Leuprolide provides a medical castration for the patient and deprives hormonally-dependent tumors of testosterone or estrogen. During short-term or intermittent therapy, leuprolide has the same stimulatory action as GnRH, but long-term therapy suppresses gonadotropin release from the pituitary gland and reduces steroidogenesis in the ovaries and testicles. Normally, GnRH is released in a pulsatile fashion, but the sustained activity of leuprolide leads to downregulation of the receptor and decreased production of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). In the male, this activity stops testosterone production in the testis. In the female, it stops estrogen production in the ovaries. In patients with endometriosis, this reversible hypoestrogenic state produces symptomatic relief of the pain of endometriosis and decreases the number of endometriotic lesions. Initially, there is a surge of FSH and LH, which can cause a flare reaction in prostate or breast carcinoma. Eventually, the flare reaction will diminish.
Leuprolide appears in the following formulation and dosage:
Lupron (IR) suspension for injection – 5mg/ml
Lupron Depot - 4 month powder for susp. Inj. – 30mg/vial
1 month powder for sus. Inj – 3.75, 7.5 mg/vial
3 month powder for susp. Inj. – 11.25,2.5 mg/vial
General data on Leuprolide Active Pharmaceutical Ingredient
CAS Registry: 53714-56-0
ATC: L02AE02
Molecular Formula: C59H84N16O12
Molecular Weight: 1209.4
Pharmacopoeias:In Eur.
Ph. Eur. 5.5: Leuprorelin is a synthetic nonapeptide analogue of the hypothalamic peptide gonadorelin. It is obtained by chemical synthesis and is available as an acetate. Leuprorelin is a white or almost white, hygroscopic, powder.
TAPI's Leuprolide Active Pharmaceutical Ingredient
TAPI's Leuprolide Active Pharmaceutical Ingredient is produced in Assia Industries Limited –Teva Tech site in Beer Sheva, Israel.
Over the last 15 years TAPI has developed the expertise in developing and commercialization of peptide Active pharmaceutical ingredients, such as Leuprolide. With numerous worldwide approvals, we are continuously driven by the goal of helping our customers achieve success-and ultimately approval for their peptide APIs. We offer grams to hundred kilograms production capabilities, comprehensive technology platform including solid phase, solution phase, and hybrid approach, combined with a well established scientific experience, enabling the implementation of efficient process aimed for high quality product. We offer Custom Synthesis and Manufacturing services on peptide Active pharmaceutical ingredients.
TAPI provide full service on Leuprolide and other APIs in our portfolio. Our local sales offices provide full information on our product, regulatory compliance and documentation on Leuprolide.
Other products, in the group of ANTINEOPLASTIC AGENTS - Hormone agonists and related agents available on TAPI's portfolio are:
Goserelin Acetate and Letrozole. Contact us today for information on these products.
2008 Available DMF: EU CTD, CEP and Japan DMF.
