Pub. Date : 2015 Dec 1
PMID : 26514315
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | The studies reported herein examined whether fostamatinib and R406 are inhibitors of P-glycoprotein (P-gp) in vitro and evaluated the effect of fostamatinib on the pharmacokinetic parameters of digoxin to understand drug-drug interaction (DDI) potential in the clinic. | fostamatinib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | METHODS: Inhibition of P-gp-mediated digoxin transport by fostamatinib and R406 was determined across Caco-2 cell monolayers. | fostamatinib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | FINDINGS: Fostamatinib (but not R406) was determined to be a P-gp inhibitor in vitro (IC50 = 3.2 muM). | fostamatinib | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | IMPLICATIONS: Fostamatinib was confirmed to be a P-gp inhibitor in vitro and in vivo, and a DDI with digoxin was apparent. | fostamatinib | ATP binding cassette subfamily B member 1 | Homo sapiens |