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<p>建立内容为“{{drugbox | Verifiedfields = changed | UNII_Ref = {{fdacite|changed|FDA}} | UNII = X78UG0A0RN| verifiedrevid = 407466945 | IUPAC_name = &#039;&#039;N&#039;&#039;-(2-chloro-6-methylph…”的新页面</p> <p><b>新页面</b></p><div>{{drugbox<br /> | Verifiedfields = changed<br /> | UNII_Ref = {{fdacite|changed|FDA}}<br /> | UNII = X78UG0A0RN| verifiedrevid = 407466945<br /> | IUPAC_name = ''N''-(2-chloro-6-methylphenyl)-2-&lt;nowiki&gt;[[&lt;/nowiki&gt;6-[4-(2-hydroxyethyl)-&lt;br&gt;1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole&lt;br&gt;carboxamide monohydrate<br /> | image = Dasatinib.svg<br /> | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}= {{chemspidercite|correct|chemspider}}<br /> | ChemSpiderID = 2323020<br /> | InChI1 = 1/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)<br /> | InChIKey1 = ZBNZXTGUTAYRHI-UHFFFAOYAC<br /> | smiles = Cc1cccc(c1NC(=O)c2cnc(s2)Nc3cc(nc(n3)C)N4CCN(CC4)CCO)Cl<br /> | ChEMBL_Ref = {{ebicite|correct|EBI}}<br /> | ChEMBL = 1421<br /> | StdInChI_Ref = {{stdinchicite|correct|chemspider}}= {{stdinchicite|correct|chemspider}}<br /> | StdInChI = 1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)<br /> | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}= {{stdinchicite|correct|chemspider}}<br /> | StdInChIKey = ZBNZXTGUTAYRHI-UHFFFAOYSA-N<br /> | CAS_number = 302962-49-8<br /> | ATC_prefix = L01<br /> | ATC_suffix = XE06<br /> | PubChem = 3062316<br /> | DrugBank = <br /> | C = 22 | H = 26 | N = 7 | O = 2 | S = 1 | Cl = 1<br /> | molecular_weight = 488.01 g/mol<br /> | bioavailability = <br /> | protein_bound = 96%<br /> | metabolism = [[Liver|Hepatic]]<br /> | elimination_half-life = 1.3 to 5 hours<br /> | excretion = Fecal (85%), [[kidney|renal]] (4%)<br /> | licence_EU = Sprycel<br /> | licence_US = Dasatinib<br /> | pregnancy_AU = D<br /> | pregnancy_US = D<br /> | legal_US = Rx-only<br /> | routes_of_administration = Oral<br /> }}<br /> '''达沙替尼'''（{{lang-en|Dasatinib}}），此前亦称'''BMS-354825'''，是一种由[[百时美施贵宝]]生产并以“{{lang|en|Sprycel}}”为名义销售的一种[[癌症]]治疗药物。达沙替尼是一种针对[[费城染色体]]（{{lang|en|Philadelphia chromosome}}）和SRC[[基因]]（{{lang|en|Src Gene}}）[[变异]]的[[酪氨酸激酶抑制剂]]，其主要用于[[伊马替尼]]（{{lang|en|imatinib}}）治疗后期的[[慢性粒细胞性白血病]]（{{lang|en|chronic myelogenous leukemia}}）以及费城染色体呈阳性的急性髓性[[白血病]]（{{lang|en|Ph+ ALL}}）患者。该药也被证明可治疗许多其他类型的癌症，包括加速期的[[前列腺癌]]&lt;ref&gt;{{cite journal | author = Das J ''et al.'' | title = 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-&lt;nowiki&gt;[[&lt;/nowiki&gt;6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor | journal = J Med Chem | volume = 49 | issue = 23 | pages = 6819–32 | year = 2006 | pmid = 17154512 | doi = 10.1021/jm060727j}}&lt;/ref&gt;。<br /> <br /> == 详情 ==<br /> <br /> ===[[药物作用]]===<br /> <br /> 在2006年6月的[[临床试验]]中，达沙替尼是提供予对使用伊马替尼而产生[[抗药性]]和依赖性的患者&lt;ref name=&quot;pmid16775234&quot;&gt;{{cite journal |author=Talpaz M, Shah NP, Kantarjian H, ''et al.'' |title=Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias |journal=N. Engl. J. Med. |volume=354 |issue=24 |pages=2531–41 |year=2006 |month=June |pmid=16775234 |doi=10.1056/NEJMoa055229 |url=http://content.nejm.org/cgi/pmidlookup?view=short&amp;amp;pmid=16775234&amp;amp;promo=ONFLNS19}}&lt;/ref&gt;，40例慢性期慢性粒细胞性白血病患者中的37名在服用后达到了完成[[血液]]反应标准；而44例的[[加速期慢性粒细胞性白血病]]患者中有31例达到标准。<br /> <br /> ===[[分子]]靶位===<br /> <br /> 达沙替尼主要是针对费城染色体、SRC基因、c-Kit、复合弗[[激酶]]以及其他[[酪氨酸激酶]]，但并不针对EGFR、Her2等erbB激酶。<br /> <br /> ===药效===<br /> <br /> 在慢性期的慢性粒细胞性白血病患者中有95%的病例能够平均随访时间中保持在在12个月以上药效。在加速期的患者中，82%的患者得以缓解，尽管平均随访时间只有五个月。几乎所有的急变期患者或费城染色体数值全部阳性的患者，都在6个月内恢复数值。<br /> <br /> ===受影响的基因群===<br /> <br /> 除了T315I[[基因突变]]以外，所有的费城染色体基因群都受到药物反应。<br /> <br /> ===[[副作用]]与[[毒性]] ===<br /> <br /> 中性[[白细胞增多]]和[[骨髓抑制]]（[[白细胞减少]]）是比较普遍的[[毒性反应]]。服用该药中的18%患者，会犯有并发性的[[胸膜]][[积液]]。一些病人会需要做[[胸腔穿刺术]]或[[胸膜固定术]]去治疗这种疾患。其他严重的反应包括有中型的[[腹泻]]、外周性的[[水肿]]和[[头疼]]。少数患者在[[肝功能试验]]中显示异常。而极少低血钙症副作用也被指明，但是其并未证明会导致任何严重问题。<br /> <br /> ==参考==<br /> <br /> {{reflist|2}}<br /> <br /> ==外部链接==<br /> *[http://www.fda.gov/cder/foi/nda/2006/021986_022072_SprycelTOC.htm Summary Basis for Approval from the U.S. Food and Drug Administration Freedom of Information homepage]<br /> *[http://www.dasatinib.com/ Prescribing information from Bristol-Myers Squibb]<br /> *[http://www.newcmldrug.com/diary_interface/Results/Diary.asp Diary of a CML patient involved in the clinical trials for dasatinib]<br /> *[http://www.emea.europa.eu/humandocs/PDFs/EPAR/sprycel/H-709-PI-en.pdf Sprycel Summary of Product Characteristics] (from the European Medicines Agency website)<br /> {{Extracellular chemotherapeutic agents}}<br /> <br /> [[Category:鸦片类药物]]<br /> <br /> [[Category:酪氨酸激酶抑制剂]] [[Category:噻唑]] [[Category:哌嗪]] [[Category:百时美施贵宝]] [[Category:抗癌药物]] [[Category:嘧啶]] [[Category:酰替苯胺]]<br /> ==参考来源==<br /> *[http://zh.wikipedia.org/wiki/%E8%BE%BE%E6%B2%99%E6%9B%BF%E5%B0%BC 维基百科-达沙替尼]</div>

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