阿非昔芬
外觀
![]() | |
臨床資料 | |
---|---|
商品名 | TamoGel |
其他名稱 | 4-羥基他莫昔芬、4-OHT、4-HT、OHTAM |
給藥途徑 | 外用(凝膠) |
識別資訊 | |
| |
CAS號 | 68392-35-8 ![]() |
PubChem CID | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.163.120 |
化學資訊 | |
化學式 | C26H29NO2 |
摩爾質量 | 387.52 g·mol−1 |
3D模型(JSmol) | |
| |
|
阿非昔芬(INN:afimoxifene),也叫4-羥基他莫昔芬(簡稱4-OHT),是三苯乙烯基的選擇性雌激素受體調節劑(SERM),也是他莫昔芬的活性代謝物。[1][2][3]該藥物正在開發中,暫定品牌為TamoGel,作為治療乳腺增生的外用凝膠。[1][4]它已經完成了針對周期性乳腺痛的II期臨床試驗,[5]但阿非昔芬獲批用於該適應症並上市之前還需要進一步研究。[4]
阿非昔芬是一種SERM,因此可作為雌激素受體ERα和ERβ的組織選擇性激動劑或拮抗劑,根據組織的不同,具有混合的雌激素和抗雌激素活性。它也是G蛋白偶聯雌激素受體(GPER)的激動劑,具有相對較低的親和力(100-1,000 nM,對比雌二醇的3-6 nM)。[6]除了其雌激素和抗雌激素活性外,阿非昔芬還被發現可作為雌激素相關受體ERRβ和ERRγ的拮抗劑。[7][8][9]
參考資料
[編輯]- ^ 1.0 1.1 Afimoxifene - BHR Pharma. AdisInsight. Springer Nature Switzerland AG.
- ^ Desta Z, Ward BA, Soukhova NV, Flockhart DA. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. The Journal of Pharmacology and Experimental Therapeutics. September 2004, 310 (3): 1062–1075. PMID 15159443. S2CID 21413981. doi:10.1124/jpet.104.065607.
- ^ Statement on a nonproprietary name adopted by the USAN council: Afimoxifene (PDF). American Medical Association. [2008-03-26].
- ^ 4.0 4.1 Goyal A, Mansel RE. Mastalgia. Jatoi I, Rody A (編). Management of Breast Diseases. Springer. 16 November 2016: 77–. ISBN 978-3-319-46356-8.
- ^ Mansel R, Goyal A, Nestour EL, Masini-Etévé V, O'Connell K. A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women. Breast Cancer Research and Treatment. December 2007, 106 (3): 389–397. PMID 17351746. S2CID 22382077. doi:10.1007/s10549-007-9507-x.
- ^ Prossnitz ER, Arterburn JB. International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacological Reviews. July 2015, 67 (3): 505–540. PMC 4485017
. PMID 26023144. doi:10.1124/pr.114.009712.
- ^ Levine AC. Hormones and Cancer: Breast and Prostate, An Issue of Endocrinology and Metabolism Clinics of North America. Elsevier Health Sciences. 3 October 2011: 271–. ISBN 978-1-4557-1239-7.
- ^ Khetan SK. Anti-Androgenic Chemicals. Endocrine Disruptors in the Environment. Wiley. 23 May 2014: 104–. ISBN 978-1-118-89115-5.
- ^ Ariazi EA, Jordan VC. Estrogen-related receptors as emerging targets in cancer and metabolic disorders. Current Topics in Medicinal Chemistry. 2006, 6 (3): 203–215. PMID 16515477. doi:10.2174/1568026610606030203.