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PMC10273406
core_pubmed_pmc
In silico clinical trial evaluating lisdexamfetamine’s and methylphenidate’s mechanism of action computational models in an attention-deficit/hyperactivity disorder virtual patients’ population
In silico clinical trial evaluating lisdexamfetamine’s and methylphenidate’s mechanism of action computational models in an attention-deficit/hyperactivity disorder virtual patients’ population Abstract Abstract Introduction Attention-deficit/hyperactivity disorder (ADHD) is an impairing psychiatric condition with the ...
PMC5744090
core_pubmed_pmc
Evaluation of Posaconazole Pharmacokinetics in Adult Patients with Invasive Fungal Infection
Evaluation of Posaconazole Pharmacokinetics in Adult Patients with Invasive Fungal Infection Abstract Mortality and morbidity due to invasive fungal infections have increased over the years. Posaconazole is a second-generation triazole agent with an extended spectrum of activity, which shows a high interindividual vari...
PMC5434659
core_pubmed_pmc
Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist
Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist Abstract The physiologic properties of glucagon-like peptide 1 (GLP-1) make it a potent candidate drug target in the treatment of type 2 diabetes mellitus (T2DM). GLP-1 is capable of regulating the blood glucose level by...
PMC12030311
core_pubmed_pmc
PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation
PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation Abstract Proteolysis targeting chimeras (PROTACs), heterobifunctional molecules that hijack the ubiquitin–proteasome system (UPS) to degrade specific proteins, hold great promise in treating d...
PMC5668101
core_pubmed_pmc
Phase I clinical trial of the base excision repair inhibitor methoxyamine in combination with fludarabine for patients with advanced hematologic malignancies
Phase I clinical trial of the base excision repair inhibitor methoxyamine in combination with fludarabine for patients with advanced hematologic malignancies Abstract Purpose We determined the safety, pharmacokinetics, pharmacodynamics and recommended phase II dose of the base excision repair blocker methoxyamine combi...
PMC5939830
core_pubmed_pmc
Human Abuse Potential of an Abuse-Deterrent (AD), Extended-Release (ER) Morphine Product Candidate (Morphine-ADER Injection-Molded Tablets) vs Extended-Release Morphine Administered Intranasally in Nondependent Recreational Opioid Users
Human Abuse Potential of an Abuse-Deterrent (AD), Extended-Release (ER) Morphine Product Candidate (Morphine-ADER Injection-Molded Tablets) vs Extended-Release Morphine Administered Intranasally in Nondependent Recreational Opioid Users Abstract Abstract Objective. To compare the relative human abuse potential after in...
PMC6125572
core_pubmed_pmc
Population Pharmacokinetics and Cerebrospinal Fluid Penetration of Fluconazole in Adults with Cryptococcal Meningitis
Population Pharmacokinetics and Cerebrospinal Fluid Penetration of Fluconazole in Adults with Cryptococcal Meningitis Abstract Robust population pharmacokinetic (PK) data for fluconazole are scarce. The variability of fluconazole penetration into the central nervous system (CNS) is not known. ABSTRACT Robust population...
PMC4626378
core_pubmed_pmc
Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib
Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib Abstract Abstract Patients have responded well to the multi-targeted tyrosine kinase inhibitor (TKI) Sunitinib in the clinic. But the severe toxic side effects associated with Sunitinib limit its therapeutic index. ...
PMC7564034
core_pubmed_pmc
Identification of bioactive anti-angiogenic components targeting tumor endothelial cells in Shenmai injection using multidimensional pharmacokinetics
Identification of bioactive anti-angiogenic components targeting tumor endothelial cells in Shenmai injection using multidimensional pharmacokinetics Abstract Shenmai injection (SMI) is a well-defined herbal preparation that is widely and clinically used as an adjuvant therapy for cancer. Previously, we found that SMI ...
PMC3121579
core_pubmed_pmc
PKreport: report generation for checking population pharmacokinetic model assumptions
PKreport: report generation for checking population pharmacokinetic model assumptions Abstract Background Graphics play an important and unique role in population pharmacokinetic (PopPK) model building by exploring hidden structure among data before modeling, evaluating model fit, and validating results after modeling....
PMC9664847
core_pubmed_pmc
Safety and Pharmacokinetics of LHF-535, a Potential Treatment for Lassa Fever, in Healthy Adults
Safety and Pharmacokinetics of LHF-535, a Potential Treatment for Lassa Fever, in Healthy Adults Abstract ABSTRACT LHF-535 is a small-molecule antiviral currently under development as a therapeutic option to treat Lassa fever and other viral hemorrhagic fevers of arenavirus origin. The human safety and pharmacokinetics...
PMC10027508
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, safety, and efficacy of crizanlizumab in patients with sickle cell disease
Pharmacokinetics, pharmacodynamics, safety, and efficacy of crizanlizumab in patients with sickle cell disease Abstract Key Points • Results from SOLACE-adults demonstrate the PK and PD properties of crizanlizumab in patients with SCD during long-term treatment. • Results also show that no new safety signals were ident...
PMC9784203
core_pubmed_pmc
Effect of Dispersion Medium on Pharmacokinetic Profile of Rotigotine Crystalline Suspension following Subcutaneous Injection
Effect of Dispersion Medium on Pharmacokinetic Profile of Rotigotine Crystalline Suspension following Subcutaneous Injection Abstract Abstract Rotigotine (RTG) is prescribed as a once-daily transdermal patch for managing early Parkinson’s disease (PD), which presents issues such as skin irritation and poor patient adhe...
PMC2889283
core_pubmed_pmc
Fractional dynamics pharmacokinetics–pharmacodynamic models
Fractional dynamics pharmacokinetics–pharmacodynamic models Abstract Abstract While an increasing number of fractional order integrals and differential equations applications have been reported in the physics, signal processing, engineering and bioengineering literatures, little attention has been paid to this class of...
PMC4514311
core_pubmed_pmc
Postcataract endophthalmitis prophylaxis using irrigation, incision hydration, and eye pressurization with vancomycin
Postcataract endophthalmitis prophylaxis using irrigation, incision hydration, and eye pressurization with vancomycin Abstract Purpose This study aimed to determine whether switching from balanced salt solution (BSS) to vancomycin 20 g/mL BSS for incision hydration and eye pressurization reduces the rate of postcatarac...
PMC9417124
core_pubmed_pmc
Safety and Pharmacokinetics of Monoclonal Antibodies VRC07-523LS and PGT121 Administered Subcutaneously for Human Immunodeficiency Virus Prevention
Safety and Pharmacokinetics of Monoclonal Antibodies VRC07-523LS and PGT121 Administered Subcutaneously for Human Immunodeficiency Virus Prevention Abstract Abstract Background Effective, long-acting prevention approaches are needed to reduce human immunodeficiency virus (HIV) incidence. We evaluated the safety and pha...
PMC12190993
core_pubmed_pmc
Antechodynamics and Antechokinetics: Dynamics and Kinetics of Antibiotic Resistance Biomolecules
Antechodynamics and Antechokinetics: Dynamics and Kinetics of Antibiotic Resistance Biomolecules Abstract The pharmacology of antimicrobial agents comprises pharmacodynamics and pharmacokinetics. Pharmacodynamics refers to studying drugs’ mode of action on their molecular targets at various concentrations and the resul...
PMC10893797
core_pubmed_pmc
Developing mathematical models to compare and analyse the pharmacokinetics of morphine and fentanyl
Developing mathematical models to compare and analyse the pharmacokinetics of morphine and fentanyl Abstract Abstract Background and Aims: The two-compartment model is generally used in pharmacokinetics to illustrate the distribution and excretion of drugs. In this study, we evaluated the distribution patterns of morph...
PMC12692235
core_pubmed_pmc
3-CMC: Acute Effects in Male and Female Mice, Human Intoxication Case Series (Italy, 2014–2025), and Prediction of ADMET Properties
3-CMC: Acute Effects in Male and Female Mice, Human Intoxication Case Series (Italy, 2014–2025), and Prediction of ADMET Properties Abstract 3-chloromethcathinone (3-CMC) is a synthetic cathinone that gained relevance, having been involved in a large number of seizures and poisoning reports. Despite this, literature cu...
PMC11522094
core_pubmed_pmc
Population Pharmacokinetic Analysis of Tucatinib in Healthy Participants and Patients with Breast Cancer or Colorectal Cancer
Population Pharmacokinetic Analysis of Tucatinib in Healthy Participants and Patients with Breast Cancer or Colorectal Cancer Abstract Background and Objective Tucatinib is a highly selective, oral, reversible, human epidermal growth factor receptor 2 (HER2)-specific tyrosine kinase inhibitor. Tucatinib is approved at ...
PMC8388650
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Profile, Bioavailability, and Withdrawal Time of Tylosin Tartrate Following a Single Intramuscular Administration in Olive Flounder ( Paralichthys olivaceus )
Pharmacokinetic-Pharmacodynamic Profile, Bioavailability, and Withdrawal Time of Tylosin Tartrate Following a Single Intramuscular Administration in Olive Flounder ( Paralichthys olivaceus ) Abstract Simple Summary Fishes usually stop eating food when they are sick, and treating diseased fish with oral drugs is a serio...
PMC12634772
core_pubmed_pmc
Clinical applications of tacrolimus in the treatment of ocular diseases: a narrative literature review
Clinical applications of tacrolimus in the treatment of ocular diseases: a narrative literature review Abstract Abstract Purpose To narratively review clinical use of topical and periocular tacrolimus in ophthalmology, with emphasis on allergic keratoconjunctivitis (VKC/AKC), ocular GVHD, post‑keratoplasty prophylaxis,...
PMC8496351
core_pubmed_pmc
Mechanistic Coupling of a Novel in silico Cotyledon Perfusion Model and a Physiologically Based Pharmacokinetic Model to Predict Fetal Acetaminophen Pharmacokinetics at Delivery
Mechanistic Coupling of a Novel in silico Cotyledon Perfusion Model and a Physiologically Based Pharmacokinetic Model to Predict Fetal Acetaminophen Pharmacokinetics at Delivery Abstract Little is known about placental drug transfer and fetal pharmacokinetics despite increasing drug use in pregnant women. While physiol...
PMC8225528
core_pubmed_pmc
PBPK Modeling Approach to Predict the Behavior of Drugs Cleared by Kidney in Pregnant Subjects and Fetus
PBPK Modeling Approach to Predict the Behavior of Drugs Cleared by Kidney in Pregnant Subjects and Fetus Abstract Abstract The purpose of this study was to develop a physiologically based pharmacokinetic (PBPK) model predicting the pharmacokinetics (PK) of different compounds in pregnant subjects. This model considers ...
PMC8477747
core_pubmed_pmc
A Single Animal Species-Based Prediction of Human Clearance and First-in-Human Dose of Monoclonal Antibodies: Beyond Monkey
A Single Animal Species-Based Prediction of Human Clearance and First-in-Human Dose of Monoclonal Antibodies: Beyond Monkey Abstract These days, there is a lot of emphasis on the prediction of human clearance (CL) from a single species for monoclonal antibodies (mabs). Many studies indicate that monkey is the most suit...
PMC10615561
core_pubmed_pmc
Prediction of the Clinical Course of Immune Thrombocytopenia in Children by Platelet Kinetics
Prediction of the Clinical Course of Immune Thrombocytopenia in Children by Platelet Kinetics Abstract Childhood immune thrombocytopenia (ITP) is a rare autoimmune disorder characterized by isolated thrombocytopenia. Prolonged ITP (persistent and chronic) leads to a reduced quality of life for children in many domains....
PMC11009648
core_pubmed_pmc
Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer
Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer Abstract Significance The mammalian switch/sucrose nonfermentable (mSWI/SNF) complex is a promising therapeutic target for enhancer-driven cancers. PROTACs (proteolysis-targeting chimera), which enabl...
PMC12623720
core_pubmed_pmc
Engineered long-acting Irisin-albumin binding domain fusion protein for enhanced anti-inflammatory efficacy in lipopolysaccharide-induced systemic inflammation
Engineered long-acting Irisin-albumin binding domain fusion protein for enhanced anti-inflammatory efficacy in lipopolysaccharide-induced systemic inflammation Abstract Abstract Irisin is a peptide hormone with notable anti-inflammatory and metabolic regulatory effects but has limited clinical utility due to its extrem...
PMC12358309
core_pubmed_pmc
Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV 1 ) in Uncontrolled Moderate‐To‐Severe Asthma
Semi‐Mechanistic Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Dupilumab on Pre‐Bronchodilator Forced Expiratory Volume in 1 Second (FEV 1 ) in Uncontrolled Moderate‐To‐Severe Asthma Abstract ABSTRACT In this study, we investigated the pharmacokinetic/pharmacodynamic (PK/PD) relationship of dupilumab a...
PMC12389682
core_pubmed_pmc
Variations in Plasma Levels of Orally Administered Ivermectin Could Hamper Its Potential Drug Repositioning: Results of a Bioequivalence Study in Mexican Population
Variations in Plasma Levels of Orally Administered Ivermectin Could Hamper Its Potential Drug Repositioning: Results of a Bioequivalence Study in Mexican Population Abstract Abstract Background/Objectives : Despite its initial promise as a treatment for COVID-19 due to its antiviral properties, controlled randomized tr...
PMC7193397
core_pubmed_pmc
Assessing short-term impact of PM 10 on mortality using a semiparametric generalized propensity score approach
Assessing short-term impact of PM 10 on mortality using a semiparametric generalized propensity score approach Abstract Abstract Background The shape of the exposure-response curve describing the effects of air pollution on population health has crucial regulatory implications, and it is important in assessing causal i...
PMC10329961
core_pubmed_pmc
Crossover Randomized Study of Pharmacologic Effects of Ripasudil–Brimonidine Fixed-Dose Combination Versus Ripasudil or Brimonidine
Crossover Randomized Study of Pharmacologic Effects of Ripasudil–Brimonidine Fixed-Dose Combination Versus Ripasudil or Brimonidine Abstract Abstract Introduction Multidrug regimens for glaucoma treatment often result in adherence issues due to inconvenience; these issues may be improved with fixed-dose combination dru...
PMC5924739
core_pubmed_pmc
Microfluidic Organ-on-a-Chip Models of Human Intestine
Microfluidic Organ-on-a-Chip Models of Human Intestine Abstract Abstract Microfluidic organ-on-a-chip models of human intestine have been developed and used to study intestinal physiology and pathophysiology. In this article, we review this field and describe how microfluidic Intestine Chips offer new capabilities not ...
PMC8056739
core_pubmed_pmc
Population pharmacokinetic analysis of peficitinib in patients with rheumatoid arthritis
Population pharmacokinetic analysis of peficitinib in patients with rheumatoid arthritis Abstract Abstract Aims To analyse the population pharmacokinetics (PK) of peficitinib in patients with rheumatoid arthritis (RA) and assess the potential PK covariates to identify the requirement for dose adjustment in RA patients....
PMC5030464
core_pubmed_pmc
A Phase 1B, randomized, double blind, placebo controlled, multiple-dose escalation study of NSI-189 phosphate, a neurogenic compound, in depressed patients
A Phase 1B, randomized, double blind, placebo controlled, multiple-dose escalation study of NSI-189 phosphate, a neurogenic compound, in depressed patients Abstract We wanted to examine tolerability and efficacy of NSI-189, a benzylpiperizine-aminiopyridine neurogenic compound for treating major depressive disorder (MD...
PMC4769563
core_pubmed_pmc
Radix Puerariae lobatae ( Gegen ) suppresses the anticoagulation effect of warfarin: a pharmacokinetic and pharmacodynamics study
Radix Puerariae lobatae ( Gegen ) suppresses the anticoagulation effect of warfarin: a pharmacokinetic and pharmacodynamics study Abstract Abstract Background Radix Salvia miltiorrhiza ( Danshen ) and Radix Puerariae lobatae ( Gegen ) are used in Traditional Chinese Medicine to treat cardiovascular diseases. However, a...
PMC4618649
core_pubmed_pmc
Evacetrapib: in vitro and clinical disposition, metabolism, excretion, and assessment of drug interaction potential with strong CYP3A and CYP2C8 inhibitors
Evacetrapib: in vitro and clinical disposition, metabolism, excretion, and assessment of drug interaction potential with strong CYP3A and CYP2C8 inhibitors Abstract Evacetrapib is an investigational cholesteryl ester transfer protein inhibitor (CETPi) for reduction of risk of major adverse cardiovascular events in pati...
PMC8249284
core_pubmed_pmc
The Effect of Renal Impairment on the Pharmacokinetics and Safety of Talazoparib in Patients with Advanced Solid Tumors
The Effect of Renal Impairment on the Pharmacokinetics and Safety of Talazoparib in Patients with Advanced Solid Tumors Abstract Background Pharmacokinetic (PK) studies suggest that talazoparib is primarily eliminated unchanged via renal excretion. The current study investigated how varying degrees of renal impairment ...
PMC11772103
core_pubmed_pmc
Effects of short‐term exposure to moderate amounts of alcohol on brain volume
Effects of short‐term exposure to moderate amounts of alcohol on brain volume Abstract Abstract Aim Although numerous studies have reported that chronic alcohol consumption causes brain volume reduction and cerebrospinal fluid volume increase, few studies have examined the acute effects of alcohol on brain structure. T...
PMC11205536
core_pubmed_pmc
Metabolite Profiling Analysis of the Tongmai Sini Decoction in Rats after Oral Administration through UHPLC-Q-Exactive-MS/MS
Metabolite Profiling Analysis of the Tongmai Sini Decoction in Rats after Oral Administration through UHPLC-Q-Exactive-MS/MS Abstract Tongmai Sini decoction (TSD), the classical prescriptions of traditional Chinese medicine, consisting of three commonly used herbal medicines, has been widely applied for the treatment o...
PMC8940165
core_pubmed_pmc
Therapeutic Drug Monitoring of Conditioning Agents in Pediatric Allogeneic Stem Cell Transplantation; Where do We Stand?
Therapeutic Drug Monitoring of Conditioning Agents in Pediatric Allogeneic Stem Cell Transplantation; Where do We Stand? Abstract Abstract Allogeneic hematopoietic stem cell transplantation (HSCT) is an established curative treatment that has significantly improved clinical outcome of pediatric patients with malignant ...
PMC10184974
core_pubmed_pmc
Repurposing of drugs against methyltransferase as potential Zika virus therapies
Repurposing of drugs against methyltransferase as potential Zika virus therapies Abstract In recent years, the outbreak of infectious disease caused by Zika Virus (ZIKV) has posed a major threat to global public health, calling for the development of therapeutics to treat ZIKV disease. Several possible druggable target...
PMC10143161
core_pubmed_pmc
A Method for Evaluating Robustness of Limited Sampling Strategies—Exemplified by Serum Iohexol Clearance for Determination of Measured Glomerular Filtration Rate
A Method for Evaluating Robustness of Limited Sampling Strategies—Exemplified by Serum Iohexol Clearance for Determination of Measured Glomerular Filtration Rate Abstract Abstract In combination with Bayesian estimates based on a population pharmacokinetic model, limited sampling strategies (LSS) may reduce the number ...
PMC11173101
core_pubmed_pmc
The Relationship between the Measured Blood Concentration of Rocuronium in Stable Muscle Relaxation with a Closed-Loop Control and the Estimated Blood Concentration from a Pharmacokinetic Simulation
The Relationship between the Measured Blood Concentration of Rocuronium in Stable Muscle Relaxation with a Closed-Loop Control and the Estimated Blood Concentration from a Pharmacokinetic Simulation Abstract Abstract We developed a system to adjust the rate of a continuous rocuronium (Rb) infusion to achieve 3 ≤ %T1 ≤ ...
PMC11879453
core_pubmed_pmc
Chemical evolution of ASO-like DNAzymes for effective and extended gene silencing in cells
Chemical evolution of ASO-like DNAzymes for effective and extended gene silencing in cells Abstract Abstract Antisense oligonucleotides (ASOs) and small interfering RNA (siRNA) therapeutics highlight the power of oligonucleotides in silencing disease-causing messenger RNAs (mRNAs). Another promising class of gene-silen...
PMC3840328
core_pubmed_pmc
Current clinical evidence on pioglitazone pharmacogenomics
Current clinical evidence on pioglitazone pharmacogenomics Abstract Pioglitazone is the most widely used thiazolidinedione and acts as an insulin-sensitizer through activation of the Peroxisome Proliferator-Activated Receptor-γ (PPARγ). Pioglitazone is approved for use in the management of type 2 diabetes mellitus (T2D...
PMC8927028
core_pubmed_pmc
Population Pharmacokinetic–B Cell Modeling for Ofatumumab in Patients with Relapsing Multiple Sclerosis
Population Pharmacokinetic–B Cell Modeling for Ofatumumab in Patients with Relapsing Multiple Sclerosis Abstract Abstract Background Ofatumumab, a fully human anti-CD20 monoclonal antibody indicated for the treatment of relapsing forms of multiple sclerosis (RMS), binds to a unique conformational epitope, thereby deple...
PMC8613074
core_pubmed_pmc
Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach
Influence of CYP2D6 Phenotypes on the Pharmacokinetics of Aripiprazole and Dehydro-Aripiprazole Using a Physiologically Based Pharmacokinetic Approach Abstract Background and Objectives Aripiprazole is an atypical antipsychotic drug that is metabolized by cytochrome P450 (CYP) 2D6 and CYP3A4, which mainly form its acti...
PMC5292145
core_pubmed_pmc
Renal safety of lithium in HIV-infected patients established on tenofovir disoproxil fumarate containing antiretroviral therapy: analysis from a randomized placebo-controlled trial
Renal safety of lithium in HIV-infected patients established on tenofovir disoproxil fumarate containing antiretroviral therapy: analysis from a randomized placebo-controlled trial Abstract Background The prevalence of bipolar disorder in HIV-infected patients is higher than the general population. Lithium is the most ...
PMC10143675
core_pubmed_pmc
High-Dose Spermidine Supplementation Does Not Increase Spermidine Levels in Blood Plasma and Saliva of Healthy Adults: A Randomized Placebo-Controlled Pharmacokinetic and Metabolomic Study
High-Dose Spermidine Supplementation Does Not Increase Spermidine Levels in Blood Plasma and Saliva of Healthy Adults: A Randomized Placebo-Controlled Pharmacokinetic and Metabolomic Study Abstract (1) Background: Spermidine is a biogenic polyamine that plays a crucial role in mammalian metabolism. As spermidine levels...
PMC7894166
core_pubmed_pmc
A phase 2, open‐label study of single‐dose dupilumab in children aged 6 months to <6 years with severe uncontrolled atopic dermatitis: pharmacokinetics, safety and efficacy
A phase 2, open‐label study of single‐dose dupilumab in children aged 6 months to <6 years with severe uncontrolled atopic dermatitis: pharmacokinetics, safety and efficacy Abstract Abstract Background Dupilumab has demonstrated efficacy and acceptable safety in adults and children (aged 6–17 years) with moderate‐to‐se...
PMC7522073
core_pubmed_pmc
Variability of Skin Pharmacokinetic Data: Insights from a Topical Bioequivalence Study Using Dermal Open Flow Microperfusion
Variability of Skin Pharmacokinetic Data: Insights from a Topical Bioequivalence Study Using Dermal Open Flow Microperfusion Abstract Purpose Dermal open flow microperfusion (dOFM) has previously demonstrated its utility to assess the bioequivalence (BE) of topical drug products in a clinical study. We aimed to charact...
PMC11440922
core_pubmed_pmc
Advances and challenges in immunoPET methodology
Advances and challenges in immunoPET methodology Abstract Abstract Immuno-positron emission tomography (immunoPET) enables imaging of specific targets that play a role in targeted therapy and immunotherapy, such as antigens on cell membranes, targets in the disease microenvironment, or immune cells. The most common imm...
PMC10974941
core_pubmed_pmc
The Validation and Determination of Empagliflozin Concentration in the Presence of Grapefruit Juice Using HPLC for Pharmacokinetic Applications
The Validation and Determination of Empagliflozin Concentration in the Presence of Grapefruit Juice Using HPLC for Pharmacokinetic Applications Abstract Type 2 diabetes mellitus is a multifactorial disorder whose primary manifestation usually initiates with elevated blood sugar levels. Several antidiabetic agents are u...
PMC4933725
core_pubmed_pmc
Traxoprodil, a selective antagonist of the NR2B subunit of the NMDA receptor, potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice
Traxoprodil, a selective antagonist of the NR2B subunit of the NMDA receptor, potentiates the antidepressant-like effects of certain antidepressant drugs in the forced swim test in mice Abstract One of the newest substances, whose antidepressant activity was shown is traxoprodil, which is a selective antagonist of the ...
PMC4929099
core_pubmed_pmc
A randomized phase I trial of nanoparticle albumin-bound paclitaxel with or without mifepristone for advanced breast cancer
A randomized phase I trial of nanoparticle albumin-bound paclitaxel with or without mifepristone for advanced breast cancer Abstract Purpose Glucocorticoid receptor (GR) overexpression is associated with poor prognosis ER-negative breast cancer. GR antagonism with mifepristone increases chemotherapy-induced breast canc...
PMC12238578
core_pubmed_pmc
High-resolution fecal pharmacokinetic modeling in mice with orally administered antibiotics
High-resolution fecal pharmacokinetic modeling in mice with orally administered antibiotics Abstract Abstract High-resolution fecal pharmacokinetics are crucial for optimizing therapeutic design and evaluating gastrointestinal motility. However, empirical studies with detailed fecal concentration over time data remain ...
PMC8609446
core_pubmed_pmc
Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example
Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles: rhIFNα-1b example Abstract Abstract Coated microneedles (MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs (GEC-MNs) was developed...
PMC5114328
core_pubmed_pmc
A phase I pharmacokinetic and safety study of cabazitaxel in adult cancer patients with normal and impaired renal function
A phase I pharmacokinetic and safety study of cabazitaxel in adult cancer patients with normal and impaired renal function Abstract Purpose Limited data are available on cabazitaxel pharmacokinetics in patients with renal impairment. This open-label, multicenter study assessed cabazitaxel in patients with advanced soli...
PMC10941563
core_pubmed_pmc
Supplementing clinical lactation studies with PBPK modeling to inform drug therapy in lactating mothers: Prediction of primaquine exposure as a case example
Supplementing clinical lactation studies with PBPK modeling to inform drug therapy in lactating mothers: Prediction of primaquine exposure as a case example Abstract Abstract Evaluating the safety of primaquine (PQ) during breastfeeding requires an understanding of its pharmacokinetics (PKs) in breast milk and its expo...
PMC10972161
core_pubmed_pmc
ADME Gene-Related Pharmacogenomic Labeling of FDA-Approved Drugs: Comparison with Clinical Pharmacogenetics Implementation Consortium (CPIC) Evidence Levels
ADME Gene-Related Pharmacogenomic Labeling of FDA-Approved Drugs: Comparison with Clinical Pharmacogenetics Implementation Consortium (CPIC) Evidence Levels Abstract Abstract Pharmacogenomics (PGx) can facilitate the transition to patient-specific drug regimens and thus improve their efficacy and reduce toxicity. The a...
PMC12368721
core_pubmed_pmc
Antiviral Effect of Piperine on Chikungunya Virus: In Vitro Evidence and In Silico Analysis of E1-E2 Binding
Antiviral Effect of Piperine on Chikungunya Virus: In Vitro Evidence and In Silico Analysis of E1-E2 Binding Abstract Chikungunya virus (CHIKV) is an emerging arbovirus that causes acute and chronic disease with significant public health concerns. Although recent vaccines have been licensed, no specific antiviral treat...
PMC7449211
core_pubmed_pmc
Population Pharmacokinetics of Praziquantel in Pregnant and Lactating Filipino Women Infected with Schistosoma japonicum
Population Pharmacokinetics of Praziquantel in Pregnant and Lactating Filipino Women Infected with Schistosoma japonicum Abstract An estimated 40 million women of reproductive age are infected with one of three species of the waterborne parasite Schistosoma spp. Treatment with praziquantel (PZQ) via mass drug administr...
PMC10609774
core_pubmed_pmc
Development, Characterization and Pharmacological Evaluation of Cannabidiol-Loaded Long Circulating Niosomes
Development, Characterization and Pharmacological Evaluation of Cannabidiol-Loaded Long Circulating Niosomes Abstract Cannabidiol (CBD) is a promising drug candidate with pleiotropic pharmacological activity, whose low aqueous solubility and unfavorable pharmacokinetics have presented obstacles to its full clinical imp...
PMC10233611
core_pubmed_pmc
Phase I/II results of ceralasertib as monotherapy or in combination with acalabrutinib in high-risk relapsed/refractory chronic lymphocytic leukemia
Phase I/II results of ceralasertib as monotherapy or in combination with acalabrutinib in high-risk relapsed/refractory chronic lymphocytic leukemia Abstract Background: Patients with relapsed/refractory (R/R) chronic lymphocytic leukemia (CLL) have limited treatment options. Ceralasertib, a selective ataxia telangiect...
PMC11694626
core_pubmed_pmc
Spiro thiochromene–oxindoles as novel anti-inflammatory agents: design, sustainable synthesis, in vitro and in silico evaluations †
Spiro thiochromene–oxindoles as novel anti-inflammatory agents: design, sustainable synthesis, in vitro and in silico evaluations † Abstract Abstract A one-pot, acid-, base-, and metal-free, multicomponent strategy has been developed to synthesize spiro thiochromene–oxindole derivatives as potential anti-inflammatory a...
PMC6989258
core_pubmed_pmc
Population pharmacodynamics of cilostazol in healthy Korean subjects
Population pharmacodynamics of cilostazol in healthy Korean subjects Abstract Cilostazol is used for the treatment of intermittent claudication, ulceration and pain. This study was conducted to develop a population pharmacodynamic (PD) model for cilostazol's closure time (CT) prolongation effect in healthy Korean subje...
PMC10149867
core_pubmed_pmc
High-fat diets enhance and delay ursodeoxycholic acid absorption but elevate circulating hydrophobic bile salts
High-fat diets enhance and delay ursodeoxycholic acid absorption but elevate circulating hydrophobic bile salts Abstract Background: Ursodeoxycholic acid (UDCA) is a natural drug essential for the treatment of cholestatic liver diseases. The food effects on the absorption of UDCA and the disposition of circulating bile...
PMC10772056
core_pubmed_pmc
Pharmacokinetics of low doses of colchicine in the leukocytes of Japanese healthy individuals
Pharmacokinetics of low doses of colchicine in the leukocytes of Japanese healthy individuals Abstract Abstract The venerable drug colchicine has garnered significant recent attention due to its endorsement by the United States Food and Drug Administration as an anti-inflammatory medication for cardiovascular diseases....
PMC11359394
core_pubmed_pmc
Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model
Solubilization of Paclitaxel with Natural Compound Rubusoside toward Improving Oral Bioavailability in a Rodent Model Abstract Abstract Paclitaxel, which features low water solubility and permeability, is an efflux pump substrate. The current paclitaxel drugs are given intravenously after resolving the solubility issue...
PMC9131799
core_pubmed_pmc
A randomized, double-blind, parallel-group, single-dose comparative pharmacokinetic study of DRL_TZ, a candidate biosimilar of trastuzumab, with Herceptin ® (EU) in healthy adult males
A randomized, double-blind, parallel-group, single-dose comparative pharmacokinetic study of DRL_TZ, a candidate biosimilar of trastuzumab, with Herceptin ® (EU) in healthy adult males Abstract Background & objectives : Trastuzumab (TZ) is a recombinant DNA-derived humanized monoclonal antibody approved for human epide...
PMC9687076
core_pubmed_pmc
Fosfomycin Pharmacokinetic Profile in Plasma and Urine and Quantitative Estimation in Prostate and Seminal Vesicles after One and Two Consecutive Doses of Oral Fosfomycin Trometamol in Healthy Male Volunteers
Fosfomycin Pharmacokinetic Profile in Plasma and Urine and Quantitative Estimation in Prostate and Seminal Vesicles after One and Two Consecutive Doses of Oral Fosfomycin Trometamol in Healthy Male Volunteers Abstract Abstract The present Phase I study investigated, for the first time, fosfomycin pharmacokinetics in hu...
PMC11429409
core_pubmed_pmc
Dosing Evaluation of Ceftazidime–Avibactam in Intensive Care Unit Patients Based on Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling and Simulation
Dosing Evaluation of Ceftazidime–Avibactam in Intensive Care Unit Patients Based on Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling and Simulation Abstract Abstract P. aeruginosa is the most common microorganism involved in many ICU-acquired infections. A correct dosage regimen is pivotal to avoiding resistance develo...
PMC4768433
core_pubmed_pmc
Examining the predictive accuracy of the novel 3D N-linear algebraic molecular codifications on benchmark datasets
Examining the predictive accuracy of the novel 3D N-linear algebraic molecular codifications on benchmark datasets Abstract Background Recently, novel 3D alignment-free molecular descriptors (also known as QuBiLS-MIDAS) based on two-linear, three-linear and four-linear algebraic forms have been introduced. These descri...
PMC3750485
core_pubmed_pmc
Anakinra pharmacokinetics in children and adolescents with systemic-onset juvenile idiopathic arthritis and autoinflammatory syndromes
Anakinra pharmacokinetics in children and adolescents with systemic-onset juvenile idiopathic arthritis and autoinflammatory syndromes Abstract Background Anakinra pharmacokinetics and pharmacodynamics were investigated in children and adolescents treated for systemic-onset juvenile idiopathic arthritis (SJIA) and auto...
PMC11884411
core_pubmed_pmc
Mogrol Regulates the Expression of ATPase Na+/K+ Transport Subunit 3, Inhibits Cardiomyocyte Apoptosis, and Plays a Protective Role Against Myocardial Infarction
Mogrol Regulates the Expression of ATPase Na+/K+ Transport Subunit 3, Inhibits Cardiomyocyte Apoptosis, and Plays a Protective Role Against Myocardial Infarction Abstract Background With the advancements in medical technology, the death rate from myocardial infarction (MI), a prevalent heart illness, has gradually decr...
PMC12919187
core_pubmed_pmc
The Impact of CYP3A5 Genotype on Tacrolimus Pharmacokinetics in Children following Heart Transplant
The Impact of CYP3A5 Genotype on Tacrolimus Pharmacokinetics in Children following Heart Transplant Abstract Tacrolimus is a first-line immunosuppressant used after solid organ transplantation that suffers from extensive intra- and inter-patient variability and a narrow therapeutic window. Tacrolimus clearance is predo...
PMC11771645
core_pubmed_pmc
Determination of Vatiquinone Drug‐Drug Interactions, as CYP450 Perpetrator and Victim, Using Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation
Determination of Vatiquinone Drug‐Drug Interactions, as CYP450 Perpetrator and Victim, Using Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation Abstract Abstract Vatiquinone, a 15‐lipoxygenase inhibitor, is in development for patients with Friedreich's ataxia. Physiologically based pharmacokinetic (PB...
PMC9747319
core_pubmed_pmc
Integrated Brain Metabolomics and Network Pharmacology Analysis to Reveal the Improvement Effect of Bai Chan Ting on Parkinson's Disease
Integrated Brain Metabolomics and Network Pharmacology Analysis to Reveal the Improvement Effect of Bai Chan Ting on Parkinson's Disease Abstract Background Baichanting (BCT),a traditional Chinese medicine prescription, is a combination of Acanthopanax senticosus , Paeonia lactiflora , and Uncaria three herbs, which ha...
PMC10555929
core_pubmed_pmc
Dissecting the human gut microbiome to better decipher drug liability: A once-forgotten organ takes center stage
Dissecting the human gut microbiome to better decipher drug liability: A once-forgotten organ takes center stage Abstract Highlights • Dynamic factors altering distal intestine exposure and MDM rate co-contribute to MDM impact on drug PK. • Evolving therapeutic landscape demands GM metabolism consideration for risk man...
PMC10033182
core_pubmed_pmc
Mechanisms of Obesity-Induced Changes in Pharmacokinetics of IgG in Rats
Mechanisms of Obesity-Induced Changes in Pharmacokinetics of IgG in Rats Abstract Abstract Purpose To evaluate how obesity affects the pharmacokinetics of human IgG following subcutaneous (SC) and intravenous (IV) administration to rats and the homeostasis of endogenous rat IgG. Methods Differences in body weight and s...
PMC5892677
core_pubmed_pmc
Safety and pharmacokinetics of dolutegravir in HIV-positive pregnant women: a systematic review
Safety and pharmacokinetics of dolutegravir in HIV-positive pregnant women: a systematic review Abstract Abstract Background The integrase strand transfer inhibitor dolutegravir (DTG) is being introduced into low- and middle-income countries (LMICs) as an alternative to first-line treatment with non-nucleoside reverse ...
PMC11876674
core_pubmed_pmc
Semi-mechanistic efficacy model for PARP + ATR inhibitors—application to rucaparib and talazoparib in combination with gartisertib in breast cancer PDXs
Semi-mechanistic efficacy model for PARP + ATR inhibitors—application to rucaparib and talazoparib in combination with gartisertib in breast cancer PDXs Abstract Abstract Background Promising cancer treatments, such as DDR inhibitors, are often challenged by the heterogeneity of responses in clinical trials. The presen...
PMC7180925
core_pubmed_pmc
Quantification of an Antibody-Conjugated Drug in Fat Plasma by an Affinity Capture LC-MS/MS Method for a Novel Prenyl Transferase-Mediated Site-Specific Antibody–Drug Conjugate
Quantification of an Antibody-Conjugated Drug in Fat Plasma by an Affinity Capture LC-MS/MS Method for a Novel Prenyl Transferase-Mediated Site-Specific Antibody–Drug Conjugate Abstract The novel prenyl transferase-mediated, site-specific, antibody–drug conjugate LCB14-0110 is comprised of a proprietary beta-glucuronid...
PMC12622538
core_pubmed_pmc
High‐Throughput Strategies for Streamlining Lipid Nanoparticle Development Pipeline
High‐Throughput Strategies for Streamlining Lipid Nanoparticle Development Pipeline Abstract Abstract Lipid nanoparticles (LNPs) have become clinically validated nanocarriers for nucleic acid delivery, enabling applications in mRNA vaccines and therapies for cancer, ocular, and infectious diseases. Identifying LNPs for...
PMC7549385
core_pubmed_pmc
Dose Rationale for Amoxicillin in Neonatal Sepsis When Referral Is Not Possible
Dose Rationale for Amoxicillin in Neonatal Sepsis When Referral Is Not Possible Abstract Background Despite the widespread use of amoxicillin in young children, efforts to establish the feasibility of simplified dosing regimens in resource-limited settings have relied upon empirical evidence of efficacy. Given the anti...
PMC10113037
core_pubmed_pmc
A French Real-World Evidence Study Evaluating the Efficacy, Safety, and Pharmacokinetic Parameters of rVIII-SingleChain in Patients with Hemophilia A Receiving Prophylaxis
A French Real-World Evidence Study Evaluating the Efficacy, Safety, and Pharmacokinetic Parameters of rVIII-SingleChain in Patients with Hemophilia A Receiving Prophylaxis Abstract Background rVIII-SingleChain is a recombinant factor VIII (FVIII) with increased binding affinity to von Willebrand factor compared with ot...
PMC8158513
core_pubmed_pmc
Bio-Distribution and Pharmacokinetics of Topically Administered γ-Cyclodextrin Based Eye Drops in Rabbits
Bio-Distribution and Pharmacokinetics of Topically Administered γ-Cyclodextrin Based Eye Drops in Rabbits Abstract The purpose of this study was to evaluate the ocular pharmacokinetics, bio-distribution and local tolerability of γ-cyclodextrin (γCD) based irbesartan 1.5% eye drops and candesartan 0.15% eye drops after ...
PMC4279896
core_pubmed_pmc
In vivo evaluation of mutant selection window of cefquinome against Escherichia coli in piglet tissue-cage model
In vivo evaluation of mutant selection window of cefquinome against Escherichia coli in piglet tissue-cage model Abstract Background The resistance of cephalosporins is significantly serious in veterinary clinic. In order to inhibit the bacterial resistance production, the mutant selection window (MSW) hypothesis with ...
PMC10061841
core_pubmed_pmc
A double-blinded, placebo-controlled, randomized study to evaluate the efficacy of perioperative dextromethorphan compared to placebo for the treatment of postoperative pain: a study protocol
A double-blinded, placebo-controlled, randomized study to evaluate the efficacy of perioperative dextromethorphan compared to placebo for the treatment of postoperative pain: a study protocol Abstract Background Pain management is a critical component of comprehensive postsurgical care, as it influences patient safety ...
PMC9319670
core_pubmed_pmc
Current Antithrombotic Therapy Strategies in Children with a Focus on Off-Label Direct Oral Anticoagulants—A Narrative Review
Current Antithrombotic Therapy Strategies in Children with a Focus on Off-Label Direct Oral Anticoagulants—A Narrative Review Abstract Abstract (1) Background: The incidence of thromboembolic events is relatively low in the general population, but it increases in hospitalized children and those who underwent thrombogen...
PMC12008288
core_pubmed_pmc
Network control energy reductions under DMT relate to serotonin receptors, signal diversity, and subjective experience
Network control energy reductions under DMT relate to serotonin receptors, signal diversity, and subjective experience Abstract Abstract Psychedelics offer a profound window into the human brain through their robust effects on perception, subjective experience, and brain activity patterns. The serotonergic psychedelic ...
PMC8299544
core_pubmed_pmc
Physiologically based modelling of tranexamic acid pharmacokinetics following intravenous, intramuscular, sub-cutaneous and oral administration in healthy volunteers
Physiologically based modelling of tranexamic acid pharmacokinetics following intravenous, intramuscular, sub-cutaneous and oral administration in healthy volunteers Abstract Highlights • Tranexamic acid (TXA) as a treatment for post-partum haemorrhage (PPH) depends on early intervention and rapid systemic exposure. • ...
PMC12655055
core_pubmed_pmc
Predicting Pharmacokinetics of Drugs in Patients with Heart Failure and Optimizing Their Dosing Strategies Using a Physiologically Based Pharmacokinetic Model
Predicting Pharmacokinetics of Drugs in Patients with Heart Failure and Optimizing Their Dosing Strategies Using a Physiologically Based Pharmacokinetic Model Abstract Abstract Background: Heart failure (HF), as the end stage of various cardiac diseases, alters blood flow to key organs responsible for drug clearance. T...
PMC10339695
core_pubmed_pmc
Evaluation of the cytochrome P450 2C19 and 3A4 inhibition potential of the complement factor 5a receptor 1 antagonist ACT‐1014‐6470 in vitro and in vivo
Evaluation of the cytochrome P450 2C19 and 3A4 inhibition potential of the complement factor 5a receptor 1 antagonist ACT‐1014‐6470 in vitro and in vivo Abstract Abstract ACT‐1014‐6470 is an orally available complement factor 5a receptor 1 antagonist and a novel treatment option in auto‐inflammatory diseases. The in vi...
PMC4080980
core_pubmed_pmc
The pharmacokinetics of anthocyanins and their metabolites in humans
The pharmacokinetics of anthocyanins and their metabolites in humans Abstract Abstract Background and Purpose Anthocyanins are phytochemicals with reported vasoactive bioactivity. However, given their instability at neutral pH, they are presumed to undergo significant degradation and subsequent biotransformation. The a...
PMC4273425
core_pubmed_pmc
An alternative mebendazole formulation for cystic echinococcosis: the treatment efficacy, pharmacokinetics and safety in mice
An alternative mebendazole formulation for cystic echinococcosis: the treatment efficacy, pharmacokinetics and safety in mice Abstract Abstract Background Cystic echinococcosis is a serious zoonotic infection worldwide caused by metacestodes of Echinococcus gruanulosus . Mebendazole and albendazole are the only two dru...
PMC9305158
core_pubmed_pmc
Translational Approaches for Brain Delivery of Biologics via Cerebrospinal Fluid
Translational Approaches for Brain Delivery of Biologics via Cerebrospinal Fluid Abstract Abstract Delivery of biologics via cerebrospinal fluid (CSF) has demonstrated potential to access the tissues of the central nervous system (CNS) by circumventing the blood‐brain barrier and blood‐CSF barrier. Developing an effect...
PMC12254954
core_pubmed_pmc
Translational Model‐Informed Dose Selection for Iruplinalkib, a Selective Oral ALK / ROS1 Tyrosine Kinase Inhibitor
Translational Model‐Informed Dose Selection for Iruplinalkib, a Selective Oral ALK / ROS1 Tyrosine Kinase Inhibitor Abstract ABSTRACT We utilized an integrated approach for model‐informed dose selection to predict the recommended phase 2 dose (RP2D) of iruplinalkib, a selective oral ALK and ROS1 tyrosine kinase inhibit...
PMC12851612
core_pubmed_pmc
A Randomized, Single-Dose, Single-Sequence, Two-Arm (Fasting and Fed), Open-Label Study on the Oral Pharmacokinetics of a Nanodispersible Cannabidiol Solution (150 mg/mL)
A Randomized, Single-Dose, Single-Sequence, Two-Arm (Fasting and Fed), Open-Label Study on the Oral Pharmacokinetics of a Nanodispersible Cannabidiol Solution (150 mg/mL) Abstract Abstract Introduction Cannabidiol (CBD), a non-psychoactive phytocannabinoid, attributed to its therapeutic benefits and positive safety pro...