Drug intelligence / Profile preview

relugolix + megestrol acetate + medroxyprogesterone acetate

Development stage
Unknown
Lead developer
Myovant Sciences
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

**relugolix + megestrol acetate + medroxyprogesterone acetate** is an investigational combination drug comprised of three active ingredients: relugolix, megestrol acetate, and medroxyprogesterone acetate. - **Relugolix** is a small molecule, oral gonadotropin-releasing hormone (GnRH) receptor antagonist. It acts by competitively inhibiting the GnRH receptor in the anterior pituitary, reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which leads to decreased production of sex hormones (estrogen and testosterone)[4]. - **Megestrol acetate** and **medroxyprogesterone acetate** are synthetic progestins, which act primarily by binding to the progesterone receptor. Their roles in combination with relugolix are likely to provide supportive hormonal control and mitigate potential hypoestrogenic effects[2]. This combination is currently studied for the treatment of **heavy menstrual bleeding associated with uterine fibroids in women**[1]. Mechanistically, this combination seeks both to suppress ovarian hormone production and provide progestin support to balance endocrine effects commonly observed with GnRH antagonism.

02

Targets

3β-HSD (3β-Hydroxysteroid Dehydrogenase/Δ5-4 isomerase type 1)PR (Progesterone receptor)GnRHR (Gonadotropin-releasing hormone receptor)

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