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PMC9909729 | core_pubmed_pmc | Synthesis and biological evaluation of coumarin-quinone hybrids as multifunctional bioactive agents | Synthesis and biological evaluation of coumarin-quinone hybrids as multifunctional bioactive agents Abstract We report the synthesis, structural characterization and pharmaceutical activity of four coumarin-quinone hybrids. The compounds were significantly active against Staphylococcus aureus , Pseudomonas aeoginosa an... |
PMC2994217 | core_pubmed_pmc | A phase I dose-escalation study to evaluate safety and tolerability of sorafenib combined with sirolimus in patients with advanced solid cancer | A phase I dose-escalation study to evaluate safety and tolerability of sorafenib combined with sirolimus in patients with advanced solid cancer Abstract Abstract Background: The combination of sorafenib (vascular endothelial growth factor receptor 2 inhibitor) and sirolimus (mammalian target of rapamycin inhibitor) mig... |
PMC12904192 | core_pubmed_pmc | In Silico Assessment of Limited Blood Sampling Strategies for Individualised Pharmacokinetic‐guided Dosing of Efanesoctocog Alfa in Haemophilia A Patients | In Silico Assessment of Limited Blood Sampling Strategies for Individualised Pharmacokinetic‐guided Dosing of Efanesoctocog Alfa in Haemophilia A Patients Abstract ABSTRACT Introduction Efanesoctocog alfa is a novel factor VIII (FVIII) concentrate with a unique molecular design that enables Von Willebrand Factor‐indepe... |
PMC10166914 | core_pubmed_pmc | GTN057 , a komaroviquinone derivative, induced myeloma cells' death in vivo and inhibited c‐MET tyrosine kinase | GTN057 , a komaroviquinone derivative, induced myeloma cells' death in vivo and inhibited c‐MET tyrosine kinase Abstract Abstract Objective Despite the development of newly developed drugs, most multiple myeloma (MM) patients with high‐risk cytogenetic abnormalities such as t(4;14) or del17p relapse at anin early stage... |
PMC9958007 | core_pubmed_pmc | Development and validation of a cynomolgus macaque grimace scale for acute pain assessment | Development and validation of a cynomolgus macaque grimace scale for acute pain assessment Abstract Abstract Cynomolgus macaques may undergo surgical procedures for scientific and veterinary purposes. Recognition and assessment of pain using validated tools is a necessary first step for adequately managing pain in thes... |
PMC8972016 | core_pubmed_pmc | Human Milk and Plasma Pharmacokinetics of Single-Dose Rimegepant 75 mg in Healthy Lactating Women | Human Milk and Plasma Pharmacokinetics of Single-Dose Rimegepant 75 mg in Healthy Lactating Women Abstract Abstract Objective: Investigate whether rimegepant—an oral small molecule calcitonin gene-related peptide receptor antagonist for the treatment of migraine—is excreted in human milk after a single 75 mg dose and c... |
PMC7646098 | core_pubmed_pmc | Application of Nanotechnology in Cancer Diagnosis and Therapy - A Mini-Review | Application of Nanotechnology in Cancer Diagnosis and Therapy - A Mini-Review Abstract Cancer is a leading cause of death and poor quality of life globally. Even though several strategies are devised to reduce deaths, reduce chronic pain and improve the quality of life, there remains a shortfall in the adequacies of th... |
PMC11561750 | core_pubmed_pmc | First case report of a vertebral osteomyelitis caused by carbapenem-resistant Enterobacter cloacae treated with imipenem/cilastatin/relebactam prolonged infusion then meropenem/vaborbactam in continuous infusion | First case report of a vertebral osteomyelitis caused by carbapenem-resistant Enterobacter cloacae treated with imipenem/cilastatin/relebactam prolonged infusion then meropenem/vaborbactam in continuous infusion Abstract Abstract Introduction Bone and joint infections (BJIs) caused by multidrug-resistant bacteria are b... |
PMC10714946 | core_pubmed_pmc | Prediction of pediatric dose of tirzepatide from the reference adult dose using physiologically based pharmacokinetic modelling | Prediction of pediatric dose of tirzepatide from the reference adult dose using physiologically based pharmacokinetic modelling Abstract Tirzepatide is an emerging hypoglycemic agent that has been increasing used in adults, yet its pharmacokinetic (PK) behavior and dosing regimen in pediatric population remain unclear.... |
PMC5571291 | core_pubmed_pmc | Comparison of Omadacycline and Tigecycline Pharmacokinetics in the Plasma, Epithelial Lining Fluid, and Alveolar Cells of Healthy Adult Subjects | Comparison of Omadacycline and Tigecycline Pharmacokinetics in the Plasma, Epithelial Lining Fluid, and Alveolar Cells of Healthy Adult Subjects Abstract ABSTRACT The steady-state concentrations of omadacycline and tigecycline in the plasma, epithelial lining fluid (ELF), and alveolar cells (AC) of 58 healthy adult sub... |
PMC6590144 | core_pubmed_pmc | Accelerating Drug Development in Pediatric Oncology With the Clinical Pharmacology Storehouse | Accelerating Drug Development in Pediatric Oncology With the Clinical Pharmacology Storehouse Abstract Abstract Pediatric drug development is a challenging process due to the rarity of the population, the need to meet regulatory requirements across the globe, the associated uncertainty in extrapolating data from adults... |
PMC9863109 | core_pubmed_pmc | Safety and Pharmacokinetics of the Substance of the Anti-Smallpox Drug NIOCH-14 after Oral Administration to Laboratory Animals | Safety and Pharmacokinetics of the Substance of the Anti-Smallpox Drug NIOCH-14 after Oral Administration to Laboratory Animals Abstract Background: Since most of the modern human population has no anti-smallpox immunity, it is extremely important to develop and implement effective drugs for the treatment of smallpox a... |
PMC9280300 | core_pubmed_pmc | Characterization of ADME Gene Variation in Colombian Population by Exome Sequencing | Characterization of ADME Gene Variation in Colombian Population by Exome Sequencing Abstract In genes related to drug pharmacokinetics, molecular variations determine interindividual variability in the therapeutic efficacy and adverse drug reactions. The assessment of single-nucleotide variants (SNVs) is used with grow... |
PMC9755918 | core_pubmed_pmc | Population pharmacokinetic‐pharmacodynamic analyses of amyloid positron emission tomography and plasma biomarkers for lecanemab in subjects with early Alzheimer's disease | Population pharmacokinetic‐pharmacodynamic analyses of amyloid positron emission tomography and plasma biomarkers for lecanemab in subjects with early Alzheimer's disease Abstract Abstract Lecanemab is a humanized immunoglobulin G1 monoclonal antibody that selectively binds to soluble Aβ aggregate species, while demons... |
PMC8775213 | core_pubmed_pmc | Results of a phase 1, randomized, placebo-controlled first-in-human trial of griffithsin formulated in a carrageenan vaginal gel | Results of a phase 1, randomized, placebo-controlled first-in-human trial of griffithsin formulated in a carrageenan vaginal gel Abstract HIV pre-exposure prophylaxis (PrEP) is dominated by clinical therapeutic antiretroviral (ARV) drugs. Griffithsin (GRFT) is a non-ARV lectin with potent anti-HIV activity. GRFT’s prec... |
PMC12507754 | core_pubmed_pmc | Efficacy of vedolizumab as maintenance therapy in a patient with ulcerative colitis on hemodialysis for end-stage renal failure: a case report | Efficacy of vedolizumab as maintenance therapy in a patient with ulcerative colitis on hemodialysis for end-stage renal failure: a case report Abstract Background Hemodialysis is an important life-sustaining treatment for patients with end-stage renal failure (ESRF), but its ultrafiltration process may induce hypoalbum... |
PMC9589333 | core_pubmed_pmc | Phase I studies of BI 1015550, a preferential phosphodiesterase 4B inhibitor, in healthy males and patients with idiopathic pulmonary fibrosis | Phase I studies of BI 1015550, a preferential phosphodiesterase 4B inhibitor, in healthy males and patients with idiopathic pulmonary fibrosis Abstract Introduction BI 1015550 is a phosphodiesterase 4 (PDE4) inhibitor that has antifibrotic properties. Phase I and Ic studies were conducted to investigate the safety, tol... |
PMC12104055 | core_pubmed_pmc | Development and application of a UHPLC-MS/MS method for the simultaneous determination of firmonertinib and its main metabolite AST-5902 in rat plasma: a study on the in vivo drug interaction between firmonertinib and paxlovid | Development and application of a UHPLC-MS/MS method for the simultaneous determination of firmonertinib and its main metabolite AST-5902 in rat plasma: a study on the in vivo drug interaction between firmonertinib and paxlovid Abstract Abstract Due to the potential occurrence of drug interactions, the combined applicat... |
PMC11218538 | core_pubmed_pmc | In vitro interaction of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen in the asexual blood stage of Plasmodium falciparum 3D7 | In vitro interaction of naphthoquine with ivermectin, atovaquone, curcumin, and ketotifen in the asexual blood stage of Plasmodium falciparum 3D7 Abstract ABSTRACT Naphthoquine is a promising candidate for antimalarial combination therapy. Its combination with artemisinin has demonstrated excellent efficacy in clinical... |
PMC7247487 | core_pubmed_pmc | In Silico computational screening of Kabasura Kudineer - Official Siddha Formulation and JACOM against SARS-CoV-2 spike protein | In Silico computational screening of Kabasura Kudineer - Official Siddha Formulation and JACOM against SARS-CoV-2 spike protein Abstract Abstract Background Siddha Medicine is a valuable therapeutic choice which is classically used for treating viral respiratory infections, this principle of medicine is proven to conta... |
PMC8149920 | core_pubmed_pmc | Correlation of exhaled propofol with Narcotrend index and calculated propofol plasma levels in children undergoing surgery under total intravenous anesthesia - an observational study | Correlation of exhaled propofol with Narcotrend index and calculated propofol plasma levels in children undergoing surgery under total intravenous anesthesia - an observational study Abstract Abstract Background Exhaled propofol concentrations correlate with propofol concentrations in adult human blood and the brain ti... |
PMC10166826 | core_pubmed_pmc | Revolutionizing drug development: harnessing the potential of organ-on-chip technology for disease modeling and drug discovery | Revolutionizing drug development: harnessing the potential of organ-on-chip technology for disease modeling and drug discovery Abstract The inefficiency of existing animal models to precisely predict human pharmacological effects is the root reason for drug development failure. Microphysiological system/organ-on-a-chip... |
PMC9147001 | core_pubmed_pmc | Nonclinical Pharmacokinetics and Pharmacodynamics Characterization of Anti-CD79b/CD3 T Cell-Dependent Bispecific Antibody Using a Surrogate Molecule: A Potential Therapeutic Agent for B Cell Malignancies | Nonclinical Pharmacokinetics and Pharmacodynamics Characterization of Anti-CD79b/CD3 T Cell-Dependent Bispecific Antibody Using a Surrogate Molecule: A Potential Therapeutic Agent for B Cell Malignancies Abstract Abstract The T cell-dependent bispecific (TDB) antibody, anti-CD79b/CD3, targets CD79b and CD3 cell-surface... |
PMC11573600 | core_pubmed_pmc | Case study of CD19 CAR T therapy in a subject with immune-mediate necrotizing myopathy treated in the RESET-Myositis phase I/II trial | Case study of CD19 CAR T therapy in a subject with immune-mediate necrotizing myopathy treated in the RESET-Myositis phase I/II trial Abstract Under compassionate use, chimeric antigen receptor (CAR) T cells have elicited durable remissions in patients with refractory idiopathic inflammatory myopathies (IIMs). Here, we... |
PMC9024361 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution, Metabolism and Excretion of a Novel COX-2 Inhibitor, Vitacoxib, in Rats | Pharmacokinetics, Tissue Distribution, Metabolism and Excretion of a Novel COX-2 Inhibitor, Vitacoxib, in Rats Abstract Abstract The objectives of this study were to elucidate absorption, tissue distribution, excretion, and metabolism of vitacoxib, a novel selective cyclooxygenase-2 inhibitor, in Wistar rats. Vitacoxib... |
PMC9175552 | core_pubmed_pmc | Dose–exposure–IGF-I response of once-weekly somapacitan in adults with GH deficiency | Dose–exposure–IGF-I response of once-weekly somapacitan in adults with GH deficiency Abstract Objective Growth hormone (GH) replacement therapy in patients with adult growth hormone deficiency (AGHD) is individually titrated due to variable dose–responses among patients. The aim of this study was to provide clinical gu... |
PMC10830448 | core_pubmed_pmc | Population pharmacokinetics of lenalidomide in Chinese patients with influence of genetic polymorphisms of ABCB1 | Population pharmacokinetics of lenalidomide in Chinese patients with influence of genetic polymorphisms of ABCB1 Abstract Abstract Affected by differences in the pharmacokinetics (PK) of lenalidomide, the toxicity of lenalidomide varies among different patients, with serious toxicity leading to dose reduction or discon... |
PMC6624387 | core_pubmed_pmc | Population pharmacokinetics of immediate‐ and prolonged‐release tacrolimus formulations in liver, kidney and heart transplant recipients | Population pharmacokinetics of immediate‐ and prolonged‐release tacrolimus formulations in liver, kidney and heart transplant recipients Abstract Abstract Aims Develop a population pharmacokinetics model of tacrolimus in organ transplant recipients receiving twice‐daily, immediate‐release (IR‐T; Prograf) and/or once‐da... |
PMC9488889 | core_pubmed_pmc | Insight into mode-of-action and structural determinants of the compstatin family of clinical complement inhibitors | Insight into mode-of-action and structural determinants of the compstatin family of clinical complement inhibitors Abstract Abstract With the addition of the compstatin-based complement C3 inhibitor pegcetacoplan, another class of complement targeted therapeutics have recently been approved. Moreover, compstatin deriva... |
PMC4282489 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of 6-month daily dosing of an oral formulation of cyclosporine (ATOPICA for cats®) in cats | Safety, tolerability, and pharmacokinetics of 6-month daily dosing of an oral formulation of cyclosporine (ATOPICA for cats®) in cats Abstract Cyclosporine was proven efficacious in the treatment of feline hypersensitivity dermatitis. This target animal study was conducted to evaluate the safety, tolerability, and phar... |
PMC6061756 | core_pubmed_pmc | Pharmacodynamic considerations of collateral sensitivity in design of antibiotic treatment regimen | Pharmacodynamic considerations of collateral sensitivity in design of antibiotic treatment regimen Abstract Abstract Introduction Antibiotics have greatly reduced the morbidity and mortality due to infectious diseases. Although antibiotic resistance is not a new problem, its breadth now constitutes a significant threat... |
PMC12180521 | core_pubmed_pmc | Recent advances in nano vehicles encapsulating cinnamic acid and its derivatives as promising anticancer agents | Recent advances in nano vehicles encapsulating cinnamic acid and its derivatives as promising anticancer agents Abstract Although progress in cancer diagnosis and treatment has been substantial over recent decades, several challenges remain unresolved. Among these challenges are drug resistance, the recurrence of metas... |
PMC3660459 | core_pubmed_pmc | Rapid Countermeasure Discovery against Francisella tularensis Based on a Metabolic Network Reconstruction | Rapid Countermeasure Discovery against Francisella tularensis Based on a Metabolic Network Reconstruction Abstract In the future, we may be faced with the need to provide treatment for an emergent biological threat against which existing vaccines and drugs have limited efficacy or availability. To prepare for this even... |
PMC7497079 | core_pubmed_pmc | BAY 81‐8973 prophylaxis and pharmacokinetics in haemophilia A: Interim results from the TAURUS study | BAY 81‐8973 prophylaxis and pharmacokinetics in haemophilia A: Interim results from the TAURUS study Abstract Abstract Objectives To report interim data from TAURUS, a study assessing real‐world prophylactic treatment with unmodified, full‐length recombinant FVIII BAY 81‐8973 (Kovaltry ® ; Bayer) indicated for haemophi... |
PMC10045534 | core_pubmed_pmc | Preparation and Evaluation of 6-Gingerol Derivatives as Novel Antioxidants and Antiplatelet Agents | Preparation and Evaluation of 6-Gingerol Derivatives as Novel Antioxidants and Antiplatelet Agents Abstract Ginger ( Zingiber officinale ) is widely used as a spice and a traditional medicine. Many bioactivities have been reported for its extracts and the isolated compounds, including cardiovascular protective effects.... |
PMC7685322 | core_pubmed_pmc | The Development of a Novel Nanobody Therapeutic for SARS-CoV-2 | The Development of a Novel Nanobody Therapeutic for SARS-CoV-2 Abstract Abstract Combating the COVID-19 pandemic requires potent and low-cost therapeutics. We identified a novel series of single-domain antibodies (i.e., nanobody), Nanosota-1 , from a camelid nanobody phage display library. Structural data showed that N... |
PMC11908343 | core_pubmed_pmc | Local ancestry informed GWAS of warfarin dose requirement in African Americans identifies a novel CYP2C19 splice QTL | Local ancestry informed GWAS of warfarin dose requirement in African Americans identifies a novel CYP2C19 splice QTL Abstract Abstract African Americans (AAs) are underrepresented in pharmacogenomics which has led to a significant gap in knowledge. AAs are admixed and can inherit specific loci from either their African... |
PMC3318205 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Darunavir and Etravirine in HIV-1–Infected, Treatment-Experienced Patients in the Gender, Race, and Clinical Experience (GRACE) Trial | Pharmacokinetics and Pharmacodynamics of Darunavir and Etravirine in HIV-1–Infected, Treatment-Experienced Patients in the Gender, Race, and Clinical Experience (GRACE) Trial Abstract Objectives . Evaluation of pharmacokinetics and pharmacodynamics of darunavir and etravirine among HIV-1–infected, treatment-experienced... |
PMC6765355 | core_pubmed_pmc | Brodifacoum does not modulate human cannabinoid receptor-mediated hyperpolarization of AtT20 cells or inhibition of adenylyl cyclase in HEK 293 cells | Brodifacoum does not modulate human cannabinoid receptor-mediated hyperpolarization of AtT20 cells or inhibition of adenylyl cyclase in HEK 293 cells Abstract Abstract Background Synthetic cannabinoids are a commonly used class of recreational drugs that can have significant adverse effects. There have been sporadic re... |
PMC8110485 | core_pubmed_pmc | Pharmacokinetics of UGN-101, a mitomycin-containing reverse thermal gel instilled via retrograde catheter for the treatment of low-grade upper tract urothelial carcinoma | Pharmacokinetics of UGN-101, a mitomycin-containing reverse thermal gel instilled via retrograde catheter for the treatment of low-grade upper tract urothelial carcinoma Abstract Abstract Purpose To evaluate the pharmacokinetic properties of UGN-101, a mitomycin-containing reverse thermal gel used as primary chemoablat... |
PMC11933221 | core_pubmed_pmc | Dose Optimization of Elranatamab to Mitigate the Risk of Cytokine Release Syndrome in Patients with Multiple Myeloma | Dose Optimization of Elranatamab to Mitigate the Risk of Cytokine Release Syndrome in Patients with Multiple Myeloma Abstract Abstract Background Elranatamab is a BCMA-CD3 bispecific antibody approved for the treatment of relapsed or refractory multiple myeloma. Cytokine release syndrome is one of the most common adver... |
PMC12745177 | core_pubmed_pmc | Nanomedicine Strategies Against Biofilm‐Associated Infections: Advances, Challenges, and Translational Barriers | Nanomedicine Strategies Against Biofilm‐Associated Infections: Advances, Challenges, and Translational Barriers Abstract ABSTRACT Antimicrobial resistance continues to rise globally, with biofilm‐associated infections intensifying the clinical burden through persistent tolerance to antibiotics and evasion of immune res... |
PMC3649748 | core_pubmed_pmc | New Oral Anticoagulants in the Treatment of Pulmonary Embolism: Efficacy, Bleeding Risk, and Monitoring | New Oral Anticoagulants in the Treatment of Pulmonary Embolism: Efficacy, Bleeding Risk, and Monitoring Abstract Abstract Anticoagulation therapy is mandatory in patients with pulmonary embolism to prevent significant morbidity and mortality. The mainstay of therapy has been vitamin-K antagonist therapy bridged with pa... |
PMC5004175 | core_pubmed_pmc | Abcb1 in Pigs: Molecular cloning, tissues distribution, functional analysis, and its effect on pharmacokinetics of enrofloxacin | Abcb1 in Pigs: Molecular cloning, tissues distribution, functional analysis, and its effect on pharmacokinetics of enrofloxacin Abstract Abstract P-glycoprotein (P-gp) is one of the best-known ATP-dependent efflux transporters, contributing to differences in pharmacokinetics and drug-drug interactions. Until now, studi... |
PMC4699331 | core_pubmed_pmc | Can physicochemical properties of antimicrobials be used to predict their pharmacokinetics during extracorporeal membrane oxygenation? Illustrative data from ovine models | Can physicochemical properties of antimicrobials be used to predict their pharmacokinetics during extracorporeal membrane oxygenation? Illustrative data from ovine models Abstract Abstract Introduction Ex vivo experiments in extracorporeal membrane oxygenation (ECMO) circuits have identified octanol-water partition coe... |
PMC8779022 | core_pubmed_pmc | Phase Ib Study of the Histone Deacetylase 6 Inhibitor Citarinostat in Combination With Paclitaxel in Patients With Advanced Solid Tumors | Phase Ib Study of the Histone Deacetylase 6 Inhibitor Citarinostat in Combination With Paclitaxel in Patients With Advanced Solid Tumors Abstract Background Citarinostat (CC-96241; previously ACY-241), an oral inhibitor of histone deacetylases (HDACs) with selectivity for HDAC6, has demonstrated synergistic anticancer ... |
PMC8034232 | core_pubmed_pmc | Urine Colorimetry for Levofloxacin Pharmacokinetics and Personalized Dosing in People with Drug-resistant Tuberculosis | Urine Colorimetry for Levofloxacin Pharmacokinetics and Personalized Dosing in People with Drug-resistant Tuberculosis Abstract Background: Levofloxacin is a preferred drug for multidrug-resistant (MDR)-tuberculosis (TB) with bactericidal activity that correlates with the pharmacokinetic exposures of serum peak concent... |
PMC7923293 | core_pubmed_pmc | On Absorption Modeling and Food Effect Prediction of Rivaroxaban, a BCS II Drug Orally Administered as an Immediate-Release Tablet | On Absorption Modeling and Food Effect Prediction of Rivaroxaban, a BCS II Drug Orally Administered as an Immediate-Release Tablet Abstract The present work evaluates the food effect on the absorption of rivaroxaban (Riva), a BCS II drug, from the orally administered commercial immediate-release tablet (Xarelto IR) usi... |
PMC11941477 | core_pubmed_pmc | Structure-Based Identification of SARS-CoV-2 nsp10-16 Methyltransferase Inhibitors Using Molecular Dynamics Insights | Structure-Based Identification of SARS-CoV-2 nsp10-16 Methyltransferase Inhibitors Using Molecular Dynamics Insights Abstract Abstract SARS-CoV-2 evades immune detection via nsp10-16 methyltransferase-mediated 2′-O-methylation of viral mRNA, making it a key antiviral target. Our study employed structure-based drug disc... |
PMC6167998 | core_pubmed_pmc | Self-nanoemulsifying drug delivery system of bruceine D: a new approach for anti-ulcerative colitis | Self-nanoemulsifying drug delivery system of bruceine D: a new approach for anti-ulcerative colitis Abstract Abstract Background Bruceine D (BD) is a major bioactive component isolated from the traditional Chinese medicinal plant Brucea javanica which has been widely utilized to treat dysentery (also known as ulcerativ... |
PMC11093668 | core_pubmed_pmc | Pharmacokinetics and Safety of Twice-daily Ritonavir-boosted Atazanavir With Rifampicin | Pharmacokinetics and Safety of Twice-daily Ritonavir-boosted Atazanavir With Rifampicin Abstract Abstract Background Critical drug-drug interactions (DDI) and hepatotoxicity complicate concurrent use of rifampicin and protease inhibitors. We investigated whether dose escalation of atazanavir/ritonavir could safely over... |
PMC5093184 | core_pubmed_pmc | A class of non-linear exposure-response models suitable for health impact assessment applicable to large cohort studies of ambient air pollution | A class of non-linear exposure-response models suitable for health impact assessment applicable to large cohort studies of ambient air pollution Abstract The effectiveness of regulatory actions designed to improve air quality is often assessed by predicting changes in public health resulting from their implementation. ... |
PMC4265842 | core_pubmed_pmc | Phase I study of BAY 94-9027, a PEGylated B-domain-deleted recombinant factor VIII with an extended half-life, in subjects with hemophilia A | Phase I study of BAY 94-9027, a PEGylated B-domain-deleted recombinant factor VIII with an extended half-life, in subjects with hemophilia A Abstract Abstract Background BAY 94-9027 is a B-domain-deleted recombinant factor VIII (rFVIII) with site-specific attachment of poly(ethylene glycol) that has shown an extended h... |
PMC7793942 | core_pubmed_pmc | Simulation Training to Improve Informed Consent and Pharmacokinetic/Pharmacodynamic Sampling in Pediatric Trials | Simulation Training to Improve Informed Consent and Pharmacokinetic/Pharmacodynamic Sampling in Pediatric Trials Abstract Abstract Background : Pediatric trials to add missing data for evidence-based pharmacotherapy are still scarce. A tailored training concept appears to be a promising tool to cope with critical and c... |
PMC12547526 | core_pubmed_pmc | Long-Circulating Liposomes Codelivering Amphotericin B and Retinoic Acid for Cutaneous Leishmaniasis Treatment | Long-Circulating Liposomes Codelivering Amphotericin B and Retinoic Acid for Cutaneous Leishmaniasis Treatment Abstract Leishmaniasis is a neglected tropical disease that mainly affects socially vulnerable populations. It is caused by various Leishmania species, and manifests primarily as cutaneous (CL) or visceral lei... |
PMC9652441 | core_pubmed_pmc | Population pharmacokinetics of everolimus in adult liver transplant patients: Comparison to tacrolimus disposition and extrapolation to pediatrics | Population pharmacokinetics of everolimus in adult liver transplant patients: Comparison to tacrolimus disposition and extrapolation to pediatrics Abstract Abstract Everolimus has recently been used to prevent graft rejection in liver transplantation and reduces the incidence of kidney dysfunction caused by calcineurin... |
PMC12645147 | core_pubmed_pmc | Restoring Gut-brain Function by Medicinal Herbs Offering Neuroprotection through Suppressing Inflammatory Pathways: A Systematic Review | Restoring Gut-brain Function by Medicinal Herbs Offering Neuroprotection through Suppressing Inflammatory Pathways: A Systematic Review Abstract Abstract Introduction Neurodegenerative diseases (NDDs) refer to a progressive degeneration of the nervous system and are on the rise. Researchers are trying to reveal the cru... |
PMC8790013 | core_pubmed_pmc | Restoration of Nusinersen Levels Following Treatment Interruption in People With Spinal Muscular Atrophy: Simulations Based on a Population Pharmacokinetic Model | Restoration of Nusinersen Levels Following Treatment Interruption in People With Spinal Muscular Atrophy: Simulations Based on a Population Pharmacokinetic Model Abstract Abstract Background Nusinersen is approved for the treatment of spinal muscular atrophy. The most common approved dosing regimen is four intrathecal ... |
PMC3701691 | core_pubmed_pmc | Predictors of Hepatitis B Cure Using Gene Therapy to Deliver DNA Cleavage Enzymes: A Mathematical Modeling Approach | Predictors of Hepatitis B Cure Using Gene Therapy to Deliver DNA Cleavage Enzymes: A Mathematical Modeling Approach Abstract Abstract Most chronic viral infections are managed with small molecule therapies that inhibit replication but are not curative because non-replicating viral forms can persist despite decades of s... |
PMC12845072 | core_pubmed_pmc | Do Cenobamate Pharmacokinetics Change with Co-Administered Antiseizure Medications? An Exploratory Analysis of Responder Patients with Focal Drug-Resistant Epilepsy | Do Cenobamate Pharmacokinetics Change with Co-Administered Antiseizure Medications? An Exploratory Analysis of Responder Patients with Focal Drug-Resistant Epilepsy Abstract Abstract Background: Cenobamate (CNB) is an anti-seizure medication (ASM) approved for the treatment of drug-resistant focal epilepsy in adults. N... |
PMC7783227 | core_pubmed_pmc | Developed simvastatin chitosan nanoparticles co-crosslinked with tripolyphosphate and chondroitin sulfate for ASGPR-mediated targeted HCC delivery with enhanced oral bioavailability | Developed simvastatin chitosan nanoparticles co-crosslinked with tripolyphosphate and chondroitin sulfate for ASGPR-mediated targeted HCC delivery with enhanced oral bioavailability Abstract Abstract Simvastatin (SV) repurposing has emerged as an alternative approach for the treatment of cancer. In this study, SV chito... |
PMC11335370 | core_pubmed_pmc | Enabling population protein dynamics through Bayesian modeling | Enabling population protein dynamics through Bayesian modeling Abstract Abstract Motivation The knowledge of protein dynamics, or turnover, in patients provides invaluable information related to certain diseases, drug efficacy, or biological processes. A great corpus of experimental and computational methods has been d... |
PMC10684418 | core_pubmed_pmc | Population Pharmacokinetics of Total and Unbound Isavuconazole in Critically Ill Patients: Implications for Adaptive Dosing Strategies | Population Pharmacokinetics of Total and Unbound Isavuconazole in Critically Ill Patients: Implications for Adaptive Dosing Strategies Abstract Background and Objectives Isavuconazole is a broad-spectrum antifungal agent for the management of invasive fungal disease. Optimised drug exposure is critical for patient outc... |
PMC12275915 | core_pubmed_pmc | High-Fat Meal Increase Blonanserin Bioavailability 5-Fold in Chinese Healthy Subjects | High-Fat Meal Increase Blonanserin Bioavailability 5-Fold in Chinese Healthy Subjects Abstract Purpose Although blonanserin is widely used in clinical practice, existing studies have shown significant variations in the magnitude of food effects on its pharmacokinetics. This study was conducted to evaluate the impact of... |
PMC11176610 | core_pubmed_pmc | Predicted efficacy and tolerance of different dosage regimens of benzylpenicillin in horses based on a pharmacokinetic study with three IM formulations and one IV formulation | Predicted efficacy and tolerance of different dosage regimens of benzylpenicillin in horses based on a pharmacokinetic study with three IM formulations and one IV formulation Abstract Introduction Benzylpenicillin (BP) is a first-line antibiotic in horses but there are discrepancies between manufacturers and literature... |
PMC6400024 | core_pubmed_pmc | Effect of Multidrug-Resistant 1 (MDR1) and CYP3A4*1B Polymorphisms on Cyclosporine-Based Immunosuppressive Therapy in Renal Transplant Patients | Effect of Multidrug-Resistant 1 (MDR1) and CYP3A4*1B Polymorphisms on Cyclosporine-Based Immunosuppressive Therapy in Renal Transplant Patients Abstract Background Immunosuppressive drugs such as cyclosporine A (CsA) are characterized by a narrow therapeutic range and high interindividual pharmacokinetic variations. Th... |
PMC11916956 | core_pubmed_pmc | Incidence and predictors of vancomycin nephrotoxicity and mortality in patients with chronic liver disease: a two-center retrospective cohort study | Incidence and predictors of vancomycin nephrotoxicity and mortality in patients with chronic liver disease: a two-center retrospective cohort study Abstract Abstract Background Patients with liver disease express multiple pathophysiological variations that alter the pharmacokinetics of numerous drugs. At this time, the... |
PMC4014769 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Modeling of Interstrain Variability in Trichloroethylene Metabolism in the Mouse | Physiologically Based Pharmacokinetic (PBPK) Modeling of Interstrain Variability in Trichloroethylene Metabolism in the Mouse Abstract Background: Quantitative estimation of toxicokinetic variability in the human population is a persistent challenge in risk assessment of environmental chemicals. Traditionally, interind... |
PMC8467379 | core_pubmed_pmc | Effects of SLCO1B1 and SLCO1B3 Genetic Polymorphisms on Valsartan Pharmacokinetics in Healthy Korean Volunteers | Effects of SLCO1B1 and SLCO1B3 Genetic Polymorphisms on Valsartan Pharmacokinetics in Healthy Korean Volunteers Abstract Purpose: This study aimed to examine OATP1B1 ( SLCO1B1 ) and OATP1B3 ( SLCO1B3 ) on the pharmacokinetics of valsartan. Twenty-five subjects were genotyped for 16 single-nucleotide polymorphisms of th... |
PMC9428562 | core_pubmed_pmc | Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation | Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation Abstract Abstract Shaogan Fuzi Decoction (SGFD), one of the classical prescriptions of Chinese Medicine, has a long history in the treatment of rheumatoid arthritis (RA), but definitive studies on its... |
PMC7554781 | core_pubmed_pmc | Small Molecules and Peptides Targeting Glial Cell Line-Derived Neurotrophic Factor Receptors for the Treatment of Neurodegeneration | Small Molecules and Peptides Targeting Glial Cell Line-Derived Neurotrophic Factor Receptors for the Treatment of Neurodegeneration Abstract Abstract Glial cell line-derived neurotrophic factor (GDNF) family ligands (GFLs) are able to promote the survival of multiple neuronal populations in the body and, therefore, hol... |
PMC12829376 | core_pubmed_pmc | Haemoglobin vesicles as artificial red blood cells developed for use as a transfusion alternative: an open-label, single-centre phase Ib study protocol in Japan | Haemoglobin vesicles as artificial red blood cells developed for use as a transfusion alternative: an open-label, single-centre phase Ib study protocol in Japan Abstract Abstract Introduction Haemoglobin vesicles (HbVs) (product name, NMU-HbVs [Nara Medical University-Haemoglobin Vesicles]), which contain purified huma... |
PMC5587689 | core_pubmed_pmc | Revisiting myocardial necrosis biomarkers: assessment of the effect of conditioning therapies on infarct size by kinetic modelling | Revisiting myocardial necrosis biomarkers: assessment of the effect of conditioning therapies on infarct size by kinetic modelling Abstract Infarct size is a major predictor of subsequent cardiovascular events following ST-segment elevation myocardial infarction (STEMI) and is frequently used in clinical trials focused... |
PMC11192378 | core_pubmed_pmc | Unrevealing the multitargeted potency of 3-1-BCMIYPPA against lung cancer structural maintenance and suppression proteins through pharmacokinetics, QM-DFT, and multiscale MD simulation studies | Unrevealing the multitargeted potency of 3-1-BCMIYPPA against lung cancer structural maintenance and suppression proteins through pharmacokinetics, QM-DFT, and multiscale MD simulation studies Abstract Lung cancer, a relentless and challenging disease, demands unwavering attention in drug design research. Single-target... |
PMC12460204 | core_pubmed_pmc | Demonstrating Bioequivalence for a Lumacaftor Monosubstance Formulation Versus Orkambi ® (Lumacaftor/Ivacaftor) in Healthy Subjects | Demonstrating Bioequivalence for a Lumacaftor Monosubstance Formulation Versus Orkambi ® (Lumacaftor/Ivacaftor) in Healthy Subjects Abstract Abstract Background and Objective Lumacaftor is an active ingredient in the US Food and Drug Administration-approved combination medication Orkambi ® , which is used for treating ... |
PMC5791972 | core_pubmed_pmc | Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice | Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice Abstract Background Forty million adults in the US suffer from anxiety disorders, making these the most common forms of mental illness. Transient receptor potential channel canonical subfamily (TRPC) mem... |
PMC3298494 | core_pubmed_pmc | Oral contraceptives modify DNA methylation and monocyte-derived macrophage function | Oral contraceptives modify DNA methylation and monocyte-derived macrophage function Abstract Background Fertile women may be encouraged to use contraception during clinical trials to avoid potential drug effects on fetuses. However, hormonal contraception interferes with pharmacokinetics and pharmacodynamics and modifi... |
PMC3853146 | core_pubmed_pmc | Is switching from brand name to generic formulations of phenobarbital associated with loss of antiepileptic efficacy?: a pharmacokinetic study with two oral formulations (Luminal® vet, Phenoleptil®) in dogs | Is switching from brand name to generic formulations of phenobarbital associated with loss of antiepileptic efficacy?: a pharmacokinetic study with two oral formulations (Luminal® vet, Phenoleptil®) in dogs Abstract Abstract Background In human medicine, adverse outcomes associated with switching between bioequivalent ... |
PMC8614818 | core_pubmed_pmc | Translation of Pharmacodynamic Biomarkers of Antibiotic Efficacy in Specific Populations to Optimize Doses | Translation of Pharmacodynamic Biomarkers of Antibiotic Efficacy in Specific Populations to Optimize Doses Abstract Antibiotic efficacy determination in clinical trials often relies on non-inferiority designs because they afford smaller study sample sizes. These efficacy studies tend to exclude patients within specific... |
PMC3896858 | core_pubmed_pmc | Small and Innovative Molecules as New Strategy to Revert MDR | Small and Innovative Molecules as New Strategy to Revert MDR Abstract Abstract Multidrug resistance (MDR) is a complex phenomenon principally due to the overexpression of some transmembrane proteins belonging to the ATP binding cassette (ABC) transporter family. Among these transporters, P-glycoprotein (P-gp) is mostly... |
PMC12645946 | core_pubmed_pmc | A Dual-Targeted Therapy with Fucoidan-Functionalized Thrombolytic Discoidal Microparticles for Pulmonary Thromboembolism | A Dual-Targeted Therapy with Fucoidan-Functionalized Thrombolytic Discoidal Microparticles for Pulmonary Thromboembolism Abstract Abstract Background Pulmonary thromboembolism, a pathological condition characterized by the occlusion of pulmonary vasculature by free-circulating thrombus, constitutes the third leading ca... |
PMC6990966 | core_pubmed_pmc | Treatment of Porphyromonas gulae infection and downstream pathology in the aged dog by lysine‐gingipain inhibitor COR388 | Treatment of Porphyromonas gulae infection and downstream pathology in the aged dog by lysine‐gingipain inhibitor COR388 Abstract Abstract COR388, a small‐molecule lysine‐gingipain inhibitor, is currently being investigated in a Phase 2/3 clinical trial for Alzheimer's disease (AD) with exploratory endpoints in periodo... |
PMC8518624 | core_pubmed_pmc | Pharmacokinetics of Asfotase Alfa in Adult Patients With Pediatric‐Onset Hypophosphatasia | Pharmacokinetics of Asfotase Alfa in Adult Patients With Pediatric‐Onset Hypophosphatasia Abstract Abstract Hypophosphatasia is a rare metabolic disease resulting from variant(s) in the gene‐encoding tissue‐nonspecific isozyme of alkaline phosphatase. In this 13‐week, phase 2a, multicenter, randomized, open‐label, dose... |
PMC9716452 | core_pubmed_pmc | Vancomycin area under the curve/minimum inhibitory concentration and trough level concordance–evaluation on an urban health unit | Vancomycin area under the curve/minimum inhibitory concentration and trough level concordance–evaluation on an urban health unit Abstract Abstract Background: A vancomycin AUC/MIC (area under the curve/minimum inhibitory concentration) of 400–600 mg•h/L is associated with improved clinical outcomes for the treatment of... |
PMC4961079 | core_pubmed_pmc | Population Exposure‐Response Modeling of Naloxegol in Patients With Noncancer‐Related Pain and Opioid‐Induced Constipation | Population Exposure‐Response Modeling of Naloxegol in Patients With Noncancer‐Related Pain and Opioid‐Induced Constipation Abstract Abstract Naloxegol is a polyethylene glycol derivative of naloxone approved in the US as a once‐daily oral treatment for opioid‐induced constipation (OIC) in adults with chronic noncancer ... |
PMC3390066 | core_pubmed_pmc | Use of antiarrhythmic drugs in elderly patients | Use of antiarrhythmic drugs in elderly patients Abstract Abstract Human aging is a global issue with important implications for current and future incidence and prevalence of health conditions and disability. Cardiac arrhythmias, including atrial fibrillation, sudden cardiac death, and bradycardia requiring pacemaker p... |
PMC7212460 | core_pubmed_pmc | Natural Product Ginsenoside 20(S)-25-Methoxyl-Dammarane-3β, 12β, 20-Triol in Cancer Treatment: A Review of the Pharmacological Mechanisms and Pharmacokinetics | Natural Product Ginsenoside 20(S)-25-Methoxyl-Dammarane-3β, 12β, 20-Triol in Cancer Treatment: A Review of the Pharmacological Mechanisms and Pharmacokinetics Abstract Panax ginseng has been used as an herbal medicine for thousands of years. Most of its pharmacological effects are attributed to its constituent ginsenos... |
PMC12910383 | core_pubmed_pmc | Vancomycin target attainment improved following population pharmacokinetic model switch: a large-scale quasi-experimental study of precision dosing | Vancomycin target attainment improved following population pharmacokinetic model switch: a large-scale quasi-experimental study of precision dosing Abstract Abstract Objectives The aim of this study was to evaluate the impact of switching population pharmacokinetic models used for model-informed precision dosing (MIPD)... |
PMC12117184 | core_pubmed_pmc | Pharmacokinetics and Safety of Ceftazidime-Avibactam in Neonates and Young Infants: A Phase 2a, Multicenter Prospective Trial | Pharmacokinetics and Safety of Ceftazidime-Avibactam in Neonates and Young Infants: A Phase 2a, Multicenter Prospective Trial Abstract Abstract Background This phase 2a study evaluated pharmacokinetics and safety of ceftazidime-avibactam (CAZ/AVI; combination dosed as fixed 4:1 ratio) in neonates and young infants with... |
PMC12034585 | core_pubmed_pmc | Target-Controlled Infusion of Propofol: A Systematic Review of Recent Results | Target-Controlled Infusion of Propofol: A Systematic Review of Recent Results Abstract Abstract This study presents a systematic review conducted according to the PRISMA 2020 guidelines, evaluating pharmacokinetic-pharmacodynamic (PK-PD) models for target-controlled infusion (TCI) of propofol. A structured search was p... |
PMC12389140 | core_pubmed_pmc | Enhancing the Solubility and Oral Bioavailability of Trimethoprim Through PEG-PLGA Nanoparticles: A Comprehensive Evaluation of In Vitro and In Vivo Performance | Enhancing the Solubility and Oral Bioavailability of Trimethoprim Through PEG-PLGA Nanoparticles: A Comprehensive Evaluation of In Vitro and In Vivo Performance Abstract Background/Objectives: Trimethoprim (TMP), a sulfonamide antibacterial synergist, is widely used in antimicrobial therapy owing to its broad-spectrum ... |
PMC4698184 | core_pubmed_pmc | Potent inhibition of enterovirus D68 and human rhinoviruses by dipeptidyl aldehydes and α-ketoamides | Potent inhibition of enterovirus D68 and human rhinoviruses by dipeptidyl aldehydes and α-ketoamides Abstract Abstract Enterovirus D68 (EV-D68) is an emerging pathogen responsible for mild to severe respiratory infections that occur mostly in infants, children and teenagers. EV-D68, one of more than 100 non-polio enter... |
PMC12314107 | core_pubmed_pmc | Pharmacokinetics, Bioequivalence, and Safety Studies of Crisaborole Ointment in Healthy Chinese Subjects | Pharmacokinetics, Bioequivalence, and Safety Studies of Crisaborole Ointment in Healthy Chinese Subjects Abstract Abstract The aim of this study was to evaluate the bioequivalence and safety of a single application of crisaborole ointment to test formulation and reference formulation in healthy subjects under fasting c... |
PMC10134766 | core_pubmed_pmc | Total body fluid is the factor that affects the pharmacokinetics of tolvaptan, and its efficacy, in acute worsening heart failure patients | Total body fluid is the factor that affects the pharmacokinetics of tolvaptan, and its efficacy, in acute worsening heart failure patients Abstract Abstract The optimal starting dose of tolvaptan to effectively improve fluid retention in patients with heart failure (HF) is unknown. This study explored the factors affec... |
PMC4731946 | core_pubmed_pmc | Prioritization of anti-malarial hits from nature: chemo-informatic profiling of natural products with in vitro antiplasmodial activities and currently registered anti-malarial drugs | Prioritization of anti-malarial hits from nature: chemo-informatic profiling of natural products with in vitro antiplasmodial activities and currently registered anti-malarial drugs Abstract Background A large number of natural products have shown in vitro antiplasmodial activities. Early identification and prioritizat... |
PMC4302143 | core_pubmed_pmc | Clinical considerations in transitioning patients with epilepsy from clonazepam to clobazam: a case series | Clinical considerations in transitioning patients with epilepsy from clonazepam to clobazam: a case series Abstract Introduction In treating refractory epilepsy, many clinicians are interested in methods used to transition patients receiving clonazepam to clobazam to maintain or increase seizure control, improve tolera... |
PMC5378006 | core_pubmed_pmc | Drug interactions between hormonal contraceptives and antiretrovirals | Drug interactions between hormonal contraceptives and antiretrovirals Abstract Abstract Objective: To summarize published evidence on drug interactions between hormonal contraceptives and antiretrovirals. Design: Systematic review of the published literature. Methods: We searched PubMed, POPLINE, and EMBASE for peer-re... |
PMC5118030 | core_pubmed_pmc | Influence of curcumin on the pharmacodynamics and pharmacokinetics of gliclazide in animal models | Influence of curcumin on the pharmacodynamics and pharmacokinetics of gliclazide in animal models Abstract Purpose Patients suffering from obesity-related diseases use multiple prescription drugs to control their condition, and it is therefore essential to determine the safety and efficacy of any combination. Gliclazid... |
PMC6314320 | core_pubmed_pmc | Co-delivery doxorubicin and silybin for anti-hepatoma via enhanced oral hepatic-targeted efficiency | Co-delivery doxorubicin and silybin for anti-hepatoma via enhanced oral hepatic-targeted efficiency Abstract Background To establish the combination of doxorubicin (DOX) and silybin (SLB) in oral hepatic-targeting liposomes with the goal of reducing cardiotoxic side effects and improve oral hepatoma treatment. Methods ... |
PMC6976992 | core_pubmed_pmc | Hepatic and intestinal biotransformation gene expression and drug disposition in a dextran sulfate sodium-induced colitis mouse model | Hepatic and intestinal biotransformation gene expression and drug disposition in a dextran sulfate sodium-induced colitis mouse model Abstract We examined the impact of gut inflammation on the expression of cytochrome P450 (P450) and other biotransformation genes in male mice using a dextran sulfate sodium (DSS)-induce... |
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