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PMC8105776
core_pubmed_pmc
Exploration and insights into the cellular internalization and intracellular fate of amphiphilic polymeric nanocarriers
Exploration and insights into the cellular internalization and intracellular fate of amphiphilic polymeric nanocarriers Abstract The beneficial or deleterious effects of nanomedicines emerge from their complex interactions with intracellular pathways and their subcellular fate. Moreover, the dynamic nature of plasma me...
PMC5642319
core_pubmed_pmc
SYSTEMIC PHARMACOKINETICS AND PHARMACODYNAMICS OF INTRAVITREAL AFLIBERCEPT, BEVACIZUMAB, AND RANIBIZUMAB
SYSTEMIC PHARMACOKINETICS AND PHARMACODYNAMICS OF INTRAVITREAL AFLIBERCEPT, BEVACIZUMAB, AND RANIBIZUMAB Abstract After monthly intravitreal injections, the systemic exposures of aflibercept, bevacizumab, and ranibizumab were distinct and correlated with different reductions in plasma free–vascular endothelial growth f...
PMC7395075
core_pubmed_pmc
Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors
Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors Abstract UDP-glucuronosyltransferases (UGTs) are involved in phase II conjugation reactions of xenobiotics and differences in their isoform activities result in interindividua...
PMC8400310
core_pubmed_pmc
Modelling Tools to Characterize Acetaminophen Pharmacokinetics in the Pregnant Population
Modelling Tools to Characterize Acetaminophen Pharmacokinetics in the Pregnant Population Abstract This review describes acetaminophen pharmacokinetics (PK) throughout pregnancy, as analyzed by three methods (non-compartmental analyses (NCA), population PK, and physiologically based PK (PBPK) modelling). Eighteen studi...
PMC3682086
core_pubmed_pmc
Effects of Fluvastatin on the Pharmacokinetics of Repaglinide: Possible Role of CYP3A4 and P-glycoprotein Inhibition by Fluvastatin
Effects of Fluvastatin on the Pharmacokinetics of Repaglinide: Possible Role of CYP3A4 and P-glycoprotein Inhibition by Fluvastatin Abstract The purpose of this study was to investigate the effects of fluvastatin on the pharmacokinetics of repaglinide in rats. The effect of fluvastatin on P-glycoprotein and CYP3A4 acti...
PMC5610524
core_pubmed_pmc
Tools for the Individualized Therapy of Teicoplanin for Neonates and Children
Tools for the Individualized Therapy of Teicoplanin for Neonates and Children Abstract ABSTRACT The aim of this study was to develop a population pharmacokinetic (PK) model for teicoplanin across childhood age ranges to be used as Bayesian prior information in the software constructed for individualized therapy. We dev...
PMC7383507
core_pubmed_pmc
A glycosylated Fc ‐fused glucagon‐like peptide‐1 receptor agonist exhibits equivalent glucose lowering to but fewer gastrointestinal side effects than dulaglutide
A glycosylated Fc ‐fused glucagon‐like peptide‐1 receptor agonist exhibits equivalent glucose lowering to but fewer gastrointestinal side effects than dulaglutide Abstract Abstract Aim To evaluate the pharmacokinetic and pharmacodynamic properties of a novel glycosylated Fc‐fused glucagon‐like peptide‐1(GLP‐1‐gFc) rece...
PMC4191077
core_pubmed_pmc
Modeling hemoglobin and hemoglobin:haptoglobin complex clearance in a non-rodent species–pharmacokinetic and therapeutic implications
Modeling hemoglobin and hemoglobin:haptoglobin complex clearance in a non-rodent species–pharmacokinetic and therapeutic implications Abstract Background: Haptoglobin (Hp) prevents hemoglobin (Hb) extravasation and attenuates Hb induced tissue oxidation and vasoconstriction. Small animal models such as mouse, rat and g...
PMC6055049
core_pubmed_pmc
Nanotherapeutics for Treatment of Pulmonary Arterial Hypertension
Nanotherapeutics for Treatment of Pulmonary Arterial Hypertension Abstract Abstract Pulmonary arterial hypertension (PAH) is a devastating and fatal chronic lung disease. While current pharmacotherapies have improved patient quality of life, PAH drugs suffer from limitations in the form of short-term pharmacokinetics, ...
PMC4017092
core_pubmed_pmc
Multiscale Design of Cell-Type–Specific Pharmacokinetic/Pharmacodynamic Models for Personalized Medicine: Application to Temozolomide in Brain Tumors
Multiscale Design of Cell-Type–Specific Pharmacokinetic/Pharmacodynamic Models for Personalized Medicine: Application to Temozolomide in Brain Tumors Abstract Optimizing anticancer therapeutics needs to account for variable drug responses in heterogeneous cell populations within the tumor as well as in organs of toxici...
PMC6640706
core_pubmed_pmc
Pharmacologic Considerations in the Disposition of Antibodies and Antibody-Drug Conjugates in Preclinical Models and in Patients
Pharmacologic Considerations in the Disposition of Antibodies and Antibody-Drug Conjugates in Preclinical Models and in Patients Abstract Abstract The rapid advancement in the development of therapeutic proteins, including monoclonal antibodies (mAbs) and antibody-drug conjugates (ADCs), has created a novel mechanism t...
PMC11409195
core_pubmed_pmc
Bioavailability of a novel sustained‐release pellet formulation of 5‐flucytosine in healthy‐fed participants for use in patients with cryptococcal meningitis
Bioavailability of a novel sustained‐release pellet formulation of 5‐flucytosine in healthy‐fed participants for use in patients with cryptococcal meningitis Abstract Abstract Cryptococcal meningoencephalitis (CM) is an opportunistic fungal infection and a major cause of death among people living with human immunodefic...
PMC7187372
core_pubmed_pmc
Population Pharmacokinetics of Glasdegib in Patients With Advanced Hematologic Malignancies and Solid Tumors
Population Pharmacokinetics of Glasdegib in Patients With Advanced Hematologic Malignancies and Solid Tumors Abstract Abstract Glasdegib is an inhibitor of the Hedgehog pathway recently approved in the United States for the treatment of acute myeloid leukemia. A population pharmacokinetic analysis was conducted to char...
PMC11518658
core_pubmed_pmc
Perinatal Caffeine Administration Improves Outcomes in an Ovine Model of Neonatal Hypoxia-Ischemia
Perinatal Caffeine Administration Improves Outcomes in an Ovine Model of Neonatal Hypoxia-Ischemia Abstract BACKGROUND: Neonatal hypoxic-ischemic encephalopathy disproportionately affects low- and middle-income countries, where ≈96% of affected infants reside. The current standard of care, therapeutic hypothermia, is f...
PMC6600547
core_pubmed_pmc
Insight of the Interaction between 2,4-thiazolidinedione and Human Serum Albumin: A Spectroscopic, Thermodynamic and Molecular Docking Study
Insight of the Interaction between 2,4-thiazolidinedione and Human Serum Albumin: A Spectroscopic, Thermodynamic and Molecular Docking Study Abstract Abstract Thiazolidinedione derivatives (TZDs) have attracted attention because of their pharmacological effects. For example, certain TZDs have been reported to ameliorat...
PMC9756848
core_pubmed_pmc
Kinetics of free and ligand-bound atacicept in human serum
Kinetics of free and ligand-bound atacicept in human serum Abstract Abstract BAFF (B cell activation factor of the TNF family/B lymphocyte stimulator, BLyS) and APRIL (a proliferation-inducing ligand) are targeted by atacicept, a decoy receptor consisting of the extracellular domain of TACI (transmembrane activator and...
PMC8944443
core_pubmed_pmc
Rational Use of Danofloxacin for Treatment of Mycoplasma gallisepticum in Chickens Based on the Clinical Breakpoint and Lung Microbiota Shift
Rational Use of Danofloxacin for Treatment of Mycoplasma gallisepticum in Chickens Based on the Clinical Breakpoint and Lung Microbiota Shift Abstract The study was to explore the rational use of danofloxacin against Mycoplasma gallisepticum ( MG ) based on its clinical breakpoint (CBP) and the effect on lung microbiot...
PMC8429641
core_pubmed_pmc
Optimal single sampling time-point for monitoring of praziquantel exposure in children
Optimal single sampling time-point for monitoring of praziquantel exposure in children Abstract Praziquantel pharmacokinetics studies in schistosomiasis infected children are scarce partly due to the challenges/complexity of intensive blood sampling in the target population. This study was aimed to investigate the opti...
PMC7428791
core_pubmed_pmc
Pharmacogenetics of immunosuppressant drugs: A new aspect for individualized therapy
Pharmacogenetics of immunosuppressant drugs: A new aspect for individualized therapy Abstract Abstract In recent years, pharmacogenetics has emerged as an important tool for choosing the right immunosuppressant drug and its appropriate dose. Indeed, pharmacogenetics may exert its action on immunosuppressant drugs at th...
PMC4578755
core_pubmed_pmc
Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery
Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery Abstract Background Proteins that ‘read’ the histone code are central elements in epigenetic control and bromodomains, which bind acetyl-lysine motifs, are increasingly recognized as potential mediators of dis...
PMC6540510
core_pubmed_pmc
Pharmacokinetic interaction of riociguat and antiretroviral combination regimens in HIV-1-infected adults
Pharmacokinetic interaction of riociguat and antiretroviral combination regimens in HIV-1-infected adults Abstract Abstract Riociguat, a first-in-class soluble guanylate cyclase stimulator, is approved for the treatment of pulmonary arterial hypertension (PAH), a serious potential complication of human immunodeficiency...
PMC10971044
core_pubmed_pmc
Polycarbonate-Based Copolymer Micelles as Biodegradable Carriers of Anticancer Podophyllotoxin or Juniper Extracts
Polycarbonate-Based Copolymer Micelles as Biodegradable Carriers of Anticancer Podophyllotoxin or Juniper Extracts Abstract Podophyllotoxin (PPT) is used in the industrial production of efficient anticancer, antiviral and other drugs. Sinopodophyllum hexandrum or Podophyllum peltatum are natural sources of PPT, but at ...
PMC5306109
core_pubmed_pmc
Model-based contextualization of in vitro toxicity data quantitatively predicts in vivo drug response in patients
Model-based contextualization of in vitro toxicity data quantitatively predicts in vivo drug response in patients Abstract Understanding central mechanisms underlying drug-induced toxicity plays a crucial role in drug development and drug safety. However, a translation of cellular in vitro findings to an actual in vivo...
PMC6113196
core_pubmed_pmc
Leveraging PET to image folate receptor α therapy of an antibody-drug conjugate
Leveraging PET to image folate receptor α therapy of an antibody-drug conjugate Abstract Abstract Background The folate receptor α (FRα)-targeting antibody-drug conjugate (ADC), IMGN853, shows great antitumor activity against FRα-expressing tumors in vivo, but patient selection and consequently therapy outcome are base...
PMC12829857
core_pubmed_pmc
Association between multi-metal co-exposure and thyroid cancer risk in Shanxi, China: A case-control study
Association between multi-metal co-exposure and thyroid cancer risk in Shanxi, China: A case-control study Abstract Abstract Environmental metals are established thyroid carcinogens, yet how their co-exposure collectively reshapes carcinogenic mechanisms remains elusive. This study used ICP-MS to quantify plasma concen...
PMC9854650
core_pubmed_pmc
Development of a Predictive Dosing Nomogram to Achieve PK/PD Targets of Amikacin Initial Dose in Critically Ill Patients: A Non-Parametric Approach
Development of a Predictive Dosing Nomogram to Achieve PK/PD Targets of Amikacin Initial Dose in Critically Ill Patients: A Non-Parametric Approach Abstract Abstract French guidelines recommend reaching an amikacin concentration of ≥8 × MIC 1 h after beginning infusion (C 1h ), with MIC = 8 mg/L for probabilistic thera...
PMC7589296
core_pubmed_pmc
Injectables and Depots to Prolong Drug Action of Proteins and Peptides
Injectables and Depots to Prolong Drug Action of Proteins and Peptides Abstract Abstract Proteins and peptides have emerged in recent years to treat a wide range of multifaceted diseases such as cancer, diabetes and inflammation. The emergence of polypeptides has yielded advancements in the fields of biopharmaceutical ...
PMC7176801
core_pubmed_pmc
Acute-on-chronic liver failure alters meropenem pharmacokinetics in critically ill patients with continuous hemodialysis: an observational study
Acute-on-chronic liver failure alters meropenem pharmacokinetics in critically ill patients with continuous hemodialysis: an observational study Abstract Background Infection and sepsis are a main cause of acute-on-chronic liver failure (ACLF). Adequate dosing of antimicrobial therapy is of central importance to improv...
PMC3734602
core_pubmed_pmc
Modeling and Validating Chronic Pharmacological Manipulation of Circadian Rhythms
Modeling and Validating Chronic Pharmacological Manipulation of Circadian Rhythms Abstract Circadian rhythms can be entrained by a light-dark (LD) cycle and can also be reset pharmacologically, for example, by the CK1δ/ε inhibitor PF-670462. Here, we determine how these two independent signals affect circadian timekeep...
PMC12564310
core_pubmed_pmc
Natural and Synthetic Compounds Against Colorectal Cancer: An Update of Preclinical Studies in Saudi Arabia
Natural and Synthetic Compounds Against Colorectal Cancer: An Update of Preclinical Studies in Saudi Arabia Abstract Simple Summary Colorectal cancer is one of the most common and deadly cancers worldwide, and its cases are rising in Saudi Arabia, especially among younger people. Scientists are now exploring new ways t...
PMC5814509
core_pubmed_pmc
A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients
A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients Abstract Background and Objectives Abemaciclib, a dual inhibitor of cyclin-dependent kinases 4 and 6, has demonstrated clinical activity in a number of different cancer types. The objectives of this s...
PMC8746890
core_pubmed_pmc
Therapeutic Drug Monitoring of Ganciclovir: Where Are We?
Therapeutic Drug Monitoring of Ganciclovir: Where Are We? Abstract Background: Ganciclovir is the mainstay of therapy for the prophylaxis and treatment of Cytomegalovirus . However, therapy with this antiviral agent is hindered by side effects such as myelosuppression, which often leads to therapy cessation. Underdosin...
PMC10056953
core_pubmed_pmc
Intragastric Carbon Dioxide Release Prolongs the Gastric Residence Time of Postprandially Administered Caffeine
Intragastric Carbon Dioxide Release Prolongs the Gastric Residence Time of Postprandially Administered Caffeine Abstract Abstract Sparkling water is said to increase gastric motility by the release of carbon dioxide, thereby potentially affecting the pharmacokinetics of orally administered drugs. The hypothesis of the ...
PMC5980569
core_pubmed_pmc
Comparison of Power, Prognosis, and Extrapolation Properties of Four Population Pharmacodynamic Models of HbA1c for Type 2 Diabetes
Comparison of Power, Prognosis, and Extrapolation Properties of Four Population Pharmacodynamic Models of HbA1c for Type 2 Diabetes Abstract Reusing published models saves time; time to be used for informing decisions in drug development. In antihyperglycemic drug development, several published HbA1c models are availab...
PMC12673054
core_pubmed_pmc
Delayed Dexamethasone Absorption from Gluteal Abscesses: Persistent Iatrogenic Cushing Syndrome
Delayed Dexamethasone Absorption from Gluteal Abscesses: Persistent Iatrogenic Cushing Syndrome Abstract Iatrogenic Cushing syndrome can occur due to the use of external glucocorticoids. We present a case involving prolonged exposure to glucocorticoids from intramuscular dexamethasone injections, with diagnosis confirm...
PMC12049946
core_pubmed_pmc
Tissue distribution pharmacokinetics of intrathecal U1 adaptor oligonucleotide in mice
Tissue distribution pharmacokinetics of intrathecal U1 adaptor oligonucleotide in mice Abstract Abstract U1 Adaptor is a novel gene-silencing technology, offering an innovative approach to target genes in the CNS for the treatment of diseases. Intrathecal delivery is a medically viable route of administration of CNS-bo...
PMC2871167
core_pubmed_pmc
Adding insulin glargine vs. NPH insulin to metformin results in a more efficient postprandial β -cell protection in individuals with type 2 diabetes
Adding insulin glargine vs. NPH insulin to metformin results in a more efficient postprandial β -cell protection in individuals with type 2 diabetes Abstract Abstract Aim: Postprandial release of intact proinsulin (IP) is an independent marker for β -cell dysfunction in patients with type 2 diabetes. This open-label, p...
PMC6832671
core_pubmed_pmc
Transgender women on oral HIV pre‐exposure prophylaxis have significantly lower tenofovir and emtricitabine concentrations when also taking oestrogen when compared to cisgender men
Transgender women on oral HIV pre‐exposure prophylaxis have significantly lower tenofovir and emtricitabine concentrations when also taking oestrogen when compared to cisgender men Abstract Abstract Introduction Oral HIV Pre‐Exposure Prophylaxis (PrEP) with tenofovir (TFV) disoproxil fumarate (TDF)/emtricitabine (FTC) ...
PMC6152436
core_pubmed_pmc
Comparison of biosimilar CT-P10 and innovator rituximab in patients with rheumatoid arthritis: a randomized controlled Phase 3 trial
Comparison of biosimilar CT-P10 and innovator rituximab in patients with rheumatoid arthritis: a randomized controlled Phase 3 trial Abstract ABSTRACT This multinational, randomized, double-blind trial, (ClinicalTrials.gov identifier NCT02149121 ) was designed to demonstrate equivalence in pharmacokinetics and efficacy...
PMC12735298
core_pubmed_pmc
NNZ-2591 in Children and Adolescents With Phelan-McDermid Syndrome
NNZ-2591 in Children and Adolescents With Phelan-McDermid Syndrome Abstract Background and Objectives Phelan-McDermid syndrome (PMS) is a rare genetic neurodevelopmental disorder with no currently approved treatments. NNZ-2591, a synthetic analog of the insulin-like growth factor 1 metabolite cyclic glycine-proline, wa...
PMC5546766
core_pubmed_pmc
In vitro and in vivo evaluation of SN-38 nanocrystals with different particle sizes
In vitro and in vivo evaluation of SN-38 nanocrystals with different particle sizes Abstract 7-Ethyl-10-hydroxycamptothecin (SN-38) is a potent broad-spectrum antitumor drug derived from irinotecan hydrochloride (CPT-11). Due to its poor solubility and instability of the active lactone ring, its clinical use is signifi...
PMC9406097
core_pubmed_pmc
3-Chloro-3-methyl-2,6-diarylpiperidin-4-ones as Anti-Cancer Agents: Synthesis, Biological Evaluation, Molecular Docking, and In Silico ADMET Prediction
3-Chloro-3-methyl-2,6-diarylpiperidin-4-ones as Anti-Cancer Agents: Synthesis, Biological Evaluation, Molecular Docking, and In Silico ADMET Prediction Abstract Piperidine pharmacophore-containing compounds have demonstrated therapeutic efficacy against a range of diseases and are now being investigated in cancer. A se...
PMC2938266
core_pubmed_pmc
Phase I trial of CYT997, a novel cytotoxic and vascular-disrupting agent
Phase I trial of CYT997, a novel cytotoxic and vascular-disrupting agent Abstract Abstract Background: CYT997 is a novel microtubule inhibitor and vascular-disrupting agent with marked preclinical anti-tumour activity. Methods: This phase I dose-escalation study assessed the safety, tolerability, pharmacokinetics and p...
PMC6190795
core_pubmed_pmc
Population Pharmacokinetic Study of Cefazolin Used Prophylactically in Canine Surgery for Susceptibility Testing Breakpoint Determination
Population Pharmacokinetic Study of Cefazolin Used Prophylactically in Canine Surgery for Susceptibility Testing Breakpoint Determination Abstract This study aimed to determine the population pharmacokinetic (Pop PK) parameters of cefazolin administered prophylactically at 25 mg/kg intravenously (IV) 30 min before surg...
PMC11711049
core_pubmed_pmc
Tasurgratinib in patients with cholangiocarcinoma or gastric cancer: Expansion part of the first‐in‐human phase I study
Tasurgratinib in patients with cholangiocarcinoma or gastric cancer: Expansion part of the first‐in‐human phase I study Abstract Abstract Fibroblast growth factor receptors (FGFRs) are a highly conserved family of transmembrane receptor tyrosine kinases with multiple roles in the regulation of key cellular processes. S...
PMC6133078
core_pubmed_pmc
Determination of Puquitinib in Human Plasma by HPLC–ESI MS/MS: Application to Pharmacokinetic Study
Determination of Puquitinib in Human Plasma by HPLC–ESI MS/MS: Application to Pharmacokinetic Study Abstract Abstract Background and Objective Puquitinib mesylate (XC-302) is a new multiple-target anticancer inhibitor, which directly suppresses the activity of phosphatidylinositol 3-kinase (PI3K). This study was aimed ...
PMC10781094
core_pubmed_pmc
Thymol-Modified Oleic and Linoleic Acids Encapsulated in Polymeric Nanoparticles: Enhanced Bioactivity, Stability, and Biomedical Potential
Thymol-Modified Oleic and Linoleic Acids Encapsulated in Polymeric Nanoparticles: Enhanced Bioactivity, Stability, and Biomedical Potential Abstract Abstract Unsaturated fatty acids, such as oleic acid (OA) and linoleic acid (LA), are promising antimicrobial and cytostatic agents. We modified OA and LA with thymol (TOA...
PMC12189049
core_pubmed_pmc
Development of a System to Deliver Inhalational Antibiotics to Marmosets
Development of a System to Deliver Inhalational Antibiotics to Marmosets Abstract Abstract Background: Inhalational antibiotics have been used effectively to treat chronic diseases such as Pseudomonas aeruginosa infections associated with cystic fibrosis. This approach may enhance treatment options for difficult-to-tre...
PMC9986061
core_pubmed_pmc
Cusatuzumab plus azacitidine in Japanese patients with newly diagnosed acute myeloid leukemia ineligible for intensive treatment
Cusatuzumab plus azacitidine in Japanese patients with newly diagnosed acute myeloid leukemia ineligible for intensive treatment Abstract Abstract We present the results of a phase 1 study that evaluated the safety, pharmacokinetics, pharmacodynamics, immunogenicity, and preliminary disease response to cusatuzumab, a n...
PMC11935455
core_pubmed_pmc
Anticoagulation Management During ECMO: Narrative Review
Anticoagulation Management During ECMO: Narrative Review Abstract Extracorporeal membrane oxygenation (ECMO) is a critical intervention for patients with severe respiratory or cardiac failure, requiring careful management of anticoagulation to prevent thromboembolic complications. This review examines current practices...
PMC4809624
core_pubmed_pmc
Approaching Pharmacometrics as a Paleontologist Would: Recovering the Links Between Drugs and the Body Through Reconstruction
Approaching Pharmacometrics as a Paleontologist Would: Recovering the Links Between Drugs and the Body Through Reconstruction Abstract Abstract Our knowledge of dinosaurs comes primarily from the fossil record. Notwithstanding the condition of these vestiges, paleontologists reconstruct early reptilian life by comparis...
PMC6936809
core_pubmed_pmc
Potentially inappropriate medication in older participants of the Berlin Aging Study II (BASE-II) – Sex differences and associations with morbidity and medication use
Potentially inappropriate medication in older participants of the Berlin Aging Study II (BASE-II) – Sex differences and associations with morbidity and medication use Abstract Introduction Multimorbidity in advanced age and the need for drug treatment may lead to polypharmacy, while pharmacokinetic and pharmacodynamic ...
PMC11705982
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Two Fixed-Dose Combination Tablets of Valsartan/Amlodipine (80/5 Mg) in Healthy Chinese Subjects
Pharmacokinetics and Bioequivalence of Two Fixed-Dose Combination Tablets of Valsartan/Amlodipine (80/5 Mg) in Healthy Chinese Subjects Abstract Purpose The study aimed to investigate the pharmacokinetics and bioequivalence of coformulations of valsartan and amlodipine in healthy Chinese subjects under both fasting and...
PMC3673986
core_pubmed_pmc
A Sensitive and Selective Liquid Chromatography/Tandem Mass Spectrometry Method for Quantitative Analysis of Efavirenz in Human Plasma
A Sensitive and Selective Liquid Chromatography/Tandem Mass Spectrometry Method for Quantitative Analysis of Efavirenz in Human Plasma Abstract A selective and a highly sensitive method for the determination of the non-nucleoside reverse transcriptase inhibitor (NNRTI), efavirenz, in human plasma has been developed and...
PMC9245059
core_pubmed_pmc
Optimal target saturation of ligand-blocking anti-GITR antibody IBI37G5 dictates FcγR-independent GITR agonism and antitumor activity
Optimal target saturation of ligand-blocking anti-GITR antibody IBI37G5 dictates FcγR-independent GITR agonism and antitumor activity Abstract Summary Glucocorticoid-induced tumor necrosis factor receptor (GITR) is a co-stimulatory receptor and an important target for cancer immunotherapy. We herein present a potent Fc...
PMC3350959
core_pubmed_pmc
Influence of Fructooligosaccharide on Pharmacokinetics of Isoflavones in Postmenopausal Women
Influence of Fructooligosaccharide on Pharmacokinetics of Isoflavones in Postmenopausal Women Abstract The objective of the present paper was to determine the influence of fructooligosaccharide (FOS) on the pharmacokinetics of isoflavones in healthy postmenopausal women. The study was a fixed-sequence, two-phase, cross...
PMC7997865
core_pubmed_pmc
Synergistic Antitumor Efficacy Mediated by Liposomal Co-Delivery of Polymeric Micelles of Vinorelbine and Cisplatin in Non-Small Cell Lung Cancer
Synergistic Antitumor Efficacy Mediated by Liposomal Co-Delivery of Polymeric Micelles of Vinorelbine and Cisplatin in Non-Small Cell Lung Cancer Abstract Purpose Non-small cell lung cancer (NSCLC) is an aggressive tumor with high mortality and poor prognosis. In this study, we designed a liposome encapsulating polymer...
PMC11457676
core_pubmed_pmc
Can capillary microsampling facilitate a clinical pharmacokinetics study of cefazolin in critically ill children?
Can capillary microsampling facilitate a clinical pharmacokinetics study of cefazolin in critically ill children? Abstract Aim: Pharmacokinetic studies in children are limited, in part due to challenges in blood sampling. We compare the use of capillary microsampling and conventional sampling techniques in pediatric pa...
PMC11360778
core_pubmed_pmc
Drug-Drug Interactions between COVID-19 and Tuberculosis Medications: A Comprehensive Review of CYP450 and Transporter-Mediated Effects
Drug-Drug Interactions between COVID-19 and Tuberculosis Medications: A Comprehensive Review of CYP450 and Transporter-Mediated Effects Abstract Abstract Most medications undergo metabolism and elimination via CYP450 enzymes, while uptake and efflux transporters play vital roles in drug elimination from various organs....
PMC10836378
core_pubmed_pmc
First exploration of the on-treatment changes in tumor and organ uptake of a radiolabeled anti PD-L1 antibody during chemoradiotherapy in patients with non-small cell lung cancer using whole body PET
First exploration of the on-treatment changes in tumor and organ uptake of a radiolabeled anti PD-L1 antibody during chemoradiotherapy in patients with non-small cell lung cancer using whole body PET Abstract Abstract Background In patients with locally advanced unresectable non-small cell lung cancer (NSCLC), durvalum...
PMC12574595
core_pubmed_pmc
PKPy: a Python-based framework for automated population pharmacokinetic analysis
PKPy: a Python-based framework for automated population pharmacokinetic analysis Abstract We present PKPy, an open-source Python framework designed to automate population pharmacokinetic analysis workflows. The framework emphasizes user accessibility by minimizing the need for manual parameter initialization while main...
PMC9959027
core_pubmed_pmc
The Parasite Reduction Ratio (PRR) Assay Version 2: Standardized Assessment of Plasmodium falciparum Viability after Antimalarial Treatment In Vitro
The Parasite Reduction Ratio (PRR) Assay Version 2: Standardized Assessment of Plasmodium falciparum Viability after Antimalarial Treatment In Vitro Abstract With artemisinin-resistant Plasmodium falciparum parasites emerging in Africa, the need for new antimalarial chemotypes is persistently high. The ideal pharmacody...
PMC7962107
core_pubmed_pmc
Structure-Based Virtual Screening Identifies Multiple Stable Binding Sites at the RecA Domains of SARS-CoV-2 Helicase Enzyme
Structure-Based Virtual Screening Identifies Multiple Stable Binding Sites at the RecA Domains of SARS-CoV-2 Helicase Enzyme Abstract Abstract With the emergence and global spread of the COVID-19 pandemic, the scientific community worldwide has focused on search for new therapeutic strategies against this disease. One ...
PMC12479645
core_pubmed_pmc
Role of Antidrug Antibodies in Oncolytic Viral Therapy: A Dynamic Modelling Approach in Cancer Patients Treated with V937 Alone or in Combination
Role of Antidrug Antibodies in Oncolytic Viral Therapy: A Dynamic Modelling Approach in Cancer Patients Treated with V937 Alone or in Combination Abstract Background and Objective Oncolytic viruses (OVs) are a growing immuno-oncology therapeutic class that rely on their capability to activate the dormant endogenous ant...
PMC8525095
core_pubmed_pmc
Urine volume to hydration volume ratio is associated with pharmacokinetics of high‐dose methotrexate in patients with primary central nervous system lymphoma
Urine volume to hydration volume ratio is associated with pharmacokinetics of high‐dose methotrexate in patients with primary central nervous system lymphoma Abstract Abstract High‐dose methotrexate (HD‐MTX)‐based chemotherapy is the first‐line treatment for primary central nervous system lymphoma (PCNSL), but is assoc...
PMC8229114
core_pubmed_pmc
Prolonged Infusion of β-Lactams Decreases Mortality in Patients with Septic Shock: A Retrospective before-and-after Study
Prolonged Infusion of β-Lactams Decreases Mortality in Patients with Septic Shock: A Retrospective before-and-after Study Abstract Abstract Septic shock substantially alters the pharmacokinetic properties of β-lactams with a subsequently high risk of insufficiently low serum concentrations and treatment failure. Consid...
PMC7825189
core_pubmed_pmc
Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug‐Drug Interactions Using Physiologically Based Pharmacokinetic Modeling
Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug‐Drug Interactions Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Levonorgestrel (LNG) is the active moiety in many hormonal contraceptive formulations. It is typically coformulated with ethinyl estradiol (EE) to decreas...
PMC10883629
core_pubmed_pmc
Prognostic Value of the Modeled Prostate-Specific Antigen KELIM Confirmation in Metastatic Castration-Resistant Prostate Cancer Treated With Taxanes in FIRSTANA
Prognostic Value of the Modeled Prostate-Specific Antigen KELIM Confirmation in Metastatic Castration-Resistant Prostate Cancer Treated With Taxanes in FIRSTANA Abstract PURPOSE In a previous exploratory study, modeled early longitudinal prostate-specific antigen (PSA) kinetics observed within the 100-first treatment d...
PMC8157623
core_pubmed_pmc
A phase 2 double-blind placebo-controlled 24-week treatment clinical study of the p38 alpha kinase inhibitor neflamapimod in mild Alzheimer’s disease
A phase 2 double-blind placebo-controlled 24-week treatment clinical study of the p38 alpha kinase inhibitor neflamapimod in mild Alzheimer’s disease Abstract Background In preclinical studies, p38⍺ kinase is implicated in Alzheimer’s disease (AD) pathogenesis. In animal models, it mediates impaired synaptic dysfunctio...
PMC12825571
core_pubmed_pmc
The 95% effective dose of ciprofol-assisted sedation for knee arthroplasty in elderly patients: a prospective cohort study
The 95% effective dose of ciprofol-assisted sedation for knee arthroplasty in elderly patients: a prospective cohort study Abstract Background: Sedation is an important component of regional anesthesia. The pharmacokinetics and pharmacodynamics of elderly patients undergo changes with increasing age, resulting in heigh...
PMC12950519
core_pubmed_pmc
Bacteriophage Therapy: Current Strategies and Future Perspectives
Bacteriophage Therapy: Current Strategies and Future Perspectives Abstract ABSTRACT Antimicrobial resistance represents a significant global health threat, demanding alternative treatments beyond traditional antibiotics. Phage therapy has resurged as a promising solution to address this challenge. This manuscript offer...
PMC10967583
core_pubmed_pmc
Assessment of the Effective Tissue Concentrations of Injectable Lidocaine and a Lidocaine-Impregnated Latex Band for Castration in Calves
Assessment of the Effective Tissue Concentrations of Injectable Lidocaine and a Lidocaine-Impregnated Latex Band for Castration in Calves Abstract Simple Summary Castration is commonly performed in young dairy calves and results in pain and discomfort. This study aimed to assess the effective tissue concentrations of t...
PMC12836451
core_pubmed_pmc
Cyclic Peptide–Polymer Conjugate Nanotubes for Delivery of SN‐38 in Treatment of Colorectal Cancer Model
Cyclic Peptide–Polymer Conjugate Nanotubes for Delivery of SN‐38 in Treatment of Colorectal Cancer Model Abstract Abstract Cyclic peptide‐polymer conjugate nanotubes have been shown to be powerful drug delivery vectors, due to their propensity for dynamic self‐assembly, high aspect ratio morphology and structural inter...
PMC7307347
core_pubmed_pmc
Evaluation of pharmacokinetics and safety with bioequivalence of Amlodipine in healthy Chinese volunteers: Bioequivalence Study Findings
Evaluation of pharmacokinetics and safety with bioequivalence of Amlodipine in healthy Chinese volunteers: Bioequivalence Study Findings Abstract Abstract Background and Objective Amlodipine, a main series of L‐type calcium channel blockers (CCBs), exerts potent antihypertensive effects. The aim of this trial was to ex...
PMC10806538
core_pubmed_pmc
Treatment-emergent antidrug antibodies related to PD-1, PD-L1, or CTLA-4 inhibitors across tumor types: a systematic review
Treatment-emergent antidrug antibodies related to PD-1, PD-L1, or CTLA-4 inhibitors across tumor types: a systematic review Abstract Abstract Background Increased understanding of how the immune system regulates tumor growth has innovated the use of immunotherapeutics to treat various cancers. The impact of such therap...
PMC3586862
core_pubmed_pmc
A Review on Therapeutic Drug Monitoring of Immunosuppressant Drugs
A Review on Therapeutic Drug Monitoring of Immunosuppressant Drugs Abstract Immunosuppressants require therapeutic drug monitoring because of their narrow therapeutic index and significant inter-individual variability in blood concentrations. This variability can be because of factors like drug-nutrient interactions, d...
PMC11542719
core_pubmed_pmc
What matters for drug delivery to tumor by nanoparticles: Gaining insights from PBPK/PD simulation of drug nanocrystals
What matters for drug delivery to tumor by nanoparticles: Gaining insights from PBPK/PD simulation of drug nanocrystals Abstract Abstract Background and purpose In our previous studies, drug nanocrystals were directly prepared by solution crystallization, possessing uniform particle size and morphology suitable for int...
PMC5678478
core_pubmed_pmc
Lithium Intoxication: A Possible Interaction with Moxifloxacin
Lithium Intoxication: A Possible Interaction with Moxifloxacin Abstract Abstract Lithium is a well-known treatment for patients with mood disorders. Intoxication by lithium may be lethal particularly in elderly due to altered pharmacokinetics, renal impairment or multiple drug use. We presented a 74-year-old female pat...
PMC9169977
core_pubmed_pmc
In silico exploration of amyloid‐related imaging abnormalities in the gantenerumab open‐label extension trials using a semi‐mechanistic model
In silico exploration of amyloid‐related imaging abnormalities in the gantenerumab open‐label extension trials using a semi‐mechanistic model Abstract Abstract Introduction Amyloid‐related imaging abnormalities with edema/effusion (ARIA‐E) are commonly observed with anti‐amyloid therapies in Alzheimer's disease. We dev...
PMC12183507
core_pubmed_pmc
Molecular pharmacokinetic mechanism of quercetin-encapsulated polymeric micelles in alleviating cisplatin-induced nephrotoxicity and enhancing antineoplastic effects
Molecular pharmacokinetic mechanism of quercetin-encapsulated polymeric micelles in alleviating cisplatin-induced nephrotoxicity and enhancing antineoplastic effects Abstract Introduction Cisplatin (DDP), a platinum-based chemotherapy drug, shows broad antineoplastic activity, however, its clinical use is limited by do...
PMC12863000
core_pubmed_pmc
A phase 1 single and multiple ascending dose study of orforglipron in Japanese participants with type 2 diabetes
A phase 1 single and multiple ascending dose study of orforglipron in Japanese participants with type 2 diabetes Abstract ABSTRACT Introduction We aimed to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of orforglipron in Japanese participants with type 2 diabetes...
PMC5401985
core_pubmed_pmc
First‐in‐human randomized study of bimekizumab, a humanized monoclonal antibody and selective dual inhibitor of IL‐17A and IL‐17F, in mild psoriasis
First‐in‐human randomized study of bimekizumab, a humanized monoclonal antibody and selective dual inhibitor of IL‐17A and IL‐17F, in mild psoriasis Abstract Abstract Aims To assess safety, pharmacokinetics (PK) and clinical efficacy of bimekizumab (formerly UCB4940), a novel humanized monoclonal antibody and dual inhi...
PMC8938140
core_pubmed_pmc
A Reasonable Evaluation of Chuanxiong Rhizoma Processing with Wine through Comparative Pharmacokinetic Study of Bioactive Components: Dominant Effect on Middle Cerebral Artery Occlusion Model Rats
A Reasonable Evaluation of Chuanxiong Rhizoma Processing with Wine through Comparative Pharmacokinetic Study of Bioactive Components: Dominant Effect on Middle Cerebral Artery Occlusion Model Rats Abstract According to the ancient documents and Chinese herbal medicine processing experience, Chuanxiong Rhizoma was usual...
PMC12073025
core_pubmed_pmc
A Liquid Chromatography-Tandem Mass Spectrometry Method for the Quantification of Cystic Fibrosis Drugs (Caftors) in Plasma and Its Application for Therapeutic Monitoring
A Liquid Chromatography-Tandem Mass Spectrometry Method for the Quantification of Cystic Fibrosis Drugs (Caftors) in Plasma and Its Application for Therapeutic Monitoring Abstract Cystic fibrosis (CF) is a life-threatening disorder caused by mutations in the CFTR gene, leading to defective chloride ion transport and th...
PMC5326739
core_pubmed_pmc
Preventive Gabapentin versus Pregabalin to Decrease Postoperative Pain after Lumbar Microdiscectomy: A Randomized Controlled Trial
Preventive Gabapentin versus Pregabalin to Decrease Postoperative Pain after Lumbar Microdiscectomy: A Randomized Controlled Trial Abstract Study Design Randomized controlled trial. Purpose The purpose of this study was to compare pregabalin and gabapentin for mean postoperative visual analog score (VAS) for pain in pa...
PMC5862475
core_pubmed_pmc
Development and validation of a physiology-based model for the prediction of pharmacokinetics/toxicokinetics in rabbits
Development and validation of a physiology-based model for the prediction of pharmacokinetics/toxicokinetics in rabbits Abstract The environmental fates of pharmaceuticals and the effects of crop protection products on non-target species are subjects that are undergoing intense review. Since measuring the concentration...
PMC8868565
core_pubmed_pmc
Efficacy of Vancomycin and Meropenem in Central Nervous System Infections in Children and Adults: Current Update
Efficacy of Vancomycin and Meropenem in Central Nervous System Infections in Children and Adults: Current Update Abstract Abstract The current antimicrobial therapy of bacterial infections of the central nervous system (CNS) in adults and pediatric patients is faced with many pitfalls as the drugs have to reach necessa...
PMC7355427
core_pubmed_pmc
Physiologically-Based Pharmacokinetic (PBPK) Modeling of Buprenorphine in Adults, Children and Preterm Neonates
Physiologically-Based Pharmacokinetic (PBPK) Modeling of Buprenorphine in Adults, Children and Preterm Neonates Abstract Buprenorphine plays a crucial role in the therapeutic management of pain in adults, adolescents and pediatric subpopulations. However, only few pharmacokinetic studies of buprenorphine in children, p...
PMC3734062
core_pubmed_pmc
Polymorphism of ORM1 Is Associated with the Pharmacokinetics of Telmisartan
Polymorphism of ORM1 Is Associated with the Pharmacokinetics of Telmisartan Abstract Abstract Background The pharmacokinetics (PKs) and pharmacodynamics (PDs) of telmisartan varies among the individuals, and the main causes remain unknown. The aim of this study was to evaluate the impact of ORM1 , as well as ABCC2, ABC...
PMC11905874
core_pubmed_pmc
Pharmacokinetics of Depemokimab Delivered by Safety Syringe Device or Autoinjector in Healthy Adults: A Phase 1, Single‐Dose Study
Pharmacokinetics of Depemokimab Delivered by Safety Syringe Device or Autoinjector in Healthy Adults: A Phase 1, Single‐Dose Study Abstract Abstract This Phase I, randomized, multicenter, open‐label, parallel‐group, single‐dose study assessed the relative bioavailability of the anti–interleukin‐5 antibody depemokimab (...
PMC8920090
core_pubmed_pmc
Structure-based drug repurposing: Traditional and advanced AI/ML-aided methods
Structure-based drug repurposing: Traditional and advanced AI/ML-aided methods Abstract Abstract The current global health emergency in the form of the Coronavirus 2019 (COVID-19) pandemic has highlighted the need for fast, accurate, and efficient drug discovery pipelines. Traditional drug discovery projects relying on...
PMC3994241
core_pubmed_pmc
Dosing and switching of paliperidone ER in patients with schizophrenia: recommendations for clinical practice
Dosing and switching of paliperidone ER in patients with schizophrenia: recommendations for clinical practice Abstract Many patients with schizophrenia receive long-term treatment with antipsychotic medication. Switching of antipsychotic medication due to lack of efficacy, tolerability issues, and partial/non-adherence...
PMC12649037
core_pubmed_pmc
Simultaneous determination of iloperidone and its metabolites in rat plasma using a novel UPLC-MS/MS method: an application for drug-drug interaction
Simultaneous determination of iloperidone and its metabolites in rat plasma using a novel UPLC-MS/MS method: an application for drug-drug interaction Abstract Abstract This study aimed to develop and validate a novel ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the simultaneo...
PMC8354907
core_pubmed_pmc
Japanese subpopulation analysis of MONARCH 2: phase 3 study of abemaciclib plus fulvestrant for treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative breast cancer that progressed on endocrine therapy
Japanese subpopulation analysis of MONARCH 2: phase 3 study of abemaciclib plus fulvestrant for treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative breast cancer that progressed on endocrine therapy Abstract Abstract Background This was a Japanese subpopulation analysis of MONARCH ...
PMC5955168
core_pubmed_pmc
Selumetinib-based therapy in uveal melanoma patient-derived xenografts
Selumetinib-based therapy in uveal melanoma patient-derived xenografts Abstract The prognosis of metastatic uveal melanoma (UM) is among the worst of all human cancers. The identification of near-ubiquitous GNAQ/GNA11 mutations and the activation of MAPK signaling in UM have raised hopes of more effective, targeted the...
PMC10380722
core_pubmed_pmc
GL-II-73, a Positive Allosteric Modulator of α5GABA A Receptors, Reverses Dopamine System Dysfunction Associated with Pilocarpine-Induced Temporal Lobe Epilepsy
GL-II-73, a Positive Allosteric Modulator of α5GABA A Receptors, Reverses Dopamine System Dysfunction Associated with Pilocarpine-Induced Temporal Lobe Epilepsy Abstract Abstract Although seizures are a hallmark feature of temporal lobe epilepsy (TLE), psychiatric comorbidities, including psychosis, are frequently asso...
PMC4694690
core_pubmed_pmc
Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy
Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy Abstract The pharmacoenhancement of plasma concentrations of protease inhibitors by coadministration of so-called boosters has been an integral part of antiretroviral therapy for human immunodeficiency virus (HIV) for 1.5 decades. ...
PMC7586988
core_pubmed_pmc
A Phase 1, Randomized, Placebo‐Controlled Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Immunogenicity of Subcutaneous Tezepelumab in Healthy Japanese Men
A Phase 1, Randomized, Placebo‐Controlled Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Immunogenicity of Subcutaneous Tezepelumab in Healthy Japanese Men Abstract Abstract Tezepelumab, a human immunoglobulin G2 monoclonal antibody against thymic stromal lymphopoietin, is currently under clinical de...
PMC4724689
core_pubmed_pmc
Implementation of a reference-scaled average bioequivalence approach for highly variable generic drug products of agomelatine in Chinese subjects
Implementation of a reference-scaled average bioequivalence approach for highly variable generic drug products of agomelatine in Chinese subjects Abstract Abstract The aim of this study was to apply the reference-scaled average bioequivalence (RSABE) approach to evaluate the bioequivalence of 2 formulations of agomelat...
PMC4700704
core_pubmed_pmc
New High-performance Liquid Chromatography-DAD Method for Analytical Determination of Arbutin and Hydroquinone in Rat Plasma
New High-performance Liquid Chromatography-DAD Method for Analytical Determination of Arbutin and Hydroquinone in Rat Plasma Abstract Abstract Natural substances present in herbal preparations should be carefully used because they can give toxic or therapeutic effects despite of their amount or the way of administratio...