What is the Origin of CYP3A4 Inhibitors?

The nomenclature is derived from the official classification of the Cytochrome P450 enzyme superfamily, where 'CYP' denotes the enzyme class, and '3A4' specifies the gene family, subfamily, and isoform, indicating its unique genetic and structural identity. The term 'inhibitor' denotes its functional property of reducing enzymatic activity.

What is the Mechanism of CYP3A4 Inhibitors?

These inhibitors exert their effect by binding directly to the active site of the CYP3A4 enzyme, or by forming a complex with the enzyme's iron center, which prevents the enzyme from performing its necessary oxidative metabolism on other co-administered drug substrates. This inhibition leads to reduced clearance of the substrate drug, causing a substantial increase in its systemic concentration and heightening the risk of dose-dependent toxicity.

CYP3A4 Inhibitors ∞ Area

CYP3A4 Inhibitors

Meaning

CYP3A4 Inhibitors are a class of chemical compounds or pharmacological agents that significantly decrease the metabolic capacity of the Cytochrome P450 3A4 enzyme, which is the most abundant and clinically important enzyme in the liver responsible for the Phase I metabolism of a vast number of endogenous and exogenous substances. These inhibitors are a major source of clinically relevant drug-drug interactions.