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PMC4623496 | core_pubmed_pmc | Comparison of methods for the analysis of therapeutic immunoglobulin G Fc-glycosylation profiles—Part 1: Separation-based methods | Comparison of methods for the analysis of therapeutic immunoglobulin G Fc-glycosylation profiles—Part 1: Separation-based methods Abstract Abstract Immunoglobulin G (IgG) crystallizable fragment (Fc) glycosylation is crucial for antibody effector functions, such as antibody-dependent cell-mediated cytotoxicity, and for... |
PMC8481180 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Tolerability of AZD5718, an Oral 5-Lipoxygenase-Activating Protein (FLAP) Inhibitor, in Healthy Japanese Male Subjects | Pharmacokinetics, Pharmacodynamics, and Tolerability of AZD5718, an Oral 5-Lipoxygenase-Activating Protein (FLAP) Inhibitor, in Healthy Japanese Male Subjects Abstract Background and Objective AZD5718, a 5-lipoxygenase-activating protein (FLAP) inhibitor, is in clinical development for treatment of coronary artery dise... |
PMC10684612 | core_pubmed_pmc | Plasma Pharmacokinetics of N-Acetylgalactosamine-Conjugated Small-Interfering Ribonucleic Acids (GalNAc-Conjugated siRNAs) | Plasma Pharmacokinetics of N-Acetylgalactosamine-Conjugated Small-Interfering Ribonucleic Acids (GalNAc-Conjugated siRNAs) Abstract Small-interfering ribonucleic acids (siRNAs) with N-acetylgalactosamine (GalNAc) conjugation for improved liver uptake represent an emerging class of drugs that modulate liver-expressed th... |
PMC3120766 | core_pubmed_pmc | Quantitative Whole Body Biodistribution of Fluorescent-Labeled Agents by Non-Invasive Tomographic Imaging | Quantitative Whole Body Biodistribution of Fluorescent-Labeled Agents by Non-Invasive Tomographic Imaging Abstract When small molecules or proteins are injected into live animals, their physical and chemical properties will significantly affect pharmacokinetics, tissue penetration, and the ultimate routes of metabolism... |
PMC11077957 | core_pubmed_pmc | A ketogenic diet enhances fluconazole efficacy in murine models of systemic fungal infection | A ketogenic diet enhances fluconazole efficacy in murine models of systemic fungal infection Abstract ABSTRACT Invasive fungal infections are a significant public health concern, with mortality rates ranging from 20% to 85% despite current treatments. Therefore, we examined whether a ketogenic diet could serve as a suc... |
PMC11347206 | core_pubmed_pmc | Antibiotic pharmacokinetics in infected pleural effusions | Antibiotic pharmacokinetics in infected pleural effusions Abstract Abstract Pleural infection is usually treated with empirical broad-spectrum antibiotics, but limited data exist on their penetrance into the infected pleural space. We performed a pharmacokinetic study analysing the concentration of five intravenous ant... |
PMC9981820 | core_pubmed_pmc | Time–Action Profile of Technosphere Insulin in Children with Type 1 Diabetes | Time–Action Profile of Technosphere Insulin in Children with Type 1 Diabetes Abstract Abstract Introduction Technosphere insulin (TI) is an inhaled dry powder ultra-rapid-acting insulin. This report describes the results of the first study of TI in children with type 1 diabetes (T1D). Methods Pharmacokinetics (PK) of T... |
PMC9782298 | core_pubmed_pmc | Optimising Fluvoxamine Maternal/Fetal Exposure during Gestation: A Pharmacokinetic Virtual Clinical Trials Study | Optimising Fluvoxamine Maternal/Fetal Exposure during Gestation: A Pharmacokinetic Virtual Clinical Trials Study Abstract Abstract Fluvoxamine plasma concentrations have been shown to decrease throughout pregnancy. CYP2D6 polymorphisms significantly influence these changes. However, knowledge of an optimum dose adjustm... |
PMC6966184 | core_pubmed_pmc | Evaluation of QT Liability for PF‐05251749 in the Presence of Potential Circadian Rhythm Modification | Evaluation of QT Liability for PF‐05251749 in the Presence of Potential Circadian Rhythm Modification Abstract Abstract PF‐05251749 is a dual inhibitor of casein kinase 1 δ/ε, key regulators of circadian rhythm. As a result of its mechanism of action, PF‐05251749 may also change the heart rate corrected QT (QTc) circad... |
PMC8783908 | core_pubmed_pmc | First-in-human phase 1 study of budigalimab, an anti-PD-1 inhibitor, in patients with non-small cell lung cancer and head and neck squamous cell carcinoma | First-in-human phase 1 study of budigalimab, an anti-PD-1 inhibitor, in patients with non-small cell lung cancer and head and neck squamous cell carcinoma Abstract Abstract Background Budigalimab is a humanized, recombinant immunoglobulin G1 monoclonal antibody targeting programmed cell death protein 1 (PD-1). We prese... |
PMC11885842 | core_pubmed_pmc | RSM and AI based machine learning for quality by design development of rivaroxaban push-pull osmotic tablets and its PBPK modeling | RSM and AI based machine learning for quality by design development of rivaroxaban push-pull osmotic tablets and its PBPK modeling Abstract Abstract The study is based on applying Artificial Neural Network (ANN) based machine learning and Response Surface Methodology (RSM) as simultaneous bivariate approaches in develo... |
PMC11017203 | core_pubmed_pmc | Physiologically based modeling reveals different risk of respiratory depression after fentanyl overdose between adults and children | Physiologically based modeling reveals different risk of respiratory depression after fentanyl overdose between adults and children Abstract Abstract Despite a rapid increase in pediatric mortality rate from prescription and illicit opioids, there is limited research on the dose‐dependent impact of opioids on respirato... |
PMC12651555 | core_pubmed_pmc | Evaluation of Aminoglycoside Dosing Regimens Adjusted for Renal Function and In Vitro Susceptibility Test Interpretive Criteria for Enterobacterales and Pseudomonas aeruginosa | Evaluation of Aminoglycoside Dosing Regimens Adjusted for Renal Function and In Vitro Susceptibility Test Interpretive Criteria for Enterobacterales and Pseudomonas aeruginosa Abstract Abstract Background Appropriate in vitro susceptibility testing interpretive criteria (STIC) are crucial to ensure optimal patient care... |
PMC7066534 | core_pubmed_pmc | Phase I and pharmacokinetic study of the vascular‐disrupting agent CKD‐516 (NOV120401) in patients with refractory solid tumors | Phase I and pharmacokinetic study of the vascular‐disrupting agent CKD‐516 (NOV120401) in patients with refractory solid tumors Abstract Abstract We report a phase I pharmacological study of an oral formulation of CKD‐516, a vascular‐disrupting agent, in patients with refractory solid tumors. Twenty‐seven patients (16 ... |
PMC10227923 | core_pubmed_pmc | Computational Studies Applied to Linalool and Citronellal Derivatives Against Alzheimer's and Parkinson's Disorders: A Review with Experimental Approach | Computational Studies Applied to Linalool and Citronellal Derivatives Against Alzheimer's and Parkinson's Disorders: A Review with Experimental Approach Abstract Abstract Alzheimer's and Parkinson's are neurodegenerative disorders that affect a great number of people around the world, seriously compromising the quality... |
PMC12272312 | core_pubmed_pmc | Dose Selection for DuoBody ®‐ CD40x4 ‐ 1BB ( GEN1042 / BNT312 ) Using a mPBPK / RO Model Leveraging Preclinical and Clinical Data | Dose Selection for DuoBody ®‐ CD40x4 ‐ 1BB ( GEN1042 / BNT312 ) Using a mPBPK / RO Model Leveraging Preclinical and Clinical Data Abstract Optimizing target engagement for bispecific antibodies (bsAbs) is challenging, as bsAbs bind to two different targets in vivo to form a trimolecular complex (trimer), and likely dis... |
PMC6132866 | core_pubmed_pmc | Pharmacodynamic modelling of resistance to epidermal growth factor receptor inhibition in brain metastasis mouse models | Pharmacodynamic modelling of resistance to epidermal growth factor receptor inhibition in brain metastasis mouse models Abstract Abstract Purpose Epidermal growth factor receptor (EGFR) is thought to play a role in the regulation of cell proliferation; with its activation stimulating tumour growth. EGFR inhibitors have... |
PMC7238185 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects | Population Pharmacokinetic Analysis of Tiropramide in Healthy Korean Subjects Abstract Abstract The purpose of this study was to perform population pharmacokinetic (PPK) analysis of tiropramide in healthy Korean subjects, as well as to investigate the possible effects of various covariates on pharmacokinetic (PK) param... |
PMC8547841 | core_pubmed_pmc | Simultaneous measurement of tadehaginoside and its principal metabolite in rats by HPLC–MS/MS and its application in pharmacokinetics and tissue distribution study | Simultaneous measurement of tadehaginoside and its principal metabolite in rats by HPLC–MS/MS and its application in pharmacokinetics and tissue distribution study Abstract Abstract Context Tadehaginoside, an active ingredient isolated from Tadehagi triquetrum (Linn.) Ohashi (Leguminosae), exhibited various biological ... |
PMC9284491 | core_pubmed_pmc | AMEERA-1 phase 1/2 study of amcenestrant, SAR439859, in postmenopausal women with ER-positive/HER2-negative advanced breast cancer | AMEERA-1 phase 1/2 study of amcenestrant, SAR439859, in postmenopausal women with ER-positive/HER2-negative advanced breast cancer Abstract AMEERA-1 is a Phase 1/2 open-label single-arm study evaluating once-daily (QD) amcenestrant, an orally bioavailable selective estrogen receptor (ER) degrader, in postmenopausal wom... |
PMC11265130 | core_pubmed_pmc | ENDOLUNG trial. A phase 1/2 study of the Akt/mTOR inhibitor and autophagy inducer Ibrilatazar (ABTL0812) in combination with paclitaxel/carboplatin in patients with advanced/recurrent endometrial cancer | ENDOLUNG trial. A phase 1/2 study of the Akt/mTOR inhibitor and autophagy inducer Ibrilatazar (ABTL0812) in combination with paclitaxel/carboplatin in patients with advanced/recurrent endometrial cancer Abstract Background Carboplatin and paclitaxel (CP) have been the standard of care for advanced/recurrent endometrial... |
PMC11292202 | core_pubmed_pmc | Bystander Effects, Pharmacokinetics, and Linker-Payload Stability of EGFR-Targeting Antibody-Drug Conjugates Losatuxizumab Vedotin and Depatux-M in Glioblastoma Models | Bystander Effects, Pharmacokinetics, and Linker-Payload Stability of EGFR-Targeting Antibody-Drug Conjugates Losatuxizumab Vedotin and Depatux-M in Glioblastoma Models Abstract Abstract Purpose: Antibody-drug conjugates (ADC) are targeted therapies with robust efficacy in solid cancers, and there is intense interest in... |
PMC7424564 | core_pubmed_pmc | ZYBT1, a potent, irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer | ZYBT1, a potent, irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer Abstract Abstract Bruton's tyrosine kinase (BTK) plays a central and pivotal role in controlling the pathways involved in the pathobiology of cancer, rheumatoid arthriti... |
PMC9478925 | core_pubmed_pmc | Applying a clinical lens to animal models of CAR-T cell therapies | Applying a clinical lens to animal models of CAR-T cell therapies Abstract Abstract Chimeric antigen receptor (CAR)-T cells have emerged as a promising treatment modality for various hematologic and solid malignancies over the past decade. Animal models remain the cornerstone of pre-clinical evaluation of human CAR-T c... |
PMC9249689 | core_pubmed_pmc | An Integral Pharmacokinetic Analysis of Piperacillin and Tazobactam in Plasma and Urine in Critically Ill Patients | An Integral Pharmacokinetic Analysis of Piperacillin and Tazobactam in Plasma and Urine in Critically Ill Patients Abstract Background and Objectives Although dose optimization studies have been performed for piperacillin and tazobactam separately, a combined integral analysis is not yet reported. As piperacillin and t... |
PMC9227141 | core_pubmed_pmc | The Effect of Pregnancy and Inflammatory Bowel Disease on the Pharmacokinetics of Drugs Related to Inflammatory Bowel Disease—A Systematic Literature Review | The Effect of Pregnancy and Inflammatory Bowel Disease on the Pharmacokinetics of Drugs Related to Inflammatory Bowel Disease—A Systematic Literature Review Abstract Abstract Due to ethical and practical reasons, a knowledge gap exists on the pharmacokinetics (PK) of inflammatory bowel disease (IBD)-related drugs in pr... |
PMC4255937 | core_pubmed_pmc | A methodological framework for drug development in rare diseases | A methodological framework for drug development in rare diseases Abstract Introduction Developing orphan drugs is challenging because of their severity and the requisite for effective drugs. The small number of patients does not allow conducting adequately powered randomized controlled trials (RCTs). There is a need to... |
PMC5561046 | core_pubmed_pmc | Cytochrome P450/ABC transporter inhibition simultaneously enhances ivermectin pharmacokinetics in the mammal host and pharmacodynamics in Anopheles gambiae | Cytochrome P450/ABC transporter inhibition simultaneously enhances ivermectin pharmacokinetics in the mammal host and pharmacodynamics in Anopheles gambiae Abstract Abstract Mass administration of endectocides, drugs that kill blood-feeding arthropods, has been proposed as a complementary strategy to reduce malaria tra... |
PMC8928966 | core_pubmed_pmc | Renadirsen, a Novel 2′OMeRNA/ENA ® Chimera Antisense Oligonucleotide, Induces Robust Exon 45 Skipping for Dystrophin In Vivo | Renadirsen, a Novel 2′OMeRNA/ENA ® Chimera Antisense Oligonucleotide, Induces Robust Exon 45 Skipping for Dystrophin In Vivo Abstract Abstract Duchenne muscular dystrophy (DMD) is a progressive muscle-wasting disease caused by out-of-frame or nonsense mutation in the dystrophin gene. It begins with a loss of ambulation... |
PMC4147052 | core_pubmed_pmc | Lower Exposure and Faster Clearance of Bevacizumab in Gastric Cancer and the Impact of Patient Variables: Analysis of Individual Data from AVAGAST Phase III Trial | Lower Exposure and Faster Clearance of Bevacizumab in Gastric Cancer and the Impact of Patient Variables: Analysis of Individual Data from AVAGAST Phase III Trial Abstract Altered pharmacokinetics of antibody drugs has been reported in advanced gastric cancer (AGC). We aim to evaluate bevacizumab pharmacokinetics in AG... |
PMC11802250 | core_pubmed_pmc | Pharmacokinetics and Safety of Pemafibrate in Patients with both Dyslipidemia and Severe Renal Impairment: A Phase 4 Study | Pharmacokinetics and Safety of Pemafibrate in Patients with both Dyslipidemia and Severe Renal Impairment: A Phase 4 Study Abstract Aims: Per the package insert, pemafibrate was contraindicated for use in patients with severe renal impairment despite its biliary excretion. To validate this, we evaluated the pharmacokin... |
PMC12870795 | core_pubmed_pmc | Current use of pre-clinical models for evaluation of human adenovirus-based cancer therapeutics | Current use of pre-clinical models for evaluation of human adenovirus-based cancer therapeutics Abstract Human adenoviruses (HAdVs) are enjoying a renaissance in interest for the development of cancer therapies following the approval of Adstiladrin (Ferring Pharmaceuticals) for the treatment of bladder cancer, strong p... |
PMC6282936 | core_pubmed_pmc | Evaluation of Potential Disease‐Mediated Drug–Drug Interaction in Patients With Moderate‐to‐Severe Atopic Dermatitis Receiving Dupilumab | Evaluation of Potential Disease‐Mediated Drug–Drug Interaction in Patients With Moderate‐to‐Severe Atopic Dermatitis Receiving Dupilumab Abstract Abstract This open‐label drug–drug interaction study assessed whether blockade by dupilumab of interleukin (IL)‐4 and IL‐13 signaling affects the pharmacokinetics of drugs me... |
PMC9715613 | core_pubmed_pmc | Identification of potential extracellular signal-regulated protein kinase 2 inhibitors based on multiple virtual screening strategies | Identification of potential extracellular signal-regulated protein kinase 2 inhibitors based on multiple virtual screening strategies Abstract Abstract The integration of multiple virtual screening strategies facilitates the balance of computational efficiency and prediction accuracy. In this study, we constructed an e... |
PMC9926492 | core_pubmed_pmc | Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis | Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis Abstract Mycobacterium tuberculosis cytochrome bd quinol oxidase (cyt bd ), the alternative terminal oxidase of the respiratory chain, has been i... |
PMC11282117 | core_pubmed_pmc | Challenges in Pharmacokinetic Modelling of [ 18 F]fluoro-PEG-folate PET/CT Imaging in Epithelial Ovarian Cancer Patients | Challenges in Pharmacokinetic Modelling of [ 18 F]fluoro-PEG-folate PET/CT Imaging in Epithelial Ovarian Cancer Patients Abstract Abstract Purpose To describe the pharmacokinetic properties of the [ 18 F]fluoro-polyethylene glycol(PEG)-folate radiotracer in PET/CT imaging of patients with advanced stage epithelial ovar... |
PMC10359479 | core_pubmed_pmc | Investigation of preclinical pharmacokinetics of N -demethylsinomenine, a potential novel analgesic candidate, using an UPLC-MS/MS quantification method | Investigation of preclinical pharmacokinetics of N -demethylsinomenine, a potential novel analgesic candidate, using an UPLC-MS/MS quantification method Abstract Abstract N- Demethylsinomenine (NDSM), the in vivo demethylated metabolite of sinomenine, has exhibited antinociceptive efficacy against various pain models a... |
PMC12428713 | core_pubmed_pmc | Molecular Aspects of Geriatric Pharmacotherapy | Molecular Aspects of Geriatric Pharmacotherapy Abstract Abstract Pharmacotherapy in the geriatric population is one of the greatest challenges in modern medicine. Elderly patients, characterized by multimorbidity and the resulting polypharmacy, are significantly more exposed to adverse drug reactions (ADRs), which ofte... |
PMC4608262 | core_pubmed_pmc | Using water–solvent systems to estimate in vivo blood–tissue partition coefficients | Using water–solvent systems to estimate in vivo blood–tissue partition coefficients Abstract Abstract Background Blood–tissue partition coefficients indicate how a chemical will distribute throughout the body and are an important part of any pharmacokinetic study. They can be used to assess potential toxicological effe... |
PMC6472033 | core_pubmed_pmc | Stereo-Selective Pharmacokinetics of Ilimaquinone Epimers Extracted from a Marine Sponge in Rats | Stereo-Selective Pharmacokinetics of Ilimaquinone Epimers Extracted from a Marine Sponge in Rats Abstract Abstract An ilimquinone (IQ) mixture isolated from Hippiospongia metachromia , consisting of IQ and epi-ilimaquinone (epi-IQ), exerts anti-HIV, anti-microbial, anti-inflammatory, and anti-cancer effects. An HPLC-MS... |
PMC5056486 | core_pubmed_pmc | Individualized prophylaxis for optimizing hemophilia care: can we apply this to both developed and developing nations? | Individualized prophylaxis for optimizing hemophilia care: can we apply this to both developed and developing nations? Abstract Abstract Prophylaxis is considered optimal care for hemophilia patients to prevent bleeding and to preserve joint function thereby improving quality of life (QoL). The evidence for prophylaxis... |
PMC3428524 | core_pubmed_pmc | Pharmacokinetics of sepantronium bromide (YM155), a small-molecule suppressor of survivin, in Japanese patients with advanced solid tumors: dose proportionality and influence of renal impairment | Pharmacokinetics of sepantronium bromide (YM155), a small-molecule suppressor of survivin, in Japanese patients with advanced solid tumors: dose proportionality and influence of renal impairment Abstract Abstract Purpose The purpose of this analysis was to investigate the pharmacokinetics (PK) of sepantronium (YM155), ... |
PMC6187748 | core_pubmed_pmc | Antipsychotic Drugs: From Receptor-binding Profiles to Metabolic Side Effects | Antipsychotic Drugs: From Receptor-binding Profiles to Metabolic Side Effects Abstract Background: Antipsychotic-induced metabolic side effects are major concerns in psychopharmacology and clinical psychiatry. Their pathogenetic mechanisms are still not elucidated. Methods: Herein, we review the impact of neurotransmit... |
PMC8763762 | core_pubmed_pmc | Improved pharmacokinetic and pharmacodynamic profile of a novel PEGylated native Erwinia chrysanthemi L-Asparaginase | Improved pharmacokinetic and pharmacodynamic profile of a novel PEGylated native Erwinia chrysanthemi L-Asparaginase Abstract Introduction . Erwinase® (native Erwinia chrysanthemi L-Asparaginase (nErA)) is an approved second-line treatment for acute lymphoblastic leukaemia (ALL) in children and adolescents, who develop... |
PMC10578235 | core_pubmed_pmc | DEVOTE Study Exploring Higher Dose of Nusinersen in Spinal Muscular Atrophy: Study Design and Part A Results | DEVOTE Study Exploring Higher Dose of Nusinersen in Spinal Muscular Atrophy: Study Design and Part A Results Abstract Abstract Background: Pharmacokinetic/pharmacodynamic modeling indicates that the higher dose of nusinersen may be associated with a clinically meaningful increase in efficacy above that seen with the 12... |
PMC11876874 | core_pubmed_pmc | First-in-human phase I study to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, immunogenicity, and antitumor activity of PF-07209960 in patients with advanced or metastatic solid tumors | First-in-human phase I study to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, immunogenicity, and antitumor activity of PF-07209960 in patients with advanced or metastatic solid tumors Abstract Background PF-07209960 is an antibody–cytokine fusion molecule that consists of a single potency-reduced ... |
PMC7653034 | core_pubmed_pmc | A Phase 1 dose-escalation study to evaluate safety, pharmacokinetics and pharmacodynamics of AsiDNA, a first-in-class DNA repair inhibitor, administered intravenously in patients with advanced solid tumours | A Phase 1 dose-escalation study to evaluate safety, pharmacokinetics and pharmacodynamics of AsiDNA, a first-in-class DNA repair inhibitor, administered intravenously in patients with advanced solid tumours Abstract Background AsiDNA, a first-in-class oligonucleotide-mimicking double-stranded DNA breaks, acts as a deco... |
PMC3784064 | core_pubmed_pmc | A phase I/II study of carfilzomib 2–10-min infusion in patients with advanced solid tumors | A phase I/II study of carfilzomib 2–10-min infusion in patients with advanced solid tumors Abstract Purpose Tolerability, pharmacokinetics (PK), pharmacodynamics, and antitumor activity of carfilzomib, a selective proteasome inhibitor, administered twice weekly by 2–10-min intravenous (IV) infusion on days 1, 2, 8, 9, ... |
PMC11042112 | core_pubmed_pmc | Target-controlled infusion: A comparative, prospective, observational study of the conventional TCI pump and the novel smartphone-based application iTIVA | Target-controlled infusion: A comparative, prospective, observational study of the conventional TCI pump and the novel smartphone-based application iTIVA Abstract Background and Aims: Empirically adjusted, standard drug doses fail to address interindividual pharmacokinetic and pharmacodynamics variability. Target-contr... |
PMC10616469 | core_pubmed_pmc | Pharmacokinetics and tissue distribution of four major bioactive components of Cynanchum auriculatum extract: a UPLC–MS/MS study in normal and functional dyspepsia rats | Pharmacokinetics and tissue distribution of four major bioactive components of Cynanchum auriculatum extract: a UPLC–MS/MS study in normal and functional dyspepsia rats Abstract Introduction: Cynanchum auriculatum (CA) is usually used to treat digestive disorders, such as anorexia, enteritis, dysentery, and indigestion... |
PMC8957918 | core_pubmed_pmc | Vaginal Microbiota and Mucosal Pharmacokinetics of Tenofovir in Healthy Women Using a 90-Day Tenofovir/Levonorgestrel Vaginal Ring | Vaginal Microbiota and Mucosal Pharmacokinetics of Tenofovir in Healthy Women Using a 90-Day Tenofovir/Levonorgestrel Vaginal Ring Abstract Abstract Background A relationship between the vaginal microbiota and tenofovir (TFV) concentrations and activity after topical administration has been previously reported. Objecti... |
PMC6563007 | core_pubmed_pmc | Clinical Studies on Drug–Drug Interactions Involving Metabolism and Transport: Methodology, Pitfalls, and Interpretation | Clinical Studies on Drug–Drug Interactions Involving Metabolism and Transport: Methodology, Pitfalls, and Interpretation Abstract Abstract Many drug–drug interactions (DDIs) are based on alterations of the plasma concentrations of a victim drug due to another drug causing inhibition and/or induction of the metabolism o... |
PMC4165923 | core_pubmed_pmc | Nonresponders to Daily Paroxetine and Another SSRI in Men With Lifelong Premature Ejaculation: A Pharmacokinetic Dose-Escalation Study for a Rare Phenomenon | Nonresponders to Daily Paroxetine and Another SSRI in Men With Lifelong Premature Ejaculation: A Pharmacokinetic Dose-Escalation Study for a Rare Phenomenon Abstract Purpose Nonresponse to any selective serotonin reuptake inhibitor (SSRI) treatment is rare. In this study, we aimed to investigate ejaculation delay nonre... |
PMC11573879 | core_pubmed_pmc | Population Pharmacokinetic Quantification of CYP2D6 Activity in Codeine Metabolism in Ambulatory Surgical Patients for Model-Informed Precision Dosing | Population Pharmacokinetic Quantification of CYP2D6 Activity in Codeine Metabolism in Ambulatory Surgical Patients for Model-Informed Precision Dosing Abstract Abstract Background and Objective Codeine metabolism in humans is complex due to the involvement of multiple cytochrome P450 (CYP) enzymes, and has a strong gen... |
PMC11103997 | core_pubmed_pmc | Preparation and evaluation of fenbendazole methyl- β -cyclodextrin inclusion complexes | Preparation and evaluation of fenbendazole methyl- β -cyclodextrin inclusion complexes Abstract Abstract As an orally effective benzimidazole anthelmintic agent, fenbendazole was not only widely used in agriculture and animal husbandry to prevent and treat parasites, but also shows anti-cancer effects against several t... |
PMC8088679 | core_pubmed_pmc | Factors associated with reduced infliximab exposure in the treatment of pediatric autoimmune disorders: a cross-sectional prospective convenience sampling study | Factors associated with reduced infliximab exposure in the treatment of pediatric autoimmune disorders: a cross-sectional prospective convenience sampling study Abstract Abstract Background Inadequate systemic exposure to infliximab (IFX) is associated with treatment failure. This work evaluated factors associated with... |
PMC7892953 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Safety Relationship of Paclitaxel Liposome in Patients With Non-small Cell Lung Cancer | Population Pharmacokinetics and Exposure–Safety Relationship of Paclitaxel Liposome in Patients With Non-small Cell Lung Cancer Abstract Abstract Purpose Paclitaxel liposome (Lipusu) is the first commercialized liposomal formulation of paclitaxel. There has been little data collected on the pharmacokinetics (PK) of pac... |
PMC7452880 | core_pubmed_pmc | Investigation of Potential Drug–Drug Interactions between Peficitinib (ASP015K) and Methotrexate in Patients with Rheumatoid Arthritis | Investigation of Potential Drug–Drug Interactions between Peficitinib (ASP015K) and Methotrexate in Patients with Rheumatoid Arthritis Abstract Abstract Background Methotrexate is frequently used to treat rheumatoid arthritis. Peficitinib (ASP015K; Smyraf ® ), an oral Janus kinase inhibitor indicated for the treatment ... |
PMC12204647 | core_pubmed_pmc | Clinical efficacy, safety and pharmacokinetics of novel β-lactam/β-lactamase inhibitor combinations: a systematic review | Clinical efficacy, safety and pharmacokinetics of novel β-lactam/β-lactamase inhibitor combinations: a systematic review Abstract Abstract Background Antimicrobial resistance is a global public health threat that requires urgent solutions. One strategy to decrease resistance of Gram-negative bacteria (GNB) to β-lactam ... |
PMC12137978 | core_pubmed_pmc | Design, molecular characterization and therapeutic investigation of a novel CCR8 peptide antagonist that attenuates acute liver injury by inhibiting infiltration and activation of macrophages | Design, molecular characterization and therapeutic investigation of a novel CCR8 peptide antagonist that attenuates acute liver injury by inhibiting infiltration and activation of macrophages Abstract During liver injury, intrahepatic macrophage compartment is augmented by circulating monocytes that infiltrate the live... |
PMC11542141 | core_pubmed_pmc | The novel ROCK2 selective inhibitor NRL-1049 preserves the blood-brain barrier after acute injury | The novel ROCK2 selective inhibitor NRL-1049 preserves the blood-brain barrier after acute injury Abstract Abstract Endothelial blood-brain barrier (BBB) dysfunction is critical in the pathophysiology of brain injury. Rho-associated protein kinase (ROCK) activation disrupts BBB integrity in the injured brain. We aimed ... |
PMC6408865 | core_pubmed_pmc | Evolving data analysis of an Oral Lipid Tolerance Test toward the standard for the Oral Glucose Tolerance Test: Cross species modeling effects of AZD 7687 on plasma triacylglycerol | Evolving data analysis of an Oral Lipid Tolerance Test toward the standard for the Oral Glucose Tolerance Test: Cross species modeling effects of AZD 7687 on plasma triacylglycerol Abstract Abstract We have developed a novel mechanistic pharmacokinetic‐pharmacodynamic ( PK / PD ) model to describe the time course of pl... |
PMC5798776 | core_pubmed_pmc | Enhancement of pharmacokinetic and pharmacological behavior of ocular dorzolamide after factorial optimization of self-assembled nanostructures | Enhancement of pharmacokinetic and pharmacological behavior of ocular dorzolamide after factorial optimization of self-assembled nanostructures Abstract Abstract Dorzolamide hydrochloride is frequently administered for the control of the intra-ocular pressure associated with glaucoma. The aim of this study is to develo... |
PMC7575924 | core_pubmed_pmc | Shortwave Infrared-Emitting Theranostics for Breast Cancer Therapy Response Monitoring | Shortwave Infrared-Emitting Theranostics for Breast Cancer Therapy Response Monitoring Abstract Therapeutic drug monitoring (TDM) in cancer, while imperative, has been challenging due to inter-patient variability in drug pharmacokinetics. Additionally, most pharmacokinetic monitoring is done by assessments of the drugs... |
PMC6331646 | core_pubmed_pmc | Antidepressant-Like Activity of Typical Antidepressant Drugs in the Forced Swim Test and Tail Suspension Test in Mice Is Augmented by DMPX, an Adenosine A 2A Receptor Antagonist | Antidepressant-Like Activity of Typical Antidepressant Drugs in the Forced Swim Test and Tail Suspension Test in Mice Is Augmented by DMPX, an Adenosine A 2A Receptor Antagonist Abstract Abstract Unsatisfactory therapeutic effects of currently used antidepressants force to search for new pharmacological treatment strat... |
PMC11721648 | core_pubmed_pmc | Intradiscal pharmacokinetics of oral antibiotics to treat Chronic Lower Back Pain | Intradiscal pharmacokinetics of oral antibiotics to treat Chronic Lower Back Pain Abstract Oral coamoxiclav and amoxicillin, for extended dose regimens of up to 100 days, have shown benefit in the treatment of Chronic Lower Back Pain (CLBP) associated with vertebral bone oedema, known as Modic type 1 changes, which may... |
PMC9520775 | core_pubmed_pmc | Everolimus pharmacokinetics and exposure-response relationship in Japanese patients with advanced breast cancer | Everolimus pharmacokinetics and exposure-response relationship in Japanese patients with advanced breast cancer Abstract Background: Everolimus is one of the key drugs for the treatment of advanced breast cancer. The optimal target concentration range for everolimus therapy in patients with breast cancer has not yet be... |
PMC7392460 | core_pubmed_pmc | Linezolid-Associated Neurologic Adverse Events in Patients with Multidrug-Resistant Tuberculosis, France | Linezolid-Associated Neurologic Adverse Events in Patients with Multidrug-Resistant Tuberculosis, France Abstract Abstract Linezolid is one of the most effective drugs for treating multidrug-resistant tuberculosis (MDR TB), but adverse effects remain problematic. We evaluated 57 MDR TB patients who had received > 1 dos... |
PMC7751735 | core_pubmed_pmc | The Association for Human Pharmacology in the Pharmaceutical Industry London Meeting October 2019: Impending Change, Innovation, and Future Challenges | The Association for Human Pharmacology in the Pharmaceutical Industry London Meeting October 2019: Impending Change, Innovation, and Future Challenges Abstract Abstract The Association for Human Pharmacology in the Pharmaceutical Industry (AHPPI) annual meeting focused on impending change, innovation, and future challe... |
PMC8252002 | core_pubmed_pmc | Phase 1b trial of isatuximab, an anti‐CD38 monoclonal antibody, in combination with carfilzomib as treatment of relapsed/refractory multiple myeloma | Phase 1b trial of isatuximab, an anti‐CD38 monoclonal antibody, in combination with carfilzomib as treatment of relapsed/refractory multiple myeloma Abstract Abstract Background Isatuximab (Isa), an anti‐CD38 monoclonal antibody, and carfilzomib (K), a next‐generation proteasome inhibitor (PI), both have potent single‐... |
PMC11396989 | core_pubmed_pmc | Orthoflaviviral Inhibitors in Clinical Trials, Preclinical In Vivo Efficacy Targeting NS2B-NS3 and Cellular Antiviral Activity via Competitive Protease Inhibition | Orthoflaviviral Inhibitors in Clinical Trials, Preclinical In Vivo Efficacy Targeting NS2B-NS3 and Cellular Antiviral Activity via Competitive Protease Inhibition Abstract Abstract Orthoflaviviruses, including zika (ZIKV), West Nile (WNV), and dengue (DENV) virus, induce severely debilitating infections and contribute ... |
PMC7304296 | core_pubmed_pmc | Saliva for Precision Dosing of Antifungal Drugs: Saliva Population PK Model for Voriconazole Based on a Systematic Review. | Saliva for Precision Dosing of Antifungal Drugs: Saliva Population PK Model for Voriconazole Based on a Systematic Review. Abstract Abstract Precision dosing for many antifungal drugs is now recommended. Saliva sampling is considered as a non-invasive alternative to plasma sampling for therapeutic drug monitoring (TDM)... |
PMC4443604 | core_pubmed_pmc | Comparative pharmacokinetics and bioavailability of albendazole sulfoxide in sheep and goats, and dose-dependent plasma disposition in goats | Comparative pharmacokinetics and bioavailability of albendazole sulfoxide in sheep and goats, and dose-dependent plasma disposition in goats Abstract Background The aims of this study were to compare the pharmacokinetics of albendazole sulfoxide (ABZ-SO, ricobendazole) in goats and sheep at a dose of 5 mg/kg bodyweight... |
PMC6244726 | core_pubmed_pmc | Nutritional Status Differentially Alters Cytochrome P450 3A4 (CYP3A4) and Uridine 5′-Diphospho-Glucuronosyltransferase (UGT) Mediated Drug Metabolism: Effect of Short-Term Fasting and High Fat Diet on Midazolam Metabolism | Nutritional Status Differentially Alters Cytochrome P450 3A4 (CYP3A4) and Uridine 5′-Diphospho-Glucuronosyltransferase (UGT) Mediated Drug Metabolism: Effect of Short-Term Fasting and High Fat Diet on Midazolam Metabolism Abstract Abstract Background and Objectives Previous studies have shown that nutritional status ca... |
PMC12710153 | core_pubmed_pmc | Tolerability, Safety, and Pharmacokinetics of Ivermectin After Nasal Application in Healthy Adult Subjects | Tolerability, Safety, and Pharmacokinetics of Ivermectin After Nasal Application in Healthy Adult Subjects Abstract Abstract Nasal epithelium is the site of infection for SARS‐CoV2 viruses, with interactions of the viral spike protein with the ACE2 receptor of the host cell. Molecular docking studies have shown that iv... |
PMC12715037 | core_pubmed_pmc | Importance of Lysosomal Trapping and Plasmodium Parasite Infection on the Pharmacokinetics of Pyronaridine: A Physiologically Based Pharmacokinetic Model-Based Study | Importance of Lysosomal Trapping and Plasmodium Parasite Infection on the Pharmacokinetics of Pyronaridine: A Physiologically Based Pharmacokinetic Model-Based Study Abstract Abstract Background and Objective Pyronaridine is a blood schizonticide with a high blood-to-plasma ratio, effective against Plasmodium parasites... |
PMC10778198 | core_pubmed_pmc | First-in-Human Dose-Escalation Study of the Novel Oral Depsipeptide Class I-Targeting HDAC Inhibitor Bocodepsin (OKI-179) in Patients with Advanced Solid Tumors | First-in-Human Dose-Escalation Study of the Novel Oral Depsipeptide Class I-Targeting HDAC Inhibitor Bocodepsin (OKI-179) in Patients with Advanced Solid Tumors Abstract Simple Summary Histone deacetylase (HDAC) inhibitors are anti-cancer agents that have demonstrated efficacy in hematologic malignancies; however, the ... |
PMC4397403 | core_pubmed_pmc | Evaluation of Opioid Modulation in Major Depressive Disorder | Evaluation of Opioid Modulation in Major Depressive Disorder Abstract Abstract Although opioids have known antidepressant activity, their use in major depressive disorder (MDD) has been greatly limited by risk of abuse and addiction. Our aim was to determine whether opioid modulation achieved through a combination of a... |
PMC7011964 | core_pubmed_pmc | The effects of triptolide on the pharmacokinetics of sorafenib in rats and its potential mechanism | The effects of triptolide on the pharmacokinetics of sorafenib in rats and its potential mechanism Abstract Abstract Context: Combining sorafenib with triptolide could inhibit tumour growth with greater efficacy than single-agent treatment. However, their herb–drug interaction remains unknown. Objective: This study inv... |
PMC7719388 | core_pubmed_pmc | First Clinical Study with AP30663 ‐ a K Ca 2 Channel Inhibitor in Development for Conversion of Atrial Fibrillation | First Clinical Study with AP30663 ‐ a K Ca 2 Channel Inhibitor in Development for Conversion of Atrial Fibrillation Abstract Pharmacological cardioversion of atrial fibrillation (AF) is frequently inefficacious. AP30663, a small conductance Ca 2+ activated K + (K Ca 2) channel blocker, prolonged the atrial effective re... |
PMC5694499 | core_pubmed_pmc | Influence of Morbid Obesity on the Pharmacokinetics of Morphine, Morphine-3-Glucuronide, and Morphine-6-Glucuronide | Influence of Morbid Obesity on the Pharmacokinetics of Morphine, Morphine-3-Glucuronide, and Morphine-6-Glucuronide Abstract Abstract Introduction Obesity is associated with many pathophysiological changes that may result in altered drug metabolism. The aim of this study is to investigate the influence of obesity on th... |
PMC4891504 | core_pubmed_pmc | First-in-human phase I study of the DNA-repair inhibitor DT01 in combination with radiotherapy in patients with skin metastases from melanoma | First-in-human phase I study of the DNA-repair inhibitor DT01 in combination with radiotherapy in patients with skin metastases from melanoma Abstract Background: DT01 is a DNA-repair inhibitor preventing recruitment of DNA-repair enzymes at damage sites. Safety, pharmacokinetics and preliminary efficacy through intrat... |
PMC7359121 | core_pubmed_pmc | An Open-Label, Randomized, Single-Dose, Crossover, Comparative Pharmacokinetics Study of YLB113 and the Etanercept Reference Product in Healthy Adult Male Subjects | An Open-Label, Randomized, Single-Dose, Crossover, Comparative Pharmacokinetics Study of YLB113 and the Etanercept Reference Product in Healthy Adult Male Subjects Abstract Background and Objectives YLB113 is being developed as a biosimilar of the antitumor necrosis factor-alpha antagonist etanercept, which is approved... |
PMC4421097 | core_pubmed_pmc | The Effect of Pioglitazone on Pharmacokinetics of Carbamazepine in Healthy Rabbits | The Effect of Pioglitazone on Pharmacokinetics of Carbamazepine in Healthy Rabbits Abstract Abstract Introduction Drug–drug interactions can lead to serious and potentially lethal adverse events. In recent years, several drugs have been withdrawn from the market due to interaction-related adverse events. The objective ... |
PMC10220677 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Rationale for Extending VEGF Inhibition Increasing Intravitreal Aflibercept Dose | Pharmacokinetic and Pharmacodynamic Rationale for Extending VEGF Inhibition Increasing Intravitreal Aflibercept Dose Abstract Background: The effects of various dosages and treatment regimens on intravitreal aflibercept concentrations and the proportion of free vascular endothelial growth factor (VEGF) to total VEGF we... |
PMC9819210 | core_pubmed_pmc | Population Pharmacokinetics of Nivolumab in Japanese Patients with Nonsmall Cell Lung Cancer | Population Pharmacokinetics of Nivolumab in Japanese Patients with Nonsmall Cell Lung Cancer Abstract Supplemental Digital Content is Available in the Text. Key Words: nivolumab, population pharmacokinetics, real-world data, nonsmall cell lung cancer Background: Nivolumab is an antiprogrammed death-1 (PD-1) antibody us... |
PMC12845078 | core_pubmed_pmc | Unraveling Cannabidiol’s Bidirectional Regulation of Melatonin Pharmacokinetics via PEPT1/CYP1A2: Mechanistic Insights and Quantitative Projections | Unraveling Cannabidiol’s Bidirectional Regulation of Melatonin Pharmacokinetics via PEPT1/CYP1A2: Mechanistic Insights and Quantitative Projections Abstract Abstract Background: Chronic insomnia is associated with elevated cardiovascular disease risk, and current therapeutic options for this condition remain inadequate... |
PMC4412688 | core_pubmed_pmc | Narrow therapeutic index drugs: a clinical pharmacological consideration to flecainide | Narrow therapeutic index drugs: a clinical pharmacological consideration to flecainide Abstract Abstract Purpose The therapeutic index (TI) is the range of doses at which a medication is effective without unacceptable adverse events. Drugs with a narrow TI (NTIDs) have a narrow window between their effective doses and ... |
PMC7660510 | core_pubmed_pmc | Soluble dimeric prion protein ligand activates Adgrg6 receptor but does not rescue early signs of demyelination in PrP-deficient mice | Soluble dimeric prion protein ligand activates Adgrg6 receptor but does not rescue early signs of demyelination in PrP-deficient mice Abstract The adhesion G-protein coupled receptor Adgrg6 (formerly Gpr126) is instrumental in the development, maintenance and repair of peripheral nervous system myelin. The prion protei... |
PMC11871479 | core_pubmed_pmc | Enhanced transdermal delivery of pioglitazone hydrochloride via conductive hydrogel microneedles combined with iontophoresis | Enhanced transdermal delivery of pioglitazone hydrochloride via conductive hydrogel microneedles combined with iontophoresis Abstract The conventional oral administration of pioglitazone for Type II diabetes management is frequently compromised by hepatic first-pass metabolism and associated systemic adverse effects, n... |
PMC10579053 | core_pubmed_pmc | Elranatamab in relapsed or refractory multiple myeloma: the MagnetisMM-1 phase 1 trial | Elranatamab in relapsed or refractory multiple myeloma: the MagnetisMM-1 phase 1 trial Abstract Multiple myeloma (MM) is a plasma cell malignancy expressing B cell maturation antigen (BCMA). Elranatamab, a bispecific antibody, engages BCMA on MM and CD3 on T cells. The MagnetisMM-1 trial evaluated its safety, pharmacok... |
PMC12272318 | core_pubmed_pmc | Exploring the Association Between Intra‐Patient Variability in Trough Concentration of Pazopanib and Clinical Outcomes in Renal Cell Carcinoma and Soft Tissue Sarcoma Patients | Exploring the Association Between Intra‐Patient Variability in Trough Concentration of Pazopanib and Clinical Outcomes in Renal Cell Carcinoma and Soft Tissue Sarcoma Patients Abstract Abstract Pazopanib is an oral tyrosine kinase inhibitor used in patients with either metastatic renal cell carcinoma or soft tissue sar... |
PMC6587493 | core_pubmed_pmc | Pharmacodynamic biomarkers and differential effects of TNF ‐ and GM ‐ CSF ‐targeting biologics in rheumatoid arthritis | Pharmacodynamic biomarkers and differential effects of TNF ‐ and GM ‐ CSF ‐targeting biologics in rheumatoid arthritis Abstract Abstract Aim The aim of our study was to identify pharmacodynamic biomarkers and assess differential effects of tumor necrosis factor ( TNF )‐ and non‐ TNF ‐targeting agents on rheumatoid arth... |
PMC8658774 | core_pubmed_pmc | Berberine as a Potential Anticancer Agent: A Comprehensive Review | Berberine as a Potential Anticancer Agent: A Comprehensive Review Abstract Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present review consolidates salient information concernin... |
PMC3309443 | core_pubmed_pmc | Pharmacokinetics of mycophenolic acid and its phenyl glucuronide metabolite in kidney transplant recipients with renal impairment | Pharmacokinetics of mycophenolic acid and its phenyl glucuronide metabolite in kidney transplant recipients with renal impairment Abstract Introduction The aim of the study was to analyse the influence of renal impairment on the pharmacokinetic parameters (PK) of mycophenolic acid (MPA) and its glucuronide metabolite (... |
PMC10648799 | core_pubmed_pmc | Innovative Phospholipid Carriers: A Viable Strategy to Counteract Antimicrobial Resistance | Innovative Phospholipid Carriers: A Viable Strategy to Counteract Antimicrobial Resistance Abstract The overuse and misuse of antibiotics have led to the emergence and spread of multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria strains, usually associated with poorer pat... |
PMC9316313 | core_pubmed_pmc | Biochemical Properties of Atranorin-Induced Behavioral and Systematic Changes of Laboratory Rats | Biochemical Properties of Atranorin-Induced Behavioral and Systematic Changes of Laboratory Rats Abstract Atranorin (ATR) is a secondary metabolite of lichens. While previous studies investigated the effects of this substance predominantly in an in vitro environment, in our study we investigated the basic physicochemic... |
PMC8268918 | core_pubmed_pmc | Exploring a combined biomarker for tuberculosis treatment response: protocol for a prospective observational cohort study | Exploring a combined biomarker for tuberculosis treatment response: protocol for a prospective observational cohort study Abstract Introduction An improved understanding of factors explaining tuberculosis (TB) treatment response is urgently needed to help clinicians optimise and personalise treatment and assist scienti... |
PMC5962569 | core_pubmed_pmc | Molecular Size Modulates Pharmacokinetics, Biodistribution, and Renal Deposition of the Drug Delivery Biopolymer Elastin-like Polypeptide | Molecular Size Modulates Pharmacokinetics, Biodistribution, and Renal Deposition of the Drug Delivery Biopolymer Elastin-like Polypeptide Abstract Abstract Elastin-like polypeptides (ELP) are engineered proteins that consist of repetitions of a five amino acid motif, and their composition is easily modified to adjust t... |
PMC12189962 | core_pubmed_pmc | Ability of Linezolid to Combat Staphylococcus aureus and Pseudomonas aeruginosa Isolated from Polymicrobial Wound Infections | Ability of Linezolid to Combat Staphylococcus aureus and Pseudomonas aeruginosa Isolated from Polymicrobial Wound Infections Abstract Background/Objectives : The optimal therapy for polymicrobial wound infections is poorly defined. We sought to characterize the ability of linezolid to combat mixed cultures of Staphyloc... |
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