| Hazard Information | Back Directory | [Description]
Corifollitropin is a follicle-stimulating hormone (FSH) receptor agonist
that was approved as an infertility treatment in the European
Union in 2010. FSH belongs to the gonadotropin family of glycoproteins that are excreted
from the pituitary gland by gonadotrope cells. Other members include
thyroid-stimulating hormone (TSH), luteinizing hormone (LH), and
human chorionic gonadotropin (hCG). TSH and LH are produced in
the pituitary gland, whereas hCG is produced in the placenta. The
gonadotropins all have a dimeric structure in which the a-subunit is a
shared, nearly identical, substructure, and the glycosylated b-subunit is
varied and is responsible for receptor selectivity. Since the 1990s, rFSH has been employed. A unique approach developed by Boime and his research group involved using the carboxy peptide terminus (CPT) of the b-chain of hCG to increase the half-life of FSH, while maintaining the b-chain of FSH to confer selectivity and potency for the FSH receptor. These hybrid glycopeptides were produced using recombinant DNA methods in Chinese Hamster Ovary (CHO) cells. One of the analogs produced from this effort was corifollitropin alfa. Corifollitropin has been compared to rFSH both in vitro and in vivo. Corifollitropin binds to the FSH receptor with equal potency compared to rFSH. | [Originator]
N.V. Organon (Netherlands) | [Uses]
Corifollitropin alfa (Org 36286) is a long-acting recombinant follicle-stimulating hormone (FSH) analog. Corifollitropin alfa is a FSH Receptor agonist with an EC50 of 5.0 pM. Corifollitropin alfa stimulates ovulation and can be used in the research of infertility[1][2][3]. | [Brand name]
Elonva | [in vivo]
Corifollitropin alfa (20 μg/kg, s.c., single injection) shows a t1/2 of 17.3 h and Cmax of 3.2 ng/mL/μg/kg in female Wistar rats[2].
Corifollitropin alfa (2.5-40 μg/kg, s.c.) stimulates superovulation in rats[2].
Corifollitropin alfa (3 μg, supplemented with hCG, s.c.) increases ovulation rate and recovered embryos in rabbits[3].
| Animal Model: | Rats[2] | | Dosage: | 2.5, 5, 10, 20, 40 μg/kg. | | Administration: | Subcutaneous injection (s.c), four injections given on 2 subsequent days (0, 8, 24, and 32 h). | | Result: | Increased the number of ovulated oocytes, reached maximal value at 20 μg/kg. |
| [References]
[1] Loutradis D, et al. Corifollitropin alfa, a long-acting follicle-stimulating hormone agonist for the treatment of infertility. Curr Opin Investig Drugs. 2009 Apr;10(4):372-80. PMID:19337959
[2] Verbost P, et al. Pharmacologic profiling of corifollitropin alfa, the first developed sustained follicle stimulant. Eur J Pharmacol. 2011 Jan 25;651(1-3):227-33. DOI:10.1016/j.ejphar.2010.10.078
[3] Viudes-de-Castro MP, et a. A single injection of corifollitropin alfa supplemented with human chorionic gonadotropin increases follicular recruitment and transferable embryos in the rabbit. Reprod Domest Anim. 2019 Apr;54(4):696-701. DOI:10.1111/rda.13411 |
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