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PMC8043005 | core_pubmed_pmc | Predicting the risk of drug–drug interactions in psychiatric hospitals: a retrospective longitudinal pharmacovigilance study | Predicting the risk of drug–drug interactions in psychiatric hospitals: a retrospective longitudinal pharmacovigilance study Abstract Abstract Objectives The aim was to use routine data available at a patient’s admission to the hospital to predict polypharmacy and drug–drug interactions (DDI) and to evaluate the predic... |
PMC12925892 | core_pubmed_pmc | Electrocardiographic effects of HBI-3000 (sulcardine sulfate), a new drug for termination of atrial fibrillation | Electrocardiographic effects of HBI-3000 (sulcardine sulfate), a new drug for termination of atrial fibrillation Abstract Abstract Background HBI-3000 (sulcardine sulfate) inhibits multiple cardiac ion channels in vitro including peak sodium current, late sodium current, L-type calcium current, and the rapid component ... |
PMC6104105 | core_pubmed_pmc | Tracking disease progression non‐invasively in Duchenne and Becker muscular dystrophies | Tracking disease progression non‐invasively in Duchenne and Becker muscular dystrophies Abstract Abstract Background Analysis of muscle biopsies allowed to characterize the pathophysiological changes of Duchenne and Becker muscular dystrophies (D/BMD) leading to the clinical phenotype. Muscle tissue is often investigat... |
PMC12852032 | core_pubmed_pmc | Development of an anti-rat complement C2 antibody that improves renal outcome in a rat kidney transplant model | Development of an anti-rat complement C2 antibody that improves renal outcome in a rat kidney transplant model Abstract Abstract Background Previously we reported on the therapeutic monoclonal anti-human C2 antibody empasiprubart that inhibits activation of the classical and lectin pathways of complement. Preclinical s... |
PMC8599978 | core_pubmed_pmc | Mechanistic Computational Models of Epithelial Cell Transporters-the Adorned Heroes of Pharmacokinetics | Mechanistic Computational Models of Epithelial Cell Transporters-the Adorned Heroes of Pharmacokinetics Abstract Abstract Epithelial membrane transporter kinetics portray an irrefutable role in solute transport in and out of cells. Mechanistic models are used to investigate the transport of solutes at the organ, tissue... |
PMC11339345 | core_pubmed_pmc | Natural Coptidis Rhizoma Nanoparticles Improved the Oral Delivery of Docetaxel | Natural Coptidis Rhizoma Nanoparticles Improved the Oral Delivery of Docetaxel Abstract Abstract Purpose Docetaxel (DTX) is a valuable anti-tumor chemotherapy drug with limited oral bioavailability. This study aims to develop an effective oral delivery system for DTX using natural nanoparticles (Nnps) derived from Copt... |
PMC9854597 | core_pubmed_pmc | Sorting Out the Risks and Benefits of the #797 Recommended Intrapartum Vancomycin Dosing Approach | Sorting Out the Risks and Benefits of the #797 Recommended Intrapartum Vancomycin Dosing Approach Abstract ACOG Committee Opinion #797 proposed intrapartum vancomycin dosing guidelines in the absence of thorough evaluation of its risk versus benefit profile on the maternal and neonatal systems. The previously published... |
PMC12958289 | core_pubmed_pmc | Pharmacokinetic Optimization of Radiocopper-Based Theranostic Pretargeting | Pharmacokinetic Optimization of Radiocopper-Based Theranostic Pretargeting Abstract In vivo pretargeting offers a strategy to improve nuclear imaging and radiopharmaceutical therapy by increasing tumor-to-background activity concentration ratios and decreasing radiation burden to healthy tissues. One particularly promi... |
PMC7496630 | core_pubmed_pmc | The Effect of Renal Impairment on the Pharmacokinetics and Safety of Itacitinib | The Effect of Renal Impairment on the Pharmacokinetics and Safety of Itacitinib Abstract Abstract Itacitinib is a novel, selective, Janus kinase 1 inhibitor in development for treatment of graft‐versus‐host disease. The objective of this study was to assess pharmacokinetics and safety of 300‐mg itacitinib dosed in part... |
PMC3241378 | core_pubmed_pmc | Canakinumab (ACZ885, a fully human IgG1 anti-IL-1β mAb) induces sustained remission in pediatric patients with cryopyrin-associated periodic syndrome (CAPS) | Canakinumab (ACZ885, a fully human IgG1 anti-IL-1β mAb) induces sustained remission in pediatric patients with cryopyrin-associated periodic syndrome (CAPS) Abstract Abstract Introduction Cryopyrin-associated periodic syndrome (CAPS) represents a spectrum of three auto-inflammatory syndromes, familial cold auto-inflamm... |
PMC8004710 | core_pubmed_pmc | Cystic Fibrosis: Recent Insights into Inhaled Antibiotic Treatment and Future Perspectives | Cystic Fibrosis: Recent Insights into Inhaled Antibiotic Treatment and Future Perspectives Abstract Although new inhaled antibiotics have profoundly improved respiratory diseases in cystic fibrosis (CF) patients, lung infections are still the leading cause of death. Inhaled antibiotics, i.e., colistin, tobramycin, aztr... |
PMC10759330 | core_pubmed_pmc | Enhanced renal clearance impacts levetiracetam concentrations in patients with traumatic brain injury with and without augmented renal clearance | Enhanced renal clearance impacts levetiracetam concentrations in patients with traumatic brain injury with and without augmented renal clearance Abstract Abstract Background The purpose of this study was to examine the impact of ARC on levetiracetam concentrations during the first week following acute TBI. The hypothes... |
PMC5026276 | core_pubmed_pmc | The influence of CYP2C8*3 on carbamazepine serum concentration in epileptic pediatric patients | The influence of CYP2C8*3 on carbamazepine serum concentration in epileptic pediatric patients Abstract Abstract The aim of the present study was to investigate the distribution of CYP2C8 variants *3 and *5 , as well as their effect on carbamazepine pharmacokinetic properties, in 40 epileptic pediatric patients on carb... |
PMC3932137 | core_pubmed_pmc | Simple, sensitive and rapid determination of linifanib (ABT-869), a novel tyrosine kinase inhibitor in rat plasma by UHPLC-MS/MS | Simple, sensitive and rapid determination of linifanib (ABT-869), a novel tyrosine kinase inhibitor in rat plasma by UHPLC-MS/MS Abstract Abstract Background Linifanib (ABT-869) is an orally active receptor tyrosine kinase inhibitor, which simultaneously inhibits vascular endothelial and platelet derived growth factor ... |
PMC12033006 | core_pubmed_pmc | Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach | Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach Abstract ABSTRACT Tislelizumab 200 mg once every 3 weeks (Q3W) is approved for the treatment of multiple cancers. We used a model‐based approach to propose three alternative dosing regimens, 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W, ... |
PMC8081719 | core_pubmed_pmc | The Impact of ABCB1 and CES1 Polymorphisms on Dabigatran Pharmacokinetics in Healthy Chinese Subjects | The Impact of ABCB1 and CES1 Polymorphisms on Dabigatran Pharmacokinetics in Healthy Chinese Subjects Abstract Abstract Dabigatran is a novel direct oral anticoagulant agent, whose plasma concentration is closely related to bleeding risk. Genetic polymorphisms can affect the level of plasma dabigatran. The purpose of t... |
PMC8811118 | core_pubmed_pmc | Effect of Sophocarpine on the Pharmacokinetics of Umbralisib in Rat Plasma Using a Novel UPLC-MS/MS Method | Effect of Sophocarpine on the Pharmacokinetics of Umbralisib in Rat Plasma Using a Novel UPLC-MS/MS Method Abstract Umbralisib is a dual inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ) and casein kinase 1 epsilon (CK1ε) for treating marginal zone lymphoma (MZL) and follicular lymphoma (FL). This study aimed to... |
PMC8868248 | core_pubmed_pmc | Metabolomics-Based Profiling of Clerodendrum speciosum (Lamiaceae) Leaves Using LC/ESI/MS-MS and In Vivo Evaluation of Its Antioxidant Activity Using Caenorhabditis elegans Model | Metabolomics-Based Profiling of Clerodendrum speciosum (Lamiaceae) Leaves Using LC/ESI/MS-MS and In Vivo Evaluation of Its Antioxidant Activity Using Caenorhabditis elegans Model Abstract Abstract We investigated the antioxidant activity of the total methanol extract of C. speciosum leaves (CST), the ethyl acetate (CSE... |
PMC8597263 | core_pubmed_pmc | Eculizumab Pharmacokinetics and Pharmacodynamics in Patients With Neuromyelitis Optica Spectrum Disorder | Eculizumab Pharmacokinetics and Pharmacodynamics in Patients With Neuromyelitis Optica Spectrum Disorder Abstract Objective: To investigate the pharmacokinetics and pharmacodynamics of the approved 900/1,200 mg dosing regimen for the terminal complement component 5 (C5) inhibitor eculizumab in patients with neuromyelit... |
PMC8248323 | core_pubmed_pmc | Evaluation of the CYP3A and CYP2B6 Drug‐Drug Interaction Potential of Lemborexant | Evaluation of the CYP3A and CYP2B6 Drug‐Drug Interaction Potential of Lemborexant Abstract Abstract Lemborexant is approved for treating insomnia and is under investigation for treating irregular sleep‐wake rhythm disorder. Based on in vitro drug‐drug interaction (DDI) characteristics, phase 1, open‐label DDI studies w... |
PMC6449575 | core_pubmed_pmc | Prediction of lefamulin epithelial lining fluid penetration after intravenous and oral administration using Phase 1 data and population pharmacokinetics methods | Prediction of lefamulin epithelial lining fluid penetration after intravenous and oral administration using Phase 1 data and population pharmacokinetics methods Abstract Abstract Objectives Lefamulin is a semi-synthetic intravenous and oral pleuromutilin antibiotic with activity against pathogens commonly associated wi... |
PMC9504618 | core_pubmed_pmc | Racial/Ethnic Differences in the Pharmacokinetics of Antipsychotics: Focusing on East Asians | Racial/Ethnic Differences in the Pharmacokinetics of Antipsychotics: Focusing on East Asians Abstract Empirical clinical studies have suggested that East Asian patients may require lower dosages of psychotropic drugs, such as antipsychotics, lithium, and antidepressants, than non-Asians. Both the pharmacokinetic and ph... |
PMC6239267 | core_pubmed_pmc | Biochemical significance of limonene and its metabolites: future prospects for designing and developing highly potent anticancer drugs | Biochemical significance of limonene and its metabolites: future prospects for designing and developing highly potent anticancer drugs Abstract Abstract Monocyclic monoterpenes have been recognized as useful pharmacological ingredients due to their ability to treat numerous diseases. Limonene and perillyl alcohol as we... |
PMC10014688 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, safety and tolerability of cilofexor, a novel nonsteroidal Farnesoid X receptor agonist, in healthy volunteers | Pharmacokinetics, pharmacodynamics, safety and tolerability of cilofexor, a novel nonsteroidal Farnesoid X receptor agonist, in healthy volunteers Abstract Abstract Cilofexor is a nonsteroidal farnesoid X receptor (FXR) agonist being evaluated for treatment of nonalcoholic steatohepatitis (NASH) and primary sclerosing ... |
PMC5078935 | core_pubmed_pmc | Cerebrospinal fluid penetration of meropenem in neurocritical care patients with proven or suspected ventriculitis: a prospective observational study | Cerebrospinal fluid penetration of meropenem in neurocritical care patients with proven or suspected ventriculitis: a prospective observational study Abstract Abstract Background Ventriculitis is a complication of temporary intraventricular drains. The limited penetration of meropenem into the cerebrospinal fluid (CSF)... |
PMC8484505 | core_pubmed_pmc | Levels of circulating semaglutide determine reductions in HbA1c and body weight in people with type 2 diabetes | Levels of circulating semaglutide determine reductions in HbA1c and body weight in people with type 2 diabetes Abstract Summary Glucagon-like peptide-1 receptor agonists (GLP-1RA) are used for the treatment of type 2 diabetes. Whether clinically important responses and adverse events (AEs) are dependent on the route of... |
PMC10492813 | core_pubmed_pmc | A novel retinoic acid receptor-γ agonist antagonizes immune checkpoint resistance in lung cancers by altering the tumor immune microenvironment | A novel retinoic acid receptor-γ agonist antagonizes immune checkpoint resistance in lung cancers by altering the tumor immune microenvironment Abstract Abstract All- trans -retinoic acid (ATRA), the retinoic acid receptors (RARs) agonist, regulates cell growth, differentiation, immunity, and survival. We report that A... |
PMC12504394 | core_pubmed_pmc | Comparison of interpatient and intrapatient variability in doxorubicin exposure using a validated limited sampling model in dogs with cancer | Comparison of interpatient and intrapatient variability in doxorubicin exposure using a validated limited sampling model in dogs with cancer Abstract Abstract Background Doxorubicin (DOX) is an anthracycline chemotherapeutic used for many canine malignancies, and its adverse event (AE) profile has been well-described i... |
PMC11976150 | core_pubmed_pmc | Clinical development of oral semaglutide for the treatment of type 2 diabetes mellitus: focusing on early phase clinical trials | Clinical development of oral semaglutide for the treatment of type 2 diabetes mellitus: focusing on early phase clinical trials Abstract Abstract Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder often associated with obesity and elevated cardiovascular risks. Glucagon-like peptide-1 receptor agonists (GL... |
PMC6955217 | core_pubmed_pmc | Establishment of a novel culture method for maintaining intestinal stem cells derived from human induced pluripotent stem cells | Establishment of a novel culture method for maintaining intestinal stem cells derived from human induced pluripotent stem cells Abstract ABSTRACT The small intestine plays an important role in the pharmacokinetics of orally administered drugs due to the presence of drug transporters and drug-metabolizing enzymes. Howev... |
PMC4301857 | core_pubmed_pmc | The Calcineurin Inhibitor-Sparing (CIS) Trial - individualised calcineurin-inhibitor treatment by immunomonitoring in renal allograft recipients: protocol for a randomised controlled trial | The Calcineurin Inhibitor-Sparing (CIS) Trial - individualised calcineurin-inhibitor treatment by immunomonitoring in renal allograft recipients: protocol for a randomised controlled trial Abstract Background Adequate monitoring tools are required to optimise the immunosuppressive therapy of an individual patient. Part... |
PMC11256074 | core_pubmed_pmc | Antihistamines H 1 as Potential Anthelmintic Agents against the Zoonotic Parasite Angiostrongylus cantonensis | Antihistamines H 1 as Potential Anthelmintic Agents against the Zoonotic Parasite Angiostrongylus cantonensis Abstract Abstract Infections caused by parasitic helminths pose significant health concerns for both humans and animals. The limited efficacy of existing drugs underscores the urgent need for novel anthelmintic... |
PMC6152039 | core_pubmed_pmc | Development of a UPLC-MS/MS Method for Simultaneous Determination of Six Flavonoids in Rat Plasma after Administration of Maydis stigma Extract and Its Application to a Comparative Pharmacokinetic Study in Normal and Diabetic Rats | Development of a UPLC-MS/MS Method for Simultaneous Determination of Six Flavonoids in Rat Plasma after Administration of Maydis stigma Extract and Its Application to a Comparative Pharmacokinetic Study in Normal and Diabetic Rats Abstract Abstract Maydis stigma is an important medicine herb used in many parts of the w... |
PMC7295208 | core_pubmed_pmc | Impact of Halobetasol Propionate and Tazarotene Lotion 0.01%/0.045% in the Management of Plaque Psoriasis in Adults | Impact of Halobetasol Propionate and Tazarotene Lotion 0.01%/0.045% in the Management of Plaque Psoriasis in Adults Abstract Abstract Halobetasol propionate and tazarotene lotion 0.01%/0.045% (HP/TAZ) is a topical medication approved for the treatment of plaque psoriasis in adults. As a treatment modality, HP/TAZ has a... |
PMC5084761 | core_pubmed_pmc | Crisaborole Topical Ointment, 2% in Patients Ages 2 to 17 Years with Atopic Dermatitis: A Phase 1b, Open‐Label, Maximal‐Use Systemic Exposure Study | Crisaborole Topical Ointment, 2% in Patients Ages 2 to 17 Years with Atopic Dermatitis: A Phase 1b, Open‐Label, Maximal‐Use Systemic Exposure Study Abstract Abstract Background Phosphodiesterase‐4 (PDE4) is a promising target in atopic dermatitis (AD) treatment. The pharmacokinetics (PK), safety, and efficacy of crisab... |
PMC12957174 | core_pubmed_pmc | Predicting drug–drug interactions between ayahuasca alkaloids and SSRIs using physiologically based pharmacokinetic modeling | Predicting drug–drug interactions between ayahuasca alkaloids and SSRIs using physiologically based pharmacokinetic modeling Abstract Introduction Ayahuasca is a psychedelic preparation containing N,N-dimethyltryptamine (DMT) and the β-carboline harmine (HRM), a reversible monoamine oxidase A inhibitor that enables DMT... |
PMC9305136 | core_pubmed_pmc | Randomised clinical trial: a phase 1b study of GB004, an oral HIF‐1α stabiliser, for treatment of ulcerative colitis | Randomised clinical trial: a phase 1b study of GB004, an oral HIF‐1α stabiliser, for treatment of ulcerative colitis Abstract Summary Background Epithelial barrier dysfunction contributes to a dysregulated intestinal immune response in ulcerative colitis (UC). GB004 is an orally administered, small molecule, gut‐target... |
PMC8698378 | core_pubmed_pmc | Improving the Drug Development Pipeline for Mycobacteria: Modelling Antibiotic Exposure in the Hollow Fibre Infection Model | Improving the Drug Development Pipeline for Mycobacteria: Modelling Antibiotic Exposure in the Hollow Fibre Infection Model Abstract Mycobacterial infections are difficult to treat, requiring a combination of drugs and lengthy treatment times, thereby presenting a substantial burden to both the patient and health servi... |
PMC3585760 | core_pubmed_pmc | Cardiovascular Safety Profile of Dapoxetine during the Premarketing Evaluation | Cardiovascular Safety Profile of Dapoxetine during the Premarketing Evaluation Abstract The cardiovascular safety profile of dapoxetine, a novel selective serotonin reuptake inhibitor (SSRI) developed as an on-demand oral treatment for premature ejaculation (PE) in men, is evaluated. The cardiovascular assessment of da... |
PMC5064157 | core_pubmed_pmc | Linezolid for Infants and Toddlers With Disseminated Tuberculosis: First Steps | Linezolid for Infants and Toddlers With Disseminated Tuberculosis: First Steps Abstract Abstract Background. Infants and toddlers often present with disseminated and lymph node tuberculosis, in which Mycobacterium tuberculosis ( Mtb ) is predominantly intracellular. Linezolid, used to treat tuberculosis in adults, has ... |
PMC7178524 | core_pubmed_pmc | Comparative Pharmacokinetic Profiles of Puerarin in Rat Plasma by UHPLC-MS/MS after Oral Administration of Pueraria lobata Extract and Pure Puerarin | Comparative Pharmacokinetic Profiles of Puerarin in Rat Plasma by UHPLC-MS/MS after Oral Administration of Pueraria lobata Extract and Pure Puerarin Abstract Puerarin is the main biologically active isoflavone in Pueraria lobata and has a wide range of biological activities. However, due to its poor water solubility an... |
PMC11185170 | core_pubmed_pmc | Pharmacokinetics and Bioequivalence of Apremilast Tablets in Chinese Healthy Subjects Under Fasting and Postprandial States | Pharmacokinetics and Bioequivalence of Apremilast Tablets in Chinese Healthy Subjects Under Fasting and Postprandial States Abstract Objective This study compared the pharmacokinetics, safety and bioequivalence (BE) of generic and original apremilast tablets in healthy Chinese subjects under fasting and postprandial co... |
PMC10410275 | core_pubmed_pmc | Establishment of a mathematical prediction model for voriconazole stable maintenance dose: a prospective study | Establishment of a mathematical prediction model for voriconazole stable maintenance dose: a prospective study Abstract Background In patients with invasive fungal infection (IFI), the steady-state serum trough concentration ( C min ) of voriconazole (VCZ) is highly variable and can lead to treatment failure ( C min < ... |
PMC12590855 | core_pubmed_pmc | High-throughput screening and meta-analysis for lead compounds in antimalarial drug discovery | High-throughput screening and meta-analysis for lead compounds in antimalarial drug discovery Abstract Abstract Background The discovery of novel antimalarial drugs against Plasmodium falciparum has become globally urgent due to the consistent increase in mortality, morbidity, and drug resistance in endemic areas. Meth... |
PMC6994442 | core_pubmed_pmc | Oral vinorelbine versus intravenous vinorelbine, in combination with epirubicin as first-line chemotherapy in Chinese patients with metastatic breast cancer | Oral vinorelbine versus intravenous vinorelbine, in combination with epirubicin as first-line chemotherapy in Chinese patients with metastatic breast cancer Abstract Abstract Oral VRL offers easier administration, better quality of life, and cost saving. This study aimed to evaluate the treatment efficacy in terms of t... |
PMC11867916 | core_pubmed_pmc | Exploring the Impact of Developmental Clearance Saturation on Propylene Glycol Exposure in Adults and Term Neonates Using Physiologically Based Pharmacokinetic Modeling | Exploring the Impact of Developmental Clearance Saturation on Propylene Glycol Exposure in Adults and Term Neonates Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Propylene glycol (PG) is a pharmaceutical excipient which is generally regarded as safe (GRAS), though clinical toxicity has been rep... |
PMC12565047 | core_pubmed_pmc | Polypharmacy as a Chronic Condition: A Diagnostic Mindset for Safer and Smarter Care | Polypharmacy as a Chronic Condition: A Diagnostic Mindset for Safer and Smarter Care Abstract Polypharmacy is typically seen as an unavoidable consequence of multimorbidity and aging, with clinicians addressing complex medication lists unsystematically. In this perspective, we argue that polypharmacy should be managed ... |
PMC11254484 | core_pubmed_pmc | The Clinical Translation of α -humulene – A Scoping Review | The Clinical Translation of α -humulene – A Scoping Review Abstract Abstract α -humulene, a sesquiterpene found in essential oils of various plant species, has garnered interest due to its potential therapeutic applications. This scoping review aims to consolidate α -humuleneʼs evidence base, informing clinical transla... |
PMC10290838 | core_pubmed_pmc | Meropenem Pharmacokinetics and Target Attainment in Critically Ill Patients | Meropenem Pharmacokinetics and Target Attainment in Critically Ill Patients Abstract Purpose This study aimed to investigate the pharmacokinetics and target attainment of meropenem and compare the effect of meropenem dosing regimens in critically ill patients. Patients and Methods Thirty-seven critically ill patients w... |
PMC3263420 | core_pubmed_pmc | On safety, pharmacokinetics and dosage of bevacizumab in ROP treatment – a review | On safety, pharmacokinetics and dosage of bevacizumab in ROP treatment – a review Abstract Off-label intravitreal use of the vascular endothelial growth factor (VEGF) antibody bevacizumab for retinopathy of prematurity (ROP) increases despite lack of studies on safety, pharmacokinetics and dosage in developing individu... |
PMC6430154 | core_pubmed_pmc | Power Determination During Drug Development: Is Optimizing the Sample Size Based on Exposure‐Response Analyses Underutilized? | Power Determination During Drug Development: Is Optimizing the Sample Size Based on Exposure‐Response Analyses Underutilized? Abstract The use of model‐based drug development (MBDD) has been demonstrated to improve the efficiency of clinical trial design. However, MBDD complexity can limit its use, particularly early i... |
PMC8187357 | core_pubmed_pmc | PD-1 derived CA-170 is an oral immune checkpoint inhibitor that exhibits preclinical anti-tumor efficacy | PD-1 derived CA-170 is an oral immune checkpoint inhibitor that exhibits preclinical anti-tumor efficacy Abstract Small molecule immune checkpoint inhibitors targeting PD-1 and other pathways may offer advantages including ease of dosing, ability to manage immune-related adverse events (irAEs) due to their shorter phar... |
PMC4536011 | core_pubmed_pmc | Selamectin Is the Avermectin with the Best Potential for Buruli Ulcer Treatment | Selamectin Is the Avermectin with the Best Potential for Buruli Ulcer Treatment Abstract Abstract A comprehensive analysis was done to evaluate the potential use of anti-parasitic macrocyclic lactones (including avermectins and milbemycins) for Buruli ulcer (BU) therapy. A panel containing nearly all macrocyclic lacton... |
PMC6131117 | core_pubmed_pmc | Critical Review of the Use of Second-Generation Antipsychotics in Obsessive–Compulsive and Related Disorders | Critical Review of the Use of Second-Generation Antipsychotics in Obsessive–Compulsive and Related Disorders Abstract Currently, all second-generation antipsychotics are approved for schizophrenia. Many are also approved for bipolar disorder, with some also approved as adjunctive treatment for depression and autism-rel... |
PMC7743980 | core_pubmed_pmc | The pharmacodynamic and differential gene expression analysis of PPAR α/δ agonist GFT505 in CDAHFD-induced NASH model | The pharmacodynamic and differential gene expression analysis of PPAR α/δ agonist GFT505 in CDAHFD-induced NASH model Abstract Peroxisome proliferator-activated receptor α/δ (PPAR α/δ), regulating glucolipid metabolism and immune inflammation, has been identified as an effective therapeutic target in non-alcoholic stea... |
PMC3679788 | core_pubmed_pmc | Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study | Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study Abstract Abstract Background Although some studies show higher antiretroviral concentrations in women compared to men, data are limited. We conducted a cross-... |
PMC12686766 | core_pubmed_pmc | Next‐Generation Proteolysis‐Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation | Next‐Generation Proteolysis‐Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation Abstract ABSTRACT Proteolysis‐targeting chimeras (PROTACs)‐mediated protein degradation has been recently developed as a game‐changing approach ... |
PMC9207260 | core_pubmed_pmc | Harnessing Clinical Trial and Real-World Data Towards an Understanding of Sex Effects on Drug Pharmacokinetics, Pharmacodynamics and Efficacy | Harnessing Clinical Trial and Real-World Data Towards an Understanding of Sex Effects on Drug Pharmacokinetics, Pharmacodynamics and Efficacy Abstract Abstract Increasing clinical data on sex-related differences in drug efficacy and toxicity has highlighted the importance of understanding the impact of sex on drug phar... |
PMC10751104 | core_pubmed_pmc | Fentanyl in cancer pain management: avoiding hasty judgments and discerning its potential benefits | Fentanyl in cancer pain management: avoiding hasty judgments and discerning its potential benefits Abstract Abstract Cancer pain is an important challenge in treatment and requires a rapid onset of action for its control. In particular, breakthrough cancer pain (BTcP) should be adequately controlled with a stable dose ... |
PMC12681842 | core_pubmed_pmc | CD276-directed supramolecular nanoplatform with pH-triggered gemcitabine release for potent tumor stromal and vascular suppression | CD276-directed supramolecular nanoplatform with pH-triggered gemcitabine release for potent tumor stromal and vascular suppression Abstract Abstract Gemcitabine (Gem) remains a cornerstone chemotherapy for pancreatic ductal adenocarcinoma, but its clinical efficacy is limited by poor pharmacokinetics, dense fibrotic st... |
PMC3198174 | core_pubmed_pmc | Comparison of D 2 dopamine receptor occupancy after oral administration of quetiapine fumarate immediate-release and extended-release formulations in healthy subjects | Comparison of D 2 dopamine receptor occupancy after oral administration of quetiapine fumarate immediate-release and extended-release formulations in healthy subjects Abstract Quetiapine is an established drug for treatment of schizophrenia, bipolar disorder, and major depressive disorder. While initially manufactured ... |
PMC4510652 | core_pubmed_pmc | Lansoprazole is an antituberculous prodrug targeting cytochrome bc 1 | Lansoprazole is an antituberculous prodrug targeting cytochrome bc 1 Abstract Better antibiotics capable of killing multi-drug-resistant Mycobacterium tuberculosis are urgently needed. Despite extensive drug discovery efforts, only a few promising candidates are on the horizon and alternative screening protocols are re... |
PMC12002126 | core_pubmed_pmc | In vivo and in situ monitoring of doxorubicin pharmacokinetics with an implantable bioresorbable optical sensor | In vivo and in situ monitoring of doxorubicin pharmacokinetics with an implantable bioresorbable optical sensor Abstract Abstract Cancer treatment, particularly chemotherapy, requires balancing efficacy and toxicity. Although traditional monitoring methods can lead to suboptimal outcomes, emerging implantable chemical ... |
PMC7963108 | core_pubmed_pmc | Physiologically based pharmacokinetic/pharmacodynamic model for the prediction of morphine brain disposition and analgesia in adults and children | Physiologically based pharmacokinetic/pharmacodynamic model for the prediction of morphine brain disposition and analgesia in adults and children Abstract Abstract Morphine is a widely used opioid analgesic, which shows large differences in clinical response in children, even when aiming for equivalent plasma drug conc... |
PMC10235636 | core_pubmed_pmc | Chitosan and chito-oligosaccharide: a versatile biopolymer with endless grafting possibilities for multifarious applications | Chitosan and chito-oligosaccharide: a versatile biopolymer with endless grafting possibilities for multifarious applications Abstract Chito-oligosaccharides (COS), derived from chitosan (CH), are attracting increasing attention as drug delivery carriers due to their biocompatibility, biodegradability, and mucoadhesive ... |
PMC12255621 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Safety of Nipocalimab in Healthy Chinese Volunteers: A Single-Dose, Phase I Study | Pharmacokinetics, Pharmacodynamics, and Safety of Nipocalimab in Healthy Chinese Volunteers: A Single-Dose, Phase I Study Abstract Introduction Nipocalimab is a high-affinity, fully human, immunoglobulin G (IgG) 1 monoclonal antibody that inhibits the neonatal Fc receptor. Nipocalimab is under development for the treat... |
PMC12296181 | core_pubmed_pmc | SGLT2 Inhibitors: From Structure–Effect Relationship to Pharmacological Response | SGLT2 Inhibitors: From Structure–Effect Relationship to Pharmacological Response Abstract Abstract SGLT2 inhibitors have become increasingly used due to their effectiveness in improving not only type 2 diabetes but also cardiovascular, renal and hepatic diseases, as well as the obesity found in metabolic syndrome. Star... |
PMC9377743 | core_pubmed_pmc | Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody–drug Conjugate Targeting AXL-expressing Cancers | Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody–drug Conjugate Targeting AXL-expressing Cancers Abstract Abstract AXL, a tyrosine kinase receptor that is overexpressed in many solid and hematologic malignancies, facilitates cancer progression and is associated with poor clinical ... |
PMC9654315 | core_pubmed_pmc | Clinical Pharmacology of Factor XI Inhibitors: New Therapeutic Approaches for Prevention of Venous and Arterial Thrombotic Disorders | Clinical Pharmacology of Factor XI Inhibitors: New Therapeutic Approaches for Prevention of Venous and Arterial Thrombotic Disorders Abstract Bleeding is the dominant adverse event of anticoagulation and often discourages many patients and physicians from starting treatment with anticoagulant drugs. The fact that facto... |
PMC12890520 | core_pubmed_pmc | Preclinical assessment of oral TLR7 agonist SA-5 in a nonhuman primate model | Preclinical assessment of oral TLR7 agonist SA-5 in a nonhuman primate model Abstract Abstract TLR7 agonists are promising immunostimulatory agents for the treatment of chronic infections and cancer. However, their systemic toxicity remains a challenge. In this study, SA-5, a potentially novel liver-targeted, orally av... |
PMC3651817 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of moist inhalation epinephrine using a mobile inhaler | Pharmacokinetics and pharmacodynamics of moist inhalation epinephrine using a mobile inhaler Abstract Abstract Background Intramuscular (L-)epinephrine is used as self-medication for serious hypersensitivity reactions. Inhalative administration has the theoretical advantage of a more rapid absorption and better control... |
PMC5511603 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of Dexmedetomidine | Clinical Pharmacokinetics and Pharmacodynamics of Dexmedetomidine Abstract Dexmedetomidine is an α 2 -adrenoceptor agonist with sedative, anxiolytic, sympatholytic, and analgesic-sparing effects, and minimal depression of respiratory function. It is potent and highly selective for α 2 -receptors with an α 2 :α 1 ratio ... |
PMC9608800 | core_pubmed_pmc | Population pharmacokinetics of mycophenolate mofetil in pediatric patients early after liver transplantation | Population pharmacokinetics of mycophenolate mofetil in pediatric patients early after liver transplantation Abstract Abstract Objective: To investigate the factors influencing the pharmacokinetics of mycophenolate mofetil (MMF) in pediatric patients after liver transplantation, and to establish a population pharmacoki... |
PMC12053371 | core_pubmed_pmc | Stochastic pharmacodynamics of a heterogeneous tumour-cell population | Stochastic pharmacodynamics of a heterogeneous tumour-cell population Abstract Abstract Standard pharmacodynamic models are ordinary differential equations without the features of stochasticity and heterogeneity. We develop and analyse a stochastic model of a heterogeneous tumour-cell population treated with a drug, wh... |
PMC12248041 | core_pubmed_pmc | Hybrid Population PK-Machine Learning Modeling to Predict Infliximab Pharmacokinetics in Pediatric and Young Adult Patients with Crohn’s Disease | Hybrid Population PK-Machine Learning Modeling to Predict Infliximab Pharmacokinetics in Pediatric and Young Adult Patients with Crohn’s Disease Abstract Abstract Population pharmacokinetic (PK) model-based Bayesian estimation is widely used for dose individualization, particularly when sample availability is limited. ... |
PMC5653488 | core_pubmed_pmc | A Simulation Study of Propofol Effect-Site Concentration for Appropriate Sedation in Pediatric Patients Undergoing Brain MRI: Pharmacodynamic Analysis | A Simulation Study of Propofol Effect-Site Concentration for Appropriate Sedation in Pediatric Patients Undergoing Brain MRI: Pharmacodynamic Analysis Abstract Abstract Purpose We aimed to establish the propofol effect-site concentration (Ce) for appropriate sedation by pharmacodynamic analysis and to determine the pro... |
PMC10419975 | core_pubmed_pmc | A Novel Betulinic Acid Analogue: Synthesis, Solubility, Antitumor Activity and Pharmacokinetic Study in Rats | A Novel Betulinic Acid Analogue: Synthesis, Solubility, Antitumor Activity and Pharmacokinetic Study in Rats Abstract Abstract Betulinic acid (BA) and betulin (BE) are naturally pentacyclic triterpenes with documented biological activities, especially antitumor and anti-inflammatory activity. However, their bioavailabi... |
PMC4263153 | core_pubmed_pmc | Abuse potential, pharmacokinetics, pharmacodynamics, and safety of intranasally administered crushed oxycodone HCl abuse-deterrent controlled-release tablets in recreational opioid users | Abuse potential, pharmacokinetics, pharmacodynamics, and safety of intranasally administered crushed oxycodone HCl abuse-deterrent controlled-release tablets in recreational opioid users Abstract The objective of this study was to evaluate abuse potential, pharmacokinetics, pharmacodynamics, and safety of intranasally ... |
PMC11181194 | core_pubmed_pmc | Meeting the Therapeutic Challenges of Emergent and Rare Invasive Fungal Diseases Through Novel Clinical Trial Designs | Meeting the Therapeutic Challenges of Emergent and Rare Invasive Fungal Diseases Through Novel Clinical Trial Designs Abstract Abstract Treatments for emerging and rare invasive fungal diseases (IFDs) represent a critical unmet medical need. For IFDs that occur less frequently than invasive aspergillosis, such as mucor... |
PMC8411588 | core_pubmed_pmc | Development and validation of assays for the quantification of β-D-N 4 -hydroxycytidine in human plasma and β-D-N 4 -hydroxycytidine-triphosphate in peripheral blood mononuclear cell lysates | Development and validation of assays for the quantification of β-D-N 4 -hydroxycytidine in human plasma and β-D-N 4 -hydroxycytidine-triphosphate in peripheral blood mononuclear cell lysates Abstract Abstract The novel antiviral prodrug molnupiravir is under evaluation for the treatment of SARS-CoV-2. Molnupiravir is c... |
PMC9308414 | core_pubmed_pmc | Pharmacokinetics of isavuconazole in healthy cats after oral and intravenous administration | Pharmacokinetics of isavuconazole in healthy cats after oral and intravenous administration Abstract Abstract Background Isavuconazole is a triazole antifungal drug that has shown good efficacy in human patients. Absorption and pharmacokinetics have not been evaluated in cats. Objectives To determine the pharmacokineti... |
PMC11678170 | core_pubmed_pmc | Personalized Secukinumab Treatment in Patients with Plaque Psoriasis Using Model-Informed Precision Dosing | Personalized Secukinumab Treatment in Patients with Plaque Psoriasis Using Model-Informed Precision Dosing Abstract Background/Objectives: Patient care and control of inflammatory disorders, such as psoriasis, can be improved by model-informed precision dosing (MIPD) techniques based on population pharmacokinetic/pharm... |
PMC12603464 | core_pubmed_pmc | Efficacy, pharmacokinetics, and safety of nebulized HL231 inhalation solution in patients with chronic obstructive pulmonary disease: a randomized trial | Efficacy, pharmacokinetics, and safety of nebulized HL231 inhalation solution in patients with chronic obstructive pulmonary disease: a randomized trial Abstract Background Long-acting beta-agonist (LABA) plus long-acting muscarinic antagonist (LAMA) is superior to monotherapy or corticosteroid/LABA in terms of improvi... |
PMC12458090 | core_pubmed_pmc | Examination of oxidative stress and glutamate as potential mechanisms of N-acetylcysteine in the treatment of non-suicidal self-injury in young people assigned female at birth: randomised trial | Examination of oxidative stress and glutamate as potential mechanisms of N-acetylcysteine in the treatment of non-suicidal self-injury in young people assigned female at birth: randomised trial Abstract Abstract Background Non-suicidal self-injury (NSSI) often emerges during adolescence and young adulthood. A prior ope... |
PMC9544893 | core_pubmed_pmc | Efficacy and safety of cannabidivarin treatment of epilepsy in girls with Rett syndrome: A phase 1 clinical trial | Efficacy and safety of cannabidivarin treatment of epilepsy in girls with Rett syndrome: A phase 1 clinical trial Abstract Summary Objective Rett syndrome (RTT), commonly caused by methyl‐CpG‐binding protein 2 ( MECP2 ) pathogenic variants, has many comorbidities. Fifty to ninety percent of children with RTT have epile... |
PMC8779473 | core_pubmed_pmc | Pharmacokinetics of Pullulan–Dexamethasone Conjugates in Retinal Drug Delivery | Pharmacokinetics of Pullulan–Dexamethasone Conjugates in Retinal Drug Delivery Abstract The treatment of retinal diseases by intravitreal injections requires frequent administration unless drug delivery systems with long retention and controlled release are used. In this work, we focused on pullulan (≈67 kDa) conjugate... |
PMC8073512 | core_pubmed_pmc | Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy | Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy Abstract Abstract Poly(ADP-ribose) polymerases (PARP) are proteins responsible for DNA damage detection and signal transduction. PARP inhibitors (PARPi) are able to interact with the binding site... |
PMC9461731 | core_pubmed_pmc | Enhanced toxicity to chemoradiation in a patient with Anti-Jo-1-antisynthetase syndrome | Enhanced toxicity to chemoradiation in a patient with Anti-Jo-1-antisynthetase syndrome Abstract Abstract Appropriate counseling of patients with autoimmune connective tissue disorders (ACTDs) is often challenging for radiation oncologists, especially regarding anticipated side-effects of radiation treatment. These pat... |
PMC4728453 | core_pubmed_pmc | Pharmacokinetics of Selected Anticancer Drugs in Elderly Cancer Patients: Focus on Breast Cancer | Pharmacokinetics of Selected Anticancer Drugs in Elderly Cancer Patients: Focus on Breast Cancer Abstract Abstract Background: Elderly patients receiving anticancer drugs may have an increased risk to develop treatment-related toxicities compared to their younger peers. However, a potential pharmacokinetic (PK) basis f... |
PMC9291915 | core_pubmed_pmc | Evaluation of the drug‐drug interaction potential of treosulfan using a physiologically‐based pharmacokinetic modelling approach | Evaluation of the drug‐drug interaction potential of treosulfan using a physiologically‐based pharmacokinetic modelling approach Abstract Abstract Aims The aim of this work is the development of a mechanistic physiologically‐based pharmacokinetic (PBPK) model using in vitro to in vivo extrapolation to conduct a drug‐dr... |
PMC3287161 | core_pubmed_pmc | Paracetamol serum concentrations in preterm infants treated with paracetamol intravenously: a case series | Paracetamol serum concentrations in preterm infants treated with paracetamol intravenously: a case series Abstract Abstract Introduction Until now, studies on paracetamol given intravenously have mainly been performed with the pro-drug propacetamol or with paracetamol in preterm babies above 32 weeks of gestation. Stud... |
PMC8803428 | core_pubmed_pmc | Pharmacokinetics of Ginsenoside Rb1, Rg3, Rk1, Rg5, F2, and Compound K from Red Ginseng Extract in Healthy Korean Volunteers | Pharmacokinetics of Ginsenoside Rb1, Rg3, Rk1, Rg5, F2, and Compound K from Red Ginseng Extract in Healthy Korean Volunteers Abstract Individual differences in ginsenoside pharmacokinetics following ginseng administration in humans are still unclear. We aimed to investigate the pharmacokinetic properties of various gin... |
PMC11873997 | core_pubmed_pmc | Identification of Structurally Novel KRAS G12C Inhibitors through Covalent DNA-Encoded Library Screening | Identification of Structurally Novel KRAS G12C Inhibitors through Covalent DNA-Encoded Library Screening Abstract Abstract Covalent inhibition of the KRAS G12C oncoprotein has emerged as a promising therapeutic approach for the treatment of nonsmall cell lung cancer (NSCLC). The identification of KRAS G12C inhibitors h... |
PMC10253591 | core_pubmed_pmc | A Non-Systemic Phosphodiesterase-5 Inhibitor Suppresses Colon Proliferation in Mice | A Non-Systemic Phosphodiesterase-5 Inhibitor Suppresses Colon Proliferation in Mice Abstract Phosphodiesterase-5 inhibitors (PDE5i) are under investigation for repurposing for colon cancer prevention. A drawback to conventional PDE5i are their side-effects and drug–drug interactions. We designed an analog of the protot... |
PMC4739345 | core_pubmed_pmc | In Vitro Determination of Respimat ® Dose Delivery in Children: An Evaluation Based on Inhalation Flow Profiles and Mouth–Throat Models | In Vitro Determination of Respimat ® Dose Delivery in Children: An Evaluation Based on Inhalation Flow Profiles and Mouth–Throat Models Abstract Abstract Background: Aerosol therapy in young children can be difficult. A realistic model based on handling studies and in vitro investigations can complement clinical deposi... |
PMC11857448 | core_pubmed_pmc | Is N 1-Methylnicotinamide a Good Organic Cation Transporter 2 (OCT2) Biomarker? | Is N 1-Methylnicotinamide a Good Organic Cation Transporter 2 (OCT2) Biomarker? Abstract Background/Objectives: The impact of potential precipitant drugs on plasma or urinary exposure of endogenous biomarkers is emerging as an alternative approach to evaluating drug–drug interaction (DDI) liability. N 1-Methylnicotinam... |
PMC9544977 | core_pubmed_pmc | Anti‐KIT monoclonal antibody CDX‐0159 induces profound and durable mast cell suppression in a healthy volunteer study | Anti‐KIT monoclonal antibody CDX‐0159 induces profound and durable mast cell suppression in a healthy volunteer study Abstract Abstract Background Mast cells (MC) are powerful inflammatory immune sentinel cells that drive numerous allergic, inflammatory, and pruritic disorders when activated. MC‐targeted therapies are ... |
PMC9421219 | core_pubmed_pmc | Effect of Rifabutin in Dolutegravir Dosing: A Case Series | Effect of Rifabutin in Dolutegravir Dosing: A Case Series Abstract Background: Tuberculosis (TB) is the leading cause of death in human immunodeficiency virus (HIV)-infected people worldwide. Currently there are no studies examining the use of Rifabutin (RBN) and Dolutegravir (DTG) in co-infected persons. This is a cas... |
PMC11706421 | core_pubmed_pmc | Vancomycin population pharmacokinetic models: Uncovering pharmacodynamic divergence amid clinicobiological resemblance | Vancomycin population pharmacokinetic models: Uncovering pharmacodynamic divergence amid clinicobiological resemblance Abstract Abstract Vancomycin is an antibiotic used for severe infections. To ensure microbiological efficacy, a ratio of AUC/MIC ≥400 is recommended. However, there is significant interindividual varia... |
PMC12361604 | core_pubmed_pmc | Dataset on insight into inhibition capacity of cyclic tetra-amino acid based compounds as efficient crystal structure of human insulin-degrading enzyme inhibitors | Dataset on insight into inhibition capacity of cyclic tetra-amino acid based compounds as efficient crystal structure of human insulin-degrading enzyme inhibitors Abstract Abstract The biochemical evaluation of nine cyclopeptide derivatives were investigated using computational approaches. Key software in drug design a... |
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