Goserelin Acetate

Goserelin Acetate, goserelin; goserelin api; goserelin supplier

Goserelin Acetate

4141427

Regulatory Documentation

CAS-Number

65807-02-5 (net), 145781-92-6 (acetate)

Synonyms

Goserelin
Goserelina
(D-Ser(tBu)6,Azagly10)-LHRH

Sequence

Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH2 acetate salt

WHAT IS GOSERELIN? 

Goserelin acetate is a synthetic peptide of 10 amino-acids sold under the brand name

Zoladex®. It belongs to the family of the GnRH agonist (gonadotropin-releasing hormone) like leuprolide or triptorelin among others. It acts in the pituitary gland to repress the expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It is primarily used in the treatment of certain hormone-sensitive conditions, such as prostate cancer, breast cancer, and certain gynecological conditions. 

HOW DOES GOSERELIN WORK?

Goserelin mechanism of action 

Goserelin, being a synthetic GnRH agonist, emulates the functions of GnRH in the pituitary gland by stimulating the release of LH and FSH. LH and FSH are pivotal messengers directing the production of sex hormones testosterone in males and oestradiol in females.  

Goserelin is administered via sub-cutaneous implant and because of the continuous administration, it desensitizes the pituitary gland receptors. This desensitization gradually leads to a reduction in LH and FSH production by the pituitary gland. From this sustained decrease in the secretion of LH and FSH, it results in a noteworthy reduction in testosterone for males and oestradiol for females. 

For what is Goserelin used? 

The hormonal suppression of goserelin has the following therapeutic applications:  

  • In prostate cancer, which is often hormone-sensitive, reducing testosterone levels can help slow down the growth of cancer cells.  
  • In certain gynecological conditions, such as endometriosis, suppressing oestradiol production can alleviate symptoms associated with these conditions.  
  • In breast cancer, which can be influenced by oestradiol, goserelin may be used to suppress its growth. 

WHAT ARE THE APPLICATIONS OF GOSERELIN? 

Initially marketed as a daily injection in 1987, goserelin acetate is sold under the brand name Zoladex® as an implant administered subcutaneously on a monthly or three monthly basis.

 

Zoladex® has also been approved by FDA for use in combination with the antiandrogen agent flutamide in prostate cancer and can be used in combination with tamoxifen and an aromatase inhibitor in breast cancer. 

Company 

Molecule 

Branded Product 

Dosage/Strength 

Indication 

AstraZeneca 

goserelin acetate 

Zoladex®  

  • 3.6 mg 
  • 10.8 mg 
  • Prostate Cancer 
  • Breast Cancer 
  • Endometriosis 

TerSera Therapeutics 

goserelin acetate 

Zoladex®  

  • 3.6 mg 
  • 10.8 mg 
  • Prostate Cancer 
  • Breast Cancer 
  • Endometriosis 

HOW IS GOSERELIN PRODUCED? 

Goserelin, like all others GnRH analogues, is synthesized via liquid-phase peptide synthesis (LPPS). As shown in the picture below, GnRH analogues possess a common segment conferring significant advantages when it comes to the manufacturing of these APIs. LPPS enables a convergent approach and offers a better cost efficiency, consistent quality, faster synthesis and secured supply chain. 

Generic Api Production

Benefit from extensive experience in generic API manufacturing

 

With extensive background in the production of GMP-grade peptides, we are specialized in the large-scale manufacturing and supply of high-quality GnRH agonists, commonly known as relins. Utilizing liquid-phase synthesis (LPPS), we annually deliver hundreds of kilograms of relin APIs for these essential medicines. As a pioneer and leader in the market, we deeply understand the paramount importance of experience, efficiency, quality and sustainability. 

To ensure that your GnRH agonists meet the highest standards, we prioritize quality at every step of the manufacturing process and are additionally offering an optimized production process. Embracing the principles of sustainability, we not only meet industry standards but exceed them, making a positive impact on both the environment and our customers’ experiences. 

 

From complex to simple: Bachem is your partner of choice 

 

Recognizing the pivotal elements of time, regulatory compliance, and quality in achieving your success, we have tailored our offerings accordingly. We are dedicated to delivering customer-centric services to enhance and simplify your life.  

Our customers enjoy the advantages of prompt delivery from our stocked inventory, accelerated registration facilitated by readily available Drug Master Files (DMFs) and Certificates of Suitability to the monographs of the European Pharmacopoeia (CEPs), and a comprehensive impurity service. In addition to these benefits, our committed team provides robust regulatory support, fostering a partnership that prioritizes our customers’ regulatory success. Our all-encompassing service includes an evolving catalog of impurities, ensuring we meet the dynamic needs of our customers throughout their regulatory journey. 

List of impurities and related products: 

 

Product Number 

Name 

Sequence 

4039400 

(Des-Gly¹⁰,D-Ser(tBu)⁶,Pro-NHNH₂⁹)-LHRH 

Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHNH₂ 

4035303 

(D-His²,D-Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-D-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4047922 

(D-Ser⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser-Tyr-D-Ser-Leu-Arg-Pro-Azagly-NH₂ 

4054732 

(Ser(Ac)⁴,D-Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser(Ac)-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4035307 

(Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser-Tyr-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4038252 

(D-Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4073798 

(D-Ser(tBu)⁶,Azagly¹⁰)-LHRH (free base) 

Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4037082 

(D-Ser(tBu)⁶,D-Leu⁷,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-D-Leu-Arg-Pro-Azagly-NH₂ 

4035304 

(D-Ser⁴,D-Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-D-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

4035302 

(D-Tyr⁵,D-Ser(tBu)⁶,Azagly¹⁰)-LHRH 

Pyr-His-Trp-Ser-D-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH₂ 

You can find these impurities here

Fields of Application

Advanced hormone-dependent prostate cancer
Advanced hormone-dependent breast cancer
Endometriosis
Uterine myoma
Use in reproductive medicine

Active Substance

Goserelin Acetate is a potent GnRH (LHRH) agonist. After a transient increase, continuous administration of goserelin results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

Molecular Information

Molecular Formula

C59H84N18O14

Relative Molecular Mass

1269.43 g/mol

Long-term Storage

-20 ± 5°C

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