Goserelin

Goserelin
Cat. No.
BT16264
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by:
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
Usage
THE BioTek's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
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Description

Goserelin contains 10 amino acids Glu1-His2-Trp3-Ser4-Tyr5-D-Ser(tBu)6-Leu7-Arg8-Pro9-AzGly10-NH2 and having a molecular weight of 1269.43 Dalton.

Product Specs

Introduction
Goserelin is a synthetic hormone that mimics the natural gonadotropin-releasing hormone (GnRH) produced by the hypothalamus gland. It is classified as a GnRH agonist and is utilized in the treatment of prostate and breast cancer. Goserelin exerts its therapeutic effect by reducing the production of estrogen and testosterone hormones. This hormonal modulation helps manage endometriosis and breast cancer by suppressing their growth. Additionally, Goserelin can assist in thinning the uterine lining before surgical interventions. By reducing testosterone levels, Goserelin provides a treatment approach for prostate cancer.
Description
Goserelin is a decapeptide, meaning it consists of ten amino acids. Its amino acid sequence is: Glu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-AzGly-NH2. The molecular weight of Goserelin is 1269.43 Daltons.
Physical Appearance
Goserelin is supplied as a sterile, white powder that has been lyophilized (freeze-dried).
Formulation
The Goserelin peptide was lyophilized without the addition of any other substances.
Solubility
To reconstitute the lyophilized Goserelin, it is recommended to dissolve it in sterile 18MΩ-cm H2O at a concentration of at least 100 µg/ml. Once reconstituted, it can be further diluted in other aqueous solutions.
Stability
Lyophilized Goserelin remains stable at room temperature for up to 3 weeks; however, it should be stored in a dry environment below -18°C. After reconstitution, Goserelin should be stored at 4°C for 2-7 days. For longer-term storage, it is recommended to freeze it below -18°C. To enhance stability during long-term storage, consider adding a carrier protein like 0.1% HSA or BSA. Avoid repeated freeze-thaw cycles.
Purity
The purity of Goserelin is greater than 98.0%, as determined by: (a) Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) analysis and (b) Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE) analysis.

Product Science Overview

Chemical Structure and Properties

Goserelin is a decapeptide, meaning it consists of ten amino acids. Its chemical formula is C59H84N18O14, and it has a molar mass of approximately 1269.43 g/mol . The structure of goserelin includes modifications to the natural GnRH decapeptide to inhibit rapid degradation, making it more effective for therapeutic use .

Mechanism of Action

Goserelin works by overstimulating the body’s production of certain hormones, which leads to a temporary shutdown of that production. Specifically, it stimulates the pituitary gland to produce luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in a non-pulsatile manner. This disrupts the hormonal feedback systems, resulting in the down-regulation of testosterone and estrogen production .

Medical Uses

Goserelin is used to treat hormone-sensitive cancers, including:

  • Prostate Cancer: It lowers testosterone levels, which can shrink the prostate cancer or stop it from growing .
  • Breast Cancer: In pre- and peri-menopausal women, it reduces estrogen levels, which can help manage hormone-sensitive breast cancer .

Additionally, goserelin is used to treat certain benign gynecological disorders such as endometriosis, uterine fibroids, and for endometrial thinning .

Administration

Goserelin is administered as a small pellet injected under the skin (subcutaneously) of the abdomen. The pellet releases the drug slowly as it dissolves. It is available in different formulations, typically administered every 4 weeks or every 12 weeks, depending on the specific treatment regimen .

History and Development

Goserelin was patented in 1976 and approved for medical use in 1987 . It is included in the World Health Organization’s List of Essential Medicines, highlighting its importance in a basic health system .

Side Effects

Common side effects of goserelin include hot flashes, sexual dysfunction, and injection site reactions. More serious side effects can include bone thinning and cardiovascular issues .

Goserelin represents a significant advancement in the treatment of hormone-sensitive cancers, providing an effective means to manage and control the progression of these diseases.

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THE BIOTEK
THE BioTek is a global biotech company offering highly purified proteins for research in cancer, apoptosis, development, endocrinology, immunology, neuroscience, proteases, and stem cells.
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