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PMC8249281 | core_pubmed_pmc | Pharmacokinetics and Drug–Drug Interactions of Long-Acting Intramuscular Cabotegravir and Rilpivirine | Pharmacokinetics and Drug–Drug Interactions of Long-Acting Intramuscular Cabotegravir and Rilpivirine Abstract Combined antiretroviral treatments have significantly improved the morbidity and mortality related to HIV infection, thus transforming HIV infection into a chronic disease; however, the efficacy of antiretrovi... |
PMC5703966 | core_pubmed_pmc | Systemic clearance and brain distribution of carbazole-based cyanine compounds as Alzheimer’s disease drug candidates | Systemic clearance and brain distribution of carbazole-based cyanine compounds as Alzheimer’s disease drug candidates Abstract SLM and SLOH, two analogues of carbazole-based cyanine compounds, have been shown to inhibit β-amyloid peptide aggregation in vitro and in Alzheimer’s disease model mice, which could be potenti... |
PMC11651071 | core_pubmed_pmc | Development of the Curcumin Analog CA7 Liposome and Its Evaluation for Efficacy Against Cervical Cancer in vitro and in vivo | Development of the Curcumin Analog CA7 Liposome and Its Evaluation for Efficacy Against Cervical Cancer in vitro and in vivo Abstract Abstract Objective The objective of this study was to develop liposomes (LP) containing a curcumin (CU) analog CA7 to enhance its pharmacokinetic profile and anti-cervical cancer (CC) ef... |
PMC9729727 | core_pubmed_pmc | The effect of food on the pharmacokinetics of WXFL10203614, a potential selective JAK1 inhibitor, in healthy Chinese subjects | The effect of food on the pharmacokinetics of WXFL10203614, a potential selective JAK1 inhibitor, in healthy Chinese subjects Abstract Objective: This study was performed to investigate the effect of food on the pharmacokinetics (PK) of WXFL10203614 in healthy Chinese subjects. Methods: This was a randomized, open-labe... |
PMC3586101 | core_pubmed_pmc | Evaluation of the Pharmacokinetic Interaction between Lesogaberan (AZD3355) and Esomeprazole in Healthy Subjects | Evaluation of the Pharmacokinetic Interaction between Lesogaberan (AZD3355) and Esomeprazole in Healthy Subjects Abstract Background: Transient lower esophageal sphincter relaxations (TLESRs) have been identified as a primary cause of reflux events in patients with gastroesophageal reflux disease (GERD). GABAB receptor... |
PMC8960439 | core_pubmed_pmc | Transgenic Canola Oil Improved Blood Omega-3 Profiles: A Randomized, Placebo-Controlled Trial in Healthy Adults | Transgenic Canola Oil Improved Blood Omega-3 Profiles: A Randomized, Placebo-Controlled Trial in Healthy Adults Abstract Long-chain omega-3 polyunsaturated fatty acids (LC-ω3 PUFA), including eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), play key roles in physiological functions and disease prevention. Th... |
PMC11579209 | core_pubmed_pmc | Population pharmacokinetics and exposure–response relationships of maribavir in transplant recipients with cytomegalovirus infection | Population pharmacokinetics and exposure–response relationships of maribavir in transplant recipients with cytomegalovirus infection Abstract Maribavir is approved for management of post-transplant cytomegalovirus (CMV) infections refractory and/or resistant to CMV therapies at a dose of 400 mg twice daily (BID). Popul... |
PMC6817767 | core_pubmed_pmc | Dolutegravir And Lamivudine Combination For The Treatment Of HIV-1 Infection | Dolutegravir And Lamivudine Combination For The Treatment Of HIV-1 Infection Abstract Abstract There have been remarkable advances in drug development for the treatment of HIV-1 infection. From the co-formulation of combination antiretroviral therapy (cART) into single-tablet regimens to the development of long-acting ... |
PMC6885506 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 ( SLCO1B1 ) Drug–Drug–Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole | Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 ( SLCO1B1 ) Drug–Drug–Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole Abstract Abstract Background Drug–drug interactions (DDIs) and drug–gene interactio... |
PMC11649715 | core_pubmed_pmc | Pharmacokinetics of Omadacycline in Adults with Cystic Fibrosis | Pharmacokinetics of Omadacycline in Adults with Cystic Fibrosis Abstract Abstract Background Omadacycline offers a potential advancement in the management of infections in people with cystic fibrosis (CF) because of its spectrum of activity, intrapulmonary penetration, and oral bioavailability. A prospective single-dos... |
PMC11480974 | core_pubmed_pmc | Development of CD33-Targeted Dual Drug-Loaded Nanoparticles for the Treatment of Pediatric Acute Myeloid Leukemia | Development of CD33-Targeted Dual Drug-Loaded Nanoparticles for the Treatment of Pediatric Acute Myeloid Leukemia Abstract Abstract Paediatric acute myeloid leukemia (AML) is a heterogeneous hematological malignancy still heavily reliant on traditional chemotherapeutic approaches. Combination treatments have shown to b... |
PMC8843956 | core_pubmed_pmc | Reversible Complete Heart Block in a Pregnant Woman Related to Sertraline Treatment | Reversible Complete Heart Block in a Pregnant Woman Related to Sertraline Treatment Abstract Complete heart block (CHB) is a serious condition, usually affecting older patients. We report a case of CHB in a 31-year-old pregnant woman treated with sertraline in whom atrioventricular (AV) conduction normalized after disc... |
PMC12802081 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Oral TYK2 Inhibitor D‐2570 in Healthy Subjects: A First‐in‐Human Phase I Study | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Oral TYK2 Inhibitor D‐2570 in Healthy Subjects: A First‐in‐Human Phase I Study Abstract ABSTRACT D‐2570 selectively binds to the pseudokinase domain of tyrosine kinase 2, which mediates the downstream cytokine signaling pathways involved in immune regu... |
PMC9487926 | core_pubmed_pmc | Transdermal delivery of colchicine using dissolvable microneedle arrays for the treatment of acute gout in a rat model | Transdermal delivery of colchicine using dissolvable microneedle arrays for the treatment of acute gout in a rat model Abstract Abstract Colchicine (Col) is used to prevent and treat acute gout flare; however, its therapeutic use is strictly limited owing to severe gastrointestinal side effects after oral administratio... |
PMC11156749 | core_pubmed_pmc | Imatinib pharmacokinetics and creatine kinase levels in chronic myeloid leukemia patients: implications for therapeutic response and monitoring | Imatinib pharmacokinetics and creatine kinase levels in chronic myeloid leukemia patients: implications for therapeutic response and monitoring Abstract Background Imatinib treatment for certain cancers can lead to elevated creatine kinase (CK) levels, potentially indicating muscle injury, and ongoing research aims to ... |
PMC12743464 | core_pubmed_pmc | Engineering Optimized Nanostructured Lipid Carriers for Astaxanthin: A Response Surface Methodology Approach | Engineering Optimized Nanostructured Lipid Carriers for Astaxanthin: A Response Surface Methodology Approach Abstract Abstract Introduction The xanthophyll carotenoid astaxanthin is well-known for its potent antioxidant properties, which are superior to those of other antioxidants such as vitamins C and E. However, thi... |
PMC6221039 | core_pubmed_pmc | Amenamevir: Studies of Potential CYP2C8‐ and CYP2B6‐Mediated Pharmacokinetic Interactions With Montelukast and Bupropion in Healthy Volunteers | Amenamevir: Studies of Potential CYP2C8‐ and CYP2B6‐Mediated Pharmacokinetic Interactions With Montelukast and Bupropion in Healthy Volunteers Abstract Abstract Amenamevir (formerly ASP2151) induces cytochrome P450 (CYP)2B6 and CYP3A4 and inhibits CYP2C8. We conducted 2 studies, 1 using montelukast as a probe to assess... |
PMC4223074 | core_pubmed_pmc | Rapid and Simultaneous Quantification of Levetiracetam and Its Carboxylic Metabolite in Human Plasma by Liquid Chromatography Tandem Mass Spectrometry | Rapid and Simultaneous Quantification of Levetiracetam and Its Carboxylic Metabolite in Human Plasma by Liquid Chromatography Tandem Mass Spectrometry Abstract A simple liquid chromatography tandem mass spectrometry method was developed and validated according to the guidelines of the US Food and Drug Administration an... |
PMC7335633 | core_pubmed_pmc | Identification of potential inhibitors against SARS-CoV-2 by targeting proteins responsible for envelope formation and virion assembly using docking based virtual screening, and pharmacokinetics approaches | Identification of potential inhibitors against SARS-CoV-2 by targeting proteins responsible for envelope formation and virion assembly using docking based virtual screening, and pharmacokinetics approaches Abstract WHO has declared the outbreak of COVID-19 as a public health emergency of international concern. The ever... |
PMC9543705 | core_pubmed_pmc | Profiling of warfarin pharmacokinetics‐associated genetic variants: Black Africans portray unique genetic markers important for an African specific warfarin pharmacogenetics‐dosing algorithm | Profiling of warfarin pharmacokinetics‐associated genetic variants: Black Africans portray unique genetic markers important for an African specific warfarin pharmacogenetics‐dosing algorithm Abstract Abstract Background Warfarin dose variability observed in patients is attributed to variation in genes involved in the w... |
PMC10520102 | core_pubmed_pmc | Mirikizumab Pharmacokinetics in Patients with Moderately to Severely Active Ulcerative Colitis: Results from Phase III LUCENT Studies | Mirikizumab Pharmacokinetics in Patients with Moderately to Severely Active Ulcerative Colitis: Results from Phase III LUCENT Studies Abstract Background and Objective Mirikizumab is a humanized anti-interleukin-23-p19 monoclonal antibody being developed for ulcerative colitis and Crohn’s disease. This analysis charact... |
PMC5007276 | core_pubmed_pmc | Pharmacokinetics and excretion of 14 C-omacetaxine in patients with advanced solid tumors | Pharmacokinetics and excretion of 14 C-omacetaxine in patients with advanced solid tumors Abstract Summary Background Omacetaxine mepesuccinate is indicated in adults with chronic myeloid leukemia resistant and/or intolerant to ≥ 2 tyrosine kinase inhibitor treatments. This phase I study assessed the disposition, elimi... |
PMC8301577 | core_pubmed_pmc | Impact of carboxylesterase 1 genetic polymorphism on trandolapril activation in human liver and the pharmacokinetics and pharmacodynamics in healthy volunteers | Impact of carboxylesterase 1 genetic polymorphism on trandolapril activation in human liver and the pharmacokinetics and pharmacodynamics in healthy volunteers Abstract Abstract Trandolapril, an angiotensin‐converting enzyme inhibitor prodrug, needs to be activated by carboxylesterase 1 (CES1) in the liver to exert its... |
PMC6744479 | core_pubmed_pmc | Mimicking in-vivo exposures to drug combinations in-vitro : anti-tuberculosis drugs in lung lesions and the hollow fiber model of infection | Mimicking in-vivo exposures to drug combinations in-vitro : anti-tuberculosis drugs in lung lesions and the hollow fiber model of infection Abstract Here, we evaluate protocol requirements to mimic therapeutically relevant drug concentrations at the site of infection (i.e. lung lesion) in an in-vitro hollow fibre model... |
PMC10746753 | core_pubmed_pmc | Preclinical Pharmacokinetics and Translational Pharmacokinetic/Pharmacodynamic Modeling of M8891, a Potent and Reversible Inhibitor of Methionine Aminopeptidase 2 | Preclinical Pharmacokinetics and Translational Pharmacokinetic/Pharmacodynamic Modeling of M8891, a Potent and Reversible Inhibitor of Methionine Aminopeptidase 2 Abstract Abstract Introduction M8891 is a selective and reversible inhibitor of methionine aminopeptidase 2 (MetAP2). We describe translational research to d... |
PMC8853508 | core_pubmed_pmc | Evidence for the early emergence of piperaquine-resistant Plasmodium falciparum malaria and modeling strategies to mitigate resistance | Evidence for the early emergence of piperaquine-resistant Plasmodium falciparum malaria and modeling strategies to mitigate resistance Abstract Abstract Multidrug-resistant Plasmodium falciparum parasites have emerged in Cambodia and neighboring countries in Southeast Asia, compromising the efficacy of first-line antim... |
PMC5108032 | core_pubmed_pmc | Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy | Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy Abstract The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen... |
PMC11724043 | core_pubmed_pmc | Sitravatinib in combination with nivolumab plus ipilimumab in patients with advanced clear cell renal cell carcinoma: a phase 1 trial | Sitravatinib in combination with nivolumab plus ipilimumab in patients with advanced clear cell renal cell carcinoma: a phase 1 trial Abstract We conducted a phase I trial to determine the optimal dose of triplet therapy with the tyrosine kinase inhibitor sitravatinib plus nivolumab plus ipilimumab in 22 previously unt... |
PMC11526151 | core_pubmed_pmc | In silico prediction of some pharmacokinetic, safety, biological activity and molecular docking studies of 1-piperazine indole hybrid with nicotinic amide and nicotinic acid and their analogues | In silico prediction of some pharmacokinetic, safety, biological activity and molecular docking studies of 1-piperazine indole hybrid with nicotinic amide and nicotinic acid and their analogues Abstract Abstract Background: In silico predictions are now being utilized in drug discovery and design to assess the physicoc... |
PMC7808403 | core_pubmed_pmc | Recent Advancement in Nanotechnology-Based Drug Delivery System Against Viral Infections | Recent Advancement in Nanotechnology-Based Drug Delivery System Against Viral Infections Abstract Abstract In the last few decades, the exponential rise in the incidence of viral infections sets a global health emergency across the world. The biomimetic architecture, the ability to hijack host immune responses, continu... |
PMC3990384 | core_pubmed_pmc | Pharmacokinetics of Zidovudine Dosed Twice Daily According to World Health Organization Weight Bands in Ugandan HIV-infected Children | Pharmacokinetics of Zidovudine Dosed Twice Daily According to World Health Organization Weight Bands in Ugandan HIV-infected Children Abstract Supplemental Digital Content is available in the text. Keywords: zidovudine, pharmacokinetics, HIV, children, Africa Abstract Data on zidovudine pharmacokinetics in children dos... |
PMC6594244 | core_pubmed_pmc | Effects of Oral Ginger Supplementation on the INR | Effects of Oral Ginger Supplementation on the INR Abstract Abstract Although there are competing options for anticoagulation, many Americans remain on warfarin. Concurrently, the use of alternative medicines is on the rise. With that, the potential for interactions between them is increasing. Ginger has gained populari... |
PMC8748612 | core_pubmed_pmc | Maximizing response to intratumoral immunotherapy in mice by tuning local retention | Maximizing response to intratumoral immunotherapy in mice by tuning local retention Abstract Abstract Direct injection of therapies into tumors has emerged as an administration route capable of achieving high local drug exposure and strong anti-tumor response. A diverse array of immune agonists ranging in size and targ... |
PMC9323134 | core_pubmed_pmc | Monocrotaline Toxicity Alters the Function of Hepatocyte Membrane Transporters in Rats | Monocrotaline Toxicity Alters the Function of Hepatocyte Membrane Transporters in Rats Abstract Pyrrolizidine alkaloid monocrotaline (MCT) induces sinusoidal obstruction syndrome (SOS) in rats characterised by a sinusoidal congestive obstruction. Additionally, MCT administration decreases the biliary excretion of gadob... |
PMC6691366 | core_pubmed_pmc | Single-dose pharmacokinetics of meropenem in porcine cancellous bone determined by microdialysis | Single-dose pharmacokinetics of meropenem in porcine cancellous bone determined by microdialysis Abstract Objectives Meropenem may be an important drug in the treatment of open tibial fractures and chronic osteomyelitis. Therefore, the objective of this study was to describe meropenem pharmacokinetics in plasma, subcut... |
PMC10394562 | core_pubmed_pmc | Pharmacokinetics of recombinant factor VIII in adults with severe hemophilia A: fixed-sequence single-dose study of octocog alfa, rurioctocog alfa pegol, and efanesoctocog alfa | Pharmacokinetics of recombinant factor VIII in adults with severe hemophilia A: fixed-sequence single-dose study of octocog alfa, rurioctocog alfa pegol, and efanesoctocog alfa Abstract Background Efanesoctocog alfa is a new class of factor (F) VIII replacement therapy designed to provide high sustained factor levels f... |
PMC6986439 | core_pubmed_pmc | Sultiame pharmacokinetic profile in plasma and erythrocytes after single oral doses: A pilot study in healthy volunteers | Sultiame pharmacokinetic profile in plasma and erythrocytes after single oral doses: A pilot study in healthy volunteers Abstract Abstract A pilot study was conducted aiming at specifying sultiame's pharmacokinetic profile, completed by in vitro assays evaluating the intraerythrocytic transfer of sultiame and by a phar... |
PMC8901605 | core_pubmed_pmc | Targeting Mcl-1 by AMG-176 During Ibrutinib and Venetoclax Therapy in Chronic Lymphocytic Leukemia | Targeting Mcl-1 by AMG-176 During Ibrutinib and Venetoclax Therapy in Chronic Lymphocytic Leukemia Abstract B-cell receptor (BCR) signaling pathway and Bcl-2 family prosurvival proteins, specifically Bcl-2 and Mcl-1, are functional in the pathobiology of chronic lymphocytic leukemia (CLL). A pivotal and apical molecule... |
PMC4614199 | core_pubmed_pmc | Phase I Study of OPB-31121, an Oral STAT3 Inhibitor, in Patients with Advanced Solid Tumors | Phase I Study of OPB-31121, an Oral STAT3 Inhibitor, in Patients with Advanced Solid Tumors Abstract Abstract Purpose OPB-31121 is an oral STAT3 inhibitor with a good preclinical antitumor activity. This phase I dose-escalation study of OPB-31121 was conducted to determine maximum-tolerated dose (MTD), safety, pharmaco... |
PMC11773116 | core_pubmed_pmc | Exploring the contribution of genetic variants to high sunitinib exposure in patients with cancer | Exploring the contribution of genetic variants to high sunitinib exposure in patients with cancer Abstract Abstract Aims Sunitinib exhibits considerable interindividual variability in exposure. While the target total plasma concentration of sunitinib and its active metabolite is 50–87.5 ng/mL for the intermittent dosin... |
PMC7000638 | core_pubmed_pmc | Anti-MAdCAM-1 antibody (PF-00547659) for active refractory Crohn’s disease in Japanese and Korean patients: the OPERA study | Anti-MAdCAM-1 antibody (PF-00547659) for active refractory Crohn’s disease in Japanese and Korean patients: the OPERA study Abstract Background/Aims PF-00547659 is a monoclonal antibody against human mucosal addressin cell adhesion molecule-1 (MAdCAM-1) that prevents the binding of α4β7 + lymphocytes to MAdCAM-expressi... |
PMC8010309 | core_pubmed_pmc | Application of a Physiologically Based Pharmacokinetic Model to Characterize Time-dependent Metabolism of Voriconazole in Children and Support Dose Optimization | Application of a Physiologically Based Pharmacokinetic Model to Characterize Time-dependent Metabolism of Voriconazole in Children and Support Dose Optimization Abstract Background: Voriconazole is a potent antifungal drug with complex pharmacokinetics caused by time-dependent inhibition and polymorphisms of metabolizi... |
PMC9476775 | core_pubmed_pmc | Brusatol: A potential anti-tumor quassinoid from Brucea javanica | Brusatol: A potential anti-tumor quassinoid from Brucea javanica Abstract Brusatol, a triterpene lactone compound mainly from Brucea javanica , sensitizes a broad spectrum of cancer cells. It is known as a specific inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway. In this review, we provide a com... |
PMC8741190 | core_pubmed_pmc | Real-time monitoring of drug pharmacokinetics within tumor tissue in live animals | Real-time monitoring of drug pharmacokinetics within tumor tissue in live animals Abstract Abstract The efficacy and safety of a chemotherapy regimen fundamentally depends on its pharmacokinetics. This is currently measured based on blood samples, but the abnormal vasculature and physiological heterogeneity of the tumo... |
PMC7881784 | core_pubmed_pmc | Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation | Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation Abstract Purpose The purpose of this proposed research was to investigate a nano-formulation developed using self-nanoemulsifying drug delivery system (SNEDDS) to improve the pharmacodynam... |
PMC5236087 | core_pubmed_pmc | A Generic Multi-Compartmental CNS Distribution Model Structure for 9 Drugs Allows Prediction of Human Brain Target Site Concentrations | A Generic Multi-Compartmental CNS Distribution Model Structure for 9 Drugs Allows Prediction of Human Brain Target Site Concentrations Abstract Purpose Predicting target site drug concentration in the brain is of key importance for the successful development of drugs acting on the central nervous system. We propose a g... |
PMC8420880 | core_pubmed_pmc | Comparison of Drug Availability in the Inner Ear After Oral, Transtympanic, and Combined Administration | Comparison of Drug Availability in the Inner Ear After Oral, Transtympanic, and Combined Administration Abstract Abstract Although combination of oral and transtympanic drug therapy (CT) has been proved more effective and safer for idiopathic sudden sensorineural hearing loss (ISSNHL) by some clinical trials, there are... |
PMC10582678 | core_pubmed_pmc | A randomized, controlled single, and multiple ascending dose trial of the safety, pharmacokinetics and pharmacodynamics of SN1011 in healthy subjects | A randomized, controlled single, and multiple ascending dose trial of the safety, pharmacokinetics and pharmacodynamics of SN1011 in healthy subjects Abstract Abstract The purpose of this study was to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of SN1011, a novel Bruton tyrosine kinase ... |
PMC10196163 | core_pubmed_pmc | The pharmacokinetics and pharmacodynamics of esomeprazole in sheep after intravenous dosing | The pharmacokinetics and pharmacodynamics of esomeprazole in sheep after intravenous dosing Abstract Abomasal (gastric) ulceration is a morbidity in sheep, and currently, there is a paucity of pharmacokinetic and pharmacodynamic data for gastroprotectant drugs reported for this species. The proton pump inhibitor esomep... |
PMC8577762 | core_pubmed_pmc | Effects of concurrent and staggered dosing of semi-solid enteral nutrients on pharmacokinetic behavior of antiepileptic drugs after oral administration in rats | Effects of concurrent and staggered dosing of semi-solid enteral nutrients on pharmacokinetic behavior of antiepileptic drugs after oral administration in rats Abstract Abstract Background The use of enteral nutrients plays a highly important role in accurate nutrition management, but limited information is currently a... |
PMC12163612 | core_pubmed_pmc | Gender-stratified 9-month comparison of paliperidone extended-release tablets and paliperidone palmitate injection in schizophrenia | Gender-stratified 9-month comparison of paliperidone extended-release tablets and paliperidone palmitate injection in schizophrenia Abstract Abstract Background Gender differences in antipsychotic efficacy for schizophrenia (SCZ) remain understudied despite evidence of sex-dependent pharmacokinetic, neurobiological, an... |
PMC11651182 | core_pubmed_pmc | Identification of fibrinogen as a plasma protein binding partner for lecanemab biosimilar IgG | Identification of fibrinogen as a plasma protein binding partner for lecanemab biosimilar IgG Abstract Abstract Objective Recombinant monoclonal therapeutic antibodies like lecanemab, which target amyloid beta in Alzheimer's disease, offer a promising approach for modifying the disease progression. Due to its relativel... |
PMC6168621 | core_pubmed_pmc | Atypical Pharmacodynamic Properties and Metabolic Profile of the Abused Synthetic Cannabinoid AB-PINACA: Potential Contribution to Pronounced Adverse Effects Relative to Δ 9 -THC | Atypical Pharmacodynamic Properties and Metabolic Profile of the Abused Synthetic Cannabinoid AB-PINACA: Potential Contribution to Pronounced Adverse Effects Relative to Δ 9 -THC Abstract Abstract Recreational use of marijuana is associated with few adverse effects, but abuse of synthetic cannabinoids (SCBs) can result... |
PMC11675703 | core_pubmed_pmc | Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest | Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest Abstract Altrenogest is a key regulatory hormone for intensive and batch management of reserve sows in breeding farms. As a synthetic hormone, altrenogest could make ovaries stay at the initial stage of follicles and in... |
PMC9292509 | core_pubmed_pmc | A Dose‐Confirmation Phase 1 Study to Evaluate the Safety and Pharmacology of Glucarpidase in Healthy Volunteers | A Dose‐Confirmation Phase 1 Study to Evaluate the Safety and Pharmacology of Glucarpidase in Healthy Volunteers Abstract Abstract Glucarpidase rapidly decomposes methotrexate. A phase 1 study of glucarpidase in an open‐label, randomized parallel group was conducted to evaluate the safety, pharmacokinetics, and other ph... |
PMC7559746 | core_pubmed_pmc | Influence of Probenecid on the Pharmacokinetics and Pharmacodynamics of Sorafenib | Influence of Probenecid on the Pharmacokinetics and Pharmacodynamics of Sorafenib Abstract Prior studies have demonstrated an organic anion transporter 6 (OAT6)-mediated accumulation of sorafenib in keratinocytes. The OAT6 inhibitor probenecid decreases sorafenib uptake in skin and might, therefore, decrease sorafenib-... |
PMC7032114 | core_pubmed_pmc | Pharmacokinetics of a ternary conjugate based pH-responsive 10-HCPT prodrug nano-micelle delivery system | Pharmacokinetics of a ternary conjugate based pH-responsive 10-HCPT prodrug nano-micelle delivery system Abstract Abstract A pH-responsive conjugate based 10-hydroxycamptothecin-thiosemicarbazide-polyethene glycol 2000 (10-HCPT-hydro-PEG) nano-micelles were prepared in our previous study. In the present study, ultra-pe... |
PMC6226112 | core_pubmed_pmc | No Pharmacokinetic Interactions Between Elbasvir or Grazoprevir and Buprenorphine/Naloxone in Healthy Participants and Participants Receiving Stable Opioid Agonist Therapy | No Pharmacokinetic Interactions Between Elbasvir or Grazoprevir and Buprenorphine/Naloxone in Healthy Participants and Participants Receiving Stable Opioid Agonist Therapy Abstract Abstract The aims of these phase I trials were to evaluate the pharmacokinetic interaction between elbasvir (EBR) or grazoprevir (GZR) and ... |
PMC6401406 | core_pubmed_pmc | Quantitative MALDI Imaging of Spatial Distributions and Dynamic Changes of Tetrandrine in Multiple Organs of Rats | Quantitative MALDI Imaging of Spatial Distributions and Dynamic Changes of Tetrandrine in Multiple Organs of Rats Abstract Detailed spatio-temporal information on drug distribution in organs is of paramount importance to assess drug clinically-relevant properties and potential side-effects. Matrix-assisted laser desorp... |
PMC10733202 | core_pubmed_pmc | Active Uptake of Oxycodone at Both the Blood-Cerebrospinal Fluid Barrier and The Blood-Brain Barrier without Sex Differences: A Rat Microdialysis Study | Active Uptake of Oxycodone at Both the Blood-Cerebrospinal Fluid Barrier and The Blood-Brain Barrier without Sex Differences: A Rat Microdialysis Study Abstract Background Oxycodone active uptake across the blood-brain barrier (BBB) is associated with the putative proton-coupled organic cation (H + /OC) antiporter syst... |
PMC7015960 | core_pubmed_pmc | Effect of rifampin and itraconazole on the pharmacokinetics of zanubrutinib (a Bruton's tyrosine kinase inhibitor) in Asian and non-Asian healthy subjects | Effect of rifampin and itraconazole on the pharmacokinetics of zanubrutinib (a Bruton's tyrosine kinase inhibitor) in Asian and non-Asian healthy subjects Abstract Purpose Zanubrutinib (BGB-3111) is a potent Bruton’s tyrosine kinase inhibitor with promising clinical activity in B-cell malignancies. Zanubrutinib was sho... |
PMC5909787 | core_pubmed_pmc | Population pharmacokinetics and dosing optimization of cefathiamidine in children with hematologic infection | Population pharmacokinetics and dosing optimization of cefathiamidine in children with hematologic infection Abstract Abstract Purpose Cefathiamidine, a first-generation cephalosporin, has approval from the China Food and Drug Administration for the treatment of infections caused by susceptible bacteria in both adults ... |
PMC10725258 | core_pubmed_pmc | A multicompartment population PK model to predict tenofovir and emtricitabine mucosal tissue concentrations for HIV prevention | A multicompartment population PK model to predict tenofovir and emtricitabine mucosal tissue concentrations for HIV prevention Abstract Abstract A priori use of mathematical modeling and simulation to predict outcomes from incomplete adherence or reduced frequency dosing strategies may mitigate the risk of clinical tri... |
PMC10462944 | core_pubmed_pmc | Extended safety and tolerability of subcutaneous CAP256V2LS and VRC07-523LS in HIV-negative women: study protocol for the randomised, placebo-controlled double-blinded, phase 2 CAPRISA 012C trial | Extended safety and tolerability of subcutaneous CAP256V2LS and VRC07-523LS in HIV-negative women: study protocol for the randomised, placebo-controlled double-blinded, phase 2 CAPRISA 012C trial Abstract Abstract Introduction Women-controlled HIV prevention technologies that overcome adherence challenges of available ... |
PMC8880204 | core_pubmed_pmc | Application of Semi-Mechanistic Pharmacokinetic and Pharmacodynamic Model in Antimicrobial Resistance | Application of Semi-Mechanistic Pharmacokinetic and Pharmacodynamic Model in Antimicrobial Resistance Abstract Antimicrobial resistance is a major public health issue. The pharmacokinetic/pharmacodynamic (PK/PD) model is an essential tool to optimize dosage regimens and alleviate the emergence of resistance. The semi-m... |
PMC12562389 | core_pubmed_pmc | In Silico Network Pharmacology, Molecular Docking, and Molecular Dynamics Analysis of Rosemary-Derived Compounds as Potential HSP90 Inhibitors for Cancer Therapy | In Silico Network Pharmacology, Molecular Docking, and Molecular Dynamics Analysis of Rosemary-Derived Compounds as Potential HSP90 Inhibitors for Cancer Therapy Abstract Abstract Cancer remains a major global health challenge, emphasizing the need for new and effective therapies. This study investigates the anticancer... |
PMC12569548 | core_pubmed_pmc | Recurrent fexuprazan‐induced liver injury following unintentional re‐exposure | Recurrent fexuprazan‐induced liver injury following unintentional re‐exposure Abstract Fexuprazan, a potassium‐competitive acid blocker, is increasingly used for the treatment of gastroesophageal reflux disease in South Korea. While generally well tolerated, data regarding its hepatotoxic potential are scarce. We repor... |
PMC8399031 | core_pubmed_pmc | Association between Olaparib Exposure and Early Toxicity in BRCA-Mutated Ovarian Cancer Patients: Results from a Retrospective Multicenter Study | Association between Olaparib Exposure and Early Toxicity in BRCA-Mutated Ovarian Cancer Patients: Results from a Retrospective Multicenter Study Abstract Factors associated with olaparib toxicity remain unknown in ovarian cancer patients. The large inter-individual variability in olaparib pharmacokinetics could contrib... |
PMC11770187 | core_pubmed_pmc | Unveiling the biological activities of Heliotropium indicum L. plant extracts: anti-inflammatory activities, GC–MS analysis, and in-silico molecular docking | Unveiling the biological activities of Heliotropium indicum L. plant extracts: anti-inflammatory activities, GC–MS analysis, and in-silico molecular docking Abstract Heliotropium indicum is well-known for its diverse medicinal properties, traditionally utilized to treat ailments such as diabetes, obesity, bacterial inf... |
PMC11939361 | core_pubmed_pmc | diAcCA, a Pro-Drug for Carnosic Acid That Activates the Nrf2 Transcriptional Pathway, Shows Efficacy in the 5xFAD Transgenic Mouse Model of Alzheimer’s Disease | diAcCA, a Pro-Drug for Carnosic Acid That Activates the Nrf2 Transcriptional Pathway, Shows Efficacy in the 5xFAD Transgenic Mouse Model of Alzheimer’s Disease Abstract The antioxidant/anti-inflammatory compound carnosic acid (CA) is a phenolic diterpene found in the herbs rosemary and sage. Upon activation, CA manifes... |
PMC10085060 | core_pubmed_pmc | A phase I trial of riluzole and sorafenib in patients with advanced solid tumors: CTEP #8850 | A phase I trial of riluzole and sorafenib in patients with advanced solid tumors: CTEP #8850 Abstract Abstract Background: Overexpression of metabotropic glutamate receptor 1 (GRM1) has been implicated in the pathogenesis of multiple cancers. Riluzole, an inhibitor of glutamate release, showed synergistic antitumor act... |
PMC8522776 | core_pubmed_pmc | Determinants of primaquine and carboxyprimaquine exposures in children and adults with Plasmodium vivax malaria | Determinants of primaquine and carboxyprimaquine exposures in children and adults with Plasmodium vivax malaria Abstract Abstract Background Primaquine is the only widely available drug for radical cure of Plasmodium vivax malaria. There is uncertainty whether the pharmacokinetic properties of primaquine are altered si... |
PMC5715499 | core_pubmed_pmc | Paracetamol clinical dosing routine leads to paracetamol underexposure in an adult severely ill sub-Saharan African hospital population: a drug concentration measurement study | Paracetamol clinical dosing routine leads to paracetamol underexposure in an adult severely ill sub-Saharan African hospital population: a drug concentration measurement study Abstract Background Hospitals in sub-Saharan Africa (SSA) continue to receive high numbers of severely ill (HIV-infected) patients with physical... |
PMC12804367 | core_pubmed_pmc | A phase II study of the AKT inhibitor TAS-117 in patients with advanced solid tumors and germline PTEN mutations | A phase II study of the AKT inhibitor TAS-117 in patients with advanced solid tumors and germline PTEN mutations Abstract Abstract Background Protein kinase B (AKT)-directed therapies offer promise for patients with cancers harboring germline and somatic phosphatase and tensin homolog ( PTEN ) mutations. TAS-117 is an ... |
PMC12285691 | core_pubmed_pmc | Allopregnanolone Concentrations After Ascending Single Dose Administration of Progesterone to Healthy Volunteers | Allopregnanolone Concentrations After Ascending Single Dose Administration of Progesterone to Healthy Volunteers Abstract ABSTRACT Background Postpartum depression (PPD) is associated with significant morbidity and mortality. It affects as many as 11.5% of women giving birth. Allopregnanolone (an endogenous progesteron... |
PMC12642065 | core_pubmed_pmc | Cohort profile: the pharmacogenomics and pharmacokinetics study in Ghanaian HIV patients (GenoPharm-GH) | Cohort profile: the pharmacogenomics and pharmacokinetics study in Ghanaian HIV patients (GenoPharm-GH) Abstract Abstract Background The GenoPharm-GH project initiated in 2019, as a longitudinal, multi-site observational cohort study aimed at bridging gaps in understanding the influence of host genetics, pharmacokineti... |
PMC9440868 | core_pubmed_pmc | Pharmacodynamic effect of bempedoic acid and statin combinations: predictions from a dose–response model | Pharmacodynamic effect of bempedoic acid and statin combinations: predictions from a dose–response model Abstract Abstract Aims Many patients are unable to achieve guideline-recommended LDL cholesterol (LDL-C) targets, despite taking maximally tolerated lipid-lowering therapy. Bempedoic acid, a competitive inhibitor of... |
PMC12746359 | core_pubmed_pmc | Feasibility of dried blood spot collection for caffeine pharmacokinetic studies in microgravity: Insights from parabolic flight campaigns | Feasibility of dried blood spot collection for caffeine pharmacokinetic studies in microgravity: Insights from parabolic flight campaigns Abstract Abstract Aims Therapeutic drug monitoring for astronauts faces limitations in conventional blood sampling and sample management onboard the international space station. Here... |
PMC9145325 | core_pubmed_pmc | Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies | Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Apremilast: In Vitro Evaluation and Pharmacokinetics Studies Abstract Psoriatic arthritis is an autoimmune disease of the joints that can lead to persistent inflammation, irreversible joint damage and disability. The current treatments are of limited efficacy and in... |
PMC8080052 | core_pubmed_pmc | Antidepressant activity of rose oxide essential oil: possible involvement of serotonergic transmission | Antidepressant activity of rose oxide essential oil: possible involvement of serotonergic transmission Abstract Abstract Rose oxide (RO) is a monoterpene found in rose oil fragrances. This monoterpene has been reported to possess anti-inflammatory activity, however, little is known regarding its pharmacological activit... |
PMC7497674 | core_pubmed_pmc | Phase 1b/2a study of galunisertib, a small molecule inhibitor of transforming growth factor-beta receptor I, in combination with standard temozolomide-based radiochemotherapy in patients with newly diagnosed malignant glioma | Phase 1b/2a study of galunisertib, a small molecule inhibitor of transforming growth factor-beta receptor I, in combination with standard temozolomide-based radiochemotherapy in patients with newly diagnosed malignant glioma Abstract Summary Purpose Galunisertib, a TGF-β inhibitor, has demonstrated antitumor effects in... |
PMC9534738 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Model-Informed Dosing Guidelines for Pediatric Clinical Care: A Pragmatic Approach for a Special Population | Physiologically Based Pharmacokinetic (PBPK) Model-Informed Dosing Guidelines for Pediatric Clinical Care: A Pragmatic Approach for a Special Population Abstract Physiologically based pharmacokinetic (PBPK) modeling can be an attractive tool to increase the evidence base of pediatric drug dosing recommendations by maki... |
PMC6985102 | core_pubmed_pmc | A general covalent binding model between cytotoxic selenocompounds and albumin revealed by mass spectrometry and X-ray absorption spectroscopy | A general covalent binding model between cytotoxic selenocompounds and albumin revealed by mass spectrometry and X-ray absorption spectroscopy Abstract Selenocompounds (SeCs) are promising therapeutic agents for a wide range of diseases including cancer. The treatment results are heterogeneous and dependent on both the... |
PMC6497007 | core_pubmed_pmc | Development, Validation of LC-MS/MS Method and Determination of Pharmacokinetic Parameters of the Stroke Neuroprotectant Neurounina-1 in Beagle Dog Plasma After Intravenous Administration | Development, Validation of LC-MS/MS Method and Determination of Pharmacokinetic Parameters of the Stroke Neuroprotectant Neurounina-1 in Beagle Dog Plasma After Intravenous Administration Abstract Neurounina-1 [chemical name: 7-nitro-5-phenyl-1-(pyrrolidin-1-ylmethyl)-1H-benzo[e]diazepin-2(3H)-one] is a new compound pr... |
PMC5113768 | core_pubmed_pmc | Extended‐Release Once‐Daily Formulation of Tofacitinib: Evaluation of Pharmacokinetics Compared With Immediate‐Release Tofacitinib and Impact of Food | Extended‐Release Once‐Daily Formulation of Tofacitinib: Evaluation of Pharmacokinetics Compared With Immediate‐Release Tofacitinib and Impact of Food Abstract Abstract Tofacitinib is an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis. An extended‐release (XR) formulation has been designed to provi... |
PMC12402090 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic studies of injectable nocathiacin as a novel antibacterial agent | Pharmacokinetic and pharmacodynamic studies of injectable nocathiacin as a novel antibacterial agent Abstract The extreme hydrophobicity of nocathiacin, a potent thiopeptide antibiotic against multidrug-resistant (MDR) Gram-positive pathogens, has limited its clinical development. This study formulated an injectable ly... |
PMC5028085 | core_pubmed_pmc | Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans | Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans Abstract Background Evaluating the potential risk of metabolic drug–drug interactions (DDIs) is clinically important. Objective To develop a physiologically based pharmacokinetic (... |
PMC10896214 | core_pubmed_pmc | Somatostatin Receptor Subtype-2 Targeting System for Specific Delivery of Temozolomide | Somatostatin Receptor Subtype-2 Targeting System for Specific Delivery of Temozolomide Abstract Temozolomide (TMZ) is a DNA alkylating agent that produces objective responses in patients with neuroendocrine tumors (NETs) when the DNA repair enzyme O 6 -methylguanine-DNA methyltransferase (MGMT) is inactivated. At high ... |
PMC9199870 | core_pubmed_pmc | Pharmacokinetics/pharmacodynamics of L‐ornithine phenylacetate in overt hepatic encephalopathy and the effect of plasma ammonia concentration reduction on clinical outcomes | Pharmacokinetics/pharmacodynamics of L‐ornithine phenylacetate in overt hepatic encephalopathy and the effect of plasma ammonia concentration reduction on clinical outcomes Abstract Abstract Hepatic encephalopathy (HE) is a serious neurocognitive complication of liver dysfunction, often associated with elevated plasma ... |
PMC12065821 | core_pubmed_pmc | The pharmacokinetic-nephrotoxicity relationships of CMS and CMS-E2 from the perspective of plasma and kidney drug concentrations in rats | The pharmacokinetic-nephrotoxicity relationships of CMS and CMS-E2 from the perspective of plasma and kidney drug concentrations in rats Abstract Abstract Nephrotoxicity has seriously affected the clinical application of colistin methanesulphonate (CMS). Colistin B methanesulphonate (CMS-E2) is a novel polymyxin develo... |
PMC12516152 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Valemetostat to Inform Dose Recommendations When Coadministered With CYP3A /P‐gp Modulators | Physiologically Based Pharmacokinetic Modeling of Valemetostat to Inform Dose Recommendations When Coadministered With CYP3A /P‐gp Modulators Abstract ABSTRACT Valemetostat tosylate (valemetostat) is an oral, potent, selective dual inhibitor of enhancer of zeste homolog (EZH)2 and EZH1, approved in Japan for the treatm... |
PMC8717895 | core_pubmed_pmc | Phase I study using crenolanib to target PDGFR kinase in children and young adults with newly diagnosed DIPG or recurrent high-grade glioma, including DIPG | Phase I study using crenolanib to target PDGFR kinase in children and young adults with newly diagnosed DIPG or recurrent high-grade glioma, including DIPG Abstract Abstract Background Platelet-derived growth factor receptor (PDGFR) signaling has been directly implicated in pediatric high-grade gliomagenesis. This stud... |
PMC7406372 | core_pubmed_pmc | Dose Regimen Rationale for Panitumumab in Cancer Patients: To Be Based on Body Weight or Not | Dose Regimen Rationale for Panitumumab in Cancer Patients: To Be Based on Body Weight or Not Abstract Introduction Body weight can affect exposure, safety and efficacy of antibody-based therapies; sometimes these effects may not be clinically relevant. Panitumumab is approved for wild-type RAS metastatic colorectal can... |
PMC12015958 | core_pubmed_pmc | Predicting Liver-Related In Vitro Endpoints with Machine Learning to Support Early Detection of Drug-Induced Liver Injury | Predicting Liver-Related In Vitro Endpoints with Machine Learning to Support Early Detection of Drug-Induced Liver Injury Abstract Abstract Drug-induced liver injury (DILI) is a major cause of drug development failures and postmarket drug withdrawals, posing significant challenges to public health and pharmaceutical re... |
PMC3293351 | core_pubmed_pmc | Pharmacokinetics and Excretion Studies on CDRI-85/92, an Antiulcer Proton Pump Inhibitor | Pharmacokinetics and Excretion Studies on CDRI-85/92, an Antiulcer Proton Pump Inhibitor Abstract Abstract CDRI 85/92 is an antiulcer pharmacophore and a proton pump inhibitor, which is in an advanced stage of preclinical trials. In view of its importance, pharmacokinetic and excretion were studied in Sprague Dawley ra... |
PMC10144034 | core_pubmed_pmc | Senkyunolide I: A Review of Its Phytochemistry, Pharmacology, Pharmacokinetics, and Drug-Likeness | Senkyunolide I: A Review of Its Phytochemistry, Pharmacology, Pharmacokinetics, and Drug-Likeness Abstract Abstract Senkyunolide I (SI) is a natural phthalide that has drawn increasing interest for its potential as a cardio-cerebral vascular drug candidate. In this paper, the botanical sources, phytochemical characteri... |
PMC6302520 | core_pubmed_pmc | Rivaroxaban versus standard anticoagulation for acute venous thromboembolism in childhood. Design of the EINSTEIN-Jr phase III study | Rivaroxaban versus standard anticoagulation for acute venous thromboembolism in childhood. Design of the EINSTEIN-Jr phase III study Abstract Abstract Background Venous thromboembolism (VTE) is a relatively rare condition in childhood with treatment mainly based on extrapolation from studies in adults. Therefore, clini... |
PMC7818492 | core_pubmed_pmc | Evaluation of the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Emicizumab in Healthy Chinese Subjects | Evaluation of the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Emicizumab in Healthy Chinese Subjects Abstract Abstract This phase 1, open‐label, single‐center study evaluated the pharmacokinetics (PK), pharmacodynamics, safety, and tolerability of single‐dose emicizumab in healthy Chinese males. ... |
PMC6220931 | core_pubmed_pmc | Interchangeability of Generic Drugs: A Nonparametric Pharmacokinetic Model of Gabapentin Generic Drugs | Interchangeability of Generic Drugs: A Nonparametric Pharmacokinetic Model of Gabapentin Generic Drugs Abstract Substitution by generic drugs is allowed when bioequivalence to the originator drug has been established. However, it is known that similarity in exposure may not be achieved at every occasion for all individ... |
PMC12677105 | core_pubmed_pmc | Pharmacodynamics, Safety, and Tolerability of Pyridostigmine Bromide in Heart Failure | Pharmacodynamics, Safety, and Tolerability of Pyridostigmine Bromide in Heart Failure Abstract Abstract Background Pyridostigmine bromide is a short-acting carbamate acetylcholinesterase inhibitor that has been shown to acutely augment parasympathetic signaling in cardiovascular disease populations. Objective This stud... |
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