Title : Inhibition of Intestinal OATP2B1 by the Calcium Receptor Antagonist Ronacaleret Results in a Significant Drug-Drug Interaction by Causing a 2-Fold Decrease in Exposure of Rosuvastatin.

Pub. Date : 2017 Jan

PMID : 27737931






3 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Inhibition of Intestinal OATP2B1 by the Calcium Receptor Antagonist Ronacaleret Results in a Significant Drug-Drug Interaction by Causing a 2-Fold Decrease in Exposure of Rosuvastatin. Rosuvastatin Calcium solute carrier organic anion transporter family member 2B1 Homo sapiens
2 Rosuvastatin is a widely prescribed antihyperlipidemic which undergoes limited metabolism, but is an in vitro substrate of multiple transporters [organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, OATP1A2, OATP2B1, sodium-taurocholate cotransporting polypeptide, breast cancer resistance protein (BCRP), multidrug resistance protein 2 (MRP2), MRP4, organic anion transporter 3]. Rosuvastatin Calcium solute carrier organic anion transporter family member 2B1 Homo sapiens
3 Therefore, a likely mechanism of the observed DDI is inhibition of intestinal OATP2B1, demonstrating the in vivo importance of this transporter in rosuvastatin absorption in humans. Rosuvastatin Calcium solute carrier organic anion transporter family member 2B1 Homo sapiens