id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC10501348 | core_pubmed_pmc | Inadequate Lopinavir Concentrations With Modified 8-hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV | Inadequate Lopinavir Concentrations With Modified 8-hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV Abstract Abstract Background Lopinavir/ritonavir plasma concentrations are profoundly reduced when co-administered with rifampicin. Super-boosting of lopin... |
PMC3969805 | core_pubmed_pmc | Mechanistic considerations for the use of monoclonal antibodies for cancer therapy | Mechanistic considerations for the use of monoclonal antibodies for cancer therapy Abstract Abstract Since the approval of rituximab in 1997, monoclonal antibodies (mAbs) have become an increasingly important component of therapeutic regimens in oncology. The success of mAbs as a therapeutic class is a result of great ... |
PMC4595236 | core_pubmed_pmc | Plasma pharmacokinetic profile of fluralaner (Bravecto™) and ivermectin following concurrent administration to dogs | Plasma pharmacokinetic profile of fluralaner (Bravecto™) and ivermectin following concurrent administration to dogs Abstract Abstract Background Fluralaner is a novel systemic ectoparasiticide for dogs providing immediate and persistent flea, tick and mite control after a single oral dose. Ivermectin has been used in d... |
PMC9097280 | core_pubmed_pmc | From Fitting the Average to Fitting the Individual: A Cautionary Tale for Mathematical Modelers | From Fitting the Average to Fitting the Individual: A Cautionary Tale for Mathematical Modelers Abstract Abstract An outstanding challenge in the clinical care of cancer is moving from a one-size-fits-all approach that relies on population-level statistics towards personalized therapeutic design. Mathematical modeling ... |
PMC9502677 | core_pubmed_pmc | Inflammation and Autophagy: A Convergent Point between Autism Spectrum Disorder (ASD)-Related Genetic and Environmental Factors: Focus on Aluminum Adjuvants | Inflammation and Autophagy: A Convergent Point between Autism Spectrum Disorder (ASD)-Related Genetic and Environmental Factors: Focus on Aluminum Adjuvants Abstract Autism spectrum disorder (ASD), schizophrenia, and bipolar disorder are genetically complex and heterogeneous neurodevelopmental disorders (NDDs) resultin... |
PMC8684501 | core_pubmed_pmc | Exploring the Pharmacokinetics of Phenoxymethylpenicillin (Penicillin-V) in Adults: A Healthy Volunteer Study | Exploring the Pharmacokinetics of Phenoxymethylpenicillin (Penicillin-V) in Adults: A Healthy Volunteer Study Abstract Abstract This healthy volunteer study aimed to explore phenoxymethylpenicillin (penicillin-V) pharmacokinetics (PK) to support the planning of large dosing studies in adults. Volunteers were dosed with... |
PMC9854118 | core_pubmed_pmc | Antimicrobial pharmacodynamics of vancomycin and disulfiram (Antabuse®) in Staphylococcus aureus | Antimicrobial pharmacodynamics of vancomycin and disulfiram (Antabuse®) in Staphylococcus aureus Abstract Introduction Intravenous vancomycin (VAN) is the primary treatment for systemic infections due to methicillin-resistant Staphylococcus aureus (MRSA). Pharmacokinetic/pharmacodynamic target (PK/PD) indices for VAN t... |
PMC11434912 | core_pubmed_pmc | A Meta-Analysis Methodology in Stan to Estimate Population Pharmacokinetic Parameters from Multiple Aggregate Concentration–Time Datasets: Application to Gevokizumab mPBPK Model | A Meta-Analysis Methodology in Stan to Estimate Population Pharmacokinetic Parameters from Multiple Aggregate Concentration–Time Datasets: Application to Gevokizumab mPBPK Model Abstract Abstract The aim of the present study was to develop and evaluate the performance of a methodology to estimate the population pharmac... |
PMC5022129 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of a 13-mer LNA-inhibitor-miR-221 in Mice and Non-human Primates | Pharmacokinetics and Pharmacodynamics of a 13-mer LNA-inhibitor-miR-221 in Mice and Non-human Primates Abstract Locked nucleic acid (LNA) oligonucleotides have been successfully used to efficiently inhibit endogenous small noncoding RNAs in vitro and in vivo. We previously demonstrated that the direct miR-221 inhibitio... |
PMC11178588 | core_pubmed_pmc | Image-based dosimetry for [ 225 Ac]Ac-PSMA-I&T therapy and the effect of daughter-specific pharmacokinetics | Image-based dosimetry for [ 225 Ac]Ac-PSMA-I&T therapy and the effect of daughter-specific pharmacokinetics Abstract Purpose Although 221 Fr and 213 Bi have sufficient gamma emission probabilities, quantitative SPECT after [ 225 Ac]Ac-PSMA-I&T therapy remains challenging due to low therapeutic activities. Furthermore, ... |
PMC10079447 | core_pubmed_pmc | Population Pharmacokinetics and Monte Carlo Simulation of Cefepime in Critically Ill Patients with Hospital-Acquired/Ventilator-Associated Pneumonia | Population Pharmacokinetics and Monte Carlo Simulation of Cefepime in Critically Ill Patients with Hospital-Acquired/Ventilator-Associated Pneumonia Abstract Abstract Background This study aimed to investigate the population pharmacokinetics (PK) profile and determine the optimal dosage regimen of cefepime in criticall... |
PMC6435118 | core_pubmed_pmc | Increased branching and sialylation of N-linked glycans correlate with an improved pharmacokinetic profile for BAY 81–8973 compared with other full-length rFVIII products | Increased branching and sialylation of N-linked glycans correlate with an improved pharmacokinetic profile for BAY 81–8973 compared with other full-length rFVIII products Abstract Abstract Background BAY 81–8973 (Kovaltry) is an unmodified full-length recombinant factor VIII (rFVIII) for treatment of hemophilia A. The ... |
PMC12736958 | core_pubmed_pmc | Surfactants Significantly Improved the Oral Bioavailability of Curcumin Amorphous Solid Dispersions and Its Underlying Mechanism | Surfactants Significantly Improved the Oral Bioavailability of Curcumin Amorphous Solid Dispersions and Its Underlying Mechanism Abstract Background/Objectives: Surfactants are commonly used in amorphous solid dispersions (ASDs) to improve drug dissolution. A mechanistic understanding of their impact on in vitro dissol... |
PMC5651591 | core_pubmed_pmc | Role of renal function in risk assessment of target non-attainment after standard dosing of meropenem in critically ill patients: a prospective observational study | Role of renal function in risk assessment of target non-attainment after standard dosing of meropenem in critically ill patients: a prospective observational study Abstract Abstract Background Severe bacterial infections remain a major challenge in intensive care units because of their high prevalence and mortality. Ad... |
PMC8105215 | core_pubmed_pmc | Mass spectrometric identification and quantification of the antibiotic clavulanic acid in broiler chicken plasma and meat as a necessary analytical tool in finding ways to increase the effectiveness of currently used antibiotics in the treatment of broiler chickens | Mass spectrometric identification and quantification of the antibiotic clavulanic acid in broiler chicken plasma and meat as a necessary analytical tool in finding ways to increase the effectiveness of currently used antibiotics in the treatment of broiler chickens Abstract Abstract Clavulanic acid is a molecule with a... |
PMC7895541 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Emicizumab in Persons with Hemophilia A with Factor VIII Inhibitors: HAVEN 1 Study | Pharmacokinetics and Pharmacodynamics of Emicizumab in Persons with Hemophilia A with Factor VIII Inhibitors: HAVEN 1 Study Abstract Abstract Emicizumab, a bispecific monoclonal antibody, bridges activated factor IX (FIXa) and FX, replacing the function of missing FVIIIa to restore effective hemostasis in persons with ... |
PMC7184189 | core_pubmed_pmc | Structure-Guided In Vitro to In Vivo Pharmacokinetic Optimization of Propargyl-Linked Antifolates | Structure-Guided In Vitro to In Vivo Pharmacokinetic Optimization of Propargyl-Linked Antifolates Abstract Abstract Pharmacokinetic/pharmacodynamic properties are strongly correlated with the in vivo efficacy of antibiotics. Propargyl-linked antifolates, a novel class of antibiotics, demonstrate potent antibacterial ac... |
PMC5958109 | core_pubmed_pmc | Assessing the Feasibility of Neutralizing Osteopontin with Various Therapeutic Antibody Modalities | Assessing the Feasibility of Neutralizing Osteopontin with Various Therapeutic Antibody Modalities Abstract Abstract Osteopontin is a secreted glycophosphoprotein that is highly implicated in many physiological and pathological processes such as biomineralization, cell-mediated immunity, inflammation, fibrosis, cell su... |
PMC12706408 | core_pubmed_pmc | Exposure–Response Analysis of Repotrectinib to Support the Dose Recommendation for Patients With ROS1‐Positive NSCLC or NTRK‐Positive Solid Tumors | Exposure–Response Analysis of Repotrectinib to Support the Dose Recommendation for Patients With ROS1‐Positive NSCLC or NTRK‐Positive Solid Tumors Abstract ABSTRACT To support the benefit–risk assessment and dose justification of repotrectinib for patients with c‐ros oncogene 1 ( ROS1 ) positive non‐small cell lung can... |
PMC10550201 | core_pubmed_pmc | Dose-escalation part of Phase I study of single-agent mosunetuzumab in Japanese patients with relapsed/refractory B-cell non-Hodgkin lymphoma | Dose-escalation part of Phase I study of single-agent mosunetuzumab in Japanese patients with relapsed/refractory B-cell non-Hodgkin lymphoma Abstract Abstract Objective This dose-escalation part of an ongoing Phase I study assessed the tolerability, safety and pharmacokinetics of mosunetuzumab in Japanese patients wit... |
PMC10534409 | core_pubmed_pmc | Meropenem PK/PD Variability and Renal Function: “We Go Together” | Meropenem PK/PD Variability and Renal Function: “We Go Together” Abstract Abstract Background: Meropenem is a carbapenem antibiotic widely employed for serious bacterial infections. Therapeutic drug monitoring (TDM) is a strategy to optimize dosing, especially in critically ill patients. This study aims to show how TDM... |
PMC3726366 | core_pubmed_pmc | Rivaroxaban and other novel oral anticoagulants: pharmacokinetics in healthy subjects, specific patient populations and relevance of coagulation monitoring | Rivaroxaban and other novel oral anticoagulants: pharmacokinetics in healthy subjects, specific patient populations and relevance of coagulation monitoring Abstract Abstract Unlike traditional anticoagulants, the more recently developed agents rivaroxaban, dabigatran and apixaban target specific factors in the coagulat... |
PMC7020312 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling for Predicting Drug Interactions of a Combination of Olanzapine and Samidorphan | Physiologically‐Based Pharmacokinetic Modeling for Predicting Drug Interactions of a Combination of Olanzapine and Samidorphan Abstract Abstract A combination of the antipsychotic olanzapine and the opioid receptor antagonist samidorphan (OLZ/SAM) is intended to provide the antipsychotic efficacy of olanzapine while mi... |
PMC9397503 | core_pubmed_pmc | Prolonged-Release Once-Daily Formulation of Tacrolimus Versus Standard-of-Care Tacrolimus in de novo Kidney Transplant Patients Across Europe | Prolonged-Release Once-Daily Formulation of Tacrolimus Versus Standard-of-Care Tacrolimus in de novo Kidney Transplant Patients Across Europe Abstract Abstract Background: Tacrolimus is the calcineurin inhibitor of choice for preventing acute rejection episodes in kidney transplant patients. However, tacrolimus has a n... |
PMC12394274 | core_pubmed_pmc | Pharmacokinetics and Safety of Ripretinib in Participants with Hepatic Impairment: A Phase 1 Study | Pharmacokinetics and Safety of Ripretinib in Participants with Hepatic Impairment: A Phase 1 Study Abstract Introduction Ripretinib, an oral switch-control inhibitor of KIT tyrosine kinase and platelet-derived growth factor receptor alpha kinase, is approved for adults with advanced gastrointestinal stromal tumor who r... |
PMC9863707 | core_pubmed_pmc | The Chemotherapeutic Efficacy of Hyaluronic Acid Coated Polymeric Nanoparticles against Breast Cancer Metastasis in Female NCr-Nu/Nu Nude Mice | The Chemotherapeutic Efficacy of Hyaluronic Acid Coated Polymeric Nanoparticles against Breast Cancer Metastasis in Female NCr-Nu/Nu Nude Mice Abstract Polyethylene glycol (PEG) coated Poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) for cancer treatment are biocompatible, nonimmunogenic and accumulate in tumour... |
PMC6084339 | core_pubmed_pmc | Selection of 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation Through Comparison of Pharmacokinetic Profiles of 4 Sustained‐Release Prototype Formulations and Standard Acetaminophen Formulation: An Open‐Label, Randomized, Proof‐of‐Principle Pharmacokinetic Study | Selection of 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation Through Comparison of Pharmacokinetic Profiles of 4 Sustained‐Release Prototype Formulations and Standard Acetaminophen Formulation: An Open‐Label, Randomized, Proof‐of‐Principle Pharmacokinetic Study Abstract Abstract Acetaminophen (APAP; p... |
PMC4433458 | core_pubmed_pmc | Perampanel efficacy and tolerability with enzyme-inducing AEDs in patients with epilepsy | Perampanel efficacy and tolerability with enzyme-inducing AEDs in patients with epilepsy Abstract Objective: Evaluate the impact of concomitant enzyme (CYP3A4)-inducer antiepileptic drugs (EIAEDs) on the efficacy and safety of perampanel in patients from the 3 phase-III clinical trials. Methods: Patients with pharmacor... |
PMC10974272 | core_pubmed_pmc | Cytotoxic and Antiproliferative Activity of LASSBio-2208 and the Attempts to Determine Its Drug Metabolism and Pharmacokinetics In Vitro Profile | Cytotoxic and Antiproliferative Activity of LASSBio-2208 and the Attempts to Determine Its Drug Metabolism and Pharmacokinetics In Vitro Profile Abstract Inappropriate expression of histone deacetylase (HDAC-6) and deregulation of the phosphatidylinositol 3-kinase (PI3K) signalling pathway are common aberrations observ... |
PMC10229474 | core_pubmed_pmc | Population plasma and urine pharmacokinetics and the probability of target attainment of fosfomycin in healthy male volunteers | Population plasma and urine pharmacokinetics and the probability of target attainment of fosfomycin in healthy male volunteers Abstract Purpose A population pharmacokinetic model of fosfomycin was developed in healthy volunteers after intravenous administration, and different dosing regimens were evaluated in terms of ... |
PMC5995792 | core_pubmed_pmc | A Phase I Study of the Pharmacokinetics and Pharmacodynamics of Intranasal Doxylamine in Subjects with Chronic Intermittent Sleep Impairment | A Phase I Study of the Pharmacokinetics and Pharmacodynamics of Intranasal Doxylamine in Subjects with Chronic Intermittent Sleep Impairment Abstract Introduction Doxylamine tablets are approved as an over-the-counter sleep aid. We developed a doxylamine succinate intranasal metered-dose delivery system with the expect... |
PMC12917701 | core_pubmed_pmc | Immunocapture-LC-MS/MS Method for Quantification of the Anti-Alzheimer’s Monoclonal Antibody Donanemab in Human and Mice Serum | Immunocapture-LC-MS/MS Method for Quantification of the Anti-Alzheimer’s Monoclonal Antibody Donanemab in Human and Mice Serum Abstract Abstract Monoclonal antibodies hold significant promise for the treatment of Alzheimer’s disease (AD), and donanemab is the latest therapeutic human IgG1 antibody approved for clinical... |
PMC6013504 | core_pubmed_pmc | Inhibition of Tissue Factor Pathway Inhibitor (TFPI) as a Treatment for Haemophilia: Rationale with Focus on Concizumab | Inhibition of Tissue Factor Pathway Inhibitor (TFPI) as a Treatment for Haemophilia: Rationale with Focus on Concizumab Abstract Replacement therapy with missing factor (F) VIII or IX in haemophilia patients for bleed management and preventative treatment or prophylaxis is standard of care. Restoration of thrombin gene... |
PMC5599994 | core_pubmed_pmc | Effects of Tenapanor on Cytochrome P450‐Mediated Drug‐Drug Interactions | Effects of Tenapanor on Cytochrome P450‐Mediated Drug‐Drug Interactions Abstract Abstract Tenapanor (RDX5791, AZD1722) is an inhibitor of sodium/hydrogen exchanger isoform 3 in development for the treatment of constipation‐predominant irritable bowel syndrome and the treatment of hyperphosphatemia in patients with chro... |
PMC6175367 | core_pubmed_pmc | A Randomized, Single‐Center, Double‐Blind, Placebo‐Controlled Multiple‐Dose Phase 1 Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of Imarikiren in Healthy Adult Nonelderly and Elderly Male Subjects | A Randomized, Single‐Center, Double‐Blind, Placebo‐Controlled Multiple‐Dose Phase 1 Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of Imarikiren in Healthy Adult Nonelderly and Elderly Male Subjects Abstract Abstract Imarikiren hydrochloride (TAK‐272/ SCO‐272) is a novel direct renin inhibitor. Th... |
PMC6006693 | core_pubmed_pmc | Pharmacokinetics of rectal levetiracetam as add-on treatment in dogs affected by cluster seizures or status epilepticus | Pharmacokinetics of rectal levetiracetam as add-on treatment in dogs affected by cluster seizures or status epilepticus Abstract Abstract Background Levetiracetam can be used for seizure control alone or in combination with other antiepileptic medications. A previous study achieved the minimum targeted serum drug conce... |
PMC11678411 | core_pubmed_pmc | Development of a Population Pharmacokinetic Gabapentin Model Leveraging Therapeutic Drug Monitoring Concentrations | Development of a Population Pharmacokinetic Gabapentin Model Leveraging Therapeutic Drug Monitoring Concentrations Abstract Abstract Background/Objectives: Gabapentin has variable pharmacokinetics (PK), which contributes to difficulty in dosing and increased risk of adverse events. The objective of this study was to le... |
PMC9303630 | core_pubmed_pmc | Pharmacokinetics of Ipatasertib in Subjects With Hepatic Impairment Using 2 Methods of Classification of Hepatic Function | Pharmacokinetics of Ipatasertib in Subjects With Hepatic Impairment Using 2 Methods of Classification of Hepatic Function Abstract Abstract Ipatasertib is a highly selective small‐molecule pan‐Akt inhibitor in clinical development. Ipatasertib is predominantly eliminated by the liver, and therefore, the effect of hepat... |
PMC11972659 | core_pubmed_pmc | Glycoprotein Matrix-Bound Iron Improves Absorption Compared to Ferrous Bisglycinate Chelate and Ferrous Fumarate: A Randomized Crossover Trial | Glycoprotein Matrix-Bound Iron Improves Absorption Compared to Ferrous Bisglycinate Chelate and Ferrous Fumarate: A Randomized Crossover Trial Abstract Introduction The biotransformation of minerals through glycosylation by microorganisms, such as yeast or probiotics, can produce nutrients bound to a food matrix, poten... |
PMC12949670 | core_pubmed_pmc | Two-Hour Post-dose (C2)-Monitored Cyclosporine Microemulsion as a Practical Alternative to Voclosporin in Mixed Class IV/V Lupus Nephritis: A Case Report | Two-Hour Post-dose (C2)-Monitored Cyclosporine Microemulsion as a Practical Alternative to Voclosporin in Mixed Class IV/V Lupus Nephritis: A Case Report Abstract Lupus nephritis (LN) is a major cause of chronic kidney disease and progression to end-stage kidney disease in patients with systemic lupus erythematosus. Ca... |
PMC8606731 | core_pubmed_pmc | Phase III double-blind study comparing the efficacy and safety of proposed biosimilar MYL-1402O and reference bevacizumab in stage IV non-small-cell lung cancer | Phase III double-blind study comparing the efficacy and safety of proposed biosimilar MYL-1402O and reference bevacizumab in stage IV non-small-cell lung cancer Abstract Purpose: This phase III study compared the efficacy and safety of proposed biosimilar MYL-1402O with reference bevacizumab (BEV), as first-line treatm... |
PMC6966183 | core_pubmed_pmc | Quantitative Systems Pharmacology for Neuroscience Drug Discovery and Development: Current Status, Opportunities, and Challenges | Quantitative Systems Pharmacology for Neuroscience Drug Discovery and Development: Current Status, Opportunities, and Challenges Abstract The substantial progress made in the basic sciences of the brain has yet to be adequately translated to successful clinical therapeutics to treat central nervous system (CNS) disease... |
PMC3169519 | core_pubmed_pmc | A Combined Experimental and Mathematical Approach for Molecular-based Optimization of Irinotecan Circadian Delivery | A Combined Experimental and Mathematical Approach for Molecular-based Optimization of Irinotecan Circadian Delivery Abstract Circadian timing largely modifies efficacy and toxicity of many anticancer drugs. Recent findings suggest that optimal circadian delivery patterns depend on the patient genetic background. We pre... |
PMC11680012 | core_pubmed_pmc | The Development of an Age-Appropriate Fixed Dose Combination for Tuberculosis Using Physiologically-Based Pharmacokinetic Modeling (PBBM) and Risk Assessment | The Development of an Age-Appropriate Fixed Dose Combination for Tuberculosis Using Physiologically-Based Pharmacokinetic Modeling (PBBM) and Risk Assessment Abstract Abstract Background/Objectives: The combination of isoniazid (INH) and rifampicin (RIF) is indicated for the treatment maintenance phase of tuberculosis ... |
PMC12458872 | core_pubmed_pmc | Finding the optimal regimen for Mycobacteroides abscessus treatment (FORMaT) in people with Mycobacteroides abscessus pulmonary disease: a multicentre, randomised, multi-arm, adaptive platform trial | Finding the optimal regimen for Mycobacteroides abscessus treatment (FORMaT) in people with Mycobacteroides abscessus pulmonary disease: a multicentre, randomised, multi-arm, adaptive platform trial Abstract Abstract ABSTRACT Introduction Mycobacteroides abscessus (MABS) is within the non-tuberculous mycobacteria famil... |
PMC4822798 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic analysis of teicoplanin in patients with MRSA infections | Pharmacokinetic/pharmacodynamic analysis of teicoplanin in patients with MRSA infections Abstract Background Teicoplanin is a glycopeptide antibiotic that has been used to treat serious, invasive infections caused by Gram-positive bacteria. The area under the drug concentration–time curve (AUC)/minimum inhibitory conce... |
PMC7396190 | core_pubmed_pmc | Intraocular Pharmacokinetics of 10-fold Intravitreal Ranibizumab Injection Dose in Rabbits | Intraocular Pharmacokinetics of 10-fold Intravitreal Ranibizumab Injection Dose in Rabbits Abstract Abstract Purpose To investigate intraocular pharmacokinetics of 10-fold dose of intravitreally injected ranibizumab compared with the conventional dose in an experimental model. Methods Ranibizumab 30 µL at 10 mg/mL (con... |
PMC4282340 | core_pubmed_pmc | A chronic oral reference dose for hexavalent chromium-induced intestinal cancer † | A chronic oral reference dose for hexavalent chromium-induced intestinal cancer † Abstract High concentrations of hexavalent chromium [Cr(VI)] in drinking water induce villous cytotoxicity and compensatory crypt hyperplasia in the small intestines of mice (but not rats). Lifetime exposure to such cytotoxic concentratio... |
PMC12781337 | core_pubmed_pmc | Tafenoquine lactation pharmacokinetics: a pilot study | Tafenoquine lactation pharmacokinetics: a pilot study Abstract Background Radical cure with an 8-aminoquinoline is required to prevent relapses from Plasmodium vivax . Single-dose treatment with tafenoquine offers significant advantages over primaquine, but the amount of tafenoquine excreted in breastmilk is unknown. A... |
PMC10550877 | core_pubmed_pmc | Comparison of the effects of the GPIIb-IIIa antagonist Zalunfiban and the P2Y12 antagonist Selatogrel on Platelet Aggregation | Comparison of the effects of the GPIIb-IIIa antagonist Zalunfiban and the P2Y12 antagonist Selatogrel on Platelet Aggregation Abstract Abstract Understanding the pharmacodynamic effects of platelet inhibitors is standard for developing more effective antithrombotic therapies. An example is the antithrombotic treatment ... |
PMC11048809 | core_pubmed_pmc | The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride | The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride Abstract The present study explored the effectiveness of bile-salt-based nano-vesicular carriers (bilosomes) for delivering anti-psychotic medication, Sulpiride (Su), via the skin. A response... |
PMC11506717 | core_pubmed_pmc | Peptide–Oligonucleotide Conjugation: Chemistry and Therapeutic Applications | Peptide–Oligonucleotide Conjugation: Chemistry and Therapeutic Applications Abstract Abstract Oligonucleotides have been identified as powerful therapeutics for treating genetic disorders and diseases related to epigenetic factors such as metabolic and immunological dysfunctions. However, they face certain obstacles in... |
PMC9916719 | core_pubmed_pmc | Interaction of Varenicline with Classic Antiseizure Medications in the Mouse Maximal Electroshock-Induced Seizure Model | Interaction of Varenicline with Classic Antiseizure Medications in the Mouse Maximal Electroshock-Induced Seizure Model Abstract Varenicline (VAR) is a partial agonist of brain α4β2 nicotinic acetylcholine receptors recommended as a first line pharmacotherapy for smoking cessation. The aim of this study was to examine ... |
PMC5356695 | core_pubmed_pmc | A phase 1 study of oral ridaforolimus in pediatric patients with advanced solid tumors | A phase 1 study of oral ridaforolimus in pediatric patients with advanced solid tumors Abstract Abstract Purpose Ridaforolimus is an investigational, potent, selective mTOR inhibitor. This study was conducted to determine the recommended phase 2 dose (RP2D), maximum tolerated dose, safety, pharmacokinetics, and antitum... |
PMC12610823 | core_pubmed_pmc | In Silico Integrated Systems Biology Analysis of Gut-Derived Metabolites from Philippine Medicinal Plants Against Atopic Dermatitis | In Silico Integrated Systems Biology Analysis of Gut-Derived Metabolites from Philippine Medicinal Plants Against Atopic Dermatitis Abstract Atopic dermatitis (AD) is a multifactorial skin disorder characterized by immune and barrier dysfunction. The gut–skin axis is a bidirectional pathway through which gut and skin i... |
PMC11319388 | core_pubmed_pmc | JEWELFISH: 24-month results from an open-label study in non-treatment-naïve patients with SMA receiving treatment with risdiplam | JEWELFISH: 24-month results from an open-label study in non-treatment-naïve patients with SMA receiving treatment with risdiplam Abstract Abstract Risdiplam is a once-daily oral, survival of motor neuron 2 ( SMN2 ) splicing modifier approved for the treatment of spinal muscular atrophy (SMA). JEWELFISH (NCT03032172) in... |
PMC5599448 | core_pubmed_pmc | A Pharmacokinetic Bioequivalence Study Comparing Pirfenidone Tablet and Capsule Dosage Forms in Healthy Adult Volunteers | A Pharmacokinetic Bioequivalence Study Comparing Pirfenidone Tablet and Capsule Dosage Forms in Healthy Adult Volunteers Abstract Abstract Introduction Pirfenidone film-coated tablets were developed to offer an alternative to the marketed capsule formulation. This study assessed the bioequivalence of the tablet and cap... |
PMC12402148 | core_pubmed_pmc | Hyaluronidase-enhanced subcutaneous delivery of bNAbs: a phase 1 randomized controlled clinical trial in HIV-uninfected women | Hyaluronidase-enhanced subcutaneous delivery of bNAbs: a phase 1 randomized controlled clinical trial in HIV-uninfected women Abstract Broadly neutralizing antibodies (bNAbs) offer a promising strategy for HIV prevention. Subcutaneous (SC) administration is more feasible than intravenous delivery but may be limited by ... |
PMC2905769 | core_pubmed_pmc | Augmentation of Clozapine with Aripiprazole in Severe Psychotic Bipolar and Schizoaffective Disorders: A Pilot Study | Augmentation of Clozapine with Aripiprazole in Severe Psychotic Bipolar and Schizoaffective Disorders: A Pilot Study Abstract Aim: To evaluate the efficacy and safety of the augmentation of clozapine with aripiprazole in patients with treatment-resistant schizoaffective and psychotic bipolar disorders in a retrospectiv... |
PMC11156759 | core_pubmed_pmc | Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer | Integrated models of population pharmacokinetics and exposure response to optimize dosage regimen for anaprazole sodium in duodenal ulcer Abstract Abstract Anaprazole sodium enteric-coated tablet is a novel proton pump inhibitor which has been approved for the treatment of duodenal ulcer. The aim of this study is to pr... |
PMC9254363 | core_pubmed_pmc | Andrographolide induces anti-SARS-CoV-2 response through host-directed mechanism: an in silico study | Andrographolide induces anti-SARS-CoV-2 response through host-directed mechanism: an in silico study Abstract Abstract Aim: Considering the present alarming situation of COVID-19 pandemic, we concentrated on evaluating the efficacy of a novel natural antiviral drug-candidate andrographolide against SARS-CoV-2 through a... |
PMC6182375 | core_pubmed_pmc | Interactions of Mexiletine with Novel Antiepileptic Drugs in the Maximal Electroshock Test in Mice: An Isobolographic Analysis | Interactions of Mexiletine with Novel Antiepileptic Drugs in the Maximal Electroshock Test in Mice: An Isobolographic Analysis Abstract The aim of the study was to evaluate precisely the type of interactions between mexiletine (an antiarrhythmic drug) and four new generation antiepileptic drugs: lamotrigine, oxcarbazep... |
PMC9483103 | core_pubmed_pmc | Regulatory mechanisms of tetramethylpyrazine on central nervous system diseases: A review | Regulatory mechanisms of tetramethylpyrazine on central nervous system diseases: A review Abstract Central nervous system (CNS) diseases can lead to motor, sensory, speech, cognitive dysfunction, and sometimes even death. These diseases are recognized to cause a substantial socio-economic impact on a global scale. Tetr... |
PMC9054899 | core_pubmed_pmc | Integrated exposure–response analysis of efficacy and safety of lurbinectedin to support the dose regimen in small-cell lung cancer | Integrated exposure–response analysis of efficacy and safety of lurbinectedin to support the dose regimen in small-cell lung cancer Abstract Purpose These exposure–response (E–R) analyses integrated lurbinectedin effects on key efficacy and safety variables in relapsed SCLC to determine the adequacy of the dose regimen... |
PMC11394983 | core_pubmed_pmc | Gastrodin, a Promising Natural Small Molecule for the Treatment of Central Nervous System Disorders, and Its Recent Progress in Synthesis, Pharmacology and Pharmacokinetics | Gastrodin, a Promising Natural Small Molecule for the Treatment of Central Nervous System Disorders, and Its Recent Progress in Synthesis, Pharmacology and Pharmacokinetics Abstract Abstract Gastrodia elata Blume is a traditional medicinal and food homology substance that has been used for thousands of years, is mainly... |
PMC9420883 | core_pubmed_pmc | Model-Predicted Impact of ECG Monitoring Strategies During Bedaquiline Treatment | Model-Predicted Impact of ECG Monitoring Strategies During Bedaquiline Treatment Abstract Abstract Background The M2 metabolite of bedaquiline causes QT-interval prolongation, making electrocardiogram (ECG) monitoring of patients receiving bedaquiline for drug-resistant tuberculosis necessary. The objective of this stu... |
PMC3579428 | core_pubmed_pmc | Population pharmacokinetics of cabazitaxel in patients with advanced solid tumors | Population pharmacokinetics of cabazitaxel in patients with advanced solid tumors Abstract Abstract Purpose To develop a population pharmacokinetic (PK) model for cabazitaxel in patients with advanced solid tumors and examine the influence of demographic and baseline parameters. Methods One hundred and seventy patients... |
PMC8769241 | core_pubmed_pmc | A Review of Pharmacology, Toxicity and Pharmacokinetics of 2,3,5,4′-Tetrahydroxystilbene-2-O-β-D-Glucoside | A Review of Pharmacology, Toxicity and Pharmacokinetics of 2,3,5,4′-Tetrahydroxystilbene-2-O-β-D-Glucoside Abstract Polygonum multiflorum Thunb. ( He-shou-wu in Chinese), a Chinese botanical drug with a long history, is widely used to treat a variety of chronic diseases in clinic, and has been given the reputation of “... |
PMC2914641 | core_pubmed_pmc | Lack of association between stavudine exposure and lipoatrophy, dysglycaemia, hyperlactataemia and hypertriglyceridaemia: a prospective cross sectional study | Lack of association between stavudine exposure and lipoatrophy, dysglycaemia, hyperlactataemia and hypertriglyceridaemia: a prospective cross sectional study Abstract Abstract Background Stavudine continues to be widely used in resource poor settings despite its toxicity. Our objective was to determine association betw... |
PMC9721025 | core_pubmed_pmc | Pharmacokinetic study of the main components of Tanreqing capsules and Tanreqing injections in beagles by liquid chromatography–tandem mass spectrometry | Pharmacokinetic study of the main components of Tanreqing capsules and Tanreqing injections in beagles by liquid chromatography–tandem mass spectrometry Abstract Abstract Background Tanreqing capsules (TRQCs) and Tanreqing injections (TRQIs) are widely used in the treatment of respiratory diseases. In this study, a sim... |
PMC12947635 | core_pubmed_pmc | Comprehensively investigating pharmacokinetics and metabolic fate of andrographolide in rats by liquid chromatography/mass spectrometry-based approach | Comprehensively investigating pharmacokinetics and metabolic fate of andrographolide in rats by liquid chromatography/mass spectrometry-based approach Abstract Abstract Andrographolide, a natural labdane diterpenoid lactone isolated from Andrographis paniculata , possesses diverse pharmacological properties such as ant... |
PMC11533107 | core_pubmed_pmc | Impact of obesity and roux‐en‐Y gastric bypass on the pharmacokinetics of ( R )‐ and ( S )‐omeprazole and intragastric pH | Impact of obesity and roux‐en‐Y gastric bypass on the pharmacokinetics of ( R )‐ and ( S )‐omeprazole and intragastric pH Abstract Abstract This study employed physiologically‐based pharmacokinetic–pharmacodynamics (PBPK/PD) modeling to predict the effect of obesity and gastric bypass surgery on the pharmacokinetics an... |
PMC9792241 | core_pubmed_pmc | Research Progress of Population Pharmacokinetic of Metformin | Research Progress of Population Pharmacokinetic of Metformin Abstract Metformin is commonly used as first-line treatment for T2DM (type2 diabetes mellitus). Owing to the high pharmacokinetic (PK) variability, several population pharmacokinetic (PPK) models have been developed for metformin to explore potential covariat... |
PMC3472020 | core_pubmed_pmc | A Randomized Pharmacokinetic Study of Generic Tacrolimus Versus Reference Tacrolimus in Kidney Transplant Recipients | A Randomized Pharmacokinetic Study of Generic Tacrolimus Versus Reference Tacrolimus in Kidney Transplant Recipients Abstract Pharmacokinetic analyses comparing generic tacrolimus preparations versus the reference drug in kidney transplant patients are lacking. A prospective, multicenter, open-label, randomized, two-pe... |
PMC12089016 | core_pubmed_pmc | Preparation and preclinical evaluation of 18 F-labeled folate-RGD peptide conjugate for PET imaging of triple-negative breast carcinoma | Preparation and preclinical evaluation of 18 F-labeled folate-RGD peptide conjugate for PET imaging of triple-negative breast carcinoma Abstract Background Simultaneous targeting of RGD and FA receptors on breast carcinoma could improve the diagnostic outcome of breast cancer patients. In this study, we have designed a... |
PMC5571334 | core_pubmed_pmc | Ethambutol Partitioning in Tuberculous Pulmonary Lesions Explains Its Clinical Efficacy | Ethambutol Partitioning in Tuberculous Pulmonary Lesions Explains Its Clinical Efficacy Abstract ABSTRACT Clinical trials and practice have shown that ethambutol is an important component of the first-line tuberculosis (TB) regime. This contrasts the drug's rather modest potency and lack of activity against nongrowing ... |
PMC5821700 | core_pubmed_pmc | Quantification of 11β-hydroxysteroid dehydrogenase 1 kinetics and pharmacodynamic effects of inhibitors in brain using mass spectrometry imaging and stable-isotope tracers in mice | Quantification of 11β-hydroxysteroid dehydrogenase 1 kinetics and pharmacodynamic effects of inhibitors in brain using mass spectrometry imaging and stable-isotope tracers in mice Abstract 11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1; EC 1.1.1.146) generates active glucocorticoid hormones. Small molecule inhibitors hav... |
PMC4785617 | core_pubmed_pmc | Drug-drug interactions and QT prolongation as a commonly assessed cardiac effect - comprehensive overview of clinical trials | Drug-drug interactions and QT prolongation as a commonly assessed cardiac effect - comprehensive overview of clinical trials Abstract Abstract Background Proarrhythmia assessment is one of the major concerns for regulatory bodies and pharmaceutical industry. ICH guidelines recommending preclinical tests have been estab... |
PMC5132270 | core_pubmed_pmc | Pharmacologic study (JP28927) of alectinib in Japanese patients with ALK+ non‐small‐cell lung cancer with or without prior crizotinib therapy | Pharmacologic study (JP28927) of alectinib in Japanese patients with ALK+ non‐small‐cell lung cancer with or without prior crizotinib therapy Abstract Abstract We report pharmacokinetics, efficacy and safety data for a new 150‐mg alectinib capsule in ALK+ non‐small‐cell lung cancer in a multicenter, open‐label pharmaco... |
PMC11671327 | core_pubmed_pmc | Pharmacokinetics of vancomycin in sputum of intubated patients: Optimized intravenous delivery vs . inhaled therapy | Pharmacokinetics of vancomycin in sputum of intubated patients: Optimized intravenous delivery vs . inhaled therapy Abstract Abstract Aims Intubated patients with methicillin‐resistant Staphylococcus aureus pneumonia, fail optimized treatment with intravenous (IV) vancomycin (serum trough 15–20 μg/mL) in 38–79% of case... |
PMC10656371 | core_pubmed_pmc | Use of patient-reported outcomes (PRO) data to complement exposure–response analysis in early clinical cancer drug development | Use of patient-reported outcomes (PRO) data to complement exposure–response analysis in early clinical cancer drug development Abstract Background This proof-of-concept retrospective case study investigated whether patient-reported outcomes (PRO) instruments, designed to capture symptomatic adverse event data, could id... |
PMC8271486 | core_pubmed_pmc | Assessment of Antidiabetic Activity of the Shikonin by Allosteric Inhibition of Protein-Tyrosine Phosphatase 1B (PTP1B) Using State of Art: An In Silico and In Vitro Tactics | Assessment of Antidiabetic Activity of the Shikonin by Allosteric Inhibition of Protein-Tyrosine Phosphatase 1B (PTP1B) Using State of Art: An In Silico and In Vitro Tactics Abstract Diabetes mellitus is a multifactorial disease that affects both developing and developed countries and is a major public health concern. ... |
PMC10787200 | core_pubmed_pmc | Applied physiologically‐based pharmacokinetic modeling to assess uridine diphosphate‐glucuronosyltransferase‐mediated drug–drug interactions for Vericiguat | Applied physiologically‐based pharmacokinetic modeling to assess uridine diphosphate‐glucuronosyltransferase‐mediated drug–drug interactions for Vericiguat Abstract Abstract Vericiguat (Verquvo; US: Merck, other countries: Bayer) is a novel drug for the treatment of chronic heart failure. Preclinical studies have demon... |
PMC5412686 | core_pubmed_pmc | A comparative evaluation of models to predict human intestinal metabolism from nonclinical data | A comparative evaluation of models to predict human intestinal metabolism from nonclinical data Abstract Abstract Extensive gut metabolism is often associated with the risk of low and variable bioavailability. The prediction of the fraction of drug escaping gut wall metabolism as well as transporter‐mediated secretion ... |
PMC12833033 | core_pubmed_pmc | Network pharmacology-based identification of potential drug targets and bioactive compounds in Lycii Fructus (Gouqizi) for the therapeutics of Parkinson’s disease | Network pharmacology-based identification of potential drug targets and bioactive compounds in Lycii Fructus (Gouqizi) for the therapeutics of Parkinson’s disease Abstract Introduction Parkinson’s disease (PD) is a common neurodegenerative disease characterized by the loss of dopaminergic neurons without any curable tr... |
PMC9794753 | core_pubmed_pmc | The pharmacokinetics of levobupivacaine 0.5% after infraorbital or inferior alveolar block in anesthetized dogs | The pharmacokinetics of levobupivacaine 0.5% after infraorbital or inferior alveolar block in anesthetized dogs Abstract Introduction Data are lacking on the pharmacokinetic profile and safety of levobupivacaine (LB) used for regional anesthesia of the maxilla and mandibles in dogs. Methods Infraorbital block ( n = 10)... |
PMC8236049 | core_pubmed_pmc | Buprenorphine–cannabis interaction in patients undergoing opioid maintenance therapy | Buprenorphine–cannabis interaction in patients undergoing opioid maintenance therapy Abstract Abstract Buprenorphine is a partial μ-opioid agonist widely used for opioid maintenance therapy (OMT). It is mainly metabolized to pharmacologically active norbuprenorphine by the cytochrome P450 (CYP) isozyme 3A4. This may gi... |
PMC9997082 | core_pubmed_pmc | Engineered antibody cytokine chimera synergizes with DNA-launched nanoparticle vaccines to potentiate melanoma suppression in vivo | Engineered antibody cytokine chimera synergizes with DNA-launched nanoparticle vaccines to potentiate melanoma suppression in vivo Abstract Abstract Cancer immunotherapy has demonstrated great promise with several checkpoint inhibitors being approved as the first-line therapy for some types of cancer, and new engineere... |
PMC5809392 | core_pubmed_pmc | Improved therapeutic potential of tapentadol employing cationic exchange resins as carriers in neuropathic pain: evidence from pharmacokinetic and pharmacodynamics study | Improved therapeutic potential of tapentadol employing cationic exchange resins as carriers in neuropathic pain: evidence from pharmacokinetic and pharmacodynamics study Abstract Current investigation was endeavoured to overcome problem of poor palatability and bioavailability of centrally acting analgesic, tapentadol ... |
PMC9538808 | core_pubmed_pmc | A phase I, randomized, placebo‐controlled study of molnupiravir in healthy Japanese to support special approval in Japan to treat COVID‐19 | A phase I, randomized, placebo‐controlled study of molnupiravir in healthy Japanese to support special approval in Japan to treat COVID‐19 Abstract Abstract Molnupiravir (MK‐4482) is an oral prodrug of the antiviral ribonucleoside analog, N ‐hydroxycytidine (NHC), which has activity against RNA viruses, including sever... |
PMC7747597 | core_pubmed_pmc | Population pharmacokinetic analysis of doripenem for Japanese patients in intensive care unit | Population pharmacokinetic analysis of doripenem for Japanese patients in intensive care unit Abstract Abstract We aimed to construct a novel population pharmacokinetics (PPK) model of doripenem (DRPM) for Japanese patients in intensive care unit, incorporating the clearance of DRPM by continuous renal replacement ther... |
PMC12777127 | core_pubmed_pmc | Zhimu-Huangbai codecoction for the treatment of type II diabetes mellitus through its self-assembling nanoparticles | Zhimu-Huangbai codecoction for the treatment of type II diabetes mellitus through its self-assembling nanoparticles Abstract Abstract Traditional Chinese medicine (TCM) decoctions represent a complex system comprising multiple phases, and their therapeutic effects cannot be fully elucidated solely at the molecular leve... |
PMC9835796 | core_pubmed_pmc | Quantum and Classical Evaluations of Carboxylic Acid Bioisosteres: From Capped Moieties to a Drug Molecule | Quantum and Classical Evaluations of Carboxylic Acid Bioisosteres: From Capped Moieties to a Drug Molecule Abstract Using the Quantum Theory of Atoms in Molecules, the average electron density (AED) tool was developed and employed to quantitatively evaluate the similarities between bioisosteric moieties in drug design.... |
PMC7540322 | core_pubmed_pmc | Response to Inhibition of Receptor‐Interacting Protein Kinase 1 (RIPK1) in Active Plaque Psoriasis: A Randomized Placebo‐Controlled Study | Response to Inhibition of Receptor‐Interacting Protein Kinase 1 (RIPK1) in Active Plaque Psoriasis: A Randomized Placebo‐Controlled Study Abstract Abstract Receptor‐interacting protein kinase 1 (RIPK1), a regulator of inflammation and cell death, is a potential therapeutic target in immune‐mediated inflammatory disease... |
PMC6004616 | core_pubmed_pmc | Quantification and pharmacokinetic study of tumor-targeting agent MHI148-clorgyline amide in mouse plasma using liquid chromatography-electrospray ionization tandem mass spectrometry | Quantification and pharmacokinetic study of tumor-targeting agent MHI148-clorgyline amide in mouse plasma using liquid chromatography-electrospray ionization tandem mass spectrometry Abstract A high-performance liquid chromatography-electrospray ionization tandem mass spectrometric (HPLC-ESI-MS/MS) method was developed... |
PMC10317887 | core_pubmed_pmc | Hypoglycaemia frequency and physiological response after double or triple doses of once-weekly insulin icodec vs once-daily insulin glargine U100 in type 2 diabetes: a randomised crossover trial | Hypoglycaemia frequency and physiological response after double or triple doses of once-weekly insulin icodec vs once-daily insulin glargine U100 in type 2 diabetes: a randomised crossover trial Abstract Aims/hypothesis This study compared the frequency of hypoglycaemia, time to hypoglycaemia and recovery from hypoglyc... |
PMC7700391 | core_pubmed_pmc | Overview of Pharmacokinetics and Liver Toxicities of Radix Polygoni Multiflori | Overview of Pharmacokinetics and Liver Toxicities of Radix Polygoni Multiflori Abstract Abstract Radix Polygoni Multiflori (RPM), a traditional Chinese medicine, has been used as a tonic and an anti-aging remedy for centuries. However, its safe and effective application in clinical practice could be hindered by its liv... |
PMC9365381 | core_pubmed_pmc | Anti-CD79B Antibody–Drug Conjugate DCDS0780A in Patients with B-Cell Non-Hodgkin Lymphoma: Phase 1 Dose-Escalation Study | Anti-CD79B Antibody–Drug Conjugate DCDS0780A in Patients with B-Cell Non-Hodgkin Lymphoma: Phase 1 Dose-Escalation Study Abstract Abstract Purpose: Targeting CD79B using antibody–drug conjugates (ADC) is an effective therapeutic strategy in B-cell non-Hodgkin lymphoma (B-NHL). We investigated DCDS0780A, an anti-CD79B A... |
PMC9880172 | core_pubmed_pmc | Flat dose regimen of toripalimab based on model-informed drug development approach | Flat dose regimen of toripalimab based on model-informed drug development approach Abstract Abstract Introduction: Flat dosing regimen has recently been approved for programmed death receptor-1 (PD-1) inhibitors including toripalimab, nivolumab and pembrolizumab. The objective of this study is to provide pharmacologica... |
PMC6894203 | core_pubmed_pmc | A phase Ib study of utomilumab (PF-05082566) in combination with mogamulizumab in patients with advanced solid tumors | A phase Ib study of utomilumab (PF-05082566) in combination with mogamulizumab in patients with advanced solid tumors Abstract Background Expressed on activated T and natural killer cells, 4-1BB/CD137 is a costimulatory receptor that signals a series of events resulting in cytokine secretion and enhanced effector funct... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.