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PMC3333798 | core_pubmed_pmc | Pharmacodynamic analysis of the analgesic effect of capsaicin 8% patch (Qutenza™) in diabetic neuropathic pain patients: detection of distinct response groups | Pharmacodynamic analysis of the analgesic effect of capsaicin 8% patch (Qutenza™) in diabetic neuropathic pain patients: detection of distinct response groups Abstract Abstract Treatment of chronic pain is associated with high variability in the response to pharmacological interventions. A mathematical pharmacodynamic ... |
PMC10506699 | core_pubmed_pmc | Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine | Novel Approaches to Characterize Individual Drug Metabolism and Advance Precision Medicine Abstract Abstract Interindividual variability in drug metabolism can significantly affect drug concentrations in the body and subsequent drug response. Understanding an individual’s drug metabolism capacity is important for predi... |
PMC7666712 | core_pubmed_pmc | An in-silico study on selected organosulfur compounds as potential drugs for SARS-CoV-2 infection via binding multiple drug targets | An in-silico study on selected organosulfur compounds as potential drugs for SARS-CoV-2 infection via binding multiple drug targets Abstract Abstract The emerging paradigm shift from ‘one molecule, one target, for one disease’ towards ‘multi-targeted small molecules’ has paved an ingenious pathway in drug discovery in ... |
PMC8085979 | core_pubmed_pmc | Phase 1b study of galunisertib and ramucirumab in patients with advanced hepatocellular carcinoma | Phase 1b study of galunisertib and ramucirumab in patients with advanced hepatocellular carcinoma Abstract Abstract Background Preclinical data suggest that vascular endothelial growth factor (VEGF) and transforming growth factor (TGF)‐β signaling interact to stimulate angiogenesis and suppress antitumor immune respons... |
PMC7395816 | core_pubmed_pmc | Pharmacokinetics, tissue distribution and excretion of 6- O -demethylmenisporphine, a bioactive oxoisoaporphine alkaloid from Menispermi Rhizoma, as determined by a HPLC-MS/MS method | Pharmacokinetics, tissue distribution and excretion of 6- O -demethylmenisporphine, a bioactive oxoisoaporphine alkaloid from Menispermi Rhizoma, as determined by a HPLC-MS/MS method Abstract Highlights • A HPLC-MS/MS method for analysis of 6- O -demethylmenisporphine in biomatrices was firstly developed. • The HPLC-MS... |
PMC12115326 | core_pubmed_pmc | Novel Drug–Drug Cocrystalline Forms of Carbamazepine with Sulfacetamide: Preparation, Characterization, and In Vitro/In Vivo Performance Evaluation | Novel Drug–Drug Cocrystalline Forms of Carbamazepine with Sulfacetamide: Preparation, Characterization, and In Vitro/In Vivo Performance Evaluation Abstract Abstract Objectives : Drug–drug cocrystallization represents a promising approach for the development of novel combination drugs with improved physicochemical and ... |
PMC11276960 | core_pubmed_pmc | CTC-177, a novel drug–Fc conjugate, shows promise as an immunoprophylactic agent against multidrug-resistant Gram-negative bacterial infections | CTC-177, a novel drug–Fc conjugate, shows promise as an immunoprophylactic agent against multidrug-resistant Gram-negative bacterial infections Abstract Abstract Background The widespread emergence of antibiotic resistance including MDR in Gram-negative bacterial pathogens poses a critical challenge to the current anti... |
PMC7519830 | core_pubmed_pmc | A Rare Case of Euphoria Caused by Lidocaine After an Erector Spinae Plane Block: A Case Report | A Rare Case of Euphoria Caused by Lidocaine After an Erector Spinae Plane Block: A Case Report Abstract Abstract Lidocaine is a cost-effective drug that is widely used for local and regional anesthesia. However, central nervous system (CNS) toxicity can occur when lidocaine is administered above the maximum recommended... |
PMC5573929 | core_pubmed_pmc | Reduction of postprandial glucose by lixisenatide vs sitagliptin treatment in J apanese patients with type 2 diabetes on background insulin glargine: A randomized phase IV study (NEXTAGE Study) | Reduction of postprandial glucose by lixisenatide vs sitagliptin treatment in J apanese patients with type 2 diabetes on background insulin glargine: A randomized phase IV study (NEXTAGE Study) Abstract Aim To evaluate the pharmacodynamics of lixisenatide once daily vs sitagliptin once daily in J apanese patients with ... |
PMC10239516 | core_pubmed_pmc | An assessment of nicotine pharmacokinetics and subjective effects of the pulze heated tobacco system compared with cigarettes | An assessment of nicotine pharmacokinetics and subjective effects of the pulze heated tobacco system compared with cigarettes Abstract Abstract Nicotine delivery and subjective effects are determinants of the ability of potentially less harmful tobacco products such as heated tobacco products (HTPs) to support adult sm... |
PMC9062351 | core_pubmed_pmc | Novel mono-lipidated dimeric glucagon-like peptide-1 receptor agonist with improved long-acting and hypoglycemic activity † | Novel mono-lipidated dimeric glucagon-like peptide-1 receptor agonist with improved long-acting and hypoglycemic activity † Abstract Dimerization is a useful tool to boost ligand–receptor interaction. Both lipidation and dimerization effectively prolong the short half-life ( t 1/2 ) of peptides by facilitating binding ... |
PMC9294735 | core_pubmed_pmc | Pharmacokinetics and Main Metabolites of Anwulignan in Mice | Pharmacokinetics and Main Metabolites of Anwulignan in Mice Abstract Abstract Anwulignan is a representative component of Chinese traditional medicine Schisandra sphenanthera , with strong pharmacological activities. However, there are few reports on its pharmacokinetics and metabolites in the body. In this study, a me... |
PMC12008253 | core_pubmed_pmc | Assessment of the biocompatibility and biodistribution of fluorescent oleic acid capped ZnSe/CdS/ core shell quantum dots after intravenous injection in Balb/c mice | Assessment of the biocompatibility and biodistribution of fluorescent oleic acid capped ZnSe/CdS/ core shell quantum dots after intravenous injection in Balb/c mice Abstract Introduction: Quantum dots (QDs) are semiconductor nanocrystals with inherent fluorescence having several advantages over traditional fluorescent ... |
PMC12783171 | core_pubmed_pmc | Population Pharmacokinetics of a Novel Oral Fosfomycin Prophylactic Scheme in the Plasma and Prostate of Patients Undergoing Endoscopic Surgery for Benign Prostatic Hyperplasia | Population Pharmacokinetics of a Novel Oral Fosfomycin Prophylactic Scheme in the Plasma and Prostate of Patients Undergoing Endoscopic Surgery for Benign Prostatic Hyperplasia Abstract Abstract Background and Objective Fosfomycin trometamol may be a valuable option for antimicrobial prophylaxis before urological surge... |
PMC12327295 | core_pubmed_pmc | Pharmacokinetics and safety evaluation of anemoside B4 in healthy Beagle dogs | Pharmacokinetics and safety evaluation of anemoside B4 in healthy Beagle dogs Abstract Background Anemoside B4 (AB4), a pentacyclic triterpenoid saponin extracted from the traditional Chinese medicinal herb Pulsatilla chinensis , has shown anti-inflammatory and immunomodulatory effects in both preclinical and clinical ... |
PMC7329797 | core_pubmed_pmc | Population pharmacokinetics of standard-dose meropenem in critically ill patients on continuous renal replacement therapy: a prospective observational trial | Population pharmacokinetics of standard-dose meropenem in critically ill patients on continuous renal replacement therapy: a prospective observational trial Abstract Abstract Background The primary objective of this study was to develop a population pharmacokinetic model of meropenem, based on the population of critica... |
PMC8875329 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Model of Gold Nanoparticle-Based Drug Delivery System for Stavudine Biodistribution | Physiologically Based Pharmacokinetic (PBPK) Model of Gold Nanoparticle-Based Drug Delivery System for Stavudine Biodistribution Abstract Abstract Computational modelling has gained attention for evaluating nanoparticle-based drug delivery systems. Physiologically based pharmacokinetic (PBPK) modelling provides a mecha... |
PMC5925426 | core_pubmed_pmc | Propranolol pharmacokinetics in infants treated for Infantile Hemangiomas requiring systemic therapy: Modeling and dosing regimen recommendations | Propranolol pharmacokinetics in infants treated for Infantile Hemangiomas requiring systemic therapy: Modeling and dosing regimen recommendations Abstract Abstract Propranolol has become the first choice therapy for complicated Infantile Hemangiomas ( IH ). The pharmacokinetics of propranolol were evaluated after repea... |
PMC8331296 | core_pubmed_pmc | Effect of Single-Dose and Short-Term Administration of Si Jun Zi Tang on the Pharmacokinetics of Gefitinib in Rats | Effect of Single-Dose and Short-Term Administration of Si Jun Zi Tang on the Pharmacokinetics of Gefitinib in Rats Abstract Abstract Background Si Jun Zi Tang (SJZ), a four-herb Chinese medicine formula that has been described for approximately one thousand years, is often prescribed for cancer patients as a complement... |
PMC8455565 | core_pubmed_pmc | Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection | Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection Abstract Abstract The selective Bruton tyrosine kinase (BTK) inhibitor poseltinib has been shown to inhibit the BCR signal transduction pathway and cytokine production in B cell... |
PMC5982750 | core_pubmed_pmc | SNPs in predicting clinical efficacy and toxicity of chemotherapy: walking through the quicksand | SNPs in predicting clinical efficacy and toxicity of chemotherapy: walking through the quicksand Abstract Abstract In the “precision medicine” era, chemotherapy still remains the backbone for the treatment of many cancers, but no affordable predictors of response to the chemodrugs are available in clinical practice. Si... |
PMC6767367 | core_pubmed_pmc | Pharmacokinetic Properties of Ibuprofen (IBU) From the Fixed‐Dose Combination IBU/Caffeine (400/100 mg; FDC) in Comparison With 400 mg IBU as Acid or Lysinate Under Fasted and Fed Conditions—Data From 2 Single‐Center, Single‐Dose, Randomized Crossover Studies in Healthy Volunteers | Pharmacokinetic Properties of Ibuprofen (IBU) From the Fixed‐Dose Combination IBU/Caffeine (400/100 mg; FDC) in Comparison With 400 mg IBU as Acid or Lysinate Under Fasted and Fed Conditions—Data From 2 Single‐Center, Single‐Dose, Randomized Crossover Studies in Healthy Volunteers Abstract Abstract Rapid onset of analg... |
PMC7384155 | core_pubmed_pmc | A randomized, double‐blind, single‐dose, three‐arm, parallel group study to determine pharmacokinetic similarity of ABP 959 and eculizumab (Soliris ® ) in healthy male subjects | A randomized, double‐blind, single‐dose, three‐arm, parallel group study to determine pharmacokinetic similarity of ABP 959 and eculizumab (Soliris ® ) in healthy male subjects Abstract Abstract Objectives ABP 959 is a proposed biosimilar to eculizumab, a monoclonal antibody targeting the human C5 complement protein. T... |
PMC11386250 | core_pubmed_pmc | A randomized, double‐blind, placebo‐controlled, dose‐escalating phase IIa trial to evaluate the safety, tolerability, efficacy, and pharmacokinetics of multiple oral doses of Pynegabine tablets as add‐on therapy in patients with focal epilepsy | A randomized, double‐blind, placebo‐controlled, dose‐escalating phase IIa trial to evaluate the safety, tolerability, efficacy, and pharmacokinetics of multiple oral doses of Pynegabine tablets as add‐on therapy in patients with focal epilepsy Abstract Abstract Aims This study aims to investigate the safety, tolerabili... |
PMC3742415 | core_pubmed_pmc | Analysis of UGT1A1*28 genotype and SN-38 pharmacokinetics for irinotecan-based chemotherapy in patients with advanced colorectal cancer: results from a multicenter, retrospective study in Shanghai | Analysis of UGT1A1*28 genotype and SN-38 pharmacokinetics for irinotecan-based chemotherapy in patients with advanced colorectal cancer: results from a multicenter, retrospective study in Shanghai Abstract Background The UGT1A1*28 polymorphism, although closely linked with CPT-11-related adverse effects, cannot be used... |
PMC9163831 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Colistin Combined With Isopropoxy Benzene Guanidine Against mcr-1 -Positive Salmonella in an Intestinal Infection Model | Pharmacokinetics and Pharmacodynamics of Colistin Combined With Isopropoxy Benzene Guanidine Against mcr-1 -Positive Salmonella in an Intestinal Infection Model Abstract Plasmid-borne colistin resistance mediated by mcr-1 is a growing problem, which poses a serious challenge to the clinical application of colistin for ... |
PMC6933800 | core_pubmed_pmc | Particulate Systems in the Enhancement of the Antiglaucomatous Drug Pharmacodynamics: A Meta-Analysis Study | Particulate Systems in the Enhancement of the Antiglaucomatous Drug Pharmacodynamics: A Meta-Analysis Study Abstract Abstract Glaucoma is a very serious disease that can lead to blindness in severe cases. In an attempt to increase the efficacy of the drugs used in treating this disease, many particulate systems (micro/... |
PMC8212741 | core_pubmed_pmc | Adverse event profiles of epidermal growth factor receptor‐tyrosine kinase inhibitors in cancer patients: A systematic review and meta‐analysis | Adverse event profiles of epidermal growth factor receptor‐tyrosine kinase inhibitors in cancer patients: A systematic review and meta‐analysis Abstract Abstract Abstract The efficacy of agents targeting epidermal growth factor receptor (EGFR) in patients with various cancers was well elucidated. However, the safety pr... |
PMC12548078 | core_pubmed_pmc | Circadian clock genes and insomnia: molecular mechanisms and therapeutic implications | Circadian clock genes and insomnia: molecular mechanisms and therapeutic implications Abstract Abstract Background Insomnia, affecting 30–40% of the global population, is a debilitating sleep disorder linked to significant health risks, including cardiovascular disease, metabolic syndrome, and neurodegeneration. Emergi... |
PMC8673996 | core_pubmed_pmc | SwissPK cdw – A clinical data warehouse for the optimization of pediatric dosing regimens | SwissPK cdw – A clinical data warehouse for the optimization of pediatric dosing regimens Abstract Abstract Clinical trials have been performed mainly in adults and accordingly the necessary information is lacking for pediatric patients, especially regarding dosage recommendation for approved drugs. This gap in informa... |
PMC8650159 | core_pubmed_pmc | Tanimilast, A Novel Inhaled Pde4 Inhibitor for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease | Tanimilast, A Novel Inhaled Pde4 Inhibitor for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease Abstract Abstract Chronic respiratory diseases are the third leading cause of death, behind cardiovascular diseases and cancer, affecting approximately 550 million of people all over the world. Most of the c... |
PMC4961458 | core_pubmed_pmc | The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer | The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer Abstract Abstract ER-targeted therapeutics provide valuable treatment options for patients with ER+ breast cancer, however, current relapse and mortality rates emphasize the need for improved therapeutic strateg... |
PMC12749976 | core_pubmed_pmc | Pharmacodynamics of direct oral anticoagulants associated with post-endoscopic delayed mucosal resection bleeding of colorectal neoplasms | Pharmacodynamics of direct oral anticoagulants associated with post-endoscopic delayed mucosal resection bleeding of colorectal neoplasms Abstract Anticoagulant effects of direct oral anticoagulants (DOACs) are influenced by their plasma levels and anti-factor Xa (FXa) activity. Delayed bleeding is a major adverse even... |
PMC7277767 | core_pubmed_pmc | Review on Current Status of Echinocandins Use | Review on Current Status of Echinocandins Use Abstract Abstract Fungal infections are rising all over the world every year. There are only five medical compound classes for treatment: triazoles, echinocandins, polyenes, flucytosine and allylamine. Currently, echinocandins are the most important compounds, because of th... |
PMC5814316 | core_pubmed_pmc | Effects of ketoconazole on cyclophosphamide metabolism: evaluation of CYP3A4 inhibition effect using the in vitro and in vivo models | Effects of ketoconazole on cyclophosphamide metabolism: evaluation of CYP3A4 inhibition effect using the in vitro and in vivo models Abstract Cyclophosphamide (CP) is widely used in anticancer therapy regimens and 2-dechloroethylcyclophosphamide (DECP) is its side-chain dechloroethylated metabolite. N-dechloroethylatio... |
PMC10953761 | core_pubmed_pmc | Polypharmacy and precision medicine | Polypharmacy and precision medicine Abstract Precision medicine is an approach to maximise the effectiveness of disease treatment and prevention and minimise harm from medications by considering relevant demographic, clinical, genomic and environmental factors in making treatment decisions. Precision medicine is comple... |
PMC9856157 | core_pubmed_pmc | Pancreatic Cancer Resistance to Treatment: The Role of Microbiota | Pancreatic Cancer Resistance to Treatment: The Role of Microbiota Abstract Abstract Pancreatic cancer (PC) is an aggressive malignancy and the fourth leading cause of cancer death in the United States and Europe. It is estimated that PC will be the second leading cause of cancer death by 2030. In addition to late diagn... |
PMC6882484 | core_pubmed_pmc | Influence of verapamil on the pharmacokinetics of oridonin in rats | Influence of verapamil on the pharmacokinetics of oridonin in rats Abstract Abstract Context: Oridonin has been traditionally used in Chinese treatment of various cancers, but its poor bioavailability limits its therapeutic uses. Verapamil can enhance the absorption of some drugs with poor oral bioavailability. Whether... |
PMC11199618 | core_pubmed_pmc | A novel insight into neurological disorders through HDAC6 protein–protein interactions | A novel insight into neurological disorders through HDAC6 protein–protein interactions Abstract Abstract Due to its involvement in physiological and pathological processes, histone deacetylase 6 (HDAC6) is considered a promising pharmaceutical target for several neurological manifestations. However, the exact regulator... |
PMC10638233 | core_pubmed_pmc | Optimal molecular binding data and pharmacokinetic profiles of novel potential triple-action inhibitors of chymase, spleen tyrosine kinase, and prostaglandin D2 receptor in the treatment of asthma | Optimal molecular binding data and pharmacokinetic profiles of novel potential triple-action inhibitors of chymase, spleen tyrosine kinase, and prostaglandin D2 receptor in the treatment of asthma Abstract Abstract Background Asthma is a chronic and complex pulmonary condition that affects the airways. A total of 250,0... |
PMC7357297 | core_pubmed_pmc | Increased dystrophin production with golodirsen in patients with Duchenne muscular dystrophy | Increased dystrophin production with golodirsen in patients with Duchenne muscular dystrophy Abstract Objective To report safety, pharmacokinetics, exon 53 skipping, and dystrophin expression in golodirsen-treated patients with Duchenne muscular dystrophy (DMD) amenable to exon 53 skipping. Methods Part 1 was a randomi... |
PMC12131164 | core_pubmed_pmc | Synthesis and biological characterization of an orally bioavailable lactate dehydrogenase-A inhibitor against pancreatic cancer | Synthesis and biological characterization of an orally bioavailable lactate dehydrogenase-A inhibitor against pancreatic cancer Abstract Abstract Lactate dehydrogenase-A (LDHA) is the major isoform of lactate dehydrogenases (LDH) that is overexpressed and linked to poor survival in pancreatic ductal adenocarcinoma (PDA... |
PMC12139233 | core_pubmed_pmc | Pericardial Effusion Associated With Direct Oral Anticoagulant Use in a Single Center Experience | Pericardial Effusion Associated With Direct Oral Anticoagulant Use in a Single Center Experience Abstract Abstract Background Pericardial effusion (PEff) has been described to occur in association with direct oral anticoagulant (DOAC). Objectives The purpose of this study was to assess the incidence, characteristics, a... |
PMC9669016 | core_pubmed_pmc | First-in-human phase Ia study of the PI3Kα inhibitor CYH33 in patients with solid tumors | First-in-human phase Ia study of the PI3Kα inhibitor CYH33 in patients with solid tumors Abstract PIK3CA mutations are highly prevalent in solid tumors. Targeting phosphatidylinositol 3-kinase α is therefore an attractive strategy for treating cancers harboring PIK3CA mutations. Here, we report the results from a phase... |
PMC4762581 | core_pubmed_pmc | Safety of apixaban for venous thromboembolism prophylaxis: the evidence to date | Safety of apixaban for venous thromboembolism prophylaxis: the evidence to date Abstract Abstract Apixaban, a direct orally active anticoagulant (selective, direct factor Xa inhibitor) is approved for (primary) prevention of venous thromboembolism (VTE) in patients undergoing elective total-hip or total-knee arthroplas... |
PMC6320772 | core_pubmed_pmc | Pharmacodynamic Effect of Luteolin Micelles on Alleviating Cerebral Ischemia Reperfusion Injury | Pharmacodynamic Effect of Luteolin Micelles on Alleviating Cerebral Ischemia Reperfusion Injury Abstract Oxidative stress and inflammation are important mechanisms of cerebral ischemia reperfusion (IR) injury. Luteolin (Lu), one of the major active components in the classical Tibetan prescription, which has been used i... |
PMC3220843 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of High-Dose Human Regular U-500 Insulin Versus Human Regular U-100 Insulin in Healthy Obese Subjects | Pharmacokinetics and Pharmacodynamics of High-Dose Human Regular U-500 Insulin Versus Human Regular U-100 Insulin in Healthy Obese Subjects Abstract Abstract OBJECTIVE Human regular U-500 (U-500R) insulin (500 units/mL) is increasingly being used clinically, yet its pharmacokinetics (PK) and pharmacodynamics (PD) have ... |
PMC12655065 | core_pubmed_pmc | Practical Pharmacokinetic–Pharmacodynamic Models in Oncology | Practical Pharmacokinetic–Pharmacodynamic Models in Oncology Abstract Abstract Integrated pharmacokinetic (PK) and pharmacodynamic (PD) models are essential for the understanding of quantitative relationship between drug exposure and response towards the identification of optimal dosing regimens in drug development and... |
PMC11315824 | core_pubmed_pmc | Pharmacokinetics, Tolerability, and Safety of Esmethadone in Subjects with Chronic Kidney Disease or Hepatic Impairment | Pharmacokinetics, Tolerability, and Safety of Esmethadone in Subjects with Chronic Kidney Disease or Hepatic Impairment Abstract Abstract Background and Objectives Esmethadone (dextromethadone; d-methadone; S-methadone (+)-methadone; REL-1017) is a low potency N -methyl- D -aspartate (NMDA) receptor channel blocker tha... |
PMC11442496 | core_pubmed_pmc | Pharmacokinetics and pharmacogenomics of ribociclib in black patients with metastatic breast cancer the LEANORA study | Pharmacokinetics and pharmacogenomics of ribociclib in black patients with metastatic breast cancer the LEANORA study Abstract Abstract Underrepresented populations’ participation in clinical trials remains limited, and the potential impact of genomic variants on drug metabolism remains elusive. This study aimed to ass... |
PMC5655345 | core_pubmed_pmc | Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children | Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children Abstract Background The antiretroviral drug nevirapine and the antimalarial artemisinin-based combination therapy artemether-lumefantrine are commonly co-administered to treat malaria in the context o... |
PMC12804472 | core_pubmed_pmc | Molecular insights into the bioactivity of H-thiazine compounds against breast cancer cells: a computational study | Molecular insights into the bioactivity of H-thiazine compounds against breast cancer cells: a computational study Abstract Abstract Breast cancer, a leading cause of global mortality, necessitates novel therapies targeting key drivers like the epidermal growth factor receptor (EGFR). This computational study evaluates... |
PMC9246790 | core_pubmed_pmc | Unbound Brain-to-Plasma Partition Coefficient, K p,uu,brain —a Game Changing Parameter for CNS Drug Discovery and Development | Unbound Brain-to-Plasma Partition Coefficient, K p,uu,brain —a Game Changing Parameter for CNS Drug Discovery and Development Abstract Abstract Purpose More than 15 years have passed since the first description of the unbound brain-to-plasma partition coefficient (K p,uu,brain ) by Prof. Margareta Hammarlund-Udenaes, w... |
PMC6595623 | core_pubmed_pmc | Effect of allopurinol in addition to hypothermia treatment in neonates for hypoxic-ischemic brain injury on neurocognitive outcome ( ALBINO ): study protocol of a blinded randomized placebo-controlled parallel group multicenter trial for superiority (phase III) | Effect of allopurinol in addition to hypothermia treatment in neonates for hypoxic-ischemic brain injury on neurocognitive outcome ( ALBINO ): study protocol of a blinded randomized placebo-controlled parallel group multicenter trial for superiority (phase III) Abstract Background Perinatal asphyxia and resulting hypox... |
PMC4966484 | core_pubmed_pmc | Therapeutic drug monitoring of eculizumab: Rationale for an individualized dosing schedule | Therapeutic drug monitoring of eculizumab: Rationale for an individualized dosing schedule Abstract Abstract The annual cost of eculizumab maintenance therapy in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic–uremic syndrome (aHUS) exceeds $300,000 per patient. A better understanding of eculizumab pha... |
PMC9293137 | core_pubmed_pmc | Pharmacokinetic Drug‐Drug Interaction Study of Omecamtiv Mecarbil With Amiodarone and Digoxin in Healthy Subjects | Pharmacokinetic Drug‐Drug Interaction Study of Omecamtiv Mecarbil With Amiodarone and Digoxin in Healthy Subjects Abstract Abstract Omecamtiv mecarbil (OM), a novel cardiac myosin activator, is being evaluated for the treatment of heart failure with reduced ejection fraction. In vitro studies demonstrate OM as a substr... |
PMC4211741 | core_pubmed_pmc | Correlation between Compartmental Tenofovir Concentrations and an Ex Vivo Rectal Biopsy Model of Tissue Infectibility in the RMP-02/MTN-006 Phase 1 Study | Correlation between Compartmental Tenofovir Concentrations and an Ex Vivo Rectal Biopsy Model of Tissue Infectibility in the RMP-02/MTN-006 Phase 1 Study Abstract Objectives This study was designed to assess the dose-response relationship between tissue, blood, vaginal and rectal compartment concentrations of tenofovir... |
PMC9501938 | core_pubmed_pmc | Cytotoxic effects of extracts and isolated compounds from Ifloga spicata (forssk.) sch. bip against HepG-2 cancer cell line: Supported by ADMET analysis and molecular docking | Cytotoxic effects of extracts and isolated compounds from Ifloga spicata (forssk.) sch. bip against HepG-2 cancer cell line: Supported by ADMET analysis and molecular docking Abstract The purpose of this study was to determine the anticancer potential of Ifloga spicata ( I. spicata ) against HepG-2 cell line. To assess... |
PMC3051160 | core_pubmed_pmc | Sex Differences in Drug Disposition | Sex Differences in Drug Disposition Abstract Physiological, hormonal, and genetic differences between males and females affect the prevalence, incidence, and severity of diseases and responses to therapy. Understanding these differences is important for designing safe and effective treatments. This paper summarizes sex... |
PMC12845211 | core_pubmed_pmc | Dermal Concentration Versus Systemic Bioavailability of Topical Lidocaine and Tetracaine: An Exploratory Pharmacokinetic Pilot Study in Göttingen Minipigs | Dermal Concentration Versus Systemic Bioavailability of Topical Lidocaine and Tetracaine: An Exploratory Pharmacokinetic Pilot Study in Göttingen Minipigs Abstract Background: Lidocaine, classified as an amide-type agent, and tetracaine, designated as an ester-type agent, are frequently co-formulated for dermatologic p... |
PMC11001781 | core_pubmed_pmc | A toxicology study of Csf2ra complementation and pulmonary macrophage transplantation therapy of hereditary PAP in mice | A toxicology study of Csf2ra complementation and pulmonary macrophage transplantation therapy of hereditary PAP in mice Abstract Pulmonary macrophage transplantation (PMT) is a gene and cell transplantation approach in development as therapy for hereditary pulmonary alveolar proteinosis (hPAP), a surfactant accumulatio... |
PMC8273943 | core_pubmed_pmc | A randomised controlled unblinded multicentre non-inferiority trial with activated vitamin D and prednisolone treatment in patients with minimal change nephropathy (ADAPTinMCN) | A randomised controlled unblinded multicentre non-inferiority trial with activated vitamin D and prednisolone treatment in patients with minimal change nephropathy (ADAPTinMCN) Abstract Background Minimal change nephropathy (MCN) is a common cause of nephrotic syndrome in both adults and children. International guideli... |
PMC3866333 | core_pubmed_pmc | Temporal linear mode complexity as a surrogate measure of the anesthetic drug effects during sevoflurane anesthesia | Temporal linear mode complexity as a surrogate measure of the anesthetic drug effects during sevoflurane anesthesia Abstract Abstract Background The aims of this study were to compare the stability, correlation with end-tidal sevoflurane, and area below the effect (AUC effect ) vs. time curves of temporal linear mode c... |
PMC6977345 | core_pubmed_pmc | Advancing Biosimilar Development Using Pharmacodynamic Biomarkers in Clinical Pharmacology Studies | Advancing Biosimilar Development Using Pharmacodynamic Biomarkers in Clinical Pharmacology Studies Modeling Considerations for PD Biomarker Assessment and PK/PD Similarity Study Design Criteria for PD biomarkers intended to support a demonstration of biosimilarity are inherently different from criteria for surrogate bi... |
PMC7877868 | core_pubmed_pmc | Mechanistic Modeling of Intra‐Tumor Spatial Distribution of Antibody‐Drug Conjugates: Insights into Dosing Strategies in Oncology | Mechanistic Modeling of Intra‐Tumor Spatial Distribution of Antibody‐Drug Conjugates: Insights into Dosing Strategies in Oncology Abstract Abstract Antibody drug conjugates (ADCs) provide targeted delivery of cytotoxic agents directly inside tumor cells. However, many ADCs targeting solid tumors have exhibited limited ... |
PMC9747123 | core_pubmed_pmc | Leveraging patient‐centric sampling for clinical drug development and decentralized clinical trials: Promise to reality | Leveraging patient‐centric sampling for clinical drug development and decentralized clinical trials: Promise to reality Abstract Abstract Advances in the technologies to enable patient‐centric sampling (PCS) have the potential to improve blood sample collection by enabling clinical trial participants to collect samples... |
PMC6765696 | core_pubmed_pmc | Application of Physiologically‐Based and Population Pharmacokinetic Modeling for Dose Finding and Confirmation During the Pediatric Development of Moxifloxacin | Application of Physiologically‐Based and Population Pharmacokinetic Modeling for Dose Finding and Confirmation During the Pediatric Development of Moxifloxacin Abstract Moxifloxacin is a widely used fluoroquinolone for the treatment of complicated intra‐abdominal infections. We applied physiologically‐based pharmacokin... |
PMC8079059 | core_pubmed_pmc | Evaluation of the anti-inflammatory and antioxidant pharmcodynamic compoents of naoxintong capsules as a basis of broad spectrum effects | Evaluation of the anti-inflammatory and antioxidant pharmcodynamic compoents of naoxintong capsules as a basis of broad spectrum effects Abstract Abstract Context Naoxintong capsule (NXT) is one of the most prevalent Traditional Chinese Medicine formulations in the treatment of coronary heart disease (CHD), yet the act... |
PMC7153646 | core_pubmed_pmc | Lisdexamfetamine Dimesylate for Preschool Children with Attention-Deficit/Hyperactivity Disorder | Lisdexamfetamine Dimesylate for Preschool Children with Attention-Deficit/Hyperactivity Disorder Abstract Abstract Objectives: Describe the safety and tolerability of lisdexamfetamine dimesylate (LDX) and provide data on clinical effects for efficacy-related endpoints and pharmacokinetics in preschool-aged children wit... |
PMC7351863 | core_pubmed_pmc | Determination of the absolute bioavailability of oral imatinib using a stable isotopically labeled intravenous imatinib-d8 microdose | Determination of the absolute bioavailability of oral imatinib using a stable isotopically labeled intravenous imatinib-d8 microdose Abstract Abstract Purpose The aim of this study was to ascertain whether the absolute bioavailability of oral imatinib (Glivec®) during steady state plasma pharmacokinetics in cancer pati... |
PMC12731201 | core_pubmed_pmc | Pharmacological and Pharmacokinetic Profile of Cannabidiol in Human Epilepsy: A Review of Metabolism, Therapeutic Drug Monitoring, and Interactions with Antiseizure Medications | Pharmacological and Pharmacokinetic Profile of Cannabidiol in Human Epilepsy: A Review of Metabolism, Therapeutic Drug Monitoring, and Interactions with Antiseizure Medications Abstract Abstract Cannabidiol (CBD) has transitioned from anecdotal use to an evidence-based adjunctive therapy for Lennox–Gastaut syndrome, Dr... |
PMC11696203 | core_pubmed_pmc | Body mass index affects imatinib exposure: Real‐world evidence from TDM with adaptive dosing | Body mass index affects imatinib exposure: Real‐world evidence from TDM with adaptive dosing Abstract Abstract Background Imatinib is the treatment of elderly or frail patients with chronic myeloid leukemia (CML). Trough levels of around 1000 ng/ml are considered as the target exposure. Objectives We searched for basel... |
PMC11862793 | core_pubmed_pmc | Population pharmacokinetics and exposure–response relationships of dostarlimab in primary advanced or recurrent endometrial cancer in part 1 of RUBY | Population pharmacokinetics and exposure–response relationships of dostarlimab in primary advanced or recurrent endometrial cancer in part 1 of RUBY Abstract Abstract Aims Dostarlimab‐gxly is a humanized monoclonal antibody of the IgG4 isotype that binds to the programmed cell death protein‐1 (PD‐1) receptor and blocks... |
PMC4805697 | core_pubmed_pmc | Morphine interaction with prasugrel: a double-blind, cross-over trial in healthy volunteers | Morphine interaction with prasugrel: a double-blind, cross-over trial in healthy volunteers Abstract Background Morphine decreases the concentrations and effects of clopidogrel, which could lead to treatment failure in myocardial infarction. Objectives To clarify whether more potent P2Y 12 -inhibitors may provide an ef... |
PMC11193826 | core_pubmed_pmc | Central Nervous System Medications: Pharmacokinetic and Pharmacodynamic Considerations for Older Adults | Central Nervous System Medications: Pharmacokinetic and Pharmacodynamic Considerations for Older Adults Abstract Most drugs have not been evaluated in the older population. Recognizing physiological alterations associated with changes in drug disposition and with the ultimate effect, especially in central nervous syste... |
PMC10535484 | core_pubmed_pmc | Development and Pharmacokinetic Evaluation of Novasomes for the Trans-nasal Delivery of Fluvoxamine Using Arachidonic Acid-Carboxymethyl Chitosan Conjugate | Development and Pharmacokinetic Evaluation of Novasomes for the Trans-nasal Delivery of Fluvoxamine Using Arachidonic Acid-Carboxymethyl Chitosan Conjugate Abstract Depression is the major mental illness which causes along with loss of interest in daily life, a feeling of hopelessness, appetite or weight changes, anger... |
PMC10954323 | core_pubmed_pmc | Twice-Daily Dosing of Dolutegravir in Infants on Rifampicin Treatment: A Pharmacokinetic Substudy of the EMPIRICAL Trial | Twice-Daily Dosing of Dolutegravir in Infants on Rifampicin Treatment: A Pharmacokinetic Substudy of the EMPIRICAL Trial Abstract Abstract Background We evaluated dolutegravir pharmacokinetics in infants with human immunodeficiency virus (HIV) receiving dolutegravir twice daily (BID) with rifampicin-based tuberculosis ... |
PMC8502297 | core_pubmed_pmc | Model-based assessment of the safety of community interventions with primaquine in sub-Saharan Africa | Model-based assessment of the safety of community interventions with primaquine in sub-Saharan Africa Abstract Abstract Background Single low-dose primaquine (SLD-PQ) is recommended in combination with artemisinin-based combination therapy to reduce Plasmodium falciparum transmission in areas threatened by artemisinin ... |
PMC9932205 | core_pubmed_pmc | Clofazimine for the treatment of tuberculosis | Clofazimine for the treatment of tuberculosis Abstract Shorter (6–9 months), fully oral regimens containing new and repurposed drugs are now the first-choice option for the treatment of drug-resistant tuberculosis (DR-TB). Clofazimine, long used in the treatment of leprosy, is one such repurposed drug that has become a... |
PMC7256122 | core_pubmed_pmc | Pharmacodynamic assessment of mycophenolic acid in resting and activated target cell population during the first year after renal transplantation | Pharmacodynamic assessment of mycophenolic acid in resting and activated target cell population during the first year after renal transplantation Abstract Aims To explore the pharmacodynamics of mycophenolic acid (MPA) through inosine monophosphate dehydrogenase (IMPDH) capacity measurement and purine levels in periphe... |
PMC6969462 | core_pubmed_pmc | The effect of therapeutic drug monitoring of beta-lactam and fluoroquinolones on clinical outcome in critically ill patients: the DOLPHIN trial protocol of a multi-centre randomised controlled trial | The effect of therapeutic drug monitoring of beta-lactam and fluoroquinolones on clinical outcome in critically ill patients: the DOLPHIN trial protocol of a multi-centre randomised controlled trial Abstract Abstract Background Critically ill patients undergo extensive physiological alterations that will have impact on... |
PMC10339703 | core_pubmed_pmc | Safety, tolerability, pharmacokinetic/pharmacodynamic characteristics of bersiporocin, a novel prolyl‐tRNA synthetase inhibitor, in healthy subjects | Safety, tolerability, pharmacokinetic/pharmacodynamic characteristics of bersiporocin, a novel prolyl‐tRNA synthetase inhibitor, in healthy subjects Abstract Abstract Bersiporocin, a novel first‐in‐class prolyl‐tRNA synthetase (PRS) inhibitor currently under clinical development, was shown to exert an antifibrotic effe... |
PMC11546852 | core_pubmed_pmc | Preparation and Pharmacokinetics of Brain-Targeted Nanoliposome Loaded with Rutin | Preparation and Pharmacokinetics of Brain-Targeted Nanoliposome Loaded with Rutin Abstract Rutin is a flavonoid compound with potential for treating Alzheimer’s disease, preventing brain damage, mitigating cerebral ischemia–reperfusion injury, and exhibiting anti-glioblastoma activity. However, its efficacy is limited ... |
PMC10386914 | core_pubmed_pmc | CYP3A4*22 Genotype-Guided Dosing of Kinase Inhibitors in Cancer Patients | CYP3A4*22 Genotype-Guided Dosing of Kinase Inhibitors in Cancer Patients Abstract Introduction A genetic variant explaining a part of the exposure of many kinase inhibitors (KIs) is the single nucleotide polymorphism (SNP) CYP3A4*22 , resulting in less CYP3A4 enzyme activity. The primary aim of this study was to invest... |
PMC9860979 | core_pubmed_pmc | In-Depth Analysis of Physiologically Based Pharmacokinetic (PBPK) Modeling Utilization in Different Application Fields Using Text Mining Tools | In-Depth Analysis of Physiologically Based Pharmacokinetic (PBPK) Modeling Utilization in Different Application Fields Using Text Mining Tools Abstract Abstract In the past decade, only a small number of papers have elaborated on the application of physiologically based pharmacokinetic (PBPK) modeling across different ... |
PMC10606431 | core_pubmed_pmc | Exploring Hydrophilic PD-L1 Radiotracers Utilizing Phosphonic Acids: Insights into Unforeseen Pharmacokinetics | Exploring Hydrophilic PD-L1 Radiotracers Utilizing Phosphonic Acids: Insights into Unforeseen Pharmacokinetics Abstract Immune checkpoint inhibitor therapy targeting the PD-1/PD-L1 axis in cancer patients, is a promising oncological treatment. However, the number of non-responders remains high, causing a burden for the... |
PMC11578133 | core_pubmed_pmc | Development of a physiologically based pharmacokinetic model of fostemsavir and its pivotal application to support dosing in pregnancy | Development of a physiologically based pharmacokinetic model of fostemsavir and its pivotal application to support dosing in pregnancy Abstract Abstract It is critical to understand the impact of significant physiological changes during pregnancy on the extent of maternal and fetal drug exposure. Fostemsavir (FTR) is a... |
PMC11925446 | core_pubmed_pmc | Prediction and prevention of post-procedural bleedings in patients with cirrhosis | Prediction and prevention of post-procedural bleedings in patients with cirrhosis Abstract Although post-procedural bleedings are infrequent in patients with cirrhosis, they are associated with significant morbidity and mortality. Therefore, predicting and preventing such bleedings is important. Established predictors ... |
PMC10534806 | core_pubmed_pmc | Pharmacokinetic Analysis of Ethanol in a Human Study: New Modification of Mathematic Model | Pharmacokinetic Analysis of Ethanol in a Human Study: New Modification of Mathematic Model Abstract Abstract In the pharmacokinetic analysis of ethanol after oral administration, only single- or two-compartment models are used, but their precision in estimating pharmacokinetic parameters might be insufficient. In a rec... |
PMC8597184 | core_pubmed_pmc | A randomized study of natalizumab dosing regimens for relapsing–remitting multiple sclerosis | A randomized study of natalizumab dosing regimens for relapsing–remitting multiple sclerosis Abstract Background: REFINE was an exploratory, dose- and frequency-blinded, prospective, randomized, dose-ranging study in relapsing–remitting multiple sclerosis (RRMS) patients. Objective: To examine the efficacy, safety, and... |
PMC6702525 | core_pubmed_pmc | Evaluation of Plazomicin, Tigecycline, and Meropenem Pharmacodynamic Exposure against Carbapenem-Resistant Enterobacteriaceae in Patients with Bloodstream Infection or Hospital-Acquired/Ventilator-Associated Pneumonia from the CARE Study (ACHN-490-007) | Evaluation of Plazomicin, Tigecycline, and Meropenem Pharmacodynamic Exposure against Carbapenem-Resistant Enterobacteriaceae in Patients with Bloodstream Infection or Hospital-Acquired/Ventilator-Associated Pneumonia from the CARE Study (ACHN-490-007) Abstract Abstract Introduction CARE was a Phase 3, randomized study... |
PMC9972437 | core_pubmed_pmc | Severity of coeliac disease and clinical management study when using a non-metabolised medication: a phase I pharmacokinetic study | Severity of coeliac disease and clinical management study when using a non-metabolised medication: a phase I pharmacokinetic study Abstract Objective The non-metabolised antihistamine fexofenadine has oral absorption resulting from transporter activity. Uptake by enterocyte organic anion transporting polypeptides and e... |
PMC8262664 | core_pubmed_pmc | Assessing the Pregnancy Protective Impact of Scheduled Nonadherence to a Novel Progestin-Only Pill: Protocol for a Prospective, Multicenter, Randomized, Crossover Study | Assessing the Pregnancy Protective Impact of Scheduled Nonadherence to a Novel Progestin-Only Pill: Protocol for a Prospective, Multicenter, Randomized, Crossover Study Abstract Abstract Background Progestin-only contraceptive pills (POP) are commonly reserved for women with medical comorbidities but in actuality, POPs... |
PMC12678241 | core_pubmed_pmc | Structure-based identification of Jervine as a potent dual-targeting inhibitor of cell cycle kinases | Structure-based identification of Jervine as a potent dual-targeting inhibitor of cell cycle kinases Abstract Mitotic regulators play an essential role in cell cycle progression by ensuring correct chromosomal alignment, segregation, DNA replication, repair, and division, thereby maintaining genomic stability. Aberrant... |
PMC6572254 | core_pubmed_pmc | Reverse Transcriptase Inhibitors Nanosystems Designed for Drug Stability and Controlled Delivery | Reverse Transcriptase Inhibitors Nanosystems Designed for Drug Stability and Controlled Delivery Abstract Abstract An in-depth analysis of nanotechnology applications for the improvement of solubility, distribution, bioavailability and stability of reverse transcriptase inhibitors is reported. Current clinically used n... |
PMC12426234 | core_pubmed_pmc | Zebrafish-based assessment of luteolin’s potential in modulating seizure responses | Zebrafish-based assessment of luteolin’s potential in modulating seizure responses Abstract Introduction Epilepsy is a chronic neurological disorder marked by recurrent seizures. Neuroinflammation and mammalian target of rapamycin (mTOR) signaling are involved in neuronal hyperexcitability, contributing to the onset an... |
PMC7767980 | core_pubmed_pmc | Safety and pharmacokinetics of polatuzumab vedotin in Japanese patients with relapsed/refractory B-cell non-Hodgkin lymphoma: a phase 1 dose-escalation study | Safety and pharmacokinetics of polatuzumab vedotin in Japanese patients with relapsed/refractory B-cell non-Hodgkin lymphoma: a phase 1 dose-escalation study Abstract Abstract Objective A phase 1 dose-escalation study of polatuzumab vedotin (pola) was conducted to assess safety, pharmacokinetics and preliminary antitum... |
PMC7217814 | core_pubmed_pmc | Favorable Pharmacokinetic Characteristics of Extended-Half-Life Recombinant Factor VIII BAY 94-9027 Enable Robust Individual Profiling Using a Population Pharmacokinetic Approach | Favorable Pharmacokinetic Characteristics of Extended-Half-Life Recombinant Factor VIII BAY 94-9027 Enable Robust Individual Profiling Using a Population Pharmacokinetic Approach Abstract Abstract Background Prophylaxis with factor VIII (FVIII) should be individualized based on patient characteristics, including FVIII ... |
PMC7235753 | core_pubmed_pmc | The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches | The Quest to Enhance the Efficacy of Berberine for Type-2 Diabetes and Associated Diseases: Physicochemical Modification Approaches Abstract Berberine is a quaternary isoquinoline alkaloid that has been isolated from numerous plants which are still in use today as medicine and herbal supplements. The great deal of enth... |
PMC10850765 | core_pubmed_pmc | Pharmacogenomic Analysis of CYP3A5*3 and Tacrolimus Trough Concentrations in Vietnamese Renal Transplant Outcomes | Pharmacogenomic Analysis of CYP3A5*3 and Tacrolimus Trough Concentrations in Vietnamese Renal Transplant Outcomes Abstract Abstract Purpose CYP3A5 polymorphisms have been associated with variations in the pharmacokinetics of tacrolimus (Tac) in kidney transplant patients. Our study aims to quantify how the CYP3A5 genot... |
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