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What is CYP450 phenotyping?

In vitro identification and measurement of the contribution of the major cytochrome P450 enzymes (CYP450s) involved in the metabolism of a new drug candidate is called “CYP450 phenotyping”. Information from these assays is used to predict the impact...

What are "Control Silensomes HLM"?

Control Silensomes™ HLM are the true control microsomes for comparison of metabolism in “CYP-silenced” Silensomes™ HLM since they have been processed under the same conditions as Silensomes™ HLM but in the absence of the mechanism based inhibitor...

What is fm value and why is important to have that data in-vitro/in-vivo?

The fm value is the percent of enzyme (e.g. CYP) contribution to the metabolism of a test compound. The in-vitro fm value is important to measure to predict the in vivo fm which is important to estimate the potential for drug-drug interactions with...

How can in-vitro fm value be estimated using Silensomes HLM?

The Silensomes™ HLM directly predict the CYP contribution to drug metabolism and the in-vitro fm. .This is carried out by measuring the intrinsic clearance (Clint) of a test compound in Silensomes™ and in concurrent Control SilensomesTM HLM. The...

Do you also sell the boxes or cases for the Nucleofector Core, X, Y and LV units? 

Yes, see this list of part codes for the different types of transport boxes: Part code: AAK-1001Items: 4D-Nucleofector™ Demo Suitcase (2 units)Suited for: Core + X or Core + Y or X + YPart...

What are the parameters that affect the accuracy of my fm value?

The parameters that affect the accuracy of in-vitro fm value calculation include: 1) the choice of analytics (e.g. disappearance of parent vs appearance of metabolite), 2) the activities in the initial HLM batch, and 3) the balance between the CYPs....

What is the regulatory position of the fm value?

The FDA and EMA guidelines consider metabolism to be a significant pathway when it contributes to 25% or more of the drug’s overall elimination. When the CYP contribution is ~25% (In-vitro fm value > 25 %) or unknown, in vivo studies using...

What are the Storage and thaw-refreeze conditions for Silensomes HLM?

The Silensomes™ HLM and associated Control Silensomes™ HLM should be stored at or below -70°C. CYP450 enzyme activities in Silensomes™ HLM and associated Control Silensomes™ HLM are stable for up to 5 years when stored at -70°C and can be...

How can we approach the in-vitro fm value for low clearance compounds when using Silensomes HLM?

The in-vitro fm value of low clearance compounds can be measured by optimizing or extending the incubation time with certain limit. In addition, the appearance of metabolites can be measured instead of the disappearance of the parent compound.

What is the benefit of using Silensomes instead of the classical testing methods?

Compared to classical phenotyping protocols relying on reversible, as well irreversible, inhibitors Silensomes™ HLM offer a superior performance and high level of quality. The mechanism based inhibitors used to make Silensomes™ HLM are irreversible,...
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