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PMC6288471
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of an Oral Formulation of Apixaban in Horses After Oral and Intravenous Administration
Pharmacokinetics and Pharmacodynamics of an Oral Formulation of Apixaban in Horses After Oral and Intravenous Administration Abstract Abstract Horses with inflammatory and infectious disorders are often treated with injectable heparin anticoagulants to prevent thrombotic complications. In humans, a new class of direct ...
PMC10491557
core_pubmed_pmc
Potentially Harmful Drug–Drug Interactions and Their Associated Factors Among Hospitalized Cardiac Patients: A Cross-Sectional Study
Potentially Harmful Drug–Drug Interactions and Their Associated Factors Among Hospitalized Cardiac Patients: A Cross-Sectional Study Abstract Background Cardiovascular diseases are responsible for a significant proportion of mortalities worldwide. Elderly patients are the most affected by cardiovascular diseases, and b...
PMC9155615
core_pubmed_pmc
Pharmacokinetics of First-Line Drugs in Children With Tuberculosis, Using World Health Organization–Recommended Weight Band Doses and Formulations
Pharmacokinetics of First-Line Drugs in Children With Tuberculosis, Using World Health Organization–Recommended Weight Band Doses and Formulations Abstract Abstract Background Dispersible pediatric fixed-dose combination (FDC) tablets delivering higher doses of first-line antituberculosis drugs in World Health Organiza...
PMC12704320
core_pubmed_pmc
Non-linear pharmacokinetics of penciclovir in healthy cats after single and multiple oral administration of famciclovir
Non-linear pharmacokinetics of penciclovir in healthy cats after single and multiple oral administration of famciclovir Abstract Introduction Feline Infectious Rhinobronchitis (FVR) is a common and serious infectious upper respiratory disease. Famciclovir, an antiviral prodrug initially developed for human herpesviruse...
PMC5391214
core_pubmed_pmc
Association of genetic variations with pharmacokinetics and lipid-lowering response to atorvastatin in healthy Korean subjects
Association of genetic variations with pharmacokinetics and lipid-lowering response to atorvastatin in healthy Korean subjects Abstract Background Statins are effective agents in the primary and secondary prevention of cardiovascular disease, but treatment response to statins varies among individuals. We analyzed multi...
PMC8347666
core_pubmed_pmc
Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats
Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats Abstract The aim of the present research was to describe the consequences of hyperlipidemia (HL) on the pharmacokinetics of glibenclamide (Gb) in poloxamer 407-induced hyperlipidemic rats. Rats were given intraperitoneal dose of p...
PMC7322745
core_pubmed_pmc
Effects of gut microbiota on the pharmacokinetics of protopanaxadiol ginsenosides Rd, Rg3, F2, and compound K in healthy volunteers treated orally with red ginseng
Effects of gut microbiota on the pharmacokinetics of protopanaxadiol ginsenosides Rd, Rg3, F2, and compound K in healthy volunteers treated orally with red ginseng Abstract Abstract Background It is well recognized that gut microbiota is involved in the biotransformation of ginsenosides by converting the polar ginsenos...
PMC11168663
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of intravenously and subcutaneously administered pantoprazole in sheep ( Ovis aries )
Pharmacokinetics and pharmacodynamics of intravenously and subcutaneously administered pantoprazole in sheep ( Ovis aries ) Abstract Abstract Abomasal ulcers are recognized in sheep of all ages, but research regarding therapeutic interventions is limited. Proton Pump Inhibitors (PPIs) such as pantoprazole, are clinical...
PMC10960884
core_pubmed_pmc
Exposure–Response Efficacy Modeling to Support Trofinetide Dosing in Individuals with Rett Syndrome
Exposure–Response Efficacy Modeling to Support Trofinetide Dosing in Individuals with Rett Syndrome Abstract Abstract Introduction Trofinetide was recently approved for the treatment of Rett syndrome (RTT) on the basis of the efficacy and safety findings of the phase 3 LAVENDER study, which used a body weight-based dos...
PMC4858693
core_pubmed_pmc
Triple combination MPT vaginal microbicide using curcumin and efavirenz loaded lactoferrin nanoparticles
Triple combination MPT vaginal microbicide using curcumin and efavirenz loaded lactoferrin nanoparticles Abstract We report that a combination of anti-HIV-1 drug efavirenz (EFV), anti-microbial-spermicidal curcumin (Cur) and lactoferrin nanoparticles (ECNPs) act as MPT formulation. These nanoparticles are of well dispe...
PMC7899551
core_pubmed_pmc
Phase 1 study of Z-endoxifen in patients with advanced gynecologic, desmoid, and hormone receptor-positive solid tumors
Phase 1 study of Z-endoxifen in patients with advanced gynecologic, desmoid, and hormone receptor-positive solid tumors Abstract Abstract Background: Differential responses to tamoxifen may be due to inter-patient variability in tamoxifen metabolism into pharmacologically active Z-endoxifen. Z-endoxifen administration ...
PMC11545717
core_pubmed_pmc
Determining the Pharmacokinetic Properties of Two Different Doses of Meloxicam in Barred Owls ( Strix varia )
Determining the Pharmacokinetic Properties of Two Different Doses of Meloxicam in Barred Owls ( Strix varia ) Abstract Simple Summary Wildlife are negatively affected by human activities, and these encounters often lead to traumatic injuries requiring treatment. Unfortunately, our understanding of analgesics for injure...
PMC9188223
core_pubmed_pmc
Fluazuron orally administered to guinea pigs: pharmacokinetic and efficacy against Amblyomma sculptum
Fluazuron orally administered to guinea pigs: pharmacokinetic and efficacy against Amblyomma sculptum Abstract Background Brazilian spotted fever (BSF), the most lethal tick-borne disease in the Western Hemisphere, is caused by the bacterium Rickettsia rickettsii and transmitted by the bite of Amblyomma sculptum . Capy...
PMC12332861
core_pubmed_pmc
Single Ascending-Dose Study of Selective ErbB4 Agonist JK07 in Heart Failure With Reduced Ejection Fraction
Single Ascending-Dose Study of Selective ErbB4 Agonist JK07 in Heart Failure With Reduced Ejection Fraction Abstract Highlights • JK07 is a complex biologic consisting of the active domain of a fully human recombinant neuregulin-1 fused with an ErbB3 antagonist antibody, designed to selectively stimulate ErbB4. • Fourt...
PMC12185637
core_pubmed_pmc
Clinical Pharmacology of Loop Diuretics in Critical Care
Clinical Pharmacology of Loop Diuretics in Critical Care Abstract Abstract Loop diuretics are a cornerstone in the management of fluid overload in critically ill patients; however, their use is often complicated by variable pharmacokinetics and the phenomenon of diuretic resistance. This narrative review comprehensivel...
PMC5340827
core_pubmed_pmc
Pharmacokinetics and Bioavailability of the GnRH Analogs in the Form of Solution and Zn 2+ -Suspension After Single Subcutaneous Injection in Female Rats
Pharmacokinetics and Bioavailability of the GnRH Analogs in the Form of Solution and Zn 2+ -Suspension After Single Subcutaneous Injection in Female Rats Abstract Background and Objectives Although many synthetic gonadoliberin analogs have been developed, only a few of them, including buserelin, were introduced into cl...
PMC12313450
core_pubmed_pmc
Evaluation of amoxicillin and benzylpenicillin therapy in early-onset neonatal sepsis: a pharmacometric external validation and simulation study
Evaluation of amoxicillin and benzylpenicillin therapy in early-onset neonatal sepsis: a pharmacometric external validation and simulation study Abstract Abstract Background and objectives Early-onset sepsis (EOS) poses a significant morbidity and mortality risk in neonates, for which early diagnosis and adequate antib...
PMC11570885
core_pubmed_pmc
Preclinical characterization of MTX-101: a novel bispecific CD8 Treg modulator that restores CD8 Treg functions to suppress pathogenic T cells in autoimmune diseases
Preclinical characterization of MTX-101: a novel bispecific CD8 Treg modulator that restores CD8 Treg functions to suppress pathogenic T cells in autoimmune diseases Abstract Introduction Regulatory CD8 T cells (CD8 Treg) are responsible for the selective killing of self-reactive and pathogenic CD4 T cells. In autoimmu...
PMC7398703
core_pubmed_pmc
Antipsychotics drug aripiprazole as a lead against breast cancer cell line (MCF-7) in vitro
Antipsychotics drug aripiprazole as a lead against breast cancer cell line (MCF-7) in vitro Abstract Breast cancer is the second leading cause of death among women globally. The existing treatment options for breast cancer are largely associated with severe toxicities, and lower efficacies. Therefore, there is an urgen...
PMC6933454
core_pubmed_pmc
Sotatercept Safety and Effects on Hemoglobin, Bone, and Vascular Calcification
Sotatercept Safety and Effects on Hemoglobin, Bone, and Vascular Calcification Abstract Abstract Introduction Patients with end-stage kidney disease (ESKD) exhibit anemia, chronic kidney disease‒mineral bone disorder (CKD–MBD), and cardiovascular disease. The REN-001 and REN-002 phase II, multicenter, randomized studie...
PMC10121353
core_pubmed_pmc
Pharmacodynamic Material Basis and Potential Mechanism Study of Spatholobi Caulis in Reversing Osteoporosis
Pharmacodynamic Material Basis and Potential Mechanism Study of Spatholobi Caulis in Reversing Osteoporosis Abstract Abstract Objective To elucidate the mechanism of Spatholobi Caulis (SC) in treating osteoporosis (OP) integrated zebrafish model and bioinformatics. Methods Skeleton staining coupled with image quantific...
PMC5760785
core_pubmed_pmc
Development and validation of analytical method for the estimation of lamivudine in rabbit plasma
Development and validation of analytical method for the estimation of lamivudine in rabbit plasma Abstract Abstract Lamivudine has been widely used in the treatment of HIV disease. A reliable, sensitive reversed phase high performance liquid chromatography (RP-HPLC) method was developed and validated for lamivudine in ...
PMC11285397
core_pubmed_pmc
Smoking reduction using an electronic nicotine delivery system (ENDS) with nicotine delivery similar to combustible cigarettes
Smoking reduction using an electronic nicotine delivery system (ENDS) with nicotine delivery similar to combustible cigarettes Abstract Abstract Background Electronic nicotine delivery systems (ENDS) offer a promising approach to tobacco harm reduction, but many people use both ENDS and combustible cigarettes (“dual us...
PMC7004556
core_pubmed_pmc
First‐in‐human phase I study of E7090, a novel selective fibroblast growth factor receptor inhibitor, in patients with advanced solid tumors
First‐in‐human phase I study of E7090, a novel selective fibroblast growth factor receptor inhibitor, in patients with advanced solid tumors Abstract Abstract Fibroblast growth factor receptors (FGFR) are a family of transmembrane receptor tyrosine kinases involved in regulating cellular processes. FGFR mutations are i...
PMC11060733
core_pubmed_pmc
Drug-regulated CD33-targeted CAR T cells control AML using clinically optimized rapamycin dosing
Drug-regulated CD33-targeted CAR T cells control AML using clinically optimized rapamycin dosing Abstract Chimeric antigen receptor (CAR) designs that incorporate pharmacologic control are desirable; however, designs suitable for clinical translation are needed. We designed a fully human, rapamycin-regulated drug produ...
PMC9680514
core_pubmed_pmc
Rates of Divergent Pharmacogenes in a Psychiatric Cohort of Inpatients with Depression—Arguments for Preemptive Testing
Rates of Divergent Pharmacogenes in a Psychiatric Cohort of Inpatients with Depression—Arguments for Preemptive Testing Abstract Background: The international drug agencies annotate pharmacogenes for many years. Pharmacogenetic testing is thus far only established in few settings, assuming that only few patients are ac...
PMC8443777
core_pubmed_pmc
Advances in Chemical Constituents, Clinical Applications, Pharmacology, Pharmacokinetics and Toxicology of Erigeron breviscapus
Advances in Chemical Constituents, Clinical Applications, Pharmacology, Pharmacokinetics and Toxicology of Erigeron breviscapus Abstract Dengzhanxixin (DZXX), the dried whole plant of Erigeron breviscapus (Vaniot) Hand.-Mazz., belonging to Compositae and first published in Materia Medica of South Yunnan by Lan Mao in t...
PMC9283706
core_pubmed_pmc
Structural Modification in Anesthetic Drug Development for Prodrugs and Soft Drugs
Structural Modification in Anesthetic Drug Development for Prodrugs and Soft Drugs Abstract Abstract Among the advancements in drug structural modifications, the increased focus on drug metabolic and pharmacokinetic properties in the anesthetic drug design process has led to significant developments. Drug metabolism al...
PMC11495198
core_pubmed_pmc
Self-Nanoemulsifying Drug Delivery System of Morin: A New Approach for Combating Acute Alcohol Intoxication
Self-Nanoemulsifying Drug Delivery System of Morin: A New Approach for Combating Acute Alcohol Intoxication Abstract Abstract Purpose Acute alcohol intoxication (AAI) is a life-threatening medical condition resulting from excessive alcohol consumption. Our research revealed the potential of morin (MOR) in treating AAI....
PMC6349786
core_pubmed_pmc
The potential impact of hematocrit correction on evaluation of tacrolimus target exposure in pediatric kidney transplant patients
The potential impact of hematocrit correction on evaluation of tacrolimus target exposure in pediatric kidney transplant patients Abstract Background Tacrolimus is an important immunosuppressive agent with high intra- and inter-individual pharmacokinetic variability and a narrow therapeutic index. As tacrolimus extensi...
PMC8861059
core_pubmed_pmc
In-situ x-ray fluorescence imaging of the endogenous iodine distribution in murine thyroids
In-situ x-ray fluorescence imaging of the endogenous iodine distribution in murine thyroids Abstract X-ray fluorescence imaging (XFI) is a non-invasive detection method of small quantities of elements, which can be excited to emit fluorescence x-ray photons upon irradiation with an incident x-ray beam. In particular, i...
PMC10452719
core_pubmed_pmc
Pharmacodynamic Model of the Dynamic Response of Pseudomonas aeruginosa Biofilms to Antibacterial Treatments
Pharmacodynamic Model of the Dynamic Response of Pseudomonas aeruginosa Biofilms to Antibacterial Treatments Abstract Abstract Accurate pharmacokinetic–pharmacodynamic (PK-PD) models of biofilm treatment could be used to guide formulation and administration strategies to better control bacterial lung infections. To thi...
PMC10728507
core_pubmed_pmc
Adrenaline auto injectors pharmacokinetic/pharmacodynamic studies and potential consequences for clinical practice
Adrenaline auto injectors pharmacokinetic/pharmacodynamic studies and potential consequences for clinical practice Abstract Abstract Background Anaphylaxis is a sudden multisystem allergic reaction which may result in a fatal outcome if not treated promptly. Guidelines worldwide suggest intramuscular adrenaline as the ...
PMC9355056
core_pubmed_pmc
Dipeptidyl peptidase IV inhibition of phytocompounds from Artocarpus champeden (Lour.) Stokes: In silico molecular docking study and ADME-Tox prediction approach
Dipeptidyl peptidase IV inhibition of phytocompounds from Artocarpus champeden (Lour.) Stokes: In silico molecular docking study and ADME-Tox prediction approach Abstract ABSTRACT The present study examines the potential activity prediction based on free binding energy (ΔG) and interaction confirmation of phytocompound...
PMC3996866
core_pubmed_pmc
Potential Synergy Activity of the Novel Ceragenin, CSA-13, against Carbapenem-Resistant Acinetobacter baumannii Strains Isolated from Bacteremia Patients
Potential Synergy Activity of the Novel Ceragenin, CSA-13, against Carbapenem-Resistant Acinetobacter baumannii Strains Isolated from Bacteremia Patients Abstract Abstract Carbapenem-resistant Acinetobacter baumannii is an important cause of nosocomial infections, particularly in patients in the intensive care units. A...
PMC8089108
core_pubmed_pmc
Comparison of Pharmacokinetic, Pharmacodynamic and Tolerability Profiles of CKD-11101, Darbepoetin Alfa (NESP ® ) Biosimilar, to Those of NESP ® After a Single Subcutaneous or Intravenous Administration to Healthy Subjects
Comparison of Pharmacokinetic, Pharmacodynamic and Tolerability Profiles of CKD-11101, Darbepoetin Alfa (NESP ® ) Biosimilar, to Those of NESP ® After a Single Subcutaneous or Intravenous Administration to Healthy Subjects Abstract Introduction Darbepoetin alfa (NESP ® and ARANESP ® ) has a sustained erythropoietic act...
PMC8309192
core_pubmed_pmc
Investigating Ex Vivo Animal Models to Test the Performance of Intravitreal Liposomal Drug Delivery Systems
Investigating Ex Vivo Animal Models to Test the Performance of Intravitreal Liposomal Drug Delivery Systems Abstract Abstract There is a strong need for innovative and efficient drug delivery systems for ocular therapy development. However, testing intravitreal drug delivery systems without using live animals is challe...
PMC12066935
core_pubmed_pmc
Plasma and Urine Pharmacokinetics of Long‐Acting Injectable Omeprazole Following Intramuscular Administrations to Healthy Thoroughbred Horses
Plasma and Urine Pharmacokinetics of Long‐Acting Injectable Omeprazole Following Intramuscular Administrations to Healthy Thoroughbred Horses Abstract ABSTRACT Omeprazole is a gastric acid secretion inhibitor used as an effective anti‐ulcer drug. Based on oral administration studies, its International Screening Limit (...
PMC7960760
core_pubmed_pmc
Repurposing Treatment of Wernicke–Korsakoff Syndrome for Th-17 Cell Immune Storm Syndrome and Neurological Symptoms in COVID-19: Thiamine Efficacy and Safety, In-Vitro Evidence and Pharmacokinetic Profile
Repurposing Treatment of Wernicke–Korsakoff Syndrome for Th-17 Cell Immune Storm Syndrome and Neurological Symptoms in COVID-19: Thiamine Efficacy and Safety, In-Vitro Evidence and Pharmacokinetic Profile Abstract Coronavirus disease identified in 2019 (COVID-19) can be complicated by the Th17 cell-mediated IL-17 proin...
PMC4082882
core_pubmed_pmc
Quercetin Significantly Inhibits the Metabolism of Caffeine, a Substrate of Cytochrome P450 1A2 Unrelated to CYP 1 A 2*1 C (−2964G>A) and *1 F (734C>A) Gene Polymorphisms
Quercetin Significantly Inhibits the Metabolism of Caffeine, a Substrate of Cytochrome P450 1A2 Unrelated to CYP 1 A 2*1 C (−2964G>A) and *1 F (734C>A) Gene Polymorphisms Abstract Abstract Background . Quercetin is abundant in plants and human diets. Previous studies indicated that quercetin inhibited the activity of C...
PMC12144534
core_pubmed_pmc
The impact of sex on blood pressure
The impact of sex on blood pressure Abstract Purpose of review Hypertension is the most prevalent cardiovascular disease worldwide and the leading cause of mortality in both men and women. Despite well documented sex differences in prevalence, risk factors, and treatment responses, current guidelines still fail to take...
PMC9825299
core_pubmed_pmc
Olutasidenib (FT-2102) in patients with relapsed or refractory IDH1 -mutant glioma: A multicenter, open-label, phase Ib/II trial
Olutasidenib (FT-2102) in patients with relapsed or refractory IDH1 -mutant glioma: A multicenter, open-label, phase Ib/II trial Abstract Abstract Background Olutasidenib (FT-2102) is a highly potent, orally bioavailable, brain-penetrant and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). The aim of th...
PMC6058521
core_pubmed_pmc
Multivesicular liposomes for sustained release of bevacizumab in treating laser-induced choroidal neovascularization
Multivesicular liposomes for sustained release of bevacizumab in treating laser-induced choroidal neovascularization Abstract Abstract Bevacizumab is an anti-vascular endothelial growth factor drug that can be used to treat choroidal neovascularization (CNV). Bevacizumab-loaded multivesicular liposomes (Bev-MVLs) have ...
PMC2784073
core_pubmed_pmc
Effect of apomorphine on cognitive performance and sensorimotor gating in humans
Effect of apomorphine on cognitive performance and sensorimotor gating in humans Abstract Introduction Dysfunction of brain dopamine systems is involved in various neuropsychiatric disorders. Challenge studies with dopamine receptor agonists have been performed to assess dopamine receptor functioning, classically using...
PMC4153977
core_pubmed_pmc
Does a Hot Drink Provide Faster Absorption of Paracetamol Than a Tablet? A Pharmacoscintigraphic Study in Healthy Male Volunteers
Does a Hot Drink Provide Faster Absorption of Paracetamol Than a Tablet? A Pharmacoscintigraphic Study in Healthy Male Volunteers Abstract Purpose To investigate the hypothesis that paracetamol is absorbed faster from a hot drink than from a standard tablet using simultaneous scintigraphic imaging and pharmacokinetic s...
PMC4959752
core_pubmed_pmc
Pharmacokinetics in Wistar Rats of 5-[(4-Carboxybutanoyl)Amino]-2-Hydroxybenzoic Acid: A Novel Synthetic Derivative of 5-Aminosalicylic Acid (5-ASA) with Possible Anti-Inflammatory Activity
Pharmacokinetics in Wistar Rats of 5-[(4-Carboxybutanoyl)Amino]-2-Hydroxybenzoic Acid: A Novel Synthetic Derivative of 5-Aminosalicylic Acid (5-ASA) with Possible Anti-Inflammatory Activity Abstract 5-[(4-carboxybutanoyl)amino]-2-hydroxybenzoic acid ( C2 ) is a novel synthetic derivative of 5-aminosalicylic acid (5-ASA...
PMC10515999
core_pubmed_pmc
Anti-thymocyte globulin exposure in patients with diffuse cutaneous systemic sclerosis undergoing autologous haematopoietic stem cell transplantation
Anti-thymocyte globulin exposure in patients with diffuse cutaneous systemic sclerosis undergoing autologous haematopoietic stem cell transplantation Abstract Abstract Introduction: Autologous haematopoietic stem cell transplantation improves event-free survival and lung function and reduces skin thickening in patients...
PMC12956365
core_pubmed_pmc
A Phase 1b Study of Lenvatinib plus Nivolumab in Patients with Unresectable Hepatocellular Carcinoma
A Phase 1b Study of Lenvatinib plus Nivolumab in Patients with Unresectable Hepatocellular Carcinoma Abstract Abstract Introduction Despite recent advances in treatment for unresectable hepatocellular carcinoma (uHCC), median overall survival (OS) in the first-line setting across immune-based combination therapies has ...
PMC8025786
core_pubmed_pmc
Single-Arm, Multicenter Phase I/II Clinical Trial for the Treatment of Envenomings by Massive Africanized Honey Bee Stings Using the Unique Apilic Antivenom
Single-Arm, Multicenter Phase I/II Clinical Trial for the Treatment of Envenomings by Massive Africanized Honey Bee Stings Using the Unique Apilic Antivenom Abstract We evaluated the safety, optimal dose, and preliminary effectiveness of a new-approach Africanized honeybee ( Apis mellifera ) Antivenom (AAV) in a phase ...
PMC8086052
core_pubmed_pmc
The safety, tolerability and pharmacokinetics of niraparib in Japanese patients with solid tumours: results of a phase I dose-escalation study
The safety, tolerability and pharmacokinetics of niraparib in Japanese patients with solid tumours: results of a phase I dose-escalation study Abstract Abstract Background Niraparib is the only poly (adenosine diphosphate-ribose)-polymerase (PARP) inhibitor available as oral monotherapy for maintenance, regardless of B...
PMC12053227
core_pubmed_pmc
A translational physiologically-based pharmacokinetic model for MMAE-based antibody-drug conjugates
A translational physiologically-based pharmacokinetic model for MMAE-based antibody-drug conjugates Abstract The objective of this work was to develop a translational physiologically-based pharmacokinetic (PBPK) model for antibody-drug conjugates (ADCs), using monomethyl auristatin E (MMAE)-based ADCs. A previously est...
PMC6442111
core_pubmed_pmc
Development and effects of tacrolimus-loaded nanoparticles on the inhibition of corneal allograft rejection
Development and effects of tacrolimus-loaded nanoparticles on the inhibition of corneal allograft rejection Abstract Abstract Tacrolimus has been widely applied to prevent organ rejection after transplantation. However, the conventional pharmaceutical formulation of tacrolimus limits its applications in ocular therapy ...
PMC6543330
core_pubmed_pmc
The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics: in vitro and ex vivo Models
The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics: in vitro and ex vivo Models Abstract Prevention strategies against sexual transmission of human immunodeficiency virus (HIV) are essential to curb the rate of new infections. In the absence of a correlate of protection against HIV infection, pre-clinica...
PMC9395488
core_pubmed_pmc
First-in-human study of IM156, a novel potent biguanide oxidative phosphorylation (OXPHOS) inhibitor, in patients with advanced solid tumors
First-in-human study of IM156, a novel potent biguanide oxidative phosphorylation (OXPHOS) inhibitor, in patients with advanced solid tumors Abstract Preclinical models suggest anticancer activity of IM156, a novel biguanide mitochondrial protein complex 1 inhibitor of oxidative phosphorylation (OXPHOS). This first-in-...
PMC5338049
core_pubmed_pmc
Applications of polymers in intraocular drug delivery systems
Applications of polymers in intraocular drug delivery systems Abstract Abstract We are entering a new era of ophthalmic pharmacology where new drugs are rapidly being developed for the treatment of anterior and posterior segment of the eye disease. The pharmacokinetics of drug delivery to the eye remains a very active ...
PMC9963565
core_pubmed_pmc
Design, Characterization and Pharmacokinetic–Pharmacodynamic Evaluation of Poloxamer and Kappa-Carrageenan-Based Dual-Responsive In Situ Gel of Nebivolol for Treatment of Open-Angle Glaucoma
Design, Characterization and Pharmacokinetic–Pharmacodynamic Evaluation of Poloxamer and Kappa-Carrageenan-Based Dual-Responsive In Situ Gel of Nebivolol for Treatment of Open-Angle Glaucoma Abstract Abstract This study developed a dual-responsive in situ gel of nebivolol (NEB), a selective β-adrenergic antagonist. The...
PMC11847257
core_pubmed_pmc
Efficacy, safety, and pharmacokinetics of eribulin as monotherapy or in combination with irinotecan for patients with pediatric rhabdomyosarcoma, non-rhabdomyosarcoma soft tissue sarcoma, or Ewing sarcoma
Efficacy, safety, and pharmacokinetics of eribulin as monotherapy or in combination with irinotecan for patients with pediatric rhabdomyosarcoma, non-rhabdomyosarcoma soft tissue sarcoma, or Ewing sarcoma Abstract Background In this report, we present results from studies of eribulin as monotherapy (Study 223) and in c...
PMC10145603
core_pubmed_pmc
Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery
Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery Abstract The development of effective drug formulations and delivery systems for newly developed or marketed drug molecules remains a significant challenge. These drugs can exhibit polymorphic conversion, poor bioavailability, and systemic ...
PMC8866912
core_pubmed_pmc
Impact of polymorphisms of pharmacokinetics‐related genes and the inflammatory response on the metabolism of voriconazole
Impact of polymorphisms of pharmacokinetics‐related genes and the inflammatory response on the metabolism of voriconazole Abstract Abstract The effects of inflammatory responses and polymorphisms of the genes encoding cytochrome P450 (CYP) ( CYP2C19 and CYP3A5 ), flavin‐containing monooxygenase 3 ( FMO3 ), pregnane X r...
PMC8658079
core_pubmed_pmc
Anti-Xa Activity of Enoxaparin for Prevention of Venous Thromboembolism in Severe Nephrotic Syndrome—A Single Center Prospective Study
Anti-Xa Activity of Enoxaparin for Prevention of Venous Thromboembolism in Severe Nephrotic Syndrome—A Single Center Prospective Study Abstract Severe nephrotic syndrome (NS) is associated with high risk of venous thromboembolic events (VTE), as well as presumably altered heparin pharmacokinetics and pharmacodynamics. ...
PMC7894405
core_pubmed_pmc
A mechanism‐based pharmacokinetic model of remdesivir leveraging interspecies scaling to simulate COVID‐19 treatment in humans
A mechanism‐based pharmacokinetic model of remdesivir leveraging interspecies scaling to simulate COVID‐19 treatment in humans Abstract Abstract The severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) outbreak initiated the global coronavirus disease 2019 (COVID‐19) pandemic resulting in 42.9 million confirmed...
PMC7490523
core_pubmed_pmc
A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Recombinant Human Hyaluronidase PH20 Administered Intravenously in Healthy Volunteers
A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Recombinant Human Hyaluronidase PH20 Administered Intravenously in Healthy Volunteers Abstract Abstract Background Recombinant human hyaluronidase PH20 (rHuPH20) is used in subcutaneous formulations (eg, RITUXAN HYCELA [ritu...
PMC9468560
core_pubmed_pmc
A randomized, placebo‐controlled study to evaluate safety and pharmacokinetics of inhaled ribavirin
A randomized, placebo‐controlled study to evaluate safety and pharmacokinetics of inhaled ribavirin Abstract Abstract Ribavirin is an inosine monophosphate dehydrogenase inhibitor. Studies suggest ribavirin aerosol could be a safe and efficacious treatment option in the fight against coronaviruses. However, current tre...
PMC12775016
core_pubmed_pmc
When blood hits the brain: altered glymphatic and dural lymphatic function after surface bleeds
When blood hits the brain: altered glymphatic and dural lymphatic function after surface bleeds Abstract Background The impact of acute subdural hematoma (aSDH) on measures of glymphatic–meningeal lymphatic function has not previously been reported. We present a descriptive observational study including a small case se...
PMC4649706
core_pubmed_pmc
Alpha-2-macroglobulin loaded microcapsules enhance human leukocyte functions and innate immune response
Alpha-2-macroglobulin loaded microcapsules enhance human leukocyte functions and innate immune response Abstract Abstract Synthetic microstructures can be engineered to deliver bioactive compounds impacting on their pharmacokinetics and pharmacodynamics. Herein, we applied dextran-based layer-by-layer (LbL) microcapsul...
PMC9272939
core_pubmed_pmc
Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro / in vivo evaluation
Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro / in vivo evaluation Abstract Abstract Asthma represents a globally serious non-communicable ailment with significant public health outcomes for both pediatrics an...
PMC10640380
core_pubmed_pmc
FooDrugs: a comprehensive food–drug interactions database with text documents and transcriptional data
FooDrugs: a comprehensive food–drug interactions database with text documents and transcriptional data Abstract Abstract Food–drug interactions (FDIs) occur when a food item alters the pharmacokinetics or pharmacodynamics of a drug. FDIs can be clinically relevant, as they can hamper or enhance the therapeutic effects ...
PMC11371380
core_pubmed_pmc
Long-term efficacy and safety of subcutaneous tocilizumab in clinical trials of polyarticular or systemic juvenile idiopathic arthritis
Long-term efficacy and safety of subcutaneous tocilizumab in clinical trials of polyarticular or systemic juvenile idiopathic arthritis Abstract Abstract Objective To investigate the safety and efficacy of subcutaneous tocilizumab (SC-TCZ) treatment in a long-term extension (LTE) of clinical trials in polyarticular or ...
PMC6594083
core_pubmed_pmc
Clinical pharmacology study of ipragliflozin in Japanese patients with type 1 diabetes mellitus: A phase 2, randomized, placebo‐controlled trial
Clinical pharmacology study of ipragliflozin in Japanese patients with type 1 diabetes mellitus: A phase 2, randomized, placebo‐controlled trial Abstract Abstract Aim To evaluate the pharmacodynamics, pharmacokinetics, and safety of the novel oral sodium‐glucose co‐transporter‐2 inhibitor, ipragliflozin, in Japanese pa...
PMC6354225
core_pubmed_pmc
Synthesis and Preclinical Characterization of the PSMA-Targeted Hybrid Tracer PSMA-I&F for Nuclear and Fluorescence Imaging of Prostate Cancer
Synthesis and Preclinical Characterization of the PSMA-Targeted Hybrid Tracer PSMA-I&F for Nuclear and Fluorescence Imaging of Prostate Cancer Abstract Abstract The prostate-specific membrane antigen (PSMA)–targeted radiotracers 68 Ga/ 177 Lu-PSMA-I&T and 99m Tc-PSMA-I&S (for i maging and s urgery) are currently succes...
PMC12259427
core_pubmed_pmc
Population pharmacokinetics of teicoplanin and dosage optimization in sepsis patients based on continuous renal replacement therapy
Population pharmacokinetics of teicoplanin and dosage optimization in sepsis patients based on continuous renal replacement therapy Abstract Abstract Purpose It is well known that pharmacokinetics (PK) of drugs is significantly altered in sepsis patients receiving continuous renal replacement therapy (CRRT). However, c...
PMC4532713
core_pubmed_pmc
Developmental changes rather than repeated administration drive paracetamol glucuronidation in neonates and infants
Developmental changes rather than repeated administration drive paracetamol glucuronidation in neonates and infants Abstract Purpose Based on recovered metabolite ratios in urine, it has been concluded that paracetamol glucuronidation may be up-regulated upon multiple dosing. This study investigates paracetamol clearan...
PMC8858832
core_pubmed_pmc
Pharmacokinetics of Esomeprazole in Critically Ill Patients
Pharmacokinetics of Esomeprazole in Critically Ill Patients Abstract Abstract Background Esomeprazole, a potent proton pump inhibitor (PPI), is widely used for the prevention of stress ulcers in intensive care unit (ICU) patients. Objective This study investigates the pharmacokinetics (PK) of esomeprazole in critically...
PMC6836086
core_pubmed_pmc
Population Pharmacokinetics of Cis -, Trans -, and Total Cefprozil in Healthy Male Koreans
Population Pharmacokinetics of Cis -, Trans -, and Total Cefprozil in Healthy Male Koreans Abstract Cefprozil, one of cephalosporin antibiotics, has been used extensively in clinics. However, pharmacokinetic (PK) information on cefprozil is still very limited. There have been no reports of population pharmacokinetics (...
PMC7414938
core_pubmed_pmc
Bioequivalence Study of Amitriptyline Hydrochloride Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions
Bioequivalence Study of Amitriptyline Hydrochloride Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions Abstract Purpose This study compares the pharmacokinetic and safety profiles between a new generic and a branded reference formulation of amitriptyline hydrochloride tablets, and assesses the bioeq...
PMC7509523
core_pubmed_pmc
Safety and efficacy of intravenous belimumab in children with systemic lupus erythematosus: results from a randomised, placebo-controlled trial
Safety and efficacy of intravenous belimumab in children with systemic lupus erythematosus: results from a randomised, placebo-controlled trial Abstract Abstract Objectives This ongoing Phase-2, randomised, placebo-controlled, double-blind study evaluated the efficacy, safety and pharmacokinetics of intravenous belimum...
PMC5414891
core_pubmed_pmc
Impact of Physiologically Based Pharmacokinetic Models on Regulatory Reviews and Product Labels: Frequent Utilization in the Field of Oncology
Impact of Physiologically Based Pharmacokinetic Models on Regulatory Reviews and Product Labels: Frequent Utilization in the Field of Oncology Abstract Physiologically based pharmacokinetic (PBPK) modeling can be used to predict drug pharmacokinetics in virtual populations using models that integrate understanding of p...
PMC4129930
core_pubmed_pmc
Modified Titanium Implant as a Gateway to the Human Body: The Implant Mediated Drug Delivery System
Modified Titanium Implant as a Gateway to the Human Body: The Implant Mediated Drug Delivery System Abstract The aim of this study was to investigate the efficacy of a proposed new implant mediated drug delivery system (IMDDS) in rabbits. The drug delivery system is applied through a modified titanium implant that is c...
PMC6155683
core_pubmed_pmc
Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas
Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas Abstract Abstract Zuojin formula (ZJ) is a traditional Chinese medicine (TCM) prescription consisted of Coptidis Rhizoma (CR) and Euodiae Fructus (EF), and has been used to treat gastrointestinal (GI) dise...
PMC12958104
core_pubmed_pmc
Artificial lipidation of proteins and peptides: from mechanism to clinical applications
Artificial lipidation of proteins and peptides: from mechanism to clinical applications Abstract Abstract The landscape of modern medicine has been transformed by protein‐based therapeutics, offering targeted treatments for complex disorders with remarkable specificity and efficacy. However, these biologics face signif...
PMC5899833
core_pubmed_pmc
Population pharmacokinetics/pharmacodynamics of micafungin against Candida species in obese, critically ill, and morbidly obese critically ill patients
Population pharmacokinetics/pharmacodynamics of micafungin against Candida species in obese, critically ill, and morbidly obese critically ill patients Abstract Abstract Background Dosing in obese critically ill patients is challenging due to pathophysiological changes derived from obesity and/or critical illness, and ...
PMC12561008
core_pubmed_pmc
Pharmacokinetics of Sofosbuvir and Velpatasvir for Hepatitis C Treatment in Pregnancy
Pharmacokinetics of Sofosbuvir and Velpatasvir for Hepatitis C Treatment in Pregnancy Abstract Abstract Background : Pregnancy is a time when women are uniquely engaged with the healthcare system and are often motivated to participate in activities directed toward improvement of their own health and ensuring the health...
PMC11739129
core_pubmed_pmc
Impact of Methotrexate and 7‐Hydroxymethotrexate Exposure on Renal Toxicity in Pediatric Non‐Hodgkin Lymphoma
Impact of Methotrexate and 7‐Hydroxymethotrexate Exposure on Renal Toxicity in Pediatric Non‐Hodgkin Lymphoma Abstract ABSTRACT Background 7‐Hydroxymethotrexate (7‐OHMTX) is the main metabolite in plasma following high‐dose MTX (HD‐MTX), which may result in activity and toxicity of the MTX. Moreover, 7‐OHMTX could prod...
PMC8706398
core_pubmed_pmc
Therapeutic Potential of Injectable Nano-Mupirocin Liposomes for Infections Involving Multidrug-Resistant Bacteria
Therapeutic Potential of Injectable Nano-Mupirocin Liposomes for Infections Involving Multidrug-Resistant Bacteria Abstract Abstract Antibiotic resistance is a global health threat. There are a few antibiotics under development, and even fewer with new modes of action and no cross-resistance to established antibiotics....
PMC11568265
core_pubmed_pmc
Exploring peptide dendrimers for intestinal lymphatic targeting: formulation and evaluation of peptide dendrimer conjugated liposomes for enhancing the oral bioavailability of Asenapine maleate
Exploring peptide dendrimers for intestinal lymphatic targeting: formulation and evaluation of peptide dendrimer conjugated liposomes for enhancing the oral bioavailability of Asenapine maleate Abstract Asenapine maleate (ASPM) is a second-generation atypical antipsychotic that is approved for treating acute schizophre...
PMC7708882
core_pubmed_pmc
COVID-19 infection in a kidney transplant recipient—special emphasis on pharmacokinetic interactions: A case report
COVID-19 infection in a kidney transplant recipient—special emphasis on pharmacokinetic interactions: A case report Abstract Abstract BACKGROUND Solid organ transplant recipients are considered to be at high-risk of developing coronavirus disease 2019 (COVID-19)-related complications. The optimal treatment for this pat...
PMC11354333
core_pubmed_pmc
Three Years On: The Role of Pegcetacoplan in Paroxysmal Nocturnal Hemoglobinuria (PNH) since Its Initial Approval
Three Years On: The Role of Pegcetacoplan in Paroxysmal Nocturnal Hemoglobinuria (PNH) since Its Initial Approval Abstract Abstract Paroxysmal nocturnal hemoglobinuria (PNH) is a rare disease characterized by complement-mediated hemolysis and potentially life-threatening complications. Pegcetacoplan, an inhibitor of co...
PMC12389255
core_pubmed_pmc
Population Pharmacokinetics of Tideglusib in Congenital and Childhood Myotonic Dystrophy Type 1: Influence of Demographic and Clinical Factors on Systemic Exposure
Population Pharmacokinetics of Tideglusib in Congenital and Childhood Myotonic Dystrophy Type 1: Influence of Demographic and Clinical Factors on Systemic Exposure Abstract Background : GSK3β is an intracellular regulatory kinase that is dysregulated in multiple tissues in Type 1 myotonic dystrophy (DM-1). Tideglusib i...
PMC7560740
core_pubmed_pmc
Design and in vivo evaluation of a microparticulate depot formulation of buprenorphine for veterinary use
Design and in vivo evaluation of a microparticulate depot formulation of buprenorphine for veterinary use Abstract Buprenorphine is a frequently used analgetic agent in veterinary medicine. A major drawback, however, is the short duration of action requiring several daily administrations. We therefore designed a poly-l...
PMC7242285
core_pubmed_pmc
JNJ-4178 (adafosbuvir, odalasvir, and simeprevir) in Japanese patients with chronic hepatitis C virus genotype 1 or 2 infection with or without compensated cirrhosis: the Phase IIa OMEGA-3 study
JNJ-4178 (adafosbuvir, odalasvir, and simeprevir) in Japanese patients with chronic hepatitis C virus genotype 1 or 2 infection with or without compensated cirrhosis: the Phase IIa OMEGA-3 study Abstract Background The efficacy, safety, and pharmacokinetics of the combination of three direct-acting antiviral (DAA) agen...
PMC9343941
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamics of Isoniazid and its Metabolite Acetylisoniazid in Chinese Population
Population Pharmacokinetics and Pharmacodynamics of Isoniazid and its Metabolite Acetylisoniazid in Chinese Population Abstract Objective: We aimed to establish a population pharmacokinetic (PPK) model for isoniazid (INH) and its major metabolite Acetylisoniazid (AcINH) in healthy Chinese participants and tuberculosis ...
PMC12280725
core_pubmed_pmc
Clinical pharmacokinetics of potassium competitive acid blockers: a systematic review and meta-analysis
Clinical pharmacokinetics of potassium competitive acid blockers: a systematic review and meta-analysis Abstract Background Potassium competitive acid blockers (P-CABs) are a new class of acid suppressants that provide rapid and sustained inhibition of gastric acid secretion. Understanding the pharmacokinetic (PK) char...
PMC9379304
core_pubmed_pmc
Population pharmacokinetic models of anti-PD-1 mAbs in patients with multiple tumor types: A systematic review
Population pharmacokinetic models of anti-PD-1 mAbs in patients with multiple tumor types: A systematic review Abstract Aims and background A number of population pharmacokinetic (PPK) models of anti-programmed cell death-1 (PD-1) monoclonal antibodies (mAbs) in multiple tumor types have been published to characterize ...
PMC11222276
core_pubmed_pmc
Together or Apart? Revealing the Impact of Dietary Interventions on Bioavailability of Quinolones: A Systematic Review with Meta-analyses
Together or Apart? Revealing the Impact of Dietary Interventions on Bioavailability of Quinolones: A Systematic Review with Meta-analyses Abstract Abstract Background and Objective Managing drug-food interactions is essential for optimizing the effectiveness and safety profile of quinolones. Following PRISMA guidelines...
PMC4346873
core_pubmed_pmc
Systems Pharmacology Dissection of the Anti-Inflammatory Mechanism for the Medicinal Herb Folium Eriobotryae
Systems Pharmacology Dissection of the Anti-Inflammatory Mechanism for the Medicinal Herb Folium Eriobotryae Abstract Abstract Inflammation is a hallmark of many diseases like diabetes, cancers, atherosclerosis and arthritis. Thus, lots of concerns have been raised toward developing novel anti-inflammatory agents. Many...
PMC9051964
core_pubmed_pmc
Study of influence of Catha edulis (Khat) chewing on oral pharmacokinetics of irbesartan in rats using a newly developed HPLC-UV method
Study of influence of Catha edulis (Khat) chewing on oral pharmacokinetics of irbesartan in rats using a newly developed HPLC-UV method Abstract Khat consumers might use a number of drugs for underlying conditions; however the potential drug-herb interaction between khat and other drugs including Irbesartan (IRB) is un...
PMC11580331
core_pubmed_pmc
Advancing understanding of human variability through toxicokinetic modeling, in vitro-in vivo extrapolation, and new approach methodologies
Advancing understanding of human variability through toxicokinetic modeling, in vitro-in vivo extrapolation, and new approach methodologies Abstract The merging of physiology and toxicokinetics, or pharmacokinetics, with computational modeling to characterize dosimetry has led to major advances for both the chemical an...
PMC6347888
core_pubmed_pmc
Levetiracetam optimal dose-finding as first-line treatment for neonatal seizures occurring in the context of hypoxic-ischaemic encephalopathy (LEVNEONAT-1): study protocol of a phase II trial
Levetiracetam optimal dose-finding as first-line treatment for neonatal seizures occurring in the context of hypoxic-ischaemic encephalopathy (LEVNEONAT-1): study protocol of a phase II trial Abstract Introduction Therapeutic schedules for treating neonatal seizures remain elusive. First-line treatment with phenobarbit...
PMC11530481
core_pubmed_pmc
Computational Modelling of the Impact of Evaporation on In-Vitro Dermal Absorption
Computational Modelling of the Impact of Evaporation on In-Vitro Dermal Absorption Abstract Abstract Purpose Volatiles are common in personal care products and dermatological drugs. Determining the impact of evaporation of volatiles on skin permeation is crucial to evaluate and understand their delivery, bioavailabilit...
PMC6956244
core_pubmed_pmc
Noninvasive Assessment of Exosome Pharmacokinetics In Vivo: A Review
Noninvasive Assessment of Exosome Pharmacokinetics In Vivo: A Review Abstract Abstract Exosomes, intraluminal vesicles that contain informative DNA, RNA, proteins, and lipid membranes derived from the original donor cells, have recently been introduced to therapy and diagnosis. With their emergence as an alternative to...