Ethacrynic acid, Glutathione S-transferase (GST) inhibitor

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

CYP2C9 also known as Cytochrome P450 2C9 is an enzyme that plays a significant role in drug metabolism. It is a member of the cytochrome P450 superfamily with a molecular mass of approximately 55 kDa. The enzyme is predominantly found in the liver where it contributes to the oxidation of various substrates including drugs cholesterol and other lipids. It is an important target in pharmacogenomics due to its influence on drug clearance and interaction.

Biological function summary

CYP2C9 participates in the phase I metabolism of xenobiotics and endogenous compounds. It is not part of a larger complex but works closely with other enzymes to sustain metabolic processes. CYP2C9 converts lipophilic molecules into more hydrophilic forms which facilitates their subsequent conjugation and elimination. Its activity affects the pharmacokinetics and pharmacodynamics of nonsteroidal anti-inflammatory drugs (NSAIDs) and oral anticoagulants.

Pathways

CYP2C9 is essential in the arachidonic acid metabolism and steroid hormone biosynthesis pathways. In these pathways it interacts with other cytochrome P450 enzymes like CYP3A4 to metabolize drugs and steroids. The synergy between CYP2C9 and related enzymes ensures efficient metabolic clearance of drugs and bioactive lipids although it can also lead to drug interactions if multiple drugs are metabolized by the same enzyme.

CYP2C9 polymorphisms have been linked to altered drug metabolism particularly affecting therapeutic outcomes in cardiovascular conditions and epilepsy. Variants of CYP2C9 can lead to increased or decreased metabolism of warfarin commonly used in cardiovascular disease management. Disorders related to CYP2C9 activity often involve impaired clearance of therapeutic agents and are also seen in conjunction with variations in other metabolic enzymes such as GST (glutathione S-transferase).