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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 ... |
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