Prevost R R
Department of Pharmacy, Celebration Health, Florida Hospital Health Systems, 34747, USA.
Pharmacotherapy. 1998 Sep-Oct;18(5):1001-10.
The frequency of infertility in developed countries is approximately 8-10%. New drugs are available for assisted reproduction techniques. Two recombinant follicle-stimulating hormone (FSH) products, follitropin-beta (Follistim in the United States, Puregon in Europe) and follitropin-alpha (Gonal-F), join compounds derived through transfecting nonhuman cell lines with genetic material capable of replicating identical amino acid sequences to human compounds. The cell line used for recombinant (r)-FSH production is the Chinese hamster ovary (CHO). Previously, the only agents that showed benefit in controlled ovulatory stimulation were derived from the urine of menopausal women. Those compounds contain additional substances, such as urinary proteins and various amounts of luteininzing hormone. The amino acid sequence of r-FSH is identical to that of human FSH, but the two recombinant products exist in many different isoforms and differ from each other and from human FSH due to varied carbohydrate side chains. Due to variation in the carbohydrate side chains, follitropin-beta in solution has a higher pH than urine-derived FSH, which enhances receptor affinity and therefore is a greater inducer of folliculogenesis. Follitropin-beta does not cause endogenous production of anti-CHO or anti-FSH antibodies, and is well tolerated.
发达国家的不孕不育发生率约为8%-10%。辅助生殖技术有了新的药物。两种重组促卵泡激素（FSH）产品，促卵泡素β（在美国为Follistim，在欧洲为Puregon）和促卵泡素α（Gonal-F），加入了通过用能够复制与人类化合物相同氨基酸序列的遗传物质转染非人类细胞系而获得的化合物。用于生产重组（r）-FSH的细胞系是中国仓鼠卵巢（CHO）细胞系。以前，在控制性排卵刺激中显示出益处的唯一药物来自绝经后妇女的尿液。这些化合物含有其他物质，如尿蛋白和不同量的促黄体生成素。r-FSH的氨基酸序列与人类FSH相同，但这两种重组产品存在许多不同的异构体，由于碳水化合物侧链不同，它们彼此之间以及与人类FSH都有所不同。由于碳水化合物侧链的差异，溶液中的促卵泡素β的pH值高于尿源性FSH，这增强了受体亲和力，因此是卵泡生成的更强诱导剂。促卵泡素β不会引起内源性抗CHO或抗FSH抗体的产生，并且耐受性良好。
