| 词条 | Orteronel |
| 释义 |
| ImageFile = Orteronel.svg | ImageSize = 200px | IUPACName = 6-(7-Hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methylnaphthalene-2-carboxamide | OtherNames = TAK-700 |Section1={{Chembox Identifiers | CASNo = 566939-85-3 | CASNo_Ref = {{cascite|correct|CAS}} | PubChem = 9883029 | ChemSpiderID = 8058704 | KEGG = D10146 | ChEMBL = 1921976 | KEGG_Ref = {{keggcite|correct|kegg}} | UNII = UE5K2FNS92 | SMILES = O=C(NC)c2ccc1cc(ccc1c2)C4(O)c3cncn3CC4 | InChI = InChI=1S/C18H17N3O2/c1-19-17(22)14-3-2-13-9-15(5-4-12(13)8-14)18(23)6-7-21-11-20-10-16(18)21/h2-5,8-11,23H,6-7H2,1H3,(H,19,22) |Section2={{Chembox Properties | C=18 | H=17 | N=3 | O=2 | Appearance = | Density = | MeltingPt = | BoilingPt = | Solubility = |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = }}Orteronel (TAK-700) is a nonsteroidal CYP17A1 inhibitor that was being developed for the treatment of cancer by Takeda Pharmaceutical Company in conjunction with Millennium Pharmaceuticals.[1] It completed two phase III clinical trials for metastatic, hormone-refractory prostate cancer but failed to extend overall survival rates, and development was voluntarily terminated as a result.[2] Orteronel is an androgen biosynthesis inhibitor. It selectively inhibits the enzyme CYP17A1[3] which is expressed in testicular, adrenal, and prostatic tumor tissues. CYP17 catalyzes two sequential reactions: (a) the conversion of pregnenolone and progesterone to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of dehydroepiandrosterone (DHEA) and androstenedione, respectively, by its 17,20-lyase activity.[4] DHEA and androstenedione are androgens and precursors of testosterone. Inhibition of CYP17 activity thus decreases circulating levels of testosterone. See also
References1. ^Millennium and Takeda Announce Advancement of Prostate Cancer Program, Millennium Pharmaceuticals {{Antiandrogens}}{{Androgenics}}{{drug-stub}}2. ^{{cite web | url = http://www.marketwatch.com/story/takeda-announces-termination-of-orteronel-tak-700-development-for-prostate-cancer-in-japan-usa-and-europe-2014-06-19 | author = MarketWatch | title = Takeda Announces Termination of Orteronel (TAK-700) Development for Prostate Cancer in Japan, U.S.A. and Europe | year = 2014}} 3. ^{{cite journal | pmid = 22249003 | year = 2012 | last1 = Yamaoka | first1 = M | last2 = Hara | first2 = T | last3 = Hitaka | first3 = T | last4 = Kaku | first4 = T | last5 = Takeuchi | first5 = T | last6 = Takahashi | first6 = J | last7 = Asahi | first7 = S | last8 = Miki | first8 = H | last9 = Tasaka | first9 = A | last10 = Kusaka | first10 = Masami | title = Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: Effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys | volume = 129 | issue = 3–5 | pages = 115–28 | doi = 10.1016/j.jsbmb.2012.01.001 | journal = The Journal of Steroid Biochemistry and Molecular Biology| display-authors = 8 }} 4. ^{{cite journal |vauthors=Attard G, Belldegrun AS, de Bono JS | title = Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer | journal = BJU Int. | volume = 96 | issue = 9 | pages = 1241–6 |date=December 2005 | pmid = 16287438 | doi = 10.1111/j.1464-410X.2005.05821.x }} 7 : Abandoned drugs|Carboxamides|CYP17A1 inhibitors|Enzyme inhibitors|Naphthalenes|Nonsteroidal antiandrogens|Takeda Pharmaceutical Company |
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