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PMC11638555 | core_pubmed_pmc | Target-site cefiderocol pharmacokinetics in soft tissues of healthy volunteers | Target-site cefiderocol pharmacokinetics in soft tissues of healthy volunteers Abstract Abstract Background Cefiderocol may potentially be used to treat skin and soft tissue infections (SSTIs). However, the pharmacokinetics of cefiderocol in human soft tissues have not yet been determined. The objective of the present ... |
PMC8945187 | core_pubmed_pmc | Hispolon-Loaded Liquid Crystalline Nanoparticles: Development, Stability, In Vitro Delivery Profile, and Assessment of Hepatoprotective Activity in Hepatocellular Carcinoma | Hispolon-Loaded Liquid Crystalline Nanoparticles: Development, Stability, In Vitro Delivery Profile, and Assessment of Hepatoprotective Activity in Hepatocellular Carcinoma Abstract Abstract The present work describes the development and characterization of liquid crystalline nanoparticles of hispolon (HP-LCNPs) for tr... |
PMC7471576 | core_pubmed_pmc | Pharmacokinetics and Monte Carlo Dosing Simulations of Imipenem in Critically Ill Patients with Life-Threatening Severe Infections During Support with Extracorporeal Membrane Oxygenation | Pharmacokinetics and Monte Carlo Dosing Simulations of Imipenem in Critically Ill Patients with Life-Threatening Severe Infections During Support with Extracorporeal Membrane Oxygenation Abstract Abstract Background Extracorporeal membrane oxygenation (ECMO), a cardiopulmonary bypass device, has been found to increase ... |
PMC4636270 | core_pubmed_pmc | Trough Concentrations of Vancomycin in Patients Undergoing Extracorporeal Membrane Oxygenation | Trough Concentrations of Vancomycin in Patients Undergoing Extracorporeal Membrane Oxygenation Abstract Abstract To investigate the appropriateness of the current vancomycin dosing strategy in adult patients with extracorporeal membrane oxygenation (ECMO), between March 2013 and November 2013, patients who were treated... |
PMC6726679 | core_pubmed_pmc | FF‐10832 enables long survival via effective gemcitabine accumulation in a lethal murine peritoneal dissemination model | FF‐10832 enables long survival via effective gemcitabine accumulation in a lethal murine peritoneal dissemination model Abstract Abstract Chemotherapy has been the treatment of choice for unresectable peritoneal dissemination; however, it is difficult to eradicate such tumors because of poor drug delivery. To solve thi... |
PMC9283731 | core_pubmed_pmc | A randomized, cross‐over trial of metoprolol succinate formulations to evaluate PK and PD end points for therapeutic equivalence | A randomized, cross‐over trial of metoprolol succinate formulations to evaluate PK and PD end points for therapeutic equivalence Abstract Abstract There are limited comparison data throughout the dosing interval for generic versus brand metoprolol extended‐release (ER) tablets. We compared the pharmacokinetics (PKs) an... |
PMC3737021 | core_pubmed_pmc | Herbal-drug interaction induced rhabdomyolysis in a liposarcoma patient receiving trabectedin | Herbal-drug interaction induced rhabdomyolysis in a liposarcoma patient receiving trabectedin Abstract Abstract Background Rhabdomyolysis is an uncommon side effect of trabectedin which is used for the second line therapy of metastatic sarcoma after anthracycline and ifosfamide failure. This side effect may be due to p... |
PMC11111944 | core_pubmed_pmc | Improving prediction of tacrolimus concentration using a combination of population pharmacokinetic modeling and machine learning in chinese renal transplant recipients | Improving prediction of tacrolimus concentration using a combination of population pharmacokinetic modeling and machine learning in chinese renal transplant recipients Abstract Abstract Aims The population pharmacokinetic (PPK) model-based machine learning (ML) approach offers a novel perspective on individual concentr... |
PMC8043511 | core_pubmed_pmc | Pharmacokinetics and Safety of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in HIV-infected Children With Severe Acute Malnutrition in Sub-Saharan Africa: IMPAACT Protocol P1092 | Pharmacokinetics and Safety of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in HIV-infected Children With Severe Acute Malnutrition in Sub-Saharan Africa: IMPAACT Protocol P1092 Abstract Background: Severe acute malnutrition (SAM) may alter the pharmacokinetics (PK), efficacy, and safety of antiretroviral therapy. T... |
PMC12468695 | core_pubmed_pmc | Revisiting Curcumin in Cancer Therapy: Recent Insights into Molecular Mechanisms, Nanoformulations, and Synergistic Combinations | Revisiting Curcumin in Cancer Therapy: Recent Insights into Molecular Mechanisms, Nanoformulations, and Synergistic Combinations Abstract Curcumin has been extensively investigated as an anticancer agent, yet its clinical application remains constrained by low bioavailability, incomplete mechanistic understanding, and ... |
PMC8213419 | core_pubmed_pmc | End‐to‐end application of model‐informed drug development for ertugliflozin, a novel sodium‐glucose cotransporter 2 inhibitor | End‐to‐end application of model‐informed drug development for ertugliflozin, a novel sodium‐glucose cotransporter 2 inhibitor Abstract Abstract Model‐informed drug development (MIDD) is critical in all stages of the drug‐development process and almost all regulatory submissions for new agents incorporate some form of m... |
PMC12141788 | core_pubmed_pmc | Disease Progression Modeling of Estimated Glomerular Filtration Rate (eGFR): A Pharmacometrics Approach | Disease Progression Modeling of Estimated Glomerular Filtration Rate (eGFR): A Pharmacometrics Approach Abstract ABSTRACT Background Estimated glomerular filtration rate (eGFR) is a key clinical marker for assessing kidney complications in type 2 diabetes mellitus (T2DM). This study aimed to develop and validate a dise... |
PMC3825860 | core_pubmed_pmc | Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract | Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract Abstract Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro . However, previous studies have focused on the pharmacokinetics of a ... |
PMC10433341 | core_pubmed_pmc | Targeting Staphylococcal Cell–Wall Biosynthesis Protein FemX Through Steered Molecular Dynamics and Drug-Repurposing Approach | Targeting Staphylococcal Cell–Wall Biosynthesis Protein FemX Through Steered Molecular Dynamics and Drug-Repurposing Approach Abstract Staphylococcus aureus -mediated infection is a serious threat in this antimicrobial-resistant world. S. aureus has become a “superbug” by challenging conventional as well as modern trea... |
PMC9386138 | core_pubmed_pmc | Association between CES1 rs2244613 and the pharmacokinetics and safety of dabigatran: Meta-analysis and quantitative trait loci analysis | Association between CES1 rs2244613 and the pharmacokinetics and safety of dabigatran: Meta-analysis and quantitative trait loci analysis Abstract Abstract Objective To date, the influence of the carboxylesterase 1 ( CES1 ) rs2244613 genotype on the pharmacokinetics (PKs) and safety of dabigatran remains controversial. ... |
PMC3942304 | core_pubmed_pmc | Long-term efficacy and safety of iloperidone: an update | Long-term efficacy and safety of iloperidone: an update Abstract Schizophrenia is a devastating neuropsychiatric disease with a worldwide prevalence of approximately 0.5%–1%. Since many patients do not achieve adequate symptom relief from available agents, alternate pharmacotherapeutic approaches are needed. In this co... |
PMC12916015 | core_pubmed_pmc | Informing Dose for Pediatric Rare Diseases—A Survey of Recent Orphan Drugs Approvals | Informing Dose for Pediatric Rare Diseases—A Survey of Recent Orphan Drugs Approvals Abstract ABSTRACT Collectively, pediatric rare diseases affect millions of children worldwide. Yet, treatment options are limited. Dose selection presents unique challenges in pediatric rare disease drug development. Traditional dose‐f... |
PMC10458293 | core_pubmed_pmc | Novel nasal niosomes loaded with lacosamide and coated with chitosan: A possible pathway to target the brain to control partial-onset seizures | Novel nasal niosomes loaded with lacosamide and coated with chitosan: A possible pathway to target the brain to control partial-onset seizures Abstract Abstract This work aimed to develop and produce lacosamide-loaded niosomes coated with chitosan (LCA-CTS-NSM) using a thin-film hydration method and the Box-Behnken des... |
PMC11364570 | core_pubmed_pmc | Interleukin-1α inhibitor bermekimab in patients with atopic dermatitis: randomized and nonrandomized studies | Interleukin-1α inhibitor bermekimab in patients with atopic dermatitis: randomized and nonrandomized studies Abstract Bermekimab is a human-derived recombinant monoclonal antibody that exhibits immunoregulatory activity by specifically blocking interleukin-1α activity. Four phase 2 studies evaluated efficacy and safety... |
PMC5006244 | core_pubmed_pmc | Sobol Sensitivity Analysis: A Tool to Guide the Development and Evaluation of Systems Pharmacology Models | Sobol Sensitivity Analysis: A Tool to Guide the Development and Evaluation of Systems Pharmacology Models Abstract Abstract A systems pharmacology model typically integrates pharmacokinetic, biochemical network, and systems biology concepts into a unifying approach. It typically consists of a large number of parameters... |
PMC11578127 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of long‐acting extended‐release naltrexone in pregnant women with opioid use disorder | Physiologically based pharmacokinetic modeling of long‐acting extended‐release naltrexone in pregnant women with opioid use disorder Abstract Abstract Opioid use disorders (OUD) are a major issue in the U.S. Current treatments for pregnant women, like methadone and buprenorphine require daily dosing and have adverse ef... |
PMC6619336 | core_pubmed_pmc | An Open‐Label, Single‐Dose, Human Mass Balance Study of Amenamevir in Healthy Male Adults | An Open‐Label, Single‐Dose, Human Mass Balance Study of Amenamevir in Healthy Male Adults Abstract Abstract Amenamevir is an inhibitor of the helicase‐primase enzyme complex developed for the treatment of varicella zoster virus. This mass balance study investigated the absorption, metabolism, and excretion of a single ... |
PMC7012096 | core_pubmed_pmc | Combining antimalarial drugs and vaccine for malaria elimination campaigns: a randomized safety and immunogenicity trial of RTS,S/AS01 administered with dihydroartemisinin, piperaquine, and primaquine in healthy Thai adult volunteers | Combining antimalarial drugs and vaccine for malaria elimination campaigns: a randomized safety and immunogenicity trial of RTS,S/AS01 administered with dihydroartemisinin, piperaquine, and primaquine in healthy Thai adult volunteers Abstract ABSTRACT Introduction : RTS,S/AS01 is currently the most advanced malaria vac... |
PMC4026623 | core_pubmed_pmc | Abuse Potential of Intravenous Oxycodone/Naloxone Solution in Nondependent Recreational Drug Users | Abuse Potential of Intravenous Oxycodone/Naloxone Solution in Nondependent Recreational Drug Users Abstract Abstract Background and Objective Abuse of opioid analgesics has become a public health issue. Some opioid abusers use intravenous administration to increase the magnitude of positive reinforcing effects. Intrave... |
PMC9795990 | core_pubmed_pmc | Optimal dosing of enoxaparin in overweight and obese children | Optimal dosing of enoxaparin in overweight and obese children Abstract Abstract Aim Current enoxaparin dosing guidelines in children are based on total body weight. This is potentially inappropriate in obese children as it may overestimate the drug clearance. Current evidence suggests that obese children may require lo... |
PMC10382785 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of azithromycin in severe malaria bacterial co-infection in African children (TABS-PKPD): a protocol for a Phase II randomised controlled trial | Pharmacokinetics and pharmacodynamics of azithromycin in severe malaria bacterial co-infection in African children (TABS-PKPD): a protocol for a Phase II randomised controlled trial Abstract Abstract Background: African children with severe malaria are susceptible to Gram-negative bacterial co-infection, largely non-ty... |
PMC6544081 | core_pubmed_pmc | A Dose Escalation Study of Trientine Plus Carboplatin and Pegylated Liposomal Doxorubicin in Women With a First Relapse of Epithelial Ovarian, Tubal, and Peritoneal Cancer Within 12 Months After Platinum-Based Chemotherapy | A Dose Escalation Study of Trientine Plus Carboplatin and Pegylated Liposomal Doxorubicin in Women With a First Relapse of Epithelial Ovarian, Tubal, and Peritoneal Cancer Within 12 Months After Platinum-Based Chemotherapy Abstract Abstract Background: Epithelial ovarian cancer (EOC) is the leading cause of gynecologic... |
PMC11582170 | core_pubmed_pmc | Obesity-related drug transporter expression alterations in human liver and kidneys | Obesity-related drug transporter expression alterations in human liver and kidneys Abstract Background Pathophysiological changes associated with obesity might impact various drug pharmacokinetics (PK) parameters. The liver and kidneys are the primary organs involved in drug clearance, and the function of hepatic and r... |
PMC8301552 | core_pubmed_pmc | Pharmacokinetics and tolerability of apremilast in healthy Korean adult men | Pharmacokinetics and tolerability of apremilast in healthy Korean adult men Abstract Abstract We performed a two‐part study to evaluate the pharmacokinetics, safety, and tolerability of oral apremilast, a phosphodiesterase 4 inhibitor indicated for the treatment of psoriasis, in healthy Korean adult men. In part 1, the... |
PMC10808627 | core_pubmed_pmc | Phase 2 study of ibrutinib plus venetoclax in Japanese patients with relapsed/refractory mantle cell lymphoma | Phase 2 study of ibrutinib plus venetoclax in Japanese patients with relapsed/refractory mantle cell lymphoma Abstract Background Despite high response rates to initial therapy, most patients with mantle cell lymphoma (MCL) experience relapsed or refractory (R/R) disease. Here, we report the efficacy, safety, and pharm... |
PMC9929485 | core_pubmed_pmc | Effect of the pseudomonas metabolites HQNO on the Toxoplasma gondii RH strain in vitro and in vivo | Effect of the pseudomonas metabolites HQNO on the Toxoplasma gondii RH strain in vitro and in vivo Abstract Toxoplasmosis is a widespread disease in humans and animals. Currently, toxoplasmosis chemotherapy options are limited due to severe side effects. There is an urgent need to develop new drugs with better efficacy... |
PMC10090777 | core_pubmed_pmc | Effect of sainfoin ( Onobrychis viciifolia ) on cyathostomin eggs excretion, larval development, larval community structure and efficacy of ivermectin treatment in horses | Effect of sainfoin ( Onobrychis viciifolia ) on cyathostomin eggs excretion, larval development, larval community structure and efficacy of ivermectin treatment in horses Abstract Alternative strategies to chemical anthelmintics are needed for the sustainable control of equine strongylids. Bioactive forages like sainfo... |
PMC6747466 | core_pubmed_pmc | An Update on Pharmacological Potential of Boswellic Acids against Chronic Diseases | An Update on Pharmacological Potential of Boswellic Acids against Chronic Diseases Abstract Natural compounds, in recent years, have attracted significant attention for their use in the prevention and treatment of diverse chronic diseases as they are devoid of major toxicities. Boswellic acid (BA), a series of pentacyc... |
PMC4970212 | core_pubmed_pmc | Effects and synergy of feed ingredients on canine neoplastic cell proliferation | Effects and synergy of feed ingredients on canine neoplastic cell proliferation Abstract Abstract Background Adjunctive use of nutraceuticals in human cancer has shown promise, but little work has been done in canine neoplasia. Previous human research has shown that polyphenols and carotenoids can target multiple pathw... |
PMC8452805 | core_pubmed_pmc | Concentrations and pharmacokinetic parameters of MRI and SPECT hepatobiliary agents in rat liver compartments | Concentrations and pharmacokinetic parameters of MRI and SPECT hepatobiliary agents in rat liver compartments Abstract Abstract Background In hepatobiliary imaging, systems detect the total amount of agents originating from extracellular space, bile canaliculi, and hepatocytes. They add in situ concentration of each co... |
PMC6613017 | core_pubmed_pmc | Systems approach reveals photosensitivity and PER2 level as determinants of clock‐modulator efficacy | Systems approach reveals photosensitivity and PER2 level as determinants of clock‐modulator efficacy Abstract Abstract In mammals, the master circadian clock synchronizes daily rhythms of physiology and behavior with the day–night cycle. Failure of synchrony, which increases the risk for numerous chronic diseases, can ... |
PMC5216056 | core_pubmed_pmc | Cannabinoid CB 2 receptor ligand profiling reveals biased signalling and off-target activity | Cannabinoid CB 2 receptor ligand profiling reveals biased signalling and off-target activity Abstract Abstract The cannabinoid CB 2 receptor (CB 2 R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to... |
PMC8860597 | core_pubmed_pmc | Chirality matters: stereo-defined phosphorothioate linkages at the termini of small interfering RNAs improve pharmacology in vivo | Chirality matters: stereo-defined phosphorothioate linkages at the termini of small interfering RNAs improve pharmacology in vivo Abstract Abstract A critical challenge for the successful development of RNA interference-based therapeutics therapeutics has been the enhancement of their in vivo metabolic stability. In th... |
PMC11699081 | core_pubmed_pmc | Lower-intensity CPX-351 plus venetoclax induction for adults with newly diagnosed AML unfit for intensive chemotherapy | Lower-intensity CPX-351 plus venetoclax induction for adults with newly diagnosed AML unfit for intensive chemotherapy Abstract Key Points • Lower-intensity CPX-351 plus venetoclax was tolerated as induction therapy in adults with poor-risk AML unfit for intense chemotherapy. • Combination of lower-intensity CPX-351 pl... |
PMC12567279 | core_pubmed_pmc | Escitalopram Dose Optimization During Pregnancy: A PBPK Modeling Approach | Escitalopram Dose Optimization During Pregnancy: A PBPK Modeling Approach Abstract Abstract Background/Objectives : Escitalopram, a first-line antidepressant, is primarily metabolized by CYP2C19. Its pharmacokinetics are altered during pregnancy. This study aims to predict maternal and fetal exposure to escitalopram du... |
PMC7686198 | core_pubmed_pmc | Liver Injury with Ulipristal Acetate: Exploring the Underlying Pharmacological Basis | Liver Injury with Ulipristal Acetate: Exploring the Underlying Pharmacological Basis Abstract Abstract Introduction The European Medicines Agency has suspended the use of ulipristal acetate (UPA) in the treatment of uterine fibroids and is reassessing its association with a risk of liver injury. Objectives Our objectiv... |
PMC11396014 | core_pubmed_pmc | ORIC-101, a Glucocorticoid Receptor Antagonist, in Combination with Nab-Paclitaxel in Patients with Advanced Solid Tumors | ORIC-101, a Glucocorticoid Receptor Antagonist, in Combination with Nab-Paclitaxel in Patients with Advanced Solid Tumors Abstract Abstract Purpose: In preclinical models, glucocorticoid receptor (GR) signaling drives resistance to taxane chemotherapy in multiple solid tumors via upregulation of antiapoptotic pathways.... |
PMC9174522 | core_pubmed_pmc | Case Report: Safety and Efficacy of Enfortumab Vedotin in a Patient With Metastatic Urothelial Carcinoma Undergoing Peritoneal Dialysis | Case Report: Safety and Efficacy of Enfortumab Vedotin in a Patient With Metastatic Urothelial Carcinoma Undergoing Peritoneal Dialysis Abstract Abstract The clinical management of metastatic urothelial carcinoma has significantly evolved with the emergence of monoclonal antibodies and antibody-drug conjugates (ADCs). ... |
PMC3324422 | core_pubmed_pmc | Lopinavir/ritonavir significantly influences pharmacokinetic exposure of artemether/lumefantrine in HIV-infected Ugandan adults | Lopinavir/ritonavir significantly influences pharmacokinetic exposure of artemether/lumefantrine in HIV-infected Ugandan adults Abstract Background Treatment of HIV/malaria-coinfected patients with antiretroviral therapy (ART) and artemisinin-based combination therapy has potential for drug interactions. We investigate... |
PMC10037547 | core_pubmed_pmc | Diurnal Changes in Capecitabine Clock-Controlled Metabolism Enzymes Are Responsible for Its Pharmacokinetics in Male Mice | Diurnal Changes in Capecitabine Clock-Controlled Metabolism Enzymes Are Responsible for Its Pharmacokinetics in Male Mice Abstract The circadian timing system controls absorption, distribution, metabolism, and elimination processes of drug pharmacokinetics over a 24-h period. Exposure of target tissues to the active fo... |
PMC10488149 | core_pubmed_pmc | Interaction of Blenoxane and Congeners Bleomycins A2 and B2 with Human Plasma Proteins Using Circular Dichroism Spectroscopy | Interaction of Blenoxane and Congeners Bleomycins A2 and B2 with Human Plasma Proteins Using Circular Dichroism Spectroscopy Abstract Bleomycin is a glycopeptide congeners’ family of antitumor antibiotics employed for the treatment of several types of tumors such as squamous cell carcinomas and malignant lymphomas. The... |
PMC12666312 | core_pubmed_pmc | A First-in-Class mAb (BI-1607) Targeting FcγRIIB: Preclinical Data and First-in-Human Studies in Patients with HER2-Positive Advanced Solid Tumors | A First-in-Class mAb (BI-1607) Targeting FcγRIIB: Preclinical Data and First-in-Human Studies in Patients with HER2-Positive Advanced Solid Tumors Abstract Abstract Purpose: BI-1607 is a human mAb that specifically blocks FcγRIIB, the sole inhibitory Fc receptor and master regulator of humoral and innate immune homeost... |
PMC9748837 | core_pubmed_pmc | Low risk of the TMPRSS2 inhibitor camostat mesylate and its metabolite GBPA to act as perpetrators of drug-drug interactions | Low risk of the TMPRSS2 inhibitor camostat mesylate and its metabolite GBPA to act as perpetrators of drug-drug interactions Abstract Abstract Camostat mesylate, a potent inhibitor of the human transmembrane protease, serine 2 (TMPRSS2), is currently under investigation for its effectiveness in COVID-19 patients. For i... |
PMC9900004 | core_pubmed_pmc | Pharmacokinetics and biosafety evaluation of a veterinary drug florfenicol in rainbow trout, Oncorhynchus mykiss (Walbaum 1792) as a model cultivable fish species in temperate water | Pharmacokinetics and biosafety evaluation of a veterinary drug florfenicol in rainbow trout, Oncorhynchus mykiss (Walbaum 1792) as a model cultivable fish species in temperate water Abstract In two experimental trials; florfenicol pharmacokinetics following a single dose oral administration at 15 mg kg −1 fish body wei... |
PMC7646415 | core_pubmed_pmc | Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment | Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment Abstract Purpose Zolmitriptan (ZT) is a selective serotonin agonist that is used for the treatment of migraine. It belongs to BCS class III with high solubility and low... |
PMC10989545 | core_pubmed_pmc | A validated liquid chromatography‐tandem mass spectroscopy method for the quantification of tolinapant in human plasma | A validated liquid chromatography‐tandem mass spectroscopy method for the quantification of tolinapant in human plasma Abstract Abstract Tolinapant (ASTX660), a pan‐selective inhibitor of apoptosis protein antagonist with dual cIAP/XIAP activity, was identified as a clinical candidate in preclinical efficacy, pharmacok... |
PMC10555494 | core_pubmed_pmc | Determination of Tenacissoside G, Tenacissoside H, and Tenacissoside I in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics | Determination of Tenacissoside G, Tenacissoside H, and Tenacissoside I in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics Abstract An ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) method was developed for the determination of tenacissoside G, tenacissoside H, and tenacissoside I in r... |
PMC12478601 | core_pubmed_pmc | Development and Validation of an HPLC-MS/MS Method for Determining I-BET151 in Rat Plasma and Its application to Pharmacokinetic Studies | Development and Validation of an HPLC-MS/MS Method for Determining I-BET151 in Rat Plasma and Its application to Pharmacokinetic Studies Abstract Abstract Propose A bromodomain and extra-terminal domain inhibitor (I-BET151) is effective in treating chronic graft-versus-host disease and has been extensively studied in r... |
PMC5873441 | core_pubmed_pmc | Pharmacokinetics and tolerability of semaglutide in people with hepatic impairment | Pharmacokinetics and tolerability of semaglutide in people with hepatic impairment Abstract Abstract Aims To investigate whether the pharmacokinetic characteristics of semaglutide were altered in people with hepatic impairment, assessed using Child–Pugh criteria, vs those with normal hepatic function. Methods In this m... |
PMC6084333 | core_pubmed_pmc | Evaluation of a 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation: A Randomized, 3‐Way Crossover Pharmacokinetic and Safety Study in Healthy Volunteers | Evaluation of a 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation: A Randomized, 3‐Way Crossover Pharmacokinetic and Safety Study in Healthy Volunteers Abstract Abstract Acetaminophen (paracetamol) is a first‐line treatment for mild and moderate pain. A twice‐daily sustained‐release (SR) formulation may... |
PMC12583746 | core_pubmed_pmc | OSU-ERβ-12: a promising pre-clinical candidate selective estrogen receptor beta agonist | OSU-ERβ-12: a promising pre-clinical candidate selective estrogen receptor beta agonist Abstract Estrogen receptor beta (ERβ) is a favorable therapeutic target for mediating inflammation, attenuating fibrosis, and treating cancer. However, selectively targeting ERβ over estrogen receptor alpha (ERα) has been a longstan... |
PMC7643797 | core_pubmed_pmc | Randomized Controlled Crossover Trials of the Pharmacokinetics of PRC-063, a Novel Multilayer Extended-Release Formulation of Methylphenidate, in Healthy Adults | Randomized Controlled Crossover Trials of the Pharmacokinetics of PRC-063, a Novel Multilayer Extended-Release Formulation of Methylphenidate, in Healthy Adults Abstract Supplemental digital content is available in the text. Abstract Purpose/Background PRC-063 is a once-daily, extended-release oral formulation of methy... |
PMC8253124 | core_pubmed_pmc | High drug payload curcumin nanosuspensions stabilized by mPEG-DSPE and SPC: in vitro and in vivo evaluation | High drug payload curcumin nanosuspensions stabilized by mPEG-DSPE and SPC: in vitro and in vivo evaluation Abstract Abstract Context : Curcumin (CUR) is a promising drug candidate based on its broad bioactivities and good antitumor effect, but the application of CUR is potentially restricted because of its poor solubi... |
PMC12085449 | core_pubmed_pmc | Amylin: From Mode of Action to Future Clinical Potential in Diabetes and Obesity | Amylin: From Mode of Action to Future Clinical Potential in Diabetes and Obesity Abstract Abstract Precision diabetology is increasingly becoming diabetes phenotype-driven, whereby the specific hormonal imbalances involved are taken into consideration. Concomitantly, body weight-favorable therapeutic approaches are bei... |
PMC3528047 | core_pubmed_pmc | Simultaneous Determination of Atorvastatin and Aspirin in Human Plasma by LC–MS/MS: Its Pharmacokinetic Application | Simultaneous Determination of Atorvastatin and Aspirin in Human Plasma by LC–MS/MS: Its Pharmacokinetic Application Abstract Abstract A simple, rapid, and sensitive liquid chromatography tandem mass spectro-metric (LC–MS/MS) assay method has been developed and fully validated for the simultaneous quantification of ator... |
PMC8585827 | core_pubmed_pmc | Ultra Rapid Lispro (URLi) Accelerates Insulin Lispro Absorption and Insulin Action vs Humalog ® Consistently Across Study Populations: A Pooled Analysis of Pharmacokinetic and Glucodynamic Data | Ultra Rapid Lispro (URLi) Accelerates Insulin Lispro Absorption and Insulin Action vs Humalog ® Consistently Across Study Populations: A Pooled Analysis of Pharmacokinetic and Glucodynamic Data Abstract Background and Objective Ultra rapid lispro (URLi) is a novel insulin lispro formulation developed to more closely ma... |
PMC12146338 | core_pubmed_pmc | Bioanalytical assay for the quantification of rucaparib in rat plasma using UPLC-MS/MS: development, and validation for interaction with myricetin | Bioanalytical assay for the quantification of rucaparib in rat plasma using UPLC-MS/MS: development, and validation for interaction with myricetin Abstract Rucaparib is used to treat ovarian cancer patients with BRCA gene mutations. Myricetin, a flavonol that strongly inhibits CYP450, is widely found in natural plants ... |
PMC7279318 | core_pubmed_pmc | Computational Simulations to Guide Enzyme-Mediated Prodrug Activation | Computational Simulations to Guide Enzyme-Mediated Prodrug Activation Abstract Abstract Prodrugs are designed to improve pharmaceutical/biopharmaceutical characteristics, pharmacokinetic/pharmacodynamic properties, site-specificity, and more. A crucial step in successful prodrug is its activation, which releases the ac... |
PMC12706722 | core_pubmed_pmc | Mass spectrometry in ocular drug research | Mass spectrometry in ocular drug research Abstract Abstract Mass spectrometry (MS) has been proven as an excellent tool in ocular drug research allowing analyzes from small samples and low concentrations. This review begins with a short introduction to eye physiology and ocular pharmacokinetics and the relevance of adv... |
PMC12645700 | core_pubmed_pmc | Eschweilenol C and subfractions from Terminalia plants disrupt haemoglobin metabolism, inhibiting Plasmodium falciparum growth at rings and trophozoite stages | Eschweilenol C and subfractions from Terminalia plants disrupt haemoglobin metabolism, inhibiting Plasmodium falciparum growth at rings and trophozoite stages Abstract Background The rising prevalence of artemisinin-resistant malaria parasites in Africa underscores the urgent demand for new and effective therapeutic op... |
PMC11646947 | core_pubmed_pmc | Immunogenicity dynamics and covariate effects after satralizumab administration predicted with a hidden Markov model | Immunogenicity dynamics and covariate effects after satralizumab administration predicted with a hidden Markov model Abstract Abstract Immunogenicity is the propensity of a therapeutic protein to generate an immune response to itself. While reporting of antidrug antibodies (ADAs) is increasing, model‐based analysis of ... |
PMC9943962 | core_pubmed_pmc | Pharmacokinetics and Dosing Regimens of Direct Oral Anticoagulants in Morbidly Obese Patients: An Updated Literature Review | Pharmacokinetics and Dosing Regimens of Direct Oral Anticoagulants in Morbidly Obese Patients: An Updated Literature Review Abstract Data on the impact of morbid obesity (body mass index [BMI] ≥ 40 kg/m 2 ) on the pharmacokinetics (PK), pharmacodynamics (PD) of direct oral anticoagulants (DOACs) are relatively limited,... |
PMC8875967 | core_pubmed_pmc | The Prevalence of Potential Drug-Drug Interactions in CKD-A Retrospective Observational Study of Cerrahpasa Nephrology Unit | The Prevalence of Potential Drug-Drug Interactions in CKD-A Retrospective Observational Study of Cerrahpasa Nephrology Unit Abstract Background and Objectives: Chronic kidney disease (CKD) is usually linked with polypharmacy and patients are invariably at risk of complex medication regimens. The present study was desig... |
PMC11171481 | core_pubmed_pmc | Differences in Metabolite Profiles of Dihydroberberine and Micellar Berberine in Caco-2 Cells and Humans—A Pilot Study | Differences in Metabolite Profiles of Dihydroberberine and Micellar Berberine in Caco-2 Cells and Humans—A Pilot Study Abstract Abstract We investigated the pharmacokinetic pathway of berberine and its metabolites in vitro, in Caco-2 cells, and in human participants following the administration of dihydroberberine (DHB... |
PMC11254985 | core_pubmed_pmc | Model-based comparison of subcutaneous versus sublingual apomorphine administration in the treatment of motor fluctuations in Parkinson’s disease | Model-based comparison of subcutaneous versus sublingual apomorphine administration in the treatment of motor fluctuations in Parkinson’s disease Abstract The objective of this study was to compare the effectiveness of subcutaneous (SC) and sublingual (SL) formulations of apomorphine for the treatment of motor fluctuat... |
PMC12586667 | core_pubmed_pmc | Genome edited intestine liver on a chip system for integrated intestinal hepatic drug absorption and metabolism evaluation | Genome edited intestine liver on a chip system for integrated intestinal hepatic drug absorption and metabolism evaluation Abstract Evaluation of the intestinal absorption and hepatic metabolism is crucial to the development of orally administered drugs. Previous evaluation systems have assessed intestinal epithelial c... |
PMC11439818 | core_pubmed_pmc | Study on pharmacokinetic and tissue distribution of hyperin, astragalin, kaempferol-3-O-β-D-glucuronide from rats with multiple administrations of Semen Cuscutae processed with salt solution with effect of treating recurrent spontaneous abortion | Study on pharmacokinetic and tissue distribution of hyperin, astragalin, kaempferol-3-O-β-D-glucuronide from rats with multiple administrations of Semen Cuscutae processed with salt solution with effect of treating recurrent spontaneous abortion Abstract Abstract Introduction Semen Cuscutae is a traditional Chinese med... |
PMC11125168 | core_pubmed_pmc | Evaluation of Silybin Nanoparticles against Liver Damage in Murine Schistosomiasis mansoni Infection | Evaluation of Silybin Nanoparticles against Liver Damage in Murine Schistosomiasis mansoni Infection Abstract Abstract Silybin (SIB) is a hepatoprotective drug known for its poor oral bioavailability, attributed to its classification as a class IV drug with significant metabolism during the first-pass effect. This stud... |
PMC7998456 | core_pubmed_pmc | Accelerating Development of Benziamidazole-Class Proton Pump Inhibitors: A Mechanism-Based PK/PD Model to Optimize Study Design with Ilaprazole as a Case Drug | Accelerating Development of Benziamidazole-Class Proton Pump Inhibitors: A Mechanism-Based PK/PD Model to Optimize Study Design with Ilaprazole as a Case Drug Abstract Abstract Proton pump inhibitors (PPIs) are the mainstay for treatment of acid-related diseases. This study developed a mechanism-based pharmacokinetic (... |
PMC12845235 | core_pubmed_pmc | Phosphatidylinositol-3-Kinase (PI3K) and Histone Deacetylase (HDAC) Multitarget Inhibitors: An Update on Clinical and Preclinical Candidates | Phosphatidylinositol-3-Kinase (PI3K) and Histone Deacetylase (HDAC) Multitarget Inhibitors: An Update on Clinical and Preclinical Candidates Abstract Phosphatidylinositol-3-kinases (PI3Ks) constitute an important validated therapeutic class involved in crucial cellular processes, and their dysregulation is associated w... |
PMC6657216 | core_pubmed_pmc | Defining the Contribution of CYP1A1 and CYP1A2 to Drug Metabolism Using Humanized CYP1A1/1A2 and Cyp1a1/Cyp1a2 Knockout Mice | Defining the Contribution of CYP1A1 and CYP1A2 to Drug Metabolism Using Humanized CYP1A1/1A2 and Cyp1a1/Cyp1a2 Knockout Mice Abstract Abstract Cytochrome P450s CYP1A1 and CYP1A2 can metabolize a broad range of foreign compounds and drugs. However, these enzymes have significantly overlapping substrate specificities. To... |
PMC9611727 | core_pubmed_pmc | Optimization of a Novel Mandelamide-Derived Pyrrolopyrimidine Series of PERK Inhibitors | Optimization of a Novel Mandelamide-Derived Pyrrolopyrimidine Series of PERK Inhibitors Abstract Abstract The protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is one of three endoplasmic reticulum (ER) transmembrane sensors of the unfolded protein response (UPR) responsible for regulating protein synthes... |
PMC8052134 | core_pubmed_pmc | Development of a Population Pharmacokinetic Model for Cyclosporine from Therapeutic Drug Monitoring Data | Development of a Population Pharmacokinetic Model for Cyclosporine from Therapeutic Drug Monitoring Data Abstract Abstract Aim To develop a population pharmacokinetic model for Uruguayan patients under treatment with cyclosporine (CsA) that can be applied to TDM. Patients and Methods . A total of 53 patients under trea... |
PMC10070753 | core_pubmed_pmc | Population pharmacokinetics of nalbuphine in patients undergoing general anesthesia surgery | Population pharmacokinetics of nalbuphine in patients undergoing general anesthesia surgery Abstract Abstract Purpose: The aim of this study was to build a population pharmacokinetics (PopPK) model of nalbuphine and to estimate the suitability of bodyweight or fixed dosage regimen. Method: Adult patients who were under... |
PMC6338786 | core_pubmed_pmc | Detection of anthracycline-induced cardiotoxicity using perfusion-corrected 99m Tc sestamibi SPECT | Detection of anthracycline-induced cardiotoxicity using perfusion-corrected 99m Tc sestamibi SPECT Abstract Abstract By the time cardiotoxicity-associated cardiac dysfunction is detectable by echocardiography it is often beyond meaningful intervention. 99m Tc-sestamibi is used clinically to image cardiac perfusion by s... |
PMC7894401 | core_pubmed_pmc | Physiologically‐Based Pharmacokinetic Modeling of the Drug–Drug Interaction of the UGT Substrate Ertugliflozin Following Co‐Administration with the UGT Inhibitor Mefenamic Acid | Physiologically‐Based Pharmacokinetic Modeling of the Drug–Drug Interaction of the UGT Substrate Ertugliflozin Following Co‐Administration with the UGT Inhibitor Mefenamic Acid Abstract Abstract The sodium‐glucose cotransporter 2 inhibitor ertugliflozin is metabolized by the uridine 5'‐diphospho‐glucuronosyltransferase... |
PMC9978179 | core_pubmed_pmc | Predicting treatment response to vancomycin using bacterial DNA load as a pharmacodynamic marker in premature and very low birth weight neonates: A population PKPD study | Predicting treatment response to vancomycin using bacterial DNA load as a pharmacodynamic marker in premature and very low birth weight neonates: A population PKPD study Abstract Abstract Background: While positive blood cultures are the gold standard for late-onset sepsis (LOS) diagnosis in premature and very low birt... |
PMC7355699 | core_pubmed_pmc | The Use of Capsule Endoscopy to Determine Tablet Disintegration In Vivo | The Use of Capsule Endoscopy to Determine Tablet Disintegration In Vivo Abstract The preferred delivery route for drugs targeted for systemic effect is by oral administration. Following oral administration, a solid dosage form must disintegrate and the drug dissolve, thereafter permeating the intestinal mucosa. Several... |
PMC12868800 | core_pubmed_pmc | Micro pharmacokinetics-pharmacodynamics monitoring of anti-Parkinson’s disease drugs using a microphysiological BBB-brain organ-on-a-chip | Micro pharmacokinetics-pharmacodynamics monitoring of anti-Parkinson’s disease drugs using a microphysiological BBB-brain organ-on-a-chip Abstract Establishing robust pharmacokinetics-pharmacodynamics (PK-PD) correlations remains a major challenge owing to high selectivity and low permeability of the blood-brain barrie... |
PMC8431978 | core_pubmed_pmc | Efficacy, Toxicity, and Pharmacokinetics of Intra-Arterial Chemotherapy Versus Intravenous Chemotherapy for Retinoblastoma in Animal Models and Patients | Efficacy, Toxicity, and Pharmacokinetics of Intra-Arterial Chemotherapy Versus Intravenous Chemotherapy for Retinoblastoma in Animal Models and Patients Abstract Purpose Through controlled comparative rabbit experiments and parallel patient studies, our purpose was to understand mechanisms underlying differences in eff... |
PMC6520319 | core_pubmed_pmc | A Multi-Center, Open-Label, Pharmacokinetic Drug Interaction Study of Erenumab and a Combined Oral Contraceptive in Healthy Females | A Multi-Center, Open-Label, Pharmacokinetic Drug Interaction Study of Erenumab and a Combined Oral Contraceptive in Healthy Females Abstract Background Erenumab is a human anti-calcitonin gene-related peptide monoclonal antibody developed for migraine prevention. Migraine predominately affects women of childbearing age... |
PMC9789074 | core_pubmed_pmc | Effects of rifampin on the pharmacokinetics and pharmacodynamics of milvexian, a potent, selective, oral small molecule factor XIa inhibitor | Effects of rifampin on the pharmacokinetics and pharmacodynamics of milvexian, a potent, selective, oral small molecule factor XIa inhibitor Abstract Abstract Milvexian (BMS-986177/JNJ-70033093) is a potent, oral small molecule that inhibits the active form of factor XI with high affinity and selectivity. This study as... |
PMC5111190 | core_pubmed_pmc | Changes in ceftriaxone pharmacokinetics/pharmacodynamics during the early phase of sepsis: a prospective, experimental study in the rat | Changes in ceftriaxone pharmacokinetics/pharmacodynamics during the early phase of sepsis: a prospective, experimental study in the rat Abstract Background Sepsis is characterized by the loss of the perm-selectivity properties of the glomerular filtration barrier (GFB) with consequent albuminuria. We examined whether t... |
PMC11667563 | core_pubmed_pmc | Development and optimization of dapagliflozin oral nano-bilosomes using response surface method: in vitro evaluation, in vivo evaluation | Development and optimization of dapagliflozin oral nano-bilosomes using response surface method: in vitro evaluation, in vivo evaluation Abstract Abstract In treating type 2 diabetes, avoiding glucose reabsorption (glucotoxicity) and managing hyperglycemia are also important. A metabolic condition known as diabetes (ty... |
PMC12735883 | core_pubmed_pmc | Curcumin and Tetrahydrocurcumin as Multi-Organ Modulators of the Adipose Tissue–Gut–Liver Axis: Mechanistic Insights, Therapeutic Potential, and Translational Challenges | Curcumin and Tetrahydrocurcumin as Multi-Organ Modulators of the Adipose Tissue–Gut–Liver Axis: Mechanistic Insights, Therapeutic Potential, and Translational Challenges Abstract Obesity and its related disorders, such as type 2 diabetes mellitus (T2DM) and metabolic dysfunction-associated steatotic liver disease (MASL... |
PMC4031103 | core_pubmed_pmc | Population Pharmacokinetic Study of Benznidazole in Pediatric Chagas Disease Suggests Efficacy despite Lower Plasma Concentrations than in Adults | Population Pharmacokinetic Study of Benznidazole in Pediatric Chagas Disease Suggests Efficacy despite Lower Plasma Concentrations than in Adults Abstract Abstract Introduction Chagas disease, caused by the parasite Trypanosoma cruzi , can lead to long term cardiac morbidity. Treatment of children with benznidazole is ... |
PMC12422617 | core_pubmed_pmc | Surgical approaches to inner ear therapies | Surgical approaches to inner ear therapies Abstract Purpose of review Drug delivery to the cochlea has been hampered by the very mechanisms that exist to protect its delicate neurosensory epithelium from pathogens. The blood-brain barrier restricts the distribution of systemic therapies, while local administration is c... |
PMC10747343 | core_pubmed_pmc | Physiologically Based Biopharmaceutics Model (PBBM) of Minimally Absorbed Locally Acting Drugs in the Gastrointestinal Tract—Case Study: Tenapanor | Physiologically Based Biopharmaceutics Model (PBBM) of Minimally Absorbed Locally Acting Drugs in the Gastrointestinal Tract—Case Study: Tenapanor Abstract Abstract A physiologically based biopharmaceutics model (PBBM) was developed to predict stool and urine sodium content in response to tenapanor administration in he... |
PMC3637024 | core_pubmed_pmc | Electroencephalogram-based pharmacodynamic measures: a review | Electroencephalogram-based pharmacodynamic measures: a review Abstract Pharmacokinetics and pharmacodynamics can provide a useful modeling framework for predicting drug activity and can serve as a basis for dose optimization. Determining a suitable biomarker or surrogate measure of drug effect for pharmacodynamic model... |
PMC11420244 | core_pubmed_pmc | Evaluation of the effect of modafinil on the pharmacokinetics of encorafenib and binimetinib in patients with BRAF V600-mutant advanced solid tumors | Evaluation of the effect of modafinil on the pharmacokinetics of encorafenib and binimetinib in patients with BRAF V600-mutant advanced solid tumors Abstract Abstract Background A clinical drug-drug interaction (DDI) study was designed to evaluate the effect of multiple doses of modafinil, a moderate CYP3A4 inducer at ... |
PMC9883540 | core_pubmed_pmc | Study on pharmacokinetic interactions between SHR2554 and itraconazole in healthy subjects: A single‐center, open‐label phase I trial | Study on pharmacokinetic interactions between SHR2554 and itraconazole in healthy subjects: A single‐center, open‐label phase I trial Abstract Abstract Background SHR2554, a novel oral Enhancer of Zeste Homolog 2 inhibitor, shows broad‐spectrum anti‐tumor efficacy in preclinical studies. As SHR2554 is mainly metabolize... |
PMC6091483 | core_pubmed_pmc | A complex micellar system co-delivering curcumin with doxorubicin against cardiotoxicity and tumor growth | A complex micellar system co-delivering curcumin with doxorubicin against cardiotoxicity and tumor growth Abstract Abstract Background Dose-dependent irreversible cardiac toxicity of doxorubicin (DOX) becomes a major obstacle for the clinical use. Nowadays much attention is being paid to combination therapy with DOX an... |
PMC12166629 | core_pubmed_pmc | Enhancing cannabinoid bioavailability: a crossover study comparing a novel self-nanoemulsifying drug delivery system and a commercial oil-based formulation | Enhancing cannabinoid bioavailability: a crossover study comparing a novel self-nanoemulsifying drug delivery system and a commercial oil-based formulation Abstract Purpose The oral bioavailability of cannabinoids is limited due to extensive first-pass metabolism, reducing their therapeutic efficacy. This study aimed t... |
PMC6443786 | core_pubmed_pmc | 3D-QSAR, Docking, ADME/Tox studies on Flavone analogs reveal anticancer activity through Tankyrase inhibition | 3D-QSAR, Docking, ADME/Tox studies on Flavone analogs reveal anticancer activity through Tankyrase inhibition Abstract Abstract Flavones are known as an inhibitor of tankyrase, a potential drug target of cancer. We here expedited the use of different computational approaches and presented a fast, easy, cost-effective a... |
PMC10787297 | core_pubmed_pmc | Pharmacokinetics and tissue distribution of vigabatrin enantiomers in rats | Pharmacokinetics and tissue distribution of vigabatrin enantiomers in rats Abstract Purpose To investigate the pharmacokinetics and tissue distribution of VGB racemate and its single enantiomers, and explore the potential of clinic development for single enantiomer S-VGB. Methods In the pharmacokinetics study, male Spr... |
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