| 词条 | Mitoxantrone |
| 释义 |
| verifiedrevid = 462252883 | IUPAC_name = 1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino) ethylamino]-anthracene-9,10-dione | image = Mitoxantrone skeletal.svg | image2 = Mitoxantrone ball-and-stick.png | tradename = Novantrone | Drugs.com = {{drugs.com|monograph|mitoxantrone-hydrochloride}} | MedlinePlus = a608019 | pregnancy_US = D | legal_status = Rx-only | routes_of_administration = Mainly intravenous | bioavailability = n/a | protein_bound = 78% | metabolism = Hepatic (CYP2E1) | elimination_half-life = 75 hours | excretion = Renal | IUPHAR_ligand = 7242 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 65271-80-9 | ATC_prefix = L01 | ATC_suffix = DB07 | PubChem = 4212 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB01204 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4067 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = BZ114NVM5P | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08224 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 50729 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 58 | PDB_ligand = MIX | C=22 | H=28 | N=4 | O=6 | molecular_weight = 444.481 g/mol | SMILES = O=C2c1c(c(NCCNCCO)ccc1NCCNCCO)C(=O)c3c2c(O)ccc3O | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C22H28N4O6/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32/h1-4,23-30H,5-12H2 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = KKZJGLLVHKMTCM-UHFFFAOYSA-N }} Mitoxantrone (INN, BAN, USAN; also known as Mitozantrone in Australia; trade name Novantrone) is an anthracenedione antineoplastic agent. UsesMitoxantrone is used to treat certain types of cancer, mostly metastatic breast cancer, acute myeloid leukemia, and non-Hodgkin's lymphoma. It improves the survival rate of children suffering from acute lymphoblastic leukemia relapse.[1] The combination of mitoxantrone and prednisone is approved as a second-line treatment for metastatic hormone-refractory prostate cancer. Until recently this combination was the first line of treatment; however, a combination of docetaxel and prednisone improves survival rates and lengthens the disease-free period.[2] Mitoxantrone is also used to treat multiple sclerosis (MS), most notably the subset of the disease known as secondary-progressive MS. In the absence of a cure, mitoxantrone is effective in slowing the progression of secondary-progressive MS and extending the time between relapses in both relapsing-remitting MS and progressive-relapsing MS.[3] Side effectsMitoxantrone, as with other drugs in its class, may cause adverse reactions of varying severity, including nausea, vomiting, hair loss, heart damage and immunosuppression, possibly with delayed onset. Cardiomyopathy is a particularly concerning effect as it is irreversible; thus regular monitoring with echocardiograms or MUGA scans is recommended for patients. Because of the risk of cardiomyopathy, mitoxantrone carries a limit on the cumulative lifetime dose (based on body surface area) in MS patients.[4] Mechanism of actionMitoxantrone is a type II topoisomerase inhibitor; it disrupts DNA synthesis and DNA repair in both healthy cells and cancer cells by intercalation[6][7] between DNA bases. See also
References1. ^{{cite journal |vauthors=Parker C, Waters R, Leighton C, Hancock J, Sutton R, Moorman AV, Ancliff P, Morgan M, Masurekar A, Goulden N, Green N, Révész T, Darbyshire P, Love S, Saha V |title=Effect of mitoxantrone on outcome of children with first relapse of acute lymphoblastic leukaemia (ALL R3): an open-label randomised trial |journal=Lancet |volume= 376|issue= 9757|pages= 2009–2017|year=2010 |pmid=21131038 |doi=10.1016/S0140-6736(10)62002-8 |pmc=3010035}} {{Chemotherapeutic agents}}2. ^{{cite book |chapter=Cancer Chemotherapy |author=Katzung, Bertram G. |title=Basic and clinical pharmacology |publisher=McGraw-Hill Medical Publishing Division |location=New York |year=2006 |isbn=0-07-145153-6 |edition=10th |oclc=157011367}} 3. ^{{cite journal |author=Fox E |title=Management of worsening multiple sclerosis with mitoxantrone: a review |journal=Clin Ther |volume=28 |issue=4 |pages=461–74 |year=2006 |pmid=16750460 |doi=10.1016/j.clinthera.2006.04.013}} 4. ^{{cite web|title=Mitoxantrone Hydrochloride (marketed as Novantrone and generics) – Healthcare Professional Sheet text version|url=http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm126445.htm|publisher=U.S. Food and Drug Administration|accessdate=19 September 2014|ref=fdapostmarket}} 5. ^{{Cite journal | last1 = Wu | first1 = C. -C. | last2 = Li | first2 = Y. -C. | last3 = Wang | first3 = Y. -R. | last4 = Li | first4 = T. -K. | last5 = Chan | first5 = N. -L. | title = On the structural basis and design guidelines for type II topoisomerase-targeting anticancer drugs | doi = 10.1093/nar/gkt828 | journal = Nucleic Acids Research | volume = 41 | issue = 22 | pages = 10630–10640 | year = 2013 | pmid = 24038465 | pmc = 3905874}} 6. ^{{cite journal |vauthors=Mazerski J, Martelli S, Borowski E |title=The geometry of intercalation complex of antitumor mitoxantrone and ametantrone with DNA: molecular dynamics simulations |journal=Acta Biochim. Pol. |volume=45 |issue=1 |pages=1–11 |year=1998 |pmid= 9701490|doi= |url=}} 7. ^Kapuscinski J, Darzynkiewicz Z. (1985) Interactions of antitumor agents Ametantrone and Mitoxantrone (Novatrone) with double-stranded DNA.Biochem Pharmacol. 1985;34:4203-13, {{PMID|4074383}} 7 : Topoisomerase inhibitors|IARC Group 2B carcinogens|Alcohols|Aromatic amines|Dihydroxyanthraquinones|Hydroquinones|DNA intercalaters |
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