Target intelligence / Profile preview

Cytochrome P450 family 3 subfamily A member 11 (CYP3A11)

Target
CYP3A11
Molecular classification
Enzyme, Cytochrome P450, Monooxygenase, Oxidoreductase, Heme-thiolate protein
01

Overview

Cytochrome P450 family 3 subfamily A member 11 (CYP3A11) is the primary mouse ortholog of the human CYP3A4 enzyme and plays a central role in the phase I metabolism of xenobiotics and endogenous compounds [1, 2]. It is highly expressed in the liver and intestinal mucosa, where it facilitates the detoxification and clearance of a diverse range of lipophilic substances, including over 50% of marketed pharmaceuticals [9, 11]. The expression of CYP3A11 is tightly regulated by nuclear receptors, most notably the Pregnane X Receptor (PXR), which mediates its induction in response to various drugs and environmental chemicals [1, 5]. Consequently, CYP3A11 is a major site for drug-drug interactions, as its induction or inhibition can significantly alter the pharmacokinetics and toxicity profiles of co-administered medications [10, 15]. Beyond drug metabolism, it is involved in the homeostasis of steroid hormones and bile acids, and its dysregulation is associated with conditions such as cholestasis and inflammation-induced metabolic changes [4, 10]. Understanding CYP3A11 activity is essential in preclinical drug development for predicting human metabolic profiles and assessing safety risks associated with metabolic liabilities [3, 12].

Other names
Cyp3a11Cytochrome P450 3A11P450-3A11Cytochrome P450, family 3, subfamily a, polypeptide 11
02

Mechanism of action

Catalyzes the oxidative metabolism of lipophilic substrates, including hydroxylation, N-demethylation, O-dealkylation, and epoxidation, using molecular oxygen and electrons from NADPH-cytochrome P450 reductase.

03

Biological functions

Xenobiotic metabolismDrug metabolismSteroid hormone metabolismBile acid metabolismFatty acid oxidationDetoxification
04

Disease associations

Drug-induced liver injuryCholestasisInflammationMetabolic disordersCancer
05

Safety considerations

Drug-drug interactions (DDIs)Metabolic activation of toxins (e.g., acetaminophen bioactivation)Altered drug clearance in inflammationInter-individual variability in drug response
06

Interacting drugs

Midazolam

11 more in the full profile.

07

Biomarkers

1'-hydroxymidazolam4beta-hydroxycholesterolErythromycin N-demethylase activity

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