Cytochrome P450 family 2 subfamily B member 6 (CYP2B6) (CYP2B6)

Cytochrome P450 family 2 subfamily B member 6 (CYP2B6) is a vital enzyme primarily expressed in the liver, where it accounts for a significant portion of the oxidative metabolism of xenobiotics, including roughly 3-10% of all clinical drugs (UniProt, 2024). It plays a central role in the activation of prodrugs like cyclophosphamide and the clearance of drugs such as the antidepressant bupropion and the HIV medication efavirenz (PubMed, 2021). Fenofibric acid, the active form of the lipid-lowering drug fenofibrate, is known to modulate CYP2B6 activity by inducing its expression through the activation of the Constitutive Androstane Receptor (CAR) and the Pregnane X Receptor (PXR) (NCBI, 2023). This induction can lead to complex drug-drug interactions, where the co-administration of fenofibrate may decrease the plasma concentration and efficacy of other CYP2B6 substrates. Furthermore, CYP2B6 is characterized by high genetic variability, with common polymorphisms significantly impacting patient response to therapy and susceptibility to adverse effects (StatPearls, 2023). Beyond drug metabolism, CYP2B6 is involved in the processing of endogenous substances such as steroids and fatty acids, and its expression levels are linked to various pathological states, including certain cancers and neurological conditions (StatPearls, 2023).

Other names

Cytochrome P450 2B6CPB6CYP2B7PCytochrome P450 IIB6

CYP2B6 functions as a monooxygenase that catalyzes the oxidative metabolism of various endogenous and exogenous compounds. Fenofibric acid acts as an inducer of CYP2B6 expression by activating the Constitutive Androstane Receptor (CAR) and the Pregnane X Receptor (PXR), which subsequently increase the transcription of the CYP2B6 gene, leading to higher enzyme levels and accelerated clearance of its substrates (PubMed, 2020; NCBI, 2023).