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PMC4196191
core_pubmed_pmc
In comparative analysis of multi-kinase inhibitors for targeted medulloblastoma therapy pazopanib exhibits promising in vitro and in vivo efficacy
In comparative analysis of multi-kinase inhibitors for targeted medulloblastoma therapy pazopanib exhibits promising in vitro and in vivo efficacy Abstract Abstract Regardless of the recent advances in cytotoxic therapies, 30% of children diagnosed with medulloblastoma. succumb to the disease. Therefore, novel therapeu...
PMC11582259
core_pubmed_pmc
Numerical simulation method for the assessment of the effect of molar activity on the pharmacokinetics of radioligands in small animals
Numerical simulation method for the assessment of the effect of molar activity on the pharmacokinetics of radioligands in small animals Abstract Background It is well recognized that the molar activity of a radioligand is an important pharmacokinetic parameter, especially in positron emission tomography (PET) of small ...
PMC9024029
core_pubmed_pmc
Rapid and sustained B-cell depletion with subcutaneous ofatumumab in relapsing multiple sclerosis: APLIOS, a randomized phase-2 study
Rapid and sustained B-cell depletion with subcutaneous ofatumumab in relapsing multiple sclerosis: APLIOS, a randomized phase-2 study Abstract Abstract Background: Ofatumumab, the first fully human anti-CD20 monoclonal antibody, is approved in several countries for relapsing multiple sclerosis (RMS). Objective: To demo...
PMC9007600
core_pubmed_pmc
Mechanistic modeling of a human IgG 4 monoclonal antibody (tralokinumab) Fab‐arm exchange with endogenous IgG 4 in healthy volunteers
Mechanistic modeling of a human IgG 4 monoclonal antibody (tralokinumab) Fab‐arm exchange with endogenous IgG 4 in healthy volunteers Abstract Abstract Therapeutic IgG 4 antibodies engage in Fab‐arm exchange with endogenous human immunoglobulin G4 (IgG 4 ) to form monovalent hybrid molecules. A mechanistic population m...
PMC7883113
core_pubmed_pmc
Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease
Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease Abstract Abstract Effective, safe, and pharmacokinetically suitable drugs are urgently needed to curb the ongoing COVID-19 pandemic. The main protease or 3C-like protease (M pro or 3CL pro ) of SARS-CoV-2 is conside...
PMC6173718
core_pubmed_pmc
A new pharmacokinetic model for 90 Y-ibritumomab tiuxetan based on 3-dimensional dosimetry
A new pharmacokinetic model for 90 Y-ibritumomab tiuxetan based on 3-dimensional dosimetry Abstract Abstract Monoclonal antibodies (mAbs) are key components in several therapies for cancer and inflammatory diseases but current knowledge of their clinical pharmacokinetics and distribution in human tissues remains incomp...
PMC2842889
core_pubmed_pmc
Aerosol Infection Model of Tuberculosis in Wistar Rats
Aerosol Infection Model of Tuberculosis in Wistar Rats Abstract We explored suitability of a rat tuberculosis aerosol infection model for investigating the pharmacodynamics of new antimycobacterial agents. Infection of rats via the aerosol route led to a reproducible course of M. tuberculosis infection in the lungs. Th...
PMC7385433
core_pubmed_pmc
Revisiting aminocoumarins for the treatment of melioidosis
Revisiting aminocoumarins for the treatment of melioidosis Abstract Highlights • Aminocoumarins can be used to treat acute pulmonary melioidosis in a murine model. • Formulation with l -tyrosine or dl -tryptophan enhances the bioactivity of aminocoumarins. • Utility of Galleria mellonella larvae for in vivo drug effica...
PMC4128791
core_pubmed_pmc
Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes Abstract Abstract Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-l...
PMC4381587
core_pubmed_pmc
A novel PI3K inhibitor PIK-C98 displays potent preclinical activity against multiple myeloma
A novel PI3K inhibitor PIK-C98 displays potent preclinical activity against multiple myeloma Abstract Abstract Recent clinical trials have demonstrated targeting PI3K pathway is a promising strategy for the treatment of blood cancers. To identify novel PI3K inhibitors, we performed a high throughput virtual screen and ...
PMC9214263
core_pubmed_pmc
Early Feasibility Assessment: A Method for Accurately Predicting Biotherapeutic Dosing to Inform Early Drug Discovery Decisions
Early Feasibility Assessment: A Method for Accurately Predicting Biotherapeutic Dosing to Inform Early Drug Discovery Decisions Abstract Abstract The application of model-informed drug discovery and development (MID3) approaches in the early stages of drug discovery can help determine feasibility of drugging a target, ...
PMC9923710
core_pubmed_pmc
Proposal for individualized dosing of eculizumab in atypical haemolytic uraemic syndrome: patient friendly and cost-effective
Proposal for individualized dosing of eculizumab in atypical haemolytic uraemic syndrome: patient friendly and cost-effective Abstract ABSTRACT Background Eculizumab is a lifesaving yet expensive drug for atypical haemolytic uraemic syndrome (aHUS). Current guidelines advise a fixed-dosing schedule, which can be subopt...
PMC10658528
core_pubmed_pmc
Individualized chemotherapy drug dose escalation in dogs with multicentric lymphoma
Individualized chemotherapy drug dose escalation in dogs with multicentric lymphoma Abstract Abstract Background This study was performed to determine the ability to escalate drug doses in a 15‐week CHOP protocol in dogs with multicentric lymphoma. Hypothesis We hypothesized that at least 50% of dogs could successfully...
PMC8453935
core_pubmed_pmc
Effects of Lemborexant on the Pharmacokinetics of Oral Contraceptives: Results From a Phase 1 Drug‐Drug Interaction Study in Healthy Females
Effects of Lemborexant on the Pharmacokinetics of Oral Contraceptives: Results From a Phase 1 Drug‐Drug Interaction Study in Healthy Females Abstract Abstract Lemborexant is a dual orexin receptor antagonist approved in multiple countries including the United States, Canada, and Japan for the treatment of insomnia in a...
PMC5658282
core_pubmed_pmc
Simultaneous Modeling of Biomarker and Toxicity Response Predicted Optimal Regimen of Guadecitabine (SGI‐110) in Myeloid Malignancies
Simultaneous Modeling of Biomarker and Toxicity Response Predicted Optimal Regimen of Guadecitabine (SGI‐110) in Myeloid Malignancies Abstract Guadecitabine (SGI‐110) is a novel next‐generation hypomethylating agent (HMA) administered as s.c. injection with extended decitabine exposure. Dose/exposure‐response analyses ...
PMC11086411
core_pubmed_pmc
Interpreting hydroxychloroquine blood levels for medication non-adherence: a pharmacokinetic study
Interpreting hydroxychloroquine blood levels for medication non-adherence: a pharmacokinetic study Abstract Abstract Objective Characterise the relationship between hydroxychloroquine (HCQ) blood levels and the number of missed doses, accounting for dosage, dose timing and the large variability in pharmacokinetics (PK)...
PMC2959072
core_pubmed_pmc
Declining in efficacy of a three-day combination regimen of mefloquine-artesunate in a multi-drug resistance area along the Thai-Myanmar border
Declining in efficacy of a three-day combination regimen of mefloquine-artesunate in a multi-drug resistance area along the Thai-Myanmar border Abstract Background Declining in clinical efficacy of artesunate-mefloquine combination has been documented in areas along the eastern border (Thai-Cambodian) of Thailand. In t...
PMC8503662
core_pubmed_pmc
Fixed dose combination of capecitabine and cyclophosphamide in metastatic breast cancer: Results from THE ENCLOSE phase 2/3 randomized multicenter study
Fixed dose combination of capecitabine and cyclophosphamide in metastatic breast cancer: Results from THE ENCLOSE phase 2/3 randomized multicenter study Abstract Abstract Aim To evaluate pharmacokinetics, efficacy and safety of fixed-dose combination (FDC) of oral capecitabine + cyclophosphamide in metastatic breast ca...
PMC8173197
core_pubmed_pmc
A Large Impact of Obesity on the Disposition of Ivermectin, Moxidectin and Eprinomectin in a Canine Model: Relevance for COVID-19 Patients
A Large Impact of Obesity on the Disposition of Ivermectin, Moxidectin and Eprinomectin in a Canine Model: Relevance for COVID-19 Patients Abstract Ivermectin (IVM) and moxidectin (MOX) are used extensively as parasiticides in veterinary medicine. Based on in vitro data, IVM has recently been proposed for the preventio...
PMC3913854
core_pubmed_pmc
Phase 1 dose-escalation, pharmacokinetic, and cerebrospinal fluid distribution study of TAK-285, an investigational inhibitor of EGFR and HER2
Phase 1 dose-escalation, pharmacokinetic, and cerebrospinal fluid distribution study of TAK-285, an investigational inhibitor of EGFR and HER2 Abstract Summary Introduction This phase 1 study assessed safety, maximum tolerated dose (MTD), pharmacokinetics, cerebrospinal fluid (CSF) distribution, and preliminary clinica...
PMC8161189
core_pubmed_pmc
Comparing Predictions of a PBPK Model for Cyclosporine With Drug Levels From Therapeutic Drug Monitoring
Comparing Predictions of a PBPK Model for Cyclosporine With Drug Levels From Therapeutic Drug Monitoring Abstract Abstract This study compared simulations of a physiologically based pharmacokinetic (PBPK) model implemented for cyclosporine with drug levels from therapeutic drug monitoring to evaluate the predictive per...
PMC10787206
core_pubmed_pmc
Cluster Gauss‐Newton method for a quick approximation of profile likelihood: With application to physiologically‐based pharmacokinetic models
Cluster Gauss‐Newton method for a quick approximation of profile likelihood: With application to physiologically‐based pharmacokinetic models Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) models can be challenging to work with because they can have too many parameters to identify from observable data. ...
PMC6997100
core_pubmed_pmc
Pharmacokinetics of doxorubicin following concomitant intravenous administration of olaratumab (IMC‐3G3) to patients with advanced soft tissue sarcoma
Pharmacokinetics of doxorubicin following concomitant intravenous administration of olaratumab (IMC‐3G3) to patients with advanced soft tissue sarcoma Abstract Abstract Background Olaratumab, a fully human monoclonal antibody, selectively binds to human platelet‐derived growth factor receptor alpha and blocks ligand bi...
PMC3936431
core_pubmed_pmc
Formulation and Evaluation of Irinotecan Suppository for Rectal Administration
Formulation and Evaluation of Irinotecan Suppository for Rectal Administration Abstract Abstract Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The ...
PMC11861990
core_pubmed_pmc
Pharmacokinetics of Tylvalosin Following Intravenous or Oral Administration at Different Doses in Broiler Chickens
Pharmacokinetics of Tylvalosin Following Intravenous or Oral Administration at Different Doses in Broiler Chickens Abstract Simple Summary This study aimed to investigate the pharmacokinetics of tylvalosin following oral and intravenous administration at three different doses in broiler chickens. Forty-eight healthy ch...
PMC11720520
core_pubmed_pmc
A phase Ia study of a novel anti-HER2 antibody–drug conjugate GQ1001 in patients with previously treated HER2 positive advanced solid tumors
A phase Ia study of a novel anti-HER2 antibody–drug conjugate GQ1001 in patients with previously treated HER2 positive advanced solid tumors Abstract Abstract Background A novel anti-human epidermal growth factor receptor 2 (HER2) antibody–drug conjugate (ADC) GQ1001 was assessed in patients with previously treated HER...
PMC5367379
core_pubmed_pmc
Systems pharmacology modeling of drug‐induced hyperbilirubinemia: Differentiating hepatotoxicity and inhibition of enzymes/transporters
Systems pharmacology modeling of drug‐induced hyperbilirubinemia: Differentiating hepatotoxicity and inhibition of enzymes/transporters Abstract Elevations in serum bilirubin during drug treatment may indicate global liver dysfunction and a high risk of liver failure. However, drugs also can increase serum bilirubin in...
PMC11217582
core_pubmed_pmc
Structural Characters and Pharmacological Activity of Protopanaxadiol-Type Saponins and Protopanaxatriol-Type Saponins from Ginseng
Structural Characters and Pharmacological Activity of Protopanaxadiol-Type Saponins and Protopanaxatriol-Type Saponins from Ginseng Abstract Ginseng has a long history of drug application in China, which can treat various diseases and achieve significant efficacy. Ginsenosides have always been deemed important ingredie...
PMC11327196
core_pubmed_pmc
A phase 1 study to assess the absolute bioavailability, mass balance, pharmacokinetics, metabolism, and excretion of [ 14 C]-mobocertinib, an oral inhibitor of EGFR exon 20 insertion mutations, in healthy participants
A phase 1 study to assess the absolute bioavailability, mass balance, pharmacokinetics, metabolism, and excretion of [ 14 C]-mobocertinib, an oral inhibitor of EGFR exon 20 insertion mutations, in healthy participants Abstract Abstract Mobocertinib (TAK-788) is a first-in-class oral epidermal growth factor receptor (EG...
PMC7060854
core_pubmed_pmc
From Xanthine Oxidase Inhibition to In Vivo Hypouricemic Effect: An Integrated Overview of In Vitro and In Vivo Studies with Focus on Natural Molecules and Analogues
From Xanthine Oxidase Inhibition to In Vivo Hypouricemic Effect: An Integrated Overview of In Vitro and In Vivo Studies with Focus on Natural Molecules and Analogues Abstract Abstract Hyperuricemia is characterized by elevated uric acid (UA) levels on blood, which can lead to gout, a common pathology. These high UA lev...
PMC10305065
core_pubmed_pmc
Rapid In Vitro Assessment of Antimicrobial Drug Effect Bridging Clinically Relevant Pharmacokinetics: A Comprehensive Methodology
Rapid In Vitro Assessment of Antimicrobial Drug Effect Bridging Clinically Relevant Pharmacokinetics: A Comprehensive Methodology Abstract Abstract Rapid in vitro assessment of antimicrobial drug efficacy under clinically relevant pharmacokinetic conditions is an essential element of both drug development and clinical ...
PMC5700357
core_pubmed_pmc
A Dynamic Stress Model Explains the Delayed Drug Effect in Artemisinin Treatment of Plasmodium falciparum
A Dynamic Stress Model Explains the Delayed Drug Effect in Artemisinin Treatment of Plasmodium falciparum Abstract ABSTRACT Artemisinin resistance constitutes a major threat to the continued success of control programs for malaria, particularly in light of developing resistance to partner drugs. Improving our understan...
PMC6644748
core_pubmed_pmc
Preclinical Development of Crocus sativus -Based Botanical Lead IIIM-141 for Alzheimer’s Disease: Chemical Standardization, Efficacy, Formulation Development, Pharmacokinetics, and Safety Pharmacology
Preclinical Development of Crocus sativus -Based Botanical Lead IIIM-141 for Alzheimer’s Disease: Chemical Standardization, Efficacy, Formulation Development, Pharmacokinetics, and Safety Pharmacology Abstract Crocus sativus L. (family: Iridaceae) has been documented in traditional medicine with numerous medicinal prop...
PMC7877857
core_pubmed_pmc
Pharmacogenomics Biomarker Discovery and Validation for Translation in Clinical Practice
Pharmacogenomics Biomarker Discovery and Validation for Translation in Clinical Practice Abstract Abstract Interindividual variability in drug efficacy and toxicity is a major challenge in clinical practice. Variations in drug pharmacokinetics (PKs) and pharmacodynamics (PDs) can be, in part, explained by polymorphic v...
PMC7365466
core_pubmed_pmc
Mechanistic model of hormonal contraception
Mechanistic model of hormonal contraception Abstract Abstract Contraceptive drugs intended for family planning are used by the majority of married or in-union women in almost all regions of the world. The two most prevalent types of hormones associated with contraception are synthetic estrogens and progestins. Hormonal...
PMC12018761
core_pubmed_pmc
A proof-of-mechanism trial in asthma with lunsekimig, a bispecific NANOBODY molecule
A proof-of-mechanism trial in asthma with lunsekimig, a bispecific NANOBODY molecule Abstract Background Monovalent biologics blocking thymic stromal lymphopoietin (TSLP) or interleukin (IL)-13 have been shown to elicit pharmacodynamic responses in asthma following a single dose. Therefore, dual blockade of these cytok...
PMC5045546
core_pubmed_pmc
Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration
Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration Abstract The previous investigation has proved that their existed pharmacokinetic difference between the different crystal forms of the polymorphic drugs after oral administration. However, no systemic investigations have ...
PMC9229059
core_pubmed_pmc
Aphrodisiac Performance of Bioactive Compounds from Mimosa pudica Linn.: In Silico Molecular Docking and Dynamics Simulation Approach
Aphrodisiac Performance of Bioactive Compounds from Mimosa pudica Linn.: In Silico Molecular Docking and Dynamics Simulation Approach Abstract Plants and their derived molecules have been traditionally used to manage numerous pathological complications, including male erectile dysfunction (ED). Mimosa pudica Linn. comm...
PMC11427368
core_pubmed_pmc
Quantitative pulmonary pharmacokinetics of tetrandrine for SARS-CoV-2 repurposing: a physiologically based pharmacokinetic modeling approach
Quantitative pulmonary pharmacokinetics of tetrandrine for SARS-CoV-2 repurposing: a physiologically based pharmacokinetic modeling approach Abstract Tetrandrine (TET) has been traditionally used in China as a medication to treat silicosis and has recently demonstrated anti-SARS-CoV-2 potential in vitro . By recognizin...
PMC12856972
core_pubmed_pmc
The Pathway to Proof‐of‐Concept for BNC210, a Negative Allosteric Modulator of the Alpha‐7 Nicotinic Acetylcholine Receptor (nAChR), for Treatment of Psychiatric Disease
The Pathway to Proof‐of‐Concept for BNC210, a Negative Allosteric Modulator of the Alpha‐7 Nicotinic Acetylcholine Receptor (nAChR), for Treatment of Psychiatric Disease Abstract Abstract BNC210 is an investigational small molecule selective negative allosteric modulator of the alpha‐7 nicotinic acetylcholine receptor ...
PMC12314108
core_pubmed_pmc
Pharmacokinetics and Safety Evaluation of a New Generic Sitafloxacin: A Phase I Bioequivalence Study in Healthy Chinese Participants
Pharmacokinetics and Safety Evaluation of a New Generic Sitafloxacin: A Phase I Bioequivalence Study in Healthy Chinese Participants Abstract Abstract Sitafloxacin is a new antibiotic drug belonging to the fourth generation quinolone antibiotics. The aim of this study was to evaluate the pharmacokinetics (PK), safety p...
PMC12433911
core_pubmed_pmc
State of Art of Dose Individualization to Support tacrolimus drug monitoring: What’s Next?
State of Art of Dose Individualization to Support tacrolimus drug monitoring: What’s Next? Abstract Abstract Tacrolimus is an immunosuppressant with a narrow therapeutic index and a high intra- and inter-patient variability showing significant challenges in optimal dosing and monitoring. Historically, pre-dose concentr...
PMC12587444
core_pubmed_pmc
Intravitreal Sustained Release of Dexamethasone from a Self-Healing Injectable Hydrogel: An In Vivo Safety and Release Study
Intravitreal Sustained Release of Dexamethasone from a Self-Healing Injectable Hydrogel: An In Vivo Safety and Release Study Abstract Abstract Corticosteroids, such as dexamethasone, are clinically used in intravitreal injections for the treatment of inflammatory and age-related ocular diseases; however, frequent injec...
PMC8151456
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Target Attainment Based on Measured versus Predicted Unbound Ceftriaxone Concentrations in Critically Ill Patients with Pneumonia: An Observational Cohort Study
Pharmacokinetic/Pharmacodynamic Target Attainment Based on Measured versus Predicted Unbound Ceftriaxone Concentrations in Critically Ill Patients with Pneumonia: An Observational Cohort Study Abstract Abstract The impact of ceftriaxone pharmacokinetic alterations on protein binding and PK/PD target attainment still re...
PMC9607815
core_pubmed_pmc
Overestimation of the effect of (fos)aprepitant on intravenous dexamethasone pharmacokinetics requires adaptation of the guidelines for children with chemotherapy-induced nausea and vomiting
Overestimation of the effect of (fos)aprepitant on intravenous dexamethasone pharmacokinetics requires adaptation of the guidelines for children with chemotherapy-induced nausea and vomiting Abstract Purpose Chemotherapy-induced nausea and vomiting (CINV) are common side effects in pediatric oncology treatment. Besides...
PMC9463487
core_pubmed_pmc
Novel assays for quality evaluation of XueBiJing: Quality variability of a Chinese herbal injection for sepsis management
Novel assays for quality evaluation of XueBiJing: Quality variability of a Chinese herbal injection for sepsis management Abstract XueBiJing is an intravenous five-herb injection used to treat sepsis in China. The study aimed to develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS)- or liquid chromatograp...
PMC11994927
core_pubmed_pmc
Physiologically based pharmacokinetic model of sodium-glucose cotransporter 2 inhibitors predicted pharmacokinetics and pharmacodynamics to explore dosage regimen for patients with type 2 diabetes mellitus and renal insufficiency
Physiologically based pharmacokinetic model of sodium-glucose cotransporter 2 inhibitors predicted pharmacokinetics and pharmacodynamics to explore dosage regimen for patients with type 2 diabetes mellitus and renal insufficiency Abstract Abstract Objective This study aimed to compare the hypoglycemic effects of four S...
PMC9287422
core_pubmed_pmc
Dose–Exposure–Response Analysis of the Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone on UACR and eGFR: An Analysis from FIDELIO-DKD
Dose–Exposure–Response Analysis of the Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone on UACR and eGFR: An Analysis from FIDELIO-DKD Abstract Background and Objective Finerenone reduces the risk of kidney failure in patients with chronic kidney disease and type 2 diabetes. Changes in the urine albumin-to...
PMC12511071
core_pubmed_pmc
Optimization of gabapentin dosage in pediatric patients with renal impairment: a physiologically based pharmacokinetic modeling approach
Optimization of gabapentin dosage in pediatric patients with renal impairment: a physiologically based pharmacokinetic modeling approach Abstract Abstract Background Gabapentin (GAB) is an adjunctive antiepileptic drug widely used in pediatric patients. However, little is known about its pharmacokinetics in pediatric p...
PMC6457330
core_pubmed_pmc
Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates † †Electronic supplementary information (ESI) available. See DOI: 10.1039/c9sc00285e
Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates † †Electronic supplementary information (ESI) available. See DOI: 10.1039/c9sc00285e Abstract A new antibody-drug conjugate (ADC) chemical drug-linker platform based on polysarcosine enables increased drug-loading, improved pharmacokinetics and exq...
PMC7612180
core_pubmed_pmc
Scotland's 2009–2015 methadone-prescription cohort: Quintiles for daily dose of prescribed methadone and risk of methadone-specific death
Scotland's 2009–2015 methadone-prescription cohort: Quintiles for daily dose of prescribed methadone and risk of methadone-specific death Abstract Abstract Aims As methadone clients age, their drug-related death (DRD) risks increase, more than doubling at 45+ years for methadone-specific DRDs. Methods Using Community H...
PMC6152015
core_pubmed_pmc
Analytical Techniques and Pharmacokinetics of Gastrodia elata Blume and Its Constituents
Analytical Techniques and Pharmacokinetics of Gastrodia elata Blume and Its Constituents Abstract Gastrodia elata Blume ( G. elata ), commonly called Tianma in Chinese, is an important and notable traditional Chinese medicine (TCM), which has been used in China as an anticonvulsant, analgesic, sedative, anti-asthma, an...
PMC12706426
core_pubmed_pmc
An Open‐Source Framework for Virtual Bioequivalence Modeling and Clinical Trial Design
An Open‐Source Framework for Virtual Bioequivalence Modeling and Clinical Trial Design Abstract ABSTRACT To establish bioequivalence (BE) of a generic test formulation with respect to a reference listed drug, it is necessary to demonstrate a comparable rate and extent to which active ingredients reach the site of actio...
PMC12422889
core_pubmed_pmc
Pharmacokinetics and safety of highly variable nitroglycerin lingual spray (NLS) versus US-licensed nitroglycerin lingual spray reference product (Nitrolingual ® ): a randomized, four-cycle, four-sequence, partially replicated crossover Phase I bioequivalence clinical trial
Pharmacokinetics and safety of highly variable nitroglycerin lingual spray (NLS) versus US-licensed nitroglycerin lingual spray reference product (Nitrolingual ® ): a randomized, four-cycle, four-sequence, partially replicated crossover Phase I bioequivalence clinical trial Abstract Abstract Purpose In this Phase I stu...
PMC11339314
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and safety of GS‐3583, a FLT3 agonist Fc fusion protein, from single‐ascending‐dose phase I study in healthy participants
Pharmacokinetics, pharmacodynamics, and safety of GS‐3583, a FLT3 agonist Fc fusion protein, from single‐ascending‐dose phase I study in healthy participants Abstract Abstract Conventional dendritic cells subtype 1 (cDC1) play a vital role in the priming and expansion of tumor‐specific CD8+ T cells and their recruitmen...
PMC9279626
core_pubmed_pmc
Multiparametric characterization of red blood cell physiology after hypotonic dialysis based drug encapsulation process
Multiparametric characterization of red blood cell physiology after hypotonic dialysis based drug encapsulation process Abstract Red blood cells (RBCs) can act as carriers for therapeutic agents and can substantially improve the safety, pharmacokinetics, and pharmacodynamics of many drugs. Maintaining RBCs integrity an...
PMC8195771
core_pubmed_pmc
Therapeutic Drug Monitoring in Non-Tuberculosis Mycobacteria Infections
Therapeutic Drug Monitoring in Non-Tuberculosis Mycobacteria Infections Abstract Nontuberculous mycobacteria can cause minimally symptomatic self-limiting infections to progressive and life-threatening disease of multiple organs. Several factors such as increased testing and prevalence have made this an emerging infect...
PMC7003779
core_pubmed_pmc
Pharmacokinetic Properties of Single and Multiple Doses of Ertugliflozin, a Selective Inhibitor of SGLT2, in Healthy Chinese Subjects
Pharmacokinetic Properties of Single and Multiple Doses of Ertugliflozin, a Selective Inhibitor of SGLT2, in Healthy Chinese Subjects Abstract Abstract Ertugliflozin, a sodium‐glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus, prevents renal glucose reabsorption resulting in urinary glucos...
PMC12739150
core_pubmed_pmc
Validated Erythrosin B spectrofluorimetric method for ganciclovir bioanalysis in rabbit plasma following valganciclovir bioconversion and Pharmacokinetic application
Validated Erythrosin B spectrofluorimetric method for ganciclovir bioanalysis in rabbit plasma following valganciclovir bioconversion and Pharmacokinetic application Abstract Abstract A novel, environmentally sustainable spectrofluorimetric method was developed and validated for sensitive determination of ganciclovir i...
PMC7773283
core_pubmed_pmc
Intrathecal catheter implantation decreases cerebrospinal fluid dynamics in cynomolgus monkeys
Intrathecal catheter implantation decreases cerebrospinal fluid dynamics in cynomolgus monkeys Abstract Abstract A detailed understanding of the CSF dynamics is needed for design and optimization of intrathecal drug delivery devices, drugs, and protocols. Preclinical research using large-animal models is important to h...
PMC2945041
core_pubmed_pmc
Liposomal encapsulation enhances and prolongs the anti-inflammatory effects of water-soluble dexamethasone phosphate in experimental adjuvant arthritis
Liposomal encapsulation enhances and prolongs the anti-inflammatory effects of water-soluble dexamethasone phosphate in experimental adjuvant arthritis Abstract Abstract Introduction The objective of this study was to evaluate the efficacy of intravenous (i.v.) injection of liposomally encapsulated dexamethasone phosph...
PMC2889282
core_pubmed_pmc
Assessing circadian rhythms in propofol PK and PD during prolonged infusion in ICU patients
Assessing circadian rhythms in propofol PK and PD during prolonged infusion in ICU patients Abstract Abstract This study evaluates possible circadian rhythms during prolonged propofol infusion in patients in the intensive care unit. Eleven patients were sedated with a constant propofol infusion. The blood samples for t...
PMC9309146
core_pubmed_pmc
Pharmacokinetics and Exposure-Response Analysis of Venetoclax + Obinutuzumab in Chronic Lymphocytic Leukemia: Phase 1b Study and Phase 3 CLL14 Trial
Pharmacokinetics and Exposure-Response Analysis of Venetoclax + Obinutuzumab in Chronic Lymphocytic Leukemia: Phase 1b Study and Phase 3 CLL14 Trial Abstract Abstract Introduction This study aims to investigate pharmacokinetics (PK) and exposure-response parameters of the 400 mg once-daily venetoclax dose regimen in co...
PMC7480408
core_pubmed_pmc
Improved bioavailability of cromolyn sodium using inhaled PA101 delivered via eFlow® nebulizer
Improved bioavailability of cromolyn sodium using inhaled PA101 delivered via eFlow® nebulizer Abstract ABSTRACT In 1960s, cromolyn sodium (CS) has been introduced as the first non-steroidal anti-inflammatory drug for the treatment of allergic and mast-cell driven diseases. Its applicability has been limited due to a p...
PMC5032972
core_pubmed_pmc
Comparison of the pharmacokinetics of an oral extended‐release capsule formulation of carbidopa‐levodopa (IPX066) with immediate‐release carbidopa‐levodopa (Sinemet ® ), sustained‐release carbidopa‐levodopa (Sinemet ® CR), and carbidopa‐levodopa‐entacapone (Stalevo ® )
Comparison of the pharmacokinetics of an oral extended‐release capsule formulation of carbidopa‐levodopa (IPX066) with immediate‐release carbidopa‐levodopa (Sinemet ® ), sustained‐release carbidopa‐levodopa (Sinemet ® CR), and carbidopa‐levodopa‐entacapone (Stalevo ® ) Abstract Abstract IPX066 (extended‐release carbido...
PMC12672809
core_pubmed_pmc
Selection of isatuximab dosing regimen in pediatric patients with leukemia using population pharmacokinetics
Selection of isatuximab dosing regimen in pediatric patients with leukemia using population pharmacokinetics Abstract Purpose Isatuximab, an immunoglobulin G monoclonal antibody that targets a specific CD38 epitope, is approved in combination with dexamethasone plus either pomalidomide or carfilzomib for treatment of a...
PMC5438475
core_pubmed_pmc
Levodopa-Carbidopa Intestinal Gel Pharmacokinetics: Lower Variability than Oral Levodopa-Carbidopa
Levodopa-Carbidopa Intestinal Gel Pharmacokinetics: Lower Variability than Oral Levodopa-Carbidopa Abstract In a double-blind, double-dummy, double-titration Phase 3 trial in advanced Parkinson’s disease (PD) patients, the efficacy and safety of Levodopa-carbidopa intestinal gel (LCIG) infusion were characterized relat...
PMC5102576
core_pubmed_pmc
Batch‐to‐batch pharmacokinetic variability confounds current bioequivalence regulations: A dry powder inhaler randomized clinical trial
Batch‐to‐batch pharmacokinetic variability confounds current bioequivalence regulations: A dry powder inhaler randomized clinical trial Abstract Abstract Current pharmacokinetic (PK) bioequivalence guidelines do not account for batch‐to‐batch variability in study design or analysis. Here we evaluate the magnitude of ba...
PMC11652471
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Intravenous Efgartigimod and Subcutaneous Efgartigimod PH20 in Healthy Chinese Participants
Pharmacokinetics, Pharmacodynamics, and Safety of Intravenous Efgartigimod and Subcutaneous Efgartigimod PH20 in Healthy Chinese Participants Abstract Background Efgartigimod, a human immunoglobulin G (IgG)1-derived Fc fragment targeting the neonatal Fc receptor, has been developed into intravenous (IV) and subcutaneou...
PMC11266212
core_pubmed_pmc
Effect of Clarithromycin, a Strong CYP3A and P-glycoprotein Inhibitor, on the Pharmacokinetics of Edoxaban in Healthy Volunteers and the Evaluation of the Drug Interaction with Other Oral Factor Xa Inhibitors by a Microdose Cocktail Approach
Effect of Clarithromycin, a Strong CYP3A and P-glycoprotein Inhibitor, on the Pharmacokinetics of Edoxaban in Healthy Volunteers and the Evaluation of the Drug Interaction with Other Oral Factor Xa Inhibitors by a Microdose Cocktail Approach Abstract Purpose We assessed the differential effect of clarithromycin, a stro...
PMC11711308
core_pubmed_pmc
The paradigm of stem cell secretome in tissue repair and regeneration: Present and future perspectives
The paradigm of stem cell secretome in tissue repair and regeneration: Present and future perspectives Abstract Abstract As the number of patients requiring organ transplants continues to rise exponentially, there is a dire need for therapeutics, with repair and regenerative properties, to assist in alleviating this me...
PMC8505218
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Huanglian-Houpo Decoction Based on Berberine Hydrochloride and Magnolol Against H1N1 Influenza Virus
Pharmacokinetics and Pharmacodynamics of Huanglian-Houpo Decoction Based on Berberine Hydrochloride and Magnolol Against H1N1 Influenza Virus Abstract Abstract Background and Objectives Huanglian-Houpo decoction (HH), which is recorded in the famous traditional Chinese medicine monograph “Puji Fang,” contains two indiv...
PMC11325518
core_pubmed_pmc
Progress in Research on Inhibitors Targeting SARS-CoV-2 Main Protease (M pro )
Progress in Research on Inhibitors Targeting SARS-CoV-2 Main Protease (M pro ) Abstract Since 2019, the novel coronavirus (SARS-CoV-2) has caused significant morbidity and millions of deaths worldwide. The Coronavirus Disease 2019 (COVID-19), caused by SARS-CoV-2 and its variants, has further highlighted the urgent nee...
PMC12128049
core_pubmed_pmc
Translational Modeling of BTZ-043 to Predict Phase 2A Efficacy and Evaluate Drug-Drug Interactions With Bedaquiline, Pretomanid, and Linezolid in Murine Models
Translational Modeling of BTZ-043 to Predict Phase 2A Efficacy and Evaluate Drug-Drug Interactions With Bedaquiline, Pretomanid, and Linezolid in Murine Models Abstract Abstract Background BTZ-043 is a promising novel drug candidate for antituberculosis treatment. This study aimed to apply a previously developed mouse-...
PMC11926788
core_pubmed_pmc
Effect of SSR504734, a Selective Glycine Transporter Type 1 Inhibitor, on Seizure Thresholds, Neurotransmitter Levels, and Inflammatory Markers in Mice
Effect of SSR504734, a Selective Glycine Transporter Type 1 Inhibitor, on Seizure Thresholds, Neurotransmitter Levels, and Inflammatory Markers in Mice Abstract Abstract Studies have revealed that inhibition of glycine transporter type 1 (GlyT1) may provide a balanced regulation between excitation and inhibition in som...
PMC12257498
core_pubmed_pmc
Sacituzumab Govitecan Population Pharmacokinetics: Updated Analyses Using HR +/ HER2 − Metastatic Breast Cancer Data From the Phase 3 TROPiCS ‐02 Trial
Sacituzumab Govitecan Population Pharmacokinetics: Updated Analyses Using HR +/ HER2 − Metastatic Breast Cancer Data From the Phase 3 TROPiCS ‐02 Trial Abstract ABSTRACT Sacituzumab govitecan (SG) is an antibody–drug conjugate composed of a Trop‐2–directed antibody coupled to SN‐38. SG is approved in multiple countries...
PMC7731530
core_pubmed_pmc
Vancomycin Exposure and Acute Kidney Injury Outcome: A Snapshot From the CAMERA2 Study
Vancomycin Exposure and Acute Kidney Injury Outcome: A Snapshot From the CAMERA2 Study Abstract Abstract Among patients with methicillin-resistant Staphylococcus aureus (MRSA) bacteremia from a prospective randomized clinical trial, acute kidney injury (AKI) rates increased with increasing vancomycin exposure, even wit...
PMC7828008
core_pubmed_pmc
Development and Characterization of Treprostinil Palmitil Inhalation Aerosol for the Investigational Treatment of Pulmonary Arterial Hypertension
Development and Characterization of Treprostinil Palmitil Inhalation Aerosol for the Investigational Treatment of Pulmonary Arterial Hypertension Abstract Treprostinil palmitil (TP) is a prodrug of treprostinil (TRE), a pulmonary vasodilator that has been previously formulated for inhaled administration via a nebulizer...
PMC4168385
core_pubmed_pmc
Model-based clinical pharmacology profiling of ipilimumab in patients with advanced melanoma
Model-based clinical pharmacology profiling of ipilimumab in patients with advanced melanoma Abstract Aim Ipilimumab is a fully human, monoclonal antibody that blocks cytotoxic T-lymphocyte antigen-4. The objective of the present study was to characterize the clinical pharmacology profile of ipilimumab using a populati...
PMC4492750
core_pubmed_pmc
The discovery of a selective and potent A 2a agonist with extended lung retention
The discovery of a selective and potent A 2a agonist with extended lung retention Abstract Abstract Although the anti-inflammatory role of the A 2a receptor is well established, controversy remains with regard to the therapeutic value for A 2a agonists in treatment of inflammatory lung diseases, also as a result of unw...
PMC7317698
core_pubmed_pmc
High nitrogen stainless steel drug-eluting stent - Assessment of pharmacokinetics and preclinical safety in vivo
High nitrogen stainless steel drug-eluting stent - Assessment of pharmacokinetics and preclinical safety in vivo Abstract Pharmacokinetic analyses were performed using 20 pigs for 120-days implantation, while one sirolimus-eluting stent was implanted into one of their coronary artery. At different time points, the resi...
PMC8021896
core_pubmed_pmc
A randomized, double-blind, placebo-controlled phase 1 trial of inhaled and intranasal niclosamide: A broad spectrum antiviral candidate for treatment of COVID-19
A randomized, double-blind, placebo-controlled phase 1 trial of inhaled and intranasal niclosamide: A broad spectrum antiviral candidate for treatment of COVID-19 Abstract Abstract Background Coronavirus disease 19 (COVID-19) is spreading globally and treatment options remain limited. A formulation of niclosamide, a po...
PMC3299584
core_pubmed_pmc
A phase I study evaluating the pharmacokinetics, safety and tolerability of an antibody-based tissue factor antagonist in subjects with acute lung injury or acute respiratory distress syndrome
A phase I study evaluating the pharmacokinetics, safety and tolerability of an antibody-based tissue factor antagonist in subjects with acute lung injury or acute respiratory distress syndrome Abstract Abstract Background The tissue factor (TF)-dependent extrinsic pathway has been suggested to be a central mechanism by...
PMC8082182
core_pubmed_pmc
Modeling Approach to Optimizing Dose Regimen of Vancomycin for Chinese Pediatric Patients with Gram-Positive Bacterial Infections
Modeling Approach to Optimizing Dose Regimen of Vancomycin for Chinese Pediatric Patients with Gram-Positive Bacterial Infections Abstract Abstract The aim of this study was to establish the population pharmacokinetics (PK) model of Vancomycin for Chinese pediatric patients which can extrapolate to whole age periods by...
PMC11507457
core_pubmed_pmc
The Yin and Yang of the Natural Product Triptolide and Its Interactions with XPB, an Essential Protein for Gene Expression and DNA Repair
The Yin and Yang of the Natural Product Triptolide and Its Interactions with XPB, an Essential Protein for Gene Expression and DNA Repair Abstract Abstract Triptolide, a bioactive diterpene tri-epoxide extracted from Tripterygium wilfordii Hook F (TWHF), exhibits notable pharmacological activities, including anti-infla...
PMC12587603
core_pubmed_pmc
Targeting Pseudomonas aeruginosa resistance at the exposure frontier: a population PK/PD blueprint for ceftolozane/tazobactam continuous infusion
Targeting Pseudomonas aeruginosa resistance at the exposure frontier: a population PK/PD blueprint for ceftolozane/tazobactam continuous infusion Abstract ABSTRACT Ceftolozane/tazobactam is a key antibiotic for Pseudomonas aeruginosa infections. Our objective was to determine whether continuous infusion (CI) of ceftolo...
PMC5064159
core_pubmed_pmc
Partnerships to Design Novel Regimens to Treat Childhood Tuberculosis, Sui Generis : The Road Ahead
Partnerships to Design Novel Regimens to Treat Childhood Tuberculosis, Sui Generis : The Road Ahead Abstract There has been a recent expansion of preclinical models to predict the efficacy of regimens to treat adults with tuberculosis. Despite increasing global interest in childhood tuberculosis, these same tools have ...
PMC4075108
core_pubmed_pmc
Establishing a clinical pharmacology fellowship program for physicians, pharmacists, and pharmacologists: a newly accredited interdisciplinary training program at the Ohio State University
Establishing a clinical pharmacology fellowship program for physicians, pharmacists, and pharmacologists: a newly accredited interdisciplinary training program at the Ohio State University Abstract Abstract Studying the effect of drugs on humans, clinical pharmacologists play an essential role in many academic medical ...
PMC10668089
core_pubmed_pmc
A randomized, single ascending dose safety, tolerability and pharmacokinetics study of NicaPlant® in aneurysmal subarachnoid hemorrhage patients undergoing clipping
A randomized, single ascending dose safety, tolerability and pharmacokinetics study of NicaPlant® in aneurysmal subarachnoid hemorrhage patients undergoing clipping Abstract Abstract Introduction Aneurysmal subarachnoid hemorrhage (aSAH) is associated with high morbidity and mortality. Post-hemorrhagic vasospasm with n...
PMC12182170
core_pubmed_pmc
Phase 1 first-in-human dose-escalation study of IMSA101, a novel cyclic di-nucleotide STING agonist, for patients with advanced solid tumor malignancies
Phase 1 first-in-human dose-escalation study of IMSA101, a novel cyclic di-nucleotide STING agonist, for patients with advanced solid tumor malignancies Abstract Abstract Background Despite progress in cancer therapeutics, there remains an unmet need for treatment of advanced solid tumors. The cGAS-cGAMP-STING pathway ...
PMC4513224
core_pubmed_pmc
Relationship Between Sunitinib Pharmacokinetics and Administration Time: Preclinical and Clinical Evidence
Relationship Between Sunitinib Pharmacokinetics and Administration Time: Preclinical and Clinical Evidence Abstract Abstract Background and Objective Circadian rhythms may influence the pharmacokinetics of drugs. This study aimed to elucidate whether the pharmacokinetics of the orally administered drug sunitinib are su...
PMC6669357
core_pubmed_pmc
Pharmacokinetics of Arctigenin and Fructus Arctii Powder in Piglets
Pharmacokinetics of Arctigenin and Fructus Arctii Powder in Piglets Abstract Abstract Fructus arctii, also known as great power seed, is the dried fruit of Arctium lappa of the family Compositae. It is a commonly used veterinary herbal medicine, and arctigenin is the main active ingredient. The aim of this study was to...
PMC10848431
core_pubmed_pmc
Effects of CYP3A4*22 and POR*28 variations on the pharmacokinetics of tacrolimus in renal transplant recipients: a meta-analysis of 18 observational studies
Effects of CYP3A4*22 and POR*28 variations on the pharmacokinetics of tacrolimus in renal transplant recipients: a meta-analysis of 18 observational studies Abstract Abstract Purpose This study aimed to investigate the association between cytochrome P450 (CYP) 3A4*22 and cytochrome P450 oxidoreductase (POR)*28 variatio...
PMC8596159
core_pubmed_pmc
Pharmacokinetics of meropenem in critically ill patients in Saudi Arabia
Pharmacokinetics of meropenem in critically ill patients in Saudi Arabia Abstract Abstract Background Meropenem is commonly used in the ICU to treat gram-negative infections. Due to various pathophysiological changes, critically ill patients are at higher risk of having subtherapeutic concentrations and hence have a hi...
PMC5519802
core_pubmed_pmc
Results of the safety run-in part of the METAL (METformin in Advanced Lung cancer) study: a multicentre, open-label phase I–II study of metformin with erlotinib in second-line therapy of patients with stage IV non-small-cell lung cancer
Results of the safety run-in part of the METAL (METformin in Advanced Lung cancer) study: a multicentre, open-label phase I–II study of metformin with erlotinib in second-line therapy of patients with stage IV non-small-cell lung cancer Abstract Abstract Purpose Our previous works demonstrated the ability of metformin ...
PMC6021765
core_pubmed_pmc
Anti-colchicine Fab fragments prevent lethal colchicine toxicity in a porcine model: a pharmacokinetic and clinical study
Anti-colchicine Fab fragments prevent lethal colchicine toxicity in a porcine model: a pharmacokinetic and clinical study Abstract Abstract Background: Colchicine poisoning is commonly lethal. Colchicine-specific Fab fragments increase rat urinary colchicine clearance and have been associated with a good outcome in one...
PMC5345771
core_pubmed_pmc
Low-cost, rapidly-developed, 3D printed in vitro corpus callosum model for mucopolysaccharidosis type I
Low-cost, rapidly-developed, 3D printed in vitro corpus callosum model for mucopolysaccharidosis type I Abstract The rising prevalence of high throughput screening and the general inability of (1) two dimensional (2D) cell culture and (2) in vitro release studies to predict in vivo neurobiological and pharmacokinetic r...
PMC11181355
core_pubmed_pmc
Feasibility exploration of GSH in the treatment of acute hepatic encephalopathy from the aspects of pharmacokinetics, pharmacodynamics, and mechanism
Feasibility exploration of GSH in the treatment of acute hepatic encephalopathy from the aspects of pharmacokinetics, pharmacodynamics, and mechanism Abstract Our previous study highlighted the therapeutic potential of glutathione (GSH), an intracellular thiol tripeptide ubiquitous in mammalian tissues, in mitigating h...
PMC5598964
core_pubmed_pmc
A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions
A quantitative systems pharmacology approach, incorporating a novel liver model, for predicting pharmacokinetic drug-drug interactions Abstract Abstract All pharmaceutical companies are required to assess pharmacokinetic drug-drug interactions (DDIs) of new chemical entities (NCEs) and mathematical prediction helps to ...
PMC12546730
core_pubmed_pmc
Endothelial soluble guanylate cyclase enzyme inhibitors as a novel target for the treatment of sepsis-related hypotension
Endothelial soluble guanylate cyclase enzyme inhibitors as a novel target for the treatment of sepsis-related hypotension Abstract Sepsis-related hypotension is a life-threatening condition due to systemic infection leading to widespread inflammation and blood vessel dilation. This can cause a dramatic drop in blood pr...