Tìm theo
Follitropin Alpha
Các tên gọi khác (8 ) :
  • Follitrophin alfa
  • Follitrophin alpha
  • Follitropin alfa
  • Follitropin alpha
  • FSH alpha
  • FSH-a
  • FSH-A
  • rFSH-alpha
Thuốc Gốc
Biotech
CAS: 56832-30-5
Follitropin alpha is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin alpha was the world’s first recombinant human FSH preparation and is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “alpha” differentiates it from another recombinant human FSH product that was marketed later as follitropin beta. Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH.
Dược Lực Học : The main pharmacodynamic parameters are serum inhibin, estradiol and total follicular volume with daily injections of follitropin. The quickest response was noticed with serum inhibin, which declined rapidly after discontinuation. Follicular growth showed late response and continued even after discontinuation of the drug and after decline of the serum concentrations. Thus follicular growth was better correlated with serum inhibin and estradiol rather than peal levels of the drug. It should be noted that there is great inter-individual variability.
Cơ Chế Tác Dụng : Follitropin alpha is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin alpha was the world’s first recombinant human FSH preparation and is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “alpha” differentiates it from another recombinant human FSH product that was marketed later as follitropin beta. Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. Follitropin is important for spermatogenesis, gonadal steroid production and follicule growth and maturation .
Dược Động Học :
▧ Absorption :
The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males.
▧ Volume of Distribution :
No significant difference is expected in the pharmacokinetics in males and females after subcutaneous injections. Studies in healthy females after intravenous administration seem to suggest that the distribution may follow a two-compartment model with a distribution half-life of 2 to 2.5 hours. Steady state concentrations are reached after 4 to 5 days of daily administration.
▧ Route of Elimination :
Via liver and kidneys.
▧ Half Life :
Elimination half-life in healthy female volunteers after subcutaneous injection was 24-53 hours and in males it was 32-41 hours.
▧ Clearance :
Total clearance after IV administration is 0.6L/h and the renal clearance is 0.07L/h.
Độc Tính : Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers.
Chỉ Định : In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF).
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cinnal-f
  • Công ty :
    Sản phẩm biệt dược : Gonal-F
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB09024
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