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PMC11913096 | core_pubmed_pmc | MBX 2109, A Once-Weekly Parathyroid Hormone Replacement Therapy Prodrug: Phase 1, First-In-Human, Randomized Trial | MBX 2109, A Once-Weekly Parathyroid Hormone Replacement Therapy Prodrug: Phase 1, First-In-Human, Randomized Trial Abstract Abstract Context Hypoparathyroidism denotes parathyroid hormone (PTH) deficiency and impaired mineral metabolism. MBX 2109, a novel prodrug yielding a biologically active PTH peptide agonist (PTH,... |
PMC7520416 | core_pubmed_pmc | Prior information for population pharmacokinetic and pharmacokinetic/pharmacodynamic analysis: overview and guidance with a focus on the NONMEM PRIOR subroutine | Prior information for population pharmacokinetic and pharmacokinetic/pharmacodynamic analysis: overview and guidance with a focus on the NONMEM PRIOR subroutine Abstract Abstract Abstract Population pharmacokinetic analysis is used to estimate pharmacokinetic parameters and their variability from concentration data. Du... |
PMC8188465 | core_pubmed_pmc | PBPK model reporting template for chemical risk assessment applications | PBPK model reporting template for chemical risk assessment applications Abstract Abstract Physiologically-based pharmacokinetic (PBPK) modeling analysis does not stand on its own for regulatory purposes but is a robust tool to support drug/chemical safety assessment. While the development of PBPK models have grown stea... |
PMC4171013 | core_pubmed_pmc | Characterization of a quantitative method to measure free proprotein convertase subtilisin/kexin type 9 in human serum | Characterization of a quantitative method to measure free proprotein convertase subtilisin/kexin type 9 in human serum Abstract Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease that plays an important role in the regulation of serum low-density lipoprotein (LDL) cholesterol by downreg... |
PMC4376748 | core_pubmed_pmc | Pharmacokinetics and Tolerability of Inhaled Umeclidinium and Vilanterol Alone and in Combination in Healthy Chinese Subjects: A Randomized, Open-Label, Crossover Trial | Pharmacokinetics and Tolerability of Inhaled Umeclidinium and Vilanterol Alone and in Combination in Healthy Chinese Subjects: A Randomized, Open-Label, Crossover Trial Abstract Inhaled umeclidinium (UMEC) and the combination of inhaled UMEC with vilanterol (UMEC/VI) are approved maintenance treatments for chronic obst... |
PMC8067465 | core_pubmed_pmc | Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance | Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance Abstract Abstract Candesartan cilexetil (CC), a prodrug and highly effective antihypertensive agent, is a poorly soluble (BCS Class II) drug with limited bioavailability. Here, we attem... |
PMC12653362 | core_pubmed_pmc | Digital Twins in Pediatric Infectious Diseases: Virtual Models for Personalized Management | Digital Twins in Pediatric Infectious Diseases: Virtual Models for Personalized Management Abstract Digital twins (DTs), virtual replicas that integrate mechanistic modeling with real-time clinical data, are emerging as powerful tools in healthcare with particular promise in pediatrics, where age-dependent physiology a... |
PMC11150559 | core_pubmed_pmc | Immunomodulation profile of the biosimilar trastuzumab MYL-1401O in a bioequivalence phase I study | Immunomodulation profile of the biosimilar trastuzumab MYL-1401O in a bioequivalence phase I study Abstract Abstract The initial Phase-I single centre, single dose, randomized, double-blind, cross-over study was planned to assess the pharmacokinetic and pharmacodynamic bioequivalence of the trastuzumab biosimilar (MYL-... |
PMC6590134 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Acetaminophen and Metabolites in Children After Cardiac Surgery With Cardiopulmonary Bypass | Population Pharmacokinetic Modeling of Acetaminophen and Metabolites in Children After Cardiac Surgery With Cardiopulmonary Bypass Abstract Abstract Children undergoing cardiac surgery often receive acetaminophen (paracetamol) as part of their postoperative pain treatment. To date, there is no information on the pharma... |
PMC8604822 | core_pubmed_pmc | Linking categorical models for prediction of pleasantness score using individual predictions of sweetness and creaminess: An advancement of categorical modeling | Linking categorical models for prediction of pleasantness score using individual predictions of sweetness and creaminess: An advancement of categorical modeling Abstract Abstract The aim of this work was to develop and evaluate approaches of linked categorical models using individual predictions of probability. A model... |
PMC11313909 | core_pubmed_pmc | Exploring the Potential of Oleanolic Acid Dimers–Cytostatic and Antioxidant Activities, Molecular Docking, and ADMETox Profile | Exploring the Potential of Oleanolic Acid Dimers–Cytostatic and Antioxidant Activities, Molecular Docking, and ADMETox Profile Abstract The presented work aimed to explore the potential of oleanolic acid dimers (OADs): their cytostatic and antioxidant activities, molecular docking, pharmacokinetics, and ADMETox profile... |
PMC9576439 | core_pubmed_pmc | In Silico Identification of New Anti-SARS-CoV-2 Main Protease (M pro ) Molecules with Pharmacokinetic Properties from Natural Sources Using Molecular Dynamics (MD) Simulations and Hierarchical Virtual Screening | In Silico Identification of New Anti-SARS-CoV-2 Main Protease (M pro ) Molecules with Pharmacokinetic Properties from Natural Sources Using Molecular Dynamics (MD) Simulations and Hierarchical Virtual Screening Abstract Infectious agents such as SARS-CoV, MERS-CoV, and SARS-CoV-2 have emerged in recent years causing ep... |
PMC11919258 | core_pubmed_pmc | Analysis of C4 Concentrations to Predict Impact of Patient‐Reported Diarrhea Associated With the Ileal Bile Acid Transporter Inhibitor Linerixibat | Analysis of C4 Concentrations to Predict Impact of Patient‐Reported Diarrhea Associated With the Ileal Bile Acid Transporter Inhibitor Linerixibat Abstract ABSTRACT Linerixibat, an ileal bile acid transporter (IBAT) inhibitor, is being evaluated for the treatment of pruritus in primary biliary cholangitis (PBC). Diarrh... |
PMC4895289 | core_pubmed_pmc | Reviewing 15 years of experience with sirolimus | Reviewing 15 years of experience with sirolimus Abstract Abstract Here, we review 15 years of clinical use of sirolimus in our transplant center, in context with the developing immunosuppressive strategies use worldwide. The majority of studies were conducted in de novo kidney transplant recipients, using sirolimus (SR... |
PMC8868220 | core_pubmed_pmc | Curcumin: Biological Activities and Modern Pharmaceutical Forms | Curcumin: Biological Activities and Modern Pharmaceutical Forms Abstract Curcumin (1,7-bis-(4-hydroxy-3-methoxyphenyl)-hepta-1,6-diene-3,5-dione) is a natural lipophilic polyphenol that exhibits significant pharmacological effects in vitro and in vivo through various mechanisms of action. Numerous studies have identifi... |
PMC10740541 | core_pubmed_pmc | Comparative Meropenem Pharmacodynamics and Emergence of Resistance against Carbapenem-Susceptible Non-Carbapenemase-Producing and Carbapenemase-Producing Enterobacterales: A Pharmacodynamic Study in a Hollow-Fiber Infection Model | Comparative Meropenem Pharmacodynamics and Emergence of Resistance against Carbapenem-Susceptible Non-Carbapenemase-Producing and Carbapenemase-Producing Enterobacterales: A Pharmacodynamic Study in a Hollow-Fiber Infection Model Abstract Resistance to carbapenems has become a problem due to Klebsiella pneumoniae ( K. ... |
PMC5951219 | core_pubmed_pmc | Pharmacokinetic comparison of a fixed-dose combination versus concomitant administration of fimasartan, amlodipine, and rosuvastatin using partial replicated design in healthy adult subjects | Pharmacokinetic comparison of a fixed-dose combination versus concomitant administration of fimasartan, amlodipine, and rosuvastatin using partial replicated design in healthy adult subjects Abstract Objective The aim of this study was to compare the pharmacokinetics (PK) and safety profiles of a fixed-dose combination... |
PMC11054815 | core_pubmed_pmc | Cryo-Milled β-Glucan Nanoparticles for Oral Drug Delivery | Cryo-Milled β-Glucan Nanoparticles for Oral Drug Delivery Abstract Gemcitabine is a nucleoside analog effective against a number of cancers. However, it has an oral bioavailability of less than 10%, due to its high hydrophilicity and low permeability through the intestinal epithelium. Therefore, the aim of this project... |
PMC12782866 | core_pubmed_pmc | Preclinical Pharmacological and Toxicological Evaluation of SB5794, a Novel Aryl Hydrocarbon Receptor Modulator on the Kynurenine–AhR Axis | Preclinical Pharmacological and Toxicological Evaluation of SB5794, a Novel Aryl Hydrocarbon Receptor Modulator on the Kynurenine–AhR Axis Abstract Abstract Conventional aryl hydrocarbon receptor (AhR) antagonists, which play a critical role in modulating tumor immune evasion, have shown limited clinical translation du... |
PMC6201861 | core_pubmed_pmc | Generation and characterization of novel recombinant anti-hERG1 scFv antibodies for cancer molecular imaging | Generation and characterization of novel recombinant anti-hERG1 scFv antibodies for cancer molecular imaging Abstract Abstract Modern molecular imaging techniques have greatly improved tumor detection and post-treatment follow-up of cancer patients. In this context, antibody-based imaging is rapidly becoming the gold s... |
PMC10963774 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic evaluation study of etomidate: a randomized, open-label, 2-period crossover study in healthy Chinese subjects | Pharmacokinetic and pharmacodynamic evaluation study of etomidate: a randomized, open-label, 2-period crossover study in healthy Chinese subjects Abstract Etomidate is a sedative and hypnotic drug through intravenous administration that act on the central nervous system through GABA (Gamma-Amino Butyric Acid) receptors... |
PMC12144343 | core_pubmed_pmc | Predicting drug–drug interactions and optimal dosing of betrixaban with physiologically based pharmacokinetic modeling in patients with renal impairment who were coadministered with P-glycoprotein inhibitors | Predicting drug–drug interactions and optimal dosing of betrixaban with physiologically based pharmacokinetic modeling in patients with renal impairment who were coadministered with P-glycoprotein inhibitors Abstract Objective To optimize dosing adjustments in patients with renal impairment who were coadministered with... |
PMC7757978 | core_pubmed_pmc | A Randomized, Open, Single-Centre, Crossed Study of the Effect of Food on the Pharmacokinetics of One Oral Dose of Alflutinib Mesylate Tablets (AST2818) in Healthy Male Subjects | A Randomized, Open, Single-Centre, Crossed Study of the Effect of Food on the Pharmacokinetics of One Oral Dose of Alflutinib Mesylate Tablets (AST2818) in Healthy Male Subjects Abstract Abstract The aim of the study was to study the PK of AST2818 tablets after one oral dose in healthy male subjects on an empty stomach... |
PMC5404562 | core_pubmed_pmc | Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine | Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine Abstract ABSTRACT Intermittent preventive treatment (IPT) is used to reduce malaria morbidity and mortality, especially in vulnerable groups such as children and pregnant women. IPT with the fixed dose combination o... |
PMC7064600 | core_pubmed_pmc | Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development | Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development Abstract Abstract Emerging drug resistance and high-attrition rates in early and late stage drug development necessitate accelerated development of antimalarial compounds. However, systematic and... |
PMC12899163 | core_pubmed_pmc | Combined Nanoparticle-Based Delivery of Estrogens and Raloxifen in Postmenopausal Osteoporosis | Combined Nanoparticle-Based Delivery of Estrogens and Raloxifen in Postmenopausal Osteoporosis Abstract Osteoporosis (OP) is a common chronic disease that significantly increases the risk of bone fractures. Pharmacotherapy uses, among others, 17beta-estradiol (E2), which has been replaced in recent years by raloxifene ... |
PMC12706401 | core_pubmed_pmc | Comparative Analysis of Isavuconazole DDIs With Other Azole Antifungal Drugs and PBPK Model‐Informed Dosing Recommendations for Anticancer Drugs | Comparative Analysis of Isavuconazole DDIs With Other Azole Antifungal Drugs and PBPK Model‐Informed Dosing Recommendations for Anticancer Drugs Abstract ABSTRACT Isavuconazole is a broad‐spectrum triazole approved for the treatment of invasive aspergillosis or mucormycosis in adults and children aged ≥ 1 year. Current... |
PMC6151385 | core_pubmed_pmc | Simultaneous Determination of Seven Phenolic Acids in Rat Plasma Using UHPLC-ESI-MS/MS after Oral Administration of Echinacea purpurea Extract | Simultaneous Determination of Seven Phenolic Acids in Rat Plasma Using UHPLC-ESI-MS/MS after Oral Administration of Echinacea purpurea Extract Abstract Abstract A rapid and sensitive Ultra High Performance Liquid Chromatography Electrospray Ionization Tandem Mass Spectrometry (UHPLC-ESI-MS/MS) method was developed and ... |
PMC6058601 | core_pubmed_pmc | Improved lymphatic targeting: effect and mechanism of synthetic borneol on lymph node uptake of 7-ethyl-10-hydroxycamptothecin nanoliposomes following subcutaneous administration | Improved lymphatic targeting: effect and mechanism of synthetic borneol on lymph node uptake of 7-ethyl-10-hydroxycamptothecin nanoliposomes following subcutaneous administration Abstract Abstract Borneol as a penetration enhancer is widely used in guiding other components through the biological barrier into the target... |
PMC6201082 | core_pubmed_pmc | Population Pharmacokinetics of Tafenoquine, a Novel Antimalarial | Population Pharmacokinetics of Tafenoquine, a Novel Antimalarial Abstract Tafenoquine is a novel 8-aminoquinoline antimalarial drug recently approved by the U.S. Food and Drug Administration (FDA) for the radical cure of acute Plasmodium vivax malaria, which is the first new treatment in almost 60 years. KEYWORDS: tafe... |
PMC12722991 | core_pubmed_pmc | A phase Ib/II study of modakafusp alfa alone and in combination with pembrolizumab in patients with advanced or metastatic solid tumors | A phase Ib/II study of modakafusp alfa alone and in combination with pembrolizumab in patients with advanced or metastatic solid tumors Abstract Background Modakafusp alfa is a novel immunocytokine comprising two attenuated interferon-α2b molecules fused to an anti-CD38 IgG4 monoclonal antibody. Modakafusp alfa has sho... |
PMC7559546 | core_pubmed_pmc | Pharmacokinetic Comparison of Three Different Administration Routes for Topotecan Hydrochloride in Rats | Pharmacokinetic Comparison of Three Different Administration Routes for Topotecan Hydrochloride in Rats Abstract Abstract Topotecan is actively used in clinic, with its primary use being in treatment of various types of cancer. The approved administration routes are oral and intravenous. The purpose of this study was t... |
PMC11677465 | core_pubmed_pmc | Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization | Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization Abstract Abstract Background: Bromodomain and extra-terminal (BET) proteins are critical regulators of gene transcription, as they recognize acetylated lysine residues. The BD1 bromodomain of BRD4, a memb... |
PMC12323519 | core_pubmed_pmc | Nemvaleukin alfa monotherapy in patients with advanced melanoma and renal cell carcinoma: results from the phase 1/2 non-randomized ARTISTRY-1 trial | Nemvaleukin alfa monotherapy in patients with advanced melanoma and renal cell carcinoma: results from the phase 1/2 non-randomized ARTISTRY-1 trial Abstract Abstract Background Despite improved outcomes with immune checkpoint inhibitors (ICIs) and their combinations in advanced solid tumors, a subset of patients remai... |
PMC3415771 | core_pubmed_pmc | Monitoring imatinib plasma concentrations in chronic myeloid leukemia | Monitoring imatinib plasma concentrations in chronic myeloid leukemia Abstract Abstract Imatinib has proved to be effective in the treatment of chronic myeloid leukemia, but plasma levels above 1,000 ng/mL must be achieved to optimize activity. Therapeutic drug monitoring of imatinib is useful for patients that do not ... |
PMC10023024 | core_pubmed_pmc | Effect of Various Dosing Schedules on the Pharmacokinetics of Oral Semaglutide: A Randomised Trial in Healthy Subjects | Effect of Various Dosing Schedules on the Pharmacokinetics of Oral Semaglutide: A Randomised Trial in Healthy Subjects Abstract Background Prescribing information instructs taking oral semaglutide (a glucagon-like peptide-1 analogue) in the fasting state, followed by a post-dose fasting period of ≥ 30 min. This trial c... |
PMC8596765 | core_pubmed_pmc | Effect of Upadacitinib on the Pharmacokinetics of Rosuvastatin or Atorvastatin in Healthy Subjects | Effect of Upadacitinib on the Pharmacokinetics of Rosuvastatin or Atorvastatin in Healthy Subjects Abstract Abstract This phase 1, 2‐part, 2‐period, open‐label, drug‐drug interaction study evaluated the potential for pharmacokinetic interactions between upadacitinib and rosuvastatin, an organic anion transporting polyp... |
PMC6709420 | core_pubmed_pmc | A Minimal Physiologically‐Based Pharmacokinetic Model for Tacrolimus in Living‐Donor Liver Transplantation: Perspectives Related to Liver Regeneration and the cytochrome P450 3A5 (CYP3A5) Genotype | A Minimal Physiologically‐Based Pharmacokinetic Model for Tacrolimus in Living‐Donor Liver Transplantation: Perspectives Related to Liver Regeneration and the cytochrome P450 3A5 (CYP3A5) Genotype Abstract Abstract In adult patients after living‐donor liver transplantation, postoperative days and the cytochrome P450 3A... |
PMC7172977 | core_pubmed_pmc | Stem cell-based Lung-on-Chips: The best of both worlds? ☆ | Stem cell-based Lung-on-Chips: The best of both worlds? ☆ Abstract Pathologies of the respiratory system such as lung infections, chronic inflammatory lung diseases, and lung cancer are among the leading causes of morbidity and mortality, killing one in six people worldwide. Development of more effective treatments is ... |
PMC11958634 | core_pubmed_pmc | Computational discovery of natural inhibitors targeting enterovirus D68 3C protease using molecular docking pharmacokinetics and dynamics simulations | Computational discovery of natural inhibitors targeting enterovirus D68 3C protease using molecular docking pharmacokinetics and dynamics simulations Abstract Enterovirus D68 (EV-D68) is a significant global health threat, responsible for severe respiratory and neurological complications, with no FDA-approved antiviral... |
PMC12487479 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics of Dexmedetomidine two-phase flow atomization in healthy subjects: a randomized, parallel study | Safety, pharmacokinetics, and pharmacodynamics of Dexmedetomidine two-phase flow atomization in healthy subjects: a randomized, parallel study Abstract Abstract Background In this study, we aimed to compare the sedative effects, pharmacokinetics (PKs), and safety of dexmedetomidine (DEX) administered using a two-phase ... |
PMC12286339 | core_pubmed_pmc | TunR2, a novel mode-of-action tunicamycin-type antibiotic: Pharmacokinetics in C57BL/6 mouse and Holstein cattle | TunR2, a novel mode-of-action tunicamycin-type antibiotic: Pharmacokinetics in C57BL/6 mouse and Holstein cattle Abstract We have investigated the pharmacokinetics of TunR2, a modified tunicamycin-type antibiotic, in mice and cattle. TunR2 has previously been shown to be effective in a mycobacterial disease model using... |
PMC7917791 | core_pubmed_pmc | Circulation of Fluorescently Labelled Phage in a Murine Model | Circulation of Fluorescently Labelled Phage in a Murine Model Abstract Abstract Interactions between bacteriophages and mammals strongly affect possible applications of bacteriophages. This has created a need for tools that facilitate studies of phage circulation and deposition in tissues. Here, we propose red fluoresc... |
PMC5388374 | core_pubmed_pmc | Phase I Dose‐Escalation Study of Pilaralisib (SAR245408, XL147) in Combination with Paclitaxel and Carboplatin in Patients with Solid Tumors | Phase I Dose‐Escalation Study of Pilaralisib (SAR245408, XL147) in Combination with Paclitaxel and Carboplatin in Patients with Solid Tumors Abstract Abstract Lessons Learned. Despite involvement of PI3K pathway activation in tumorigenesis of solid tumors, single‐agent PI3K inhibitors have shown modest clinical activit... |
PMC2933032 | core_pubmed_pmc | Biodistribution and radiation dosimetry of 11 C-labelled docetaxel in cancer patients | Biodistribution and radiation dosimetry of 11 C-labelled docetaxel in cancer patients Abstract Abstract Purpose Docetaxel is an important chemotherapeutic agent used for the treatment of several cancer types. As radiolabelled anticancer agents provide a potential means for personalized treatment planning, docetaxel was... |
PMC9692530 | core_pubmed_pmc | Analysis of Galangin and Its In Vitro/In Vivo Metabolites via Ultra-High-Performance Liquid Chromatography/Quadrupole Time-of-Flight Mass Spectrometry | Analysis of Galangin and Its In Vitro/In Vivo Metabolites via Ultra-High-Performance Liquid Chromatography/Quadrupole Time-of-Flight Mass Spectrometry Abstract Galangin, a naturally available flavonoid, induces a variety of pharmacological activities and biological effects via several mechanisms. However, in vivo metab... |
PMC11292616 | core_pubmed_pmc | Usefulness of dalbavancin in early discharge and nonhospitalization. It’s time to throw your heart over the obstacle? | Usefulness of dalbavancin in early discharge and nonhospitalization. It’s time to throw your heart over the obstacle? Abstract ABSTRACT Introduction: Dalbavancin is a semisynthetic lipoglycopeptide long-acting antibiotic approved for the treatment of acute bacterial skin and skin structure infections (ABSSSIs). Its fea... |
PMC7765183 | core_pubmed_pmc | The Therapeutic Efficacy of Dendrimer and Micelle Formulations for Breast Cancer Treatment | The Therapeutic Efficacy of Dendrimer and Micelle Formulations for Breast Cancer Treatment Abstract Abstract Breast cancer is among the most common types of cancer in women and it is the cause of a high rate of mortality globally. The use of anticancer drugs is the standard treatment approach used for this type of canc... |
PMC6966871 | core_pubmed_pmc | First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer | First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer Abstract Background BPI-9016M is a novel small-molecule inhibitor that simultaneously targets both c-Met and AXL tyrosine kinases. This phase I study aimed to determine the maximum tolerated dose (MTD), safe... |
PMC12597483 | core_pubmed_pmc | Effects of Pemafibrate on Cholesterol Synthesis and Absorption: a Post-Hoc Subgroup Analysis of a Phase 2 Clinical Trial | Effects of Pemafibrate on Cholesterol Synthesis and Absorption: a Post-Hoc Subgroup Analysis of a Phase 2 Clinical Trial Abstract Aim: Recently, we reported that a pemafibrate extended-release (XR) formulation lowered low-density lipoprotein cholesterol (LDL-C) and cholesterol synthesis and absorption markers in a phas... |
PMC12034656 | core_pubmed_pmc | Acute cannabis intoxication among the paediatric population | Acute cannabis intoxication among the paediatric population Abstract Abstract This narrative review synthesizes the toxicological, clinical and medico-legal aspects of paediatric cannabis intoxication. By providing a comprehensive overview, it aims to inform future research, guide policymaking, and enhance clinical and... |
PMC8559552 | core_pubmed_pmc | Mechanistic Modeling of Placental Drug Transfer in Humans: How Do Differences in Maternal/Fetal Fraction of Unbound Drug and Placental Influx/Efflux Transfer Rates Affect Fetal Pharmacokinetics? | Mechanistic Modeling of Placental Drug Transfer in Humans: How Do Differences in Maternal/Fetal Fraction of Unbound Drug and Placental Influx/Efflux Transfer Rates Affect Fetal Pharmacokinetics? Abstract Background: While physiologically based pharmacokinetic (PBPK) models generally predict pharmacokinetics in pregnant... |
PMC9326888 | core_pubmed_pmc | Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review | Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review Abstract Abstract This review addressed drug interactions precipitated by fruit juices other than grapefruit juice based on randomized controlled trials (RCTs). Literature was identified by searching PubMed, Cochrane Libra... |
PMC12802879 | core_pubmed_pmc | Enhanced antimycobacterial efficacy of simulated inhaled clofazimine versus oral clofazimine in combination with azithromycin and ethambutol in a hollow-fiber system | Enhanced antimycobacterial efficacy of simulated inhaled clofazimine versus oral clofazimine in combination with azithromycin and ethambutol in a hollow-fiber system Abstract Abstract Background and objectives Treatment outcomes in Mycobacterium avium complex pulmonary disease may be improved by adding clofazimine, ins... |
PMC5712296 | core_pubmed_pmc | Pretargeting of internalizing trastuzumab and cetuximab with a 18 F-tetrazine tracer in xenograft models | Pretargeting of internalizing trastuzumab and cetuximab with a 18 F-tetrazine tracer in xenograft models Abstract Abstract Background Pretargeting-based approaches are being investigated for radioimmunoimaging and therapy applications to reduce the effective radiation burden to the patient. To date, only a few studies ... |
PMC7866126 | core_pubmed_pmc | DNA-Binding Anticancer Drugs: One Target, Two Actions | DNA-Binding Anticancer Drugs: One Target, Two Actions Abstract Abstract Amsacrine, an anticancer drug first synthesised in 1970 by Professor Cain and colleagues, showed excellent preclinical activity and underwent clinical trial in 1978 under the auspices of the US National Cancer Institute, showing activity against ac... |
PMC12771989 | core_pubmed_pmc | Therapeutic Drug Monitoring and Point-of-Care Technologies: Opportunities and Current Challenges | Therapeutic Drug Monitoring and Point-of-Care Technologies: Opportunities and Current Challenges Abstract Abstract Background: This review re-evaluates therapeutic drug monitoring (TDM) by comparing the current analytical and subsequent clinical interpretation capabilities of hospital or community medical laboratories ... |
PMC11796441 | core_pubmed_pmc | Oleanolic Acid Cubic Liquid Crystal Nanoparticle-Based Thermosensitive Gel Attenuates Depression Symptoms in Chronic Unpredictable Mild Stress Rats | Oleanolic Acid Cubic Liquid Crystal Nanoparticle-Based Thermosensitive Gel Attenuates Depression Symptoms in Chronic Unpredictable Mild Stress Rats Abstract Abstract Purpose Major depressive disorder (MDD) is a global health concern. Studies have demonstrated that oleanolic acid (OA) has a regulatory effect on MDD. How... |
PMC10472989 | core_pubmed_pmc | Pharmacokinetics and tolerability of multiple‐day oral dosing of mycophenolate mofetil in healthy horses | Pharmacokinetics and tolerability of multiple‐day oral dosing of mycophenolate mofetil in healthy horses Abstract Abstract Background Additional efficacious immunomodulatory treatment is needed for the management of immune‐mediated disease in horses. Mycophenolate mofetil (MMF) is an immunosuppressive drug that warrant... |
PMC12312149 | core_pubmed_pmc | Data-Driven Prediction of Nanoparticle Biodistribution from Physicochemical Descriptors | Data-Driven Prediction of Nanoparticle Biodistribution from Physicochemical Descriptors Abstract Abstract Nanoparticles have gained significant attention in biomedicine, electronics, and environmental science due to their unique physicochemical properties, which critically influence their absorption, distribution, meta... |
PMC4835132 | core_pubmed_pmc | Clinically relevant genetic variants of drug-metabolizing enzyme and transporter genes detected in Thai children and adolescents with autism spectrum disorder | Clinically relevant genetic variants of drug-metabolizing enzyme and transporter genes detected in Thai children and adolescents with autism spectrum disorder Abstract Single-nucleotide polymorphisms (SNPs) among drug-metabolizing enzymes and transporters (DMETs) influence the pharmacokinetic profile of drugs and exhib... |
PMC8207516 | core_pubmed_pmc | Pharmacokinetics, Immunogenicity and Safety Study for SHR-1309 Injection and Perjeta® in Healthy Chinese Male Volunteers | Pharmacokinetics, Immunogenicity and Safety Study for SHR-1309 Injection and Perjeta® in Healthy Chinese Male Volunteers Abstract Objectives: Pertuzumab is a monoclonal antibody for the treatment of breast cancer. The aim of this study was to compare the pharmacokinetics, immunogenicity and safety of the test preparati... |
PMC7478617 | core_pubmed_pmc | Pharmacokinetics and bioequivalence assessment of optimized directly compressible Aceclofenac (100 mg) tablet formulation in healthy human subjects | Pharmacokinetics and bioequivalence assessment of optimized directly compressible Aceclofenac (100 mg) tablet formulation in healthy human subjects Abstract Abstract The aim of the study was to determine the various pharmacokinetic parameters of the newly developed cost-effective aceclofenac 100 mg tablet formulation (... |
PMC6524478 | core_pubmed_pmc | In vitro activity of the novel oral antimicrobial SMT-571, with a new mechanism of action, against MDR and XDR Neisseria gonorrhoeae : future treatment option for gonorrhoea? | In vitro activity of the novel oral antimicrobial SMT-571, with a new mechanism of action, against MDR and XDR Neisseria gonorrhoeae : future treatment option for gonorrhoea? Abstract Abstract Background Lack of effective treatment of gonorrhoea due to increasing antimicrobial resistance in Neisseria gonorrhoeae is a s... |
PMC3595976 | core_pubmed_pmc | Comparison of the systemic bioavailability of mometasone furoate after oral inhalation from a mometasone furoate/formoterol fumarate metered-dose inhaler versus a mometasone furoate dry-powder inhaler in patients with chronic obstructive pulmonary disease | Comparison of the systemic bioavailability of mometasone furoate after oral inhalation from a mometasone furoate/formoterol fumarate metered-dose inhaler versus a mometasone furoate dry-powder inhaler in patients with chronic obstructive pulmonary disease Abstract Background Coadministration of mometasone furoate (MF) ... |
PMC7081093 | core_pubmed_pmc | An Exploratory Phase IIa Study of the PPAR delta/gamma Agonist T3D-959 Assessing Metabolic and Cognitive Function in Subjects with Mild to Moderate Alzheimer’s Disease | An Exploratory Phase IIa Study of the PPAR delta/gamma Agonist T3D-959 Assessing Metabolic and Cognitive Function in Subjects with Mild to Moderate Alzheimer’s Disease Abstract Abstract Background: T3D-959 is a chemically unique, brain penetrant, dual PPAR delta/gamma agonist with 15-fold higher PPAR delta selectivity.... |
PMC9290462 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of BI 705564, a highly selective, covalent inhibitor of Bruton's tyrosine kinase, in Phase I clinical trials in healthy volunteers | Safety, pharmacokinetics and pharmacodynamics of BI 705564, a highly selective, covalent inhibitor of Bruton's tyrosine kinase, in Phase I clinical trials in healthy volunteers Abstract Abstract Aims To evaluate the safety, pharmacokinetics and pharmacodynamics of single‐ and multiple‐rising doses (MRDs) of BI 705564 a... |
PMC11340219 | core_pubmed_pmc | Effect of chronic kidney disease on adverse drug reactions to anti-tubercular treatment: a retrospective cohort study | Effect of chronic kidney disease on adverse drug reactions to anti-tubercular treatment: a retrospective cohort study Abstract Abstract Introduction Patients with chronic kidney disease (CKD) are at increased risk of developing tuberculosis (TB). These patients may also be at higher risk of developing antitubercular tr... |
PMC8111447 | core_pubmed_pmc | SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer | SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer Abstract SH-1028 is an irreversible third-generation EGFR TKI. Both SH-1028 and osimertinib have a pyrimidine structure (a typical mutant-selective EGFR TKI structure). Compared with osimertinib, SH-102... |
PMC6153505 | core_pubmed_pmc | Pharmacokinetics of ferric pyrophosphate citrate administered via dialysate and intravenously to pediatric patients on chronic hemodialysis | Pharmacokinetics of ferric pyrophosphate citrate administered via dialysate and intravenously to pediatric patients on chronic hemodialysis Abstract Abstract Background Iron deficiency is a common cause of anemia in pediatric patients with hemodialysis-dependent chronic kidney disease (CKD-5HD). Ferric pyrophosphate ci... |
PMC9697187 | core_pubmed_pmc | An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats | An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats Abstract Feline infectious peritonitis (FIP) is a fatal disease of cats that currently lacks licensed and affor... |
PMC10848080 | core_pubmed_pmc | Piperine improves levodopa availability in the 6‐OHDA ‐lesioned rat model of Parkinson's disease by suppressing gut bacterial tyrosine decarboxylase | Piperine improves levodopa availability in the 6‐OHDA ‐lesioned rat model of Parkinson's disease by suppressing gut bacterial tyrosine decarboxylase Abstract Abstract Aim Tyrosine decarboxylase (TDC) presented in the gut‐associated strain Enterococcus faecalis can convert levodopa (L‐dopa) into dopamine (DA), and its i... |
PMC7526808 | core_pubmed_pmc | Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison for a 3-Day Loading Dose Regimen and 15-Day Steady-State Administration of SUBA-Itraconazole and Conventional Itraconazole Capsules in Healthy Adults | Open-Label Crossover Oral Bioequivalence Pharmacokinetics Comparison for a 3-Day Loading Dose Regimen and 15-Day Steady-State Administration of SUBA-Itraconazole and Conventional Itraconazole Capsules in Healthy Adults Abstract Super bioavailability (SUBA) itraconazole (S-ITZ), which releases drug in the duodenum, and ... |
PMC12889036 | core_pubmed_pmc | Efficacy of cefiderocol in murine models of ventilator-associated pneumonia caused by carbapenem-resistant non-fermenting Gram-negative bacilli, with pharmacokinetic evaluation | Efficacy of cefiderocol in murine models of ventilator-associated pneumonia caused by carbapenem-resistant non-fermenting Gram-negative bacilli, with pharmacokinetic evaluation Abstract ABSTRACT Ventilator-associated pneumonia (VAP) caused by carbapenem-resistant non-fermenting Gram-negative bacilli poses a serious cli... |
PMC10067098 | core_pubmed_pmc | Phase 1 study of DS‐1205c combined with gefitinib for EGFR mutation‐positive non‐small cell lung cancer | Phase 1 study of DS‐1205c combined with gefitinib for EGFR mutation‐positive non‐small cell lung cancer Abstract Abstract Background Tyrosine kinase inhibitors (TKIs) are effective for the treatment of non‐small cell lung cancer (NSCLC) patients with activating mutations of the epidermal growth factor receptor (EGFR), ... |
PMC10676321 | core_pubmed_pmc | Human Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASC42, a Novel Farnesoid X Receptor Agonist | Human Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASC42, a Novel Farnesoid X Receptor Agonist Abstract Background ASC42 is a non-steroidal farnesoid X receptor agonist currently in clinical development for chronic liver diseases, such as nonalcoholic fatty liver disease/nonalcoholic steatohepatitis ... |
PMC3364551 | core_pubmed_pmc | Microglial KCa3.1 Channels as a Potential Therapeutic Target for Alzheimer's Disease | Microglial KCa3.1 Channels as a Potential Therapeutic Target for Alzheimer's Disease Abstract There exists an urgent need for new target discovery to treat Alzheimer's disease (AD); however, recent clinical trials based on anti-A β and anti-inflammatory strategies have yielded disappointing results. To expedite new dru... |
PMC7008059 | core_pubmed_pmc | An HIV-infected Patient with No Serious Adverse Events after Overdosing on Raltegravir | An HIV-infected Patient with No Serious Adverse Events after Overdosing on Raltegravir Abstract Abstract Patients with HIV infection represent a high-risk group for medication overdose because of the high frequency of complicating psychiatric disorders. Raltegravir is well-known for its low frequency of adverse effects... |
PMC3458211 | core_pubmed_pmc | Quantification of rifampicin in human plasma and cerebrospinal fluid by a highly sensitive and rapid liquid chromatographic–tandem mass spectrometric method | Quantification of rifampicin in human plasma and cerebrospinal fluid by a highly sensitive and rapid liquid chromatographic–tandem mass spectrometric method Abstract Abstract A highly sensitive and rapid liquid chromatography tandem mass spectrometry (LC–MS/MS) method has been developed to measure the levels of the ant... |
PMC8758560 | core_pubmed_pmc | Repurposing Artemisinin and its Derivatives as Anticancer Drugs: A Chance or Challenge? | Repurposing Artemisinin and its Derivatives as Anticancer Drugs: A Chance or Challenge? Abstract Abstract Cancer has become a global health problem, accounting for one out of six deaths. Despite the recent advances in cancer therapy, there is still an ever-growing need for readily accessible new therapies. The process ... |
PMC5133431 | core_pubmed_pmc | Efficacy and Safety of High-Dose Ivermectin for Reducing Malaria Transmission (IVERMAL): Protocol for a Double-Blind, Randomized, Placebo-Controlled, Dose-Finding Trial in Western Kenya | Efficacy and Safety of High-Dose Ivermectin for Reducing Malaria Transmission (IVERMAL): Protocol for a Double-Blind, Randomized, Placebo-Controlled, Dose-Finding Trial in Western Kenya Abstract Abstract Background Innovative approaches are needed to complement existing tools for malaria elimination. Ivermectin is a br... |
PMC9469700 | core_pubmed_pmc | Population pharmacokinetic analysis of etrolizumab in patients with moderately‐to‐severely active ulcerative colitis | Population pharmacokinetic analysis of etrolizumab in patients with moderately‐to‐severely active ulcerative colitis Abstract Abstract Etrolizumab is an IgG1‐humanized monoclonal antibody that specifically targets the β7 subunit of α4β7 and α4Eβ7 integrins, and it has been evaluated for the treatment of moderately‐to‐s... |
PMC3660130 | core_pubmed_pmc | Profile of once-daily zonisamide as monotherapy for treatment of partial seizures in adults | Profile of once-daily zonisamide as monotherapy for treatment of partial seizures in adults Abstract Epilepsy is one of the most common neurologic disorders, affecting about 50 million people around the world. It is recognized that around 50% of patients with newly diagnosed epilepsy become seizure-free with the first ... |
PMC11681640 | core_pubmed_pmc | Phase 1 study of AYP-101 (soybean phosphatidylcholine): safety, pharmacokinetics, and lipid profile effects for reducing submental fat | Phase 1 study of AYP-101 (soybean phosphatidylcholine): safety, pharmacokinetics, and lipid profile effects for reducing submental fat Abstract Background Excessive submental fat under the chin is a known aesthetic concern because of its negative impact on facial appearance and psychological well-being. AYP-101 is a ne... |
PMC9028714 | core_pubmed_pmc | Impact of the Genotype and Phenotype of CYP3A and P-gp on the Apixaban and Rivaroxaban Exposure in a Real-World Setting | Impact of the Genotype and Phenotype of CYP3A and P-gp on the Apixaban and Rivaroxaban Exposure in a Real-World Setting Abstract Abstract Apixaban and rivaroxaban are the two most prescribed direct factor Xa inhibitors. With the increased use of DOACs in real-world settings, safety and efficacy concerns have emerged, p... |
PMC11015172 | core_pubmed_pmc | Determining the exposure of maternal medicines through breastfeeding: the UmbrelLACT study protocol—a contribution from the ConcePTION project | Determining the exposure of maternal medicines through breastfeeding: the UmbrelLACT study protocol—a contribution from the ConcePTION project Abstract Abstract Introduction Breastfeeding is beneficial for the health of the mother and child. However, at least 50% of postpartum women need pharmacotherapy, and this numbe... |
PMC5340925 | core_pubmed_pmc | Use of a Novel Artificial Intelligence Platform on Mobile Devices to Assess Dosing Compliance in a Phase 2 Clinical Trial in Subjects With Schizophrenia | Use of a Novel Artificial Intelligence Platform on Mobile Devices to Assess Dosing Compliance in a Phase 2 Clinical Trial in Subjects With Schizophrenia Abstract Background Accurately monitoring and collecting drug adherence data can allow for better understanding and interpretation of the outcomes of clinical trials. ... |
PMC4235294 | core_pubmed_pmc | Analysis of biomarker utility using a PBPK/PD model for carbaryl | Analysis of biomarker utility using a PBPK/PD model for carbaryl Abstract Abstract There are many types of biomarkers; the two common ones are biomarkers of exposure and biomarkers of effect. The utility of a biomarker for estimating exposures or predicting risks depends on the strength of the correlation between bioma... |
PMC4212661 | core_pubmed_pmc | Time Course of the Changes in Novel Trioxane Antimalarial 99/411 Pharmacokinetics upon Antiepileptic Drugs Co-Administration in SD Rats | Time Course of the Changes in Novel Trioxane Antimalarial 99/411 Pharmacokinetics upon Antiepileptic Drugs Co-Administration in SD Rats Abstract Abstract Objective . The study aimed to evaluate the influences of coadministration of antiepileptic drugs (AEDs) on an antimalarial candidate 99/411 pharmacokinetic (PK) prof... |
PMC9740939 | core_pubmed_pmc | A Network-Pharmacology-Combined Integrated Pharmacokinetic Strategy to Investigate the Mechanism of Potential Liver Injury due to Polygonum multiflorum | A Network-Pharmacology-Combined Integrated Pharmacokinetic Strategy to Investigate the Mechanism of Potential Liver Injury due to Polygonum multiflorum Abstract Polygonum multiflorum (PM) has been used as a tonic and anti-aging remedy for centuries in Asian countries. However, its application in the clinic has been hin... |
PMC10449733 | core_pubmed_pmc | Predicting [ 177 Lu]Lu-HA-DOTATATE kidney and tumor accumulation based on [ 68 Ga]Ga-HA-DOTATATE diagnostic imaging using semi-physiological population pharmacokinetic modeling | Predicting [ 177 Lu]Lu-HA-DOTATATE kidney and tumor accumulation based on [ 68 Ga]Ga-HA-DOTATATE diagnostic imaging using semi-physiological population pharmacokinetic modeling Abstract Abstract Background Prediction of [ 177 Lu]Lu-HA-DOTATATE kidney and tumor uptake based on diagnostic [ 68 Ga]Ga-HA-DOTATATE imaging w... |
PMC10933797 | core_pubmed_pmc | Effects of Enteric-Coated Formulation of Sodium Bicarbonate on Bicarbonate Absorption and Gastrointestinal Discomfort | Effects of Enteric-Coated Formulation of Sodium Bicarbonate on Bicarbonate Absorption and Gastrointestinal Discomfort Abstract Sodium bicarbonate is used as an ergogenic supplement to enhance people’s performances in various exercises. This study aimed to evaluate the effects of intestinal delivery of sodium bicarbonat... |
PMC7589583 | core_pubmed_pmc | Hydroxylation of Antitubercular Drug Candidate, SQ109, by Mycobacterial Cytochrome P450 | Hydroxylation of Antitubercular Drug Candidate, SQ109, by Mycobacterial Cytochrome P450 Abstract Abstract Spreading of the multidrug-resistant (MDR) strains of the one of the most harmful pathogen Mycobacterium tuberculosis (Mtb) generates the need for new effective drugs. SQ109 showed activity against resistant Mtb an... |
PMC7663239 | core_pubmed_pmc | Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential | Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential Abstract Calanolides are tetracyclic 4-substituted dipyranocoumarins. Calanolide A, isolated from the leaves and twigs of Calophyllum lanigerum var. austrocoriaceum (Whitmore) P. F. Stevens, is the ... |
PMC8494515 | core_pubmed_pmc | A Practical, One-Clinic Visit Protocol for Pharmacokinetic Profile Generation with the ADVATE myPKFiT Dosing Tool in Severe Hemophilia A Subjects | A Practical, One-Clinic Visit Protocol for Pharmacokinetic Profile Generation with the ADVATE myPKFiT Dosing Tool in Severe Hemophilia A Subjects Abstract Standard pharmacokinetic (PK) assessments are demanding for persons with hemophilia A, requiring a 72-hour washout and 5 to 11 timed blood samples. A no-washout, sin... |
PMC12359200 | core_pubmed_pmc | Saliva Based Clozapine Therapeutic Drug Monitoring: A Systematic Review | Saliva Based Clozapine Therapeutic Drug Monitoring: A Systematic Review Abstract ABSTRACT Clozapine is superior in the treatment of treatment‐refractory schizophrenia but requires therapeutic drug monitoring (TDM) due to its unpredictable pharmacokinetics and dose‐dependent side effects. This systematic review evaluate... |
PMC5953983 | core_pubmed_pmc | Population pharmacokinetics and exposure–response modeling and simulation for evolocumab in healthy volunteers and patients with hypercholesterolemia | Population pharmacokinetics and exposure–response modeling and simulation for evolocumab in healthy volunteers and patients with hypercholesterolemia Abstract Evolocumab, a novel human monoclonal antibody, inhibits proprotein convertase subtilisin/kexin type 9, a protein that targets low-density lipoprotein-cholesterol... |
PMC10719473 | core_pubmed_pmc | Protocol of the IntenSify‐Trial: An open‐label phase I trial of the CYP3A inhibitor cobicistat and the cytostatics gemcitabine and nab‐paclitaxel in patients with advanced stage or metastatic pancreatic ductal adenocarcinoma to evaluate the combination's pharmacokinetics, safety, and efficacy | Protocol of the IntenSify‐Trial: An open‐label phase I trial of the CYP3A inhibitor cobicistat and the cytostatics gemcitabine and nab‐paclitaxel in patients with advanced stage or metastatic pancreatic ductal adenocarcinoma to evaluate the combination's pharmacokinetics, safety, and efficacy Abstract Abstract Expressi... |
PMC11543921 | core_pubmed_pmc | Preclinical validation of human recombinant glutamate-oxaloacetate transaminase for the treatment of acute ischemic stroke | Preclinical validation of human recombinant glutamate-oxaloacetate transaminase for the treatment of acute ischemic stroke Abstract Summary The blood enzyme glutamate-oxaloacetate transaminase (GOT) has been postulated as an effective therapeutic to protect the brain during stroke. To demonstrate its potential clinical... |
PMC7016293 | core_pubmed_pmc | Optimized functional and structural design of dual-target LMRAP, a bifunctional fusion protein with a 25-amino-acid antitumor peptide and GnRH Fc fragment | Optimized functional and structural design of dual-target LMRAP, a bifunctional fusion protein with a 25-amino-acid antitumor peptide and GnRH Fc fragment Abstract Abstract To develop fusion protein of a GnRH Fc fragment and the integrin targeting AP25 antitumor peptide for GnRH receptor-expressing cancer therapy. The ... |
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