Organic cation transporter/solute carrier family 22a is involved in drug transfer into milk in mice.

Article Details

Citation

Ito N, Ito K, Ikebuchi Y, Kito T, Miyata H, Toyoda Y, Takada T, Hisaka A, Honma M, Oka A, Kusuhara H, Suzuki H

Organic cation transporter/solute carrier family 22a is involved in drug transfer into milk in mice.

J Pharm Sci. 2014 Oct;103(10):3342-8. doi: 10.1002/jps.24138. Epub 2014 Aug 29.

PubMed ID
25175747 [ View in PubMed
]
Abstract

Drug transfer into milk is a general concern during lactation. So far, breast cancer resistance protein (Bcrp) is the only transporter known to be involved in this process, whereas participation of other transporters remains unclear. We investigated the importance of organic cation transporter (Oct) in drug transfer into milk in mice. The mammary glands of lactating versus nonlactating FVB strain mice revealed elevated mRNA levels of Oct1 and Bcrp, whereas Oct2 and Oct3 mRNA levels were decreased. Specific uptake of cimetidine, acyclovir, metformin, and terbutaline was observed in human embryonic kidney 293 cells transfected with murine Oct1 or Oct2. The milk-to-plasma concentration ratio (M/P) values of cimetidine and acyclovir were significantly decreased in Bcrp knockout and Oct1/2 double-knockout (DKO) mice compared with control FVB mice, whereas the M/P values of terbutaline and metformin were significantly decreased in Oct1/2 DKO mice alone. These are the first to suggest that Oct1 might be involved in secretory transfer of substrate drugs into milk.

DrugBank Data that Cites this Article

Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
TerbutalineSolute carrier family 22 member 2ProteinHumans
Unknown
Substrate
Details
TerbutalineSolute carrier family 22 member 5ProteinHumans
Unknown
Substrate
Details