TABLE 4

Range of substrates for CYP2J2 and the metabolic pathways by which they are formed

Substrates include both endogenous compounds and exogenous drugs and the main metabolic pathways are hydroxylation and epoxygenation.

SubstrateMetabolic PathwayKm (μM)aVmax/Turnover No. (nmol/min per nmol)a
Endogenous
 Arachidonic acidEpoxygenation0.065
 Linoleic acidEpoxygenation0.105
 Docosahexaenoic acidEpoxygenation (major) ω-1/ω hydroxylation (minor)0.228 ± 0.008
 Eicosapentaenoic acidEpoxygenation (major) ω-1/ω hydroxylation (minor)0.943 ± 0.017
 Vitamin D325-Hydroxylation7.7 ± 1.20.087 ± 0.013
 Vitamin D225-Hydroxylation2.0 ± 0.30.16 ± 0.03
 1α(OH)D325-Hydroxylation4.4 ± 0.72.2
Drugs
 Albendazoleω-Hydroxylation sulfoxidation
 Amiodarone3-Hydroxylation 4-hydroxylation54.6
 ApixabanO-demethylation0.27 ± 0.06
 AstemizoleaO-demethylation0.651.129
 BenzphetamineN-demethylation0.08
 Bufuralol0.17
 Cyclosporine AHydroxylation
 DanazolHydroxylation
 EbastinaHydroxylation1.3/18.340.6/8.2
 Eperisoneω- Hydroxylation ω-1 hydroxylation0.0266
 HydroxyebastineCarboxylation0.759.86
 TerfenadineHydroxylation0.420
 ThioridazineSulfoxidation
 VorapaxarHydroxylation0.0306

  • ↵a Metabolic pathway used solely by CYP2J2.

  • b Some Km and Vmax values remain unknown.