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奥拉帕尼Olaparib原是英国生物技术公司KuDOS Pharmaceuticals的药物,2005年阿斯利康将KuDOS公司收购后,继续开发。2014年12月19日阿斯利康的抗癌药奥拉帕尼(olaparib,商品名:Lynparza)“死而复生”,欧盟委员会(EC)已批准Lynparza作为一种单药疗法,用于铂敏感复发性BRCA突变卵巢癌成人患者的维持治疗,该药也成为用于BRCA突变铂敏感复发性卵巢癌的*PARP抑制剂。
奥拉帕尼(Olaparib)是一种创新的、*口服多聚ADP核糖聚合酶(PARP)抑制剂,PARP可修复DNA损伤,在DNA损伤修复与细胞凋亡中发挥着重要作用。通常DNA双链断裂如果得不到修复,可触发细胞死亡。健康的细胞由于有多条修复断裂DNA的信号通路,PARP抑制剂对其影响不大,而癌细胞发生的一些特定突变,对PARP抑制敏感。PARP与广泛的肿瘤类型相关,这种作用模式,赋予奥拉帕尼治疗具有DNA修复缺陷的广泛肿瘤类型的潜力。尤其是乳腺癌和卵巢癌。2009年《新英格兰医学杂志》和2010年《柳叶刀》杂志均公布药物Olaparib在治疗乳腺癌、卵巢癌及前列腺癌时效果显着。
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Olaparib
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Olaparib Impurity 1
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Olaparib Impurity 2
3-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid
Olaparib Impurity 3
3-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzonitrile
Olaparib Impurity 4
3-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile
Olaparib Impurity 5
2-fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile
Olaparib Impurity 6
2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzonitrile
Olaparib Impurity 7
2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid
Olaparib Impurity 8
2-methoxy-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid
Olaparib Impurity 9
2-methoxy-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzonitrile
Olaparib Impurity 10
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-methoxybenzyl)phthalazin-1(2H)-one
Olaparib Impurity 11
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-hydroxybenzyl)phthalazin-1(2H)-one
Olaparib Impurity 12
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzoyl)phthalazin-1(2H)-one
Olaparib Impurity 13
4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Olaparib Impurity 14
2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzamide
Olaparib Impurity 15
4-(3-(4-acetylpiperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Olaparib Impurity 16
4-(3-(4-butyrylpiperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Olaparib Impurity 17
4-(4-fluoro-3-(4-propionylpiperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Olaparib Impurity 18
4-(4-fluoro-3-(4-isobutyrylpiperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Olaparib Impurity 19
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-5-fluorobenzyl)phthalazin-1(2H)-one
Olaparib Impurity 20
4-(5-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-2-fluorobenzyl)phthalazin-1(2H)-one
Olaparib Impurity 21
2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzohydrazide
Olaparib Impurity 22
3-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzylidene)isobenzofuran-1(3H)-one
Olaparib Impurity 23
4-(3-(4-(cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)-1,2-dihydrophthalazin-1-yl cyclopropanecarboxylate
Olaparib Impurity 24
4-(4-fluoro-3-(4-pivaloylpiperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Olaparib Impurity 25
4,4'-(((piperazine-1,4-dicarbonyl)bis(4-fluoro-3,1-phenylene))bis(methylene))bis(phthalazin-1(2H)-one)