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PMC5683800 | core_pubmed_pmc | Use of ceftolozane-tazobactam in a cystic fibrosis patient with multidrug-resistant pseudomonas infection and renal insufficiency | Use of ceftolozane-tazobactam in a cystic fibrosis patient with multidrug-resistant pseudomonas infection and renal insufficiency Abstract We report the successful use of ceftolozane/tazobactam (C/T) to treat a pulmonary exacerbation in a 35 year old female, post lung transplant, with cystic fibrosis (CF), malnutrition... |
PMC7965839 | core_pubmed_pmc | Pharmacodynamic analysis of hypertension caused by lenvatinib using real‐world postmarketing surveillance data | Pharmacodynamic analysis of hypertension caused by lenvatinib using real‐world postmarketing surveillance data Abstract Abstract Lenvatinib is a tyrosine kinase inhibitor of the vascular endothelial growth factor receptor used against nonoperative thyroid cancer; however, hypertension is a major dose‐limiting side effe... |
PMC10163150 | core_pubmed_pmc | First-in-human, phase I study of AK109, an anti-VEGFR2 antibody in patients with advanced or metastatic solid tumors | First-in-human, phase I study of AK109, an anti-VEGFR2 antibody in patients with advanced or metastatic solid tumors Abstract Background Vascular endothelial growth factor receptor 2 (VEGFR2) plays a key role in antiangiogenesis which has been an essential strategy for cancer treatment. We report the first-in-human stu... |
PMC9438944 | core_pubmed_pmc | An ACE2-IgG4 Fc Fusion Protein Demonstrates Strong Binding to All Tested SARS-CoV-2 Variants and Reduced Lung Inflammation in Animal Models of SARS-CoV-2 and Influenza | An ACE2-IgG4 Fc Fusion Protein Demonstrates Strong Binding to All Tested SARS-CoV-2 Variants and Reduced Lung Inflammation in Animal Models of SARS-CoV-2 and Influenza Abstract Background: The continued emergence of SARS-CoV-2 variants has caused concern that a constantly evolving virus will escape vaccines and antibod... |
PMC9292343 | core_pubmed_pmc | Use of oral tetracyclines in the treatment of adult outpatients with skin and skin structure infections: Focus on doxycycline, minocycline, and omadacycline | Use of oral tetracyclines in the treatment of adult outpatients with skin and skin structure infections: Focus on doxycycline, minocycline, and omadacycline Abstract Abstract Oral tetracyclines have been used in clinical practice for over 60 years. One of the most common indications for use of oral tetracyclines is for... |
PMC3808212 | core_pubmed_pmc | High-efficiency liposomal encapsulation of a tyrosine kinase inhibitor leads to improved in vivo toxicity and tumor response profile | High-efficiency liposomal encapsulation of a tyrosine kinase inhibitor leads to improved in vivo toxicity and tumor response profile Abstract Abstract Staurosporine (STS) is a potent pan-kinase inhibitor with marked activity against several chemotherapy-resistant tumor types in vitro. The translational progress of this... |
PMC5599463 | core_pubmed_pmc | PK/PD studies on non-selective PDE inhibitors in rats using cAMP as a marker of pharmacological response | PK/PD studies on non-selective PDE inhibitors in rats using cAMP as a marker of pharmacological response Abstract In recent years, phosphodiesterase (PDE) inhibitors have been frequently tested for the treatment of experimental inflammatory and immune disorders. It is suggested that anti-inflammatory properties of PDE ... |
PMC6930861 | core_pubmed_pmc | Quantitative Systems Pharmacology and Physiologically‐Based Pharmacokinetic Modeling With mrgsolve: A Hands‐On Tutorial | Quantitative Systems Pharmacology and Physiologically‐Based Pharmacokinetic Modeling With mrgsolve: A Hands‐On Tutorial Abstract mrgsolve is an open‐source R package available on the Comprehensive R Archive Network. It combines R and C++ coding for simulation from hierarchical, ordinary differential equation–based mode... |
PMC10053229 | core_pubmed_pmc | Clinical Predictors and Prediction Models for rFVIII-Fc Half Life in Real-World People with Severe Hemophilia A | Clinical Predictors and Prediction Models for rFVIII-Fc Half Life in Real-World People with Severe Hemophilia A Abstract The half life of recombinant factor VIII-Fc (rFVIII-Fc) for people with hemophilia A (PwHA) varies greatly. Understanding the factors influencing the variation and assessment of rFVIII-Fc half life i... |
PMC10716197 | core_pubmed_pmc | In silico studies on cytotoxicity and antitumoral activity of acetogenins from Annona muricata L | In silico studies on cytotoxicity and antitumoral activity of acetogenins from Annona muricata L Abstract As life expectancy increases, the number of people affected by cancer is increasing. The available drugs still cause several adverse reactions, and it is important to look for less toxic drugs that act on resistant... |
PMC9293315 | core_pubmed_pmc | Comparison of tissue pharmacokinetics of esflurbiprofen plaster with flurbiprofen tablets in patients with knee osteoarthritis: A multicenter randomized controlled trial | Comparison of tissue pharmacokinetics of esflurbiprofen plaster with flurbiprofen tablets in patients with knee osteoarthritis: A multicenter randomized controlled trial Abstract Abstract This open‐label, multicenter, prospective, randomized controlled trial aimed to determine the effectiveness of esflurbiprofen plaste... |
PMC5814678 | core_pubmed_pmc | LC–MS/MS method for simultaneous determination of diethylcarbamazine, albendazole and albendazole metabolites in human plasma: Application to a clinical pharmacokinetic study | LC–MS/MS method for simultaneous determination of diethylcarbamazine, albendazole and albendazole metabolites in human plasma: Application to a clinical pharmacokinetic study Abstract Highlights • The first LC–MS/MS method of diethylcarbamazine and albendazole along with its active metabolites. • The method was success... |
PMC10162880 | core_pubmed_pmc | The Clinical Application and Progress of Mirogabalin on Neuropathic Pain as a Novel Selective Gabapentinoids | The Clinical Application and Progress of Mirogabalin on Neuropathic Pain as a Novel Selective Gabapentinoids Abstract Background Neuropathic pain is a complex sort of pain that is detrimental to individuals' health, both physically and mentally, but merely a small portion of them could witness pain alleviation. Mirogab... |
PMC5286781 | core_pubmed_pmc | Severe toxicity induced by accumulation of active sunitinib metabolite in a Japanese patient with renal cell carcinoma: a case report | Severe toxicity induced by accumulation of active sunitinib metabolite in a Japanese patient with renal cell carcinoma: a case report Abstract Background Sunitinib is a multi-targeted tyrosine kinase inhibitor that is approved for treatment of renal cell carcinoma as an oral anticancer drug. Therapeutic drug monitoring... |
PMC4940002 | core_pubmed_pmc | The effects of ferulic acid on the pharmacokinetics of warfarin in rats after biliary drainage | The effects of ferulic acid on the pharmacokinetics of warfarin in rats after biliary drainage Abstract Abstract According to previous research studies, warfarin can be detected in human bile after oral administration. Ferulic acid (FA) is the main bioactive component of many Chinese herbs for the treatment of cardiova... |
PMC4156782 | core_pubmed_pmc | A Review of the Pharmacological Properties of Insulin Degludec and Their Clinical Relevance | A Review of the Pharmacological Properties of Insulin Degludec and Their Clinical Relevance Abstract Insulin degludec (IDeg) is a new-generation basal insulin with an ultra-long duration of action. To date, a large number of studies have been conducted to investigate the pharmacokinetic and pharmacodynamic properties o... |
PMC9611936 | core_pubmed_pmc | Implementation and Cross-Validation of a Pharmacokinetic Model for Precision Dosing of Busulfan in Hematopoietic Stem Cell Transplanted Children | Implementation and Cross-Validation of a Pharmacokinetic Model for Precision Dosing of Busulfan in Hematopoietic Stem Cell Transplanted Children Abstract Abstract Busulfan, a drug used in conditioning prior to hematopoietic stem cell transplantation (HSCT) in children, has a narrow therapeutic margin. The model-informe... |
PMC3394719 | core_pubmed_pmc | Anti-Tumour Effects of a Specific Anti-ADAM17 Antibody in an Ovarian Cancer Model In Vivo | Anti-Tumour Effects of a Specific Anti-ADAM17 Antibody in an Ovarian Cancer Model In Vivo Abstract ADAM 17 (TNF-α converting enzyme, TACE) is a potential target for cancer therapy, but the small molecule inhibitors reported to date are not specific to this ADAM family member. This membrane-bound metalloproteinase is re... |
PMC3832545 | core_pubmed_pmc | Treatment with Insulin Analog X10 and IGF-1 Increases Growth of Colon Cancer Allografts | Treatment with Insulin Analog X10 and IGF-1 Increases Growth of Colon Cancer Allografts Abstract Abstract Obesity and type 2 diabetes are associated with an increased risk for development of certain forms of cancer, including colon cancer. The publication of highly controversial epidemiological studies in 2009 raised t... |
PMC11280076 | core_pubmed_pmc | Clinical Ocular Exposure Extrapolation for a Complex Ophthalmic Suspension Using Physiologically Based Pharmacokinetic Modeling and Simulation | Clinical Ocular Exposure Extrapolation for a Complex Ophthalmic Suspension Using Physiologically Based Pharmacokinetic Modeling and Simulation Abstract The development of generic ophthalmic drug products with complex formulations is challenging due to the complexity of the ocular system and a lack of sensitive testing ... |
PMC12114300 | core_pubmed_pmc | Development of a Population Pharmacokinetic Model of Levofloxacin in Healthy Adults and Identification of Optimal Dosing Regimens | Development of a Population Pharmacokinetic Model of Levofloxacin in Healthy Adults and Identification of Optimal Dosing Regimens Abstract Abstract Background/Objectives : Levofloxacin dosing guidelines recommend adjustments only when the creatinine clearance (CrCl) is <50 mL/min. We hypothesized that further dose stra... |
PMC11652601 | core_pubmed_pmc | Model-informed precision dosing of quetiapine in bipolar affective disorder patients: initial dose recommendation | Model-informed precision dosing of quetiapine in bipolar affective disorder patients: initial dose recommendation Abstract Abstract Objective Bipolar affective disorder (BAD) is a mood disorder with high morbidity and mortality. Quetiapine can be used in the treatment of patients with BAD; however, the precise administ... |
PMC6220787 | core_pubmed_pmc | A Prospective Randomized, Double‐Blind, Two‐Period Crossover Pharmacokinetic Trial Comparing Green Coffee Bean Extract—A Botanically Sourced Caffeine—With a Synthetic USP Control | A Prospective Randomized, Double‐Blind, Two‐Period Crossover Pharmacokinetic Trial Comparing Green Coffee Bean Extract—A Botanically Sourced Caffeine—With a Synthetic USP Control Abstract Abstract Coffee is a primary dietary source of the chlorogenic acids (CGAs) of phenolic compounds. Coffee contains caffeine and othe... |
PMC6649305 | core_pubmed_pmc | The effect of surface treatment on the brain delivery of curcumin nanosuspension: in vitro and in vivo studies | The effect of surface treatment on the brain delivery of curcumin nanosuspension: in vitro and in vivo studies Abstract Abstract Background: Curcumin, a bioactive component with multiple characteristics, has been shown to have many therapeutic effects. However, there are several limitations regarding the use of curcumi... |
PMC12665186 | core_pubmed_pmc | Building a Beta‐Lactam Model‐Informed Precision Dosing Service in a Quaternary Care Children's Hospital | Building a Beta‐Lactam Model‐Informed Precision Dosing Service in a Quaternary Care Children's Hospital Abstract ABSTRACT There has been growing interest in precision dosing of beta‐lactam antibiotics in recent years. At our institution, a quaternary children's hospital, we launched a new PK consult service utilizing a... |
PMC6180848 | core_pubmed_pmc | Pharmacokinetic Analysis of Propofol Target-Controlled Infusion Models in Chinese Patients with Hepatic Insufficiency | Pharmacokinetic Analysis of Propofol Target-Controlled Infusion Models in Chinese Patients with Hepatic Insufficiency Abstract Abstract Background Effects of liver dysfunction on target-controlled infusion (TCI) with Marsh parameters of propofol remain poorly documented. The purpose of this study was to evaluate the pe... |
PMC4260001 | core_pubmed_pmc | Linking the Population Pharmacokinetics of Tenofovir and Its Metabolites With Its Cellular Uptake and Metabolism | Linking the Population Pharmacokinetics of Tenofovir and Its Metabolites With Its Cellular Uptake and Metabolism Abstract Empirical pharmacokinetic models are used to explain the pharmacokinetics of the antiviral drug tenofovir (TFV) and its metabolite TFV diphosphate (TFV-DP) in peripheral blood mononuclear cells. The... |
PMC9292235 | core_pubmed_pmc | Pharmacokinetics and Metabolism of Ziritaxestat (GLPG1690) in Healthy Male Volunteers Following Intravenous and Oral Administration | Pharmacokinetics and Metabolism of Ziritaxestat (GLPG1690) in Healthy Male Volunteers Following Intravenous and Oral Administration Abstract Abstract Ziritaxestat is a novel inhibitor of autotaxin, an enzyme responsible for the production of lysophosphatidic acid, the downstream signaling of which mediates responses to... |
PMC5351411 | core_pubmed_pmc | Prediction of in vivo and in vitro infection model results using a semimechanistic model of avibactam and aztreonam combination against multidrug resistant organisms | Prediction of in vivo and in vitro infection model results using a semimechanistic model of avibactam and aztreonam combination against multidrug resistant organisms Abstract Abstract The combination of aztreonam‐avibactam is active against multidrug‐resistant Enterobacteriaceae that express metallo‐β‐lactamases. A com... |
PMC4007625 | core_pubmed_pmc | A phase I study of AST1306, a novel irreversible EGFR and HER2 kinase inhibitor, in patients with advanced solid tumors | A phase I study of AST1306, a novel irreversible EGFR and HER2 kinase inhibitor, in patients with advanced solid tumors Abstract Abstract Background AST1306 is an orally active irreversible small molecule inhibitor of EGFR (erbB1), HER2 (erbB2) and HER4 (erbB4) signaling. This is a phase I, open-label, dose-escalation ... |
PMC12540684 | core_pubmed_pmc | Central composite design optimized fluorescent method using dual doped graphene quantum dots for lacosamide determination in biological samples | Central composite design optimized fluorescent method using dual doped graphene quantum dots for lacosamide determination in biological samples Abstract Abstract Lacosamide is a third-generation antiepileptic drug used for the treatment of partial-onset seizures. This study investigates the development and validation o... |
PMC9835899 | core_pubmed_pmc | Pharmacokinetic and clinical comparison of super-bioavailable itraconazole and conventional itraconazole at different dosing in dermatophytosis | Pharmacokinetic and clinical comparison of super-bioavailable itraconazole and conventional itraconazole at different dosing in dermatophytosis Abstract Background Due to changing face of dermatophytosis in India, many dermatologists practice different dosing patterns of itraconazole (ITZ). Recently, a new form of ITZ,... |
PMC8275874 | core_pubmed_pmc | The Population Pharmacokinetics of Meropenem in Adult Patients With Rifampicin-Sensitive Pulmonary Tuberculosis | The Population Pharmacokinetics of Meropenem in Adult Patients With Rifampicin-Sensitive Pulmonary Tuberculosis Abstract Background: Meropenem is being investigated for repurposing as an anti-tuberculosis drug. This study aimed to develop a meropenem population pharmacokinetics model in patients with pulmonary tubercul... |
PMC11762053 | core_pubmed_pmc | Clinical Pharmacokinetics of Atogepant in Healthy Japanese and White Adults | Clinical Pharmacokinetics of Atogepant in Healthy Japanese and White Adults Abstract Introduction Atogepant is a calcitonin gene-related peptide receptor antagonist approved for the preventive treatment of migraine in adults in the USA, EU, and several other countries. The objectives of this study were to evaluate the ... |
PMC12786477 | core_pubmed_pmc | Subcutaneous Estradiol Pellets as Hormone Therapy in Menopause: Clinical Pharmacology, Patient Selection and Safety Considerations | Subcutaneous Estradiol Pellets as Hormone Therapy in Menopause: Clinical Pharmacology, Patient Selection and Safety Considerations Abstract Background: Among hormone therapy options for menopause, subcutaneous estradiol pellets offer sustained hormone release, avoid first-pass hepatic metabolism, and maintain a near-ph... |
PMC12232731 | core_pubmed_pmc | Phase 1 trial of HR070803 (an Irinotecan liposome) in combination with 5-fluorouracil, leucovorin, and oxaliplatin for untreated advanced or metastatic pancreatic ductal adenocarcinoma | Phase 1 trial of HR070803 (an Irinotecan liposome) in combination with 5-fluorouracil, leucovorin, and oxaliplatin for untreated advanced or metastatic pancreatic ductal adenocarcinoma Abstract Abstract Background This study assessed the safety, preliminary antitumor activity, and pharmacokinetics of HR070803 (a novel ... |
PMC12310911 | core_pubmed_pmc | An investigation of extended-interval dosing of atezolizumab in Japanese patients with advanced solid tumors: safety and pharmacokinetics of a dose of 1680 mg every 4 weeks | An investigation of extended-interval dosing of atezolizumab in Japanese patients with advanced solid tumors: safety and pharmacokinetics of a dose of 1680 mg every 4 weeks Abstract Abstract In Japan, atezolizumab is indicated for several cancers at a dose of 1200 mg every 3 weeks or 840 mg every 2 weeks. This open-lab... |
PMC12709141 | core_pubmed_pmc | Clinical and Biochemical Factors Associated With Infliximab Pharmacokinetics in Adult Patients With Inflammatory Bowel Disease | Clinical and Biochemical Factors Associated With Infliximab Pharmacokinetics in Adult Patients With Inflammatory Bowel Disease Abstract Abstract Many patients with inflammatory bowel disease (IBD) do not adequately respond to infliximab, potentially due to individual differences in pharmacokinetics (PK). This study aim... |
PMC8781607 | core_pubmed_pmc | Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids | Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids Abstract This study aimed to optimize and evaluate self-assembled liquid crystalline nanoparticles (SALCs) prepared from phospholipids and oleic acid for enhancing the absorption of Ω-3s. We ... |
PMC6373391 | core_pubmed_pmc | Long-Term Efficacy and Safety of Biosimilar CT-P10 Versus Innovator Rituximab in Rheumatoid Arthritis: 48-Week Results from a Randomized Phase III Trial | Long-Term Efficacy and Safety of Biosimilar CT-P10 Versus Innovator Rituximab in Rheumatoid Arthritis: 48-Week Results from a Randomized Phase III Trial Abstract Objective The aim of this study was to investigate long-term clinical outcomes of extended treatment with CT-P10, a rituximab biosimilar, compared with rituxi... |
PMC12347391 | core_pubmed_pmc | Sulforaphane-Rich Broccoli Sprout Extract Promotes Hair Regrowth in an Androgenetic Alopecia Mouse Model via Enhanced Dihydrotestosterone Metabolism | Sulforaphane-Rich Broccoli Sprout Extract Promotes Hair Regrowth in an Androgenetic Alopecia Mouse Model via Enhanced Dihydrotestosterone Metabolism Abstract Androgenetic alopecia (AGA) is a common progressive hair loss disorder driven by elevated dihydrotestosterone (DHT) levels, leading to follicular miniaturization.... |
PMC10142820 | core_pubmed_pmc | Xeomin ® , a Commercial Formulation of Botulinum Neurotoxin Type A, Promotes Regeneration in a Preclinical Model of Spinal Cord Injury | Xeomin ® , a Commercial Formulation of Botulinum Neurotoxin Type A, Promotes Regeneration in a Preclinical Model of Spinal Cord Injury Abstract Xeomin ® is a commercial formulation of botulinum neurotoxin type A (BoNT/A) clinically authorized for treating neurological disorders, such as blepharospasm, cervical dystonia... |
PMC7661247 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia | Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia Abstract Abstract Background Reduction in elevated serum cholesterol concentrations is important in the management of individuals at risk of atherosclerotic cardiovascular disease (ASCVD), such as myocar... |
PMC12162633 | core_pubmed_pmc | Current developments of metal- and metalloid-based quinoline compounds as leishmanicidal agents | Current developments of metal- and metalloid-based quinoline compounds as leishmanicidal agents Abstract The quinoline moiety represents an important scaffold for the development of leishmanicidal agents. In particular, its hybridization with metal/metalloids has generated highly active compounds that are, in some case... |
PMC9029538 | core_pubmed_pmc | Dosing Colistimethate Every 8 h Results in Higher Plasma Concentrations of Active Colistin Than Every 12-Hourly Dosing without Increase in Nephrotoxicity: A Phase 1 Pharmacokinetics Trial in Healthy Adult Volunteers | Dosing Colistimethate Every 8 h Results in Higher Plasma Concentrations of Active Colistin Than Every 12-Hourly Dosing without Increase in Nephrotoxicity: A Phase 1 Pharmacokinetics Trial in Healthy Adult Volunteers Abstract Abstract Despite its use for decades, pharmacokinetic (PK) and safety studies on colistin are l... |
PMC11591545 | core_pubmed_pmc | Model-Based Dose Identification of Dalbavancin for Long-Term Suppressive Outpatient Treatment of Ventricular Assist Device Infections | Model-Based Dose Identification of Dalbavancin for Long-Term Suppressive Outpatient Treatment of Ventricular Assist Device Infections Abstract Abstract Increasing evidence suggests that dalbavancin is an effective long-term treatment for ventricular assist device (VAD) infections, with various prolonged dosing regimens... |
PMC4071174 | core_pubmed_pmc | Modeling of the Parathyroid Hormone Response after Calcium Intake in Healthy Subjects | Modeling of the Parathyroid Hormone Response after Calcium Intake in Healthy Subjects Abstract Abstract Plasma ionized calcium (Ca 2+ ) concentrations are tightly regulated in the body and maintained within a narrow range; thus it is challenging to quantify calcium absorption under normal physiologic conditions. This s... |
PMC4932520 | core_pubmed_pmc | In-vivo absorption of pinocembrin-7- O-β -D-glucoside in rats and its in-vitro biotransformation | In-vivo absorption of pinocembrin-7- O-β -D-glucoside in rats and its in-vitro biotransformation Abstract Abstract Pinocembrin-7- O-β -D-glucoside (PCBG), a flavonoid isolated from Penthorum chinense Pursh., has significant liver-protecting effects. The pharmacokinetics of PCBG and its major metabolite pinocembrin (PCB... |
PMC6694471 | core_pubmed_pmc | A phase 1/2 trial to evaluate the pharmacokinetics, safety, and efficacy of NI-03 in patients with chronic pancreatitis: study protocol for a randomized controlled trial on the assessment of camostat treatment in chronic pancreatitis (TACTIC) | A phase 1/2 trial to evaluate the pharmacokinetics, safety, and efficacy of NI-03 in patients with chronic pancreatitis: study protocol for a randomized controlled trial on the assessment of camostat treatment in chronic pancreatitis (TACTIC) Abstract Abstract Background Chronic pancreatitis (CP) is a progressive, fibr... |
PMC10043346 | core_pubmed_pmc | Evaluation of limited-sampling strategies to calculate AUC (0–24) and the role of CYP3A5 in Chilean pediatric kidney recipients using extended-release tacrolimus | Evaluation of limited-sampling strategies to calculate AUC (0–24) and the role of CYP3A5 in Chilean pediatric kidney recipients using extended-release tacrolimus Abstract Background: Kidney transplantation (KTx) requires immunosuppressive drugs such as Tacrolimus (TAC) which is mainly metabolized by CYP3A5. TAC is rout... |
PMC6337338 | core_pubmed_pmc | Pharmacokinetic and Metabolism Studies of Curculigoside C by UPLC-MS/MS and UPLC-QTOF-MS | Pharmacokinetic and Metabolism Studies of Curculigoside C by UPLC-MS/MS and UPLC-QTOF-MS Abstract Abstract Pharmacokinetic and metabolism studies were carried out on curculigoside C (CC), a natural product with good antioxidant and neuroprotective effects, with the purpose of investigating the effects of the hydroxyl g... |
PMC7255978 | core_pubmed_pmc | First-in-Human, Multicenter, Phase I Dose-Escalation and Expansion Study of Anti-Mesothelin Antibody–Drug Conjugate Anetumab Ravtansine in Advanced or Metastatic Solid Tumors | First-in-Human, Multicenter, Phase I Dose-Escalation and Expansion Study of Anti-Mesothelin Antibody–Drug Conjugate Anetumab Ravtansine in Advanced or Metastatic Solid Tumors Abstract Abstract PURPOSE This phase I study, which to our knowledge is the first-in-human study of this kind, investigates the safety, tolerabil... |
PMC6394644 | core_pubmed_pmc | Pharmacokinetics of Tramadol and Celecoxib in Japanese and Caucasian Subjects Following Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label Study | Pharmacokinetics of Tramadol and Celecoxib in Japanese and Caucasian Subjects Following Administration of Co-Crystal of Tramadol-Celecoxib (CTC): A Randomised, Open-Label Study Abstract Abstract Background and Objectives Co-Crystal of Tramadol-Celecoxib (CTC) is a first-in-class active pharmaceutical ingredient (API–AP... |
PMC5995786 | core_pubmed_pmc | Evaluation of the Pharmacokinetics and Safety of a Single Oral Dose of Fasiglifam in Subjects with Mild or Moderate Hepatic Impairment | Evaluation of the Pharmacokinetics and Safety of a Single Oral Dose of Fasiglifam in Subjects with Mild or Moderate Hepatic Impairment Abstract Abstract Background and Aims Fasiglifam, a potent, selective novel agonist of G protein-coupled receptor 40, stimulates insulin secretion at elevated blood glucose levels in a ... |
PMC5661853 | core_pubmed_pmc | In vivo study of doxorubicin-loaded cell-penetrating peptide-modified pH-sensitive liposomes: biocompatibility, bio-distribution, and pharmacodynamics in BALB/c nude mice bearing human breast tumors | In vivo study of doxorubicin-loaded cell-penetrating peptide-modified pH-sensitive liposomes: biocompatibility, bio-distribution, and pharmacodynamics in BALB/c nude mice bearing human breast tumors Abstract In vivo evaluation of drug delivery vectors is essential for clinical translation. In BALB/c nude mice bearing h... |
PMC11903579 | core_pubmed_pmc | Are contemporary antifungal doses sufficient for critically ill patients? Outcomes from an international, multicenter pharmacokinetics study for Screening Antifungal Exposure in Intensive Care Units—the SAFE-ICU study | Are contemporary antifungal doses sufficient for critically ill patients? Outcomes from an international, multicenter pharmacokinetics study for Screening Antifungal Exposure in Intensive Care Units—the SAFE-ICU study Abstract Abstract Purpose Appropriate antifungal therapy is a major determinant of survival in critica... |
PMC10122531 | core_pubmed_pmc | The Impact of Medical Nutritional Therapy on the Efficacy of Premix Insulin in Glycemic Control in Patients with Type 2 Diabetes | The Impact of Medical Nutritional Therapy on the Efficacy of Premix Insulin in Glycemic Control in Patients with Type 2 Diabetes Abstract Background: Medical nutritional therapy (MNT) is a key component in the treatment of Diabetes mellitus (DM). MNT is completely individual and should be present in the treatment of di... |
PMC9546317 | core_pubmed_pmc | Medication control of flunixin in racing horses: Possible detection times using Monte Carlo simulations | Medication control of flunixin in racing horses: Possible detection times using Monte Carlo simulations Abstract Summary Background For medication control in several jurisdictions, withdrawal time is the period of refrain from racing after drug administration. It is set by adding a safety period to an experimental dete... |
PMC3730214 | core_pubmed_pmc | Pharmacokinetic Properties and Systemic Safety of Vancomycin-Impregnated Cancellous Bone Grafts in the Treatment of Spondylodiscitis | Pharmacokinetic Properties and Systemic Safety of Vancomycin-Impregnated Cancellous Bone Grafts in the Treatment of Spondylodiscitis Abstract The aim of the present study was to investigate the local pharmacokinetic properties and the systemic safety of vancomycin-impregnated cancellous bone grafts in the treatment of ... |
PMC9219738 | core_pubmed_pmc | A Critical Review of the Pharmacokinetics, Pharmacodynamics, and Safety Data of Antibiotics in Avian Species | A Critical Review of the Pharmacokinetics, Pharmacodynamics, and Safety Data of Antibiotics in Avian Species Abstract In avian medicine, the use of antibiotic dosing regimens based on species-specific pharmacological studies is ideal. However, due to a lack of such studies, dose extrapolation, which may cause inefficac... |
PMC4862506 | core_pubmed_pmc | Incorporating Stage-Specific Drug Action into Pharmacological Modeling of Antimalarial Drug Treatment | Incorporating Stage-Specific Drug Action into Pharmacological Modeling of Antimalarial Drug Treatment Abstract Abstract Pharmacological modeling of antiparasitic treatment based on a drug's pharmacokinetic and pharmacodynamic properties plays an increasingly important role in identifying optimal drug dosing regimens an... |
PMC6924018 | core_pubmed_pmc | Pharmacodynamics of Pre-Operative PD1 checkpoint blockade and receptor activator of NFkB ligand (RANKL) inhibition in non-small cell lung cancer (NSCLC): study protocol for a multicentre, open-label, phase 1B/2, translational trial (POPCORN) | Pharmacodynamics of Pre-Operative PD1 checkpoint blockade and receptor activator of NFkB ligand (RANKL) inhibition in non-small cell lung cancer (NSCLC): study protocol for a multicentre, open-label, phase 1B/2, translational trial (POPCORN) Abstract Abstract Background Neoadjuvant immunotherapy targeting immune checkp... |
PMC4637958 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic profiling of imipenem in patients admitted to an intensive care unit in India: A nonrandomized, cross-sectional, analytical, open-labeled study | Pharmacokinetic/pharmacodynamic profiling of imipenem in patients admitted to an intensive care unit in India: A nonrandomized, cross-sectional, analytical, open-labeled study Abstract Abstract Background and Aim: Widespread use of imipenem in intensive care units (ICUs) in India has led to the development of numerous ... |
PMC12484410 | core_pubmed_pmc | A Physiologically Based Modeling Approach to Evaluate Intravenous Levetiracetam Dosing in Term and Preterm Neonates | A Physiologically Based Modeling Approach to Evaluate Intravenous Levetiracetam Dosing in Term and Preterm Neonates Abstract Abstract Seizures are the most common neurologic emergency in neonates and are associated with significant morbidity and mortality. Current first‐line pharmacotherapy, phenobarbital, is associate... |
PMC4997829 | core_pubmed_pmc | Wild-Type and Non-Wild-Type Mycobacterium tuberculosis MIC Distributions for the Novel Fluoroquinolone Antofloxacin Compared with Those for Ofloxacin, Levofloxacin, and Moxifloxacin | Wild-Type and Non-Wild-Type Mycobacterium tuberculosis MIC Distributions for the Novel Fluoroquinolone Antofloxacin Compared with Those for Ofloxacin, Levofloxacin, and Moxifloxacin Abstract Antofloxacin (AFX) is a novel fluoroquinolone that has been approved in China for the treatment of infections caused by a variety... |
PMC12569551 | core_pubmed_pmc | Probability of pharmacokinetic/pharmacodynamic target attainment for different piperacillin/tazobactam dosing regimens in renally impaired patients in a non‐intensive care unit setting | Probability of pharmacokinetic/pharmacodynamic target attainment for different piperacillin/tazobactam dosing regimens in renally impaired patients in a non‐intensive care unit setting Abstract Aims To optimize antibiotic therapy for pathogens classified as susceptible, increased exposure (I) , an increased exposure of... |
PMC3409367 | core_pubmed_pmc | A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer | A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer Abstract Abstract Afatinib (BIBW 2992) is an ErbB-family blocker that irreversibly inhibits signaling from all relevant ErbB-family dimers. Afatinib has demonstrated preclinical acti... |
PMC6479204 | core_pubmed_pmc | Pre-clinical Safety and Efficacy of Lentiviral Vector-Mediated Ex Vivo Stem Cell Gene Therapy for the Treatment of Mucopolysaccharidosis IIIA | Pre-clinical Safety and Efficacy of Lentiviral Vector-Mediated Ex Vivo Stem Cell Gene Therapy for the Treatment of Mucopolysaccharidosis IIIA Abstract Hematopoietic stem cell gene therapy is a promising therapeutic strategy for the treatment of neurological disorders, since transplanted gene-corrected cells can traffic... |
PMC12196159 | core_pubmed_pmc | Ferulic Acid as an Anti-Inflammatory Agent: Insights into Molecular Mechanisms, Pharmacokinetics and Applications | Ferulic Acid as an Anti-Inflammatory Agent: Insights into Molecular Mechanisms, Pharmacokinetics and Applications Abstract Abstract Ferulic acid (FA), a hydroxycinnamic acid derivative, is a key bioactive component in traditional medicinal plants including Angelica sinensis and Asafoetida . Accumulating evidence suppor... |
PMC11235173 | core_pubmed_pmc | Clickable tryptophan modification for late-stage diversification of native peptides | Clickable tryptophan modification for late-stage diversification of native peptides Abstract Abstract As the least abundant residue in proteins, tryptophan widely exists in peptide drugs and bioactive natural products and contributes to drug-target interactions in multiple ways. We report here a clickable tryptophan mo... |
PMC10135111 | core_pubmed_pmc | Novel Antimicrobial Agents for Gram-Negative Pathogens | Novel Antimicrobial Agents for Gram-Negative Pathogens Abstract Abstract Gram-negative bacterial resistance to antimicrobials has had an exponential increase at a global level during the last decades and represent an everyday challenge, especially for the hospital practice of our era. Concerted efforts from the researc... |
PMC7937587 | core_pubmed_pmc | Effect of Food on the Pharmacokinetics of the Oral Docetaxel Tablet Formulation ModraDoc006 Combined with Ritonavir (ModraDoc006/r) in Patients with Advanced Solid Tumours | Effect of Food on the Pharmacokinetics of the Oral Docetaxel Tablet Formulation ModraDoc006 Combined with Ritonavir (ModraDoc006/r) in Patients with Advanced Solid Tumours Abstract Introduction ModraDoc006 is a novel docetaxel tablet formulation that is co-administrated with the cytochrome P450 3A4 and P-glycoprotein i... |
PMC8774130 | core_pubmed_pmc | Intra-Arterial Infusion Chemotherapy in Advanced Pancreatic Cancer: A Comprehensive Review | Intra-Arterial Infusion Chemotherapy in Advanced Pancreatic Cancer: A Comprehensive Review Abstract Simple Summary Pancreatic cancer has a very poor prognosis. The few available therapeutic options are characterized by low efficacy and high toxicity due to the intrinsic chemoresistance of this tumor type. To improve cl... |
PMC7605631 | core_pubmed_pmc | Intracellular Distribution of Lipids and Encapsulated Model Drugs from Cationic Liposomes with Different Uptake Pathways | Intracellular Distribution of Lipids and Encapsulated Model Drugs from Cationic Liposomes with Different Uptake Pathways Abstract Aim The uptake pathway of liposomes into cells is mainly via endocytosis or membrane fusion; however, the relationship between the uptake pathway and the intracellular pharmacokinetics of th... |
PMC12296649 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Two Formulations of Apixaban Tablets: A Double-Blind, Single-Dose, Crossover Study in Healthy Subjects | Pharmacokinetics and Bioequivalence of Two Formulations of Apixaban Tablets: A Double-Blind, Single-Dose, Crossover Study in Healthy Subjects Abstract Background The present study aimed to determine the pharmacokinetic parameters and bioequivalence of the test medicinal product, apixaban 5 mg tablet, and its reference ... |
PMC8005605 | core_pubmed_pmc | Population Pharmacokinetic Study of Cefathiamidine in Infants With Augmented Renal Clearance | Population Pharmacokinetic Study of Cefathiamidine in Infants With Augmented Renal Clearance Abstract Abstract Objectives: Augmented renal clearance (ARC) of primarily renally eliminated antibacterial agents may result in subtherapeutic antibiotic concentrations and, as a consequence, worse clinical outcomes. Cefathiam... |
PMC7587338 | core_pubmed_pmc | Determination of Lekethromycin, a Novel Macrolide Lactone, in Rat Plasma by UPLC-MS/MS and Its Application to a Pharmacokinetic Study | Determination of Lekethromycin, a Novel Macrolide Lactone, in Rat Plasma by UPLC-MS/MS and Its Application to a Pharmacokinetic Study Abstract Lekethromycin, a new macrolide lactone, exhibits significant antibacterial activity. In this study, a reliable analytical ultrahigh-performance liquid chromatography electrospra... |
PMC9412264 | core_pubmed_pmc | Relationship between Pharmacokinetic/Pharmacodynamic Target Attainment and Microbiological Outcome in Critically Ill COVID-19 Patients with Documented Gram-Negative Superinfections Treated with TDM-Guided Continuous-Infusion Meropenem | Relationship between Pharmacokinetic/Pharmacodynamic Target Attainment and Microbiological Outcome in Critically Ill COVID-19 Patients with Documented Gram-Negative Superinfections Treated with TDM-Guided Continuous-Infusion Meropenem Abstract Objectives: The objective of this study was to explore the relationship betw... |
PMC4884413 | core_pubmed_pmc | In vivo therapeutic efficacy and pharmacokinetics of colistin sulfate in an experimental model of enterotoxigenic Escherichia coli infection in weaned pigs | In vivo therapeutic efficacy and pharmacokinetics of colistin sulfate in an experimental model of enterotoxigenic Escherichia coli infection in weaned pigs Abstract Enterotoxigenic Escherichia coli (ETEC: F4) associated with post-weaning diarrhea (PWD) in pigs has developed resistance against several antimicrobial fami... |
PMC9304635 | core_pubmed_pmc | Diosgenin and Its Analogs: Potential Protective Agents Against Atherosclerosis | Diosgenin and Its Analogs: Potential Protective Agents Against Atherosclerosis Abstract Abstract Atherosclerosis is a chronic inflammatory disease of the artery wall associated with lipid metabolism imbalance and maladaptive immune response, which mediates most cardiovascular events. First-line drugs such as statins an... |
PMC3586119 | core_pubmed_pmc | Comparison of the Pharmacokinetic and Pharmacodynamic Profiles of One US-Marketed and Two European-Marketed Epoetin Alfas | Comparison of the Pharmacokinetic and Pharmacodynamic Profiles of One US-Marketed and Two European-Marketed Epoetin Alfas Abstract Objectives: The aim of this study was to investigate the bioequivalence and potency of registered epoetin alfa products that have not been compared before in a randomized controlled clinica... |
PMC3055807 | core_pubmed_pmc | Development of an erythropoietin prescription simulator to improve abilities for the prescription of erythropoietin stimulating agents: Is it feasible? | Development of an erythropoietin prescription simulator to improve abilities for the prescription of erythropoietin stimulating agents: Is it feasible? Abstract Abstract Background The increasing use of erythropoietins with long half-lives and the tendency to lengthen the administration interval to monthly injections c... |
PMC9155607 | core_pubmed_pmc | Omadacycline efficacy in the hollow fibre system model of pulmonary Mycobacterium avium complex and potency at clinically attainable doses | Omadacycline efficacy in the hollow fibre system model of pulmonary Mycobacterium avium complex and potency at clinically attainable doses Abstract Abstract Objectives The standard of care (SOC) for the treatment of pulmonary Mycobacterium avium complex (MAC) disease (clarithromycin, rifabutin, and ethambutol) achieves... |
PMC11011029 | core_pubmed_pmc | Design and Preclinical Evaluation of a Novel Prostate-Specific Membrane Antigen Radioligand Modified with a Transthyretin Binder | Design and Preclinical Evaluation of a Novel Prostate-Specific Membrane Antigen Radioligand Modified with a Transthyretin Binder Abstract Abstract Simple Summary Prostate-specific membrane antigen (PSMA)-targeting radioligands have been used clinically to treat metastatic prostate cancer. To deliver a sufficient radiat... |
PMC8068971 | core_pubmed_pmc | In Silico Prediction of Drug–Drug Interactions Mediated by Cytochrome P450 Isoforms | In Silico Prediction of Drug–Drug Interactions Mediated by Cytochrome P450 Isoforms Abstract Drug–drug interactions (DDIs) can cause drug toxicities, reduced pharmacological effects, and adverse drug reactions. Studies aiming to determine the possible DDIs for an investigational drug are part of the drug discovery and ... |
PMC7647411 | core_pubmed_pmc | Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors | Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors Abstract Highlights • Prorteases (Mpro and PLpro) are part of the replication machinery of corona virus. • Mpro and PLpro inhibitors may serve as therapeutic weapons against ... |
PMC8598294 | core_pubmed_pmc | Clinical pharmacokinetics and dose recommendations for posaconazole gastroresistant tablets in children with cystic fibrosis | Clinical pharmacokinetics and dose recommendations for posaconazole gastroresistant tablets in children with cystic fibrosis Abstract Abstract Objectives To investigate the population pharmacokinetics of posaconazole gastroresistant tablets in children with cystic fibrosis (CF) and perform simulations to recommend opti... |
PMC6321651 | core_pubmed_pmc | First-in-human study assessing safety, tolerability, and pharmacokinetics of 2-hydroxybenzylamine acetate, a selective dicarbonyl electrophile scavenger, in healthy volunteers | First-in-human study assessing safety, tolerability, and pharmacokinetics of 2-hydroxybenzylamine acetate, a selective dicarbonyl electrophile scavenger, in healthy volunteers Abstract Abstract Background 2-Hydroxybenzylamine (2-HOBA) is a selective scavenger of dicarbonyl electrophiles that protects proteins and lipid... |
PMC6409701 | core_pubmed_pmc | Improved Pharmacokinetics of Icariin (ICA) within Formulation of PEG-PLLA/PDLA-PNIPAM Polymeric Micelles | Improved Pharmacokinetics of Icariin (ICA) within Formulation of PEG-PLLA/PDLA-PNIPAM Polymeric Micelles Abstract Abstract Icariin (ICA) is a major flavonoid that contains the active compound Epimedii Folium . However, ICA’s pharmacokinetic characteristics remain unsatisfactory due to its low bioavailability, and hence... |
PMC10895699 | core_pubmed_pmc | Covariates in population pharmacokinetic studies of critically ill adults receiving β-lactam antimicrobials: a systematic review and narrative synthesis | Covariates in population pharmacokinetic studies of critically ill adults receiving β-lactam antimicrobials: a systematic review and narrative synthesis Abstract Abstract Introduction Population pharmacokinetic studies of β-lactam antimicrobials in critically ill patients derive models that inform their dosing. In non-... |
PMC5297980 | core_pubmed_pmc | Pharmacokinetic Interactions Between Isavuconazole and the Drug Transporter Substrates Atorvastatin, Digoxin, Metformin, and Methotrexate in Healthy Subjects | Pharmacokinetic Interactions Between Isavuconazole and the Drug Transporter Substrates Atorvastatin, Digoxin, Metformin, and Methotrexate in Healthy Subjects Abstract Abstract This article summarizes 4 phase 1 trials that explored interactions between the novel, triazole antifungal isavuconazole and substrates of the d... |
PMC3215676 | core_pubmed_pmc | Use of mefloquine in children - a review of dosage, pharmacokinetics and tolerability data | Use of mefloquine in children - a review of dosage, pharmacokinetics and tolerability data Abstract Abstract Background Use of anti-malarial medication in children is hampered by a paucity of dosage, pharmacokinetic and tolerability data. Methods Data on the use of mefloquine in children, particularly in young children... |
PMC3249860 | core_pubmed_pmc | Chirality and anaesthetic drugs: A review and an update | Chirality and anaesthetic drugs: A review and an update Abstract Abstract Many molecules can exist as right-handed and left-handed forms that are non-superimposable mirror images of each other. They are known as enantiomers or substances of opposite shape. Such compounds are also said to be chiral (Greek chiros meaning... |
PMC11754279 | core_pubmed_pmc | Population pharmacokinetics and dosing optimization of imipenem in Chinese elderly patients | Population pharmacokinetics and dosing optimization of imipenem in Chinese elderly patients Abstract Objectives To assess the pharmacokinetics and pharmacodynamics of imipenem in a retrospective cohort of hospitalized Chinese older patients. Methods A population pharmacokinetic (PPK) model was constructed utilizing a n... |
PMC6292180 | core_pubmed_pmc | Prasugrel in critically ill patients | Prasugrel in critically ill patients Abstract Summary While prasugrel is indicated for the treatment of myocardial infarction, its effects in the most severely affected patients requiring intensive care is unknown, so that we measured the antiplatelet effects and sparse pharmacokinetics of prasugrel in critically ill p... |
PMC7335848 | core_pubmed_pmc | Pharmacokinetic Disposition Difference Between Cyclosporine and Voclosporin Drives Their Distinct Efficacy and Safety Profiles in Clinical Studies | Pharmacokinetic Disposition Difference Between Cyclosporine and Voclosporin Drives Their Distinct Efficacy and Safety Profiles in Clinical Studies Abstract Abstract Background Voclosporin, a more potent derivative of cyclosporine, has been studied extensively in patients with immunologic disorders such as psoriasis, or... |
PMC5378937 | core_pubmed_pmc | Noncompetitive Inhibition of 5-HT 3 Receptors by Citral, Linalool, and Eucalyptol Revealed by Nonlinear Mixed-Effects Modeling | Noncompetitive Inhibition of 5-HT 3 Receptors by Citral, Linalool, and Eucalyptol Revealed by Nonlinear Mixed-Effects Modeling Abstract Abstract Citral, eucalyptol, and linalool are widely used as flavorings, fragrances, and cosmetics. Here, we examined their effects on electrophysiological and binding properties of hu... |
PMC11354794 | core_pubmed_pmc | Precision Medicine in Childhood Cancer: The Influence of Genetic Polymorphisms on Vincristine-Induced Peripheral Neuropathy | Precision Medicine in Childhood Cancer: The Influence of Genetic Polymorphisms on Vincristine-Induced Peripheral Neuropathy Abstract Cancer is the leading cause of disease-related death among children. Vincristine (VCR), a key component of childhood cancer treatment protocols, is associated with the risk of peripheral ... |
PMC9292371 | core_pubmed_pmc | Pharmacokinetically‐guided dosing to improve the efficacy of brigatinib in non‐small cell lung cancer patients | Pharmacokinetically‐guided dosing to improve the efficacy of brigatinib in non‐small cell lung cancer patients Abstract Abstract Brigatinib was recently approved for the treatment of anaplastic lymphoma kinase‐positive non‐small cell lung cancer and is dosed according to a one‐dose‐fits‐all paradigm. We aimed to identi... |
PMC8376137 | core_pubmed_pmc | Scientific and regulatory evaluation of mechanistic in silico drug and disease models in drug development: Building model credibility | Scientific and regulatory evaluation of mechanistic in silico drug and disease models in drug development: Building model credibility Abstract Abstract The value of in silico methods in drug development and evaluation has been demonstrated repeatedly and convincingly. While their benefits are now unanimously recognized... |
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