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PMC11831190 | core_pubmed_pmc | Phase I clinical trial to assess safety and efficacy of Oraxol, a novel oral paclitaxel chemotherapy agent, in patients with previously treated metastatic breast cancer | Phase I clinical trial to assess safety and efficacy of Oraxol, a novel oral paclitaxel chemotherapy agent, in patients with previously treated metastatic breast cancer Abstract Abstract Oraxol, a novel oral paclitaxel chemotherapy agent, has emerged as a potential alternative for treating metastatic breast cancer (MBC... |
PMC10144804 | core_pubmed_pmc | Behavioral, Neurochemical and Developmental Effects of Chronic Oral Methylphenidate: A Review | Behavioral, Neurochemical and Developmental Effects of Chronic Oral Methylphenidate: A Review Abstract The majority of animal studies on methylphenidate (MP) use intraperitoneal (IP) injections, subcutaneous (SC) injections, or the oral gavage route of administration. While all these methods allow for delivery of MP, i... |
PMC8905690 | core_pubmed_pmc | Eculizumab precision-dosing algorithm for thrombotic microangiopathy in children and young adults undergoing HSCT | Eculizumab precision-dosing algorithm for thrombotic microangiopathy in children and young adults undergoing HSCT Abstract Key Points This large study examined eculizumab PK/PD in bleeding and nonbleeding patients with TA-TMA. PK/PD model-based eculizumab dosing is needed for bleeding in TA-TMA, whereas fixed-dose regi... |
PMC12691189 | core_pubmed_pmc | Machine Learning-Based Algorithm for Tacrolimus Dose Optimization in Hospitalized Kidney Transplant Patients | Machine Learning-Based Algorithm for Tacrolimus Dose Optimization in Hospitalized Kidney Transplant Patients Abstract Abstract Background : Tacrolimus is a cornerstone immunosuppressant in kidney transplantation, but its narrow therapeutic index and marked inter-patient variability complicate dose optimization. Convent... |
PMC7487995 | core_pubmed_pmc | Navafenterol (AZD8871) in patients with COPD: a randomized, double-blind, phase I study evaluating safety and pharmacodynamics of single doses of this novel, inhaled, long-acting, dual-pharmacology bronchodilator | Navafenterol (AZD8871) in patients with COPD: a randomized, double-blind, phase I study evaluating safety and pharmacodynamics of single doses of this novel, inhaled, long-acting, dual-pharmacology bronchodilator Abstract Abstract Background Navafenterol (AZD8871) is a dual-pharmacology muscarinic antagonist β 2− agoni... |
PMC7990449 | core_pubmed_pmc | Effects of Helicobacter pylori on Levodopa Pharmacokinetics | Effects of Helicobacter pylori on Levodopa Pharmacokinetics Abstract Background: Infection with Helicobacter pylori seems overrepresented in Parkinson’s disease. Clinical observations suggest a suboptimal treatment effect of levodopa in Helicobacter positive patients. Objective: Describe and explain the connection betw... |
PMC9692130 | core_pubmed_pmc | Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes | Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes Abstract Abstract UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgeni... |
PMC6120116 | core_pubmed_pmc | Nanoparticle-Mediated Delivery of Neuroprotective Substances for the Treatment of Diabetic Retinopathy | Nanoparticle-Mediated Delivery of Neuroprotective Substances for the Treatment of Diabetic Retinopathy Abstract Background: Diabetic retinopathy (DR) is a major complication of diabetes, characterized by extensive vascular pathology leading to vision loss. Neuronal suffering and death are also present in the diabetic r... |
PMC10689590 | core_pubmed_pmc | Single time point quantitation of cerebral glucose metabolism by FDG-PET without arterial sampling | Single time point quantitation of cerebral glucose metabolism by FDG-PET without arterial sampling Abstract Abstract Background Until recently, quantitation of the net influx of 2-[ 18 F]fluorodeoxyglucose (FDG) to brain ( K i ) and the cerebrometabolic rate for glucose (CMR glc ) required serial arterial blood samplin... |
PMC4086096 | core_pubmed_pmc | DDI-CPI , a server that predicts drug–drug interactions through implementing the chemical–protein interactome | DDI-CPI , a server that predicts drug–drug interactions through implementing the chemical–protein interactome Abstract Abstract Drug–drug interactions (DDIs) may cause serious side-effects that draw great attention from both academia and industry. Since some DDIs are mediated by unexpected drug–human protein interactio... |
PMC6584248 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Immune Checkpoint Inhibitors | Clinical Pharmacokinetics and Pharmacodynamics of Immune Checkpoint Inhibitors Abstract Abstract Immune checkpoint inhibitors (ICIs) have demonstrated significant clinical impact in improving overall survival of several malignancies associated with poor outcomes; however, only 20–40% of patients will show long-lasting ... |
PMC9938521 | core_pubmed_pmc | Clinical significance of the rivaroxaban–dronedarone interaction: insights from physiologically based pharmacokinetic modelling | Clinical significance of the rivaroxaban–dronedarone interaction: insights from physiologically based pharmacokinetic modelling Abstract Abstract Patients with atrial fibrillation may require rhythm control therapy in addition to anticoagulation therapy for the prevention of stroke. Since 2012, the European Society of ... |
PMC5317268 | core_pubmed_pmc | An in vivo mechanism for the reduced peripheral neurotoxicity of NK105: a paclitaxel-incorporating polymeric micellar nanoparticle formulation | An in vivo mechanism for the reduced peripheral neurotoxicity of NK105: a paclitaxel-incorporating polymeric micellar nanoparticle formulation Abstract In our previous rodent studies, the paclitaxel (PTX)-incorporating polymeric micellar nanoparticle formulation NK105 had showed significantly stronger antitumor effects... |
PMC12631680 | core_pubmed_pmc | Pharmacokinetic Characterization of Single-Stranded DNA in Murine Models Using High-Specific-Activity 68 Ga Radiolabeling Coupled with Dynamic Positron Emission Tomography | Pharmacokinetic Characterization of Single-Stranded DNA in Murine Models Using High-Specific-Activity 68 Ga Radiolabeling Coupled with Dynamic Positron Emission Tomography Abstract Abstract This study aimed to develop an efficient concentration methodology to enhance the specific activity of 68 Ga. By systematically op... |
PMC12756206 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of a High-Dose, Rapid-Infusion Monoclonal Antibody: Phase I Results for Intravenous Sotrovimab 3000 mg | Safety, Tolerability and Pharmacokinetics of a High-Dose, Rapid-Infusion Monoclonal Antibody: Phase I Results for Intravenous Sotrovimab 3000 mg Abstract Background and Objectives The emergence of severe acute respiratory syndrome coronavirus 2 variants against which sotrovimab has lower in vitro neutralisation activit... |
PMC4387274 | core_pubmed_pmc | A phase 1 dose escalation study of BI 831266, an inhibitor of Aurora kinase B, in patients with advanced solid tumors | A phase 1 dose escalation study of BI 831266, an inhibitor of Aurora kinase B, in patients with advanced solid tumors Abstract Summary Purpose BI 831266 is a potent, selective, low-molecular-weight inhibitor of Aurora kinase B. This trial aimed to determine the maximum tolerated dose (MTD) of BI 831266 in patients with... |
PMC5002098 | core_pubmed_pmc | Evaluation of high-dose rifampin in patients with new, smear-positive tuberculosis (HIRIF): study protocol for a randomized controlled trial | Evaluation of high-dose rifampin in patients with new, smear-positive tuberculosis (HIRIF): study protocol for a randomized controlled trial Abstract Background Evidence has existed for decades that higher doses of rifampin may be more effective, but potentially more toxic, than standard doses used in tuberculosis trea... |
PMC7187331 | core_pubmed_pmc | Pharmacokinetics of Patisiran, the First Approved RNA Interference Therapy in Patients With Hereditary Transthyretin‐Mediated Amyloidosis | Pharmacokinetics of Patisiran, the First Approved RNA Interference Therapy in Patients With Hereditary Transthyretin‐Mediated Amyloidosis Abstract Abstract Hereditary transthyretin‐mediated (hATTR) amyloidosis is a rare, inherited, progressively debilitating, and often fatal disease caused by deposition of mutated tran... |
PMC4706279 | core_pubmed_pmc | Pharmacokinetic Interactions for Drugs with a Long Half-Life—Evidence for the Need of Model-Based Analysis | Pharmacokinetic Interactions for Drugs with a Long Half-Life—Evidence for the Need of Model-Based Analysis Abstract Pharmacokinetic drug-drug interactions (DDIs) can lead to undesired drug exposure, resulting in insufficient efficacy or aggravated toxicity. Accurate quantification of DDIs is therefore crucial but may b... |
PMC6541859 | core_pubmed_pmc | Pharmacokinetics of intravenous and intramuscular danofloxacin in red-eared slider turtles ( Trachemys scripta elegans ) | Pharmacokinetics of intravenous and intramuscular danofloxacin in red-eared slider turtles ( Trachemys scripta elegans ) Abstract This study aimed to investigate the pharmacokinetics of danofloxacin in red-eared slider turtle ( Trachemys scripta elegans ) following a single intravenous (IV) and intramuscular (IM) admin... |
PMC6373389 | core_pubmed_pmc | The Role of Fluoroquinolones in the Treatment of Tuberculosis in 2019 | The Role of Fluoroquinolones in the Treatment of Tuberculosis in 2019 Abstract The inability to use powerful antituberculosis drugs in an increasing number of patients seems to be the biggest threat towards global tuberculosis (TB) elimination. Simplified, shorter and preferably less toxic drug regimens are being inves... |
PMC12299613 | core_pubmed_pmc | Discrepancies in Recommendations on Pharmacokinetic Drug Interactions for Anticancer Medications and Direct Oral Anticoagulants (DOAC): A Comparative Analysis of Different Clinical Decision Support Systems and Sources | Discrepancies in Recommendations on Pharmacokinetic Drug Interactions for Anticancer Medications and Direct Oral Anticoagulants (DOAC): A Comparative Analysis of Different Clinical Decision Support Systems and Sources Abstract Background/objectives: In some cases of concomitant use of direct oral anticoagulants (DOAC) ... |
PMC8586700 | core_pubmed_pmc | Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats | Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats Abstract The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in huma... |
PMC12875155 | core_pubmed_pmc | Pharmacokinetic Comparability of ABP 654, a Biosimilar to Ustekinumab, Administered Either via Prefilled Syringe or Autoinjector in Healthy Adults: Results from a Randomized, Open‐Label, Parallel‐Group Study | Pharmacokinetic Comparability of ABP 654, a Biosimilar to Ustekinumab, Administered Either via Prefilled Syringe or Autoinjector in Healthy Adults: Results from a Randomized, Open‐Label, Parallel‐Group Study Abstract Abstract ABP 654, a biosimilar to ustekinumab reference product, is available in a prefilled syringe (P... |
PMC4984914 | core_pubmed_pmc | Mipsagargin, a novel thapsigargin-based PSMA-activated prodrug: results of a first-in-man phase I clinical trial in patients with refractory, advanced or metastatic solid tumours | Mipsagargin, a novel thapsigargin-based PSMA-activated prodrug: results of a first-in-man phase I clinical trial in patients with refractory, advanced or metastatic solid tumours Abstract Abstract Background: Mipsagargin (G-202; (8- O -(12-aminododecanoyl)-8- O -debutanoyl thapsigargin)-Asp- γ -Glu- γ -Glu- γ -GluGluOH... |
PMC12518216 | core_pubmed_pmc | Decoding the EPAR scientific assessment for clinical practice: a tutorial using tislelizumab in NSCLC | Decoding the EPAR scientific assessment for clinical practice: a tutorial using tislelizumab in NSCLC Abstract Abstract European Public Assessment Reports (EPARs) are among the most scientifically rigorous sources available for evaluating newly approved oncology therapeutics, yet their complexity often limits clinical ... |
PMC12567244 | core_pubmed_pmc | Innovative Amino-Functionalization of Pyrido[2,3- d ]pyrimidine Scaffolds for Broad Therapeutic Applications Supported by Computational Analyses | Innovative Amino-Functionalization of Pyrido[2,3- d ]pyrimidine Scaffolds for Broad Therapeutic Applications Supported by Computational Analyses Abstract Abstract Background: Derivatives of Pyrido[2,3- d ]pyrimidine-6-carboxylate are promising multi-target scaffolds. This study focused on synthesizing 16 amino-function... |
PMC6018888 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and tolerability of verinurad, a selective uric acid reabsorption inhibitor, in healthy Japanese and non-Asian male subjects | Pharmacokinetics, pharmacodynamics, and tolerability of verinurad, a selective uric acid reabsorption inhibitor, in healthy Japanese and non-Asian male subjects Abstract Purpose Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for treatment of gout and asymptomatic hyperurice... |
PMC10830790 | core_pubmed_pmc | Imperatorin interacts additively with novel antiseizure medications in the mouse maximal electroshock-induced seizure model: an isobolographic transformation | Imperatorin interacts additively with novel antiseizure medications in the mouse maximal electroshock-induced seizure model: an isobolographic transformation Abstract Abstract Background Anticonvulsant effects of imperatorin (IMP) have been experimentally confirmed earlier, but no information is available on the intera... |
PMC6278385 | core_pubmed_pmc | Preclinical Pharmacokinetics of C118P, a Novel Prodrug of Microtubules Inhibitor and Its Metabolite C118 in Mice, Rats, and Dogs | Preclinical Pharmacokinetics of C118P, a Novel Prodrug of Microtubules Inhibitor and Its Metabolite C118 in Mice, Rats, and Dogs Abstract Abstract C118P, a phosphate prodrug of C118, which is a novel microtubule protein inhibitor, is currently under Phase I clinical development in China for treating ovarian cancer and ... |
PMC7533260 | core_pubmed_pmc | Design and tests of prospective property predictions for novel antimalarial 2-aminopropylaminoquinolones | Design and tests of prospective property predictions for novel antimalarial 2-aminopropylaminoquinolones Abstract Abstract There is a pressing need to improve the efficiency of drug development, and nowhere is that need more clear than in the case of neglected diseases like malaria. The peculiarities of pyrimidine meta... |
PMC12196403 | core_pubmed_pmc | Thermosensitive Mucoadhesive Intranasal In Situ Gel of Risperidone for Nose-to-Brain Targeting: Physiochemical and Pharmacokinetics Study | Thermosensitive Mucoadhesive Intranasal In Situ Gel of Risperidone for Nose-to-Brain Targeting: Physiochemical and Pharmacokinetics Study Abstract Background/Objectives: Non-invasive central nervous system (CNS) therapies are limited by complex mechanisms and the blood–brain barrier, but nasal delivery offers a promisi... |
PMC12217487 | core_pubmed_pmc | Evaluating tigecycline dosing for hospital-acquired pneumonia patients: insights from physiologically-based pharmacokinetic modeling of lung exposure | Evaluating tigecycline dosing for hospital-acquired pneumonia patients: insights from physiologically-based pharmacokinetic modeling of lung exposure Abstract ABSTRACT Tigecycline is increasingly used off-label for hospital-acquired pneumonia (HAP), though its efficacy and optimal dosing remain uncertain. Lung exposure... |
PMC12621185 | core_pubmed_pmc | Design, Syntheses, and Pharmacological Evaluations of Core Ring Expanded Fentanyl Analogues as Potential Counteracting Agents Against Fentanyl Induced Respiratory Depression | Design, Syntheses, and Pharmacological Evaluations of Core Ring Expanded Fentanyl Analogues as Potential Counteracting Agents Against Fentanyl Induced Respiratory Depression Abstract Abstract The escalating synthetic opioid crisis necessitates novel treatments, especially for fentanyl overdose. This study presents 84 r... |
PMC11124240 | core_pubmed_pmc | In Silico Design of Potential Small-Molecule Antibiotic Adjuvants against Salmonella typhimurium Ortho Acetyl Sulphydrylase Synthase to Address Antimicrobial Resistance | In Silico Design of Potential Small-Molecule Antibiotic Adjuvants against Salmonella typhimurium Ortho Acetyl Sulphydrylase Synthase to Address Antimicrobial Resistance Abstract Abstract The inhibition of O -acetyl sulphydrylase synthase isoforms has been reported to represent a promising approach for the development o... |
PMC7039713 | core_pubmed_pmc | Genotype tailored treatment of mild symptomatic acid reflux in children with uncontrolled asthma (GenARA): Rationale and methods | Genotype tailored treatment of mild symptomatic acid reflux in children with uncontrolled asthma (GenARA): Rationale and methods Abstract Abstract Asthma causes enormous suffering and cost for children in the US and around the world [ , , ]. Co-morbid gastroesophageal reflux disease (GERD) makes asthma management more ... |
PMC9103378 | core_pubmed_pmc | Unraveling enhanced brain delivery of paliperidone-loaded lipid nanoconstructs: pharmacokinetic, behavioral, biochemical, and histological aspects | Unraveling enhanced brain delivery of paliperidone-loaded lipid nanoconstructs: pharmacokinetic, behavioral, biochemical, and histological aspects Abstract Abstract Antipsychotics are accompanied by extrapyramidal side effects that deter treatment adherence and patient compliance. Paliperidone (PPD), an atypical (secon... |
PMC11727040 | core_pubmed_pmc | Monophosphate Derivatives of Luteolin and Apigenin as Efficient Precursors with Improved Oral Bioavailability in Rats | Monophosphate Derivatives of Luteolin and Apigenin as Efficient Precursors with Improved Oral Bioavailability in Rats Abstract Luteolin (Lut) and apigenin (Apn), flavones present in various edible plants, exhibit diverse antioxidant and pharmacological activities but have limited in vivo efficacy due to low water solub... |
PMC3910009 | core_pubmed_pmc | Use of a Population Pharmacokinetic Approach for the Clinical Development of a Fixed-Dose Subcutaneous Formulation of Trastuzumab | Use of a Population Pharmacokinetic Approach for the Clinical Development of a Fixed-Dose Subcutaneous Formulation of Trastuzumab Abstract A new subcutaneous (s.c.) trastuzumab formulation provides savings in terms of time and is preferred by patients and health care professionals relative to standard intravenous (i.v.... |
PMC10347189 | core_pubmed_pmc | Amelioration of Cancer Employing Chitosan, Its Derivatives, and Chitosan-Based Nanoparticles: Recent Updates | Amelioration of Cancer Employing Chitosan, Its Derivatives, and Chitosan-Based Nanoparticles: Recent Updates Abstract The limitations associated with the conventional treatment of cancer have necessitated the design and development of novel drug delivery systems based mainly on nanotechnology. These novel drug delivery... |
PMC4636169 | core_pubmed_pmc | Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment | Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment Abstract Celastrol (CL), a triterpenoid extracted from the Chinese herb Tripterygium wilfordii , has recently attracted interest for its potential antitumor effects. However, unfavorable physicochemical and pharmacokinetics properties suc... |
PMC11117356 | core_pubmed_pmc | Meropenem Disposition in Neonatal and Pediatric Extracorporeal Membrane Oxygenation and Continuous Renal Replacement Therapy | Meropenem Disposition in Neonatal and Pediatric Extracorporeal Membrane Oxygenation and Continuous Renal Replacement Therapy Abstract Abstract This study aimed to characterize the impact of extracorporeal membrane oxygenation (ECMO) on the pharmacokinetics (PK) of meropenem in neonates and children and to provide recom... |
PMC4921118 | core_pubmed_pmc | Everolimus pharmacokinetics and its exposure–toxicity relationship in patients with thyroid cancer | Everolimus pharmacokinetics and its exposure–toxicity relationship in patients with thyroid cancer Abstract Background Everolimus is a mTOR inhibitor used for the treatment of different solid malignancies. Many patients treated with the registered fixed 10 mg dose once daily are in need of dose interruptions, reduction... |
PMC7338825 | core_pubmed_pmc | Effect of food on the pharmacokinetics of the WEE1 inhibitor adavosertib (AZD1775) in patients with advanced solid tumors | Effect of food on the pharmacokinetics of the WEE1 inhibitor adavosertib (AZD1775) in patients with advanced solid tumors Abstract Purpose To support future dosing recommendations, the effect of food on the pharmacokinetics of adavosertib, a first-in-class, small-molecule reversible inhibitor of WEE1 kinase, was assess... |
PMC11269472 | core_pubmed_pmc | Stimulus mediation, specificity and impact of menthol in rats trained to discriminate puffs of nicotine e-cigarette aerosol from nicotine-free aerosol | Stimulus mediation, specificity and impact of menthol in rats trained to discriminate puffs of nicotine e-cigarette aerosol from nicotine-free aerosol Abstract Abstract Rationale It is unclear if e-cigarettes have reduced abuse liability relative to traditional cigarettes, especially when considering advanced devices w... |
PMC7125811 | core_pubmed_pmc | Evaluation of potential herb-drug interactions between oseltamivir and commonly used anti-influenza Chinese medicinal herbs | Evaluation of potential herb-drug interactions between oseltamivir and commonly used anti-influenza Chinese medicinal herbs Abstract Ethnopharmacological relevance According to Traditional Chinese Medicine theory, influenza is categorized as a warm disease or Wen Bing. The Wen Bing formulas, such as Yin-Qiao-San and Sa... |
PMC5785470 | core_pubmed_pmc | Characterization of Nanodiamond-based anti-HIV drug Delivery to the Brain | Characterization of Nanodiamond-based anti-HIV drug Delivery to the Brain Abstract Human Immunodeficiency Virus Type 1 (HIV-1) remains one of the leading causes of death worldwide. Present combination antiretroviral therapy has substantially improved HIV-1 related pathology. However, delivery of therapeutic agents to t... |
PMC9305536 | core_pubmed_pmc | Decreased isavuconazole trough concentrations in the treatment of invasive aspergillosis in an adult patient receiving extracorporeal membrane oxygenation support | Decreased isavuconazole trough concentrations in the treatment of invasive aspergillosis in an adult patient receiving extracorporeal membrane oxygenation support Abstract Abstract Purpose We present the case of a 56-year-old man with stage IV sarcoidosis on veno-venous extracorporeal membrane oxygenation (VV-ECMO) sup... |
PMC6231440 | core_pubmed_pmc | In vitro and in vivo quantification of chloroprocaine release from an implantable device in a piglet postoperative pain model | In vitro and in vivo quantification of chloroprocaine release from an implantable device in a piglet postoperative pain model Abstract Abstract Background The pharmacokinetic properties and clinical advantages of the local anesthetic chloroprocaine are well known. Here, we studied the pharmacokinetic profile of a new h... |
PMC9291816 | core_pubmed_pmc | Model‐Based Drug–Drug Interaction Extrapolation Strategy From Adults to Children: Risdiplam in Pediatric Patients With Spinal Muscular Atrophy | Model‐Based Drug–Drug Interaction Extrapolation Strategy From Adults to Children: Risdiplam in Pediatric Patients With Spinal Muscular Atrophy Abstract Abstract Risdiplam (Evrysdi) improves motor neuron function in patients with spinal muscular atrophy (SMA) and has been approved for the treatment of patients ≥2 months... |
PMC8726733 | core_pubmed_pmc | Development of a fully canine anti-canine CTLA4 monoclonal antibody for comparative translational research in dogs with spontaneous tumors | Development of a fully canine anti-canine CTLA4 monoclonal antibody for comparative translational research in dogs with spontaneous tumors Abstract ABSTRACT The immune checkpoint inhibitor (ICI) ipilimumab has revolutionized the treatment of patients with different cancer histologies, including melanoma, renal cell car... |
PMC5078031 | core_pubmed_pmc | Phase I clinical study of RG7356, an anti-CD44 humanized antibody, in patients with acute myeloid leukemia | Phase I clinical study of RG7356, an anti-CD44 humanized antibody, in patients with acute myeloid leukemia Abstract Abstract RG7356, a recombinant anti-CD44 immunoglobulin G1 humanized monoclonal antibody, inhibits cell adhesion and has been associated with macrophage activation in preclinical models. We report results... |
PMC10220852 | core_pubmed_pmc | Exposure–Response Analysis of the Sodium–Glucose Cotransporter-2 Inhibitors Dapagliflozin and Empagliflozin on Kidney Hemodynamics in Patients with Type 2 Diabetes | Exposure–Response Analysis of the Sodium–Glucose Cotransporter-2 Inhibitors Dapagliflozin and Empagliflozin on Kidney Hemodynamics in Patients with Type 2 Diabetes Abstract Abstract Sodium–glucose cotransporter-2 (SGLT2) inhibitors improve markers for renal and cardiovascular outcomes in patients with and without type ... |
PMC3064895 | core_pubmed_pmc | A phase I open-label study evaluating the cardiovascular safety of sorafenib in patients with advanced cancer | A phase I open-label study evaluating the cardiovascular safety of sorafenib in patients with advanced cancer Abstract Purpose To characterize the cardiovascular profile of sorafenib, a multitargeted kinase inhibitor, in patients with advanced cancer. Methods Fifty-three patients with advanced cancer received oral sora... |
PMC5649121 | core_pubmed_pmc | Lack of QT Prolongation for 2′- O -Methoxyethyl-Modified Antisense Oligonucleotides Based on Retrospective Exposure/Response Analysis of Ten Phase 1 Dose-Escalation Placebo-Controlled Studies in Healthy Subjects | Lack of QT Prolongation for 2′- O -Methoxyethyl-Modified Antisense Oligonucleotides Based on Retrospective Exposure/Response Analysis of Ten Phase 1 Dose-Escalation Placebo-Controlled Studies in Healthy Subjects Abstract The potential of QT prolongation of ten 2′- O -methoxyethyl-modified (2′-MOE) antisense oligonucleo... |
PMC9599532 | core_pubmed_pmc | PHLPP Inhibitor NSC74429 Is Neuroprotective in Rodent Models of Cardiac Arrest and Traumatic Brain Injury | PHLPP Inhibitor NSC74429 Is Neuroprotective in Rodent Models of Cardiac Arrest and Traumatic Brain Injury Abstract Pleckstrin homology domain and leucine rich repeat protein phosphatase (PHLPP) knockout mice have improved outcomes after a stroke, traumatic brain injury (TBI), and decreased maladaptive vascular remodeli... |
PMC7830329 | core_pubmed_pmc | Complex Factors and Challenges that Affect the Pharmacology, Safety and Efficacy of Nanocarrier Drug Delivery Systems | Complex Factors and Challenges that Affect the Pharmacology, Safety and Efficacy of Nanocarrier Drug Delivery Systems Abstract Abstract Major developments in nanomedicines, such as nanoparticles (NPs), nanosomes, and conjugates, have revolutionized drug delivery capabilities over the past four decades. Although nanocar... |
PMC5818482 | core_pubmed_pmc | Experimental study of the anti-tumour activity and pharmacokinetics of arctigenin and its valine ester derivative | Experimental study of the anti-tumour activity and pharmacokinetics of arctigenin and its valine ester derivative Abstract Arctigenin (ARG) is a functional active component that has important physiological and pharmacological activities. The anti-tumour and anti-inflammatory activities of ARG show good potential for ap... |
PMC4612330 | core_pubmed_pmc | A phase 1 study evaluating the pharmacokinetics and preliminary efficacy of veliparib (ABT-888) in combination with carboplatin/paclitaxel in Japanese subjects with non-small cell lung cancer (NSCLC) | A phase 1 study evaluating the pharmacokinetics and preliminary efficacy of veliparib (ABT-888) in combination with carboplatin/paclitaxel in Japanese subjects with non-small cell lung cancer (NSCLC) Abstract Abstact Introduction Veliparib is a potent, orally bioavailable PARP inhibitor that enhances efficacy of DNA-da... |
PMC8779255 | core_pubmed_pmc | Determining the Anticancer Activity of Sphingosine Kinase Inhibitors Containing Heteroatoms in Their Tail Structure | Determining the Anticancer Activity of Sphingosine Kinase Inhibitors Containing Heteroatoms in Their Tail Structure Abstract Abstract Sphingosine kinase (SK) enzyme, a central player of sphingolipid rheostat, catalyzes the phosphorylation of sphingosine to the bioactive lipid mediator sphingosine 1 phosphate (S1P), whi... |
PMC11255394 | core_pubmed_pmc | Piperacillin/tazobactam treatment in children: evidence of subtherapeutic concentrations | Piperacillin/tazobactam treatment in children: evidence of subtherapeutic concentrations Abstract Abstract Objective Piperacillin/tazobactam (PIP/TAZ) is used for the treatment of lower respiratory tract bacterial infections in children. This study was performed to evaluate if the current dosing regimen results in ther... |
PMC7693160 | core_pubmed_pmc | Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling to Predict the Impact of CYP2C9 Genetic Polymorphisms, Co-Medication and Formulation on the Pharmacokinetics and Pharmacodynamics of Flurbiprofen | Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling to Predict the Impact of CYP2C9 Genetic Polymorphisms, Co-Medication and Formulation on the Pharmacokinetics and Pharmacodynamics of Flurbiprofen Abstract Abstract Physiologically based pharmacokinetic/pharmacodynamic (PBPK/PD) models can serve as a powerfu... |
PMC8621408 | core_pubmed_pmc | Absorption of N-acetylcysteine in Healthy and Mycoplasma gallisepticum -Infected Chickens | Absorption of N-acetylcysteine in Healthy and Mycoplasma gallisepticum -Infected Chickens Abstract Abstract N-acetylcysteine (NAC) is widely used as a mucolytic agent in cases with inflammation of the lungs. NAC is applied in poultry with aflatoxin B1 intoxication as an antioxidant, but its pharmacokinetics are not kno... |
PMC10542238 | core_pubmed_pmc | A field bioassay for assessing ivermectin bio-efficacy in wild malaria vectors | A field bioassay for assessing ivermectin bio-efficacy in wild malaria vectors Abstract Abstract Background Ivermectin (IVM) mass drug administration is a candidate complementary malaria vector control tool. Ingestion of blood from IVM treated hosts results in reduced survival in mosquitoes. Estimating bio-efficacy of ... |
PMC3765993 | core_pubmed_pmc | The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold | The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold Abstract Background Drugs targeting insomnia ideally promote sleep throughout the night, maintain normal sleep architecture, and are devoid of residual effects associated with morning sedation. Th... |
PMC10133580 | core_pubmed_pmc | Computational pharmacology and computational chemistry of 4-hydroxyisoleucine: Physicochemical, pharmacokinetic, and DFT-based approaches | Computational pharmacology and computational chemistry of 4-hydroxyisoleucine: Physicochemical, pharmacokinetic, and DFT-based approaches Abstract Abstract Computational pharmacology and chemistry of drug-like properties along with pharmacokinetic studies have made it more amenable to decide or predict a potential drug... |
PMC8190023 | core_pubmed_pmc | Capsule and Sprinkle Formulations of Lubiprostone Are Not Biologically Similar in Patients with Functional Constipation | Capsule and Sprinkle Formulations of Lubiprostone Are Not Biologically Similar in Patients with Functional Constipation Abstract Introduction Lubiprostone capsules are approved for managing three different chronic constipation conditions. A “sprinkle” formulation may facilitate use in individuals with difficulty swallo... |
PMC8716378 | core_pubmed_pmc | Radiolabeled Monoclonal Antibody Against Colony-Stimulating Factor 1 Receptor Specifically Distributes to the Spleen and Liver in Immunocompetent Mice | Radiolabeled Monoclonal Antibody Against Colony-Stimulating Factor 1 Receptor Specifically Distributes to the Spleen and Liver in Immunocompetent Mice Abstract Macrophages can promote tumor development. Preclinically, targeting macrophages by colony-stimulating factor 1 (CSF1)/CSF1 receptor (CSF1R) monoclonal antibodie... |
PMC5963635 | core_pubmed_pmc | Ocular Distribution and Pharmacokinetics of Lifitegrast in Pigmented Rabbits and Mass Balance in Beagle Dogs | Ocular Distribution and Pharmacokinetics of Lifitegrast in Pigmented Rabbits and Mass Balance in Beagle Dogs Abstract Abstract Purpose: Lifitegrast is approved in the United States for the treatment of dry eye disease (DED). We assessed lifitegrast's ocular distribution/pharmacokinetic profile in rabbits, and 14 C-lifi... |
PMC10100048 | core_pubmed_pmc | Acetaminophen pharmacokinetics in infants and children with congenital heart disease | Acetaminophen pharmacokinetics in infants and children with congenital heart disease Abstract Abstract Background Acetaminophen is routinely used for perioperative analgesia in children undergoing major surgical procedures. There are few estimates of acetaminophen pharmacokinetic parameters in children with congenital ... |
PMC6437720 | core_pubmed_pmc | Introduction of the YTE mutation into the non-immunogenic HIV bnAb PGT121 induces anti-drug antibodies in macaques | Introduction of the YTE mutation into the non-immunogenic HIV bnAb PGT121 induces anti-drug antibodies in macaques Abstract Recombinant antibodies play increasingly important roles as immunotherapeutic treatments for human cancers as well as inflammatory and infectious diseases and have revolutionized their management.... |
PMC11169020 | core_pubmed_pmc | In vitro to in vivo extrapolation to derive a metabolism factor for estimating the aggregate exposure to salicylic acid after dermal exposure of its esters | In vitro to in vivo extrapolation to derive a metabolism factor for estimating the aggregate exposure to salicylic acid after dermal exposure of its esters Abstract As part of the safety assessment of salicylate esters in cosmetics, we developed a metabolism factor based on in vitro to in vivo extrapolation (IVIVE) to ... |
PMC7497411 | core_pubmed_pmc | Applications of the microphysiology systems database for experimental ADME-Tox and disease models † | Applications of the microphysiology systems database for experimental ADME-Tox and disease models † Abstract The Microphysiology Systems Database (MPS) is a critical tool for the design, management, analysis, and sharing of MPS study data. Abstract To accelerate the development and application of Microphysiological Sys... |
PMC6955637 | core_pubmed_pmc | Comparison of the Pharmacokinetics, Safety, and Tolerability of the Autoinjector (AI) and Pre-Filled Syringe (PFS) of SB4 in Healthy Subjects | Comparison of the Pharmacokinetics, Safety, and Tolerability of the Autoinjector (AI) and Pre-Filled Syringe (PFS) of SB4 in Healthy Subjects Abstract Purpose SB4 is an etanercept biosimilar, approved by the European Commission (EC) and the US Food and Drug Administration (FDA) following a demonstration of equivalent e... |
PMC9579388 | core_pubmed_pmc | Effect of CSL112 (apolipoprotein A‐I [human]) on cholesterol efflux capacity in Japanese subjects: Findings from a phase I study and a cross‐study comparison | Effect of CSL112 (apolipoprotein A‐I [human]) on cholesterol efflux capacity in Japanese subjects: Findings from a phase I study and a cross‐study comparison Abstract Abstract CSL112 (apolipoprotein A‐I [apoA‐I, human]) is a novel drug in development to reduce the risk of recurrent cardiovascular events following acute... |
PMC8066515 | core_pubmed_pmc | Drug-Drug Interactions Leading to Adverse Drug Reactions with Rivaroxaban: A Systematic Review of the Literature and Analysis of VigiBase | Drug-Drug Interactions Leading to Adverse Drug Reactions with Rivaroxaban: A Systematic Review of the Literature and Analysis of VigiBase Abstract Abstract Rivaroxaban has become an alternative to vitamin K antagonists, which are considered to be at higher risk of drug-drug interactions (DDI) and more difficult to use.... |
PMC4626400 | core_pubmed_pmc | The Safety and Pharmacokinetics of Carprofen, Flunixin and Phenylbutazone in the Cape Vulture ( Gyps coprotheres ) following Oral Exposure | The Safety and Pharmacokinetics of Carprofen, Flunixin and Phenylbutazone in the Cape Vulture ( Gyps coprotheres ) following Oral Exposure Abstract The following study evaluates the overt toxic potential of carprofen (CRP), flunixin (FXN) and phenylbutazone (PBZ) in Old world vultures in relation to historic toxicity d... |
PMC10494459 | core_pubmed_pmc | A randomized trial comparing LY01011, biosimilar candidate, with the reference product denosumab (Xgeva®) in healthy Chinese subjects | A randomized trial comparing LY01011, biosimilar candidate, with the reference product denosumab (Xgeva®) in healthy Chinese subjects Abstract Highlights • Patients with bone metastasis from solid tumors could experience skeletal related events, which lead to impaired functional status and quality of life. • The refere... |
PMC12163105 | core_pubmed_pmc | Do Liposomal Vitamin C Formulations Have Improved Bioavailability? A Scoping Review Identifying Future Research Directions | Do Liposomal Vitamin C Formulations Have Improved Bioavailability? A Scoping Review Identifying Future Research Directions Abstract ABSTRACT Due to the essential requirement of vitamin C (ascorbate) by humans, formulation of the vitamin to increase its bioavailability is of relevance, particularly for those with higher... |
PMC8930943 | core_pubmed_pmc | The Effect of Hepatic Impairment on the Pharmacokinetics of Dacomitinib | The Effect of Hepatic Impairment on the Pharmacokinetics of Dacomitinib Abstract Background and Objective Dacomitinib is a kinase inhibitor indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR)-activating mutations. To evaluate... |
PMC9747129 | core_pubmed_pmc | Platelet thromboxane inhibition by low‐dose aspirin in polycythemia vera: Ex vivo and in vivo measurements and in silico simulation | Platelet thromboxane inhibition by low‐dose aspirin in polycythemia vera: Ex vivo and in vivo measurements and in silico simulation Abstract Abstract Low‐dose aspirin is currently recommended for patients with polycythemia vera (PV), a myeloproliferative neoplasm with increased risk of arterial and venous thromboses. B... |
PMC8491459 | core_pubmed_pmc | The use of GA‐RxODE (Genetics Algorithms and Running simulations from Ordinary Differential Equations‐based model) method to optimize bioequivalence studies | The use of GA‐RxODE (Genetics Algorithms and Running simulations from Ordinary Differential Equations‐based model) method to optimize bioequivalence studies Abstract Abstract Bioequivalence (BE) studies are prerequisite in generic products approval. Normally, they are quite simple in design and expensive in execution, ... |
PMC9866473 | core_pubmed_pmc | Evaluation of pH-Sensitive Polymeric Micelles Using Citraconic Amide Bonds for the Co-Delivery of Paclitaxel, Etoposide, and Rapamycin | Evaluation of pH-Sensitive Polymeric Micelles Using Citraconic Amide Bonds for the Co-Delivery of Paclitaxel, Etoposide, and Rapamycin Abstract Paclitaxel (PTX), etoposide (ETP), and rapamycin (RAPA) have different mechanisms, allowing multiple pathways to be targeted simultaneously, effectively treating various cancer... |
PMC10954986 | core_pubmed_pmc | A Population Pharmacokinetic Analysis of l -Glutamine Exposure in Patients with Sickle Cell Disease: Evaluation of Dose and Food Effects | A Population Pharmacokinetic Analysis of l -Glutamine Exposure in Patients with Sickle Cell Disease: Evaluation of Dose and Food Effects Abstract Background and Objective l -Glutamine is a treatment for children and adults with sickle cell disease. A comprehensive evaluation of the pharmacokinetics of l -glutamine in s... |
PMC8176130 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic interaction of Rosuvastatin calcium with guggulipid extract in rats | Pharmacokinetic and pharmacodynamic interaction of Rosuvastatin calcium with guggulipid extract in rats Abstract Abstract Background & objectives Rosuvastatin calcium (RC) is a potent and competitive synthetic inhibitor of HMG-CoA reductase used for the treatment of dyslipidemia. Guggulipid obtained from Commiphora muk... |
PMC10156102 | core_pubmed_pmc | Development and application of a thin‐film molecularly imprinted polymer for the measurement of mycophenolic acid in human plasma | Development and application of a thin‐film molecularly imprinted polymer for the measurement of mycophenolic acid in human plasma Abstract Abstract Background Mycophenolic acid (MPA) is used to suppress the immune response following organ transplantation; however, complex pharmacokinetic behavior and a large interperso... |
PMC12905065 | core_pubmed_pmc | Recombinant von Willebrand factor for von Willebrand disease: mechanism of action and clinical application | Recombinant von Willebrand factor for von Willebrand disease: mechanism of action and clinical application Abstract Abstract Von Willebrand disease (VWD) is an inherited bleeding disorder resulting from a deficiency in von Willebrand factor (VWF), either quantitative or qualitative. Recombinant VWF (rVWF) presents a no... |
PMC11988044 | core_pubmed_pmc | Development and Validation of an LC–MS/MS Method for Quantifying Gabapentin in Plasma: Application to a Pharmacokinetic Study in Cats | Development and Validation of an LC–MS/MS Method for Quantifying Gabapentin in Plasma: Application to a Pharmacokinetic Study in Cats Abstract Simple Summary Gabapentin is an analogue of the neurotransmitter γ-aminobutyric acid, which is commonly used to treat neuropathic pain and epilepsy. However, studies have shown ... |
PMC12571643 | core_pubmed_pmc | Challenges in Extrapolating Healthy Volunteer Pharmacokinetics to Oncology Populations: Advocating for a Holistic Perspective | Challenges in Extrapolating Healthy Volunteer Pharmacokinetics to Oncology Populations: Advocating for a Holistic Perspective Abstract ABSTRACT Phase I clinical pharmacology (CP) studies in healthy volunteers (HVs) are conducted to assess factors influencing drug pharmacokinetic (PK) properties and guide potential dose... |
PMC7813200 | core_pubmed_pmc | A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis | A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis Abstract Abstract Background Glioma is sensitive to microtubule-targeting agents (MTAs), but most MTAs do not cross the blood brain barrier (BBB). To address this limitation, we developed the new chemical entity, ST-401, a bra... |
PMC7288058 | core_pubmed_pmc | Modulating the Properties of Fe(III) Macrocyclic MRI Contrast Agents by Appending Sulfonate or Hydroxyl Groups | Modulating the Properties of Fe(III) Macrocyclic MRI Contrast Agents by Appending Sulfonate or Hydroxyl Groups Abstract Abstract Complexes of Fe(III) that contain a triazacyclononane (TACN) macrocycle, two pendant hydroxyl groups, and a third ancillary pendant show promise as MRI contrast agents. The ancillary group pl... |
PMC10182103 | core_pubmed_pmc | Mechanistic Pharmacokinetic/Pharmacodynamic Modeling in Support of a Patient-Convenient, Longer Dosing Interval for Carfilzomib, a Covalent Inhibitor of the Proteasome | Mechanistic Pharmacokinetic/Pharmacodynamic Modeling in Support of a Patient-Convenient, Longer Dosing Interval for Carfilzomib, a Covalent Inhibitor of the Proteasome Abstract Abstract Background Carfilzomib is an irreversible second-generation proteasome inhibitor that has a short elimination half-life but much longe... |
PMC9426668 | core_pubmed_pmc | Pharmacokinetics, Safety and Efficacy of Intravenous Vedolizumab in Paediatric Patients with Ulcerative Colitis or Crohn’s Disease: Results from the Phase 2 HUBBLE Study | Pharmacokinetics, Safety and Efficacy of Intravenous Vedolizumab in Paediatric Patients with Ulcerative Colitis or Crohn’s Disease: Results from the Phase 2 HUBBLE Study Abstract Abstract Background and Aims To date, there are no systematic pharmacokinetic [PK] data on vedolizumab in paediatric inflammatory bowel disea... |
PMC7046625 | core_pubmed_pmc | Pharmacokinetics of Intravenous and Oral Phenobarbital Sodium in Healthy Goats | Pharmacokinetics of Intravenous and Oral Phenobarbital Sodium in Healthy Goats Abstract Abstract Phenobarbital is a common drug used to manage epilepsy in goats. However, the recommended dose and dosing frequency are based on studies in dogs and horses. Studies describing the pharmacokinetics of phenobarbital when admi... |
PMC11862783 | core_pubmed_pmc | External evaluation of intravenous vancomycin population pharmacokinetic models in adults receiving high‐flux intermittent haemodialysis | External evaluation of intravenous vancomycin population pharmacokinetic models in adults receiving high‐flux intermittent haemodialysis Abstract Abstract Aims Patients undergoing haemodialysis (HD) are at greater risk of methicillin‐resistant Staphylococcus aureus infections requiring intravenous vancomycin. Close van... |
PMC2941486 | core_pubmed_pmc | Evidence of d -phenylglycine as delivering tool for improving l -dopa absorption | Evidence of d -phenylglycine as delivering tool for improving l -dopa absorption Abstract Background l -Dopa has been used for Parkinson's disease management for a long time. However, its wide variety in the rate and the extent of absorption remained challenge in designing suitable therapeutic regime. We report here a ... |
PMC3432792 | core_pubmed_pmc | Eribulin mesylate in patients with refractory cancers: a Phase I study | Eribulin mesylate in patients with refractory cancers: a Phase I study Abstract Summary Eribulin mesylate (Halaven™, E7389) is a synthetic analog of the marine natural product halichondrin B that acts via a mechanism distinct from conventional tubulin-targeted agents. This Phase I study (clinicaltrials.gov identifier: ... |
PMC6600332 | core_pubmed_pmc | Liquid Chromatography-Tandem Mass Spectrometry of Desoxo-Narchinol a and Its Pharmacokinetics and Oral Bioavailability in Rats and Mice | Liquid Chromatography-Tandem Mass Spectrometry of Desoxo-Narchinol a and Its Pharmacokinetics and Oral Bioavailability in Rats and Mice Abstract Desoxo-narchinol A is one of the major active constituents from Nardostachys jatamansi , which has been reported to possess various pharmacological activities, including anti-... |
PMC4648969 | core_pubmed_pmc | Phase I and pharmacological trial of lapatinib in combination with gemcitabine in patients with advanced breast cancer | Phase I and pharmacological trial of lapatinib in combination with gemcitabine in patients with advanced breast cancer Abstract Summary Background Lapatinib has proven efficacy as monotherapy and in combination with capecitabine in patients with metastatic breast cancer (MBC) overexpressing HER2 and/or EGFR. Gemcitabin... |
PMC10507879 | core_pubmed_pmc | Knowledge, attitude and perceptions of pharmacists regarding renal dose adjustment among chronic kidney disease patients in Pakistan | Knowledge, attitude and perceptions of pharmacists regarding renal dose adjustment among chronic kidney disease patients in Pakistan Abstract Abstract Background Chronic kidney disease (CKD) poses a significant public health challenge. CKD patients have compromised renal function, which not only alters the pharmacokine... |
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