/G, and ABCB1-3435C/T Polymorphisms with Tacrolimus Dose, Serum Concentration, and Biochemical Parameters in Mexican Patients with Kidney Transplant Abstract Tacrolimus (TAC) is an immunosuppressant drug that prevents organ rejection after transplantation. This drug is transpor...
PMC7547831
core_pubmed_pmc
Identifying potential anti-COVID-19 pharmacological components of traditional Chinese medicine Lianhuaqingwen capsule based on human exposure and ACE2 biochromatography screening
Identifying potential anti-COVID-19 pharmacological components of traditional Chinese medicine Lianhuaqingwen capsule based on human exposure and ACE2 biochromatography screening Abstract Lianhuaqingwen (LHQW) capsule, a herb medicine product, has been clinically proved to be effective in coronavirus disease 2019 (COVI...
PMC7342499
core_pubmed_pmc
Effects of Dexmedetomidine on the Pharmacokinetics of Dezocine, Midazolam and Its Metabolite 1-Hydroxymidazolam in Beagles by UPLC-MS/MS
Effects of Dexmedetomidine on the Pharmacokinetics of Dezocine, Midazolam and Its Metabolite 1-Hydroxymidazolam in Beagles by UPLC-MS/MS Abstract Abstract Objective We developed and validated a sensitive and reliable UPLC-MS/MS method for simultaneous determination of dezocine (DEZ), midazolam (MDZ) and its metabolite ...
PMC11765396
core_pubmed_pmc
The Rise of Fentanyl: Molecular Aspects and Forensic Investigations
The Rise of Fentanyl: Molecular Aspects and Forensic Investigations Abstract Fentanyl is a synthetic opioid widely used for its potent analgesic effects in chronic pain management and intraoperative anesthesia. However, its high potency, low cost, and accessibility have also made it a significant drug of abuse, contrib...
PMC10057977
core_pubmed_pmc
Use of In Vivo Imaging and Physiologically-Based Kinetic Modelling to Predict Hepatic Transporter Mediated Drug–Drug Interactions in Rats
Use of In Vivo Imaging and Physiologically-Based Kinetic Modelling to Predict Hepatic Transporter Mediated Drug–Drug Interactions in Rats Abstract Gadoxetate, a magnetic resonance imaging (MRI) contrast agent, is a substrate of organic-anion-transporting polypeptide 1B1 and multidrug resistance-associated protein 2. Si...
PMC8759082
core_pubmed_pmc
Use of Physiologically Based Pharmacokinetic Modeling to Predict Human Gut Microbial Conversion of Daidzein to S-Equol
Use of Physiologically Based Pharmacokinetic Modeling to Predict Human Gut Microbial Conversion of Daidzein to S-Equol Abstract A physiologically based pharmacokinetic (PBPK) model was developed for daidzein and its metabolite S-equol. Anaerobic in vitro incubations of pooled fecal samples from S-equol producers and no...
PMC8665220
core_pubmed_pmc
On the usefulness of four in vitro methods in assessing the intraluminal performance of poorly soluble, ionisable compounds in the fasted state
On the usefulness of four in vitro methods in assessing the intraluminal performance of poorly soluble, ionisable compounds in the fasted state Abstract Abstract A small-scale two-stage biphasic system, a small-scale two-stage dissolution-permeation system, the Erweka mini-paddle apparatus, and the BioGIT system were e...
PMC9965990
core_pubmed_pmc
A Physiologically Based Pharmacokinetic Model of Ketoconazole and Its Metabolites as Drug–Drug Interaction Perpetrators
A Physiologically Based Pharmacokinetic Model of Ketoconazole and Its Metabolites as Drug–Drug Interaction Perpetrators Abstract The antifungal ketoconazole, which is mainly used for dermal infections and treatment of Cushing’s syndrome, is prone to drug–food interactions (DFIs) and is well known for its strong drug–dr...
PMC12622487
core_pubmed_pmc
Optimized Monothiol Thioredoxin Derivative (ORP100S) Protects In Vitro and In Vivo from Radiation and Chemotoxicity Without Promoting Tumor Proliferation
Optimized Monothiol Thioredoxin Derivative (ORP100S) Protects In Vitro and In Vivo from Radiation and Chemotoxicity Without Promoting Tumor Proliferation Abstract Abstract Human thioredoxin‐1 (TRX) is a target‐selective disulfide reductase with antioxidant, anti‐inflammatory, and regulatory functions that mitigates cel...
PMC8071704
core_pubmed_pmc
Population Pharmacokinetics and Safety of Oral Tetra-Arsenic Tetra-Sulfide Formula in Pediatric Acute Promyelocytic Leukemia
Population Pharmacokinetics and Safety of Oral Tetra-Arsenic Tetra-Sulfide Formula in Pediatric Acute Promyelocytic Leukemia Abstract Background An oral tetra-arsenic tetra-sulfide (AS 4 S 4 ) formula has been recommended as an outpatient post-remission treatment for Chinese adults with acute promyelocytic leukemia (AP...
PMC9007602
core_pubmed_pmc
A workflow for the joint modeling of longitudinal and event data in the development of therapeutics: Tools, statistical methods, and diagnostics
A workflow for the joint modeling of longitudinal and event data in the development of therapeutics: Tools, statistical methods, and diagnostics Abstract Abstract Clinical trials investigate treatment endpoints that usually include measurements of pharmacodynamic and efficacy biomarkers in early‐phase studies and patie...
PMC9896003
core_pubmed_pmc
Discovery of a novel, liver-targeted thyroid hormone receptor-β agonist, CS271011 , in the treatment of lipid metabolism disorders
Discovery of a novel, liver-targeted thyroid hormone receptor-β agonist, CS271011 , in the treatment of lipid metabolism disorders Abstract Abstract Introduction Thyroid hormone receptor β (THR-β) plays a critical role in metabolism regulation and has become an attractive target for treating lipid metabolism disorders ...
PMC10962491
core_pubmed_pmc
Population pharmacokinetics of the GIP/GLP receptor agonist tirzepatide
Population pharmacokinetics of the GIP/GLP receptor agonist tirzepatide Abstract Abstract Tirzepatide is a first‐in‐class glucose‐dependent insulinotropic polypeptide and glucagon‐like peptide‐1 receptor agonist approved as for the treatment of type 2 diabetes mellitus. A population‐based pharmacokinetic (PK) model was...
PMC9292342
core_pubmed_pmc
Tolerance and Pharmacokinetics of Galliprant™ Administered Orally to Collies Homozygous for MDR1‐1Δ
Tolerance and Pharmacokinetics of Galliprant™ Administered Orally to Collies Homozygous for MDR1‐1Δ Abstract Abstract The objectives of the study were to evaluate the pharmacokinetics and tolerance of grapiprant, a substrate of the human P‐gp transporter, in collies homozygous for MDR1‐1Δ when administered at the label...
PMC12912046
core_pubmed_pmc
Bixin Beyond Colour: Expanding Therapeutic Horizons Through the Integration of Pharmacological Potential with Modern Drug Design and Delivery Strategies
Bixin Beyond Colour: Expanding Therapeutic Horizons Through the Integration of Pharmacological Potential with Modern Drug Design and Delivery Strategies Abstract Abstract Bixin, a vibrant apocarotenoid derived from the seeds of Bixa orellana Linn. (commonly known as annatto), has been traditionally used as a natural co...
PMC7345016
core_pubmed_pmc
Principles of N -Linked Glycosylation Variations of IgG-Based Therapeutics: Pharmacokinetic and Functional Considerations
Principles of N -Linked Glycosylation Variations of IgG-Based Therapeutics: Pharmacokinetic and Functional Considerations Abstract The development of recombinant therapeutic proteins has been a major revolution in modern medicine. Therapeutic-based monoclonal antibodies (mAbs) are growing rapidly, providing a potential...
PMC7596670
core_pubmed_pmc
Impact of CYP2C19 , CYP3A4 , ABCB1 , and FMO3 genotypes on plasma voriconazole in Thai patients with invasive fungal infections
Impact of CYP2C19 , CYP3A4 , ABCB1 , and FMO3 genotypes on plasma voriconazole in Thai patients with invasive fungal infections Abstract Abstract Voriconazole is the first‐line antifungal choice in the treatment of invasive fungal infections (IFIs). Single nucleotide polymorphisms (SNPs) in drug‐metabolizing and transp...