What is the Origin of CYP2D6 Metabolism?

The concept is foundational to pharmacogenetics and clinical pharmacology, stemming from the discovery and characterization of the Cytochrome P450 superfamily of enzymes responsible for xenobiotic metabolism. The specific nomenclature CYP2D6 designates the enzyme's family, subfamily, and isoform based on genetic and structural homology.

What is the Mechanism of CYP2D6 Metabolism?

The CYP2D6 enzyme functions by introducing polar groups into lipophilic substrates, preparing them for excretion. For prodrugs, such as certain selective estrogen receptor modulators (SERMs) or opioids, this metabolism is necessary to convert the inactive compound into its active therapeutic form. Poor metabolizers may experience reduced efficacy due to insufficient activation, while ultrarapid metabolizers may suffer increased toxicity from excessive formation of the active metabolite, highlighting the enzyme's clinical significance in endocrine and neurological treatments.

CYP2D6 Metabolism

Meaning

CYP2D6 Metabolism refers to the biotransformation of various drugs and endogenous substances catalyzed by the Cytochrome P450 2D6 enzyme, a crucial component of the hepatic and extrahepatic detoxification system. This enzyme is highly polymorphic, meaning genetic variations in the CYP2D6 gene lead to different metabolic phenotypes, ranging from ultrarapid to poor metabolizers. Understanding an individual’s CYP2D6 status is essential for personalizing drug dosing, particularly for hormonal agents and psychoactive medications.