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PMC11615510 | core_pubmed_pmc | Population pharmacokinetic analysis identifies an absorption process model for mycophenolic acid in patients with renal transplant | Population pharmacokinetic analysis identifies an absorption process model for mycophenolic acid in patients with renal transplant Abstract Abstract The pharmacokinetics (PKs) of mycophenolic acid (MPA) exhibit considerable complexity and large variability. We developed a population pharmacokinetic (popPK) model to pre... |
PMC11331591 | core_pubmed_pmc | Commentary: Pharmacokinetic Theory Must Consider Published Experimental Data | Commentary: Pharmacokinetic Theory Must Consider Published Experimental Data Abstract Recently, we have proposed simple methodology to derive clearance and rate constant equations, independent of differential equations, based on Kirchhoff’s Laws, a common methodology from physics used to describe rate-defining processe... |
PMC8628618 | core_pubmed_pmc | The influence of storage time on ponazuril concentrations in feline plasma | The influence of storage time on ponazuril concentrations in feline plasma Abstract Background The pharmacokinetics of ponazuril have been determined in several species; however, there is very little information on the stability of the drug after storage for long periods of time. This study was undertaken to determine ... |
PMC9180621 | core_pubmed_pmc | Preparation of Novel Pyrazolo[4,3- e ]tetrazolo[1,5- b ][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies | Preparation of Novel Pyrazolo[4,3- e ]tetrazolo[1,5- b ][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies Abstract Abstract Pyrazolo[4,3- e ]tetrazolo[1,5- b ]triazine sulfonamides constitute a novel class of heterocyclic compounds with broad biological activity, including antican... |
PMC3651343 | core_pubmed_pmc | Clinical trial simulation to evaluate power to compare the antiviral effectiveness of two hepatitis C protease inhibitors using nonlinear mixed effect models: a viral kinetic approach | Clinical trial simulation to evaluate power to compare the antiviral effectiveness of two hepatitis C protease inhibitors using nonlinear mixed effect models: a viral kinetic approach Abstract Background Models of hepatitis C virus (HCV) kinetics are increasingly used to estimate and to compare in vivo drug’s antiviral... |
PMC11878006 | core_pubmed_pmc | Targeted delivery of antitubercular drugs using glucan lipid particles | Targeted delivery of antitubercular drugs using glucan lipid particles Abstract ABSTRACT Simpler, safer, and faster chemotherapeutic regimens for tuberculosis and other respiratory mycobacterial infections are an urgent need. Many current therapies suffer from suboptimal drug exposure and dose-limiting systemic adverse... |
PMC7700423 | core_pubmed_pmc | Differential Effects of 1α,25-Dihydroxyvitamin D 3 on the Expressions and Functions of Hepatic CYP and UGT Enzymes and Its Pharmacokinetic Consequences In Vivo | Differential Effects of 1α,25-Dihydroxyvitamin D 3 on the Expressions and Functions of Hepatic CYP and UGT Enzymes and Its Pharmacokinetic Consequences In Vivo Abstract The compound 1α,25-Dihydroxyvitamin D 3 (1,25(OH) 2 D 3 ) is the active form of vitamin D 3 and a representative ligand of the vitamin D receptor (VDR)... |
PMC9303933 | core_pubmed_pmc | Dosing Regimen Prediction and Confirmation With Rivaroxaban for Thromboprophylaxis in Children After the Fontan Procedure: Insights From the Phase III UNIVERSE Study | Dosing Regimen Prediction and Confirmation With Rivaroxaban for Thromboprophylaxis in Children After the Fontan Procedure: Insights From the Phase III UNIVERSE Study Abstract Abstract Thrombosis remains an important complication for children with single‐ventricle physiology following the Fontan procedure, and effective... |
PMC12588642 | core_pubmed_pmc | Therapeutic Drug Monitoring of Oral Targeted Anticancer Drugs: Achievements, Experiences, Challenges, and the Path Forward | Therapeutic Drug Monitoring of Oral Targeted Anticancer Drugs: Achievements, Experiences, Challenges, and the Path Forward Abstract Abstract Background: The introduction of oral targeted anticancer drugs has revolutionized anticancer treatments. Exposure to these drugs is often affected by individual, disease, or drug ... |
PMC6044034 | core_pubmed_pmc | Pharmacokinetics of lotilaner following a single oral or intravenous administration in cats | Pharmacokinetics of lotilaner following a single oral or intravenous administration in cats Abstract Background Credelio TM (lotilaner) is an oral ectoparasiticide from the isoxazoline class developed for the treatment of flea and tick infestations in cats. It is formulated as a pure S -enantiomer in flavoured chewable... |
PMC11023818 | core_pubmed_pmc | Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice | Pharmacokinetic Effects of Different Models of Nonalcoholic Fatty Liver Disease in Transgenic Humanized OATP1B Mice Abstract Abstract Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 (collectively, OATP1B) transporters encoded by the solute carrier organic anion transporter ( SLCO) genes mediate uptake of ... |
PMC7558941 | core_pubmed_pmc | Impact of Sampling Period on Population Pharmacokinetic Analysis of Antibiotics: Why do You Take Blood Samples Following the Fourth Dose? | Impact of Sampling Period on Population Pharmacokinetic Analysis of Antibiotics: Why do You Take Blood Samples Following the Fourth Dose? Abstract Abstract To date, many population pharmacokinetic models of antibiotics have been developed using blood sampling data after the fourth or fifth dose, which represents steady... |
PMC4302127 | core_pubmed_pmc | The combined effects of extracorporeal membrane oxygenation and renal replacement therapy on meropenem pharmacokinetics: a matched cohort study | The combined effects of extracorporeal membrane oxygenation and renal replacement therapy on meropenem pharmacokinetics: a matched cohort study Abstract Introduction The scope of extracorporeal membrane oxygenation (ECMO) is expanding; however, optimal drug prescription during ECMO remains a developing science. Current... |
PMC4310268 | core_pubmed_pmc | Absence of a significant pharmacokinetic interaction between atorvastatin and fenofibrate: a randomized, crossover, study of a fixed-dose formulation in healthy Mexican subjects | Absence of a significant pharmacokinetic interaction between atorvastatin and fenofibrate: a randomized, crossover, study of a fixed-dose formulation in healthy Mexican subjects Abstract Several clinical trials have substantiated the efficacy of the co-administration of statins like atorvastatin (ATO) and fibrates. Wit... |
PMC10058280 | core_pubmed_pmc | In Vitro Hepatic Models to Assess Herb–Drug Interactions: Approaches and Challenges | In Vitro Hepatic Models to Assess Herb–Drug Interactions: Approaches and Challenges Abstract Abstract A newfound appreciation for the benefits of herbal treatments has emerged in recent decades. However, herbal medication production still needs to establish standardized protocols that adhere to strict guidelines for qu... |
PMC6503535 | core_pubmed_pmc | Use of PBPK Modeling To Evaluate the Performance of Dissolv It , a Biorelevant Dissolution Assay for Orally Inhaled Drug Products | Use of PBPK Modeling To Evaluate the Performance of Dissolv It , a Biorelevant Dissolution Assay for Orally Inhaled Drug Products Abstract Abstract The dissolution of inhaled drug particles in the lungs is a challenge to model using biorelevant methods in terms of (i) collecting a respirable emitted aerosol fraction an... |
PMC7191301 | core_pubmed_pmc | Population Pharmacokinetic, Pharmacogenetic, and Pharmacodynamic Analysis of Cyclophosphamide in Ethiopian Breast Cancer Patients | Population Pharmacokinetic, Pharmacogenetic, and Pharmacodynamic Analysis of Cyclophosphamide in Ethiopian Breast Cancer Patients Abstract Cyclophosphamide (CPA) containing chemotherapy regimen is the standard of care for breast cancer treatment in sub-Saharan Africa. Wide inter-individual variations in pharmacokinetic... |
PMC8518152 | core_pubmed_pmc | Ginsenosides emerging as both bifunctional drugs and nanocarriers for enhanced antitumor therapies | Ginsenosides emerging as both bifunctional drugs and nanocarriers for enhanced antitumor therapies Abstract Ginsenosides, the main components isolated from Panax ginseng , can play a therapeutic role by inducing tumor cell apoptosis and reducing proliferation, invasion, metastasis; by enhancing immune regulation; and b... |
PMC8621720 | core_pubmed_pmc | Dietary Supplement Use and Interactions with Tamoxifen and Aromatase Inhibitors in Breast Cancer Survivors Enrolled in Lifestyle Interventions | Dietary Supplement Use and Interactions with Tamoxifen and Aromatase Inhibitors in Breast Cancer Survivors Enrolled in Lifestyle Interventions Abstract Abstract The use of dietary supplements is common in the general population and even more prevalent among cancer survivors. The World Cancer Research Fund/American Inst... |
PMC12781431 | core_pubmed_pmc | Development and application of artificial intelligence in traditional Chinese medicine research and development | Development and application of artificial intelligence in traditional Chinese medicine research and development Abstract Background The integration of artificial intelligence (AI) into traditional Chinese medicine (TCM) research and development offers promising solutions to longstanding challenges in the field. These c... |
PMC12872343 | core_pubmed_pmc | Lithium toxicity following a change from semaglutide to tirzepatide for weight loss management | Lithium toxicity following a change from semaglutide to tirzepatide for weight loss management Abstract Introduction Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are increasingly prescribed for weight management. Although generally well-tolerated, these agents may alter the pharmacokinetics of concurrently adm... |
PMC8395520 | core_pubmed_pmc | NMDARs Containing NR2B Subunit Do Not Contribute to the LTP Form of Hippocampal Plasticity: In Vivo Pharmacological Evidence in Rats | NMDARs Containing NR2B Subunit Do Not Contribute to the LTP Form of Hippocampal Plasticity: In Vivo Pharmacological Evidence in Rats Abstract Abstract Synaptic plasticity is the key to synaptic health, and aberrant synaptic plasticity, which in turn impairs the functioning of large-scale brain networks, has been associ... |
PMC12585024 | core_pubmed_pmc | The efficacy and safety of lignocaine-embedded dissolvable microneedle versus EMLA for topical analgesia in adults undergoing venepuncture: A single-centre, parallel-group, double-blind randomised clinical trial protocol in a tertiary care setting | The efficacy and safety of lignocaine-embedded dissolvable microneedle versus EMLA for topical analgesia in adults undergoing venepuncture: A single-centre, parallel-group, double-blind randomised clinical trial protocol in a tertiary care setting Abstract Venepuncture-associated pain is a major source of distress comm... |
PMC11090832 | core_pubmed_pmc | Complexation of histone deacetylase inhibitor belinostat to Cu(II) prevents premature metabolic inactivation in vitro and demonstrates potent anti-cancer activity in vitro and ex vivo in colon cancer | Complexation of histone deacetylase inhibitor belinostat to Cu(II) prevents premature metabolic inactivation in vitro and demonstrates potent anti-cancer activity in vitro and ex vivo in colon cancer Abstract Purpose The histone deacetylase inhibitor (HDACi), belinostat, has had limited therapeutic impact in solid tumo... |
PMC11458339 | core_pubmed_pmc | Advanced clinical symptoms of the antihangover compound HK-GCM-H01 in healthy Koreans | Advanced clinical symptoms of the antihangover compound HK-GCM-H01 in healthy Koreans Abstract Abstract A hangover is a combination of negative mental and physical symptoms, such as headache, diarrhea, and loss of appetite, that occur after alcohol consumption and can vary depending on individual genetic and environmen... |
PMC12749539 | core_pubmed_pmc | High-throughput in vitro screening and in silico analysis for Zika virus inhibitor identification | High-throughput in vitro screening and in silico analysis for Zika virus inhibitor identification Abstract Abstract Zika Virus (ZIKV) is a mosquito-borne virus that can cause serious health problems, including birth defects and neurological complications. Unfortunately, there are no antivirals currently approved for it... |
PMC10497414 | core_pubmed_pmc | Control of acute myeloid leukemia by a trifunctional NKp46-CD16a-NK cell engager targeting CD123 | Control of acute myeloid leukemia by a trifunctional NKp46-CD16a-NK cell engager targeting CD123 Abstract Abstract CD123, the alpha chain of the IL-3 receptor, is an attractive target for acute myeloid leukemia (AML) treatment. However, cytotoxic antibodies or T cell engagers targeting CD123 had insufficient efficacy o... |
PMC10965878 | core_pubmed_pmc | Effect of Renal Impairment on Pharmacokinetics and Safety of Ensitrelvir, a SARS-CoV-2 3CL Protease Inhibitor | Effect of Renal Impairment on Pharmacokinetics and Safety of Ensitrelvir, a SARS-CoV-2 3CL Protease Inhibitor Abstract Abstract Introduction Ensitrelvir, a novel oral inhibitor of 3C-like protease of SARS-CoV-2, shows efficacy and safety in participants with mild to moderate COVID-19. Since urinary recovery of ensitrel... |
PMC8073511 | core_pubmed_pmc | Emerging Approaches in Intravenous Moderate and Deep Sedation | Emerging Approaches in Intravenous Moderate and Deep Sedation Abstract Abstract Successful pharmacological innovations that have made a difference in daily practice are rare in the world of anesthesia and sedation. After many years of research, it seems that we finally have two new drug innovations that are likely to c... |
PMC6660183 | core_pubmed_pmc | Intramuscular administration of hexachloroplatinate reverses cyanide‐induced metabolic derangements and counteracts severe cyanide poisoning | Intramuscular administration of hexachloroplatinate reverses cyanide‐induced metabolic derangements and counteracts severe cyanide poisoning Abstract Abstract Cyanide is a highly toxic industrial chemical that is widely used by manufactures. Smoke inhalation during household fires is the most common source of cyanide p... |
PMC11721854 | core_pubmed_pmc | Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship | Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship Abstract Abstract Acetazolamide (AZM) is a strong pharmacological sulphonamide-type (R-SO 2 -NH 2 , p K a 7.2) inhibitor of the activity of several carbonic anhydrase (CA) isoforms, notably of renal CA II ( K i , ... |
PMC8879872 | core_pubmed_pmc | Model Calibration of Pharmacokinetic-Pharmacodynamic Lung Tumour Dynamics for Anticancer Therapies | Model Calibration of Pharmacokinetic-Pharmacodynamic Lung Tumour Dynamics for Anticancer Therapies Abstract Abstract Individual curves for tumor growth can be expressed as mathematical models. Herein we exploited a pharmacokinetic-pharmacodynamic (PKPD) model to accurately predict the lung growth curves when using data... |
PMC6440464 | core_pubmed_pmc | Pharmacokinetic comparison of quercetin, isoquercitrin, and quercetin-3-O-β-D-glucuronide in rats by HPLC-MS | Pharmacokinetic comparison of quercetin, isoquercitrin, and quercetin-3-O-β-D-glucuronide in rats by HPLC-MS Abstract Background Quercetin (Qr), isoquercitrin (IQ), and quercetin-3-O-β-D-glucuronide (QG) are powerful phytochemicals that have been shown to exhibit disease prevention and health promotion properties. Howe... |
PMC7877846 | core_pubmed_pmc | Characterization of the Relationship of Inotuzumab Ozogamicin Exposure With Efficacy and Safety End Points in Adults With Relapsed or Refractory Acute Lymphoblastic Leukemia | Characterization of the Relationship of Inotuzumab Ozogamicin Exposure With Efficacy and Safety End Points in Adults With Relapsed or Refractory Acute Lymphoblastic Leukemia Abstract Inotuzumab ozogamicin (InO), an anti‐CD22 monoclonal antibody conjugated to calicheamicin, is approved in Europe and the United States fo... |
PMC7515962 | core_pubmed_pmc | Population pharmacokinetic analysis of nanoparticle-bound and free camptothecin after administration of NLG207 in adults with advanced solid tumors | Population pharmacokinetic analysis of nanoparticle-bound and free camptothecin after administration of NLG207 in adults with advanced solid tumors Abstract Abstract Purpose NLG207 (formerly CRLX101) is a nanoparticle–drug conjugate (NDC) of the potent topoisomerase I inhibitor, camptothecin (CPT). The present study so... |
PMC4376184 | core_pubmed_pmc | Single and multiple dose pharmacokinetics and tolerability of HX-1171, a novel antioxidant, in healthy volunteers | Single and multiple dose pharmacokinetics and tolerability of HX-1171, a novel antioxidant, in healthy volunteers Abstract Background HX-1171 (1-O-hexyl-2,3,5-trimethylhydroquinone) is a promising antioxidant with therapeutic potential for hepatic fibrosis. The aim of this study was to investigate the tolerability and ... |
PMC12363466 | core_pubmed_pmc | Emptying the fridge syndrome: a case of nocturnal food craving associated with peak perampanel concentration | Emptying the fridge syndrome: a case of nocturnal food craving associated with peak perampanel concentration Abstract Highlights • Off-label antiseizure drug use is common but lacks full safety or efficacy data. • High-dose perampanel may cause nocturnal compulsive food-seeking behaviour. • Adverse events might go unre... |
PMC3413817 | core_pubmed_pmc | Phase 1b dose-finding study of motesanib with docetaxel or paclitaxel in patients with metastatic breast cancer | Phase 1b dose-finding study of motesanib with docetaxel or paclitaxel in patients with metastatic breast cancer Abstract The purpose of this study was to investigate the safety, tolerability, and pharmacokinetics of motesanib when combined with docetaxel or paclitaxel in patients with metastatic breast cancer. In this ... |
PMC7409018 | core_pubmed_pmc | Genetics and Opioids: Towards More Appropriate Prescription in Cancer Pain | Genetics and Opioids: Towards More Appropriate Prescription in Cancer Pain Abstract Abstract Opioids are extensively used in patients with cancer pain; despite their efficacy, several patients can experience ineffective analgesia and/or side effects. Pharmacogenetics is a new approach to drug prescription based on the ... |
PMC9549471 | core_pubmed_pmc | Understanding the Mechanism of Drug Transfer and Retention of Drug-Coated Balloons | Understanding the Mechanism of Drug Transfer and Retention of Drug-Coated Balloons Abstract Objective: The purpose of this study was to determine the impact of varying inflation parameters on paclitaxel delivery and retention using a commercially available DCB. Background: Drug-coated balloons (DCB) have become the sta... |
PMC4881758 | core_pubmed_pmc | Pharmacokinetics of a Cholesterol-conjugated Aptamer Against the Hepatitis C Virus (HCV) NS5B Protein | Pharmacokinetics of a Cholesterol-conjugated Aptamer Against the Hepatitis C Virus (HCV) NS5B Protein Abstract Hepatitis C virus (HCV) is the major cause of progressive liver disease such as chronic hepatitis, cirrhosis, and hepatocellular carcinoma. Previously, we reported that a 29 nucleotide-long 2'-F pyrimidine mod... |
PMC4454552 | core_pubmed_pmc | Effects of the CYP3A4*1B Genetic Polymorphism on the Pharmacokinetics of Tacrolimus in Adult Renal Transplant Recipients: A Meta-Analysis | Effects of the CYP3A4*1B Genetic Polymorphism on the Pharmacokinetics of Tacrolimus in Adult Renal Transplant Recipients: A Meta-Analysis Abstract Abstract Background and Objective The association between the CYP3A4*1B single nucleotide polymorphism (SNP) and tacrolimus pharmacokinetics in different studies is controve... |
PMC6902860 | core_pubmed_pmc | Pharmacokinetics and Safety of Esketamine in Chinese Patients Undergoing Painless Gastroscopy in Comparison with Ketamine: A Randomized, Open-Label Clinical Study | Pharmacokinetics and Safety of Esketamine in Chinese Patients Undergoing Painless Gastroscopy in Comparison with Ketamine: A Randomized, Open-Label Clinical Study Abstract Abstract Purpose To assess the pharmacokinetics and safety of pure S-ketamine (esketamine) in Chinese patients undergoing painless gastroscopy and e... |
PMC10156125 | core_pubmed_pmc | Effectiveness and Pharmacokinetic Exposures of First-Line Drugs Used to Treat Drug-Susceptible Tuberculosis in Children: A Systematic Review and Meta-Analysis | Effectiveness and Pharmacokinetic Exposures of First-Line Drugs Used to Treat Drug-Susceptible Tuberculosis in Children: A Systematic Review and Meta-Analysis Abstract Abstract Background Optimal doses of first-line drugs for treatment of drug-susceptible tuberculosis in children and young adolescents remain uncertain.... |
PMC8089078 | core_pubmed_pmc | The Pharmacology, Efficacy, and Safety of Rivaroxaban in Obese Patient Populations | The Pharmacology, Efficacy, and Safety of Rivaroxaban in Obese Patient Populations Abstract Abstract Cardiovascular disease (CVD) remains the leading cause of death in the USA. Several risk factors have been identified, and obesity has become one of prominent concern. Excessive weight is considered a risk factor for CV... |
PMC8931498 | core_pubmed_pmc | Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites | Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites Abstract Abstract The psychedelic alkaloid ibogaine is increasingly used as an oral treatment for substance use disorders, despite being unlicensed in m... |
PMC3870082 | core_pubmed_pmc | Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates | Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates Abstract We previously reported the synthesis of three DOX conjugates that represented different targeting vehicles and showed them to have antitumor activity both in vitro and in vivo . However, the relationshi... |
PMC6775958 | core_pubmed_pmc | Jejunal wall delivery of insulin via an ingestible capsule in anesthetized swine—A pharmacokinetic and pharmacodynamic study | Jejunal wall delivery of insulin via an ingestible capsule in anesthetized swine—A pharmacokinetic and pharmacodynamic study Abstract Abstract Biotherapeutic agents must be administered parenterally to obtain therapeutic blood concentrations, lowering patient compliance and complicating care. An oral delivery platform ... |
PMC4956805 | core_pubmed_pmc | Pharmacodynamic correlations using fresh and cryopreserved tissue following use of vaginal rings containing dapivirine and/or maraviroc in a randomized, placebo controlled trial | Pharmacodynamic correlations using fresh and cryopreserved tissue following use of vaginal rings containing dapivirine and/or maraviroc in a randomized, placebo controlled trial Abstract Abstract Background: The ex vivo challenge assay is a bio-indicator of drug efficacy and was utilized in this randomized, placebo con... |
PMC12258238 | core_pubmed_pmc | From Nature to Nanotechnology: The Bioactivities of Mangiferin Explored | From Nature to Nanotechnology: The Bioactivities of Mangiferin Explored Abstract Abstract Mangiferin, a naturally occurring C-glucosylxanthone derived from various parts of the mango tree ( Mangifera indica ), has gained significant attention for its diverse pharmacological properties, including antioxidant, anti-infla... |
PMC8453901 | core_pubmed_pmc | GLPG1205, a GPR84 Modulator: Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Subjects | GLPG1205, a GPR84 Modulator: Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Subjects Abstract Abstract GLPG1205 is a modulator of GPR84, a G‐protein–coupled receptor reported to be associated with several diseases. Safety, tolerability, pharmacokinetics, and pharmacodynamics of GLPG1205 in healthy subjects w... |
PMC12472963 | core_pubmed_pmc | Liposomal Encapsulation of Tartar Emetic Improves Pharmacokinetic Profile and Mitigates Cardiotoxicity in Murine Experimental Model | Liposomal Encapsulation of Tartar Emetic Improves Pharmacokinetic Profile and Mitigates Cardiotoxicity in Murine Experimental Model Abstract Abstract Background/Objectives: Visceral leishmaniasis remains a serious public health issue, with current antimonial therapies limited by systemic toxicity. Liposomal drug delive... |
PMC9647081 | core_pubmed_pmc | Anakinra Pilot – a clinical trial to demonstrate safety, feasibility and pharmacokinetics of interleukin 1 receptor antagonist in preterm infants | Anakinra Pilot – a clinical trial to demonstrate safety, feasibility and pharmacokinetics of interleukin 1 receptor antagonist in preterm infants Abstract Abstract Background Bronchopulmonary dysplasia (BPD), its complication pulmonary hypertension (BPD-PH) and preterm brain and gut injury lead to significant morbidity... |
PMC6325982 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Once-Weekly Somapacitan in Children and Adults: Supporting Dosing Rationales with a Model-Based Analysis of Three Phase I Trials | Pharmacokinetics and Pharmacodynamics of Once-Weekly Somapacitan in Children and Adults: Supporting Dosing Rationales with a Model-Based Analysis of Three Phase I Trials Abstract Background Somapacitan, a long-acting growth hormone (GH) derivative, has been well-tolerated in children with GH deficiency (GHD) and adults... |
PMC12485016 | core_pubmed_pmc | Computational identification and evaluation of novel PD-L1 inhibitors for cancer immunotherapy | Computational identification and evaluation of novel PD-L1 inhibitors for cancer immunotherapy Abstract Abstract Antibody-based therapies targeting the PD-1/PD-L1 pathway have shown promise in anticancer immunotherapy; however, challenges such as high cost, immunogenicity, and limited penetration highlight the need for... |
PMC12214960 | core_pubmed_pmc | Bioequivalence study of two formulations of lurasidone film coated tablets in healthy subjects under fed conditions | Bioequivalence study of two formulations of lurasidone film coated tablets in healthy subjects under fed conditions Abstract Abstract To define the bioequivalence (BE) of two orally administered film coated tablets containing 40 mg lurasidone hydrochloride. A single-dose, open-label, randomized two-way crossover trial ... |
PMC10676332 | core_pubmed_pmc | Effect of High-Fat Food on the Pharmacokinetic Profile and Safety of SAF-189s, an ALK/ROS1 Inhibitor, in Healthy Chinese Adults | Effect of High-Fat Food on the Pharmacokinetic Profile and Safety of SAF-189s, an ALK/ROS1 Inhibitor, in Healthy Chinese Adults Abstract Abstract Background and Objectives This study was conducted to investigate the effect of high-fat meals on the pharmacokinetics (PK) and safety profile of SAF-189s, a novel ALK/ROS1 i... |
PMC8464955 | core_pubmed_pmc | Prediction of Drug–Drug Interaction Potential of Tegoprazan Using Physiologically Based Pharmacokinetic Modeling and Simulation | Prediction of Drug–Drug Interaction Potential of Tegoprazan Using Physiologically Based Pharmacokinetic Modeling and Simulation Abstract Abstract This study aimed to develop a physiologically based pharmacokinetic (PBPK) model of tegoprazan and to predict the drug–drug interaction (DDI) potential between tegoprazan and... |
PMC9468568 | core_pubmed_pmc | Rituximab pediatric drug development: Pharmacokinetic and pharmacodynamic modeling to inform regulatory approval for rituximab treatment in patients with granulomatosis with polyangiitis or microscopic polyangiitis | Rituximab pediatric drug development: Pharmacokinetic and pharmacodynamic modeling to inform regulatory approval for rituximab treatment in patients with granulomatosis with polyangiitis or microscopic polyangiitis Abstract Abstract Anti‐neutrophil cytoplasmic antibody‐associated vasculitides granulomatosis with polyan... |
PMC5927357 | core_pubmed_pmc | Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics | Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics Abstract Abstract Background and aim Drugs that are effective against diseases in the central nervous system and reach the brain via blood must pass through the blood–brain barrier (BBB), ... |
PMC12576106 | core_pubmed_pmc | Pharmacokinetic variability of vancomycin in patients undergoing hematopoietic stem cell transplantation: a retrospective cohort study in Peru | Pharmacokinetic variability of vancomycin in patients undergoing hematopoietic stem cell transplantation: a retrospective cohort study in Peru Abstract Background: Vancomycin exhibits high pharmacokinetic variability, particularly in hematopoietic stem cell transplantation (HSCT) patients, where augmented renal clearan... |
PMC12909856 | core_pubmed_pmc | Different metabolic pathways associated with total cortisol exposure and the cortisol time profile: a randomized crossover trial | Different metabolic pathways associated with total cortisol exposure and the cortisol time profile: a randomized crossover trial Abstract Excess cortisol exposure and disruption of its circadian pattern have both been linked to adverse health outcomes; however, whether distinct metabolic signatures differentiate total ... |
PMC8753592 | core_pubmed_pmc | Long-acting capsid inhibitor protects macaques from repeat SHIV challenges | Long-acting capsid inhibitor protects macaques from repeat SHIV challenges Abstract Because no currently available vaccine can prevent HIV infection, pre-exposure prophylaxis (PrEP) with antiretrovirals (ARVs) is an important tool for combating the HIV pandemic 1 , 2 . Long-acting ARVs promise to build on the success o... |
PMC11739743 | core_pubmed_pmc | Building Confidence in Physiologically Based Pharmacokinetic Modeling of CYP3A Induction Mediated by Rifampin: An Industry Perspective | Building Confidence in Physiologically Based Pharmacokinetic Modeling of CYP3A Induction Mediated by Rifampin: An Industry Perspective Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) modeling offers a viable approach to predict induction drug–drug interactions (DDIs) with the potential to streamline or r... |
PMC12397716 | core_pubmed_pmc | A Retrospective Analysis of PK and Response of Oral Ibuprofen in the Treatment of a Patent Ductus Arteriosus in Extremely Low Gestational Age Neonates | A Retrospective Analysis of PK and Response of Oral Ibuprofen in the Treatment of a Patent Ductus Arteriosus in Extremely Low Gestational Age Neonates Abstract Abstract Oral ibuprofen is the preferred pharmacotherapeutic option for treatment of a persistent patent ductus arteriosus (PDA), but evidence for its optimal u... |
PMC4888295 | core_pubmed_pmc | ABC transporters P-gp and Bcrp do not limit the brain uptake of the novel antipsychotic and anticonvulsant drug cannabidiol in mice | ABC transporters P-gp and Bcrp do not limit the brain uptake of the novel antipsychotic and anticonvulsant drug cannabidiol in mice Abstract Cannabidiol (CBD) is currently being investigated as a novel therapeutic for the treatment of CNS disorders like schizophrenia and epilepsy. ABC transporters such as P-glycoprotei... |
PMC11809910 | core_pubmed_pmc | Differences in sensory nerve block between levobupivacaine and bupivacaine at low concentrations in humans and animals | Differences in sensory nerve block between levobupivacaine and bupivacaine at low concentrations in humans and animals Abstract Physiochemical properties of levobupivacaine and bupivacaine are identical, but pharmacokinetic and pharmacodynamics properties differ due to stereoselective interactions at the molecular site... |
PMC4412827 | core_pubmed_pmc | Comparability of Biosimilar Filgrastim with Originator Filgrastim: Protein Characterization, Pharmacodynamics, and Pharmacokinetics | Comparability of Biosimilar Filgrastim with Originator Filgrastim: Protein Characterization, Pharmacodynamics, and Pharmacokinetics Abstract Abstract Background Biosimilars provide safety, purity, and potency similar to those of a reference biologic product. Methods An array of protein analytical techniques was used to... |
PMC7552959 | core_pubmed_pmc | Population pharmacokinetics of lopinavir/ritonavir in Covid-19 patients | Population pharmacokinetics of lopinavir/ritonavir in Covid-19 patients Abstract Objective To develop a population pharmacokinetic model for lopinavir boosted by ritonavir in coronavirus disease 2019 (Covid-19) patients. Methods Concentrations of lopinavir/ritonavir were assayed by an accredited LC-MS/MS method. The po... |
PMC7555902 | core_pubmed_pmc | Infliximab concentrations in two non-switching cohorts of patients with inflammatory bowel disease: originator vs. biosimilar | Infliximab concentrations in two non-switching cohorts of patients with inflammatory bowel disease: originator vs. biosimilar Abstract Biosimilars are replacing originator compounds due to their similar effectiveness, safety and pharmacokinetics. Our objective was to compare the differences in pharmacokinetics and clin... |
PMC10890738 | core_pubmed_pmc | Comprehensive characterization of the effect of mineralocorticoid receptor antagonism with spironolactone on the renin-angiotensin-aldosterone system in healthy dogs | Comprehensive characterization of the effect of mineralocorticoid receptor antagonism with spironolactone on the renin-angiotensin-aldosterone system in healthy dogs Abstract Objective To characterize the dose-exposure-response effect of spironolactone on biomarkers of the classical and alternative arms of the renin-an... |
PMC3665573 | core_pubmed_pmc | Expansion of guidance for the day 8 initiation dose of paliperidone palmitate to avoid a missed dose | Expansion of guidance for the day 8 initiation dose of paliperidone palmitate to avoid a missed dose Abstract Background Paliperidone palmitate (PP) is a long-acting injectable formulation of an atypical antipsychotic, paliperidone. Its dose can be expressed in milligram or milligram equivalents (mg eq) of active palip... |
PMC3621790 | core_pubmed_pmc | Metabolism and Pharmacokinetics of the Anti-Tuberculosis Drug Ethionamide in a Flavin-Containing Monooxygenase Null Mouse | Metabolism and Pharmacokinetics of the Anti-Tuberculosis Drug Ethionamide in a Flavin-Containing Monooxygenase Null Mouse Abstract Multiple drug resistance (MDR) in Mycobacterium tuberculosis (mTB), the causative agent for tuberculosis (TB), has led to increased use of second-line drugs, including ethionamide (ETA). ET... |
PMC6709422 | core_pubmed_pmc | NONMEM Tutorial Part II: Estimation Methods and Advanced Examples | NONMEM Tutorial Part II: Estimation Methods and Advanced Examples Abstract In this second tutorial on NONMEM, the examples of typical pharmacokinetic/pharmacodynamic modeling problems that occur in the pharmaceutical field will be presented, which the reader can use as a template for his or her own modeling endeavors. ... |
PMC10042906 | core_pubmed_pmc | Determination of the Optimal Single Dose Treatment for Acoziborole, a Novel Drug for the Treatment of Human African Trypanosomiasis: First-in-Human Study | Determination of the Optimal Single Dose Treatment for Acoziborole, a Novel Drug for the Treatment of Human African Trypanosomiasis: First-in-Human Study Abstract Abstract Background and Objectives Acoziborole is a novel boron-containing candidate developed as an oral drug for the treatment of human African trypanosomi... |
PMC12385104 | core_pubmed_pmc | Reconstructing the Antibiotic Pipeline: Natural Alternatives to Antibacterial Agents | Reconstructing the Antibiotic Pipeline: Natural Alternatives to Antibacterial Agents Abstract The discovery of penicillin led to remarkable progress in the treatment of diseases and far-reaching advancements in novel antibiotics’ development and use. However, the uncontrolled use and abuse of antibiotics in subsequent ... |
PMC12030040 | core_pubmed_pmc | Matrix Approach Assessment of Cabotegravir Drug–Drug Interactions with OAT1/OAT3 Substrates and UGT1A1/UGT1A9 Inhibitors Using Physiologically-Based Pharmacokinetic Modeling | Matrix Approach Assessment of Cabotegravir Drug–Drug Interactions with OAT1/OAT3 Substrates and UGT1A1/UGT1A9 Inhibitors Using Physiologically-Based Pharmacokinetic Modeling Abstract Background/Objective: Cabotegravir (CAB), available as an oral tablet and as a long-acting (LA) nanosuspension for intramuscular injectio... |
PMC12486803 | core_pubmed_pmc | Phase 1, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study of the safety, tolerability, and pharmacokinetics of intravenous xeruborbactam (QPX7728) in healthy adult subjects | Phase 1, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study of the safety, tolerability, and pharmacokinetics of intravenous xeruborbactam (QPX7728) in healthy adult subjects Abstract ABSTRACT The objective of this First-in-Human Phase 1, double-blind, randomized, placebo-controlled... |
PMC6510372 | core_pubmed_pmc | Pharmacokinetic and Drug–Drug Interaction Profiles of the Combination of Tezacaftor/Ivacaftor | Pharmacokinetic and Drug–Drug Interaction Profiles of the Combination of Tezacaftor/Ivacaftor Abstract Drug–drug interaction ( DDI ) studies are described for tezacaftor/ivacaftor, a new cystic fibrosis transmembrane conductance regulator modulator therapy for the treatment of cystic fibrosis. Three phase I DDI studies... |
PMC11610950 | core_pubmed_pmc | Genome-scale metabolic modeling in antimicrobial pharmacology ☆ | Genome-scale metabolic modeling in antimicrobial pharmacology ☆ Abstract Abstract The increasing antimicrobial resistance has seriously threatened human health worldwide over the last three decades. This severe medical crisis and the dwindling antibiotic discovery pipeline require the development of novel antimicrobial... |
PMC4405819 | core_pubmed_pmc | C YP2B6*6, CYP2B6*18 , Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe | C YP2B6*6, CYP2B6*18 , Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe Abstract Abstract Background Efavirenz (EFV) therapeutic response and toxicity are associated with high inter-individual variabilit... |
PMC7041308 | core_pubmed_pmc | Bioequivalence of two tacrolimus 1-mg formulations under fasting conditions in healthy subjects: A randomized, two-period crossover trial | Bioequivalence of two tacrolimus 1-mg formulations under fasting conditions in healthy subjects: A randomized, two-period crossover trial Abstract Abstract Objective: The present study compared the pharmacokinetics of two (1 mg) tacrolimus formulations (test (generic from Panacea) and reference (innovator from Astellas... |
PMC7819331 | core_pubmed_pmc | Smokeless consumption of medical cannabis pharmacokinetics, safety and feasibility of the CannaHALER© a phase 1a study | Smokeless consumption of medical cannabis pharmacokinetics, safety and feasibility of the CannaHALER© a phase 1a study Abstract Abstract Background Substantial advancements were achieved in the management of postoperative pain, however the need for further improvement remains. This study explores the pharmacokinetics a... |
PMC9415858 | core_pubmed_pmc | Structural and Functional Analysis of CEX Fractions Collected from a Novel Avastin ® Biosimilar Candidate and Its Innovator: A Comparative Study | Structural and Functional Analysis of CEX Fractions Collected from a Novel Avastin ® Biosimilar Candidate and Its Innovator: A Comparative Study Abstract Avastin ® is a humanized recombinant monoclonal antibody used to treat cancer by targeting VEGF-A to inhibit angiogenesis. SIMAB054, an Avastin ® biosimilar candidate... |
PMC11782309 | core_pubmed_pmc | A Phase 1 Randomized, Placebo-Controlled Study Evaluating the Safety, Tolerability, and Pharmacokinetics of Enteric-Coated Stabilized Sulforaphane (SFX-01) in Male Participants | A Phase 1 Randomized, Placebo-Controlled Study Evaluating the Safety, Tolerability, and Pharmacokinetics of Enteric-Coated Stabilized Sulforaphane (SFX-01) in Male Participants Abstract Abstract Introduction Sulforaphane (SFN) is a naturally occurring isothiocyanate associated with various health benefits, including re... |
PMC3269340 | core_pubmed_pmc | Pharmacokinetics of memantine in rats and mice | Pharmacokinetics of memantine in rats and mice Abstract Abstract To evaluate the potential of memantine as a therapeutic agent for Huntington’s disease (HD) we have undertaken a series of in vitro, ex vivo and whole animal studies to characterize its pharmacokinetics (PK) and pharmacodynamics (PD) in rats and mice. Res... |
PMC3735276 | core_pubmed_pmc | Antitumor activity of docetaxel-loaded polymeric nanoparticles fabricated by Shirasu porous glass membrane-emulsification technique | Antitumor activity of docetaxel-loaded polymeric nanoparticles fabricated by Shirasu porous glass membrane-emulsification technique Abstract Abstract Docetaxel (DTX) has excellent efficiency against a wide spectrum of cancers. However, the current clinical formulation has limited its usage, as it causes some severe sid... |
PMC3929889 | core_pubmed_pmc | Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro – in vivo correlations | Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro – in vivo correlations Abstract Abstract Background: Several tyrosine kinase inhibitors (TKIs) can decrease docetaxel clearance in patients by an unknown mechanism. We hypothesised that these interactions are mediated by the hepatic uptake transporter OATP1B... |
PMC11493964 | core_pubmed_pmc | Model-based meta-analysis of HbA1c reduction across SGLT2 inhibitors using dose adjusted by urinary glucose excretion | Model-based meta-analysis of HbA1c reduction across SGLT2 inhibitors using dose adjusted by urinary glucose excretion Abstract This study was aimed to evaluate whether the dose–response relationship of the sodium glucose co-transporter-2 inhibitors (SGLT2is) in patients with type 2 diabetes mellitus (T2DM)—canagliflozi... |
PMC6702134 | core_pubmed_pmc | Eugenia jambolana extract reduces the systemic exposure of Sitagliptin and improves conditions associated with diabetes: A pharmacokinetic and a pharmacodynamic herb-drug interaction study | Eugenia jambolana extract reduces the systemic exposure of Sitagliptin and improves conditions associated with diabetes: A pharmacokinetic and a pharmacodynamic herb-drug interaction study Abstract Abstract Eugenia jambolana (EJ) is an Indian traditional herb widely used for the treatment of diabetes mellitus. This her... |
PMC11579087 | core_pubmed_pmc | Mixed effect estimation in deep compartment models: Variational methods outperform first-order approximations | Mixed effect estimation in deep compartment models: Variational methods outperform first-order approximations Abstract This work focusses on extending the deep compartment model (DCM) framework to the estimation of mixed-effects. By introducing random effects, model predictions can be personalized based on drug measure... |
PMC8917970 | core_pubmed_pmc | Clonidine for sedation in infants during therapeutic hypothermia with neonatal encephalopathy: pilot study | Clonidine for sedation in infants during therapeutic hypothermia with neonatal encephalopathy: pilot study Abstract Objective: To determine a safe dose of clonidine (CLON) to be used in infants with hypoxic ischemic encephalopathy (HIE) undergoing therapeutic hypothermia (TH). Study Design: A pilot prospective study wa... |
PMC7898055 | core_pubmed_pmc | In vivo Pharmacokinetics and in vitro Release of Imatinib Mesylate-Loaded Liposomes for Pulmonary Delivery | In vivo Pharmacokinetics and in vitro Release of Imatinib Mesylate-Loaded Liposomes for Pulmonary Delivery Abstract Abstract Background Pulmonary arterial hypertension (PAH) is characterized by abnormal proliferation of vascular endothelial and smooth muscle cells and causes occlusion of pulmonary arterioles that event... |
PMC7087413 | core_pubmed_pmc | Safety and pharmacokinetics of the orally available antiprionic compound PRI‐002: A single and multiple ascending dose phase I study | Safety and pharmacokinetics of the orally available antiprionic compound PRI‐002: A single and multiple ascending dose phase I study Abstract Abstract Introduction PRI‐002 is an orally available anti–amyloid beta (Aβ) prionic compound developed for direct disassembly of toxic Aβ oligomers relevant to Alzheimer's diseas... |
PMC4036747 | core_pubmed_pmc | Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling | Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling Abstract Background Successful programmatic use of anti-malarials faces challenges that are not covered by standard drug development processes. The development of appro... |
PMC10877170 | core_pubmed_pmc | Anti-miRNA103/107 encapsulated in transferrin-conjugated lipid nanoparticles crosses blood-brain barrier and reduces brain ischemic damage | Anti-miRNA103/107 encapsulated in transferrin-conjugated lipid nanoparticles crosses blood-brain barrier and reduces brain ischemic damage Abstract MicroRNA (miRNA), by post-transcriptionally regulating the expression of genes involved in stroke response, represents important effectors in stroke pathophysiology. Recent... |
PMC2883699 | core_pubmed_pmc | Decreased exposure to sunitinib due to concomitant administration of ifosfamide: results of a phase I and pharmacokinetic study on the combination of sunitinib and ifosfamide in patients with advanced solid malignancies | Decreased exposure to sunitinib due to concomitant administration of ifosfamide: results of a phase I and pharmacokinetic study on the combination of sunitinib and ifosfamide in patients with advanced solid malignancies Abstract Abstract Background: This study aimed to define the maximally tolerated dose (MTD) of sunit... |
PMC11527646 | core_pubmed_pmc | Pharmacological blockade of the mast cell MRGPRX2 receptor supports investigation of its relevance in skin disorders | Pharmacological blockade of the mast cell MRGPRX2 receptor supports investigation of its relevance in skin disorders Abstract Abstract Introduction Because MRGPRX2 is now recognized as the mast cell receptor for basic secretagogues, there is currently a tremendous interest in whether MRGRPX2 could play an important rol... |
PMC8415502 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of a Novel Virulent Klebsiella Phage Kp_Pokalde_002 in a Mouse Model | Pharmacokinetics and Pharmacodynamics of a Novel Virulent Klebsiella Phage Kp_Pokalde_002 in a Mouse Model Abstract Abstract Phage therapy is one of the most promising alternatives to antibiotics as we face global antibiotic resistance crisis. However, the pharmacokinetics (PK) and pharmacodynamics (PD) of phage therap... |
PMC10480258 | core_pubmed_pmc | Dried Blood Spots—A Platform for Therapeutic Drug Monitoring (TDM) and Drug/Disease Response Monitoring (DRM) | Dried Blood Spots—A Platform for Therapeutic Drug Monitoring (TDM) and Drug/Disease Response Monitoring (DRM) Abstract Abstract This review provides an overview on the current applications of dried blood spots (DBS) as matrices for therapeutic drug (TDM) and drug or disease response monitoring (DRM). Compared with conv... |
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