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PMC12144160
core_pubmed_pmc
Computational discovery of novel aryl hydrocarbon receptor modulators for psoriasis therapy
Computational discovery of novel aryl hydrocarbon receptor modulators for psoriasis therapy Abstract Abstract The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcription factor involved in the regulation of many pathophysiological processes. Among these, immune system modulation, as well as regulation of sk...
PMC4940708
core_pubmed_pmc
Neurotrophic factor small-molecule mimetics mediated neuroregeneration and synaptic repair: emerging therapeutic modality for Alzheimer’s disease
Neurotrophic factor small-molecule mimetics mediated neuroregeneration and synaptic repair: emerging therapeutic modality for Alzheimer’s disease Abstract Alzheimer’s disease (AD) is an incurable and debilitating chronic progressive neurodegenerative disorder which is the leading cause of dementia worldwide. AD is a he...
PMC9320685
core_pubmed_pmc
Quality Control Dissolution Data Is Biopredictive for a Modified Release Ropinirole Formulation: Virtual Experiment with the Use of Re-Developed and Verified PBPK Model
Quality Control Dissolution Data Is Biopredictive for a Modified Release Ropinirole Formulation: Virtual Experiment with the Use of Re-Developed and Verified PBPK Model Abstract Physiologically based pharmacokinetic and absorption modeling are being used by industry and regulatory bodies to address various scientifical...
PMC6771222
core_pubmed_pmc
A multicentre, phase IIa study of zolbetuximab as a single agent in patients with recurrent or refractory advanced adenocarcinoma of the stomach or lower oesophagus: the MONO study
A multicentre, phase IIa study of zolbetuximab as a single agent in patients with recurrent or refractory advanced adenocarcinoma of the stomach or lower oesophagus: the MONO study Abstract Abstract Background Claudin 18.2 (CLDN18.2) is physiologically confined to gastric mucosa tight junctions; however, upon malignant...
PMC7770183
core_pubmed_pmc
Enhanced Bioavailability of Boswellic Acid by Piper longum : A Computational and Pharmacokinetic Study
Enhanced Bioavailability of Boswellic Acid by Piper longum : A Computational and Pharmacokinetic Study Abstract Chronic inflammation is a key culprit factor in the onset and progression of several diseases. Novel and pharmacologically effective therapeutic approaches are needed for new treatment remedy or improved phar...
PMC4592188
core_pubmed_pmc
Bayesian Population Physiologically-Based Pharmacokinetic (PBPK) Approach for a Physiologically Realistic Characterization of Interindividual Variability in Clinically Relevant Populations
Bayesian Population Physiologically-Based Pharmacokinetic (PBPK) Approach for a Physiologically Realistic Characterization of Interindividual Variability in Clinically Relevant Populations Abstract Abstract Interindividual variability in anatomical and physiological properties results in significant differences in drug...
PMC7033599
core_pubmed_pmc
Resistance Evolution Against Antimicrobial Peptides in Staphylococcus aureus Alters Pharmacodynamics Beyond the MIC
Resistance Evolution Against Antimicrobial Peptides in Staphylococcus aureus Alters Pharmacodynamics Beyond the MIC Abstract Abstract Antimicrobial peptides (AMPs) have been proposed as a promising class of new antimicrobials partly because they are less susceptible to bacterial resistance evolution. This is possibly c...
PMC8885938
core_pubmed_pmc
Safety, Pharmacokinetic, and Pharmacodynamic Study of a Sublingual Formula for the Treatment of Vasovagal Syncope
Safety, Pharmacokinetic, and Pharmacodynamic Study of a Sublingual Formula for the Treatment of Vasovagal Syncope Abstract Background Vasovagal syncope is a common cause of syncope which, if recurrent, can have multiple negative consequences such as injury and occupational disability. Various medications can be used to...
PMC12245000
core_pubmed_pmc
Intravitreal Administration of Adalimumab‐Loaded Poly(Lactic‐co‐Glycolic Acid) Nanoparticles: Effects on Biodistribution and Pharmacokinetics
Intravitreal Administration of Adalimumab‐Loaded Poly(Lactic‐co‐Glycolic Acid) Nanoparticles: Effects on Biodistribution and Pharmacokinetics Abstract Adalimumab, a monoclonal antibody used for treating inflammatory diseases, including eye diseases, faces challenges in biodistribution and targeted delivery. Nanoparticl...
PMC2825345
core_pubmed_pmc
Combining the in vivo comet and micronucleus assays: a practical approach to genotoxicity testing and data interpretation
Combining the in vivo comet and micronucleus assays: a practical approach to genotoxicity testing and data interpretation Abstract Abstract Despite regulatory directives requiring the reduction of animal use in safety testing, recent modifications to genotoxicity testing guidelines now propose the use of two in vivo ge...
PMC6010978
core_pubmed_pmc
Response to Single Low-dose 177 Lu-DOTA-EB-TATE Treatment in Patients with Advanced Neuroendocrine Neoplasm: A Prospective Pilot Study
Response to Single Low-dose 177 Lu-DOTA-EB-TATE Treatment in Patients with Advanced Neuroendocrine Neoplasm: A Prospective Pilot Study Abstract Abstract Objective: 177 Lu-DOTA-EB-TATE is a theranostic agent based on octreotate that uses an Evans blue structure to bind albumin to improve the pharmacokinetics and pharmac...
PMC9850716
core_pubmed_pmc
A Multifaceted Review of Eurycoma longifolia Nutraceutical Bioactives: Production, Extraction, and Analysis in Drugs and Biofluids
A Multifaceted Review of Eurycoma longifolia Nutraceutical Bioactives: Production, Extraction, and Analysis in Drugs and Biofluids Abstract Eurycoma longifolia Jack (known as Tongkat Ali) is a popular traditional herbal medicine, native to southeast Asia, that is well-known for its aphrodisiac as well as several other ...
PMC5560554
core_pubmed_pmc
Targeting of CDK9 with indirubin 3’-monoxime safely and durably reduces HIV viremia in chronically infected humanized mice
Targeting of CDK9 with indirubin 3’-monoxime safely and durably reduces HIV viremia in chronically infected humanized mice Abstract Abstract Successful propagation of HIV in the human host requires entry into a permissive cell, reverse transcription of viral RNA, integration into the human genome, transcription of the ...
PMC8841494
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of itepekimab in healthy adults and patients with asthma: Phase I first‐in‐human and first‐in‐patient trials
Pharmacokinetics and pharmacodynamics of itepekimab in healthy adults and patients with asthma: Phase I first‐in‐human and first‐in‐patient trials Abstract Abstract Itepekimab is a monoclonal antibody that targets interleukin (IL‐33) and has been shown to reduce airway inflammation and associated tissue damage in precl...
PMC4153963
core_pubmed_pmc
Effect of Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on Omeprazole Plasma Pharmacokinetics in Healthy Adults
Effect of Icosapent Ethyl (Eicosapentaenoic Acid Ethyl Ester) on Omeprazole Plasma Pharmacokinetics in Healthy Adults Abstract Abstract Background Icosapent ethyl (IPE) is a high-purity prescription form of eicosapentaenoic acid ethyl ester approved by the US Food and Drug Administration as an adjunct to diet to reduce...
PMC4139609
core_pubmed_pmc
A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters
A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters Abstract Abstract Background Plantago ovata husk therapy could be used in patients with Parkinson disease to reduce the symptoms of gastrointestinal disorders...
PMC8596416
core_pubmed_pmc
Pharmacokinetics and Use‐Testing of Apalutamide Prepared in Aqueous Food Vehicles for Alternative Administration
Pharmacokinetics and Use‐Testing of Apalutamide Prepared in Aqueous Food Vehicles for Alternative Administration Abstract Abstract Patients may have difficulty swallowing a whole daily dose of 240 mg (4 × 60‐mg tablets) of apalutamide. One of the unique properties of apalutamide tablets is easy disintegration and dispe...
PMC10569676
core_pubmed_pmc
Relationship Between Real-time TDM-guided Pharmacodynamic Target Attainment of Continuous Infusion Beta-lactam Monotherapy and Microbiologic Outcome in the Treatment of Critically Ill Children With Severe Documented Gram-negative Infections
Relationship Between Real-time TDM-guided Pharmacodynamic Target Attainment of Continuous Infusion Beta-lactam Monotherapy and Microbiologic Outcome in the Treatment of Critically Ill Children With Severe Documented Gram-negative Infections Abstract Objectives: To explore the relationship between real-time therapeutic ...
PMC12107630
core_pubmed_pmc
Impact of CYP3A5 1* and 3* single nucleotide variants on tacrolimus pharmacokinetics and graft rejection risk in pediatric kidney transplant patients
Impact of CYP3A5 1* and 3* single nucleotide variants on tacrolimus pharmacokinetics and graft rejection risk in pediatric kidney transplant patients Abstract Tacrolimus, a calcineurin inhibitor, is widely used to prevent allograft rejection in kidney transplant recipients. Its metabolism is predominantly mediated by t...
PMC9662207
core_pubmed_pmc
Joint modeling under competing risks: Application to survival prediction in patients admitted in Intensive Care Unit for sepsis with daily Sequential Organ Failure Assessment score assessments
Joint modeling under competing risks: Application to survival prediction in patients admitted in Intensive Care Unit for sepsis with daily Sequential Organ Failure Assessment score assessments Abstract Abstract Joint models of longitudinal process and time‐to‐event data have recently gained attention, notably to provid...
PMC12914500
core_pubmed_pmc
Unravelling Voriconazole's Hepatic Metabolism: A Narrative Review on Factors Impacting Voriconazole‐N‐Oxide Exposure
Unravelling Voriconazole's Hepatic Metabolism: A Narrative Review on Factors Impacting Voriconazole‐N‐Oxide Exposure Abstract ABSTRACT Background Voriconazole (VRC), a triazole antifungal agent, is recommended as primary treatment for invasive aspergillosis. Due to its unpredictable dose‐exposure relationship, therapeu...
PMC10079507
core_pubmed_pmc
Evaluation of pharmacokinetic interactions between lobeglitazone, empagliflozin, and metformin in healthy subjects
Evaluation of pharmacokinetic interactions between lobeglitazone, empagliflozin, and metformin in healthy subjects Abstract Abstract Concomitant administration of lobeglitazone, empagliflozin, and metformin is expected to enhance blood glucose-lowering effects and improve medication compliance in patients with diabetes...
PMC3112027
core_pubmed_pmc
Do pharmacokinetic polymorphisms explain treatment failure in high-risk patients with neuroblastoma?
Do pharmacokinetic polymorphisms explain treatment failure in high-risk patients with neuroblastoma? Abstract Purpose Neuroblastoma is the most common extracranial solid tumour in childhood. It accounts for 15% of all paediatric oncology deaths. In the last few decades, improvement in treatment outcome for high-risk pa...
PMC10498806
core_pubmed_pmc
Development of in silico models to predict viscosity and mouse clearance using a comprehensive analytical data set collected on 83 scaffold-consistent monoclonal antibodies
Development of in silico models to predict viscosity and mouse clearance using a comprehensive analytical data set collected on 83 scaffold-consistent monoclonal antibodies Abstract ABSTRACT Biologic drug discovery pipelines are designed to deliver protein therapeutics that have exquisite functional potency and selecti...
PMC10571049
core_pubmed_pmc
Cannabidiol plasma determination and pharmacokinetics conducted at beginning, middle and end of long-term supplementation of a broad-spectrum hemp oil to healthy adult dogs
Cannabidiol plasma determination and pharmacokinetics conducted at beginning, middle and end of long-term supplementation of a broad-spectrum hemp oil to healthy adult dogs Abstract Abstract Introduction Veterinary hemp products containing cannabidiol (CBD) and negligible psychoactive (THC) have increased popularity si...
PMC8468767
core_pubmed_pmc
Optimisation of a Microfluidic Method for the Delivery of a Small Peptide
Optimisation of a Microfluidic Method for the Delivery of a Small Peptide Abstract Abstract Peptides hold promise as therapeutics, as they have high bioactivity and specificity, good aqueous solubility, and low toxicity. However, they typically suffer from short circulation half-lives in the body. To address this issue...
PMC8451790
core_pubmed_pmc
Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK‐906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo‐Controlled Single‐ and Multiple‐Dose Escalation Study in Healthy Participants
Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK‐906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo‐Controlled Single‐ and Multiple‐Dose Escalation Study in Healthy Participants Abstract Abstract Gastroparesis is a chronic neuromuscular disorder of the upper gastrointe...
PMC6058267
core_pubmed_pmc
The impact of body weight on rivaroxaban pharmacokinetics
The impact of body weight on rivaroxaban pharmacokinetics Abstract Abstract Essentials The optimal dosing strategy of rivaroxaban for patients at the extremes of body weight is not known. A pharmacokinetic study was conducted based in real‐world patients in a London teaching hospital. In the cohort of patients studied,...
PMC10537618
core_pubmed_pmc
Effect of Betanin, the Major Pigment of Red Beetroot ( Beta vulgaris L.), on the Activity of Recombinant Human Cytochrome P450 Enzymes
Effect of Betanin, the Major Pigment of Red Beetroot ( Beta vulgaris L.), on the Activity of Recombinant Human Cytochrome P450 Enzymes Abstract Most of the currently available drugs are derived from natural sources, but they are used only after extensive chemical modifications to improve their safety and efficacy. Natu...
PMC9698634
core_pubmed_pmc
A Physiologically Based Pharmacokinetic (PBPK) Modeling Framework for Mixtures of Dioxin-like Compounds
A Physiologically Based Pharmacokinetic (PBPK) Modeling Framework for Mixtures of Dioxin-like Compounds Abstract Humans are exposed to persistent organic pollutants, such as dioxin-like compounds (DLCs), as mixtures. Understanding and predicting the toxicokinetics and thus internal burden of major constituents of a DLC...
PMC5404337
core_pubmed_pmc
Adverse drug reactions and kinetics of cisplatin excretion in urine of patients undergoing cisplatin chemotherapy and radiotherapy for head and neck cancer: a prospective study
Adverse drug reactions and kinetics of cisplatin excretion in urine of patients undergoing cisplatin chemotherapy and radiotherapy for head and neck cancer: a prospective study Abstract Abstract Background Cisplatin is a high-potency anticancer agent; however, it causes significant adverse drug reactions (ADRs). Potent...
PMC5541360
core_pubmed_pmc
Comparison of Ticagrelor Pharmacokinetics and Pharmacodynamics in STEMI and NSTEMI Patients (PINPOINT): protocol for a prospective, observational, single-centre study
Comparison of Ticagrelor Pharmacokinetics and Pharmacodynamics in STEMI and NSTEMI Patients (PINPOINT): protocol for a prospective, observational, single-centre study Abstract Introduction The most common classification of acute myocardial infarction (AMI) is based on electrocardiographic findings and distinguishes ST-...
PMC5628680
core_pubmed_pmc
In vivo evaluation of cetuximab-conjugated poly(γ-glutamic acid)-docetaxel nanomedicines in EGFR-overexpressing gastric cancer xenografts
In vivo evaluation of cetuximab-conjugated poly(γ-glutamic acid)-docetaxel nanomedicines in EGFR-overexpressing gastric cancer xenografts Abstract Epidermal growth factor receptor (EGFR), upregulated in gastric cancer patients, is an oncogene of interest in the development of targeted cancer nanomedicines. This study d...
PMC12931727
core_pubmed_pmc
Microbiome compositional changes and clonal engraftment in a phase 3 trial of fecal microbiota, live-jslm for recurrent Clostridioides difficile infection
Microbiome compositional changes and clonal engraftment in a phase 3 trial of fecal microbiota, live-jslm for recurrent Clostridioides difficile infection Abstract ABSTRACT Live microbiota therapies have shown promise in many gastrointestinal diseases, including in the prevention of recurrent Clostridioides difficile i...
PMC3675106
core_pubmed_pmc
Vincristine Chemotherapy Trials and Pharmacokinetics in Tasmanian Devils with Tasmanian Devil Facial Tumor Disease
Vincristine Chemotherapy Trials and Pharmacokinetics in Tasmanian Devils with Tasmanian Devil Facial Tumor Disease Abstract Tasmanian Devil Facial Tumor Disease (DFTD) is a transmissible cancer threatening to cause the extinction of Tasmanian Devils in the wild. The aim of this study was to determine the susceptibility...
PMC11511931
core_pubmed_pmc
The regulatory T cell-selective interleukin-2 receptor agonist rezpegaldesleukin in the treatment of inflammatory skin diseases: two randomized, double-blind, placebo-controlled phase 1b trials
The regulatory T cell-selective interleukin-2 receptor agonist rezpegaldesleukin in the treatment of inflammatory skin diseases: two randomized, double-blind, placebo-controlled phase 1b trials Abstract Regulatory T cell (Treg) impairment is implicated in the pathogenesis of chronic inflammatory diseases, but relativel...
PMC2841147
core_pubmed_pmc
The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma
The inhaled phosphodiesterase 4 inhibitor GSK256066 reduces allergen challenge responses in asthma Abstract Abstract GSK256066 is a selective phosphodiesterase 4 inhibitor that can be given by inhalation, minimising the potential for side effects. We evaluated the effects of GSK256066 on airway responses to allergen ch...
PMC9695338
core_pubmed_pmc
Influences of Glimepiride Self-Nanoemulsifying Drug Delivery System Loaded Liquisolid Tablets on the Hypoglycemic Activity and Pancreatic Histopathological Changes in Streptozotocin-Induced Hyperglycemic Rats
Influences of Glimepiride Self-Nanoemulsifying Drug Delivery System Loaded Liquisolid Tablets on the Hypoglycemic Activity and Pancreatic Histopathological Changes in Streptozotocin-Induced Hyperglycemic Rats Abstract The development of an oral anti-diabetic medication characterized by enhanced hypoglycemic activity is...
PMC3469239
core_pubmed_pmc
Long-acting dihydropyridine calcium-channel blockers and sympathetic nervous system activity in hypertension: A literature review comparing amlodipine and nifedipine GITS
Long-acting dihydropyridine calcium-channel blockers and sympathetic nervous system activity in hypertension: A literature review comparing amlodipine and nifedipine GITS Abstract Calcium-channel blockers (CCBs) constitute a diverse group of compounds but are often referred to as a single homogeneous class of drug and ...
PMC3558400
core_pubmed_pmc
P276-00, a cyclin-dependent kinase inhibitor, modulates cell cycle and induces apoptosis in vitro and in vivo in mantle cell lymphoma cell lines
P276-00, a cyclin-dependent kinase inhibitor, modulates cell cycle and induces apoptosis in vitro and in vivo in mantle cell lymphoma cell lines Abstract Abstract Background Mantle cell lymphoma (MCL) is a well-defined aggressive lymphoid neoplasm characterized by proliferation of mature B-lymphocytes that have a remar...
PMC3232196
core_pubmed_pmc
Pharmacogenetic & Pharmacokinetic Biomarker for Efavirenz Based ARV and Rifampicin Based Anti-TB Drug Induced Liver Injury in TB-HIV Infected Patients
Pharmacogenetic & Pharmacokinetic Biomarker for Efavirenz Based ARV and Rifampicin Based Anti-TB Drug Induced Liver Injury in TB-HIV Infected Patients Abstract Abstract Background Implication of pharmacogenetic variations and efavirenz pharmacokinetics in concomitant efavirenz based antiviral therapy and anti-tubercula...
PMC6824394
core_pubmed_pmc
Relative Oral Bioavailability of an Abuse-Deterrent, Immediate-Release Formulation of Oxycodone, Oxycodone ARIR in a Randomized Study
Relative Oral Bioavailability of an Abuse-Deterrent, Immediate-Release Formulation of Oxycodone, Oxycodone ARIR in a Randomized Study Abstract Abstract Introduction Oxycodone ARIR is a novel oral, abuse-deterrent, immediate-release (IR) formulation with physical and chemical properties that deter misuse and abuse by no...
PMC11525524
core_pubmed_pmc
Exploring Thermal Stability, Vibrational Properties, and Biological Assessments of Dichloro( l -histidine)copper(II): A Combined Theoretical and Experimental Study
Exploring Thermal Stability, Vibrational Properties, and Biological Assessments of Dichloro( l -histidine)copper(II): A Combined Theoretical and Experimental Study Abstract Abstract Dichloro( l -histidine)copper(II) crystal ([Cu( l -His)Cl 2 ] complex) was obtained by the slow evaporation method and characterized conce...
PMC9229894
core_pubmed_pmc
In Silico, In Vitro, and Pharmacokinetic Studies of UBMC-4, a Potential Novel Compound for Treating against Trypanosoma cruzi
In Silico, In Vitro, and Pharmacokinetic Studies of UBMC-4, a Potential Novel Compound for Treating against Trypanosoma cruzi Abstract Abstract The lack of therapeutic alternatives for the treatment of Chagas disease, a neglected disease, drives the discovery of new drugs with trypanocidal activity. Consequently, we co...
PMC12202829
core_pubmed_pmc
Cardiovascular and Pharmacokinetic Profiles of Intravenous Etripamil in Conscious Telemetered Cynomolgus Monkeys
Cardiovascular and Pharmacokinetic Profiles of Intravenous Etripamil in Conscious Telemetered Cynomolgus Monkeys Abstract Paroxysmal supraventricular tachycardia (PSVT) is a common cardiac arrhythmia associated with substantial health care burden. Etripamil, a fast-acting non-dihydropyridine calcium channel blocker dev...
PMC12640667
core_pubmed_pmc
Potent Antisickling Furaldehyde Analogs for Acute Sickle Cell Therapy: Enhanced Efficacy and Intravenous Formulation Potential
Potent Antisickling Furaldehyde Analogs for Acute Sickle Cell Therapy: Enhanced Efficacy and Intravenous Formulation Potential Abstract Sickle cell disease (SCD) is a debilitating inherited blood disorder characterized by acute crises that require immediate intervention. Aromatic aldehydes that increase hemoglobin (Hb)...
PMC10870265
core_pubmed_pmc
Oral Release Kinetics, Biodistribution, and Excretion of Dopants from Barium-Containing Bioactive Glass in Rats
Oral Release Kinetics, Biodistribution, and Excretion of Dopants from Barium-Containing Bioactive Glass in Rats Abstract Background : Inorganic biomaterials are biologically active and are used as implants and drug delivery system. They have therapeutically active elements present in their framework that are released i...
PMC6394163
core_pubmed_pmc
Development and Validation of Liquid Chromatography Method for Determination of Glimepiride in Presence of (Vimto ® ) Soft Drinks in Rats: Application to Pharmacokinetics Studies.
Development and Validation of Liquid Chromatography Method for Determination of Glimepiride in Presence of (Vimto ® ) Soft Drinks in Rats: Application to Pharmacokinetics Studies. Abstract Abstract Context: Diet and beverages are thought to have notable effects on drugs. Recently, this relationship has received signifi...
PMC7350388
core_pubmed_pmc
The PK/PD Integration and Resistance of Tilmicosin against Mycoplasma hyopneumoniae
The PK/PD Integration and Resistance of Tilmicosin against Mycoplasma hyopneumoniae Abstract Mycoplasma hyopneumoniae is the major pathogen causing enzootic pneumonia in pigs. M. hyopneumoniae infection can lead to considerable economic losses in the pig-breeding industry. Here, this study established a first-order abs...
PMC7109127
core_pubmed_pmc
A multicentre phase 1b/2 study of tivozanib in patients with advanced inoperable hepatocellular carcinoma
A multicentre phase 1b/2 study of tivozanib in patients with advanced inoperable hepatocellular carcinoma Abstract Background Hepatocellular carcinoma (HCC) is a major cause of cancer-related death. It is a highly vascular tumour with multiple angiogenic factors, most importantly vascular endothelial growth factor (VEG...
PMC8478771
core_pubmed_pmc
Identifying Safety Thresholds for Immunosuppressive Drugs: Applying Insights from Primary Antibody Deficiencies to Mitigate Adverse Events in Secondary Antibody Deficiencies Using Mathematical Modeling of Preclinical and Early Clinical Data
Identifying Safety Thresholds for Immunosuppressive Drugs: Applying Insights from Primary Antibody Deficiencies to Mitigate Adverse Events in Secondary Antibody Deficiencies Using Mathematical Modeling of Preclinical and Early Clinical Data Abstract Immunosuppressive drugs can alleviate debilitating symptoms of autoimm...
PMC9314093
core_pubmed_pmc
Evaluation of pharmacokinetics and safety of talazoparib in patients with advanced cancer and varying degrees of hepatic impairment
Evaluation of pharmacokinetics and safety of talazoparib in patients with advanced cancer and varying degrees of hepatic impairment Abstract Abstract Aim This phase I study investigated talazoparib pharmacokinetics (PK) and safety in patients with advanced solid tumours and varying degrees of hepatic function. Methods ...
PMC12301304
core_pubmed_pmc
Potential induction of the relative mRNA expression levels of CYP450 by Zhicaowu-Hezi (Aconiti kusnezoffii radix preparata and Terminalia chebula Retz.)
Potential induction of the relative mRNA expression levels of CYP450 by Zhicaowu-Hezi (Aconiti kusnezoffii radix preparata and Terminalia chebula Retz.) Abstract Abstract Background Processed Aconiti Kusnezoffii Radix (Aconiti kusnezoffii Radix Preparata, Zhicaowu) and Terminalia chebula Retz. (Hezi) are a classic herb...
PMC10955104
core_pubmed_pmc
Recent advances in carbon monoxide-releasing nanomaterials ☆
Recent advances in carbon monoxide-releasing nanomaterials ☆ Abstract As an endogenous signaling molecule, carbon monoxide (CO) has emerged as an increasingly promising option regarding as gas therapy due to its positive pharmacological effects in various diseases. Owing to the gaseous nature and potential toxicity, it...
PMC5554291
core_pubmed_pmc
Prospective Clinical and Pharmacological Evaluation of the Delcath System’s Second-Generation (GEN2) Hemofiltration System in Patients Undergoing Percutaneous Hepatic Perfusion with Melphalan
Prospective Clinical and Pharmacological Evaluation of the Delcath System’s Second-Generation (GEN2) Hemofiltration System in Patients Undergoing Percutaneous Hepatic Perfusion with Melphalan Abstract Abstract Introduction Percutaneous hepatic perfusion (PHP) with melphalan is an effective treatment for patients with h...
PMC10620120
core_pubmed_pmc
Serine protease inhibitors decrease metastasis in prostate, breast, and ovarian cancers
Serine protease inhibitors decrease metastasis in prostate, breast, and ovarian cancers Abstract Targeted therapies for prostate, breast, and ovarian cancers are based on their activity against primary tumors rather than their anti‐metastatic activity. Consequently, there is an urgent need for new agents targeting the ...
PMC11762134
core_pubmed_pmc
Activity of Aztreonam-avibactam and other β-lactamase inhibitor combinations against Gram-negative bacteria isolated from patients hospitalized with pneumonia in United States medical centers (2020–2022)
Activity of Aztreonam-avibactam and other β-lactamase inhibitor combinations against Gram-negative bacteria isolated from patients hospitalized with pneumonia in United States medical centers (2020–2022) Abstract Background Initial antimicrobial therapy for pneumonia is frequently empirical and resistance to antimicrob...
PMC9542796
core_pubmed_pmc
Bridging Efficacy of Tofacitinib Immediate‐Release to Extended‐Release Formulations for Treatment of Ulcerative Colitis: Application of a Model‐Informed Drug Development Approach
Bridging Efficacy of Tofacitinib Immediate‐Release to Extended‐Release Formulations for Treatment of Ulcerative Colitis: Application of a Model‐Informed Drug Development Approach Abstract Abstract Tofacitinib is an oral, small molecule Janus kinase inhibitor for the treatment of ulcerative colitis (UC). We report a mod...
PMC12566952
core_pubmed_pmc
Virtual Bioequivalence Assessment and Dissolution Safe Space Exploration for Fixed-Dose Metformin–Glyburide Tablet Using Physiologically Based Biopharmaceutics Modeling
Virtual Bioequivalence Assessment and Dissolution Safe Space Exploration for Fixed-Dose Metformin–Glyburide Tablet Using Physiologically Based Biopharmaceutics Modeling Abstract Abstract Background/Objectives : Fixed-dose combinations (FDCs) hold significant clinical value for the management of hypertension, diabetes a...
PMC12165324
core_pubmed_pmc
Impact of Renal Impairment on the Pharmacodynamic and Pharmacokinetic Profiles of Epaminurad, a Novel Uric Acid Transporter 1 Inhibitor
Impact of Renal Impairment on the Pharmacodynamic and Pharmacokinetic Profiles of Epaminurad, a Novel Uric Acid Transporter 1 Inhibitor Abstract ABSTRACT Epaminurad, a novel uricosuric agent, exhibits potent inhibitory activity against the human uric acid transporter. This study aimed to investigate the effects of rena...
PMC12638730
core_pubmed_pmc
Phase I Randomized, Placebo-Controlled, Cross-Over Dose-Finding Study of Coenzyme Q10 on Doxorubicin Pharmacokinetics during Breast Cancer Treatment
Phase I Randomized, Placebo-Controlled, Cross-Over Dose-Finding Study of Coenzyme Q10 on Doxorubicin Pharmacokinetics during Breast Cancer Treatment Abstract Abstract Aim: To determine effects of Coenzyme Q10 (CoQ10) supplementation in breast cancer patients receiving doxorubicin treatment. Methods: Phase I randomized,...
PMC4767723
core_pubmed_pmc
Effects of Fostamatinib on the Pharmacokinetics of Oral Contraceptive, Warfarin, and the Statins Rosuvastatin and Simvastatin: Results From Phase I Clinical Studies
Effects of Fostamatinib on the Pharmacokinetics of Oral Contraceptive, Warfarin, and the Statins Rosuvastatin and Simvastatin: Results From Phase I Clinical Studies Abstract Abstract Background and objectives Fostamatinib is a spleen tyrosine kinase inhibitor that has been investigated as therapy for rheumatoid arthrit...
PMC8545549
core_pubmed_pmc
Paclitaxel: Application in Modern Oncology and Nanomedicine-Based Cancer Therapy
Paclitaxel: Application in Modern Oncology and Nanomedicine-Based Cancer Therapy Abstract Abstract Paclitaxel is a broad-spectrum anticancer compound, which was derived mainly from a medicinal plant, in particular, from the bark of the yew tree Taxus brevifolia Nutt. It is a representative of a class of diterpene taxan...
PMC11843794
core_pubmed_pmc
Haloperidol dopamine receptor occupancy and antagonism correspond to delirium agitation scores and EPS risk: A PBPK-PD modeling analysis
Haloperidol dopamine receptor occupancy and antagonism correspond to delirium agitation scores and EPS risk: A PBPK-PD modeling analysis Abstract Background: Delirium is a severe neuropsychiatric disorder associated with increased morbidity and mortality. Numerous precipitating factors and etiologies merge into the pat...
PMC7506777
core_pubmed_pmc
Effect of pharmacokinetic/pharmacodynamic ratio on tigecycline clinical response and toxicity in critically ill patients with multidrug-resistant Gram-negative infections
Effect of pharmacokinetic/pharmacodynamic ratio on tigecycline clinical response and toxicity in critically ill patients with multidrug-resistant Gram-negative infections Abstract Abstract Introduction: The information about the pharmacokinetics and optimal dose of tigecycline in critically ill patients with severe und...
PMC12114997
core_pubmed_pmc
Risk of Potentially Neurotoxic Exposure in Infants Under High-Dose Cefepime Treatment—A Pharmacometric Simulation Study
Risk of Potentially Neurotoxic Exposure in Infants Under High-Dose Cefepime Treatment—A Pharmacometric Simulation Study Abstract Background: Optimal dosing of cefepime in infants 1–2 months remains undefined. Objectives : We aimed to quantify the risk of potentially neurotoxic exposure with high-dose cefepime (50 mg/kg...
PMC12297938
core_pubmed_pmc
Tunable Intranasal Polymersome Nanocarriers Triggered Olanzapine Brain Delivery and Improved In Vivo Antipsychotic Activity
Tunable Intranasal Polymersome Nanocarriers Triggered Olanzapine Brain Delivery and Improved In Vivo Antipsychotic Activity Abstract Abstract Background : Olanzapine (Ola) is a second-generation antipsychotic with clinical utility limited by poor brain bioavailability due to blood–brain barrier restriction, hepatic fir...
PMC3104459
core_pubmed_pmc
Teicoplanin Dosing Strategy for Treatment of Staphylococcus aureus in Korean Patients with Neutropenic Fever
Teicoplanin Dosing Strategy for Treatment of Staphylococcus aureus in Korean Patients with Neutropenic Fever Abstract Abstract Purpose The present study was conducted to determine and compare the target attainment rate (TAR) between microorganism-nonspecific (C trough ) and microorganism-specific (AUC 24 /MIC) targets ...
PMC12468763
core_pubmed_pmc
New chalcone compound exhibits microrna-mediated anticancer properties in glioblastoma
New chalcone compound exhibits microrna-mediated anticancer properties in glioblastoma Abstract Abstract Background Therapy-resistant glioblastoma constitutes the most lethal adult brain malignancy, bearing extremely poor patients’ prognosis. Combinational therapies are accompanied by severe side effects and significan...
PMC7541708
core_pubmed_pmc
First‐in‐Human Studies of MW01‐6‐189WH, a Brain‐Penetrant, Antineuroinflammatory Small‐Molecule Drug Candidate: Phase 1 Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Studies in Healthy Adult Volunteers
First‐in‐Human Studies of MW01‐6‐189WH, a Brain‐Penetrant, Antineuroinflammatory Small‐Molecule Drug Candidate: Phase 1 Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Studies in Healthy Adult Volunteers Abstract Abstract MW01‐6‐189WH (MW189) is a novel central nervous system–penetrant small‐molecule drug ca...
PMC10675244
core_pubmed_pmc
A Physiologically Based Pharmacokinetic Approach to Recommend an Individual Dose of Tacrolimus in Adult Heart Transplant Recipients
A Physiologically Based Pharmacokinetic Approach to Recommend an Individual Dose of Tacrolimus in Adult Heart Transplant Recipients Abstract Tacrolimus is the principal immunosuppressive drug which is administered after heart transplantation. Managing tacrolimus therapy is challenging due to a narrow therapeutic index ...
PMC5057311
core_pubmed_pmc
Multiplexing of receptor occupancy measurements for pharmacodynamic biomarker assessment of biopharmaceuticals
Multiplexing of receptor occupancy measurements for pharmacodynamic biomarker assessment of biopharmaceuticals Abstract Background Receptor occupancy (RO) assays measure drug target engagement, and are used as pharmacodynamic (PD) biomarkers. RO assays are commonly performed by flow cytometry and often require multiple...
PMC4700386
core_pubmed_pmc
Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial
Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial Abstract Summary Background Artefenomel (OZ439) is a novel synthetic trioxolane with improved pharmacokinetic properties compared wi...
PMC12478331
core_pubmed_pmc
Spatial‐hindrance‐based pro‐Adalimumab prevents anti‐idiotypic antibody interference in pharmacokinetic and therapeutic efficacy
Spatial‐hindrance‐based pro‐Adalimumab prevents anti‐idiotypic antibody interference in pharmacokinetic and therapeutic efficacy Abstract Abstract Adalimumab (Humira) represents a major advance in rheumatoid arthritis (RA) therapy. However, with long‐term administration of Adalimumab, anti‐idiotypic antibody (anti‐Id A...
PMC8241153
core_pubmed_pmc
Systemic effects of angiogenesis inhibition alter pharmacokinetics and intratumoral delivery of nab -paclitaxel
Systemic effects of angiogenesis inhibition alter pharmacokinetics and intratumoral delivery of nab -paclitaxel Abstract Abstract Angiogenesis is critical to the growth of tumors. Vascularization-targeting agents, with or without cytotoxic drugs, are widely used for the treatment of several solid tumors including esoph...
PMC7160569
core_pubmed_pmc
Computational studies of a series of 2-substituted phenyl-2-oxo-, 2-hydroxyl- and 2-acylloxyethylsulfonamides as potent anti-fungal agents
Computational studies of a series of 2-substituted phenyl-2-oxo-, 2-hydroxyl- and 2-acylloxyethylsulfonamides as potent anti-fungal agents Abstract Botrytis Cinerea is a plant pathogen that affect a large number of plant species like tomatoes, Lettuce, Grapes, and Strawberries among others. Sulfonamides are widely used...
PMC11597902
core_pubmed_pmc
Potential Protective Effect of Orlistat: A Formulation of Nanocrystals Targeting Inflammation, Oxidative Stress, and Apoptosis in an Experimental Model of Doxorubicin-Induced Cardiotoxicity
Potential Protective Effect of Orlistat: A Formulation of Nanocrystals Targeting Inflammation, Oxidative Stress, and Apoptosis in an Experimental Model of Doxorubicin-Induced Cardiotoxicity Abstract Background : Doxorubicin (DOX) is a widely used chemotherapeutic agent; nevertheless, cardiotoxicity limits its effective...
PMC9531608
core_pubmed_pmc
Multiple Dose Pharmacokinetics of Tapentadol Oral Solution for the Treatment of Moderate to Severe Acute Pain in Children Aged 2 to <7 Years
Multiple Dose Pharmacokinetics of Tapentadol Oral Solution for the Treatment of Moderate to Severe Acute Pain in Children Aged 2 to <7 Years Abstract Background This prospective, open-label trial was conducted to fulfil a post-approval commitment made to the competent authorities to extend the indication of the strong ...
PMC6920765
core_pubmed_pmc
Population Pharmacokinetics Modelling and Simulation of Mitotane in Patients with Adrenocortical Carcinoma: An Individualized Dose Regimen to Target All Patients at Three Months?
Population Pharmacokinetics Modelling and Simulation of Mitotane in Patients with Adrenocortical Carcinoma: An Individualized Dose Regimen to Target All Patients at Three Months? Abstract Mitotane is the most effective agent in post-operative treatment of adrenocortical carcinoma. In adults, the starting dose is 2–3 g/...
PMC9144775
core_pubmed_pmc
Physiologically-Based Pharmacokinetics Modeling for Hydroxychloroquine as a Treatment for Malaria and Optimized Dosing Regimens for Different Populations
Physiologically-Based Pharmacokinetics Modeling for Hydroxychloroquine as a Treatment for Malaria and Optimized Dosing Regimens for Different Populations Abstract Malaria is a severe parasite infectious disease with high fatality. As one of the approved treatments of this disease, hydroxychloroquine (HCQ) lacks clinica...
PMC7994227
core_pubmed_pmc
Evaluation of tramadol human pharmacokinetics and safety after co-administration of magnesium ions in randomized, single- and multiple-dose studies
Evaluation of tramadol human pharmacokinetics and safety after co-administration of magnesium ions in randomized, single- and multiple-dose studies Abstract Background Magnesium ions (Mg 2+ ) increase and prolong opioid analgesia in chronic and acute pain. The nature of this synergistic analgesic interaction has not ye...
PMC8048549
core_pubmed_pmc
Prediction of Fracture Risk From Early‐Stage Bone Markers in Patients With Osteoporosis Treated With Once‐Yearly Administered Zoledronic Acid
Prediction of Fracture Risk From Early‐Stage Bone Markers in Patients With Osteoporosis Treated With Once‐Yearly Administered Zoledronic Acid Abstract Abstract The prevention of fractures is the ultimate goal of osteoporosis treatments. To achieve this objective, developing a method to predict fracture risk in the earl...
PMC12765438
core_pubmed_pmc
Longitudinal pharmacokinetic and safety studies of an antibody-erythropoietin fusion protein for Alzheimer's disease
Longitudinal pharmacokinetic and safety studies of an antibody-erythropoietin fusion protein for Alzheimer's disease Abstract Abstract Erythropoietin (EPO) shows promise for Alzheimer's disease (AD) but has poor brain penetration, necessitating high doses that cause hematopoietic side effects. To improve brain delivery...
PMC9297210
core_pubmed_pmc
Potential new fluoroquinolone treatments for suspected bacterial keratitis
Potential new fluoroquinolone treatments for suspected bacterial keratitis Abstract Abstract Topical fluoroquinolones (FQs) are an established treatment for suspected microbial keratitis. An increased FQ resistance in some classes of bacterial pathogens is a concern. Some recently developed FQs have an extended spectru...
PMC9322514
core_pubmed_pmc
A Physiologically Based Pharmacokinetic and Pharmacodynamic Model of the CYP3A4 Substrate Felodipine for Drug–Drug Interaction Modeling
A Physiologically Based Pharmacokinetic and Pharmacodynamic Model of the CYP3A4 Substrate Felodipine for Drug–Drug Interaction Modeling Abstract Abstract The antihypertensive felodipine is a calcium channel blocker of the dihydropyridine type, and its pharmacodynamic effect directly correlates with its plasma concentra...
PMC11139746
core_pubmed_pmc
Combined whole-body dynamic and static PET/CT with low-dose [ 18 F]PSMA-1007 in prostate cancer patients
Combined whole-body dynamic and static PET/CT with low-dose [ 18 F]PSMA-1007 in prostate cancer patients Abstract Abstract Aim In addition to significant improvements in sensitivity and image quality, the recent introduction of long axial field-of-view (LAFOV) PET/CT scanners has enabled dynamic whole-body imaging for ...
PMC11822664
core_pubmed_pmc
First‐In‐Human Dose Finding Study of Venadaparib ( IDX ‐1197), a Potent and Selective PARP Inhibitor, in Patients With Advanced Solid Tumors
First‐In‐Human Dose Finding Study of Venadaparib ( IDX ‐1197), a Potent and Selective PARP Inhibitor, in Patients With Advanced Solid Tumors Abstract ABSTRACT Background Venadaparib, a novel poly (ADP‐ribose) polymerase (PARP) inhibitor, has demonstrated high PARP‐1/2 selectivity over other PARP family members and exhi...
PMC11181028
core_pubmed_pmc
3D computer modeling of inhibitors targeting the MCF-7 breast cancer cell line
3D computer modeling of inhibitors targeting the MCF-7 breast cancer cell line Abstract Abstract This study focused on developing new inhibitors for the MCF-7 cell line to contribute to our understanding of breast cancer biology and various experimental techniques. 3D QSAR modeling was used to design new tetrahydrobenz...
PMC9546385
core_pubmed_pmc
The [ 13 C ]octanoic acid breath test for gastric emptying quantification: A focus on nutrition and modeling
The [ 13 C ]octanoic acid breath test for gastric emptying quantification: A focus on nutrition and modeling Abstract Abstract Gastric emptying (GE) is the process of food being processed by the stomach and delivered to the small intestine where nutrients such as lipids are absorbed into the blood circulation. The comb...
PMC12853688
core_pubmed_pmc
The NewroBus platform: engineered humanized anti-TfR1 nanobodies for efficient brain delivery
The NewroBus platform: engineered humanized anti-TfR1 nanobodies for efficient brain delivery Abstract Background Delivery of biologic therapeutics to the central nervous system (CNS) is hindered by the blood–brain barrier (BBB), which restricts large molecule passage. Receptor-mediated transcytosis via transferrin rec...
PMC10892260
core_pubmed_pmc
Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation
Nanoparticles of Thiolated Xanthan Gum for the Oral Delivery of Miconazole Nitrate: In Vitro and In Vivo Evaluation Abstract Abstract The objective of this research was to develop a mucoadhesive delivery system that improves permeation for the administration of poorly absorbed oral medications. Thiolation of xanthan gu...
PMC4335132
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Nebulized Sodium Nitrite (AIR001) Following Repeat-Dose Inhalation in Healthy Subjects
Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Nebulized Sodium Nitrite (AIR001) Following Repeat-Dose Inhalation in Healthy Subjects Abstract Introduction The efficacy of nebulized sodium nitrite (AIR001) has been demonstrated in animal models of pulmonary arterial hypertension (PAH), but it was not k...
PMC12649081
core_pubmed_pmc
Characterization of intramuscular Isoflupredone acetate in horses: pharmacokinetics and effects on anti-inflammatory mediators and plasma electrolytes
Characterization of intramuscular Isoflupredone acetate in horses: pharmacokinetics and effects on anti-inflammatory mediators and plasma electrolytes Abstract Abstract Background Corticosteroids, such as isoflupredone, are effective anti-inflammatory medications and as such are commonly used to treat inflammation asso...
PMC7066310
core_pubmed_pmc
The effect for hyperuricemia inpatient of uric acid overproduction type or in combination with topiroxostat on the pharmacokinetics, pharmacodynamics and safety of dotinurad, a selective urate reabsorption inhibitor
The effect for hyperuricemia inpatient of uric acid overproduction type or in combination with topiroxostat on the pharmacokinetics, pharmacodynamics and safety of dotinurad, a selective urate reabsorption inhibitor Abstract Abstract Background Dotinurad, a novel selective urate reabsorption inhibitor (SURI), increases...
PMC12142322
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic relationship of a novel pleuromutilin derivative p -furoylamphenmulin against Mycoplasma gallisepticum in vivo in chickens
Pharmacokinetic/pharmacodynamic relationship of a novel pleuromutilin derivative p -furoylamphenmulin against Mycoplasma gallisepticum in vivo in chickens Abstract Abstract Mycoplasma gallisepticum ( M. gallisepticum , MG ) is the primary pathogen of chronic respiratory disease ( CRD ) in chickens and leads to pneumoni...
PMC11011119
core_pubmed_pmc
Stereoselective Pharmacokinetics of Ketamine Administered at a Low Dose in Awake Dogs
Stereoselective Pharmacokinetics of Ketamine Administered at a Low Dose in Awake Dogs Abstract Abstract Simple Summary Ketamine is commonly recommended as an adjunct to analgesic drugs, particularly in the postoperative care of hospitalized patients. Utilizing low doses is advised to target antinociceptive concentratio...
PMC9323574
core_pubmed_pmc
In Vitro Anatomical Models for Nasal Drug Delivery
In Vitro Anatomical Models for Nasal Drug Delivery Abstract Abstract Nasal drug delivery has been utilized for locally acting diseases for decades. The nose is also a portal to the systemic circulation and central nervous system (CNS). In the age of SARS-CoV2, the development of nasal sprays for vaccination and prophyl...
PMC8664201
core_pubmed_pmc
Pharmacokinetics and drug-likeness of antidiabetic flavonoids: Molecular docking and DFT study
Pharmacokinetics and drug-likeness of antidiabetic flavonoids: Molecular docking and DFT study Abstract Abstract Computer aided toxicity and pharmacokinetic prediction studies attracted the attention of pharmaceutical industries as an alternative means to predict potential drug candidates. In the present study, in-sili...
PMC9314283
core_pubmed_pmc
Quality Assurance of PBPK Modeling Platforms and Guidance on Building, Evaluating, Verifying and Applying PBPK Models Prudently under the Umbrella of Qualification: Why, When, What, How and By Whom?
Quality Assurance of PBPK Modeling Platforms and Guidance on Building, Evaluating, Verifying and Applying PBPK Models Prudently under the Umbrella of Qualification: Why, When, What, How and By Whom? Abstract Modeling and simulation emerges as a fundamental asset of drug development. Mechanistic modeling builds upon its...
PMC7076505
core_pubmed_pmc
Drug Flux Across RPE Cell Models: The Hunt for An Appropriate Outer Blood–Retinal Barrier Model for Use in Early Drug Discovery
Drug Flux Across RPE Cell Models: The Hunt for An Appropriate Outer Blood–Retinal Barrier Model for Use in Early Drug Discovery Abstract The retinal pigment epithelial (RPE) cell monolayer forms the outer blood–retinal barrier and has a crucial role in ocular pharmacokinetics. Although several RPE cell models are avail...