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奧拉帕尼Olaparib原是英國生物技術(shù)公司KuDOS Pharmaceuticals的藥物，2005年阿斯利康將KuDOS公司收購后，繼續(xù)開發(fā)。2014年12月19日阿斯利康的抗癌藥奧拉帕尼（olaparib，商品名：Lynparza）“死而復(fù)生”，歐盟委員會（EC）已批準(zhǔn)Lynparza作為一種單藥療法，用于鉑敏感復(fù)發(fā)性BRCA突變卵巢癌成人患者的維持治療，該藥也成為用于BRCA突變鉑敏感復(fù)發(fā)性卵巢癌的*PARP抑制劑。 
奧拉帕尼（Olaparib）是一種創(chuàng)新的、*口服多聚ADP核糖聚合酶（PARP）抑制劑，PARP可修復(fù)DNA損傷，在DNA損傷修復(fù)與細(xì)胞凋亡中發(fā)揮著重要作用。通常DNA雙鏈斷裂如果得不到修復(fù)，可觸發(fā)細(xì)胞死亡。健康的細(xì)胞由于有多條修復(fù)斷裂DNA的信號通路，PARP抑制劑對其影響不大，而癌細(xì)胞發(fā)生的一些特定突變，對PARP抑制敏感。PARP與廣泛的腫瘤類型相關(guān)，這種作用模式，賦予奧拉帕尼治療具有DNA修復(fù)缺陷的廣泛腫瘤類型的潛力。尤其是乳腺癌和卵巢癌。2009年《新英格蘭醫(yī)學(xué)雜志》和2010年《柳葉刀》雜志均公布藥物Olaparib在治療乳腺癌、卵巢癌及前列腺癌時(shí)效果顯著。 

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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)