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. 2024 Jul 2;12(7):1467. doi: 10.3390/biomedicines12071467

Table 1.

CYP450 families, main functions, and substrates [15,39].

CYP Family Main Function Subfamily Substrate/Endogenous Compound
CYP1 Biotransformation CYP1A1 Granisetron and riociguat
CYP1A2 Polycyclic aromatic hydrocarbons, caffeine, tizanidine, clozapine, olanzapine, theophylline, alosetron, duloxetine, melatonin, pirfenidone, ramelteon, tasimelteon, acetaminophen, antipyrine, bufuralol, ondansetron, phenacetin, and tacrine
CYP2 Biotransformation CYP2A6 Nicotine, coumarin, and valproic acid
CYP2B6 Efavirenz
CYP2C8 Metabolizes over 60 clinically relevant drugs, including montelukast, pioglitazone, repaglinide, and rosiglitazone
CYP2C9 Warfarin, carvedilol, celecoxib, glipizide, glimepiride, ibuprofen, irbesartan, losartan, phenytoin, and tolbutamide
CYP2C19 Omeprazole, lansoprazole, and phenobarbital
CYP2D6 Antidepressants, antipsychotics, beta-blockers, antiretroviral agents, antiarrhythmics, morphine derivatives, and Tamoxifen
CYP2E1 Ethanol, acetaminophen, theophylline, and verapamil metabolism
CYP3 Biotransformation CYP3A4 Alprazolam, amlodipine, buspirone, calcium channel blockers, caffeine, citalopram, clopidogrel, cocaine, cyclosporine, diazepam, erythromycin, drugs, montelukast, quetiapine, sertraline, sildenafil, statin drugs, tacrolimus, warfarin, zolpidem, estradiol, lidocaine, losartan, and many chemotherapeutic agents
CYP4 Fatty acid metabolism CYP4A Arachidonic acid (AA)
CYP5 Thromboxane A2 synthesis -
CYP7 Bile acid biosynthesis CYP7A1 Converts cholesterol to 7α-hydroxycholesterol
CYP7B1 Metabolizes dehydroepiandrosterone
CYP8 Bile acid and prostacyclin biosynthesis CYP8A1 Converts prostaglandin H2 to thromboxane A
CYP11 Steroid biosynthesis CYP11A1 Converts cholesterol to pregnenolone plus 4-methylpentanal
CYP17 Steroid biosynthesis CYP17A1 Converts corticosterone to cortisol
CYP19 Steroid biosynthesis CYP19A1 Metabolizes androstenedione and testosterone
CYP20 Unknown function -
CYP21 Steroid biosynthesis CYP21A2 Converts progesterone to deoxycortisone in pregnancy
CYP24 Vitamin D degeneration CYP24A1 Converts 1,25-dihydroxyvitamin D3 (calcitriol) to 1α,24R,25-trihydroxyvitamin D3
CYP26 Retinoic acid hydroxylation CYP26A1, CYP26B1, and CYP26C1 Convert retinoic acid to 4-hydroxyretinoic acid
CYP27 Vitamin D3 and bile acid biosynthesis CYP27C1 Converts retinol (vitamin A1) to 3,4-didehydroretinol (vitamin A2)
CYP39 Cholesterol synthesis CYP39A1 Converts 24-hydroxycholesterol to 7α,24-dihydroxycholesterol
CYP46 Cholesterol synthesis CYP46A1 Converts cholesterol to 24(S)-hydroxycholesterol
CYP51 Cholesterol synthesis CYP51A1 Lanosterol