UROFOLLITROPIN

Chemical Properties

Almost white or slightly yellowish powder.

Uses

Hormone (follicle-stimulating).

brand name

Bravelle (Ferring Pharmaceuticals); Fertinex (Serono); Metrodin (Serono).

Clinical Use

Urofollitropin, a natural product like the menotropins, is obtained from the urine of postmenopausal women and then highly purified so as to contain only FSH, reportedly with only minute amounts of LH. Urofollitropin is used for its ability to stimulate follicle development, such as in women undergoing drug-induced pituitary suppression (GnRH antagonist or superagonist) for purposes of IVF (i.e., multiple follicle development or egg donation). When the number and size of the ovarian follicles are correct, as determined by ultrasound, hCG is administered so as to effect ovulation, and the oocytes are retrieved for IVF.
This drug also is indicated for women who have infertility caused by polycystic ovary syndrome, which generally is observed clinically as enlarged, cystic ovaries containing relatively small follicles. These patients often develop hirsutism, their androgen and LH levels appear elevated while their FSH levels are low, and the early exposure to these improper hormone levels may be causing the follicular atresia. The patient's monthly cycle is controlled by previous pituitary suppression via treatment with a GnRH superagonist or antagonist; urofollitropin, as an exogenous source of FSH, is administered and stimulates follicle maturation to preovulatory size, with little or no exposure of the follicles to additional LH. When the follicles have matured to preovulatory size, ovulation is assisted by the administration of hCG. The couple is then advised to engage in sexual intercourse daily, beginning on the day before hCG administration and until ovulation has occurred.

Synthesis

A method for the preparation of UROFOLLITROPIN, the preparation method is easy to operate, the production cost is low, and the urinary follicle stimulating hormone obtained is more pure and free of contamination from exogenous proteins. the FSH specific activity is greater than 10,000 IU/mg of protein, and the LH:FSH potency is less than 1:100. the method for the preparation comprises the following steps: (1) Human menopausal gonadotropin crude product is purified by anion exchange chromatography to obtain urinary follicle stimulating hormone intermediate I; (2) Urofolliculin intermediate I was purified by cation exchange chromatography to obtain urofolliculin intermediate II; (3) Urofolliculin intermediate II was purified by dye affinity chromatography to obtain urofolliculin intermediate III; (4) Urofolliculin intermediate III was purified by hydrophobic chromatography to obtain a solution of high purity urofolliculin;

in vivo