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PMC12901897 | core_pubmed_pmc | Donor and recipient genetic polymorphisms modulate tacrolimus pharmacokinetics during voriconazole co-therapy: a drug–drug interaction study in liver transplant recipients | Donor and recipient genetic polymorphisms modulate tacrolimus pharmacokinetics during voriconazole co-therapy: a drug–drug interaction study in liver transplant recipients Abstract Abstract Background: While recipient cytochrome P450 (CYP) genetic polymorphisms are established modulators of tacrolimus (TAC) pharmacokin... |
PMC12634867 | core_pubmed_pmc | Oral AZD5438 is a clinically translatable otoprotectant against cisplatin-induced hearing loss | Oral AZD5438 is a clinically translatable otoprotectant against cisplatin-induced hearing loss Abstract Highlights • Cisplatin, a mainstay cancer drug, causes irreversible hearing loss in up to 60% of patients, creating a major unmet need. With ∼500,000 U.S. patients receiving platinum and other platinum-based therapie... |
PMC5412926 | core_pubmed_pmc | Impact of Target‐Mediated Elimination on the Dose and Regimen of Evolocumab, a Human Monoclonal Antibody Against Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) | Impact of Target‐Mediated Elimination on the Dose and Regimen of Evolocumab, a Human Monoclonal Antibody Against Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Abstract Abstract Understanding the pharmacokinetic (PK) and pharmacodynamic (PD) relationship of a therapeutic monoclonal antibody against proprotein co... |
PMC8424592 | core_pubmed_pmc | Influence of food on pharmacokinetics and pharmacodynamics of 4-phenylbutyrate in patients with urea cycle disorders | Influence of food on pharmacokinetics and pharmacodynamics of 4-phenylbutyrate in patients with urea cycle disorders Abstract Abstract Urea cycle disorders (UCDs), inborn errors of hepatocyte metabolism, cause hyperammonemia and lead to neurocognitive deficits, coma, and even death. Sodium 4-phenylbutyrate (NaPB), a st... |
PMC3696095 | core_pubmed_pmc | Anti-Tumour Efficacy of Capecitabine in a Genetically Engineered Mouse Model of Pancreatic Cancer | Anti-Tumour Efficacy of Capecitabine in a Genetically Engineered Mouse Model of Pancreatic Cancer Abstract Capecitabine (CAP) is a 5-FU pro-drug approved for the treatment of several cancers and it is used in combination with gemcitabine (GEM) in the treatment of patients with pancreatic adenocarcinoma (PDAC). However,... |
PMC3258254 | core_pubmed_pmc | Intestinal Absorption and First-Pass Metabolism of Polyphenol Compounds in Rat and Their Transport Dynamics in Caco-2 Cells | Intestinal Absorption and First-Pass Metabolism of Polyphenol Compounds in Rat and Their Transport Dynamics in Caco-2 Cells Abstract Abstract Background Polyphenols, a group of complex naturally occurring compounds, are widely distributed throughout the plant kingdom and are therefore readily consumed by humans. The re... |
PMC6595370 | core_pubmed_pmc | A randomized double‐blind, placebo‐controlled clinical phase IIa trial on safety, immunomodulatory effects and pharmacokinetics of EA‐230 during experimental human endotoxaemia | A randomized double‐blind, placebo‐controlled clinical phase IIa trial on safety, immunomodulatory effects and pharmacokinetics of EA‐230 during experimental human endotoxaemia Abstract Abstract Aims EA‐230 is a human chorionic gonadotropin hormone‐derived linear tetrapeptide, developed for the treatment of systemic in... |
PMC8912909 | core_pubmed_pmc | Drug development for the treatment of onchocerciasis: Population pharmacokinetic and adverse events modeling of emodepside | Drug development for the treatment of onchocerciasis: Population pharmacokinetic and adverse events modeling of emodepside Abstract Abstract Background To accelerate the progress towards onchocerciasis elimination, a macrofilaricidal drug that kills the adult parasite is urgently needed. Emodepside has shown macrofilar... |
PMC4937648 | core_pubmed_pmc | Pharmacokinetics, safety, and tolerability following single-dose migalastat hydrochloride (GR181413A/AT1001) in healthy male Japanese subjects | Pharmacokinetics, safety, and tolerability following single-dose migalastat hydrochloride (GR181413A/AT1001) in healthy male Japanese subjects Abstract Abstract Objective Fabry disease is a rare X-linked disease caused by mutations to the GLA gene, resulting in a deficiency of the lysosomal enzyme alpha-galactosidase A... |
PMC3546736 | core_pubmed_pmc | Effects of Schizonepetin on Activity and mRNA Expression of Cytochrome P450 Enzymes in Rats | Effects of Schizonepetin on Activity and mRNA Expression of Cytochrome P450 Enzymes in Rats Abstract The aim of this study was to find out whether Schizonepetin influences the pharmacokinetics of the main substrates drugs of CYP1A2, CYP3A1/2, CYP2E1, CYP2C19 and CYP2D6 in rats; the influence on the levels of CYP mRNA w... |
PMC6362423 | core_pubmed_pmc | Pharmacokinetics, Tissue Distribution, Metabolism, and Excretion of Naringin in Aged Rats | Pharmacokinetics, Tissue Distribution, Metabolism, and Excretion of Naringin in Aged Rats Abstract Abstract Aging is an inevitable biological process characterized by the loss of functional capacity and associated with changes in all phases of pharmacokinetic processes. Naringin, a dietary flavanone glycoside, has been... |
PMC6634414 | core_pubmed_pmc | Discovery of potential urine-accessible metabolite biomarkers associated with muscle disease and corticosteroid response in the mdx mouse model for Duchenne | Discovery of potential urine-accessible metabolite biomarkers associated with muscle disease and corticosteroid response in the mdx mouse model for Duchenne Abstract Urine is increasingly being considered as a source of biomarker development in Duchenne Muscular Dystrophy (DMD), a severe, life-limiting disorder that af... |
PMC5692925 | core_pubmed_pmc | Neurophysiologically-informed markers of individual variability and pharmacological manipulation of human cortical gamma | Neurophysiologically-informed markers of individual variability and pharmacological manipulation of human cortical gamma Abstract The ability to quantify synaptic function at the level of cortical microcircuits from non-invasive data would be enormously useful in the study of neuronal processing in humans and the patho... |
PMC4023283 | core_pubmed_pmc | In vitro and in vivo Evaluation of CYP1A Interaction Potential of Terminalia Arjuna Bark | In vitro and in vivo Evaluation of CYP1A Interaction Potential of Terminalia Arjuna Bark Abstract Terminalia arjuna Wight and Arn. (Combretaceae) is a tree having an extensive medicinal potential in cardiovascular disorders. Triterpenoids are mainly responsible for cardiovascular properties. Aqueous, hydroalcoholic and... |
PMC7003869 | core_pubmed_pmc | First‐in‐Human Study of AG10, a Novel, Oral, Specific, Selective, and Potent Transthyretin Stabilizer for the Treatment of Transthyretin Amyloidosis: A Phase 1 Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Study in Healthy Adult Volunteers | First‐in‐Human Study of AG10, a Novel, Oral, Specific, Selective, and Potent Transthyretin Stabilizer for the Treatment of Transthyretin Amyloidosis: A Phase 1 Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Study in Healthy Adult Volunteers Abstract Abstract AG10 is a novel, potent, and selective oral trans... |
PMC8003343 | core_pubmed_pmc | Species Differences in Microsomal Metabolism of Xanthine-Derived A 1 Adenosine Receptor Ligands | Species Differences in Microsomal Metabolism of Xanthine-Derived A 1 Adenosine Receptor Ligands Abstract Abstract Tracer development for positron emission tomography (PET) requires thorough evaluation of pharmacokinetics, metabolism, and dosimetry of candidate radioligands in preclinical animal studies. Since variation... |
PMC12896485 | core_pubmed_pmc | Risks, Benefits, and Molecular Targets of Fenugreek Administration in the Treatment of Hepatocellular Carcinoma | Risks, Benefits, and Molecular Targets of Fenugreek Administration in the Treatment of Hepatocellular Carcinoma Abstract Simple Summary Liver cancer is a serious disease with limited treatment options, and many patients experience side effects from current therapies. Fenugreek is a commonly used medicinal plant that ha... |
PMC12414031 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Remimazolam | Clinical Pharmacokinetics and Pharmacodynamics of Remimazolam Abstract Abstract Remimazolam is a benzodiazepine with a high affinity for the γ-aminobutyric acid type A-receptor thereby inducing sedation and amnesia. It is a short-acting drug, has a fast onset, short duration of action, and a predictable recovery profil... |
PMC8305619 | core_pubmed_pmc | High-Trough Plasma Concentration of Afatinib Is Associated with Dose Reduction | High-Trough Plasma Concentration of Afatinib Is Associated with Dose Reduction Abstract Simple Summary Afatinib is used to treat non-small-cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) mutation as a second-generation EGFR-tyrosine kinase inhibitor (TKI). We examined the relationship between... |
PMC4614203 | core_pubmed_pmc | Phase I Study of Axitinib in Combination with Cisplatin and Capecitabine in Patients with Previously Untreated Advanced Gastric Cancer | Phase I Study of Axitinib in Combination with Cisplatin and Capecitabine in Patients with Previously Untreated Advanced Gastric Cancer Abstract Purpose This phase I trial evaluated the question of whether the standard starting dose of axitinib could be administered in combination with therapeutic doses of cisplatin/cap... |
PMC12239809 | core_pubmed_pmc | Impact of antibody Fc engineering on translational pharmacology, and safety: insights from industry case studies | Impact of antibody Fc engineering on translational pharmacology, and safety: insights from industry case studies Abstract ABSTRACT Therapeutic monoclonal antibodies (mAbs) are often designed to not only bind targets via their antigen-binding domains (Fabs) but to also engage with cell surface receptors, FcγRs and FcRn,... |
PMC12815976 | core_pubmed_pmc | A comparison of pharmacometric software programs for atezolizumab population pharmacokinetic simulation | A comparison of pharmacometric software programs for atezolizumab population pharmacokinetic simulation Abstract Purpose We compare our experience with three pharmacometric modeling workflows for simulating alternative dosing regimens of atezolizumab: (1) the gold-standard, NONMEM software used in combination with R, (... |
PMC11001548 | core_pubmed_pmc | The Use of Muscle Relaxants After Chemotherapy and Radiotherapy | The Use of Muscle Relaxants After Chemotherapy and Radiotherapy Abstract Abstract Introduction Patients after chemotherapy and radiotherapy while being operated can suffer from different systemic problems, which may complicate the anesthetic management. Some interactions between muscle relaxants and chemotherapeutics c... |
PMC10174233 | core_pubmed_pmc | Toward therapeutic drug monitoring of citalopram in depression? Insights from a systematic review | Toward therapeutic drug monitoring of citalopram in depression? Insights from a systematic review Abstract Background Within the framework of individualized psychopharmacotherapy, therapeutic drug monitoring (TDM) has gained increasing relevance. In the absence of high-quality evidence, the TDM of citalopram (CIT) and ... |
PMC9349160 | core_pubmed_pmc | Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resistant Tuberculosis Patients Receiving Delamanid Alone or Coadministered with Bedaquiline | Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resistant Tuberculosis Patients Receiving Delamanid Alone or Coadministered with Bedaquiline Abstract Background and Objective Delamanid is a nitroimidazole, a novel class of drug for treating tuberculosis, and is primarily metabolized by ... |
PMC5343373 | core_pubmed_pmc | Phase 1b randomized, double-blind study of namilumab, an anti-granulocyte macrophage colony-stimulating factor monoclonal antibody, in mild-to-moderate rheumatoid arthritis | Phase 1b randomized, double-blind study of namilumab, an anti-granulocyte macrophage colony-stimulating factor monoclonal antibody, in mild-to-moderate rheumatoid arthritis Abstract Background Namilumab (AMG203) is an immunoglobulin G1 monoclonal antibody that binds with high affinity to the GM-CSF ligand. This was a p... |
PMC5905882 | core_pubmed_pmc | Efficacy and safety of biosimilar insulins compared to their reference products: A systematic review | Efficacy and safety of biosimilar insulins compared to their reference products: A systematic review Abstract Abstract Importance For nearly a century, no generic form of insulin has been available in the United States. However, the first biosimilar insulin, Basaglar, was approved by the U.S. Food and Drug Administrati... |
PMC8518835 | core_pubmed_pmc | First evaluation of the safety, pharmacokinetics, and pharmacodynamics of BAY 2433334, a small molecule targeting coagulation factor XIa | First evaluation of the safety, pharmacokinetics, and pharmacodynamics of BAY 2433334, a small molecule targeting coagulation factor XIa Abstract Abstract Background Coagulation factor XI (FXI) contributes to the development of thrombosis but appears to play a minor role in hemostasis and is, therefore, an attractive a... |
PMC7801313 | core_pubmed_pmc | Effect of lurbinectedin on the QTc interval in patients with advanced solid tumors: an exposure–response analysis | Effect of lurbinectedin on the QTc interval in patients with advanced solid tumors: an exposure–response analysis Abstract Purpose This study assessed the effect of lurbinectedin, a highly selective inhibitor of oncogenic transcription, on the change from baseline in Fridericia’s corrected QT interval (∆QTcF) and elect... |
PMC5732773 | core_pubmed_pmc | Metabolism, pharmacokinetics, and bioavailability of ZB716, a Steroidal Selective Estrogen Receptor Downregulator (SERD) | Metabolism, pharmacokinetics, and bioavailability of ZB716, a Steroidal Selective Estrogen Receptor Downregulator (SERD) Abstract ZB716 is a selective estrogen receptor downregulator (SERD) with excellent oral bioavailability and superior efficacy. In this study, we investigate the in vitro and in vivo metabolism and t... |
PMC8299459 | core_pubmed_pmc | Structural Investigations, Cellular Imaging, and Radiolabeling of Neutral, Polycationic, and Polyanionic Functional Metalloporphyrin Conjugates | Structural Investigations, Cellular Imaging, and Radiolabeling of Neutral, Polycationic, and Polyanionic Functional Metalloporphyrin Conjugates Abstract Over the past decade, porphyrin derivatives have emerged as invaluable synthetic building blocks and theranostic kits for the delivery of cellular fluorescence imaging... |
PMC12389705 | core_pubmed_pmc | Integrative Transcriptomic and Network Pharmacology Analysis Reveals Key Targets and Mechanisms of Moschus (musk) Against Viral Respiratory Tract Infections | Integrative Transcriptomic and Network Pharmacology Analysis Reveals Key Targets and Mechanisms of Moschus (musk) Against Viral Respiratory Tract Infections Abstract Background/Objectives : Moschus (musk) has long been used in traditional Tibetan medicine to prevent and treat epidemic febrile illnesses. However, its an... |
PMC9029529 | core_pubmed_pmc | Distinct Mechanisms of Cytotoxicity in Novel Nitrogenous Heterocycles: Future Directions for a New Anti-Cancer Agent | Distinct Mechanisms of Cytotoxicity in Novel Nitrogenous Heterocycles: Future Directions for a New Anti-Cancer Agent Abstract Electron-rich, nitrogenous heteroaromatic compounds interact more with biological/cellular components than their non-nitrogenous counterparts. The strong intermolecular interactions with protein... |
PMC6667348 | core_pubmed_pmc | Pharmacokinetic interactions between telmisartan/amlodipine and rosuvastatin after multiple oral administrations in healthy Korean male subjects | Pharmacokinetic interactions between telmisartan/amlodipine and rosuvastatin after multiple oral administrations in healthy Korean male subjects Abstract Abstract Purpose Hypertension and dyslipidemia are major risk factors for cardiovascular diseases, and reduction of cardiovascular risks can be achieved by combining ... |
PMC5874213 | core_pubmed_pmc | Open-Label Single-Sequence Crossover Study Evaluating Pharmacokinetics, Efficacy, and Safety of Once-Daily Dosing of Nitisinone in Patients with Hereditary Tyrosinemia Type 1 | Open-Label Single-Sequence Crossover Study Evaluating Pharmacokinetics, Efficacy, and Safety of Once-Daily Dosing of Nitisinone in Patients with Hereditary Tyrosinemia Type 1 Abstract Abstract Background : Although nitisinone is successfully used to treat hereditary tyrosinemia type 1 (HT-1) with the recommended twice-... |
PMC9887116 | core_pubmed_pmc | SDI-118, a novel procognitive SV2A modulator: First-in-human randomized controlled trial including PET/fMRI assessment of target engagement | SDI-118, a novel procognitive SV2A modulator: First-in-human randomized controlled trial including PET/fMRI assessment of target engagement Abstract Abstract Background: Current treatments for progressive neurodegenerative disorders characterized by cognitive impairment either have limited efficacy or are lacking altog... |
PMC8602551 | core_pubmed_pmc | Effects of Letermovir and/or Methylprednisolone Coadministration on Voriconazole Pharmacokinetics in Hematopoietic Stem Cell Transplantation: A Population Pharmacokinetic Study | Effects of Letermovir and/or Methylprednisolone Coadministration on Voriconazole Pharmacokinetics in Hematopoietic Stem Cell Transplantation: A Population Pharmacokinetic Study Abstract Abstract Objective The aim of this study was to identify factors affecting blood concentrations of voriconazole following letermovir c... |
PMC12398856 | core_pubmed_pmc | A GLP-1 analogue optimized for cAMP-biased signaling improves weight loss in obese mice | A GLP-1 analogue optimized for cAMP-biased signaling improves weight loss in obese mice Abstract Objective Glucagon-like peptide 1 (GLP-1) receptor (GLP-1R) agonism is foundational to modern obesity pharmacotherapies. These compounds were engineered for maximal G protein alpha(s) (Gsα) signaling potency and downstream ... |
PMC10929708 | core_pubmed_pmc | Poor prognostic factors of pharmacokinetic origin predict outcomes in inflammatory bowel disease patients treated with anti-tumor necrosis factor-α | Poor prognostic factors of pharmacokinetic origin predict outcomes in inflammatory bowel disease patients treated with anti-tumor necrosis factor-α Abstract Introduction We evaluated baseline Clearance of anti-tumor necrosis factors and human leukocyte antigen variant (HLA DQA1*05) in combination as poor prognostic fac... |
PMC11986329 | core_pubmed_pmc | Simulation-based evaluation of the impact of dose fractionation study design on antibiotic PKPD analyses | Simulation-based evaluation of the impact of dose fractionation study design on antibiotic PKPD analyses Abstract Abstract Objectives To evaluate the impact of antibiotic dose fractionation study design on pharmacokinetic/pharmacodynamic (PK/PD) indices and PKPD model estimation. Methods PKPD models for meropenem and p... |
PMC6202467 | core_pubmed_pmc | Neovascular Age‐Related Macular Degeneration: A Visual Acuity Model of Natural Disease Progression and Ranibizumab Treatment Effect | Neovascular Age‐Related Macular Degeneration: A Visual Acuity Model of Natural Disease Progression and Ranibizumab Treatment Effect Abstract Abstract Intravitreal ranibizumab is a first‐line therapy for neovascular age‐related macular degeneration (nAMD), but there is a need to optimize patient outcomes while minimizin... |
PMC10092787 | core_pubmed_pmc | A phase 1/2, open‐label, multicenter study of isatuximab in combination with cemiplimab in patients with lymphoma | A phase 1/2, open‐label, multicenter study of isatuximab in combination with cemiplimab in patients with lymphoma Abstract Abstract Patients with relapsed or refractory lymphoma have limited treatment options, requiring newer regimens. In this Phase 1/2 study ( NCT03769181 ), we assessed the safety, efficacy, and pharm... |
PMC6680228 | core_pubmed_pmc | Population pharmacokinetic analysis of certolizumab pegol in patients with Crohn's disease | Population pharmacokinetic analysis of certolizumab pegol in patients with Crohn's disease Abstract Abstract Certolizumab pegol (CZP), an anti–tumor necrosis factor α agent, is an effective therapy for Crohn's disease (CD). A population pharmacokinetic (PK) analysis of subcutaneously administered CZP was performed usin... |
PMC12662786 | core_pubmed_pmc | AAV Gene Therapy Drug Development and Translation of Engineered Ocular and Neurotropic Capsids: A Systematic Review Using Natural Language Processing | AAV Gene Therapy Drug Development and Translation of Engineered Ocular and Neurotropic Capsids: A Systematic Review Using Natural Language Processing Abstract ABSTRACT Natural AAV serotypes often lack specificity and efficiency, leading to off‐target effects and a low therapeutic index. To overcome these limitations of... |
PMC8409961 | core_pubmed_pmc | Star polyester-based folate acid-targeting nanoparticles for doxorubicin and curcumin co-delivery to combat multidrug-resistant breast cancer | Star polyester-based folate acid-targeting nanoparticles for doxorubicin and curcumin co-delivery to combat multidrug-resistant breast cancer Abstract Abstract Chemotherapeutic treatments are indispensable in the treatment of breast cancer. However, the emergence of multidrug-resistance, strong cell toxicity, and poor ... |
PMC7168968 | core_pubmed_pmc | Maternal ABVD chemotherapy for Hodgkin lymphoma in a dichorionic diamniotic pregnancy: a case report | Maternal ABVD chemotherapy for Hodgkin lymphoma in a dichorionic diamniotic pregnancy: a case report Abstract Background Hodgkin lymphoma (HL) is the most common hematological malignancy during pregnancy. The first-line treatment for HL in pregnancy is the standard ABVD regimen without any drug and/or dose adjustment. ... |
PMC12691666 | core_pubmed_pmc | Pharmacokinetic modeling and efficacy of ceftobiprole medocaril against pneumonic tularemia in cynomolgus macaques | Pharmacokinetic modeling and efficacy of ceftobiprole medocaril against pneumonic tularemia in cynomolgus macaques Abstract ABSTRACT Francisella tularensis is the etiologic agent of tularemia, and there are few FDA-approved antibiotics to treat infections. Ceftobiprole medocaril has potential for being developed as a t... |
PMC3476883 | core_pubmed_pmc | Pharmacodynamic Effect of Cilostazol Plus Standard Clopidogrel Versus Double-Dose Clopidogrel in Patients With Type 2 Diabetes Undergoing Percutaneous Coronary Intervention | Pharmacodynamic Effect of Cilostazol Plus Standard Clopidogrel Versus Double-Dose Clopidogrel in Patients With Type 2 Diabetes Undergoing Percutaneous Coronary Intervention Abstract OBJECTIVE To determine the effect of adding cilostazol (100 mg b.i.d.) to standard-dose clopidogrel (75 mg/d) (TRIPLE) compared with doubl... |
PMC12532702 | core_pubmed_pmc | Precemtabart tocentecan, an anti-CEACAM5 antibody–drug conjugate, in metastatic colorectal cancer: a phase 1 trial | Precemtabart tocentecan, an anti-CEACAM5 antibody–drug conjugate, in metastatic colorectal cancer: a phase 1 trial Abstract CEACAM5, a cell surface protein, is overexpressed in colorectal cancer (CRC). Precemtabart tocentecan (Precem-TcT, previously M9140) is an anti-CEACAM5 antibody–drug conjugate with the topoisomera... |
PMC9402719 | core_pubmed_pmc | Optimized scaling of translational factors in oncology: from xenografts to RECIST | Optimized scaling of translational factors in oncology: from xenografts to RECIST Abstract Abstract Purpose Tumor growth inhibition (TGI) models are regularly used to quantify the PK–PD relationship between drug concentration and in vivo efficacy in oncology. These models are typically calibrated with data from xenogra... |
PMC3764110 | core_pubmed_pmc | In Vivo Activity and Pharmacokinetics of Nemorosone on Pancreatic Cancer Xenografts | In Vivo Activity and Pharmacokinetics of Nemorosone on Pancreatic Cancer Xenografts Abstract Pancreatic cancer is one of the leading cancer-related causes of death in the western world with an urgent need for new treatment strategies. Recently, hyperforin and nemorosone have been described as promising anti-cancer lead... |
PMC12159098 | core_pubmed_pmc | Population Pharmacokinetics for Belantamab Mafodotin Monotherapy and Combination Therapies in Patients with Relapsed/Refractory Multiple Myeloma | Population Pharmacokinetics for Belantamab Mafodotin Monotherapy and Combination Therapies in Patients with Relapsed/Refractory Multiple Myeloma Abstract Background and Objective Belantamab mafodotin is an antibody-drug conjugate (ADC) comprising a monoclonal antibody targeting B-cell maturation antigen (BCMA) conjugat... |
PMC5862603 | core_pubmed_pmc | Prolonged in vivo expression and anti-tumor response of DNA-based anti-HER2 antibodies | Prolonged in vivo expression and anti-tumor response of DNA-based anti-HER2 antibodies Abstract Abstract Antibody gene transfer presents an appealing alternative to conventional antibody protein therapy. This pre-clinical study evaluates the impact of various parameters on the pharmacokinetics and efficacy of in vivo e... |
PMC11894798 | core_pubmed_pmc | A model-based evaluation of the pharmacokinetics-pharmacodynamics (PKPD) of avibactam in combination with ceftazidime | A model-based evaluation of the pharmacokinetics-pharmacodynamics (PKPD) of avibactam in combination with ceftazidime Abstract Abstract Background The emergence of β-lactamase-producing bacteria limits the effectiveness of β-lactam (BL) antibiotics, and the combination with a β-lactamase inhibitor (BLI) aims to counter... |
PMC3117731 | core_pubmed_pmc | A systems biology approach to dynamic modeling and inter-subject variability of statin pharmacokinetics in human hepatocytes | A systems biology approach to dynamic modeling and inter-subject variability of statin pharmacokinetics in human hepatocytes Abstract Abstract Background The individual character of pharmacokinetics is of great importance in the risk assessment of new drug leads in pharmacological research. Amongst others, it is severe... |
PMC5951862 | core_pubmed_pmc | Epoetin Biosimilars in the Treatment of Renal Anemia: What Have We Learned from a Decade of European Experience? | Epoetin Biosimilars in the Treatment of Renal Anemia: What Have We Learned from a Decade of European Experience? Abstract Abstract Biosimilars are biological medicines that are approved via stringently defined regulatory pathways on the basis that comparable safety, efficacy, and quality have been demonstrated to their... |
PMC10301217 | core_pubmed_pmc | Prevalence of Drug–Drug Interactions in Primary Care Prescriptions in Egypt: A Cross-Sectional Retrospective Study | Prevalence of Drug–Drug Interactions in Primary Care Prescriptions in Egypt: A Cross-Sectional Retrospective Study Abstract Abstract In clinical practice, drug–drug interactions (DDIs) pose significant risks to a large number of patients. Consequently, healthcare providers are required to diligently identify, monitor, ... |
PMC3396277 | core_pubmed_pmc | A placebo-controlled, double-blind, dose-escalation study to assess the safety, tolerability and pharmacokinetics/pharmacodynamics of single and multiple intravenous infusions of AZD9773 in patients with severe sepsis and septic shock | A placebo-controlled, double-blind, dose-escalation study to assess the safety, tolerability and pharmacokinetics/pharmacodynamics of single and multiple intravenous infusions of AZD9773 in patients with severe sepsis and septic shock Abstract Abstract Introduction Tumor necrosis factor-alpha (TNF-α), an early mediator... |
PMC9884426 | core_pubmed_pmc | A phase 1 clinical trial of the repurposable acetyllysine mimetic, n -methyl-2-pyrrolidone (NMP), in relapsed or refractory multiple myeloma | A phase 1 clinical trial of the repurposable acetyllysine mimetic, n -methyl-2-pyrrolidone (NMP), in relapsed or refractory multiple myeloma Abstract Abstract Background N -methyl-2-pyrrolidone (NMP) is an epigenetically active chemical fragment and organic solvent with numerous applications including use as a drug-del... |
PMC8057977 | core_pubmed_pmc | Pharmacometrics-Based Considerations for the Design of a Pharmacogenomic Clinical Trial Assessing Irinotecan Safety | Pharmacometrics-Based Considerations for the Design of a Pharmacogenomic Clinical Trial Assessing Irinotecan Safety Abstract Abstract Purpose Pharmacometric models provide useful tools to aid the rational design of clinical trials. This study evaluates study design-, drug-, and patient-related features as well as analy... |
PMC7341526 | core_pubmed_pmc | Intravitreal Pharmacokinetic Study of the Antiangiogenic Glycoprotein Opticin | Intravitreal Pharmacokinetic Study of the Antiangiogenic Glycoprotein Opticin Abstract Abstract Opticin is an endogenous vitreous glycoprotein that may have therapeutic potential as it has been shown that supranormal concentrations suppress preretinal neovascularization. Herein we investigated the pharmacokinetics of o... |
PMC6860008 | core_pubmed_pmc | Dose finding for new vaccines: The role for immunostimulation/immunodynamic modelling | Dose finding for new vaccines: The role for immunostimulation/immunodynamic modelling Modeling Immunostimulation (IS) /Immunodynamic (ID) modelling: Mathematical modelling for improved vaccine dose decision making The world of drug development has faced similar drug-dosing questions, yet is far more advanced in the use... |
PMC5572697 | core_pubmed_pmc | A first-in-human study of the novel HIV-fusion inhibitor C34-PEG 4 -Chol | A first-in-human study of the novel HIV-fusion inhibitor C34-PEG 4 -Chol Abstract Long-acting injectable antiretroviral (LA-ARV) drugs with low toxicity profiles and propensity for drug-drug interactions are a goal for future ARV regimens. C34-PEG 4 -Chol is a novel cholesterol tagged LA HIV-fusion-inhibitor (FI). We a... |
PMC8953844 | core_pubmed_pmc | Sex-Specific Catabolic Metabolism Alterations in the Critically Ill following High Dose Vitamin D | Sex-Specific Catabolic Metabolism Alterations in the Critically Ill following High Dose Vitamin D Abstract Pharmacological interventions are essential for the treatment and management of critical illness. Although women comprise a large proportion of the critically ill, sex-specific pharmacological properties are poorl... |
PMC12418472 | core_pubmed_pmc | Modulation of antibody transport in the brain and spinal cord through the intranasal pathway | Modulation of antibody transport in the brain and spinal cord through the intranasal pathway Abstract Abstract The intranasal pathway is a promising antibody delivery route for the treatment of neurological diseases, but the mechanisms mediating nose-to-brain/spinal cord transport are poorly understood. The aim of our ... |
PMC5373004 | core_pubmed_pmc | The History of Clotting Factor Concentrates Pharmacokinetics | The History of Clotting Factor Concentrates Pharmacokinetics Abstract Abstract Clotting factor concentrates (CFCs) underwent tremendous modifications during the last forty years. Plasma-derived concentrates made the replacement therapy feasible not only in the hospital but also at patients’ home by on-demand or prophyl... |
PMC12685592 | core_pubmed_pmc | PEGylation Overcomes Pharmacological Barriers to Improve Systemic Pharmacokinetics and Therapeutic Efficacy of Phages against MDR Escherichia coli | PEGylation Overcomes Pharmacological Barriers to Improve Systemic Pharmacokinetics and Therapeutic Efficacy of Phages against MDR Escherichia coli Abstract Abstract Systemic bacteriophage therapy against multidrug-resistant (MDR) Escherichia coli is fundamentally limited by rapid immune-mediated clearance, complement a... |
PMC10941589 | core_pubmed_pmc | Power to identify exposure‐response relationships in phase IIa pulmonary tuberculosis trials with multi‐dimensional bacterial load modeling | Power to identify exposure‐response relationships in phase IIa pulmonary tuberculosis trials with multi‐dimensional bacterial load modeling Abstract Abstract Adequate power to identify an exposure‐response relationship in a phase IIa clinical trial for pulmonary tuberculosis (TB) is important for dose selection and des... |
PMC12434130 | core_pubmed_pmc | Unveiling the therapeutic potential of caudatin: Structural optimization, pharmacological mechanisms, and therapeutic implications | Unveiling the therapeutic potential of caudatin: Structural optimization, pharmacological mechanisms, and therapeutic implications Abstract Caudatin is a C 21 steroidal glycoside isolated from many species of the genus Cynanchum , has been utilized by traditional medicine to treat cancer and inflammation which is incre... |
PMC3040319 | core_pubmed_pmc | Role of Organic Cation Transporter 1, OCT1 in the Pharmacokinetics and Toxicity of cis -Diammine(pyridine)chloroplatinum(II) and Oxaliplatin in Mice | Role of Organic Cation Transporter 1, OCT1 in the Pharmacokinetics and Toxicity of cis -Diammine(pyridine)chloroplatinum(II) and Oxaliplatin in Mice Abstract Purpose The goal of this study was to test the hypothesis that by controlling intracellular uptake, organic cation transporter 1, Oct1 is a key determinant of the... |
PMC12618410 | core_pubmed_pmc | Immunoglobulin G Receptors (FcγR), in Addition to Target-Antigen and Neonatal Fc Receptor (FcRn), Influence Rituximab Pharmacokinetics | Immunoglobulin G Receptors (FcγR), in Addition to Target-Antigen and Neonatal Fc Receptor (FcRn), Influence Rituximab Pharmacokinetics Abstract Introduction Rituximab, an anti-cluster of differentiation (CD)-20 monoclonal antibody, is used in the treatment of non-Hodgkin lymphoma (NHL), chronic lymphocytic leukemia, an... |
PMC7104901 | core_pubmed_pmc | Single-Dose Euglycemic Clamp Study Demonstrating Pharmacokinetic and Pharmacodynamic Similarity Between SAR341402 Insulin Aspart and US- and EU-Approved Versions of Insulin Aspart in Subjects with Type 1 Diabetes | Single-Dose Euglycemic Clamp Study Demonstrating Pharmacokinetic and Pharmacodynamic Similarity Between SAR341402 Insulin Aspart and US- and EU-Approved Versions of Insulin Aspart in Subjects with Type 1 Diabetes Abstract Background: The objective of this study was to demonstrate the pharmacokinetic and pharmacodynamic... |
PMC8731286 | core_pubmed_pmc | Simultaneous Determination of Ten Bioactive Components from Shenling Baizhu San in Rat Plasma by UHPLC-MS/MS: Application to a Comparative Pharmacokinetic Study in Normal and Two Models of Ulcerative Colitis Rats | Simultaneous Determination of Ten Bioactive Components from Shenling Baizhu San in Rat Plasma by UHPLC-MS/MS: Application to a Comparative Pharmacokinetic Study in Normal and Two Models of Ulcerative Colitis Rats Abstract Shenling Baizhu San, a traditional formula, has a long history of treating spleen asthenic diarrhe... |
PMC5072519 | core_pubmed_pmc | Use of ICS/LABA (extra-fine and non-extra-fine) in elderly asthmatics | Use of ICS/LABA (extra-fine and non-extra-fine) in elderly asthmatics Abstract Age represents an exclusion criterion in randomized clinical trials designed to test the efficacy and safety of inhaled drugs in asthma. As a consequence, data on efficacy and safety of inhaled corticosteroid (ICS) and long-acting β2 agonist... |
PMC5573917 | core_pubmed_pmc | Modeling Pharmacokinetic Profiles of Insulin Regimens to Enhance Understanding of Subcutaneous Insulin Regimens | Modeling Pharmacokinetic Profiles of Insulin Regimens to Enhance Understanding of Subcutaneous Insulin Regimens Abstract Abstract Insulin pharmacokinetics following subcutaneous administration were modeled, simulated, and displayed through an interactive and user‐friendly interface to illustrate the time course of admi... |
PMC5813203 | core_pubmed_pmc | Single‐dose euglycaemic clamp studies demonstrating pharmacokinetic and pharmacodynamic similarity between MK‐1293 insulin glargine and originator insulin glargine (Lantus) in subjects with type 1 diabetes and healthy subjects | Single‐dose euglycaemic clamp studies demonstrating pharmacokinetic and pharmacodynamic similarity between MK‐1293 insulin glargine and originator insulin glargine (Lantus) in subjects with type 1 diabetes and healthy subjects Abstract Abstract Aims MK‐1293 is an insulin glargine that has an amino acid sequence identic... |
PMC9226319 | core_pubmed_pmc | Peripherally restricted transthyretin-based delivery system for probes and therapeutics avoiding opioid-related side effects | Peripherally restricted transthyretin-based delivery system for probes and therapeutics avoiding opioid-related side effects Abstract Several investigations into the sites of action of opioid analgesics have utilized peripherally acting mu-opioid receptor antagonists (PAMORAs), which have been incorrectly assumed to po... |
PMC6448326 | core_pubmed_pmc | Severe Hypocalcemia and Dramatic Increase in Parathyroid Hormone after Denosumab in a Dialysis Patient: A Case Report and Review of the Literature | Severe Hypocalcemia and Dramatic Increase in Parathyroid Hormone after Denosumab in a Dialysis Patient: A Case Report and Review of the Literature Abstract Abstract Chronic kidney disease-mineral and bone disorder (CKD-MBD) is frequently present in advanced stages of chronic kidney disease (CKD) patients with high risk... |
PMC9524735 | core_pubmed_pmc | Characterizing Absorption Properties of Dispersible Pretomanid Tablets Using Population Pharmacokinetic Modelling | Characterizing Absorption Properties of Dispersible Pretomanid Tablets Using Population Pharmacokinetic Modelling Abstract Abstract Background and Introduction The dispersible tablet formulation (DTF) of pretomanid has been developed to facilitate future use in children. This work aimed to assess the pharmacokinetics (... |
PMC7405733 | core_pubmed_pmc | Pharmacokinetics of micafungin in patients treated with extracorporeal membrane oxygenation: an observational prospective study | Pharmacokinetics of micafungin in patients treated with extracorporeal membrane oxygenation: an observational prospective study Abstract Abstract Objective To determine micafungin plasma levels and pharmacokinetic behavior in patients treated with extracorporeal membrane oxygenation. Methods The samples were taken thro... |
PMC12628970 | core_pubmed_pmc | Cannabidiol in pancreatic ductal adenocarcinoma: preclinical evidence, molecular mechanisms, and translational challenges | Cannabidiol in pancreatic ductal adenocarcinoma: preclinical evidence, molecular mechanisms, and translational challenges Abstract Background Pancreatic ductal adenocarcinoma (PDAC) remains one of the deadliest and most treatment-resistant cancers, with limited progress in improving patient survival. Cannabidiol (CBD),... |
PMC7851634 | core_pubmed_pmc | Treatment of Community-Acquired Pneumonia: A Focus on Lefamulin | Treatment of Community-Acquired Pneumonia: A Focus on Lefamulin Abstract Abstract Objective The goal of this article is to review the clinical pharmacology, pharmacokinetics, efficacy, and safety of lemafulin. Data Sources We performed a systematic literature review using the search terms of lefamulin and BC-3781 in th... |
PMC6267684 | core_pubmed_pmc | Pharmacokinetic evaluation of the PNC disassembler metarrestin in wild-type and Pdx1-Cre;LSL-Kras G12D/+ ;Tp53 R172H/+ (KPC) mice, a genetically engineered model of pancreatic cancer | Pharmacokinetic evaluation of the PNC disassembler metarrestin in wild-type and Pdx1-Cre;LSL-Kras G12D/+ ;Tp53 R172H/+ (KPC) mice, a genetically engineered model of pancreatic cancer Abstract Purpose Metarrestin is a first-in-class small molecule clinical candidate capable of disrupting the perinucleolar compartment, a... |
PMC8763688 | core_pubmed_pmc | Use of Physiologically-Based Kinetics Modelling to Reliably Predict Internal Concentrations of the UV Filter, Homosalate, After Repeated Oral and Topical Application | Use of Physiologically-Based Kinetics Modelling to Reliably Predict Internal Concentrations of the UV Filter, Homosalate, After Repeated Oral and Topical Application Abstract Abstract Ethical and legal considerations have led to increased use of non-animal methods to evaluate the safety of chemicals for human use. We d... |
PMC11845643 | core_pubmed_pmc | Development and evaluation of Hsp90-targeting nanobodies for visualisation of extracellular Hsp90 in tumours using PET imaging | Development and evaluation of Hsp90-targeting nanobodies for visualisation of extracellular Hsp90 in tumours using PET imaging Abstract Background The extracellular localisation of the Heat shock protein 90 (Hsp90) is associated with the diseased state and wound healing and presents a promising opportunity for cancer t... |
PMC5071694 | core_pubmed_pmc | PD‐1 Pathway Inhibitors: Immuno‐Oncology Agents for Restoring Antitumor Immune Responses | PD‐1 Pathway Inhibitors: Immuno‐Oncology Agents for Restoring Antitumor Immune Responses Abstract Immune checkpoint inhibitors are designed to restore a patient's own antitumor immune response that has been suppressed during tumor development. The first monoclonal antibodies against the immune checkpoint programmed dea... |
PMC11619387 | core_pubmed_pmc | Interspecies interactions alter the antibiotic sensitivity of Pseudomonas aeruginosa | Interspecies interactions alter the antibiotic sensitivity of Pseudomonas aeruginosa Abstract ABSTRACT Polymicrobial infections are infections that are caused by multiple pathogens and are common in patients with cystic fibrosis (CF). Although polymicrobial infections are associated with poor treatment responses in CF,... |
PMC8468023 | core_pubmed_pmc | Comparison of the Intestinal Pharmacokinetics of Two Different Florfenicol Dosing Regimens and Its Impact on the Prevalence and Phenotypic Resistance of E. coli and Enterococcus over Time | Comparison of the Intestinal Pharmacokinetics of Two Different Florfenicol Dosing Regimens and Its Impact on the Prevalence and Phenotypic Resistance of E. coli and Enterococcus over Time Abstract In order to mitigate the food animal sector’s role in the growing threat of antimicrobial resistance (AMR), the World Healt... |
PMC5500545 | core_pubmed_pmc | Prediction of efficacy for conversion from adjunctive therapy to monotherapy with eslicarbazepine acetate 800 mg once daily for partial-onset epilepsy | Prediction of efficacy for conversion from adjunctive therapy to monotherapy with eslicarbazepine acetate 800 mg once daily for partial-onset epilepsy Abstract Purpose Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED) indicated for partial-onset seizures (POS). Clinical studies of gradual... |
PMC7665884 | core_pubmed_pmc | Population-based meta-analysis of chloroquine: informing chloroquine pharmacokinetics in COVID-19 patients | Population-based meta-analysis of chloroquine: informing chloroquine pharmacokinetics in COVID-19 patients Abstract Aims Chloroquine (CQ) has been repurposed to treat coronavirus disease 2019 (COVID-19). Understanding the pharmacokinetics (PK) in COVID-19 patients is essential to study its exposure–efficacy/safety rela... |
PMC3899471 | core_pubmed_pmc | Randomized, Double-Blind, Placebo-Controlled, Crossover Study of the Effects of Lisdexamfetamine Dimesylate and Mixed Amphetamine Salts on Cognition Throughout the Day in Adults with Attention-Deficit/Hyperactivity Disorder | Randomized, Double-Blind, Placebo-Controlled, Crossover Study of the Effects of Lisdexamfetamine Dimesylate and Mixed Amphetamine Salts on Cognition Throughout the Day in Adults with Attention-Deficit/Hyperactivity Disorder Abstract Abstract Background Understanding the nature and time course of the pharmacodynamic eff... |
PMC5054555 | core_pubmed_pmc | Fundamentals of aerosol therapy in critical care | Fundamentals of aerosol therapy in critical care Abstract Abstract Drug dosing in critically ill patients is challenging due to the altered drug pharmacokinetics–pharmacodynamics associated with systemic therapies. For many drug therapies, there is potential to use the respiratory system as an alternative route for dru... |
PMC11149982 | core_pubmed_pmc | Cellular pharmacokinetic of methotrexate and its modulation by folylpolyglutamate synthetase and γ-glutamyl hydrolase in tumor cells | Cellular pharmacokinetic of methotrexate and its modulation by folylpolyglutamate synthetase and γ-glutamyl hydrolase in tumor cells Abstract Background and purpose Clinical studies showed that prolonged infusion of methotrexate (MTX) leads to more severe adverse reactions than short infusion of MTX at the same dose. W... |
PMC5899915 | core_pubmed_pmc | An exploratory clinical study of p38 α kinase inhibition in Alzheimer's disease | An exploratory clinical study of p38 α kinase inhibition in Alzheimer's disease Abstract Abstract Objective The aim of this study was to preliminarily evaluate an oral small molecule p38 α kinase inhibitor in patients with early Alzheimer's disease ( AD ) for the effects on brain amyloid plaque load and episodic memory... |
PMC9671979 | core_pubmed_pmc | Respiratory effects of oral mitragynine and oxycodone in a rodent model | Respiratory effects of oral mitragynine and oxycodone in a rodent model Abstract Abstract Rationale Kratom derives from Mitragyna speciosa (Korth.), a tropical tree in the genus Mitragyna (Rubiaceae) that also includes the coffee tree. Kratom leaf powders, tea-like decoctions, and commercial extracts are taken orally, ... |
PMC4859549 | core_pubmed_pmc | Pharmacokinetic Study of Praziquantel Enantiomers and Its Main Metabolite R-trans -4-OH-PZQ in Plasma, Blood and Dried Blood Spots in Opisthorchis viverrini -Infected Patients | Pharmacokinetic Study of Praziquantel Enantiomers and Its Main Metabolite R-trans -4-OH-PZQ in Plasma, Blood and Dried Blood Spots in Opisthorchis viverrini -Infected Patients Abstract Background Praziquantel (PZQ) is the treatment of choice for infections with the liver fluke Opisthorchis viverrini , a major health pr... |
PMC10123480 | core_pubmed_pmc | Role of Cytochrome P450 2C9 in COVID-19 Treatment: Current Status and Future Directions | Role of Cytochrome P450 2C9 in COVID-19 Treatment: Current Status and Future Directions Abstract Abstract The major human liver drug metabolising cytochrome P450 (CYP) enzymes are downregulated during inflammation and infectious disease state, especially during coronavirus disease 2019 (COVID-19) infection. The influx ... |
PMC3497871 | core_pubmed_pmc | Scale up, optimization and stability analysis of Curcumin C3 complex-loaded nanoparticles for cancer therapy | Scale up, optimization and stability analysis of Curcumin C3 complex-loaded nanoparticles for cancer therapy Abstract Background Nanoparticle based delivery of anticancer drugs have been widely investigated. However, a very important process for Research & Development in any pharmaceutical industry is scaling nanoparti... |
PMC7819280 | core_pubmed_pmc | Dobutamine Alters the Pharmacokinetic and Pharmacodynamic Behavior of Esmolol | Dobutamine Alters the Pharmacokinetic and Pharmacodynamic Behavior of Esmolol Abstract Background and objective This study involved an investigation into the pharmacokinetic and pharmacodynamic behavior of esmolol in the presence of dobutamine in healthy subjects of European ancestry. Methods We conducted a single-cent... |
PMC6094896 | core_pubmed_pmc | A comparative clinical study of PF-06410293, a candidate adalimumab biosimilar, and adalimumab reference product (Humira®) in the treatment of active rheumatoid arthritis | A comparative clinical study of PF-06410293, a candidate adalimumab biosimilar, and adalimumab reference product (Humira®) in the treatment of active rheumatoid arthritis Abstract Background This double-blind, randomized, 78-week study evaluated the efficacy, safety, immunogenicity, pharmacokinetics, and pharmacodynami... |
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