General Information of This Metabolic Reaction (MR) (ID: MR002252)
Formula
CYP3A4 ...
SVG example
N-Demethylation
Reactant Sildenafil citrate Product Desmethylsildenafil
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Mephenytoin 4-hydroxylase (CYP2C19) DME Info
Cytochrome P450 2D6 (CYP2D6) DME Info
Cytochrome P450 2C9 (CYP2C9) DME Info
Cytochrome P450 3A5 (CYP3A5) DME Info
Cytochrome P450 2E1 (CYP2E1) DME Info
Metabolic Type Oxidation - N-Demethylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR002253 Sildenafil citrate N-dealkyl Sildenafil Oxidation - N-Dealkylation Sildenafil citrate [1]
Other MR(s) Related to The Product of This MR
Other MR(s) That Produce The Product of This MR
MR ID Reactant Product MR Type Related Drug REF
MR013895 Sildenafil N-desmethyl Sildenafil Unclear - Unclear Sildenafil [2], [3], [4]
References
1 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
2 Functional Measurement of CYP2C9 and CYP3A4 Allelic Polymorphism on Sildenafil Metabolism
3 In vitro biotransformation of sildenafil (Viagra): identification of human cytochromes and potential drug interactions. Drug Metab Dispos. 2000 Apr;28(4):392-7.
4 Contribution of CYP3A isoforms to dealkylation of PDE5 inhibitors: a comparison between sildenafil N-demethylation and tadalafil demethylenation. Biol Pharm Bull. 2015;38(1):58-65.

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