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Literature summary for 1.14.14.1 extracted from

  • Tang, L.W.T.; Teng, J.W.; Koh, S.K.; Zhou, L.; Go, M.L.; Chan, E.C.Y.
    Mechanism-based inactivation of cytochrome P450 3A4 and 3A5 by the fibroblast growth factor receptor inhibitor erdafitinib (2021), Chem. Res. Toxicol., 34, 1800-1813 .
    View publication on PubMed
Search for more literature for 1.14.14.1

Inhibitors

Inhibitors Comment Organism Structure
erdafitinib fibroblast growth factor receptor inhibitor, irreversible covalent mechanism-based inhibitor of both isoforms CYP3A4 and CYP3A5; fibroblast growth factor receptor inhibitor, irreversible covalent mechanism-based inhibitor of both isoforms CYP3A4 and CYP3A5 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P20815 isoform CYP3A5
-
Homo sapiens Q9HB55 isoform CYP3A4
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
midazolam + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens 1'-hydroxymidazolam + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
rivaroxaban + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens ? + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
testosterone + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens 6beta-hydroxytestosterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

Synonyms Comment Organism
CYP3A4
-
 Homo sapiens
CYP3A5
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.004
-
 erdafitinib substrate rivaroxaban, pH 7.4, 37°C Homo sapiens
0.01
-
 erdafitinib substrate rivaroxaban, pH 7.4, 37°C Homo sapiens