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Vol. 8, Issue 4 (2019)

Evaluation of the effect of selective CYP 450 enzymes on NCE

Author(s):
Sai Laxmi Kesana, Vamaraju Harinadha Babu, Dodle Jaya Prakash and Pooja Borra
Abstract:
Background: With the increasing knowledge about Cytochrome P450 enzymes, the Pharmacokinetic and toxicological profile of the drug can be studied. The determination of the cytochrome P450, on the metabolism of New Chemical Entity using an in vitro approach has become essential for the prospective understanding of any drug. It is an important filter in the drug screening and before checking with the animal models.
Purpose: The in vitro approach of incubation with the selective enzymes aims
i.To aid in preclinical screening of the drug metabolism without utilization of animals
ii.Illustrate the mechanistic pathway of the NCE via the CYP enzymes
Materials and Methods: The Test compound was incubated in vitro, using selective CYP enzymes like 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4 in presence and absence of their CYP inhibitors and then extrapolated the observations using Microsoft excel Curves and Graphs.
Result: The influence of the selective enzymes on Test compound’s metabolism is of the order CYP 3A4 > CYP 2D6 > CYP 2C9 > CYP 1A2 > CYP 2C19> CYP 2B6 > CYP 2C8
Conclusion: In vitro metabolism of the Test compound by the CYP is observed. CYP3A4 has shown highest activity whereas the least was shown by CYP 2C8, while CYP 2D6 & CYP 2C9 depicted an average activity. The data drawn gave an understanding about the individual activity of the commercially viable enzymes on the Test compound providing the metabolic pathway of the Test compound under the given experimental conditions.
High Lights
•The CYP enzymatic influence on the metabolism of the NCE is observed
•The selective CYP activity is measured without an authentic standard
The specific role of CYP in metabolism and the sustainability of the Test compound as a drug in the process of lead optimization are commented.
Pages: 718-725  |  312 Views  47 Downloads


The Pharma Innovation Journal
How to cite this article:
Sai Laxmi Kesana, Vamaraju Harinadha Babu, Dodle Jaya Prakash, Pooja Borra. Evaluation of the effect of selective CYP 450 enzymes on NCE. Pharma Innovation 2019;8(4):718-725.

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