id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC10386266 | core_pubmed_pmc | Advanced In Vivo Prediction by Introducing Biphasic Dissolution Data into PBPK Models | Advanced In Vivo Prediction by Introducing Biphasic Dissolution Data into PBPK Models Abstract Abstract Coupling biorelevant in vitro dissolution with in silico physiological-based pharmacokinetic (PBPK) tools represents a promising method to describe and predict the in vivo performance of drug candidates in formulatio... |
PMC8606766 | core_pubmed_pmc | Phase I study of single agent NIZ985, a recombinant heterodimeric IL-15 agonist, in adult patients with metastatic or unresectable solid tumors | Phase I study of single agent NIZ985, a recombinant heterodimeric IL-15 agonist, in adult patients with metastatic or unresectable solid tumors Abstract Abstract Background NIZ985 is a recombinant heterodimer of physiologically active interleukin (IL-)15 and IL-15 receptor alpha. In preclinical models, NIZ985 promotes ... |
PMC8709266 | core_pubmed_pmc | Preparation and Characterization of Fenofibrate Microparticles with Surface-Active Additives: Application of a Supercritical Fluid-Assisted Spray-Drying Process | Preparation and Characterization of Fenofibrate Microparticles with Surface-Active Additives: Application of a Supercritical Fluid-Assisted Spray-Drying Process Abstract In this study, supercritical fluid-assisted spray-drying (SA-SD) was applied to achieve the micronization of fenofibrate particles possessing surface-... |
PMC6199364 | core_pubmed_pmc | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects | Pharmacokinetics and safety of Enasidenib following single oral doses in Japanese and Caucasian subjects Abstract Abstract The aim of this study was to assess and compare the pharmacokinetics (PK) and safety of Enasidenib in healthy adult male Japanese subjects to healthy adult male Caucasian subjects. This was a phase... |
PMC11062943 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of high-dose isoniazid for the treatment of rifampicin- or multidrug-resistant tuberculosis in Indonesia | Pharmacokinetics and pharmacodynamics of high-dose isoniazid for the treatment of rifampicin- or multidrug-resistant tuberculosis in Indonesia Abstract Abstract Background Pharmacokinetic data on high-dose isoniazid for the treatment of rifampicin-/multidrug-resistant tuberculosis (RR/MDR-TB) are limited. We aimed to d... |
PMC11532403 | core_pubmed_pmc | First-in-human, phase 1 dose-escalation and dose-expansion study of a RET inhibitor SY-5007 in patients with advanced RET -altered solid tumors | First-in-human, phase 1 dose-escalation and dose-expansion study of a RET inhibitor SY-5007 in patients with advanced RET -altered solid tumors Abstract Abstract Oncogenic RET alteration is an important, tissue-agnostic therapeutic target across diverse cancers. We conducted a first-in-human phase 1 study on SY-5007, a... |
PMC9740244 | core_pubmed_pmc | Comparative Pharmacokinetics and Tissue Distribution of M10 and Its Metabolite Myricetin in Normal and Dextran-Sodium-Sulfate-Induced Colitis Mice | Comparative Pharmacokinetics and Tissue Distribution of M10 and Its Metabolite Myricetin in Normal and Dextran-Sodium-Sulfate-Induced Colitis Mice Abstract M10, a novel myricetin derivative, is an anti-inflammatory agent designed for treatment of colitis. Here, we aim to investigate its pharmacokinetic behavior and tis... |
PMC12932851 | core_pubmed_pmc | Pharmacogenomic profiling of ABCB1 and CES1 in atrial fibrillation patients on dabigatran from a multiethnic Malaysian cohort | Pharmacogenomic profiling of ABCB1 and CES1 in atrial fibrillation patients on dabigatran from a multiethnic Malaysian cohort Abstract Abstract Direct oral anticoagulants (DOACs) are preferred for atrial fibrillation (AF) due to their efficacy and safety, though response variabilities raises concerns about fixed-dose r... |
PMC6274096 | core_pubmed_pmc | The Current Case of Quinolones: Synthetic Approaches and Antibacterial Activity | The Current Case of Quinolones: Synthetic Approaches and Antibacterial Activity Abstract Abstract Quinolones are broad-spectrum synthetic antibacterial drugs first obtained during the synthesis of chloroquine. Nalidixic acid, the prototype of quinolones, first became available for clinical consumption in 1962 and was u... |
PMC5813098 | core_pubmed_pmc | Reverse Translation in PBPK and QSP: Going Backwards in Order to Go Forward With Confidence | Reverse Translation in PBPK and QSP: Going Backwards in Order to Go Forward With Confidence Abstract Abstract Significant events have taken place shaping the recent industrialization of physiologically based pharmacokinetic in vitro–in vivo extrapolation (PBPK‐IVIVE) use in drug development. Due to our knowledge gaps a... |
PMC3469233 | core_pubmed_pmc | Oral calcitonin | Oral calcitonin Abstract Abstract Calcitonin is a hormone secreted by the C-cells of the thyroid gland in response to elevations of the plasma calcium level. It reduces bone resorption by inhibiting mature active osteoclasts and increases renal calcium excretion. It is used in the management of postmenopausal osteoporo... |
PMC9894647 | core_pubmed_pmc | Fixed Dose Versus Loose Dose: Analgesic Combinations | Fixed Dose Versus Loose Dose: Analgesic Combinations Abstract Combinations of drugs may be fixed (two or more entities in a single product) or loose (two or more agents taken together but as individual agents) to help address multimechanistic pain. The use of opioids plus nonopioids can result in lower opioid consumpti... |
PMC11631816 | core_pubmed_pmc | Model-informed approach to estimate treatment effect in placebo-controlled clinical trials using an artificial intelligence-based propensity weighting methodology to account for non-specific responses to treatment | Model-informed approach to estimate treatment effect in placebo-controlled clinical trials using an artificial intelligence-based propensity weighting methodology to account for non-specific responses to treatment Abstract Abstract In randomized, placebo controlled clinical trials (RCT) in major depressive disorders (M... |
PMC6026321 | core_pubmed_pmc | Time-resolved hypothalamic open flow micro-perfusion reveals normal leptin transport across the blood–brain barrier in leptin resistant mice | Time-resolved hypothalamic open flow micro-perfusion reveals normal leptin transport across the blood–brain barrier in leptin resistant mice Abstract Objective The inability of leptin to suppress food intake in diet-induced obesity, sometimes referred to as leptin resistance, is associated with several distinct patholo... |
PMC5801568 | core_pubmed_pmc | Liquid chromatography–tandem mass spectrometry for the simultaneous quantitation of ceftriaxone, metronidazole and hydroxymetronidazole in plasma from seriously ill, severely malnourished children | Liquid chromatography–tandem mass spectrometry for the simultaneous quantitation of ceftriaxone, metronidazole and hydroxymetronidazole in plasma from seriously ill, severely malnourished children Abstract Abstract We have developed and validated a novel, sensitive, selective and reproducible reversed-phase high-perfor... |
PMC10254897 | core_pubmed_pmc | Development and Validation of a New LC-MS/MS Bioanalytical Method for the Simultaneous Determination of Levodopa, Levodopa Methyl Ester, and Carbidopa in Human Plasma Samples | Development and Validation of a New LC-MS/MS Bioanalytical Method for the Simultaneous Determination of Levodopa, Levodopa Methyl Ester, and Carbidopa in Human Plasma Samples Abstract Levodopa (L-DOPA) treatment, combined with the administration of dopa-decarboxylase inhibitors (DDCIs), is still the most effective symp... |
PMC6095527 | core_pubmed_pmc | Comparison of the dose-response pharmacodynamic profiles of detemir and glargine in severely obese patients with type 2 diabetes: A single-blind, randomised cross-over trial | Comparison of the dose-response pharmacodynamic profiles of detemir and glargine in severely obese patients with type 2 diabetes: A single-blind, randomised cross-over trial Abstract Abstract Background Despite their widespread use in this population, data on the pharmacodynamic (PD) properties of the insulin analogs d... |
PMC5270297 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modeling of Tumor Size Dynamics in Pembrolizumab‐Treated Advanced Melanoma | Population Pharmacokinetic/Pharmacodynamic Modeling of Tumor Size Dynamics in Pembrolizumab‐Treated Advanced Melanoma Abstract Pembrolizumab is a potent immune‐modulating antibody active in advanced melanoma, as demonstrated in the KEYNOTE‐001, ‐002, and ‐006 studies. Longitudinal tumor size modeling was pursued to qua... |
PMC10993987 | core_pubmed_pmc | XTX301, a Tumor-Activated Interleukin-12 Has the Potential to Widen the Therapeutic Index of IL12 Treatment for Solid Tumors as Evidenced by Preclinical Studies | XTX301, a Tumor-Activated Interleukin-12 Has the Potential to Widen the Therapeutic Index of IL12 Treatment for Solid Tumors as Evidenced by Preclinical Studies Abstract Abstract IL12 is a proinflammatory cytokine, that has shown promising antitumor activity in humans by promoting the recruitment and activation of immu... |
PMC12072221 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Model of Tyrosine Kinase Inhibitors to Predict Target Site Penetration, with PET‐Guided Verification | Physiologically Based Pharmacokinetic Model of Tyrosine Kinase Inhibitors to Predict Target Site Penetration, with PET‐Guided Verification Abstract ABSTRACT Osimertinib, a tyrosine kinase inhibitor (TKI), treats non‐small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) mutations. However, its effi... |
PMC10393866 | core_pubmed_pmc | Oral antimicrobial agents in patients with short bowel syndrome: worth a try! | Oral antimicrobial agents in patients with short bowel syndrome: worth a try! Abstract Abstract Background The use of oral antimicrobial agents in patients with short bowel syndrome (SBS) is challenging due to the changes in gastrointestinal anatomy that may result in diminished absorption and altered drug bioavailabil... |
PMC8405508 | core_pubmed_pmc | Pharmacometric estimation methods for aggregate data, including data simulated from other pharmacometric models | Pharmacometric estimation methods for aggregate data, including data simulated from other pharmacometric models Abstract Abstract Lack of data is an obvious limitation to what can be modelled. However, aggregate data in the form of means and possibly (co)variances, as well as previously published pharmacometric models,... |
PMC11222998 | core_pubmed_pmc | Systematic studies on the kinetic process of 20(S)-protopanaxadiol in rats and dogs: absorption, distribution, metabolism and excretion | Systematic studies on the kinetic process of 20(S)-protopanaxadiol in rats and dogs: absorption, distribution, metabolism and excretion Abstract Abstract Background and Objective Ginseng has been regarded as a precious medicinal herb with miraculous effects in Eastern culture. The primary chemical constituents of ginse... |
PMC11833615 | core_pubmed_pmc | ADME/Tox study and the effect of β-Caryophyllene on the resistant strain of Staphylococcus aureus carrying the QacA/B efflux pump gene | ADME/Tox study and the effect of β-Caryophyllene on the resistant strain of Staphylococcus aureus carrying the QacA/B efflux pump gene Abstract The Gram-positive bacterium Staphylococcus aureus is responsible for causing both community-acquired and healthcare-associated infections, and it exhibits high antibiotic resis... |
PMC7687815 | core_pubmed_pmc | Attenuation of LPS-induced acute lung injury by continentalic acid in rodents through inhibition of inflammatory mediators correlates with increased Nrf2 protein expression | Attenuation of LPS-induced acute lung injury by continentalic acid in rodents through inhibition of inflammatory mediators correlates with increased Nrf2 protein expression Abstract Background Acute lung injury (ALI) together with acute respiratory distress syndrome (ARDS) are associated with high rate of mortality and... |
PMC6290887 | core_pubmed_pmc | Assessment of nivolumab exposure and clinical safety of 480 mg every 4 weeks flat-dosing schedule in patients with cancer | Assessment of nivolumab exposure and clinical safety of 480 mg every 4 weeks flat-dosing schedule in patients with cancer Abstract Abstract Background A nivolumab monotherapy flat-dosing regimen of 480 mg every 4 weeks (Q4W) has been approved in several markets, including the United States, Canada, and European Union, ... |
PMC12194504 | core_pubmed_pmc | Left Ventricular Assist Device Implantation Under Argatroban Anticoagulation in Heparin-Induced Thrombocytopenia: A Literature Review and Clinical Case Presentation | Left Ventricular Assist Device Implantation Under Argatroban Anticoagulation in Heparin-Induced Thrombocytopenia: A Literature Review and Clinical Case Presentation Abstract Abstract This review provides an in-depth analysis of argatroban as an alternative anticoagulant in cardiac surgery, with a focus on its use in pa... |
PMC12869285 | core_pubmed_pmc | Novel pyridine-heterocycle hybrids: synthesis via Hantzsch and Biginelli reactions, docking simulations, and anticancer activity | Novel pyridine-heterocycle hybrids: synthesis via Hantzsch and Biginelli reactions, docking simulations, and anticancer activity Abstract Abstract Cancer is a serious global health issue and remains one of the top causes of death worldwide. To overcome the problems of the existing anticancer drugs in terms of specifici... |
PMC8597174 | core_pubmed_pmc | Single‐ and Multiple‐Dose Pharmacokinetics and Pharmacodynamics of PN‐943, a Gastrointestinal‐Restricted Oral Peptide Antagonist of α4β7, in Healthy Volunteers | Single‐ and Multiple‐Dose Pharmacokinetics and Pharmacodynamics of PN‐943, a Gastrointestinal‐Restricted Oral Peptide Antagonist of α4β7, in Healthy Volunteers Abstract Abstract PN‐943 is an orally stable, gastrointestinal‐restricted peptide that binds specifically to α4ß7 integrin on leukocytes, blocking leukocyte tra... |
PMC4065302 | core_pubmed_pmc | Distinct Prandial and Basal Glucose-Lowering Effects of Insulin Degludec/Insulin Aspart (IDegAsp) at Steady State in Subjects with Type 1 Diabetes Mellitus | Distinct Prandial and Basal Glucose-Lowering Effects of Insulin Degludec/Insulin Aspart (IDegAsp) at Steady State in Subjects with Type 1 Diabetes Mellitus Abstract Introduction/aim Insulin degludec/insulin aspart (IDegAsp) is a soluble co-formulation of long-acting and short-acting insulin analogs. The primary objecti... |
PMC12371011 | core_pubmed_pmc | HLA-B*58:01 genotyping prevalence and the association with allopurinol-induced severe cutaneous adverse reactions: a living systematic review and meta-analysis | HLA-B*58:01 genotyping prevalence and the association with allopurinol-induced severe cutaneous adverse reactions: a living systematic review and meta-analysis Abstract Abstract Evidence on the prevalence of HLA-B*58:01 genotyping and its association with allopurinol-induced severe cutaneous adverse reactions (SCARs) i... |
PMC5992762 | core_pubmed_pmc | A strategy for designing voriconazole dosage regimens to prevent invasive pulmonary aspergillosis based on a cellular pharmacokinetics/pharmacodynamics model | A strategy for designing voriconazole dosage regimens to prevent invasive pulmonary aspergillosis based on a cellular pharmacokinetics/pharmacodynamics model Abstract Abstract Background Invasive pulmonary aspergillosis (IPA) is a life-threatening disease in immunosuppressed patients. Voriconazole is commonly used to p... |
PMC10943190 | core_pubmed_pmc | Development of extended pharmacokinetic models for propofol based on measured blood and brain concentrations | Development of extended pharmacokinetic models for propofol based on measured blood and brain concentrations Abstract Abstract Propofol’s pharmacokinetics have been extensively studied using human blood samples and applied to target-controlled infusion systems; however, information on its concentration in the brain rem... |
PMC4767141 | core_pubmed_pmc | Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen | Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen Abstract WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. We report the discovery and opt... |
PMC12641081 | core_pubmed_pmc | Pharmacomicrobiomics | Pharmacomicrobiomics Abstract Oral medications encounter gut commensal microbes that participate directly and indirectly in drug effects through metabolism, interactions with drug metabolites, or production of substrates that compete with drugs for drug‐metabolizing enzymes, consequently influencing drug pharmacokineti... |
PMC10334253 | core_pubmed_pmc | A phase II study of TAS-117 in patients with advanced solid tumors harboring germline PTEN -inactivating mutations | A phase II study of TAS-117 in patients with advanced solid tumors harboring germline PTEN -inactivating mutations Abstract PTEN acts as a potent tumor suppressor within the PI3K/AKT/mTOR pathway. Germline mutations in the PTEN gene are a hallmark of PTEN hamartoma tumor syndrome, which includes Cowden syndrome, where ... |
PMC8692923 | core_pubmed_pmc | A phase 1, open‐label study to evaluate the drug interaction between islatravir (MK‐8591) and the oral contraceptive levonorgestrel/ethinyl estradiol in healthy adult females | A phase 1, open‐label study to evaluate the drug interaction between islatravir (MK‐8591) and the oral contraceptive levonorgestrel/ethinyl estradiol in healthy adult females Abstract Abstract Introduction Hormonal contraceptives are among the most effective forms of reversible contraception, but many other compounds, ... |
PMC8907708 | core_pubmed_pmc | Solving the Evidence Interpretability Crisis in Health Technology Assessment: A Role for Mechanistic Models? | Solving the Evidence Interpretability Crisis in Health Technology Assessment: A Role for Mechanistic Models? Abstract Abstract Health technology assessment (HTA) aims to be a systematic, transparent, unbiased synthesis of clinical efficacy, safety, and value of medical products (MPs) to help policymakers, payers, clini... |
PMC11266716 | core_pubmed_pmc | Pharmacokinetics of anti- Mycobacterium avium-intracellulare disease drugs in silkworms | Pharmacokinetics of anti- Mycobacterium avium-intracellulare disease drugs in silkworms Abstract Abstract Pulmonary Mycobacterium avium-intracellulare complex (MAC) disease is a typical non-tuberculous mycobacterial infection. The incidence of pulmonary MAC is increasing worldwide. This study aimed to clarify the pharm... |
PMC7154760 | core_pubmed_pmc | Bioavailability and safety of diazepam intranasal solution compared to oral and rectal diazepam in healthy volunteers | Bioavailability and safety of diazepam intranasal solution compared to oral and rectal diazepam in healthy volunteers Abstract Abstract Objective The study assesses the bioavailability of diazepam after intranasal administration (diazepam nasal spray) in healthy volunteers. Comparative agents were diazepam rectal gel, ... |
PMC8905292 | core_pubmed_pmc | IgG-like Bispecific Antibody CD3×EpCAM Generated by Split Intein Against Colorectal Cancer | IgG-like Bispecific Antibody CD3×EpCAM Generated by Split Intein Against Colorectal Cancer Abstract Background: Colorectal cancer is a commonly diagnosed cancer with high mortality worldwide. Postoperative recidivation and metastasis still are the main challenges in clinical treatments. Thus, it is urgent to develop ne... |
PMC4370301 | core_pubmed_pmc | Venovenous haemodiafiltration for the management of dabigatran overdose in intensive care unit | Venovenous haemodiafiltration for the management of dabigatran overdose in intensive care unit Abstract Abstract Dabigatran is a direct thrombin inhibitor indicated for thromboembolism prophylaxis in patients with non-valvular atrial fibrillation. The procedure to manage dabigatran-associated haemorrhages is not well f... |
PMC7289785 | core_pubmed_pmc | Quantification of the endogenous growth hormone and prolactin lowering effects of a somatostatin-dopamine chimera using population PK/PD modeling | Quantification of the endogenous growth hormone and prolactin lowering effects of a somatostatin-dopamine chimera using population PK/PD modeling Abstract A phase 1 clinical trial in healthy male volunteers was conducted with a somatostatin-dopamine chimera (BIM23B065), from which information could be obtained on the c... |
PMC6878041 | core_pubmed_pmc | Meropenem pharmacokinetics during relapsing peritonitis due to ESBL‐producing Enterobacteriaciae in a liver transplant recipient | Meropenem pharmacokinetics during relapsing peritonitis due to ESBL‐producing Enterobacteriaciae in a liver transplant recipient Abstract Abstract We report on an 8‐year‐old girl with Wilson disease who developed three episodes of peritonitis due to extended‐spectrum beta‐lactamase‐producing Escherichia coli after live... |
PMC8761719 | core_pubmed_pmc | Clinical Pharmacokinetics and Pharmacodynamics of the Selective Progesterone Receptor Modulator Vilaprisan: A Comprehensive Overview | Clinical Pharmacokinetics and Pharmacodynamics of the Selective Progesterone Receptor Modulator Vilaprisan: A Comprehensive Overview Abstract Abstract Vilaprisan is a highly potent selective progesterone receptor modulator in development for the treatment of symptomatic uterine fibroids and endometriosis. Its pharmacok... |
PMC6400998 | core_pubmed_pmc | Soy Isoflavone Extract Does Not Increase the Intoxicating Effects of Acute Alcohol Ingestion in Human Volunteers | Soy Isoflavone Extract Does Not Increase the Intoxicating Effects of Acute Alcohol Ingestion in Human Volunteers Abstract Abstract Soy beans contain isoflavones, including daidzein and genistein, with biological activities related to therapeutic effects in reducing osteoporosis, decreasing adverse menopausal manifestat... |
PMC4145254 | core_pubmed_pmc | Persistent pharmacokinetic challenges to pediatric drug development | Persistent pharmacokinetic challenges to pediatric drug development Abstract Abstract The development of new therapeutic agents for the mitigation of pediatric disorders is largely hindered by the inability for investigators to assess pediatric pharmacokinetics (PK) in healthy patients due to substantial safety concern... |
PMC3445513 | core_pubmed_pmc | Pharmacokinetic Analysis of 111 In-Labeled Liposomal Doxorubicin in Murine Glioblastoma after Blood-Brain Barrier Disruption by Focused Ultrasound | Pharmacokinetic Analysis of 111 In-Labeled Liposomal Doxorubicin in Murine Glioblastoma after Blood-Brain Barrier Disruption by Focused Ultrasound Abstract The goal of this study was to evaluate the pharmacokinetics of targeted and untargeted 111 In-doxorubicin liposomes after these have been intravenously administrate... |
PMC10328662 | core_pubmed_pmc | In-silico approach to designing effective antiviral drugs against SARS-CoV-2 and SARS-CoV-1 from reported phytochemicals: a quality improvement study | In-silico approach to designing effective antiviral drugs against SARS-CoV-2 and SARS-CoV-1 from reported phytochemicals: a quality improvement study Abstract Computer-aided drug design by molecular docking, statistical analysis like multiple linear regression (MLR), principal component analysis (PCA), and molecular dy... |
PMC12702241 | core_pubmed_pmc | Methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium infections in children in the Oceania region: review of the epidemiology, antimicrobial availability, treatment, clinical trial and pharmacokinetic data and key evidence gaps | Methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium infections in children in the Oceania region: review of the epidemiology, antimicrobial availability, treatment, clinical trial and pharmacokinetic data and key evidence gaps Abstract Summary Antimicrobial resistance poses a signi... |
PMC11586560 | core_pubmed_pmc | The effect of concurrent clopidogrel and omeprazole administration on clopidogrel metabolism and platelet function in healthy cats | The effect of concurrent clopidogrel and omeprazole administration on clopidogrel metabolism and platelet function in healthy cats Abstract Abstract Background Some studies in humans show that the concurrent use of clopidogrel and omeprazole decreases plasma clopidogrel active metabolite (CAM) concentrations and clopid... |
PMC10719454 | core_pubmed_pmc | Academia and industry agreement on a feasibility tool for first‐time‐in‐human clinical trial units | Academia and industry agreement on a feasibility tool for first‐time‐in‐human clinical trial units Abstract Abstract First‐time‐in‐human (FTIH) trials are designed to generate information on the safety, tolerability, as well as the pharmacokinetic and pharmacodynamics profile of new drugs. To ensure the safety of parti... |
PMC9697873 | core_pubmed_pmc | Construction and Evaluation of a Novel Organic Anion Transporter 1/3 CRISPR/Cas9 Double-Knockout Rat Model | Construction and Evaluation of a Novel Organic Anion Transporter 1/3 CRISPR/Cas9 Double-Knockout Rat Model Abstract Abstract Background: Organic anion transporter 1 (OAT1) and OAT3 have an overlapping spectrum of substrates such that one can exert a compensatory effect when the other is dysfunctional. As a result, the ... |
PMC8184478 | core_pubmed_pmc | Wuzhi capsule increased systemic exposure to methotrexate by inhibiting the expression of OAT1/3 and P-gp | Wuzhi capsule increased systemic exposure to methotrexate by inhibiting the expression of OAT1/3 and P-gp Abstract Abstract Background Methotrexate (MTX) is an important anticancer agent and immunosuppressant with a narrow therapeutic window. Wuzhi capsule (WZC) is an extract of Schisandra which is widely used to treat... |
PMC6963693 | core_pubmed_pmc | Phage-Antibiotic Combination Treatments: Antagonistic Impacts of Antibiotics on the Pharmacodynamics of Phage Therapy? | Phage-Antibiotic Combination Treatments: Antagonistic Impacts of Antibiotics on the Pharmacodynamics of Phage Therapy? Abstract Bacteria can evolve resistance to antibiotics. Even without changing genetically, bacteria also can display tolerance to antibiotic treatments. Many antibiotics are also broadly acting, as can... |
PMC12126168 | core_pubmed_pmc | Design and Synthesis of Novel 5,6,7,8-Tetrahydropyrido[2,3- D ]pyrimidine Derivatives as VCP/p97 Inhibitors for the Treatment of Acute Myeloid Leukemia (AML) | Design and Synthesis of Novel 5,6,7,8-Tetrahydropyrido[2,3- D ]pyrimidine Derivatives as VCP/p97 Inhibitors for the Treatment of Acute Myeloid Leukemia (AML) Abstract Abstract Background VCP/p97 plays an important role in endoplasmic reticulum related degradation pathways, and inhibition of p97 was shown to induce ER s... |
PMC7822411 | core_pubmed_pmc | Pharmacokinetics of Mephedrone Enantiomers in Whole Blood after a Controlled Intranasal Administration to Healthy Human Volunteers | Pharmacokinetics of Mephedrone Enantiomers in Whole Blood after a Controlled Intranasal Administration to Healthy Human Volunteers Abstract Abstract Mephedrone, which is one of the most popular synthetic cathinones, has one chiral centre and thus exists as two enantiomers: R -(+)-mephedrone and S -(−)-mephedrone. There... |
PMC9673116 | core_pubmed_pmc | Chicken xenobiotic receptor upregulates the BCRP/ABCG2 transporter | Chicken xenobiotic receptor upregulates the BCRP/ABCG2 transporter Abstract The transporter breast cancer resistance protein ( BCRP , encoded by ABCG2) influences the bioavailability and elimination of numerous substrate drugs during clinical therapy. The xenobiotic-sensing nuclear receptors pregnane X receptor ( PXR )... |
PMC9686913 | core_pubmed_pmc | Pharmacokinetics of Vancomycin among Patients with Chemotherapy-Associated Febrile Neutropenia: Which Would Be the Best Dosing to Obtain Appropriate Exposure? | Pharmacokinetics of Vancomycin among Patients with Chemotherapy-Associated Febrile Neutropenia: Which Would Be the Best Dosing to Obtain Appropriate Exposure? Abstract Abstract Previous research has determined that the required doses for treating febrile neutropenia with vancomycin are higher than the doses used conven... |
PMC12966213 | core_pubmed_pmc | NFE2L2 rs35652124C>T polymorphism predicts Grade 4 neutropenia in esophageal cancer patients treated with docetaxel, cisplatin, and fluorouracil chemotherapy: results from exploratory and validation cohorts | NFE2L2 rs35652124C>T polymorphism predicts Grade 4 neutropenia in esophageal cancer patients treated with docetaxel, cisplatin, and fluorouracil chemotherapy: results from exploratory and validation cohorts Abstract Purpose Chemotherapy-induced neutropenia is a serious adverse event. Combination chemotherapy with docet... |
PMC6791658 | core_pubmed_pmc | Future Directions of Pharmacovigilance Studies Using Electronic Medical Recording and Human Genetic Databases | Future Directions of Pharmacovigilance Studies Using Electronic Medical Recording and Human Genetic Databases Abstract Adverse drug reactions (ADRs) constitute key factors in determining successful medication therapy in clinical situations. Integrative analysis of electronic medical record (EMR) data and use of proper ... |
PMC12845219 | core_pubmed_pmc | Old Drug, New Science: Metformin and the Future of Pharmaceutics | Old Drug, New Science: Metformin and the Future of Pharmaceutics Abstract Metformin, a 60-year-old biguanide and cornerstone of type 2 diabetes therapy, continues to challenge and inspire modern pharmaceutical science. Despite its chemical simplicity, metformin displays highly complex pharmacokinetic and pharmacodynami... |
PMC6259217 | core_pubmed_pmc | The Pharmacokinetics of Raloxifene and Its Interaction with Apigenin in Rat | The Pharmacokinetics of Raloxifene and Its Interaction with Apigenin in Rat Abstract Abstract Purpose : Raloxifene is a selective estrogen receptor modulator which is structurally similar to tamoxifen. As flavonoids can interact with raloxifene in vitro , we evaluated the in vivo pharmacokinetics of raloxifene in rats ... |
PMC10612570 | core_pubmed_pmc | A biomimetic chip to assess subcutaneous bioavailability of monoclonal antibodies in humans | A biomimetic chip to assess subcutaneous bioavailability of monoclonal antibodies in humans Abstract Abstract Subcutaneous (subQ) injection is a common route for delivering biotherapeutics, wherein pharmacokinetics is largely influenced by drug transport in a complex subQ tissue microenvironment. The selection of good ... |
PMC4767496 | core_pubmed_pmc | Phase 1b study of lenvatinib (E7080) in combination with temozolomide for treatment of advanced melanoma | Phase 1b study of lenvatinib (E7080) in combination with temozolomide for treatment of advanced melanoma Abstract Objective and Methods In this phase 1b study, patients with stage 4 or unresectable stage 3 melanoma were treated with escalating doses of lenvatinib (once daily) and temozolomide (TMZ) (days 1–5) in 28-day... |
PMC5538706 | core_pubmed_pmc | Design of theranostic nanomedicine (II): synthesis and physicochemical properties of a biocompatible polyphosphazene–docetaxel conjugate | Design of theranostic nanomedicine (II): synthesis and physicochemical properties of a biocompatible polyphosphazene–docetaxel conjugate Abstract To prepare an efficient theranostic polyphosphazene–docetaxel (DTX) conjugate, a new drug delivery system was designed by grafting a multifunctional lysine ethylester (LysOEt... |
PMC3364125 | core_pubmed_pmc | Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study | Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study Abstract Abstract Background: In a phase I dose-escalation study, regorafenib demonstrated tolerability and antitumour activity in solid tumour patients. The study was expanded to focus on patients with metastatic colorectal cancer (CRC). Methods:... |
PMC9941671 | core_pubmed_pmc | Formulation development of lipid polymer hybrid nanoparticles of doxorubicin and its in-vitro, in-vivo and computational evaluation | Formulation development of lipid polymer hybrid nanoparticles of doxorubicin and its in-vitro, in-vivo and computational evaluation Abstract Abstract The purpose of this study was to assess the parameters of doxorubicin (DOX) loaded lipid polymer hybrid nanoparticles (LPHNs) formulation development, and then the bioava... |
PMC9025106 | core_pubmed_pmc | Local Anesthetic Plasma Concentrations as a Valuable Tool to Confirm the Diagnosis of Local Anesthetic Systemic Toxicity? A Report of 10 Years of Experience | Local Anesthetic Plasma Concentrations as a Valuable Tool to Confirm the Diagnosis of Local Anesthetic Systemic Toxicity? A Report of 10 Years of Experience Abstract Background: Local anesthetic systemic toxicity (LAST) has been reported as a serious complication of local anesthetic (LA) peripheral injection. The signs... |
PMC8656417 | core_pubmed_pmc | The Monte Carlo Simulation of Three Antimicrobials for Empiric Treatment of Adult Bloodstream Infections With Carbapenem-Resistant Enterobacterales in China | The Monte Carlo Simulation of Three Antimicrobials for Empiric Treatment of Adult Bloodstream Infections With Carbapenem-Resistant Enterobacterales in China Abstract Introduction: The aim of this study was to predict and evaluate three antimicrobials for treatment of adult bloodstream infections (BSI) with carbapenem-r... |
PMC5786797 | core_pubmed_pmc | Antibacterial and Sterilizing Effect of Benzylpenicillin in Tuberculosis | Antibacterial and Sterilizing Effect of Benzylpenicillin in Tuberculosis Abstract ABSTRACT The modern chemotherapy era started with Fleming's discovery of benzylpenicillin. He demonstrated that benzylpenicillin did not kill Mycobacterium tuberculosis . In this study, we found that >64 mg/liter of static benzylpenicilli... |
PMC11456271 | core_pubmed_pmc | A Comprehensive Review of Coptidis Rhizoma and Magnoliae Officinalis Cortex Drug Pair and Their Chemical Composition, Pharmacological Effects and Pharmacokinetics Analysis | A Comprehensive Review of Coptidis Rhizoma and Magnoliae Officinalis Cortex Drug Pair and Their Chemical Composition, Pharmacological Effects and Pharmacokinetics Analysis Abstract Abstract Herbal pairs are unique combinations of two relatively fixed herbs that are used in clinical practice. This is the most fundamenta... |
PMC10376546 | core_pubmed_pmc | Isavuconazole Exposure in Critically Ill Patients Treated with Extracorporeal Membrane Oxygenation: Two Case Reports and a Narrative Literature Review | Isavuconazole Exposure in Critically Ill Patients Treated with Extracorporeal Membrane Oxygenation: Two Case Reports and a Narrative Literature Review Abstract Abstract Effective dosing of isavuconazole in patients supported by extracorporeal membrane oxygenation (ECMO) is important due to the role of isavuconazole as ... |
PMC5702904 | core_pubmed_pmc | Cell Signaling Model Connects Vorinostat Pharmacokinetics and Tumor Growth Response in Multiple Myeloma Xenografts | Cell Signaling Model Connects Vorinostat Pharmacokinetics and Tumor Growth Response in Multiple Myeloma Xenografts Abstract Abstract Multiple myeloma is a fatal hematological malignancy with high rates of drug resistance and relapse. Vorinostat, a histone deacetylase inhibitor, has shown promise in enhancing efficacy w... |
PMC5762321 | core_pubmed_pmc | Indomethacin-based stimuli-responsive micelles combined with paclitaxel to overcome multidrug resistance | Indomethacin-based stimuli-responsive micelles combined with paclitaxel to overcome multidrug resistance Abstract Abstract Development of multidrug resistance against antitumor agents is a major limiting factor for the successful chemotherapy. Currently, both amphiphilic polymeric micelles and chemosensitizers have bee... |
PMC8249799 | core_pubmed_pmc | Pharmacokinetics of Acetaminophen and Metformin Hydrochloride in Rats After Exposure to Simulated High Altitude Hypoxia | Pharmacokinetics of Acetaminophen and Metformin Hydrochloride in Rats After Exposure to Simulated High Altitude Hypoxia Abstract The pharmacokinetic characteristics of drugs were altered under high altitude hypoxia, thereby affecting the absorption, distribution, metabolism, and excretion of drug. However, there are fe... |
PMC3251867 | core_pubmed_pmc | Phase I study of the histone deacetylase inhibitor entinostat in combination with 13- cis retinoic acid in patients with solid tumours | Phase I study of the histone deacetylase inhibitor entinostat in combination with 13- cis retinoic acid in patients with solid tumours Abstract Abstract Background: Preclinical studies suggest that histone deacetylase (HDAC) inhibitors may restore tumour sensitivity to retinoids. The objective of this study was to dete... |
PMC9305486 | core_pubmed_pmc | Common UGT1A9 polymorphisms do not have a clinically meaningful impact on the apparent oral clearance of dapagliflozin in type 2 diabetes mellitus | Common UGT1A9 polymorphisms do not have a clinically meaningful impact on the apparent oral clearance of dapagliflozin in type 2 diabetes mellitus Abstract Abstract Dapagliflozin is an inhibitor of human renal sodium‐glucose cotransporter 2 (SGLT2), first approved for the treatment of type 2 diabetes mellitus (T2DM). D... |
PMC8894159 | core_pubmed_pmc | Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers | Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers Abstract Purpose Evaluate the pharmacodynamics, pharmacokinetics, and safety of paltusotine, an orally bioavailable, nonpeptide, somatostatin receptor subtype 2 (SST2) agonist being developed for the tre... |
PMC10303028 | core_pubmed_pmc | The Real-World Clinical Outcomes of Favipiravir Treatment with Telemedicine Monitoring in Preventing Disease Progression in Mild to Moderate COVID-19 Patients; A Retrospective Cohort Study | The Real-World Clinical Outcomes of Favipiravir Treatment with Telemedicine Monitoring in Preventing Disease Progression in Mild to Moderate COVID-19 Patients; A Retrospective Cohort Study Abstract Background : Favipiravir has complex pharmacokinetics, and varied efficacy has been reported in treating COVID-19. Telehea... |
PMC7725558 | core_pubmed_pmc | Material Basis of the Difference between Hedysari Radix and Honey-Processed Hedysari Radix in Buzhong Yiqi | Material Basis of the Difference between Hedysari Radix and Honey-Processed Hedysari Radix in Buzhong Yiqi Abstract Abstract Objective To compare the changes of chemical components of Hedysari Radix (HR) before and after honey-processing, and to explore the material basis of the difference between HR and honey-processe... |
PMC6852510 | core_pubmed_pmc | The influence of bariatric surgery on oral drug bioavailability in patients with obesity: A systematic review | The influence of bariatric surgery on oral drug bioavailability in patients with obesity: A systematic review Abstract Summary Anatomical changes in the gastrointestinal tract and subsequent weight loss may influence drug disposition and thus drug dosing following bariatric surgery. This review systematically examines ... |
PMC4468340 | core_pubmed_pmc | A quasi-quantitative dual multiplexed immunoblot method to simultaneously analyze ATM and H2AX Phosphorylation in human peripheral blood mononuclear cells | A quasi-quantitative dual multiplexed immunoblot method to simultaneously analyze ATM and H2AX Phosphorylation in human peripheral blood mononuclear cells Abstract Pharmacologic inhibition of DNA repair may increase the efficacy of many cytotoxic cancer agents. Inhibitors of DNA repair enzymes including APE1, ATM, ATR,... |
PMC8257053 | core_pubmed_pmc | Rufinamide-Loaded Chitosan Nanoparticles in Xyloglucan-Based Thermoresponsive In Situ Gel for Direct Nose to Brain Delivery | Rufinamide-Loaded Chitosan Nanoparticles in Xyloglucan-Based Thermoresponsive In Situ Gel for Direct Nose to Brain Delivery Abstract In 2004, the US FDA approved Rufinamide, an anti-epileptic drug under the brand name Banzel ® . In 2015, Banzel ® received approval for its use in pediatric patients (ages 1–4 years). Ruf... |
PMC9817100 | core_pubmed_pmc | Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132 | Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132 Abstract Abstract Purpose The aim of this study was to improve the intratumoral accumulation of an antibody–drug conjugate (ADC) and minimize its off-target t... |
PMC8305961 | core_pubmed_pmc | Optimizing Antimicrobial Drug Dosing in Critically Ill Patients | Optimizing Antimicrobial Drug Dosing in Critically Ill Patients Abstract A fundamental step in the successful management of sepsis and septic shock is early empiric antimicrobial therapy. However, for this to be effective, several decisions must be addressed simultaneously: (1) antimicrobial choices should be adequate,... |
PMC9400884 | core_pubmed_pmc | Supramolecular Rotaxane‐Based Multi‐Modal Probes for Cancer Biomarker Imaging ** | Supramolecular Rotaxane‐Based Multi‐Modal Probes for Cancer Biomarker Imaging ** Abstract Abstract Mechanically interlocked molecules present opportunities to construct therapeutic drugs and diagnostic imaging agents but harnessing supramolecular chemistry to make biologically active probes in water is a challenge. Her... |
PMC3085302 | core_pubmed_pmc | Perspectives on the Role of Fospropofol in the Monitored Anesthesia Care Setting | Perspectives on the Role of Fospropofol in the Monitored Anesthesia Care Setting Abstract Monitored anesthesia care (MAC) is a safe, effective, and appropriate form of anesthesia for many minor surgical procedures. The proliferation of outpatient procedures has heightened interest in MAC sedation agents. Among the most... |
PMC9246587 | core_pubmed_pmc | Pharmacokinetics of Veratramine and Jervine from Alcohol Extracts of Radix Veratri | Pharmacokinetics of Veratramine and Jervine from Alcohol Extracts of Radix Veratri Abstract Abstract Background Chinese Materia Medica and Jiangsu New Medical College record that Radix Veratri root is Liliaceae Veratrum taliense Loses. f. and the root of Veratrum stenophyllum Diels . According to traditional Chinese me... |
PMC6100004 | core_pubmed_pmc | Modulation of Rat Hepatic CYP1A and 2C Activity by Honokiol and Magnolol: Differential Effects on Phenacetin and Diclofenac Pharmacokinetics In Vivo | Modulation of Rat Hepatic CYP1A and 2C Activity by Honokiol and Magnolol: Differential Effects on Phenacetin and Diclofenac Pharmacokinetics In Vivo Abstract Honokiol (2-(4-hydroxy-3-prop-2-enyl-phenyl)-4-prop-2-enyl-phenol) and magnolol (4-Allyl-2-(5-allyl-2-hydroxy-phenyl)phenol) are the major active polyphenol const... |
PMC8841266 | core_pubmed_pmc | Remimazolam: pharmacological characteristics and clinical applications in anesthesiology | Remimazolam: pharmacological characteristics and clinical applications in anesthesiology Abstract Abstract A novel ultra-short-acting benzodiazepine (BDZ), remimazolam (CNS 7056), has been designed by ‘soft drug’ development to achieve a better sedative profile than that of the current drugs. Notably, the esterase link... |
PMC12910649 | core_pubmed_pmc | Optimizing the Antibiotic Potency and Metabolic Stability of Pyridomycin Using a Semisynthetic Approach | Optimizing the Antibiotic Potency and Metabolic Stability of Pyridomycin Using a Semisynthetic Approach Abstract Pyridomycin is a natural product with potent activity against Mycobacterium tuberculosis ( Mtb ), acting through direct inhibition of the fatty acid synthesis enzyme InhA. As a direct inhibitor, pyridomycin ... |
PMC7670640 | core_pubmed_pmc | Phase I evaluation of the safety, tolerability, and pharmacokinetics of GSK3640254, a next‐generation HIV‐1 maturation inhibitor | Phase I evaluation of the safety, tolerability, and pharmacokinetics of GSK3640254, a next‐generation HIV‐1 maturation inhibitor Abstract Abstract Despite advances in HIV‐1 management with antiretroviral therapy, drug resistance and toxicities with multidrug regimens can result in treatment failure. Hence, there is a c... |
PMC12501271 | core_pubmed_pmc | Comparing neutralizing antibody activity over time between naïve and convalesced COVID-19 vaccinated individuals | Comparing neutralizing antibody activity over time between naïve and convalesced COVID-19 vaccinated individuals Abstract Abstract Longitudinal data comprised of neutralizing antibody (NAb) activity measurements from subjects who received COVID-19 vaccinations were collected between November 2020 and April 2022. To det... |
PMC12706425 | core_pubmed_pmc | Nipocalimab Dose Selection in Generalized Myasthenia Gravis | Nipocalimab Dose Selection in Generalized Myasthenia Gravis Abstract ABSTRACT Nipocalimab is a fully human immunoglobulin G (IgG)1 monoclonal antibody (mAb) designed to selectively block the IgG binding site of neonatal fragment crystallizable receptor (FcRn) to inhibit IgG recycling and decrease circulating IgG, inclu... |
PMC12065759 | core_pubmed_pmc | Beyond the linear model in concentration-QT analysis | Beyond the linear model in concentration-QT analysis Abstract Abstract The white-paper regression model is the standard method for assessing QT liability of drugs. The quantity of interest, placebo-corrected QTc change from baseline (ΔΔQTc) with corresponding confidence interval (CI), is derived from the difference in ... |
PMC10106309 | core_pubmed_pmc | Pharmacokinetic Interactions Between Bazedoxifene and Cholecalciferol: An Open-Label, Randomized, Crossover Study in Healthy Male Volunteers | Pharmacokinetic Interactions Between Bazedoxifene and Cholecalciferol: An Open-Label, Randomized, Crossover Study in Healthy Male Volunteers Abstract Purpose The combined administration of bazedoxifene, a tissue-selective estrogen receptor modulator, and cholecalciferol can be a promising therapeutic option for postmen... |
PMC12161285 | core_pubmed_pmc | Muscular and Renal Safety of Ticagrelor with High-Intensity Statins: Retrospective Cohort Findings | Muscular and Renal Safety of Ticagrelor with High-Intensity Statins: Retrospective Cohort Findings Abstract Abstract Introduction Ticagrelor is a widely used antiplatelet agent approved in over 70 countries, including the European Union and the United States, for reducing thrombotic events in patients with acute corona... |
PMC6735388 | core_pubmed_pmc | Evaluation of novel formulations for transarterial chemoembolization: combining elements of Lipiodol emulsions with Drug-eluting Beads | Evaluation of novel formulations for transarterial chemoembolization: combining elements of Lipiodol emulsions with Drug-eluting Beads Abstract There are currently two methods widely used in clinical practice to perform transarterial chemoembolization (TACE). One is based on mixing an aqueous drug with an iodized oil (... |
PMC9816204 | core_pubmed_pmc | Practical application of the interim internal threshold of toxicological concern (iTTC): a case study based on clinical data | Practical application of the interim internal threshold of toxicological concern (iTTC): a case study based on clinical data Abstract Abstract We present a case study that provides a practical step-by-step example of how the internal Threshold of Toxicological Concern (iTTC) can be used as a tool to refine a TTC-based ... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.