卡培他滨治疗和DPYD基因型。

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凯恩院长L, M

卡培他滨治疗和DPYD基因型。

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PubMed ID

28520372 (在PubMed

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文摘

卡培他滨(品牌Xeloda)是一个属于药物化疗剂类fluoropyrimidines。广泛用于治疗结肠癌等恶性肿瘤,转移性结直肠癌,转移性乳腺癌。卡培他滨是一种前体药物,保持酶的转化为活性形式,氟尿嘧啶(也称为5 -氟尿嘧啶),它充当一个抗代谢物减缓肿瘤的生长。DPYD基因编码dihydropyrimidine脱氢酶(DPD),一种酶,这种酶催化的病原反应一步氟尿嘧啶新陈代谢。80 - 90%的5 -氟尿嘧啶Dihydropyrimidine脱氢酶灭活(研究者用)5,6-dihydro-fluorouracil。DPYD基因的遗传变异可导致酶减少或没有活动。非功能性的人至少有一个副本(例如,c DPYD变体。1905 + 1 g >(原* 2;rs3918290)或c。1679 t > G (p.I560S;以前* 13; rs55886062)) will not be able to metabolize fluorouracil at normal rates. Consequently, these individuals are at risk of potentially life-threatening fluorouracil toxicity, such as bone marrow suppression, gastrointestinal toxicity and, rarely, neurotoxicity. The prevalence of DPD partial deficiency varies in different populations but is approximately 3-5%. There is an FDA-approved antidote for 5-FU overdose: uridine triacetate. Overdose can occur in individuals with partial DPD deficiency taking either capecitabine or 5-FU. The FDA-approved drug label for capecitabine states that no capecitabine dose has been proven safe in individuals with absent DPD activity, and that there is insufficient data to recommend a specific dose in individuals with partial DPD activity as measured by any specific test (Table 1) (1). The Clinical Pharmacogenetics Implementation Consortium (CPIC) and the Dutch Pharmacogenetics Working Group (DPWG) have published dosing recommendations for fluoropyrimidines (capecitabine and fluorouracil) based on DPYD genotype (Tables 2 and 3). Both recommendations include dose reductions for intermediate metabolizers (with reduced enzyme activity), and avoiding fluorouracil and choosing an alternative agent for poor metabolizers (with absent enzyme activity) (2, 3, 4).

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药物

卡培他滨