Drug intelligence / Profile preview

buserelin + megestrol acetate

Development stage
Preclinical
Lead developer
Hoechst
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intranasal
01

Overview

Buserelin + megestrol acetate is a combination of two pharmaceutical agents used primarily in the management of hormone-responsive cancers, particularly metastatic breast cancer. Buserelin is a potent luteinizing hormone-releasing hormone (LHRH) agonist that suppresses gonadotropin release, leading to reduced production of ovarian and testicular steroids such as estrogen and testosterone. This results in decreased stimulation of hormone-dependent tumor growth[4][1]. Megestrol acetate is a synthetic progestin with antineoplastic activity; it acts by interfering with the hormonal environment required for certain cancers to grow, exerting both anti-estrogenic and direct antiproliferative effects on tumor cells[5][7][10]. The combination has been studied for its potential to enhance endocrine blockade in advanced or metastatic breast cancer, especially when other hormonal therapies are insufficient or not tolerated[1].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)PR (Progesterone receptor)AR (Adrenergic receptors)PXR (Pregnane X receptor)

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