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Gonadorelin Acetate

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CAT#
10-101-19
Synonyms/Alias
GnRH; Gonadotropin-releasing hormone; LHRH; Luteinizing hormone-releasing factor acetate (salt) hydrate; Dirigestran; Fertagyl; Gonadoliberin; Hypocrine; Luliberin; Lutrefact; Relefact; Luforan; Lutamin; Lutal
CAS No.
34973-08-5
Sequence
Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 acetate salt
M.W/Mr.
1242.36
Molecular Formula
C55H75N17O13.C2H4O2
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Gonadorelin is also known as LHRH. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Description
Gonadorelin is a trophic peptide hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is synthesized and released from GnRH neurons within the hypothalamus. The peptide belongs to gonadotropin-releasing hormone family. It constitutes the initial step in the hypothalamic–pituitary–gonadal axis.
Areas of Interest
Hormonal therapy
  • Background
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  • References

Gonadorelin is a synthetic peptide analog of gonadotropin-releasing hormone (GnRH) or luteinizing hormone releasing hormone (LHRH). Gonadorelin acts as an agonist at the GnRH/LHRH receptor, inducing release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This hormone is clinically used to treat endometriosis. Gonadorelin exhibits anti-androgen and anticancer chemotherapeutic activities. In vitro and in vivo, gonadorelin inhibits testosterone activation of androgen receptors. Additionally, gonadorelin increases proliferation of normal cells but inhibits proliferation of prostate cancer cells through a mechanism that involved activation of the ryanodine receptor and increases in intracellular Ca2+ levels.

CAS: 33515-09-2 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 hydrochloride salt
M.W: 1182.31
Molecular Formula: C55H75N17O13
CAS: 83930-13-6 (net)
Sequence: H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH2 acetate salt
M.W: 5039.72
Molecular Formula: C215H358N72O66S
CAS: 76712-82-8 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt acetate salt
M.W: 1323.5
Molecular Formula: C66H86N18O12
CAS: 63968-82-1
Sequence: Asp-Val-Pro-Lys-Ser-Asp-Gln-Phe-Val-Gly-Leu-Met-NH2
M.W: 1334.54
Molecular Formula: C59H95N15O18S
CAS: 74381-53-6
Sequence: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
M.W: 1269.46
Molecular Formula: C59H84N16O12.C2H4O2

Recently, several reports of adverse reactions after pulsatile GnRH (gonadorelin hydrochloride) infusion therapy have appeared in the medical literature. Although the cause of these reactions has been associated with GnRH itself, the contributions of impurities and degradation products in the administered drug have not been determined, suggesting that the use of high-purity material may be advantageous in controlling unwanted side effects. This study evaluates the purity and long-term stability of a new GnRH product, gonadorelin acetate (Lutrepulse, Ortho Pharmaceutical Corporation). Both the purity and potency of the drug substance, the lyophilized product for injection, and the reconstituted material that would be transferred to the infusion pump system were monitored using high-performance liquid chromatography. The gonadorelin acetate drug substance was found to be stable for at least 12 months when stored at 24 degrees C in 50% relative humidity, and showed no degradation even under accelerated storage conditions. Similarly, the lyophilized product also showed excellent stability for at least 18 months when stored at 24 degrees C in 50% relative humidity. Upon reconstitution, gonadorelin acetate was found to be stable for at least 45 days when stored at 24 degrees C or 37 degrees C.

Wong, W., Mercorelli, M., DeLuccia, F., Young, R., Lane, P. A., Hoerig, J., & Turan, A. (1990). Stability and purity profile of gonadorelin acetate: a high-purity gonadotropin-releasing hormone. International journal of fertility, 35(5), 302-309.

Gonadotropin-releasing hormone analogues are generally regarded as safe drugs. Gonadorelin acetate has been widely used for the diagnosis of central precocious puberty, and life-threatening reactions to gonadorelin acetate are extremely rare. Herein, we described - to the best of our knowledge - the first pediatric case in which severe anaphylaxis was encountered after intravenous gonadorelin acetate administration. An 8-year-old girl who was diagnosed with central precocious puberty was receiving triptorelin acetate treatment uneventfully for 6 months. In order to evaluate the efficacy of the treatment, an LH-RH stimulation test with gonadorelin acetate was planned. Within 3 min after intravenous administration of gonadorelin acetate, she lost consciousness and tonic seizures began in her hands and feet. She was immediately treated with epinephrine, diphenhydramine, and fluids. Her vital signs recovered within 30 min. Based on the results, anaphylaxis should be anticipated and the administration of these drugs should be performed in a setting that is equipped to deal with systemic reactions.

Akın, O., Yavuz, S. T., Hacıhamdioğlu, B., Sarı, E., Gürsel, O., & Yeşilkaya, E. (2015). Anaphylaxis to gonadorelin acetate in a girl with central precocious puberty. Journal of Pediatric Endocrinology and Metabolism, 28(11-12), 1387-1389.

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