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      無債一身輕,無病一生福 求勞拉替尼3922哪里購買?購買價格多少錢一個月?威bxyzxq

    1. 采購類型:現貨/標準
    2. 詢價日期:2019-06-08
    3. 聯系方式: 報價后可見
    4. 分享到:
      針對基因突變的靶向藥,肺癌相對其他腫瘤來說,算是比較多的。EGFR突變是非小細胞肺癌中最為常見突變類型。目前臨床上用于EGFR突變的靶向藥物包括易瑞沙(吉非替尼)、阿法替尼(2992)、奧西替尼(AZD9291)等。EGFR“黃金突變”的肺癌患者是被大多數人羨慕的,因為意味著這部分患者有更多選擇,可以服用副作用較低的一代EGFR-TKI類藥物,免去放化療的痛苦。  

          “鉆石突變”也是名副其實,該靶點的靶向藥定價都很高,超出很多癌癥患者家庭的承受范圍。但忽略價格,ALK基因融合突變也是幸運的,一方面因為已經有多種靶向藥獲批用于治療該靶點突變的肺癌患者,且療效并不亞于“黃金突變”對應藥物的效果;另一方面幸運的,是在三代ALK抑制劑勞拉替尼(3922)耐藥后(如果是存在L1198F導致的耐藥),能重新用回一代藥克唑替尼,這是其他基因突變都無法實現的有效輪回用藥!

          一、克唑替尼——第一代ALK抑制劑

          上市情況:2011年8月,美國FDA正式批準輝瑞的克唑替尼作為ALK陽性NSCLC靶向治療藥物,也是第一個獲得FDA批準的ALK陽性NSCLC靶向治療藥物。

          臨床效果:克唑替尼治療ALK陽性的非小細胞肺癌客觀緩解率達60%,無進展生存期為8-10個月,相比于化療顯著改善并延長的總生存期。

          不良反應:常見的有皮疹、腹瀉、惡心嘔吐、食欲不振、肝功能異常等,不良反應嚴重程度也因個體差異而不同。

          色瑞替尼的活性是克唑替尼的20倍,對于ALK+肺癌患者可一線使用,也可在克唑替尼耐藥后使用。

          中國上市情況:尚未在中國獲批上市。

          值得注意的是,細胞水平的研究表明,色瑞替尼對克唑替尼耐藥性細胞有明顯的抑制作用,其對耐藥突變L1196M、G1269A、I1171T和S1206Y抑制作用明顯,但對G1202R和F1174C突變無效。

          三、艾樂替尼

          上市情況:2015年12月,美國FDA批準羅氏的艾樂替尼上市,用于克唑替尼耐藥或者副作用不耐受的ALK融合的肺癌患者,作為二代ALK+抑制劑;2017年11月7日,美國FDA批準艾樂替尼用于一線治療ALK陽性的轉移性非小細胞肺癌患者。

          臨床效果:根據三期臨床試驗(代號ALEX)結果,艾樂替尼VS克唑替尼:艾樂替尼組的有效率是82.9%,包括4%的患者腫瘤完全消失;克唑替尼組的有效率75.5%,1%的患者腫瘤完全消失。艾樂替尼組的無進展生存期是25.7個月,克唑替尼組只有10.4個月。

          不良反應:最常見不良反應(發生率≥20%)是疲乏,便秘,水腫和肌痛

          一種新型的ALK和EGFR雙重抑制劑,可強效抑制ALK的L1196M突變和EGFR的T790M突變。

          中國上市情況:尚未在中國獲批上市。

          值得注意的是,90mg劑量組則有1個病人達到完全緩解CR。在90mg劑量組,中位無進展時間PFS為9.2個月。180mg劑量組較90mg劑量組的患者,疾病進展或死亡的風險降低45%。

          五、勞拉替尼

          勞拉替尼在輝瑞看來是ALK靶點的二代靶向藥(一代是克唑替尼),但是從整體來看,勞拉替尼又屬于三代,因為二代已經被色瑞替尼、艾樂替尼、AP26113這些所占據。

          中國上市情況:尚未在中國獲批上市。

          值得注意的是,這其中先前服用過一種ALK靶向藥的ALK陽性患者的ORR達到57%,先前服用過至少兩種ALK靶向藥的ALK陽性患者的ORR達到42%,并且有入腦效果。

          另外,輝瑞針對勞拉替尼Lorlatinib的III期臨床CROWN(NCT03052608)也在近期開展。這是一個持續的、開放標簽、隨機、雙臂的研究,主要比較Lorlatinib和克唑替尼(Crizotinib)一線治療轉移性ALK+非小細胞癌患者的療效。

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