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PMC12816458
core_pubmed_pmc
Pharmacokinetics and Safety of Ustekinumab in Patients with Juvenile Psoriatic Arthritis: Results of the Real-World Ustekinumab Pediatric Opportunistic Pharmacokinetics Study (U-POPS)
Pharmacokinetics and Safety of Ustekinumab in Patients with Juvenile Psoriatic Arthritis: Results of the Real-World Ustekinumab Pediatric Opportunistic Pharmacokinetics Study (U-POPS) Abstract Introduction The “Ustekinumab Pediatric Opportunistic Pharmacokinetics Study” (U-POPS) was conducted to evaluate the pharmacoki...
PMC3726368
core_pubmed_pmc
Glomerular Filtration Rate (GFR) determination via individual kinetics of the inulin-like polyfructosan sinistrin versus creatinine-based population-derived regression formulae
Glomerular Filtration Rate (GFR) determination via individual kinetics of the inulin-like polyfructosan sinistrin versus creatinine-based population-derived regression formulae Abstract Background In renal patients estimation of GFR is routinely done by means of population-based formulae using serum creatinine levels. ...
PMC4873565
core_pubmed_pmc
Application of the Multistate Tuberculosis Pharmacometric Model in Patients With Rifampicin‐Treated Pulmonary Tuberculosis
Application of the Multistate Tuberculosis Pharmacometric Model in Patients With Rifampicin‐Treated Pulmonary Tuberculosis Abstract This is the first clinical implementation of the Multistate Tuberculosis Pharmacometric (MTP) model describing fast‐, slow‐, and nonmultiplying bacterial states of Mycobacterium tuberculos...
PMC3271346
core_pubmed_pmc
In silico Models of Alcohol Dependence and Treatment
In silico Models of Alcohol Dependence and Treatment Abstract Abstract In this paper we view alcohol dependence and the response to treatment as a recurrent bio-behavioral process developing in time and propose formal models of this process combining behavior and biology in silico . The behavioral components of alcohol...
PMC6921073
core_pubmed_pmc
Folate Receptor-Targeting and Reactive Oxygen Species-Responsive Liposomal Formulation of Methotrexate for Treatment of Rheumatoid Arthritis
Folate Receptor-Targeting and Reactive Oxygen Species-Responsive Liposomal Formulation of Methotrexate for Treatment of Rheumatoid Arthritis Abstract Abstract Multifunctional nanomedicines with active targeting and stimuli-responsive drug release function utilizing pathophysiological features of the disease are regarde...
PMC5634778
core_pubmed_pmc
Fixed Dosing of Monoclonal Antibodies in Oncology
Fixed Dosing of Monoclonal Antibodies in Oncology Abstract In the field of oncology, most drugs are administered in a body–size‐based dosing schedule instead of a fixed dose for all patients. This article presents the advantages of fixed dosing of monoclonal antibodies, arguing in favor of fixed dosing schemes for all ...
PMC9314635
core_pubmed_pmc
OX40L Inhibition Suppresses KLH‐driven Immune Responses in Healthy Volunteers: A Randomized Controlled Trial Demonstrating Proof‐of‐Pharmacology for KY1005
OX40L Inhibition Suppresses KLH‐driven Immune Responses in Healthy Volunteers: A Randomized Controlled Trial Demonstrating Proof‐of‐Pharmacology for KY1005 Abstract The safety, tolerability, immunogenicity, and pharmacokinetic (PK) profile of an anti‐OX40L monoclonal antibody (KY1005, currently amlitelimab) were evalua...
PMC9639121
core_pubmed_pmc
Population pharmacokinetics in critically ill neonates and infants undergoing extracorporeal membrane oxygenation: a literature review
Population pharmacokinetics in critically ill neonates and infants undergoing extracorporeal membrane oxygenation: a literature review Abstract Abstract Extracorporeal membrane oxygenation (ECMO) increases circulating blood volume, causes capillary leak and temporarily alters kidney function. Consequently, pharmacokine...
PMC5627594
core_pubmed_pmc
A Quadrupole Dalton-based multi-attribute method for product characterization, process development, and quality control of therapeutic proteins
A Quadrupole Dalton-based multi-attribute method for product characterization, process development, and quality control of therapeutic proteins Abstract ABSTRACT During manufacturing and storage process, therapeutic proteins are subject to various post-translational modifications (PTMs), such as isomerization, deamidat...
PMC10099789
core_pubmed_pmc
Fifty years with aspirin and platelets
Fifty years with aspirin and platelets Abstract Abstract In 2021, we reached the 50th anniversary of the publication of Sir John Vane's seminal paper in Nature New Biology describing the experiments supporting his mechanistic hypothesis that inhibition of prostaglandin synthesis might explain the main pharmacological e...
PMC6411714
core_pubmed_pmc
Inhibitors of Human ABCG2: From Technical Background to Recent Updates With Clinical Implications
Inhibitors of Human ABCG2: From Technical Background to Recent Updates With Clinical Implications Abstract Abstract The ATP-binding cassette transporter G2 (ABCG2; also known as breast cancer resistance protein, BCRP) has been suggested to be involved in clinical multidrug resistance (MDR) in cancer like other ABC tran...
PMC3539064
core_pubmed_pmc
A phase II study of UCN-01 in combination with irinotecan in patients with metastatic triple negative breast cancer
A phase II study of UCN-01 in combination with irinotecan in patients with metastatic triple negative breast cancer Abstract Abstract Mutations in TP53 lead to a defective G1 checkpoint and the dependence on checkpoint kinase 1 (Chk1) for G2 or S phase arrest in response to DNA damage. In preclinical studies, Chk1 inhi...
PMC10581936
core_pubmed_pmc
Multivariate Exact Discrepancy: A New Tool for PK/PD Model Evaluation
Multivariate Exact Discrepancy: A New Tool for PK/PD Model Evaluation Abstract Background Pharmacokinetic models are evaluated using three types of metrics: those based on estimating the typical pharmacokinetic parameters, those based on predicting individual pharmacokinetic parameters and those that compare data and m...
PMC9965523
core_pubmed_pmc
Mannosylated-Chitosan-Coated Andrographolide Nanoliposomes for the Treatment of Hepatitis: In Vitro and In Vivo Evaluations
Mannosylated-Chitosan-Coated Andrographolide Nanoliposomes for the Treatment of Hepatitis: In Vitro and In Vivo Evaluations Abstract Abstract A key diterpene lactone of Andrographis paniculata, i.e., andrographolide (AG), exhibits a variety of physiological properties, including hepatoprotection. The limited solubility...
PMC7499187
core_pubmed_pmc
Development and Application of a Mechanistic Population Modeling Approach to Describe Abemaciclib Pharmacokinetics
Development and Application of a Mechanistic Population Modeling Approach to Describe Abemaciclib Pharmacokinetics Abstract Abstract Abemaciclib is an oral anticancer drug that inhibits cyclin dependent kinases 4 and 6 and is metabolized by cytochrome P450 3A in the intestines and liver to active metabolites. The objec...
PMC6985915
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Anti-infective Agents during Continuous Veno-venous Hemofiltration in Critically Ill Patients: Lessons Learned from an Ancillary Study of the IVOIRE Trial
Pharmacokinetics and Pharmacodynamics of Anti-infective Agents during Continuous Veno-venous Hemofiltration in Critically Ill Patients: Lessons Learned from an Ancillary Study of the IVOIRE Trial Abstract Abstract Background Hemofiltration rate, changes in blood and ultrafiltration flow, and discrepancies between the p...
PMC6462292
core_pubmed_pmc
Pharmacokinetics and Biodistribution of Rhopalurus junceus Scorpion Venom in Tumor-Bearing Mice after Intravenous and Oral Administration
Pharmacokinetics and Biodistribution of Rhopalurus junceus Scorpion Venom in Tumor-Bearing Mice after Intravenous and Oral Administration Abstract Abstract Introduction: Rhopalurus junceus scorpion venom has shown potential for anticancer treatment. However, there are no scientific evidence about venom pharmacokinetic ...
PMC10834751
core_pubmed_pmc
Towards a better detection of patients at-risk of linezolid toxicity in clinical practice: a prospective study in three Belgian hospital centers
Towards a better detection of patients at-risk of linezolid toxicity in clinical practice: a prospective study in three Belgian hospital centers Abstract Introduction: Linezolid is a last-resort antibiotic for infections caused by multidrug-resistant microorganisms. It is widely used for off-label indications and for l...
PMC9299227
core_pubmed_pmc
A phase 1 multiple‐ascending dose study of tirzepatide in Japanese participants with type 2 diabetes
A phase 1 multiple‐ascending dose study of tirzepatide in Japanese participants with type 2 diabetes Abstract Abstract Aim To investigate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of tirzepatide in Japanese participants with type 2 diabetes (T2D). Methods This phase 1, double‐blind, pla...
PMC12431657
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Discovery and mechanistic insights of dibenzoylmethane as a broad spectrum inhibitor of coronavirus
Discovery and mechanistic insights of dibenzoylmethane as a broad spectrum inhibitor of coronavirus Abstract Abstract Coronavirus, a large family of positive-sense RNA viruses, are responsible for both mild and severe respiratory illnesses, ranging from the common cold to life-threatening conditions. Despite significan...
PMC10960098
core_pubmed_pmc
Hepatotoxicity in patients with non-small cell lung cancer treated with sotorasib after prior immunotherapy: a comprehensive clinical and pharmacokinetic analysis
Hepatotoxicity in patients with non-small cell lung cancer treated with sotorasib after prior immunotherapy: a comprehensive clinical and pharmacokinetic analysis Abstract Summary Background Sotorasib given after immunotherapy could put patients at increased risk of hepatotoxicity. Therefore, there is a need to gain in...
PMC9127571
core_pubmed_pmc
Combining SJ733, an oral ATP4 inhibitor of Plasmodium falciparum , with the pharmacokinetic enhancer cobicistat: An innovative approach in antimalarial drug development
Combining SJ733, an oral ATP4 inhibitor of Plasmodium falciparum , with the pharmacokinetic enhancer cobicistat: An innovative approach in antimalarial drug development Abstract Summary Background SJ733, a newly developed inhibitor of P. falciparum ATP4, has a favorable safety profile and rapid antiparasitic effect but...
PMC6273160
core_pubmed_pmc
Phenylethanoid Glycosides: Research Advances in Their Phytochemistry, Pharmacological Activity and Pharmacokinetics
Phenylethanoid Glycosides: Research Advances in Their Phytochemistry, Pharmacological Activity and Pharmacokinetics Abstract Abstract Phenylethanoid glycosides (PhGs) are widely distributed in traditional Chinese medicines as well as in other medicinal plants, and they were characterized by a phenethyl alcohol (C 6 -C ...
PMC10836277
core_pubmed_pmc
Safety, tolerability and pharmacokinetics of forsythin in healthy subjects: a double-blinded, placebo-controlled single-dose and multiple-dose escalation and food effect study
Safety, tolerability and pharmacokinetics of forsythin in healthy subjects: a double-blinded, placebo-controlled single-dose and multiple-dose escalation and food effect study Abstract Abstract Background Forsythin, an active compound from Forsythiae Fructus, has the potential to treat the common cold and influenza thr...
PMC6204762
core_pubmed_pmc
Using Quantitative Systems Toxicology to Investigate Observed Species Differences in CKA-Mediated Hepatotoxicity
Using Quantitative Systems Toxicology to Investigate Observed Species Differences in CKA-Mediated Hepatotoxicity Abstract Abstract CKA, a chemokine receptor antagonist intended for treating inflammatory conditions, produced dose-dependent hepatotoxicity in rats but advanced into the clinic where single doses of CKA up ...
PMC7695171
core_pubmed_pmc
Equine Drug Transporters: A Mini-Review and Veterinary Perspective
Equine Drug Transporters: A Mini-Review and Veterinary Perspective Abstract Abstract Xenobiotic transport proteins play an important role in determining drug disposition and pharmacokinetics. Our understanding of the role of these important proteins in humans and pre-clinical animal species has increased substantially ...
PMC12691192
core_pubmed_pmc
Rationale and Emerging Evidence on the Potential Role of HoLEP-Mediated Relief of Bladder Outlet Obstruction in NMIBC Outcomes Through Optimal Management of Chronic Urinary Retention
Rationale and Emerging Evidence on the Potential Role of HoLEP-Mediated Relief of Bladder Outlet Obstruction in NMIBC Outcomes Through Optimal Management of Chronic Urinary Retention Abstract Simple Summary Bladder cancer is a common disease that often comes back even after successful treatment. This review looked at h...
PMC6309567
core_pubmed_pmc
Impact of pharmacogenetics on statin-induced myopathy in South-Indian subjects
Impact of pharmacogenetics on statin-induced myopathy in South-Indian subjects Abstract Objectives Statins are the most commonly prescribed medications for the treatment of atherosclerotic cardiovascular disease. Statin-associated adverse effects occur in ∼10% of patients and are associated with polymorphisms in severa...
PMC11519794
core_pubmed_pmc
Aspects and prospects of preclinical theranostic radiopharmaceutical development
Aspects and prospects of preclinical theranostic radiopharmaceutical development Abstract Abstract This article provides an overview of preclinical theranostic radiopharmaceutical development, highlighting aspects of the preclinical development stages that can lead towards a clinical trial. The key stages of theranosti...
PMC7913859
core_pubmed_pmc
In Silico Screening of Natural Products Isolated from Mexican Herbal Medicines against COVID-19
In Silico Screening of Natural Products Isolated from Mexican Herbal Medicines against COVID-19 Abstract Abstract The COVID-19 pandemic has already taken the lives of more than 2 million people worldwide, causing several political and socio-economic disturbances in our daily life. At the time of publication, there are ...
PMC8148525
core_pubmed_pmc
Polymeric and Lipid Nanoparticles: Which Applications in Pediatrics?
Polymeric and Lipid Nanoparticles: Which Applications in Pediatrics? Abstract This review aims to provide the state of the art on polymeric and lipid nanoparticles, used or suggested to approach pediatric diseases’ problems and needs, and to inspire new researches in this field. Several drugs are currently not availabl...
PMC6989266
core_pubmed_pmc
Characterization of circadian blood pressure patterns using non-linear mixed effects modeling
Characterization of circadian blood pressure patterns using non-linear mixed effects modeling Abstract Characterizing the time course of baseline or pre-drug blood pressure is important in acquiring unbiased estimates of antihypertensive drug effect. In this study, we recruited 23 healthy male volunteers and measured s...
PMC8241079
core_pubmed_pmc
Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance
Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance Abstract Abstract The purpose of the current study was to develop tizanidine HCl (TIZ; a myotonolytic agent used for treatment of spasticity) loaded nanotransfersomes intende...
PMC7854449
core_pubmed_pmc
Pharmacokinetics, Safety and Tolerability of Once-Weekly Subcutaneous Semaglutide in Healthy Chinese Subjects: A Double-Blind, Phase 1, Randomized Controlled Trial
Pharmacokinetics, Safety and Tolerability of Once-Weekly Subcutaneous Semaglutide in Healthy Chinese Subjects: A Double-Blind, Phase 1, Randomized Controlled Trial Abstract Abstract Introduction Once-weekly (OW) subcutaneous (s.c.) semaglutide is an injectable glucagon-like peptide-1 (GLP-1) analogue approved for the t...
PMC5811797
core_pubmed_pmc
Model‐Based Approach to Predict Adherence to Protocol During Antiobesity Trials
Model‐Based Approach to Predict Adherence to Protocol During Antiobesity Trials Abstract Abstract Development of antiobesity drugs is continuously challenged by high dropout rates during clinical trials. The objective was to develop a population pharmacodynamic model that describes the temporal changes in body weight, ...
PMC6842351
core_pubmed_pmc
Effect of Macitentan on the Pharmacokinetics of the Breast Cancer Resistance Protein Substrates, Rosuvastatin and Riociguat, in Healthy Male Subjects
Effect of Macitentan on the Pharmacokinetics of the Breast Cancer Resistance Protein Substrates, Rosuvastatin and Riociguat, in Healthy Male Subjects Abstract Background Macitentan is a clinically approved endothelin receptor antagonist for the treatment of pulmonary arterial hypertension (PAH). Increasing use of combi...
PMC10402254
core_pubmed_pmc
Single Protein Encapsulated SN38 for Tumor-Targeting Treatment
Single Protein Encapsulated SN38 for Tumor-Targeting Treatment Abstract Abstract Background The alkaloid camptothecin analog SN38 is a potent antineoplastic agent, but cannot be used directly for clinical application due to its poor water solubility. Currently, the prodrug approach on SN38 has resulted in 3 FDA-approve...
PMC10353071
core_pubmed_pmc
Levetiracetam Pharmacokinetics and Brain Uptake in a Lateral Fluid Percussion Injury Rat Model
Levetiracetam Pharmacokinetics and Brain Uptake in a Lateral Fluid Percussion Injury Rat Model Abstract Abstract Post-traumatic epilepsy (PTE) occurs in some patients after moderate/severe traumatic brain injury (TBI). Although there are no approved therapies to prevent epileptogenesis, levetiracetam (LEV) is commonly ...
PMC9259996
core_pubmed_pmc
Pulsatilla chinensis (Bge.) Regel: A Systematic Review on Anticancer of Its Pharmacological Properties, Clinical Researches and Pharmacokinetic Studies
Pulsatilla chinensis (Bge.) Regel: A Systematic Review on Anticancer of Its Pharmacological Properties, Clinical Researches and Pharmacokinetic Studies Abstract Pulsatilla chinensis (Bge.) Regel (PC) is one of the most commonly used Chinese medicines and has a history of thousands of years. This article reviews the res...
PMC6951913
core_pubmed_pmc
Comparing Model Performance in Characterizing the PK/PD of the Anti‐Myostatin Antibody Domagrozumab
Comparing Model Performance in Characterizing the PK/PD of the Anti‐Myostatin Antibody Domagrozumab Abstract Abstract Modeling and simulation provides quantitative information on target coverage for dose selection. Optimal model selection often relies on fit criteria and is not necessarily mechanistically driven. One s...
PMC6554663
core_pubmed_pmc
Pharmaceutical Effects of Inhibiting the Soluble Epoxide Hydrolase in Canine Osteoarthritis
Pharmaceutical Effects of Inhibiting the Soluble Epoxide Hydrolase in Canine Osteoarthritis Abstract Osteoarthritis (OA) is a degenerative joint disease that causes pain and bone deterioration driven by an increase in prostaglandins (PGs) and inflammatory cytokines. Current treatments focus on inhibiting prostaglandin ...
PMC4716581
core_pubmed_pmc
Pharmacokinetics of Anti‐VEGF Agent Aflibercept in Cancer Predicted by Data‐Driven, Molecular‐Detailed Model
Pharmacokinetics of Anti‐VEGF Agent Aflibercept in Cancer Predicted by Data‐Driven, Molecular‐Detailed Model Abstract Abstract Mathematical models can support the drug development process by predicting the pharmacokinetic (PK) properties of the drug and optimal dosing regimens. We have developed a pharmacokinetic model...
PMC12623632
core_pubmed_pmc
Exploring the Therapeutic Potential of Virtual Screened Novel HER2 Inhibitors via QSAR, Molecular Docking and Dynamics Simulations
Exploring the Therapeutic Potential of Virtual Screened Novel HER2 Inhibitors via QSAR, Molecular Docking and Dynamics Simulations Abstract Abstract Objectives HER2 overexpression is almost invariably associated with advanced breast cancer disease and poor prognosis, hence its extensive review. This study therefore aim...
PMC6044082
core_pubmed_pmc
Safety of lotilaner flavoured chewable tablets (Credelio TM ) after oral administration in cats
Safety of lotilaner flavoured chewable tablets (Credelio TM ) after oral administration in cats Abstract Background Lotilaner is a new member of the isoxazoline class for treatment of flea and tick infestations in cats. This laboratory study with lotilaner vanilla-yeast flavoured chewable tablets (Credelio TM , Elanco)...
PMC9241897
core_pubmed_pmc
Comparison of Ceftolozane/Tazobactam Infusion Regimens in a Hollow-Fiber Infection Model against Extensively Drug-Resistant Pseudomonas aeruginosa Isolates
Comparison of Ceftolozane/Tazobactam Infusion Regimens in a Hollow-Fiber Infection Model against Extensively Drug-Resistant Pseudomonas aeruginosa Isolates Abstract ABSTRACT The aim of this study was to compare the efficacy of intermittent (1-h), extended (4-h), and continuous ceftolozane-tazobactam (C/T) infusion agai...
PMC6005047
core_pubmed_pmc
Plasma and CSF pharmacokinetics of meropenem in neonates and young infants: results from the NeoMero studies
Plasma and CSF pharmacokinetics of meropenem in neonates and young infants: results from the NeoMero studies Abstract Abstract Background Sepsis and bacterial meningitis are major causes of mortality and morbidity in neonates and infants. Meropenem, a broad-spectrum antibiotic, is not licensed for use in neonates and i...
PMC7452990
core_pubmed_pmc
Pharmacists’ Knowledge About the Impact of Augmented Renal Clearance on Antimicrobial Dosing in Critically Ill Patients: A Cross-Sectional Study
Pharmacists’ Knowledge About the Impact of Augmented Renal Clearance on Antimicrobial Dosing in Critically Ill Patients: A Cross-Sectional Study Abstract Background Broad-spectrum antibiotics are commonly prescribed in critically ill patients. While it is commonly believed that only patients with impaired renal functio...
PMC10067675
core_pubmed_pmc
Leveraging in vitro and pharmacokinetic models to support bench to bedside investigation of XTMAB-16 as a novel pulmonary sarcoidosis treatment
Leveraging in vitro and pharmacokinetic models to support bench to bedside investigation of XTMAB-16 as a novel pulmonary sarcoidosis treatment Abstract Abstract Background: Sarcoidosis is a chronic, multisystem inflammatory disorder characterized by non-caseating epithelioid granulomas; infiltration of mononuclear cel...
PMC7275018
core_pubmed_pmc
A Phase II Randomized Trial to Explore the Potential for Pharmacokinetic Drug–Drug Interactions with Stiripentol or Valproate when Combined with Cannabidiol in Patients with Epilepsy
A Phase II Randomized Trial to Explore the Potential for Pharmacokinetic Drug–Drug Interactions with Stiripentol or Valproate when Combined with Cannabidiol in Patients with Epilepsy Abstract Abstract Background In recent randomized, placebo-controlled, phase III trials, highly purified cannabidiol demonstrated efficac...
PMC4928757
core_pubmed_pmc
Influence of Food on Paediatric Gastrointestinal Drug Absorption Following Oral Administration: A Review
Influence of Food on Paediatric Gastrointestinal Drug Absorption Following Oral Administration: A Review Abstract The objective of this paper was to review existing information regarding food effects on drug absorption within paediatric populations. Mechanisms that underpin food–drug interactions were examined to consi...
PMC11937411
core_pubmed_pmc
[ 18 F]FluorThanatrace PET imaging as a biomarker of response to PARP inhibitors in breast cancer
[ 18 F]FluorThanatrace PET imaging as a biomarker of response to PARP inhibitors in breast cancer Abstract Abstract Background Poly (ADP-ribose) polymerase inhibitors (PARPi) are approved for Breast Cancer gene ( BRCA )-mutant HER2- breast cancer, and there is clinical interest in expanding indications to include homol...
PMC12277848
core_pubmed_pmc
An overview of randomized phase III clinical trials of cancer nanomedicines
An overview of randomized phase III clinical trials of cancer nanomedicines Abstract Abstract Background Cancer therapy has undergone significant advances in recent decades attributed to personalized medicine and targeted drug delivery. Among the promising approaches, the use of nano-based delivery systems has become a...
PMC3781034
core_pubmed_pmc
A Small-Animal Pharmacokinetic/Pharmacodynamic PET Study of Central Serotonin 1A Receptor Occupancy by a Potential Therapeutic Agent for Overactive Bladder
A Small-Animal Pharmacokinetic/Pharmacodynamic PET Study of Central Serotonin 1A Receptor Occupancy by a Potential Therapeutic Agent for Overactive Bladder Abstract Serotonin 1A (5-HT 1A ) receptors have been mechanistically implicated in micturition control, and there has been a need for an appropriate biomarker surro...
PMC4291103
core_pubmed_pmc
Mathematical modeling of postmenopausal osteoporosis and its treatment by the anti-catabolic drug denosumab
Mathematical modeling of postmenopausal osteoporosis and its treatment by the anti-catabolic drug denosumab Abstract Abstract Denosumab, a fully human monoclonal antibody, has been approved for the treatment of postmenopausal osteoporosis. The therapeutic effect of denosumab rests on its ability to inhibit osteoclast d...
PMC7710212
core_pubmed_pmc
Controlled Delivery of Bile Acids to the Colon
Controlled Delivery of Bile Acids to the Colon Abstract Abstract INTRODUCTION: Bile acids, such as chenodeoxycholic acid, play an important role in digestion but are also involved in intestinal motility, fluid homeostasis, and humoral activity. Colonic delivery of sodium chenodeoxycholate (CDC) has demonstrated clinica...
PMC8456640
core_pubmed_pmc
Treatment of bipolar disorders in older adults: a review
Treatment of bipolar disorders in older adults: a review Abstract Abstract Background Old age bipolar disorder has been an orphan of psychiatric research for a long time despite the fact that bipolar disorder (BD)-I and II together may affect 0.5–1.0% of the elderly. It is also unclear whether aetiology, course of illn...
PMC9080097
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Identification of absorbed constituents and evaluation of the pharmacokinetics of main compounds after oral administration of yindanxinnaotong by UPLC-Q-TOF-MS and UPLC-QqQ-MS †
Identification of absorbed constituents and evaluation of the pharmacokinetics of main compounds after oral administration of yindanxinnaotong by UPLC-Q-TOF-MS and UPLC-QqQ-MS † Abstract Abstract Yindanxinnaotong capsule (YDXNT), a traditional Chinese formula, has been used to treat cardio-cerebrovascular diseases for ...
PMC9809135
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Graph theoretical network analysis, in silico exploration, and validation of bioactive compounds from Cynodon dactylon as potential neuroprotective agents against α-synuclein
Graph theoretical network analysis, in silico exploration, and validation of bioactive compounds from Cynodon dactylon as potential neuroprotective agents against α-synuclein Abstract Abstract Introduction: Parkinson's disease (PD) is a chronic, devastating neurodegenerative disorder marked by the death of dopaminergic...
PMC5423986
core_pubmed_pmc
Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years
Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years Abstract Purpose The aims of the study were to develop a population pharmacokinetic model of orally administered brivaracetam in paediatric patients and to provide dosing suggestions. Methods Analysis included 600 brivaracetam p...
PMC11877486
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Population pharmacokinetics of colistin sulfate in patients on continuous veno-venous hemodiafiltration
Population pharmacokinetics of colistin sulfate in patients on continuous veno-venous hemodiafiltration Abstract Abstract Objective The aim of this study is to establish a population pharmacokinetic (PK) model for patients undergoing continuous veno-venous hemodiafiltration (CVVHDF) and optimize the dosing regimen of c...
PMC4939706
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The triptolide derivative MRx102 inhibits Wnt pathway activation and has potent anti-tumor effects in lung cancer
The triptolide derivative MRx102 inhibits Wnt pathway activation and has potent anti-tumor effects in lung cancer Abstract Abstract Background The natural compound triptolide has been shown to decrease cell proliferation and induce apoptosis and cellular senescence. We previously demonstrated that triptolide decreases ...
PMC8979112
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Exploration of Q-Marker of Rhubarb Based on Intelligent Data Processing Techniques and the AUC Pooled Method
Exploration of Q-Marker of Rhubarb Based on Intelligent Data Processing Techniques and the AUC Pooled Method Abstract Abstract Rhubarb, as a traditional Chinese medicine, has several positive therapeutic effects, such as purging and attacking accumulation, clearing heat and purging fire, cooling blood, and detoxificati...
PMC5444187
core_pubmed_pmc
Impact of Mucositis on Absorption and Systemic Drug Exposure of Isavuconazole
Impact of Mucositis on Absorption and Systemic Drug Exposure of Isavuconazole Abstract ABSTRACT Isavuconazonium sulfate is the water-soluble prodrug of isavuconazole. Population analyses have demonstrated relatively predictable pharmacokinetic (PK) behavior in diverse patient populations. We evaluated the impact of muc...
PMC9054865
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PDI inhibitor LTI6426 enhances panobinostat efficacy in preclinical models of multiple myeloma
PDI inhibitor LTI6426 enhances panobinostat efficacy in preclinical models of multiple myeloma Abstract Abstract The histone deacetylase inhibitor (HDACi), panobinostat (Pano), is approved by the United States Food and Drug Administration (FDA) and European Medicines Agency (EMA) for treatment of relapsed/refractory mu...
PMC8571351
core_pubmed_pmc
SCO-267, a GPR40 Full Agonist, Stimulates Islet and Gut Hormone Secretion and Improves Glycemic Control in Humans
SCO-267, a GPR40 Full Agonist, Stimulates Islet and Gut Hormone Secretion and Improves Glycemic Control in Humans Abstract Abstract SCO-267 is a full agonist of the free fatty acid receptor 1 (GPR40), which regulates the secretion of islet and gut hormones. In this phase 1 study, we aimed to evaluate the clinical profi...
PMC10911225
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MSG-15: Super-Bioavailability Itraconazole Versus Conventional Itraconazole in the Treatment of Endemic Mycoses—A Multicenter, Open-Label, Randomized Comparative Trial
MSG-15: Super-Bioavailability Itraconazole Versus Conventional Itraconazole in the Treatment of Endemic Mycoses—A Multicenter, Open-Label, Randomized Comparative Trial Abstract Abstract Background Invasive fungal disease caused by dimorphic fungi is associated with significant morbidity and mortality. Super-bioavailabi...
PMC11456355
core_pubmed_pmc
Obicetrapib as an Adjunct to Stable Statin Therapy in Japanese Subjects: Results from a Randomized Phase 2 Trial
Obicetrapib as an Adjunct to Stable Statin Therapy in Japanese Subjects: Results from a Randomized Phase 2 Trial Abstract Aims: Obicetrapib is a highly selective cholesteryl ester transfer protein (CETP) inhibitor shown to reduce low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B (apoB), when taken as mon...
PMC9363195
core_pubmed_pmc
Preclinical Pharmacokinetics, Biodistribution, and Acute Toxicity Evaluation of Caerin 1.9 Peptide in Sprague Dawley Rats
Preclinical Pharmacokinetics, Biodistribution, and Acute Toxicity Evaluation of Caerin 1.9 Peptide in Sprague Dawley Rats Abstract Caerin 1.9 is a natural peptide derived from the skin secretions of the Australian tree frog ( Litoria ) with broad-spectrum antimicrobial and anticancer bioactivity. It improves the effica...
PMC5853094
core_pubmed_pmc
Differential impact of diabetes mellitus on antiplatelet effects of prasugrel and clopidogrel
Differential impact of diabetes mellitus on antiplatelet effects of prasugrel and clopidogrel Abstract Background Although prasugrel exerts stronger antiplatelet effects compared with clopidogrel, the factors affecting platelet reactivity under prasugrel have not been fully determined. This study aimed to find the nove...
PMC11535547
core_pubmed_pmc
Multiscale, mechanistic model of Rheumatoid Arthritis to enable decision making in late stage drug development
Multiscale, mechanistic model of Rheumatoid Arthritis to enable decision making in late stage drug development Abstract Abstract Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects about 0.1% to 2% of the population worldwide. Despite the development of several novel therapies, there is ...
PMC10146624
core_pubmed_pmc
In Vitro–In Vivo Correlation of Posaconazole–Amphotericin B Combination against Candida albicans : In Vitro Interacting Concentrations Are Associated with In Vivo Free Drug Levels
In Vitro–In Vivo Correlation of Posaconazole–Amphotericin B Combination against Candida albicans : In Vitro Interacting Concentrations Are Associated with In Vivo Free Drug Levels Abstract The in vitro/in vivo correlation of antifungal combination testing is necessary in order to assess the efficacy of combination regi...
PMC10777847
core_pubmed_pmc
A phase I, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study of the pharmacokinetics, safety, and tolerability of oral ceftibuten in healthy adult subjects
A phase I, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study of the pharmacokinetics, safety, and tolerability of oral ceftibuten in healthy adult subjects Abstract ABSTRACT This was a phase I, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study ...
PMC10107600
core_pubmed_pmc
Quantifying Antibody Persistence After a Single Dose of COVID ‐19 Vaccine Ad26. COV2 .S in Humans Using a Mechanistic Modeling and Simulation Approach
Quantifying Antibody Persistence After a Single Dose of COVID ‐19 Vaccine Ad26. COV2 .S in Humans Using a Mechanistic Modeling and Simulation Approach Abstract Understanding persistence of humoral immune responses elicited by vaccination against coronavirus disease 2019 (COVID‐19) is critical for informing the duration...
PMC8135237
core_pubmed_pmc
Nonclinical Development of SRK-181: An Anti-Latent TGFβ1 Monoclonal Antibody for the Treatment of Locally Advanced or Metastatic Solid Tumors
Nonclinical Development of SRK-181: An Anti-Latent TGFβ1 Monoclonal Antibody for the Treatment of Locally Advanced or Metastatic Solid Tumors Abstract Checkpoint inhibitors offer a promising immunotherapy strategy for cancer treatment; however, due to primary or acquired resistance, many patients do not achieve lasting...
PMC11350760
core_pubmed_pmc
Association between Extended Meropenem Regimen and Achievement of Aggressive PK/PD in Patients Receiving Continuous Renal Replacement Therapy for Septic AKI
Association between Extended Meropenem Regimen and Achievement of Aggressive PK/PD in Patients Receiving Continuous Renal Replacement Therapy for Septic AKI Abstract Aggressive pharmacokinetic (PK)/pharmacodynamic (PD) targets have shown better microbiological eradication rates and a lower propensity to develop resista...
PMC12766356
core_pubmed_pmc
Iptacopan for Immune Thrombocytopenia and Cold Agglutinin Disease: A Global Phase 2 Basket Clinical Trial
Iptacopan for Immune Thrombocytopenia and Cold Agglutinin Disease: A Global Phase 2 Basket Clinical Trial Abstract ABSTRACT Iptacopan is a first‐in‐class, oral, selective inhibitor of complement factor B that has demonstrated positive efficacy across several complement‐driven diseases. Here we evaluate the efficacy and...
PMC8911314
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of YYD601, a Dual Delayed-Release Formulation of Esomeprazole, Following Single and Multiple Doses in Healthy Adult Volunteers Under Fasting and Fed Conditions
Pharmacokinetics and Pharmacodynamics of YYD601, a Dual Delayed-Release Formulation of Esomeprazole, Following Single and Multiple Doses in Healthy Adult Volunteers Under Fasting and Fed Conditions Abstract Abstract Background YYD601 was developed as a novel dual delayed release (DDR) formulation of esomeprazole to pro...
PMC4809456
core_pubmed_pmc
PBPK Model for Atrazine and Its Chlorotriazine Metabolites in Rat and Human
PBPK Model for Atrazine and Its Chlorotriazine Metabolites in Rat and Human Abstract Abstract The previously-published physiologically based pharmacokinetic model for atrazine (ATZ), deisopropylatrazine (DIA), deethylatrazine (DEA), and diaminochlorotriazine (DACT), which collectively comprise the total chlorotriazines...
PMC3868110
core_pubmed_pmc
Dexmedetomidine: An Adjuvant Making Large Inroads into Clinical Practice
Dexmedetomidine: An Adjuvant Making Large Inroads into Clinical Practice Abstract Abstract The introduction of newer more selective α −2 adrenergic agonist, dexmedetomidine has made a revolution in the field of anesthesia owing to its varied application. The aim of the current review is to highlight the various clinica...
PMC4289211
core_pubmed_pmc
How do we use therapeutic drug monitoring to improve outcomes from severe infections in critically ill patients?
How do we use therapeutic drug monitoring to improve outcomes from severe infections in critically ill patients? Abstract Abstract High mortality and morbidity rates associated with severe infections in the critically ill continue to be a significant issue for the healthcare system. In view of the diverse and unique ph...
PMC6670186
core_pubmed_pmc
Novel prodrugs of decitabine with greater metabolic stability and less toxicity
Novel prodrugs of decitabine with greater metabolic stability and less toxicity Abstract Background DNA demethylation therapy is now used in practice for hematological tumors and is being developed for solid tumors. Nevertheless, it is difficult to achieve stable pharmacokinetics with the current DNA-demethylating agen...
PMC11955805
core_pubmed_pmc
A First‐In‐Human Phase 1 Study to Evaluate the Safety and Tolerability of LEM ‐ S401 , a Novel siRNA ‐ DegradaBALL Drug Targeting CTGF in Healthy Adults
A First‐In‐Human Phase 1 Study to Evaluate the Safety and Tolerability of LEM ‐ S401 , a Novel siRNA ‐ DegradaBALL Drug Targeting CTGF in Healthy Adults Abstract ABSTRACT This study evaluated the safety, tolerability, and pharmacokinetics of LEM‐S401, a novel siRNA therapeutic with DegradaBALL, a mesoporous silica nano...
PMC11492252
core_pubmed_pmc
Molecular modelling and antimicrobial activity of newly synthesized benzothiazolo[3,2- a ]pyrimidine clubbed thiazole derivatives
Molecular modelling and antimicrobial activity of newly synthesized benzothiazolo[3,2- a ]pyrimidine clubbed thiazole derivatives Abstract Abstract A series of benzothiazolopyrimidine-thiazole conjugates 7 , 8 , and 9 were produced through the reactions of 8-acetylbenzothiazolopyrimidine-thiosemicarbazone compound 6 wi...
PMC8653950
core_pubmed_pmc
3D Bioprinting Strategies, Challenges, and Opportunities to Model the Lung Tissue Microenvironment and Its Function
3D Bioprinting Strategies, Challenges, and Opportunities to Model the Lung Tissue Microenvironment and Its Function Abstract Abstract Human lungs are organs with an intricate hierarchical structure and complex composition; lungs also present heterogeneous mechanical properties that impose dynamic stress on different ti...
PMC11812944
core_pubmed_pmc
Quantitative pharmacology of dual‐targeted bicistronic CAR‐T‐cell therapy using multiscale mechanistic modeling
Quantitative pharmacology of dual‐targeted bicistronic CAR‐T‐cell therapy using multiscale mechanistic modeling Abstract Abstract Despite the initial success of single‐targeted chimeric‐antigen receptor (CAR) T‐cell therapy in hematological malignancies, its long‐term effectiveness is often hindered by antigen heteroge...
PMC9813072
core_pubmed_pmc
Comparison of pharmacokinetics, pharmacodynamics, safety, and immunogenicity of teriparatide biosimilar with EU- and US-approved teriparatide reference products in healthy men and postmenopausal women
Comparison of pharmacokinetics, pharmacodynamics, safety, and immunogenicity of teriparatide biosimilar with EU- and US-approved teriparatide reference products in healthy men and postmenopausal women Abstract Abstract Summary Biosimilar teriparatide (INTG-8) was tested in a healthy population of males and postmenopaus...
PMC6540077
core_pubmed_pmc
Sustained delivery of a camptothecin prodrug – CZ48 by nanosuspensions with improved pharmacokinetics and enhanced anticancer activity
Sustained delivery of a camptothecin prodrug – CZ48 by nanosuspensions with improved pharmacokinetics and enhanced anticancer activity Abstract Background and aim: We have synthesized a novel lactone-stabilized camptothecin (CPT) analog named CZ48 and demonstrated its potent anticancer effects via bioconversion to the ...
PMC5069450
core_pubmed_pmc
Effects of Food Intake on the Pharmacokinetics of Azilsartan Medoxomil and Chlorthalidone Alone and in Fixed‐Dose Combination in Healthy Adults
Effects of Food Intake on the Pharmacokinetics of Azilsartan Medoxomil and Chlorthalidone Alone and in Fixed‐Dose Combination in Healthy Adults Abstract Abstract Azilsartan medoxomil is a long‐acting angiotensin II receptor blocker used to treat hypertension as monotherapy or in fixed‐dose combination (FDC) with chlort...
PMC7862213
core_pubmed_pmc
Model-Informed Precision Dosing of Everolimus: External Validation in Adult Renal Transplant Recipients
Model-Informed Precision Dosing of Everolimus: External Validation in Adult Renal Transplant Recipients Abstract Abstract Background and Objective The immunosuppressant everolimus is increasingly applied in renal transplantation. Its extensive pharmacokinetic variability necessitates therapeutic drug monitoring, typica...
PMC8941354
core_pubmed_pmc
Site of Alcohol First-Pass Metabolism Among Women
Site of Alcohol First-Pass Metabolism Among Women Methods Methods This cross-sectional study included 12 women who had SG surgery within the past 5 years at Carle Foundation Hospital (CFH) in Urbana, Illinois, and 9 women who did not undergo surgery and had equivalent age, body max index, and alcohol drinking patterns ...
PMC4265066
core_pubmed_pmc
Adjuvant therapies for HIV-associated neurocognitive disorders
Adjuvant therapies for HIV-associated neurocognitive disorders Abstract Abstract Objective HIV-associated neurocognitive disorder (HAND) is a frequent and heterogeneous complication of HIV, affecting nearly 50% of infected individuals in the combined antiretroviral therapy (cART) era. This is a particularly devastating...
PMC2879225
core_pubmed_pmc
Elevated Serum Sorbitol and not Fructose in Type 2 Diabetic Patients
Elevated Serum Sorbitol and not Fructose in Type 2 Diabetic Patients Abstract Abstract Reductions in fasting serum fructose or erythrocyte sorbitol have been proposed as markers for early proof of mechanism in clinical development of aldose reductase (AR) inhibitors. However fructose is significantly impacted by meals ...
PMC4449373
core_pubmed_pmc
Comparable Liraglutide Pharmacokinetics in Pediatric and Adult Populations with Type 2 Diabetes: A Population Pharmacokinetic Analysis
Comparable Liraglutide Pharmacokinetics in Pediatric and Adult Populations with Type 2 Diabetes: A Population Pharmacokinetic Analysis Abstract Background and Objective The safety, tolerability, and pharmacokinetics of the once-daily human glucagon-like peptide-1 (GLP-1) analog liraglutide have been evaluated in pediat...
PMC8809194
core_pubmed_pmc
Standard ganciclovir dosing results in slow decline of cytomegalovirus viral loads
Standard ganciclovir dosing results in slow decline of cytomegalovirus viral loads Abstract Abstract Background Cytomegalovirus (CMV) can cause severe disease, including rejection in transplant recipients. Ganciclovir and its oral prodrug valganciclovir have been used as first-line therapy for CMV disease in transplant...
PMC5032984
core_pubmed_pmc
Effects of luseogliflozin, a sodium–glucose co‐transporter 2 inhibitor, on 24‐h glucose variability assessed by continuous glucose monitoring in Japanese patients with type 2 diabetes mellitus: a randomized, double‐blind, placebo‐controlled, crossover study
Effects of luseogliflozin, a sodium–glucose co‐transporter 2 inhibitor, on 24‐h glucose variability assessed by continuous glucose monitoring in Japanese patients with type 2 diabetes mellitus: a randomized, double‐blind, placebo‐controlled, crossover study Abstract Abstract The aim of the present study was to determin...
PMC12351365
core_pubmed_pmc
Development of a Novel Immunoprecipitation Method for Extracting Monoclonal Antibodies From Brain Tissue and Its Application to Assessing In Vivo Brain Penetration in Mouse via Liquid Chromatography–Mass Spectrometry
Development of a Novel Immunoprecipitation Method for Extracting Monoclonal Antibodies From Brain Tissue and Its Application to Assessing In Vivo Brain Penetration in Mouse via Liquid Chromatography–Mass Spectrometry Abstract ABSTRACT A novel extraction method was developed to quantify monoclonal antibodies from brain ...
PMC7523758
core_pubmed_pmc
A Phase 2 Study of Nivolumab Using a Fixed Dose of 40 mg (Nivo40) in Patients With Relapsed/Refractory Hodgkin Lymphoma
A Phase 2 Study of Nivolumab Using a Fixed Dose of 40 mg (Nivo40) in Patients With Relapsed/Refractory Hodgkin Lymphoma Abstract Supplemental Digital Content is available in the text Abstract The introduction of nivolumab has changed the landscape of relapsed/refractory classical Hodgkin lymphoma (r/r cHL) treatment. D...
PMC12709605
core_pubmed_pmc
Biliary pharmacokinetic/pharmacodynamic analysis of continuous infusion meropenem/vaborbactam in a case series of orthotopic liver transplant recipients
Biliary pharmacokinetic/pharmacodynamic analysis of continuous infusion meropenem/vaborbactam in a case series of orthotopic liver transplant recipients Abstract Abstract Objective To analyse the biliary pharmacokinetics/pharmacodynamics (PK/PD) of continuous infusion (CI) meropenem-vaborbactam (MEM-VBM) in a case seri...
PMC11204421
core_pubmed_pmc
Antimicrobial Pharmacokinetic Considerations in Extracorporeal Membrane Oxygenation
Antimicrobial Pharmacokinetic Considerations in Extracorporeal Membrane Oxygenation Abstract Abstract Critical illness creates challenges for healthcare providers in determining the optimal treatment of severe disease, particularly in determining the most appropriate selection and dosing of medications. Critically ill ...
PMC8359310
core_pubmed_pmc
Effect of capmatinib on the pharmacokinetics of digoxin and rosuvastatin administered as a 2‐drug cocktail in patients with MET ‐dysregulated advanced solid tumours: A phase I, multicentre, open‐label, single‐sequence drug–drug interaction study
Effect of capmatinib on the pharmacokinetics of digoxin and rosuvastatin administered as a 2‐drug cocktail in patients with MET ‐dysregulated advanced solid tumours: A phase I, multicentre, open‐label, single‐sequence drug–drug interaction study Abstract Abstract Aims Capmatinib, an orally bioavailable, highly potent a...