| 词条 | Apaziquone |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 457134883 | IUPAC_name = (E)-5-(1-Azirinyl)-3-(hydroxymethyl)-2-(3-hydroxy-1-propenyl)-1-methyl-1H-indole-4,7-dione | image = Apaziquone.svg | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Investigational New Drug | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 114560-48-4 | ATC_prefix = None | ATC_suffix = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 73822 | PubChem = 5813717 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4710342 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = H464ZO600O | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D02965 | C=15 | H=16 | N=2 | O=4 | molecular_weight = 288 g/mol | smiles = Cn1c(c(c2c1C(=O)C=C(C2=O)N3CC3)CO)/C=C/CO | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C15H16N2O4/c1-16-10(3-2-6-18)9(8-19)13-14(16)12(20)7-11(15(13)21)17-4-5-17/h2-3,7,18-19H,4-6,8H2,1H3/b3-2+ | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = MXPOCMVWFLDDLZ-NSCUHMNNSA-N }} Apaziquone (tentative trade name EOquin)[1] is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases. The active metabolites alkylate DNA and lead to apoptosis.[2] This activity is preferentially expressed in neoplastic cells. After administration of apaziquone directly into the urinary bladder (intravesically), the drug and its active metabolite were not detected in plasma, and there were no systemic side effects.[3][4] Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan for the treatment of superficial (non-muscle invasive) bladder cancer.[3] Approximately 70% of all newly diagnosed patients with bladder cancer have non-muscle invasive bladder cancer and over one million patients in the United States and Europe are affected by the disease. The U.S. Food and Drug Administration (FDA) has granted Fast Track review status to apaziquone for this indication.[5] References1. ^{{cite web|title=UvA researcher develops new bladder cancer medication |date=25 Jul 2007 |publisher=University of Amsterdam |url=http://www.student.uva.nl/eco/actueeleco.cfm/FCE6CA35-1321-B0BE-688CD4EE5D63A36B |deadurl=yes |archiveurl=https://web.archive.org/web/20110716090159/http://www.student.uva.nl/eco/actueeleco.cfm/FCE6CA35-1321-B0BE-688CD4EE5D63A36B |archivedate=2011-07-16 }} 2. ^{{cite web |url=http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=42095 |author=NCI |title=apaziquone| accessdate=2009-06-07| archiveurl= https://web.archive.org/web/20090509182946/http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=42095| archivedate= 9 May 2009 | deadurl= no}} 3. ^1 {{cite journal |vauthors=Puri R, Palit V, Loadman PM |title=Phase I/II pilot study of intravesical apaziquone (EO9) for superficial bladder cancer |journal=J. Urol. |volume=176 |issue=4 Pt 1 |pages=1344–8 |date=October 2006 |pmid=16952628 |doi=10.1016/j.juro.2006.06.047 |url=http://linkinghub.elsevier.com/retrieve/pii/S0022-5347(06)01426-1|display-authors=etal}} 4. ^{{cite journal |vauthors=Hendricksen K, Gleason D, Young JM |title=Safety and side effects of immediate instillation of apaziquone following transurethral resection in patients with nonmuscle invasive bladder cancer |journal=J. Urol. |volume=180 |issue=1 |pages=116–20 |date=July 2008 |pmid=18485407 |doi=10.1016/j.juro.2008.03.031 |url=http://linkinghub.elsevier.com/retrieve/pii/S0022-5347(08)00591-0|display-authors=etal}} 5. ^{{cite web |title=FDA Designates Fast Track Status For Apaziquone (EOquin) For Bladder Cancer |date=22 Jul 2009 |publisher=Medical News Today |url=http://www.medicalnewstoday.com/articles/158443.php}} 4 : Alcohols|Antineoplastic drugs|Aziridines|Indolequinones |
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