Ultra‐Fast UPLC‐MS/MS Method for the Ripretinib Quantification in the HLMs Matrix With Metabolic Stability Assessment: In‐Silico Study for Toxic Alerts and the Metabolic Lability
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DOI: 10.1002/ardp.70130
Abstract: Ripretinib (QINLOCK) is a broad‐spectrum, orally‐administered, switch‐controlled kinase inhibitor that got FDA approval in May 2020 for the treatment of advanced gastrointestinal stromal tumors (GIST) in adult patients who have formerly had treatment with three or… read more here.
Keywords: hlms matrix; stability; metabolic stability; silico ... See more keywords
Monocarbonyl curcuminoids as antituberculosis agents with their moderate in‐vitro metabolic stability on human liver microsomes
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.22754
Abstract: Tuberculosis, an airborne infectious disease, results in a high morbidity and mortality rate. The continuous emergence of TB resistance strains including MDR (multidrug‐resistant tuberculosis), XDR (extensive drug‐resistant tuberculosis), and especially TDR (totally drug‐resistant tuberculosis) is… read more here.
Keywords: vitro metabolic; metabolic stability; monocarbonyl curcuminoids; tuberculosis ... See more keywords
Application of MetMax™ pooled donor human hepatocytes in a higher throughput assay for human hepatic metabolic stability screening
Sign Up to like & getrecommendations! Published in 2018 at "Drug Metabolism and Pharmacokinetics"
DOI: 10.1016/j.dmpk.2017.11.208
Abstract: • Both MetMaxTM and Intact Human Hepatocytes yielded data comparable to clinical systemic clearance One interesting finding was that MetMaxTM hepatocytes were superior to pooled cryopreserved human hepatocytes in the evaluation of afatinib, a drug… read more here.
Keywords: stability screening; metabolic stability; pooled donor; drug ... See more keywords
Tetrazolylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
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DOI: 10.1016/j.ejmech.2018.10.021
Abstract: A series of derivatives of 1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one (3) and 1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one (4) was synthesized and tested for fatty acid amide hydrolase (FAAH) inhibitory potency and phase I metabolic stability. Introduction of certain substituents like 4-chlorophenyl, 4-methoxycarbonylphenyl and… read more here.
Keywords: acid amide; metabolic stability; fatty acid; amide hydrolase ... See more keywords
Minor chemical modifications of the aminosteroid derivative RM-581 lead to major impact on its anticancer activity, metabolic stability and aqueous solubility.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111990
Abstract: The aminosteroid (AM) RM-581 is built around a mestranol backbone and has recently emerged as this family's lead candidate, showing in vitro and in vivo potency over different types of cancer, including high fatality pancreatic cancer. To… read more here.
Keywords: cancer; activity; metabolic stability; anticancer activity ... See more keywords
Synthesis of 17β-hydroxysteroid dehydrogenase type 10 steroidal inhibitors: Selectivity, metabolic stability and enhanced potency.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112909
Abstract: 17beta-Hydroxysteroid dehydrogenase type 10 (17β-HSD10) is the only mitochondrial member of 17β-HSD family. This enzyme can oxidize estradiol (E2) into estrone (E1), thus reducing concentration of this neuroprotective steroid. Since 17β-HSD10 possesses properties that suggest… read more here.
Keywords: steroidal; hydroxysteroid dehydrogenase; metabolic stability; dehydrogenase type ... See more keywords
Natural Amino Acid-Bearing Carbamate Prodrugs of Daidzein Increase Water Solubility and Improve Phase II Metabolic Stability for Enhanced Oral Bioavailability.
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DOI: 10.1021/acs.jafc.4c01251
Abstract: Daidzein (DAN) is an isoflavone, and it is often found in its natural form in soybean and food supplements. DAN has poor bioavailability owing to its extremely low water solubility and first-pass metabolism. Herein, we… read more here.
Keywords: water solubility; metabolic stability; water; amino acid ... See more keywords
An Ultrafast UPLC‐MS/MS Approach for Determining the In Vitro Metabolic Stability of Duvelisib in the HLMs: In Silico Screening for Metabolic Lability, ADME Features, and DEREK Alerts
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DOI: 10.1155/ianc/9508534
Abstract: Duvelisib (COPIKTRA, Pfizer) is a prescription medication indicated for people with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) who have received at least two previous treatments that were ineffective or have ceased to… read more here.
Keywords: stability; metabolic stability; metabolic lability; uplc approach ... See more keywords
Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability
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DOI: 10.1371/journal.pone.0214598
Abstract: Dacomitinib (DMB) is a second-generation irreversible tyrosine kinase inhibitor (TKI) that is claimed to overcome the disadvantages of the resistance reported for first-line epidermal growth factor receptor (EGFR) TKIs. Towards the end of 2018, the… read more here.
Keywords: validated assay; metabolic stability; kinase inhibitor; quantification ... See more keywords
Metabolic Stability Assessment of Larotrectinib Using Liquid Chromatography Tandem Mass Spectrometry
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DOI: 10.2147/dddt.s235934
Abstract: Introduction Larotrectinib (VITRAKVI) is an orally potent tropomyosin receptor kinase (Trk) inhibitor that acts by competitive inhibition of all corresponding receptor kinases. It demonstrated a marked response rate (75%) and robust anticancer activity in Trk… read more here.
Keywords: metabolic stability; larotrectinib using; assessment larotrectinib; stability ... See more keywords
Metabolism of Peptide Drugs and Strategies to Improve their Metabolic Stability.
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DOI: 10.2174/1389200219666180628171531
Abstract: BACKGROUND Despite the therapeutic use of peptides is limited because of their metabolism in vivo, there are no systematic reviews explaining degradation of peptides by peptidases. This review summarizes peptidases present in the tissues and… read more here.
Keywords: improve metabolic; metabolic stability; metabolism; peptide drugs ... See more keywords