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PMC4224420
core_pubmed_pmc
Unsupervised Deconvolution of Dynamic Imaging Reveals Intratumor Vascular Heterogeneity and Repopulation Dynamics
Unsupervised Deconvolution of Dynamic Imaging Reveals Intratumor Vascular Heterogeneity and Repopulation Dynamics Abstract With the existence of biologically distinctive malignant cells originated within the same tumor, intratumor functional heterogeneity is present in many cancers and is often manifested by the interm...
PMC7469251
core_pubmed_pmc
Gestational Age–Dependent Abundance of Human Placental Transporters as Determined by Quantitative Targeted Proteomics
Gestational Age–Dependent Abundance of Human Placental Transporters as Determined by Quantitative Targeted Proteomics Abstract Abstract Some women take medication during pregnancy to address a variety of clinical conditions. Because of ethical and logistical concerns, it is impossible to determine fetal drug exposure, ...
PMC3289390
core_pubmed_pmc
Ginsenosides as Anticancer Agents: In vitro and in vivo Activities, Structure–Activity Relationships, and Molecular Mechanisms of Action
Ginsenosides as Anticancer Agents: In vitro and in vivo Activities, Structure–Activity Relationships, and Molecular Mechanisms of Action Abstract Abstract Conventional chemotherapeutic agents are often toxic not only to tumor cells but also to normal cells, limiting their therapeutic use in the clinic. Novel natural pr...
PMC4467237
core_pubmed_pmc
Effects of Ketoconazole on the Pharmacokinetics of Lenvatinib (E7080) in Healthy Participants
Effects of Ketoconazole on the Pharmacokinetics of Lenvatinib (E7080) in Healthy Participants Abstract Background Lenvatinib is an oral, multitargeted, tyrosine kinase inhibitor under clinical investigation in solid tumors. In vitro evidence indicates that lenvatinib metabolism may be modulated by ketoconazole, an inhi...
PMC10059125
core_pubmed_pmc
The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics Abstract Abstract Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless...
PMC12888862
core_pubmed_pmc
An alveolar macrophage-targeted ciprofloxacin polymeric prodrug improves survival in a murine model of Klebsiella pneumoniae pneumonia
An alveolar macrophage-targeted ciprofloxacin polymeric prodrug improves survival in a murine model of Klebsiella pneumoniae pneumonia Abstract ABSTRACT Klebsiella pneumoniae is a leading cause of both hospital- and community-acquired pneumonia. Nanomaterials have the potential to deliver antibiotics directly to sites ...
PMC11451978
core_pubmed_pmc
Enhanced quantitation of pathological α-synuclein in patient biospecimens by RT-QuIC seed amplification assays
Enhanced quantitation of pathological α-synuclein in patient biospecimens by RT-QuIC seed amplification assays Abstract Abstract Disease associated pathological aggregates of alpha-synuclein (αSyn D ) exhibit prion-like spreading in synucleinopathies such as Parkinson’s disease (PD) and dementia with Lewy bodies (DLB)....
PMC11170845
core_pubmed_pmc
Population pharmacokinetics and dose optimization of magnesium sulfate in Chinese preeclampsia population
Population pharmacokinetics and dose optimization of magnesium sulfate in Chinese preeclampsia population Abstract Abstract Objective To establish the population pharmacokinetics (PPK) of magnesium sulfate (MgSO 4 )in women with preeclampsia (PE), and to determine the key covariates having an effect in magnesium pharma...
PMC5473410
core_pubmed_pmc
Dose Titration Algorithm Tuning (DTAT) should supersede ‘the’ Maximum Tolerated Dose (MTD) in oncology dose-finding trials
Dose Titration Algorithm Tuning (DTAT) should supersede ‘the’ Maximum Tolerated Dose (MTD) in oncology dose-finding trials Abstract Background . Absent adaptive, individualized dose-finding in early-phase oncology trials, subsequent ‘confirmatory’ Phase III trials risk suboptimal dosing, with resulting loss of statisti...
PMC12027173
core_pubmed_pmc
Pharmacogenomic and Pharmacomicrobiomic Aspects of Drugs of Abuse
Pharmacogenomic and Pharmacomicrobiomic Aspects of Drugs of Abuse Abstract Background/Objectives: This review examines the role of pharmacogenomics in individual responses to the pharmacotherapy of various drugs of abuse, including alcohol, cocaine, and opioids, to identify genetic variants that contribute to variabili...
PMC7414100
core_pubmed_pmc
Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo
Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo Abstract The present study involves the development of Dipivefrin hydrochloride (DV) containing Poloxamers (P407 and P188)-Carbopol-934 (CP) based thermoresponsive-gels ...
PMC7138916
core_pubmed_pmc
Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats
Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats Abstract Abstract In clinical pharmacology, the free drug hypothesis has been widely applied in the interpretation of the relationship between pharmacokinetics and pha...
PMC5973995
core_pubmed_pmc
Vortioxetine: Clinical Pharmacokinetics and Drug Interactions
Vortioxetine: Clinical Pharmacokinetics and Drug Interactions Abstract Abstract Vortioxetine is a novel antidepressant with multimodal activity currently approved for the treatment of major depressive disorder. Vortioxetine is orally administered once daily at 5- to 20-mg doses. The pharmacokinetics of vortioxetine are...
PMC9636444
core_pubmed_pmc
Safety of sildenafil in premature infants at risk of bronchopulmonary dysplasia: Rationale and methods of a phase II randomized trial
Safety of sildenafil in premature infants at risk of bronchopulmonary dysplasia: Rationale and methods of a phase II randomized trial Abstract Abstract Bronchopulmonary dysplasia (BPD) is a disease of chronic respiratory insufficiency stemming from premature birth and iatrogenic lung injury leading to alveolar simplifi...
PMC8604880
core_pubmed_pmc
Minimal brain PBPK model to support the preclinical and clinical development of antibody therapeutics for CNS diseases
Minimal brain PBPK model to support the preclinical and clinical development of antibody therapeutics for CNS diseases Abstract There are several antibody therapeutics in preclinical and clinical development, industry-wide, for the treatment of central nervous system (CNS) disorders. Due to the limited permeability of ...
PMC12443583
core_pubmed_pmc
Defactinib with avutometinib in patients with solid tumors: the phase 1 FRAME trial
Defactinib with avutometinib in patients with solid tumors: the phase 1 FRAME trial Abstract Use of signal transduction inhibitors as single agents to treat cancer leads to resistance because of the plasticity of intracellular signaling, and combination therapy can overcome this. We describe the first-in-human trial of...
PMC12481485
core_pubmed_pmc
Development of Optimized Exatecan-Based Immunoconjugates with Potent Antitumor Efficacy in HER2-Positive Breast Cancer
Development of Optimized Exatecan-Based Immunoconjugates with Potent Antitumor Efficacy in HER2-Positive Breast Cancer Abstract The prognosis of human epidermal growth factor receptor 2 (HER2)-positive breast cancer has significantly improved with the advent of anti-HER2 therapies, especially antibody-drug conjugates (...
PMC3884839
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics utilizing unbound target tissue exposure as part of a disposition-based rationale for lead optimization of benzoxaboroles in the treatment of Stage 2 Human African Trypanosomiasis
Pharmacokinetics and pharmacodynamics utilizing unbound target tissue exposure as part of a disposition-based rationale for lead optimization of benzoxaboroles in the treatment of Stage 2 Human African Trypanosomiasis Abstract SUMMARY This review presents a progression strategy for the discovery of new anti-parasitic d...
PMC10822116
core_pubmed_pmc
In vitro and in vivo Biological Evaluation of Newly Tacrine-Selegiline Hybrids as Multi-Target Inhibitors of Cholinesterases and Monoamine Oxidases for Alzheimer’s Disease
In vitro and in vivo Biological Evaluation of Newly Tacrine-Selegiline Hybrids as Multi-Target Inhibitors of Cholinesterases and Monoamine Oxidases for Alzheimer’s Disease Abstract Purpose Alzheimer’s disease (AD) is the most common neurodegenerative disease, and its multifactorial nature increases the difficulty of me...
PMC9205434
core_pubmed_pmc
In vitro Antibacterial Activity and Resistance Prevention of Antimicrobial Combinations for Dihydropteroate Synthase-Carrying Stenotrophomonas maltophilia
In vitro Antibacterial Activity and Resistance Prevention of Antimicrobial Combinations for Dihydropteroate Synthase-Carrying Stenotrophomonas maltophilia Abstract Abstract Background Stenotrophomonas maltophilia ( S. maltophilia ) is a multidrug-resistant gram-negative bacillus that is known to be an opportunistic pat...
PMC12847419
core_pubmed_pmc
Population pharmacokinetics of imipenem in different populations for individualized dosing: a systematic review
Population pharmacokinetics of imipenem in different populations for individualized dosing: a systematic review Abstract Abstract Background Imipenem is a broad-spectrum carbapenem antibiotic for severe infections with significant pharmacokinetic (PK) variability. This review systematically synthesized published popula...
PMC4875921
core_pubmed_pmc
Characterisation of Population Pharmacokinetics and Endogenous Follicle-Stimulating Hormone (FSH) Levels After Multiple Dosing of a Recombinant Human FSH (FE 999049) in Healthy Women
Characterisation of Population Pharmacokinetics and Endogenous Follicle-Stimulating Hormone (FSH) Levels After Multiple Dosing of a Recombinant Human FSH (FE 999049) in Healthy Women Abstract Abstract Objective The aim of this study was to characterise the population pharmacokinetics of FE 999049, a novel recombinant h...
PMC12660502
core_pubmed_pmc
Intratympanic dexamethasone microcrystals/lidocaine‐loaded PLGA non‐spherical microparticles for local drug delivery to the inner ear
Intratympanic dexamethasone microcrystals/lidocaine‐loaded PLGA non‐spherical microparticles for local drug delivery to the inner ear Abstract Abstract Background Sudden sensorineural hearing loss (SSNHL), often associated with tinnitus, significantly impacts individuals' quality of life. Current treatments, such as fr...
PMC5064742
core_pubmed_pmc
Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [ 13 C 8 ]‐evacetrapib as a tracer
Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [ 13 C 8 ]‐evacetrapib as a tracer Abstract This open‐label, single‐period study in healthy subjects estimated evacetrapib absolute bioavailability following simultaneous administrat...
PMC11755472
core_pubmed_pmc
The Pharmacokinetic Changes in Cystic Fibrosis Patients Population: Narrative Review
The Pharmacokinetic Changes in Cystic Fibrosis Patients Population: Narrative Review Abstract Abstract Cystic fibrosis (CF) is a rare genetic disorder commonly affecting multiple organs such as the lungs, pancreas, liver, kidney, and intestine. Our search focuses on the pathophysiological changes that affect the drugs’...
PMC10683027
core_pubmed_pmc
Discovery of tert -Butyl Ester Based 6-Diazo-5-oxo- l -norleucine Prodrugs for Enhanced Metabolic Stability and Tumor Delivery
Discovery of tert -Butyl Ester Based 6-Diazo-5-oxo- l -norleucine Prodrugs for Enhanced Metabolic Stability and Tumor Delivery Abstract The glutamine antagonist 6-diazo-5-oxo- l -norleucine (DON) exhibits remarkable anticancer efficacy; however, its therapeutic potential is hindered by its toxicity to gastrointestinal ...
PMC8965223
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of repeat dosing of gabapentin in adult horses
Pharmacokinetics and pharmacodynamics of repeat dosing of gabapentin in adult horses Abstract Abstract Background The repeated administration of high doses of gabapentin may provide better analgesia in horses than current clinical protocols. Hypothesis and Objectives Administration of gabapentin at 40 and 120 mg/kg PO ...
PMC5934980
core_pubmed_pmc
Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets
Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets Abstract Abstract Multidrug binding and transport by the ATP-binding cassette transporter ABCG2 is a factor in the clinical resistance to chemotherapy in leukaemia, and a contributory factor to the pharmacokinetic profiles o...
PMC12618412
core_pubmed_pmc
Population Pharmacokinetic Analysis of Balcinrenone in Healthy Participants and Participants with Heart Failure and Chronic Kidney Disease
Population Pharmacokinetic Analysis of Balcinrenone in Healthy Participants and Participants with Heart Failure and Chronic Kidney Disease Abstract Abstract Background and Objective Balcinrenone is a novel mineralocorticoid receptor modulator which, based on preclinical data, maintains cardio-renal benefits without inc...
PMC12856346
core_pubmed_pmc
Long-term follow-up of zevor-cel in patients with relapsed/refractory multiple myeloma ∗
Long-term follow-up of zevor-cel in patients with relapsed/refractory multiple myeloma ∗ Abstract Key Points • At ∼5-year follow-up, objective response rate with zevor-cel was 100%, and 78.6% patients achieved complete or better response. • No grade ≥3 cytokine release syndrome, grade ≥3 neurotoxicity, or other delayed...
PMC12621395
core_pubmed_pmc
Analgesic and sedative drug dosing in critically ill patients with Acute Kidney Injury undergoing different modalities of Kidney Replacement Therapy
Analgesic and sedative drug dosing in critically ill patients with Acute Kidney Injury undergoing different modalities of Kidney Replacement Therapy Abstract Critically ill patients frequently require analgesic and sedative medications to manage pain, agitation, and the stress associated with their condition. The onset...
PMC11489133
core_pubmed_pmc
Obicetrapib exhibits favorable physiochemical and pharmacokinetic properties compared to previous cholesteryl ester transfer protein inhibitors: An integrated summary of results from non‐human primate studies and clinical trials
Obicetrapib exhibits favorable physiochemical and pharmacokinetic properties compared to previous cholesteryl ester transfer protein inhibitors: An integrated summary of results from non‐human primate studies and clinical trials Abstract Abstract Anacetrapib, a cholesteryl ester transfer protein (CETP) inhibitor previo...
PMC11771128
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of ciprofol after continuous infusion in elderly patients
Pharmacokinetics and pharmacodynamics of ciprofol after continuous infusion in elderly patients Abstract Abstract Background Ciprofol, a novel intravenous anesthetic, which has primarily been used for the induction and maintenance of general anesthesia in adults, is characterized by rapid onset, short duration of actio...
PMC4232039
core_pubmed_pmc
Early non-steady-state population pharmacokinetics of oral cyclosporine in renal transplant recipients
Early non-steady-state population pharmacokinetics of oral cyclosporine in renal transplant recipients Abstract Abstract This study aimed to evaluate the change in the pharmacokinetics (PK) of cyclosporine in the non-steady-state period in the first week after renal transplantation; the factors influencing this change,...
PMC8240971
core_pubmed_pmc
Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo , bio-distribution and in vivo pharmacokinetic studies
Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo , bio-distribution and in vivo pharmacokinetic studies Abstract Abstract Being one of the highly effective drugs in treatment of Alzheimer’s disease, Rivastigmine brain targeting is highly demandable, therefo...
PMC11771590
core_pubmed_pmc
Time Course of Reversal of Fentanyl‐Induced Respiratory Depression in Healthy Subjects by Intramuscular Nalmefene and Intramuscular and Intranasal Naloxone
Time Course of Reversal of Fentanyl‐Induced Respiratory Depression in Healthy Subjects by Intramuscular Nalmefene and Intramuscular and Intranasal Naloxone Abstract Abstract The increase in opioid overdose deaths, particularly involving potent, long‐acting synthetic opioids, has led to calls for stronger, longer‐acting...
PMC6260118
core_pubmed_pmc
Single-dose ciraparantag safely and completely reverses anticoagulant effects of edoxaban
Single-dose ciraparantag safely and completely reverses anticoagulant effects of edoxaban Abstract Summary Of the new direct oral anticoagulants, direct factor Xa inhibitors are limited by the absence of a proven reversal agent. We assessed the safety, tolerability and impact on anticoagulation reversal of ciraparantag...
PMC6890626
core_pubmed_pmc
Are Standard Doses of Renally-Excreted Antiretrovirals in Older Patients Appropriate: A PBPK Study Comparing Exposures in the Elderly Population With Those in Renal Impairment
Are Standard Doses of Renally-Excreted Antiretrovirals in Older Patients Appropriate: A PBPK Study Comparing Exposures in the Elderly Population With Those in Renal Impairment Abstract Abstract Background and Objectives The elderly population receives the majority of prescription drugs but are usually excluded from Pha...
PMC12408551
core_pubmed_pmc
From a traditional medicine monomer to a modern neurotherapeutic scaffold: a review of SAR-Driven tetramethylpyrazine derivatives for cerebrovascular and cognitive health
From a traditional medicine monomer to a modern neurotherapeutic scaffold: a review of SAR-Driven tetramethylpyrazine derivatives for cerebrovascular and cognitive health Abstract Abstract Tetramethylpyrazine (TMP), a bioactive alkaloid isolated from the traditional Chinese medicine Ligusticum wallichii ( Chuanxiong) ,...
PMC6720094
core_pubmed_pmc
Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats
Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats Abstract Background Oxyresveratrol is a major bioactive component derived from the heartwood of Artocarpus lacucha . This compound exerts several biological activities, including neuroprotective effects in vit...
PMC8648015
core_pubmed_pmc
Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles
Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles Abstract Abstract Context As an inhibitor cytochrome P450 family 2 subfamily C polypeptide 8 (CYP2C8), quercetin is a naturally occurring flavonoid with its glycosides consumed at least 100 mg per day in food. However, it is s...
PMC10912040
core_pubmed_pmc
CD19-CAR-DNT cells (RJMty19) in patients with relapsed or refractory large B-cell lymphoma: a phase 1, first-in-human study
CD19-CAR-DNT cells (RJMty19) in patients with relapsed or refractory large B-cell lymphoma: a phase 1, first-in-human study Abstract Summary Background Current approved chimeric antigen receptor (CAR) T-cell products are autologous cell therapies that are costly and poorly accessible to patients. We aimed to evaluate t...
PMC4345959
core_pubmed_pmc
Efficacy and safety of nebulized glycopyrrolate for administration using a high efficiency nebulizer in patients with chronic obstructive pulmonary disease
Efficacy and safety of nebulized glycopyrrolate for administration using a high efficiency nebulizer in patients with chronic obstructive pulmonary disease Abstract Aims To establish the dose−response for pharmacodynamics (bronchodilatation), safety and pharmacokinetics for a nebulized formulation of the long acting mu...
PMC9421621
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic profiles of a novel phospholipid-aspirin complex liquid formulation and low dose enteric-coated aspirin: results from a prospective, randomized, crossover study
Pharmacokinetic and pharmacodynamic profiles of a novel phospholipid-aspirin complex liquid formulation and low dose enteric-coated aspirin: results from a prospective, randomized, crossover study Abstract Abstract Low dose enteric-coated aspirin (EC-ASA) is routinely used for secondary cardiovascular event prevention....
PMC9580807
core_pubmed_pmc
Computational Models for Diagnosing and Treating Endometriosis
Computational Models for Diagnosing and Treating Endometriosis Abstract Abstract Endometriosis is a common but poorly understood disease. Symptoms can begin early in adolescence, with menarche, and can be debilitating. Despite this, people often suffer several years before being correctly diagnosed and adequately treat...
PMC10119371
core_pubmed_pmc
A Mouse Model to Test Novel Therapeutics for Parkinson’s Disease: an Update on the Thy1-aSyn (“line 61”) Mice
A Mouse Model to Test Novel Therapeutics for Parkinson’s Disease: an Update on the Thy1-aSyn (“line 61”) Mice Abstract Development of neuroprotective therapeutics for Parkinson’s disease (PD) is facing a lack of translation from pre-clinical to clinical trials. One strategy for improvement is to increase predictive val...
PMC4302124
core_pubmed_pmc
Modelling chemotherapy effects on granulopoiesis
Modelling chemotherapy effects on granulopoiesis Abstract Abstract Background Although the growth-factor G-CSF is widely used to prevent granulotoxic side effects of cytotoxic chemotherapies, its optimal use is still unknown since treatment outcome depends on many parameters such as dosing and timing of chemotherapies,...
PMC3102616
core_pubmed_pmc
Characterization of the bronchodilatory dose response to indacaterol in patients with chronic obstructive pulmonary disease using model-based approaches
Characterization of the bronchodilatory dose response to indacaterol in patients with chronic obstructive pulmonary disease using model-based approaches Abstract Abstract Background Indacaterol is a once-daily long-acting inhaled β 2 -agonist indicated for maintenance treatment of moderate-to-severe chronic obstructive...
PMC9618653
core_pubmed_pmc
Enhanced anti-breast cancer efficacy of co-delivery liposomes of docetaxel and curcumin
Enhanced anti-breast cancer efficacy of co-delivery liposomes of docetaxel and curcumin Abstract The successful treatment of breast cancer is hampered by toxicity to normal cells, impaired drug accumulation at the tumor site, and multidrug resistance. We designed a novel multifunctional liposome, CUR-DTX-L, to co-deliv...
PMC7179577
core_pubmed_pmc
An Individual Participant Data Population Pharmacokinetic Meta-analysis of Drug-Drug Interactions between Lumefantrine and Commonly Used Antiretroviral Treatment
An Individual Participant Data Population Pharmacokinetic Meta-analysis of Drug-Drug Interactions between Lumefantrine and Commonly Used Antiretroviral Treatment Abstract Treating malaria in HIV-coinfected individuals should consider potential drug-drug interactions. Artemether-lumefantrine is the most widely recommend...
PMC9685553
core_pubmed_pmc
Comparative pharmacokinetics of new curcumin preparations and evidence for increased bioavailability in healthy adult participants
Comparative pharmacokinetics of new curcumin preparations and evidence for increased bioavailability in healthy adult participants Abstract Abstract Objective: Theracurmin, which contains the curcumin composition, CR-033P, has been demonstrated to be highly bioavailable. To compare the pharmacokinetics of the three com...
PMC9469693
core_pubmed_pmc
Exposure‐response relationships of etrolizumab in patients with moderately‐to‐severely active ulcerative colitis
Exposure‐response relationships of etrolizumab in patients with moderately‐to‐severely active ulcerative colitis Abstract Abstract Etrolizumab is an IgG1‐humanized monoclonal anti‐β7 integrin antibody. Phase III trials with induction and/or maintenance phases were conducted in patients with moderately‐to‐severely activ...
PMC3743526
core_pubmed_pmc
Pharmacodynamics of vancomycin in elderly patients aged 75 years or older with methicillin-resistant Staphylococcus aureus hospital-acquired pneumonia
Pharmacodynamics of vancomycin in elderly patients aged 75 years or older with methicillin-resistant Staphylococcus aureus hospital-acquired pneumonia Abstract Abstract Background Methicillin-resistant Staphylococcus aureus (MRSA) infections are associated with significant mortality and health care costs. To improve tr...
PMC10968602
core_pubmed_pmc
Nephrotic Syndrome: From Pathophysiology to Novel Therapeutic Approaches
Nephrotic Syndrome: From Pathophysiology to Novel Therapeutic Approaches Abstract Abstract Nephrotic edema stands out as one of the most common complications of nephrotic syndrome. The effective management of hypervolemia is paramount in addressing this condition. Initially, “the underfill hypothesis” suggested that pr...
PMC9402490
core_pubmed_pmc
Pharmacokinetic Assessment and Treatment Effect of Lusutrombopag in Child–Pugh Class C Patients: Review of Patient Data from Two Clinical Studies and Post-Marketing Surveillance
Pharmacokinetic Assessment and Treatment Effect of Lusutrombopag in Child–Pugh Class C Patients: Review of Patient Data from Two Clinical Studies and Post-Marketing Surveillance Abstract Introduction Patients with thrombocytopenia and chronic liver disease are at increased risk of bleeding during invasive procedures du...
PMC11123365
core_pubmed_pmc
Evaluation of the Metabolite Profile of Fish Oil Omega-3 Fatty Acids (n-3 FAs) in Micellar and Enteric-Coated Forms—A Randomized, Cross-Over Human Study
Evaluation of the Metabolite Profile of Fish Oil Omega-3 Fatty Acids (n-3 FAs) in Micellar and Enteric-Coated Forms—A Randomized, Cross-Over Human Study Abstract Abstract This study evaluated the differences in the metabolite profile of three n-3 FA fish oil formulations in 12 healthy participants: (1) standard softgel...
PMC4674516
core_pubmed_pmc
Potentially Inappropriate Medications in the Elderly in Korean Long-Term Care Facilities
Potentially Inappropriate Medications in the Elderly in Korean Long-Term Care Facilities Abstract Abstract Background Elderly residents of long-term care facilities are more vulnerable to being prescribed inappropriate medications because of the high incidence of co-medication in this population resulting from the pres...
PMC6155221
core_pubmed_pmc
A UPLC-MS/MS Method for Simultaneous Determination of Free and Total Forms of a Phenolic Acid and Two Flavonoids in Rat Plasma and Its Application to Comparative Pharmacokinetic Studies of Polygonum capitatum Extract in Rats
A UPLC-MS/MS Method for Simultaneous Determination of Free and Total Forms of a Phenolic Acid and Two Flavonoids in Rat Plasma and Its Application to Comparative Pharmacokinetic Studies of Polygonum capitatum Extract in Rats Abstract Abstract The principal active constituents of Polygonum capitatum are phenolic acids a...
PMC6658739
core_pubmed_pmc
Sequential Open-Label Study of the Safety, Tolerability, and Pharmacokinetic Interactions between Dihydroartemisinin-Piperaquine and Mefloquine in Healthy Thai Adults
Sequential Open-Label Study of the Safety, Tolerability, and Pharmacokinetic Interactions between Dihydroartemisinin-Piperaquine and Mefloquine in Healthy Thai Adults Abstract Artemisinin-based combination therapies (ACTs) have contributed substantially to the global decline in Plasmodium falciparum morbidity and morta...
PMC6697719
core_pubmed_pmc
Impact of mammalian cell culture conditions on monoclonal antibody charge heterogeneity: an accessory monitoring tool for process development
Impact of mammalian cell culture conditions on monoclonal antibody charge heterogeneity: an accessory monitoring tool for process development Abstract Recombinant monoclonal antibodies are predominantly produced in mammalian cell culture bioprocesses. Post-translational modifications affect the micro-heterogeneity of t...
PMC5351006
core_pubmed_pmc
Modeling and Experimental Studies of Obeticholic Acid Exposure and the Impact of Cirrhosis Stage
Modeling and Experimental Studies of Obeticholic Acid Exposure and the Impact of Cirrhosis Stage Abstract Obeticholic acid (OCA), a semisynthetic bile acid, is a selective and potent farnesoid X receptor (FXR) agonist in development for the treatment of chronic nonviral liver diseases. Physiologic pharmacokinetic model...
PMC5023160
core_pubmed_pmc
Efficacy and Safety of AmBisome in Combination with Sodium Stibogluconate or Miltefosine and Miltefosine Monotherapy for African Visceral Leishmaniasis: Phase II Randomized Trial
Efficacy and Safety of AmBisome in Combination with Sodium Stibogluconate or Miltefosine and Miltefosine Monotherapy for African Visceral Leishmaniasis: Phase II Randomized Trial Abstract Background SSG&PM over 17 days is recommended as first line treatment for visceral leishmaniasis in eastern Africa, but is painful a...
PMC11946702
core_pubmed_pmc
Physicochemical Characterization and Oral Bioavailability of Curcumin–Phospholipid Complex Nanosuspensions Prepared Based on Microfluidic System
Physicochemical Characterization and Oral Bioavailability of Curcumin–Phospholipid Complex Nanosuspensions Prepared Based on Microfluidic System Abstract Background : Curcumin has been proved to have promising prospects in the fields of anti-inflammation, antibacterial, anti-oxidation, and neuroprotection. However, its...
PMC10950984
core_pubmed_pmc
Safety and pharmacokinetics of imaradenant (AZD4635) in Japanese patients with advanced solid malignancies: a phase I, open-label study
Safety and pharmacokinetics of imaradenant (AZD4635) in Japanese patients with advanced solid malignancies: a phase I, open-label study Abstract Abstract Purpose Imaradenant is a novel potent and selective adenosine A2A receptor antagonist that is hypothesized to reduce immune suppression in the tumor microenvironment....
PMC11420247
core_pubmed_pmc
A sub-pharmacological test dose does not predict individual docetaxel exposure in prostate cancer patients
A sub-pharmacological test dose does not predict individual docetaxel exposure in prostate cancer patients Abstract Abstract Purpose Docetaxel is a cytotoxic drug used for first-line treatment of various malignancies. It has a narrow therapeutic index and shows wide interpatient variability in clearance and toxicity. T...
PMC9979628
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of imatinib for optimal drug repurposing from cancer to COVID-19
Pharmacokinetics and pharmacodynamics of imatinib for optimal drug repurposing from cancer to COVID-19 Abstract Introduction In the randomized double-blind placebo-controlled CounterCOVID study, oral imatinib treatment conferred a positive clinical outcome and a signal for reduced mortality in COVID-19 patients. High c...
PMC12626027
core_pubmed_pmc
A Review Vancomycin Role in Gram Positive Biofilm-Associated Infections: Challenges and Emerging Solutions
A Review Vancomycin Role in Gram Positive Biofilm-Associated Infections: Challenges and Emerging Solutions Abstract Abstract Biofilm-associated infections pose a significant challenge in clinical settings due to their increased resistance to antibiotics and evasion of host immune responses. These infections are respons...
PMC3859605
core_pubmed_pmc
Genetic and Non-Genetic Determinants of Raltegravir Penetration into Cerebrospinal Fluid: A Single Arm Pharmacokinetic Study
Genetic and Non-Genetic Determinants of Raltegravir Penetration into Cerebrospinal Fluid: A Single Arm Pharmacokinetic Study Abstract Abstract Background Antiretroviral drugs vary in their central nervous system penetration, with better penetration possibly conferring neurocognitive benefit during human immunodeficienc...
PMC5297975
core_pubmed_pmc
Pharmacokinetic Effects of Isavuconazole Coadministration With the Cytochrome P450 Enzyme Substrates Bupropion, Repaglinide, Caffeine, Dextromethorphan, and Methadone in Healthy Subjects
Pharmacokinetic Effects of Isavuconazole Coadministration With the Cytochrome P450 Enzyme Substrates Bupropion, Repaglinide, Caffeine, Dextromethorphan, and Methadone in Healthy Subjects Abstract Abstract This report describes phase 1 clinical trials performed to assess interactions of oral isavuconazole at the clinica...
PMC9834611
core_pubmed_pmc
Vinblastine pharmacokinetics in mouse, dog, and human in the context of a physiologically based model incorporating tissue‐specific drug binding, transport, and metabolism
Vinblastine pharmacokinetics in mouse, dog, and human in the context of a physiologically based model incorporating tissue‐specific drug binding, transport, and metabolism Abstract Abstract Vinblastine (VBL) is a vinca alkaloid‐class cytotoxic chemotherapeutic that causes microtubule disruption and is typically used to...
PMC10050909
core_pubmed_pmc
Pharmacokinetics of antitubercular drugs in patients hospitalized with HIV-associated tuberculosis: a population modeling analysis
Pharmacokinetics of antitubercular drugs in patients hospitalized with HIV-associated tuberculosis: a population modeling analysis Abstract Background Early mortality among hospitalized HIV-associated tuberculosis (TB/HIV) patients is high despite treatment. The pharmacokinetics of rifampicin, isoniazid, and pyrazinami...
PMC10983022
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and safety of frunexian in healthy Chinese volunteer adults: A randomized dose‐escalation phase I study
Pharmacokinetics, pharmacodynamics, and safety of frunexian in healthy Chinese volunteer adults: A randomized dose‐escalation phase I study Abstract Abstract The purpose of this study was to evaluate the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of frunexian (formerly known as EP‐7041 and HSK36273) injec...
PMC11163651
core_pubmed_pmc
Format-tuning of in vivo-launched bispecific T cell engager enhances efficacy against renal cell carcinoma
Format-tuning of in vivo-launched bispecific T cell engager enhances efficacy against renal cell carcinoma Abstract Abstract Background Advanced clear cell renal cell carcinoma (ccRCC) is a prevalent kidney cancer for which long-term survival rates are abysmal, though immunotherapies are showing potential. Not yet clin...
PMC3876315
core_pubmed_pmc
Sedative Dosing of Propofol for Treatment of Migraine Headache in the Emergency Department: A Case Series
Sedative Dosing of Propofol for Treatment of Migraine Headache in the Emergency Department: A Case Series Abstract Introduction: Migraine headaches requiring an emergency department visit due to failed outpatient rescue therapy present a significant challenge in terms of length of stay (LOS) and financial costs. Propof...
PMC9548544
core_pubmed_pmc
Population pharmacokinetic model of vancomycin in postoperative neurosurgical patients
Population pharmacokinetic model of vancomycin in postoperative neurosurgical patients Abstract Objective: Vancomycin is commonly used in postoperative neurosurgical patients for empirical anti-infective treatment due to the low success rate of bacterial culture in cerebrospinal fluid (about 20%) and the high mortality...
PMC4370683
core_pubmed_pmc
Pharmacokinetics, safety, and efficacy of APF530 (extended-release granisetron) in patients receiving moderately or highly emetogenic chemotherapy: results of two Phase II trials
Pharmacokinetics, safety, and efficacy of APF530 (extended-release granisetron) in patients receiving moderately or highly emetogenic chemotherapy: results of two Phase II trials Abstract Background Despite advances with new therapies, a significant proportion of patients (>30%) suffer delayed-onset chemotherapy-induce...
PMC8842656
core_pubmed_pmc
The Maximum-Tolerated Dose and Pharmacokinetics of a Novel Chemically Modified Curcumin in Rats
The Maximum-Tolerated Dose and Pharmacokinetics of a Novel Chemically Modified Curcumin in Rats Abstract Purpose CMC 2.24, a chemically modified curcumin, was developed as a novel, pleiotropic MMP-inhibitor to treat various inflammatory/collagenolytic diseases including periodontitis. To date, this compound has shown e...
PMC11635537
core_pubmed_pmc
Drug Therapy-related Problems Detected by Clinical Pharmacists in a Closed Loop Medication Management; A Cross-sectional Study in UAE
Drug Therapy-related Problems Detected by Clinical Pharmacists in a Closed Loop Medication Management; A Cross-sectional Study in UAE Abstract Abstract Introduction: Drug therapy-related problems (DTRP) can lead to avoidable negative health consequences, particularly during hospital admissions. This study aimed to asse...
PMC7615677
core_pubmed_pmc
DNDI-6174, a preclinical candidate for visceral leishmaniasis that targets the cytochrome bc1 complex
DNDI-6174, a preclinical candidate for visceral leishmaniasis that targets the cytochrome bc1 complex Abstract New drugs for visceral leishmaniasis that are safe, low cost and adapted to the field are urgently required. Despite concerted efforts over the last several years, the number of new chemical entities with nove...
PMC8518427
core_pubmed_pmc
Benefit‐Risk Assessment of Off‐Label Drug Use in Children: The Bravo Framework
Benefit‐Risk Assessment of Off‐Label Drug Use in Children: The Bravo Framework Abstract Abstract A drug is granted a license for use after a thorough assessment of risks and benefits based on high‐quality scientific proof of its efficacy and safety. Many drugs that are relevant to children are not licensed for use in t...
PMC4225328
core_pubmed_pmc
A clinical and pharmacokinetic study of the combination of etravirine plus raltegravir in HIV patients with expanded intolerance or resistance
A clinical and pharmacokinetic study of the combination of etravirine plus raltegravir in HIV patients with expanded intolerance or resistance Abstract Introduction The combination of etravirine (ETR) plus raltegravir (RAL) could be an option for HIV patients with resistance, intolerance or important interactions with ...
PMC11634579
core_pubmed_pmc
Network pharmacology, experimental validation and pharmacokinetics integrated strategy to reveal pharmacological mechanism of goutengsan on methamphetamine dependence
Network pharmacology, experimental validation and pharmacokinetics integrated strategy to reveal pharmacological mechanism of goutengsan on methamphetamine dependence Abstract Background Goutengsan (GTS) is a traditional Chinese medicine formula that can improve multiple nervous system diseases, such as methamphetamine...
PMC12616239
core_pubmed_pmc
Tarlatamab Exposure–Efficacy and Exposure–Safety Relationships to Inform Dose Selection in Patients with Small Cell Lung Cancer
Tarlatamab Exposure–Efficacy and Exposure–Safety Relationships to Inform Dose Selection in Patients with Small Cell Lung Cancer Abstract Abstract Purpose: Tarlatamab is a first-in-class, half-life extended bispecific T-cell engager immunotherapy targeting delta-like ligand 3, currently approved for the treatment of adu...
PMC10879373
core_pubmed_pmc
A Randomized, Open-Label Study Conducted to Evaluate the Bioequivalence of Pegfilgrastim-cbqv On-Body Injector Versus Prefilled Syringe in Healthy Male Participants
A Randomized, Open-Label Study Conducted to Evaluate the Bioequivalence of Pegfilgrastim-cbqv On-Body Injector Versus Prefilled Syringe in Healthy Male Participants Abstract Introduction To help prevent febrile neutropenia, pegfilgrastim-cbqv (UDENYCA ® ; Coherus BioSciences), a pegfilgrastim (NEULASTA ® ; Amgen) biosi...
PMC9439991
core_pubmed_pmc
Population Pharmacokinetic Modelling of Intravenous Immunoglobulin Treatment in Patients with Guillain–Barré Syndrome
Population Pharmacokinetic Modelling of Intravenous Immunoglobulin Treatment in Patients with Guillain–Barré Syndrome Abstract Abstract Background and Objective Intravenous immunoglobulin (IVIg) at a standard dosage is the treatment of choice for Guillain–Barré syndrome. The pharmacokinetics, however, is highly variabl...
PMC8529019
core_pubmed_pmc
Evaluation of Natalizumab Pharmacokinetics and Pharmacodynamics: Toward Individualized Doses
Evaluation of Natalizumab Pharmacokinetics and Pharmacodynamics: Toward Individualized Doses Abstract Background: Plasma concentration of natalizumab falls above the therapeutic threshold in many patients who, therefore, receive more natalizumab than necessary and have higher risk of progressive multifocal leukoencepha...
PMC12440994
core_pubmed_pmc
Advances of paeoniflorin in depression: the molecular mechanism and formula application
Advances of paeoniflorin in depression: the molecular mechanism and formula application Abstract Abstract Paeoniflorin (PF) is widely present in species of the Paeonia genus. In recent years, numerous preclinical studies have shown that PF has preventive and therapeutic effects on various neurological diseases, particu...
PMC12821564
core_pubmed_pmc
First‐In‐Human Study to Assess the Pharmacokinetics and Safety of DS‐6016a After Single Subcutaneous Injection in Healthy Japanese Adults
First‐In‐Human Study to Assess the Pharmacokinetics and Safety of DS‐6016a After Single Subcutaneous Injection in Healthy Japanese Adults Abstract Abstract Fibrodysplasia ossificans progressiva is a rare, progressive autosomal dominant genetic disease caused by an activin receptor‐like kinase 2 (ALK2) mutation with a n...
PMC7448909
core_pubmed_pmc
Pharmacokinetics and tissue residue of enrofloxacin in healthy, Eimeria -infected broiler chickens and those pre-treated with amprolium and toltrazuril
Pharmacokinetics and tissue residue of enrofloxacin in healthy, Eimeria -infected broiler chickens and those pre-treated with amprolium and toltrazuril Abstract ABSTRACT The pharmacokinetics of enrofloxacin was compared in healthy chickens, Eimeria infected chickens and in Eimeria infected chickens pre-treated with amp...
PMC10930379
core_pubmed_pmc
A Systematic Review of Clozapine Concentration–Dose Ratio from Therapeutic Drug Monitoring Studies in Children and Adolescents Treated with Clozapine for Mental Disorders
A Systematic Review of Clozapine Concentration–Dose Ratio from Therapeutic Drug Monitoring Studies in Children and Adolescents Treated with Clozapine for Mental Disorders Abstract Abstract Background: Therapeutic drug monitoring of clozapine in children and adolescents has received insufficient attention. Calculation o...
PMC4226160
core_pubmed_pmc
Quantitative Systems Pharmacology can reduce attrition and improve productivity in pharmaceutical research and development
Quantitative Systems Pharmacology can reduce attrition and improve productivity in pharmaceutical research and development Abstract Abstract The empirical hypothesis generation and testing approach to pharmaceutical research and development (R&D), and biomedical research has proven very effective over the last half-cen...
PMC7973531
core_pubmed_pmc
Confirmation of the cardiac safety of nolasiban in a randomised cohort of healthy female volunteers
Confirmation of the cardiac safety of nolasiban in a randomised cohort of healthy female volunteers Abstract Abstract Nolasiban is an orally active oxytocin receptor antagonist being developed to increase the efficiency of assisted reproductive technologies. This study evaluated the pharmacokinetics, pharmacodynamics, ...
PMC7034090
core_pubmed_pmc
Drug-interactive mPEG- b -PLA-Phe(Boc) micelles enhance the tolerance and anti-tumor efficacy of docetaxel
Drug-interactive mPEG- b -PLA-Phe(Boc) micelles enhance the tolerance and anti-tumor efficacy of docetaxel Abstract Abstract Docetaxel (DTX) is one of the most promising chemotherapeutic agents for a variety of solid tumors. However, the clinical efficacy of the marketed formulation, Taxotere ® , is limited due to its ...
PMC8188985
core_pubmed_pmc
Direct Oral Anticoagulants: From Randomized Clinical Trials to Real-World Clinical Practice
Direct Oral Anticoagulants: From Randomized Clinical Trials to Real-World Clinical Practice Abstract Abstract Direct oral anticoagulants (DOACs) are a more manageable alternative than vitamin K antagonists (VKAs) to prevent stroke in patients with nonvalvular atrial fibrillation and to prevent and treat venous thromboe...
PMC11936838
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Immunogenicity of ALXN1820 (Tarperprumig) in Healthy Adults: Results of a Phase I Study
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Immunogenicity of ALXN1820 (Tarperprumig) in Healthy Adults: Results of a Phase I Study Abstract ABSTRACT Properdin is an endogenous positive regulator of the complement alternative pathway (AP). Tarperprumig (ALXN1820), a novel humanized bispecific antibody...
PMC5034697
core_pubmed_pmc
Abundance of Hepatic Transporters in Caucasians: A Meta-Analysis
Abundance of Hepatic Transporters in Caucasians: A Meta-Analysis Abstract This study aimed to derive quantitative abundance values for key hepatic transporters suitable for in vitro–in vivo extrapolation within a physiologically based pharmacokinetic modeling framework. A meta-analysis was performed whereby data on abu...
PMC4147055
core_pubmed_pmc
Diurnal Variation in P-glycoprotein-Mediated Transport and Cerebrospinal Fluid Turnover in the Brain
Diurnal Variation in P-glycoprotein-Mediated Transport and Cerebrospinal Fluid Turnover in the Brain Abstract Nearly all bodily processes exhibit circadian rhythmicity. As a consequence, the pharmacokinetic and pharmacodynamic properties of a drug may also vary with time of day. The objective of this study was to inves...
PMC6628362
core_pubmed_pmc
A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4- d ]Pyrimidine Dual Src/P-Glycoprotein Inhibitor
A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4- d ]Pyrimidine Dual Src/P-Glycoprotein Inhibitor Abstract Abstract Overexpression of P-glycoprotein (P-gp) and other ATP-binding cassette (ABC) transporters in multidrug resistant (MDR) cancer cells is ...
PMC3787887
core_pubmed_pmc
Curcumin enhances the lung cancer chemopreventive efficacy of phospho-sulindac by improving its pharmacokinetics
Curcumin enhances the lung cancer chemopreventive efficacy of phospho-sulindac by improving its pharmacokinetics Abstract Abstract Phospho-sulindac (PS) is a safe sulindac derivative with promising anticancer efficacy in colon cancer. We evaluated whether its combination with curcumin could enhance the efficacy in the ...
PMC12298344
core_pubmed_pmc
Advances in Liposomal Drug Delivery: Multidirectional Perspectives on Overcoming Biological Barriers
Advances in Liposomal Drug Delivery: Multidirectional Perspectives on Overcoming Biological Barriers Abstract Abstract Liposomes represent a cornerstone of modern drug delivery systems due to their unique structural and physicochemical characteristics. Extensive research has refined their formulation, stability, and ta...