Hi all,
I'm working on ADME of some potential drug and I'm looking for the best way to determine in vitro clearance in hepatocytes.
As far as I understand, HepG2 cell line was used in past but the level of CYPs is rather low (also I don't see any decrease in drug amount in case of my compounds using HepG2 cells ON incubation).
A different models I found are HepaRG cell line and primary cryopreserved hepatocytes that should be comparable in terms of CYPs expression. Is there anybody who could share some experience with these? Which is more convenient in case I need to measure the in vitro clearance lets say once a month? Can be cryopreseved hepatocytes grown a bit, aliquoted and then used several times? Or how people deal with it when using cryohepatocytes? Is everyone buying a new stock every time when experiment is to be done?
Any suggestion or advice is welcome, thanks
Jakub
HepaRG is definitely more accurate as it has better induction of CYP enzyme expression compared to HepG2 which does not express CYPs as well. The main difference however, is cost. HepaRG is a lot more expensive to maintain and grow (think special maintenance medium and supplements) compared to HepG2 which can simply grow in DMEM.
You can check the heparg website for more information https://www.heparg.com/rubrique-features#pub_aff_article.72
They might give academic labs a discount.
If you just want to measure invitro clearance though, why not use microsomes directly? its easier to use because you dont need to grow anything
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