Leuprorelin Human

Leuprolide Human
Cat. No.
BT16604
Source
Synonyms
Leuprolide, Leuprorelin.
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by RP-HPLC.
Usage
Prospec'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

Leuprolide Human Synthetic is a single, non-glycosylated, polypeptide chain containing 9 amino acids and having a molecular mass of 1209 Dalton. The molecular formula is C59H84N16O12.

Product Specs

Introduction
Leuprorelin, also known as leuprolide acetate, belongs to the gonadotropin-releasing hormone agonist (GnRH agonist) class of medications. Its mechanism involves continuous stimulation of pituitary GnRH receptors, initially leading to a surge in hormone production (flare) followed by a decrease in the secretion of gonadotropins, specifically luteinizing hormone (LH) and follicle-stimulating hormone (FSH), by the pituitary gland (downregulation). Leuprorelin shares similarities with other GnRH agonists and finds application in various medical scenarios. These include treating hormone-sensitive cancers like prostate and breast cancer, managing estrogen-dependent conditions such as endometriosis and uterine fibroids, addressing precocious puberty, and regulating ovarian stimulation during in vitro fertilization (IVF).
Description
Leuprolide Human Synthetic consists of a single polypeptide chain that lacks glycosylation. It comprises 9 amino acids, resulting in a molecular weight of 1209 Daltons. The chemical formula for Leuprolide Human Synthetic is C59H84N16O12.
Physical Appearance
The appearance of this product is a white powder that has been sterilized through filtration and lyophilized (freeze-dried).
Formulation
To prepare the lyophilized form of Leuprorelin, a concentrated solution (1mg/ml) is subjected to the lyophilization process. Notably, this process is carried out without the addition of any other substances.
Solubility
To reconstitute the lyophilized Leoprolide, it is advisable to dissolve it in sterile 18MΩ-cm H2O at a concentration not lower than 100µg/ml. This solution can be further diluted using other aqueous solutions if required.
Stability
Lyophilized Leoprolide demonstrates stability at room temperature for a duration of 3 weeks. However, it is recommended to store it in a desiccated state below -18°C. Once reconstituted, Leuprorelin should be stored at 4°C for a period of 2-7 days. For extended storage, it is advisable to store it below -18°C. To ensure optimal long-term storage, consider adding a carrier protein such as 0.1% HSA or BSA. It is important to avoid subjecting the product to repeated freeze-thaw cycles.
Purity
Using RP-HPLC (Reverse Phase High Performance Liquid Chromatography) analysis, the purity of this product is determined to be greater than 98.0%.
Synonyms
Leuprolide, Leuprorelin.
Amino Acid Sequence
pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt.

Product Science Overview

Chemical Structure and Mechanism of Action

Leuprolide is a peptide-based GnRH receptor superagonist. It is a synthetic 9-residue peptide analogue of GnRH, containing a single D-amino acid (D-leucyl) residue. This modification increases its circulating half-life from approximately three to four minutes to about three hours . By binding to the GnRH receptor (GnRHR), leuprolide induces downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for its clinical efficacy .

Clinical Uses

Leuprolide is used for various medical conditions, including:

  • Prostate Cancer: It is used for the palliative treatment of advanced prostate cancer .
  • Breast Cancer: It helps in managing hormone-responsive breast cancer .
  • Endometriosis: Leuprolide is used to alleviate symptoms of endometriosis .
  • Uterine Fibroids: It is used in combination with iron supplementation for the preoperative hematological improvement of anemic patients with uterine leiomyomata .
  • Central Precocious Puberty (CPP): It is used in pediatric patients to manage early onset puberty .
Administration and Dosage

Leuprolide is administered via injection, either intramuscularly or subcutaneously. The dosage and frequency of administration depend on the condition being treated. For instance, it can be given as a daily subcutaneous injection or as a long-acting intramuscular or subcutaneous product that can be dosed once every six months .

Side Effects and Precautions

Common side effects of leuprolide include hot flashes, unstable mood, trouble sleeping, headaches, and pain at the injection site . Other potential side effects may include high blood sugar, allergic reactions, and problems with the pituitary gland . It is important to note that use during pregnancy may harm fetal development .

Historical Background

Leuprolide was first patented in 1973 and approved for medical use in the United States in 1985 . Since its initial approval, various formulations have been developed to improve patient compliance and convenience . It is also listed on the World Health Organization’s List of Essential Medicines, highlighting its importance in healthcare .

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