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PMC7867880 | core_pubmed_pmc | Narrative review of intrathecal drug delivery (IDD): indications, devices and potential complications | Narrative review of intrathecal drug delivery (IDD): indications, devices and potential complications Abstract The management of chronic refractory pain (non-neoplastic and cancer-related pain) remains a therapeutic challenge. The continuous intrathecal (IT) administration of drugs may play an important role in the pos... |
PMC4944871 | core_pubmed_pmc | A phase I study of the human anti‐activin receptor‐like kinase 1 antibody PF ‐03446962 in Asian patients with advanced solid tumors | A phase I study of the human anti‐activin receptor‐like kinase 1 antibody PF ‐03446962 in Asian patients with advanced solid tumors Abstract Abstract Preclinical studies suggest that ALK ‐1 signaling mediates a complementary angiogenesis pathway activated upon development of resistance to vascular endothelial growth fa... |
PMC11641643 | core_pubmed_pmc | Comparison of Orthogonal Determination Methods of Acid/Base Constants with Meta-Analysis | Comparison of Orthogonal Determination Methods of Acid/Base Constants with Meta-Analysis Abstract The accurate determination of acid/base constants (proton dissociation constants—p K a , or equivalently protonation constants—log K ) is essential for the physicochemical characterization of new molecules, especially in d... |
PMC9783500 | core_pubmed_pmc | Current Status of Therapeutic Drug Monitoring in Mental Health Treatment: A Review | Current Status of Therapeutic Drug Monitoring in Mental Health Treatment: A Review Abstract Therapeutic drug monitoring (TDM) receives growing interest in different psychiatric clinical settings (emergency, inpatient, and outpatient services). Despite its usefulness, TDM remains underemployed in mental health. This is ... |
PMC3899497 | core_pubmed_pmc | Clinical Pharmacokinetics of Clopidogrel and Its Metabolites in Patients with Cardiovascular Diseases | Clinical Pharmacokinetics of Clopidogrel and Its Metabolites in Patients with Cardiovascular Diseases Abstract Abstract Background and Objective Approximately 5–40 % of patients treated with clopidogrel do not display an adequate antiplatelet response. Clopidogrel resistance may be caused by insufficient drug absorptio... |
PMC9031498 | core_pubmed_pmc | Optimizing Antimicrobial Dosing for Critically Ill Patients with MRSA Infections: A New Paradigm for Improving Efficacy during Continuous Renal Replacement Therapy | Optimizing Antimicrobial Dosing for Critically Ill Patients with MRSA Infections: A New Paradigm for Improving Efficacy during Continuous Renal Replacement Therapy Abstract Abstract The dosage regimen of vancomycin, teicoplanin and daptomycin remains controversial for critically ill patients undergoing continuous renal... |
PMC12968516 | core_pubmed_pmc | Single‐Dose Pharmacokinetics of Intranasal Levetiracetam in Healthy Dogs | Single‐Dose Pharmacokinetics of Intranasal Levetiracetam in Healthy Dogs Abstract ABSTRACT Cluster seizures and status epilepticus in dogs are emergencies requiring rapid intervention. Intranasal (IN) benzodiazepines are effective for early seizure cessation, but the pharmacokinetics of longer‐acting antiseizure medica... |
PMC12106149 | core_pubmed_pmc | Safety and Tolerability of Relugolix in Combination with Abiraterone or Apalutamide for Treatment of Patients with Advanced Prostate Cancer: Data from a 52-Week Clinical Trial | Safety and Tolerability of Relugolix in Combination with Abiraterone or Apalutamide for Treatment of Patients with Advanced Prostate Cancer: Data from a 52-Week Clinical Trial Abstract Abstract Background The gonadotropin-releasing hormone (GnRH) receptor antagonist relugolix is the only oral androgen deprivation thera... |
PMC7898166 | core_pubmed_pmc | Personalized Medicine of Monoclonal Antibodies in Inflammatory Bowel Disease: Pharmacogenetics, Therapeutic Drug Monitoring, and Beyond | Personalized Medicine of Monoclonal Antibodies in Inflammatory Bowel Disease: Pharmacogenetics, Therapeutic Drug Monitoring, and Beyond Abstract Abstract The pharmacotherapy of inflammatory bowel diseases (Crohn’s disease and ulcerative colitis) has experienced significant progress with the advent of monoclonal antibod... |
PMC4140707 | core_pubmed_pmc | Predictive performance of gentamicin dosing nomograms | Predictive performance of gentamicin dosing nomograms Abstract Background Several nomograms have been proposed to facilitate the determination of initial gentamicin dosing regimens in clinical settings. This study aimed to assess the predictive performance of these nomograms in Korean patients. Methods Gentamicin conce... |
PMC9913583 | core_pubmed_pmc | Multi-Fold Computational Analysis to Discover Novel Putative Inhibitors of Isethionate Sulfite-Lyase (Isla) from Bilophila wadsworthia: Combating Colorectal Cancer and Inflammatory Bowel Diseases | Multi-Fold Computational Analysis to Discover Novel Putative Inhibitors of Isethionate Sulfite-Lyase (Isla) from Bilophila wadsworthia: Combating Colorectal Cancer and Inflammatory Bowel Diseases Abstract Simple Summary Hydrogen sulfide (H 2 S) has been produced by certain gut bacteria and associated with the developme... |
PMC8645912 | core_pubmed_pmc | Association of cabozantinib pharmacokinetics, progression and toxicity in metastatic renal cell carcinoma patients: results from a pharmacokinetics/pharmacodynamics study | Association of cabozantinib pharmacokinetics, progression and toxicity in metastatic renal cell carcinoma patients: results from a pharmacokinetics/pharmacodynamics study Abstract Background Cabozantinib is a tyrosine kinase inhibitor with a substantial efficacy in metastatic renal cell carcinoma, and is associated wit... |
PMC11275925 | core_pubmed_pmc | Antibiotics, Analgesic Sedatives, and Antiseizure Medications Frequently Used in Critically Ill Neonates: A Narrative Review | Antibiotics, Analgesic Sedatives, and Antiseizure Medications Frequently Used in Critically Ill Neonates: A Narrative Review Abstract Antibiotic, analgesic sedative, and antiseizure medications are among the most commonly used medications in preterm/sick neonates, who are at high risk of nosocomial infections, central ... |
PMC6271459 | core_pubmed_pmc | Method Development and Validation for Pharmacokinetic and Tissue Distributions of Ellagic Acid Using Ultrahigh Performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS) | Method Development and Validation for Pharmacokinetic and Tissue Distributions of Ellagic Acid Using Ultrahigh Performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS) Abstract Ellagic acid is a dietary polyphenol found in numerous fruits and vegetables, possessing several health benefits such as antioxi... |
PMC6968672 | core_pubmed_pmc | Resveratrol loaded glycyrrhizic acid-conjugated human serum albumin nanoparticles for tail vein injection II: pharmacokinetics, tissue distribution and bioavailability | Resveratrol loaded glycyrrhizic acid-conjugated human serum albumin nanoparticles for tail vein injection II: pharmacokinetics, tissue distribution and bioavailability Abstract Abstract There are many kinds of biological activities of resveratrol itself, but its clinical application is limited by its poor solubility in... |
PMC10064633 | core_pubmed_pmc | Efficacy and Safety of Garadacimab in Combination with Standard of Care Treatment in Patients with Severe COVID-19 | Efficacy and Safety of Garadacimab in Combination with Standard of Care Treatment in Patients with Severe COVID-19 Abstract Background Garadacimab, a fully human IgG4 monoclonal antibody, inhibits the kallikrein–kinin pathway at a key initiator, activated coagulation factor XII (FXIIa), and may play a protective role i... |
PMC10052025 | core_pubmed_pmc | Differential Preincubation Effects of Nicardipine on OATP1B1- and OATP1B3-Mediated Transport in the Presence and Absence of Protein: Implications in Assessing OATP1B1- and OATP1B3-Mediated Drug–Drug Interactions | Differential Preincubation Effects of Nicardipine on OATP1B1- and OATP1B3-Mediated Transport in the Presence and Absence of Protein: Implications in Assessing OATP1B1- and OATP1B3-Mediated Drug–Drug Interactions Abstract Abstract Impaired transport activity of hepatic OATP1B1 and OATP1B3 due to drug–drug interactions (... |
PMC11963607 | core_pubmed_pmc | Amikacin dosing in neonates: evaluation of target attainment using a simplified and complex pharmacokinetic model-derived dosing regimen in clinical practice | Amikacin dosing in neonates: evaluation of target attainment using a simplified and complex pharmacokinetic model-derived dosing regimen in clinical practice Abstract ABSTRACT Amikacin is frequently used for the treatment of neonatal sepsis. The Dutch Pediatric Formulary recommends a complex pharmacokinetic (PK) model-... |
PMC12525728 | core_pubmed_pmc | Safety, Pharmacokinetics, Translational and Molecular Mechanistic Insights on the Prostate Cancer Recurrence Suppressor Pseurotin A | Safety, Pharmacokinetics, Translational and Molecular Mechanistic Insights on the Prostate Cancer Recurrence Suppressor Pseurotin A Abstract Abstract Elevated cholesterol levels play important mitogenic roles. Pseurotin A (PsA) is a fermentation product that has recently been reported as a dual inhibitor of proprotein ... |
PMC4688356 | core_pubmed_pmc | Vitamin C in Health and Disease: Its Role in the Metabolism of Cells and Redox State in the Brain | Vitamin C in Health and Disease: Its Role in the Metabolism of Cells and Redox State in the Brain Abstract Ever since Linus Pauling published his studies, the effects of vitamin C have been surrounded by contradictory results. This may be because its effects depend on a number of factors such as the redox state of the ... |
PMC6523079 | core_pubmed_pmc | Pharmacokinetics and Metabolism of Acetyl Triethyl Citrate, a Water-Soluble Plasticizer for Pharmaceutical Polymers in Rats | Pharmacokinetics and Metabolism of Acetyl Triethyl Citrate, a Water-Soluble Plasticizer for Pharmaceutical Polymers in Rats Abstract Acetyl triethyl citrate (ATEC) is a water-soluble plasticizer used in pharmaceutical plasticized polymers. In this study, the pharmacokinetics and metabolism of ATEC were investigated usi... |
PMC7189875 | core_pubmed_pmc | An Introduction to Machine Learning | An Introduction to Machine Learning Abstract In the last few years, machine learning (ML) and artificial intelligence have seen a new wave of publicity fueled by the huge and ever‐increasing amount of data and computational power as well as the discovery of improved learning algorithms. However, the idea of a computer ... |
PMC12717067 | core_pubmed_pmc | AI-assisted identification of innovative phytochemicals from Aizoon canariense aimed at brachyury protein in chordoma: a computational strategy | AI-assisted identification of innovative phytochemicals from Aizoon canariense aimed at brachyury protein in chordoma: a computational strategy Abstract Chordoma is an unique and aggressive bone malignancy along with limited therapeutic options, largely due to the undruggable nature of the TBXT oncoprotein. In this stu... |
PMC10898835 | core_pubmed_pmc | Differential cannabinoid‐like effects and pharmacokinetics of ADB‐BICA, ADB‐BINACA, ADB‐4en‐PINACA and MDMB‐4en‐PINACA in mice: A comparative study | Differential cannabinoid‐like effects and pharmacokinetics of ADB‐BICA, ADB‐BINACA, ADB‐4en‐PINACA and MDMB‐4en‐PINACA in mice: A comparative study Abstract Abstract Despite synthetic cannabinoids' (SCs) prevalent use among humans, these substances often lack comprehensive pharmacological data, primarily due to their r... |
PMC12326963 | core_pubmed_pmc | Clinically applicable parasite viability assay for rapid assessment of antimalarial pharmacodynamic endpoints | Clinically applicable parasite viability assay for rapid assessment of antimalarial pharmacodynamic endpoints Abstract ABSTRACT Evaluating the efficacy of antimalarial drugs is crucial in the fight against malaria, as the parasiticidal effectiveness of these drugs often predicts their clinical success. Parasite Reducti... |
PMC5748433 | core_pubmed_pmc | Study on the effect of EMD386088, a 5-HT 6 receptor partial agonist, in enhancing the anti-immobility action of some antidepressants in rats | Study on the effect of EMD386088, a 5-HT 6 receptor partial agonist, in enhancing the anti-immobility action of some antidepressants in rats Abstract The effect of some antidepressants co-administered with EMD386088 in the modified forced swim test in rats was investigated. Additionally, the pharmacokinetics, metabolic... |
PMC12502310 | core_pubmed_pmc | Bioequivalence evaluation of generic febuxostat versus Feburic ® in healthy Chinese subjects: a randomized crossover study | Bioequivalence evaluation of generic febuxostat versus Feburic ® in healthy Chinese subjects: a randomized crossover study Abstract Abstract Purpose Febuxostat, a xanthine oxidase inhibitor, is a first-line treatment for gout with hyperuricemia. This study evaluated the pharmacokinetic (PK) bioequivalence, safety profi... |
PMC9146401 | core_pubmed_pmc | Current Approaches to Monitor Macromolecules Directly from the Cerebral Interstitial Fluid | Current Approaches to Monitor Macromolecules Directly from the Cerebral Interstitial Fluid Abstract Gaining insights into the pharmacokinetic and pharmacodynamic properties of lead compounds is crucial during drug development processes. When it comes to the treatment of brain diseases, collecting information at the sit... |
PMC9678530 | core_pubmed_pmc | Monitoring of blood immunosuppressant concentrations and lymphocyte activation for predicting viral infections following kidney transplantation: A pilot study | Monitoring of blood immunosuppressant concentrations and lymphocyte activation for predicting viral infections following kidney transplantation: A pilot study Abstract The current standard pharmacokinetic monitoring of immunosuppressive therapy does not consider inter- and intra-individual differences in the biological... |
PMC11054770 | core_pubmed_pmc | Quantification of Etoricoxib in Low Plasma Volume by UPLC-PDA and Application to Preclinical Pharmacokinetic Study | Quantification of Etoricoxib in Low Plasma Volume by UPLC-PDA and Application to Preclinical Pharmacokinetic Study Abstract Abstract An ultra-performance liquid chromatography with photodiode array (UPLC-PDA) UV detection method was developed here for the first time for simple, rapid, selective and sensitive quantifica... |
PMC6950400 | core_pubmed_pmc | Fragmented Dosing of β-alanine Induces A Body Weight-Independent Pharmacokinetic Response | Fragmented Dosing of β-alanine Induces A Body Weight-Independent Pharmacokinetic Response Abstract Abstract Personalised dosing of performance-enhancing food supplements is a hot topic. β-alanine is currently dosed using a fixed dose; however, evidence suggests that this might favour light compared to heavy subjects. A... |
PMC7066280 | core_pubmed_pmc | Clinical pharmacokinetics and pharmacodynamics of ivosidenib, an oral, targeted inhibitor of mutant IDH1, in patients with advanced solid tumors | Clinical pharmacokinetics and pharmacodynamics of ivosidenib, an oral, targeted inhibitor of mutant IDH1, in patients with advanced solid tumors Abstract Summary Background Mutant isocitrate dehydrogenase 1 and 2 (IDH1/IDH2) enzymes produce the oncometabolite D-2-hydroxyglutarate (2-HG). Ivosidenib (AG-120) is a target... |
PMC3667252 | core_pubmed_pmc | A Long-Acting Human Growth Hormone With Delayed Clearance (VRS-317): Results of a Double-Blind, Placebo-Controlled, Single Ascending Dose Study in Growth Hormone–Deficient Adults | A Long-Acting Human Growth Hormone With Delayed Clearance (VRS-317): Results of a Double-Blind, Placebo-Controlled, Single Ascending Dose Study in Growth Hormone–Deficient Adults Abstract Background: Administration of daily recombinant human GH (rhGH) poses a considerable challenge to patient compliance. Reduced dosing... |
PMC9565400 | core_pubmed_pmc | Pilot clinical and pharmacokinetic study of Δ 9 -Tetrahydrocannabinol (THC)/Cannabidiol (CBD) nanoparticle oro-buccal spray in patients with advanced cancer experiencing uncontrolled pain | Pilot clinical and pharmacokinetic study of Δ 9 -Tetrahydrocannabinol (THC)/Cannabidiol (CBD) nanoparticle oro-buccal spray in patients with advanced cancer experiencing uncontrolled pain Abstract This pilot study aimed to assess the safety, tolerability, pharmacokinetics and exploratory analgesic effect of a novel wat... |
PMC5794198 | core_pubmed_pmc | Inhibitors of Trypanosoma cruzi Sir2 related protein 1 as potential drugs against Chagas disease | Inhibitors of Trypanosoma cruzi Sir2 related protein 1 as potential drugs against Chagas disease Abstract Chagas disease remains one of the most neglected diseases in the world despite being the most important parasitic disease in Latin America. The characteristic chronic manifestation of chagasic cardiomyopathy is the... |
PMC12301914 | core_pubmed_pmc | Riboflavin metabolism involved into comparison of therapeutic action of wild-simulated and transplanted Astragali Radix to treat chronic atrophic gastritis rats based on endogenous-xenobiotics metabolism | Riboflavin metabolism involved into comparison of therapeutic action of wild-simulated and transplanted Astragali Radix to treat chronic atrophic gastritis rats based on endogenous-xenobiotics metabolism Abstract Abstract Objective Astragali Radix (AR, Huangqi in Chinese) has been utilized generally as a bulk drug for ... |
PMC4991613 | core_pubmed_pmc | A Single-Dose, Single-Period Pharmacokinetic Assessment of an Extended-Release Orally Disintegrating Tablet of Methylphenidate in Children and Adolescents with Attention-Deficit/Hyperactivity Disorder | A Single-Dose, Single-Period Pharmacokinetic Assessment of an Extended-Release Orally Disintegrating Tablet of Methylphenidate in Children and Adolescents with Attention-Deficit/Hyperactivity Disorder Abstract Abstract Objective: To determine the pharmacokinetic (PK) profile of a proprietary formulation of methylphenid... |
PMC8380243 | core_pubmed_pmc | Differences in P-glycoprotein activity in human and rodent blood–brain barrier assessed by mechanistic modelling | Differences in P-glycoprotein activity in human and rodent blood–brain barrier assessed by mechanistic modelling Abstract Abstract Variation in the efficacy and safety of central nervous system drugs between humans and rodents can be explained by physiological differences between species. An important factor could be P... |
PMC9977891 | core_pubmed_pmc | Translatability of preclinical to early clinical tolerable and pharmacologically active dose ranges for central nervous system active drugs | Translatability of preclinical to early clinical tolerable and pharmacologically active dose ranges for central nervous system active drugs Abstract The primary purpose of this study was to assess the translatability of preclinical to early clinical tolerable and pharmacologically active dose ranges for central nervous... |
PMC4045341 | core_pubmed_pmc | A phase 1, open-label, dose-escalation study of BIIB022 (anti-IGF-1R monoclonal antibody) in subjects with relapsed or refractory solid tumors | A phase 1, open-label, dose-escalation study of BIIB022 (anti-IGF-1R monoclonal antibody) in subjects with relapsed or refractory solid tumors Abstract Summary Purpose The IGF-1R signaling pathway has been implicated in multiple cancers as important for cell survival, proliferation, invasion and metastasis. BIIB022 is ... |
PMC4869338 | core_pubmed_pmc | Pre-clinical evaluation of CYP 2D6 dependent drug–drug interactions between primaquine and SSRI/SNRI antidepressants | Pre-clinical evaluation of CYP 2D6 dependent drug–drug interactions between primaquine and SSRI/SNRI antidepressants Abstract Abstract Background The liver-stage anti-malarial activity of primaquine and other 8-aminoquinoline molecules has been linked to bio-activation through CYP 2D6 metabolism. Factors such as CYP 2D... |
PMC6269943 | core_pubmed_pmc | Determination and Pharmacokinetics of Di-(2-ethylhexyl) Phthalate in Rats by Ultra Performance Liquid Chromatography with Tandem Mass Spectrometry | Determination and Pharmacokinetics of Di-(2-ethylhexyl) Phthalate in Rats by Ultra Performance Liquid Chromatography with Tandem Mass Spectrometry Abstract Abstract Di-(2-ethylhexyl) phthalate (DEHP) is used to increase the flexibility of plastics for industrial products. However, the illegal use of the plasticizer DEH... |
PMC5029575 | core_pubmed_pmc | Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens | Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens Abstract Abstract This randomized, double‐blind, placebo‐controlled, parallel‐group study was to determine the pharmacokinetic characteristics, safety, and tolerability of multiple doses of inhaled loxapine aerosol ... |
PMC9495190 | core_pubmed_pmc | Tissue Penetration of Antimicrobials in Intensive Care Unit Patients: A Systematic Review—Part I | Tissue Penetration of Antimicrobials in Intensive Care Unit Patients: A Systematic Review—Part I Abstract The challenging severity of some infections, especially in critically ill patients, makes the diffusion of antimicrobial drugs within tissues one of the cornerstones of chemotherapy. The knowledge of how antibacter... |
PMC10011554 | core_pubmed_pmc | BET inhibitor trotabresib in heavily pretreated patients with solid tumors and diffuse large B-cell lymphomas | BET inhibitor trotabresib in heavily pretreated patients with solid tumors and diffuse large B-cell lymphomas Abstract Abstract Bromodomain and extraterminal proteins (BET) play key roles in regulation of gene expression, and may play a role in cancer-cell proliferation, survival, and oncogenic progression. CC-90010-ST... |
PMC9028280 | core_pubmed_pmc | Emerging Albumin-Binding Anticancer Drugs for Tumor-Targeted Drug Delivery: Current Understandings and Clinical Translation | Emerging Albumin-Binding Anticancer Drugs for Tumor-Targeted Drug Delivery: Current Understandings and Clinical Translation Abstract Abstract Albumin has shown remarkable promise as a natural drug carrier by improving pharmacokinetic (PK) profiles of anticancer drugs for tumor-targeted delivery. The exogenous or endoge... |
PMC7260212 | core_pubmed_pmc | Soluble HLA-G expression levels and HLA-G/irinotecan association in metastatic colorectal cancer treated with irinotecan-based strategy | Soluble HLA-G expression levels and HLA-G/irinotecan association in metastatic colorectal cancer treated with irinotecan-based strategy Abstract Abstract We here explore the soluble Human Leukocyte Antigen-G (sHLA-G) expression level as clinical biomarker in metastatic colorectal cancer (mCRC). To this aim the sHLA-G p... |
PMC11392661 | core_pubmed_pmc | Loganin Ameliorates Acute Kidney Injury and Restores Tofacitinib Metabolism in Rats: Implications for Renal Protection and Drug Interaction | Loganin Ameliorates Acute Kidney Injury and Restores Tofacitinib Metabolism in Rats: Implications for Renal Protection and Drug Interaction Abstract Tofacitinib, a Janus kinase (JAK) inhibitor used to treat rheumatoid arthritis, is metabolized through hepatic cytochrome P450 (CYP), specifically CYP3A1/2 and CYP2C11. Pr... |
PMC7954267 | core_pubmed_pmc | Novel antisense therapy targeting microRNA-132 in patients with heart failure: results of a first-in-human Phase 1b randomized, double-blind, placebo-controlled study | Novel antisense therapy targeting microRNA-132 in patients with heart failure: results of a first-in-human Phase 1b randomized, double-blind, placebo-controlled study Abstract Abstract Aims Cardiac microRNA-132-3p (miR-132) levels are increased in patients with heart failure (HF) and mechanistically drive cardiac remod... |
PMC5795976 | core_pubmed_pmc | The Herb–Drug Pharmacokinetic Interaction of 5-Fluorouracil and Its Metabolite 5-Fluoro-5,6-Dihydrouracil with a Traditional Chinese Medicine in Rats | The Herb–Drug Pharmacokinetic Interaction of 5-Fluorouracil and Its Metabolite 5-Fluoro-5,6-Dihydrouracil with a Traditional Chinese Medicine in Rats Abstract Abstract Background: Xiang-Sha-Liu-Jun-Zi-Tang (XSLJZT) is the most common traditional formula given to colorectal and breast cancer patients in Taiwan, accordin... |
PMC11002205 | core_pubmed_pmc | Dosing optimization of rituximab for primary membranous nephropathy by population pharmacokinetic and pharmacodynamic study | Dosing optimization of rituximab for primary membranous nephropathy by population pharmacokinetic and pharmacodynamic study Abstract Abstract Primary membranous nephropathy (PMN) is the most common cause for adult nephrotic syndrome. Rituximab has demonstrated promising clinical efficacy by random controlled trials and... |
PMC11272611 | core_pubmed_pmc | Phase Ib and pharmacokinetics study of alpelisib, a PIK3CA inhibitor, and capecitabine in patients with advanced solid tumors | Phase Ib and pharmacokinetics study of alpelisib, a PIK3CA inhibitor, and capecitabine in patients with advanced solid tumors Abstract Abstract Background This phase Ib study was performed to determine the safety of combination capecitabine with alpleisib (phosphatidylinositol 3-kinase catalytic subunit p110α blockade)... |
PMC9007292 | core_pubmed_pmc | 8‐Prenylnaringenin tissue distribution and pharmacokinetics in mice and its binding to human serum albumin and cellular uptake in human embryonic kidney cells | 8‐Prenylnaringenin tissue distribution and pharmacokinetics in mice and its binding to human serum albumin and cellular uptake in human embryonic kidney cells Abstract Abstract 8‐Prenylnaringenin (8‐PN), a hop flavonoid, is a promising food substance with health benefits. Compared with nonprenylated naringenin, 8‐PN ex... |
PMC6370240 | core_pubmed_pmc | Mechanistic framework predicts drug-class specific utility of antiretrovirals for HIV prophylaxis | Mechanistic framework predicts drug-class specific utility of antiretrovirals for HIV prophylaxis Abstract Abstract Currently, there is no effective vaccine to halt HIV transmission. However, pre-exposure prophylaxis (PrEP) with the drug combination Truvada can substantially decrease HIV transmission in individuals at ... |
PMC10423561 | core_pubmed_pmc | Effects of the CYP3A inhibitors, voriconazole, itraconazole, and fluconazole on the pharmacokinetics of osimertinib in rats | Effects of the CYP3A inhibitors, voriconazole, itraconazole, and fluconazole on the pharmacokinetics of osimertinib in rats Abstract Abstract Background Osimertinib, as third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), is the first-line treatment approved to treat advanced T790M mu... |
PMC7214223 | core_pubmed_pmc | Utilization of Physiologically Based Pharmacokinetic Modeling in Clinical Pharmacology and Therapeutics: an Overview | Utilization of Physiologically Based Pharmacokinetic Modeling in Clinical Pharmacology and Therapeutics: an Overview Abstract The purpose of this review was to assess the advancement of applications for physiologically based pharmacokinetic (PBPK) modeling in various therapeutic areas. We conducted a PubMed search, and... |
PMC7388097 | core_pubmed_pmc | The first study in pediatric: Population pharmacokinetics of sirolimus and its application in Chinese children with immune cytopenia | The first study in pediatric: Population pharmacokinetics of sirolimus and its application in Chinese children with immune cytopenia Abstract Abstract The narrow therapeutic index and large inter-individual variability in sirolimus pharmacokinetics (PK) make therapeutic drug monitoring (TDM) necessary. Factors responsi... |
PMC5729432 | core_pubmed_pmc | A Phase 1 study of ARQ 087, an oral pan-FGFR inhibitor in patients with advanced solid tumours | A Phase 1 study of ARQ 087, an oral pan-FGFR inhibitor in patients with advanced solid tumours Abstract Background: ARQ 087 is an orally administered pan-FGFR inhibitor with multi-kinase activity. This Phase 1 study evaluated safety, pharmacokinetics, and pharmacodynamics of ARQ 087 and defined the recommended Phase 2 ... |
PMC8224000 | core_pubmed_pmc | Population Pharmacokinetics and Probability of Target Attainment of Different Dosing Regimens of Ceftazidime in Critically Ill Patients with a Proven or Suspected Pseudomonas aeruginosa Infection | Population Pharmacokinetics and Probability of Target Attainment of Different Dosing Regimens of Ceftazidime in Critically Ill Patients with a Proven or Suspected Pseudomonas aeruginosa Infection Abstract Abstract Altered pharmacokinetics (PK) of hydrophilic antibiotics in critically ill patients is common, with possib... |
PMC11043739 | core_pubmed_pmc | Epirubicin for the Treatment of Sepsis and Septic Shock (EPOS-1): study protocol for a randomised, placebo-controlled phase IIa dose-escalation trial | Epirubicin for the Treatment of Sepsis and Septic Shock (EPOS-1): study protocol for a randomised, placebo-controlled phase IIa dose-escalation trial Abstract Introduction Sepsis remains the major cause of death among hospitalised patients in intensive care. While targeting sepsis-causing pathogens with source control ... |
PMC7287933 | core_pubmed_pmc | In Vitro Investigations of Acetohexamide Binding to Glycated Serum Albumin in the Presence of Fatty Acid | In Vitro Investigations of Acetohexamide Binding to Glycated Serum Albumin in the Presence of Fatty Acid Abstract The interaction of drugs with human serum albumin (HSA) is an important element of therapy. Albumin affects the distribution of the drug substance in the body, as well as its pharmacokinetic and pharmacodyn... |
PMC11589337 | core_pubmed_pmc | Bispectral Index Guidance Reduced Target Plasma Propofol Concentration During ERCP in Patients with Liver Cirrhosis | Bispectral Index Guidance Reduced Target Plasma Propofol Concentration During ERCP in Patients with Liver Cirrhosis Abstract Objective The primary aim of this study was to investigate the guidance effect of the bispectral index (BIS) on the target plasma concentration (TPC) of propofol required for deep sedation during... |
PMC4856747 | core_pubmed_pmc | A Long-term Co-perfused Disseminated Tuberculosis-3D Liver Hollow Fiber Model for Both Drug Efficacy and Hepatotoxicity in Babies | A Long-term Co-perfused Disseminated Tuberculosis-3D Liver Hollow Fiber Model for Both Drug Efficacy and Hepatotoxicity in Babies Abstract Treatment of disseminated tuberculosis in children ≤ 6 years has not been optimized. The pyrazinamide-containing combination regimen used to treat disseminated tuberculosis in babie... |
PMC6066954 | core_pubmed_pmc | Effect of hypothermia on interleukin-1 receptor antagonist pharmacodynamics in inflammatory-sensitized hypoxic-ischemic encephalopathy of term newborns | Effect of hypothermia on interleukin-1 receptor antagonist pharmacodynamics in inflammatory-sensitized hypoxic-ischemic encephalopathy of term newborns Abstract Abstract Background Hypothermia is increasingly tested in several neurological conditions, such as neonatal encephalopathy, stroke, traumatic brain injury, sub... |
PMC8234196 | core_pubmed_pmc | FcRn as a Transporter for Nasal Delivery of Biologics: A Systematic Review | FcRn as a Transporter for Nasal Delivery of Biologics: A Systematic Review Abstract FcRn plays a major role in regulating immune homeostasis, but it is also able to transport biologics across cellular barriers. The question of whether FcRn could be an efficient transporter of biologics across the nasal epithelial barri... |
PMC12072232 | core_pubmed_pmc | PBPK Modeling: Empowering Drug Development and Precision Dosing in China | PBPK Modeling: Empowering Drug Development and Precision Dosing in China Abstract ABSTRACT Physiologically based pharmacokinetic (PBPK) modeling, a cornerstone of model‐informed drug development and model‐informed precision dosing, simulates drug disposition in the human body by integrating physiological, biochemical, ... |
PMC10157363 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Analysis of Savolitinib plus Osimertinib in an EGFR Mutation–Positive, MET-Amplified Non–Small Cell Lung Cancer Model | Pharmacokinetic/Pharmacodynamic Analysis of Savolitinib plus Osimertinib in an EGFR Mutation–Positive, MET-Amplified Non–Small Cell Lung Cancer Model Abstract Abstract Osimertinib is a third-generation, irreversible, oral EGFR tyrosine kinase inhibitor (TKI) recommended as first-line treatment for patients with locally... |
PMC11188489 | core_pubmed_pmc | Pharmacokinetic assessment of tacrolimus in combination with deoxyschizandrin in rats | Pharmacokinetic assessment of tacrolimus in combination with deoxyschizandrin in rats Abstract Background Tacrolimus (Tac) is commonly used for postoperative immunosuppressive therapy in transplant patients. However, problems, for example, low bioavailability and unstable plasma concentration, persist for a long time, ... |
PMC11417322 | core_pubmed_pmc | A pilot pharmacokinetic and Metabolite identification study of Erinacine A in a Single landrace pig model | A pilot pharmacokinetic and Metabolite identification study of Erinacine A in a Single landrace pig model Abstract Abstract Erinacine A has been proven to have the ability to protect nerves and have the benefit of neurohealth. However, the pharmacokinetic and metabolites study of erinacine A in pigs, whose physiology a... |
PMC4303402 | core_pubmed_pmc | Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in patients with peripheral arterial disease | Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in patients with peripheral arterial disease Abstract Purpose We previously determined the pharmacokinetic (PK) parameters of landiolol in healthy male volunteers and gynecological patients. In this study, we determined the PK paramet... |
PMC4199969 | core_pubmed_pmc | Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study | Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study Abstract Background Fimasartan is a novel angiotensin II receptor blocker. Fimasartan is mainly eliminated via biliary excretion, and its urinary elimination is less than 3%. Objective Based on guidance from the Uni... |
PMC12304805 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of empagliflozin in paediatric patients aged 10–17 years with type 2 diabetes mellitus | Pharmacokinetics and pharmacodynamics of empagliflozin in paediatric patients aged 10–17 years with type 2 diabetes mellitus Abstract Aims To characterize the pharmacokinetics (PK) and PK/pharmacodynamics (PD) regarding glycosylated haemoglobin (HbA 1c ) lowering using the paediatric data from DINAMO and to assess diff... |
PMC10747400 | core_pubmed_pmc | The Development of Lipid-Based Sorafenib Granules to Enhance the Oral Absorption of Sorafenib | The Development of Lipid-Based Sorafenib Granules to Enhance the Oral Absorption of Sorafenib Abstract Sorafenib (SFN) is an anticancer multi-kinase inhibitor with great therapeutic potential. However, SFN has low aqueous solubility, which limits its oral absorption. Lipids and surfactants have the potential to improve... |
PMC7076507 | core_pubmed_pmc | Preparation and Characterization of a Novel Swellable and Floating Gastroretentive Drug Delivery System ( sf GRDDS) for Enhanced Oral Bioavailability of Nilotinib | Preparation and Characterization of a Novel Swellable and Floating Gastroretentive Drug Delivery System ( sf GRDDS) for Enhanced Oral Bioavailability of Nilotinib Abstract Regarding compliance and minimization of side effects of nilotinib therapy, there is a medical need to have a gastroretentive drug delivery system (... |
PMC7178269 | core_pubmed_pmc | A Machine Learning-Based Identification of Genes Affecting the Pharmacokinetics of Tacrolimus Using the DMET TM Plus Platform | A Machine Learning-Based Identification of Genes Affecting the Pharmacokinetics of Tacrolimus Using the DMET TM Plus Platform Abstract Tacrolimus is an immunosuppressive drug with a narrow therapeutic index and larger interindividual variability. We identified genetic variants to predict tacrolimus exposure in healthy ... |
PMC5411399 | core_pubmed_pmc | Concentration-Dependent Antagonism and Culture Conversion in Pulmonary Tuberculosis | Concentration-Dependent Antagonism and Culture Conversion in Pulmonary Tuberculosis Abstract Abstract Background. There is scant evidence to support target drug exposures for optimal tuberculosis outcomes. We therefore assessed whether pharmacokinetic/pharmacodynamic (PK/PD) parameters could predict 2-month culture con... |
PMC8377444 | core_pubmed_pmc | Phase 1 study in healthy participants of the safety, pharmacokinetics, and pharmacodynamics of enpatoran (M5049), a dual antagonist of toll‐like receptors 7 and 8 | Phase 1 study in healthy participants of the safety, pharmacokinetics, and pharmacodynamics of enpatoran (M5049), a dual antagonist of toll‐like receptors 7 and 8 Abstract Abstract This study evaluated the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple oral doses of enpato... |
PMC11761217 | core_pubmed_pmc | Shenmai injection revives cardiac function in rats with hypertensive heart failure: involvement of microbial-host co-metabolism | Shenmai injection revives cardiac function in rats with hypertensive heart failure: involvement of microbial-host co-metabolism Abstract Heart failure (HF) is a complex syndrome marked by considerable expenditures and elevated mortality and morbidity rates globally. Shenmai injection (SMI), a form of Traditional Chines... |
PMC9978195 | core_pubmed_pmc | The pharmacogenetics of the new-generation antipsychotics – A scoping review focused on patients with severe psychiatric disorders | The pharmacogenetics of the new-generation antipsychotics – A scoping review focused on patients with severe psychiatric disorders Abstract Abstract Exploring the possible correlations between gene variations and the clinical effects of the new-generation antipsychotics is considered essential in the framework of perso... |
PMC8776883 | core_pubmed_pmc | A comprehensive physiologically based pharmacokinetic (PBPK) model for nicotine in humans from using nicotine-containing products with different routes of exposure | A comprehensive physiologically based pharmacokinetic (PBPK) model for nicotine in humans from using nicotine-containing products with different routes of exposure Abstract Abstract Physiologically based pharmacokinetic (PBPK) modeling can be a useful tool for characterizing nicotine pharmacokinetics (PK) from use of t... |
PMC7956511 | core_pubmed_pmc | Response and Toxicity to Cytarabine Therapy in Leukemia and Lymphoma: From Dose Puzzle to Pharmacogenomic Biomarkers | Response and Toxicity to Cytarabine Therapy in Leukemia and Lymphoma: From Dose Puzzle to Pharmacogenomic Biomarkers Abstract Abstract Simple Summary In this review, the authors propose a crosswise examination of cytarabine-related issues ranging from the spectrum of clinical activity and severe toxicities, through upd... |
PMC7496689 | core_pubmed_pmc | Atogepant Has No Clinically Relevant Effects on the Pharmacokinetics of an Ethinyl Estradiol/Levonorgestrel Oral Contraceptive in Healthy Female Participants | Atogepant Has No Clinically Relevant Effects on the Pharmacokinetics of an Ethinyl Estradiol/Levonorgestrel Oral Contraceptive in Healthy Female Participants Abstract Abstract The incidence of migraine is higher among women than men and peaks during the reproductive years, when contraceptive medication use is common. A... |
PMC11895359 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic assessment of oral nicotinamide in the NEAT clinical trial for early Alzheimer’s disease | Pharmacokinetic and pharmacodynamic assessment of oral nicotinamide in the NEAT clinical trial for early Alzheimer’s disease Abstract Background Nicotinamide, a form of B3 vitamin, is an NAD + precursor that reduces pTau 231 levels via histone deacetylase inhibition in murine models of Alzheimer’s disease (AD). A recen... |
PMC7015520 | core_pubmed_pmc | Risk assessment of substances used in food supplements: the example of the botanical Gymnema sylvestre | Risk assessment of substances used in food supplements: the example of the botanical Gymnema sylvestre Abstract Abstract Botanicals and preparations derived from these are among the substances frequently added to foods and food supplements, yet the safety of many botanicals has not been systematically assessed. In the ... |
PMC11528469 | core_pubmed_pmc | Exploring the therapeutic mechanisms of millet in obesity through molecular docking, pharmacokinetics, and dynamic simulation | Exploring the therapeutic mechanisms of millet in obesity through molecular docking, pharmacokinetics, and dynamic simulation Abstract Abstract Obesity, a prevalent global health concern, is characterized by excessive fat accumulation, which confers significant nutritional and health risks, including a shortened lifesp... |
PMC7229331 | core_pubmed_pmc | Bioanalytical method by HPLC-FLD for curcumin analysis in supplemented athletes | Bioanalytical method by HPLC-FLD for curcumin analysis in supplemented athletes Abstract Abstract In sports, curcumin, a substance derived from the rhizome of Curcuma longa (turmeric) plant with antioxidant effect 8 times greater than vitamin E, has attracted the attention of scientists because of its potent antioxidan... |
PMC9234961 | core_pubmed_pmc | Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo | Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo Abstract Abstract The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degr... |
PMC12215139 | core_pubmed_pmc | Impact of body weight on mycophenolic acid population pharmacokinetics in paediatric lupus nephritis: a pharmacogenomic integration study | Impact of body weight on mycophenolic acid population pharmacokinetics in paediatric lupus nephritis: a pharmacogenomic integration study Abstract Abstract Background Mycophenolic acid (MPA) is recommended for the treatment of lupus nephritis (LN). However, the high pharmacokinetic (PK) variability of MPA contributes t... |
PMC11782447 | core_pubmed_pmc | Clinical Pharmacokinetics of Antitubercular Drugs in the Overweight and Obese Population: Implications for Dosage Adjustments | Clinical Pharmacokinetics of Antitubercular Drugs in the Overweight and Obese Population: Implications for Dosage Adjustments Abstract The rise in global obesity prevalence has increased the need to understand the pharmacokinetics of drugs in overweight and obese individuals. Tuberculosis remains a significant health c... |
PMC5788078 | core_pubmed_pmc | Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study | Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study Abstract Background: Children and infants with impaired swallow or compromised enteral absorption require alternative routes for administration of analgesia. Recent clinical guidance and practice fo... |
PMC5662392 | core_pubmed_pmc | Regorafenib-induced retinal and gastrointestinal hemorrhage in a metastatic colorectal cancer patient with liver dysfunction | Regorafenib-induced retinal and gastrointestinal hemorrhage in a metastatic colorectal cancer patient with liver dysfunction Abstract Abstract Rationale: Regorafenib is effective for metastatic colorectal cancer but its toxicity such as hemorrhage should be considered. The safety of regorafenib for the patient with the... |
PMC7299043 | core_pubmed_pmc | Pharmacokinetics during therapeutic hypothermia for neonatal hypoxic ischaemic encephalopathy: a literature review | Pharmacokinetics during therapeutic hypothermia for neonatal hypoxic ischaemic encephalopathy: a literature review Abstract Background Neonatal hypoxic ischaemic encephalopathy due to perinatal asphyxia, can result in severe neurodevelopmental disability or mortality. Hypothermia is at present the only proven neuroprot... |
PMC9985389 | core_pubmed_pmc | New IMB16-4 Hot-Melt Extrusion Preparation Improved Oral Bioavailability and Enhanced Anti-Cholestatic Effect on Rats | New IMB16-4 Hot-Melt Extrusion Preparation Improved Oral Bioavailability and Enhanced Anti-Cholestatic Effect on Rats Abstract Background Cholestasis is challenging to treat due to lacked effective drugs. N-(3,4,5-trichlorophenyl)-2 (3-nitrobenzenesulfonamido) benzamide, abbreviated as IMB16-4, which may be effective f... |
PMC12196179 | core_pubmed_pmc | Chemical Composition and Anti-Lung Cancer Activities of Melaleuca quinquenervia Leaf Essential Oil: Integrating Gas Chromatography–Mass Spectrometry (GC/MS) Profiling, Network Pharmacology, and Molecular Docking | Chemical Composition and Anti-Lung Cancer Activities of Melaleuca quinquenervia Leaf Essential Oil: Integrating Gas Chromatography–Mass Spectrometry (GC/MS) Profiling, Network Pharmacology, and Molecular Docking Abstract Abstract Background/Objectives: This study investigates the phytochemical composition and anticance... |
PMC10931427 | core_pubmed_pmc | CPX-351 Pharmacokinetics and Safety in Adults with Hematologic Malignancies and Renal Function Impairment: Phase 1 Trial | CPX-351 Pharmacokinetics and Safety in Adults with Hematologic Malignancies and Renal Function Impairment: Phase 1 Trial Abstract Abstract Simple Summary CPX-351 has been approved for the treatment of acute myeloid leukemia. Previous studies have indicated that dose adjustment is not warranted for patients with mild to... |
PMC12718314 | core_pubmed_pmc | Antipsychotic load during olanzapine mono- versus polytherapy and in relation to age | Antipsychotic load during olanzapine mono- versus polytherapy and in relation to age Abstract Abstract Purpose While antipsychotic monotherapy is generally recommended in treatment of psychotic disorders, polytherapy is frequently observed in clinical practice. We aimed to investigate the total antipsychotic load among... |
PMC7984881 | core_pubmed_pmc | Classical Active Ingredients and Extracts of Chinese Herbal Medicines: Pharmacokinetics, Pharmacodynamics, and Molecular Mechanisms for Ischemic Stroke | Classical Active Ingredients and Extracts of Chinese Herbal Medicines: Pharmacokinetics, Pharmacodynamics, and Molecular Mechanisms for Ischemic Stroke Abstract Stroke is a leading cause of death and disability worldwide, and approximately 87% of cases are attributed to ischemia. The main factors that cause ischemic st... |
PMC8129567 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Nemonoxacin in a Neutropenic Murine Lung Infection Model Against Streptococcus Pneumoniae | Pharmacokinetics and Pharmacodynamics of Nemonoxacin in a Neutropenic Murine Lung Infection Model Against Streptococcus Pneumoniae Abstract Abstract Nemonoxacin, a novel nonfluorinated quinolone for the treatment of community-acquired pneumonia. We reported the pharmacokinetic/pharmacodynamic (PK/PD) targets and PK/PD ... |
PMC7689521 | core_pubmed_pmc | Phase 2a, open-label, dose-escalating, multi-center pharmacokinetic study of favipiravir (T-705) in combination with oseltamivir in patients with severe influenza | Phase 2a, open-label, dose-escalating, multi-center pharmacokinetic study of favipiravir (T-705) in combination with oseltamivir in patients with severe influenza Abstract Abstract Background The pharmacokinetics and appropriate dose regimens of favipiravir are unknown in hospitalized influenza patients; such data are ... |
PMC8540716 | core_pubmed_pmc | Research Progress in Chinese Herbal Medicines for Treatment of Sepsis: Pharmacological Action, Phytochemistry, and Pharmacokinetics | Research Progress in Chinese Herbal Medicines for Treatment of Sepsis: Pharmacological Action, Phytochemistry, and Pharmacokinetics Abstract Abstract Sepsis is a life-threatening organ dysfunction caused by a dysregulated host response to infection; the pathophysiology of sepsis is complex. The incidence of sepsis is s... |
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