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PMC11620482 | core_pubmed_pmc | Phase 1 drug-drug interaction study to assess the effect of CYP3A4 inhibition and pan-CYP induction on the pharmacokinetics and safety of fosmanogepix in healthy participants | Phase 1 drug-drug interaction study to assess the effect of CYP3A4 inhibition and pan-CYP induction on the pharmacokinetics and safety of fosmanogepix in healthy participants Abstract ABSTRACT Immunocompromised patients are susceptible to fungal infections, and drug-drug interactions with antifungals may occur due to c... |
PMC5702897 | core_pubmed_pmc | Combining “Bottom‐up” and “Top‐down” Approaches to Assess the Impact of Food and Gastric pH on Pictilisib (GDC‐0941) Pharmacokinetics | Combining “Bottom‐up” and “Top‐down” Approaches to Assess the Impact of Food and Gastric pH on Pictilisib (GDC‐0941) Pharmacokinetics Abstract Pictilisib, a weakly basic compound, is an orally administered, potent, and selective pan‐inhibitor of phosphatidylinositol 3‐kinases for oncology indications. To investigate th... |
PMC12486830 | core_pubmed_pmc | Piperacillin reaches high concentrations in bile and target tissues of the biliary system: an experimental study in pigs | Piperacillin reaches high concentrations in bile and target tissues of the biliary system: an experimental study in pigs Abstract ABSTRACT The antibiotic combination of piperacillin/tazobactam (TZP) is commonly utilized for preventing and treating infections in the biliary system, with piperacillin being the primary ag... |
PMC6572212 | core_pubmed_pmc | Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation | Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation Abstract Abstract Background and Objectives: Lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) have resurged the eminence of nanoemulsions by modest adjustments and offer... |
PMC9502080 | core_pubmed_pmc | Adoption of Machine Learning in Pharmacometrics: An Overview of Recent Implementations and Their Considerations | Adoption of Machine Learning in Pharmacometrics: An Overview of Recent Implementations and Their Considerations Abstract Pharmacometrics is a multidisciplinary field utilizing mathematical models of physiology, pharmacology, and disease to describe and quantify the interactions between medication and patient. As these ... |
PMC4228152 | core_pubmed_pmc | The effect of the novel phosphodiesterase-4 inhibitor MEM 1414 on the allergen induced responses in mild asthma | The effect of the novel phosphodiesterase-4 inhibitor MEM 1414 on the allergen induced responses in mild asthma Abstract Background Inhaled allergen challenge is a standard method to study airway responses to inflammatory provocation and evaluate the therapeutic potential of novel anti-inflammatory compounds in asthma.... |
PMC5288521 | core_pubmed_pmc | Pharmacokinetic and Toxicological Evaluation of a Zinc Gluconate-Based Chemical Sterilant Using In Vitro and In Silico Approaches | Pharmacokinetic and Toxicological Evaluation of a Zinc Gluconate-Based Chemical Sterilant Using In Vitro and In Silico Approaches Abstract Sclerosing agents as zinc gluconate-based chemical sterilants (Infertile®) are used for chemical castration. This solution is injected into the animal testis, but there are not enou... |
PMC8443793 | core_pubmed_pmc | Development, Testing, Parameterisation and Calibration of a Human PBPK Model for the Plasticiser, Di-(2-propylheptyl) Phthalate (DPHP) Using in Silico, in vitro and Human Biomonitoring Data | Development, Testing, Parameterisation and Calibration of a Human PBPK Model for the Plasticiser, Di-(2-propylheptyl) Phthalate (DPHP) Using in Silico, in vitro and Human Biomonitoring Data Abstract Abstract A physiologically based pharmacokinetic model for Di-(2-propylheptyl) phthalate (DPHP) was developed to interpre... |
PMC11257205 | core_pubmed_pmc | Determination of the anticancer activity of standardized extract of Centella asiatica (ECa 233) on cell growth and metastatic behavior in oral cancer cells | Determination of the anticancer activity of standardized extract of Centella asiatica (ECa 233) on cell growth and metastatic behavior in oral cancer cells Abstract Abstract Background and purpose: The anticancer drugs used for oral cancer treatment present many disadvantages, such as low solubility, low permeability, ... |
PMC8286988 | core_pubmed_pmc | A review on the pharmacokinetic properties and toxicity considerations for chloroquine and hydroxychloroquine to potentially treat coronavirus patients | A review on the pharmacokinetic properties and toxicity considerations for chloroquine and hydroxychloroquine to potentially treat coronavirus patients Abstract The SARS-CoV-2 virus, caused a novel emerged coronavirus disease, is growing rapidly worldwide. Few studies have evaluated the efficacy and safety of Chloroqui... |
PMC10525963 | core_pubmed_pmc | Conditionally Active, pH-Sensitive Immunoregulatory Antibodies Targeting VISTA and CTLA-4 Lead an Emerging Class of Cancer Therapeutics | Conditionally Active, pH-Sensitive Immunoregulatory Antibodies Targeting VISTA and CTLA-4 Lead an Emerging Class of Cancer Therapeutics Abstract Abstract Immune checkpoints and other immunoregulatory targets can be difficult to precisely target due to expression on non-tumor immune cells critical to maintaining immune ... |
PMC10196431 | core_pubmed_pmc | Mechanistic modeling of generic orally inhaled drug products: A workshop summary report | Mechanistic modeling of generic orally inhaled drug products: A workshop summary report Abstract Abstract In silico mechanistic modeling approaches have been designed by various stakeholders with the goal of supporting development and approval of generic orally inhaled drug products in the United States. This review su... |
PMC7891441 | core_pubmed_pmc | Evaluation of the Relationship of Glasdegib Exposure and Safety End Points in Patients With Refractory Solid Tumors and Hematologic Malignancies | Evaluation of the Relationship of Glasdegib Exposure and Safety End Points in Patients With Refractory Solid Tumors and Hematologic Malignancies Abstract Abstract Glasdegib is approved for treating acute myeloid leukemia in elderly patients at 100 mg once daily in combination with low‐dose cytarabine. Exposure‐efficacy... |
PMC8402634 | core_pubmed_pmc | Intranasal Administration of a Monoclonal Neutralizing Antibody Protects Mice against SARS-CoV-2 Infection | Intranasal Administration of a Monoclonal Neutralizing Antibody Protects Mice against SARS-CoV-2 Infection Abstract Abstract Despite the recent availability of vaccines against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2), there is an urgent need for specific anti-SARS-CoV-2 drugs. Monoclonal neutr... |
PMC7988345 | core_pubmed_pmc | Modeling of SARS-CoV-2 Treatment Effects for Informed Drug Repurposing | Modeling of SARS-CoV-2 Treatment Effects for Informed Drug Repurposing Abstract Several repurposed drugs are currently under investigation in the fight against coronavirus disease 2019 (COVID-19). Candidates are often selected solely by their effective concentrations in vitro , an approach that has largely not lived up... |
PMC10525314 | core_pubmed_pmc | Development and Validation of a High-Performance Liquid Chromatography with Tandem Mass Spectrometry (HPLC-MS/MS) Method for Quantification of Major Molnupiravir Metabolite (β-D-N4-hydroxycytidine) in Human Plasma | Development and Validation of a High-Performance Liquid Chromatography with Tandem Mass Spectrometry (HPLC-MS/MS) Method for Quantification of Major Molnupiravir Metabolite (β-D-N4-hydroxycytidine) in Human Plasma Abstract Molnupiravir is an antiviral drug against viral RNA polymerase activity approved by the FDA for t... |
PMC8674004 | core_pubmed_pmc | Regulatory utility of pharmacometrics in the development and evaluation of antimicrobial agents and its recent progress in China | Regulatory utility of pharmacometrics in the development and evaluation of antimicrobial agents and its recent progress in China Abstract Abstract Pharmacometrics is an emerging science that interprets drug, disease, and trial information in a mathematical fashion to inform and facilitate efficient drug development and... |
PMC10532907 | core_pubmed_pmc | Pharmacogenetic Variants Associated with Fluoxetine Pharmacokinetics from a Bioequivalence Study in Healthy Subjects | Pharmacogenetic Variants Associated with Fluoxetine Pharmacokinetics from a Bioequivalence Study in Healthy Subjects Abstract Fluoxetine is one of the most prescribed antidepressants, yet it still faces challenges due to high intersubject variability in patient response. Mainly metabolized by the highly polymorphic gen... |
PMC7496554 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modeling of Glenzocimab (ACT017) a Glycoprotein VI Inhibitor of Collagen‐Induced Platelet Aggregation | Population Pharmacokinetic/Pharmacodynamic Modeling of Glenzocimab (ACT017) a Glycoprotein VI Inhibitor of Collagen‐Induced Platelet Aggregation Abstract Abstract Glenzocimab (ACT017) is a humanized monoclonal antigen‐binding fragment (Fab) directed against the human platelet glycoprotein VI, a key receptor for collage... |
PMC6407737 | core_pubmed_pmc | Phase I Study of the Focal Adhesion Kinase Inhibitor BI 853520 in Japanese and Taiwanese Patients with Advanced or Metastatic Solid Tumors | Phase I Study of the Focal Adhesion Kinase Inhibitor BI 853520 in Japanese and Taiwanese Patients with Advanced or Metastatic Solid Tumors Abstract Abstract Background Focal adhesion kinase (FAK) inhibitors have demonstrated anti-tumor activity preclinically and are currently being evaluated in humans. A first-in-human... |
PMC12511766 | core_pubmed_pmc | Pharmacokinetics, safety and tolerability of ipatasertib in combination with palbociclib and fulvestrant in patients with advanced breast cancer in a phase Ib study | Pharmacokinetics, safety and tolerability of ipatasertib in combination with palbociclib and fulvestrant in patients with advanced breast cancer in a phase Ib study Abstract Introduction Ipatasertib is a potent, highly selective, small molecule AKT inhibitor that has been evaluated in combination with palbociclib and f... |
PMC7719393 | core_pubmed_pmc | Systemic Lupus Erythematosus Activity Affects the Sinusoidal Uptake Transporter OATP1B1 Evaluated by the Pharmacokinetics of Atorvastatin | Systemic Lupus Erythematosus Activity Affects the Sinusoidal Uptake Transporter OATP1B1 Evaluated by the Pharmacokinetics of Atorvastatin Abstract Abstract The present study assessed the effect of systemic lupus erythematosus (SLE) activity, a chronic and inflammatory autoimmune disease, on the sinusoidal uptake transp... |
PMC4143601 | core_pubmed_pmc | Phase I dose-escalation study of the HSP90 inhibitor AUY922 in Japanese patients with advanced solid tumors | Phase I dose-escalation study of the HSP90 inhibitor AUY922 in Japanese patients with advanced solid tumors Abstract Purpose AUY922 is a potent non-geldanamycin inhibitor of heat-shock protein 90. This study was carried out in Japanese patients to determine the maximum tolerated dose (MTD), and to characterize safety, ... |
PMC10393585 | core_pubmed_pmc | Pharmacokinetics of Apixaban Among Peritoneal Dialysis Patients | Pharmacokinetics of Apixaban Among Peritoneal Dialysis Patients Abstract Abstract Rationale & Objective The efficacy and safety profile of apixaban remains uncertain in patients receiving peritoneal dialysis (PD) despite increasing use in this population. Accordingly, we assessed the pharmacokinetics of apixaban among ... |
PMC9099122 | core_pubmed_pmc | Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women | Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women Abstract Abstract This study evaluated the effect of repeated doses of elagolix on the pharmacokinetics (PK) of omeprazole and its metabolites in healthy premenopausal female subjects. Adult premenopausal female... |
PMC3978604 | core_pubmed_pmc | Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: implications for SYK inhibitors in autoimmune disease therapy | Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: implications for SYK inhibitors in autoimmune disease therapy Abstract Abstract Introduction Spleen tyrosine kinase (SYK) is a key integrator ... |
PMC8694721 | core_pubmed_pmc | The effects of linalool acupoint application therapy on sleep regulation | The effects of linalool acupoint application therapy on sleep regulation Abstract Abstract The Shenque acupoint is located in the umbilicus of the human body. In the human body meridians, the Shenque acupoint can regulate body functions. The Shenque acupoint was one of the important acupuncture acupoints for the treatm... |
PMC11768525 | core_pubmed_pmc | Curcumin-Based Nanoparticles: Advancements and Challenges in Tumor Therapy | Curcumin-Based Nanoparticles: Advancements and Challenges in Tumor Therapy Abstract Abstract Curcumin, a bioactive compound derived from the rhizome of Curcuma longa L., has garnered significant attention for its potent anticancer properties. Despite its promising therapeutic potential, its poor bioavailability, rapid ... |
PMC6070450 | core_pubmed_pmc | The tetraamine chelator outperforms HYNIC in a new technetium-99m-labelled somatostatin receptor 2 antagonist | The tetraamine chelator outperforms HYNIC in a new technetium-99m-labelled somatostatin receptor 2 antagonist Abstract Abstract Background Somatostatin receptor targeting radiopeptides are successfully being used to image, stage, and monitor patients with neuroendocrine tumours. They are exclusively agonists that inter... |
PMC7070793 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study | Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study Abstract Excessive activation of the mineralocorticoid receptor (MR) underlies the pathophysiology of heart failure and chronic kidney disease. Hyperkalemia risk limits ... |
PMC8536414 | core_pubmed_pmc | The LC-MS/MS-Based Measurement of Isopimaric Acid in Rat Plasma and Application of Pharmacokinetics | The LC-MS/MS-Based Measurement of Isopimaric Acid in Rat Plasma and Application of Pharmacokinetics Abstract Abstract Isopimaric acid (IPA) exhibits a diverse array of pharmacological activities, having been shown to function as an antihypertensive, antitumor, antibacterial, and hypocholesterolemic agent. However, few ... |
PMC12151664 | core_pubmed_pmc | First-in-class intranasal epinephrine spray for anaphylaxis: Dose finding clinical study | First-in-class intranasal epinephrine spray for anaphylaxis: Dose finding clinical study Abstract Background Anaphylaxis is a life-threatening clinical presentation of acute systemic allergic reactions. Timely administration of epinephrine, usually by intramuscular autoinjector, is a robust life-saving treatment. Despi... |
PMC11402398 | core_pubmed_pmc | Plug-and-play nucleic acid-mediated multimerization of biparatopic nanobodies for molecular imaging | Plug-and-play nucleic acid-mediated multimerization of biparatopic nanobodies for molecular imaging Abstract Abstract In cancer molecular imaging, selecting binders with high specificity and affinity for biomarkers is paramount for achieving high-contrast imaging within clinical time frames. Nanobodies have emerged as ... |
PMC12265020 | core_pubmed_pmc | Donanemab exposure‐response in early symptomatic Alzheimer's disease | Donanemab exposure‐response in early symptomatic Alzheimer's disease Abstract Abstract INTRODUCTION These analyses aimed to identify factors impacting donanemab exposure, amyloid plaque, and clinical efficacy in early symptomatic Alzheimer's disease using a population pharmacokinetic/pharmacodynamic (PK/PD) approach. M... |
PMC8628514 | core_pubmed_pmc | Glycoengineering of Therapeutic Antibodies with Small Molecule Inhibitors | Glycoengineering of Therapeutic Antibodies with Small Molecule Inhibitors Abstract Monoclonal antibodies (mAbs) are one of the cornerstones of modern medicine, across an increasing range of therapeutic areas. All therapeutic mAbs are glycoproteins, i.e., their polypeptide chain is decorated with glycans, oligosaccharid... |
PMC10192568 | core_pubmed_pmc | Comparison of pharmacokinetic profiles of seven major bioactive components in normal and non-alcoholic fatty liver disease (NAFLD) rats after oral administration of Ling-Gui-Zhu-Gan decoction by UPLC-MS/MS | Comparison of pharmacokinetic profiles of seven major bioactive components in normal and non-alcoholic fatty liver disease (NAFLD) rats after oral administration of Ling-Gui-Zhu-Gan decoction by UPLC-MS/MS Abstract Abstract A sensitive and rapid ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/... |
PMC8368853 | core_pubmed_pmc | The varying effects of antibiotics on gut microbiota | The varying effects of antibiotics on gut microbiota Abstract Abstract Antibiotics are lifesaving therapeutic drugs that have been used by human for decades. They are used both in the fight against bacterial pathogens for both human and for animal feeding. However, of recent, their effects on the gut microbial composit... |
PMC11732010 | core_pubmed_pmc | Drug-resistant bacteria in the critically ill: patterns and mechanisms of resistance and potential remedies | Drug-resistant bacteria in the critically ill: patterns and mechanisms of resistance and potential remedies Abstract Antimicrobial resistance in the intensive care unit is an ongoing global healthcare concern associated with high mortality and morbidity rates and high healthcare costs. Select groups of bacterial pathog... |
PMC11960066 | core_pubmed_pmc | The tradeoffs between persistence and mutation rates at sub-inhibitory antibiotic concentrations in Staphylococcus aureus | The tradeoffs between persistence and mutation rates at sub-inhibitory antibiotic concentrations in Staphylococcus aureus Abstract ABSTRACT The rational design of the antibiotic treatment of bacterial infections employs these drugs to reach concentrations that exceed the minimum needed to prevent the replication of the... |
PMC3850926 | core_pubmed_pmc | Evaluation of the adverse event profile and pharmacodynamics of toceranib phosphate administered to dogs with solid tumors at doses below the maximum tolerated dose | Evaluation of the adverse event profile and pharmacodynamics of toceranib phosphate administered to dogs with solid tumors at doses below the maximum tolerated dose Abstract Background The receptor kinase inhibitor toceranib phosphate (Palladia) was approved for use in dogs in 2009 using a dose of 3.25 mg/kg administer... |
PMC9704087 | core_pubmed_pmc | Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo | Solid lipid nanoparticle as an effective drug delivery system of a novel curcumin derivative: formulation, release in vitro and pharmacokinetics in vivo Abstract Abstract Context Curcumin (Cur) has a short duration of action which limits its therapeutic efficacy. Carbonic acid 17-(1,5-dimethyl-hexyl)-10,13-dimethyl-2,3... |
PMC3525665 | core_pubmed_pmc | SLC22A1-ABCB1 Haplotype Profiles Predict Imatinib Pharmacokinetics in Asian Patients with Chronic Myeloid Leukemia | SLC22A1-ABCB1 Haplotype Profiles Predict Imatinib Pharmacokinetics in Asian Patients with Chronic Myeloid Leukemia Abstract Objective This study aimed to explore the influence of SLC22A1, PXR, ABCG2, ABCB1 and CYP3A5*3 genetic polymorphisms on imatinib mesylate (IM) pharmacokinetics in Asian patients with chronic myelo... |
PMC11434833 | core_pubmed_pmc | Pharmacokinetics of Piperacillin–Tazobactam in Critically Ill Patients with Open Abdomen and Vacuum-Assisted Wound Closure: Dosing Considerations Using Monte Carlo Simulation | Pharmacokinetics of Piperacillin–Tazobactam in Critically Ill Patients with Open Abdomen and Vacuum-Assisted Wound Closure: Dosing Considerations Using Monte Carlo Simulation Abstract Abstract Background: Open abdomen with vacuum-assisted wound closure therapy (OA/VAC) is frequently used in critically ill patients alth... |
PMC8248099 | core_pubmed_pmc | Phase 1 Renal Impairment Trial Results Supports Targeted Individualized Dosing of ELX‐02 in Patients With Nephropathic Cystinosis | Phase 1 Renal Impairment Trial Results Supports Targeted Individualized Dosing of ELX‐02 in Patients With Nephropathic Cystinosis Abstract Abstract The aim of this study was to assess the pharmacokinetics (PK) and safety of ELX‐02 in a renally impaired population and apply these findings to the individualized dosing of... |
PMC5055303 | core_pubmed_pmc | Identification and Tumour-Binding Properties of a Peptide with High Affinity to the Disialoganglioside GD2 | Identification and Tumour-Binding Properties of a Peptide with High Affinity to the Disialoganglioside GD2 Abstract Neuroectodermal tumours are characterized by aberrant processing of disialogangliosides concomitant with high expression of GD2 or GD3 on cell surfaces. Antibodies targeting GD2 are already in clinical us... |
PMC3416976 | core_pubmed_pmc | A multicenter, open-label, efficacy, pharmacokinetic, and safety study of adalimumab in Japanese patients with ankylosing spondylitis | A multicenter, open-label, efficacy, pharmacokinetic, and safety study of adalimumab in Japanese patients with ankylosing spondylitis Abstract We evaluated the efficacy, pharmacokinetics, and safety of adalimumab in Japanese patients with active ankylosing spondylitis (AS) who had an inadequate response to, or who were... |
PMC6278136 | core_pubmed_pmc | Pharmacokinetics of rivaroxaban in children using physiologically based and population pharmacokinetic modelling: an EINSTEIN-Jr phase I study | Pharmacokinetics of rivaroxaban in children using physiologically based and population pharmacokinetic modelling: an EINSTEIN-Jr phase I study Abstract Background The EINSTEIN-Jr program will evaluate rivaroxaban for the treatment of venous thromboembolism (VTE) in children, targeting exposures similar to the 20 mg onc... |
PMC7171252 | core_pubmed_pmc | Pharmacokinetics, mass balance, tissue distribution, metabolism, and excretion of praliciguat, a clinical‐stage soluble guanylate cyclase stimulator in rats | Pharmacokinetics, mass balance, tissue distribution, metabolism, and excretion of praliciguat, a clinical‐stage soluble guanylate cyclase stimulator in rats Abstract Abstract The pharmacokinetics (PK), metabolism, excretion, mass balance, and tissue distribution of [ 14 C]praliciguat were evaluated following oral admin... |
PMC6245886 | core_pubmed_pmc | Expanding behavior pattern sensitivity analysis with model selection and survival analysis | Expanding behavior pattern sensitivity analysis with model selection and survival analysis Abstract Abstract Background Sensitivity analysis is an essential step in mathematical modeling because it identifies parameters with a strong influence on model output, due to natural variation or uncertainty in the parameter va... |
PMC5443883 | core_pubmed_pmc | Developing the Totality of Evidence for Biosimilars: Regulatory Considerations and Building Confidence for the Healthcare Community | Developing the Totality of Evidence for Biosimilars: Regulatory Considerations and Building Confidence for the Healthcare Community Abstract Biosimilars are highly similar versions of approved branded biologics. Unlike generics, they are not exact replicas of reference products. Minor differences between biosimilars an... |
PMC12784657 | core_pubmed_pmc | Pharmacologic Targeting of miR29b with Bortezomib and Sorafenib to Improve Decitabine Sensitivity in Patients with Acute Myeloid Leukemia: Results from a Phase 1 Dose-Escalation Trial | Pharmacologic Targeting of miR29b with Bortezomib and Sorafenib to Improve Decitabine Sensitivity in Patients with Acute Myeloid Leukemia: Results from a Phase 1 Dose-Escalation Trial Abstract Simple Summary Decitabine is a commonly used drug for acute myeloid leukemia (AML), an aggressive blood cancer, but it does not... |
PMC12841350 | core_pubmed_pmc | Evaluation of Vortioxetine on Global DNA Methylation in Maternal and Offspring Rats and In Silico Molecular Docking to Key Epigenetic Enzymes | Evaluation of Vortioxetine on Global DNA Methylation in Maternal and Offspring Rats and In Silico Molecular Docking to Key Epigenetic Enzymes Abstract Mothers face high depression risks during pregnancy, and untreated depression can harm both mother and baby. Vortioxetine is a novel antidepressant with a multimodal mec... |
PMC8966651 | core_pubmed_pmc | PKPD Modeling of the Inoculum Effect of Acinetobacter baumannii on Polymyxin B in vivo | PKPD Modeling of the Inoculum Effect of Acinetobacter baumannii on Polymyxin B in vivo Abstract Abstract The reduction in antimicrobial activity at high bacterial counts is a microbiological phenomenon known as the inoculum effect (IE). In a previous in vitro study, a significant IE was observed for polymyxin B (PMB) a... |
PMC10707387 | core_pubmed_pmc | Illicium verum L. (Star Anise) Essential Oil: GC/MS Profile, Molecular Docking Study, In Silico ADME Profiling, Quorum Sensing, and Biofilm-Inhibiting Effect on Foodborne Bacteria | Illicium verum L. (Star Anise) Essential Oil: GC/MS Profile, Molecular Docking Study, In Silico ADME Profiling, Quorum Sensing, and Biofilm-Inhibiting Effect on Foodborne Bacteria Abstract Abstract Illicium verum , or star anise, has many uses ranging from culinary to religious. It has been used in the food industry si... |
PMC11754044 | core_pubmed_pmc | UGT2B15 single nucleotide polymorphism reduces dabigatran acylglucuronide formation in humans | UGT2B15 single nucleotide polymorphism reduces dabigatran acylglucuronide formation in humans Abstract Background Dabigatran etexilate (DABE), a prodrug of dabigatran (DAB), is a direct thrombin inhibitor used to prevent ischemic stroke and thromboembolism during atrial fibrillation. The effect of genetic polymorphisms... |
PMC12896389 | core_pubmed_pmc | A Combined Model‐Based Meta‐Analysis of Aggregated and Individual FEV1 Data From Randomized COPD Trials | A Combined Model‐Based Meta‐Analysis of Aggregated and Individual FEV1 Data From Randomized COPD Trials Abstract ABSTRACT Model‐based meta‐analysis allows integration of aggregated‐level data (AD) from different clinical trials in one model to assess population efficacy/safety. However, AD is limited in individual‐leve... |
PMC7064984 | core_pubmed_pmc | Low‐dose empagliflozin as adjunct‐to‐insulin therapy in type 1 diabetes: A valid modelling and simulation analysis to confirm efficacy | Low‐dose empagliflozin as adjunct‐to‐insulin therapy in type 1 diabetes: A valid modelling and simulation analysis to confirm efficacy Abstract Abstract Aim To confirm the observed reduction in HbA1c for the 2.5 mg dose in EASE‐3 by modelling and simulation analyses. Materials and methods Independent of data from EASE‐... |
PMC6058678 | core_pubmed_pmc | Multiseed liposomal drug delivery system using micelle gradient as driving force to improve amphiphilic drug retention and its anti-tumor efficacy | Multiseed liposomal drug delivery system using micelle gradient as driving force to improve amphiphilic drug retention and its anti-tumor efficacy Abstract Abstract To improve drug retention in carriers for amphiphilic asulacrine (ASL), a novel active loading method using micelle gradient was developed to fabricate the... |
PMC9071095 | core_pubmed_pmc | Pharmacokinetic-Pharmacodynamic Model of Vedolizumab for Targeting Endoscopic Remission in Patients With Crohn Disease: Posthoc Analysis of the LOVE-CD Study | Pharmacokinetic-Pharmacodynamic Model of Vedolizumab for Targeting Endoscopic Remission in Patients With Crohn Disease: Posthoc Analysis of the LOVE-CD Study Abstract Abstract Background Higher serum concentrations of vedolizumab have been associated with improved outcomes in inflammatory bowel disease. It is unclear h... |
PMC11111609 | core_pubmed_pmc | Population Pharmacokinetics of the Anti-Interferon-Gamma Monoclonal Antibody Emapalumab: An Updated Analysis | Population Pharmacokinetics of the Anti-Interferon-Gamma Monoclonal Antibody Emapalumab: An Updated Analysis Abstract Introduction Emapalumab is a fully human monoclonal antibody that targets free and receptor-bound interferon-gamma (IFNγ), neutralizing its biological activity. IFNγ levels differ by orders of magnitude... |
PMC11377050 | core_pubmed_pmc | Comparison of intravenous versus perineural dexamethasone as a local anaesthetic adjunct for peripheral nerve blocks in the lower limb | Comparison of intravenous versus perineural dexamethasone as a local anaesthetic adjunct for peripheral nerve blocks in the lower limb Abstract BACKGROUND As a local anaesthetic adjunct, the systemic absorption of perineural dexamethasone in the lower limb could be restricted because of decreased vascularity when compa... |
PMC12944594 | core_pubmed_pmc | Development and Validation of a UPLC-MS/MS Method for the Quantification of Amantadine in Rat Plasma: Application to a Pharmacokinetic Study Under High-Altitude Hypoxia and Mechanistic Insights | Development and Validation of a UPLC-MS/MS Method for the Quantification of Amantadine in Rat Plasma: Application to a Pharmacokinetic Study Under High-Altitude Hypoxia and Mechanistic Insights Abstract Background/Objectives : This study aimed to develop an ultra-performance liquid chromatography–tandem mass spectromet... |
PMC3558805 | core_pubmed_pmc | First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials | First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials Abstract Aims To assess the safety and pharmacokinetics of a new synthetic ozonide antimalarial, OZ439, in a first-in-man, double-blind study in healthy volunteers. Meth... |
PMC8326712 | core_pubmed_pmc | Adaptive study design to assess effect of TRPV4 inhibition in patients with chronic cough | Adaptive study design to assess effect of TRPV4 inhibition in patients with chronic cough Abstract Abstract Objective Airway sensory nerves involved in the cough reflex are activated by adenosine triphosphate (ATP) agonism of P2X purinoceptor 3 (P2X3) receptors. Transient receptor potential vanilloid 4 (TRPV4) channel ... |
PMC12283818 | core_pubmed_pmc | Melatonin for prevention of delirium in patients receiving mechanical ventilation in the intensive care unit: a multiarm multistage adaptive randomized controlled clinical trial (DEMEL) | Melatonin for prevention of delirium in patients receiving mechanical ventilation in the intensive care unit: a multiarm multistage adaptive randomized controlled clinical trial (DEMEL) Abstract Abstract Purpose To determine the dose of melatonin with an optimal pharmacokinetic profile and to test whether this dose red... |
PMC12462634 | core_pubmed_pmc | DrugCombo: an informatics bridge for anticancer drug combination Phase I trial design | DrugCombo: an informatics bridge for anticancer drug combination Phase I trial design Abstract Abstract The promise of combinational drug therapies for cancer is hindered by the high failure rate of Phase I trials, perhaps attributable to the inavailability of an integrated source of toxicity data for cancer drugs to a... |
PMC7533387 | core_pubmed_pmc | Pharmacokinetics of thalidomide in dogs: can feeding affect it? A preliminary study | Pharmacokinetics of thalidomide in dogs: can feeding affect it? A preliminary study Abstract Abstract Background Tumor-associated neoangiogenesis is a crucial target for antitumor therapies. Thalidomide (TAL) is a promising anti-neoangiogenetic drug that has recently been used in the treatment of several malignancies i... |
PMC10043195 | core_pubmed_pmc | PBPK-based dose finding for sildenafil in pregnant women for antenatal treatment of congenital diaphragmatic hernia | PBPK-based dose finding for sildenafil in pregnant women for antenatal treatment of congenital diaphragmatic hernia Abstract Abstract Sildenafil is a potent vasodilator and phosphodiesterase type five inhibitor, commercially known as Revatio ® and approved for the treatment of pulmonary arterial hypertension. Maternal ... |
PMC8149166 | core_pubmed_pmc | An open-label randomized controlled trial of the effect of lopinavir/ritonavir, lopinavir/ritonavir plus IFN-β-1a and hydroxychloroquine in hospitalized patients with COVID-19 | An open-label randomized controlled trial of the effect of lopinavir/ritonavir, lopinavir/ritonavir plus IFN-β-1a and hydroxychloroquine in hospitalized patients with COVID-19 Abstract Objectives We evaluated the clinical, virological and safety outcomes of lopinavir/ritonavir, lopinavir/ritonavir–interferon (IFN)-β-1a... |
PMC10180080 | core_pubmed_pmc | A Remarkable Difference in Pharmacokinetics of Fluorinated Versus Iodinated Photosensitizers Derived from Chlorophyll-a and a Direct Correlation between the Tumor Uptake and Anti-Cancer Activity | A Remarkable Difference in Pharmacokinetics of Fluorinated Versus Iodinated Photosensitizers Derived from Chlorophyll-a and a Direct Correlation between the Tumor Uptake and Anti-Cancer Activity Abstract To investigate and compare the pharmacokinetic profile and anti-cancer activity of fluorinated and iodinated photose... |
PMC11983324 | core_pubmed_pmc | Exploratory Study of Sex Differences in P‐Glycoprotein Function at the Blood–Brain Barrier | Exploratory Study of Sex Differences in P‐Glycoprotein Function at the Blood–Brain Barrier Abstract ABSTRACT Permeability‐glycoprotein (P‐gp), a crucial efflux pump transporter encoded by the ABCB1 gene, plays a pivotal role in drug disposition at the blood–brain barrier (BBB) and is involved in the pharmacokinetics of... |
PMC6363067 | core_pubmed_pmc | Open Source Pharmacokinetic/Pharmacodynamic Framework: Tutorial on the BioGears Engine | Open Source Pharmacokinetic/Pharmacodynamic Framework: Tutorial on the BioGears Engine Abstract Abstract BioGears is an open‐source, lumped parameter, full‐body human physiology engine. Its purpose is to provide realistic and comprehensive simulations for medical training, research, and education. BioGears incorporates... |
PMC3035038 | core_pubmed_pmc | A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and In Vivo Antitumor Efficacy and Safety | A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and In Vivo Antitumor Efficacy and Safety Abstract Abstract The purpose of this study was to prepare a novel paclitaxel (PTX) microemulsion containing a reduced amount of Cremophor EL (CrEL) which had simila... |
PMC9083543 | core_pubmed_pmc | Minimal Physiologically-Based Pharmacokinetic (mPBPK) Metamodeling of Target Engagement in Skin Informs Anti-IL17A Drug Development in Psoriasis | Minimal Physiologically-Based Pharmacokinetic (mPBPK) Metamodeling of Target Engagement in Skin Informs Anti-IL17A Drug Development in Psoriasis Abstract Abstract The pharmacologic effect(s) of biotherapeutics directed against soluble targets are driven by the magnitude and duration of free target suppression at the ti... |
PMC4098115 | core_pubmed_pmc | In Vivo Imaging of Multidrug Resistance Using a Third Generation MDR1 Inhibitor | In Vivo Imaging of Multidrug Resistance Using a Third Generation MDR1 Inhibitor Abstract Abstract Cellular up-regulation of multidrug resistance protein 1 (MDR1) is a common cause for resistance to chemotherapy; development of third generation MDR1 inhibitors—several of which contain a common 6,7-dimethoxy-2-phenethyl-... |
PMC12051621 | core_pubmed_pmc | A pharmacokinetic and safety study of oral arsenic trioxide in patients with acute promyelocytic leukemia | A pharmacokinetic and safety study of oral arsenic trioxide in patients with acute promyelocytic leukemia Abstract Key Points • In this crossover PK study, SY-2101 in the fasted state demonstrated comparable systemic exposure to ATO IV. • The similar PK between SY-2101 and ATO IV supports the likelihood of clinical equ... |
PMC6395911 | core_pubmed_pmc | Bone and Joint Tissue Penetration of the Staphylococcus -Selective Antibiotic Afabicin in Patients Undergoing Elective Hip Replacement Surgery | Bone and Joint Tissue Penetration of the Staphylococcus -Selective Antibiotic Afabicin in Patients Undergoing Elective Hip Replacement Surgery Abstract Afabicin (formerly Debio 1450, AFN-1720) is a prodrug of afabicin desphosphono (Debio 1452, AFN-1252), a novel antibiotic in development which targets the staphylococca... |
PMC9311539 | core_pubmed_pmc | Antibacterial Activity against Clinical Isolates and In Vivo Efficacy of Coralmycins | Antibacterial Activity against Clinical Isolates and In Vivo Efficacy of Coralmycins Abstract Abstract Coralmycins, such as coralmycin A and DH-coralmycin A, have novel molecular skeletons and have been reported to exhibit potent antibacterial activity against standard Gram-positive bacterial strains. Here, the in vitr... |
PMC10045098 | core_pubmed_pmc | Exploring the Long-Term Tissue Accumulation and Excretion of 3 nm Cerium Oxide Nanoparticles after Single Dose Administration | Exploring the Long-Term Tissue Accumulation and Excretion of 3 nm Cerium Oxide Nanoparticles after Single Dose Administration Abstract Nanoparticle (NP) pharmacokinetics significantly differ from traditional small molecule principles. From this emerges the need to create new tools and concepts to harness their full pot... |
PMC4271452 | core_pubmed_pmc | Determining the mechanisms underlying augmented renal drug clearance in the critically ill: use of exogenous marker compounds | Determining the mechanisms underlying augmented renal drug clearance in the critically ill: use of exogenous marker compounds Abstract Introduction The aim of this study was to explore changes in glomerular filtration (GFR) and renal tubular function in critically ill patients at risk of augmented renal clearance (ARC)... |
PMC5750663 | core_pubmed_pmc | Application of Pharmacokinetics Modelling to Predict Human Exposure of a Cationic Liposomal Subunit Antigen Vaccine System | Application of Pharmacokinetics Modelling to Predict Human Exposure of a Cationic Liposomal Subunit Antigen Vaccine System Abstract Abstract The pharmacokinetics of a liposomal subunit antigen vaccine system composed of the cationic lipid dimethyldioctadecylammonium bromide (DDA) and the immunostimulatory agent trehalo... |
PMC4992793 | core_pubmed_pmc | Unraveling the Effect of Immunogenicity on the PK/PD, Efficacy, and Safety of Therapeutic Proteins | Unraveling the Effect of Immunogenicity on the PK/PD, Efficacy, and Safety of Therapeutic Proteins Abstract Biologics have emerged as a powerful and diverse class of molecular and cell-based therapies that are capable of replacing enzymes, editing genomes, targeting tumors, and more. As this complex array of tools aris... |
PMC9372427 | core_pubmed_pmc | Tutorial: Statistical analysis and reporting of clinical pharmacokinetic studies | Tutorial: Statistical analysis and reporting of clinical pharmacokinetic studies Abstract Abstract Pharmacokinetics is the cornerstone of understanding drug absorption, distribution, metabolism, and elimination. It is also the key to describing variability in drug response caused by drug‐drug interactions (DDIs), pharm... |
PMC8694146 | core_pubmed_pmc | Population Pharmacokinetics and Dosing Optimization of Piperacillin-Tazobactam in Critically Ill Patients on Extracorporeal Membrane Oxygenation and the Influence of Concomitant Renal Replacement Therapy | Population Pharmacokinetics and Dosing Optimization of Piperacillin-Tazobactam in Critically Ill Patients on Extracorporeal Membrane Oxygenation and the Influence of Concomitant Renal Replacement Therapy Abstract ABSTRACT Critical illness and extracorporeal circulation, such as extracorporeal membrane oxygenation (ECMO... |
PMC7608663 | core_pubmed_pmc | Pharmacokinetic–pharmacodynamic modelling of the hypoglycaemic effect of pulsatile administration of human insulin in rats | Pharmacokinetic–pharmacodynamic modelling of the hypoglycaemic effect of pulsatile administration of human insulin in rats Abstract The relationship between the plasma insulin (INS) concentration–time course and plasma glucose concentration–time course during and after pulsatile INS administration to rats was character... |
PMC5055355 | core_pubmed_pmc | Impact of Age and Sex on CD4+ Cell Count Trajectories following Treatment Initiation: An Analysis of the Tanzanian HIV Treatment Database | Impact of Age and Sex on CD4+ Cell Count Trajectories following Treatment Initiation: An Analysis of the Tanzanian HIV Treatment Database Abstract Objective New guidelines recommend that all HIV-infected individuals initiate antiretroviral treatment (ART) immediately following diagnosis. This study describes how immune... |
PMC8809196 | core_pubmed_pmc | Simultaneous pharmacokinetic/pharmacodynamic (PKPD) assessment of ampicillin and gentamicin in the treatment of neonatal sepsis | Simultaneous pharmacokinetic/pharmacodynamic (PKPD) assessment of ampicillin and gentamicin in the treatment of neonatal sepsis Abstract Abstract Objectives This study aimed to simultaneously investigate the pharmacokinetics of ampicillin and gentamicin, currently the WHO standard of care for treating neonatal sepsis. ... |
PMC11382051 | core_pubmed_pmc | Multi-omics reveals protective effects of Ling Gui Zhu Gan Decoction on hyperlipidaemia in hamster | Multi-omics reveals protective effects of Ling Gui Zhu Gan Decoction on hyperlipidaemia in hamster Abstract Abstract Ling Gui Zhu Gan decoction (LGZGD) is a traditional Chinese medicine (TCM) prescription that is widely used in cardiovascular disease clinical prevention and treatment with high efficacy. Recent studies ... |
PMC10955330 | core_pubmed_pmc | Synthesis of salcaprozate sodium and its significance in enhancing pancreatic kininogenase absorption performance | Synthesis of salcaprozate sodium and its significance in enhancing pancreatic kininogenase absorption performance Abstract Abstract We conducted pharmacokinetic research wherein salcaprozate sodium (SNAC) was utilized as a penetration enhancer by incorporating it into pancreatic kininogenase (PK) to improve the bioavai... |
PMC5890687 | core_pubmed_pmc | Visceral leishmaniasis relapse hazard is linked to reduced miltefosine exposure in patients from Eastern Africa: a population pharmacokinetic/pharmacodynamic study | Visceral leishmaniasis relapse hazard is linked to reduced miltefosine exposure in patients from Eastern Africa: a population pharmacokinetic/pharmacodynamic study Abstract Abstract Background Low efficacy of miltefosine in the treatment of visceral leishmaniasis was recently observed in Eastern Africa. Objectives To d... |
PMC11674295 | core_pubmed_pmc | Small Molecule with Big Impact: Metarrestin Targets the Perinucleolar Compartment in Cancer Metastasis | Small Molecule with Big Impact: Metarrestin Targets the Perinucleolar Compartment in Cancer Metastasis Abstract Metarrestin (ML246) is a first-in-class pyrrole–pyrimidine-derived small molecule that selectively targets the perinucleolar compartment (PNC). PNC is a distinct subnuclear structure predominantly found in so... |
PMC6951481 | core_pubmed_pmc | Pharmacokinetics and enterohepatic circulation of jervine, an antitumor steroidal alkaloid from Veratrum nigrum in rats | Pharmacokinetics and enterohepatic circulation of jervine, an antitumor steroidal alkaloid from Veratrum nigrum in rats Abstract Abstract Jervine, a novel steroidal alkaloid from Veratrum nigrum L., exhibits both antitumor effect and potential toxicity. The aim of study was to characterize the pharmacokinetic behaviors... |
PMC11768147 | core_pubmed_pmc | Partial AUCs in Long-Acting Injectables: Rationale, Challenges, Variability, Usefulness, and Clinical Relevance | Partial AUCs in Long-Acting Injectables: Rationale, Challenges, Variability, Usefulness, and Clinical Relevance Abstract Abstract Regulatory authorities typically require bioequivalence to be demonstrated by comparing pharmacokinetic parameters like area under the plasma concentration-time curve (AUC) and maximum plasm... |
PMC12135060 | core_pubmed_pmc | Development of a Physiologically Based Biopharmaceutics Model Report Template: Considerations for Improved Quality in View of Regulatory Submissions | Development of a Physiologically Based Biopharmaceutics Model Report Template: Considerations for Improved Quality in View of Regulatory Submissions Abstract Pharmaceutical innovators and generic companies use Physiologically Based Biopharmaceutics Models (PBBMs) to guide drug product development and potentially waive ... |
PMC12649734 | core_pubmed_pmc | Targeting Oral Pathogens with Salvia officinalis and Nigella sativa Supercritical CO 2 Extracts: A Pharmacodynamic Approach and Three-Dimensional Checkerboard Synergy for Novel Dental Antimicrobials | Targeting Oral Pathogens with Salvia officinalis and Nigella sativa Supercritical CO 2 Extracts: A Pharmacodynamic Approach and Three-Dimensional Checkerboard Synergy for Novel Dental Antimicrobials Abstract Abstract Background : Oral infections such as dental caries and candidiasis are mediated by resilient biofilms, ... |
PMC9249724 | core_pubmed_pmc | Population Pharmacokinetics and Dosing Simulations of Ceftriaxone in Critically Ill Patients Receiving Extracorporeal Membrane Oxygenation (An ASAP ECMO Study) | Population Pharmacokinetics and Dosing Simulations of Ceftriaxone in Critically Ill Patients Receiving Extracorporeal Membrane Oxygenation (An ASAP ECMO Study) Abstract Background Despite the surge in use of extracorporeal membrane oxygenation (ECMO) in the adult intensive care unit, little guidance is available on the... |
PMC10045483 | core_pubmed_pmc | Comparative Pharmacokinetic Study of 5 Active Ingredients after Oral Administration of Zuogui Pill in Osteoporotic Rats with Different Syndrome Types | Comparative Pharmacokinetic Study of 5 Active Ingredients after Oral Administration of Zuogui Pill in Osteoporotic Rats with Different Syndrome Types Abstract Zuogui Pill is a kidney-yin-tonifying formula in traditional Chinese medicine that is widely used to manage osteoporosis with kidney-yin-deficiency in China. Her... |
PMC10635345 | core_pubmed_pmc | Busulfan Interlaboratory Proficiency Testing Program Revealed Worldwide Errors in Drug Quantitation and Dose Recommendations | Busulfan Interlaboratory Proficiency Testing Program Revealed Worldwide Errors in Drug Quantitation and Dose Recommendations Abstract Background: The clinical outcomes of busulfan-based conditioning regimens for hematopoietic cell transplantation (HCT) have been improved by personalizing the doses to target narrow busu... |
PMC7651685 | core_pubmed_pmc | The rate of dasotraline brain entry is slow following intravenous administration | The rate of dasotraline brain entry is slow following intravenous administration Abstract Rationale Drugs that rapidly increase dopamine levels have an increased risk of abuse. Dasotraline (DAS) is a dopamine and norepinephrine reuptake inhibitor characterized by slow oral absorption with low potential for abuse. Howev... |
PMC8817058 | core_pubmed_pmc | In Vitro to In Vivo Extrapolation Linked to Physiologically Based Pharmacokinetic Models for Assessing the Brain Drug Disposition | In Vitro to In Vivo Extrapolation Linked to Physiologically Based Pharmacokinetic Models for Assessing the Brain Drug Disposition Abstract Drug development for the central nervous system (CNS) is a complex endeavour with low success rates, as the structural complexity of the brain and specifically the blood-brain barri... |
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