Various anti-cancer drugs like pazopanib, vandetanib, nilotinib, canertinib and erlotinib are known to be transported via OATPs (OATP-1B1 and OATP-1B3).
[7] The various paralogues in a mammal have differing but overlapping substrate specificities and tissue distributions as summarized by Hagenbuch and Meier.
[4] These authors also provide a phylogenetic tree of the mammalian members of the family, showing that they fall into five recognizable subfamilies, four of which exhibit deep branching sub-subfamilies.
These transporters have been characterized in mammals, but homologues are present in Drosophila melanogaster, Anopheles gambiae, and Caenorhabditis elegans.
The mammalian OAT family proteins exhibit a high degree of tissue specificity.
The OATPs play a role in the transport of some classes of drugs across the cell membrane, particularly in the liver and kidney.
[8] The most clinically relevant interactions have been associated with the lipid lowering drugs statins, which led to the removal of cerivastatin from the market in 2002.
Many modulators of OATP function have been identified based on in vitro research in OATP-transfected cell lines.
OATPs are present in many animals, including fruit flies, zebrafish, dogs, cows, rats, mice, monkeys and horses.