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PMC11578126
core_pubmed_pmc
Recent applications of pharmacometrics and systems pharmacology approaches to improve and optimize drug therapy for pregnant and lactating women
Recent applications of pharmacometrics and systems pharmacology approaches to improve and optimize drug therapy for pregnant and lactating women Modeling QUANTITATIVE APPROACHES TO PREDICT DRUG EXPOSURE: POPULATION PK, PBPK, AND MODEL‐BASED META ANALYSIS Other articles in this themed issue can be broadly classified int...
PMC11226197
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Coriandrum sativum L., essential oil as a promising source of bioactive compounds with GC/MS, antioxidant, antimicrobial activities : in vitro and in silico predictions
Coriandrum sativum L., essential oil as a promising source of bioactive compounds with GC/MS, antioxidant, antimicrobial activities : in vitro and in silico predictions Abstract Introduction: Coriandrum sativum L. essential oil (CS-EO) is being evaluated in vitro for its antioxidant and antimicrobial properties, and it...
PMC5933261
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A phase 1 dose-escalation study of veliparib with bimonthly FOLFIRI in patients with advanced solid tumours
A phase 1 dose-escalation study of veliparib with bimonthly FOLFIRI in patients with advanced solid tumours Abstract Background Veliparib is a potent poly(ADP-ribose) polymerase inhibitor. This phase 1 study aimed to establish the maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D) of veliparib combined wi...
PMC7247678
core_pubmed_pmc
The Effect of Size, Maturation, Global Asphyxia, Cerebral Ischemia, and Therapeutic Hypothermia on the Pharmacokinetics of High-Dose Recombinant Erythropoietin in Fetal Sheep
The Effect of Size, Maturation, Global Asphyxia, Cerebral Ischemia, and Therapeutic Hypothermia on the Pharmacokinetics of High-Dose Recombinant Erythropoietin in Fetal Sheep Abstract Abstract High-dose human recombinant erythropoietin (rEPO) is a promising potential neuroprotective treatment in preterm and full-term n...
PMC5831710
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Therapeutic and pharmaco-biological, dose-ranging multicentre trial to determine the optimal dose of TRAnexamic acid to reduce blood loss in haemorrhagic CESarean delivery (TRACES): study protocol for a randomised, double-blind, placebo-controlled trial
Therapeutic and pharmaco-biological, dose-ranging multicentre trial to determine the optimal dose of TRAnexamic acid to reduce blood loss in haemorrhagic CESarean delivery (TRACES): study protocol for a randomised, double-blind, placebo-controlled trial Abstract Abstract Background Postpartum haemorrhage (PPH) is the l...
PMC6746691
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Clinical and Pharmacokinetic Outcomes of Peak–Trough-Based Versus Trough-Based Vancomycin Therapeutic Drug Monitoring Approaches: A Pragmatic Randomized Controlled Trial
Clinical and Pharmacokinetic Outcomes of Peak–Trough-Based Versus Trough-Based Vancomycin Therapeutic Drug Monitoring Approaches: A Pragmatic Randomized Controlled Trial Abstract Background Vancomycin therapeutic drug monitoring (TDM) is based on achieving 24-h area under the concentration–time curve to minimum inhibit...
PMC3798139
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Modulation of drug efflux by aloe materials: An In Vitro investigation across rat intestinal tissue
Modulation of drug efflux by aloe materials: An In Vitro investigation across rat intestinal tissue Abstract Background: Clinically, significant herb-drug interactions have been previously documented and can be pharmacodynamic and/or pharmacokinetic in nature. Pharmacokinetic interactions have been attributed to induct...
PMC5209333
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Genetic Variation in the Histamine Production, Response, and Degradation Pathway Is Associated with Histamine Pharmacodynamic Response in Children with Asthma
Genetic Variation in the Histamine Production, Response, and Degradation Pathway Is Associated with Histamine Pharmacodynamic Response in Children with Asthma Abstract Abstract Introduction: There is growing knowledge of the wide ranging effects of histamine throughout the body therefore it is important to better under...
PMC10447285
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Therapeutic dilemma’s: antipsychotics use for neuropsychiatric symptoms of dementia, delirium and insomnia and risk of falling in older adults, a clinical review
Therapeutic dilemma’s: antipsychotics use for neuropsychiatric symptoms of dementia, delirium and insomnia and risk of falling in older adults, a clinical review Abstract Key summary points Purpose This clinical review summarizes the current evidence on the risks of antipsychotic-related falls in older adults, includin...
PMC5958415
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Unified approach for extrapolation and bridging of adult information in early-phase dose-finding paediatric studies
Unified approach for extrapolation and bridging of adult information in early-phase dose-finding paediatric studies Abstract The number of trials conducted and the number of patients per trial are typically small in paediatric clinical studies. This is due to ethical constraints and the complexity of the medical proces...
PMC11258509
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Understanding antimicrobial pharmacokinetics in critically ill patients to optimize antimicrobial therapy: A narrative review
Understanding antimicrobial pharmacokinetics in critically ill patients to optimize antimicrobial therapy: A narrative review Abstract Effective treatment of sepsis not only demands prompt administration of appropriate antimicrobials but also requires precise dosing to enhance the likelihood of patient survival. Adequa...
PMC5084787
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Marizomib irreversibly inhibits proteasome to overcome compensatory hyperactivation in multiple myeloma and solid tumour patients
Marizomib irreversibly inhibits proteasome to overcome compensatory hyperactivation in multiple myeloma and solid tumour patients Abstract Summary Proteasome inhibitors (PIs) are highly active in multiple myeloma (MM) but resistance is commonly observed. All clinical stage PIs effectively inhibit chymotrypsin‐like (CT‐...
PMC5603587
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Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD
Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD Abstract Binding of calcium to its intracellular receptor calmodulin (CaM) activates a family of Ca 2+ /CaM-dependent protein kinases. CaMKK2 (Ca 2+ /CaM-dependent protein kinase kinase 2) is a central member of this kinase famil...
PMC11720188
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Effect of Genetic Variants on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Involvement of ABCG2 , SLCO1B1 and NAT2
Effect of Genetic Variants on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Involvement of ABCG2 , SLCO1B1 and NAT2 Abstract Abstract Statins are the primary drugs used to prevent cardiovascular disease by inhibiting the HMG-CoA reductase, an enzyme crucial for the synthesis of LDL cholesterol in the liver. A si...
PMC12555100
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Dextromethorphan Versus Dextrorphan: A Quantitative Comparison of Antitussive Potency Following Separate Administration of Metabolite
Dextromethorphan Versus Dextrorphan: A Quantitative Comparison of Antitussive Potency Following Separate Administration of Metabolite Abstract Abstract To assess the antitussive effects of dextrorphan (DOR) relative to its parent compound, dextromethorphan (DEX) a double‐blind, randomized, placebo‐controlled crossover ...
PMC5649598
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Long-Term Clinical Outcomes After Switching from Remicade ® to Biosimilar CT-P13 in Inflammatory Bowel Disease
Long-Term Clinical Outcomes After Switching from Remicade ® to Biosimilar CT-P13 in Inflammatory Bowel Disease Abstract Abstract Background Limited data are available on long-term clinical outcomes regarding the switch from Remicade ® to the infliximab biosimilar CT-P13 in inflammatory bowel disease (IBD) patients. Aim...
PMC10378577
core_pubmed_pmc
Adverse Effects of Antidepressant Medications and their Management in Children and Adolescents
Adverse Effects of Antidepressant Medications and their Management in Children and Adolescents Abstract Introduction: Selective serotonin reuptake inhibitors (SSRIs) and, to a lesser extent, serotonin-norepinephrine reuptake inhibitors (SNRIs) are the cornerstone of pharmacotherapy for children and adolescents with anx...
PMC11907689
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Expanding paclitaxel's therapeutic window: Investigating the pharmacokinetic, clinical formulation and mechanistic aspects of paclitaxel‑lipoate conjugate
Expanding paclitaxel's therapeutic window: Investigating the pharmacokinetic, clinical formulation and mechanistic aspects of paclitaxel‑lipoate conjugate Abstract Abstract Paclitaxel (PTX) is among the most widely used antimicrotubular chemotherapy agents available from natural sources. It has a wide range of antitumo...
PMC12304828
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First‐time cefuroxime target tissue concentrations in long‐lasting spine surgery: Continuous evaluation after repeated weight‐dosed administrations
First‐time cefuroxime target tissue concentrations in long‐lasting spine surgery: Continuous evaluation after repeated weight‐dosed administrations Abstract Abstract Aims Antimicrobial prophylaxis is central in preventing postoperative spine infections, yet knowledge on clinical target spine tissue concentrations remai...
PMC8861063
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Increase water solubility of Centella asiatica extract by indigenous bioenhancers could improve oral bioavailability and disposition kinetics of triterpenoid glycosides in beagle dogs
Increase water solubility of Centella asiatica extract by indigenous bioenhancers could improve oral bioavailability and disposition kinetics of triterpenoid glycosides in beagle dogs Abstract A newly standardised extract of Centella asiatica (Centell-S) with better water solubility than the previous standardised extra...
PMC8122992
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Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit
Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit Abstract Abstract Critically ill pediatric patients often require complex medical procedures as well as invasive testing and monitoring which tend to be painful and anxiety-provoking, necessitating the provision of analgesia and sedation to re...
PMC11963566
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A phase I, single-center, randomized, open-label, three-period crossover study to evaluate the drug–drug interaction between ZSP1273 and oseltamivir in healthy Chinese subjects
A phase I, single-center, randomized, open-label, three-period crossover study to evaluate the drug–drug interaction between ZSP1273 and oseltamivir in healthy Chinese subjects Abstract ABSTRACT ZSP1273 is a novel small-molecule anti-influenza drug that targets the RNA polymerase PB2 subunit, while oseltamivir is the f...
PMC10582670
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A phase I, randomized, ascending‐dose study to assess safety, pharmacokinetics, and activity of GDC‐8264, a RIP1 inhibitor, in healthy volunteers
A phase I, randomized, ascending‐dose study to assess safety, pharmacokinetics, and activity of GDC‐8264, a RIP1 inhibitor, in healthy volunteers Abstract Abstract Receptor‐interacting protein 1 (RIP1) is a key regulator of multiple signaling pathways that mediate inflammatory responses and cell death. RIP1 kinase acti...
PMC5147036
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Safety and Tolerability of CSL112, a Reconstituted, Infusible, Plasma-Derived Apolipoprotein A-I, After Acute Myocardial Infarction
Safety and Tolerability of CSL112, a Reconstituted, Infusible, Plasma-Derived Apolipoprotein A-I, After Acute Myocardial Infarction Abstract Supplemental Digital Content is available in the text. Keywords: alipoprotein A-I, myocardial infarction Abstract Background: Human or recombinant apolipoprotein A-I (apoA-I) has ...
PMC6678465
core_pubmed_pmc
Treatment Options for Colistin Resistant Klebsiella pneumoniae : Present and Future
Treatment Options for Colistin Resistant Klebsiella pneumoniae : Present and Future Abstract Abstract Multidrug-resistant (MDR) Klebsiella pneumoniae represents an increasing threat to human health, causing difficult-to-treat infections with a high mortality rate. Since colistin is one of the few treatment options for ...
PMC11599528
core_pubmed_pmc
Target-controlled dialysis for antibiotics (TCD-ABx)
Target-controlled dialysis for antibiotics (TCD-ABx) Abstract Background Effective antimicrobial therapy is an essential part of intensive care medicine and renal replacement therapy is an important and common intervention which significantly affects the pharmacokinetics of many antimicrobials. This is especially criti...
PMC5909771
core_pubmed_pmc
Landiolol: pharmacology and its use for rate control in atrial fibrillation in an emergency setting
Landiolol: pharmacology and its use for rate control in atrial fibrillation in an emergency setting Abstract Abstract This article provides new insight on landiolol, an ultra-short acting injectable betablocker, recently approved in Europe, with regard to its pharmacokinetic and pharmacodynamic profile, along with its ...
PMC9673813
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Novel Curcumin Derivative-Decorated Ultralong-Circulating Paclitaxel Nanoparticles: A Novel Delivery System with Superior Anticancer Efficacy and Safety
Novel Curcumin Derivative-Decorated Ultralong-Circulating Paclitaxel Nanoparticles: A Novel Delivery System with Superior Anticancer Efficacy and Safety Abstract Purpose Paclitaxel (PTX) has been widely utilized for the treatment of breast cancer. However, drawbacks, such as poor aqueous solubility, rapid blood clearan...
PMC7292221
core_pubmed_pmc
A phase 1, randomized, double‐blind, placebo‐controlled study to evaluate the safety, tolerability, and pharmacokinetics of single and multiple doses of lisdexamfetamine dimesylate in Japanese and Caucasian healthy adult subjects
A phase 1, randomized, double‐blind, placebo‐controlled study to evaluate the safety, tolerability, and pharmacokinetics of single and multiple doses of lisdexamfetamine dimesylate in Japanese and Caucasian healthy adult subjects Abstract Abstract Aim To assess safety, tolerability, and pharmacokinetics of lisdexamfeta...
PMC5074783
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Interleukin-1 antagonists in the treatment of autoinflammatory syndromes, including cryopyrin-associated periodic syndrome
Interleukin-1 antagonists in the treatment of autoinflammatory syndromes, including cryopyrin-associated periodic syndrome Abstract Cryopyrin-associated periodic syndrome (CAPS) include a group of rare autoinflammatory disorders, the spectrum of which ranges from the mildest form, ie, familial cold autoinflammatory syn...
PMC12951621
core_pubmed_pmc
An in vitro-in silico workflow for predicting renal clearance of environmental chemicals and drugs
An in vitro-in silico workflow for predicting renal clearance of environmental chemicals and drugs Abstract Accurate prediction of human renal clearance is essential for evaluating drug pharmacokinetics and environmental chemical risks, yet current methods often neglect rate-determining active transporter-mediated mech...
PMC8762230
core_pubmed_pmc
Application of Population Pharmacokinetic Analysis to Characterize CYP2C19 Mediated Metabolic Mechanism of Voriconazole and Support Dose Optimization
Application of Population Pharmacokinetic Analysis to Characterize CYP2C19 Mediated Metabolic Mechanism of Voriconazole and Support Dose Optimization Abstract Abstract Purpose: The aims of this study were to establish a joint population pharmacokinetic model for voriconazole and its N-oxide metabolite in immunocompromi...
PMC12580772
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A First-in-Human Study of ATM Inhibitor Lartesertib as Monotherapy in Patients with Advanced Solid Tumors
A First-in-Human Study of ATM Inhibitor Lartesertib as Monotherapy in Patients with Advanced Solid Tumors Abstract Abstract Purpose: This first-in-human phase I, open-label study ( NCT04882917 ) evaluated the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and maximum tolerated dose (MTD) of the hig...
PMC8129718
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Physiologically‐based pharmacokinetic modeling to support bioequivalence and approval of generic products: A case for diclofenac sodium topical gel, 1%
Physiologically‐based pharmacokinetic modeling to support bioequivalence and approval of generic products: A case for diclofenac sodium topical gel, 1% Abstract Abstract Establishing bioequivalence (BE) for dermatological drug products by conducting comparative clinical end point studies can be costly and the studies m...
PMC12713689
core_pubmed_pmc
Multicenter Bioavailability Study of Long-Acting Paliperidone in Patients With Schizophrenia or Schizoaffective Disorder
Multicenter Bioavailability Study of Long-Acting Paliperidone in Patients With Schizophrenia or Schizoaffective Disorder Abstract Purpose/Background: Schizophrenia is often associated with nonadherence to oral antipsychotic therapy, which increases the risk of relapse, hospitalization, and higher health care costs. To ...
PMC5009562
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Leveraging syntactic and semantic graph kernels to extract pharmacokinetic drug drug interactions from biomedical literature
Leveraging syntactic and semantic graph kernels to extract pharmacokinetic drug drug interactions from biomedical literature Abstract Background Information about drug–drug interactions (DDIs) supported by scientific evidence is crucial for establishing computational knowledge bases for applications like pharmacovigila...
PMC3873811
core_pubmed_pmc
Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1) Abstract Abstract The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 ...
PMC12706099
core_pubmed_pmc
Dose–effect relationship of intravenous tranexamic acid on perioperative haemoglobin drop in total hip arthroplasty (PRADO study): study protocol for a randomised, double-blind, placebo-controlled, dose–response study
Dose–effect relationship of intravenous tranexamic acid on perioperative haemoglobin drop in total hip arthroplasty (PRADO study): study protocol for a randomised, double-blind, placebo-controlled, dose–response study Abstract Introduction Preoperative administration of tranexamic acid (TXA) reduces perioperative blood...
PMC9959124
core_pubmed_pmc
UPLC-MS/MS Based Identification and Quantification of a Novel Dual Orexin Receptor Antagonist in Plasma Samples by Validated SWGTOX Guidelines
UPLC-MS/MS Based Identification and Quantification of a Novel Dual Orexin Receptor Antagonist in Plasma Samples by Validated SWGTOX Guidelines Abstract Lemborexant (LEM) is a novel dual orexin receptor antagonist (DORA), recently approved for the treatment of insomnia. As with other DORAs, LEM has potential of abuse an...
PMC9800022
core_pubmed_pmc
Therapeutic potential of green tea catechin, (-)-epigallocatechin-3- O -gallate (EGCG) in SARS-CoV-2 infection: Major interactions with host/virus proteases
Therapeutic potential of green tea catechin, (-)-epigallocatechin-3- O -gallate (EGCG) in SARS-CoV-2 infection: Major interactions with host/virus proteases Abstract Background The current COVID-19 pandemic from the human pathogenic virus SARS-CoV-2 has resulted in a major health hazard globally. The morbidity and tran...
PMC10489017
core_pubmed_pmc
Emerging Developments in Separation Techniques and Analysis of Chiral Pharmaceuticals
Emerging Developments in Separation Techniques and Analysis of Chiral Pharmaceuticals Abstract Chiral separation, the process of isolating enantiomers from a racemic mixture, holds paramount importance in diverse scientific disciplines. Using chiral separation methods like chromatography and electrophoresis, enantiomer...
PMC9291109
core_pubmed_pmc
Doxycycline pharmacokinetics in geese
Doxycycline pharmacokinetics in geese Abstract Abstract The study aims to describe the pharmacokinetics of doxycycline after a single intravenous and oral dose (20 mg/kg) in geese. In addition, two multiple‐dose simulations have been performed to investigate the predicted plasma concentration after either a 10 or 20 mg...
PMC9306578
core_pubmed_pmc
Clinical trial diversity: An opportunity for improved insight into the determinants of variability in drug response
Clinical trial diversity: An opportunity for improved insight into the determinants of variability in drug response Abstract Abstract Although the number of countries participating in pivotal trials submitted to enable drug registration has nearly doubled over the past 25 years, there has not been a substantial increas...
PMC12558576
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Comparing Outcomes With Subcutaneous Infliximab (CT-P13 SC) by Baseline Immunosuppressant Use: A Post Hoc Analysis of the LIBERTY-CD and LIBERTY-UC Studies
Comparing Outcomes With Subcutaneous Infliximab (CT-P13 SC) by Baseline Immunosuppressant Use: A Post Hoc Analysis of the LIBERTY-CD and LIBERTY-UC Studies Abstract Abstract Background Superior efficacy of subcutaneous infliximab (CT-P13 SC) over placebo for maintenance therapy in patients with Crohn’s disease (CD) and...
PMC11514655
core_pubmed_pmc
A Phase 1a/1b Study of Fostroxacitabine Bralpamide (Fostrox) Monotherapy in Hepatocellular Carcinoma and Solid Tumor Liver Metastases
A Phase 1a/1b Study of Fostroxacitabine Bralpamide (Fostrox) Monotherapy in Hepatocellular Carcinoma and Solid Tumor Liver Metastases Abstract Purpose To evaluate safety, preliminary efficacy, pharmacokinetics, and pharmacodynamics, of fostroxacitabine bralpamide (fostrox, MIV-818), a novel oral troxacitabine nucleotid...
PMC5045831
core_pubmed_pmc
Effects of Lemon and Seville Orange Juices on the Pharmacokinetic Properties of Sildenafil in Healthy Subjects
Effects of Lemon and Seville Orange Juices on the Pharmacokinetic Properties of Sildenafil in Healthy Subjects Abstract Abstract Purpose Several severe drug interactions have been reported when sildenafil, a potent drug for the treatment of erectile dysfunction, is co-administered with drugs or herbal remedies that inh...
PMC6355558
core_pubmed_pmc
Drug Interactions between Dolutegravir and Artemether-Lumefantrine or Artesunate-Amodiaquine
Drug Interactions between Dolutegravir and Artemether-Lumefantrine or Artesunate-Amodiaquine Abstract Across sub-Saharan Africa, patients with HIV on antiretrovirals often get malaria and need cotreatment with artemisinin-containing therapies. We undertook two pharmacokinetic studies in healthy volunteers, using standa...
PMC9780527
core_pubmed_pmc
Population pharmacokinetics of liposomal amphotericin B in adults with HIV-associated cryptococcal meningoencephalitis
Population pharmacokinetics of liposomal amphotericin B in adults with HIV-associated cryptococcal meningoencephalitis Abstract Abstract Background Single, high-dose liposomal amphotericin B (LAmB; AmBisome, Gilead Sciences) has demonstrated non-inferiority to amphotericin B deoxycholate in combination with other antif...
PMC10968794
core_pubmed_pmc
Bioconversion, Pharmacokinetics, and Therapeutic Mechanisms of Ginsenoside Compound K and Its Analogues for Treating Metabolic Diseases
Bioconversion, Pharmacokinetics, and Therapeutic Mechanisms of Ginsenoside Compound K and Its Analogues for Treating Metabolic Diseases Abstract Rare ginsenoside compound K (CK) is an intestinal microbial metabolite with a low natural abundance that is primarily produced by physicochemical processing, side chain modifi...
PMC8724184
core_pubmed_pmc
Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment
Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment Abstract Purpose Esaxerenone is a novel, oral, nonsteroidal treatment for hypertension. Physiologically based pharmacokinet...
PMC5615269
core_pubmed_pmc
Assessment of Initial Vancomycin Dosing in Pediatric Oncology Patients
Assessment of Initial Vancomycin Dosing in Pediatric Oncology Patients Abstract Abstract This was a retrospective audit assessing vancomycin dosing of 60 mg/kg/day in the attainment of therapeutic concentrations between 10–20 mcg/mL among 56 pediatric oncology patients. Twelve patients (21%) achieved therapeutic concen...
PMC3446492
core_pubmed_pmc
Body mass index influences the response to infliximab in ankylosing spondylitis
Body mass index influences the response to infliximab in ankylosing spondylitis Abstract Abstract Introduction The excess of adipose tissue in obese individuals may have immunomodulating properties and pharmacokinetic consequences. The aim of this study was to determine whether body mass index (BMI) affects response to...
PMC5931107
core_pubmed_pmc
Clinical pharmacodynamic/exposure characterisation of the multikinase inhibitor ilorasertib (ABT-348) in a phase 1 dose-escalation trial
Clinical pharmacodynamic/exposure characterisation of the multikinase inhibitor ilorasertib (ABT-348) in a phase 1 dose-escalation trial Abstract Abstract Background Ilorasertib (ABT-348) inhibits Aurora and VEGF receptor (VEGFR) kinases. Patients with advanced solid tumours participated in a phase 1 dose-escalation tr...
PMC6061126
core_pubmed_pmc
Model reduction in mathematical pharmacology
Model reduction in mathematical pharmacology Abstract Abstract In this paper we present a framework for the reduction and linking of physiologically based pharmacokinetic (PBPK) models with models of systems biology to describe the effects of drug administration across multiple scales. To address the issue of model com...
PMC11773103
core_pubmed_pmc
Inter‐regional pharmacokinetics and exposure–response analyses of belimumab in patients with system lupus erythematosus
Inter‐regional pharmacokinetics and exposure–response analyses of belimumab in patients with system lupus erythematosus Abstract Abstract Aims The pharmacokinetics (PK) of belimumab, a human immunoglobulin G1λ (IgG1λ) monoclonal antibody treatment for systemic lupus erythematosus (SLE), have been well reported. Clinica...
PMC9253220
core_pubmed_pmc
Superior Bioavailability of a Novel Lutein and Zeaxanthin Formulation in Healthy Human Subjects
Superior Bioavailability of a Novel Lutein and Zeaxanthin Formulation in Healthy Human Subjects Abstract Introduction Lutein (L) and zeaxanthin (Z) are carotenoids that are found in the macula of the human eye and are known to improve visual functions. However, poor bioavailability of supplemental L and Z poses a chall...
PMC7090366
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NanoSolveIT Project: Driving nanoinformatics research to develop innovative and integrated tools for in silico nanosafety assessment
NanoSolveIT Project: Driving nanoinformatics research to develop innovative and integrated tools for in silico nanosafety assessment Abstract Highlights • The variability of nanomaterials makes case-by-case risk assessment impractical. • Read-across and machine learning approaches are required to ensure consumer safety...
PMC10450632
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Pharmacometabolomics of trabectedin in metastatic soft tissue sarcoma patients
Pharmacometabolomics of trabectedin in metastatic soft tissue sarcoma patients Abstract Abstract Objective: Trabectedin is an anti-cancer drug commonly used for the treatment of patients with metastatic soft tissue sarcoma (mSTS). Despite its recognized efficacy, significant variability in pharmacological response has ...
PMC6720683
core_pubmed_pmc
Curcumin: Biological, Pharmaceutical, Nutraceutical, and Analytical Aspects
Curcumin: Biological, Pharmaceutical, Nutraceutical, and Analytical Aspects Abstract Abstract Turmeric is a curry spice that originated from India, which has attracted great interest in recent decades because it contains bioactive curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin). Curcumin (1,7-bis-(...
PMC11417411
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Lonicerae Japonicae Flos with the homology of medicine and food: a review of active ingredients, anticancer mechanisms, pharmacokinetics, quality control, toxicity and applications
Lonicerae Japonicae Flos with the homology of medicine and food: a review of active ingredients, anticancer mechanisms, pharmacokinetics, quality control, toxicity and applications Abstract Abstract Lonicerae Japonicae Flos (LJF, called Jinyinhua in China), comes from the dried flower buds or flowers to be opened of Lo...
PMC4053305
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METFORMIN: an efficacy, safety and pharmacokinetic study on the short-term and long-term use in obese children and adolescents – study protocol of a randomized controlled study
METFORMIN: an efficacy, safety and pharmacokinetic study on the short-term and long-term use in obese children and adolescents – study protocol of a randomized controlled study Abstract Background The prevalence of childhood obesity and insulin resistance is rising, increasing the risk of diabetes mellitus type 2. To p...
PMC4453456
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Pharmacokinetics of concomitant cisplatin and paclitaxel administered by hyperthermic intraperitoneal chemotherapy to patients with peritoneal carcinomatosis from epithelial ovarian cancer
Pharmacokinetics of concomitant cisplatin and paclitaxel administered by hyperthermic intraperitoneal chemotherapy to patients with peritoneal carcinomatosis from epithelial ovarian cancer Abstract Abstract Background: Hyperthermic intraperitoneal chemotherapy (HIPEC) is advised as a treatment option for epithelial ova...
PMC9858415
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Drug Repurposing in Non-Small Cell Lung Carcinoma: Old Solutions for New Problems
Drug Repurposing in Non-Small Cell Lung Carcinoma: Old Solutions for New Problems Abstract Abstract Lung cancer is the second most common cancer and the leading cause of cancer-related deaths in 2022. The majority (80%) of lung cancer cases belong to the non-small cell lung carcinoma (NSCLC) subtype. Despite the increa...
PMC4235214
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QseC Inhibitors as an Antivirulence Approach for Gram-Negative Pathogens
QseC Inhibitors as an Antivirulence Approach for Gram-Negative Pathogens Abstract ABSTRACT Invasive pathogens interface with the host and its resident microbiota through interkingdom signaling. The bacterial receptor QseC, which is a membrane-bound histidine sensor kinase, responds to the host stress hormones epinephri...
PMC6068960
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Methadone for Analgesia in Children with Life-Limiting Illness: Experience from a Tertiary Children’s Health Service
Methadone for Analgesia in Children with Life-Limiting Illness: Experience from a Tertiary Children’s Health Service Abstract Abstract Methadone has the potential to assist in the management of pain in children with life-limiting illness, but its use is limited by its complex pharmacokinetic profile and limited researc...
PMC8044591
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Monepantel pharmaco-therapeutic evaluation in cattle: Pattern of efficacy against multidrug resistant nematodes
Monepantel pharmaco-therapeutic evaluation in cattle: Pattern of efficacy against multidrug resistant nematodes Abstract The goal of the current work was to perform an integrated evaluation of monepantel (MNP) pharmacokinetics (PK) and pharmacodynamics, measured as anthelmintic efficacy, after its oral administration t...
PMC10051726
core_pubmed_pmc
What Is the Best Vancomycin Therapeutic Drug Monitoring Parameter to Assess Efficacy? A Critical Review of Experimental Data and Assessment of the Need for Individual Patient Minimum Inhibitory Concentration Value
What Is the Best Vancomycin Therapeutic Drug Monitoring Parameter to Assess Efficacy? A Critical Review of Experimental Data and Assessment of the Need for Individual Patient Minimum Inhibitory Concentration Value Abstract Abstract Therapeutic drug monitoring is recommended for the use of vancomycin, but a recent widel...
PMC8169765
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Harnessing PET to track micro- and nanoplastics in vivo
Harnessing PET to track micro- and nanoplastics in vivo Abstract Abstract The proliferation of plastics in the environment continues at an alarming rate. Plastic particles have been found to be persistent and ubiquitous pollutants in a variety of environments, including sea water, fresh water, soil, and air. In light o...
PMC9133015
core_pubmed_pmc
Targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 with a highly selective inhibitor for the treatment of prostate cancer
Targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 with a highly selective inhibitor for the treatment of prostate cancer Abstract Abstract Prostate cancer (PCa) is one of the most prevalent cancers in men worldwide, and hormonal therapy plays a key role in the treatment of PCa. However, the drug re...
PMC8484140
core_pubmed_pmc
Phase I Study and Pilot Efficacy Analysis of Entinostat, a Novel Histone Deacetylase Inhibitor, in Chinese Postmenopausal Women with Hormone Receptor-Positive Metastatic Breast Cancer
Phase I Study and Pilot Efficacy Analysis of Entinostat, a Novel Histone Deacetylase Inhibitor, in Chinese Postmenopausal Women with Hormone Receptor-Positive Metastatic Breast Cancer Abstract Abstract Background Previous clinical trials have demonstrated that entinostat in combination with exemestane had good tolerabi...
PMC7985749
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First-in-Human Randomized Trial to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the KDM1A Inhibitor Vafidemstat
First-in-Human Randomized Trial to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the KDM1A Inhibitor Vafidemstat Abstract Abstract Background Vafidemstat, an inhibitor of the histone lysine-specific demethylase KDM1A, corrects cognition deficits and behavior alterations in rodent models. Here, w...
PMC3303559
core_pubmed_pmc
Nevirapine-Based Antiretroviral Therapy Impacts Artesunate and Dihydroartemisinin Disposition in HIV-Infected Nigerian Adults
Nevirapine-Based Antiretroviral Therapy Impacts Artesunate and Dihydroartemisinin Disposition in HIV-Infected Nigerian Adults Abstract Background . Nevirapine- (NVP-) based antiretroviral therapy (ART) and artesunate-amodiaquine are frequently coprescribed in areas of HIV and malaria endemicity. We explored the impact ...
PMC6929178
core_pubmed_pmc
Model Optimization and In Silico Analysis of Potential Dipeptidyl Peptidase IV Antagonists from GC-MS Identified Compounds in Nauclea latifolia Leaf Extracts
Model Optimization and In Silico Analysis of Potential Dipeptidyl Peptidase IV Antagonists from GC-MS Identified Compounds in Nauclea latifolia Leaf Extracts Abstract Dipeptidyl peptidase IV (DPP-IV) is a pharmacotherapeutic target in type 2 diabetes. Inhibitors of this enzyme constitute a new class of drugs used in th...
PMC10647374
core_pubmed_pmc
Improving the Biological Properties of Thrombin-Binding Aptamer by Incorporation of 8-Bromo-2′-Deoxyguanosine and 2′-Substituted RNA Analogues
Improving the Biological Properties of Thrombin-Binding Aptamer by Incorporation of 8-Bromo-2′-Deoxyguanosine and 2′-Substituted RNA Analogues Abstract Thrombin-binding aptamer (TBA) is one of the best-known G-quadruplex (G4)-forming aptamers. By adopting its peculiar chair-like G4 structure, TBA can efficiently bind t...
PMC8903831
core_pubmed_pmc
Gut microbiota induces high platelet response in patients with ST segment elevation myocardial infarction after ticagrelor treatment
Gut microbiota induces high platelet response in patients with ST segment elevation myocardial infarction after ticagrelor treatment Abstract Abstract Background: Ticagrelor is a first-line drug for the treatment of acute ST elevation myocardial infarction (STEMI). However, approximately 20% STEMI patients taking ticag...
PMC11025818
core_pubmed_pmc
Decreased risk of underdosing with continuous infusion versus intermittent administration of cefotaxime in patients with sickle cell disease and acute chest syndrome
Decreased risk of underdosing with continuous infusion versus intermittent administration of cefotaxime in patients with sickle cell disease and acute chest syndrome Abstract Objective Underdosing of antibiotics is common in patients with sickle cell disease (SCD). We hypothesized that in critically-ill patients with S...
PMC9032762
core_pubmed_pmc
Role of the Antioxidant Activity of Melatonin in Myocardial Ischemia-Reperfusion Injury
Role of the Antioxidant Activity of Melatonin in Myocardial Ischemia-Reperfusion Injury Abstract Abstract Ischemia-reperfusion injury is a common problem in the age of interventional cardiology; it is primarily mediated by oxidative stress and reactive agents. Melatonin has antioxidative properties that make its use pr...
PMC8653660
core_pubmed_pmc
Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation
Improved Ocular Bioavailability of Moxifloxacin HCl using PLGA Nanoparticles: Fabrication, Characterization, In-vitro and In-vivo Evaluation Abstract Abstract Improving the bioavailability of a drug at the ocular surface presents a profound challenge. Due to ocular physiological barriers, conventional eye drops exhibit...
PMC4905153
core_pubmed_pmc
Extended-Interval Aminoglycoside Use in Cystic Fibrosis Exacerbation in Children and Young Adults
Extended-Interval Aminoglycoside Use in Cystic Fibrosis Exacerbation in Children and Young Adults Abstract Abstract This is a prospective quality improvement project for patients with cystic fibrosis who are 5 years of age and older who were admitted for intravenous antibiotic administration as part of treatment of cys...
PMC4274041
core_pubmed_pmc
Impact of crystal polymorphism on the systemic bioavailability of rifaximin, an antibiotic acting locally in the gastrointestinal tract, in healthy volunteers
Impact of crystal polymorphism on the systemic bioavailability of rifaximin, an antibiotic acting locally in the gastrointestinal tract, in healthy volunteers Abstract Abstract Background Rifaximin is an antibiotic, acting locally in the gastrointestinal tract, which may exist in different crystal as well as amorphous ...
PMC12159257
core_pubmed_pmc
Sodium-glucose co-transporter 2 inhibitors: Prospects for canine myxomatous mitral valve disease and finding the “right drug” and the “right dose” for dogs
Sodium-glucose co-transporter 2 inhibitors: Prospects for canine myxomatous mitral valve disease and finding the “right drug” and the “right dose” for dogs Abstract Abstract Human pharmaceuticals are widely used in veterinary medicine. Nevertheless, identifying the optimal pharmaceuticals and dosages has been a signifi...
PMC9977795
core_pubmed_pmc
Protective effect of compatible herbs in Jin-Gu-Lian formula against Alangium chinense -induced neurotoxicity via oxidative stress, neurotransmitter metabolisms, and pharmacokinetics
Protective effect of compatible herbs in Jin-Gu-Lian formula against Alangium chinense -induced neurotoxicity via oxidative stress, neurotransmitter metabolisms, and pharmacokinetics Abstract Background: A. chinense frequently used in Miao medicine to treat rheumatic diseases. However, as a famous toxic herb, Alangium ...
PMC3065561
core_pubmed_pmc
A multidisciplinary approach to improve drug therapy in nursing homes
A multidisciplinary approach to improve drug therapy in nursing homes Abstract Management of drug therapy in nursing home patients is challenging due to complex health problems, use of multiple medications, and age-related changes in pharmacokinetics and pharmacodynamics. The objective of this study was, first, to exam...
PMC11429240
core_pubmed_pmc
Application of Physiologically Based Pharmacokinetic Model to Delineate the Impact of Aging and Renal Impairment on Ceftazidime Clearance
Application of Physiologically Based Pharmacokinetic Model to Delineate the Impact of Aging and Renal Impairment on Ceftazidime Clearance Abstract Abstract The impact of physiological changes during aging on drug disposition has not always been thoroughly assessed in clinical studies. This has left an open question suc...
PMC5627750
core_pubmed_pmc
Protective effects on myocardial infarction model: delivery of schisandrin B using matrix metalloproteinase-sensitive peptide-modified, PEGylated lipid nanoparticles
Protective effects on myocardial infarction model: delivery of schisandrin B using matrix metalloproteinase-sensitive peptide-modified, PEGylated lipid nanoparticles Abstract Abstract Purpose Schisandrin B (Sch B) is clinically applied for the treatment of hepatitis and ischemic disease. However, its clinical efficacy ...
PMC10095456
core_pubmed_pmc
Developing a Warning Model of Potentially Inappropriate Medications in Older Chinese Outpatients in Tertiary Hospitals: A Machine-Learning Study
Developing a Warning Model of Potentially Inappropriate Medications in Older Chinese Outpatients in Tertiary Hospitals: A Machine-Learning Study Abstract Due to multiple comorbid illnesses, polypharmacy, and age-related changes in pharmacokinetics and pharmacodynamics in older adults, the prevalence of potentially inap...
PMC8074046
core_pubmed_pmc
Evaluation of the MeroRisk Calculator, A User-Friendly Tool to Predict the Risk of Meropenem Target Non-Attainment in Critically Ill Patients
Evaluation of the MeroRisk Calculator, A User-Friendly Tool to Predict the Risk of Meropenem Target Non-Attainment in Critically Ill Patients Abstract Abstract Background: The MeroRisk-calculator, an easy-to-use tool to determine the risk of meropenem target non-attainment after standard dosing (1000 mg; q8h), uses a p...
PMC5480250
core_pubmed_pmc
Tralokinumab pharmacokinetics and tolerability when administered by different subcutaneous injection methods and rates
Tralokinumab pharmacokinetics and tolerability when administered by different subcutaneous injection methods and rates Abstract Abstract Objective: Tralokinumab, administered as two 1-mL subcutaneous injections every 2 weeks, at the target dose 300 mg, has been shown to improve lung function in patients with asthma. Th...
PMC7136079
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of a fixed-dose combination of gemigliptin/metformin sustained release 25/500 mg compared to the loose combination in healthy male subjects
Pharmacokinetics and pharmacodynamics of a fixed-dose combination of gemigliptin/metformin sustained release 25/500 mg compared to the loose combination in healthy male subjects Abstract A fixed-dose combination (FDC) of gemigliptin/metformin can improve the medication adherence in patients with type 2 diabetes mellitu...
PMC12459307
core_pubmed_pmc
Innovative Chitosan‐Based Formulation for Controlled Release of Enrofloxacin: Pharmacokinetic Analysis in Rabbits
Innovative Chitosan‐Based Formulation for Controlled Release of Enrofloxacin: Pharmacokinetic Analysis in Rabbits Abstract ABSTRACT The present study was conducted to evaluate the pharmacokinetics (PK) of a novel triple‐layer formulation of enrofloxacin (ENR) compared to a conventional ENR formulation following subcuta...
PMC5376397
core_pubmed_pmc
The multistate tuberculosis pharmacometric model: a semi-mechanistic pharmacokinetic-pharmacodynamic model for studying drug effects in an acute tuberculosis mouse model
The multistate tuberculosis pharmacometric model: a semi-mechanistic pharmacokinetic-pharmacodynamic model for studying drug effects in an acute tuberculosis mouse model Abstract The Multistate Tuberculosis Pharmacometric (MTP) model, a pharmacokinetic-pharmacodynamic disease model, has been used to describe the effect...
PMC12353614
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Predicting Maternal and Fetal Exposures of Elexacaftor–Tezacaftor–Ivacaftor during Pregnancy through Physiologically Based Pharmacokinetic Models
Predicting Maternal and Fetal Exposures of Elexacaftor–Tezacaftor–Ivacaftor during Pregnancy through Physiologically Based Pharmacokinetic Models Abstract The use of elexacaftor/tezacaftor/ivacaftor (ETI) has been associated with increased fertility in women with cystic fibrosis (CF) and is increasingly used during pre...
PMC6912361
core_pubmed_pmc
Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition
Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition Abstract Abstract CDK8/19 kinases, which mediate transcriptional reprogramming, have become an active target for cancer drug discovery. Several small-molecule CDK8/19 inhibitors showed in vivo efficacy and two hav...
PMC9197530
core_pubmed_pmc
Model‐informed drug development of voxelotor in sickle cell disease: Population pharmacokinetics in whole blood and plasma
Model‐informed drug development of voxelotor in sickle cell disease: Population pharmacokinetics in whole blood and plasma Abstract Abstract Oxbryta (voxelotor) is a small‐molecule inhibitor of sickle hemoglobin (Hb) polymerization approved for patients with sickle cell disease (SCD) aged greater than or equal to 12 ye...
PMC9800282
core_pubmed_pmc
Angiopoietin-like 3-derivative LNA043 for cartilage regeneration in osteoarthritis: a randomized phase 1 trial
Angiopoietin-like 3-derivative LNA043 for cartilage regeneration in osteoarthritis: a randomized phase 1 trial Abstract Osteoarthritis (OA) is a common, debilitating, chronic disease with no disease-modifying drug approved to date. We discovered LNA043—a derivative of angiopoietin-like 3 (ANGPTL3)—as a potent chondroge...
PMC11556718
core_pubmed_pmc
Pembrolizumab 400 mg every 6 weeks as first-line therapy for advanced melanoma (KEYNOTE-555): Results from cohort B of an open-label, phase 1 study
Pembrolizumab 400 mg every 6 weeks as first-line therapy for advanced melanoma (KEYNOTE-555): Results from cohort B of an open-label, phase 1 study Abstract Abstract Intravenous pembrolizumab 400 mg every 6 weeks was approved across tumor types based on pharmacokinetic modeling, which showed exposures consistent with p...
PMC9643841
core_pubmed_pmc
Nontargeted metabolomics study and pharmacodynamic evaluation of bidirectional fermentation for Ganoderma lucidum with Marsdenia tenacissima
Nontargeted metabolomics study and pharmacodynamic evaluation of bidirectional fermentation for Ganoderma lucidum with Marsdenia tenacissima Abstract Lung cancer is one of the malignant tumors with the fastest incidence rate and mortality growth and the greatest threat to human health and life. Marsdenia tenacissima is...
PMC11881042
core_pubmed_pmc
Network-Based Drug Optimization toward the Treatment of Parkinson’s Disease: NRF2, MAO-B, Oxidative Stress, and Chronic Neuroinflammation
Network-Based Drug Optimization toward the Treatment of Parkinson’s Disease: NRF2, MAO-B, Oxidative Stress, and Chronic Neuroinflammation Abstract Abstract Parkinson’s disease (PD), the second most common neurodegenerative disorder, affects around 10 million people worldwide. It is a multifactorial disease marked by do...
PMC4826489
core_pubmed_pmc
Comparison of the Pharmacokinetics of Nicotine Following Single and Ad Libitum Use of a Tobacco Heating System or Combustible Cigarettes
Comparison of the Pharmacokinetics of Nicotine Following Single and Ad Libitum Use of a Tobacco Heating System or Combustible Cigarettes Abstract Introduction: We aimed to compare the pharmacokinetics of nicotine between the heat-not-burn Tobacco Heating System 2.1 (THS 2.1) and combustible cigarettes (CCs). We also ex...
PMC11967363
core_pubmed_pmc
Coumarins from Citrus aurantiifolia (Christm.) Swingle Peel with Potential Cytotoxic Activity Against MCF-7 Breast Cancer Cell Line: In Vitro and In Silico Studies
Coumarins from Citrus aurantiifolia (Christm.) Swingle Peel with Potential Cytotoxic Activity Against MCF-7 Breast Cancer Cell Line: In Vitro and In Silico Studies Abstract Aim Breast cancer remains a prevalent and challenging health issue for women globally. In the pursuit of more effective and less harmful therapies,...