Breast cancer resistance protein (ABCG2)
Also known as: BCRP, ABCG2
Efflux transporter (ABCG2) present in the gut, liver, kidney and placenta, which limits the absorption of several drugs and endogenous substrates (e.g. uric acid).
BCRP inhibition increases exposure to substrates such as rosuvastatin, methotrexate and sulfasalazine; combination with inhibitors (e.g. ciclosporin) may require dose reduction.
Substrates: rosuvastatin, atorvastatin (partial), methotrexate, sulfasalazine, allopurinol (oxipurinol), nitrofurantoin.
Inhibitors: ciclosporin, eltrombopag, curcumin, grapefruit juice.
Inducers: rifampicin.
The rosuvastatin + ciclosporin interaction (increased exposure) is documented in the rosuvastatin label and requires a dose limit.
DailyMed/FDA (NIH/NLM) — approved Rosuvastatin label; EMC-UK (MHRA) — SmPC
