Thursday, 18 February 2016

Silensomes: Quantifying the Contribution of CYP Enzymes in Drug Metabolism

I would like to introduce to you a new and representative model, capable of directly quantifying and predicting the contribution of CYP enzymes in drug metabolism: Silensomes™.

Silensomes™ are validated human pooled liver microsomes (HLMs) chemically and irreversibly inactivated for one specific CYP using mechanism based inhibitors (MBI). Each Silensomes™ is available as ready-to-use HLMs chemically knocked-out for one specific CYP activity (1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4) with each showing high specificity and efficiency of their targeted CYP inhibition (>80%), and only minor impact (<20%).

Key Advantages of Silensomes™:
  • Irreversibly inhibited CYPs
  • For initial rate conditions
  • For saturating conditions
  • One single model for CYP phenotyping assays, instead of a battery of in-vitro tests
  • Quantitative: the true contribution of the CYP450 in the metabolism of the compound can be measured
  • A powerful model with an excellent specificity, potency, stability and predictability to ensure reliable extrapolation of the drug-drug interaction risk
  • More representative of in-vivo, using human liver microsomes rather than recombinant enzymes isolated from non-mammalian cells
Silensomes™ are available for compound screening purposes and also for regulatory validation.

Please click here to view the current Silensomes™ that are available to purchase.

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