【中文品名】阿巴瑞克 【药效类别】抗肿瘤药>GnRH拮抗剂类 【通用药名】ABARELIX 【别　　名】R-3827，PPI-l490, Plenaxis 【化学名称】 D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl- 【CA登记号】[183552-38-7] 【结 构 式】 【分 子 式】 【分 子 量】 【收录药典】 -------------------------------------------------------------------------------- 【简　　介】 ABARELIX是一个促性腺素释放激素(GnRH)拮抗剂。最先由美国Praecis制药公司研制开发，现已在欧洲进行了用于前列腺癌治疗的III期临床实验。在美国也正在进行用于子宫内膜异位症治疗的临床实验。该药曾用代号为R-3827和PPI-l490。 体外实验表明，ABARELIX对促黄体激素释放素(LHRH)受体具有高亲和性(KD＝1nmol/L)，是LHRH的完全拮抗剂。该药与LHRH受体结合后，能阻断D-His6-GNRH的激动作用。体外大鼠腹膜巨噬细胞实验还证明，此化合物具有微弱的组胺释放活性，EC50为100mg/ml。此外，ABARELIX易溶于水。所有实验结果均证明，ABARELIX在阻断性激素生成方面具有潜在疗效。 Plenaxis® (abarelix) is our lead product. It is the first in a new class of hormonal products to treat advanced and metastatic prostate cancer. Plenaxis® is a a gonadotrophin-releasing hormone receptor (GnRH) blocker and it works by direct blockade of the GnRH receptors, resulting in a rapid and sustained reduction in testosterone levels and rapid and sustained disease control. As a result, Plenaxis® is the first antagonist hormonal for managing prostate cancer that overcomes the need for anti-androgen co-prescribing. It has a rapid onset and offset of action, leading to fast and profound PSA and prostate volume reduction. Clinical studies have shown that no hormonal surge or clinical flare occurs with Plenaxis® (unlike with agonist hormonal therapy), the efficacy is equal to the combined use of an agonist and anti-androgen and the effects on testosterone are reversible on stopping treatment. Plenaxis® is available in Germany and roll out across Europe is planned following the approval of the drug in eleven additional EU Countries in August 2010.