Spectrofluorimetric Method for Determination of Letrozole: Analytical Applications to Brain Tissue Samples and Alkaline Degradation Kinetic Study

El-Kosasy, Amira M.; Rahman, Mona Hamdy Abdel; Abdelaal, Sarah H.

doi:10.1007/s10812-019-00905-2

Cited by 3 publications

(1 citation statement)

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“…The chromatographic approach was successfully applied using different detector systems such as UV/Vis, fluorescence, and mass spectroscopy 5 , 8–10 . Spectroscopic methodologies were also used for assaying the drug in pharmaceutical formulations 11–13 .…”

Section: Introductionmentioning

confidence: 99%

Interaction of letrozole and its degradation products with aromatase: chemometric assessment of kinetics and structure-based binding validation

Luca

Occhiuzzi

Rizzuti

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

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Letrozole is one of the most prescribed drugs for the treatment of breast cancer in post-menopausal women, and it is endowed with selective peripheral aromatase inhibitory activity. The efficacy of this drug is also a consequence of its long-lasting activity, likely due to its metabolic stability. The reactivity of cyano groups in the letrozole structure could, however, lead to chemical derivatives still endowed with residual biological activity. Herein, the chemical degradation process of the drug was studied by coupling multivariate curve resolution and spectrophotometric methodologies in order to assess a detailed kinetic profile. Three main derivatives were identified after drug exposure to different degradation conditions, consisting of acid-base and oxidative environments and stressing light. Molecular docking confirmed the capability of these compounds to accommodate into the active site of the enzyme, suggesting that the sustained inhibitory activity of letrozole may be at least in part attributed to the degradation compounds.

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Section: Introductionmentioning

confidence: 99%