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dc.date.accessioned 2012-08-28T11:50:16Z
dc.date.available 2012-08-28T11:50:16Z
dc.date.issued 2012
dc.identifier.uri http://sedici.unlp.edu.ar/handle/10915/20208
dc.description.abstract Tacrolimus (Brand name: Prograf), a kind of immunosuppressants, has been reported to induce drug-drug interaction with many clinical drugs. Tacrolimus-mycophenolic acid (MPA) interaction has been widely and frequently reported. Intestinal UDP-glucuronosyltransferase (UGT) 1A8-mediated metabolism plays a key role in the elimination of MPA, and alteration of the activity of UGT1A8 resulting from gene polymorphisms could significantly influence the catalyzing activity of MPA glucuronidation. The aim of the present study is to investigate the inhibitory potential of tacrolimus towards UGT1A8, which was speculated to be a potential cause for tacrolimus-MPA interaction. The recombinant UGT1A8 was used as enzyme source, and a nonspecific substrate 4-methylumbelliferone (4-MU) was utilized as substrate. The results showed that 100 μM of tacrolimus inhibited UGT1A8-mediated 4-MU glucuronidation activity by 82.3%. Further inhibition kinetic investigation showed that the inhibition of UGT1A8 by tacrolimus was best fit to competitive inhibition type, and the inhibition kinetic parameter (Ki) was determined to be 6.1 μM. All these results indicated that tacrolimus could exhibit strong inhibition towards UGT1A8, which should be paid more attention when explaining clinical tacrolimus-MPA interaction. en
dc.format.extent 625-627 es
dc.language en es
dc.subject Drug-Drug Interaction (DDI) en
dc.subject Mycophenolic Acid (MPA) en
dc.subject Glucuronosiltransferasa es
dc.subject Ácido Micofenólico es
dc.subject Tacrolimus en
dc.subject UDP-Glucuronosyltransferase (UGT) 1A8 en
dc.title Tacrolimus (Tacro) strongly inhibits intestinal UDP-glucuronosyltransferase (UGT) 1A8 en
dc.type Articulo es
sedici.identifier.uri http://www.latamjpharm.org/resumenes/31/4/LAJOP_31_4_2_3.pdf es
sedici.identifier.issn 0326-2383
sedici.creator.person Yu, Jian es
sedici.creator.person Wang, Chuan-Qiang es
sedici.creator.person Fang, Long-Hao es
sedici.creator.person Li, Meng es
sedici.creator.person Wang, Xiangyang es
sedici.creator.person Dai, Lu-Lu es
sedici.creator.person Gao, Ya-Jie es
sedici.subject.materias Farmacia es
sedici.description.fulltext false es
mods.originInfo.place Colegio de Farmacéuticos de la Provincia de Buenos Aires es
sedici.subtype Comunicacion es
sedici.description.peerReview peer-review es
sedici.relation.journalTitle Latin American Journal of Pharmacy es
sedici.relation.journalVolumeAndIssue vol. 31, no. 4 es


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