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PMC8143174
core_pubmed_pmc
Laboratory Monitoring of Direct Oral Anticoagulants (DOACs)
Laboratory Monitoring of Direct Oral Anticoagulants (DOACs) Abstract The introduction of direct oral anticoagulants (DOACs), such as dabigatran, rivaroxaban, apixaban, edoxaban, and betrixaban, provides safe and effective alternative to previous anticoagulant therapies. DOACs directly, selectively, and reversibly inhib...
PMC6810667
core_pubmed_pmc
Higher MICs (>2 mg/L) Predict 30-Day Mortality in Patients With Lower Respiratory Tract Infections Caused by Multidrug- and Extensively Drug-Resistant Pseudomonas aeruginosa Treated With Ceftolozane/Tazobactam
Higher MICs (>2 mg/L) Predict 30-Day Mortality in Patients With Lower Respiratory Tract Infections Caused by Multidrug- and Extensively Drug-Resistant Pseudomonas aeruginosa Treated With Ceftolozane/Tazobactam Abstract Abstract Background Ceftolozane/tazobactam (C/T) efficacy and safety in ventilator-associated pneumon...
PMC6819847
core_pubmed_pmc
Computational and spectral studies of 3,3'-(propane-1,3-diyl)bis(7,8-dimethoxy-1,3,4,5-tetrahydro-2H-benzo[d]azepin-2-one)
Computational and spectral studies of 3,3'-(propane-1,3-diyl)bis(7,8-dimethoxy-1,3,4,5-tetrahydro-2H-benzo[d]azepin-2-one) Abstract Detection and qualification of unknown impurities during commercial drug synthesis have been mandated by the regulatory authorities. 3,3'-(propane-1,3-diyl)bis(7,8-dimethoxy-1,3,4,5-tetrah...
PMC11872518
core_pubmed_pmc
Palbociclib exposure in relation to efficacy and toxicity in patients with advanced breast cancer
Palbociclib exposure in relation to efficacy and toxicity in patients with advanced breast cancer Abstract Abstract Background Data on exposure–response or exposure–toxicity relationships of cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) are limited and inconclusive. We aimed to investigate whether there is an associ...
PMC11678214
core_pubmed_pmc
Rationale and Logistics of Continuous Infusion Cephalosporin Antibiotics
Rationale and Logistics of Continuous Infusion Cephalosporin Antibiotics Abstract Cephalosporins have traditionally been administered as an intermittent infusion. With the knowledge that cephalosporins demonstrate a time-dependent pharmacodynamic profile, administration via continuous infusion may provide more effectiv...
PMC5315738
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Afatinib
Clinical Pharmacokinetics and Pharmacodynamics of Afatinib Abstract Afatinib is an oral, irreversible ErbB family blocker that covalently binds to the kinase domains of epidermal growth factor receptor (EGFR), human EGFRs (HER) 2, and HER4, resulting in irreversible inhibition of tyrosine kinase autophosphorylation. St...
PMC11500426
core_pubmed_pmc
Development of a Physiologically Based Pharmacokinetic (PBPK) Model for F-53B in Pregnant Mice and Its Extrapolation to Humans
Development of a Physiologically Based Pharmacokinetic (PBPK) Model for F-53B in Pregnant Mice and Its Extrapolation to Humans Abstract Abstract Chlorinated polyfluorinated ether sulfonic acid (F-53B), a commonly utilized alternative for perfluorooctane sulfonate, was detected in pregnant women and cord blood recently....
PMC9909267
core_pubmed_pmc
Multicenter review of a tadalafil suspension formulation for infants and children with pulmonary hypertension: A North American experience
Multicenter review of a tadalafil suspension formulation for infants and children with pulmonary hypertension: A North American experience Abstract Introduction Phosphodiesterase type 5 (PDE5) inhibitors, with sildenafil the earliest among them, are widely used in the management of pediatric pulmonary arterial hyperten...
PMC11742092
core_pubmed_pmc
UPLC-MS/MS Method for Givinostat in Rat Plasma: Development, Validation, in vivo Pharmacokinetics Study and in vitro Metabolic Stability Research
UPLC-MS/MS Method for Givinostat in Rat Plasma: Development, Validation, in vivo Pharmacokinetics Study and in vitro Metabolic Stability Research Abstract Abstract Background Givinostat, a potent histone deacetylase (HDAC) inhibitor, is promising for the treatment of relapsed leukemia and myeloma. Purpose This study ai...
PMC7383509
core_pubmed_pmc
The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Oliceridine
The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Oliceridine Abstract Abstract Oliceridine is a G protein–biased ligand at the μ‐opioid receptor in development for treatment of moderate to severe acute pain. A phase 1, open‐label, single‐dose study investigated the pharm...
PMC12383002
core_pubmed_pmc
Ceftazidime–Avibactam in Critically Ill Patients: A Multicenter Observational Study
Ceftazidime–Avibactam in Critically Ill Patients: A Multicenter Observational Study Abstract Abstract Ceftazidime–avibactam (CAZ-AVI) is a second-generation intravenous β-lactam/β-lactamase inhibitor combination. In recent years, substantial evidence has emerged regarding the efficacy and safety of CAZ-AVI. However, da...
PMC7993283
core_pubmed_pmc
Effect of Crohn’s Disease on Villous Length and CYP3A4 Expression in the Pediatric Small Intestine
Effect of Crohn’s Disease on Villous Length and CYP3A4 Expression in the Pediatric Small Intestine Abstract Changes in absorptive capacity and first‐pass metabolism in the small intestine affect oral drug bioavailability. Characterization of such changes as a consequence of inflammation is important for developing phys...
PMC10098839
core_pubmed_pmc
Single‐dose pharmacokinetics of telmisartan oral solution and effect of feeding in dogs
Single‐dose pharmacokinetics of telmisartan oral solution and effect of feeding in dogs Abstract Abstract Telmisartan is an angiotensin II receptor blocker that has great potential to improve the treatment of hypertension, proteinuria, and cardiovascular disease in dogs. A feline‐approved telmisartan oral solution (TOS...
PMC6048694
core_pubmed_pmc
Knowledge is power: general practitioners prescribing of new oral anticoagulants in Ireland
Knowledge is power: general practitioners prescribing of new oral anticoagulants in Ireland Abstract Abstract Objective New oral anticoagulants (NOACs) aim to overcome warfarin’s shortcomings, however their pharmacokinetic characteristics make prescribing complex. Thus it is imperative that general practitioners (GPs) ...
PMC3927193
core_pubmed_pmc
Pregabalin-associated myoclonic encephalopathy without evidence of drug accumulation in a patient with acute renal failure
Pregabalin-associated myoclonic encephalopathy without evidence of drug accumulation in a patient with acute renal failure Abstract Abstract Pregabalin, used for treating partial epilepsy and neuropathic pain, is usually well tolerated. Patients with impaired renal function are at risk to develop more serious adverse e...
PMC4478358
core_pubmed_pmc
L-Dopa Pharmacokinetic Profile with Effervescent Melevodopa/Carbidopa versus Standard-Release Levodopa/Carbidopa Tablets in Parkinson's Disease: A Randomised Study
L-Dopa Pharmacokinetic Profile with Effervescent Melevodopa/Carbidopa versus Standard-Release Levodopa/Carbidopa Tablets in Parkinson's Disease: A Randomised Study Abstract Abstract Objectives. To characterize the pharmacokinetic profile of levodopa (L-dopa) and carbidopa after repeated doses of the effervescent tablet...
PMC10975701
core_pubmed_pmc
PK Modeling of L-4-Boronophenylalanine and Development of Bayesian Predictive Platform for L-4-Boronophenylalanine PKs for Boron Neutron Capture Therapy
PK Modeling of L-4-Boronophenylalanine and Development of Bayesian Predictive Platform for L-4-Boronophenylalanine PKs for Boron Neutron Capture Therapy Abstract Abstract L-4-[( 10 B)]Boronophenylalanine (BPA) is an amino acid analogue with a boron-10 moiety. It is most widely used as a boron carrier in boron neutron c...
PMC6141109
core_pubmed_pmc
Pharmacokinetics of evocalcet in secondary hyperparathyroidism patients receiving hemodialysis: first-in-patient clinical trial in Japan
Pharmacokinetics of evocalcet in secondary hyperparathyroidism patients receiving hemodialysis: first-in-patient clinical trial in Japan Abstract Abstract Purpose Cinacalcet is a positive allosteric modulator of calcium-sensing receptors in the parathyroid gland and an effective treatment for secondary hyperparathyroid...
PMC6035379
core_pubmed_pmc
Effect of Korean Red Ginseng extracts on drug-drug interactions
Effect of Korean Red Ginseng extracts on drug-drug interactions Abstract Abstract Background Ginseng has been the subject of many experimental and clinical studies to uncover the diverse biological activities of its constituent compounds. It is a traditional medicine that has been used for its immunostimulatory, antith...
PMC9695321
core_pubmed_pmc
Aptamer-Based Probes for Cancer Diagnostics and Treatment
Aptamer-Based Probes for Cancer Diagnostics and Treatment Abstract Abstract Aptamers are single-stranded DNA or RNA oligomers that have the ability to generate unique and diverse tertiary structures that bind to cognate molecules with high specificity. In recent years, aptamer researches have witnessed a huge surge, ow...
PMC11434876
core_pubmed_pmc
Drug–Drug Interactions in Nosocomial Infections: An Updated Review for Clinicians
Drug–Drug Interactions in Nosocomial Infections: An Updated Review for Clinicians Abstract Abstract Prevention, assessment, and identification of drug–drug interactions (DDIs) represent a challenge for healthcare professionals, especially in nosocomial settings. This narrative review aims to provide a thorough assessme...
PMC12786445
core_pubmed_pmc
Discovering the Anti-Inflammatory Potential of Compounds Isolated from the Aerial Parts of Gelasia tomentosa (L.) Zaika, Sukhor. & N.Kilian (Syn. Scorzonera tomentosa ), Through In Vitro Techniques and Advanced In Silico Modeling Approaches
Discovering the Anti-Inflammatory Potential of Compounds Isolated from the Aerial Parts of Gelasia tomentosa (L.) Zaika, Sukhor. & N.Kilian (Syn. Scorzonera tomentosa ), Through In Vitro Techniques and Advanced In Silico Modeling Approaches Abstract Abstract Gelasia tomentosa (L.) Zaika, Sukhor. & N.Kilian which is kno...
PMC7070709
core_pubmed_pmc
Design, Synthesis, and In Vitro Evaluation of Hydroxybenzimidazole-Donepezil Analogues as Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease
Design, Synthesis, and In Vitro Evaluation of Hydroxybenzimidazole-Donepezil Analogues as Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease Abstract A series of multi-target-directed ligands (MTDLs), obtained by attachment of a hydroxyphenylbenzimidazole (BIM) unit to donepezil (DNP) active mimetic ...
PMC12256768
core_pubmed_pmc
Unveiling the dual threat: combined elevated triglyceride-glucose index and intracranial arterial stenosis burden for enhanced stroke risk stratification
Unveiling the dual threat: combined elevated triglyceride-glucose index and intracranial arterial stenosis burden for enhanced stroke risk stratification Abstract Abstract Background The relationship between an elevated triglyceride-glucose index (TyG) combined with intracranial arterial stenosis (ICAS) and stroke recu...
PMC4425807
core_pubmed_pmc
Investigating interactions between phentermine, dexfenfluramine, and 5-HT 2C agonists, on food intake in the rat
Investigating interactions between phentermine, dexfenfluramine, and 5-HT 2C agonists, on food intake in the rat Abstract Rationale Synergistic or supra-additive interactions between the anorectics (dex)fenfluramine and phentermine have been reported previously in the rat and in the clinic. Studies with 5-HT 2C antagon...
PMC3969253
core_pubmed_pmc
In silico structure-based screening of versatile P-glycoprotein inhibitors using polynomial empirical scoring functions
In silico structure-based screening of versatile P-glycoprotein inhibitors using polynomial empirical scoring functions Abstract P-glycoprotein (P-gp) is an ATP (adenosine triphosphate)-binding cassette transporter that causes multidrug resistance of various chemotherapeutic substances by active efflux from mammalian c...
PMC9045709
core_pubmed_pmc
The Efficacy of a Didactic and Case-Based Pharmacogenomics Education Program on Improving the Knowledge and Confidence of Alberta Pharmacists
The Efficacy of a Didactic and Case-Based Pharmacogenomics Education Program on Improving the Knowledge and Confidence of Alberta Pharmacists Abstract Background Pharmacogenomics (PGx) is the study of how genetic variations for functional proteins, such as metabolizing enzymes and drug receptors, impact drug pharmacoki...
PMC7894397
core_pubmed_pmc
A population pharmacokinetics analysis assessing the exposure of raltegravir once‐daily 1200 mg in pregnant women living with HIV
A population pharmacokinetics analysis assessing the exposure of raltegravir once‐daily 1200 mg in pregnant women living with HIV Abstract Abstract Once‐daily two 600 mg tablets (1200 mg q.d.) raltegravir offers an easier treatment option compared to the twice‐daily regimen of one 400 mg tablet. No pharmacokinetic, eff...
PMC5677780
core_pubmed_pmc
Pharmacokinetic profile and partitioning in red blood cells of romifidine after single intravenous administration in the horse
Pharmacokinetic profile and partitioning in red blood cells of romifidine after single intravenous administration in the horse Abstract Abstract The aims of this study were to assess the plasma concentrations of romifidine in horses after intravenous injection, to evaluate the red blood cell ( RBC ) partitioning of the...
PMC6469740
core_pubmed_pmc
Objective measures of non-adherence in cardiometabolic diseases: a review focused on urine biochemical screening
Objective measures of non-adherence in cardiometabolic diseases: a review focused on urine biochemical screening Abstract Abstract Cardiometabolic diseases are among the most prevalent and harmful conditions worldwide. They are complex, comorbid conditions that require polypharmacy – a known contributor to non-adherenc...
PMC6521709
core_pubmed_pmc
Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis -infected BALB/c mice
Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis -infected BALB/c mice Abstract Abstract Background: Cutaneous leishmaniasis (CL) is a parasitic disease caused by the protozoan Leishmania spp. Pentavalent antimonial agents have been used as an effective therapy, despite their side ...
PMC12559684
core_pubmed_pmc
Repurposing Existing Drugs for the Treatment of Post-Traumatic Stress Disorder
Repurposing Existing Drugs for the Treatment of Post-Traumatic Stress Disorder Abstract Abstract Chronic stress and traumatic events affect the psychological and physiological state of a person. Post-traumatic stress disorder (PTSD) is a type of psychological stress that occurs in critical situations that pose a direct...
PMC6611588
core_pubmed_pmc
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors Abstract CD47 is an immune checkpoint molecule that downregulates key aspects of both the innate and adaptive anti-tumor immune response via its counter receptor SIRPα, and it is expressed at high levels...
PMC10386912
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of the Next Generation Androgen Receptor Inhibitor—Darolutamide
Clinical Pharmacokinetics and Pharmacodynamics of the Next Generation Androgen Receptor Inhibitor—Darolutamide Abstract Abstract Darolutamide is a next-generation androgen receptor signaling inhibitor (ARSI) currently approved for the treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC) and metastat...
PMC9411058
core_pubmed_pmc
Pharmacometric approach to assist dosage regimen design in neonates undergoing therapeutic hypothermia
Pharmacometric approach to assist dosage regimen design in neonates undergoing therapeutic hypothermia Abstract Background Therapeutic hypothermia (TH) is the treatment of choice for neonates diagnosed with perinatal asphyxia (PA). Dosing recommendations of various therapeutic agents including antimicrobials were not s...
PMC7071312
core_pubmed_pmc
Erythrocyte Ascorbate Is a Potential Indicator of Steady-State Plasma Ascorbate Concentrations in Healthy Non-Fasting Individuals
Erythrocyte Ascorbate Is a Potential Indicator of Steady-State Plasma Ascorbate Concentrations in Healthy Non-Fasting Individuals Abstract Plasma vitamin C concentrations fluctuate in response to recent dietary intake; therefore levels are typically determined in the fasting state. Erythrocyte ascorbate concentrations ...
PMC4622731
core_pubmed_pmc
Generation and characterization of ABT-981, a dual variable domain immunoglobulin (DVD-Ig TM ) molecule that specifically and potently neutralizes both IL-1α and IL-1β
Generation and characterization of ABT-981, a dual variable domain immunoglobulin (DVD-Ig TM ) molecule that specifically and potently neutralizes both IL-1α and IL-1β Abstract Interleukin-1 (IL-1) cytokines such as IL-1α, IL-1β, and IL-1Ra contribute to immune regulation and inflammatory processes by exerting a wide r...
PMC6977279
core_pubmed_pmc
Pharmacokinetics and pharmacodynamic effect of crenezumab on plasma and cerebrospinal fluid beta-amyloid in patients with mild-to-moderate Alzheimer’s disease
Pharmacokinetics and pharmacodynamic effect of crenezumab on plasma and cerebrospinal fluid beta-amyloid in patients with mild-to-moderate Alzheimer’s disease Abstract Background Crenezumab, a fully humanized anti-beta-amyloid (Aβ) immunoglobulin G4 (IgG4) monoclonal antibody, binds to both monomeric and aggregated for...
PMC9821414
core_pubmed_pmc
Drug-drug interaction and acute kidney injury development: A correlation-based network analysis
Drug-drug interaction and acute kidney injury development: A correlation-based network analysis Abstract Abstract Background Drug-induced nephrotoxicity is a relatively common preventable cause of acute kidney injury (AKI), providing early recognition and management. The pharmacokinetics or pharmacodynamics of drug-dru...
PMC10328871
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Recombinant Human Neuregulin-1 in Healthy Chinese Subjects
Safety, Tolerability, and Pharmacokinetics of Recombinant Human Neuregulin-1 in Healthy Chinese Subjects Abstract Abstract Background We investigated the safety, tolerability, and pharmacokinetics of intravenous recombinant human Neuregulin-1 (rhNRG-1), a DNA recombinant protein for the treatment of chronic heart failu...
PMC7586797
core_pubmed_pmc
Phase 1 Study to Evaluate the Effect of the Investigational Anticancer Agent Sapanisertib on the QTc Interval in Patients With Advanced Solid Tumors
Phase 1 Study to Evaluate the Effect of the Investigational Anticancer Agent Sapanisertib on the QTc Interval in Patients With Advanced Solid Tumors Abstract Abstract The aim of this phase 1 study was to determine the effects of sapanisertib on the heart rate–corrected QT (QTc) interval in patients with advanced solid ...
PMC6104801
core_pubmed_pmc
Development of a population pharmacokinetic model of olanzapine for Chinese health volunteers and patients with schizophrenia
Development of a population pharmacokinetic model of olanzapine for Chinese health volunteers and patients with schizophrenia Abstract Objective Olanzapine is an atypical antipsychotic drug commonly used for the treatment of schizophrenia. However, there are still many complications associated with the use of olanzapin...
PMC10187793
core_pubmed_pmc
Corticosteroid–Antibiotic Interactions in Bacteria that Cause Corneal Infection
Corticosteroid–Antibiotic Interactions in Bacteria that Cause Corneal Infection Abstract Abstract Purpose Although a comprehensive knowledge of antibiotic/corticosteroid combinations is essential for the appropriate treatment of eye infections, the impact of their co-administration has not been well studied to date. A ...
PMC9891290
core_pubmed_pmc
Platelet-Mimicking Nanosponges for Functional Reversal of Antiplatelet Agents
Platelet-Mimicking Nanosponges for Functional Reversal of Antiplatelet Agents Abstract Background: During long-term antiplatelet agents (APAs) administration, patients with thrombotic diseases take a fairly high risk of life-threatening bleeding, especially when in need of urgent surgery. Rapid functional reversal of A...
PMC10819729
core_pubmed_pmc
Systemic and Brain Pharmacokinetics of Milnacipran in Mice: Comparison of Intraperitoneal and Intravenous Administration
Systemic and Brain Pharmacokinetics of Milnacipran in Mice: Comparison of Intraperitoneal and Intravenous Administration Abstract Milnacipran is a dual serotonin and norepinephrine reuptake inhibitor, clinically used for the treatment of major depression or fibromyalgia. Currently, there are no studies reporting the ph...
PMC7533164
core_pubmed_pmc
Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling
Qualification and application of liquid chromatography-quadrupole time-of-flight mass spectrometric method for the determination of carisbamate in rat plasma and prediction of its human pharmacokinetics using physiologically based pharmacokinetic modeling Abstract Abstract Carisbamate is an antiepileptic drug and it al...
PMC12575765
core_pubmed_pmc
Synergistic effects of colistin-based combinations against colistin and carbapenem-resistant Klebsiella pneumoniae isolated from nosocomial bloodstream infections
Synergistic effects of colistin-based combinations against colistin and carbapenem-resistant Klebsiella pneumoniae isolated from nosocomial bloodstream infections Abstract The emergence of colistin and carbapenem-resistant Klebsiella pneumoniae (CRCR-KP) poses a critical challenge in treating bloodstream infections. As...
PMC12030428
core_pubmed_pmc
Pharmacokinetics of Psilocybin: A Systematic Review
Pharmacokinetics of Psilocybin: A Systematic Review Abstract Abstract Background: Psilocybin has shown promise in therapeutic applications for mental disorders. Understanding the pharmacokinetics of psilocybin and its active metabolite psilocin is crucial for optimizing its clinical use and minimizing adverse effects. ...
PMC6451721
core_pubmed_pmc
Population Pharmacokinetics of Fludarabine in Children and Adults during Conditioning Prior to Allogeneic Hematopoietic Cell Transplantation
Population Pharmacokinetics of Fludarabine in Children and Adults during Conditioning Prior to Allogeneic Hematopoietic Cell Transplantation Abstract Background Fludarabine is often used as an important drug in reduced toxicity conditioning regimens prior to hematopoietic cell transplantation (HCT). As no definitive ph...
PMC9897045
core_pubmed_pmc
Novel Investigational Anti-SARS-CoV-2 Agent Ensitrelvir “S-217622”: A Very Promising Potential Universal Broad-Spectrum Antiviral at the Therapeutic Frontline of Coronavirus Species
Novel Investigational Anti-SARS-CoV-2 Agent Ensitrelvir “S-217622”: A Very Promising Potential Universal Broad-Spectrum Antiviral at the Therapeutic Frontline of Coronavirus Species Abstract Abstract Lately, nitrogenous heterocyclic antivirals, such as nucleoside-like compounds, oxadiazoles, thiadiazoles, triazoles, qu...
PMC12702981
core_pubmed_pmc
Population pharmacokinetics of efpeglenatide in individuals with obesity and with type 2 diabetes
Population pharmacokinetics of efpeglenatide in individuals with obesity and with type 2 diabetes Abstract Background Efpeglenatide (HM11260C) is a long-acting GLP-1 receptor agonist under development for obesity. A population pharmacokinetic (PK) analysis was conducted to characterize its PK properties and evaluate co...
PMC9866629
core_pubmed_pmc
Pharmacokinetics of Novel Furoxan/Coumarin Hybrids in Rats Using LC-MS/MS Method and Physiologically Based Pharmacokinetic Model
Pharmacokinetics of Novel Furoxan/Coumarin Hybrids in Rats Using LC-MS/MS Method and Physiologically Based Pharmacokinetic Model Abstract Abstract Novel furoxan/coumarin hybrids were synthesized, and pharmacologic studies showed that the compounds displayed potent antiproliferation activities via downregulating both th...
PMC7300220
core_pubmed_pmc
Initial Dosage Recommendation for Sirolimus in Children With Tuberous Sclerosis Complex
Initial Dosage Recommendation for Sirolimus in Children With Tuberous Sclerosis Complex Abstract Sirolimus is already used in the treatment of tuberous sclerosis complex (TSC), however, with narrow therapeutic range and considerable inter- and intra-individual pharmacokinetic variability, making it hard to develop an a...
PMC8443776
core_pubmed_pmc
Population Pharmacokinetics of Rituximab in Pediatric Patients With Frequent-Relapsing or Steroid-Dependent Nephrotic Syndrome
Population Pharmacokinetics of Rituximab in Pediatric Patients With Frequent-Relapsing or Steroid-Dependent Nephrotic Syndrome Abstract Abstract Objectives: Rituximab is frequently used off-label for the treatment of frequent-relapsing nephrotic syndrome (FRNS) or steroid-dependent nephrotic syndrome (SDNS), but the re...
PMC11843070
core_pubmed_pmc
Correlations of vancomycin trough concentration and its efficacy and toxicity in patients in the intensive care unit
Correlations of vancomycin trough concentration and its efficacy and toxicity in patients in the intensive care unit Abstract BACKGROUND Plasma concentration monitoring is crucial for optimizing vancomycin use, particularly in patients in the intensive care unit (ICU). However, the reference interval for vancomycin pla...
PMC11192707
core_pubmed_pmc
BOLERO-5: a phase II study of everolimus and exemestane combination in Chinese post-menopausal women with ER + /HER2- advanced breast cancer
BOLERO-5: a phase II study of everolimus and exemestane combination in Chinese post-menopausal women with ER + /HER2- advanced breast cancer Abstract Background The global BOLERO-2 trial established the efficacy and safety of combination everolimus (EVE) and exemestane (EXE) in the treatment of estrogen receptor positi...
PMC9840109
core_pubmed_pmc
Consecutive baicalin treatment relieves its accumulation in rats with intrahepatic cholestasis by increasing MRP2 expression
Consecutive baicalin treatment relieves its accumulation in rats with intrahepatic cholestasis by increasing MRP2 expression Abstract Abstract Baicalin, an important flavonoid isolated from Scutellaria baicalensis Georgi, is a Chinese herb widely used in clinical practice. We previously reported the in vivo accumulatio...
PMC5856873
core_pubmed_pmc
A Population Pharmacokinetic Model to Predict the Individual Starting Dose of Tacrolimus Following Pediatric Renal Transplantation
A Population Pharmacokinetic Model to Predict the Individual Starting Dose of Tacrolimus Following Pediatric Renal Transplantation Abstract Background Multiple clinical, demographic, and genetic factors affect the pharmacokinetics of tacrolimus in children, yet in daily practice, a uniform body-weight based starting do...
PMC8415218
core_pubmed_pmc
A pharmacokinetics‐based approach to the monitoring of patient adherence to atorvastatin therapy
A pharmacokinetics‐based approach to the monitoring of patient adherence to atorvastatin therapy Abstract Abstract The inadequate adherence of patients whose hyperlipidemia is treated with atorvastatin (ATR) to medical instructions presents a serious health risk. Our aim was to develop a flexible approach based on ther...
PMC3837842
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Considerations in Antimalarial Dose Optimization
Pharmacokinetic and Pharmacodynamic Considerations in Antimalarial Dose Optimization Abstract Antimalarial drugs have usually been first deployed in areas of malaria endemicity at doses which were too low, particularly for high-risk groups such as young children and pregnant women. This may accelerate the emergence and...
PMC5306091
core_pubmed_pmc
Pharmacokinetic and exposure–response analyses of pertuzumab in combination with trastuzumab and docetaxel during neoadjuvant treatment of HER2+ early breast cancer
Pharmacokinetic and exposure–response analyses of pertuzumab in combination with trastuzumab and docetaxel during neoadjuvant treatment of HER2+ early breast cancer Abstract Purpose The NeoSphere trial evaluated pertuzumab in the neoadjuvant setting [early breast cancer (EBC)] with pathological complete response (pCR) ...
PMC5548487
core_pubmed_pmc
Reverse translation of adverse event reports paves the way for de-risking preclinical off-targets
Reverse translation of adverse event reports paves the way for de-risking preclinical off-targets Abstract Abstract The Food and Drug Administration Adverse Event Reporting System (FAERS) remains the primary source for post-marketing pharmacovigilance. The system is largely un-curated, unstandardized, and lacks a metho...
PMC5766727
core_pubmed_pmc
Clinical Pharmacokinetic Characteristics of Cebranopadol, a Novel First-in-Class Analgesic
Clinical Pharmacokinetic Characteristics of Cebranopadol, a Novel First-in-Class Analgesic Abstract Abstract Background and Objectives Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clini...
PMC8585800
core_pubmed_pmc
Validation of a Population Pharmacokinetic Model of Vortioxetine Using Therapeutic Drug Monitoring Data
Validation of a Population Pharmacokinetic Model of Vortioxetine Using Therapeutic Drug Monitoring Data Abstract Introduction Vortioxetine is an antidepressant primarily metabolized by the polymorphic enzyme cytochrome P450 (CYP) 2D6. A population pharmacokinetic (popPK) model of vortioxetine and its CYP2D6-dependent m...
PMC9854442
core_pubmed_pmc
Pharmacokinetics of Antimicrobials in Children with Emphasis on Challenges Faced by Low and Middle Income Countries, a Clinical Review
Pharmacokinetics of Antimicrobials in Children with Emphasis on Challenges Faced by Low and Middle Income Countries, a Clinical Review Abstract Abstract Effective antimicrobial exposure is essential to treat infections and prevent antimicrobial resistance, both being major public health problems in low and middle incom...
PMC3852831
core_pubmed_pmc
Urodynamic investigation by telemetry in Beagle dogs: validation and effects of oral administration of current urological drugs: a pilot study
Urodynamic investigation by telemetry in Beagle dogs: validation and effects of oral administration of current urological drugs: a pilot study Abstract Abstract Background Vesico-urethral function may be evaluated in humans and dogs by conventional urodynamic testing (cystometry and urethral pressure profilometry) or b...
PMC9842066
core_pubmed_pmc
Implantable device actuated by manual button clicks for noninvasive self‐drug administration
Implantable device actuated by manual button clicks for noninvasive self‐drug administration Abstract Abstract Self‐injectable therapy has several advantages in the treatment of metabolic disorders. However, frequent injections with needles impair patient compliance and medication adherence. Therefore, we develop a ful...
PMC5080647
core_pubmed_pmc
Quantitative Prediction of Drug–Drug Interactions Involving Inhibitory Metabolites in Drug Development: How Can Physiologically Based Pharmacokinetic Modeling Help?
Quantitative Prediction of Drug–Drug Interactions Involving Inhibitory Metabolites in Drug Development: How Can Physiologically Based Pharmacokinetic Modeling Help? Abstract This subteam under the Drug Metabolism Leadership Group (Innovation and Quality Consortium) investigated the quantitative role of circulating inhi...
PMC7728077
core_pubmed_pmc
Double-Headed Cationic Lipopeptides: An Emerging Class of Antimicrobials
Double-Headed Cationic Lipopeptides: An Emerging Class of Antimicrobials Abstract Antimicrobial peptides (AMPs) constitute a promising tool in the development of novel therapeutic agents useful in a wide range of bacterial and fungal infections. Among the modifications improving pharmacokinetic and pharmacodynamic char...
PMC12238946
core_pubmed_pmc
First-in-human phase I open-label study of the anti–TIM-3 monoclonal antibody INCAGN02390 in patients with select advanced or metastatic solid tumors
First-in-human phase I open-label study of the anti–TIM-3 monoclonal antibody INCAGN02390 in patients with select advanced or metastatic solid tumors Abstract Abstract Background T-cell immunoglobulin and mucin domain-containing protein-3 (TIM-3) is an immune checkpoint receptor upregulated during anti-programmed death...
PMC12439282
core_pubmed_pmc
Competing Risks Analysis of the Finnish Diabetes Prevention Study
Competing Risks Analysis of the Finnish Diabetes Prevention Study Abstract ABSTRACT Clinical studies often observe one interesting event in the presence of other competing events. When both types of events can occur at any time but are only observed at clinical visits (i.e., interval censored), standard survival models...
PMC12953449
core_pubmed_pmc
Identification of predictive biomarkers and dose optimization for camrelizumab combined with apatinib in the treatment of advanced hepatocellular carcinoma: a quantitative systems pharmacology approach
Identification of predictive biomarkers and dose optimization for camrelizumab combined with apatinib in the treatment of advanced hepatocellular carcinoma: a quantitative systems pharmacology approach Abstract Introduction The combination of camrelizumab and apatinib represents a promising treatment strategy for patie...
PMC10046369
core_pubmed_pmc
Low-Affinity/High-Selectivity Dopamine Transport Inhibition Sufficient to Rescue Cognitive Functions in the Aging Rat
Low-Affinity/High-Selectivity Dopamine Transport Inhibition Sufficient to Rescue Cognitive Functions in the Aging Rat Abstract The worldwide increase in cognitive decline, both in aging and with psychiatric disorders, warrants a search for pharmacological treatment. Although dopaminergic treatment approaches represent ...
PMC9225039
core_pubmed_pmc
Ecdysteroids as Potent Enzyme Inhibitors and Verification of Their Activity Using In Vitro and In Silico Docking Studies
Ecdysteroids as Potent Enzyme Inhibitors and Verification of Their Activity Using In Vitro and In Silico Docking Studies Abstract Ecdysteroids represent arthropods’ steroidal hormones, and they exist in about 5–6% of plant species. In this study, the enzyme inhibitory activity of 20 ecdysteroids was assessed for the fi...
PMC4980920
core_pubmed_pmc
Platelet-to-lymphocyte ratio but not neutrophil-to-lymphocyte ratio predicts high on-treatment platelet reactivity in clopidogrel-treated patients with acute coronary syndrome
Platelet-to-lymphocyte ratio but not neutrophil-to-lymphocyte ratio predicts high on-treatment platelet reactivity in clopidogrel-treated patients with acute coronary syndrome Abstract Abstract Objectives: Dual antiplatelet therapy (DAPT), consisting of clopidogrel and aspirin, is the main-stay treatment of acute coron...
PMC2797436
core_pubmed_pmc
Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers
Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers Abstract Purpose Axitinib, a potent and selective inhibitor of vascular endothelial growth factor receptors 1, 2, 3, is metabolized by cytochrome P450 3A4 and glucuronidation. This study evaluated the effect ...
PMC3937833
core_pubmed_pmc
Comparative Pharmacokinetics of Naringin in Rat after Oral Administration of Chaihu-Shu-Gan-San Aqueous Extract and Naringin Alone
Comparative Pharmacokinetics of Naringin in Rat after Oral Administration of Chaihu-Shu-Gan-San Aqueous Extract and Naringin Alone Abstract Chaihu-Shu-Gan-San (CSGS), a traditional Chinese medicine (TCM) formula containing seven herbal medicines, has been used in the clinical treatment of gastritis, peptic ulcer, irrit...
PMC6824350
core_pubmed_pmc
Effect of Caffeine on the Bioavailability and Pharmacokinetics of an Acetylsalicylic Acid-Paracetamol Combination: Results of a Phase I Study
Effect of Caffeine on the Bioavailability and Pharmacokinetics of an Acetylsalicylic Acid-Paracetamol Combination: Results of a Phase I Study Abstract Introduction Caffeine is used as an adjuvant in analgesic combinations to enhance their efficacy. The present study aimed to determine the effect of caffeine on the phar...
PMC6804255
core_pubmed_pmc
Broccoli or Sulforaphane: Is It the Source or Dose That Matters?
Broccoli or Sulforaphane: Is It the Source or Dose That Matters? Abstract There is robust epidemiological evidence for the beneficial effects of broccoli consumption on health, many of them clearly mediated by the isothiocyanate sulforaphane. Present in the plant as its precursor, glucoraphanin, sulforaphane is formed ...
PMC9729534
core_pubmed_pmc
Serum and brain metabolomic study reveals the protective effects of Bai-Mi-Decoction on rats with ischemic stroke
Serum and brain metabolomic study reveals the protective effects of Bai-Mi-Decoction on rats with ischemic stroke Abstract Abstract Bai-Mi-Decoction (BMD), which is composed of Eugenia caryophyllata , Myristica fragrans , Moschus berezovskii , and Crocus sativu , is a characteristic TCM multi-herb formula for brain dis...
PMC9872218
core_pubmed_pmc
Urinary Pharmacokinetics of Immediate and Controlled Release Oxycodone and its Phase I and II Metabolites Using LC–MS-MS
Urinary Pharmacokinetics of Immediate and Controlled Release Oxycodone and its Phase I and II Metabolites Using LC–MS-MS Abstract Abstract Oxycodone (OC) is a schedule II semisynthetic opioid in the USA that is prescribed for its analgesic effects and has a high potential for abuse. Prescriptions for OC vary based on t...
PMC12894229
core_pubmed_pmc
From venom peptides to neurotherapeutics: BmK defensins and short-chain peptides as modulators of ion channels
From venom peptides to neurotherapeutics: BmK defensins and short-chain peptides as modulators of ion channels Abstract Scorpions, having inhabited the Earth long before the emergence of humans, represent an ancient lineage of arthropods. While often regarded with fear due to their potential to induce severe pain or fa...
PMC7954774
core_pubmed_pmc
Structural insights on the interaction potential of natural leads against major protein targets of SARS-CoV-2: Molecular modelling, docking and dynamic simulation studies
Structural insights on the interaction potential of natural leads against major protein targets of SARS-CoV-2: Molecular modelling, docking and dynamic simulation studies Abstract Abstract Though significant efforts are in progress for developing drugs and vaccines against COVID-19, limited therapeutic agents are avail...
PMC7408675
core_pubmed_pmc
Impacts of High Intra- and Inter-Individual Variability in Tacrolimus Pharmacokinetics and Fast Tacrolimus Metabolism on Outcomes of Solid Organ Transplant Recipients
Impacts of High Intra- and Inter-Individual Variability in Tacrolimus Pharmacokinetics and Fast Tacrolimus Metabolism on Outcomes of Solid Organ Transplant Recipients Abstract Abstract Tacrolimus is a first-line calcineurin inhibitor (CNI) and an integral part of the immunosuppressive strategy in solid organ transplant...
PMC3201932
core_pubmed_pmc
Methadone adverse reaction presenting with large increase in plasma methadone binding: a case series
Methadone adverse reaction presenting with large increase in plasma methadone binding: a case series Abstract Introduction The use of methadone as an analgesic is on the increase, but it is widely recognized that the goal of predictable and reproducible dosing is confounded by considerable variability in methadone phar...
PMC5370399
core_pubmed_pmc
Delineating the Role of Various Factors in Renal Disposition of Digoxin through Application of Physiologically Based Kidney Model to Renal Impairment Populations
Delineating the Role of Various Factors in Renal Disposition of Digoxin through Application of Physiologically Based Kidney Model to Renal Impairment Populations Abstract Development of submodels of organs within physiologically-based pharmacokinetic (PBPK) principles and beyond simple perfusion limitations may be chal...
PMC5840103
core_pubmed_pmc
Pharmacokinetics, Antiviral Activity, and Safety of Rilpivirine in Pregnant Women with HIV-1 Infection: Results of a Phase 3b, Multicenter, Open-Label Study
Pharmacokinetics, Antiviral Activity, and Safety of Rilpivirine in Pregnant Women with HIV-1 Infection: Results of a Phase 3b, Multicenter, Open-Label Study Abstract Introduction Physiologic changes during pregnancy may impact the pharmacokinetics of drugs. In addition, efficacy and safety/tolerability concerns have be...
PMC2866686
core_pubmed_pmc
Association between Serum Perfluorooctanoic Acid (PFOA) and Thyroid Disease in the U.S. National Health and Nutrition Examination Survey
Association between Serum Perfluorooctanoic Acid (PFOA) and Thyroid Disease in the U.S. National Health and Nutrition Examination Survey Abstract Abstract Background Perfluorooctanoic acid (PFOA, also known as C8) and perfluorooctane sulfonate (PFOS) are stable compounds with many industrial and consumer uses. Their pe...
PMC8669916
core_pubmed_pmc
Pharmacogenetics Based Dose Prediction Model for Initial Tacrolimus Dosing in Renal Transplant Recipients
Pharmacogenetics Based Dose Prediction Model for Initial Tacrolimus Dosing in Renal Transplant Recipients Abstract Abstract Tacrolimus, an immunosuppressant used in solid organ transplantation, has a narrow therapeutic index and exhibits inter-individual pharmacokinetic variability. Achieving and maintaining a therapeu...
PMC9578216
core_pubmed_pmc
An area under the concentration–time curve threshold as a predictor of efficacy and nephrotoxicity for individualizing polymyxin B dosing in patients with carbapenem-resistant gram-negative bacteria
An area under the concentration–time curve threshold as a predictor of efficacy and nephrotoxicity for individualizing polymyxin B dosing in patients with carbapenem-resistant gram-negative bacteria Abstract Abstract Background Evidence supports therapeutic drug monitoring of polymyxin B, but clinical data for establis...
PMC7463651
core_pubmed_pmc
Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma
Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma Abstract Abstract Tenalisib (RP6530), a dual phosphoinositide 3-kinase δ/γ inhibitor was evaluated in a phase I/Ib study for maximum tolerated dose (MTD), pharmacokinetics, and efficacy in patients wit...
PMC12736062
core_pubmed_pmc
Photodynamic Action of Hypocrellin A and Hypocrellin B against Cancer—A Review
Photodynamic Action of Hypocrellin A and Hypocrellin B against Cancer—A Review Abstract Cancer is a major global health concern, affecting nearly 20 million individuals annually, according to the International Agency for Research on Cancer (IARC). There are some unconventional and conventional treatments for cancer. Ty...
PMC11086890
core_pubmed_pmc
The fungicidal effectiveness of 2-Chloro-3-hydrazinylquinoxaline, a newly developed quinoxaline derivative, against Candida species
The fungicidal effectiveness of 2-Chloro-3-hydrazinylquinoxaline, a newly developed quinoxaline derivative, against Candida species Abstract Background Candida represents a prevalent fungal infection, notable for its substantial implications on morbidity and mortality rates. In the landscape of prospective treatments, ...
PMC12345486
core_pubmed_pmc
Preliminary Pharmacokinetics and Appetite Stimulant Efficacy of Oral Mirtazapine in Guinea Pigs ( Cavia porcellus )
Preliminary Pharmacokinetics and Appetite Stimulant Efficacy of Oral Mirtazapine in Guinea Pigs ( Cavia porcellus ) Abstract Simple Summary Guinea pigs are cecal fermenters requiring frequent and consistent feed intake to ensure normal gut motility. Transport, age-related disease, diet changes, and other sources of chr...
PMC8711605
core_pubmed_pmc
Week 96 extension results of a Phase 3 study evaluating long-acting cabotegravir with rilpivirine for HIV-1 treatment
Week 96 extension results of a Phase 3 study evaluating long-acting cabotegravir with rilpivirine for HIV-1 treatment Abstract Background: ATLAS (NCT02951052), a phase 3, multicenter, open-label study, demonstrated that switching to injectable cabotegravir (CAB) with rilpivirine (RPV) long-acting dosed every 4 weeks wa...
PMC8091127
core_pubmed_pmc
Exposure-Response Modeling to Support Dosing Selection for Phase IIb Development of Kukoamine B in Sepsis Patients
Exposure-Response Modeling to Support Dosing Selection for Phase IIb Development of Kukoamine B in Sepsis Patients Abstract Abstract Aim: Kukoamine B, a small molecule compound, is being developed for the treatment of sepsis in a Phase II clinical trial. The objective of this study was to optimize dosing selection for ...
PMC11370788
core_pubmed_pmc
Evaluation of Factors Predictive of Efficacy Among Patients With Complicated Urinary Tract Infection and/or Acute Pyelonephritis
Evaluation of Factors Predictive of Efficacy Among Patients With Complicated Urinary Tract Infection and/or Acute Pyelonephritis Abstract Abstract Background Antibiotic treatment for complicated urinary tract infections (cUTI)/acute pyelonephritis (AP) is often followed by recurrent bacteriuria in the absence of clinic...
PMC3815145
core_pubmed_pmc
First-day iodine kinetics is useful for individualizing radiation safety precautions for thyroid carcinoma patients
First-day iodine kinetics is useful for individualizing radiation safety precautions for thyroid carcinoma patients Abstract Abstract Objective There is considerable variation in the national regulations of different countries for the release of patients from hospitals after radioiodine therapy. Individual variations m...
PMC3260134
core_pubmed_pmc
Anticancer activity of an extract from needles and twigs of Taxus cuspidata and its synergistic effect as a cocktail with 5-fluorouracil
Anticancer activity of an extract from needles and twigs of Taxus cuspidata and its synergistic effect as a cocktail with 5-fluorouracil Abstract Abstract Background Botanical medicines are increasingly combined with chemotherapeutics as anticancer drug cocktails. This study aimed to assess the chemotherapeutic potenti...
PMC8914174
core_pubmed_pmc
Pharmacokinetics of Caffeine: A Systematic Analysis of Reported Data for Application in Metabolic Phenotyping and Liver Function Testing
Pharmacokinetics of Caffeine: A Systematic Analysis of Reported Data for Application in Metabolic Phenotyping and Liver Function Testing Abstract Abstract Caffeine is by far the most ubiquitous psychostimulant worldwide found in tea, coffee, cocoa, energy drinks, and many other beverages and food. Caffeine is almost ex...