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PMC10534762 | core_pubmed_pmc | Enhancing Osteoporosis Treatment through Targeted Nanoparticle Delivery of Risedronate: In Vivo Evaluation and Bioavailability Enhancement | Enhancing Osteoporosis Treatment through Targeted Nanoparticle Delivery of Risedronate: In Vivo Evaluation and Bioavailability Enhancement Abstract Abstract Risedronate-loaded mPEG-coated hydroxyapatite, thiolated chitosan-based (coated) and non-coated nanoparticles were tested for their potential effects in the treatm... |
PMC12089657 | core_pubmed_pmc | A Selective GSK3β Inhibitor, Tideglusib, Decreases Intermittent Access and Binge Ethanol Self‐Administration in C57BL/6J Mice | A Selective GSK3β Inhibitor, Tideglusib, Decreases Intermittent Access and Binge Ethanol Self‐Administration in C57BL/6J Mice Abstract ABSTRACT Over 10% of the US population over 12 years old meets criteria for alcohol use disorder (AUD), yet few effective, long‐term treatments are currently available. Glycogen synthas... |
PMC5061321 | core_pubmed_pmc | Preclinical Study of Single-Dose Moxidectin, a New Oral Treatment for Scabies: Efficacy, Safety, and Pharmacokinetics Compared to Two-Dose Ivermectin in a Porcine Model | Preclinical Study of Single-Dose Moxidectin, a New Oral Treatment for Scabies: Efficacy, Safety, and Pharmacokinetics Compared to Two-Dose Ivermectin in a Porcine Model Abstract Background Scabies is one of the commonest dermatological conditions globally; however it is a largely underexplored and truly neglected infec... |
PMC9886246 | core_pubmed_pmc | Integrated network pharmacology and molecular modeling approach for the discovery of novel potential MAPK3 inhibitors from whole green jackfruit flour targeting obesity-linked diabetes mellitus | Integrated network pharmacology and molecular modeling approach for the discovery of novel potential MAPK3 inhibitors from whole green jackfruit flour targeting obesity-linked diabetes mellitus Abstract Abstract The current study investigates the effectiveness of phytocompounds from the whole green jackfruit flour meth... |
PMC3232172 | core_pubmed_pmc | Bioequivalence of oxymorphone extended release and crush-resistant oxymorphone extended release | Bioequivalence of oxymorphone extended release and crush-resistant oxymorphone extended release Abstract Background A formulation of crush-resistant extended-release opioids may deter abuse. The purpose of this study was to evaluate the bioequivalence of oxymorphone extended-release (Oxy-ER) and a crush-resistant formu... |
PMC5759732 | core_pubmed_pmc | A Pilot Dose‐Finding Study of Etanercept in Rheumatoid Arthritis | A Pilot Dose‐Finding Study of Etanercept in Rheumatoid Arthritis Abstract Abstract A randomized, parallel‐dose study assessed the pharmacokinetics (PK) and pharmacodynamics (PD) of etanercept in 61 patients with rheumatoid arthritis (RA) who received doses from 10 mg once‐weekly to 50 mg twice‐weekly for 4 weeks. Empir... |
PMC10069031 | core_pubmed_pmc | Effects of regorafenib on the mononuclear/phagocyte system and how these contribute to the inhibition of colorectal tumors in mice | Effects of regorafenib on the mononuclear/phagocyte system and how these contribute to the inhibition of colorectal tumors in mice Abstract Background Regorafenib was previously shown to reduce tumor-associated macrophages and potently inhibit colony-stimulating factor 1 receptor (CSF1R), also known as CD115, in bioche... |
PMC8875976 | core_pubmed_pmc | Exploring Toxins for Hunting SARS-CoV-2 Main Protease Inhibitors: Molecular Docking, Molecular Dynamics, Pharmacokinetic Properties, and Reactome Study | Exploring Toxins for Hunting SARS-CoV-2 Main Protease Inhibitors: Molecular Docking, Molecular Dynamics, Pharmacokinetic Properties, and Reactome Study Abstract The main protease (M pro ) is a potential druggable target in SARS-CoV-2 replication. Herein, an in silico study was conducted to mine for M pro inhibitors fro... |
PMC7335652 | core_pubmed_pmc | Pharmacokinetics and Safety of Two Voriconazole Formulations after Intravenous Infusion in Healthy Korean Volunteers | Pharmacokinetics and Safety of Two Voriconazole Formulations after Intravenous Infusion in Healthy Korean Volunteers Abstract Background Voriconazole, a triazole antifungal agent exhibits broad-spectrum antifungal activity. It is used to treat severe, invasive fungal infections, including invasive aspergillosis and can... |
PMC8946662 | core_pubmed_pmc | Topical Bimiralisib Shows Meaningful Cutaneous Drug Levels in Healthy Volunteers and Mycosis Fungoides Patients but No Clinical Activity in a First-in-Human, Randomized Controlled Trial | Topical Bimiralisib Shows Meaningful Cutaneous Drug Levels in Healthy Volunteers and Mycosis Fungoides Patients but No Clinical Activity in a First-in-Human, Randomized Controlled Trial Abstract Abstract Simple Summary Primary cutaneous T-cell lymphomas (CTCLs) are a group of lymphomas that present in the skin without ... |
PMC8620281 | core_pubmed_pmc | Preparation, Characterization, and Anticancer Effects of Capsaicin-Loaded Nanoliposomes | Preparation, Characterization, and Anticancer Effects of Capsaicin-Loaded Nanoliposomes Abstract Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. Howev... |
PMC4279136 | core_pubmed_pmc | Evaluation of Rapidly Disintegrating Vaginal Tablets of Tenofovir, Emtricitabine and Their Combination for HIV-1 Prevention | Evaluation of Rapidly Disintegrating Vaginal Tablets of Tenofovir, Emtricitabine and Their Combination for HIV-1 Prevention Abstract Abstract Vaginal tablets are being developed as an alternative to gels as an inexpensive, discreet dosage form for the administration of microbicides. This work describes the pharmacokine... |
PMC5645818 | core_pubmed_pmc | Pharmacokinetic‐pharmacodynamic integration of enrofloxacin and its metabolite ciprofloxacin in buffalo calves | Pharmacokinetic‐pharmacodynamic integration of enrofloxacin and its metabolite ciprofloxacin in buffalo calves Abstract Abstract The present study was planned with an objective to test the pharmacokinetics of a new formulation of enrofloxacin (Flobac ® SA) in buffalo calves. The drug was administered at the dose rate o... |
PMC6719119 | core_pubmed_pmc | Reaction Kinetic Models of Antibiotic Heteroresistance | Reaction Kinetic Models of Antibiotic Heteroresistance Abstract Abstract Bacterial heteroresistance (i.e., the co-existence of several subpopulations with different antibiotic susceptibilities) can delay the clearance of bacteria even with long antibiotic exposure. Some proposed mechanisms have been successfully descri... |
PMC11380229 | core_pubmed_pmc | Modeling of Parkinson’s Disease Progression and Implications for Detection of Disease Modification in Treatment Trials | Modeling of Parkinson’s Disease Progression and Implications for Detection of Disease Modification in Treatment Trials Abstract Abstract Background: Objectively measuring Parkinson’s disease (PD) signs and symptoms over time is critical for the successful development of treatments aimed at halting the disease progressi... |
PMC5198030 | core_pubmed_pmc | A Comparative Pharmacokinetics Study of the Anti-Parkinsonian Drug Pramipexole | A Comparative Pharmacokinetics Study of the Anti-Parkinsonian Drug Pramipexole Abstract The present study aimed to compare pharmacokinetic parameters of two pramipexole 0.25 mg formulations in order to show bioequivalence. The study was conducted in a randomized, open-label, two-period, two-sequence, and crossover desi... |
PMC8659078 | core_pubmed_pmc | A Validated HPLC-PDA-HRMS Method to Investigate the Biological Stability and Metabolism of Antiparasitic Triterpenic Esters | A Validated HPLC-PDA-HRMS Method to Investigate the Biological Stability and Metabolism of Antiparasitic Triterpenic Esters Abstract Abstract Pentacyclic triterpenes (PTs) are commonly found in medicinal plants with well-known antiparasitic effects. Previous research on C-3 and C-27 triterpenic esters showed effective ... |
PMC10099095 | core_pubmed_pmc | Estimating the In Vivo Function of CYP2D6 Alleles through Population Pharmacokinetic Modeling of Brexpiprazole | Estimating the In Vivo Function of CYP2D6 Alleles through Population Pharmacokinetic Modeling of Brexpiprazole Abstract Accurate prediction of CYP2D6 phenotype from genotype information is important to support safe and efficacious pharmacotherapy with CYP2D6 substrates. To facilitate accurate CYP2D6 genotype–phenotype ... |
PMC11379377 | core_pubmed_pmc | Exploration of alpha-glucosidase inhibitors: A comprehensive in silico approach targeting a large set of triazole derivatives | Exploration of alpha-glucosidase inhibitors: A comprehensive in silico approach targeting a large set of triazole derivatives Abstract Background The increasing prevalence of diabetes and the side effects associated with current medications necessitate the development of novel candidate drugs targeting alpha-glucosidas... |
PMC9387129 | core_pubmed_pmc | Mitochondrial Imbalance of Trypanosoma cruzi Induced by the Marine Alkaloid 6-Bromo-2′-de- N -Methylaplysinopsin | Mitochondrial Imbalance of Trypanosoma cruzi Induced by the Marine Alkaloid 6-Bromo-2′-de- N -Methylaplysinopsin Abstract Chagas disease, caused by Trypanosoma cruzi , affects seven million people worldwide and lacks effective treatments. Using bioactivity-guided fractionation, NMR, and electrospray ionization-high res... |
PMC5024450 | core_pubmed_pmc | New medical treatments for lower urinary tract symptoms due to benign prostatic hyperplasia and future perspectives | New medical treatments for lower urinary tract symptoms due to benign prostatic hyperplasia and future perspectives Abstract Background Lower Urinary Tract Symptoms (LUTS) in men are a common clinical problem in urology and have been historically strictly linked to benign prostatic hyperplasia (BPH), which may lead to ... |
PMC8583772 | core_pubmed_pmc | Synergistic effect of ursolic acid and piperine in CCl 4 induced hepatotoxicity | Synergistic effect of ursolic acid and piperine in CCl 4 induced hepatotoxicity Abstract Abstract Background Ursolic acid (UA) is a potent plant-based hepatoprotective agent having poor bioavailability, which hampers its therapeutic efficacy. The present study tries to overcome this limitation by combining it with pipe... |
PMC6930853 | core_pubmed_pmc | Performance of the SAEM and FOCEI Algorithms in the Open‐Source, Nonlinear Mixed Effect Modeling Tool nlmixr | Performance of the SAEM and FOCEI Algorithms in the Open‐Source, Nonlinear Mixed Effect Modeling Tool nlmixr Abstract The free and open‐source package nlmixr implements pharmacometric nonlinear mixed effects model parameter estimation in R. It provides a uniform language to define pharmacometric models using ordinary d... |
PMC9694621 | core_pubmed_pmc | Drug Delivery Systems as a Strategy to Improve the Efficacy of FDA-Approved Alzheimer’s Drugs | Drug Delivery Systems as a Strategy to Improve the Efficacy of FDA-Approved Alzheimer’s Drugs Abstract Alzheimer’s disease (AD) is the most common form of dementia, with a high impact worldwide, accounting for more than 46 million cases. The continuous increase of AD demands the fast development of preventive and curat... |
PMC4079925 | core_pubmed_pmc | Broad-spectrum β-lactams in obese non-critically ill patients | Broad-spectrum β-lactams in obese non-critically ill patients Abstract Abstract Objectives: Obesity may alter the pharmacokinetics of β-lactams. The goal of this study was to evaluate if and why serum concentrations are inadequate when standard β-lactam regimens are administered to obese, non-critically ill patients. S... |
PMC3411307 | core_pubmed_pmc | Degree of freezing does not affect efficacy of frozen gloves for prevention of docetaxel-induced nail toxicity in breast cancer patients | Degree of freezing does not affect efficacy of frozen gloves for prevention of docetaxel-induced nail toxicity in breast cancer patients Abstract Abstract Purpose Frozen gloves (FG) are effective in preventing docetaxel-induced nail toxicity (DNT), but uncomfortable. The preventive effect of FG for DNT was compared usi... |
PMC5944177 | core_pubmed_pmc | Extending the DIDEO ontology to include entities from the natural product drug interaction domain of discourse | Extending the DIDEO ontology to include entities from the natural product drug interaction domain of discourse Abstract Abstract Background Prompted by the frequency of concomitant use of prescription drugs with natural products, and the lack of knowledge regarding the impact of pharmacokinetic-based natural product-dr... |
PMC12271010 | core_pubmed_pmc | Systemic Effects of Intravitreal Anti-VEGF Therapy: A Review of Safety across Organ Systems | Systemic Effects of Intravitreal Anti-VEGF Therapy: A Review of Safety across Organ Systems Abstract Abstract Intravitreal anti-vascular endothelial growth factor (anti-VEGF) therapies have transformed the management of retinal diseases such as diabetic macular edema and neovascular age-related macular degeneration. Ho... |
PMC11483610 | core_pubmed_pmc | Development and validation of PBPK models for genistein and daidzein for use in a next-generation risk assessment | Development and validation of PBPK models for genistein and daidzein for use in a next-generation risk assessment Abstract Introduction All cosmetic ingredients must be evaluated for their safety to consumers. In the absence of in vivo data, systemic concentrations of ingredients can be predicted using Physiologically ... |
PMC11117716 | core_pubmed_pmc | Comparative Analysis of Posiphen Pharmacokinetics across Different Species—Similar Absorption and Metabolism in Mouse, Rat, Dog and Human | Comparative Analysis of Posiphen Pharmacokinetics across Different Species—Similar Absorption and Metabolism in Mouse, Rat, Dog and Human Abstract Abstract Posiphen is a small molecule that exhibits neuroprotective properties by targeting multiple neurotoxic proteins involved in axonal transport, synaptic transmission,... |
PMC10058836 | core_pubmed_pmc | Identification of Potential Inhibitors for the Treatment of Alkaptonuria Using an Integrated In Silico Computational Strategy | Identification of Potential Inhibitors for the Treatment of Alkaptonuria Using an Integrated In Silico Computational Strategy Abstract Abstract Alkaptonuria (AKU) is a rare genetic autosomal recessive disorder characterized by elevated serum levels of homogentisic acid (HGA). In this disease, tyrosine metabolism is int... |
PMC7552719 | core_pubmed_pmc | Estradiol-17β Pharmacokinetics and Histological Assessment of the Ovaries and Uterine Horns following Intramuscular Administration of Estradiol Cypionate in Feral Cats | Estradiol-17β Pharmacokinetics and Histological Assessment of the Ovaries and Uterine Horns following Intramuscular Administration of Estradiol Cypionate in Feral Cats Abstract Simple Summary Feral cats ( Felis catus ) have a devastating impact on Australian native fauna. Several programs exist to control their numbers... |
PMC8003312 | core_pubmed_pmc | Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat | Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat Abstract Abstract A major challenge in the management of antiretroviral therapy (ART) is to improve the patient’s adherence, reducing the burden caused by the high number of drugs that compose the treatment... |
PMC9398170 | core_pubmed_pmc | RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors | RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors Abstract Abstract Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-... |
PMC12001266 | core_pubmed_pmc | Elucidating Contributions of Drug Transporters/Enzyme to Nonlinear Pharmacokinetics of Grazoprevir by PBPK Modeling With a Cluster Gauss–Newton Method | Elucidating Contributions of Drug Transporters/Enzyme to Nonlinear Pharmacokinetics of Grazoprevir by PBPK Modeling With a Cluster Gauss–Newton Method Abstract ABSTRACT Grazoprevir (GZR), a direct‐acting agent for hepatitis C virus, is recognized as a substrate for organic anion transporting polypeptide 1B (OATP1B), cy... |
PMC6900590 | core_pubmed_pmc | Statistical Methods for Adjusting Estimates of Treatment Effectiveness for Patient Nonadherence in the Context of Time-to-Event Outcomes and Health Technology Assessment: A Systematic Review of Methodological Papers | Statistical Methods for Adjusting Estimates of Treatment Effectiveness for Patient Nonadherence in the Context of Time-to-Event Outcomes and Health Technology Assessment: A Systematic Review of Methodological Papers Abstract Introduction. Medication nonadherence can have a significant negative impact on treatment effec... |
PMC9464203 | core_pubmed_pmc | Topical nitroglycerin to detect reversible microcirculatory dysfunction in patients with circulatory shock after cardiovascular surgery: an observational study | Topical nitroglycerin to detect reversible microcirculatory dysfunction in patients with circulatory shock after cardiovascular surgery: an observational study Abstract Abstract Persistent abnormalities in microcirculatory function are associated with poor clinical outcomes in patients with circulatory shock. We sought... |
PMC9905199 | core_pubmed_pmc | Interactions between natural products and cancer treatments: underlying mechanisms and clinical importance | Interactions between natural products and cancer treatments: underlying mechanisms and clinical importance Abstract Natural products, also referred to as dietary supplements, complementary and alternative medicines, and health or food supplements are widely used by people living with cancer. These products are predomin... |
PMC6960228 | core_pubmed_pmc | Ethoxysanguinarine, a Novel Direct Activator of AMP-Activated Protein Kinase, Induces Autophagy and Exhibits Therapeutic Potential in Breast Cancer Cells | Ethoxysanguinarine, a Novel Direct Activator of AMP-Activated Protein Kinase, Induces Autophagy and Exhibits Therapeutic Potential in Breast Cancer Cells Abstract Abstract Ethoxysanguinarine (Eth) is a benzophenanthridine alkaloid extracted from Macleaya cordata (Willd) R. Br . It possesses antibacterial and antiviral ... |
PMC10291551 | core_pubmed_pmc | Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist | Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist Abstract Abstract We have recently reported on the use of aryl-fluorosulfates in designing water- and plasma-stable agents that covalently target Lys, Tyr, or His residues in the BIR3 domain of the inhibito... |
PMC11916023 | core_pubmed_pmc | Pharmacokinetic study of eplerenone in rats after long‐term coadministration with buckwheat tea | Pharmacokinetic study of eplerenone in rats after long‐term coadministration with buckwheat tea Abstract Abstract The aim of this study was to investigate the effect of long‐term intake of Tartary buckwheat tea on the pharmacokinetics (PK) of eplerenone in rats. A validated high‐performance liquid chromatography‐mass s... |
PMC12881105 | core_pubmed_pmc | Population Pharmacokinetics of Total and Protein-Unbound Prednisolone in Children with Immune-Mediated and Systemic Inflammatory Diseases | Population Pharmacokinetics of Total and Protein-Unbound Prednisolone in Children with Immune-Mediated and Systemic Inflammatory Diseases Abstract Abstract Background and Objective High-dose systemic prednisolone is the mainstay treatment of children with various (auto)immune diseases. The standard empirical dosing reg... |
PMC9403776 | core_pubmed_pmc | Characteristics of Prescription Opioid Analgesics in Pregnancy and Risk of Neonatal Opioid Withdrawal Syndrome in Newborns | Characteristics of Prescription Opioid Analgesics in Pregnancy and Risk of Neonatal Opioid Withdrawal Syndrome in Newborns Abstract Key Points Question Does risk of neonatal opioid withdrawal syndrome (NOWS) after in utero exposure to prescription opioids vary across commonly prescribed types of opioids? Findings In th... |
PMC12041147 | core_pubmed_pmc | Population Pharmacokinetics of Cefepime in Critically Ill Children and Young Adults: Model Development and External Validation for Monte Carlo Simulations and Model-Informed Precision Dosing | Population Pharmacokinetics of Cefepime in Critically Ill Children and Young Adults: Model Development and External Validation for Monte Carlo Simulations and Model-Informed Precision Dosing Abstract Abstract Background and Objective This study aimed to develop a population pharmacokinetic model for cefepime in critica... |
PMC7896741 | core_pubmed_pmc | Preparation, Characterization and in vitro/in vivo Evaluation of Lovastatin-Loaded PLGA Microspheres by Local Administration for Femoral Head Necrosis | Preparation, Characterization and in vitro/in vivo Evaluation of Lovastatin-Loaded PLGA Microspheres by Local Administration for Femoral Head Necrosis Abstract Abstract Background The present work is an effort to develop a novel locally injection LVTT-loaded PLGA microspheres (LVTT-PLGA-MS) on the treatment of rabbits ... |
PMC3236147 | core_pubmed_pmc | Comparison of Three Aspirin Formulations in Human Volunteers | Comparison of Three Aspirin Formulations in Human Volunteers Abstract Abstract Introduction The treatment of acute coronary syndrome (ACS) includes the administration of aspirin. Current guidelines recommend chewing aspirin tablets to increase absorption. While this is intuitive, there are scant data supporting this re... |
PMC7984210 | core_pubmed_pmc | Prevalence and Associated Factors of Drug-Related Problems Among Older People: A Cross-Sectional Study at King Chulalongkorn Memorial Hospital in Bangkok | Prevalence and Associated Factors of Drug-Related Problems Among Older People: A Cross-Sectional Study at King Chulalongkorn Memorial Hospital in Bangkok Abstract Abstract Background and Objective The use of multiple medications and altered pharmacokinetics/pharmacodynamics may lead to drug-related problems in members ... |
PMC9297904 | core_pubmed_pmc | Population Pharmacokinetics of TAK‐931, a Cell Division Cycle 7 Kinase Inhibitor, in Patients With Advanced Solid Tumors | Population Pharmacokinetics of TAK‐931, a Cell Division Cycle 7 Kinase Inhibitor, in Patients With Advanced Solid Tumors Abstract Abstract A population pharmacokinetic (PK) analysis was conducted to characterize sources of interpatient variability on the PK of TAK‐931, a cell division cycle 7 kinase inhibitor, in adult... |
PMC5992651 | core_pubmed_pmc | Antiepileptic drugs in critically ill patients | Antiepileptic drugs in critically ill patients Abstract Abstract Background The incidence of seizures in intensive care units ranges from 3.3% to 34%. It is therefore often necessary to initiate or continue anticonvulsant drugs in this setting. When a new anticonvulsant is initiated, drug factors, such as onset of acti... |
PMC7267503 | core_pubmed_pmc | Severe COVID-19 in a renal transplant recipient: A focus on pharmacokinetics | Severe COVID-19 in a renal transplant recipient: A focus on pharmacokinetics Abstract Abstract The current coronavirus disease 2019 (COVID-19) pandemic requires extra attention for immunocompromised patients, including solid organ transplant recipients. We report on a case of a 35-year-old renal transplant recipient wh... |
PMC8332554 | core_pubmed_pmc | Pharmacokinetics and Exposure-Response Relationship of Teprotumumab, an Insulin-Like Growth Factor-1 Receptor-Blocking Antibody, in Thyroid Eye Disease | Pharmacokinetics and Exposure-Response Relationship of Teprotumumab, an Insulin-Like Growth Factor-1 Receptor-Blocking Antibody, in Thyroid Eye Disease Abstract Background and Objective Thyroid eye disease (TED) is characterized by inflammation/expansion of orbital tissues, proptosis, and diplopia. Teprotumumab is the ... |
PMC10772668 | core_pubmed_pmc | Safety, pharmacokinetics, and target engagement of a brain penetrant RIPK1 inhibitor, SAR443820 (DNL788), in healthy adult participants | Safety, pharmacokinetics, and target engagement of a brain penetrant RIPK1 inhibitor, SAR443820 (DNL788), in healthy adult participants Abstract Abstract SAR443820 (DNL788) is a selective, orally bioavailable, brain penetrant inhibitor of receptor‐interacting serine/threonine protein kinase 1 (RIPK1). This phase I firs... |
PMC9772825 | core_pubmed_pmc | Identification of potential inhibitors of omicron variant of SARS-Cov-2 RBD based virtual screening, MD simulation, and DFT | Identification of potential inhibitors of omicron variant of SARS-Cov-2 RBD based virtual screening, MD simulation, and DFT Abstract Abstract Emergence of the SARS-CoV-2 Omicron variant of concern (VOC; B.1.1.529) resulted in a new peak of the COVID-19 pandemic, which called for development of effective therapeutics ag... |
PMC5045937 | core_pubmed_pmc | Population pharmacokinetic and pharmacodynamic analyses of safinamide in subjects with Parkinson's disease | Population pharmacokinetic and pharmacodynamic analyses of safinamide in subjects with Parkinson's disease Abstract Abstract Safinamide is an orally administered α ‐aminoamide derivative with both dopaminergic and non‐dopaminergic properties. Nonlinear mixed effects models for population pharmacokinetic ( PK ) and phar... |
PMC7719371 | core_pubmed_pmc | Quantification of Natural Growth of Two Strains of Mycobacterium Marinum for Translational Antituberculosis Drug Development | Quantification of Natural Growth of Two Strains of Mycobacterium Marinum for Translational Antituberculosis Drug Development Abstract The zebrafish infected with Mycobacterium marinum ( M. marinum ) is an attractive tuberculosis disease model, showing similar pathogenesis to Mycobacterium tuberculosis ( M. tuberculosis... |
PMC11573869 | core_pubmed_pmc | Clinical Pharmacology of Asciminib: A Review | Clinical Pharmacology of Asciminib: A Review Abstract Asciminib is a first-in-class allosteric inhibitor of the kinase activity of BCR::ABL1, specifically targeting the ABL myristoyl pocket (STAMP). This review focuses on the pharmacokinetic (PK) and pharmacodynamic data of asciminib, which is approved at a total daily... |
PMC3394807 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of the Reverse Transcriptase Inhibitor Tenofovir and Prophylactic Efficacy against HIV-1 Infection | Pharmacokinetics and Pharmacodynamics of the Reverse Transcriptase Inhibitor Tenofovir and Prophylactic Efficacy against HIV-1 Infection Abstract Antiviral pre-exposure prophylaxis (PrEP) through daily drug administration can protect healthy individuals from HIV-1 infection. While PrEP was recently approved by the FDA,... |
PMC12454832 | core_pubmed_pmc | Investigation of the Efficacy and Safety of Xeligekimab (GR1501) in Patients with Moderate-to-Severe Plaque Psoriasis: A Multicenter, Randomized, Double-Blind Phase II Clinical trial | Investigation of the Efficacy and Safety of Xeligekimab (GR1501) in Patients with Moderate-to-Severe Plaque Psoriasis: A Multicenter, Randomized, Double-Blind Phase II Clinical trial Abstract Abstract Introduction Psoriasis is a chronic inflammatory skin disease. This study evaluated the efficacy and safety of xeligeki... |
PMC4788153 | core_pubmed_pmc | Impact of Cytochrome P450 2D6 Function on the Chiral Blood Plasma Pharmacokinetics of 3,4-Methylenedioxymethamphetamine (MDMA) and Its Phase I and II Metabolites in Humans | Impact of Cytochrome P450 2D6 Function on the Chiral Blood Plasma Pharmacokinetics of 3,4-Methylenedioxymethamphetamine (MDMA) and Its Phase I and II Metabolites in Humans Abstract Abstract 3,4-methylenedioxymethamphetamine (MDMA; ecstasy) metabolism is known to be stereoselective, with preference for S -stereoisomers.... |
PMC3566806 | core_pubmed_pmc | A novel small molecule hydroxamate preferentially inhibits HDAC6 activity and tumour growth | A novel small molecule hydroxamate preferentially inhibits HDAC6 activity and tumour growth Abstract Abstract Background: This study investigates whether a histone deacetylase subtype 6 (HDAC6) inhibitor could be used in the treatment of solid tumours. Methods: We evaluated the effect of a novel inhibitor, C1A, on HDAC... |
PMC6301732 | core_pubmed_pmc | Decreased protein binding of moxifloxacin in patients with sepsis? | Decreased protein binding of moxifloxacin in patients with sepsis? Abstract Abstract The mean (SD) unbound fraction of moxifloxacin in plasma from patients with severe sepsis or septic shock was determined by ultrafiltration to 85.5±3.0% (range 81.9 and 91.6%) indicating a decreased protein binding of moxifloxacin in t... |
PMC11152392 | core_pubmed_pmc | A Comparative Analysis on the Potential Anticancer Properties of Tetrahydrocannabinol, Cannabidiol, and Tetrahydrocannabivarin Compounds Through In Silico Approach | A Comparative Analysis on the Potential Anticancer Properties of Tetrahydrocannabinol, Cannabidiol, and Tetrahydrocannabivarin Compounds Through In Silico Approach Abstract Objective: The purpose of this study is to comparatively analyze the anticancer properties of Tetrahydrocannabinol (THC), Cannabidiol (CBD), and Te... |
PMC10987880 | core_pubmed_pmc | Nanoparticle-based optical interfaces for retinal neuromodulation: a review | Nanoparticle-based optical interfaces for retinal neuromodulation: a review Abstract Degeneration of photoreceptors in the retina is a leading cause of blindness, but commonly leaves the retinal ganglion cells (RGCs) and/or bipolar cells extant. Consequently, these cells are an attractive target for the invasive electr... |
PMC7595966 | core_pubmed_pmc | Scutellarin is Highly Likely to be Responsible for Drug-Drug Interactions Mediated by Hepatic Organic Anion-Transporting Polypeptide1B3 | Scutellarin is Highly Likely to be Responsible for Drug-Drug Interactions Mediated by Hepatic Organic Anion-Transporting Polypeptide1B3 Abstract Abstract Purpose Scutellarin, a flavonoid derived from the plant Erigeron breviscapus, is currently widely used to treat cerebrovascular diseases, liver-related diseases, and ... |
PMC11682888 | core_pubmed_pmc | In vitro elimination of antimicrobials during ADVanced Organ Support hemodialysis | In vitro elimination of antimicrobials during ADVanced Organ Support hemodialysis Abstract Background Acute kidney injury (AKI) requiring continuous renal replacement therapy is common in critically ill patients. The ADVanced Organ Support (ADVOS) system is a novel hemodialysis machine that uses albumin enriched dialys... |
PMC5849912 | core_pubmed_pmc | Inhibitory effect of celecoxib on agomelatine metabolism in vitro and in vivo | Inhibitory effect of celecoxib on agomelatine metabolism in vitro and in vivo Abstract Abstract Aim The aim of this study was to study the effect of celecoxib on agomelatine metabolism in vitro and in vivo. Methods Ten healthy male Sprague–Dawley rats were randomly divided into 2 groups: Group A (control group) and Gro... |
PMC12648701 | core_pubmed_pmc | Targeting telomere dynamics with plant-derived compounds: Molecular strategies against aging | Targeting telomere dynamics with plant-derived compounds: Molecular strategies against aging Abstract Telomeres, the repetitive DNA–protein complexes capping eukaryotic chromosomes, preserve genomic stability and regulate cellular replicative capacity. Progressive telomere shortening, coupled with diminished telomerase... |
PMC11098164 | core_pubmed_pmc | RPEM : Randomized Monte Carlo parametric expectation maximization algorithm | RPEM : Randomized Monte Carlo parametric expectation maximization algorithm Abstract Abstract Inspired from quantum Monte Carlo, by sampling discrete and continuous variables at the same time using the Metropolis–Hastings algorithm, we present a novel, fast, and accurate high performance Monte Carlo Parametric Expectat... |
PMC12285933 | core_pubmed_pmc | A Novel HPLC-MS/MS Method for the Intracellular Quantification of the Active Triphosphate Metabolite of Remdesivir: GS-443902 | A Novel HPLC-MS/MS Method for the Intracellular Quantification of the Active Triphosphate Metabolite of Remdesivir: GS-443902 Abstract Abstract Background: Remdesivir (RDV) is a broad-spectrum antiviral prodrug, which is rapidly metabolized in vivo within cells to the pharmacologically active triphosphate metabolite, G... |
PMC7093582 | core_pubmed_pmc | Acute Effects of 2C-E in Humans: An Observational Study | Acute Effects of 2C-E in Humans: An Observational Study Abstract Abstract 2,5-Dimethoxy-4-ethylphenethylamine (2C-E) is psychedelic phenylethylamine, with a chemical structure similar to mescaline, used as new psychoactive substance (NPS). It inhibits norepinephrine and serotonin uptake and, more relevant, acts as a pa... |
PMC5836871 | core_pubmed_pmc | Pharmacokinetics of Nintedanib in Subjects With Hepatic Impairment | Pharmacokinetics of Nintedanib in Subjects With Hepatic Impairment Abstract Abstract Nintedanib is an intracellular inhibitor of tyrosine kinases used in the treatment of non–small cell lung cancer and idiopathic pulmonary fibrosis (IPF). This phase 1 open‐label study investigated the influence of mild and moderate hep... |
PMC7023239 | core_pubmed_pmc | Evaluation of the Biodistribution of Serinolamide-Derivatized C 60 Fullerene | Evaluation of the Biodistribution of Serinolamide-Derivatized C 60 Fullerene Abstract Carbon nanoparticles have consistently been of great interest in medicine. However, there are currently no clinical materials based on carbon nanoparticles, due to inconsistent biodistribution and excretion data. In this work, we have... |
PMC10143085 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model to Predict Determinants of Variability in Epirubicin Exposure and Tissue Distribution | A Physiologically Based Pharmacokinetic Model to Predict Determinants of Variability in Epirubicin Exposure and Tissue Distribution Abstract Abstract Background: Epirubicin is an anthracycline antineoplastic drug that is primarily used in combination therapies for the treatment of breast, gastric, lung and ovarian canc... |
PMC3418081 | core_pubmed_pmc | Improved pharmacokinetics and reduced toxicity of brucine after encapsulation into stealth liposomes: role of phosphatidylcholine | Improved pharmacokinetics and reduced toxicity of brucine after encapsulation into stealth liposomes: role of phosphatidylcholine Abstract Abstract Objective: Brucine was encapsulated into stealth liposomes using the ammonium sulfate gradient method to improve therapeutic index. Materials and methods: Four brucine stea... |
PMC12776292 | core_pubmed_pmc | Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer’s Disease Models | Optimization and Characterization of SHIP1 Ligands for Cellular Target Engagement and Activity in Alzheimer’s Disease Models Abstract Abstract Src homology 2 domain-containing inositol 5-phosphatase 1 (SHIP1), encoded by the gene INPP5D, is a lipid phosphatase that negatively regulates immune receptor signaling in hema... |
PMC9404876 | core_pubmed_pmc | A Proof of Concept of the Usefulness of a TDM-Guided Strategy for Optimizing Pharmacokinetic/Pharmacodynamic Target of Continuous Infusion Ampicillin-Based Regimens in a Case Series of Patients with Enterococcal Bloodstream Infections and/or Endocarditis | A Proof of Concept of the Usefulness of a TDM-Guided Strategy for Optimizing Pharmacokinetic/Pharmacodynamic Target of Continuous Infusion Ampicillin-Based Regimens in a Case Series of Patients with Enterococcal Bloodstream Infections and/or Endocarditis Abstract Abstract (1) Objective: To describe the usefulness of a ... |
PMC8880587 | core_pubmed_pmc | Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet | Design and Optimization of Pioglitazone Hydrochloride Self-Nanoemulsifying Drug Delivery System (SNEDDS) Incorporated into an Orally Disintegrating Tablet Abstract Abstract Pioglitazone Hydrochloride (PGZ) suffers from poor aqueous solubility. The aim of this research was to design orally disintegrating tablets with se... |
PMC4545922 | core_pubmed_pmc | Treatment of systemic lupus erythematosus patients with the BAFF antagonist “peptibody” blisibimod (AMG 623/A-623): results from randomized, double-blind phase 1a and phase 1b trials | Treatment of systemic lupus erythematosus patients with the BAFF antagonist “peptibody” blisibimod (AMG 623/A-623): results from randomized, double-blind phase 1a and phase 1b trials Abstract Abstract Introduction Blisibimod is a potent B cell-activating factor (BAFF) antagonist that binds to both cell membrane-express... |
PMC5318333 | core_pubmed_pmc | Evaluation of Amikacin Pharmacokinetics and Pharmacodynamics for Optimal Initial Dosing Regimen | Evaluation of Amikacin Pharmacokinetics and Pharmacodynamics for Optimal Initial Dosing Regimen Abstract Abstract Amikacin has been one of the important antimicrobial agents against Gram-negative pathogens. However, there is discrepancy regarding the amikacin initial dosage, with some reports recently recommending ≥25 ... |
PMC7898708 | core_pubmed_pmc | Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity | Polymeric nanoencapsulation of zaleplon into PLGA nanoparticles for enhanced pharmacokinetics and pharmacological activity Abstract Abstract Zaleplon (ZP) is a sedative and hypnotic drug used for the treatment of insomnia. Despite its potent anticonvulsant activity, ZP is not commonly used for the treatment of convulsi... |
PMC6471170 | core_pubmed_pmc | Simulation-Based Analysis of the Impact of Renal Impairment on the Pharmacokinetics of Highly Metabolized Compounds | Simulation-Based Analysis of the Impact of Renal Impairment on the Pharmacokinetics of Highly Metabolized Compounds Abstract Renal impairment (RI) is a highly prevalent disease which can alter the pharmacokinetics (PK) of xenobiotics, including those that are predominately metabolized. The expression and activity of dr... |
PMC9425318 | core_pubmed_pmc | The von Willebrand factor A-1 domain binding aptamer BT200 elevates plasma levels of von Willebrand factor and factor VIII: a first-in-human trial | The von Willebrand factor A-1 domain binding aptamer BT200 elevates plasma levels of von Willebrand factor and factor VIII: a first-in-human trial Abstract von Willebrand factor (VWF) and factor VIII (FVIII) circulate in a noncovalent complex in blood and promote primary hemostasis and clotting, respectively. A new VWF... |
PMC11919263 | core_pubmed_pmc | Disease–Drug–Drug Interaction of Imatinib in COVID‐19 ARDS: A Pooled Population Pharmacokinetic Analysis | Disease–Drug–Drug Interaction of Imatinib in COVID‐19 ARDS: A Pooled Population Pharmacokinetic Analysis Abstract ABSTRACT Prior pharmacokinetic (PK) analysis revealed that increased alpha‐1‐acid glycoprotein (AAG) levels are associated with decreased imatinib unbound fraction in coronavirus disease 2019 (COVID‐19) pat... |
PMC10856407 | core_pubmed_pmc | Polymer Nanoparticles with 2-HP-β-Cyclodextrin for Enhanced Retention of Uptake into HCE-T Cells | Polymer Nanoparticles with 2-HP-β-Cyclodextrin for Enhanced Retention of Uptake into HCE-T Cells Abstract Triamcinolone acetonide (TA), a medium-potency synthetic glucocorticoid, is primarily employed to treat posterior ocular diseases using vitreous injection. This study aimed to design novel ocular nanoformulation dr... |
PMC10928832 | core_pubmed_pmc | Effects of dapagliflozin on body weight in patients with type 2 diabetes mellitus: Evidence‑based practice | Effects of dapagliflozin on body weight in patients with type 2 diabetes mellitus: Evidence‑based practice Abstract Abstract The dose-dependent pharmacological response to dapagliflozin in patients with type 2 diabetes mellitus (T2DM) with regard to weight loss remain unknown. The aim of the present study was to invest... |
PMC7026271 | core_pubmed_pmc | Engineering Targeting Materials for Therapeutic Cancer Vaccines | Engineering Targeting Materials for Therapeutic Cancer Vaccines Abstract Abstract Therapeutic cancer vaccines constitute a valuable tool to educate the immune system to fight tumors and prevent cancer relapse. Nevertheless, the number of cancer vaccines in the clinic remains very limited to date, highlighting the need ... |
PMC9898402 | core_pubmed_pmc | Phloroglucinol-Derived Medications are Effective in Reducing Pain and Spasms of Urinary and Biliary Tracts: Results of Phase 3 Multicentre, Open-Label, Randomized, Comparative Studies of Clinical Effectiveness and Safety | Phloroglucinol-Derived Medications are Effective in Reducing Pain and Spasms of Urinary and Biliary Tracts: Results of Phase 3 Multicentre, Open-Label, Randomized, Comparative Studies of Clinical Effectiveness and Safety Abstract Abstract Introduction Pain and spasms of urinary and biliary tracts are conditions causing... |
PMC7127848 | core_pubmed_pmc | Pre-Clinical Pharmacokinetics, Tissue Distribution and Physicochemical Studies of CLBQ14, a Novel Methionine Aminopeptidase Inhibitor for the Treatment of Infectious Diseases | Pre-Clinical Pharmacokinetics, Tissue Distribution and Physicochemical Studies of CLBQ14, a Novel Methionine Aminopeptidase Inhibitor for the Treatment of Infectious Diseases Abstract Introduction CLBQ14, a derivative of 8-hydroxyquinoline, exerts its chemotherapeutic effect by inhibiting methionine aminopeptidase (Met... |
PMC5075792 | core_pubmed_pmc | Pharmacokinetic comparison between quercetin and quercetin 3- O - β -glucuronide in rats by UHPLC-MS/MS | Pharmacokinetic comparison between quercetin and quercetin 3- O - β -glucuronide in rats by UHPLC-MS/MS Abstract Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3- O - β -glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolize... |
PMC9626641 | core_pubmed_pmc | Anti-liver fibrosis activity of curcumin/chitosan-coated green silver nanoparticles | Anti-liver fibrosis activity of curcumin/chitosan-coated green silver nanoparticles Abstract Liver fibrosis results from the hepatic accumulation of the extracellular matrix accompanied by a failure of the mechanisms responsible for matrix dissolution. Pathogenesis of liver fibrosis is associated with many proteins fro... |
PMC3049598 | core_pubmed_pmc | Hypertension and overall survival in metastatic colorectal cancer patients treated with bevacizumab-containing chemotherapy | Hypertension and overall survival in metastatic colorectal cancer patients treated with bevacizumab-containing chemotherapy Abstract Background: Hypertension (HTN) is a common toxicity of anti-VEGF (vascular endothelial growth factor) antibody treatment. It may be a marker of VEGF signalling pathway inhibition and ther... |
PMC10624720 | core_pubmed_pmc | The Pharmacokinetic Profile of Palovarotene: An Open-Label Phase I Trial Investigating the Effect of Food and Potential for Drug–Drug Interaction in Healthy Participants | The Pharmacokinetic Profile of Palovarotene: An Open-Label Phase I Trial Investigating the Effect of Food and Potential for Drug–Drug Interaction in Healthy Participants Abstract Abstract Background and Objectives Palovarotene is under development for the treatment of fibrodysplasia ossificans progressiva (FOP). The ob... |
PMC6118266 | core_pubmed_pmc | Spectroscopic and molecular modeling studies of binding interaction between bovine serum albumin and roflumilast | Spectroscopic and molecular modeling studies of binding interaction between bovine serum albumin and roflumilast Abstract Abstract Background The binding interaction between bovine serum albumin (BSA) and roflumilast (ROF) was explored in this study. The binding of drugs to albumin plays a vital role in their pharmacok... |
PMC8003675 | core_pubmed_pmc | Dexibuprofen Therapeutic Advances: Prodrugs and Nanotechnological Formulations | Dexibuprofen Therapeutic Advances: Prodrugs and Nanotechnological Formulations Abstract Abstract S -(+) enantiomer of ibuprofen (IBU) dexibuprofen (DXI) is known to be more potent than its R -(−) form and exhibits many advantages over the racemic mixture of IBU such as lower toxicity, greater clinical efficacy, and les... |
PMC8265363 | core_pubmed_pmc | Evaluation of the Association of Polymorphisms With Palbociclib‐Induced Neutropenia: Pharmacogenetic Analysis of PALOMA ‐2/‐3 | Evaluation of the Association of Polymorphisms With Palbociclib‐Induced Neutropenia: Pharmacogenetic Analysis of PALOMA ‐2/‐3 Abstract Abstract Background The most frequently reported treatment‐related adverse event in clinical trials with the cyclin‐dependent kinase 4/6 (CDK4/6) inhibitor palbociclib is neutropenia. A... |
PMC7078569 | core_pubmed_pmc | In vitro and in vivo characterization of domperidone-loaded fast dissolving buccal films | In vitro and in vivo characterization of domperidone-loaded fast dissolving buccal films Abstract Abstract The delivery of drugs via fast dissolving films is an effective alternative for drugs with low bioavailability when administered by other routes. This is the case of domperidone (DMP) an anti-emetic drug with low ... |
PMC5901014 | core_pubmed_pmc | Effect of Study Design on Sample Size in Studies Intended to Evaluate Bioequivalence of Inhaled Short‐Acting β‐Agonist Formulations | Effect of Study Design on Sample Size in Studies Intended to Evaluate Bioequivalence of Inhaled Short‐Acting β‐Agonist Formulations Abstract Abstract Pharmacodynamic studies that use methacholine challenge to assess bioequivalence of generic and innovator albuterol formulations are generally designed per published Food... |
PMC12895846 | core_pubmed_pmc | Therapeutic potential of acidic cannabinoids: an update | Therapeutic potential of acidic cannabinoids: an update Abstract Cannabis sativa yields a wide range of bioactive compounds, including terpenes, flavonoids, and cannabinoids. Tetrahydrocannabinolic acid (THCA), cannabidiolic acid (CBDA), cannabigerolic acid (CBGA), and cannabichromenic acid (CBCA) are the acidic biosyn... |
PMC11209285 | core_pubmed_pmc | Exploring the Impact of Efavirenz on Aflatoxin B1 Metabolism: Insights from a Physiologically Based Pharmacokinetic Model and a Human Liver Microsome Study | Exploring the Impact of Efavirenz on Aflatoxin B1 Metabolism: Insights from a Physiologically Based Pharmacokinetic Model and a Human Liver Microsome Study Abstract Abstract Physiologically based pharmacokinetic (PBPK) models were utilized to investigate potential interactions between aflatoxin B1 (AFB1) and efavirenz ... |
PMC8742634 | core_pubmed_pmc | Exploratory window‐of‐opportunity trial to investigate the tumor pharmacokinetics/pharmacodynamics of the IAP antagonist Debio 1143 in patients with head and neck cancer | Exploratory window‐of‐opportunity trial to investigate the tumor pharmacokinetics/pharmacodynamics of the IAP antagonist Debio 1143 in patients with head and neck cancer Abstract Abstract Inhibitor of apoptosis proteins (IAPs) regulate apoptosis and modulate NF‐κB signaling thereby driving expression of genes involved ... |
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