Table 1. List of anticancer drugs metabolized by glucuronidation.
| Drug | Class | UGT enzyme | Ref. |
|---|---|---|---|
| ABT-751 | Antimitotic agent | UGT1A1, UGT1A4, UGT1A8 (major) and UGT2B7 [187] | [187-189] |
| Anastrozole | Aromatase inhibitor | UGT1A4 [190] | [190,191] |
| Dasatinib | Tyrosine kinase inhibitor | Unknown | [192] |
| Desmethyl arzoxifene and 4′F-desmethyl arzoxifene |
Benzothiophene selective estrogen receptor modulators |
Unknown | [193] |
| 5,6-dimethylxanthenone-4- acetic acid |
Vascular-disrupting agent | UGT1A9 and UGT2B7 (major) [194] | [194-197] |
| Doxorubicin | Anthracycline | Unknown | [198] |
| Epirubicin | Anthracycline | UGT2B7 [148] | [146-149,199-204] |
| Erlotinib | Tyrosine kinase inhibitor | Unknown | [205] |
| Etoposide | Topoisomerase II inhibitor | UGT1A1 [206,207] | [206,207] |
| Flavopiridol | Cyclin-dependent kinase inhibitor |
UGT1A1, UGT1A4, UGT1A9 (major) and UGT1A10 [170,171] |
[75,167,170,171] |
| Flutamide | Nonsteroidal anti-androgen drug |
UGT1A1 and UGT1A6 (major) [208] | [208] |
|
N-(2-hydroxyethyl)-3,5- dinitrobenzamide 2-mustard prodrugs: SN 27858 (PR-140A), SN 29546, SN 27686 and SN 29893 |
Dinitrobenzamide mustards | Unknown | [209] |
| Indisulam | Multitargeted cell-cycle inhibitor |
Unknown | [210,211] |
| Lasofoxifene | Selective estrogen receptor modulator |
UGT1A1, UGT1A3, UGT1A6, UGT1A8, UGT1A9 and UGT1A10 [212] | [212] |
| 2-methoxyestradiol | Angiogenesis inhibitor | Unknown | [213] |
| NU/ICRF 505 | Topoisomerase I inhibitor | UGT1A1, UGT1A8, UGT1A9 (main enzyme for tyrosine glucuronide formation), UGT1A10 and UGT2B7 (main enzyme for O-glucuronide formation) [214,215] |
[214-216] |
| Raloxifene | Selective estrogen receptor modulator |
UGT1A1 (main enzyme for 6-glucuronide formation), UGT1A3, UGT1A8, UGT1A9 (major enzyme for 4′-glucuronide formation), UGT1A10 and UGT2B7 [136-138] |
[134, 136-139, 217,218] |
| SN-38 (active metabolite of irinotecan) |
Topoisomerase I inhibitor | UGT1A1 (major), UGT1A3, UGT1A6, UGT1A7 and UGT1A9 [16-22,215] |
[16-22,215] |
| Sorafenib | Tyrosine protein kinase inhibitor |
UGT1A9 [304] | [304] |
| Tamoxifen | Anti-estrogen | UGT1A4 for N-glucuronidation of tamoxifen and 4-hydroxytamoxifen [112,114,115,119]; UGT1A1, UGT1A8 UGT1A9, UGT1A10, UGT2B7, UGT2B15 for O-glucuronidation of 4-hydroxytamoxifen and endoxifen [113,115,116] |
[110-117,119,120] |
| TAS-103 | Topoisomerase I and II inhibitor |
UGT1A1 [174] | [174,175,219] |
| Tipifarnib | Farnesyltransferase inhibitor | Unknown | [220,221] |
| Topotecan | Topoisomerase I inhibitor | Unknown | [222] |
| Vorinostat | Histone deacetylase inhibitor | UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B7 and UGT2B17 (major) [164,165] |
[164,165] |
UGT: Uridine 5′-diphosphoglucuronosyltransferase.