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PMC9676626
core_pubmed_pmc
Ionophore coccidiostats – disposition kinetics in laying hens and residues transfer to eggs
Ionophore coccidiostats – disposition kinetics in laying hens and residues transfer to eggs Abstract Poultry production is linked with the use of veterinary medicinal products to manage diseases. Ionophore coccidiostats have been permitted for use as feed additives within the European Union ( EU ) for the prevention of...
PMC11906769
core_pubmed_pmc
Targeting the retinoid signaling pathway with YCT-529 for effective and reversible oral contraception in mice and primates
Targeting the retinoid signaling pathway with YCT-529 for effective and reversible oral contraception in mice and primates Abstract Abstract Background The retinoic acid receptor alpha (Rarα) has been validated as a male contraceptive target by genetic knockouts resulting in male sterility. The effects on spermatogenes...
PMC8251541
core_pubmed_pmc
Randomised study: effects of the 5‐HT 4 receptor agonist felcisetrag vs placebo on gut transit in patients with gastroparesis
Randomised study: effects of the 5‐HT 4 receptor agonist felcisetrag vs placebo on gut transit in patients with gastroparesis Abstract Summary Background Gastroparesis is defined by delayed gastric emptying with associated symptoms in the absence of mechanical obstruction. Aim To evaluate pharmacokinetics and pharmacod...
PMC12718473
core_pubmed_pmc
Antioxidant Effects of Aqueous Bidens pilosa in Fructose-Fed Rats
Antioxidant Effects of Aqueous Bidens pilosa in Fructose-Fed Rats Abstract Abstract This narrative review synthesizes preclinical evidence on the antioxidant potential of simple water extracts from the aerial parts of Bidens pilosa in rodent models exposed to chronic fructose feeding. It examines study designs, aqueous...
PMC12890502
core_pubmed_pmc
Icotrokinra induces early and sustained pharmacodynamic responses in phase IIb study of patients with moderate-to-severe psoriasis
Icotrokinra induces early and sustained pharmacodynamic responses in phase IIb study of patients with moderate-to-severe psoriasis Abstract Abstract BACKGROUND Icotrokinra is the first and only targeted oral peptide that selectively binds the IL-23 receptor with high affinity to precisely inhibit IL-23 signaling. Icotr...
PMC9177980
core_pubmed_pmc
Impact of guanidine-containing backbone linkages on stereopure antisense oligonucleotides in the CNS
Impact of guanidine-containing backbone linkages on stereopure antisense oligonucleotides in the CNS Abstract Abstract Attaining sufficient tissue exposure at the site of action to achieve the desired pharmacodynamic effect on a target is an important determinant for any drug discovery program, and this can be particul...
PMC4879370
core_pubmed_pmc
Population Pharmacokinetics Analysis To Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years
Population Pharmacokinetics Analysis To Inform Efavirenz Dosing Recommendations in Pediatric HIV Patients Aged 3 Months to 3 Years Abstract Abstract Efavirenz (EFV) is a nonnucleoside reverse transcriptase inhibitor approved worldwide for the treatment of HIV in adults and children over 3 years of age or weighing over ...
PMC11520371
core_pubmed_pmc
Abnormally high plasma concentrations of M-4, the active metabolite of edoxaban, at the onset of acute kidney injury in a patient receiving rifampin and clarithromycin: a case report
Abnormally high plasma concentrations of M-4, the active metabolite of edoxaban, at the onset of acute kidney injury in a patient receiving rifampin and clarithromycin: a case report Abstract Abstract Background Edoxaban, the only factor Xa inhibitor with active metabolites, is metabolized by carboxylesterase-1 to its ...
PMC8701970
core_pubmed_pmc
Drug–Drug Interactions in Vestibular Diseases, Clinical Problems, and Medico-Legal Implications
Drug–Drug Interactions in Vestibular Diseases, Clinical Problems, and Medico-Legal Implications Abstract Abstract Peripheral vestibular disease can be treated with several approaches (e.g., maneuvers, surgery, or medical approach). Comorbidity is common in elderly patients, so polytherapy is used, but it can generate t...
PMC10295316
core_pubmed_pmc
Cefiderocol Treatment for Severe Infections due to Difficult-to-Treat-Resistant Non-Fermentative Gram-Negative Bacilli in ICU Patients: A Case Series and Narrative Literature Review
Cefiderocol Treatment for Severe Infections due to Difficult-to-Treat-Resistant Non-Fermentative Gram-Negative Bacilli in ICU Patients: A Case Series and Narrative Literature Review Abstract Cefiderocol (FDC) is a siderophore cephalosporin now recognized as a new weapon in the treatment of difficult-to-treat-resistant ...
PMC5841286
core_pubmed_pmc
Image-Guided Focused-Ultrasound CNS Molecular Delivery: An Implementation via Dynamic Contrast-Enhanced Magnetic-Resonance Imaging
Image-Guided Focused-Ultrasound CNS Molecular Delivery: An Implementation via Dynamic Contrast-Enhanced Magnetic-Resonance Imaging Abstract Abstract Focused ultrasound (FUS) exposure with microbubbles can transiently open the blood-brain barrier (BBB) to deliver therapeutic molecules into CNS tissues. However, delivere...
PMC12813652
core_pubmed_pmc
A Phase 1 Dose‐Escalation, Food Effect, and Drug–Drug Interaction Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MALT1 Inhibitor, SGR‐1505, in Healthy Volunteers
A Phase 1 Dose‐Escalation, Food Effect, and Drug–Drug Interaction Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MALT1 Inhibitor, SGR‐1505, in Healthy Volunteers Abstract Abstract SGR‐1505 is a novel small‐molecule inhibitor of MALT1, a key mediator of NF‐κB signaling implicate...
PMC12877024
core_pubmed_pmc
Intrathecal CRISPR-edited allogeneic IL-13Rα2 CAR T Cells for recurrent high-grade Glioma: preclinical characterization and phase I trial
Intrathecal CRISPR-edited allogeneic IL-13Rα2 CAR T Cells for recurrent high-grade Glioma: preclinical characterization and phase I trial Abstract Patients with recurrent high-grade glioblastoma have a median survival of 6-8 months, with limited therapeutic options. In recent years, interest has grown in applying chime...
PMC9029523
core_pubmed_pmc
Interrogating and Quantifying In Vitro Cancer Drug Pharmacodynamics via Agent-Based and Bayesian Monte Carlo Modelling
Interrogating and Quantifying In Vitro Cancer Drug Pharmacodynamics via Agent-Based and Bayesian Monte Carlo Modelling Abstract Abstract The effectiveness of chemotherapy in cancer cell regression is often limited by drug resistance, toxicity, and neoplasia heterogeneity. However, due to the significant complexities en...
PMC9682077
core_pubmed_pmc
Mechanistic modeling as an explanatory tool for clinical treatment of chronic catatonia
Mechanistic modeling as an explanatory tool for clinical treatment of chronic catatonia Abstract Abstract Mathematical modeling of neural systems is an effective means to integrate complex information about the brain into a numerical tool that can help explain observations. However, the use of neural models to inform c...
PMC9500525
core_pubmed_pmc
A comprehensive review of Rubia cordifolia L.: Traditional uses, phytochemistry, pharmacological activities, and clinical applications
A comprehensive review of Rubia cordifolia L.: Traditional uses, phytochemistry, pharmacological activities, and clinical applications Abstract Abstract Rubia cordifolia (family: Rubiaceae) L ( R. cordifolia ) is a perennial botanical drug climbing vine. As the main part of the traditional Chinese medicine, the rhizome...
PMC9254177
core_pubmed_pmc
Vancomycin dosing in an obese patient with acute renal failure: A case report and review of literature
Vancomycin dosing in an obese patient with acute renal failure: A case report and review of literature Abstract BACKGROUND Vancomycin is the most commonly used drug for methicillin-resistant Staphylococcus aureus . The empirical clinical doses of vancomycin based on non-obese patients may not be optimal for obese ones....
PMC11621151
core_pubmed_pmc
Translational population target binding model for the anti-FcRn fragment antibody efgartigimod
Translational population target binding model for the anti-FcRn fragment antibody efgartigimod Abstract Abstract Efgartigimod is a human IgG1 antibody Fc-fragment that lowers IgG levels through blockade of the neonatal Fc receptor (FcRn) and is being evaluated for the treatment of patients with severe autoimmune diseas...
PMC9866064
core_pubmed_pmc
Targeting Tumor-Associated Macrophages for Imaging
Targeting Tumor-Associated Macrophages for Imaging Abstract As an important component of the tumor immune microenvironment (TIME), tumor-associated macrophages (TAMs) occupy a significant niche in tumor margin aggregation and respond to changes in the TIME. Thus, targeting TAMs is important for tumor monitoring, surgic...
PMC9157583
core_pubmed_pmc
Safety, target engagement, and biomarker effects of bosutinib in dementia with Lewy bodies
Safety, target engagement, and biomarker effects of bosutinib in dementia with Lewy bodies Abstract Abstract Introduction Bosutinib, a dual Abelson/Src inhibitor, was investigated in individuals with dementia with Lewy bodies (DLB). Methods A single site, randomized, double‐blind, placebo‐controlled study of the effect...
PMC7878837
core_pubmed_pmc
Generation of Human-Induced Pluripotent Stem Cell-Derived Functional Enterocyte-Like Cells for Pharmacokinetic Studies
Generation of Human-Induced Pluripotent Stem Cell-Derived Functional Enterocyte-Like Cells for Pharmacokinetic Studies Abstract Summary We aimed to establish an in vitro differentiation procedure to generate matured small intestinal cells mimicking human small intestine from human-induced pluripotent stem cells (iPSCs)...
PMC4031148
core_pubmed_pmc
Genetic Deletion of Mst1 Alters T Cell Function and Protects against Autoimmunity
Genetic Deletion of Mst1 Alters T Cell Function and Protects against Autoimmunity Abstract Abstract Mammalian sterile 20-like kinase 1 (Mst1) is a MAPK kinase kinase kinase which is involved in a wide range of cellular responses, including apoptosis, lymphocyte adhesion and trafficking. The contribution of Mst1 to Ag-s...
PMC11303617
core_pubmed_pmc
Safety and clinical activity of JNJ-78306358, a human leukocyte antigen-G (HLA-G) x CD3 bispecific antibody, for the treatment of advanced stage solid tumors
Safety and clinical activity of JNJ-78306358, a human leukocyte antigen-G (HLA-G) x CD3 bispecific antibody, for the treatment of advanced stage solid tumors Abstract Background JNJ-78306358 is a bispecific antibody that redirects T cells to kill human leukocyte antigen-G (HLA-G)-expressing tumor cells. This dose escal...
PMC11207104
core_pubmed_pmc
Anti-Vasculogenic, Antioxidant, and Anti-Inflammatory Activities of Sulfated Polysaccharide Derived from Codium tomentosum : Pharmacokinetic Assay
Anti-Vasculogenic, Antioxidant, and Anti-Inflammatory Activities of Sulfated Polysaccharide Derived from Codium tomentosum : Pharmacokinetic Assay Abstract Abstract The purpose of this paper was to investigate the anti-inflammatory and anti-angiogenic activities of sulfated polysaccharide from C. tomentosum (PCT) using...
PMC4688281
core_pubmed_pmc
A phase I dose-escalation study of a biosimilar trastuzumab in Chinese metastasis breast cancer patients
A phase I dose-escalation study of a biosimilar trastuzumab in Chinese metastasis breast cancer patients Abstract Abstract Trastuzumab has been widely used among the breast cancer patients with human epidermal growth factor receptor 2 (HER2) overexpression. The genetically engineered trastuzumab traded as Cipterbin® wa...
PMC11281955
core_pubmed_pmc
Evaluation of 68 Ga-PSMA-11 PET/CT: a Phase 1 clinical study in Japanese patients with primary, recurrent, or suspected recurrent prostate cancer
Evaluation of 68 Ga-PSMA-11 PET/CT: a Phase 1 clinical study in Japanese patients with primary, recurrent, or suspected recurrent prostate cancer Abstract Abstract Background Prostate-specific membrane antigen (PSMA)-targeted radiopharmaceuticals allow whole-body imaging to detect prostate cancer (PC). Positron emissio...
PMC4027935
core_pubmed_pmc
Udenafil for the treatment of erectile dysfunction
Udenafil for the treatment of erectile dysfunction Abstract Abstract Erectile dysfunction (ED) is often perceived by both patients and sexual partners as a serious problem that can jeopardize quality of life, psychosocial or emotional well-being, and the partnership in the long term. Since their introduction, oral phos...
PMC11655701
core_pubmed_pmc
Population pharmacokinetic modelling of cetirizine concentrations in human breast milk—A contribution from the ConcePTION project
Population pharmacokinetic modelling of cetirizine concentrations in human breast milk—A contribution from the ConcePTION project Abstract Abstract Cetirizine is an antihistamine commonly used to treat allergic rhinitis and other allergic conditions. Cetirizine is often prescribed to breastfeeding mothers although ther...
PMC10343098
core_pubmed_pmc
A systematic review on maternal-to-infant transfer of drugs through breast milk during the treatment of malaria, tuberculosis, and neglected tropical diseases
A systematic review on maternal-to-infant transfer of drugs through breast milk during the treatment of malaria, tuberculosis, and neglected tropical diseases Abstract Background Exclusive breastfeeding of infants under 6 months of age is recommended by the World Health Organization. In 2021, over 300 million combined ...
PMC6767327
core_pubmed_pmc
Enantiospecific Pharmacogenomics of Fluvastatin
Enantiospecific Pharmacogenomics of Fluvastatin Abstract Abstract The aim of this study was to investigate how variability in multiple genes related to pharmacokinetics affects fluvastatin exposure. We determined fluvastatin enantiomer pharmacokinetics and sequenced 379 pharmacokinetic genes in 200 healthy volunteers. ...
PMC9784994
core_pubmed_pmc
Ranolazine Interacts Antagonistically with Some Classical Antiepileptic Drugs—An Isobolographic Analysis
Ranolazine Interacts Antagonistically with Some Classical Antiepileptic Drugs—An Isobolographic Analysis Abstract Abstract Ranolazine, an antianginal and antiarrhythmic drug blocking slow inactivating persistent sodium currents, is described as a compound with anticonvulsant potential. Since arrhythmia often accompanie...
PMC9959361
core_pubmed_pmc
Therapeutic Drug Monitoring of Vancomycin Concentrations for the Management of Bone and Joint Infections: An Urgent Need
Therapeutic Drug Monitoring of Vancomycin Concentrations for the Management of Bone and Joint Infections: An Urgent Need Abstract Vancomycin is used for the treatment of bone and joint infections (BJI), but scarce information is available about its pharmacokinetic/pharmacodynamic (PK/PD) characteristics. We aimed to id...
PMC6733981
core_pubmed_pmc
Drug Disposition and Pharmacotherapy in Neonatal ECMO: From Fragmented Data to Integrated Knowledge
Drug Disposition and Pharmacotherapy in Neonatal ECMO: From Fragmented Data to Integrated Knowledge Abstract Extracorporeal membrane oxygenation (ECMO) is a lifesaving support technology for potentially reversible neonatal cardiac and/or respiratory failure. As the survival and the overall outcome of patients rely on t...
PMC9944386
core_pubmed_pmc
An Analytical Solution for Saturable Absorption in Pharmacokinetics Models
An Analytical Solution for Saturable Absorption in Pharmacokinetics Models Abstract Objective The first-order absorption is a common model used in Pharmacokinetics. The absorption of some drugs follows carrier mediated transport. It has been proposed that the amount of drug available may saturate the transport mechanis...
PMC6159808
core_pubmed_pmc
Effects of ABCB1 rs1045642 polymorphisms on the efficacy and safety of amlodipine therapy in Caucasian patients with stage I–II hypertension
Effects of ABCB1 rs1045642 polymorphisms on the efficacy and safety of amlodipine therapy in Caucasian patients with stage I–II hypertension Abstract Abstract Purpose The aim of this study was to determine the impact of ABCB1 (MDR1) rs1045642 polymorphisms on the efficacy and safety of amlodipine in Caucasian patients....
PMC11381650
core_pubmed_pmc
MHC class I and II-deficient humanized mice are suitable tools to test the long-term antitumor efficacy of immune checkpoint inhibitors and T-cell engagers
MHC class I and II-deficient humanized mice are suitable tools to test the long-term antitumor efficacy of immune checkpoint inhibitors and T-cell engagers Abstract Abstract Background Immunodeficient mice engrafted with peripheral blood mononuclear cells (PBMCs) are models to study new cancer immunotherapy agents. How...
PMC5471477
core_pubmed_pmc
IN VIVO EFFECT OF GUIDING-HERB RADIX PLATYCODONIS AND RADIX CYATHULAE ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS
IN VIVO EFFECT OF GUIDING-HERB RADIX PLATYCODONIS AND RADIX CYATHULAE ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS Abstract Abstract Background: Xuefu Zhuyu Tang (XFZYT), first recorded in Correction of Errors in Medical Works by Qing-ren Wang, has been proven reliable and effective for curing various d...
PMC7387323
core_pubmed_pmc
Safety of Janus Kinase Inhibitors in Older Patients: A Focus on the Thromboembolic Risk
Safety of Janus Kinase Inhibitors in Older Patients: A Focus on the Thromboembolic Risk Abstract Abstract The Janus kinase (JAK)–signal transducer and activator of transcription (STAT) pathway is a membrane-to-nucleus signaling cascade that effects activation of gene transcription. JAK inhibitors have demonstrated effe...
PMC11360631
core_pubmed_pmc
Pharmacokinetics, optimal dosages and withdrawal time of amoxicillin in Nile tilapia ( Oreochromis niloticus ) reared at 25 and 30 °C
Pharmacokinetics, optimal dosages and withdrawal time of amoxicillin in Nile tilapia ( Oreochromis niloticus ) reared at 25 and 30 °C Abstract Abstract Knowledge of amoxicillin (AMX) pharmacokinetics (PK) and tissue residues in fish, which is necessary for prudent drug use, remains limited. The study aimed to explore t...
PMC6089833
core_pubmed_pmc
Physiologically‐based pharmacokinetic model of vaginally administered dapivirine ring and film formulations
Physiologically‐based pharmacokinetic model of vaginally administered dapivirine ring and film formulations Abstract Aims A physiologically‐based pharmacokinetic (PBPK) model of the vaginal space was developed with the aim of predicting concentrations in the vaginal and cervical space. These predictions can be used to ...
PMC11537750
core_pubmed_pmc
A Comprehensive Review on Potential In Silico Screened Herbal Bioactive Compounds and Host Targets in the Cardiovascular Disease Therapy
A Comprehensive Review on Potential In Silico Screened Herbal Bioactive Compounds and Host Targets in the Cardiovascular Disease Therapy Abstract Abstract Herbal medicines (HMs) have deciphered indispensable therapeutic effects against cardiovascular disease (CVD) (the predominant cause of death worldwide). The convent...
PMC7079517
core_pubmed_pmc
Characterization of two in vivo challenge models to measure functional activity of monoclonal antibodies to Plasmodium falciparum circumsporozoite protein
Characterization of two in vivo challenge models to measure functional activity of monoclonal antibodies to Plasmodium falciparum circumsporozoite protein Abstract Background New strategies are needed to reduce the incidence of malaria, and promising approaches include the development of vaccines and monoclonal antibod...
PMC4804727
core_pubmed_pmc
Using Pharmacokinetic Profiles and Digital Quantification of Stained Tissue Microarrays as a Medium-Throughput, Quantitative Method for Measuring the Kinetics of Early Signaling Changes Following Integrin-Linked Kinase Inhibition in an In Vivo Model of Cancer
Using Pharmacokinetic Profiles and Digital Quantification of Stained Tissue Microarrays as a Medium-Throughput, Quantitative Method for Measuring the Kinetics of Early Signaling Changes Following Integrin-Linked Kinase Inhibition in an In Vivo Model of Cancer Abstract Abstract A small molecule inhibitor (QLT0267) targe...
PMC5890624
core_pubmed_pmc
Dual IL-17A and IL-17F neutralisation by bimekizumab in psoriatic arthritis: evidence from preclinical experiments and a randomised placebo-controlled clinical trial that IL-17F contributes to human chronic tissue inflammation
Dual IL-17A and IL-17F neutralisation by bimekizumab in psoriatic arthritis: evidence from preclinical experiments and a randomised placebo-controlled clinical trial that IL-17F contributes to human chronic tissue inflammation Abstract Abstract Objective Interleukin (IL)-17A has emerged as pivotal in driving tissue pat...
PMC5153265
core_pubmed_pmc
Systemic side effects of eye drops: a pharmacokinetic perspective
Systemic side effects of eye drops: a pharmacokinetic perspective Abstract Abstract When administering eye drops, even when completely correctly applied, several routes of absorption are possible and excess amounts can sometimes cause an unwanted systemic bioavailability of the drops when not completely absorbed into t...
PMC9314471
core_pubmed_pmc
Pharmacokinetics of Buprenorphine Buccal Film and Orally-administered Oxycodone in a Respiratory Study: An Analysis of Secondary Outcomes from a Randomized Controlled Trial
Pharmacokinetics of Buprenorphine Buccal Film and Orally-administered Oxycodone in a Respiratory Study: An Analysis of Secondary Outcomes from a Randomized Controlled Trial Abstract Objective To evaluate pharmacokinetic (PK) parameters and oxygen saturation as markers of abuse potential after administration of buprenor...
PMC8247316
core_pubmed_pmc
Ocrelizumab in relapsing and primary progressive multiple sclerosis: Pharmacokinetic and pharmacodynamic analyses of OPERA I, OPERA II and ORATORIO
Ocrelizumab in relapsing and primary progressive multiple sclerosis: Pharmacokinetic and pharmacodynamic analyses of OPERA I, OPERA II and ORATORIO Abstract Aims Ocrelizumab is a humanized monoclonal antibody that selectively targets CD20‐positive B cells and is indicated for treatment of patients with relapsing forms ...
PMC12580603
core_pubmed_pmc
Driving performance in the morning after bedtime vornorexant administration: A randomized clinical trial using a driving simulator
Driving performance in the morning after bedtime vornorexant administration: A randomized clinical trial using a driving simulator Abstract Abstract Aim Sedative hypnotics can impair driving performance to a degree comparable to blood alcohol concentrations of 0.05%–0.08%. This study aimed to evaluate the residual effe...
PMC8467158
core_pubmed_pmc
Tylosin Dosage Adjustment Based on Allometric Scaling in Male Turkeys
Tylosin Dosage Adjustment Based on Allometric Scaling in Male Turkeys Abstract Turkeys’ body weight (BW) increases 10-fold within only 2.5 months, leading to a change in the pharmacokinetics (PK) of drugs according to allometric principles. Thus, the same dosage may lead to age-dependent variability in efficacy, in par...
PMC6224167
core_pubmed_pmc
Mouse genome-wide association studies and systems genetics uncover the genetic architecture associated with hepatic pharmacokinetic and pharmacodynamic properties of a constrained ethyl antisense oligonucleotide targeting Malat1
Mouse genome-wide association studies and systems genetics uncover the genetic architecture associated with hepatic pharmacokinetic and pharmacodynamic properties of a constrained ethyl antisense oligonucleotide targeting Malat1 Abstract Abstract Antisense oligonucleotides (ASOs) have demonstrated variation of efficacy...
PMC4590726
core_pubmed_pmc
Comparative pharmacokinetics of zolpidem tartrate in five ethnic populations of China
Comparative pharmacokinetics of zolpidem tartrate in five ethnic populations of China Abstract The objective of this study was to evaluate the difference in the pharmacokinetics of zolpidem tatrate in subjects from five Chinese ethnicities (Han, Mongolian, Uigur, Korean and Hui). Healthy subjects (10 Hans, 10 Mongolian...
PMC6307981
core_pubmed_pmc
Model-Based Drug Development in Pulmonary Delivery: Pharmacokinetic Analysis of Novel Drug Candidates for Treatment of Pseudomonas aeruginosa Lung Infection
Model-Based Drug Development in Pulmonary Delivery: Pharmacokinetic Analysis of Novel Drug Candidates for Treatment of Pseudomonas aeruginosa Lung Infection Abstract Abstract Antibiotic resistance is a major public health threat worldwide. In particular, about 80% of cystic fibrosis patients have chronic Pseudomonas ae...
PMC4026918
core_pubmed_pmc
Influence of Flunixin on the Disposition Kinetic of Cefepime in Goats
Influence of Flunixin on the Disposition Kinetic of Cefepime in Goats Abstract The pharmacokinetic profile of cefepime (10 mg/kg b.w.) was studied following intravenous and intramuscular administration of cefepime alone and coadministered with flunixin (2.2 mg/kg b.w.) in goats. Cefepime concentrations in serum were de...
PMC7403171
core_pubmed_pmc
Overview of the Clinical Pharmacology of Ertugliflozin, a Novel Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitor
Overview of the Clinical Pharmacology of Ertugliflozin, a Novel Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitor Abstract Abstract Ertugliflozin, a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), is approved in the US, EU, and other regions for the treatment of adults with type 2 diabetes mellitus (T2DM)...
PMC5315728
core_pubmed_pmc
Progress in Prediction and Interpretation of Clinically Relevant Metabolic Drug-Drug Interactions: a Minireview Illustrating Recent Developments and Current Opportunities
Progress in Prediction and Interpretation of Clinically Relevant Metabolic Drug-Drug Interactions: a Minireview Illustrating Recent Developments and Current Opportunities Abstract Abstract Purpose of Review This review gives a perspective on the current “state of the art” in metabolic drug-drug interaction (DDI) predic...
PMC8829480
core_pubmed_pmc
Low Exposure to Direct Oral Anticoagulants Is Associated with Ischemic Stroke and Its Severity
Low Exposure to Direct Oral Anticoagulants Is Associated with Ischemic Stroke and Its Severity Abstract Background and purpose In acute stroke patients, plasma concentrations of direct oral anticoagulants (DOAC) at hospital admission only poorly mirror DOAC exposure or the coagulation status at the time of the event. H...
PMC8339258
core_pubmed_pmc
First-in-Human, Double-Blind, Randomized, Placebo-Controlled Trial of TQ-F3083, a New Dipeptidyl Peptidase-4 Inhibitor, in Healthy Chinese Adults
First-in-Human, Double-Blind, Randomized, Placebo-Controlled Trial of TQ-F3083, a New Dipeptidyl Peptidase-4 Inhibitor, in Healthy Chinese Adults Abstract Abstract Background: As a novel dipeptidyl peptidase-4 (DPP-4) inhibitor, TQ-F3083 represents a promising new drug for type 2 diabetes mellitus (T2DM). This phase I,...
PMC11389264
core_pubmed_pmc
Effect of isavuconazole on the pharmacokinetics of sunitinib and its mechanism
Effect of isavuconazole on the pharmacokinetics of sunitinib and its mechanism Abstract Abstract Background Sunitinib, a newly developed multi-targeted tyrosine kinase inhibitor (TKI), has become a common therapeutic option for managing advanced renal cell carcinoma (RCC). Examining the mechanism underlying the interac...
PMC4930290
core_pubmed_pmc
Pharmacokinetic Interaction of Chrysin with Caffeine in Rats
Pharmacokinetic Interaction of Chrysin with Caffeine in Rats Abstract Pharmacokinetic interaction of chrysin, a flavone present in honey, propolis and herbs, with caffeine was investigated in male Sprague-Dawley rats. Because chrysin inhibited CYP1A-selective ethoxyresorufin O -deethylase and methoxyresorufin O -demeth...
PMC10674798
core_pubmed_pmc
Derivation and Clinical Utility of Safety Targets for Linezolid-Related Adverse Events in Drug-Resistant Tuberculosis Treatment
Derivation and Clinical Utility of Safety Targets for Linezolid-Related Adverse Events in Drug-Resistant Tuberculosis Treatment Abstract Abstract Long-term usage of linezolid can result in adverse events such as peripheral neuropathy, anemia and thrombocytopenia. Therapeutic drug monitoring data from 75 drug-resistant ...
PMC10989020
core_pubmed_pmc
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability Abstract ABSTRACT Protease inhibitors (PIs) remain an important component of antiretroviral therapy for the treatment of HIV-1 infection due to their high genetic barrier to resistance development. Nevertheless...
PMC10879272
core_pubmed_pmc
Hexasodium fytate exposure-response correlations in a randomized, placebo-controlled study of patients on dialysis with cardiovascular calcification
Hexasodium fytate exposure-response correlations in a randomized, placebo-controlled study of patients on dialysis with cardiovascular calcification Abstract Background: Patients receiving dialysis have high cardiovascular risk in part due to extensive vascular calcification. In the CaLIPSO study, infusion of hexasodiu...
PMC9543620
core_pubmed_pmc
Comparison of ciprofol (HSK3486) versus propofol for the induction of deep sedation during gastroscopy and colonoscopy procedures: A multi‐centre, non‐inferiority, randomized, controlled phase 3 clinical trial
Comparison of ciprofol (HSK3486) versus propofol for the induction of deep sedation during gastroscopy and colonoscopy procedures: A multi‐centre, non‐inferiority, randomized, controlled phase 3 clinical trial Abstract Abstract Ciprofol is a propofol analogue with improved pharmacokinetic properties. A multi‐centre, no...
PMC7229803
core_pubmed_pmc
Pranlukast Antagonizes CD49f and Reduces Stemness in Triple-Negative Breast Cancer Cells
Pranlukast Antagonizes CD49f and Reduces Stemness in Triple-Negative Breast Cancer Cells Abstract Abstract Introduction Cancer stem cells (CSCs) drive the initiation, maintenance, and therapy response of breast tumors. CD49f is expressed in breast CSCs and functions in the maintenance of stemness. Thus, blockade of C...
PMC11563405
core_pubmed_pmc
Discovery of α-amylase and α-glucosidase dual inhibitors from NPASS database for management of Type 2 Diabetes Mellitus: A chemoinformatic approach
Discovery of α-amylase and α-glucosidase dual inhibitors from NPASS database for management of Type 2 Diabetes Mellitus: A chemoinformatic approach Abstract Abstract Postprandial hyperglycemia, typical manifestation of Type 2 Diabetes Mellitus (T 2 DM), is associated with notable global morbidity and mortality. Prevent...
PMC11058079
core_pubmed_pmc
Predictive performance of pharmacokinetic-guided prophylactic dosing of factor concentrates in hemophilia A and B
Predictive performance of pharmacokinetic-guided prophylactic dosing of factor concentrates in hemophilia A and B Abstract Abstract Background Pharmacokinetic (PK)-guided dosing is used to individualize factor (F)VIII and FIX replacement therapy. Objectives This study investigates the reliability and feasibility of PK-...
PMC5423959
core_pubmed_pmc
An evaluation of the prevalence of potentially inappropriate medications in older people with cognitive impairment living in Northern Sweden using the EU(7)-PIM list
An evaluation of the prevalence of potentially inappropriate medications in older people with cognitive impairment living in Northern Sweden using the EU(7)-PIM list Abstract Abstract Purpose As people get older, their sensitivity to drugs and adverse drug reactions can increase due to pharmacokinetic and pharmacodynam...
PMC3885732
core_pubmed_pmc
Effect of chronic lead intoxication on the distribution and elimination of amoxicillin in goats
Effect of chronic lead intoxication on the distribution and elimination of amoxicillin in goats Abstract A study of amoxicillin pharmacokinetics was conducted in healthy goats and goats with chronic lead intoxication. The intoxicated goats had increased serum concentrations of liver enzymes (alanine aminotransferase an...
PMC7497676
core_pubmed_pmc
Phase I dose escalation study of BI 836826 (CD37 antibody) in patients with relapsed or refractory B-cell non-Hodgkin lymphoma
Phase I dose escalation study of BI 836826 (CD37 antibody) in patients with relapsed or refractory B-cell non-Hodgkin lymphoma Abstract Summary BI 836826 is a chimeric immunoglobulin G1 antibody targeting CD37, a tetraspanin transmembrane protein predominantly expressed on normal and malignant B cells. This phase I, op...
PMC6201807
core_pubmed_pmc
Borneol and Α-asarone as adjuvant agents for improving blood–brain barrier permeability of puerarin and tetramethylpyrazine by activating adenosine receptors
Borneol and Α-asarone as adjuvant agents for improving blood–brain barrier permeability of puerarin and tetramethylpyrazine by activating adenosine receptors Abstract Abstract Puerarin (PUE) and tetramethylpyrazine (TMP) are central nervous system (CNS) drugs used in cerebrovascular diseases. Poor brain–blood barrier (...
PMC3180444
core_pubmed_pmc
Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration
Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration Abstract Artesunate (AS) is a clinically versatile artemisinin derivative utilized for the treatment of mild to severe malaria infection. Given the thera...
PMC11144487
core_pubmed_pmc
Extrapolation of lung pharmacokinetics of antitubercular drugs from preclinical species to humans using PBPK modelling
Extrapolation of lung pharmacokinetics of antitubercular drugs from preclinical species to humans using PBPK modelling Abstract Abstract Objectives To develop physiologically based pharmacokinetic (PBPK) models for widely used anti-TB drugs, namely rifampicin, pyrazinamide, isoniazid, ethambutol and moxifloxacin lung p...
PMC12454585
core_pubmed_pmc
Published Population Pharmacokinetic Models of Imatinib Perform Poorly on TDM Data from Pediatric Patients
Published Population Pharmacokinetic Models of Imatinib Perform Poorly on TDM Data from Pediatric Patients Abstract Abstract Background Population pharmacokinetic models can potentially provide suggestions for an initial dose and the magnitude of dose adjustment during therapeutic drug monitoring procedures of imatinib...
PMC6232255
core_pubmed_pmc
Drug Transport at the Brain and Endothelial Dysfunction in Preeclampsia: Implications and Perspectives
Drug Transport at the Brain and Endothelial Dysfunction in Preeclampsia: Implications and Perspectives Abstract Abstract Transport of drugs across biological barriers has been a subject of study for decades. The discovery and characterization of proteins that confer the barrier properties of endothelia and epithelia, i...
PMC4186430
core_pubmed_pmc
Modeling of age-dependent amyloid accumulation and γ-secretase inhibition of soluble and insoluble Aβ in a transgenic mouse model of amyloid deposition
Modeling of age-dependent amyloid accumulation and γ-secretase inhibition of soluble and insoluble Aβ in a transgenic mouse model of amyloid deposition Abstract Abstract According to the “amyloid hypothesis,” accumulation of amyloid beta (Aβ) peptides in the brain is linked to the development of Alzheimer's disease. Th...
PMC9786754
core_pubmed_pmc
Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment
Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment Abstract Flibanserin was licensed by the United States Food and Drug Administration (FDA) as an oral non-hormonal therapy for pre-menopausal women with inhi...
PMC12732791
core_pubmed_pmc
Nanomedicine for Cancer and Autoimmune Immunotherapy
Nanomedicine for Cancer and Autoimmune Immunotherapy Abstract Abstract Nanomedicine has now become a transformative platform that enhances the precision and efficacy of immunotherapy approaches and allows customizations like never before when it comes to cancer, as well as autoimmune conditions. Using platforms based o...
PMC12845158
core_pubmed_pmc
Artificial Intelligence and Predictive Modelling for Precision Dosing of Immunosuppressants in Kidney Transplantation
Artificial Intelligence and Predictive Modelling for Precision Dosing of Immunosuppressants in Kidney Transplantation Abstract Abstract Optimizing immunosuppressant dosing presents significant challenges in kidney transplantation due to narrow therapeutic ranges and considerable inter-patient pharmacokinetic difference...
PMC8351251
core_pubmed_pmc
A Phase 1 first‐in‐human study of the safety, tolerability, and pharmacokinetics of the ROBO2 fusion protein PF‐06730512 in healthy participants
A Phase 1 first‐in‐human study of the safety, tolerability, and pharmacokinetics of the ROBO2 fusion protein PF‐06730512 in healthy participants Abstract Abstract Proteinuria associated with podocyte effacement is a hallmark of focal segmental glomerulosclerosis (FSGS). Preclinical studies implicated ROBO2/SLIT2 signal...
PMC12339158
core_pubmed_pmc
Penicillium-Derived Inhibitors of Plasmodium falciparum Lactate Dehydrogenase (PfLDH): A Computational Approach for Novel Antimalarial Therapy Development
Penicillium-Derived Inhibitors of Plasmodium falciparum Lactate Dehydrogenase (PfLDH): A Computational Approach for Novel Antimalarial Therapy Development Abstract Malaria remains a major global health challenge, necessitating the discovery of novel therapeutic agents. This study investigates secondary metabolites from...
PMC6391151
core_pubmed_pmc
Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor
Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor Abstract Background Ticagrelor (TCG) is used to inhibit platelet aggregation in patients with acute coronary syndrome, but its poor solubility and low bioavailability limit it...
PMC9482464
core_pubmed_pmc
Preclinical Pharmacokinetics, Tissue Distribution and in vitro Metabolism of FHND6091, a Novel Oral Proteasome Inhibitor
Preclinical Pharmacokinetics, Tissue Distribution and in vitro Metabolism of FHND6091, a Novel Oral Proteasome Inhibitor Abstract Introduction FHND6091, a novel N-capped dipeptidyl boronic acid proteasome inhibitor with promising pharmacological properties, entirely converted into active form FHND6081 under physiologic...
PMC3439991
core_pubmed_pmc
Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs
Reversible Crystallization of Argatroban after Subcutaneous Application in Pigs Abstract Abstract Argatroban is a thrombin inhibitor used as anticoagulant in patients with heparin-induced thrombocytopenia. It is usually administered as an intravenous bolus followed by infusion. Nevertheless, its pharmacokinetics after ...
PMC7265561
core_pubmed_pmc
UPLC-Tandem Mass Spectrometry for Quantification of Busulfan in Human Plasma: Application to Therapeutic Drug Monitoring
UPLC-Tandem Mass Spectrometry for Quantification of Busulfan in Human Plasma: Application to Therapeutic Drug Monitoring Abstract Busulfan (Bu) is an alkylating agent commonly used in preparative regimens for hematologic malignant and non-malignant patients undergoing hematopoietic stem cell transplantation (HSCT). The...
PMC8908148
core_pubmed_pmc
Population pharmacokinetics of polymyxin B: a systematic review
Population pharmacokinetics of polymyxin B: a systematic review Abstract Background Polymyxin B (PMB) is a basic cyclic polypeptide antibiotic produced by Bacillus polymyxa , and is one of the last options for treating multi-drug-resistant negative bacterial infections in clinical practice. In recent years, many popula...
PMC12838478
core_pubmed_pmc
A combined study of pharmacodynamics and pharmacokinetics of methamphetamine and its metabolite in male mice
A combined study of pharmacodynamics and pharmacokinetics of methamphetamine and its metabolite in male mice Abstract Background Methamphetamine (METH) is typically characterized as a potent dependent psychostimulant. Various behavioral models have been used to study METH drug dependence. The objective of this study wa...
PMC5350996
core_pubmed_pmc
The Safety, Pharmacokinetics, and Nervous System Effects of Two Natural Sources of Caffeine in Healthy Adult Males
The Safety, Pharmacokinetics, and Nervous System Effects of Two Natural Sources of Caffeine in Healthy Adult Males Abstract Abstract This double‐blind crossover clinical trial randomized 12 adult males to receive 200 mg of caffeine from a green coffee extract, a guayusa leaf extract, and a synthetic control to compare ...
PMC11342082
core_pubmed_pmc
The effect of novel aromatic heterocycle substituted aminamidine derivatives on Necator americanus
The effect of novel aromatic heterocycle substituted aminamidine derivatives on Necator americanus Abstract Abstract Background The efficacy of current drugs against hookworms at a single dose is highly variable across regions, age groups and infection intensity. Extensive and repeated use of these drugs also leads to ...
PMC9298103
core_pubmed_pmc
Point-specific interactions of isovitexin with the neighboring amino acid residues of the hACE2 receptor as a targeted therapeutic agent in suppressing the SARS-CoV-2 influx mechanism
Point-specific interactions of isovitexin with the neighboring amino acid residues of the hACE2 receptor as a targeted therapeutic agent in suppressing the SARS-CoV-2 influx mechanism Abstract Objective: Despite the development of several vaccines against severe acute respiratory syndrome coronavirus-2, the need for an...
PMC11332921
core_pubmed_pmc
Assessing anti oxidant, antidiabetic potential and GCMS profiling of ethanolic root bark extract of Zanthoxylum rhetsa (Roxb.) DC: Supported by in vitro , in vivo and in silico molecular modeling
Assessing anti oxidant, antidiabetic potential and GCMS profiling of ethanolic root bark extract of Zanthoxylum rhetsa (Roxb.) DC: Supported by in vitro , in vivo and in silico molecular modeling Abstract Abstract Zanthoxylum rhetsa (ZR) is used traditionally to manage a variety of ailments, including diabetes. Oxidati...
PMC3757855
core_pubmed_pmc
Influence of Circulation System on Estimation of Absorption and Elimination Constant after per oral Drug Administration: A Reanalysis
Influence of Circulation System on Estimation of Absorption and Elimination Constant after per oral Drug Administration: A Reanalysis Abstract Abstract This study aimed to identify the cause of atypical shape of measured concentration-time profile in the peak area by one compartment open model with a lag time (Bateman ...
PMC6107792
core_pubmed_pmc
Pharmacokinetics of β-Alanine Using Different Dosing Strategies
Pharmacokinetics of β-Alanine Using Different Dosing Strategies Abstract Abstract Introduction: The ergogenic response following long-term ingestion of β-alanine shows a high inter-individual variation. It is hypothesized that this variation is partially caused by a variable pharmacokinetic response induced by inferior...
PMC12548523
core_pubmed_pmc
Artificial Intelligence‐Driven Nanoarchitectonics for Smart Targeted Drug Delivery
Artificial Intelligence‐Driven Nanoarchitectonics for Smart Targeted Drug Delivery Abstract Abstract The development of data‐driven and targeted drug delivery systems is essential for advancing precision therapeutics. Despite substantial progress in nanocarrier development, conventional platforms continue to face major...
PMC4092090
core_pubmed_pmc
Investigation of a MMP-2 Activity-Dependent Anchoring Probe for Nuclear Imaging of Cancer
Investigation of a MMP-2 Activity-Dependent Anchoring Probe for Nuclear Imaging of Cancer Abstract Abstract Purpose Since matrix metalloproteinase-2 (MMP-2) is an important marker of tumor malignancy, we developed an original drug design strategy, MMP-2 activity dependent anchoring probes (MDAP), for use in MMP-2 activ...
PMC10656908
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic herb-drug interactions—part I. Herbal medicines of the central nervous system
Pharmacokinetic and pharmacodynamic herb-drug interactions—part I. Herbal medicines of the central nervous system Abstract Abstract Unlike conventional drug substances, herbal medicines are composed of a complex of biologically active compounds. Therefore, the potential occurrence of herb-drug interactions is even more...
PMC8517257
core_pubmed_pmc
Common Statin Intolerance Variants in ABCB1 and LILRB5 Show Synergistic Effects on Statin Response: An Observational Study Using Electronic Health Records
Common Statin Intolerance Variants in ABCB1 and LILRB5 Show Synergistic Effects on Statin Response: An Observational Study Using Electronic Health Records Abstract Abstract Background: Statin intolerance impacts approximately 10% of statin users, with side effects ranging from mild myalgia to extreme intolerance result...
PMC6080383
core_pubmed_pmc
Neutrophil elastase inhibition effectively rescued angiopoietin-1 decrease and inhibits glial scar after spinal cord injury
Neutrophil elastase inhibition effectively rescued angiopoietin-1 decrease and inhibits glial scar after spinal cord injury Abstract After spinal cord injury (SCI), neutrophil elastase (NE) released at injury site disrupts vascular endothelium integrity and stabilization. Angiopoietins (ANGPTs) are vascular growth fact...
PMC4895685
core_pubmed_pmc
Plasma Peak and Trough Gentamicin Concentrations in Hospitalized Horses Receiving Intravenously Administered Gentamicin
Plasma Peak and Trough Gentamicin Concentrations in Hospitalized Horses Receiving Intravenously Administered Gentamicin Abstract Abstract Background Gentamicin is an aminoglycoside antimicrobial commonly used in horses at 6.6 mg/kg IV once daily. Therapeutic drug monitoring (TDM) can confirm desired peak concentration ...
PMC12882764
core_pubmed_pmc
Addressing Causality and Homogeneity Assumptions in Exposure‐Response Analyses
Addressing Causality and Homogeneity Assumptions in Exposure‐Response Analyses Abstract Abstract Exposure‐response, or pharmacokinetic–pharmacodynamic (PKPD), analyses support many drug development decisions. It is typically applied without assessment of causality and homogeneity, where the latter refers to the assumpt...
PMC9687458
core_pubmed_pmc
WP1234—A Novel Anticancer Agent with Bifunctional Activity in a Glioblastoma Model
WP1234—A Novel Anticancer Agent with Bifunctional Activity in a Glioblastoma Model Abstract Glioblastoma multiforme (GBM) is the most common primary malignant brain tumor in adults with a poor prognosis. Despite significant progress in drug development, the blood–brain barrier (BBB) continues to limit the use of novel ...