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PMC5387971 | core_pubmed_pmc | Relative bioavailability of single doses of prolonged-release tacrolimus administered as a suspension, orally or via a nasogastric tube, compared with intact capsules: a phase 1 study in healthy participants | Relative bioavailability of single doses of prolonged-release tacrolimus administered as a suspension, orally or via a nasogastric tube, compared with intact capsules: a phase 1 study in healthy participants Abstract Abstract Objective Tacrolimus, an immunosuppressant widely used in solid organ transplantation, is avai... |
PMC11199918 | core_pubmed_pmc | Parameter grouping and co-estimation in physiologically based kinetic models using genetic algorithms | Parameter grouping and co-estimation in physiologically based kinetic models using genetic algorithms Abstract Abstract Physiologically based kinetic (PBK) models are widely used in pharmacology and toxicology for predicting the internal disposition of substances upon exposure, voluntarily or not. Due to their complexi... |
PMC8411307 | core_pubmed_pmc | Neuropharmacology of Antiseizure Drugs | Neuropharmacology of Antiseizure Drugs Abstract Abstract Background Antiseizure drugs (ASDs) are the primary therapy for epilepsy, with more than 20 drugs introduced into clinical practice to date. These drugs are typically grouped by their mechanisms of action and therapeutic spectrum. This article aims to educate non... |
PMC10417080 | core_pubmed_pmc | Phase I study of cisplatin and nanoparticle albumin‐bound‐paclitaxel combined with concurrent radiotherapy in locally advanced esophageal squamous cell carcinoma | Phase I study of cisplatin and nanoparticle albumin‐bound‐paclitaxel combined with concurrent radiotherapy in locally advanced esophageal squamous cell carcinoma Abstract Abstract Background This phase I study aimed to assess the safety, dose‐limiting toxicity (DLT), maximum tolerated dose (MTD) and preliminary effect ... |
PMC6292857 | core_pubmed_pmc | Pharmacokinetic Interactions of Clinical Interest Between Direct Oral Anticoagulants and Antiepileptic Drugs | Pharmacokinetic Interactions of Clinical Interest Between Direct Oral Anticoagulants and Antiepileptic Drugs Abstract Abstract Direct oral anticoagulants (DOACs), namely apixaban, dabigatran, edoxaban, and rivaroxaban are being increasingly prescribed among the general population, as they are considered to be associate... |
PMC6429499 | core_pubmed_pmc | Pharmacokinetic and Metabolomic Studies with BIO 300, a Nanosuspension of Genistein, in a Nonhuman Primate Model | Pharmacokinetic and Metabolomic Studies with BIO 300, a Nanosuspension of Genistein, in a Nonhuman Primate Model Abstract Genistein is a naturally occurring phytoestrogen isoflavone and is the active drug ingredient in BIO 300, a radiation countermeasure under advanced development for acute radiation syndrome (H-ARS) a... |
PMC8883311 | core_pubmed_pmc | Cefepime Dosing Requirements in Elderly Patients Attended in the Emergency Rooms | Cefepime Dosing Requirements in Elderly Patients Attended in the Emergency Rooms Abstract Abstract Objective This study aimed to assess the probability of reaching an adequate pharmacokinetic/pharmacodynamic (pK/pD) index for different cefepime dosages in frail patients with bacteremia treated in the emergency room. Me... |
PMC8892321 | core_pubmed_pmc | A deep eutectic-based, self-emulsifying subcutaneous depot system for apomorphine therapy in Parkinson’s disease | A deep eutectic-based, self-emulsifying subcutaneous depot system for apomorphine therapy in Parkinson’s disease Abstract Significance Parkinson’s disease (PD) is a progressive disorder of the central nervous system that affects motor control. While subcutaneous injection of apomorphine (Apokyn) is clinically used to a... |
PMC7354648 | core_pubmed_pmc | Effect of Cellgevity® Supplement on Selected Rat Liver Cytochrome P450 Enzyme Activity and Pharmacokinetic Parameters of Carbamazepine | Effect of Cellgevity® Supplement on Selected Rat Liver Cytochrome P450 Enzyme Activity and Pharmacokinetic Parameters of Carbamazepine Abstract Abstract Background There is considerable evidence that many patients concurrently administer dietary supplements with conventional drugs, creating a risk for potential drug-su... |
PMC4448518 | core_pubmed_pmc | A rare case of delayed subarachnoid anesthetic blockade effects in a 103-year-old female patient | A rare case of delayed subarachnoid anesthetic blockade effects in a 103-year-old female patient Abstract Background: The elderly represent a unique challenge for the effects of regional anesthesia, and very few cases of block onset delay have been described. Their delayed response is attributed to a number of factors ... |
PMC8968419 | core_pubmed_pmc | Exploring Dried Blood Spot Cortisol Concentrations as an Alternative for Monitoring Pediatric Adrenal Insufficiency Patients: A Model-Based Analysis | Exploring Dried Blood Spot Cortisol Concentrations as an Alternative for Monitoring Pediatric Adrenal Insufficiency Patients: A Model-Based Analysis Abstract Abstract Congenital adrenal hyperplasia (CAH) is the most common form of adrenal insufficiency in childhood; it requires cortisol replacement therapy with hydroco... |
PMC9652432 | core_pubmed_pmc | An evaluation of a supratherapeutic dose of inclisiran on cardiac repolarization in healthy volunteers: A phase I, randomized study | An evaluation of a supratherapeutic dose of inclisiran on cardiac repolarization in healthy volunteers: A phase I, randomized study Abstract Abstract Inclisiran is a small interfering RNA molecule that has been shown to provide an effective and sustained reduction in low‐density lipoprotein cholesterol levels. This stu... |
PMC7317421 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Liver‐Targeting Acetyl‐CoA Carboxylase Inhibitor (PF‐05221304): A Three‐Part Randomized Phase 1 Study | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Liver‐Targeting Acetyl‐CoA Carboxylase Inhibitor (PF‐05221304): A Three‐Part Randomized Phase 1 Study Abstract Abstract PF‐05221304 is a liver‐targeted inhibitor of acetyl‐CoA carboxylase, an enzyme that catalyzes the first committed step in de novo lipo... |
PMC9835114 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling for primary metabolites of CYP3A and P‐glycoprotein inhibitors in drug–drug interactions: Should we assume the free drug hypothesis? | Physiologically‐based pharmacokinetic modeling for primary metabolites of CYP3A and P‐glycoprotein inhibitors in drug–drug interactions: Should we assume the free drug hypothesis? Modeling PBPK models of itraconazole and verapamil PBPK modeling is a mechanistic approach to quantitatively describe in vivo drug concentra... |
PMC4621192 | core_pubmed_pmc | Safety and pharmacokinetics of dicloxacillin in healthy Chinese volunteers following single and multiple oral doses | Safety and pharmacokinetics of dicloxacillin in healthy Chinese volunteers following single and multiple oral doses Abstract Background Dicloxacillin, a semisynthetic isoxazolyl penicillin antibiotic, has antimicrobial activity against a wide variety of gram-positive bacteria including Staphylococcus aureus , Streptoco... |
PMC4968608 | core_pubmed_pmc | Phase I study of palbociclib, a cyclin‐dependent kinase 4/6 inhibitor, in Japanese patients | Phase I study of palbociclib, a cyclin‐dependent kinase 4/6 inhibitor, in Japanese patients Abstract Abstract This phase I study in Japanese patients evaluated the safety, pharmacokinetics, and preliminary efficacy of palbociclib, a highly selective and reversible oral cyclin‐dependent kinase 4/6 inhibitor, as monother... |
PMC12445284 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Immunogenicity of CM313 in Healthy Participants: An Open‐Label/Double‐Blind, Randomized, Placebo‐Controlled Phase 1 Trial | Pharmacokinetics, Pharmacodynamics, and Immunogenicity of CM313 in Healthy Participants: An Open‐Label/Double‐Blind, Randomized, Placebo‐Controlled Phase 1 Trial Abstract ABSTRACT CM313, a novel humanized anti‐CD38 monoclonal antibody, has demonstrated therapeutic potential in autoimmune diseases. This Phase 1 trial ev... |
PMC5467944 | core_pubmed_pmc | The safety and pharmacokinetics of rapid iloprost aerosol delivery via the BREELIB nebulizer in pulmonary arterial hypertension | The safety and pharmacokinetics of rapid iloprost aerosol delivery via the BREELIB nebulizer in pulmonary arterial hypertension Abstract The BREELIB nebulizer was developed for iloprost to reduce inhalation times for patients with pulmonary arterial hypertension (PAH). This multicenter, randomized, unblinded, four-part... |
PMC3114339 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Therapeutic Doses of Basal Insulins NPH, Glargine, and Detemir After 1 Week of Daily Administration at Bedtime in Type 2 Diabetic Subjects | Pharmacokinetics and Pharmacodynamics of Therapeutic Doses of Basal Insulins NPH, Glargine, and Detemir After 1 Week of Daily Administration at Bedtime in Type 2 Diabetic Subjects Abstract OBJECTIVE To compare the pharmacokinetics and pharmacodynamics of NPH, glargine, and detemir insulins in type 2 diabetic subjects. ... |
PMC7689305 | core_pubmed_pmc | Systems and Clinical Pharmacology of COVID-19 Therapeutic Candidates: A Clinical and Translational Medicine Perspective | Systems and Clinical Pharmacology of COVID-19 Therapeutic Candidates: A Clinical and Translational Medicine Perspective Abstract Abstract Over 50 million people have been infected with the SARS-CoV-2 virus, while around 1 million have died due to COVID-19 disease progression. COVID-19 presents flu-like symptoms that ca... |
PMC7418156 | core_pubmed_pmc | Ethosome-Derived Invasomes as a Potential Transdermal Delivery System for Vardenafil Hydrochloride: Development, Optimization and Application of Physiologically Based Pharmacokinetic Modeling in Adults and Geriatrics | Ethosome-Derived Invasomes as a Potential Transdermal Delivery System for Vardenafil Hydrochloride: Development, Optimization and Application of Physiologically Based Pharmacokinetic Modeling in Adults and Geriatrics Abstract Aim The aim of the current work was to develop vardenafil hydrochloride (VRD)-loaded ethosome-... |
PMC5131373 | core_pubmed_pmc | Limitations of MIC as sole metric of pharmacodynamic response across the range of antimicrobial susceptibilities within a single bacterial species | Limitations of MIC as sole metric of pharmacodynamic response across the range of antimicrobial susceptibilities within a single bacterial species Abstract The minimum inhibitory concentration (MIC) of an antimicrobial drug for a bacterial pathogen is used as a measure of the bacterial susceptibility to the drug. Howev... |
PMC11858051 | core_pubmed_pmc | PK/PD Analysis of High-Dose Daptomycin Use in the Treatment of Bone and Joint Infections: Data from a Real-World Setting | PK/PD Analysis of High-Dose Daptomycin Use in the Treatment of Bone and Joint Infections: Data from a Real-World Setting Abstract Background: Daptomycin is widely used in bone and joint infections (BJIs) caused by Gram-positive cocci. The pharmacokinetics of daptomycin are characterized by relevant variability in terms... |
PMC10719089 | core_pubmed_pmc | IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial | IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial Abstract Abstract Toll-like receptor–driven and interleukin-1 (IL-1) receptor–driven inflammation mediated by IL-1 receptor–associated kinase 4 (IRAK4) is involved in the pathophysiology of hidradenitis suppurativa (HS) and atopic dermati... |
PMC12095254 | core_pubmed_pmc | Vancomycin dosing in neonates: enhancing outcomes using population pharmacokinetics and simulation | Vancomycin dosing in neonates: enhancing outcomes using population pharmacokinetics and simulation Abstract Introduction Optimizing vancomycin dosing in neonates is a critical yet complex goal. Traditional trough concentration-based dosing strategies correlate poorly with therapeutic efficacy and often fail to account ... |
PMC12078327 | core_pubmed_pmc | Quantifying the temporal trends of the combined effect of temperature and relative humidity on hand, foot, and mouth disease in Yunnan, China | Quantifying the temporal trends of the combined effect of temperature and relative humidity on hand, foot, and mouth disease in Yunnan, China Abstract Background Hand, foot, and mouth disease (HFMD) poses a significant risk to children. While most studies focus on the individual effects of temperature or relative humid... |
PMC12250075 | core_pubmed_pmc | The Pharmacokinetics of Saliva and Plasma N-Oxides Following a Single Administration of a Plant-Based Bioequivalent Inorganic Nitrate Oral Supplement in an Open-Label, Phase 1, Single-Arm Study | The Pharmacokinetics of Saliva and Plasma N-Oxides Following a Single Administration of a Plant-Based Bioequivalent Inorganic Nitrate Oral Supplement in an Open-Label, Phase 1, Single-Arm Study Abstract Abstract Background/Objective: Hypertension and other modifiable risk factors for cardiovascular disease are characte... |
PMC4749360 | core_pubmed_pmc | Calcitriol in Combination Therapy for Prostate Cancer: Pharmacokinetic and Pharmacodynamic Interactions | Calcitriol in Combination Therapy for Prostate Cancer: Pharmacokinetic and Pharmacodynamic Interactions Abstract Abstract Epidemiological studies indicate that vitamin D insufficiency could have an etiological role in prostate cancer. In addition, calcitriol, used in combination with currently available drugs, has the ... |
PMC12626967 | core_pubmed_pmc | A case report of drug–drug interaction between voriconazole and simnotrelvir/ritonavir | A case report of drug–drug interaction between voriconazole and simnotrelvir/ritonavir Abstract Abstract Co-administration of simnotrelvir/ritonavir with voriconazole should be avoided, as stated in the product insert of simnotrelvir/ritonavir, due to the anticipated decrease in the plasma concentration of voriconazole... |
PMC10144566 | core_pubmed_pmc | Pharmacokinetic Profile Evaluation of Novel Combretastatin Derivative, LASSBio-1920, as a Promising Colorectal Anticancer Agent | Pharmacokinetic Profile Evaluation of Novel Combretastatin Derivative, LASSBio-1920, as a Promising Colorectal Anticancer Agent Abstract LASSBio-1920 was synthesized due to the poor solubility of its natural precursor, combretastatin A4 (CA4). The cytotoxic potential of the compound against human colorectal cancer cell... |
PMC4686227 | core_pubmed_pmc | Idiopathic pulmonary fibrosis: current treatment options and critical appraisal of nintedanib | Idiopathic pulmonary fibrosis: current treatment options and critical appraisal of nintedanib Abstract Abstract Idiopathic pulmonary fibrosis (IPF) is the most common type of idiopathic interstitial pneumonia and is characterized by a poor prognosis, with an estimated 5-year survival of approximately 20%. Progressive a... |
PMC8766850 | core_pubmed_pmc | Integration Analysis of Pharmacokinetics and Metabolomics to Predict Metabolic Phenotype and Drug Exposure of Remdesivir | Integration Analysis of Pharmacokinetics and Metabolomics to Predict Metabolic Phenotype and Drug Exposure of Remdesivir Abstract Remdesivir has displayed pharmacological activity against SARS-CoV-2. However, no pharmacometabolomics (PM) or correlation analysis with pharmacokinetics (PK) was revealed. Rats were intrave... |
PMC8363697 | core_pubmed_pmc | Predicting Inter-individual Variability During Lipid Resuscitation of Bupivacaine Cardiotoxicity in Rats: A Virtual Population Modeling Study | Predicting Inter-individual Variability During Lipid Resuscitation of Bupivacaine Cardiotoxicity in Rats: A Virtual Population Modeling Study Abstract Introduction Intravenous lipid emulsions (ILE) have been credited for successful resuscitation in drug intoxication cases where other cardiac life-support methods have f... |
PMC12005340 | core_pubmed_pmc | Development and validation of a recombinant human TNF-α based ELISA to detect and quantify adalimumab | Development and validation of a recombinant human TNF-α based ELISA to detect and quantify adalimumab Abstract Adalimumab, a humanized IgG1 monoclonal antibody is currently used to treat inflammatory diseases. However, a sensitive, in-house ELISA for evaluating inter- and intra-individual pharmacokinetic variability of... |
PMC9718268 | core_pubmed_pmc | Tissue distribution of sprifermin (recombinant human fibroblast growth factor 18) in the rat following intravenous and intra-articular injection | Tissue distribution of sprifermin (recombinant human fibroblast growth factor 18) in the rat following intravenous and intra-articular injection Abstract Summary Objective Fibroblast growth factor 18 (FGF18) is involved in chondrogenesis and articular cartilage repair. We investigated tissue distribution and pharmacoki... |
PMC11472182 | core_pubmed_pmc | Nonclinical evaluations of deucravacitinib and Janus kinase inhibitors in homeostatic and inflammatory pathways | Nonclinical evaluations of deucravacitinib and Janus kinase inhibitors in homeostatic and inflammatory pathways Abstract Abstract Translational medicine provides insight into novel drugs and predicts unwanted effects. In well-characterized pathways (e.g., cytokine-Janus kinase [JAK]-signal transducers and activators of... |
PMC5698284 | core_pubmed_pmc | Pharmacokinetic, Ambulatory, and Hyperthermic Effects of 3,4-Methylenedioxy- N -Methylcathinone (Methylone) in Rats | Pharmacokinetic, Ambulatory, and Hyperthermic Effects of 3,4-Methylenedioxy- N -Methylcathinone (Methylone) in Rats Abstract Methylone (3,4-methylenedioxy- N -methylcathinone) is a synthetic cathinone analog of the recreational drug ecstasy. Although it is marketed to recreational users as relatively safe, fatalities d... |
PMC5911580 | core_pubmed_pmc | YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR L858R, T790M ‐mutant resistance in vitro and in vivo | YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR L858R, T790M ‐mutant resistance in vitro and in vivo Abstract Abstract YL143 was identified as a novel wild‐type sparing EGFR T790M inhibitor with good pharmacokinetic properties. It potently suppresses EGFR L858R/T790M with an 50% inhibitory c... |
PMC4337691 | core_pubmed_pmc | Population pharmacokinetics of pegaptanib sodium (Macugen ® ) in patients with diabetic macular edema | Population pharmacokinetics of pegaptanib sodium (Macugen ® ) in patients with diabetic macular edema Abstract Objective Population pharmacokinetic modeling of pegaptanib was undertaken to determine influence of renal function on apparent clearance. Methods In a randomized, double-masked multicenter trial, intravitreal... |
PMC11917174 | core_pubmed_pmc | A novel in vitro serum stability assay for antibody therapeutics incorporating internal standards | A novel in vitro serum stability assay for antibody therapeutics incorporating internal standards Abstract ABSTRACT Antibody-based therapeutics have demonstrated remarkable therapeutic benefit, but their susceptibility to biotransformation and degradation in the body can affect their safety, efficacy, and pharmacokinet... |
PMC9301000 | core_pubmed_pmc | Modeling Polygenic Antibiotic Resistance Evolution in Biofilms | Modeling Polygenic Antibiotic Resistance Evolution in Biofilms Abstract The recalcitrance of biofilms to antimicrobials is a multi-factorial phenomenon, including genetic, physical, and physiological changes. Individually, they often cannot account for biofilm recalcitrance. However, their combination can increase the ... |
PMC5627025 | core_pubmed_pmc | Monte Carlo Simulations Suggest Current Chlortetracycline Drug-Residue Based Withdrawal Periods Would Not Control Antimicrobial Resistance Dissemination from Feedlot to Slaughterhouse | Monte Carlo Simulations Suggest Current Chlortetracycline Drug-Residue Based Withdrawal Periods Would Not Control Antimicrobial Resistance Dissemination from Feedlot to Slaughterhouse Abstract Abstract Antimicrobial use in beef cattle can increase antimicrobial resistance prevalence in their enteric bacteria, including... |
PMC7277375 | core_pubmed_pmc | Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells | Garcinol Exhibits Anti-Neoplastic Effects by Targeting Diverse Oncogenic Factors in Tumor Cells Abstract Abstract Garcinol, a polyisoprenylated benzophenone, is the medicinal component obtained from fruits and leaves of Garcinia indica ( G. indica ) and has traditionally been extensively used for its antioxidant and an... |
PMC6051076 | core_pubmed_pmc | An Unusual Case of Ototoxicity with Use of Oral Vancomycin | An Unusual Case of Ototoxicity with Use of Oral Vancomycin Abstract Introduction Systemic absorption of oral vancomycin is poor due to the size of the molecule and its pharmacokinetics. It has an elimination half life of 5–11 hours in patients with normal renal function. We present a rare case of ototoxicity after oral... |
PMC8995781 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Relationships of Tulathromycin Against Actinobacillus pleuropneumoniae in a Porcine Tissue Cage Infection Model | Pharmacokinetic/Pharmacodynamic Relationships of Tulathromycin Against Actinobacillus pleuropneumoniae in a Porcine Tissue Cage Infection Model Abstract Tulathromycin is a semi-synthetic macrolide antibiotic that is highly effective in treating respiratory tract bacterial infections. We evaluated the in vivo antibacter... |
PMC5741785 | core_pubmed_pmc | Phase I dose-finding study of eribulin and capecitabine for metastatic breast cancer: JBCRG-18 cape study | Phase I dose-finding study of eribulin and capecitabine for metastatic breast cancer: JBCRG-18 cape study Abstract Abstract Background Eribulin is a nontaxane microtubule inhibitor with activity in patients with metastatic breast cancer (MBC). We conducted a phase I dose-finding study of eribulin and capecitabine in pa... |
PMC10851760 | core_pubmed_pmc | Pharmacological and mechanistic aspects of quercetin in osteoporosis | Pharmacological and mechanistic aspects of quercetin in osteoporosis Abstract Osteoporosis (OP) is a bone disease associated with increasing age. Currently, the most common medications used to treat OP are anabolic agents, anti-resorptive agents, and medications with other mechanisms of action. However, many of these m... |
PMC8973513 | core_pubmed_pmc | International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update | International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update Abstract Our previous International Union of Basic and Clinical Pharmacology report on the nomenclature and classification of adenosine receptors (2011) contained a number of emerging developments with respect to this G ... |
PMC8560969 | core_pubmed_pmc | Effect of CYP3A4 Inhibitors and Inducers on Pharmacokinetics and Pharmacodynamics of Saxagliptin and Active Metabolite M2 in Humans Using Physiological-Based Pharmacokinetic Combined DPP-4 Occupancy | Effect of CYP3A4 Inhibitors and Inducers on Pharmacokinetics and Pharmacodynamics of Saxagliptin and Active Metabolite M2 in Humans Using Physiological-Based Pharmacokinetic Combined DPP-4 Occupancy Abstract Abstract We aimed to develop a physiological-based pharmacokinetic and dipepidyl peptidase 4 (DPP-4) occupancy m... |
PMC7658763 | core_pubmed_pmc | Population pharmacokinetics and pharmacogenomics of tacrolimus in Chinese children receiving a liver transplant: initial dose recommendation | Population pharmacokinetics and pharmacogenomics of tacrolimus in Chinese children receiving a liver transplant: initial dose recommendation Abstract Abstract Background In order to improve the precision of treatment with tacrolimus in Chinese patients undergoing pediatric liver transplantation, the optimum initial dos... |
PMC9541759 | core_pubmed_pmc | Diagnostic Accuracy of Therapeutic Drug Monitoring During Tuberculosis Treatment | Diagnostic Accuracy of Therapeutic Drug Monitoring During Tuberculosis Treatment Abstract Abstract Patients with tuberculosis (TB) coinfected with HIV are more likely to have low blood concentrations of the first‐line anti‐TB drugs (associated with poor outcomes). Therapeutic drug monitoring (TDM) is recommended for ce... |
PMC8359408 | core_pubmed_pmc | Single‐Dose Pharmacokinetics and Safety of Atogepant in Adults With Hepatic Impairment: Results From an Open‐Label, Phase 1 Trial | Single‐Dose Pharmacokinetics and Safety of Atogepant in Adults With Hepatic Impairment: Results From an Open‐Label, Phase 1 Trial Abstract Abstract Atogepant is a selective oral calcitonin gene‐related peptide receptor antagonist in development for migraine prevention. Here, we report the pharmacokinetics (PK) and safe... |
PMC12311883 | core_pubmed_pmc | A Global Cross‐Sectional Database Study of Low Dose FVIII SHL Prophylaxis in Haemophilia A | A Global Cross‐Sectional Database Study of Low Dose FVIII SHL Prophylaxis in Haemophilia A Abstract ABSTRACT Introduction Haemophilia treatment is costly and only 25% of patients receive adequate care. Although not optimal, Factor VIII (FVIII) low‐dose prophylaxis (LDP) may reduce annual joint bleeding rates. Understan... |
PMC7359947 | core_pubmed_pmc | In Vitro ‐to‐ In Vivo Extrapolation of Transporter Inhibition Data for Drugs Approved by the US Food and Drug Administration in 2018 | In Vitro ‐to‐ In Vivo Extrapolation of Transporter Inhibition Data for Drugs Approved by the US Food and Drug Administration in 2018 Abstract Abstract A systematic analysis of the inhibition transporter data available in New Drug Applications of drugs approved by the US Food and Drug Administration (FDA) in 2018 ( N = ... |
PMC6825159 | core_pubmed_pmc | Evidence that fodipir (DPDP) binds neurotoxic Pt 2+ with a high affinity: An electron paramagnetic resonance study | Evidence that fodipir (DPDP) binds neurotoxic Pt 2+ with a high affinity: An electron paramagnetic resonance study Abstract Abstract Oxaliplatin typically causes acute neuropathic problems, which may, in a dose-dependent manner, develop into a chronic form of chemotherapy-induced peripheral neuropathy (CIPN), which is ... |
PMC7288841 | core_pubmed_pmc | Functionally Significant Coumarin-Related Variant Alleles and Time to Therapeutic Range in Chilean Cardiovascular Patients | Functionally Significant Coumarin-Related Variant Alleles and Time to Therapeutic Range in Chilean Cardiovascular Patients Abstract Despite the development of new oral agents over the last decade, vitamin K antagonists (VKAs) remain the most widely used anticoagulants for treating and preventing thromboembolism worldwi... |
PMC12603877 | core_pubmed_pmc | Pharmacodynamic Safety Endpoints for Propofol Anesthesia in Children by Age and Sex: A Multicohort Observational Study | Pharmacodynamic Safety Endpoints for Propofol Anesthesia in Children by Age and Sex: A Multicohort Observational Study Abstract ABSTRACT Background Propofol is a commonly used intravenous sedative and general anesthetic, with rapid onset and short duration of action. It has a narrow therapeutic index and significant in... |
PMC7417621 | core_pubmed_pmc | Pharmacokinetics of Pimobendan and Its Metabolite O-Desmethyl-Pimobendan Following Rectal Administration to Healthy Dogs | Pharmacokinetics of Pimobendan and Its Metabolite O-Desmethyl-Pimobendan Following Rectal Administration to Healthy Dogs Abstract Objective: This study describes the pharmacokinetics of parent pimobendan (PIM) and its active metabolite, o-desmethyl-pimobendan (ODMP), after oral and rectal administration of pimobendan t... |
PMC7357115 | core_pubmed_pmc | Bioanalytical Method Development and Validation of Veratraldehyde and Its Metabolite Veratric Acid in Rat Plasma: An Application for a Pharmacokinetic Study | Bioanalytical Method Development and Validation of Veratraldehyde and Its Metabolite Veratric Acid in Rat Plasma: An Application for a Pharmacokinetic Study Abstract Abstract A simple, sensitive, and rapid UHPLC-MS/MS method was developed for the simultaneous determination of veratraldehyde and its metabolite veratric ... |
PMC10272303 | core_pubmed_pmc | Population pharmacokinetics of tenofovir given as either tenofovir disoproxil fumarate or tenofovir alafenamide in an African population | Population pharmacokinetics of tenofovir given as either tenofovir disoproxil fumarate or tenofovir alafenamide in an African population Abstract Abstract Tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF) are prodrugs of the nucleotide analogue tenofovir, which acts intracellularly to inhibit HIV repl... |
PMC11924148 | core_pubmed_pmc | Discovering Severe Adverse Reactions From Pharmacokinetic Drug–Drug Interactions Through Literature Analysis and Electronic Health Record Verification | Discovering Severe Adverse Reactions From Pharmacokinetic Drug–Drug Interactions Through Literature Analysis and Electronic Health Record Verification Abstract While drug–drug interactions (DDIs) and their pharmacokinetic (PK) mechanisms are well‐studied prior to drug approval, severe adverse drug reactions (SADRs) cau... |
PMC11406655 | core_pubmed_pmc | Phase I/II study of the clinical activity and safety of GSK3326595 in patients with myeloid neoplasms | Phase I/II study of the clinical activity and safety of GSK3326595 in patients with myeloid neoplasms Abstract Background: GSK3326595 is a potent, selective, reversible protein arginine methyltransferase 5 (PRMT5) inhibitor under investigation for treatment of myelodysplastic syndrome (MDS), chronic myelomonocytic leuk... |
PMC11167448 | core_pubmed_pmc | Computational exploration of Picrasma quassioides compounds as CviR-mediated quorum sensing inhibitors against Chromobacterium violaceum | Computational exploration of Picrasma quassioides compounds as CviR-mediated quorum sensing inhibitors against Chromobacterium violaceum Abstract Abstract Chromobacterium violaceum an opportunistic human pathogenic bacterium, exhibits resistance to conventional antibiotics by exploiting its quorum sensing mechanism to ... |
PMC8757767 | core_pubmed_pmc | Multiple Sclerosis: LIFNano-CD4 for Trojan Horse Delivery of the Neuro-Protective Biologic “LIF” Into the Brain: Preclinical Proof of Concept | Multiple Sclerosis: LIFNano-CD4 for Trojan Horse Delivery of the Neuro-Protective Biologic “LIF” Into the Brain: Preclinical Proof of Concept Abstract Abstract Multiple sclerosis (MS) is a demyelinating autoimmune disease that attacks the brain, with year-on-year loss of brain volume, starting late teens and becoming m... |
PMC11607094 | core_pubmed_pmc | A global sensitivity analysis of a mechanistic model of neoadjuvant chemotherapy for triple negative breast cancer constrained by in vitro and in vivo imaging data | A global sensitivity analysis of a mechanistic model of neoadjuvant chemotherapy for triple negative breast cancer constrained by in vitro and in vivo imaging data Abstract Abstract Neoadjuvant chemotherapy (NAC) is a standard-of-care treatment for locally advanced triple negative breast cancer (TNBC) before surgery. T... |
PMC12651817 | core_pubmed_pmc | Beyond Weight Loss: Optimizing GLP-1 Receptor Agonist Use in Children | Beyond Weight Loss: Optimizing GLP-1 Receptor Agonist Use in Children Abstract Abstract Background/Objectives : Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have emerged as a transformative therapy for obesity and type 2 diabetes (T2D) in pediatric populations. This review synthesizes current evidence on effica... |
PMC7781482 | core_pubmed_pmc | Synergistic interaction between trazodone and gabapentin in rodent models of neuropathic pain | Synergistic interaction between trazodone and gabapentin in rodent models of neuropathic pain Abstract Abstract Neuropathic pain is a chronic debilitating condition caused by injury or disease of the nerves of the somatosensory system. Although several therapeutic approaches are recommended, none has emerged as an opti... |
PMC12878650 | core_pubmed_pmc | Case Report: Scurvy—a modifiable cause of psychiatric refractoriness and lithium pharmacokinetic abnormalities in autism | Case Report: Scurvy—a modifiable cause of psychiatric refractoriness and lithium pharmacokinetic abnormalities in autism Abstract Scurvy, although rare in developed countries, can notably occur in individuals with extreme dietary selectivity, particularly those with neurodevelopmental disorders. We describe the case of... |
PMC4720091 | core_pubmed_pmc | Phase I Study of CKD-516, a Novel Vascular Disrupting Agent, in Patients with Advanced Solid Tumors | Phase I Study of CKD-516, a Novel Vascular Disrupting Agent, in Patients with Advanced Solid Tumors Abstract Abstract Purpose CKD-516 is a newly developed vascular disrupting agent. This phase I dose-escalation study of CKD-516 was conducted to determine maximum-tolerated dose (MTD), safety, pharmacokinetics, and preli... |
PMC4767722 | core_pubmed_pmc | Applicability of a Single Time Point Strategy for the Prediction of Area Under the Concentration Curve of Linezolid in Patients: Superiority of C trough - over C max -Derived Linear Regression Models | Applicability of a Single Time Point Strategy for the Prediction of Area Under the Concentration Curve of Linezolid in Patients: Superiority of C trough - over C max -Derived Linear Regression Models Abstract Abstract Background and Objectives Linezolid, a oxazolidinone, was the first in class to be approved for the tr... |
PMC9300116 | core_pubmed_pmc | A randomized study of the safety and pharmacokinetics of GSK3358699, a mononuclear myeloid‐targeted bromodomain and extra‐terminal domain inhibitor | A randomized study of the safety and pharmacokinetics of GSK3358699, a mononuclear myeloid‐targeted bromodomain and extra‐terminal domain inhibitor Abstract Abstract Aims GSK3358699 is a mononuclear myeloid‐targeted bromodomain and extra‐terminal domain (BET) family inhibitor which demonstrates immunomodulatory effects... |
PMC8583760 | core_pubmed_pmc | Pharmacokinetic interaction between rhynchopylline and pellodendrine via CYP450 enzymes and P-gp | Pharmacokinetic interaction between rhynchopylline and pellodendrine via CYP450 enzymes and P-gp Abstract Abstract Context Rhynchopylline and pellodendrine are major extractions of commonly used Chinese medicine in gynaecology. The interaction between these two compounds could affect treatment efficiency and even resul... |
PMC11549183 | core_pubmed_pmc | Assessment of Abuse Liability and Nicotine Pharmacokinetics of glo Heated Tobacco Products in a Randomized, Crossover Study | Assessment of Abuse Liability and Nicotine Pharmacokinetics of glo Heated Tobacco Products in a Randomized, Crossover Study Abstract Abstract Background and Objective Heated tobacco products (HTPs) are a class of non-combustible, inhaled tobacco products with the potential to reduce the harm associated with cigarette s... |
PMC2858646 | core_pubmed_pmc | Exploiting Nanotechnologies and TRPV1 Channels to Investigate the Putative Anandamide Membrane Transporter | Exploiting Nanotechnologies and TRPV1 Channels to Investigate the Putative Anandamide Membrane Transporter Abstract Abstract Background Considerable efforts have been made to characterize the pathways regulating the extracellular levels of the endocannabinoid anandamide. However, none of such pathways has been so argue... |
PMC11919259 | core_pubmed_pmc | Mirikizumab pharmacokinetics and exposure–response in pediatric patients with moderate‐to‐severe ulcerative colitis | Mirikizumab pharmacokinetics and exposure–response in pediatric patients with moderate‐to‐severe ulcerative colitis Abstract Abstract Mirikizumab is a p19‐directed anti‐interleukin‐23 antibody approved for the treatment of adults with moderate‐to‐severe ulcerative colitis (UC). Here, we report the first data of mirikiz... |
PMC11279886 | core_pubmed_pmc | A Novel Lactose/MCC/L-HPC Triple-Based Co-Processed Excipients with Improved Tableting Performance Designed for Metoclopramide Orally Disintegrating Tablets | A Novel Lactose/MCC/L-HPC Triple-Based Co-Processed Excipients with Improved Tableting Performance Designed for Metoclopramide Orally Disintegrating Tablets Abstract Abstract New co-processed excipients comprising lactose (filler and sweetener), microcrystalline cellulose (MCC, filler), and low-substituted hydroxypropy... |
PMC6389131 | core_pubmed_pmc | Development and evaluation of novel tumor-targeting paclitaxel-loaded nano-carriers for ovarian cancer treatment: in vitro and in vivo | Development and evaluation of novel tumor-targeting paclitaxel-loaded nano-carriers for ovarian cancer treatment: in vitro and in vivo Abstract Abstract Background Ovarian cancer is the most leading cause of death and the third most common gynecologic malignancy in women. Traditional chemotherapy has inevitable drawbac... |
PMC9502688 | core_pubmed_pmc | Advances in Pharmacokinetic Mechanisms of Transporter-Mediated Herb-Drug Interactions | Advances in Pharmacokinetic Mechanisms of Transporter-Mediated Herb-Drug Interactions Abstract As the use of herbs has become more popular worldwide, there are increasing reports of herb-drug interactions (HDIs) following the combination of herbs and drugs. The active components of herbs are complex and have a variety ... |
PMC10732257 | core_pubmed_pmc | The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies | The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies Abstract Abstract To evade cell cycle controls, malignant cells rely upon rapid expression of select proteins to mitigate proapoptotic signa... |
PMC2855319 | core_pubmed_pmc | Flow-Based Cytometric Analysis of Cell Cycle via Simulated Cell Populations | Flow-Based Cytometric Analysis of Cell Cycle via Simulated Cell Populations Abstract We present a new approach to the handling and interrogating of large flow cytometry data where cell status and function can be described, at the population level, by global descriptors such as distribution mean or co-efficient of varia... |
PMC11671317 | core_pubmed_pmc | A randomized phase I study of the safety and pharmacokinetics of BI 1291583 in healthy Japanese male subjects | A randomized phase I study of the safety and pharmacokinetics of BI 1291583 in healthy Japanese male subjects Abstract Abstract Aims Bronchiectasis patients face an unmet need for treatment options that reduce inflammation. Cathepsin C inhibition is expected to achieve this by reducing the activation of neutrophil‐deri... |
PMC6790584 | core_pubmed_pmc | Updated Population Pharmacokinetic Model of Cabozantinib Integrating Various Cancer Types Including Hepatocellular Carcinoma | Updated Population Pharmacokinetic Model of Cabozantinib Integrating Various Cancer Types Including Hepatocellular Carcinoma Abstract Abstract An integrated population pharmacokinetic (PPK) model was used to evaluate the effects of liver dysfunction on the pharmacokinetics (PK) of cabozantinib in patients with hepatoce... |
PMC11544216 | core_pubmed_pmc | Prediction of vancomycin plasma concentration in elderly patients based on multi-algorithm mining combined with population pharmacokinetics | Prediction of vancomycin plasma concentration in elderly patients based on multi-algorithm mining combined with population pharmacokinetics Abstract The pharmacokinetics of vancomycin exhibit significant inter-individual variability, particularly among elderly patients. This study aims to develop a predictive model tha... |
PMC7722423 | core_pubmed_pmc | Citalopram intoxication in four week old infant | Citalopram intoxication in four week old infant Abstract Background In contrast to intoxications in toddlers which can be due to accidental ingestions, many intoxications in infants are due to medication errors . To our knowledge, this is the first case report of a citalopram intoxication in an infant, and may offer ne... |
PMC11449996 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of Dalbavancin and C-Reactive Protein in Patients with Staphylococcal Osteoarticular Infections | Population Pharmacokinetics and Pharmacodynamics of Dalbavancin and C-Reactive Protein in Patients with Staphylococcal Osteoarticular Infections Abstract Background and Objective Dalbavancin is increasingly used for the long-term treatment of chronic osteoarticular infections. A population pharmacokinetic/pharmacodynam... |
PMC6274395 | core_pubmed_pmc | Using Light Microscopy and Liquid Chromatography Tandem Mass Spectrometry for Qualitative and Quantitative Control of a Combined Three-Herb Formulation in Different Preparations | Using Light Microscopy and Liquid Chromatography Tandem Mass Spectrometry for Qualitative and Quantitative Control of a Combined Three-Herb Formulation in Different Preparations Abstract Abstract Artemisia capillaries Thunb, Gardenia jasminoides Ellis, and Rheum officinale Baill have been combined to treat jaundice for... |
PMC12922413 | core_pubmed_pmc | Phytochemical study of Homalanthus giganteus : isolation, antiproliferative activity, and computational mechanistic insights of tigliane diterpenes against colorectal cancer | Phytochemical study of Homalanthus giganteus : isolation, antiproliferative activity, and computational mechanistic insights of tigliane diterpenes against colorectal cancer Abstract Abstract Context Colorectal cancer is the third most common and second deadliest cancer worldwide. Late diagnosis, poor outcomes in metas... |
PMC11477725 | core_pubmed_pmc | Advancing Bioanalytical Method Validation: A Comprehensive ICH M10 Approach for Validating LC–MS/MS to Quantify Fluoxetine in Human Plasma and Its Application in Pharmacokinetic Studies | Advancing Bioanalytical Method Validation: A Comprehensive ICH M10 Approach for Validating LC–MS/MS to Quantify Fluoxetine in Human Plasma and Its Application in Pharmacokinetic Studies Abstract Abstract A fast and sample cleanup approach for fluoxetine in human plasma was developed using protein precipitation coupled ... |
PMC8724759 | core_pubmed_pmc | Plasma concentration guided dosing of drugs used for the treatment of childhood leukaemias: protocol for a systematic review | Plasma concentration guided dosing of drugs used for the treatment of childhood leukaemias: protocol for a systematic review Abstract Abstract Introduction Childhood leukaemia is the most common type of cancer in children and represents among 25% of the diagnoses in children <15 years old. Childhood survival rates have... |
PMC6496039 | core_pubmed_pmc | Generating Robust and Informative Nonclinical In Vitro and In Vivo Bacterial Infection Model Efficacy Data To Support Translation to Humans | Generating Robust and Informative Nonclinical In Vitro and In Vivo Bacterial Infection Model Efficacy Data To Support Translation to Humans Abstract In June 2017, the National Institute of Allergy and Infectious Diseases, part of the National Institutes of Health, organized a workshop entitled “Pharmacokinetics-Pharmac... |
PMC6997373 | core_pubmed_pmc | Renal cyst growth is attenuated by a combination treatment of tolvaptan and pioglitazone, while pioglitazone treatment alone is not effective | Renal cyst growth is attenuated by a combination treatment of tolvaptan and pioglitazone, while pioglitazone treatment alone is not effective Abstract Abstract Autosomal Dominant Polycystic Kidney Disease (ADPKD) is one of the most common monogenic disorders, characterized by the progressive formation of fluid-filled c... |
PMC11486673 | core_pubmed_pmc | Dynamic contrast enhanced high field magnetic resonance imaging for canine primary intracranial neoplasia | Dynamic contrast enhanced high field magnetic resonance imaging for canine primary intracranial neoplasia Abstract Abstract Introduction Distinguishing meningiomas from other intracranial neoplasms is clinically relevant as the prognostic and therapeutic implications differ greatly and influence clinical decision makin... |
PMC9124352 | core_pubmed_pmc | A modeling‐based proposal for safe and efficacious reintroduction of bedaquiline after dose interruption: A population pharmacokinetics study | A modeling‐based proposal for safe and efficacious reintroduction of bedaquiline after dose interruption: A population pharmacokinetics study Abstract Abstract Bedaquiline (BDQ) is recommended for treatment of multidrug‐resistant tuberculosis (MDR‐TB) for the majority of patients. Given its long terminal half‐life and ... |
PMC11410029 | core_pubmed_pmc | Preclinical Development of SHR-1819, a Potent Humanized IL-4Rα Antibody for Treating Type 2 Inflammatory Diseases | Preclinical Development of SHR-1819, a Potent Humanized IL-4Rα Antibody for Treating Type 2 Inflammatory Diseases Abstract Abstract Background Interleukin (IL)-4 and IL-13 are critical pathogenic factors for type 2 inflammation-related allergic diseases, sharing the mutual receptor subunit IL-4Rα. However, it was ineff... |
PMC6506861 | core_pubmed_pmc | Toxicity and pharmacokinetic profile of SGM-101, a fluorescent anti-CEA chimeric antibody for fluorescence imaging of tumors in patients | Toxicity and pharmacokinetic profile of SGM-101, a fluorescent anti-CEA chimeric antibody for fluorescence imaging of tumors in patients Abstract Highlights • Fluorescence guided surgery represents a considerable advance for oncology surgeons. • SGM-101 is an innovative antibody-dye conjugate targeting carcinoembryonic... |
PMC5351412 | core_pubmed_pmc | Mathematical modeling of the effects of CK2.3 on mineralization in osteoporotic bone | Mathematical modeling of the effects of CK2.3 on mineralization in osteoporotic bone Abstract Osteoporosis is caused by decreased bone mineral density (BMD) and new treatments for this disease are desperately needed. Bone morphogenetic protein 2 (BMP2) is crucial for bone formation. The mimetic peptide CK2.3 acts downs... |
PMC3221841 | core_pubmed_pmc | Population Pharmacokinetics of Telapristone (CDB-4124) and its Active Monodemethylated Metabolite CDB-4453, with a Mixture Model for Total Clearance | Population Pharmacokinetics of Telapristone (CDB-4124) and its Active Monodemethylated Metabolite CDB-4453, with a Mixture Model for Total Clearance Abstract Abstract Telapristone is a selective progesterone antagonist that is being developed for the long-term treatment of symptoms associated with endometriosis and ute... |
PMC7284824 | core_pubmed_pmc | Curcumin, Curcumin Nanoparticles and Curcumin Nanospheres: A Review on Their Pharmacodynamics Based on Monogastric Farm Animal, Poultry and Fish Nutrition | Curcumin, Curcumin Nanoparticles and Curcumin Nanospheres: A Review on Their Pharmacodynamics Based on Monogastric Farm Animal, Poultry and Fish Nutrition Abstract Abstract Nanotechnology is an emerging field of science that is widely used in medical sciences. However, it has limited uses in monogastric farm animal as ... |
PMC12946586 | core_pubmed_pmc | Single‐Dose Pharmacokinetic Assessment of TNX‐102 SL (Cyclobenzaprine HCl Sublingual Tablets): Results From Randomized, Open‐Label Studies in Healthy Volunteers | Single‐Dose Pharmacokinetic Assessment of TNX‐102 SL (Cyclobenzaprine HCl Sublingual Tablets): Results From Randomized, Open‐Label Studies in Healthy Volunteers Abstract Abstract Daily oral cyclobenzaprine hydrochloride (HCl) has provided transient benefits in fibromyalgia, a chronic pain condition. To improve this eff... |
PMC4949396 | core_pubmed_pmc | The effects of apremilast on the QTc interval in healthy male volunteers: a formal, thorough QT study | The effects of apremilast on the QTc interval in healthy male volunteers: a formal, thorough QT study Abstract Objective: This study was conducted to evaluate the effect of apremilast and its major metabolites on the placebo-corrected change-from-baseline QTc interval of an electrocardiogram (ECG). Materials and method... |
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