Title : New insights into drug absorption: studies with sirolimus.

Pub. Date : 2004 Oct

PMID : 15385826






4 Functional Relationships(s)
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1 Likewise, sirolimus is a substrate for the major drug-metabolizing enzyme cytochrome P450 3A4 (CYP3A4) and the efflux transporter P-glycoprotein (P-gp), both of which are expressed in close proximity in epithelial cells lining the small intestine. Sirolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Likewise, sirolimus is a substrate for the major drug-metabolizing enzyme cytochrome P450 3A4 (CYP3A4) and the efflux transporter P-glycoprotein (P-gp), both of which are expressed in close proximity in epithelial cells lining the small intestine. Sirolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Modified Caco-2 cells metabolized [14C]sirolimus to the same CYP3A4-mediated metabolites as human small intestinal and liver microsomes. Sirolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 Along with CYP3A4-mediated metabolism and P-gp-mediated efflux, a novel elimination pathway was identified that may also contribute to the first-pass extraction, and hence low oral bioavailability, of sirolimus. Sirolimus cytochrome P450 family 3 subfamily A member 4 Homo sapiens