What is leuprolide acetate?

Leuprolide, also known as leuprorelin, is a synthetic agonist analog of gonadotropin-releasing hormone (GnRH), repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It is used to treat prostate cancer, breast cancer, endometriosis, uterine fibroids and central precocious puberty (CPP). Leuprolide is a short peptide consisting of nine amino acids.

How does leuprolide work?

Leuprolide mechanism of action (MOA)

Leuprolide is a synthetic analog of GnRH, a hormone produced by the hypothalamus in the brain. Leuprolide MOA regulates the production of sex hormones, including luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

When applied as subcutaneous injection, leuprolide MOA initially start with the stimulation of the pituitary gland in the brain to release LH and FSH, just like natural GnRH. This stimulation prompts the pituitary gland to release LH and FSH, which are the messengers that signal the testes in males and the ovaries in females to produce sex hormones, such as testosterone and oestradiol.

However, with continued administration of leuprolide, a process known as “downregulation” occurs. This means that the pituitary gland becomes less responsive to the constant GnRH-like signals generated by leuprolide.

As a result of this desensitization, LH and FSH production by the pituitary gland decreases over time. Since LH and FSH are crucial for stimulating the production of sex hormones, their reduction leads to a significant decrease in the production of testosterone in males and oestradiol in females.

Ultimately, the diminished production of sex hormones leads to a state of hypogonadism, where the levels of testosterone or oestradiol in the body drops significantly below the normal range. This controlled reduction of sex hormones is the desired therapeutic outcome in various conditions. For example, in prostate cancer, lowering testosterone levels can slow the growth of cancer cells, while in conditions like endometriosis and uterine fibroids, it can reduce symptoms associated with excess oestradiol.

What are the applications of leuprolide?

Initially marketed as a daily injection in 1985, a new long-acting formulation was developed and commercialized four years later for monthly injection. Leuprolide is now sold under different brand names:

A new salt form has been developed, leuprolide mesylate, and is sold under the brand name Camcevi®. This new form is the first-ever ready-to-inject sterile formulation of leuprolide mesylate and comes in a pre-filled syringe, where no mixing is required anymore.

How is leuprolide produced?

Benefit from extensive experience

We leverage our extensive proficiency in the production of gonadorelin analogs driven by the synergies within the synthesis of these relin products. We go the extra mile and enables our customers to reap the rewards of an optimized process.

From complex to simple: Bachem is your partner of choice

We provide customer-centric services designed to streamline and improve our customer’s lives. From our rich experience, we understand that time, regulatory assistance, and quality are crucial factors for our customers’ success. 

Our customers benefit from swift delivery of our readily available stock, expedited registration through already available DMFs and CEPs, and comprehensive impurity management. Moreover, our dedicated team offers robust regulatory support, coupled with an all-around service offering an evolving catalog of impurities.

List of impurities and related products:

CEP, DMF

Leuprorelin; (Des-Gly10,D-Leu6,Pro-NHEt9)-LHRH

Leuprorelina

Leuprorelina acetato

Leuproreline

Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt

Molecular Formula

C₅₉H₈₄N₁₆O₁₂

Relative Molecular Mass

1209.5 (net)

CAS-Number

53714-56-0 (net), 74381-53-6 (acetate)

Long-term Storage

-20 ± 5°C

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