Table 1.
Drug substrates known for metabolism by the CYP2B6 enzyme.
| Therapeutic class | Substratea | Reaction (type)b | Other CYPsc | References |
|---|---|---|---|---|
| Antiretroviral | Efavirenz | 8-hydroxylation (major reaction) | CYP3A4, 3A5, 1A2, 2A6 | Patel and Patel, 2018 |
| Nevirapine | Hydroxylation (major reaction) | CYP3A4 3A5, 2C9, 2D6 | Giardina et al., 2018 | |
| Antimalarial | Artemether | Demethylation (minor reaction) | CYP3A4, 3A5 | Agency, 2017 |
| Artemisinin | Unknown (major reaction) | CYP3A4 | Agency, 2017 | |
| Anticancer | Cyclophosphamide | 4-hydroxylation (major reaction) N-dechloroethylation (minor reaction) | CY2C19, 3A4, 2E1 | Stingl et al., 2013; Schurig et al., 2018 |
| Ifosfamide | 4-hydroxylation N-dechloroethylation (major reaction) | CYP3A4, 2C9, 2C19, 2C8 | Stingl et al., 2013 | |
| Tamoxifen | 4-hydroxylated (minor reaction) | CYP2D6, 3A4, 2C9, 2C19 | Weinshilboum, 2003; Evans and Relling, 2004 | |
| Antidepressants | Bupropion | Hydroxylation (major reaction) | CYP3A4, CYP2D6, | Lynch and Price, 2007; Zanger and Schwab, 2013 |
| Esketamine | N-demethylation (major reaction) | CYP3A4, 2C9, 2C19 | Lonsdale et al., 2013; Nebert et al., 2013 | |
| Vortioxetine | Hydroxylation (minor reaction) | CYP2D6, 3A4/5, 2C19, 2C9, 2A6, 2C8 | Thorn et al., 2010 | |
| Amitriptyline | N-demethylation (minor reaction) | CYP2C9, 2C19, 1A2, 3A4, 2D6, 2B6, 2C8 | Desta et al., 2021 | |
| Fluoxetine | N-demethylation (minor reaction) | CYP2D6, 2C9, 3A4 | Rendic, 2002 | |
| Mianserin | N-demethylation (minor reaction) | CYP3A4, 2C19, 1A2 | Hanna et al., 2000 | |
| Sertraline | N-demethylation (minor reaction) | CYP3A4, 2C19, 2D6, 2C9 | Zanger et al., 2008; Sarfo et al., 2014 | |
| Anticonvulsants | Phenytoin | Oxidation (minor reaction) | CYP1A2, 2A6, 2C19, 2C8, 2C9, 2D6, 2E1, CYP3A4 | Kharasch and Greenblatt, 2019 |
| S-mephenytoin | N-demethylation (minor reaction) | CYP2C9, 2C19 | Chaivichacharn et al., 2020 | |
| Carbamazepine | 3-hydroxylation (minor reaction) | CYP3A4, CYP2C8, CYP3A5 | Bank et al., 2019 | |
| Valproic acid | 4, 5-hydroxylation (minor reaction) | CYP2C9, 2A6, 3A5 | Kim et al., 2017 | |
| Anxiolytics, anticonvulsants | Diazepam | N-demethylation (minor reaction) | CYP2C19, 3A4, 3A5, 2C9 | Bielinski et al., 2014 |
| Clotiazepam | N-demethylation (minor) reaction | CYP3A4, 2C18, 2C19, | Dolgin, 2011 | |
| Clobazam | N-demethylation (minor reaction) | CYP3A4, 2C19 | Drozda et al., 2018 | |
| Temazepam | N-demethylation (minor reaction) | CYP2C19, 3A4 | Bielinski et al., 2014 | |
| Anesthetics | Kitamine | N-demethylation (major reaction) | CYP3A4, 2C9 | Lonsdale et al., 2013 |
| Propofol | 4-hydroxylation (major reaction) | CYP2C9 | Hesse et al., 2004; Zanger and Schwab, 2013 | |
| Opioid | Methadone | N-demethylation (major reaction) | CYP3A4, 2C19, 2C9, 2C8, 2D6, | Ekins et al., 1998; Lang et al., 2001 |
| MAOI | Selegiline | N-demethylation (major reaction) | CYP2C19, 3A4, 1A2, 2D6, 2C9 | Wang et al., 2003a,b |
| Antiplatelet | Clopidogrel | Oxidation (minor reaction) | CYP1A2, 2B6, 2C19, 2C9, 3A4 | Lee et al., 2003 |
| Smoking cessation agent | Nicotine | N-demethylation (minor reaction) | CYP2A6, 3A4 | Aitken and Morgan, 2007; Liptrott et al., 2009 |
| Analgesics | Tramadol | N-demethylation (minor reaction) | CYP2D6, 3A4, | Faucette et al., 2004; Lo et al., 2010 |
| Diclofenac | 5-hydroxylation (minor reaction) | CYP2C8, 2C19, 2C9 | Pearce et al., 2016 | |
| Gastro-intestinals | Loperamide | N-demethylation (minor reaction) | CYP219, 3A4, 2D6, 2C8, | Lewis and Lake, 1997 |
| Steriod | Testosterone | Hydroxylation (minor reaction) | CYP3A4, 2C9, 2C19 | Ekins et al., 2008 |
| Anticoagulant | Coumarin | Aromatic hydroxylation (minor reaction) | CYP2A6, 1A1, 1A2, 3A4 | Xie et al., 2003 |
| SERM | Ospemifene | Hydroxylation (minor reaction) | CYP3A4, 2C9, 2C19, | Hidestrand et al., 2001 |
a
According to the drug Bank (https://go.drugbank.com/categories/DBCAT002619) and online literature.
b
CYP2B6 is either the major enzyme or the minor enzyme in the biotransformation of the drug. The type of metabolic reaction according to the information from Pharmacogenomics Knowledge base (PharmGKB) website, drug bank and online literature.
c
Other cytochromes that are involve in the metabolism of the drug, taken from PharmGKB website, drug bank and online literature.
SERM, Selective estrogen receptor modulators.
MAOI, Monoamine oxidase inhibitors.