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PMC12962171 | core_pubmed_pmc | Selective inhibition of ALDH1A3 impedes breast cancer growth and metastasis by blocking ALDH1A3-driven transcriptional programs | Selective inhibition of ALDH1A3 impedes breast cancer growth and metastasis by blocking ALDH1A3-driven transcriptional programs Abstract Summary Aldehyde dehydrogenase 1A3 (ALDH1A3) promotes tumor growth, metastasis, and chemoresistance in multiple cancers, including triple-negative breast cancer (TNBC), yet no clinica... |
PMC8588360 | core_pubmed_pmc | Pharmacokinetics of Azalomycin F, a Natural Macrolide Produced by Streptomycete Strains, in Rats | Pharmacokinetics of Azalomycin F, a Natural Macrolide Produced by Streptomycete Strains, in Rats Abstract As antimicrobial resistance has been increasing, new antimicrobial agents are desperately needed. Azalomycin F, a natural polyhydroxy macrolide, presents remarkable antimicrobial activities. To investigate its phar... |
PMC6827394 | core_pubmed_pmc | Pharmacokinetics of tulathromycin following administration to stocker cattle with remote delivery devices | Pharmacokinetics of tulathromycin following administration to stocker cattle with remote delivery devices Abstract Abstract Remote delivery devices ( RDD ) are used by some to administer antimicrobials ( AM ) to cattle when treatment by manual injection is logistically difficult. However, it is not clear that the pharm... |
PMC12149786 | core_pubmed_pmc | Pharmacokinetics of continuous infusion ceftolozane/tazobactam in two patients with extensive total body surface area burns | Pharmacokinetics of continuous infusion ceftolozane/tazobactam in two patients with extensive total body surface area burns Abstract Abstract Introduction Treatment of infections in patients with burn injuries is challenging due to altered antimicrobial pharmacokinetics. Continuous infusion β‐lactam therapy may be a us... |
PMC10719327 | core_pubmed_pmc | A dose-escalation study of HP501, a highly selective URAT1 inhibitor, in male Chinese patients with hyperuricemia | A dose-escalation study of HP501, a highly selective URAT1 inhibitor, in male Chinese patients with hyperuricemia Abstract Abstract HP501 is a highly selective renal urate transporter 1 (URAT1) inhibitor used for treating hyperuricemia. This study aimed to evaluate the tolerability, pharmacokinetics, and pharmacodynami... |
PMC12613745 | core_pubmed_pmc | Betulinic acid as a novel AT1R inhibitor: attenuation of liver fibrosis via modulation of endothelial–mesenchymal transition in chronic hepatic injury | Betulinic acid as a novel AT1R inhibitor: attenuation of liver fibrosis via modulation of endothelial–mesenchymal transition in chronic hepatic injury Abstract Abstract Background Endothelial-to-mesenchymal transition (EndMT) has emerged as a pivotal pathological process during liver fibrosis. Angiotensin II receptor t... |
PMC4559826 | core_pubmed_pmc | Phase I and pharmacological study of pazopanib in combination with oral topotecan in patients with advanced solid tumours | Phase I and pharmacological study of pazopanib in combination with oral topotecan in patients with advanced solid tumours Abstract Background: This phase I study evaluated the safety, tolerability, maximum tolerated dose (MTD) and pharmacokinetics of two dosing schedules of oral topotecan in combination with pazopanib ... |
PMC12965899 | core_pubmed_pmc | Early Development of Ocadusertib, a Selective Receptor‐Interacting Serine/Threonine‐Protein Kinase 1 Inhibitor | Early Development of Ocadusertib, a Selective Receptor‐Interacting Serine/Threonine‐Protein Kinase 1 Inhibitor Abstract ABSTRACT Receptor‐interacting serine/threonine‐protein kinase 1 (RIPK1) inhibitors are being investigated for chronic inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, an... |
PMC9494977 | core_pubmed_pmc | Steering Away from Current Amoxicillin Dose Reductions in Hospitalized Patients with Impaired Kidney Function to Avoid Subtherapeutic Drug Exposure | Steering Away from Current Amoxicillin Dose Reductions in Hospitalized Patients with Impaired Kidney Function to Avoid Subtherapeutic Drug Exposure Abstract Current dose reductions recommended for amoxicillin in patients with impaired kidney function could lead to suboptimal treatments. In a prospective, observational ... |
PMC10338846 | core_pubmed_pmc | Optimal treatment of ceftazidime-avibactam and aztreonam-avibactam against bloodstream infections or lower respiratory tract infections caused by extensively drug-resistant or pan drug-resistant (XDR/PDR) Pseudomonas aeruginosa | Optimal treatment of ceftazidime-avibactam and aztreonam-avibactam against bloodstream infections or lower respiratory tract infections caused by extensively drug-resistant or pan drug-resistant (XDR/PDR) Pseudomonas aeruginosa Abstract Objective To evaluate the efficacy of ceftazidime-avibactam (CZA) and aztreonam-avi... |
PMC9664902 | core_pubmed_pmc | Applying machine learning to the pharmacokinetic modeling of cyclosporine in adult renal transplant recipients: a multi-method comparison | Applying machine learning to the pharmacokinetic modeling of cyclosporine in adult renal transplant recipients: a multi-method comparison Abstract Abstract Objective: The aim of this study was to identify the important factors affecting cyclosporine (CsA) blood concentration and estimate CsA concentration using seven d... |
PMC12300260 | core_pubmed_pmc | PBPK Modeling of Acetaminophen in Pediatric Populations: Incorporation of SULT Enzyme Ontogeny to Predict Age-Dependent Metabolism and Systemic Exposure | PBPK Modeling of Acetaminophen in Pediatric Populations: Incorporation of SULT Enzyme Ontogeny to Predict Age-Dependent Metabolism and Systemic Exposure Abstract Abstract Sulfotransferase (SULT) enzymes contribute significantly to drug metabolism in pediatric patients. The purpose of this study was to develop a PBPK mo... |
PMC10610918 | core_pubmed_pmc | High-throughput synthesis provides data for predicting molecular properties and reaction success | High-throughput synthesis provides data for predicting molecular properties and reaction success Abstract Abstract The generation of attractive scaffolds for drug discovery efforts requires the expeditious synthesis of diverse analogues from readily available building blocks. This endeavor necessitates a trade-off betw... |
PMC9232434 | core_pubmed_pmc | Population Pharmacokinetic Modelling of Acetaminophen and Ibuprofen: the Influence of Body Composition, Formulation and Feeding in Healthy Adult Volunteers | Population Pharmacokinetic Modelling of Acetaminophen and Ibuprofen: the Influence of Body Composition, Formulation and Feeding in Healthy Adult Volunteers Abstract Abstract Background and Objective Combined acetaminophen and ibuprofen are common antipyretic and analgesic drugs. Formulation and feeding affect drug abso... |
PMC9145014 | core_pubmed_pmc | Pharmacogenetics of Donepezil and Memantine in Healthy Subjects | Pharmacogenetics of Donepezil and Memantine in Healthy Subjects Abstract Donepezil and memantine are the most common drugs used for Alzheimer’s disease. Their low effectiveness could partly be explained by genetic factors. Thus, we aim to identify Single Nucleotide Polymorphisms (SNPs) associated with pharmacokinetics,... |
PMC9877529 | core_pubmed_pmc | Structure-based pharmacophore modeling, virtual screening, and molecular dynamics simulation studies for identification of Plasmodium falciparum 5-aminolevulinate synthase inhibitors | Structure-based pharmacophore modeling, virtual screening, and molecular dynamics simulation studies for identification of Plasmodium falciparum 5-aminolevulinate synthase inhibitors Abstract Plasmodium falciparum ( Pf ) 5-aminolevulinic acid synthase (5-ALAS) is an essential enzyme with high selectivity during liver s... |
PMC3101112 | core_pubmed_pmc | Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics | Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics Abstract Abstract Background: Acute myeloid leukemia (AML) is a life-threatening malignancy with limited treatment options in chemotherapy-refractory patients. A ... |
PMC8234226 | core_pubmed_pmc | Hepatic Arterial Infusion of Chemotherapy for Advanced Hepatobiliary Cancers: State of the Art | Hepatic Arterial Infusion of Chemotherapy for Advanced Hepatobiliary Cancers: State of the Art Abstract Simple Summary Liver functional failure is one of the leading causes of cancer-related death. Systemic chemotherapy usually offers a modest benefit in terms of disease control rate, progression-free survival, and ove... |
PMC12217479 | core_pubmed_pmc | A pre-post quasi-experimental study of antimicrobial stewardship exploring the impact of a multidisciplinary approach aimed at attaining an aggressive joint pharmacokinetic/pharmacodynamic target with ceftazidime/avibactam on treatment outcome of KPC-producing Klebsiella pneumoniae infections and on ceftazidime/avibact... | A pre-post quasi-experimental study of antimicrobial stewardship exploring the impact of a multidisciplinary approach aimed at attaining an aggressive joint pharmacokinetic/pharmacodynamic target with ceftazidime/avibactam on treatment outcome of KPC-producing Klebsiella pneumoniae infections and on ceftazidime/avibact... |
PMC6695151 | core_pubmed_pmc | A pharmacokinetic model including arrival time for two inputs and compensating for varying applied flip-angle in dynamic gadoxetic acid-enhanced MR imaging | A pharmacokinetic model including arrival time for two inputs and compensating for varying applied flip-angle in dynamic gadoxetic acid-enhanced MR imaging Abstract Abstract Purpose Pharmacokinetic models facilitate assessment of properties of the micro-vascularization based on DCE-MRI data. However, accurate pharmacok... |
PMC8263768 | core_pubmed_pmc | Deep Analysis of the Peripheral Immune System in IBD Reveals New Insight in Disease Subtyping and Response to Monotherapy or Combination Therapy | Deep Analysis of the Peripheral Immune System in IBD Reveals New Insight in Disease Subtyping and Response to Monotherapy or Combination Therapy Abstract Abstract Background Inflammatory bowel disease (IBD) is a complex disease with variable presentation, progression, and response to therapies. Current disease classifi... |
PMC7719366 | core_pubmed_pmc | Twice‐Daily Doravirine Overcomes the Interaction Effect from Once‐Weekly Rifapentine and Isoniazid in Healthy Volunteers | Twice‐Daily Doravirine Overcomes the Interaction Effect from Once‐Weekly Rifapentine and Isoniazid in Healthy Volunteers Abstract Doravirine (DOR) is a non‐nucleoside reverse transcriptase inhibitor indicated for the treatment of HIV‐1. Its use in combination with rifapentine (RPT), an antituberculosis (TB) antibiotic,... |
PMC12627770 | core_pubmed_pmc | Obesity Paradox in Cancer: A Complex Interplay Between Risk and Therapeutic Outcomes | Obesity Paradox in Cancer: A Complex Interplay Between Risk and Therapeutic Outcomes Abstract ABSTRACT Obesity is a recognized risk factor for cancer development and progression. Paradoxically, growing clinical evidence across several cancer types indicates that elevated body mass index (BMI) or specific body compositi... |
PMC4218760 | core_pubmed_pmc | Effect of Smoking on the Pharmacokinetics of Inhaled Loxapine | Effect of Smoking on the Pharmacokinetics of Inhaled Loxapine Abstract Abstract Background: Loxapine inhalation powder delivered by a hand-held device as a thermally generated aerosol (ADASUVE) was recently approved in the United States and European Union for use in the acute treatment of agitation in patients with bip... |
PMC5535261 | core_pubmed_pmc | Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane | Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane Abstract Abstract We describe the first systematic study of antimalarial 1,2,4-trioxolanes bearing a substitution pattern regioisomeric to that of arterolane. Conformational analysis suggested that trans -3″-subs... |
PMC11718458 | core_pubmed_pmc | Application of Dorzagliatin in peritoneal dialysis patients with type 2 diabetes mellitus: A case report | Application of Dorzagliatin in peritoneal dialysis patients with type 2 diabetes mellitus: A case report Abstract Abstract BACKGROUND Treating diabetes in dialysis patients remains a challenge, with many hypoglycemic drugs requiring dose adjustments or avoidance in these patients. CASE SUMMARY This report describes an ... |
PMC12426524 | core_pubmed_pmc | Cannabidiol (CBD) and cognitive function in older adults: a mini review | Cannabidiol (CBD) and cognitive function in older adults: a mini review Abstract As the global population ages, the need for effective interventions to support cognitive health in older adults is growing. Cannabidiol (CBD), a non-intoxicating component of cannabis, has emerged as a potential neuroprotective agent due t... |
PMC8705659 | core_pubmed_pmc | Dose Finding and Food Effect Studies of a Novel Abiraterone Acetate Formulation for Oral Suspension in Comparison to a Reference Formulation in Healthy Male Subjects | Dose Finding and Food Effect Studies of a Novel Abiraterone Acetate Formulation for Oral Suspension in Comparison to a Reference Formulation in Healthy Male Subjects Abstract Currently approved formulations of the androgen synthesis inhibitor abiraterone acetate (AA) consist of multiple tablets administered daily in a ... |
PMC6399102 | core_pubmed_pmc | A novel soluble guanylate cyclase activator with reduced risk of hypotension by short‐acting vasodilation | A novel soluble guanylate cyclase activator with reduced risk of hypotension by short‐acting vasodilation Abstract Abstract Cinaciguat, a soluble guanylate cyclase (sGC) activator, was under clinical development for use in acute decompensated heart failure (ADHF), but was discontinued due to occurrence of hypotension. ... |
PMC11785709 | core_pubmed_pmc | Angelica gigas Nakai (Korean Dang-gui) Root Alcoholic Extracts in Health Promotion and Disease Therapy – active Phytochemicals and In Vivo Molecular Targets | Angelica gigas Nakai (Korean Dang-gui) Root Alcoholic Extracts in Health Promotion and Disease Therapy – active Phytochemicals and In Vivo Molecular Targets Abstract Abstract Angelica gigas Nakai (AGN) root is a medicinal herbal widely used in traditional medicine in Korea. AGN root ethanolic extracts have been markete... |
PMC7658073 | core_pubmed_pmc | Metabolism and Pharmacokinetic Drug–Drug Interaction Profile of Vericiguat, A Soluble Guanylate Cyclase Stimulator: Results From Preclinical and Phase I Healthy Volunteer Studies | Metabolism and Pharmacokinetic Drug–Drug Interaction Profile of Vericiguat, A Soluble Guanylate Cyclase Stimulator: Results From Preclinical and Phase I Healthy Volunteer Studies Abstract Abstract Background Vericiguat is a stimulator of soluble guanylate cyclase currently under investigation as a first-in-class therap... |
PMC7327189 | core_pubmed_pmc | Pharmacokinetics and bioequivalence of fixed-dose combination of candesartan cilexetil/amlodipine besylate (16/10 mg) versus coadministration of individual formulations in healthy subjects | Pharmacokinetics and bioequivalence of fixed-dose combination of candesartan cilexetil/amlodipine besylate (16/10 mg) versus coadministration of individual formulations in healthy subjects Abstract Abstract This study compared the pharmacokinetics of a fixed-dose combination (FDC) of candesartan (16 mg) and amlodipine ... |
PMC10774013 | core_pubmed_pmc | Direct-Acting Oral Anticoagulants in patients at extremes of body weight: a review of pharmacological considerations and clinical implications | Direct-Acting Oral Anticoagulants in patients at extremes of body weight: a review of pharmacological considerations and clinical implications Abstract Abstract Patients at extremes of body weight are underrepresented in randomized controlled trials of direct-acting oral anticoagulants (DOACs). Therefore, their optimal... |
PMC7823784 | core_pubmed_pmc | Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective | Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective Abstract Crystalline organic nanoparticles and their amorphous equivalents (ONP) have the potential to become a next-generation formulation technology for dissolution-rate limited biopharmaceutical clas... |
PMC8226704 | core_pubmed_pmc | Cefiderocol in Critically Ill Patients with Multi-Drug Resistant Pathogens: Real-Life Data on Pharmacokinetics and Microbiological Surveillance | Cefiderocol in Critically Ill Patients with Multi-Drug Resistant Pathogens: Real-Life Data on Pharmacokinetics and Microbiological Surveillance Abstract Abstract Cefiderocol is a new siderophore-cephalosporin for the treatment of multi-drug resistant Gram-negative pathogens. As a reserve agent, it will and should be us... |
PMC8416768 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of the Serotonin 5-HT6 Receptor Antagonist, HEC30654, in Healthy Chinese Subjects | Safety, Tolerability and Pharmacokinetics of the Serotonin 5-HT6 Receptor Antagonist, HEC30654, in Healthy Chinese Subjects Abstract Background and Objective: HEC30654 is a selective 5-HT6 receptor antagonist that was safe and well-tolerated in preclinical models of Alzheimer’s disease. The objective of this double-bli... |
PMC12605696 | core_pubmed_pmc | Optimizing phenobarbital dosing in critically ill patients with refractory and superrefractory status epilepticus using a population pharmacokinetic model | Optimizing phenobarbital dosing in critically ill patients with refractory and superrefractory status epilepticus using a population pharmacokinetic model Abstract Abstract Objective Current weight‐based dosing fails to account for pharmacokinetic variability in refractory and superrefractory status epilepticus (RSE, S... |
PMC8076310 | core_pubmed_pmc | Fc-GDF15 glyco-engineering and receptor binding affinity optimization for body weight regulation | Fc-GDF15 glyco-engineering and receptor binding affinity optimization for body weight regulation Abstract Abstract GDF15 is a distant TGF-β family member that induces anorexia and weight loss. Due to its function, GDF15 has attracted attention as a potential therapeutic for the treatment of obesity and its associated m... |
PMC12135494 | core_pubmed_pmc | In Silico drug evaluation by molecular docking, ADME studies and DFT calculations of 2-(6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl)- N , N -dipropylacetamide | In Silico drug evaluation by molecular docking, ADME studies and DFT calculations of 2-(6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl)- N , N -dipropylacetamide Abstract In this study, the structural, electronic, pharmacokinetic, and biological properties of molecule 2-(6-kloro-2-(4-klorofenil)imidazo[1,2-a]pir... |
PMC3779313 | core_pubmed_pmc | The Relationship Between Fluticasone Furoate Systemic Exposure and Cortisol Suppression | The Relationship Between Fluticasone Furoate Systemic Exposure and Cortisol Suppression Abstract Abstract Introduction The inhaled corticosteroid (ICS) fluticasone furoate is in development, in combination with the long-acting beta 2 -agonist vilanterol for the once-daily treatment of asthma and chronic obstructive pul... |
PMC4040677 | core_pubmed_pmc | Antitumor activity of [Pt( O,O' -acac)( γ -acac)(DMS)] in mouse xenograft model of breast cancer | Antitumor activity of [Pt( O,O' -acac)( γ -acac)(DMS)] in mouse xenograft model of breast cancer Abstract The higher and selective cytotoxicity of [Pt( O,O′- acac)( γ -acac)(DMS)] toward cancer cell in both immortalized cell lines and in breast cancer cells in primary cultures, stimulated a pre-clinical study so as to ... |
PMC11706426 | core_pubmed_pmc | Low‐dimensional neural ordinary differential equations accounting for inter‐individual variability implemented in Monolix and NONMEM | Low‐dimensional neural ordinary differential equations accounting for inter‐individual variability implemented in Monolix and NONMEM Abstract Abstract Neural ordinary differential equations (NODEs) are an emerging machine learning (ML) method to model pharmacometric (PMX) data. Combining mechanism‐based components to d... |
PMC3944116 | core_pubmed_pmc | Effect of CYP3A4*22, CYP3A5*3, and CYP3A Combined Genotypes on Cyclosporine, Everolimus, and Tacrolimus Pharmacokinetics in Renal Transplantation | Effect of CYP3A4*22, CYP3A5*3, and CYP3A Combined Genotypes on Cyclosporine, Everolimus, and Tacrolimus Pharmacokinetics in Renal Transplantation Abstract Cyclosporine, everolimus, and tacrolimus are the cornerstone of immunosuppressive therapy in renal transplantation. These drugs are characterized by narrow therapeut... |
PMC9792705 | core_pubmed_pmc | Anticancer potential of phytochemicals from Oroxylum indicum targeting Lactate Dehydrogenase A through bioinformatic approach | Anticancer potential of phytochemicals from Oroxylum indicum targeting Lactate Dehydrogenase A through bioinformatic approach Abstract Abstract In recent years, small molecule inhibition of LDHA (Lactate Dehydrogenase A) has evolved as an appealing option for anticancer therapy. LDHA catalyzes the interconversion of py... |
PMC7667152 | core_pubmed_pmc | Toward a Mathematical Modeling of Diseases’ Impact on Bone Remodeling: Technical Review | Toward a Mathematical Modeling of Diseases’ Impact on Bone Remodeling: Technical Review Abstract A wide variety of bone diseases have hitherto been discovered, such as osteoporosis, Paget’s disease, osteopetrosis, and metastatic bone disease, which are not well defined in terms of changes in biochemical and mechanobiol... |
PMC5410648 | core_pubmed_pmc | Evaluation of Bioequivalence of Two Long-Acting 20% Oxytetracycline Formulations in Pigs | Evaluation of Bioequivalence of Two Long-Acting 20% Oxytetracycline Formulations in Pigs Abstract Abstract The aim of this study was to explore the bioequivalence of long-acting oxytetracycline in two formulations, a reference formulation (Terramycin 20% LA, Pfizer) and a test one (Kangtekang 20% LA, Huishen). Both for... |
PMC12676666 | core_pubmed_pmc | First-in-Human Study of [ 211 At]NaAt as Targeted α-Therapy in Patients with Radioiodine-Refractory Thyroid Cancer (Alpha-T1 Trial) | First-in-Human Study of [ 211 At]NaAt as Targeted α-Therapy in Patients with Radioiodine-Refractory Thyroid Cancer (Alpha-T1 Trial) Abstract 211 At, a cyclotron-produced α-emitter, has attracted interest as a potential alternative to radioactive iodine (RAI) because of its superior cytotoxic properties. This first-in-h... |
PMC4226672 | core_pubmed_pmc | A first in man phase I trial of the oral immunomodulator, indoximod, combined with docetaxel in patients with metastatic solid tumors | A first in man phase I trial of the oral immunomodulator, indoximod, combined with docetaxel in patients with metastatic solid tumors Abstract Abstract Background Indoleamine 2,3-dioxygenase (IDO) is an enzyme that tumors use to create a state of immunosuppression. Indoximod is an IDO pathway inhibitor. Preclinical stu... |
PMC11097614 | core_pubmed_pmc | Analysing the Anticancer Properties of Pterostilbene Through Absorption, Distribution, Metabolism, and Excretion (ADME) and Molecular Docking Studies | Analysing the Anticancer Properties of Pterostilbene Through Absorption, Distribution, Metabolism, and Excretion (ADME) and Molecular Docking Studies Abstract Aim The aim of this study is to examine the possible therapeutic effect of pterostilbene (PTS), a chemical present in grapes and blueberries, in the treatment of... |
PMC12327849 | core_pubmed_pmc | Population pharmacokinetic/pharmacodynamic modeling to optimize aztreonam-avibactam dose regimens for adult patients | Population pharmacokinetic/pharmacodynamic modeling to optimize aztreonam-avibactam dose regimens for adult patients Abstract ABSTRACT Aztreonam-avibactam, a fixed-ratio (3:1) β-lactam/β-lactamase inhibitor combination, was approved in Europe in 2024 for adults with complicated intra-abdominal infection (cIAI), complic... |
PMC10855241 | core_pubmed_pmc | Impact of Levosimendan and Its Metabolites on Platelet Activation Mechanisms in Patients during Antiplatelet Therapy—Pilot Study | Impact of Levosimendan and Its Metabolites on Platelet Activation Mechanisms in Patients during Antiplatelet Therapy—Pilot Study Abstract Abstract Levosimendan is used for the short-term treatment of severe heart failure or other cardiac conditions. The area of existing clinical applications for levosimendan has increa... |
PMC12775438 | core_pubmed_pmc | Identification and in silico evaluation of natural compounds from Annona muricata (soursop) leaves for colon cancer treatment | Identification and in silico evaluation of natural compounds from Annona muricata (soursop) leaves for colon cancer treatment Abstract Abstract Annona muricata (soursop), a traditional medicinal plant renowned for its anticancer properties due to annonaceous acetogenins, was investigated to identify potent phytochemica... |
PMC9203406 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Properties of Cemdisiran, an RNAi Therapeutic Targeting Complement Component 5, in Healthy Subjects and Patients with Paroxysmal Nocturnal Hemoglobinuria | Pharmacokinetic and Pharmacodynamic Properties of Cemdisiran, an RNAi Therapeutic Targeting Complement Component 5, in Healthy Subjects and Patients with Paroxysmal Nocturnal Hemoglobinuria Abstract Background Cemdisiran, an N -acetylgalactosamine (GalNAc) conjugated RNA interference (RNAi) therapeutic, is currently un... |
PMC12297522 | core_pubmed_pmc | Advanced human FcRn knock-in mice for pharmacokinetic profiling of therapeutic antibodies | Advanced human FcRn knock-in mice for pharmacokinetic profiling of therapeutic antibodies Abstract IgG-based therapeutic antibodies are increasingly adopted for diverse human diseases, such as cancer and autoimmune disorders displaying remarkable therapeutic performance. A key factor in their success lies in the extend... |
PMC7983068 | core_pubmed_pmc | Imaging-based characterization of convective tissue properties | Imaging-based characterization of convective tissue properties Abstract Convective transport is an important phenomenon for nanomedicine delivery. We present an imaging-based approach to recover tissue properties that are significant in the accumulation of nanoparticles delivered via systemic methods. The classical pha... |
PMC10508484 | core_pubmed_pmc | Development and application of a PBPK modeling strategy to support antimalarial drug development | Development and application of a PBPK modeling strategy to support antimalarial drug development Abstract Abstract As part of a collaboration between Medicines for Malaria Venture (MMV), Certara UK and Monash University, physiologically‐based pharmacokinetic (PBPK) models were developed for 20 antimalarials, using data... |
PMC10753706 | core_pubmed_pmc | Nanomedicine-Based Drug-Targeting in Breast Cancer: Pharmacokinetics, Clinical Progress, and Challenges | Nanomedicine-Based Drug-Targeting in Breast Cancer: Pharmacokinetics, Clinical Progress, and Challenges Abstract Breast cancer (BC) is a malignant neoplasm that begins in the breast tissue. After skin cancer, BC is the second most common type of cancer in women. At the end of 2040, the number of newly diagnosed BC case... |
PMC8448095 | core_pubmed_pmc | Longitudinal Model-Based Biomarker Analysis of Exposure-Response Relationships in Adults with Pulmonary Tuberculosis | Longitudinal Model-Based Biomarker Analysis of Exposure-Response Relationships in Adults with Pulmonary Tuberculosis Abstract ABSTRACT The identification of sensitive, specific, and reliable biomarkers that can be quantified in the early phases of tuberculosis treatment and predictive of long-term outcome is key for th... |
PMC11997986 | core_pubmed_pmc | Positron Emission Tomography Imaging of Acinetobacter baumannii Infection: Comparison of Gallium-68 Labeled Siderophores | Positron Emission Tomography Imaging of Acinetobacter baumannii Infection: Comparison of Gallium-68 Labeled Siderophores Abstract Acinetobacter baumannii (AB) is an opportunistic pathogen with growing clinical relevance due to its increasing level of antimicrobial resistance in the last few decades. In the event of an ... |
PMC6962035 | core_pubmed_pmc | Modulation of lymphocyte-mediated tissue repair by rational design of heterocyclic aryl hydrocarbon receptor agonists | Modulation of lymphocyte-mediated tissue repair by rational design of heterocyclic aryl hydrocarbon receptor agonists Abstract Abstract Aryl hydrocarbon receptor (AHR) is an essential regulator of gut immunity and a promising therapeutic target for inflammatory bowel disease (IBD). Current AHR agonists are inadequate f... |
PMC3892053 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic modeling for the determination of a cimicoxib dosing regimen in the dog | Pharmacokinetic/pharmacodynamic modeling for the determination of a cimicoxib dosing regimen in the dog Abstract Background Cimicoxib is a new coxib anti-inflammatory drug for use in the dog. To determine a preclinical dosage regimen for cimicoxib in dog, a reversible model of kaolin–induced paw inflammation was used. ... |
PMC7447777 | core_pubmed_pmc | Heterologous expression of high-activity cytochrome P450 in mammalian cells | Heterologous expression of high-activity cytochrome P450 in mammalian cells Abstract The evaluation of Cytochrome P450 (CYP) enzymatic activity is essential to estimate drug pharmacokinetics. Numerous CYP allelic variants have been identified; the functional characterisation of these variants is required for their appl... |
PMC7555381 | core_pubmed_pmc | Improvements in the Oral Absorption and Anticancer Efficacy of an Oxaliplatin-Loaded Solid Formulation: Pharmacokinetic Properties in Rats and Nonhuman Primates and the Effects of Oral Metronomic Dosing on Colorectal Cancer | Improvements in the Oral Absorption and Anticancer Efficacy of an Oxaliplatin-Loaded Solid Formulation: Pharmacokinetic Properties in Rats and Nonhuman Primates and the Effects of Oral Metronomic Dosing on Colorectal Cancer Abstract Abstract Objective The anticancer efficacy of orally administered chemotherapeutics is ... |
PMC9748994 | core_pubmed_pmc | Tranexamic acid dose–response relationship for antifibrinolysis in postpartum haemorrhage during Caesarean delivery: TRACES, a double-blind, placebo-controlled, multicentre, dose-ranging biomarker study | Tranexamic acid dose–response relationship for antifibrinolysis in postpartum haemorrhage during Caesarean delivery: TRACES, a double-blind, placebo-controlled, multicentre, dose-ranging biomarker study Abstract Abstract Background The optimal dose of tranexamic acid to inhibit hyperfibrinolysis in postpartum haemorrha... |
PMC12806659 | core_pubmed_pmc | A review of clinical pharmacology considerations in antibody-drug conjugates approved by the US Food and Drug Administration between 2000 and 2025 | A review of clinical pharmacology considerations in antibody-drug conjugates approved by the US Food and Drug Administration between 2000 and 2025 Abstract Antibody-drug conjugates (ADCs) represent a promising class of anticancer therapies with rapidly expanding development. However, regulatory approval remains complex... |
PMC6616849 | core_pubmed_pmc | Isoniazid Concentration and NAT2 Genotype Predict Risk of Systemic Drug Reactions during 3HP for LTBI | Isoniazid Concentration and NAT2 Genotype Predict Risk of Systemic Drug Reactions during 3HP for LTBI Abstract Weekly rifapentine and isoniazid therapy (known as 3HP) for latent tuberculosis infection (LTBI) is increasingly used, but systemic drug reactions (SDR) remain a major concern. Methods: We prospectively recrui... |
PMC10844384 | core_pubmed_pmc | Armeniacae semen amarum : a review on its botany, phytochemistry, pharmacology, clinical application, toxicology and pharmacokinetics | Armeniacae semen amarum : a review on its botany, phytochemistry, pharmacology, clinical application, toxicology and pharmacokinetics Abstract Armeniacae semen amarum —seeds of Prunus armeniaca L. (Rosaceae) (ASA), also known as Kuxingren in Chinese, is a traditional Chinese herbal drug commonly used for lung disease a... |
PMC4205926 | core_pubmed_pmc | Virtual Systems Pharmacology (ViSP) software for simulation from mechanistic systems-level models | Virtual Systems Pharmacology (ViSP) software for simulation from mechanistic systems-level models Abstract Multiple software programs are available for designing and running large scale system-level pharmacology models used in the drug development process. Depending on the problem, scientists may be forced to use sever... |
PMC11343721 | core_pubmed_pmc | Evaluation and optimization of sample size of neonates and infants for pediatric clinical studies on cefiderocol using a model‐based approach | Evaluation and optimization of sample size of neonates and infants for pediatric clinical studies on cefiderocol using a model‐based approach Abstract Abstract When planning pediatric clinical trials, optimizing the sample size of neonates/infants is essential because it is difficult to enroll these subjects. In this s... |
PMC6430155 | core_pubmed_pmc | Pharmacodynamic Models of Differential Bortezomib Signaling Across Several Cell Lines of Multiple Myeloma | Pharmacodynamic Models of Differential Bortezomib Signaling Across Several Cell Lines of Multiple Myeloma Abstract Abstract The heterogeneous polyclonal nature of multiple myeloma complicates the identification of protein biomarkers predictive of drug response. In this study, a pharmacodynamic systems modeling approach... |
PMC5497534 | core_pubmed_pmc | Pharmacodynamic effects of daclizumab in the intrathecal compartment | Pharmacodynamic effects of daclizumab in the intrathecal compartment Abstract Abstract Objective It was previously demonstrated that daclizumab therapy normalizes cellular cerebrospinal fluid ( CSF ) abnormalities typical of multiple sclerosis ( MS ) in the majority of treated patients. However, CSF cells represent onl... |
PMC8709176 | core_pubmed_pmc | Parametric and Nonparametric Population Pharmacokinetic Models to Assess Probability of Target Attainment of Imipenem Concentrations in Critically Ill Patients | Parametric and Nonparametric Population Pharmacokinetic Models to Assess Probability of Target Attainment of Imipenem Concentrations in Critically Ill Patients Abstract Population pharmacokinetic modeling and simulation (M&S) are used to improve antibiotic dosing. Little is known about the differences in parametric and... |
PMC10477139 | core_pubmed_pmc | The Neonatal and Paediatric Pharmacokinetics of Antimicrobials study (NAPPA): investigating amoxicillin, benzylpenicillin, flucloxacillin and piperacillin pharmacokinetics from birth to adolescence | The Neonatal and Paediatric Pharmacokinetics of Antimicrobials study (NAPPA): investigating amoxicillin, benzylpenicillin, flucloxacillin and piperacillin pharmacokinetics from birth to adolescence Abstract Abstract Background Pharmacokinetic (PK) data underlying paediatric penicillin dosing remain limited, especially ... |
PMC9509579 | core_pubmed_pmc | A validated LC–MS/MS method for analysis of Cabergoline in human plasma with its implementation in a bioequivalent study: investigation of method greenness | A validated LC–MS/MS method for analysis of Cabergoline in human plasma with its implementation in a bioequivalent study: investigation of method greenness Abstract Cabergoline (CAB) is effective prolactin lowering drug. Evaluation of the bioequivalence for the new test product (0.5 mg CAB film-coated tablets) in Egypt... |
PMC12587243 | core_pubmed_pmc | Coated glucose microbeads stimulate enteric hormone release and improve glucose tolerance in Phase 1 and 2 clinical trials | Coated glucose microbeads stimulate enteric hormone release and improve glucose tolerance in Phase 1 and 2 clinical trials Abstract Abstract Aims Incretin agonists are used to treat obesity and metabolic dysfunction. Instead of systemically delivering high levels of hormone receptor agonists that can lead to adverse ef... |
PMC7263918 | core_pubmed_pmc | Allometric analysis of tylosin tartrate pharmacokinetics in growing male turkeys | Allometric analysis of tylosin tartrate pharmacokinetics in growing male turkeys Abstract Background Despite common use of tylosin in turkeys, the pharmacokinetic (PK) data for this drug in turkeys is limited. Within a few months of growth, PK of drugs in turkeys undergoes changes that may decrease their efficacy due t... |
PMC3551687 | core_pubmed_pmc | A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan | A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan Abstract Abstract Background Pregnancy is associated with an increased risk of developing a malaria infection and a higher risk of developing severe malaria. The pharmacokinetic... |
PMC9929129 | core_pubmed_pmc | Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof‐of‐Principle | Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof‐of‐Principle Abstract Abstract Pseudomonas aeruginosa (PA) is an opportunistic human pathogen, which is involved in a wide range of dangerous infections. It develops alarming resistances toward antibiotic treatment. There... |
PMC3847111 | core_pubmed_pmc | Meta-Modeling of Methylprednisolone Effects on Glucose Regulation in Rats | Meta-Modeling of Methylprednisolone Effects on Glucose Regulation in Rats Abstract Abstract A retrospective meta-modeling analysis was performed to integrate previously reported data of glucocorticoid (GC) effects on glucose regulation following a single intramuscular dose (50 mg/kg), single intravenous doses (10, 50 m... |
PMC11047698 | core_pubmed_pmc | Age-Related Differences in Vancomycin-Associated Nephrotoxicity and Efficacy in Methicillin-Resistant Staphylococcus aureus Infection: A Comparative Study between Elderly and Adult Patients | Age-Related Differences in Vancomycin-Associated Nephrotoxicity and Efficacy in Methicillin-Resistant Staphylococcus aureus Infection: A Comparative Study between Elderly and Adult Patients Abstract Abstract Elderly patients (age ≥ 65 years) are susceptible to methicillin-resistant Staphylococcus aureus (MRSA) infectio... |
PMC4224540 | core_pubmed_pmc | A trait-based trade-off between growth and mortality: evidence from 15 tropical tree species using size-specific relative growth rates | A trait-based trade-off between growth and mortality: evidence from 15 tropical tree species using size-specific relative growth rates Abstract A life-history trade-off between low mortality in the dark and rapid growth in the light is one of the most widely accepted mechanisms underlying plant ecological strategies in... |
PMC10995391 | core_pubmed_pmc | Effect of NAT2, GSTM1 and CYP2E1 genetic polymorphisms on plasma concentration of isoniazid and its metabolites in patients with tuberculosis, and the assessment of exposure-response relationships | Effect of NAT2, GSTM1 and CYP2E1 genetic polymorphisms on plasma concentration of isoniazid and its metabolites in patients with tuberculosis, and the assessment of exposure-response relationships Abstract Abstract Objectives: Isoniazid is a key drug in the chemotherapy of tuberculosis (TB), however, interindividual va... |
PMC11106169 | core_pubmed_pmc | Predictions of Bedaquiline Central Nervous System Exposure in Patients with Tuberculosis Meningitis Using Physiologically based Pharmacokinetic Modeling | Predictions of Bedaquiline Central Nervous System Exposure in Patients with Tuberculosis Meningitis Using Physiologically based Pharmacokinetic Modeling Abstract Background and Objective The use of bedaquiline as a treatment option for drug-resistant tuberculosis meningitis (TBM) is of interest to address the increased... |
PMC3399570 | core_pubmed_pmc | Acute and Chronic Administrations of Rheum palmatum Reduced the Bioavailability of Phenytoin in Rats: A New Herb-Drug Interaction | Acute and Chronic Administrations of Rheum palmatum Reduced the Bioavailability of Phenytoin in Rats: A New Herb-Drug Interaction Abstract The rhizome of Rheum palmatum (RP) is a commonly used herb in clinical Chinese medicine. Phenytoin (PHT) is an antiepileptic with narrow therapeutic window. This study investigated ... |
PMC9095523 | core_pubmed_pmc | Pharmacokinetics and toxicity evaluation following oral exposure to bisphenol F | Pharmacokinetics and toxicity evaluation following oral exposure to bisphenol F Abstract Bisphenol F is a substitute material for bisphenol A and is widely used in household products as a raw material for polycarbonate resin, epoxy resin, and plastic reinforcement. It is known to be mainly used in food containers, ther... |
PMC12187371 | core_pubmed_pmc | Therapeutic effect of novel drug candidate, PRG-N-01, on NF2 syndrome-related tumor | Therapeutic effect of novel drug candidate, PRG-N-01, on NF2 syndrome-related tumor Abstract Abstract Background NF2-related schwannomatosis (NF2-SWN) is associated with multiple benign tumors in the nervous system. NF2-SWN, caused by mutations in the NF2 gene, has developed into intracranial and spinal schwannomas. Be... |
PMC11647203 | core_pubmed_pmc | First-in-Human Dose-Escalation Study of Fianlimab, an Antilymphocyte Activation Gene-3 Antibody, with Cemiplimab in Patients with Advanced Malignancies | First-in-Human Dose-Escalation Study of Fianlimab, an Antilymphocyte Activation Gene-3 Antibody, with Cemiplimab in Patients with Advanced Malignancies Abstract Abstract Purpose: Preclinical data indicate that fianlimab (antilymphocyte activation gene-3) plus cemiplimab (anti–PD-1) enhances antitumor activity. Here, we... |
PMC12676031 | core_pubmed_pmc | Informatics Approach Towards Targeting HTR1B Pathways in Neuropharmacology for Migraine Treatment | Informatics Approach Towards Targeting HTR1B Pathways in Neuropharmacology for Migraine Treatment Abstract Abstract Introduction Migraine is a prevalent and debilitating neurological disorder, with current therapies are frequently ineffective and have side effects. Recent studies in neuropharmacology present the seroto... |
PMC3475088 | core_pubmed_pmc | Continuous beta-lactam infusion in critically ill patients: the clinical evidence | Continuous beta-lactam infusion in critically ill patients: the clinical evidence Abstract There is controversy over whether traditional intermittent bolus dosing or continuous infusion of beta-lactam antibiotics is preferable in critically ill patients. No significant difference between these two dosing strategies in ... |
PMC4895465 | core_pubmed_pmc | A Review of the Studies Using Buprenorphine in Cats | A Review of the Studies Using Buprenorphine in Cats Abstract Abstract Pain management is a crucial component of feline medicine and surgery. This review critically evaluates studies using buprenorphine in cats and highlights the clinical application of the opioid in this species. The pharmacokinetic‐pharmacodynamic (PK... |
PMC8380063 | core_pubmed_pmc | Lumbriculus variegatus : A novel organism for in vivo pharmacology education | Lumbriculus variegatus : A novel organism for in vivo pharmacology education Abstract Abstract Pharmacology graduates require an understanding of both in vitro and in vivo drug responses but there has been a decline in animal use in pharmacology education over the last 30 years. To address this, we present the novel in... |
PMC11679858 | core_pubmed_pmc | From Psychoactivity to Antimicrobial Agents: Multifaceted Applications of Synthetic Cathinones and Catha edulis Extracts | From Psychoactivity to Antimicrobial Agents: Multifaceted Applications of Synthetic Cathinones and Catha edulis Extracts Abstract The emergence of new psychoactive substances (NPS) in the global drug market since the 2000s has posed major challenges for regulators and law enforcement agencies. Among these, synthetic ca... |
PMC9500858 | core_pubmed_pmc | Comparative Study of Chemical Stability of a PK20 Opioid–Neurotensin Hybrid Peptide and Its Analogue [Ile 9 ]PK20—The Effect of Isomerism of a Single Amino Acid | Comparative Study of Chemical Stability of a PK20 Opioid–Neurotensin Hybrid Peptide and Its Analogue [Ile 9 ]PK20—The Effect of Isomerism of a Single Amino Acid Abstract Chemical stability is one of the main problems during the discovery and development of potent drugs. When ignored, it may lead to unreliable biologica... |
PMC9032906 | core_pubmed_pmc | Model-Informed Precision Dosing of Linezolid in Patients with Drug-Resistant Tuberculosis | Model-Informed Precision Dosing of Linezolid in Patients with Drug-Resistant Tuberculosis Abstract Abstract Linezolid is an efficacious medication for the treatment of drug-resistant tuberculosis but has been associated with serious safety issues that can result in treatment interruption. The objectives of this study w... |
PMC10058050 | core_pubmed_pmc | A Bitter Taste Receptor as a Novel Molecular Target on Cancer-Associated Fibroblasts in Pancreatic Ductal Adenocarcinoma | A Bitter Taste Receptor as a Novel Molecular Target on Cancer-Associated Fibroblasts in Pancreatic Ductal Adenocarcinoma Abstract Abstract Cancer-associated fibroblasts (CAFs) execute diverse and complex functions in cancer progression. While reprogramming the crosstalk between CAFs and cancer epithelial cells is a pro... |
PMC9540491 | core_pubmed_pmc | Effect of Chronic Kidney Disease on the Renal Secretion via Organic Anion Transporters 1/3: Implications for Physiologically‐Based Pharmacokinetic Modeling and Dose Adjustment | Effect of Chronic Kidney Disease on the Renal Secretion via Organic Anion Transporters 1/3: Implications for Physiologically‐Based Pharmacokinetic Modeling and Dose Adjustment Abstract There is growing evidence that active tubular secretory clearance (CL s ) may not decline proportionally with the glomerular filtration... |
PMC12678462 | core_pubmed_pmc | Implementation of an integrative safety consultation service for the use of dietary and herbal supplements among patients with hematological diseases | Implementation of an integrative safety consultation service for the use of dietary and herbal supplements among patients with hematological diseases Abstract Abstract Introduction Dietary and herbal supplements (DHS) are used by 30% of hematological patients despite safety concerns. A service of integrative safety con... |
PMC7067455 | core_pubmed_pmc | Pharmacogenetic—Whole blood and intracellular pharmacokinetic—Pharmacodynamic (PG-PK 2 -PD) relationship of tacrolimus in liver transplant recipients | Pharmacogenetic—Whole blood and intracellular pharmacokinetic—Pharmacodynamic (PG-PK 2 -PD) relationship of tacrolimus in liver transplant recipients Abstract Abstract Tacrolimus (TAC) is the cornerstone of immunosuppressive therapy in liver transplantation. This study aimed at elucidating the interplay between pharmac... |
PMC5352756 | core_pubmed_pmc | A phase 1 study of the pharmacokinetics of nucleoside analog trifluridine and thymidine phosphorylase inhibitor tipiracil (components of TAS-102) vs trifluridine alone | A phase 1 study of the pharmacokinetics of nucleoside analog trifluridine and thymidine phosphorylase inhibitor tipiracil (components of TAS-102) vs trifluridine alone Abstract Summary Background Trifluridine, a thymidine-based chemotherapeutic, has limited bioavailability after clinical administration as it is rapidly... |
PMC12227017 | core_pubmed_pmc | Pharmacokinetics of Belumosudil and Its Metabolites in Individuals With Hepatic Impairment | Pharmacokinetics of Belumosudil and Its Metabolites in Individuals With Hepatic Impairment Abstract ABSTRACT Belumosudil, an orally administered Rho‐associated coiled‐coil–containing protein kinase 2 selective inhibitor drug for treatment of chronic graft‐versus‐host disease (GVHD), is predominantly eliminated via the ... |
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