Articles with "active metabolite" as a keyword



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Biophysical interaction of temozolomide and its active metabolite with biomembrane models: The relevance of drug‐membrane interaction for Glioblastoma Multiforme therapy

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Published in 2019 at "European Journal of Pharmaceutics and Biopharmaceutics"

DOI: 10.1016/j.ejpb.2019.01.015

Abstract: Graphical abstract Figure. No Caption available. ABSTRACT Temozolomide (TMZ) is the first‐line treatment for Glioblastoma Multiforme (GBM). After administration, TMZ is rapidly converted into its active metabolite (MTIC). However, its pharmacological activity is reduced due… read more here.

Keywords: active metabolite; biomembrane models; glioblastoma multiforme; drug ... See more keywords
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Effects of norquetiapine, the active metabolite of quetiapine, on cloned hERG potassium channels

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Published in 2018 at "Neuroscience Letters"

DOI: 10.1016/j.neulet.2017.11.029

Abstract: Quetiapine is an atypical antipsychotic drug that is widely used for the treatment of schizophrenia. It is mainly metabolized by a cytochrome P450 system in the liver. Norquetiapine is a major active metabolite in humans… read more here.

Keywords: herg current; active metabolite; effects norquetiapine; block ... See more keywords
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Decoy peptide targeted to Toll-IL-1R domain inhibits LPS and TLR4-active metabolite morphine-3 glucuronide sensitization of sensory neurons

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Published in 2017 at "Scientific Reports"

DOI: 10.1038/s41598-017-03447-9

Abstract: Accumulating evidence indicates that Toll-like receptor (TLR) signaling adapter protein interactions with Toll/Interleukin-1 Receptor (TIR) domains present in sensory neurons may modulate neuropathic pain states. Following ligand interaction with TLRs, TIR serves to both initiate… read more here.

Keywords: active metabolite; decoy peptide; tlr4 active; tlr ... See more keywords
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A novel LC-MS/MS method for simultaneous estimation of acalabrutinib and its active metabolite acalabrutinib M27 in human plasma and application to a human pharmacokinetic study

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Published in 2022 at "RSC Advances"

DOI: 10.1039/d1ra09026g

Abstract: A simple, specific, selective and accurate bioanalytical method was developed and validated for simultaneous estimation of acalabrutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Deuterated analogs of both the… read more here.

Keywords: human plasma; acalabrutinib active; estimation acalabrutinib; active metabolite ... See more keywords
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Dried plasma spot assay for sunitinib and its active metabolite by high performance liquid chromatography tandem mass spectrometry: 547P

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Published in 2017 at "Annals of Oncology"

DOI: 10.1093/annonc/mdx678.004

Abstract: plasma protein-A (PAPP-A) is a metalloproteinase that cleaves insulin-like growth factor 1 (IGF-1) from a circulating complex formed with insulin-like growth factor binding protein 4 (IGFBP4). Increased bioavailability of IGF1 subsequently impacts on tumour biology.… read more here.

Keywords: active metabolite; dried plasma; sunitinib active; plasma spot ... See more keywords
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Application of a Validated RP-HPLC Method in Solubility and Dissolution Testing for Simultaneous Estimation of Diacerein and Its Active Metabolite Rhein in Presence of Coformers in the Eutectic Tablet Formulation.

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Published in 2020 at "Journal of chromatographic science"

DOI: 10.1093/chromsci/bmaa109

Abstract: The present study aimed to develop and validate a novel reversed-phase high-performance liquid chromatography method for simultaneous estimation of Diacerein (DIA) and Rhein (Rh, alkaline degradation product and active metabolite) in the presence of various… read more here.

Keywords: active metabolite; presence; simultaneous estimation; method ... See more keywords
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A Sensitive and Rapid LC-MS-MS Method for Simultaneous Determination of Propafenone and Its Active Metabolite 5-Hydroxypropafenone in Human Plasma and Its Application in a Pharmacokinetic Study.

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Published in 2017 at "Journal of chromatographic science"

DOI: 10.1093/chromsci/bmx049

Abstract: A simple and rapid high-performance liquid chromatography tandem mass spectrometry method for the determination of propafenone (PPF) and its active metabolite 5-hydroxypropafenone (5-OHP) in human plasma was developed and validated. This new method was linear… read more here.

Keywords: active metabolite; plasma; human plasma; method ... See more keywords
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Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects

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Published in 2017 at "British Journal of Clinical Pharmacology"

DOI: 10.1111/bcp.13379

Abstract: AIMS Based on in vitro data, there is evidence to suggest that cytochrome P450 (CYP) 2C8 is involved in the metabolism of selexipag and its active metabolite, ACT-333679. The present study evaluated the possible pharmacokinetic… read more here.

Keywords: act 333679; rifampicin; selexipag active; active metabolite ... See more keywords
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Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects

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Published in 2020 at "British Journal of Clinical Pharmacology"

DOI: 10.1111/bcp.14365

Abstract: Selexipag is a prostacyclin receptor agonist approved for the treatment of pulmonary arterial hypertension. Cytochrome P450 (CYP) 2C8 is involved in the metabolism of selexipag and its active metabolite, ACT‐333679. This study evaluated the interaction… read more here.

Keywords: selexipag; active metabolite; cyp2c8 inhibitor; clopidogrel cyp2c8 ... See more keywords
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Cytochrome P450–Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol

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Published in 2021 at "Drug Metabolism and Disposition"

DOI: 10.1124/dmd.120.000350

Abstract: Cannabidiol (CBD) is a naturally occurring nonpsychotoxic phytocannabinoid that has gained increasing attention as a popular consumer product and for its use in Food and Drug Administration–approved Epidiolex (CBD oral solution) for the treatment of… read more here.

Keywords: active metabolite; cbd; metabolism; cbd metabolism ... See more keywords
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Assessment of exposure risk of irinotecan and its active metabolite, SN-38, through perspiration during chemotherapy

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Published in 2019 at "Journal of Oncology Pharmacy Practice"

DOI: 10.1177/1078155218769136

Abstract: Background Irinotecan (CPT-11) is the key drug used in chemotherapy for many malignant tumors. CPT-11 has cholinergic activity and induces perspiration during intravenous administration. In this study, concentrations of CPT-11 and its active metabolite, SN-38,… read more here.

Keywords: active metabolite; perspiration; risk; sweat ... See more keywords