Gosset Cytochrome P450 3A4 Overview
Cytochrome P450 3A4 (CYP3A4) is a key enzyme in the cytochrome P450 superfamily, responsible for metabolizing approximately 50-60% of all prescribed drugs and many endogenous compounds, including steroids and fatty acids. It is predominantly expressed in the liver and intestine. Due to its broad substrate specificity, CYP3A4 is a major contributor to drug-drug interactions, with many drugs acting as inhibitors or inducers of its activity. This can lead to altered plasma concentrations of co-administered medications, resulting in therapeutic failure or toxicity. It also has epoxide activity, converting arachidonic acid into epoxyeicosatrienoic acids (EETs) which have roles including cancer cell growth promotion.
Mechanism of Action
CYP3A4 catalyzes monooxygenation reactions, primarily involved in the metabolism of a vast array of xenobiotics and endogenous compounds. It can be inhibited or induced by drugs, altering the metabolism of its substrates.
Biological Functions
Disease Associations
Safety Considerations
- Drug-drug interactions due to inhibition or induction
- Therapeutic failure due to accelerated drug metabolism
- Drug toxicity due to reduced drug metabolism
- Potential for bioactivation of pro-toxic compounds