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PMC11124264 | core_pubmed_pmc | Evaluating Drug Interactions between Ritonavir and Opioid Analgesics: Implications from Physiologically Based Pharmacokinetic Simulation | Evaluating Drug Interactions between Ritonavir and Opioid Analgesics: Implications from Physiologically Based Pharmacokinetic Simulation Abstract Abstract Several commonly used opioid analgesics, such as fentanyl, sufentanil, alfentanil, and hydrocodone, are by report primarily metabolized by the CYP3A4 enzyme. The con... |
PMC9414624 | core_pubmed_pmc | Tolerability of Atovaquone—Proguanil Application in Common Buzzard Nestlings | Tolerability of Atovaquone—Proguanil Application in Common Buzzard Nestlings Abstract Abstract Simple Summary Many wild animals, and particularly birds, are commonly infected and can suffer health consequences by blood parasites related to Plasmodium , the causative agents of malaria in humans. Atovaquone–proguanil (Ma... |
PMC5473874 | core_pubmed_pmc | Machine learning workflow to enhance predictions of Adverse Drug Reactions (ADRs) through drug-gene interactions: application to drugs for cutaneous diseases | Machine learning workflow to enhance predictions of Adverse Drug Reactions (ADRs) through drug-gene interactions: application to drugs for cutaneous diseases Abstract Adverse drug reactions (ADRs) pose critical public health issues, affecting over 6% of hospitalized patients. While knowledge of potential drug-drug inte... |
PMC5766692 | core_pubmed_pmc | Effects of processing method on the pharmacokinetics and tissue distribution of orally administered ginseng | Effects of processing method on the pharmacokinetics and tissue distribution of orally administered ginseng Abstract Background The use of different methods for the processing of ginseng can result in alterations in its medicinal properties and efficacy. White ginseng (WG), frozen ginseng (FG), and red ginseng (RG) are... |
PMC9241781 | core_pubmed_pmc | Detection of Ganciclovir-Resistant Cytomegalovirus in a Prospective Cohort of Kidney Transplant Recipients Receiving Subtherapeutic Valganciclovir Prophylaxis | Detection of Ganciclovir-Resistant Cytomegalovirus in a Prospective Cohort of Kidney Transplant Recipients Receiving Subtherapeutic Valganciclovir Prophylaxis Abstract ABSTRACT Cytomegalovirus infection during antiviral prophylaxis occurs in transplant recipients despite individualized regimens based on renal function.... |
PMC11209592 | core_pubmed_pmc | Antiviral Use in Mild-to-Moderate SARS-CoV-2 Infections during the Omicron Wave in Geriatric Patients | Antiviral Use in Mild-to-Moderate SARS-CoV-2 Infections during the Omicron Wave in Geriatric Patients Abstract Abstract (1) Background: Geriatric patients are at high risk of complications of Coronavirus disease-2019 (COVID-19) and are good candidates for antiviral drugs. (2) Methods: A retrospective study of electroni... |
PMC7042210 | core_pubmed_pmc | Immunogenicity of Biosimilars for Rheumatic Diseases, Plaque Psoriasis, and Inflammatory Bowel Disease: A Review from Clinical Trials and Regulatory Documents | Immunogenicity of Biosimilars for Rheumatic Diseases, Plaque Psoriasis, and Inflammatory Bowel Disease: A Review from Clinical Trials and Regulatory Documents Abstract Abstract The goal of this narrative review was to summarize immunogenicity data of biosimilars or biosimilar candidates for rheumatic diseases, plaque p... |
PMC12299433 | core_pubmed_pmc | Challenges in the Investigation of Therapeutic Equivalence of Locally Applied/Locally Acting Drugs in the Gastrointestinal Tract: The Rifaximin Case | Challenges in the Investigation of Therapeutic Equivalence of Locally Applied/Locally Acting Drugs in the Gastrointestinal Tract: The Rifaximin Case Abstract Background: Locally acting gastrointestinal (GI) drugs present challenges for generic drug development because traditional bioequivalence measures, which rely on ... |
PMC10536587 | core_pubmed_pmc | Predicting Volume of Distribution in Neonates: Performance of Physiologically Based Pharmacokinetic Modelling | Predicting Volume of Distribution in Neonates: Performance of Physiologically Based Pharmacokinetic Modelling Abstract The volume of distribution at steady state (Vss) in neonates is still often estimated through isometric scaling from adult values, disregarding developmental changes beyond body weight. This study aime... |
PMC11174219 | core_pubmed_pmc | In Silico Analysis of Selective Bioactive Compounds from Acronychia Pedunculata as a Potential Inhibitor of HER2 in Colorectal Cancer | In Silico Analysis of Selective Bioactive Compounds from Acronychia Pedunculata as a Potential Inhibitor of HER2 in Colorectal Cancer Abstract A BSTRACT Colorectal cancer (CRC) is a pervasive malignancy that stands as a prominent contributor to global cancer-related mortality. Among the numerous causative factors, the ... |
PMC6897335 | core_pubmed_pmc | European Federation for Exploratory Medicines Development Lyon Conference 2019: The Changing Landscape of Early Medicines Development—Be Prepared | European Federation for Exploratory Medicines Development Lyon Conference 2019: The Changing Landscape of Early Medicines Development—Be Prepared Abstract The second biennial conference of the European Federation for Exploratory Medicines Development (EUFEMED) was the result of a continued effort of EUFEMED to gather a... |
PMC3790192 | core_pubmed_pmc | A phase 1 trial of imatinib, bevacizumab, and metronomic cyclophosphamide in advanced colorectal cancer | A phase 1 trial of imatinib, bevacizumab, and metronomic cyclophosphamide in advanced colorectal cancer Abstract Abstract Background: This phase 1 clinical trial was conducted to determine the safety, maximum-tolerated dose (MTD), and pharmacokinetics of imatinib, bevacizumab, and metronomic cyclophosphamide in patient... |
PMC4368844 | core_pubmed_pmc | Population Pharmacokinetic Meta-Analysis to Bridge Ferumoxytol Plasma Pharmacokinetics Across Populations | Population Pharmacokinetic Meta-Analysis to Bridge Ferumoxytol Plasma Pharmacokinetics Across Populations Abstract Background Ferumoxytol is approved for the treatment of iron-deficiency anaemia (IDA) in adult patients with chronic kidney disease (CKD). Ferumoxytol has recently been investigated for use in all-cause ID... |
PMC6920861 | core_pubmed_pmc | Co-Encapsulation of Chlorin e6 and Chemotherapeutic Drugs in a PEGylated Liposome Enhance the Efficacy of Tumor Treatment: Pharmacokinetics and Therapeutic Efficacy | Co-Encapsulation of Chlorin e6 and Chemotherapeutic Drugs in a PEGylated Liposome Enhance the Efficacy of Tumor Treatment: Pharmacokinetics and Therapeutic Efficacy Abstract Long-circulating PEG-modified liposome has been shown to improve pharmacokinetic properties and reduce systemic toxicity in cancer treatment. Howe... |
PMC12567289 | core_pubmed_pmc | Sustained-Release Oral Delivery of NSAIDs and Acetaminophen: Advances and Recent Formulation Strategies—A Systematic Review | Sustained-Release Oral Delivery of NSAIDs and Acetaminophen: Advances and Recent Formulation Strategies—A Systematic Review Abstract Background : Sustained-release (SR) formulations of non-steroidal anti-inflammatory drugs (NSAIDs) aim to prolong therapeutic activity, reduce dosing frequency, and improve patient adhere... |
PMC12498271 | core_pubmed_pmc | A First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors | A First-In-Human Dose-Escalation Phase I Study of Basroparib, a Tankyrase Inhibitor, in Patients with Advanced-Stage Solid Tumors Abstract Abstract Purpose: The pathogenesis of colorectal cancer is largely driven by mutations of the tumor suppressor gene APC (adenomatous polyposis coli) that lead to aberrant activation... |
PMC12196915 | core_pubmed_pmc | Intravenous Administration of sRNA Nanoparticles for Treatment of Osteoporosis in Mice | Intravenous Administration of sRNA Nanoparticles for Treatment of Osteoporosis in Mice Abstract Abstract Background : With the intensification of population aging, osteoporosis has become one of the significant public health issues affecting human health. Currently available medications for treating osteoporosis are as... |
PMC10272304 | core_pubmed_pmc | Pharmacokinetic‐pharmacodynamic model of urinary δ‐aminolevulinic acid reduction after givosiran treatment in patients with acute hepatic porphyria | Pharmacokinetic‐pharmacodynamic model of urinary δ‐aminolevulinic acid reduction after givosiran treatment in patients with acute hepatic porphyria Abstract Abstract Givosiran, an RNA interference‐based therapeutic, is a recent addition to the limited treatment armamentarium for acute hepatic porphyria (AHP). As a smal... |
PMC8304089 | core_pubmed_pmc | Transcending toward Advanced 3D-Cell Culture Modalities: A Review about an Emerging Paradigm in Translational Oncology | Transcending toward Advanced 3D-Cell Culture Modalities: A Review about an Emerging Paradigm in Translational Oncology Abstract Abstract Cancer is a disorder characterized by an uncontrollable overgrowth and a fast-moving spread of cells from a localized tissue to multiple organs of the body, reaching a metastatic stat... |
PMC7729195 | core_pubmed_pmc | Pharmacodynamic Functions of Synthetic Derivatives for Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) and Mycobacterium tuberculosis | Pharmacodynamic Functions of Synthetic Derivatives for Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) and Mycobacterium tuberculosis Abstract Drug resistant bacteria have emerged, so robust methods are needed to evaluate combined activities of known antibiotics as well as new synthetic compounds as nov... |
PMC8895951 | core_pubmed_pmc | Development and Evaluation of Competitive Inhibitors of Trastuzumab-HER2 Binding to Bypass the Binding-Site Barrier | Development and Evaluation of Competitive Inhibitors of Trastuzumab-HER2 Binding to Bypass the Binding-Site Barrier Abstract Abstract Our group has developed and experimentally validated a strategy to increase antibody penetration in solid tumors through transient inhibition of antibody-antigen binding. In prior work, ... |
PMC6320896 | core_pubmed_pmc | Long-Circulating Hyaluronan-Based Nanohydrogels as Carriers of Hydrophobic Drugs | Long-Circulating Hyaluronan-Based Nanohydrogels as Carriers of Hydrophobic Drugs Abstract Abstract Nanohydrogels based on natural polymers, such as polysaccharides, are gaining interest as vehicles for therapeutic agents, as they can modify the pharmacokinetics and pharmacodynamics of the carried drugs. In this work, h... |
PMC6551597 | core_pubmed_pmc | Mixed micelles loaded with the 5-benzylidenethiazolidine-2,4-dione derivative SKLB023 for efficient treatment of non-alcoholic steatohepatitis | Mixed micelles loaded with the 5-benzylidenethiazolidine-2,4-dione derivative SKLB023 for efficient treatment of non-alcoholic steatohepatitis Abstract Background: SKLB023, a novel 5-benzylidenethiazolidine-2,4-dione based-derivative, specifically inhibits inducible nitric oxide synthase and shows promise for treating ... |
PMC10235118 | core_pubmed_pmc | Part two: an unblinded, parallel, randomized study to assess nicotine pharmacokinetics of four Vuse Solo ENDS flavors in smokers | Part two: an unblinded, parallel, randomized study to assess nicotine pharmacokinetics of four Vuse Solo ENDS flavors in smokers Abstract We report the findings from a randomized, parallel study designed to evaluate nicotine pharmacokinetics (PK) following 10 min of ad libitum use of electronic nicotine delivery system... |
PMC3908787 | core_pubmed_pmc | Ceftazidime–avibactam: an evidence-based review of its pharmacology and potential use in the treatment of Gram-negative bacterial infections | Ceftazidime–avibactam: an evidence-based review of its pharmacology and potential use in the treatment of Gram-negative bacterial infections Abstract Abstract Avibactam (NXL104, AVE1330A) is a semi-synthetic, non-β-lactam, β-lactamase inhibitor that is active against Ambler class A, class C, and some class D serine β-l... |
PMC12608307 | core_pubmed_pmc | Personalized Approaches to Patients with Intra-Abdominal Infections | Personalized Approaches to Patients with Intra-Abdominal Infections Abstract Intra-abdominal infections (IAIs) continue to be an important cause of morbidity and mortality worldwide. The optimal management of patients with IAIs relies on early and accurate diagnosis, prompt and adequate source control, appropriate anti... |
PMC7547139 | core_pubmed_pmc | Biomimetic Synthesis and Evaluation of Interconnected Bimodal Mesostructured MSF@Poly(Ethyleneimine)s for Improved Drug Loading and Oral Adsorption of the Poorly Water-Soluble Drug, Ibuprofen | Biomimetic Synthesis and Evaluation of Interconnected Bimodal Mesostructured MSF@Poly(Ethyleneimine)s for Improved Drug Loading and Oral Adsorption of the Poorly Water-Soluble Drug, Ibuprofen Abstract Abstract Purpose The aim of this study was to improve the oral bioavailability and anti-inflammatory activity of the po... |
PMC5778159 | core_pubmed_pmc | Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method | Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method Abstract Abstract Tianeptine is an atypical antidepressant with a unique mechanism of action and recently it has been also... |
PMC7010644 | core_pubmed_pmc | Developmental Population Pharmacokinetics and Dosing Optimization of Cefepime in Neonates and Young Infants | Developmental Population Pharmacokinetics and Dosing Optimization of Cefepime in Neonates and Young Infants Abstract Abstract Objective Cefepime is used to treat severe infections in neonates. Pharmacokinetic data have only been evaluated among preterm neonates and population pharmacokinetic model lacked external valid... |
PMC8696178 | core_pubmed_pmc | Comparison of Female Genital Tract Cytokine and Microbiota Signatures Induced by Initiation of Intramuscular DMPA and NET-EN Hormonal Contraceptives - a Prospective Cohort Analysis | Comparison of Female Genital Tract Cytokine and Microbiota Signatures Induced by Initiation of Intramuscular DMPA and NET-EN Hormonal Contraceptives - a Prospective Cohort Analysis Abstract Background Cervicovaginal inflammation, bacterial microbiota and hormonal contraceptives all influence sexual and reproductive hea... |
PMC4871544 | core_pubmed_pmc | Quantifying Isoniazid Levels in Small Hair Samples: A Novel Method for Assessing Adherence during the Treatment of Latent and Active Tuberculosis | Quantifying Isoniazid Levels in Small Hair Samples: A Novel Method for Assessing Adherence during the Treatment of Latent and Active Tuberculosis Abstract Background Tuberculosis (TB) is the leading cause of death from an infectious pathogen worldwide and the most prevalent opportunistic infection in people living with... |
PMC3558798 | core_pubmed_pmc | Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects | Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects Abstract Aims To evaluate apixaban single dose safety, tolerability, pharmacokinetics and pharmacodynamics and assess the effect of food on apixaban pharmacokinetics. Methods A doubl... |
PMC12811852 | core_pubmed_pmc | Pharmacokinetics and Safety of Clofazimine in Women With Rifampicin-resistant Tuberculosis During Pregnancy and the Postpartum Period: Results From IMPAACT P1026s | Pharmacokinetics and Safety of Clofazimine in Women With Rifampicin-resistant Tuberculosis During Pregnancy and the Postpartum Period: Results From IMPAACT P1026s Abstract Abstract Background There are no published data on clofazimine pharmacokinetics during pregnancy, and safety data are limited. We present data from ... |
PMC11623990 | core_pubmed_pmc | Deferasirox and Ciprofloxacin: Potential Ternary Complex Formation With Ferric Iron, Pharmacodynamic, and Pharmacokinetic Interactions | Deferasirox and Ciprofloxacin: Potential Ternary Complex Formation With Ferric Iron, Pharmacodynamic, and Pharmacokinetic Interactions Abstract The main aim of this work was to assess the potential formation of ternary chelate complexes, involving deferasirox (DFX), ciprofloxacin (CP), and ferric iron. The coadministra... |
PMC7994213 | core_pubmed_pmc | Sotalol does not interfere with the antielectroshock action of selected second-generation antiepileptic drugs in mice | Sotalol does not interfere with the antielectroshock action of selected second-generation antiepileptic drugs in mice Abstract Background Due to blocking β-receptors, and potassium KCNH2 channels, sotalol may influence seizure phenomena. In the previous study, we have shown that sotalol potentiated the antielectroshock... |
PMC11015068 | core_pubmed_pmc | Establishment of the HPLC fluorescence detection method for plasma trace ivermectin and its pharmacokinetics in Bactrian camel | Establishment of the HPLC fluorescence detection method for plasma trace ivermectin and its pharmacokinetics in Bactrian camel Abstract Abstract Background and objective Ivermectin (IVM), a widely used veterinary anthelmintic, lacks recommended doses for Bactrian camels. This study aims to establish its pharmacokinetic... |
PMC10212229 | core_pubmed_pmc | Physiologically-Based Pharmacokinetic Modeling of PAXLOVID™ with First-Order Absorption Kinetics | Physiologically-Based Pharmacokinetic Modeling of PAXLOVID™ with First-Order Absorption Kinetics Abstract Abstract Purpose PAXLOVID™ is nirmatrelvir tablets co-packaged with ritonavir tablets. Ritonavir is used as a pharmacokinetics (PK) enhancer to reduce metabolism and increase exposure of nirmatrelvir. This is the f... |
PMC12580930 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacokinetic‐Pharmacodynamic Analysis for Clazakizumab in Patients With End‐Stage Kidney Disease Undergoing Dialysis | Population Pharmacokinetic and Pharmacokinetic‐Pharmacodynamic Analysis for Clazakizumab in Patients With End‐Stage Kidney Disease Undergoing Dialysis Abstract ABSTRACT The inflammatory cytokine interleukin‐6 (IL‐6) plays a significant role in the progression of cardiovascular disease (CVD). We evaluated the impact of ... |
PMC10290475 | core_pubmed_pmc | One Rare Warfarin Resistance Case and Possible Mechanism Exploration | One Rare Warfarin Resistance Case and Possible Mechanism Exploration Abstract Abstract One 59-year-old female patient with deep venous thrombosis (DVT) and pulmonary embolism (PE) was treated with 6 mg warfarin once daily as an anticoagulant. Before taking warfarin, her international normalized ratio (INR) was 0.98. Tw... |
PMC11533105 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling predicts the drug interaction potential of GLS4 in co‐administered with ritonavir | Physiologically‐based pharmacokinetic modeling predicts the drug interaction potential of GLS4 in co‐administered with ritonavir Abstract Abstract GLS4 is a first‐in‐class hepatitis B virus (HBV) capsid assembly modulator (class I) that is co‐administered with ritonavir to maintain the anticipated concentration require... |
PMC12462604 | core_pubmed_pmc | Developing a Two‐Sided Decision Box to Facilitate Shared Decision‐Making for Switching From Conventional to Pharmacokinetic‐Tailored Prophylaxis in Haemophilia | Developing a Two‐Sided Decision Box to Facilitate Shared Decision‐Making for Switching From Conventional to Pharmacokinetic‐Tailored Prophylaxis in Haemophilia Abstract ABSTRACT Introduction Decision‐making in haemophilia is challenging due to the small evidence base, disease heterogeneity, and inter‐patient variabilit... |
PMC11619381 | core_pubmed_pmc | Population pharmacokinetics of cabotegravir following intramuscular thigh injections in adults with and without HIV | Population pharmacokinetics of cabotegravir following intramuscular thigh injections in adults with and without HIV Abstract ABSTRACT Cabotegravir intramuscular gluteal injection is approved for HIV treatment (with rilpivirine) and prevention. Thigh muscle is a potential alternative injection site. We aim to characteri... |
PMC3681103 | core_pubmed_pmc | Topical Melatonin for Treatment of Androgenetic Alopecia | Topical Melatonin for Treatment of Androgenetic Alopecia Abstract Abstract Background: In the search for alternative agents to oral finasteride and topical minoxidil for the treatment of androgenetic alopecia (AGA), melatonin, a potent antioxidant and growth modulator, was identified as a promising candidate based on i... |
PMC3468617 | core_pubmed_pmc | Combinatorial Pharmacogenetic Interactions of Bucindolol and β 1 , α 2C Adrenergic Receptor Polymorphisms | Combinatorial Pharmacogenetic Interactions of Bucindolol and β 1 , α 2C Adrenergic Receptor Polymorphisms Abstract Abstract Background Pharmacogenetics involves complex interactions of gene products affecting pharmacodynamics and pharmacokinetics, but there is little information on the interaction of multiple genetic m... |
PMC9028383 | core_pubmed_pmc | The Influence of the CES1 Genotype on the Pharmacokinetics of Enalapril in Patients with Arterial Hypertension | The Influence of the CES1 Genotype on the Pharmacokinetics of Enalapril in Patients with Arterial Hypertension Abstract The angiotensin-converting enzyme inhibitor enalapril is hydrolysed to an active metabolite, enalaprilat, in the liver via carboxylesterase 1 (CES1). Previous studies show that variant rs71647871 in t... |
PMC3964022 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of acetylsalicylic acid after intravenous and oral administration to healthy volunteers | Pharmacokinetics and pharmacodynamics of acetylsalicylic acid after intravenous and oral administration to healthy volunteers Abstract Background The pharmacology of single doses of acetylsalicylic acid (ASA) administered intravenously (250 or 500 mg) or orally (100, 300, or 500 mg) was evaluated in a randomized, place... |
PMC8026019 | core_pubmed_pmc | Physiologically based metformin pharmacokinetics model of mice and scale-up to humans for the estimation of concentrations in various tissues | Physiologically based metformin pharmacokinetics model of mice and scale-up to humans for the estimation of concentrations in various tissues Abstract Metformin is the primary drug for type 2 diabetes treatment and a promising candidate for other disease treatment. It has significant deviations between individuals in t... |
PMC9304147 | core_pubmed_pmc | Drug–Drug Interactions in People Living With HIV at Risk of Hepatic and Renal Impairment: Current Status and Future Perspectives | Drug–Drug Interactions in People Living With HIV at Risk of Hepatic and Renal Impairment: Current Status and Future Perspectives Abstract Abstract Despite the advancement of antiretroviral therapy (ART) for the treatment of human immunodeficiency virus (HIV), drug–drug interactions (DDIs) remain a relevant clinical iss... |
PMC12435454 | core_pubmed_pmc | Ceftaroline pharmacokinetics/pharmacodynamics in the hollow-fibre model of Mycobacterium abscessus lung disease | Ceftaroline pharmacokinetics/pharmacodynamics in the hollow-fibre model of Mycobacterium abscessus lung disease Abstract SUMMARY BACKGROUND Guideline-based therapy (GBT) of Mycobacterium abscessus (MAB) lung disease (LD) achieves a sputum culture conversion rate in ∼35% of patients. The β-lactam antibiotics, imipenem a... |
PMC10110837 | core_pubmed_pmc | LZM008, a proposed tocilizumab biosimilar: Pharmacokinetics, safety, and immunogenicity profiles compared with ACTEMRA ® in Chinese healthy male subjects | LZM008, a proposed tocilizumab biosimilar: Pharmacokinetics, safety, and immunogenicity profiles compared with ACTEMRA ® in Chinese healthy male subjects Abstract Background: This study aimed to investigate the pharmacokinetics, safety, and immunogenicity of recombinant humanized anti-human IL-6R monoclonal antibody in... |
PMC7403548 | core_pubmed_pmc | Assessing the Impact of Losmapimod on Proteinuria in Idiopathic Focal Segmental Glomerulosclerosis | Assessing the Impact of Losmapimod on Proteinuria in Idiopathic Focal Segmental Glomerulosclerosis Abstract Abstract Introduction Idiopathic focal segmental glomerulosclerosis (FSGS) is a leading cause of nephrotic syndrome and end-stage renal disease. In preclinical models and biopsies of human FSGS kidneys, p38 mitog... |
PMC7749589 | core_pubmed_pmc | Safety and pharmacokinetics of bimagrumab in healthy older and obese adults with body composition changes in the older cohort | Safety and pharmacokinetics of bimagrumab in healthy older and obese adults with body composition changes in the older cohort Abstract Abstract Background Bimagrumab prevents activity of myostatin and other negative regulators of skeletal muscle mass. This randomized double‐blind, placebo‐controlled study investigated ... |
PMC3579462 | core_pubmed_pmc | Marqibo ® (vincristine sulfate liposome injection) improves the pharmacokinetics and pharmacodynamics of vincristine | Marqibo ® (vincristine sulfate liposome injection) improves the pharmacokinetics and pharmacodynamics of vincristine Abstract Vincristine (VCR) is a mainstay of treatment of hematologic malignancies and solid tumors due to its well-defined mechanism of action, demonstrated anticancer activity and its ability to be comb... |
PMC12199309 | core_pubmed_pmc | Isolation, structural elucidation, and integrated biological and computational evaluation of antidiabetic labdane diterpenes from Curcuma zedoaria rhizomes † | Isolation, structural elucidation, and integrated biological and computational evaluation of antidiabetic labdane diterpenes from Curcuma zedoaria rhizomes † Abstract The phytochemical investigation of the EtOAc-soluble extract of the rhizomes of Curcuma zedoaria (Berg.) Roscoe led to the isolation of five labdane-type... |
PMC3110144 | core_pubmed_pmc | BICEPP: an example-based statistical text mining method for predicting the binary characteristics of drugs | BICEPP: an example-based statistical text mining method for predicting the binary characteristics of drugs Abstract Background The identification of drug characteristics is a clinically important task, but it requires much expert knowledge and consumes substantial resources. We have developed a statistical text-mining ... |
PMC6504668 | core_pubmed_pmc | Enhanced transdermal permeability and drug deposition of rheumatoid arthritis via sinomenine hydrochloride-loaded antioxidant surface transethosome | Enhanced transdermal permeability and drug deposition of rheumatoid arthritis via sinomenine hydrochloride-loaded antioxidant surface transethosome Abstract Abstract Background: Transdermal drug delivery system (TDDS) curing rheumatoid arthritis (RA) for long-term treatment can improve patients’ compliance and reduce t... |
PMC12953180 | core_pubmed_pmc | Managing High‐Risk Drug Interactions With Nirmatrelvir/Ritonavir: Experience From a Dedicated Pharmacology Advice Service | Managing High‐Risk Drug Interactions With Nirmatrelvir/Ritonavir: Experience From a Dedicated Pharmacology Advice Service Abstract ABSTRACT Nirmatrelvir boosted with ritonavir is a key antiviral against COVID‐19, yet ritonavir's potent CYP3A4 inhibition exposes patients to numerous drug–drug interactions. To make presc... |
PMC3950770 | core_pubmed_pmc | The Dynamics of Compound, Transcript, and Protein Effects After Treatment With 2OMePS Antisense Oligonucleotides in mdx Mice | The Dynamics of Compound, Transcript, and Protein Effects After Treatment With 2OMePS Antisense Oligonucleotides in mdx Mice Abstract Antisense-mediated exon skipping is currently in clinical development for Duchenne muscular dystrophy (DMD) to amend the consequences of the underlying genetic defect and restore dystrop... |
PMC7997716 | core_pubmed_pmc | Immortalized Canine Dystrophic Myoblast Cell Lines for Development of Peptide-Conjugated Splice-Switching Oligonucleotides | Immortalized Canine Dystrophic Myoblast Cell Lines for Development of Peptide-Conjugated Splice-Switching Oligonucleotides Abstract Duchenne muscular dystrophy (DMD) is a severe muscle-wasting disease caused by frameshift or nonsense mutations in the DMD gene, resulting in the loss of dystrophin from muscle membranes. ... |
PMC9136610 | core_pubmed_pmc | Structure‒tissue exposure/selectivity relationship (STR) correlates with clinical efficacy/safety | Structure‒tissue exposure/selectivity relationship (STR) correlates with clinical efficacy/safety Abstract Drug optimization, which improves drug potency/specificity by structure‒activity relationship (SAR) and drug-like properties, is rigorously performed to select drug candidates for clinical trials. However, the cur... |
PMC10729942 | core_pubmed_pmc | Towards better antivenoms: navigating the road to new types of snakebite envenoming therapies | Towards better antivenoms: navigating the road to new types of snakebite envenoming therapies Abstract Abstract Snakebite envenoming is a significant global health challenge, and for over a century, traditional plasma-derived antivenoms from hyperimmunized animals have been the primary treatment against this infliction... |
PMC11684200 | core_pubmed_pmc | Vedolizumab serum trough concentrations with and without thiopurines in ulcerative colitis: The prospective VIEWS pharmacokinetics study | Vedolizumab serum trough concentrations with and without thiopurines in ulcerative colitis: The prospective VIEWS pharmacokinetics study Abstract BACKGROUND Ulcerative colitis (UC) is a chronic inflammatory condition requiring continuous treatment and monitoring. There is limited pharmacokinetic data on vedolizumab dur... |
PMC11510293 | core_pubmed_pmc | Optimization and Appraisal of Nintedanib-Loaded Mixed Polymeric Micelles as a Potential Nanovector for Non-Invasive Pulmonary Fibrosis Mitigation | Optimization and Appraisal of Nintedanib-Loaded Mixed Polymeric Micelles as a Potential Nanovector for Non-Invasive Pulmonary Fibrosis Mitigation Abstract Abstract Background/Objectives: Nintedanib (NTD), a triple tyrosine kinase receptor inhibitor, is the recommended first-line tackling option for idiopathic pulmonary... |
PMC8695949 | core_pubmed_pmc | Development and validation of a sensitive LC-MS/MS method for pioglitazone: application towards pharmacokinetic and tissue distribution study in rats † | Development and validation of a sensitive LC-MS/MS method for pioglitazone: application towards pharmacokinetic and tissue distribution study in rats † Abstract Abstract In the present study, a sensitive LC-MS/MS method was developed and validated to measure pioglitazone (PGZ) concentrations in rat plasma and tissues. ... |
PMC8561403 | core_pubmed_pmc | Pharmacokinetics and Perceptions of Children and Young Adults Using Cannabis for Attention-Deficit/Hyperactivity Disorder and Oppositional Defiant Disorder: Protocol for a Mixed Methods Proof-of-Concept Study | Pharmacokinetics and Perceptions of Children and Young Adults Using Cannabis for Attention-Deficit/Hyperactivity Disorder and Oppositional Defiant Disorder: Protocol for a Mixed Methods Proof-of-Concept Study Abstract Abstract Background Despite the lack of evidence on the use of cannabis for the treatment of attention... |
PMC9385814 | core_pubmed_pmc | Nicotine pharmacokinetics and subjective responses after using nicotine pouches with different nicotine levels compared to combustible cigarettes and moist smokeless tobacco in adult tobacco users | Nicotine pharmacokinetics and subjective responses after using nicotine pouches with different nicotine levels compared to combustible cigarettes and moist smokeless tobacco in adult tobacco users Abstract Abstract Rationale Oral tobacco–derived nicotine products include on!® nicotine pouches (NPs) which are tobacco-le... |
PMC7759686 | core_pubmed_pmc | Pharmacokinetics and Immunological Effects of Romidepsin in Rhesus Macaques | Pharmacokinetics and Immunological Effects of Romidepsin in Rhesus Macaques Abstract Abstract HIV/SIV persistence in latent reservoirs requires lifelong antiretroviral treatment and calls for effective cure strategies. Romidepsin (RMD), a histone deacetylase inhibitor, was reported to reactivate HIV/SIV from reservoirs... |
PMC12562105 | core_pubmed_pmc | Long-Term Efficacy and Safety of Inhaled Cannabis Therapy for Painful Diabetic Neuropathy: A 5-Year Longitudinal Observational Study | Long-Term Efficacy and Safety of Inhaled Cannabis Therapy for Painful Diabetic Neuropathy: A 5-Year Longitudinal Observational Study Abstract Background/Objectives: Diabetic neuropathy (DN) is a prevalent complication of diabetes mellitus, affecting up to 50% of long-term patients and causing significant pain, reduced ... |
PMC12596122 | core_pubmed_pmc | Long-acting Cabotegravir/Rilpivirine for Treatment of HIV During Pregnancy: A Case Series | Long-acting Cabotegravir/Rilpivirine for Treatment of HIV During Pregnancy: A Case Series Abstract Abstract We present pharmacokinetic data on long-acting cabotegravir/rilpivirine (LA CAB/RPV) from two patients during their second and third trimesters. Monthly LA CAB/RPV dosing maintained concentrations above the propo... |
PMC12753994 | core_pubmed_pmc | Integrated in silico – in vitro and pharmacokinetic profiling of Thymus vulgaris -derived metabolites targeting multidrug resistance pathways in extensively drug-resistant Acinetobacter baumannii (muks92) | Integrated in silico – in vitro and pharmacokinetic profiling of Thymus vulgaris -derived metabolites targeting multidrug resistance pathways in extensively drug-resistant Acinetobacter baumannii (muks92) Abstract Abstract Background Acinetobacter baumannii is a major nosocomial pathogen with extensive drug resistance ... |
PMC8165381 | core_pubmed_pmc | Transcriptional Regulation of Drug Metabolizing CYP Enzymes by Proinflammatory Wnt5A Signaling in Human Coronary Artery Endothelial Cells | Transcriptional Regulation of Drug Metabolizing CYP Enzymes by Proinflammatory Wnt5A Signaling in Human Coronary Artery Endothelial Cells Abstract Abstract Downregulation of drug metabolizing enzymes and transporters by proinflammatory mediators in hepatocytes, enterocytes and renal tubular epithelium is an established... |
PMC12579717 | core_pubmed_pmc | Comparison of Three Mathematical Models of the Pharmacokinetics of Heparin to Guide the Use of Protamine in a Large Simulated Cohort of Patients | Comparison of Three Mathematical Models of the Pharmacokinetics of Heparin to Guide the Use of Protamine in a Large Simulated Cohort of Patients Abstract Abstract Background: In cardiac surgery, protamine is used to reverse the effects of heparin after separation from cardiopulmonary bypass (CPB). Excess of protamine h... |
PMC11685120 | core_pubmed_pmc | Anticoagulation approach in morbid obesity: a comprehensive review on venous thromboembolism management | Anticoagulation approach in morbid obesity: a comprehensive review on venous thromboembolism management Abstract Obesity is a recognized risk factor for venous thromboembolism (VTE), associated with distinct challenges in managing anticoagulation therapy. There is still limited evidence regarding the impact of extreme ... |
PMC9138651 | core_pubmed_pmc | Targeted Strategy in Lipid-Lowering Therapy | Targeted Strategy in Lipid-Lowering Therapy Abstract Abstract Dyslipidemia is characterized by a diminished lipid profile, including increased level of total cholesterol and low-density lipoprotein cholesterol (LDL-c) and reduced level of high-density lipoprotein cholesterol (HDL-c). Lipid-lowering agents represent an ... |
PMC12551048 | core_pubmed_pmc | Optimizing Mycophenolate Therapy in Renal Transplant Patients Using Machine Learning and Population Pharmacokinetic Modeling | Optimizing Mycophenolate Therapy in Renal Transplant Patients Using Machine Learning and Population Pharmacokinetic Modeling Abstract Abstract Background/Objectives: Mycophenolic acid (MPA) is used as part of first-line combination immunosuppressive therapy for renal transplant recipients. Personalized dosing approache... |
PMC3359440 | core_pubmed_pmc | Sildenafil, a phosphodiesterase type 5 inhibitor, enhances the antidepressant activity of amitriptyline but not desipramine, in the forced swim test in mice | Sildenafil, a phosphodiesterase type 5 inhibitor, enhances the antidepressant activity of amitriptyline but not desipramine, in the forced swim test in mice Abstract Abstract The cholinergic theory of depression highlights the involvement of muscarinic acetylcholine receptors in the neurobiology of mood disorders. The ... |
PMC4317919 | core_pubmed_pmc | Phase I / II study of brentuximab vedotin in Japanese patients with relapsed or refractory CD30-positive Hodgkin's lymphoma or systemic anaplastic large-cell lymphoma | Phase I / II study of brentuximab vedotin in Japanese patients with relapsed or refractory CD30-positive Hodgkin's lymphoma or systemic anaplastic large-cell lymphoma Abstract Brentuximab vedotin is an antibody–drug conjugate that selectively delivers the antimicrotubule agent monomethyl auristatin E into CD30-expressi... |
PMC5102573 | core_pubmed_pmc | Pharmacokinetic Evaluation of a Drug Transporter Cocktail Consisting of Digoxin, Furosemide, Metformin, and Rosuvastatin | Pharmacokinetic Evaluation of a Drug Transporter Cocktail Consisting of Digoxin, Furosemide, Metformin, and Rosuvastatin Abstract Abstract This article reports the clinical investigation of a probe drug cocktail containing substrates of key drug transporters. Single oral doses of 0.25 mg digoxin (P‐gp), 5 mg furosemide... |
PMC8558846 | core_pubmed_pmc | An oral lipidic native testosterone formulation that is absorbed independent of food | An oral lipidic native testosterone formulation that is absorbed independent of food Abstract Abstract Context There is no licensed oral native testosterone (NT) because of challenges in the formulation. Licensed oral formulations of the ester, testosterone undecanoate (TU), require a meal for absorption and generate s... |
PMC8175292 | core_pubmed_pmc | Clinical validity of increased cortical binding of tau ligands of the THK family and PBB3 on PET as biomarkers for Alzheimer’s disease in the context of a structured 5-phase development framework | Clinical validity of increased cortical binding of tau ligands of the THK family and PBB3 on PET as biomarkers for Alzheimer’s disease in the context of a structured 5-phase development framework Abstract Abstract Purpose The research community has focused on defining reliable biomarkers for the early detection of the ... |
PMC6766828 | core_pubmed_pmc | LC–MS/MS Method for Simultaneous Determination of Linarin and Its Metabolites in Rat Plasma and Liver Tissue Samples: Application to Pharmacokinetic and Liver Tissue Distribution Study After Oral Administration of Linarin | LC–MS/MS Method for Simultaneous Determination of Linarin and Its Metabolites in Rat Plasma and Liver Tissue Samples: Application to Pharmacokinetic and Liver Tissue Distribution Study After Oral Administration of Linarin Abstract Linarin, a flavone glycoside, is considered to be a promising natural product due to its ... |
PMC12072222 | core_pubmed_pmc | Genotype, Ethnicity, and Drug–Drug Interaction Modeling as Means of Verifying Transporter Biomarker PBPK Model: The Coproporphyrin‐I Story | Genotype, Ethnicity, and Drug–Drug Interaction Modeling as Means of Verifying Transporter Biomarker PBPK Model: The Coproporphyrin‐I Story Abstract ABSTRACT Coproporphyrin‐I (CP‐I) is a selective endogenous biomarker of organic anion‐transporting polypeptide (OATP)1B. Multiple CP‐I PBPK models with differing input para... |
PMC11015076 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling of prominent oral contraceptive agents and applications in drug–drug interactions | Physiologically‐based pharmacokinetic modeling of prominent oral contraceptive agents and applications in drug–drug interactions Abstract Abstract Considerable interest remains across the pharmaceutical industry and regulatory landscape in capabilities to model oral contraceptives (OCs), whether combined (COCs) with et... |
PMC4035221 | core_pubmed_pmc | Molecular pharmacodynamics of new oral drugs used in the treatment of multiple sclerosis | Molecular pharmacodynamics of new oral drugs used in the treatment of multiple sclerosis Abstract Abstract New oral drugs have considerably enriched the therapeutic armamentarium for the treatment of multiple sclerosis. This review focuses on the molecular pharmacodynamics of fingolimod, dimethyl fumarate (BG-12), laqu... |
PMC11289896 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of asundexian in healthy Chinese and Japanese volunteers, and comparison with Caucasian data | Pharmacokinetics, pharmacodynamics, and safety of asundexian in healthy Chinese and Japanese volunteers, and comparison with Caucasian data Abstract Abstract There is an unmet clinical need for effective anticoagulant therapies for the management of thromboembolic diseases that are not associated with a relevant risk o... |
PMC7214647 | core_pubmed_pmc | Ubrogepant Is Not Associated With Clinically Meaningful Elevations of Alanine Aminotransferase in Healthy Adult Males | Ubrogepant Is Not Associated With Clinically Meaningful Elevations of Alanine Aminotransferase in Healthy Adult Males Abstract Abstract Ubrogepant is a novel, oral calcitonin gene‐related peptide (CGRP) receptor antagonist intended for the acute treatment of migraine attacks. Ubrogepant has a chemical structure distinc... |
PMC6419354 | core_pubmed_pmc | Therapeutic efficacy, pharmacokinetic profiles, and toxicological activities of humanized antibody-drug conjugate Zt/g4-MMAE targeting RON receptor tyrosine kinase for cancer therapy | Therapeutic efficacy, pharmacokinetic profiles, and toxicological activities of humanized antibody-drug conjugate Zt/g4-MMAE targeting RON receptor tyrosine kinase for cancer therapy Abstract Abstract Background Aberrant expression of the RON receptor tyrosine kinase is a pathogenic feature and a validated drug target ... |
PMC11326189 | core_pubmed_pmc | Computational modeling of drug response identifies mutant-specific constraints for dosing panRAF and MEK inhibitors in melanoma | Computational modeling of drug response identifies mutant-specific constraints for dosing panRAF and MEK inhibitors in melanoma Abstract Abstract Purpose: This study explores the potential of preclinical in vitro cell line response data and computational modeling in identifying optimal dosage requirements of pan-RAF (B... |
PMC11768951 | core_pubmed_pmc | Drug-Drug Interactions Between HIV Antivirals and Concomitant Drugs in HIV Patients: What We Know and What We Need to Know | Drug-Drug Interactions Between HIV Antivirals and Concomitant Drugs in HIV Patients: What We Know and What We Need to Know Abstract Abstract Highly active antiretroviral therapy has led to a significant increase in the life expectancy of people living with HIV. The trade-off is that HIV-infected patients often suffer f... |
PMC9505538 | core_pubmed_pmc | P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure | P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure Abstract EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR). It targets T... |
PMC12671050 | core_pubmed_pmc | Cerebrospinal fluid and plasma pharmacokinetics of ceftazidime/avibactam in a neurocritical patient with CRKP intracranial infection and augmented renal clearance | Cerebrospinal fluid and plasma pharmacokinetics of ceftazidime/avibactam in a neurocritical patient with CRKP intracranial infection and augmented renal clearance Abstract Abstract Background Intracranial infections caused by carbapenem-resistant Klebsiella pneumoniae (CRKP) pose significant therapeutic challenges, pri... |
PMC7555349 | core_pubmed_pmc | 1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study | 1,4-Disubstituted-1,2,3-Triazole Compounds Induce Ultrastructural Alterations in Leishmania amazonensis Promastigote: An in Vitro Antileishmanial and in Silico Pharmacokinetic Study Abstract The current standard treatment for leishmaniasis has remained the same for over 100 years, despite inducing several adverse effec... |
PMC12262575 | core_pubmed_pmc | Open-science discovery of DNDI-6510, a compound that addresses genotoxic and metabolic liabilities of the COVID Moonshot SARS-CoV-2 Mpro lead inhibitor | Open-science discovery of DNDI-6510, a compound that addresses genotoxic and metabolic liabilities of the COVID Moonshot SARS-CoV-2 Mpro lead inhibitor Abstract Abstract The 2020 SARS-CoV-2 coronavirus pandemic highlighted the urgent need for novel small molecule antiviral drugs. (S)- x38 DNDI-6510 is a non-covalent SA... |
PMC6376350 | core_pubmed_pmc | Development and evaluation of isradipine via rutin-loaded coated solid–lipid nanoparticles | Development and evaluation of isradipine via rutin-loaded coated solid–lipid nanoparticles Abstract The objective was to develop a stable and non-compliance coated solid–lipid nanoparticles (coated SLN) using polymer (Eudragit L100) and lipoid (glycerol monostearate: soya lecithin) for partial dose reduction of isradip... |
PMC8262897 | core_pubmed_pmc | Potent Killing of Pseudomonas aeruginosa by an Antibody-Antibiotic Conjugate | Potent Killing of Pseudomonas aeruginosa by an Antibody-Antibiotic Conjugate Abstract ABSTRACT Pseudomonas aeruginosa causes life-threatening infections that are associated with antibiotic failure. Previously, we identified the antibiotic G2637, an analog of arylomycin, targeting bacterial type I signal peptidase, whic... |
PMC6918900 | core_pubmed_pmc | Concentration-Dependent Activity of Hydromethylthionine on Cognitive Decline and Brain Atrophy in Mild to Moderate Alzheimer’s Disease | Concentration-Dependent Activity of Hydromethylthionine on Cognitive Decline and Brain Atrophy in Mild to Moderate Alzheimer’s Disease Abstract Background: Although hydromethylthionine is a potent tau aggregation inhibitor, no difference was found in either of two Phase III trials in mild to moderate Alzheimer’s diseas... |
PMC9285051 | core_pubmed_pmc | Highly sensitive quantification of pemetrexed in human plasma using UPLC‐MS/MS to support microdosing studies | Highly sensitive quantification of pemetrexed in human plasma using UPLC‐MS/MS to support microdosing studies Abstract Abstract Pemetrexed is an antifolate drug approved for the treatment of non‐small‐cell lung cancer and mesothelioma. Assessing pemetrexed pharmacokinetics after administration of a microdose (100 μg) m... |
PMC12901815 | core_pubmed_pmc | Preclinical pharmacokinetics and tissue distribution of a polyhexamethylene guanidine derivative after ocular mucosal administration | Preclinical pharmacokinetics and tissue distribution of a polyhexamethylene guanidine derivative after ocular mucosal administration Abstract Antibiotic resistance is a critical medical issue. Antiseptics, which play a key role in treating and preventing eye infections and inflammations, have the potential to induce re... |
PMC10829176 | core_pubmed_pmc | A pilot study investigating plasma pharmacokinetics and tolerance of oral capecitabine in carcinoma-bearing dogs | A pilot study investigating plasma pharmacokinetics and tolerance of oral capecitabine in carcinoma-bearing dogs Abstract Abstract Background Capecitabine is an oral prodrug of the active metabolite 5-fluorouracil, which has been used effectively in human colorectal, head and neck, and mammary carcinomas. Capecitabine ... |
PMC12860887 | core_pubmed_pmc | Association of Proton Pump Inhibitor and Potassium‐Competitive Acid Blocker Use With Discontinuation and Intolerance of Oral 5‐Aminosalicylic Acid in Patients With Ulcerative Colitis | Association of Proton Pump Inhibitor and Potassium‐Competitive Acid Blocker Use With Discontinuation and Intolerance of Oral 5‐Aminosalicylic Acid in Patients With Ulcerative Colitis Abstract ABSTRACT Aims Proton pump inhibitors (PPIs) and potassium‐competitive acid blockers (PCABs) are widely used for acid‐related dis... |
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