Drug intelligence / Profile preview

gonadotropin releasing hormone agonist + progesterone

Development stage
Phase 4
Lead developer
Takeda
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Peptides
Administration
Intramuscular, Subcutaneous, Intranasal, Oral
01

Overview

This is a combination therapy consisting of a gonadotropin-releasing hormone (GnRH) agonist and a progestogen (progesterone or synthetic progestin). GnRH agonists are synthetic analogs of the natural hypothalamic hormone that initially stimulate, then suppress, pituitary secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased production of sex steroids such as estrogen and testosterone. Chronic administration results in hypoestrogenism. Progesterone or progestins are added as "add-back" therapy to mitigate the side effects associated with low estrogen levels, such as bone loss and vasomotor symptoms, without significantly reducing the efficacy of GnRH agonists in suppressing ovarian function. This combination is used primarily for conditions like endometriosis, severe premenstrual syndrome (PMS), uterine fibroids, polycystic ovary syndrome (PCOS), and sometimes for ovarian suppression in breast cancer management[1][2][5][6][7].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)PR (Progesterone receptor)

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