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::: Imatinib mesylate 甲磺酸伊马替尼 :::

伊马替尼(Imatinib)是一种用于治疗费城染色体(Bcr-Abl)阳性的慢性骨髓性白血病(CML)成人患者的口服药物，伊马替尼(imatinib)是酪氨酸激酶抑制剂，能选择性地抑制慢性髓细胞白血病(CML)患者Bcr-Abl蛋白的酪氨酸激酶活性，从而阻断多条信号传导途径，达到治疗白血病的目的。此外,该药还能抑制c-Kit、血小板源性生长因子受体(PDGFR)、ARG等受体型酪氨酸激酶活性，从而起到抗瘤作用。该药自临床应用以来，已显示出其特异性、高效性和低毒性。

共有1000多名患者参加了这项全球性的Ⅰ期及Ⅱ期临床试验。试验中，患者定期接受骨髓检查、血细胞计数及其它实验室检查。若白细胞计数下降一半，且情况稳定2周，则该患者被认为出现“血液学反应”(hematologic response)；如果白细胞计数低于10000/mm，血小板计数低于450/mm，且稳定时间达到4周，则被认为出现“完全血液学反应”(complete hematologic response)。α干扰素治疗无效的CML慢性期患者在使用Imatinib后有90%的病人持续出现完全血液学反应，超过50%的患者骨髓中的Bcr-Abl完全消失或几乎完全消失；加速期患者的血液学反应和细胞生成反应率也维持在较高水平；即使危象期病人也有近三分之一出现血液学反应。多数患者在治疗过程中可能会出现轻度到中度的药物不良反应。因产生不良反应而中止试验的慢性期、加速期及危象期患者分别占该类患者总数的1%、2%和5%。最常见的不良反应包括恶心、体液潴留、肌肉痛性痉挛、腹泻、呕吐、出血、肌肉骨骼痛、皮疹、头痛、疲劳、关节痛、消化不良、呼吸困难、嗜中性白细胞减少症和血小板减少症。临床试验表明，越早采用Imatinib治疗，疗效越好。

目前，Imatinib已在美国、巴西、瑞士及澳大利亚等35个国家上市。在美国，Imatinib由于疗效确切，只用了32个月就获得上市批准，而普通药物通常需要近6年的时间。目前正在进行的是将Imatinib用于其它肿瘤治疗的试验，预计这个“重磅炸弹”在2005年的年销售额将突破10亿美元。
 
Imatinib is a drug used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec® (USA) or Glivec® (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally still referred to as CGP57148B or STI571 (especially in older publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of simply inhibiting rapidly dividing cells.

Imatinib mesylate is a white to off-white to brownish or yellowish tinged crystalline powder. Its molecular formula is C29H31N7O · CH4SO3 and its molecular weight is 589.7. Imatinib mesylate is soluble in aqueous buffers < pH 5.5 but is very slightly soluble to insoluble in neutral/alkaline aqueous buffers. In non-aqueous solvents, the drug substance is freely soluble to very slightly soluble in dimethyl sulfoxide, methanol and ethanol, but is insoluble in n-octanol, acetone and acetonitrile.

Imatinib Mesylate
Cas Number: 220127-57-1
Chemical name: N-{4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl}nicotinamide methanesulfonate

Imatinib free base [CAS# 152459-95-5] & Intermediates
4-[(4-Methyl-1-piperazinyl)methyl]benzoic acid dihydrochloride hemihydrate
Cas number: 106261-49-8

4-(4-methylpiperazinomethyl)benzoyl chloride dihydrochloride

4-(chloromethyl)-N-4-methyl-3-[(4-(3-pyridinyl)-2-pyrimidinyl)amino]phenylbenzamide
Cas number: 404844-11-7, (404844-10-6 for HCl salt)
N-(5-Amino-2-methyl phenyl)-4-(3-pyridyl)-2-pyrimidineamine
Cas number: 152460-10-1

N-(2-methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidineamine
Cas number: 152460-09-8

2-dimethylamino-1-(3-pyridyl)-2-propene-1-one
Cas number: 55314-16-4 (unspec), 75415-01-9 (Z), 123367-26-0 (E)
2-Methyl-5-nitro phenyl guanidine nitrate
Cas number: 152460-08-7, (152460-07-6 for free base)