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PMC7352201 | core_pubmed_pmc | Pharmacokinetics of Oral Cholecalciferol in Healthy Subjects with Vitamin D Deficiency: A Randomized Open-Label Study | Pharmacokinetics of Oral Cholecalciferol in Healthy Subjects with Vitamin D Deficiency: A Randomized Open-Label Study Abstract Background: The aim of this study was to investigate the pharmacokinetic (PK) and safety profile of high-dose vitamin D supplementation, comparing different schedules (daily, weekly, or bi-week... |
PMC12057351 | core_pubmed_pmc | PKPD modeling of the inoculum effect of combined ceftazidime/avibactam and colistin against KPC-3 Klebsiella pneumoniae isolate | PKPD modeling of the inoculum effect of combined ceftazidime/avibactam and colistin against KPC-3 Klebsiella pneumoniae isolate Abstract ABSTRACT The inoculum effect (IE) characterizes a decrease in the antimicrobial effect of antibiotics with increasing inoculum. To face antimicrobial resistance, antibiotic combinatio... |
PMC7053556 | core_pubmed_pmc | Complex formation of anti‐VEGF‐C with VEGF‐C released during blood coagulation resulted in an artifact in its serum pharmacokinetics | Complex formation of anti‐VEGF‐C with VEGF‐C released during blood coagulation resulted in an artifact in its serum pharmacokinetics Abstract Abstract A phage‐derived human monoclonal antibody against VEGF‐C was developed as a potential anti‐tumor therapeutic and exhibited fast clearance in preclinical species, with no... |
PMC9046096 | core_pubmed_pmc | Dolutegravir dosing for children with HIV weighing less than 20 kg: pharmacokinetic and safety substudies nested in the open-label, multicentre, randomised, non-inferiority ODYSSEY trial | Dolutegravir dosing for children with HIV weighing less than 20 kg: pharmacokinetic and safety substudies nested in the open-label, multicentre, randomised, non-inferiority ODYSSEY trial Abstract Summary Background Dolutegravir-based antiretroviral therapy is a preferred first-line treatment for adults and children liv... |
PMC11332424 | core_pubmed_pmc | Chitosan Nanoparticles for Targeted Cancer Therapy: A Review of Stimuli-Responsive, Passive, and Active Targeting Strategies | Chitosan Nanoparticles for Targeted Cancer Therapy: A Review of Stimuli-Responsive, Passive, and Active Targeting Strategies Abstract Abstract Despite all major advancements in drug discovery and development in the pharmaceutical industry, cancer is still one of the most arduous challenges for the scientific community.... |
PMC11047177 | core_pubmed_pmc | A phase I study to evaluate the safety, pharmacokinetics, and pharmacodynamics of PF-06939999 (PRMT5 inhibitor) in patients with selected advanced or metastatic tumors with high incidence of splicing factor gene mutations ☆ | A phase I study to evaluate the safety, pharmacokinetics, and pharmacodynamics of PF-06939999 (PRMT5 inhibitor) in patients with selected advanced or metastatic tumors with high incidence of splicing factor gene mutations ☆ Abstract Abstract Background Protein arginine methyltransferase 5 (PRMT5) methylates multiple su... |
PMC10094389 | core_pubmed_pmc | Iron Acquisition and Metabolism as a Promising Target for Antimicrobials (Bottlenecks and Opportunities): Where Do We Stand? | Iron Acquisition and Metabolism as a Promising Target for Antimicrobials (Bottlenecks and Opportunities): Where Do We Stand? Abstract Abstract The emergence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) infections is one of the most crucial challenges currently faced by the scientific community. Dev... |
PMC8685314 | core_pubmed_pmc | Assessment of Knowledge, Attitudes, and Factors Influencing the Selection Student of Generic Medicine | Assessment of Knowledge, Attitudes, and Factors Influencing the Selection Student of Generic Medicine Abstract Background: Generic replacements for branded medicines have become a typical practice among registered pharmacists all over the world. Therefore, this study was aimed to determine the influence of the knowledg... |
PMC10719464 | core_pubmed_pmc | Ethnic sensitivity assessment: Polatuzumab vedotin pharmacokinetics in Asian and non‐Asian patients with previously untreated diffuse large B‐cell lymphoma in POLARIX | Ethnic sensitivity assessment: Polatuzumab vedotin pharmacokinetics in Asian and non‐Asian patients with previously untreated diffuse large B‐cell lymphoma in POLARIX Abstract Abstract This ethnic sensitivity analysis used data from the phase III POLARIX study (NCT03274492) to assess polatuzumab vedotin pharmacokinetic... |
PMC10474647 | core_pubmed_pmc | Role of trazodone in treatment of major depressive disorder: an update | Role of trazodone in treatment of major depressive disorder: an update Abstract Major depressive disorder (MDD) is the most common mood disorder and a leading cause of disability worldwide. Trazodone, a triazolopyridine serotonin receptor antagonist and reuptake inhibitor (SARI) antidepressant approved for major depres... |
PMC12489760 | core_pubmed_pmc | Exploring the role of sex in asthma and COPD pharmacological treatment | Exploring the role of sex in asthma and COPD pharmacological treatment Abstract Sex is a fundamental determinant in pharmacology, influencing disease prevalence, severity, and therapeutic responses. Differences in pharmacokinetics and pharmacodynamics between men and women contribute to variations in drug efficacy and ... |
PMC11283214 | core_pubmed_pmc | Comparative pharmacokinetics of six components in normal and rheumatoid arthritis rats after intragastrical administration of Qianghuo Shengshi Decoction granules by LC-MS/MS | Comparative pharmacokinetics of six components in normal and rheumatoid arthritis rats after intragastrical administration of Qianghuo Shengshi Decoction granules by LC-MS/MS Abstract Objective To investigate the plasma pharmacokinetics of six representative components (nodakenin, osthole, 5- O -methylvisammioside, fer... |
PMC5629784 | core_pubmed_pmc | An open-label study to evaluate the long-term safety and efficacy of lanadelumab for prevention of attacks in hereditary angioedema: design of the HELP study extension | An open-label study to evaluate the long-term safety and efficacy of lanadelumab for prevention of attacks in hereditary angioedema: design of the HELP study extension Abstract Abstract Background Hereditary angioedema (HAE) is characterized by recurrent attacks of subcutaneous or submucosal edema. Attacks are unpredic... |
PMC8752548 | core_pubmed_pmc | Impact of a High-Fat Meal and Sprinkled Administration on the Bioavailability and Pharmacokinetics of Viloxazine Extended-Release Capsules (Qelbree TM ) in Healthy Adult Subjects | Impact of a High-Fat Meal and Sprinkled Administration on the Bioavailability and Pharmacokinetics of Viloxazine Extended-Release Capsules (Qelbree TM ) in Healthy Adult Subjects Abstract Abstract Background and Objectives Viloxazine extended-release (viloxazine ER) capsules (Qelbree TM ) is a novel nonstimulant recent... |
PMC8595249 | core_pubmed_pmc | Development of highly stable and de-immunized versions of recombinant alpha interferon: Promising candidates for the treatment of chronic and emerging viral diseases | Development of highly stable and de-immunized versions of recombinant alpha interferon: Promising candidates for the treatment of chronic and emerging viral diseases Abstract Abstract Human interferon alpha (hIFN-α) administration constitutes the current FDA approved therapy for chronic Hepatitis B and C virus infectio... |
PMC10345962 | core_pubmed_pmc | ONC201 in Combination with Paxalisib for the Treatment of H3K27-Altered Diffuse Midline Glioma | ONC201 in Combination with Paxalisib for the Treatment of H3K27-Altered Diffuse Midline Glioma Abstract Abstract Diffuse midline gliomas (DMG), including diffuse intrinsic pontine gliomas (DIPG), are the most lethal of childhood cancers. Palliative radiotherapy is the only established treatment, with median patient sur... |
PMC11179701 | core_pubmed_pmc | Population pharmacokinetics of intraperitoneal irinotecan and SN‐38 in patients with peritoneal metastases from colorectal origin | Population pharmacokinetics of intraperitoneal irinotecan and SN‐38 in patients with peritoneal metastases from colorectal origin Abstract Abstract Peritoneal metastases (PM) are common in patients with colorectal cancer. Patients with PM have a poor prognosis, and for those who are not eligible for cytoreductive surge... |
PMC12030419 | core_pubmed_pmc | The Clinical Utility of Precision-Guided Dosing for Adalimumab Therapy Optimization in Inflammatory Bowel Disease: A Clinical Experience Program † | The Clinical Utility of Precision-Guided Dosing for Adalimumab Therapy Optimization in Inflammatory Bowel Disease: A Clinical Experience Program † Abstract Abstract Background/Objectives : This study aimed to establish the clinical utility of a therapeutic drug monitoring (TDM)-supported, model-informed precision dosin... |
PMC10461573 | core_pubmed_pmc | Tusamitamab Ravtansine in Patients with Advanced Solid Tumors: Phase I Study of Safety, Pharmacokinetics, and Antitumor Activity Using Alternative Dosing Regimens | Tusamitamab Ravtansine in Patients with Advanced Solid Tumors: Phase I Study of Safety, Pharmacokinetics, and Antitumor Activity Using Alternative Dosing Regimens Abstract Abstract Purpose: Tusamitamab ravtansine is an antibody–drug conjugate that targets carcinoembryonic antigen-related cell adhesion molecule 5 (CEACA... |
PMC7341081 | core_pubmed_pmc | Sulfoxide‐Containing Polymer‐Coated Nanoparticles Demonstrate Minimal Protein Fouling and Improved Blood Circulation | Sulfoxide‐Containing Polymer‐Coated Nanoparticles Demonstrate Minimal Protein Fouling and Improved Blood Circulation Abstract Abstract Minimizing the interaction of nanomedicines with the mononuclear phagocytic system (MPS) is a critical challenge for their clinical translation. Conjugating polyethylene glycol (PEG) to... |
PMC5822518 | core_pubmed_pmc | Studying the Inhibitory Effect of Quercetin and Thymoquinone on Human Cytochrome P450 Enzyme Activities | Studying the Inhibitory Effect of Quercetin and Thymoquinone on Human Cytochrome P450 Enzyme Activities Abstract Background: Quercetin (QR) and thymoquinone (TQ) are herbal remedies that are currently extensively used by the general population to prevent and treat various chronic conditions. Therefore, investigating th... |
PMC10189459 | core_pubmed_pmc | Injectable sustained‐release poly(lactic‐co‐glycolic acid) (PLGA) microspheres of exenatide prepared by supercritical fluid extraction of emulsion process based on a design of experiment approach | Injectable sustained‐release poly(lactic‐co‐glycolic acid) (PLGA) microspheres of exenatide prepared by supercritical fluid extraction of emulsion process based on a design of experiment approach Abstract Abstract This study aimed to develop an improved sustained‐release (SR) PLGA microsphere of exenatide using supercr... |
PMC10831265 | core_pubmed_pmc | Nanosphere pharmacodynamics improves safety of immunostimulatory cytokine therapy | Nanosphere pharmacodynamics improves safety of immunostimulatory cytokine therapy Abstract Summary Systemic administration of interleukin (IL)-12 induces potent anti-tumor immune responses in preclinical cancer models through the systemic activation of effector immune cells and release of proinflammatory cytokines. IL-... |
PMC11217592 | core_pubmed_pmc | Pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid in rainbow trout ( Oncorhynchus mykiss ) | Pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid in rainbow trout ( Oncorhynchus mykiss ) Abstract Abstract Background Although research on the mechanism and control of pain and inflammation in fish has increased in recent years, the use of analgesic drugs is limited due to the lack of ph... |
PMC4929566 | core_pubmed_pmc | The metabolome of [2- 14 C](−)-epicatechin in humans: implications for the assessment of efficacy, safety, and mechanisms of action of polyphenolic bioactives | The metabolome of [2- 14 C](−)-epicatechin in humans: implications for the assessment of efficacy, safety, and mechanisms of action of polyphenolic bioactives Abstract Abstract Diet is a major life style factor affecting human health, thus emphasizing the need for evidence-based dietary guidelines for primary disease p... |
PMC10840439 | core_pubmed_pmc | Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies | Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies Abstract Epigenetic pathways play a critical role in the initiation, progression, and metastasis of cancer. Over the past few decades, significant progress has been made in the development of targeted epigenetic modul... |
PMC11390758 | core_pubmed_pmc | Physiologically-based pharmacokinetic models versus allometric scaling for prediction of tyrosine-kinase inhibitor exposure from adults to children | Physiologically-based pharmacokinetic models versus allometric scaling for prediction of tyrosine-kinase inhibitor exposure from adults to children Abstract Purpose Model-based methods can predict pediatric exposure and support initial dose selection. The aim of this study was to evaluate the performance of allometric ... |
PMC7497701 | core_pubmed_pmc | Onapristone Extended Release: Safety Evaluation from Phase I–II Studies with an Emphasis on Hepatotoxicity | Onapristone Extended Release: Safety Evaluation from Phase I–II Studies with an Emphasis on Hepatotoxicity Abstract Introduction Antiprogestins have demonstrated promising activity against breast and gynecological cancers, but liver-related safety concerns limited the advancement of this therapeutic class. Onapristone ... |
PMC11348505 | core_pubmed_pmc | Momelotinib: Mechanism of action, clinical, and translational science | Momelotinib: Mechanism of action, clinical, and translational science Abstract Abstract Myelofibrosis is a chronic myeloproliferative disorder characterized by bone marrow fibrosis, splenomegaly, anemia, and constitutional symptoms, with a median survival of ≈6 years from diagnosis. While currently approved Janus kinas... |
PMC12908737 | core_pubmed_pmc | Growth Trajectories of Medication Adherence in Pediatric Organ Transplantation and Their Relationship to Posttransplant Health Outcomes | Growth Trajectories of Medication Adherence in Pediatric Organ Transplantation and Their Relationship to Posttransplant Health Outcomes Abstract Abstract Background. Nonadherence to immunosuppressive medication remains one of the most critical predictors of late acute rejection, hospitalization, and graft loss in pedia... |
PMC12287053 | core_pubmed_pmc | Case Report: I want more olanzapine: pharmacogenetic insights into a patient's preference for high-dose olanzapine | Case Report: I want more olanzapine: pharmacogenetic insights into a patient's preference for high-dose olanzapine Abstract Olanzapine is an effective antipsychotic agent, but its metabolism shows considerable interindividual variability. We present a case of a patient with treatment-resistant schizophrenia who consist... |
PMC11522146 | core_pubmed_pmc | Coadministration of Cariprazine with a Moderate CYP3A4 Inhibitor in Patients with Schizophrenia: Implications for Dose Adjustment and Safety Monitoring | Coadministration of Cariprazine with a Moderate CYP3A4 Inhibitor in Patients with Schizophrenia: Implications for Dose Adjustment and Safety Monitoring Abstract Background Cariprazine is metabolised mainly by CYP3A4 and to a lesser extent by CYP2D6. Aim This study aimed to evaluate the effects of erythromycin, a modera... |
PMC11374634 | core_pubmed_pmc | Dynamics and implications of anti-drug antibodies against adalimumab using ultra-sensitive and highly drug-tolerant assays | Dynamics and implications of anti-drug antibodies against adalimumab using ultra-sensitive and highly drug-tolerant assays Abstract Abstract Background Adalimumab induces the production of anti-drug antibodies (ADA) that may lead to reduced drug concentration and loss-of-response, posing significant clinical challenges... |
PMC8398060 | core_pubmed_pmc | Lipid Nanocarriers for Anti-HIV Therapeutics: A Focus on Physicochemical Properties and Biotechnological Advances | Lipid Nanocarriers for Anti-HIV Therapeutics: A Focus on Physicochemical Properties and Biotechnological Advances Abstract Since HIV was first identified, and in a relatively short period of time, AIDS has become one of the most devastating infectious diseases of the 21st century. Classical antiretroviral therapies wer... |
PMC11280233 | core_pubmed_pmc | Assessment of Infant Exposure to Antidepressants through Breastfeeding: A Literature Review of Currently Available Approaches | Assessment of Infant Exposure to Antidepressants through Breastfeeding: A Literature Review of Currently Available Approaches Abstract Abstract Despite the prevalence of depression in lactating mothers, there is a lack of knowledge about the excretion of antidepressants into breast milk and its potential adverse effect... |
PMC10301382 | core_pubmed_pmc | Novel Bioequivalent Tablet of Solifenacin Succinate Prepared Using Direct Compression Technique for Improved Chemical Stability | Novel Bioequivalent Tablet of Solifenacin Succinate Prepared Using Direct Compression Technique for Improved Chemical Stability Abstract Abstract We designed a bioequivalent tablet form of solifenacin succinate (SOL) with an improved storage stability using a direct compression (DC) technique. An optimal direct compres... |
PMC8880589 | core_pubmed_pmc | Drug-Herb Interactions among Thai Herbs and Anticancer Drugs: A Scoping Review | Drug-Herb Interactions among Thai Herbs and Anticancer Drugs: A Scoping Review Abstract Abstract More than half of Thai patients with cancer take herbal preparations while receiving anticancer therapy. There is no systematic or scoping review on interactions between anticancer drugs and Thai herbs, although several res... |
PMC8451805 | core_pubmed_pmc | A Pharmacokinetic Bioequivalence Study of Fremanezumab Administered Subcutaneously Using an Autoinjector and a Prefilled Syringe | A Pharmacokinetic Bioequivalence Study of Fremanezumab Administered Subcutaneously Using an Autoinjector and a Prefilled Syringe Abstract Abstract Fremanezumab (AJOVY; Teva Pharmaceutical Industries Ltd, Netanya, Israel), approved for the preventive treatment of migraine, is available as a subcutaneous injection either... |
PMC3513198 | core_pubmed_pmc | Pharmacogenetics of rheumatoid arthritis: Potential targets from susceptibility genes and present therapies | Pharmacogenetics of rheumatoid arthritis: Potential targets from susceptibility genes and present therapies Abstract Abstract Rheumatoid arthritis (RA) is a chronic heterogeneous autoimmune disorder of unknown etiology resulting in inflammation in the synovium, cartilage, and bone. Genetic factors play an important rol... |
PMC7308462 | core_pubmed_pmc | Liposomal Delivery of Mycophenolic Acid With Quercetin for Improved Breast Cancer Therapy in SD Rats | Liposomal Delivery of Mycophenolic Acid With Quercetin for Improved Breast Cancer Therapy in SD Rats Abstract Abstract The present study explores the influence of mycophenolic acid (MPA) in combination therapy with quercetin (QC) (impeding MPA metabolic rate) delivered using the liposomal nanoparticles (LNPs). Mycophen... |
PMC5216653 | core_pubmed_pmc | Application of a Mechanistic Model to Evaluate Putative Mechanisms of Tolvaptan Drug-Induced Liver Injury and Identify Patient Susceptibility Factors | Application of a Mechanistic Model to Evaluate Putative Mechanisms of Tolvaptan Drug-Induced Liver Injury and Identify Patient Susceptibility Factors Abstract Abstract Tolvaptan is a selective vasopressin V2 receptor antagonist, approved in several countries for the treatment of hyponatremia and autosomal dominant poly... |
PMC11491004 | core_pubmed_pmc | CHF6523 data suggest that the phosphoinositide 3-kinase delta isoform is not a suitable target for the management of COPD | CHF6523 data suggest that the phosphoinositide 3-kinase delta isoform is not a suitable target for the management of COPD Abstract Abstract Background Chronic obstructive pulmonary disease (COPD) is a chronic inflammatory condition. Given patients with COPD continue to experience exacerbations despite the availability ... |
PMC3904834 | core_pubmed_pmc | Overview of the role of nanotechnological innovations in the detection and treatment of solid tumors | Overview of the role of nanotechnological innovations in the detection and treatment of solid tumors Abstract Abstract Nanotechnology, although still in its infantile stages, has the potential to revolutionize the diagnosis, treatment, and monitoring of disease progression and success of therapy for numerous diseases a... |
PMC7870480 | core_pubmed_pmc | Comparative Study on Pharmacokinetics of Four Long-Acting Injectable Formulations of Enrofloxacin in Pigs | Comparative Study on Pharmacokinetics of Four Long-Acting Injectable Formulations of Enrofloxacin in Pigs Abstract Abstract A comparative study on pharmacokinetics of four long-acting enrofloxacin injectable formulations was investigated in 36 healthy pigs after intramuscular injection according to the recommended sing... |
PMC3619536 | core_pubmed_pmc | Liposomal Doxorubicin in the Treatment of Breast Cancer Patients: A Review | Liposomal Doxorubicin in the Treatment of Breast Cancer Patients: A Review Abstract Abstract Drug delivery systems can provide enhanced efficacy and/or reduced toxicity for anticancer agents. Liposome drug delivery systems are able to modify the pharmacokinetics and biodistribution of cytostatic agents, increasing the ... |
PMC5763271 | core_pubmed_pmc | Pharmacokinetics and Safety of a Single Oral Dose of Mirogabalin in Japanese Subjects With Varying Degrees of Renal Impairment | Pharmacokinetics and Safety of a Single Oral Dose of Mirogabalin in Japanese Subjects With Varying Degrees of Renal Impairment Abstract Abstract Mirogabalin (DS‐5565) is a novel preferentially selective α 2 δ‐1 ligand being developed for the treatment of diabetic peripheral neuropathic pain and postherpetic neuralgia. ... |
PMC10175358 | core_pubmed_pmc | Population Pharmacokinetic and Pharmacodynamic Modeling of Fesoterodine in Pediatric Patients with Neurogenic Detrusor Overactivity | Population Pharmacokinetic and Pharmacodynamic Modeling of Fesoterodine in Pediatric Patients with Neurogenic Detrusor Overactivity Abstract Abstract Background and Objective Fesoterodine is a muscarinic receptor antagonist approved for the treatment of overactive bladder (OAB) in adults and neurogenic detrusor overact... |
PMC11403021 | core_pubmed_pmc | Exploring Apixaban Pharmacokinetics, Pharmacodynamics, and Safety in Hemodiafiltration Patients | Exploring Apixaban Pharmacokinetics, Pharmacodynamics, and Safety in Hemodiafiltration Patients Results Results The study was conducted between May 2021 and October 2022. The study design is shown in Supplementary Figure S1 , and a detailed protocol can be found in the supplementary material . Ten patients on dialysis ... |
PMC11264651 | core_pubmed_pmc | Pharmacokinetics, Safety, and Immunogenicity of Intravenous and Subcutaneous Single-Dose QX002N Injection in Healthy Subjects: A Randomized, Open, Parallel, Single-Center, Phase I Study | Pharmacokinetics, Safety, and Immunogenicity of Intravenous and Subcutaneous Single-Dose QX002N Injection in Healthy Subjects: A Randomized, Open, Parallel, Single-Center, Phase I Study Abstract Abstract Introduction Interleukin-17A (IL-17A) plays a crucial role in the pathogenesis of ankylosing spondylitis (AS), altho... |
PMC10819636 | core_pubmed_pmc | Triterpenes Drug Delivery Systems, a Modern Approach for Arthritis Targeted Therapy | Triterpenes Drug Delivery Systems, a Modern Approach for Arthritis Targeted Therapy Abstract Abstract Arthritis is a major cause of disability. Currently available anti-arthritic drugs, such as disease-modifying anti-rheumatic drugs (DMARDs), have serious side-effects associated with long-term use. Triterpenoids are na... |
PMC5514197 | core_pubmed_pmc | A two-step deconvolution-analysis-informed population pharmacodynamic modeling approach for drugs targeting pulsatile endogenous compounds | A two-step deconvolution-analysis-informed population pharmacodynamic modeling approach for drugs targeting pulsatile endogenous compounds Abstract Pharmacodynamic modeling of pulsatile endogenous compounds (e.g. growth hormone [GH]) is currently limited to the identification of a low number of pulses. Commonly used ph... |
PMC7679441 | core_pubmed_pmc | Adjuvant role of Ocimum sanctum hydroalcoholic extract with carbamazepine and phenytoin in experimental model of acute seizures | Adjuvant role of Ocimum sanctum hydroalcoholic extract with carbamazepine and phenytoin in experimental model of acute seizures Abstract Highlights • Ocimum sanctum hydroalcoholic extract (OSHE) potential as an adjuvant to antiepileptic drugs (AEDs) carbamazepine and phenytoin is studied in maximal electroshock seizure... |
PMC8818956 | core_pubmed_pmc | Genistein: A Review on its Anti-Inflammatory Properties | Genistein: A Review on its Anti-Inflammatory Properties Abstract Nowadays, non-resolving inflammation is becoming a major trigger in various diseases as it plays a significant role in the pathogenesis of atherosclerosis, asthma, cancer, obesity, inflammatory bowel disease, chronic obstructive pulmonary disease, neurode... |
PMC6604691 | core_pubmed_pmc | Immuno-PET Imaging to Assess Target Engagement: Experience from 89 Zr-Anti-HER3 mAb (GSK2849330) in Patients with Solid Tumors | Immuno-PET Imaging to Assess Target Engagement: Experience from 89 Zr-Anti-HER3 mAb (GSK2849330) in Patients with Solid Tumors Abstract Abstract PET imaging with radiolabeled drugs provides information on tumor uptake and dose-dependent target interaction to support selection of an optimal dose for future efficacy test... |
PMC6375436 | core_pubmed_pmc | Evaluation and Optimization of Pharmacokinetic Models for in Vitro to in Vivo Extrapolation of Estrogenic Activity for Environmental Chemicals | Evaluation and Optimization of Pharmacokinetic Models for in Vitro to in Vivo Extrapolation of Estrogenic Activity for Environmental Chemicals Abstract Background: To effectively incorporate in vitro data into regulatory use, confidence must be established in the quantitative extrapolation of in vitro activity to relev... |
PMC6300689 | core_pubmed_pmc | A Novel, Rapid, and Low-Volume Assay for Therapeutic Drug Monitoring of Posaconazole and Other Long-Chain Azole-Class Antifungal Drugs | A Novel, Rapid, and Low-Volume Assay for Therapeutic Drug Monitoring of Posaconazole and Other Long-Chain Azole-Class Antifungal Drugs Abstract This work describes an effective assay for TDM of long-chain azole-class antifungal drugs that can be used in diluted human serum samples. This assay will provide a quick, cost... |
PMC6710528 | core_pubmed_pmc | Effects of CYP3A inhibitors on the pharmacokinetics of quizartinib, a potent and selective FLT3 inhibitor, and its active metabolite | Effects of CYP3A inhibitors on the pharmacokinetics of quizartinib, a potent and selective FLT3 inhibitor, and its active metabolite Abstract Abstract Aims Quizartinib is an oral, highly potent and selective next‐generation FMS‐like tyrosine kinase 3 (FLT3) inhibitor under investigation in patients with FLT3 ‐internal ... |
PMC8359308 | core_pubmed_pmc | Pharmacokinetics and Safety of Glasdegib in Participants With Moderate/Severe Hepatic Impairment: A Phase I, Single‐Dose, Matched Case‐Control Study | Pharmacokinetics and Safety of Glasdegib in Participants With Moderate/Severe Hepatic Impairment: A Phase I, Single‐Dose, Matched Case‐Control Study Abstract Abstract This phase I open‐label trial ( NCT03627754 ) assessed glasdegib pharmacokinetics and safety in otherwise healthy participants with moderate (Child‐Pugh ... |
PMC12235394 | core_pubmed_pmc | Derisking Phase II Clinical Trials in Heart Failure | Derisking Phase II Clinical Trials in Heart Failure Abstract Phase II clinical trials play an important role in drug development, providing key data that guide decision-making for promising therapeutic candidates. An important objective of phase II is to establish proof of concept by demonstrating that the drug produce... |
PMC6058681 | core_pubmed_pmc | Plateau hypoxia attenuates the metabolic activity of intestinal flora to enhance the bioavailability of nifedipine | Plateau hypoxia attenuates the metabolic activity of intestinal flora to enhance the bioavailability of nifedipine Abstract Abstract Nifedipine is completely absorbed by the gastrointestinal tract and its pharmacokinetics and metabolism may be influenced by microorganisms. If gut microbes are involved in the metabolism... |
PMC9825044 | core_pubmed_pmc | Afoxolaner (NexGard®) in pet snakes for the treatment and control of Ophionyssus natricis (Mesostigmata: Macronyssidae) | Afoxolaner (NexGard®) in pet snakes for the treatment and control of Ophionyssus natricis (Mesostigmata: Macronyssidae) Abstract Abstract Background Ophionyssus natricis is the main species of mite that infests captive reptiles. High infestations may result in the host experiencing general discomfort and deleterious ef... |
PMC12202199 | core_pubmed_pmc | The Impact of Augmented Renal Clearance on the Pharmacokinetics of Levetiracetam in Critically Ill Patients: A Literature Review | The Impact of Augmented Renal Clearance on the Pharmacokinetics of Levetiracetam in Critically Ill Patients: A Literature Review Abstract Abstract Levetiracetam is an antiseizure medication (ASM) that has several advantages over other ASMs, such as dose‐proportional pharmacokinetics, high bioavailability, and minimal d... |
PMC8705663 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of T-Cell Bispecifics in the Tumour Interstitial Fluid | Pharmacokinetics and Pharmacodynamics of T-Cell Bispecifics in the Tumour Interstitial Fluid Abstract Abstract The goal of this study is to investigate the pharmacokinetics in plasma and tumour interstitial fluid of two T-cell bispecifics (TCBs) with different binding affinities to the tumour target and to assess the s... |
PMC11708499 | core_pubmed_pmc | Superior bioavailability of EPA and DHA from a L-lysine salt formulation: a randomized, three-way crossover study | Superior bioavailability of EPA and DHA from a L-lysine salt formulation: a randomized, three-way crossover study Abstract Abstract Background Omega-3 fatty acids, including eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), are polyunsaturated fatty acids (PUFAs) with notable health benefits. Due to limited p... |
PMC3476427 | core_pubmed_pmc | Bioavailability and pharmacokinetics of oral meloxicam in llamas | Bioavailability and pharmacokinetics of oral meloxicam in llamas Abstract Abstract Background South American camelids in the United States have rapidly developed into an important agricultural industry in need of veterinary services. Pain management is challenging in camelids because there are no drugs currently approv... |
PMC8575045 | core_pubmed_pmc | Ustekinumab in Paediatric Patients with Moderately to Severely Active Crohn’s Disease: Pharmacokinetics, Safety, and Efficacy Results from UniStar, a Phase 1 Study | Ustekinumab in Paediatric Patients with Moderately to Severely Active Crohn’s Disease: Pharmacokinetics, Safety, and Efficacy Results from UniStar, a Phase 1 Study Abstract Abstract Background and Aims The objective was to evaluate the pharmacokinetics, safety/tolerability, and efficacy of ustekinumab in children with ... |
PMC8026424 | core_pubmed_pmc | Evaluating clinical impact of a shortened infusion duration for ramucirumab: a model-based approach | Evaluating clinical impact of a shortened infusion duration for ramucirumab: a model-based approach Abstract Purpose We investigated the impact of infusion duration (30 and 60 min) on the pharmacokinetic profile of ramucirumab using a population pharmacokinetic (PopPK) modeling approach. We also assessed the relationsh... |
PMC4092331 | core_pubmed_pmc | Tuning Pharmacokinetics and Biodistribution of a Targeted Drug Delivery System Through Incorporation of a Passive Targeting Component | Tuning Pharmacokinetics and Biodistribution of a Targeted Drug Delivery System Through Incorporation of a Passive Targeting Component Abstract Major challenges in the development of drug delivery systems (DDSs) have been the short half-life, poor bioavailability, insufficient accumulation and penetration of the DDSs in... |
PMC12706414 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Datopotamab Deruxtecan (Dato‐ DXd ), a TROP2 ‐Directed Antibody‐Drug Conjugate, in Patients With Advanced Solid Tumors | Population Pharmacokinetic Analysis of Datopotamab Deruxtecan (Dato‐ DXd ), a TROP2 ‐Directed Antibody‐Drug Conjugate, in Patients With Advanced Solid Tumors Abstract ABSTRACT Datopotamab deruxtecan (Dato‐DXd) is a trophoblast cell surface antigen 2 (TROP2)‐directed antibody‐drug conjugate (ADC) developed for the treat... |
PMC6220743 | core_pubmed_pmc | The Herb-Drug Interaction of Clopidogrel and Xuesaitong Dispersible Tablet by Modulation of the Pharmacodynamics and Liver Carboxylesterase 1A Metabolism | The Herb-Drug Interaction of Clopidogrel and Xuesaitong Dispersible Tablet by Modulation of the Pharmacodynamics and Liver Carboxylesterase 1A Metabolism Abstract Objective Clopidogrel and Xuesaitong dispersible tablet (XST) have been clinically proven to be effective for treating cardiocerebrovascular disease. The pre... |
PMC11468589 | core_pubmed_pmc | Liposomes and Extracellular Vesicles as Drug Delivery Systems: A Comparison of Composition, Pharmacokinetics, and Functionalization | Liposomes and Extracellular Vesicles as Drug Delivery Systems: A Comparison of Composition, Pharmacokinetics, and Functionalization Abstract Abstract Over the past decades, lipid‐based nanoparticle drug delivery systems (DDS) have caught the attention of researchers worldwide, encouraging the field to rapidly develop i... |
PMC10128151 | core_pubmed_pmc | A Comparison of the Pharmacokinetics and Safety of Dapagliflozin Formate, an Ester Prodrug of Dapagliflozin, to Dapagliflozin Propanediol Monohydrate in Healthy Subjects | A Comparison of the Pharmacokinetics and Safety of Dapagliflozin Formate, an Ester Prodrug of Dapagliflozin, to Dapagliflozin Propanediol Monohydrate in Healthy Subjects Abstract Abstract Background Dapagliflozin formate (DAP-FOR, DA-2811), an ester prodrug of dapagliflozin, was developed to improve the stability and p... |
PMC7484914 | core_pubmed_pmc | Proposed Therapeutic Range of Treosulfan in Reduced Toxicity Pediatric Allogeneic Hematopoietic Stem Cell Transplant Conditioning: Results From a Prospective Trial | Proposed Therapeutic Range of Treosulfan in Reduced Toxicity Pediatric Allogeneic Hematopoietic Stem Cell Transplant Conditioning: Results From a Prospective Trial Abstract Treosulfan is given off‐label in pediatric allogeneic hematopoietic stem cell transplant. This study investigated treosulfan's pharmacokinetics (PK... |
PMC9412022 | core_pubmed_pmc | Integrate thermostabilized fusion protein apocytochrome b 562 RIL and N-glycosylation mutations: A novel approach to heterologous expression of human UDP-glucuronosyltransferase (UGT) 2B7 | Integrate thermostabilized fusion protein apocytochrome b 562 RIL and N-glycosylation mutations: A novel approach to heterologous expression of human UDP-glucuronosyltransferase (UGT) 2B7 Abstract Human UDP-glucuronosyltransferase (UGT) 2B7 is a crucial phase II metabolic enzyme that transfers glucuronic acid from UDP-... |
PMC6989240 | core_pubmed_pmc | Non-compartmental data analysis using SimBiology and MATLAB | Non-compartmental data analysis using SimBiology and MATLAB Abstract MATLAB® is widely used for numerical analysis, modeling, and simulation. One of MATLAB's tools, SimBiology®, is often used for pharmacokinetic, pharmacodynamic model and dynamic systems; however, SimBiology seems to be rarely used for non-compartmenta... |
PMC6402190 | core_pubmed_pmc | Intravenous Hydroxypropyl β‐Cyclodextrin Formulation of Letermovir: A Phase I, Randomized, Single‐Ascending, and Multiple‐Dose Trial | Intravenous Hydroxypropyl β‐Cyclodextrin Formulation of Letermovir: A Phase I, Randomized, Single‐Ascending, and Multiple‐Dose Trial Abstract Abstract Letermovir is a novel antiviral in clinical development for prophylaxis against human cytomegalovirus in immunocompromised transplant recipients. This two‐part, single‐c... |
PMC11039630 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic analysis of drug liking blockade by buprenorphine subcutaneous depot (CAM2038) in participants with opioid use disorder | Pharmacokinetic-pharmacodynamic analysis of drug liking blockade by buprenorphine subcutaneous depot (CAM2038) in participants with opioid use disorder Abstract Abstract Buprenorphine is used to treat opioid use disorder (OUD). Weekly and monthly subcutaneous long-acting buprenorphine injections (CAM2038) provide more ... |
PMC9167405 | core_pubmed_pmc | First-in-Human Phase I Study of the Novel Injectable Calcimimetic Agent Upacicalcet in Healthy Adult Japanese Participants | First-in-Human Phase I Study of the Novel Injectable Calcimimetic Agent Upacicalcet in Healthy Adult Japanese Participants Abstract Abstract Background and Objective Upacicalcet sodium hydrate is a novel small-molecule calcimimetic and has potential as a therapeutic agent for secondary hyperparathyroidism. We assessed ... |
PMC12641077 | core_pubmed_pmc | Microbiome‐Informed Dosing: Exploring Gut Microbial Communities Impact on Mycophenolate Enterohepatic Circulation and Therapeutic Target Achievement | Microbiome‐Informed Dosing: Exploring Gut Microbial Communities Impact on Mycophenolate Enterohepatic Circulation and Therapeutic Target Achievement Abstract Pharmacomicrobiomics is an emerging field due to important microbiome effects on pharmacokinetics and clinical outcomes. However, the application of this knowledg... |
PMC12856065 | core_pubmed_pmc | The Regularized Horseshoe for Covariate Selection Improves Convenience and Predictive Performance in Population PK/PD Models | The Regularized Horseshoe for Covariate Selection Improves Convenience and Predictive Performance in Population PK/PD Models Abstract ABSTRACT We introduce the Regularized Horseshoe (RHS) in the context of covariate selection for population PK/PD models. Unlike stepwise approaches which are commonly used in this contex... |
PMC12974148 | core_pubmed_pmc | Nanobody-Based Drug Delivery: Emerging Strategies for Targeted Cancer Therapy | Nanobody-Based Drug Delivery: Emerging Strategies for Targeted Cancer Therapy Abstract Abstract Traditional cancer treatments such as chemotherapy and radiotherapy remain effective but lack specificity, often causing collateral damage to healthy tissues. Antibody-drug conjugates (ADCs) using monoclonal antibodies (mAbs... |
PMC8213422 | core_pubmed_pmc | Nonparametric goodness‐of‐fit testing for parametric covariate models in pharmacometric analyses | Nonparametric goodness‐of‐fit testing for parametric covariate models in pharmacometric analyses Abstract Abstract The characterization of covariate effects on model parameters is a crucial step during pharmacokinetic/pharmacodynamic analyses. Although covariate selection criteria have been studied extensively, the cho... |
PMC8049015 | core_pubmed_pmc | Exposure‐Response Analyses for Upadacitinib Efficacy in Subjects With Atopic Dermatitis—Analyses of Phase 2b Study to Support Selection of Phase 3 Doses | Exposure‐Response Analyses for Upadacitinib Efficacy in Subjects With Atopic Dermatitis—Analyses of Phase 2b Study to Support Selection of Phase 3 Doses Abstract Abstract Upadacitinib is a selective Janus kinase 1 inhibitor that was recently approved for treatment of rheumatoid arthritis and is currently being evaluate... |
PMC11754493 | core_pubmed_pmc | Modified dosing schedule efficacy of fosmidomycin and clindamycin against murine malaria Plasmodium berghei | Modified dosing schedule efficacy of fosmidomycin and clindamycin against murine malaria Plasmodium berghei Abstract Abstract Fosmidomycin and clindamycin target the Plasmodium apicoplast. Combination clinical trials have produced mixed results with the primary problem being the recrudescent infection frequency by day ... |
PMC9321685 | core_pubmed_pmc | Pharmacokinetics of glucagon after intravenous, intraperitoneal and subcutaneous administration in a pig model | Pharmacokinetics of glucagon after intravenous, intraperitoneal and subcutaneous administration in a pig model Abstract Abstract Introduction There is increasing scientific evidence to substantiate using low‐dose glucagon as a supplement to insulin therapy in artificial pancreata for diabetes mellitus type 1. The deliv... |
PMC11910062 | core_pubmed_pmc | A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects | A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics of BGT-002, a Novel ATP-Citrate Lyase Inhibitor, in Healthy Chinese Subjects Abstract Objective This Phase I study evaluated the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of BGT-002, a novel ATP-citrate lyase (ACLY) inhib... |
PMC12009758 | core_pubmed_pmc | Ocular pharmacokinetics of intravitreal conbercept in a rabbit model following retinal scatter laser photocoagulation | Ocular pharmacokinetics of intravitreal conbercept in a rabbit model following retinal scatter laser photocoagulation Abstract Abstract Objective The present study aims to evaluate the ocular pharmacokinetics of intravitreal conbercept after retinal scatter laser photocoagulation. Methods Thirty male Chinchilla rabbits... |
PMC6163367 | core_pubmed_pmc | The Protective Effect of a Long-Acting and Multi-Target HM-3-Fc Fusion Protein in Rheumatoid Arthritis | The Protective Effect of a Long-Acting and Multi-Target HM-3-Fc Fusion Protein in Rheumatoid Arthritis Abstract Abstract Current treatment of rheumatoid arthritis (RA) is limited by relative shortage of treatment targets. HM-3 is a novel anti-RA polypeptide consisting of 18 amino acids with integrin αVβ3 and α5β1 as ta... |
PMC10821095 | core_pubmed_pmc | Preclinical Pharmacokinetics and Biodistribution of LR004, a Novel Antiepidermal Growth Factor Receptor Monoclonal Antibody | Preclinical Pharmacokinetics and Biodistribution of LR004, a Novel Antiepidermal Growth Factor Receptor Monoclonal Antibody Abstract LR004 is a novel chimeric (human/mouse) monoclonal antibody developed for the treatment of advanced colorectal carcinoma with detectable epidermal growth factor receptor (EGFR) expression... |
PMC6348461 | core_pubmed_pmc | Phase 1, randomized, parallel-group, double-blind, placebo-controlled trial to evaluate the effects of erenumab (AMG 334) and concomitant sumatriptan on blood pressure in healthy volunteers | Phase 1, randomized, parallel-group, double-blind, placebo-controlled trial to evaluate the effects of erenumab (AMG 334) and concomitant sumatriptan on blood pressure in healthy volunteers Abstract Abstract Objectives The aim of this study was to assess the effects of concomitant administration of erenumab and sumatri... |
PMC8602678 | core_pubmed_pmc | Prediction of Belimumab Pharmacokinetics in Chinese Pediatric Patients with Systemic Lupus Erythematosus | Prediction of Belimumab Pharmacokinetics in Chinese Pediatric Patients with Systemic Lupus Erythematosus Abstract Abstract Background and Objective Intravenous (IV) belimumab is the first treatment approved for children ≥5 years of age with active autoantibody-positive systemic lupus erythematosus (SLE) in the USA, Eur... |
PMC12777568 | core_pubmed_pmc | The effect of antacid and mineral supplements on bictegravir pharmacokinetics: results from a Phase 1, open-label, drug–drug interaction study | The effect of antacid and mineral supplements on bictegravir pharmacokinetics: results from a Phase 1, open-label, drug–drug interaction study Abstract ABSTRACT The mechanism of action of integrase strand transfer inhibitors involves binding to magnesium ions in the active site of the HIV integrase enzyme, making them ... |
PMC10534510 | core_pubmed_pmc | Optimized Extraction of Polyphenols from Unconventional Edible Plants: LC-MS/MS Profiling of Polyphenols, Biological Functions, Molecular Docking, and Pharmacokinetics Study | Optimized Extraction of Polyphenols from Unconventional Edible Plants: LC-MS/MS Profiling of Polyphenols, Biological Functions, Molecular Docking, and Pharmacokinetics Study Abstract Abstract Plant bioactive phenolic metabolites have recently attracted the attention of researchers due to their numerous health advantage... |
PMC3790193 | core_pubmed_pmc | Aerosolised 5-azacytidine suppresses tumour growth and reprogrammes the epigenome in an orthotopic lung cancer model | Aerosolised 5-azacytidine suppresses tumour growth and reprogrammes the epigenome in an orthotopic lung cancer model Abstract Abstract Background: Epigenetic silencing by promoter methylation and chromatin remodelling affects hundreds of genes and is a causal event for lung cancer. Treatment of patients with low doses ... |
PMC9985528 | core_pubmed_pmc | A Randomised Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of Palovarotene Ophthalmic Solution | A Randomised Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of Palovarotene Ophthalmic Solution Abstract Abstract Background and Objective Palovarotene, a selective retinoic acid receptor γ agonist, is under investigation for the treatment of dry eye disease. This study aimed to determine the ocu... |
PMC3884958 | core_pubmed_pmc | Managing insomnia: an overview of insomnia and pharmacologic treatment strategies in use and on the horizon | Managing insomnia: an overview of insomnia and pharmacologic treatment strategies in use and on the horizon Abstract Abstract This review explores basic sleep physiology, the mechanism of action for each class of hypnotic agents, their clinical application based on pharmacodynamic and pharmacokinetic factors, and poten... |
PMC7497038 | core_pubmed_pmc | Lipid droplet‐mediated scavenging as novel intrinsic and adaptive resistance factor against the multikinase inhibitor ponatinib | Lipid droplet‐mediated scavenging as novel intrinsic and adaptive resistance factor against the multikinase inhibitor ponatinib Abstract Abstract Ponatinib is a small molecule multi‐tyrosine kinase inhibitor clinically approved for anticancer therapy. Molecular mechanisms by which cancer cells develop resistance agains... |
PMC10582143 | core_pubmed_pmc | Pharmacokinetics of Oral Vitamin D in Children with Obesity and Asthma | Pharmacokinetics of Oral Vitamin D in Children with Obesity and Asthma Abstract Abstract Background and Objective Vitamin D insufficiency is common in several pediatric diseases including obesity and asthma. Little data exist describing the pharmacokinetics of oral vitamin D in children or the optimal dosing to achieve... |
PMC11716996 | core_pubmed_pmc | Pharmacokinetics of Geraniol and Its Metabolites in Mice After Oral Administration | Pharmacokinetics of Geraniol and Its Metabolites in Mice After Oral Administration Abstract ABSTRACT Geraniol is an acyclic monoterpene alcohol that is extracted from the essential oils of aromatic plants. Geraniol has several biological activities such as anti‐cancer, anti‐inflammatory, antioxidant, and neuroprotectiv... |
PMC3817799 | core_pubmed_pmc | Development and Evaluation of Solid Lipid Nanoparticles of Raloxifene Hydrochloride for Enhanced Bioavailability | Development and Evaluation of Solid Lipid Nanoparticles of Raloxifene Hydrochloride for Enhanced Bioavailability Abstract Abstract Raloxifene hydrochloride (RL-HCL) is an orally selective estrogen receptor modulator (SERM) with poor bioavailability of nearly 2% due to its poor aqueous solubility and extensive first pas... |
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