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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...