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PMC11784359 | core_pubmed_pmc | Evaluation of a potent LpxC inhibitor for post-exposure prophylaxis treatment of antibiotic-resistant Burkholderia pseudomallei in a murine infection model | Evaluation of a potent LpxC inhibitor for post-exposure prophylaxis treatment of antibiotic-resistant Burkholderia pseudomallei in a murine infection model Abstract ABSTRACT LPC-233 (a.k.a. VB-233) is a potent antibiotic targeting the essential enzyme LpxC in Gram-negative bacteria. We present herein the pharmacokineti... |
PMC9291861 | core_pubmed_pmc | Population Pharmacokinetic Analyses of Ertugliflozin in Select Ethnic Populations | Population Pharmacokinetic Analyses of Ertugliflozin in Select Ethnic Populations Abstract Abstract Ertugliflozin, a sodium‐glucose cotransporter 2 inhibitor, is approved for treatment of type 2 diabetes. Two population pharmacokinetic (PK) analyses were conducted, using data from up to 17 phase 1 to 3 studies, to char... |
PMC10867616 | core_pubmed_pmc | Benefits of remimazolam as an anesthetic sedative for older patients: A review | Benefits of remimazolam as an anesthetic sedative for older patients: A review Abstract Abstract Owing to the decreased levels of receptors in the peripheral and central nervous systems, the functions of various organ systems decline in older patients. When administering anesthesia to older patients, it is necessary to... |
PMC9622310 | core_pubmed_pmc | Effects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition of Tofacitinib in Rats | Effects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition of Tofacitinib in Rats Abstract Tofacitinib, a Janus kinase 1 and 3 inhibitor, is mainly metabolized by CYP3A1/2 and CYP2C11 in the liver. The drug has been approved for the chronic treatment of severe ulcerative colitis, a chronic inflamma... |
PMC8144129 | core_pubmed_pmc | The power of modelling pulsatile profiles | The power of modelling pulsatile profiles Abstract Abstract The quantitative description of individual observations in non-linear mixed effects models over time is complicated when the studied biomarker has a pulsatile release (e.g. insulin, growth hormone, luteinizing hormone). Unfortunately, standard non-linear mixed... |
PMC10087276 | core_pubmed_pmc | Influence of Renal Function on Phosphoramide Mustard Exposure: A Nonlinear Mixed‐Effects Analysis | Influence of Renal Function on Phosphoramide Mustard Exposure: A Nonlinear Mixed‐Effects Analysis Abstract Abstract Phosphoramide mustard (PM) is the final cytotoxic metabolite formed from the parent compound cyclophosphamide through a complex metabolic pathway, primarily through hepatic metabolism. Little is known abo... |
PMC11345919 | core_pubmed_pmc | Scaling approaches for the prediction of human clearance of LNA-i-mir-221: A retrospective validation | Scaling approaches for the prediction of human clearance of LNA-i-mir-221: A retrospective validation Abstract LNA-i-miR-221 is a novel microRNA(miRNA)-221 inhibitor designed for the treatment of human malignancies. It has recently undergone phase 1 clinical trial (P1CT) and early pharmacokinetics (PKs) data in cancer ... |
PMC11018670 | core_pubmed_pmc | Drug-Drug Interactions Between Glucagon-Like Peptide 1 Receptor Agonists and Oral Medications: A Systematic Review | Drug-Drug Interactions Between Glucagon-Like Peptide 1 Receptor Agonists and Oral Medications: A Systematic Review Abstract Abstract Background Glucagon-like peptide 1 receptor agonists (GLP1RAs) are used in the treatment of diabetes and obesity. Their slowing effect of gastric emptying might change oral drug absorptio... |
PMC9867583 | core_pubmed_pmc | Simultaneous Determination of Three Compounds in Rat Plasma by UHPLC-QQQ-MS/MS and Its Application to Pharmacokinetics of Banxia Baizhu Tianma Tang | Simultaneous Determination of Three Compounds in Rat Plasma by UHPLC-QQQ-MS/MS and Its Application to Pharmacokinetics of Banxia Baizhu Tianma Tang Abstract A rapid and highly selective and sensitive ultra-high-performance liquid chromatography coupled with triple quadrupole mass spectrometry (UHPLC-QQQ-MS/MS) method w... |
PMC10957469 | core_pubmed_pmc | MYC targeting by OMO-103 in solid tumors: a phase 1 trial | MYC targeting by OMO-103 in solid tumors: a phase 1 trial Abstract Abstract Among the ‘most wanted’ targets in cancer therapy is the oncogene MYC, which coordinates key transcriptional programs in tumor development and maintenance. It has, however, long been considered undruggable. OMO-103 is a MYC inhibitor consisting... |
PMC9145573 | core_pubmed_pmc | A Comprehensive Review of the Cardiovascular Protective Properties of Silibinin/Silymarin: A New Kid on the Block | A Comprehensive Review of the Cardiovascular Protective Properties of Silibinin/Silymarin: A New Kid on the Block Abstract Abstract Silibinin/silymarin has been used in herbal medicine for thousands of years and it is well-known for its hepato-protective properties. The present comprehensive literature review aimed to ... |
PMC7678077 | core_pubmed_pmc | Bioequivalence of levamlodipine besylate tablets in healthy Chinese subjects: a single-dose and two-period crossover randomized study | Bioequivalence of levamlodipine besylate tablets in healthy Chinese subjects: a single-dose and two-period crossover randomized study Abstract Abstract Background Levamlodipine, a calcium channel blocker, has been show act as a cardiovascular drug. To compare the pharmacokinetic parameters between levamlodipine (test f... |
PMC11862003 | core_pubmed_pmc | Copper-Induced Neurodegenerative Disorders and Therapeutic Potential of Curcumin-Loaded Nanoemulsion | Copper-Induced Neurodegenerative Disorders and Therapeutic Potential of Curcumin-Loaded Nanoemulsion Abstract Abstract Copper accumulation in neurons induces oxidative stress, disrupts mitochondrial activity, and accelerates neuronal death, which is central to the pathophysiology of neurodegenerative diseases like Wils... |
PMC12928139 | core_pubmed_pmc | Isoflurane as a cost-effective alternative to sevoflurane for short-duration gynaecological brachytherapy: a randomised non-inferiority trial of emergence | Isoflurane as a cost-effective alternative to sevoflurane for short-duration gynaecological brachytherapy: a randomised non-inferiority trial of emergence Abstract Abstract Purpose The optimal anaesthetic choice for gynaecological brachytherapy remains uncertain. While sevoflurane offers rapid recovery due to favourabl... |
PMC3889329 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Rising Doses of Empagliflozin in Patients with Type 2 Diabetes Mellitus | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Rising Doses of Empagliflozin in Patients with Type 2 Diabetes Mellitus Abstract Abstract Introduction This study examined the safety, tolerability, pharmacokinetics, and pharmacodynamics of empagliflozin, a potent and highly selective sodium gluc... |
PMC12393703 | core_pubmed_pmc | Population pharmacokinetic modeling of missed mycophenolate mofetil doses: Impact on exposure and exploration of mitigation strategies | Population pharmacokinetic modeling of missed mycophenolate mofetil doses: Impact on exposure and exploration of mitigation strategies Abstract Background Missed doses of mycophenolate mofetil (MMF) are frequent in transplant recipients and may lead to subtherapeutic exposure to mycophenolic acid (MPA), potentially com... |
PMC6268695 | core_pubmed_pmc | Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics | Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics Abstract Abstract This study aimed to investigate the in vitro skin permeation and in vivo antineoplastic effect of curcumin by using liposomes as the transdermal drug-delivery system. Soybean phospholipids (SPC), egg ... |
PMC4802699 | core_pubmed_pmc | Cost savings of anti-TNF therapy using a test-based strategy versus an empirical dose escalation in Crohn's disease patients who lose response to infliximab | Cost savings of anti-TNF therapy using a test-based strategy versus an empirical dose escalation in Crohn's disease patients who lose response to infliximab Abstract Abstract Background The use of pharmacokinetics is associated with cost savings in anti-tumor necrosis factor (anti-TNF) therapy, but the long-term cost s... |
PMC3236732 | core_pubmed_pmc | Dynamics of Parasite Clearance in Cutaneous Leishmaniasis Patients Treated with Miltefosine | Dynamics of Parasite Clearance in Cutaneous Leishmaniasis Patients Treated with Miltefosine Abstract Parasite loads were quantified in repeated skin biopsies from lesions of 2 patients with Old-World cutaneous leishmaniasis (CL) caused by Leishmania major and L. infantum during and after treatment with miltefosine. Mil... |
PMC12472987 | core_pubmed_pmc | Effect of Drying Methods on Bioactivity of Pyrostegia venusta Extracts: Antioxidant Assays, Cytotoxicity, and Computational Approaches | Effect of Drying Methods on Bioactivity of Pyrostegia venusta Extracts: Antioxidant Assays, Cytotoxicity, and Computational Approaches Abstract Background/Objectives: Pyrostegia venusta (Cipó-de-São-João), a native Brazilian Cerrado plant, is rich antioxidant phytochemicals. The efficacy of herbal extracts, particularl... |
PMC6150361 | core_pubmed_pmc | Spectrum-Effect Relationships between Fingerprints of Caulophyllum robustum Maxim and Inhabited Pro-Inflammation Cytokine Effects | Spectrum-Effect Relationships between Fingerprints of Caulophyllum robustum Maxim and Inhabited Pro-Inflammation Cytokine Effects Abstract Abstract Caulophyllum robustum Maxim (CRM) is a Chinese folk medicine with significant effect on treatment of rheumatoid arthritis (RA). This study was designed to explore the spect... |
PMC6930690 | core_pubmed_pmc | Docetaxel and Doxorubicin Codelivery by Nanocarriers for Synergistic Treatment of Prostate Cancer | Docetaxel and Doxorubicin Codelivery by Nanocarriers for Synergistic Treatment of Prostate Cancer Abstract Combination chemotherapy has been proven to be an efficient strategy for the treatment of prostate cancer (PCA). However, the pharmacokinetic distinction between the relevant drugs is an insurmountable barrier to ... |
PMC3674995 | core_pubmed_pmc | Safety, Pharmacokinetic, and Efficacy Studies of Oral DB868 in a First Stage Vervet Monkey Model of Human African Trypanosomiasis | Safety, Pharmacokinetic, and Efficacy Studies of Oral DB868 in a First Stage Vervet Monkey Model of Human African Trypanosomiasis Abstract Abstract There are no oral drugs for human African trypanosomiasis (HAT, sleeping sickness). A successful oral drug would have the potential to reduce or eliminate the need for pati... |
PMC9420434 | core_pubmed_pmc | Scientific Rationale for Waiving Clinical Efficacy Testing of Biosimilars | Scientific Rationale for Waiving Clinical Efficacy Testing of Biosimilars Abstract Abstract After 18 years and the administration of billions of doses, there is little doubt about biosimilars’ safety and efficacy. Yet, only 14 molecules in the EU and 9 in the US are available as biosimilars, among the 200+ targets, due... |
PMC6046594 | core_pubmed_pmc | Performing and interpreting individual pharmacokinetic profiles in patients with Hemophilia A or B: Rationale and general considerations | Performing and interpreting individual pharmacokinetic profiles in patients with Hemophilia A or B: Rationale and general considerations Abstract Abstract Objectives In a separate document, we have provided specific guidance on performing individual pharmacokinetic (PK) studies using limited samples in persons with hem... |
PMC6800500 | core_pubmed_pmc | DALBACEN cohort: dalbavancin as consolidation therapy in patients with endocarditis and/or bloodstream infection produced by gram-positive cocci | DALBACEN cohort: dalbavancin as consolidation therapy in patients with endocarditis and/or bloodstream infection produced by gram-positive cocci Abstract Abstract Objectives To analyse the effectiveness of dalbavancin (DBV) in clinical practice as consolidation therapy in patients with bloodstream infection (BSI) and/o... |
PMC6222316 | core_pubmed_pmc | UPLC-MS/MS Method for the Determination of 14 Compounds in Rat Plasma and Its Application in a Pharmacokinetic Study of Orally Administered Xiaoyao Powder | UPLC-MS/MS Method for the Determination of 14 Compounds in Rat Plasma and Its Application in a Pharmacokinetic Study of Orally Administered Xiaoyao Powder Abstract Xiaoyao Powder (XYP), a common Chinese medicine, comprises eight traditional Chinese herbs and has been widely used clinically to treat liver damage and men... |
PMC7468263 | core_pubmed_pmc | Mechanisms and pharmacokinetic/pharmacodynamic profiles underlying the low nephrotoxicity and ototoxicity of etimicin | Mechanisms and pharmacokinetic/pharmacodynamic profiles underlying the low nephrotoxicity and ototoxicity of etimicin Abstract Abstract Etimicin (ETM), a fourth-generation aminoglycosides (AGs), is now widely clinically used in China due to its high efficacy and low toxicity. However, the mechanisms underlying its low ... |
PMC4012347 | core_pubmed_pmc | Possible impact of the CYP2D6*10 polymorphism on the nonlinear pharmacokinetic parameter estimates of paroxetine in Japanese patients with major depressive disorders | Possible impact of the CYP2D6*10 polymorphism on the nonlinear pharmacokinetic parameter estimates of paroxetine in Japanese patients with major depressive disorders Abstract It has been suggested that the reduced function allele with reduced cytochrome P450 (CYP) 2D6 activity, CYP2D6*10 , is associated with the interi... |
PMC6862800 | core_pubmed_pmc | Contributions of a blended learning based on peer evaluation for teaching drug-drug interactions to undergraduate pharmacy students | Contributions of a blended learning based on peer evaluation for teaching drug-drug interactions to undergraduate pharmacy students Abstract Abstract Background Numerous studies have pointed out the need for better training of healthcare professionals in drug-drug interactions management in order to minimize adverse dr... |
PMC10831332 | core_pubmed_pmc | A Phase Ib First-In-Patient Study Assessing the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Ponsegromab in Participants with Cancer and Cachexia | A Phase Ib First-In-Patient Study Assessing the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Ponsegromab in Participants with Cancer and Cachexia Abstract Abstract Purpose: Cachexia is common in patients with advanced cancer and is associated with elevated serum growth differentiation factor 15 (GDF-... |
PMC10406827 | core_pubmed_pmc | Targeted dosing for susceptible heteroresistant subpopulations may improve rational dosage regimen prediction for colistin in broiler chickens | Targeted dosing for susceptible heteroresistant subpopulations may improve rational dosage regimen prediction for colistin in broiler chickens Abstract Abstract The dosage of colistin for the treatment of enteric E. coli in animals necessitates considering the heteroresistant (HR) nature of the targeted inoculum, descr... |
PMC10362308 | core_pubmed_pmc | Dynamic 2-deoxy- D -glucose-enhanced multispectral optoacoustic tomography for assessing metabolism and vascular hemodynamics of breast cancer | Dynamic 2-deoxy- D -glucose-enhanced multispectral optoacoustic tomography for assessing metabolism and vascular hemodynamics of breast cancer Abstract Clinical tools for measuring tumor vascular hemodynamics, such as dynamic contrast-enhanced MRI, are clinically important to assess tumor properties. Here we explored t... |
PMC6295742 | core_pubmed_pmc | The pharmacokinetics of intranasal droperidol in volunteers characterised via population modelling | The pharmacokinetics of intranasal droperidol in volunteers characterised via population modelling Abstract Abstract Background: Droperidol is used parenterally to treat nausea and vomiting, migraine and acute behavioural disturbance. Intranasal use is not reported for droperidol. Intranasal drug administration reduces... |
PMC11538706 | core_pubmed_pmc | Integrated Electrochemical Aptamer Biosensing and Colorimetric pH Monitoring via Hydrogel Microneedle Assays for Assessing Antibiotic Treatment | Integrated Electrochemical Aptamer Biosensing and Colorimetric pH Monitoring via Hydrogel Microneedle Assays for Assessing Antibiotic Treatment Abstract Abstract Current methods for therapeutic drug monitoring (TDM) have a long turnaround time as they involve collecting patients' blood samples followed by transferring ... |
PMC10534584 | core_pubmed_pmc | Safety Evaluation and Population Pharmacokinetics of Camostat Mesylate and Its Major Metabolites Using a Phase I Study | Safety Evaluation and Population Pharmacokinetics of Camostat Mesylate and Its Major Metabolites Using a Phase I Study Abstract Camostat mesylate is expected to be promising as a treatment option for COVID-19, in addition to other indications for which it is currently used. Furthermore, in vitro experiments have confir... |
PMC5598389 | core_pubmed_pmc | Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)- N -(1 H -pyrazol-3-yl)- N -(2-thienylmethyl)acetamide | Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)- N -(1 H -pyrazol-3-yl)- N -(2-thienylmethyl)acetamide Abstract Abstract A toxicological evaluation of a novel cooling agent, 2-(4-methylphenoxy)- N -(1 H -pyrazol-3-yl)- N -(2-thienylmethyl) acetamide (S2227; CAS 1374760-95-8), was completed for... |
PMC5064152 | core_pubmed_pmc | Drug Concentration Thresholds Predictive of Therapy Failure and Death in Children With Tuberculosis: Bread Crumb Trails in Random Forests | Drug Concentration Thresholds Predictive of Therapy Failure and Death in Children With Tuberculosis: Bread Crumb Trails in Random Forests Abstract Background. The role of drug concentrations in clinical outcomes in children with tuberculosis is unclear. Target concentrations for dose optimization are unknown. Methods. ... |
PMC3586143 | core_pubmed_pmc | Pharmacokinetic Drug Interactions with Vandetanib during Coadministration with Rifampicin or Itraconazole | Pharmacokinetic Drug Interactions with Vandetanib during Coadministration with Rifampicin or Itraconazole Abstract Abstract Objective: The aim of this study was to investigate the effects of a potent CYP3A4 inducer, rifampicin (Study A), and a potent CYP3A4 inhibitor, itraconazole (Study B), on the pharmacokinetics of ... |
PMC9876408 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Anti-C5a Antibody BDB-001 for Severe COVID-19: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Clinical Trial in Healthy Chinese Adults | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Anti-C5a Antibody BDB-001 for Severe COVID-19: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Clinical Trial in Healthy Chinese Adults Abstract Introduction Severe Coronavirus Disease 2019 (COVID-19) progresses with inflammation and coagulation, du... |
PMC10865928 | core_pubmed_pmc | CC-96673 (BMS-986358), an affinity-tuned anti-CD47 and CD20 bispecific antibody with fully functional fc, selectively targets and depletes non-Hodgkin’s lymphoma | CC-96673 (BMS-986358), an affinity-tuned anti-CD47 and CD20 bispecific antibody with fully functional fc, selectively targets and depletes non-Hodgkin’s lymphoma Abstract ABSTRACT Cluster of differentiation 47 (CD47) is a transmembrane protein highly expressed in tumor cells that interacts with signal regulatory protei... |
PMC7114756 | core_pubmed_pmc | Quantum Chemical Lipophilicities of Antimalarial Drugs in Relation to Terminal Half-Life | Quantum Chemical Lipophilicities of Antimalarial Drugs in Relation to Terminal Half-Life Abstract According to the WHO, artemisinin-based combination therapies (ACTs) have been integral to the recent reduction in deaths due to Plasmodium falciparum malaria. ACT-resistant strains are an emerging problem and have evolved... |
PMC11373093 | core_pubmed_pmc | Anti-infectivity efficacy and pharmacokinetics of WHO recommended single low-dose primaquine in children with acute Plasmodium falciparum in Burkina Faso: study protocol | Anti-infectivity efficacy and pharmacokinetics of WHO recommended single low-dose primaquine in children with acute Plasmodium falciparum in Burkina Faso: study protocol Abstract Background Primaquine (PQ) has activity against mature P. falciparum gametocytes and proven transmission blocking efficacy (TBE) between huma... |
PMC6312076 | core_pubmed_pmc | Apolipoprotein E mimetic peptide CN-105 improves outcome in a murine model of SAH | Apolipoprotein E mimetic peptide CN-105 improves outcome in a murine model of SAH Abstract Objective Subarachnoid haemorrhage (SAH) accounts for 3% of all strokes, and is associated with significant morbidity and mortality. There is growing evidence implicating apolipoprotein E (apoE) in mediating adaptive anti-inflamm... |
PMC6520478 | core_pubmed_pmc | Cognitive impairment in depression: recent advances and novel treatments | Cognitive impairment in depression: recent advances and novel treatments Abstract Abstract In the past, little or no attention was paid to cognitive disorders associated with depression (a condition sometimes termed pseudodementia). However, recent years have seen a growing interest in these changes, not only because o... |
PMC9328278 | core_pubmed_pmc | Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects | Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects Abstract Abstract Aims Selexipag is a prostacyclin receptor agonist approved for the treatment of pulmonary arterial hypertension. Cytochrome P450 (CYP) 2C8 is involv... |
PMC9144278 | core_pubmed_pmc | Inclusion of a Phytomedicinal Flavonoid in Biocompatible Surface-Modified Chylomicron Mimic Nanovesicles with Improved Oral Bioavailability and Virucidal Activity: Molecular Modeling and Pharmacodynamic Studies | Inclusion of a Phytomedicinal Flavonoid in Biocompatible Surface-Modified Chylomicron Mimic Nanovesicles with Improved Oral Bioavailability and Virucidal Activity: Molecular Modeling and Pharmacodynamic Studies Abstract Morin hydrate (MH) is a widely-used Asian phytomedicinal flavonoid with a wide range of reported the... |
PMC9372429 | core_pubmed_pmc | Longitudinal nonlinear mixed effects modeling of EGFR mutations in ctDNA as predictor of disease progression in treatment of EGFR‐mutant non‐small cell lung cancer | Longitudinal nonlinear mixed effects modeling of EGFR mutations in ctDNA as predictor of disease progression in treatment of EGFR‐mutant non‐small cell lung cancer Abstract Abstract Correlations between increasing concentrations of circulating tumor DNA (ctDNA) in plasma and disease progression have been shown. A nonli... |
PMC8398527 | core_pubmed_pmc | Repurposing of the Fasciolicide Triclabendazole to Treat Infections Caused by Staphylococcus spp. and Vancomycin-Resistant Enterococci | Repurposing of the Fasciolicide Triclabendazole to Treat Infections Caused by Staphylococcus spp. and Vancomycin-Resistant Enterococci Abstract Abstract One approach to combat the increasing incidence of multidrug-resistant (MDR) bacterial pathogens involves repurposing existing compounds with known safety and developm... |
PMC12389175 | core_pubmed_pmc | Indazole Derivatives Against Murine Cutaneous Leishmaniasis | Indazole Derivatives Against Murine Cutaneous Leishmaniasis Abstract Background/Objectives : Leishmaniasis is a zoonotic and anthropozoonotic disease with significant public health impact worldwide and is classified as a neglected tropical disease. The search for new affordable treatments, particularly oral and/or topi... |
PMC11322809 | core_pubmed_pmc | Estimation of withdrawal interval recommendations following administration of fenbendazole medicated feed to ring-necked pheasants ( Phasianus colchicus ) | Estimation of withdrawal interval recommendations following administration of fenbendazole medicated feed to ring-necked pheasants ( Phasianus colchicus ) Abstract Introduction Prescribing fenbendazole medicated feed for pheasants in the USA is considered extra-label drug use under CPG Sec 615.115, and a safe estimated... |
PMC7069879 | core_pubmed_pmc | Extended half‐life rFIX in major surgery—How to improve clinical practice: An intraindividual comparison | Extended half‐life rFIX in major surgery—How to improve clinical practice: An intraindividual comparison Abstract Abstract Practical, safe, and effective hemostatic approach to orthopedic surgery using Extended Half‐Life factor IX in hemophilia B. By intraindividual comparison, we found a lower FIX consumption, number ... |
PMC4775925 | core_pubmed_pmc | Population Pharmacokinetics of Pyronaridine in Pediatric Malaria Patients | Population Pharmacokinetics of Pyronaridine in Pediatric Malaria Patients Abstract Pyramax is a pyronaridine (PYR)-artesunate (PA) combination for the treatment of uncomplicated malaria in adult and pediatric patients. A granule formulation of this combination is being developed for treatment of uncomplicated P. falcip... |
PMC12184067 | core_pubmed_pmc | INTERCEPT-AD, a phase 1 study of intravenous sabirnetug in participants with mild cognitive impairment or mild dementia due to Alzheimer's disease | INTERCEPT-AD, a phase 1 study of intravenous sabirnetug in participants with mild cognitive impairment or mild dementia due to Alzheimer's disease Abstract Background Soluble species of multimeric amyloid-beta including globular amyloid-beta oligomers (AβOs) and linear amyloid-beta protofibrils are toxic to neurons. Sa... |
PMC9199868 | core_pubmed_pmc | Evaluation of the potential for pharmacokinetic interaction between tirabrutinib and levonorgestrel/ethinyl estradiol in healthy female volunteers | Evaluation of the potential for pharmacokinetic interaction between tirabrutinib and levonorgestrel/ethinyl estradiol in healthy female volunteers Abstract Abstract Tirabrutinib (TIRA), a potent and nonreversible oral Bruton tyrosine kinase inhibitor, is evaluated for treatment of certain hematological malignancies and... |
PMC8551512 | core_pubmed_pmc | The correlation between the level of 3-hydroxypropyl mercapturic acid, CYP2B6 polymorphisms, and hematuria occurrences after cyclophosphamide administration and its bioanalytical methods: A systematic review | The correlation between the level of 3-hydroxypropyl mercapturic acid, CYP2B6 polymorphisms, and hematuria occurrences after cyclophosphamide administration and its bioanalytical methods: A systematic review Abstract Abstract Background Cyclophosphamide (CPA) is a cytotoxic prodrug that needs to be metabolized by cytoc... |
PMC5812399 | core_pubmed_pmc | Phase I study of tomuzotuximab, a glycoengineered therapeutic antibody against the epidermal growth factor receptor, in patients with advanced carcinomas | Phase I study of tomuzotuximab, a glycoengineered therapeutic antibody against the epidermal growth factor receptor, in patients with advanced carcinomas Abstract Background Changes in glycosylation of the constant domain (Fc) of monoclonal antibodies (mAbs) enhance antibody-dependent cell-mediated cytotoxicity indepen... |
PMC11727424 | core_pubmed_pmc | Oxidative Stress Induced by Antivirals: Implications for Adverse Outcomes During Pregnancy and in Newborns | Oxidative Stress Induced by Antivirals: Implications for Adverse Outcomes During Pregnancy and in Newborns Abstract Abstract Oxidative stress plays a critical role in various physiological and pathological processes, particularly during pregnancy, where it can significantly affect maternal and fetal health. In the cont... |
PMC12014616 | core_pubmed_pmc | HPLC-UV method development and validation for anticancer drug sorafenib and the co-prescribed drug dexamethasone: application to pharmacokinetic evaluation of sorafenib nanoformulations | HPLC-UV method development and validation for anticancer drug sorafenib and the co-prescribed drug dexamethasone: application to pharmacokinetic evaluation of sorafenib nanoformulations Abstract Abstract Sorafenib is used to treat advanced renal cell carcinoma. A high-performance liquid chromatography (HPLC) method was... |
PMC12803216 | core_pubmed_pmc | CD99Targeted Irinotecan Containing Nanoparticles Show Twenty-Fold Greater Anti-Tumor Effect Than Free Irinotecan For Treatment of Ewing Sarcoma | CD99Targeted Irinotecan Containing Nanoparticles Show Twenty-Fold Greater Anti-Tumor Effect Than Free Irinotecan For Treatment of Ewing Sarcoma Abstract Abstract Purpose: To assess the antitumor efficacy, pharmacokinetics, and safety of NV103, a CD99-targeted liposomal irinotecan nanoparticle, in a preclinical Ewing sa... |
PMC12735253 | core_pubmed_pmc | Molecular Docking and Dynamics Simulations Reveal the Antidiabetic Potential of a Novel Fucoxanthin Derivative from Chnoospora minima | Molecular Docking and Dynamics Simulations Reveal the Antidiabetic Potential of a Novel Fucoxanthin Derivative from Chnoospora minima Abstract Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder requiring safer and more effective therapeutic alternatives. This study investigates a novel fucoxanthin derivati... |
PMC11533328 | core_pubmed_pmc | A Phase 1 Study of ABI ‐009 ( Nab ‐sirolimus) in Combination With Temozolomide and Irinotecan in Pediatric Patients With Recurrent or Refractory Solid Tumors, Including CNS Tumors—A Children's Oncology Group Pediatric Early Phase Clinical Trial Network Study ADVL1514 | A Phase 1 Study of ABI ‐009 ( Nab ‐sirolimus) in Combination With Temozolomide and Irinotecan in Pediatric Patients With Recurrent or Refractory Solid Tumors, Including CNS Tumors—A Children's Oncology Group Pediatric Early Phase Clinical Trial Network Study ADVL1514 Abstract ABSTRACT Background Nab ‐sirolimus (ABI‐009... |
PMC8589691 | core_pubmed_pmc | Design of FLAIR: a Phase 2b Study of the 5-Lipoxygenase Activating Protein Inhibitor AZD5718 in Patients With Proteinuric CKD | Design of FLAIR: a Phase 2b Study of the 5-Lipoxygenase Activating Protein Inhibitor AZD5718 in Patients With Proteinuric CKD Abstract Introduction Patients with chronic kidney disease (CKD) remain at risk for kidney and cardiovascular events resulting from residual albuminuria, despite available treatments. Leukotrien... |
PMC4977098 | core_pubmed_pmc | Role of isavuconazole in the treatment of invasive fungal infections | Role of isavuconazole in the treatment of invasive fungal infections Abstract Abstract Despite recent advances in both diagnosis and prevention, the incidence of invasive fungal infections continues to rise. Available antifungal agents to treat invasive fungal infections include polyenes, triazoles, and echinocandins. ... |
PMC10267409 | core_pubmed_pmc | Hydroxyurea pharmacokinetics and precision dosing in low-resource settings | Hydroxyurea pharmacokinetics and precision dosing in low-resource settings Abstract Abstract Introduction: Hydroxyurea is effective disease-modifying treatment for sickle cell anemia (SCA). Escalation to maximum tolerated dose (MTD) achieves superior benefits without additional toxicities, but requires dose adjustments... |
PMC11619718 | core_pubmed_pmc | Kratom: A Narrative Review of the Possible Clinical Uses and Dangers of This Opioid-Like Plant | Kratom: A Narrative Review of the Possible Clinical Uses and Dangers of This Opioid-Like Plant Abstract Abstract The term "kratom" refers to a plant species formally known as Mitragyna speciosa. Kratom is composed of over 40 alkaloids, a type of organic compound that contains nitrogen. These compounds work primarily vi... |
PMC12476711 | core_pubmed_pmc | Antimicrobial dosing considerations in critically ill patients with acute kidney injury: A review | Antimicrobial dosing considerations in critically ill patients with acute kidney injury: A review Abstract Abstract Sepsis-associated acute kidney injury is common in critically ill patients and is strongly associated with an increased risk of adverse outcomes and mortality. While early and appropriate antimicrobials f... |
PMC9174596 | core_pubmed_pmc | Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study | Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study Abstract Background Enteropathy is prevalent in tuberculosis-endemic areas, and it has been shown to impair intestinal absorptive function; therefore, enteropathogen bu... |
PMC12127241 | core_pubmed_pmc | Impact of Drug–Drug Interactions on Clinical Outcomes in Metastatic Melanoma Patients Treated With Combined BRAF/MEK Inhibitors: A Real‐World Study | Impact of Drug–Drug Interactions on Clinical Outcomes in Metastatic Melanoma Patients Treated With Combined BRAF/MEK Inhibitors: A Real‐World Study Abstract ABSTRACT The unique pharmacokinetics of BRAF and MEK inhibitors make patients vulnerable to drug–drug interactions (DDIs), which may compromise treatment efficacy ... |
PMC5565967 | core_pubmed_pmc | Pharmacodynamics of the Orotomides against Aspergillus fumigatus : New Opportunities for Treatment of Multidrug-Resistant Fungal Disease | Pharmacodynamics of the Orotomides against Aspergillus fumigatus : New Opportunities for Treatment of Multidrug-Resistant Fungal Disease Abstract ABSTRACT F901318 is an antifungal agent with a novel mechanism of action and potent activity against Aspergillus spp. An understanding of the pharmacodynamics (PD) of F901318... |
PMC5099555 | core_pubmed_pmc | Clinical trials for authorized biosimilars in the European Union: a systematic review | Clinical trials for authorized biosimilars in the European Union: a systematic review Abstract Aim In 2006, Omnitrope (by Sandoz) was the first approved biosimilar in Europe. To date, 21 biosimilars for seven different biologics are on the market. The present study compared the clinical trials undertaken to obtain mark... |
PMC10238757 | core_pubmed_pmc | A phase I, first‐in‐human study investigating the safety, tolerability, and pharmacokinetics of the maturation inhibitor GSK3739937 | A phase I, first‐in‐human study investigating the safety, tolerability, and pharmacokinetics of the maturation inhibitor GSK3739937 Abstract Abstract We report the safety and pharmacokinetic properties of the HIV‐1 maturation inhibitor GSK3739937 (GSK'937) in healthy participants. This was a phase I, first‐in‐human, do... |
PMC5644271 | core_pubmed_pmc | Design of a Bayesian adaptive phase 2 proof-of-concept trial for BAN2401, a putative disease-modifying monoclonal antibody for the treatment of Alzheimer's disease | Design of a Bayesian adaptive phase 2 proof-of-concept trial for BAN2401, a putative disease-modifying monoclonal antibody for the treatment of Alzheimer's disease Abstract Abstract Introduction Recent failures in phase 3 clinical trials in Alzheimer's disease (AD) suggest that novel approaches to drug development are ... |
PMC10011291 | core_pubmed_pmc | A Pharmacokinetic, Safety, and Tolerability Trial of Palovarotene in Healthy Japanese and Non-Japanese Participants | A Pharmacokinetic, Safety, and Tolerability Trial of Palovarotene in Healthy Japanese and Non-Japanese Participants Abstract Background and Objective Palovarotene is an oral, selective retinoic acid receptor gamma agonist under investigation for fibrodysplasia ossificans progressiva (FOP). Palovarotene is primarily met... |
PMC12043489 | core_pubmed_pmc | The pharmacokinetics and Concentration-QTc analysis of a new etomidate analog ET-26-HCl: a phase I trial in healthy Chinese subjects | The pharmacokinetics and Concentration-QTc analysis of a new etomidate analog ET-26-HCl: a phase I trial in healthy Chinese subjects Abstract Methoxetamine hydrochloride (ET-26-HCl) is a novel short-acting intravenous general anesthetic that retains the advantages of etomidate while minimizing its impact on adrenal cor... |
PMC11287742 | core_pubmed_pmc | Polymer-Tethered Quenched Fluorescent Probes for Enhanced Imaging of Tumor-Associated Proteases | Polymer-Tethered Quenched Fluorescent Probes for Enhanced Imaging of Tumor-Associated Proteases Abstract Fluorescence-based contrast agents enable real-time detection of solid tumors and their neovasculature, making them ideal for use in image-guided surgery. Several agents have entered late-stage clinical trials or se... |
PMC9962863 | core_pubmed_pmc | Scaling Pharmacodynamics from Rats to Humans to Support Erythropoietin and Romiplostim Combination Therapy to Treat Erythropoietin-Resistant Anemia | Scaling Pharmacodynamics from Rats to Humans to Support Erythropoietin and Romiplostim Combination Therapy to Treat Erythropoietin-Resistant Anemia Abstract Abstract Recombinant human erythropoietin (rHuEPO) is one of the most effective drugs for the treatment of anemia in patients with chronic kidney disease. However,... |
PMC6449316 | core_pubmed_pmc | Mathematical modeling in cancer nanomedicine: a review | Mathematical modeling in cancer nanomedicine: a review Abstract Cancer continues to be among the leading healthcare problems worldwide, and efforts continue not just to find better drugs, but also better drug delivery methods. The need for delivering cytotoxic agents selectively to cancerous cells, for improved safety ... |
PMC10203393 | core_pubmed_pmc | Fecal metabolomics combined with 16S rRNA gene sequencing to analyze the effect of Jiaotai pill intervention in type 2 diabetes mellitus rats | Fecal metabolomics combined with 16S rRNA gene sequencing to analyze the effect of Jiaotai pill intervention in type 2 diabetes mellitus rats Abstract The occurrence and development of type 2 diabetes mellitus (T2DM) are closely related to gut microbiota. Jiaotai pill (JTP) is used to treat type 2 diabetes mellitus, wi... |
PMC8364835 | core_pubmed_pmc | A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes | A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes Abstract Abstract Diabetes mellitus is a multifactorial global health disorder that is rising at an alarming rate. Cardiovascular diseases, kidney damage and neuropathy are the main cause of high mortality ... |
PMC9884086 | core_pubmed_pmc | Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia | Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia Abstract Abstract PDE10A is an important regulator of striatal signaling that, when inhibited, can normalize dysfunctional activity. Given the involvement of dysfunctional striatal activity with schizophrenia, PDE10A... |
PMC8238023 | core_pubmed_pmc | Novel associations between CYP2B6 polymorphisms, perioperative methadone metabolism and clinical outcomes in children | Novel associations between CYP2B6 polymorphisms, perioperative methadone metabolism and clinical outcomes in children Abstract Abstract Aim: Methadone exhibits significant variability in clinical response. This study explores the genetic influence of variable methadone pharmacokinetics. Methods: This is a prospective s... |
PMC8292428 | core_pubmed_pmc | Nanoparticle T-cell engagers as a modular platform for cancer immunotherapy | Nanoparticle T-cell engagers as a modular platform for cancer immunotherapy Abstract Abstract T-cell-based immunotherapy, such as CAR-T cells and bispecific T-cell engagers (BiTEs), has shown promising clinical outcomes in many cancers; however, these therapies have significant limitations, such as poor pharmacokinetic... |
PMC11360309 | core_pubmed_pmc | Patient resuscitated after cardiopulmonary arrest exhibits abnormally increased phenytoin metabolic rate due to unknown factors: a case report | Patient resuscitated after cardiopulmonary arrest exhibits abnormally increased phenytoin metabolic rate due to unknown factors: a case report Abstract Background Fosphenytoin (FOS) is a prodrug of phenytoin (PHT) with a metabolism that exhibits Michaelis–Menten-type kinetics. Genetic polymorphisms of the metabolic enz... |
PMC8204096 | core_pubmed_pmc | Next‐generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells | Next‐generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells Abstract Abstract Objectives Bruton's tyrosine kinase (BTK) plays a non‐redundant signaling role downstream of the B‐cell receptor (BCR) in ... |
PMC10195965 | core_pubmed_pmc | Comparative Bioequivalence of Tablet and Capsule Formulations of Ulotaront and the Effect of Food on the Pharmacokinetics of the Tablet Form in Humans | Comparative Bioequivalence of Tablet and Capsule Formulations of Ulotaront and the Effect of Food on the Pharmacokinetics of the Tablet Form in Humans Abstract Introduction Ulotaront (SEP-363856), a dual trace animeassociated receptor 1 (TAAR1) and 5-HT 1A receptor agonist, is in phase 3 clinical development for the tr... |
PMC12896379 | core_pubmed_pmc | Novel Drug‐Disease Modeling Framework for Oncology Benefit–Risk Evaluation: Application to Tusamitamab Ravtansine | Novel Drug‐Disease Modeling Framework for Oncology Benefit–Risk Evaluation: Application to Tusamitamab Ravtansine Abstract ABSTRACT This study introduces a novel drug‐disease modeling framework designed to assess the benefit–risk balance of antibody‐drug conjugates (ADC) in oncology. The framework integrates dose level... |
PMC7323835 | core_pubmed_pmc | A Phase 1 Study of SLC-0111, a Novel Inhibitor of Carbonic Anhydrase IX, in Patients With Advanced Solid Tumors | A Phase 1 Study of SLC-0111, a Novel Inhibitor of Carbonic Anhydrase IX, in Patients With Advanced Solid Tumors Abstract Supplemental Digital Content is available in the text. Objectives: SLC-0111 is an ureido-substituted benzenesulfonamide small molecule inhibitor of carbonic anhydrase IX. The objectives of this first... |
PMC5318329 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics Modelling of Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome | Population Pharmacokinetics and Pharmacodynamics Modelling of Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome Abstract Abstract Introduction Dilmapimod is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor and was investigated in a study ( NCT00996840 ) for its anti-infl... |
PMC3663203 | core_pubmed_pmc | Utility of CSF in translational neuroscience | Utility of CSF in translational neuroscience Abstract Abstract Human cerebrospinal fluid (CSF) sampling is of high value as the only general applicable methodology to obtain information on free drug concentrations in individual human brain. As the ultimate interest is in the free drug concentration at the CNS target si... |
PMC11666027 | core_pubmed_pmc | Optimization of meropenem continuous infusion based on Monte Carlo simulation integrating with degradation study | Optimization of meropenem continuous infusion based on Monte Carlo simulation integrating with degradation study Abstract Objective Meropenem degradation poses a challenge to continuous infusion (CI) implementation. However, data about the impact of degradation on the probability of target attainment (PTA) of meropenem... |
PMC11254990 | core_pubmed_pmc | Oral docetaxel plus encequidar – A pharmacokinetic model and evaluation against IV docetaxel | Oral docetaxel plus encequidar – A pharmacokinetic model and evaluation against IV docetaxel Abstract Abstract The development of optimized dosing regimens plays a crucial role in oncology drug development. This study focused on the population pharmacokinetic modelling and simulation of docetaxel, comparing the pharmac... |
PMC7266304 | core_pubmed_pmc | A Pharmacokinetic Drug Interaction Between Fimasartan and Linagliptin in Healthy Volunteers | A Pharmacokinetic Drug Interaction Between Fimasartan and Linagliptin in Healthy Volunteers Abstract Objective Fimasartan, an angiotensin II type 1 receptor blocker, and linagliptin, a dipeptidyl-peptidase-4 inhibitor, are frequently coadministered to treat patients with hypertension and diabetes, respectively. This st... |
PMC5315068 | core_pubmed_pmc | Phase I Study of Anti-GM2 Ganglioside Monoclonal Antibody BIW-8962 as Monotherapy in Patients with Previously Treated Multiple Myeloma | Phase I Study of Anti-GM2 Ganglioside Monoclonal Antibody BIW-8962 as Monotherapy in Patients with Previously Treated Multiple Myeloma Abstract Introduction BIW-8962 is a monoclonal antibody to GM2 ganglioside that shows preclinical activity towards multiple myeloma (MM) cell lines and in animal models bearing MM xenog... |
PMC12368495 | core_pubmed_pmc | Pharmacokinetic/pharmacodynamic parameters of teicoplanin for predicting clinical outcome of glycopeptide-susceptible Enterococcus faecium bacteraemia | Pharmacokinetic/pharmacodynamic parameters of teicoplanin for predicting clinical outcome of glycopeptide-susceptible Enterococcus faecium bacteraemia Abstract Abstract Objectives The objective of this study was to determine the pharmacokinetic/pharmacodynamic parameters of teicoplanin associated with optimal outcomes ... |
PMC8880227 | core_pubmed_pmc | Ayahuasca as a Decoction Applied to Human: Analytical Methods, Pharmacology and Potential Toxic Effects | Ayahuasca as a Decoction Applied to Human: Analytical Methods, Pharmacology and Potential Toxic Effects Abstract Ahyahuasca is a term commonly used to describe a decoction prepared by cooking the bark or crushed stems of the liana Banisteriopsis caapi (contains β -carbolines) alone or in combination with other plants, ... |
PMC12086182 | core_pubmed_pmc | Utilizing gentamicin concentrations to estimate glomerular filtration rate in intensive care unit patients | Utilizing gentamicin concentrations to estimate glomerular filtration rate in intensive care unit patients Abstract Abstract Estimated glomerular filtration rate (eGFR) based on creatinine (eGFR Creatinine ) or cystatin C (eGFR CystatinC ) require steady-state conditions and thus have limitations in intensive care unit... |
PMC10087075 | core_pubmed_pmc | Model‐informed precision dosing of teicoplanin for the rapid achievement of the target area under the concentration‐time curve: A simulation study | Model‐informed precision dosing of teicoplanin for the rapid achievement of the target area under the concentration‐time curve: A simulation study Abstract Abstract Teicoplanin, a glycopeptide antimicrobial, is recommended for therapeutic drug monitoring, but it remains unclear how to target the area under the concentr... |
PMC9887159 | core_pubmed_pmc | Investigating bile acid-mediated cholestatic drug-induced liver injury using a mechanistic model of multidrug resistance protein 3 (MDR3) inhibition | Investigating bile acid-mediated cholestatic drug-induced liver injury using a mechanistic model of multidrug resistance protein 3 (MDR3) inhibition Abstract Abstract Inhibition of the canalicular phospholipid floppase multidrug resistance protein 3 (MDR3) has been implicated in cholestatic drug-induced liver injury (D... |
PMC11521791 | core_pubmed_pmc | Natural killer cell engagers: From bi‐specific to tri‐specific and tetra‐specific engagers for enhanced cancer immunotherapy | Natural killer cell engagers: From bi‐specific to tri‐specific and tetra‐specific engagers for enhanced cancer immunotherapy Abstract Abstract Natural killer cell engagers (NKCEs) are a specialised subset of antibodies capable of simultaneously targeting endogenous NK cells and tumour cells, generating precise and effe... |
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