促性腺激素释放激素拮抗剂的 5 年临床应用：安全性和过敏潜力评估。

Five years' clinical use of GnRH antagonists: evaluation of safety and allergic potential.

机构信息

University of Schleswig-Holstein, Department of Gynecology and Obstetrics, University Clinic Hospital, Campus Lübeck, Ratzeburger Allee 160, 23538 Lübeck, Germany.

出版信息

Reprod Biomed Online. 2005 Jun;10 Suppl 3:61-5. doi: 10.1016/s1472-6483(11)60392-1.

DOI:10.1016/s1472-6483(11)60392-1

PMID:23577417

Abstract

Three antagonists of gonadotrophin-releasing hormone are currently clinically available. Cetrorelix (Cetrotide) and ganirelix (Orgalutran/Antagon) have been safely used in assisted reproduction since 1999 and 2000 respectively. The structurally similar abarelix (Plenaxis) has been approved for the therapy of advanced androgen sensitive prostate cancer. However, due to the occurrence of allergic reactions, its use is restricted to only a subgroup of patients. These allergic side effects may not be due to abarelix, as the drug itself does not have a strong histamine liberating potential in vitro, but could be attributed to carboxymethylcellulose (CMC), which only Plenaxis, but not Cetrotide or Orgalutran/Antagon contain. CMC is used to obtain the sustained-release characteristics of Plenaxis. Since 1973, numerous case reports and studies have been published regarding allergic reactions and specific immunoglobulin E antibodies against CMC. Thus, the allergic side effects of Plenaxis could be rather due to CMC than to abarelix.

摘要

目前有三种促性腺激素释放激素拮抗剂可用于临床。西曲瑞克（Cetrotide）和加尼瑞克（Orgalutran/拮抗剂）分别于 1999 年和 2000 年在辅助生殖领域安全使用。结构相似的阿巴瑞克（Plenaxis）已被批准用于治疗晚期雄激素敏感前列腺癌。然而，由于过敏反应的发生，其使用仅限于仅一小部分患者。这些过敏副作用可能不是由于阿巴瑞克引起的，因为该药物本身在体外没有很强的组胺释放潜力，而可能归因于羧甲基纤维素（CMC），只有 Plenaxis，而不是 Cetrotide 或 Orgalutran/拮抗剂含有。CMC 用于获得 Plenaxis 的缓释特性。自 1973 年以来，已经发表了许多关于过敏反应和针对 CMC 的特异性免疫球蛋白 E 抗体的病例报告和研究。因此，Plenaxis 的过敏副作用可能是由于 CMC 而不是阿巴瑞克引起的。