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PMC9334565 | core_pubmed_pmc | Case report: Non-response to fluoxetine in a homozygous 5-HTTLPR S-allele carrier of the serotonin transporter gene | Case report: Non-response to fluoxetine in a homozygous 5-HTTLPR S-allele carrier of the serotonin transporter gene Abstract We report the case of a 50-year-old male with major depressive disorder (MDD) to illustrate the challenge of finding effective antidepressant pharmacotherapy and the role that the patient’s genet... |
PMC6525989 | core_pubmed_pmc | A self-assembled, modular nucleic acid-based nanoscaffold for multivalent theranostic medicine | A self-assembled, modular nucleic acid-based nanoscaffold for multivalent theranostic medicine Abstract Abstract Rationale : Within the field of personalized medicine there is an increasing focus on designing flexible, multifunctional drug delivery systems that combine high efficacy with minimal side effects, by tailor... |
PMC6305107 | core_pubmed_pmc | Neoadjuvant administration of hydroxychloroquine in a phase 1 clinical trial induced plasma Par-4 levels and apoptosis in diverse tumors | Neoadjuvant administration of hydroxychloroquine in a phase 1 clinical trial induced plasma Par-4 levels and apoptosis in diverse tumors Abstract Abstract Chloroquine and hydroxychloroquine (HCQ) are robust inducers of the tumor suppressor Par-4 secretion from normal cells. Secreted Par-4 causes paracrine apoptosis of ... |
PMC10728861 | core_pubmed_pmc | Amphotericin B Pharmacokinetics: Inter-strain Differences in Rats Following Intravenous Administration of the Most Commonly Marketed Formulations of the Drug | Amphotericin B Pharmacokinetics: Inter-strain Differences in Rats Following Intravenous Administration of the Most Commonly Marketed Formulations of the Drug Abstract Background Amphotericin B (AmB) is the first-line drug to treat invasive fungal infections. However, its delivery to the body and clinical use faces many... |
PMC3873925 | core_pubmed_pmc | Peptide-Mediated Liposomal Doxorubicin Enhances Drug Delivery Efficiency and Therapeutic Efficacy in Animal Models | Peptide-Mediated Liposomal Doxorubicin Enhances Drug Delivery Efficiency and Therapeutic Efficacy in Animal Models Abstract Lung cancer ranks among the most common malignancies, and is the leading cause of cancer-related mortality worldwide. Chemotherapy for lung cancer can be made more specific to tumor cells, and les... |
PMC6273324 | core_pubmed_pmc | UHPLC-MS/MS Determination, Pharmacokinetic, and Bioavailability Study of Taxifolin in Rat Plasma after Oral Administration of its Nanodispersion | UHPLC-MS/MS Determination, Pharmacokinetic, and Bioavailability Study of Taxifolin in Rat Plasma after Oral Administration of its Nanodispersion Abstract Abstract A rapid and sensitive LC-MS/MS method based on the Triple Quad system has been developed and validated for the determination and pharmacokinetics of taxifoli... |
PMC9687670 | core_pubmed_pmc | Enhanced Efficacy of Radiopharmaceuticals When Using Technetium-99m-Labeled Liposomal Agents: Synthesis and Pharmacokinetic Properties | Enhanced Efficacy of Radiopharmaceuticals When Using Technetium-99m-Labeled Liposomal Agents: Synthesis and Pharmacokinetic Properties Abstract Abstract Challenges posed by the retention of radiopharmaceuticals in unintended organs affect the quality of patient procedures when undergoing diagnostics and therapeutics. T... |
PMC8058073 | core_pubmed_pmc | Effect of TAAR1/5-HT 1A agonist SEP-363856 on REM sleep in humans | Effect of TAAR1/5-HT 1A agonist SEP-363856 on REM sleep in humans Abstract Abstract SEP-363856 is a trace amine-associated receptor 1 (TAAR1) and 5-hydroxytryptamine type 1A (5-HT 1A ) agonist, currently in Phase 3 clinical trials for the treatment of schizophrenia. Although SEP-363856 activates TAAR1 and 5-HT 1A recep... |
PMC8005090 | core_pubmed_pmc | Bioanalytical Method Development and Validation Study of Neuroprotective Extract of Kashmiri Saffron Using Ultra-Fast Liquid Chromatography-Tandem Mass Spectrometry (UFLC-MS/MS): In Vivo Pharmacokinetics of Apocarotenoids and Carotenoids | Bioanalytical Method Development and Validation Study of Neuroprotective Extract of Kashmiri Saffron Using Ultra-Fast Liquid Chromatography-Tandem Mass Spectrometry (UFLC-MS/MS): In Vivo Pharmacokinetics of Apocarotenoids and Carotenoids Abstract Abstract Kashmir saffron ( Crocus sativus L.), also known as Indian saffr... |
PMC11946379 | core_pubmed_pmc | Prodrug Approach as a Strategy to Enhance Drug Permeability | Prodrug Approach as a Strategy to Enhance Drug Permeability Abstract Abstract Absorption and permeability are critical physicochemical parameters that must be balanced to achieve optimal drug uptake. These key factors are closely linked to the maximum absorbable dose required to provide appropriate plasma levels of dru... |
PMC4797375 | core_pubmed_pmc | Pharmacokinetic modeling of [ 18 F]fluorodeoxyglucose (FDG) for premature infants, and newborns through 5-year-olds | Pharmacokinetic modeling of [ 18 F]fluorodeoxyglucose (FDG) for premature infants, and newborns through 5-year-olds Abstract Background Absorbed dose estimates for pediatric patients require pharmacokinetics that are, to the extent possible, age-specific. Such age-specific pharmacokinetic data are lacking for many of t... |
PMC6873202 | core_pubmed_pmc | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens Abstract Abstract WT P53-Induced Phosphatase 1 (WIP1) is a member of the magnesium-dependent serine/threonine protein phosphatase (PPM) family and is induced by P53 in response to DNA... |
PMC12393523 | core_pubmed_pmc | Physiologically-based pharmacokinetic model for CAR-T cells delivery and efficacy in solid tumors | Physiologically-based pharmacokinetic model for CAR-T cells delivery and efficacy in solid tumors Abstract Abstract Abnormal blood vessels limit the delivery and function of endogenous T cells as well as adoptively transferred Chimeric Antigen Receptor (CAR)-T cells in the tumor microenvironment (TME). We recently show... |
PMC3724274 | core_pubmed_pmc | A review of the gastrointestinal therapeutic system (GITS) formulation and its effectiveness in the delivery of antihypertensive drug treatment (focus on nifedipine GITS) | A review of the gastrointestinal therapeutic system (GITS) formulation and its effectiveness in the delivery of antihypertensive drug treatment (focus on nifedipine GITS) Abstract Hypertension treatment guidelines do not discriminate within drug classes and, furthermore, do not consider whether or not all of the formul... |
PMC7389632 | core_pubmed_pmc | Prediction of lisinopril pediatric dose from the reference adult dose by employing a physiologically based pharmacokinetic model | Prediction of lisinopril pediatric dose from the reference adult dose by employing a physiologically based pharmacokinetic model Abstract Background This study aimed to assess the pediatric lisinopril doses using an adult physiological based pharmacokinetic (PBPK) model. As the empirical rules of dose calculation canno... |
PMC10014067 | core_pubmed_pmc | Proof‐of‐concept for incorporating mechanistic insights from multi‐omics analyses of polymyxin B in combination with chloramphenicol against Klebsiella pneumoniae | Proof‐of‐concept for incorporating mechanistic insights from multi‐omics analyses of polymyxin B in combination with chloramphenicol against Klebsiella pneumoniae Abstract Abstract Carbapenemase‐resistant Klebsiella pneumoniae (KP) resistant to multiple antibiotic classes necessitates optimized combination therapy. Our... |
PMC4995486 | core_pubmed_pmc | Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial | Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial Abstract Abstract Ticagrelor has a greater antiplatelet efficacy than clopidogrel but may be accompanied by an increased risk of bleeding. This study evaluated t... |
PMC12789730 | core_pubmed_pmc | Targeting Dlat-Trpv3 pathway by hyperforin elicits non-canonical promotion of adipose thermogenesis as an effective anti-obesity strategy | Targeting Dlat-Trpv3 pathway by hyperforin elicits non-canonical promotion of adipose thermogenesis as an effective anti-obesity strategy Abstract Highlights • HPF exhibits anti-obesity properties and favorable oral bioavailability. • HPF stimulates adipose thermogenesis without adverse cardiac effects. • Dlat +/- comp... |
PMC11533104 | core_pubmed_pmc | Hepatic OATP1B zonal distribution: Implications for rifampicin‐mediated drug–drug interactions explored within a PBPK framework | Hepatic OATP1B zonal distribution: Implications for rifampicin‐mediated drug–drug interactions explored within a PBPK framework Abstract Abstract OATP1B facilitates the uptake of xenobiotics into hepatocytes and is a prominent target for drug–drug interactions (DDIs). Reduced systemic exposure of OATP1B substrates has ... |
PMC8592516 | core_pubmed_pmc | LaTeX tutorial for the standardization and automation of population analysis reports | LaTeX tutorial for the standardization and automation of population analysis reports Abstract Abstract Writing population analysis reports that fulfilling the specifications of submission readiness is a time‐consuming process and prone to human error. Thus, there is a need to streamline the creation of these reports th... |
PMC12402809 | core_pubmed_pmc | Donanemab immunogenicity in participants with early symptomatic Alzheimer's disease | Donanemab immunogenicity in participants with early symptomatic Alzheimer's disease Abstract Abstract INTRODUCTION Donanemab is an immunoglobulin G1 antibody that targets an N‐terminal truncated form of amyloid beta present in mature plaques. Treatment‐emergent (TE) anti‐drug antibodies (ADAs) were quantified in donane... |
PMC6932964 | core_pubmed_pmc | Sialic Acid-Engineered IL4–10 Fusion Protein is Bioactive and Rapidly Cleared from the Circulation | Sialic Acid-Engineered IL4–10 Fusion Protein is Bioactive and Rapidly Cleared from the Circulation Abstract Purpose Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4–10 fusion protein (IL4–10 FP) on in... |
PMC6183514 | core_pubmed_pmc | Phylogenetic analysis of the cytochrome P450 (CYP450) nucleotide sequences of the horse and predicted CYP450s of the white rhinoceros ( Ceratotherium simum ) and other mammalian species | Phylogenetic analysis of the cytochrome P450 (CYP450) nucleotide sequences of the horse and predicted CYP450s of the white rhinoceros ( Ceratotherium simum ) and other mammalian species Abstract Background The plight of the white rhinoceros ( Ceratotherium simum ) and the increasing need of treatment options for injure... |
PMC7587605 | core_pubmed_pmc | Antibody–Drug Conjugates for Cancer Therapy | Antibody–Drug Conjugates for Cancer Therapy Abstract Antibody–drug conjugates (ADCs) are novel drugs that exploit the specificity of a monoclonal antibody (mAb) to reach target antigens expressed on cancer cells for the delivery of a potent cytotoxic payload. ADCs provide a unique opportunity to deliver drugs to tumor ... |
PMC10155901 | core_pubmed_pmc | Sutimlimab for the Treatment of Cold Agglutinin Disease | Sutimlimab for the Treatment of Cold Agglutinin Disease Abstract Abstract Cold agglutinin disease (CAD) is a rare autoimmune hemolytic anemia and a bone marrow clonal lymphoproliferative disorder. Hemolysis in CAD is complement-dependent and mediated by the classical activation pathway. Patients also frequently suffer ... |
PMC6425379 | core_pubmed_pmc | Pharmacokinetic Study and Tissue Distribution of Lorlatinib in Mouse Serum and Tissue Samples by Liquid Chromatography-Mass Spectrometry | Pharmacokinetic Study and Tissue Distribution of Lorlatinib in Mouse Serum and Tissue Samples by Liquid Chromatography-Mass Spectrometry Abstract In the present study, we developed and validated a rapid and simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of lorlatinib in mo... |
PMC7179259 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Antimalarial Activity of the Novel Plasmodium Phosphatidylinositol 4-Kinase Inhibitor MMV390048 in Healthy Volunteers | Safety, Tolerability, Pharmacokinetics, and Antimalarial Activity of the Novel Plasmodium Phosphatidylinositol 4-Kinase Inhibitor MMV390048 in Healthy Volunteers Abstract MMV390048 is a novel antimalarial compound that inhibits Plasmodium phosphatidylinositol-4-kinase. The safety, tolerability, pharmacokinetic profile,... |
PMC6023695 | core_pubmed_pmc | Useful pharmacodynamic endpoints in children: selection, measurement, and next steps | Useful pharmacodynamic endpoints in children: selection, measurement, and next steps Abstract Abstract Pharmacodynamic (PD) endpoints are essential for establishing the benefit-to-risk ratio for therapeutic interventions in children and neonates. This article discusses the selection of an appropriate measure of respons... |
PMC11210303 | core_pubmed_pmc | Simulated Target Attainment of Multidose Regimens of Dalbavancin for Prolonged Durations of Therapy | Simulated Target Attainment of Multidose Regimens of Dalbavancin for Prolonged Durations of Therapy Abstract Abstract Background Dalbavancin is a long-acting lipoglycopeptide antibiotic that is increasingly utilized for infections that require prolonged treatment durations despite the lack of Food and Drug Administrati... |
PMC10681408 | core_pubmed_pmc | The impact of CYP3A4 and CYP3A5 genetic variations on tacrolimus treatment of living‐donor Egyptian kidney transplanted patients | The impact of CYP3A4 and CYP3A5 genetic variations on tacrolimus treatment of living‐donor Egyptian kidney transplanted patients Abstract Abstract Background Tacrolimus (TAC) is the mainstay of immunosuppressive regimen for kidney transplantations. Its clinical use is complex due to high inter‐individual variations whi... |
PMC5461687 | core_pubmed_pmc | Lipodox® (generic doxorubicin hydrochloride liposome injection): in vivo efficacy and bioequivalence versus Caelyx® (doxorubicin hydrochloride liposome injection) in human mammary carcinoma (MX-1) xenograft and syngeneic fibrosarcoma (WEHI 164) mouse models | Lipodox® (generic doxorubicin hydrochloride liposome injection): in vivo efficacy and bioequivalence versus Caelyx® (doxorubicin hydrochloride liposome injection) in human mammary carcinoma (MX-1) xenograft and syngeneic fibrosarcoma (WEHI 164) mouse models Abstract Abstract Background Doxorubicin (DXR) hydrochloride (... |
PMC7495267 | core_pubmed_pmc | Prescribing medicines to older people—How to consider the impact of ageing on human organ and body functions | Prescribing medicines to older people—How to consider the impact of ageing on human organ and body functions Abstract Abstract Ageing is associated with several changes in human organs, which result in altered medication pharmacokinetics and pharmacodynamics. Ageing is also associated with changes in human body functio... |
PMC9931704 | core_pubmed_pmc | Application of a physiologically based pharmacokinetic model in predicting captopril disposition in children with chronic kidney disease | Application of a physiologically based pharmacokinetic model in predicting captopril disposition in children with chronic kidney disease Abstract Over the last several decades, angiotensin-converting enzyme inhibitors (ACEIs) have been a staple in the treatment of hypertension and renovascular disorders in children. On... |
PMC4857012 | core_pubmed_pmc | Pharmacokinetics, bioavailability, metabolism and excretion of δ -viniferin in rats | Pharmacokinetics, bioavailability, metabolism and excretion of δ -viniferin in rats Abstract A highly rapid and sensitive liquid chromatographic–electrospray ionization tandem mass spectrometric (LC–ESI-MS/MS) method was developed and validated for the determination of trans - δ -viniferin (Rs-1) in rat plasma, urine a... |
PMC12379277 | core_pubmed_pmc | Multi-omics analysis reveals RNA polymerase II degradation as a novel mechanism of PF-3758309’s anti-tumor activity | Multi-omics analysis reveals RNA polymerase II degradation as a novel mechanism of PF-3758309’s anti-tumor activity Abstract PF-3758309, a pyrrolopyrimidine-based inhibitor of p21-activated kinase 4 (PAK4), has demonstrated preclinical anti-tumor activity. However, due to poor pharmacokinetics and off-target effects, i... |
PMC10522605 | core_pubmed_pmc | Formulation development, in vivo bioequivalence and pediatric PBPK modeling studies of taste-masked ciprofloxacin chewable tablets | Formulation development, in vivo bioequivalence and pediatric PBPK modeling studies of taste-masked ciprofloxacin chewable tablets Abstract A taste-masked chewable tablet of ciprofloxacin using ion exchange resin Kyron T-134 for enhancing compliance for the paediatric population was developed. The drug-to-resin ratio w... |
PMC11314561 | core_pubmed_pmc | Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3- b ]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling | Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3- b ]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling Abstract The inhibitory-kappaB kinases (IKKs) IKKα and IKKβ play central roles in regulating the non-canonical and canonical NF-κB signalling pathways. Whilst the prot... |
PMC12856755 | core_pubmed_pmc | Artificial intelligence and precision medicine: a pilot study predicting optimal ceftaroline dosage for pediatric patients | Artificial intelligence and precision medicine: a pilot study predicting optimal ceftaroline dosage for pediatric patients Abstract Abstract Background Accurate drug dosing in pediatrics is complicated by age-related physiological variability. Standard weight-based dosing may result in either subtherapeutic exposure or... |
PMC12370926 | core_pubmed_pmc | Discovery of novel SND1 inhibitors by in silico–based molecular docking and dynamics simulation methods for managing hepatocellular carcinoma | Discovery of novel SND1 inhibitors by in silico–based molecular docking and dynamics simulation methods for managing hepatocellular carcinoma Abstract Abstract Hepatocellular carcinoma (HCC) is one of the life–threatening cancers in the current decade. Earlier reports suggest that protein arginine methyl transferase 5 ... |
PMC9640990 | core_pubmed_pmc | Pharmacokinetic herb-drug interactions: Altered systemic exposure and tissue distribution of ciprofloxacin, a substrate of multiple transporters, after combined treatment with Polygonum capitatum Buch.-Ham. ex D. Don extracts | Pharmacokinetic herb-drug interactions: Altered systemic exposure and tissue distribution of ciprofloxacin, a substrate of multiple transporters, after combined treatment with Polygonum capitatum Buch.-Ham. ex D. Don extracts Abstract Abstract Background: Combination of Polygonum capitatum Buch.-Ham. ex D. Don extract ... |
PMC9235206 | core_pubmed_pmc | Pharmacokinetics of magnetic iron oxide nanoparticles for medical applications | Pharmacokinetics of magnetic iron oxide nanoparticles for medical applications Abstract Abstract Magnetic iron oxide nanoparticles (MNPs) have been under intense investigation for at least the last five decades as they show enormous potential for many biomedical applications, such as biomolecule separation, MRI imaging... |
PMC11213957 | core_pubmed_pmc | A unifying model to explain frequent SARS-CoV-2 rebound after nirmatrelvir treatment and limited prophylactic efficacy | A unifying model to explain frequent SARS-CoV-2 rebound after nirmatrelvir treatment and limited prophylactic efficacy Abstract Abstract In a pivotal trial (EPIC-HR), a 5-day course of oral ritonavir-boosted nirmatrelvir, given early during symptomatic SARS-CoV-2 infection (within three days of symptoms onset), decreas... |
PMC4902307 | core_pubmed_pmc | Defining the Active Fraction of Daptomycin against Methicillin-Resistant Staphylococcus aureus (MRSA) Using a Pharmacokinetic and Pharmacodynamic Approach | Defining the Active Fraction of Daptomycin against Methicillin-Resistant Staphylococcus aureus (MRSA) Using a Pharmacokinetic and Pharmacodynamic Approach Abstract Our objective was to study the pharmacodynamics of daptomycin in the presence of varying concentrations of human serum (HS) in vitro to quantify the fractio... |
PMC6325219 | core_pubmed_pmc | Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus | Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus Abstract NVR 3-778 is the first capsid assembly modulator (CAM) that has demonstrated antiviral activity in hepatitis B virus (HBV)-infected patients. NVR 3-778 inhibited the generation of infectious HBV DNA-... |
PMC9588906 | core_pubmed_pmc | A phase I/II study of arfolitixorin and 5-fluorouracil in combination with oxaliplatin (plus or minus bevacizumab) or irinotecan in metastatic colorectal cancer | A phase I/II study of arfolitixorin and 5-fluorouracil in combination with oxaliplatin (plus or minus bevacizumab) or irinotecan in metastatic colorectal cancer Abstract Abstract Background 5-fluorouracil (5-FU) combined with a folate remains an essential treatment component for metastatic colorectal cancer (mCRC). Leu... |
PMC9445216 | core_pubmed_pmc | A randomized, double-blind, parallel control study to evaluate the biosimilarity of QL1209 with Perjeta ® in healthy male subjects | A randomized, double-blind, parallel control study to evaluate the biosimilarity of QL1209 with Perjeta ® in healthy male subjects Abstract Abstract Purpose: This is the first study to compare the pharmacokinetics, safety and, immunogenicity of QL1209, a biosimilar of Perjeta ® . Methods: This study was a randomized, d... |
PMC6587432 | core_pubmed_pmc | M281, an Anti‐FcRn Antibody: Pharmacodynamics, Pharmacokinetics, and Safety Across the Full Range of IgG Reduction in a First‐in‐Human Study | M281, an Anti‐FcRn Antibody: Pharmacodynamics, Pharmacokinetics, and Safety Across the Full Range of IgG Reduction in a First‐in‐Human Study Abstract Abstract M281 is a fully human, anti‐neonatal Fc receptor (FcRn) antibody that inhibits FcRn‐mediated immunoglobulin G (IgG) recycling to decrease pathogenic IgG while pr... |
PMC11589087 | core_pubmed_pmc | Evaluation of Drug-Related Problems of Intensive Care Unit Patients by Clinical Pharmacists: A Retrospective Study | Evaluation of Drug-Related Problems of Intensive Care Unit Patients by Clinical Pharmacists: A Retrospective Study Abstract Abstract Objectives The study aimed to identify drug-related problems (DRPs) and risk factors associated with the emergence of DRPs in intensive care unit (ICU) patients. Materials and Methods Thi... |
PMC12189772 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Antibiotics in Children: Perspectives on Model-Informed Precision Dosing | Physiologically Based Pharmacokinetic Modeling of Antibiotics in Children: Perspectives on Model-Informed Precision Dosing Abstract Abstract The appropriate use of antibiotics is crucial and involves selecting an optimal dosing regimen based on pharmacokinetic (PK) and pharmacodynamic (PD) indicators. Physiologically b... |
PMC12512771 | core_pubmed_pmc | Molecular screening of natural compounds targeting KRAS(G12C): a multi-parametric strategy against acute lymphoblastic leukemia | Molecular screening of natural compounds targeting KRAS(G12C): a multi-parametric strategy against acute lymphoblastic leukemia Abstract Abstract Acute lymphoblastic leukaemia (ALL) is a highly aggressive hematological malignancy that necessitates safer, more effective therapies. This study applied a multi-parametric c... |
PMC10191551 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of Oral Ferric Maltol in Children With Iron Deficiency: Phase 1 Study | Safety, Tolerability, and Pharmacokinetics of Oral Ferric Maltol in Children With Iron Deficiency: Phase 1 Study Abstract Supplemental Digital Content is available in the text. Objectives: Iron deficiency is common in children and can have negative effects on behavior and function. Standard oral ferrous iron replacemen... |
PMC10847913 | core_pubmed_pmc | A 13.2 mg epinephrine intranasal spray demonstrates comparable pharmacokinetics, pharmacodynamics, and safety to a 0.3 mg epinephrine autoinjector | A 13.2 mg epinephrine intranasal spray demonstrates comparable pharmacokinetics, pharmacodynamics, and safety to a 0.3 mg epinephrine autoinjector Abstract Abstract Background Recent acute anaphylaxis guideline updates have identified remaining unmet needs based on currently available therapeutic options as a critical ... |
PMC10051286 | core_pubmed_pmc | Model-Informed Target Morning 17α-Hydroxyprogesterone Concentrations in Dried Blood Spots for Pediatric Congenital Adrenal Hyperplasia Patients | Model-Informed Target Morning 17α-Hydroxyprogesterone Concentrations in Dried Blood Spots for Pediatric Congenital Adrenal Hyperplasia Patients Abstract Abstract Monitoring cortisol replacement therapy in congenital adrenal hyperplasia (CAH) patients is vital to avoid serious adverse events such as adrenal crises due t... |
PMC7396179 | core_pubmed_pmc | Nonclinical Pharmacokinetic and Pharmacodynamic Assessment of Bimatoprost Following a Single Intracameral Injection of Sustained-Release Implants | Nonclinical Pharmacokinetic and Pharmacodynamic Assessment of Bimatoprost Following a Single Intracameral Injection of Sustained-Release Implants Abstract Purpose To assess the pharmacokinetic (PK)/pharmacodynamic (PD) relationship following intracameral Bimatoprost sustained-release (SR) implants (8, 15, 30, and 60 µg... |
PMC5346872 | core_pubmed_pmc | GP2015, a proposed etanercept biosimilar: Pharmacokinetic similarity to its reference product and comparison of its autoinjector device with prefilled syringes | GP2015, a proposed etanercept biosimilar: Pharmacokinetic similarity to its reference product and comparison of its autoinjector device with prefilled syringes Abstract Abstract Aims To assess pharmacokinetics (PK) and safety of GP2015, a proposed etanercept biosimilar, in two studies: comparison with etanercept origin... |
PMC5629940 | core_pubmed_pmc | Efficacy and safety of the biosimilar ABP 501 compared with adalimumab in patients with moderate to severe rheumatoid arthritis: a randomised, double-blind, phase III equivalence study | Efficacy and safety of the biosimilar ABP 501 compared with adalimumab in patients with moderate to severe rheumatoid arthritis: a randomised, double-blind, phase III equivalence study Abstract Abstract Objectives ABP 501 is a Food and Drug Administration-approved biosimilar to adalimumab; structural, functional and ph... |
PMC8452301 | core_pubmed_pmc | Prediction of the drug–drug interaction potential of the α1‐acid glycoprotein bound, CYP3A4/CYP2C9 metabolized oncology drug, erdafitinib | Prediction of the drug–drug interaction potential of the α1‐acid glycoprotein bound, CYP3A4/CYP2C9 metabolized oncology drug, erdafitinib Abstract Abstract Erdafitinib is a potent oral pan‐fibroblast growth factor receptor inhibitor being developed as oncology drug for patients with alterations in the fibroblast growth... |
PMC9033597 | core_pubmed_pmc | The phytochemistry, pharmacology and traditional medicinal use of Glechomae Herba – a systematic review † | The phytochemistry, pharmacology and traditional medicinal use of Glechomae Herba – a systematic review † Abstract Abstract Glechomae Herba is a Chinese herb, which has been used in China for thousands of years, mainly for the treatment of nephrolithiasis. This paper summarizes the modern research progress on Glechomae... |
PMC11488827 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Natalizumab 6-Week Dosing vs Continued 4-Week Dosing for Relapsing-Remitting Multiple Sclerosis | Pharmacokinetics and Pharmacodynamics of Natalizumab 6-Week Dosing vs Continued 4-Week Dosing for Relapsing-Remitting Multiple Sclerosis Abstract Background and Objectives Exposure to natalizumab, an efficacious treatment for relapsing-remitting multiple sclerosis (RRMS), is associated with increased risk of progressiv... |
PMC8359437 | core_pubmed_pmc | Population Pharmacokinetic Model for Ertugliflozin in Healthy Subjects and Patients With Type 2 Diabetes Mellitus | Population Pharmacokinetic Model for Ertugliflozin in Healthy Subjects and Patients With Type 2 Diabetes Mellitus Abstract Abstract Ertugliflozin is a selective sodium‐glucose cotransporter 2 inhibitor approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM)... |
PMC5681604 | core_pubmed_pmc | Body mass index and clinical response to intravenous or subcutaneous abatacept in patients with rheumatoid arthritis | Body mass index and clinical response to intravenous or subcutaneous abatacept in patients with rheumatoid arthritis Abstract Abstract This post hoc analysis of ACQUIRE ( NCT00559585 ) explored the effect of baseline body mass index (BMI) on the pharmacokinetics of and clinical response to subcutaneous (SC) or intraven... |
PMC12746510 | core_pubmed_pmc | Quantitative Model‐Informed Dose Selection for a Milvexian Phase III Study in Patients With Atrial Fibrillation | Quantitative Model‐Informed Dose Selection for a Milvexian Phase III Study in Patients With Atrial Fibrillation Abstract Abstract Milvexian, an activated factor XI inhibitor, is being evaluated in the LIBREXIA phase III program for the prevention of thrombotic events, including in patients with atrial fibrillation (LIB... |
PMC10410848 | core_pubmed_pmc | Influence of timing of Levosimendan administration on outcomes in cardiac surgery | Influence of timing of Levosimendan administration on outcomes in cardiac surgery Abstract Abstract Purpose Though a subgroup analysis has shown improved survival for patients suffering severely reduced ventricular function undergoing coronary artery bypass grafting, RCTs were not able to demonstrate overall beneficial... |
PMC11473394 | core_pubmed_pmc | PBPK-based translation from preclinical species to humans for the full-size IgG therapeutic efalizumab | PBPK-based translation from preclinical species to humans for the full-size IgG therapeutic efalizumab Abstract Introduction Animal models play a vital role in pharmaceutical research and development by supporting the planning and design of later clinical studies. To improve confidence and reliability of first in human... |
PMC11557628 | core_pubmed_pmc | The impact of age and renal function on the pharmacokinetics and protein binding characteristics of fludarabine in paediatric and adult patients undergoing allogeneic haematopoietic stem cell transplantation conditioning | The impact of age and renal function on the pharmacokinetics and protein binding characteristics of fludarabine in paediatric and adult patients undergoing allogeneic haematopoietic stem cell transplantation conditioning Abstract Abstract Aim To evaluate the population pharmacokinetics of unbound F-Ara-A (the circulati... |
PMC3369139 | core_pubmed_pmc | Preclinical evaluation of two 68 Ga-siderophores as potential radiopharmaceuticals for Aspergillus fumigatus infection imaging | Preclinical evaluation of two 68 Ga-siderophores as potential radiopharmaceuticals for Aspergillus fumigatus infection imaging Abstract Purpose Invasive pulmonary aspergillosis is mainly caused by Aspergillus fumigatus , and is one of the major causes of morbidity and mortality in immunocompromised patients. The mortal... |
PMC7845657 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic-Pharmacodynamics Model Characterizing CYP2C19 Polymorphisms to Predict Clopidogrel Pharmacokinetics and Its Anti-Platelet Aggregation Effect Following Oral Administration to Coronary Artery Disease Patients With or Without Diabetes | Physiologically-Based Pharmacokinetic-Pharmacodynamics Model Characterizing CYP2C19 Polymorphisms to Predict Clopidogrel Pharmacokinetics and Its Anti-Platelet Aggregation Effect Following Oral Administration to Coronary Artery Disease Patients With or Without Diabetes Abstract Background and Objective: Clopidogrel (CL... |
PMC8541175 | core_pubmed_pmc | Phase Lag Entropy as a Surrogate Measurement of Hypnotic Depth during Sevoflurane Anesthesia | Phase Lag Entropy as a Surrogate Measurement of Hypnotic Depth during Sevoflurane Anesthesia Abstract Background and Objectives : Phase lag entropy, an electroencephalographic monitor, evaluates the variety in temporal patterns of phase relationship between frontal and prefrontal brain region. Phase lag entropy can ref... |
PMC11071686 | core_pubmed_pmc | Nano vitamin E improved the antioxidant capacity of broiler chickens | Nano vitamin E improved the antioxidant capacity of broiler chickens Abstract Abstract Vitamin E (VE) is a potent nutritional antioxidant that is critical in alleviating poultry oxidative stress. However, the hydrophobic nature and limited stability of VE restrict its effective utilization. Nanotechnology offers a prom... |
PMC2890319 | core_pubmed_pmc | An exploratory study of sunitinib plus paclitaxel as first-line treatment for patients with advanced breast cancer | An exploratory study of sunitinib plus paclitaxel as first-line treatment for patients with advanced breast cancer Abstract Abstract Background: Sunitinib has shown single-agent activity in patients with previously treated metastatic breast cancer (MBC). We investigated the safety of the combination of sunitinib and pa... |
PMC10296931 | core_pubmed_pmc | Dose Optimization in Oncology Drug Development: The Emerging Role of Pharmacogenomics, Pharmacokinetics, and Pharmacodynamics | Dose Optimization in Oncology Drug Development: The Emerging Role of Pharmacogenomics, Pharmacokinetics, and Pharmacodynamics Abstract Abstract Simple Summary Accelerated clinical development of anticancer drugs is crucial to ensure patients’ access to the most safe and effective treatments. At the same time, the devel... |
PMC12267423 | core_pubmed_pmc | Comparisons of pharmacokinetics of glimepiride in combination with Ojeok-san versus glimepiride alone: an open-label, one-sequence, two-treatment controlled clinical study | Comparisons of pharmacokinetics of glimepiride in combination with Ojeok-san versus glimepiride alone: an open-label, one-sequence, two-treatment controlled clinical study Abstract Abstract Glimepiride remains a cost-effective antidiabetic treatment despite its potential risks. However, its interaction with traditional... |
PMC4137940 | core_pubmed_pmc | Frequencies of two functionally significant SNPs and their haplotypes of organic anion transporting polypeptide 1B1 SLCO1B1 gene in six ethnic groups of Pakistani population | Frequencies of two functionally significant SNPs and their haplotypes of organic anion transporting polypeptide 1B1 SLCO1B1 gene in six ethnic groups of Pakistani population Abstract Abstract Objective(s): Organic anion transporter polypeptide 1B1 (OATP1B1) encoded by solute carrier organic transporter 1B1 (SLCO1B1) ge... |
PMC10875059 | core_pubmed_pmc | Pharmacogenomics and non-genetic factors affecting drug response in autism spectrum disorder in Thai and other populations: current evidence and future implications | Pharmacogenomics and non-genetic factors affecting drug response in autism spectrum disorder in Thai and other populations: current evidence and future implications Abstract Autism spectrum disorder (ASD) may affect family and social life profoundly. Although there is no selective pharmacotherapy for ASD, the Food and ... |
PMC4317230 | core_pubmed_pmc | Genetic variation in aryl N -acetyltransferase results in significant differences in the pharmacokinetic and safety profiles of amifampridine (3,4-diaminopyridine) phosphate | Genetic variation in aryl N -acetyltransferase results in significant differences in the pharmacokinetic and safety profiles of amifampridine (3,4-diaminopyridine) phosphate Abstract Abstract The clinical use of amifampridine phosphate for neuromuscular junction disorders is increasing. The metabolism of amifampridine ... |
PMC12354672 | core_pubmed_pmc | Curated CYP450 Interaction Dataset: Covering the Majority of Phase I Drug Metabolism | Curated CYP450 Interaction Dataset: Covering the Majority of Phase I Drug Metabolism Abstract We collected and organized a detailed dataset encompassing both substrates and non-substrates for six principal cytochrome P450 (CYP450) isozymes, responsible for 90% of Phase I drug metabolism in humans. These isozymes, speci... |
PMC4120018 | core_pubmed_pmc | Application of a Physiologically Based Pharmacokinetic Model to Predict OATP1B1 -Related Variability in Pharmacodynamics of Rosuvastatin | Application of a Physiologically Based Pharmacokinetic Model to Predict OATP1B1 -Related Variability in Pharmacodynamics of Rosuvastatin Abstract Abstract Typically, pharmacokinetic–pharmacodynamic (PK/PD) models use plasma concentration as the input that drives the PD model. However, interindividual variability in upt... |
PMC6046475 | core_pubmed_pmc | Safe use of proton pump inhibitors in patients with cirrhosis | Safe use of proton pump inhibitors in patients with cirrhosis Abstract Aims Proton pump inhibitors (PPIs) belong to the most frequently used drugs, also in patients with cirrhosis. PPIs are extensively metabolized by the liver, but practice guidance on prescribing in cirrhosis is lacking. We aim to develop practical gu... |
PMC4474170 | core_pubmed_pmc | Population Pharmacokinetics of Obinutuzumab (GA101) in Chronic Lymphocytic Leukemia (CLL) and Non-Hodgkin's Lymphoma and Exposure–Response in CLL | Population Pharmacokinetics of Obinutuzumab (GA101) in Chronic Lymphocytic Leukemia (CLL) and Non-Hodgkin's Lymphoma and Exposure–Response in CLL Abstract Abstract Treatment regimens involving obinutuzumab (GA101) demonstrated increased efficacy to rituximab in clinical trials for non-Hodgkin's lymphoma (NHL) and chron... |
PMC10582675 | core_pubmed_pmc | Drug–drug interaction study of ciprofol and sodium divalproex: Pharmacokinetics, pharmacodynamics, and safety in healthy Chinese subjects | Drug–drug interaction study of ciprofol and sodium divalproex: Pharmacokinetics, pharmacodynamics, and safety in healthy Chinese subjects Abstract Abstract Ciprofol (also known as HSK3486) is a promising intravenous anesthetic candidate derived from propofol and independently developed by Haisco Pharmaceutical Group Co... |
PMC4775973 | core_pubmed_pmc | Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria | Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria Abstract Abstract Artemether-lumefantrine is a first-line regimen for the treatment of uncomplicated malaria during the second and third trimesters of pregnancy. Pr... |
PMC10276002 | core_pubmed_pmc | Measuring the diversity gap of cannabis clinical trial participants compared to people who report using cannabis | Measuring the diversity gap of cannabis clinical trial participants compared to people who report using cannabis Abstract Abstract Little is known about the demographics of people who use cannabis, including how use trends within population subgroups have evolved over time. It is therefore challenging to know if the de... |
PMC3651412 | core_pubmed_pmc | Optimization of personalized therapies for anticancer treatment | Optimization of personalized therapies for anticancer treatment Abstract Background As today, there are hundreds of targeted therapies for the treatment of cancer, many of which have companion biomarkers that are in use to inform treatment decisions. If we would consider this whole arsenal of targeted therapies as a tr... |
PMC5379095 | core_pubmed_pmc | Availability, Pharmaceutics, Security, Pharmacokinetics, and Pharmacological Activities of Patchouli Alcohol | Availability, Pharmaceutics, Security, Pharmacokinetics, and Pharmacological Activities of Patchouli Alcohol Abstract Patchouli alcohol (PA), a tricyclic sesquiterpene, is one of the critical bioactive ingredients and is mainly isolated from aerial part of Pogostemon cablin (known as guanghuoxiang in China) belonging t... |
PMC12244171 | core_pubmed_pmc | Evaluating the pharmacodynamic effects of padsevonil in healthy volunteers using simultaneous [ 11 C]-UCB-J PET and MR Arterial Spin Labeling measurements | Evaluating the pharmacodynamic effects of padsevonil in healthy volunteers using simultaneous [ 11 C]-UCB-J PET and MR Arterial Spin Labeling measurements Abstract Introduction Integrated PET-MR scanners can measure simultaneously tracer binding, downstream cerebral blood flow (CBF) and neuronal activation. An integrat... |
PMC10984932 | core_pubmed_pmc | Why do we use 100 mg of clofazimine in TB and NTM treatment? | Why do we use 100 mg of clofazimine in TB and NTM treatment? Abstract Abstract Current tuberculosis and non-tuberculous mycobacterial disease guidelines recommend the use of clofazimine in a 100 mg once-daily dose. The rationale behind this exact dose is not provided. I performed a literature review to determine the re... |
PMC5103602 | core_pubmed_pmc | Serum fluoxetine and norfluoxetine levels support the safety of fluoxetine in overdose | Serum fluoxetine and norfluoxetine levels support the safety of fluoxetine in overdose Abstract Abstract Background Previous literature has found fluoxetine to be relatively safe in overdose. This study hopes to examine this idea along with support from published pharmacokinetic information including serum fluoxetine a... |
PMC9785850 | core_pubmed_pmc | Encorafenib Acts as a Dual-Activity Chemosensitizer through Its Inhibitory Effect on ABCC1 Transporter In Vitro and Ex Vivo | Encorafenib Acts as a Dual-Activity Chemosensitizer through Its Inhibitory Effect on ABCC1 Transporter In Vitro and Ex Vivo Abstract Encorafenib (LGX818, trade name Braftovi), a novel BRAF inhibitor, has been approved for the treatment of melanoma and colorectal cancer. In the present work, we evaluated encorafenib’s p... |
PMC6161010 | core_pubmed_pmc | A Simple and Sensitive Liquid Chromatography with Tandem Mass Spectrometric Method for the Simultaneous Determination of Anthraquinone Glycosides and Their Aglycones in Rat Plasma: Application to a Pharmacokinetic Study of Rumex acetosa Extract | A Simple and Sensitive Liquid Chromatography with Tandem Mass Spectrometric Method for the Simultaneous Determination of Anthraquinone Glycosides and Their Aglycones in Rat Plasma: Application to a Pharmacokinetic Study of Rumex acetosa Extract Abstract Abstract Rumex acetosa ( R. acetosa ) has been used in folk remedi... |
PMC5354528 | core_pubmed_pmc | Pharmacokinetics and tolerability of DA-8031, a novel selective serotonin reuptake inhibitor for premature ejaculation in healthy male subjects | Pharmacokinetics and tolerability of DA-8031, a novel selective serotonin reuptake inhibitor for premature ejaculation in healthy male subjects Abstract Objective DA-8031 is a selective serotonin reuptake inhibitor under development for the treatment of premature ejaculation. This is the first-in-human study aimed at e... |
PMC12648364 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics and safety of casdatifan, a novel hypoxia‐inducible factor‐2α inhibitor, in healthy participants | Pharmacokinetics, pharmacodynamics and safety of casdatifan, a novel hypoxia‐inducible factor‐2α inhibitor, in healthy participants Abstract Aims Casdatifan is an orally bioavailable small‐molecule hypoxia‐inducible factor‐2α (HIF‐2α) inhibitor currently in development for treating patients with clear cell renal cell c... |
PMC11685405 | core_pubmed_pmc | Pharmacokinetics of tebipenem pivoxil used in children suffering from shigellosis: a pilot study in Bangladesh | Pharmacokinetics of tebipenem pivoxil used in children suffering from shigellosis: a pilot study in Bangladesh Abstract Abstract With increasing antibiotic resistance in gram-negative bacteria, including those causing Shigellosis, evidence of safety and pharmacokinetics data on new oral antibiotics is crucial. We aimed... |
PMC9611814 | core_pubmed_pmc | Formulation and Evaluation of a Drug-in-Adhesive Patch for Transdermal Delivery of Colchicine | Formulation and Evaluation of a Drug-in-Adhesive Patch for Transdermal Delivery of Colchicine Abstract Gout is one of the most prevalent rheumatic diseases, globally. Colchicine (COL) is the first-line drug used for the treatment of acute gout. However, the oral administration of COL is restricted, owing to serious adv... |
PMC10899319 | core_pubmed_pmc | Protocol for a randomized, placebo-controlled, double-blind phase IIa study of the safety, tolerability, and symptomatic efficacy of the ROCK-inhibitor Fasudil in patients with Parkinson’s disease (ROCK-PD) | Protocol for a randomized, placebo-controlled, double-blind phase IIa study of the safety, tolerability, and symptomatic efficacy of the ROCK-inhibitor Fasudil in patients with Parkinson’s disease (ROCK-PD) Abstract Abstract Background The Rho-kinase (ROCK) inhibitor Fasudil has shown symptomatic and disease-modifying ... |
PMC12735958 | core_pubmed_pmc | Pharmacokinetic Cross-Over Study of Pharmacy-Compounded Chenodeoxycholic Acid Capsules Compared to Authorized Capsules | Pharmacokinetic Cross-Over Study of Pharmacy-Compounded Chenodeoxycholic Acid Capsules Compared to Authorized Capsules Abstract Abstract Purpose: The Amsterdam UMC pharmacy has been compounding chenodeoxycholic acid (CDCA) capsules for Dutch cerebrotendinous xanthomatosis patients since 2018. However, limited data are ... |
PMC11341794 | core_pubmed_pmc | Safety and Efficacy of Multiple Escalating Doses of RC28-E for Neovascular Age-Related Macular Degeneration: A Phase 1b Trial | Safety and Efficacy of Multiple Escalating Doses of RC28-E for Neovascular Age-Related Macular Degeneration: A Phase 1b Trial Abstract Abstract Introduction To assess the safety and efficacy of repeated intravitreal injections of RC28-E, a novel bispecific antibody that simultaneously binds vascular endothelial growth ... |
PMC6194310 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Integration to Evaluate the Changes in Susceptibility of Actinobacillus pleuropneumoniae After Repeated Administration of Danofloxacin | Pharmacokinetic/Pharmacodynamic Integration to Evaluate the Changes in Susceptibility of Actinobacillus pleuropneumoniae After Repeated Administration of Danofloxacin Abstract Abstract To evaluate the relationship between pharmacokinetic/pharmacodynamic (PK/PD) parameters and changes in susceptibility and resistance fr... |
PMC8516514 | core_pubmed_pmc | Antiviral Activity and Pharmacokinetics of the Hepatitis B Virus (HBV) Capsid Assembly Modulator GLS4 in Patients With Chronic HBV Infection | Antiviral Activity and Pharmacokinetics of the Hepatitis B Virus (HBV) Capsid Assembly Modulator GLS4 in Patients With Chronic HBV Infection Abstract Abstract Background GLS4 is a first-in-class hepatitis B virus (HBV) capsid assembly modulator (class I) that can inhibit HBV replication by interfering with the assembly... |
PMC9662202 | core_pubmed_pmc | Performance of Cox proportional hazard models on recovering the ground truth of confounded exposure–response relationships for large‐molecule oncology drugs | Performance of Cox proportional hazard models on recovering the ground truth of confounded exposure–response relationships for large‐molecule oncology drugs Abstract Abstract A Cox proportional hazard (CoxPH) model is conventionally used to assess exposure–response (E–R), but its performance to uncover the ground truth... |
PMC6657004 | core_pubmed_pmc | Artificial Intelligence and Pharmacometrics: Time to Embrace, Capitalize, and Advance? | Artificial Intelligence and Pharmacometrics: Time to Embrace, Capitalize, and Advance? Methods ML Methods for Pharmacometrics Model selection in pharmacometrics is often described as a linear process, starting with “structural” features and followed by random effects and covariate effects, each tested one at a time. In... |
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