Summary
CYP3A4/3A5 substrates are compounds that are metabolized by CYP3A4 and CPY3A5 (cytochrome P450 enzymes), but do not necessarily affect their activity.
CYP3A4 and CYP3A5 are structurally very similar and largely share the same substrates, but CYP3A5 is generally considered to be less metabolically active and is usually present in lower amounts, particularly in people of European descent.[1]
In the presence of CYP3A4/3A5 inhibitors or inducers, the metabolism of CYP3A4/3A5 substrates can be affected.
The table below outlines some of the most common or clinically relevant CYP3A4/3A5 substrates.[1][2][3] Importantly, this list is not exhaustive.
CYP3A4/3A5 Substrates |
---|
Acetaminophen |
Alprazolam |
Aprepitant |
Atorvastatin |
Budesonide |
Buprenorphine |
Carbamazepine |
Citalopram |
Clarithromycin |
Clindamycin |
Codeine |
Colchicine |
Cyclobenzaprine |
Cyclophosphamide* |
Cyclosporine |
Dexamethasone |
Dextromethorphan |
Diazepam |
Diltiazem |
Docetaxel |
Eletriptan |
Felodipine |
Fenofibrate |
Fentanyl |
Glyburide |
Haloperidol |
Hydromorphone |
Indinavir |
Irinotecan |
Isotretinoin |
Loperamide |
Lopinavir |
Lovastatin |
Methadone |
Midazolam |
Mifepristone |
Mirtazapine |
Nifedipine |
Oxycodone |
Quetiapine |
Quinine |
Ritonavir |
Rivaroxaban |
Sildenafil |
Simvastatin |
Tacrolimus |
Tadalafil |
Testosterone |
Ticagrelor |
Tramadol |
Trazodone |
Triazolam |
Verapamil |
Zolpidem |
* Prodrugs are indicated with an asterisk
References
- ^Song Y, Li C, Liu G, Liu R, Chen Y, Li W, Cao Z, Zhao B, Lu C, Liu YDrug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes.Clin Pharmacokinet.(2021-May)
- ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
- ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)