Drug intelligence / Profile preview

leuprorelin + exemestane

Development stage
Unknown
Lead developer
International Breast Cancer Study Group
Modality
Peptides, Small Molecules
Administration
Intramuscular, Subcutaneous, Oral
01

Overview

Leuprorelin + exemestane is a combination therapy used primarily in premenopausal women with hormone receptor-positive breast cancer and is under investigation for other hormone-driven cancers such as recurrent adult-type granulosa cell tumor of the ovary. Leuprorelin (also known as leuprolide) is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function by downregulating pituitary GnRH receptors, leading to decreased secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn reduces estrogen production from the ovaries. Exemestane is an aromatase inhibitor that blocks the conversion of androgens to estrogens in peripheral tissues, further reducing circulating estrogen levels. This dual approach achieves profound estrogen deprivation, which inhibits the growth of estrogen-dependent tumors[2][5][6]. The combination has been shown to be effective for adjuvant treatment after surgery or chemotherapy in premenopausal women with ER-positive breast cancer, especially those at higher risk of recurrence[5][6]. It may also be used off-label or investigated for other indications where ovarian suppression plus aromatase inhibition could provide benefit.

Brand names
Lupron Depot
Other names
Depo Lupron + aromatase inhibitorleuprolide depot + aromatase inhibitorGnRH agonist + aromatase inhibitor
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CYP19A1 (Aromatase)

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