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PMC3004644 | core_pubmed_pmc | Extended-release morphine sulfate in treatment of severe acute and chronic pain | Extended-release morphine sulfate in treatment of severe acute and chronic pain Abstract Abstract Morphine is the archetypal opioid analgesic. Because it is a short-acting opioid, its use has been limited to the management of acute pain. The development of extended-release formulations have resulted in the increased ut... |
PMC9495010 | core_pubmed_pmc | Vancomycin Area under the Concentration-Time Curve Estimation Using Bayesian Modeling versus First-Order Pharmacokinetic Equations: A Quasi-Experimental Study | Vancomycin Area under the Concentration-Time Curve Estimation Using Bayesian Modeling versus First-Order Pharmacokinetic Equations: A Quasi-Experimental Study Abstract Abstract Aim: To evaluate the efficiency of Bayesian modeling software and first-order pharmacokinetic (PK) equations to calculate vancomycin area under... |
PMC11676658 | core_pubmed_pmc | Prediction of SPT-07A Pharmacokinetics in Rats, Dogs, and Humans Using a Physiologically-Based Pharmacokinetic Model and In Vitro Data | Prediction of SPT-07A Pharmacokinetics in Rats, Dogs, and Humans Using a Physiologically-Based Pharmacokinetic Model and In Vitro Data Abstract Background/Objectives: SPT-07A, a D-borneol, is currently being developed in China for the treatment of ischemic stroke. We aimed to create a whole-body physiologically-based p... |
PMC5487684 | core_pubmed_pmc | Safety, Pharmacokinetics, and Antiviral Activity of a Novel HIV Antiviral, ABX464, in Treatment-Naive HIV-Infected Subjects in a Phase 2 Randomized, Controlled Study | Safety, Pharmacokinetics, and Antiviral Activity of a Novel HIV Antiviral, ABX464, in Treatment-Naive HIV-Infected Subjects in a Phase 2 Randomized, Controlled Study Abstract ABSTRACT We investigated the safety and antiviral effects of an anti-HIV compound (ABX464) with a unique mechanism of viral replication inhibitio... |
PMC3429834 | core_pubmed_pmc | Ceftiaxone-Induced Neurotoxicity: Case Report, Pharmacokinetic Considerations, and Literature Review | Ceftiaxone-Induced Neurotoxicity: Case Report, Pharmacokinetic Considerations, and Literature Review Abstract Ceftriaxone is widely used in patients for the treatment of serious gram-negative infections. Ceftriaxone can induce some potential side effects, including neurotoxicity, however, nonconvulsive status epileptic... |
PMC10372714 | core_pubmed_pmc | Safety, Virology, Pharmacokinetics, and Clinical Experience of High-Dose Intravenous Sotrovimab for the Treatment of Mild to Moderate COVID-19: An Open-Label Clinical Trial | Safety, Virology, Pharmacokinetics, and Clinical Experience of High-Dose Intravenous Sotrovimab for the Treatment of Mild to Moderate COVID-19: An Open-Label Clinical Trial Abstract Abstract Background Five hundred milligrams of intravenous (IV) sotrovimab has been shown to be well tolerated and efficacious against pre... |
PMC11748473 | core_pubmed_pmc | A phase 1/2 study of gilteritinib in combination with chemotherapy in newly diagnosed patients with AML in Asia | A phase 1/2 study of gilteritinib in combination with chemotherapy in newly diagnosed patients with AML in Asia Abstract Abstract Objective This interim analysis of a phase 1/2, open-label, single-arm study assessed the safety, efficacy, and pharmacokinetics of gilteritinib plus chemotherapy in adults with newly diagno... |
PMC10107294 | core_pubmed_pmc | Effects of Tablet Formulation, Food, or Gastric pH on the Bioavailability of Asundexian | Effects of Tablet Formulation, Food, or Gastric pH on the Bioavailability of Asundexian Abstract ABSTRACT Absolute bioavailability (F) and the impact of gastric pH, tablet formulation, and food on the pharmacokinetics and safety of asundexian, an oral factor XIa inhibitor, was assessed in healthy White men aged 18–45 y... |
PMC12008189 | core_pubmed_pmc | A comparison between radiomic biological age and chronological age in estimating kidney function | A comparison between radiomic biological age and chronological age in estimating kidney function Abstract Abstract Accurate kidney function estimation hinges on essential markers of age and body size. The relative benefit of both markers has been debated with the emerging biological age and novel body size descriptors.... |
PMC7594230 | core_pubmed_pmc | Pharmacokinetics in routine haemophilia clinical practice: rationale and modalities—a practical review | Pharmacokinetics in routine haemophilia clinical practice: rationale and modalities—a practical review Abstract Prophylactic therapy with exogenous clotting factor concentrates in haemophilia A and B aims to achieve levels of circulating FVIII or FIX that are adequate for the prevention or reduction of spontaneous join... |
PMC9415580 | core_pubmed_pmc | Beyond Formulation: Contributions of Nanotechnology for Translation of Anticancer Natural Products into New Drugs | Beyond Formulation: Contributions of Nanotechnology for Translation of Anticancer Natural Products into New Drugs Abstract Nature is the largest pharmacy in the world. Doxorubicin (DOX) and paclitaxel (PTX) are two examples of natural-product-derived drugs employed as first-line treatment of various cancer types due to... |
PMC7463465 | core_pubmed_pmc | Simulation of Physicochemical and Pharmacokinetic Properties of Vitamin D 3 and Its Natural Derivatives | Simulation of Physicochemical and Pharmacokinetic Properties of Vitamin D 3 and Its Natural Derivatives Abstract Vitamin D 3 is an endogenous fat-soluble secosteroid, either biosynthesized in human skin or absorbed from diet and health supplements. Multiple hydroxylation reactions in several tissues including liver and... |
PMC9716490 | core_pubmed_pmc | Cannabidiol in clinical and preclinical anxiety research. A systematic review into concentration–effect relations using the IB-de-risk tool | Cannabidiol in clinical and preclinical anxiety research. A systematic review into concentration–effect relations using the IB-de-risk tool Abstract Abstract Background: Preclinical research suggests that cannabidiol (CBD) may have therapeutic potential in pathological anxiety. Dosing guidelines to inform future human ... |
PMC12003457 | core_pubmed_pmc | Influence of cigarette smoking on drugs’ metabolism and effects: a systematic review | Influence of cigarette smoking on drugs’ metabolism and effects: a systematic review Abstract Abstract Purpose Cigarette smoke continues to be widely used around the world and it contains several substances that can affect the pharmacokinetics and/or pharmacodynamics of medications, altering their safety and effectiven... |
PMC10177140 | core_pubmed_pmc | Development and Application of a Physiologically Based Pharmacokinetic Model for Diclazuril in Broiler Chickens | Development and Application of a Physiologically Based Pharmacokinetic Model for Diclazuril in Broiler Chickens Abstract Abstract Simple Summary Coccidiosis is a devastating poultry disease with significant economic implications. The prevention and control of coccidiosis currently rely on the administration of anticocc... |
PMC3315513 | core_pubmed_pmc | Pharmacokinetic Modeling of an Induction Regimen for In Vivo Combined Testing of Novel Drugs against Pediatric Acute Lymphoblastic Leukemia Xenografts | Pharmacokinetic Modeling of an Induction Regimen for In Vivo Combined Testing of Novel Drugs against Pediatric Acute Lymphoblastic Leukemia Xenografts Abstract Abstract Current regimens for induction therapy of pediatric acute lymphoblastic leukemia (ALL), or for re-induction post relapse, use a combination of vincrist... |
PMC8071233 | core_pubmed_pmc | Immunotherapy Combined with Metronomic Dosing: An Effective Approach for the Treatment of NSCLC | Immunotherapy Combined with Metronomic Dosing: An Effective Approach for the Treatment of NSCLC Abstract Simple Summary Non-small cell lung cancer (NSCLC) claims almost 80% of the total lung cancer cases, with the late-stage disease having an estimated median survival time of up to five years. Patients with NSCLC benef... |
PMC12665252 | core_pubmed_pmc | Proteomic Identification of Plasma Biomarkers of Response to IL‐5 Inhibitor Biologics in Healthy Subjects | Proteomic Identification of Plasma Biomarkers of Response to IL‐5 Inhibitor Biologics in Healthy Subjects Abstract ABSTRACT Proteomics can identify pharmacodynamic (PD) biomarkers by detecting protein changes in response to drug treatment, providing insights into drug mechanism and biological effects. In this study, we... |
PMC3284369 | core_pubmed_pmc | Drug-Drug Interaction Analysis of Pyronaridine/Artesunate and Ritonavir in Healthy Volunteers | Drug-Drug Interaction Analysis of Pyronaridine/Artesunate and Ritonavir in Healthy Volunteers Abstract Abstract A multiple dose, parallel group study was conducted to assess for a drug-drug interaction between the pyronaridine/artesunate (PA) combination antimalarial and ritonavir. Thirty-four healthy adults were rando... |
PMC9609094 | core_pubmed_pmc | Dendrimer-Conjugated nSMase2 Inhibitor Reduces Tau Propagation in Mice | Dendrimer-Conjugated nSMase2 Inhibitor Reduces Tau Propagation in Mice Abstract Alzheimer’s disease (AD) is characterized by the progressive accumulation of amyloid-β and hyperphosphorylated tau (pTau), which can spread throughout the brain via extracellular vesicles (EVs). Membrane ceramide enrichment regulated by the... |
PMC8172219 | core_pubmed_pmc | The influence of Javanese turmeric ( Curcuma xanthorrhiza ) on the pharmacokinetics of warfarin in rats with single and multiple-dose studies | The influence of Javanese turmeric ( Curcuma xanthorrhiza ) on the pharmacokinetics of warfarin in rats with single and multiple-dose studies Abstract Abstract Context Co-administration between warfarin (WF) and Curcuma xanthorrhiza Roxb. (Zingiberaceae) (CX) is found in Indonesian patients and need to be evaluated. Ob... |
PMC8427859 | core_pubmed_pmc | Development of weight and age-based dosing of daily primaquine for radical cure of vivax malaria | Development of weight and age-based dosing of daily primaquine for radical cure of vivax malaria Abstract Background In many endemic areas, Plasmodium vivax malaria is predominantly a disease of young adults and children. International recommendations for radical cure recommend fixed target doses of 0.25 or 0.5 mg/kg/d... |
PMC10931676 | core_pubmed_pmc | Prediction of Human Pharmacokinetics of E0703, a Novel Radioprotective Agent, Using Physiologically Based Pharmacokinetic Modeling and an Interspecies Extrapolation Approach | Prediction of Human Pharmacokinetics of E0703, a Novel Radioprotective Agent, Using Physiologically Based Pharmacokinetic Modeling and an Interspecies Extrapolation Approach Abstract Abstract E0703, a new steroidal compound optimized from estradiol, significantly increased cell proliferation and the survival rate of KM... |
PMC6130633 | core_pubmed_pmc | Effects of Ginkgo leaf tablets on the pharmacokinetics of losartan and its metabolite EXP3174 in rats and its mechanism | Effects of Ginkgo leaf tablets on the pharmacokinetics of losartan and its metabolite EXP3174 in rats and its mechanism Abstract Abstract Context: Ginkgo leaf tablets (GLTs) and losartan are often simultaneously used for the treatment of hypertension in Chinese clinics. However, the herb–drug interaction between GLT an... |
PMC7327946 | core_pubmed_pmc | The Kinetic Component in Drug Discovery: Using the Most Basic Pharmacological Concepts to Advance in Selecting Drugs to Combat CNS Diseases | The Kinetic Component in Drug Discovery: Using the Most Basic Pharmacological Concepts to Advance in Selecting Drugs to Combat CNS Diseases Abstract To reach the central nervous system (CNS), drugs must cross the brain-blood barrier and have appropriate pharmacokinetic/dynamic properties. However, in early drug discove... |
PMC12406680 | core_pubmed_pmc | Pharmacokinetics, safety, and tolerability of onradivir in participants with severe renal impairment and matched healthy control participants | Pharmacokinetics, safety, and tolerability of onradivir in participants with severe renal impairment and matched healthy control participants Abstract ABSTRACT Onradivir is an influenza A virus RNA polymerase basic protein 2 inhibitor that is currently under development for the treatment of influenza A. Renal impairmen... |
PMC10022669 | core_pubmed_pmc | Baseline Characteristics of Pediatric Patients With Heart Failure Due to Systemic Left Ventricular Systolic Dysfunction in the PANORAMA-HF Trial | Baseline Characteristics of Pediatric Patients With Heart Failure Due to Systemic Left Ventricular Systolic Dysfunction in the PANORAMA-HF Trial Abstract Background: Sacubitril/valsartan has been approved for the management of heart failure (HF) with reduced ejection fraction in adults. PANORAMA-HF trial (Prospective T... |
PMC5465189 | core_pubmed_pmc | Dynamic Contrast-enhanced MRI in Renal Tumors: Common Subtype Differentiation using Pharmacokinetics | Dynamic Contrast-enhanced MRI in Renal Tumors: Common Subtype Differentiation using Pharmacokinetics Abstract Preoperative renal tumor subtype differentiation is important for radiology and urology in clinical practice. Pharmacokinetic data ( K trans & V e , etc.) derived from dynamic contrast-enhanced MRI (DCE-MRI) ha... |
PMC10130219 | core_pubmed_pmc | Ameliorative effect of cheqianzi decoction on hyperuricemia and kidney injury and underlying mechanism in rats | Ameliorative effect of cheqianzi decoction on hyperuricemia and kidney injury and underlying mechanism in rats Abstract Cheqianzi Decoction (CQD) is a Traditional Chinese Medicine (TCM) formula comprising four herbs and is recorded in the Ancient Materia Medica “Shengji Zonglu”. Individually, these four herbs have been... |
PMC8129194 | core_pubmed_pmc | Evaluation of Factors Impacting the Efficacy of Single or Combination Therapies of Valproic Acid, Carbamazepine, and Oxcarbazepine: A Longitudinal Observation Study | Evaluation of Factors Impacting the Efficacy of Single or Combination Therapies of Valproic Acid, Carbamazepine, and Oxcarbazepine: A Longitudinal Observation Study Abstract Abstract Objective: This study aimed to determine the efficacy and clinical factors related to the pharmacodynamics of single or combination thera... |
PMC11638319 | core_pubmed_pmc | A Single‐Dose Study to Evaluate the Relative Bioavailability, Safety, and Tolerability of Monthly Extended-Release Buprenorphine at Alternative Injection Locations in Adult Participants with Opioid Use Disorder | A Single‐Dose Study to Evaluate the Relative Bioavailability, Safety, and Tolerability of Monthly Extended-Release Buprenorphine at Alternative Injection Locations in Adult Participants with Opioid Use Disorder Abstract Abstract Background and Objectives Buprenorphine extended-release monthly formulation (BUP-XR, SUBLO... |
PMC9668477 | core_pubmed_pmc | Molecular Docking and Dynamics Simulation of Several Flavonoids Predict Cyanidin as an Effective Drug Candidate against SARS-CoV-2 Spike Protein | Molecular Docking and Dynamics Simulation of Several Flavonoids Predict Cyanidin as an Effective Drug Candidate against SARS-CoV-2 Spike Protein Abstract The in silico method has provided a versatile process of developing lead compounds from a large database in a short duration. Therefore, it is imperative to look for ... |
PMC9572189 | core_pubmed_pmc | Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers | Pharmacokinetics and Endocrine Effects of an Oral Dose of D-Pinitol in Human Fasting Healthy Volunteers Abstract The present study characterizes the oral pharmacokinetics of D-Pinitol, a natural insulin mimetic inositol, in human healthy volunteers (14 males and 11 females). D-Pinitol absorption was studied in (a) subj... |
PMC10290335 | core_pubmed_pmc | Pharmacokinetics of ivermectin metabolites and their activity against Anopheles stephensi mosquitoes | Pharmacokinetics of ivermectin metabolites and their activity against Anopheles stephensi mosquitoes Abstract Abstract Background Ivermectin (22,23-dihydroavermectin B 1a : H 2 B 1a ) is an endectocide used to treat worm infections and ectoparasites including lice and scabies mites. Furthermore, survival of malaria tra... |
PMC10567933 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Bioequivalence of Pegfilgrastim-cbqv Delivered via a Prefilled Autoinjector and Prefilled Syringe in Healthy Male Participants | Pharmacokinetic and Pharmacodynamic Bioequivalence of Pegfilgrastim-cbqv Delivered via a Prefilled Autoinjector and Prefilled Syringe in Healthy Male Participants Abstract Introduction Pegfilgrastim-cbqv (UDENYCA ® ; Coherus BioSciences, Redwood City, CA, USA) is a pegfilgrastim (Neulasta ® ; Amgen, Thousand Oaks, CA, ... |
PMC12655400 | core_pubmed_pmc | Advancing Personalized Medicine Through FDM 3D Printing: Ketoprofen Tablets with Customizable Drug Release Profiles and In Silico Simulation | Advancing Personalized Medicine Through FDM 3D Printing: Ketoprofen Tablets with Customizable Drug Release Profiles and In Silico Simulation Abstract Abstract Background/Objectives : Fused deposition modeling (FDM) three-dimensional (3D) printing represents an emerging manufacturing platform for personalized oral dosag... |
PMC12584636 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic modeling of a highly potent and broadly neutralizing anti-CD4 trimeric nanobody to inhibit HIV-1 infection | Pharmacokinetic-pharmacodynamic modeling of a highly potent and broadly neutralizing anti-CD4 trimeric nanobody to inhibit HIV-1 infection Abstract ABSTRACT Nb 457 is a novel anti-CD4 nanobody derived from a CD4-immunized alpaca, exhibiting high potency and broad-spectrum activity against HIV-1. This study aims to use ... |
PMC6851537 | core_pubmed_pmc | A Framework Proposal to Follow‐Up on Preclinical Convulsive Signals of a New Molecular Entity in First‐in‐Human Studies Using Electroencephalographic Monitoring | A Framework Proposal to Follow‐Up on Preclinical Convulsive Signals of a New Molecular Entity in First‐in‐Human Studies Using Electroencephalographic Monitoring Abstract Traditionally, in dose‐escalating first‐in‐human (FiH) studies, a dose cap with a 10‐fold safety margin to the no observed effect level in animals is ... |
PMC7825058 | core_pubmed_pmc | Comparison of Five Oral Cannabidiol Preparations in Adult Humans: Pharmacokinetics, Body Composition, and Heart Rate Variability | Comparison of Five Oral Cannabidiol Preparations in Adult Humans: Pharmacokinetics, Body Composition, and Heart Rate Variability Abstract Abstract Data supporting the physiological effects of cannabidiol (CBD) ingestion in humans are conflicting. Differences between CBD preparations and bioavailability may contribute t... |
PMC8396736 | core_pubmed_pmc | Pharmacokinetics of tulathromycin in pregnant ewes ( Ovis aries ) challenged with Campylobacter jejuni | Pharmacokinetics of tulathromycin in pregnant ewes ( Ovis aries ) challenged with Campylobacter jejuni Abstract Abstract The purpose of this study was to evaluate the pharmacokinetics of tulathromycin in the plasma and maternal and fetal tissues of pregnant ewes when administered within 24 hours of a single, IV Campylo... |
PMC7774723 | core_pubmed_pmc | Overnight fasting before lapatinib administration to breast cancer patients leads to reduced toxicity compared with nighttime dosing: a retrospective cohort study from a randomized clinical trial | Overnight fasting before lapatinib administration to breast cancer patients leads to reduced toxicity compared with nighttime dosing: a retrospective cohort study from a randomized clinical trial Abstract Abstract Background The bioavailability of lapatinib is affected by food, even following the 1 hour fast recommende... |
PMC4209234 | core_pubmed_pmc | A first-in-human study of the anti-α5β1 integrin monoclonal antibody PF-04605412 administered intravenously to patients with advanced solid tumors | A first-in-human study of the anti-α5β1 integrin monoclonal antibody PF-04605412 administered intravenously to patients with advanced solid tumors Abstract Abstract Purpose A first-in-human clinical trial of a fully human, Fc-engineered IgG1 monoclonal antibody targeting integrin α5β1 was conducted to evaluate tolerabi... |
PMC9981212 | core_pubmed_pmc | Safety and Efficacy of Engineered Toxin Body MT-3724 in Relapsed or Refractory B-cell Non-Hodgkin's Lymphomas and Diffuse Large B-cell Lymphoma | Safety and Efficacy of Engineered Toxin Body MT-3724 in Relapsed or Refractory B-cell Non-Hodgkin's Lymphomas and Diffuse Large B-cell Lymphoma Abstract Abstract MT-3724, a novel engineered toxin body comprised of an anti-CD20 single-chain variable fragment genetically fused to Shiga-like Toxin A subunit, is capable of... |
PMC8906246 | core_pubmed_pmc | Association of Baseline and Pharmacodynamic Biomarkers With Outcomes in Patients Treated With the PD-1 Inhibitor Budigalimab | Association of Baseline and Pharmacodynamic Biomarkers With Outcomes in Patients Treated With the PD-1 Inhibitor Budigalimab Abstract Budigalimab, a novel anti–PD-1 monoclonal antibody, demonstrated efficacy and biomarker pharmacodynamics in patients with head and neck squamous cell carcinoma (HNSCC) or non–small cell ... |
PMC11729436 | core_pubmed_pmc | Development and Clinical Validation of Model-Informed Precision Dosing for Everolimus in Liver Transplant Recipients | Development and Clinical Validation of Model-Informed Precision Dosing for Everolimus in Liver Transplant Recipients Abstract Everolimus presents significant dosing challenges due to between- and within-patient pharmacokinetic variabilities. This study aimed to develop and validate a model-informed precision dosing str... |
PMC4780207 | core_pubmed_pmc | Naringenin-loaded solid lipid nanoparticles: preparation, controlled delivery, cellular uptake, and pulmonary pharmacokinetics | Naringenin-loaded solid lipid nanoparticles: preparation, controlled delivery, cellular uptake, and pulmonary pharmacokinetics Abstract Abstract Naringenin (NRG), a flavonoid compound, had been reported to exhibit extensive pharmacological effects, but its water solubility and oral bioavailability are only~46±6 µg/mL a... |
PMC8019539 | core_pubmed_pmc | Opioid toxicity due to CNS depressant polypharmacy: A case report | Opioid toxicity due to CNS depressant polypharmacy: A case report Abstract Abstract The interaction between methadone and central nervous system depressants can cause serious adverse effects, including profound sedation, respiratory depression, coma, and death. This poses a challenge in the treatment of patients with c... |
PMC11106139 | core_pubmed_pmc | Development of a Weight-Band Dosing Approach for Vosoritide in Children with Achondroplasia Using a Population Pharmacokinetic Model | Development of a Weight-Band Dosing Approach for Vosoritide in Children with Achondroplasia Using a Population Pharmacokinetic Model Abstract Background and Objective Vosoritide is a recently approved therapy for achondroplasia, the most common form of disproportionate short stature, that has been shown to be well tole... |
PMC8452294 | core_pubmed_pmc | A best practice framework for applying physiologically‐based pharmacokinetic modeling to pediatric drug development | A best practice framework for applying physiologically‐based pharmacokinetic modeling to pediatric drug development Abstract Pediatric physiologically‐based pharmacokinetic (PBPK) models have broad application in the drug development process and are being used not only to project doses for clinical trials but increasin... |
PMC12405907 | core_pubmed_pmc | Impact of the transcription factor nuclear factor 1 B T>C polymorphism on clozapine metabolism in vivo and expression of intestinal transporters in vitro | Impact of the transcription factor nuclear factor 1 B T>C polymorphism on clozapine metabolism in vivo and expression of intestinal transporters in vitro Abstract Clozapine’s (CLZ) pharmacokinetics involves multiple enzymes and transporters, which may be influenced by genetic variability. A variant in the nuclear facto... |
PMC7235806 | core_pubmed_pmc | Pharmacokinetics of Macrolide Antibiotics and Transport into the Interstitial Fluid: Comparison among Erythromycin, Clarithromycin, and Azithromycin | Pharmacokinetics of Macrolide Antibiotics and Transport into the Interstitial Fluid: Comparison among Erythromycin, Clarithromycin, and Azithromycin Abstract Recent research has found higher levels and longer total exposure of azithromycin, a macrolide antibiotic agent, in the interstitial fluid of the skin than in the... |
PMC8343194 | core_pubmed_pmc | Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo | Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo Abstract Abstract Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. Howe... |
PMC11321701 | core_pubmed_pmc | Generation and Characterization of Novel Pan‐Cancer Anti‐uPAR Fluorescent Nanobodies as Tools for Image‐Guided Surgery | Generation and Characterization of Novel Pan‐Cancer Anti‐uPAR Fluorescent Nanobodies as Tools for Image‐Guided Surgery Abstract Abstract Fluorescence molecular imaging plays a vital role in image‐guided surgery. In this context, the urokinase plasminogen activator receptor (uPAR) is an interesting biomarker enabling th... |
PMC5011881 | core_pubmed_pmc | Open label study of escalating doses of oral treprostinil diethanolamine in patients with systemic sclerosis and digital ischemia: pharmacokinetics and correlation with digital perfusion | Open label study of escalating doses of oral treprostinil diethanolamine in patients with systemic sclerosis and digital ischemia: pharmacokinetics and correlation with digital perfusion Abstract Abstract Introduction Treprostinil diethanolamine is an innovative salt form of the prostacyclin analogue, treprostinil sodi... |
PMC12209997 | core_pubmed_pmc | A 2‐Part, Open‐Label, Phase 1 Bioequivalence and Food‐Effect Study of Ubrogepant in Healthy Adult Participants | A 2‐Part, Open‐Label, Phase 1 Bioequivalence and Food‐Effect Study of Ubrogepant in Healthy Adult Participants Abstract Abstract This Phase 1 study of ubrogepant was conducted to establish the bioequivalence (BE) of the 50‐ and 100‐mg to‐be‐marketed (TBM) tablet formulations with the clinical trial (CT) 100‐mg tablet f... |
PMC3461153 | core_pubmed_pmc | Dose banding as an alternative to body surface area-based dosing of chemotherapeutic agents | Dose banding as an alternative to body surface area-based dosing of chemotherapeutic agents Abstract Background: Dose banding is a recently suggested dosing method that uses predefined ranges (bands) of body surface area (BSA) to calculate each patient’s dose by using a single BSA-value per band. Thus, drugs with suffi... |
PMC4895495 | core_pubmed_pmc | Pharmacokinetics of Single‐Dose Rectal Zonisamide Administration in Normal Dogs | Pharmacokinetics of Single‐Dose Rectal Zonisamide Administration in Normal Dogs Abstract Background Few medications are available for parental administration to animals with seizures. Rectal administration of medications is often used if the animal cannot be administered oral medications. Hypothesis/Objectives To deter... |
PMC12125134 | core_pubmed_pmc | Population Pharmacokinetics of Tranexamic Acid in Chinese Population Undergoing Cardiac Surgery with Cardiopulmonary Bypass | Population Pharmacokinetics of Tranexamic Acid in Chinese Population Undergoing Cardiac Surgery with Cardiopulmonary Bypass Abstract Background Population pharmacokinetics (PK) models could provide specific references for the formulation of personal drug delivery protocols, however, there is no population PK study of t... |
PMC8582169 | core_pubmed_pmc | Reviewing Data Integrated for PBPK Model Development to Predict Metabolic Drug-Drug Interactions: Shifting Perspectives and Emerging Trends | Reviewing Data Integrated for PBPK Model Development to Predict Metabolic Drug-Drug Interactions: Shifting Perspectives and Emerging Trends Abstract Abstract Physiologically-based pharmacokinetics (PBPK) modeling is a robust tool that supports drug development and the pharmaceutical industry and regulatory authorities.... |
PMC6765697 | core_pubmed_pmc | Quantitative Systems Pharmacology Model of a Masked, Tumor‐Activated Antibody | Quantitative Systems Pharmacology Model of a Masked, Tumor‐Activated Antibody Abstract Abstract PROBODY therapeutics (Pb‐Tx) are protease‐activatable prodrugs of monoclonal antibodies (mAbs) designed to target tumors where protease activity is elevated while avoiding normal tissue. They are composed of a parental mAb, ... |
PMC10377309 | core_pubmed_pmc | Anesthetic Management for Awake Craniotomy Applied to Neurosurgery | Anesthetic Management for Awake Craniotomy Applied to Neurosurgery Abstract Our anesthetic technique proposed for awake craniotomy is the monitored anesthesia care (MAC) technique, with the patient in sedation throughout the intervention. Our protocol involves analgo-sedation through the administration of dexmedetomidi... |
PMC11101992 | core_pubmed_pmc | First‐in‐human safety, tolerability, and pharmacokinetic results of DFV890, an oral low‐molecular‐weight NLRP3 inhibitor | First‐in‐human safety, tolerability, and pharmacokinetic results of DFV890, an oral low‐molecular‐weight NLRP3 inhibitor Abstract Abstract This first‐in‐human study evaluated the safety, tolerability, single‐ and multiple‐dose pharmacokinetic profiles with dietary influence, and pharmacodynamics (PD) of DFV890, an oral... |
PMC7238139 | core_pubmed_pmc | Pharmacokinetic Models to Characterize the Absorption Phase and the Influence of a Proton Pump Inhibitor on the Overall Exposure of Dacomitinib | Pharmacokinetic Models to Characterize the Absorption Phase and the Influence of a Proton Pump Inhibitor on the Overall Exposure of Dacomitinib Abstract Abstract Introduction: Dacomitinib is an epidermal growth factor receptor (EGFR) inhibitor approved for the treatment of metastatic non-small cell lung cancer (NSCLC) ... |
PMC4026632 | core_pubmed_pmc | An Integrated Population Pharmacokinetic Meta-Analysis of Propofol in Morbidly Obese and Nonobese Adults, Adolescents, and Children | An Integrated Population Pharmacokinetic Meta-Analysis of Propofol in Morbidly Obese and Nonobese Adults, Adolescents, and Children Abstract This study describes a population pharmacokinetic meta-analysis of propofol to characterize the influence of body size measures and age in morbidly obese and nonobese adults, adol... |
PMC3600725 | core_pubmed_pmc | Effect of Ritonavir on 99m Technetium–Mebrofenin Disposition in Humans: A Semi-PBPK Modeling and In Vitro Approach to Predict Transporter-Mediated DDIs | Effect of Ritonavir on 99m Technetium–Mebrofenin Disposition in Humans: A Semi-PBPK Modeling and In Vitro Approach to Predict Transporter-Mediated DDIs Abstract Abstract A semiphysiologically based pharmacokinetic (semi-PBPK) model was developed to describe a unique blood, liver, and bile clinical data set for the hepa... |
PMC7724925 | core_pubmed_pmc | Evaluation of the pharmacokinetics and efficacy of transdermal flunixin for pain mitigation following castration in goats | Evaluation of the pharmacokinetics and efficacy of transdermal flunixin for pain mitigation following castration in goats Abstract Abstract The mitigation of pain associated with common management procedures is a rising concern among veterinarians, producers and consumers. Nonsteroidal anti-inflammatory drugs are vital... |
PMC7856631 | core_pubmed_pmc | Diffusion and Protein Corona Formation of Lipid-Based Nanoparticles in the Vitreous Humor: Profiling and Pharmacokinetic Considerations | Diffusion and Protein Corona Formation of Lipid-Based Nanoparticles in the Vitreous Humor: Profiling and Pharmacokinetic Considerations Abstract The vitreous humor is the first barrier encountered by intravitreally injected nanoparticles. Lipid-based nanoparticles in the vitreous are studied by evaluating their diffusi... |
PMC8484135 | core_pubmed_pmc | Covariate effects and population pharmacokinetic analysis of the anti-FGFR2b antibody bemarituzumab in patients from phase 1 to phase 2 trials | Covariate effects and population pharmacokinetic analysis of the anti-FGFR2b antibody bemarituzumab in patients from phase 1 to phase 2 trials Abstract Abstract Purpose A population pharmacokinetic (PK) analysis of the anti-fibroblast growth factor receptor 2b antibody, bemarituzumab, was performed to evaluate the impa... |
PMC12182541 | core_pubmed_pmc | LY3522348, A New Ketohexokinase Inhibitor: A First-in-Human Study in Healthy Adults | LY3522348, A New Ketohexokinase Inhibitor: A First-in-Human Study in Healthy Adults Abstract Introduction This study aimed to assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple doses of the ketohexokinase inhibitor LY3522348 in healthy participants. Methods This fir... |
PMC12563216 | core_pubmed_pmc | Real-World Assessment of Pharmacokinetics, Clinical Outcomes, and Costs After Switching from Standard Half-Life to Extended Half-Life FVIII in Well-Controlled Hemophilia A Patients | Real-World Assessment of Pharmacokinetics, Clinical Outcomes, and Costs After Switching from Standard Half-Life to Extended Half-Life FVIII in Well-Controlled Hemophilia A Patients Abstract Abstract Objective: This study aimed to analyze pharmacokinetic and clinical parameters (bleeding rates and joint health) before a... |
PMC12625129 | core_pubmed_pmc | State‐of‐the‐Art on Model‐Informed Drug Development Approaches for Pediatric Rare Diseases | State‐of‐the‐Art on Model‐Informed Drug Development Approaches for Pediatric Rare Diseases Abstract ABSTRACT Pediatric rare diseases present unique challenges for drug development due to small patient populations, ethical constraints on clinical trial design, and limited prospectively defined natural history data. Mode... |
PMC8259366 | core_pubmed_pmc | Infliximab clearance decreases in the second and third trimesters of pregnancy in inflammatory bowel disease | Infliximab clearance decreases in the second and third trimesters of pregnancy in inflammatory bowel disease Abstract Abstract Background Infliximab therapy during pregnancy in inflammatory bowel disease is challenged by a dilemma between maintaining adequate maternal disease control while minimizing fetal infliximab e... |
PMC10168221 | core_pubmed_pmc | Generating immunogenomic data-guided virtual patients using a QSP model to predict response of advanced NSCLC to PD-L1 inhibition | Generating immunogenomic data-guided virtual patients using a QSP model to predict response of advanced NSCLC to PD-L1 inhibition Abstract Abstract Generating realistic virtual patients from a limited amount of patient data is one of the major challenges for quantitative systems pharmacology modeling in immuno-oncology... |
PMC7908059 | core_pubmed_pmc | Dichondra repens J.R.Forst. and G.Forst.: A Review of Its Traditional Uses, Chemistry, Pharmacology, Toxicology and Applications | Dichondra repens J.R.Forst. and G.Forst.: A Review of Its Traditional Uses, Chemistry, Pharmacology, Toxicology and Applications Abstract Ethnopharmacology relevance: Dichondra repens J.R.Forst. and G.Forst (DRF; Convolvulaceae, called Matijin in Chinese), has been traditionally used to treat jaundice, bacillary dysent... |
PMC4317222 | core_pubmed_pmc | Characterization of the 5-HT 2C receptor agonist lorcaserin on efficacy and safety measures in a rat model of diet-induced obesity | Characterization of the 5-HT 2C receptor agonist lorcaserin on efficacy and safety measures in a rat model of diet-induced obesity Abstract The 5-HT 2C receptor agonist lorcaserin (Belviq®) has been Food and Drug Administration (FDA) approved for the treatment of obesity. The present study is a back translational inves... |
PMC10619746 | core_pubmed_pmc | Examination of betahistine bioavailability in combination with the monoamine oxidase B inhibitor, selegiline, in humans—a non-randomized, single-sequence, two-period titration, open label single-center phase 1 study (PK-BeST) | Examination of betahistine bioavailability in combination with the monoamine oxidase B inhibitor, selegiline, in humans—a non-randomized, single-sequence, two-period titration, open label single-center phase 1 study (PK-BeST) Abstract Abstract Background Betahistine was registered in Europe in the 1970s and approved in... |
PMC8532761 | core_pubmed_pmc | Imipenem/Relebactam Ex Vivo Clearance during Continuous Renal Replacement Therapy | Imipenem/Relebactam Ex Vivo Clearance during Continuous Renal Replacement Therapy Abstract Abstract (1) Purpose of this study: determination of adsorption and transmembrane clearances (CL TM ) of imipenem and relebactam in ex vivo continuous hemofiltration (CH) and continuous hemodialysis (CHD) models. These clearances... |
PMC3644404 | core_pubmed_pmc | Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics | Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics Abstract Summary Purpose Given distinct mechanism of actions of enzastaurin and bevacizumab, preclinical studies suggest enhanced antitumor activity in combination. This phase I study assessed the combin... |
PMC9706003 | core_pubmed_pmc | Tacrolimus pharmacokinetics in pediatric nephrotic syndrome: A combination of population pharmacokinetic modelling and machine learning approaches to improve individual prediction | Tacrolimus pharmacokinetics in pediatric nephrotic syndrome: A combination of population pharmacokinetic modelling and machine learning approaches to improve individual prediction Abstract Abstract Background and Aim: Tacrolimus (TAC) is a first-line immunosuppressant for the treatment of refractory nephrotic syndrome ... |
PMC7801660 | core_pubmed_pmc | Early impact of donor CYP3A5 genotype and Graft-to-Recipient Weight Ratio on tacrolimus pharmacokinetics in pediatric liver transplant patients | Early impact of donor CYP3A5 genotype and Graft-to-Recipient Weight Ratio on tacrolimus pharmacokinetics in pediatric liver transplant patients Abstract Tacrolimus (TAC) pharmacokinetics is influenced by the donor CYP3A5 genotype and the age of pediatric liver recipients. However, an optimization of a genotype-based al... |
PMC7158095 | core_pubmed_pmc | Intraoperative surgical site infection control and prevention: a position paper and future addendum to WSES intra-abdominal infections guidelines | Intraoperative surgical site infection control and prevention: a position paper and future addendum to WSES intra-abdominal infections guidelines Abstract Background Surgical site infections (SSI) represent a considerable burden for healthcare systems. They are largely preventable and multiple interventions have been p... |
PMC4142165 | core_pubmed_pmc | Milk and Blood Pharmacokinetics of Tylosin and Tilmicosin following Parenteral Administrations to Cows | Milk and Blood Pharmacokinetics of Tylosin and Tilmicosin following Parenteral Administrations to Cows Abstract Abstract The aim of this study is to determine the pharmacokinetics of tylosin and tilmicosin in serum and milk in healthy Holstein breed cows ( n = 12) and reevaluate the amount of residue in milk. Following... |
PMC11673240 | core_pubmed_pmc | Natural Compounds Targeting Thymic Stromal Lymphopoietin (TSLP): A Promising Therapeutic Strategy for Atopic Dermatitis | Natural Compounds Targeting Thymic Stromal Lymphopoietin (TSLP): A Promising Therapeutic Strategy for Atopic Dermatitis Abstract Atopic dermatitis (AD) is a chronic inflammatory skin disease with rising prevalence, marked by eczematous lesions, itching, and a weakened skin barrier often tied to filaggrin gene mutations... |
PMC6451706 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Modeling to Optimize the Dose of Vestronidase Alfa, an Enzyme Replacement Therapy for Treatment of Patients with Mucopolysaccharidosis Type VII: Results from Three Trials | Pharmacokinetic and Pharmacodynamic Modeling to Optimize the Dose of Vestronidase Alfa, an Enzyme Replacement Therapy for Treatment of Patients with Mucopolysaccharidosis Type VII: Results from Three Trials Abstract Abstract Introduction Mucopolysaccharidosis type VII (MPS VII, Sly Syndrome) is a progressive, debilitat... |
PMC7924795 | core_pubmed_pmc | Pharmacokinetic / pharmacodynamic relationships of liposomal amphotericin B and miltefosine in experimental visceral leishmaniasis | Pharmacokinetic / pharmacodynamic relationships of liposomal amphotericin B and miltefosine in experimental visceral leishmaniasis Abstract Background There is a continued need to develop effective and safe treatments for visceral leishmaniasis (VL). Preclinical studies on pharmacokinetics and pharmacodynamics of anti-... |
PMC10520121 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Dorzagliatin in Healthy Subjects and Patients with Type 2 Diabetes Mellitus | Population Pharmacokinetic Analysis of Dorzagliatin in Healthy Subjects and Patients with Type 2 Diabetes Mellitus Abstract Background and Objectives Dorzagliatin is a first-in-class small molecule glucokinase activator (GKA) that improves pancreatic insulin secretion behavior and regulates hepatic glucose conversion i... |
PMC9070875 | core_pubmed_pmc | Multi-center prospective population pharmacokinetic study and the performance of web-based individual dose optimization application of intravenous vancomycin for adults in Hong Kong: A study protocol | Multi-center prospective population pharmacokinetic study and the performance of web-based individual dose optimization application of intravenous vancomycin for adults in Hong Kong: A study protocol Abstract Abstract A recent consensus guideline recommends migrating the therapeutic drug monitoring practice for intrave... |
PMC9198545 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Fungal Defensin NZX Against Staphylococcus aureus -Induced Mouse Peritonitis Model | Pharmacokinetics and Pharmacodynamics of Fungal Defensin NZX Against Staphylococcus aureus -Induced Mouse Peritonitis Model Abstract Abstract Staphylococcus aureus ( S. aureus ) is one of the most common pathogenic bacteria responsible for causing a life-threatening peritonitis disease. NZX, as a variant of fungal defe... |
PMC11063992 | core_pubmed_pmc | Massive lignocaine overdose while on veno-arterial extracorporeal membrane oxygenation (VA ECMO) | Massive lignocaine overdose while on veno-arterial extracorporeal membrane oxygenation (VA ECMO) Abstract We present the extraordinary circumstance of a female patient in her sixties who suffered a massive lignocaine overdose while undergoing treatment with Veno-Arterial Extracorporeal Membrane Oxygenation (VA ECMO) fo... |
PMC9078972 | core_pubmed_pmc | Identification of a new series of benzothiazinone derivatives with excellent antitubercular activity and improved pharmacokinetic profiles † | Identification of a new series of benzothiazinone derivatives with excellent antitubercular activity and improved pharmacokinetic profiles † Abstract Nitrobenzothiazinone (BTZ) is a promising scaffold with potent activity against M. tuberculosis by inhibiting decaprenylphosphoryl-beta- d -ribose 2′-oxidase (DprE1). But... |
PMC5327911 | core_pubmed_pmc | The effect of apixaban on the pharmacokinetics of digoxin and atenolol in healthy subjects | The effect of apixaban on the pharmacokinetics of digoxin and atenolol in healthy subjects Abstract Purpose Apixaban is often coadministered with treatments for cardiovascular comorbidities, which may lead to unintended drug–drug interactions (DDIs). The effects of apixaban on pharmacokinetics (PK) of multidose Lanoxin... |
PMC3637904 | core_pubmed_pmc | Development and Validation of HPLC Method for Determination of Crocetin, a constituent of Saffron, in Human Serum Samples | Development and Validation of HPLC Method for Determination of Crocetin, a constituent of Saffron, in Human Serum Samples Abstract Abstract Objective(s): The present study reports the development and validation of a sensitive and rapid extraction method beside high performance liquid chromatographic method for the dete... |
PMC12496429 | core_pubmed_pmc | Safety and pharmacology of AMY109, a long-acting anti–interleukin-8 antibody, for endometriosis: a double-blind, randomized phase 1 trial | Safety and pharmacology of AMY109, a long-acting anti–interleukin-8 antibody, for endometriosis: a double-blind, randomized phase 1 trial Abstract Abstract Objective To evaluate the safety and pharmacokinetics/pharmacodynamics of AMY109, an anti–interleukin-8 recycling antibody in a first-in-human phase 1 trial in heal... |
PMC11515640 | core_pubmed_pmc | Bioequivalence study of eltrombopag 75 mg film-coated tablets under fasting conditions during the Covid-19 pandemic in healthy Caucasian male subjects | Bioequivalence study of eltrombopag 75 mg film-coated tablets under fasting conditions during the Covid-19 pandemic in healthy Caucasian male subjects Abstract This study aims to determine the bioequivalence of the reference preparation and the test preparation containing eltrombopag when both were given during the COV... |
PMC9182653 | core_pubmed_pmc | In Vivo Toxicity and Pharmacokinetics of Polytetrafluoroethylene Microplastics in ICR Mice | In Vivo Toxicity and Pharmacokinetics of Polytetrafluoroethylene Microplastics in ICR Mice Abstract Abstract The increased use of plastics has led to severe environmental pollution, particularly by microplastics—plastic particles 5 mm or less in diameter. These particles are formed by environmental factors such as weat... |
PMC3572379 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic effects of comedication of clopidogrel and dabigatran etexilate in healthy male volunteers | Pharmacokinetic and pharmacodynamic effects of comedication of clopidogrel and dabigatran etexilate in healthy male volunteers Abstract Purpose To evaluate the pharmacokinetic and pharmacodynamic effects of concomitant administration of single loading doses of clopidogrel or multiple doses of clopidogrel with multiple ... |
PMC4617862 | core_pubmed_pmc | Determination of the Optimal Concentration of Valproic Acid in Patients with Epilepsy: A Population Pharmacokinetic-Pharmacodynamic Analysis | Determination of the Optimal Concentration of Valproic Acid in Patients with Epilepsy: A Population Pharmacokinetic-Pharmacodynamic Analysis Abstract Valproic acid (VPA) is one of the most widely prescribed antiepileptic drugs for the treatment of epileptic seizures. Although it is well known that the doses of VPA and ... |
PMC11685967 | core_pubmed_pmc | Enhancing gene transfer to renal tubules and podocytes by context-dependent selection of AAV capsids | Enhancing gene transfer to renal tubules and podocytes by context-dependent selection of AAV capsids Abstract Abstract AAV vectors show promise for gene therapy; however, kidney gene transfer remains challenging. Here we conduct a barcode-seq-based comparison of 47 AAV capsids administered through different routes in m... |
PMC4414146 | core_pubmed_pmc | PACE4 inhibitors and their peptidomimetic analogs block prostate cancer tumor progression through quiescence induction, increased apoptosis and impaired neovascularisation | PACE4 inhibitors and their peptidomimetic analogs block prostate cancer tumor progression through quiescence induction, increased apoptosis and impaired neovascularisation Abstract Prostate cancer is the leading cancer in North American men. Current pharmacological treatments are limited to anti-androgen strategies and... |
PMC11297572 | core_pubmed_pmc | Construction and Evaluation of BAL-PTX Co-Loaded Lipid Nanosystem for Promoting the Anti-Lung Cancer Efficacy of Paclitaxel and Reducing the Toxicity of Chemotherapeutic Drugs | Construction and Evaluation of BAL-PTX Co-Loaded Lipid Nanosystem for Promoting the Anti-Lung Cancer Efficacy of Paclitaxel and Reducing the Toxicity of Chemotherapeutic Drugs Abstract Abstract Purpose The present study aimed to develop a lipid nanoplatform, denoted as “BAL-PTX-LN”, co-loaded with chiral baicalin deriv... |
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