MATERIALS AND METHODS FOR TREATING PATIENTS WITH TAXOXIFEN
    1.
    发明申请
    MATERIALS AND METHODS FOR TREATING PATIENTS WITH TAXOXIFEN 审中-公开
    用TAXOXIFEN治疗患者的材料和方法

    公开(公告)号:US20120088247A1

    公开(公告)日:2012-04-12

    申请号:US13202418

    申请日:2010-02-23

    IPC分类号: C12Q1/68

    摘要: A pathway for the metabolism of tamoxifen is identified including the activity of at least 2 different isoforms of UGY2B7. This pathway includes isozymes of CYP3A which convert tamoxifen (TAM) to N-desmethyl-TAM, which is then converted to endoxifen by the action of CYP2D6. Once formed, endoxifen may be degraded by at least one isozyme of UGT2B7. Patients that have highly active isoforms of CYP2D6 and slow acting isoforms of UGT2B7 accumulate high levels of endoxifen and are good candidates for treatment with tamoxifen. Also disclosed are methods for screening patients with a high likelihood of benefiting from treatment with tamoxifen. These methods include testing patients for various alleles of genes known to be involved in tamoxifen metabolism and treating patients accordingly.

    摘要翻译: 确定了他莫昔芬代谢途径,包括UGY2B7至少2种不同同种型的活性。 该途径包括将他莫昔芬(TAM)转化为N-去甲基-TAM的CYP3A同功酶,然后通过CYP2D6的作用将其转化为内毒素。 一旦形成,内皮素可能被UGT2B7的至少一种同功酶降解。 具有CYP2D6高活性同种型和UGT2B7慢作用亚型的患者积累高水平的内皮素,是治疗他莫昔芬的良好候选药物。 还公开了用于筛选可能受益于他莫昔芬治疗的患者的方法。 这些方法包括测试患者已知参与他莫昔芬代谢的基因的各种等位基因,并相应地治疗患者。