Target intelligence / Profile preview

Cytochrome P450 2D6 (CYP2D6)

Target
CYP2D6
Molecular classification
Enzyme, Cytochrome P450, Monooxygenase, Heme-containing monooxygenase
01

Overview

Cytochrome P450 2D6 (CYP2D6) is a key enzyme in the cytochrome P450 superfamily, primarily expressed in the liver and also present in certain regions of the central nervous system. It plays a crucial role in metabolizing and eliminating approximately 20–25% of all clinically used drugs, including antidepressants, antipsychotics, analgesics (such as codeine), beta-blockers, and anticancer agents. CYP2D6 is also involved in activating some prodrugs and metabolizes several endogenous compounds like neurosteroids and tyramine derivatives. Genetic polymorphisms in CYP2D6 lead to varying levels of enzyme activity, impacting drug efficacy and toxicity.

Other names
CYP2D6P450 2D6Cytochrome P-450 2D6EC 1.14.14.1
02

Mechanism of action

Hydroxylation, demethylation, dealkylation of drugs and endogenous substrates.

03

Biological functions

Drug metabolismXenobiotic metabolismSteroid metabolismActivation of prodrugsInactivation of drugs
04

Disease associations

Adverse drug reactionsDrug resistancePharmacogenomics-related diseases
05

Safety considerations

Drug-drug interactionsAdverse drug reactions due to altered metabolismLack of efficacy due to impaired prodrug activationIncreased risk of toxicity due to decreased drug clearance
06

Interacting drugs

Antidepressants

6 more in the full profile.

07

Biomarkers

CYP2D6 genotypeCYP2D6 phenotype (PM, IM, EM/NM, UM)

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