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Biotech / Medical : Incyte (INCY)
INCY 104.18+0.1%Nov 17 3:59 PM EST
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To: software salesperson who wrote (2712)12/15/2011 8:10:11 AM
From: Biotech Jim   of 3202
 
Depends on the cytochrome P450 enzyme (CYP) that the live uses to clear tofacitinib.

I could not find the pathway of metabolism/clearance for the PFE compound in the published literature. Some CYPs are polymorphic in man, so there can be substantial differences in clearance, like for example with CYP2D6. This can be problematic as there could be either underdosing or overdosing with potential consequent effects on efficacy and toxicity. CNS drugs in particular can be CYP2D6 substrates. On the other hand more than half small molecules can be cleared by CYP3A4. This enzyme has a broad substrate specificity and has a very high capacity, but there can be drug interactions with this enzyme also. Recall that tofacitinib was originally developed for kidney transplants, and it would not be wise to develop a drug for this indication that would be cleared by the kidney.

On the other hand, kidney clearance has been realized to be more complex over the past 5-10 years as there are several transporter proteins that are responsible for kidney clearance of small molecules (eg, the so-called ABC transporters, amongst others). There can be drug-drug interactions for kidney cleared drugs as well, but this seems to be much less common.

So the bottom line here is that it depends on what enzymes and transporters are involved in the metabolism/clearance of tofacitinib and for '050.
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