Tamoxifen metabolism (WP691)
Homo sapiens
Tamoxifen (TMX), sold under the brand name Nolvadex among others, is a medication that is used to prevent breast cancer in women and treat breast cancer in women and men.[1] It is also being studied for other types of cancer[1]. Tamoxifen is currently used for the treatment of both early and advanced estrogen receptor (ER)-positive (ER+) breast cancer in pre- and post-menopausal women[2]. Additionally, it is the most common hormone treatment for male breast cancer. [1]: https://www.cancer.gov/about-cancer/treatment/drugs/tamoxifencitrate [2]: Jordan, V. Craig. "A current view of tamoxifen for the treatment and prevention of breast cancer." British journal of pharmacology 110.2 (1993): 507-517.
Authors
Pieter Giesbertz , Kristina Hanspers , Egon Willighagen , Daniela Digles , Zahra Roudbari , Denise Slenter , and Eric WeitzActivity
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Cited In
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- Human Monocytes Exposed to SARS-CoV-2 Display Features of Innate Immune Memory Producing High Levels of CXCL10 upon Restimulation (2023).
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Organisms
Homo sapiensCommunities
Annotations
Disease Ontology
estrogen-receptor positive breast cancerPathway Ontology
xenobiotic metabolic pathway breast cancer pathway| Label | Type | Compact URI | Comment |
|---|---|---|---|
| Tamoxifen-N-oxide | Metabolite | pubchem.compound:3033895 | |
| cis-4-hydroxytamoxifen | Metabolite | pubchem.compound:449459 | |
| SSRI | Metabolite | chebi:50949 | |
| alpha-hydroxy-N-desmethyltamoxifen | Metabolite | pubchem.compound:10474509 | |
| PAP | Metabolite | hmdb:HMDB0000061 | |
| tamoxifen-N-glucuronide | Metabolite | pubchem.compound:5460873 | |
| PAPS | Metabolite | pubchem.compound:10214 | |
| 4-hydroxy-N-desmethyltamoxifen | Metabolite | pubchem.compound:3035980 | |
| trans-tamoxifen | Metabolite | hmdb:HMDB0014813 | |
| deamino-hydroxytamoxifen | Metabolite | pubchem.compound:3033897 | |
| alpha-hydroxytamoxifen | Metabolite | hmdb:HMDB0060585 | |
| N,N-didesmethyltamoxifen | Metabolite | pubchem.compound:3036172 | |
| Metabolite | Metabolite | chebi:25212 | |
| trans-4-hydroxytamoxifen | Metabolite | pubchem.compound:5352135 | |
| N-desmethyltamoxifen | Metabolite | pubchem.compound:3032890 | |
| CYP2D6 | GeneProduct | ensembl:ENSG00000100197 | |
| CYP2A6 | GeneProduct | ensembl:ENSG00000255974 | |
| SULT2A1 | GeneProduct | ensembl:ENSG00000105398 | |
| CYP2C9 | GeneProduct | ensembl:ENSG00000138109 | |
| CYP3A5 | GeneProduct | ensembl:ENSG00000106258 | |
| CYP2C19 | GeneProduct | ensembl:ENSG00000165841 | |
| CYP3A4 | GeneProduct | ensembl:ENSG00000160868 | |
| UGT1A10 | GeneProduct | ncbigene:54575 | |
| CYP1A2 | GeneProduct | ensembl:ENSG00000140505 | |
| UGT2B7 | GeneProduct | ncbigene:7364 | |
| SULT1E1 | GeneProduct | ensembl:ENSG00000109193 | |
| SULT1A1 | GeneProduct | ensembl:ENSG00000196502 | |
| FMO1 | GeneProduct | ensembl:ENSG00000010932 | |
| CYP2E1 | GeneProduct | ensembl:ENSG00000130649 | |
| FMO3 | GeneProduct | ensembl:ENSG00000007933 | |
| UGT1A4 | GeneProduct | ncbigene:54657 | |
| CYP1B1 | GeneProduct | ensembl:ENSG00000138061 | |
| UGT1A8 | GeneProduct | ncbigene:54576 | |
| CYP1A1 | GeneProduct | ensembl:ENSG00000140465 | |
| CYP2C8 | GeneProduct | ensembl:ENSG00000138115 | |
| UGT2B15 | GeneProduct | ensembl:ENSG00000196620 |
References
- Fourteenth Gaddum Memorial Lecture. A current view of tamoxifen for the treatment and prevention of breast cancer. Jordan VC. Br J Pharmacol. 1993 Oct;110(2):507–17. PubMed Europe PMC Scholia
- Quaternary ammonium-linked glucuronidation of tamoxifen by human liver microsomes and UDP-glucuronosyltransferase 1A4. Kaku T, Ogura K, Nishiyama T, Ohnuma T, Muro K, Hiratsuka A. Biochem Pharmacol. 2004 Jun 1;67(11):2093–102. PubMed Europe PMC Scholia
- Quaternary ammonium-linked glucuronidation of trans-4-hydroxytamoxifen, an active metabolite of tamoxifen, by human liver microsomes and UDP-glucuronosyltransferase 1A4. Ogura K, Ishikawa Y, Kaku T, Nishiyama T, Ohnuma T, Muro K, et al. Biochem Pharmacol. 2006 Apr 28;71(9):1358–69. PubMed Europe PMC Scholia
- Chemoprevention of breast cancer with selective oestrogen-receptor modulators. Jordan VC. Nat Rev Cancer. 2007 Jan;7(1):46–53. PubMed Europe PMC Scholia
- New insights into the metabolism of tamoxifen and its role in the treatment and prevention of breast cancer. Jordan VC. Steroids. 2007 Nov;72(13):829–42. PubMed Europe PMC Scholia
- Potential role of UGT pharmacogenetics in cancer treatment and prevention: focus on tamoxifen. Lazarus P, Blevins-Primeau AS, Zheng Y, Sun D. Ann N Y Acad Sci. 2009 Feb;1155:99–111. PubMed Europe PMC Scholia