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PMC10927884 | core_pubmed_pmc | Formulation, pharmacokinetics, and antibacterial activity of florfenicol-loaded niosome | Formulation, pharmacokinetics, and antibacterial activity of florfenicol-loaded niosome Abstract The growing interest in employing nano-sized pharmaceutical formulations in veterinary medicine has prompted the exploration of the novel nanocarriers’ ability to augment the therapeutic outcome. In this study, we harnessed... |
PMC9975770 | core_pubmed_pmc | Anti-BCMA/CD19 CAR T Cells with Early Immunomodulatory Maintenance for Multiple Myeloma Responding to Initial or Later-Line Therapy | Anti-BCMA/CD19 CAR T Cells with Early Immunomodulatory Maintenance for Multiple Myeloma Responding to Initial or Later-Line Therapy Abstract Abstract We conducted a phase I clinical trial of anti-BCMA chimeric antigen receptor T cells (CART-BCMA) with or without anti-CD19 CAR T cells (huCART19) in multiple myeloma (MM)... |
PMC5318341 | core_pubmed_pmc | A Review of Clinical Outcomes Associated with Two Meropenem Dosing Strategies | A Review of Clinical Outcomes Associated with Two Meropenem Dosing Strategies Abstract Meropenem is a carbapenem antibiotic that exhibits time-dependent bactericidal activity, traditionally dosed intravenously at 1 g every 8 h. In order to maximize its pharmacodynamic activity and reduce costs, an alternative regimen e... |
PMC11035414 | core_pubmed_pmc | A comparison study of dynamic [ 18 F]Alfatide II imaging and [ 11 C]MET in orthotopic rat models of glioblastoma | A comparison study of dynamic [ 18 F]Alfatide II imaging and [ 11 C]MET in orthotopic rat models of glioblastoma Abstract Purpose To investigate and compare the dynamic positron emission tomography (PET) imaging with [ 18 F]Alfatide II Imaging and [ 11 C]Methionine ([ 11 C]MET) in orthotopic rat models of glioblastoma ... |
PMC5114692 | core_pubmed_pmc | Development of a population pharmacokinetic model of prucalopride in children with functional constipation | Development of a population pharmacokinetic model of prucalopride in children with functional constipation Abstract Abstract A recent phase 3 trial of prucalopride in children with functional constipation ( SPD 555‐303 ClinicalTrials.gov Identifier: NCT01330381 ) reported negative efficacy results. Here, we developed a... |
PMC7338667 | core_pubmed_pmc | Wild-Type MIC Distribution for Re-evaluating the Critical Concentration of Anti-TB Drugs and Pharmacodynamics Among Tuberculosis Patients From South India | Wild-Type MIC Distribution for Re-evaluating the Critical Concentration of Anti-TB Drugs and Pharmacodynamics Among Tuberculosis Patients From South India Abstract The World Health Organization (WHO) has developed specific guidelines for critical concentrations (CCs) of antibiotics used for tuberculosis (TB) treatment,... |
PMC7412606 | core_pubmed_pmc | Implementing a pharmacogenetic-driven algorithm to guide dual antiplatelet therapy (DAPT) in Caribbean Hispanics: protocol for a non-randomised clinical trial | Implementing a pharmacogenetic-driven algorithm to guide dual antiplatelet therapy (DAPT) in Caribbean Hispanics: protocol for a non-randomised clinical trial Abstract Abstract Introduction Minority populations in the USA are disproportionately affected by cardiovascular conditions. Reduced responsiveness to clopidogre... |
PMC6686215 | core_pubmed_pmc | Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog | Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog Abstract Background Although the new isoxazoline drug fluralaner (Bravecto®) is generally well tolerated in dogs, adverse drug reactions involving neurological dysfunction occurred in individual dogs. However, most o... |
PMC3326684 | core_pubmed_pmc | First-in-man phase I trial of two schedules of the novel synthetic tetrahydroisoquinoline alkaloid PM00104 (Zalypsis) in patients with advanced solid tumours | First-in-man phase I trial of two schedules of the novel synthetic tetrahydroisoquinoline alkaloid PM00104 (Zalypsis) in patients with advanced solid tumours Abstract Background: PM00104 binds guanines at DNA minor grooves, impacting DNA replication and transcription. A phase I study was undertaken to investigate safet... |
PMC10597649 | core_pubmed_pmc | Effect of Astragali radix extract on pharmacokinetic behavior of dapagliflozin in healthy and type 2 diabetic rats | Effect of Astragali radix extract on pharmacokinetic behavior of dapagliflozin in healthy and type 2 diabetic rats Abstract Abstract Objective: This study aimed to investigate effect of antidiabetic herb Astragali Radix (AR) on pharmacokinetic behavior of dapagliflozin (DAPA) in healthy rats and type 2 diabetes mellitu... |
PMC3487793 | core_pubmed_pmc | Selected statins produce rapid spinal motor neuron loss in vitro | Selected statins produce rapid spinal motor neuron loss in vitro Abstract Background Hmg-CoA reductase inhibitors (statins) are widely used to prevent disease associated with vascular disease and hyperlipidemia. Although side effects are uncommon, clinical observations suggest statin exposure may exacerbate neuromuscul... |
PMC12378465 | core_pubmed_pmc | Cabotegravir pharmacokinetics in Asians with and without HIV | Cabotegravir pharmacokinetics in Asians with and without HIV Abstract Abstract Objective: Cabotegravir is approved for HIV treatment (with rilpivirine) and prevention. The established cabotegravir population pharmacokinetic (PPK) model included 1.2% Asian participants. We aimed to compare cabotegravir pharmacokinetics ... |
PMC5696449 | core_pubmed_pmc | Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients | Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients Abstract Abstract Introduction Because of the high mortality of invasive fungal infections (IFIs), appropriate exposure to antifungals appears to be crucial for therapeutic efficacy and safety. Materials and methods This re... |
PMC11179702 | core_pubmed_pmc | Population pharmacokinetics and exposure–response analyses of polatuzumab vedotin in patients with previously untreated DLBCL from the POLARIX study | Population pharmacokinetics and exposure–response analyses of polatuzumab vedotin in patients with previously untreated DLBCL from the POLARIX study Abstract Abstract Polatuzumab vedotin is a CD79b‐directed antibody–drug conjugate that targets B cells and delivers the cytotoxic payload monomethyl auristatin E (MMAE). T... |
PMC12449448 | core_pubmed_pmc | A phase 1b, multicentre, dose escalation, safety and pharmacokinetics study of tilvestamab (BGB149) in relapsed, platinum-resistant, high-grade serous ovarian cancer (PROC) patients | A phase 1b, multicentre, dose escalation, safety and pharmacokinetics study of tilvestamab (BGB149) in relapsed, platinum-resistant, high-grade serous ovarian cancer (PROC) patients Abstract Background Tilvestamab is a highly selective humanised immunoglobulin G1 anti-AXL monoclonal antibody. This phase 1 study evaluat... |
PMC12473541 | core_pubmed_pmc | Strategic and Chemical Advances in Antibody–Drug Conjugates | Strategic and Chemical Advances in Antibody–Drug Conjugates Abstract Antibody–drug conjugates (ADCs) are a rapidly advancing class of targeted cancer therapeutics that couple the antigen specificity of monoclonal antibodies (mAbs) with the potent cytotoxicity of small-molecule drugs. In their core design, a tumor-targe... |
PMC7550287 | core_pubmed_pmc | Sub-additive (antagonistic) interaction of lacosamide with lamotrigine and valproate in the maximal electroshock-induced seizure model in mice: an isobolographic analysis | Sub-additive (antagonistic) interaction of lacosamide with lamotrigine and valproate in the maximal electroshock-induced seizure model in mice: an isobolographic analysis Abstract Background Launching polytherapy with two or three antiseizure drugs (ASDs) in patients with epilepsy is still problematic. The choice of AS... |
PMC10239696 | core_pubmed_pmc | A cheminformatics-biophysics correlate to identify promising lead molecules against matrix metalloproteinase-2 (MMP-2) enzyme: A promising anti-cancer target | A cheminformatics-biophysics correlate to identify promising lead molecules against matrix metalloproteinase-2 (MMP-2) enzyme: A promising anti-cancer target Abstract Abstract Matrix metalloproteinase-2 (MMP-2) is an endopeptidase enzyme that is devoted to extracellular matrix proteins degradation. The enzyme is warran... |
PMC9605917 | core_pubmed_pmc | An integrative analysis of Qingfei Paidu Decoction for its anti-HCoV-229E mechanism in cold and damp environment based on the pharmacokinetics, metabolomics and molecular docking technology | An integrative analysis of Qingfei Paidu Decoction for its anti-HCoV-229E mechanism in cold and damp environment based on the pharmacokinetics, metabolomics and molecular docking technology Abstract Background The novel coronavirus pneumonia (COVID-19) has spread rapidly around the world. As a member against the epidem... |
PMC8135083 | core_pubmed_pmc | Pharmacokinetics and safety of TCMCB07, a melanocortin‐4 antagonist peptide in dogs | Pharmacokinetics and safety of TCMCB07, a melanocortin‐4 antagonist peptide in dogs Abstract Abstract The melanocortin‐4 receptor (MC4R) antagonistic peptide TCMCB07 was developed for the treatment of cachexia. The objectives of this study were to examine pharmacokinetics and safety of TCMCB07 administered subcutaneous... |
PMC9026114 | core_pubmed_pmc | Micelle/Hydrogel Composite as a “Natural Self-Emulsifying Reversible Hybrid Hydrogel (N’SERH)” Enhances the Oral Bioavailability of Free (Unconjugated) Resveratrol | Micelle/Hydrogel Composite as a “Natural Self-Emulsifying Reversible Hybrid Hydrogel (N’SERH)” Enhances the Oral Bioavailability of Free (Unconjugated) Resveratrol Abstract The poor oral bioavailability, rapid biotransformation to less active metabolites, and fast elimination from systemic circulation have been identif... |
PMC9978810 | core_pubmed_pmc | Modeling antibody dynamics following herpes zoster indicates that higher varicella-zoster virus viremia generates more VZV-specific antibodies | Modeling antibody dynamics following herpes zoster indicates that higher varicella-zoster virus viremia generates more VZV-specific antibodies Abstract Introduction Studying antibody dynamics following re-exposure to infection and/or vaccination is crucial for a better understanding of fundamental immunological process... |
PMC8110503 | core_pubmed_pmc | There is Only One Valid Definition of Clearance: Critical Examination of Clearance Concepts Reveals the Potential for Errors in Clinical Drug Dosing Decisions | There is Only One Valid Definition of Clearance: Critical Examination of Clearance Concepts Reveals the Potential for Errors in Clinical Drug Dosing Decisions Abstract Abstract Drug dosing decisions in clinical medicine and in introducing a drug to market for the past 60 years are based on the pharmacokinetic/clinical ... |
PMC12937849 | core_pubmed_pmc | Oritavancin for Gram-Positive Bone and Joint Infections: A Comprehensive Review of the Literature | Oritavancin for Gram-Positive Bone and Joint Infections: A Comprehensive Review of the Literature Abstract Background: Bone and joint infections (BJIs), including osteomyelitis, septic arthritis, and periprosthetic joint infections, typically require prolonged antimicrobial therapy and often involve complex outpatient ... |
PMC3221297 | core_pubmed_pmc | Communicating trends in resistance using a drug resistance index | Communicating trends in resistance using a drug resistance index Abstract Abstract Background Antibiotic resistance is a growing problem worldwide, but communicating this challenge to policymakers and non-experts is complicated by the multiplicity of bacterial pathogens and the distinct classes of antibiotics used to t... |
PMC11728769 | core_pubmed_pmc | Description and Modeling of Relevant Demographic and Laboratory Variables in a Large Oncology Cohort to Generate Virtual Populations | Description and Modeling of Relevant Demographic and Laboratory Variables in a Large Oncology Cohort to Generate Virtual Populations Abstract Abstract Background/Objectives : Pathophysiological variability in patients with cancer is associated with differences in responses to pharmacotherapy. In this work, we aimed to ... |
PMC12031879 | core_pubmed_pmc | The Beta‐Blocker Pharmacogenetic Puzzle: More Pieces of Evidence for Pharmacodynamic Candidate Variants | The Beta‐Blocker Pharmacogenetic Puzzle: More Pieces of Evidence for Pharmacodynamic Candidate Variants Abstract ABSTRACT Previous pharmacogenetic findings for beta‐blocker pharmacodynamic candidate genes ( ADRB1 , ADRB2 , ADRA2C, GRK4, and GRK5) have been inconsistent. Therefore, the purpose of this study was to deter... |
PMC12472474 | core_pubmed_pmc | Comparative Pharmacological and Pharmaceutical Perspectives on Antidiabetic Therapies in Humans, Dogs, and Cats | Comparative Pharmacological and Pharmaceutical Perspectives on Antidiabetic Therapies in Humans, Dogs, and Cats Abstract Abstract Background/Objectives: Diabetes mellitus (DM) is an increasingly prevalent endocrine disorder affecting humans and companion animals. Type 1 DM (T1DM) and type 2 DM (T2DM) are well character... |
PMC10799622 | core_pubmed_pmc | Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting | Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting Abstract Abstract Background Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, sever... |
PMC8413969 | core_pubmed_pmc | High-dose IL-2/CD25 fusion protein amplifies vaccine-induced CD4 + and CD8 + neoantigen-specific T cells to promote antitumor immunity | High-dose IL-2/CD25 fusion protein amplifies vaccine-induced CD4 + and CD8 + neoantigen-specific T cells to promote antitumor immunity Abstract Background Immunization with tumor neoantigens is a promising vaccine approach to promote antitumor immunity due to their high immunogenicity, lack of expression in normal tiss... |
PMC12277590 | core_pubmed_pmc | Decoding Drug Interactions: Character and Degree of Pharmacokinetic Interactions Between Telmisartan and Sorafenib or Donafenib in Rats | Decoding Drug Interactions: Character and Degree of Pharmacokinetic Interactions Between Telmisartan and Sorafenib or Donafenib in Rats Abstract Abstract Background Sorafenib and lenvatinib play a significant role as small molecule targeted drugs in the treatment of advanced hepatocellular carcinoma. However, both drug... |
PMC7318030 | core_pubmed_pmc | A Phase 2 Randomized, Double-Blind, Placebo-Controlled Trial of MHAA4549A, a Monoclonal Antibody, plus Oseltamivir in Patients Hospitalized with Severe Influenza A Virus Infection | A Phase 2 Randomized, Double-Blind, Placebo-Controlled Trial of MHAA4549A, a Monoclonal Antibody, plus Oseltamivir in Patients Hospitalized with Severe Influenza A Virus Infection Abstract For patients hospitalized with severe influenza A virus infection, morbidity and mortality remain high. MHAA4549A, a human monoclon... |
PMC10876765 | core_pubmed_pmc | Modified medication use in dysphagia: the effect of thickener on drug bioavailability—a systematic review | Modified medication use in dysphagia: the effect of thickener on drug bioavailability—a systematic review Abstract Key summary points Aim To understand further the effect of thickener on medications and their pharmacokinetic and therapeutic profiles, using a literature search. Findings Despite dysphagia and polypharmac... |
PMC3356326 | core_pubmed_pmc | Quantitative Analysis and Comparison Study of [ 18 F]AlF-NOTA-PRGD2, [ 18 F]FPPRGD2 and [ 68 Ga]Ga-NOTA-PRGD2 Using a Reference Tissue Model | Quantitative Analysis and Comparison Study of [ 18 F]AlF-NOTA-PRGD2, [ 18 F]FPPRGD2 and [ 68 Ga]Ga-NOTA-PRGD2 Using a Reference Tissue Model Abstract With favorable pharmacokinetics and binding affinity for α v β 3 integrin, 18 F-labeled dimeric cyclic RGD peptide ([ 18 F]FPPRGD2) has been intensively used as a PET ima... |
PMC12015869 | core_pubmed_pmc | Retrospective Bayesian Reanalysis of Single Gentamicin Concentrations: A Neonatal Case Series | Retrospective Bayesian Reanalysis of Single Gentamicin Concentrations: A Neonatal Case Series Abstract Background/Objectives : Nomograms for adjusting gentamicin therapy in neonates using a single concentration are limited. The Dersch–Mills nomogram is inefficient for short-duration therapies, while the NeoFax nomogram... |
PMC4413526 | core_pubmed_pmc | Cobicistat-boosted darunavir in HIV-1-infected adults: week 48 results of a Phase IIIb, open-label single-arm trial | Cobicistat-boosted darunavir in HIV-1-infected adults: week 48 results of a Phase IIIb, open-label single-arm trial Abstract Abstract Background Cobicistat is an alternative pharmacoenhancer to ritonavir. In healthy volunteers, darunavir exposure was comparable when darunavir 800 mg once daily was co-administered with ... |
PMC9653415 | core_pubmed_pmc | A simple label-free method reveals bacterial growth dynamics and antibiotic action in real-time | A simple label-free method reveals bacterial growth dynamics and antibiotic action in real-time Abstract Understanding the response of bacteria to environmental stress is hampered by the relative insensitivity of methods to detect growth. This means studies of antibiotic resistance and other physiological methods often... |
PMC12974557 | core_pubmed_pmc | Leveraging Two‐Stage δ Global Sensibility Analysis Method to Inform Parameter Estimation in PBPK Models | Leveraging Two‐Stage δ Global Sensibility Analysis Method to Inform Parameter Estimation in PBPK Models Abstract ABSTRACT Appropriately performing Global Sensitivity Analysis (GSA) and refining models through the estimation of key parameters on individual data are fundamental steps in PBPK modeling, yet they remain ins... |
PMC5351008 | core_pubmed_pmc | Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction | Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction Abstract Abstract Acebilustat is a new once‐daily oral antiinflammatory drug in development for treatment of cystic fibrosis (CF) and other diseases. It is an inhibitor of leukotriene A4 hydrolase; therefore, production... |
PMC6379231 | core_pubmed_pmc | Optimization of dosing regimens of isoniazid and rifampicin in children with tuberculosis in India | Optimization of dosing regimens of isoniazid and rifampicin in children with tuberculosis in India Abstract Abstract Aims Pharmacokinetic studies in the past have shown inadequate antituberculosis drug levels in children with the currently available dosing regimens. This study attempted to investigate the pharmacokinet... |
PMC9704105 | core_pubmed_pmc | In vivo pharmacokinetic and pharmacodynamic study of co-spray-dried inhalable pirfenidone microparticles in rats | In vivo pharmacokinetic and pharmacodynamic study of co-spray-dried inhalable pirfenidone microparticles in rats Abstract Abstract Pirfenidone (PRF) is the first FDA-approved API in the treatment of idiopathic pulmonary fibrosis (IPF). However, PRF induces serious side effects, such as photophobia and gastrointestinal ... |
PMC9403502 | core_pubmed_pmc | Localization of drug biodistribution in a 3D-bioengineered subcutaneous neovascularized microenvironment | Localization of drug biodistribution in a 3D-bioengineered subcutaneous neovascularized microenvironment Abstract Local immunomodulation has shown the potential to control the immune response in a site-specific manner for wound healing, cancer, allergy, and cell transplantation, thus abrogating adverse effects associat... |
PMC10514787 | core_pubmed_pmc | Community Pharmacists’ Knowledge, Attitudes and the Perceived Safety and Effectiveness of Melatonin Supplements: A Cross-Sectional Survey | Community Pharmacists’ Knowledge, Attitudes and the Perceived Safety and Effectiveness of Melatonin Supplements: A Cross-Sectional Survey Abstract Abstract Melatonin, which is classified as a dietary supplement by the Saudi Food and Drug Authority, is used to manage sleep disorders. In this study, community pharmacists... |
PMC7096243 | core_pubmed_pmc | A Preliminary Study on the Establishment of the PDTX Model | A Preliminary Study on the Establishment of the PDTX Model Abstract Abstract Objective The current study aims to explore the establishment of the patient-derived tumor xenograft (PDTX) model. Materials and Methods Twenty patients with gastric cancer, 10 males and 10 females, were enrolled in the current study. Firstly,... |
PMC7698315 | core_pubmed_pmc | Bioanalytical Assay Development and Validation for the Pharmacokinetic Study of GMC1, a Novel FKBP52 Co-chaperone Inhibitor for Castration Resistant Prostate Cancer | Bioanalytical Assay Development and Validation for the Pharmacokinetic Study of GMC1, a Novel FKBP52 Co-chaperone Inhibitor for Castration Resistant Prostate Cancer Abstract Background: GMC1 (2-(1H-benzimidazol-2-ylsulfanyl)- N -[(Z)-(4-methoxyphenyl) methylideneamino] acetamide) effectively inhibits androgen receptor ... |
PMC6207397 | core_pubmed_pmc | CYP3A5 genotype-based model to predict tacrolimus dosage in the early postoperative period after living donor liver transplantation | CYP3A5 genotype-based model to predict tacrolimus dosage in the early postoperative period after living donor liver transplantation Abstract Purpose Liver transplantation is the treatment of choice for patients with end-stage liver disease. Due to the between- and within-individual pharmacokinetic variability in tacrol... |
PMC3889505 | core_pubmed_pmc | Importance of hematocrit for a tacrolimus target concentration strategy | Importance of hematocrit for a tacrolimus target concentration strategy Abstract Abstract Purpose To identify patient characteristics that influence tacrolimus individual dose requirement in kidney transplant recipients. Methods Data on forty-four 12-h pharmacokinetic profiles from 29 patients and trough concentrations... |
PMC5971566 | core_pubmed_pmc | Population Pharmacokinetic Analyses for Rezafungin (CD101) Efficacy Using Phase 1 Data | Population Pharmacokinetic Analyses for Rezafungin (CD101) Efficacy Using Phase 1 Data Abstract ABSTRACT Rezafungin (CD101) is a novel echinocandin antifungal agent currently in clinical development for the treatment of candidemia and invasive candidiasis. Rezafungin has potent in vitro activity against Candida albican... |
PMC5599467 | core_pubmed_pmc | Assessment of Pharmacokinetic Interactions Between Obeticholic Acid and Caffeine, Midazolam, Warfarin, Dextromethorphan, Omeprazole, Rosuvastatin, and Digoxin in Phase 1 Studies in Healthy Subjects | Assessment of Pharmacokinetic Interactions Between Obeticholic Acid and Caffeine, Midazolam, Warfarin, Dextromethorphan, Omeprazole, Rosuvastatin, and Digoxin in Phase 1 Studies in Healthy Subjects Abstract Introduction Obeticholic acid (OCA), a potent and selective farnesoid X receptor agonist, is indicated for the tr... |
PMC6220930 | core_pubmed_pmc | Population PK and Exposure–Response Relationships for the Antibody–Drug Conjugate Brentuximab Vedotin in CTCL Patients in the Phase III ALCANZA Study | Population PK and Exposure–Response Relationships for the Antibody–Drug Conjugate Brentuximab Vedotin in CTCL Patients in the Phase III ALCANZA Study Abstract Abstract The antibody–drug conjugate (ADC) brentuximab vedotin consists of the CD30‐directed antibody attached to the microtubule‐disrupting agent monomethyl aur... |
PMC11313719 | core_pubmed_pmc | Knowledge of Food–Drug Interactions among Medical University Students | Knowledge of Food–Drug Interactions among Medical University Students Abstract Background: Food–drug interactions (FDIs) may alter drug pharmacokinetics and pharmacodynamics, modifying the whole therapy’s effectiveness. Some of them cause the attenuation of drug effects, while others inhibit the medicines’ metabolism r... |
PMC7550380 | core_pubmed_pmc | Drug–Drug Interactions with Antiretroviral Drugs in Pregnant Women Living with HIV: Are They Different from Non-Pregnant Individuals? | Drug–Drug Interactions with Antiretroviral Drugs in Pregnant Women Living with HIV: Are They Different from Non-Pregnant Individuals? Abstract Background and Objective Although the separate effects of drug–drug interactions and pregnancy on antiretroviral drug pharmacokinetics have been widely studied and described, th... |
PMC4648507 | core_pubmed_pmc | Miltefosine Lipid Nanocapsules for Single Dose Oral Treatment of Schistosomiasis Mansoni: A Preclinical Study | Miltefosine Lipid Nanocapsules for Single Dose Oral Treatment of Schistosomiasis Mansoni: A Preclinical Study Abstract Abstract Miltefosine (MFS) is an alkylphosphocholine used for the local treatment of cutaneous metastases of breast cancer and oral therapy of visceral leishmaniasis. Recently, the drug was reported in... |
PMC5039936 | core_pubmed_pmc | Physiologically based and population PK modeling in optimizing drug development: A predict–learn–confirm analysis | Physiologically based and population PK modeling in optimizing drug development: A predict–learn–confirm analysis Abstract Abstract Physiologically based pharmacokinetic (PBPK) modeling and classical population pharmacokinetic (PK) model‐based simulations are increasingly used to answer various drug development questio... |
PMC3056416 | core_pubmed_pmc | Cannabinoid system and cyclooxygenases inhibitors | Cannabinoid system and cyclooxygenases inhibitors Abstract Abstract Rationale. The cannabinoid system consists of a complex array of receptors, substances with agonist/antagonist properties for those receptors, biosynthetic machineries and mechanisms for cellular uptake and degradation for endocannabinoids. This system... |
PMC6606825 | core_pubmed_pmc | Impact of NR1I2 , adenosine triphosphate–binding cassette transporters genetic polymorphisms on the pharmacokinetics of ginsenoside compound K in healthy Chinese volunteers | Impact of NR1I2 , adenosine triphosphate–binding cassette transporters genetic polymorphisms on the pharmacokinetics of ginsenoside compound K in healthy Chinese volunteers Abstract Background Ginsenoside compound K (CK) is a promising drug candidate for rheumatoid arthritis. This study examined the impact of polymorph... |
PMC6989223 | core_pubmed_pmc | Understanding the pharmacokinetics of prodrug and metabolite | Understanding the pharmacokinetics of prodrug and metabolite Abstract This tutorial explains the pharmacokinetics of a prodrug and its active metabolite (or parent drug) using a two-step, consecutive, first-order irreversible reaction as a basic model for prodrug metabolism. In this model, the prodrug is metabolized an... |
PMC10017418 | core_pubmed_pmc | BJTJ-1837, a novel FXI activation-blocking antibody | BJTJ-1837, a novel FXI activation-blocking antibody Abstract Abstract Background Factor (F)XI contributes to thrombosis development while it plays a limited role in normal hemostasis. FXI targeting has the potential for preventing and treating thrombosis with little bleeding risk. Objectives The aim of this study was t... |
PMC5417014 | core_pubmed_pmc | A quantitative mechanistic PK/PD model directly connects Btk target engagement and in vivo efficacy † | A quantitative mechanistic PK/PD model directly connects Btk target engagement and in vivo efficacy † Abstract Correlating target engagement with in vivo drug activity remains a central challenge in efforts to improve the efficiency of drug discovery. Abstract Correlating target engagement with in vivo drug activity re... |
PMC12489372 | core_pubmed_pmc | Pharmacokinetic analysis of morphine-3-glucuronide after acute morphine intravenous bolus administration to rats with traumatic brain injury | Pharmacokinetic analysis of morphine-3-glucuronide after acute morphine intravenous bolus administration to rats with traumatic brain injury Abstract This study investigates the effects of traumatic brain injury (TBI) on the pharmacokinetics of morphine and its metabolite, morphine-3-glucuronide (M3G), and their influe... |
PMC6389038 | core_pubmed_pmc | Short-term effects of ambient fine particulate matter pollution on hospital visits for chronic obstructive pulmonary disease in Beijing, China | Short-term effects of ambient fine particulate matter pollution on hospital visits for chronic obstructive pulmonary disease in Beijing, China Abstract Abstract Background Little is known about the effect of ambient fine particulate matter (PM 2.5 ) on chronic obstructive pulmonary disease (COPD) in China. The objectiv... |
PMC10229459 | core_pubmed_pmc | Results from a first-in-human study of dersimelagon, an investigational oral selective MC1R agonist | Results from a first-in-human study of dersimelagon, an investigational oral selective MC1R agonist Abstract Purpose To describe outcomes from the first-in-human study of dersimelagon, an investigational oral selective MC1R agonist, under development for the treatment of erythropoietic protoporphyria (EPP) and X-linked... |
PMC9796269 | core_pubmed_pmc | Phase 1 safety, tolerability, pharmacokinetics and pharmacodynamics results of a long‐acting C‐type natriuretic peptide prodrug, TransCon CNP | Phase 1 safety, tolerability, pharmacokinetics and pharmacodynamics results of a long‐acting C‐type natriuretic peptide prodrug, TransCon CNP Abstract Aim TransCon CNP is a novel prodrug designed to provide sustained release of C‐type natriuretic peptide (CNP) for once‐weekly therapy, addressing the pathology leading t... |
PMC12655041 | core_pubmed_pmc | Anemoside B4 Rectal Thermosensitive In Situ Gel to Treat Ulcerative Colitis by Overcoming Oral Bioavailability Barriers with Absorption Enhancer-Assisted Delivery | Anemoside B4 Rectal Thermosensitive In Situ Gel to Treat Ulcerative Colitis by Overcoming Oral Bioavailability Barriers with Absorption Enhancer-Assisted Delivery Abstract Background: Anemoside B4 (AB4), the major bioactive saponin from Pulsatilla chinensis, exhibits anti-inflammatory, anti-tumor, anti-apoptotic, and a... |
PMC8734216 | core_pubmed_pmc | vCOMBAT: a novel tool to create and visualize a computational model of bacterial antibiotic target-binding | vCOMBAT: a novel tool to create and visualize a computational model of bacterial antibiotic target-binding Abstract Abstract Background As antibiotic resistance creates a significant global health threat, we need not only to accelerate the development of novel antibiotics but also to develop better treatment strategies... |
PMC8445934 | core_pubmed_pmc | Transformation of tenofovir into stable ProTide nanocrystals with long-acting pharmacokinetic profiles | Transformation of tenofovir into stable ProTide nanocrystals with long-acting pharmacokinetic profiles Abstract Abstract Treatment and prevention of human immunodeficiency virus type one (HIV-1) infection was transformed through widespread use of antiretroviral therapy (ART). However, ART has limitations in requiring l... |
PMC12547747 | core_pubmed_pmc | Steroidal Alkaloids from Sarcococca saligna (Buxaceae): In Vitro and In Silico Evaluation of Their Cytotoxic Potential | Steroidal Alkaloids from Sarcococca saligna (Buxaceae): In Vitro and In Silico Evaluation of Their Cytotoxic Potential Abstract Sarcococca saligna ( S. saligna ), a medicinal shrub rich in therapeutic steroidal alkaloids (SAs), is ethnomedicinally used to treat ulcers, tumors, and wounds. In this study, to explore the ... |
PMC11364104 | core_pubmed_pmc | Discovery of SARS-CoV-2 papain-like protease (PL pro ) inhibitors with efficacy in a murine infection model | Discovery of SARS-CoV-2 papain-like protease (PL pro ) inhibitors with efficacy in a murine infection model Abstract Abstract Vaccines and first-generation antiviral therapeutics have provided important protection against COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, there re... |
PMC10703858 | core_pubmed_pmc | A simple and green capillary electrophoresis-mass spectrometry method for therapeutic drug monitoring of colistin in clinical plasma samples | A simple and green capillary electrophoresis-mass spectrometry method for therapeutic drug monitoring of colistin in clinical plasma samples Abstract Abstract Colistin and other polymyxin antibiotics have become increasingly used in clinical settings as a result of treating multidrug-resistant infections in critically ... |
PMC7979583 | core_pubmed_pmc | Population pharmacokinetics and pharmacodynamics of a novel vascular adhesion protein-1 inhibitor using a multiple-target mediated drug disposition model | Population pharmacokinetics and pharmacodynamics of a novel vascular adhesion protein-1 inhibitor using a multiple-target mediated drug disposition model Abstract Abstract ASP8232 is a novel inhibitor of vascular adhesion protein-1 that was under evaluation for reducing residual albuminuria in patients with diabetic ki... |
PMC7478952 | core_pubmed_pmc | Mechanistic Multilayer Quantitative Model for Nonlinear Pharmacokinetics, Target Occupancy and Pharmacodynamics (PK/TO/PD) Relationship of D-Amino Acid Oxidase Inhibitor, TAK-831 in Mice | Mechanistic Multilayer Quantitative Model for Nonlinear Pharmacokinetics, Target Occupancy and Pharmacodynamics (PK/TO/PD) Relationship of D-Amino Acid Oxidase Inhibitor, TAK-831 in Mice Abstract Purpose TAK-831 is a highly selective and potent inhibitor of D-amino acid oxidase (DAAO) currently under clinical developme... |
PMC11839822 | core_pubmed_pmc | Residue depletion profile and withdrawal interval estimation of ivermectin in eggs following topical administration of injectable ivermectin to domestic chickens ( Gallus domesticus ): a pilot study | Residue depletion profile and withdrawal interval estimation of ivermectin in eggs following topical administration of injectable ivermectin to domestic chickens ( Gallus domesticus ): a pilot study Abstract Abstract Introduction Topical ivermectin is commonly prescribed extra-label for the control of mite infestations... |
PMC12009570 | core_pubmed_pmc | Functional Liposomes Improve the Oral Absorption of Lurasidone Hydrochloride by Overcoming Multiple Absorption Barriers and Eliminating Food Effect | Functional Liposomes Improve the Oral Absorption of Lurasidone Hydrochloride by Overcoming Multiple Absorption Barriers and Eliminating Food Effect Abstract Purpose Mental illness is the leading cause of the global burden of non-fatal disease. Lurasidone hydrochloride (LSD) is an important antipsychotic drug, but has p... |
PMC11782438 | core_pubmed_pmc | Improving Understanding of Fexofenadine Pharmacokinetics to Assess Pgp Phenotypic Activity in Older Adult Patients Using Population Pharmacokinetic Modeling | Improving Understanding of Fexofenadine Pharmacokinetics to Assess Pgp Phenotypic Activity in Older Adult Patients Using Population Pharmacokinetic Modeling Abstract Abstract Background and Objective Fexofenadine is commonly used as a probe substrate to assess P-glycoprotein (Pgp) activity. While its use in healthy vol... |
PMC5947523 | core_pubmed_pmc | Effect of Chronic Kidney Disease on Nonrenal Elimination Pathways: A Systematic Assessment of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and OATP | Effect of Chronic Kidney Disease on Nonrenal Elimination Pathways: A Systematic Assessment of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and OATP Abstract Our recent studies have shown that chronic kidney disease (CKD) affects the pharmacokinetics (PKs) of cytochrome P450 (CYP)2D6‐metabolized drugs, whereas effects were less evi... |
PMC6028879 | core_pubmed_pmc | Characterization of the Pharmacokinetics of Vilaprisan: Bioavailability, Excretion, Biotransformation, and Drug–Drug Interaction Potential | Characterization of the Pharmacokinetics of Vilaprisan: Bioavailability, Excretion, Biotransformation, and Drug–Drug Interaction Potential Abstract Background and objectives In-vitro data suggest that clearance of vilaprisan is mediated by cytochrome P450 3A4 (oxidation) and aldoketoreductases (reduction). To fully und... |
PMC12671744 | core_pubmed_pmc | Pharmacokinetic profiles of Moutan Cortex after single and repeated administration in a dinitrobenzene sulfonic acid-induced colitis model | Pharmacokinetic profiles of Moutan Cortex after single and repeated administration in a dinitrobenzene sulfonic acid-induced colitis model Abstract Abstract Moutan Cortex (MC), the dried root bark of Paeonia suffruticosa , is used in traditional Chinese and Korean medicine to treat enteritis for its anti-inflammatory p... |
PMC11211351 | core_pubmed_pmc | Construction of warfarin population pharmacokinetics and pharmacodynamics model in Han population based on Bayesian method | Construction of warfarin population pharmacokinetics and pharmacodynamics model in Han population based on Bayesian method Abstract The purpose of this paper is to study the genetic polymorphisms of related gene loci (CYP2C9*3, VKORC1-1639G > A) based on demographic and clinical factors, and use the maximum a posterior... |
PMC4468904 | core_pubmed_pmc | Pharmacogenomic and clinical data link non-pharmacokinetic metabolic dysregulation to drug side effect pathogenesis | Pharmacogenomic and clinical data link non-pharmacokinetic metabolic dysregulation to drug side effect pathogenesis Abstract Abstract Drug side effects cause a significant clinical and economic burden. However, mechanisms of drug action underlying side effect pathogenesis remain largely unknown. Here, we integrate phar... |
PMC7726197 | core_pubmed_pmc | In silico Assessment of Pharmacological Profile of Low Molecular Weight Oligo-Hydroxyalkanoates | In silico Assessment of Pharmacological Profile of Low Molecular Weight Oligo-Hydroxyalkanoates Abstract Abstract Polyhydroxyalkanoates (PHAs) are a large class of polyesters that are biosynthesized by microorganisms at large molecular weights ( Mw > 80 kDa) and have a great potential for medical applications because o... |
PMC8048879 | core_pubmed_pmc | How Semiphysiological Population Pharmacokinetic Modeling Incorporating Active Hepatic Uptake Supports Phase II Dose Selection of RO7049389, A Novel Anti–Hepatitis B Virus Drug | How Semiphysiological Population Pharmacokinetic Modeling Incorporating Active Hepatic Uptake Supports Phase II Dose Selection of RO7049389, A Novel Anti–Hepatitis B Virus Drug Abstract The pharmacokinetics (PK) of RO7049389, a new hepatitis B virus (HBV) core protein allosteric modulator of class I, and of its active ... |
PMC12131413 | core_pubmed_pmc | Use of Hoteling’s T 2 multivariate control chart for effective monitoring of a laboratory test with a 3-level quality control scheme | Use of Hoteling’s T 2 multivariate control chart for effective monitoring of a laboratory test with a 3-level quality control scheme Abstract Introduction A control chart based on Hotelling’s T 2 multivariate statistics was used to monitor the quality of an immunoenzymatic assay for plasma levetiracetam. The chart inco... |
PMC9906379 | core_pubmed_pmc | Phase 1 first-in-human study of dalutrafusp alfa, an anti–CD73-TGF-β-trap bifunctional antibody, in patients with advanced solid tumors | Phase 1 first-in-human study of dalutrafusp alfa, an anti–CD73-TGF-β-trap bifunctional antibody, in patients with advanced solid tumors Abstract Abstract Background Cluster of differentiation (CD)73-adenosine and transforming growth factor (TGF)-β pathways are involved in abrogated antitumor immune responses and can le... |
PMC12704187 | core_pubmed_pmc | A Step Toward Precision Dosing of Escitalopram in Chinese Patients: An External Evaluation of Published Population Pharmacokinetic Models | A Step Toward Precision Dosing of Escitalopram in Chinese Patients: An External Evaluation of Published Population Pharmacokinetic Models Abstract Objective This study aims to evaluate the predictive performance of the published population pharmacokinetic (PopPK) model of escitalopram in Chinese patients using an exter... |
PMC10386937 | core_pubmed_pmc | Semi-physiological Enriched Population Pharmacokinetic Modelling to Predict the Effects of Pregnancy on the Pharmacokinetics of Cytotoxic Drugs | Semi-physiological Enriched Population Pharmacokinetic Modelling to Predict the Effects of Pregnancy on the Pharmacokinetics of Cytotoxic Drugs Abstract Background and Objective As a result of changes in physiology during pregnancy, the pharmacokinetics (PK) of drugs can be altered. It is unclear whether under- or over... |
PMC9015998 | core_pubmed_pmc | Non-clinical Pharmacology of YTX-7739: a Clinical Stage Stearoyl-CoA Desaturase Inhibitor Being Developed for Parkinson’s Disease | Non-clinical Pharmacology of YTX-7739: a Clinical Stage Stearoyl-CoA Desaturase Inhibitor Being Developed for Parkinson’s Disease Abstract Stearoyl-CoA desaturase (SCD) is a potential therapeutic target for Parkinson’s and related neurodegenerative diseases. SCD inhibition ameliorates neuronal toxicity caused by aberra... |
PMC5944627 | core_pubmed_pmc | A Preclinical Population Pharmacokinetic Model for Anti‐CD20/CD3 T‐Cell‐Dependent Bispecific Antibodies | A Preclinical Population Pharmacokinetic Model for Anti‐CD20/CD3 T‐Cell‐Dependent Bispecific Antibodies Abstract Abstract CD20 is a cell‐surface receptor expressed by healthy and neoplastic B cells and is a well‐established target for biologics used to treat B‐cell malignancies. Pharmacokinetic (PK) and pharmacodynamic... |
PMC12341985 | core_pubmed_pmc | A multi-scale semi-mechanistic CK/PD model for CAR T-cell therapy | A multi-scale semi-mechanistic CK/PD model for CAR T-cell therapy Abstract Abstract Chimeric antigen receptor T (CAR T) cell therapy has shown remarkable success in treating various leukemias and lymphomas. Cellular kinetic (CK) and pharmacodynamic (PD) behavior of CAR T cell therapy is distinct from other therapies du... |
PMC12236148 | core_pubmed_pmc | Bioanalytical method development and validation for determination of olutasidenib and its application to pharmacokinetic studies | Bioanalytical method development and validation for determination of olutasidenib and its application to pharmacokinetic studies Abstract Abstract Olutasidenib is an inhibitor licensed by the FDA, indicated against mutations in isocitrate dehydrogenase-1 (IDH1). For individuals with vulnerable IDH1 mutations, it has be... |
PMC8981079 | core_pubmed_pmc | Identification of absorbed compounds of Xiao Yao San Jia Wei and pharmacokinetic study in depressed rats by force swimming stress † | Identification of absorbed compounds of Xiao Yao San Jia Wei and pharmacokinetic study in depressed rats by force swimming stress † Abstract Abstract Xiao-Yao-San-Jia-Wei (XYSJW) is a commonly prescribed formulation for depression and anorexia in the Jiang Su Province Hospital of Chinese Medicine. Unfortunately, the pr... |
PMC10973052 | core_pubmed_pmc | Long-term safety and efficacy of cipaglucosidase alfa plus miglustat in individuals living with Pompe disease: an open-label phase I/II study (ATB200-02) | Long-term safety and efficacy of cipaglucosidase alfa plus miglustat in individuals living with Pompe disease: an open-label phase I/II study (ATB200-02) Abstract Cipaglucosidase alfa plus miglustat (cipa + mig) is a novel, two-component therapy for Pompe disease. We report data from the Phase I/II ATB200-02 study for ... |
PMC11992655 | core_pubmed_pmc | The new big is small: Leveraging knowledge from small trials for rare disease drug development: Blarcamesine for Rett syndrome | The new big is small: Leveraging knowledge from small trials for rare disease drug development: Blarcamesine for Rett syndrome Abstract Big data in drug development may not satisfactorily address the demands of precision medicine in a rare disease population, making the use of smaller clinical trials necessary. Consequ... |
PMC3826324 | core_pubmed_pmc | NCCAM/NCI Phase 1 Study of Mistletoe Extract and Gemcitabine in Patients with Advanced Solid Tumors | NCCAM/NCI Phase 1 Study of Mistletoe Extract and Gemcitabine in Patients with Advanced Solid Tumors Abstract Abstract Purpose. European Mistletoe ( Viscum album L.) extracts (mistletoe) are commonly used for cancer treatment in Europe. This phase I study of gemcitabine (GEM) and mistletoe in advanced solid cancers (ASC... |
PMC12706397 | core_pubmed_pmc | The Evolving Role of In Vitro–In Vivo Correlation in Model‐Informed Drug Development: A Multi‐Stakeholder Perspective | The Evolving Role of In Vitro–In Vivo Correlation in Model‐Informed Drug Development: A Multi‐Stakeholder Perspective Abstract ABSTRACT In vitro–in vivo correlation/relationship (IVIVC/R) models such as physiologically based biopharmaceutics modeling (PBBM) are crucial tools that link biopharmaceutical properties to cl... |
PMC10196439 | core_pubmed_pmc | PBPK modeling of ivermectin—Considerations for the purpose of developing alternative routes to optimize its safety profile | PBPK modeling of ivermectin—Considerations for the purpose of developing alternative routes to optimize its safety profile Abstract Abstract Although single‐dose ivermectin has been widely used in mass‐drug administration programs for onchocerciasis and lymphatic filariasis for many years, ivermectin may have utility a... |
PMC8138871 | core_pubmed_pmc | Antibody Format and Serum Disposition Govern Ocular Pharmacokinetics of Intravenously Administered Protein Therapeutics | Antibody Format and Serum Disposition Govern Ocular Pharmacokinetics of Intravenously Administered Protein Therapeutics Abstract Protein therapeutics have witnessed tremendous use and application in recent years in treatment of various diseases. Predicting efficacy and safety during drug discovery and translational dev... |
PMC10088082 | core_pubmed_pmc | Tiered approach to evaluate the CYP3A victim and perpetrator drug–drug interaction potential for vonoprazan using PBPK modeling and clinical data to inform labeling | Tiered approach to evaluate the CYP3A victim and perpetrator drug–drug interaction potential for vonoprazan using PBPK modeling and clinical data to inform labeling Abstract Abstract Vonoprazan is metabolized extensively through CYP3A and is an in vitro time‐dependent inhibitor of CYP3A. A tiered approach was applied t... |
PMC5295419 | core_pubmed_pmc | Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma | Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma Abstract The bromodomain inhibitor OTX015 (MK-8628) has shown anti-lymphoma activity as a single agent in both the preclinical and clinical settings, as well as in vitro synergism with several antica... |
PMC7830787 | core_pubmed_pmc | High-Performance Liquid Chromatography-Tandem Mass Spectrometry for Buprenorphine Evaluation in Plasma—Application to Pharmacokinetic Studies in Rabbits | High-Performance Liquid Chromatography-Tandem Mass Spectrometry for Buprenorphine Evaluation in Plasma—Application to Pharmacokinetic Studies in Rabbits Abstract Abstract The precise and reliable determination of buprenorphine concentration is fundamental in certain medical or research applications, particularly in pha... |
PMC4046089 | core_pubmed_pmc | Population pharmacokinetics of mefloquine, administered as a fixed-dose combination of artesunate-mefloquine in Indian patients for the treatment of acute uncomplicated Plasmodium falciparum malaria | Population pharmacokinetics of mefloquine, administered as a fixed-dose combination of artesunate-mefloquine in Indian patients for the treatment of acute uncomplicated Plasmodium falciparum malaria Abstract Background Fixed-dose combinations of artemisinin combination therapy are strongly recommended to facilitate dru... |
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