Drug intelligence / Profile preview

oral contraceptive + leuprolide

Development stage
Preclinical
Lead developer
Abbott
Modality
Small Molecules
Administration
Intramuscular, Oral, Subcutaneous
01

Overview

This is a combination therapy consisting of an oral contraceptive (typically a combined estrogen-progestin formulation) and leuprolide, a gonadotropin-releasing hormone (GnRH) agonist. Oral contraceptives suppress ovulation and stabilize endometrial tissue through negative feedback on the hypothalamic-pituitary-ovarian axis, while leuprolide acts as a potent inhibitor of gonadotropin release, leading to decreased estrogen production. This combination may be used in the management of endometriosis-associated pelvic pain or for menstrual suppression in specific clinical scenarios. The rationale for combining these agents is to maximize suppression of ovarian function and control symptoms such as pain or abnormal bleeding[1][6][8]. Leuprolide is also commonly used with norethindrone acetate as "add-back" therapy to mitigate hypoestrogenic side effects; however, the use with combined oral contraceptives is less common but has been studied[1].

02

Targets

PR (Progesterone receptor)ESR1 (ERα)GnRHR (Gonadotropin-releasing hormone receptor)

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