词条 | Trioxifene |
释义 |
| IUPAC_name = [2-(4-methoxyphenyl)-3,4-dihydronaphthalen-1-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone | image = Trioxifene.png | width = 250 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 63619-84-1 | CAS_supplemental = 68307-81-3 (mesylate) | ATC_prefix = none | ATC_suffix = | PubChem = 50139 | ChemSpiderID = 45471 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = R0130F043H | synonyms = LY-133,314 | C=30 | H=31 | N=1 | O=3 | molecular_weight = 453.57 g/mol }}Trioxifene (INN) (developmental code name LY-133,314), or as the salt trioxifene mesylate (USAN), is a selective estrogen receptor modulator (SERM) with competitive binding activity against estradiol for the ERα and antagonistic activity against ERα-mediated gene expression, that was under preclinical and clinical development by Eli Lilly and Company for breast cancer and prostate cancer,[1] but was abandoned.[2]{{rp|11}}[3][4] References1. ^{{cite journal |vauthors=Neubauer BL, McNulty AM, Chedid M, Chen K, Goode RL, Johnson MA, Jones CD, Krishnan V, Lynch R, Osborne HE, Graff JR |title=The selective estrogen receptor modulator trioxifene (LY133314) inhibits metastasis and extends survival in the PAIII rat prostatic carcinoma model |journal=Cancer Research |volume=63 |issue=18 |pages=6056–62 |date=September 2003 |pmid=14522935 |doi= }} {{Estrogen receptor modulators}}{{antineoplastic-drug-stub}}2. ^Philipp Y. Maximov, Russell E. McDaniel, V. Craig Jordan. Tamoxifen: Pioneering Medicine in Breast Cancer. Milestones in Drug Therapy. Springer Science & Business Media, 2013. {{ISBN|9783034806640}} 3. ^{{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA1252|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=1252–}} 4. ^{{cite book|author1=I.K. Morton|author2=Judith M. Hall|title=Concise Dictionary of Pharmacological Agents: Properties and Synonyms|url=https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA281|date=6 December 2012|publisher=Springer Science & Business Media|isbn=978-94-011-4439-1|pages=281–}} 6 : Abandoned drugs|Aromatic ketones|Pyrrolidines|Selective estrogen receptor modulators|Phenol ethers|Phenols |
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